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51. 发明授权

US4988711A HMG-CoA reductare-inhibiting N-substituted N-amino-pyrroles 失效
标题翻译： HMG-CoA还原抑制N-取代的N-氨基吡咯
公开(公告)号：US4988711A
公开(公告)日：1991-01-29
申请号：US337001
申请日：1989-04-12
申请人： Rolf Angerbauer , Walter Hubsch , Peter Fey , Hilmar Bischoff , Dieter Petzinna , Delf Schmidt , Gunter Thomas
发明人： Rolf Angerbauer , Walter Hubsch , Peter Fey , Hilmar Bischoff , Dieter Petzinna , Delf Schmidt , Gunter Thomas
IPC分类号： A61K31/40 , A61K31/4427 , A61K31/443 , A61K31/445 , A61K31/55 , A61P3/06 , A61P9/10 , C07D207/50 , C07D401/04 , C07D405/06
CPC分类号： C07D401/04 , C07D207/50
摘要： Inhibiting HMG-CoA reductase, as in treating hyperlipopproteinaemia, lipoproteinaemia and arteriosclerosis, with the new N-substituted N-amino-pyrroles of the formula ##STR1## in which R.sup.1 is an organic radical,R.sup.2 is an aryl or heteroaryl radical,R.sup.3 is a hydrogen or an organic radical,R.sup.4 and R.sup.5 each independently is hydrogen or an organic radical or, together, they complete a heterocylic ring,X is --CH.sub.2 --CH.sub.2 -- or --CH.dbd.CH--,A is ##STR2## R.sup.10 is hydrogen or alkyl, and R.sup.11 is hydrogen, an organic radical or a cation.
摘要翻译：与治疗高脂蛋白血症，脂蛋白血症和动脉硬化的HMG-CoA还原酶一起，其中R1是有机基团的新的N-取代的N-氨基吡咯基，其中R 2是芳基或杂芳基，R 3是氢或有机基团，R 4和R 5各自独立地是氢或有机基团，或者它们一起完成杂环，X是-CH 2 -CH 2 - 或-CH = CH-，A是 R 10是氢或烷基，R 11是氢，有机基或阳离子。

52. 发明授权

US4968689A Certain 2,6-diisopropyl-4-(4-fluoro-phenyl)-3,5-bis-dimethyl-3',5'-dihydroxy-hep t-6-enoate-pyridine derivatives useful for treating lipoproteinaemia and arteriosclerosis 失效
标题翻译：某些用于治疗脂蛋白血症和动脉硬化的2,6-二异丙基-4-（4-氟 - 苯基）-3,5-二 - 二甲基-3'，5'-二羟基 - 庚-6-烯酸 - 吡啶衍生物
公开(公告)号：US4968689A
公开(公告)日：1990-11-06
申请号：US298453
申请日：1989-01-17
申请人： Rolf Angerbauer , Peter Fey , Walter Hubsch , Thomas Philipps , Hilmar Bischoff , Dieter Petzinna , Delf Schmidt , Thomas Gunter
发明人： Rolf Angerbauer , Peter Fey , Walter Hubsch , Thomas Philipps , Hilmar Bischoff , Dieter Petzinna , Delf Schmidt , Thomas Gunter
IPC分类号： C07D333/24 , A61K31/44 , A61K31/4418 , A61K31/443 , A61K31/4433 , A61P3/00 , A61P9/00 , A61P9/10 , C07C69/738 , C07C229/32 , C07C255/14 , C07D213/30 , C07D213/48 , C07D213/54 , C07D213/55 , C07D213/80 , C07D307/54 , C07D401/04 , C07D401/14 , C07D405/04 , C07D405/06 , C07D405/14 , C07D409/04 , C07D409/14 , C07D413/04 , C07D413/14 , C07D417/04 , C07D417/14
CPC分类号： C07D405/04 , C07D213/55 , C07D409/04
摘要： For the treatment of lipoproteinaemia and arteriosclerosis, the new disubstituted pyridines of the formula ##STR1## in which R.sup.1 is optionally substituted aryl or heteroaryl,R.sup.2 is cycloalkyl or optionally substituted alkyl,R.sup.3 is hydrogen, cycloalkyl, or optionally substituted alkyl, aryl or heteroaryl,X is --CH.sub.2 --CH.sub.2 -- or --CH.dbd.CH--,A is ##STR2## R.sup.6 is hydrogen or alkyl, and R.sup.7 is hydrogen, alkyl, aralkyl or a cation.
摘要翻译：对于脂蛋白血症和动脉硬化的治疗，式（I）的新二取代吡啶其中R 1为任选取代的芳基或杂芳基，R 2为环烷基或任选取代的烷基，R 3为氢，环烷基或任选取代的烷基，芳基或杂芳基，X是-CH 2 -CH 2 - 或-CH = CH-，A是R 6是氢或烷基，R 7是氢，烷基，芳烷基或阳离子。

