公开(公告)号：EP3092216B1

公开(公告)日：2018-12-12

申请号：EP15700817.8

申请日：2015-01-05

Applicant: Bristol-Myers Squibb Company

Inventor： DUAN, Jingwu ,  DHAR, T. G. Murali ,  JIANG, Bin ,  LU, Zhonghui ,  KARMAKAR, Ananta ,  GUPTA, Arun Kumar ,  WEIGELT, Carolyn A.

IPC: C07D213/04 ,  C07D309/08 ,  C07D231/14 ,  C07D401/02 ,  C07D403/04 ,  C07D237/06 ,  C07D405/02 ,  C07D239/28 ,  C07C317/00 ,  C07D241/24 ,  C07D249/04 ,  C07D471/04 ,  C07D205/04 ,  C07D207/277 ,  C07D277/60 ,  C07D295/00 ,  C07D211/36 ,  A61K31/33 ,  A61K31/10 ,  A61P29/00

CPC classification number: C07C317/14 ,  C07C317/20 ,  C07C317/22 ,  C07C317/30 ,  C07C317/32 ,  C07C317/44 ,  C07C317/46 ,  C07C317/50 ,  C07C2601/02 ,  C07C2601/04 ,  C07C2601/08 ,  C07C2601/10 ,  C07C2601/14 ,  C07C2601/16 ,  C07C2602/08 ,  C07D205/04 ,  C07D211/36 ,  C07D211/62 ,  C07D213/30 ,  C07D213/40 ,  C07D213/56 ,  C07D213/75 ,  C07D213/81 ,  C07D213/85 ,  C07D231/12 ,  C07D237/08 ,  C07D239/38 ,  C07D241/12 ,  C07D257/04 ,  C07D261/08 ,  C07D263/32 ,  C07D271/06 ,  C07D285/06 ,  C07D295/108 ,  C07D295/155 ,  C07D295/18 ,  C07D295/185 ,  C07D295/20 ,  C07D295/22 ,  C07D303/06 ,  C07D303/34 ,  C07D305/14 ,  C07D309/04 ,  C07D309/14 ,  C07D317/44 ,  C07D319/20 ,  C07D401/04 ,  C07D471/04 ,  C07D471/10

Abstract: Described are RORγ modulators of the formula (I), or stereoisomers, tautomers, pharmaceutically acceptable salts, solvates, or prodrugs thereof, wherein all substituents are defined herein. Also provided are pharmaceutical compositions comprising the same. Such compounds and compositions are useful in methods for modulating RORγ activity in a cell and methods for treating a subject suffering from a disease or disorder in which the subject would therapeutically benefit from modulation of RORγ activity, for example, autoimmune and/or inflammatory disorders.

公开(公告)号：EP2321269B1

公开(公告)日：2018-09-19

申请号：EP09790863.6

申请日：2009-07-28

Applicant: Intervet International B.V.

Inventor： PAQUETTE, Leo, A. ,  TOWSON, James, C.

IPC: C07D263/14 ,  C07C315/04 ,  C07D263/16

CPC classification number: C07C315/04 ,  C07B2200/07 ,  C07D263/14 ,  C07D263/16 ,  C07C317/32

Abstract: Processes for preparing oxazoline compounds are disclosed. These oxazoline compounds are useful intermediates in the preparation of Florfenicol and related compounds.

公开(公告)号：EP3303292A1

公开(公告)日：2018-04-11

申请号：EP16730288.4

申请日：2016-06-03

Applicant: Lead Pharma Holding B.V. ,  SANOFI

Inventor： CALS, Joseph Maria Gerardus Barbara ,  DE KIMPE, Vera ,  NABUURS, Sander Bernardus ,  CADICAMO, Cosimo Damiano ,  LEMMERS, Jaap Gerardus Henricus

IPC: C07D213/75 ,  C07D231/12 ,  C07D333/36 ,  C07D233/61 ,  C07C311/20 ,  C07C317/32 ,  C07D409/04 ,  C07D249/08 ,  C07D263/32 ,  C07D271/06 ,  C07D277/46 ,  A61K31/10 ,  A61K31/18 ,  A61P29/00 ,  A61P37/00

