公开(公告)号：DE69820989D1

公开(公告)日：2004-02-12

申请号：DE69820989

申请日：1998-01-07

Applicant: HOFFMANN LA ROCHE

Inventor： BOES MICHAEL ,  STADLER HEINZ ,  WICHMANN JUERGEN

IPC: C07D217/24 ,  A61K31/40 ,  A61K31/403 ,  A61K31/435 ,  A61K31/473 ,  A61P1/00 ,  A61P7/02 ,  A61P9/00 ,  A61P9/12 ,  A61P25/00 ,  C07D209/62 ,  C07D221/10 ,  C07D491/04 ,  C07D491/056

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.

公开(公告)号：DK0941994T3

公开(公告)日：2003-09-08

申请号：DK99102872

申请日：1999-03-03

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 ,  C07D495/04

Abstract: The present invention is concerned with pyrazolopyrimidines and pyrazolotriazines of the general formulae and their pharmaceutically acceptable salts. Surprisingly, these compounds have a selective affinity to 5HT-6 receptors. They are accordingly suitable for the treatment and prevention of central nervous disorders such as, for example, psychoses, schizophrenia, manic depressions, depressions, neurological disorders, memory disorders, Parkinson's disease, amyotrophic lateral sclerosis, Alzheimer's disease and Huntington's chorea.

公开(公告)号：AR029614A1

公开(公告)日：2003-07-10

申请号：ARP000100737

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: 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 ,  C07D213/36 ,  C07D213/22 ,  C07D401/02 ,  A61K31/4406 ,  A61P1/43

Abstract: Derivados de 4-fenil-piridina de formula general (1), en donde R es hidrogeno, alquilo inferior, alcoxi inferior, halogeno o trifluorometilo; R1 es hidrogeno o halogeno; o R y R1 pueden ser conjuntamente -CH=CH-CH=CH-; R2 Y R2' son independientemente, hidrogeno, halogeno, triflurometilo, ciano o alcoxi inferior; o R2 y R2' pueden ser conjuntamente -CH=CH-CH=CH-, sustituido opcionalmente por uno o dos sustituyentes seleccionados del alquilo inferior o del alcoxi inferior; R3 es hidrogeno, alquilo inferior o forma un grupo cicloalquilo; R4 es hidrogeno, -N(R5)2, -N(R5) (CH2)nOH, -N(R5)S(O)2- alquilo inferior, -N(R5)S(O)2-fenilo, -N=CH-N(R5)2, -N(R5)C(O)R5 o una amina terciaria cíclica del grupo (2); R5 es independientemente, hidrogeno, C3-6-cicloalquilo, bencilo o alquilo inferior; R6 es hidrogeno, hidroxi, alquilo inferior, -(CH2)nCOO-alquilo inferior, -N(R5)CO-alquilo inferior, hidroxi-alquilo-inferior, ciano, -(CH2)nO(CH2)nOH, -CHO o un grupo heterocíclico de 5 o 6 miembros, unido opcionalmente por un grupo alquileno, X es -C(O)N(R5)-, -(CH2)mO-, -(CH2)mN(R5)-, -N(R5)C(O)-, o -N(R5) (CH2)m-; n es 0-4; y m es 1o 2; y sales derivadas de una adicion ácida farmacéuticamente aceptables. Los compuestos de formula (1) muestran una mayor afinidad por el receptor de NK-1. Estos se pueden usar para el tratamiento de enfermedades que estén relacionadas con antagonistas del receptor de NK-1.

公开(公告)号：DE69716062T2

公开(公告)日：2003-06-18

申请号：DE69716062

申请日：1997-04-24

Applicant: HOFFMANN LA ROCHE

Inventor： BOES MICHAEL ,  STADLER HEINZ ,  WICHMANN JUERGEN

IPC: A61K31/34 ,  A61K31/343 ,  A61P25/00 ,  A61P25/20 ,  A61P25/28 ,  C07D307/85 ,  C07D307/86

Abstract: The invention is concerned with the use of compounds of the general formula wherein R1-R4 signify hydrogen, halogen, lower-alkyl, lower-alkoxy, aryl, benzyloxy, lower-alkoxy-lower-alkyl, lower-alkyl-sulphanyl, lower-alkyl-sulphanyl-lower-alkyl or R1 and R2 together signify the group -O-(CH2)2- or -(CH2)2-O- and R5 signifies hydrogen or hydroxy, as well as their pharmaceutically acceptable salts in the control or prevention of illnesses or disorders of the central nervous system such as migraine, schizophrenia, anxiety states, sleep disorders, anorexia, Alzheimer's disease, addictions (alcohol, nicotine, benzodiazepine, cocaine, etc.), as well as disorders which result from damage to the head/brain or to the spinal column/bone marrow and, respectively, for the production of corresponding medicaments.

公开(公告)号：HU0201710A2

公开(公告)日：2002-10-28

申请号：HU0201710

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：HU0201527A2

公开(公告)日：2002-08-28

申请号：HU0201527

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：HU0200124A2

公开(公告)日：2002-08-28

申请号：HU0200124

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: C07C211/44 ,  A61K31/167 ,  A61K31/44 ,  A61P25/00 ,  A61P29/00 ,  C07C211/54 ,  C07C233/29 ,  C07C233/33 ,  C07C233/44 ,  C07C317/14 ,  C07C317/40 ,  C07C323/41 ,  C07D213/75 ,  C07D213/79 ,  C07D213/81 ,  C07D295/12 ,  C07D295/135 ,  C07D401/04

Abstract: The present invention is a series of compounds formed from phenyl substituted pyridine or benzene derivatives and their pharmaceutically acceptable salts. These compounds have shown high affinity as antagonists to the NK-1 receptor.

公开(公告)号：HU0200139A2

公开(公告)日：2002-06-29

申请号：HU0200139

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：DK0815861T3

公开(公告)日：2002-01-21

申请号：DK97109984

申请日：1997-06-19

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 ,  C07D209/40

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.