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1. 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。

2. 发明申请

US20080312277A1 Gpr41 and Modulators Thereof for the Treatment of Insulin-Related Disorders 审中-公开
标题翻译： Gpr41及其调节剂治疗胰岛素相关性疾病
公开(公告)号：US20080312277A1
公开(公告)日：2008-12-18
申请号：US11666910
申请日：2005-11-01
申请人： James N. Leonard , Zhi Liang Chu , Marc A. Bruce , P. Douglas Boatman
发明人： James N. Leonard , Zhi Liang Chu , Marc A. Bruce , P. Douglas Boatman
IPC分类号： A61K31/47 , G01N33/566 , C07D215/38 , A61P3/10 , A61K31/4709 , C07D407/04
CPC分类号： G01N33/66 , G01N2500/04
摘要： The present invention relates to a method for identifying a glycemic stabilizing compound by: a) contacting a candidate compound with GPR41, and b) determining whether GPR41 functionality is modulated, where a modulation in GPR41 functionality is indicative of the candidate compound being a glycemic stabilizing compound. In addition, the invention relates to a method for identifying a glycemic stabilizing compound, comprising: a) contacting a candidate compound with GPR41, and b) determining whether GPR41 functionality is increased, wherein an increase in GPR41 functionality is indicative of the candidate compound being a glycemic stabilizing compound. Further, the invention relates to a method for identifying a glycemic stabilizing compound, comprising: a) contacting a candidate compound with GPR41, and b) determining whether GPR41 functionality is decreased, wherein a decrease in GPR41 functionality is indicative of the candidate compound being a glycemic stabilizing compound.
摘要翻译：本发明涉及通过以下方式鉴定血糖稳定化合物的方法：a）使候选化合物与GPR41接触，和b）确定是否调节GPR41功能性，其中GPR41官能度的调节指示候选化合物是血糖稳定剂复合。此外，本发明涉及一种鉴定血糖稳定化合物的方法，包括：a）使候选化合物与GPR41接触，和b）确定GPR41的功能是否增加，其中GPR41功能的增加指示候选化合物为血糖稳定化合物。此外，本发明涉及用于鉴定血糖稳定化合物的方法，其包括：a）使候选化合物与GPR41接触，和b）确定GPR41的功能性是否降低，其中GPR41官能度的降低指示候选化合物为血糖稳定化合物。

3. 发明授权

US5637732A Tricyclic and tetracyclic taxanes 失效
标题翻译：三环和四环紫杉烷
公开(公告)号：US5637732A
公开(公告)日：1997-06-10
申请号：US383775
申请日：1995-02-06
申请人： Robert A. Holton , Carmen Somoza , Hyeong B. Kim , Mitsuru Shindo , Ronald J. Biediger , P. Douglas Boatman , Chase Smith , Feng Liang , Krishna Murthi
发明人： Robert A. Holton , Carmen Somoza , Hyeong B. Kim , Mitsuru Shindo , Ronald J. Biediger , P. Douglas Boatman , Chase Smith , Feng Liang , Krishna Murthi
IPC分类号： C07D317/36 , C07C49/733 , C07C69/00 , C07C69/608 , C07C69/757 , C07D305/14 , C07D307/93 , C07D307/935 , C07D317/72 , C07D319/08 , C07D493/10 , C07F7/18
CPC分类号： C07D307/935 , C07D305/14 , C07D307/93 , C07D317/72 , C07D493/10
摘要： The synthesis of taxol and other tricyclic and tetracyclic taxanes.
摘要翻译：紫杉醇等三环和四环紫杉烷的合成。

4. 发明授权

US5405972A Synthetic process for the preparation of taxol and other tricyclic and tetracyclic taxanes 失效
标题翻译：制备紫杉醇和其他三环和四环紫杉烷的合成方法
公开(公告)号：US5405972A
公开(公告)日：1995-04-11
申请号：US189058
申请日：1994-01-27
申请人： Robert A. Holton , Carmen Somoza , Hyeong B. Kim , Mitsuru Shindo , Ronald J. Biediger , P. Douglas Boatman , Chase Smith , Feng Liang , Krishna Murthi
发明人： Robert A. Holton , Carmen Somoza , Hyeong B. Kim , Mitsuru Shindo , Ronald J. Biediger , P. Douglas Boatman , Chase Smith , Feng Liang , Krishna Murthi
IPC分类号： C07D317/36 , C07C49/733 , C07C69/00 , C07C69/608 , C07C69/757 , C07D305/14 , C07D307/93 , C07D307/935 , C07D317/72 , C07D319/08 , C07D493/10 , C07F7/18 , C07D317/70
CPC分类号： C07D307/935 , C07D305/14 , C07D307/93 , C07D317/72 , C07D493/10
摘要： Process for the synthesis of taxol and other tricyclic and tetracyclic taxanes.
摘要翻译：紫杉醇和其他三环和四环紫杉烷的合成方法。

5. 发明授权

US06433189B1 Tricyclic and tetracyclic taxane intermediates 有权
公开(公告)号：US06433189B1
公开(公告)日：2002-08-13
申请号：US09907330
申请日：2001-07-17
申请人： Robert A. Holton , Carmen Somoza , Hyeong Baik Kim , Mitsuru Shindo , Ronald J. Biediger , P. Douglas Boatman , Chase Smith , Feng Liang , Krishna Murthi
发明人： Robert A. Holton , Carmen Somoza , Hyeong Baik Kim , Mitsuru Shindo , Ronald J. Biediger , P. Douglas Boatman , Chase Smith , Feng Liang , Krishna Murthi
IPC分类号： C07D31770
摘要： The synthesis of taxol and other tricyclic and tetracyclic taxanes.

