公开(公告)号：EP3225614A4

公开(公告)日：2018-08-01

申请号：EP15862425

申请日：2015-08-08

申请人： ZHEJIANG JIUZHOU PHARM CO LTD

发明人： ZHOU QILIN ,  XIE JIANHUA ,  YANG XIAOHUI ,  WANG LIXIN

IPC分类号： C07C67/48 ,  B01J31/24 ,  C07C29/149 ,  C07C31/20 ,  C07C33/26 ,  C07C69/675 ,  C07C69/708 ,  C07C69/732 ,  C07D309/30

CPC分类号： C07C69/675 ,  B01J31/181 ,  B01J31/189 ,  B01J31/24 ,  B01J31/249 ,  B01J2231/646 ,  B01J2531/827 ,  C07B53/00 ,  C07B57/00 ,  C07B2200/07 ,  C07C29/149 ,  C07C31/20 ,  C07C33/26 ,  C07C67/48 ,  C07C69/708 ,  C07C69/732 ,  C07D211/02 ,  C07D211/12 ,  C07D305/06 ,  C07D309/06 ,  C07D309/30 ,  C07D473/06

摘要： The present invention relates to kinetic resolution of racemic ´ -hydroxyl ester via asymmetric catalytic hydrogenation and an application thereof. In the presence of chiral spiro pyridyl phosphine ligand Iridium catalyst and base, racemic ´-hydroxyl esters were subjected to asymmetric catalytic hydrogenation to obtain extent optical purity chiral ´-hydroxyl esters and corresponding 1,5-diols. The method is a new, efficient, highly selective, economical, desirably operable and environmentally friendly method suitable for industrial production. An optically active chiral ´ -hydroxyl ester and 1,5-diols can be obtained at very high enantioselectivity and yield with relatively low usage of catalyst. The chiral ´ -hydroxyl ester and 1,5-diols obtained by using the method can be used as a critical raw material for asymmetric synthesis of chiral drugs (R)-lisofylline and natural drugs (+)-civet, (-)-indolizidine 167B and (-)-coniine.

公开(公告)号：EP3055296A1

公开(公告)日：2016-08-17

申请号：EP14781188.9

申请日：2014-10-07

申请人： Bayer CropScience Aktiengesellschaft

发明人： DESBORDES, Philippe ,  RINOLFI, Philippe ,  TSUCHIYA, Tomoki

IPC分类号： C07D401/06 ,  C07D403/06 ,  C07D405/06 ,  C07D405/14 ,  C07D409/06 ,  C07D417/06 ,  C07D207/06 ,  C07D211/12 ,  C07D405/04 ,  A01N43/36 ,  A01N43/56 ,  A01N43/647 ,  A01P3/00

CPC分类号： C07D403/06 ,  A01N43/36 ,  A01N43/56 ,  A01N43/647 ,  A01N43/78 ,  A01N61/00 ,  C07D207/06 ,  C07D211/12 ,  C07D401/06 ,  C07D405/04 ,  C07D405/06 ,  C07D405/14 ,  C07D409/06 ,  C07D417/06

摘要： The present invention relates to fungicidal N-hetarylcarbonyl-2-(benzocycloalken-1-yl)piperidines or pyrrolidines of formula (I), and their thiocarbonyl derivatives, wherein A represents a carbo-linked, unsaturated or partially saturated, 5-membered heterocyclyl group that can be substituted by up to four groups R that can be the same or different; T represents 0 or S; n represents 1 or 2; m represents 1, 2 or 3; p represents 1, 2, 3 or 4, L1 and L2 independently represent CZ4Z5, NZ6, 0, S, S(O) or S(0)2; and R and Z1-Z6 are as defined in the claims; their process of preparation and intermediate compounds for their preparation, their use as fungicides, particularly in the form of fungicidal compositions and methods for the control of phytopathogenic fungi of plants using these compounds or their compositions.

