-
公开(公告)号：US5489611A
公开(公告)日：1996-02-06
申请号：US388043
申请日：1995-02-10
IPC分类号： A61K31/07 , A61K31/11 , A61K31/203 , A61K31/215 , A61K31/23 , A61P7/00 , A61K31/19
CPC分类号： A61K31/11 , A61K31/07 , A61K31/203 , A61K31/215 , Y10S514/824
摘要： Retinoids are effective to lower plasma levels of Lp (a) in mammals.
摘要翻译： 类维生素A有助于降低哺乳动物中的Lp（a）的血浆水平。
-
公开(公告)号：US5366987A
公开(公告)日：1994-11-22
申请号：US19411
申请日：1993-02-18
申请人： Helen T. Lee , Patrick M. O'Brien , Joseph A. Picard , Claude F. Purchase, Jr. , Bruce D. Roth , Drago R. Sliskovic , Andrew D. White
发明人： Helen T. Lee , Patrick M. O'Brien , Joseph A. Picard , Claude F. Purchase, Jr. , Bruce D. Roth , Drago R. Sliskovic , Andrew D. White
IPC分类号： A61K31/41 , A61K31/34 , A61K31/341 , A61K31/38 , A61K31/381 , A61K31/40 , A61K31/415 , A61K31/42 , A61K31/421 , A61K31/4245 , A61K31/425 , A61K31/426 , A61K31/433 , A61K31/435 , A61K31/44 , A61K31/4427 , A61K31/47 , A61K31/495 , A61K31/496 , A61K31/505 , A61P3/06 , A61P9/10 , A61P43/00 , C07D207/337 , C07D215/38 , C07D231/12 , C07D231/38 , C07D233/54 , C07D233/64 , C07D233/88 , C07D239/42 , C07D249/04 , C07D249/06 , C07D257/04 , C07D261/08 , C07D263/32 , C07D271/06 , C07D271/10 , C07D277/20 , C07D277/22 , C07D277/30 , C07D285/12 , C07D307/54 , C07D333/24 , C07D401/04 , C07D401/06 , C07D401/12 , C07D401/14 , C07D403/12 , C07D405/12 , C07D471/04
CPC分类号： C07D231/12 , C07D233/56 , C07D249/04 , C07D257/04 , C07D261/08 , C07D271/06 , C07D271/10 , C07D277/22 , C07D401/06 , C07D401/12 , C07D401/14 , C07D403/12 , C07D471/04
摘要： Pharmaceutically useful compounds having ACAT inhibitory activity of the formula ##STR1## wherein n is 0, 1, or 2, for X other than tetrazole and n=2 then R.sub.2 =R.sub.3 =H; R.sub.1 is phenyl, substituted phenyl, naphthyl, substituted naphthyl, a heteroaromatic group or a hydrocarbon group having from one to 18 carbon atoms; R.sub.2 and R.sub.3 are hydrogen, halo, hydroxy, alkyl, alkenyl, cycloalkyl, phenyl, substituted phenyl, a heteroaryl, or form a spiroalkyl group; X is a heteromonocyclic 5-membered ring containing one to four heteroatoms, said heteroatoms being nitrogen, oxygen or sulfur, and combination thereof; and R.sub.4 is a hydrocarbon group having from one to 20 carbon atoms are described as well as methods of their manufacture.
