公开(公告)号：FR2790473A1

公开(公告)日：2000-09-08

申请号：FR0002170

申请日：2000-02-22

Applicant: HOFFMANN LA ROCHE

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

IPC: A61K20060101 ,  A61K31/44 ,  A61K31/4409 ,  A61K31/4418 ,  A61K31/4427 ,  A61K31/444 ,  A61K31/455 ,  A61K31/496 ,  A61P1/00 ,  A61P9/00 ,  A61P11/00 ,  A61P25/00 ,  A61P25/04 ,  A61P25/28 ,  A61P25/30 ,  A61P27/02 ,  A61P29/00 ,  A61P43/00 ,  C07D20060101 ,  C07D213/30 ,  C07D213/38 ,  C07D213/40 ,  C07D213/63 ,  C07D213/65 ,  C07D213/74 ,  C07D213/75 ,  C07D213/78 ,  C07D213/82 ,  C07D401/04 ,  C07D401/12 ,  C07D413/12 ,  C07D413/14 ,  A61K31/4545

Abstract: The present invention relates to compounds of the general formula wherein R is hydrogen, lower alkyl, lower alkoxy, halogen or trifluoromethyl; R is hydrogen or halogen; or R and R may be together -CH=CH-CH=CH-; R and R are independently from each other hydrogen, halogen, trifluoromethyl, lower alkoxy or cyano; or R and R may be together -CH=CH-CH=CH-, optionally substituted by one or two substituents selected from lower alkyl or lower alkoxy; R is hydrogen, lower alkyl or form a cycloalkyl group; R is hydrogen, -N(R )2, -N(R )(CH2)nOH, -N(R )S(O)2-lower alkyl, -N(R )S(O)2-phenyl, -N=CH-N(R )2, -N(R )C(O)R or a cyclic tertiary amine of the group R is, independently from each other, hydrogen, C3-6-cycloalkyl, benzyl or lower alkyl; R is hydrogen, hydroxy, lower alkyl, -(CH2)nCOO-lower alkyl, -N(R )CO-lower alkyl, hydroxy-lower alkyl, cyano, -(CH2)nO(CH2)nOH, -CHO or a 5-or 6 membered heterocyclic group, optionally bonded via an alkylene group, X is -C(O)N(R )-, -(CH2)mO-, -(CH2)mN(R )-, -N(R )C(O)-, or -N(R )(CH2)m-; n is 0 - 4; and m is 1 or 2; and to pharmaceutically acceptable acid addition salts thereof. The compounds of formula I show a high affinity to the NK-1 receptor. They may be used for the treatment of diseases, which relate to NK-1 receptor antagonists.

公开(公告)号：NO20000885L

公开(公告)日：2000-08-25

申请号：NO20000885

申请日：2000-02-23

Applicant: HOFFMANN LA ROCHE

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

IPC: A61K20060101 ,  A61K31/44 ,  A61K31/4409 ,  A61K31/4418 ,  A61K31/4427 ,  A61K31/444 ,  A61K31/455 ,  A61K31/496 ,  A61P1/00 ,  A61P9/00 ,  A61P11/00 ,  A61P25/00 ,  A61P25/04 ,  A61P25/28 ,  A61P25/30 ,  A61P27/02 ,  A61P29/00 ,  A61P43/00 ,  C07D20060101 ,  C07D213/30 ,  C07D213/38 ,  C07D213/40 ,  C07D213/63 ,  C07D213/65 ,  C07D213/74 ,  C07D213/75 ,  C07D213/78 ,  C07D213/82 ,  C07D401/04 ,  C07D401/12 ,  C07D413/12 ,  C07D413/14 ,  C07D213/81 ,  C07D401/06 ,  C07D413/06

Abstract: The present invention relates to compounds of the general formula wherein R is hydrogen, lower alkyl, lower alkoxy, halogen or trifluoromethyl; R is hydrogen or halogen; or R and R may be together -CH=CH-CH=CH-; R and R are independently from each other hydrogen, halogen, trifluoromethyl, lower alkoxy or cyano; or R and R may be together -CH=CH-CH=CH-, optionally substituted by one or two substituents selected from lower alkyl or lower alkoxy; R is hydrogen, lower alkyl or form a cycloalkyl group; R is hydrogen, -N(R )2, -N(R )(CH2)nOH, -N(R )S(O)2-lower alkyl, -N(R )S(O)2-phenyl, -N=CH-N(R )2, -N(R )C(O)R or a cyclic tertiary amine of the group R is, independently from each other, hydrogen, C3-6-cycloalkyl, benzyl or lower alkyl; R is hydrogen, hydroxy, lower alkyl, -(CH2)nCOO-lower alkyl, -N(R )CO-lower alkyl, hydroxy-lower alkyl, cyano, -(CH2)nO(CH2)nOH, -CHO or a 5-or 6 membered heterocyclic group, optionally bonded via an alkylene group, X is -C(O)N(R )-, -(CH2)mO-, -(CH2)mN(R )-, -N(R )C(O)-, or -N(R )(CH2)m-; n is 0 - 4; and m is 1 or 2; and to pharmaceutically acceptable acid addition salts thereof. The compounds of formula I show a high affinity to the NK-1 receptor. They may be used for the treatment of diseases, which relate to NK-1 receptor antagonists.

