Lifearc

Genentech, Inc.

Merck Sharp + Dohme Corp.

Suzhou Yabao Pharmaceutical R&d Co., Ltd.

Medical Research Council Technology

Edward Giles Mciver

Stephen John Lewis

Jon James Winter-Holt

Joanne Osborne

Martin Ambler

Kayleigh Webb-Smith

Zachary Kevin Sweeney

Anthony A Estrada

Huifen Chen

Bryan K Chan

Martin Richard Teall

Stephen Robert Fletcher

Paul Joseph Oakley

Daniel Shore

Lin Zhu

Frank Burkamp

Ling Wu

Yan Xia

Graham David Checksfield

Yang Song

Yuanyuan Xu

Chunjun Chu

Miao Liu

Justin Stephen Bryans

Joanne Hough

Denise Jamilla Harding

Ela Smiljanic

Joane Hough

The present invention relates to compounds of formulae I and H, or pharmaceutically acceptable salts or esters thereof. Further aspects of the invention relate to pharmaceutical compositions and therapeutic uses of said compounds in the treatment of diseases of uncontrolled cell growth, proliferation and/or survival, inappropriate cellular immune responses, inappropriate cellular inflammatory responses, or neurodegenerative disorders, preferably tauopathies, even more preferably. Alzheimer's disease. 

Fused thiazolopyrimidine derivatives as MNKs inhibitors

Provided are a substituted tricyclic heterocyclic compound of formula I or a stereoisomer, a tautomer, an N-oxide, a hydrate, a solvate, a metabolite, a pharmaceutically acceptable salt, ester or a prodrug thereof, a pharmaceutical composition including the same and uses thereof. The substituted tricyclic heterocyclic compounds and the pharmaceutical compositions comprising the compounds disclosed herein can be used for treating a disorder caused by at least one of cancer and neurodegenerative diseases. Further the compounds and the pharmaceutical compositions comprising the compounds disclosed herein can be also used for preventing or treating a disorder caused by, associated with or accompanied by any abnormal kinase activity. 

Substituted tricyclic heterocyclic compounds and use thereof

The present invention relates to compounds of formulae I and H, or pharmaceutically acceptable salts or esters thereof. Further aspects of the invention relate to pharmaceutical compositions and therapeutic uses of said compounds in the treatment of diseases of uncontrolled cell growth, proliferation and/or survival, inappropriate cellular immune responses, inappropriate cellular inflammatory responses, or neurodegenerative disorders, preferably tauopathies, even more preferably, Alzheimer's disease. 

Fused thiazolopyrimidine derivatives as MNKS inhibitors

The present invention relates to compounds of formulae I, or pharmaceutically acceptable salts or esters thereof, wherein: Ris selected from H and CO&#x2014;NRR, wherein Rand Rare each independently selected from H, alkyl, cycloalkyl and mono or bicyclic heterocycloalkyl, wherein said alkyl group is optionally substituted by one or more Rgroups, and said heterocycloalkyl is optionally substituted by Ror R; or Rand Rare linked, together with the nitrogen to which they are attached, to form a heterocycloalkyl group optionally containing one or more additional heteroatoms, and optionally substituted by one or more groups select from Rand (CH)R; Ris selected from H and alkyl, wherein said alkyl group is optionally substituted by one or more Rgroups; Ris selected from alkyl, cycloalkyl and heterocycloalkyl, each of which may be optionally substituted by halo, OH or alkoxy; Z, Z, Zand Zare all C; R, R, Rand Rare each independently selected from H, alkyl, CN, NO, OH, alkoxy, NHCO-alkyl, halo and haloalkyl; or Z, Zand Zare all C, Zis N, Ris absent and R, Rand Rare as defined above; or Z, Zand Zare all C, Zis N, Ris absent and R, Rand Rare as defined above; each Rand R11 is independently alkyl; each Ris independently selected from COR, COOH, OH, alkoxy, haloalkyl, NH, NHR, NRR, heteroaryl and heterocycloalkyl; Ris H or halo. Further aspects relate to pharmaceutical compositions and therapeutic uses of said compounds in the treatment of diseases of uncontrolled cell growth, proliferation and/or survival, inappropriate cellular immune responses, inappropriate cellular inflammatory responses, or neurodegenerative disorders, preferably tauopathies, even more preferably, Alzheimer's disease. 

Pyrropyrimidine compounds as MNKs inhibitors

The present invention relates to substituted pyrazolopyridine compounds, and pharmaceutically acceptable salts or esters thereof. The present invention further relates to therapeutic uses of pharmaceutical compositions comprising the substituted pyrazolopyridine compounds, for example, in cancer and neurodegenerative diseases.

Compounds and their administration for treating a neurodegenerative disease as well as a method for identifying a compound capable of inhibiting a kinase, such as LRRK

Tetrahydroindole derivatives of formula (I): are disclosed. These compounds modulate the activity of gamma-secretase and hence find use in treatment or prevention of Alzheimer's disease. 

Tetrahydroindole derivatives for treatment of alzheimer's disease

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London, United Kingdom

Edward Giles Mciver