公开(公告)号：EP3870587B1

公开(公告)日：2024-09-11

申请号：EP20717200.8

申请日：2020-04-09

IPC: C07D493/08

CPC classification number: C07D493/08

公开(公告)号：EP4419700A1

公开(公告)日：2024-08-28

申请号：EP22808990.0

申请日：2022-10-20

Applicant: Givaudan SA

Inventor： EICHHORN, Eric ,  SCARDUA, Alessandro ,  ULLMANN, Christophe

IPC: C12P17/02 ,  C12P17/18 ,  C07D313/08 ,  C11B9/00

CPC classification number: C12P17/02 ,  C12P17/181 ,  C11B9/0073 ,  C07D313/08 ,  C12Y504/99017 ,  C07D493/08 ,  C07D313/20

公开(公告)号：EP3049391B1

公开(公告)日：2018-12-26

申请号：EP14772317.5

申请日：2014-09-22

Applicant: F. Hoffmann-La Roche AG

Inventor： BALLARD, Theresa Maria ,  GROEBKE ZBINDEN, Katrin ,  PINARD, Emmanuel ,  RYCKMANS, Thomas ,  SCHAFFHAUSER, Herve ,  BLANC, Jean-Baptiste

IPC: C07D209/42 ,  C07D403/10 ,  C07D405/12 ,  C07D405/14 ,  C07D413/14 ,  C07D417/14 ,  C07D471/04 ,  A61K31/404 ,  A61K31/416 ,  A61P25/28

CPC classification number: C07D209/42 ,  C07D401/06 ,  C07D401/14 ,  C07D403/10 ,  C07D405/10 ,  C07D405/12 ,  C07D405/14 ,  C07D409/12 ,  C07D413/14 ,  C07D417/14 ,  C07D471/04 ,  C07D493/08

Abstract: The present invention relates to compounds of formula I or pharmaceutically acceptable addition salts, racemic mixtures or the corresponding enantiomers and optical isomers thereof. The compounds may be used for the treatment or prophylaxis of Alzheimer's disease, cognitive impairment, schizophrenia, pain and sleep disorder.

公开(公告)号：EP2810939B1

公开(公告)日：2018-12-26

申请号：EP13744073.1

申请日：2013-02-01

Applicant: Nihon Nohyaku Co., Ltd.

Inventor： SATOH, Eikou ,  MURATA, Tetsuya ,  HARAYAMA, Hiroto ,  NAKANO, Motofumi ,  FUKATSU, Kosuke ,  INUKAI, Kayo ,  KASAHARA, Ryota ,  ABE, Yutaka ,  HAYASHI, Nobuyuki ,  FUJITA, Naoya

IPC: C07D239/34 ,  A01N43/54 ,  A01N43/653 ,  A01N47/02 ,  A01P7/04 ,  A61K31/505 ,  A61K31/506 ,  A61P33/14 ,  C07D407/04 ,  C07F7/18 ,  C07D405/14 ,  A01N43/56 ,  A01N43/76 ,  A01N43/78 ,  A01N43/80 ,  A01N43/82 ,  A01N43/84 ,  A01N47/28

CPC classification number: A01N43/54 ,  A01N43/56 ,  A01N43/653 ,  A01N43/76 ,  A01N43/78 ,  A01N43/80 ,  A01N43/82 ,  A01N43/84 ,  A01N43/90 ,  A01N47/02 ,  A01N47/28 ,  A01N55/00 ,  C07D239/34 ,  C07D239/52 ,  C07D401/04 ,  C07D401/06 ,  C07D401/12 ,  C07D403/04 ,  C07D403/06 ,  C07D405/04 ,  C07D405/06 ,  C07D405/14 ,  C07D409/04 ,  C07D411/04 ,  C07D413/04 ,  C07D413/06 ,  C07D417/04 ,  C07D493/04 ,  C07D493/08 ,  C07D493/10 ,  C07D495/10 ,  C07D497/10 ,  C07F7/0812 ,  C07F7/1804

