公开(公告)号：US20220081390A1

公开(公告)日：2022-03-17

申请号：US17532618

申请日：2021-11-22

申请人： Metacrine, Inc.

发明人： Nicholas D. SMITH ,  Steven P. GOVEK ,  Johnny Y. NAGASAWA

IPC分类号： C07C233/80 ,  C07D333/32 ,  C07D239/34 ,  C07D241/18 ,  C07D263/32 ,  C07D205/04 ,  C07D207/27 ,  C07D275/03 ,  C07D277/34 ,  C07D213/65 ,  A61K45/06 ,  C07D207/12 ,  C07D213/75 ,  C07D207/08 ,  C07D213/68 ,  C07D211/42 ,  C07D211/46 ,  C07D213/40 ,  C07D213/64 ,  C07D213/80 ,  C07C271/20 ,  C07C233/63 ,  C07C237/22 ,  C07C237/42 ,  C07C233/59 ,  C07C233/62 ,  A61K31/167 ,  A61K31/216 ,  A61K31/381 ,  A61K31/397 ,  A61K31/40 ,  A61K31/4015 ,  A61K31/421 ,  A61K31/425 ,  A61K31/426 ,  A61K31/4418 ,  A61K31/445 ,  A61K31/4965 ,  A61K31/505 ,  C07D207/24 ,  C07D211/94

摘要： Described herein are compounds that are farnesoid X receptor agonists, methods of making such compounds, pharmaceutical compositions and medicaments comprising such compounds, and methods of using such compounds in the treatment of conditions, diseases, or disorders associated with farnesoid X receptor activity.

公开(公告)号：US10385014B2

公开(公告)日：2019-08-20

申请号：US15914621

申请日：2018-03-07

申请人： ARBOR PHARMACEUTICALS, LLC

发明人： Mark A. Gallop ,  Fenmei Yao ,  Maria J. Ludwikow ,  Thu Phan ,  Ge Peng

IPC分类号： C07C269/06 ,  C07C271/22 ,  C07D213/79 ,  C07D307/30 ,  C07D333/32 ,  C07D333/38 ,  C07D307/68 ,  A61K31/27

摘要： The disclosures herein relate generally to acyloxyalkyl carbamate prodrugs of (±)-4-amino-3-(4-chlorophenyl)butanoic acid and analogs thereof, pharmaceutical compositions thereof, methods of making prodrugs of (±)-4-amino-3-(4-chlorophenyl)butanoic acid and analogs thereof, methods of using prodrugs of (±)-4-amino-3-(4-chlorophenyl)butanoic acid and analogs thereof, and pharmaceutical compositions thereof for treating or preventing common diseases and/or disorders such as spasticity and/or acid reflux disease. The disclosures herein also relate to acyloxyalkyl carbamate prodrugs of (±)-4-amino-3-(4-chlorophenyl)butanoic acid and analogs thereof which are suitable for oral administration and to sustained release oral dosage forms thereof.

公开(公告)号：US20180282263A1

公开(公告)日：2018-10-04

申请号：US15758707

申请日：2016-09-16

申请人： Metacrine, Inc.

发明人： Nicholas D. SMITH ,  Steven P. GOVEK ,  Johnny Y. NAGASAWA

IPC分类号： C07C233/80 ,  C07D213/65 ,  A61K31/4418 ,  A61K45/06 ,  A61K31/167 ,  C07D207/27 ,  A61K31/4015 ,  A61K31/216 ,  C07D263/32 ,  A61K31/421 ,  C07D277/34 ,  A61K31/426 ,  C07D333/32 ,  A61K31/381 ,  C07D239/34 ,  A61K31/505 ,  C07D241/18 ,  A61K31/4965 ,  C07D275/03 ,  A61K31/425 ,  C07D205/04 ,  A61K31/397 ,  C07D207/24 ,  A61K31/40 ,  C07D211/94 ,  A61K31/445

摘要： Described herein are compounds that are farnesoid X receptor agonists, methods of making such compounds, pharmaceutical compositions and medicaments comprising such compounds, and methods of using such compounds in the treatment of conditions, diseases, or disorders associated with farnesoid X receptor activity.

