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1. 发明授权

US09309273B2 Metalloenzyme inhibitor compounds 有权
公开(公告)号：US09309273B2
公开(公告)日：2016-04-12
申请号：US14364276
申请日：2012-12-10
申请人： Viamet Pharmaceuticals, Inc.
发明人： William J. Hoekstra , Christopher M. Yates
IPC分类号： A61K31/675 , A61K31/535 , A61K31/50 , A61K31/501 , A61K31/4965 , A61K31/445 , A61K31/44 , A61K31/41 , C07D413/00 , C07D401/00 , C07D403/00 , C07D405/00 , C07D409/00 , C07D411/00 , C07D417/00 , C07D419/00 , C07F9/06 , C07F9/28 , C07D211/68 , C07D211/80 , C07D213/02 , C07D421/00 , C07D257/00 , A61K31/4439 , C07D401/06 , C07D409/14 , C07D401/14 , C07D405/14 , C07D413/14 , C07D403/06 , C07D403/14 , C07D409/06 , C07D417/14 , A01N43/713 , A01N43/84 , A01N57/16
CPC分类号： C07D401/06 , A01N43/713 , A01N43/84 , A01N57/16 , A61K31/4439 , C07D401/14 , C07D403/06 , C07D403/14 , C07D405/14 , C07D409/06 , C07D409/14 , C07D413/14 , C07D417/14 , C07F9/06 , C07F9/65583 , Y02A50/409 , Y02A50/411 , Y02A50/414 , Y02A50/415
摘要： The instant invention describes compounds having metalloenzyme modulating activity, and methods of treating diseases, disorders or symptoms thereof mediated by such metalloenzymes.

2. 发明授权

US09289430B2 Compounds and methods for inhibiting phosphate transport 有权
公开(公告)号：US09289430B2
公开(公告)日：2016-03-22
申请号：US14337028
申请日：2014-07-21
申请人： Ardelyx, Inc.
发明人： Jason G. Lewis , Jeffrey W. Jacobs , Nicholas Reich , Michael R. Leadbetter , Noah Bell , Han-Ting Chang , Tao Chen , Marc Navre , Dominique Charmot , Christopher Carreras , Eric Labonte
IPC分类号： A61K31/4439 , A61K31/454 , C07D401/12 , A61K31/5377 , A61K31/4965 , A61K31/505 , A61K45/06 , C07D211/68 , C07D231/40 , C07D233/88 , C07D255/02 , C07D277/46 , C07D285/135 , A61K31/415 , A61K31/4545 , A61K31/59 , C07D249/14
CPC分类号： A61K31/5377 , A61K31/415 , A61K31/454 , A61K31/4545 , A61K31/4965 , A61K31/505 , A61K31/59 , A61K45/06 , C07D211/68 , C07D231/40 , C07D233/88 , C07D249/14 , C07D255/02 , C07D277/46 , C07D285/135 , C07D401/12 , A61K2300/00
摘要： Compounds having activity as phosphate transport inhibitors, more specifically, inhibitors of intestinal apical membrane Na/phosphate co-transport, are disclosed. The compounds have the following structure (I): including stereoisomers, pharmaceutically acceptable salts and prodrugs thereof, wherein X, Y and A are as defined herein. Methods associated with preparation and use of such compounds, as well as pharmaceutical compositions comprising such compounds, are also disclosed.

3. 发明授权

US09163013B2 Use of 1H-indazole-3-carboxamide compounds as glycogen synthase kinase 3 beta inhibitors 有权
标题翻译：使用1H-吲唑-3-甲酰胺化合物作为糖原合酶激酶3β抑制剂
公开(公告)号：US09163013B2
公开(公告)日：2015-10-20
申请号：US14373393
申请日：2013-02-08
申请人： AZIENDE CHIMICHE RIUNITE ANGELINI FRANCESCO A.C.R.A.F. S.P.A.
发明人： Maria Alessandra Alisi , Nicola Cazzolla , Barbara Garofalo , Guido Furlotti , Gabriele Magaro′ , Rosella Ombrato , Francesca Mancini
IPC分类号： A61K31/5377 , A61K31/454 , C07D413/14 , C07D211/68 , C07D417/14 , C07D401/14 , C07D405/14 , C07D401/12
CPC分类号： A61K31/454 , A61K31/4545 , A61K31/5377 , C07D401/12 , C07D401/14 , C07D405/14 , C07D413/14 , C07D417/14
摘要： 1H-indazole-3-carboxamide compounds as glycogen synthase kinase 3 beta inhibitors. The present invention relates to the 1H-indazole-3-carboxamide compounds for use as glycogen synthase kinase 3 beta (GSK-3β) inhibitors and to their use in the treatment of GSK-3β-related disorders such as, for example, (i) insulin-resistance disorders; (ii) neurodegenerative diseases; (iii) mood disorders; (iv) schizophrenic disorders; (v) cancerous disorders; (vi) inflammation, (vii) substance abuse disorders; and (viii) epilepsies.
摘要翻译： 1H-吲唑-3-甲酰胺化合物作为糖原合酶激酶3β抑制剂。本发明涉及用作糖原合酶激酶3β（GSK-3＆bgr））抑制剂的1H-吲唑-3-甲酰胺化合物，以及它们在治疗GSK-3和相关病症中的用途，例如，（i）胰岛素抵抗障碍; （ii）神经变性疾病; （iii）情绪障碍; （四）精神分裂症; （v）癌症; （vi）炎症，（vii）物质滥用障碍; 和（viii）癫痫。

