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1. 发明公开

EP0266533A2 Precursors and synthesis of methyl-9-oxo-11 alpha, 16-di-hydroxy-16-vinyl-5-cis-13-transprostadienoates 失效
标题翻译： Vorläuferund Synthese von甲基-9-氧代-11-α，16-二羟基-16-乙烯基-5-顺式-13-转葡糖基二烯酸。
公开(公告)号：EP0266533A2
公开(公告)日：1988-05-11
申请号：EP87113814.5
申请日：1987-09-22
申请人： AMERICAN CYANAMID COMPANY
发明人： Wissner, Allan , Green, Kenneth E. , Hamann, Philp R. , Levin, Jeremy
IPC分类号： C07C43/32 , C07C177/00 , C07F1/08 , C07F7/22 , C07F7/18 , C07C41/60
CPC分类号： C07C43/32 , C07C41/60 , C07F7/18
摘要： This disclosure describes novel compounds which are useful as precursors in the synthesis of 9-oxo-11α, 16-dihydroxy-16-vinyl-5- cis -13- trans -prostadienoate esters which possess activity as hypotensive agents and/or as vasodilators.
摘要翻译：本公开描述了在合成作为降血压剂和/或作为血管扩张剂的活性的9-氧代-11α，16-二羟基-16-乙烯基-5-顺式-13-反 - 前列腺素酯的合成中可用作前体的新型化合物。

2. 发明公开

EP0458037A1 Bis-aryl amide and urea antagonists of platelet activating factor 无效转让
标题翻译：双芳酰胺和Harnstoffe mitPlättchenaktivierender Faktor（PAF）-antagonistischer Wirkung。
公开(公告)号：EP0458037A1
公开(公告)日：1991-11-27
申请号：EP91104964.1
申请日：1991-03-28
申请人： AMERICAN CYANAMID COMPANY
发明人： Wissner, Allan
IPC分类号： C07D277/22 , A61K31/425 , C07D277/28 , C07D213/20 , C07D233/61 , C07D471/04 , A61K31/44 , A61K31/41
CPC分类号： C07D213/20 , C07D231/12 , C07D233/56 , C07D249/08 , C07D277/22 , C07D277/28 , C07D471/04
摘要： Bis-aryl amide and urea compounds of the general formula:

wherein X is a divalent amide or urea substituent and Y is a nitrogen containing heterocycle, which compounds are inhibitors of platelet activating factor. Pharmaceutical compositions containing the compounds and methods of treating platelet activating factor associated conditions are also included.
摘要翻译：双芳基酰胺和通式为：CHEM的脲化合物，其中X是二价酰胺或脲取代基，Y是含氮杂环，该化合物是血小板活化因子的抑制剂。还包括含有该化合物的药物组合物和治疗血小板激活因子相关病症的方法。

3. 发明公开

EP0374513A2 Novel bis-arylphosphate ester antagonists of platelet activating factor 失效
标题翻译：双芳基磷酸酯 - 拮抗剂vom Thrombocyten aktivierenden Faktor。
公开(公告)号：EP0374513A2
公开(公告)日：1990-06-27
申请号：EP89121680.6
申请日：1989-11-23
申请人： AMERICAN CYANAMID COMPANY
发明人： Wissner, Allan , Green, Kenneth , Schaub, Robert Eugene
IPC分类号： C07F9/6539 , A61K31/675 , C07F9/58 , C07F9/60 , C07F9/62 , C07F9/6506 , C07F9/6509 , C07F9/6512
CPC分类号： C07F9/65061 , C07F9/581 , C07F9/60 , C07F9/62 , C07F9/650911 , C07F9/650958 , C07F9/65121 , C07F9/6539
摘要： The invention is novel compounds of the formula:
which are antagonists of platelet activating factor.
摘要翻译：本发明是下式的新型化合物：作为血小板活化因子的拮抗剂的。

