Patents by Inventor Joseph M. Muchowski

Joseph M. Muchowski has filed for patents to protect the following inventions. This listing includes patent applications that are pending as well as patents that have already been granted by the United States Patent and Trademark Office (USPTO).

  • Patent number: 4826869
    Abstract: N-(lower alkyl)-2-(3'-ureidobenzyl)pyrrolidines and N-(lower alkyl)-2-(3'-ureidobenzyl)-5-(lower alkyl)pyrrolidines are useful for lowering intraocular pressure in mammals, for example, in the treatment of glaucoma.
    Type: Grant
    Filed: February 19, 1988
    Date of Patent: May 2, 1989
    Assignee: Syntex (U.S.A.) Inc.
    Inventors: Joseph M. Muchowski, Robin D. Clark, L. David Waterbury
  • Patent number: 4803269
    Abstract: 4-Monosubstituted and 4,6-disubstituted phenoxazines, methods of preparing them and pharmaceutical compositions containing them. These compounds are useful as anti-inflammatories.
    Type: Grant
    Filed: August 14, 1987
    Date of Patent: February 7, 1989
    Assignee: Syntex (U.S.A.) Inc.
    Inventors: Joseph M. Muchowski, Robert J. Greenhouse, Angel Guzman
  • Patent number: 4755531
    Abstract: Thiol esters of 4,5-allenyl prostaglandins, methods of making them, and pharmaceutical compositions containing them. These compounds are useful as gastric acid secretion inhibitors.
    Type: Grant
    Filed: August 11, 1986
    Date of Patent: July 5, 1988
    Assignee: Syntex (U.S.A.) Inc.
    Inventors: Joseph M. Muchowski, Angel Guzman
  • Patent number: 4725622
    Abstract: A method of treating rheumatoid arthritis which method comprises administering to a mammal in need of such treatment a therapeutically effective amount of a compound of the formula: ##STR1## and the pharmaceutically acceptable salts thereof, wherein:A is oxygen or sulfur;R.sup.1 is selected from the group consisting of H, ##STR2## in which Y is oxygen or sulfur:R.sup.2 is alkyl, haloalkyl or --NR.sup.4 R.sup.5, where R.sup.4 and R.sup.5 are independently H, alkyl, haloalkyl, cycloalkyl, phenyl optionally monosubstituted with halogen, hydroxy, carboxy, chlorocarbonyl, sulfonylamino, nitro, cyano, phenyl, alkyl, acyl, alkoxycarbonyl, acylamino, dialkylamino or dialkylaminoethoxycarbonyl, phenyl optionally disubstituted with hydroxy, carboxy, nitro or alkyl, or benzyl optionally substituted with dialkylamino;n is an integer from 0-6;R.sup.3 is H alkyl or a pharmaceutically acceptable cation;Q and R are independently H or --CO.sub.2 R.sup.
    Type: Grant
    Filed: January 23, 1986
    Date of Patent: February 16, 1988
    Assignee: Syntex (U.S.A.) Inc.
    Inventors: Peter H. Nelson, Anthony C. Allison, Elsie M. Eugui, Joseph M. Muchowski
  • Patent number: 4707473
    Abstract: 4-Monosubstitued and 4,6-disubstituted phenoxazines, methods of preparing them and pharmaceutical compositions containing them. These compounds are useful as anti-inflammatories.
    Type: Grant
    Filed: May 30, 1986
    Date of Patent: November 17, 1987
    Assignee: Syntex (U.S.A.) Inc.
    Inventors: Joseph M. Muchowski, Robert J. Greenhouse, Angel Guzman
  • Patent number: 4681889
    Abstract: Compounds of the formula ##STR1## wherein R.sub.1 and R.sub.2 are each independently --H or lower alkoxy;R.sub.3 and R.sub.4 are each independently lower alkyl; andR.sub.5 and R.sub.6 are each --OCH.sub.3, or together form --OCH.sub.2 O-- or --OCH.sub.2 CH.sub.2 O--and pharmaceutically acceptable acid addition salts thereof are calcium channel blockers useful for treating cardiovascular disorders including angina, hypertension and congestive heart failure.
