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31. 发明授权

US4038308A Prostaglandin derivatives 失效
公开(公告)号：US4038308A
公开(公告)日：1977-07-26
申请号：US722458
申请日：1976-09-13
申请人： Donald P. Strike
发明人： Donald P. Strike
IPC分类号： C07C405/00 , C07D317/72 , C07C177/00
CPC分类号： C07D317/72 , C07C405/00
摘要： Derivatives of 11-deoxy-PGE.sub.1 and 11-deoxy-PGE.sub.2 are prepared. These new compounds not heretofore found in nature possess various pharmacological activities, one of which is bronchodilation.

32. 发明授权

US5877324A 2-(substituted sulfanyl)-3,5-dihydro-imidazol-4-one derivatives 失效
标题翻译：（取代的硫烷基）-3,5-二氢 - 咪唑-4-酮衍生物
公开(公告)号：US5877324A
公开(公告)日：1999-03-02
申请号：US754441
申请日：1996-11-21
申请人： Hassan M. Elokdah , Theodore S. Sulkowski , Donald P. Strike
发明人： Hassan M. Elokdah , Theodore S. Sulkowski , Donald P. Strike
IPC分类号： C07D233/86
CPC分类号： C07D233/86
摘要： The compound of formula I: ##STR1## wherein R is phenyl or phenyl optionally substituted with one or more groups selected from halogen, alkyl, perfluoroalkyl, alkoxy, perfluoroalkoxy, hydroxy, alkanoyloxy, aroyloxy or arylalkanoyloxy; R.sup.3 is alkyl, aryl or arylalkyl; or a pharmaceutically acceptable salt thereof, are use for increasing HDL blood levels.
摘要翻译：式I的化合物：其中R是苯基或任选被一个或多个选自卤素，烷基，全氟烷基，烷氧基，全氟烷氧基，羟基，烷酰氧基，芳氧基或芳基烷酰氧基的基团取代的苯基; R3是烷基，芳基或芳基烷基; 或其药学上可接受的盐用于增加HDL血液水平。

33. 发明授权

US5602151A Cholesterol ester hydrolase inhibitors 失效
标题翻译：胆固醇酯水解酶抑制剂
公开(公告)号：US5602151A
公开(公告)日：1997-02-11
申请号：US572993
申请日：1995-12-15
申请人： Richard E. Mewshaw , Thomas J. Commons , Donald P. Strike
发明人： Richard E. Mewshaw , Thomas J. Commons , Donald P. Strike
IPC分类号： C07C271/40 , C07D295/205 , A61K31/445 , C07D211/06
CPC分类号： C07D295/205 , C07C271/40 , C07C2101/14 , C07C2103/93
摘要： The compounds of the formula: ##STR1## in which X is ##STR2## where R.sup.7 is hydrogen, alkyl, hydroxy, alkanoyloxy, hydroxyalkyl, hydroxycarbonyl, alkoxycarbonyl, phenyl or substituted phenyl, in which the substituent is alkyl, alkoxy, halo, nitro, cyano, haloalkyl, perhaloalkyl or dialkylaminoalkyl; R.sup.8 is hydrogen or alkyl or R.sup.7 and R.sup.8 taken together are polymethylene; R.sup.9 is hydrogen, alkyl, phenyl or substituted phenyl, in which the substituent is alkyl, alkoxy, halo, nitro, cyano or perhaloalkyl; R.sup.10 is hydrogen, alkyl or gemdialkyl; n is one of the integers 0, 1 or 2; and R.sup.3, R.sup.4, R.sup.5 and R.sup.6 are, independently, hydrogen, alkyl, alkoxy, halo, nitro, cyano or perhaloalkyl, alkoxycarbonyl or hydroxycarbonyl; and when X is --NR.sup.9 -- or R.sup.7 is an amino alkyl group, a pharmaceutically acceptable salt thereof; are useful as inhibitors of cholesterol ester hydrolase.
摘要翻译：其中X为的化合物，其中R 7为氢，烷基，羟基，烷酰氧基，羟基烷基，羟基羰基，烷氧基羰基，苯基或取代的苯基，其中取代基为烷基，烷氧基，卤素，硝基，氰基，卤代烷基，全卤代烷基或二烷基氨基烷基; R8是氢或烷基或R7和R8一起是聚亚甲基; R9是氢，烷基，苯基或取代的苯基，其中取代基是烷基，烷氧基，卤素，硝基，氰基或全卤代烷基; R10为氢，烷基或偕二烷基; n是整数0,1或2之一; 并且R 3，R 4，R 5和R 6独立地为氢，烷基，烷氧基，卤素，硝基，氰基或全卤代烷基，烷氧基羰基或羟基羰基。当X是-NR9-或R7是氨基烷基时，其药学上可接受的盐; 可用作胆固醇酯水解酶的抑制剂。

