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1. 发明授权

US5646144A 1-acylpiperidine compounds 失效
标题翻译： 1-酰基哌啶化合物
公开(公告)号：US5646144A
公开(公告)日：1997-07-08
申请号：US482704
申请日：1995-06-07
申请人： Walter Schilling , Silvio Ofner , Siem J. Veenstra
发明人： Walter Schilling , Silvio Ofner , Siem J. Veenstra
IPC分类号： C07D211/26 , A61K31/4427 , A61K31/443 , A61K31/4433 , A61K31/445 , A61K31/451 , A61K31/452 , A61K31/4523 , A61K31/4525 , A61K31/4535 , A61K31/454 , A61K31/47 , A61K31/4709 , A61P1/00 , A61P11/08 , A61P25/00 , A61P25/04 , A61P25/18 , A61P25/20 , A61P25/24 , A61P25/26 , A61P27/02 , A61P29/00 , A61P43/00 , C07D20060101 , C07D211/58 , C07D401/06 , C07D401/12 , C07D401/14 , C07D405/12 , C07D409/12 , C07D471/04 , C07D215/12 , C07D409/00
CPC分类号： C07D401/12 , C07D211/58 , C07D401/14 , C07D405/12 , C07D409/12 , C07D471/04
摘要： 1-Acylpiperidine compound of the formula I ##STR1## in which R.sub.1 is an optionally substituted aralkyl, aryloxyalkyl, heteroaralkyl, aroyl, heteroaroyl, cycloalkylcarbonyl, aralkanoyl, heteroarylalkanoyl, aralkoxycarbonyl or arylcarbamoyl radical or the acyl radical of an .alpha.-amino acid which is optionally N-substituted by lower alkanoyl or carbamoyl-lower-alkanoyl, R.sub.2 is cycloalkyl or an optionally substituted aryl or heteroaryl radical, R.sub.3 is hydrogen, alkyl, carbamoyl or an alkanoyl or alkenoyl radical which is optionally substituted by carboxyl or esterified or amidated carboxyl, R.sub.4 is an optionally substituted aryl or optionally partially hydrogenated heteroaryl radical, X.sub.1 is methylene, ethylene, a direct linkage, an optionally ketalized carbonyl group or an optionally etherified hydroxymethylene group, X.sub.2 is alkylene, carbonyl or a direct linkage, and X.sub.3 is carbonyl, oxo-lower-alkylene, oxo(aza)-lower-alkylene or an alkylene radical which is optionally substituted by phenyl, hydroxymethyl, optionally esterified or amidated carboxyl or, in higher than the .alpha. position, by hydroxyl, and its salts have substance-P-antagonistic properties and can be used as pharmaceutically active substances in pharmaceuticals for the treatment of disorders in whose development substance P plays an essential part.
摘要翻译：式I的1-酰基哌啶化合物其中R 1是任选取代的芳烷基，芳氧基烷基，杂芳烷基，芳酰基，杂芳酰基，环烷基羰基，芳烷酰基，杂芳基烷酰基，芳烷氧基羰基或芳基氨基甲酰基或α-氨基的酰基酸，其任选被低级烷酰基或氨基甲酰基 - 低级 - 烷酰基N-取代，R 2是环烷基或任选取代的芳基或杂芳基，R 3是氢，烷基，氨基甲酰基或任选被羧基或酯化的烷酰基或烯酰基或酰胺化的羧基，R 4是任选取代的芳基或任选部分氢化的杂芳基，X 1是亚甲基，亚乙基，直接连接，任意缩醛化的羰基或任选醚化的羟基亚甲基，X 2是亚烷基，羰基或直链， X 3是羰基，氧代 - 低级 - 亚烷基，氧代（氮杂） - 低级 - 亚烷基或任选被苯基取代的亚烷基，羟甲基，任选酯化或酰胺化的羧基，或高于α位置的羟基，其盐具有物质P-拮抗性质，可用作药物中的药物活性物质，用于治疗其发育物质P所起的障碍一个重要的部分。

