公开(公告)号：EP1626720A1

公开(公告)日：2006-02-22

申请号：EP04725291.1

申请日：2004-04-02

申请人： H. LUNDBECK A/S

发明人： PÜSCHL, Ask ,  JORGENSEN, Morten ,  RUHLAND, Thomas ,  BRYAN, STENSBOl, Tine ,  BANG-ANDERSEN, Benny

IPC分类号： A61K31/451 ,  C07D211/24 ,  C07D407/12 ,  A61P25/00

CPC分类号： C07D405/12 ,  C07D211/20 ,  C07D211/24

摘要： The invention provides compounds represented by the general formula (I) wherein the substituents are defined in the application. The compounds are useful in the treatment of an affective disorder, including depression, anxiety disorders including general anxiety disorder and panic disorder and obsessive compulsive disorder.

公开(公告)号：EP1572207A1

公开(公告)日：2005-09-14

申请号：EP03814662.7

申请日：2003-12-08

申请人： FMC CORPORATION

发明人： DING, Ping ,  HENRIE II, Robert, H. ,  COHEN, Daniel, H. ,  LYGA, John, W. ,  ROSEN, David, S. ,  THEODORIDIS, George ,  ZHANG, Qun ,  YEAGER, Walter, H. ,  DONOVAN, Stephen, F. ,  ZHANG, Steven, Shunxiang ,  SHULMAN, Inna ,  YU, Seong, Jae ,  WANG, Guozhi ,  ZHANG, Y., Larry ,  GOPALSAMY, Ariamala ,  WARKENTIN, Dennis, L. ,  RENSNER, Paul, E. ,  SILVERMAN, Ian, R. ,  CULLEN, Thomas, G.

IPC分类号： A61K31/44 ,  C07D401/02

CPC分类号： C07D405/14 ,  A01N43/40 ,  A01N43/54 ,  A01N43/713 ,  C07D211/14 ,  C07D211/18 ,  C07D211/22 ,  C07D211/24 ,  C07D211/26 ,  C07D211/28 ,  C07D211/32 ,  C07D211/94 ,  C07D401/06 ,  C07D401/10 ,  C07D401/12 ,  C07D401/14 ,  C07D413/12 ,  C07D417/12 ,  C07D451/14 ,  C07D513/04

摘要： It has now been found that certain novel N-(substituted aryl)-4(disubstituted methyl)piperidine and pyridine derivatives have provided unexpected insecticidal activity. These compounds are represented by formula (I): wherein m, n, q, r, and s are independently selected fronn 0 or 1 ; and p is 0, 1, 2, or 3; A is C or CH; and B, D, E, R, R1, R2, R3, R4, R5, R6, R7 and R8 are fully described herein. In addition, compositions comprising an insecticidally effective amount of at least one compound of formula I, and optionally, an effective amount of at least one of a second compound, with at least one insecticidally compatible carrier are also disclosed; along with methods of controlling insects comprising applying said compositions to a locus where insects are present or are expected to be present.

公开(公告)号：EP1433783A2

公开(公告)日：2004-06-30

申请号：EP04006920.5

申请日：1999-10-04

申请人： AstraZeneca AB

发明人： Dedinas, Robert, AstraZeneca R&D Wilmington ,  Bernstein, Peter, AstraZeneca R&D Wilmington ,  Ohnmacht, Cyrus Jr., AstraZeneca R&D Wilmington ,  Russell, Keith, AstraZeneca R&D Wilmington ,  Sherwood, Scott Alan

IPC分类号： C07D211/24 ,  A61K31/445 ,  C07C255/57 ,  C07C235/66 ,  C07D417/12 ,  C07D211/26 ,  C07F9/59 ,  C07D413/10 ,  C07D401/04 ,  C07D211/22 ,  C07D211/34 ,  C07D211/20

CPC分类号： C07D401/04 ,  C07C235/66 ,  C07C255/57 ,  C07D211/18 ,  C07D211/22 ,  C07D211/24 ,  C07D211/26 ,  C07D211/28 ,  C07D211/34 ,  C07D211/76 ,  C07D401/10 ,  C07D413/10 ,  C07D417/12 ,  C07F9/592

