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91. 发明申请

WO2005040120A1 TETRAHYDROPYRIDINE DERIVATIVES 审中-公开
标题翻译：四氢吡啶衍生物
公开(公告)号：WO2005040120A1
公开(公告)日：2005-05-06
申请号：PCT/EP2004/011088
申请日：2004-10-05
申请人： ACTELION PHARMACEUTICALS LTD , BEZENCON, Olivier , SIFFERLEN, Thierry , BUR, Daniel , FISCHLI, Walter , WELLER, Thomas , REMEN, Lubos , RICHARD-BILDSTEIN, Sylvia
发明人： BEZENCON, Olivier , SIFFERLEN, Thierry , BUR, Daniel , FISCHLI, Walter , WELLER, Thomas , REMEN, Lubos , RICHARD-BILDSTEIN, Sylvia
IPC分类号： C07D211/78
CPC分类号： C07D211/78
摘要： The invention relates to novel tetrahydropyridine derivatives and use thereof as active ingredients in the preparation of pharmaceutical compositions. The invention also concerns related aspects including processes for the preparation of the compounds, pharmaceutical compositions containing one or more of those compounds and especially their use as inhibitors of renin. (I) wherein X and Y represent independently hydrogen, fluorine or a methyl group; X and Y do not represent both hydrogen at the same time or X and Y may together form a cyclopropyl ring; W represents a phenyl or a heteroaryl, the heteroaryl ring being a six-membered and non-fused ring, the phenyl ring and the heteroaryl are substituted with V in position 3 or 4; A and B independently represent -O-;-S-;-SO- or -SO 2 -; U represents aryl or heteroaryl; T represents -CONR 1 -;-(CH 2 ) p OCO-; -(CH 2 ) p N(R 1 )CO-; -(CH 2 ) p N(R 1 )SO 2 -; -COO-; -(CH 2 ) p OCONR 1 - or -(CH 2 ) p N(R 2 )CONR 1 -; R 1 and R 2 independently respresent hydrogen; lower alkyl; lower alkenyl; lower alkynil; cycloalkyl; aryl-lower alkyl, heteroaryl-lower alkyl or cycloalkyl - lower alkyl; Q represents lower alkylene or lower alkenylene; M represents hydrogen; cycloalkyl; aryl; heterocyclyl or heteroaryl:
摘要翻译：本发明涉及新型四氢吡啶衍生物及其在制备药物组合物中作为活性成分的用途。本发明还涉及包括制备化合物的方法，含有一种或多种这些化合物的药物组合物，特别是其作为肾素抑制剂的用途的相关方面。（I）其中X和Y独立地表示氢，氟或甲基; X和Y不同时表示氢，X和Y可以一起形成环丙基环; W表示苯基或杂芳基，杂芳基环为6元和非稠合环，苯环和杂芳基被V 3或4取代; A和B独立地表示-O - ; - S - ; - SO-或-SO 2 - ; U表示芳基或杂芳基; T表示-CONR 1 - ; - （CH 2）pOCO-; - （CH 2）p N（R <1>）CO-; - （CH 2）p N（R <1>）SO 2 - ; -COO-; - （CH 2）pOCONR 1 - 或 - （CH 2）p N（R 2）CONR 1 - ; R 1和R 2独立地表示氢; 低级烷基低级链烯基低级炔环烷基; 芳基 - 低级烷基，杂芳基 - 低级烷基或环烷基 - 低级烷基; Q表示低级亚烷基或低级亚烯基; M表示氢; 环烷基; 芳基; 杂环基或杂芳基：