公开(公告)号：EP2762467B1

公开(公告)日：2016-08-03

申请号：EP14152648.3

申请日：2014-01-27

申请人： Takasago International Corporation

发明人： MASHIMA, Kazushi ,  Kita, Yusuke ,  Nagano, Takuto ,  Iimuro, Atsuhiro ,  Yamaji, Kenta ,  Hida, Shoji ,  Hori, Kiyoto ,  Nara, Hideki

IPC分类号： C07D211/12 ,  C07B53/00

CPC分类号： C07D213/26 ,  C07B53/00 ,  C07D211/12

公开(公告)号：EP2118048A2

公开(公告)日：2009-11-18

申请号：EP08701841.2

申请日：2008-01-17

申请人： KING'S COLLEGE LONDON

发明人： AMOBI, Nnaemeka, Ikechukwu ,  SMITH, Christopher

IPC分类号： C07C211/27 ,  C07C211/55 ,  C07C217/56 ,  C07D207/06 ,  C07D207/09 ,  C07D211/04 ,  C07D211/26 ,  C07D211/48 ,  C07D213/38 ,  A61K31/40 ,  A61P15/16

CPC分类号： C07C211/27 ,  C07C211/45 ,  C07C217/16 ,  C07C2603/26 ,  C07D207/09 ,  C07D209/08 ,  C07D211/12 ,  C07D211/14 ,  C07D211/26 ,  C07D215/06 ,  C07D215/12 ,  C07D217/10 ,  C07D221/04 ,  C07D279/26 ,  C07D279/28 ,  C07D295/03 ,  C07D401/06 ,  C07D417/06

摘要： A compound having formula (I). R1, R2, R3 and R4 are independently H or lower alkyl. R5 is aryl, heteroaryl, cycloalkyl, heterocycloalkyl, aryloxy, heteroaryloxy, cycloalkyloxy, heterocycloalkyloxy, arylamino, heteroarylamino, cycloalkylamino, heterocycloalkyl amino, arylthio, heteroarylthio, cycloalkylthio, heterocycloalkylthio, or cyclic olefin, any of which may be substituted or non-substituted; or substituted alkyl, substituted alkyl oxy or substituted alkyl amino wherein the substituent is an aryl, a heteroaryl, a cycloalkyl, a heterocycloalkyl or a cyclic olefin, any of which may be substituted or non-substituted. X is C or N. n and p are independently whole numbers selected from 0,1 and 2. (CH2)n and (CH2)P may be substituted or non-substituted. Ar1 and Ar2 are independently aryl or heteroaryl groups which may be substituted or non-substituted. Certain specific compounds are excluded. The compounds can be used in a medicament or a method for the reduction or prevention of the emission of sperm, or for the reduction or prevention of transmission of viral agents-transmitted in seminal fluid.

公开(公告)号：EP0975595B1

公开(公告)日：2009-06-17

申请号：EP98915409.1

申请日：1998-04-07

申请人： GEORGETOWN UNIVERSITY ,  Kozikowski, Alan, P. ,  Araldi, Gian, Luca

发明人： KOZIKOWSKI, Alan, P. ,  ARALDI, Gian, Luca

IPC分类号： C07D211/60 ,  C07D211/22 ,  A61K31/445 ,  C07D211/20 ,  C07D211/14 ,  C07D211/12

CPC分类号： C07D211/60 ,  C07B59/002 ,  C07B2200/07 ,  C07D211/12 ,  C07D211/14 ,  C07D211/20 ,  C07D211/22

摘要： The invention provides a compound of formula (I), wherein R?1, R2, R3¿, and Y have any of the meanings defined in the specification; as well as a pharmaceutical composition comprising a compound of formula (I); intermediates and methods useful for preparing a compound of formula (I); and therapeutic methods for treating drug addiction, Parkinson's disease or depression comprising administering a compound of formula (I), to a mammal in need of such treatment.

