公开(公告)号：ZA8105112B

公开(公告)日：1982-08-25

申请号：ZA8105112

申请日：1981-07-24

Applicant: HOFFMANN LA ROCHE

Inventor： BRANCA QUIRICO ,  FISCHLI ALBERT EDUARD ,  SZENTE ANDRE

IPC: A61K31/135 ,  A61K31/15 ,  A61P5/38 ,  C07C67/00 ,  C07C239/00 ,  C07C251/48 ,  C07D243/24 ,  C07C ,  A61K

CPC classification number: C07D243/24

公开(公告)号：AU7941782A

公开(公告)日：1982-07-22

申请号：AU7941782

申请日：1982-01-11

Applicant: HOFFMANN LA ROCHE

Inventor： ASCHWANDEN WERNER ,  BRANCA QUIRICO ,  KYBURZ EMILIO ,  PFISTER RUDOLF

IPC: C07D295/02 ,  A61K31/00 ,  A61P37/08 ,  C07C1/00 ,  C07C13/547 ,  C07C67/00 ,  C07C209/00 ,  C07C209/04 ,  C07C209/08 ,  C07C209/22 ,  C07C211/32 ,  C07D295/03 ,  A61K31/40 ,  A61K31/425 ,  A61K31/445 ,  A61K31/495 ,  A61K31/535 ,  A61K31/645 ,  C07C21/24 ,  C07C87/458 ,  C07C87/459

公开(公告)号：HRP20080306B1

公开(公告)日：2015-01-30

申请号：HRP20080306

申请日：2008-06-27

Applicant: HOFFMANN LA ROCHE

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

IPC: C07D213/82 ,  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 ,  C07D401/04 ,  C07D401/12 ,  C07D413/12 ,  C07D413/14

Abstract: Prikazani izum se odnosi na spojeve opće formuleRje nezavisno jedan od drugoga vodik, Ccikloalkil, benzil ili niži alkilRje vodik, hidroksi, niži alkil, -(CH)COO-niži alkil,-N(R)CO-niži alkil, hidroksi-niži alkil, cijano,-(CH)O(CH)OH ili -CHO ili petero ili šestero člana heterociklička skupina, povoljno je vezana preko alkilen skupina, X je -C(O)N(R)-, -(CH)O-, -(CH)N(R)-, -N(R)C(O)- ili -N(R) (CH)-;n je 0-4; tem je 1 ili 2;kao i na njihove farmaceutski prihvatljive kiselinske adicijske soli. Spojevi formule I pokazuju snažni afinitet prema NK-1 receptorima. Oni se mogu koristiti za liječenje oboljenja povezanih s antagonistima NK-1 receptora.

公开(公告)号：SK287912B6

公开(公告)日：2012-03-02

申请号：SK50522008

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: C07D213/00 ,  A61K20060101 ,  A61K31/00 ,  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 ,  C07D401/00 ,  C07D401/04 ,  C07D401/12 ,  C07D413/12 ,  C07D413/14

Abstract: They are described 4-phenylpyridine derivates of the general formula (I), the substituent have specific meaning, and pharmaceutically acceptable acid addition salts thereof. The compounds of formula (I) show a high affinity to the NK-1 receptor. They can be used for the treatment of diseases, which relate to NK-1 receptor antagonists.

公开(公告)号：RS20080562A

公开(公告)日：2009-09-08

申请号：RSP20080562

申请日：2000-02-22

Applicant: HOFFMANN LA ROCHE

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

IPC: C07D213/82 ,  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 ,  C07D401/04 ,  C07D401/12 ,  C07D413/12 ,  C07D413/14

