Patents by Inventor William J. Welstead, Jr.
William J. Welstead, Jr. 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).
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Patent number: 5273993Abstract: Methods of treating chronic arthritis and osteoporosis which utilize both known and novel compounds which would fall under the general formula:(HO)p--A--[--OS(O).sub.2 NR.sup.1 R.sup.2 ].sub.zwherein A encompasses a wide range of values including but not limited to aryl, loweralkyl, cycloalkyl, and carbohydrates including sucrose and fructose; p is equal to the number of unreacted hydroxy groups contained on the molecule and may be zero; z is the number of --OS(O).sub.2 NR.sup.1 R.sup.2 groups and is always at least one; R.sup.1 and R.sup.2 are selected from hydrogen, loweralkyl, carboxy and the like; a novel process for preparing the compounds is provided wherein an appropriate sulfamic acid aryl ester is reacted with a hydroxy substituted A radical which may or may not contain thereon protected carboxyl, amino or hydroxy substituents, in an aprotic solvent containing a tertiary amine base. Pharmaceutical compositions for the treatment of chronic arthritis and osteoporosis are also provided.Type: GrantFiled: November 19, 1992Date of Patent: December 28, 1993Assignee: A. H. Robins Company, IncorporatedInventors: Young S. Lo, Joseph C. Nolan, William J. Welstead, Jr., David A. Walsh, Dwight A. Shamblee, Ibrahim M. Uwaydah
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Patent number: 5194446Abstract: Methods of treating chronic arthritis and osteoporosis which utilize both known and novel compounds which would fall under the general formula:(HO)p--A--[--OS(O).sub.2 NR.sup.1 R.sup.2 ].sub.zwherein A encompasses a wide range of values including but not limited to aryl, loweralkyl, cycloalkyl, and carbohydrates including sucrose and fructose; p is equal to the number of unreacted hydroxy groups contained on the molecule and may be zero; z is the number of --OS(O).sub.2 NR.sup.1 R.sup.2 groups and is always at least one; R.sup.1 and R.sup.2 are selected from hydrogen, loweralkyl, carboxy and the like; a novel process for preparing the compounds is provided wherein an appropriate sulfamic acid aryl ester is reacted with a hydroxy substituted A radical which may or may not contain thereon protected carboxyl, amino or hydroxy substituents, in an aprotic solvent containing a tertiary amine base. Pharmaceutical compositions for the treatment of chronic arthritis and osteoporosis are also provided.Type: GrantFiled: July 24, 1991Date of Patent: March 16, 1993Assignee: A. H. Robins Company, IncorporatedInventors: Young S. Lo, Joseph C. Nolan, William J. Welstead, Jr., David A. Walsh, Dwight A. Shamblee, Ibrahim M. Uwaydah
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Patent number: 5183903Abstract: This invention relates to an improved process for the preparation of 3-phenoxy-1-azetidinecarboxamides of Formula I which are useful ##STR1## in the treatment of epileptic seizures. Under Formula I, n is 1 to 3, X is H, halogen, trifluoromethyl, C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy, acetyl, or aminocarbonyl, and R is H or methyl. This process involves heating a 3-phenoxyazetidine with urea to obtain the Formula I compound. Urea is inexpensive and easily removed by washing the solid Formula I product with water.Type: GrantFiled: November 26, 1991Date of Patent: February 2, 1993Assignee: A. H. Robins Company, IncorporatedInventors: William J. Welstead, Jr., Young S. Lo
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Patent number: 4749788Abstract: A process is described wherein pyrido[1,4]benzodiazepines having the formula: ##STR1## wherein Q is NR.sup.1 R.sup.2 or ##STR2## are prepared from unsubstituted pyridobenzodiazepinones by alkylation reaction with halo-alkyl-Q followed by acylation of the other nitrogen; breaking the ring with an aryl Grignard reagent and recyclizing to add the aryl radical and form the azepine ring. Novel intermediates are thereby disclosed.Type: GrantFiled: April 13, 1987Date of Patent: June 7, 1988Assignee: A. H. Robins Company, IncorporatedInventors: Young S. Lo, William J. Welstead, Jr.
