公开(公告)号：US20240299357A1

公开(公告)日：2024-09-12

申请号：US18610100

申请日：2024-03-19

Applicant: HUA Medicine (Shanghai) Ltd.

Inventor： Li Chen ,  Yongguo Li ,  Gaosen Wang ,  Huisheng Gao

IPC: A61K31/4155 ,  A61K9/16 ,  A61K9/20 ,  A61K9/28 ,  A61K31/155 ,  A61K31/40 ,  A61K31/403 ,  A61K31/4035 ,  A61K31/4439 ,  A61K31/4985 ,  A61K31/522 ,  A61K31/7034 ,  A61K45/06 ,  A61K47/38 ,  A61P3/10 ,  C07D231/38 ,  C07D403/12

CPC classification number: A61K31/4155 ,  A61K9/1611 ,  A61K9/1617 ,  A61K9/1635 ,  A61K9/1694 ,  A61K9/2009 ,  A61K9/2013 ,  A61K9/2027 ,  A61K9/2054 ,  A61K9/2086 ,  A61K9/2095 ,  A61K9/2813 ,  A61K9/284 ,  A61K9/2866 ,  A61K31/155 ,  A61K31/40 ,  A61K31/403 ,  A61K31/4035 ,  A61K31/4439 ,  A61K31/4985 ,  A61K31/522 ,  A61K31/7034 ,  A61K45/06 ,  A61K47/38 ,  A61P3/10 ,  C07D231/38 ,  C07D403/12

Abstract: Disclosed is a pharmaceutical combination comprising a glucokinase activator or a pharmaceutically acceptable salt thereof, an isotopic label thereof, a crystalline form thereof, a hydrate, a solvate, a diastereomeric or enantiomeric form thereof, and a DPP-IV inhibitor. Disclosed are a pharmaceutical composition and a fixed dose of a compound preparation, and the methods for preparing the pharmaceutical composition and the fixed dose of the compound preparation and the uses thereof.

公开(公告)号：US12054461B2

公开(公告)日：2024-08-06

申请号：US17618184

申请日：2020-06-11

Applicant: NodThera Limited

Inventor： Mark G. Bock ,  David Harrison ,  Jane E. Scanlon

IPC: C07D231/40 ,  C07D231/38

CPC classification number: C07D231/40 ,  C07D231/38

Abstract: The present disclosure relates to compounds of Formula (I)




and to their prodrugs, pharmaceutically acceptable salts, pharmaceutical compositions, methods of use, and methods for their preparation. The compounds disclosed herein are useful for inhibiting the maturation of cytokines of the IL-1 family by inhibiting inflammasomes and may be used in the treatment of disorders in which inflammasome activity is implicated, such as inflammatory, autoinflammatory and autoimmune diseases and cancers.

公开(公告)号：US20240150297A1

公开(公告)日：2024-05-09

申请号：US18264994

申请日：2022-02-10

Applicant: The Trustees of Columbia University in the City of New York ,  Albany College of Pharmacy and Health Sciences in the City of Albany ,  PETRUKIN, Konstantin ,  RACZ, Boglarka ,  VARADI, Andras ,  CIOFFI, Christopher, L. ,  MUTHURAMAN, Parthasarathy ,  RAJA, Arun

Inventor： Konstantin Petrukhin ,  Boglarka Racz ,  Andras Varadi ,  Christopher : Cioffi ,  Parthasarathy Muthuraman ,  Arun Raja

IPC: C07D231/38 ,  A61K31/496 ,  A61P27/02 ,  C07D261/14 ,  C07D275/03 ,  C07D403/12 ,  C07D413/12 ,  C07D417/12

CPC classification number: C07D231/38 ,  A61K31/496 ,  A61P27/02 ,  C07D261/14 ,  C07D275/03 ,  C07D403/12 ,  C07D413/12 ,  C07D417/12

Abstract: The present invention provides a compound having the structure:




wherein

X1 is N or CR5,



wherein R5 is H, OH, halogen or alkyl;

X2, X3 and X4 are each independently NH, N, S, O or CR6, wherein each R6 is independently H, OH, halogen, alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkylalkyl, haloalkyl, —O—(alkyl), —S—(alkyl), —NH2, —NH—(alkyl), —N(alkyl)2 or —CO2H;

