AR072792A1 - DERIVADOS DE PIRROLOPIRIDINILPIRIMIDIN-2-IL-AMINA, PROCEDIMIENTO DE PREPARACIoN Y COMPOSICIONES FARMACEUTICAS - Google Patents

DERIVADOS DE PIRROLOPIRIDINILPIRIMIDIN-2-IL-AMINA, PROCEDIMIENTO DE PREPARACIoN Y COMPOSICIONES FARMACEUTICAS

Info

Publication number
AR072792A1
AR072792A1 ARP090102492A ARP090102492A AR072792A1 AR 072792 A1 AR072792 A1 AR 072792A1 AR P090102492 A ARP090102492 A AR P090102492A AR P090102492 A ARP090102492 A AR P090102492A AR 072792 A1 AR072792 A1 AR 072792A1
Authority
AR
Argentina
Prior art keywords
atoms
het
hal
cycloalkyl
mono
Prior art date
Application number
ARP090102492A
Other languages
English (en)
Inventor
Dirk Finsinger
Ulrich Graedler
Margarita Wuchrer
David Bruge
Dieter Dorsch
Christina Esdar
Original Assignee
Merck Patent Gmbh
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Merck Patent Gmbh filed Critical Merck Patent Gmbh
Publication of AR072792A1 publication Critical patent/AR072792A1/es

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Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D471/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04Ortho-condensed systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/4353Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/437Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12Antivirals
    • A61P31/14Antivirals for RNA viruses
    • A61P31/18Antivirals for RNA viruses for HIV
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • A61P35/02Antineoplastic agents specific for leukemia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • A61P35/04Antineoplastic agents specific for metastasis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/14Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing three or more hetero rings

Landscapes

  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Oncology (AREA)
  • Virology (AREA)
  • Engineering & Computer Science (AREA)
  • Molecular Biology (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • AIDS & HIV (AREA)
  • Communicable Diseases (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Hematology (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Plural Heterocyclic Compounds (AREA)

Abstract

Los compuestos de la formula (1) en donde R1 es H o A, R2 es A, Hal, CN, (CH2)nCONH(CH2)pAr, -C(OH)R5-Ar, -[C(R5)2]n-Ar, [C(R5)2]n-Het, -[C(R5)2]n-cicloalquilo, -NR5A, -NR5Ar, NR5Het, -[C(R5)2]mN(R5)2, 1-hidroxi-ciclopentan-1-ilo o 1-hidroxiciclohexan-1-ilo, R3 es H, R5, -[C(R5)2]n-Ar, -[C(R5)2]n-Het, -[C(R5)2]n-cicloalquilo, R4 es H, Het-, Ar-, -R5, -OR5, -[C(R6)2]nC(O)N(R6)2, CO-Het u O(CH2)pHet1, R5 es H, A o cicloalquilo, R6 es H o A', A' es alquilo no ramificado o ramificado con 1-10 átomos de C, en donde 1-7 átomos de H pueden estar reemplazados por F, cicloalquilo es alquilo cíclico con 3-7 átomos de C, que puede estar adicionalmente sustituido con alquilo con 1-6 átomos de C, A es alquilo no ramificado o ramificado con 1-10 átomos de C, en donde uno o dos grupos CH y/o CH2 pueden estar reemplazados por átomos de N, O, S y/o por grupos -CH=CH y/o también 1-7 átomos de H pueden estar reemplazados por F, X es NH, O, S o SO2, Ar es fenilo no sustituido o mono-, di- o trisustituido con Hal, A, OR5, N(R5)2, NO2, CN, COOR5, CON(R5)2, NR5COA, NR5SO2A, COR5, SO2N(R5)2 y/o S(O)pA, Het es un heterociclo saturado, insaturado o aromático mono- o bicíclico no sustituido o mono- o disustituido con Hal, A, OR5, (CH2)pN(R5)2, NO2, CN, (CH2)pCOOR5, (CH2)pCON(R5)2, NR5COA, (CH2)pHet1, (CH2)pCOHet1, NR5SO2A, COR5, SO2NR5 y/o S(O)pA con 1a 4 átomos de N y/u O y/o S, Het1 es un heterociclo saturado no sustituido o mono- o disustituido con A, S(O)pA y/o COA con 1 a 4 átomos de N, O y o S, Hal es F, Cl, Br o I, m es 1, 2, 3, o 4, n es 0, 1, 2, 3, o 4, p es 0, 1 o 2, así como sus sales, tautomeros y estereoisomeros farmacéuticamente aceptables, incluyendo sus mezclas en todas las proporciones. Son inhibidores de la proliferacion celular / vitalidad celular y se pueden emplear para el tratamiento de tumores.
ARP090102492A 2008-07-03 2009-07-03 DERIVADOS DE PIRROLOPIRIDINILPIRIMIDIN-2-IL-AMINA, PROCEDIMIENTO DE PREPARACIoN Y COMPOSICIONES FARMACEUTICAS AR072792A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
DE102008031517A DE102008031517A1 (de) 2008-07-03 2008-07-03 Pyrrolopyridinyl-pyrimidin-2-yl-amin-derivate

