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1.发明授权N,N-disubstituted arylcycloalkylamines, the salts thereof, pharmaceutical compositions containing these compounds and the use thereof and processes for preparing them 失效N，N-二取代的芳基环烷基胺，其盐，含有这些化合物的药物组合物及其用途及其制备方法
公开(公告)号：US5455273A
公开(公告)日：1995-10-03
申请号：US154644
申请日：1993-11-19
申请人： Roland Maier , Peter Muller , Eberhard Woitun , Rudolf Hurnaus , Michael Mark , Bernhard Eisele , Ralph-Michael Budzinski , Gerhard Hallermayer
发明人： Roland Maier , Peter Muller , Eberhard Woitun , Rudolf Hurnaus , Michael Mark , Bernhard Eisele , Ralph-Michael Budzinski , Gerhard Hallermayer
IPC分类号： A61K31/18 , A61K31/27 , A61P1/16 , A61P3/06 , C07C211/27 , C07C211/35 , C07C233/41 , C07C233/62 , C07C233/79 , C07C237/06 , C07C255/24 , C07C311/07 , C07C311/20 , C07D333/38 , A61K31/165
CPC分类号： C07C311/20 , C07C233/62 , C07C233/79 , C07C237/06 , C07C255/24 , C07C311/07 , C07D333/38 , C07C2101/02 , C07C2101/14 , C07C2102/04 , C07C2102/10
摘要： The invention relates to N,N-disubstituted arylcycloalkylamines of general formula ##STR1## wherein n, m, A, X and R.sup.1 to R.sup.7 are defined as in claim 1, the isomers, isomer mixtures and salts thereof, which have valuable properties, particularly an inhibitory effect on cholesterol biosynthesis.
摘要翻译： 本发明涉及通式为（I）的N，N-二取代的芳基环烷基胺，其中n，m，A，X和R 1至R 7如权利要求1所定义，其异构体，异构体混合物和盐具有有价值的 特性，特别是对胆固醇生物合成的抑制作用。
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2.发明授权Arylidene-1-azacycloalkanes and arylalkyl-1-azacyclo-alkanes, their salts, medicaments containing these compounds and their use, and processes for their preparation 失效亚芳基-1-氮杂环烷烃和芳基烷基-1-氮杂环烷烃，其盐，含有这些化合物的药物及其用途及其制备方法
公开(公告)号：US5466687A
公开(公告)日：1995-11-14
申请号：US218092
申请日：1994-03-25
申请人： Roland Maier , Peter Muller , Eberhard Woitun , Rudolf Hurnaus , Michael Mark , Bernhard Eisele , Ralph-Michael Budzinski , Gerhard Hallermayer
发明人： Roland Maier , Peter Muller , Eberhard Woitun , Rudolf Hurnaus , Michael Mark , Bernhard Eisele , Ralph-Michael Budzinski , Gerhard Hallermayer
IPC分类号： C07D403/10 , C07D413/10 , C07D413/14 , C07D417/10 , A61K31/55 , A61K31/54 , C07D279/06 , C07D405/10
CPC分类号： C07D403/10 , C07D413/10 , C07D413/14 , C07D417/10
摘要： The invention relates to arylidene-1-azacycloalkanes and arylalkyl-1-azacycloalkanes of the general formula ##STR1## (wherein n, m, p, A, W.sup.1, W.sup.2, X, Y, and R.sup.1 to R.sup.11 are as defined in claim 1) and the isomers, isomer mixtures and salts thereof, which have useful properties, in particular an inhibitory effect on cholesterol biosynthesis.
