Pharmacia & Upjohn Company

Sugen Incorporated

Other

Pharmacia Corporation

Agouron Pharmaceuticals, Inc.

Ping Gao

Walter Morozowich

Malcolm Wilson Moon

Marcel Koenig

Peng Cho Tang

James Carnegie Forbes

Aziz Karim

Narmada R Shenoy

Hong Zhuang

Andrew M Brugger

Fred Hassan

Anand Sistla

Pharmaceutical compositions suitable for oral administration comprising paclitaxel, a solvent, a surfactant, a substituted cellulosic polymer, and optionally but preferably a P-glycoprotein inhibitor. The composition may further comprise a diglyceride or mixture of diglyceride and monoglyceride. The composition generates a supersaturated paclitaxel microemulsion upon contact with water resulting in improved oral bioavailability of paclitaxel.

Chemotherapeutic microemulsion compositions of paclitaxel with improved oral bioavailability

The present invention is directed to prodrugs of certain 3-(pyrrol-2-yl-methylidene)-2-indolinone derivatives that modulate the activity of protein kinases ('PKs'). Pharmaceutical compositions comprising these compounds, methods of treating diseases related to abnormal PK activity utilizing pharmaceutical compositions comprising these compounds and methods of preparing them are also disclosed.

Prodrugs of 3-(pyrrol-2-ylmethylidene)-2-indolinone derivatives

The present invention is directed to formulations comprising 3-(pyrrol-2-ylmethylidene)-2-indolinone derivatives that modulate the activity of protein kinases ('PKs'). Methods of treating diseases related to abnormal PK activity utilizing the formulations comprising these compounds and methods of making these formulations are also disclosed.

Pharmaceutical formulations comprising indolinone derivatives

The present invention is directed to Mannich base prodrugs of certain 3-(pyrrol-2-ylmethylidene)-2-indolinone derivatives that modulate the activity of protein kinases ('PKs'). Pharmaceutical compositions comprising these compounds, methods of treating diseases related to abnormal PK activity utilizing pharmaceutical compositions comprising these compounds and methods of preparing them are also disclosed.

Mannich base prodrugs of 3-(pyrrol-2-yl-methylidene)-2-indolinone derivatives

The present invention is directed to 1-pyrrolidin-1-ylmethyl-3-(pyrrol-2-ylmethylidene)-2-indolinone derivatives that modulate the activity of protein kinases ('PKs'). Pharmaceutical compositions comprising these compounds, methods of treating diseases related to abnormal PK activity utilizing pharmaceutical compositions comprising these compounds and methods of preparing them are also disclosed.

1-(Pyrrolidin-1-ylmethyl)-3-(pyrrol-2-ylmethylidene)-2-indolinone derivatives

A process is provided for preparing a celecoxib-crystallization inhibitor composite wherein at least a detectable amount of celecoxib is in amorphous form. Also provided are compositions prepared according to such a process. Also provided is a method of treating a medical condition or disorder in a subject where treatment with a cyclooxygenase-2 inhibitor is indicated, comprising administering, for example orally, a composition of the invention in a therapeutically effective amount.

Stable amorphous celecoxib composite and process therefor

The present invention is directed to prodrugs of certain 3-(pyrrol-2-yl-methylidene)-2-indolinone derivatives that modulate the activity of protein kinases (&ldquo;PKs&rdquo;). Pharmaceutical compositions comprising these compounds, methods of treating diseases related to abnormal PK activity utilizing pharmaceutical compositions comprising these compounds and methods of preparing them are also disclosed.

The present invention is directed to Mannich base prodrugs of certain 3-(pyrrol-2-ylmethylidene)-2-indolinone derivatives that modulate the activity of protein kinases (&ldquo;PKs&rdquo;). Pharmaceutical compositions comprising these compounds, methods of treating diseases related to abnormal PK activity utilizing pharmaceutical compositions comprising these compounds and methods of preparing them are also disclosed.

Mannich base prodrugs of 3-(pyrrol-2-ylmethylidene)-2-indolinone derivatives

There is provided a method of rapidly relieving pain in a mammalian, preferably human, subject. The method comprises orally administering to the subject an effective pain-relieving amount of a composition comprising celecoxib formulated in such a way as to provide, when tested in fasting humans in accordance with standard pharmacokinetic practice, a blood plasma concentration profile of celecoxib in which a concentration of about 250 ng/ml is attained not later than about 30 minutes after oral administration.

Use of a celecoxib composition for fast pain relief

The present invention provides a novel pharmaceutical composition based on the use of a particular oil phase which comprises a lipophilic, pharmaceutically active agent, a mixture of diglyceride and monoglyceride in a ratio of from about 9:1 to about 6:4 by weight (diglyceride:monoglyceride) wherein the diglyceride and monoglyceride are mono- or di- unsaturated fatty acid esters of glycerol having sixteen to twenty-two carbon chain length, one or more pharmaceutically acceptable solvents, and one or more pharmaceutically acceptable surfactants. The composition is in a form of self-emulsifying formulation which provides high concentration and high oral bioavailability for lipophilic compounds.

Self-emulsifying formulation for lipophilic compounds

The present invention is directed to 1-pyrrolidin-1-ylmethyl-3-(pyrrol-2-ylmethylidene)-2-indolinone derivatives that modulate the activity of protein kinases (&ldquo;PKs&rdquo;). Pharmaceutical compositions comprising these compounds, methods of treating diseases related to abnormal PK activity utilizing pharmaceutical compositions comprising these compounds and methods of preparing them are also disclosed.

1-(pyrrolidin-1-ylmethyl)-3-(pyrrol-2-ylmethylidene)-2-indolinone derivatives

The present invention provides a novel pharmaceutical composition based on the use of a particular amount of basic amine which comprises a pyranone compound as a pharmaceutically active agent, a basic amine in an amount of from about 0.1% to about 10% by weight of the total composition, one or more pharmaceutically acceptable solvents, and one or more pharmaceutically acceptable surfactants. In addition, the composition may further comprises one or more pharmaceutically acceptable oils. The composition is in a form of self-emulsifying formulation which provides high concentration and high oral bioavailability for lipophilic pyranone compounds.

Pharmaceutical composition for acidic lipophilic compounds in a form of a self-emulsifying formulation

The present invention provides a novel pharmaceutical composition based on the use of a particular oil phase which comprises a pyranone compound as a pharmaceutically active agent, a mixture of diglyceride and monoglyceride in a ratio of from about 9:1 to about 6:4 (diglyceride:monoglyceride) wherein the diglyceride and monoglyceride are mono- or di- unsaturated fatty acid esters of glycerol having sixteen to twenty-two carbon chain length, one or more pharmaceutically acceptable solvents, and one or more pharmaceutically acceptable surfactants. The composition is in a form of a self-emulsifying formulation which provides high concentration and high oral bioavailability for lipophilic pyranone compounds.

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Portage, MI, United States of America

Ping Gao