Amgen Inc.

Takeda Pharmaceutical Company Limited

Thomas Nixey

Stephen A Hitchcock

Patricia Lopez

Qiufen May Xue

Wenge Zhong

Yuan Cheng

Ted Charles Judd

James A Brown

Holger Monenschein

Scott S Harried

Bryant Yang

Craig E Masse

Brian K Albrecht

Matthew M Weiss

Vinod Francis Patel

Thomas T Nguyen

Liping H Pettus

Hui-Ling Wang

Michael D Bartberger

Daniel La

Russell Graceffa

Lewis D Pennington

Michael D Croghan

Charles Kreiman

Randall W Hungate

Stuart C Chaffee

Christopher Hulme

Ryan Brown

Ning Chen

Mark Henry Norman

Robert Michael Rzasa

Matthew R Kaller

Elizabeth M Doherty

Jiawang Zhu

Celia Dominguez

Christopher Harold Fotsch

Markian Myroslaw Stec

James Richard Falsey

Vassil I Ognyanov

Nick A Paras

Partha P Chakrabarti

Jodie Katon

Denise Lyn Andersen

Andrew Stewart Tasker

Bin Wu

Anthony B Reed

Victor J Cee

Brian Alan Lanman

Ryan Paul Wurz

Vu Van Ma

Paul A Tempest

Bradley J Herberich

Timothy Powers

Claire L M Jackson

Dean Hickman

Christopher Michael Tegley

Gang Liu

Jian Jeffrey Chen

Joseph L Kim

Ana Elena Minatti

Benjamin Jones

Qi Huang

Daniel B Horne

Huikai Sun

Maria Hopkins

Shannon Rumfelt

Andre A Kiryanov

Kaustav Biswas

Adrian Leonard Smith

David Joseph St Jean, Jr

Jerry Ryan Holder

Guity P Balow

Frank Chavez

Sean Timothy Murphy

Matthew Lee

Jon Kuehler

Steve Fong Poon

Kate Ashton

Frenel Fils De Morin

Jason Green

Daniel Martin Retz

Jeffrey Petkus

Matthew K Kaller

Dan Horne

Jennifer Aral

James Brown

Adrian L Smith

Daniel M Retz

Disclosed are compounds of Formula 1 and pharmaceutically acceptable salts thereof, wherein L, R, R, R, R, R, X, X, X, X, X, and Z are defined in the specification. This disclosure also relates to materials and methods for preparing compounds of Formula 1, to pharmaceutical compositions which contain them, and to their use for treating diseases, disorders, and conditions associated with GPR6.

Piperidinyl- and piperazinyl-substituted heteroaromatic carboxamides as modulators of GPR6

The invention relates to bicyclic compounds of formulas I and Ia, and salts thereof. In some embodiments, the invention relates to inhibitors or modulators of Pim-1 and/or Pim-2, and/or Pim-3 protein kinase activity or enzyme function. In still further embodiments, the invention relates to pharmaceutical compositions comprising compounds disclosed herein, and their use in the prevention and treatment of Pim kinase related conditions and diseases, preferably cancer.

Azole compounds as PIM inhibitors

The present invention comprises a new class of compounds useful for the modulation of Beta-secretase enzyme activity and for the treatment of Beta-secretase mediated diseases, including Alzheimer's disease (AD) and related conditions. In one embodiment, the compounds have a general Formula I wherein ring A, B, B, B, L, R, R, Rand m of Formula I are defined herein. The invention also includes use of these compounds in pharmaceutical compositions for treatment, prophylactic or therapeutic, of disorders and conditions related to the activity of beta-secretase protein. Such disorders include, for example, Alzheimer's Disease (AD), cognitive deficits, cognitive impairment, schizophrenia and other central nervous system conditions related to and/or caused by the formation and/or deposition of plaque on the brain. The invention also comprises further embodiments of Formula I, intermediates and processes useful for the preparation of compounds of Formula I. 

Amino heteroaryl compounds as beta-secretase modulators and methods of use

The invention relates to bicyclic compounds of formula (1'), and salts thereof. In some embodiments, the invention relates to inhibitors or modulators of Pim-1 and/or Pim-2, and/or Pim-3 protein kinase activity or enzyme function. In still further embodiments, the invention relates to pharmaceutical compositions comprising compounds disclosed herein, and their use in the prevention and treatment of Pim kinase related conditions and diseases, preferably cancer. 

