公开(公告)号：EP2155703A1

公开(公告)日：2010-02-24

申请号：EP08750615.0

申请日：2008-05-16

申请人： Inhibox Ltd.

发明人： JIRGENSONS, Aigars ,  LEITIS, Gundars ,  KALVINSH, Ivars ,  ROBINSON, Daniel ,  FINN, Paul ,  KHAN, Nagma

IPC分类号： C07D275/06 ,  C07D401/12 ,  C07D411/10 ,  C07D413/10 ,  C07D513/04 ,  A61K31/428 ,  A61P19/02 ,  A61P29/00 ,  A61P37/00

CPC分类号： C07D417/10 ,  C07D275/06 ,  C07D417/04 ,  C07D417/12

摘要： This invention pertains generally to the field of therapeutic compounds, and more particularly, to certain bicyclosulfonyl acid (BCSA) compounds which act as inhibitors of Tumour Necrosis Factor-α Converting Enzyme (TACE). The compounds are useful in the treatment of conditions mediated by TNF-α, such as rheumatoid arthritis; inflammation; psoriasis; septic shock; graft rejection; cachexia; anorexia; congestive heart failure; post ischaemic reperfusion injury; inflammatory disease of the central nervous system; inflammatory bowel disease; insulin resistance; HIV infection; cancer; chronic obstructive pulmonary disease (COPD); and asthma. The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo, in the inhibition of TACE, and in the treatment of conditions that are ameliorated by the inhibition of TACE.

公开(公告)号：EP1200423A1

公开(公告)日：2002-05-02

申请号：EP00949242.2

申请日：2000-07-03

申请人： Bayer Aktiengesellschaft

发明人： ANDREE, Roland ,  DREWES, Mark-Wilhelm ,  DAHMEN, Peter ,  FEUCHT, Dieter ,  PONTZEN, Rolf

IPC分类号： C07D405/10 ,  C07D409/10 ,  C07D411/10 ,  A01N43/54

CPC分类号： C07D405/10 ,  A01N43/54 ,  C07D409/10 ,  C07D411/10

摘要： The invention relates to novel substituted phenyl uracils of general formula (I), wherein A represents alkanediyl or alkenediyl, optionally substituted with cyano, halogen or C1-C4-alkyl, C1-C4-alkoxycarbonyl or C2-C4-alkenyl, optionally substituted with halogen or C1-C4-alkoxy; or interrupted with O (oxygen), with 2 to 5 carbon atoms, respectively, or cyclohexane-1,2-diyl or 1,2-phenylene; Q1 represents O (oxygen) or S (sulphur); Q2 represents O (oxygen) or S (sulphur); R1 represents hydrogen, amino or alkyl, optionally substituted with cyano, halogen or C¿1?-C4-alkoxy, with 1 to 4 carbon atoms; R?2¿ represents alkyl substituted with halogen and with 1 to 4 carbon atoms; R3 represents hydrogen, halogen or alkyl, optionally substituted with halogen and with 1 to 4 carbon atoms; R4 represents hydrogen, cyano, carbamoyl, thiocarbamoyl or halogen; R5 represents cyano, carbamoyl, thiocarbamoyl or alkyl or alkoxy, optionally substituted with halogen and with 1 to 4 carbon atoms, respectively; and R6 represents hydrogen or alkyl with 1 to 4 carbon atoms. The invention also relates to a method for producing the inventive phenyl uracils and to their use as herbicides.

公开(公告)号：EP0958292B1

公开(公告)日：2007-01-03

申请号：EP98907930.6

申请日：1998-01-08

申请人： BASF Aktiengesellschaft

发明人： VON DEYN, Wolfgang ,  HILL, Regina, Luise ,  BAUMANN, Ernst ,  ENGEL, Stefan ,  MAYER, Guido ,  RHEINHEIMER, Joachim ,  WITSCHEL, Matthias ,  MISSLITZ, Ulf ,  WAGNER, Oliver ,  OTTEN, Martina ,  WALTER, Helmut ,  WESTPHALEN, Karl-Otto

IPC分类号： C07D413/10 ,  A01N43/72 ,  A01N43/48 ,  C07D417/10 ,  C07D409/10 ,  C07D405/10 ,  C07D401/10 ,  C07D403/10 ,  C07D411/10 ,  C07D231/20 ,  C07D231/24