摘要翻译： 本发明涉及通式为（I）（其中n，m，p，A，W 1，W 2，X，Y和R 1至R 11如所定义的亚芳基-1-氮杂环烷烃和芳基烷基-1-氮杂环烷烃 权利要求1）及其异构体，异构体混合物和盐，其具有有用的特性，特别是对胆固醇生物合成的抑制作用。
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3.发明授权O-acyl-4-phenyl-cyclohexanols, their salts, medicaments containing such compounds, and their use, as well as a method of preparing them 失效O-酰基-4-苯基 - 环己醇，其盐，含有这些化合物的药物及其用途，以及制备它们的方法
公开(公告)号：US5962507A
公开(公告)日：1999-10-05
申请号：US986101
申请日：1997-12-05
申请人： Eberhard Woitun , Roland Maier , Peter Muller , Rudolf Hurnaus , Michael Mark , Bernard Eisele , Ralph-Michael Budzinski , Gerhard Hallermayer
发明人： Eberhard Woitun , Roland Maier , Peter Muller , Rudolf Hurnaus , Michael Mark , Bernard Eisele , Ralph-Michael Budzinski , Gerhard Hallermayer
IPC分类号： C07C219/24 , C07C237/06 , C07D295/096 , A01N43/36 , C07D207/04 , C07D211/18 , C07D211/34
CPC分类号： C07D295/096 , C07C219/24 , C07C237/06 , C07C2101/14
摘要： Compounds that inhibit the enzyme 2,3-epoxysqualene-lanosterol-cyclase and cholesterol biosynthesis, of the formula I ##STR1## wherein n denotes the number 0 or 1, m denotes the number 1 or 2, p denotes the number 0 or 1, R.sup.1 and R.sup.2 each denote hydrogen, lower alkyl, alkenyl or alkynyl, which may optionally also be substituted, or together with the nitrogen atom between the denote 5- to 7-membered saturated, monocyclic or heterocyclic rings which may optionally also be interrupted by an oxygen or sulfur atom or by an imino group, R.sup.3, R.sup.4, R.sup.5 and R.sup.6 denote hydrogen or lower alkyl, R.sup.5 additionally denotes lower alkoxy, R.sup.7 denotes hydrogen, cycloalkyl, phenyl or substituted phenyl, naphthyl, tetrahydronaphthyl, thienyl, furyl or pyridyl and A denotes a chemical bond or alkyl, alkenyl having up to 17 carbon atoms.
摘要翻译： 抑制酶-2,3-环氧喹喔啉 - 羊毛甾醇环化酶和胆固醇生物合成的化合物，其中n表示数字0或1，m表示数字1或2，p表示数字0或1，R1和R2 各自表示氢，低级烷基，烯基或炔基，其也可任选地被取代，或与表示5-或7-元饱和的单环或杂环之间的氮原子一起，其也可任选地被氧或硫中断 原子或亚氨基，R3，R4，R5和R6表示氢或低级烷基，R5另外表示低级烷氧基，R7表示氢，环烷基，苯基或取代的苯基，萘基，四氢萘基，噻吩基，呋喃基或吡啶基，A表示 化学键或烷基，具有至多17个碳原子的烯基。
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4.发明授权O-acyl-4-phenyl-cyclohexanols, their salts, medicaments containing such compounds and their use, as well as a method of preparing them 失效O-酰基-4-苯基 - 环己醇，其盐，含有这些化合物的药物及其用途，以及制备它们的方法
公开(公告)号：US5726205A
公开(公告)日：1998-03-10
申请号：US718364
申请日：1997-01-17
申请人： Eberhard Woitun , Roland Maier , Peter Muller , Rudolf Hurnaus , Michael Mark , Bernard Eisele , Ralph-Michael Budzinski , Gerhard Hallermayer
发明人： Eberhard Woitun , Roland Maier , Peter Muller , Rudolf Hurnaus , Michael Mark , Bernard Eisele , Ralph-Michael Budzinski , Gerhard Hallermayer
IPC分类号： A23K1/18 , A23K1/16 , A61K31/215 , A61K31/22 , A61K31/24 , A61K31/335 , A61K31/34 , A61K31/38 , A61K31/40 , A61K31/435 , A61K31/445 , A61K31/4465 , A61K31/455 , A61K31/495 , A61K31/53 , A61K31/535 , A61K31/5375 , A61K31/55 , A61P3/06 , A61P3/10 , A61P9/10 , A61P13/02 , A61P15/00 , A61P31/04 , A61P43/00 , C07C219/24 , C07C219/32 , C07C229/06 , C07C229/08 , C07C237/06 , C07C255/24 , C07C311/06 , C07C311/11 , C07D20060101 , C07D207/08 , C07D213/80 , C07D295/08 , C07D295/096 , C07D307/68 , C07D317/54 , C07D333/40 , A61K31/135
