公开(公告)号：US20240002350A1

公开(公告)日：2024-01-04

申请号：US18037406

申请日：2021-11-17

申请人： UNIVERSITY OF PITTSBURGH-OF THE COMMONWEALTH SYSTEM OF HIGHER EDUCATION ,  NATIONAL CENTER FOR ADVANCING TRANSLATIONAL SCIENCES/DPI/NIH

发明人： Sally Ellen MORGANROTH ,  Valerian KAGAN ,  Jinming ZHAO ,  Ganesha RAI ,  Hulya BAYIR ,  Yulia TYURINA ,  Haider DAR ,  Tamil ANTHONYMUTHU ,  Joel GREENBERGER ,  Michael EPPERLY ,  Diane LUCI ,  Juan MARUGAN ,  Anton SIMEONOV ,  Alexey V. ZAKHAROV ,  Adam YASGAR ,  Andrew AMOSCATO

IPC分类号： C07D239/42 ,  C07D233/84 ,  C07D233/88 ,  C07D403/12 ,  C07C335/16 ,  C07D401/04 ,  C07D237/20 ,  C07D249/10 ,  C07D263/46 ,  C07D263/48 ,  C07D277/36 ,  C07D277/42 ,  A61P25/00

CPC分类号： C07D239/42 ,  C07D233/84 ,  C07D233/88 ,  C07D403/12 ,  C07C335/16 ,  C07D401/04 ,  C07D237/20 ,  C07D249/10 ,  C07D263/46 ,  C07D263/48 ,  C07D277/36 ,  C07D277/42 ,  A61P25/00

摘要： Disclosed are compounds and methods for preventing or treating necroinflammation associated with ferroptotic processes. The method includes inhibiting 15 lipoxygenase/phosphatidylethanolamine binding protein (15LOX/PEBP1) complex, wherein the inhibitor exhibits a higher binding affinity or binding activity for 15LOX/PEBP1 complex compared to 15LOX alone. Necroinflammation associated with ferroptotic processes causes several pathogenic conditions including upper or lower respiratory disorders, acute or chronic brain injury, renal injury, injury by radiation, neurodegenerative disorder, among others. The disclosed compounds and methods are useful in subjects diagnosed with one or more of these conditions.

公开(公告)号：US20230134821A1

公开(公告)日：2023-05-04

申请号：US17966227

申请日：2022-10-14

申请人： THE UNIVERSITY OF BRITISH COLUMBIA

发明人： ARTEM TCHERKASSOV ,  PAUL S. RENNIE ,  FUQIANG BAN ,  ERIC J.J. LEBLANC ,  LAVINIA A. CARABET ,  NADA LALLOUS ,  KRITI SINGH ,  HELENE MORIN ,  ANH-TIEN TON

IPC分类号： C07C237/22 ,  C07C255/66 ,  C07C275/30 ,  C07C311/18 ,  C07C335/16 ,  C07C335/18 ,  C07D211/42 ,  C07D213/40 ,  C07D213/61 ,  C07D231/14 ,  C07D239/42 ,  C07D241/24 ,  C07D249/08 ,  C07D261/08 ,  C07D265/30 ,  C07D265/36 ,  C07D277/36 ,  C07D307/14 ,  C07D311/16 ,  C07D333/20 ,  C07D403/06 ,  C07D403/12 ,  C07D405/12 ,  C07D409/06 ,  C07D413/12 ,  C07D417/06 ,  C07D417/12 ,  C07D471/04

摘要： Provided herein are Myc-Max inhibitory compounds having the structure of Formula (I) and compositions thereof for use in the treatment of cancer. In particular, the Myc-Max inhibitory compounds may be useful for the treatment of cancers selected from one or more of: prostate cancer, breast cancer, colon cancer, cervical cancer, small-cell lung carcinomas, neuroblastomas, osteosarcomas, glioblastomas, melanoma and myeloid leukaemia.

