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公开(公告)号:US20190119225A1
公开(公告)日:2019-04-25
申请号:US16230634
申请日:2018-12-21
IPC分类号: C07D263/46 , C07D213/70 , A61P27/02 , C07D239/34 , A61K31/421 , C07D213/65 , C07D263/38 , A61K31/415 , C07D231/22 , C07D231/12 , A61K31/505 , A61K31/4418
摘要: Provided is a heterocyclic compound having a superior RBP4-lowering action and useful as a medicament for the prophylaxis or treatment of a disease or symptom mediated by an increase in RBP4 or retinol supplied by RBP4.A compound represented by the formula (I): wherein each symbol is as defined in the Description, or a salt thereof has a superior RBP4-lowering action, and is useful as a medicament for the prophylaxis or treatment of a disease or symptom mediated by an increase in RBP4 or retinol supplied by RBP4.
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公开(公告)号:US10226426B2
公开(公告)日:2019-03-12
申请号:US15554688
申请日:2016-03-01
IPC分类号: A61K9/14 , A61K47/16 , A61K47/18 , A61K47/20 , A61K47/22 , A61K47/32 , A61K47/34 , A61K9/10 , A61K47/38 , A61K31/341 , A61K31/405 , A61K31/55 , A61K31/522 , A61K9/16
摘要: The present invention provides a method of producing a suspension containing a nano-cocrystal having an average particle size of not more than 300 nm, a polymer having a number average molecular weight of not less than 3,000, a surfactant having a number average molecular weight of less than 3,000 and water, which method including wet grinding a cocrystal, which is constituted of an organic compound and a cocrystal former and is not dissociated by wet grinding, in water containing the polymer and the surfactant.
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公开(公告)号:US10202376B2
公开(公告)日:2019-02-12
申请号:US15538297
申请日:2015-12-21
发明人: Eiji Kimura , Yuhei Miyanohana , Masaki Ogino , Yuta Tanaka , Makoto Fushimi , Tomohiro Okawa , Yuki Hanya , Tatsuki Koike
IPC分类号: C07D471/04 , A61K31/437 , C07D487/04 , A61P25/00 , A61P29/00
摘要: Provided is a compound having an antagonistic action on an NMDA receptor containing the NR2B subunit, and is useful as a prophylactic or therapeutic agent for major depression, bipolar disorder, migraine, pain, peripheral symptoms of dementia and the like. A compound represented by the formula (I): wherein each symbol is as described in the DESCRIPTION, (excluding N-(4-bromo-3-(1H-1,2,4-triazol-5-yl)thiophen-2-yl)-2-(imidazo[1,2-a]pyridin-5-yl)acetamide) or a salt thereof.
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公开(公告)号:US20190000981A1
公开(公告)日:2019-01-03
申请号:US16064061
申请日:2016-12-21
申请人: Nigel W. Bunnett , Christopher J.H. Porter , Derek Cole , Gareth Hicks , Junya Shirai , Gavin Hirst , Takeda Pharmaceutical Company Limited
发明人: Nigel W. Bunnett , Christopher J.H. Porter , Derek Cole , Gareth Hicks , Junya Shirai , Gavin Hirst
IPC分类号: A61K47/54 , A61K47/60 , A61K31/575 , A61K31/44 , A61P43/00
摘要: The present invention relates to tripartite compounds comprising a modulator moiety for endosomal G protein-coupled receptors like neurokinin-1 receptor, a linker and a lipid anchor suitable for anchoring the tripartite compound into a plasma membrane. The present invention also relates to a prodrug and a pharmaceutical composition comprising the tripartite compound and the use of the tripartite compound for the treatment of a disease or disorder mediated by endosomal G protein-coupled receptors signalling like NK1R signalling.
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公开(公告)号:US10093629B2
公开(公告)日:2018-10-09
申请号:US15321609
申请日:2015-06-30
发明人: Satoshi Yamamoto , Junya Shirai , Tsuneo Oda , Mitsunori Kono , Atsuko Ochida , Takashi Imada , Hidekazu Tokuhara , Yoshihide Tomata , Naoki Ishii , Michiko Tawada , Yoshiyuki Fukase , Tomoya Yukawa , Shoji Fukumoto
IPC分类号: C07D217/26 , C07D491/056 , C07D491/048 , C07F7/08 , C07D471/04 , A61K31/4375 , A61K31/472 , A61K31/4741 , C07D217/14 , C07D491/14
摘要: Provided are heterocyclic compounds having a RORγt inhibitory action represented by the formula (I): wherein each symbol is as defined in the specification, or a salt thereof.
