WO2007054556A1 - Nouvelle pyridopyrazine et son utilisation pour la modulation de kinases - Google Patents

Nouvelle pyridopyrazine et son utilisation pour la modulation de kinases Download PDF

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WO2007054556A1
WO2007054556A1 PCT/EP2006/068322 EP2006068322W WO2007054556A1 WO 2007054556 A1 WO2007054556 A1 WO 2007054556A1 EP 2006068322 W EP2006068322 W EP 2006068322W WO 2007054556 A1 WO2007054556 A1 WO 2007054556A1
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alkyl
heterocyclyl
group
heteroaryl
aryl
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PCT/EP2006/068322
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German (de)
English (en)
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Eckhard Claus
Irene Seipelt
Eckhard Günther
Emmanuel Polymeropoulos
Michael Czech
Tilmann Schuster
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Æterna Zentaris Gmbh
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Priority claimed from EP05024693A external-priority patent/EP1785423A1/fr
Priority to JP2008539443A priority Critical patent/JP5527972B2/ja
Priority to EP06819385A priority patent/EP1957487A1/fr
Priority to CA002628039A priority patent/CA2628039A1/fr
Priority to RU2008123222/04A priority patent/RU2515944C9/ru
Priority to AU2006313701A priority patent/AU2006313701B2/en
Application filed by Æterna Zentaris Gmbh filed Critical Æterna Zentaris Gmbh
Priority to BRPI0618452-9A priority patent/BRPI0618452A2/pt
Priority to KR1020087014068A priority patent/KR101400905B1/ko
Priority to CN2006800507541A priority patent/CN101356173B/zh
Publication of WO2007054556A1 publication Critical patent/WO2007054556A1/fr
Priority to IL191139A priority patent/IL191139A0/en
Priority to NO20082511A priority patent/NO20082511L/no
Priority to HK09104745.1A priority patent/HK1126474A1/en

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Definitions

  • Novel pyridopyrazines and their use as modulators of kinases are novel pyridopyrazines and their use as modulators of kinases.
  • the invention relates to kinase modulators of the pyrido [2,3-b] pyrazine type, to their preparation and use as medicaments for modulating misdirected cellular signal transduction processes, in particular for influencing the function of tyrosine, serine / threonine and lipid kinases and to Treatment of malignant or benign tumors and other diseases based on pathological cell proliferation diseases such.
  • the phosphorylation of proteins is generally initiated by extracellular signals and provides a universal mechanism for the control of various cellular events, such as cell proliferation. As metabolic processes, cell growth, cell migration, cell differentiation, membrane transport and apoptosis. For protein phosphorylation, the protein family of kinases is responsible. These enzymes catalyze the phosphate transfer to specific substrate proteins. Based on substrate specificity, the kinases are divided into three major classes, the tyrosine kinases, the serine / threonine kinases, and the lipid kinases.
  • Both the receptor tyrosine kinases and the cytoplasmic tyrosine, serine / threonine and lipid kinases are important proteins of the signal transduction of the cell. Overexpression or degeneration of these proteins plays an important role in disorders based on pathological cell proliferation. These include metabolic diseases, connective tissue and blood vessel diseases, as well as malignant and benign tumors. They occur in tumor development and development often as oncogenes, ie as aberrant, constitutively active kinase proteins. The consequences of this excessive Kinaseeducation ist are z. For example, uncontrolled cell growth and reduced cell death. The stimulation of tumor-induced growth factors can also be the cause of the overstimulation of kinases. The development of kinase modulators is therefore of particular interest for all pathogenic processes that are influenced by kinases.
  • diseases such as cancer, neurodegeneration and inflammatory diseases
  • the individual components of these signaling cascades represent important therapeutic targets for the intervention of the various disease processes (Weinstein-Oppenheimer CR et al 2000, Chang F. et al., 2003, Katso R. et al., 2001 and Lu Y. et al., 2003).
  • a variety of growth factors, cytokines and oncogenes transduce their growth-promoting signals via activation of G-protein coupled ras, which is used to activate the serine-threonine kinase Raf and to activate mitogen-activated protein kinase kinase 1 and 2 (MAPKK1 / 2 or Mek1 / 2) and in the phosphorylation and activation of MAPK 1 and 2 - also known as Extracellular Signal Regulated Kinase (Erk1 and 2).
  • G-protein coupled ras which is used to activate the serine-threonine kinase Raf and to activate mitogen-activated protein kinase kinase 1 and 2 (MAPKK1 / 2 or Mek1 / 2) and in the phosphorylation and activation of MAPK 1 and 2 - also known as Extracellular Signal Regulated Kinase (Erk1 and 2).
  • the ras-Raf-Mek-Erk pathway combines a large number of proto-oncogenes, including ligands, tyrosine kinase receptors, G proteins, kinases, and nuclear transcription factors.
  • Tyrosine kinases such as EGFR (Menelsohn J. et al., 2000) often mediate constitutive active signals to the downstream ras-Raf-Mek- Erk signaling pathway in tumors due to overexpression and mutation. Ras mutations are mutated in 30% of all human tumors (Khleif SN et al., 1999, Marshall C, 1999), the highest incidence being 90% in pancreatic carcinomas (Friess H.
  • Raf kinases also have Mek-Erk independent, anti-apoptotic functions, whose molecular steps are not yet fully described.
  • Ask1, Bcl-2, Akt and Bag1 have been described as possible interaction partners for the Mek-Erk-independent Raf activity (Chen J et al., 2001, Troppajier J. et al., 2003, Rapp UR et al., 2004, Gotz R. et al., 2005). It is now believed that both Mek-Erk-dependent and Mek-Erk-independent signal transduction mechanisms control the activation of the ras and Raf stimuli located above.
  • the isoenzymes of phosphatidylinositol 3-kinases function predominantly as lipid kinases and catalyze the D3 phosphorylation of second messenger lipids Ptdlns (phosphatidylinositol) to Ptdlns (3) P, Ptdlns (3,4) P 2 , Ptdlns (3,4 , 5) P 3 phosphatidylinositol phosphates.
  • the class I PI3Ks are structurally composed of the catalytic (pHOalpha, beta, gamma, delta) and regulatory (p85alpha, beta or p101gamma) subunits.
  • class II (PI3K-C2alpha, PI3K-C2beta) and class IN (Vps34p) enzymes belong to the family of PI3 kinases (Wymann MP et al., 1998, Van Haesebroeck B. et al., 2001).
  • the PIP increase triggered by PI3Ks activates the proliferative ras-Raf-Mek-Erk signaling pathway via the coupling of ras (Rodriguez-Viciana P.
  • PI3Ks fulfills at least 2 crucial mechanisms of tumorigenesis, namely the activation of cell growth and cell differentiation and the inhibition of apoptosis.
  • the PI3K also have protein-phosphorylating properties (Dhand et al., 1994, Bondeva T. et al., 1998, Bondev A. et al., 1999, Van Haesebroeck B.
  • PI3Ks also have kinase-independent, regulatory effector properties, for example in the control of cardiac contraction (Crackower - A -
  • PI3Kdelta and PI3Kgamma are specifically expressed on hematopoietic cells and thus potential targets for isoenzyme-specific PI3Kdelta and PI3Kgamma inhibitors in the treatment of inflammatory diseases such as rheumatism, asthma and allergies and in the treatment of B- and T- Cell lymphomas (Okkenhaug K. et al., 2003, Ali K. et al., 2004, Sujobert P. et al., 2005).
  • PI3Kalpha which has recently been identified as a proto-oncogene (Shayesteh L.
  • PI3K-related kinases include the serine / threonine kinases mTOR, ATM, ATR, h-SMG-1, and DNA-PK (Chiang G.G. et al., 2004).
  • PIKK PI3K-related kinases
  • Their catalytic domains have high sequence homology to the catalytic domain of the PI3Ks.
  • Phosphorylation contributes to the overactivation of Akt and its downstream cascade components, thus underlining the causal role of PI3K as a target for tumor therapy.
  • the kinase inhibitor Bay 43-9006 (WO 99/32111, WO 03/068223) already in clinical trials shows a relatively nonspecific inhibition pattern of serine / threonine and tyrosine kinases such as Raf, VEGFR2 / 3, Flt-3 , PDGFR, c-Kit and other kinases.
  • This inhibitor is of great importance in angiogenesis-induced advanced tumor diseases (eg in renal cell carcinoma) but also in melanomas with a high B-Raf mutation rate.
  • the clinical effect of Bay 43-9006 is currently also being investigated in patients with refractory solid tumors in combination with eg docetaxel. So far, mild side effects and promising anti-tumoral effects have been described. Inhibition of the kinases in the PI3K-Akt signaling pathway is not described or disclosed for Bay 43-9006.
  • the Mek1 / 2 inhibitor PD0325901 (WO 02/06213) is currently undergoing Phase I clinical trials.
  • the precursor CM 040 (WO 00/35435, WO 00/37141) was noted for its high Mek specificity and target affinity , However, this compound proved to be metabolically unstable in Phase I / II studies.
  • Clinical data of the current successor substance PD0325901 are pending. However, neither an interaction with Erk1 or Erk2, nor a PI3K-Akt signaling pathway inhibiting function or its simultaneous modulation is published or disclosed for this Mek inhibitor.
  • ICOS disclosed a PI3K inhibitor IC87114 with high PI3Kdelta isoenzyme specificity (WO 01/81346).
  • PI103 Yamanouchi / Piramed describe a selectivity versus the PI3Kalpha isoform.
  • a highly regarded research environment exists (see review R. Wetzker et al., 2004).
  • Inhibitors of the SAPK signaling pathway are described in the literature (Gum RJ., 1998, Bennett BL et al 2001, Davies SP et al 2000). However, for these SAPK inhibitors, no PI3Ks-inhibiting function and also no specific inhibition of Erk1 or Erk2 or simultaneous inhibition of SAPKs, Erk1, Erk2, or PI3Ks is disclosed. In the 6- or 7-position substituted pyrido [2,3-b] pyrazine derivatives are widely used as pharmacologically active compounds and as building blocks in pharmaceutical chemistry.
  • patents WO 04/104002 and WO 04/104003 describe pyrido [2,3-b] pyrazines, which may be substituted in the 6- or 7-position by urea, thiourea, amidine or guanidine groups. These compounds possess properties as inhibitors or modulators of kinases, in particular of tyrosine and serine / threonine kinases, and a use as medicaments is indicated. In contrast, a use of these compounds as modulators of lipid kinases, alone or in combination with tyrosine and serine / threonine kinases, is not described.
  • patent WO 99/17759 describes pyrido [2,3-b] pyrazines which carry, inter alia, alkyl, aryl and heteroaryl-substituted carbamates in the 6-position. These compounds will be used to modulate the function of serine-threonine protein kinases.
  • 6- and 7-position urea-substituted pyrido [2,3-b] pyrazines are given in the patent WO 05/056547 (Bemis et al.).
  • the compounds in this patent have additional carbonyl, sulfoxy, sulfonic or imine substitution in the 2- or 3-position, whereby the compounds are structurally distinct from the pyrido [2,3-b] pyrazines of the invention described in this invention differ.
  • the pyridopyrazines indicated in WO 05/056547 are described as inhibitors of protein kinases, in particular of GSK-3, Syk and JAK-3.
  • the invention is therefore directed to providing novel compounds which are useful as modulators of receptor tyrosine kinases, cytoplasmic tyrosine, serine / threonine kinases and lipid kinases. Since not all in dysregulated signal transduction cascades connected in series kinases - such. For example, in Raf-Mek-Erk or PI3K-Akt - must be present as oncogenic kinases or as constitutively active enzymes, in this invention, the non-active kinases are considered as therapeutic target proteins, i. The new compounds can bind to both active and non-active kinases, thereby influencing signal transduction.
  • the invention is further directed to providing novel compounds which possess as a modulator of receptor tyrosine kinases, cytoplasmic tyrosine, serine / threonine kinases and lipid kinases the property of both a single and two or more kinases, in particular Erk1 / 2 and PI3K, from one or several signal transduction cascades, in particular ras Raf Mek Erk and PI3K act to influence.
  • a dual mechanism, i. H. the simultaneous inhibition of two or more signal-induction cascades in comparison to the therapeutic attack of only one signal transduction pathway should lead to an increase in the effect in the treatment of all pathogenic processes which are influenced by kinases.
