公开(公告)号：US12110277B2

公开(公告)日：2024-10-08

申请号：US17929153

申请日：2022-09-01

申请人： SPRINGWORKS THERAPEUTICS, INC.

发明人： Kristin Patterson ,  Mark Hatcher

IPC分类号： C07D233/88 ,  C07C227/26 ,  C07D263/44

CPC分类号： C07D233/88 ,  C07C227/26 ,  C07D263/44

摘要： The present disclosures are directed to processes for synthesizing (S)-2-(((S)-6,8-difluoro-1,2,3,4-tetrahydronaphthalen-2-yl)amino)-N-(1-(2-methyl-1-(neopentylamino)propan-2-yl)-1H-imidazol-4-yl)pentanamide (“nirogacestat”).

公开(公告)号：US12030856B2

公开(公告)日：2024-07-09

申请号：US18238732

申请日：2023-08-28

申请人： ACESION PHARMA APS

发明人： Antonio Mete ,  Ulrik Sørensen

IPC分类号： C07D233/88

CPC分类号： C07D233/88

摘要： A compound of the general formula (I), and the pharmaceutical composition including a compound of formula (I) and optionally a pharmaceutically acceptable additive. Also, the treatment of a cardiac disease, disorder or condition in a mammal, which includes the administration to the mammal a therapeutically effective amount of at least one compound of formula (I), or the pharmaceutically acceptable salt thereof.

公开(公告)号：US11884634B2

公开(公告)日：2024-01-30

申请号：US18057633

申请日：2022-11-21

申请人： Pfizer Inc.

发明人： Elaine Greer ,  Stephen Anderson ,  Mark Maloney ,  Shu Yu ,  Ekaterina Albert ,  Emily Rigsbee

IPC分类号： A61K31/40 ,  C07D233/88 ,  A61P21/00

CPC分类号： C07D233/88 ,  A61P21/00 ,  A61K31/40 ,  C07B2200/13

摘要： The present disclosure relates to: a) solid state forms of hydrobromide salts of Compound 1; b) pharmaceutical compositions comprising one or more solid state forms of hydrobromide salts of Compound 1, and, optionally, a pharmaceutically acceptable carrier; c) methods of treating tumors or cancers by administering one or more solid state forms of hydrobromide salts of Compound 1 to a subject in need thereof; and d) methods for the preparation of solid state forms of Compound 1.

公开(公告)号：US20230399301A1

公开(公告)日：2023-12-14

申请号：US18238732

申请日：2023-08-28

申请人： ACESION PHARMA APS

发明人： Antonio METE ,  Ulrik SØRENSEN

IPC分类号： C07D233/88

CPC分类号： C07D233/88

摘要： A compound of the general formula (I), and the pharmaceutical composition including a compound of formula (I) and optionally a pharmaceutically acceptable additive. Also, the treatment of a cardiac disease, disorder or condition in a mammal, which includes the administration to the mammal a therapeutically effective amount of at least one compound of formula (I), or the pharmaceutically acceptable salt thereof.

公开(公告)号：US20230286922A1

公开(公告)日：2023-09-14

申请号：US18000429

申请日：2021-04-19

申请人： UNIVERSITY OF NOTRE DAME DU LAC

发明人： Christian MELANDER ,  Veronica HUBBLE

IPC分类号： C07D233/88 ,  A61P31/04 ,  A61K31/7048 ,  A61K31/4174

CPC分类号： C07D233/88 ,  A61P31/04 ,  A61K31/7048 ,  A61K31/4174

摘要： We report improved adjuvant compounds that have an aryl 2-aminoimidazole structure for macrolide potentiation against a virulent strain of gram-negative bacteria, AB5075. Compounds were discovered to retain significant adjuvant activity at 10 μM, lowering the minimum inhibitory concentration (MIC) of clarithromycin (CLR) from 8-fold to 128-fold or greater. 2-Aminoimidazole compounds linked to aryl groups via either an amide or urea linker showed significantly improved activity over control compounds.

公开(公告)号：US11673887B2

公开(公告)日：2023-06-13

申请号：US16809244

申请日：2020-03-04

申请人： Pliant Therapeutics, Inc.

