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1. 发明申请

WO2004058249A1 1,5-DIARYL-PYRROLE-3-CARBOXAMIDE DERIVATIVES AND THEIR USE AS CANNABINOID RECEPTOR MODULATORS 审中-公开
标题翻译： 1,5-二氨基-3-吡啶酰胺衍生物及其作为CANNABINOID受体调节剂的用途
公开(公告)号：WO2004058249A1
公开(公告)日：2004-07-15
申请号：PCT/GB2003/005569
申请日：2003-12-18
申请人： ASTRAZENECA AB , ASTRAZENECA UK LIMITED , BERGGREN, Anna, Ingrid, Kristina , BOSTROM, Stig, Jonas , CHENG, Leifeng , ELEBRING, Stig, Thomas , GREASLEY, Peter , NAGARD, Mats , WILSTERMANN, Johan, Michael , TERRICABRAS, Emma
发明人： BERGGREN, Anna, Ingrid, Kristina , BOSTROM, Stig, Jonas , CHENG, Leifeng , ELEBRING, Stig, Thomas , GREASLEY, Peter , NAGARD, Mats , WILSTERMANN, Johan, Michael , TERRICABRAS, Emma
IPC分类号： A61K31/402
CPC分类号： C07D401/04 , A61K31/402 , A61K31/4025 , A61K31/454 , C07D207/34 , C07D401/06
摘要： The present invention relates to a compound of formula (I) (A chemical formula should be inserted here - please see paper copy enclosed herewith) in which R 1 and R 2 independently represent phenyl, thienyl or pyridyl each of which is optionally substituted by one, two or three groups represented by Z; and R 3 is H, a C 1-3 alkyl group, a C 1-3 alkoxymethyl group, trifluoromethyl, a hydroxyC 1-3 alkyl group, an aminoC 1-3 alkyl group, C 1-3 alkoxycarbonyl, carboxy, cyano, carbamoyl, mono or di C 1-3 alkylcarbamoyl, acetyl, or hydrazinocarbonyl of formula -CONHNR a R b wherein R a and R b are as defined for R 4 and R 5 respectively; X is CO or SO 2 ; Y is absent or represents NH optionally substituted by a C 1-3 alkyl group; R 4 and R 5 independently represent: a C 1-6 alkyl group; an (amino)C 1-4 alkyl- group in which the amino is optionally substituted by one or more C 1-3 alkyl groups; an optionally substituted non-aromatic C 3-15 carbocyclic group; a (C 3-12 cycloalkyl)C 1-3 alkyl- group; a group -(CH 2 ) r (phenyl ) s ; naphthyl; anthracenyl; a saturated 5 to 8 membered heterocyclic group containing one nitrogen and optionally one of the following: oxygen, sulphur or an additional nitrogen wherein the heterocyclic group is optionally substituted ;1-adamantylmethyl; a group - (CH 2 ) t Het where Het represents an aromatic heterocycle optionally substituted; or R 4 represents H and R 5 is as defined above; or R 4 and R 5 together with the nitrogen atom to which they are attached represent a saturated 5 to 8 membered heterocyclic group; R 6 is H, a C 1-3 alkyl group, a C 1-3 alkoxymethyl group, trifluoromethyl, a hydroxyC 1-3 alkyl group, C 1-3 alkoxycarbonyl, carboxy, cyano, carbamoyl, mono or di C 1-3 alkylcarbamoyl, acetyl, or hydrazinocarbonyl of formula -CONHNR a R b ; with provisos; to processes for preparing such compounds, to their use in the treatment of obesity, psychiatric and neurological disorders particularly obesity, to methods for their therapeutic use and to pharmaceutical compositions containing them.
摘要翻译：本发明涉及式（I）化合物（此处应插入化学式 - 请参见随附的纸质复制品），其中R 1和R 2独立地表示苯基，噻吩基或吡啶基，其各自为任选被一个，两个或三个由Z表示的基团取代; R 3为H，C 1-3烷基，C 1-3烷氧基甲基，三氟甲基，羟基C 1-3烷基，氨基C 1-3烷基，C 1-3烷氧基羰基，羧基，氰基，氨基甲酰基，一或二C 1-3烷基氨基甲酰基，乙酰基或肼基羰基，其中R a和R b分别如R 4和R 5所定义; X是CO或SO2; Y不存在或表示任选被C 1-3烷基取代的NH; R 4和R 5独立地表示：C 1-6烷基; 氨基被一个或多个C 1-3烷基任选取代的（氨基）C 1-4烷基 - 基团; 任选取代的非芳族C 3-15碳环基团; （C3-12环烷基）C1-3烷基; 基团 - （CH 2）r（苯基）s; 萘; 蒽; 含有一个氮的饱和5至8元杂环基和任选的以下之一：氧，硫或另外的氮，其中杂环基任选被取代; 1-金刚烷基甲基; 基团 - （CH 2）t Het，其中Het表示任选取代的芳族杂环; 或R 4表示H且R 5如上所定义; 或R 4和R 5与它们所连接的氮原子一起表示饱和的5至8元杂环基; R 6是H，C 1-3烷基，C 1-3烷氧基甲基，三氟甲基，羟基C 1-3烷基，C 1-3烷氧基羰基，羧基，氰基，氨基甲酰基，一或二C 1-3烷基氨基甲酰基，乙酰基或肼基羰基 -CONHNR

