Heterodimers of glutamic acid

Inactive Publication Date: 2008-08-14
MOLECULAR INSIGHT PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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An estimated $2 billion is currently spent worldwide on surgical, radiation, drug therapy and minimally invasive treatments, $1 billion of the spending in the U.S. There is presently no effective therapy for relapsing, metastat

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  • Heterodimers of glutamic acid
  • Heterodimers of glutamic acid
  • Heterodimers of glutamic acid

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Definitions

[0036]“Pharmaceutically acceptable salt” refers to those salts which retain the biological effectiveness and properties of the free bases and which are obtained by reaction with inorganic acids such as hydrochloric acid, hydrobromic acid, sulfuric acid, nitric acid, phosphoric acid, methanesulfonic acid, ethanesulfonic acid, p-toluenesulfonic acid, salicylic acid and the like.

[0037]“Alkyl” refers to a straight-chain, branched or cyclic saturated aliphatic hydrocarbon. Typical alkyl groups include methyl, ethyl, propyl, isopropyl, butyl, isobutyl, tertiary butyl, pentyl, hexyl and the like. The alkyl group may be optionally substituted with one or more substituents selected from the group consisting of hydroxyl, cyano, or alkoxy. When the alky group is an R′ substituent, it is a lower alkyl of from 1 to 6 carbons, more preferably 1 to 4 carbons.

[0038]“Aryl” refers to an aromatic group which has at least one ring having a conjugated pi electron system and includes carbocycl...

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Abstract

Compounds of Formula (Ia)
wherein R is a C6-C12 substituted or unsubstituted aryl, a C6-C12 substituted or unsubstituted heteroaryl, a C1-C6 substituted or unsubstituted alkyl or —NR′R′,
  • Q is C(O), O, NR′, S, S(O)2, C(O)2 (CH2)p
  • Y is C(O), O, NR′, S, S(O)2, C(O)2 (CH2)p
  • Z is H or C1-C4 alkyl,
  • R′ is H, C(O), S(O)2, C(O)2, a C6-C12 substituted or unsubstituted aryl, a C6-C12 substituted or unsubstituted heteroaryl or a C1-C6 substituted or unsubstituted alkyl, when substituted, aryl, heteroaryl and alkyl are substituted with halogen, C6-C12 heteroaryl, —NR′R′ or COOZ, which have diagnostic and therapeutic properties, such as the treatment and management of prostate cancer and other diseases related to NAALADase inhibition. Radiolabels can be incorporated into the structure through a variety of prosthetic groups attached at the X amino acid side chain via a carbon or hetero atom linkage.

Description

CROSS-REFERENCE TO RELATED APPLICATIONS[0001]This application claims priority to U.S. provisional application No. 60 / 857,490 filed Nov. 8, 2006 and U.S. provisional application No. 60 / 878,678 filed Jan. 5, 2007, the disclosures of which are incorporated herein by reference in their entireties.BACKGROUND OF THE INVENTION[0002]At least 1 million men suffer from prostate cancer and it's estimated that the disease will strike one in six U.S. men between the ages of 60 and 80. There are more than 300,000 new cases of prostate cancer diagnosed each year. Prostate cancer will affect one in six men in the United States, and the mortality from the disease is second only to lung cancer. An estimated $2 billion is currently spent worldwide on surgical, radiation, drug therapy and minimally invasive treatments, $1 billion of the spending in the U.S. There is presently no effective therapy for relapsing, metastatic, androgen-independent prostate cancer. New agents that will enable rapid visualiz...

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Application Information

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IPC IPC(8): A61K49/00C07D213/04C07C275/04A61K31/17A61P35/00A61K31/444C07F13/00
CPCC07B59/001C07C275/16C07D213/38C07C275/30C07C311/19C07C275/24A61K51/0455C07B59/002C07D213/36C07F1/005C07F13/005A61P21/00A61P21/02A61P25/00A61P25/02A61P25/04A61P25/18A61P25/28A61P29/00A61P35/00A61K39/385
Inventor BABICH, JOHN W.ZIMMERMAN, CRAIG N.MARESCA, KEVIN P.
Owner MOLECULAR INSIGHT PHARMA
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