公开(公告)号：EP3189070A4

公开(公告)日：2018-06-27

申请号：EP15829982

申请日：2015-08-03

申请人： UNIV DREXEL

发明人： KORTAGERE SANDHYA ,  ARTLETT CAROL M

IPC分类号： A61K31/519 ,  A61K31/167 ,  A61K31/4162 ,  A61K31/427 ,  A61K31/4439 ,  A61K38/20 ,  A61K45/06 ,  A61P35/00 ,  C07K14/54

CPC分类号： C07D417/14 ,  A61K31/167 ,  A61K31/36 ,  A61K31/4162 ,  A61K31/427 ,  A61K31/4439 ,  A61K31/47 ,  A61K31/519 ,  A61K38/00 ,  A61K45/06 ,  C07C237/52 ,  C07C317/44 ,  C07C2601/08 ,  C07C2601/14 ,  C07D211/90 ,  C07D215/54 ,  C07D249/08 ,  C07D263/56 ,  C07D309/32 ,  C07D317/58 ,  C07D317/66 ,  C07D401/04 ,  C07D471/04 ,  C07D487/04 ,  C07D491/052 ,  C07D493/04 ,  C07D513/04 ,  A61K2300/00

摘要： The present invention provides compounds useful for treating or preventing an IL-1R-mediated disease or disorder. In certain embodiments, the disease or disorder comprises scleroderma.

公开(公告)号：EP2970157B1

公开(公告)日：2018-04-25

申请号：EP14715479.3

申请日：2014-03-07

申请人： Janssen Pharmaceutica NV

发明人： SUI, Zhihua ,  SUBASINGHE, Nalin L.

IPC分类号： C07D263/56

CPC分类号： C07D307/80 ,  C07D231/56 ,  C07D263/56 ,  C07D277/64 ,  C07D307/79 ,  C07D307/81 ,  C07D307/82 ,  C07D307/84 ,  C07D333/54 ,  C07D333/56 ,  C07D401/12 ,  C07D405/12 ,  C07D493/02 ,  C07D493/04

摘要： The present invention is directed to benzo-fused heterocyclic derivatives, pharmaceutical compositions containing them and their use in the treatment of disorders and conditions modulated by GPR120. More particularly, the compounds of the present invention are agonists of GPR120, useful in the treatment of, such as for example, Type II diabetes mellitus.

公开(公告)号：EP2428504B1

公开(公告)日：2017-05-17

申请号：EP11181871.2

申请日：2009-04-14

申请人： The Board of Regents of the University of Texas System ,  The Arizona Board of Regents on behalf of the University of Arizona

发明人： Mahadevan, Daruka ,  Meuillet, Emmanuelle, J ,  Mash, Eugene, A ,  Gokhale, Vijay, M ,  Powis, Garth ,  Zhang, Shuxing

IPC分类号： C07D213/75 ,  C07D237/18 ,  C07D239/42 ,  C07D239/69 ,  C07D263/40 ,  C07D271/10 ,  C07D285/12 ,  C07D333/36 ,  C07D403/12 ,  C07D405/12 ,  C07D413/12 ,  C07D417/12 ,  C07D285/135 ,  C07D295/135 ,  C07D285/125 ,  C07D401/12 ,  C07D417/10 ,  C07D417/06 ,  C07D413/06 ,  A61K31/433 ,  A61P35/00

CPC分类号： A61K31/433 ,  C07C59/90 ,  C07C65/40 ,  C07C233/75 ,  C07C235/64 ,  C07C237/42 ,  C07C271/22 ,  C07C311/21 ,  C07C317/14 ,  C07C317/18 ,  C07C317/28 ,  C07C317/44 ,  C07C323/65 ,  C07D213/50 ,  C07D213/643 ,  C07D213/74 ,  C07D213/76 ,  C07D231/06 ,  C07D231/12 ,  C07D231/20 ,  C07D231/38 ,  C07D231/42 ,  C07D233/20 ,  C07D233/26 ,  C07D233/64 ,  C07D237/08 ,  C07D237/18 ,  C07D239/26 ,  C07D239/34 ,  C07D239/38 ,  C07D239/42 ,  C07D239/52 ,  C07D261/08 ,  C07D261/20 ,  C07D263/32 ,  C07D263/42 ,  C07D263/56 ,  C07D271/10 ,  C07D271/113 ,  C07D277/52 ,  C07D277/64 ,  C07D285/12 ,  C07D285/125 ,  C07D285/135 ,  C07D295/135 ,  C07D295/192 ,  C07D295/26 ,  C07D333/38 ,  C07D401/12 ,  C07D403/12 ,  C07D405/12 ,  C07D413/06 ,  C07D417/06 ,  C07D417/10 ,  C07D417/12 ,  C07F9/65583

