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31. 发明授权

US4939127A Antihypertensive phosphate derivatives 失效
标题翻译：抗高血压磷酸盐衍生物
公开(公告)号：US4939127A
公开(公告)日：1990-07-03
申请号：US96910
申请日：1987-09-15
申请人： Allan Wissner
发明人： Allan Wissner
IPC分类号： C07F9/10
CPC分类号： C07F9/10
摘要： Antihypertensive phosphate derivatives having the following formula are described: ##STR1## wherein W is selected from the group consisting of methyl and phenyl optionally substituted with C.sub.1 -C.sub.3 alkyl, C.sub.1 -C.sub.3 alkoxy and phenyl; r, n, m and a are integers such that the expression r+(n+1)m+a is also an integer and has a value of 3 to 20; r is greater than or equal to 2; n is greater than or equal to 2; m is greater than or equal to zero and a is greater than or equal to zero; T is selected from the group consisting of hydrogen and ##STR2## wherein R.sub.1 is selected from the group consisting of hydrogen, C.sub.1 -C.sub.4 branched or straight chain alkyl, C.sub.1 -C.sub.4 branched or straight chain alkoxy and C.sub.1 -C.sub.4 branched or straight chain alkylamino; Q is a bivalent radical selected from --(CH.sub.2).sub.p -- and --(CHR).sub.p --, wherein p is an integer 2-12 and the moiety --(CHR.sub.p -- represents an alkylene chain which is substituted by one or more C.sub.1 -C.sub.10 alkyl groups or phenyl groups; Z is selected from the group consisting of .+-.N(R.sub.2).sub.3 ##STR3## wherein R.sub.2 may be the same or different and is selected fromthe group consisting of hydrogen and C.sub.1 -C.sub.4 branched or straight chain alkyl and q is an integer from 4-7; in either the racemic or optically active forms.
摘要翻译：描述了具有下式的抗高血压磷酸酯衍生物：其中W选自甲基和任选被C 1 -C 3烷基，C 1 -C 3烷氧基和苯基取代的苯基; r，n，m和a是整数，使得表达式r +（n + 1）m + a也是整数，并且具有3至20的值; r大于或等于2; n大于或等于2; m大于或等于零，a大于或等于零; T选自氢和其中R 1选自氢，C 1 -C 4支链或直链烷基，C 1 -C 4支链或直链烷氧基和C 1 -C 4支链或直链烷基氨基 ; Q是选自 - （CH 2）p - 和（CHR）p - 的二价基团，其中p是整数2-12，部分 - （CHRp-表示被一个或多个C 1 -C 10取代的亚烷基链烷基或苯基; Z选自+/- N（R 2）3，其中R 2可以相同或不同，并且选自氢和C 1 -C 4支链或直链烷基 q为4-7的整数;以外消旋或旋光形式存在。

32. 发明授权

US4897385A Antihypertensive phosphate derivatives 失效
标题翻译：抗高血压磷酸盐衍生物
公开(公告)号：US4897385A
公开(公告)日：1990-01-30
申请号：US96945
申请日：1987-09-15
申请人： Allan Wissner , Phaik-Eng Sum
发明人： Allan Wissner , Phaik-Eng Sum
IPC分类号： C07F9/10
CPC分类号： C07F9/10
摘要： Antihypertensive phosphate derivatives having the following formula are described: ##STR1## wherein X is selected from the group consisting of a phenyl radical substituted at any position with a C.sub.1 -C.sub.20 branched or straight chain alkoxy or benzyloxy and optionally substituted at any other positions with one or more groups consisting of C.sub.1 -C.sub.15 branched or straight chain alkyl, C.sub.1 -C.sub.15 branched or straight chain alkoxy and halogen, and a naphthalene radical substituted at any position with a C.sub.1 -C.sub.20 branched or straight chain alkoxy or benzyloxy and optionally substituted at any other positions with one or more groups consisting of C.sub.1 -C.sub.15 branched or straight chain alkyl, C.sub.1 -C.sub.15 branched or straight chain alkoxy and halogen; T is selected from the group consisting of hydrogen and ##STR2## wherein R.sub.1 is selected from the group consisting of hydrogen, C.sub.1 C.sub.4 branched or straight chain alkyl, C.sub.1 -C.sub.4 branched or straight chain alkoxy and C.sub.1 -C.sub.4 branched or straight chain alkylamino; Y is selected from the group of bivalent radicals consisting of --(CH.sub.2).sub.p -- and --(CHR).sub.p --, wherein p is an integer from 2 to 10 and the moiety --(CHR).sub.p -- represents an alkylene chain substituted with one or more C.sub.1 -C.sub.8 alkyl groups or phenyl groups; Z is selected from the group consisting of ##STR3## wherein q is an integer from 4-7 and R.sub.2 may be the same or different and is selected from the group consisting of hydrogen and C.sub.1 -C.sub.4 branched or straight chain alkyl.
摘要翻译：描述了具有下式的抗高血压磷酸酯衍生物：其中X选自在任何位置被C 1 -C 20支链或直链烷氧基或苄氧基取代的苯基，并且任选在任何其它位置被取代的苯基与一个或多个由C 1 -C 15支链或直链烷基，C 1 -C 15支链或直链烷氧基和卤素组成的基团和在任何位置被C 1 -C 20支链或直链烷氧基或苄氧基取代的萘基和任选取代的在一个或多个由C 1 -C 15支链或直链烷基，C 1 -C 15支链或直链烷氧基和卤素组成的基团的任何其它位置; 其中R 1选自氢，C 1 -C 4支链或直链烷基，C 1 -C 4支链或直链烷氧基和C 1 -C 4支链或直链烷基氨基; Y选自由 - （CH 2）p - 和（CHR）p - 组成的二价基团，其中p是2至10的整数， - （CHR）p - 部分代表被一个或更多的C 1 -C 8烷基或苯基; Z选自其中q是4-7的整数，R2可以相同或不同，并且选自氢和C 1 -C 4支链或直链烷基。

