Patents Represented by Attorney Gildo E. Fato
  • Patent number: 4868181
    Abstract: 1,4-Dihydropyridine derivatives which combine both calcium agonist and alpha.sub.1 -antagonist activity are useful in treating congestive heart failure. These derivatives are compounds having the formula: ##STR1## wherein Ar, R.sup.3, R.sup.4, R.sup.5 and R.sup.6 are defined in the specification.
    Type: Grant
    Filed: June 30, 1987
    Date of Patent: September 19, 1989
    Assignee: E. I. Du Pont de Nemours and Company
    Inventors: Alexander L. Johnson, Philip Ma, Petrus B. M. W. M. Timmermans, Ruth R. Wexler
  • Patent number: 4857552
    Abstract: An injectable, aqueous pharmaceutical composition for the treatment of cardiac conditions comprising an effective amount of methyl 3-[4-(2-hydroxy-3-isopropylamino)propoxy]phenylpropionate hydrochloride (esmolol) for treating such a cardiac condition, said composition comprising about 1 mg to 250 mg of esmolol per milliliter of said injectable pharmaceutical composition; 0.01 to 0.02M buffer; said composition having a pH range of 4.5 to 5.5, the esmolol degrading in aqueous solution to produce 3-[4-(3-propionic acid)phenoxy]-1-isopropylamino-2-propanol hydrochloride, said 3-[4-(3-propionic acid)-phenoxyl]-1-isopropylamino-2-propanol hydrochloride having a pK in the pH range of said composition to thereby act as a secondary buffer to increase the buffer capacity and minimize the change in pH as degradation occurs, whereby the stability of esmolol in an aqueous composition is enhanced.
    Type: Grant
    Filed: June 8, 1988
    Date of Patent: August 15, 1989
    Assignee: E. I. du Pont de Nemours and Co.
    Inventors: Leonard S. Rosenberg, Cheryl Black, Earl R. Speicher, Dietmar Wagenknecht
  • Patent number: 4850981
    Abstract: Intravenous infusion sets suitable for the parenteral administration of nitroglycerin solutions and methods of using such sets are provided. The intravenous infusion sets and methods herein utilize flexible drip tubes having their inner surfaces constructed of polyolefin plastic material. Polyolefin or polyolefin-lined drip tubes can be advantageously used to infuse nitroglycerin solutions with minimized loss of nitroglycerin solution potency.
    Type: Grant
    Filed: January 24, 1983
    Date of Patent: July 25, 1989
    Assignee: E. I. Du Pont de Nemours and Company
    Inventors: Dietmar M. Wagenknecht, Anton H. Amann, Daphne R. Gallagher
  • Patent number: 4849515
    Abstract: A novel compound, also known as 7(s)-chloro-7-deoxylincomycin-2-phosphoryl benzylate, useful an an intermediate in the production of the antibiotic, clindamycin-2-phosphate.
    Type: Grant
    Filed: August 22, 1988
    Date of Patent: July 18, 1989
    Assignee: E. I. du Pont de Nemours and Company
    Inventors: William L. Matier, Chi Woo, Ying-Chi Lee
  • Patent number: 4810704
    Abstract: Described are compounds of the formula: ##STR1## wherein Y denotes dimethylamino, methylpropynylamino, pyrrolidino, piperidino, or morpholino; R.sub.1 and R.sub.2 independently of each other denote hydrogen or loweralkyl; and X denotes loweralkyl, loweralkoxy, or halo; and n is an integer from 1 to 3 inclusive, or pharmaceutically acceptable salts thereof.The compounds exhibit antiarrhythmic activity without unwanted sympathomimetic effects.
    Type: Grant
    Filed: May 26, 1988
    Date of Patent: March 7, 1989
    Assignee: E. I. du Pont de Nemours and Company
    Inventors: David M. Stout, William L. Matier, Lawrence A. Black
  • Patent number: 4810714
    Abstract: Described are compounds of the formula: ##STR1## wherein Y denotes dimethylamino, methylpropynylamino, pyrrolidino, piperidino, or morpholino; R.sub.1 and R.sub.2 independently of each other denote hydrogen or loweralkyl; and X denotes loweralkyl, loweralkoxy, or halo; and n is an integer from 1 to 3 inclusive, or pharmaceutically acceptable salts thereof.The compounds exhibit antiarrhythmic activity without unwanted sympathomimetic effects.