发明人： Lan Jiang ,  David John Morgans, Jr. ,  Gustave Bergnes ,  Chun Chen ,  Hui Li ,  Patrick Andre ,  Randall Halcomb ,  Jacob Cha ,  Timothy Hom

IPC分类号： C07D471/04 ,  C07D213/74 ,  C07D233/70 ,  C07D233/88 ,  C07D241/06 ,  C07D241/08 ,  C07D263/28 ,  C07D265/08 ,  C07D277/18 ,  C07D279/06 ,  C07D498/04 ,  A61P1/00 ,  A61P1/16 ,  A61P9/00 ,  A61P11/00 ,  A61P13/12 ,  A61P17/00

CPC分类号： C07D471/04 ,  A61P1/00 ,  A61P1/16 ,  A61P9/00 ,  A61P11/00 ,  A61P13/12 ,  A61P17/00 ,  C07D213/74 ,  C07D233/70 ,  C07D233/88 ,  C07D241/06 ,  C07D241/08 ,  C07D263/28 ,  C07D265/08 ,  C07D277/18 ,  C07D279/06

摘要： The invention relates to compounds of formula (I):




or a salt thereof, wherein R1, A, L, and R2 and n are as described herein. Compounds of formula (I) and pharmaceutical compositions thereof are αvβ1 integrin inhibitors that are useful for treating tissue specific fibrosis.

公开(公告)号：US20180305321A1

公开(公告)日：2018-10-25

申请号：US15770968

申请日：2016-10-27

申请人： KATHOLIEKE UNIVERSITEIT LEUVEN

发明人： Geert Hooyberghs ,  Stijn Robijns ,  Hans Steenackers ,  Erik Van Der Eycken

IPC分类号： C07D233/88 ,  A61P31/04

CPC分类号： C07D233/88 ,  A61P31/04

摘要： The present invention relates to substituted 5-aryl-2-aminoimidiazole compounds being active against microbial biofilm formation. The invention also relates to compositions comprising a microbial biofilm inhibiting amount of said substituted 5-aryl-2-aminoimidiazole compounds in combination with excipients. Methods for inhibiting or controlling microbial biofilm formation in a plant, a body part of a human or an animal, or a surface with which a human or an animal may come into contact are also disclosed.

公开(公告)号：US10059708B2

公开(公告)日：2018-08-28

申请号：US15497783

申请日：2017-04-26

申请人： Northwestern University

发明人： Ali Shilatifard ,  Kaiwei Liang ,  Edwin Richard Smith

IPC分类号： C07D471/04 ,  C07D233/88

CPC分类号： C07D471/04 ,  C07D233/88

摘要： Disclosed are methods for treating cancers associated with rearrangements in the mixed lineage leukemia gene (MLL-r), including MLL-r leukemia. The methods typically include administering a therapeutic amount of one or more therapeutic agents that inhibit the biological activity of one or more members of the interleukin-1 signaling pathway such inhibitors of interleukin-1 receptor-associated kinase 4 (IRAK4).

公开(公告)号：US20180194773A1

公开(公告)日：2018-07-12

申请号：US15738734

申请日：2016-06-21

申请人： Sumitomo Dainippon Pharma Co., Ltd.

发明人： Hitoshi Ban ,  Manabu Kusagi ,  Yosuke Takanashi ,  Futoshi Hasegawa

IPC分类号： C07D491/056 ,  C07D405/12 ,  C07D498/04 ,  C07D471/04 ,  C07D495/04 ,  C07D403/12 ,  C07D401/12 ,  C07D233/88 ,  C07D513/04 ,  A61P35/02

CPC分类号： C07D491/056 ,  A61K31/4365 ,  A61K31/437 ,  A61K31/4375 ,  A61K31/4709 ,  A61K45/00 ,  A61P35/02 ,  C07D233/88 ,  C07D401/12 ,  C07D403/12 ,  C07D405/12 ,  C07D405/14 ,  C07D471/04 ,  C07D495/04 ,  C07D498/04 ,  C07D513/04