2. 发明申请

WO2004058255A1 4, 5-DIARYLTHIAZOLE DERIVATIVES AS CB-1 LIGANDS 审中-公开
标题翻译： 4，作为CB-1配体的5-二氨基噻唑衍生物
公开(公告)号：WO2004058255A1
公开(公告)日：2004-07-15
申请号：PCT/GB2003/005542
申请日：2003-12-18
申请人： ASTRAZENECA AB , ASTRAZENECA UK LIMITED , BERGGREN, Anna, Ingrid, Kristina , BOSTROM, Stig, Jonas , ELEBRING, Stig, Thomas , FALLEFORS, Linda , WILSTERMANN, Johan, Michael , GREASLEY, Peter
发明人： BERGGREN, Anna, Ingrid, Kristina , BOSTROM, Stig, Jonas , ELEBRING, Stig, Thomas , FALLEFORS, Linda , WILSTERMANN, Johan, Michael , GREASLEY, Peter
IPC分类号： A61K31/426
CPC分类号： C07D417/04 , C07D277/56 , C07D417/12
摘要： The present invention relates to compounds of formula (I): in which R 1 and R 2 independently represent phenyl, thienyl or pyridyl and R 3 represents a group -X-Y-NR 4 R 5 in which X is CO or SO 2 ; Y is absent or represents NH and the other substituente are as defined in the description and their use in the treatment of obesity, psychiatric and neurological disorders and to pharmaceutical compositions containing them.
摘要翻译：本发明涉及式（I）化合物：其中R 1和R 2独立地代表苯基，噻吩基或吡啶基，R 3代表基团-XY-NR 4 R 5 其中X为CO或SO2; Y不存在或表示NH，另一个取代基如描述中所定义，以及它们在治疗肥胖，精神病和神经障碍中的用途以及含有它们的药物组合物。

3. 发明申请

WO2004074844A1 SCREENING ASSAYS FOR CANNABINOID-LIGAND-TYPE MODULATORS OF GPR55 审中-公开
标题翻译： GPR55的CANNABINOID-LIGAND型调制器的屏幕测试
公开(公告)号：WO2004074844A1
公开(公告)日：2004-09-02
申请号：PCT/GB2004/000571
申请日：2004-02-13
申请人： ASTRAZENECA AB , ASTRAZENECA UK LIMITED , DRMOTA, Tomas , GREASLEY, Peter , GROBLEWSKI, Thierry
发明人： DRMOTA, Tomas , GREASLEY, Peter , GROBLEWSKI, Thierry
IPC分类号： G01N33/94
CPC分类号： G01N33/948 , G01N2500/00 , G01N2500/02
摘要： Screening assays for compounds that modulate the interaction between cannabinoids and the GPR55 receptor are disclosed. Furthermore, a method for determining the selectivity of a test compound against a panel of cannabinoid receptors including GPR55 is disclosed.
摘要翻译：公开了调节大麻素与GPR55受体之间的相互作用的化合物的筛选测定。此外，公开了一种用于确定测试化合物对包括GPR55的大麻素受体的选择性的方法。

