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公开(公告)号：US10017506B2
公开(公告)日：2018-07-10
申请号：US15296601
申请日：2016-10-18
Applicant: BIOGEN MA INC.
Inventor： Kevin M. Guckian , Gnanasambandam Kumaravel , Bin Ma , Sha Mi , Hairuo Peng , Zhaohui Shao , Lihong Sun , Arthur G. Taveras , Deping Wang , Zhili Xin , Lei Zhang
IPC: A61K31/015 , A61K31/4375 , A61K31/44 , C07D451/02 , C07D217/22 , A61K31/472 , A61K45/06 , A61K31/4725 , C07D401/06
CPC classification number: C07D451/02 , A61K31/136 , A61K31/196 , A61K31/439 , A61K31/445 , A61K31/46 , A61K31/472 , A61K31/4725 , A61K31/5375 , A61K31/55 , A61K45/06 , C07B2200/07 , C07C217/22 , C07C229/46 , C07C229/48 , C07C255/59 , C07C2601/04 , C07C2601/08 , C07C2601/14 , C07C2602/42 , C07D209/52 , C07D211/34 , C07D211/62 , C07D217/22 , C07D221/22 , C07D223/06 , C07D295/096 , C07D401/06 , C07D471/08 , Y02A50/401
Abstract: Disclosed are bicyclic aryl compounds of formula (I), that can modulate the activity of the autotaxin (ATX) enzyme. This invention further relates to compounds that are ATX inhibitors, and methods of making and using such compounds in the treatment of demyelination due to injury or disease, as well as for treating proliferative disorders such as cancer.
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公开(公告)号：US20180118680A1
公开(公告)日：2018-05-03
申请号：US15851322
申请日：2017-12-21
Applicant: Genentech, Inc.
Inventor： Huifen Chen , Yanyan Chu , Steven Do , Anthony Estrada , Baihua Hu , Aleksandr Kolesnikov , Xingyu Lin , Joseph P. Lyssikatos , Daniel Shore , Vishal Verma , Lan Wang , Guosheng Wu , Po-wai Yuen
IPC: C07D207/48 , C07D403/14 , C07D417/12 , C07D403/12 , C07D451/02 , C07D405/14 , C07D401/14 , C07D491/048 , C07D401/12
Abstract: The invention is concerned with the compounds of formula I or II: and salts thereof. In addition, the present invention relates to methods of manufacturing and methods of using the compounds of formula I or II as well as pharmaceutical compositions containing such compounds. The compounds may be useful in treating diseases and conditions mediated by TRPA1, such as pain.
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公开(公告)号：US09908899B2
公开(公告)日：2018-03-06
申请号：US15337354
申请日：2016-10-28
Applicant: BIOMARIN PHARMACEUTICAL INC.
Inventor： Vincent Jacques , James R. Rusche , Norton P. Peet , Jasbir Singh
IPC: A61K31/397 , A61K31/46 , A61K31/4427 , A61K31/445 , A61K31/337 , C07D513/04 , C07D263/32 , C07D471/04 , C07D231/12 , C07D261/08 , C07D211/70 , C07D403/10 , C07D403/06 , C07D211/78 , C07D451/02 , C07D305/10 , C07D205/06 , C07D401/06 , C07D471/08 , C07D277/34 , C07D277/30
CPC classification number: C07D513/04 , C07D205/06 , C07D211/70 , C07D211/78 , C07D231/12 , C07D261/08 , C07D263/32 , C07D277/30 , C07D277/34 , C07D305/10 , C07D401/06 , C07D403/06 , C07D403/10 , C07D451/02 , C07D471/04 , C07D471/08
Abstract: The compounds provided herein are phenyl analine amides and are useful for inhibiting histone deacteylase (“HDAC”) enzymes, such as HDAC1, HDAC2, and HDAC3.
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公开(公告)号：US20170304305A1
公开(公告)日：2017-10-26
申请号：US15645300
申请日：2017-07-10
Applicant: XUANZHU PHARMA CO., LTD.
