The Upjohn Co.

Pharmacia & Upjohn Company

Herman W Smith

Wendell Wierenga

Harvey I Skulnick

Robert J Smith

Roy A Johnson

Donna Lee Romero

Michael R Barbachyn

Robert C Gadwood

Valerie Ann Vaillancourt

Paul A Aristoff

Richard Charles Thomas

John R Palmer

Dana Scott Toops

The present invention relates to compounds of formula (I) which are imidazo&lsqb;2,1-b&rsqb;benzothiazole-3-methanol and imidazo&lsqb;2,1-b&rsqb;thiazole-5-methanol derivatives useful for inhibiting a retrovirus in a mammalian cell infected with said retrovirus, wherein R,is &mdash;H or &mdash;CH,; wherein R,is &mdash;H or &mdash;CH,; or wherein R,and R,taken together are (a) formula (II), or (b) formula (III).

Methanol derivatives for treatment of retroviral infections especially HIV infections

Compounds useful in the preparation of pharmaceutical preparations for the treatment of microbial infection where such compounds are of structural Formula I ##STR1## or pharmaceutically acceptable salts thereof wherein: R.sup.1 is --CHO, --COCH.sub.3, --COCHCl.sub.2, --COCHF.sub.2, --CO.sub.2 CH.sub.3, --SO.sub.2 CH.sub.3, or --COCH.sub.2 OH; X.sup.1 and X.sup.2 are independently H, F, or Cl; and Q is a five membered ting heterocycle (azolyl ring) of the general form: ##STR2## wherein A, B, and C are independently oxygen (O), nitrogen (N), sulfur (S) or Carbon (C). In all cases, the piperazine nitrogen atom is attached at the carbon atom of the carbon-nitrogen double bond.

Azolyl piperazinyl phenyl oxazolidinone antimicrobials

The present invention includes diaromatic substituted heterocyclic compounds (III) ##STR1## which are useful in treating individuals infected with the HIV virus.

Diaromatic substituted compounds as anti-HIV-1 agents

Novel acids, esters, and salts of phenyl, naphthyl, quinoxalinyl, and biphenyl bisphosphonic acids and 1,2-oxaphosphepins are described. These compounds are useful as antiinflammatory and anti-arthritic agents. Also described are known compounds of the phenyl, naphthyl, quinoxalinyl, and biphenyl bisphosphonate classes which are also useful as antiinflammatory and anti-arthritic agents. Representative compounds include [1,2-phenyldiyl]bis(methylene)bisphosphonic acid tetramethyl ester, [2,3-quinoxalindiyl]bis(methylene)bisphosphonic acid tetramethyl ester, [[3-(propyl)-4-(methoxy)-1,8-naphthalenediyl]bis(methylene)]bisphosphonic acid tetramethyl ester, [2,6-naphthalenediylbis(methylene)bisphosphonic acid tetraethyl ester, and [2,2'-biphenylenebis(methyl)]bisphosphonic acid tetramethyl ester. Representative oxaphosphepins include the preferred 3,4-dihydro-3-methoxy-7-(phenylmethoxy)-1H-naphth[1,8de][1,2]oxaphosphepin -3-oxide.

Bisphosphonic acid derivatives useful as anti-arthritic agents

Novel acids, esters, and salts of phenyl, naphthyl, quinoxalinyl, and biphenyl bisphosphonic acids and 1,2-oxaphosphepins are described. These compounds are useful as antiinflammatory and anti-arthritic agents. Also described are known compounds of the phenyl, naphthyl, quinoxalinyl, and biphenyl bisphosphonate classes which are also useful as antiinflammatory and anti-arthritic agents. Representative compounds include [1,2-phenyldiyl]bis (methylene)bisphosphonic acid tetramethyl ester, [2,3-quinoxalindiyl]bis(methylene)bisphosphonic acid tetramethyl ester, [[3-(propyl)-4-(methoxy)-1,8-naphthalenediyl]bis(methylene)]bisphosphonic acid tetramethyl ester, [2,6-naphthalenediylbis(methylene) bisphosphonic acid tetraethyl ester, and [2,2'-biphenylenebis(methyl)]bisphosphonic acid tetramethyl ester. Representative oxaphosphepins include the preferred 3,4-dihydro-3-methoxy -7-(phenylmethoxy)-1H-naphth[1,8de][1,2]oxaphosphepin-3-oxide.

Phosphonic acid derivatives useful as anti-inflammatory agents

Cyclopentapyrazole and tetrahydroindazole compounds and their use as

This invention relates to selected hydrogenated 5,6-dihydro-6-aryluracils.

6-aryluracils and selected novel intermediates used in the preparation

This invention relates to the use of 6-aryluracils as antiinflammatory and antiarthritic agents and also to both novel intermediates and novel processes for the preparation of selected 6-aryluracils.

Use of 6-aryluracils as antiinflammatory and antiarthritic agents

Processes for the preparation of 6-aryluracils

The present invention also provides novel compositions of matter. In particular, the present invention provides novel 3-substituted compounds of formula I which are from among the selected 5,6,7,8-tetrahydroquinolines and 5,6-dihydropyrindines having use as inhibitors of the synthesis of leukotrienes and as inhibitors of the action of lipoxygenase in mammalian metabolism.

Use of 5,6,7,8-tetrahydroquinolines and 5,6-dihydropyrindines as

Process for the preparation of 1,3-oxazine-4-ones

Novel structural analogues of 5,6-dihydro PGI.sub.2 of the formula: ##STR1## and the corresponding 10,11-didehydro-11-deoxy derivatives are useful as antiallergy agents.

Analogs of 5,6-dihydro PGI.sub.2

6-Aryluracils

This invention relates to certain structural and pharmacological analogs of prostacyclin (PGI.sub.2) wherein the C-5 to C-6 double bond is isomerized to the C-4 to C-5 position. These novel trans-4,5-didehydro-5,6-dihydro prostacyclin-type compounds are useful as smooth muscle stimulators.

Trans-4,5,13,14-tetradehydro-PGI.sub.1 compounds

Novel structural analogues of 5,6-dihydro PGI.sub.1 of the formula: ##STR1## useful as antiallergy agents.

Growing community of inventors

Kalamazoo, MI, United States of America

Herman W Smith