NAD synthetase inhibitors and uses thereof

US6861448B2 · kind B2 · utility

Assignees

• Virtual Drug Development, Inc. · US
• THE UAB RESEARCH FOUNDATION · US

Inventors

• Wayne J. Brouillette · Pelham, US
• Lawrence J. DeLucas · Birmingham, US
• Christie G. Brouillette · Pelham, US
• Sadanandan E. Velu · Birmingham, US
• Yong-Chul Kim · Noan-myeon, KR
• Liyuan Mou · Beijing, CN
• R. Stephen Porter · Brentwood, US

Key dates

• Filing date: Feb 22, 2002
• Grant date: Mar 1, 2005
• Expiry date: Feb 22, 2022

Classification

• Technology area (CPC C): Chemistry; Metallurgy
• CPC primary: C40B40/00
• WIPO field: Pharmaceuticals
• WIPO sector: Chemistry

Abstract

Disclosed are compounds that inhibit the microbial NAD synthetase enzyme. For example, disclosed are compounds of the formula Ar1—X—Ar2—Y—L—Z—Q, wherein Q is Q1Ar3 or Ar3Q1; Ar1, Ar2, and Ar3 are independently aryl or heteroaryl, optionally substituted with one or more substituents; X, Y, and Z are independently selected from the group consisting of a covalent bond or groups containing one or more of C, H, N, O, S atoms; L is a linker and Q1 is an alkylenyl, alkylenyl carbonyloxy alkyl, or alkylenyl carbonylamino alkyl group, optionally having a substituent; a covalent bond; a group containing amidine or guanidine function wherein the amidine or guanidine may be optionally N-substituted with an alkyl; or a zwitterion; or a pharmaceutically acceptable salt thereof. Also disclosed are methods which involve the use of the compounds of the present invention, for example, in treating or preventing a microbial infection in a mammal or plant, killing a prokaryote or decreasing prokaryotic growth, disinfecting a material or environment contaminated by a microbe, increasing food animal production, controlling harm to plants by a pest or insect, and combating agroterrorism. Examples of micro…