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1. 发明授权

US07241792B2 Fused pyrazole derivatives and methods of treatment of metabolic-related disorders thereof 有权
标题翻译：融合的吡唑衍生物及其代谢相关病症的治疗方法
公开(公告)号：US07241792B2
公开(公告)日：2007-07-10
申请号：US11315753
申请日：2005-12-22
申请人： P. Douglas Boatman , Thomas O. Schrader , Graeme Semple , Philip J. Skinner , Jae-Kyu Jung
发明人： P. Douglas Boatman , Thomas O. Schrader , Graeme Semple , Philip J. Skinner , Jae-Kyu Jung
IPC分类号： A61K31/407 , C07D231/54
CPC分类号： C07D403/04 , C07D209/80 , C07D209/88 , C07D231/54 , C07D265/36 , C07D471/04 , C07D471/14
摘要： The present invention relates to certain fused pyrazole derivatives of Formula (Ia), 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, DP receptor antagonists, and the like.
摘要翻译：本发明涉及式（Ia）的某些稠合吡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型糖尿病的方法，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，DP受体拮抗剂等。

2. 发明授权

US07612106B2 Fused pyrazole derivatives and methods of treatment of metabolic-related disorders thereof 有权
标题翻译：融合的吡唑衍生物及其代谢相关病症的治疗方法
公开(公告)号：US07612106B2
公开(公告)日：2009-11-03
申请号：US11601184
申请日：2006-11-17
申请人： P. Douglas Boatman , Thomas O. Schrader , Graeme Semple , Philip J. Skinner , Jae-Kyu Jung
发明人： P. Douglas Boatman , Thomas O. Schrader , Graeme Semple , Philip J. Skinner , Jae-Kyu Jung
IPC分类号： A61K31/407 , C07D231/54
CPC分类号： C07D403/04 , C07D209/80 , C07D209/88 , C07D231/54 , C07D265/36 , C07D471/04 , C07D471/14
摘要： The present invention relates to certain fused pyrazole derivatives of Formula (Ia), 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, DP receptor antagonists, and the like.
摘要翻译：本发明涉及式（Ia）的某些稠合吡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型糖尿病的方法，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，DP受体拮抗剂等。

3. 发明申请

US20090258892A1 FUSED PYRAZOLE DERIVATIVES AND METHODS OF TREATMENT OF METABOLIC-RELATED DISORDERS THEREOF 审中-公开
标题翻译：熔化的吡唑衍生物及其代谢相关疾病的治疗方法
公开(公告)号：US20090258892A1
公开(公告)日：2009-10-15
申请号：US12433704
申请日：2009-04-30
申请人： P. Douglas Boatman , Thomas O. Schrader , Graeme Semple , Philip J. Skinner , Jae-Kyu Jung
发明人： P. Douglas Boatman , Thomas O. Schrader , Graeme Semple , Philip J. Skinner , Jae-Kyu Jung
IPC分类号： A61K31/437 , C07D231/54 , C07D403/04 , A61K31/416 , A61K31/41 , A61K31/40
CPC分类号： C07D403/04 , C07D209/80 , C07D209/88 , C07D231/54 , C07D265/36 , C07D471/04 , C07D471/14
摘要： The present invention relates to certain fused pyrazole derivatives of Formula (Ia), 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, DP receptor antagonists, and the like.
摘要翻译：本发明涉及式（Ia）的某些稠合吡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型糖尿病的方法，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，DP受体拮抗剂等。

4. 发明授权

US08507473B2 3H-imidazo[4,5-b]pyridin-5-ol derivatives useful in the treatment of GPR81 receptor disorders 失效
标题翻译：可用于治疗GPR81受体疾病的3H-咪唑并[4,5-b]吡啶-5-醇衍生物
公开(公告)号：US08507473B2
公开(公告)日：2013-08-13
申请号：US13063305
申请日：2009-09-10
申请人： P. Douglas Boatman , Benjamin R. Johnson , Jae-Kyu Jung , Michelle Kasem , Thomas O. Schrader , Philip J. Skinner , Steven Colletti
发明人： P. Douglas Boatman , Benjamin R. Johnson , Jae-Kyu Jung , Michelle Kasem , Thomas O. Schrader , Philip J. Skinner , Steven Colletti
IPC分类号： C07D471/04 , A61K31/437 , A61K31/55 , A61P3/06 , A61P3/10 , A61P9/10
CPC分类号： C07D471/04
摘要： The present invention is directed to certain 3H-imidazo[4,5-b]pyridin-5-ol derivatives of Formula (Ia) and pharmaceutically acceptable salts thereof, which exhibit useful pharmacological properties, for example, as agonists of the GPR81 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 GPR81 associated disorders, for example, dyslipidemia, atherosclerosis, atheromatous disease, hypertension, coronary heart disease, stroke, insulin resistance, impaired glucose tolerance, type 2 diabetes, syndrome X, obesity, psoriasis, rheumatoid arthritis, Crohn's disease, transplant rejection, multiple sclerosis, systemic lupus erythematosus, ulcerative colitis, type 1 diabetes and acne.
摘要翻译：本发明涉及式（Ia）的某些3H-咪唑并[4,5-b]吡啶-5-醇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GPR81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GPR81相关疾病例如血脂异常，动脉粥样硬化，动脉粥样硬化疾病，高血压，冠心病，中风，胰岛素抵抗，葡萄糖耐量异常，2型糖尿病，X综合征，肥胖症，牛皮癣，类风湿性关节炎，克罗恩病，移植排斥反应，多发性硬化，系统性红斑狼疮，溃疡性结肠炎，1型糖尿病和痤疮。