4. 发明授权

US09156801B2 2-substituted oleanolic acid derivative, method preparing for same, and application thereof 有权
标题翻译： 2-取代的齐墩果酸衍生物，其制备方法及其应用
公开(公告)号：US09156801B2
公开(公告)日：2015-10-13
申请号：US14362017
申请日：2012-11-30
申请人： HANGZHOU BENSHENG PHARMACEUTICAL CO., LTD.
发明人： Rongzhen Xu , Frank Rong , Hongxi Lai , Fuwen Xie
IPC分类号： A61K31/21 , A61K31/44 , A61K31/497 , A61K31/535 , C07C69/74 , C07D211/68 , C07D265/30 , C07D241/04 , C07D487/00 , C07D295/13 , C07J63/00 , C07C235/84 , C07D213/40
CPC分类号： C07D295/13 , C07C235/84 , C07D213/40 , C07J63/00 , C07J63/008
摘要： The present invention belongs to the field of natural medicine and pharmaceutical chemistry, and specifically relates to novel 2-substituted oleanolic acid derivatives of formula (I) or a pharmaceutically acceptable salt thereof, to a process for the preparation of these compounds, compositions containing such compounds and their use in preparing antineoplastic medicaments.
摘要翻译：本发明属于天然药物和药物化学领域，具体涉及式（I）的新型2-取代齐墩果酸衍生物或其药学上可接受的盐，涉及制备这些化合物的方法，含有这些化合物的组合物化合物及其在制备抗肿瘤药物中的应用。

5. 发明授权

US08940898B2 Piperidinyl alkyne orexin receptor antagonists 有权
标题翻译：哌啶基炔炔食欲素受体拮抗剂
公开(公告)号：US08940898B2
公开(公告)日：2015-01-27
申请号：US14354454
申请日：2012-10-19
申请人： Scott D. Kuduk , Jason W. Skudlarek
发明人： Scott D. Kuduk , Jason W. Skudlarek
IPC分类号： C07D211/68 , A61K31/47 , C07D401/10 , C07D401/12 , C07D401/14 , C07D417/06 , C07D417/14
CPC分类号： C07D401/10 , C07D401/12 , C07D401/14 , C07D417/06 , C07D417/14
摘要： The present invention is directed to piperidinyl alkyne compounds which are antagonists of orexin receptors. The present invention is also directed to uses of the piperidinyl alkyne compounds described herein in the treatment or prevention of neurological and psychiatric disorders and diseases in which orexin receptors are involved. The present invention is also directed to pharmaceutical compositions comprising these compounds. The present invention is also directed to uses of these pharmaceutical compositions in the prevention or treatment of such diseases in which orexin receptors are involved.
摘要翻译：本发明涉及作为食欲素受体拮抗剂的哌啶基炔化合物。本发明还涉及本文所述的哌啶基炔化合物在治疗或预防涉及食欲素受体的神经和精神病症和疾病中的用途。本发明还涉及包含这些化合物的药物组合物。本发明还涉及这些药物组合物在预防或治疗涉及食欲素受体的疾病中的用途。