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公开(公告)号:US10081624B2
公开(公告)日:2018-09-25
申请号:US15506380
申请日:2015-08-25
发明人: Akira Kaieda , Naoki Ishii , Hiroshi Nara , Masato Yoshikawa , Masaki Daini , Masashi Toyofuku , Kousuke Hidaka
IPC分类号: C07D413/12 , C07D413/14 , C07D417/14 , C07D471/04 , C07D487/04 , C07D491/08 , C07D513/04
CPC分类号: C07D413/12 , A61K31/4245 , A61K31/454 , A61K31/4709 , A61K31/4725 , A61K31/496 , A61K31/5377 , A61K31/55 , C07D413/14 , C07D417/14 , C07D471/04 , C07D487/04 , C07D491/08 , C07D491/107 , C07D513/04
摘要: The present invention provides a heterocyclic compound having a HDAC inhibitory action, and useful for the treatment of autoimmune diseases and/or inflammatory diseases, graft versus host disease, cancers, central nervous diseases including neurodegenerative diseases and the like, and a medicament comprising the compound.The present invention relates to a compound represented by the formula (I): wherein each symbol is as defined in the specification, or a salt thereof.
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公开(公告)号:US10077266B2
公开(公告)日:2018-09-18
申请号:US15621761
申请日:2017-06-13
发明人: Jason W. Brown , Stephen Hitchcock , Maria Hopkins , Shota Kikuchi , Holger Monenschein , Holly Reichard , Kristin Schleicher , Huikai Sun , Todd Macklin
IPC分类号: A61K31/4985 , C07D471/04
摘要: The present invention provides compounds of formula I: which are useful as modulators of GPR6, pharmaceutical compositions thereof, methods for treatment of conditions associated with GPR6, processes for making the compounds and intermediates thereof.
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公开(公告)号:US10053468B2
公开(公告)日:2018-08-21
申请号:US14902309
申请日:2014-07-02
发明人: Satoshi Yamamoto , Junya Shirai , Hiroyuki Watanabe , Shoji Fukumoto , Tsuneo Oda , Hidekazu Tokuhara , Yoshihide Tomata , Naoki Ishii , Michiko Tawada , Mitsunori Kono , Atsuko Ochida , Takashi Imada , Yoshiyuki Fukase , Tomoya Yukawa
IPC分类号: C07D491/056 , C07D217/26 , C07D401/06 , C07D405/06 , C07D409/06 , C07D413/06 , C07D417/06 , C07D471/04 , C07D491/048 , C07D401/12 , C07D413/12 , C07D491/04 , C07D413/14 , C07D401/04 , C07D405/12 , C07F7/08
CPC分类号: C07D491/056 , C07D217/26 , C07D401/04 , C07D401/06 , C07D401/12 , C07D405/06 , C07D405/12 , C07D409/06 , C07D413/06 , C07D413/12 , C07D413/14 , C07D417/06 , C07D471/04 , C07D491/04 , C07D491/048 , C07F7/0812
摘要: The present invention relates to compound (I) or a salt thereof which has a RORγt inhibitory action. wherein each symbol is as defined in the specification.
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公开(公告)号:US09963443B2
公开(公告)日:2018-05-08
申请号:US15316937
申请日:2015-06-08
发明人: Tatsuki Koike , Shuhei Ikeda
IPC分类号: A61K31/506 , C07D401/14 , A61K51/04 , C07D401/04 , C07D405/14 , C07D417/14
CPC分类号: C07D401/14 , A61K51/0455 , A61K51/0459 , C07B59/002 , C07B2200/05 , C07D401/04 , C07D405/14 , C07D417/14
摘要: The present invention provides radiolabeled compounds useful as radiotracers for quantitative imaging of CH24H in mammals. The compound of the present invention is represented by the formula (I): wherein each symbol is as defined in the specification.
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公开(公告)号:US20180118708A1
公开(公告)日:2018-05-03
申请号:US15572231
申请日:2016-05-06
发明人: Toshitake KOBAYASHI , Morihisa SAITOH , Yasufumi WADA , Hiroshi NARA , Nobuyuki NEGORO , Masashi YAMASAKI , Takahiro TANAKA , Naomi KITAMOTO
CPC分类号: C07D317/72 , A61K31/357 , A61P1/16 , A61P9/10 , A61P25/02 , A61P29/00 , A61P37/00
摘要: The present invention provides compounds having a Toll-like receptor 4 (TLR4) signaling inhibitory action useful as preventive and therapeutic drugs of autoimmune disease and/or inflammatory disease or diseases such as chemotherapy-induced peripheral neuropathy (CIPN), chemotherapy-induced neuropathic pain (CINP), liver injury, ischemia-reperfusion injury (IRI) and the like.The present invention relates to a compound represented by formula (I) and a salt thereof: (wherein, each symbol is explained in greater detail in the specification).
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