2. 发明授权

US5310743A 1-acylpiperidine compounds 失效
标题翻译： 1-酰基哌啶化合物
公开(公告)号：US5310743A
公开(公告)日：1994-05-10
申请号：US929186
申请日：1992-08-11
申请人： Walter Schilling , Silvio Ofner , Siem J. Veenstra
发明人： Walter Schilling , Silvio Ofner , Siem J. Veenstra
IPC分类号： C07D211/26 , A61K31/4427 , A61K31/443 , A61K31/4433 , A61K31/445 , A61K31/451 , A61K31/452 , A61K31/4523 , A61K31/4525 , A61K31/4535 , A61K31/454 , A61K31/47 , A61K31/4709 , A61P1/00 , A61P11/08 , A61P25/00 , A61P25/04 , A61P25/18 , A61P25/20 , A61P25/24 , A61P25/26 , A61P27/02 , A61P29/00 , A61P43/00 , C07D20060101 , C07D211/58 , C07D401/06 , C07D401/12 , C07D401/14 , C07D405/12 , C07D409/12 , C07D471/04 , C07D215/12 , A01N43/42 , C07D215/16
CPC分类号： C07D401/12 , C07D211/58 , C07D401/14 , C07D405/12 , C07D409/12 , C07D471/04
摘要： 1-Acylpiperidine compound of the formula I ##STR1## in which R.sub.1 is an optionally substituted aralkyl, aryloxyalkyl, heteroaralkyl, aroyl, heteroaroyl, cycloalkylcarbonyl, aralkanoyl, heteroarylalkanoyl, aralkoxycarbonyl or arylcarbamoyl radical or the acyl radical of an .alpha.-amino acid which is optionally N-substituted by lower alkanoyl or carbamoyl-lower-alkanoyl, R.sub.2 is cycloalkyl or an optionally substituted aryl or heteroaryl radical, R.sub.3 is hydrogen, alkyl, carbamoyl or an alkanoyl or alkenoyl radical which is optionally substituted by carboxyl or esterified or amidated carboxyl, R.sub.4 is an optionally substituted aryl or optionally partially hydrogenated heteroaryl radical, X.sub.1 is methylene, ethylene, a direct linkage, an optionally ketalised carbonyl group or an optionally etherified hydroxymethylene group, X.sub.2 is alkylene, carbonyl or a direct linkage, and X.sub.3 is carbonyl, oxo-lower-alkylene, oxo(aza)-lower-alkylene or an alkylene radical which is optionally substituted by phenyl, hydroxymethyl, optionally esterified or amidated carboxyl or, in higher than the .alpha. position, by hydroxyl, and its salts have substance-P-antagonistic properties and can be used as pharmaceutically active substances in pharmaceuticals for the treatment of disorders in whose development substance P plays an essential part.
摘要翻译：式I的1-酰基哌啶化合物其中R 1是任选取代的芳烷基，芳氧基烷基，杂芳烷基，芳酰基，杂芳酰基，环烷基羰基，芳烷酰基，杂芳基烷酰基，芳烷氧基羰基或芳基氨基甲酰基或α-氨基的酰基酸，其任选被低级烷酰基或氨基甲酰基 - 低级 - 烷酰基N-取代，R 2是环烷基或任选取代的芳基或杂芳基，R 3是氢，烷基，氨基甲酰基或任选被羧基或酯化的烷酰基或烯酰基或酰胺化的羧基，R 4是任选取代的芳基或任选部分氢化的杂芳基，X 1是亚甲基，亚乙基，直链，任选的缩酮化羰基或任选醚化的羟基亚甲基，X 2是亚烷基，羰基或直链， X 3是羰基，氧代 - 低级 - 亚烷基，氧代（氮杂） - 低级 - 亚烷基或任选被苯基取代的亚烷基，羟甲基，任选酯化或酰胺化的羧基，或高于α位置的羟基，其盐具有物质P-拮抗性质，可用作药物中的药物活性物质，用于治疗其发育物质P所起的障碍一个重要的部分。

