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31. 发明公开

EP0981349A1 PREGNAN-3-OL-20-ONES 失效
标题翻译：孕-3- OL-20-ONES
公开(公告)号：EP0981349A1
公开(公告)日：2000-03-01
申请号：EP98918789.3
申请日：1998-04-28
申请人： AMERICAN HOME PRODUCTS CORPORATION
发明人： KAGAN, Michael, Z. , SHAH, Syed, Muzafar
IPC分类号： A61K31/57
CPC分类号： A61K31/57
摘要： This invention provides a method of providing progestational therapy to a mammal in need thereof which comprises administering a progestationally effective amount of a pharmaceutically acceptable salt of 5α-pregnan-3β-ol-20-one 3-sulfate ester to said mammal.
摘要翻译：本发明提供了一种为有需要的哺乳动物提供促孕疗法的方法，该方法包括给所述哺乳动物施用促孕有效量的5α-孕烷-3β-醇-20-酮3-硫酸酯的药学上可接受的盐。

32. 发明公开

EP0977994A1 METHOD FOR THE IDENTIFICATION AND CHARACTERIZATION OF NUCLEAR RECEPTOR LIGANDS 失效
标题翻译：方法鉴定和表征配体核受体
公开(公告)号：EP0977994A1
公开(公告)日：2000-02-09
申请号：EP98914486.0
申请日：1998-04-06
申请人： AMERICAN HOME PRODUCTS CORPORATION
发明人： CHESKIS, Borris, Y. , LYTTLE, C., Richard
IPC分类号： G01N33/74 , C12Q1/68
CPC分类号： G01N33/743
摘要： The present invention is directed to a methodology to study the effect of ligands that can modulate functions of nuclear receptors, and specifically, their interaction with specific DNA or other transcription factors. These receptors play a major role in the cascade of inter and intracellular physiological and biochemical events. They generally have a modular construction which enables them to recognize and bind to certain DNA sequences, or binding elements, such as hormone response elements. Various ligands, such as hormones, affect this interaction. In accordance with the methodology presented herein, measurements of such interactions are taken in real time and kinetic pattern. This allows the user to identify and to characterize ligands that are able to affect a receptor's interaction with its binding element. Hence, the present invention provides a useful tool for the elucidation, and development of ligands that affect transcription of target genes, either directly or indirectly.

33. 发明公开

EP0977846A1 NEURONAL MORT1 ISOFORMS 失效
标题翻译：神经MORT -1亚型
公开(公告)号：EP0977846A1
公开(公告)日：2000-02-09
申请号：EP98915540.3
申请日：1998-04-14
申请人： AMERICAN HOME PRODUCTS CORPORATION
发明人： BINGHAM, Brendan, William , YOUNG, Kathleen, H. , WOOD, Andrew, Timothy , BIRSAN, Camelia
IPC分类号： C12N15/12 , C07K14/47 , C07K14/715
CPC分类号： C07K14/715
摘要： A MORT1 gene initially cloned from HeLa cells and identified as a member of the receptor mediated apoptotic pathway, is expressed in the human neuronal cell line, NTERA2. Isolation of the MORT1 from this cell line revealed a transcript isoform that differed from the known MORT1 sequence by a deletion of 21 base pairs (bp 172-192 of the coding sequence). Cloning of MORT1 from adult human brain revealed two isoforms, one similarly deleted for bp 172-192, the other with a basepair substitution, A for G at position 173. Assessment of MORT1 function in a yeast two hybrid system indicates that the deleted and intact forms of MORT1 differ in their capacity to interact with other members of the apoptotic pathway.

34. 发明公开

EP0975753A2 $g(b)-AMYLOID PEPTIDE-BINDING PROTEINS AND POLYNUCLEOTIDES ENCODING THE SAME 失效
标题翻译： WHICHβ-淀粉样肽结合蛋白和多核苷酸，以确保CODE
公开(公告)号：EP0975753A2
公开(公告)日：2000-02-02
申请号：EP98918186.2
申请日：1998-04-14
申请人： AMERICAN HOME PRODUCTS CORPORATION
发明人： OZENBERGER, Bradley, Alton , KAJKOWSKI, Eileen, Marie , JACOBSEN, Jack, Steven , BARD, Jonathan, Adam , WALKER, Stephen, Glenn
IPC分类号： C12N15/12 , C07K14/47 , C12N15/62 , C12N15/11 , C12Q1/68 , C07K16/18 , G01N33/53 , A61K48/00 , A01K67/00
CPC分类号： C07K14/47 , A61K38/00 , C07K14/4711 , C07K2319/00
摘要： Novel proteins which bind human β-amyloid peptide, polynucleotides which encode these proteins, and methods for producing these proteins are provided. Diagnostic, therapeutic, and screening methods employing the polynucleotides and polypeptides of the present invention are also provided.

