ECSP003359A - DERIVATIVES OF 4- PHENYL PIRIDINE - Google Patents
DERIVATIVES OF 4- PHENYL PIRIDINEInfo
- Publication number
- ECSP003359A ECSP003359A ECSP003359A ECSP003359A EC SP003359 A ECSP003359 A EC SP003359A EC SP003359 A ECSP003359 A EC SP003359A EC SP003359 A ECSP003359 A EC SP003359A
- Authority
- EC
- Ecuador
- Prior art keywords
- lower alkyl
- hydrogen
- halogen
- group
- phenyl
- Prior art date
Links
- 125000000217 alkyl group Chemical group 0.000 abstract 8
- 229910052739 hydrogen Inorganic materials 0.000 abstract 7
- 239000001257 hydrogen Substances 0.000 abstract 7
- 125000004435 hydrogen atom Chemical group [H]* 0.000 abstract 7
- 125000003545 alkoxy group Chemical group 0.000 abstract 3
- 229910052736 halogen Inorganic materials 0.000 abstract 3
- 150000002367 halogens Chemical class 0.000 abstract 3
- 102000002002 Neurokinin-1 Receptors Human genes 0.000 abstract 2
- 108010040718 Neurokinin-1 Receptors Proteins 0.000 abstract 2
- 150000001875 compounds Chemical class 0.000 abstract 2
- 125000004093 cyano group Chemical group *C#N 0.000 abstract 2
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 abstract 2
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 abstract 1
- 125000002373 5 membered heterocyclic group Chemical group 0.000 abstract 1
- 125000004070 6 membered heterocyclic group Chemical group 0.000 abstract 1
- 239000002253 acid Substances 0.000 abstract 1
- 125000002947 alkylene group Chemical group 0.000 abstract 1
- 125000001797 benzyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])* 0.000 abstract 1
- -1 cyclic tertiary amine Chemical class 0.000 abstract 1
- 125000000753 cycloalkyl group Chemical group 0.000 abstract 1
- 201000010099 disease Diseases 0.000 abstract 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 abstract 1
- 125000002887 hydroxy group Chemical group [H]O* 0.000 abstract 1
- 239000002464 receptor antagonist Substances 0.000 abstract 1
- 229940044551 receptor antagonist Drugs 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 125000001424 substituent group Chemical group 0.000 abstract 1
Landscapes
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Abstract
La presente invención se refiere a compuestos de la fórmula general (gráficos), en donde R es hidrógeno, alquilo inferior, alcoxi inferior, halógeno o trifluorometilo; R1 es hidrógeno o halógeno; o R y R1 pueden ser conjuntamente -CH=CH-CH=CH-; R2 y R2¿son independientemente, hidrógeno, halógeno, trifluorometilo, 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 hidrógeno, alquilo inferior o forma un grupo cicloalquilo; R1 es hidrógeno , -N(R5)S (O)2- fenilo, -N=CH-N(R5)2,-N(R5)C(O)R5 o una amina terciaria ciclica del grupo (gráfico), R5 es independientemente, hidrógeno, C3-6 cicloalquilo, bencilo o alquilo inferior; R6 es hidrógeno, hidroxi, alquilo inferior, -(CH2)n COO- alquilo inferior, -N(R5)CO-alquilo inferior, hidroxi-alquilo-inferior, ciano, -(CH2)n O(CH2)n OH, -CHO o un grupo heterociclico de 5 o 6 miembros, unido opcionalmente porun grupo alquileno, X es -C(O)N(R5)-, -(CH2)mO-, -(CH2)mN(R5)-, -N(R5)C(O)-, ó -N(R5) (CH2)m-; n es 0-4; y m es 1 ó 2; y sales derivadas de una adición ácida farmacéuticamente aceptables. Los compuestos de la fórmula I muestran una mayor afinidad por el receptor de NK-1. Estos se pueden usar para el tratamiento de enfermedades que están relacionadas con antagonistas del recptor de NK-1The present invention relates to compounds of the general formula (graphics), wherein R is hydrogen, lower alkyl, lower alkoxy, halogen, or trifluoromethyl; R1 is hydrogen or halogen; or R and R1 can be together -CH = CH-CH = CH-; R2 and R2¿ are independently hydrogen, halogen, trifluoromethyl, cyano or lower alkoxy; or R2 and R2¿ can be together -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 a cycloalkyl group; R1 is hydrogen, -N (R5) S (O) 2-phenyl, -N = CH-N (R5) 2, -N (R5) C (O) R5 or a cyclic tertiary amine from the group (graph), R5 it is independently 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, optionally linked 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 0-4; and m is 1 or 2; and salts derived from a pharmaceutically acceptable acid addition. The compounds of formula I show a higher affinity for the NK-1 receptor. These can be used to treat diseases that are related to NK-1 receptor antagonists.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| ECSP003359 ECSP003359A (en) | 2000-02-24 | 2000-02-24 | DERIVATIVES OF 4- PHENYL PIRIDINE |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| ECSP003359 ECSP003359A (en) | 2000-02-24 | 2000-02-24 | DERIVATIVES OF 4- PHENYL PIRIDINE |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| ECSP003359A true ECSP003359A (en) | 2000-09-22 |
Family
ID=42040990
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ECSP003359 ECSP003359A (en) | 2000-02-24 | 2000-02-24 | DERIVATIVES OF 4- PHENYL PIRIDINE |
Country Status (1)
| Country | Link |
|---|---|
| EC (1) | ECSP003359A (en) |
-
2000
- 2000-02-24 EC ECSP003359 patent/ECSP003359A/en unknown
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