公开(公告)号：US20210363113A1

公开(公告)日：2021-11-25

申请号：US17047422

申请日：2019-04-17

Applicant: THE REGENTS OF THE UNIVERSITY OF MICHIGAN ,  THE REGENTS OF THE UNIVERSITY OF CALIFORNIA

Inventor： Michael Holinstat ,  Reheman Adili ,  Andrew White ,  Theodore R. Holman

IPC: C07D249/12 ,  A61P7/02 ,  C07D403/12

Abstract: Disclosed herein are small molecule inhibitors of platelet function, and methods of using the small molecules to treat diseases, such as platelet hemostasis and thrombosis. In particular, disclosed herein are compounds of Formula (I) and pharmaceutically acceptable salts thereof: wherein the substituents are as described.

公开(公告)号：US20210219551A1

公开(公告)日：2021-07-22

申请号：US16945369

申请日：2020-07-31

Applicant: Vanderbilt University

Inventor： Laurence Zwiebel ,  Gregory M. Pask ,  David C. Rinker ,  Ian M. Romaine ,  Gary A. Sulikowski ,  Paul R. Reid ,  Alex G. Waterson ,  Kwangho Kim ,  Patrick L. Jones ,  Robert W. Taylor

IPC: A01N43/653 ,  A01N43/82 ,  A01N43/78 ,  A01N43/90 ,  A01N25/08 ,  A01N47/16 ,  A01N47/18 ,  A01N53/00 ,  C07D249/12 ,  C07D401/04 ,  C07D401/14 ,  C07D403/04 ,  C07D405/04 ,  C07D405/06 ,  C07D405/14 ,  C07D409/04 ,  C07D409/14 ,  C07D413/14 ,  C07D471/04 ,  C07D491/048 ,  C07D491/052 ,  C07D491/056 ,  C07D513/04

Abstract: In one aspect, the invention relates to chemical modulators of insect olfactory receptors. In particular, compounds and compositions are provided that can inhibit sensory (e.g., host targeting) functions in airborne insects such as mosquitos. Methods of employing such agents, and articles incorporating the same, are also provided. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.

公开(公告)号：US11008294B2

公开(公告)日：2021-05-18

申请号：US16663054

申请日：2019-10-24

Applicant: Neuropore Therapies, Inc.

Inventor： Wolfgang J. Wrasidlo ,  Emily M. Stocking ,  Srinivasa Reddy Natala ,  Diana Luz Price

IPC: C07D249/12 ,  A61P25/28 ,  A61K9/10 ,  A61P3/00 ,  C07D243/10 ,  A61K31/18

Abstract: The present disclosure relates to substituted phenyl sulfonyl phenyl triazole thiones, pharmaceutical compositions containing them, and methods of using them.

公开(公告)号：US20210079017A1

公开(公告)日：2021-03-18

申请号：US16947214

申请日：2020-07-23

Applicant: THERAVANCE BIOPHARMA R&D IP, LLC

Inventor： Roland Gendron ,  Melissa Fleury ,  Adam D. Hughes

IPC: C07D498/08 ,  C07D213/81 ,  C07D231/14 ,  C07D233/26 ,  C07D233/90 ,  C07D237/24 ,  C07D239/34 ,  C07D241/24 ,  C07D249/04 ,  C07D249/10 ,  C07D249/18 ,  C07D257/04 ,  C07D261/20 ,  C07D263/34 ,  C07D271/06 ,  C07D277/56 ,  C07D307/68 ,  C07D333/70 ,  C07D401/04 ,  C07D401/06 ,  C07D403/04 ,  C07D403/06 ,  C07D405/12 ,  C07D409/06 ,  C07D471/04 ,  C07D498/04 ,  C07D261/18 ,  C07D207/34 ,  C07D239/36 ,  C07D413/06 ,  A61K31/42 ,  A61K31/422 ,  A61K31/5377 ,  A61K45/06 ,  C07D413/04 ,  C07D413/12 ,  C07D213/79 ,  C07D213/80 ,  C07D237/04 ,  C07D249/08 ,  C07D249/12 ,  C07D261/12 ,  C07D263/56 ,  C07D277/46 ,  C07D333/40

Abstract: In one aspect, the invention relates to compounds having the formula: where R1-R6, a, b, 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：US20210072254A1

公开(公告)日：2021-03-11

申请号：US17080373

申请日：2020-10-26

Applicant: Dana-Farber Cancer Institute, Inc.

Inventor： Jarrod A Marto ,  Scott B Ficarro ,  Guillaume Adelmant

IPC: G01N33/68 ,  C07C225/14 ,  C07C233/33 ,  C07C255/60 ,  C07C321/04 ,  C07C321/14 ,  C07D209/34 ,  C07D211/70 ,  C07D219/04 ,  C07D233/88 ,  C07D241/04 ,  C07D249/12 ,  C07D265/30 ,  C07D265/34 ,  C07D265/36 ,  C07D295/185 ,  C07D307/54 ,  C07D401/04 ,  C07D401/12 ,  C07D401/14 ,  C07D403/04 ,  C07D403/12 ,  C07D471/04 ,  C07D487/04 ,  C07D498/06

Abstract: The present application relates to mass spectrometry methods for use in identifying proteins or other biomolecules which are bound irreversibly by test compounds.

公开(公告)号：US20210032211A1

公开(公告)日：2021-02-04

申请号：US16962834

申请日：2019-01-18

Applicant: FMC Corporation

Inventor： Wuqiang TU ,  Bolin FAN ,  Guanghui LI

IPC: C07D249/12 ,  B01J31/02

Abstract: Disclosed are processes for the synthesis of sulfentrazone, which provide a high conversion of sulfentrazone amine and high yield of the final sulfentrazone product.

