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71. 发明申请

WO0067746A8 CARBOXYLIC ACID DERIVATIVES THAT INHIBIT THE BINDING OF INTEGRINS TO THEIR RECEPTORS 审中-公开
标题翻译：阻止整合素与其受体结合的羧酸衍生物
公开(公告)号：WO0067746A8
公开(公告)日：2002-02-28
申请号：PCT/US0012303
申请日：2000-05-05
申请人： TEXAS BIOTECHNOLOGY CORP , BIEDIGER RONALD J , CHEN QI , HOLLAND GEORGE W , KASSIR JAMAL M , LI WEN , MARKET ROBERT V , SCOTT IAN L , WU CHENGDE
发明人： BIEDIGER RONALD J , CHEN QI , HOLLAND GEORGE W , KASSIR JAMAL M , LI WEN , MARKET ROBERT V , SCOTT IAN L , WU CHENGDE
IPC分类号： C07D239/36 , A61K31/215 , A61K31/216 , A61K31/335 , A61K31/357 , A61K31/36 , A61K31/38 , A61K31/381 , A61K31/4015 , A61K31/4025 , A61K31/44 , A61K31/4409 , A61K31/4412 , A61K31/4427 , A61K31/445 , A61K31/4523 , A61K31/47 , A61K31/506 , A61K31/55 , A61P1/00 , A61P3/10 , A61P9/10 , A61P11/06 , A61P17/00 , A61P19/00 , A61P19/02 , A61P25/00 , A61P29/00 , A61P35/00 , A61P35/02 , A61P37/06 , A61P37/08 , A61P43/00 , C07C69/66 , C07C275/32 , C07C275/34 , C07D207/04 , C07D207/18 , C07D207/416 , C07D211/68 , C07D211/72 , C07D213/02 , C07D213/64 , C07D213/69 , C07D213/73 , C07D213/74 , C07D213/75 , C07D215/00 , C07D215/38 , C07D221/04 , C07D233/96 , C07D239/46 , C07D239/47 , C07D317/58 , C07D333/20 , C07D401/06 , C07D405/12 , C07D409/12 , C07D409/14 , C07D471/04 , C07D487/04
CPC分类号： C07D213/75 , C07D239/47 , C07D405/12 , C07D409/14
摘要： A method for the inhibition of the binding of alpha 4 beta 1 integrin to its receptors, for example VCAM-1 (vascular cell adhesion molecule-1) and fibronectin; compounds that inhibit this binding; pharmaceutically active compositions comprising such compounds; and to the use of such compounds either as above, or in formulations for the control or prevention of diseases states in which alpha 4 beta 1 is involved.
摘要翻译：抑制α4β1整联蛋白与其受体结合的方法，例如VCAM-1（血管细胞粘附分子-1）和纤连蛋白; 抑制这种结合的化合物; 包含这些化合物的药物活性组合物; 以及如上所述的这种化合物的使用，或用于控制或预防涉及α4β1的疾病状态的制剂中。