摘要： A compound having the formula (I)
wherein R 1 is oxo, -OR a , -OC(=O)R b ; or (A);
R 2 is H; or R 1 is -OR c and R 2 is -OR d ; or R 1 and R 2 together form -O(CH 2 ) m O-; R 3 is H or alkyl; R 4 , R 5 and R 6 are independently selected from hydroxy, cyano, nitro, trifluoromethoxy, trifluoromethyl, alkylsulfonyl, halo, alkoxy, alkyl, cyanoalkyl, alkenyl, alkynyl, carboxy, alkoxy-carbonyl, carbamoyl, alkylcarbamoyl, di-alkylcarbamoyl, alkanoyl, alkanoylamino, aminosulfonyl, and substituted alkyl; or R 4 and R 5 together form -OCH 2 O- or -OC(CH 3 ) 2 O-; R 6 may additionally be hydrogen; R 7 is substituted phenyl; R 8 is selected from hydrogen, hydroxy, alkoxy, alkanoyloxy, alkanoyl, alkoxycarbonyl, alkanoylamino, alkyl, carbamoyl, alkylcarbamoyl, and bis(alkyl)carbamoyl; R a is hydrogen or alkyl; R b is alkyl, aryl or arylalkyl; R c and R d are independently selected from alkyl; m is 2, 3, or 4; and X 1 and X 2 are independently H or halogen, wherein at least one of X 1 and X 2 are halogen; and any pharmaceutically-acceptable salt thereof along with their use in treating depression, anxiety, asthma, rheumatoid arthritis, Alzheimer's disease, cancer, schizophrenia, oedema, allergic rhinitis, inflammation, pain, gastrointestinal-hypermotility, anxiety, emesis, Huntington's disease, psychoses including depression, hypertension, migraine, bladder hypermotility, or urticaria, along with methods of making the compounds and pharmaceutical compositions containing the compounds.

摘要翻译： 具有式CHEM的化合物，其中R 1是氧代，-OR a，-OC（= O）R b; 或 R 2为H; 或R 1为-OR c且R 2为-OR d。 或R 1和R 2一起形成-O（CH 2）m O-; 焦虑，哮喘，类风湿关节炎，阿尔茨海默氏病，癌症，精神分裂症，水肿，过敏性鼻炎，炎症，疼痛，胃肠道过度运动，焦虑，呕吐，亨廷顿病，精神病 包括抑郁症，高血压，偏头痛，膀胱过度运动或荨麻疹，以及制备含有化合物的化合物和药物组合物的方法。

公开(公告)号：EP1428822A2

公开(公告)日：2004-06-16

申请号：EP03027033.4

申请日：2000-12-22

申请人： A. Carlsson Research AB

发明人： Sonesson, Claes ,  Waters, Susanna ,  Waters, Nicholas ,  Tedroff, Joakim ,  Andersson, Bengt , 

IPC分类号： C07D295/096 ,  C07D295/08

CPC分类号： C07D295/073 ,  C07D211/18 ,  C07D211/20 ,  C07D211/22 ,  C07D211/24 ,  C07D211/32 ,  C07D211/34 ,  C07D211/70 ,  C07D295/096 ,  C07D295/112 ,  C07D295/155 ,  C07D405/06

摘要： New 3-substituted 4-(phenyl-N-alkyl)-piperazine and 4-(phenyl-N-alkyl)-piperidine compounds of Formula 1:
wherein X N, CH, or C, however X may only be C when the compound comprises a double bond at the dotted line; R 1 is OSO 2 CF 3 , OSO 2 CH 3 , SOR 3 , SO 2 R 3 , COR 3 , NO 2 , or CONHR 3 and when X is CH or C R 1 may also be CF 3 , CN, F, Cl, Br, or I; R 2 is a C 1 -C 4 alkyl, an allyl, CH 2 SCH 3 , CH 2 CH 2 OCH 3 , CH 2 CH 2 CH 2 F, CH 2 CF 3 , 3,3,3-trifluoropropyl, 4,4,4-trifluorobutyl, or -(CH 2 )-R 4 ; R 3 is a C 1 -C 3 alkyl, CF 3 , or N(R 2 ) 2 ; R 4 is a C 3 -C 6 cycloalkyl, 2-tetrahydrofurane or 3-tetra-hydrofurane, as well as pharmaceutically acceptable salts thereof are disclosed.
   Also pharmaceutical compositions comprising the above compounds and methods wherein the above compounds are used for treatment of disorders in the central nervous system are disclosed.

