AR059594A1 - Derivados de 2,4-diaminopirimidinas - Google Patents
Derivados de 2,4-diaminopirimidinasInfo
- Publication number
- AR059594A1 AR059594A1 ARP070100726A ARP070100726A AR059594A1 AR 059594 A1 AR059594 A1 AR 059594A1 AR P070100726 A ARP070100726 A AR P070100726A AR P070100726 A ARP070100726 A AR P070100726A AR 059594 A1 AR059594 A1 AR 059594A1
- Authority
- AR
- Argentina
- Prior art keywords
- piperazin
- benzo
- ylamino
- trifluoromethyl
- phenylamino
- Prior art date
Links
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D498/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
- C07D498/04—Ortho-condensed systems
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P37/00—Drugs for immunological or allergic disorders
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P37/00—Drugs for immunological or allergic disorders
- A61P37/02—Immunomodulators
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
- C07D403/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
- C07D413/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
- C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
- C07D487/04—Ortho-condensed systems
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Public Health (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Immunology (AREA)
- Pain & Pain Management (AREA)
- Rheumatology (AREA)
- Communicable Diseases (AREA)
- Oncology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Plural Heterocyclic Compounds (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
Abstract
Reivindicacion 1: Compuestos de la formula general (1) en donde significan X O o N, y Y -CH2- o C=O, y R1 y R1' en cada caso independientemente entre sí, hidrogeno o un radical eventualmente sustituido una o varias veces seleccionado del grupo constituido por alquiloC1-5, cicloalquilo C3-6, arilo, heterociclilo y heteroarilo, pudiendo ser el o los sustituyentes iguales o diferentes y se seleccionan del grupo constituido por halogeno, -ORa, -C(=O)Ra, -C(=O)ORa, -C(=O)NRaRa, -NRaRa, - NRaC(=O)Ra, -NRaC(=O)ORa, -NRaC(=O)NRaRa, -NRaSO2Ra, -N=CRaRa, -SRa, -SORa, -SO2Ra, -SO2NRaRa, -NRaSO2NRaRa, -OSO2NRaRa y pseudohalogeno, o eventualmente los R1' que se encuentran en el mismo átomo de C pueden formar conjuntamente un anillo cicloalquílico C3-7, o eventualmente R1 puede estar unido con un R1' formando un puente alquílico comun de 3-6 miembros, saturado o parcialmente insaturado, el cual puede contener eventualmente uno a dos heteroátomos, y R2 un radical heterociclilo eventualmente sustituido una o varias veces, pudiendo ser el/los sustituyentes iguales o diferentes y se seleccionan del grupo constituido por alquiloC1-5, alquenilo C2-5, alquinilo C2-5, cicloalquil C3-6-alquilo C0-3 y R3 hidrogeno o alquilo C1-3 o R2 y R3 forman conjuntamente un anillo heterociclilo eventualmente una o varias veces sustituido, el cual eventualmente puede contener uno a dos heteroátomos, pudiendo ser el/los sustituyentes iguales o distintos y se seleccionan del grupo constituido por alquilo C1-5, alquenilo C2-5, alquinilo C2-5 y cicloalquil C3-6-alquilo C0-3 o un sustituyente adecuado seleccionado del grupo constituido por halogeno, -ORa, -C(=O)Ra, -C(=O)ORa, -C(=O)NRaRa, -NRaRa, -NRaC(=O)Ra, -NRaC(=O)ORa, - NRaC(=O)NRaRa, -NRaSO2Ra, -N=CRaRa, -SRa, -SORa, -SO2Ra, -SO2NRaRa, -NRaSO2NRaRa, -OSO2NRaRa