公开(公告)号：US11547679B2

公开(公告)日：2023-01-10

申请号：US16670326

申请日：2019-10-31

Applicant: LUNELLA BIOTECH, INC.

Inventor： Michael P. Lisanti ,  Federica Sotgia

IPC: A61K31/55 ,  C07D403/04 ,  A61P31/00 ,  A61P35/00 ,  A61K31/137 ,  C07D295/135 ,  C07C217/74 ,  C07D223/04 ,  C07D401/04 ,  C07C235/46 ,  C07D491/107 ,  C07C275/24 ,  C07D513/04 ,  C07D207/06 ,  A61P15/16 ,  A61K31/14 ,  A61K31/155 ,  A61K31/66 ,  G16C20/50 ,  A61K9/00 ,  A61K31/40 ,  A61K31/436 ,  A61K31/519 ,  A61K31/5513

Abstract: The present disclosure relates to inhibitors of mitochondrial function. Methods of screening compounds for mitochondrial inhibition are disclosed. Also described are methods of using mitochondrial inhibitors called mitoriboscins—mitochondrial-based therapeutic compounds having anti-cancer and antibiotic properties—to prevent or treat cancer, bacterial infections, and pathogenic yeast, as well as methods of using mitochondrial inhibitors to provide anti-aging benefits. Specific mitoriboscin compounds and groups of mitoriboscins are also disclosed.

公开(公告)号：US11542275B2

公开(公告)日：2023-01-03

申请号：US16982800

申请日：2019-03-20

Applicant: Aurigene Discovery Technologies Limited

Inventor： Dinesh Chikkanna ,  Sunil Kumar Panigrahi ,  Srinivasa Raju Sammeta

IPC: C07D498/08 ,  C07D401/14 ,  C07D405/14 ,  C07D413/14 ,  C07D471/08 ,  C07D487/04 ,  C07D491/107 ,  C07D493/08 ,  C07D495/04

Abstract: The present invention relates to substituted imidazolidin-2-one derivatives of formula (I) or pharmaceutically acceptable salts thereof. The present invention further provides the methods of preparation of compound of formula (I) and utility as PRMT5 inhibitors. The compounds are useful as medicaments in the treatment of conditions and disorders mediated by PRMT5, such as cancer, metabolic disorders, inflammation, autoimmune disease and hemoglobinopathies.

公开(公告)号：US20220411367A1

公开(公告)日：2022-12-29

申请号：US17766889

申请日：2020-10-06

Applicant: D. E. Shaw Research, LLC

Inventor： Fabrizio GIORDANETTO ,  Morten Østergaard JENSEN ,  Vishwanath JOGINI ,  Roger John SNOW

IPC: C07D207/06 ,  C07D471/04 ,  C07D491/107 ,  C07D223/04 ,  C07D205/04 ,  C07D491/113 ,  C07D401/04 ,  C07D401/06 ,  C07D413/06 ,  C07D471/10 ,  C07D405/04 ,  C07D487/04

Abstract: A compound of Formula (I), or a pharmaceutically acceptable salt thereof, is described, wherein the substituents are as defined herein. Pharmaceutical compositions comprising the same and method of using the same are also described.

公开(公告)号：US11535618B2

公开(公告)日：2022-12-27

申请号：US17282521

申请日：2019-10-04

Applicant: FORMA Therapeutics, Inc.

Inventor： Alex J. Buckmelter ,  Justin Andrew Caravella ,  Hongbin Li ,  Matthew W. Martin ,  Steven Mischke ,  David James Richard ,  Angela V. West

IPC: C07D471/18 ,  C07D403/12 ,  C07D471/08 ,  C07D487/08 ,  C07D487/18 ,  C07D491/107

Abstract: The disclosure relates to USP30 Inhibitor Compounds I, pharmaceutically acceptable salts thereof, pharmaceutical compositions comprising same, and medical uses involving same. (I)

公开(公告)号：US20220402940A1

公开(公告)日：2022-12-22

申请号：US17887062

申请日：2022-08-12

Applicant: Global Blood Therapeutics, Inc.

Inventor： Zhe Li ,  Qing Xu ,  Brian W. Metcalf ,  Stephen L. Gwaltney, II ,  Jason R. Harris ,  Calvin W. Yee

IPC: C07D498/08 ,  C07D213/74 ,  C07D401/04 ,  C07D403/04 ,  C07D491/107

Abstract: Provide herein are compounds and pharmaceutical compositions suitable as modulators of hemoglobin, methods and intermediates for their preparation, and methods for their use in treating disorders mediated by hemoglobin and disorders that would benefit from tissue and/or cellular oxygenation.

