专利快速检索-快速检索全球专利，免费商用专利数据库-IPRDB

1. 发明授权

US5026708A Pyrimidine type mevalonolactones 失效
标题翻译：嘧啶型甲羟戊酸内酯
公开(公告)号：US5026708A
公开(公告)日：1991-06-25
申请号：US243468
申请日：1988-09-12
申请人： Yoshihiro Fujikawa , Mikio Suzuki , Hiroshi Iwasaki , Mitsuaki Sakashita , Masaki Kitahara
发明人： Yoshihiro Fujikawa , Mikio Suzuki , Hiroshi Iwasaki , Mitsuaki Sakashita , Masaki Kitahara
IPC分类号： C07D239/26 , C07D405/06
CPC分类号： C07D239/26 , C07D405/06
摘要： A compound of the formula: ##STR1## wherein R.sup.1 and R.sup.2 are independently hydrogen, C.sub.1-6 alkyl, C.sub.3-6 cycloalkyl, C.sub.1-3 alkoxy, n-butoxy, i-butoxy, sec-butoxy, R.sup.5 R.sup.6 N-- (wherein R.sup.5 and R.sup.6 are independently hydrogen or C.sub.1-3 alkyl), trifluoromethyl, trifluoromethoxy, difluoromethoxy, fluoro, chloro, bromo, phenyl, phenoxy, benzyloxy, hydroxy, trimethylsilyloxy, diphenyl-t-butylsilyloxy, hydroxymethyl or --O(CH.sub.2).sub.l OR.sup.15 (wherein R.sup.15 is hydrogen or C.sub.1-3 alkyl, and l is 1, 2 or 3); or when located at the ortho position to each other, R.sup.1 and R.sup.2 together form --CH.dbd.CH--CH.dbd.CH-- or methylene dioxy; Y is --CH.sub.2 --, --CH.sub.2 CH.sub.2 --, --CH.dbd.CH--, --CH.sub.2 --CH.dbd.CH-- or --CH.dbd.CH--CH.sub.2 --; Z is --Q--CH.sub.2 WCH.sub.2 --CO.sub.2 R.sup.12, ##STR2## (wherein Q is --C(O)--, --C(OR.sup.13).sub.2 -- or --CH(OH)--; W is --C(O)--, --C(OR.sup.13).sub.2 -- or --C(R.sup.11) (OH)--; R.sup.11 is hydrogen or C.sub.1-3 alkyl; R.sup.12 is hydrogen or R.sup.14 (wherein R.sup.14 is physiologically hydrolyzable alkyl or M (wherein M is NH.sub.4, sodium, potassium, 1/2 calcium or a hydrate of lower alkylamine, di-lower alkylamine or tri-lower alkylamine)); two R.sup.13 are independently primary or secondary C.sub.1-6 alkyl; or two R.sup.13 together form --(CH.sub.2).sub.2 -- or --(CH.sub.2).sub.3 --; R.sup.16 and R.sup.17 are independently hydrogen or C.sub.1-3 alkyl; R.sup.3 is hydrogen, C.sub.1-6 alkyl, C.sub.2-3 alkenyl, C.sub.3-6 cycloalkyl, ##STR3## (wherein R.sup.7 is hydrogen, C.sub.1-4 alkyl, C.sub.1-3 alkoxy, fluoro, chloro, bromo or trifluoromethyl), phenyl--(CH.sub.2).sub.m -- (wherein m is 1, 2 or 3), --(CH.sub.2).sub.n CH(CH.sub.3)--phenyl or phenyl--(CH.sub.2).sub.n CH(CH.sub.3)-- (wherein n is 0, 1 or 2): R.sup.4 is C.sub.1-8 alkyl, C.sub.3-7 cycloalkyl, .alpha.- or .beta.-naphthyl, 2--, 3-- or 4-pyridyl, ##STR4## (wherein R.sup.8, R.sup.9 and R.sup.10 are independently hydrogen, C.sub.1-4 alkyl, C.sub.1-8 alkoxy, C.sub.1-3 alkylthio, chloro, bromo, fluoro, --NR.sup.18 R.sup.19 (wherein R.sup.18 and R.sup.19 are independently C.sub.1-3 alkyl), trichloromethyl, trifluoromethyl, trifluoromethoxy, difluoromethoxy, phenoxy, benzyloxy, hydroxy, trimethylsilyloxy, diphenyl-t-butylsilyloxy, hydroxymethyl or --O(CH.sub.2).sub.k OR.sup.20 (wherein R.sup.20 is hydrogen or C.sub.1-3 alkyl, and k is 1, 2 or 3); when R.sup.10 is hydrogen and when located at the ortho position to each other, R.sup.8 and R.sup.9 together form --OC(R.sup.23) (R.sup.24)O-- (wherein R.sup.23 and R.sup.24 are independently hydrogen or C.sub.1-3 alkyl)), ##STR5## (wherein R.sup.25 is hydrogen, C.sub.1-4 alkyl, C.sub.1-3 alkoxy, chloro, bromo, or fluoro) or C.sub.1-3 alkyl substituted by 1 member selected from the group consisting of ##STR6## (wherein R.sup.8, R.sup.9 and R.sup.10 are as defined above) and naphthyl and by 0, 1 or 2 members selected from the group consisting of C.sub.1-8 alkyl.

