公开(公告)号：US20220098143A1

公开(公告)日：2022-03-31

申请号：US17548281

申请日：2021-12-10

申请人： Pano Therapeutics, Inc.

发明人： Francesca Fieni

IPC分类号： C07C233/20 ,  C07C69/734 ,  C07C69/708 ,  C07D295/033 ,  C07D401/12 ,  C07D401/04 ,  C07D211/08 ,  C07D311/68 ,  C07D217/02

摘要： Provided herein are combinations of capsaicin and TrpV1 modulators that are useful for treating capsaicin-responsive diseases or disorders.

公开(公告)号：US20200207797A1

公开(公告)日：2020-07-02

申请号：US16696196

申请日：2019-11-26

申请人： Lumena Pharmaceuticals LLC

发明人： Bronislava GEDULIN ,  Michael GREY ,  Niall O'DONNELL

IPC分类号： C07H13/12 ,  C07D295/13 ,  C07D281/10 ,  C07D211/06 ,  C07C279/12 ,  A61K31/7028 ,  C07H15/26 ,  C07D487/08 ,  C07D413/12 ,  C07D401/12 ,  C07D337/08 ,  C07D285/36 ,  C07D211/08 ,  C07D207/04 ,  C07C257/10 ,  A61K45/06 ,  A61K31/7042 ,  A61K31/554 ,  A61K31/5377 ,  A61K31/4995 ,  A61K31/495 ,  A61K31/454 ,  A61K31/4453 ,  A61K31/4436 ,  A61K31/40 ,  A61K31/38 ,  A61K31/155 ,  C07H15/18

摘要： Provided herein are methods of treating or ameliorating hypercholemia or a cholestatic liver disease by administering to an individual in need thereof a therapeutically effective amount of an Apical Sodium-dependent Bile Acid Transporter Inhibitor (ASBTI) or a pharmaceutically acceptable salt thereof. Also provided are methods for treating or ameliorating a liver disease, decreasing the levels of serum bile acids or hepatic bile acids, treating or ameliorating pruritis, reducing liver enzymes, or reducing bilirubin comprising administering to an individual in need thereof a therapeutically effective amount of ASBTI or a pharmaceutically acceptable salt thereof.

公开(公告)号：US10556853B2

公开(公告)日：2020-02-11

申请号：US15866924

申请日：2018-01-10

申请人： OWEN-BARRY PHARMACEUTICALS INC.

发明人： Michael Poulter ,  Tony Durst

IPC分类号： C07C69/78 ,  C07C65/32 ,  C07C49/753 ,  C07C49/697 ,  C07C49/683 ,  C07C235/84 ,  C07C317/24 ,  C07C321/28 ,  C07C255/40 ,  C07C49/603 ,  C07D211/08 ,  A61P25/08

摘要： The present application relates to compounds and methods for reducing the severity of convulsant activity or epileptic seizures, or for the treatment of chronic or acute pain.

公开(公告)号：US10399933B2

公开(公告)日：2019-09-03

申请号：US15564153

申请日：2016-04-01

申请人： BRISTOL-MYERS SQUIBB COMPANY

发明人： James Aaron Balog ,  Weiwei Guo ,  Audris Huang ,  Jay A. Markwalder ,  Weifang Shan ,  David K. Williams ,  Susheel Jethanand Nara ,  Saumya Roy

