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1. 发明申请

WO2004041802A1 4(PHENYL-PIPERAZINYL-METHYL) BENZAMIDE DERIVATIVES AND THEIR USE FOR THE TREATMENT OF PAIN OR GASTROINTESTINAL DISORDERS 审中-公开
标题翻译： 4（苯基 - 哌嗪 - 甲基）苯甲酰胺衍生物及其用于治疗疼痛或胃肠疾病的用途
公开(公告)号：WO2004041802A1
公开(公告)日：2004-05-21
申请号：PCT/SE2003/001707
申请日：2003-11-05
申请人： ASTRAZENECA AB , BROWN, William , GRIFFIN, Andrew , JONES, Paul , PAGÉ, Daniel , PLOBECK, Niklas , WALPOLE, Christopher
发明人： BROWN, William , GRIFFIN, Andrew , JONES, Paul , PAGÉ, Daniel , PLOBECK, Niklas , WALPOLE, Christopher
IPC分类号： C07D295/155
CPC分类号： C07D213/38 , C07D215/12 , C07D233/64 , C07D277/28 , C07D295/155 , C07D307/52 , C07D333/20
摘要： Compounds of general formula (I) wherein R 1 , R 2 and R 3 are as defined in the specification, as well as salts, enantiomers thereof and pharmaceutical compositions including the compounds are prepared. They are useful in therapy, in particular in the management of pain.
摘要翻译：制备其中R 1，R 2，R 3，如说明书中所定义的通式（I）的化合物及其盐，对映异构体和包含该化合物的药物组合物。它们可用于治疗，特别是治疗疼痛。

2. 发明申请

WO2004041800A1 4(PHENYL-PIPERAZINYL-METHYL) BENZAMIDE DERIVATIVES AND THEIR USE FOR THE TREATMENT OF PAIN OR GASTROINTESTINAL DISORDERS 审中-公开
标题翻译： 4（苯基 - 哌嗪 - 甲基）苯甲酰胺衍生物及其用于治疗疼痛或胃肠疾病的用途
公开(公告)号：WO2004041800A1
公开(公告)日：2004-05-21
申请号：PCT/SE2003/001703
申请日：2003-11-05
申请人： ASTRAZENECA AB , BROWN, William , GRIFFIN, Andrew , PLOBECK, Niklas , WALPOLE, Christopher
发明人： BROWN, William , GRIFFIN, Andrew , PLOBECK, Niklas , WALPOLE, Christopher
IPC分类号： C07D295/155
CPC分类号： C07D295/155 , C07D307/52
摘要： Compounds of general formula: wherein R 1 and R 2 are as defined in the specification, as well as salts, enantiomers thereof and pharmaceutical compositions including the compounds are prepared. They are useful in therapy, in particular in the management of pain.
摘要翻译：其中R 1和R 2如本说明书中所定义的化合物及其盐，对映异构体和包括该化合物的药物组合物。它们可用于治疗，特别是治疗疼痛。

3. 发明申请

WO2002094794A1 4 (PHENYL-PIPERAZINYL-METHYL) BENZAMIDE DERIVATIVES AND THEIR USE FOR THE TREATMENT OF PAIN ANXIETY OR GASTROINTESTINAL DISORDERS 审中-公开
标题翻译： 4（苯基 - 哌嗪 - 甲基）苯甲酸衍生物及其用于治疗疼痛或胃肠疾病的用途
公开(公告)号：WO2002094794A1
公开(公告)日：2002-11-28
申请号：PCT/SE2002/000956
申请日：2002-05-16
申请人： ASTRAZENECA AB , BROWN, William , WALPOLE, Christopher , PLOBECK, Niklas
发明人： BROWN, William , WALPOLE, Christopher , PLOBECK, Niklas
IPC分类号： C07D233/94
CPC分类号： C07D295/155 , C07D233/24 , C07D307/52 , C07D333/20
摘要： Compounds of general formula I R 1 is selected from any one of phenyl, pyridinyl, thienyl, furanyl, imidazolyl, pyrrolyl, triazolyl, thiazolyl, and pyridine N-oxide; R 2 is independently selected from ethyl and isopropyl; R 3 is independently selected from hydrogen and fluoro; R 4 is independently selected from -OH, -NH 2 and -NHSO 2 R 5 ; and R 5 is independently selected from hydrogen, -CF 3 and C 1 -C 6 alkyl, or salts thereof or separate enantiomers and salts thereof; where each R 1 heteroaromatic ring may optionally and independently be further substituted by 1, 2 or 3 substituents selected from straight and branched C 1 -C 6 alkyl, NO 2 , CF 3 , C 1 -C 6 alkoxy, chloro, fluoro, bromo, and iodo. The substitutions on the heteroaromatic ring may take place in any position on said ring systems; are disclosed and claimed in the present application, as well as separate enantiomers of the compounds and salts and pharmaceutical compositions comprising the novel compounds and their use in therapy, in particular in the management of pain, anxiety and functional gastrointestinal disorders.
摘要翻译：通式I R 1的化合物选自苯基，吡啶基，噻吩基，呋喃基，咪唑基，吡咯基，三唑基，噻唑基和吡啶N-氧化物中的任一种; R 2独立地选自乙基和异丙基; R 3独立地选自氢和氟; R 4独立地选自-OH，-NH 2和-NHSO 2 R 5; 和R 5独立地选自氢，-CF 3和C 1 -C 6烷基，或其盐或其单独的对映异构体和盐; 其中每个R 1杂芳环可任选地且独立地被1,2或3个选自直链和支链C 1 -C 6烷基，NO 2，CF 3，C 1 -C 6烷氧基，氯，氟，溴和碘的取代基取代。杂芳环上的取代可以在所述环体系上的任何位置进行; 在本申请中公开和要求保护，以及包含新化合物的化合物和盐和药物组合物的分开的对映异构体及其在治疗中的用途，特别是在治疗疼痛，焦虑和功能性胃肠道疾病中的用途。