摘要： The present invention provides a bicyclic heterocyclic amide derivative of formula (1) wherein ring Q1 is optionally-substituted C6-10 aryl group, etc.; R1 and R2 are independently hydrogen atom, etc.; W1 is optionally-substituted C1-4 alkylene group; W2 is —NR3aC(O)—, etc. wherein R3a is hydrogen atom or C1-6 alkyl group; Cy1 is the following group of formula (11), etc.; ring Q2 is optionally-substituted benzene ring, etc.; n and m are independently 0, 1 or 2, provided that n and m are not simultaneously 0; X is NR5, etc.; R5 is hydrogen atom, etc.; p is 1, 2, 3, 4 or 5; R4 is, independently when two or more exist, hydrogen atom, etc.; and a pharmacologically acceptable salt thereof, which have a potent inhibitory effect on the sphere-forming ability of cancer cells and are useful as an orally-available anti-tumor agent.

公开(公告)号：US20180099988A1

公开(公告)日：2018-04-12

申请号：US15837371

申请日：2017-12-11

申请人： BASF SE

发明人： Urs Lehmann ,  Daniel Heizler

IPC分类号： C07F15/04 ,  C07F11/00 ,  C07F15/00 ,  G02B5/20 ,  B29C65/16 ,  B29C65/00 ,  C07D239/22 ,  G02B5/22 ,  B29B13/02 ,  C07D233/84 ,  C07D233/86 ,  C07D233/88 ,  B29K55/02 ,  B29K33/00 ,  B29K27/00 ,  B29K25/00 ,  B29K23/00 ,  B29C35/08 ,  B29C35/02 ,  B29K67/00 ,  B29K77/00 ,  B29K81/00 ,  B29K105/00 ,  B41M3/14 ,  B29K69/00

CPC分类号： C07F15/045 ,  B29B13/024 ,  B29C35/0272 ,  B29C65/00 ,  B29C65/1616 ,  B29C65/1674 ,  B29C65/1677 ,  B29C66/71 ,  B29C66/7332 ,  B29C66/73366 ,  B29C66/73921 ,  B29C2035/0822 ,  B29K2023/12 ,  B29K2025/08 ,  B29K2027/16 ,  B29K2033/08 ,  B29K2033/12 ,  B29K2055/02 ,  B29K2067/00 ,  B29K2067/003 ,  B29K2067/006 ,  B29K2069/00 ,  B29K2077/00 ,  B29K2081/04 ,  B29K2081/06 ,  B29K2105/0085 ,  B29K2105/0088 ,  B29K2995/0017 ,  B29K2995/002 ,  B29K2995/0026 ,  B29K2995/0027 ,  B41M3/14 ,  C07D233/84 ,  C07D233/86 ,  C07D233/88 ,  C07D239/22 ,  C07F11/00 ,  C07F15/0066 ,  C07F15/0093 ,  G02B5/208 ,  G02B5/22 ,  G02B5/223

摘要： The invention relates to the use of compounds of formulae (I) and/or (II) as colorless 1R absorbers wherein M is Ni, Pd, Pt, Au, Ir, Fe, Zn, W, Cu, Mo, In, Mn, Co, Mg, V, Cr or Ti, X1, X2 and X3 are each independently of the others sulfur or oxygen, R1, R2, R3, R4, R5 and R6 are each independently of the others hydrogen, NR7R8, unsubstituted or substituted C1-C18alkyl, C1-C18 alkyl wherein the alkylene chain is interrupted with oxygen, unsubstituted or substituted C1-C18alkenyl, unsubstituted or substituted aryl, unsubstituted or substituted arylalkyl or unsubstituted or substituted heteroarylalkyl, R7 and R8, each independently of the other, being unsubstituted or substituted C1-C18alkyl, unsubstituted or substituted aryl, un substituted or substituted arylalkyl or unsubstituted or substituted heteroarylalkyl, a further IR absorber optionally being added to the compounds of formulae (I) and (II). The invention relates also to novel dithiolene compounds of formulae (I) and (II) wherein X1 is oxygen and X2 and X3 are oxygen or sulfur. The invention relates furthermore to novel dithiolene compounds of formulae (I) and (II) wherein R1 to R6 arc NR7R8.