Back to results
US 7,115,758 B2Granted
Vitamin D derivatives with cyclic substructures in the side chains, process and intermediate products for their production, and the use for the production of pharmaceutical agents
AssigneeSchering Corporation
InventorsAndreas Steinmeyer, Katica Schwarz, Claudia Giesen, Martin Haberey, Marianne Fähnrich
Life of this patent
Estimating the term…
Abstract
The invention relates to vitamin D derivatives of general formula I, process for their production, intermediate products of the process as well as the use for the production of pharmaceutical agents.
Claims31
A compound formula I,
- in which
- Y1 and Y2, independently of one another are, each a hydrogen atom or —C(O)R5,
- Y3 is a hydrogen atom, hydroxy, a halogen atom, —OC(O)R5 or —OR5, wherein Y3 can be present in the 2α-situation or the epimeric 2β-situation,
- R5 is an aromatic radical with 5 to 12 C atoms or an aliphatic, straight-chain or branched, saturated or unsaturated C1–C12 alkyl radical, which optionally is interrupted by 1–2 oxygen atoms, 1–2 sulfur atoms and/or 1–2 NH groups and/or optionally is substituted by 1–2 hydroxy groups, 1–2 amino groups, 1–2 SH groups, 1–2 COOH groups and/or 1–2 phenyl groups,
- R1 and R2 are each a hydrogen atom or together are an exocyclic methylene group,
- R3 and R4, independently of one another, are each a hydrogen atom, a fluorine, chlorine or bromine atom, an alkyl group with 1 to 4 carbon atoms, or together are a methylene group or together with quaternary carbon atom 20 a 3- to 7-membered, saturated or unsaturated carbocyclic ring,
- Q is a straight-chain alkylene group with 1 to 5 carbon atoms,
- X1 and X2 together are a double-bound keto-oxygen atom or, independently of one another, are each a hydrogen atom, a hydroxy group, —O(CO)R5, or a fluorine, chlorine or bromine atom, wherein X1 and X2, are not both a hydroxy group or both an —O(CO)R5 group,
- Z is an oxazole, thiazole, benzoxazole, or benzothiazole ring, which in each case is unsubstituted or substituted by one or more fluorine, chlorine, bromine or iodine atoms, one or more hydroxy groups, one or more COOR6 groups, and/or one or more C1–C5 alkyl groups, which in turn can be substituted by one or more fluorine, chlorine, bromine or iodine atoms, C1–C6 alkoxy groups and/or COOR6 groups, and
- R6 is C1–C6 alkyl, benzyl or phenyl,
- and all possible epimers or diastereomers and mixtures thereof.
8 more elements
Dependencies are inferred from the claim text.