Vertex Pharmaceuticals, Inc.

Novartis Ag

Xiaoling Xie

Guy W Bemis

Francois Maltais

Jeremy Green

Michael Robin Hale

Qing Tang

Michael D Mullican

Jingrong Cao

James Walter Janetka

Christopher Todd Baker

Judith Straub

Keith P Wilson

William Markland

Michael Su

Yong Gu

Paul R Caron

Robert Mashal

Edward Fox

John Louis Diener

Tiancen Hu

Kathrin Ladetzki-Baehs

Felix Hartlepp

Xenia Karola Wezler

Lars Gadtke

Cesare Russo

Michael John Romanowski

This disclosure relates to anti-Natriuretic Peptide Receptor 1 (NPR1) antibodies including agonist antibodies which are able to activate the NPR1 receptor, pharmaceutical compositions comprising the same, and methods of treatment comprising the same.

Natriuretic peptide receptor 1 antibodies and methods of use

The present invention relates to molecules and molecular complexes which comprise the active site binding pockets of JNK3 or close structural homologues of the active site binding pockets.

Crystallization of C-Jun N-Terminal Kinase 3 (JNK3)

The present invention relates to a data storage medium encoded with the corresponding structure coordinates of molecules and molecular complexes which comprise the active site-binding pockets of JNK3. A computer comprising such data storage material is capable of displaying such molecules and molecular complexes, or their structural homologues, as a graphical three-dimensional representation on a computer screen. This invention also relates to methods of using the structure coordinates to solve the structure of homologous proteins or protein complexes. In addition, this invention relates to methods of using the structure coordinates to screen and design compounds, including inhibitory compounds, that bind to JNK3 or homologues thereof. This invention also relates to molecules and molecular complexes which comprise the active site binding pockets of JNK3 or close structural homologues of the active site binding pockets.

Methods of designing inhibitors for JNK kinases

Described herein are compounds that are useful as protein kinase inhibitors having the formula: where R, Q, and T are described in the specification. The compounds are useful for treating disease states in mammals that are alleviated by a protein kinase inhibitor, particularly diseases such as cancer, inflammatory disorders, restenosis, and cardiovascular disease.

Pyrazole compositions useful as inhibitors of erk

This invention provides a method of treating a disease state in mammals that is alleviated by treatment with a protein kinase inhibitor, especially an ERK inhibitor, which method comprises administering a compound having the pharmacophoric features Grp 1, Grp 2 and Grp 3:Grp 1 is an optionally substituted aryl or aliphatic group; Grp 2 is a heteroaromatic ring having one to three nitrogens, said ring comprising a hydrogen bond acceptor HBA2 optionally bonded to a hydrogen bond donor HBD2, and Grp 3 is a heteroaromatic ring comprising a hydrogen bond donor HBD1, with distances between the pharmacophoric features defined in the specification. The method is useful for treating cancer, stroke, diabetes, hepatomegaly, cardiovascular disease, Alzheimer's disease, cystic fibrosis, viral disease, autoimmune diseases, atherosclerosis, restenosis, psoriasis, allergic reactions, inflammation, neurological disorders or a hormone-related disease.

Compositions useful as inhibitors of ERK

This invention provides a method of treating a disease state in mammals that is alleviated by treatment with a protein kinase inhibitor, especially an ERK inhibitor, which method comprises administering a compound having the pharmacophoric features Grp1, Grp2 and Grp3: Grp 1 is an optionally substituted aryl or aliphatic group; Grp 2 is a heteroaromatic ring having one to three nitrogens, said ring comprising a hydrogen bond acceptor HBA2 optionally bonded to a hydrogen bond donor HBD2, and Grp3 is a heteroaromatic ring comprising a hydrogen bond donor HBD1, with distances between the pharmacophoric features defined in the specification. The method is useful for treating cancer, stroke, diabetes, hepatomegaly, cardiovascular disease, Alzheimer's disease, cystic fibrosis, viral disease, autoimmune diseases, atherosclerosis, restenosis, psoriasis, allergic reactions, inflammation, neurological disorders or a hormone-related disease.

Pyrazole compositions useful as inhibitors of ERK

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Cambridge, MA, United States of America

Xiaoling Xie