4. 发明申请

WO2006014133A1 DIARYLMETHYL PIPERAZINE DERIVATIVES, PREPARATIONS THEREOF AND USES THEREOF 审中-公开
标题翻译：二甲基哌嗪衍生物，其制备及其用途
公开(公告)号：WO2006014133A1
公开(公告)日：2006-02-09
申请号：PCT/SE2005/001186
申请日：2005-07-27
申请人： AstraZeneca AB , BROWN, William , GRIFFIN, Andrew , HUDZIK, Thomas , MACIAG, Carla , SMAGIN, Gennady , WALPOLE, Christopher
发明人： BROWN, William , GRIFFIN, Andrew , HUDZIK, Thomas , MACIAG, Carla , SMAGIN, Gennady , WALPOLE, Christopher
IPC分类号： C07D295/155
CPC分类号： C07D295/145 , C07D295/155
摘要： Compounds of general formula: , as well as salts, enantiomers thereof and pharmaceutical compositions including the compounds are prepared. They are useful in therapy, in particular in the management of pain, depression and anxiety.
摘要翻译：制备通式的化合物，以及其盐，对映异构体和包括该化合物的药物组合物。它们可用于治疗，特别是治疗疼痛，抑郁和焦虑。

5. 发明申请

WO2004063157A1 DIARYLMETHYLIDENE PIPERIDINE DERIVATIVES, PREPARATIONS THEREOF AND USES THEREOF 审中-公开
标题翻译：二甲基苯胺哌啶衍生物，其制备及其用途
公开(公告)号：WO2004063157A1
公开(公告)日：2004-07-29
申请号：PCT/GB2004/000116
申请日：2004-01-13
申请人： ASTRAZENECA AB , ASTRAZENECA UK LIMITED , BROWN, William , GRIFFIN, Andrew , WALPOLE, Christopher
发明人： BROWN, William , GRIFFIN, Andrew , WALPOLE, Christopher
IPC分类号： C07D211/70
CPC分类号： C07D211/70 , C07D405/06 , C07D409/06 , C07D417/06
摘要： Compounds of general formula: wherein R 1 , R 2 , R 3 , R 4 , and R 5 are as defined in the specification, as well as salts, enantiomers thereof and pharmaceutical compositions including the compounds are prepared. They are useful in therapy, in particular in the management of pain.
摘要翻译：通式的化合物：其中R 1，R 2，R 3，R 4和R 5如说明书中所定义，以及其盐，对映体和药物组合物，包括制备化合物。它们可用于治疗，特别是治疗疼痛。