72. 发明申请

WO01032611A1 N-GUANIDINOALKYLAMIDES, THEIR PREPARATION, THEIR USE, AND PHARMACEUTICAL PREPARATIONS COMPRISING THEM 审中-公开
标题翻译： N-GUANIDINOALKYLAMIDES，他们的准备工作，他们的使用和药物制剂包括他们
公开(公告)号：WO01032611A1
公开(公告)日：2001-05-10
申请号：PCT/EP2000/010395
申请日：2000-10-21
IPC分类号： A61K31/155 , A61K31/16 , A61K31/166 , A61K31/167 , A61K31/197 , A61K31/198 , A61K31/223 , A61K31/4402 , A61K31/4406 , A61K31/4409 , A61K31/47 , A61K31/505 , A61P7/02 , A61P9/10 , A61P11/00 , A61P29/00 , A61P43/00 , C07C277/08 , C07C279/14 , C07D213/30 , C07D213/40 , C07D215/48 , C07D233/96 , C07D239/28
CPC分类号： C07D213/30 , C07C279/14 , C07D213/40 , C07D215/48 , C07D239/28
摘要： The present invention relates to compounds of formula (I), in which A, L, Y and k have the meanings indicated in the claims. The compounds of the formula (I) are valuable pharmacologically active compounds. They exhibit a strong antithrombotic effect and are suitable, for example, for the therapy and prophylaxis of cardiovascular disorders like thromboembolic diseases or restenoses. They are reversible inhibitors of the blood clotting enzymes factor Xa and/or factor VIIa and can in general be applied in conditions in which an undesired activity of factor Xa and/or factor VIIa is present or for the cure or prevention of which an inhibition of factor Xa and/or factor VIIa is intended. The invention furthermore relates to processes for the preparation of compounds of the formula (I), their use, in particular as active ingredients in pharmaceuticals, and pharmaceutical preparations comprising them.
摘要翻译：本发明涉及式（I）化合物，其中A，L，Y和k具有权利要求中所示的含义。式（I）的化合物是有价值的药理活性化合物。它们具有强烈的抗血栓形成作用，并且适用于例如治疗和预防心血管疾病如血栓栓塞性疾病或再狭窄。它们是血液凝固酶因子Xa和/或因子VIIa的可逆抑制剂，并且通常可以在其中存在因子Xa和/或因子VIIa的不期望的活性或用于治疗或预防其抑制因子Xa和/或因子VIIa是预期的。本发明还涉及式（I）化合物的制备方法，其用途，特别是药物中的活性成分，以及包含它们的药物制剂。

73. 发明申请

WO00071517A1 PHENOXYPROPYLAMINE COMPOUNDS 审中-公开
标题翻译：苯甲酰胺化合物
公开(公告)号：WO00071517A1
公开(公告)日：2000-11-30
申请号：PCT/JP2000/003279
申请日：2000-05-22
IPC分类号： A61P1/00 , A61P9/00 , A61P25/00 , A61P25/24 , A61P43/00 , C07D209/42 , C07D401/12 , C07D401/14 , C07D405/12 , C07D405/14 , C07D409/12 , C07D409/14 , C07D413/04 , C07D413/12 , C07D413/14 , C07D417/12 , C07D417/14 , C07D491/10 , C07D491/107 , A61K31/404 , A61K31/4166 , A61K31/421 , A61K31/438 , A61K31/4525 , A61K31/453 , A61K31/4535 , A61K31/454 , A61K31/496 , A61K31/5377 , C07D207/36 , C07D233/96 , C07D263/22 , C07D307/33 , C07D307/46 , C07D407/12
CPC分类号： C07D413/14 , C07D209/42 , C07D401/12 , C07D401/14 , C07D405/12 , C07D405/14 , C07D409/12 , C07D409/14 , C07D413/04 , C07D413/12 , C07D417/12 , C07D417/14 , C07D491/10
摘要： Phenoxypropylamine compounds represented by general formula (I), optically active isomers thereof or pharmaceutically acceptable salts thereof and hydrates of the same which have an affinity selectively for 5-HT1A receptor, simultaneously show an antagonistic activity, and inhibit the reuptake of 5-HT, thereby being usable as antidepressant agents quickly achieving an antidepressant effect wherein each symbol is as defined in the description.
摘要翻译：由通式（I）表示的苯氧基丙胺化合物，其光学活性异构体或其药学上可接受的盐及其对5-HT 1A受体具有亲和力选择性的水合物同时显示出拮抗活性，并抑制5-HT的再摄取，从而可用作抗抑郁剂快速达到抗抑郁作用，其中每个符号如说明书中所定义。