  • a first aspect of the present application describes novel compounds from the series of pyrido [2,3-b] pyrazines according to the general formula (I),
  • radicals Z3, Z4 or both radicals Z3, Z4 is independently “substituted aryl", where "substituted aryl" is substituted by at least one substituent, identical or different, selected from the group consisting of:
  • Substituted aryl is substituted with “heterocyclylalkyl", the other radical Z3 or Z4 is not “substituted or unsubstituted aryl", where optionally additionally one of the radicals Z3, Z4 or additionally both radicals Z3, Z4 can also be further substituted independently of one another with min. at least one substituent, identical or different, selected from the group consisting of:
  • X124, X125, X126, X127, X128, X129, X130, X131, X132, X133, X134, X135, X136, X137, X138, X139, X140, X141, X142, X143, X144, X145, X146, X147, X148, x149, X150, X151, X152, x153 are X154 independently selected from the group consisting of: "alkyl, (Cg-C 3 o) alkyl, cycloalkyl, cycloalkylalkyl, heterocyclyl, heterocyclylalkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl" and alternatively, X109, X110 and / or X1 18, X119 and / or X131, X132 and / or X138, X139 and / or X147,
  • alkyl "alkyl, (C 3 -C 30) alkyl, cycloalkyl, cycloalkylalkyl, heterocyclyl, heterocyclylalkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, F, Cl, Br, I, CN, CF 3 , N 3 , NH 2 , -NHX155, -NX156X157, -NO 2 , -OH, -OCF 3 , -SH, -O-SO 3 H, -
  • OS OS (O 2) -X177, -NHC (O) -XI78, -NX179C (O) -XI80, -NH-C (O) -O- X181, -NH-C (O) -NH-XI82, -NH -C (O) -NXI83X184, -NX185-C (O) - O-X186, -NX187-C (O) -NH-XI88, -NX189-C (O) -NXI90X191, - NHS (O 2) -X192 , -NX193S (O 2) -X194, -S-x195, -S (O) -XI96, -S (O 2) - X197, -S (O 2) NH-XI 98, -S (O 2) NXI 99X200, -S (O 2) O-X201, - P (O) (OX202) (OX203),
  • X187, X188, X189, X190, X191, X192, X193, X194, X195, X196, X197, X198, X199, X200, X201, X202, X203, X204, X205, X206 are independently selected from the group consisting of: alkyl, (C 9 -C 3 o) alkyl, cycloalkyl, cycloalkylalkyl, heterocyclyl, heterocyclylalkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl "and wherein alternatively X161,
  • X162 and / or X170, X171 and / or X183, X184 and / or X190, X191 and / or X199, X200 may together also form "heterocyclyl";
  • radicals Z3, Z4 or both radicals Z3, Z4 are independently "substituted aryl", where "substituted aryl" is substituted by at least one substituent, identical or different, selected from the group consisting of:
  • X217, X218, X219, X220, X221, X222, X223, X224, X225, X226, X227, X228, X229, X230, X231, X232, X233, X234, X235, X236, X237, X238, X239, X240, X241, X242, x243, X244, X245, X246, are x247, x248 independently selected from the group consisting of: "alkyl, (C 9 -C 3 o) alkyl, cycloalkyl, cycloalkylalkyl, heterocyclyl, heterocyclylalkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl "and wherein alternatively X216, X217 and / or X221, X222 and / or X227, X228
  • X415, X416, X417, X418, X419, X420, X421, X422, X423, X424, X425, X426, X427, X428, X429, X430, X431, X432, X433, X434, X435, X436, X437, X438, X439, X440, X441, X442, X443, X444, X445, X446, X447, X448, X449, X450, X451, X452, X453, X454, X455, X456 independent are independently selected from the group consisting of: "(C 9 -C 3 o) alkyl, alkyl, cycloalkyl, cycloalkylalkyl, heterocyclyl, heterocyclylalkyl, aryl, arylalkyl, heteroaryl, heteroary
  • Z3, Z4 or none of Z3, Z4 is independently selected from the group consisting of: (e) hydrogen;
  • alkyl (C 9 -C 30 ) alkyl, cycloalkyl, cycloalkylalkyl, heterocyclyl, heterocyclylalkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, F, Cl, Br, I, CN, CF 3 , N 3 , NH 2 , -NHX509, -NX510X511, -NO 2 , -OH, -OCF 3 , -
  • X538, X539, X540, X541, X542, X543, X544, X545, X546, X547, X548, X549, X550, X551, X552, X553, X554, X555, X556, X557, X558, X559, X560 are independently selected the group consisting of: "alkyl, (C 3 -C 30) alkyl, cycloalkyl, cyclo- alkylalkyl, heterocyclyl, heterocyclylalkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl "and wherein alternatively X515, X516 and / or X524, X525 and / or X537, X538 and / or X544, X545 and / or X553, X554 in each case also" heterocyclyl " can form;
  • substituents of the substituent group (ii) above may in turn be substituted independently of one another with at least one substituent, identical or different, selected from the group consisting of:
  • X652, X653, X654, X655, X656, X657, X658, X659, X660, X661, X662, are X663, X664 are independently selected from the group consisting of: "alkyl, (30 Cg-C) alkyl, cycloalkyl, cycloalkylalkyl, heterocyclyl, heterocyclylalkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl "and wherein alternatively X619, X620 and / or X628, X629 and / or
  • X641, X642 and / or X648, X649 and / or X657, X658 may together also form "heterocyclyl", where optionally substituents of the substituent group (i) above may be substituted independently of one another with at least one at least one substituent, the same or different, selected from the group consisting of:
  • X694, X695, X696, X697, X698, X699, X700, X701, X702, X703, X704, X705, X706, X707, X708, X709, X710, X711, X712, X713, X714, X715, X716 are independently selected consisting of the group consisting of: "alkyl, (Cg-C 3 o) alkyl, cycloalkyl, cyclo- alkylalkyl, heterocyclyl, heterocyclylalkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl" and wherein alternatively X671, X672 and / or X680, X681 and / or X693, X694 and / or X700, X701 and / or X709, X710 may together also form "heterocyclyl
  • X725, X726, X727, X728, X729, X730, X731, X732, X733, X734, X735, X736, X737, X738, X739, X740, X741, X742, X743, X744, X745, X746, X747, X748, X749, X750, X751, X752, X753, X754, X755, X756, X757, X758, X759, X760, X761, X762, X763, X764, X765, X766, X767, X768 are independently selected from the group consisting of: "alkyl, (C 9 -C 30 ) alkyl, cycloalkyl, cycloalkylalkyl, heterocyclyl, heterocyclylalkyl, aryl, arylalkyl
  • X762 together can also form "heterocyclyl"
  • heteroaryl radical may be substituted by at least one substituent, identical or different, selected from the group consisting of:
  • X808, X809, X810, X81 1, X812, X813, X814, X815, X816, X817, X818, X819, X820 are independently selected from the group consisting of: "alkyl, (C 9 -C 3 o) alkyl, cycloalkyl , cycloalkylalkyl, heterocyclyl, heterocyclylalkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl "and wherein alternatively X775, X776 and / or X784, X785 and / or
  • X797, X798 and / or X804, X805 and / or X813, X814 may together also form "heterocyclyl", where optionally substituents of the substituent group (i) above may be substituted independently of one another by at least one substituent, identical or different, selected from the group consisting of:
  • X850, X851, X852, X853, X854, X855, X856, X857, X858, X859, X860, X861, X862, X863, X864, X865, X866, X867, X868, X869, X870, X871, X872 are independently selected consisting of the group consisting of: "alkyl, (C 9 -C 3 o) alkyl, cycloalkyl, cyclo-
  • alkyl (C 3 -C 30) alkyl, cycloalkyl, cycloalkylalkyl, heterocyclyl, heterocyclylalkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, F, Cl,
  • X881, X882, X883, X884, X885, X886, X887, X888, X889, X890, X891, X892, X893, X894, X895, X896, X897, X898, X899, X900, X901, X902, X903, X904, X905, X906, X907, X908, X909, X910, X91 1, X912, X913, X914, X915, X916, X917, X918, X919, X920, X921, X922, X923, X924 are independently selected from the group consisting of: "alkyl , (C 9 -C 3 o) alkyl, cycloalkyl, cycloalkylalkyl, as heterocyclyl, heterocyclylalkyl, aryl, aryl
  • X918 may together also form "heterocyclyl"
  • Z6 is independently selected from the group consisting of: (i) "hydrogen, alkyl, (Cg-C 3 o) alkyl, cycloalkyl, cycloalkylalkyl, heterocyclyl, heterocyclylalkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl"; in which optional substituents of the substituent group (i) may in turn be substituted independently of one another with at least one substituent, identical or different, selected from the group consisting of:
  • X954, X955, X956, X957, X958, X959, X960, X961, X962, X963, X964, X965, X966, X967, X968, X969, X970, X971, X972, X973, X974, X975, X976 are independently selected from consisting of the group consisting of: "alkyl, (C 9 -C 3 o) alkyl, cycloalkyl, cyclo-
  • alkyl (C 3 -C 30) alkyl, cycloalkyl, cycloalkylalkyl, heterocyclyl, heterocyclylalkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, F, Cl,
  • X1019, X1020, X1021, X1022, X1023, X1024, X1025, X1026, X1027, X1028 are independently selected from the group consisting of: "alkyl, (Cg-C 3 o) alkyl, cycloalkyl, cycloalkylalkyl, heterocyclyl, heterocyclylalkyl, aryl , arylalkyl, heteroaryl, heteroarylalkyl "and alternatively, X983, X984 and / or X992, X993 and / or X1005, X1006 and / or X1012, X1013 and / or X1021, X1022 may each together also form" heterocyclyl ";
  • Z7 is independently selected from the group consisting of: "hydrogen, alkyl, (C” 9 " -C” 30 " ) alkyl, cycloalkyl, cycloalkylalkyl, heterocyclyl, heterocyclylalkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl”; optionally wherein the above substituents of the substituent group ( i) may in turn be substituted independently of one another by at least one substituent, identical or different, selected from the group consisting of:
  • X1068, X1069, X1070, X1071, X1072, X1073, X1074, X1075, X1076, X1077, X1078, X1079, x1080 independently selected from the group consisting of: "alkyl, (C 9 - C 3 o) alkyl, cycloalkyl, cycloalkylalkyl, heterocyclyl, heterocyclylalkyl,
  • X1035, X1036 and / or X1044, X1045 and / or X1057, X1058 and / or X1064, X1065 and / or X1073, X1074 may together also form "heterocyclyl" wherein optionally substituents of substituent group (ii) 25 optionally substituted independently of one another may be at least one substituent, the same or different, selected from the group consisting of:
  • alkyl "alkyl, (C 9 -C 3 o) alkyl, cycloalkyl, cycloalkylalkyl, heterocyclyl, heterocyclylalkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, F, Cl,
  • X1112, X1113, X1114, X1115, X1116, X1117, X1118, X1119, X1120, X1121, X1122, X1123, X1124, X1125, X1126, X1127, X1128, X1129, X1130, X1131, X1132 are independently selected from the group consisting of : "alkyl, (Cg-C 30) alkyl, cycloalkyl, cycloalkylalkyl, heterocyclyl, heterocycly- lalkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl" and wherein alternatively X1087, X1088 and / or X1096, X1097 and / or X1 109, X1 110 and / or X11 16, X11 17 and / or X1125, X1 126 may each together also form "heterocycly
  • NZ8Z9 wherein Z8, Z9 are independently selected from the group consisting of:
  • OSi (X1 158) (X1159) (X1160), -0S (0 2 ) -X1161, -NHC (O) -X1 162, -NX1 163C (O) -X1 164, -NH-C (O) -O- X1165, -N HC (O) -NH-X1 166, -NH-C (O) -NX1 167X1168, -NX1 169-C (O) -O-X1170, -NX1 171-C (O) -NH- X1172, -NX1 173-C (O) -NXI 174X1175, - NHS (0 2 ) -X 1 176, -NX 1 177S (O 2 ) -X 1178, -S-X 1 179, -S (O) -
  • X1 154, X1 155, X1 156, X1 157, X1158, X1159, X1160, X1161, X1 162, X1 163, X1 164, X1 165, X1166, X1167, X1168, X1169, X1 170, X1 171, X1 172, X1 173, X1174, X1175, X1176, X1177, X1 178, X1 179, X1 180, X1 181, X1182, X1183, X1184, X1185, X1 186, X1 187, X1 188, X1 189, X1190 are independently selected from the group consisting of: "alkyl, (C 9 - C 3 o) alkyl, cycloalkyl, cycloalkylalkyl, heterocyclyl, heterocyclylalkyl, aryl, arylal
  • alkyl "alkyl, (Cg-C 30) alkyl, cycloalkyl, cycloalkylalkyl, heterocyclyl, HE terocyclylalkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, F, Cl, Br, I 1 1 CN CF 3, N 3, NH 2 , -NHX1 191, -NX1 192X1193, -NO 2 , -
  • one of Z3, Z4 or both Z3, Z4 are independently "substituted heteroaryl", wherein “substituted heteroaryl” is substituted with at least one substituent selected from the group consisting of: (a) "alkyl, cycloalkyl, heterocyclyl , aryl, heteroaryl, -NH-V1, -N (alkyl) 2 , -
  • Substituents the same or different, selected from the group consisting of: (i) "(C 3 -C 30) alkyl, cycloalkyl, cycloalkylalkyl, heterocyclyl, heterocyclylalkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, N 3 , -NH-cycloalkyl, -NH-cycloalkylalkyl, -NH-heteroaryl, -NH- heteroarylalkyl, -NH-arylalkyl, -NH-heterocyclyl, -NH-heterocyclylalkyl, -NV4V5, -S-cycloalkyl, -S-cycloalkylalkyl, -S-aryl, -S-arylalkyl, -S-heteroaryl, -S-heteroarylalkyl, -S-heteroarylalkyl, -
  • Z3, Z4 independently of one another may also be further substituted by at least one substituent, identical or different, selected from the group consisting of: (b) "alkyl, (C 3 -C 30) alkyl, cycloalkyl, cycloalkylalkyl, heterocyclyl, heterocyclicalkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, F, Cl, Br, I, CN, CF 3 , N 3 , NH 2, -NHV53, -NV54V55, -NO 2, -OH, -OCF3, -SH, -0-SO3H, -OP (O) (OH) 2, - CHO, -COOH, -C (O) NH 2, -SO 3 H, -P (O) (OH) 2, -C (O) -V56, -C (O) O-V57, -C (O) NH-V58, -C (O) NV59V60
  • V80, V81, V82, V83, V84, V85, V86, V87, V88, V89, V90, V91, V92, V93, V94, V95, V96, V97, V98, V99, V100, V101, V102, V103, V104 are independent are selected from the group consisting of: "alkyl, (C 9 - C 3 o) alkyl, cycloalkyl, cycloalkylalkyl, heterocyclyl, heterocyclylalkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl" and wherein alternatively V59, V60 and / or
  • V68, V69 and / or V81, V82 and / or V88, V89 and / or V97, V98 may together also form "heterocyclyl" wherein optional substituents above the substituent group (b) may be independently substituted with at least one substituent, the same or different, selected from the group consisting of:
  • V148, V149, V150, V151, V152, V153, V154, V155, V156 independently selected from the group consisting of: "alkyl, (Cg-C 3 o) alkyl, cycloalkyl, cycloalkylalkyl, heterocyclyl, heterocyclylalkyl, aryl, arylalkyl , heteroaryl, heteroarylalkyl "and wherein alternatively V1 11, V1 12 and / or V120, V121 and / or V133, V134 and / or V140, V141 and / or V149, V150 may together also form" heterocyclyl "; wherein optionally above substituents of the substituent group (i) and / or substituent group (ii) may be independently substituted with at least one substituent, same or different, selected from the group consisting of:
  • radicals Z3, Z4 or both radicals Z3, Z4 independently of one another are "substituted heteroaryl", where "substituted heteroaryl” is substituted by at least one substituent, identical or different, selected from the group consisting of:
  • V230, V231, V232, V233, V234, V235, V236, V237, V238, V239, V240, V241, V242, V243, V244, V245, V246, V247, V248, V249, V250, V251, V252 are selected independently the group consisting of: "alkyl, (C 9 -C 3 o) alkyl, cycloalkyl, cycloalkylalkyl, heterocyclyl, heterocycloalkyl lylalkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl" and wherein alternatively V218,
  • V219 and / or V223, V224 and / or V229, V230 and / or V233, V234 and / or V238, V239 and / or V241, V242 may together also form "heterocyclyl", with the proviso that the substituents "- N (alkyl) 2 "," - C (O) N (alkyl) 2 ",” - C (O) N (cycloalkyl) 2 ",” - C (O) N (aryl) 2 ", C (O) N (heteroaryl) 2 "are further substituted by at least one substituent selected from sub-substituent group (i); wherein optionally substituted substituents of the substituent group (c) may in turn be independently substituted with at least one substituent, same or different, selected from the group consisting of:
  • V279 -NH-C (O) -NH-V280, -NH-C (O) -NV281V282, -NV283-C (O) -O-V284, -NV285-C (O) -NH-V286, -NV287 -C (O) -NV288V289, - NHS (O 2) -V290, -NV291S (O 2) -V292, -S-V293, -S (O) -V294, -S (O 2) - V295, -S (O 2) N H-V296, -S (O 2) NV297V298, -S (O 2) O-V299, - P (O) (OV300) (OV301), -Si (V302) (V303 ) (V304) "; wherein V253, V254, V255, V256, V257, V258, V259, V260, V261, V262, V263, V264, V26