公开(公告)号：US11465135B2

公开(公告)日：2022-10-11

申请号：US16976151

申请日：2019-01-24

申请人： KOREA UNIVERSITY RESEARCH AND BUSINESS FOUNDATION

发明人： Deok-Chan Ha ,  Jae Ho Shim

IPC分类号： B01J31/02 ,  C07C335/12 ,  C07C335/16 ,  C07C201/12 ,  C07C227/22 ,  C07D207/28 ,  C07C205/04 ,  C07C229/36

摘要： The present invention relates to a bifunctional chiral organocatalytic compound having excellent enantioselectivity, a preparation method therefor, and a method for producing a non-natural gamma amino acid from a nitro compound by using the chiral organocatalytic compound. According to the present invention, the bifunctional chiral organocatalytic compound having excellent enantioselectivity can be easily synthesized, gamma-amino acids with high optical selectivity can be obtained at a high yield by an economical and convenient method using the chiral organocatalytic compound, and various (R)-configuration gamma-amino acids, which are not present in nature, can be produced with high optical purity in large quantities by using a small amount of a catalyst, and therefore, the present invention can be widely utilized in various industrial fields including the pharmaceutical industry.

公开(公告)号：US10385004B2

公开(公告)日：2019-08-20

申请号：US15550224

申请日：2016-02-11

申请人： Novartis AG

发明人： Benjamin Martin ,  Francesca Mandrelli ,  Francesco Venturoni

IPC分类号： C07C201/10 ,  C07C201/12 ,  C07C227/04 ,  C07C335/16 ,  C07F9/535 ,  C07D207/06 ,  B01J31/02 ,  C07C205/04 ,  C07C205/44 ,  C07C205/51 ,  C07F7/18

摘要： The present invention relates to a new chemical synthesis, intermediates and catalysts useful for the preparation of the neprilysin (NEP) inhibitor sacubitril. It further relates to new intermediate compounds and their use for said new chemical synthesis route.

公开(公告)号：US20170320863A1

公开(公告)日：2017-11-09

申请号：US15520302

申请日：2015-10-13

申请人： Syngenta Participations AG

发明人： Shuji HACHISU ,  Alan Joseph HENNESSY ,  Jeffrey Steven WAILES ,  Nigel James WILLETTS ,  Christopher John MATHEWS ,  Janice BLACK ,  Suzanna Jane DALE

IPC分类号： C07D413/12 ,  A01N35/06 ,  C07D333/34 ,  C07D295/195 ,  C07D263/58 ,  C07D261/18 ,  C07D261/14 ,  C07D239/42 ,  C07D231/16 ,  C07D213/81 ,  C07D213/75 ,  C07C335/26 ,  C07C335/16 ,  C07C311/29 ,  C07C311/16 ,  C07C311/03 ,  C07C275/64 ,  C07C275/28 ,  C07C275/24 ,  C07C255/58 ,  C07C251/38 ,  C07C225/12 ,  A01N47/36 ,  A01N47/34 ,  A01N47/30 ,  A01N47/28 ,  A01N43/84 ,  A01N43/76 ,  A01N43/56 ,  A01N43/40 ,  A01N43/10 ,  A01N41/06 ,  A01N37/50 ,  A01N37/34 ,  C07D401/12 ,  C07D403/12