CPC classification number: C07C317/32 ,  A61K31/167 ,  A61K31/381 ,  A61K31/415 ,  A61K31/4164 ,  A61K31/4196 ,  A61K31/421 ,  A61K31/4245 ,  A61K31/426 ,  A61K31/4402 ,  A61K31/4436 ,  A61K31/4439 ,  C07C311/20 ,  C07C317/44 ,  C07C2601/02 ,  C07D213/72 ,  C07D213/75 ,  C07D231/12 ,  C07D233/61 ,  C07D249/08 ,  C07D263/32 ,  C07D271/06 ,  C07D277/46 ,  C07D277/54 ,  C07D333/36 ,  C07D409/04 ,  C07D417/12 ,  Y02A50/409

Abstract: The present invention relates to compounds according to Formula I: or a pharmaceutically acceptable salt thereof wherein the variables are as defined in the claims. The compounds can be used as inhibitors of ROR³ and are useful for the treatment of ROR³ mediated diseases.

公开(公告)号：EP3133061A4

公开(公告)日：2017-08-30

申请号：EP14889255

申请日：2014-04-16

Applicant: MASTEAM BIO-TECH CO LTD

Inventor： PENG YAOWU ,  TIAN WENJING ,  YE QING ,  FANG ZHICHENG

IPC: C07C317/32 ,  C07C315/04 ,  C07D263/10 ,  C07D263/20

CPC classification number: C07C315/04 ,  C07D263/10 ,  C07D263/20 ,  C07C317/32

Abstract: The present invention discloses a new florfenicol synthesizing method. The method synthesizes florfenicol products meeting requirements of the Drug Administration by a series of combinations of cyclization, selective reduction, fluorinated open ring, deprotection and acylation, hydroxyl sulfoacid esterified configuration converting reaction, hydrolysis reaction and the like. The synthesizing method of the present invention utilizing chiral amine closed-ring aziridine three-membered ring uses a physical separation method to repeatedly purify chiral aminoketone of high yield obtaining single R configuration, and uses selective reduction and converts the configuration to obtain florfenicol, greatly improving atom economy, while avoiding waste water pollution caused by the existing process, and greatly reducing costs for treating waste water and reducing pollution to the environment, thus lowering costs and simplifying the process. In addition, the present invention uses triethylamine hydrofluoride as a fluorinated open-ring reagent, to improve safety of a liquid reaction compared to a gas reaction and reduce corrosion of equipment, facilitating industrial production.

Abstract translation: 本发明公开了一种新的氟苯尼考合成方法。 该方法通过环化，选择性还原，氟化开环，脱保护和酰化，羟基磺酸酯化构型转化反应，水解反应等一系列组合合成满足药物管理局要求的氟苯尼考产品。 本发明利用手性胺闭环氮丙啶三元环的合成方法采用物理分离的方法反复纯化高收率的手性氨基酮，得到单一R构型，并采用选择性还原将其转化为氟苯尼考，大大提高 同时避免了现有工艺造成的废水污染，大大降低了废水处理成本，减少了对环境的污染，从而降低了成本，简化了工艺流程。 此外，本发明使用三乙胺氢氟酸作为氟化开环试剂，与气体反应相比提高液体反应的安全性并减少设备的腐蚀，促进工业生产。

公开(公告)号：EP3033326A1

公开(公告)日：2016-06-22

申请号：EP14847604.7

申请日：2014-09-24

Applicant: Adesso Advanced Materials Wuxi Co., Ltd.

Inventor： QIN, Bing ,  LI, Xin ,  LIANG, Bo

IPC: C07C251/76 ,  C07C251/86 ,  C07C251/84 ,  C07C249/16 ,  C08G59/50 ,  C08L63/00

CPC classification number: C08G59/4014 ,  C07C251/76 ,  C07C251/84 ,  C07C251/86 ,  C07C317/32 ,  C08G59/245 ,  C08G59/4064 ,  C08G59/50 ,  C08G59/5046 ,  C08J5/042 ,  C08J5/24 ,  C08J11/16 ,  C08J11/24 ,  C08J2363/02 ,  C09D163/00

Abstract: This invention provides, among others, curing agents of Formula II, methods for preparing these curing agents, prepreg materials, degradable cross-linked polymers and reinforced composites made from these curing agents and epoxy resins, and methods for degrading and/or recycling the degradable polymers and reinforced composites.