Abstract: Ovaj pronalazak se odnosi na jedinjenja opšte formule u kojoj označavaju R vodonik, niži alkil, niži alkoksi, halogen ili trifluormetil, R1 vodonik ili halogen, ili R i R1 mogu zajedno formirati -CH=CH-CH=CH-, R2 i R2' nezavisno jedan od drugog označavaju vodonik, halogen, trifluormetil, niži alkoksi ili cijan grupu, ili R2 i R2' mogu zajedno formirati grupu -CH=CH-CH=CH- koja je opciono supstituisana sa jednim ili dva supstituenta odabrana između nižeg alkila ili niže alkoksi-grupe, R3 vodonik, niži alkil ili formira cikloalkil-grupu, R4 vodonik, -N(R5)2, -N(R5) (CH2)nOH, -N(R5)S(O)2-niži alkil, -N (R5)S(O)2-fenil, -N=CH-N (R5)2, -N(R5)C(O)R5 ili ciklični tercijarni amin grupe R5 nezavisno jedan od drugog označava vodonik, C3-6-cikloalkil, benzil ili niži alkil, R6 vodonik, hidroksi, niži alkil, -(CH2)nCOO-niži alkil, -N(R5)CO-niži alkil, hidroksi-niži alkil, cijan, (CH2)nO(CH2)nOH, -CHO ili petočlanu ili šestočlanu heterocikličnu grupu koja je opciono vezana preko alkilenske grupe X -C(O)N(R5)-, -(CH2)mO-, -(CH2)mN(R5)-, -N(R5)C(O)- ili -N(R5)(CH2)m-, n 0-4 i m 1 ili 2, i na njihove farmaceutski prihvatljive kiselinske adicione soli. Jedinjenja formule I pokazuju visok afinitet prema NK-1 receptoru. Ona se mogu primeniti za lečenje bolesti koje su u vezi sa antagonistima NK-1 receptora.

公开(公告)号：HRP20080306A2

公开(公告)日：2008-11-30

申请号：HRP20080306

申请日：2008-06-27

Applicant: HOFFMANN LA ROCHE

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

IPC: C07D213/82 ,  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 ,  C07D401/04 ,  C07D401/12 ,  C07D413/12 ,  C07D413/14

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：DE60014216T2

公开(公告)日：2006-03-02

申请号：DE60014216

申请日：2000-02-15

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

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：DK1035115T3

公开(公告)日：2005-01-24

申请号：DK00102260

申请日：2000-02-15

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

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：DE60014216D1

公开(公告)日：2004-11-04

申请号：DE60014216

申请日：2000-02-15

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

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：BG104187A

公开(公告)日：2000-11-30

申请号：BG10418700

申请日：2000-02-24

Applicant: HOFFMANN LA ROCHE

Inventor： BOAS 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 ,  A61K31/00

Abstract: The compounds show high activity to the NK-1 receptor and can be applied for the treatment of diseases related to the NK-1 receptor antagonists. They have the general formula where R is hydrogen, lower alkyl, halogen or trifluoromethyl; R1 is hydrogen or halogen; or R and R1 can together be -CH=CH-CH=CH-; R2 and R2' individually are hydrogen, halogen, trifluoromethyl, lower alkoxy or cyano; or R2 and R2' together can mean -CH=CH-CH=CH-, optionally substituted by one or two substituents selected from lower alkyl or lower alkoxy; R3 is hydrogen, lower alkyl or forms cycloalkyl group; R4 is hydrogen, -N(R5)(CH2)nOH2, -N(R5)S(O)2-lower alkyl, -N(R5)SO)2-phenyl, -N=CH-N(R5)2, -N(R5)C(O)R5 or cyclic tertiary amine of the group or the group R5 individually from the remaining substituents is hydrogen, C3-6-cycloalkyl, benzyl or lower alkyl; R6 is hydrogen, hydroxy, lower alkyl, -(CH2)nCOO-lower alkyl, -N(R5)CO-lower alkyl, hydroxy-lower alkyl, cyano, -CH2)n(O(CH2)nOH, -CHO or 5- or 6-member heterocyclic group, optionally bound by 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 from 0 to 4; and m is 1 or 2. The invention also relates to their pharmaceutically acceptable adjunctive to acid salts. 11 claims