35. 发明公开

EP0955296A3 Tertiary alkyl functionalized piperazine derivatives 失效
标题翻译：哌嗪衍生物
公开(公告)号：EP0955296A3
公开(公告)日：2000-01-19
申请号：EP99108070.6
申请日：1990-04-20
申请人： AMERICAN HOME PRODUCTS CORPORATION , JOHN WYETH & BROTHER LIMITED
发明人： Cliffe, Ian Anthony , Abou-Gharbia, Magid Abdel-Megid , Yardley, John Patrick
IPC分类号： C07D295/12 , C07D295/08 , C07D239/42 , C07D295/14 , A61K31/495
CPC分类号： C07D295/145 , C07C2601/14 , C07D239/42 , C07D295/088 , C07D295/13 , C07D295/15
摘要： Compounds of the formula: in which R 1 is alkyl; R 2 and R 3 are alkyl or taken together they are polymethylene, R 2 and R 3 complete a 5-norbornen-2-yl moiety; X is -CO 2 -, -OCO-, -OCO 2 -, -N(R 7 )CO-, -NHNHCO-, -ON(R 7 )CO-, -CON(R 7 )-, -N(R 7 )CO 2 -, -OCON(R 7 )- or -N(R 7 )CON(R 8 )-, wherein R 7 and R 8 are, independently, hydrogen, alkyl, phenyl, benzyl, substituted phenyl or substituted benzyl in which the substituents are halo, alkyl, alkoxy, cyano, nitro or perhalomethyl; R 4 is hydrogen or alkyl; R 5 is hydrogen, alkyl, hydroxyalkyl, phenyl, benzyl, substituted phenyl or substituted benzyl in which the substituents are hydroxy, halo, alkyl, alkoxy, trifluoromethyl, nitro, cyano, carbalkoxy, carboxamido, amino, alkylamino or dialkylamino; R 6 is phenyl, benzyl, 2-, 3-, or 4-pyridinyl, 2-pyrimidinyl or 2-pyrazinyl, any of which may be substituted by one or more hydroxy, halo, alkyl, alkoxy, trifluoromethyl, nitro, cyano, carbalkoxy, carboxamido, amino, alkylamino or dialkylamino; n is one of the integers 1, 2, 3, 4 or 5; or a pharmaceutically acceptable salt thereof, with the proviso that when X is -CON(R 7 )- and R 7 is alkyl, R 6 is other than 2-pyrimidinyl, are antidepressant and/or anxiolytic agents.
摘要翻译：其中R 1是烷基的式的化合物; R 2和R 3是烷基或一起它们是聚亚甲基，R 2和R 3完成5-降冰片烯-2-基部分; X是-CO 2 - ， - OCO - ， - OCO 2 - ， - N（R 7）CO - ， - NHNHCO-，-ON（R 7）CO-，-CON（R 7） -N（R 7）CO 2 - ， - OCON（R 7） - 或-N（R 7）CON（R 8） - ，其中R 7和R 8是烷基，苯基，苄基，取代的苯基或取代的苄基，其中取代基是卤素，烷基，烷氧基，氰基，硝基或全卤代甲基; R 4是氢或烷基; R 5是氢，烷基，羟基烷基，苯基，苄基，取代的苯基或取代的苄基，其中取代基是羟基，卤素，烷基，烷氧基，三氟甲基，硝基，氰基，烷氧基，甲酰胺基，氨基，烷基氨基或二烷基氨基; R 6是苯基，苄基，2-，3-或4-吡啶基，2-嘧啶基或2-吡嗪基，其中任何一个可以被一个或多个羟基，卤素，烷基，烷氧基，三氟甲基，硝基，氰基，烷氧基，甲酰胺基，氨基，烷基氨基或二烷基氨基; n是整数1,2,3,4或5之一; 或其药学上可接受的盐，条件是当X是-CON（R 7） - 且R 7是烷基时，R 6不是2-嘧啶基，是抗抑郁剂和/或抗焦虑剂。

