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1. 发明申请

WO2005113523A1 2-((HETERO) ARYL)-BENZOXAZOLE COMPOUNDS AND DERIVATIVES, COMPOSITIONS AND METHODS FOR STABILIZING TRANSTHYRETIN AND INHIBITING TRANSTHYRETIN MISFOLDING 审中-公开
标题翻译： 2 - （（异噻唑）芳基） - 苯并噻唑化合物和衍生物，用于稳定TRANSTHYRETIN和抑制TRANSTHYRETIN MISFOLDING的组合物和方法
公开(公告)号：WO2005113523A1
公开(公告)日：2005-12-01
申请号：PCT/US2005/017612
申请日：2005-05-20
申请人： FOLDRX PHARMACEUTICALS, INC. , LABAUDINIERE, Richard
发明人： LABAUDINIERE, Richard
IPC分类号： C07D263/56
CPC分类号： C07D307/91 , C07C39/367 , C07C65/24 , C07C229/42 , C07C229/58 , C07C229/60 , C07C251/48
摘要： Compounds, compositions and methods are provided for stabilizing transthyretin and for treating, preventing, or ameliorating one or more symptoms of transthyretin mediated diseases. In one embodiment, the compounds are benzoxazoles and related compounds, where Y is COOH, COOR 5 , CONR 7 R 8 , tetrazolyl, CONHOH, B(OH) 2 , CONHSO 2 Ar, CONHCH(R 6 )COOH, OH, CH 2 OH or -(CH 2 ) n -C(R 6 )(NH 2 )-COOH; X is O, S or NR 11 ; Het is heteroaryl, optionally substituted with halo, OR, alkyl or haloalkyl; and where R, R 1 -R 3 , R 5 -R 8 and R 11 are as described in the application.
摘要翻译：提供化合物，组合物和方法用于稳定转甲状腺素蛋白并用于治疗，预防或改善转甲状腺素蛋白介导的疾病的一种或多种症状。在一个实施方案中，化合物是苯并恶唑和相关化合物，其中Y是COOH，COOR 5，CONR 7 R 8，四唑基，CONHOH，B（OH）2，CONHSO 2 Ar，CONHCH（R 6） COOH，OH，CH 2 OH或 - （CH 2）n C（R 6）（NH 2）-COOH; X是O，S或NR 11; Het是杂芳基，任选被卤素，OR，烷基或卤代烷基取代; 并且其中R，R 1 -R 3，R 5 -R 8和R 11如申请中所述。

2. 发明申请

WO2005025556A3 ANTIBIOTIC CYCLOALKYLTETRAHYDROQUINOLINE DERIVATIVES 审中-公开
公开(公告)号：WO2005025556A3
公开(公告)日：2005-03-24
申请号：PCT/US2004/025937
申请日：2004-08-11
申请人： OSCIENT PHARMACEUTICALS , LABAUDINIERE, Richard, F. , XIANG, Yibin , JALLURI, Ravi, K. , ARVANITES, Anthony, C.
发明人： LABAUDINIERE, Richard, F. , XIANG, Yibin , JALLURI, Ravi, K. , ARVANITES, Anthony, C.
IPC分类号： C07D221/16 , C07D401/04 , A61K31/444 , A61P31/04
摘要： A method of treating a subject for a bacterial infection includes administering to a subject in need of treatment for a bacterial infection an effective amount of a compound represented by structural formula (I), or a pharmaceutically acceptable salt, solvate, or hydrate thereof. The variables in structural formula (I) are described herein.

