Patent ID: 6387949
Filing Date: 2002-05-14
Classification: C07C,C07D

Abstract:
A compound according to formula I: wherein:m and n are each independently an integer from 1-3, and one or more of the hydrogens in the alkylene chain may optionally be substituted by any one of a C1-C6 alkyl; a C1-C6 alkoxy; or a hydroxy; or one or more of the methylene groups may optionally be substituted by a heteroatom selected from O, N or S; R1 is selected from hydrogen; a branched or straight C1-C6 alkyl; a C2-C6 alkenyl; a C3-C8 cycloalkyl; a C4-C8(alkyl-cycloalkyl) wherein the alkyl is a C1-C2 alkyl and the cycloalkyl is a C3-C6 cycloalkyl; R2 is selected from any of: (i) hydrogen; (ii) a straight or branched C1-C6 alkyl; a C2-C6 alkenyl; or a C2-C6 alkynyl; (iii) a ((CH2)q-aryl); (iv) a ((CH2)r-heteroaryl) wherein the heteroaryl has from 5 to 10 atoms, each heteroatom being selected from any of S, N and O; and wherein the heteroaryl may optionally and independently be substituted by 1 or 2 substituents Y, wherein each Y is as defined below; and wherein q and r are each independently an integer from 0 to 3; (v) a C3-C10 cycloalkyl, optionally comprising one or more unsaturations and optionally substituted by one or more heteroaryls, wherein each heteroaryl has from 5 to 10 atoms and each heteroatom is selected from any of S, N and O; and wherein an aryl or heteroaryl may optionally and independently be substituted by 1 or 2 substituents Y, wherein each Y is as defined below; (vi) a heteroaryl having from 5 to 10 atoms, each heteroatom being selected from any of S, N and O; wherein the heteroaryl may optionally and independently be substituted by 1 or 2 substituents Y, wherein each Y is as defined below; or R1 and R2 may optionally form a heterocyclic ring, which may optionally be saturated or unsaturated; R3 is selected from any one of: (i) hydrogen; (ii) a straight or branched C1-C6 alkyl; C2-C6 alkenyl; or C2-C6 alkynyl; (iii) a C6-C10 arylalkyl, wherein the aryl may optionally be substituted by one or more heteroaryls having from 5 to 10 atoms, each heteroatom being selected from any of S, N and O; and wherein the aryl and heteroaryl may optionally and independently be substituted by 1 or 2 substituents Y, wherein each Y is as defined below; (iv) a heteroaryl-(C5-C10 alkyl), wherein the heteroaryl has from 5 to 10 atoms, each heteroatom being selected from any of S, N, O, and wherein the heteroaryl may optionally and independently be substituted by 1 or 2 substituents Y, wherein each Y is as defined below; (v) a C3-C10 cycloalkyl, optionally comprising one or more unsaturations and optionally substituted by one or more heteroaryls having from 5 to 10 atoms, each heteroatom being selected from any of S, N and O, and wherein the aryl and heteroaryl may optionally and independently be substituted by 1 or 2 substituents Y, wherein each Y is as defined below; (vi) a (C3-C6 cycloalkyl-(CH2)q) wherein q is an integer from 1 to 3; R4 is selected from: (i) hydrogen; (ii) a straight or branched C1-C6 alkyl; C2C6 alkenyl; or C2-C6 alkynyl; (iii) a C6-C10 arylalkyl, wherein the aryl may optionally be substituted by one or more heteroaryls having from 5 to 10 atoms, each heteroatom being selected from any of S, N and O; and wherein the aryl and heteroaryl may optionally and independently be substituted by 1 or 2 substituents Y, wherein each Y is as defined below; (iv) a heteroaryl-(C5-C10 alkyl), wherein the heteroaryl has from 5 to 10 atoms, each heteroatom being selected from any of S, N and O, and wherein the heteroaryl may optionally and independently be substituted by 1 or 2 substituents Y, wherein each Y is as defined below; (v) a C3-C10 cycloalkyl, optionally comprising one or more unsaturations and optionally substituted by one or more heteroaryls wherein each heteroaryl has