2. 发明授权

US5137891A 2',3' cyclic fused pyrazolopyrimidine type mevalonolactones 失效
标题翻译： 2'，3'环稠合吡唑并嘧啶型甲羟戊酸内酯
公开(公告)号：US5137891A
公开(公告)日：1992-08-11
申请号：US715456
申请日：1991-06-14
申请人： Yoshihiro Fujikawa , Mikio Suzuki , Hiroshi Iwasaki , Mitsuaki Sakashita , Masaki Kitahara
发明人： Yoshihiro Fujikawa , Mikio Suzuki , Hiroshi Iwasaki , Mitsuaki Sakashita , Masaki Kitahara
IPC分类号： A61K31/505 , A61P3/06 , A61P9/10 , A61P43/00 , C07D487/04
CPC分类号： C07D487/04
摘要： The present invention provides a compound of the formula: ##STR1## process for their production, pharmaceutical compositions containing them and their pharmaceutical uses, and intermediates useful for their production and processes for the production of such intermediates.
摘要翻译：本发明提供下式的化合物：其制备方法，含有它们的药物组合物及其药物用途，以及可用于其生产的中间体和用于生产这种中间体的方法。

3. 发明授权

US5102888A Quinoline type mevalonolactones useful for treating hyperlipidemia and related diseases 失效
标题翻译：适用于治疗高脂血症和相关疾病的喹诺酮类型的美洛酮
公开(公告)号：US5102888A
公开(公告)日：1992-04-07
申请号：US483724
申请日：1990-02-23
申请人： Yoshihiro Fujikawa , Mikio Suzuki , Hiroshi Iwasaki , Mitsuaki Sakashita , Masaki Kitahara
发明人： Yoshihiro Fujikawa , Mikio Suzuki , Hiroshi Iwasaki , Mitsuaki Sakashita , Masaki Kitahara
IPC分类号： A61K31/47 , A61K31/473 , A61P3/06 , A61P7/00 , A61P9/10 , C07D215/12 , C07D215/14 , C07D215/18 , C07D215/20 , C07D215/38 , C07D215/54 , C07D221/06 , C07D405/06 , C07D491/056
CPC分类号： C07D405/06 , C07D215/14 , C07D215/18 , C07D215/20
摘要： A compound of the formula: ##STR1## wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4 and R.sup.6 are independently hydrogen, C.sub.1-6 alkyl, C.sub.1-6 cycloalkyl, C.sub.1-3 alkoxy, n-botoxy, i-botoxy, sec-butoxy, R.sup.7 R.sup.8 N-- (wherein R.sup.7 and R.sup.8 are independently hydrogen or C.sub.1-3 alkyl), trifluoromethyl, trifluoromethoxy, difluoromethoxy, fluoro, chloro, bromo, phenyl, phenoxy, benzyloxy, hydroxy, trimethylsilyloxy, diphenyl-t-butylsilyloxy, hydroxymethyl or --O(CH.sub.2).sub.l OR.sup.19 (wherein R.sup.19 is hydrogen or C.sub.1-3 alkyl, and l is 1,2 or 3); or when located at the ortho position to each other, R.sup.1 and R.sup.2, or R.sup.3 and R.sup.4 together form --CH.dbd.CH--CH.dbd.CH--; or when located at the ortho position to each other, R.sup.1 and R.sup.2 together form --OC(R.sup.15) (R.sup.16)O--(wherein R.sup.15 and R.sup.16 are independently hydrogen or C.sub.1-3 alkyl); Y is --CH.sub.2 --, --CH.sub.2 CH.sub.2 --, --CH.dbd.CH--, --CH.sub.2 --CH.dbd.CH-- or -- CH.dbd.CH--CH.sub.2 --; and Z is --Q--CH.sub.2 WCH.sub.2 --CO.sub.2 R.sup.12, ##STR2## (wherein Q is --C(O)--, --C(OR.sup.13).sub.2 -- or --CH(OH)--; W is --C(O)--, --C(OR.sup.13).sub.2 -- or --C(R.sup.11) (OH)--; R.sup.11 is hydrogen atom or C.sub.1-3 alkyl; R.sup.12 is hydrogen or R.sup.14 (wherein R.sup.14 is physiologically hydrolyzable alkyl or M (wherein M is NH.sub.4, sodium, potassium, 1/2 calcium or a hydrate of lower alkyl amine, di-lower alkyl amine or tri-lower alkyl amine)); two R.sup.13 are independently primary or secondary C.sub.1-6 alkyl; or two R.sup.13 together form --(CH.sub.2).sub.2 -- or --(CH.sub.2).sub.3 ; R.sup.17 and R.sup.18 are independently hydrogen or C.sub.1-3 alkyl; and R.sup.5 is hydrogen, C.sub.1-6 alkyl, C.sub.2-3 alkenyl, C.sub.3-6 cycloalkyl, ##STR3## wherein R.sup.9 is a hydrogen atom, C.sub.1-4 alkyl, C.sub.1-3 alkoxy, fluoro, chloro, bromo or trifluoromethyl), phenyl-(CH.sub.2).sub.m -- (wherein m is 1,2 or 3), --(CH.sub.2).sub.n CH(CH.sub.3)--phenyl or phenyl--(CH.sub.2).sub.n CH(CH.sub.3)-- (wherein n is 0,1 or 2).

