公开(公告)号：US20240228431A1

公开(公告)日：2024-07-11

申请号：US18090953

申请日：2022-12-29

申请人： Codagen Biosciences, Inc.

发明人： Célina Reverdy ,  Gaetan Gitton ,  Xiangying Guan ,  Indranil Adhya ,  Rama Krishna Dumpati ,  Samir Roy ,  Santu Chall ,  Anisha Ghosh ,  Gauthier Errasti ,  Thomas Delacroix ,  Raj Chakrabarti

IPC分类号： C07C235/40 ,  C07D209/82 ,  C07D213/56 ,  C07D215/50 ,  C07D223/28 ,  C07D295/155 ,  C07D333/80

CPC分类号： C07C235/40 ,  C07D209/82 ,  C07D213/56 ,  C07D215/50 ,  C07D223/28 ,  C07D295/155 ,  C07D333/80

摘要： In one aspect, compounds modulating sirtuin activity are described herein. Sirtuin modulation by compounds described herein includes sirtuin activation and sirtuin inhibition. Modulation of sirtuin activity includes sirtuin activation and/or sirtuin inhibition. In some embodiments, a sirtuin modulating compound and/or salt thereof is of Formula I described herein.

公开(公告)号：US20240132469A1

公开(公告)日：2024-04-25

申请号：US18488924

申请日：2023-10-17

申请人： KayoThera Inc. ,  The Trustees of Princeton University

发明人： Mark ESPOSITO ,  John PROUDFOOT ,  Yibin KANG ,  John PIWINSKI

IPC分类号： C07D401/12 ,  A61P35/00 ,  C07D215/50 ,  C07D413/12 ,  C07D417/12 ,  C07D471/04 ,  C07D491/048 ,  C07D498/04 ,  C07D513/04

CPC分类号： C07D401/12 ,  A61P35/00 ,  C07D215/50 ,  C07D413/12 ,  C07D417/12 ,  C07D471/04 ,  C07D491/048 ,  C07D498/04 ,  C07D513/04

摘要： Provided herein are novel heterocyclic compounds, for example, compounds having Formula I, I-P, II, II-P, III, or IV. Also provided herein are pharmaceutical compositions comprising the compounds and methods of using the same, for example, in inhibiting aldehyde dehydrogenases, retinoid pathway activation, and/or for treating various cancers, cancer metastasis, type 2 diabetes, pulmonary arterial hypertension (PAH) or neointimal hyperplasia (NIH) or as a male contraceptive.

公开(公告)号：US20240002332A1

公开(公告)日：2024-01-04

申请号：US18253031

申请日：2021-11-18

申请人： Wenwei Huang ,  Khalida Shamim ,  Hengli Tang ,  The USA, as represented by The Secretary, Dept. of Health and Human Services ,  The Florida State University Research Foundation

发明人： Wenwei Huang ,  Khalida Shamim ,  Hengli Tang

IPC分类号： C07C235/84 ,  C07D211/46 ,  C07D209/26 ,  C07D277/44 ,  A61P31/14 ,  A61K9/00 ,  C07D215/50

CPC分类号： C07C235/84 ,  C07D211/46 ,  C07D209/26 ,  C07D277/44 ,  A61P31/14 ,  A61K9/0019 ,  C07D215/50

摘要： The present disclosure relates generally to compounds, pharmaceutical compositions comprising them, and methods of using the compounds and compositions for treating disease caused by severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2), commonly referred to as coronavirus disease 2019 (COVID-19). The present disclosure relates more particularly to small molecule inhibitors of SARS-CoV-2 of Formula (II) and prodrug derivatives thereof of Formula (I), and methods of treating COVID-19 therewith.

公开(公告)号：US11690838B2

公开(公告)日：2023-07-04

申请号：US17513946

申请日：2021-10-29

申请人： TAIHO PHARMACEUTICAL CO., LTD.

