Pharmacia & Upjohn Company

Mcneil Ab

Pfizer Corporation

Mark Peter Warchol

Walter Morozowich

Michael John Hawley

Malcolm Wilson Moon

Patrick J Lennon

Kristina Thyresson

Elisabeth Sthengel

Dominique Bonafoux

Mark Kontny

Craig D Wegner

Sue K Cammarata

Ivan Richards

Sergey Gregory Wolfson

Karen Patrice Kolbasa

Satish Kumar Singh

Sven-Börje Andersson

Folke Morén

Folke Moren

Sven-Boerje Andersson

Provided are liquid pharmaceutical formulations comprising nicotine in any form for administration essentially to the lungs being acidified and/or alkalized by buffering and/or pH regulation providing for a tof nicotine in arterial blood of a subject within a short period of time after administration. The administration is preferably accomplished by spraying an aerosol into the oral cavity for further distribution essentially into the lungs. Methods for manufacturing the formulation is also disclosed, as are uses of the formulation in therapy, such as therapy for treating addiction to tobacco.

Formulation and use thereof

A liquid pharmaceutical formulation comprising nicotine in any form for administration essentially to the lungs being acidified and/or alkalized by buffering and/or pH regulation providing for a tof nicotine in arterial blood of a subject within a short period of time after administration. The administration is preferably by spraying an aerosol into the oral cavity for further distribution essentially into the lungs. A method for manufacturing said formulation. Use of said formulation in therapy, such as therapy for treating addiction to tobacco.

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 concerns novel pharmaceutically active compounds, pharmaceutical compositions containing the same, the compounds for use as medicaments, and use of the compounds for the manufacture of specific medicaments. The present invention also concerns a method of treatment involving administration of the compounds. Specifically, the compounds are pharmaceutically acceptable salts of tolterodine or hydroxytolterodine, wherein the salt is of an acid selected from the group consisting of aliphatic mono- and dicarboxylic acids comprising from 7 to 24 carbon atoms, alkanedisulfonic acids comprising from 2 to 4 carbon atoms, naphthoic acid derivatives comprising from 11 to 27 carbon atoms, maleic acid and fumaric acid.

Tolterodine salts

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

Growing community of inventors

Kalamazoo, MI, United States of America

Mark Peter Warchol