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1. 发明申请

WO1997030050A1 HETEROCYCLYL-ERGOLINE DERIVATIVES AS 5-HT1A RECEPTOR LIGANDS 审中-公开
标题翻译：作为5-HT1A受体配体的间苯二酚衍生物
公开(公告)号：WO1997030050A1
公开(公告)日：1997-08-21
申请号：PCT/EP1997000582
申请日：1997-02-07
申请人： PHARMACIA & UPJOHN S.P.A. , MANTEGANI, Sergio , BANDIERA, Tiziano , MERONI, Maurizio , VARASI, Mario , CACCIA, Carla
发明人： PHARMACIA & UPJOHN S.P.A.
IPC分类号： C07D457/04
CPC分类号： C07D457/02 , C07D457/00
摘要： Ergoline derivative having formula (I) wherein R1 is hydrogen atom or C1-4 alkyl group; R2 is hydrogen, chlorine, or bromine atom, methyl or C1-4 alkylthio group; n is 0, 1 or 2; the substituent at position 8 is in alpha or beta configuration; Het represents an aromatic 5-membered heterocyclic ring, said ring having three heteroatoms which are the same or different and which are selected from the group consisting of sulfur, oxygen and nitrogen atom and X is hydrogen, chlorine or bromine or fluorine atom, or a pharmaceutically acceptable acid addition salt thereof are active at the Central Nervous System level. A process for their preparation is also described, as are pharmaceutical compositions containing them.
摘要翻译：式（I）的衍生物，其中R 1是氢原子或C 1-4烷基; R2是氢，氯或溴原子，甲基或C1-4烷硫基; n为0,1或2; 位置8处的取代基是α或β构型; Het表示芳族5元杂环，所述环具有三个相同或不同的杂原子，选自硫，氧和氮原子，X是氢，氯或溴或氟原子，或其药学上可接受的酸加成盐在中枢神经系统水平上是有活性的。还描述了其制备方法，以及含有它们的药物组合物。

2. 发明申请

WO1991011447A1 PROCESS FOR PREPARING ERGOLINE DERIVATIVES 审中-公开
标题翻译：制备葡萄糖衍生物的方法
公开(公告)号：WO1991011447A1
公开(公告)日：1991-08-08
申请号：PCT/EP1991000104
申请日：1991-01-21
申请人： FARMITALIA CARLO ERBA S.R.L. , MANTEGANI, Sergio , TRAQUANDI, Gabriella , BANDIERA, Tiziano , BRAMBILLA, Enzo
发明人： FARMITALIA CARLO ERBA S.R.L.
IPC分类号： C07D457/02
CPC分类号： C07D457/12 , C07D457/02
摘要： Ergoline derivatives of formula (I), wherein R represents hydrogen or C1-C4 alkyl; R1 represents hydrogen, chlorine, bromine or methyl; either R2 and R3 both represent hydrogen or together represent a chemical bond; R4 represents a C1-C4 hydrocarbon group; each of R5, R6, R8 and R9 independently represents hydrogen or C1-C4 alkyl; R7 represents hydrogen, C1-C4 alkyl, phenyl or C3-C7 cycloalkyl and n is 0, 1 or 2; are prepared by reaction between compounds of formulae (II) and (III), and subsequent cyclization of the resultant compounds. The compounds of formula (I) are known useful anxiolytic, antipsychotic and anti-parkinson agents.
摘要翻译：式（I）的咪唑啉衍生物，其中R表示氢或C1-C4烷基; R1代表氢，氯，溴或甲基; R2和R3均表示氢或一起代表化学键; R4代表C1-C4烃基; R5，R6，R8和R9各自独立地表示氢或C1-C4烷基; R 7表示氢，C 1 -C 4烷基，苯基或C 3 -C 7环烷基，n为0,1或2; 通过式（II）和（III）的化合物之间的反应制备，随后使所得化合物环化。式（I）化合物是已知的有用的抗焦虑药，抗精神病药和抗帕金森药。

