Elan Pharmaceuticals, Inc.

Wyeth

Other

Imago Pharmaceuticals, Inc.

Ying-Zi Xu

Andrei William Konradi

Christopher Michael Semko

Eugene D Thorsett

Michael A Pleiss

Darren B Dressen

Francine S Grant

Jenifer Lea Smith

Susan Ashwell

Anthony Frank Kreft

Gregory Scott Welmaker

Frank Stappenbeck

Dimitrios Sarantakis

Kassandra Inez Rossiter

Juri Y Fukuda

Brian P Stupi

Simeon Bowers

Roy K Hom

Albert W Garofalo

Jing Wu

Shendong Yuan

Anh P Truong

Martin Neitzel

Matthew N Mattson

Francine S Farouz

Hing L Sham

Dean R Artis

Jacek J Jagodzinski

Xiaocong Michael Ye

Chris Semko

Jacek J Jagodinski

Michael A Pliess

Brian P Stupl

Dimitrios Sarntakis

David Wone

Compounds are provided having a structure according to Formula (I): wherein A, A, A, Y, R, R, R, R, R, R, m, n and p are defined herein. Further provided are pharmaceutical compositions including the compounds provided and methods of making and using the compounds and compositions as provided, e.g., in the treatment and prevention of various disorders, such as Alzheimer's disease. 

Spirocyclic dihydro-thiazine and dihydro-oxazine BACE inhibitors, and compositions and uses thereof

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 present invention provides compounds that are alpha4 integrin antagonists having a structure according to the following formula: or a tautomer, mixture of tautomers, salt or solvate thereof, wherein Cy, ring A, m, n, p, R, R, R, R, Rand Rare defined in the specification. The invention further provides pharmaceutical compositions including the compounds of the invention as well as methods of making and using the compounds and compositions of the invention, e.g., in the treatment and prevention of various conditions and disorders, such as Crohn's disease and ulcerative colitis.

Pyridinone antagonists of alpha-4 integrins

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, Crohn's 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 sulfonamide 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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Palo Alto, CA, United States of America

Ying-Zi Xu