UY25857A1 - 4-alquenil (y alquinil) oxindoles los cuales inhiben las quinasas dependientes de ciclina (cdks) - Google Patents

4-alquenil (y alquinil) oxindoles los cuales inhiben las quinasas dependientes de ciclina (cdks)

Info

Publication number
UY25857A1
UY25857A1 UY25857A UY25857A UY25857A1 UY 25857 A1 UY25857 A1 UY 25857A1 UY 25857 A UY25857 A UY 25857A UY 25857 A UY25857 A UY 25857A UY 25857 A1 UY25857 A1 UY 25857A1
Authority
UY
Uruguay
Prior art keywords
conr6r7
coor4
pharmaceutically acceptable
oxindoles
cdks
Prior art date
Application number
UY25857A
Other languages
English (en)
Inventor
Steven Gregory Mischke
Paige E Mahaney
Kin-Chun Luk
Jin-Jun Liu
Apostolos Dermatakis
Yi Chen
Wendy Lea Corbett
Original Assignee
Hoffmann La Roche
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 Hoffmann La Roche filed Critical Hoffmann La Roche
Publication of UY25857A1 publication Critical patent/UY25857A1/es

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Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/14Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
    • 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
    • A61K31/40Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
    • A61K31/403Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with carbocyclic rings, e.g. carbazole
    • A61K31/404Indoles, e.g. pindolol
    • 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
    • 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
    • C07D403/02Heterocyclic 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
    • C07D403/06Heterocyclic 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 carbon chain containing only aliphatic carbon atoms
    • 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D405/00Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/14Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D409/00Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/14Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing three or more hetero rings

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)

Abstract

Nuevos 4-alquenil y 4-alquinil oxindoles que presentan la fórmula I (como por ejemplo: (Z)-1,3-dihidro-4-(6-hidroxi-1-hexinil)-3-[(-3metoxi-1H-pirrol-2-il)metileno]-2H-indol-2-ona) y II (como poe ejemplo: (R)-(Z)-1,3-dihidro-4-[(5-etilimino-6-metil)-6H-piran-2-il]-5-fluoro-3-[(3.metoxi-1H-pirrol-2-il)metileno)]-2H-indol-2-ona) y las sales farmacéuticamente aceptables de los mismos en los que R1 es H, COR4, COOR4, CONR6R7, alquilo inferior, etc; R2 se selecciona entre H, OR4, COOR4, CONR6R7, NR6R7, halogeno, NO2, CN, SO2R4, SO2NR6R7, perfluoroalquilo, etc; R3 es H, OR4, COOR4, CONR6R7, perfluoroalquilo, alquilo inferioretc; a es un enlace opcional, b es cicloalquilo, heterociclo, que pueden estar opcionalmente sustituidos y X es =N, =C(R5), o =C(COOOR8) son como se definen aquí. Una composición farmacéutica que contiene como ingrediente activo un compuesto de fórmula l o ll y un vehiculo o excipiente farmacéuticamente aceptable. El uso de dichos compuestos o una sal farmacéuticamente aceptable del mismo para la fabricación de un medicamento, el cual inhiben las quinasas dependientes de ciclina (CDKs), en particular la CDK2, y son útiles como agentes antiproliferativos en el tratamiento o control de trastornos de la proliferación celular, en particular tumores de colon o de mama.
UY25857A 1998-12-17 1999-12-16 4-alquenil (y alquinil) oxindoles los cuales inhiben las quinasas dependientes de ciclina (cdks) UY25857A1 (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US11259198P 1998-12-17 1998-12-17
US14907399P 1999-08-16 1999-08-16

Publications (1)

Publication Number Publication Date
UY25857A1 true UY25857A1 (es) 2001-07-31

Family

ID=26810131

Family Applications (1)

Application Number Title Priority Date Filing Date
UY25857A UY25857A1 (es) 1998-12-17 1999-12-16 4-alquenil (y alquinil) oxindoles los cuales inhiben las quinasas dependientes de ciclina (cdks)

Country Status (20)

Country Link
US (3) US6130239A (es)
EP (1) EP1157019B1 (es)
JP (1) JP2002532492A (es)
KR (1) KR100649925B1 (es)
CN (1) CN1138773C (es)
AR (1) AR024847A1 (es)
AT (1) ATE234830T1 (es)
AU (1) AU770375B2 (es)
BR (1) BR9916327A (es)
CA (1) CA2354873A1 (es)
CO (1) CO5261600A1 (es)
DE (1) DE69906152T2 (es)
DK (1) DK1157019T3 (es)
ES (1) ES2192877T3 (es)
PE (1) PE20001537A1 (es)
PT (1) PT1157019E (es)
TR (1) TR200101860T2 (es)
TW (1) TW550262B (es)
UY (1) UY25857A1 (es)
WO (1) WO2000035908A1 (es)