CPC分类号： C07D413/12 ,  A01N35/06 ,  A01N37/34 ,  A01N37/44 ,  A01N37/50 ,  A01N41/06 ,  A01N41/10 ,  A01N43/10 ,  A01N43/40 ,  A01N43/54 ,  A01N43/56 ,  A01N43/76 ,  A01N43/80 ,  A01N43/84 ,  A01N47/28 ,  A01N47/30 ,  A01N47/34 ,  A01N47/36 ,  A01N47/38 ,  C07C225/12 ,  C07C225/18 ,  C07C251/38 ,  C07C255/57 ,  C07C255/58 ,  C07C275/24 ,  C07C275/28 ,  C07C275/54 ,  C07C275/64 ,  C07C311/03 ,  C07C311/16 ,  C07C311/29 ,  C07C335/16 ,  C07C335/26 ,  C07C2601/08 ,  C07D213/61 ,  C07D213/74 ,  C07D213/75 ,  C07D213/76 ,  C07D213/78 ,  C07D213/81 ,  C07D213/84 ,  C07D231/16 ,  C07D233/96 ,  C07D239/28 ,  C07D239/42 ,  C07D261/04 ,  C07D261/14 ,  C07D261/18 ,  C07D263/58 ,  C07D295/195 ,  C07D333/34 ,  C07D401/12 ,  C07D403/12

摘要： The present invention relates to a compound of formula (I) wherein: wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R11 and G are as defined herein; and wherein the compound of formula (I) is optionally present as an agrochemically acceptable salt thereof. These compounds are thought to be suitable for use as herbicides. The invention therefore also relates to a method of controlling weeds, especially grassy monocotyledonous weeds, in crops of useful plants, comprising applying a compound of formula (I), or a herbicidal composition comprising such a compound, to the plants or to the locus thereof.

公开(公告)号：US20170115262A1

公开(公告)日：2017-04-27

申请号：US15310601

申请日：2014-12-11

申请人： University of Oregon

发明人： Michelle WATT ,  Darren W. JOHNSON ,  Michael M. HALEY

IPC分类号： G01N31/22 ,  C07C275/34 ,  C07D251/24 ,  C07C275/42 ,  C07C335/16 ,  C07C275/30 ,  C07C335/18

CPC分类号： G01N31/227 ,  C07C275/30 ,  C07C275/34 ,  C07C275/42 ,  C07C335/16 ,  C07C335/18 ,  C07C335/20 ,  C07D251/24 ,  G01N31/22

摘要： A compound, or a protonate or salt thereof, having a formula I of: wherein Y represents an optionally substituted aromatic group; n is 1 or 2; a is 0 to 4; R1 and R2 are each independently H; optionally substituted alkyl; optionally substituted aralkyl; acyl; phosphonyl; —S02R12; —C(0)R13; —C(0)OR14; —C(0)NR15R16; —C(0)CH2R17; or —C(S)—NR18R19; —S(0)R20; or —S02NR21R22, wherein R12-R22 are each independently H, optionally substituted alkyl, optionally substituted aralkyl, optionally substituted aryl, or —C(0)R23, wherein R23 is H, optionally substituted alkyl, optionally substituted aralkyl, or optionally substituted aryl; and each R3 is independently optionally substituted alkyl, halogen, optionally substituted alkoxy, optionally substituted carboxyl, amide; amino; or nitro.

公开(公告)号：US09561216B2

公开(公告)日：2017-02-07

申请号：US14972362

申请日：2015-12-17

申请人： AJINOMOTO CO., INC.

发明人： Masayuki Sugiki ,  Toru Okamatsu ,  Tetsuo Yano ,  Shinya Taniguchi

IPC分类号： A61K31/4402 ,  A23L27/20 ,  C07C275/42 ,  C07C309/51 ,  C07C311/32 ,  C07C311/51 ,  C07C333/08 ,  C07C335/16 ,  C07D209/14 ,  C07D213/74 ,  C07D233/61 ,  C07D271/10 ,  C07D295/16 ,  C07D413/04 ,  C07D213/75 ,  C07D295/192 ,  A61K31/185 ,  A61K31/198 ,  A61K31/27 ,  A61K31/4045 ,  A61K31/417 ,  A61K31/4245 ,  A61K31/44 ,  A61K31/5375

