Pharmacia & Upjohn Company

Pfizer Corporation

The Upjohn Co.

Theupjohn Company

William W McWhorter, Jr

Eric Jon Jacobsen

Kristine E Frank

Jian-Min Fu

Michael D Ennis

Donald J Rogier

Brad A Acker

Jed F Fisher

Jeanette Kay Morris

Bruce Allen Pearlman

Thomas J Fleck

Noriie Itoh

Hiroshi Kushida

Kazunori Ozawa

Mikio Taniguchi

Kazuo Tsuzuki

Mineo Kunihara

Syunji Nomura

Byung H Lee

Fred E Dutton

Keiko Koh

Valentina Badescu

Pil H Lee

Disclosed are compounds of Formula (I):wherein R-R, p and q have any of the values described in the specification, as well as pharmaceutical salts thereof, and pharmaceutical compositions containing such compounds or salts. The compounds and salts are 5-HT ligands and are useful for treating diseases, disorders, and/or conditions in a mammal wherein activity of a 5-HT receptor is implicated. The compounds and salts are particularly useful for treating diseases of the central nervous system.

Substituted azepino[4,5b]indole derivatives

Substituted azepino&lsqb;4,5b&rsqb;indoline derivatives

Therapeutic compounds

Therapeutic 5-HT ligand compounds

Substituted azepino&lsqb;4,5b&rsqb;indole derivatives

This invention relates to processes for the synthesis of various optically active amino pyrrolidinyl stereoisomers, or enantiomers, that may be attached to quinolonecarboxylic acids or naphthyridones. Processes and essential intermediates are disclosed and claimed for the synthesis of compounds represented by the structure shown in figure BG.sub.4-1, below. ##STR1## where R.sup.50, R.sup.6 and R.sup.9 are defined independently and are H, --(C.sub.1 -C.sub.8)alkyl, --(C.sub.3 -C.sub.8)cycloalkyl, --(C.sub.1 -C.sub.8)alkyl-(C.sub.3 -C.sub.8)cycloalkyl, --(C.sub.6 -C.sub.12 aryl), --(C.sub.1 -C.sub.8)alkyl-(C.sub.6 -C.sub.12 aryl), or the aryl or alkyl is substituted with one to three of the following groups, (C.sub.6 -C.sub.12 aryl), (C.sub.1 -C.sub.3)alkyl, (C.sub.1 -C.sub.3) alkoxy, halogen, trifluoromethyl;

Optically active 3-(1-(carbamoyl))alkyl-2-oxo-pyrrolidines and optically

This invention relates to processes for the synthesis of various optically active amino pyrrolidinyl stereoisomers, or enantiomers, that may be attached to quinolonecarboxylic acids or naphthyridones. Processes and essential intermediates are disclosed and claimed for the synthesis of compounds represented by the structure shown in figure BG.sub.4-1, below. ##STR1## where R.sup.50, R.sup.6 and R.sup.9 are defined independently and are H, --(C.sub.1 -C.sub.8)alkyl, --(C.sub.3 -C.sub.8)cycloalkyl, --(C.sub.1 -C.sub.8)alkyl-(C.sub.3 -C.sub.8)cycloalkyl, --(C.sub.6 -C.sub.12 aryl), --(C.sub.1 -C.sub.8) alkyl-(C.sub.6 -C.sub.12 aryl), or the aryl or alkyl is substituted with one to three of the following groups, (C.sub.6 -C.sub.12 aryl), (C.sub.1 -C.sub.3)alkyl, (C.sub.1 -C.sub.3) alkoxy, halogen, trifluoromethyl;

Optically active 3-(1-(alkylamino))alkyl pyrrolidines

This invention comprises novel compounds that inhibit the growth of helminths. The compounds have the structure of Formula I, below. ##STR1## Where the R groups are defined according to the specification and claims.

Cycloanthelmintic inhibitors

The present invention provides novel tropolone derivatives of the formula I ##STR1## wherein R.sub.10 is a substituted or unsubstituted piperazinyl or benzothiazolidinyl group, and pharamaceutical compositions thereof. These compounds are useful for the prevention and treatment of ischemic diseases, including cerebrovascular diseases and cardiovascular diseases.

Tropolone derivatives and pharmaceutical composition thereof for

Imidazobenzoquinones and composition for preventing or treating

Growing community of inventors

Parchment, MI, United States of America

William W McWhorter, Jr