摘要翻译： 本发明提供了式（I）化合物，其中R 1，R 2，R 3和Y具有说明书中定义的任何含义; 以及包含式（I）化合物的药物组合物; 用于制备式（I）化合物的中间体和方法; 和用于治疗药物成瘾，帕金森病或抑郁症的治疗方法，包括给需要这种治疗的哺乳动物施用式（I）化合物。

公开(公告)号：EP1968616A2

公开(公告)日：2008-09-17

申请号：EP07716225.3

申请日：2007-01-04

申请人： Southern Research Institute

发明人： PIAZZA, Gary ,  REYNOLDS, Robert

IPC分类号： A61K31/74

CPC分类号： C07C317/44 ,  C07C323/62 ,  C07C2602/08 ,  C07D207/06 ,  C07D207/09 ,  C07D211/12 ,  C07D213/38 ,  C07D213/40 ,  C07D233/61 ,  C07D233/64 ,  C07D295/108 ,  C07D295/13 ,  C07D307/42 ,  C07D307/52 ,  C07D307/58

摘要： Derivatives of sulindac are provided along with-pharmaceutical compositions containing them and use for precancerous conditions and treating cancer. Derivatives of sulindac are also suitable for treating chronic inflammatory conditions. A method for preparing the derivatives is also provided.

摘要翻译： 提供舒林酸的衍生物以及含有它们的药物组合物，并用于癌前病症和治疗癌症。 舒林酸的衍生物也适用于治疗慢性炎症病症。 还提供了制备衍生物的方法。

公开(公告)号：EP1513513A4

公开(公告)日：2006-08-02

申请号：EP00950822

申请日：2000-07-28

申请人： UNIV KENTUCKY RES FOUND

发明人： DWOSKIN LINDA P ,  CROOKS PETER A ,  JONES MARLON D

IPC分类号： A61K31/445 ,  C07D211/12 ,  C07D211/22 ,  C07D211/32 ,  A61K31/33 ,  A61K31/40 ,  A61K31/55 ,  C07D207/08 ,  C07D207/10 ,  C07D207/12 ,  C07D207/14 ,  C07D207/16 ,  C07D211/18 ,  C07D211/20 ,  C07D211/24 ,  C07D211/26 ,  C07D211/30 ,  C07D225/00

CPC分类号： C07D211/32 ,  A61K31/445 ,  C07D211/12 ,  C07D211/22

公开(公告)号：EP1318988A2

公开(公告)日：2003-06-18

申请号：EP01970926.0

申请日：2001-09-12

申请人： Sepracor, Inc.

发明人： AQUILA, Brian, M. ,  BANNISTER, Thomas, D. ,  CUNY, Gregory, D. ,  HAUSKE, James, R. ,  HOLLAND, Joanne, M. ,  PERSONS, Paul, E. ,  RADEKE, Heike ,  WANG, Fengjian ,  SHAO, Liming

IPC分类号： C07D295/16

CPC分类号： C40B40/04 ,  C07B2200/11 ,  C07C255/46 ,  C07C2601/04 ,  C07D205/02 ,  C07D207/06 ,  C07D207/08 ,  C07D207/09 ,  C07D211/12 ,  C07D211/16 ,  C07D211/18 ,  C07D211/20 ,  C07D211/26 ,  C07D211/32 ,  C07D211/40 ,  C07D211/42 ,  C07D211/60 ,  C07D233/04 ,  C07D233/10 ,  C07D265/30 ,  C07D267/10 ,  C07D303/08 ,  C07D401/06 ,  C07D401/12 ,  C07D405/06 ,  C07D405/12 ,  C07D413/06 ,  C40B30/04 ,  C40B50/14

摘要： One aspect of the present invention relates to heterocyclic compounds formula A; whereof the substituents are defined in the description. A second aspect of the present invention relates to the use of the heterocyclic compounds as ligands for various mammalian cellular receptors, including dopamine, serotonin, or norepinephrine transporters. The compounds of the present invention will find use in the treatment of numerous aliments, conditions and diseases which afflict mammals, including but not limited to addiction, anxiety, depression, sexual dysfunction, hypertension, migraine, Alzheimer's disease, obesity, emesis, psychosis, schizophrenia, Parkinson's disease, inflammatory pain, neuropathic pain, Lesche-Nyhane disease, Wilson's disease, and Tourette's syndrome. An additional aspect of the present invention relates to the synthesis of combinatorial libraries of the heterocyclic compounds, and the screening of those libraries for biological activity, e.g., in assays based on dopamine transporters.