Bicyclic compounds as Pim inhibitors

The present invention comprises a new class of compounds useful for the modulation of Beta-secretase enzyme activity and for the treatment of Beta-secretase mediated diseases, including Alzheimer's disease (AD) and related conditions. In one embodiment, the compounds have a general Formula (I); wherein ring A, B, B, B, L, R, R, ring Z, m and n of Formula I are defined herein. The invention also includes use of these compounds in pharmaceutical compositions for treatment, prophylactic or therapeutic, of disorders and conditions related to the activity of beta-secretase protein. Such disorders include, for example, Alzheimer's Disease (AD), cognitive deficits, cognitive impairment, schizophrenia and other central nervous system conditions related to and/or caused by the formation and/or deposition of plaque on the brain. The invention also comprises further embodiments of Formula (I), intermediates and processes useful for the preparation of compounds of Formula (I). 

The present invention comprises a new class of compounds capable of modulating Raf kinase and, accordingly, useful for treatment of Raf kinase mediated diseases, including melanomas, tumors and other cancer-related conditions. The compounds have a general Formula I wherein Ris and A, A, A, A, X, Z, Z', R, R, R, R, Rand Rare defined herein. The invention further comprises pharmaceutical compositions, methods for treatment of Raf kinase mediated diseases, and intermediates and processes useful for the preparation of compounds of the invention.

Substituted pyrimidine compounds as RAF inhibitors and methods of use

The present invention comprises a new class of compounds useful for the modulation of Beta-secretase enzyme activity and for the treatment of Beta-secretase mediated diseases, including Alzheimer's disease (AD) and related conditions. In one embodiment, the compounds have a general Formula I wherein A, B, R, R, R, i and j are defined herein. The invention also comprises pharmaceutical compositions including one or more compounds of Formula I, methods of use for these compounds, including treatment of AD and related diseases, by administering the compound(s) of Formula I, or compositions including them, to a subject. The invention also comprises further embodiments of Formulas II and III, intermediates and processes useful for the preparation of compounds of the invention.

Beta-secretase modulators and methods of use

The present invention comprises a new class of compounds useful for the modulation of Beta-secretase enzyme activity and for the treatment of Beta-secretase mediated diseases, including Alzheimer's disease (AD) and related conditions. In one embodiment, the compounds have a general Formula I wherein A, B, W, R, R, R, i and j are defined herein. The invention also comprises pharmaceutical compositions including one or more compounds of Formula I, methods of use for these compounds, including treatment of AD and related diseases, by administering the compound(s) of Formula I, or compositions including them, to a subject. The invention also comprises further embodiments of Formulas II and III, intermediates and processes useful for the preparation of compounds of the invention.

Beta-Secretase modulators and methods of use

The present invention comprises a new class of compounds useful for the modulation of Beta-secretase enzyme activity and for the treatment of Beta-secretase mediated diseases, including Alzheimer's disease (AD) and related conditions. In one embodiment, the compounds have a general Formula I wherein R, W, B, R, R, R, i and j are defined herein. The invention also comprises pharmaceutical compositions including one or more compounds of Formula I, methods of use for these compounds, including treatment of AD and related diseases, by administering the compound(s) of Formula I, or compositions including them, to a subject. The invention also comprises further embodiments of Formulas II and III, intermediates and processes useful for the preparation of compounds of the invention.

Novel compounds, or pharmaceutically-acceptable salts, tautomers or prodrugs thereof, of Formula I wherein A, W, X, Z, R-R, and Rare as defined in the specification, are provided. Also provided are methods of treating or preventing a melanin concentrating hormone-mediated disorder in a subject, comprising administering to a subject in need of such treatment or prevention a compound of Formula I.

Melanin concentrating hormone receptor antagonist

Compounds having the general structure and compositions containing them, for the treatment of acute, inflammatory and neuropathic pain, dental pain, general headache, migraine, cluster headache, mixed-vascular and non-vascular syndromes, tension headache, general inflammation, arthritis, rheumatic diseases, osteoarthritis, inflammatory bowel disorders, inflammatory eye disorders, inflammatory or unstable bladder disorders, psoriasis, skin complaints with inflammatory components, chronic inflammatory conditions, inflammatory pain and associated hyperalgesia and allodynia, neuropathic pain and associated hyperalgesia and allodynia, diabetic neuropathy pain, causalgia, sympathetically maintained pain, deafferentation syndromes, asthma, epithelial tissue damage or dysfunction, herpes simplex, disturbances of visceral motility at respiratory, genitourinary, gastrointestinal or vascular regions, wounds, burns, allergic skin reactions, pruritus, vitiligo, general gastrointestinal disorders, gastric ulceration, duodenal ulcers, diarrhea, gastric lesions induced by necrotising agents, hair growth, vasomotor or allergic rhinitis, bronchial disorders or bladder disorders.

Vanilloid receptor ligands and their use in treatments

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Newbury Park, CA, United States of America

Thomas Nixey