Patents Represented by Attorney John J. Kolano

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  • Hydroxymethyl-indolizidines and quinolizidines and their use as .alpha.-glucosidase I inhibitors
    Patent number: 5028614
    Abstract: The present invention describes a group of polyhydroxylated indolizidines and quinolizidines and their esters. These compounds are prepared starting from 2,6-dideoxy-2,6-dideoxy-2,6-imino-1,3,4,5-tetrakis-O- (phenylmethyl)-D-glycero-L-gulo-heptitol or a corresponding N-substituted compound. The compounds are useful in the treatment of diabetes and as .alpha.-glucosidase I inhibitors.
    Type: Grant
    Filed: March 30, 1990
    Date of Patent: July 2, 1991
    Assignee: Merrell Dow Pharmaceuticals Inc.
    Inventors: Paul S. Liu, Mohinder S. Kang, Roland S. Rogers, Barry L. Rhinehart
  • Castanospermine esters and glycosides
    Patent number: 5017563
    Abstract: Castanospermine mono- and di-esters and glycosides active as inhibitors of carbohydrate digestive enzymes and useful in treating diabetes are described herein. The compounds are prepared by the reaction of castanospermine with an appropriate acid halide or anhydride or with an appropriate glycosyl halide or glycosyl acetimidate under conditions which would favor the isolation of the mono- and di-esterified and glycosylated products. Various blocking groups, which can be selectively removed under mild conditions, can also be used to favor the formation of certain isomers.
    Type: Grant
    Filed: May 1, 1990
    Date of Patent: May 21, 1991
    Assignee: Merrell Dow Pharmaceuticals Inc.
    Inventors: Paul S. Liu, Barry L. Rhinehart, John K. Daniel
  • Substituted triazolopyridazines, pharmaceutical compositions and use
    Patent number: 5011835
    Abstract: This invention is directed to a group of compounds which are acyl derivatives of amino substituted triazolopyridazines. They are prepared by the reaction of an aminotriazolopyridazine or an aminotriazolophthalazine with an appropriate acid chloride. These compounds possess bronchodilating and antiallergenic activity.
    Type: Grant
    Filed: February 7, 1990
    Date of Patent: April 30, 1991
    Assignee: Merrell Dow Pharmaceuticals Inc.
    Inventors: Norton P. Peet, Shyam Sunder
  • Process for the preparation of castanospermine esters
    Patent number: 4970317
    Abstract: 1-Esters of castanospermine have been prepared enzymatically from appropriate activated esters using substilisin. The esters obtained in this way can be further reacted enzymatically to give diesters which can, in turn, be selectively hydrolyzed to give monoesters in good yield.
    Type: Grant
    Filed: August 8, 1989
    Date of Patent: November 13, 1990
    Assignee: Merrell Dow Pharmaceuticals Inc.
    Inventors: Alexey L. Margolin, Deborah L. Delinck
  • 4-substituted 17.beta.-(cyclopropylamino)androst-5-en-3.beta.-ol and related compounds useful as C.sub.17-20 lyase inhibitors
    Patent number: 4966898
    Abstract: This invention is directed to 4-substituted 17.beta.-(cyclopropylamino)androst-5-en-3.beta.-ol and related compounds and also to a method for using such compounds in the treatment of androgen-dependent disorders. The compounds are prepared by the hydride reduction of an appropriate steroidal imine or enamine.
    Type: Grant
    Filed: August 15, 1989
    Date of Patent: October 30, 1990
    Assignee: Merrell Dow Pharmaceuticals Inc.
    Inventors: Michael R. Angelastro, Thomas R. Blohm
  • 4-substituted 17.beta.-(cyclopropyloxy)androst-5-en-3.beta.-ol and related compounds useful as C17-20 lyase inhibitors
    Patent number: 4966897
    Abstract: This invention is directed to 4-substituted 17.beta.-(cyclopropyloxy)androst-5-en-3.beta.-ols and related compounds and also to a method for using such compounds in the treatment of androgen-dependent disorders. The ethers are prepared by using the Simmons-Smith reaction and an appropriate vinyl ether.
    Type: Grant
    Filed: August 15, 1989
    Date of Patent: October 30, 1990
    Assignee: Merrell Dow Pharmaceuticals Inc.
    Inventors: Michael R. Angelastro, Thomas R. Blohm
  • Method of treatment using 18-cyanoprogesterone derivatives
    Patent number: 4954491
    Abstract: The present invention is directed to a method for the treatment of hyperaldosteronism and related disorders which comprises administering to an appropriate patient an appropriate 18-cyanopregnane.
