Invention Grant
- Patent Title: CB1 receptor modulators
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Application No.: US12519432Application Date: 2007-12-17
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Publication No.: US08124634B2Publication Date: 2012-02-28
- Inventor: Martin Cooper , Jean-Marie Receveur , Thomas Hoegberg , Peter Aadal Nielsen , Jean-Michel Linget , Pia Karina Noeregaard , Anthony Murray , Emelie Bjurling
- Applicant: Martin Cooper , Jean-Marie Receveur , Thomas Hoegberg , Peter Aadal Nielsen , Jean-Michel Linget , Pia Karina Noeregaard , Anthony Murray , Emelie Bjurling
- Applicant Address: DK
- Assignee: 7TM Pharma A/S
- Current Assignee: 7TM Pharma A/S
- Current Assignee Address: DK
- Agency: Banner & Witcoff, Ltd.
- Priority: GB0625197.9 20061218; GB071798.9 20070914
- International Application: PCT/GB2007/004831 WO 20071217
- International Announcement: WO2008/075012 WO 20080626
- Main IPC: A61K31/415
- IPC: A61K31/415 ; A61K31/41 ; C07D231/12 ; C07D257/04

Abstract:
Compounds of formula (I) suppress the normal signalling activity CB1 receptors, and are thus useful in the treatment of diseases or conditions which are mediated by CB1 receptor signalling activity, such as treatment of obesity and overweight, prevention of weigh gain, treatment of diseases and conditions directly or indirectly associated with obesity and overweight: wherein A1 is hydrogen, —COOH, or tetrazolyl, and A2 is hydrogen, —COOH, or tetrazolyl, provided that one of A1 and A2 is either —COOH or tetrazolyl; p is 0 or 1 and A3 is phenyl or cycloalkyl, either of which is optionally substituted with R4 and/or R5; q is 0 or 1; R3 is hydrogen, C1-C4 alkyl, cycloalkyl, —CF3, or —OR9; R4 and R5 independently —R9, —CN, —F, —Cl, —Br, —OR9, —NR7R8, —NR7COR6, —NR7SO2R6, —COR6, —SR9, —SOR9, or —SO2R6; R6 is C1-C4 alkyl, cycloalkyl, —CF3 or —NR7R8; R7 and R8 are independently hydrogen, C1-C4 alkyl, —CF3, or cycloalkyl; R9 is hydrogen, C1-C4 alkyl, cycloalkyl, fully or partially fluorinated C1-C4 alkyl; R1 is (i) a bond, or (ii) —(CH2)aB1(CH2)b— wherein a and b are independently 0, 1, 2 or 3 provided that a+b is 1, 2 or 3; or (iii) —C(R10)(R11)—*, —C(R10)(R11)—O—*, —C(R10)(R11)CH2—*, —C(R10)(R11)CH2—O—*, —CH2C(R10)(R11)—*, —CH2C(R10)(R11)—O—*, —CH2—O—C(R10)(R11)—* or —C(R10)(R11)—O—CH2—*, wherein the bond indicated by an asterisk is attached to the pyrazole ring; R2 is a divalent radical of formula -Q1-A4-[Q2]w- wherein Q1, A4 Q2 and w are as defined in the specification; and R10 is hydrogen and R11 is (C1-C3)alkyl or —OH; or R10 and R11 are both (C1-C3)alkyl; or R10 and R11 taken together with the carbon atom to which they are attached form a (C3-C5)cycloalkyl ring.
Public/Granted literature
- US20100010061A1 CB1 RECEPTOR MODULATORS Public/Granted day:2010-01-14
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