Viro Chem Pharma, Inc.

Societe De Conseils De Recherches Et D'applications Scientifiques (s.c.r.a.s.)

Ipsen Pharma S.a.s.

Vertex Pharmaceuticals, Inc.

Societe De Conseils De Recherches Et D'applications Scientifiques

Christophe Moinet

Laval Chan Chun Kong

Christophe Thurieau

Marc Courchesne

Monica Bubenik

Louis Vaillancourt

Jérôme Gonzalez

Thumkunta Jagadeeswar Reddy

Oswy Z Pereira

Carole Sackur

Liliane Halab

Charles Blais

Ming-Qiang Zhang

Nathalie Chauret

Barry A Morgan

Thomas D Gordon

Carl Poisson

Lydie Francine Poitout

Constantin G Yannopoulos

Bingcan Liu

Caroline Cadilhac

Marie-Odile Galcera

Melanie Proulx

Dennis C H Bigg

Réal Denis

Paul Nguyen-Ba

Nathalie Turcotte

The invention relates to 21-keto triterpene compounds of formula (I): wherein R, X and Y are as defined herein, and pharmaceutically acceptable salts and solvates thereof. These compounds exhibit significant anti-HIV activity. Thus, the invention also relates to methods for prevention or treatment of HIV infections by administering therapeutically effective amounts of a compound of formula (I), or a pharmaceutically acceptable salt or solvate thereof to a subject in need of such treatment.

C-21-keto lupane derivatives preparation and use thereof

The invention relates to 21-keto triterpene compounds of formula (I): wherein R, X, and Y are as defined herein, and pharmaceutically acceptable salts and solvates thereof. These compounds exhibit significant anti-HIV activity. Thus, the invention also relates to methods for prevention or treatment of HIV infections by administering therapeutically effective amounts of a compound of formula (I), or a pharmaceutically acceptable salt or solvate thereof to a subject in need of such treatment. 

Lupane derivatives useful for treating HIV

Compounds according to formula (I): wherein R, R, R, n and X are defined as defined herein, and the pharmaceutically acceptable salts, hydrates and solvates thereof, are useful for the modulation of CCR5 chemokine receptor activity. Additionally, compounds according to Formula III: wherein Z, R', and R&#x2032;are defined as defined herein, and the pharmaceutically acceptable salts, hydrates and solvates thereof, are useful as intermediates for production of compounds that modulate CCR5 chemokine receptor activity.

Spirotropane compounds

A subject of the present application is new derivatives of 4-aminopiperidines of formula in which R, Rand Rrepresent various radical, and their preparation processes by synthetic methods in parallel in liquid and solid phase. These products having a good affinity with certain sub-types of somatostatin receptors, they are particularly useful for treating the pathological states or diseases in which one (or more) somatostatin receptors are involved.

Derivatives of 4-aminopiperidine and their use as a medicament

Compounds according to formula (I): wherein A, Rand Rare as defined herein, and the pharmaceutically acceptable salts, hydrates and solvates thereof are useful for the modulation of CCR5 chemokine receptor activity.

Spirotropane compounds and methods for the modulation of chemokine receptor activity

Compounds according to formula (I): wherein A, R, Rand Rare defined as defined herein, and the pharmaceutically acceptable salts, hydrates and solvates thereof, are useful for the modulation of CCR5 chemokine receptor activity.

Novel compounds represented by formula (I): wherein R, R, Rand Rare as defined herein, and pharmaceutically acceptable salts, hydrates and solvates thereof, are useful for the modulation of CCR5 chemokine receptor activity.

Spirohydantoin compounds and methods for the modulation of chemokine receptor activity

The present invention is directed to imidazolyl derivatives of formula (I) where the substituents are defined in the specification, which are useful as agonist or antagonists of somatostatin receptors.

Imidazolyl derivatives

Compounds of formula I wherein R, R, R, Rand Rare as defined herein, or pharmaceutically acceptable salts, hydrates or solvates thereof, are useful for the modulation of CCR5 chemokine receptor activity.

Compounds of formula I wherein X, Y, Z, W, Rand Ras defined herein, or pharmaceutically acceptable salts, hydrates or solvates thereof, are useful for the modulation of CCR5 chemokine receptor activity.

Spiro compounds and methods for the modulation of chemokine receptor activity

The present invention is drawn to compounds of the formula in racemic and enantiomeric form or all combinations of these forms wherein the various substituents are as defined in the application which compounds have a good affinity for certain subtypes of somatostatin receptors and have useful pharmacological properties.

Derivatives of 2-arylimino-2,3-dihydrothiazoles, their preparation processes and their therapeutic use

A subject of the present application is new derivatives of 4-aminopiperidines of formulain which R, Rand Rrepresent various radical, and their preparation processes by synthetic methods in parallel in liquid and solid phase. These products having a good affinity with certain sub-types of somatostatin receptors, they are particularly useful for treating the pathological states or diseases in which one (or more) somatostatin receptors are involved.

4-aminopiperidine and their use as a medicine

The invention concerns novel 2-arylimino-2,3-dihydrothiazole derivatives of general formula (I), their preparation methods and their use as medicines, in particular for treating pathological conditions or diseases wherein one (or several) somatostatin receptors is/are involved. Said pathological conditions include in particular acromegaly, pituitary adenoma or endocrine gastroenteropanceatic tumors including the carcinoid syndrome, and gastrointestinal bleeding. In general formula (I), R1 represents in particular an alkyl, aralkyl, cyclohexyl radical optionally substituted by an amino radical or R1 represents a &mdash;C(R11)(R12)&mdash;CO&mdash;R10 radical wherein R11 represents H, R12 represents in particular H, carbocyclic or heterocyclic alkyl, cycloalkyl or aralkyl and R10 represents in particular an aminoalkylamino radical; R2 represents a carcyclic or heterocyclic aryl radical optionally substituted; R3 represents in particular COR5 or a carbocyclic or heterocyclic alkyl, adamantyl, aryl radical optionally substituted, carbocyclic or heterocyclic aralkyl optionally substituted on the aryl group; and R5 represents a radical fixed by a nitrogen atom to the group CO.

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Montreal, Canada

Christophe Moinet