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Patent number: 4624961Abstract: A pharmaceutical method for improving memory or correcting memory deficiency is disclosed, utilizing compounds having the formula: ##STR1## wherein m and n are zero and one and when m is zero, the dotted line represents a double bond; X is oxygen or sulfur; R.sup.1 and R.sup.2 are hydrogen, loweralkyl, phenyl or phenylloweralkyl, or R.sup.1 and R.sup.2 taken together may form a fused second ring with the nitrogen atoms having three or four methylene groups to which may be attached at any second ring carbon atom thereof, a loweralkyl or phenyl radical; R.sup.3 is hydrogen or loweralkyl; Ar is phenyl, pyridyl, furanyl, thienyl, methoxy-1H-benzotriazolyl, indolinyl, methoxyindolinyl, methoxypyrimidinyl, aminomethoxypyrimidinyl, 1,3-benzodioxolyl or naphthalenyl, the active optical isomers; and the pharmaceutically acceptable acid addition salts thereof.Type: GrantFiled: April 17, 1985Date of Patent: November 25, 1986Assignee: A. H. Robins Company, IncorporatedInventor: William J. Welstead, Jr.
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Patent number: 4605652Abstract: A pharmaceutical method for improving memory or correcting memory deficiency is disclosed, utilizing compounds having the formula: ##STR1## wherein n.sup.1, n.sup.2, n.sup.3, and n.sup.4 =0 to 3; R.sup.1, R.sup.2, R.sup.3, and R.sup.4 =H, loweralkyl or phenyl; R.sup.5 =H or loweralkyl; X=O or S; Ar=phenyl, substituted phenyl, pyridinyl, furanyl, thienyl, methoxy-1H-benzotriazolyl, indolinyl, methoxyindolinyl, methoxypyrimidinyl, amino-methoxypyrimadinyl, 1,3-benzodioxolyl, or naphthalenyl, and the pharmaceutically acceptable acid addition salts, hydrates and alcoholates thereof.Type: GrantFiled: February 4, 1985Date of Patent: August 12, 1986Assignee: A. H. Robins Company, Inc.Inventor: William J. Welstead, Jr.
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Patent number: 4585785Abstract: Cis and trans-3-aryloxy-4-hydroxypyrrolidines and derivatives thereof having the formula: ##STR1## are disclosed wherein R.sub.1 is hydrogen, loweralkyl, benzyloxycarbonyl and N-loweralkylcarbamoyl; R.sub.2 is hydrogen, lower alkyl, cycloalkyl, phenylalkyl, benzyloxycarbonyl, carbamoyl, N-loweralkylcarbamoyl, N-diloweralkylcarbamoyl and parafluorobenzoyl-lower-alkyl; Ar is phenyl, substituted phenyl, 1-naphthyl, 2-naphthyl, 1-indenyl and 2-indenyl and pharmaceutically acceptable acid addition and quaternary salts thereof. The compounds have antidepressant, antihypertensive and antiarrythmic activity in animals.Type: GrantFiled: March 10, 1980Date of Patent: April 29, 1986Assignee: A. H. Robins Company, Inc.Inventors: David A. Walsh, William J. Welstead, Jr.
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Patent number: 4568695Abstract: Novel 2-amino-3-benzoylphenethylalcohols are provided having the formula: ##STR1## wherein; X is hydrogen, loweralkyl, loweralkoxy, halogen or trifluoromethyl, andY is hydrogen, loweralkyl, loweralkoxy, halogen, trifluoromethyl, --S--loweralkyl, ##STR2## The compounds exhibit anti-inflammatory activity.Type: GrantFiled: December 7, 1983Date of Patent: February 4, 1986Assignee: A. H. Robins Company, IncorporatedInventors: Henry W. Moran, William J. Welstead, Jr.
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Patent number: 4452809Abstract: Cis and trans-3-aryloxy-4-hydroxypyrrolidines and derivatives thereof having the formula: ##STR1## are disclosed wherein R.sub.1 is hydrogen, loweralkyl, benzyloxycarbonyl and N-loweralkylcarbamoyl; R.sub.2 is hydrogen, lower alkyl, cycloalkyl, phenylalkyl, benzyloxycarbonyl, carbamoyl, N-loweralkylcarbamoyl, N-diloweralkylcarbamoyl and parafluorobenzoyl-lower-alkyl; Ar is phenyl, substituted phenyl, 1-naphthyl, 2-naphthyl, 1-indenyl and 2-indenyl and pharmaceutically acceptable acid addition and quaternary salts thereof. The compounds have antidepressant, antihypertensive and antiarrythmic activity in animals.Type: GrantFiled: April 22, 1983Date of Patent: June 5, 1984Assignee: A. H. Robins Company, Inc.Inventors: David A. Walsh, William J. Welstead, Jr.