y pseudohalogeno, y R4 en cada caso independientemente entre sí un radical seleccionado del grupo constituido por halogeno, NO2, -ORa, -C(=O)Ra, -C(=O)ORa, - C(=O)NRaRa, -NRaRa, -NRaCORa, -NRaC(=O)ORa, -NRaC(=O)NRaRa, -NRaC(=O)ONRaRa, -NRaSO2Ra, -N=CRaRa, -SRa, -SORa, -SO2Ra, -SO2NRaRa, -NRaSO2NRaRa, -OSO2NRaRa y pseudohalogeno; y R5 hidrogeno, halogeno, alquilo C1-3, alquenilo C2-3, alquinilo C2-3, halogeno-alquilo C1-3, -ORa o pseudohalogeno, y R6 en cada caso independientemente entre sí, un radical seleccionado del grupo constituido por halogeno, alquilo C1-3, -ORa y pseudohalogeno, y Ra en cada caso independientemente entre sí, hidrogeno o un radical seleccionado del grupo constituido por alquilo C1-8 eventualmente sustituido, alquenilo C2-8, alquinilo C2-8, cicloalquilo C3-10, arilo, heterociclilo y heteroarilo, pudiendo ser el/los sustituyentes iguales o diferentes y se seleccionan del grupo constituido por halogeno, -NH2, -OH y pseudohalogeno; y m es 0, 1 o 2; y n en cada caso independientemente entre sí, 0, 1 o 2, eventualmente en forma de sus tautomeros, sus racematos, sus enantiomeros, sus diastereoisomeros y sus mezclas, así como eventualmente sus sales farmacologicamente tolerables, con la condicion de que están excluidos 2-(2-metoxi-4-piperazin-1-il-fenilamino)-4-(3,3-dimetil-5-oxo-2,3,4,5- benzo[°][1,4]oxazepin-6-ilamino-5-trifluormetil-pirimidina, 2-(2-metoxi-4- piperazin-l-il-fenilamino)-4-((S)-4-oxo-2,3,10,10a-tetrahidro-1H,4H-9-oxa-3a-aza-benzo[°]azulen-5-ilamino-5-trifluormetil-pirimidina, 2-[4-(4-etil-piperazin-1-il)-2-metoxi-fenilamino]-4-((S)-4-oxo-2,3,10,10a-tetrahidro-1H,4H-9-oxa-3a-aza- benzo[°]azulen-5-ilamino-5-trifluormetil-pirimidina, 2-[4-(4-metil-piperazin-1-il)-2-metoxi-fenilamino]-4-((S)-4-oxo-2,3,10,10a tetrahidro-1H,4H-9-oxa-3a-aza-benzo[°]azulen-5-ilamino-5-trifluormetil-pirimidina, 3,3-dimetil-6-{2-[4-(4-metil-piperazin- 1-il)-fenilamino]-5-trifluormetil-pirimidin-4-ilamino}-3,4-dihidro-2H-benzo[°][1,4]oxazepin-5-ona, 6-{2-[4-(4-etil-piperazin-1-il)-fenilamino]-5-trifluormetil-pirimidin-4-ilamino}-3,3-dimetil-3,4-dihidro-2H-benzo[°][1,4]oxazepin-5-ona; 3,3-dimetil-6- {2-[4-(4-prop-2-inil-piperazin-1-il)-fenilamino]5trifluometil-pirimidin-4-ilamino}-3,4-dihidro-2H-benzo[°][1,4]oxazepin-5-ona, 6-{2-[4-(4-isopropil-piperazin-1-il)-fenilamino]-5-trifluormetil-pirimidin-4iIamino}-3,3-dimetil-3,4-dihidro-2H- benzo[°][1,4]oxazepin-5-ona, (S)-3-metil-6-[2-(4-piperazin-1-il-fenilamino)-5-trifluormetil-pirimidin-4-ilamino]-3,4-dihidro-2H-benzo[°][1,4]oxazepin-5-ona, (S)-3-metil-6-{2[4-(4-metil-piperazin-1-iI)-fenilamino]-5-trifluormetiI-pirimidin-4-ilamino}- 3,4-dihidro-2H-benzo[°][1,4]oxazepin-5-ona, (S)-6-{2-[4-(4-isopropil-piperazin-1-il-fenilamino]-5-trifluormetil-pirimidin-4-ilamino}-3-metil-3,4-dihidro-2H-benzo[°][1,4]oxazepin-5-ona, (S)-3-metil-6-{2-[4-(4-prop-2-iniI-piperazin-1-il)-fenilamino]-5- trifluormetil- pirimidin-4-ilamino}-3,4-dihidro-2H-benzo[°][1,4]oxazepin-5-ona, (S)-3-etil-6-[2-(4-piperazin-1-il-fenilamino)-5-trifluormetil-pirimidin-4-ilamino]-3,4-dihidro-2H-benzo[°][1,4joxazepin-5-ona, (S)-6-[2-(4-piperazin-1-il-fenilamino)-5- trifluormetil-pirimidin-4-ilamino]-3-propil-3,4-dihidro-2H-benzo[°][1,4]oxazepin-5-ona, (S)-6-{2-[4-(4-prop-2-inil-piperazin-1-il)-fenilamino]-5-trifluormetil-pirimidin-4-ilamino}-1,2,3,11a-tetrahidro-10H-benzo[e]pirrolo[1,2-a][1,4}diazepin-5,11- diona, (S)-6-{2-[4-(4-etil-piperazin-1-il)-fenilamino]-5-trifluormetil-pirimidin-4-ilamino}-1,2,3,11a-tetrahidro-10H-benzo[e]pirrolo[1,2-a][1,4]diazepin-5,11-diona, (S)-6-{2-[4-(4-isobutil-piperazin-1-il)-fenilamino]-5-trifluormetil-pirimidin-4- ilamino}-1,2,3,11a-tetrahidro-10H-benzo[e]pirrolo[1,2-a][1,4]diazepin-5,11-diona, (S)-6-{2-[4-(4-metil-piperazin-1-il)-fenilamino]-5-trifluormetil-pirimidin-4-ilamino}-1,2,3,11a-tetrahidro-10H-benzo[e]pirrolo[1,2-a][1,4]diazepin-5,11-diona, 6-{2-[4- (4-etil-piperazin-1-il)-fenilamino]-5-trifluormetil-pirimidin-4-ilamino}-3,3-dimetil-3,4-dihidro-1H-benzo[e][1,4]diazepin-2,5-diona, 3,3-dimetiI-6-{2-[4-(4-metil-piperazin-1-il)-feniIamino]-5-trifluormetiI-pirimidin-4-ilamino} -3,4-dihidro-1H- benzo[e][1,4]diazepin-2,5-diona, 6-{2-[4-(4-isopropil-piperazin-1-il)-feniIamino]-5-trifluormetiI-pirimidin-4-ilamino}-3,3-dimetil-3,4-dihidro-1H-benzo[e][1,4]diazepin-2,5-diona, 3,3-dimetil-6-{2-[4-(4-prop-2-inil-piperazin-1-i1l-fenilamino]-5- trifluormetil-pirimidin-4-ilamino}-3,4-dihidro-1H-benzo[e][1,4]diazepin-2,5-diona, (S)-6-{2-[4-(4-isopropil-piperazin-1-il)-fenilamino]-5-trifluormetil-pirimidin-4-ilamino}-1,2,3,11a-tetrahidro-10H-benzo[e]pirrolo[1,2-a][1,4]diazepin-5,11-diona, (S)- 6-{2-[4-(4-isopropil-piperazin-1-il)-fenilamino]-5-trifluormetil-pirimidin-4-ilamino}-3-metil-3,4-dihidro-1H-benzo[e][1,4]diazepin-2,5-diona, (S)-3-metil-6-{2-[4-(4-metil-piperazin-1-il)-fenilamino]-5-trifluormetil-pirimidin-4-ilamino}-3,4-dihidro- 1H-benzo[e][1,4]diazepin-2,5-diona, (S)-3-metil-6-{2-[4-(4-prop-2-inil-piperazin-1-il)-fenilamino]-5-trifluormetil-pirimidin-4-ilamino}-3,4-dihidro-1H-benzo[e][1,4]diazepin-2,5-diona, (S)-6-{2-[4-(4-etil-piperazin-1-il)-fenilamino]-5-trifluormetil- pirimidin-4-ilamino}-3-metil-3,4-dihidro-1H-benzo[e][1,4]diazepin-2,5-diona y {(S)-2,5-dioxo-6-[2-(4-piperazin-1-il-fenilamino)-5-trifluormetil-pirimidin-4-ilamino]-2,3,4,5-tetrahidro-1H-benzo[e][1,4]diazepin-3-il}-metiléster del ácido acético.
Applications Claiming Priority (1)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
EP06110303 | 2006-02-22 |
Publications (1)
Publication Number | Publication Date |
---|---|
AR059594A1 true AR059594A1 (es) | 2008-04-16 |
Family
ID=36997219
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
ARP070100726A AR059594A1 (es) | 2006-02-22 | 2007-02-21 | Derivados de 2,4-diaminopirimidinas |
Country Status (7)
Country | Link |
---|---|
US (1) | US7569561B2 (es) |
EP (1) | EP1989198B1 (es) |
JP (1) | JP5306830B2 (es) |
AR (1) | AR059594A1 (es) |
CA (1) | CA2638095C (es) |
TW (1) | TW200804364A (es) |
WO (1) | WO2007096351A1 (es) |
Families Citing this family (19)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
CA2669111C (en) | 2006-10-23 | 2016-04-12 | Cephalon, Inc. | Fused bicyclic derivatives of 2,4-diaminopyrimidine as alk and c-met inhibitors |
AU2008258560C1 (en) * | 2007-06-08 | 2014-04-10 | Janssen Pharmaceutica N.V. | Piperidine/piperazine derivatives |
AR066911A1 (es) * | 2007-06-08 | 2009-09-23 | Janssen Pharmaceutica Nv | Derivados de piperidina / piperazina |
JO2972B1 (en) * | 2007-06-08 | 2016-03-15 | جانسين فارماسوتيكا ان. في | Piperidine / piperazine derivatives |