74. 发明申请

WO00035885A1 CYCLIC HYDRAZINE DERIVATIVES AS TNF-ALPHA INHIBITORS 审中-公开
标题翻译：循环盐酸衍生物作为TNF-ALPHA抑制剂
公开(公告)号：WO00035885A1
公开(公告)日：2000-06-22
申请号：PCT/EP1999/009423
申请日：1999-12-02
IPC分类号： A61K31/4166 , A61K31/4184 , A61K31/433 , A61K31/438 , A61K31/4439 , A61K31/496 , A61K31/513 , A61K31/517 , A61K31/519 , A61K31/53 , A61K31/549 , A61P7/00 , A61P7/04 , A61P9/00 , A61P9/10 , A61P11/00 , A61P19/02 , A61P29/00 , A61P31/04 , A61P35/00 , A61P37/00 , A61P43/00 , C07D233/34 , C07D233/38 , C07D233/80 , C07D233/84 , C07D233/86 , C07D233/96 , C07D235/02 , C07D239/22 , C07D239/54 , C07D239/96 , C07D241/08 , C07D249/12 , C07D251/34 , C07D253/06 , C07D285/10 , C07D285/18 , C07D401/06 , C07D471/04 , C07D471/10 , C07D487/04 , C07D495/04 , A61K31/395
CPC分类号： C07D235/02 , C07D233/34 , C07D233/80 , C07D233/84 , C07D233/96 , C07D239/54 , C07D239/96 , C07D241/08 , C07D249/12 , C07D251/34 , C07D285/10 , C07D285/18 , C07D401/06 , C07D471/10 , C07D487/04 , C07D495/04
摘要： Hydrazine derivatives of formula (I) wherein W represents O, S, CO, NR , (CR R )m, or CR ; X represents CO, NR , (CH2)n, CR or CHR ; Y represents CO, NR , (CH2)p, or CHR ; Z represents CO, CS, SO2, or CH2; m stands for 0 or 1; n and p each individually stand for 0, 1, or 2; R represents lower alkyl, lower alkenyl, lower cycloalkyl, lower cycloalkyl-lower alkyl, aryl or aryl-lower alkyl; R represents lower alkyl, lower alkenyl, lower cycloalkyl, lower cycloalkyl-lower alkyl or a group of the formula V-aryl, V-heterocyclyl or -(CH2)q-CH=CR R ; R , R , R , R and R each independently represent hydrogen, optionally substituted lower alkyl, lower alkenyl, lower cycloalkyl, lower cycloalkyl-lower alkyl, aryl, aryl-lower alkyl, heterocyclyl or heterocyclyl-lower alkyl; or R and R together with the carbon atom to which they are attached form a 3- to 8-membered ring; or R and R or R and R together with the nitrogen atoms to which they are attached form a 3- to 8-membered ring; or R and R together with the sp carbon atoms to which they are attached form a fused lower cycloalkenyl, aryl or heteroaryl ring; or R with either R or R together represent lower alkylene in which a CH2 group is optionally replaced by a heteroatom; or either R or R with either R or R together represent lower alkylene in which a CH2 group is optionally replaced by a heteroatom; or R and R together represent lower alkylene in which a CH2 group is optionally replaced by a heteroatom; V represents a spacer group; R and R together represent lower alkylene in which a CH2 group is optionally replaced by a heteroatom; and q stands for 1 or 2; with the provisos that (i) at least one of W, X and Y represents one of the heteroatoms previously indicated for these substituents or CO, (ii) Z represents CO or SO2 or CS when W represents O; (iii) W, X, Y and Z are not all CO and (iv) W, X and Y are not all NR , NR and NR , respectively; and pharmaceutically acceptable salts thereof inhibit the release of tumour necrosis factor alpha (TNF- alpha ) from cells. They can be used as medicaments, especially in the treatment of inflammatory and autoimmune diseases, osteoarthritis, respiratory diseases, tumours, cachexia, cardiovascular diseases, fever, haemorrhage and sepsis.
摘要翻译：式（I）的肼衍生物，其中W表示O，S，CO，NR 5，（CR 3 R 4）m或CR 11; X表示CO，NR 6，（CH 2）n，CR 12或CHR 13; Y表示CO，NR 7，（CH 2）p或CHR 14; Z表示CO，CS，SO2或CH2; m代表0或1; n和p各自分别代表0,1或2; R 1表示低级烷基，低级烯基，低级环烷基，低级环烷基 - 低级烷基，芳基或芳基 - 低级烷基; R 2表示低级烷基，低级烯基，低级环烷基，低级环烷基 - 低级烷基或式V-芳基，V-杂环基或 - （CH 2）q -CH = CR 8 R 9的基团。 R 3，R 4，R 5，R 6和R 7各自独立地表示氢，任选取代的低级烷基，低级烯基，低级环烷基，低级环烷基 - 低级烷基，芳基，芳基 - 低级烷基，杂环基或杂环基 - 低级烷基; 或R 3和R 4与它们所连接的碳原子一起形成3至8元环; 或R 5和R 6或R 5和R 7与它们所连接的氮原子一起形成3-至8-元环; 或R 11和R 12与它们所连接的sp 2碳原子一起形成稠合的低级环烯基，芳基或杂芳基环; 或R 5与R 13或R 14一起代表低级亚烷基，其中CH2基团任选被杂原子取代; 或R 6或R 7与R 3或R 4一起代表低级亚烷基，其中CH2基团任选被杂原子取代; 或R 3和R 4一起代表其中CH2基团任选被杂原子取代的低级亚烷基; V表示间隔基; R 8和R 9一起代表其中CH2基团任选被杂原子取代的低级亚烷基; q代表1或2; 条件是（i）W，X和Y中的至少一个表示先前对这些取代基或CO表示的杂原子之一，（ii）当W表示O时，Z表示CO或SO 2或CS; （iii）W，X，Y和Z不都是CO，（iv）W，X和Y不分别是NR 5，NR 6和NR 7; 和其药学上可接受的盐抑制肿瘤坏死因子α（TNF-α）从细胞的释放。它们可以用作药物，特别是用于治疗炎性和自身免疫疾病，骨关节炎，呼吸系统疾病，肿瘤，恶病质，心血管疾病，发热，出血和败血症。