3. 发明申请

WO2010060854A1 BICYCLIC PYRAZOLE AND ISOXAZOLE DERIVATIVES AS ANTITUMOR AND ANTINEURODEGENERATIVE AGENTS 审中-公开
标题翻译：双羟基吡唑和异佛唑酮衍生物作为抗肿瘤剂和抗原转移剂
公开(公告)号：WO2010060854A1
公开(公告)日：2010-06-03
申请号：PCT/EP2009/065480
申请日：2009-11-19
申请人： NERVIANO MEDICAL SCIENCES S.R.L. , MANTEGANI, Sergio , BRASCA, Maria Gabriella , CASUSCELLI, Francesco , FERGUSON, Ron , POSTERI, Helena , VISCO, Carlo , CASALE, Elena , ZUCCOTTO, Fabio
发明人： MANTEGANI, Sergio , BRASCA, Maria Gabriella , CASUSCELLI, Francesco , FERGUSON, Ron , POSTERI, Helena , VISCO, Carlo , CASALE, Elena , ZUCCOTTO, Fabio
IPC分类号： C07D471/04 , C07D487/04 , C07D498/04 , A61K31/437 , A61K31/4162 , A61P35/00
CPC分类号： C07D471/04 , C07D487/04 , C07D498/04
摘要： Bicyclic pyrazole and isoxazole derivatives of formula (I) and pharmaceutically acceptable salts thereof, as defined in the specification, process for their preparation and pharmaceutical compositions comprising them are disclosed; the compounds of the invention may be useful in therapy in the treatment of diseases mediated by HSP90 protein, like cancer and neurodegenerative disorders.
摘要翻译：公开了本说明书中定义的式（I）的双环吡唑和异恶唑衍生物及其药学上可接受的盐，其制备方法和包含它们的药物组合物; 本发明的化合物可用于治疗由HSP90蛋白介导的疾病，如癌症和神经变性疾病。

4. 发明申请

WO03006447A2 INTERACTION INHIBITORS OF TCF-4 WITH BETA-CATENIN 审中-公开
标题翻译： TCF-4与贝他肽的相互作用抑制剂
公开(公告)号：WO03006447A2
公开(公告)日：2003-01-23
申请号：PCT/EP0207536
申请日：2002-07-03
申请人： PHARMACIA ITALIA SPA , MOLL JUERGEN , KNAPP STEFAN , DALVIT CLAUDIO , TROSSET JEAN-YVES , SUNDSTROM MICHAEL , MANTEGANI SERGIO
发明人： MOLL JUERGEN , KNAPP STEFAN , DALVIT CLAUDIO , TROSSET JEAN-YVES , SUNDSTROM MICHAEL , MANTEGANI SERGIO
IPC分类号： G01N33/50 , A61K31/00 , A61K31/42 , A61K31/4245 , A61K31/428 , A61K31/444 , A61K31/496 , A61K31/5377 , A61K45/00 , A61P17/14 , A61P25/28 , A61P35/00 , A61P35/04 , A61P43/00 , C07D261/08 , C07D261/14 , C07D261/18 , C07D271/10 , C07D271/113 , C07D277/20 , C07D277/32 , C07D277/84 , C07D307/52 , C07D307/66 , C07D307/68 , C07D333/22 , C07D333/28 , C07D333/38 , C07D333/40 , C07D403/06 , C07D405/06 , C07D405/12 , C07D405/14 , C07D407/12 , C07D409/14 , C07D413/06 , C07D413/12 , C07D413/14 , C07D417/06 , C07D417/12 , C07D513/04 , G01N33/15 , A61K31/341 , A61K31/381 , A61K31/404 , A61K31/473 , A61K31/517 , G01N33/574
CPC分类号： C07D271/113 , A61K31/00 , C07D261/08 , C07D261/14 , C07D277/32 , C07D277/84 , C07D307/52 , C07D307/66 , C07D307/68 , C07D333/22 , C07D333/28 , C07D333/38 , C07D403/06 , C07D405/06 , C07D405/12 , C07D405/14 , C07D407/12 , C07D409/14 , C07D413/06 , C07D413/12 , C07D413/14 , C07D417/06 , C07D417/12 , C07D513/04
摘要： A compound of formula (I) is provided which is able to interact with beta -catenin/TCF-4 binding site, having a structure essentially equivalent to a pharmacophore (IA), as herein described.
摘要翻译：提供式（I）化合物，其能够与β-连环蛋白/ TCF-4结合位点相互作用，其具有基本上等同于如本文所述的药效团（IA）的结构。