4. 发明公开

EP0374510A1 Products for the treatment of endotoxic shock in a mammal 失效
标题翻译： Verfahren zur Behandlung des Endotoxin -Schocks bei einemSäugetier。
公开(公告)号：EP0374510A1
公开(公告)日：1990-06-27
申请号：EP89121661.6
申请日：1989-11-23
申请人： AMERICAN CYANAMID COMPANY
发明人： Wissner, Allan , Kerwar, Suresh S. , Kohler, Constance
IPC分类号： A61K39/395
CPC分类号： A61K39/395 , A61K31/395 , A61K31/38 , A61K31/675 , A61K31/66 , A61K2300/00
摘要： The invention is a method of treating endotoxic shock in a mammal which compnses administering to the mammal a therapeutically effective amount of an antagonist to Platelet Activating Factor in combination with a therapeutically effective amount of one or more monoclonal or polyclonal antibodies directed towards either Tumor Necrosis Factor a, Interieukin-1β, Gamma Interferon, or bacterial cell wall lipopolysaccharides.
摘要翻译：本发明是一种治疗哺乳动物的内毒素性休克的方法，其包括给予哺乳动物治疗有效量的血小板活化因子拮抗剂与治疗有效量的一种或多种针对肿瘤坏死因子的单克隆或多克隆抗体 α，Interieukin-1β，Gamma干扰素或细菌细胞壁脂多糖。

5. 发明公开

EP0787722A1 Substituted quinazoline derivatives 失效
标题翻译：取代中药
公开(公告)号：EP0787722A1
公开(公告)日：1997-08-06
申请号：EP97300703.2
申请日：1997-02-04
申请人： American Cyanamid Company
发明人： Wissner, Allan , Johnson, Bernard Dean , Floyd, Middleton Brawner, Jr. , Kitchen, Douglas Bruce
IPC分类号： C07D239/94 , A61K31/505
CPC分类号： C07D239/94
摘要： This invention provides a compound having the formula
wherein:

X is phenyl which is optionally substituted;
R and R 1 are each, independently, hydrogen, halogen, alkyl, alkoxy, hydroxy, or trifluoromethyl;
R 2 is hydrogen, alkyl, alkoxy, hydroxy, trifluoromethyl;
Y is a radical selected from the group consisting of

R 3 is independently hydrogen, alkyl, carboxy, carboalkoxy, phenyl, or carboalkyl; n = 2-4;
or a pharmaceutically acceptable salt thereof, with the proviso that each R 3 of Y may be the same or different which are useful as antineoplastic agents.
摘要翻译：本发明提供具有式CHEM的化合物，其中：X为任选取代的苯基; R和R 1各自独立地为氢，卤素，烷基，烷氧基，羟基或三氟甲基; R2是氢，烷基，烷氧基，羟基，三氟甲基; Y是选自下列基团的基团：CH 2 CH 3 R 3独立地是氢，烷基，羧基，烷氧羰基，苯基或烷基烷基; n = 2-4; 或其药学上可接受的盐，条件是Y的每个R 3可以相同或不同，其可用作抗肿瘤剂。

6. 发明授权

EP0374510B1 Products for the treatment of endotoxic shock in a mammal 失效
标题翻译：产品应用于治疗哺乳动物内毒素-Schocks的
公开(公告)号：EP0374510B1
公开(公告)日：1997-01-15
申请号：EP89121661.6
申请日：1989-11-23
申请人： AMERICAN CYANAMID COMPANY
发明人： Wissner, Allan , Kerwar, Suresh S. , Kohler, Constance
IPC分类号： A61K39/395
CPC分类号： A61K39/395 , A61K31/395 , A61K31/38 , A61K31/675 , A61K31/66 , A61K2300/00

7. 发明公开

EP0002590A1 Novel prostaglandin compounds, processes for the preparation thereof and pharmaceutical compositions containing them 失效
标题翻译：前列腺素，它们的制备方法和含有它们的药物组合物。
公开(公告)号：EP0002590A1
公开(公告)日：1979-06-27
申请号：EP78300772.7
申请日：1978-12-08
申请人： AMERICAN CYANAMID COMPANY
发明人： Wissner, Allan
IPC分类号： C07C177/00 , A61K31/557
CPC分类号： C07F7/2212 , C07B2200/07 , C07B2200/09 , C07C29/095 , C07C29/10 , C07C29/147 , C07C29/40 , C07C29/62 , C07C33/042 , C07C45/00 , C07C45/292 , C07C45/305 , C07C45/41 , C07C45/45 , C07C45/63 , C07C49/227 , C07C51/60 , C07C405/0025 , C07C2601/02 , C07C2601/04 , C07C2601/08 , C07C2601/14 , C07C2601/18 , C07C2601/20 , C07D309/12 , C07D317/12 , C07D317/16 , C07D317/20 , C07D317/34 , C07F7/0812 , C07F7/0818 , C07F7/1852 , C07F7/1856 , C07C47/11 , C07C49/753 , C07C47/277 , C07C49/16 , C07C49/293 , C07C49/743 , C07C49/707 , C07C59/82 , C07C31/135 , C07C31/1336 , C07C33/34 , C07C33/05 , C07C33/38 , C07C33/423 , C07C33/12 , C07C33/42 , C07C35/06 , C07C35/08 , C07C35/20 , C07C33/30 , C07C33/483
摘要： The invention provides novel prostaglandin compounds and processes for the preparation thereof which are prostaglandins of the E, F, or A series having on the terminal methylene carbon of the alpha chain a substituent selected from the group consisting of

