Claims
- 1. A compound of formula I, a pharmaceutically acceptable salt of said compound of formula I, or a trifluoroacetic acid salt of said compound of formula I:
- 2. A compound of claim 1, a pharmaceutically acceptable salt of said compound of claim 1, or a trifluoroacetic acid salt of said compound of claim 1, wherein:
R1 and R2
are independently selected from the group consisting of H, F, Cl, Br, CH3, CF3, SO2CH3, and SO2NH2, provided that R1 and R2 are not both hydrogen; R3 is hydrogen, F or Cl; R4 is hydrogen, alkyl having 1, 2, 3 or 4 carbon atoms, or cyclopropyl; R5 and R6 are hydrogen or together a bond; R7 and R8
together with the two carbon atoms to which R7 and R8 are attached, form a (C5-C10) cycloalkenyl ring which may be unsubstituted or substituted with one or more fluorine atoms; or R7 and R8
together with the two carbon atoms to which R7 and R8 are attached, form a ring of the following formula; 87wherein,
R10 and R11 are independently hydrogen, OH, fluorine or chlorine; R9 and R12 are both hydrogen, or R9 is hydrogen while R12 is F, Cl, Br, CN, COOH, CO—NR13R14, SO2—NR13R14 or —(X)n—CqH2q—Z, or R12 is hydrogen while R9 is F, Cl, Br, CN, COOH, CO—NR13R14, SO2—NR13R14 or —(X)n—CqH2q—Z, wherein
R13 and R14 are independently hydrogen or methyl; n is zero or 1; X is oxygen, NH, N—CH3 or S(O)k; k is zero, 1 or 2; q is zero, 1, 2, 3 or 4; Z is hydrogen or CF3.
- 3. A compound of claim 1, a pharmaceutically acceptable salt of said compound of claim 1, or a trifluoroacetic acid salt of said compound of claim 1, wherein:
R1 and R2 are independently F, Cl, Br, CH3 or CF3; R3 is hydrogen; R4 is hydrogen, methyl or ethyl; R5 and R6 are hydrogen or together are a bond; R7 and R8
together with the two carbon atoms to which R7 and R8 are attached, form a (C5-C10) cycloalkenyl ring which may be unsubstituted or substituted with one or more fluorine atoms; or R7 and R8
together with the two carbon atoms to which R7 and R8 are attached, form a ring of the following formula: 88wherein,
R10 and R11 are independently hydrogen, OH or fluorine; R9 and R12 are both hydrogen, or R9 is hydrogen while R12 is F, Cl, Br or —(X)n—CqH2q—Z, or R12 is hydrogen while R9 is F, Cl, Br or —(X)n—CqH2q—Z, wherein:
n is zero or 1; X is oxygen, NH, N—CH3 or S(O)k; k is zero, 1 or 2; q is zero or 1; and Z is hydrogen or CF3.
- 4. A compound of claim 1, selected from the group consisting of:
trans-R,R-2-chlorine-3N-(3a,4,5,6,7,7a-hexahydro-1H-2-benzimidazolyl)-4-methyl-3-thienylamine, trans-R,R-2-bromo-3N-(3a,4,5,6,7,7a-hexahydro-1H-2-benzimidazolyl)-4-methyl-3-thienylamine, 2-chloro-3N-(2-benzimidazolyl)-4-methyl-3-th ienylamine, 2-bromo-3N-(2-benzimidazolyl)-4-methyl-3-thienylamine, 2-chloro-3N-(4-methyl-2-benzimidazolyl)-4-methyl-3-thienylamine, 2-chloro-3N-(5-fluoro-2-benzimidazolyl)-4-methyl-3-th ienylamine, 2-chloro-3N-(4-chloro-2-benzimidazolylamino)-4-methylthiophene, 2-bromo-3N-(4-chloro-2-benzimidazolylamino)-4-methylthiophene, 2-bromo-3N-(4-fluoro-2-benzimidazolylamino)-4-methylthiophene, 2-chloro-3N-(4-fluoro-2-benzimidazolylamino)-4-methylthiophene, 2-chloro-3N-(4-hydroxy-2-benzimidazolylamino)-4-methylthiophene, (1H-benzimidazol-2-yl)-(2-chloro-4-methylthiophen-3-yl)-methylamine, (2-bromo-4-methylthiophen-3-yl)-(5-fluoro-1H-benzimidazol-2-yl)-amine, 2,4-dichloro-3N-(2-benzimidazolylamino)thiophen, 2-bromo-4-chloro-3N-(2-benzimidazolylamino)thiophen, 2,4-dichloro-3N-(4-methyl-2-benzimidazolyl-amino)thiophen, trans-R,R-2,4-dichloro-3N-(3a,4,5,6,7,7a-hexahydro-1H-2-benzimidazolyl)-3-thienylamin, 2,4-dichloro-3N-(4-chloro-2-benzimidazolyl-amino)thiophen and 2-chloro-3N-(2-benzimidazolylamino)-4-methylthiophene.