公开(公告)号：US20220396585A1

公开(公告)日：2022-12-15

申请号：US17182756

申请日：2021-02-23

Applicant: NOVARTIS AG

Inventor： Christine Hiu-Tung Chen ,  Zhuoliang Chen ,  Michael Dore ,  Jorge Garcia Fortanet ,  John William Giraldes ,  Rajesh Karki ,  Mitsunori Kato ,  Matthew J. LaMarche ,  Lawrence Blas Perez ,  Martin Sendzik ,  Troy Douglas Smith ,  Bakary-Barry Toure ,  Sarah Williams

IPC: C07D498/10 ,  C07D241/18 ,  C07D241/20 ,  C07D401/04 ,  C07D401/14 ,  C07D403/04 ,  C07D471/10 ,  C07D491/107 ,  C07D495/10

Abstract: The present invention relates to compounds of formula I: in which p, q, Y1, Y2, R1, R2a, R2b, R3a, R3b, R4a, R4b, R5a, R5b, R7 and R8 are defined in the Summary of the Invention; capable of inhibiting the activity of SHP2. The invention further provides a process for the preparation of compounds of the invention, pharmaceutical preparations comprising such compounds and methods of using such compounds and compositions in the management of diseases or disorders associated with the aberrant activity of SHP2.

公开(公告)号：US20220387395A1

公开(公告)日：2022-12-08

申请号：US17631886

申请日：2020-07-27

Applicant: Nurix Therapeutics, Inc.

Inventor： Arthur T. SANDS ,  Neil F. BENCE ,  Christoph W. ZAPF ,  Frederick COHEN ,  Chenbo WANG ,  Thomas CUMMINS ,  Hiroko TANAKA ,  Morgan LAWRENZ ,  Mario CARDOZO ,  Dahlia WEISS ,  Jennifa GOSLING

IPC: A61K31/4196 ,  C07D249/10 ,  C07D249/08 ,  C07D405/06 ,  C07D498/20 ,  C07D401/12 ,  C07D403/12 ,  C07D471/04 ,  C07D498/04 ,  C07D401/14 ,  C07D471/20 ,  C07D487/04 ,  C07D405/14 ,  C07D413/12 ,  C07D413/14 ,  C07D471/10 ,  C07D491/107 ,  C07D487/10 ,  C07D498/10 ,  C07D417/12 ,  C07F5/02 ,  A61K38/17 ,  A61K35/17 ,  A61K39/395 ,  A61K31/704 ,  A61K31/427 ,  A61K31/407 ,  A61K38/14 ,  A61K31/473 ,  A61K31/7048 ,  A61K31/136 ,  A61K31/351 ,  A61K38/12 ,  A61K31/4995 ,  A61K31/337 ,  A61K38/08 ,  A61K31/437 ,  A61K31/439 ,  A61K31/7072 ,  A61K31/513 ,  A61K31/706 ,  A61K31/7068 ,  A61K31/519 ,  A61K31/7076 ,  A61K31/52 ,  A61K31/517 ,  A61K31/655 ,  A61K31/495 ,  A61K31/496 ,  A61K31/047 ,  A61K31/336 ,  A61K31/66 ,  A61K31/7028 ,  A61K31/155 ,  A61K31/396 ,  A61K31/10 ,  A61K31/4184 ,  A61K31/573 ,  A61K31/131 ,  A61K31/137 ,  A61K33/243 ,  A61K31/282 ,  A61P35/00 ,  A61K31/5386 ,  A61K31/4439 ,  A61K31/4709 ,  A61K31/4375 ,  A61K31/5383 ,  A61K31/444 ,  A61K31/501 ,  A61K31/5377 ,  A61K31/4985 ,  A61K31/422 ,  A61K31/506 ,  A61K31/438 ,  A61K31/537 ,  A61K31/635 ,  A61K31/541 ,  A61K47/54 ,  C12N5/0783 ,  C12N15/62 ,  C12N15/86

Abstract: Compounds of formulae (I) and (II), compositions, and methods for use in inhibiting the E3 enzyme Cbl-b in the ubiquitin proteasome pathway are disclosed. The compounds, compositions, and methods can be used to modulate the immune system, to treat diseases amenable to immune system modulation, and for treatment of cells in vivo, in vitro, or ex vivo.

公开(公告)号：US20220380319A1

公开(公告)日：2022-12-01

申请号：US17760864

申请日：2020-09-17

Applicant: Bial - R&D Investments, S.A.