wherein R is an alkyl group and R 15 is C 1 -C 4 alkyl, di-C 1 -C 4 - alkylamino and phenyl or phenyl substituted with one or more substituents selected from the group consisting of C 1 -C 4 alkyl, OR, SR, F or C1 wherein R is as previously defined. Processes for the preparation of these compounds are described as well as pharmaceutical compositions containing them. The compounds have a potential utility in medicine as for example: hypotensive agents, anti-ulcer agents and bronchodilators.
摘要翻译：本发明提供了用于制备它们的哪些是选自下组中的取代基的E，F，或具有在α链的末端亚甲基的碳的一系列前列腺素由......组成的worin R是烷基新颖前列腺素化合物和方法基和R15为C1-C4烷基，二C1-C4烷基氨基，并用选自C1-C4烷基，OR，SR中选择的一个或多个取代基的苯基或苯基substituiertem，F或C1 worin R是如上定义的，用于合成的化合物的制备方法描述以及含有它们的药物组合物。的化合物具有在医学上的电势作为实用程序，例如：降血压剂，抗溃疡剂和支气管扩张剂。

8. 发明公开

EP0336142A3 Novel antagonists of platelet activating factor 失效
标题翻译：电极激活因子的新的拮抗剂
公开(公告)号：EP0336142A3
公开(公告)日：1991-04-24
申请号：EP89104429.9
申请日：1989-03-13
申请人： AMERICAN CYANAMID COMPANY
发明人： Wissner, Allan , Schaub, Robert E. , Sum, Phaik-Eng
IPC分类号： C07F9/12 , C07C149/46 , C07F9/54 , C07F9/65 , A61K31/66 , A61K31/095 , C07D215/10 , C07D521/00 , C07D213/20 , C07D277/22 , C07F9/58 , C07F9/62
CPC分类号： C07D213/20 , C07C43/1745 , C07C43/1785 , C07C59/125 , C07C309/73 , C07D215/10 , C07D231/12 , C07D233/56 , C07D249/08 , C07D277/22 , C07F9/12 , C07F9/581 , C07F9/60 , C07F9/62 , C07F9/650911 , C07F9/650958 , C07F9/6539
摘要： The invention is a compound of R or S enantiomers or racemic mixtures of compounds of the formula:
wherein:
(A) X is
(i) C 1 -C 24 (ii) C 1 -C 24 alkoxy; (iii) C 1 -C 24 carboamoyloxy; or
wherein n is an integer from 1 to 25 and m is an integer from 0 to 24 and the sum of n and m is less than or equal to 25; (v) phenyl; (vi) mono- or polysubstituted phenyl substituted with C 1 -C 20 alkyl, C 1 -C 20 alkoxy, halogen, trifluoromethyl, phenyl, substituted phenyl or benzyloxy; (vii) phenoxy; (viii) mono- or polysubstituted phenoxy substituted with C 1 -C 20 alkyl, Ci-C 2 o alkoxy, halogen, trifluoromethyl, phenyl substituted phenyl or benzyloxy; (ix) naphthaloxy; (x) mono- or polysubstituted naphthaloxy substituted with C 1 -C 20 alkyl, C 1 -C 20 alkoxy or halogen; (xi) -O-(CH 2 ) r -O-((CH 2 ) p O) t -(CH 2 ) a -W wherein W is methyl or phenyl optionally substituted with C,-C 3 alkyl, C 1 -C 3 alkoxy or phenyl, r, p, t and a are integers such that the expression r + (p + 1)t + a is also an integer and has a value of 3 to 20; r is greater than or equal to 2; p is greater than or equal to 2; t is greater than or equal to zero; and a is greater than or equal to zero; (B) i is an integer from 1 to 3 and j is an integer from 1 to 6; (C) Q is -OR 2 ,
or O-C-R 2 , wherein R 2 is hydrogen, C 1 -C 6 alkyl or C 1 -C 6 alkenyl; (D) Y is a divalent radical
or (E) the moiety R 3 represents one or more C 1 -C 5 alkyl, C 1 -C 5 alkoxy or halogen substituents of the aromatic ring; (F) the moiety -CH 2 A may be in the ortho, meta or para position wherein A is
(i) a 5-7 member aromatic heterocyclic ring containing at least one nitrogen and one or more nitrogen or sulfur atoms: (ii)
or (iii)
which are PAF inhibitors.

