Research Corporation Technologies, Inc.

Southern Methodist University

University of Central Florida Research Foundation, Inc.

Other

Alamx, LLC

John D Buynak

Venkata Ramana Doppalapudi

Akireddy Srinivasa Rao

Brian Bachmann

Greg C Adam

Kyle Rohde

Thu Q Nguyen

Sundar Ram Reddy Pagadala

Weirui Chai

Maha Alqurafi

Lakshminarayana Vogeti

Rashmi Gupta

A Srinivasa Rao

Noora M S A Al-Kharji

Anjaneyulu Sheri

Sirishkumar D Nidamarthy

Hansong Chen

The present invention includes a composition, method of making and method of using a novel C5-substituted carbapenem antibiotic of formula 1: 

C5-substituted carbapenem antibiotics, compositions containing such compounds, and methods of use in treatment of mycobacterium tuberculosis and non-tubercular mycobacteria

C5-substituted carbapenem antibiotics, compositions containing such compounds, and methods of use in treatment ofand non-tubercular mycobacteria

The present invention includes compositions, methods of making and using novel carbapenem compounds including active agents, compounds, antibacterial agents, pharmaceutically acceptable salts of C1&#x3b1;-C1&#x3b2; di-substituted carbapenem compounds, C5&#x3b1; substituted carbapenem compounds, C6&#x3b1;-C6&#x3b2; di-substituted carbapenem compounds and combinations thereof.

Methods of generating beta-lactamase resistant carbapenem compounds

Inhibitors of the enzyme beta-lactamase are provided comprising compounds of formula (II) wherein Ror Ris a pyridyl group and Ris a group of formula The compounds are adapted to inhibit beta-lactamase as produced by beta-lactam resistant bacterial strains. Methods of treatment of beta-lactam resistant bacterial infections in patients are provided.

Beta-lactamase inhibitory compounds

Inhibitors of the enzyme beta-lactamase of formula (I): 

The invention provides compounds of formula (I): wherein: R-Rand A have any of the values defined in the specification, and their pharmaceutically acceptable salts, are useful for inhibiting &#x3b2;-lactamase enzymes, for enhancing the activity of &#x3b2;-lactam antibiotics, and for treating &#x3b2;-lactam resistant bacterial infections in a mammal. The invention also provides pharmaceutical compositions, processes for preparing compounds of formula (I), and intermediates useful for the synthesis of compounds of formula (I).

7-alkylidene-3-substituted-3-cephem-4-carboxylates as beta-lactamase inhibitors

Compounds of formula I: wherein R, R, R, Rand n have any of the values defined in the specification, and their pharmaceutically acceptable salts, are useful for inhibiting &#x3b2;-lactamase enzymes, for enhancing the activity of &#x3b2;-lactam antibiotics, and for treating &#x3b2;-lactam resistant bacterial infections in a mammal. The invention also provides pharmaceutical compositions, processes for preparing compounds of formula I, and novel intermediates useful for the synthesis of compounds of formula I.

Penicillanic acid derivative compounds and methods of making

Compounds of formula (I):wherein R, R, R, Rand n have any of the values defined in the specification, and their pharmaceutically acceptable salts, are useful for inhibiting simultaneously serine and metallo-&#x3b2;-lactamase enzymes, for enhancing the activity of &#x3b2;-lactam antibiotics, and for treating &#x3b2;-lactam resistant bacterial infections in a mammal. The invention also provides pharmaceutical compositions, processes for preparing compounds of formula I, and novel intermediates useful for the synthesis of compounds of formula I.

Inhibitors of serine and metallo-&#x3b2;-lactamases

The invention provides compounds of formula (I):wherein: R-Rand A have any of the values defined in the specification, and their pharmaceutically acceptable salts, are useful for inhibiting &#x3b2;-lactamase enzymes, for enhancing the activity of &#x3b2;-lactam antibiotics, and for treating &#x3b2;-lactam resistant bacterial infections in a mammal. The invention also provides pharmaceutical compositions, processes for preparing compounds of formula (I), wherein Rand Rare each independently hydrogen, (C-C)alkyl, (C-C)alkenyl, (C-C)alkenyl, (C-C)cycloalkyl, (C-C)alkoxy, (C-C)alkanoyl, (C-C)alkanoyloxy, (C-C)alkoxycarbonyl, aryl, heterocycle, halo, cyano, nitro, &#x2014;COOR, &#x2014;C(&#x2550;O)NRR, &#x2014;OC(&#x2550;O)NRR, NRR, or &#x2014;S(O)R; Ris hydrogen, halo, aryl, heteroaryl, &#x2014;S(O)R, or &#x2014;CH&#x2550;CHC(&#x2550;O)NRR; Ris hydrogen; A is thio, sulfinyl, or sulfonyl; and intermediates useful for the synthesis of compounds of formula (I).

7-Alkylidene-3-substituted-3-cephem-4-carboxylates as &#x3b2;-lactamase inhibitors

The invention provides pharmaceutical compositions comprising compounds of formula I and IV:

Compositions for inhibiting beta-lactamase

Derivatives of 7-alkylidene cephalosporanic acid sulfone and the pharmaceutically active salts thereof are found to be potent inhibitors of &bgr;-lactamase enzymes.

Growing community of inventors

Dallas, TX, United States of America

John D Buynak