发明人： Akio Fujioka

IPC分类号： A61K31/47 ,  A61P11/00 ,  C07D215/50

CPC分类号： A61K31/47 ,  A61P11/00 ,  C07D215/50

摘要： Provided are a therapeutic agent and a pharmaceutical composition exerting an excellent prophylactic or therapeutic effect on fibrosis and symptoms associated with fibrosis. The therapeutic agent for fibrosis comprises 4-[2-fluoro-4-[[[(2-phenylacetyl)amino]thioxomethyl]amino]-phenoxy]-7-methoxy-N-methyl-6-quinolinecarboxamide or a salt thereof as an active ingredient.

公开(公告)号：US09795610B2

公开(公告)日：2017-10-24

申请号：US15399543

申请日：2017-01-05

申请人： HMI Medical Innovations, LLC

发明人： Gerard M. Housey

IPC分类号： A61K31/5377 ,  A61K31/506 ,  A61K31/47 ,  A61K31/4709 ,  A61K31/505 ,  A61K31/53 ,  A61K31/517 ,  A61K31/27 ,  A61K31/195 ,  A61K31/166 ,  A61K31/175 ,  A61K31/415 ,  A61K31/495 ,  A61K31/4196 ,  A61K31/44 ,  A61K31/444 ,  A61K31/4436 ,  G01N33/50

CPC分类号： A61K31/5377 ,  A61K31/166 ,  A61K31/175 ,  A61K31/195 ,  A61K31/27 ,  A61K31/415 ,  A61K31/4196 ,  A61K31/44 ,  A61K31/4436 ,  A61K31/444 ,  A61K31/47 ,  A61K31/4709 ,  A61K31/495 ,  A61K31/505 ,  A61K31/506 ,  A61K31/517 ,  A61K31/53 ,  C07C243/38 ,  C07D213/77 ,  C07D213/81 ,  C07D213/86 ,  C07D213/87 ,  C07D215/38 ,  C07D215/50 ,  C07D231/14 ,  C07D239/42 ,  C07D239/48 ,  C07D239/84 ,  C07D253/065 ,  C07D253/075 ,  C07D401/12 ,  C07D403/12 ,  C07D405/12 ,  C07D409/12 ,  G01N33/5011 ,  G01N33/502 ,  G01N33/5041 ,  G01N33/573 ,  G01N33/574 ,  G01N2500/00 ,  G01N2500/10

摘要： This invention relates to agents that are inhibitors or activators of variant forms of endogenous proteins and novel methods of identifying such variants. Of particular interest are inhibitors and activators of endogenous protein variants, encoded by genes which have mutated, which variants often arise or are at least first identified as having arisen following exposure to a chemical agent which is known to be an inhibitor or activator of the corresponding unmutated endogenous protein.

公开(公告)号：US09708286B2

公开(公告)日：2017-07-18

申请号：US14748925

申请日：2015-06-24

申请人： LEO Laboratories Limited

发明人： Gunnar Grue-Sørensen ,  Xifu Liang ,  Thomas Högberg ,  Kristoffer Månsson ,  Per Vedsø ,  Thomas Vifian

IPC分类号： C07C271/34 ,  C07D333/38 ,  C07C271/36 ,  C07C271/38 ,  C07D249/06 ,  C07D261/18 ,  C07D277/32 ,  C07D295/21 ,  C07D309/08 ,  C07D401/04 ,  C07D471/04 ,  C07D495/04 ,  C07D265/36 ,  C07D271/08 ,  C07D277/587 ,  C07D295/205 ,  C07D307/00 ,  C07D307/94 ,  C07D405/06 ,  C07D513/04 ,  A61K31/365 ,  A61K31/381 ,  A61K31/404 ,  A61K31/415 ,  A61K31/416 ,  A61K31/4192 ,  A61K31/42 ,  A61K31/472 ,  A61K31/502 ,  A61K31/5375 ,  A61K31/538 ,  C07D209/42 ,  C07D217/26 ,  C07D231/14 ,  C07D231/56 ,  C07D237/28 ,  C07D249/04