公开(公告)号：NO20000885A

公开(公告)日：2000-08-25

申请号：NO20000885

申请日：2000-02-23

Applicant: HOFFMANN LA ROCHE

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

IPC: A61K20060101 ,  A61K31/44 ,  A61K31/4409 ,  A61K31/4418 ,  A61K31/4427 ,  A61K31/444 ,  A61K31/455 ,  A61K31/496 ,  A61P1/00 ,  A61P9/00 ,  A61P11/00 ,  A61P25/00 ,  A61P25/04 ,  A61P25/28 ,  A61P25/30 ,  A61P27/02 ,  A61P29/00 ,  A61P43/00 ,  C07D20060101 ,  C07D213/30 ,  C07D213/38 ,  C07D213/40 ,  C07D213/63 ,  C07D213/65 ,  C07D213/74 ,  C07D213/75 ,  C07D213/78 ,  C07D213/82 ,  C07D401/04 ,  C07D401/12 ,  C07D413/12 ,  C07D413/14 ,  C07D213/81 ,  C07D401/06 ,  C07D413/06

CPC classification number: C07D213/30 ,  C07D213/38 ,  C07D213/40 ,  C07D213/74 ,  C07D213/75 ,  C07D213/82 ,  C07D401/04 ,  C07D401/12 ,  C07D413/12 ,  C07D413/14

公开(公告)号：HK1007865A1

公开(公告)日：1999-04-30

申请号：HK98108915

申请日：1998-07-07

Applicant: HOFFMANN LA ROCHE

Inventor： BOES MICHAEL ,  GODEL THIERRY ,  RIEMER CLAUS ,  SLEIGHT ANDREW

IPC: A61K31/63 ,  A61K31/18 ,  A61K31/325 ,  A61K31/40 ,  A61K31/403 ,  A61K31/404 ,  A61K31/44 ,  A61K31/505 ,  A61P25/00 ,  C07C311/21 ,  C07C311/38 ,  C07C311/44 ,  C07D209/08 ,  C07D213/76 ,  C07D239/48 ,  C07D239/50 ,  C07D239/69 ,  C07D403/04 ,  A61K ,  C07C ,  C07D

Abstract: Use of sulphonamide compounds of formula (I) is claimed for treatment of central nervous disorders. Z = a group of formula (a)-(e); R = H, NH2, lower alkylamino, dialkylamino or alkyl, or halo or CF3; R = H or lower alkyl; R = H, NH2, lower alkylamino, dialkylamino, alkyl or alkoxy, or halo or CF3; R = NH2 or halo, or lower alkylamino, dialkylamino, alkyl or alkoxy; R = H or halo, or lower alkylamino, dialkylamino or alkoxy; R = lower alkyl, alkylamino, dialkylamino or alkoxy, or halo or CF3; R = NH2, lower alkylamino, dialkylamino, alkoxy or alkylsulphanyl, SH, pyrrolidin-1-yl or azetidin-1-yl; R = NH2, lower alkylamino, dialkylamino, alkoxy or alkylsulphanyl, benzylamino, halo, pyrrolidin-1-yl or azetidin-1-yl; R , R = lower alkoxy or alkylamino; R = H or halo; R = H or lower alkyl; and provided that R and R are not both OCH3.

公开(公告)号：MX9802816A

公开(公告)日：1998-09-30

申请号：MX9802816

申请日：1998-04-08

Applicant: HOFFMANN LA ROCHE

Inventor： GODEL THIERRY ,  RIEMER CLAUS ,  EDENHOFER ALBRECHT

IPC: A61K31/505 ,  A61P25/18 ,  C07D239/26 ,  C07D239/42 ,  C07D239/47 ,  C07D239/48 ,  C07D401/06

Abstract: La invencion se refiere a compuestos de la formula general (1), caracterizado porque R1 Y R2 cada uno significan individualmente amino o alquilo inferiores, A significa A1, A2, A3, A4, A5, A6, A7-; B significa hidrogeno en A4, A5 y A6; (i) en A1 - A6; alquilo inferior en A4 -A6; y alquilo inferior, estirilo, feniletimilo o benzoiloxi-alquilo inferior en A1 y A2; n significa 0, 2 m,p significa 0,1 y R3, R4, R5 y R6 cada uno significa independientemente, hidrogeno, halogeno, alquilo inferior, trifluorometilo, alcoxi inferior o nitro, y las sales de adicion del ácido farmacéuticamente aceptables del mismo. Estos compuestos se pueden usar en el control o prevencion de enfermedades las cuales son causadas por desordenes del sistema de la dopamina. Enfermedades sicoticas tales como por ejemplo, esquizofrenia correspondiente a estos.

