公开(公告)号：US12122788B2

公开(公告)日：2024-10-22

申请号：US18093142

申请日：2023-01-04

Applicant: Vertex Pharmaceuticals Incorporated

Inventor： Paul Angell ,  John E. Cochran ,  Benjamin J. Littler ,  David Siesel ,  Armando Urbina ,  Corey Don Anderson ,  Jeremy J. Clemens ,  Thomas Cleveland ,  Timothy Richard Coon ,  Bryan Frieman ,  Peter Grootenhuis ,  Sara Sabina Hadida Ruah ,  Jason McCartney ,  Mark Thomas Miller ,  Prasuna Paraselli ,  Fabrice Pierre ,  Sara E. Swift ,  Jinglan Zhou

IPC: C07D513/22 ,  C07D207/08 ,  C07D213/71 ,  C07D213/82 ,  C07D231/20 ,  C07D401/04 ,  C07D401/14

CPC classification number: C07D513/22 ,  C07D207/08 ,  C07D213/71 ,  C07D213/82 ,  C07D231/20 ,  C07D401/04 ,  C07D401/14

Abstract: The disclosure provides processes for synthesizing Compound I, and pharmaceutically acceptable salts thereof.

公开(公告)号：US20240300960A1

公开(公告)日：2024-09-12

申请号：US18649712

申请日：2024-04-29

Applicant: Merck Sharp & Dohme LLC

Inventor： Feng XU ,  Zhuqing LIU ,  Richard DESMOND ,  Jeonghan PARK ,  Alexei KALININ ,  Birgit KOSJEK ,  Hallena STROTMAN ,  Hongmei LI ,  Johannah MONCECCHI

IPC: C07D487/04 ,  C07C215/30 ,  C07D207/08 ,  C07D207/12 ,  C12P17/10

CPC classification number: C07D487/04 ,  C07C215/30 ,  C07D207/08 ,  C07D207/12 ,  C12P17/10

Abstract: The application is directed to efficient and economical processes as described in more detail below for the preparation of the beta 3 agonists of the formula of I-7 and intermediate compounds that can be used for making these agonists. The present disclosure relates to a process for making beta-3 agonists and intermediates using ketoreductase (KRED) biocatalyst enzymes and methods of using the biocatalysts.

公开(公告)号：US20240002372A1

公开(公告)日：2024-01-04

申请号：US18254405

申请日：2021-11-24

Applicant: REZUBIO PHARMACEUTICALS CO., LTD

Inventor： Yusheng XIONG ,  Hongping GUAN

IPC: C07D413/12 ,  C07D207/12 ,  C07D207/08

CPC classification number: C07D413/12 ,  C07D207/12 ,  C07D207/08

Abstract: Compounds shown in Formula (I), pharmaceutical compositions, and methods of using related to muscarinic acetylcholine receptors. The compounds herein are typically muscarinic acetylcholine receptor antagonists, such as M3 antagonists, which can be used for treating a variety of disorders, conditions or diseases such as hyperhidrosis.

公开(公告)号：US20230399343A1

公开(公告)日：2023-12-14

申请号：US18093142

申请日：2023-01-04

Applicant: Vertex Pharmaceuticals Incorporated

Inventor： Paul Angell ,  John E. Cochran ,  Benjamin J. Littler ,  David Siesel ,  Armando Urbina ,  Corey Don Anderson ,  Jeremy J. Clemens ,  Thomas Cleveland ,  Timothy Richard Coon ,  Bryan Frieman ,  Peter Grootenhuis ,  Sara Sabina Hadida Ruah ,  Jason McCartney ,  Mark Thomas Miller ,  Prasuna Paraselli ,  Fabrice Pierre ,  Sara E. Swift ,  Jinglan Zhou

IPC: C07D513/22 ,  C07D207/08 ,  C07D213/71 ,  C07D213/82 ,  C07D231/20 ,  C07D401/04 ,  C07D401/14

CPC classification number: C07D513/22 ,  C07D207/08 ,  C07D213/71 ,  C07D213/82 ,  C07D231/20 ,  C07D401/04 ,  C07D401/14

Abstract: The disclosure provides processes for synthesizing Compound I, and pharmaceutically acceptable salts thereof.

公开(公告)号：US20230348369A1

公开(公告)日：2023-11-02

申请号：US17923167

申请日：2021-05-05

Applicant: Cytokinetics, Inc.