    Type: Grant
    Filed: June 27, 1986
    Date of Patent: July 21, 1987
    Assignee: Syntex (U.S.A.) Inc.
    Inventors: Robin Clark, Joseph M. Muchowski, Fang-Ting Chiu, John O. Gardner, Jacob Berger
  • Patent number: 4670465
    Abstract: Long chain unsaturated hydrocarbon derivatives, having from 13 to 21 carbon atoms, which are substituted at the 1-position by a phenoxy, phenylthio or a phenyl that bear a carboxylic acid group at the ortho, meta or para positions, and up to 4 carbon-carbon triple bonds, methods of preparing them, and pharmaceutical preparations containing them. These compounds are useful as lipoxygenase inhibitors, and therefore as antiinflammatory agents.
    Type: Grant
    Filed: May 21, 1986
    Date of Patent: June 2, 1987
    Assignee: Syntex (U.S.A.) Inc.
    Inventors: Angel Guzman, Joseph M. Muchowski
  • Patent number: 4667038
    Abstract: Compounds of the formula ##STR1## wherein R.sub.1 and R.sub.2 and each independently --H or lower alkoxy; R.sub.3 and R.sub.4 are each independently lower alkyl; and R.sub.5 and R.sub.6 are each --OCH.sub.3, or together form --OCH.sub.2 O-- or --OCH.sub.2 CH.sub.2 O--, and pharmaceutically acceptable acid addition salts thereof are prepared by cyclizing, deoxygenating, coupling, or hydrogenating the intermediates disclosed herein.
    Type: Grant
    Filed: September 22, 1986
    Date of Patent: May 19, 1987
    Assignee: Syntex (U.S.A.) Inc.
    Inventors: Robin Clark, Joseph M. Muchowski, Fang-Ting Chiu, John O. Gardner, Jacob Berger
  • Patent number: 4654360
    Abstract: Disclosed are compounds of the formula ##STR1## wherein the several groups are defined herein. These compounds are useful for treating inflammation.
    Type: Grant
    Filed: June 1, 1984
    Date of Patent: March 31, 1987
    Assignee: Syntex (U.S.A.) Inc.
    Inventors: Robert J. Greenhouse, Joseph M. Muchowski
  • Patent number: 4613606
    Abstract: Compounds of the formula ##STR1## wherein R.sub.1 and R.sub.2 are each independently --H or lower alkoxy;R.sub.3 and R.sub.4 are each independently lower alkyl; andR.sub.5 and R.sub.6 are each --OCH.sub.3, or together form --OCH.sub.2 O-- or --OCH.sub.2 CH.sub.2 O--and pharmaceutically acceptable acid addition salts thereof are calcium channel blockers useful for treating cardiovascular disorders including angina, hypertension and congestive heart failure.
    Type: Grant
    Filed: December 2, 1985
    Date of Patent: September 23, 1986
    Assignee: Syntex (U.S.A.) Inc.
    Inventors: Robin Clark, Joseph M. Muchowski, Fang-Ting Chiu, John O. Gardner, Jacob Berger
  • Patent number: 4612325
    Abstract: Novel 5-aroyl-6-methylthio-, 6-methylsulfinyl-, or 6-methylsulfonyl-1,2-dihydro-3H-pyrrolo[1,2-a]pyrrole-1-carboxylic acids represented by the formulas ##STR1## and the pharmaceutically acceptable, non-toxic esters and salts thereof, whereinR.sub.1 is lower alkylthio, lower alkylsulfinyl, or lower alkylsulfonyl;R.sub.2 is hydrogen, hydroxy, lower alkyl, vinyl, cyclohexyl, cyclopropyl, lower alkoxy, fluoro, chloro, bromo, trifluoromethyl, trifluoromethoxy, nitro, amino, lower alkylcarbonylamino, lower alkylthio, lower alkylsulfonyl, or lower alkylsulfinyl;X is oxygen, sulfur, N--R.sub.3 where R.sub.3 is hydrogen or lower alkyl.This invention describes intermediates of the process and the process for the production of these compounds and their pharmaceutically acceptable non-toxic salts and pharmaceutical composition thereof. The claimed compounds are useful as anti-inflammatories and analgesics in mammals.
