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1. 发明申请

US20100173915A1 PHARMACEUTICAL COMPOSITIONS FOR THE TREATMENT OF CHRONIC HEART FAILURE COMPRISING PYRAZOLOPYRIMIDINONE DERIVATIVE COMPOUND 审中-公开
标题翻译：用于治疗包含吡唑并吡啶酮衍生化合物的慢性心力衰竭的药物组合物
公开(公告)号：US20100173915A1
公开(公告)日：2010-07-08
申请号：US12602847
申请日：2008-06-03
申请人： Jee-Hyun Shin , Gook-Jun Ahn , Kyung-Koo Kang , Byoung-Ok Ahn , Moo-Hi Yoo
发明人： Jee-Hyun Shin , Gook-Jun Ahn , Kyung-Koo Kang , Byoung-Ok Ahn , Moo-Hi Yoo
IPC分类号： A61K31/519 , A61P9/00 , C07D487/04 , A61P9/04
CPC分类号： A61K31/519 , A61K9/2059 , A61K9/4866
摘要： Disclosed herein is a therapeutic agent for chronic heart failure comprising, as an effective ingredient, 5-[2-propyloxy-5-(1-methyl-2-pyrrolidinyl-ethylamidosulfonyl)phenyl]-1-methyl-propyl-1,6-dihydro-7H-pyrazolo(4,3-d)pyrimidine-7-one. The compound inhibits phosphodiesterase-5 (PDE-5), which catalyzes the intracellular degradation of cyclic guanosine monophosphatase (cGMP), thereby mitigating several signs of chronic heart failure, that is, thereby preventing left ventricular dilatation, decreasing ventricular wall thinning, lowering elevated cardiac and circulating levels of atrial natriuretic peptide (ANP), and inhibiting ventricular fibrosis. Also, the compound has advantages in that it reaches the maximal plasma level in a short time, has an in vivo half-life longer than conventional PDE-5 inhibitors, allowing decreased administration frequency, and has fewer side effects, thus ensuring safety. Thus, the compound is useful as a therapeutic agent for chronic heart failure.
摘要翻译：本文公开了一种用于慢性心力衰竭的治疗剂，其包含作为有效成分的5- [2-丙氧基-5-（1-甲基-2-吡咯烷基 - 乙基氨基磺酰基）苯基] -1-甲基 - 丙基-1,6- 二氢-7H-吡唑并（4,3-d）嘧啶-7-酮。该化合物抑制磷酸二酯酶-5（PDE-5），其催化环鸟苷酸单磷酸酶（cGMP）的细胞内降解，从而减轻慢性心力衰竭的几个迹象，从而预防左心室扩张，降低心室壁变薄，降低升高心脏和循环水平的心房钠尿肽（ANP），并抑制心室纤维化。此外，该化合物具有在短时间内达到最大血浆水平的优点，具有比常规PDE-5抑制剂更长的体内半衰期，允许降低给药频率，并且具有较少的副作用，从而确保安全性。因此，该化合物可用作慢性心力衰竭的治疗剂。

2. 发明申请

US20100240725A1 NOVEL 1,3-DIHYDRO-5-ISOBENZOFURANCARBONITRILE DERIVATIVES AND PHARMACEUTICAL COMPOSITION THEREOF FOR THE TREATMENT OF PREMATURE EJACULATION 失效
标题翻译：新型1,3-二氢-5-ISOBENZFURBANITRILE衍生物及其药物组合物，用于治疗预防性呕吐
公开(公告)号：US20100240725A1
公开(公告)日：2010-09-23
申请号：US12739870
申请日：2008-10-31
申请人： Yeong Geon Lee , Soo-Jung Choi , Tae-Kyung Kang , Mi-Jeong Seo , Chang-Yong Shin , Kyung-Seok Lee , Gook-Jun Ahn , Seul-Min Choi , Yong-Duck Kim , Dong-Hwan Kim , Kyung-Koo Kang , Hyun-Joo Shim , Dong-Sung Kim , Byoung-Ok Ahn , Moo-Hi Yoo
发明人： Yeong Geon Lee , Soo-Jung Choi , Tae-Kyung Kang , Mi-Jeong Seo , Chang-Yong Shin , Kyung-Seok Lee , Gook-Jun Ahn , Seul-Min Choi , Yong-Duck Kim , Dong-Hwan Kim , Kyung-Koo Kang , Hyun-Joo Shim , Dong-Sung Kim , Byoung-Ok Ahn , Moo-Hi Yoo
IPC分类号： A61K31/4178 , C07D307/87 , A61K31/343 , A61P15/00 , C07D405/06 , A61K31/4155 , C07D409/04 , A61K31/381
CPC分类号： C07D307/87 , C07D405/06 , C07D409/04 , C07D409/06
摘要： Disclosed herein are novel 1,3-dihydro-5-isobenzofurancarbonitrile derivatives represented by Formula 1, or pharmaceutically acceptable salts thereof. Also disclosed is a pharmaceutical composition for treating or preventing premature ejaculation including the compound. The 1,3-dihydro-5-isobenzofurancarbonitrile derivatives have a short half-life and inhibit the ejaculation process by selectively inhibiting serotonin reuptake via a serotonin reuptake transporter present in a presynaptic neuron. Thus, the compounds are useful in the treatment and prevention of premature ejaculation.
摘要翻译：本文公开了由式1表示的新的1,3-二氢-5-异苯并呋喃腈衍生物或其药学上可接受的盐。还公开了用于治疗或预防早泄的药物组合物，包括该化合物。 1,3-二氢-5-异苯并呋喃腈衍生物具有短的半衰期，并通过选择性地通过存在于突触前神经元中的5-羟色胺再摄取转运蛋白选择性抑制5-羟色胺再摄取来抑制射精过程。因此，这些化合物可用于治疗和预防早泄。

