Patent ID: 6797708
Filing Date: 2004-09-28
Classification: A61P,C07D

Abstract:
A compound of the formula: wherein:R is selected from the formulae â€”(CH2)nâ€”A, â€”(CH2)nâ€”Sâ€”A, and â€”(CH2)nâ€”Oâ€”A, wherein A is selected from the moieties: â€ƒwherein D is selected from the group consisting of C1-C6 lower alkyl, C1-C6 lower alkoxy, C3-C6 cylcoalkyl, â€”CF3 and â€”(CH2)1-3â€”CF3; B and C are independently selected from the group consisting of phenyl, pyridinyl, pyrimidinyl, furyl, thienyl and pyrrolyl groups, each optionally substituted by from 1 to 3 substituents selected independently from H, halogen, â€”CN, â€”CHO, â€”CF3, â€”OCF3, â€”OH, â€”C1-C6 alkyl, C1-C6 alkoxy, â€”NH2, â€”N(C1-C6)2, â€”NH(C1-C6), â€”Nâ€”C(O)â€”(C1-C6), and â€”NO2, or by a 5- or 6-membered heterocyclic or heteroaromatic ring containing 1 or 2 heteroatoms selected from O, N or S; and n is an integer from 0 to 3; n1 is an integer from 1 to 3; n2 is an integer from 0 to 4; n3 is an integer from 0 to 3; n4 is an integer from 0 to 2; X1 is selected from a chemical bond, â€”Sâ€”, â€”Oâ€”, â€”S(O)â€”, â€”S(O)2â€”, â€”NHâ€”, â€”NHC(O)â€”, â€”C&boxH;Câ€”, R1 is selected from C1-C6 alkyl, C1-C6 fluorinated alkyl, C3-C6 cycloalkyl, tetrahydropyranyl, camphoryl, adamantyl, CN, â€”N(C1-C6 alkyl)2, phenyl, pyridinyl, pyrimidinyl, furyl, thienyl, naphthyl, morpholinyl, triazolyl, pyrazolyl, piperidinyl, pyrrolidinyl, imidazolyl, piperazinyl, thiazolidinyl, thiomorpholinyl, tetrazole, indole, benzoxazole, benzofuran, imidazolidine-2-thione, 7,7,dimethyl-bicyclo[2.2.1]heptan-2-one, Benzo[1,2,5]oxadiazole, 2-Oxa-5-aza-bicyclo[2.2.1]heptane, Piperazin-2-one or pyrrolyl groups, each optionally substituted by from 1 to 3 substituents independently selected from H, halogen, â€”CN, â€”CHO, â€”CF3, OCF3, â€”OH, â€”C1-C6 alkyl, C1-C6 alkoxy, â€”NH2, â€”N(C1-C6)2, â€”NH(C1-C6), â€”Nâ€”C(O)â€”(C1-C6), â€”NO2, â€”SO2(C1-C3 alkyl), â€”SO2NH2, â€”SO2NH(C1-C3 alkyl), â€”SO2N(C1-C3 alkyl)2, â€”COOH, â€”CH2â€”COOH, â€”CH2â€”N(C1-C6 alkyl), â€”CH2â€”N(C1-C6 alkyl)2, â€”CH2â€”NH2, pyridine, 2-Methyl-thiazole, morpholino, 1-Chloro-2-methyl-propyl, â€”C1-C6 thioalkyl, phenyl (further optionally substituted with halogens), benzyloxy, (C1-C3 alkyl)C(O)CH3, (C1-C6 alkyl)OCH3, C(O)NH2, or X2 is selected from â€”Oâ€”, â€”CH2â€”, â€”Sâ€”, â€”SOâ€”, â€”SO2â€”, â€”NHâ€”, â€”C(O)â€”, R2 is a ring moiety selected from phenyl, pyridinyl, pyrimidinyl, furyl, thienyl or pyrrolyl groups, the ring moiety being substituted by a group of the formula â€”(CH2)n4â€”CO2H or a pharmaceutically acceptable acid mimic or mimetic selected from the group consisting of: â€ƒwherein Ra is selected from â€”CF3, â€”CH3, phenyl, or benzyl, with the phenyl or benzyl groups being optionally substituted by from 1 to 3 groups selected from C1-C6 alkyl, C1-C6 alkoxy, C1-C6 thioalkyl, â€”CF3, halogen, â€”OH, or â€”COOH; Rb is selected from â€”CF3, â€”CH3, â€”NH2, phenyl, or benzyl, with the phenyl or benzyl groups being optionally substituted by from 1 to 3 groups selected from C1-C6 alkyl, C1-C6 alkoxy, C1-C6 thioalkyl, â€”CF3, halogen, â€”OH, or â€”COOH; and Rc is selected from â€”CF3 or C1-C6 alkyl â€ƒand also optionally substituted by 1 or 2 additional substituents independently selected from H, halogen, â€”CN, â€”CHO, â€”CF3, â€”OCF3, â€”OH, â€”C1-C6 alkyl, C1-C6 alkoxy, C1-C6 thioalkyl, â€”NH2, â€”N(C1-C6)2, â€”NH(C1-C6), â€”Nâ€”C(O)â€”(C1-C6), and â€”NO2; R3 is selected from H, halogen, â€”CN, â€”CHO, â€”CF3, â€”OCF3, â€”OH, â€”C1-C6 alkyl, C1-C6 alkoxy, C1-C6 thioalkyl, â€”NH2, â€”N(C1-C6)2, â€”NH(C1-C6), â€”Nâ€”C(O)â€”(C1-C6), and â€”NO2; R4 is selected from H, halogen, â€”CN, â€”CHO, â€”CF3, â€”OCF3, â€”OH, â€”C1-C6 alkyl, C1-C6 alkoxy, C1-C6 thioalkyl, â€”NH2, â€”N(C1-C6)2, â€”NH(C1-C6), â€”Nâ€”C(O)â€”(C1-C6), â€”NO2, â€”Nâ€”C(O)â€”N(C1-C3 alkyl)2, â€”Nâ€”C(O)â€”NH(C1-C3 alkyl), â€”Nâ€”C(O)â€”Oâ€”(C1-C3 alkyl), â€”SO2â€”C1-C6 alkyl, â€”Sâ€”C3-C6 cycloalkyl, â€”Sâ€”CH2â€”C3-C6 cycloalkyl, â€”SO2â€”C3-C6 cycloalkyl, â€”SO2â€”CH2â€”C3-C6 cycloalkyl, C3-C6 cycloalkyl, â€”CH2â€”C3-C6 cycloalkyl, â€”Oâ€”C3-C6 cycloalkyl, â€”Oâ€”CH2â€”C3-C6 cycloalkyl, phenyl, benzyl, benzyloxy, morpholino, pyrrolidino, piperidine, piperizine furan, thiophene, imidazole, tetrazole, pyrazine, pyrazolone, pyrazole, imidazole, oxazole and isoxazole, the rings of each of these R4 groups each being optionally substituted by from 1 to 3 substituents selected from the group of H, halogen, â€”CN, â€”CHO, â€”CF3, â€”OH, â€”C1-C6 alkyl, C1-C6 alkoxy, â€”NH2, â€”N(C1-C6)2, â€”NH(C1-C6), â€”Nâ€”C(O)â€”(C1-C6), â€”NO2, â€”SO2(C1-C3 alkyl), â€”SO2NH(C1-C3 alkyl), â€”SO2N(C1-C3 alkyl)2, and OCF3; or a pharmaceutically acceptable salt form thereof.