CPC分类号： C07D295/096 , C07C219/24 , C07C237/06 , C07C2101/14
摘要： This document describes O-acyl-4-phenyl-cycloalkanols of general formula I ##STR1## wherein n denotes the number 0 or 1, m denotes the number 1 or 2, p denotes the number 0 or 1, R.sup.1 and R.sup.2 each denote hydrogen, lower alkyl, alkenyl or alkynyl, which may optionally also be substituted, or together with the nitrogen atom between them denote 5- to 7-membered saturated, monocyclic, heterocyclic rings which may optionally also be interrupted by an oxygen or sulphur atom or by an imino group, R.sup.3, R.sup.4, R.sup.5 and R.sup.6 denote hydrogen or lower alkyl, R.sup.5 additionally denotes lower alkoxy, R.sup.7 denotes hydrogen, cycloalkyl, phenyl or substituted phenyl, naphthyl, tetrahydronaphthyl, thienyl, furyl or pyridyl and A denotes a chemical bond or alkyl, alkenyl or alkynyl having up to 17 carbon atoms, and also processes for preparing them, pharmaceutical compositions containing these compounds and the use of these pharmaceutical compositions which intervene in cholesterol biosynthesis. The antihypercholesterolaemic substances can be used for the treatment and prophylaxis of atherosclerosis; they inhibit the enzyme 2,3-epoxysqualene-lanosterol-cyclase.
摘要翻译： PCT No.PCT / EP94 / 01276 Sec。 371日期1997年1月17日 102（e）日期1997年1月17日PCT 1994年4月25日PCT PCT。 公开号WO95 / 29148 日期：1995年11月2日本文件描述了通式I（I）的O-酰基-4-苯基 - 环烷醇，其中n表示数字0或1，m表示数字1或2，p表示数字0或 1，R 1和R 2各自表示氢，低级烷基，烯基或炔基，其可以任选地被取代，或者与它们之间的氮原子一起表示可以任选地被中断的5-至7-元饱和的单环杂环 通过氧或硫原子或亚氨基，R3，R4，R5和R6表示氢或低级烷基，R5另外表示低级烷氧基，R7表示氢，环烷基，苯基或取代的苯基，萘基，四氢萘基，噻吩基，呋喃基或 吡啶基和A表示化学键或具有至多17个碳原子的烷基，烯基或炔基，以及其制备方法，含有这些化合物的药物组合物以及介入胆固醇生物合成的这些药物组合物的用途。 抗高胆固醇血症物质可用于治疗和预防动脉粥样硬化; 它们抑制酶2,3-环氧喹喔啉 - 羊毛甾醇环化酶。
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5.发明授权Benzothiazoles and benzoxazoles, drugs containing them, their use and methods of preparing them 失效苯并噻唑和苯并恶唑，含有它们的药物，其用途和制备方法
公开(公告)号：US5919807A
公开(公告)日：1999-07-06
申请号：US945612
申请日：1997-10-28
申请人： Peter Muller , Rudolph Hurnaus , Roland Maier , Michael Mark , Bernhard Eisele , Ralph-Michael Budzinski , Leo Thomas , Gerhard Hallermayer
发明人： Peter Muller , Rudolph Hurnaus , Roland Maier , Michael Mark , Bernhard Eisele , Ralph-Michael Budzinski , Leo Thomas , Gerhard Hallermayer
IPC分类号： A23K20/137 , A61K31/42 , A61K31/423 , A61K31/425 , A61K31/428 , A61P1/16 , A61P3/06 , A61P3/08 , A61P31/04 , A61P35/00 , C07D263/56 , C07D277/64 , C07D277/66 , C07D277/68 , C07D277/74 , C07D277/76 , C07D277/82 , C07D417/04 , C07D417/12
CPC分类号： C07D263/56 , A23K20/137 , C07D277/64 , C07D277/66 , C07D277/68 , C07D277/74 , C07D277/76 , C07D417/04 , C07D417/12
摘要： The invention relates to benzothiazoles and benzoxazoles of general formula ##STR1## wherein R.sup.1 to R.sup.3, X, Z and n are defined as in claim 1, the enantiomers, diastereomers and salts thereof, particularly the physiologically acceptable acid addition salts thereof which have valuable properties, particularly an inhibitory effect on cholesterol biosynthesis, pharmaceutical compositions containing these compounds, the use thereof and processes for preparing them.