    Type: Grant
    Filed: May 26, 1988
    Date of Patent: March 7, 1989
    Assignee: E. I. du Pont de Nemours and Company
    Inventors: David M. Stout, William L. Matier, Lawrence A. Black
  • Patent number: 4810717
    Abstract: Novel compounds of the general formula ##STR1## wherein Ar represents a substituted or unsubstituted aromatic or heterocyclic group; W represents alkylene of from 1 to about 10 carbon atoms; and B represents --NR.sub.2 COR.sub.1, --NR.sub.2 CONR.sub.1 R.sub.3, --NR.sub.2 SO.sub.2 R.sub.1, --NR.sub.2 SO.sub.2 NR.sub.1 R.sub.3, or --NR.sub.2 COOR.sub.1 wherein R.sub.1, R.sub.2 and R.sub.3 may be the same or different and may be hydrogen, alkyl, alkoxyalkyl, cycloalkyl, alkenyl, alkynyl, aryl, heteroaryl, or aralkyl, except that R.sub.1 is not hydrogen when B is --NR.sub.2 SO.sub.2 R.sub.1 or --NR.sub.2 COOR.sub.1, or R.sub.1 and R.sub.3 may together with N form a 5 to 7 membered heterocyclic group; and the pharmaceutically acceptable salts thereof. These compounds exhibit .beta.-adrenergic blocking activity and are also useful in the treatment of glaucoma.
    Type: Grant
    Filed: March 10, 1986
    Date of Patent: March 7, 1989
    Assignee: E. I. du Pont de Nemours and Company
    Inventors: Sheung T. Kam, William L. Matier
  • Patent number: 4804677
    Abstract: Novel compounds of the general formula ##STR1## wherein R.sub.1 is lower alkyl, lower cycloalkyl, lower alkenyl, lower alkynyl, lower alkyl carboxymethyl, aryl carboxymethyl, aryl, or aralkyl; A is a direct bond, lower alkylene, or lower alkenylene; x is 1 or 2, provided that when x is greater than 1, different occurrences of the ##STR2## group may be the same or different; Ar is heterocyclic unsubstituted aromatic or aromatic substituted with lower alkyl, lower alkenyl, lower alkynyl, lower alkoxy, halogen, acetamido, amino, nitro, lower alkylamino, hydroxy, lower hydroxyalkyl or cyano; W is alkylene containing from 1 to about 10 carbon atoms; and B is --NR.sub.2 COR.sub.3, --NR.sub.2 CONR.sub.3 R.sub.4, --NR.sub.2 SO.sub.2 R.sub.3, --NR.sub.2 SO.sub.2 NR.sub.3 R.sub.4, or --NR.sub.2 COOR.sub.5, wherein R.sub.2, R.sub.3, R.sub.4 and R.sub.5 may be the same or different and may be hydrogen, alkyl, alkoxyalkyl, alkoxyaryl, cycloalkyl, alkenyl, alkynyl, aryl, heteroaryl, or aralkyl, except that R.sub.3 and R.
    Type: Grant
    Filed: September 8, 1987
    Date of Patent: February 14, 1989
    Assignee: E. I. du Pont de Nemours and Company
    Inventors: Paul W. Erhardt, William L. Matier
  • Patent number: 4798892
    Abstract: The present invention relates to compounds of the general formula ##STR1## wherein Ar represents a substituted or unsubstituted heterocyclic group; W represents alkylene of from 1 to about 10 carbon atoms; and B represents --NR.sub.2 COR.sub.1, --NR.sub.2 CONR.sub.1 R.sub.3, --NR.sub.2 SO.sub.2 R.sub.1, NR.sub.2 SO.sub.2 NR.sub.1 R.sub.3, or --NR.sub.2 COOR.sub.1, wherein R.sub.1, R.sub.2 and R.sub.3 may be alike or different and may be hydrogen, alkyl, alkoxyalkyl cycloalkyl, alkenyl, alkynyl, aryl, heteroaryl, or aralkyl, except that R.sub.1 is not hydrogen when B is --NR.sub.2 SO.sub.2 R.sub.1 or --NR.sub.2 COOR.sub.1, or R.sub.1 and R.sub.3 may together with N form a 5 to 7 membered heterocyclic group and the pharmaceutically acceptable salts thereof. The compounds exhibit beta-adrenergic blocking activity and are also useful in the treatment of glaucoma.