    Type: Grant
    Filed: June 8, 1982
    Date of Patent: September 16, 1986
    Assignee: Syntex (U.S.A) Inc.
    Inventors: Joseph M. Muchowski, Robert Greenhouse
  • Patent number: 4560699
    Abstract: Novel 5-(4-vinyl- or 4-ethynylbenzoyl)-1,2-dihydro-3H-pyrrolo[1,2-a]pyrrole-1-carboxylic acids represented by the formula ##STR1## and the pharmaceutically acceptable, non-toxic alkyl esters and salts thereof, wherein R is vinyl or ethynyl, and Y is hydrogen, a lower alkyl group having from 1 to 6 carbon atoms, chloro or bromo.
    Type: Grant
    Filed: January 17, 1983
    Date of Patent: December 24, 1985
    Assignee: Syntex (U.S.A.) Inc.
    Inventors: Joseph M. Muchowski, Stefan H. Unger
  • Patent number: 4548949
    Abstract: A compound of the formula ##STR1## and the pharmaceutically acceptable acid addition salts thereof are potent antihypertensive agents and are therefore useful as cardiovascular system regulators. These compounds are also useful as bronchodilators.
    Type: Grant
    Filed: August 29, 1983
    Date of Patent: October 22, 1985
    Assignee: Syntex (U.S.A.) Inc.
    Inventors: Joseph M. Muchowski, Robert Greenhouse, Jack Ackrell, Tsung-Tee Li, Jurg R. Pfister
  • Patent number: 4548951
    Abstract: Compounds of the formula ##STR1## and the pharmaceutically acceptable, nontoxic, acid addition salts thereof, whereinR.sub.1 and R.sub.2 are each independently --H, lower alkyl, or cycloalkyl, with the proviso that R.sub.1 and R.sub.2 cannot both be --H or cycloalkyl at the same time;R.sub.1 and R.sub.2 taken together are cycloalkyl of 4-7 carbons;n is 0 or 1;X is (CH.sub.2).sub.2, CH.dbd.CH, or C.tbd.C;Y is independently selected from the group of --H, --Fl, --Br, --Cl, lower alkyl, and --OR.sub.3 ; wherein R.sub.3 is --H or lower alkyl; anda is 1 or 2, ortwo Y's taken together are --OCH.sub.2 O--;are useful as regulators of the cardiovascular system, particularly as hypotensive agents.
    Type: Grant
    Filed: April 21, 1983
    Date of Patent: October 22, 1985
    Assignee: Syntex (U.S.A.) Inc.
    Inventors: Joseph M. Muchowski, Jack Ackrell
  • Patent number: 4543361
    Abstract: A compound of the formula ##STR1## and the pharmaceutically acceptable acid addition salts thereof are potent antihypertensive agents and are therefore useful as cardiovascular system regulators.
    Type: Grant
    Filed: August 29, 1983
    Date of Patent: September 24, 1985
    Inventors: Joseph M. Muchowski, Robert Greenhouse, Jack Ackrell, Tsung-Tee Li, Jurg R. Pfister
  • Patent number: 4532138
    Abstract: Compounds of the formula: ##STR1## and the pharmaceutically acceptable, non-toxic salts and esters (alkyl, 1-6C) thereof, wherein:X is O or S;R.sup.1 is selected from the group consisting of:(a) alkyl or cycloalkyl of 3-8 carbons,(b) ##STR2## in which Z is O, S or --CH.sub.2, and Y is lower alkyl (1-4C), lower alkoxy (1-4C), halo, or --CF.sub.3, and(c) ##STR3## in which Z and X are as herein defined; and R.sup.2 is hydrogen or methyl;exhibit prostaglandin-like activity and are, thus, useful as platelet aggregation inhibitors.
    Type: Grant
    Filed: November 2, 1983
    Date of Patent: July 30, 1985
    Assignee: Syntex (U.S.A.) Inc.