公开(公告)号：EP3095787A1

公开(公告)日：2016-11-23

申请号：EP15169052.6

申请日：2015-05-22

申请人： Universiteit Leiden

发明人： VAN DER STELT, Mario ,  JANSSEN, Freek ,  BAGGELAAR, Marc ,  HUMMEL, Jessica

IPC分类号： C07D498/04 ,  C07D263/56 ,  A61K31/423 ,  A61K31/424 ,  A61P25/30 ,  A61P3/04 ,  A61P25/28

CPC分类号： C07D498/04 ,  C07D263/56

摘要： The present invention relates to novel compounds which are highly selective inhibitors of diacylglycerol lipase α and β. These compounds are suitable for the treatment or prevention of disorders associated with, accompanied by or caused by increased 2-arachidonoylglycerol levels. Diacylglycerol lipase-α (alternative name: Sn1-specific diacylglycerol hydrolase a; DAGL-α) and -β are enzymes responsible for the biosynthesis of the endocannabinoid 2-arachidonoylglycerol. Selective and reversible inhibitors are required to study the function of DAGLs in neuronal cells in an acute and temporal fashion. The inventive ompounds are in particular suitable for the treatment of neurodegenerative diseases, inflammatory diseases, drug abuse and impaired energy balance, such as obesity.

摘要翻译： 本发明涉及二酰基甘油脂肪酶±和²的高选择性抑制剂的新型化合物。 这些化合物适用于治疗或预防与2-花生四烯酰甘油水平升高伴随或引起的疾病。 二酰基甘油脂肪酶（替代名称：Sn1特异性二酰基甘油水解酶a; DAGL-±）和--2是负责内源性大麻素2-花生四烯酰甘油的生物合成的酶。 需要选择性和可逆抑制剂以急性和时间方式研究神经元细胞中DAGLs的功能。 本发明的特征特别适用于治疗神经变性疾病，炎性疾病，药物滥用和受损的能量平衡，例如肥胖症。

公开(公告)号：EP3059225A1

公开(公告)日：2016-08-24

申请号：EP14853664.2

申请日：2014-10-17

申请人： Shionogi & Co., Ltd.

发明人： KOBAYASHI, Naotake ,  ASAHI, Kentarou ,  TOMIDA, Yutaka ,  OHDAN, Masahide ,  FUMOTO, Masataka ,  SASAKI, Yoshikazu ,  KURAHASHI, Kana ,  INOUE, Takatsugu ,  URABE, Tomomi ,  NISHIURA, Yuji ,  IWATSU, Masafumi ,  MIYAZAKI, Keisuke ,  OHYABU, Naoki ,  WADA, Toshihiro ,  KATOU, Manabu

IPC分类号： C07C233/18 ,  A61K31/165 ,  A61K31/17 ,  A61K31/416 ,  A61K31/423 ,  A61K31/426 ,  A61K31/4725 ,  A61K31/4965 ,  A61K31/497 ,  A61K31/506 ,  A61K31/517 ,  A61K31/553 ,  A61P3/04 ,  A61P3/10 ,  A61P43/00 ,  C07C233/31 ,  C07C275/24 ,  C07D213/64 ,  C07D213/69 ,  C07D231/56

CPC分类号： C07C233/22 ,  C07C233/18 ,  C07C233/31 ,  C07C275/10 ,  C07C2601/02 ,  C07D213/64 ,  C07D213/69 ,  C07D231/56 ,  C07D239/80 ,  C07D241/18 ,  C07D261/20 ,  C07D263/56 ,  C07D267/14 ,  C07D277/20 ,  C07D277/34 ,  C07D277/64 ,  C07D277/68 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D403/14 ,  C07D413/12 ,  C07D417/12