9. 发明公开

EP0374513A3 Novel bis-arylphosphate ester antagonists of platelet activating factor 失效
标题翻译：新型双磷酸钠酯酶活性因子的拮抗剂
公开(公告)号：EP0374513A3
公开(公告)日：1991-04-03
申请号：EP89121680.6
申请日：1989-11-23
申请人： AMERICAN CYANAMID COMPANY
发明人： Wissner, Allan , Green, Kenneth , Schaub, Robert Eugene
IPC分类号： C07F9/6539 , A61K31/675 , C07F9/58 , C07F9/60 , C07F9/62 , C07F9/6506 , C07F9/6509 , C07F9/6512
CPC分类号： C07F9/65061 , C07F9/581 , C07F9/60 , C07F9/62 , C07F9/650911 , C07F9/650958 , C07F9/65121 , C07F9/6539
摘要： The invention is novel compounds of the formula:
which are antagonists of platelet activating factor.

10. 发明公开

EP0072872A1 1-Hydroxymethyl-prosten-1-ol derivatives 失效
标题翻译： 1-羟甲基prosten -1-醇 - 衍生物。
公开(公告)号：EP0072872A1
公开(公告)日：1983-03-02
申请号：EP81106499.7
申请日：1981-08-21
申请人： AMERICAN CYANAMID COMPANY
发明人： Wissner, Allan , Floyd, Middleton Brawner, Jr.
IPC分类号： C07C177/00 , A61K31/557
CPC分类号： C07D307/32 , C07C45/59 , C07C59/245 , C07C405/0025 , C07D307/54 , C07D317/12 , C07D317/24 , C07D317/34 , C07F7/1856 , C07F9/5407 , C07C49/743
摘要： There is provided novel 1-hydroxy-1-hydroxymethy) prostaglandins and method of use for vasodepression, smooth muscle stimulation and as antilipolytic agents. The novel compounds have the structure:
wherein n is the interger 3-5 inclusive; X is CH 2 CH 2 or CH CH (cis); R 1 is hydrogen or hydroxy, R' and R are the same or different and are hydrogen, C, to C. alkyl, C, to C 6 alkanoyl or optionally substituted benzoyl, wherein said substituents on said benzoyl moiety are selected from the group C, to C 4 alkoxy, halo and trifluoromethyl; and R 2 is selected from the group consisting of

wherein R 4 is hydrogen or methyl; R 5 is selected from the group consisting of C 4 -C 7 alkyl; R s is selected from the group consisting of C 3 -C 6 : R 11 is selected from the group consisting of C 3 -C 7 alkyl; the racemic mixtures thereof and the individual optically active enantiomers thereof; and the phar- maceutially acceptable non-toxic salts thereof.
摘要翻译：提供了新颖的1-羟基-1-羟甲基前列腺素和用于血管舒缓平滑肌刺激和抗溶血剂的方法。这些新化合物具有以下结构：其中n为整数3-5; X是CH 2 CH 2或CH-CH（顺式）; R1是氢或羟基，R和Rmin相同或不同并且是氢，C1至C4烷基，C1至C6烷酰基或任选取代的苯甲酰基，其中所述苯甲酰基部分上的所述取代基选自C1至C4烷氧基，卤素和三氟甲基; 并且R 2选自由以下组成的组：其中R 4为氢或甲基; R5选自C4-C7烷基; R9选自C3-C6; R 11选自C 3 -C 7烷基; 其外消旋混合物和其各自的光学活性对映异构体; 及其药学上可接受的无毒盐。

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