92. 发明申请

WO02076940A3 PROCESS FOR PREPARING ARYLPIPERIDINE CARBINOL INTERMEDIATES AND DERIVATIVES 审中-公开
标题翻译：制备亚油酸二苯乙烯中间体和衍生物的方法
公开(公告)号：WO02076940A3
公开(公告)日：2003-05-22
申请号：PCT/US0208666
申请日：2002-03-21
申请人： PENTECH PHARMACEUTICALS INC
发明人： RONSEN BRUCE , UPADHYAYA SUBHASH P
IPC分类号： C07C253/30 , C07C255/41 , C07D211/78 , C07C69/76 , C07C229/00 , C07D211/22
CPC分类号： C07D211/78 , C07B2200/07 , C07C255/41
摘要： A process for the synthesis of arylpiperidine carbinol intermediates and derivatives is disclosed. A preferred process embodiment provides the synthesis of intermediate compounds of structural formula (I) and structural formula (II): Formula (I) Formula (II) where X is halo, C1-C10 alkoxy, C1-C10 haloalkyl, or hydroxy; R2 and R3 are each C1-C4 alkyl, and R2 and R3 are the same. The compound of structural formula (I) is made by condensing a corresponding cinnamonitrile with a corresponding diester malonate. The compound of structural formula (II) in the (±)-trans configuration is obtained by hydrogenating the compound of structural formula (I). The compounds of structural formula (I) and structural formula (II) are useful chemical intermediates for synthesizing 4-arylpiperidine-3-carbinols and their derivatives in (-)-trans configuration.
摘要翻译：公开了合成芳基哌啶甲醇中间体及其衍生物的方法。优选的方法实施方案提供了结构式（I）和结构式（II）的中间体化合物的合成：其中X为卤素，C 1 -C 10烷氧基，C 1 -C 10卤代烷基或羟基的式（I）式（II） R2和R3各自为C1-C4烷基，R2和R3相同。通过将相应的肉桂腈与相应的二酯丙二酸酯缩合来制备结构式（I）的化合物。通过使结构式（I）的化合物氢化，得到（±） - 反式构型中的结构式（II）的化合物。结构式（I）和结构式（II）的化合物是用于在（ - ） - 反式构型中合成4-芳基哌啶-3-甲醇及其衍生物的有用的化学中间体。

93. 发明申请

WO2002094787A1 2-OXO-PIPERIDINYL- AND 2-OXO-AZEPANYL ALKANOIC ACID DERIVATIVES FOR THE TREATMENT OF EPILEPSY AND OTHER NEUROLOGICAL DISORDERS 审中-公开
标题翻译：用于治疗癫痫发作和其他神经疾病的2-氧代哌嗪基和2-氧代氮杂环己烷酸衍生物
公开(公告)号：WO2002094787A1
公开(公告)日：2002-11-28
申请号：PCT/EP2002/005503
申请日：2002-05-17
申请人： UCB, S.A. , MICHEL, Philippe , KENDA, Benoît
发明人： MICHEL, Philippe , KENDA, Benoît
IPC分类号： C07D211/76
CPC分类号： C07D409/04 , C07D211/76 , C07D211/78 , C07D223/10
摘要： This invention relates to new 2-oxo-piperidinyl- and 2-oxo-azepanyl alkanoic acid derivatives of formula (1) having anticonvulsan t activity which are useful as therapeutic agents for the treatment or prevention of epilepsy and other neurological disorders. The invention also concerns processes for preparing these derivatives and novel intermediates used in the preparation of these derivatives.
摘要翻译：本发明涉及具有抗惊厥活性的式（1）的新的2-氧代 - 哌啶基和2-氧代 - 氮杂螺环烷酸衍生物，其可用作治疗或预防癫痫和其它神经障碍的治疗剂。本发明还涉及制备这些衍生物的方法和用于制备这些衍生物的新型中间体。

94. 发明申请

WO1996014844A1 CYCLIC AMIDINE ANALOGS AS INHIBITORS OF NITRIC OXIDE SYNTHASE 审中-公开
标题翻译：作为氮氧化物合成酶抑制剂的循环胺类似物
公开(公告)号：WO1996014844A1
公开(公告)日：1996-05-23
申请号：PCT/US1995014812
申请日：1995-11-13
申请人： MERCK & CO., INC. , GUTHIKONDA, Ravindra, N. , GRANT, Stephan, K. , MACCOSS, Malcolm , SHAH, Shrenik, K. , SHANKARAN, Kothandaraman , CALDWELL, Charles, G. , DURETTE, Philippe, L.
发明人： MERCK & CO., INC.
IPC分类号： A61K31/44
CPC分类号： C07D215/38 , C07D207/22 , C07D211/72 , C07D211/74 , C07D211/78 , C07D221/04 , C07D223/12 , C07D225/02 , C07D241/06 , C07D241/44 , C07D243/08 , C07D243/14 , C07D265/36 , C07D267/10 , C07D279/12 , C07D279/16 , C07D471/04 , C07D487/04 , C07D491/04
摘要： Disclosed herein are the heterocyclic compounds and pharmaceutically acceptable salts thereof which have been found to be useful in the treatment of nitric oxide synthase mediated diseases and disorders.
摘要翻译：本文公开了已被发现可用于治疗一氧化氮合酶介导的疾病和病症的杂环化合物及其药学上可接受的盐。