5. 发明申请

WO2005005414A3 PYRAZOLYL-INDOLE DERIVATIVES ACTIVE AS KINASE INHIBITORS, PROCESS FOR THEIR PREPARATION AND PHARMACEUTICAL COMPOSITIONS COMPRISING THEM 审中-公开
标题翻译：作为激酶抑制剂活性的吡唑并吲哚衍生物，其制备方法和包含它们的药物组合物
公开(公告)号：WO2005005414A3
公开(公告)日：2005-04-21
申请号：PCT/EP2004007479
申请日：2004-07-08
申请人： PHARMACIA ITALIA SPA , GAVINA BERTA DANIELA , FORTE BARBARA , MANTEGANI SERGIO , VARASI MARIO , VIANELLO PAOLA
发明人： GAVINA BERTA DANIELA , FORTE BARBARA , MANTEGANI SERGIO , VARASI MARIO , VIANELLO PAOLA
IPC分类号： A61K31/416 , C07D401/14 , C07D403/04 , C07D403/14 , C07D405/14 , A61K31/4155
CPC分类号： C07D403/04 , A61K31/416 , C07D401/14 , C07D403/14 , C07D405/14
摘要： Pyrazolyl-indole derivatives of formula (I) as defined in the specification, and pharmaceutically acceptable salts thereof, process for their preparation and pharmaceutical compositions comprising them are disclosed; the compounds of the invention may be useful, in therapy, in the treatment of diseases associated with a disregulated protein kinase activity, like cancer.
摘要翻译：公开了说明书中定义的式（I）的吡唑基 - 吲哚衍生物及其药学上可接受的盐，其制备方法和包含它们的药物组合物; 本发明的化合物在治疗中可用于治疗与失调的蛋白激酶活性相关的疾病，如癌症。

6. 发明申请

WO1998000424A1 ANTINEURODEGENERATIVE ERGOLINE DERIVATIVES 审中-公开
标题翻译：过氧化物衍生物衍生物
公开(公告)号：WO1998000424A1
公开(公告)日：1998-01-08
申请号：PCT/EP1997002955
申请日：1997-05-29
申请人： PHARMACIA & UPJOHN S.P.A. , MANTEGANI, Sergio , BRAMBILLA, Enzo , CARFAGNA, Nicola , VARASI, Mario
发明人： PHARMACIA & UPJOHN S.P.A.
IPC分类号： C07D457/02
CPC分类号： C07D457/10 , A61K31/48 , C07D457/02
摘要： The present invention provides the new use in the treatment of neurodegenerative diseases with ergoline derivatives of formula (I) wherein R1 represents a hydrogen atom or a linear or branched C1-C5 alkyl or C2-C5 alkenyl group optionally substituted with a C3-C7 cycloalkyl, a hydroxy group or a R3-substituted phenyl group wherein R3 is a hydroxy or a hydroxymethyl group; R2 represents a hydrogen atom or a linear or branched C1-C5 alkyl or a C2-C5 alkenyl group optionally substituted with a hydroxy group, or a R3-substituted phenyl group wherein R3 is as above defined, or with a C1-C5 alkoxy group; the symbols -- at positions 2,3 and 8, 9 independently denote a single or double chemical bond and Z represents a group (CH2)nOH, wherein n is 0 or an integer from 1 to 3, or a group C(R4)2OH wherein R4 is a C1-C5 alkyl or a phenyl group, or a pharmaceutically acceptable salt thereof. Some compounds of formula (I) are novel. Processes for their preparation and pharmaceutical compositions containing them are also described.
摘要翻译：本发明提供了用于治疗神经变性疾病的新用途，其中式（I）的麦角灵衍生物，其中R 1表示氢原子或任选被C 3 -C 7环烷基取代的直链或支链C 1 -C 5烷基或C 2 -C 5烯基，羟基或R 3取代的苯基，其中R 3是羟基或羟甲基; R2表示氢原子或任选被羟基取代的直链或支链C 1 -C 5烷基或C 2 -C 5烯基，或其中R 3如上所定义的R 3取代苯基，或与C 1 -C 5烷氧基 ; 符号 - 位置2,3和8,9独立地表示单一或双重化学键，Z表示基团（CH 2）n OH，其中n为0或1至3的整数，或基团C（R 4）其中R 4是C 1 -C 5烷基或苯基，或其药学上可接受的盐。一些式（I）化合物是新的。还描述了其制备方法和含有它们的药物组合物。

