公开(公告)号：US20210228563A1

公开(公告)日：2021-07-29

申请号：US17228590

申请日：2021-04-12

Applicant: Belite Bio, Inc.

Inventor： Yu-Hsin Tom LIN ,  Cheng-Chi Irene WANG

IPC: A61K31/4545 ,  A61K31/5383 ,  A61K31/5365 ,  A61K31/519 ,  A61K9/00 ,  A61P3/04 ,  A61P3/10 ,  A61K31/4985

Abstract: Provided herein are heterocyclic derivative compounds and pharmaceutical compositions comprising said compounds that are useful for the treatment of retinal binding protein (RBP4) related diseases, such as obesity and the like.

公开(公告)号：US11071721B2

公开(公告)日：2021-07-27

申请号：US15828271

申请日：2017-11-30

Applicant: Genentech, Inc.

Inventor： Snahel Patel ,  Gregory Hamilton ,  Guiling Zhao ,  Huifen Chen

IPC: C07D471/04 ,  A61K31/16 ,  A61P9/10 ,  C07D519/00 ,  A61P9/00 ,  A61P29/00 ,  A61P43/00 ,  A61K31/396 ,  A61K31/397 ,  A61K31/4025 ,  A61K31/416 ,  A61K31/4196 ,  A61K31/44 ,  A61K31/5383 ,  C07D487/04 ,  C07D491/04 ,  C07D491/048

Abstract: The invention provides novel compounds having the general formula I: wherein R1, R2, the A ring and the B ring are as described herein, pharmaceutical compositions including the compounds and methods of using the compounds.

公开(公告)号：US11053245B2

公开(公告)日：2021-07-06

申请号：US14394469

申请日：2013-04-14

Applicant: INTRA-CELLULAR THERAPIES, INC.

Inventor： Sharon Mates ,  Robert Davis ,  Kimberly Vanover

IPC: C07D471/14 ,  A61K45/06 ,  A61K31/5383 ,  A61K31/4985 ,  C07D471/16 ,  A61K31/445

Abstract: Use of particular substituted heterocycle fused gamma-carboline compounds as pharmaceuticals for the treatment of agitation, aggressive behaviors, posttraumatic stress disorder or impulse control disorders.

公开(公告)号：US11034692B1

公开(公告)日：2021-06-15

申请号：US16542129

申请日：2019-08-15

Applicant: Genentech, Inc.

Inventor： Bryan Chan ,  Blake Daniels ,  Joy Drobnick ,  Lewis Gazzard ,  Timothy Heffron ,  Malcolm Huestis ,  Jun Liang ,  Sushant Malhotra ,  Rohan Mendonca ,  Naomi Rajapaksa ,  Michael Siu ,  Craig Stivala ,  John Tellis ,  Weiru Wang ,  BinQing Wei ,  Aihe Zhou ,  Matthew W. Cartwright ,  Emanuela Gancia ,  Graham Jones ,  Michael Lainchbury ,  Andrew Madin ,  Eileen Seward ,  David Favor ,  Kin Chiu Fong ,  Andrew Good ,  Yonghan Hu ,  Baihua Hu ,  Aijun Lu

IPC: C07D471/04 ,  A61K45/06 ,  A61P35/00 ,  A61K31/444 ,  A61K31/4375 ,  A61K31/506 ,  C07D519/00 ,  A61K31/4545 ,  A61K31/4725 ,  A61K31/5383 ,  A61K31/496 ,  A61K31/5377 ,  A61K31/5025 ,  A61K31/551 ,  A61K31/55

Abstract: Naphthyridine compounds and their use as inhibitors of HPK1 are described. The compounds are useful in treating HPK1-dependent disorders and enhancing an immune response. Also described are methods of inhibiting HPK1, methods of treating HPK1-dependent disorders, methods for enhancing an immune response, and methods for preparing the naphthyridine compounds.

公开(公告)号：US11007186B2

公开(公告)日：2021-05-18

申请号：US16272911

申请日：2019-02-11

Applicant: Belite Bio, Inc

Inventor： Yu-Hsin Tom Lin ,  Cheng-Chi Irene Wang

IPC: A61K31/4545 ,  A61K31/5383 ,  A61P3/04 ,  A61P3/10 ,  A61K31/5365 ,  A61K31/519 ,  A61K9/00 ,  A61K31/4985

Abstract: Provided herein are heterocyclic derivative compounds and pharmaceutical compositions comprising said compounds that are useful for the treatment of retinal binding protein (RBP4) related diseases, such as obesity and the like.