3. 发明授权

US08440669B2 Pharmaceutical composition for prevention and treatment of diabetes or obesity comprising a compound that inhibits activity of dipeptidyl peptidase-IV, and other antidiabetic or antiobesity agents as active ingredients 有权
标题翻译：用于预防和治疗糖尿病或肥胖症的药物组合物，其包含抑制二肽基肽酶-IV的活性的化合物和其它抗糖尿病或抗肥胖剂作为活性成分
公开(公告)号：US08440669B2
公开(公告)日：2013-05-14
申请号：US13124150
申请日：2009-10-16
申请人： Chang Yell Shin , Song-Hyen Choi , Yu Na Chae , Eun Kyoung Yang , Gook Jun Ahn , Moon-Ho Son , Heung Jae Kim , Woo Young Kwak , Jong Pil Min , Tae Hyun Yoon , Soon Hoe Kim , Moohi Yoo
发明人： Chang Yell Shin , Song-Hyen Choi , Yu Na Chae , Eun Kyoung Yang , Gook Jun Ahn , Moon-Ho Son , Heung Jae Kim , Woo Young Kwak , Jong Pil Min , Tae Hyun Yoon , Soon Hoe Kim , Moohi Yoo
IPC分类号： A01N43/60 , A61K31/50 , A61K31/497
CPC分类号： A61K45/06 , A61K9/0019 , A61K9/145 , A61K9/2059 , A61K31/155 , A61K31/4439 , A61K31/495 , A61K31/5377 , A61K31/64 , A61K31/7028 , A61K47/02 , Y02P20/582 , A61K2300/00
摘要： The present invention relates to a pharmaceutical composition for the prevention and treatment of diabetes or obesity comprising as active ingredients a compound which inhibits the activity of dipeptidyl peptidase-IV (DPP-IV), a pharmaceutically acceptable salt thereof, a hydrate thereof, or a solvate thereof, and one or more other antidiabetic or antiobesity agents. The pharmaceutical composition exhibits excellent glucose tolerance and may be useful in the prevention and treatment of diabetes, obesity, and the like by effectively inhibiting blood glucose levels and reducing fat mass.
摘要翻译：本发明涉及用于预防和治疗糖尿病或肥胖症的药物组合物，其包含抑制二肽基肽酶-IV（DPP-IV）的活性的化合物，其药学上可接受的盐，其水合物或其一种或多种其它抗糖尿病或抗肥胖剂。药物组合物表现出优异的葡萄糖耐量，可有效抑制血糖水平和降低脂肪量，可用于预防和治疗糖尿病，肥胖症等。