摘要翻译： 对于除了四唑之外的X，n = 2，然后R2 = R3 = H，具有式IMAImage的ACAT抑制活性的药学上有用的化合物，其中n为0,1或2。 R 1是苯基，取代的苯基，萘基，取代的萘基，杂芳基或具有1至18个碳原子的烃基; R2和R3是氢，卤素，羟基，烷基，烯基，环烷基，苯基，取代的苯基，杂芳基或形成螺烷基; X是含有一至四个杂原子的杂单环五元环，所述杂原子是氮，氧或硫，以及它们的组合; 并且描述了R4是具有1至20个碳原子的烃基以及它们的制备方法。
-
公开(公告)号：US5441975A
公开(公告)日：1995-08-15
申请号：US274088
申请日：1994-07-12
申请人： Helen T. Lee , Patrick M. O'Brien , Joseph A. Picard , Claude F. Purchase, Jr. , Bruce D. Roth , Drago R. Sliskovic , Andrew D. White
发明人： Helen T. Lee , Patrick M. O'Brien , Joseph A. Picard , Claude F. Purchase, Jr. , Bruce D. Roth , Drago R. Sliskovic , Andrew D. White
IPC分类号： A61K31/41 , A61K31/34 , A61K31/341 , A61K31/38 , A61K31/381 , A61K31/40 , A61K31/415 , A61K31/42 , A61K31/421 , A61K31/4245 , A61K31/425 , A61K31/426 , A61K31/433 , A61K31/435 , A61K31/44 , A61K31/4427 , A61K31/47 , A61K31/495 , A61K31/496 , A61K31/505 , A61P3/06 , A61P9/10 , A61P43/00 , C07D207/337 , C07D215/38 , C07D231/12 , C07D231/38 , C07D233/54 , C07D233/64 , C07D233/88 , C07D239/42 , C07D249/04 , C07D249/06 , C07D257/04 , C07D261/08 , C07D263/32 , C07D271/06 , C07D271/10 , C07D277/20 , C07D277/22 , C07D277/30 , C07D285/12 , C07D307/54 , C07D333/24 , C07D401/04 , C07D401/06 , C07D401/12 , C07D401/14 , C07D403/12 , C07D405/12 , C07D471/04
CPC分类号： C07D231/12 , C07D233/56 , C07D249/04 , C07D257/04 , C07D261/08 , C07D271/06 , C07D271/10 , C07D277/22 , C07D401/06 , C07D401/12 , C07D401/14 , C07D403/12 , C07D471/04
摘要： Pharmaceutically useful compounds having ACAT inhibitory activity of the formula ##STR1## wherein n is 0, 1, or 2, for X other than tetrazole and n=2 then R.sub.2 =R.sub.3 =H; R.sub.1 is phenyl, substituted phenyl, naphthyl, substituted naphthyl, a heteroaromatic group or a hydrocarbon group having from one to 18 carbon atoms; R.sub.2 and R.sub.3 are hydrogen, halo, hydroxy, alkyl, alkenyl, cycloalkyl, phenyl, substituted phenyl, a heteroaryl, or form a spiroalkyl group; X is a heteromonocyclic 5-membered ring containing one to four heteroatoms, said heteroatoms being nitrogen, oxygen or sulfur, and combination thereof; and R.sub.4 is a hydrocarbon group having from one to 20 carbon atoms are described as well as methods of their manufacture.
摘要翻译： 对于除了四唑之外的X，n = 2，然后R2 = R3 = H，具有式IMAImage的ACAT抑制活性的药学上有用的化合物，其中n为0,1或2。 R 1是苯基，取代的苯基，萘基，取代的萘基，杂芳基或具有1至18个碳原子的烃基; R2和R3是氢，卤素，羟基，烷基，烯基，环烷基，苯基，取代的苯基，杂芳基或形成螺烷基; X是含有一至四个杂原子的杂单环五元环，所述杂原子是氮，氧或硫，以及它们的组合; 并且描述了R4是具有1至20个碳原子的烃基以及它们的制备方法。
-
4.发明授权Trans-6-(2-(n-heteroaryl-3,5-disubstituted)pyrazol-4-yl)-ethyl- or ethenyl)tetrahydro-4-hydroxypyran-2-one inhibitors of cholesterol biosynthesis 失效反式-6-（2-（正 - 杂芳基-3,5-二取代）吡唑-4-基） - 乙基或乙烯基）四氢-4-羟基吡喃-2-酮胆固醇生物合成抑制剂
公开(公告)号：US5102893A
公开(公告)日：1992-04-07
申请号：US540047
申请日：1990-06-19
IPC分类号： C07D405/14 , C07D409/14 , C07D417/14
CPC分类号： C07D405/14 , C07D409/14 , C07D417/14
摘要： Certain trans-6-[2-(N-heteroaryl-3,5-disubstituted) pyrazol-4-yl)ethyl]- or ethenyl]tetrahydro-4-hydroxy-2H-pyran-2-ones and the corresponding ring-opened acids, esters and N-oxides derived therefrom which are potent inhibitors of the enzyme 3-hydroxy-3-methylglutaryl-coenzyme A reductase (HMG CoA reductase) and are thus useful hydrolipidemic or hypocholesterolemic agents. Pharmaceutical compositions containing such compounds, and a method of inhibiting the biosynthesis of cholesterol employing such pharmaceutical compositions are also disclosed.
