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11. 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”。

12. 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。

13. 发明授权

US5147864A 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：US5147864A
公开(公告)日：1992-09-15
申请号：US599580
申请日：1990-10-18
申请人： Allan Wissner , Kenneth Green , Robert E. Schaub
发明人： Allan Wissner , Kenneth Green , Robert E. Schaub
IPC分类号： C07F9/58 , C07F9/60 , C07F9/62 , C07F9/6506 , C07F9/6509 , C07F9/6512 , C07F9/6539
CPC分类号： C07F9/60 , C07F9/581 , C07F9/62 , C07F9/65061 , C07F9/650911 , C07F9/650958 , C07F9/65121 , C07F9/6539
摘要： The invention is novel compounds of the formula: ##STR1## wherein: X is a phenyl or naphthyl ring optionally substituted in any position with one to four substituents of;(i) --R.sub.2, wherein R.sub.2 is C.sub.1 -C.sub.25 alkyl, C.sub.1 -C.sub.25 alkenyl, C.sub.1 -C.sub.25 alkoxy, C.sub.1 -C.sub.25 thioalkyl, C.sub.1 -C.sub.25 alkenyloxy, phenyl, phenoxy, substituted phenyl or substituted phenoxy wherein the substituents are C.sub.1 -C.sub.20 alkyl, C.sub.1 -C.sub.20 alkoxy, halogen and trifluoremethyl;(ii) hydrogen, halogen, trifluoromethyl, cyano and nitro;(iii) --CO.sub.2 R.sub.3, --CONHR.sub.3, --CHO, OCONHR.sub.3, and --NHCOR.sub.3 wherein R.sub.3 is C.sub.1 -C.sub.25 alkyl, C.sub.1 -C.sub.25 alkenyl, phenyl or substituted phenyl wherein the substituents are C.sub.1 -C.sub.20 alkyl, C.sub.1 -C.sub.20 alkoxy, halogen or trifluoromethyl;R.sub.1 is one to four substituents on the aromatic ring which may be in any position and are hydrogen, C.sub.1 -C.sub.5 alkyl, C.sub.1 -C.sub.5 alkoxy or halogen;--CH.sub.2 --Y is a single substituent of the aromatic ring which may occupy any position where Y is ##STR2## wherein R.sub.4 represents one to four substituents of the heterocyclic ring which may occupy a non-hetero atom position and is C.sub.1 -C.sub.5 alkyl, C.sub.1 -C.sub.5 alkoxy, hydrogen or halogen; and n is the integer 0 or 1 which are antagonists of platelet activating factor.
摘要翻译：本发明是下式的新化合物：其中：X是任选在任何位置被一至四个取代基取代的苯基或萘基环; （i）-R2，其中R2是C1-C25烷基，C1-C25烯基，C1-C25烷氧基，C1-C25硫代烷基，C1-C25烯氧基，苯基，苯氧基，取代的苯基或取代的苯氧基，其中取代基是C1-C20 烷基，C 1 -C 20烷氧基，卤素和三氟甲基; （ii）氢，卤素，三氟甲基，氰基和硝基; （iii）-CO 2 R 3，-CONHR 3，-CHO，OCONHR 3和-NHCOR 3，其中R 3是C 1 -C 25烷基，C 1 -C 25烯基，苯基或取代的苯基，其中取代基是C 1 -C 20烷基，C 1 -C 20烷氧基，卤素或三氟甲基 R 1是芳环上一至四个可以在任何位置并且是氢，C 1 -C 5烷基，C 1 -C 5烷氧基或卤素的取代基; -CH 2 -Y是芳环的单个取代基，其可以占据任何位置，其中Y是可以占据非杂原子位置的杂环的一至四个取代基，是C 1 -C 5烷基，C 1 -C 5烷氧基，氢或卤素; 并且n是作为血小板活化因子的拮抗剂的整数0或1。