6. 发明授权

US08921563B2 1-[(4-hydroxypiperidin-4-yl)methyl]pyridin-2(1H)-one derivatives, preparation methods and uses thereof 有权
标题翻译： 1 - [（4-羟基哌啶-4-基）甲基]吡啶-2（1H） - 酮衍生物，其制备方法和用途
公开(公告)号：US08921563B2
公开(公告)日：2014-12-30
申请号：US13697857
申请日：2011-04-08
申请人： Yunfeng Li , Rifang Yang , Youzhi Zhang , Yongzhen Li , Zengliang Jin , Peng Li , Li Yuan , Liuhong Yun , Nan Zhao , Cheng Zhang , Xiaodan Xu , Rusheng Zhao , Hongxia Chen , Rui Xue , Juanjuan Qin , Zhenzhen Wang , Jiazhi Yao
发明人： Yunfeng Li , Rifang Yang , Youzhi Zhang , Yongzhen Li , Zengliang Jin , Peng Li , Li Yuan , Liuhong Yun , Nan Zhao , Cheng Zhang , Xiaodan Xu , Rusheng Zhao , Hongxia Chen , Rui Xue , Juanjuan Qin , Zhenzhen Wang , Jiazhi Yao
IPC分类号： A61K31/445 , A61K31/505 , C07D211/68 , C07D239/02 , C07D401/06
CPC分类号： C07D401/06
摘要： Provided are N-[(4-hydroxypiperidin-4-yl)methyl]pyridin-2(1H)-one derivatives represented by formula I, stereoisomers, pharmaceutically acceptable salts or solvates thereof. The above compounds have the dual activities of 5-hydroxytryptamine 1A receptor ligand and selective serotonin reuptake inhibitor. The preparation methods of the above compounds, the uses of these compounds for the prevention or treatment of nervous system diseases related to 5-hydroxytryptamine system dysfunction and the pharmaceutical compositions containing these compounds are also provided.
摘要翻译：提供由式I表示的N - [（4-羟基哌啶-4-基）甲基]吡啶-2（1H） - 酮衍生物，其立体异构体，药学上可接受的盐或溶剂合物。上述化合物具有5-羟色胺1A受体配体和选择性5-羟色胺再摄取抑制剂的双重活性。还提供了上述化合物的制备方法，这些化合物用于预防或治疗与5-羟色胺系统功能障碍有关的神经系统疾病的用途和含有这些化合物的药物组合物。

7. 发明授权

US08809540B2 N-adamantyl benzamides as inhibitors of 11-beta-hydroxysteroid dehydrogenase 有权
标题翻译： N-金刚烷基苯甲酰胺作为11-β-羟基类固醇脱氢酶的抑制剂
公开(公告)号：US08809540B2
公开(公告)日：2014-08-19
申请号：US13739408
申请日：2013-01-11
申请人： High Point Pharmaceuticals, LLC
发明人： Soren Ebdrup
IPC分类号： A61K31/44 , C07D211/68
CPC分类号： C07D471/08 , C07C235/54 , C07C2601/14 , C07C2603/74 , C07D207/26 , C07D207/27 , C07D211/22 , C07D211/60 , C07D211/96 , C07D213/30 , C07D213/61 , C07D213/65 , C07D295/088 , C07D295/215 , C07D295/26 , C07D309/06 , C07D309/12 , C07D451/06
摘要： Novel substituted benzamide based inhibitors, their use in therapy, pharmaceutical compositions comprising the compounds, the use of said compounds in the manufacture of medicaments, and therapeutic methods comprising the administration of said compounds are described. The present compounds modulate the activity of 11β-hydroxysteroid dehydrogenase type 1 (11βHSD1) and are accordingly useful in the treatment of diseases in which such a modulation is beneficial, such as the metabolic syndrome.
摘要翻译：描述了新型取代的苯甲酰胺基抑制剂，它们在治疗中的用途，包含该化合物的药物组合物，所述化合物在制备药物中的用途，以及包括施用所述化合物的治疗方法。本发明化合物调节11β-羟基类固醇脱氢酶1（11＆bgr，HSD1）的活性，因此可用于治疗这种调节有益的疾病，如代谢综合征。

8. 发明授权

US08598206B2 Trypsin-like serine protease inhibitors, and their preparation and use 有权
标题翻译：胰蛋白酶样丝氨酸蛋白酶抑制剂及其制备和用途
公开(公告)号：US08598206B2
公开(公告)日：2013-12-03
申请号：US13015734
申请日：2011-01-28
申请人： Peter Herold , Mohammed Daghish , Stjepan Jelakovic , Friedrich-Alexander Ludwig , Claudia Reichelt , Alexander Schulze , Andrea Schweinitz
发明人： Peter Herold , Mohammed Daghish , Stjepan Jelakovic , Friedrich-Alexander Ludwig , Claudia Reichelt , Alexander Schulze , Andrea Schweinitz
IPC分类号： A01N43/40 , A61K31/445 , C07D257/00 , C07D211/68 , C07D211/80 , C07D213/02 , C07D211/32 , C07D405/00 , C07D409/00 , C07D411/00 , C07D413/00 , C07D417/00 , C07D419/00 , C07D421/00
CPC分类号： C07K5/06139 , A61K31/445 , A61K38/00 , C07D211/34 , C07D401/12 , C07D413/12 , C07K5/06078
摘要： The invention provides compounds that are effective as inhibitors of human plasmin and plasma kallikrein, and that are useful for the prevention of blood loss and as components of fibrin adhesives. The invention further provides methods of making and using the compounds.
摘要翻译：本发明提供了作为人类纤溶酶和血浆激肽释放酶抑制剂有效的化合物，其可用于预防失血和作为纤维蛋白粘合剂的组分。本发明还提供了制备和使用该化合物的方法。