75. 发明申请

WO00020384A1 DIPHENYL COMPOUNDS SUBSTITUTED BY CAMPHOR OR HYDANTOIN DERIVATIVES AS SUNSCREEN COMPOSITIONS 审中-公开
标题翻译：作为SUNSCREEN组合物取代或由羟胺衍生物取代的二苯醚化合物
公开(公告)号：WO00020384A1
公开(公告)日：2000-04-13
申请号：PCT/EP1999/006985
申请日：1999-09-21
IPC分类号： C07D233/96 , A61K8/00 , A61K8/35 , A61K8/42 , A61K8/46 , A61K8/49 , A61Q5/00 , A61Q17/04 , C07B61/00 , C07C45/66 , C07C45/74 , C07C49/683 , C07C303/22 , C07C309/23 , C07C309/24 , C07D235/00 , C07D235/02 , A61K7/42
CPC分类号： C07C309/24 , A61K8/35 , A61K8/466 , A61K8/4946 , A61Q17/04 , C07C45/74 , C07C49/683
摘要： A description is given of diphenyl compounds of formula (1) wherein R is a camphor or hydantoin derivative; and R1 is hydrogen; or C1-C5alkyl. These compounds are suitable as light stabilisers in cosmetic, pharmaceutical and veterinary formulations.
摘要翻译：描述了式（1）的二苯基化合物，其中R是樟脑或乙内酰脲衍生物; 并且R 1是氢; 或C 1 -C 5烷基。这些化合物适合作为化妆品，药物和兽药制剂中的光稳定剂。

