Patent ID: 6699862
Filing Date: 2004-03-02
Classification: A61P,C07D

Abstract:
Indolyl-2-phenyl bisamidines comprising a compound of Formula (1.0.1): or a pharmaceutically acceptable salt thereof, wherein:R1 is (C1-C3)alkyl; R3, R4, R5, R8, R9, and R10 are each independently selected from the group consisting of (C1-C3)alkyl; â€” or â€”R3 and R4 may be taken together, or R8 and R9 may be taken together with the nitrogen atoms to which they are attached, to form an imidazolinyl group; or further together with an additional ring carbon, â€”CH2â€”, to form a 1,4,5,6-tetrahydropyrimidinyl group; R14 is independently selected from the group consisting of â€”H; â€”NHC(&boxH;O)(CH2)mR20; â€”(CH2)mR20; â€”CH(CH3)R20; (CH2)m(C6H4)â€”R17; â€”(CH2)m(C6H4)â€”R20; â€”(CH2)m(heterocyclyl)â€”R17; â€”(CH2)m(heterocyclyl)â€”R20; â€”CH2CH&boxH;CHR20; â€”(CH2)mC(&boxH;O)NHCHR20R21; and â€”(CH2)mC(&boxH;O)NHâ€”CH2â€”C(&boxH;O)NHCHR20R21; R15 is independently selected from the group consisting of hydrogen; â€”OR1; â€”Oâ€”(C1-C3)alkylenyl-R20; and â€”OR20; R17 is independently selected from the group consisting of hydrogen; halogen; (C1-C3)alkyl; â€”CF3; â€”CN; â€”NO2; â€”N(R1)2; â€”OH; and (C1-C3) alkyl(C1-C3)alkoxy; R20 is independently selected from the group consisting of â€”C(&boxH;O)OR1; CH(OH)CH2OH; â€”C(&boxH;O)NH2; and â€”C(&boxH;O)H; R21 is independently selected from the group consisting of hydrogen; (C1-C6)alkyl; â€”(CH2)nR22; â€”CH(CH3)CH2C(&boxH;O)OR1; and â€”CH2â€”(C6H5); R22 is independently selected from the group consisting of â€”H; â€”NH2; â€”OR1; â€”SR1; â€”CN; â€”OCH2â€”(C6H5); â€”O(CH2)mâ€”OR1; â€”C(&boxH;O)OR1; thienyl; tetrahydropyranyl; â€”CH(OH)CH2OH; â€”C(&boxH;O)C(CH3)&boxH;CH2; â€”NHC(&boxH;O)OCH2â€”(C6H5); and â€”S(&boxH;O)2R1; m is an integer independently selected from 1, 2, and 3; â€”andâ€”n is an integer independently selected from 1 through 5, inclusive.