Invention Grant
- Patent Title: Cannabinoid receptor modulators
- Patent Title (中): 大麻素受体调节剂
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Application No.: US12745708Application Date: 2008-12-08
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Publication No.: US08173680B2Publication Date: 2012-05-08
- Inventor: Jean-Marie Receveur , Emelie Bjurling , Anthony Murray , Thomas Hoegberg , Peter Aadal Nielsen , Jean-Michel Linget , Pia Karina Noerregaard , Dorthe Almholt
- Applicant: Jean-Marie Receveur , Emelie Bjurling , Anthony Murray , Thomas Hoegberg , Peter Aadal Nielsen , Jean-Michel Linget , Pia Karina Noerregaard , Dorthe Almholt
- Applicant Address: DK Hoersholm
- Assignee: 7TM Pharma A/S
- Current Assignee: 7TM Pharma A/S
- Current Assignee Address: DK Hoersholm
- Agency: Banner & Witcoff, Ltd.
- Priority: GB0724096.3 20071210; GB0813350.6 20080721
- International Application: PCT/GB2008/004051 WO 20081208
- International Announcement: WO2009/074782 WO 20090618
- Main IPC: A61K31/445
- IPC: A61K31/445 ; A61K31/41 ; A61K31/415 ; C07D401/02 ; C07D271/06 ; C07D231/00

Abstract:
Compounds of formula (I) are modulators of cannabinoid receptor CB1, useful inter alia for treatment of obesity: Formula (I). Wherein: X is a bond, or a divalent radical selected from —C(R10)(R11)—*, —C(R10)(R11)—O—*, —C(R10)(R11)CH2—*, —C(R10)(R11)CH2—O—*, —CH2C(R10)(R11)—*, —CH2C(R10)(R11)—O—*, and —CH2—O—C(R10)(R11)—*, wherein the bond indicated by an asterisk is attached to the pyrazole ring; Z is a carboxyl isostere radical selected from the group specified; R3 is hydrogen, (C1-C)alkyl or (C1C3)fluoroalkyl; R4 is a radical of formula -(Alk1)p-(Q1)r (L)s-Q2 wherein p, r, s, Alk1, L, Q1 and Q2 are as specified; or R3and R4 taken together with the nitrogen to which they are attached form a cyclic amino ring of 4 to 7 ring atoms which is optionally substituted by a radical of formula -(L)s-Q2 wherein s, L and Q2 are as defined above, or by an optional substituent selected from hydroxy, methoxy, —NH2—, or mono- or di-(C1C3)alkylamino; R5, R6, R7 and R8 are each independently selected from hydrogen —F, —Cl, —Br, —CN, (C1-C3)alkyl, (C1C3)fluoroalkyl, cyclopropyl, and —OR9; R10 is hydrogen, (C1C3)alkyl, hydroxyl or NH2, and R11 is hydrogen or (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
- US20100292273A1 Cannabinoid Receptor Modulators Public/Granted day:2010-11-18
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