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1. 发明申请

WO2009123714A3 PROCESSES FOR THE PREPARATION OF PYRAZOLE DERIVATIVES USEFUL AS MODULATORS OF THE 5-HT2A SEROTONIN RECEPTOR 审中-公开
标题翻译：制备作为5-HT2A丝氨酸受体的调节剂的吡唑衍生物的方法
公开(公告)号：WO2009123714A3
公开(公告)日：2010-01-28
申请号：PCT/US2009002019
申请日：2009-04-01
申请人： ARENA PHARM INC , KRISHNAN ASHWIN M , GHARBAOUI TAWFIK
发明人： KRISHNAN ASHWIN M , GHARBAOUI TAWFIK
IPC分类号： C07D241/04 , A61K31/496 , A61P25/20 , C07D403/06
CPC分类号： C07D403/06 , C07D231/16 , C07D241/04
摘要： The present invention relates to processes for preparing pyrazole derivatives of Formula (I) and salts and pharmaceutical compositions of the salts thereof, useful as modulators of 5-HT2A serotonin receptor activity. The present invention also relates to intermediates used in the processes, and their preparation. The present invention also relates to salts of compounds of Formula (I) and pharmaceutical compositions thereof.
摘要翻译：本发明涉及制备式（I）的吡唑衍生物的方法及其盐及其盐的药物组合物，其可用作5-HT2A 5-羟色胺受体活性的调节剂。本发明还涉及用于该方法及其制备的中间体。本发明还涉及式（I）化合物的盐及其药物组合物。

2. 发明申请

WO2009111004A1 PROCESSES FOR THE PREPARATION OF INTERMEDIATES RELATED TO THE 5-HT2C AGONIST (R)-8-CHLORO-1-METHYL-2,3,4,5-TETRAHYDRO-1H-3-BENZAZEPINE 审中-公开
标题翻译：制备与5-羟色胺-8-CH-1-甲基-2,3,4,5-四氢-1H-苯并恶唑相关的中间体的方法
公开(公告)号：WO2009111004A1
公开(公告)日：2009-09-11
申请号：PCT/US2009/001340
申请日：2009-03-03
申请人： ARENA PHARMACEUTICALS, INC. , CARLOS, Marlon V. , CASTRO, Ryan O. , GHARBAOUI, Tawfik , LU, Xiao-Xiong , MA, You-An , SAN MARTIN, Nicholas D.
发明人： CARLOS, Marlon V. , CASTRO, Ryan O. , GHARBAOUI, Tawfik , LU, Xiao-Xiong , MA, You-An , SAN MARTIN, Nicholas D.
IPC分类号： C07C17/16 , C07C215/08 , C07C209/68 , C07C211/29 , C07D223/16
CPC分类号： C07C209/74 , C07C17/16 , C07C17/38 , C07C213/08 , C07C25/02 , C07C211/29 , C07C215/08
摘要： The present invention provides processes and intermediates useful in the preparation of 8-chloro-1-methyl-2,3,4,5-tetrahydro-1 H -3-benzazepine, a serotonin (5-HT) receptor agonist that is useful in the treatment or prophylaxis of, for example, central nervous system disorders, such as obesity.
摘要翻译：本发明提供了可用于制备8-氯-1-甲基-2,3,4,5-四氢-1H-3-苯并吖庚因的方法和中间体，5-羟色胺（5-HT）受体激动剂可用于治疗或预防例如中枢神经系统疾病，例如肥胖症。