14. 发明授权

US4894367A Antihypertensive phosphate derivatives 失效
标题翻译：抗高血压磷酸盐衍生物
公开(公告)号：US4894367A
公开(公告)日：1990-01-16
申请号：US194748
申请日：1988-07-18
申请人： Allan Wissner , Phaik E. Sum , Robert E. Schaub
发明人： Allan Wissner , Phaik E. Sum , Robert E. Schaub
IPC分类号： C07F9/10
CPC分类号： C07F9/10
摘要： Antihypertensive phosphate derivatives having the following formula: ##STR1## wherein X is selected from one or more of C.sub.1 -C.sub.24 alkyl; C.sub.1 -C.sub.24 alkoxy; n and m are integers from 0 to 25 and the sum of which are less than or equal to 25; phenyl or substituted phenyl alkoxy, halogen, trifluoromethyl, phenyl, and substituted phenyl, phenoxy; and substituted phenoxy, wherein the substituents are C.sub.1 -C.sub.20 branched or straight chain alkyl, halogen, trifluoromethyl, phenyl and substituted phenyl; Q is selected from ##STR2## and --OR.sub.3 R.sub.1 is selected form hydrogen, C.sub.1 -C.sub.4 alkoxy and C.sub.1 -C.sub.4 alklyamino and R.sub.3 is C.sub.1 -C.sub.4 alkyl, with the provision that when Q is ##STR3## R.sub.1 is C.sub.1 -C.sub.4 branched or straight chain alkyl; T is a bivalent radical selected from alkylene or arylalkylene substituted at any position with one or more C.sub.1 -C.sub.10 alkyl with oxygen atom attached directly to the aromatic ring; Z is ##STR4## R.sub.2 is hydrogen or C.sub.1 -C.sub.4 branched straight chain alkyl; Q is an integer from 4-7.
摘要翻译：具有下式的抗高血压磷酸酯衍生物：其中X选自C 1 -C 24烷基中的一种或多种; C 1 -C 24烷氧基; n和m是0至25的整数，其总和小于或等于25; 苯基或取代的苯基烷氧基，卤素，三氟甲基，苯基和取代的苯基，苯氧基; 和取代的苯氧基，其中取代基是C 1 -C 20支链或直链烷基，卤素，三氟甲基，苯基和取代的苯基; Q选自，-OR3 R1选自氢，C1-C4烷氧基和C1-C4烷基氨基，R3是C1-C4烷基，条件是当Q是C1-C4支链或直链烷基; T是选自在具有一个或多个具有氧原子直接连接到芳环上的C 1 -C 10烷基的任何位置处取代的亚烷基或芳基亚烷基的二价基团; Z是R 2是氢或C 1 -C 4支链直链烷基; Q是4-7的整数。

15. 发明授权

US4883816A Antihypertensive derivatives 失效
标题翻译：抗高血压衍生物
公开(公告)号：US4883816A
公开(公告)日：1989-11-28
申请号：US157055
申请日：1988-02-16
申请人： Allan Wissner , Phaik E. Sum , Robert E. Schaub
发明人： Allan Wissner , Phaik E. Sum , Robert E. Schaub
IPC分类号： C07F9/10
CPC分类号： C07F9/10
摘要： Antihypertensive sulfonyl derivatives having the following formula are described: ##STR1## where R" is a C.sub.2 -C.sub.20 alkyl group,R".sub.1 is a C.sub.1 to C.sub.4 alkyl group,y is an integer from 2 to 10 andJ.sup.- is a pharmocologically acceptable anion.
摘要翻译：描述了具有下式的抗高血压磺酰基衍生物：其中R“为C 2 -C 20烷基，R”1为C 1至C 4烷基，y为2至10的整数，J为 - 药学上可接受的阴离子。

16. 发明授权

US4699990A Antihypertensive phosphate derivatives 失效
标题翻译：抗高血压磷酸盐衍生物
公开(公告)号：US4699990A
公开(公告)日：1987-10-13
申请号：US679791
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
CPC分类号： C07F9/10
摘要： Antihypertensive phosphate derivatives are described having the following formula: ##STR1## wherein n is an integer 1 or 2; m is an integer 1 or 2, and the sum of n and m must be 3; X is selected from the group consisting of C.sub.1 -C.sub.24 branched or straight chain alkoxy and substituted phenoxy wherein the substituents are selected from one or more of the group consisting of C.sub.1 -C.sub.20 branched or straight chain alkyl, C.sub.1 -C.sub.20 branched or straight chain alkoxy, halogen, phenyl and substituted phenyl; 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).sub.p --, where p is an integer from 2 to 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 --.sup.+ N(R.sub.2).sub.3 and ##STR3## wherein 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 and q is an integer from 4 to 7.
摘要翻译：抗高血压磷酸酯衍生物被描述为具有下列结构式：其中n是整数1或2; m为整数1或2，n和m之和必须为3; X选自C 1 -C 24支链或直链烷氧基和取代苯氧基，其中取代基选自C1-C20支链或直链烷基，C1-C20支链或直链烷氧基中的一个或多个，卤素，苯基和取代的苯基; 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2至12的整数，并且 - （CHR）p - 部分代表亚烷基链，被一个或多个C 1 -C 10烷基或苯基取代; Z选自 - + N（R 2）3和，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是整数从4到7。

17. 发明授权

US4983592A 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：US4983592A
公开(公告)日：1991-01-08
申请号：US286193
申请日：1988-12-19
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.