IPC分类号： C07D309/14 ,  C07C275/40 ,  C07D211/10 ,  A61K31/17 ,  A61K31/196 ,  A61K31/277 ,  A61K31/351 ,  A61K31/382 ,  A61K31/397 ,  A61K31/428 ,  A61K31/437 ,  A61K31/445 ,  A61K31/501 ,  A61K31/505 ,  A61K31/506 ,  A61K31/519 ,  A61K31/5375 ,  A61K31/5377 ,  A61K31/538 ,  A61K39/395 ,  C07C229/42 ,  C07C255/58 ,  C07D205/04 ,  C07D211/14 ,  C07D239/47 ,  C07D265/36 ,  C07D277/64 ,  C07D295/155 ,  C07D309/04 ,  C07D335/02 ,  C07D401/12 ,  C07D405/12 ,  C07D405/14 ,  C07D409/12 ,  C07D413/12 ,  C07D417/12 ,  C07D471/04 ,  C07D487/04 ,  C07D407/12 ,  C07D487/08 ,  C07D265/30 ,  C07D207/08 ,  C07D211/08 ,  C07D307/22 ,  C07C255/57 ,  C07C235/38 ,  C07C235/56 ,  C07C233/81 ,  C07C275/42 ,  C07D207/12 ,  C07D239/34 ,  C07D317/46 ,  C07D413/14 ,  C07D471/08 ,  C07C275/30 ,  A61K45/06

摘要： There are disclosed compounds of formula (I) that modulate or inhibit the enzymatic activity of indoleamine-2,3-dioxygenase (IDO), pharmaceutical compositions containing said compounds and methods of treating proliferative disorders, such as cancer, viral infections and/or inflammatory disorders utilizing the compounds of the invention.

公开(公告)号：US10399932B2

公开(公告)日：2019-09-03

申请号：US15564146

申请日：2016-04-01

申请人： BRISTOL-MYERS SQUIBB COMPANY

发明人： James Aaron Balog ,  Emily Charlotte Cherney ,  Jay A. Markwalder ,  Steven P. Seitz ,  Weifang Shan ,  David K. Williams ,  Audris Huang ,  Susheel Jethanand Nara ,  Saumya Roy ,  Soodamani Thangavel ,  Ramesh Kumar Sistla ,  Srinivas Cheruku ,  Srinivasan Thangathirupathy ,  Yadagiri Kanyaboina ,  Nagalakshmi Pulicharla

IPC分类号： C07D309/14 ,  C07D405/12 ,  C07D413/12 ,  C07D335/02 ,  C07D211/10 ,  C07D265/30 ,  C07D409/12 ,  C07C275/40 ,  A61K31/17 ,  A61K31/196 ,  A61K31/277 ,  A61K31/351 ,  A61K31/382 ,  A61K31/397 ,  A61K31/428 ,  A61K31/437 ,  A61K31/445 ,  A61K31/501 ,  A61K31/505 ,  A61K31/506 ,  A61K31/519 ,  A61K31/5375 ,  A61K31/5377 ,  A61K31/538 ,  A61K39/395 ,  C07C229/42 ,  C07C255/58 ,  C07D205/04 ,  C07D211/14 ,  C07D239/47 ,  C07D265/36 ,  C07D277/64 ,  C07D295/155 ,  C07D309/04 ,  C07D401/12 ,  C07D405/14 ,  C07D417/12 ,  C07D471/04 ,  C07D487/04 ,  C07D407/12 ,  C07D487/08 ,  C07D207/08 ,  C07D211/08 ,  C07D307/22 ,  C07C255/57 ,  C07C235/38 ,  C07C235/56 ,  C07C233/81 ,  C07C275/42 ,  C07D207/12 ,  C07D239/34 ,  C07D317/46 ,  C07D413/14 ,  C07D471/08 ,  C07C275/30 ,  A61K45/06

摘要： There are disclosed compounds of formula (I) that modulate or inhibit the enzymatic activity of indoleamine-2,3-dioxygenase (IDO), pharmaceutical compositions containing said compounds and methods of treating proliferative disorders, such as cancer, viral infections and/or inflammatory disorders utilizing the compounds of the invention.

公开(公告)号：US10206893B2

公开(公告)日：2019-02-19

申请号：US15422118

申请日：2017-02-01

申请人： Flexus Biosciences, Inc.

