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US 7,582,775 B2Granted
Vitamin D receptor modulators
AssigneeEli Lilly and Company
InventorsJianliang Lu, Tainwei Ma, Sunil Nagpal, Quanrong Shen, Alan M. Warshawsky, Ying Kwong Yee, Michael John Rupp
Life of this patent
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Abstract
The present invention relates to novel, non-secosteroidal, phenyl-benzothiophene compounds with vitamin D receptor (VDR) modulating activity that are less hypercalcemic than 1α,25 dihydroxy vitamin D3. These compounds are useful for treating bone disease and psoriasis.
Claims17
A compound or a pharmaceutically acceptable salt thereof represented by a formula below:
- wherein
- R and R′ are independently C1-C5 alkyl, or together R and R′ form a carbocyclic ring having from 3 to 8 carbon atoms;
- RP3 is hydrogen, or C1-C5 alkyl;
- (LP1) is —(CH2)m—O—;
- (LP2) is
- is where m is 0, 1, or 2;
- ZP is a branched C3-C5 alkyl or 1-ethyl-1-hydroxypropyl;
- ZTB is selected from
- —O—SO2—(C1-C5 alkyl,)
- —CO2H,
- —CO2Me,
- —CO2Et,
- —C(O)NH2,
- —C(O)NMe2,
- —C(O)NH—CH2—C(O)OH,
- —C(O)NH—CH2—C(O)OMe,
- —C(O)NH—CH2—C(O)OEt,
- —C(O)NH—CH2—C(O)OiPr,
- —C(O)NH—CH2—C(O)OtBu,
- —C(O)NH—CH(Me)-C(O)OH,
- —C(O)NH—CH(Me)-C(O)OMe,
- —C(O)NH—CH(Me)-C(O)OEt,
- —C(O)NH—CH(Me)-C(O)iPr,
- —C(O)NH—CH(Me)-C(O)tBu,
- —C(O)NH—CH(Et)-C(O)OH,
- —C(O)NH—C(Me)2-C(O)OH,
- —C(O)NH—C(Me)2-C(O)OMe,
- —C(O)NH—C(Me)2-C(O)OEt,
- —C(O)NH—C(Me)2-C(O)iPr,
- —C(O)NH—C(Me)2-C(O)tBu,
- provided that -(LTB)-ZTB is substituted at either the 5 or 6 position of the benzothiophene ring.
28 more elements
Dependencies are inferred from the claim text.