  • V285, V286, V287, V288, V289, V290, V291, V292, V293, V294, V295, V296, V297, V298, V299, V300, V301, V302, V303, V304 are independently selected from the group consisting of: " alkyl, (C 9 -C 3 o) alkyl, cycloalkyl, cycloalkylalkyl, heterocyclyl, heterocyclylalkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl "and wherein alternatively V259,
  • V260 and / or V268, V269 and / or V281, V282 and / or V288, V289 and / or V297, V298 may together also form "heterocyclyl", optionally additionally one of the radicals Z3, Z4 or additionally both radicals Z3, Z4 independently from each other can also be further substituted with at least one substituent, identical or different, selected from
  • V350 may also together form "heterocyclyl", where optionally substituted substituents of the substituent group (d) may in turn be substituted by at least one substituent, identical or different, selected from the group consisting of:
  • V367, V368, V369, V370, V371, V372, V373, V374, V375, V376, V377, V378, V379, V380, V381, V382, V383, V384, V385, V386, V387, V388, V389, V390, V391, V392, V393, V394, V395, V396, V397, V398, V399, V400, V401, V402, V403, V404, V405, V406, V407, V408 are independently selected from the group consisting of: "alkyl,
  • V430, V431, V432, V433, V434, V435, V436, V437, V438, V439, V440, V441, V442, V443, V444, V445, V446, V447, V448, V449, V450, V451, V452, V453, V454, V455, V456a, V456b, V456c, V456d, V456e are independently selected from the group consisting of: "alkyl, (C 9 -C 30 ) alkyl, cycloalkyl, cycloalkylalkyl, heterocyclyl, heterocyclylalkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl and wherein alternatively V415, V416 and / or V424, V425 and / or V437, V438 and / or V444, V445 and / or V453, V454 may together also form "heterocyclyl";
  • Z3, Z4 or none of Z3, Z4 is independently selected from the group consisting of:
  • (g) unsubstituted or substituted alkyl or (Cg-C3o) alkyl may be optionally substituted with (C 9 -C 30 C) alkyl moiety of the alkyl or at least one substituent, identical or different, selected from the group-consisting of pe:
  • V463, V464 and /: are V506, V507, V508 independently selected from the group consisting of or V472, V473 and / or V485, V486 and / or V492, V493 and / or V501, V502 may each together also form "heterocyclyl"; optionally substituents of the substituent group (i) above may be substituted independently of one another with at least at least one substituent, the same or different, selected from the group consisting of:
  • V538, V539, V540, V541, V542, V543, V544, V545, V546, V547, V548, V549, V550, V551, V552, V553, V554, V555, V556, V557, V558, V559, V560 are independently selected from consisting of the group consisting of: "alkyl, (Cg-C 3 o) alkyl, cycloalkyl, cyclo- alkylalkyl, heterocyclyl, heterocyclylalkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl" and wherein alternatively V515, V516 and / or V524, V525, and / or V537, V538 and / or V544, V545 and / or V553, V554 may together also form "heterocyclyl"; in which optional substituents of the substituent group (ii) may in turn be substituted independently of one another with at least one substituent
  • V569, V570, V571, V572, V573, V574, V575, V576, V577, V578, V579, V580, V581, V582, V583, V584, V585, V586, V587, V588, V589, V590, V591, V592, V593, V594, V595, V596, V597, V598, V599, V600, V601, V602, V603, V604, V605, V606, V607, V608, V609, V610, V611, V612 are independently selected from the group consisting of: "alkyl, (C 9 -C 30 ) alkyl, cycloalkyl, cycloalkylalkyl, heterocyclyl, heterocyclylalkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl and, alternatively, V567, V568 and / or V576, V577 and / or V589, V5
  • V606 may together also form "heterocyclyl"
  • V662 V663 (V664) "; wherein V613, V614, V615, V616, V617, V618, V619, V620, V621, V622, V623, V624, V625, V626, V627, V628, V629, V630, V631 , V632, V633, V634, V635, V636, V637, V638, V639, V640, V641, V642, V643, V644, V645, V646, V647, V648, V649, V650, V651,
  • V652, V653, V654, V655, V656, V657, V658, V659, V660, V661, V662, V663, V664 are each independently selected from the group consisting of: "alkyl, (C 9 -C 3 o) alkyl, cycloalkyl, cycloalkylalkyl, heterocyclyl, heterocyclylalkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, and wherein alternatively V619, V620 and / or V628, V629 and / or
  • V641, V642 and / or V648, V649 and / or V657, V658 may in each case also form "heterocyclyl", where optionally substituents of the substituent group (i) above may be substituted independently of one another by at least one substituent, identical or different, selected from the group consisting of:
  • V694, V695, V696, V697, V698, V699, V700, V701, V702, V703, V704, V705, V706, V707, V708, V709, V710, V71 1, V712, V713, V714, V715, V716 are independently selected from the group consisting of: "alkyl, (C 9 -C 3 o) alkyl, cycloalkyl, cyclo-
  • V671, V672 and / or V680, V681 and / or V693, V694 and / or V700, V701 and / or V709, V710 also together also "heterocyclyl "can form; in which optional substituents of substituent group (ii) 20 may in turn be substituted independently of one another with at least one substituent, identical or different, selected from the group consisting of:
  • alkyl (C 3 -C 30) alkyl, cycloalkyl, cycloalkylalkyl, heterocyclyl, heterocyclylalkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, F, Cl,
  • V725, V726, V727, V728, V729, V730, V731, V732, V733, V734, V735, V736, V737, V738, V739, V740, V741, V742, V743, V744, V745, V746, V747, V748, V749, V750, V751, V752, V753, V754, V755, V756, V757, V758, V759, V760, V761, V762, V763, V764, V765, V766, V767, V768 are independently selected from the group consisting of: "alkyl, (C 9 -C 3 o) alkyl, cycloalkyl, cycloalkylalkyl, as heterocyclyl, heterocyclylalkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl "and wherein alternatively V723, V724 and / or V732, V733 and / or V745, V7
  • V762 may together also form "heterocyclyl"
  • heteroaryl radical may be substituted by at least one substituent, identical or different, selected from the group consisting of:
  • V798, V799, V800, V801, V802, V803, V804, V805, V806, V807, V808, V809, V810, V811, V812, V813, V814, V815, V816, V817, V818, V819, V820 are independently selected from the group consisting of: "alkyl, (C 9 -C 3 o) alkyl, cycloalkyl, cycloalkylalkyl, heterocyclyl, heterocyclylalkyl, aryl, arylalkyl, heteroaryl, heteroarylal- alkyl" and wherein alternatively V775, V776 and / or V784, V785 and or V797, V798 and / or V804, V805 and / or V813, V814 may together also form "heterocyclyl"; in which optionally above substituents of the substituent group (i) can in turn be substituted independently of one another with at least one substituent,
  • alkyl (C 9 -C 30 ) alkyl, cycloalkyl, cycloalkylalkyl, heterocyclyl, heterocyclylalkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, F, Cl, Br, I, CN, CF 3 , N 3 , NH 2 , -NHV821, -NV822V823, -NO 2 , -OH, -OCF 3 , -
  • alkyl (C 3 -C 30) alkyl, cycloalkyl, cycloalkylalkyl, heterocyclyl, heterocyclylalkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl
  • V827, V828 and / or V836, V837 and / or V849, V850 and / or V856, V857 and / or V865, V866 may together also form "heterocyclyl";
  • substituents of the substituent group (ii) above may be substituted independently with at least one substituent, identical or different, selected from the group consisting of:
  • NV905-C O-NH-V906, -NV907-C (O) -NV908V909, - NHS (O 2) -V910, -NV911S (O 2) -V912, -S-V913, -S (O) - V914, -S (O 2) -V915, -S (O 2) NH-V916, -S (O 2) NV917V918, -S (O 2) O- V919, -P (O) (OV920) (OV921) , -Si (V922) (V923) (V924) ";
  • V881, V882, V883, V884, V885, V886, V887, V888, V889, V890, V891, V892, V893, V894, V895, V896, V897, V898, V899, V900, V901, V902, V903, V904, V905, V906, V907, V908, V909, V910, V911, V912, V913, V914, V915, V916, V917, V918, V919, V920, V921, V922, V923, V924 are independently selected from the group consisting of: "alkyl, (C 3 -C 30) alkyl, cycloalkyl, cycloalkylalkyl, heterocyclyl, heterocyclylalkyl, aryl, arylalkyl heteroaryl, heteroarylalkyl "and wherein alternatively V879, V880 and / or V888, V889 and / or V901, V902 and
  • alkyl (Cg-C 3 o) alkyl, cycloalkyl, cyclo- alkylalkyl, heterocyclyl, heterocyclylalkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl
  • V931, V932 and / or V940, V941 and / or V953, V954 and / or V960, V961 and / or V969, V970 may together also form "heterocyclyl";
  • substituents of the substituent group (ii) above may be substituted independently with at least one substituent, identical or different, selected from the group consisting of:
  • V1025 30 P (O) (OVI 024) (OV1025), -Si (VI 026) (V1027) (V1028) "; wherein V977, V978, V979, V980, V981, V982, V983, V984, V985, V986, V987, V988, V989, V990, V991, V992, V993, V994, V995, V996, V997, V998, V999, V1000, V1001, V1002, V1003, V1004, V1005, V1006, V1007, V1008, V1009, V1010, V1011, V1012, V1013, V1014, V1015, V1016, V1017, V1018, V1019, V1020, V1021, V1022, V1023, V1024, V1025, V1026, V1027, V1028 are independently selected from the group consisting of: "alkyl, (C 9 -C 3 o) alkyl, cycloalkyl, cycloalkyl
  • Z7 is independently selected from the group consisting of: "hydrogen, alkyl, (C” 9 " -C” 30 " ) alkyl, cycloalkyl, cycloalkylalkyl, heterocyclyl, heterocyclylalkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl”; optionally wherein the above substituents of the substituent group ( i) may in turn be substituted independently of one another with at least one substituent, identical or different, selected from the group consisting of:
  • alkyl (C 9 -C 30 ) alkyl, cycloalkyl, cycloalkylalkyl, heterocyclyl, heterocyclylalkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, F, Cl, Br, I, CN, CF 3 , N 3 , NH 2 , -NHV1029, -NV1030V1031, -NO 2 , -OH, -
  • NV1044V1045 -OP (O) (OVI 046) (OV1047), - OSi (VI 048) (V1049) (V1050), -OS (O 2) -V1051, -N HC (O) -VI 052, - NV1053C ( O) -VI 054, -NH-C (O) -O-VI 055, -NH-C (O) -NH-V1056, -NH-C (O) -NVI 057V1058, -NV1059-C (O) - O-VI 060, - NV1061-C (O) -NH-VI 062, -NV1063-C (O) -NVI 064V1065, -
  • V1060 V1061, V1062, V1063, V1064, V1065, V1066, V1067,
  • alkyl (- C 30 9 C) alkyl, cycloalkyl, cycloalkylalkyl, "alkyl,: are V1068, V1069, V1070, V1071, V1072, V1073, V1074, V1075, V1076, V1077, V1078, V1079, V1080 independently selected from the group consisting of , heterocyclyl, heterocyclylalkyl, 10 aryl, arylalkyl, heteroaryl, heteroarylalkyl "and wherein alternatively
  • V1035, V1036 and / or V1044, V1045 and / or V1057, V1058 and / or V1064, V1065 and / or V1073, V1074 may together also form "heterocyclyl" wherein optionally substituted substituents of substituent group (ii) 15 in turn independently substituted may be at least one substituent, the same or different, selected from the group consisting of:
  • alkyl (C 3 -C 30) alkyl, cycloalkyl, cycloalkylalkyl, heterocyclyl, heterocyclylalkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, F, Cl,
  • V1131 35 Si (VI 130) (V1131) (V1132) "; wherein V1081, V1082, V1083, V1084, V1085, V1086, V1087, V1088, V1089, V1090, V1091, V1092, V1093, V1094, V1095, V1096, V1097, V1098, V1099, V1100, V1101, V1102, V1103, V1104, V1105 , V1106, V1107, V1108, V1109, V1110, V1111, VII ⁇ 1 VIIIa 1 VIIU 1 VIIIS 1 VIIIe 1 VIIIy 1 VIIIe 1 VIIIg 1
  • V1120, V1121, V1122, V1123, V1124, V1125, V1126, V1127, V1128, V1129, V1130, V1131, V1132 are independently selected from the group consisting of: "alkyl, (C 9 - C 30 ) alkyl, cycloalkyl, cycloalkylalkyl , heterocyclyl, heterocyclylalkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl "and where alternatively V1087, V1088 and / or V1096, V1097 and / or V1109, V1110 and / or V1116, V1117 and / or V1125, V1126 also together also" heterocyclyl "can form;
  • V1180 -S (0 2) -V1 181, -S (O 2) NH-V1 182, -S (O 2) NVI 183V1184, - S (O 2) O-V1185, -P (O) (OV1186) (OV1 187), -Si (VI 188) (V1189) (V1190) ", wherein V1139, V1140, V1141, V1142, V1143, V1144, V1145,
  • V1186, V1187, V1188, V1 189 V1 190 are independently selected from the group consisting of: "alkyl, (Cg-C 30) alkyl, cycloalkyl, cycloalkylalkyl, heterocyclyl, heterocyclylalkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl" and alternatively, V1145, V1146 and / or V1 154, V1 155 and / or V1 167, V1 168
  • V1 174, V1 175 and / or V1 183, V1184 may together also also form "heterocyclyl", where optionally substituents of the substituent group (ii) above may be substituted independently with at least one substituent, identical or different - 30 selects from the group consisting of:
  • V1238, V1239, V1240, V1241 are, V1242 independently selected from the group consisting of: "alkyl, (C 9 - C 3 o) alkyl, cycloalkyl, cycloalkylalkyl, heterocyclyl, heterocycly- lalkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl" and wherein alternatively V1197, V1198 and / or V1206, V1207 and / or
  • V1219, V1220 and / or V1226, V1227 and / or V1235, V1236 may together also form "heterocyclyl";
  • one of the radicals Z3, Z4 or both radicals Z3, Z4 is independently "substituted alkyl", where "substituted alkyl” is substituted by at least one substituent selected from the group consisting of: (a) "alkyl, (C 3 -C 30) alkyl, cycloalkyl, cycloalkylalkyl, heterocyclyl, heterocyclylalkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, F, Cl, Br, I, CN, CF 3 , N 3 , NH 2, -NHW1, -NW2W3, -NO2, -OH, -OCF3, -SH, -0-SO3H, - OP (O) (OH) 2, -CHO, -COOH, -C (O) NH 2 , -SO 3 H, -P (O) (OH) 2 , -C (O) -W 4, -C (O) (
  • W26, W27, W28, W29, W30, W31, W32, W33, W34, W35, W36, W37, W38, W39, W40, W41, W42, W43, W44, W45, W46, W47, W48, W49, W50, W51, W52 are independently selected from the group consisting of: "alkyl, (Cg-C 3 o) alkyl, cycloalkyl, cycloalkylalkyl, hetero- cyclyl, heterocyclylalkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl” and wherein alternatively W7, W8 and or W16, W17 and / or W29, W30 and / or W36, W37 and / or W45, W46 may together also form "heterocyclyl”; with the proviso that "--C (O) NH-aryl", "- C (O) NH-heteroaryl", "
  • W99, W100, W101, W102, W103, W104 are independently selected from the group consisting of: "alkyl, (Cg-C 3 o) alkyl, cycloalkyl, cycloalkylalkyl, heterocyclyl, heterocyclylalkyl, aryl, arylal- kyl, heteroaryl, heteroarylalkyl and alternatively W59, W60 and / or W68, W69 and / or W81, W82 and / or W88, W89 and / or W97, W98 may together also form "heterocyclyl"; in which optional substituents of the substituent group (i) may in turn be substituted independently of one another by at least one substituent, identical or different, selected from the group consisting of:
  • alkyl "alkyl, (Cg-C 30) alkyl, cycloalkyl, cycloalkylalkyl, heterocyclyl, heterocyclylalkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, F, Cl, Br, I, CN, CF 3, N 3, NH 2, - NHW105, -NW106W107, -NO2, - OH, -OCF3, -SH, -0-SO3H, -OP (O) (OH) 2, -CHO, -COOH, -
  • W153, W154, W155, are W156 independently selected from the group consisting of: "alkyl, (Cg-C 3 o) alkyl, cycloalkyl, cycloalkylalkyl, heterocyclyl, heterocyclylalkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl" and wherein alternatively W1 11 , W1 12 and / or W120, W121 and / or W133, W134 and / or W140, W141 and / or W149, W150 may together also form "heterocyclyl";
  • Z3, Z4 or both radicals Z3, Z4 are independently "(C 9 -C 3 o) alkyl" are one another, wherein "(Cg-C 3 o) alkyl” may optionally be independently substituted with at least one substituent , the same or different, selected from the group consisting of:
  • alkyl (Cg-C 30) alkyl, cycloalkyl, cycloalkylalkyl, heterocyclyl, heterocyclylal- kyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, F, Cl, Br, I, CN, CF 3, N 3, NH 2 .
