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.

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.

公开(公告)号：AT317389T

公开(公告)日：2006-02-15

申请号：AT00927234

申请日：2000-05-24

Applicant: HOFFMANN LA ROCHE

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

IPC: A61K31/496 ,  A61K31/505 ,  A61K31/506 ,  A61K31/5377 ,  A61P1/04 ,  A61P1/08 ,  A61P9/00 ,  A61P11/06 ,  A61P17/02 ,  A61P19/02 ,  A61P25/00 ,  A61P25/06 ,  A61P25/16 ,  A61P25/22 ,  A61P25/24 ,  A61P25/28 ,  A61P25/36 ,  A61P27/00 ,  A61P27/02 ,  A61P29/00 ,  A61P37/08 ,  A61P43/00 ,  C07D213/00 ,  C07D239/00 ,  C07D239/28 ,  C07D239/32 ,  C07D239/34 ,  C07D239/38 ,  C07D239/42 ,  C07D239/48 ,  C07D295/00 ,  C07D401/04 ,  C07D403/04

Abstract: The invention provides compounds of the formulawhereinR1 is hydrogen or halogen;R2 is hydrogen, halogen, lower alkyl or lower alkoxy;R1 and R2 may together be -CH=CH-CH=CH-, wherein R1 and R2 together with the two carbon ring atoms to which they are attached form a fused ring;R3 is halogen, trifluoromethyl, lower alkyl or lower alkoxy;R4/R4' are each independently hydrogen or lower alkyl;R5 is lower alkyl, lower alkoxy, amino, phenyl, hydroxy-lower alkyl, cyano-lower alkyl, carbamoyl-lower alkyl, pyridyl, pyrimidyl, -(CH2)n-piperazinyl, which is optionally substituted by one or two lower alkyl groups or by hydroxy-lower alkyl, -(CH2)n-morpholinyl, -(CH2)n-piperidinyl, -(CH2)n+1-imidazolyl, lower alkyl-sulfanyl, lower alkyl-sulfonyl, benzylamino, -NH-(CH2)n+1N(R4'')2, -(CH2)n+1N(R4'')2, -O-(CH2)n+1-morpholinyl, -O-(CH2)n+1-piperidinyl or -O-(CH2)n+1N(R4'')2, wherein R4'' is hydrogen or lower alkyl; andn is 0-2;X is -C(O)N(R4'')- or -N(R4'')C(O)-;and to pharmaceutically acceptable acid addition salts thereof.It has been shown that the compounds have a good affinity to the NK-1 receptor and may therefore used for the treatment of diseases related to this receptor.

公开(公告)号：PT1157005E

公开(公告)日：2005-02-28

申请号：PT00909174

申请日：2000-02-15

Applicant: HOFFMANN LA ROCHE

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

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.

公开(公告)号：DE60017110D1

公开(公告)日：2005-02-03

申请号：DE60017110

申请日：2000-02-28

Applicant: HOFFMANN LA ROCHE

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

IPC: C07D295/14 ,  A61K31/166 ,  A61K31/167 ,  A61K31/495 ,  A61K31/496 ,  A61P1/04 ,  A61P1/08 ,  A61P11/06 ,  A61P25/24 ,  A61P25/28 ,  A61P29/00 ,  A61P37/08 ,  A61P43/00 ,  C07C41/01 ,  C07C43/174 ,  C07C209/06 ,  C07C209/50 ,  C07C211/29 ,  C07C211/45 ,  C07C217/54 ,  C07C231/02 ,  C07C231/08 ,  C07C233/11 ,  C07C233/15 ,  C07C233/44 ,  C07C233/66 ,  C07C235/42 ,  C07D295/155

Abstract: The invention relates to compounds of the formulawhereinR is hydrogen, lower alkyl, lower alkoxy halogen, amino, -N(R6)2 or trifluoromethyl;R1 is hydrogen lower alkoxy or halogen,R and R1 may be together -CH=CH-CH=CH-;R2 is halogen, lower alkyl or trifluoromethyl;R3 is hydrogen or lower alkyl;R4 is hydrogen or a cyclic tertiary amine, optionally substituted by lower alkyl;R5 is hydrogen, nitro, amino or -N(R6)2;R6 is hydrogen or lower alkyl,X is -C(O)N(R6)-, -(CH2)nO-, (CH2)nN(R6)-, -N(R6)C(O)- or -N(R6)(CH2)n-; andn is 1 or 2;and pharmaceutically acceptable acid addition salts thereof.The compounds of formula I may be used for the treatment of diseases related to the NK-1 receptor.

