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US 6,472,382 B2Granted
4-halogenated steroids, their preparation process and intermediates, their use as medicaments and the pharmaceutical compositions containing them
AssigneeAventis Pharma S.A.
InventorsYamina Bouali, Francois Nique, Jean-Georges Teutsch, Patrick Van De Velde
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Abstract
A subject of the invention is the compounds of formula (I): in which X is a halogen atom, D represents the remainder of an optionally substituted pentagonal or hexagonal ring and optionally carrying an unsaturation, R1, R2, R3, R4, Y and n are as defined in the description, their preparation process and intermediates, their use as medicaments and the compositions containing them.
Claims9
A compound selected from the group consisting of a compound of the formula
- wherein R1 is selected from the group consisting of hydrogen, —(CH2)m-Ar, —(CO)-Ar, —(CH2)m-Alk and —(CO)-Alk, R2 is optionally unsaturated alkyl of 1 to 6 carbon atoms, D forms with the carbons to which it is attached a 5 or 6 membered ring unsubstituted or substituted and saturated or unsaturated, X is halogen, Y is selected from the group consisting of -O-, -S-, -SO-, -SO2- and -NH-, n is an integer of 2 to 8, m is an integer from 0 to 3, R3 and R4 are individually selected from the group consisting of hydrogen, —(CH2)m-Ar, —(CH2)m-Alk and —(CH2)m-Het with at least one being —(CH2)m-Het or together with the nitrogen to which they are attached form an aromatic on non-aromatic, saturated or non-saturated mono or polycyclic heterocyclic of 3 to 15 members optionally containing 1 to 3 heteroatoms selected from the group consisting of oxygen, sulfur and nitrogen and unsubstituted or substituted, Ar is carbocyclic aryl of 6 to 8 carbon atoms, Het is saturated or unsaturated, aromatic or non-aromatic heterocycle of 1 to 9 ring carbon atoms and 1 to 5 ring heteroatoms selected from the group consisting of oxygen, sulfur and nitrogen, Alk is saturated or unsaturated alkyl and cycloalkyl of up to 12 carbon atoms, the Ar, Het and Alk unsubstituted or substituted and its addition salts with non-toxic, pharmaceutically acceptable acid and bases.
Dependencies are inferred from the claim text.