18. 发明授权

US4900731A Antihypertensive phosphate derivatives 失效
标题翻译：抗高血压磷酸盐衍生物
公开(公告)号：US4900731A
公开(公告)日：1990-02-13
申请号：US97100
申请日：1987-09-15
申请人： Allan Wissner , Robert E. Schaub
发明人： Allan Wissner , Robert E. Schaub
IPC分类号： C07F9/10
CPC分类号： C07F9/10
摘要： Antihypertensive phosphate derivatives are described having the following formula: ##STR1## wherein n is an integer 1 or 2; m is an integer 1 or 2, and the sum of n and m must be 3; X is selected from the group consisting of C.sub.1 -C.sub.24 branched or straight chain alkoxy and substituted phenoxy wherein the substituents are selected from one or more of the group consisting of C.sub.1 -C.sub.20 branched or straight chain alkyl, C.sub.1 -C.sub.20 branched or straight chain alkoxy, halogen, phenyl and substituted phenyl; 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).sub.p --, where p is an integer from 2 to 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 ##STR3## wherein 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 and q is an integer from 4 to 7.
摘要翻译：抗高血压磷酸酯衍生物被描述为具有下列结构式：其中n是整数1或2; m为整数1或2，n和m之和必须为3; X选自C 1 -C 24支链或直链烷氧基和取代苯氧基，其中取代基选自C1-C20支链或直链烷基，C1-C20支链或直链烷氧基中的一个或多个，卤素，苯基和取代的苯基; 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2至12的整数，并且 - （CHR）p - 部分代表亚烷基链，被一个或多个C 1 -C 10烷基或苯基取代; Z选自，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是4至7的整数。

19. 发明授权

US4640913A Phosphocholine derivatives having antihypertensive action 失效
标题翻译：具有抗高血压作用的磷酸胆碱衍生物
公开(公告)号：US4640913A
公开(公告)日：1987-02-03
申请号：US457097
申请日：1983-01-10
申请人： Allan Wissner , Robert E. Schaub , Phaik E. Sum
发明人： Allan Wissner , Robert E. Schaub , Phaik E. Sum
IPC分类号： C07F9/10 , A61K31/185
CPC分类号： C07F9/10
摘要： Phosphocholine derivatives and compositions are described which are useful as hypotensive agents and in the treatment of hypertension in warm-blooded animals.
摘要翻译：描述了磷酸胆碱衍生物和组合物，其可用作降血压剂和在温血动物中治疗高血压。

20. 发明申请

US20080268460A1 Assays to Identify Irreversibly Binding Inhibitors of Receptor Tyrosine Kinases 审中-公开
标题翻译：鉴定受体酪氨酸激酶不可逆结合抑制剂的方法
公开(公告)号：US20080268460A1
公开(公告)日：2008-10-30
申请号：US11569288
申请日：2005-05-11
申请人： Frank Loganzo , Lee M. Greenberger , Xingshi Tan , Allan Wissner
发明人： Frank Loganzo , Lee M. Greenberger , Xingshi Tan , Allan Wissner
IPC分类号： G01N33/53
CPC分类号： C12Q1/485 , G01N33/74 , G01N2500/00
摘要： The present invention relates to a method of identifying an inhibitor of a receptor tyrosine kinase that irreversibly binds to the kinase. Specifically, the method comprises using a variety of assays, either alone or in combination, to identify compounds that irreversibly bind to tyrosine kinases. More specifically, there are four assays, which are novel variations of a basic enzyme assay and identify irreversible binding inhibitors.
摘要翻译：本发明涉及鉴定不可逆地结合激酶的受体酪氨酸激酶抑制剂的方法。具体地，该方法包括单独或组合地使用多种测定来鉴定不可逆地结合酪氨酸激酶的化合物。更具体地，有四种测定法，其是碱性酶测定的新变体并鉴定不可逆结合抑制剂。

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