3. 发明申请

WO1998016526A1 TETRAHYDRO-6H-PYRAZINO[1,2-B]ISOQUINOLINE 1,4-DIONES AS APOPROTEIN B-100 INHIBITORS 审中-公开
标题翻译：四氢呋喃-6H-吡咯并[1,2-B]异喹啉1,4-二酮作为APOPROTEIN B-100抑制剂
公开(公告)号：WO1998016526A1
公开(公告)日：1998-04-23
申请号：PCT/EP1997005636
申请日：1997-10-15
申请人： GLAXO GROUP LIMITED , LABAUDINIERE, Richard, Frederic , MARTRES, Paul , DODIC, Nerina , DUMAITRE, Bernard, Andre
发明人： GLAXO GROUP LIMITED
IPC分类号： C07D471/04
CPC分类号： C07D471/04
摘要： The prevent invention relates to compounds of formula (I) wherein R represents C3-8 cycloalkyl, optionally substituted by C1-4 alkyl; R represents hydrogen, halogen, NO2, CN, CHO, NHSO2R , NR R , NR COR , a 5-membered heteroaromatic ring optionally substituted by C1-4 alkyl, or a group X-Z; R represents hydrogen or a prop-2-enyl group; Y represents methylene or difluoromethylene; X represents a C1-6 alkylene, C2-6 alkenylene, C3-6 alkynylene or an N-linked imine group; Z represents hydrogen, C1-4alkoxy, CO2R , or an optionally substituted 5- or 6-membered heteroaromatic or phenyl group, where optional substitution is selected from a group consisting of CO2R , NR R , and NO2; Ar represents a phenyl or 5- or 6-membered heteroaromatic group optionally substituted by one or more groups selected from halogen, cyano, C1-4 alkyl, C1-4 alkoxy, CF3, S(O)nR , NHSO2R , NO2, NR R , NR COR , CO2R , CONR R , OCF3, and a 5-membered heterocyclic group optionally substituted by C1-4 alkyl; R represents C1-4 alkyl or trifluoromethyl; R and R independently represent hydrogen or C1-4 alkyl, or together R and R form a 3- to 6-membered cycloalkylamine ring; R and R independently represent hydrogen or C1-4 alkyl; R represents C1-4 alkyl or (CH2)mE, where m is 0 or 1 and E is a 5- or 6-membered heteroaromatic group; n is an integer from 0-3; and pharmaceutically acceptable derivatives thereof, to processes for their preparation; and their use in the treatment of conditions mediated by ApoB-100 regulation.
摘要翻译：本发明涉及式（I）化合物，其中R 0表示任选被C 1-4烷基取代的C 3-8环烷基; R 1表示氢，卤素，NO 2，CN，CHO，NHSO 2 R 3，NR 4 R 5，NR 6 COR 7，任选被C 1-4取代的5元杂芳环烷基或基团XZ; R 2表示氢或丙-2-烯基; Y表示亚甲基或二氟亚甲基; X表示C 1-6亚烷基，C 2-6亚烯基，C 3-6亚炔基或N-连接的亚胺基; Z表示氢，C 1-4烷氧基，CO 2 R 6或任选取代的5或6元杂芳族或苯基，其中任选的取代选自CO 2 R 6，NR 4 R 5 >和NO2; Ar表示任选被一个或多个选自卤素，氰基，C 1-4烷基，C 1-4烷氧基，CF 3，S（O）n R 5，NHSO 2 R 5的基团取代的苯基或5-或6-元杂芳基 >，NO 2，NR 4 R 5，NR 6 COR 8，CO 2 R 6，CONR 4 R 5，OCF 3和任选被C 1 -C 6取代的5元杂环基， 4烷基; R 3表示C 1-4烷基或三氟甲基; R 4和R 5独立地表示氢或C 1-4烷基，或者R 4和R 5一起形成3-至6-元环烷基胺环; R 6和R 8独立地表示氢或C 1-4烷基; R 7表示C 1-4烷基或（CH 2）mE，其中m为0或1，E为5或6元杂芳基; n是0-3的整数; 及其药学上可接受的衍生物，用于其制备方法; 及其用于治疗由ApoB-100调节介导的病症。