76. 发明申请

WO9840374A3 OLEFIN POLYMERIZATION CATALYSTS CONTAINING GROUP 8-10 TRANSITION METALS, BIDENTALE LIGANTDS, PROCESSES EMPLOYING SUCH CATALYSTS AND POLYMERS OBTAINED THEREFROM 审中-公开
标题翻译：含烯烃聚合催化剂8-10过渡金属，BIDENTALE LIGANTDS，使用这种催化剂的方法和获得的聚合物
公开(公告)号：WO9840374A3
公开(公告)日：1998-12-10
申请号：PCT/US9803593
申请日：1998-02-24
申请人： EASTMAN CHEM CO
发明人： MACKENZIE PETER BORDEN , MOODY LESLIE SHANE , KILLIAN CHRISTOPHER MOORE , PONASIK JAMES ALLEN JR , MCDEVITT JASON PATRICK
IPC分类号： C07C251/36 , C07C257/14 , C07D233/96 , C07D241/06 , C07D265/30 , C07D285/10 , C07D319/12 , C07D339/08 , C07D513/04 , C07D521/00 , C07F9/50 , C07F15/00 , C07F15/02 , C07F15/04 , C07F15/06 , C08F4/70 , C08F4/80 , C08F10/00 , C08F110/02 , C08F210/16 , C07D319/02 , C07C2/24 , C07C247/14 , C07C257/06
CPC分类号： C07D241/06 , C07C251/36 , C07C257/14 , C07D231/12 , C07D233/56 , C07D233/96 , C07D249/08 , C07D265/30 , C07D285/10 , C07D319/12 , C07D339/08 , C07D513/04 , C07F9/5022 , C07F9/5031 , C07F15/006 , C07F15/0066 , C07F15/02 , C07F15/025 , C07F15/04 , C07F15/045 , C07F15/06 , C07F15/065 , C08F10/00 , C08F110/02 , C08F210/16 , C08F2500/10 , C08F2500/02 , C08F2500/03 , C08F2500/09 , C08F210/14 , C08F4/7006
摘要： Methods for preparing olefin polymers, or oligomers catalysts for preparing olefin polymers and bidentate ligand used for preparing these catalysts are disclosed. The polymers can be prepared containing the corresponding monomers with a Group 8-10 transition metal catalyst. The polymers are suitable for processing in conventional extrusion processes, and can be formed into high barrier sheets or films, or low molecular weight resins for use in synthetic waxes in wax coatings or as emulsions.

77. 发明申请

WO98040420A2 CATALYST COMPOSITIONS FOR THE POLYMERIZATION OF OLEFINS 审中-公开
标题翻译：用于烯烃聚合的催化组合物
公开(公告)号：WO98040420A2
公开(公告)日：1998-09-17
申请号：PCT/US1998/003592
申请日：1998-02-24
IPC分类号： C07D249/08 , B01J31/18 , C07C251/36 , C07C257/14 , C07D231/12 , C07D233/96 , C07D241/06 , C07D257/04 , C07D265/30 , C07D277/28 , C07D285/10 , C07D319/12 , C07D339/08 , C07D513/04 , C07D521/00 , C07F9/50 , C07F15/00 , C07F15/02 , C07F15/04 , C07F15/06 , C08F4/70 , C08F10/00 , C08F110/02 , B01J31/24
CPC分类号： C07D241/06 , C07C251/36 , C07C257/14 , C07D231/12 , C07D233/56 , C07D233/96 , C07D249/08 , C07D265/30 , C07D285/10 , C07D319/12 , C07D339/08 , C07D513/04 , C07F9/5022 , C07F9/5031 , C07F15/006 , C07F15/0066 , C07F15/02 , C07F15/025 , C07F15/04 , C07F15/045 , C07F15/06 , C07F15/065 , C08F10/00 , C08F110/02 , C08F2500/10 , C08F2500/02 , C08F4/7006 , C08F4/7013
摘要： The present invention includes novel ligands which may be utilized as part of a catalyst system. A catalyst system of the present invention is a transition metal-ligand complex. In particular, the catalyst system includes a transition metal component and a ligand component comprising a Nitrogen atom and/or functional groups comprising a Nitrogen atom, generally in the form of an imine functional group. In certain embodiments, the ligand component may further comprise a phosphorous atom. Preferred ligand components are bidentate (bind to the transition metal at two or more sites) and include a nitrogen-transition metal bond. The transition metal-ligand complex is generally cationic and associated with a weakly coordinating anion. A catalyst system of the present invention may further comprise a Lewis or Bronsted acid. The Lewis or Bronsted acid may be complexed with the ligand component of the transition metal-ligand complex.
摘要翻译：本发明包括可用作催化剂体系的一部分的新配体。本发明的催化剂体系是过渡金属 - 配体络合物。特别地，催化剂体系包括过渡金属组分和包含氮原子和/或包含通常为亚胺官能团形式的氮原子的官能团的配体组分。在某些实施方案中，配体组分可以进一步包含磷原子。优选的配体组分是双齿（在两个或多个位点处与过渡金属结合）并且包括氮 - 过渡金属键。过渡金属 - 配体络合物通常是阳离子的并且与弱配位阴离子相关联。本发明的催化剂体系还可以包含路易斯酸或布朗斯台德酸。路易斯或布朗斯台德酸可以与过渡金属 - 配体络合物的配体组分络合。

