公开(公告)号：JP2000247957A

公开(公告)日：2000-09-12

申请号：JP2000047003

申请日：2000-02-24

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

Abstract: PROBLEM TO BE SOLVED: To obtain a new 4-phenylpyridine derivative which is a neurokinin 1 receptor antagonist and is useful for pain, headache, Alzheimer's disease, multiple sclerosis, amorphinism relaxation, cardiovascular change, swelling, chronic inflammatory diseases, respiratory diseases, and the like. SOLUTION: A compound of formula I [R is H, a lower alkyl, a lower alkoxy, a halogen or the like; R1 is H or a halogen; R2, R2' are each H, a halogen, trifluoromethyl, a lower alkoxy or cyano, or R and R1, R2 and R2' together form CH=CH-CH=CH which may be substituted by one or more alkyls or the like; R3 is H, a lower alkyl or a cycloalkyl; R4 is H, N(R5)2 (R5 is H, a 3-6C cycloalkyl or the like) or the like; R6 is H, OH, a lower alkyl or the like; X is C(O)N(R5) or the like; (n) is 0-4; (m) is 1 or 2]. For example, N-(3,5-bis-trifluoromethyl-benzyl)-N-methyl-4-o-tolyl-nicotinamide. The compound of formula I is obtained, for example, by reacting a compound of formula II with a compound of formula III.

公开(公告)号：CA2299139C

公开(公告)日：2011-03-29

申请号：CA2299139

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: C07D213/82 ,  A61K20060101 ,  A61K31/44 ,  A61K31/4409 ,  A61K31/4418 ,  A61K31/4427 ,  A61K31/444 ,  A61K31/455 ,  A61K31/496 ,  A61K31/506 ,  A61K31/5377 ,  A61K31/541 ,  A61P1/00 ,  A61P9/00 ,  A61P11/00 ,  A61P11/06 ,  A61P19/02 ,  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 ,  C07D405/12 ,  C07D409/12 ,  C07D413/12 ,  C07D413/14 ,  C07D417/12

Abstract: The present invention relates to compounds of the general formula (see formula I) wherein R is hydrogen, lower alkyl, lower alkoxy, halogen or trifluoromethyl; R1 is hydrogen or halogen; or R and R1, when adjacent, may be together -CH=CH-CH=CH-; R2 and R2' are independently from each other hydrogen, halogen, trifluoromethyl, lower alkoxy or cyano; or R2 and R2', when adjacent, may be together -CH=CH-CH-CH-, optionally substituted by one or two substituents selected from lower alkyl or lower alkoxy; R3 and R3' are each hydrogen, lower alkyl or together with the carbon to which they are attached form a cycloalkyl group; R4 is hydrogen, -N(R)2, -N(R5)(CH2)n OH, -N(R5)S(O)2-lower alkyl, -N(R5)S(O)2--phenyl, -N=CH-N(R5)2, -N(R5)C(O)R5 or a cyclic tertiary amine of the group (see formula II) or the group (see formula III); R5 is, independently from each other, hydrogen, C3-6-cycloalkyl, benzyl or lower alkyl; R6 is hydrogen, hydroxy, lower alkyl, -(CH2)n COO-lower alkyl, -N(R5)CO-lower alkyl, hydroxy-lower alkyl, cyano, -(CH2)n O(CH2)n OH, -CHO or a 5-or 6--membered heterocyclic group, wherein said 5- or 6-membered heterocyclic group is optionally bonded via an alkylene group, X is -C(O)N(R5)-, -(CH2)m O-, -(CH2)m N(R5)-, -N(R5)C(O)-, or -N(R)(CH2)m-; n is 0-4; and m is 1 or 2; with the proviso that the compound is other than 2-(3,5-Bis-trifluoromethyl-phenyl)-N--methyl-N-(6-morpholin-4-yl-4-o-tolyl-pyridin-3-yl)-isobutyramide, 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：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：CZ291514B6

