Claims
- 1. A compound according to the formula
- 2. A compound according to claim 1 wherein:
R1 and R2 are independently straight chain alkyls of 1 to 3 carbon atoms, or branched alkyls of 3 to 6 carbons atoms; R3 is an aryl or heteroaryl moiety, wherein aryl is defined as phenyl, or naphthalene, and heteroaryl is defined as pyridine, pyrazine, pyrimidine, pyridazine, and triazine, each optionally substituted with 1 to 2 groups selected independently from C1-C6 alkyl, C1-C6 alkoxy, cyano, F, Cl, Br, C1-C6 alkylthio, CO2R1, CONH2, OH, NH2, and NO2; n is 0 or 1; R4 is a straight chain alkyl group of 1 to 6 carbons atoms, or a branched alkyl of 3 to 6 carbons; and all crystalline forms or a pharmaceutically acceptable salt thereof.
- 3. A compound according to claim 1 wherein:
R1 and R2 are independently straight chain alkyls of 1 to 3 carbon atoms; R3 is an phenyl or pyridine, optionally substituted with 0 to 2 groups, selected independently from C1-C6 alkyl, C1-C6 alkoxy, cyano, F, Cl, Br, C1-C6, alkylthio, CO2R1, CONH2, OH, NH2, and NO2; R4 is a straight chain alkyl group of 3 to 6 carbons atoms, or a branched alkyl of 3 to 6 carbons; and all crystalline forms or a pharmaceutically acceptable salt thereof.
- 4. A compound according to claim 1 which is selected from the group consisting of:
N(3)-(2,2-dimethyl-propyl)-2,5-dimethyl-N(4)-pyridin4-ylmethyl-2H-pyrazole-3,4-diamine or a pharmaceutically acceptable salt thereof; 4-{[5-(2,2-dimethyl-propylamino)-1,3-dimethyl-1H-pyrazol4-ylamino]-methyl}-benzonitrile or a pharmaceutically acceptable salt thereof; N(3)-(2 ,2-dimethyl-propyl)-N(4)-(4-fluoro-benzyl)-2,5-dimethyl-2H-pyrazole-3,4-diamine or a pharmaceutically acceptable salt thereof; N(4)-(2,4-dichloro-benzyl)-N(3)-(2,2-dimethyl-propyl)-2,5-dimethyl-2H-pyrazole-3,4-diamine or a pharmaceutically acceptable salt thereof; 4-{[5-(2,2-dimethyl-butylamino)-1,3-dimethyl-1H-pyrazol4-ylamino]-methyl}-benzonitrile or a pharmaceutically acceptable salt thereof; N(4)-(2,4-difluoro-benzyl)-N(3)-(2,2-dimethyl-propyl)-2,5-dimethyl-2H-pyrazole-3,4-diamine or a pharmaceutically acceptable salt thereof; N(3)-(2,2-dimethyl-propyl)-2,5-dimethyl-N(4)-pyridin-3-ylmethyl-2H-pyrazole-3,4-diamine or a pharmaceutically acceptable salt thereof; N(3)-(2,2-dimethyl-propyl)-2,5-dimethyl-N(4)-(2,4,6-trimethyl-benzyl)-2H-pyrazole-3,4-diamine or a pharmaceutically acceptable salt thereof; N(3)-(2,2-dimethyl-butyl)-2,5-dimethyl-N(4)-pyridin-4-ylmethyl-2H-pyrazole-3,4-diamine or a pharmaceutically acceptable salt thereof; N(4)-benzyl-N(3)-(2,2-dimethyl-butyl)-2,5-dimethyl-2H-pyrazole-3,4-diamine or a pharmaceutically acceptable salt thereof; N(3)-(2,2-dimethyl-propyl)-2,5-dimethyl-N(4)-phenyl-2H-pyrazole-3,4-diamine or a pharmaceutically acceptable salt thereof; N(4)-(4-chloro-2-methyl-phenyl)-N(3)-(2,2-dimethyl-propyl)-2,5-dimethyl-2H-pyrazole-3,4-diamine or a pharmaceutically acceptable salt thereof; 4-[5-(2,2-dimethyl-propylamino)-1,3-dimethyl-1H-pyrazol4-ylamino]-benzonitrile or a pharmaceutically acceptable salt thereof; and N(4)-(4-chloro-phenyl)-N(3)-(2,2-dimethyl-propyl)-2,5-dimethyl-2H-pyrazole-3,4-diamine or a pharmaceutically acceptable salt thereof.
- 5. A method of treating disorders associated with spastic or excessive smooth muscle contractions of the urinary tract, the gastro-intestinal tract, or asthma or hair loss in a mammal which comprises administration to said mammal of a therapeutically effective amount of a compound according to claim 1.
- 6. The method according to claim 5 wherein the disorder treated is urge urinary incontinence.
- 7. The method according to claim 5 wherein the disorder treated is irritable bowel syndrome.
- 8. A method of treating diseases in mammals amenable to treatment with potassium channel activators which comprises administration to such a mammal of a therapeutically effective amount of a compound according to claim 1.
- 9. The method according to claim 8 wherein the disease treated is peripheral vascular disease, hypertension, congestive heart failure, stroke, anxiety, cerebral anoxia or other neurodegenerdtive disorder.
- 10. A pharmaceutical composition comprising a pharmaceutically acceptable carrier and a therapeutically effective amount of a compound according to claim 1.
- 11. A process for the preparation of a compound according to claim 1 which comprises reacting a compound of formula II
Parent Case Info
[0001] This application claims the benefit of U.S. Provisional Application No. 60/099,348, filed Jun. 8, 1998.
Provisional Applications (1)
|
Number |
Date |
Country |
|
60099384 |
Sep 1998 |
US |
Divisions (2)
|
Number |
Date |
Country |
Parent |
09327065 |
Jun 1999 |
US |
Child |
09963254 |
Sep 2001 |
US |
Parent |
09655891 |
Sep 2000 |
US |
Child |
09963254 |
Sep 2001 |
US |