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1. 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。

2. 发明授权

US5187284A N-phenyl-N'-benzothienylmethyl-bis-diamino-5-methylene-1,3-diox ane-4,6-dione derivatives 失效
标题翻译： N-苯基-N'-苯并噻吩基甲基 - 二 - 二氨基-5-亚甲基-1,3-二恶烷-4,6-二酮衍生物
公开(公告)号：US5187284A
公开(公告)日：1993-02-16
申请号：US914886
申请日：1992-07-22
申请人： William F. Fobare , Donald P. Strike
发明人： William F. Fobare , Donald P. Strike
IPC分类号： C07D405/12 , C07D409/12
CPC分类号： C07D405/12 , C07D409/12
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 hydrogen, alkyl, alkenyl, cycloalkyl, phenyl, benzyl or substituted phenyl or benzyl or alkoxy; 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是氢，烷基，烯基，环烷基，苯基，苄基或取代的苯基或苄基或烷氧基; 或其药学上可接受的盐是ACAT抑制剂。

3. 发明授权

US5179216A 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： N，N'，N'-三取代-5-联苯甲酰-1,3-二氧戊环-4,6-二酮的ACYL-COA：胆固醇 - 乙酸转移酶抑制剂
公开(公告)号：US5179216A
公开(公告)日：1993-01-12
申请号：US719873
申请日：1991-06-24
申请人： William F. Fobare , Donald P. Strike
发明人： William F. Fobare , Donald P. Strike
IPC分类号： A61K31/335 , A61K31/357 , A61P3/06 , A61P9/10 , C07D319/06 , C07D405/12 , C07F7/18
CPC分类号： C07D405/12 , C07D319/06 , 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 alkyl, hydroxyalkyl, alkenyl, cycloalkyl, phenylcycloalkyl, 1-hydroxymethylphenethyl, 1-(t-butyl)dimethylsilyloxymethyl-phenethyl, 1-(t-butyl)dimethylsilyloxymethylisopentyl, 1-hydroxymethylisopentyl, phenyl, benzyl or substituted phenyl or benzyl, where the substituents are alkyl, alkoxy, halogen, cyano, trifluoromethyl, amino, alkylamino, dialkylamino, nitro or phenyl, benzyl, phenethyl or R.sub.1 is thienyl, imidazolyl, thiazolyl, pyridinyl, pyrimidinyl, pyrazinyl, benzamidazolyl, phenylalkylpiperidinyl or morpholino; R.sub.2 is 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.

4. 发明授权

US5380853A 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：US5380853A
公开(公告)日：1995-01-10
申请号：US152656
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 , C07D401/12
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。

5. 发明授权

US4792614A Substituted furans as inhibitors of 3-hydroxy-3-methylglutaryl-coa reductase 失效
标题翻译：取代呋喃作为3-羟基-3-甲基戊二酰辅酶A还原酶的抑制剂
公开(公告)号：US4792614A
公开(公告)日：1988-12-20
申请号：US082013
申请日：1987-08-05
申请人： William F. Fobare , Donald P. Strike
发明人： William F. Fobare , Donald P. Strike
IPC分类号： C07D307/54 , C07D407/06 , C07D309/30 , C07D307/34
CPC分类号： C07D407/06 , C07D307/54
摘要： Compounds of the formula: ##STR1## in which ##STR2## where M is hydrogen or alkyl; one of R.sup.2 and R.sup.3 is phenyl or substituted phenyl where the substituent is alkyl, alkoxy, halogen, trifluoromethyl, nitro, amino, cyano or carboxyl; and the other of R.sup.2 and R.sup.3 is hydrogen, alkyl, or a halogen; or a pharmaceutically acceptable salt thereof, are HMG--CoA reductase inhibitors useful in the treatment of atherosclerosis, hypercholesterolaemia, hyperlipaemia and similar disease states characterized by elevated cholesterol levels in the blood.
摘要翻译：下式的化合物：其中M为氢或烷基的其中 + TR R2和R3中的一个是苯基或取代的苯基，其中取代基是烷基，烷氧基，卤素，三氟甲基，硝基，氨基，氰基或羧基; R2和R3中的另一个是氢，烷基或卤素; 或其药学上可接受的盐是可用于治疗动脉粥样硬化，高胆固醇血症，高脂血症和以血液中升高的胆固醇水平为特征的类似疾病状态的HMG-CoA还原酶抑制剂。

6. 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。

7. 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。

8. 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。

9. 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。

10. 发明授权

US5153218A N,N',N'-trisubstituted-bis-amino-3-methylene-2,4(3H,5H)-furandione inhibitors of acyl-CoA:cholesterol-acyl transferase 失效
标题翻译： N，N'，N'-三取代 - 双 - 氨基-3-亚甲基-2,4（3H，5H） - 呋喃二酮的酰基辅酶A：胆固醇 - 酰基转移酶
公开(公告)号：US5153218A
公开(公告)日：1992-10-06
申请号：US784202
申请日：1991-10-28
申请人： William F. Fobare
发明人： William F. Fobare
IPC分类号： C07D307/34
CPC分类号： C07D307/34
摘要： The 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, hydroxyalkyl, alkenyl, cycloalkyl, phenyl, benzyl, phenylethyl or substituted phenyl, benzyl or phenylethyl, alkoxy, halogen, cyano, trifluoromethyl, amino, alkylamino, dialkylamino, nitro, phenyl, benzyl or phenethyl or R.sub.1 is thienyl, imidazolyl, thiazolyl, pyridinyl, pyrimidinyl, pyrazinyl or benzamidazolyl; R.sub.2 is hydrogen, alkyl, cycloalkyl, phenyl, benzyl or substituted phenyl or benzyl, alkoxy, hologen, cyano, trifluoromethyl amino, nitro, alkylamino or dialkylamino; or a pharmaceutically acceptable salt thereof, are useful as ACAT inhibitors.
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，烷基或烷氧基; 卤素，氰基，三氟甲基，氨基，烷基氨基，二烷基氨基，硝基，苯基，苄基或苯乙基，或者R 1是噻吩基，咪唑基，噻唑基，吡啶基，嘧啶基，吡嗪基或苯并咪唑基; R 2是氢，烷基，环烷基，苯基，苄基或取代的苯基或苄基，烷氧基，氢原子，氰基，三氟甲基氨基，硝基，烷基氨基或二烷基氨基; 或其药学上可接受的盐可用作ACAT抑制剂。

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