WIPO logo
Mobile | Deutsch | Español | Français | 日本語 | 한국어 | Português | Русский | 中文 | العربية |
PATENTSCOPE

Search International and National Patent Collections
World Intellectual Property Organization
Search
 
Browse
 
Translate
 
Options
 
News
 
Login
 
Help
 
Machine translation
1. (WO2010146395) PYRAZINE CARBOXAMIDES AS INHIBITORS OF DGAT1
Latest bibliographic data on file with the International Bureau   

Pub. No.:    WO/2010/146395    International Application No.:    PCT/GB2010/051003
Publication Date: 23.12.2010 International Filing Date: 17.06.2010
IPC:
C07D 241/24 (2006.01), C07D 401/12 (2006.01), C07D 413/10 (2006.01), A61K 31/4965 (2006.01), A61K 31/497 (2006.01), A61P 3/10 (2006.01)
Applicants: ASTRAZENECA AB [SE/SE]; SE-151 85 Södertälje (SE) (AE, AG, AL, AM, AO, AT, AU, AZ, BA, BB, BE, BF, BG, BH, BJ, BR, BW, BY, BZ, CA, CF, CG, CH, CI, CL, CM, CN, CO, CR, CU, CY, CZ, DE, DK, DM, DO, DZ, EC, EE, EG, ES, FI, FR, GA, GB, GD, GE, GH, GM, GN, GQ, GR, GT, GW, HN, HR, HU, ID, IE, IL, IN, IS, IT, JP, KE, KG, KM, KN, KP, KR, KZ, LA, LC, LK, LR, LS, LT, LU, LV, LY, MA, MC, MD, ME, MK, ML, MN, MR, MT, MW, MX, MY, MZ, NA, NE, NG, NI, NL, NO, NZ, OM, PE, PG, PH, PL, PT, RO, RS, RU, SC, SD, SE, SG, SI, SK, SL, SM, SN, ST, SV, SY, SZ, TD, TG, TH, TJ, TM, TN, TR, TT, TZ, UA, UG, UZ, VC, VN, ZA, ZM, ZW only).
ASTRAZENECA UK LIMITED [GB/GB]; 15 Stanhope Gate London Greater London W1K 1LN (GB) (MG only).
BIRCH, Alan Martin [GB/GB]; (GB) (For US Only).
BUTLIN, Roger John [GB/GB]; (GB) (For US Only).
CAMPBELL, Leonie [GB/GB]; (GB) (For US Only).
GREEN, Clive [GB/GB]; (GB) (For US Only).
LEACH, Andrew [GB/GB]; (GB) (For US Only).
MURRAY, Paul Michael [IE/GB]; (GB) (For US Only).
RYBERG, Per Olof [SE/SE]; (SE) (For US Only).
WARING, Michael James [GB/GB]; (GB) (For US Only)
Inventors: BIRCH, Alan Martin; (GB).
BUTLIN, Roger John; (GB).
CAMPBELL, Leonie; (GB).
GREEN, Clive; (GB).
LEACH, Andrew; (GB).
MURRAY, Paul Michael; (GB).
RYBERG, Per Olof; (SE).
WARING, Michael James; (GB)
Agent: ASTRAZENECA INTELLECTUAL PROPERTY; AstraZeneca AB S-151 85 Södertälje (SE)
Priority Data:
61/218,539 19.06.2009 US
Title (EN) PYRAZINE CARBOXAMIDES AS INHIBITORS OF DGAT1
(FR) CARBOXAMIDES DE PYRAZINE UTILES COMME INHIBITEURS DE LA DGAT1
Abstract: front page image
(EN)DGAT-1 inhibitor compounds of formula (I), pharmaceutically-acceptable salts and pro-drugs thereof are described, together with pharmaceutical compositions, processes for making them and their use in treating, for example, obesity wherein, for example, r is 0 or 1 and X1 is linear (1-3C)alkyl; q is 0 or 1 and X1 is fluoro, chloro or (1-3C)alkyl; Y1 is selected from fluoro, chloro, bromo, cyano, (1-3C)alkyl and (1-2C)alkoxy; n is 0, 1 or 2 and Y2 is fluoro, chloro or (1-3C)alkyl; p is 0, 1 or 2 and Y3 is (1-3C)alkyl or forms a (3-5C)cycloalkyl ring; Z is carboxy or - CONHSO2 Me or –CONRbRc wherein Rb and Rc are independently selected, for example, from hydrogen and (1-4C)alkyl or Rb and Rc are linked so as to form a morpholine ring or a (4-6C)heterocyclic ring and when Z is –CONRbRc the Rb and Rc groups may be optionally substituted by carboxy.
(FR)L'invention concerne des composés inhibiteurs de la DGAT-1 de formule (I), et des sels pharmaceutiquement acceptables et des promédicaments de ceux-ci, ainsi que des compositions pharmaceutiques, leurs procédés de fabrication et leur utilisation dans le traitement de l'obésité, par exemple, formule dans laquelle r représente 0 ou 1 et X1 représente un (1-3C)alkyle linéaire; q représente 0 ou 1 et X1 représente fluoro, chloro ou (1-3C)alkyle; Y1 est sélectionné parmi fluoro, chloro, bromo, cyano, (1-3C)alkyle et (1-2C)alkoxy; n représente 0, 1 ou 2 et Y2 représente fluoro, chloro ou (1-3C)alkyle; p représente 0, 1 ou 2 et Y3 représente (1-3C)alkyle ou forme un noyau (3-5C)cycloalkyle; Z représente carboxy ou - CONHSO2 Me ou –CONRbRc, Rb et Rc étant indépendamment sélectionnés, par exemple, parmi hydrogène et (1-4C)alkyle ou Rb et Rc sont liés de façon à former un noyau morpholine ou un noyau (4-6C)hétérocyclique, et lorsque Z représente –CONRbRc, les groupes Rb et Rc peuvent être éventuellement substitués par carboxy.
Designated States: AE, AG, AL, AM, AO, AT, AU, AZ, BA, BB, BG, BH, BR, BW, BY, BZ, CA, CH, CL, 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, PE, PG, PH, PL, PT, RO, RS, RU, SC, SD, SE, SG, SK, SL, SM, ST, SV, SY, TH, TJ, TM, TN, TR, TT, TZ, UA, UG, US, UZ, VC, VN, ZA, ZM, ZW.
African Regional Intellectual Property Organization (BW, GH, GM, KE, LR, 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 (AL, 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, SM, 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)