R1, R2, R3 and R4 are each independently —H, —F, —Cl, —Br, —I, —NO2, —CN, —CF3, —CF2H, —OCF3, -(alkyl), -(haloalkyl), -(alkenyl), -(alkynyl), -(aryl), -(heteroaryl), -(cycloalkyl), -(cycloalkylalkyl), -(heteroalkyl), heterocycle, heterocycloalkyl, -(alkylheteroalkyl), -(alkylaryl), —OH, —OAc, —O-(alkyl), —O-(alkenyl), —O-(alkynyl), —O-(aryl), (heteroaryl), —SH, —S-(alkyl), —S-(alkenyl), —S-(alkynyl), —S-(aryl), —S-(heteroaryl), —NH2, —NH-(alkyl), —NH-(alkenyl), —NH-(alkynyl), —NH-(aryl), —NH-(heteroaryl), —C(O)R7, —S(O)R7, —SO2R7, —NHSO2R7, —OC(O)R7, —SC(O)R7, —NHC(O)R7 or —NHC(S)R7,

wherein R7 is, H, —(alkyl), —OH, —O(alkyl), —NH2, —NH(alkyl) or —N(alkyl)2;

B is absent or present, and when present is











wherein R8 is H, OH, halogen, alkyl, cycloalkyl,
cycloalkylalkyl, —O-(alkyl), —S-(alkyl), —NH2, —NH-(alkyl), —N(alkyl)2 or —CO2H; and

C is H, substituted or unsubstituted monocycle, bicycle, heteromonocycle, heterobicycle, aryl, heteroaryl, alkyl, cycloalkyl, cycloalkylalkyl, CO2H, COOR9, OH, OR9, NH2, NHR9, NR9R10, SO2R11, CH2NHR9, CH2NR9R10 or CH2COOR9,

wherein R9 and R10 are each independently H, alkyl, cycloalkyl, —C(O)-alkyl, —C(O)-cycloalkyl, —C(O)OH, —C(O)—O-alkyl, —C(O)—O-cycloalkyl, —C(O)NH2, —C(O)NH(alkyl), —C(O)NH(cycloalkyl), —C(O)N(alkyl)2, —CH2NH(alkyl), —CH2COOH, —SO2CH3, —OH, —O(alkyl), —NH2, —NH(alkyl) or —N(alkyl)
wherein R11 is alkyl, haloalkyl, cycloalkyl, aryl, heteroaryl, NH2, NH(alkyl), NH(cycloalkyl), NH(heterocycle), NH(aryl), NH(heteroaryl) or NHCOR12,

wherein R12 is alkyl, haloalkyl, cycloalkyl, heterocycle, aryl or heteroaryl,

or a pharmaceutically acceptable salt thereof.

公开(公告)号：US20230346748A1

公开(公告)日：2023-11-02

申请号：US18311846

申请日：2023-05-03

Applicant: HUA Medicine (Shanghai) Ltd.

Inventor： Li Chen ,  Yongguo Li ,  Gaosen Wang ,  Huisheng Gao

IPC: A61K31/4155 ,  A61K31/4439 ,  A61K45/06 ,  A61K9/16 ,  A61K31/403 ,  A61K31/4985 ,  A61K9/20 ,  A61K31/522 ,  A61K31/40 ,  A61K31/7034 ,  C07D403/12 ,  C07D231/38 ,  A61K9/28 ,  A61K31/155 ,  A61P3/10 ,  A61K31/4035 ,  A61K47/38

CPC classification number: A61K31/4155 ,  A61K31/4439 ,  A61K45/06 ,  A61K9/1611 ,  A61K31/403 ,  A61K31/4985 ,  A61K9/2054 ,  A61K9/2013 ,  A61K9/1617 ,  A61K31/522 ,  A61K9/2009 ,  A61K9/2086 ,  A61K9/2095 ,  A61K31/40 ,  A61K31/7034 ,  C07D403/12 ,  A61K9/1635 ,  C07D231/38 ,  A61K9/2813 ,  A61K9/2866 ,  A61K31/155 ,  A61P3/10 ,  A61K31/4035 ,  A61K9/284 ,  A61K9/1694 ,  A61K47/38 ,  A61K9/2027

Abstract: The present invention relates to a pharmaceutical combination, the pharmaceutical combination comprising a glucokinase activator or a pharmaceutically acceptable salt thereof, an isotopic label thereof, a crystal form thereof, a hydrate, a solvate, a diastereomer or enantiomer, and a K-ATP channel blocker. The present invention further relates to a pharmaceutical composition, a fixed dose compound preparation, and a method for preparing the pharmaceutical composition and the fixed dose compound preparation as well as a use thereof.