Publications (1)

Publication Number Publication Date
AR072792A1 true AR072792A1 (es) 2010-09-22

Family

ID=40849173

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP090102492A AR072792A1 (es) 2008-07-03 2009-07-03 DERIVADOS DE PIRROLOPIRIDINILPIRIMIDIN-2-IL-AMINA, PROCEDIMIENTO DE PREPARACIoN Y COMPOSICIONES FARMACEUTICAS

Country Status (16)

Country Link
US (1) US8420820B2 (es)
EP (1) EP2291375B1 (es)
JP (2) JP5587874B2 (es)
KR (1) KR20110027835A (es)
CN (1) CN102056926B (es)
AR (1) AR072792A1 (es)
AU (1) AU2009266090B2 (es)
BR (1) BRPI0913832A2 (es)
CA (1) CA2729725C (es)
DE (1) DE102008031517A1 (es)
EA (1) EA201100125A1 (es)
ES (1) ES2564204T3 (es)
IL (1) IL210406A (es)
MX (1) MX2010013919A (es)
WO (1) WO2010000364A1 (es)
ZA (1) ZA201100876B (es)

Families Citing this family (21)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE102008031517A1 (de) * 2008-07-03 2010-01-07 Merck Patent Gmbh Pyrrolopyridinyl-pyrimidin-2-yl-amin-derivate
DE102009060174A1 (de) * 2009-12-23 2011-06-30 Merck Patent GmbH, 64293 Pyrrolopyridinyl-pyrimidin-2-yl-amin-derivate
DK2558446T5 (da) 2010-04-16 2019-12-09 Ac Immune Sa Nye forbindelser til behandling af sygdomme associerede med amyloid- eller amyloidlignende proteiner
CN102985422A (zh) * 2010-05-12 2013-03-20 Abbvie公司 激酶的吡咯并吡啶和吡咯并嘧啶抑制剂
DE102010050558A1 (de) 2010-11-05 2012-05-10 Merck Patent Gmbh 1H-Pyrrolo[2,3-b]pyridinderivate
DE102010053347A1 (de) * 2010-12-03 2012-06-06 Merck Patent Gmbh 3-Hetaryl-substituierte Pyrrolo[2,3-b] pyridin-derivative als PDK1-Inhibitoren
DE102011009961A1 (de) * 2011-02-01 2012-08-02 Merck Patent Gmbh 7-Azaindolderivate
DE102011105469A1 (de) * 2011-06-24 2012-12-27 Merck Patent Gmbh 7-Azaindolderivate
AP3902A (en) 2012-06-29 2016-11-17 Pfizer Novel 4-(substituted-amino)-7H-pyrrolo[2,3-d]pyrimidines as LRRK2 inhibitors
MX2015012456A (es) * 2013-03-15 2016-02-03 Plexxikon Inc Compuestos heterociclicos y usos de los mismos.
US20140303121A1 (en) 2013-03-15 2014-10-09 Plexxikon Inc. Heterocyclic compounds and uses thereof
JP6487921B2 (ja) 2013-12-17 2019-03-20 ファイザー・インク LRRK2阻害薬としての新規の3,4−二置換−1H−ピロロ[2,3−b]ピリジンおよび4,5−二置換−7H−ピロロ[2,3−c]ピリダジン
MX2017009571A (es) * 2015-01-23 2018-09-27 Aclaris Therapeutics Inc Inhibidores heterociclicos de itk para el tratamiento de la inflamacion y cancer.
CN106432246B (zh) * 2015-08-05 2020-07-07 广东东阳光药业有限公司 杂芳化合物及其在药物中的应用
MX2018003215A (es) 2015-09-14 2018-06-08 Pfizer Derivados de imidazo[4,5-c]quinolina e imidazo[4,5-c][1,5]naftirid ina novedosos como inhibidores de lrrk2.
GB201704965D0 (en) 2017-03-28 2017-05-10 Astex Therapeutics Ltd Pharmaceutical compounds
EP3694855A1 (en) 2017-10-13 2020-08-19 Plexxikon Inc. Solid forms of a compound for modulating kinases
EP3706086A4 (en) 2017-10-31 2021-07-21 Alise Devices, S.L. PROCESS FOR MANUFACTURING PERSONALIZED DOCUMENTARY SECURITY OPTICAL ELEMENTS AND ELEMENT THUS OBTAINED
JP7018333B2 (ja) 2018-03-08 2022-02-10 大林道路株式会社 複装式カッター
IL278142B2 (en) 2018-04-24 2023-11-01 Merck Patent Gmbh Antiproliferative compounds and their uses
SG11202104404XA (en) * 2018-11-16 2021-05-28 California Inst Of Techn Erk inhibitors and uses thereof