3. 发明申请

WO2007136689A2 CRYSTALLINE FORMS AND PROCESSES FOR THE PREPARATION OF PHENYL-PYRAZOLES USEFUL AS MODULATORS OF THE 5-HT2A SEROTONIN RECEPTOR 审中-公开
标题翻译：用于制备作为5-HT2A丝氨酸受体的调节剂的苯基吡唑的晶体形式和方法
公开(公告)号：WO2007136689A2
公开(公告)日：2007-11-29
申请号：PCT/US2007011810
申请日：2007-05-17
申请人： ARENA PHARM INC , GHARBAOUI TAWFIK , SENGUPTA DIPANJAN , KRISHNAN ASHWIN M , SHAH NAINESH , MACIAS MARK , HART RYAN M , LALLY EDWARD A
发明人： GHARBAOUI TAWFIK , SENGUPTA DIPANJAN , KRISHNAN ASHWIN M , SHAH NAINESH , MACIAS MARK , HART RYAN M , LALLY EDWARD A
IPC分类号： C07D231/12 , A61K31/415 , A61P7/00
CPC分类号： C07D231/12
摘要： The present invention relates to processes for preparing phenyl-pyrazoles of Formula (I) and salts and pharmaceutical compositions thereof, useful as modulators of 5-HT 2A serotonin receptor activity. The present invention also relates to intermediates used in the processes, and their preparation. The present invention also relates to crystalline forms of 5-HT 2A serotonin receptor modulators, compositions thereof and methods of using the same.
摘要翻译：本发明涉及制备式（I）的苯基 - 吡唑的方法及其盐和药物组合物，其可用作5-HT 2A 5-羟色胺受体活性的调节剂。本发明还涉及用于该方法及其制备的中间体。本发明还涉及5-HT 2A 5-羟色胺受体调节剂的结晶形式，其组合物及其使用方法。

4. 发明申请

WO2005044816A1 TETRAZOLE DERIVATIVES AND METHODS OF TREATMENT OF METABOLIC-RELATED DISORDERS THEREOF 审中-公开
标题翻译：四唑衍生物及其代谢相关疾病的治疗方法
公开(公告)号：WO2005044816A1
公开(公告)日：2005-05-19
申请号：PCT/US2004/035927
申请日：2004-10-29
申请人： ARENA PHARMACEUTICALS, INC. , MERCK & CO., INC. , SEMPLE, Graeme , SCHRADER, Thomas , SKINNER, Philip, J. , COLLETTI, Steven, L. , GHARBAOUI, Tawfik , IMBRIGLIO, Jason, E. , JUNG, Jae-Kyi , LIANG, Rui , RAGHAVAN, Subharekha , SCHMIDT, Darby , TATA, James, R.
发明人： SEMPLE, Graeme , SCHRADER, Thomas , SKINNER, Philip, J. , COLLETTI, Steven, L. , GHARBAOUI, Tawfik , IMBRIGLIO, Jason, E. , JUNG, Jae-Kyi , LIANG, Rui , RAGHAVAN, Subharekha , SCHMIDT, Darby , TATA, James, R.
IPC分类号： C07D403/04
CPC分类号： C07D491/04 , C07D403/04 , C07D495/04
摘要： The present invention relates to certain tetrazole derivatives of Formula (I), and pharmaceutically acceptable salts thereof, which exhibit useful pharmacological properties, for example, as agonists for the RUP25 receptor. Also provided by the present invention are pharmaceutical compositions containing compounds of the invention, and methods of using the compounds and compositions of the invention in the treatment of metabolic-related disorders, including dyslipidemia, atherosclerosis, coronary heart disease, insulin resistance, type 2 diabetes, Syndrome-X and the like. In addition, the present invention also provides for the use of the compounds of the invention in combination with other active agents such as those belonging to the class of α-glucosidase inhibitors, aldose reductase inhibitors, biguanides, HMG-CoA reductase inhibitors, squalene synthesis inhibitors, fibrates, LDL catabolism enhancers, angiotensin converting enzyme (ACE) inhibitors, insulin secretion enhancers and the like.
摘要翻译：本发明涉及式（I）的某些四唑衍生物及其药学上可接受的盐，其表现出有用的药理学性质，例如作为RUP25受体的激动剂。本发明还提供含有本发明化合物的药物组合物，以及使用本发明化合物和组合物治疗代谢相关疾病包括血脂异常，动脉粥样硬化，冠心病，胰岛素抵抗，2型糖尿病，综合征-X等。此外，本发明还提供本发明化合物与其它活性剂如属于α-葡糖苷酶抑制剂类，醛糖还原酶抑制剂，双胍类，HMG-CoA还原酶抑制剂，角鲨烯合成抑制剂，贝特类，LDL分解代谢增强剂，血管紧张素转换酶（ACE）抑制剂，胰岛素分泌增强剂等。