34. 发明授权

US5399697A N,N',N'-trisubstituted-5-bisaminomethylene-1,3-dioxane-4,6-dione inhibitors of acyl-CoA:cholesterol-acyl transferase 失效
标题翻译：酰基辅酶A的N，N'，N'-三取代-5-二氨基亚甲基-1,3-二恶烷-4,6-二酮抑制剂：胆固醇 - 酰基转移酶
公开(公告)号：US5399697A
公开(公告)日：1995-03-21
申请号：US152613
申请日：1993-11-15
申请人： William F. Fobare , Donald P. Strike
发明人： William F. Fobare , Donald P. Strike
IPC分类号： C07D319/06 , C07D405/12 , C07F7/18 , C07D215/38 , C07D215/40
CPC分类号： C07D319/06 , C07D405/12 , C07F7/1852
摘要： The compounds of the formula: ##STR1## in which X, Y and Z are, independently, hydrogen, halogen, hydroxy, nitro, cyano, carboxyl, trifluoromethyl, phenyl, amino, alkylamino, dialkylamino, alkyl, alkoxy or phenylalkyloxy; R.sub.1 is thienyl, imidazolyl, thiazolyl, pyridinyl, quinolinyl, pyrimidinyl, pyrazinyl, benzamidazolyl, phenylalkylpiperidinyl or morpholino or athaae analogous hetercyclic groups with from one to three substituents selected from halogen, hydroxy, nitro, cyano, carboxyl, trifluoromethyl, phenyl, amino, alkylamino of 1 to 6 carbon atoms, dialkylamino in which each alkyl group has 1 to 6 carbon atoms, alkyl of 1 to 6 carbon atoms, or alkoxy of 1 to 6 carbon atoms; R.sub.2 is hydrogen, alkyl, cycloalkyl, phenyl, benzyl or substituted phenyl or benzyl in which said substituent is alkyl, alkoxy, halogen, cyano, trifluoromethyl amino, nitro, alkylamino or dialkylamino; and a pharmaceutically acceptable salt thereof; are ACAT inhibitors, some of which possess antioxidant properties.
摘要翻译：下式的化合物：其中X，Y和Z独立地为氢，卤素，羟基，硝基，氰基，羧基，三氟甲基，苯基，氨基，烷基氨基，二烷基氨基，烷基，烷氧基或苯基烷氧基。 R 1是具有1至3个选自卤素，羟基，硝基，氰基，羧基，三氟甲基，苯基，氨基，苯基，噻唑基，噻唑基，噻唑基，吡啶基，喹啉基，嘧啶基，吡嗪基，苯并咪唑基，苯基烷基哌啶基或吗啉代或类似的杂环基， 1至6个碳原子的烷基氨基，每个烷基具有1至6个碳原子的二烷基氨基，1至6个碳原子的烷基或1至6个碳原子的烷氧基; R 2是氢，烷基，环烷基，苯基，苄基或取代的苯基或苄基，其中所述取代基是烷基，烷氧基，卤素，氰基，三氟甲基氨基，硝基，烷基氨基或二烷基氨基; 及其药学上可接受的盐; 是ACAT抑制剂，其中一些具有抗氧化性质。

