Sun Pharma Advanced Research Company Limited

Sun Pharmaceutical Industries Limited

Hemant Ashvinbhai Chokshi

Rajamannar Thennati

Trinadha Rao Chitturi

Prabal Sengupta

Sabbirhusen Yusufbhai Chimanwala

Varun Anilkumar Mehta

Ajay Sohanlal Midha

Chitturi Trinadha Rao

Dipali Manubhai Desai

Chetan Surjitsingh Puri

Jonathan David Atkinson

The present invention relates to novel amidoheteroaryl aroyl hydrazide ethynes as tyrosine kinase inhibitors, process of preparation thereof, and use of the compounds for preparation of pharmaceutical compositions in the therapeutic treatment of disorders related to tyrosine kinases in humans.

Amidoheteroaryl aroyl hydrazide ethynes

The present invention relates to novel diarylacetylene hydrazide compounds of formula (I) or pharmaceutically acceptable salt thereof, as tyrosine kinase inhibitors, the process for their preparation, and to the use of the compounds of formula (I) in the preparation of pharmaceutical compositions for the therapeutic treatment of disorders related to tyrosine kinases, in warm-blooded animals. 

Diarylacetylene hydrazide containing tyrosine kinase inhibitors

A compound of formula I wherein X, Y, X' & Y&#x2032; are selected from hydrogen, halogen, substituted or unsubstituted alkyl (linear, branched or cyclo), aryl, alkyloxy and haloalkyl group; R, R, R& Rare selected from hydrogen, substituted or unsubstituted alkyl groups (linear, branched or cyclo), aryl, heteroaryl groups or aralkyl groups, heterocycles containing one or more of hetero atoms (viz., N, S, O), substituted or unsubstituted alkenyl or alkynyl groups of carbon 2 to 6; wherein the substituents R& Ron the piperazinyl moiety are either syn or anti to each other and optionally Rand Rtogether with the carbons to which they are attached form a monocyclic saturated or aryl or substituted aryl or heteroaryl or substituted heteroaryl ring containing one or more hetero atoms selected from N, S and O with a ring size ranging from 3 to 6; with a proviso that when R& Rtogether do not form part of a ring they may exist in either E or Z configuration; Ris (CH)&#x2014;O&#x2014;CH&#x2014;CO-Z wherein n is 1 to 6; Z is selected from OH, OR, NRR&#x2032;, N(OR)R&#x2032;, N(R)&#x2014;N(R)R&#x2032;and wherein R & R&#x2032; are selected from hydrogen, substituted or unsubstituted alkyl groups (linear, branched or cyclo), aryl, heteroaryl groups or aralkyl groups, heterocycles containing one or more of hetero atoms (viz., N, S, O), substituted or unsubstituted alkenyl or alkynyl groups of carbon 2 to 6; and B is selected from &#x2014;(CH)n-(n is 1 to 6) and &#x2014;(CH)x-D-(CH)y where D is O, NR, S or SO, x and y are independently 1 to 6; and m is selected from 1 to 6; and pharmaceutically acceptable salts thereof.

4-(diarylmethyl)-1-piperazinyl derivatives

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Baroda, India

Hemant Ashvinbhai Chokshi