CPC分类号： C07D261/18 ,  A61K31/365 ,  A61K31/381 ,  A61K31/404 ,  A61K31/415 ,  A61K31/416 ,  A61K31/4192 ,  A61K31/42 ,  A61K31/472 ,  A61K31/502 ,  A61K31/5375 ,  A61K31/538 ,  C07C271/34 ,  C07C271/36 ,  C07C271/38 ,  C07C2603/86 ,  C07D209/08 ,  C07D209/42 ,  C07D213/79 ,  C07D215/50 ,  C07D217/26 ,  C07D231/14 ,  C07D231/56 ,  C07D233/90 ,  C07D237/28 ,  C07D239/28 ,  C07D249/04 ,  C07D249/06 ,  C07D261/20 ,  C07D263/34 ,  C07D265/36 ,  C07D271/08 ,  C07D277/32 ,  C07D277/56 ,  C07D277/587 ,  C07D295/182 ,  C07D295/205 ,  C07D295/21 ,  C07D307/00 ,  C07D307/68 ,  C07D307/94 ,  C07D309/08 ,  C07D333/38 ,  C07D333/40 ,  C07D401/04 ,  C07D405/06 ,  C07D471/04 ,  C07D493/08 ,  C07D495/04 ,  C07D513/04

摘要： The invention relates to compounds of general formula I wherein R is heteroaryl optionally substituted by R7; or R is heterocycloalkyl or heterocycloalkenyl, optionally substituted by R8; or R is X wherein X is —NR11R12; and pharmaceutically acceptable salts, hydrates, or solvates thereof, for use—alone or in combination with one or more other pharmaceutically active compounds—in therapy, for preventing, treating or ameliorating diseases or conditions responsive to stimulation of neutrophil oxidative burst, responsive to stimulation of keratinocyte IL-8 release or responsive to induction of necrosis.

公开(公告)号：US09040553B2

公开(公告)日：2015-05-26

申请号：US13940008

申请日：2013-07-11

申请人： Iraj Lalezari ,  Jill Fabricant

发明人： Iraj Lalezari ,  Jill Fabricant

IPC分类号： C07D307/87 ,  C07D215/14 ,  C07D215/52 ,  C07C235/72 ,  C07D215/50 ,  C07D219/04 ,  C07C275/42 ,  C07C229/40 ,  A61K8/41 ,  A61K8/42 ,  A61K8/49 ,  A61Q19/08 ,  C07C215/76 ,  C07C233/75 ,  C07C235/74 ,  C07C275/34 ,  C07D215/12

CPC分类号： C07D307/87 ,  A61K8/411 ,  A61K8/42 ,  A61K8/4926 ,  A61Q19/08 ,  C07C215/76 ,  C07C229/40 ,  C07C233/75 ,  C07C235/72 ,  C07C235/74 ,  C07C275/34 ,  C07C275/42 ,  C07D215/12 ,  C07D215/14 ,  C07D215/50 ,  C07D215/52 ,  C07D219/04

摘要： The present invention provides a process for the synthesis of substituted phenoxymethylpropionic acid and related compounds. The compounds are useful for inhibiting the formation of AGEs (Advanced Glycation End Products).

摘要翻译： 本发明提供了一种合成取代的苯氧基甲基丙酸和相关化合物的方法。 该化合物可用于抑制AGEs（高级糖化终产物）的形成。

公开(公告)号：US20150133441A1

公开(公告)日：2015-05-14

申请号：US14297863

申请日：2014-06-06

申请人： HMI Medical Innovations, LLC.

发明人： Gerard M. Housey

IPC分类号： A61K31/5377 ,  A61K31/47 ,  G01N33/50 ,  A61K31/505 ,  A61K31/53 ,  A61K31/506 ,  A61K31/4709

CPC分类号： A61K31/5377 ,  A61K31/166 ,  A61K31/175 ,  A61K31/195 ,  A61K31/27 ,  A61K31/415 ,  A61K31/4196 ,  A61K31/44 ,  A61K31/4436 ,  A61K31/444 ,  A61K31/47 ,  A61K31/4709 ,  A61K31/495 ,  A61K31/505 ,  A61K31/506 ,  A61K31/517 ,  A61K31/53 ,  C07C243/38 ,  C07D213/77 ,  C07D213/81 ,  C07D213/86 ,  C07D213/87 ,  C07D215/38 ,  C07D215/50 ,  C07D231/14 ,  C07D239/42 ,  C07D239/48 ,  C07D239/84 ,  C07D253/065 ,  C07D253/075 ,  C07D401/12 ,  C07D403/12 ,  C07D405/12 ,  C07D409/12 ,  G01N33/5011 ,  G01N33/502 ,  G01N33/5041 ,  G01N33/573 ,  G01N33/574 ,  G01N2500/00 ,  G01N2500/10

