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公开(公告)号：US09956224B2
公开(公告)日：2018-05-01
申请号：US15394058
申请日：2016-12-29
Applicant: Dart Neuroscience (Cayman) Ltd.
Inventor： Bryan Branstetter , James Breitenbucher , Brian Dyck , Laurent Gomez , Andrew Richard Hudson , Tami Jo Marrone , Marco Peters , Troy Vickers , Michael Weinhouse
IPC: A61K31/519 , A61K31/5377 , A61K31/55 , A61K31/553 , A61K31/5386 , A61K31/551
Abstract: Described herein are compounds of Formula I and Formula II, methods of their synthesis, compositions comprising the compounds, and use of the compounds and compositions in treating numerous diseases and disorders, including cognitive deficits associated with CNS diseases and disorders.
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公开(公告)号：US09951065B2
公开(公告)日：2018-04-24
申请号：US15153527
申请日：2016-05-12
Applicant: Gilead Sciences, Inc.
Inventor： Mark J. Bartlett , Julian Andrew Codelli , Britton Kenneth Corkey , Jennifer Leigh Cosman , Kristyna Elbel , Jennifer Alissa Loyer-Drew , David Sperandio , Joshua Van Veldhuizen , Hai Yang , Suet Chung Yeung
IPC: C07D235/06 , C07D235/24 , C07D295/125 , C07D401/12 , C07D471/04 , A61K45/06 , C07D235/08 , A61K31/4184 , A61K31/5377 , A61K31/454 , A61K31/437 , A61K31/506 , A61K31/497 , A61K31/55 , A61K31/541 , A61K31/439 , C07D405/12 , C07D405/14 , C07D471/08 , A61K31/553 , C07D235/30 , C07D235/14 , C07D401/04 , C07D235/12 , A61K31/444 , A61K31/4545 , A61K31/538 , A61K31/5386 , A61K31/438 , C07D403/12 , A61K31/4439 , C07D413/12 , A61K31/496 , C07D487/04 , A61K31/4725 , C07D235/28 , C07D235/16 , C07D409/12
CPC classification number: C07D471/04 , A61K31/4184 , A61K31/437 , A61K31/438 , A61K31/439 , A61K31/4439 , A61K31/444 , A61K31/454 , A61K31/4545 , A61K31/4725 , A61K31/496 , A61K31/497 , A61K31/506 , A61K31/5377 , A61K31/538 , A61K31/5386 , A61K31/541 , A61K31/55 , A61K31/553 , A61K45/06 , C07D235/06 , C07D235/08 , C07D235/12 , C07D235/14 , C07D235/16 , C07D235/24 , C07D235/28 , C07D235/30 , C07D295/125 , C07D401/04 , C07D401/12 , C07D403/12 , C07D405/12 , C07D405/14 , C07D409/12 , C07D413/12 , C07D471/08 , C07D487/04
Abstract: The present disclosure provides indoleamine 2,3-dioxygenase 1 (IDO1) inhibitors of Formula I: or pharmaceutically acceptable salts thereof, in which X, L, n, m, R1, R2a, R2b, Rn, Rm, and Rt are as defined herein, as well as pharmaceutical compositions that include a compound of Formula I, or pharmaceutically acceptable salts thereof, and methods of using the same to treat conditions mediated by IDO1.