    Inventors: Joseph M. Muchowski, Angel Guzman
  • Patent number: 4505927
    Abstract: 5-benzoyl-7-halo-1,2-dihydro-3H-pyrrolo[1,2-a]-pyrrole-1-carboxylic acids, represented by the formula ##STR1## and the pharmaceutically acceptable non-toxic esters and salts thereof, wherein:R is hydrogen or lower alkyl;X is hydrogen, lower alkyl, lower alkoxyl, lower alkoxycarbonyl, carboxyl, lower alkylcarbonyl, sulfonic acid, sulfonic acid alkyl ester, fluoro, chloro, or bromo; and Y is chloro or bromo, which are novel, and 5-benzoyl-1,2-dihydro-3H-pyrrolo[1,2-a]pyrrole-1-carboxylic acids which are represented by the formula ##STR2## wherein X and R are as above defined except that X cannot be chloro or bromo, are prepared by decarboxylation of the corresponding 1,1 dicarboxylates. Intermediates in said preparation are also disclosed.
    Type: Grant
    Filed: January 15, 1982
    Date of Patent: March 19, 1985
    Assignee: Syntex (U.S.A.) Inc.
    Inventors: Joseph M. Muchowski, Robert Greenhouse
  • Patent number: 4496577
    Abstract: This invention relates to novel imidazolidinone prostaglandin compounds of the formula ##STR1## and the pharmaceutically acceptable salts thereof, wherein R.sup.1 and R.sup.2 are independently hydrogen or alkyl of 1 to 4 carbons; R.sup.3 is hydrogen or methyl; and R4 is --(CH.sub.2).sub.n CH.sub.3 wherein n is 3-7, cycloalkyl of 5-7 carbons, a substituent of the formula ##STR2## wherein R.sup.5 is hydrogen, alkyl of 1 to 4 carbons, alkoxy of 1 to 4 carbons, halo or trifluoromethyl. These compounds are inhibitors of blood platelet aggregation.
    Type: Grant
    Filed: October 5, 1983
    Date of Patent: January 29, 1985
    Assignee: Syntex (U.S.A.) Inc.
    Inventors: Joseph M. Muchowski, Angel Guzman
  • Patent number: 4458081
    Abstract: 5-Substituted-1,2-dihydro-3H-pyrrolo[1,2-a]pyrrole-1-carboxylic acids of the formula ##STR1## wherein: X is hydrogen or lower alkyl; Ar is a moiety selected from the group consisting of ##STR2## in which: Y is oxygen or sulfur;R is hydrogen, methyl, chloro, or bromo, the R substitution being at the 3, 4 or 5 position of the ring;R.sup.1 is hydrogen, lower alkyl, lower alkoxyl, lower alkoxycarbonyl, lower alkylcarbonyl, fluoro, chloro or bromo, the R.sup.1 substitution being at any available position in the ring;R.sup.2 is hydrogen or lower alkyl;are prepared by .beta.-decarboxylation of the corresponding dialkyl-1,1-dicarboxylates. Certain substituted pyrroles are useful as intermediates for preparing the compounds of formula I.
    Type: Grant
    Filed: June 11, 1982
    Date of Patent: July 3, 1984
    Assignee: Syntex (U.S.A.) Inc.
    Inventors: Joseph M. Muchowski, Robert Greenhouse
  • Patent number: 4456759
    Abstract: 5-benzoyl-7-halo-1,2-dihydro-3H-pyrrolo[1,2-a]-pyrrole-1-carboxylic acids, represented by the formula ##STR1## and the pharmaceutically acceptable non-toxic esters and salts thereof, wherein:R is hydrogen or lower alkyl;X is hydrogen, lower alkyl, lower alkoxyl, lower alkoxycarbonyl, carboxyl, lower alkylcarbonyl, sulfonic acid, sulfonic acid alkyl ester, fluoro, chloro, or bromo; and Y is chloro or bromo, which are novel, and 5-benzoyl-1,2-dihydro-3H-pyrrolo[1,2-a]pyrrole-1-carboxylic acids which are represented by the formula ##STR2## wherein X and R are as above defined except that X cannot be chloro or bromo, are prepared by decarboxylation of the corresponding 1,1 dicarboxylates. Intermediates in said preparation are also disclosed.
    Type: Grant
    Filed: June 11, 1982
    Date of Patent: June 26, 1984
    Assignee: Syntex (U.S.A.) Inc.
    Inventors: Joseph M. Muchowski, Robert Greenhouse