33. 发明授权

US4827011A Antihypertensive phosphate derivatives 失效
标题翻译：抗高血压磷酸盐衍生物
公开(公告)号：US4827011A
公开(公告)日：1989-05-02
申请号：US679790
申请日：1984-12-10
申请人： Allan Wissner , Robert E. Schaub
发明人： Allan Wissner , Robert E. Schaub
IPC分类号： C07F9/10 , A61K31/685
CPC分类号： C07F9/10
摘要： Antihypertensive phosphate derivatives having the following formula are described: ##STR1## wherein X is a C.sub.1 -C.sub.24 branched or straight chain alkyl group; R is selected from the group consisting of hydrogen and C.sub.1 -C.sub.4 alkyl, with the proviso that at least one R group is not hydrogen; T is selected from the group consisting of hydrogen and ##STR2## wherein R.sub.1 is selected from the group consisting of hydrogen, C.sub.1 -C.sub.4 branched or straight chain alkyl, C.sub.1 -C.sub.4 branched or straight chain alkoxy and C.sub.1 -C.sub.4 branched or straight chain alkylamino; Q is a bivalent radical selected from the group consisting of --(CH.sub.2).sub.p -- and --(CHR.sup.1).sub.p --, wherein p is an integer from 2 to 12 and the moiety --(CHR.sup.1).sub.p -- represents an alkylene chain which is substituted by one or more C.sub.1 -C.sub.10 alkyl groups or phenyl groups; Z is selected from the group consisting of ##STR3## wherein R.sub.2 may be chain alkyl and q is an integer from 4 to 7; in either the racemic or in the optically active form.
摘要翻译：描述了具有下式的抗高血压磷酸酯衍生物：其中X是C 1 -C 24支链或直链烷基; R选自氢和C 1 -C 4烷基，条件是至少一个R基团不是氢; T选自氢和其中R 1选自氢，C 1 -C 4支链或直链烷基，C 1 -C 4支链或直链烷氧基和C 1 -C 4支链或直链烷基氨基 ; Q是选自 - （CH 2）p - 和（CHR 1）p - 的二价基团，其中p是2至12的整数，并且 - （CHR 1）p - 部分代表被取代的亚烷基链通过一个或多个C 1 -C 10烷基或苯基; Z选自，其中R 2可以是链烷基，q是4至7的整数; 以外消旋或旋光形式。

