Wyeth

Wyeth Holdings Corporation

Yanzhong Wu

Panolil C Raveendranath

David Michael Blum

Jean Schmid

Jay Thomas Afragola

Semiramis Ayral-Kaloustian

Bogdan Kazimierz Wilk

Timothy John Doyle

Nan Zhang

Mannching Sherry Ku

Sreenivasulu Megati

Arkadiy Zinoviy Rubezhov

Jianxin Ren

Mousumi Ghosh

Zhixian Ding

Thurairajah Padmanathan

Karen Sutherland

Mahmut Levent

Charles Chao Wu

Constantine Gletsos

Xinxu Shi

Haris Durutlic

Wei Tong

John Thomas Kendall

Thai Nguyen

Fang Fang Qi

Panolil Raveendrath

Processes for preparing oxindoles, which can be utilized in the preparation of a variety of useful compounds, and methods for minimizing or preventing N-alkylation of amide containing compounds, including oxindoles, are provided. Also provided is a compound of the following structure: 

Process for the synthesis of progesterone receptor modulators

A process for making a compound of formula I and intermediate compounds thereof, wherein Ris CN, F or Cl; Ris H or Br; and Rand Rare each independently H or F. The compounds of formula I are useful in the treatment of chronic inflammatory diseases, such as rheumatoid arthritis.

Process for the synthesis of 3-(3-fluoro-4-hydroxyphenyl)-7-hydroxynaphthonitrile

There is provided a process for the preparation of substituted amino alcohols HO&#x2014;(CH)&#x2014;NRRfrom haloalcohols HO&#x2014;(CH)&#x2014;X, where X is Cl, Br or I, by reaction with an amine HNRR, in water as solvent at a temperature range of about 20&#xb0; C. to about 90&#xb0; C. optionally in the presence of a catalytic amount of an iodide source metal iodides. The haloalcohols are useful in the preparation of 6-[(substituted)phenyl]-triazolopyrimidine compounds which are useful in the treatment of cancer.

Process for preparation of substituted amino alcohols

This invention relates to certain 6-[(substituted)phenyl]triazolopyrimidine compounds or pharmaceutically acceptable salts thereof, and compositions containing said compounds or pharmaceutically acceptable salts thereof, wherein said compounds are anti-cancer agents useful for the treatment of cancer in mammals. This invention further relates to a method of treating or inhibiting the growth of cancerous tumor cells and associated diseases in a mammal and further provides a method for the treatment or prevention of cancerous tumors that express multiple drug resistance (MDR) or are resistant because of MDR, in a mammal in need thereof which method comprises administering to said mammal an effective amount of said compounds or pharmaceutically acceptable salts thereof. The present invention relates to a method of treating or inhibiting the growth of cancerous tumor cells and associated diseases in a mammal in need thereof by promotion of microtubule polymerization which comprises administering to said mammal an effective amount of said compounds and pharmaceutically acceptable salts thereof.

6-[(substituted)phenyl]triazolopyrimidines as anticancer agents

The invention provides 6-chloro-5-{2,6-difluoro-4-[3-(methylamino)propoxy]phenyl}-2-pyrazin-2-yl-N-[(1S)-2,2,2-trifluoro-1-methylethyl]pyrimidin-4-amine hemifumarate which is a tubulin inhibitor useful in the treatment of cancer and processes of making said hemifumarate.

Tubulin inhibitor and process for its preparation

The present invention relates to crystalline forms of 5-chloro-6-{2,6-difluoro-4-[3-(methylamino)propoxy]phenyl}-N-[(1S)-2,2,2-trifluoro-1-methylethyl][1,2,4]triazolo[1,5-a]pyrimidin-7-amine salts; processes for the production thereof; pharmaceutical compositions thereof; and methods for inhibiting tumor growth therewith.

Crystalline forms of 5-chloro-6-{2,6-difluoro-4-[3-(methylamino)propoxy]phenyl}-N-[(1S)-2,2,2-trifluoro-1-methylethyl][1,2,4]triazolo[1,5-a]pyrimidin-7-amine salts

The present invention provides a process for the preparation of 6-[(substituted)phenyl]-triazolopyrimidine dicarboxylic acid salt and as a hydrated salt having the structural formula (I) wherein:

Process for the preparation of tubulin inhibitors

A process for making a compound of formula (I) in which process the compound HC&#x2261;C&#x2014;(CH)&#x2014;NHis reacted with the compound R&#x2014;SOCl to produce an intermediate compound, which intermediate compound is then reacted with the compound of formula to produce the compound of formula (I), and compounds produced by the process of this invention. The terms R, R, R, Rand n have the definitions set forth in the specification.

Advanced route for the synthesis of cPLA2 inhibitors

The present invention describes a process for preparing N-substituted phthalimides of Formula I which are widely useful as intermediates in the preparation of organic compounds such as pharmaceuticals 

Processes for the preparation of N-substituted phthalimides

The invention provides 6-chloro-5-{2,6-difluoro-4-[3-(methylamino)propoxy]phenyl}-2-pyrazin-2-yl-N-[(1S)-2,2,2-trifluoro-1-methylethyl]pyrimidin-4-amine hemifumarate which is a tubulin inhibitor useful in the treatment of cancer and processes of making hemifumarate compounds and compositioning of the present invention.

The invention is a process for the preparation of compounds of the Formula I:where R, R, R, Rand Rare defined in the specification, which are intermediates useful for the preparation of tubulin inhibitors which are useful in the treatment of cancer.

Process for the synthesis of intermediates useful for the synthesis of tubulin inhibitors

A process for making a compound of formula (I)in which process the compound HC&#x2261;C&#x2014;(CH)&#x2014;NHis reacted with the compound R&#x2014;SOCl to produce an intermediate compound, which intermediate compound is then reacted with the compound of formulato produce the compound of formula (I), and compounds produced by the process of this invention. The terms R, R, R, Rand n have the definitions set forth in the specification.

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Bronx, NY, United States of America

Yanzhong Wu