35. 发明授权

US5281714A N,N',N'-trisubstituted-5-bisaminomethylene-1,3-dioxane-4,6-dione inhibitors of acyl-CoA: cholesterol-acyl transferase 失效
标题翻译：酰基辅酶A的N，N'，N'-三取代-5-二氨基亚甲基-1,3-二恶烷-4,6-二酮抑制剂：胆固醇 - 酰基转移酶
公开(公告)号：US5281714A
公开(公告)日：1994-01-25
申请号：US998213
申请日：1992-12-30
申请人： William F. Fobare , Donald P. Strike
发明人： William F. Fobare , Donald P. Strike
IPC分类号： C07D319/06 , C07D405/12 , C07F7/18
CPC分类号： C07D319/06 , C07D405/12 , C07F7/1852
摘要： The compounds of the formula: ##STR1## in which X, Y and Z are, independently, hydrogen, halogen, hydroxy, nitro, cyano, carboxyl, trifluoromethyl, phenyl, amino, alkylamino, dialkylamino, alkyl, alkoxy or phenylalkyloxy; R.sub.1 is thienyl, imidazolyl, thiazolyl, pyridinyl, quinolinyl, pyrimidinyl, pyrazinyl, benzamidazolyl, phenylalkylpiperidinyl or morpholino or athaae analogous hetercyclic groups with from one to tahree substituents selected from halogen, hydroxy, nitro, cyano, carboxyl, trifluoromethyl, phenyl, amino, alkylamino of 1 to 6 carbon atoms, dialkylamino in which each alkyl group has 1 to 6 carbon atoms, alkyl of 1 to 6 carbon atoms, or alkoxy of 1 to 6 carbon atoms; R.sub.2 is hydrogen, alkyl, cycloalkyl, phenyl, benzyl or substituted phenyl or benzyl in which said substituent is alkyl, alkoxy, halogen, cyano, trifluoromethyl amino, nitro, alkylamino or dialkylamino; and a pharmaceutically acceptable salt thereof; are ACAT inhibitors, some of which possess antioxidant properties.
摘要翻译：下式的化合物：其中X，Y和Z独立地为氢，卤素，羟基，硝基，氰基，羧基，三氟甲基，苯基，氨基，烷基氨基，二烷基氨基，烷基，烷氧基或苯基烷氧基。 R 1是具有1至多个取代基的选自卤素，羟基，硝基，氰基，羧基，三氟甲基，苯基，氨基，噻唑基，噻唑基，噻唑基，吡啶基，喹啉基，嘧啶基，吡嗪基，苯并咪唑基，苯基烷基哌啶基或吗啉代或类似的杂环基团。 1至6个碳原子的烷基氨基，每个烷基具有1至6个碳原子的二烷基氨基，1至6个碳原子的烷基或1至6个碳原子的烷氧基; R 2是氢，烷基，环烷基，苯基，苄基或取代的苯基或苄基，其中所述取代基是烷基，烷氧基，卤素，氰基，三氟甲基氨基，硝基，烷基氨基或二烷基氨基; 及其药学上可接受的盐; 是ACAT抑制剂，其中一些具有抗氧化性质。

36. 发明授权

US5177219A N-phenyl-N'-thienylmethyl-bis-diamino-5-methylene-1,3-dioxane-4,6-dione compounds 失效
标题翻译： N-苯基-N'-噻吩基甲基 - 二 - 二氨基-5-亚甲基-1,3-二恶烷-4,6-二酮化合物
公开(公告)号：US5177219A
公开(公告)日：1993-01-05
申请号：US847127
申请日：1992-03-06
申请人： William F. Fobare , Donald P. Strike
发明人： William F. Fobare , Donald P. Strike
IPC分类号： C07D319/06 , C07D333/20 , C07D405/12 , C07D409/12
CPC分类号： C07D405/12 , C07D319/06 , C07D333/20 , C07D409/12
摘要： The compounds of the formula: ##STR1## wherein X, Y and Z are, independently, hydrogen, halogen, hydroxy, nitro, cyano, carboxyl, trifluoromethyl, phenyl, amino, mono and dialkylamino, C.sub.1 -C.sub.12 alkyl or C.sub.1 -C.sub.12 alkoxy; R.sup.1 represents hydrogen, C.sub.1 -C.sub.18 saturated or unsaturated alkyl, cycloalkyl, phenyl, benzyl or substituted phenyl or substituted benzyl where the substituents are C.sub.1 -C.sub.12 alkyl, or C.sub.1 -C.sub.12 alkoxy; R.sup.2 represents a substituted thienyl group where the substituents are, independently, the same as X, Y and Z; or a pharmaceutically acceptable salt thereof, are ACAT inhibitors.
摘要翻译：下式的化合物其中X，Y和Z独立地是氢，卤素，羟基，硝基，氰基，羧基，三氟甲基，苯基，氨基，单和二烷基氨基，C 1 -C 12烷基或C 1 -C 12烷氧基 ; R1表示氢，C1-C18饱和或不饱和的烷基，环烷基，苯基，苄基或取代的苯基或取代的苄基，其中取代基是C1-C12烷基或C1-C12烷氧基; R 2表示取代基，其中取代基独立地与X，Y和Z相同; 或其药学上可接受的盐是ACAT抑制剂。