95. 发明申请

WO1995000484A1 N-SUBSTITUTED AZAHETEROCYCLIC CARBOXYLIC ACIDS AND ESTERS THEREOF 审中-公开
标题翻译： N-取代的唑烷基羧酸及其酯
公开(公告)号：WO1995000484A1
公开(公告)日：1995-01-05
申请号：PCT/DK1994000251
申请日：1994-06-22
申请人： NOVO NORDISK A/S
发明人： NOVO NORDISK A/S , ANDERSEN, Knud, Erik , LAU, Jesper , SORENSEN, Per, Olaf , PETERSEN, Hans , LUNDT, Friedrich, Behrend
IPC分类号： C07D211/60
CPC分类号： C07D211/78 , C07D211/60
摘要： The present invention relates to therapeutically active azaheterocyclic compounds of formula (I), a method of preparing the same and to pharmaceutical compositions comprising the compounds. The novel compounds are useful in treating a central nervous system ailment related to the GABA uptake. In formula (I) A is a saturated or unsaturated five or six-membered carbocyclic ring optionally substituted with a phenyl, benzylidene, C1-4-alkyl substituted with phenyl or C2-4-alkenyl substituted with phenyl which phenyl or benzylidene is optionally substituted with halogen, C1-4-alkyl, C1-4-alkoxy or trifluoromethyl and which saturated or unsaturated five or six-membered carbocyclic ring may be optionally fused with a benzo ring.
摘要翻译：本发明涉及式（I）的治疗活性氮杂环化合物，其制备方法和包含该化合物的药物组合物。新化合物可用于治疗与GABA摄取相关的中枢神经系统疾病。在式（I）中，A是饱和或不饱和的五或六元碳环，其任选被苯基，亚苄基，被苯基取代的C 1-4 - 烷基或被苯基取代的C 2-4 - 烯基取代，该苯基或亚苄基任选被取代与卤素，C 1-4 - 烷基，C 1-4 - 烷氧基或三氟甲基并且饱和或不饱和的五元或六元碳环可以任选地与苯并环稠合。

96. 发明申请

WO1992006959A1 1,2,5,6-TETRAHYDROPYRIDINE OXIME DERIVATIVES 审中-公开
标题翻译： 1,2,5,6-四氢吡啶氧化衍生物
公开(公告)号：WO1992006959A1
公开(公告)日：1992-04-30
申请号：PCT/GB1991001751
申请日：1991-10-09
申请人： BEECHAM GROUP PLC , BROMIDGE, Steven, Mark , ORLEK, Barry, Sidney , DABBS, Steven
发明人： BEECHAM GROUP PLC
IPC分类号： C07D211/70
CPC分类号： C07D213/89 , C07D211/70 , C07D211/78 , C07D211/94
摘要： Compounds of formula (I) or a pharmaceutically acceptable salt thereof wherein R1 represents a 1,2,5,6-tetrahydropyridin-3-yl group N-substituted by R10 wherein R10 represents OH; a group hydrolysable in vivo to OH or hydrogen; C1-8 alkoxy; C2-8 alkenyloxy; C2-8 alkynyloxy; C3-8 cycloalkyloxy; or COR13 wherein R13 represents hydrogen, C1-8 alkyl, phenyl or phenyl C1-4 alkyl; in which any phenyl moiety is optionally substituted by up to 3 substituents independently selected from C1-6 alkoxy, C1-6 alkyl, halo, C1-6 alkoxycarbonyl, cyano, C1-6 alkylthio or C1-6 alkylsulphonyl; enhance acetylcholine function via an action at muscarinic receptors within the central nervous system and are therefore of potential use in the treatment and/or prophylaxis of dementia in mammals.
摘要翻译：式（I）化合物或其药学上可接受的盐，其中R 1表示被R 10取代的1,2,5,6-四氢吡啶-3-基，其中R 10表示OH; 可在体内水解成OH或氢的基团; C 1-8烷氧基 C2-8烯氧基; C2-8炔氧基; C3-8环烷基氧基; 或COR 13，其中R 13表示氢，C 1-8烷基，苯基或苯基C 1-4烷基; 其中任何苯基部分任选被至多3个独立地选自C 1-6烷氧基，C 1-6烷基，卤素，C 1-6烷氧基羰基，氰基，C 1-6烷硫基或C 1-6烷基磺酰基的取代基取代; 通过中枢神经系统内毒蕈碱受体的作用增强乙酰胆碱的功能，因此在哺乳动物的治疗和/或预防痴呆中具有潜在的用途。