  • W176, W177, W178, W179, W180, W181, W182, W183, W184, W185, W186, W187, W188, W189, W190, W191, W192, W193, W194, W195, W196, W197, W198, W199, W200, W201, W202, W203, W204, W205, W206, W207, W208 are independently selected from the group consisting of: "alkyl, (Cg-C 3 o) alkyl, cycloalkyl, cycloalkylalkyl, hetero- rocyclyl, heterocyclylalkyl, aryl, arylalkyl heteroaryl, heteroarylalkyl "and alternatively W163, W164 and / or W172, W173 and / or W185, W186 and / or W192, W193 and / or W201, W202 may together also form" heterocyclyl "; in which optional substituents of the substituent group (i) may in
  • alkyl consisting of: "alkyl, (C 9 -C 3 o) alkyl, cycloalkyl, cycloalkylalkyl, heterocyclyl, heterocyclylalkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl" and wherein alternatively W215, W216 and / or W224, W225 and / or W237, W238 and / or W244, W245 and / or W253, W254 can in each case together also form "heterocyclyl";
  • Z3, Z4 or none of Z3, Z4 is independently selected from the group consisting of:
  • alkyl or (Cg-C 3 o) alkyl group may be substituted with at least one substituent, identical or different, selected from the group consisting of: (i) "alkyl, (Cg-C 30) alkyl, cycloalkyl, cycloalkylalkyl, heterocyclyl, heterocyclylalkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, F, Cl, Br, I, CN, CF 3, N 3, NH 2, - NHW457, -NW458W459, -NO 2 , -OH, -OCF 3 , -SH, -O-SO 3 H, -OP (O) (OH) 2 , -CHO, -COOH, -C (O) NH 2 , -SO 3 H, -P (O) (
  • W493, W494, W495, W496, W497, W498, W499, W500, W501, W502, W503, W504, W505, W506, W507, W508 are independently selected from the group consisting of: "alkyl, (Cg-C 30 ) alkyl, cycloalkyl, cycloalkylalkyl, heterocyclyl, heterocyclylalkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl "and where alternatively W463,
  • W464 and / or W472, W473 and / or W485, W486 and / or W492, W493 and / or W501, W502 may in each case also form "heterocyclyl", where optionally the above substituents of the substituent group (i) in turn are substituted independently of one another may be substituted by at least one substituent, the same or different, selected from the group consisting of:
  • alkyl (C 3 -C 30) alkyl, cycloalkyl, cycloalkylalkyl, heterocyclyl, heterocyclylalkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, F, Cl, Br, I, CN, CF 3 , N 3 , NH 2 , -NHW509, -NW510W511, -NO 2 , -OH, -OCF 3 ,
  • W553, W554, W555, W556, W557, W558, W559, W560 are independently selected from the group consisting of: "alkyl, (C 9 -C 3 o) alkyl, cycloalkyl, cycloalkylalkyl, heterocyclyl, hetero- rocyclylalkyl, aryl , arylalkyl, heteroaryl, heteroarylalkyl "and alternatively W515, W516 and / or W524, W525 and / or W537,
  • W538 and / or W544, W545 and / or W553, W554 may together also form "heterocyclyl", where optionally substituents of the substituent group (ii) above may be substituted independently with at least one substituent, identical or different, selected selects from the group consisting of:
  • alkyl "alkyl, (C 3 -C 30) alkyl, cycloalkyl, cycloalkylalkyl, heterocyclyl, heterocyclylalkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, F, Cl, Br, I, CN, CF 3 , N 3 , NH 2 , -NHW561, -NW562W563, -NO 2 , -OH, -OCF 3 , -SH, -O-SO 3 H, -OP (O) (OH) 2 , -CHO, -COOH, -
  • W577, W578, W579, W580, W581, W582, W583, W584, W585, W586, W587, W588, W589, W590, W591, W592, W593, W594, W595, W596, W597, W598, W599, W600, W601, W602, W603, W604, W605, W606, W607, W608, W609, W610, W61 1, W612 are independently selected from the group consisting of: "alkyl, (C 9 -C 3 o) alkyl, cycloalkyl, cycloalkylalkyl, heterocyclyl , heterocyclylalkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl "and alternatively W567, W568 and / or W576, W577 and / or W589, W590 and / or W596, W597 and / or W605, W606 may each together
  • W640, W641, W642, W643, W644, W645, W646, W647, W648, W649, W650, W651, W652, W653, W654, W655, W656, W657, W658, W659, W660, W661, W662, W663, W664 independent are selected from the group consisting of: "alkyl, (C 9 - C 30 ) alkyl, cycloalkyl, cycloalkyl alkyl, heterocyclyl, heterocyclylalkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl" and wherein alternatively W619, W620 and / or W628, W629 and / or W641, W642 and / or W648, W649 and / or W657, W658 may each also together form "heterocyclyl"; in which optional substituents of the substituent group (i) may in turn be substituted independently of one another with at least one substitu
  • alkyl (C 3 -C 30) alkyl, cycloalkyl, cycloalkylalkyl, heterocyclyl, heterocyclylalkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, F, Cl, Br, I,
  • W709, W710, W71 1, W712, W713, W714, W715, W716 are independently selected from the group consisting of: "alkyl, (C 9 -C 3 o) alkyl, cycloalkyl, cycloalkylalkyl, heterocyclyl, hetero- rocyclylalkyl, aryl , arylalkyl, heteroaryl, heteroarylalkyl "and where 10 alternatively W671, W672 and / or W680, W681 and / or W693,
  • W694 and / or W700, W701 and / or W709, W710 may together also form "heterocyclyl", where optionally substituents of the substituent group (ii) above may be substituted independently of one another with
  • At least one substituent identical or different, selected from the group consisting of:
  • alkyl "alkyl, (C 9 -C 30 ) alkyl, cycloalkyl, cycloalkylalkyl, heterocyclyl, heterocyclylalkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, F, Cl, Br, I, CN, CF 3 , N 3 , NH 2 , -NHW717, -NW718W719, -NO 2 , -
  • OSi (W736) (W737) (W738), -OS (O2) -W739, -NHC (O) -W740, -NW741C (O) -W742, -NH-C (O) -O-W743, -NH -C (O) -NH-W744, -NHC (O) -N W745W746, -NW747-C (O) -O-W748, -NW749-C (O) -NH-W750, -NW751 -C (O ) -N W752W753, -
  • W757, W758, W759, W760, W761, W762, W763, W764 are, W765, W766, W767, W768 are independently selected from the group consisting of: "alkyl, (C 9 -C 3 o) alkyl, cycloalkyl, cycloalkylalkyl, heterocyclyl, heterocyclylalkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl "and wherein alternatively
  • W723, W724 and / or W732, W733 and / or W745, W746 and / or W752, W753 and / or W761, W762 may together also form "heterocyclyl";
  • heteroaryl radical may be substituted by at least one substituent, identical or different, selected from the group consisting of:
  • OSi (W788) (W789) (W790), -OS (O2) -W791, -NHC (O) -W792, - NW793C (O) -W794, -NH-C (O) -O-W795, -N HC (O) -NH-W796, -NHC (O) -N W797W798, -NW799-C (O) -O-W800, -NW801-C (O) -NH-W802, -NW803-C (O ) -NW804W805, -NHS (O2) -W806, - NW807S (O2) -W808, -S-W809, -S (0) -W810, -S (O2) -W81 1 -
  • W879, W880 and / or W888, W889 and / or W901, W902 and / or W908, W909 and / or W917, W918 may together also form "heterocyclyl";
  • alkyl (C 9 -C 30 ) alkyl, cycloalkyl, cycloalkylalkyl, heterocyclyl, heterocyclylalkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, F, Cl, Br, I, CN, CF 3 , N 3 , NH 2 , -NHW925, -NW926W927, -NO 2 , -OH, -OCF 3 ,
  • W970, W971, W972, W973, W974, W975, W976 are independently selected from the group consisting of: "alkyl, (C 9 -C 3 o) alkyl, cycloalkyl, cycloalkylalkyl, heterocyclyl, hetero- rocyclylalkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl "and where alternatively 10 W931, W932 and / or W940, W941 and / or W953,
  • W954 and / or W960, W961 and / or W969, W970 may together also form "heterocyclyl", where optionally substituents of the substituent group (ii) above may be substituted independently of one another with
  • At least one substituent identical or different, selected from the group consisting of:
  • alkyl "alkyl, (C 9 -C 30 ) alkyl, cycloalkyl, cycloalkylalkyl, heterocyclyl, heterocyclylalkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, F, Cl, Br, I, CN, CF 3 , N 3 , NH 2 , -NHW977, -NW978W979, -NO 2 , -
  • OSi (W996) (W997) (W998), -OS (O2) -W999, -NHC (O) -WIOOO, -NW1001 C (O) -WI 002, -NH-C (O) -O-WI 003 , -NH-C (O) -NH-W1004, -NH-C (O) -NWI 005W1006, -NW1007-C (O) -O-W1008, -NW1009-C (O) -NH-WI 010, - NW1011-C (O) -
  • W1015, W1016, W1017, W1018, W1019, W1020, W1021, W1022, W1023, W1024, W1025, W1026, W1027, are W1028 independently selected from the group consisting of: "alkyl, (Cg-C 3 o) alkyl, cycloalkyl , cycloalkylalkyl, heterocyclyl, heterocyclylalkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl and, alternatively, W983, W984 and / or W992, W993 and / or W1005, W1006 and / or W1012, W1013 and / or W1021, W1022, respectively together may also form "heterocyclyl";
  • alkyl (C 3 -C 30) alkyl, cycloalkyl, cycloalkylalkyl, heterocyclyl, heterocyclylalkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, F, Cl, Br, I, CN, CF 3 , N 3 , NH 2 , -NHW1029, -NW1030W1031, -NO 2 , -OH, -
  • W1068, W1069, W1070, W1071, W1072, W1073, W1074, W1075, W1076, W1077, W1078, W1079, W1080 are independently selected from the group consisting of: "alkyl, alkyl, cycloalkyl, cycloalkylalkyl (Cg-C 30), heterocyclyl, heterocyclylalkyl,
  • W1035, W1036 and / or W1044, W1045 and / or W1057, W1058 and / or W1064, W1065 and / or W1073, W1074 may together also form "heterocyclyl" wherein optionally substituted substituents of substituent group (ii) 20 in turn independently substituted may be at least one substituent, the same or different, selected from the group consisting of:
  • alkyl (C 3 -C 30) alkyl, cycloalkyl, cycloalkylalkyl, heterocyclyl, heterocyclylalkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, F, Cl,
  • W1 108, W1109, W11 10, W1 11 1, W1 112, W11 13, W11 14, W1 115, W11 16, W11 17, W1 118, W1 119, W1120, W1121, W1 122, W1123, W1124, W1 125, W1 126, W1127, W1128, W1 129, W1130, W1131, W1 132 are independently selected from the group consisting of: "alkyl, (Cg-)
  • W1 170, W1171, W1172, W1 173, W1 174, W1175, W1176, W1 177, W1 178, W1179, W1180, W1 181, W1 182, W1183, W1184, W1 185, W1 186, W1187, W1188, W1 189, W1190 are independently selected from the group consisting of: "alkyl, (C 9 - C 30) alkyl, cycloalkyl, cycloalkylalkyl, heterocyclyl, heterocyclylalkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl" and wherein alternatively W1 145, W1146 and / or W1 154, W1155 and / or W1 167, W1 168 and / or W1174, W1 175 and / or W1 183, W1184 may together also form "heterocyclyl"; in which optional substituents of the substituent group (ii) may in turn
  • alkyl (C 9 -C 30 ) alkyl, cycloalkyl, cycloalkylalkyl, heterocyclyl, heterocyclylalkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, F, Cl, Br, I 1 CN 1 CF 3 , N 3 , NH 2 , -NHW 1 191, -NW 1192 W 1193, -NO 2 , -OH, -OCF 3 , -SH, -O-SO 3 H, -OP (O) (OH) 2 , -CHO, -COOH, -C ( O) NH 2 , -SO 3 H, -P (O) (OH) 2 , -C (O) -W 1194, -C (O) O-
  • W1239, W1240, W1241, W1242 are independently selected from the group consisting of: "alkyl, (Cg-C 30) alkyl, cycloalkyl, cycloalkylalkyl, heterocyclyl, heterocycly- lalkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl” and wherein alternatively W1 197, W1 198 and / or W1206, W1207 and / or W1219, W1220 and / or W1226, W1227 and / or W1235, W1236 may together also form "heterocyclyl";
  • radicals Z3, Z4 or both radicals Z3, Z4 are independently selected from the group consisting of:
  • radicals Z10, Z11 or both radicals Z10, Z1 1 and radicals Z12, Z13 being selected independently of one another from the group consisting of:
  • Q26, Q27, Q28, Q29, Q30, Q31, Q32, Q33, Q34, Q35, Q36, Q37, Q38, Q39, Q40, Q41, Q42, Q43, Q44, Q45, Q46, Q47, Q48, Q49 are independently selected are selected from the group consisting of: "alkyl, (Cg-C 3 o) alkyl, cycloalkyl, cycloalkylalkyl, heterocyclyl, hetero- rocyclylalkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl" and wherein alternatively Q10, Q11 and / or Q23, Q24, and or Q27, Q28 and / or Q34, Q35 and / or Q47, Q48 may together also form "heterocyclyl"; in which optionally above substituents of the substituent group (a) and / or the substituent group (i) may in turn be independently substituted with at least one substitu
  • alkyl (C 9 -C 30 ) alkyl, cycloalkyl, cycloalkylalkyl, heterocyclyl, heterocyclylalkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, F, Cl, Br, I, CN, CF 3 , N 3 , NH 2 , -NHQ50, -NQ51 Q52, -NO 2 , -OH, -OCF 3 , -
  • OSi (Q69) (Q70) (Q71), -OS (O 2) -Q72, -NHC (O) -Q73, - NQ74C (O) -Q75, -NH-C (O) -O-Q76, -N HC (O) -NH-Q77, -NH-C (O) -NQ78Q79, -NQ80-C (O) -O-Q81, -NQ82-C (O) -NH-Q83, -NQ84-C (O ) -NQ85Q86, -NHS (O 2 ) -Q87, -NQ88S (O 2 ) -Q89, -S- Q90, -S (0) -Q91, -S (O 2) -Q92, -S (O 2) NH-Q93, -S (O 2) NQ94Q95, -S (O 2) O-Q96, -P ( O) (OQ97)
  • Q85, Q86, Q87, Q88, Q89, Q90, Q91, Q92, Q93, Q94, Q95, Q96, Q97, Q98, Q99, Q100, Q101 are independently selected from the group consisting of: "alkyl, (Cg-C 3 o) alkyl, cycloalkyl, cycloalkylalkyl, heterocyclyl, heterocyclylalkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, and alternatively Q56, Q57 and / or Q65, Q66 and / or Q78, Q79 and / or Q85, Q86 and / or or Q94, Q95 may together also form "heterocyclyl"; in which optional substituents of substituent group (ii) 15 can in turn be substituted independently of one another with at least one substituent, identical or different, selected from the group consisting of:
