The Upjohn Co.

Other

Massachusetts Institute of Technology

Roy A Johnson

John C Sih

John E Pike

Frank H Lincoln, Jr

Gordon L Bundy

Gilbert A Youngdale

Douglas R Morton

Donald P Wallach, Deceased

Chiu-Hong Lin

Robert C Kelly

Herman W Smith

Harvey I Skulnick

Eldon George Nidy

Milton E Herr

Jackson B Hester, Jr

Karl B Sharpless

By Vera Wallach, Legal Representative

Wallach, Legal Representative, By Vera M

Vera M Wallach, Legal Representative

This invention provides 7-deoxy-taxol analogs of Formula I: The compounds of Formula I (including II and III) are useful for the same cancers for which taxol has been shown active, including human ovarian cancer, breast cancer, and malignant melanoma as well as lung cancer, gastric cancer, colon cancer, head and neck cancer, and leukemia.

Method of preparing a taxol derivative

The invention relates to a method for encapsulating lead paint on a surface comprises the steps of applying a glass mesh to the surface containing the lead paint and applying an encapsulating mixture in a continuous layer over the glass mesh and to the encapsulated lead paint surface. The invention completely seals and encapsulates the lead paint and has significant structural integrity to prevent exposure to lead paint.

Method of lead paint encapsulation

Provided are cyclic hydrocarbons of Formula I ##STR1## with an aminoalkyl sidechain that are useful for treating phospholipase A2 mediated conditions, diabetes, and obesity.

Cyclic hydrocarbons with an aminoalkyl sidechain

This invention provides a new use of acids, esters, and salts of arylmethylphosphonates of Formula I, ##STR1## or a phosphonic acid of Formula II ##STR2## and derivatives as anti-inflammatory and anti-arthritic agents. Representative compounds include 4-dodecyloxybenzylphosphonic acid dimethyl ester, (2-naphthalenylmethyl)phosphonic acid dimethyl ester, and ([1,1'-biphenyl]-2-ylmethyl)phosphonic acid dimethyl ester.

Arylmethylphosphonates and phosphonic acids useful as anti-inflammatory

This invention provides 7-deoxy-.DELTA..sup.6,7 -taxol and 7-deoxy-.DELTA..sup.6,7 -taxol analogs of Formula I: ##STR1## The compounds of Formula I are useful for the same cancers for which taxol has been shown active, including human ovarian cancer, breast cancer, and malignant melanoma as well as lung cancer, gastric cancer, colon cancer, head and neck cancer, and leukemia.

.DELTA..sup.6,7 -taxols antineoplatic use and pharmaceutical

This invention provides a new use of acids, esters, and salts of arylmethylphosphonates of Formula I, ##STR1## or phosphonic acid derivatives of Formula II ##STR2## as anti-inflammatory and anti-arthritic agents. Representative compounds include 4-dodecyloxybenzylphosphonic acid dimethyl ester, (2-naphthalenylmethyl)phosphonic acid dimethyl ester, and ([1,1 '-biphenyl]-2-ylmethyl)phosphonic acid dimethyl ester. The invention also provides novel acids, esters, and salts of arylmethylphosphonic acid, phosphonic acid and derivatives.

Steroid compounds

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

Provided are novel dialkyl (dialkoxyphosphinyl)methyl phosphates of formula ##STR1## which am useful as anti-inflammatory and anti-arthritic agents. The compounds are synthesized from the reaction of tetraethyl oxiranylidenebisphosphonate and unsubstituted or alkyl-amines. Representative compounds include 2-(benzylamino)-1-(diethoxyphosphinyl)ethyl phosphonic acid diethyl ester, 1-(diethoxyphosphinyl)-2-[2'-(1', 2', 3', 4'-tetrahydro)napthylamino]ethyl phosphonic acid diethyl ester, 2-(3-fluorobenzylamino)-1-(diethoxyphosphinyl)ethyl phosphonic acid diethyl ester, and 5,5 -dimethyl-2-[2-(3-fluorobenzyl)amino-1-[(5,5-dimethyl-1,3,2-dioxaphosphori nan-2-yl)oxy]ethyl]-1,3,2-dioxaphosphorinane P,2-dioxide.

Dialkyl (dialkoxyphosphinyl)methyl phosphates as anti-inflammatory 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

Provided are cyclic hydrocarbons of Formula I ##STR1## with an aminoalkyl sidechain.

Growing community of inventors

Kalamazoo, MI, United States of America

Roy A Johnson