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1. (WO2009133135) SPIRO (PIPERIDINE-4, 2 ' -PYRROLIDINE) -1- (3, 5- TRIFLUOROMETHYL PHENYL) METHYLCARBOXAMIDES AS NK1 TACHIKYNIN RECEPTOR ANTAGONISTS
Latest bibliographic data on file with the International Bureau   

Pub. No.:    WO/2009/133135    International Application No.:    PCT/EP2009/055190
Publication Date: 05.11.2009 International Filing Date: 29.04.2009
IPC:
C07D 471/10 (2006.01), C07D 498/20 (2006.01), A61P 25/22 (2006.01), A61P 25/24 (2006.01), A61P 29/00 (2006.01)
Applicants: GLAXO WELLCOME MANUFACTURING PTE LTD [SG/SG]; 1 Pioneer Sector 1 Jurong 628413 (SG) (For All Designated States Except US).
ALVARO, Giuseppe [IT/IT]; (IT) (For US Only).
CASTIGLIONI, Emiliano [IT/IT]; (IT) (For US Only).
MARASCO, Agostino [IT/IT]; (IT) (For US Only)
Inventors: ALVARO, Giuseppe; (IT).
CASTIGLIONI, Emiliano; (IT).
MARASCO, Agostino; (IT)
Agent: PEZZOLI, Anna; (GB)
Priority Data:
0808030.1 01.05.2008 GB
Title (EN) SPIRO (PIPERIDINE-4, 2 ' -PYRROLIDINE) -1- (3, 5- TRIFLUOROMETHYL PHENYL) METHYLCARBOXAMIDES AS NK1 TACHIKYNIN RECEPTOR ANTAGONISTS
(FR) SPIRO (PIPÉRIDINE-4, 2 ' -PYRROLIDINE) -1- (3, 5- TRI FLUOROMÉTHYL PHÉNYLE) MÉTHYLCARBOXAMIDES EN TANT QU’ANTAGONISTES DU RÉCEPTEUR NKL TACHIKYNINE.
Abstract: front page image
(EN)Compounds of formula (I) or a pharmaceutically acceptable salt thereof wherein R is hydrogen or C 1-4 alkyl; R1 is hydrogen, C 1-4 alkyl, C(O)OH, C(O)NH2 or (C 1-4 alkylene)R10; R2 and R3 are independently hydrogen, C 1-4 alkyl or R2 together with R3 and together with the carbon atom to which they are attached form a C3-8 cycloalkyl group; R4 is C 1-4 alkyl, C 1-4 alkoxy or halogen; R5 and R7 are independently hydrogen, hydroxy, halogen, C(O)NH2, C(O)OH or (C 1-4 alkylene) R10; R6 and R8 are independently hydrogen or halogen; R9 is hydrogen, (C 1-4 alkylene)R10, C(O)NH2, C(O)OH or R9 together with R form a 6 membered heterocyclic ring optionally containing a further heteroatom selected from oxygen, sulphur or nitrogen; R10 is hydrogen, halogen, hydroxy, C(O)NH2, C(O)NH(C 1-4 alkyl), C(O)N(C 1-4 alkyl)2 or C(O)OH; n is O, 1 or 2. processes for their preparation, to compositions containing them and to their use in the treatment of diseases and conditions for which antagonism of NK1 is beneficial.
(FR)L’invention concerne des composés de formule (I) ou un sel pharmaceutiquement acceptable de ceux-ci, où R est hydrogène ou C 1-4 alkyle ; R1 est hydrogène, C1-4 alkyle, C(O)OH, C(O)NH2 ou (C 1-4 alkylène)R10 ; R2 et R3 sont indépendamment hydrogène, C1-4 alkyle ou R2 avec R3 et avec l’atome de carbone auquel ils sont attachés constituent un groupe cycloalkyle C3-8 ; R4 est C 1-4 alkyle, C1-4 alcoxy ou halogène ; R5 et R7 sont indépendamment hydrogène, hydroxy, halogène, C(O)NH2, C(O)OH ou (C1-4 allylène) R10 ; R6 et R8 sont indépendamment hydrogène ou halogène ; R9 est hydrogène, (C1-4 alkylène)R10, C(O)NH2, C(O)OH ou R9 avec R constituent un cycle hétérocyclique à 6 éléments contenant éventuellement un hétéroatome supplémentaire sélectionné parmi oxygène, sulfure ou azote ; R10 est hydrogène, halogène, hydroxy, C(O)NH2, C(O)NH(C1-4 alkyl), C(O)N(C1-4 alkyl)2 ou C(O)OH ; n est O, 1 ou 2. L’invention concerne en outre des processus pour leur préparation, des compositions les contenant et leur utilisation dans le traitement de maladies et d’affections pour lesquelles l’antagonisme de NK1 est avantageux.
Designated States: AE, AG, AL, AM, AO, AT, AU, AZ, BA, BB, BG, BH, BR, BW, BY, BZ, CA, CH, CN, CO, CR, CU, CZ, DE, DK, DM, DO, 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, ST, SV, SY, TJ, TM, TN, TR, TT, TZ, UA, UG, US, UZ, VC, VN, ZA, ZM, ZW.
African Regional Intellectual Property Organization (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, HR, HU, IE, IS, IT, LT, LU, LV, MC, MK, MT, NL, NO, 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)