摘要： This invention relates to agents that are inhibitors or activators of variant forms of endogenous proteins and novel methods of identifying such variants. Of particular interest are inhibitors and activators of endogenous protein variants, encoded by genes which have mutated, which variants often arise or are at least first identified as having arisen following exposure to a chemical agent which is known to be an inhibitor or activator of the corresponding unmutated endogenous protein.

摘要翻译： 本发明涉及作为内源性蛋白质的变体形式的抑制剂或活化剂的试剂，以及鉴定这些变体的新方法。 特别令人感兴趣的是内源性蛋白质变体的抑制剂和活化剂，其由具有突变的基因编码，所述变体经常出现或至少首先被鉴定为在暴露于化学试剂之后产生，已知其是相应的抑制剂或活化剂 未突变的内源蛋白

公开(公告)号：US20140243314A1

公开(公告)日：2014-08-28

申请号：US14347671

申请日：2012-09-24

申请人： BRISTOL-MYERS SQUIBB COMPANY

发明人： Jennifer X. Qiao ,  Carol Hui Hu ,  Tammy C. Wang

IPC分类号： C07D215/50 ,  C07D417/12 ,  C07D401/12

CPC分类号： C07D215/50 ,  C07D215/22 ,  C07D215/54 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D413/12 ,  C07D417/12 ,  C07D417/14 ,  C07D419/12

摘要： The present invention provides compounds of Formula (I): as defined in the specification and compositions comprising any of such novel compounds. These compounds are endothelial lipase inhibitors which may be used as medicaments.

摘要翻译： 本发明提供式（I）化合物：如说明书中所定义和包含任何这些新化合物的组合物。 这些化合物是可用作药物的内皮脂肪酶抑制剂。

公开(公告)号：US20140235548A1

公开(公告)日：2014-08-21

申请号：US14117816

申请日：2012-05-10

申请人： Cleave Biosciences, Inc.

发明人： Han-Jie Zhou ,  Francesco Parlati ,  Matthieu Roufflet ,  Ethan D. Emberley ,  Raymond J. Deshaies ,  Seth Cohen

IPC分类号： C07K5/06 ,  C07D215/36 ,  C07D215/48 ,  C07D215/54 ,  C07D215/50 ,  C07D215/18 ,  A61K38/05 ,  C07D215/42

CPC分类号： C07K5/06 ,  A61K31/4709 ,  A61K38/05 ,  C07D215/18 ,  C07D215/36 ,  C07D215/42 ,  C07D215/48 ,  C07D215/50 ,  C07D215/54

摘要： Compounds, pharmaceutical compositions, and methods of using such compounds to treat or prevent diseases or disorders associated with or mediated by JAMM proteins are disclosed. The compounds and compositions inhibit the enzymatic activity of a JAMM domain, including the JAMM domain of the CSN5 subunit of the COP9-signalsome (CSN), the JAMM domain of the Rpn11/Poh1/Psmd14 subunit of the 26S proteasome, the JAMM domain of AMSH, the JAMM domain of AMSH-LP, the JAMM domain of BRCC36, among other JAMM domains.

摘要翻译： 公开了化合物，药物组合物和使用这些化合物治疗或预防与JAMM蛋白相关或介导的疾病或病症的方法。 该化合物和组合物抑制JAMM结构域的酶活性，包括COP9-信号素（CSN）的CSN5亚基的JAMM结构域，26S蛋白酶体的Rpn11 / Poh1 / Psmd14亚基的JAMM结构域，JAMM结构域 AMSH，AMSH-LP的JAMM域，BRCC36的JAMM域以及其他JAMM域。