Abstract: Piperazinyl derivatives containing a 3-alkylene-2,4-thiazolidinedione heterocyclic component with relatively selective psychotropic properties are disclosed. The compound 3-[4-[4-(2-pyrimidinyl)-1-piperazinyl]butyl]-2,4-thiazolidinedione which has selective anxiolytic activity constitutes a typical embodiment of the invention.
Type:
Grant
Filed:
August 3, 1981
Date of Patent:
January 4, 1983
Assignee:
Mead Johnson & Company
Inventors:
Davis L. Temple, Jr., Richard E. Yeager
Abstract: Imidazopyrimidinones and other diazaheterocyclopyrimidinones having an additional fused imidazole or triazole ring have utility as bronchodilators, mediator release inhibitors, phosphodiesterase inhibitors, and peripheral vasodilators. They are orally active and useful in the prophylaxis and treatment of asthma. A preferred compound is 4-[(4-chlorophenyl)methyl]-6,7-dihydro-3H-imidazo[1,2-a]purin-9(4H)-one.
Abstract: 1-[4-(4,4-Dialkyl-2,6-piperidinedion-1-yl)butyl]piperazines with 2-2-(3-cyano)pyridyl substituents in the 4- position have been synthesized and demonstrate useful psychotropic properties.
Type:
Grant
Filed:
December 28, 1981
Date of Patent:
November 30, 1982
Assignee:
Mead Johnson & Company
Inventors:
Davis L. Temple, Jr., Joseph P. Yevich, Walter G. Lobeck, Jr.
Abstract: Novel spiro-quaternary ammonium halides are disclosed. The new compounds are particularly valuable as intermediates in preparation of N-(2-pyrimidinyl)piperazinylalkyl derivatives of azaspiroalkanediones such as the psychopharmacologic agent 8-[4-[4-(2-pyrimidinyl)-1-piperazinyl]butyl]-8-azaspiro[4.5]decane-7,9-dio ne.
Type:
Grant
Filed:
October 16, 1980
Date of Patent:
September 28, 1982
Assignee:
Mead Johnson & Company
Inventors:
Jack C. Simms, deceased, Old National Bank in Evansville, administrator
Abstract: 4-Ethyl-6-methoxy-7-(oxiranylmethoxy)quinazoline and its isomer 4-ethyl-7-methoxy-6-(oxiranylmethoxy)quinazoline have potent anti-tumor activity in animals.
Type:
Grant
Filed:
March 6, 1981
Date of Patent:
August 10, 1982
Assignee:
Mead Johnson & Company
Inventors:
William E. Kreighbaum, William T. Comer
Abstract: Phenoxyethyl substituted-1,2,4,-triazolones having antidepressant properties typified by 2-[3-[4-(3-chlorophenyl)-1-piperazinyl]propyl]-5-ethyl-4-(2-phenoxyethyl)- 2H-1,2,4-triazol-3(4H)-one are disclosed.
Type:
Grant
Filed:
March 16, 1981
Date of Patent:
July 6, 1982
Assignee:
Mead Johnson & Company
Inventors:
Davis L. Temple, Jr., Walter G. Lobeck, Jr.
Abstract: Indanyloxy compounds having 2-alkynyl substituents which exhibit diuretic, saluretic, and uricosuric activity are described. The compounds are obtained according to a process involving selective etherification of a 5-hydroxyindanone followed by alkynylation with a silylated alkynyl bromide to provide novel silylated intermediates which are hydrolyzed to indanyloxy compounds such as (6,7-dichloro-1-oxo-2-phenyl-2-propargyl-5-indanyloxy)acetic acid.
Abstract: 4-Hydroxy-3-methoxy-N-[2-[2-(1-methyl-2-piperidinyl)ethyl]-phenyl]benzamide is an antiarrhythmic agent having relatively low toxicity and increased duration of action.
Abstract: A bran tablet unit dosage form composition employing comminuted bran useful as a bulk cathartic agent is provided. The bran tablet compositions have suitable characteristics with respect to handling and packaging procedures and are substantially more palatable than whole bran.
Type:
Grant
Filed:
April 2, 1975
Date of Patent:
May 4, 1982
Assignee:
Mead Johnson & Company
Inventors:
John L. Gabby, Gerald K. Ashby, Dennis W. Cameron, Richard C. Theuer
Abstract: 2-[2-[2-[(4-Methoxybenzoyl)amino]phenyl]ethyl]-1-methyl-1-alkylpiperidinium halides and 2-[2-[2-[(4-methoxybenzoyl)amino]phenyl]ethyl]-1-methyl-1-benzylpiperidini um halides are antiarrhythmic agents having reduced toxicity relative to the corresponding piperidine compound.