CPC分类号： A61K31/4402 ,  A23L27/202 ,  A23L27/204 ,  A61K31/185 ,  A61K31/198 ,  A61K31/27 ,  A61K31/4045 ,  A61K31/417 ,  A61K31/4245 ,  A61K31/44 ,  A61K31/5375 ,  C07C275/42 ,  C07C309/51 ,  C07C311/32 ,  C07C311/51 ,  C07C333/08 ,  C07C335/16 ,  C07C2601/14 ,  C07C2601/18 ,  C07D209/14 ,  C07D213/74 ,  C07D213/75 ,  C07D233/61 ,  C07D271/10 ,  C07D295/16 ,  C07D295/192 ,  C07D413/04

摘要： A composition containing a compound represented by General Formula (I) below (see the definition in the specification for the symbols in the formula) or a salt thereof has an excellent CaSR agonistic effect and provides a pharmaceutical agent, a CaSR agonistic agent, a prophylactic or therapeutic agent for a disease that can be ameliorated through CaSR activation as well as seasonings and an agent for imparting kokumi.

摘要翻译： 含有下述通式（I）表示的化合物的组合物（参照式中的符号的说明书中的定义）或其盐具有优异的CaSR激动作用，并且提供药剂，CaSR激动剂，预防 或用于通过CaSR活化可以改善的疾病以及调味料和用于赋予小丸的药剂的治疗剂。

公开(公告)号：US09283254B2

公开(公告)日：2016-03-15

申请号：US14569416

申请日：2014-12-12

申请人： Ottawa Hospital Research Institute

发明人： John Bell ,  Jean-Simon Diallo ,  Fabrice Le Boeuf

IPC分类号： A61K35/766 ,  A61K31/341 ,  A61K45/06 ,  C07C49/675 ,  C07C49/747 ,  C07C205/37 ,  C07C217/84 ,  C07C233/32 ,  C07C233/38 ,  C07C243/38 ,  C07C255/37 ,  C07C311/44 ,  C07C323/42 ,  C07C323/60 ,  C07C335/16 ,  C07C337/06 ,  C07C337/08 ,  C07D213/75 ,  C07D233/90 ,  C07D257/04 ,  C07D307/58 ,  C07D319/20 ,  C07D333/04 ,  C07D403/12 ,  C07D409/12 ,  C12N7/00 ,  A61K31/275 ,  A61K31/365 ,  A61K38/00

CPC分类号： A61K35/766 ,  A61K31/275 ,  A61K31/341 ,  A61K31/365 ,  A61K38/00 ,  A61K45/06 ,  C07C49/675 ,  C07C49/747 ,  C07C205/37 ,  C07C217/84 ,  C07C233/32 ,  C07C233/38 ,  C07C243/38 ,  C07C255/37 ,  C07C311/44 ,  C07C323/42 ,  C07C323/60 ,  C07C335/16 ,  C07C337/06 ,  C07C337/08 ,  C07C2601/02 ,  C07C2601/14 ,  C07C2603/26 ,  C07C2603/34 ,  C07D213/75 ,  C07D233/90 ,  C07D257/04 ,  C07D307/58 ,  C07D319/20 ,  C07D333/04 ,  C07D403/12 ,  C07D409/12 ,  C12N7/00 ,  C12N2760/20232 ,  C12N2760/20251 ,  A61K2300/00

摘要： Provided are viral sensitizing compounds that enhance the efficacy of viruses by increasing spread of the virus in cells, increasing the titer of virus in cells, or increasing the cytotoxicity of virus to cells. Other uses, compositions and methods of using same are also provided.

