Title:
COMPOUNDS ACTIVE AT THE GLUCOCORTICOID RECEPTOR II
Document Type and Number:
WIPO Patent Application WO2002043648
Kind Code:
A8
Abstract:
This invention relates to novel compounds that are liver selective glucocorticoid receptor antagonists, to methods of preparing such compounds, and to methods for using such compounds in therapy and in the regulation of metabolism, especially lowering blood glucose levels. The compounds referred to are compounds according to the formula 1: wherein X is selected from: CH2, CHYR<7>, CHYC(O)R<7>, C=O, C=S, and C=NOR<8>,; Y is selected from: O, S, and NR<8>; R<1> is selected from: COOH and heteroaryl; R<2> and R<3> are independently of each other selected from: hydrogen, halogen, and C1-6 alkyl, provided that one of R<2> or R<3> is other than hydrogen; R<4> is selected from: C1-6-alkyl, C2-6 alkenyl, C2-6-alkynyl, halogen, (R<9>)(R<10>)N, R<8>C(Z)N(R<11>), R<8>OC(Z)N(R<11>), (R<9>)(R<10>)NC(Z)N(R<11>),R<8>S(O)2N(R<11>), (R<9>)(R<10>)NS(O)2N(R<11>), and R<8>SC (Z)N(R<11>);R<5> is selected from: (i) C1-6-alkyl which is substituted by a group selected from A, provided that A is not halogen; (ii) C7-12-alkyl, C2-12-alkenyl and C2-12-alkynyl; (iii) C1-12-alkyl, where one or more carbon atoms are replaced by Y, and where one or more carbons are optionally substituted by a group selected from A, provided that if more than one carbon is replaced by Y, the said Y groups are not directly connected to each other; R<6> is selected from: C1-12-alkyl, C3-8-cycloalkyl, C3-8-heterocycloalkyl, C2-6-alkenyl, and C2-6-alkynyl, aryl, and heteroaryl; R<7> is optionally selected from hydrogen; R<8>, R<9>, R<10> and R<11> are independently of each other selected from: hydrogen, C1-6-alkyl, C3-8-cycloalkyl, C2-6-alkenyl, C2-6-alkynyl, and C3-8-heterocycloalkyl, aryl and heteroaryl; or where any pair of R<8>, R<9>, R<10> and R<11> together with the atom or atoms to which they are bound form a ring having 3-7 ring members; or pharmaceutically acceptable salts, stereoisomers or prodrugs thereof.
Inventors:
PELCMAN BENJAMIN (SE)
GUSTAFSSON ANNIKA (SE)
KYM PHILIP R (US)
GUSTAFSSON ANNIKA (SE)
KYM PHILIP R (US)
Application Number:
PCT/IB2001/002302
Publication Date:
September 06, 2002
Filing Date:
November 28, 2001
Export Citation:
Assignee:
KAROBIO AB (SE)
ABBOTT LAB (US)
PELCMAN BENJAMIN (SE)
GUSTAFSSON ANNIKA (SE)
KYM PHILIP R (US)
ABBOTT LAB (US)
PELCMAN BENJAMIN (SE)
GUSTAFSSON ANNIKA (SE)
KYM PHILIP R (US)
International Classes:
A61K31/192; C07D295/08; A61K31/36; A61K31/426; A61K31/4409; A61K31/4453; A61K31/5375; A61P1/04; A61P3/04; A61P3/06; A61P3/08; A61P3/10; A61P3/14; A61P5/46; A61P7/02; A61P9/10; A61P9/12; A61P11/06; A61P13/12; A61P15/00; A61P15/08; A61P17/00; A61P17/02; A61P19/02; A61P19/08; A61P25/02; A61P25/18; A61P25/20; A61P25/22; A61P25/24; A61P25/28; A61P25/36; A61P27/00; A61P27/06; A61P29/00; A61P31/18; A61P35/00; A61P35/02; A61P37/02; A61P37/08; A61P43/00; C07C59/90; C07C69/76; C07C205/34; C07C205/35; C07C323/12; C07D213/30; C07D277/24; C07D295/092; C07D317/62; (IPC1-7): A61K/
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