97. 发明申请

WO1992004323A1 1,2,5,6-TETRAHYDROPYRIDINE OXIME DERIVATIVES 审中-公开
标题翻译： 1,2,5,6-四氢吡啶氧化衍生物
公开(公告)号：WO1992004323A1
公开(公告)日：1992-03-19
申请号：PCT/GB1991001456
申请日：1991-08-29
申请人： BEECHAM GROUP PLC , BROMIDGE, Steven, Mark , ORLEK, Bary, Sidney , DABBS, Steven
发明人： BEECHAM GROUP PLC
IPC分类号： C07D211/70
CPC分类号： C07D211/70 , C07D211/78 , C07D213/57
摘要： Compounds of formula (I) or a pharmaceutically acceptable salt thereof, wherein R1 represents a 1,2,5,6-tetrahydropyridin-3-yl group N-substituted by R10 wherein R10 represents hydrogen, C1-2 alkyl, prop-2-enyl, prop-2-ynyl or cyclopropyl; R2 is a group OR4, where R4 is C1-4 alkyl, C2-4 alkenyl, C2-4 alkynyl, a group OCOR5 where R5 is hydrogen or R4, or a group NHR6, or NR7R8 where R6, R7 and R8 are independently C1-2 alkyl; and R3 is chloro, fluoro, bromo, methoxy, C1-3 alkyl substituted by one, two or three halogen atoms, or R3 is a group (CH2)nR9 where R9 is -CN, -SH or -SCH3 and n is 0 or 1, with the proviso that when n is 0, R9 is not -SH; enhance acetylcholine function via an action at muscarinic receptors within the central nervous system and are therefore of potential use in the treatment and/or prophylaxis of dementia in mammals.
摘要翻译：式（I）化合物或其药学上可接受的盐，其中R 1表示被R 10取代的1,2,5,6-四氢吡啶-3-基，其中R 10表示氢，C 1-2烷基，丙-2-醇，丙炔基，丙-2-炔基或环丙基; R2是OR4基团，其中R4是C1-4烷基，C2-4烯基，C2-4炔基，其中R5是氢或R4的基团OCOR5，或者NHR6或NR7R8，其中R6，R7和R8独立地是C1 -2烷基; 并且R 3是氯，氟，溴，甲氧基，被一个，两个或三个卤素原子取代的C 1-3烷基，或者R 3是基团（CH 2）n R 9，其中R 9是-CN，-SH或-SCH 3，n是0或 1，条件是当n为0时，R 9不是-SH; 通过中枢神经系统内毒蕈碱受体的作用增强乙酰胆碱的功能，因此在哺乳动物的治疗和/或预防痴呆中具有潜在的用途。

98. 发明授权

KR101879011B1 구아니딘 화합물 有权
公开(公告)号：KR101879011B1
公开(公告)日：2018-07-16
申请号：KR1020137022652
申请日：2012-03-13
申请人： 아스테라스 세이야쿠 가부시키가이샤
发明人： 요시하라고우세이 , 스즈키다이스케 , 야마키스스무 , 야마다히로요시 , 미하라히사시 , 세키노리오
IPC分类号： C07D413/04 , C07D401/04 , A61K31/5377 , A61P3/10 , A61P29/00
CPC分类号： C07D413/12 , A61K31/4412 , C07D205/04 , C07D211/60 , C07D211/78 , C07D213/38 , C07D213/64 , C07D213/74 , C07D217/06 , C07D217/22 , C07D237/20 , C07D239/26 , C07D239/34 , C07D239/42 , C07D239/48 , C07D241/20 , C07D267/10 , C07D277/42 , C07D277/46 , C07D277/56 , C07D295/06 , C07D295/08 , C07D295/18 , C07D295/192 , C07D295/20 , C07D309/08 , C07D309/14 , C07D401/04 , C07D401/12 , C07D401/14 , C07D403/04 , C07D403/06 , C07D403/12 , C07D405/12 , C07D405/14 , C07D413/04 , C07D413/14
摘要： 본발명은, 의약조성물, 특히, VAP-1 관련질환의예방및/또는치료용의약조성물의유효성분으로서유용한화합물을제공한다. 본발명자들은, VAP-1 저해활성을갖는화합물에대해서예의검토한결과, 본발명화합물또는그의염이, 우수한 VAP-1 저해활성을나타내어, VAP-1 관련질환, 특히당뇨병성신증혹은당뇨병성황반부종의예방및/또는치료에유용한것을발견하여, 본발명을완성하였다. 또한, 본발명은, 본발명화합물또는그의염, 및부형제를함유하는의약조성물, 특히, VAP-1 관련질환의예방및/또는치료용의약조성물에관한것이다.