公开(公告)号：EP2934117A4

公开(公告)日：2016-06-15

申请号：EP13866319

申请日：2013-12-18

Applicant: DOW AGROSCIENCES LLC

Inventor： LO WILLIAM C ,  HUNTER JAMES E ,  WATSON GERALD B ,  PATNY AKSHAY ,  IYER PRAVIN S ,  BORUWA JOSHODEEP

IPC: A01N25/26

CPC classification number: C07D405/04 ,  A01N25/08 ,  A01N33/04 ,  A01N37/10 ,  A01N37/18 ,  A01N37/28 ,  A01N37/32 ,  A01N37/34 ,  A01N37/36 ,  A01N37/46 ,  A01N41/10 ,  A01N43/08 ,  A01N43/16 ,  A01N43/20 ,  A01N43/36 ,  A01N43/38 ,  A01N43/40 ,  A01N43/50 ,  A01N43/54 ,  A01N43/58 ,  A01N43/60 ,  A01N43/653 ,  A01N43/78 ,  A01N43/80 ,  A01N43/82 ,  A01N43/84 ,  A01N47/18 ,  A01N47/28 ,  A01N47/32 ,  A01N47/36 ,  A01N47/38 ,  A01N53/00 ,  C07C63/70 ,  C07C63/74 ,  C07C211/27 ,  C07C211/29 ,  C07C211/42 ,  C07C233/13 ,  C07C233/14 ,  C07C233/56 ,  C07C233/59 ,  C07C233/65 ,  C07C233/66 ,  C07C233/76 ,  C07C233/83 ,  C07C235/80 ,  C07C237/06 ,  C07C237/22 ,  C07C243/34 ,  C07C243/36 ,  C07C243/38 ,  C07C255/57 ,  C07C255/58 ,  C07C259/06 ,  C07C259/08 ,  C07C271/14 ,  C07C275/24 ,  C07C317/32 ,  C07C317/44 ,  C07C323/59 ,  C07C323/60 ,  C07C323/62 ,  C07C323/63 ,  C07C327/42 ,  C07C327/46 ,  C07C327/48 ,  C07C335/12 ,  C07C335/14 ,  C07C2601/02 ,  C07C2602/08 ,  C07C2602/10 ,  C07D207/16 ,  C07D207/27 ,  C07D209/08 ,  C07D209/48 ,  C07D209/50 ,  C07D211/58 ,  C07D213/40 ,  C07D213/56 ,  C07D213/61 ,  C07D213/64 ,  C07D213/74 ,  C07D213/75 ,  C07D233/64 ,  C07D237/32 ,  C07D239/26 ,  C07D241/12 ,  C07D249/08 ,  C07D249/10 ,  C07D249/14 ,  C07D271/10 ,  C07D277/30 ,  C07D277/32 ,  C07D277/64 ,  C07D295/073 ,  C07D295/096 ,  C07D295/155 ,  C07D295/192 ,  C07D307/14 ,  C07D307/16 ,  C07D307/52 ,  C07D309/14 ,  C07D331/04 ,  C07D401/10

Abstract: This document discloses molecules having the following formula (“Formula One”): and processes associated therewith.

公开(公告)号：EP2168944B1

公开(公告)日：2016-05-11

申请号：EP08777226.5

申请日：2008-06-13

Applicant: Mitsubishi Tanabe Pharma Corporation

Inventor： KIUCHI, Masatoshi ,  TASHIRO, Kaoru ,  HAMADA, Maiko ,  SUGAHARA, Kunio

IPC: C07C217/64 ,  A61K31/137 ,  A61K31/165 ,  A61K31/343 ,  A61K31/36 ,  A61K31/381 ,  A61K31/4453 ,  A61K31/5375 ,  A61K31/661 ,  A61P37/02 ,  A61P37/08 ,  A61P41/00 ,  A61P43/00 ,  C07C255/54 ,  C07C255/59 ,  C07C317/22 ,  C07C323/19 ,  C07C323/32 ,  C07D211/14 ,  C07F9/653

CPC classification number: C07C255/54 ,  C07C217/70 ,  C07C255/59 ,  C07C317/32 ,  C07C323/19 ,  C07C323/32 ,  C07C2601/02 ,  C07C2601/14 ,  C07C2602/08 ,  C07C2602/10 ,  C07D211/14 ,  C07D295/08 ,  C07D307/79 ,  C07D317/22 ,  C07D317/62 ,  C07D333/16 ,  C07D333/28 ,  C07D333/56 ,  C07F9/091 ,  C07F9/5456 ,  C07F9/653 ,  C07F9/65517 ,  C07F9/655345 ,  C07F9/655354 ,  C07F9/65586