4. 发明申请

WO2004008150A1 METHODS TO IDENTIFY TRUE ANTAGONISTS AND INVERSE AGONISTS OF THE CANNABINOID RECEPTOR 审中-公开
标题翻译：识别CANNABINOID受体的真正拮抗剂和反向激素的方法
公开(公告)号：WO2004008150A1
公开(公告)日：2004-01-22
申请号：PCT/GB2003/003066
申请日：2003-07-14
申请人： ASTRAZENECA AB , ASTRAZENECA UK LIMITED , GREASLEY, Peter
发明人： GREASLEY, Peter
IPC分类号： G01N33/68
CPC分类号： G01N33/948 , G01N2500/00
摘要： The present invention relates to a method to identify a true antagonist and an inverse agonist of a cannabinoid receptor (CB), and to discriminate between them. The invention further relates to the use of these true antagonists and inverse agonists in the treatment of CB associated disorders such as obesity, psychiatric and neurological disorders.
摘要翻译：本发明涉及鉴定大麻素受体（CB）的真正拮抗剂和反向激动剂的方法，并且在它们之间进行区分。本发明还涉及这些真正的拮抗剂和反向激动剂在治疗CB相关疾病如肥胖，精神病和神经障碍中的用途。

5. 发明申请

WO2004007551A1 SPLICE VARIANT CANNABINOID RECEPTOR (CB1B) 审中-公开
标题翻译：小麦变种甘油三酯受体（CB1B）
公开(公告)号：WO2004007551A1
公开(公告)日：2004-01-22
申请号：PCT/GB2003/003067
申请日：2003-07-14
申请人： ASTRAZENECA AB , ASTRAZENECA UK LIMITED , VU, Huy, Khang , GROBLEWSKI, Thierry , GREASLEY, Peter
发明人： VU, Huy, Khang , GROBLEWSKI, Thierry , GREASLEY, Peter
IPC分类号： C07K14/705
CPC分类号： C07K14/70571
摘要： The invention is based on the identification of a novel splice variant of human cannabinoid 1 (CB1) receptor, termed CB1b, and its use in the identification of therapeutic agents and in the diagnosis, prevention and treatment of CB associated disorders such as obesity, psychiatric, pain and neurological disorders.
摘要翻译：本发明基于人类大麻素1（CB1）受体的新型剪接变体的鉴定，称为CB1b，其用于鉴定治疗剂以及用于诊断，预防和治疗CB相关疾病如肥胖症，精神病学，疼痛和神经系统疾病。

