公开(公告)号：US20240067656A1

公开(公告)日：2024-02-29

申请号：US18490700

申请日：2023-10-19

申请人： The Regents of the University of California

发明人： Jonathan Ostrem ,  Ulf Peters ,  Kevan M. Shokat

IPC分类号： C07D495/04 ,  A61K38/17 ,  C07C235/20 ,  C07C317/08 ,  C07D207/14 ,  C07D211/58 ,  C07D211/62 ,  C07D231/40 ,  C07D295/185 ,  C07D295/26 ,  C07D401/04 ,  C07D401/06 ,  C07D401/12 ,  C07D405/12 ,  C07D409/04 ,  C07D413/12 ,  C07D417/12 ,  C07D471/10 ,  C07D487/04 ,  C07D487/10 ,  C12N9/14 ,  C12Q1/6886

CPC分类号： C07D495/04 ,  A61K38/1709 ,  C07C235/20 ,  C07C317/08 ,  C07D207/14 ,  C07D211/58 ,  C07D211/62 ,  C07D231/40 ,  C07D295/185 ,  C07D295/26 ,  C07D401/04 ,  C07D401/06 ,  C07D401/12 ,  C07D405/12 ,  C07D409/04 ,  C07D413/12 ,  C07D417/12 ,  C07D471/10 ,  C07D487/04 ,  C07D487/10 ,  C12N9/14 ,  C12Q1/6886 ,  C12Q2600/156 ,  C12Q2600/158 ,  C12Y306/05002 ,  G01N2500/04

摘要： K-Ras is the most frequently mutated oncogene in human cancer. Disclosed herein are compositions and methods for modulating K-Ras and treating cancer.

公开(公告)号：US20240010602A1

公开(公告)日：2024-01-11

申请号：US18347724

申请日：2023-07-06

申请人： Xavier University of Louisiana

发明人： Rami A. AL-HORANI

IPC分类号： C07C59/90 ,  C07C69/734 ,  C07C235/20 ,  A61P7/02

CPC分类号： C07C59/90 ,  C07C69/734 ,  C07C235/20 ,  A61P7/02

摘要： The present disclosure is directed to compounds having Formula (I) and their enantiomers, wherein the definitions of R, Y1, Y2, W, X, Z, and n are provided in the disclosure. The disclosure is also directed to pharmaceutical compositions of the disclosed compounds, as well as their use for treatment of thrombosis and related conditions and complications.

公开(公告)号：US11339139B2

公开(公告)日：2022-05-24

申请号：US16927601

申请日：2020-07-13

申请人： CORSAIR PHARMA, INC.

发明人： Cyrus K. Becker ,  Meenakshi S. Venkatraman ,  Xiaoming Zhang

IPC分类号： C07D313/00 ,  C07C69/712 ,  C07D317/40 ,  C07D321/00 ,  C07D257/06 ,  C07D263/24 ,  C07D265/30 ,  C07D295/088 ,  C07D211/60 ,  C07D295/145 ,  C07D307/20 ,  C07C219/16 ,  C07C235/20 ,  C07D453/02 ,  C07C59/54 ,  C07C69/734 ,  C07C235/34 ,  C07D207/08 ,  C07D263/26 ,  C07D317/34 ,  A61K9/70 ,  A61K31/165 ,  A61K31/216 ,  A61K31/335 ,  C07C59/31

摘要： Compounds represented by formulae I, II, III, and IV including pro-drugs for treprostinil and prostacyclin analogs. Uses include treatment of pulmonary hypertension (PH) or pulmonary arterial hypertension (PAH). The structures of the compounds can be adapted to the particular application for a suitable treatment dosage. Transdermal applications can be used.