- 5. A pharmaceutically acceptable salt of a compound of claim 4.
- 6. A trifluoroacetic acid salt of a compound of claim 4.
- 7. A pharmaceutical composition comprising a compound of claim 1.
- 8. A pharmaceutical composition comprising a pharmaceutically acceptable salt of a compound of claim 1.
- 9. A pharmaceutical composition comprising a trifluoroacetic acid salt of a compound of claim 1.
- 10. A method of treatment or prophylaxis with a pharmaceutical composition comprising a compound of formula I and/or a pharmaceutically acceptable salt thereof of claim 1 for respiratory disorders, preferably, sleep apnea and snoring, acute and chronic renal diseases, preferably, acute kidney failure or chronic kidney failure, disorders of intestinal function, for high blood pressure, preferably, essential hypertension, disorders of the central nervous system, preferably, a disorder which is the result of CNS overexcitability, disorders of the central nervous system, preferably, anxiety, depressions and psychoses, acute and chronic damage and disorders of organs or tissue caused by ischemic events or by reperfusion events and indirect sequelae thereof, arrhythmias, atherosclerosis, hypercholesterolemia, or diseases in which cell proliferation is a primary or secondary cause, cancer, prostate hypertrophy or prostate hyperplasia, fibrotic disorders of internal organs, cardiac insufficiency, congestive heart failure, of thromboses, of disorders of gall function, of infection by ectoparasites, of disorders which are the result of endothelial dysfunction, of intermittent claudication, of protozoa disorders, in particular malaria, states of shock, diabetes and late diabetic damage, acute or chronic inflammatory disorders.
- 11. A method of treatment or prophylaxis according to claim 10, wherein said pharmaceutical composition further comprises one or more other drugs or active compounds.
- 12. A method of manufacturing a medicament by using a compound of formula I and/or a pharmaceutically acceptable salt thereof of claim 1, alone or in combination with one or more other drugs or active compounds, said medicament being used for the treatment or prophylaxis of respiratory disorders, preferably, respiratory disorders associated with sleeping.
- 13. A method of manufacturing a medicament according to claim 12, wherein said medicament is used for the treatment or prophylaxis of snoring.
- 14. A method of manufacturing a medicament according to claim 12, wherein said medicament is used the treatment or prophylaxis of acute and chronic renal diseases, preferably, acute kidney failure or chronic kidney failure.
- 15. A method of manufacturing a medicament according to claim 12, wherein said medicament is used for the treatment or prophylaxis of disorders of intestinal function.
- 16. A medicament comprising an effective amount of a compound of formula I and/or a pharmaceutically acceptable salt thereof of claim 1 together with pharmaceutically acceptable carriers and additives, said medicament being proper for human, veterinary or phytoprotective use,
- 17. A medicament of claim 16, further comprising one or more other pharmacologically active compounds or drugs.
Priority Claims (1)
Number |
Date |
Country |
Kind |
10224892.3 |
Jun 2002 |
DE |
|
Parent Case Info
[0001] This application claims benefit of U.S. Provisional Application No. 60/415,788 filed Oct. 3, 2002, and German Application No. 10224892.3, filed Jun. 4, 2002.
Provisional Applications (1)
|
Number |
Date |
Country |
|
60415788 |
Oct 2002 |
US |