摘要翻译： 本发明的一个方面涉及杂环化合物。 本发明的第二方面涉及杂环化合物作为各种哺乳动物细胞受体（包括多巴胺，5-羟色胺或去甲肾上腺素转运蛋白）的配体的用途。 本发明的化合物可用于治疗多种疾病，包括但不限于成瘾，焦虑，抑郁，性功能障碍，高血压，偏头痛，阿尔茨海默病，肥胖症，呕吐，精神病， 精神分裂症，帕金森病，炎症性疼痛，神经性疼痛，Lesche-Nyhane病，Wilson氏病和Tourette综合征。 本发明的另一方面涉及杂环化合物的组合文库的合成，以及用于生物活性的那些文库的筛选，例如在基于多巴胺转运蛋白的测定中。

公开(公告)号：EP0848707A1

公开(公告)日：1998-06-24

申请号：EP96930216.0

申请日：1996-09-05

申请人： SYNTHELABO

发明人： LARDENOIS, Patrick ,  FROST, Jonathan ,  PASAU, Patrick ,  GEORGE, Pascal ,  RENONES, Maria, Carmen ,  BARTSCH, Régine ,  LI, Wai-Tak ,  MAGAT, Pascale ,  DUPONT, Régis

IPC分类号： C07D211 ,  A61K31 ,  A61P25 ,  C07D401

CPC分类号： C07D401/06 ,  C07D211/12

摘要： Compounds of general formula (I) are described, wherein Ar is (a) a phenyl group substituted with a halogen atom or (b) a group of general formula (I'), wherein X is a group of formula -CH2-, -(CH2)2- or -(CH2)3- and Z is a hydrogen or halogen atom or a methyl group, Y is a group of formula -CH2-, -CO- or -CHOH-, R1 is a hydrogen atom or a methyl group, R2 is a C3-C7 cycloalkyl group, and n is 0, 1, 2 or 3. Said compounds are useful in therapeutical applications as neurotrophic and neuroprotective agents.

公开(公告)号：EP0635504A1

公开(公告)日：1995-01-25

申请号：EP94111307.8

申请日：1994-07-20

申请人： MITSUI TOATSU CHEMICALS, Inc.

发明人： Ogiso, Akira ,  Misawa, Tsutami ,  Imai, Rihoko ,  Itoh, Hisato

IPC分类号： C07D311/12 ,  C07D311/14 ,  C08G63/668 ,  C08K5/00

CPC分类号： C08K5/20 ,  C07D211/12 ,  C08L67/02

摘要： The invention is a 2H-1-benzopyran-2-on compound represented by the formula (1) :

and a colorless ultraviolet absorber consisting of the compound, and a thermoplastic resin composition and formed article comprising said ultraviolet absorber, and can provide a thermoplastic resin composition and a formed article of the composition which have excellent heat stability and sublimation resistance, comprise a non-coloring ultraviolet absorber, and are excellent in ultraviolet barrier property.

摘要翻译： 本发明是由式（1）表示的2H-1-苯并吡喃-2-酮化合物：和由该化合物组成的无色紫外线吸收剂和热塑性树脂组合物和包含所述紫外线吸收剂的成型制品， 提供具有优异的热稳定性和耐升华性的组合物的热塑性树脂组合物和成型体，包含非着色紫外线吸收剂，并且具有优异的紫外线阻隔性。