Taimed Biologics, Inc.

Ambrilia Biopharma, Inc.

Taimed Biologies, Inc.

Guy Milot

Brent Richard Stranix

Jean-Emmanuel Bouchard

Jean-Francois Lavallee

Nicolas Leberre

Dominik Herbart

Chandra Panchal

Stephane Branchaud

Francis Beaulieu

Wang Zhigang

Réjean Ruel

Chandra J Panchal

Marco Petrella

Michael Ge

Jinzi J Wu

Stéphane Branchaud

The present invention relates to pyridoxine (vitamin B) derived compounds of formula (I), pharmaceutically acceptable salts, or solvates thereof, wherein R, R, R, A, L Band Bare as defined in the specification, and pharmaceutical compositions comprising the compounds. Compounds of formula (I) inhibit Human Immunodeficiency Virus (HIV)-integrase enzyme and are useful for preventing and treating HIV infection and AIDS. 

HIV integrase inhibitors from pyridoxine

The present invention provides HIV protease inhibitors of formulas I, IA, IB, Ib or II, or pharmaceutically acceptable salts thereof, wherein Rmay be, for example, 2-pyridyl-CH&#x2014;, 3-pyridyl-CH&#x2014;, 4-pyridyl-CH&#x2014;, a sulfonyl group as described in the formulas herein including benzenesulfonyl or thiophenesulfonyl groups, R&#x2014;CO)&#x2014;, Rbeing selected from the group consisting of piperonyl, 2-pyranzinyl (unsubstituted or substituted with H, or an alkyl of 1 to 4 carbon atoms) or a picolylamine group as described herein, wherein R3 may be, for example, a phenyl group or diphenylmethyl group as described herein, and wherein Cx may be, for example, COOH, CONRR, CHOH or CHOR.

Protease inhibitors

The present invention relates to methods of treating hepatitis C infection, HIV infection, AIDS, or AIDS-related complex, or inhibiting HIV replication by administering a compound of Formula I  or pharmaceutically acceptable salts thereof, to a mammal.

Derivatives of pyridoxine for inhibiting HIV integrase

The present invention provides processes for synthesizing lysine based compounds of the formula; wherein Rmay be, for example, (HO)P(O)&#x2014;, (NaO)P(O)&#x2014;, wherein X may be, for example, NH, Y may be H, F, Cl, or Br, and wherein n, X', Y&#x2032;, R, R, R, Rand Rare as defined herein.

Lysine-based prodrugs of aspartyl protease inhibitors and processes for their preparation

The present invention provides HIV protease inhibitors of formulas I, IA, IB, Ib or II, or pharmaceutically acceptable salts thereof, wherein Rmay be, for example, 2-pyridyl-CH&#x2014;, 3 -pyridyl-CH&#x2014;, 4-pyridyl-CH&#x2014;, a sulfonyl group as described in the formulas herein including benzenesulfonyl or thiophenesulfonyl groups, R&#x2014;CO&#x2014;, Rbeing selected from the group consisting of piperonyl, 2-pyrazinyl (unsubstituted or substituted with H, or an alkyl of 1 to 4 carbon atoms) or a picolylamine group as described herein, wherein R3 may be, for example, a phenyl group or diphenylmethyl group as described herein, and wherein Cx may be, for example, COOH, CONRR, CHOH or CHOR.

The present invention relates to compounds of Formula I or pharmaceutically acceptable salts, solvates or formulations thereof. Compounds of Formula I inhibit HIV-integrase enzyme and are useful for preventing and treating of HIV infection, acquired immune deficiency syndrome (AIDS), AIDS-related complex (ARC), hepatitis C, and other diseases and conditions caused or mediated by HIV infection.

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Longueuil, Canada

Guy Milot