CPC分类号： C07D231/20 ,  C07D261/04 ,  C07D261/20 ,  C07D413/10 ,  C07D417/10

摘要： The invention concerns 4-(3-heterocyclyl-1-benzoyl)pyrazoles of formula (I) in which the variables have the following meanings: R1, R3: hydrogen, nitro, halogen, cyano, alkyl, alkyl halide, alkoxy, alkoxy halide, alkylthio, alkylthio halide, alkylsulphinyl, alkylsulphinyl halide, alkylsulphonyl, alkylsulphonyl halide, aminosulphonyl, N-alkylaminosulphonyl, N,N-dialkylaminosulphonyl, N-alkylsulphonylamino, N-alkylsulphonylamino halide, N-alkyl-N-alkylsulphonylamino or N-alkyl-N-alkylsulphonylamino halide; R2: an optionally substituted 5- or 6-member heterocyclyl group containing between 1 and 4 identical or different heteroatoms selected from the group comprising oxygen, sulphur or nitrogen; R4: hydrogen, halogen or alkyl; R5: substituted pyrazole bonded in position 4. The invention also concerns: the salts of these 4-(3-heterocyclyl-1-benzoyl)pyrazoles which can be used for agricultural purposes; processes for preparing these substances; agents containing them; and the use as herbicides of these derivatives or agents containing them.

公开(公告)号：EP0532705A4

公开(公告)日：1993-05-05

申请号：EP91915103

申请日：1991-05-24

申请人： RHONE-POULENC RORER INTERNATIONAL (HOLDINGS) INC.

发明人： HUANG, FU-CHIH ,  LEARN, KEITH, STEWARD ,  GAVAI, ASHVIN, V.

IPC分类号： A61K31/47 ,  A61P29/00 ,  A61P37/08 ,  C07D401/10 ,  C07D401/12 ,  C07D401/14 ,  C07D405/10 ,  C07D405/12 ,  C07D405/14 ,  C07D409/10 ,  C07D409/12 ,  C07D409/14 ,  C07D411/10 ,  C07D411/12 ,  C07D411/14 ,  C07D413/10 ,  C07D413/12 ,  C07D413/14 ,  C07D417/10 ,  C07D417/12 ,  C07D417/14 ,  C07D419/10 ,  C07D419/12

CPC分类号： C07D409/12 ,  C07D409/14 ,  C07D413/12 ,  C07D413/14

摘要： This invention relates to certain quinolinyl-benzoheterobicyclic compounds and their use as valuable pharmaceutical agents, particularly as lipoxygenase inhibitors and/or leukotriene antagonists and/or as mediator release inhibitors useful as anti-inflammatory and anti-allergic agents.

公开(公告)号：EP0320677A1

公开(公告)日：1989-06-21

申请号：EP88119635.6

申请日：1988-11-25

申请人： BASF Aktiengesellschaft

发明人： Rueb, Lothar, Dr. ,  Eicken, Karl, Dr. ,  Schwalge, Barbara, Dr. ,  Plath, Peter, Dr. ,  Wuerzer, Bruno, Dr. ,  Meyer, Norbert, Dr.

IPC分类号： C07D409/10 ,  C07D411/10 ,  A01N43/38

CPC分类号： A01N43/28 ,  A01N43/24 ,  A01N43/32 ,  C07D409/10 ,  C07D411/10

摘要： N-Phenyltetrahydrophthalimide der allgemeinen Formel I
in der bedeutet:

R 1 Wasserstoff oder Halogen
R 2 Halogen
A einen Substituenten der Formel

oder

wobei bedeutet:

X Sauerstoff oder Schwefel
n die Zahlen 0 oder 1
R 3 Wasserstoff oder ein gegebenenfalls durch Halogen, Cyano, Hydroxy, Mercapto, C 1 -C 6 -Alkoxycarbonyl. C 1 -C 4 -Alkoxy, C 1 -C 4 -Alkylthio, C 3 -C 6 -Alkenyloxy, C 3 -C 6 -Alkenylthio, C 3 -C 6 -Alkinyloxy, C 3 -C s -Alki- nylthio, C 1 -C 5 -Acyloxy substituiertes C 1 -C 3 -Alkyl oder C 1 -C 6 -Alkoxycarbonyl, Hydroxyl oder Carboxyl oder ein im Alkylether- oder Thioetherteil durch C 1 -C 6 -Alkoxycarbonyl substituiertes C 1 -C 4 -Alkoxy-C 1 -C 2 -alkyl oder C 1 -C 4 -Alkylthio-C 1 -C 2 -alkyl
R 4 Wasserstoff oder C 1 -C 3 -Alkyl
Z Methylenoxymethylen, Methylenthiomethylen oder Ethenylen (-CH = CH-)
R 5 Wasserstoff oder C 1 -C 3 -Alkyl und
R 5 Wasserstoff oder C 1 -C 3 -Alkyl bedeutet, ein Verfahren zu ihrer Herstellung und ihre Verwendung als Herbizide.