公开(公告)号：US20230227428A1

公开(公告)日：2023-07-20

申请号：US18011408

申请日：2021-06-21

Applicant: Anaxis Pharma Pty Ltd

Inventor： Jean-Marc Daniel Garnier ,  Martin Brzozowski ,  John Thomas Feutrill ,  Guillaume Laurent Lessene ,  Christopher Gardner ,  Peter Edward Czabotar ,  Angus Cowan ,  Pooja Sharma ,  Carole Annie Schuster-Klein ,  Christophe Poitevin

IPC: C07D401/12 ,  C07D401/14 ,  C07D409/14 ,  C07D403/12 ,  C07D413/14 ,  C07D231/38 ,  A61P29/00

CPC classification number: C07D401/12 ,  C07D401/14 ,  C07D409/14 ,  C07D403/12 ,  C07D413/14 ,  C07D231/38 ,  A61P29/00

Abstract: This invention relates to compounds of formula (I) and salts, solvates, tautomers, N-oxides, stereoisomers, polymorphs and/or prodrugs thereof. Also disclosed is the use of the compound of formula (I) to treat necroptosis and/or inhibit RIP1 and/or MLKL.

公开(公告)号：US20230148599A1

公开(公告)日：2023-05-18

申请号：US17910051

申请日：2021-03-11

Applicant: FMC Corporation

Inventor： Jeffrey Keith LONG ,  Srinivas CHITTABOINA ,  Travis Chandler MCMAHON

IPC: A01N43/56 ,  A01P3/00 ,  C07D231/38

CPC classification number: A01N43/56 ,  A01P3/00 ,  C07D231/38

Abstract: Disclosed is a fungicidal composition comprising (a) at least one compound selected from the compounds of Formula 1, including all geometric and stereoisomers, tautomers, iV-oxides, and salts thereof, (I) wherein R1, R2, R3, R4, R5, R6, m and n are as defined in the disclosure and (b) at least one additional fungicidal compound. Also disclosed is a method for controlling plant diseases caused by fungal plant pathogens comprising applying to the plant or portion thereof, or to the plant seed, a fungicidally effective amount of a compound of Formula 1, an A-oxide, or salt thereof (e.g., as a component in the aforesaid composition). Also disclosed is a composition comprising: (a) at least one compound selected from the compounds of Formula 1 described above, A-oxides, and salts thereof; and at least one invertebrate pest control compound or agent.

公开(公告)号：US20190185477A1

公开(公告)日：2019-06-20

申请号：US16197195

申请日：2018-11-20

Applicant: Infinity Pharmaceuticals, Inc.

Inventor： Louis Grenier ,  Andre Lescarbeau ,  Praveen Sharma ,  Daniel G. Genov

IPC: C07D487/04 ,  C07D401/06 ,  A61K9/48 ,  C07D231/38 ,  A61K31/519 ,  C07D231/12

CPC classification number: C07D487/04 ,  A61K9/485 ,  A61K9/4858 ,  A61K9/4866 ,  A61K31/519 ,  C07B2200/13 ,  C07D231/12 ,  C07D231/38 ,  C07D401/06

Abstract: Solid forms of chemical compounds that modulate kinase activity, including PI3 kinase activity, and compounds, pharmaceutical compositions, and methods of treatment of diseases and conditions associated with kinase activity, including PI3 kinase activity, are described herein. Also provided herein are processes for preparing compounds, polymorphic forms, cocrystals, and amorphous forms thereof, and pharmaceutical compositions thereof.

