公开(公告)号：US12227510B2

公开(公告)日：2025-02-18

申请号：US17599044

申请日：2020-03-20

Applicant: HANMI PHARM. CO., LTD.

Inventor： Hee Sook Oh ,  Jae Hyuk Jung ,  Ji Young Jeon ,  Sun Young Jang ,  Tae Hee Ha

IPC: C07D491/04

Abstract: Provided are crystalline forms of acid addition salts of N-(3-(2-(4-(4-methylpiperazin-1-yl)phenylamino)furo[3,2-d]pyrimidin-4-yloxy)phenyl)acrylamide, and a pharmaceutical composition including the same. The crystalline forms may be easily used in preparing the pharmaceutical composition including the same as an active ingredient.

公开(公告)号：US20240400544A1

公开(公告)日：2024-12-05

申请号：US18566282

申请日：2022-06-03

Applicant: VERTEX PHARMACEUTICALS INCORPORATED

Inventor： Elizabeth Mary BECK ,  Robert PULLIN ,  Gorka ETXEBARRIA JARDI ,  Dean STAMOS ,  Yvonne SCHMIDT ,  Joseph PONTILLO ,  Stephen Andrew THOMSON ,  David Matthew SHAW ,  Nadia M. AHMAD ,  Lidio Marx CARVALHO MEIRELES ,  Sarah SKERRATT ,  Sara S. HADIDA RUAH ,  Timothy Donald NEUBERT ,  Dennis James HURLEY ,  Alexander KINTZER ,  Steven John DURRANT ,  Christopher WRAY ,  Anisa Nizarali VIRANI ,  Kiri NORTH ,  Reece JACQUES ,  Mark Thomas Miller ,  Jinglan ZHOU ,  Ronald Marcellus KNEGTEL ,  Ewa Iwona CHUDYK ,  Joanne Louise PINDER ,  Bruno Artur SOUSA ,  James DODD ,  Michael Edward O'DONNELL ,  Bhairavi GALAN ,  Rebecca E. STEVENS

IPC: C07D413/14 ,  A61K31/4355 ,  A61K31/443 ,  A61K31/506 ,  A61K31/5377 ,  C07D405/12 ,  C07D405/14 ,  C07D491/04

Abstract: Compounds of formula (I) and pharmaceutically acceptable salts thereof, useful as inhibitors of sodium channels are provided. Also provided are pharmaceutical compositions comprising the compounds or pharmaceutically acceptable salts and methods of using the compounds, pharmaceutically acceptable salts, and pharmaceutical compositions in the treatment of various disorders, including pain.

公开(公告)号：US12129250B2

公开(公告)日：2024-10-29

申请号：US18372417

申请日：2023-09-25

Applicant: LYNK PHARMACEUTICALS CO. LTD.

Inventor： Zhaokui Wan ,  Michael Lawrence Vazquez ,  Gurmit Grewal ,  Xiaodong Li ,  Lin Su ,  Jingyu Wu

IPC: C07D471/04 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D403/14 ,  C07D405/12 ,  C07D471/18 ,  C07D487/04 ,  C07D487/08 ,  C07D491/04 ,  C07D495/04 ,  C07D498/08 ,  C07D498/18

CPC classification number: C07D471/04 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D403/14 ,  C07D405/12 ,  C07D471/18 ,  C07D487/04 ,  C07D487/08 ,  C07D491/04 ,  C07D495/04 ,  C07D498/08 ,  C07D498/18

Abstract: The invention provides a novel class of therapeutic agents that are safe and effective TYK2 inhibitors and pharmaceutical compositions of these compounds and methods of preparation and use thereof against various TYK2-mediated diseases and disorders.

公开(公告)号：US12084455B2

公开(公告)日：2024-09-10

申请号：US17224557

申请日：2021-04-07

Applicant: Gilead Sciences, Inc.