37. 发明授权

US5164505A N-phenyl-N'-alkyl-N'-pyridylmethyl-bis-diamino- 5-methylene-1,3-dioxane-4,6-diones 失效
标题翻译： N-苯基-N'-烷基-N'-吡啶基甲基 - 二 - 二氨基-5-亚甲基-1,3-二恶烷-4,6-二酮
公开(公告)号：US5164505A
公开(公告)日：1992-11-17
申请号：US879494
申请日：1992-05-07
申请人： William F. Fobare , Donald P. Strike , Patrick M. Andrae
发明人： William F. Fobare , Donald P. Strike , Patrick M. Andrae
IPC分类号： C07D405/06 , C07D405/12
CPC分类号： C07D405/06 , C07D405/12
摘要： A compound of the formula: ##STR1## wherein: X, Y and Z, independently, are hydrogen, halogen, hydroxy, nitro, cyano, carboxyl, trifluoromethyl, phenyl, amino, mono and di-alkylamino, C.sub.1 -C.sub.12 alkyl or C.sub.1 -C.sub.12 alkoxy; R.sub.1 is hydrogen, C.sub.1 -C.sub.18 saturated or unsaturated alkyl, cycloalkyl, phenyl, benzyl or substituted benzyl where the substituents are C.sub.1 -C.sub.12 alkyl, or C.sub.1 -C.sub.12 alkoxy; and R.sub.2 is represented by 2. ##STR2## in which X, Y, and Z are defined above; or a pharmaceutically acceptable salt thereof.
摘要翻译：下式化合物其中：X，Y和Z独立地是氢，卤素，羟基，硝基，氰基，羧基，三氟甲基，苯基，氨基，单和二烷基氨基，C 1 -C 12烷基或 C1-C12烷氧基; R1是氢，C1-C18饱和或不饱和的烷基，环烷基，苯基，苄基或取代的苄基，其中取代基是C1-C12烷基或C1-C12烷氧基; 其中X，Y和Z定义如上。或其药学上可接受的盐。

38. 发明授权

US5136039A N,N',N'-trisubstituted-5-bis-aminomethylene-1,3-dioxane-4,6-dione inhibitors of acyl-CoA:cholesterol-acyl transferase 失效
标题翻译：酰基辅酶A的N，N'，N'-三取代-5-二氨基亚甲基-1,3-二恶烷-4,6-二酮抑制剂：胆固醇 - 酰基转移酶
公开(公告)号：US5136039A
公开(公告)日：1992-08-04
申请号：US755918
申请日：1991-09-06
申请人： William F. Fobare , Donald P. Strike
发明人： William F. Fobare , Donald P. Strike
IPC分类号： C07D405/12
CPC分类号： C07D405/12
摘要： A compound of the formula: ##STR1## in which X, Y and Z are, independently, hydrogen, halogen, hydroxy, nitro, cyano, carboxyl, trifluoromethyl, phenyl, amino, alkylamino, dialkylamino, alkyl or alkoxy; R.sub.1 is alkyl, alkenyl, cycloalkyl, phenyl, benzyl or substituted phenyl or benzyl or alkoxy; R.sub.2 is: ##STR2## or a pharmaceutically acceptable salt thereof, are ACAT inhibitors.
摘要翻译：下式化合物：其中X，Y和Z独立地为氢，卤素，羟基，硝基，氰基，羧基，三氟甲基，苯基，氨基，烷基氨基，二烷基氨基，烷基或烷氧基; R 1是烷基，烯基，环烷基，苯基，苄基或取代的苯基或苄基或烷氧基; R2是：IMAMA或其药学上可接受的盐是ACAT抑制剂。