    Type: Grant
    Filed: January 27, 1989
    Date of Patent: September 4, 1990
    Assignee: Merrell Dow Pharmaceuticals Inc.
    Inventors: J. O'Neal Johnston, Gene W. Holbert
  • Castanospermine esters in the inhibition of tumor metastasis
    Patent number: 4952585
    Abstract: A method for the inhibition of tumor metastases is described herein. The method makes use of the administration of certain castanospermine esters or their pharmaceutically acceptable salts.
    Type: Grant
    Filed: December 15, 1988
    Date of Patent: August 28, 1990
    Assignee: Merrell Dow Pharmaceuticals Inc.
    Inventors: Sai P. Sunkara, Paul S. Liu
  • 19-fluoro- or cyano-21-hydroxyprogesterone derivatives useful as 19-hydroxylase inhibitors
    Patent number: 4920114
    Abstract: 19-Fluoro- and cyano- substituted 21-hydroxyprogesterone derivatives and related compounds which are active as 19-hydroxylase inhibitors and useful as antihypertensive agents are described herein. The compounds are prepared using appropriate synthetic pathways which will vary according to the nature of the specific 19-substituted progesterone or related compound desired.
    Type: Grant
    Filed: June 28, 1988
    Date of Patent: April 24, 1990
    Assignee: Merrell Dow Pharmaceuticals Inc.
    Inventors: Gene W. Holbert, J. O'Neal Johnston
  • 19-substituted progesterone derivatives useful as 19-hydroxylase inhibitors
    Patent number: 4910191
    Abstract: 19-Substituted progesterone derivatives and related compounds which are active as 19-hydroxylase inhibitors and useful as antihypertensive agents are described herein. The compounds are prepared using appropriate synthetic pathways which will vary according to the nature of the specific 19-substituted progesterone or related compound desired.
    Type: Grant
    Filed: June 28, 1988
    Date of Patent: March 20, 1990
    Assignee: Merrell Dow Pharmaceuticals Inc.
    Inventors: Gene W. Holbert, J. O'Neal Johnston
  • Synthesis of intermediate useful in the preparation of nojirimycin and related compounds
    Patent number: 4908439
    Abstract: 5-Amino-5-deoxy-1,2-O-isopropylidene-.alpha.-D-glucofuranose is conveniently prepared by a hydride reduction of 5-azido-5-deoxy-1,2,O-isopropylidene-.alpha.-D-glucuronolactone and can readily be converted to nojirimycin, deoxynojirimycin or homonojirimycin.
    Type: Grant
    Filed: September 16, 1988
    Date of Patent: March 13, 1990
    Assignee: Merrell Dow Pharmaceuticals Inc.
    Inventor: Peter Anzeveno
  • Esters of hexahydro-8-hydroxy-2,6-methano-2H-quinolizin-3-(4H)-one and related compounds
    Patent number: 4906755
    Abstract: The present invention is directed to a group of esters of hexahydro-8-hydroxy-2,6-methano-2H-quinolizin-3(3H)-ones and related compounds. The compounds are prepared from the appropriate carboxylic acids and alcohols by standard procedures or, where steric factors are significant, a new process which makes use of heavy metal salts of super acids can be used. The compounds involved are useful in the treatment of migraine and similar disorders and in cytotoxic drug-induced vomiting.
    Type: Grant
    Filed: June 30, 1989
    Date of Patent: March 6, 1990
    Assignee: Merrell Dow Pharmaceuticals Inc.
    Inventor: Maurice W. Gittos
  • 17.beta.-(cyclopropyloxy)androst-5-en-3.beta.-ol and related compounds useful as C.sub.17-20 lyase inhibitors
    Patent number: 4891367
    Abstract: This invention is directed to 17.beta.-(cyclopropyloxy)androst-5-en-3.beta.-ol and related compounds and also to a method for using such compounds in the treatment of androgen-dependent disorders. The ethers are prepared by using the Simmons-Smith reaction and an appropriate vinyl ether.
    Type: Grant
    Filed: April 22, 1987
    Date of Patent: January 2, 1990
    Assignee: Merrell Dow Pharmaceuticals Inc.
    Inventors: Michael R. Angelastro, Thomas R. Blohm
  • 3.beta.,17.beta.-hydroxy-substituted steroids and related steroidal compounds
    Patent number: 4882322
    Abstract: The present invention is directed to a group of compounds which are 3.beta.,17.beta.-hydroxy steriods, and related steroidal structures. These compounds are armatase inhibitors, and thus, regulate or inhibit the conversion of androgens to estrogens. These compounds may be utilized to treat conditions potentiated by the presence of estrogens. These compounds exhibit a slower onset of action and a longer half life relative to the 10-(2-alkynyl) steroidal aromatase inhibitors disclosed in U.S. Pat. No. 4,322,416.