公开(公告)号：TR199800636T1

公开(公告)日：1998-06-22

申请号：TR9800636

申请日：1996-10-04

Applicant: HOFFMANN LA ROCHE

Inventor： GODEL THIERRY ,  RIEMER CLAUS ,  EDENHOFER ALBRECHT

IPC: A61K31/505 ,  A61P25/18 ,  C07D239/26 ,  C07D239/42 ,  C07D239/47 ,  C07D239/48 ,  C07D401/06

Abstract: Compounds of the formula I wherein R1 and R2 each individually are lower-alkyl or amino, A is B is hydrogen in A4, A5 and A6; in A1-A6; lower-alkoxy in A4-A6; and lower-alkyl, styryl, phenylethynyl or benzoyloxy-lower-alkyl in A1 and A2; n is 0, 1 or 2; m, p are, independently 0, 1 and R3, R4, R5 and R6 each independently are hydrogen, halogen, lower-alkyl, trifluoromethyl, lower-alkoxy or nitro, and pharmaceutically acceptable acid addition salts thereof. These compounds are useful in the control or prevention of illnesses which are caused by disorders of the dopamine system, in particular psychotic illnesses such as schizophrenia.

公开(公告)号：TR199701577T1

公开(公告)日：1998-06-22

申请号：TR9701577

申请日：1996-06-04

Applicant: HOFFMANN LA ROCHE

Inventor： GODEL THIERRY ,  HARTMAN DEBORAH ,  RIEMER CLAUS

IPC: A61K31/44 ,  C07D211/70 ,  A61K31/4418

Abstract: A method of treating or preventing illnesses caused by a disorder of the dopamine system. The method comprises administering to a host requiring such treatment or prevention an effective amount of a pharmaceutical composition comprising a compound of the formula I wherein R1 is hydrogen, lower-alkyl, halogen, lower-alkoxy or nitro; R2 is hydrogen, lower alkyl or trifluoromethyl; and R3 is hydrogen, lower alkyl, trifluoromethyl, benzyl, hydroxy-lower-alkyl, lower alkoxy, lower-alkyl-carbonyl-amino, carbonyl-lower-alkyl, benzyl, di-lower-alkyl-amino-carbonyl, carbonylamino or amino-carbonyl-amino; or R2 and R3 together optionally are a fused benzene ring and R4 is hydrogen or halogen, or a pharmaceutically acceptable salt of a compound of formula I, and a pharmaceutically inert carrier material.

公开(公告)号：AU2841697A

公开(公告)日：1998-01-22

申请号：AU2841697

申请日：1997-06-27

Applicant: HOFFMANN LA ROCHE

Inventor： BOES MICHAEL ,  GODEL THIERRY ,  RIEMER CLAUS ,  SLEIGHT ANDREW

IPC: A61K31/63 ,  A61K31/18 ,  A61K31/325 ,  A61K31/40 ,  A61K31/403 ,  A61K31/404 ,  A61K31/44 ,  A61K31/505 ,  A61P25/00 ,  C07C311/21 ,  C07C311/38 ,  C07C311/44 ,  C07D209/08 ,  C07D213/76 ,  C07D239/48 ,  C07D239/50 ,  C07D239/69 ,  C07D403/04

Abstract: Use of sulphonamide compounds of formula (I) is claimed for treatment of central nervous disorders. Z = a group of formula (a)-(e); R = H, NH2, lower alkylamino, dialkylamino or alkyl, or halo or CF3; R = H or lower alkyl; R = H, NH2, lower alkylamino, dialkylamino, alkyl or alkoxy, or halo or CF3; R = NH2 or halo, or lower alkylamino, dialkylamino, alkyl or alkoxy; R = H or halo, or lower alkylamino, dialkylamino or alkoxy; R = lower alkyl, alkylamino, dialkylamino or alkoxy, or halo or CF3; R = NH2, lower alkylamino, dialkylamino, alkoxy or alkylsulphanyl, SH, pyrrolidin-1-yl or azetidin-1-yl; R = NH2, lower alkylamino, dialkylamino, alkoxy or alkylsulphanyl, benzylamino, halo, pyrrolidin-1-yl or azetidin-1-yl; R , R = lower alkoxy or alkylamino; R = H or halo; R = H or lower alkyl; and provided that R and R are not both OCH3.