Inventor： Renato T. Skerlj ,  Elyse Marie Josee Bourque ,  Soumya Ray ,  Peter T. Lansbury

IPC: C07D235/04 ,  C07D235/26 ,  C07D401/10 ,  C07D403/10 ,  C07D471/04 ,  C07D401/12 ,  C07D417/10 ,  C07D405/12 ,  C07D487/04 ,  C07D471/08 ,  C07D491/08 ,  C07D491/107 ,  C07D403/12 ,  C07D417/12 ,  C07D498/04

Abstract: The invention provides substituted benzimidazole carboxamides and related compounds, compositions containing such compounds, medical kits, and methods for using such compounds and compositions to treat a medical disorder, e.g., cancer, lysosomal storage disorder, neurodegenerative disorder, inflammatory disorder, in a patient.

公开(公告)号：US20220378839A1

公开(公告)日：2022-12-01

申请号：US17864307

申请日：2022-07-13

Applicant: Nurix Therapeutics, Inc.

Inventor： Arthur T. SANDS ,  Neil F. BENCE ,  Christoph W. ZAPF ,  Frederick COHEN ,  Chenbo WANG ,  Thomas CUMMINS ,  Hiroko TANAKA ,  Hunter SHUNATONA ,  Mario CARDOZO ,  Dahlia WEISS ,  Jennifa GOSLING

IPC: A61K35/17 ,  A61P35/00 ,  A61K33/243 ,  A61K31/438 ,  A61K31/454 ,  A61K31/4545 ,  A61K35/761 ,  A61K35/763 ,  A61K35/768 ,  A61K38/19 ,  A61K39/00 ,  A61K39/39 ,  A61K39/395 ,  A61K45/06 ,  A61N5/10 ,  C07D401/14 ,  C07D405/14 ,  C07D471/04 ,  C07D491/107 ,  C07F5/02 ,  C12N5/0783

Abstract: Compounds, compositions, and methods for use in inhibiting the E3 enzyme Cbl-b in the ubiquitin proteasome pathway are disclosed. The compounds, compositions, and methods can be used to modulate the immune system, to treat diseases amenable to immune system modulation, and for treatment of cells in vivo, in vitro, or ex vivo. Also disclosed are pharmaceutical compositions comprising a Cbl-b inhibitor and a cancer vaccine, as well as methods for treating cancer using a Cbl-b inhibitor and a cancer vaccine; and pharmaceutical compositions comprising a Cbl-b inhibitor and an oncolytic virus, as well as methods for treating cancer using a Cbl-b inhibitor and an oncolytic virus.

公开(公告)号：US11505559B2

公开(公告)日：2022-11-22

申请号：US16760345

申请日：2018-10-30

Applicant: THE UNITED STATES OF AMERICA, AS REPRESENTED BY THE SECRETARY, DEPARTMENT OF HEALTH AND HUMAN SERVICES ,  YALE UNIVERSITY

Inventor： Shyh Ming Yang ,  David J. Maloney ,  Natalia Martinez ,  Adam Yasgar ,  Anton Simeonov ,  Vasilis Vasiliou

IPC: C07D491/113 ,  C07D401/14 ,  C07D401/12 ,  C07D215/54 ,  C07D491/107 ,  C07D413/04 ,  C07D519/00 ,  C07D401/04 ,  C07D471/04 ,  C07D495/04 ,  C07D495/10 ,  C07D401/06 ,  C07D409/14

Abstract: The disclosure provides compounds of Formula I, which may be useful as aldehyde dehydrogenase inhibitors and the pharmaceutically acceptable salts thereof. The variables, J, R4, G, Q, and ring A are defined herein. Aldehyde dehydrogenase inhibitors of Formula I are useful for treating a variety of conditions including cancer and inflammation. The disclosure includes methods for using compounds and salts of Formula I to treat colon cancer, pancreatic cancer, nasopharyngeal carcinoma, thyroid cancer, prostate cancer, ovarian cancer, head and neck squamous cell carcinoma, lung cancer, hepatocellular carcinoma, leukemia, brain tumors breast cancer, atherosclerosis, ischaemic heart disease, acne vulgaris, asthma, autoimmune diseases, autoinflammatory diseases, chronic prostatitis, glomerulonephritis, inflammatory bowel disease, pelvic inflammatory disease, reperfusion injury, rheumatoid arthritis, sarcoidosis, transplant rejection, vasculitis, and interstitial cystitis. The disclosure also includes pharmaceutical compositions containing a compound or salt of Formula I.