78. 发明申请

WO1998014433A1 ARALKYL AND ARALKYLIDENE HETEROCYCLIC LACTAMS AND IMIDES 审中-公开
标题翻译： ARALKYL和ARALKYLIDENE杂环纤维和咪唑
公开(公告)号：WO1998014433A1
公开(公告)日：1998-04-09
申请号：PCT/IB1997001062
申请日：1997-09-08
申请人： PFIZER INC. , HOWARD, Harry, Ralph
发明人： PFIZER INC.
IPC分类号： C07D233/96
CPC分类号： C07D277/20 , A61K31/135 , A61K31/496 , C07D233/70 , C07D233/96 , C07D241/08 , C07D265/32 , C07D267/10 , C07D273/06 , C07D277/34 , C07D279/12 , C07D281/06 , C07D417/04 , C07D417/10 , C07D417/12 , C07D471/04 , C07D487/04 , A61K2300/00
摘要： Compounds of the formula (I) wherein R is a group of formula G , G , G , G , G , G or G ; Y is an optionally substituted (C1-C4) heteroalkyl bridge that, together with the atoms to which it is attached, forms a five to seven membered heterocycle containing two to four heteroatoms, intermediates for their preparation, pharmaceutical compositions containing them and their medicinal use. These compounds are useful as psychotherapeutic agents.
摘要翻译：式（I）的化合物，其中R 1是式G 1，G 2，G 3，G 4，G 5，G 6或G 7的基团 >; Y是任选取代的（C 1 -C 4）杂烷基桥，其与其连接的原子一起形成含有2至4个杂原子的5至7元杂环，其制备中间体，含有它们的药物组合物及其药物用途。这些化合物可用作心理治疗剂。

79. 发明申请

WO1993013077A1 ANGIOTENSIN II RECEPTOR ANTAGONISTS 审中-公开
标题翻译： ANGIOTENSIN II受体拮抗剂
公开(公告)号：WO1993013077A1
公开(公告)日：1993-07-08
申请号：PCT/US1992010723
申请日：1992-12-09
申请人： WARNER-LAMBERT COMPANY
发明人： WARNER-LAMBERT COMPANY , HODGES, John, Cooke , KLUTCHKO, Sylvester
IPC分类号： C07D233/96
CPC分类号： C07D401/14 , C07D233/96 , C07D403/14 , C07D409/14 , C07D413/14 , C07D417/14 , C07F7/0812
摘要： Substituted 1-benzylimidazole-5-methylidene hydantoins are disclosed as well as methods of preparing them, pharmaceutical compositions containing them, and methods of using them. Intermediates useful in the preparation of the compounds of the invention are also disclosed and synthetic methods for preparing the novel intermediates. The compounds are useful as antagonists of angiotensin II and thus are useful in the control of hypertension, hyperaldosteronism, congestive heart failure, surgically induced vascular smooth muscle proliferation, and glaucoma.

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