    Type: Grant
    Filed: October 27, 1988
    Date of Patent: November 21, 1989
    Assignee: Merrell Dow Pharmaceuticals Inc.
    Inventors: J. O'Neal Johnston, Gene W. Holbert
  • Process for hydrolyzing 2,6-dideoxy-2,6-iminoheptononitrile derivatives using trifluoroacetic acid and dinitrogen tetroxide
    Patent number: 4880917
    Abstract: A procedure for the mild conversion of a carbonitrile to the corresponding carboxylic acid by first using trifluoroacetic acid in the presence of a catalytic amount of mercuric ion followed by oxidative hydrolysis with dinitrogen tetroxide is described herein. The use of this procedure in the preparation of 1,3,4,5-tetra-O-benzoyl-2,6-dideoxy-2,6-imino-D-glycero-L-gulo-heptitol hydrochloride is also described here.
    Type: Grant
    Filed: July 1, 1988
    Date of Patent: November 14, 1989
    Assignee: Merrell Dow Pharmaceuticals Inc.
    Inventors: Peter B. Anzeveno, John K. Daniel, Laura J. Creemer, Paul S. Liu
  • Substituted imidazo(2,1-b)quinazolin-5(3H)-ones and related tricyclic compounds and use as bronchodilators
    Patent number: 4871732
    Abstract: The present invention is directed to a group of compounds which are imidazo[2,1-b]quinazolin-5(3H)-ones, related tricyclic compounds, and pharmaceutically acceptable salts thereof. These compounds are useful as bronchodilators. These compounds are prepared by the reaction of an appropriate hydrazine with an appropriate 1-substituted-2-methyl-2-imidazoline or chemically equivalent compound.
    Type: Grant
    Filed: September 22, 1988
    Date of Patent: October 3, 1989
    Assignee: Merrell Dow Pharmaceuticals Inc.
    Inventors: Norton P. Peet, Shyam Sunder
  • Novel aryloxycycloalkanolaminoalkylene aryl ketones
    Patent number: 4868315
    Abstract: This invention relates to aryloxycycloalkanolaminoalkylene aryl ketones to the processes for their preparation and to their use as antihypertensive agents.
    Type: Grant
    Filed: January 11, 1988
    Date of Patent: September 19, 1989
    Assignee: Merrell Dow Pharmaceuticals Inc.
    Inventors: Michael E. LeTourneau, James R. McCarthy, Donald L. Trepanier
  • Novel imidazole dopamine beta hydroxylase inhibitors
    Patent number: 4810800
    Abstract: 1,2-Disubstituted imidazoles useful as antihypertensive agents are described herein. The compounds are obtained from the appropriate 1-substituted imidazole which can be reacted with methyl oxalyl chloride to give the oxalyl derivative or it can be reacted with cyanogen chloride to give the 2-carbonitrile which can then be converted to the other derivatives desired.
    Type: Grant
    Filed: April 29, 1988
    Date of Patent: March 7, 1989
    Assignee: Merrell Dow Pharmaceuticals Inc.
    Inventors: Donald P. Matthews, James R. McCarthy, Jeffrey P. Whitten, Robert J. Broersma, Jr.
  • Castanospermine for inhibiting tumor metastasis
    Patent number: 4792558
    Abstract: A method for the inhibition of tumor metastases is described herein. The method makes use of the administration of castanospermine.
    Type: Grant
    Filed: May 29, 1987
    Date of Patent: December 20, 1988
    Assignee: Merrell Dow Pharmaceuticals Inc.
    Inventors: Sai P. Sunkara, Barry L. Rhinehart, Paul S. Liu
  • Process for preparing 2,6-di-tertiarybutyl-4-mercaptophenol by electrocatalysis
    Patent number: 4772363
    Abstract: This invention relates to an improvement in a process for making 2,6-di-tertiarybutyl-4-mercaptophenol and 4,4'-isopropylidenedithio-bis-(2,6-di-tertiarybutylphenol), which is effected by carrying out an electrocatalytic reduction of bis(3,5-di-tertiarybutyl-4-hydroxyphenol)polysulfide at a lead cathode in an acidic electrolyte medium.
    Type: Grant
    Filed: January 14, 1987
    Date of Patent: September 20, 1988
    Assignee: Merrell Dow Pharmaceuticals Inc.
    Inventor: Richard M. Van Effen