5. 发明申请

WO2005011677A1 5-SUBSTITUTED 2H-PYRAZOLE-3-CARBOXYLIC ACID DERIVATIVES AS AGONISTS FOR THE NICOTINIC ACID RECEPTOR RUP25 FOR THE TREATMENT OF DYSLIPIDEMIA AND RELATED DISEASES 审中-公开
标题翻译： 5-取代的2H-吡唑-3-羧酸衍生物作为用于治疗氯吡格雷和相关疾病的非甾体类受体RUP25的激动剂
公开(公告)号：WO2005011677A1
公开(公告)日：2005-02-10
申请号：PCT/US2004/018389
申请日：2004-06-10
申请人： ARENA PHARMACEUTICALS, INC. , SEMPLE, Graeme , GHARBAOUI, Tawfik , SHIN, Young-Jun , DECAIRE, Marc , AVERBUJ, Claudia , SKINNER, Philip, J.
发明人： SEMPLE, Graeme , GHARBAOUI, Tawfik , SHIN, Young-Jun , DECAIRE, Marc , AVERBUJ, Claudia , SKINNER, Philip, J.
IPC分类号： A61K31/415
CPC分类号： C07D231/14 , A61K31/415 , A61K45/06 , A61K2300/00
摘要： The present invention relates to certain pyrazole carboxylic acid and ester derivatives, and pharmaceutically acceptable salts thereof, which exhibit useful pharmaceutical properties, for example as agonists for the RUP25 receptor. (I) Also provided by the present invention are pharmaceutical compositions containing compounds of the invention, and methods of using the compounds and compositions of the invention in the prophylaxis or treatment of metabolic-related disorders, including dyslipidemia, atherosclerosis, coronary heart disease, insulin resistance, type 2 diabetes, Syndrome-X and the like. In addition, the present invention also provides for the use of the compounds of the invention in combination with other active agents such as those belonging to the class of α -glucosidase inhibitors, aldose reductase inhibitors, biguanides, HMG-CoA reductase inhibitors, squalene synthesis inhibitors, fibrates, LDL catabolism enhancers, angiotensin converting enzyme (ACE) inhibitors, insulin secretion enhancers and the like.the substituents are defined in claim 1.
摘要翻译：本发明涉及表现出有用的药物性质的某些吡唑羧酸和酯衍生物及其药学上可接受的盐，例如作为RUP25受体的激动剂。（I）本发明还提供含有本发明化合物的药物组合物，以及使用本发明化合物和组合物预防或治疗代谢相关疾病包括血脂异常，动脉粥样硬化，冠心病，胰岛素抗性，2型糖尿病，综合征等。此外，本发明还提供本发明化合物与其它活性剂如属于α-葡糖苷酶抑制剂类，醛糖还原酶抑制剂，双胍类，HMG-CoA还原酶抑制剂，角鲨烯合成抑制剂，贝特类，LDL分解代谢增强剂，血管紧张素转换酶（ACE）抑制剂，胰岛素分泌增强剂等。取代基如权利要求1中所定义。