公开(公告)号：US11220477B2

公开(公告)日：2022-01-11

申请号：US16418858

申请日：2019-05-21

申请人： The Regents of the University of California

发明人： Peter Walter ,  Carmela Sidrauski ,  Diego Acosta Alvear ,  Michelle R. Arkin ,  Christopher G. Wilson ,  Kean Hooi Ang ,  Brian R. Hearn ,  Punitha Vedantham ,  Adam R. Renslo ,  Mervyn Maze ,  Susana Vacas

IPC分类号： C07C235/14 ,  C07F7/08 ,  A61K31/4192 ,  C07D403/12 ,  C07D495/04 ,  C07C255/54 ,  C07C257/14 ,  C07C271/24 ,  C07C271/52 ,  C07C211/29 ,  C07C317/22 ,  C07C317/44 ,  C07C323/60 ,  C07C235/20 ,  C07C235/22 ,  C07C235/24 ,  A61K31/165

摘要： Provided herein, inter alia, are compounds and methods useful for modulating the translational effects of eIF2α phosphorylation, the Integrated Stress Response (ISR), and the unfolded protein response (UPR); for treating diseases; for increasing protein production, and for improving long-term memory.

公开(公告)号：US11046666B2

公开(公告)日：2021-06-29

申请号：US16569840

申请日：2019-09-13

申请人： CORSAIR PHARMA, INC.

发明人： Cyrus K. Becker ,  Meenakshi S. Venkatraman ,  Xiaoming Zhang

IPC分类号： C07D321/00 ,  C07D453/02 ,  C07D257/06 ,  C07C59/72 ,  C07C235/20 ,  A61K31/165 ,  C07C69/734 ,  A61K31/216 ,  A61K31/365 ,  C07D307/20 ,  A61K31/341 ,  A61K45/06 ,  A61K9/00 ,  C07D317/34 ,  C07C69/712 ,  C07D317/40 ,  C07C219/16 ,  C07D263/24 ,  C07D263/26 ,  C07D265/30 ,  C07D207/08 ,  C07D295/088 ,  C07D211/60 ,  C07D295/145 ,  C07C69/74 ,  C07C69/96 ,  A61K9/70

摘要： Compounds represented by formulae I, II, III, and IV including pro-drugs for treprostinil and prostacyclin analogs. Uses include treatment of pulmonary hypertension (PH) or pulmonary arterial hypertension (PAH). The structures of the compounds can be adapted to the particular application for a suitable treatment dosage. Transdermal applications can be used.

公开(公告)号：US10689407B2

公开(公告)日：2020-06-23

申请号：US15417924

申请日：2017-01-27

申请人： ACatechol, Inc.

发明人： Byung Jun Ahn ,  Bruce H. Lipshutz ,  Sam L. Nguyen ,  Roscoe Linstadt

IPC分类号： C07F9/12 ,  C09D7/63 ,  C09D5/00 ,  C07C205/43 ,  A61K6/20 ,  A61K6/62 ,  A61K6/65 ,  A61K6/78 ,  B05D3/10 ,  C07C69/01 ,  C07C205/42 ,  C07C235/06 ,  C07C271/16 ,  C07F7/08 ,  B05D3/00 ,  C07C235/20 ,  C07D217/16 ,  C07F9/62 ,  C08K5/13 ,  C08K5/107

摘要： In one embodiment, the present application discloses a photo-cleavable surface binding compound of the Formula I and Formula II: wherein the variables EG, EG1, SP1, SP2, SP3, Ar and BG are as defined herein. In another embodiment, the application discloses a method for forming a coating on a surface of a substrate using the surface binding compound.