公开(公告)日：2003-03-12

申请号：CZ82599

申请日：1999-03-10

Applicant: HOFFMANN LA ROCHE

Inventor： BOS 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

Abstract: In the present invention there are disclosed pyrazolopyrimidines and pyrazolotriazines of the general formulae I-A and I-B, in which Re1 represents phenyl, being optionally substituted with at least one alkyl containing 1 to 7 carbon atoms; a halogen, alkoxy containing 1 to 7 carbon atoms, tolyl, pyridyl, naphthyl or phenylthio, Re2 represents hydrogen alkyl containing 1 to 7 carbon atoms, alkylthio containing 1 to 7 carbon atoms or hydroxyalkoxy containing 1 to 7 carbon atoms in the alkoxy moiety, Re3 represents amino, alkylamino containing 1 to 7 carbon atoms, dialkylamino containing 1 to 7 carbon atoms in the alkyl moiety, piperazinyl being optionally substituted with at least one alkyl containing 1 to 7 carbon atoms, benzyl, phenyl or hydroxyalkyl containing 1 to 7 carbon atoms in the alkyl moiety; morpholinyl, imidazolyl, (CHi3)i2N(CHi2)inNH-, (CHi3)i2N(CHi2)inO- or morpholinyl-(CHi2)inO-, wherein n is 2 or 3, Re4 represents hydrogen, alkyl containing 1 to 7 carbon atoms or hydroxyalkyl containing 1 to 7 carbon atoms in the alkyl moiety, Re5 represents hydrogen, a halogen, alkyl containing 1 to 7 carbon atoms, cycloalkyl containing 3 to 6 carbon atoms, alkylalkoxy having 1 to 7 carbon atoms in both the moieties, hydroxyalkylalkoxy containing 1 to 7 carbon atoms in both alkyl and alkoxy moieties, (CHi3)i2N(CHi2)inNH-, piperazinyl, being optionally substituted with alkyl containing 1 to 7 carbon atoms; methylpiperazinyl, being optionally substituted with alkyl containing 1 to 7 carbon atoms; morpholinyl, methylmorpholinyl, dialkylamino containing 1 to 7 carbon atoms in the alkyl moiety or dialkylaminoalkyl containing 1 to 7 carbon atoms in both the alkyl moieties or Re4 a Re5 together form the group -(CHi2)im- or CHi2-S-CHi2-, m is 3 or 4, and pharmaceutically acceptable salts thereof. Described is also their use for treating or prevention of central nervous system 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：ES2171109A1

公开(公告)日：2002-08-16

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: Derivados de 4-fenil-piridina. Estos compuestos corresponden a la fórmula general (I) en donde los radicales R, R{sup,1}, R{sup,2}, R{sup,2''}, R{sup,3}, R{sup,4}, X, n y m son como se expresan en las reivindicaciones. Estos compuestos muestran una mayor afinidad por el receptor de NK-1. La invención también se refiere a sales derivadas de los compuestos que sean farmaceúticamente aceptables, a medicamentos que contengan uno o más de estos compuestos, y a un proceso para la preparación de los compuestos. Los productos de la invención se pueden usar para el tratamiento de enfermedades relacionadas con antagonistas del receptor de NK-1.

公开(公告)号：CO5160261A1

公开(公告)日：2002-05-30

申请号：CO00016011

申请日：2000-03-06

Applicant: HOFFMANN LA ROCHE

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

IPC: C07D295/14 ,  A61K31/165 ,  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: Compuestos de la fórmula general en dondeR es hidrógeno, alquilo inferior, alcoxi inferior, halógeno, amino, -N(R6)2 ó trifluorometilo; R1 es hidrógeno, alcoxi inferior o halógeno;R y R1 pueden ser conjuntamente -CH=CH-CH=CH-;R2 es halógeno, alquilo inferior o trifluorometilo;R3 es hidrógeno o alquilo inferior;R4 es hidrógeno o una amina terciaria cíclica, sustituida opcionalmente por alquilo inferior;R5 es hidrógeno, nitro, amino ó -N(R6)2;R6 es hidrógeno o alquilo inferior;X es -C(O)N(R6)-, -(CH2)nO-, -(CH2)nN(R6)-, -N(R6)C(O)- ó -N(R6) (CH2)n-; yn es 1-2;y sales derivadas de una adición ácida farmacéuticamenteaceptables.

公开(公告)号：CO5140088A1

公开(公告)日：2002-03-22

申请号：CO00012296

申请日：2000-02-22

Applicant: HOFFMANN LA ROCHE

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

IPC: C07C211/44 ,  A61K31/03 ,  A61K31/165 ,  A61K31/167 ,  A61K31/44 ,  A61K31/445 ,  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: Compuestos de la fórmula general en dondeR es hidrógeno, alquilo inferior, alcoxi inferior, halógeno o trifluorometilo;R1 es hidrógeno o halógeno; oR y R1 pueden ser conjuntamente -CH=CH-CH=CH-;R2 es hidrógeno, halógeno, trifluorometilo, alcoxi inferior o ciano;R3 es independientemente uno de otro, hidrógeno, alquilo inferior o forma un grupo cicloalquilo;R4 es hidrógeno, halógeno, alquilo inferior, alcoxi inferior, -N(R5)2, -N(R5)S(O)2- alquilo inferior, -N(R5)C(O)R5 o una amina terciaria cíclica del grupo R5 es independientemente uno de otro, hidrógeno, C3-6-cicloalquilo, bencilo o alquilo inferior;R6 es hidrógeno, hidroxi, alquilo inferior, -N(R5)CO-alquilo inferior, hidroxi-alquilo-inferior, ciano, -CHO o un grupo heterocíclico de 5 ó 6 miembros, unido opcionalmente por un grupo alquileno,X es -C(0)N(R5)-, -(CH2)mO-, -(CH2)mN(R5)-,-N(R5)C(0)-, -C(O)O-, ó -N(R5)(CH2)m-;Y es -(CH2)n, -O-, -S-, -S02-, -C(O)- ó -N(R5)-;Z es =N-, -CH= ó -C(CI)=;n es 0-4; ym es 1 ó 2;y sales derivadas de una adición ácida farmacéuticamente aceptables.