Family Cites Families (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5747469A (en) 1991-03-06 1998-05-05 Board Of Regents, The University Of Texas System Methods and compositions comprising DNA damaging agents and p53
GB9904387D0 (en) 1999-02-25 1999-04-21 Pharmacia & Upjohn Spa Antitumour synergistic composition
GB0308466D0 (en) 2003-04-11 2003-05-21 Novartis Ag Organic compounds
RU2403252C2 (ru) 2004-03-30 2010-11-10 Вертекс Фармасьютикалз Инкорпорейтед Азаиндолы, полезные в качестве ингибиторов jak и других протеинкиназ
CA2608333A1 (en) * 2005-05-16 2006-11-23 Irm Llc Pyrrolopyridine derivatives as protein kinase inhibitors
DE102006012617A1 (de) * 2006-03-20 2007-09-27 Merck Patent Gmbh 4-(Pyrrolopyridinyl)-pyrimidinyl-2-amin-derivate
DE102007028515A1 (de) * 2007-06-21 2008-12-24 Merck Patent Gmbh 6-(Pyrrolopyridinyl)-pyrimidinyl-2-amin-derivate
DE102008031517A1 (de) * 2008-07-03 2010-01-07 Merck Patent Gmbh Pyrrolopyridinyl-pyrimidin-2-yl-amin-derivate

Also Published As

Publication number Publication date
DE102008031517A1 (de) 2010-01-07
IL210406A0 (en) 2011-03-31
IL210406A (en) 2014-11-30
EP2291375B1 (de) 2016-01-06
KR20110027835A (ko) 2011-03-16
CN102056926B (zh) 2013-10-16
EP2291375A1 (de) 2011-03-09
CA2729725A1 (en) 2010-01-07
CN102056926A (zh) 2011-05-11
US20110218198A1 (en) 2011-09-08
JP5587874B2 (ja) 2014-09-10
CA2729725C (en) 2016-11-08
BRPI0913832A2 (pt) 2015-10-20
WO2010000364A8 (de) 2011-01-06
AU2009266090B2 (en) 2014-04-03
US8420820B2 (en) 2013-04-16
ES2564204T3 (es) 2016-03-18
ZA201100876B (en) 2011-10-26
EA201100125A1 (ru) 2011-08-30
JP2014240397A (ja) 2014-12-25
JP2011526260A (ja) 2011-10-06
JP5955902B2 (ja) 2016-07-20
AU2009266090A1 (en) 2010-01-07
WO2010000364A1 (de) 2010-01-07
MX2010013919A (es) 2011-02-21

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