6. 发明申请

WO2003051851A1 5, 6-DIARYL-PYRAZINE-2-AMIDE DERIVATIVES AS CB1 ANTAGONISTS 审中-公开
标题翻译： 5，作为CB1拮抗剂的6-DIARYL-PYRAZINE-2-AMIDE DERIVATIVES
公开(公告)号：WO2003051851A1
公开(公告)日：2003-06-26
申请号：PCT/GB2002/005742
申请日：2002-12-18
申请人： ASTRAZENECA AB , ASTRAZENECA UK LIMITED , BERGGREN, Anna, Ingrid, Kristina , BOSTROM, Stig, Jonas , ELEBRING, Stig, Thomas , GREASLEY, Peter , TERRICABRA, Emma , WILSTERMANN, Johan, Michael
发明人： BERGGREN, Anna, Ingrid, Kristina , BOSTROM, Stig, Jonas , ELEBRING, Stig, Thomas , GREASLEY, Peter , TERRICABRA, Emma , WILSTERMANN, Johan, Michael
IPC分类号： C07D241/24
CPC分类号： C07D241/24
摘要： The present invention relates to compounds of formula (I), and pharmaceutically acceptable salts, prodrugs, solvates and crystalline forms thereof, in which R 1 and R 2 independently represent: a C 1-6 alkyl group; an optionally substituted (amino)C 1-4 alkyl- group; an optionally substituted non-aromatic C 3-15 carbocyclic group; a (C 3-12 cycloalkyl)C 1-3 alkyl- group; a group -(CH 2 ) r (phenyl ) s in which r is 0,1, 2, 3 or 4, s is 1 when r is 0 otherwise s is 1 or 2 and the phenyl groups are optionally independently substituted by Z; naphthyl; anthracenyl; an optionally substituted saturated 5 to 8 membered heterocyclic group containing one nitrogen and optionally one of the following : oxygen, sulphur or an additional nitrogen; 1-adamantylmethyl; a group - (CH 2 ) t Het in which t is 0,1, 2, 3 or 4, and the alkylene chain is optionally substituted and Het represents an optionally substituted aromatic heterocycle; or R 1 represents H and R 2 is as defined above; or R 1 and R 2 together with the nitrogen atom to which they are attached represent a saturated optionally substituted 5 to 8 membered heterocyclic group as defined above; X is CO or SO 2 ; Y is absent or represents NH optionally substitututed by a C 1-3 alkyl group; R 3 and R 4 independently represent phenyl, thienyl or pyridyl substituted by Z; Z represents a C 1-3 alkyl group, a C 1-3 alkoxy group, hydroxy, halo,trifluoromethyl, trifluoromethylthio, trifluoromethoxy, trifluoromethylsulphonyl, nitro, amino, mono or di C 1-3 alkylamino, mono or di C 1-3 alkylamido, C 1-3 alkylsulphonyl, C 1-3 alkoxycarbonyl, carboxy, cyano, carbamoyl, mono or di C 1-3 alkyl carbamoyl, sulphamoyl and acetyl; and R 5 is H, a C 1-3 alkyl group, a C 1-3 alkoxymethyl group, trifluoromethyl, a hydroxyC 1-3 alkyl group, C 1-3 alkoxycarbonyl, carboxy, cyano, carbamoyl, mono or di C 1-3 alkylcarbamoyl, acetyl, or hydrazinocarbonyl of formula -CONHNR a R b ; with the provisos; and processes for preparing such compounds, their use in the treatment of obesity, psychiatric and neurological disorders, to methods for their therapeutic use and to pharmaceutical compositions containing them.
摘要翻译：本发明涉及式（I）化合物及其药学上可接受的盐，前体药物，溶剂合物和结晶形式，其中R 1和R 2独立地表示：C 1-6烷基; 任选取代的（氨基）C 1-4烷基; 任选取代的非芳族C 3-15碳环基团; （C3-12环烷基）C1-3烷基; 基团 - （CH 2）r（苯基）s，其中r为0,1,2,3或4，当r为0时，s为1，否则s为1或2，苯基任选独立地被Z取代; 萘; 蒽; 含有一个氮的任选取代的饱和5至8元杂环基和任选的以下之一：氧，硫或另外的氮; 1-金刚烷基甲基; 基团 - （CH 2）t Het，其中t为0,1,2,3或4，并且亚烷基链任选被取代，Het表示任选取代的芳族杂环; 或R 1表示H且R 2如上所定义; 或R 1和R 2与它们所连接的氮原子一起表示如上定义的饱和的任选取代的5至8元杂环基; X是CO或SO2; Y不存在或表示任选被C 1-3烷基取代的NH; R3和R4独立地表示苯基，噻吩基或被Z取代的吡啶基; Z表示C 1-3烷基，C 1-3烷氧基，羟基，卤素，三氟甲基，三氟甲硫基，三氟甲氧基，三氟甲基磺酰基，硝基，氨基，一或二C 1-3烷基氨基，一或二C 1-3烷基酰氨基，C 1-3烷基磺酰基，烷氧基羰基，羧基，氰基，氨基甲酰基，一或二C 1-3烷基氨基甲酰基，氨磺酰基和乙酰基; 并且R 5是H，C 1-3烷基，C 1-3烷氧基甲基，三氟甲基，羟基C 1-3烷基，C 1-3烷氧基羰基，羧基，氰基，氨基甲酰基，一或二C 1-3烷基氨基甲酰基，乙酰基或式-CONHNRaRb的肼基羰基 ; 附带条件以及制备这些化合物的方法，它们在治疗肥胖，精神和神经障碍中的应用，其治疗用途的方法和含有它们的药物组合物。

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