3. 发明授权

US5604247A Chromone Derivatives 失效
标题翻译：色酮衍生物
公开(公告)号：US5604247A
公开(公告)日：1997-02-18
申请号：US632971
申请日：1996-04-16
申请人： Andreas Von Sprecher , Marc Gerspacher , Robert Mah , Silvio Roggo , Walter Schilling , Silvio Ofner , Siem J. Veenstra
发明人： Andreas Von Sprecher , Marc Gerspacher , Robert Mah , Silvio Roggo , Walter Schilling , Silvio Ofner , Siem J. Veenstra
IPC分类号： A61K31/352 , A61K31/4402 , A61K31/443 , A61K31/445 , A61K31/4468 , A61P1/00 , A61P1/08 , A61P1/12 , A61P3/12 , A61P9/00 , A61P9/08 , A61P9/12 , A61P11/00 , A61P11/06 , A61P11/08 , A61P25/00 , A61P25/04 , A61P25/08 , A61P25/20 , A61P25/24 , A61P25/26 , A61P29/00 , A61P35/00 , A61P37/00 , A61P37/08 , A61P43/00 , C07D405/12 , G07D405/12
CPC分类号： C07D405/12
摘要： Compounds of formula I ##STR1## wherein rings A and B are as defined in the specification, have valuable pharmacological properties and are particularly effective as NK1 antagonists and substance P antagonists. Said compounds are prepared in a manner known per se.
摘要翻译：其中环A和B如说明书中所定义的式I的化合物具有有价值的药理学性质，并且作为NK1拮抗剂和P物质拮抗剂是特别有效的。所述化合物以本身已知的方式制备。

4. 发明授权

US5541195A 1-acylpiperidine compounds 失效
标题翻译： 1-酰基哌啶化合物
公开(公告)号：US5541195A
公开(公告)日：1996-07-30
申请号：US196360
申请日：1994-04-04
申请人： Walter Schilling , Silvio Ofner , Siem J. Veenstra
发明人： Walter Schilling , Silvio Ofner , Siem J. Veenstra
IPC分类号： C07D211/26 , A61K31/4427 , A61K31/443 , A61K31/4433 , A61K31/445 , A61K31/451 , A61K31/452 , A61K31/4523 , A61K31/4525 , A61K31/4535 , A61K31/454 , A61K31/47 , A61K31/4709 , A61P1/00 , A61P11/08 , A61P25/00 , A61P25/04 , A61P25/18 , A61P25/20 , A61P25/24 , A61P25/26 , A61P27/02 , A61P29/00 , A61P43/00 , C07D20060101 , C07D211/58 , C07D401/06 , C07D401/12 , C07D401/14 , C07D405/12 , C07D409/12 , C07D471/04 , C07D215/12 , C07D409/00
CPC分类号： C07D401/12 , C07D211/58 , C07D401/14 , C07D405/12 , C07D409/12 , C07D471/04
摘要： 1-Acylpiperidine compound of the formula I ##STR1## in which R.sub.1 is an optionally substituted aralkyl, aryloxyalkyl, heteroaralkyl, aroyl, heteroaroyl, cycloalkylcarbonyl, aralkanoyl, heteroarylalkanoyl, aralkoxycarbonyl or arylcarbamoyl radical or the acyl radical of an .alpha.-amino acid which is optionally N-substituted by lower alkanoyl or carbamoyl-lower-alkanoyl, R.sub.2 is cycloalkyl or an optionally substituted aryl or heteroaryl radical, R.sub.3 is hydrogen, alkyl, carbamoyl or an alkanoyl or alkenoyl radical which is optionally substituted by carboxyl or esterified or amidated carboxyl, R.sub.4 is an optionally substituted aryl or optionally partially hydrogenated heteroaryl radical, X.sub.1 is methylene, ethylene, a direct linkage, an optionally ketalised carbonyl group or an optionally etherified hydroxymethylene group, X.sub.2 is alkylene, carbonyl or a direct linkage, and X.sub.3 is carbonyl, oxo-lower-alkylene, oxo(aza)-lower-alkylene or an alkylene radical which is optionally substituted by phenyl, hydroxymethyl, optionally esterified or amidated carboxyl or, in higher than the .alpha. position, by hydroxyl, and its salts have substance-P-antagonistic properties and can be used as pharmaceutically active substances in pharmaceuticals for the treatment of disorders in whose development substance P plays an essential part.
摘要翻译：式I的1-酰基哌啶化合物其中R 1是任选取代的芳烷基，芳氧基烷基，杂芳烷基，芳酰基，杂芳酰基，环烷基羰基，芳烷酰基，杂芳基烷酰基，芳烷氧基羰基或芳基氨基甲酰基或α-氨基的酰基酸，其任选被低级烷酰基或氨基甲酰基 - 低级 - 烷酰基N-取代，R 2是环烷基或任选取代的芳基或杂芳基，R 3是氢，烷基，氨基甲酰基或任选被羧基或酯化的烷酰基或烯酰基或酰胺化的羧基，R 4是任选取代的芳基或任选部分氢化的杂芳基，X 1是亚甲基，亚乙基，直链，任选的缩酮化羰基或任选醚化的羟基亚甲基，X 2是亚烷基，羰基或直链， X 3是羰基，氧代 - 低级 - 亚烷基，氧代（氮杂） - 低级 - 亚烷基或任选被苯基取代的亚烷基，羟甲基，任选酯化或酰胺化的羧基，或高于α位置的羟基，其盐具有物质P-拮抗性质，可用作药物中的药物活性物质，用于治疗其发育物质P所起的障碍一个重要的部分。