    Type: Grant
    Filed: April 14, 1986
    Date of Patent: January 17, 1989
    Assignee: E. I. Du Pont de Nemours and Company
    Inventors: Sheung T. Kam, William L. Matier, Ghanshyam Patil, Khuong H. X. Mai
  • Patent number: 4778807
    Abstract: Described are compounds of the formula: ##STR1## wherein Y denotes dimethylamino, methylpropynylamino, pyrrolidino, piperidino, or morpholino; R.sub.1 and R.sub.2 independently of each other denote hydrogen or loweralkyl; and X denotes loweralkyl, loweralkoxy, or halo; and n is and integer from 1 to 3 inclusive, or pharmaceutically acceptable salts thereof.The compounds exhibit antiarrhythmic activity without unwanted sympathomimetic effects.
    Type: Grant
    Filed: October 13, 1987
    Date of Patent: October 18, 1988
    Assignee: E. I. Du Pont de Nemours & Company
    Inventors: David M. Stout, William L. Matier, Lawrence A. Black
  • Patent number: 4764630
    Abstract: A process for the preparation of N,N'-bis-trialkylsilyl carbodiimide, according to the following schematic diagram: ##STR1## where R.sub.1, R.sub.2 and R.sub.3 are each independently hydrogen, C.sub.1 -C.sub.20 alkyl, C.sub.3 -C.sub.12 cycloalkyl, C.sub.7 -C.sub.15 aralkyl, unsubstituted or substituted aryl or heteroaryl or alternatively, R.sub.1 and R.sub.2 together with the silicon atom form a 3 to 12 member heterocyclic group, optionally including oxygen, sulfur, or phosphorus as a second heteroatom, the process comprising: reacting a trialkylsilyl cyanide with cyanamide as a neat mixture to prepare the desired N,N'-bis-trialkylsilyl carbodiimide. The reaction is practically complete in one minute. The compounds so prepared are intermediates in the preparation of polymers and precursors of carbodiimide.
    Type: Grant
    Filed: December 2, 1987
    Date of Patent: August 16, 1988
    Assignee: E. I. Du Pont de Nemours and Company
    Inventors: Khuong H. X. Mai, Ghanshyam Patil
  • Patent number: 4755527
    Abstract: The present invention relates to new compounds of the formula ##STR1## where X is ##STR2## alkylene, or --S--where R.sub.1 is hydrogen, alkyl, or aryl; W is hydrogen, hydroxy, amino, alkyloxy, aryloxy, O-alkyl, or O-aralkyl; (Y).sub.A) is --CH.sub.2 NR.sub.2 R.sub.3 where R.sub.2 and R.sub.3 may be hydrogen, substituted alkyls, aryls, or together with N form a 5 to 7 membered heterocyclic group; and Ar is a substituted or unsubstituted aryl. These compounds are useful in the treatment of various cardiac arrhythmias.
    Type: Grant
    Filed: December 27, 1985
    Date of Patent: July 5, 1988
    Assignee: E. I. Du Pont de Nemours and Company
    Inventors: David M. Stout, William L. Matier
  • Patent number: 4748184
    Abstract: The present invention relates to new compounds of the formula ##STR1## wherein X is ##STR2## wherein R.sub.1 is hydrogen, lower alkyl, phenyl, benzyl, cinnamoyl, thiophene, furan, pyrrole, imidazole, pyrazole oxazole or thiazole; W is hydrogen or hydroxy; (Y).sub.A is positioned ortho to W and is an aminoloweralkyl having the formula --CH.sub.2 NR.sub.2 R.sub.3 where R.sub.2 and R.sub.3 are the same or different and may be lower alkyl or R.sub.2 and R.sub.3 may together with N form a pyrrolidine, piperidine or azepine ring, and A is 2; n and m are independently from 0 to 5; and R is straight or branched C.sub.1 -C.sub.10 alkyl, straight or branched C.sub.3 -C.sub.10 cycloalkyl, straight or branched C.sub.2 -C.sub.4 alkenyl or straight or branched C.sub.2 -C.sub.4 alkynyl, or a pharmaceutically acceptable salt thereof.These compounds are useful in the treatment of various cardiac arrhythmias.