公开(公告)号：US10987357B2

公开(公告)日：2021-04-27

申请号：US16250520

申请日：2019-01-17

Applicant: Horizon Orphan, LLC

Inventor： Mark W. Surber ,  Keith A. Bostian ,  Michael N. Dudley ,  Olga Rodny ,  David C. Griffith

IPC: A61K31/5383 ,  A61K47/02 ,  A61K9/00 ,  A61K9/51

Abstract: Disclosed herein are formulations of fluoroquinolones suitable for aerosolization and use of such formulations for aerosol administration of fluoroquinolone antimicrobials for the treatment of pulmonary bacterial infections. In particular, inhaled levofloxacin specifically formulated and delivered for bacterial infections of the lungs is described. Methods include inhalation protocols and manufacturing procedures for production and use of the compositions described.

公开(公告)号：US20210115044A1

公开(公告)日：2021-04-22

申请号：US17048811

申请日：2019-04-22

Applicant: Merck Sharp & Dohme Corp.

Inventor： Tao Yu ,  James M. Apgar ,  Alan Whitehead ,  Yonglian Zhang ,  Zhiyong Hu ,  Valerie W. Shurtleff ,  John A. McCauley ,  Izzat T. Raheem

IPC: C07D471/16 ,  A61K31/4985 ,  A61P31/18 ,  A61K31/52 ,  A61K31/435 ,  A61K31/5383 ,  A61K31/506 ,  A61K31/513 ,  A61K31/685 ,  A61K31/427

Abstract: The present invention relates to Tricyclic Heterocycle Compounds of Formula (I): (I) and pharmaceutically acceptable salts or prodrug thereof, wherein R1, R2, R3, R4, R5, R6 and n are as defined herein. The present invention also relates to compositions comprising at least one Tricyclic Heterocycle Compound, and methods of using the Tricyclic Heterocycle Compounds for treating or preventing HIV infection in a subject.

公开(公告)号：US20210069106A1

公开(公告)日：2021-03-11

申请号：US16963678

申请日：2019-01-24

Applicant: Novartis AG

Inventor： Yoen-Ju SON ,  Daniel HUANG ,  Danforth MILLER ,  Jeffry G. WEERS

IPC: A61K9/00 ,  A61K9/16 ,  C07K16/24 ,  A61K31/5383 ,  A61K31/7036 ,  A61K31/137 ,  A61M15/00

Abstract: The present invention comprises methods and formulations to increase drug payload, especially in regard to a receptacle-based, inhalation dosed, dry powder therapeutic, wherein the methods and formulations are characterized by a high product density, as well as a high TLD per receptacle, while maintaining highly efficient aerosol performance from the device. Embodiments of the present invention comprise a spray-dried pharmaceutical powder comprising particles deliverable from a dry powder inhaler, the composition comprising active agent, and a shell-forming excipient, wherein the powder is characterized by a product density greater than 50 mg/ml.

公开(公告)号：US20210052549A1

公开(公告)日：2021-02-25

申请号：US16492546

申请日：2018-03-07

Applicant: Marc Childs ,  Jacque Sauzieres ,  Olivier Petitjean ,  Guillaume Petitjean ,  Elodie Petitjean ,  Grégoire Petitjean

Inventor： Olivier Petitjean ,  Guillaume Petitjean ,  Elodie Petitjean ,  Grégoire Petitjean

IPC: A61K31/385 ,  A61K45/06 ,  A61K31/4709 ,  A61K47/55 ,  A61K31/5383 ,  A61K31/496 ,  A61K31/4468 ,  A61K31/445 ,  A61K31/454 ,  A61K31/4439 ,  A61K31/222 ,  A61K31/5415 ,  A61P9/06

Abstract: A method of treating a subject for reducing the risk of QT space prolongation associated with the intake of a drug known to prolong QT space includes administering to the subject at least one specific inhibitor of mitochondrial ROS production selected from among anethole trithione (ATT), 4-OH-anethole trithione (ATX), and an ATX ester, and administering to the subject the drug known to prolong QT space.

公开(公告)号：US10912780B2

公开(公告)日：2021-02-09

申请号：US16487317

申请日：2018-06-08

Applicant: Bugworks Research, Inc.

Inventor： Shahul Hameed Peer Mohamed ,  Nagakumar Bharatham ,  Nainesh Katagihallimath ,  Sreevalli Sharma ,  Radha Nandishaiah ,  Vasanthi Ramachandran ,  Balasubramanian Venkataraman

IPC: A61K31/5383 ,  A61K45/06 ,  C07D498/04 ,  C07D519/00 ,  A61P31/00 ,  A61P31/04

Abstract: The present disclosure relates to compounds of Formula I, or their stereoisomers, pharmaceutically acceptable salts, complexes, hydrates, solvates, tautomers, polymorphs, racemic mixtures, optically active forms and pharmaceutically active derivatives thereof, and pharmaceutical compositions containing them as the active ingredient which can be used as medicaments. The aforementioned substances can also be used in the manufacture of medicaments for treatment, prevention or suppression of diseases, and conditions mediated by microbes. The present disclosure also relates to the synthesis and characterization of aforementioned substances.