4. 发明申请

WO2005025556A2 ANTIBIOTIC CYCLOALKYLTETRAHYDROQUINOLINE DERIVATIVES 审中-公开
标题翻译：抗生素CYCLOALKYLTETRAHYDROQUINOLINE DERIVATIVES
公开(公告)号：WO2005025556A2
公开(公告)日：2005-03-24
申请号：PCT/US2004025937
申请日：2004-08-11
申请人： OSCIENT PHARMACEUTICALS , LABAUDINIERE RICHARD F , XIANG YIBIN , JALLURI RAVI K , ARVANITES ANTHONY C
发明人： LABAUDINIERE RICHARD F , XIANG YIBIN , JALLURI RAVI K , ARVANITES ANTHONY C
IPC分类号： A61K31/473 , C07D221/16 , C07D401/04 , A61K31/00
CPC分类号： C07D221/16 , A61K31/473 , C07D401/04
摘要： A method of treating a subject for a bacterial infection includes administering to a subject in need of treatment for a bacterial infection an effective amount of a compound represented by structural formula (I), or a pharmaceutically acceptable salt, solvate, or hydrate thereof. The variables in structural formula (I) are described herein.
摘要翻译：治疗受试者细菌感染的方法包括向需要治疗细菌感染的受试者施用有效量的由结构式（I）表示的化合物或其药学上可接受的盐，溶剂合物或水合物。本文描述了结构式（I）中的变量。

5. 发明申请

WO2003031376A1 SOLID PHASE SYNTHESIS OF SUBSTITUTED 1,5-BENZODIAZEPINE-2-ONE AND 1,5-BENZOTHIAZEPINE-2-ONE 审中-公开
标题翻译：取代的1,5-苯二酮-2-酮和1,5-苯并噻吩-2-酮的固相合成
公开(公告)号：WO2003031376A1
公开(公告)日：2003-04-17
申请号：PCT/US2002/032496
申请日：2002-10-10
申请人： AVENTIS PHARMACEUTICALS INC. , MORTON, George, C. , SALVINO, Joseph, M. , LABAUDINIERE, Richard, F. , HERPIN, Timothy, F.
发明人： MORTON, George, C. , SALVINO, Joseph, M. , LABAUDINIERE, Richard, F. , HERPIN, Timothy, F.
IPC分类号： C07B61/00
CPC分类号： C07D405/14 , C07B2200/11 , C07D243/12 , C07D281/10 , C07D417/12 , C07D417/14
摘要： A solid phase synthetic method for making substituted 1,5-benzodiazepine-2-one or 1,5-benzothiazepine-2-one. The method is useful for synthesis of large numbers of compounds through automated parallel synthesis or combinatorial library generation and is thus important to rapid discovery or new therapeutic agents containing the base structure of 1,5-benzodiazepine-2-one or 1,5-benzothiazepine-2-one.
摘要翻译：制备取代的1,5-苯并二氮杂-2-酮或1,5-苯并硫氮杂-酮的固相合成方法。该方法对于通过自动平行合成或组合文库产生来合成大量化合物是有用的，因此对于快速发现是重要的，或者含有1,5-苯并二氮杂-2-酮或1,5-苯并硫氮杂的基础结构的新治疗剂 -2-酮。

6. 发明申请

WO0013651A3 LUCIFERASE REPORTER BIOASSAY OF PARATHYROID HORMONE COMPOUNDS 审中-公开
标题翻译：杀虫剂报告器生物多样性的杀虫剂化合物
公开(公告)号：WO0013651A3
公开(公告)日：2000-09-08
申请号：PCT/US9919952
申请日：1999-08-31
申请人： AVENTIS PHARM PROD INC , LABAUDINIERE RICHARD F , MORSE CLARENCE C , YU KIN T , CRUMLEY GREGG R
发明人： LABAUDINIERE RICHARD F , MORSE CLARENCE C , YU KIN T , CRUMLEY GREGG R
IPC分类号： G01N33/50 , C12N5/10 , C12N15/09 , C12Q1/66 , C12Q1/68 , G01N33/15 , G01N33/566 , G01N33/68 , G01N33/74 , C12N5/06
CPC分类号： C12Q1/6897
摘要： This invention is directed to a bioassay for determining the functionality of parathyroid hormone compounds. More particularly, this invention is directed to a bioassay wherein the compound to be tested is added to a culture of parathyroid hormone receptor expressing cells bearing a reporter gene under the transcriptional control of multiple c-AMP responsive elements.
摘要翻译：本发明涉及用于测定甲状旁腺激素化合物的功能的生物测定法。更具体地，本发明涉及一种生物测定法，其中将待测化合物加入至多个c-AMP响应元件的转录控制下的带有报告基因的甲状旁腺激素受体表达细胞的培养物中。