公开(公告)号：US20170369462A1

公开(公告)日：2017-12-28

申请号：US15701565

申请日：2017-09-12

申请人： WISCONSIN ALUMNI RESEARCH FOUNDATION

发明人： Helen E. BLACKWELL ,  Grant D. GESKE ,  Jennifer C. CAMPBELL BUTLER

IPC分类号： C07D307/33 ,  C07D417/12 ,  C07D413/12 ,  C07D409/12 ,  C07D407/12 ,  C07D405/12 ,  C07D333/32 ,  C07D309/30 ,  C07D307/32 ,  C12N1/36 ,  A61K31/365

CPC分类号： C07D307/33 ,  A61K31/365 ,  C07D307/32 ,  C07D309/30 ,  C07D333/32 ,  C07D405/12 ,  C07D407/12 ,  C07D409/12 ,  C07D413/12 ,  C07D417/12 ,  C12N1/36 ,  Y02A50/471 ,  Y02A50/473

摘要： The present invention provides compounds and methods for modulation of the quorum sensing of bacteria. In an embodiment, the compounds of the present invention are able to act as replacements for naturally occurring bacterial quorum sensing ligands in a ligand-protein binding system; that is, they imitate the effect of natural ligands and produce an agonistic effect. In another embodiment, the compounds of the present invention are able to act in a manner which disturbs or inhibits the naturally occurring ligand-protein binding system in quorum sensing bacteria; that is, they produce an antagonistic effect. The compounds of the present invention comprise N-acylated-homoserine lactones (AHLs) comprised of a wide range of acyl groups.

公开(公告)号：US09708287B2

公开(公告)日：2017-07-18

申请号：US14872419

申请日：2015-10-01

申请人： Cayman Chemical Company Incorporated

发明人： Mitchell A. deLong ,  Kalla Lynn Kvalnes ,  Raymond Boissy

IPC分类号： C07D335/02 ,  C07D309/10 ,  A61K8/49 ,  A61K8/69 ,  C07D309/12 ,  A61Q19/02 ,  A61K8/60 ,  C07D215/227 ,  C07D311/94 ,  C07D313/04 ,  C07D313/18 ,  C07D333/32 ,  C07D333/64 ,  C07D493/04 ,  C07H15/203 ,  C07D311/02 ,  C07D215/22 ,  C07D319/12 ,  C07D333/48 ,  C07D307/20 ,  A61K8/33

CPC分类号： C07D335/02 ,  A61K8/33 ,  A61K8/4926 ,  A61K8/4973 ,  A61K8/498 ,  A61K8/4986 ,  A61K8/602 ,  A61K8/69 ,  A61K2800/591 ,  A61Q19/02 ,  C07D215/22 ,  C07D215/227 ,  C07D307/20 ,  C07D309/10 ,  C07D309/12 ,  C07D311/02 ,  C07D311/94 ,  C07D313/04 ,  C07D313/18 ,  C07D319/12 ,  C07D333/32 ,  C07D333/48 ,  C07D333/64 ,  C07D493/04 ,  C07H15/203

摘要： Compounds that function, alone or in combination, as inhibitors of pigmentation for the improvement of mammalian skin are described herein. Specifically, the compounds of the present disclosure, namely chiral, non-racemic compounds, function as pigment formation inhibitors thereof to beautify skin and discourage the production of melanins. One or more products, consumer and otherwise, comprising the chiral, non-racemic compounds are disclosed herein. Methods of employing both the compounds of the present disclosure and the products incorporating the present compounds are also disclosed herein.

公开(公告)号：US20170190657A1

公开(公告)日：2017-07-06

申请号：US15388870

申请日：2016-12-22

申请人： XENOPORT, INC.

发明人： Mark A. Gallop ,  Fenmei Yao ,  Maria J. Ludwikow ,  Thu Phan ,  Ge Peng

IPC分类号： C07C269/06 ,  C07D333/32 ,  C07D307/68

CPC分类号： C07C269/06 ,  A61K31/27 ,  C07C271/22 ,  C07C2101/08 ,  C07C2101/14 ,  C07C2601/08 ,  C07C2601/14 ,  C07D213/79 ,  C07D307/30 ,  C07D307/68 ,  C07D333/32 ,  C07D333/38

摘要： The disclosures herein relate generally to acyloxyalkyl carbamate prodrugs of (±)-4-amino-3-(4-chlorophenyl)butanoic acid and analogs thereof, pharmaceutical compositions thereof, methods of making prodrugs of (±)-4-amino-3-(4-chlorophenyl)butanoic acid and analogs thereof, methods of using prodrugs of (±)-4-amino-3-(4-chlorophenyl)butanoic acid and analogs thereof, and pharmaceutical compositions thereof for treating or preventing common diseases and/or disorders such as spasticity and/or acid reflux disease. The disclosures herein also relate to acyloxyalkyl carbamate prodrugs of (±)-4-amino-3-(4-chlorophenyl)butanoic acid and analogs thereof which are suitable for oral administration and to sustained release oral dosage forms thereof.