4. 发明授权

US5011930A Quinoline type mevalonolactones 失效
标题翻译：喹啉型甲羟戊酸内酯
公开(公告)号：US5011930A
公开(公告)日：1991-04-30
申请号：US483720
申请日：1990-02-23
申请人： Yoshihiro Fujikawa , Mikio Suzuki , Hiroshi Iwasaki , Mitsuaki Sakashita , Masaki Kitahara
发明人： Yoshihiro Fujikawa , Mikio Suzuki , Hiroshi Iwasaki , Mitsuaki Sakashita , Masaki Kitahara
IPC分类号： A61K31/47 , A61K31/473 , A61P3/06 , A61P7/00 , A61P9/10 , C07D215/12 , C07D215/14 , C07D215/18 , C07D215/20 , C07D215/38 , C07D215/54 , C07D221/06 , C07D405/06 , C07D491/056
CPC分类号： C07D405/06 , C07D215/14 , C07D215/18 , C07D215/20
摘要： A compound of the formula: ##STR1## wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4 and R.sup.6 are independently hydrogen, C.sub.1-6 alkyl, C.sub.1-6 cycloalkyl, C.sub.1-3 alkoxy, n-botoxy, i-botoxy, sec-butoxy, R.sup.7 R.sup.8 N-- (wherein R.sup.7 and R.sup.8 are independently hydrogen or C.sub.1-3 alkyl), trifluoromethyl, trifluoromethoxy, difluoromethoxy, fluoro, chloro, bromo, phenyl, phenoxy, benzyloxy, hydroxy, trimethylsilyloxy, diphenyl-t-butylsilyloxy, hydroxymethyl or --O(CH.sub.2).sub.l OR.sup.19 (wherein R.sup.19 is hydrogen or C.sub.1-3 alkyl, and l is 1,2 or 3); or when located at the ortho position to each other, R.sup.1 and R.sup.2, and R.sup.3 and R.sup.4 together form --CH.dbd.CH--CH.dbd.CH--; or when located at the ortho position to each other, R.sup.1 and R.sup.2 together form --OC(R.sup.15)(R.sup.16)O-- (wherein R.sup.15 and R.sup.16 are independently hydrogen or C.sub.1-3 alkyl); Y is --CH.sub.2 --, --CH.sub.2 CH.sub.2 --, --CH.dbd.CH--, --CH.sub.2 CH.dbd.CH-- or --CH.dbd.CH-- CH.sub.2 --; and Z is --Q--CH.sub.2 WCH.sub.2 --CO.sub.2 R.sup.12, ##STR2## (wherein Q is --C(O)--, --C(OR.sup.13).sub.2 -- or --CH(OH)--; W is --C(O)--, --C(OR.sup.13).sub.2 -- or --C(R.sup.11)(OH)--; R.sup.11 is hydrogen atom or C.sub.1-3 alkyl; R.sup.12 is hydrogen or R.sup.14 (wherein R.sup.14 is physiologically hydrolyzable alkyl or M (wherein M is NH.sub.4, sodium, potassium, 1/2 calcium or a hydrate of lower alkyl amine, di-lower alkyl amine or tri-lower alkyl amine)); two R.sup.13 are independently primary or secondary C.sub.1-6 alkyl; or two R.sup.13 together form --(CH.sub.2).sub.2 -- or --(CH.sub.2).sub.3 ; R.sup.17 and R.sup.18 are independently hydrogen or C.sub.1-3 alkyl; and R.sup.5 is hydrogen, C.sub.1-6 alkyl, C.sub.2-3 alkenyl, C.sub.3-6 cycloalkyl, ##STR3## (wherein R.sup.9 is a hydrogen atom, C.sub.1-4 alkyl, C.sub.1-3 alkoxy, fluoro, chloro, bromo or trifluoromethyl), phenyl-(CH.sub.2).sub.m -- (wherein m is 1,2 or 3), --(CH.sub.2).sub.n CH(CH.sub.3)-phenyl or phenyl-(CH.sub.2).sub.n CH(CH.sub.3)-- (wherein n is 0,1 or 2).
摘要翻译：下式的化合物：其中R 1，R 2，R 3，R 4和R 6独立地是氢，C 1-6烷基，C 1-6环烷基，C 1-3烷氧基，正丁氧基，异丁氧基，仲丁氧基，丁氧基，R7R8N-（其中R7和R8独立地是氢或C1-3烷基），三氟甲基，三氟甲氧基，二氟甲氧基，氟，氯，溴，苯基，苯氧基，苄氧基，羟基，三甲基甲硅烷氧基，二苯基叔丁基甲硅烷氧基，羟甲基或 - O（CH 2）lOR 19（其中R 19是氢或C 1-3烷基，且l是1,2或3）; 或当位于彼此的邻位时，R1和R2以及R3和R4一起形成-CH = CH-CH = CH-; 或者当位于彼此的邻位时，R 1和R 2一起形成-OC（R 15）（R 16）O-（其中R 15和R 16独立地是氢或C 1-3烷基）; Y是-CH 2 - ， - CH 2 CH 2 - ， - CH = CH - ， - CH 2 CH = CH-或-CH = CH-CH 2 - ; （其中Q为-C（O） - ， - C（OR 13）2 - 或-CH（OH） - ）; W为-C（O） - （CH 2），-C（OR 13）2 - 或-C（R 11）（OH） - ; R 11为氢原子或C 1-3烷基; R 12为氢或R 14（其中R 14为生理上可水解的烷基或M（其中M为NH 4，钠，二价低级烷基胺或三低级烷基胺的水合物））;两个R 13独立地为伯或仲C 1-6烷基;或两个R 13一起形成 - （CH 2） 2-或 - （CH 2）3; R 17和R 18独立地是氢或C 1-3烷基;且R 5是氢，C 1-6烷基，C 2-3烯基，C 3-6环烷基，其中R 9是氢苯基 - （CH 2）m - （其中m为1,2或3）， - （CH 2）n CH（CH 3） - 苯基或（C 1 -C 4）烷基，C 1-4烷氧基，氟，氯，溴或三氟甲基）苯基 - （CH 2）n CH（CH 3） - （其中n为0,1或2）。

