University of Massachusetts

Bridge Pharma Inc.

Glsynthesis Inc.

Other

Boston University

Microbiotix, Inc.

George Edward Wright

A K Gunnar Aberg

Jan L Chen

Andrew T Maioli

Neal C Brown

Ivan Yanachkov

Wei-Chu Xu

Chengxin Zhi

Marjorie H Barnes

Earl F Baril

Ronald McCaffrey

Ivan Borissov Yanachkov

Gunnar A K Aberg

The invention features compounds of formula (I): The compounds are useful as antibacterial agents, especially again-associated diseases. 

Selective antibacterials for clostridium difficile infections

The invention features compounds of formula I and methods of their use as antiplatelet and antithrombotic compounds: H/N=Q&#x3c7;2OOOO&#x39b;Q2-N, HR6/NIf)(^XMO-M&#x3b3;&#x3c4;OM&#xb0;&#x3c4;X1MQ')r(^rfHOOHHOOQHiN&#x3c7;iR2 Formula (I). 

Antithrombotic diadenosine tetraphosphates and related analogs

This invention features bis-amides of pyrophosphoric acid and bisphosphonic acids, their preparation, and their use in synthesis of P,P-dinucleoside tetraphosphates, tetraphosphonates, and related compounds.

Reactive pyrophosphoric and bisphosphonic acid derivatives and methods of their use

Racemic norketotifen, racemic 10-hydroxy-ketotifen, racemic 10-hydroxy-nor-ketotifen and optically active isomers of ketotifen, norketotifen, 10-hydroxy-ketotifen and 10-hydroxy-norketotifen were found to have antiallergic and anti-inflammatory effects while being devoid of the severe dose-limiting sedative side effects of Ketotifen.

Optically active isomers of ketotifen and therapeutically active metabolites thereof

Composition and methods are disclosed that include a synergistic combination of an inhibitor of Herpes simplex virus thymidine kinase, and an antiherpes substance.

Antiherpes drug combinations

The present invention relates to new tetralin compounds, the methods of preparing said tetralin compounds, the method of using said tetralin compounds as local anesthetics and dermal anesthetics, said compounds having particularly valuable properties as dermal and topical anesthetics in mammals, including man, as well as compositions containing said compounds.

Dermal anesthetic compounds and pharmaceutical compositions for inducing local anesthesia and mitigating neuropathic pain

Racemic norketotifen, racemic 10-hydroxy-ketotifen, racemic 10-hydroxy-nor-ketotifen and optically active isomers of ketotifen, norketotifen, 10-hydroxy-ketotifen and 10-hydroxy-norketotifen were found to have antiallergic and anti-inflammatory effects while being devoid of the severe dose-limiting sedative side effects of ketotifen.

The present invention relates to smooth muscle spasmolytic agents, pharmaceutical compositions containing them and method of using said compounds and compositions for the treatment of urinary incontinence, and other smooth muscle contractility conditions. More particularly, the present invention relates to certain metabolically stabilized secondary amines having smooth muscle relaxing properties while avoiding, on administration to a mammal, adverse side effects such as prominent antimuscarinic, arrhythmogenic and cardiodepressive effects.

Smooth muscle spasmolytic agents

The invention features compounds of the formula:or a pharmaceutically acceptable salt thereof, wherein A is CRand B is N; wherein n is 0-3; wherein Ris (CH)&#x2014;{(G)&#x2014;(CH)}&#x2014;L, in which G is CH, CH&#x2550;CH, C&#x2261;C, CO, O, S, or NR, where Ris H or Calkyl, CHR, where Ris OH or Calkyl, CH(CRR), where each of Rand Ris, independently, H, halo, or Calkyl, OCO, CONR, NRCO, where each of Rand Ris, independently, H or Calkyl, SONH, or NHSO; in which m is 1-4, o is 0-4, p is 0-4, and q is 0-4. The compounds disclosed herein have potent anti-microbial, e.g., both Gram-positive and Gram-negative anti-bacterial properties. The compounds inhibit DNA polymerase IIIC and DNA polymerase IIIE enzymes and thus act therapeutically by inhibiting the growth of a broad array of bacteria. The compounds can be administered to prevent or to treat Gram-positive or Gram-negative bacterial infections, e.g., in eukaryotic cell cultures, animals, or humans.

Purine and isosteric antibacterial compounds

The invention provides heterocyclic organic compounds that inhibit bacterial DNA polymerase IIIC and type II bacterial topoisomerase. The invention further provides compounds that are useful as intermediates in the synthesis of such heterocyclic organic compounds. Syntheses and uses of such heterocyclic organic molecules are also described.

Heterocyclic antibacterial compounds

The invention relates to prodrugs of N-substituted derivatives of 6-aminouracils, 6-aminoisocytosines, guanines, and 2-aminoadenines. The N-linked substituents include an ester group that is cleaved upon administration into a subject to yield a substituent having a terminal hydroxyl group. Pharmaceutical compositions including these compounds, and methods for treating Gram-positive bacterial infections using these compounds, are also disclosed.

Antibiotic prodrugs

The invention relates to antimicrobial compounds which interact with zinc in a zinc finger of a bacterial DNA polymerase, methods of screening for such compounds, and methods of using such compounds to inhibit polymerase activity or bacterial growth.

Zinc finger-reactive antimicrobial compounds

The present invention relates to new aminoindane piperidine compounds, the method of using aminoindane compounds as local anesthetics, said compounds having particularly valuable properties as dermal and topical anesthetics in mammals, including man, as well as compositions containing said compounds.

Dermal anesthetic agents

Disclosed are N-substituted hydroxyalkyl or carboxyalkyloxyalkyl analogs of 9- and/or 10-oxo-4Hbenzo&lsqb;4,5&rsqb;cycloheptal&lsqb;1,2-b&rsqb;thiophene compounds, or 9-OH and/or 10-OH-substituted analogs thereof, which possess antihistaminic and antiasthmatic properties with reduced sedative side effects. The optically active isomers and pharmaceutically acceptable salts thereof are also described. The compounds were also found to prevent smooth muscle hyperreactivity.

Growing community of inventors

Worcester, MA, United States of America

George Edward Wright