34. 发明授权

US5569762A Asymmetric synthesis of intermediates for retroviral protease inhibitor compounds 失效
标题翻译：逆转录病毒蛋白酶抑制剂化合物中间体的不对称合成
公开(公告)号：US5569762A
公开(公告)日：1996-10-29
申请号：US408362
申请日：1995-03-22
申请人： Allan Wissner , Michael P. Trova
发明人： Allan Wissner , Michael P. Trova
IPC分类号： C07D217/26 , C07D401/12 , C07D405/06 , C07D217/00
CPC分类号： C07D401/12 , C07D217/26 , C07D405/06
摘要： The disclosure describes an improved process for producing optically active compounds of Formula II or III, which compounds are useful as intermediates for preparing compounds active as inhibitors of retroviral protease enzymes: ##STR1## wherein R.sub.1, R.sub.50 and Z are described in the specification. The improved process includes either synthesis of diastereomeric iodolactones which are separated prior to conversion to compounds of Formula II or III or synthesis of an epoxide which is converted directly to compounds of Formula II and III.
摘要翻译：本公开描述了用于制备式II或III的光学活性化合物的改进方法，该化合物可用作制备作为逆转录病毒蛋白酶抑制剂有活性的化合物的中间体：其中R 1，R 50和Z 在说明书中描述。改进的方法包括合成在转化为式II或III化合物之前分离的非对映体碘内酯或合成直接转化为式II和III化合物的环氧化物。

35. 发明授权

US5432189A Bis-aryl amide and urea antagonists of platelet activating factor 失效
标题翻译：双芳基酰胺和尿素拮抗剂的血小板激活因子
公开(公告)号：US5432189A
公开(公告)日：1995-07-11
申请号：US247954
申请日：1994-05-24
申请人： Allan Wissner
发明人： Allan Wissner
IPC分类号： A61K31/415 , A61K31/425 , A61K31/426 , A61K31/44 , A61K31/4418 , A61K31/4425 , A61K31/47 , A61K31/472 , A61P7/02 , A61P9/00 , A61P9/02 , A61P11/00 , A61P11/08 , C07D213/20 , C07D213/38 , C07D213/40 , C07D215/10 , C07D217/04 , C07D217/12 , C07D233/61 , C07D277/22 , C07D277/28 , C07D471/04 , C07D521/00
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: ##STR1## 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：双芳基酰胺和通式如下的脲化合物：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活化因子相关病症的方法。

36. 发明授权

US5328901A Bis-arylphosphate ester antagonists of platelet activating factor 失效
标题翻译：血小板激活因子的双芳基磷酸酯拮抗剂
公开(公告)号：US5328901A
公开(公告)日：1994-07-12
申请号：US69638
申请日：1993-06-01
申请人： Allan Wissner , Kenneth Green , Robert E. Schaub
发明人： Allan Wissner , Kenneth Green , Robert E. Schaub
IPC分类号： A61K31/675 , A61P7/02 , A61P9/02 , A61P43/00 , C07F9/58 , C07F9/60 , C07F9/62 , C07F9/6506 , C07F9/6509 , C07F9/6512 , C07F9/6539 , C07F9/6558
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: ##STR1## which are antagonists of platelet activating factor.
摘要翻译：本发明是新颖的下式化合物：作为血小板活化因子的拮抗剂的“IMAGE”。

37. 发明授权

US5144045A Phosphocholine derivative inhibitors of phospholipase A.sub.2 失效
标题翻译：磷脂酶A2的磷酸胆碱衍生物抑制剂
公开(公告)号：US5144045A
公开(公告)日：1992-09-01
申请号：US612745
申请日：1990-11-13
申请人： Allan Wissner , Robert E. Schaub , Kenneth E. Green , Philip R. Hamann
发明人： Allan Wissner , Robert E. Schaub , Kenneth E. Green , Philip R. Hamann
IPC分类号： C07F9/10 , C07F9/568 , C07F9/655
CPC分类号： C07F9/568 , C07F9/10 , C07F9/65502
摘要： Phospocholine derivatives having the formula: ##STR1## in which W, Z, Q and R are described in the specification are disclosed as useful for inhibiting the enzyme phospholipase A.sub.2. Methods of making and using the compounds are also disclosed.
摘要翻译：公开了在说明书中描述的其中W，Z，Q和R所示的具有下式的其中的磷脂酰胆碱衍生物：其用于抑制磷脂酶A2。还公开了制备和使用化合物的方法。