5. 发明授权

US4977161A Isoxazolopyridine type mevalonolactones 失效
标题翻译：异恶唑吡啶型甲羟戊酸内酯
公开(公告)号：US4977161A
公开(公告)日：1990-12-11
申请号：US434254
申请日：1989-11-13
申请人： Yoshihiro Fujikawa , Mikio Suzuki , Hiroshi Iwasaki , Mitsuaki Sakashita , Masaki Kitahara
发明人： Yoshihiro Fujikawa , Mikio Suzuki , Hiroshi Iwasaki , Mitsuaki Sakashita , Masaki Kitahara
IPC分类号： A61K31/445 , A61P3/08 , A61P9/10 , C07D498/04
CPC分类号： C07D498/04
摘要： The present invention provides a compound of the formula: ##STR1## process for their production, pharmaceutical compositions containing them and their pharmaceutical uses, and intermediates useful for their production and processes for the production of such intermediates. The compounds are used as anti-hyperlipoproteinemic agents for example.

6. 发明授权

US5872130A Quinoline type mevalonoactones 失效
标题翻译：喹啉型甲羟戊酸酯
公开(公告)号：US5872130A
公开(公告)日：1999-02-16
申请号：US631092
申请日：1990-12-19
申请人： Yoshihiro Fujikawa , Mikio Suzuki , Hiroshi Iwasaki , Mitsuaki Sakashita , Masaki Kitahara
发明人： Yoshihiro Fujikawa , Mikio Suzuki , Hiroshi Iwasaki , Mitsuaki Sakashita , Masaki Kitahara
IPC分类号： A61K31/47 , A61K31/473 , A61P3/06 , A61P7/00 , A61P9/10 , C07D215/12 , C07D215/14 , C07D215/18 , C07D215/20 , C07D215/38 , C07D215/54 , C07D221/06 , C07D405/06 , C07D491/056
CPC分类号： C07D405/06 , C07D215/14 , C07D215/18 , C07D215/20
摘要： Described herein are mevalonolactone derivatives having a quinoline ring of formula (I) ##STR1## wherein the R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, Y and Z variables are described therein.
摘要翻译：本文描述了具有式（I）喹啉环的甲羟戊酸内酯衍生物，其中R1，R2，R3，R4，R5，Y和Z的变量在此描述。

7. 发明授权

US5854259A Quinoline type mevalonolactones 失效
标题翻译：喹啉型甲羟戊酸内酯
公开(公告)号：US5854259A
公开(公告)日：1998-12-29
申请号：US978884
申请日：1992-11-19
申请人： Yoshihiro Fujikawa , Mikio Suzuki , Hiroshi Iwasaki , Mitsuaki Sakashita , Masaki Kitahara
发明人： Yoshihiro Fujikawa , Mikio Suzuki , Hiroshi Iwasaki , Mitsuaki Sakashita , Masaki Kitahara
IPC分类号： C07D215/14 , C07D215/18 , C07D215/20 , C07D405/06 , A61K31/47 , C07D215/12
CPC分类号： C07D405/06 , C07D215/14 , C07D215/18 , C07D215/20
摘要： Described herein are mevalonolactone derivatives having a quinoline ring of formula (I) ##STR1## wherein the R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, Y and Z variables are described therein.
摘要翻译：本文描述了具有式（I）喹啉环的甲羟戊酸内酯衍生物，其中R1，R2，R3，R4，R5，Y和Z的变量在此描述。