摘要翻译： 通式的N- PhenyltetrahydrophthalimideⅠ中的意思是：R1是氢或卤素R 2卤素，A是下式的取代基，或其中表示：X是氧或硫，数字0或1 R 3为氢或任选地被卤素，氰基，羟基，巯基N， C1-C6烷氧基羰基。 C1-C4烷氧基，C1-C4烷硫基，C3-C6链烯氧基，C3-C6链烯基，C3-C6炔氧基，C3-CS - 炔基nylthio，C1-C5酰氧基取代的C1-C3烷基或 C1-C6烷氧羰基，羟基或羧基，或者被C1-C6烷氧羰基中的烷基醚或Thioetherteil取代的，C1-C4烷氧基C1-C2烷基或C1-C4烷硫基C1-C2烷基R4是氢或C1 1 -C 3烷基žmethyleneoxymethylene，Methylenthiomethylen或亚乙烯基（-CH = CH-）R5是氢或C1-C3烷基和R5是氢或C1-C3烷基，其制备方法和它们作为除草剂的用途。

公开(公告)号：EP1501819B1

公开(公告)日：2010-09-15

申请号：EP03736470.0

申请日：2003-04-18

申请人： Merck Sharp & Dohme Corp.

发明人： DININNO, Frank, P. ,  BLIZZARD, Timothy, Allen ,  MORGAN, Jerry, Dwain, II

IPC分类号： C07D327/06 ,  C07D411/10 ,  A61K31/382 ,  A61P5/30

CPC分类号： C07D327/06

摘要： The present invention relates to compounds and derivatives thereof, their synthesis, and their use as estrogen receptor modulators. The compounds of the instant invention are ligands for estrogen receptors and as such may be useful for treatment or prevention of a variety of conditions related to estrogen functioning including: bone loss, bone fractures, osteoporosis, cartilage degeneration, endometriosis, uterine fibroid disease, hot flashes, increased levels of LDL cholesterol, cardiovascular disease, impairment of cognitive functioning, cerebral degenerative disorders, restenosis, gynecomastia, vascular smooth muscle cell proliferation, obesity, incontinence, and cancer, in particular of the breast, uterus and prostate.

公开(公告)号：EP1611120A1

公开(公告)日：2006-01-04

申请号：EP04726068.2

申请日：2004-04-07

申请人： Cortical Pty Ltd

发明人： MORAND, Eric, Francis ,  ISKANDER, Magdy, Naguib ,  SKENE, Colin, Edward

IPC分类号： C07D317/20 ,  C07D277/04 ,  C07D417/10 ,  C07D317/30 ,  C07D317/22 ,  C07D317/16 ,  C07D317/12 ,  C07D231/12 ,  C07D213/69 ,  C07D339/06 ,  C07D319/06 ,  C07D411/10

CPC分类号： C07D213/69 ,  C07C43/225 ,  C07D231/12 ,  C07D233/02 ,  C07D239/04 ,  C07D251/04 ,  C07D263/10 ,  C07D263/12 ,  C07D277/04 ,  C07D317/12 ,  C07D317/16 ,  C07D317/20 ,  C07D317/22 ,  C07D317/30 ,  C07D317/34 ,  C07D319/06 ,  C07D327/04 ,  C07D327/06 ,  C07D339/06 ,  C07D405/12 ,  C07D411/10 ,  C07D417/10

摘要： Methods of inhibiting the cytokine or biological activity of Macrophage Migration Inhibitory Factor (MIF) comprising contacting MIF with a compound of formula (I) are provided. The invention also relates to methods of treating diseases or conditions where MIF cytokine or biological activity is implicated comprising administration of compounds of formula (I), either alone or as a part of combination therapy. Novel compounds of formula (I) are also provided for.

