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1. (WO2007134827) 5-PHENYL-THIAZ0L-2-YL-UREA DERIVATIVES AND USE AS PI3 KINASE INHIBITORS
Latest bibliographic data on file with the International Bureau

Pub. No.: WO/2007/134827 International Application No.: PCT/EP2007/004500
Publication Date: 29.11.2007 International Filing Date: 21.05.2007
IPC:
C07D 277/48 (2006.01) ,C07D 417/12 (2006.01) ,A61K 31/427 (2006.01) ,A61P 11/00 (2006.01)
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
277
Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings
02
not condensed with other rings
20
having two or three double bonds between ring members or between ring members and non-ring members
32
with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
38
Nitrogen atoms
44
Acylated amino or imino radicals
48
by radicals derived from carbonic acid, or sulfur or nitrogen analogues thereof, e.g. carbonylguanidines
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
417
Heterocyclic 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
02
containing two hetero rings
12
linked by a chain containing hetero atoms as chain links
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
41
having five-membered rings with two or more ring hetero atoms, at least one of which is nitrogen, e.g. tetrazole
425
Thiazoles
427
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
11
Drugs for disorders of the respiratory system
Applicants:
NOVARTIS AG [CH/CH]; Lichtstrasse 35 CH-4002 Basel, CH (AllExceptUS)
BUDD, Emma [GB/GB]; GB (UsOnly)
HAYLER, Judy, Fox [GB/GB]; GB (UsOnly)
BRUCE, Ian [GB/GB]; GB (UsOnly)
LEGRAND, Darren Mark [GB/GB]; GB (UsOnly)
COX, Brian [GB/GB]; GB (UsOnly)
Inventors:
BUDD, Emma; GB
HAYLER, Judy, Fox; GB
BRUCE, Ian; GB
LEGRAND, Darren Mark; GB
COX, Brian; GB
Agent:
ROTH, Peter R.; Novartis AG Corporate Intellectual Property CH-4002 Basel, CH
Priority Data:
0610243.823.05.2006GB
Title (EN) 5-PHENYL-THIAZ0L-2-YL-UREA DERIVATIVES AND USE AS PI3 KINASE INHIBITORS
(FR) DÉRIVÉS D'URÉE 5-PHÉNYL-THIAZ0L-2-YL ET LEUR UTILISATION EN TANT QU'INHIBITEURS DE LA KINASE PI3
Abstract:
(EN) The present invention concerns a compound of formula Ia wherein: Ra * is hydrogen or C1-C4-alkyl; Rb* is -(C1-C4-alkylene)-Y-C1-C4-haloalkyl or -(C1-C4-alkylene)-Y-C1-C4-hydroxyalkyl; Y represents -CONH- or a five membered heteroaryl group. R2* is C1-C4-alkyl or halogen; R3* is halo, -SO2-CH3, -SO2-CF3, carboxy, -CO-NH2, -CO-di(C1-C8-alkyl)amino, or a 5- or 6- membered heterocyclic ring having one or more ring hetero atoms selected from the group consisting of oxygen, nitrogen and sulphur, that ring being optionally substituted by halo, cyano, oxo, hydroxy, carboxy, nitro, C3-C8-cycloalkyl, C1-C8-alkylcarbonyl, C1-C8-alkoxy optionally substituted by aminocarbonyl, or C1-C8-alkyl optionally substituted by hydroxy, C1- C8-alkoxy, C1- C8-alkylamino or di(C1- C8-alkyl)amino; R4* is hydrogen, halo, -SO2-CH3, nitrile, C1- C8-haloalkyl, imidazolyl, C1- C8-alkyl, -NR8*R9*, or -SO2-NR8*R9*; and R5* is hydrogen, halogen or C1- C8-alkyl; R8* and R9* are independently hydrogen, amino, C1- C8-alkylamino, di(C1- C8-alkyl)amino, or CC1- C8-alkyl optionally substituted by hydroxyl; or a pharmaceutically acceptable salt, or solvate thereof, to compositions and use of the compounds in the treatment of diseases ameloriated by inhibition of phosphatidylinositol 3-kinase.