7. 发明申请

WO1997013769A1 DISUBSTITUTED PIPERIDINE DERIVATIVES 审中-公开
标题翻译：分离的哌啶衍生物
公开(公告)号：WO1997013769A1
公开(公告)日：1997-04-17
申请号：PCT/EP1996004075
申请日：1996-09-16
申请人： PHARMACIA S.P.A. , MANTEGANI, Sergio , BANDIERA, Tiziano , VILLA, Manuela , VARASI, Mario , SPECIALE, Carmela
发明人： PHARMACIA S.P.A.
IPC分类号： C07D413/06
CPC分类号： C07D413/06
摘要： Disubstituted piperidine derivatives of formula (I), wherein R1 is hydrogen; bromo; chloro; a linear or branched C1-C5 alkyl group; a linear or branched C1-C5 alkoxy group; or an optionally substituted phenyl group; R2 is hydrogen, a linear or branched C1-C5 alkyl group or an optionally substituted phenyl group; X is CH2, C=O, CHOH or C=NOH; R3 is hydrogen or a linear or branched C1-C5 alkyl group; Y is a (CH2)n group in which n is an integer from 0 to 4, CHOH, C=O or CH-A wherein A is an optionally substituted phenyl group; A is an optionally substituted phenyl group; W is hydrogen or hydroxy; if the case, either as single isomers or as racemic mixtures, and their pharmaceutically acceptable salts, which possess selective neuroprotective activity, are useful in the treatment of an acute or a degenerative CNS disease. A process for preparing compounds of formula (I) and pharmaceutical compositions comprising them are also described.
摘要翻译：式（I）的二取代的哌啶衍生物，其中R 1是氢; 溴; 氯; 直链或支链C 1 -C 5烷基; 直链或支链C 1 -C 5烷氧基; 或任选取代的苯基; R2是氢，直链或支链C1-C5烷基或任意取代的苯基; X是CH 2，C = O，CHOH或C = NOH; R3是氢或直链或支链C1-C5烷基; Y为（CH 2）n基团，其中n为0至4的整数，CHOH，C = O或CH-A，其中A为任选取代的苯基; A是任选取代的苯基; W是氢或羟基; 如果具有选择性神经保护活性的情况，作为单一异构体或外消旋混合物及其药学上可接受的盐可用于治疗急性或退行性CNS疾病。还描述了制备式（I）化合物的方法和包含它们的药物组合物。