发明人： Hilary Plake Beck ,  Juan Carlos Jaen ,  Maksim Osipov ,  Jay Patrick Powers ,  Maureen Kay Reilly ,  Hunter Paul Shunatona ,  James Ross Walker ,  Mikhail Zibinsky ,  James Aaron Balog ,  David K. Williams ,  Jay A. Markwalder ,  Steven P. Seitz ,  Emily Charlotte Cherney ,  Liping Zhang ,  Weifang Shan ,  Weiwei Guo ,  Audris Huang

IPC分类号： A61K31/166 ,  A61K31/5377 ,  A61K31/497 ,  A61K31/506 ,  A61K45/06 ,  A61K31/4709 ,  C07D487/04 ,  C07C255/50 ,  A61K31/277 ,  C07C233/65 ,  C07D211/08 ,  A61K31/445 ,  C07C211/45 ,  A61K31/136 ,  C07D215/04 ,  A61K31/47 ,  C07D215/233 ,  C07D213/68 ,  A61K31/4412 ,  A61K31/496 ,  A61K31/519 ,  A61K31/00 ,  C07C255/58 ,  C07C275/30 ,  C07C217/80 ,  C07C233/10 ,  C07C233/59 ,  C07C233/60 ,  C07C233/74

摘要： Compounds that modulate the oxidoreductase enzyme indoleamine 2,3-dioxygenase, and compositions containing the compounds, are described herein. The use of such compounds and compositions for the treatment and/or prevention of a diverse array of diseases, disorders and conditions, including cancer- and immune-related disorders, that are mediated by indoleamine 2,3-dioxygenase is also provided.

公开(公告)号：US20160137653A1

公开(公告)日：2016-05-19

申请号：US14933879

申请日：2015-11-05

申请人： Flexus Biosciences, Inc.

发明人： Hilary Plake Beck ,  Juan Carlos Jaen ,  Maksim Osipov ,  Jay Patrick Powers ,  Maureen Kay Reilly ,  Hunter Paul Shunatona ,  James Ross Walker ,  Mikhail Zibinsky ,  James Aaron Balog ,  David K. Williams ,  Jay A. Markwalder ,  Steven P. Seitz ,  Emily Charlotte Cherney ,  Liping Zhang ,  Weifang Shan ,  Weiwei Guo ,  Audris Huang

IPC分类号： C07D487/04 ,  A61K31/277 ,  C07C233/65 ,  A61K31/166 ,  C07D211/08 ,  A61K31/445 ,  C07C211/45 ,  A61K31/136 ,  C07D215/04 ,  A61K31/47 ,  A61K31/4709 ,  C07D215/233 ,  C07D213/68 ,  A61K31/4412 ,  A61K31/496 ,  A61K31/519 ,  A61K31/5377 ,  A61K45/06 ,  C07C255/50

CPC分类号： A61K31/166 ,  A61K31/00 ,  A61K31/136 ,  A61K31/277 ,  A61K31/4412 ,  A61K31/445 ,  A61K31/47 ,  A61K31/4709 ,  A61K31/496 ,  A61K31/497 ,  A61K31/506 ,  A61K31/519 ,  A61K31/5377 ,  A61K45/06 ,  C07C211/45 ,  C07C217/80 ,  C07C233/10 ,  C07C233/59 ,  C07C233/60 ,  C07C233/65 ,  C07C233/74 ,  C07C255/50 ,  C07C255/58 ,  C07C275/30 ,  C07C2601/14 ,  C07D211/08 ,  C07D213/68 ,  C07D215/04 ,  C07D215/233 ,  C07D487/04

摘要： Compounds that modulate the oxidoreductase enzyme indoleamine 2,3-dioxygenase, and compositions containing the compounds, are described herein. The use of such compounds and compositions for the treatment and/or prevention of a diverse array of diseases, disorders and conditions, including cancer- and immune-related disorders, that are mediated by indoleamine 2,3-dioxygenase is also provided.