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73.发明申请
公开(公告)号：US20170312217A9
公开(公告)日：2017-11-02
申请号：US14664522
申请日：2015-03-20
Applicant: Hsin-Yung Lin
Inventor： Hsin-Yung Lin
IPC: A61K9/00 , A61K31/46 , A61K31/277 , A61K31/198 , A61K31/137 , A61K47/02 , A61K31/635 , A61K31/616 , A61K31/554 , A61K31/55 , A61K31/519 , A61K31/498 , A61K31/445 , A61K31/4422 , A61K31/4406 , A61K31/439 , A61K31/4365 , A61K31/4152 , A61K31/405 , A61K31/34 , A61K31/27 , A61K31/21 , A61K31/197 , A61K31/192 , A61K31/165 , A61K31/13 , A61K31/48 , A61K31/5386
CPC classification number: A61K9/0004 , A61K9/007 , A61K9/0073 , A61K9/0078 , A61K31/13 , A61K31/137 , A61K31/165 , A61K31/192 , A61K31/195 , A61K31/197 , A61K31/198 , A61K31/21 , A61K31/27 , A61K31/277 , A61K31/34 , A61K31/405 , A61K31/4152 , A61K31/4365 , A61K31/439 , A61K31/4406 , A61K31/4422 , A61K31/445 , A61K31/46 , A61K31/48 , A61K31/498 , A61K31/519 , A61K31/5386 , A61K31/55 , A61K31/554 , A61K31/616 , A61K31/635 , A61K47/02
Abstract: The present invention provides an inhalation-type pharmaceutical composition for gout and preparation method thereof, comprising a first gas and an atomized medicine. The first gas comprises hydrogen. The gas volume concentration of hydrogen in the inhalation-type pharmaceutical composition is between 2 to 96%. The atomized medicine is selected from a group comprising colchicine, allopurinol, probenecid, sulfinpyrazone, and any combination thereof. The inhalation-type pharmaceutical composition of the present invention can remove harmful radicals in the body of the patient through the use of hydrogen while also increases the absorption effect of the medicine for the patient by using an atomized medicine. At the same time, because the use of the small amount of the vaporized pharmaceutical liquid can indirectly reduce the side effects on the user.
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公开(公告)号：US20170275283A1
公开(公告)日：2017-09-28
申请号：US15505277
申请日：2015-10-26
Applicant: Alexander PASTERNAK , Fa-Xiang DING , Shuzhi DONG , Jinlong JIANG , Haifeng TANG , Xin GU , Reynalda K. DEJESUS , Jessica FRIE , Qinghong FU , Takao SUZUKI , Zhifa PU , Merck Sharp & Dohme Corp.
Inventor： Alexander Pasternak , Fa-Xiang Ding , Shuzhi Dong , Jinlong Jiang , Haifeng Tang , Xin Gu , Reynalda K. DeJesus , Jessica Frie , Qinghong Fu , Takao Suzuki , Zhifa Pu
IPC: C07D471/10 , C07D498/10 , A61K31/5386 , A61K45/06 , A61K31/435 , A61K31/537 , C07D498/20 , A61K31/553 , A61K31/499 , A61K31/55
CPC classification number: C07D471/10 , A61K31/401 , A61K31/41 , A61K31/4178 , A61K31/4184 , A61K31/435 , A61K31/4422 , A61K31/499 , A61K31/537 , A61K31/5386 , A61K31/55 , A61K31/553 , A61K45/06 , C07D487/10 , C07D498/10 , C07D498/20 , A61K2300/00
Abstract: The present invention provides compounds of Formula I and the pharmaceutically acceptable salts thereof, which are inhibitors of the ROMK (Kir1.1) channel. The compounds may be used as diuretic and/or natriuretic agents and for the therapy and prophylaxis of medical conditions including cardiovascular diseases such as hypertension, heart failure and chronic kidney disease and conditions associated with excessive salt and water retention.
