Ligand Pharmaceuticals, Inc.

Abbott Laboratories Corporation

Other

Alex M Nadzan

Marcus F Boehm

Chan Kou Hwang

Beth Ann Badea

Richard Alan Heyman

Steven K White

Lin Zhang

Youssef L Bennani

Chun W Lin

Lin Zhi

Luc J Farmer

Mark W Holladay

James F Kerwin

Kazumi Shiosaki

Youe-Kong Shue

Jonathan J Hebert

Steve White

Stacie S Canan Koch

David S Garvey

Jerry R Martin

John S Tadanier

Michael D Tufano

Stephen Hanessian

Paul D May

John Y Chung

George Richard Granneman

Andre G Pernet

Hana A Kopecka

Ranjan Mukherjee

Hugh N Nellans

Paulette Johnson

John Kloss

Elizabeth A Allegretto

Laura J Dardashti

Deepak S Lala

Chan Kou (Jack) Hwang

Mark S Brodie

Stacie Canan-Koch

Compounds, compositions, and methods for modulating processes mediated by Retinoid X Receptors using retinoid-like compounds which have activity selective for members of the subclass of Retinoid X Receptors (RXRs), in preference to members of the subclass of Retinoic Acid Receptors (RARs). Examples of such compounds are bicyclic benzyl, pyridinyl, thiophene, furanyl, pyrrole, and polyenoic acid derivatives including carbocyclic polyenoic acids. The disclosed methods employ compounds for modulating processes selectively mediated by Retinoid X Receptors.

Compounds having selective activity for retinoid X receptors, and means for modulation of processes mediated by retinoid X receptors

Dimer-selective RXR modulator compounds having agonist, partial agonist and/or antagonist activity in the context of an RXR homodimer and/or RXR heterodimers are provided. Also provided are pharmaceutical compositions incorporating such dimer-selective RXR modulator compounds and methods for their therapeutic use.

Dimer-selective RXR modulators and methods for their use

The present invention relates to non-secosteroidal compounds which activate and modulate the vitamin D receptor (VDR). Because compounds of the present invention display many of the beneficial properties of 1,25(OH),D,, but with reduced calcium mobilization effects, they may be used advantageously to treat and prevent conditions that show vitamin D sensitivity. Such disease states typically show abnormal calcium regulatory, abnormal immune responsive, hyperproliferative, and/or neurodegenerative characteristics.

Vitamin D3 mimics

Novel trienoic retinoid compounds having activity for retinoic acid receptors and retinoid X receptors are provided. Also provided are pharmaceutical compositions incorporating such compounds and methods for their use.

Trienoic retinoid compounds and methods

Compounds, compositions, and methods for modulating processes mediated by Retinoid X Receptors using retinoid-like compounds which have activity selective for members of the subclass of Retinoid X Receptors (RXRs), in preference to members of the subclass of Retinoic Acid Receptors (RARs). Examples of such compounds are bicyclic benzyl, pyridinyl, thiophene, furanyl, pyrrole, and poiyenoic acid derivatives including carbocyclic polyenoic acids. The disclosed methods employ compounds for modulating processes selectively mediated by Retinoid X Receptors.

Compounds having selective activity for Retinoid X Receptors, and means

Tricyclic retinoids having activity for retinoic acid receptors and/or retinoid X receptors are provided. Also provided are pharmaceutical compositions incorporating such tricyclic retinoid compounds and methods for their therapeutic use.

Tricyclic retinoids, methods for their production and use

Novel trienoic compounds having activity for retinoic acid receptors and retinoid X receptors are provided. Also provided are pharmaceutical compositions incorporating such compounds and methods for their use.

Peptide analog type-B CCK receptor ligands or pharmaceutically-acceptable salts thereof, which are useful for treating central nervous system disorders, substance abuse, gastrointestinal disorders, endocrine disorders, eating-related disorders and for the treatment of shock, respiratory and cardiocirculatory insufficiencies.

Peptide analog type-B CCK receptor ligands

Selective and potent Type-A CCK receptor agonists of formula (I):

Derivatives of tetrapeptides as CCK agonists

A compound of the formula: ##STR1## wherein R.sub.1 and R.sub.2 are substituents; R.sub.6 is hydrogen, loweralkyl, cycloalkyl, loweralkenyl, arylalkyl, (substituted aryl)alkyl, or (heterocyclic)alkyl; B is a bond, an alkylene group, an alkenylene group, an alkadienylene group or a heteroatom containing linking group; D is a substituted acyl group or tetrazolyl; Z is CO, C(S) or S(O).sub.2 ; Ar is a heterocyclic group; and n is 1 to 3. Also disclosed are a composition and a method for antagonizing CCK, a composition and method for treating or preventing gastrointestinal, central nervous, appetite regulating and pain regulating systems, a composition and method for treating or preventing hyperinsulinemia, methods of making the compounds and intermediates useful in making the compounds.

Derivatives of D-glutamic acid and D-aspartic acid

This invention relates to a product which will provide a high caloric source upon I.V. administration. More particularly, this invention relates to glucosyl esters of malonic acids and substituted malonic acid derivatives which will permit the assimilation of glucose into the body at high concentrations but with low toxicity.

High caloric product for I.V. administration

Described are compounds of the formula ##STR1## wherein R is hydrogen or loweralkyl; R.sub.1 is --OR.sub.2 or --NR.sub.2 R.sub.3 wherein R.sub.2 and R.sub.3 independently of one another denote hydrogen or loweralkyl; n is 0 or 1; R.sub.4 and R.sub.5 independently of one another denote loweralkyl or together form a 5 or 6 membered cycloalkyl substituted by hydrogen or loweralkyl, and together with the nitrogen atom, form a ring; and pharmaceutically acceptable salts thereof and their use as anticonvulsant agents in a method of controlling convulsions or seizures.

N-alkylated carboxylic acid derivatives as anti-convulsant agents

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San Diego, CA, United States of America

Alex M Nadzan