Patent ID: 6509330
Filing Date: 2003-01-21
Classification: A61K,A61P,C07K

Abstract:
A method of treating hypertension and/or congestive heart failure, which comprises administering to a mammalian species a therapeutically effective amount of a compound of the formula or a pharmaceutically acceptable salt thereof wherein in the moiety â€œ&par;â€  denotes a single bond or a double bond, and the R group may be in the cis or trans configuration;R and R* are the same or different and are independently selected from H, alkyl, alkenyl, aryl-(CH2)pâ€”, heteroaryl-(CH2)pâ€”, or cycloheteroalkyl-(CH2)pâ€”; R1 is H or â€”COR2 where R2 is alkyl, aryl-(CH2)pâ€”, cycloheteroalkyl-(CH2)pâ€”, heteroaryl-(CH2)pâ€”, alkoxy or cycloalkyl-(CH2)pâ€”; p is 0 or an integer from 1 to 8; and A is R4 is OH, Oalkyl, Oâ€”(CH2)p-heteroaryl, â€”Oâ€”(CH2)p-aryl or â€ƒor NR1(R2) where R1 and R2 are independently H, alkyl, aryl, aryl-(CH2)p or heteroaryl; R14 is hydrogen, alkyl, cycloalkyl, or phenyl; R15 is hydrogen, alkyl, alkoxy or phenyl; R16 is alkyl or aryl-(CH2)mâ€”; and R7 is selected from hydrogen, alkyl, alkenyl, cycloalkyl-(CH2)mâ€”, aryl-(CH2)mâ€”, and heteroaryl-(CH2)mâ€”, where m is 0 to 6; R11 and R12 are independently selected from hydrogen, alkyl, alkenyl, cycloalkyl-(CH2)pâ€”, aryl-(CH2)pâ€”, and heteroaryl-(CH2)pâ€”, or R11 and R12 taken together with the carbon to which they are attached complete a saturated cycloalkyl ring of 3 to 7 carbons, or R11 and R12 taken together with the carbon to which they are attached complete a keto substituent, with the proviso that at least one or R11 and R12 is other than H, wherein the term â€œheteroarylâ€  refers to an unsaturated ring of 5 or 6 atoms containing one or two O and S atoms and/or 1 to 4 N atoms provided that the total number of hetero atoms in the ring is 4 or less, which may optionally be substituted with 1, 2 or 3 substituents, wherein the above 5 or 6-membered ring is optionally fused to a benzene or pyridyl ring to form a bicyclic ring, which mono or bicyclic ring can also be additionally substituted at an available carbon atom, and if the mono or bicyclic ring has an available N-atom such N atom can also be substituted by an N-protecting group; the term â€œcycloheteroalkylâ€  refers to a 5-, 6 - or 7-membered saturated or partially unsaturated ring which includes 1 to 2 hetero atoms which are nitrogen, oxygen and/or sulfur, linked through a carbon atom or a heteroatom, and which may include 1 to 4 substituents, and the 5-, 6-, or 7-membered ring can be fused to a cycloalkyl, aryl, heteroaryl or cycloheteroalkyl ring; and the term â€œcycloalkylâ€  refers to saturated rings of 3 to 7 carbons.