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1. WO2002022605 - PYRAZOLE COMPOUNDS USEFUL AS PROTEIN KINASE INHIBITORS

Publication Number WO/2002/022605
Publication Date 21.03.2002
International Application No. PCT/US2001/028793
International Filing Date 14.09.2001
Chapter 2 Demand Filed 15.04.2002
IPC
C07D 401/12 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
401Heterocyclic 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
02containing two hetero rings
12linked by a chain containing hetero atoms as chain links
C07D 401/14 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
401Heterocyclic 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
14containing three or more hetero rings
C07D 403/12 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
403Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/167
02containing two hetero rings
12linked by a chain containing hetero atoms as chain links
C07D 403/14 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
403Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/167
14containing three or more hetero rings
C07D 405/14 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
405Heterocyclic 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
14containing three or more hetero rings
C07D 407/14 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
407Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen atoms as the only ring hetero atoms, not provided for by group C07D405/183
14containing three or more hetero rings
CPC
A61P 1/16
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
1Drugs for disorders of the alimentary tract or the digestive system
16for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
A61P 11/06
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
11Drugs for disorders of the respiratory system
06Antiasthmatics
A61P 17/06
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
17Drugs for dermatological disorders
06Antipsoriatics
A61P 19/00
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
19Drugs for skeletal disorders
A61P 19/02
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
19Drugs for skeletal disorders
02for joint disorders, e.g. arthritis, arthrosis
A61P 19/10
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
19Drugs for skeletal disorders
08for bone diseases, e.g. rachitism, Paget's disease
10for osteoporosis
Applicants
  • VERTEX PHARMACEUTICALS INCORPORATED [US]/[US] (AllExceptUS)
  • GOLEC, Julian, M.C. [GB]/[GB] (UsOnly)
  • CHARRIER, Jean-Damien [FR]/[GB] (UsOnly)
  • KNEGTEL, Ronald [GB]/[GB] (UsOnly)
  • BEBBINGTON, David [GB]/[GB] (UsOnly)
  • DAVIES, Robert [GB]/[US] (UsOnly)
  • LI, Pan [CN]/[US] (UsOnly)
Inventors
  • GOLEC, Julian, M.C.
  • CHARRIER, Jean-Damien
  • KNEGTEL, Ronald
  • BEBBINGTON, David
  • DAVIES, Robert
  • LI, Pan
Agents
  • GOVINDASWAMY, Nandakumar
Priority Data
60/232,79515.09.2000US
60/257,88721.12.2000US
60/286,94927.04.2001US
Publication Language English (EN)
Filing Language English (EN)
Designated States
Title
(EN) PYRAZOLE COMPOUNDS USEFUL AS PROTEIN KINASE INHIBITORS
(FR) COMPOSES DE PYRAZOLE UTILES COMME INHIBITEURS DE PROTEINE KINASE
Abstract
(EN)
This invention describes novel pyrazole compositions comprising a pharmaceutically acceptable carrier and a compound of formula VIII, wherein Z1 is N or C-R9, Z2 is N or CH, and Z3 is N or C-Rx, provided that one of Z1 and Z3 is nitrogen; G is Ring C or Ring D; Ring C is selected from a phenyl, pyridinyl, pyrimidinyl, pyridazinyl, pyrazinyl, or 1,2,4-triazinyl ring, wherein said Ring C has one or two ortho substitutents independently selected from -R1; Ring D is a 5-7 membered monocyclic ring or 8-10 membered bicyclic ring selected from aryl, heteroaryl, heterocyclyl or carbocyclyl; and Rx, R1, R2, R2', R3 and R9 are as described inthe specification. The compounds are useful as protein kinase inhibitors, especially as inhibitors of aurora-2 and GSK-3, for treating diseases such as cancer, diabetes and Alzheimer's disease.
(FR)
L'invention concerne de nouvelles compositions de pyrazole qui contiennent un excipient pharmaceutiquement acceptable et un composé représenté par la formule VIII, dans laquelle Z1 représente N ou C-R9, Z2 représente N ou CH, et Z3 représente N ou C-Rx, à condition que Z1 ou Z3 représente azote ; G représente le noyau C ou le noyau D ; le noyau C est sélectionné dans le groupe comprenant un noyau phényle, pyridinyle, pyrimidinyle, pyridazinyle, pyrazinyle, ou 1,2,4-triazinyle, ce noyau C comportant un ou deux substituants en ortho sélectionnés indépendamment dans le groupe comprenant -R1; le noyau D est un noyau monocyclique doté de 5 à 7 chaînons ou un noyau bicyclique doté de 8 à 10 chaînons, sélectionné dans le groupe comprenant aryle, hétéroaryle, hétérocyclyle ou carbocyclyle ; et Rx, R1, R2, R2', R3 et R9 sont tels que décrits dans la spécification. Ces composés sont utiles comme inhibiteurs de protéine kinase, notamment comme inhibiteurs d'aurora-2 et de GSK-3, pour traiter des maladies telles que le cancer, le diabète et la maladie d'Alzheimer.
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