6. 发明申请

WO2004032928A1 5-SUBSTITUTED 2H-PYRAZONE-3-CARBOXYLIC ACID DERIVATIVES AS ANTILIPOLYTIC AGENTS FOR THE TREATMENT OF METABOLIC-RELATED DISORDERS SUCH AS DYSLIPIDEMIA 审中-公开
标题翻译： 5-取代的2H-吡唑-3-羧酸衍生物作为治疗与代谢相关的疾病如抗坏血酸的抗血小板剂
公开(公告)号：WO2004032928A1
公开(公告)日：2004-04-22
申请号：PCT/US2003/032174
申请日：2003-10-09
申请人： ARENA PHARMACEUTICALS, INC. , SEMPLE, Graeme , AVERBUJ, Claudia , SKINNER, Philip , GHARBAOUI, Tawfik , SHIN, Young-Jun
发明人： SEMPLE, Graeme , AVERBUJ, Claudia , SKINNER, Philip , GHARBAOUI, Tawfik , SHIN, Young-Jun
IPC分类号： A61K31/45
CPC分类号： C07D231/16 , C07D231/14
摘要： The present invention relates to certain pyrazole carboxylic acid derivatives of Formula (Ia), and pharmaceutically acceptable salts thereof, as antilipolytic agents and against for the receptor RUP25, wherein: R 2 is H, halogen, C 1-12 alkyl or C 1-12 haloalkyl; and R 3 is C 3-6 cycloalkyl, C 1-12 alkyl, C 1-12 haloalkyl, C 3-6 cycloalkyl-C 1-4 -alkylene, aryl-C 1-4 -alkylene or heteroaryl-C 1-4 -alkylene, wherein said aryl-C 1-4 -alkylene and heteroaryl-C 1-4 -alkylene can be optionally substituted 1 to 5 substituents selected from the substituents listed in the claims. Also provided by the present invention are pharmaceutical compositions containing compounds of the invention, and methods of using the compounds and compositions of the invention in the treatment of metabolic-related disorders, including dyslipidemia, atherosclerosis, coronary heart disease, insulin resistance, type 2 diabetes, Syndrome-X and the like. In addition, the present invention also provides for pharmaceutical compositions in combination with other active agents, for example, those agents belonging to the class of α-glucosidase inhibitors, aldose reductase inhibitors, biguanides, HMG-CoA reductase inhibitors, squalene synthesis inhibitors, fibrates, LDL catabolism enhancers, angiotensin converting enzyme (ACE) inhibitors, insulin secretion enhancers, thiazolidinedione and the like.
摘要翻译：本发明涉及某些式（Ia）的吡唑羧酸衍生物及其药学上可接受的盐，作为抗脂解剂和抗受体RUP25，其中：R2是H，卤素，C1-12烷基或C1-12卤代烷基; 且R 3为C 3-6环烷基，C 1-12烷基，C 1-12卤代烷基，C 3-6环烷基-C 1-4亚烷基，芳基-C 1-4亚烷基或杂芳基-C 1-4 - 亚烷基，其中所述芳基-C1 -4-亚烷基和杂芳基-C 1-4 - 亚烷基可以是任选取代的1至5个选自权利要求中所列取代基的取代基。本发明还提供含有本发明化合物的药物组合物，以及使用本发明化合物和组合物治疗代谢相关疾病包括血脂异常，动脉粥样硬化，冠心病，胰岛素抵抗，2型糖尿病，综合征-X等。此外，本发明还提供了与其它活性剂（例如属于α-葡糖苷酶抑制剂，醛糖还原酶抑制剂，双胍类，HMG-CoA还原酶抑制剂，角鲨烯合成抑制剂，贝特类）的那些试剂组合的药物组合物，LDL分解代谢增强剂，血管紧张素转换酶（ACE）抑制剂，胰岛素分泌增强剂，噻唑烷二酮等。

7. 发明申请

WO2007136689A3 CRYSTALLINE FORMS AND PROCESSES FOR THE PREPARATION OF PHENYL-PYRAZOLES USEFUL AS MODULATORS OF THE 5-HT2A SEROTONIN RECEPTOR 审中-公开
公开(公告)号：WO2007136689A3
公开(公告)日：2007-11-29
申请号：PCT/US2007/011810
申请日：2007-05-17
申请人： ARENA PHARMACEUTICALS, INC. , GHARBAOUI, Tawfik , SENGUPTA, Dipanjan , KRISHNAN, Ashwin M. , SHAH, Nainesh , MACIAS, Mark , HART, Ryan M. , LALLY, Edward A.
发明人： GHARBAOUI, Tawfik , SENGUPTA, Dipanjan , KRISHNAN, Ashwin M. , SHAH, Nainesh , MACIAS, Mark , HART, Ryan M. , LALLY, Edward A.
IPC分类号： C07D231/12 , A61K31/415 , A61P7/00
摘要： The present invention relates to processes for preparing phenyl-pyrazoles of Formula (I) and salts and pharmaceutical compositions thereof, useful as modulators of 5-HT 2A serotonin receptor activity. The present invention also relates to intermediates used in the processes, and their preparation. The present invention also relates to crystalline forms of 5-HT 2A serotonin receptor modulators, compositions thereof and methods of using the same.