摘要翻译： 某些反式-6- [2-（N-杂芳基-3,5-二取代）吡唑-4-基）乙基] - 或乙烯基]四氢-4-羟基-2H-吡喃-2-酮和相应的开环 酸，酯和N-氧化物，其是3-羟基-3-甲基戊二酰辅酶A还原酶（HMG CoA还原酶）的有效抑制剂，因此是有用的水溶性血液或低胆固醇血症药。 还公开了含有这些化合物的药物组合物和使用这种药物组合物抑制胆固醇生物合成的方法。
-
5.发明授权6-(((substituted)quinolinyl)ethyl)-and ethenyl)tetrahydro-4-hydroxypyran-2-one inhibitors of cholesterol biosynthesis 失效6 - （（取代的）喹啉基）乙基）和乙烯基）四氢-4-羟基吡喃-2-酮胆固醇生物合成抑制剂
公开(公告)号：US4761419A
公开(公告)日：1988-08-02
申请号：US129516
申请日：1987-12-07
IPC分类号： C07D215/12 , C07D215/18 , C07D401/04 , C07D405/06 , C07D405/14 , A61K31/34 , A61K31/47 , C07D217/12 , C07D217/14
CPC分类号： C07D401/04 , C07D215/12 , C07D215/18 , C07D405/06 , C07D405/14
摘要： Certain trans-6-[[(substituted)quinolinyl]ethyl]-and ethenyl]tetrahydro-4-hydroxypyran-2-ones and the corresponding dihydroxy ring-opened acids derived therefrom are potent inhibitors of the enzyme 3-hydroxy-3-methylglutaryl-coenzyme A reductase (HMG-CoA reductase) and are useful as hypocholesterolemic and hypolipidemic agents.
摘要翻译： 某些反式-6 - [[（取代的）喹啉基]乙基]和乙烯基]四氢-4-羟基吡喃-2-酮及其衍生的相应的二羟基开环酸是3-羟基-3-甲基戊二酰胺的有效抑制剂 辅酶A还原酶（HMG-CoA还原酶），可用作低胆固醇血症和降血脂药。
-
6.发明授权Trans-6-(2-(N-heteroaryl-3,5-disubstituted)pyrazol-4-yl)-ethyl)-or ethenyl)tetrahydro-4-hydroxypyran-2-one inhibitors of cholesterol biosynthesis 失效反式-6-（2-（N-杂芳基-3,5-二取代）吡唑-4-基） - 乙基） - 或乙烯基）四氢-4-羟基吡喃-2-酮胆固醇生物合成抑制剂
公开(公告)号：US4957971A
公开(公告)日：1990-09-18
申请号：US280756
申请日：1988-12-06
IPC分类号： C07D405/14 , C07D409/14 , C07D417/14
CPC分类号： C07D405/14 , C07D409/14 , C07D417/14
摘要： Certain trans-6-[2-(N-heteroaryl-3,5-disubstituted) pyrazol-4-yl)ethyl]- or ethenyl]tetrahydro-4-hydroxy-2H-pyran-2-ones and the corresponding ring-opened acids, esters and N-oxides derived therefrom which are potent inhibitors of the enzyme 3-hydroxy-3-methylglutaryl-coenzyme A reductase (HMG CoA reductase) and are thus useful hypolipidemic or hypocholesterolemic agents. Pharmaceutical compositions containing such compounds, and a method of inhibiting the biosynthesis of cholesterol employing such pharmaceutical compositions are also disclosed.
摘要翻译： 某些反式-6- [2-（N-杂芳基-3,5-二取代）吡唑-4-基）乙基] - 或乙烯基]四氢-4-羟基-2H-吡喃-2-酮和相应的开环 酸，酯和N-氧化物，其是3-羟基-3-甲基戊二酰辅酶A还原酶（HMG CoA还原酶）的有效抑制剂，因此可用于降血脂或降血胆固醇药物。 还公开了含有这些化合物的药物组合物和使用这种药物组合物抑制胆固醇生物合成的方法。
-
7.发明授权5-pyrimidinyl-3,5-dihydroxy-6-heptenoic acid compounds useful as inhibitors of cholesterol biosynthesis 失效可用作胆固醇生物合成抑制剂的5-嘧啶基-3,5-二羟基-6-庚烯酸化合物
公开(公告)号：US4929620A
公开(公告)日：1990-05-29
申请号：US361155
申请日：1989-06-01
IPC分类号： C07D239/26 , C07D405/06
CPC分类号： C07D239/26 , C07D405/06
摘要： Certain trans-6-[[(substituted)pyrimidin-5-yl]-ethyl]- and ethenyl]tetrahydro-4-hydroxypyran-2-ones and the corresponding dihydroxy ring-opened acids derived therefrom are potent inhibitors of the enzyme 3-hydroxy-3-methylglutaryl-coenzyme A reductase (HMG-CoA reductase) and are useful as hypocholesterolemic and hypolipidemic agents.
