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1. (NZ598924) COMPOUNDS AND COMPOSITIONS AS PROTEIN KINASE INHIBITORS

Office : New Zealand
Application Number: 598924 Application Date: 27.08.2010
Publication Number: 598924 Publication Date: 26.07.2013
Grant Number: Grant Date: 30.10.2013
Publication Kind : B
Prior PCT appl.: Application Number:PCTUS2010046930 ; Publication Number: Click to see the data
IPC:
C07D 401/14
A61K 31/506
A61P 35/00
C07D 403/04
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
401
Heterocyclic 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
14
containing three or more hetero rings
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
K
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31
Medicinal preparations containing organic active ingredients
33
Heterocyclic compounds
395
having nitrogen as a ring hetero atom, e.g. guanethidine, rifamycins
495
having six-membered rings with two nitrogen atoms as the only ring hetero atoms, e.g. piperazine
505
Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
506
not condensed and containing further heterocyclic rings
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
P
SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
35
Antineoplastic agents
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
403
Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/167
02
containing two hetero rings
04
directly linked by a ring-member-to-ring- member bond
Applicants: Novartis AG
IRM LLC
Inventors: HUANG, Shenlin
JIN, Xianming
LIU, Zuosheng
POON, Daniel
TELLEW, John E.
WAN, Yongqin
WANG, Xing
XIE, Yongping
Agents: BALDWINS INTELLECTUAL PROPERTY
Priority Data: 61/238,073 28.08.2009 US
61/313,039 11.03.2010 US
Title: (EN) COMPOUNDS AND COMPOSITIONS AS PROTEIN KINASE INHIBITORS
Abstract:
(EN) Patent 598924 Disclosed are compounds of Formula (Ia), salts thereof and methods for their preparation. Specific examples of compounds of Formula (Ia) include: methyl N-[(2S)-1-({4-[3-(3-chloro-5-methanesulfonamidophenyl)-1-(propan-2-yl)-1H-pyrazol-4-yl]pyrimidin-2-yl}amino)propan-2-yl] carbamate, methyl N-[(2S)-1-{[4-(3-{2-fluoro-3-[(3,3,3-trifluoropropane)sulfonamido]phenyl}-1-(propan-2-yl)-1H-pyrazol-4-yl)pyrimidin-2-yl]amino}propan-2-yl] carbamate, N-[5-chloro-3-(4-{2-[(2-cyanoethyl)amino]pyrimidin-4-yl}-1-(propan-2-yl)-1H-pyrazol-3-yl)-2-fluorophenyl]methanesulfonamide, and methyl N-[(2S)-I-( {4-[3-(S-chloro-2-fluoro-3-methanesulfonamidophenyl)-1-(propan-2-yl)-1H-pyrazol-4-yl]pyrimidin-2-yl}amino)propan-2-yl]carbamate. Compounds of formula Ia are useful for treating diseases or disorders associated with abnormal or deregulated kinase activity, particularly diseases of disorders that inveolve abnormal activation of B-Raf. Examples of diseases include lung carcinoma, pancreatic carcinoma, bladder carcinoma, colon carcinoma, and myeloid disorders, prostate cancer, thyroid cancer, melanoma, adenomas and carcinomas of the ovary, eye, liver, biliary tract, and nervous system...
Also published as:
RSP-2014/0430UAa201203042SG178351IL218084EP2470526DOP2012000051
JP2013503186CN102725283CA2771775EA201200373EP2727918ES2492499
KR1020120062839TN2012000081DK2470526AU2010286569VN30470ID2012/03594
TH140028IN2469/DELNP/2012WO/2011/025927