摘要： The object of the present invention is to provide novel compounds having ACC2 inhibiting activity. In addition, the object of the present invention is to provide a pharmaceutical composition comprising the compound.
A compound of formula (I):

wherein R 1 is substituted or unsubstituted fused aromatic heterocyclyl etc., ring A is substituted or unsubstituted non-aromatic carbocycle etc.,
-L 1 - is -O-(CR 6 R 7 )m- etc.,
-L 2 - is -O-(CR 6 R 7 )n- etc.,
each R 6 and R 7 are independently hydrogen, halogen etc.,
R 2 is substituted or unsubstituted alkyl,
R 3 is hydrogen or substituted or unsubstituted alkyl,
R 4 is substituted or unsubstituted alkylcarbonyl etc..

摘要翻译： 本发明的目的是提供具有ACC2抑制活性的新型化合物。 此外，本发明的目的是提供一种包含该化合物的药物组合物。 式（I）的化合物：其中R 1是取代或未取代的稠合芳族杂环基等，环A是取代或未取代的非芳族碳环等，-L 1 - 是-O-（CR 6 R 7）m- 等等，-L 2 - 为-O-（CR 6 R 7）n - 等，每个R 6和R 7独立地为氢，卤素等，R 2为取代或未取代的烷基，R 3为氢或取代 或未取代的烷基，R 4为取代或未取代的烷基羰基等。

公开(公告)号：EP2970158A2

公开(公告)日：2016-01-20

申请号：EP14720006.7

申请日：2014-03-14

申请人： Edison Pharmaceuticals, Inc.

发明人： HINMAN, Andrew, W. ,  WESSON, Kieron, E. ,  CORNELL, Christopher, R.

IPC分类号： C07D263/56 ,  C07D233/60 ,  C07D233/64 ,  C07D235/06 ,  C07D235/12 ,  C07D403/10 ,  C07D249/08 ,  C07D471/04 ,  C07D263/32 ,  C07D277/24 ,  C07D277/64 ,  A61K31/4184 ,  A61K31/428 ,  A61K31/423 ,  A61K31/4164

CPC分类号： C07D471/04 ,  C07D233/60 ,  C07D233/64 ,  C07D235/06 ,  C07D235/12 ,  C07D249/08 ,  C07D263/32 ,  C07D263/56 ,  C07D263/57 ,  C07D277/24 ,  C07D277/64 ,  C07D403/10

摘要： Disclosed herein are alkyl-heteroaryl substituted quinone derivative compounds and methods of using such compounds for treating or suppressing oxidative stress disorders, including mitochondrial disorders, impaired energy processing disorders, neurodegenerative diseases and diseases of aging.

公开(公告)号：EP2468275B1

公开(公告)日：2015-11-04

申请号：EP11192904.8

申请日：2002-06-14

申请人： Biodiem Ltd.

发明人： Denisenko, Peter Prokofievich ,  Sapronov, Nikolay Sergeevich ,  Tarasenko, Alexander Alexandrovich

IPC分类号： A61K31/4184 ,  A61P31/04

CPC分类号： A61K31/357 ,  A61K31/36 ,  A61K31/4184 ,  C07D235/06 ,  C07D235/08 ,  C07D263/56 ,  C07D317/46 ,  C07D317/52 ,  Y02A50/401 ,  Y02A50/409 ,  Y02A50/411 ,  Y02A50/47 ,  Y02A50/471 ,  Y02A50/473 ,  Y02A50/475 ,  Y02A50/479 ,  Y02A50/481

摘要： The present invention relates to a method of treatment and/or prophylaxis of a microbial infection, comprising the step of administering an effective amount of a compound of formula (I), in which X and Y are either the same or different and selected from a heteroatom; is a double or single bond depending on the heteroatoms X and Y; R 1 to R 5 are either the same or different and selected from hydrogen or a non-deleterious substituent; and R 6 and R 7 are either the same or different and selected from hydrogen and a non-deleterious substituent or one of R 6 and R 7 are absent when there is a double bond present, pharmaceutically acceptable salts or derivatives, pro-drugs, tautomers and/or isomers thereof. The present invention also relates to a method for protecting a subject from radiation damage, a method of cancer radiotherapy and use as an antimicrobial or radioprotective agent of the compound of formula (I) defined above. Some of the compounds of formula (I) are novel and are also described in the present invention, together with pharmaceutical or veterinary compositions containing them.