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Patent number: 4324791Abstract: 1-R-4-(omega-substituted alkyl)-3,3-diphenyl-2-pyrrolidinones of the formula ##STR1## wherein R is hydrogen, lower alkyl, cyclohexyl or benzyl, R.sup.1 is hydrogen, chloro, bromo, fluoro, trifluoromethyl or lower alkoxy, R.sup.2 is hydrogen, chloro, bromo, or fluoro, A is hydroxy, lower-alkylcarbonyloxy or lower-alkoxycarbonyl and n is 1, 2 or 3 having analgetic and antidiarrheal activity are disclosed. The pharmaceutically acceptable acid addition salts of the bases are within the scope of the present invention.Type: GrantFiled: August 1, 1978Date of Patent: April 13, 1982Assignee: A. H. Robins Company, Inc.Inventor: William J. Welstead, Jr.
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Patent number: 4230718Abstract: 3,4-Epoxypyrrolidines substituted in the 1-position with alkyl, cycloalkyl and phenylalkyl are disclosed which have pharmaceutical application in cataract prevention in animals and as intermediates in preparation of trans-3-aryloxy-4-hydroxypyrrolidines. The epoxypyrrolidines are prepared by a novel route involving chlorination of pyrrolines in aqueous medium.Type: GrantFiled: January 9, 1979Date of Patent: October 28, 1980Assignee: A. H. Robins Company, Inc.Inventors: David A. Walsh, William J. Welstead, Jr.
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Patent number: 4221716Abstract: A novel process for the preparation of 7-acylindolin-2-ones of the formula: ##STR1## wherein R is hydrogen, halogen, lower alkyl, lower alkoxy, or trifluoromethyl; R.sup.1 is lower alkyl, alkylphenyl, cycloalkyl, or aryl; and R.sup.2 is hydrogen, lower alkyl or benzyl is provided. The compounds are useful as intermediates in the preparation of 2-amino-3-acylphenylacetic acid compounds which possess pharmaceutical properties.Type: GrantFiled: February 16, 1979Date of Patent: September 9, 1980Assignee: A. H. Robins Company, Inc.Inventors: Young S. Lo, David A. Walsh, William J. Welstead, Jr.
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Patent number: 4182774Abstract: Novel 2-amino-3-(5- and 6-)benzoylphenylacetic acids, esters and metal salts of the formula: ##STR1## wherein R is hydrogen or lower alkyl, R.sup.1 is hydrogen, lower-alkyl, sodium or potassium, R.sup.2 is hydrogen, halogen or lower alkoxy, X is hydrogen, lower alkyl, halogen, nitro or trifluoromethyl, Y is hydrogen, lower alkyl, halogen, nitro or trifluoromethyl, and Am is primary amino (--NH.sub.2) methylamino or dimethylamino. The compounds are prepared by hydrolysis of 4-(5- and 7-)benzoylindolin-2-ones to give the 2-amino-3-(5- and 6-)benzoylphenylacetic acids wherein amino is primary amino. The free acids are converted to the esters and metal salts. The calcium and magnesium salts are disclosed and are within the scope of the present invention. The compounds inhibit blood platelet aggregation.Type: GrantFiled: February 17, 1978Date of Patent: January 8, 1980Assignee: A. H. Robins Company, IncorporatedInventors: William J. Welstead, Jr., Henry W. Moran
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Patent number: 4151282Abstract: Methods for using 5,6-dihydro-4H-pyrrolo[3,2,1-ij]quinoline-1,2-dione and pharmaceutical compositions thereof in preventing diabetic complications are disclosed.Type: GrantFiled: December 29, 1977Date of Patent: April 24, 1979Assignee: A. H. Robins Company, Inc.Inventors: William J. Welstead, Jr., Warren N. Dannenburg
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Patent number: 4151285Abstract: 1,5-Disubstituted-1,2-dihydro-2H-1,4-benzodiazepin-2-ones of the formula ##STR1## wherein R is hydrogen or fluoro, R.sup.1 is hydrogen, fluoro chloro, bromo or trifluoromethyl, and n is 2 to 4, having anticonvulsant activity and useful as anti-anxiety agents, are disclosed.Type: GrantFiled: May 12, 1978Date of Patent: April 24, 1979Assignee: A. H. Robins Company, Inc.Inventors: William J. Welstead, Jr., Robert F. Boswell, Jr.