5. 发明申请

US20110172209A1 3H-IMIDAZO[4,5-B]PYRIDIN-5-OL DERIVATIVES USEFUL IN THE TREATMENT OF GPR81 RECEPTOR DISORDERS 失效
标题翻译：用于治疗GPR81受体疾病的3H-咪唑并[4,5-B]吡啶-5-OL衍生物
公开(公告)号：US20110172209A1
公开(公告)日：2011-07-14
申请号：US13063305
申请日：2009-09-10
申请人： P. Douglas Boatman , Benjamin R. Johnson , Jae-Kyu Jung , Michelle Kasem , Thomas O. Schrader , Philip J. Skinner , Steven Colletti
发明人： P. Douglas Boatman , Benjamin R. Johnson , Jae-Kyu Jung , Michelle Kasem , Thomas O. Schrader , Philip J. Skinner , Steven Colletti
IPC分类号： A61K31/437 , C07D471/04 , A61K31/55 , A61P3/06 , A61P3/10 , A61P9/10 , A61P9/12 , A61P9/00 , A61P3/08 , A61P3/04 , A61P17/06 , A61P29/00 , A61P37/06 , A61P25/28 , A61P17/10
CPC分类号： C07D471/04
摘要： The present invention is directed to certain 3H-imidazo[4,5-b]pyridin-5-ol derivatives of Formula (Ia) and pharmaceutically acceptable salts thereof, which exhibit useful pharmacological properties, for example, as agonists of the GPR81 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 GPR81 associated disorders, for example, dyslipidemia, atherosclerosis, atheromatous disease, hypertension, coronary heart disease, stroke, insulin resistance, impaired glucose tolerance, type 2 diabetes, syndrome X, obesity, psoriasis, rheumatoid arthritis, Crohn's disease, transplant rejection, multiple sclerosis, systemic lupus erythematosus, ulcerative colitis, type 1 diabetes and acne.
摘要翻译：本发明涉及式（Ia）的某些3H-咪唑并[4,5-b]吡啶-5-醇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GPR81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GPR81相关疾病例如血脂异常，动脉粥样硬化，动脉粥样硬化疾病，高血压，冠心病，中风，胰岛素抵抗，葡萄糖耐量异常，2型糖尿病，X综合征，肥胖症，牛皮癣，类风湿性关节炎，克罗恩病，移植排斥反应，多发性硬化，系统性红斑狼疮，溃疡性结肠炎，1型糖尿病和痤疮。