4. 发明申请

US20110201624A1 Pharmaceutical Composition for Prevention and Treatment of Diabetes or Obesity Comprising a Compound that Inhibits Activity of Dipeptidyl Peptidase-IV, and other Antidiabetic or Antiobesity Agents as Active Ingredients 有权
标题翻译：用于预防和治疗糖尿病或肥胖症的药物组合物，其包含抑制二肽基肽酶-IV和其它抗糖尿病或抗肥胖剂作为活性成分的活性的化合物
公开(公告)号：US20110201624A1
公开(公告)日：2011-08-18
申请号：US13124150
申请日：2009-10-16
申请人： Chang Yell Shin , Song-Hyen Choi , Yu Na Chae , Eun Kyoung Yang , Gook Jun Ahn , Moon-Ho Son , Heung Jae Kim , Woo Young Kwak , Jong Pil Min , Tae Hyun Yoon , Soon Hoe Kim , Moohi Yoo
发明人： Chang Yell Shin , Song-Hyen Choi , Yu Na Chae , Eun Kyoung Yang , Gook Jun Ahn , Moon-Ho Son , Heung Jae Kim , Woo Young Kwak , Jong Pil Min , Tae Hyun Yoon , Soon Hoe Kim , Moohi Yoo
IPC分类号： A61K31/4965 , A61P3/04 , A61P3/10
CPC分类号： A61K45/06 , A61K9/0019 , A61K9/145 , A61K9/2059 , A61K31/155 , A61K31/4439 , A61K31/495 , A61K31/5377 , A61K31/64 , A61K31/7028 , A61K47/02 , Y02P20/582 , A61K2300/00
摘要： The present invention relates to a pharmaceutical composition for the prevention and treatment of diabetes or obesity comprising as active ingredients a compound which inhibits the activity of dipeptidyl peptidase-IV (DPP-IV), a pharmaceutically acceptable salt thereof, a hydrate thereof, or a solvate thereof, and one or more other antidiabetic or antiobesity agents. The pharmaceutical composition exhibits excellent glucose tolerance and may be useful in the prevention and treatment of diabetes, obesity, and the like by effectively inhibiting blood glucose levels and reducing fat mass.
摘要翻译：本发明涉及用于预防和治疗糖尿病或肥胖症的药物组合物，其包含抑制二肽基肽酶-IV（DPP-IV）的活性的化合物，其药学上可接受的盐，其水合物或其一种或多种其它抗糖尿病或抗肥胖剂。药物组合物表现出优异的葡萄糖耐量，可有效抑制血糖水平和降低脂肪量，可用于预防和治疗糖尿病，肥胖症等。

5. 发明授权

US08242159B2 1,3-dihydro-5-isobenzofurancarbonitrile derivatives and pharmaceutical composition thereof for the treatment of premature ejaculation 失效
标题翻译： 1,3-二氢-5-异苯并呋喃腈衍生物及其药物组合物，用于治疗早泄
公开(公告)号：US08242159B2
公开(公告)日：2012-08-14
申请号：US12739870
申请日：2008-10-31
申请人： Yeong Geon Lee , Soo-Jung Choi , Tae-Kyung Kang , Mi-Jeong Seo , Chang-Yong Shin , Kyung-Seok Lee , Gook-Jun Ahn , Seul-Min Choi , Yong-Duck Kim , Dong-Hwan Kim , Kyung-Koo Kang , Hyun-Joo Shim , Dong-Sung Kim , Byoung-Ok Ahn , Moo-Hi Yoo
发明人： Yeong Geon Lee , Soo-Jung Choi , Tae-Kyung Kang , Mi-Jeong Seo , Chang-Yong Shin , Kyung-Seok Lee , Gook-Jun Ahn , Seul-Min Choi , Yong-Duck Kim , Dong-Hwan Kim , Kyung-Koo Kang , Hyun-Joo Shim , Dong-Sung Kim , Byoung-Ok Ahn , Moo-Hi Yoo
IPC分类号： A61K31/415 , A61K31/4164 , A61K31/38 , A61K31/34 , C07D233/00 , C07D231/00 , C07D409/00 , C07D307/02
CPC分类号： C07D307/87 , C07D405/06 , C07D409/04 , C07D409/06
摘要： Disclosed herein are novel 1,3-dihydro-5-isobenzofurancarbonitrile derivatives represented by Formula 1, or pharmaceutically acceptable salts thereof. Also disclosed is a pharmaceutical composition for treating or preventing premature ejaculation including the compound. The 1,3-dihydro-5-isobenzofurancarbonitrile derivatives have a short half-life and inhibit the ejaculation process by selectively inhibiting serotonin reuptake via a serotonin reuptake transporter present in a presynaptic neuron. Thus, the compounds are useful in the treatment and prevention of premature ejaculation.
摘要翻译：本文公开了由式1表示的新的1,3-二氢-5-异苯并呋喃腈衍生物或其药学上可接受的盐。还公开了用于治疗或预防早泄的药物组合物，包括该化合物。 1,3-二氢-5-异苯并呋喃腈衍生物具有短的半衰期，并通过选择性地通过存在于突触前神经元中的5-羟色胺再摄取转运蛋白选择性抑制5-羟色胺再摄取来抑制射精过程。因此，这些化合物可用于治疗和预防早泄。

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