公开(公告)号：EP0716653B1

公开(公告)日：2000-04-26

申请号：EP94925477.5

申请日：1994-08-25

申请人： BASF AKTIENGESELLSCHAFT

发明人： SCHÄFER, Peter ,  KLINTZ, Ralf ,  HAMPRECHT, Gerhard ,  HEISTRACHER, Elisabeth ,  WESTPHALEN, Karl-Otto ,  GERBER, Matthias ,  WALTER, Helmut

IPC分类号： C07D239/54 ,  A01N43/54 ,  C07D405/10 ,  C07D409/10 ,  C07D411/10

CPC分类号： C07D239/54 ,  A01N43/54 ,  C07D405/10 ,  C07D409/10 ,  C07D411/10

摘要： Substituted 1-amino-3-phenyluracils (I), where the variables have the following meanings: R1 = H, F, Cl; Y = O, S; W = -CH=N-OH, -CH=N-O-(alkyl), -CH=N-O-(alkylene)-O-(alkyl), -CH=N-O-CH¿2?-COOH, -CH=N-O-CH(alkyl)-COOH, -CH=N-O-CH2-CO-O-(alkyl), -CH=N-O-CH(alkyl)-CO-O-(alkyl), -CH=N-O-CH2-CO-O-(alkylene)-O-(alkyl), -CH=N-O-CH(alkyl)-CO-O-(alkylene)-O-(alkyl), -CH=CH-CO-O-(alkyl), -CH=CH-CO-O-(alkylene)-O-(alkyl), -CH=C(Cl)-CO-O-(alkyl), -CH=C(Br)-CO-O-(alkyl), -CH=C(Cl)-CO-O(alkylene)-O-(alkyl), -CH=C(Br)-CO-O-(alkylene)-O-(alkyl), -CH=C(CH3)-CO-O-(alkyl), -CH=C(CH3)-CO-O-(alkylene)-O-(alkyl), -CH[X?1¿-(alkyl)][X2-(alkyl)] or a radical (a), (b), X1-X6 = O, S; R2-R11 = H, alkyl, vinyl, alkoxycarbonyl are described. Use: herbicides; desiccation/defoliation of plants.

公开(公告)号：EP3342765B1

公开(公告)日：2021-09-15

申请号：EP16840786.4

申请日：2016-08-26

发明人： WANG, Xiaojun ,  ZHOU, Pingjian ,  YANG, Chuanwen ,  HUANG, Changwei ,  XIONG, Shaohui ,  ZHANG, Yingjun ,  ZHANG, Jiancun

IPC分类号： C07C255/29 ,  C07C255/46 ,  C07C209/42 ,  C07C215/48 ,  C07C233/54 ,  C07C277/02 ,  A61K31/275 ,  C07D413/14 ,  A61K45/06 ,  A61K31/343 ,  A61K31/351 ,  A61K31/357 ,  A61K31/36 ,  A61K31/38 ,  C07D405/10 ,  C07D407/14 ,  C07D409/10 ,  C07D411/10 ,  C07D417/10 ,  C07D417/14

公开(公告)号：EP2714032B1

公开(公告)日：2019-01-16

申请号：EP12793162.4

申请日：2012-06-01

申请人： Green Cross Corporation

发明人： CHOI, Soongyu ,  SONG, Kwang-Seop ,  LEE, Suk Ho ,  KIM, Min Ju ,  SEO, Hee Jeong ,  PARK, Eun-Jung ,  KONG, Younggyu ,  PARK, So Ok ,  KANG, Hyunku ,  JUNG, Myung Eun ,  LEE, Kinam ,  KIM, Hyun Jung ,  LEE, Jun Sung ,  LEE, Min Woo ,  KIM, Mi-Soon ,  HONG, Dong Ho ,  KANG, Misuk

IPC分类号： A61K31/357 ,  A61K31/343 ,  A61K31/35 ,  A61K31/015 ,  A61P3/00 ,  C07D309/10 ,  C07D405/14 ,  C07D405/10 ,  C07D407/04 ,  C07D407/10 ,  C07D407/14 ,  C07D409/04 ,  C07D409/10 ,  C07D411/10 ,  C07D413/04 ,  C07D413/10 ,  C07D413/14 ,  C07D413/12 ,  C07D409/14