38. 发明授权

US4310700A 1-Hydroxylmethyl-11-deoxy-16-hydroxy-prosten-1-ol-derivatives 失效
标题翻译： 1-羟甲基-11-脱氧-16-羟基 - 前列腺-1-醇衍生物
公开(公告)号：US4310700A
公开(公告)日：1982-01-12
申请号：US137085
申请日：1980-04-03
申请人： Allan Wissner , Middleton B. Floyd, Jr.
发明人： Allan Wissner , Middleton B. Floyd, Jr.
IPC分类号： C07C45/59 , C07C59/245 , C07C405/00 , C07D307/42 , C07D307/46 , C07D317/16 , C07D317/24 , C07D317/34 , C07F7/18 , C07C49/597 , C07C35/06
CPC分类号： C07D307/42 , C07C405/0025 , C07C45/59 , C07C59/245 , C07D307/46 , C07D317/16 , C07D317/24 , C07D317/34 , C07F7/1856
摘要： Prostaglandin analogs are disclosed that have the .alpha.-chain terminating with the group --CH(OR')OR" wherein R' and R" are the same or different and are hydrogen, C.sub.1 to C.sub.4 alkanoyl or optionally substituted benzoyl, the substituents selected from the group C.sub.1 to C.sub.4 alkyl, C.sub.1 to C.sub.4 alkoxy, halo and trifluoromethyl. These compounds are useful as hypotensive agents, gastric secretory and platelet aggregation enhibitors and bronchodilators.
摘要翻译：公开前列腺素类似物，其具有以基团-CH（OR'）OR“终止的α-链，其中R'和R”相同或不同，并且是氢，C 1至C 4烷酰基或任选取代的苯甲酰基，取代基选自C1至C4烷基，C1至C4烷氧基，卤素和三氟甲基。这些化合物可用作降压药，胃分泌和血小板聚集抑制剂和支气管扩张剂。

39. 发明授权

US4288633A 1-Hydroxymethyl-11-deoxy-16-hydroxy-prosten-1-ol-derivatives 失效
标题翻译： 1-羟甲基-11-脱氧-16-羟基 - 前列腺-1-醇衍生物
公开(公告)号：US4288633A
公开(公告)日：1981-09-08
申请号：US137031
申请日：1980-04-03
申请人： Allan Wissner , Middleton B. Floyd, Jr.
发明人： Allan Wissner , Middleton B. Floyd, Jr.
IPC分类号： C07C45/59 , C07C49/707 , C07C51/09 , C07C405/00 , C07F7/18 , C07C35/06 , C07C49/597
CPC分类号： C07F7/1856 , C07C405/0016 , C07C405/0025 , C07C45/59 , C07C49/707 , C07C51/09
摘要： Prostaglandin analogs are disclosed that have the .alpha.-chain terminating with the group --CH(OR')OR" wherein R' and R" are the same or different and are hydrogen, C.sub.1 to C.sub.4 alkanoyl or optionally substituted benzoyl, the substituents selected from the group C.sub.1 to C.sub.4 alkyl, C.sub.1 to C.sub.4 alkoxy, halo and trifluoromethyl. These compounds are useful as hypotensive agents, gastric secretory and platelet aggregation enhibitors and bronchodilators.
摘要翻译：公开前列腺素类似物，其具有以基团-CH（OR'）OR“终止的α-链，其中R'和R”相同或不同，并且是氢，C 1至C 4烷酰基或任选取代的苯甲酰基，取代基选自C1至C4烷基，C1至C4烷氧基，卤素和三氟甲基。这些化合物可用作降压药，胃分泌和血小板聚集抑制剂和支气管扩张剂。

40. 发明授权

US4278806A 15-Deoxy-16-substituted-19-chloro-20-nor prostane derivatives of the E and F series 失效
标题翻译： E和F系列的15-脱氧-16-取代-19-氯代-20-或前列腺衍生物
公开(公告)号：US4278806A
公开(公告)日：1981-07-14
申请号：US46725
申请日：1979-06-07
申请人： Allan Wissner
发明人： Allan Wissner
IPC分类号： C07C29/42 , C07C45/45 , C07C405/00 , C07F7/08 , C07F7/18 , C07F7/22 , C07C177/00
CPC分类号： C07F7/2212 , C07C29/42 , C07C405/00 , C07C405/0025 , C07C45/45 , C07F7/0818 , C07F7/1852
摘要： The invention disclosed herein relates to pharmacologically active prostaglandin derivatives of the E and F series wherein C-16 is substituted with hydrogen, methyl, vinyl or ethynyl and C-19 substituted with chloro and the .beta.-chain consists of 7 carbon atoms.
摘要翻译：本文公开的本发明涉及E和F系列的药理学活性前列腺素衍生物，其中C-16被氢，甲基，乙烯基或乙炔基取代，C-19被氯取代，β-链由7个碳原子组成。

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