Inventor： Elizabeth M. Bacon ,  Elbert Chin ,  Jeromy J. Cottell ,  Ashley Anne Katana ,  Darryl Kato ,  John O. Link ,  Nathan Shapiro ,  Teresa Alejandra Trejo Martin ,  Zheng-Yu Yang

IPC: C07D405/14 ,  A61K31/52 ,  A61K31/55 ,  A61K31/553 ,  A61K31/685 ,  A61K31/688 ,  A61K45/06 ,  A61P31/18 ,  C07C243/28 ,  C07C275/16 ,  C07D401/12 ,  C07D403/12 ,  C07D471/08 ,  C07D487/08 ,  C07D487/10 ,  C07D491/04

CPC classification number: C07D487/08 ,  A61K31/52 ,  A61K31/55 ,  A61K31/553 ,  A61K31/685 ,  A61K31/688 ,  A61K45/06 ,  A61P31/18 ,  C07C243/28 ,  C07C275/16 ,  C07D401/12 ,  C07D403/12 ,  C07D405/14 ,  C07D471/08 ,  C07D487/10 ,  C07D491/04

Abstract: The invention provides a compound of Formula I:






or a pharmaceutically acceptable salt thereof as described herein. The invention also provides pharmaceutical compositions comprising a compound of Formula I, processes for preparing compounds of Formula I, therapeutic methods for treating the proliferation of the HIV virus, treating AIDS or delaying the onset of AIDS symptoms in a mammal using compounds of Formula I.

公开(公告)号：US12006322B2

公开(公告)日：2024-06-11

申请号：US18471250

申请日：2023-09-20

Applicant: Xinthera, Inc.

Inventor： Robert L. Hoffman ,  Porino Jinjo Va ,  Joseph Robert Pinchman ,  Qing Dong ,  Stephen W. Kaldor

IPC: A61K31/444 ,  C07D213/81 ,  C07D487/04 ,  C07D491/04

CPC classification number: C07D487/04 ,  C07D491/04

Abstract: Described herein are tricyclic PARP1 inhibitors and pharmaceutical compositions comprising said inhibitors. The subject compounds and compositions are useful for the treatment of cancer and are of Formula (Ip):

公开(公告)号：US20240158364A1

公开(公告)日：2024-05-16

申请号：US18511612

申请日：2023-11-16

Applicant: Vandria SA

Inventor： Christopher L. Rinsch ,  Penelope Andreux ,  Jonathan Mark Sutton ,  Eileen Mary Seward ,  Jamie D. Knight ,  Ian Linney ,  Peter C. Sennhen ,  Said Oumouch ,  Florent Beaufils ,  Thomas Christian Fessard

IPC: C07D311/80 ,  C07D217/24 ,  C07D279/02 ,  C07D407/12 ,  C07D491/04 ,  C07D491/107 ,  C07D493/04 ,  C07D493/10

CPC classification number: C07D311/80 ,  C07D217/24 ,  C07D279/02 ,  C07D407/12 ,  C07D491/04 ,  C07D491/107 ,  C07D493/04 ,  C07D493/10

Abstract: Disclosed are compounds, compositions, and methods useful for treating neuronal and mitochondrial diseases.

公开(公告)号：US11939337B2

公开(公告)日：2024-03-26

申请号：US17864198

申请日：2022-07-13

Applicant: UNIVERSITY OF PUERTO RICO

Inventor： Cornelis P. Vlaar ,  Suranganie Dharmawardhane Flanagan ,  Eliud Hernandez-O'Farrill ,  Linette Castillo-Pichardo

IPC: C07D491/04 ,  C07D401/14 ,  C07D403/04 ,  C07D403/14 ,  C07D409/14 ,  C07D491/048

CPC classification number: C07D491/048 ,  C07D401/14 ,  C07D403/04 ,  C07D403/14 ,  C07D409/14

Abstract: Compounds are disclosed that inhibit RhoGTPases that are useful for inhibiting hyperprofilerative and neoplastic diseases. Specifically, the compounds inhibit the GTPases Rac and Cdc42 that are overactive or overexpressed in signaling pathways in cancer and metastasis. Methods for treatment of cancer and hyperproliferative diseases are disclosed.

