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    1-acylpiperidine compounds
    4.
    发明授权
    1-acylpiperidine compounds 失效
    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。

    1-acylpiperidine compounds
    5.
    发明授权
    1-acylpiperidine compounds 失效
    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。

    1-acylpiperidine compounds
    6.
    发明授权
    1-acylpiperidine compounds 失效
    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。

    Benzofuranyl-tetrahydropyridines and -piperidines, their acid addition salts and antidepressant preparations thereof
    9.
    发明授权
    Benzofuranyl-tetrahydropyridines and -piperidines, their acid addition salts and antidepressant preparations thereof 失效
    苯并呋喃基 - 四氢吡啶和哌啶，它们的酸加成盐和抗抑郁药制剂

    公开(公告)号：US4259338A

    公开(公告)日：1981-03-31

    申请号：US140405

    申请日：1980-04-14

    申请人： Romeo Paioni ,  Walter Schilling ,  Raymond Bernasconi

    发明人： Romeo Paioni ,  Walter Schilling ,  Raymond Bernasconi

    IPC分类号： C07D405/04 ,  A61K31/443 ,  A61K31/445 ,  A61P25/24 ,  A61P25/26 ,  C07D307/79 ,  C07D307/86 ,  C07D307/91 ,  A61K31/44 ,  C07D405/02

    CPC分类号： C07D307/79 ,  C07D307/86 ,  C07D307/91

    摘要： The present invention provides new benzofuranyl-tetrahydropyridines and -piperidines of the general formula I ##STR1## in which R.sub.1 and R.sub.2 independently of one another are hydrogen or lower alkyl or together are lower alkylene, R.sub.3 is hydrogen, lower alkyl, lower alkenyl, lower alkynyl, cyclo-lower alkyl or cyclo-lower alkyl-lower alkyl and Y.sub.1 and Y.sub.2 are each hydrogen or together are an additional bond, and the ring A is not further substituted or is further substituted by lower alkyl, lower alkoxy, halogen with an atomic number not more than 35, cyano or hydroxyl and the pharmaceutically acceptable acid addition salts thereof, and antidepressant preparations containing these compounds. The compounds according to the invention have valuable pharmacological properties. In particular, they inhibit the absorption of serotonin by mesencephalic synaptosomes, the serotonin depletion induced in the brain of rats by H 75/12, the absorption of noradrenalin by mesencephalic synaptosomes in rats and the noradrenalin depletion induced in the brain of rats by H 77/77. In the same dosage they also effect inhibition of monoamino-oxidase in the brain of rats and in the liver of rats. Furthermore, they intensify the "head twitch" induced by 5-hydroxy-tryptophan, and are distinguished by good tolerance. The compounds of the general formula I and their pharmaceutically acceptable acid addition salts can therefore be used as psychopharmaceuticals and in particular as antidepressants.

    摘要翻译： 本发明提供了通式Ⅰ（I）的新的苯并呋喃基 - 四氢吡啶和哌啶，其中R 1和R 2彼此独立地是氢或低级烷基或一起是低级亚烷基，R 3是氢，低级烷基，低级 烯基，低级炔基，环低级烷基或环低级烷基 - 低级烷基，Y 1和Y 2各自为氢或一起为附加键，并且环A不被进一步取代或进一步被低级烷基，低级烷氧基， 原子数不超过35的卤素，氰基或羟基及其药学上可接受的酸加成盐，以及含有这些化合物的抗抑郁制剂。 根据本发明的化合物具有有价值的药理学性质。 特别是，它们通过中脑突触体抑制5-羟色胺的吸收，H75 / 12的大鼠脑内诱导的血清素消耗，大鼠中脑突触体的去甲肾上腺素的吸收以及大鼠脑内诱发的去甲肾上腺素的耗竭 / 77。 在相同的剂量下，它们也影响大鼠脑和大鼠肝脏中单氨氧氧化酶的抑制。 此外，它们加剧了由5-羟基色氨酸引起的“头部抽搐”，并且具有良好的耐受性。 因此，通式I的化合物及其药学上可接受的酸加成盐可以用作心理药物，特别是抗抑郁药。

    Selective NPY (Y5) antagonists
    10.
    发明申请
    Selective NPY (Y5) antagonists 失效
    选择性NPY（Y5）拮抗剂

    公开(公告)号：US20050137240A1

    公开(公告)日：2005-06-23

    申请号：US11040328

    申请日：2005-01-20

    申请人： Mohammad Marzabadi ,  Wai Wong ,  Stewart Noble ,  Peter Buhlmayer ,  Heinrich Rueger ,  Yasuchika Yamaguchi ,  Walter Schilling

    发明人： Mohammad Marzabadi ,  Wai Wong ,  Stewart Noble ,  Peter Buhlmayer ,  Heinrich Rueger ,  Yasuchika Yamaguchi ,  Walter Schilling

    IPC分类号： C07D277/42 ,  C07D277/60 ,  C07D417/12 ,  C07D513/04 ,  A61K31/426 ,  C07D277/38

    CPC分类号： C07D277/60 ,  C07D277/42 ,  C07D417/12 ,  C07D513/04

    摘要： This invention is directed to bicyclic and tricyclic compounds which are selective antagonists for NPY (Y5) receptors. The invention provides a pharmaceutical composition comprising a therapeutically effective amount of a compound of the invention and a pharmaceutically acceptable carrier. This invention provides a pharmaceutical composition made by combining a therapeutically effective amount of a compound of this invention and a pharmaceutically acceptable carrier. The invention provides a process for making a pharmaceutical composition comprising combining a therapeutically effective amount of a compound of the invention and a pharmaceutically acceptable carrier. This invention further provides the use of a compound of the invention for the preparation of a pharmaceutical composition for treating an abnormality, wherein the abnormality is alleviated by decreasing the activity of a human Y5 receptor.

    摘要翻译： 本发明涉及作为NPY（Y5）受体的选择性拮抗剂的双环和三环化合物。 本发明提供了包含治疗有效量的本发明化合物和药学上可接受的载体的药物组合物。 本发明提供通过将治疗有效量的本发明化合物和药学上可接受的载体组合而制备的药物组合物。 本发明提供了制备药物组合物的方法，其包括将治疗有效量的本发明化合物和药学上可接受的载体组合。 本发明还提供了本发明化合物用于制备用于治疗异常的药物组合物的用途，其中所述异常通过降低人Y5受体的活性而减轻。