36. 发明公开

EP0968722A1 Improved modified live BRSV vaccine 失效
标题翻译：代理人，传讯员BRSV Lebend- Impfstoff
公开(公告)号：EP0968722A1
公开(公告)日：2000-01-05
申请号：EP99115633.2
申请日：1995-05-08
申请人： AMERICAN HOME PRODUCTS CORPORATION
发明人： Chu, Hsien-Jue
IPC分类号： A61K39/39 , A61K39/155
CPC分类号： A61K39/39 , A61K39/12 , A61K39/155 , A61K2039/5254 , A61K2039/55511 , A61K2039/55555 , A61K2039/55566 , A61K2039/6093 , A61K2039/70 , C12N2710/16734 , C12N2760/18534 , C12N2760/18634 , C12N2770/24334 , A61K2300/00
摘要： The invention provides an improved BRSV vaccine composition, which advantageously provides immunity from infection after a single administration. The composition comprises a modified live BRS virus and an adjuvant, which in combination provide immunity from BRSV infection after a single administration, and elicit an immune response specific to BRSV and including cell-mediated immunity and local (secretory IgA) immunity. In a preferred embodiment, the BRS virus is strain 375, and the adjuvant comprises an unsaturated turpin hydrocarbon, preferably squalene or squalane, and a polyoxypropylene-polyoxyethylene block copolymer, most preferably one where the copolymer has a polyoxypropylene (POP) component with an average molecular weight of about 3250 to 4000 and the polyoxyethylene (POE) component comprises about 10-20% of the total molecule. The adjuvant may optionally include a surfactant, preferably a polyoxyethylenesorbitan monooleate.
摘要翻译：本发明提供了一种改进的BRSV疫苗组合物，其有利地在单一给药后提供免疫感染。组合物包含修饰的活BRS病毒和佐剂，其在单次施用后联合提供免疫BRSV感染，并引发对BRSV特异性的免疫应答并且包括细胞介导的免疫和局部（分泌型IgA）免疫。在优选的实施方案中，BRS病毒是菌株375，并且佐剂包含不饱和的翻译烃，优选角鲨烯或角鲨烷，和聚氧丙烯 - 聚氧乙烯嵌段共聚物，最优选共聚物具有平均值的聚氧丙烯（POP）组分约3250至4000的分子量和聚氧乙烯（POE）组分占总分子的约10-20％。佐剂可任选地包括表面活性剂，优选聚氧乙烯脱水山梨糖醇单油酸酯。

37. 发明公开

EP0963372A1 5-AMINOALKOXY-1,4-DIHYDROQUINOXALINE-2,3-DIONES BEING DOPAMINE AGONISTS 失效
标题翻译： 5-氨基烷氧基-1,4-二氢喹喔啉-2,3-二氧化物多巴胺激素
公开(公告)号：EP0963372A1
公开(公告)日：1999-12-15
申请号：EP98903628.0
申请日：1998-01-13
申请人： AMERICAN HOME PRODUCTS CORPORATION
发明人： NELSON, James, Albert , SHAH, Uresh, Shantilal , MEWSHAW, Richard, Eric
IPC分类号： A61K31 , A61P25 , A61P43 , C07D241 , C07D401
CPC分类号： C07D401/12 , C07D241/44
摘要： This invention relates to compounds of Formula (I) wherein: R?1 and R2¿ are independently selected from hydrogen, straight-chain and branched alkyl group having up to 10 carbon atoms or -(CH¿2?)mAr where Ar is phenyl, naphthyl or thienyl, each optionally substituted by one or two substituents selected independently from C1-C6 alkyl, halogen, C1-C6 alkoxide and trifluoromethyl; or NR?1R2¿ is 1,2,3,4-tetrahydroquinolin-1-yl or 1,2,3,4-tetrahydroisoquinolin-2-yl; m is 1-5; n is 1 or 2; Y is halogen, C¿1?-C6 alkyl, and C1-C6 alkoxy; or the pharmaceutically acceptalbe salts thereof, which are dopamine D2 agonists and therefore useful in the treatment of psychoses and Parkinson's disease.