8. 发明申请

WO2006076455A8 PROCESSES FOR PREPARING PYRAZOLO[3,4-D]PYRIMIDINE ETHERS 审中-公开
标题翻译：制备吡唑并[3,4-d]嘧啶的方法
公开(公告)号：WO2006076455A8
公开(公告)日：2006-11-02
申请号：PCT/US2006001020
申请日：2006-01-12
申请人： ARENA PHARM INC , GHARBAOUI TAWFIK , SENGUPTA DIPANJAN , LALLY EDWARD A , KATO NAOMI S , CARLOS MARLON , RODRIGUEZ NATALIE
发明人： GHARBAOUI TAWFIK , SENGUPTA DIPANJAN , LALLY EDWARD A , KATO NAOMI S , CARLOS MARLON , RODRIGUEZ NATALIE
IPC分类号： C07D487/04
CPC分类号： C07D487/04
摘要： The present invention relates to processes for preparing pyrazolo[3,4-d]pyrimidine ether compounds that are modulators of glucose metabolism and therefore useful in the treatment of metabolic disorders such as diabetes and obesity.
摘要翻译：本发明涉及制备吡唑并[3,4-d]嘧啶醚化合物的方法，所述化合物是葡萄糖代谢调节剂并因此可用于治疗代谢病症如糖尿病和肥胖症。

9. 发明申请

WO2006076455A2 PROCESSES FOR PREPARING PYRAZOLO[3,4-D]PYRIMIDINE ETHERS 审中-公开
标题翻译：制备吡唑并[3,4-d]嘧啶的方法
公开(公告)号：WO2006076455A2
公开(公告)日：2006-07-20
申请号：PCT/US2006/001020
申请日：2006-01-12
申请人： ARENA PHARMACEUTICALS, INC. , GHARBAOUI, Tawfik , SENGUPTA, Dipangjan , LALLY, Edward, A. , KATO, Naomi, S. , CARLOS, Marlon , RODRIGUEZ, Natalie
发明人： GHARBAOUI, Tawfik , SENGUPTA, Dipangjan , LALLY, Edward, A. , KATO, Naomi, S. , CARLOS, Marlon , RODRIGUEZ, Natalie
IPC分类号： C07D487/04
CPC分类号： C07D487/04
摘要： The present invention relates to processes for preparing pyrazolo[3,4-d]pyrimidine ether compounds that are modulators of glucose metabolism and therefore useful in the treatment of metabolic disorders such as diabetes and obesity.
摘要翻译：本发明涉及制备吡唑并[3,4-d]嘧啶醚化合物的方法，所述化合物是葡萄糖代谢调节剂并因此可用于治疗代谢病症例如糖尿病和肥胖症。 p>

10. 发明申请

WO2006076243A1 PROCESSES FOR PREPARING 4-(PHENOXY-5-METHYL-PYRIMIDIN-4-YLOXY)PIPERIDINE-1-CARBOXYLIC ACID DERIVATIVES AND RELATED COMPOUNDS 审中-公开
标题翻译：制备4-（苯基-5-甲基 - 嘧啶-4-基）哌嗪-1-羧酸衍生物及其相关化合物的方法
公开(公告)号：WO2006076243A1
公开(公告)日：2006-07-20
申请号：PCT/US2006/000565
申请日：2006-01-09
申请人： ARENA PHARMACEUTICALS, INC. , GHARBAOUI, Tawfik , FRITCH, John, R , KRISHNAN, Ashwin, M , THROOP, Beverly, Wolgast , KATO, Naomi, S
发明人： GHARBAOUI, Tawfik , FRITCH, John, R , KRISHNAN, Ashwin, M , THROOP, Beverly, Wolgast , KATO, Naomi, S
IPC分类号： C07D401/12
CPC分类号： C07D401/12
摘要： The invention discloses: A process for preparing a compound of Formula (I); wherein said process comprises reacting a compound of Formula (II); wherein L 2 is a leaving group, with compound of Formula (III) in the presence of a base and a salt, thereby forming the compound of Formula (I). The substituents and variables are defined in the claims.
摘要翻译：本发明公开了一种制备式（I）化合物的方法。其中所述方法包括使式（II）化合物与其中L 2是离去基团，与式（III）的化合物在碱和盐的存在下反应，从而形成式（I）的化合物。取代基和变量在权利要求书中定义。

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