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ES2192877T3 (es) * 1998-12-17 2003-10-16 Hoffmann La Roche 4-alquenil (y alquinil) oxindoles como inhibidores de kinasas ciclina-dependientes, en particular cdk2.
AU1928501A (en) * 1999-11-24 2001-06-04 Sugen, Inc. Formulations for pharmaceutical agents ionizable as free acids or free bases
US6878733B1 (en) 1999-11-24 2005-04-12 Sugen, Inc. Formulations for pharmaceutical agents ionizable as free acids or free bases
NZ519697A (en) * 1999-12-22 2004-08-27 Sugen Inc Methods of modulating c-kit tyrosine protein kinase function with indolinone compounds
CZ303705B6 (cs) * 2000-02-15 2013-03-27 Sugen, Inc. Pyrrolem substituovaná 2-indolinonová sloucenina pro pouzití jako inhibitor proteinkináz a farmaceutická kompozice s jejím obsahem
WO2001072708A2 (en) * 2000-03-24 2001-10-04 Cor Therapeutics, Inc. OXINDOLE INHIBITORS OF FACTOR Xa
MY128450A (en) 2000-05-24 2007-02-28 Upjohn Co 1-(pyrrolidin-1-ylmethyl)-3-(pyrrol-2-ylmethylidene)-2-indolinone derivatives
WO2001094312A2 (en) 2000-06-02 2001-12-13 Sugen, Inc. Indolinone derivatives as protein kinase/phosphatase inhibitors
AU2001270260A1 (en) * 2000-06-30 2002-01-14 Sugen, Inc. 4-heteroaryl-3-heteroarylidenyl-2-indolinones and their use as protein kinase inhibitors
US6677368B2 (en) * 2000-12-20 2004-01-13 Sugen, Inc. 4-aryl substituted indolinones
US6504034B2 (en) 2001-01-23 2003-01-07 Hoffmann-La Roche Inc. Naphthostyrils
AR042586A1 (es) 2001-02-15 2005-06-29 Sugen Inc 3-(4-amidopirrol-2-ilmetiliden)-2-indolinona como inhibidores de la protein quinasa; sus composiciones farmaceuticas; un metodo para la modulacion de la actividad catalitica de la proteinquinasa; un metodo para tratar o prevenir una afeccion relacionada con la proteinquinasa
FR2822155B1 (fr) * 2001-03-13 2003-12-12 Aventis Pharma Sa Composes derives des oxindoles et leur application therapeutique en cancerologie
CN100439360C (zh) * 2001-08-15 2008-12-03 法玛西雅厄普约翰美国公司 包括n-[2-(二乙氨基)乙基]-5-[(5-氟-2-氧代-3h-吲哚-3-亚基)甲基]-2,4-二甲基-1h-吡咯-3-甲酰胺的苹果酸盐的晶体、其制备方法和其组合物
CA2462950A1 (en) 2001-10-10 2003-04-17 Sugen, Inc. 3-[4-(substituted heterocyclyl)-pyrrol-2-ylmethylidene]-2-indolinone derivatives as kinase inhibitors
WO2003057690A1 (en) * 2001-12-27 2003-07-17 Theravance, Inc. Indolinone derivatives useful as protein kinase inhibitors
FR2948940B1 (fr) * 2009-08-04 2011-07-22 Servier Lab Nouveaux derives dihydroindolones, leur procede de preparation et les compositions pharmaceutiques qui les contiennent
US20140205537A1 (en) * 2011-06-24 2014-07-24 Zenobia Therapeutics, Inc. Lrrk2 inhibitors
CN106187904B (zh) * 2015-05-25 2021-07-06 中国医学科学院药物研究所 含丙炔酰胺基的2-苯基咪唑类衍生物及其制法和药物组合物与用途
KR102616949B1 (ko) 2017-09-14 2023-12-22 다이이찌 산쿄 가부시키가이샤 고리형 구조를 갖는 화합물
AR124154A1 (es) 2020-11-27 2023-02-22 Rhizen Pharmaceuticals Ag Inhibidores de cdk
WO2022149057A1 (en) 2021-01-05 2022-07-14 Rhizen Pharmaceuticals Ag Cdk inhibitors

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Also Published As

Publication number Publication date
TR200101860T2 (tr) 2001-12-21
EP1157019A1 (en) 2001-11-28
BR9916327A (pt) 2001-09-18
AR024847A1 (es) 2002-10-30
CO5261600A1 (es) 2003-03-31
PT1157019E (pt) 2003-06-30
KR100649925B1 (ko) 2007-02-28
AU1972700A (en) 2000-07-03
CA2354873A1 (en) 2000-06-22
PE20001537A1 (es) 2001-01-09
AU770375B2 (en) 2004-02-19
DK1157019T3 (da) 2003-07-14
US6252086B1 (en) 2001-06-26
WO2000035908A1 (en) 2000-06-22
EP1157019B1 (en) 2003-03-19
TW550262B (en) 2003-09-01
DE69906152T2 (de) 2004-02-12
ES2192877T3 (es) 2003-10-16
KR20010101274A (ko) 2001-11-14
US6130239A (en) 2000-10-10
DE69906152D1 (de) 2003-04-24
US6303793B1 (en) 2001-10-16
JP2002532492A (ja) 2002-10-02
CN1138773C (zh) 2004-02-18
CN1330647A (zh) 2002-01-09
ATE234830T1 (de) 2003-04-15

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