146396-04-5Relevant articles and documents
1-(TRIAZIN-3-YL/PYRIDAZIN-3-YL)-PIPER(-AZINE)IDINE DERIVATIVES AND COMPOSITIONS THEREFOR FOR INHIBITING THE ACTIVITY OF SHP2
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Paragraph 0325; 0326, (2017/01/23)
The present invention relates to compounds of formula I: in which Y1, Y2, Y3, R1, R2a, R2b, R3a, R3b, R4a, R4b, R5a, R5b are defined in the Summary of the Invention; capable of inhibiting the activity of SHP2. The invention further provides a process for the preparation of compounds of the invention, pharmaceutical preparations comprising such compounds and methods of using such compounds and compositions in the management of diseases or disorders associated with the aberrant activity of SHP2.
COMPOUNDS AND COMPOSITIONS FOR INHIBITING THE ACTIVITY OF SHP2
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Paragraph 00281, (2017/01/02)
The present invention relates to compounds of formula I. The compounds are inhibitors of the Src Homolgy-2 phosphatase (SHP2) and thus useful in the treatment of Noonan Syndrome, Leopard Syndrome and cancer.
The design and discovery of novel amide CCR5 antagonists
Pryde, David C.,Corless, Martin,Fenwick, David R.,Mason, Helen J.,Stammen, Blanda C.,Stephenson, Peter T.,Ellis, David,Bachelor, David,Gordon, David,Barber, Christopher G.,Wood, Anthony,Middleton, Donald S.,Blakemore, David C.,Parsons, Gemma C.,Eastwood, Rachel,Platts, Michelle Y.,Statham, Keith,Paradowski, Kerry A.,Burt, Catherine,Klute, Wolfgang
supporting information; scheme or table, p. 1084 - 1088 (2009/08/07)
The synthesis of a range of novel amine-containing structures and their primary potency as inhibitors of HIV-1 fusion via blocking of the CCR5 receptor is described. The development of the medicinal chemistry strategy and SAR's which led to the identification of the piperidine amide compounds 33 and 36 as excellent leads for further evaluation is described, along with key physicochemical data which highlighted their lead potential.