6. 发明申请

WO2002094785A1 4-(phenyl-(piperidin-4-yl)-amino)-benzamide derivatives and their use for the treatment of pain, anxiety or gastrointestinal disorders 审中-公开
标题翻译： 4-（苯基 - （哌啶-4-基） - 氨基） - 苯甲酰胺衍生物及其用于治疗疼痛，焦虑或胃肠道疾病
公开(公告)号：WO2002094785A1
公开(公告)日：2002-11-28
申请号：PCT/SE2002/000957
申请日：2002-05-16
申请人： ASTRAZENECA AB , BROWN, William , GRIFFIN, Andrew , WALPOLE, Christopher
发明人： BROWN, William , GRIFFIN, Andrew , WALPOLE, Christopher
IPC分类号： C07D211/58
CPC分类号： C07D401/06 , C07D211/58 , C07D405/06 , C07D409/06 , C07D417/06
摘要： Compounds of general formula I[Chemical formula should be inserted here. Please see paper copy] R 1 is selected from any one of phenyl, pyridinyl, thienyl, furanyl, imidazolyl, pyrrolyl, triazolyl, thiazolyl and pyridine N-oxide; where each R 1 phenyl ring and R 1 heteroaromatic ring may optionally and independently be further substituted by 1,2 or 3 substituents selected from straight and branched C 1 -C 6 alkyl, NO 2 , CF 3 , C 1 -C 6 alkoxy, chloro, fluoro, bromo, and iodo. The substitutions on the phenyl ring and on the heteroaromatic ring may take place in any position on said ring systems; are disclosed and claimed in the present application, as well as salts and pharmaceutical compositions comprising the novel compounds and their use in therapy, in particular in the management of pain, anxiety and functional gastrointestinal disorders.
摘要翻译：通式Ⅰ化合物[化学式应在此插入。请参见纸张复制] R1选自苯基，吡啶基，噻吩基，呋喃基，咪唑基，吡咯基，三唑基，噻唑基和吡啶N-氧化物中的任一种; 其中每个R 1苯基环和R 1杂芳环可以任选和独立地被1,2或3个选自直链和支链C 1 -C 6烷基，NO 2，CF 3，C 1 -C 6烷氧基，氯，氟，溴和碘的取代基取代。苯环上和杂芳环上的取代可以在所述环体系上的任何位置进行; 在本申请中公开和要求保护，以及包含新化合物的盐和药物组合物及其在治疗中的用途，特别是在治疗疼痛，焦虑和功能性胃肠道疾病中的用途。

7. 发明申请

WO2006068592A1 NEW BENZOTHIAZOLECARBOXAMIDES 审中-公开
标题翻译：新苯并噻唑氧化酶
公开(公告)号：WO2006068592A1
公开(公告)日：2006-06-29
申请号：PCT/SE2005/001964
申请日：2005-12-19
申请人： ASTRAZENECA AB , BROWN, William , GRIFFIN, Andrew , JOHNSTONE, Shawn , LABRECQUE, Denis , MUNRO, Alexander , PACHE, Sandrine , WALPOLE, Christopher
发明人： BROWN, William , GRIFFIN, Andrew , JOHNSTONE, Shawn , LABRECQUE, Denis , MUNRO, Alexander , PACHE, Sandrine , WALPOLE, Christopher
IPC分类号： C07D277/62 , A61K31/381 , A61P25/00 , C07D277/64 , C07D277/68 , C07D277/82
CPC分类号： C07D277/68 , C07D277/64
摘要： The present invention relates to new compounds of formula I, (I) wherein R 1 to R 4 , m, n and p, are as defined as in formula I, or salts, solvates or solvated salts thereof, processes for their preparation and to a new intermediate used in the preparation thereof, pharmaceutical formulations containing said compounds and to the use of said compounds in therapy.
摘要翻译：本发明涉及新的式I化合物，其中R 1至R 4，m，n和p的定义如式I所定义，（I）其中R 1，盐，溶剂合物或溶剂化盐，其制备方法和用于制备其的新中间体，含有所述化合物的药物制剂和所述化合物在治疗中的用途。