Inventor： Yanyan DONG , Shih CHENGKON
IPC: A61K31/517 , A61K45/06 , C07D491/08 , C07D487/10 , C07D487/08 , C07D487/04 , C07D471/10 , C07D471/08 , C07D471/04 , C07D451/06 , C07D451/02 , C07D413/14 , C07D409/12 , C07D405/12 , C07D403/14 , C07D403/12 , C07D401/12 , C07D239/94 , C07D239/86 , C07D491/107 , C07D493/08
CPC classification number: A61K31/517 , A61K31/5377 , A61K45/06 , C07D239/86 , C07D239/94 , C07D401/12 , C07D403/12 , C07D403/14 , C07D405/12 , C07D409/12 , C07D413/14 , C07D451/02 , C07D451/06 , C07D471/04 , C07D471/08 , C07D471/10 , C07D487/04 , C07D487/08 , C07D487/10 , C07D491/08 , C07D491/107 , C07D493/08
Abstract: The invention relates to quinazoline derivatives substituted by aniline which are represented by the below formula (I), pharmaceutical acceptable salts and stereoisomer thereof, wherein these groups of R1, R2, R3, R4, R5, R6, L and n have the meanings given in the specification. The invention also relates to preparation methods, pharmaceutical compositions, pharmaceutical preparation and the use for preparation of medicine of treating excessive hyperplasia and chronic obstructive pulmonary disease and uses for treating excessive hyperplasia and chronic obstructive pulmonary disease thereof.
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公开(公告)号：US09757483B2
公开(公告)日：2017-09-12
申请号：US14517276
申请日：2014-10-17
Applicant: Alseres Pharmaceuticals, Inc.
Inventor： Chris Sterzinger , Cara Ferreira , David Leyh , Richard Thorn
IPC: A61K51/00 , C07D451/00 , A61K51/04 , C07D451/02 , G21H5/02
CPC classification number: A61K51/0455 , A61K51/0448 , C07D451/02 , G21H5/02
Abstract: A diagnostic formulation is provided comprising a tropane having a radioactive concentration of at least 1.6 mCi/mL at least about 51 hours post creation. The diagnostic formulation optionally comprises a radiolabeled dopamine transporter (DAT) ligand useful in the diagnosis of Parkinson's disease (PS). One example of a radiolabeled dopamine transporter (DAT) ligand example is [123I]-2β-carbomethoxy-3β-(4-flurophenyl)-N-(3-iodo-E-allyl) nortropane.
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公开(公告)号：US20170233385A1
公开(公告)日：2017-08-17
申请号：US15123014
申请日：2015-02-27
Applicant: SHANGHAI HAIYAN PHARMACEUTICAL TECHNOLOGY CO., LTD. , YANGTZE RIVER PHARMACEUTICAL GROUP CO., LTD.
Inventor： Haiying HE , Songliang WU , Yang ZHANG , Biao MA , Yuan CHEN , Yuhe WANG , Shuhui CHEN , Qiang LV , Jiong LAN , Xing LIU
IPC: C07D451/02
CPC classification number: C07D451/02
Abstract: The present invention discloses a series of piperidine derivatives as orexin receptor antagonists and compositions thereof, and relates to the application thereof in preparing medications for the treatment of insomnia, chronic obstructive pulmonary disease, obstructive sleep apnea, hypersomnia, anxiety, obsessive-compulsive disorder, panic attack, nicotine addiction, or binge eating disorder.
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公开(公告)号：US20170137439A1
公开(公告)日：2017-05-18
申请号：US15406994
申请日：2017-01-16
Applicant: Ironwood Pharmaceuticals, Inc.
Inventor： Takashi NAKAI , Joel MOORE , Nicholas Robert PERL , Rajesh R. IYENGAR , Ara MERMERIAN , G-Yoon Jamie IM , Thomas Wai-Ho LEE , Colleen HUDSON , Glen Robert RENNIE , James JIA , Paul Allan RENHOWE , Timothy Claude BARDEN , Xiang Y. YU , James Edward SHEPPECK , Karthik IYER , Joon JUNG , George Todd MILNE , Kimberly Kafadar LONG , Mark G. CURRIE
IPC: C07D498/04 , A61K31/506 , A61K31/5377 , C07D487/04 , C07D491/107 , C07D471/10 , C07D487/10 , C07D417/14 , A61K31/541 , A61K31/55 , C07D451/02 , C07D471/04 , C07D401/14 , C07D403/04 , A61K31/517 , A61K31/519 , C07D413/14
CPC classification number: A61K31/506 , A61K31/517 , A61K31/519 , A61K31/5377 , A61K31/541 , A61K31/55 , A61K45/06 , C07D401/14 , C07D403/04 , C07D413/14 , C07D417/14 , C07D451/02 , C07D471/04 , C07D471/08 , C07D471/10 , C07D487/04 , C07D487/10 , C07D491/107 , C07D495/04 , C07D498/04 , Y02A50/423
Abstract: Compounds of Formulae I′ and I are described, which are useful as stimulators of sGC, particularly NO-independent, heme-dependent stimulators. These compounds are also useful for treating, preventing or managing various disorders that are herein disclosed.