公开(公告)号：MA26612A1

公开(公告)日：2004-12-20

申请号：MA25485

申请日：1999-03-08

Applicant: HOFFMANN LA ROCHE

Inventor： BOES MICHAEL ,  RIEMER CLAUS ,  STADLER HEINZ

IPC: A61K31/00 ,  A61K31/4162 ,  A61K31/505 ,  A61K31/519 ,  A61K31/529 ,  A61K31/53 ,  A61K31/535 ,  A61K31/5375 ,  A61K31/5377 ,  A61P9/10 ,  A61P25/00 ,  A61P25/14 ,  A61P25/16 ,  A61P25/18 ,  A61P25/24 ,  A61P25/28 ,  A61P43/00 ,  C07D231/54 ,  C07D251/72 ,  C07D487/04 ,  C07D495/14 ,  A61K31/415 ,  A61K31/495 ,  C07D239/70

公开(公告)号：AT280158T

公开(公告)日：2004-11-15

申请号：AT00909174

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.

公开(公告)号：JO2254B

公开(公告)日：2004-10-07

申请号：JO200015

申请日：2000-02-22

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

CPC classification number: C07D213/75 ,  C07D213/38 ,  C07D213/81

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

公开(公告)号：JO2235B

公开(公告)日：2004-10-07

申请号：JO200017

申请日：2000-03-02

Applicant: HOFFMANN LA ROCHE

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

IPC: C07D295/14 ,  A61K31/166 ,  A61K31/167 ,  A61K31/495 ,  A61K31/496 ,  A61P1/04 ,  A61P1/08 ,  A61P11/06 ,  A61P25/24 ,  A61P25/28 ,  A61P29/00 ,  A61P37/08 ,  A61P43/00 ,  C07C41/01 ,  C07C43/174 ,  C07C209/06 ,  C07C209/50 ,  C07C211/29 ,  C07C211/45 ,  C07C217/54 ,  C07C231/02 ,  C07C231/08 ,  C07C233/11 ,  C07C233/15 ,  C07C233/44 ,  C07C233/66 ,  C07C235/42 ,  C07D295/155

CPC classification number: C07D295/155 ,  C07C217/54 ,  C07C233/15 ,  C07C233/44 ,  C07C233/66 ,  C07C235/42

Abstract: The present invention relates to compounds of the general formula Wherein R is hydrogen, lower alkyl, lower alkoxy, halogen, amino, N(R6)2 or trifluoromethyl R1 hydroeng, lower alkoxy or halogen R and R1 may be together CH=CH-CH=CH R2 is halogen, lower alkyl or trifluoromethyl R3 is hydrogen or lower alkyl R4 is hydrogen or a cyclic tertiary amine, optionally substituted by lower alkyl R5 is hydrogen, nitro, amino or N(R6)2 R6 is hydrogen or lower alkyl X is C(O)N(R6)(CH2)and N is 1-2 And to pharmaceutical acceptable acid addition salts thereof The compounds of formula and their salts are characterized by valuable therapeutic properties.

公开(公告)号：DE60013127D1

公开(公告)日：2004-09-23

申请号：DE60013127

申请日：2000-05-24

Applicant: HOFFMANN LA ROCHE

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

IPC: A61K31/505 ,  A61K31/506 ,  A61K31/513 ,  A61K31/5377 ,  A61P1/04 ,  A61P1/08 ,  A61P9/00 ,  A61P11/02 ,  A61P11/06 ,  A61P17/02 ,  A61P25/00 ,  A61P25/06 ,  A61P25/16 ,  A61P25/22 ,  A61P25/24 ,  A61P25/28 ,  A61P25/30 ,  A61P29/00 ,  A61P37/08 ,  A61P43/00 ,  C07D213/00 ,  C07D239/00 ,  C07D239/28 ,  C07D239/34 ,  C07D239/38 ,  C07D239/42 ,  C07D239/46 ,  C07D239/48 ,  C07D295/00 ,  C07D401/04

Abstract: Compounds of the general formula are described:whereinR is hydrogen or halogen;R is hydrogen, halogen, lower alkyl or lower alkoxy;R is halogen, trifluoromethyl, lower alkoxy or lower alkyl;R /R are each independently hydrogen or lower alkyl;R is lower alkyl, lower alkoxy, amino, hydroxy, hydroxy-lower alkyl, -(CH2)n-piperazinyl, optionally substituted by lower alkyl, -(CH2)n-morpholinyl, -(CH2)n+1-imidazolyl, -O-(CH2)n+1-morpholinyl, -O-(CH2)n+1-piperidinyl, lower alkyl-sulfanyl, lower alkyl-sulfonyl, benzylamino, -NH-(CH2)n+1N(R )2, -(CH2)n-NH-(CH2)n+1N(R )2, -(CH2)n+1N(R )2, or -O-(CH2)n+1N(R )2, wherein R is hydrogen or lower alkyl;R is hydrogen;R and R or R and R may together be -CH=CH-CH=CH-, wherein R and R or R and R , respectively, together with the two carbon ring atoms to which they are attached form a fused ring, with the proviso that n for R is 1;n is independently 0-2; andX is -C(O)N(R )- or -N(R )C(O)-;and pharmaceutically acceptable acid addition salts thereof.