8. 发明申请

WO2002094782A1 4-(PHENYL-(PIPERIDIN-4-YL)-AMINO)-BENZAMIDE DERATIVATIVES AND THEIR USE FOR THE TREATMENT OF PAIN, ANXIETY OR GASTROINTESTINAL DISORDERS 审中-公开
标题翻译： 4-（苯基 - （哌啶-4-基） - 氨基） - 苯甲酸衍生物及其用于治疗疼痛，静脉炎或胃肠疾病的用途
公开(公告)号：WO2002094782A1
公开(公告)日：2002-11-28
申请号：PCT/SE2002/000944
申请日：2002-05-16
申请人： ASTRAZENECA AB , BROWN, William , GRIFFIN, Andrew , WALPOLE, Christopher
发明人： BROWN, William , GRIFFIN, Andrew , WALPOLE, Christopher
IPC分类号： C07D211/58
CPC分类号： C07D401/06 , C07D211/58 , C07D405/06 , C07D409/06 , C07D417/06 , Y02P20/55
摘要： Compounds of general formula I[Chemical formula should be inserted here. Please see paper copy] R 1 is selected from any one of phenyl, pyridinyl, pyrrolyl, thienyl, furanyl, imidazolyl, triazolyl, and pyridine N-oxide; where each R 1 phenyl ring and R 1 heteroaromatic ring may optionally and independently be further substituted by 1,2 or 3 substituents selected from straight and branched C 1 -C 6 alkyl, NO 2 , CF 3 , C 1 -C 6 alkoxy, chloro, fluoro, bromo, and iodo. The substitutions on the phenyl ring and on the heteroaromatic ring may take place in any position on said ring systems; are disclosed and claimed in the present application, as well as their pharmaceutically acceptable salts and pharmaceutical compositions comprising the novel compounds and their use in therapy, in particular in the management of pain, anxiety and functional gastrointestinal disorders.
摘要翻译：通式Ⅰ化合物[化学式应在此插入。请参见纸张复制] R1选自苯基，吡啶基，吡咯基，噻吩基，呋喃基，咪唑基，三唑基和吡啶N-氧化物中的任一种; 其中每个R 1苯基环和R 1杂芳环可以任选和独立地被1,2或3个选自直链和支链C 1 -C 6烷基，NO 2，CF 3，C 1 -C 6烷氧基，氯，氟，溴和碘的取代基取代。苯环上和杂芳环上的取代可以在所述环体系上的任何位置进行; 在本申请中公开和要求保护，以及它们的药学上可接受的盐和药物组合物，其包含新化合物及其在治疗中的用途，特别是在治疗疼痛，焦虑和功能性胃肠疾病中的用途。

9. 发明申请

WO2004063193A1 4-{`3-(SULFONYLAMINO) PHENYL! `1-(CYCLYMETHYL) PIPERIDIN-4-YLIDENE! METHYL} BENAZMIDE DERIVATIVES AS DELTA OPIOID RECEPTOR LIGANDS FOR THE TREATMENT OF PAIN, ANXIETY AND FUNCTIONAL GASTROINTESTINAL DISORDER 审中-公开
标题翻译： 4- {3-（磺酰氨基）苯基！ 1-（环己基）哌啶-4-酮甲状腺激素衍生物作为治疗疼痛，炎症和功能性胃肠疾病的阿尔法阿片受体配体
公开(公告)号：WO2004063193A1
公开(公告)日：2004-07-29
申请号：PCT/GB2004/000061
申请日：2004-01-13
申请人： ASTRAZENECA AB , ASTRAZENECA UK LIMITED , BROWN, William , GRIFFIN, Andrew , WALPOLE, Christopher
发明人： BROWN, William , GRIFFIN, Andrew , WALPOLE, Christopher
IPC分类号： C07D409/06
CPC分类号： C07D401/06 , C07D211/70 , C07D405/06 , C07D409/06 , C07D417/06
摘要： Compounds of general formula: (I) wherein R 1 , R 2 , R 3 , R 4 and R 5 are as defined in the specification, as well as salts, enantiomers thereof and pharmaceutical compositions including the compounds are prepared. They are useful in therapy, in particular in the management of pain.
摘要翻译：通式（I）的化合物，其中R 1，R 2，R 3，R 4和R 5如本说明书中所定义，以及其盐，对映异构体和制备包含该化合物的药物组合物。它们可用于治疗，特别是治疗疼痛。

10. 发明申请

WO2005066128A1 DIARYLMETHYLIDENE PIPERIDINE DERIVATIVES, PREPARATIONS THEREOF AND USES THEREOF 审中-公开
标题翻译：二甲基苯胺哌啶衍生物，其制备及其用途
公开(公告)号：WO2005066128A1
公开(公告)日：2005-07-21
申请号：PCT/SE2005/000013
申请日：2005-01-05
申请人： ASTRAZENECA AB , BROWN, William , GRIFFIN, Andrew , WALPOLE, Christopher
发明人： BROWN, William , GRIFFIN, Andrew , WALPOLE, Christopher
IPC分类号： C07D211/70
CPC分类号： C07D417/06 , C07D211/70 , C07D401/06
摘要： Compounds of Formula: wherein R 1 , R 2 , and R 3 are as defined in the specification, as well as salts, enantiomers thereof and pharmaceutical compositions including the compounds are prepared. They are useful in therapy, in particular in the management of pain.
摘要翻译：其中R 1，R 2和R 3如本说明书中所定义的化合物及其盐，对映异构体和包括该化合物的药物组合物。它们可用于治疗，特别是治疗疼痛。

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