8. 发明授权

US5026698A Thienopyridine type mevalonolactones 失效
标题翻译：噻吩并吡啶型甲羟戊酸内酯
公开(公告)号：US5026698A
公开(公告)日：1991-06-25
申请号：US423956
申请日：1989-10-19
申请人： Yoshihiro Fujikawa , Mikio Suzuki , Hiroshi Iwasaki , Mitsuaki Sakashita , Masaki Kitahara
发明人： Yoshihiro Fujikawa , Mikio Suzuki , Hiroshi Iwasaki , Mitsuaki Sakashita , Masaki Kitahara
IPC分类号： A61K31/44 , C07D495/04
CPC分类号： C07D495/04
摘要： The present invention provides a compound of the formula: ##STR1## process for their production, pharmaceutical compositions containing them and their pharmaceutical uses, and intermediates useful for their production and processes for the production of such intermediates.

9. 发明授权

US5856336A Quinoline type mevalonolactones 失效
标题翻译：喹啉型甲羟戊酸内酯
公开(公告)号：US5856336A
公开(公告)日：1999-01-05
申请号：US883398
申请日：1992-05-15
申请人： Yoshihiro Fujikawa , Mikio Suzuki , Hiroshi Iwasaki , Mitsuaki Sakashita , Masaki Kitahara
发明人： Yoshihiro Fujikawa , Mikio Suzuki , Hiroshi Iwasaki , Mitsuaki Sakashita , Masaki Kitahara
IPC分类号： A61K31/47 , A61K31/473 , A61P3/06 , A61P7/00 , A61P9/10 , C07D215/12 , C07D215/14 , C07D215/18 , C07D215/20 , C07D215/38 , C07D215/54 , C07D221/06 , C07D405/06 , C07D491/056
CPC分类号： C07D405/06 , C07D215/14 , C07D215/18 , C07D215/20
摘要： A compound of the formula ##STR1## Z=--CH(OH)--CH.sub.2 --CH(OH)--CH.sub.2 --COO.1/2Ca have HMG--CoA inhibiting effects, making them useful as inhibitors of cholesterol biosynthesis. The compound may be prepared as a pharmaceutical for reducing hyperlipidemia, hyperlipoproteinemia or atherosclerosis.
摘要翻译：具有下式的化合物[A] Z = -CH（OH）-CH 2 -CH（OH）-CH 2 COO + E，fra 1/2 + EE Ca具有HMG-CoA抑制作用，使其有用作为胆固醇生物合成的抑制剂。该化合物可以制备为用于降低高脂血症，高脂蛋白血症或动脉粥样硬化的药物。

10. 发明授权

US5055472A Pyrazolopyrimidine type mevalonolactones 失效
标题翻译：吡唑并嘧啶类型的异戊二烯
公开(公告)号：US5055472A
公开(公告)日：1991-10-08
申请号：US426156
申请日：1989-10-25
申请人： Yoshihiro Fujikawa , Mikio Suzuki , Hiroshi Iwasaki , Mitsuaki Sakashita , Masaki Kitahara
发明人： Yoshihiro Fujikawa , Mikio Suzuki , Hiroshi Iwasaki , Mitsuaki Sakashita , Masaki Kitahara
IPC分类号： A61K31/505 , A61P3/06 , A61P9/10 , A61P43/00 , C07D487/04
CPC分类号： C07D487/04
摘要： The present invention provides a compound of the formula: ##STR1## process for their production, pharmaceutical compositions containing them and their pharmaceutical uses, and intermediates useful for their production and processes for the production of such intermediates.

你已经成功收藏专利！

检索式保存成功!

IPRDB

热门服务

关于我们

友情链接

联系方式