The Upjohn Co.

Pharmacia & Upjohn Company

Other

Sugen Incorporated

Pfizer Corporation

Agouron Pharmaceuticals, Inc.

Malcolm Wilson Moon

Walter Morozowich

Ping Gao

Gabriel Kornis

Richard F Heier

Marcel Koenig

Peng Cho Tang

Joseph Walter Strohbach

Patrick J Lennon

Michael John Hawley

Jeanette Kay Morris

Mark Peter Warchol

Dominique Bonafoux

Sergey Gregory Wolfson

Craig D Wegner

Mark Kontny

Ivan Richards

Sue K Cammarata

Karen Patrice Kolbasa

Gordon L Bundy

Steven Paul Tanis

Valerie Ann Vaillancourt

Mark E Schnute

Atli Thorarensen

Suvit Thaisrivongs

David John Anderson

Steven Ronald Turner

Girts Kaugars

Victor L Rizzo

Fred L Ciske

Michael J Genin

Thomas M Judge

David R Graber

John C Sharp

Diane M Rohrstaff

Allison J Wolf

The compound 2-[(1R)-3-(diisopropylamino)-1-phenylpropyl]-4-(trifluoromethyl) phenol may be used to prepare the compound (3R)-3-[2-hydroxy-5-(trifluoromethyl)phenyl]-N,N-diisopropyl-N-methyl-3-phenylpropan-1-aminium bromide by reaction with methyl bromide.

Phenol derivative

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 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

Novel quaternary ammonium compounds of the formulaand any stereoisomers thereof, wherein R, Rand Rindependently represent C-Calkyl, optionally substituted with phenyl or hydroxyl, or both, and wherein any two of R, Rand Rmay form a ring together with the quaternary ammonium nitrogen; Rrepresents &#x2014;H, &#x2014;CH, or &#x2014;CO&#x2014;R, wherein Rrepresents &#x2014;(C-Calkyl), &#x2014;(C-Calkoxy), or &#x2014;NRR, wherein Rand Rindependently represent &#x2014;H or &#x2014;(C-Calkyl); R, Rand Rindependently represent &#x2014;H, &#x2014;OCH, &#x2014;OH, &#x2014;CONH, &#x2014;SONH, &#x2014;F, &#x2014;Cl, &#x2014;Br, &#x2014;I, &#x2014;CF, or &#x2014;(C-Calkyl), optionally substituted with one or two &#x2014;OH, &#x2014;(C-Calkoxy), &#x2014;COOH, or &#x2014;CO&#x2014;O&#x2014;(C-Calkyl); and Xrepresents an anion of a pharmaceutically acceptable acid, the compounds for use as medicaments, use of the compounds for the manufacture of specific medicaments, and pharmaceutical compositions comprising the compounds. The present invention also concerns a method of treatment involving administration of the compounds.

Quaternary ammonium compounds

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

Pyridoquinoxaline antivirals

Heterocycle carboxamides as antiviral agents

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

Tricyclic nitrogen containing compounds, having central nervous system activity of the following structural formula: ##STR1## and pharmaceutically acceptable salts thereof wherein R.sub.1, R.sub.2, and R.sub.3 are independently hydrogen, C.sub.1-6 alkyl, alkenyl, or alkynyl, C.sub.3-10 cycloalkyl, or R.sub.1 and R.sub.2 are joined to form a C.sub.3-7 cyclic amine which can contain additional heteroatoms; X is hydrogen, C.sub.1-6 alkyl, halogen, hydroxy, alkoxy, cyano, carboxamide, carboxyl, or carboalkoxyl; A is SO.sub.2, N, CH, CH.sub.2, CHCH.sub.3, C=O, C=S, C-SCH.sub.3, C=NH, C-NH.sub.2, C-NHCH.sub.3, CNHCOOCH.sub.3, or C-NHCN. B is CH.sub.2, CH, C=O, N, NH or N-CH.sub.3 ; n is 0 or 1; and D is CH, CH.sub.2, C=O, 0, N, NH or N-CH.sub.3. These new compounds are suitable for treating schizophrenia, Parkinson's disease, anxiety, depression or as compounds for lowering blood pressure in animal or human hosts.

Heterocyclic amines having central nervous system activity

Heterocyclic acetylenic amine compounds having the following structural formula ##STR1## where X is ##STR2## having cholinergic agonist or antagonist activity useful in the treatment of mental disorders, extrapyramidal motor disorders, disorders of the parasympathetic nervous system and glaucoma or as analgesics for the treatment of pain. Typical central nervous system disorders for which the subject compounds can be used include cognitive disorders of all ages, including senile dementia, Alzheimer's disease and other related disorders. The compounds are particularly developed to improve mental performance when a mental deficiency is diagnosed.

Heterocyclic acetylenic amines having central nervous system activity

Heterocyclic acetylenic amine compounds having the following structural formula ##STR1## having cholinergic agonist or antagonist activity useful in the treatment of mental disorders, extrapyramidal motor disorders, disorders of theparasympathetic nervous system and glaucoma or as analgesics for the treatment of pain. Typical central nervous system disorders for which the subject compounds can be used include cognitive disorders of all ages, including senile dementia, Alzheimer's disease and other related disorders. The compounds are particularly developed to improve mental performance when a mental deficiency is diagnosed.

Growing community of inventors

Kalamazoo, MI, United States of America

Malcolm Wilson Moon