7. 发明申请

WO2007126841A3 INHIBITION OF ALPHA-SYNUCLEIN TOXICITY 审中-公开
标题翻译：抑制ALPHA-SYNUCLEIN毒性
公开(公告)号：WO2007126841A3
公开(公告)日：2008-11-06
申请号：PCT/US2007007607
申请日：2007-03-29
申请人： FOLDRX PHARMACEUTICALS INC , WHITEHEAD BIOMEDICAL INST , LINDQUIST SUSAN L , OUTEIRO TIAGO , LABAUDINIERE RICHARD , FLEMING JAMES , BULAWA CHRISTINE ELLEN , WEIGEL CHARLOTTE , LIANG FENG , GUPTA SANDEEP , RIPKA AMY
发明人： LINDQUIST SUSAN L , OUTEIRO TIAGO , LABAUDINIERE RICHARD , FLEMING JAMES , BULAWA CHRISTINE ELLEN , WEIGEL CHARLOTTE , LIANG FENG , GUPTA SANDEEP , RIPKA AMY
IPC分类号： A61K31/33
CPC分类号： A61K31/4178 , A61K31/27 , A61K31/445 , A61K31/473 , A61K31/55 , A61K45/06 , A61K2300/00
摘要： Compounds and compositions are provided for treatment or amelioration of one or more symptoms of a-synuclein toxicity, a-synuclein mediated diseases or diseases in which a-synuclein fibrils are a symptom or cause of the disease.
摘要翻译：提供化合物和组合物用于治疗或改善一种或多种α-突触核蛋白毒性，α-突触核蛋白介导的疾病或其中α-突触核蛋白原纤维是疾病症状或原因的疾病症状。

8. 发明申请

WO9967192A3 PROCESS FOR THE SOLID PHASE SYNTHESIS OF ALDEHYDE, KETONE, OXIME, AMINE, HYDROXAMIC ACID AND alpha , beta -UNSATURATED CARBOXYLIC ACID AND ALDEHYDE COMPOUNDS 审中-公开
标题翻译：醛，酮，OXIME，胺，羟基酸和α，β-受体羧酸和醛类化合物的固相合成方法
公开(公告)号：WO9967192A3
公开(公告)日：2000-04-06
申请号：PCT/US9914251
申请日：1999-06-23
申请人： AVENTIS PHARM PROD INC , SALVINO JOSEPH M , MORTON GEORGE C , MASON HELEN J , LABAUDINIERE RICHARD F
发明人： SALVINO JOSEPH M , MORTON GEORGE C , MASON HELEN J , LABAUDINIERE RICHARD F
IPC分类号： C07C45/61 , C07C45/00 , C07C45/41 , C07C45/45 , C07C45/51 , C07C45/65 , C07C47/228 , C07C47/277 , C07C47/546 , C07C47/55 , C07C49/213 , C07C49/807 , C07C51/353 , C07C57/42 , C07C209/00 , C07C209/30 , C07C209/40 , C07C209/42 , C07C209/66 , C07C211/03 , C07C231/10 , C07C231/12 , C07C233/33 , C07C233/87 , C07C239/08 , C07C239/20 , C07C249/08 , C07C251/54 , C07C259/06 , C07C259/08 , C07C259/10 , C07C269/06 , C07C271/18 , C07C315/04 , C07C317/44 , C07C317/46 , C07D307/33 , C07D311/68 , C07D311/82 , C07D313/12 , C08F8/00 , C08F12/26 , C40B40/14 , C40B50/00 , G01N24/00 , C08G63/44
CPC分类号： C07D307/33 , C07B2200/11 , C07C45/00 , C07C45/004 , C07C45/41 , C07C45/45 , C07C45/516 , C07C51/09 , C07C209/00 , C07C209/40 , C07C209/42 , C07C209/66 , C07C239/08 , C07C259/06 , C07C259/08 , C07C259/10 , C07C315/04 , C07D311/68 , C07D311/82 , C07D313/12 , C08F8/00 , C08F8/30 , C08F2810/30 , C08J7/12 , G01N24/00 , C07C49/213 , C07C49/807 , C07C47/228 , C07C47/277 , C07C47/55 , C07C47/23 , C07C317/44 , C07C57/42 , C08F212/08 , C08F8/34 , C08F8/10 , C08F8/18 , C08F8/06 , C08F112/14 , C08F8/02
摘要： This invention is directed to a process for the solid phase synthesis of aldehyde, ketone, oxime, amine, hydroxamic acid and alpha , beta -unsaturated carboxylic acid and aldehyde compounds and to polymeric hydroxylamine resin compounds useful therefor.
摘要翻译：本发明涉及用于固相合成醛，酮，肟，胺，异羟肟酸和α，β-不饱和羧酸和醛化合物的方法以及用于其的聚合羟胺树脂化合物。