53. 发明授权

US5470982A Disubstituted pyridines 失效
标题翻译：二取代吡啶
公开(公告)号：US5470982A
公开(公告)日：1995-11-28
申请号：US950623
申请日：1992-09-24
申请人： Rolf Angerbauer , Peter Fey , Walter Hubsch , Thomas Philipps , Hilmar Bischoff , Dieter Petzinna , Delf Schmidt , Gunter Thomas
发明人： Rolf Angerbauer , Peter Fey , Walter Hubsch , Thomas Philipps , Hilmar Bischoff , Dieter Petzinna , Delf Schmidt , Gunter Thomas
IPC分类号： C07D213/55 , C07D405/04 , C07D409/04 , C07D405/14
CPC分类号： C07D213/55 , C07D405/04 , C07D409/04
摘要： For the treatment of lipoproteinaemia and arteriosclerosis, the new disubstituted pyridines of the formula ##STR1## in which R.sup.1 is optionally substituted aryl or heteroaryl,R.sup.2 is cycloalkyl or optionally substituted alkyl,R.sup.3 is hydrogen, cycloalkyl, or optionally substituted alkyl, aryl or heteroaryl,X is --CH.sub.2 --CH.sub.2 -- or --CH.dbd.CH--,A is ##STR2## R.sup.6 is hydrogen or alkyl, and R.sup.7 is hydrogen, alkyl, aralkyl or a cation.
摘要翻译：对于脂蛋白血症和动脉硬化的治疗，式（I）的新二取代吡啶其中R 1为任选取代的芳基或杂芳基，R 2为环烷基或任选取代的烷基，R 3为氢，环烷基或任选取代的烷基，芳基或杂芳基，X是-CH 2 -CH 2 - 或-CH = CH-，A是R 6或R 6是氢或烷基，R 7是氢，烷基，芳烷基或阳离子。

54. 发明授权

US5177080A Substituted pyridyl-dihydroxy-heptenoic acid and its salts 失效
标题翻译：取代的吡啶基 - 二羟基庚烯酸及其盐
公开(公告)号：US5177080A
公开(公告)日：1993-01-05
申请号：US798675
申请日：1991-11-26
申请人： Rolf Angerbauer , Peter Fey , Walter Hubsch , Thomas Philipps , Hilmar Bischoff , Dieter Petzinna , Delf Schmidt , Gunter Thomas
发明人： Rolf Angerbauer , Peter Fey , Walter Hubsch , Thomas Philipps , Hilmar Bischoff , Dieter Petzinna , Delf Schmidt , Gunter Thomas
IPC分类号： A61K31/44 , A61K31/4418 , A61P3/06 , A61P9/10 , C07D213/26 , C07D213/30 , C07D213/55 , C07D213/56
CPC分类号： C07D213/30 , C07D213/26 , C07D213/55 , C07D213/56
摘要： Substituted pyridyl-dihydroxy-heptenoic acid of the formula ##STR1## and its salts, if desired in an isomeric form, have a superior inhibitory action on HMG-CoA reductase and thus bring about a surprisingly good lowering of the cholesterol content in the blood.
摘要翻译：如果需要，取代的式（I）的吡啶基 - 二羟基 - 庚烯酸及其盐，如果需要，以异构形式，对HMG-CoA还原酶具有优异的抑制作用，因此导致令人惊奇的降低胆固醇含量血液。

