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    94.
    发明专利
    未知

    公开(公告)号：AT353881T

    公开(公告)日：2007-03-15

    申请号：AT01960225

    申请日：2001-05-18

    Applicant: HOFFMANN LA ROCHE

    Inventor： GALLEY GUIDO ,  GOERGLER ANNICK ,  GODEL THIERRY ,  HECK REINHARD

    IPC: C07D243/08 ,  A61K31/551 ,  A61K31/5517 ,  A61P1/04 ,  A61P1/08 ,  A61P9/00 ,  A61P11/06 ,  A61P13/10 ,  A61P17/02 ,  A61P19/02 ,  A61P25/00 ,  A61P25/06 ,  A61P27/02 ,  A61P29/00 ,  A61P37/08 ,  C07D243/14 ,  C07D401/06 ,  C07D401/14 ,  C07D403/06 ,  C07D409/06 ,  C07D487/04

    Abstract: The invention relates to compounds of the formulawhereinR1, R2 are independently from each other aryl or heteroaryl, wherein the heteroaryl group contains one or two heteroatoms, selected from N, O, or S, and wherein the aryl or heteroaryl groups are optionally substituted by 1 to 3 substituents, which are independently from each other halogen, CF3, lower alkoxy or lower alkyl;R3 is hydrogen, lower alkyl, -(CH2)nN(R)2, -(CH2)n-heteroaryl or is a -(CH2)n-non aromatic heterocycle, which heterocycles are optionally substituted by halogen, CF3, lower alkoxy or lower alkyl;R4 is =O, =N(CH2)nCH3 or =N(CH2)nN(R)2;R3 and R4 may be together with the N and C atoms to which they are attached the group -CR5=N-N=; R5 is hydrogen, -(CH2)nN(R)2, -(CH2)n-heteroaryl or is a -(CH2)n-non aromatic heterocycle, which heterocycles are optionally substituted by halogen, CF3, lower alkoxy or lower alkyl;R is hydrogen or lower alkyl;n is 0, 1, 2 or 3;and pharmaceutically acceptable acid addition salts and enantiomeric forms thereof. The compounds are useful in the treatment of diseases, related to the NK-1 receptor.

    3-Phenyl-pyridine derivatives
    99.
    发明专利
    3-Phenyl-pyridine derivatives 未知

    公开(公告)号：GC0000183A

    公开(公告)日：2006-03-29

    申请号：GCP2000535

    申请日：2000-02-23

    Applicant: HOFFMANN LA ROCHE

    Inventor： BOES MICHAEL ,  GALLEY GUIDO ,  GODEL THIERRY ,  HOFFMANN TORSTEN ,  HUNKELER WALTER ,  SCHNIDER PATRICK ,  STADLER HEINZ

    IPC: A61K31/44 ,  A61P25/00 ,  A61P29/00 ,  C07D213/30 ,  C07D213/38 ,  C07D213/75 ,  C07D213/81 ,  C07D401/04

    Abstract: The invention relates to compounds of the formulawhereinR is hydrogen, lower alkyl, lower alkoxy, halogen or trifluoromethyl;R1 is hydrogen or halogen; orR and R1 may be together -CH=CH-CH=CH-;R2 is hydrogen, halogen, trifluoromethyl, lower alkoxy or cyano;R3 is hydrogen, lower alkyl or form a cycloalkyl group;R4 is hydrogen, -N(R5)2, -N(R5)S(O)2-lower alkyl, -N(R5)C(O)R5 or a cyclic tertiary amine of the groupR5 is, independently from each other, hydrogen, C3-6-cycloalkyl, benzyl or lower alkyl;R6 is hydrogen, hydroxy, lower alkyl, -N(R5)CO-lower alkyl, hydroxy-lower alkyl, cyano, -CHO or a 5- or 6 membered heterocyclic group, optionally bonded via an alkylene group,X is -C(O)N(R5)-, -(CH2)mO-, -(CH2)mN(R5)-, -N(R5)C(O)-, or -N(R5)(CH2)m-;n is 0-4; andm is 1 or 2;and to pharmaceutically acceptable acid addition salts thereof.It has been shown that the above mentioned compounds have a good affinity to the NK-1 receptor.

    100.
    发明专利
    未知

    公开(公告)号：DE60015089T2

    公开(公告)日：2006-02-16

    申请号：DE60015089

    申请日：2000-02-15

    Applicant: HOFFMANN LA ROCHE

    Inventor： BOES MICHAEL ,  GALLEY GUIDO ,  GODEL THIERRY ,  HOFFMANN TORSTEN ,  HUNKELER WALTER ,  SCHNIDER PATRICK ,  STADLER HEINZ

    IPC: A61K31/44 ,  A61P25/00 ,  A61P29/00 ,  C07D213/30 ,  C07D213/38 ,  C07D213/75 ,  C07D213/81 ,  C07D401/04

    Abstract: The invention relates to compounds of the formulawhereinR is hydrogen, lower alkyl, lower alkoxy, halogen or trifluoromethyl;R1 is hydrogen or halogen; orR and R1 may be together -CH=CH-CH=CH-;R2 is hydrogen, halogen, trifluoromethyl, lower alkoxy or cyano;R3 is hydrogen, lower alkyl or form a cycloalkyl group;R4 is hydrogen, -N(R5)2, -N(R5)S(O)2-lower alkyl, -N(R5)C(O)R5 or a cyclic tertiary amine of the groupR5 is, independently from each other, hydrogen, C3-6-cycloalkyl, benzyl or lower alkyl;R6 is hydrogen, hydroxy, lower alkyl, -N(R5)CO-lower alkyl, hydroxy-lower alkyl, cyano, -CHO or a 5- or 6 membered heterocyclic group, optionally bonded via an alkylene group,X is -C(O)N(R5)-, -(CH2)mO-, -(CH2)mN(R5)-, -N(R5)C(O)-, or -N(R5)(CH2)m-;n is 0-4; andm is 1 or 2;and to pharmaceutically acceptable acid addition salts thereof.It has been shown that the above mentioned compounds have a good affinity to the NK-1 receptor.

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