Elan Pharmaceuticals, Inc.

Wyeth

Other

Athena Neurosciences, Inc.

Christopher Michael Semko

Andrei William Konradi

Michael A Pleiss

Eugene D Thorsett

Ying-Zi Xu

Darren B Dressen

Francine S Grant

Anthony Frank Kreft

Dimitrios Sarantakis

Susan Ashwell

Jenifer Lea Smith

Gregory Scott Welmaker

Frank Stappenbeck

Louis John Lombardo

Reinhardt Bernhard Baudy

Michael S Dappen

Kassandra Inez Rossiter

Juri Y Fukuda

Albert W Garofalo

Brian P Stupi

Simeon Bowers

Christopher Joseph Soares

Anh P Truong

Francine S Farouz

Jay S Tung

Sukanto Sinha

Jing Wu

Theodore A Yednock

Roy K Hom

Kiev S Ly

Christine M Tarby

Martin Neitzel

Matthew N Mattson

Xiaocong Michael Ye

Robert Warren Sullivan

Minghua Sun

Lisa Claire McConlogue

Stephen B Freedman

Gary D Probst

Danielle Aubele

Ted A Yednock

Jacek J Jagodzinski

Elizabeth Messersmith

Raymond Ng

Michael A Pliess

Brian P Stupl

Dimitrios Sarntakis

Jacek J Jagodinski

Chris Vandevert

Stephen J Karlik

Disclosed is a process for preparing polymer conjugates of agricultural, therapeutic, and food additive compounds using Mitsunobu conditions.

Preparation of polymer conjugates of therapeutic, agricultural, and food additive compounds

Disclosed are compounds which bind VLA-4. Certain of these compounds also inhibit leukocyte adhesion and, in particular, leukocyte adhesion mediated by VLA-4. Such compounds are useful in the treatment of inflammatory diseases in a mammalian patient, e.g., human, such as asthma, Alzheimer's disease, atherosclerosis, AIDS dementia, diabetes, inflammatory bowel disease, rheumatoid arthritis, tissue transplantation, tumor metastasis and myocardial ischemia. The compounds can also be administered for the treatment of inflammatory brain diseases such as multiple sclerosis.

Carbamate compounds which inhibit leukocyte adhesion mediated by VLA-4

The current invention provides compounds having a structure according to Formulae 1, 2, 3, and 4: wherein the A-ring, B-ring, C-ring, m, n, R, R, and Rare as described in the specification. The invention also provides pharmaceutical compositions comprising compounds of Formulae 1, 2, 3, and 4, as well as methods of treating cognitive disorders, such as Alzheimer's disease. The invention further provides intermediates useful in preparing the compounds of Formulae 1, 2, 3, and 4.

N-sulfonamido polycyclic pyrazolyl compounds

Disclosed are conjugates exhibiting VLA-4 antagonistic properties. Certain of these conjugates also inhibit leukocyte adhesion and, in particular, leukocyte adhesion mediated by VLA-4. The conjugates of this invention are characterized as containing more than one VLA-4 inhibiting compound covalently attached to a bio-compatible polymer, such as polyethylene glycol. Conjugates of the invention are defined by formula I, wherein A, B, and q are described in the specification. Such conjugates are useful in the treatment of inflammatory diseases in a mammalian patient, e.g., human, such as asthma, Alzheimer's disease, atherosclerosis, AIDS dementia, diabetes, inflammatory bowel disease, rheumatoid arthritis, tissue transplantation, tumor metastasis, and myocardial ischemia. The conjugates can also be administered for the treatment of inflammatory brain diseases such as multiple sclerosis.

Multimeric VLA-4 antagonists comprising polymer moieties

Disclosed are compounds of the formula: and the pharmaceutically acceptable salts thereof wherein the variables A, n, R, R-Rand Q are defined herein. These compounds bind VLA-4. Certain of these compound also inhibit leukocyte adhesion and, in particular, leukocyte adhesion mediated by VLA-4. Such compounds are useful in the treatment of inflammatory diseases in a mammalian patient, e.g., human, such as asthma, Alzheimer's disease, atherosclerosis, AIDS dementia, diabetes, inflammatory bowel disease, rheumatoid arthritis, tissue transplantation, tumor metastasis and myocardial ischemia. The compounds can also be administered for the treatment of inflammatory brain diseases such as multiple sclerosis.

Imidazolone phenylalanine derivatives

Heteroaryl, heterocyclic and aryl compounds which inhibit leukocyte adhesion mediated by VLA-4

Disclosed are compounds which bind VLA-4. Certain of these compounds also inhibit leukocyte adhesion and, in particular, leukocyte adhesion mediated by VLA-4. Such compounds are useful in the treatment of inflammatory diseases in a human or animal subject such as asthma, Alzheimer's disease, atherosclerosis, AIDS dementia, diabetes, inflammatory bowel disease, rheumatoid arthritis, tissue transplantation, tumor metastasis and myocardial ischemia. The compounds can also be administered for the treatment of inflammatory brain diseases such as multiple sclerosis.

Pyrimidinyl amide compounds which inhibit leukocyte adhesion mediated by VLA-4

The invention provides N-cyclic sulfonamido compounds and salts of Formula I:  wherein A is as described in the specification and Rand Rcombine to form a [3.3.1] or a [3.2.1] ring system, where the nitrogen is attached to the two bridgehead carbons, and the [3.3.1] or [3.2.1] ring systems are optionally fused with an heteroaryl or heterocycloalkyl ring. Compounds of Formula I are useful in treating or preventing cognitive disorders, such as Alzheimer's Disease. The invention also encompasses pharmaceutical compositions comprising compounds of Formula I, methods of treating cognitive disorders, such as Alzheimer's disease, and the intermediates useful in preparing the compounds of Formula I.

Bridged N-cyclic sulfonamido inhibitors of gamma secretase

Disclosed are certain alpha amino acid compounds which bind VLA-4. Certain of these compounds also inhibit leukocyte adhesion and, in particular, leukocyte adhesion mediated by VLA-4. Such compounds are useful in the treatment of inflammatory diseases in a mammalian patient, e.g., human, such as asthma, Alzheimer's disease, atherosclerosis, AIDS dementia, diabetes, inflammatory bowel disease, rheumatoid arthritis, tissue transplantation, tumor metastasis and myocardial ischemia. The compounds can also be administered for the treatment of inflammatory brain diseases such as multiple sclerosis.

Alpha amino acid derivatives-inhibitors of leukocyte adhesion mediated by VLA-4

The invention provides N-cyclic sulfonamido compounds of Formula I wherein A, B, R, R, R, R, Rand Rare as described in the specification. Compounds of Formula I are useful in treating or preventing cognitive disorders, such as Alzheimer's disease. The invention also encompasses pharmaceutical compositions comprising compounds of Formula I, methods of preparing compounds of formula I, and methods of treating cognitive disorders, such as Alzheimer's disease.

5-(arylsulfonyl)-pyrazolopiperidines

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Fremont, CA, United States of America

Christopher Michael Semko