Isoprenoid pathway inhibitors for stimulating cartilage growth

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United States of America Patent

SERIAL NO

11167054

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Abstract

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Compounds of the formula 1 wherein X in each of formulas (1) and (2) represents a substituted or unsubstituted alkylene, alkenylene, or alkynylene linker of 2-6C; Y is of the formula 2 or a stereoisomer thereof, wherein R.sup.1 is substituted or unsubstituted alkyl; each R.sup.2 is independently H, hydroxy, alkoxy (1-6C) or lower alkyl (1-4C); R.sup.3 is H, hydroxy, or alkoxy (1-6C); or Y is of the formula 3 wherein each n is 1, Z is N, K comprises a substituted or unsubstituted aromatic carbocyclic or heterocyclic ring system which may optionally be spaced from the linkage position shown in formula (7) by a linker of 1-2C, or in formula (7), Z may be spaced from the carbon bonded to X by .dbd.CR.sup.6-- wherein R.sup.6 is H or linear, branded or cyclic alkyl (1-6C), R.sup.5 is H or linear, branched or cyclic alkyl, and R' represents a cation, H or a substituted or unsubstituted alkyl group of 1-6C, promote bone formation and are thus useful in treating osteoporosis, bone fracture or deficiency, primary or secondary hyperparathyroidism, periodontal disease or defect, metastatic bone disease, osteolytic bone disease, post-plastic surgery, post-prosthetic joint surgery, and post-dental implantation. Also disclosed is a method to identify additional compounds which are inhibitors of enzymes in the isoprenoid scheme especially of HMG-CoA reductase which results in prenylation of proteins and in the synthesis of steroids or of inhibitors of their production which are useful in treating bone disorders.

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OSTEOSCREEN IP LLC2040 BABCOCK ROAD SUITE 201 SAN ANTONIO TX 78229

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Inventor(s)

Inventor Name Address # of filed Patents Total Citations
Baindur, Nand Edmonds, WA 50 1276
Gasper, Shirley R Seattle, WA 6 65
Labroo, Virender M Bangalore, IN 21 290
Martinez, Theresa Greenbank, WA 11 87
McKernan, Patricia A Woodinville, WA 26 135
Mundy, Gregory R San Antonio, TX 51 1764
Robbins, Kirk G Renton, WA 20 1013
West, Robert R Seattle, WA 27 186

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