公开(公告)号：US20150232420A1

公开(公告)日：2015-08-20

申请号：US14429288

申请日：2013-09-19

申请人： Celia DOMINGUEZ ,  Michael PRIME ,  Richard MARSTON ,  Frederick A. BROOKFIELD ,  Stephen M. COURTNEY ,  Douglas MACDONALD ,  John WITYAK ,  Christopher John YARNOLD ,  Darshan VAIDYA

发明人： Celia Dominguez ,  Michael Prime ,  Richard Marston ,  Frederick A. Brookfield ,  Stephen M. Courtney ,  Douglas Macdonald ,  John Wityak ,  Christopher John Yarnold ,  Darshan Vaidya

IPC分类号： C07C271/22 ,  C07D207/06 ,  C07D213/74 ,  C07D205/04 ,  C07D211/08 ,  C07D295/185 ,  C07D223/04

CPC分类号： C07C271/22 ,  C07D205/04 ,  C07D207/06 ,  C07D207/16 ,  C07D211/08 ,  C07D211/16 ,  C07D213/72 ,  C07D213/74 ,  C07D223/04 ,  C07D277/42 ,  C07D295/18 ,  C07D295/185 ,  C07D309/08 ,  C07D401/12

摘要： Certain compounds and pharmaceutically acceptable salts are provided herein. Also provided are pharmaceutical compositions comprising at least one compound or pharmaceutically acceptable salt therein and one or more pharmaceutically acceptable vehicle. Methods of treating patients suffering from certain disease states responsive to the inhibition of transglutaminase TG2 activity are described. These disease states include neurodegenerative disorders such as Huntington's disease. Also described are methods of treatment include administering at least one compound or pharmaceutically acceptable salt thereof as a single active agent or administering at least one compound or pharmaceutically acceptable salt thereof in combination with one or more other therapeutic agents.

摘要翻译： 本文提供了某些化合物和药学上可接受的盐。 还提供了包含至少一种化合物或其药学上可接受的盐的药物组合物和一种或多种药学上可接受的载体。 描述了治疗患有某种疾病状态的患者对抑制转谷氨酰胺酶TG2活性有反应的方法。 这些疾病状态包括神经变性疾病如亨廷顿病。 还描述了治疗方法，包括给予至少一种化合物或其药学上可接受的盐作为单一活性剂，或者与一种或多种其它治疗剂组合施用至少一种化合物或其药学上可接受的盐。

公开(公告)号：US08530434B2

公开(公告)日：2013-09-10

申请号：US13007967

申请日：2011-01-17

申请人： Yong Ba ,  Errol V. Mathias

发明人： Yong Ba ,  Errol V. Mathias

IPC分类号： A61K31/704 ,  A61K31/445 ,  C07H15/24 ,  C07D211/08

CPC分类号： C07D211/94 ,  C07B2200/03

摘要： Nitroxide free radicals attached to antineoplastic agents can synergize their potencies to cancer cells. This invention relates to any antineoplastic agents and their derivatives chemically attached with nitroxide free radicals, such as TEMPO and its radical derivatives. This invention also relates to precursors of such compounds, as well as the products formed from the adducts after administration.

摘要翻译： 与抗肿瘤药物连接的硝基氧自由基可以将其效力与癌细胞协同作用。 本发明涉及与氮氧自由基化学连接的任何抗肿瘤剂及其衍生物，例如TEMPO及其自由基衍生物。 本发明还涉及这些化合物的前体，以及由给药后的加合物形成的产物。

公开(公告)号：US08501777B2

公开(公告)日：2013-08-06

申请号：US12089412

申请日：2006-10-12

申请人： Clas Sonesson

发明人： Clas Sonesson

IPC分类号： C07D211/08 ,  C07D401/00 ,  C07D405/00 ,  C07D409/00 ,  C07D411/00 ,  C07D413/00 ,  C07D417/00 ,  C07D419/00 ,  C07D421/00

CPC分类号： C07D211/24

摘要： The present invention relates to compounds having therapeutic effects against disorders in the central nervous system, and in particular substituted phenylpiperidines of the formula 1: wherein R is as defined herein.

摘要翻译： 本发明涉及对中枢神经系统疾病具有治疗作用的化合物，特别涉及式1所示取代的苯基哌啶：其中R如本文所定义。