9. 发明申请

WO1998005327A1 SUBSTITUTED AROMATIC COMPOUNDS 审中-公开
标题翻译：取代的芳香化合物
公开(公告)号：WO1998005327A1
公开(公告)日：1998-02-12
申请号：PCT/US1997013343
申请日：1997-07-22
申请人： RHONE-POULENC RORER PHARMACEUTICALS INC. , HE, Wei , HULME, Christopher , HUANG, Fu-Chih , DJURIC, Stevan, W. , MORIARTY, Kevin , LABAUDINIERE, Richard
发明人： RHONE-POULENC RORER PHARMACEUTICALS INC.
IPC分类号： A61K31/44
CPC分类号： C07D207/08 , C07D207/26 , C07D213/30 , C07D213/89 , C07D401/06 , C07D401/08 , C07D401/12 , C07D401/14 , C07D403/04
摘要： This invention is directed to compound of formula (I) or hydrate thereof, solvate thereof, N-oxide thereof, prodrug thereof or a pharmaceutically acceptable salt thereof, which possess useful pharmaceutical properties. They are especially useful for inhibiting the production or physiological effects of TNF and inhibit cyclic AMP. The present invention is also directed to their pharmaceutical use, pharmaceutical compositions containing the compounds, and methods of their preparation.
摘要翻译：本发明涉及具有有用的药物性质的式（I）的化合物或其水合物，其溶剂合物，N-氧化物，其前药或其药学上可接受的盐。它们对于抑制TNF的产生或生理作用并抑制环AMP尤其有用。本发明还涉及其药物用途，含有该化合物的药物组合物及其制备方法。

10. 发明申请

WO1992019624A1 ANTISEROTONINES, PREPARTION THEREOF AND MEDICAMENTS CONTAINING THEM 审中-公开
标题翻译：抗生素，其制剂和含有它们的药物
公开(公告)号：WO1992019624A1
公开(公告)日：1992-11-12
申请号：PCT/FR1992000354
申请日：1992-04-21
申请人： RHONE-POULENC RORER S.A. , DAMOUR, Dominique , LABAUDINIERE, Richard , MALLERON, Jean-Luc , MIGNANI, Serge
发明人： RHONE-POULENC RORER S.A.
IPC分类号： C07F07/08
CPC分类号： C07D275/06 , C07D217/24 , C07D239/70 , C07F7/0816
摘要： Compounds having the formula R1-(CH2)n-Het wherein R1 is a residue having the formula (B), (C), (D); Het represents a radical phenyl-4 tetrahydro-1,2,3,6 pyridyl-1 whose phenyl cycle is optionally substituted by a halogen atom or an alkyl, alkoxy ou hydroxy radical; a radical phenyl-4 piperidino whose phenyl cyle is optionally substituted by a halogen atom or an alkyl, alkoxy or hydroxy radical; a radical phenyl-4 piperazinyl-1 whose phenyl cycle is optionally substituted by a halogen atom or an alkyl, alkoxy or hydroxy radical. R3 is a hydrogen atom or a phenyl radical; R4 is a hydrogen or halogen atom or a residue Het; R5 is a carbonyl or sulfonyl radical; R6 is a radical Si(CH3)2 or C(CH3)2; n equals 1, 2, 3 or 4; excepting {[(phenyl-4 tetrahydro-1,2,3,6 pyridyl-1)-2 ethyl] amino}-3 benzisothiazol-1,2 dioxyde-1,1; their salts, their preparation and medicaments containing them.

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