Vitamin D3 derivative and treating agent for inflammatory respiratory disease using same
AssigneeTeijin Limited
InventorsKazuya Takenouchi, Qingzhi Gao, Kenji Manabe, Ryo Sogawa, Yasuhiro Takano, Seiichi Ishizuka
Life of this patent
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Abstract
Compounds expressed by the following general formula (1), [wherein, R01 and R02 are each independently a hydrogen atom or a protecting group for a hydroxyl group; Z is one out of the following formulae (1-1) to (1-5)]. The compounds can be used as active ingredients of treating agents for inflammatory respiratory diseases, malignant tumors, rheumatoid arthritis, osteoporosis, diabetes mellitus, hypertension, alopecia, acne, psoriasis, dermatitis, hypercalcemia, hypoparathyroidism and metabolic disorder of cartilage.
Claims20
A vitamin D3 compound expressed by the following general formula (1) or pharmaceutically permissible solvates thereof,
- wherein, R01 and R02 are each independently a hydrogen atom, a trimethylsilyl group, a triethylsilyl group, a t-butyldimethylsilyl group, an acetyl group, a methoxymethyl group or a tetrahydro-4H-pyran-2-yl group;
- Z is one out of the following formulae (1-1) and (1-2),
- in the above formulae (1-1) and (1-2),
- m is an integer of 0 to 2;
- n is 0;
- X′ is NH;
- R11 and R12 are identical to or different from each other, and express a hydrogen atom or a C1-C4 alkyl group;
- K, L and M are each a hydrogen atom;
- M is a hydrogen atom, and K and L together express a single bond and express a double bond in cooperation with the single bond already shown in the formula;
- or K is a hydrogen atom, and L and M together express a single bond and express a double bond in cooperation with the single bond already shown in the formula;
- R21, R22 and R23 are identical to or different from each other, and they are a hydrogen atom, a hydroxy group, a carboxyl group, a trifluoromethyl group, a pentafluoroethyl group, a C1-C4 alkyloxycarbonyl group, a C2-C5 acyloxy group, a C1-C4 alkyloxy group or a C1-C4 alkyl group which may be substituted with a hydroxyl group, a C2-C5 acyloxy group or a alkyloxy group, or R21 and R22 together may express a C3-C6 cyclic alkyl group in cooperation with the carbon atom to which they are bonded,
- with the proviso that the following compound (a) is excluded,
- (a) a compound in which R21 and R22 are both hydroxy groups, both alkyloxy groups, or a hydroxy group and an alkyloxy group.
Dependencies are inferred from the claim text.