公开(公告)号：EP2891489A4

公开(公告)日：2016-01-27

申请号：EP13832194

申请日：2013-08-29

Applicant: UNIV TOKYO ,  NIHON NOHYAKU CO LTD

Inventor： KITA KIYOSHI ,  SUWA AKIYUKI ,  ODA MASATSUGU ,  TANAKA KOJI

IPC: A61K31/166 ,  A61K31/415 ,  A61K31/44 ,  A61P33/00 ,  C07C235/60 ,  C07C317/32 ,  C07C323/62 ,  C07D213/61 ,  C07D213/64 ,  C07D213/643 ,  C07D213/74 ,  C07D231/12 ,  C07D231/16 ,  C07D231/18 ,  C07D231/20 ,  C07D401/04

CPC classification number: C07D401/04 ,  A61K31/166 ,  A61K31/415 ,  A61K31/44 ,  C07C233/69 ,  C07C235/46 ,  C07C235/60 ,  C07C317/32 ,  C07C323/42 ,  C07C323/62 ,  C07D213/56 ,  C07D213/61 ,  C07D213/643 ,  C07D213/74 ,  C07D231/12 ,  C07D231/16 ,  C07D231/18 ,  C07D231/20

Abstract: An object of the present invention is to provide a novel endoparasite control agent as a parasiticide, an antiprotozoal or the like. Provided is an endoparasite control agent comprising a carboxamide derivative represented by the general formula (I): or a salt thereof as an active ingredient.

公开(公告)号：EP2891489A1

公开(公告)日：2015-07-08

申请号：EP13832194.8

申请日：2013-08-29

Applicant: The University of Tokyo ,  Nihon Nohyaku Co., Ltd.

Inventor： KITA, Kiyoshi ,  SUWA, Akiyuki ,  ODA, Masatsugu ,  TANAKA, Koji

IPC: A61K31/166 ,  A61K31/415 ,  A61K31/44 ,  A61P33/00

CPC classification number: C07D401/04 ,  A61K31/166 ,  A61K31/415 ,  A61K31/44 ,  C07C233/69 ,  C07C235/46 ,  C07C235/60 ,  C07C317/32 ,  C07C323/42 ,  C07C323/62 ,  C07D213/56 ,  C07D213/61 ,  C07D213/643 ,  C07D213/74 ,  C07D231/12 ,  C07D231/16 ,  C07D231/18 ,  C07D231/20

Abstract: An object of the present invention is to provide a novel endoparasite control agent as a parasiticide, an antiprotozoal or the like. Provided is an endoparasite control agent comprising a carboxamide derivative represented by the general formula (I):

or
a salt thereof as an active ingredient.

Abstract translation: 本发明的一个目的是提供一种新的内寄生虫防治剂作为杀寄生虫剂，抗原生动物剂等。 提供了一种内寄生物防治剂，其包含由通式（I）表示的甲酰胺衍生物或其盐作为活性成分。

公开(公告)号：EP2747759A4

公开(公告)日：2015-05-13

申请号：EP12824979

申请日：2012-08-27

Applicant: COGNITION THERAPEUTICS INC

Inventor： CATALANO SUSAN M ,  RISHTON GILBERT ,  IZZO NICHOLAS J

IPC: A61K31/135 ,  C07C211/28 ,  C07C211/29 ,  C07C215/54 ,  C07C217/58 ,  C07C217/62

CPC classification number: C07D491/107 ,  C07B2200/07 ,  C07C211/28 ,  C07C211/29 ,  C07C215/54 ,  C07C217/58 ,  C07C217/62 ,  C07C235/60 ,  C07C317/32 ,  C07C2601/10 ,  C07C2602/10 ,  C07D209/44 ,  C07D211/14 ,  C07D211/22 ,  C07D295/08 ,  C07D295/096 ,  C07D319/18 ,  C07D491/10

Abstract: This invention relates to novel diarylamino compounds that bind to the sigma-2 receptor, to pharmaceutical compositions comprising such compounds, and to methods for inhibiting or restoring synapse loss in neuronal cells, modulating a membrane trafficking change in neuronal cells, and treating cognitive decline and neurodegenerative diseases and disorders therewith.

Abstract translation: 本发明涉及与σ-2受体结合的新型二芳基氨基化合物，包含这些化合物的药物组合物，以及用于抑制或恢复神经元细胞突触损失，调节神经元细胞膜运输变化和治疗认知衰退的方法，以及 神经变性疾病及其病症。