公开(公告)号：US11932658B2

公开(公告)日：2024-03-19

申请号：US17142288

申请日：2021-01-06

Applicant: BRISTOL-MYERS SQUIBB COMPANY

Inventor： Xiaojun Zhang ,  Eldon Scott Priestley ,  Oz Scott Halpern ,  Wen Jiang ,  Samuel Kaye Reznik ,  Jeremy M. Richter

IPC: C07D491/04 ,  A61K31/498 ,  A61P7/02 ,  C07D493/04 ,  C07D495/04 ,  C07D498/04 ,  C07D513/04 ,  C07D515/14 ,  C07D519/00

CPC classification number: C07D519/00 ,  A61P7/02 ,  C07D515/14

Abstract: Disclosed are compounds of Formula (I) to (VIII):




or a stereoisomer, tautomer, pharmaceutically acceptable salt, solvate or prodrug thereof, wherein R3 is a tricyclic heteroaryl group substituted with R3a and zero to 2 R3b; and Ri, R2, R3a, R3b, R4, and n are defined herein. Also disclosed are methods of using such compounds as PAR4 inhibitors, and pharmaceutical compositions comprising such compounds. These compounds are useful in inhibiting or preventing platelet aggregation, and are useful for the treatment of a thromboembolic disorder or the primary prophylaxis of a thromboembolic disorder.

公开(公告)号：US11884661B2

公开(公告)日：2024-01-30

申请号：US17184179

申请日：2021-02-24

Applicant: BRISTOL-MYERS SQUIBB COMPANY

Inventor： Guohua Zhao ,  Pratik Devasthale ,  Xiang-Yang Ye ,  Kumaravel Selvakumar ,  Suresh Dhanusu ,  Palanikumar Balasubramanian ,  Leatte R. Guernon ,  Rita Civiello ,  Xiaojun Han ,  Michael Frederick Parker ,  Swanee E. Jacutin-Porte

IPC: C07D471/04 ,  C07D491/04 ,  C07D519/00 ,  A61P11/00 ,  A61P19/10 ,  A61P35/00 ,  A61P37/06

CPC classification number: C07D471/04 ,  A61P11/00 ,  A61P19/10 ,  A61P35/00 ,  A61P37/06 ,  C07D491/04 ,  C07D519/00

Abstract: The present invention provides compounds of Formula (I):




or stereoisomers, tautomers, or pharmaceutically acceptable salts or solvates thereof, wherein all the variables are as defined herein. These compounds are antagonists to αV-containing integrins. This invention also relates to pharmaceutical compositions comprising these compounds and methods of treating a disease, disorder, or condition associated with dysregulation of αv-containing integrins, such as pathological fibrosis, transplant rejection, cancer, osteoporosis, and inflammatory disorders, by using the compounds and pharmaceutical compositions.

公开(公告)号：US11858943B2

公开(公告)日：2024-01-02

申请号：US17500780

申请日：2021-10-13

Applicant: Neumora Therapeutics, Inc.

Inventor： Robert M. Jones ,  Mariangela Urbano ,  Gary Brandt ,  David Hardick ,  Chris Knight ,  Jason Tierney

IPC: C07D487/04 ,  A61P15/08 ,  A61P15/10 ,  A61P25/20 ,  C07D498/04 ,  A61P9/06 ,  A61P25/18 ,  A61P25/22 ,  C07D491/04 ,  A61P25/24

CPC classification number: C07D487/04 ,  A61P9/06 ,  A61P15/08 ,  A61P15/10 ,  A61P25/18 ,  A61P25/20 ,  A61P25/22 ,  A61P25/24 ,  C07D491/04 ,  C07D498/04

Abstract: Compounds are provided that antagonize vasopressin receptors, particularly the V1a receptor products containing such compounds, as well as to methods of their use and synthesis. Such compounds have the structure of Formula (I), or a pharmaceutically acceptable isomer, racemate, hydrate, solvate, isotope, or salt thereof:




wherein A, B, G, R1, R1b, R1c, R2 and X are as defined herein.