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1. NZ514523 - Pyrazolobenzodiazepines as CDK2 inhibitors

Office New Zealand
Application Number 514523
Application Date 28.09.2001
Publication Number 514523
Publication Date 28.11.2003
Grant Number 514523
Grant Date 09.03.2004
Publication Kind B
IPC
C07D 487/04
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
487Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/-C07D477/183
02in which the condensed system contains two hetero rings
04Ortho-condensed systems
C07D 243/22
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
243Heterocyclic compounds containing seven-membered rings having two nitrogen atoms as the only ring hetero atoms
06having the nitrogen atoms in positions 1 and 4
10condensed with carbocyclic rings or ring systems
141,4-Benzodiazepines; Hydrogenated 1,4-benzodiazepines
16substituted in position 5 by aryl radicals
18substituted in position 2 by nitrogen, oxygen or sulfur atoms
22Sulfur atoms
A61P 35/00
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
35Antineoplastic agents
A61K 31/5517
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31Medicinal preparations containing organic active ingredients
33Heterocyclic compounds
395having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
55having seven-membered rings, e.g. azelastine, pentylenetetrazole
551having two nitrogens as ring hetero atoms, e.g. clozapine, dilazep
55131,4-Benzodiazepines, e.g. diazepam
5517condensed with five-membered rings having nitrogen as a ring hetero atom, e.g. imidazobenzodiazepines, triazolam
C07D 417/06
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
417Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/196
02containing two hetero rings
06linked by a carbon chain containing only aliphatic carbon atoms
C07D 403/06
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
06linked by a carbon chain containing only aliphatic carbon atoms
CPC
A61P 1/00
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
A61P 11/00
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
11Drugs for disorders of the respiratory system
A61P 13/08
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
13Drugs for disorders of the urinary system
08of the prostate
A61P 35/00
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
35Antineoplastic agents
A61P 35/04
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
35Antineoplastic agents
04specific for metastasis
C07D 243/22
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
243Heterocyclic compounds containing seven-membered rings having two nitrogen atoms as the only ring hetero atoms
06having the nitrogen atoms in positions 1,4
10condensed with carbocyclic rings or ring systems
141,4-Benzodiazepines; Hydrogenated 1,4-benzodiazepines
16substituted in position 5 by aryl radicals
18substituted in position 2 by nitrogen, oxygen or sulfur atoms
22Sulfur atoms
Applicants F. HOFFMANN-LA ROCHE AG
Inventors Liu, Jin-Jun
Ding, Qingjie
Madison, Vincent Stewart
Pizzolato, Giacomo
Wei, Chung-Chen
Wovkulich, Peter Michael
Agents AJ PARK
Priority Data 99 130370 21.04.1999 US
Title
(EN) Pyrazolobenzodiazepines as CDK2 inhibitors
Abstract
(EN)
Patent 514523 Described is the compound of formula I wherein: R1 is hydrogen, -NO2, -CN, -halogen, -OR5, -R6OR7, -COOR7, -CONR8R9, -NR10R11, -NHCOR12, -NHSO2R13, or straight-chained lower alkyl which optionally is substituted by hydroxy and/or halogen; R2 and R4 are each independently hydrogen, -halogen, -NO2, -CF3, or straight chained lower alkyl; R3 is hydrogen, -cycloalkyl, -aryl, -heterocycle, -heteroaryl, -COOR7-CN, -alkenyl,-CONR8R9, -alkynyl, or lower alkyl which optionally is substituted by hydroxy, -OR9, F, and/or aryl; R5 is lower alkyl which optionally is substituted by halogen; R6 is lower alkyl; R7 is hydrogen or lower alkyl; R8 and R9 are each independently hydrogen or lower alkyl which itself optionally are substituted by hydroxy and/or -NH2; alternatively, R8 and R9 may form a 5-or 6-membered heterocycle which optionally is substituted by hydroxy, -NH2, and/or lower alkyl; R10, R11 and R12 are each independently hydrogen or lower alkyl; R13 is lower alkyl which optionally is substituted by halogen and/or -NR14R15; and R14 and R15 are each independently hydrogen or lower alkyl which optionally are substituted halogen, or alternatively,-NR14R15 is a heterocycle; and the pharmaceutically acceptable salts of compounds of formula I. Also described are the compounds of 3 and 5 wherein R1 to R4 are as defined above. The compounds may used as the active ingredient of pharmaceutical compositions for the treatment of breast, colon, lung and prostate tumors.