55. 发明授权

US5173495A 7-[(2,6-dialkyl-4-furyl or thienyl-pyridyl)]-3,5-di-(dihydroxy-6-enoates) useful for treating circulatory diseases 失效
标题翻译： 7 - [（2,6-二烷基-4-呋喃基或噻吩基 - 吡啶基）] - 3,5-二 - （二羟基-6-烯酸酯），可用于治疗循环系统疾病
公开(公告)号：US5173495A
公开(公告)日：1992-12-22
申请号：US564502
申请日：1990-08-08
申请人： Rolf Angerbauer , Peter Fey , Walter Hubsch , Thomas Philipps , Hilmar Bischoff , Dieter Petzinna , Delf Schmidt , Gunter Thomas
发明人： Rolf Angerbauer , Peter Fey , Walter Hubsch , Thomas Philipps , Hilmar Bischoff , Dieter Petzinna , Delf Schmidt , Gunter Thomas
IPC分类号： C07D213/55 , C07D405/04 , C07D409/04
CPC分类号： C07D405/04 , C07D213/55 , C07D409/04
摘要： For the treatment of lipoproteinaemia and arteriosclerosis, the polysubstituted pridines of the formula ##STR1## in which R.sup.1 is optionally substituted furyl or thienyl,R.sup.2 is cycloalkyl or optionally substituted alkyl,R.sup.3 is hydrogen, cycloalkyl, or optionally substituted alkyl, aryl or heteroaryl,X is --CH.dbd.CH--,A is ##STR2## R.sup.6 is hydrogen or alkyl, and R.sup.7 is hydrogen, alkyl, aralkyl or a cation.
摘要翻译：为了治疗脂蛋白血症和动脉硬化，式（I）的多取代脯氨酸其中R 1是任选被取代的呋喃基或噻吩基，R2是环烷基或任选取代的烷基，R 3是氢，环烷基或任选取代的烷基，芳基或杂芳基，X是-CH = CH-，A是R6是氢或烷基，R7是氢，烷基，芳烷基或阳离子。

56. 发明授权

US5169857A 7-(polysubstituted pyridyl)-hept-6-endates useful for treating hyperproteinaemia, lipoproteinaemia or arteriosclerosis 失效
标题翻译：可用于治疗高蛋白血症，脂蛋白血症或动脉硬化的7-（多取代吡啶基）-hept-6-末端
公开(公告)号：US5169857A
公开(公告)日：1992-12-08
申请号：US627086
申请日：1990-12-13
申请人： Rolf Angerbauer , Peter Fey , Walter Hubsch , Thomas Philipps , Hilmar Bischoff , Dieter Petzinna , Delf Schmidt , Gunter Thomas
发明人： Rolf Angerbauer , Peter Fey , Walter Hubsch , Thomas Philipps , Hilmar Bischoff , Dieter Petzinna , Delf Schmidt , Gunter Thomas
IPC分类号： C07D213/55 , C07D213/80 , C07D213/82 , C07D213/85 , C07D213/89 , C07D401/06 , C07D401/12 , C07D405/04 , C07D405/06 , C07D405/12 , C07D409/04 , C07D409/06 , C07F7/08 , C07F7/18
CPC分类号： C07D213/80 , C07D213/55 , C07D213/82 , C07D213/85 , C07D213/89 , C07D401/06 , C07D401/12 , C07D405/04 , C07D405/06 , C07D405/12 , C07D409/04 , C07D409/06 , C07F7/0812 , C07F7/0818 , C07F7/1856
摘要： Novel compounds for treating hyperproteinaemia, lipoproteinaemia or arteriosclerosis of the formula ##STR1## in which A, B, D and E can have varied meanings,X is --CH.sub.2 --CH.sub.2 or --CH.dbd.CH--, andR is ##STR2## wherein R.sup.21 denotes hydrogen or alkyl andR.sup.22denotes hydrogen,deontes alkyl, aryl or aralkyl, ordenotes a cation,and their oxidation products.
摘要翻译：用于治疗高蛋白血症，脂蛋白血症或动脉硬化的新型化合物，其中A，B，D和E可以具有不同含义，X是-CH 2 -CH 2或-CH = CH-，R是