摘要翻译： 新的3-取代的4-（苯基-N-烷基） - 哌嗪和式1的4-（苯基-N-烷基） - 哌啶化合物：其中XN，CH或C，但当化合物包含 虚线双键; R 1是OSO 2 CF 3，OSO 2 CH 3，SOR 3，SO 2 R 3，COR 3，NO 2或CONHR 3，当X是CH或CR 1也可以是CF 3，CN，F，Cl， Br或I; R 2是C 1 -C 4烷基，烯丙基，CH 2 SCH 3，CH 2 CH 2 OCH 3，CH 2 CH 2 CH 2 F，CH 2 CF 3，3,3,3-三氟丙基，4,4 ，4-三氟丁基或 - （CH 2）-R 4; R 3是C 1 -C 3烷基，CF 3或N（R 2）2; R 4是C 3 -C 6环烷基，2-四氢呋喃或3-四氢呋喃，以及其药学上可接受的盐。 公开了包含上述化合物的药物组合物和其中上述化合物用于治疗中枢神经系统疾病的方法。

公开(公告)号：EP1032561B1

公开(公告)日：2004-02-11

申请号：EP98958458.6

申请日：1998-11-18

申请人： SCHERING CORPORATION

发明人： REICHARD, Gregory, A. ,  ALAIMO, Cheryl, A. ,  SHIH, Neng-Yang ,  TING, Pauline, C. ,  CARRUTHERS, Nicholas, I. ,  LAVEY, Brian, J.

IPC分类号： C07D211/76 ,  C07D211/52 ,  C07D401/12 ,  A61K31/445

CPC分类号： C07D401/12 ,  C07D211/24 ,  C07D211/34 ,  C07D211/52 ,  C07D211/58 ,  C07D211/64 ,  C07D211/76 ,  C07D401/14 ,  C07D417/14

公开(公告)号：EP1345899A1

公开(公告)日：2003-09-24

申请号：EP01272426.6

申请日：2001-12-20

申请人： AstraZeneca AB

发明人： SHENVI, Ashokkumar Bhikkappa

IPC分类号： C07D211/24 ,  C07C255/57 ,  C07D417/12 ,  C07D211/22 ,  C07D211/34 ,  C07D211/20 ,  A61K31/445 ,  A61K31/44 ,  A61P25/00 ,  A61P29/00

CPC分类号： C07D295/125 ,  C07C233/78 ,  C07C237/22 ,  C07C255/57 ,  C07D211/22 ,  C07D211/24 ,  C07D211/34 ,  C07D211/62 ,  C07D401/12 ,  C07D403/04

摘要： A compound having general formula (I), and methods of using such compounds for the treatment of diseases and pharmaceutical composition comprising such compounds.

公开(公告)号：EP1295873A1

公开(公告)日：2003-03-26

申请号：EP01934516.4

申请日：2001-06-04

申请人： TORAY INDUSTRIES, INC.

发明人： FUJINO, Toshihiro ,  SATO, Haruyo

IPC分类号： C07D211/24

CPC分类号： C07D211/24 ,  Y02P20/582

摘要： Disclosed are a method for producing racemic piperidine derivatives by processing optically-active piperidine derivatives in a hydrogen atmosphere in the presence of a reducing catalyst; and a method for producing optically-active piperidine derivatives or their acid salts by optically resolving the racemic piperidine derivatives obtained in the former method.

摘要翻译： 公开了在还原催化剂存在下，在氢气氛中加工光学活性哌啶衍生物来制备外消旋哌啶衍生物的方法; 以及通过光学拆分前述方法得到的外消旋哌啶衍生物来制造光学活性哌啶衍生物或其酸式盐的方法。

公开(公告)号：EP0938483B1

公开(公告)日：2003-02-26

申请号：EP97936296.9

申请日：1997-08-06

申请人： SCHERING CORPORATION

发明人： LOWE, Derek, B. ,  CHANG, Wei, K. ,  KOZLOWSKI, Joseph, A. ,  BERGER, Joel, G. ,  McQUADE, Robert ,  BARNETT, Allen ,  SHERLOCK, Margaret ,  TOM, Wing ,  DUGAR, Sundeep ,  CHEN, Lian-Yong ,  CLADER, John, W. ,  CHACKALAMANNIL, Samuel ,  WANG, Yuguang ,  McCOMBIE, Stuart, W. ,  TAGAT, Jayaram, R. ,  VICE, Susan, F. ,  VACCARO, Wayne, D. ,  GREEN, Michael, J. ,  BROWNE, Margaret, E. ,  BOYLE, Craig, D. ,  JOSIEN, Hubert, B. ,  ASBEROM, Theodros

IPC分类号： C07D405/00 ,  A61K31/00

CPC分类号： C07D405/14 ,  C07C2601/14 ,  C07D211/24 ,  C07D211/32 ,  C07D239/34 ,  C07D257/04 ,  C07D295/03 ,  C07D295/088 ,  C07D295/092 ,  C07D295/096 ,  C07D295/112 ,  C07D295/116 ,  C07D295/125 ,  C07D295/13 ,  C07D295/135 ,  C07D295/145 ,  C07D295/15 ,  C07D405/12 ,  C07D409/14

摘要： Di-N-substituted piperazine or 1,4 di-substituted piperidine compounds in accordance with formula I (including all isomers, salts, esters, and solvates) wherein R, R?1, R2, R3, R4, R21, R27, R28¿, X, Y and Z as defined herein are muscarinic antagonists useful for treating cognitive disorders such as Alzheimer's disease. Pharmaceutical compositions and methods of preparation are also disclosed. Also disclosed are synergistic combinations of compounds of the above formula with acetylcholinesterase inhibitors.