公开(公告)号：US09162977B2

公开(公告)日：2015-10-20

申请号：US13731971

申请日：2012-12-31

申请人： The University of Hong Kong

发明人： Dan Yang ,  Xiang Li ,  Huiyan Zha

IPC分类号： C07C239/08 ,  C07C335/16 ,  C07K5/062 ,  C07C259/06 ,  C07C275/28 ,  C07D213/79 ,  C07D213/81 ,  C07C239/20 ,  C07D213/63 ,  C07C271/22 ,  C07C237/22

CPC分类号： C07C335/16 ,  C07B2200/07 ,  C07C237/22 ,  C07C239/08 ,  C07C239/20 ,  C07C259/06 ,  C07C271/22 ,  C07C275/28 ,  C07D213/63 ,  C07D213/79 ,  C07D213/81 ,  C07K5/06034

摘要： Provided herein are self-assembling compounds that can form ion channels in lipid bilayers or cell membranes and ion-channel-forming compositions comprising the self-assembling compounds. Also provided are methods of making and using the ion channels formed from a plurality of molecules of the self-assembling compounds. Further, provided are methods of treating or preventing conditions and diseases that are related to the dysfunction of ion channels, including chloride channels.

摘要翻译： 本文提供了可以在脂质双层或细胞膜中形成离子通道的自组装化合物和包含自组装化合物的离子通道形成组合物。 还提供了制造和使用由多个自组装化合物分子形成的离子通道的方法。 此外，提供了治疗或预防与离子通道功能障碍（包括氯化物通道）相关的病症和疾病的方法。

公开(公告)号：US08410150B2

公开(公告)日：2013-04-02

申请号：US12530429

申请日：2008-03-06

申请人： Heinz W. Pauls ,  Peter Brent Sampson ,  Bryan T. Forrest ,  Radoslaw Laufer ,  Yong Liu ,  Miklos Feher ,  Yi Yao ,  Guohua Pan

发明人： Heinz W. Pauls ,  Peter Brent Sampson ,  Bryan T. Forrest ,  Radoslaw Laufer ,  Yong Liu ,  Miklos Feher ,  Yi Yao ,  Guohua Pan

IPC分类号： C07D307/66 ,  C07D333/32 ,  C07D213/18 ,  C07D233/70 ,  C07D417/04 ,  C07D263/36 ,  C07D249/12 ,  C07D261/10 ,  C07D207/36 ,  C07D275/03 ,  C07D271/06 ,  C07D285/08 ,  C07C335/16 ,  C07C327/40 ,  C07C327/08 ,  C07C311/10 ,  C07C237/14 ,  A61K31/34 ,  A61K31/381 ,  A61K31/4025 ,  A61K31/40 ,  A61K31/415 ,  A61K31/4164 ,  A61K31/4196 ,  A61K31/42 ,  A61K31/4245 ,  A61K31/425 ,  A61K31/433 ,  A61K31/435 ,  A61K31/64 ,  A61K31/155

CPC分类号： C07D409/06 ,  C07C1/26 ,  C07C17/10 ,  C07C2529/40 ,  C07D207/325 ,  C07D213/71 ,  C07D213/82 ,  C07D231/12 ,  C07D231/14 ,  C07D263/34 ,  C07D277/48 ,  C07D295/215 ,  C07D307/24 ,  C07D307/68 ,  C07D307/82 ,  C07D333/34 ,  C07D333/40 ,  C07D401/04 ,  C07D405/06 ,  C07D409/04 ,  C07D413/04 ,  C07D413/06 ,  C07D417/04 ,  C07C9/00 ,  C07C19/075

摘要： A CPT inhibitor compound is represented by Structural Formula (I) or a pharmaceutically acceptable salt thereof: or a pharmaceutically acceptable salt thereof. A pharmaceutical composition comprises a compound represented by Structural Formula (I) or a pharmaceutically acceptable salt thereof. A method of treating a subject having cancer comprises administering to the subject a therapeutically effective amount of a compound represented by Structural Formula (I) or a pharmaceutically acceptable salt thereof.

摘要翻译： CPT抑制剂化合物由结构式（I）或其药学上可接受的盐表示：或其药学上可接受的盐。 药物组合物包含由结构式（I）表示的化合物或其药学上可接受的盐。 治疗患有癌症的受试者的方法包括向受试者施用治疗有效量的由结构式（I）表示的化合物或其药学上可接受的盐。