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公开(公告)号：US09750719B2
公开(公告)日：2017-09-05
申请号：US14802982
申请日：2015-07-17
Applicant: CONVERGENCE PHARMACEUTICALS LIMITED
Inventor： Paul Beswick , Robert James Gleave , Shuji Hachisu , Sadie Vile , Nicolas Bertheleme , Simon E. Ward
IPC: A61K31/41 , A61K31/435 , A61K31/4439 , A61K31/5386 , C07D257/04 , C07D257/06 , C07D401/14 , C07D403/06 , C07D413/06 , C07D417/06 , C07D471/10 , C07D487/14 , C07D487/08 , C07D491/08 , C07D513/04 , C07D471/04 , C07D487/04 , A61K31/496 , A61K31/4985 , A61K31/5377 , A61K31/541 , A61K31/551
CPC classification number: A61K31/41 , A61K31/435 , A61K31/4439 , A61K31/496 , A61K31/4985 , A61K31/5377 , A61K31/5386 , A61K31/541 , A61K31/551 , C07D257/04 , C07D257/06 , C07D401/14 , C07D403/06 , C07D413/06 , C07D417/06 , C07D471/04 , C07D471/10 , C07D487/04 , C07D487/08 , C07D491/08 , C07D513/04
Abstract: The present invention relates to novel tetrazole compounds; to processes for their preparation; to pharmaceutical compositions containing the compounds; and to the use of the compounds in therapy to treat diseases for which blocking the Cav2.2 calcium channels is beneficial. Formula (I) wherein A is: (II) or (III) wherein A is
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公开(公告)号：US09725465B2
公开(公告)日：2017-08-08
申请号：US14473597
申请日：2014-08-29
Applicant: Ambit Biosciences Corporation
Inventor： Mark W. Holladay , Gang Liu , Martin W. Rowbottom
IPC: C07D498/08 , A61K31/4365 , A61K31/437 , A61K31/4375 , A61K31/47 , A61K31/498 , A61K31/4985 , A61K31/5377 , A61K31/5386 , A61K31/655 , A61K45/06 , C07D413/12 , C07D471/04 , C07D487/04 , C07D495/04 , C07D403/12 , C07D413/14 , C07D498/14
CPC classification number: C07D498/08 , A61K31/4365 , A61K31/437 , A61K31/4375 , A61K31/47 , A61K31/498 , A61K31/4985 , A61K31/5377 , A61K31/5386 , A61K31/655 , A61K45/06 , C07D403/12 , C07D413/12 , C07D413/14 , C07D471/04 , C07D487/04 , C07D495/04 , C07D498/14
Abstract: Biaryl acetamide compounds and compositions and their methods of use are provided for modulating the activity of class III receptor tyrosine kinases and for the treatment, prevention or amelioration of one or more symptoms of disease of disorder mediated by class III receptor tyrosine kinases.
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公开(公告)号：US20170217897A1
公开(公告)日：2017-08-03
申请号：US15500870
申请日：2015-08-03
Applicant: Zhigan JIANG , Jianhua XIA , Haiying HE , NOVARTIS AG
Inventor： Javier de Vicente FIDALGO , Haiying HE , Cheng HU , Zhigan JIANG , Xiaolin LI , Peichao LU , Wosenu MERGO , Daniel MUTNICK , Folkert RECK , Alexey RIVKIN , Colin Keith SKEPPER , Xiaojing Michael WANG , Jianhua XIA , Yongjin XU
IPC: C07D215/38 , A61K31/4709 , A61K31/496 , C07D401/14 , C07D413/14 , C07D419/14 , C07D405/14 , C07D471/04 , C07D498/10 , A61K31/5377 , A61K31/5386 , C07D487/10 , C07D471/10 , A61K45/06 , C07D401/04
CPC classification number: C07D215/38 , A61K31/4709 , A61K31/496 , A61K31/5377 , A61K31/5386 , A61K45/06 , C07D215/22 , C07D401/04 , C07D401/14 , C07D405/14 , C07D413/14 , C07D419/14 , C07D471/04 , C07D471/10 , C07D487/10 , C07D498/10 , Y02A50/406 , Y02A50/47 , Y02A50/473 , Y02A50/475 , Y02A50/478 , Y02A50/481
Abstract: This invention is in the field of medicinal chemistry and relates to compounds, and pharmaceutical compositions thereof, that inhibit bacterial gyrase. The compounds are useful as inhibitors of bacterial gyrase activity and bacterial infections, and have the structure of Formula (I) as further described herein. The invention further provides pharmaceutical compositions comprising a compound of Formula (I) and methods of using the compounds and compositions to treat bacterial infections.