  • alkyl (C 9 -C 30 ) alkyl, cycloalkyl, cycloalkylalkyl, heterocyclyl, heterocyclylalkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, F, Cl,
  • Q146, Q147, Q148, Q149, Q150, Q151, Q152, Q153 are independently selected from the group consisting of: "alkyl, (C 9 -C 3 o) alkyl, cycloalkyl, cycloalkylalkyl, hetero- rocyclyl, heterocyclylalkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl "and wherein alternatively Q108, Q109 and / or Q117, Q1 18 and / or Q130, Q131 and / or Q137, Q138 and / or Q146, Q147 can each also together form" heterocyclyl ";
  • Q209, Q210, Q21 1 are independently selected from the group consisting of: "alkyl, (C 9 -C 30 ) alkyl, cycloalkyl, cycloalkylalkyl, heterocyclyl, heterocyclylalkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl” and wherein alternatively Q166 , Q167 and / or Q175, Q176 and / or Q188, Q189 and / or Q195, Q196 and / or Q204, Q205 may each together also form "heterocyclyl"; in which optional substituents of the substituent group (i) may in turn be substituted independently of one another with at least one substituent, identical or different, selected from the group consisting of:
  • Q239, Q240, Q241, Q242, Q243, Q244, Q245, Q246, Q247, Q248, Q249, Q250, Q251, Q252, Q253, Q254, Q255, Q256, Q257, Q258, Q259, Q260, Q261, Q262, Q263 independent are selected from the group consisting of: "alkyl,
  • substituents of the substituent group (ii) above may in turn be substituted independently of one another with at least one substituent, identical or different, selected from the group consisting of:
  • Q290, Q291, Q292, Q293, Q294, Q295, Q296, Q297, Q298, Q299, Q300, Q301, Q302, Q303, Q304, Q305, Q306, Q307, Q308, Q309, Q310, Q31 1, Q312, Q313, Q314 are Q315 independently selected from the group consist- ing of: "alkyl, (Cg-C 3 o) alkyl, cycloalkyl, cycloalkylalkyl, hetero- rocyclyl, heterocyclylalkyl, aryl, arylalkyl, heteroaryl, heteroary- lalkyl" and wherein alternatively Q270 , Q271 and / or Q279, Q280 and / or Q292, Q293 and / or Q299, Q300 and / or Q308, Q309 may together also form "heterocyclyl";
  • Z10, Z11 or none of Z10, Z11 is independently selected from the group consisting of:
  • Q361, Q362, Q363, Q364, Q365, Q366, Q367, Q368, Q369, Q370, Q371, Q372, Q373 are independently selected from the group consisting of: "alkyl, (C 9 -C 3 o) alkyl, cycloalkyl, cycloalkylalkyl, heterocyclyl, heterocyclylalkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, and alternatively Q328, Q329 and / or Q337, Q338 and / or
  • Q350, Q351 and / or Q357, Q358 and / or Q366, Q367 may together also form "heterocyclyl", where optionally substituents of the substituent group (i) above may be substituted independently of one another by at least one substituent, identical or different, selected from the group consisting of:
  • Q401, Q402, Q403, Q404, Q405, Q406, Q407, Q408, Q409, Q410, Q411, Q412, Q413, Q414, Q415, Q416, Q417, Q418, Q419, Q420, Q421, Q422, Q423, Q424, Q425 independent are selected from the group consisting of: "alkyl,
  • substituents of the substituent group (ii) above may in turn be substituted independently of one another with at least one substituent, identical or different, selected from the group consisting of:
  • Q456e, Q456f, Q456g, Q456h, Q456i, Q456J, Q456k, Q456I, Q456m, Q456n, Q456o, Q456p, Q456q, Q456r, Q456s, Q456t, Q456u, Q456v are independently selected from the group consisting of: "alkyl, (C 9 -C 3 o) alkyl, cycloalkyl, cycloalkylalkyl, heterocyclyl, heterocyclylalkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl "and wherein alternatively Q432, Q433 and / or Q441, Q442 and / or Q454, Q455 and / or Q456f, Q456g and / or Q456o, Q456p may together also form "heterocyclyl";
  • Z3, Z4 or none of Z3, Z4 is independently selected from the group consisting of:
  • alkyl (Cg-C 30) alkyl, cycloalkyl, cycloalkylalkyl, heterocyclyl, heterocycloalkyl lylalkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, F, Cl, Br, I, CN, CF 3,
  • Q506, Q507, Q508 are independently selected from the group consisting of: "alkyl, (Cg-C 3 o) alkyl, cycloalkyl, cycloalkylalkyl, heterocyclyl, heterocyclylalkyl, aryl, arylalkyl, heteroaryl, heteroarylal- alkyl" and wherein alternatively Q463, Q464 and / or Q472, Q473 and / or Q485, Q486 and / or Q492, Q493 and / or Q501, Q502 may together also form "heterocyclyl"; in which optional substituents of the substituent group (i) may in turn be substituted independently of one another with at least one substituent, identical or different, selected from the group consisting of:
  • Q545, Q546, Q547, Q548, Q549, Q550, Q551, Q552, Q553, Q554, Q555, Q556, Q557, Q558, Q559, Q560 are independently selected from the group consisting of: "alkyl, (C 9 -C 3 o) alkyl, cycloalkyl, cycloalkylalkyl, heterocyclyl, heterocyclic
  • alkyl (C 3 -C 30) alkyl, cycloalkyl, cycloalkylalkyl, heterocyclyl, heterocyclylalkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, F, Cl,
  • Q605, Q606, Q607, Q608, Q609, Q610, Q611 are, Q612 independently selected from the group consisting of: "alkyl, (Cg-C 3 o) alkyl, cycloalkyl, cycloalkylalkyl, hetero- rocyclyl, heterocyclylalkyl, aryl, arylalkyl heteroaryl, heteroarylalkyl "and wherein alternatively Q567, Q568 and / or Q576, Q577 and / or Q589, Q590 and / or Q596, Q597 and / or Q605, Q606 may each together also form" heterocyclyl ";
  • Q642, Q643, Q644, Q645, Q646, Q647, Q648, Q649, Q650, Q651, Q652, Q653, Q654, Q655, Q656, Q657, Q658, Q659, Q660, Q661, Q662, Q663, Q664 are selected independently from each other consisting of the group consisting of: "alkyl, (C 9 -C 3 o) alkyl, cycloalkyl, cycloalkylalkyl, heterocyclyl, heterocyclylalkyl, aryl, arylalkyl, heteroaryl, heteroarylal- alkyl" and wherein alternatively Q619, Q620 and / or Q628, Q629 and / or Q641, Q642 and / or Q648, Q649 and / or Q657, Q658 may each together also form "heterocyclyl"; in which optionally above substituents of the substituent group (i) can in turn be substituted independently of one another with
  • alkyl (C 9 -C 30 ) alkyl, cycloalkyl, cycloalkylalkyl, heterocyclyl, heterocyclylalkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, F, Cl, Br, I, CN, CF 3 , N 3 , NH 2 , -NHQ665, -NQ666Q667, -NO 2 , -OH, -OCF 3 ,
  • heteroaryl radical may be substituted by at least one substituent, identical or different, selected from the group consisting of:
  • Q788, Q789, Q790, Q791, Q792, Q793, Q794, Q795, Q796, Q797, Q798, Q799, Q800, Q801, Q802, Q803, Q804, Q805, Q806, Q807, Q808, Q809, Q810, Q81 1, Q812 , Q813, Q814, Q815, Q816, Q817, Q818, Q819, Q820 are independently selected from the A group consisting of: "alkyl, (C 3 -C 30) alkyl, cycloalkyl, cycloalkylalkyl, heterocyclyl, heterocyclylalkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl" and wherein alternatively Q775, Q776 and / or Q784, Q785 and / or Q797 , Q798 and / or Q804, Q805 and / or Q813, Q814 together can also form "heterocyclyl
  • Q830, Q831, Q832, Q833, Q834, Q835, Q836, Q837, Q838, Q839, Q840, Q841, Q842, Q843, Q844, Q845, Q846, Q847, Q848, Q849, Q850, Q851, Q852, Q853, Q854, Q855, Q856, Q857, Q858, Q859, Q860, Q861, Q862, Q863, Q864, Q865, Q866, Q867, Q868, Q869, Q870, Q871, Q872 are independently selected from the group consisting of: "alkyl, (Cg -C 3 o) alkyl, cycloalkyl, cycloalkylalkyl, heterocyclyl, heterocyclylalkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl "and wherein alternatively Q827, Q828 and / or Q836, Q837 and / or Q849, Q850 and
  • alkyl "alkyl, (Cg-C 30) alkyl, cycloalkyl, cycloalkylalkyl, heterocyclyl, HE terocyclylalkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, F, Cl, Br, I, CN, CF 3, N 3, NH 2 , -NHQ873, -NQ874Q875, -NO 2 , -OH,
  • OSi (Q892) (Q893) (Q894), -OS (O 2) -Q895, -NHC (O) -Q896, - NQ897C (O) -Q898, -NH-C (O) -O-Q899, -NH -C (O) -NH-Q900, -NH-C (O) -NQ901 Q902, -NQ903-C (O) -O-Q904, -NQ905-C (O) -NH-Q906, -NQ907-C ( O) -NQ908Q909, -
  • Q961, Q962, Q963, Q964, Q965, Q966, Q967, Q968, Q969, Q970, Q971, Q972, Q973, Q974, Q975, Q976 are independently selected from the group consisting of: "alkyl, (Cg-C 3 o) alkyl, cycloalkyl, cycloalkylalkyl, heterocyclyl, heterocyclylalkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl and, alternatively, Q931, Q932 and / or Q940, Q941 and / or Q953, Q954 and / or Q960, Q961 and / or Q969, Q970 in each case together can also form "heterocyclyl"; in which optional substituents of the substituent group (ii) may in turn be substituted independently of one another with at least one substituent, identical or different, selected from the group consisting of:
  • Q1009, Q1010, Q1011, Q1012, Q1013, Q1014, Q1015, Q1016, Q1017, Q1018, Q1019, Q1020, Q1021, Q1022, Q1023, Q1024, Q1025, Q1026, Q1027, Q1028 are independently selected from the group consisting of: "Alkyl, (Cg-C 3 o) alkyl, cycloalkyl, cycloalkylalkyl, heterocyclyl, HE terocyclylalkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl” and wherein alternatively Q983, Q984 and / or Q992, Q993 and / or Q1005, Q1006 and / or Q1012, Q1013 and / or Q1021, Q1022 may together also form "heterocyclyl";
  • substituent group (i) "hydrogen, alkyl, (Cg-C 30) alkyl, cycloalkyl, cycloalkylalkyl, heterocyclyl, heterocyclylalkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl"; wherein optionally above substituents of substituent group (i) in turn may be independently substituted with at least a substituent, the same or different, selected from the group consisting of:
  • C 30 alkyl, cycloalkyl, cycloalkylalkyl, heterocyclyl, heterocyclylalkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl and, alternatively, Q1035, Q1036 and / or Q1044, Q1045 and / or Q1057, Q1058 and / or Q1064, Q1065 and / or Q1073, Q1074 can together also form "heterocyclyl"; in which optional substituents of the substituent group (ii) may in turn be substituted independently of one another with at least one substituent, identical or different, selected from the group consisting of:
  • Q1130, Q1131 are, Q1132 independently selected from the group consisting of: "alkyl, (Cg-C 30) alkyl, Cyc loalkyl, cycloalkylalkyl, heterocyclyl, heterocyclylalkyl, aryl, ary lalkyl, heteroaryl, heteroarylalkyl” and wherein alternatively Q1087 , Q1088 and / or Q1096, Q1097 and / or Q1 109, Q1 110 and / or Q1 116, Q1 117 and / or Q1 125, Q1 126 may together also form "heterocyclyl";
  • NZ8Z9 wherein Z8, Z9 are independently selected from the group consisting of:
  • OSi (QI 158) (Q1 159) (Q1 160), -0S (0 2 ) -Q1 161, -NHC (O) -Q1162, -NQ1 163C (O) -Q1 164, -NH-C (O) - O-Q1 165, -NH-C (O) -NH-Q1166, -NH-C (O) -NQ1 167Q1 168, -NQ1169-C (O) -O-Q1 170, -NQ1171 -C (O) - NH-Q1 172, -NQ1173-C (O) -NQ1174Q1 175, - 10 NHS (0 2) -Q1 176, -NQ1177S (O 2) -Q1178, -S-Q1179, -S (O) -
  • (Cg-C 30) alkyl, alkyl, cycloalkyl, cycloalkylalkyl, heterocyclyl, heterocyclylalkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl and wherein alternatively: 20 Q1186, Q1187, Q1188, Q1189, Q1190 independently selected from the group consisting of Q1145, Q1146 and / or Q1154, Q1155 and / or Q1 167, Q1 168
  • Q1233, Q1234, Q1235, Q1236, Q1237, Q1238, Q1239, Q1240, Q1241, Q1242 are independently selected from the group consisting of: "alkyl, (Cg-C3o) alkyl, cycloalkyl, cycloalkylalkyl, heterocyclyl, heterocyclylalkyl, aryl , arylalkyl, heteroaryl, heteroarylalkyl "and alternatively Q1 197,
  • Q1198 and / or Q1206, Q1207 and / or Q1219, Q1220 and / or Q1226, Q1227 and / or Q1235, Q1236 may together also form "heterocyclyl";
  • U100, U101, U 102, U103, U104 are independently selected from the group consisting of: "alkyl, (C 9 -C 3 o) alkyl, cycloalkyl, cycloalkylalkyl, heterocyclyl, heterocyclylalkyl, aryl, ary lalkyl, heteroaryl, heteroarylalkyl "and alternatively U59, U60 and / or U68, U69 and / or U81, U82 and / or U88, U89
  • U98 may in each case also form "heterocyclyl", where optionally substituted substituents of substituent group (ii) may in turn be substituted independently with at least one substituent, identical or different, selected from the group consisting of:
  • alkyl "alkyl, (C 3 -C 30) alkyl, cycloalkyl, cycloalkylalkyl, heterocyclyl, heterocyclylalkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, F, Cl, Br, I, CN, CF 3 , N 3 , NH 2 , -NHU105, -NU106U107, -NO 2 , -OH, -OCF 3 , -SH, -O-SO 3 H, -OP (O) (OH) 2 , -CHO, -COOH, -
  • U151, -P (O) (OU152) (OU153), -Si (U154) (U155) (U156) ", where U105, U106, U107, U108, U10g, U110, U111, U112, U113, U114, U115, U116, U117, U118, U119, U120, U121, U122, U123, U124, U125, U126, U127, U128, U12g, U130, U131, U132, U133, U134, U135, U136, U137, U138, U139, U140, U141, U142, U143, U144, U145, U146, U147, U148, U149, U150, U151, U152, U153, U154, U155, U156 are independently selected from the group consisting of: "alkyl, (Cg-C 3 o) alkyl, cycloalkyl, cycloalkylalkyl, heterocycloalkyl