Inventor： Antonio ROMERO ,  Aroop CHANDRA ,  Christopher EVANS ,  Minxing SHEN

IPC: C07C275/26 ,  C07D401/12 ,  C07D211/58 ,  C07D213/40 ,  C07D231/12 ,  C07D261/08 ,  C07D211/26 ,  C07D413/12 ,  C07D213/74 ,  C07D221/20 ,  C07D213/38 ,  C07C275/18 ,  C07D205/12 ,  C07D207/06 ,  C07D205/04 ,  C07D401/04 ,  C07D295/16 ,  C07D215/08 ,  C07D217/04 ,  C07D209/44 ,  C07D209/08 ,  C07D307/22 ,  C07D209/54 ,  C07D265/36 ,  C07D471/04 ,  C07D305/08 ,  C07C311/13 ,  C07C311/20 ,  C07D241/04 ,  C07D215/06 ,  C07D403/12 ,  C07D231/56 ,  C07D401/06 ,  C07D403/04 ,  C07D403/10 ,  C07D213/82 ,  C07D213/81 ,  C07C317/32 ,  C07D213/87 ,  C07D295/182 ,  C07D207/08 ,  C07D241/08 ,  C07D207/267 ,  C07D249/06 ,  C07D335/02 ,  C07D231/14 ,  C07D309/08 ,  C07D211/78 ,  C07D213/75 ,  C07D213/56 ,  C07D405/06 ,  C07D413/06 ,  C07D271/10 ,  C07D263/56 ,  C07D241/12 ,  C07D249/08 ,  C07D239/26 ,  C07D213/68 ,  C07D213/65 ,  C07C317/30 ,  C07D213/71 ,  C07D401/14

CPC classification number: C07C275/26 ,  C07D401/12 ,  C07D211/58 ,  C07D213/40 ,  C07D231/12 ,  C07D261/08 ,  C07D211/26 ,  C07D413/12 ,  C07D213/74 ,  C07D221/20 ,  C07D213/38 ,  C07C275/18 ,  C07D205/12 ,  C07D207/06 ,  C07D205/04 ,  C07D401/04 ,  C07D295/16 ,  C07D215/08 ,  C07D217/04 ,  C07D209/44 ,  C07D209/08 ,  C07D307/22 ,  C07D209/54 ,  C07D265/36 ,  C07D471/04 ,  C07D305/08 ,  C07C311/13 ,  C07C311/20 ,  C07D241/04 ,  C07D215/06 ,  C07D403/12 ,  C07D231/56 ,  C07D401/06 ,  C07D403/04 ,  C07D403/10 ,  C07D213/82 ,  C07D213/81 ,  C07C317/32 ,  C07D213/87 ,  C07D295/182 ,  C07D207/08 ,  C07D241/08 ,  C07D207/267 ,  C07D249/06 ,  C07D335/02 ,  C07D231/14 ,  C07D309/08 ,  C07D211/78 ,  C07D213/75 ,  C07D213/56 ,  C07D405/06 ,  C07D413/06 ,  C07D271/10 ,  C07D263/56 ,  C07D241/12 ,  C07D249/08 ,  C07D239/26 ,  C07D213/68 ,  C07D213/65 ,  C07C317/30 ,  C07D213/71 ,  C07D401/14 ,  C07C2602/50 ,  C07C2601/14 ,  C07C2601/04 ,  C07C2601/02 ,  C07C2602/08 ,  C07C2602/10 ,  C07B2200/05

Abstract: Provided are compounds of Formula (II): or a pharmaceutically acceptable salt thereof, wherein R1, n, and Y1 are as defined herein. Also provided is a pharmaceutically acceptable composition comprising a compound of Formula (II), or a pharmaceutically acceptable salt thereof. Also provided are methods of using a compound of Formula (II), or a pharmaceutically acceptable salt thereof.

公开(公告)号：US20230331691A1

公开(公告)日：2023-10-19

申请号：US17965914

申请日：2022-10-14

Applicant: CORSAIR PHARMA, INC.

Inventor： Cyrus K. BECKER ,  Meenakshi S. VENKATRAMAN ,  Xiaoming ZHANG

IPC: C07D321/00 ,  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 ,  C07D453/02 ,  C07D257/06 ,  C07D263/24 ,  C07D263/26 ,  C07D265/30 ,  C07D207/08 ,  C07D295/088 ,  C07D211/60 ,  C07D295/145 ,  C07C59/72 ,  C07C69/74 ,  C07C69/96 ,  A61K9/70

CPC classification number: C07D321/00 ,  A61K9/0014 ,  A61K9/7023 ,  A61K31/165 ,  A61K31/216 ,  A61K31/341 ,  A61K31/365 ,  A61K45/06 ,  C07C59/72 ,  C07C69/712 ,  C07C69/734 ,  C07C69/74 ,  C07C69/96 ,  C07C219/16 ,  C07C235/20 ,  C07D207/08 ,  C07D211/60 ,  C07D257/06 ,  C07D263/24 ,  C07D263/26 ,  C07D265/30 ,  C07D295/088 ,  C07D295/145 ,  C07D307/20 ,  C07D317/34 ,  C07D317/40 ,  C07D453/02 ,  C07C2601/02 ,  C07C2601/08 ,  C07C2601/14 ,  C07C2602/42 ,  C07C2603/14

Abstract: 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：US11739104B2

公开(公告)日：2023-08-29

申请号：US16964621

申请日：2019-01-25

Applicant: YALE UNIVERSITY

Inventor： Anna Pyle ,  Olga Fedorova ,  Erik Gunnar Jagdmann ,  Michael Van Zandt ,  Lin Yuan ,  Albert DeBerardinis

