ECSP003506A - DERIVATIVES OF 5-PHENYL- PIRIMIDINE - Google Patents
DERIVATIVES OF 5-PHENYL- PIRIMIDINEInfo
- Publication number
- ECSP003506A ECSP003506A ECSP003506A ECSP003506A EC SP003506 A ECSP003506 A EC SP003506A EC SP003506 A ECSP003506 A EC SP003506A EC SP003506 A ECSP003506 A EC SP003506A
- Authority
- EC
- Ecuador
- Prior art keywords
- lower alkyl
- hydrogen
- halogen
- receptor
- compounds
- Prior art date
Links
- 125000000217 alkyl group Chemical group 0.000 abstract 6
- 229910052739 hydrogen Inorganic materials 0.000 abstract 5
- 239000001257 hydrogen Substances 0.000 abstract 5
- 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
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 abstract 2
- -1 amino, hydroxyl Chemical group 0.000 abstract 2
- 150000001875 compounds Chemical class 0.000 abstract 2
- 125000004435 hydrogen atom Chemical group [H]* 0.000 abstract 2
- 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
- 125000002768 hydroxyalkyl group Chemical group 0.000 abstract 1
- 125000004193 piperazinyl group 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
- 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)
Abstract
La invención se refiere a compuestos de fórmula general en donde R1 es hidrógeno o halogeno; R2 es hidrógeno, halógeno, alquilo inferior o alcoxilo inferior; R3 es halógeno, trifluorometilo, alcoxilo inferior o alquilo inferior; R4/R4¿son independientemente entre si, hidrógeno o alquilo inferior; R6 es alquilo inferior, alcoxilo inferior, amino, hidroxilo, hidroxialquilo inferior, -(CH2)n, piperazinilo, -(CH2)n -morfolinilo opcionalmente sustituido con alquilo inferior, -(CH2)n+1-imidazolilo, -O-(CH2)n+1 -morfolino, -O-(CH2)n+1-piperidinilo, alquilo inferior-sulfanilo, alquilo inferior-sulfonilo, bencilamino, -NH-(CH2)n+1N(R4¿¿)2, -(CH)n -NH-(CH2)n+1N(R4¿¿)2, -(CH2)n+1N(R4¿¿)2 ó -O-(CH2)n+1 N(R4¿¿)2 en donde R4¿¿ es hidrógeno o alquilo inferior; R6 es hidrógeno; R2 y R6 ó R1 y R6 pueden ser juntamente con los dos átomos de carbono del anillo, -CH=CH-CH=CH-, con la condición de que n para R1 sea 1; n es independientemente 0-2; y X es -C(O)N(R4¿¿)- ó N(R4¿¿)C(O)-; y las sales de adición ácida farmacéuticamente aceptables de los mismos. Los compuestos de fórmula I tienen una elevada afinidad para el receptor de la NK-1. Son por lo tanto, de utilidad para el tratamiento de enfermedades que están relacionadas con este receptor.The invention relates to compounds of the general formula wherein R1 is hydrogen or halogen; R2 is hydrogen, halogen, lower alkyl, or lower alkoxy; R3 is halogen, trifluoromethyl, lower alkoxy or lower alkyl; R4 / R4¿ are independently of one another hydrogen or lower alkyl; R6 is lower alkyl, lower alkoxy, amino, hydroxyl, hydroxyalkyl lower, - (CH2) n, piperazinyl, - (CH2) n -morpholinyl optionally substituted with lower alkyl, - (CH2) n + 1-imidazolyl, -O- ( CH2) n + 1 -morpholino, -O- (CH2) n + 1-piperidinyl, lower alkyl-sulfanyl, lower alkyl-sulfonyl, benzylamino, -NH- (CH2) n + 1N (R4¿¿) 2, - ( CH) n -NH- (CH2) n + 1N (R4¿¿) 2, - (CH2) n + 1N (R4¿¿) 2 or -O- (CH2) n + 1 N (R4¿¿) 2 in where R4¿¿ is hydrogen or lower alkyl; R6 is hydrogen; R2 and R6 or R1 and R6 can be together with the two carbon atoms of the ring, -CH = CH-CH = CH-, provided that n for R1 is 1; n is independently 0-2; and X is -C (O) N (R4¿¿) - or N (R4¿¿) C (O) -; and the pharmaceutically acceptable acid addition salts thereof. The compounds of formula I have a high affinity for the NK-1 receptor. They are therefore useful for the treatment of diseases that are related to this receptor.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| ECSP003506 ECSP003506A (en) | 2000-05-31 | 2000-05-31 | DERIVATIVES OF 5-PHENYL- PIRIMIDINE |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| ECSP003506 ECSP003506A (en) | 2000-05-31 | 2000-05-31 | DERIVATIVES OF 5-PHENYL- PIRIMIDINE |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| ECSP003506A true ECSP003506A (en) | 2000-12-19 |
Family
ID=42041132
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ECSP003506 ECSP003506A (en) | 2000-05-31 | 2000-05-31 | DERIVATIVES OF 5-PHENYL- PIRIMIDINE |
Country Status (1)
| Country | Link |
|---|---|
| EC (1) | ECSP003506A (en) |
-
2000
- 2000-05-31 EC ECSP003506 patent/ECSP003506A/en unknown
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