from 5 to 10 atoms and each heteroatom is selected from any of S, N and O; and wherein an aryl or heteroaryl may optionally and independently be substituted by 1 or 2 substituents Y, wherein each Y is as defined below; (vi) a heteroaryl having from 5 to 10 atoms, each heteroatom being selected from any of S, N and O; wherein the heteroaryl may optionally and independently be substituted by 1 or 2 substituents Y, wherein each Y is as defined below; R5 is selected from any one of: (i) hydrogen; (ii) a straight or branched C1-C6 alkyl; C2-C6 alkenyl; or C2-C6 alkynyl; (iii) a C6-C10 arylalkyl, wherein the aryl may optionally be substituted by one or more heteroaryls having from 5 to 10 atoms, each heteroatom being selected from any of S, N and O; and wherein the aryl and heteroaryl may optionally and independently be substituted by 1 or 2 substituents Y, wherein each Y is as defined below; (iv) a heteroaryl-(C5-C10 alkyl), wherein the heteroaryl has from 5 to 10 atoms, each heteroatom being selected from any S, N and O, and wherein the heteroaryl may optionally and independently be substituted by 1 or 2 substituents Y, wherein each Y is as defined below; (v) a C3-C10 cycloalkyl, optionally comprising one or more unsaturations and optionally substituted by one or more heteroaryls having from 5 to 10 atoms, each heteroatom being selected from any of S, N and O, and wherein an aryl or heteroaryl may optionally and independently be substituted by 1 or 2 substituents Y, wherein each Y is as defined below; (vi) a heteroaryl having from 5 to 10 atoms, each heteroatom being selected from any of S, N and O, wherein the heteroaryl may optionally and independently be substituted by 1 or 2 substituents Y, wherein each Y is as defined below; â€ƒwherein R7, R8, R9, R10 and R11 are each independently selected from: (a) hydrogen; (b) a straight or branched C1-C6 alkyl; C2-C6 alkenyl; or C2-C6 alkynyl; (c) a C6-C10 arylalkyl, wherein the aryl may optionally be substituted by one or more heteroaryls having from 5 to 10 atoms, each heteroatom being selected from any of S, N and O, and wherein the aryl and heteroaryl may optionally and independently be substituted by 1 or 2 substituents Y, wherein each Y is as defined below; (d) a heteroaryl-C5-C10 alkyl), wherein the heteroaryl has from 5 to 10 atoms, each heteroatom being selected from any of S, N and O, and wherein the heteroaryl may optionally and independently be substituted by 1 or 2 substituents Y, wherein each Y is as defined below; (e) a C3-C10 cycloalkyl, optionally comprising one or more unsaturations and optionally substituted by one or more heteroaryls, each heteroaryl having from 5 to 10 atoms, and each heteroatom being selected from any of S, N and O; and wherein an aryl or heteroaryl may optionally and independently be substituted by 1 or 2 substituents Y, wherein each Y is as defined below; or R4 and R5 may optionally form a heterocyclic ring, which may optionally be saturated or unsaturated; Y is each and independently selected from any of CH3; â€”(CH2)p1 CF3; halogen; C1-C3 alkoxy; hydroxy; â€”NO2; â€”OCF3; â€”CONRaRb; â€”COORa; â€”CORa; â€”(CH2)p2NRaRb; â€”(CH2)p3CH3; (CH2)p4SORaRb; â€”(CH2)p6SO2Ra; (CH2)p6SO2NRa; C4-C8(alkyl-cycloalkyl), wherein the alkyl is a C1-C2 alkyl and the cycloalkyl is a C3-C6 cycloalkyl; 1 or 2 heteroaryls having from 5 to 10 atoms, each heteroatom being selective from any of S, N and O; and oxides selected from N-oxides or sulfoxides; and wherein: Ra and Rb are each independently selected from hydrogen; a branched or straight C1-C6 alkyl; a C1-C6 alkenyl; a C3-C8 cycloalkyl; and wherein p1, p2, p4, p5 are p6 are each and independently 0, 1 or 2; and p3 is 1 or 2; as well as pharmaceutically acceptable salts of the compound of formula I and isomers, hydrates, isoforms and prodrugs thereof.