IPC: C07D307/80 ,  C07F5/02 ,  A61P31/10 ,  C07C49/84 ,  C07C233/65 ,  C07C233/73 ,  C07C243/38 ,  C07D207/08 ,  C07D211/16 ,  C07D217/04 ,  C07D233/64 ,  C07D239/26 ,  C07D277/24 ,  C07D277/26 ,  C07D277/66 ,  C07D295/192 ,  C07D295/215 ,  C07D307/52 ,  C07D307/83 ,  C07D405/04 ,  C07D405/12 ,  C07D413/04

CPC classification number: C07F5/027 ,  A61P31/10 ,  C07C49/84 ,  C07C233/65 ,  C07C233/73 ,  C07C243/38 ,  C07D207/08 ,  C07D211/16 ,  C07D217/04 ,  C07D233/64 ,  C07D239/26 ,  C07D277/24 ,  C07D277/26 ,  C07D277/66 ,  C07D295/192 ,  C07D295/215 ,  C07D307/52 ,  C07D307/80 ,  C07D307/83 ,  C07D405/04 ,  C07D405/12 ,  C07D413/04

Abstract: The present invention provides compositions and methods for inhibiting group II intron splicing for treating or preventing a disease or disorder associated with an organism harboring an active group II intron. The present invention also provides compositions and methods for inhibiting group II intron splicing for inhibiting, preventing or reducing growth of an organism harboring an active group II intron.

公开(公告)号：US20230192606A1

公开(公告)日：2023-06-22

申请号：US17996097

申请日：2021-04-16

Applicant: Baylor College of Medicine

Inventor： Martin Matzuk ,  Surendra Dawadi ,  Melek Ucisik ,  John Faver ,  Kurt Bohren ,  Feng Li

IPC: C07D207/08 ,  C07D405/12 ,  C07D311/68 ,  C07C279/14

CPC classification number: C07D207/08 ,  C07D405/12 ,  C07D311/68 ,  C07C279/14

Abstract: Novel direct thrombin inhibitors are provided herein, along with methods for their use as anticoagulants. The direct thrombin inhibitors described herein are useful in treating and/or preventing thromboembolism and bleeding or clotting disorders. Also provided herein are methods for inhibiting thrombin in a cell using the compounds and compositions described herein.

公开(公告)号：US11661580B2

公开(公告)日：2023-05-30

申请号：US17006338

申请日：2020-08-28

Applicant: Cassava Science, Inc.

Inventor： Hoau-Yan Wang ,  Lindsay Burns Barbier

IPC: C12N5/079 ,  C07D265/30 ,  C07D211/14 ,  C07D277/04 ,  C07D295/088 ,  C07D205/04 ,  C07D491/056 ,  C07D498/10 ,  C07D217/04 ,  C07D471/10 ,  C07D491/04 ,  C07D207/08 ,  C07D265/36 ,  C07D277/02 ,  C07D279/12 ,  C07D295/08 ,  C07D211/74 ,  G01N33/50 ,  G01N33/68 ,  G01N33/94

CPC classification number: C12N5/0622 ,  C07D205/04 ,  C07D207/08 ,  C07D211/14 ,  C07D211/74 ,  C07D217/04 ,  C07D265/30 ,  C07D265/36 ,  C07D277/02 ,  C07D277/04 ,  C07D279/12 ,  C07D295/08 ,  C07D295/088 ,  C07D471/10 ,  C07D491/04 ,  C07D491/056 ,  C07D498/10 ,  G01N33/50 ,  G01N33/6896 ,  G01N33/94 ,  G01N2333/70571 ,  G01N2800/2821 ,  G01N2800/52

Abstract: A method of inhibiting phosphorylation of the tau protein and/or a TLR4-mediated immune response is disclosed. The method contemplates administering to cells in recognized need thereof such as cells of the central nervous system an effective amount of a of a compound or a pharmaceutically acceptable salt thereof that binds to a pentapeptide of filamin A (FLNA) of SEQ ID NO: 1, and contains at least four of the six pharmacophores of FIGS. 35-40.

公开(公告)号：US20230142285A1

公开(公告)日：2023-05-11

申请号：US17604818

申请日：2020-12-17

Applicant: Janssen Pharmaceutica NV

Inventor： Wei CAI ,  Xuedong DAI ,  Oliver Alexis Georges QUEROLLE ,  Johannes Wilhelmus John F. THURING ,  Yingtao LIU ,  Lianzhu LIU ,  Yanping XU ,  Liqiang FU ,  Ming LI ,  Lichao FANG ,  Xianguin DENG ,  Qiwu ZHAO ,  Kangying LI ,  Alicia Tee Fuay NG ,  Nicolas Freddy J. DARVILLE ,  Edward CLEATOR ,  Gregor Thomas URBANIETZ ,  William Marc MATON ,  Vineet PANDA

IPC: C07D487/10 ,  C07D207/08 ,  A61P35/00

CPC classification number: C07D487/10 ,  C07D207/08 ,  A61P35/00

Abstract: The present invention relates to pharmaceutical agents useful for therapy and/or prophylaxis in a mammal, pharmaceutical composition comprising such compounds, and their use as menin/MLL protein/protein interaction inhibitors, useful for treating diseases such as cancer, including but not limited to leukemia, myelodysplastic syndrome (MDS), and myeloproliferative neoplasms (MPN); and diabetes.