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：AR037484A1

公开(公告)日：2004-11-17

申请号：ARP000104612

申请日：2000-09-04

Applicant: HOFFMANN LA ROCHE

Inventor： TROTTMANN GERDA HUMBER ,  HUNKELER WALTER ,  JAKOB-ROETNE ROLAND ,  KILPATRICK GAVIN JOHN ,  NETTEKOVEN MATTHIAS HEINRICH ,  RIEMER CLAUS

IPC: C07D213/73 ,  A61K31/437 ,  A61K31/4418 ,  A61K31/444 ,  A61K31/496 ,  A61K31/506 ,  A61K31/5377 ,  A61K31/551 ,  A61K31/635 ,  A61P9/10 ,  A61P11/06 ,  A61P11/16 ,  A61P25/00 ,  A61P25/04 ,  A61P25/08 ,  A61P25/16 ,  A61P25/18 ,  A61P25/20 ,  A61P25/24 ,  A61P25/28 ,  A61P25/30 ,  A61P37/08 ,  A61P43/00 ,  C07D409/04 ,  C07D471/04 ,  C07D519/00 ,  A61K31/4433 ,  A61K31/4436 ,  A61K31/4439 ,  C07D249/00 ,  C07D221/00

Abstract: Compuesto derivado de amino-triazolopiridina de la fórmula (1), en donde: R1 es un grupo heteroarilo de 5 ó 6 miembros, que contiene entre 1 y 3 heteroátomos, seleccionados de entre N, O ó S, y cuyos grupos se encuentran opcionalmente sustituidos por uno o dos sustituyentes, los cuales son alquilo inferior; -(CH2)nOH, halógeno o alcoxi inferior, y en donde los grupos heteroarilo se pueden encontrar de forma opcional unidos al anillo de pirazol mediante un grupo alquileno o alquenilo o es fenilo, sustituido de forma opcional por uno o dos sustituyentes que son alquilo inferior, hidroxi-alquilo inferior, halógeno, hidroxi o alcoxi inferior o es -O(CH2)nfenilo, benzofurilo, indolilo o benzotiofenilo, o es -S-alquilo inferior; R2 y R4 son independientemente uno de otro hidrógeno, ciano o -S(O)2-fenilo; R3 es hidrógeno, halógeno o es un grupo heteroarilo de 5 ó 6 miembros, que contiene entre 1 y 3 heteroátomos, seleccionados de entre N, O ó S y cuyos grupos se encuentran sustituidos de forma opcional por uno o dos sustituyentes, los cuales son alquilo inferior, -(CH2)n-arilo, hidroxi, halógeno, alcoxi inferior, morfolinilo, amino, alquilamino inferior o -C(O)NR'2, y en donde R' es alquilo inferior o hidrógeno, o es fenilo, sustituido de forma opcional por uno o dos sustituyentes que son halógeno, alquilo inferior, alcoxi inferior, amino, di-alquilamino inferior, CF3, -OCF3, -NHC(O)alquilo inferior, ciano, -C(O)-alquilo inferior, -C(O)O-alquilo inferior, -S-alquilo inferior, -S(O)2NH-fenilo, -S(O)2-metilpiperazinilo; o es -NR'R'', en donde R' y R'' son independientemente uno de otro hidrógeno, -(CH2)nfenilo, cuyo anillo de fenilo se encuentra sustituido de forma opcional por halógeno o alcoxi inferior, -CH(alquilo inferior)-fenilo, indan-1-ilo, 1,2,3,4-tetrahidro-naftaleno, o cicloalquilo; o es -O-fenilo, cuyo anillo de fenilo se encuentra sustituido de forma opcional por halógeno, alquilo inferior o alcoxi inferior, -O-tetrahidronaftalenilo ó -O-CH2-6-metil-piridin-2-ilo; o es -benzo[1,3]dioxolilo, -1H-indol-5-ilo, naftilo, benzo-furan-2-ilo, 1,3,4,9-tetrahidro-b-carbolin-2-ilo, piperidin-1-ilo, pirrolidin-1-ilo, piperazin-4-il-metilo o morfolinilo; R5 es -NR2, en donde R pude ser el mismo o diferente y es hidrógeno, alquilo inferior, fenilo, bencilo, -CO-alquilo inferior, -CO-alcoxi inferior, -alquenilo inferior, -CO(CH2)n-fenilo o -COO(CH2)n-fenilo, en donde el anillo de fenilo se encuentra sustituido de forma opcional por CF3, alcoxi inferior, halógeno o alquilo inferior, -CO(CH2)3-NHCO-alcoxi inferior, -(CH2)n-fenilo, en donde el anillo de fenilo se encuentra sustituido de forma opcional por alcoxi inferior, CF3 o halógeno o es ácido 4,5-dihidro-1H-imidazol-2-il-benzóico, ácido 1,4,5,6-tetrahidro-pirimidin-2-il-benzóico o ácido 4,5,6,7-tetrahidro-1H-[1,3]diazepin-2-il-benzóico; n es 0-4 y sus sales farmacéuticamente aceptables. También se divulga un medicamento que contiene uno o más de los compuestos derivados de amino-triazolopiridina, un proceso para la preparación de un compuesto derivado de amino-triazolopiridina y el uso del compuesto para el tratamiento de enfermedades relacionadas con el receptor de adenosina A2A o para la elaboración de los medicamentos correspondientes.

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.