  • heterocyclylalkyl aryl, arylalkyl, heteroaryl, heteroarylalkyl "and where alternatively U1 11, U1 12 and / or U 120, U 121 and / or U133, U134 and / or U140, U141 and / or U149, U150 also together in each case" heterocyclyl "can form;
  • Z23 is independently selected from the group consisting of:
  • substitution group (a) "hydrogen, alkyl, (C 3 -C 30) alkyl, cycloalkyl, cycloalkylalkyl, heterocyclyl, heterocyclylalkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl"; wherein above substituents of the substitution group (a) may be independently optionally substituted with at least a substituent, the same or different, selected from the group consisting of:
  • alkyl (C 3 -C 30) alkyl, cycloalkyl, cycloalkylalkyl, heterocyclyl, heterocyclylalkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, F, Cl, Br, I,
  • (Cg-C 3 o) alkyl, cycloalkyl, cyclo- alkylalkyl, heterocyclyl, heterocyclylalkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl alkyl are U206, U207, U208 independently selected from the group consisting of , U 164 and / or U 172,
  • U202 may in each case also form "heterocyclyl", where optionally substituted substituents of the substituent group (i) may in turn be substituted independently of one another with at least one substituent, identical or different, selected from the group consisting of:
  • alkyl (Cg-C 3 o) alkyl, cycloalkyl, cycloalkylalkyl, heterocycloalkyl
  • heterocyclylalkyl aryl, arylalkyl, heteroaryl, heteroarylalkyl "and where alternatively U215, U216 and / or U224, U225 and / or U237, U238 and / or U244, U245 and / or U253, U254 may together also also form" heterocyclyl " ;
  • (ii) may in turn be independently substituted with at least one substituent, the same or different, selected from the group consisting of:
  • NU289U290 -NU291-C (O) -O-U292, -N11293-C (O) -NH- U294, -NU295-C (O) -NU296U297, -NHS (O 2) -U298, - NU299S (O 2 ) -U300, U301 -S, -S (O) -U302, -S (O 2) -U303, -S (O 2) NH-U304, -S (O 2) NU305U306, -S (O 2) O-U307, -
  • alkyl (C 9 -C 3 o) alkyl, cycloalkyl, cycloalkylalkyl, heterocyclyl, hetero- rocyclylalkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, F, Cl, Br,
  • U376, U377, U378, U379, U380, U381, U382, U383, U384, U385, U386, U387, U388, U389, U390, U391, U392, U393, U394, U395, U396, U397, U398, U399, U400, U401, U402, U403, U404, U405, U406, U407, U408, U409, U410, U411, U412, U413, U414, U415, U416, U417, U418, U419 are independently selected from the group consisting of: "alkyl, (Cg-C 3 o) alkyl, cycloalkyl, cycloalkylalkyl, heterocyclyl, heterocyclylalkyl, aryl, arylalkyl , heteroaryl, heteroarylalkyl "and where
  • U397 and / or U403, U404 and / or U412, U413 may together also form "heterocyclyl", where optionally substituents of the substituent group (i) above may be substituted independently of one another with
  • At least one substituent identical or different, selected from the group consisting of:
  • alkyl (C 3 -C 30) alkyl, cycloalkyl, cycloalkylalkyl, heterocyclyl, heterocyclylalkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, F, Cl, Br, I, CN, CF 3 , N 3 , NH 2 , -NHU420, -NU421 U422, -NO 2 ,
  • U464, U465 may together also form "heterocyclyl", where optionally substituents of the substituent group (ii) above may be substituted independently of one another
  • U479, U480, U481, U482, U483, U484, U485, U486, U487, U488, U489, U490, U491, U492, U493, U494, U495, U496, U497, U498, U499, U500, U501, U502, U503, U504, U505, U506, U507, U508, U509, U510, U511, U512, U513, U514, U515, U516, U517, U518, U519, U520, U521, U522, U523 are independently selected from the group consisting of: "alkyl, (C 9 -C 3 o) alkyl, cycloalkyl, cycloalkylalkyl, heterocyclyl, heterocyclylalkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl "and where alternatively U478, U479 and / or U487, U488 and / or U500,
  • Rest Z5 is independently selected from the group consisting of:
  • A44, A45, A46, A47, A48, A49, A50, A51, A52 are independently selected from the group consisting of: "alkyl, (Cg-C 3 o) alkyl, cycloalkyl, cycloalkylalkyl, heterocyclyl, heterocyclylalkyl, aryl, arylalkyl , heteroaryl, het eroarylalkyl "and wherein alternatively A7, A8 and / or A16, A17 and / or A29, A30 and / or A36, A37 and / or A45, A46 may together also form" heterocyclyl "; wherein optionally substituents of the substituent group (i) above may in turn be substituted independently of one another with at least one substituent, identical or different, selected from the group consisting of:
  • A65, A66, A67, A68, A69, A70, A71, A72, A73, A74, A75, A76, A77, A78, A79, A80, A81, A82, A83, A84, A85, A86, A87, A88, A89, A90, A91, A92, A93, A94, A95, A96, A97, A98, A99, A100, A101, A102, A103, A104 are independently selected from the group consisting of: alkyl "alkyl, (Cg-C 30), cycloalkyl, cycloalkylalkyl, heterocyclyl, heterocyclylalkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl "and where alternatively A59, A60 and / or A68, A69 and / or A81, A82 and / or A88, A89 and / or A97, A98 in each case together also "heterocyclyl"
  • A124, A125, A126, A127, A128, A129, A130, A131, A132, A133, A134, A135, A136, A137, A138, A139, A140, A141, A142, A143, A144, A145, A146, A147, A148, A149, A150, A151, A152, A153, A154, A155, A156 are independently selected from the group consisting of: alkyl, (C 9 -C 30 ) alkyl, cycloalkyl, cycloalkylalkyl, heterocyclyl, heterocyclylalkyl, aryl, arylalkyl, heteroaryl "heteroarylalkyl” and wherein alternatively A11 1, A1 12 and / or A120, A121 and / or A133, A134 and / or A140, A141 and / or A149, A150 may together also form "heterocyclyl";
  • one of the radicals Z1, Z2 or both radicals Z1, Z2 are independently selected from the group consisting of: (a) -NZ24Z25; with the proviso that one of the radicals Z24, Z25 or both radicals Z24, Z25 are selected independently of one another from the group consisting of: (1) ,, - C (O) -C (O) -TI, -S (O 2) -NT2T3 "; wherein T1, T2, T3 are independently selected from the group consisting of:
  • T4 T5, T6, T7, T8, T9, T10, T11, T12, T13, T14, T15, T16, T17, T18, T19, T20, T21, T22, T23, T24, T25, T26, T27, T28, T29, T30, T31, T32, T33, T34, T35, T36, T37, T38, T39, T40, T41, T42,
  • T43, T44, T45, T46, T47, T48, T49, T50, T51, T52, T53, T54, T55 are independently selected from the group consisting of: "alkyl, (Cg-C 3 o) alkyl, cycloalkyl, cycloalkylalkyl , heterocyc IyI, heterocyclylalkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl "and alternatively T10, T1 1 and / or T19, T20 and / or T32, T33 and / or T39, T40 and / or T48, T49 also together" terocyclyl "can form; wherein optionally substituted substituents of the substitution group (I) independently of one another can also be further substituted by at least one substituent, identical or different, selected from the group consisting of:
  • OSi T75) (T76) (T77), -OS (O 2) -T78, -NHC (O) -T79, -NT80C (O) - T81, -NH-C (O) -O-T82, -N HC (O) -NH-T83, -NH-C (O) -NT84T85, -NT86-C (O) -O-T87, -NT88-C (O) -NH-T89, -NT90-C (O ) -NT91T92, -NHS (O 2 ) -T93, -NT94S (O 2 ) -T95, -S-T96, -
  • T56 T57, T58, T59, T60, T61, T62, T63, T64, T65, T66, T67, T68, T69, T70, T71, T72, T73, T74, T75, T76, T77, T78, T79, T80, T81, T82, T83, T84, T85, T86, T87, T88, T89, T90,
  • T103, T104, T105, T106, T107 are independently selected from the group consisting of: "alkyl, (Cg-C 3 o) alkyl, cycloalkyl, cycloalkylalkyl, heterocyclyl, heterocyclylalkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl" and wherein alternatively T62,
  • T101 may together also form "heterocyclyl", where optionally substituents of the substituent group (i) above may be substituted independently of one another With
  • At least one substituent identical or different, selected from the group consisting of:
  • alkyl (Cg-C 30) alkyl, cycloalkyl, cycloalkylalkyl, heterocyclyl, heterocyclylalkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, F, Cl, Br, I, CN, CF 3, N 3, NH 2, - NHT108, -NT109T110, -NO 2 , -
  • T153 may in each case also form "heterocyclyl", where optionally substituted substituents of the substituent group (ii) may in turn be substituted independently of one another with at least one substituent, identical or different, selected from the group consisting of:
  • NT195T196 -NHS (O 2) -T197, -NT198S (O 2) -T199, -S- T200, -S (O) -T201, -S (O 2) -T202, -S (O 2) NH- T203, - S (O 2) NT204T205, -S (O 2) O-T206, - P (O) (OT207) (OT208), -Si (T209) (T210), (T211) "; wherein T160, T161, T162, T163, T164, T165, T166, T167,
  • T168, T169, T170, T171, T172, T173, T174, T175, T176, T177, T178, T179, T180, T181, T182, T183, T184, T185, T186, T187, T188, T189, T190, T191, T192, T193, T194, T195, T196, T197, T198, T199, T200, T201, T202, T203, T204, T205, T206, T207, T208, T209, T210, T21 1 are independently selected from the group consisting of: "alkyl , (Cg-C 3 o) alkyl, cycloalkyl, cycloalkylal- kyl, heterocyclyl, heterocyclylalkyl, aryl, arylalkyl, heteroaromatics ryl, heteroarylalkyl "and wherein alternatively T166, T167 and / or T175, T176 and / or T188, T189, and / or
  • T195, T196 and / or T204, T205 may together also form “heterocyclyl”; alternatively, T2, T3 may together also form “heterocyclyl”;
  • Z24, Z25 or none of Z24, Z25 is also independently selected from the group consisting of:
  • T261, T262, T263 are independently selected from the group consisting of: "alkyl, (C 9 -C 30 ) alkyl, cycloalkyl, cycloalkylalkyl, heterocyclyl, heterocyclylalkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl” and alternatively T218, T219 and or T227, T228 and / or T240, T241 and / or T247, T248 and / or T256, T257 may each together also form "heterocyclyl"; in which optional substituents of the substituent group (i) may in turn be substituted independently of one another with at least one substituent, identical or different, selected from the group consisting of:
  • T293, T294, T295, T296, T297, T298, T299, T300, T301, T302, T303, T304, T305, T306, T307, T308, T309, T310, T311, T312, T313, T314, T315 are independently selected from consisting of the group consisting of: "alkyl, (C 9 -C 3 o) alkyl, cycloalkyl, Cyc
  • T270, T271 and / or T279, T280 and / or T292, T293 and / or T299, T300 and / or T308, T309 also together in each case also Can form "heterocyclyl";
  • substituents of the substituent group (ii) above may in turn be substituted independently of one another with at least one substituent, identical or different, selected from the group consisting of:
  • T366 Si (T365) (T366) (T367) "; wherein T316, T317, T318, T319, T320, T321, T322, T323, T324, T325, T326, T327, T328, T329, T330, T331, T332, T333, T334 , T335, T336, T337, T338, T339, T340, T341, T342, T343, T344, T345, T346, T347, T348, T349, T350,
  • T351, T352, T353, T354, T355, T356, T357, T358, T359, T360, T361, T362, T363, T364, T365, T366, T367 are independently selected from the group consisting of: "alkyl, (Cg-C3o ) alkyl, cycloalkyl, cycloalkylalkyl, heterocyclyl, heterocyclylalkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl and where alternatively T322, T323 and / or T331, T332 and / or T344, T345 and / or T351, T352 and / or T360, T361 may together also form "heterocyclyl";
  • radicals Z26, Z27 or both radicals Z26, Z27 are independently selected from the group consisting of:
  • T377, T378, T379, T380, T381, T382, T383, T384, T385, T386, T387, T388, T389, T390, T391, T392, T393, T394, T395, T396, T397, T398, T399, T400, T401, T402, T403, T404 are independently selected from the group consisting of:
  • alkyl, (Cg-C 3 o) alkyl, cycloalkyl, cycloalkylalkyl, heterocyclyl, heterocyclylalkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl and wherein alternatively T374, T375 and / or T381, T382 and / or T391, T392 and or T398, T399 may together also form "heterocyclyl";
  • substituents of the substituent group (i) may in turn be further independently substituted with at least one substituent, identical or different, selected from the group consisting of:
  • NT437-C (O) -NH-T438, -NT439-C (O) -NT440T441, - NHS (O 2) -T442, -NT443S (O 2) -T444, -S-T445, -S (O) - T446, -S (O 2) -T447, -S (O 2) N H-T448, -S (O 2) NT449T450, - S (O 2) O-T451, -P (O) (OT452) (OT453), - Si (T454) (T455), (T456) "; wherein T405, T406, T407, T408, T409, T410, T411, T412 , T413, T414, T415, T416, T417, T418, T419, T420, T421,
  • T431, T432, T433, T434, T435, T436, T437, T438, T439, T440, T441, T442, T443, T444, T445, T446, T447, T448, T449, T450, T451, T452, T453, T454, T455, T456 are independently selected from the group consisting of
  • T41 1, T412 and / or T420, T421 and or T433, T434 and / or T440, T441 and / or T449, T450 may together also form "heterocyclyl";
  • (ii) may in turn be independently substituted with at least one substituent, the same or different, selected from the group consisting of:
  • T483, T484, T485, T486, T487, T488, T489, T490, T491, T492, T493, T494, T495, T496, T497, T498, T499, T500, T501, T502, T503, T504, T505, T506, T507, T508 are independently selected from the group con- sisting of: "alkyl, (Cg-C 3 o) alkyl, cycloalkyl, cycloalkylal- kyl, heterocyclyl, heterocyclylalkyl, aryl, arylalkyl, heteroaromatics ryl, heteroarylalkyl" and wherein alternatively T463, T464 and / or T472, T473 and / or T485, T486 and / or T492, T493 and / or T501, T502 may together also form "heterocyclyl";
  • Z28, Z29 and at least one of Z30 is Z31 independently selected from the group consisting of: (II) "(Cg-C 3 o) alkyl, cycloalkylalkyl, heterocyclylalkyl, arylalkyl, heteroarylalkyl, -C (O) - (C 9 -C 30 ) alkyl, -C (O) -cycloalkyl, -C (O) -cycloalkylalkyl, -C (O) -arylalkyl, -C (O) -heteroarylalkyl, - C (O) -heterocyclyl, -C (O) - heterocyclylalkyl, -S (O 2) alkyl, -S (0 2) - (C 9 -C 3 O) alkyl, -S (O 2) - cycloalkyl, (2 O) -S cycloalkyl,
  • substitution group (II) may be independently further substituted with at least one substituent, same or different, selected from the group consisting of:
  • T587, T588, T589, T590, T591, T592, T593, T594, T595, T596, T597, T598, T599, T600, T601, T602, T603, T604, T605, T606, T607, T608, T609, T610, T611, T612 are independently selected from the group consisting of
  • T606 may each together also form "heterocyclyl";
  • (ii) may in turn be independently substituted with at least one substituent, the same or different, selected from the group consisting of:
  • T639, T640, T641, T642, T643, T644, T645, T646, T647, T648, T649, T650, T651, T652, T653, T654, T655, T656, T657, T658, T659, T660, T661, T662, T663, T664 are independently selected from the group con- sisting of: "alkyl, (C 9 -C 3 o) alkyl, cycloalkyl, cycloalkylal- kyl, heterocyclyl, heterocyclylalkyl, aryl, arylalkyl, heteroaromatics ryl, heteroarylalkyl" and wherein alternatively T619 , T620 and / or T628, T629 and / or T641, T642 and / or T648, T649 and / or T657, T658 may each together also form "heterocyclyl";
  • Z28, Z29 or none of Z28, Z29 and Z30, Z31 or none of Z30, Z31 and Z32 is independently selected from the group consisting of: (III) "hydrogen, alkyl, cycloalkyl, heterocyclyl, aryl, heteroaryl, -C (O) -alkyl, -C (O) -aryl, -C (O) -heteroaryl ", where optionally above substituents of the substituent group (IM) may in turn be substituted independently of one another with at least one substituent, identical or different, selected from the group consisting of:
  • T684, T685, T686, T687, T688, T689, T690, T691, T692, T693, T694, T695, T696, T697, T698, T699, T700, T701, T702, T703, T704, T705, T706, T707, T708, T709, T710, T71 1, T712, T713, T714, T715, T716 are independently selected from the group consisting of: "alkyl, (C 9 -C 30 ) -alkyl, cycloalkyl, cycloalkylalkyl, heterocyclyl, heterocyclylalkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl "and where alternatively T671, T672 and / or T680, T681 and / or T693, T694 and / or T700, T701 and / or T709, T710 may together also also form" heterocyclyl "; optional
  • T734 T735, T736, T737, T738, T739, T740, T741, T742,
  • T743, T744, T745, T746, T747, T748, T749, T750, T751, T752, T753, T754, T755, T756, T757, T758, T759, T760, T761, T762, T763, T764, T765, T766, T767, T768 are independently selected from the group consisting of
  • alkyl, (C 9 -C 30 ) alkyl, cycloalkyl, cycloalkylalkyl, heterocyclyl, heterocyclylalkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl and wherein alternatively T723, T724 and / or T732, T733 and / or T745, T746 and or T752, T753 and / or T761, T762 may together also form "heterocyclyl";
  • (ii) may in turn be independently substituted with at least one substituent, the same or different, selected from the group consisting of: (iii) "alkyl, (C 9 -C 3 o) alkyl, cycloalkyl, cycloalkylalkyl, as heterocyclyl, heterocyclylalkyl, aryl, arylalkyl, heteroaryl, heteroary- lalkyl, F, Cl, Br, I, CN, CF 3, N 3 , NH 2 , -NHT769, - NT770T771, -NO 2 , -OH, -OCF 3 , -SH, -O-SO 3 H, - OP (O) (OH) 2 , -CHO, -COOH, -C (O) NH 2 , -SO 3 H, -
  • OSi (T788) (T789), (T790), -OS (O 2) -T791, -NHC (O) -T792, -NT793C (O) -T794, -NH-C (O) -O-T795, -NH -C (O) -NH-T796, -NH-C (O) -NT797T798, -NT799-C (O) -O-T800, -NT801 -C (O) -NH-T802, -NT803-C ( O) - NT804T805, -NHS (O 2) -T806, -NT807S (O 2) -T808, -S-S-
  • NT836T837 -OP (O) (OT838) (OT839), -OSi (T840) (T814), (T842), -OS (O 2) -T843, -NHC (O) -T844, -NT845C (O) -T846 , -NH-C (O) -O-T847, -NHC (O) -NH-T848, -NH-C (O) -NT849T850, -NT851-C (O) -O-T852, -NT853- C (O) -NH-T854, -NT855- C (O) -NT856T857, -NHS (O 2) -T858, -NT859S (O 2) -T860, -S-S-
  • T870, T871, T872 are independently selected from the group consisting of: "alkyl, (C 9 -C 3 o) alkyl, cycloalkyl, Cyc loalkylalkyl, heterocyclyl, heterocyclylalkyl, aryl, arylalkyl, hetero- aryl, heteroarylalkyl" and wherein alternatively T827, T828 and / or
  • T866 may together also form "heterocyclyl", wherein optionally substituents of the substituent group (i) above may also be further substituted independently of one another
  • alkyl (C 9 -C 30 ) alkyl, cycloalkyl, cycloalkylalkyl, heterocyclyl, heterocyclylalkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, F, Cl, Br, I, CN, CF 3 , N 3 , NH 2 , -NHT873, -NT874T875, -NO 2 , -
  • OSi T892 (T893), (T894), -OS (O 2) -T895, -NHC (O) -T896 - NT897C (O) -T898, -NH-C (O) -O-T899, -NH -C (O) -NH-T900, -NH-C (O) -NT901T902, -NT903-C (O) -O-T904, - NT905-C (O) -NH-T906, -NT907-C (O ) -NT908T909, -
  • T924 T873, T874, T875, T876, T877, T878, T879, T880, T881, T882, T883, T884, T885, T886, T887, T888, T889, T890, T891, T892, T893, T894, T895, T896, T897 , T898, T899, T900, T901, T902, T903, T904, T905, T906, T907, 5 T908, T909, T910, T911, T912, T913, T914, T915, T916,
  • T917, T918, T919, T920, T921, T922, T923, T924 are independently selected from the group consisting of: "alkyl, (C 9 -C 3 o) alkyl, cycloalkyl, cycloalkylalkyl, hetero- cyclyl, heterocyclylalkyl, aryl, arylalkyl, heteroaryl, heteroaryl
  • T879, T880 and / or T888, T889 and / or T901, T902 and / or T908, T909 and / or T917, T918 may together also form "heterocyclyl"; optionally substituents of the substituent group (ii) above may be substituted independently of one another
  • NEN having at least one substituent, the same or different, selected from the group consisting of:
  • alkyl "alkyl, (C 9 -C 30 ) alkyl, cycloalkyl, cycloalkylalkyl, heterocyclyl, heterocyclylalkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, F, Cl, Br, I, CN, CF 3 , N 3 , NH 2 , -NHT925, -
  • T969, T970, T971, T972, T973, T974, T975 are, T976 independently selected from the group consisting of: "alkyl, (C 9 -C 3 o) alkyl, cycloalkyl, cycloalkylal- kyl, heterocyclyl, heterocyclylalkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl "and where alternatively T931, T932 and / or T940, T941 and / or T953, T954 and / or T960, T961 and / or T969, T970 can each also together form" heterocyclyl ";
  • radicals Z26, Z27 or none of the radicals Z26, Z27 independently of one another is also selected from the group consisting of:
  • alkyl "alkyl, (C 9 -C 3 o) alkyl, cycloalkyl, cycloalkylalkyl, heterocyclyl, hetero- cyclylalkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, -C (O) -alkyl, -
  • OSi T996) (T997), (T998), -OS (O 2) -T999, -NHC (O) -TIOOO, - NT1001C (O) -TI002, -NH-C (O) -O-TI003, -NH -C (O) -NH-TI004, -NH-C (O) -NTI005T1006, -NT1007-C (O) -O-TI008, -NT1009-C (O) -NH-TIOIO 1 -NTIOII-C (O ) -NTIO ⁇ TIOIS 1 -NHS (O 2 ) - T 1014, -NT 10 15 S (O 2 ) -T 10 16, -S-T 10 17, -S (O) -TiO 18, -S (O 2 ) -
  • T1005, T1006, T1007, T1008, T1009, T1010, T1011, T1012, T1013, T1014, T1015, T1016, T1017, T1018, T1019, T1020, T1021, T1022, T1023, T1024, T1025, T1026, T1027, T1028 are independently selected are selected from the group consisting of: "alkyl, (C 3 -C 30) alkyl, cycloalkyl, cycloalkylalkyl, heterocyclyl, heterocyclylalkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl” and alternatively T983, T984 and / or T992, T993 and / or T1005, T1006 and / or T1012, T1013 and / or T1021, T1022 may together also form "heterocyclyl"; in which optional substituents of substituent group (i) may in turn also be further substituted with at least one substituent
  • T1056 -NH-C (O) -NTI057T1058, -NT1059-C (O) -O-TI060, -NT1061-C (O) -NH-TI062, -NT1063-C (O) -NTI064T1065, -NHS (O 2) -T1066, -NT1067S (O 2) -T1068, -S-T1069, -S (O) - T1070, -S (O 2) -T1071, -S (O 2) NH-TI072, -S (O 2 ) NTI073T1074, -S (O 2 ) O-TI075, -P (O) (OTI076) (OT1077),
  • T1060, T1061, T1062, T1063, T1064, T1065, T1066, T1067, T1068, T1069, T1070, T1071, T1072, T1073, T1074, T1075, T1076, T1077, T1078, T1079, T1080 are independently selected from the group consisting of "Alkyl, (C 9 -C 30 ) alkyl, cycloalkyl, cycloalkylalkyl, heterocyclyl, heterocyclicalkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl" and alternatively T 1035, T 1036 and / or T 1044, T 1045 and / or T 1057, T 1058 and or T1064, T1065 and / or T1073, T1074 may together also form "heterocyclyl"; in which optional substituents of the substituent group (ii) may in turn be substituted independently of one another with at least one substituent, identical or different, selected from the group consisting of
  • alkyl "alkyl, (C 9 -C 30 ) alkyl, cycloalkyl, cycloalkylalkyl, heterocyclyl, heterocyclylalkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, F, Cl, Br, I, CN, CF 3 , N 3 , NH 2 , -NHT1081, -NT1082T1083, - NO 2 , -OH, -OCF 3 , -SH, -O-SO 3 H, -OP (O) (OH) 2 , -CHO, -COOH, -C (O) NH 2 , -SO 3 H, -P (O) (OH) 2 , -C (O) -Ti 084, -
  • T1 126 may together also form "heterocyclyl"; and one of the radicals Z1, Z2 or none of the radicals Z1, Z2 is independently selected from the group consisting of:
  • T1 172, T1173, T1 174, T1175, T1176, T1177, T1 178, T1179, T1 180, T1181, T1 182, T1 183, T1184 are independently selected from the group consisting of: "alkyl, (Cg -
  • T1 139, T1140 and / or T1148, T1 149 and / or T1 161, T1162 and / or T1168, T1 169 and T1177, T1 178 may together also form "heterocyclyl"; optionally optionally substituents of the substituent group (c) may be further independently substituted with at least one substituent, same or different, selected from the group consisting of: "Alkyl, (C 3 -C 30) alkyl, cycloalkyl, cycloalkylalkyl, heterocyclyl, heterocyclylalkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, F, Cl, Br, I, CN, CF 3 , N
  • T1234 (T1235) (T1236) "where T1 185, T1186, T1 187, T1188, T1189, T1190, T1191, T1192, T1193, T1194, T1195, T1196, T1197, T1198, T1199, T1200, T1201, T1202, T1203, T1204, T1205, T1206, T1207, T1208, T1209, T1210, T1211, T1212, T1213, T1214, T1215, T1216, T1217, T1218, T1219,
  • T1220, T1221, T1222, T1223, T1224, T1225, T1226, T1227, T1228, T1229, T1230, T1231, T1232, T1233, T1234, T1235, T1236 are independently selected from the group consisting of: "alkyl, (C 9 - C 30 ) alkyl, cycloalkyl, cycloalkylalkyl, heterocyclyl, heterocyc- lylalkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl "and wherein alternatively
  • T1191, T1 192 and / or T1200, T1201 and / or T1213, T1214 and / or T1220, T1221 and / or T1229, T1230 may together also form "heterocyclyl", where optionally substituents of the substituent group (i) above are also independent may be substituted with at least one substituent, identical or different, selected from the group consisting of:
  • NT1269-C (O) -NH-T1270, -NT1271-C (O) -NT1272T1273, - NHS (O 2) -T1274, -NT1275S (O 2) -T1276, -S-T1277, -S (O) - T1278, -S (O 2) -T1279, -S (O 2) NH-T1280, -S (O 2) NT1281T1282, - S (O 2) O-TI283, -P (O) (OTI284) (OT1285) , Si (T1286) (T1287) (T1288) "; wherein T1237, T1238, T1239, T1240, T1241, T1242, T1243, T1244, T1245, T1246, T1247, T1248, T1249, T1250, T1251, T1252, T1253, T1254 , T1255, T1256, T1257, T1258, T1259, T1260, T126
  • T1277, T1278, T1279, T1280, T1281, T1282, T1283, T1284, T1285, T1286, T1287, T1288 independently selected from the group consisting of: "alkyl, (Cg-C 30) alkyl, cycloalkyl, cycloalkylalkyl, heterocyclyl, heterocyclylalkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl "and wherein alternatively
  • T1243, T1244 and / or T1252, T1253 and / or T1265, T1266 and / or T1272, T1273 and / or T1281, T1282 may together also form "heterocyclyl";
  • OSi (T1308) (T1309) (T1310), - OS (O 2) -T1311, -NHC (O) -T1312, - NT1313C (O) -TI314, -NH-C (O) -O-TI315, -NH -C (O) -NH-T1316, -NH-C (O) -NTI317T1318, -NT1319-C (O) -O-TI320, -NT1321-C (O) -NH-T1322, -NT1323-C (O ) -NTI324T1325, - NHS (O 2 ) -T 1326, -NT 1327S (O 2 ) -T 1328, -S-T 1329, -S (O) -
  • T1304, T1305, T1306, T1307, T1308, T1309, T1310, T1311, T1312, T1313, T1314, T1315, T1316, T1317, T1318, T1319, T1320, T1321, T1322, T1323, T1324, T1325, T1326, T1327, T1328, are T1329, T1330, T1331, T1332, T1333, T1334, T1335, T1336, T1337, T1338, T1339, T1340 independently selected from the group consisting of: "alkyl, (C 9 - C 3 o) alkyl, cycloalkyl, cycloalkylalkyl, heterocyclyl, heterocyclylalkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl "and alternatively T1295, T1296 and / or T1304, T1305 and / or T1317, T1318 and / or T1324, T1325 and