6. 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。

7. 发明授权

US06278026B1 Intermediates for tricyclic or tetracyclic taxanes 失效
标题翻译：三环或四环紫杉烷的中间体
公开(公告)号：US06278026B1
公开(公告)日：2001-08-21
申请号：US09333382
申请日：1999-06-15
申请人： Robert A. Holton , Carmen Somoza , Hyeong Baik Kim , Mitsuru Shindo , Ronald J. Biediger , P. Douglas Boatman , Chase Smith , Feng Liang , Krishna Murthi
发明人： Robert A. Holton , Carmen Somoza , Hyeong Baik Kim , Mitsuru Shindo , Ronald J. Biediger , P. Douglas Boatman , Chase Smith , Feng Liang , Krishna Murthi
IPC分类号： C07C49623
CPC分类号： C07D307/935 , C07D305/14 , C07D317/72 , C07D493/10 , C07F7/1804
摘要： The synthesis of taxol and other tricyclic and tetracyclic taxanes.
摘要翻译：紫杉醇等三环和四环紫杉烷的合成

8. 发明授权

US6005120A Tricyclic and tetracyclic taxanes 失效
标题翻译：三环和四环紫杉烷
公开(公告)号：US6005120A
公开(公告)日：1999-12-21
申请号：US778173
申请日：1997-01-02
申请人： Robert A. Holton , Carmen Somoza , Hyeong Baik Kim , Mitsuru Shindo , Ronald J. Biediger , P. Douglas Boatman , Chase Smith , Feng Liang , Krishna Murthi
发明人： Robert A. Holton , Carmen Somoza , Hyeong Baik Kim , Mitsuru Shindo , Ronald J. Biediger , P. Douglas Boatman , Chase Smith , Feng Liang , Krishna Murthi
IPC分类号： C07C69/00 , C07D305/14 , C07D307/935 , C07D317/72 , C07D493/10 , C07D317/70
CPC分类号： C07D307/935 , C07D305/14 , C07D317/72 , C07D493/10 , C07F7/1856
摘要： The synthesis of taxol and other tricyclic and tetracyclic taxanes.
摘要翻译：紫杉醇等三环和四环紫杉烷的合成。

9. 发明授权

US5760252A Synthetic process for the preparation of tricyclic and tetracyclic taxanes 失效
标题翻译：用于制备三环和四环紫杉烷的合成方法
公开(公告)号：US5760252A
公开(公告)日：1998-06-02
申请号：US769935
申请日：1996-12-19
申请人： Robert A. Holton , Carmen Somoza , Hyeong Baik Kim , Mitsuru Shindo , Ronald J. Biediger , P. Douglas Boatman , Chase Smith , Feng Liang , Krishna Murthi
发明人： Robert A. Holton , Carmen Somoza , Hyeong Baik Kim , Mitsuru Shindo , Ronald J. Biediger , P. Douglas Boatman , Chase Smith , Feng Liang , Krishna Murthi
IPC分类号： C07D317/36 , C07C49/733 , C07C69/00 , C07C69/608 , C07C69/757 , C07D305/14 , C07D307/93 , C07D307/935 , C07D317/72 , C07D319/08 , C07D493/10 , C07F7/18
CPC分类号： C07D307/935 , C07D305/14 , C07D307/93 , C07D317/72 , C07D493/10
摘要： Process for the synthesis of taxol and other tricyclic and tetracyclic taxanes.
摘要翻译：紫杉醇和其他三环和四环紫杉烷的合成方法。

10. 发明授权

US5618952A Synthetic process for the preparation of tricyclic and tetracyclic taxanes 失效
标题翻译：用于制备三环和四环紫杉烷的合成方法
公开(公告)号：US5618952A
公开(公告)日：1997-04-08
申请号：US383956
申请日：1995-02-06
申请人： Robert A. Holton , Carmen Somoza , Hyeong B. Kim , Mitsuru Shindo , Ronald J. Biediger , P. Douglas Boatman , Chase Smith , Feng Liang , Krishna Murthi
发明人： Robert A. Holton , Carmen Somoza , Hyeong B. Kim , Mitsuru Shindo , Ronald J. Biediger , P. Douglas Boatman , Chase Smith , Feng Liang , Krishna Murthi
IPC分类号： C07D317/36 , C07C49/733 , C07C69/00 , C07C69/608 , C07C69/757 , C07D305/14 , C07D307/93 , C07D307/935 , C07D317/72 , C07D319/08 , C07D493/10 , C07F7/18 , C07D307/77
CPC分类号： C07D307/935 , C07D305/14 , C07D307/93 , C07D317/72 , C07D493/10
摘要： Process for the synthesis of taxol and other tricyclic and tetracyclic taxanes.
摘要翻译：紫杉醇和其他三环和四环紫杉烷的合成方法。

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