公开(公告)号：CO5090847A1

公开(公告)日：2001-10-30

申请号：CO99001735

申请日：1999-01-14

Applicant: HOFFMANN LA ROCHE

Inventor： BOS MICHAEL ,  HUNKELER WALTER ,  RIEMER CLAUS

IPC: C07C309/30 ,  A61K31/00 ,  A61K31/03 ,  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: Compuestos de la fórmula general en donde R1 es hidrógeno; R2 es hidrógeno, trifluorometilo o alquilo inferior; R3 es hidrógeno o amino; o R1 y R2 o R3 y R2 tomados conjuntamente son -CH=CH-CH=CH-; Z es pirimidin-4-ilo, piridin-4-ilo, piridin-2-ilo o fenilo; R4, R5 son cada uno, independientemente, hidrógeno, alquilo inferior, trifluorometilo, halógeno, alcoxilo inferior, nitrilo, amino, alquil-amino inferior, di-alquil-amino inferior, piperazinilo, morfolinilo, pirrolidinilo, vinilo, cicloalquilo de C3-C6, cicloalquenilo de C3-C6, t-butiletinilo, hidroxialquiletinilo, fenil-etinilo, naftilo, tiofenilo o fenilo, que puede estar sustituido por halógeno, alcoxilo inferior, Alquilo inferior, trifluorometilo o nitro o un grupo-NH(CH2)nNR6R7, -N(CH3)(CH2)nNR6R7, -NH(CH2)n-morfolin-4-ilo o NH(CH2)nOH; n es 2-4 R6 y R7 son cada uno, independientemente, hidrógeno o alquilo inferior, Con la salvedad que -cuando Z es pirimidin-4-ilo, R4 es diferente de R5,-cuando Z es piridin-2-ilo, R5 no es alquilo inferior y -cuando Z es fenilo, R4 y uno de R1-R3 son diferentes de hidrógeno, Y a sus sales farmacéuticamente aceptables.

公开(公告)号：HK1031223A1

公开(公告)日：2001-06-08

申请号：HK01101744

申请日：2001-03-12

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 ,  C07D ,  A61K ,  A61P

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：PE01532001A1

公开(公告)日：2001-02-08

申请号：PE0005082000

申请日：2000-05-26

Applicant: HOFFMANN LA ROCHE

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

IPC: A61K31/496 ,  A61K31/505 ,  A61K31/506 ,  A61K31/5377 ,  A61P1/04 ,  A61P1/08 ,  A61P9/00 ,  A61P11/06 ,  A61P17/02 ,  A61P19/02 ,  A61P25/00 ,  A61P25/06 ,  A61P25/16 ,  A61P25/22 ,  A61P25/24 ,  A61P25/28 ,  A61P25/36 ,  A61P27/00 ,  A61P27/02 ,  A61P29/00 ,  A61P37/08 ,  A61P43/00 ,  C07D213/00 ,  C07D239/00 ,  C07D239/28 ,  C07D239/32 ,  C07D239/34 ,  C07D239/38 ,  C07D239/42 ,  C07D239/48 ,  C07D295/00 ,  C07D401/04 ,  C07D403/04

CPC classification number: C07D239/28 ,  C07D239/34 ,  C07D239/38 ,  C07D239/42 ,  C07D239/48 ,  C07D401/04

Abstract: SE REFIERE A DERIVAADOS DE 4-FENIL-PIRIMIDINA DE FORMULA I, DONDE R1 ES H, HALOGENO; R2 ES H, HALOGENO, ALQUILO, ALCOXILO; R1 Y R2 JUNTO A C FORNAN -CH=CH-CH=CH-; R3 ES HALOGENO, TRIFLUOROMETILO, ALQUILO, ALCOXILO; R4 Y R4` SON H, ALQUILO; R5 ES ALQUILO, ALCOXILO, AMINO, FENILO, ENTRE OTROS; n ES 0-2; X ES -CON(R4")-, -NR4"CO-. SON COMPUESTOS PREFERIDOS ACIDO 4-(2-BROMO-FENIL)-2-(4-METIL-PIPERAZIN-1-IL)-PIRIMIDIN-5-CARBOXILICO (3,5-BISTRIFLUORO-METIL-BENCIL))-METIL-AMIDA, ACIDO 4-(2-CLORO-FENIL)-2-(2-DIMETILAMINO-ETIL-AMINO)-PIRIMIDIN-5-CARBOXILICO (3,5-BISTRIFLUOROMETIL-BENCIL)-METIL-AMIDA, ENTRE OTROS. TAMBIEN SE REFIERE A UN PROCEDIMIENTO PARA LA PREPARACION. EL COMPUESTO I ES UN ANTAGONISTA DEL RECEPTOR DE LA NEUROQUININA NK-1 Y PUEDE SER UTIL PARA EL TRATAMIENTO DEL DOLOR, CEFALEA, MIGRANA, ENFERMEDAD DE ALZHEIMER, ANSIEDAD DEPRESION, PSICOSIS