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公开(公告)号：US09540393B2
公开(公告)日：2017-01-10
申请号：US14773028
申请日：2014-03-07
Applicant: VIIV HEALTHCARE UK (NO.5) LIMITED
Inventor： B. Narasimhulu Naidu , Manoj Patel , Stanley D'Andrea , Zhizhen Barbara Zheng
IPC: A61K31/535 , C07D498/22 , A61K31/519 , A61K31/5383 , C07D487/04 , C07D487/16 , C07D498/16 , A61K45/06 , A61K31/529 , A61K31/5386 , C07D471/22 , C07D498/18
CPC classification number: C07D498/22 , A61K31/519 , A61K31/529 , A61K31/5383 , A61K31/5386 , A61K45/06 , C07D471/22 , C07D487/04 , C07D487/16 , C07D498/16 , C07D498/18 , A61K2300/00
Abstract: The disclosure generally relates to compounds of formula (I), including compositions and methods for treating human immunodeficiency virus (HIV) infection. The disclosure provides novel inhibitors of HIV, pharmaceutical compositions containing such compounds, and methods for using these compounds in the treatment of HIV infection.
Abstract translation: 本发明一般涉及式（I）化合物，包括用于治疗人类免疫缺陷病毒（HIV）感染的组合物和方法。 本公开提供了HIV的新型抑制剂，含有这些化合物的药物组合物，以及使用这些化合物治疗HIV感染的方法。
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公开(公告)号：US20160332989A1
公开(公告)日：2016-11-17
申请号：US15108903
申请日：2014-12-30
Applicant: XUANZHU PHARMA CO., LTD.
IPC: C07D401/14 , A61K31/506 , C07D471/10 , C07D487/10 , C07D487/04 , C07D405/14 , A61K31/5383 , C07D498/08 , A61K31/5386 , C07D471/08 , A61K31/5377 , A61K45/06 , C07D498/04
CPC classification number: C07D401/14 , A61K31/506 , A61K31/5377 , A61K31/5383 , A61K31/5386 , A61K45/06 , C07D401/04 , C07D405/14 , C07D471/04 , C07D471/08 , C07D471/10 , C07D487/04 , C07D487/08 , C07D487/10 , C07D498/04 , C07D498/08 , A61K2300/00
Abstract: The invention relates to a CDK4/6 kinase inhibitor, or a pharmaceutically acceptable salt, ester, or solvate thereof, or their isomers; a pharmaceutical formulation, pharmaceutical composition and kit comprising said CDK4/6 kinase inhibitor, or a pharmaceutically acceptable salt, ester, or solvate thereof, or their isomers, and use of said CDK4/6 kinase inhibitor, or a pharmaceutically acceptable salt, ester, or solvate thereof, or their isomers. For example, the compounds of the invention are useful for reducing or inhibiting the activity of CDK4/6 kinase in a cell, and/or treating and/or preventing a cancer-related disease mediated by CDK4/6 kinase.
Abstract translation: 本发明涉及CDK4 / 6激酶抑制剂或其药学上可接受的盐，酯或溶剂合物或其异构体; 药物制剂，包含所述CDK4 / 6激酶抑制剂或其药学上可接受的盐，酯或溶剂合物或其异构体的药物组合物和试剂盒，以及所述CDK4 / 6激酶抑制剂或其药学上可接受的盐， 或它们的异构体。 例如，本发明的化合物可用于减少或抑制细胞中CDK4 / 6激酶的活性，和/或治疗和/或预防由CDK4 / 6激酶介导的癌症相关疾病。
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公开(公告)号：US09458158B2
公开(公告)日：2016-10-04
申请号：US14836326
申请日：2015-08-26
Applicant: ASTEX THERAPEUTICS LIMITED
Inventor： Ildiko Maria Buck , Gianni Chessari , Steven Howard , David Charles Rees , Alison Jo-Anne Woolford
IPC: C07D471/04 , C07D498/04 , A61K31/519 , A61K31/4985 , A61K31/437 , A61K31/5386 , A61K45/06 , A61K31/5383 , C07D498/10
CPC classification number: C07D471/04 , A61K31/437 , A61K31/4985 , A61K31/519 , A61K31/5383 , A61K31/5386 , A61K45/06 , C07D498/04 , C07D498/10 , A61K2300/00
Abstract: The invention relates to bicyclic heterocycle compounds of formula (I): or tautomeric or stereochemically isomeric forms, N-oxides, pharmaceutically acceptable salts or the solvates thereof; wherein R1, R2, R3, A, W, U and V are as defined herein; to pharmaceutical compositions comprising said compounds and to the use of said compounds in the treatment of diseases, e.g. cancer.
