Novartis Ag

Astex Therapeutics Limited

Cellzome Limited

Amura Therapeutics Limited

Claudio Dagostin

Miles Stuart Congreve

Steven Howard

Bharat Lagu

Christopher Thomas Brain

Paul Mortenson

Yue Ping Li

Gilbert Besong

Troy Douglas Smith

Moo Je Sung

Andrew James Ratcliffe

Nigel Ramsden

Guo He

Wojciech Wrona

Kathryn Bell

Yipin Lu

Ying Hou

Nelly Piton

Clinton Alan Brooks

Michael Luzzio

Gianni Chessari

Alison Jo-Anne Woolford

Lawrence Blas Perez

Andrew James Woodhead

Martin Quibell

Fan Yang

Lee Patient

Christine Hiu-Tung Chen

Steven John Woodhead

John Paul Watts

Yaping Wang

Young Shin Cho

John William Giraldes

Steven Woodhead

Richard John Harrison

Sunkyu Kim

Marc O'Reilly

Cyrille Boussard

Steven Douglas Hiscock

Cyrille Broussard

Sally Oxenford

James Nally

Yikang Wang

Michael Joseph Luzzio

Moo Sung

Clinton A Brooks

Yue Li

Paul Neil Mortenson

John Grialdes

The disclosed compounds relate to treatments and therapies for protein kinase-associated disorders. There is also a need for compounds useful in the treatment or prevention or amelioration of one or more symptoms of cancer, transplant rejections, and autoimmune diseases. Furthermore, there is a need for methods for modulating the activity of protein kinases, such as CDK1, CDK2, CDK4, CDK5, CDK6, CDK7, CDK8 and CDK9, using the compounds provided herein. 

Pyrrolopyrimidine compounds and their uses

The invention relates to compounds of formula (I) wherein Xto X, Y, Zto Z, and R have the meaning as cited in the description and the claims. Said compounds are useful as JAK inhibitors for the treatment or prophylaxis of immunological, inflammatory, autoimmune, allergic disorders, and immunologically-mediated diseases. The invention also relates to pharmaceutical compositions including said compounds, the preparation of such compounds as well as the use as medicaments.

Heterocyclyl pyrazolopyrimidine analogues as JAK inhibitors

The present invention relates to compounds of formula (I) wherein Xto X, Y, Zto Z, and R have the meaning as cited in the description and the claims. Said compounds are useful as JAK inhibitors for the treatment or prophylaxis of immunological, inflammatory, autoimmune, allergic disorders, and immunologically-mediated diseases. The invention also relates to pharmaceutical compositions including said compounds, the preparation of such compounds as well as the use as medicaments.

Heterocyclyl pyrazolopyrimidine analogues as selective JAK inhibitors

The invention provides compounds of the formula (I): and salts, tautomers, solvates and N-oxides thereof;wherein Q is CH or N; X is N, N&#x2014;Oor CR; Y is N, N&#x2014;Oor CR; Rand Rare independently selected from hydrogen and various substituents as defined in the claims; or Rand Rtogether with the atoms to which they are attached, link to form an optionally substituted carbocyclic or heterocyclic aromatic or non-aromatic ring of 4 to 7 members; Ris selected from hydrogen and various substituents; and Ris selected from hydrogen and various substituents as defined in the claims. Also provided are pharmaceutical compositions containing the compounds of formula (I), processes for making the compounds and the medical uses of the compounds. The compounds of formula (I) have activity as inhibitors of CDK kinases and are useful in the treatment of inter alia proliferative diseases such as cancers.

Imidazole derivatives and their use as modulators of cyclin dependent kinases

The present invention relates to a process for preparing a compound of formula (Ia), (Ib), (Ic) or (Id), or a pharmaceutically acceptable salt, hydrate, solvate, complex or prodrug thereof, said process comprising the steps of: (A) (i) treating a compound of formula (IVa), where Ris alkyl or tosyl, with an oxidizing agent to form a compound of formula (Va); and (ii) converting said compound of formula (Va) to a compound of formula (Ia) or (Ic); or (B) (i) treating a compound of formula (IVb), where Ris alkyl or tosyl, with an oxidizing agent to form a compound of formula (Vb); and (ii) converting said compound of formula (Vb) to a compound of formula (Ib) or (Id). 

Tetrahydrofuro[3,2-b] pyrrol-3-one intermediates

Growing community of inventors

Cambridge, United Kingdom

Claudio Dagostin