The UAB Research Foundation (The University of Alabama at Birmingham)

Other

The University of Alabama

Virtual Drug Development, Inc.

Wayne J Brouillette

Donald D Muccio

Lawrence James DeLucas

Christie G Brouillette

Venkatram Reddy Atigadda

Ming Luo

Laurent Schmitt

Sadanandan Velu

Yancho Devedjiev

Jose Gabriel Garcia

Walter Cristofoli

John M Ruppert

Mark J Jedrzejas

Yarlagadda Sudhakara Babu

Jeonga Kim

Susan M Ruppert

Sadanadan E Velu

Yong-Chul Kim

Gillian Air

Liyuan Mou

R Stephen Porter

Clinton J Grubbs

Susan M Lobo Ruppert

Novel rexinoid compounds are provided herein. Also provided herein are methods of using the compounds to treat disorders, such as metabolic disorders, diabetes, insulin resistance, glucose intolerance, obesity, steatosis, inflammation, and/or cancer.

Rexinoid compounds and methods of using rexinoid compounds for treating metabolic disorders and cancer

Described herein are methods for making retinoids. Also described herein are retinoids and methods of use thereof.

Methods for making retinoids and uses thereof

The present invention provides new retinoid compounds and uses of the compounds in humans and animals for non-neoplastic dermal or inflammatory conditions or disorders.

Retinoids and use thereof

Disclosed are compounds that inhibit the microbial NAD synthetase enzyme. For example, disclosed are compounds of the formula Ar&#x2014;X&#x2014;Ar&#x2014;Y&#x2014;L&#x2014;Z&#x2014;Q, wherein Q is QAror ArQ; Ar, Ar, and Arare 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 Qis 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 microbes affected by the compounds of the present invention are bacteria and fungi.

NAD synthetase inhibitors and uses thereof

The present invention provides methods of synthesizing and screening inhibitors of bacterial NAD synthetase enzyme, compounds thereof, and methods of treating bacterial and microbial infections with inhibitors of bacterial NAD synthetase enzyme.

Inhibitors of bacterial NAD synthetase

The present invention provides methods of treating or preventing fungal infections in a host comprising administering a treatment effective or treatment effective amount of a yeast NAD synthetase inhibitor compound. The invention further provides a method of killing yeast comprising administering a yeast NAD synthetase compound that selectively binds to catalytic sites in yeast whereby the yeast is killed.

Methods of treating fungal infections with inhibitors of NAD synthetase enzyme

Pyrrolidin-2-one compounds and their use as neuraminidase inhibitors

The present invention provides new retinoid compounds and uses of the compounds in humans and animals for chemoprevention of skin and/or breast cancer and for therapy of leukemia.

An influenza virus neuraminidase inhibitor, its analogs, its pharmaceutically acceptable salts, derivatives, and mixtures thereof having the following formula: ##STR1## where A is CO.sub.2 H, CO.sub.2 H.sub.3, NO.sub.2, SO.sub.3 H or PO.sub.3 H.sub.2, B is CH, N, O or S, R.sub.1 and R.sub.2 are H, NO.sub.2 or (CH.sub.m).sub.n X.sub.1 where m=1 or 2, n is an integer from 0 to 4 and X.sub.1 is guanidino, OH, NH.sub.2, SH, NO.sub.2, F, Cl, Br, I, CN, CF.sub.3, CO.sub.2 H, SO.sub.3 H or PO.sub.3 H.sub.2, R.sub.3 and R.sub.4 are H, (CH.sub.o).sub.p X.sub.2, (CH.sub.o).sub.p CHX.sub.2 CH.sub.2 X.sub.2, NH(CH.sub.o).sub.p CHX.sub.2 CH.sub.2 X.sub.2, NHCO(CH.sub.o).sub.p CH.sub.2 X.sub.2 or NHCO(CH.sub.o).sub.p CHX.sub.2 CH.sub.2 X.sub.2 where o=1 or 2, p is an integer from 0 to 4 and X.sub.2 is H, guanidino, OH, NH.sub.2, SH, NO.sub.2, CF.sub.3, CO.sub.2 H, SO.sub.3 H or PO.sub.3 H.sub.2 , R.sub.5 =H, OH, NH.sub.2, (CH.sub.k).sub.1 X.sub.3, CO(CH.sub.k).sub.1 X.sub.3, SO(CH.sub.k).sub.1 X.sub.3 or SO.sub.2 (CH.sub.k).sub.1 X.sub.3 where k=1 or 2, 1 is an integer from 0 to 4 and X.sub.3 is guanidino, OH, NH.sub.2, SH, NO.sub.2, CF.sub.3, CO.sub.2 H, SO.sub.3 H or PO.sub.3 H.sub.2, R.sub.6 is H, CH(OH)X.sub.4, CH(NH.sub.2)X.sub.4, COX.sub.4, SOX.sub.4, or SO.sub.2 X.sub.4, where X.sub.4 is H, CH.sub.3, CH.sub.3 CH.sub.2, CH.sub.3 CHCH.sub.3, CH.sub.3 CH.sub.2 CH.sub.2 or halogen substituted analogs of X.sub.4. The inhibitor in a composition with a pharmaceutically acceptable carrier. A method of inhibiting influenza virus neuraminidase where the inhibitor is administered to a subject in a pharmaceutically acceptable amount along with effective amounts of a pharmaceutically acceptable carrier. Methods of marking a pharmaceutical composition of an acceptable carrier and the inhibitor. Methods of treating and preventing a subject infected with influenza virus (type A or B) using the inhibitor.

Inhibitors of influenza virus neuraminidase and methods of making and

Retinoid compounds with bioactive properties and their synthesis are described. The compounds are useful as chemopreventive or cancer-treating agents and dermatological agents. The novel retinoids are members of either of the two general structures: ##STR1## wherein X is CO.sub.2 H or CH.sub.2 OH; and in formula (I), R.sub.1 and R.sub.2 are each hydrogen, a C.sub.1-4 alkyl, a C.sub.1-4 alkoxy, or R.sub.1 and R.sub.2 taken together form a 5- to 7-membered cycloalkyl or cycloalkenyl ring; and in formula (II), R.sub.1 and R.sub.2 are each hydrogen, a C.sub.1-4 alkyl, a C.sub.1-4 alkenyl or a C.sub.1-4 alkoxy, or R.sub.2 and R.sub.3 taken together form a 5- to 7-membered cycloalkyl or cycloalkenyl with R.sub.1 and R.sub.4 being a hydrogen atom, a C.sub.1-4 alkyl, a C.sub.1-4 alkenyl or a C.sub.1-4 alkoxy.

Retinoid compounds

Growing community of inventors

Pelham, AL, United States of America

Wayne J Brouillette