  • alkyl "alkyl, (Cg-C 30) alkyl, cycloalkyl, cycloalkylalkyl, heterocyclyl, HE terocyclylalkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, F, Cl, Br, I, CN, CF 3, N 3, NH 2 , -NHT1341, -NT1342T1343, -NO 2 , -
  • alkyl "alkyl, (Cg-C 30) alkyl, cycloalkyl, cycloalkylalkyl, heterocyclyl, heterocyclylalkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, F, Cl, Br, I, CN, CF 3, N 3, NH 2, - NHT1393, -NT1394T1395,
  • NT1408T1409 -OP (O) (OTI410) (OTI411), - OSi (T1412) (T1413) (T1414), -OS (O 2) -T1415, -NHC (O) - T1416, -NT1417C (O) -T1418 , -NH-C (O) -O-TI419, -NH-C (O) -NH-TI420, -NH-C (O) -NT1421T1422, -NT1423-
  • T1400 T1401, T1402, T1403, T1404, T1405, T1406, T1407, T1408, T1409, T1410, T1411, T1412, T1413, T1414, T1415, T1416, T1417, T1418, T1419, T1420, T1421, T1422, T1423, T1424, T1425, T1426, T1427,
  • T1435, T1436, T1437, T1438, T1439, T1440, T1441, T1442, T1443, T1444 are independently selected from the group consisting of: "alkyl, (C 9 -C 30 ) -alkyl, cycloalkyl, cycloalkylalkyl, heterocyclyl, heterocyclylalkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl "and where alternatively T1399, T1400 and / or T1408, T1409 and / or T1421, T1422 and / or T1428, T1429 and / or T1437, T1438 can in each case also form" heterocyclyl ";
  • T1445, T1446, T1447 are independently selected from the group consisting of: (I)" hydrogen , alkyl, (C 9 -C 3 o) alkyl, cycloalkyl, cycloalkylalkyl, heterocyclyl, heterocyclylalkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, F, Cl, Br, I, CN, CF 3, N 3, NH 2, -NHT1448 , -NT1449T1450, - NO 2 , -OH, -OCF 3 , -SH, -O-SO 3 H, -OP (O) (OH) 2 , -CHO, -COOH, -C (O) NH 2 , - SO 3 H, -P (O) (OH) 2, -C
  • T1497 T1498) (T1499) "; wherein T1448, T1449, T1450, T1451, T1452, T1453, T1454, T1455, T1456, T1457, T1458, T1459, T1460, T1461, T1462, T1463, T1464, T1465, T1466 , T1467, T1468, T1469, T1470, T1471, T1472, T1473, T1474, T1475, T1476, T1477, T1478,
  • T1479, T1480, T1481, T1482, T1483, T1484, T1485, T1486, T1487, T1488, T1489, T1490, T1491, T1492, T1493, T1494, T1495, T1496, T1497, T1498, T1499 are independently selected from the group consisting of : "Alkyl, (Cg- C 3 o) alkyl, cycloalkyl, cycloalkylalkyl, heterocyclyl, heterocyclylalkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl "and alternatively T1454, T1455 and / or T1463, T1464 and / or T1476, T1477 and / or T1483, T1484 and / or T1492 , T1493 together can also form 5 "heterocyclyl"; wherein optionally substituted substituents of the substitution group (I) may be independently further substituted with at least one substituent, same or different, selected from the
  • T1531, T1532, T1533, T1534, T1535, T1536, T1537, T1538, T1539, T1540, T1541, T1542, T1543, T1544, T1545, T1546, T1547, T1548, T1549, T1550, T1551 are independently selected from the group consisting of : "Alkyl, (Cg- C 3 o) alkyl, cycloalkyl, cycloalkylalkyl, heterocyclyl, heterocyclylalkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl and, alternatively, T1506, T1507 and / or T1515, T1516 and / or T1528, T1529 and / or T1535, T1536 and / or T1544, T1545 each may together also form "heterocyclyl"; in which optional substituents of the substituent group (i) may in turn be substituted independently of one another with at least
  • T1573, T1574, T1575, T1576, T1577, T1578, T1579, T1580, T1581, T1582, T1583, T1584, T1585, T1586, T1587, T1588, T1589, T1590, T1591, T1592, T1593, T1594, T1595, T1596, T1597, T1598, T1599, T1600, T1601, T1602, T1603 are independently selected from the group consisting of: "alkyl, (C 9 -C 3 o) alkyl, cycloalkyl, cycloalkylalkyl, heterocyclyl, heterocyclylalkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl" and wherein alter-
  • T1580, T1581 and / or T1587, T1588 and / or T1596, T1597 may together also form "heterocyclyl", wherein optionally substituents of the substituent groups above
  • 10 pe (ii) may in turn be substituted independently of one another by at least one substituent, identical or different, selected from the group consisting of:
  • T1630 -NH-C (O) -NH-TI631, -NH-C (O) -NT1632T1633, -NT1634-C (O) -O-TI635, -NT1636-C (O) -NH-TI637, -NT1638 -C (O) -NTI639T1640, - NHS (O 2) -T1641, -NT1642S (O 2) -T1643, -S-T1644, -
  • T1604 T1605, T1606, T1607 , T1608, T1609, T1610, T1611, T1612, T1613, T1614, T1615, T1616, T1617, T1618, T1619, T1620, T1621, T1622, T1623, T1624, T1625, T1626, T1627, T1628, T1629, T1630, T1631, T1632, T1633, T1634, T1635, T1636, T1637, T1638, T1639, T1640, T1641, T1642, T1643, T1644, T1645, T1646, T1647, T1648, T1649, T1650, T1651,
  • T1652, T1653, T1654 is, T1655 independently selected from the group consisting of: "alkyl, (C 9 -C 3 o) alkyl, cycloalkyl, cycloalkylalkyl, heterocyclyl, heterocyclylalkyl, aryl, arylalkyl, heteroaryl, heteroary- lalkyl" and wherein alternatively T1610, T161 1 and / or
  • T1619, T1620 and / or T1632, T1633 and / or T1639, T1640 and / or T1648, T1649 may each also together form "heterocyclyl", alternatively T1446, T1447 may together also form "heterocyclyl";
  • (I) is hydrogen, alkyl, (C 9 -C 3 o) alkyl, cycloalkyl, cycloalkylalkyl, heterocyclyl, heterocyclylalkyl, aryl, arylalkyl, heteroaryl, heteroarylal- alkyl, -C (O) alkyl, -C (0) - (C 9 -C 3 O) alkyl, -C (O) cycloalkyl, -C (O) - cycloalkylalkyl, -C (O) -aryl, -C (O) -arylalkyl, -C (O) -heteroaryl, -
  • alkyl (C 9 -C 3 o) alkyl, cycloalkyl, cycloalkylalkyl, heterocyclyl, HE terocyclylalkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, F, Cl,
  • NHT1670 -O-C (O) -NTI 671 T1672, - OP (O) (OTI 673) (OT1674), -OSi (TI 675) (T1676) (T1677), - OS (O 2 ) -T1678, NHC (O) -TI 679, -NT1680C (O) -TI 681, -NH-C (O) -O-TI 682, -NH-C (O) -NH-TI 683, -NH-C (O) -
  • T1703, T1704, T1705, T1706, T1707 are independently selected from the group consisting of: "alkyl, (C 9 -C 30 ) -alkyl, cycloalkyl, cycloalkylalkyl, heterocyclyl, heterocyclylalkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl" and whereby
  • T1684, T1685 and / or T1691, T1692 and / or T1700, T1701 in each case together can also form "heterocyclyl", where optionally substituents of the substituent group (i) optionally substituted further independently of one another may be at least one substituent, the same or different, selected from the group consisting of:
  • alkyl (C 9 -C 3 o) alkyl, cycloalkyl, cycloalkylalkyl, heterocyclyl, heterocyclylalkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl,
  • T1743, T1744, T1745, T1746, T1747, T1748, T1749, T1750, T1751, T1752, T1753, T1754, T1755, T1756, T1757, T1758, T1759 are independently selected from the group consisting of: "alkyl, (C 9 - 30) C alkyl,
  • substituent group (ii) above may in turn be substituted independently of one another with at least one substituent, identical or different, selected from the group consisting of:
  • alkyl "alkyl, (C 9 -C 30 ) alkyl, cycloalkyl, cycloalkylalkyl, heterocyclyl, heterocyclylalkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, F, Cl, Br, I, CN, CF 3 , N 3 , NH 2 , -NHT1760, -NT1761T1762, -NO 2 , -OH, -OCF 3 , -SH, -O-SO 3 H, -OP (O) (OH) 2 , -CHO, -COOH, -C (O) NH 2 , -SO 3 H, -
  • OSi (TI779) (T1780) (T1781), -OS (O 2) -T1782, - NHC (O) -TI783, -NT1784C (O) -TI785, -NH-C (O) -O- T1786, -NH -C (O) -NH-TI787, -NH-C (O) -NT1788T1789, -NT1790-C (O) -O-TI791, -NT1792-

Abstract

L’invention concerne de nouveaux dérivés de pyrido[2,3-b]pyrazine de formules générales (I) et (II), leur fabrication et leur utilisation en tant que médicaments, notamment pour le traitement de maladies malignes et autres, provoquées par une prolifération cellulaire pathologique.
PCT/EP2006/068322 2005-11-11 2006-11-10 Nouvelle pyridopyrazine et son utilisation pour la modulation de kinases WO2007054556A1 (fr)

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CN2006800507541A CN101356173B (zh) 2005-11-11 2006-11-10 新的吡啶并吡嗪和它们作为激酶调节剂的用途
EP06819385A EP1957487A1 (fr) 2005-11-11 2006-11-10 Nouvelle pyridopyrazine et son utilisation pour la modulation de kinases
CA002628039A CA2628039A1 (fr) 2005-11-11 2006-11-10 Nouvelle pyridopyrazine et son utilisation pour la modulation de kinases
RU2008123222/04A RU2515944C9 (ru) 2005-11-11 2006-11-10 ПРОИЗВОДНЫЕ ПИРИДОПИРАЗИНА, ФАРМАЦЕВТИЧЕСКАЯ КОМПОЗИЦИЯ И СПОСОБ ЛЕЧЕНИЯ ИЛИ ПРОФИЛАКТИКИ ФИЗИОЛОГИЧЕСКИХ И/ИЛИ ПАТОФИЗИОЛОГИЧЕСКИХ СОСТОЯНИЙ ПОСРЕДСТВОМ ИНГИБИРОВАНИЯ ФЕРМЕНТОВ ERK, ERK1, ERK2, PI3K, PI3Kальфа, PI3Kбета, PI3Kгамма, PI3Kдельта, PI3K-С2альфа, PI3K-С2бета, PI3K-Vps34р (ВАРИАНТЫ)
AU2006313701A AU2006313701B2 (en) 2005-11-11 2006-11-10 Novel pyridopyrazines and their use as modulators of kinases
JP2008539443A JP5527972B2 (ja) 2005-11-11 2006-11-10 新規のピリドピラジン及び前記ピリドピラジンをキナーゼのモジュレーターとして用いる使用
BRPI0618452-9A BRPI0618452A2 (pt) 2005-11-11 2006-11-10 piridopirazinas e seu uso como moduladores de cinases
KR1020087014068A KR101400905B1 (ko) 2005-11-11 2006-11-10 신규한 피리도피라진 및 키나제의 조절제로서의 이의 용도
IL191139A IL191139A0 (en) 2005-11-11 2008-04-29 Novel pyridopyrazines and their use as modulators of kinases
NO20082511A NO20082511L (no) 2005-11-11 2008-06-03 Nye pyridopyraziner og deres anvendelse som kinasemodulatorer
HK09104745.1A HK1126474A1 (en) 2005-11-11 2009-05-26 Novel pyridopyrazines and their use as modulators of kinases

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WO2009008991A3 (fr) * 2007-07-06 2009-07-09 Us Gov Nat Inst Health Modulation de la régulation d'énergie et de la fonction cérébrale par adn-pkcs
US8217042B2 (en) 2005-11-11 2012-07-10 Zentaris Gmbh Pyridopyrazines and their use as modulators of kinases
EP2508184A1 (fr) 2011-04-06 2012-10-10 Æterna Zentaris GmbH Dérivés de pyridopyrazine et leur utilisation
WO2013061080A1 (fr) 2011-10-28 2013-05-02 Astex Therapeutics Limited Pyridopyrazines anti-cancéreuses par l'inhibition de kinases de fgfr
US9290478B2 (en) 2010-11-29 2016-03-22 Astex Therapeutics Ltd Substituted quinoxalines as FGFR kinase inhibitors
US9303029B2 (en) 2011-10-28 2016-04-05 Astex Therapeutics Ltd Substituted quinoxalines as FGFR kinase inhibitors
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US9309241B2 (en) 2011-10-28 2016-04-12 Astex Therapeutics Ltd Naphthyridine derivative compounds
US9439896B2 (en) 2011-10-28 2016-09-13 Astex Therapeutics Ltd Quinolines as FGFR kinase modulators
US9447098B2 (en) 2012-05-30 2016-09-20 Astex Therapeutics Ltd Pteridines as FGFR inhibitors
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US9532938B2 (en) 2010-07-29 2017-01-03 Eastman Chemical Company Esters of O-substituted hydroxy carboxylic acids and preparations thereof
US9850228B2 (en) 2010-04-30 2017-12-26 Astex Therapeutics Ltd Pyrazolyl quinoxaline kinase inhibitors
US9902714B2 (en) 2014-03-26 2018-02-27 Astex Therapeutics Ltd Quinoxaline derivatives useful as FGFR kinase modulators
US10085982B2 (en) 2014-03-26 2018-10-02 Astex Therapeutics Ltd Combinations
US10478494B2 (en) 2015-04-03 2019-11-19 Astex Therapeutics Ltd FGFR/PD-1 combination therapy for the treatment of cancer
US10736900B2 (en) 2014-03-26 2020-08-11 Astex Therapeutics Ltd Combinations of an FGFR inhibitor and an IGF1R inhibitor
US10898482B2 (en) 2015-02-10 2021-01-26 Astex Therapeutics Ltd Pharmaceutical compositions comprising N-(3,5-dimethoxyphenyl)-N'-1 methylethyl)-N-[3-(1-methyl-1H-pyrazol-4-yl)quinoxalin-6-yl]ethane-1,2-diamine
US11155555B2 (en) 2015-09-23 2021-10-26 Janssen Pharmaceutica Nv Compounds
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WO2007079999A3 (fr) * 2005-11-11 2007-10-04 Aeterna Zentaris Gmbh Derives pyridopyrazine et utilisation
WO2007079999A2 (fr) * 2005-11-11 2007-07-19 Æterna Zentaris Gmbh Derives pyridopyrazine et utilisation
US8937068B2 (en) 2005-11-11 2015-01-20 Zentaris Gmbh Pyridopyrazine derivatives and their use
WO2008138878A3 (fr) * 2007-05-10 2009-03-19 Aeterna Zentaris Gmbh Nouveaux dérivés de pyridopyrazine, procédé de fabrication et utilisations
WO2008138878A2 (fr) * 2007-05-10 2008-11-20 Æterna Zentaris Gmbh Nouveaux dérivés de pyridopyrazine, procédé de fabrication et utilisations
EP1990342A1 (fr) * 2007-05-10 2008-11-12 AEterna Zentaris GmbH Dérivés de pyridopyrazine, processus de fabrication et utilisations correspondantes
WO2009008991A3 (fr) * 2007-07-06 2009-07-09 Us Gov Nat Inst Health Modulation de la régulation d'énergie et de la fonction cérébrale par adn-pkcs
US10519137B2 (en) 2010-04-30 2019-12-31 Astex Therapeutics Ltd Pyrazolyl quinoxaline kinase inhibitors
US9850228B2 (en) 2010-04-30 2017-12-26 Astex Therapeutics Ltd Pyrazolyl quinoxaline kinase inhibitors
US9532938B2 (en) 2010-07-29 2017-01-03 Eastman Chemical Company Esters of O-substituted hydroxy carboxylic acids and preparations thereof
US9290478B2 (en) 2010-11-29 2016-03-22 Astex Therapeutics Ltd Substituted quinoxalines as FGFR kinase inhibitors
US9856236B2 (en) 2010-11-29 2018-01-02 Astex Therapeutics Ltd Substituted quinoxalines as FGFR kinase inhibitors
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WO2012136691A1 (fr) 2011-04-06 2012-10-11 Æterna Zentaris Gmbh Dérivés de pyridopyrazine et leur utilisation
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