公开(公告)号：CZ9702002A3

公开(公告)日：1998-01-14

申请号：CZ200297

申请日：1997-06-25

Applicant: HOFFMANN LA ROCHE

Inventor： BOES MICHAEL ,  GODEL THIERRY ,  RIEMER CLAUS ,  SLEIGHT ANDREW

IPC: A61K31/63 ,  A61K31/18 ,  A61K31/325 ,  A61K31/40 ,  A61K31/403 ,  A61K31/404 ,  A61K31/44 ,  A61K31/505 ,  A61P25/00 ,  C07C311/21 ,  C07C311/38 ,  C07C311/44 ,  C07D209/08 ,  C07D213/76 ,  C07D239/48 ,  C07D239/50 ,  C07D239/69 ,  C07D403/04

Abstract: Use of sulphonamide compounds of formula (I) is claimed for treatment of central nervous disorders. Z = a group of formula (a)-(e); R = H, NH2, lower alkylamino, dialkylamino or alkyl, or halo or CF3; R = H or lower alkyl; R = H, NH2, lower alkylamino, dialkylamino, alkyl or alkoxy, or halo or CF3; R = NH2 or halo, or lower alkylamino, dialkylamino, alkyl or alkoxy; R = H or halo, or lower alkylamino, dialkylamino or alkoxy; R = lower alkyl, alkylamino, dialkylamino or alkoxy, or halo or CF3; R = NH2, lower alkylamino, dialkylamino, alkoxy or alkylsulphanyl, SH, pyrrolidin-1-yl or azetidin-1-yl; R = NH2, lower alkylamino, dialkylamino, alkoxy or alkylsulphanyl, benzylamino, halo, pyrrolidin-1-yl or azetidin-1-yl; R , R = lower alkoxy or alkylamino; R = H or halo; R = H or lower alkyl; and provided that R and R are not both OCH3.

公开(公告)号：MX9704817A

公开(公告)日：1997-12-31

申请号：MX9704817

申请日：1997-06-26

Applicant: HOFFMANN LA ROCHE

Inventor： BOS MICHAEL ,  GODEL THIERRY ,  RIEMER CLAUS ,  SLEIGHT ANDREW

IPC: A61K31/63 ,  A61K31/18 ,  A61K31/325 ,  A61K31/40 ,  A61K31/403 ,  A61K31/404 ,  A61K31/44 ,  A61K31/505 ,  A61P25/00 ,  C07C311/21 ,  C07C311/38 ,  C07C311/44 ,  C07D209/08 ,  C07D213/76 ,  C07D239/48 ,  C07D239/50 ,  C07D239/69 ,  C07D403/04 ,  C07C317/32 ,  C07D247/00

Abstract: El presente invento se refiere a compuestos de formula general I en donde (Ver Formula) Z significa un grupo de fenilo sustituido, piridilo sustituido o indolilo sustituido de las formulas a-e (Ver Formula) R1 significa hidrogeno, amino, alquilamino inferior, dialquilamino inferior, alquilo inferior, halogeno o trifluorometilo; R2 significa hidrogeno o alquilo inferior; R3 significa hidrogeno, amino, alquilamino inferior, dialquilamino inferior, alquilo inferior, CF3, alcoxilo inferior o halogeno; R4 significa amino, alquilamino inferior, dialquilamino inferior, alquilo inferior, alcoxilo inferior o halogeno; R5 significa hidrogeno, alquilamino inferior, di-alquilamino inferior, alcoxilo inferior o halogeno; R6 significa alquilo inferior, alquilamino inferior, di-alquilamino inferior, alcoxilo inferior, halogeno o CF3, R7 significa amino, alquilamino inferior, di-alquilamino inferior, alcoxilo inferior, alquilsulfanilo inferior, mercapto, pirrolidin-1-ilo o azetidin-1-ilo; R8 significa amino, alquilamino inferior, di-alquilamino inferior, bencilamino, alcoxilo inferior, alquilsulfanilo inferior, halogeno, pirrolidin-1-ilo o azetidin-1-ilo; R9 y R10 significan cada uno, independientemente, alcoxilo inferior o alquilamino inferior; R11 significa hidrogeno o halogeno; R12 significa hidrogeno o alquilo inferior, y a significa un doble enlace opcional, con la salvedad de que R7 y R8 no significan simultáneamente metoxilo, así como sus sales farmacéuticamente aceptables, como sustancias terapéuticamente activs contra trastornos del sistema nervioso central y para la produccion de medicamentos correspondientes.