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Patent number: 4143150Abstract: Oxanilic acid derivatives having the formula: ##STR1## are disclosed wherein R is lower-alkyl, cycloalkyl, phenylalkyl or phenyl; R.sup.1 is hydrogen, lower-alkyl or phenyl; R.sup.2 is hydrogen, lower-alkyl, or lower-alkoxy; R.sup.3 is hydrogen, fluoro, chloro or bromo; X is oxygen or sulfur; and M is hydrogen, lower-alkyl or a physiologically acceptable cation. The compounds are useful for ameliorating and controlling symptoms associated with asthma.Type: GrantFiled: August 19, 1977Date of Patent: March 6, 1979Assignee: A. H. Robins Company, Inc.Inventors: William J. Welstead, Jr., Albert D. Cale, Jr.
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Patent number: 4126635Abstract: Novel 2-amino-3-(5- and 6-)benzoylphenylacetic acids, esters and metal salts of the formula: ##STR1## wherein R is hydrogen or lower alkyl, R.sup.1 is hydrogen, lower-alkyl, sodium or potassium, R.sup.2 is hydrogen, halogen or lower alkoxy, X is hydrogen, lower alkyl, halogen, nitro or trifluoromethyl, Y is hydrogen, lower alkyl, halogen, nitro or trifluoromethyl, and Am is primary amino (--NH.sub.2) methylamino or dimethylamino. The compounds are prepared by hydrolysis of 4-(5- and 7-)benzoylindolin-2-ones to give the 2-amino-3-(5- and 6-)benzoylphenylacetic acids wherein amino is primary amino. The free acids are converted to the esters and metal salts. The calcium and magnesium salts are disclosed and are within the scope of the present invention. The compounds have anti-inflammatory activity, are effective in lowering the cholesterol levels in hyperlipemic rats and inhibit blood platelet aggregation.Type: GrantFiled: April 15, 1977Date of Patent: November 21, 1978Assignee: A. H. Robins Company, IncorporatedInventors: William J. Welstead, Jr., Henry W. Moran
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Patent number: 4045576Abstract: Novel 2-amino-3-(5- and 6-)benzoylphenylacetic acids, esters and metal salts of the formula: ##STR1## wherein R is hydrogen or lower alkyl, R.sup.1 is hydrogen, lower-alkyl, sodium or potassium, R.sup.2 is hydrogen, halogen or lower alkoxy, X is hydrogen, lower alkyl, halogen, nitro or trifluoromethyl, Y is hydrogen, lower alkyl, halogen, nitro or trifluoromethyl, and Am is primary amino (--NH.sub.2) methylamino or dimethylamino. The compounds are prepared by hydrolysis of 4-(5- and 7-)benzoylindolin-2-ones to give the 2-amino-3-(5- and 6-)benzoylphenylacetic acids wherein amino is primary amino. The free acids are converted to the esters and metal salts. The calcium and magnesium salts are disclosed and are within the scope of the present invention. The compounds have anti-inflammatory activity, are effective in lowering the cholesterol levels in hyperlipemic rats and inhibit blood platelet aggregation.Type: GrantFiled: August 13, 1975Date of Patent: August 30, 1977Assignee: A. H. Robins Company, IncorporatedInventors: William J. Welstead, Jr., Henry W. Moran
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Patent number: 4021552Abstract: 10-[.omega.-(Benzoylpiperidinyl)alkyl]phenothiazines having the formula ##STR1## wherein R is hydrogen, chloro, bromo, trifluoromethyl, lower alkoxy, acetyl, sulfamoyl, or dimethylsulfamoyl, R.sup.1 is hydrogen, chloro, bromo, fluoro, trifluoromethyl, lower alkyl or lower alkoxy and n is 2, 3 or 4 are disclosed. Methods for the preparation of the compounds are described. The compounds possess tranquilizing activity and are useful as tranquilizing agents in mammals.Type: GrantFiled: April 20, 1976Date of Patent: May 3, 1977Assignee: A. H. Robins Company, IncorporatedInventors: William J. Welstead, Jr., Robert F. Boswell, Jr.
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Patent number: RE28973Abstract: 3-(OMEGA-SUBSTITUTED ALKYL)-INDOLES ARE DISCLOSED WHICH ARE USEFUL IN AMELIORATING THE TREMORS OF Parkinsonism. The compounds are prepared by metal hydride reduction of the precursor indole glyoxyloyl compounds.Type: GrantFiled: June 13, 1975Date of Patent: September 21, 1976Assignee: A. H. Robins Company, IncorporatedInventor: William J. Welstead, Jr.