CA2687912C (en) | 2007-06-08 | 2015-11-03 | Janssen Pharmaceutica N.V. | Piperidine/piperazine derivatives |
SI2300013T1 (en) | 2008-05-21 | 2018-03-30 | Adriad Pharmacaceuticals, Inc. | Phosphorus derivatives as kinase inhibitors |
US9273077B2 (en) | 2008-05-21 | 2016-03-01 | Ariad Pharmaceuticals, Inc. | Phosphorus derivatives as kinase inhibitors |
PE20140572A1 (es) | 2008-06-05 | 2014-05-16 | Janssen Pharmaceutica Nv | Combinaciones de drogas que comprenden un inhibidor de dgat y un agonista de ppar |
AR074209A1 (es) | 2008-11-24 | 2010-12-29 | Boehringer Ingelheim Int | Derivados de pirimidina utiles para el tratamiento del cancer |
AR074210A1 (es) * | 2008-11-24 | 2010-12-29 | Boehringer Ingelheim Int | Derivados de pirimidina como inhibidores de ptk2-quinasa |
US8729265B2 (en) | 2009-08-14 | 2014-05-20 | Boehringer Ingelheim International Gmbh | Regioselective preparation of 2-amino-5-trifluoromethylpyrimidine derivatives |
US8933227B2 (en) | 2009-08-14 | 2015-01-13 | Boehringer Ingelheim International Gmbh | Selective synthesis of functionalized pyrimidines |
AU2012250517B2 (en) | 2011-05-04 | 2016-05-19 | Takeda Pharmaceutical Company Limited | Compounds for inhibiting cell proliferation in EGFR-driven cancers |
EP2751110B1 (en) * | 2011-10-14 | 2017-04-19 | MedImmune Limited | Asymmetrical bis-(5H-Pyrrolo[2,1-c][1,4]benzodiazepin-5-one) derivatives for the treatment of proliferative and autoimmune diseases |
US20150166591A1 (en) | 2012-05-05 | 2015-06-18 | Ariad Pharmaceuticals, Inc. | Methods and compositions for raf kinase mediated diseases |
US9611283B1 (en) | 2013-04-10 | 2017-04-04 | Ariad Pharmaceuticals, Inc. | Methods for inhibiting cell proliferation in ALK-driven cancers |
KR102318875B1 (ko) | 2019-03-19 | 2021-11-01 | 보로노이 주식회사 | 헤테로아릴 유도체, 이를 제조하는 방법, 및 이를 유효성분으로 포함하는 약학적 조성물 |
CN112341468A (zh) * | 2020-11-19 | 2021-02-09 | 烟台大学 | 一种1,4-苯并二氮杂*类化合物及其制备与功能化方法 |
WO2023204308A1 (ja) * | 2022-04-22 | 2023-10-26 | 帝人ファーマ株式会社 | オキサゼピン誘導体 |
Family Cites Families (3)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
ES2325440T3 (es) | 2003-02-20 | 2009-09-04 | Smithkline Beecham Corporation | Compuestos de pirimidina. |
GB0305929D0 (en) | 2003-03-14 | 2003-04-23 | Novartis Ag | Organic compounds |
US7521457B2 (en) | 2004-08-20 | 2009-04-21 | Boehringer Ingelheim International Gmbh | Pyrimidines as PLK inhibitors |
-
2007
- 2007-02-16 TW TW096105940A patent/TW200804364A/zh unknown
- 2007-02-16 US US11/675,936 patent/US7569561B2/en active Active
- 2007-02-20 EP EP07704662.1A patent/EP1989198B1/de active Active
- 2007-02-20 CA CA2638095A patent/CA2638095C/en active Active
- 2007-02-20 WO PCT/EP2007/051599 patent/WO2007096351A1/de active Application Filing
- 2007-02-20 JP JP2008555777A patent/JP5306830B2/ja active Active
- 2007-02-21 AR ARP070100726A patent/AR059594A1/es unknown
Also Published As
Publication number | Publication date |
---|---|
WO2007096351A1 (de) | 2007-08-30 |
EP1989198B1 (de) | 2013-10-09 |
JP5306830B2 (ja) | 2013-10-02 |
TW200804364A (en) | 2008-01-16 |
EP1989198A1 (de) | 2008-11-12 |
US20070207999A1 (en) | 2007-09-06 |
US7569561B2 (en) | 2009-08-04 |
CA2638095C (en) | 2014-07-08 |
CA2638095A1 (en) | 2007-08-30 |
JP2009527532A (ja) | 2009-07-30 |
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---|---|---|---|
FB | Suspension of granting procedure |