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公开(公告)号：US20170081307A1
公开(公告)日：2017-03-23
申请号：US15267606
申请日：2016-09-16
Applicant: Merck Patent GmbH
Inventor： Catherine JORAND-LEBRUN , Ruoxi LAN , Austin CHEN , Ryan C. CLARK
IPC: C07D401/04 , C07D413/04 , C07D451/02 , C07D403/04 , C07D405/04
CPC classification number: C07D401/04 , A61K31/4184 , A61K31/4439 , A61K31/506 , C07D235/30 , C07D403/04 , C07D405/04 , C07D413/04 , C07D451/02 , C07D471/08
Abstract: The present invention relates to compounds of Formula I and pharmaceutically acceptable compositions thereof, useful as IRAK inhibitors.
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公开(公告)号：US20160376264A1
公开(公告)日：2016-12-29
申请号：US15139592
申请日：2016-04-27
Applicant: THERAVANCE BIOPHARMA R&D IP, LLC
Inventor： DANIEL MARQUESS , PAUL R. FATHEREE , S. DEREK TURNER , DANIEL D. LONG , SEOK-KI CHOI , ADAM A. GOLDBLUM
IPC: C07D451/02
CPC classification number: C07D451/02 , C07D451/04
Abstract: The invention provides novel quinolinone-carboxamide 5-HT4 receptor agonist compounds. The invention also provides pharmaceutical compositions comprising such compounds, methods of using such compounds to treat diseases associated with 5-HT4 receptor activity, and processes and intermediates useful for preparing such compounds.
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公开(公告)号：US09492440B2
公开(公告)日：2016-11-15
申请号：US13557681
申请日：2012-07-25
Applicant: Rudolf Mueller , Leslie Street
Inventor： Rudolf Mueller , Leslie Street
IPC: A61K31/535 , C07D498/02 , C07D265/00 , A61K31/519 , A61K31/53 , C07D209/52 , A61K31/46 , C07D451/04 , C07D451/06 , C07D453/06 , C07D471/08 , C07D491/08 , A61K31/4245 , A61K31/439 , A61K45/06 , C07D451/02 , C07D487/08
CPC classification number: A61K31/46 , A61K31/4245 , A61K31/439 , A61K31/519 , A61K31/53 , A61K45/06 , C07D209/52 , C07D451/02 , C07D451/04 , C07D451/06 , C07D453/06 , C07D471/08 , C07D487/08 , C07D491/08
Abstract: This invention relates to bicyclic amide compounds, pharmaceutical compositions and methods for use in the prevention and treatment of a variety of conditions and/or disease states including cerebral insufficiency, through the enhancement of receptor functioning in synapses in brain networks responsible for basic and higher order behaviors as defined herein. These brain networks, which are involved in regulation of breathing, and cognitive abilities related to memory impairment, such as is observed in a variety of dementias, in imbalances in neuronal activity between different brain regions, as is suggested in disorders such as Parkinson's disease, schizophrenia, respiratory depression, sleep apneas, attention deficit hyperactivity disorder and affective or mood disorders, and in other disorders wherein a deficiency in neurotrophic factors is implicated, as well as other disorders as described herein.
Abstract translation: 本发明涉及双环酰胺化合物，药物组合物和用于预防和治疗各种病症和/或疾病状态（包括脑功能不全）的方法，其通过增强负责基本和高等级的脑网络中的突触中的受体功能 行为如本文所定义。 涉及呼吸调节的这些脑网络，以及与记忆障碍有关的认知能力，例如在各种痴呆症中观察到的，在不同脑区域之间的神经元活动不均衡中，如在帕金森病， 精神分裂症，呼吸抑制，睡眠呼吸暂停，注意缺陷多动障碍和情感或情绪障碍，以及涉及神经营养因子缺乏的其它疾病以及本文所述的其它病症。
