ECSP003505A - DERIVATIVES OF 4-PHENYL- PIRIMIDINE - Google Patents
DERIVATIVES OF 4-PHENYL- PIRIMIDINEInfo
- Publication number
- ECSP003505A ECSP003505A ECSP003505A ECSP003505A EC SP003505 A ECSP003505 A EC SP003505A EC SP003505 A ECSP003505 A EC SP003505A EC SP003505 A ECSP003505 A EC SP003505A
- Authority
- EC
- Ecuador
- Prior art keywords
- lower alkyl
- hydrogen
- halogen
- alkyl
- phenyl
- Prior art date
Links
- 125000000217 alkyl group Chemical group 0.000 abstract 10
- 229910052739 hydrogen Inorganic materials 0.000 abstract 4
- 239000001257 hydrogen Substances 0.000 abstract 4
- 125000003545 alkoxy group Chemical group 0.000 abstract 3
- 229910052736 halogen Chemical group 0.000 abstract 3
- 150000002367 halogens Chemical group 0.000 abstract 3
- -1 amino, phenyl Chemical group 0.000 abstract 2
- 150000001875 compounds Chemical class 0.000 abstract 2
- 125000004435 hydrogen atom Chemical group [H]* 0.000 abstract 2
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 abstract 1
- 102000002002 Neurokinin-1 Receptors Human genes 0.000 abstract 1
- 108010040718 Neurokinin-1 Receptors Proteins 0.000 abstract 1
- 239000002253 acid Substances 0.000 abstract 1
- 125000004390 alkyl sulfonyl group Chemical group 0.000 abstract 1
- 125000004414 alkyl thio group Chemical group 0.000 abstract 1
- 125000000440 benzylamino group Chemical group [H]N(*)C([H])([H])C1=C([H])C([H])=C([H])C([H])=C1[H] 0.000 abstract 1
- 125000004432 carbon atom Chemical group C* 0.000 abstract 1
- 201000010099 disease Diseases 0.000 abstract 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 abstract 1
- 150000002431 hydrogen Chemical group 0.000 abstract 1
- 125000000587 piperidin-1-yl group Chemical group [H]C1([H])N(*)C([H])([H])C([H])([H])C([H])([H])C1([H])[H] 0.000 abstract 1
- 125000004076 pyridyl group Chemical group 0.000 abstract 1
- 125000000714 pyrimidinyl group Chemical group 0.000 abstract 1
- 102000005962 receptors Human genes 0.000 abstract 1
- 108020003175 receptors Proteins 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 abstract 1
Landscapes
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
Abstract
La presente invención se refiere a compuestos de la fórmula general (gráfico), en donde R1 es hidrógeno ó halógeno; R2 es hidrógeno, halógeno, alquilo inferior o alcoxilo inferior; R1 y R2 pueden ser junto con los dos átomos de carbono del anillo -CH=CH-CH=CH-, R3 es halógeno, trifluorometilo, alquilo inferior ó alcoxilo inferior; R4/R4¿son independientemente uno de otro hidrógeno o alquilo inferior; R5 es alquilo inferior, alcoxilo inferior, amino, fenilo, hidroxi-alquilo inferior, ciano-alquilo inferior, carbamoílo-alquilo inferior, piridilo, pirimidilo, (CH2)n -piperazinilo, el cual se encuentra sustituido opcionalmente por uno o dos grupos alquilo inferior ó por hidroxi-alquilo inferior, -(CH2)n-morfolino, (CH2)n-piperidinilo, -(CH2)n+1-imidazolilo, alquilo inferior-sulfanilo, alquilo inferior-sulfonilo, bencilamino -NH-(CH2)n+1N(R4¿¿)2, (CH2)n+1N(R4¿¿)2, -O-(CH2)n+1-morfolino, -O-(CH2)n+1-piperidinilo ó -O-(CH2)n+1N(R4¿¿)2, en donde R4 es hidrógeno ó alquilo inferior; y n es0-2; X es -C(O)N(R4¿¿) - ó -N(R4¿¿)C(O)-; y sales derivadas de una adición ácida farmacéuticamente aceptables. Se ha demostrado que los compuestos anteriormente mencionados tienen una buena afinidad por el receptor de NK-1 y por lo tanto, pueden ser utilizados para el tratamiento de enfermedades relacionadas con este receptor.The present invention relates to compounds of the general formula (graph), wherein R1 is hydrogen or halogen; R2 is hydrogen, halogen, lower alkyl, or lower alkoxy; R1 and R2 can be together with the two carbon atoms of the ring -CH = CH-CH = CH-, R3 is halogen, trifluoromethyl, lower alkyl or lower alkoxy; R4 / R4¿ are independently of each other hydrogen or lower alkyl; R5 is lower alkyl, lower alkoxy, amino, phenyl, hydroxy-lower alkyl, cyano-lower alkyl, carbamoyl-lower alkyl, pyridyl, pyrimidyl, (CH2) n -piperazinyl, which is optionally substituted by one or two alkyl groups lower or by hydroxy-lower alkyl, - (CH2) n-morpholino, (CH2) n-piperidinyl, - (CH2) n + 1-imidazolyl, lower alkyl-sulfanyl, lower alkyl-sulfonyl, benzylamino -NH- (CH2) n + 1N (R4¿¿) 2, (CH2) n + 1N (R4¿¿) 2, -O- (CH2) n + 1-morpholino, -O- (CH2) n + 1-piperidinyl or -O- (CH2) n + 1N (R4¿¿) 2, where R4 is hydrogen or lower alkyl; and n is 0-2; X is -C (O) N (R4¿¿) - or -N (R4¿¿) C (O) -; and salts derived from a pharmaceutically acceptable acid addition. The aforementioned compounds have been shown to have a good affinity for the NK-1 receptor and therefore can be used for the treatment of diseases related to this receptor.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| ECSP003505 ECSP003505A (en) | 2000-05-31 | 2000-05-31 | DERIVATIVES OF 4-PHENYL- PIRIMIDINE |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| ECSP003505 ECSP003505A (en) | 2000-05-31 | 2000-05-31 | DERIVATIVES OF 4-PHENYL- PIRIMIDINE |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| ECSP003505A true ECSP003505A (en) | 2000-12-19 |
Family
ID=42041131
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ECSP003505 ECSP003505A (en) | 2000-05-31 | 2000-05-31 | DERIVATIVES OF 4-PHENYL- PIRIMIDINE |
Country Status (1)
| Country | Link |
|---|---|
| EC (1) | ECSP003505A (en) |
-
2000
- 2000-05-31 EC ECSP003505 patent/ECSP003505A/en unknown
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