Patent ID: 6620801
Filing Date: 2003-09-16
Classification: A61P,C07J

Abstract:
A hormonal or antihormonal steroid compound of structure II, whereinR1 is (R2R3N(O)r)â€”, where r is 0 or 1 and R2 and R3 are each independently H, C1-6 alkyl, C3-8 cycloalkyl, C2-6 alkenyl or C2-6 alkynyl, any of which may be optionally substituted; or â€ƒwhere q is 0 or 1, Y is â€”(CH2)mâ€” where m is an integer of 0 to 5, or Y is â€”(CH2)nâ€”Zâ€”(CH2)pâ€” where n is an integer of 0 to 2, p is an integer of 0 to 2, and Z is a heteroatom (optionally substituted) and where any of the CH2 groups may be optionally substituted; or R1 is N-imidazolyl, â€”N-pyrrolyl-, halo-, HOâ€”, CF3SO2Oâ€”, C1-6 alkyl-Oâ€”, C1-6 alkyl-Sâ€”, C1-6 alkyl-S(O)â€”, C1-6 alkyl-S(O2)â€”, C1-6 alkyl-COâ€”, C1-6 alkyl-CH(OH)â€”, NCâ€”, HCCâ€”, C6H5CCâ€”, 2â€²-furyl, 3â€²-furyl, 2â€²-thiophenyl, 3â€²-thiophenyl, 2â€²-pyridyl, 3â€²-pyridyl, 4â€²-pyridyl, 2â€²-thiazolyl, 2â€²-N-methylimidazolyl, 5â€²-pyrimidinyl, C6H5â€”, H2C&boxH;CHâ€”, C1-6 alkyl, or MeC(&boxH;CH2)â€”; R12 is H or halo; or R1 and R12 combine to form a ring â€ƒwhere W is CH2, CH, NH, N, O, or S, and R4 is H or C1-6 alkyl; X is O or NOR5, where R5 is H or C1-6 alkyl, C3-8 cycloalkyl, C2-6 alkenyl, C2-6 alkynyl, C6-12 aryl, or heteroaryl, any of which may be optionally substituted; or X is (H, H), (H, OH), (H, OSi(C1-6 alkyl)3), or (H, OCOR5â€²), where R5â€² is C1-6 alkyl, C3-8 cycloalkyl, C2-6 alkenyl, C2-6 alkynyl, C6-12 aryl, aralkyl, aralkenyl, aralkynyl, heteroaryl, heteroaralkyl, heteroaralkenyl or heteroaralkynyl, any of which may be optionally substituted; or â€ƒwhere Yâ€² is â€”(CH2)mâ€²â€” where mâ€² is an integer of 0 to 3, or Yâ€² is â€”(CH2)nâ€”Zâ€²â€”(CH2)pâ€” where n is an integer of 0 to 2, p is an integer of 0 to 2 and Zâ€² is a heteroatom (optionally substituted) or Zâ€² is a carbon atom substituted with one or two C1-6 alkyl groups; R6 is H, C1-6 alkyl or halogen; s is 0 or 1; R9 is H, C1-6 alkyl, C2-6 alkenyl or C2-6 alkynyl, R10CO, OR11, any of which may be optionally substituted, where R10 is H, C1-18 alkyl, C2-18 alkenyl, C2-18 alkynyl, C3-8 cycloalkyl, C6-2 aryl, aralkyl, aralkenyl, aralkynyl, heteroaryl, heteroaralkyl, heteroaralkenyl or heteroaralkynyl any of which may be optionally substituted, and where R11 is H, C1-6 alkyl, Si(C1-6 alkyl)3, 2â€²-tetrahydropyranyl or R10CO where R10 is as defined above; R13 and R14 are each independently H, C1-18 alkyl, C2-18 alkenyl, C2-18 alkynyl, C3-8 cycloalkyl, C6-12 aryl, aralkyl, aralkenyl or aralkynyl, heteroaryl, heteroaralkyl, heteroaralkenyl or heteroaralkynyl, any of which may be optionally substituted; or R13R14 is O, and R15 and R16 are each H or combine to form a group &boxH;CH2, optionally substituted, and pharmaceutically acceptable salts thereof.