99. 发明公开

KR1020160048946A 면역조절제로서 유용한 화합물 审中-实审
标题翻译：化合物作为免疫调节剂有用
公开(公告)号：KR1020160048946A
公开(公告)日：2016-05-04
申请号：KR1020167008405
申请日：2014-09-02
申请人： 브리스톨-마이어스 스큅 컴퍼니
发明人： 추팩,루이스에스. , 정,샤오판
IPC分类号： C07D211/32 , C07D211/34 , C07D211/44 , C07D211/48 , C07D211/56 , C07D217/02 , C07D205/08 , C07C217/58 , A61K31/435 , A61K31/47 , A61K31/397
CPC分类号： A61K31/381 , A61K31/396 , A61K31/397 , A61K31/40 , A61K31/44 , A61K31/4427 , A61K31/445 , A61K31/4523 , A61K31/496 , A61K31/5375 , A61K31/55 , A61K31/551 , C07C217/58 , C07C229/14 , C07C229/22 , C07C233/36 , C07C233/38 , C07C233/47 , C07C233/78 , C07C235/76 , C07C237/06 , C07C255/54 , C07C271/20 , C07C275/40 , C07C279/12 , C07C279/14 , C07C311/05 , C07C2601/02 , C07C2601/04 , C07C2601/08 , C07C2601/14 , C07C2602/08 , C07C2602/10 , C07D205/04 , C07D205/08 , C07D207/08 , C07D207/14 , C07D207/16 , C07D207/27 , C07D211/32 , C07D211/34 , C07D211/44 , C07D211/48 , C07D211/56 , C07D211/60 , C07D211/62 , C07D211/76 , C07D211/78 , C07D213/57 , C07D213/63 , C07D213/64 , C07D213/65 , C07D213/69 , C07D217/02 , C07D217/04 , C07D223/06 , C07D233/61 , C07D249/08 , C07D265/30 , C07D279/12 , C07D295/12 , C07D295/13 , C07D295/14 , C07D295/16 , C07D295/18 , C07D295/185 , C07D309/14 , C07D311/08 , C07D311/14 , C07D317/50 , C07D319/18 , C07D333/20 , C07D333/32 , C07D333/36 , C07D401/06 , C07D401/12 , C07D405/12 , C07D487/10 , C07K5/0806 , C07K5/0808 , A61K31/435 , A61K31/47
摘要： 하기화학식 I의화합물이개시되어있다. 면역조절제로서의이러한화합물및 이러한화합물을포함하는제약조성물을사용하는방법이또한개시되어있다. 이들화합물은바이러스질환또는장애및 암의진행을치료, 예방또는저속화시키는데유용하다.

100. 发明公开

KR1020160013149A 디히드로피리디논 MGAT2 억제제 审中-实审
标题翻译： DIHYDROPYRIDINONE MGAT2抑制剂
公开(公告)号：KR1020160013149A
公开(公告)日：2016-02-03
申请号：KR1020157036367
申请日：2014-05-28
申请人： 브리스톨-마이어스 스큅 컴퍼니
发明人： 아마드,살림 , 네가쉬,리뎃,에이.
IPC分类号： C07D211/78 , C07D211/86 , C07D211/90 , C07D417/04 , C07D401/04 , C07D409/04 , C07D409/14 , A61K31/4412 , A61K31/427
CPC分类号： C07D211/90 , A61K31/4412 , A61K31/4436 , A61K31/4439 , A61K31/444 , A61K45/06 , C07D211/78 , C07D211/86 , C07D401/04 , C07D409/04 , C07D409/14 , C07D417/04
摘要： 본발명은하기화학식 I의화합물, 또는그의입체이성질체또는제약상허용되는염을제공한다. 이들화합물은의약으로서사용될수 있는모노아실글리세롤아실트랜스퍼라제유형 2 (MGAT2) 억제제이다. 상기식에서, 가변기는모두본원에정의된바와같다.

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