8. 发明申请

WO1995028403A1 ABEO-ERGOLINE DERIVATIVES AS 5HT1A LIGANDS 审中-公开
公开(公告)号：WO1995028403A1
公开(公告)日：1995-10-26
申请号：PCT/EP1995001398
申请日：1995-04-13
申请人： PHARMACIA S.P.A. , MANTEGANI, Sergio , BANDIERA, Tiziano , BRAMBILLA, Enzo , CACCIA, Carla , CARFAGNA, Nicola
发明人： PHARMACIA S.P.A.
IPC分类号： C07D487/06
CPC分类号： C07D487/06
摘要： There are provided compounds of formula (I), wherein R1 is a hydrogen, chlorine or bromine atom or a methyl, methylthio, hydroxy, cyano or carboxamido group; R2 is C1-C3 alkyl or an allyl group; R3 and R4 are independently a hydrogen atom, a C1-C5 alkyl group, a C3-C5 alkenyl group, a C5-C6 cycloalkyl C1-C3 alkyl group, a phenyl-C1-C3 alkyl, a phenyl -C3-C5 alkenyl or phenyl group: which groups are optionally substituted by C1-C3 alkyl, C1-C3 alkoxy, trifluoromethyl, hydroxy or amino group; or a group of formula (a), wherein R6 is hydrogen atom or a C1-C3 alkyl group and R7 is a phenyl group, a substituted phenyl group as described above or a heterocyclic ring, R5 is a hydrogen or bromine atom or an organic residue and R is H or an organic residue, or a pharmaceutically acceptable salt thereof. A process for their preparation and the pharmaceutical compositions comprising them are also provided.
摘要翻译：提供式（I）化合物，其中R 1是氢，氯或溴原子或甲基，甲硫基，羟基，氰基或甲酰氨基; R2是C1-C3烷基或烯丙基; R 3和R 4独立地是氢原子，C 1 -C 5烷基，C 3 -C 5烯基，C 5 -C 6环烷基C 1 -C 3烷基，苯基-C 1 -C 3烷基，苯基-C 3 -C 5链烯基或苯基：这些基团任选被C 1 -C 3烷基，C 1 -C 3烷氧基，三氟甲基，羟基或氨基取代; 或式（a）的基团，其中R6是氢原子或C1-C3烷基，R7是苯基，如上所述的取代苯基或杂环，R5是氢或溴原子或有机残基，R为H或有机残基，或其药学上可接受的盐。还提供了其制备方法和包含它们的药物组合物。

