公开(公告)号：NO820125A

公开(公告)日：1982-07-19

申请号：NO820125

申请日：1982-01-15

Applicant: HOFFMANN LA ROCHE

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

IPC: C07D295/02 ,  A61K31/00 ,  A61P37/08 ,  C07C1/00 ,  C07C13/547 ,  C07C17/00 ,  C07C17/16 ,  C07C17/26 ,  C07C22/04 ,  C07C27/00 ,  C07C33/34 ,  C07C35/37 ,  C07C67/00 ,  C07C301/00 ,  C07C303/22 ,  C07C303/32 ,  C07C309/63 ,  C07D207/04 ,  C07D295/03 ,  C07D

CPC classification number: C07D295/03 ,  C07C2603/32

公开(公告)号：RS50194B

公开(公告)日：2009-05-06

申请号：YUP9500

申请日：2000-02-22

Applicant: HOFFMANN LA ROCHE

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

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: Jedinjenja opšte formuleu kojoj označavaju R vodonik, C1-7-alkil, C1-7-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, C1-7-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 C1-7-alkila ili C1-7-alkoksi-grupe, R3 vodonik, C1-7-alkil ili formira c3-6-cikloalkil-grupu, R4 vodonik, -N(R5)2, -N(R5)(CH2)nOH, -N(R5)S(O)2-C,.7-alkil, -N(R5)S(O)2-fenil, -N=CH-N(R5)2, -N(R5)C(O)R5 ili ciklični tercijarni amin grupe pri čemu je ciklični tercijarni amin odabran iz grupe koja se sastoji od pirol-l-ila, imidazol-l-ila, piperidin-l-ila, piperazin-l-ila, morfolin-4-ila, tiomorfolin-4-ila, l-okso-tiomorfolin-4-ila ili 1,1-diokso-tiomorfolin-4-ila, R5 nezavisno jedan od drugog označava vodonik, c3-6-cikloalkil, benzil ili C1-7-alkil, R6 vodonik. hidroksi, C1-7-alkil, -(CH2)nCOO-C1-7-alkil, -N(R5)CO-C1-7-alkil, hidroksi-C1-7-alkil, cijan, -(CH2)nO(CH2)nOH, -CHO ili petočlanu ili šestočlanu heterocikličnu grupu koja je odabrana iz grupe koja se sastoji od piridinila, pirimidinila, oksadiazolila, triazolila, tetrazolila, tiazolila, tienila, furila, piranila, pirolila, imidazolila, pirazolila, izotiazolila, piperazinila, ili piperidila, koji su opciono vezani preko alkilenske grupe, X -(CH2)mO-, -(CH2)mN(R5)-, -N(R5)C(O)- ili -N(R5)(CH2)m-, n 0 -4 i m 1 ili 2, i njihove farmaceutski prihvatljive kiselinske adicione soli. Prijava sadrži još 6 patentnih zahteva.

公开(公告)号：HRP20000097B1

公开(公告)日：2008-12-31

申请号：HRP20000097

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: A61K31/44 ,  A61K20060101 ,  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：AR062949A2

公开(公告)日：2008-12-17

申请号：ARP070104196

申请日：2007-09-24

Applicant: HOFFMANN LA ROCHE

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

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: Derivados de 4-fenil-piridina de formula general (1) en donde R es hidrogeno, alquilo C1-7, alcoxi C1-7, 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, trifluorometilo, ciano o alcoxi C1-7; o R2 y R2' pueden ser conjuntamente -CH=CH-CH=CH-, sustituido opcionalmente por uno o dos sustituyentes seleccionados de alquilo C1-7 o de alcoxi C1-7;.R3 es hidrogeno, alquilo C1-7 o forma un grupo cicloalquilo C3-6; R4 es hidrogeno, -N(R5)2, -N(R5)(CH2)nOH, -N(R5)S(O)2-alquilo C1-7, -N(R5)S(O)2-fenilo, -N=CH-N(R5)2, -N(R5)C(O)R5 o una amina terciaria cíclica del grupo de formula (2) o (3) en donde la amina terciaria cíclica se selecciona del grupo constituido por pirrol-1-ilo, imidazol-1-ilo, piperidin-1-ilo, piperazin-1-ilo, morfolin-4-ilo, tiomorfolin-4-ilo, 1-oxo-tiomorfolin-4-ilo o 1,1-dioxo-tiomorfolin-4-ilo; R5 es independientemente, hidrogeno, cicloalquilo C3-6, bencilo o alquilo C1-7; R6 es hidrogeno, hidroxi, alquilo C1-7, -(CH2)nCOO-alquilo C1-7, ciano, -(CH2)n O(CH2)nOH, -CHO o un grupo heterocíclico de 5 o 6 miembros, seleccionado del grupo constituido por piridinilo, pirimidinilo, oxadiazolilo, triazolilo, tetrazolilo, tiazolilo, tienilo, furilo, piranilo, pirrolilo, imidazolilo, pirazolilo, isotiazolilo, piperazinilo o piperidilo, unido opcionalmente por un grupo alquileno, X es -C(O)N(R5)-, n es 0-4; y m es 1 o 2; y sales de adicion ácida farmacéuticamente aceptables de los mismos

公开(公告)号：JO2294B1

公开(公告)日：2005-09-12

申请号：JOP20000014

申请日：2000-02-22

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：JO2294B

公开(公告)日：2005-09-12

申请号：JO200014

申请日：2000-02-22

Applicant: HOFFMANN LA ROCHE

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

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：AT277905T

公开(公告)日：2004-10-15

申请号：AT00102260

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：FR2790473B1

公开(公告)日：2004-04-02

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：ES2171109B2

公开(公告)日：2003-09-16

申请号：ES200000418

申请日：2000-02-23

Applicant: HOFFMANN LA ROCHE

Inventor： BOS MICHAEL ,  BRANCA QUIRICO ,  GALLEY GUIDO ,  GODEL THIERRY ,  HOFFMANN TORSTEN ,  HUNKELER WALTER

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 ,  C07D413/04

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：SV2002000024A

公开(公告)日：2002-01-23

申请号：SV2000000024

申请日：2000-02-23

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 ,  A61K31/445 ,  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 ,  C07D211/38 ,  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: LA PRESENTE INVENCION SE REFIERE A COMPUESTOS DE LA FORMULA GENERAL, VER FORMULA, EN DONDER ES HIDROGENO, ALQUILO INFERIOR, ALCOXI INFERIOR, HALOGENO O TRIFLUOROMETILO;R1 ES HIDROGENO O HALOGENO; OR Y R1 PUEDEN SER CONJUNTAMENTE -CH=CH-CH=CH-;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 CICLICA DEL GRUPO, VER FORMULA, 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 HETEROCICLICO 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; YM ES 1 O 2;Y SALES DERIVADAS DE UNA ADICION ACIDA FARMACEUTICAMENTE ACEPTABLES. LOS COMPUESTOS DE LA FORMULA I MUESTRAN UNA MAYOR AFINIDAD POR EL RECEPTOR DE NK-1. ESTOS SE PUEDEN USAR PARA EL TRATAMIENTO DE ENFERMEDADES QUE ESTEN RELACIONADAS CON ANTAGONISTAS DEL RECEPTOR DE NK-1.