公开(公告)号：US10899719B2

公开(公告)日：2021-01-26

申请号：US16721020

申请日：2019-12-19

Applicant: YUHAN CORPORATION

Inventor： Tae Dong Han ,  Hee Jae Tak ,  Eun Kyung Kim ,  Su Bin Choi ,  Dong Hoon Kim ,  Sol Park ,  Eun Hye Jung ,  Hyun Ho Choi ,  Tae Wang Kim ,  Mi Kyeong Ju ,  Na Ry Ha

IPC: C07D403/04 ,  C07D249/08 ,  C07D401/04 ,  C07D417/04 ,  C07D409/10 ,  C07D405/10 ,  C07D407/14 ,  C07D401/10 ,  C07D403/10 ,  C07D401/14 ,  C07D405/14 ,  C07D417/14 ,  C07D413/14 ,  C07D413/10 ,  C07D417/10 ,  C07D249/12 ,  C07D403/14

Abstract: The present technology provides aryl or heteroaryl triazolone derivatives or pharmaceutically acceptable salts thereof, preparation processes thereof, pharmaceutical compositions comprising the same, and the use thereof. The aryl or heteroaryl triazolone derivatives or their pharmaceutically acceptable salts exhibit selective inhibitory activity on VAP-1 and therefore can be usefully applied, e.g., for the treatment and prophylaxis of nonalcoholic hepatosteatosis (NASH).

公开(公告)号：US10829438B2

公开(公告)日：2020-11-10

申请号：US16392920

申请日：2019-04-24

Applicant: THERAVANCE BIOPHARMA R&D IP, LLC

Inventor： Melissa Fleury ,  Adam D. Hughes

IPC: C07C229/22 ,  C07D249/18 ,  A61K31/4192 ,  A61K45/06 ,  C07D231/20 ,  A61K31/415 ,  C07D405/12 ,  A61K31/4155 ,  A61K31/4439 ,  C07D401/04 ,  C07D405/14 ,  C07D231/14 ,  C07D261/18 ,  C07D257/04 ,  C07D249/04 ,  C07D249/12 ,  A61K31/41 ,  A61K31/675 ,  C07F9/6503 ,  C07D231/18 ,  C07D253/08 ,  C07C271/22 ,  C07D207/26 ,  C07D263/38 ,  A61K31/42 ,  A61K31/4196

Abstract: In one aspect, the invention relates to compounds having the formula XII: where Ra, Rb, R2, R7, and X are as defined in the specification, or a pharmaceutically acceptable salt thereof. The compounds described herein are prodrugs of compounds having neprilysin inhibition activity. In another aspect, the invention relates to pharmaceutical compositions comprising these compounds; methods of using these compounds; and processes and intermediates for preparing these compounds.

公开(公告)号：US20200347022A1

公开(公告)日：2020-11-05

申请号：US16853604

申请日：2020-04-20

Applicant: Sanford Burnham Prebys Medical Discovery Institute

Inventor： Takuya IKEDA ,  Yoshiyuki KOBAYASHI ,  Naoki MIYOSHI ,  Osamu SUZUKI ,  Takahiro NAGAYAMA ,  Takashi TSUJI ,  Layton H. SMITH ,  Anthony B. PINKERTON

IPC: C07D249/12 ,  G16B25/00 ,  G16C99/00 ,  C07D403/12 ,  C07D403/06 ,  A61P9/10 ,  A61P3/10 ,  A61P9/12 ,  A61P13/12 ,  A61P9/04 ,  C07D401/04 ,  C07D405/04 ,  C07D405/14 ,  C07D409/04 ,  C07D409/14 ,  C07D413/14 ,  C07D417/14 ,  C07D487/04

Abstract: The present invention relates to a novel azole derivative as an apelin receptor agonist and a method for treating cardiovascular disease, diabetic disease, renal disease, hypertension, and arteriosclerosis, etc., using the same. The present invention provides a compound represented by formula (I) or a pharmacologically acceptable salt thereof wherein X represents —N═ or —CH═, X2 represents —CH═ or —N═, R1 and R2 each represent a C1 to C6 alkoxy group or the like, R3 represents a heteroaryl group (the heteroaryl group is optionally substituted by a methyl group or the like) or the like, and R4 represents a C1 to C6 alkylthio group or a C2 to C6 alkenyl group (the C1 to C6 alkylthio group and the C2 to C6 alkenyl group are each optionally substituted by one carboxy group or the like) or the like.

公开(公告)号：US10821100B2

公开(公告)日：2020-11-03

申请号：US16423992

申请日：2019-05-28

Applicant: Glenmark Pharmaceuticals S.A.

Inventor： Laxmikant A. Gharat ,  Nagarajan Muthukaman ,  Neelima Khairatkar-Joshi ,  Vidya G. Kattige

IPC: A61K31/4196 ,  C07D401/04 ,  C07D401/10 ,  C07D403/04 ,  C07D403/10 ,  C07D403/12 ,  C07D405/12 ,  C07D409/14 ,  C07D413/10 ,  C07D417/10 ,  C07D417/12 ,  A61K31/4245 ,  A61K31/428 ,  A61K31/433 ,  A61K31/4439 ,  A61K31/5377 ,  C07D249/12 ,  C07D413/12 ,  A61K31/422

Abstract: The present disclosure is directed to compounds of formula (I), and pharmaceutically acceptable salts thereof, as mPGES-1 inhibitors. These compounds are inhibitors of the microsomal prostaglandin E synthase-1 (mPGES-1) enzyme and are therefore useful in the treatment of pain and/or inflammation from a variety of diseases or conditions, such as asthma, osteoarthritis, rheumatoid arthritis, acute or chronic pain and neurodegenerative diseases.