公开(公告)号：EP2217650B1

公开(公告)日：2015-10-21

申请号：EP08859554.1

申请日：2008-12-02

申请人： Henkel AG & Co. KGaA ,  Henkel IP & Holding GmbH

发明人： KREILING, Stefan ,  SCHONFELD, Rainer ,  TADEN, Andreas ,  LEHMANN, Stanley, L.

IPC分类号： C07D263/62 ,  C07D498/06 ,  C08K5/357

CPC分类号： C08K5/357 ,  C07D263/56 ,  C07D263/62 ,  C08G18/12 ,  C08G18/6677 ,  C08G73/0233 ,  C08L79/02 ,  C08G18/3237

公开(公告)号：EP2804855A4

公开(公告)日：2015-07-29

申请号：EP13738359

申请日：2013-01-16

申请人： SHANGHAI KECHOW PHARMA INC

发明人： TIAN HONGQI ,  JI CONGHUI ,  LIU CHUNLEI ,  KONG LI ,  CHENG YING ,  HUANG GONGCHAO

IPC分类号： C07D263/54 ,  A61K31/41 ,  A61K31/42 ,  A61K31/425 ,  A61K31/433 ,  A61P29/00 ,  A61P35/00 ,  C07D209/02 ,  C07D231/54 ,  C07D277/62 ,  C07D285/14

CPC分类号： A61K31/433 ,  A61K31/423 ,  A61K31/428 ,  C07D263/56 ,  C07D277/62 ,  C07D277/64 ,  C07D285/14

摘要： Disclosed are compound of formula (I) and pharmaceutically accepted salts and prodrugs thereof, wherein each of R1, R2, R3, R4, R5, R6, X1 and X2 is as defined in the description. These compounds are protein kinases inhibitors, especially the inhibitors of Mek, which are useful in the treatment of cancers and inflammation of mammals. Disclosed are the treatment methods of cancers and inflammation of mammals as well as pharmaceutical compositions comprising the compounds described herein. The preparation of benzoheterocyclic compounds are disclosed. Disclosed are the preparation of potential drug candidates, such as benzooxazol, benzothiazol, benzothiadiazol and the like.

公开(公告)号：EP2892345A1

公开(公告)日：2015-07-15

申请号：EP13758839.8

申请日：2013-09-03

申请人： Bayer CropScience AG

发明人： FRACKENPOHL, Jens ,  HEINEMANN, Ines ,  MÜLLER, Thomas ,  DITTGEN, Jan ,  VON KOSKULL-DÖRING, Pascal ,  SCHMUTZLER, Dirk ,  HILLS, Martin Jeffrey

IPC分类号： A01N43/52 ,  A01N43/76 ,  A01N43/78 ,  C07D235/08 ,  C07D235/10 ,  C07D235/12 ,  C07D235/14 ,  C07D235/18 ,  C07D263/54 ,  C07D263/56 ,  C07D263/62 ,  C07D277/62 ,  C07D277/64 ,  C07D277/66 ,  C07D411/04

CPC分类号： A01N43/78 ,  A01N43/52 ,  A01N43/76 ,  A01N47/16 ,  C07D235/08 ,  C07D235/10 ,  C07D235/12 ,  C07D235/14 ,  C07D235/18 ,  C07D263/54 ,  C07D263/56 ,  C07D263/57 ,  C07D263/62 ,  C07D277/62 ,  C07D277/64 ,  C07D277/66 ,  C07D401/04 ,  C07D401/10 ,  C07D403/04 ,  C07D403/10 ,  C07D405/04 ,  C07D405/12 ,  C07D409/04 ,  C07D409/12 ,  C07D413/04 ,  C07D413/10 ,  C07D417/10 ,  C07D471/04 ,  C07D471/08 ,  C07D487/08 ,  C07F7/1856

摘要： The invention relates to the use of substituted 2-amidobenzimidazoles, 2-amidobenzoxazoles and 2-amidobenzothiazoles of general formula (I) or the salts thereof, the groups in general formula (I) corresponding to the definitions cited in the description, for increasing the stress tolerance of plants to abiotic stress, for strengthening plant growth and/or for increasing the plant yield. The invention also relates to specific methods for producing said compounds.