Abstract: An arylalkyloxypyrimidine derivative represented by the formula (I) wherein R 1 is an alkyl group, a cycloalkyl group, an alkenyl group, an alkynyl group, a haloalkyl group, a haloalkenyl group, a haloalkynyl group, an alkoxyalkyl group, a dioxolane group and the like; R 2 and R 3 are each a hydrogen atom, an alkyl group and the like; X is an alkyl group, a cycloalkyl group, an alkenyl group, an alkynyl group, a haloalkyl group, a haloalkenyl group, a haloalkynyl group, a trialkylsilyl group and the like; Y is CH or a nitrogen atom; q is an integer of 1 to 3; m is an integer of 0 to 5; and n is 0 or 1 or a salt thereof, and an agrohorticultural insecticide containing the compound as an active ingredient and a method of use thereof.

公开(公告)号：EP3087080B1

公开(公告)日：2018-11-28

申请号：EP14827687.6

申请日：2014-12-24

Applicant: President and Fellows of Harvard College

Inventor： SHAIR, Matthew, D. ,  RAMHARTER, Juergen ,  PELISH, Henry, Efrem ,  LIAU, Brian, Bor-Jen ,  AHN, Jae Young

IPC: C07D493/08 ,  C07D493/22 ,  C07D519/00 ,  C07K14/575 ,  C07K16/26

CPC classification number: C07D493/08 ,  C07D493/22 ,  C07D519/00 ,  C07K14/575 ,  C07K16/26

Abstract: Compounds of Formula (A), (B), (C), (D), and (E) are contemplated useful as therapeutics for treating a wide variety of conditions, e.g., including but not limited to, conditions associated with angiogenesis and with CDK8 and/or CDK19 kinase activity. Further provided are methods of inhibiting CDK8 and/or CDK19 kinase activity, methods of modulating the -catenin pathway, methods of modulating STAT1 activity, methods of modulating the TGFβ/BMP pathway, methods of modulating HIF-1-alpha activity in a cell, and methods of increasing BIM expression to induce apoptosis, using a compound of Formula (A), (B), (C), (D), or (E). Further provided are CDK8 and CDK19 point mutants and methods of use thereof.

公开(公告)号：EP3394038A1

公开(公告)日：2018-10-31

申请号：EP16880061.3

申请日：2016-12-21

Applicant: President and Fellows of Harvard College

Inventor： SHAIR, Matthew D. ,  PELISH, Henry Efrem ,  NITULESCU, Ioana Llinca ,  AHN, Jae Young

IPC: C07D239/72 ,  C07D493/08

CPC classification number: C07D493/08 ,  A61K31/4725

Abstract: The invention relates to methods to select patients for treatment with specific Cortistatin analogs.

公开(公告)号：EP2805955B1

公开(公告)日：2018-10-31

申请号：EP13739109.0

申请日：2013-01-21

Applicant: Bensen Pharmaceutical (Shanghai) Corp. Ltd.

Inventor： XU, Rongzhen ,  RONG, Frank ,  XIE, Fuwen ,  LAI, Hongxi

IPC: C07D493/08 ,  A61K31/352 ,  A61P35/00 ,  A61P35/02

CPC classification number: C07D493/08

Abstract: The present invention relates to the fields of natural medicine and medicinal chemistry, and more particularly to a 1-oxo/acylated-14-acylated oridonin derivative of a general formula (I) or a pharmaceutically acceptable salt thereof, a method for preparing the compounds, a pharmaceutical composition comprising the compounds, and application thereof in preparation of antitumor drugs.

公开(公告)号：EP3386935A1

公开(公告)日：2018-10-17

申请号：EP16872409.4

申请日：2016-12-08

Applicant: Rhodia Operations ,  Centre National de la Recherche Scientifique

Inventor： MORVAN, Didier ,  BACK, Olivier ,  WISCHERT, Raphael ,  MULLER, Eric

IPC: C07C2/50 ,  C07C209/00 ,  C07C211/00

CPC classification number: C07D493/08 ,  C07C209/48 ,  C07C211/27

Abstract: The present invention relates to the production of xylene derivatives from furfural and its derivatives. The invention describes new routes for converting furfural and its derivatives into xylene derivatives including novel intermediates.