摘要翻译： PCT No.PCT / EP96 / 01827 Sec。 371日期1997年10月28日第 102（e）1997年10月28日PCT PCT 1996年5月2日PCT公布。 公开号WO96 / 35681 日期：1996年11月14日本发明涉及以下通式的苯并噻唑和苯并恶唑：其中R1至R3，X，Z和n如权利要求1所定义，其对映体，非对映异构体及其盐，特别是其生理上可接受的酸加成盐， 有价值的性质，特别是对胆固醇生物合成的抑制作用，含有这些化合物的药物组合物，其用途及其制备方法。
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6.发明授权Urethanes, thio and dithio analogues and their use as inhibitors of cholesterol biosynthesis 有权聚氨酯，硫代和二硫代类似物及其作为胆固醇生物合成抑制剂的用途公开(公告)号：US06346545B1
公开(公告)日：2002-02-12
申请号：US09275318
申请日：1999-03-24
申请人： Roland Maier , Rudolf Hurnaus , Michael Mark , Bernhard Eisele , Peter Mueller , Gebhard Adelgoss , Gebhard Schilcher
发明人： Roland Maier , Rudolf Hurnaus , Michael Mark , Bernhard Eisele , Peter Mueller , Gebhard Adelgoss , Gebhard Schilcher
IPC分类号： A61K3127
CPC分类号： C07D295/135 , C07C271/24 , C07C271/56 , C07C333/06 , C07C333/24 , C07C2601/14 , Y02P20/55
摘要： The present invention relates to urethanes and the thio and dithio analogues thereof of general formula wherein m, n, A, X, Y and R1 to R8 are defined as in claim 1, the enantiomers, diastereomers and the salts thereof, particularly the physiologically acceptable acid addition salts thereof which have valuable properties, particularly an inhibitory effect on cholesterol biosynthesis, pharmaceutical compositions containing these compounds, their use and processes for preparing them.
摘要翻译： 本发明涉及聚氨酯，其一般形式的n，A，X，Y和R 1至R 8的硫代和二硫类似物如权利要求1中所定义，其对映异构体，非对映异构体及其盐，特别是生理上可接受的酸加成 其具有有价值的性质，特别是对胆固醇生物合成的抑制作用，含有这些化合物的药物组合物，其用途和制备方法。
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7.发明授权Urethanes derived from azacycloalkanes, the thio and dithio analogues thereof and their use as cholesterol biosynthesis inhibitors 有权衍生自氮杂环烷烃的聚氨酯，其硫代和二硫类似物及其作为胆固醇生物合成抑制剂的用途公开(公告)号：US06339096B1
公开(公告)日：2002-01-15
申请号：US09275317
申请日：1999-03-24
申请人： Roland Maier , Rudolf Hurnaus , Michael Mark , Bernhard Eisele , Peter Mueller , Gebhard Schilcher , Gebhard Adelgoss
发明人： Roland Maier , Rudolf Hurnaus , Michael Mark , Bernhard Eisele , Peter Mueller , Gebhard Schilcher , Gebhard Adelgoss
IPC分类号： A61K31445
CPC分类号： C07D211/70 , C07D211/26 , C07D211/32 , C07D211/54
摘要： The present invention relates to urethanes derived from azacycloalkanes and the thio and dithio analogues thereof of general formula wherein m, n, A, X, Y, E and R1 to R8 are defined as in claim 1, the enantiomers, diastereomers and the salts thereof, particularly the physiologically acceptable acid addition salts thereof which have valuable properties, particularly an inhibitory effect on cholesterol biosynthesis, pharmaceutical compositions containing these compounds, their use and processes for preparing them.