摘要翻译： 根据式I的二-N-取代哌嗪或1,4-二取代哌啶化合物（包括所有异构体，盐，酯和溶剂合物），其中R，R 1，R 2，R 3，R 4，R 21，R 27，R 28，X ，Y和Z如本文所定义的是可用于治疗认知障碍如阿尔茨海默氏病的毒蕈碱拮抗剂。 还公开了药物组合物和制备方法。 还公开了上式化合物与乙酰胆碱酯酶抑制剂的协同组合。

公开(公告)号：EP1119355B1

公开(公告)日：2003-01-08

申请号：EP99947737.5

申请日：1999-10-04

申请人： AstraZeneca AB

发明人： BERNSTEIN, Peter, Robert ,  DEDINAS, Robert, Frank ,  OHNMACHT, Cyrus, John ,  RUSSELL, Keith

IPC分类号： A61K31/445 ,  C07D211/28 ,  C07D401/10 ,  C07D211/66 ,  C07D401/14 ,  C07D211/58 ,  C07D417/04

CPC分类号： C07D401/04 ,  C07D211/18 ,  C07D211/24 ,  C07D211/26 ,  C07D211/28 ,  C07D211/34 ,  C07D211/58 ,  C07D211/66 ,  C07D211/76 ,  C07D401/10 ,  C07D417/04

公开(公告)号：EP1240142A1

公开(公告)日：2002-09-18

申请号：EP00989162.3

申请日：2000-12-22

申请人： A. Carlsson Research AB

发明人： ANDERSSON, Bengt ,  SONESSON, Clas ,  WATERS, Susanna ,  WATERS, Nicholas ,  TEDROFF, Joakim

IPC分类号： C07D211/18 ,  C07D295/096 ,  C07D295/155 ,  C07D295/073 ,  A61K31/496 ,  A61K31/451 ,  A61P25/00

CPC分类号： C07D295/073 ,  C07D211/18 ,  C07D211/20 ,  C07D211/22 ,  C07D211/24 ,  C07D211/32 ,  C07D211/34 ,  C07D211/70 ,  C07D295/096 ,  C07D295/112 ,  C07D295/155 ,  C07D405/06

摘要： New 3-substituted 4-(phenyl-N-alkyl)-piperazine and 4-(phenyl-N-alkyl)-piperidine compounds of Formula (1), wherein X N, CH, or C, however X may only be C when the compound comprises a double bond at the dotted line; R1 is OSO2CF3, OSO2CH3, SOR3, SO2R3, COR3, NO2, or CONHR3 and when X is CH or C R1 may also be CF3, CN, F, C1, Br, or I; R2 is a C1-C4 alkyl, an allyl, CH2SCH3, CH2CH2OCH3, CH2CH2CH2F, CH2CF3, 3,3,3-trifluoropropyl, 4,4,4- trifluorobutyl, or - (CH2) - R4; R3 is a C1-C3 alkyl, CF3, or N(R2)2; R4 is a C3-C6 cycloalkyl, 2-tetrahydrofurane or 3-tetra-hydrofurane, as well as pharmaceutically acceptable salts thereof are disclosed. Also pharmaceutical compositions comprising the above compounds and methods wherein the above compounds are used for treatment of disorders in the central nervous system are disclosed.

摘要翻译： 式（1）的新的3-取代的4-（苯基-N-烷基） - 哌嗪和4-（苯基-N-烷基） - 哌啶化合物，其中XN，CH或C，然而X可以仅为 化合物在虚线处包含双键; R1是OSO2CF3，OSO2CH3，SOR3，SO2R3，COR3，NO2或CONHR3，并且当X是CH或C时，R1也可以是CF3，CN，F，C1，Br或I; R2为C1-C4烷基，烯丙基，CH2SCH3，CH2CH2OCH3，CH2CH2CH2F，CH2CF3,3,3,3-三氟丙基，4,4,4-三氟丁基或 - （CH2）-R4; R3是C1-C3烷基，CF3或N（R2）2; R 4是C 3 -C 6环烷基，2-四氢呋喃或3-四氢呋喃及其药学上可接受的盐。 还公开了包含上述化合物和其中上述化合物用于治疗中枢神经系统病症的方法的药物组合物。