39. 发明授权

US5081253A Imidazo(4,5-C)pyridines as antiosteoporotic agents 失效
标题翻译：咪唑（4,5-C）吡啶类作为抗菌药
公开(公告)号：US5081253A
公开(公告)日：1992-01-14
申请号：US557247
申请日：1990-07-24
申请人： Arthur A. Santilli , Anthony C. Scotese , Donald P. Strike
发明人： Arthur A. Santilli , Anthony C. Scotese , Donald P. Strike
IPC分类号： A61K31/435 , A61P3/02 , A61P43/00 , C07D471/04
CPC分类号： C07D471/04
摘要： This invention relates to 2-substituted-imidazo[4,5-c]pyridines, to the process for their preparation, to pharmaceutical compositions containing said 2-substituted-imidazo[4,5-c]pyridines and to the use of said 2-substituted-imidazo[4,5-c]pyridines for modifying the balance between bone production and bone resorption in a host animal, including man.

40. 发明授权

US4728733A C-3' thiadiazinyl cephalosporin analogs 失效
标题翻译： C-3'噻二嗪基头孢菌素类似物
公开(公告)号：US4728733A
公开(公告)日：1988-03-01
申请号：US801460
申请日：1985-11-25
申请人： Jerauld S. Skotnicki , Donald P. Strike
发明人： Jerauld S. Skotnicki , Donald P. Strike
IPC分类号： A61K31/545 , C07D501/36 , C07D501/46
CPC分类号： C07D501/46
摘要： There are disclosed novel antibacterial compounds having the formula ##STR1## wherein R is hydrogen, lower alkyl, lower alkenyl, lower alkynyl, cyclo lower alkyl, aryl of 6-12 carbon atoms, all the said foregoing groups being optionally substituted with carboxy, lower alkoxycarbonyl, phenoxycarbonyl, amino, mono- or di-lower alkyl substituted amino, hydroxy, lower alkoxy, phenoxy, carbamoyl, lower alkyl carbonyl, benzoyl, cyano, nitro, formamido, lower alkanoylamino or benzamido;R.sup.1 is hydrogen, lower alkyl or an alkali metal cation;A is ##STR2## R.sup.2 and R.sup.3 are each individually hydrogen, lower alkyl, carboxy, lower alkoxycarbonyl, cyano, nitro, trifluoromethyl, phenyl or naphthyl; or R.sup.2 and R.sup.3 taken together represent ##STR3## or a 5- or 6- membered unsaturated aza-, diaza-, triaza-, tetraza-, thia-, thiaza-, oxathia-, oxathiaza-, oxa-, dioxa-, oxaza- or oxadiazacyclic moiety; and the dotted line denotes an optional double bond; andR.sup.4 is hydrogen, lower alkyl, phenyl or naphthyl.
摘要翻译：公开了具有式“IMAGE”的新型抗菌化合物，其中R是氢，低级烷基，低级烯基，低级炔基，环低级烷基，6-12个碳原子的芳基，所有上述基团任选被羧基取代，低级烷氧基羰基，苯氧基羰基，氨基，一或二低级烷基取代的氨基，羟基，低级烷氧基，苯氧基，氨基甲酰基，低级烷基羰基，苯甲酰基，氰基，硝基，甲酰氨基，低级烷酰氨基或苯甲酰氨基。 R1是氢，低级烷基或碱金属阳离子; A是图像，R 2和R 3各自独立地为氢，低级烷基，羧基，低级烷氧基羰基，氰基，硝基，三氟甲基，苯基或萘基。或者R 2和R 3一起代表一个或多个5-或6-元不饱和氮杂 - ，二氮杂 - ，三氮杂 - ，四嗪 - ，硫杂 - ，硫杂 - 氧化硫 - 氧基硫杂 - 氧杂 - 二氧杂环己二烯 - 或恶二氮环部分; 虚线表示任选的双键; R4是氢，低级烷基，苯基或萘基。

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