公开(公告)号：US20160355536A1

公开(公告)日：2016-12-08

申请号：US15238232

申请日：2016-08-16

申请人： FUJIFILM Corporation

发明人： Takayuki ITO ,  Toru WATANABE ,  Hideki OKADA ,  Hidenobu KUNIYOSHI

IPC分类号： C07H13/08 ,  C07D333/32 ,  C07H15/04

CPC分类号： C07H13/08 ,  C07D333/32 ,  C07H15/04 ,  C07H15/18

摘要： There is provided a production method of a compound represented by the following formula (II) through a step of reacting a compound represented by the following General Formula (I) with a sulfur compound. In General Formulas (I) and (II), R1 represents a hydrogen atom or an acyl group, R2 represents a hydrogen atom, a fluorine atom, an acyloxy group, an arylmethyloxy group, an allyloxy group, an arylmethyloxycarbonyloxy group, or an allyloxycarbonyloxy group, R3 represents a hydrogen atom or an acyloxy group, R5 represents an alkyl group or an aryl group, and X represents a leaving group. Here, in a case where R2 is a fluorine atom, an acyloxy group, an arylmethyloxy group, an allyloxy group, an arylmethyloxycarbonyloxy group, or an allyloxycarbonyloxy group, R3 is an acyloxy group.

摘要翻译： 在通式（I）和（II）中，R 1表示氢原子或酰基，R 2表示氢原子，氟原子，酰氧基，芳基甲氧基，烯丙氧基，芳基甲氧基羰基氧基或烯丙氧羰基氧基 基团，R 3表示氢原子或酰氧基，R 5表示烷基或芳基，X表示离去基团。 这里，在R 2为氟原子，酰氧基，芳基甲氧基，烯丙氧基，芳基甲氧基羰基氧基或烯丙氧基羰基氧基的情况下，R 3为酰氧基。

公开(公告)号：US09084773B2

公开(公告)日：2015-07-21

申请号：US14288984

申请日：2014-05-28

申请人： The Trustees of Princeton University

发明人： Bonnie L. Bassler ,  Lee R. Swem ,  Scott M. Ulrich ,  Colleen T. O'Loughlin

IPC分类号： A61K31/381 ,  C07D333/32 ,  A61K31/365 ,  A01N43/08 ,  A01N43/10 ,  A01N43/16 ,  A01N43/18 ,  A61K31/341 ,  C07D307/33 ,  C07D333/36

CPC分类号： A61K31/365 ,  A01N43/08 ,  A01N43/10 ,  A01N43/16 ,  A01N43/18 ,  A61K31/341 ,  A61K31/381 ,  C07D307/33 ,  C07D333/36

摘要： A novel small molecule antagonizes two types of acyl homoserine lactone receptors: membrane-bound and cytoplasmic. A focused library of analogs and derivatives of the original antagonist was synthesized. Analog and derivative molecules harbor a range of activities. The novel small molecule and most potent antagonist protects the eukaryote Caenorhabditis elegans from quorum-sensing-mediated killing by the bacterial pathogen Chromobacterium violaceum. The saving of C. elegans demonstrates the use of these molecules as small molecule antimicrobials.