(FR) La présente invention concerne une composition de formule Ia dans laquelle : Ra * est de l'hydrogène ou de l'alkyle C1-C4; Rb* représente -(C1-C4-alkylène)-Y-C1-C4-haloalkyle ou -(C1-C4-alkylène)-Y-C1-C4-hydroxyalkyle; Y représente -CONH- ou un groupe d'hétéroaryle à cinq chaînons. R2* représente alkyle C1-C4-ou halogène, R3* représente halo, -SO2-CH3, -SO2-CF3, carboxy, -CO-NH2, -CO-di(C1-C8-alkyl)amino, ou un anneau hétérocyclique à 5 ou 6 chaînons possédant un ou plusieurs hétéroatomes cycliques sélectionnés dans un groupe comprenant oxygène, azote et soufre, cet anneau étant éventuellement substitué par halo, cyano, oxo, hydroxy, carboxy, nitro, C3-C8-cycloalkyle, C1-C8-alkylcarbonyle, C1-C8-alkoxy substitué facultativement par aminocarbonyle, ou C1-C8-alkyle facultativement substitué par hydroxy, C1- C8-alkoxy, C1- C8-alkylamino ou di(C1- C8-alkyl)amino; R4* représente hydrogène, halo, -SO2-CH3, nitrile, C1- C8-haloalkyle, imidazolyle, C1- C8-alkyle, -NR8*R9*, ou -SO2-NR8*R9*; et R5*représente hydrogène, halogène ou C1- C8-alkyle; R8* et R9* représentent indépendamment hydrogène, amino, C1- C8-alkylamino, di(C1- C8-alkyl)amino, ou CC1- C8-alkyle éventuellement substitués par hydroxyle, ou un sel pharmaceutiquement acceptable, ou un solvate dérivé, pour des compositions et l'utilisation de compositions dans le traitement de maladies amélioré par l'inhibition de la 3-kinase inositol phosphatidyle.
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Designated States: AE, AG, AL, AM, AT, AU, AZ, BA, BB, BG, BH, BR, BW, BY, BZ, CA, CH, CN, CO, CR, CU, CZ, DE, DK, DM, DZ, EC, EE, EG, ES, FI, GB, GD, GE, GH, GM, GT, HN, HR, HU, ID, IL, IN, IS, JP, KE, KG, KM, KN, KP, KR, KZ, LA, LC, LK, LR, LS, LT, LU, LY, MA, MD, ME, MG, MK, MN, MW, MX, MY, MZ, NA, NG, NI, NO, NZ, OM, PG, PH, PL, PT, RO, RS, RU, SC, SD, SE, SG, SK, SL, SM, SV, SY, TJ, TM, TN, TR, TT, TZ, UA, UG, US, UZ, VC, VN, ZA, ZM, ZW
African Regional Intellectual Property Organization (ARIPO) (BW, GH, GM, KE, LS, MW, MZ, NA, SD, SL, SZ, TZ, UG, ZM, ZW)
Eurasian Patent Organization (AM, AZ, BY, KG, KZ, MD, RU, TJ, TM)
European Patent Office (AT, BE, BG, CH, CY, CZ, DE, DK, EE, ES, FI, FR, GB, GR, HU, IE, IS, IT, LT, LU, LV, MC, MT, NL, PL, PT, RO, SE, SI, SK, TR)
African Intellectual Property Organization (BF, BJ, CF, CG, CI, CM, GA, GN, GQ, GW, ML, MR, NE, SN, TD, TG)
Publication Language: English (EN)
Filing Language: English (EN)
Also published as:
MXMX/a/2008/014864KR1020080110931EP2029562JP2009537579US20090234132CN101448801
CA2650655AU2007253614IN9439/DELNP/2008