57. 发明授权

US5164506A Substituted 2-pyridones and pyrid-2-thiones compounds 失效
标题翻译：取代的2-吡啶酮和吡啶-2-硫酮化合物
公开(公告)号：US5164506A
公开(公告)日：1992-11-17
申请号：US673697
申请日：1991-04-19
申请人： Peter Fey , Rolf Angerbauer , Walter Hubsch , Thomas Philipps , Hilmar Bischoff , Dieter Petzinna , Delf Schmidt , Gunter Thomas
发明人： Peter Fey , Rolf Angerbauer , Walter Hubsch , Thomas Philipps , Hilmar Bischoff , Dieter Petzinna , Delf Schmidt , Gunter Thomas
IPC分类号： C07D211/90 , C07D213/64 , C07D213/70 , C07F7/18
CPC分类号： C07D213/64 , C07D211/90 , C07D213/70 , C07F7/1856
摘要： For inhibiting HMG-CoA reductase and cholesterol synthesis, the novel 2-pyridones and pyrid-2-thiones of the formula ##STR1## in which A is optionally substituted aryl or heterocyclic,B is optionally substituted alkyl, cycloalkyl or aryl,D and E independently are optionally substituted aryl or heterocyclic, H, nitro, cyano, optionally substituted alkyl, alkenyl or imino, amino, alkoxy or acyl, or forms a ring with B,G is O or S,X is --CH.sub.2 --CH.sub.2 -- or --CH.dbd.CH--, andR represents a group of the formula ##STR2## and salts thereof.
摘要翻译：为了抑制HMG-CoA还原酶和胆固醇合成，式（IMAGE）中的新的2-吡啶酮和吡啶-2-硫酮，其中A是任选取代的芳基或杂环，B是任选取代的烷基，环烷基或芳基，D和E 独立地是任选取代的芳基或杂环，H，硝基，氰基，任选取代的烷基，烯基或亚氨基，氨基，烷氧基或酰基，或与B形成环，G是O或S，X是-CH 2 -CH 2 - CH = CH-，R代表下式的基团及其盐。

58. 发明授权

US5034399A Substituted 1,8-naphthyridines and their use in medicaments 失效
标题翻译：取代的1,8-萘啶并用于药物
公开(公告)号：US5034399A
公开(公告)日：1991-07-23
申请号：US496757
申请日：1990-03-21
申请人： Walter Hubsch , Rolf Angerbauer , Peter Fey , Thomas Philipps , Hilmar Bischoff , Dieter Petzinna , Delf Schmidt
发明人： Walter Hubsch , Rolf Angerbauer , Peter Fey , Thomas Philipps , Hilmar Bischoff , Dieter Petzinna , Delf Schmidt
IPC分类号： A61K31/435 , A61P3/06 , A61P9/10 , C07D471/04
CPC分类号： C07D471/04
摘要： Inhibitors of 3-hydrooxy-3-methyl-glutarylcoenzyme A reductase which are 1,8-naphthyridines of the formula ##STR1## in which Arepresents a 3- to 7-membered heterocycle which is optionally substituted, or aryl which is optionally substituted,Brepresents cycloalkyl or alkyl which is optionally substituted, aryl which is optionally substituted,D and E are identical or different andrepresents hydrogen, halogen, mercapto, hydroxyl, alkoxy, alkyl which is optionally substituted, or a group of the formula --NR.sup.1 R.sup.2, aryl, aryloxy or arylthio having 6 to 10 carbon atoms, which is optionally substituted,Yrepresents a group of the formula ##STR2## in which Jdenotes hydrogen, hydroxyl, mercapto or halogen, or alkyl, alkoxy or alkylthio which are optionally substituted, aryloxy, benzyloxy or arylthio or a group of the formula --NR.sup.1 R.sup.2,Zdenotes oxygen or sulphur,Gdenotes hydrogen, alkyl or alkenyl which is optionally substituted,Xrepresents a group of the formula --CH.sub.2 --CH.sub.2 -- or --CH.dbd.CH--,andRrepresents a group of the formula ##STR3## in which R.sup.5denotes hydrogen or alkyl, andR.sup.6denotes hydrogen or alkyl, which may be substituted by phenyl, ordenotes aryl or a cation,and their salts.
摘要翻译：作为式“IMAGE”的1,8-萘啶的3-羟基-3-氧代-3-甲基 - 戊二酰辅酶A还原酶的抑制剂，其中A表示任选取代的3-至7-元杂环，或任选取代的芳基， B代表任选取代的环烷基或烷基，任选取代的芳基，D和E相同或不同，代表氢，卤素，巯基，羟基，烷氧基，任选被取代的烷基，或式-NR1R2的基团，芳基，芳氧基或具有6至10个碳原子的芳硫基，其任选被取代，Y表示下式的基团，其中J表示氢，羟基，巯基或卤素，或任选被取代的烷基，烷氧基或烷硫基，芳氧基，苄氧基或芳硫基或式-NR1R2的基团，Z表示氧或硫，G表示氢，任选被取代的烷基或烯基，X表示式-CH 2 -CH 2 - 或-CH = CH- ，和R 表示式为“IMAGE”的基团，其中R5表示氢或烷基，R6表示氢或可被苯基取代的烷基，或表示芳基或阳离子及其盐。