    Type: Grant
    Filed: December 27, 1985
    Date of Patent: May 31, 1988
    Assignee: E. I. Du Pont de Nemours and Company
    Inventors: David M. Stout, William L. Matier, Lawrence A. Black
  • Patent number: 4709042
    Abstract: Described is a process for preparing 2-(1-hydroxyalkyl)-5,5-diphenylhydantoin having the formula ##STR1## wherein R.sub.1, R.sub.2 and R.sub.3 are each independently hydrogen, C.sub.1 -C.sub.20 alkyl, C.sub.3 -C.sub.12 cycloalkyl, C.sub.7 -C.sub.15 aralkyl, unsubstituted or substituted aryl or heteroaryl or alternatively, or R.sub.1 and R.sub.2 together with the carbon atom form a 3 to 12 member cycloalkyl group, the process comprising: reacting diphenylhydantoin with an aldehyde or a ketone in the presence of a strong inorganic base; an alcohol was used as solvent to solubilize the reactants. The reaction is practically complete in 15 minutes.The compounds so prepared are intermediates in the preparation of phenyltoin prodrugs.
    Type: Grant
    Filed: September 19, 1986
    Date of Patent: November 24, 1987
    Assignee: E. I. Du Pont de Nemours & Co., (Inc.)
    Inventors: Khuong H. X. Mai, Ghanshyam Patil
  • Patent number: 4692446
    Abstract: Novel compounds of the general formula ##STR1## wherein R.sub.1 is lower alkyl, lower cycloalkyl, lower alkenyl, lower alkynyl, lower alkyl carboxymethyl, aryl carboxymethyl, aryl, or aralkyl; A is a direct bond, lower alkylene, or lower alkenylene; x is 1 or 2, provided that when x is greater than 1, different occurrences of the ##STR2## group may be the same or different; Ar is heterocyclic, unsubstituted aromatic or aromatic substituted with lower alkyl, lower alkenyl, lower alkynyl, lower alkoxy, halogen, acetamido, amino, nitro, lower alkylamino, hydroxy, lower hydroxyalkyl or cyano; W is alkylene containing from 1 to about 10 carbon atoms; and B is --NR.sub.2 COR.sub.3, --NR.sub.2 CONR.sub.3 R.sub.4, --NR.sub.2 SO.sub.2 R.sub.3, --NR.sub.2 SO.sub.2 NR.sub.3 R.sub.4, or --NR.sub.2 COOR.sub.5, wherein R.sub.2, R.sub.3, R.sub.4 and R.sub.5 may be the same or different and may be hydrogen, alkyl, alkoxyalkyl, alkoxyaryl, cycloalkyl, alkenyl, alkynyl, aryl, heteroaryl, or aralkyl, except that R.sub.3 and R.
    Type: Grant
    Filed: October 28, 1986
    Date of Patent: September 8, 1987
    Assignee: E. I. Du Pont de Nemours & Co., Inc.
    Inventors: Paul W. Erhardt, William L. Matier
  • Patent number: 4666924
    Abstract: The present invention relates to new compounds of the formula ##STR1## where X is ##STR2## alkylene, or --S--where R.sub.1 is hydrogen, alkyl, or aryl; W is hydrogen, hydroxy, amino, alkyloxy, aryloxy, O-alkyl, or O-aralkyl; (Y).sub.A) is --CH.sub.2 NR.sub.2 R.sub.3 where R.sub.2 and R.sub.3 may be hydrogen, substituted alkyls, aryls, or together with N form a 5 to 7 membered heterocyclic group; and Ar is a substituted or unsubstituted heteroaryl. These compounds are useful in the treatment of various cardiac arrhythmias.
    Type: Grant
    Filed: June 4, 1984
    Date of Patent: May 19, 1987
    Assignee: E. I. Du Pont de Nemours & Co.