公开(公告)号：US10428013B2

公开(公告)日：2019-10-01

申请号：US14129000

申请日：2012-06-25

申请人： Zhenpeng Yu ,  Gouping Wang ,  Zhen Zhang ,  Minyu Liu ,  Xiaoling Huang ,  Ying Liu ,  Lin Xiao ,  Li Cai ,  Xuejun Wu ,  Yifang Deng ,  Mianli Pan ,  Renhai Chen ,  Shenrong Tang ,  Quanhai Liu

发明人： Zhenpeng Yu ,  Gouping Wang ,  Zhen Zhang ,  Minyu Liu ,  Xiaoling Huang ,  Ying Liu ,  Lin Xiao ,  Li Cai ,  Xuejun Wu ,  Yifang Deng ,  Mianli Pan ,  Renhai Chen ,  Shenrong Tang ,  Quanhai Liu

IPC分类号： C07C235/84 ,  A61K31/165 ,  A61K31/166 ,  A61K31/222 ,  C07C325/02 ,  C07C235/20 ,  C07C235/26 ,  C07C251/24 ,  C07C231/02

摘要： Disclosed are amide compounds, preparation method and uses thereof, specifically, the compounds represented by formula I or pharmaceutically acceptable salts, wherein R1, R2, R3, R4, R5, Q, X and n are defined as in the description. Also disclosed are a method for preparing the compounds of formula I, a composition containing the compounds, and the uses of the same in the preparation of medicaments for regulating blood lipid and/or preventing gallstone. The compounds of formula I disclosed in the present invention have stability in vitro, good solubility in the pharmaceutical organic solvents and favorable bioavailability in animals.

公开(公告)号：US10087154B2

公开(公告)日：2018-10-02

申请号：US15664179

申请日：2017-07-31

申请人： Senomyx, Inc.

发明人： Catherine Tachdjian ,  Donald S. Karanewsky ,  Xiao-Qing Tang ,  Qing Chen ,  Peter Leeming ,  Tayyab Rashid ,  Daniel Levin

IPC分类号： C07D285/16 ,  C07C303/40 ,  C07C255/57 ,  C07C253/30 ,  C07C231/14 ,  C07C231/02 ,  C01B21/096 ,  C07C307/10 ,  C07C255/59 ,  C07C255/54 ,  C07C237/44 ,  C07C235/20

摘要： The present invention includes methods/processes and intermediates for preparing compounds having structural Formula (I): wherein X is alkyl, substituted alkyl, alkenyl, substituted alkenyl, heteroalkyl, substituted heteroalkyl, heteroalkenyl, or substituted heteroalkenyl.

公开(公告)号：US10053417B2

公开(公告)日：2018-08-21

申请号：US15806722

申请日：2017-11-08

申请人： THERAVANCE BIOPHARMA R&D IP, LLC

发明人： Erik Fenster ,  Melissa Fleury ,  Adam D. Hughes

IPC分类号： A61K31/40 ,  A61K31/42 ,  A61K31/44 ,  A61K31/197 ,  A61K31/397 ,  A61K31/5375 ,  C07D205/04 ,  C07D207/09 ,  C07D207/14 ,  C07D213/56 ,  C07C235/34 ,  C07D261/04 ,  C07D295/32 ,  C07C243/38 ,  A61K31/341 ,  A61K31/4409 ,  C07D213/86 ,  C07D213/87 ,  C07C235/80 ,  A61K31/4406 ,  A61K31/192 ,  C07D213/65 ,  A61K45/06 ,  A61K31/495 ,  A61K31/4015 ,  C07D307/68 ,  C07D213/61 ,  C07D211/62 ,  C07D211/60 ,  C07D211/48 ,  C07D211/46 ,  C07D211/42 ,  C07D211/38 ,  C07D211/22 ,  C07C243/32 ,  C07C243/24 ,  C07D493/10 ,  C07D207/16 ,  C07D207/12 ,  C07D207/08 ,  C07D265/30 ,  C07C235/78 ,  C07C235/74 ,  C07C235/20 ,  C07C235/12 ,  C07C233/56 ,  C07D261/02 ,  C07D239/36 ,  C07D405/06 ,  C07D401/04 ,  C07D233/06 ,  C07D309/08 ,  C07C259/04 ,  C07D213/75 ,  C07D491/107