摘要翻译： 某些反式-6 - [[（取代的）嘧啶-5-基] - 乙基]和乙烯基]四氢-4-羟基吡喃-2-酮和相应的衍生自其的二羟基开环酸是酶3- 羟基-3-甲基戊二酰辅酶A还原酶（HMG-CoA还原酶），可用作低胆固醇血症和降血脂药。
-
8.发明授权6-[[Substituted)pyrimidinyl)ethyl]- and ethenyl]tetrahydro-4-hydroxypyran-2-one inhibitors of cholesterol biosynthesis 失效6 - [[取代的）嘧啶基）乙基]和乙烯基]四氢-4-羟基吡喃-2-酮胆固醇生物合成抑制剂
公开(公告)号：US4868185A
公开(公告)日：1989-09-19
申请号：US130870
申请日：1987-12-10
IPC分类号： C07D239/26 , C07D405/06
CPC分类号： C07D239/26 , C07D405/06
摘要： Certain trans-6-[[(substituted)pyrimidin-5-yl]ethyl]- and ethenyl]tetrahydro-4-hydroxypyran-2-ones and the corresponding dihydroxy ring-opened acids derived therefrom are potent inhibitors of the enzyme 3-hydroxy-3-methylglutaryl-coenzyme A reductase (HMG-CoA reductase) and are useful as hypocholesterolemic and hypolipidemic agents.
摘要翻译： 某些反式-6 - [[（取代的）嘧啶-5-基]乙基]和乙烯基]四氢-4-羟基吡喃-2-酮及其衍生的相应的二羟基开环酸是3-羟基的有效抑制剂 -3-甲基戊二酰辅酶A还原酶（HMG-CoA还原酶），可用作低胆固醇血症和降血脂药。
-
9.发明授权Treating fungal infections with substituted-(6-(tetrahydro-4-hydroxy-2-oxo-2H-pyran-2-yl)ethyl)- or ethenyl)pyrazoles 失效用6-（四氢-4-羟基-2-氧代-2H-吡喃-2-基）乙基） - 或乙烯基）吡唑处理真菌感染
公开(公告)号：US4751229A
公开(公告)日：1988-06-14
申请号：US71672
申请日：1987-07-09
摘要： A method of treating fungal infections in mammals employing 1,3,5-trisubstituted-4- (4-hydroxy-2-oxo-pyran-6-yl)pyrazoles is disclosed.
摘要翻译： 公开了一种使用1,3,5-三取代-4-（4-羟基-2-氧代 - 吡喃-6-基）吡唑治疗哺乳动物真菌感染的方法。
-
10.发明授权Trans-6-[2-[2-(substituted-phenyl)-3- (or 4-) heteroaryl-5-substituted-1H-pyrrol-1-yl]-ethyl]tetrahydro-4-hydroxy-2H-p yran-2-one inhibitors of cholesterol biosynthesis 失效反式-6- [2- [2-（取代的苯基）-3-（或4-）杂芳基-5-取代-1H-吡咯-1-基] - 乙基]四氢-4-羟基-2H-吡喃-2-酮 2-one胆固醇生物合成抑制剂
公开(公告)号：US4735958A
公开(公告)日：1988-04-05
申请号：US944318
申请日：1986-12-22
申请人： Bruce D. Roth , Drago R. Sliskovic
发明人： Bruce D. Roth , Drago R. Sliskovic
IPC分类号： C07D405/14 , A61K31/395 , A61K31/44
CPC分类号： C07D405/14
摘要： Certain trans-6-[2-[2-(substituted-phenyl)-3- (or 4-)heteroaryl-5-substituted-1H-pyrrol-1-yl]ethyl]tetrahydro-4-hydroxy-2H-pyran-2-ones and the corresponding lactone-ring-opened acids are potent inhibitors of the enzyme 3-hydroxy-3-methylglutaryl-coenzyme A reductase (HMG CoA reductase) and are thus useful hypolipidemic or hypocholesterolemic agents. Pharmaceutical compositions containing such compounds, and a method of inhibiting the biosynthesis of cholesterol employing such pharmaceutical compositions are also disclosed.
摘要翻译： 某些反式-6- [2- [2-（取代的 - 苯基）-3-（或4-）杂芳基-5-取代的-1H-吡咯-1-基]乙基]四氢-4-羟基-2H- 2-酮和相应的内酯开环酸是3-羟基-3-甲基戊二酰辅酶A还原酶（HMG CoA还原酶）的有效抑制剂，因此可用于降血脂或降胆固醇。 还公开了含有这些化合物的药物组合物和使用这种药物组合物抑制胆固醇生物合成的方法。
-
-
-
-
-
-
-
-
-
搜索结果
36 条记录 (耗时 0.035 秒)