公开(公告)号：US20190059377A1

公开(公告)日：2019-02-28

申请号：US16173167

申请日：2018-10-29

Applicant: FMC CORPORATION

Inventor： JEFFREY KEITH LONG ,  WONPYO HONG ,  ANDREW EDMUND TAGGI

IPC: A01N43/56 ,  C07D417/12 ,  C07D409/04 ,  C07D407/12 ,  C07D403/12 ,  C07D231/12 ,  C07D401/12 ,  C07D401/04 ,  C07D231/38 ,  C07D231/20 ,  C07D401/14

CPC classification number: A01N43/56 ,  C07D231/12 ,  C07D231/20 ,  C07D231/38 ,  C07D401/04 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D407/12 ,  C07D409/04 ,  C07D417/12

Abstract: Disclosed are compounds of Formula 1, including all geometric and stereoisomers, N-oxides, and salts thereof, wherein Q1 is a phenyl ring, naphthalenyl ring system, a 5- to 6-membered fully unsaturated heterocyclic ring or an 8- to 10-membered heteroaromatic bicyclic ring system, each as described with optional substituents as defined in the disclosure; Q2 is a phenyl ring, a naphthalenyl ring system, a 5- to 6-membered saturated, partially unsaturated or fully unsaturated heterocyclic ring, or an 8- to 10-membered heteroaromatic bicyclic ring system, each as described with optional substituents as defined in the disclosure; X is O, S(O)m, NR4, CR15R16, C(═O) or C(═S); and R1, R1a, R2, R4, R15, R16 and m are as defined in the disclosure. Also disclosed are compositions containing the compounds of Formula 1 and methods for controlling plant disease caused by a fungal pathogen comprising applying an effective amount of a compound or a composition of the invention. Also disclosed are compounds of Formula 2, including all geometric and stereoisomers, and salts thereof, wherein X is NH; and Q1, Q2 and R2 are as defined for Formula 1; which are useful as intermediates for preparing compounds of Formula 1.

公开(公告)号：US20190000806A1

公开(公告)日：2019-01-03

申请号：US16113661

申请日：2018-08-27

Applicant: Loxo Oncology, Inc.

Inventor： Nicolas Guisot

IPC: A61K31/415 ,  A61K31/4155 ,  A61P35/00

CPC classification number: A61K31/415 ,  A61K31/4155 ,  A61K45/06 ,  A61P35/00 ,  A61P35/02 ,  A61P37/02 ,  C07D231/14 ,  C07D231/38 ,  C07D401/04 ,  C07D401/06 ,  C07D403/04 ,  C07D405/04 ,  C07D405/06 ,  C07D405/08 ,  C07D405/14 ,  C07D413/06 ,  C07D417/04

Abstract: This invention relates to novel compounds. The compounds of the invention are tyrosine kinase inhibitors. Specifically, the compounds of the invention are useful as inhibitors of Bruton's tyrosine kinase (BTK). The invention also contemplates the use of the compounds for treating conditions treatable by the inhibition of Bruton's tyrosine kinase, for example cancer, lymphoma, leukemia and immunological diseases.

公开(公告)号：US20180273489A1

公开(公告)日：2018-09-27

申请号：US15990026

申请日：2018-05-25

Applicant: Sumitomo Dainippon Pharma Co., Ltd.

Inventor： Izumi SASAKI ,  Tomohiro TOYODA ,  Hidefumi YOSHINAGA ,  Itaru NATSUTANI ,  Yoko TAKAHASHI

IPC: C07D231/20 ,  C07D231/38 ,  C07D231/18 ,  C07D405/06 ,  C07D493/08

CPC classification number: C07D231/20 ,  C07D231/18 ,  C07D231/22 ,  C07D231/38 ,  C07D231/44 ,  C07D405/06 ,  C07D493/08

Abstract: The present invention relates to a novel serotonin reuptake inhibitor which also exhibits 5-HT2C antagonistic action (antidepressive and anxiolytic effects), in particular, 5-HT2C inverse agonistic action comprising Compound (1): or a pharmaceutically acceptable salt thereof wherein R1, R2, R3 and R4 are independently hydrogen or C1-6 alkyl etc.; R5 is C4-7 alkyl or —(CR8R9)r-E; R6, R7, R8 and R9 are independently hydrogen, fluorine or C1-6 alkyl; A is C6-10 aryl or heteroaryl etc.; r is 1, 2, 3 or 4; E is C3-8 cycloalkyl or C6-10 aryl etc.; L is oxygen, sulfur or —NR10—; n is 1, 2 or 3; R10 is hydrogen or C1-6 alkyl etc.; and X is hydrogen or halogen etc.