Patents Represented by Attorney Gildo E. Fato
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Patent number: 4868181Abstract: 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: GrantFiled: June 30, 1987Date of Patent: September 19, 1989Assignee: E. I. Du Pont de Nemours and CompanyInventors: Alexander L. Johnson, Philip Ma, Petrus B. M. W. M. Timmermans, Ruth R. Wexler
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Patent number: 4857552Abstract: 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: GrantFiled: June 8, 1988Date of Patent: August 15, 1989Assignee: E. I. du Pont de Nemours and Co.Inventors: Leonard S. Rosenberg, Cheryl Black, Earl R. Speicher, Dietmar Wagenknecht
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Patent number: 4850981Abstract: 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: GrantFiled: January 24, 1983Date of Patent: July 25, 1989Assignee: E. I. Du Pont de Nemours and CompanyInventors: Dietmar M. Wagenknecht, Anton H. Amann, Daphne R. Gallagher
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Patent number: 4849515Abstract: 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: GrantFiled: August 22, 1988Date of Patent: July 18, 1989Assignee: E. I. du Pont de Nemours and CompanyInventors: William L. Matier, Chi Woo, Ying-Chi Lee
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Patent number: 4810704Abstract: 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: GrantFiled: May 26, 1988Date of Patent: March 7, 1989Assignee: E. I. du Pont de Nemours and CompanyInventors: David M. Stout, William L. Matier, Lawrence A. Black
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Patent number: 4810714Abstract: 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: GrantFiled: May 26, 1988Date of Patent: March 7, 1989Assignee: E. I. du Pont de Nemours and CompanyInventors: David M. Stout, William L. Matier, Lawrence A. Black
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Patent number: 4810717Abstract: 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: GrantFiled: March 10, 1986Date of Patent: March 7, 1989Assignee: E. I. du Pont de Nemours and CompanyInventors: Sheung T. Kam, William L. Matier
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Patent number: 4804677Abstract: 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: GrantFiled: September 8, 1987Date of Patent: February 14, 1989Assignee: E. I. du Pont de Nemours and CompanyInventors: Paul W. Erhardt, William L. Matier
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Patent number: 4798892Abstract: 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: GrantFiled: April 14, 1986Date of Patent: January 17, 1989Assignee: E. I. Du Pont de Nemours and CompanyInventors: Sheung T. Kam, William L. Matier, Ghanshyam Patil, Khuong H. X. Mai
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Patent number: 4778807Abstract: 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: GrantFiled: October 13, 1987Date of Patent: October 18, 1988Assignee: E. I. Du Pont de Nemours & CompanyInventors: David M. Stout, William L. Matier, Lawrence A. Black
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Patent number: 4764630Abstract: 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: GrantFiled: December 2, 1987Date of Patent: August 16, 1988Assignee: E. I. Du Pont de Nemours and CompanyInventors: Khuong H. X. Mai, Ghanshyam Patil
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Patent number: 4755527Abstract: 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: GrantFiled: December 27, 1985Date of Patent: July 5, 1988Assignee: E. I. Du Pont de Nemours and CompanyInventors: David M. Stout, William L. Matier
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Patent number: 4748184Abstract: 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: GrantFiled: December 27, 1985Date of Patent: May 31, 1988Assignee: E. I. Du Pont de Nemours and CompanyInventors: David M. Stout, William L. Matier, Lawrence A. Black
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Patent number: 4709042Abstract: 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: GrantFiled: September 19, 1986Date of Patent: November 24, 1987Assignee: E. I. Du Pont de Nemours & Co., (Inc.)Inventors: Khuong H. X. Mai, Ghanshyam Patil
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Patent number: 4692446Abstract: 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: GrantFiled: October 28, 1986Date of Patent: September 8, 1987Assignee: E. I. Du Pont de Nemours & Co., Inc.Inventors: Paul W. Erhardt, William L. Matier
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Patent number: 4666924Abstract: 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: GrantFiled: June 4, 1984Date of Patent: May 19, 1987Assignee: E. I. Du Pont de Nemours & Co.Inventors: David M. Stout, William L. Matier
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Patent number: 4657919Abstract: 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: GrantFiled: July 12, 1985Date of Patent: April 14, 1987Assignee: E. I. Du Pont de Nemours & Co.Inventors: David M. Stout, Diane M. Yamamoto, Cynthia Barcelon-Yang
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Patent number: 4636201Abstract: 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: GrantFiled: November 1, 1985Date of Patent: January 13, 1987Assignee: American Hospital Supply CorporationInventors: William A. Ambrose, Fernando A. Garcia
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Patent number: 4623652Abstract: 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: GrantFiled: January 16, 1985Date of Patent: November 18, 1986Assignee: American Hospital Supply CorporationInventors: Paul W. Erhardt, William L. Matier
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Patent number: D297570Type: GrantFiled: November 1, 1985Date of Patent: September 6, 1988Assignee: E. I. Du Pont de Nemours and CompanyInventors: William A. Ambrose, Fernando A. Garcia