6. 发明授权

US09085581B2 Processes for the preparation of S1P1 receptor modulators and crystalline forms thereof 有权
标题翻译：制备S1P1受体调节剂及其结晶形式的方法
公开(公告)号：US09085581B2
公开(公告)日：2015-07-21
申请号：US13581846
申请日：2011-03-02
申请人： Robert M. Jones , Daniel J. Buzard , Tawfik Gharbaoui , Benjamin R. Johnson , Michelle Kasem , Thomas O. Schrader , Scott Stirn
发明人： Robert M. Jones , Daniel J. Buzard , Tawfik Gharbaoui , Benjamin R. Johnson , Michelle Kasem , Thomas O. Schrader , Scott Stirn
IPC分类号： C07D487/16 , A61K31/403 , C07D487/04
CPC分类号： C07D487/04
摘要： The present invention relates to salts, processes, and process intermediates useful in the preparation of (R)-2-(9-chloro -7-(4-isopropoxy-3-(trifluoromethyl)benzyloxy)-2,3-dihydro-1H-pyrrolo[1,2-a]indol-1-yl)acetic acid of Formula (Ia), salts, and crystalline forms thereof. The compound (R)-2-(9-chloro-7-(4-isopropoxy-3-(trifluoromethyl)benzyloxy)-2,3-dihydro-1H-pyrrolo[1,2-a]indol-1-yl)acetic acid has been identified as an S1P1 receptor modulator that is useful in the treatment of S1P1 receptor-associated disorders, for example, diseases and disorders mediated by lymphocytes, transplant rejection, autoimmune diseases and disorders, inflammatory diseases and disorders (e.g., acute and chronic inflammatory conditions), cancer, and conditions characterized by an underlying defect in vascular integrity or that are associated with angiogenesis such as may be pathologic (e.g., as may occur in inflammation, tumor development, and atherosclerosis).
摘要翻译：本发明涉及可用于制备（R）-2-（9-氯-7-（4-异丙氧基-3-（三氟甲基）苄氧基）-2,3-二氢-1H- - 吡咯并[1,2-a]吲哚-1-基）乙酸，其盐和结晶形式。化合物（R）-2-（9-氯-7-（4-异丙氧基-3-（三氟甲基）苄氧基）-2,3-二氢-1H-吡咯并[1,2-a]吲哚-1-基）乙酸被鉴定为可用于治疗S1P1受体相关疾病的S1P1受体调节剂，例如由淋巴细胞介导的疾病和病症，移植排斥反应，自身免疫性疾病和病症，炎性疾病和病症（例如急性和慢性炎性病症），癌症和特征在于血管完整性的潜在缺陷或与血管发生相关的病症，例如可能是病理性的（例如，可能发生在炎症，肿瘤发展和动脉粥样硬化中）。

7. 发明申请

US20120329848A1 PROCESSES FOR THE PREPARATION OF S1P1 RECEPTOR MODULATORS AND CRYSTALLINE FORMS THEREOF 有权
标题翻译：制备S1P1受体调节剂的方法及其结晶形式
公开(公告)号：US20120329848A1
公开(公告)日：2012-12-27
申请号：US13581846
申请日：2011-03-02
申请人： Robert M. Jones , Daniel J. Buzard , Tawfik Gharbaoui , Benjamin R. Johnson , Michelle Kasem , Thomas O. Schrader , Scott Stirn
发明人： Robert M. Jones , Daniel J. Buzard , Tawfik Gharbaoui , Benjamin R. Johnson , Michelle Kasem , Thomas O. Schrader , Scott Stirn
IPC分类号： C07D487/04 , C07C41/01 , A61P37/00 , A61P9/10 , A61P3/10 , A61P17/10 , A61P1/16 , A61P17/06 , A61K31/407 , A61P1/04
CPC分类号： C07D487/04
摘要： The present invention relates to salts, processes, and process intermediates useful in the preparation of (R)-2-(9-chloro-7-(4-isopropoxy-3-(trifluoromethyl)benzyloxy)-2,3-dihydro-1H-pyrrolo[1,2-a]indol-1-yl)acetic acid of Formula (Ia), salts, and crystalline forms thereof. The compound (R)-2-(9-chloro-7-(4-isopropoxy-3-(trifluoromethyl)benzyloxy)-2,3-dihydro-1H-pyrrolo[1,2-a]indol-1-yl)acetic acid has been identified as an S1P1 receptor modulator that is useful in the treatment of S1P1 receptor-associated disorders, for example, diseases and disorders mediated by lymphocytes, transplant rejection, autoimmune diseases and disorders, inflammatory diseases and disorders (e.g., acute and chronic inflammatory conditions), cancer, and conditions eases characterized by an underlying defect in vascular integrity or that are associated with angiogenesis such as may be pathologic (e.g., as may occur in inflammation, tumor development, and atherosclerosis).
摘要翻译：本发明涉及可用于制备（R）-2-（9-氯-7-（4-异丙氧基-3-（三氟甲基）苄氧基）-2,3-二氢-1H- - 吡咯并[1,2-a]吲哚-1-基）乙酸，其盐和结晶形式。化合物（R）-2-（9-氯-7-（4-异丙氧基-3-（三氟甲基）苄氧基）-2,3-二氢-1H-吡咯并[1,2-a]吲哚-1-基）乙酸被鉴定为可用于治疗S1P1受体相关疾病的S1P1受体调节剂，例如由淋巴细胞介导的疾病和病症，移植排斥反应，自身免疫性疾病和病症，炎性疾病和病症（例如急性和慢性炎性病症），癌症和病症特征在于血管完整性的潜在缺陷或与血管发生相关的疾病，例如可能是病理性的（例如，可能发生在炎症，肿瘤发展和动脉粥样硬化中）。

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