5. 发明授权

US5180718A Acyl derivatives of oxazolorifamycins 失效
标题翻译：恶唑菌素的酰基衍生物
公开(公告)号：US5180718A
公开(公告)日：1993-01-19
申请号：US718894
申请日：1991-06-21
申请人： Wilhelm Kump , Christian Borel , Jen Chen , Siem J. Veenstra , John Francis , Benjamin B. Mugrage
发明人： Wilhelm Kump , Christian Borel , Jen Chen , Siem J. Veenstra , John Francis , Benjamin B. Mugrage
IPC分类号： C07D498/18
CPC分类号： C07D498/18
摘要： The invention relates to novel acyl derivatives of rifamycins of the formula ##STR1## and the salts thereof, in which the structural elements --A.sub.1 --A.sub.2 --, --A.sub.3 --A.sub.4 -- and --A.sub.5 --A.sub.6 -- each denote ethylene or vinylene or the elements --A.sub.1 --A.sub.2 -- and --A.sub.3 --A.sub.4 -- each denote ethylene and --A.sub.5 --A.sub.6 -- denotes vinylene; X represents >C(R.sub.6)-- or >N-- and R.sub.6 denotes hydrogen or alkyl; alk denotes an aliphatic hydrocarbon radical; R.sub.1 denotes hydrogen or acyl; R.sub.2 denotes acyl, or alkyl which is optionally substituted by an aromatic radical, and R.sub.3 and R.sub.3 ' represent a common bond, or R.sub.3 denotes hydrogen or acyl, and R.sub.3 ' is hydrogen; R.sub.4 denotes hydrogen, cycloalkyl or aryl; R.sub.5 denotes hydrogen or acetyl; R.sub.7 denotes hydrogen or alkyl, which can be used as active compounds in medicaments, the preparation and use thereof, and pharmaceutical products and the preparation thereof.
摘要翻译：本发明涉及式（I）的利福霉素的新型酰基衍生物及其盐，其中结构单元-A1-A2-，-A3-A4-和-A5-A6各自表示乙烯或亚乙烯基或元素-A1-A2-和-A3-A4-各自表示亚乙基，-A5-A6-表示亚乙烯基; X表示> C（R6） - 或> N-，R6表示氢或烷基; alk表示脂族烃基; R1表示氢或酰基; R 2表示酰基或任选被芳族基团取代的烷基，R 3和R 3'表示共同的键，或R 3表示氢或酰基，且R 3'是氢; R4表示氢，环烷基或芳基; R5表示氢或乙酰基; R7表示氢或烷基，其可用作药物中的活性化合物，其制备和用途，以及药物及其制备。

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