- PIPERIDINE DERIVATIVES AS NK3 ANTAGONISTS
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The invention relates to a compound of formula wherein Ar1, Ar2, R1, R2, R3, R4, R5, and R5′ or to a pharmaceutically active salt thereof. The compounds are high potential NK-3 receptor antagonists for the treatment of depression, pain, psychosis, Parkinson's disease, schizophrenia, anxiety and attention deficit hyperactivity disorder (ADHD).
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Page/Page column 7
(2009/04/24)
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- SPIROPIPERIDINE DERIVATIVES AS NK3 ANTAGONISTS
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The present invention relates to a compound of formula (I) wherein R1 is hydrogen or lower alkyl; R2 is lower alkyl, lower hydroxyalkyl or -(CHR5)x-A; R5 is hydrogen, lower alkyl or lower hydroxyalkyl, or is heteroaryl optionally substituted by lower alkyl; A is cycloalkyl, aryl, heterocyclyl or heteroaryl, which rings are optionally substituted one or more R6, wherein R6 is lower alkyl, lower alkoxy, lower alkylsulfonyl, cyano, halogen, lower alkyl substituted by halogen or lower alkoxy substituted by halogen, or is aryl, heterocyclyl or heteroaryl optionally substituted by lower alkyl or is cycloalkyl optionally substituted by lower alkyl; x is 0, 1, 2 or 3; or R1, R2 may form together with the N-atom heterocyclyl or heteroaryl, which rings are optionally substituted by one or more substituents selected from the group consisting of lower alkyl, lower alkoxy, lower alkylsulfonyl, halogen, cycloalkyl, benzyl or aryl; R3 is hydrogen or halogen; R4 is hydrogen or lower alkyl; R7 is hydrogen, halogen or lower alkyl; m is 1 or 2; when m is 2, R3 may be the same or not; n is 1 or 2; o is 1 or 2; when o is 2, R7 may be the same or not; or to a pharmaceutically suitable acid addition salt thereof. It has been found that the present compounds are high potential NK-3 receptor antagonists for the treatment of depression, pain, psychosis, Parkinson's disease, schizophrenia, anxiety and attention deficit hyperactivity disorder (ADHD).
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Page/Page column 43-44
(2008/12/07)
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- SUBSTITUTED OXIMES, HYDRAZONES AND OLEFINS AS NEUROKININ ANTAGONISTS
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Compound represented by the structural formula STR1 or a pharmaceutically acceptable salt thereof, wherein: a is 0, 1, 2 or3; b, d and e are independently 0, 1 or 2;R is H, C 1-6 alkyl,--OH or C 2-C 6 hydroxyalkyl;A is an optionally su
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- A convenient synthesis of 3-arylbutanolides and 3-arylbutenolides
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A series of 3-aryl-substituted butenolides and butanolides has been prepared in a common short synthetic sequence from the corresponding aryl aldehydes. The 3-arylbutanolides are prepared by cyclisation of 3-aryl-3- cyano-1-propanols, obtained by selectiv
- Gu, Jian-Xin,Holland, Herbert L.
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p. 3305 - 3315
(2007/10/03)
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- SUBSTITUTED OXIMES, HYDRAZONES AND OLEFINS AS NEUROKININ ANTAGONISTS
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Compound represented by the structural formula STR1 or a pharmaceutically acceptable salt thereof, wherein: a is 0, 1, 2 or 3;b, d and e are independently 0, 1 or 2;R is H, C 1-6 alkyl,--OH or C 2-C 6 hydroxyalkyl; A is an optionally s
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