CPC分类号： C07C243/38 ,  A61K31/192 ,  A61K31/197 ,  A61K31/341 ,  A61K31/397 ,  A61K31/40 ,  A61K31/4015 ,  A61K31/42 ,  A61K31/44 ,  A61K31/4406 ,  A61K31/4409 ,  A61K31/495 ,  A61K31/5375 ,  A61K45/06 ,  C07C233/56 ,  C07C235/12 ,  C07C235/20 ,  C07C235/34 ,  C07C235/74 ,  C07C235/78 ,  C07C235/80 ,  C07C243/24 ,  C07C243/32 ,  C07C259/04 ,  C07C2601/08 ,  C07C2601/16 ,  C07D205/04 ,  C07D207/08 ,  C07D207/09 ,  C07D207/12 ,  C07D207/14 ,  C07D207/16 ,  C07D211/22 ,  C07D211/38 ,  C07D211/42 ,  C07D211/46 ,  C07D211/48 ,  C07D211/60 ,  C07D211/62 ,  C07D213/56 ,  C07D213/61 ,  C07D213/65 ,  C07D213/75 ,  C07D213/86 ,  C07D213/87 ,  C07D233/06 ,  C07D239/36 ,  C07D261/02 ,  C07D261/04 ,  C07D265/30 ,  C07D295/32 ,  C07D307/68 ,  C07D309/08 ,  C07D401/04 ,  C07D405/06 ,  C07D491/107 ,  C07D493/10

摘要： In one aspect, the invention relates to compounds having the formula: where R1-R5 and X are as defined in the specification, or a pharmaceutically acceptable salt thereof. These compounds have neprilysin inhibition activity. In another aspect, the invention relates to pharmaceutical compositions comprising such compounds; methods of using such compounds; and processes and intermediates for preparing such compounds.

公开(公告)号：US10010518B2

公开(公告)日：2018-07-03

申请号：US15154631

申请日：2016-05-13

申请人： Insmed Incorporated

发明人： Vladimir Malinin ,  Walter Perkins ,  Franziska Leifer ,  Donna Konicek ,  Zhili Li ,  Adam Plaunt

IPC分类号： A61K31/225 ,  C07C69/736 ,  C07C69/753 ,  C07C235/22 ,  C07C235/20 ,  A61K31/165 ,  A61K31/216 ,  A61K47/06 ,  C07C69/712 ,  A61K9/00 ,  A61K47/60 ,  A61K47/54

CPC分类号： C07C69/734 ,  A61K9/0019 ,  A61K9/0043 ,  A61K9/0053 ,  A61K9/0073 ,  A61K9/0075 ,  A61K9/0078 ,  A61K9/10 ,  A61K9/14 ,  A61K9/51 ,  A61K31/165 ,  A61K31/216 ,  A61K31/225 ,  A61K47/06 ,  A61K47/14 ,  A61K47/24 ,  A61K47/28 ,  A61K47/34 ,  A61K47/543 ,  A61K47/544 ,  A61K47/60 ,  A61M15/0085 ,  A61M15/009 ,  A61M16/14 ,  A61M2202/064 ,  A61P9/12 ,  A61P11/00 ,  C07C69/712 ,  C07C69/736 ,  C07C69/753 ,  C07C235/20 ,  C07C235/22 ,  C07C2601/18 ,  C07C2603/14

摘要： Prostacyclin compounds and compositions comprising the same are provided herein. Specifically, prostacyclin compounds comprising treprostinil covalently linked to a linear C5-C18 alkyl, branched C5-C18 alkyl, linear C2-C18 alkenyl, branched C3-C18 alkenyl, aryl, aryl-C1-C18 alkyl or an amino acid or a peptide (e.g., dipeptide, tripeptide, tetrapeptide) are described. The linkage, in one embodiment, is via a carbamate, amide or ester bond. Prostacyclin compounds provided herein can also include at least one hydrogen atom substituted with at least one deuterium atom. Methods for treating pulmonary hypertension (e.g., pulmonary arterial hypertension) and portopulmonary hypertension are also provided.