Boc, Inc.

The Boc Group, Inc.

Anaquest, Inc.

H Kenneth Spencer

Linas V Kudzma

Jerome R Bagley

Sherry A Severnak

Nhora L Lalinde

Bor-Sheng Lin

John Moliterni

Bao-Shan Huang

Joseph William Scheblein

The present invention is directed to a method for preparing a 4-alkoxyalkyl-4-phenylaminopiperidine compound which comprises the steps of (a) reacting an N-substituted-4-piperidone compound with an aniline compound to form a Schiff base compound, (b) reacting the Schiff base compound with an anionic reagent having an anion stabilizing group to form an amine compound, and (c) reducing the amine compound in step (b) with a reducing agent to displace the anion stabilizing group. The anionic reagent in step (b) above has the general formula:

Method for preparing 4-alkoxyalkyl-4-phenylaminopiperdines and

This invention pertains to novel N-aryl-N-[N-substituted 3-alkoxy-4-piperidinyl]amides useful as analgesics, and methods of administering analgesia, which comprises the systemic administration to mammals of such compounds, and pharmaceutical compositions containing such compounds, wherein the novel compounds have the general formula: ##STR1## including optically active isomeric forms, cis/trans isomeric forms and the pharmaceutically acceptable acid addition salts thereof, wherein:

N-aryl-n-(1-substituted-3-alkoxy-4-piperidinyl)amides and pharmaceutical

This invention pertains to novel substituted N-aryl-N-[4-(1-heterocyclicalkyl)piperidinyl]amides useful as analgesics, and methods of administering analgesia, which comprises the systemic administration to mammals of such compounds, and pharmaceutical compositions containing such compounds, wherein the novel compounds have the general formula: ##STR1## including optically active isomeric forms, and the pharmaceutically acceptable acid addition salts thereof, wherein R, R.sub.1, R.sub.2, R.sub.3 and R.sub.4 are defined in the disclosure.

N-aryl-N-[4-(1-heterocyclicalkyl)piperidinyl]amides and pharmaceutical

Compounds are disclosed of the formula ##STR1## where R.sup.2 is unsubstituted or substituted phenyl, R.sup.3 is lower alkyl, lower cycloalkyl or lower alkoxy lower alkyl, and L is selected from a wide variety of groups. This new class of compounds exhibit improved analgesic and anesthetic properties.

4-phenyl-4-N-(phenyl) amido piperidine derivatives and pharmaceutical

This invention pertains to novel N-aryl-N-[N-substituted 3-alkoxy-4-piperidinyl]amides useful as analgesics, and methods of administering analgesia, which comprises the systemic administration to mammals of such compounds, and pharmaceutical compositions containing such compounds, wherein the novel compounds have the general formula: ##STR1## including optically active isomeric forms, cis/trans isomeric forms and the pharmaceutically acceptable acid addition salts therof, wherein:

N-aryl-N-(1-substituted-3-alkoxy-4-piperidinyl)amides and pharmaceutical

4-phenyl-4-[N-(phenyl)amido]piperidine compounds and pharmaceutical

This invention pertains to novel substituted N-heterocyclic-N-(4-piperidinyl)amides useful as analgesics and antagonists of opioids, wherein the compounds have the general formula: ##STR1## including optically active isomeric forms, and the pharmaceutically acceptable acid addition salts thereof, wherein:

N-heterocyclic-N-(4-piperidinyl)amides and pharmaceutical compositions

This invention pertains to novel substituted N-aryl-N-[1-substituted 3,5-dimethyl-4-piperidinyl]amides useful as analgesics, and methods of administering analgesia, which comprises the systemic administration to mammals of such compounds, and pharmaceutical compositions containing such compounds, wherein the novel compounds have the general formula: ##STR1## including optically active isomeric forms, cis/trans isomeric forms and the pharmaceutically acceptable acid addition salts thereof, wherein:

Analgesic N-aryl-N-[1-substituted-3,5-dimethyl-4-piperidinyl]amides

4-Phenyl-4-(N-(phenyl)amido) piperidine derivatives and pharmaceutical

This invention pertains to novel substituted N-heterocyclic-N-(4-piperidinyl)amides useful as analgesics and antagonists of opiolds, wherein the compounds have the general formula: ##STR1## including optically active isomeric forms, and the pharmaceutically acceptable acid addition salts thereof, wherein:

This invention pertains to novel substituted N-heterocyclic-N-(4-piperidinyl)amides useful as analgesics and antagonists of opiods, wherein the compounds have the general formula: ##STR1## including optically active isomeric forms, and the pharmaceutically acceptable acid addition salts thereof, wherein:

N-heterocyclic-N-(4-piperidinyl) amides and pharmaceutical compositions

N-heterocyclic-4-piperidiyl-amides as analgesics and antagonists of opioids with respect to such undesirable side effects as respiratory depression. Exemplary compounds have the formula ##STR1## in which formula R is a heterocyclic group, and R.sup.1 is a furanyl, thienyl, or lower alkoxy lower alkyl group, and R.sup.2 is a lower alkyl phenyl group.

N-heterocyclic-N-(4-piperidyl)amides and pharmaceutical compositions and

Compounds are disclosed of the formula ##STR1## wherein R.sup.1 is an unsubstituted or substituted herterocyclic ring system; R.sup.2 is an unsubstituted or substituted phenyl; R.sup.3 is a lower alkyl or lower alkoxy, and L is selected from a wide variety of groups.

4-heteropentacyclic-4-(N-(phenyl)amido) piperidine derivatives and

The present invention is directed to an improved stereoselective tandem substitution and reduction of an imine precursor to the cis form of 3-substituted-4-(phenylanilo)piperidine compounds or their substituted derivatives.

Stereoselective preparation of 3-substituted-4-piperidine compounds and

Compounds are disclosed of the formula ##STR1## where R.sup.1 is a six numbered heterocyclic ring; R.sup.2 is a substituted or unsubstituted phenyl; R.sup.3 is lower alkyl, and L is selected from a variety of groups.

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Chatham, NJ, United States of America

H Kenneth Spencer