摘要翻译： 一种新的小分子拮抗两种类型的酰基高丝氨酸内酯受体：膜结合和细胞质。 合成了原始拮抗剂类似物和衍生物的重点文库。 模拟和衍生分子具有一系列活动。 新型小分子和最有效的拮抗剂通过细菌病原体Chromobacterium v​​iolaceum从群体感应介导的杀伤中保护真核生物线虫。 秀丽隐杆线虫的保存证明了这些分子作为小分子抗菌药物的用途。

公开(公告)号：US08912182B2

公开(公告)日：2014-12-16

申请号：US13967922

申请日：2013-08-15

申请人： Pierre L. Beaulieu ,  Pasquale Forgione ,  Alexandre Gagnon ,  Cedrickx Godbout ,  Marc-Andre Joly ,  Montse Llinas-Brunet ,  Julie Naud ,  Martin Poirier ,  Jean Rancourt

发明人： Pierre L. Beaulieu ,  Pasquale Forgione ,  Alexandre Gagnon ,  Cedrickx Godbout ,  Marc-Andre Joly ,  Montse Llinas-Brunet ,  Julie Naud ,  Martin Poirier ,  Jean Rancourt

IPC分类号： C07D401/14 ,  C07D213/81 ,  C07D213/643 ,  C07D239/34 ,  A61K31/444 ,  C07D215/227 ,  C07D217/24 ,  C07D239/38 ,  C07D401/06 ,  C07D417/14 ,  C07D307/20 ,  C07D471/04 ,  C07D239/47 ,  C07D239/52 ,  C07D413/06 ,  C07D249/04 ,  C07D213/69 ,  A61K31/5377 ,  C07D211/38 ,  C07D417/06 ,  C07D333/32

CPC分类号： A61K31/444 ,  A61K31/5377 ,  C07D211/38 ,  C07D213/643 ,  C07D213/69 ,  C07D213/81 ,  C07D215/227 ,  C07D217/24 ,  C07D239/34 ,  C07D239/38 ,  C07D239/47 ,  C07D239/52 ,  C07D249/04 ,  C07D277/24 ,  C07D307/20 ,  C07D333/32 ,  C07D401/06 ,  C07D401/12 ,  C07D401/14 ,  C07D413/06 ,  C07D417/06 ,  C07D417/14 ,  C07D471/04

摘要： Compounds of formula I: wherein X, R2, R3, R3a, R3b, R5 and R6 are defined herein, are useful as inhibitors of the hepatitis C virus NS5B polymerase.

摘要翻译： 式I化合物：其中X，R2，R3，R3a，R3b，R5和R6如本文所定义，可用作丙型肝炎病毒NS5B聚合酶的抑制剂。

公开(公告)号：US20130224136A1

公开(公告)日：2013-08-29

申请号：US13734678

申请日：2013-01-04

申请人： Lasya, Inc.

发明人： Mitchell A. deLong ,  Kalla Lynn Kvalnes ,  Raymond Boissy

IPC分类号： A61K8/60 ,  C07D311/94 ,  A61K8/49 ,  C07D493/04 ,  A61Q19/02 ,  C07D313/04 ,  C07D215/227 ,  C07D335/02 ,  C07D333/32 ,  C07D333/64 ,  C07H15/203 ,  C07D313/18

CPC分类号： C07D335/02 ,  A61K8/33 ,  A61K8/4926 ,  A61K8/4973 ,  A61K8/498 ,  A61K8/4986 ,  A61K8/602 ,  A61K8/69 ,  A61K2800/591 ,  A61Q19/02 ,  C07D215/22 ,  C07D215/227 ,  C07D307/20 ,  C07D309/10 ,  C07D309/12 ,  C07D311/02 ,  C07D311/94 ,  C07D313/04 ,  C07D313/18 ,  C07D319/12 ,  C07D333/32 ,  C07D333/48 ,  C07D333/64 ,  C07D493/04 ,  C07H15/203

摘要： Compounds that function, alone or in combination, as inhibitors of pigmentation for the improvement of mammalian skin are described herein. Specifically, the compounds of the present disclosure, namely chiral, non-racemic compounds, function as pigment formation inhibitors thereof to beautify skin and discourage the production of melanins. One or more products, consumer and otherwise, comprising the chiral, non-racemic compounds are disclosed herein. Methods of employing both the compounds of the present disclosure and the products incorporating the present compounds are also disclosed herein.

摘要翻译： 本文描述了单独或组合作为改善哺乳动物皮肤的色素沉着抑制剂的化合物。 具体地说，本公开的化合物，即手性，非外消旋化合物，起着色素形成抑制剂的作用，从而美化皮肤并阻止黑色素的产生。 包含手性非外消旋化合物的一种或多种消费品和其它产品在此公开。 本文公开了使用本公开的化合物和掺入本发明化合物的产物的方法。