公开(公告)号：EP3371176A1

公开(公告)日：2018-09-12

申请号：EP16856299.9

申请日：2016-10-14

Applicant: William Marsh Rice University

Inventor： NICOLAOU, Kyriacos, C. ,  RHOADES, Derek ,  WANG, Yanping ,  TOTOKOTSOPOULOS, Sotirios

IPC: C07D407/06 ,  C07D405/06 ,  A61K31/425

CPC classification number: C07D407/06 ,  A61K31/4155 ,  A61K31/427 ,  A61K31/428 ,  A61K31/4427 ,  A61K39/395 ,  A61K45/06 ,  C07D405/06 ,  C07D491/08 ,  C07D493/08 ,  A61K2300/00

Abstract: In one aspect, the present disclosure provides epothilone analogs of the formula (I) wherein the variables are as defined herein. In another aspect, the present disclosure also provides methods of preparing the compounds disclosed herein. In another aspect, the present disclosure also provides pharmaceutical compositions and methods of use of the compounds disclosed herein. Additionally, drug conjugates with cell targeting moieties of the compounds are also provided.

公开(公告)号：EP3313828A1

公开(公告)日：2018-05-02

申请号：EP16815358.3

申请日：2016-06-24

Applicant: Merck Sharp & Dohme Corp.

Inventor： BENNETT, Frank ,  JIANG, Jinlong ,  PASTERNAK, Alexander ,  DONG, Shuzhi ,  GU, Xin ,  SCOTT, Jack, D. ,  TANG, Haiqun ,  ZHAO, Zhiqiang ,  HUANG, Yuhua ,  HUNTER, David ,  YANG, Dexi ,  YOUNG, Katherine ,  XIAO, Li ,  ZHANG, Zhibo ,  FU, Jianmin ,  BAI, Yunfeng ,  ZHENG, Zhixiang ,  ZHANG, Xu

IPC: C07D257/02 ,  C07D257/04 ,  A61K31/41 ,  A61K31/395

CPC classification number: C07D403/10 ,  A61K31/198 ,  A61K31/407 ,  A61K31/41 ,  A61K31/416 ,  A61K31/4184 ,  A61K31/4192 ,  A61K31/4196 ,  A61K31/421 ,  A61K31/423 ,  A61K31/4245 ,  A61K31/428 ,  A61K31/431 ,  A61K31/437 ,  A61K31/4375 ,  A61K31/439 ,  A61K31/4439 ,  A61K31/454 ,  A61K31/4545 ,  A61K31/4709 ,  A61K31/4725 ,  A61K31/496 ,  A61K31/498 ,  A61K31/5025 ,  A61K31/506 ,  A61K31/517 ,  A61K31/5377 ,  A61K31/541 ,  A61K31/546 ,  A61K45/06 ,  A61P31/04 ,  C07D401/10 ,  C07D401/14 ,  C07D403/12 ,  C07D403/14 ,  C07D405/14 ,  C07D407/14 ,  C07D413/10 ,  C07D413/14 ,  C07D417/10 ,  C07D417/14 ,  C07D453/02 ,  C07D471/04 ,  C07D487/04 ,  C07D487/10 ,  C07D493/04 ,  C07D493/08 ,  C07D495/08

Abstract: The present invention relates to metallo-beta-lactamase inhibitor compounds of Formula I: and pharmaceutically acceptable salts thereof, wherein Z, RA, X1, X 2 and R1are as defined herein. The present invention also relates to compositions which comprise a metallo-beta-lactamase inhibitor compound of the invention or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier, optionally in combination with a beta-lactam antibiotic and/or a beta-lactamase inhibitor. The invention further relates to methods for treating a bacterial infection comprising administering to a patient a therapeutically effective amount of a compound of the invention, in combination with a therapeutically effective amount of one or more β-lactam antibiotics and optionally in combination with one or more beta-lactamase inhibitor compounds. The compounds of the invention are useful in the methods described herein for overcoming antibiotic resistance.