9. 发明申请

WO2004000811A1 ARYLSULFONYLHYDROXAMIC ACID AND AMIDE DERIVATIVES AND THEIR USE AS PROTEASE INHIBITORS 审中-公开
标题翻译： ARYLSULFONYLHYDROXAMICIC酸和酰胺衍生物及其作为蛋白酶抑制剂的用途
公开(公告)号：WO2004000811A1
公开(公告)日：2003-12-31
申请号：PCT/US2003/020028
申请日：2003-06-25
申请人： PHARMACIA CORPORATION , CHEN, Yiyuan , FRESKOS, John, N. , GASIECKI, Alan, F. , GRAPPERHAUS, Margaret, L. , HANSEN, Donald, W., Jr. , HEINTZ, Robert, M. , KHANNA, Ish, K. , KOLODZIEJ, Steve, A. , MANTEGANI, Sergio , MASSA, Mark, A. , MCDONALD, Joseph, J. , MISCHKE, Deborah, A. , NAGY, Mark, A. , PERRONE, Ettore , SCHMIDT, Michelle, A. , SPANGLER, Dale, P. , TALLEY, John, J. , TRIVEDI, Mahima , WYNN, Thomas, A. , BECKER, Daniel, P. , RICO, Joseph, G.
发明人： CHEN, Yiyuan , FRESKOS, John, N. , GASIECKI, Alan, F. , GRAPPERHAUS, Margaret, L. , HANSEN, Donald, W., Jr. , HEINTZ, Robert, M. , KHANNA, Ish, K. , KOLODZIEJ, Steve, A. , MANTEGANI, Sergio , MASSA, Mark, A. , MCDONALD, Joseph, J. , MISCHKE, Deborah, A. , NAGY, Mark, A. , PERRONE, Ettore , SCHMIDT, Michelle, A. , SPANGLER, Dale, P. , TALLEY, John, J. , TRIVEDI, Mahima , WYNN, Thomas, A. , BECKER, Daniel, P. , RICO, Joseph, G.
IPC分类号： C07D213/34
CPC分类号： C07D241/12 , C07C317/46 , C07D211/66 , C07D213/34 , C07D309/08 , C07D335/02 , C07D401/12 , C07D405/12 , C07D405/14 , C07D407/12 , C07D409/12 , C07D409/14 , C07D413/12 , C07D413/14 , C07D417/12
摘要： This invention is directed generally to hydroxamic acid and amide compounds (including salts of such compounds), and, more particularly, to aryl- and heteroaryl-arylsulfonylmethyl hydroxamic acids and amides that, inter alia , inhibit protease activity, particularly matrix metalloproteinase (also known as "matrix metalloprotease" or "MMP") activity and/or aggrecanase activity. These compounds generally correspond in structure to formula (I): wherein A l , A 2 , A 3 , E l , E 2 , E 3 , and E 4 are as defined in this patent. This invention also is directed to compositions of such compounds, intermediates for the syntheses of such compounds, methods for making such compounds, and methods for treating conditions associated with MMP activity and/or aggrecanase activity, particularly pathological conditions.
摘要翻译：本发明一般涉及异羟肟酸和酰胺化合物（包括这些化合物的盐），更具体地说，涉及芳基 - 和杂芳基 - 芳基磺酰基甲基异羟肟酸和酰胺，其特别是抑制蛋白酶活性，特别是基质金属蛋白酶作为“基质金属蛋白酶”或“MMP”）活性和/或蛋白聚糖蛋白聚糖酶活性。这些化合物通常在结构上对应于式（I）：其中A 1，A 2，A 3，E 11，E 2，E 3和E 4如在该专利中定义。本发明还涉及这些化合物的组合物，用于合成这些化合物的中间体，制备这些化合物的方法，以及用于治疗与MMP活性和/或蛋白聚糖蛋白聚糖酶活性特别是病理状况相关的病症的方法。

10. 发明申请

WO1987004168A1 AMINOGLYCOSIDE STEROIDS, A PROCESS FOR THEIR PREPARATION, THEIR USE AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM 审中-公开
标题翻译：氨基丁酸酯类STEROIDS，其制备方法，其使用和含有它们的药物组合物
公开(公告)号：WO1987004168A1
公开(公告)日：1987-07-16
申请号：PCT/EP1987000005
申请日：1987-01-07
申请人： FARMITALIA CARLO ERBA S.P.A. , CHIODINI, Laura , GOBBINI, Mauro , MANTEGANI, Sergio , RUGGIERI, Daniela , TEMPERILLI, Aldemio , TRAQUANDI, Gabriella , FERRARI, Patrizia
发明人： FARMITALIA CARLO ERBA S.P.A.
IPC分类号： C07J71/00
CPC分类号： C07J71/0057
摘要： Compounds of formula (I), [R1 = H or C1-C3 alkyl, R2 = an (alkyl-substituted) aminodeoxy or aminodideoxy or aminotrideoxy sugar residue of the D and L series, the glycosidic linkage being alpha or beta ] and their pharmaceutically acceptable salts are useful as antihypertensive agents. Their preparation and use as well as pharmaceutical compositions containing them are also described.
摘要翻译： D和L系列的式（I）化合物，[R1 = H或C1-C3烷基，R2 =（烷基取代）氨基脱氧或氨基二脱氧或氨基三脱氧糖残基，糖苷键为α或β] 可接受的盐可用作抗高血压药。还描述了它们的制备和用途以及含有它们的药物组合物。

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