9. 发明授权

US08455652B2 Inhibitors for the soluble epoxide hydrolase 有权
公开(公告)号：US08455652B2
公开(公告)日：2013-06-04
申请号：US12396391
申请日：2009-03-02
申请人： Bruce D. Hammock , In-Hae Kim , Christophe Morisseau , Takaho Watanabe , John W. Newman
发明人： Bruce D. Hammock , In-Hae Kim , Christophe Morisseau , Takaho Watanabe , John W. Newman
IPC分类号： C07D211/68 , C07D211/80
CPC分类号： C07C275/26 , C07C275/30 , C07C275/42 , C07C311/04 , C07C311/05 , C07C311/51 , C07C323/59 , C07C2601/02 , C07C2601/14 , C07C2603/74 , C07D207/16 , C07D233/24 , C07D233/64
摘要： Inhibitors of the soluble epoxide hydrolase (sEH) are provided that incorporate multiple pharmacophores and are useful in the treatment of diseases.

10. 发明授权

US08410276B2 Nitrogenous heterocyclic derivative and medicine containing the same as an active ingredient 失效
标题翻译：含氮杂环衍生物和含有与活性成分相同的药物
公开(公告)号：US08410276B2
公开(公告)日：2013-04-02
申请号：US13016849
申请日：2011-01-28
申请人： Yoshikazu Takaoka , Shiro Shibayama , Rena Nishizawa
发明人： Yoshikazu Takaoka , Shiro Shibayama , Rena Nishizawa
IPC分类号： C07D211/68 , A61K31/445
CPC分类号： C07D413/12 , A61K31/00 , C07D211/58 , C07D231/12 , C07D401/06 , C07D401/12 , C07D401/14 , C07D409/14
摘要： A compound represented by formula (I), a salt thereof, an N-oxide thereof, a solvate thereof or a prodrug thereof: (wherein each symbol is as defined in the description.) The compounds represented by formula (I) has the antagonistic activity against CCR5, so they are useful in preventing and/or treating CCR5-related diseases, for example, various inflammatory diseases (asthma, nephritis, nephropathy, hepatitis, arthritis, rheumatoid arthritis, rhinitis, conjunctivitis, inflammatory bowel disease such as ulcerative colitis, etc.), immunological diseases (autoimmune diseases, rejection in organ transplantation (rejection of graft of solid organ, rejection of graft of pancreatic islet cells in therapy for diabetes, graft-versus-host disease, etc.), immunosuppression, psoriasis, multiple sclerosis, etc.), infectious diseases (infection with human immunodeficiency virus, acquired immunodeficiency syndrome, infection with RSV, etc.), allergic diseases (atopic dermatitis, urticaria, allergic bronchopulmonary aspergillosis, allergic eosinophilic gastroenteritis, etc.), cardiovascular diseases (arteriosclerosis, ischemic reperfusion injury, etc.), acute respiratory distress syndrome, shock accompanying bacterial infection, diabetes, cancer metastasis and so on.
摘要翻译：由式（I）表示的化合物，其盐，其N-氧化物，其溶剂合物或其前药：（其中各符号如说明书中所定义）。式（I）表示的化合物具有拮抗作用因此它们可用于预防和/或治疗CCR5相关疾病，例如各种炎性疾病（哮喘，肾炎，肾病，肝炎，关节炎，类风湿关节炎，鼻炎，结膜炎，炎性肠病如溃疡性结肠炎）等等），免疫疾病（自身免疫性疾病，器官移植排斥反应（实体器官移植排斥反应，胰岛细胞移植对糖尿病的治疗排斥反应，移植物抗宿主病等），免疫抑制，牛皮癣，多发性硬化症等），感染性疾病（人类免疫缺陷病毒感染，获得性免疫缺陷综合征，RSV感染等），过敏性疾病（特应性皮炎，荨麻疹，过敏性急性呼吸窘迫综合征，伴随细菌感染的休克，糖尿病，癌症转移等），心血管疾病（动脉硬化，缺血再灌注损伤等）。

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