    Inventors: David M. Stout, William L. Matier
  • Patent number: 4657919
    Abstract: Described are compounds of the formula ##STR1## wherein R is hydrogen, lower alkyl, halo, cyano, hydroxy, amino, lower alkylamino, --CH.sub.2 NH.sub.2, --CH.sub.2 OH or --COOR"; R' is hydrogen, lower cycloalkyl or lower alkyl; R' is lower alkenyl, lower alkynyl, lower cycloalkyl, --(W).sub.n Y wherein W is straight or branched chain lower alkyl or lower alkenyl, n is 0 to 5, and Y is Ar, lower cycloalkyl, lower alkenyl, lower alkynyl, --COOZ wherein Z is lower alkyl, ##STR2## or NAB wherein A and B are, independently, lower alkyl, benzyl or substituted benzyl, and Ar is 2, 3 or 4-pyridyl, pyridazinyl, pyrimidinyl, quinolyl, isoquinolyl, phthalazinyl, quinazolinyl, thiazolyl, phenyl, benzyl, furyl, tetrahydrofuryl or thienyl, unsubstituted or substituted with lower alkyl, lower alkoxy, halo, amino, or --CF.sub.3 ; R"' is --COOR", ##STR3## and X is oxygen or nitrogen; or a pharmaceutically acceptable salt thereof, and their use in the treatment of impaired ventricular myocardial contractility.
    Type: Grant
    Filed: July 12, 1985
    Date of Patent: April 14, 1987
    Assignee: E. I. Du Pont de Nemours & Co.
    Inventors: David M. Stout, Diane M. Yamamoto, Cynthia Barcelon-Yang
  • Patent number: 4636201
    Abstract: Described is a hypodermic syringe which includes provision for a rigid sheath cover or sleeve which encompasses the rubber needle cover and provides protection in the operating mode as well as other advantages. The rubber needle cover is placed over the needle and provides a sterile barrier for the needle after the syringe unit is sterilized.The sheath cover can be made of plastic and includes a plurality of teeth spaced about the opening of the cover. At least some of the teeth have a small lip projecting inwardly from the end of the teeth toward the center of the opening. When the rigid sleeve is inserted over the rubber needle cover, the lips slip over the cover to grip it so that when the sleeve is removed, the rubber cover is retained within the sleeve and the two are removed together. After the medicament is administered, the needle cover and sheath are replaced.
    Type: Grant
    Filed: November 1, 1985
    Date of Patent: January 13, 1987
    Assignee: American Hospital Supply Corporation
    Inventors: William A. Ambrose, Fernando A. Garcia
  • Patent number: 4623652
    Abstract: Novel compounds of the general formula ##STR1## wherein R.sub.1 is lower alkyl, lower cycloalkyl, lower alkenyl, lower alkynyl, lower alkyl carboxymethyl, aryl carboxymethyl, aryl, or aralkyl; A is a direct bond, lower alkylene, or lower alkenylene; x is 1 or 2, provided that when x is greater than 1, different occurrences of the ##STR2## group may be the same or different; Ar is heterocyclic, unsubstituted aromatic or aromatic substituted with lower alkyl, lower alkenyl, lower alkynyl, lower alkoxy, halogen, acetamido, amino, nitro, lower alkylamino, hydroxy, lower hydroxyalkyl or cyano; W is alkylene containing from 1 to about 10 carbon atoms; and B is --NR.sub.2 COR.sub.3, --NR.sub.2 CONR.sub.3 R.sub.4, --NR.sub.2 SO.sub.2 R.sub.3, --NR.sub.2 SO.sub.2 NR.sub.3 R.sub.4, or --NR.sub.2 COOR.sub.5, wherein R.sub.2, R.sub.3, R.sub.4 and R.sub.5 may be the same or different and may be hydrogen, alkyl, alkoxyalkyl, alkoxyaryl, cycloalkyl, alkenyl, alkynyl, aryl, heteroaryl, or aralkyl, except that R.sub.3 and R.
    Type: Grant
    Filed: January 16, 1985
    Date of Patent: November 18, 1986
    Assignee: American Hospital Supply Corporation
    Inventors: Paul W. Erhardt, William L. Matier
  • Patent number: D297570
    Type: Grant
    Filed: November 1, 1985
    Date of Patent: September 6, 1988
    Assignee: E. I. Du Pont de Nemours and Company
    Inventors: William A. Ambrose, Fernando A. Garcia