Abstract: Substituted 1-phenoxy-3-(thienyl-tert.-butylamino)-2-propanols and related 3-benzothienyl compounds are selective .beta.-receptor blocking agents. Preferred compounds bear an ortho-substituent on the phenoxy ring.
Type:
Grant
Filed:
May 7, 1981
Date of Patent:
March 23, 1982
Assignee:
Mead Johnson & Company
Inventors:
William L. Matier, William E. Kreighbaum
Abstract: N-[(4-Phenyl-1,2,3,6-tetrahydropyridin-1-yl)alkylene]azaspiroalkanediones having substituents in the phenyl ring have been synthesized and demonstrate useful tranquilizing properties. N-[(4-Hydroxy-4-phenylpiperidin-1-yl)alkylene]azaspiroalkanediones are intermediates in their synthesis.
Type:
Grant
Filed:
March 16, 1981
Date of Patent:
March 16, 1982
Assignee:
Mead Johnson & Company
Inventors:
Davis L. Temple, Jr., Joseph P. Yevich, Walter G. Lobeck, Jr.
Abstract: A reliable and sensitive immunoassay for encainide in biological fluids including a novel hapten required for antigen synthesis and an immunologically homologous labeled tracer is provided.
Abstract: 1-Aryloxy-3-[(3-indolyl)-tert.-butyl]amino-2-propanols having a heterocyclic aryl-attached substituent or aryl-fused heterocyclic ring are antihypertensive agents having vasodilator and adrenergic .beta.-receptor blocking action.
Type:
Grant
Filed:
February 13, 1979
Date of Patent:
February 9, 1982
Assignee:
Mead Johnson & Company
Inventors:
William E. Kreighbaum, William T. Comer
Abstract: 4-Methoxy-N-[2-[2-(1-methyl-2-piperidyl)ethyl]phenyl]-benzamide N-oxide is an antiarrhythmic agent having reduced toxicity and increased water solubility relative to the corresponding tertiary amine.
Abstract: Imidazopyrimidinones and other diazaheterocyclopyrimidinones having an additional fused imidazole or triazole ring have utility as bronchodilators, mediator release inhibitors, phosphodiesterase inhibitors, and peripheral vasodilators. They are orally active and useful in the prophylaxis and treatment of asthma. A preferred compound is 4-[(4-chlorophenyl)methyl]-6,7-dihydro-3H-imidazo[1,2-a]-purin-9(4H)-one.
Abstract: A series of 2,6-diamino-4-tertiary-amino-pyridine 1-oxides is disclosed. Substituents in the 4-position include diethylamino, pyrrolidinyl, piperidino, morpholino, thiomorpholino, and N-methylpiperazino. Novel oxadiazolones such as 5-amino-7-(1-piperidinyl)-2H-[1,2,4]oxadiazolo[2,3-a]pyridine-2-one which are useful in the preparation of the pyridine 1-oxides are also disclosed. The compounds of this invention lower blood pressure in normotensive and hypertensive mammals and are particularly useful in the treatment of hypertensive conditions in mammals. 2,6-Diamino-4-(1-piperidinyl)pyridine 1-oxide is a representative embodiment of the invention.
Abstract: The compounds are of the heterocyclic class of 2-phenethylpiperidines having an amido substituent in the ortho position of the phenethyl moiety. Substituents in the ortho position include formamido, benzamido, cinnamamido, 2-thiophenecarboxamido, alkanesulfonamido and alkanoylamido. They are useful as antiarrhythmic and/or antiserotonin agents. The novel compounds are prepared by reaction of appropriately substituted o-aminophenethylpiperidines and the carbonyl or sulfonyl halides or anhydrides. Typical embodiments of this invention are 4-methoxy-2'-[2-(1-methyl-2-piperidyl)ethyl]benzanilide and 2'-[2-(1-methyl-2-piperidyl)ethyl]cinnamanilide.
Abstract: The compounds are of the heterocyclic class of 2-phenethylpiperidines having an amido substituent in the ortho position of the phenethyl moiety. Substituents in the ortho position include formamido, benzamido, cinnamamido, 2-thiophenecarboxamido, alkanesulfonamido and alkanoylamido. They are useful as antiarrhythmic and/or antiserotonin agents. The novel compounds are prepared by reaction of appropriately substituted o-aminophenethylpiperidines and the carbonyl or sulfonyl halides or anhydrides. Typical embodiments of this invention are 4-methoxy-2'-[2-(1-methyl-2-piperidyl)ethyl]benzanilide and 2'-[2-(1-methyl-2-piperidyl)ethyl]cinnamanilide.