59. 发明授权

US06277833B1 Substituted triols 失效
标题翻译：取代三醇
公开(公告)号：US06277833B1
公开(公告)日：2001-08-21
申请号：US09160776
申请日：1998-09-24
申请人： Rolf Angerbauer , Peter Fey , Walter Hübsch , Thomas Philipps , Hilmar Bischoff , Hans-Peter Krause , Jörg Petersen von Gehr , Delf Schmidt
发明人： Rolf Angerbauer , Peter Fey , Walter Hübsch , Thomas Philipps , Hilmar Bischoff , Hans-Peter Krause , Jörg Petersen von Gehr , Delf Schmidt
IPC分类号： C07D207333
CPC分类号： C07F9/6561 , C07C33/28 , C07C33/36 , C07C33/38 , C07C69/013 , C07D209/12 , C07F9/3211
摘要： Substituted triols are prepared by reducing appropriately substituted carboxylic esters. The substituted triols can be used as active substances in medicaments.
摘要翻译：取代的三醇通过还原适当取代的羧酸酯来制备。取代的三醇可用作药物中的活性物质。

60. 发明申请

US20140155637A1 CHIRAL SYNTHESIS OF N--1-[2,3-DIHYDROXY-PROPYL]CYCLOPROPANESULFONAMIDES 有权
标题翻译： N-1- [2,3-二羟基丙基]环丙烷磺酰胺的CHIRAL SYNTHESIS
公开(公告)号：US20140155637A1
公开(公告)日：2014-06-05
申请号：US14122568
申请日：2012-05-24
申请人： Peter Fey , Agathe Christine Mayer
发明人： Peter Fey , Agathe Christine Mayer
IPC分类号： C07C303/38 , C07C309/71 , C07D317/24 , C07F7/18 , C07D309/12 , C07D317/18 , C07D303/34
CPC分类号： C07C303/38 , C07B2200/07 , C07C303/40 , C07C309/71 , C07C2601/02 , C07D303/34 , C07D309/12 , C07D317/18 , C07D317/24 , C07F7/1804 , C07C311/28
摘要： The present invention relates to a novel enantioselective method of preparing (S)- and (R)-enantiomers of N-{3,4-difluoro-2-[(2-fluoro-4-iodophenyl)amino]-6-5 methoxyphenyl}-1-[2,3-dihydroxy-propyl]cyclopropanesulfonamide, to novel intermediate compounds, and to the use of said novel intermediate compounds for the preparation of said (S)- and (R)-enantiomers of N-{3,4-difluoro-2-[(2-fluoro-4-iodophenyl)amino]-6-methoxyphenyl}-1-[2,3-dihydroxy-propyl]cyclopropanesulfonamide.
摘要翻译：本发明涉及制备N- {3,4-二氟-2 - [（2-氟-4-碘苯基）氨基] -6-5甲氧基苯基的（S） - 和（R） - 对映异构体的新型对映选择性方法对于新型中间体化合物，以及所述新型中间体化合物用于制备所述（S） - 和（R） - 对映异构体的用途，所述N-（3） - （2,3-二羟基 - 丙基）环丙烷磺酰胺， 4-二氟-2 - [（2-氟-4-碘苯基）氨基] -6-甲氧基苯基} -1- [2,3-二羟基 - 丙基]环丙烷磺酰胺。

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