摘要翻译： 本发明涉及衍生自氮杂环烷烃的氨基甲酸酯及其一般形式的n，A，X，Y，E和R 1至R 8的硫代和二硫代类似物，如权利要求1中所定义，其对映异构体，非对映体及其盐，特别是 其生理上可接受的酸加成盐，其具有有价值的性质，特别是对胆固醇生物合成的抑制作用，含有这些化合物的药物组合物，其用途和制备方法。
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![8-[3-amino-piperidin-1-yl]-xanthines, the preparation thereof and their use as pharmaceutical compositions](/abs-image/US/2012/02/21/US08119648B2/abs.jpg.150x150.jpg)
公开(公告)号：US08119648B2
公开(公告)日：2012-02-21
申请号：US12143219
申请日：2008-06-20
申请人： Frank Himmelsbach , Elke Langkopf , Matthias Eckhardt , Michael Mark , Roland Maier , Ralf Lotz
发明人： Frank Himmelsbach , Elke Langkopf , Matthias Eckhardt , Michael Mark , Roland Maier , Ralf Lotz
IPC分类号： A61P3/10 , A61P3/04 , A61P19/02 , C07D473/06 , C07D519/00 , A61K31/53
CPC分类号： C07D473/04 , C07D473/06 , C07D473/08 , C07D519/00
摘要： The present invention relates to substituted xanthines of general formula wherein R1 to R3 are as defined herein, the tautomers, the stereoisomers, the mixtures, the prodrugs thereof and the salts thereof which have valuable pharmacological properties, particularly an inhibiting effect on the activity of the enzyme dipeptidylpeptidase-IV (DPP-IV).
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9.发明申请Xanthine derivatives, the preparation thereof and their use as pharmaceutical compositions 审中-公开黄嘌呤衍生物，其制备及其作为药物组合物的用途公开(公告)号：US20060205711A1
公开(公告)日：2006-09-14
申请号：US11419756
申请日：2006-05-22
申请人： Frank Himmelsbach , Michael Mark , Matthias Eckhardt , Elke Langkopf , Roland Maier , Ralf Lotz
发明人： Frank Himmelsbach , Michael Mark , Matthias Eckhardt , Elke Langkopf , Roland Maier , Ralf Lotz
IPC分类号： A61K31/55 , A61K31/5377 , A61K31/522 , C07D473/02
CPC分类号： C07D473/08 , C07D473/04 , C07D473/06 , C07D473/10 , C07D473/12
摘要： The present invention relates to substituted xanthines of general formula wherein R1 to R4 are defined as in claim 1, the tautomers and the stereoisomers thereof, mixtures thereof, the prodrugs and the salts thereof which have valuable pharmacological properties, particularly an inhibiting effect on the activity of the enzyme dipeptidylpeptidase-IV (DPP-IV).
摘要翻译： 本发明涉及以下通式的取代黄嘌呤：其中R 1至R 4定义如权利要求1，互变异构体及其立体异构体，其混合物，前药和 其具有有价值的药理学特性的盐，特别是对二肽基肽酶-IV（DPP-IV）的活性的抑制作用。
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![8-[3-AMINO-PIPERIDIN-1-YL]-XANTHINES, THE PREPARATION THEREOF AND THEIR USE AS PHARMACEUTICAL COMPOSITIONS](/abs-image/US/2008/10/09/US20080249089A1/abs.jpg.150x150.jpg)
10.发明申请公开(公告)号：US20080249089A1
公开(公告)日：2008-10-09
申请号：US12143128
申请日：2008-06-20
申请人： Frank Himmelsbach , Elke Langkopf , Matthias Eckhardt , Michael Mark , Roland Maier , Ralf R.H. Lotz , Mohammad Tadayyon
发明人： Frank Himmelsbach , Elke Langkopf , Matthias Eckhardt , Michael Mark , Roland Maier , Ralf R.H. Lotz , Mohammad Tadayyon
IPC分类号： A61K31/5377 , C07D473/04 , A61P3/04 , A61P3/10 , A61K31/522
CPC分类号： C07D473/04 , C07D473/06 , C07D473/08 , C07D519/00
摘要： The present invention relates to substituted xanthines of general formula wherein R1 to R3 are defined as in claims 1 to 16, the tautomers, the stereoisomers, the mixtures, the prodrugs thereof and the salts thereof which have valuable pharmacological properties, particularly an inhibiting effect on the activity of the enzyme dipeptidylpeptidase-IV (DPP-IV).
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