38. 发明公开

EP0955049A2 6 Beta-Hydroxy - 6 alpha, 17 alpha - dimethylpregn - 4 ene - 3,20 - dione, as an inhibitor of smooth muscle proliferation 失效
标题翻译： 6β-羟基-6α，17α-二甲基孕-4-ene-3,20-dion，als Hemmer der Proliferation von glatten Muskelzellen
公开(公告)号：EP0955049A2
公开(公告)日：1999-11-10
申请号：EP99200264.2
申请日：1995-04-28
申请人： AMERICAN HOME PRODUCTS CORPORATION
发明人： Winkley, Michael William , Mitchell, Robert Dempster
IPC分类号： A61K31/57
CPC分类号： C07J7/0045 , A61K31/57 , C07J53/002
摘要： A process for the production of medrogestone, in which, in an intermediate step, the solvate 3β,5α,6β-trihydroxy-6α,17α-dimethylpregnan-20-one monomethanolate is obtained as a solid, stable compound by displacing the organic solvent from a solution of of 3β,5α,6β-trihydroxy-6α,17α-dimethylpregnan-20-one with a lower alkanol, and a Diels-Alder adduct of 6-methylene-17α-methylpregn-4-ene-3,20-dione with maleic anhydride is used as an intermediate for production of the corresponding dicarboxylic acid salt for removal of 6-methylene-17α-methylpregn-4-ene-3,20-dione contamination of the desired product. Another intermediate, 6β-hydroxy-6α,17α-dimethylpregn-4-ene-3,20-dione, has been found to prevent smooth muscle proliferation and is useful in the treatment of atherosclerosis and restinosis.
摘要翻译：制备孕激素的方法，其中在中间步骤中，获得溶剂合物3β，5α，6β-三羟基-6α，17α-二甲基孕甾-20-酮单甲醇化物作为固体稳定化合物，通过从3β，5α，6β-三羟基-6α，17α-二甲基孕烷-20-酮与低级链烷醇的溶液中取代有机溶剂，并将6-亚甲基-17α- 甲基孕-4-烯-3,20-二酮与马来酸酐用作生产相应二羧酸盐的中间体，用于除去6-亚甲基-17α-甲基孕-4-烯-3,20-二酮污染物所需产品。已经发现另一种中间体6β-羟基-6α，17α-二甲基孕-4-烯-3,20-二酮可以预防平滑肌增生，并且可用于治疗动脉粥样硬化和再狭窄。

39. 发明公开

EP0954310A1 SYNERGISTIC COMPOSITION COMPRISING RAPAMYCIN AND CALCITRIOL 失效
标题翻译：协同组合物含雷帕霉素骨化三醇
公开(公告)号：EP0954310A1
公开(公告)日：1999-11-10
申请号：EP97911933.0
申请日：1997-10-28
申请人： AMERICAN HOME PRODUCTS CORPORATION
发明人： BOUILLON, Roger , BRANISTEANU, Dumitru , MATHIEU, Chantal
IPC分类号： A61K9 , A61K31 , A61K45 , A61P29 , A61P31 , A61P35 , A61P37
CPC分类号： A61K45/06 , A61K31/59 , A61K31/70
摘要： This invention provides a combination of rapamycin and 1,25-dihydroxy-cholecalciferol (1,25(OH)2D3) which is useful for inducing immunosuppression, and in the treatment of transplantation rejection, graft vs. host disease, autoimmune diseases, diseases of inflammation, adult T-cell leukemia/lymphoma, neoplasms, fungal infections, and hyperproliferative vascular disorders.

40. 发明公开

EP0948494A1 SUBSTITUTED BENZO 1,4]DIOXANES AS ANTIOBESITY AGENTS 失效
标题翻译：取代BENZO¬1,4二氧六环作为一种手段来FETLEIBIGKEIT
公开(公告)号：EP0948494A1
公开(公告)日：1999-10-13
申请号：EP97953494.0
申请日：1997-12-18
申请人： American Home Products Corporation
发明人： VENKATESAN, Aranapakam, Mudumbai
IPC分类号： A61K31 , A61P3 , C07D319 , C07D413
CPC分类号： C07D413/06 , C07D319/20
摘要： This invention relates to novel substituted 1,4-benzodioxane compounds having antidiabetic, antihyperglycemic, and antiobesity properties represented by formula (II) wherein R?1 and R6¿ are independently hydrogen, C¿1? to C6 alkyl, trifluoromethyl, cyano, C1 to C6 alkoxy, or halogen; R?2¿ is hydrogen or C¿1? to C6 trialkylsilyl; R?3¿ is hydrogen or C¿1? to C6 alkoxycarbonyl; or R?2 and R3¿ are joined to form the oxazolidinone ring (III); R?4 and R5¿ are independently hydrogen or C¿1? to C6 alkyl; R?7 and R8¿ are independently OR?9 or NR10R11; R9¿ is hydrogen, C¿1? to C12 alkyl, C1 to C12 cycloalkyl, C1 to C12 silylalkyl, phenyl, naphthyl, phenyl C?1 to C6¿ alkyl, C¿1? to C6 alkoxy C1 to C6 alkyl, pyridyl, thiophenyl, furanyl, imidazolyl, oxazolyl, -CHR?12COOR13, -CHR12C(O)R13, -CHR12CONR10R11, -CHR12OCOOR13¿, or -CHR?12OC(O)R13; R10 and R11¿ are independently hydrogen, C¿1? to C12 alkyl, phenyl, naphthyl, phenyl-C1 to C6 alkyl, furanylalkyl, or alkoxycarbonylalkyl; R?12 and R13¿ are independently hydrogen, C¿1? to C12 alkyl, phenyl, naphthyl, or phenyl-C1 to C6 alkyl; and the pharmaceutically acceptable salts thereof, a salt thereof; an enantiomer thereof, the racemic mixtures thereof, and the diastereomeric mixtures thereof.

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