公开(公告)号：DE60001313T2

公开(公告)日：2004-01-22

申请号：DE60001313

申请日：2000-05-05

Applicant: HOFFMANN LA ROCHE

Inventor： JENCK FRANCOIS ,  HOFFMANN-EMERY FABIENNE ,  HUNKELER WALTER ,  MARTIN RICHARD ,  SLEIGHT ANDREW

IPC: A61K31/5513 ,  A61K31/5517 ,  A61P25/08 ,  A61P25/20 ,  A61P25/22 ,  C07D487/04

Abstract: The present invention relates to compound 7-Chloro-3-(5-dimethylaminomethyl-[1,2,4]oxadiazol-3-yl)-5-methyl-4,5-dihydro-imidazo[1,5-a][1,4]benzodiazepin-6-one (I)and to the use of the compound of formula I for the manufacture of medicaments to be used as anxiolytic and/or anticonvulsant and/or non-sedative sleep-inducing medicaments.

公开(公告)号：ES2193607T3

公开(公告)日：2003-11-01

申请号：ES99100149

申请日：1999-01-08

Applicant: HOFFMANN LA ROCHE

Inventor： BOS MICHAEL ,  HUNKELER WALTER ,  RIEMER CLAUS

IPC: C07C309/30 ,  A61K31/00 ,  A61K31/10 ,  A61K31/135 ,  A61K31/44 ,  A61K31/4409 ,  A61K31/4418 ,  A61K31/4427 ,  A61K31/4433 ,  A61K31/4436 ,  A61K31/505 ,  A61P25/00 ,  A61P25/14 ,  A61P25/16 ,  A61P25/18 ,  A61P25/24 ,  A61P25/28 ,  A61P43/00 ,  C07C315/04 ,  C07C317/22 ,  C07C317/32 ,  C07C317/36 ,  C07D213/61 ,  C07D213/62 ,  C07D213/71 ,  C07D213/73 ,  C07D213/74 ,  C07D213/84 ,  C07D239/38 ,  C07D401/04 ,  C07D401/14 ,  C07D409/04

Abstract: The present invention relates to novel compounds of the general formula wherein R is hydrogen; R is hydrogen, trifluoromethyl or lower alkyl; R is hydrogen or amino; or R and R or R and R taken together are -CH=CH-CH=CH-; Z is pyrimidin-4-yl, pyridin-4-yl, pyridin-2-yl or phenyl; R R are each independently hydrogen, lower alkyl, trifluoromethyl, halogen, lower alkoxy, nitrilo, amino, lower alkyl-amino, di-lower alkyl-amino, piperazinyl, morpholinyl, pyrrolidinyl, vinyl, C3-C6 cycloalkyl, C3-C6 cycloalkenyl, t-buthylethinyl, hydroxyalkylethinyl, phenylethinyl, naphthyl, thiophenyl, or phenyl, which may be substituted by halogen, lower alkoxy, lower alkyl, trifluoromethyl or nitro, or a group -NH(CH2)nNR R , -N(CH3)(CH2)nNR R , -NH(CH2)n-morpholin-4-yl or -NH(CH2)nOH; n is 2-4 R and R are each independently hydrogen or lower alkyl, and to their pharmaceutically acceptable salts. It has been found that the compounds of formula I possess a selective affinity to 5HT-6 receptors.

公开(公告)号：SI0930302T1

公开(公告)日：2003-10-31

申请号：SI9930252

申请日：1999-01-08

Applicant: HOFFMANN LA ROCHE

Inventor： BOES MICHAEL ,  HUNKELER WALTER ,  RIEMER CLAUS

IPC: C07C309/30 ,  A61K31/00 ,  A61K31/10 ,  A61K31/135 ,  A61K31/44 ,  A61K31/4409 ,  A61K31/4418 ,  A61K31/4427 ,  A61K31/4433 ,  A61K31/4436 ,  A61K31/505 ,  A61P25/00 ,  A61P25/14 ,  A61P25/16 ,  A61P25/18 ,  A61P25/24 ,  A61P25/28 ,  A61P43/00 ,  C07C315/04 ,  C07C317/22 ,  C07C317/32 ,  C07C317/36 ,  C07D213/61 ,  C07D213/62 ,  C07D213/71 ,  C07D213/73 ,  C07D213/74 ,  C07D213/84 ,  C07D239/38 ,  C07D401/04 ,  C07D401/14 ,  C07D409/04

Abstract: The present invention relates to novel compounds of the general formula wherein R is hydrogen; R is hydrogen, trifluoromethyl or lower alkyl; R is hydrogen or amino; or R and R or R and R taken together are -CH=CH-CH=CH-; Z is pyrimidin-4-yl, pyridin-4-yl, pyridin-2-yl or phenyl; R R are each independently hydrogen, lower alkyl, trifluoromethyl, halogen, lower alkoxy, nitrilo, amino, lower alkyl-amino, di-lower alkyl-amino, piperazinyl, morpholinyl, pyrrolidinyl, vinyl, C3-C6 cycloalkyl, C3-C6 cycloalkenyl, t-buthylethinyl, hydroxyalkylethinyl, phenylethinyl, naphthyl, thiophenyl, or phenyl, which may be substituted by halogen, lower alkoxy, lower alkyl, trifluoromethyl or nitro, or a group -NH(CH2)nNR R , -N(CH3)(CH2)nNR R , -NH(CH2)n-morpholin-4-yl or -NH(CH2)nOH; n is 2-4 R and R are each independently hydrogen or lower alkyl, and to their pharmaceutically acceptable salts. It has been found that the compounds of formula I possess a selective affinity to 5HT-6 receptors.