Abstract: 2-[3-[4-(3-Halophenyl)-1-piperazinyl]propyl]-5-(1-hydroxyethyl)-2,4-dihydro -[4-phenoxyalkyl-3H-1,2,4-triazol-3-ones and closely related compounds are psychotropic agents having promise as antidepressants by virtue of their receptor site binding affinity profiles and animal pharmacology.
Type:
Grant
Filed:
September 30, 1983
Date of Patent:
September 23, 1986
Assignee:
Mead Johnson & Company
Inventors:
Richard E. Gammans, David W. Smith, Joseph P. Yevich
Abstract: Disubstituted N,N-piperazinyl derivatives are disclosed wherein one substituent is a pyrimidin-2-yl ring and the other is a 4 carbon chain attached to a p-fluorophenyl ring at the terminal carbon. The terminal carbon of this butylene chain is also bonded to an oxygen atom as part of a carbonyl, carbinol, or ketal functionality. These compounds possess psychotropic properties, particularly atypical antipsychotic activity of good duration. By virtue of pre-clinical pharmacological testing, these compounds appear useful as potential antipsychotic agents which lack the typical movement disorder side-effects of standard antipsychotic agents.
Type:
Grant
Filed:
December 18, 1984
Date of Patent:
August 12, 1986
Assignee:
Bristol-Myers Company
Inventors:
Joseph P. Yevich, Walter G. Lobeck, Jr.
Abstract: Novel phthalimide intermediates are reduced to 5-sulfamoyl-6-halo-3-oxoisoindole compounds bearing a substituted 1-phenylalkyl-4-piperidinyl moiety as the isoindole N-substitutent. Preferred compounds such as 6-chloro-2,3-dihydro-3-oxo-2-[1-(phenylmethyl)-4-piperidinyl]-1H-isoindole -5-sulfonamide exhibit diuretic and antihypertensive properties.
Abstract: An improved process for the preparation of 5-ethyl-4-(2-phenoxyethyl)-1,2,4-triazolone, a useful intermediate in the synthesis of antidepressant 1,2,4-triazolones typified by 2-[3-[4-(3-chlorophenyl)-1-piperazinyl]propyl]-5-ethyl-4-(2-phenoxethyl)-2 H-1,2,4-triazol-3(4H)-one, also known as nefazodone. The improved process is shorter and higher in yield than the former process, and the starting materials are cheap and readily available.
Abstract: A series of non-opiate analgesics of Formula I ##STR1## wherein R.sup.1 is hydrogen, alkyl, aralkyl, or aryloxyalkyl; R.sup.2 is alkyl or hydrogen; and R.sup.3 and R.sup.4 are independently selected from hydrogen, alkyl, acyloxy, alkoxy, alkylthio, halogen, hydroxyl, or trifluoromethyl; or a pharmaceutically acceptable acid addition salt.
Abstract: An overcap for an antineoplastic drug container includes a cylindrical airlock with a depth to diameter ratio preferably less than 1:1, elasticity and inner surface construction to provide pressure against the container closure to seal against leakage, a beveled continuous annular locking flange, and an upstanding annular bead defining a target area for hypodermic needle insertion.
Abstract: Phenoxyalkyl 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:
September 28, 1984
Date of Patent:
March 11, 1986
Assignee:
Mead Johnson & Company
Inventors:
Davis L. Temple, Jr., Walter G. Lobeck, Jr.
Abstract: Non-disintegrating theophylline tablets having a pair of opposing substantially planar surfaces and a very thin cross-section have a high bioavailability on ingestion and a relatively steady release rate permitting a 12 hr. dosing interval for maintenance of non-toxic therapeutic blood theophylline concentrations. Excipients or tableting aids are not required, but trace amounts of a tableting lubricant are preferably included to facilitate continuous large scale production.
Type:
Grant
Filed:
June 4, 1984
Date of Patent:
October 15, 1985
Assignee:
Mead Johnson & Company
Inventors:
Stephen T. David, Dana Brooke, Claude E. Gallian
Abstract: A lyophilized pharmaceutical solid composition containing cyclophosphamide for reconstitution with water to provide a solution for oral or parenteral administration. This lyophilized cyclophosphamide solid composition demonstrates improved stability, solubility characteristics and enhanced appearance compared with currently available dry powder pre-mix compositions of cyclophosphamide. The lyophilized solid composition contains about 20 parts by weight of cyclophosphamide, about 11/4-2 parts by weight of water and from about 10-85 parts by weight of excipient which is comprised mainly of mannitol. Processes for making the composition are disclosed.
Type:
Grant
Filed:
March 13, 1984
Date of Patent:
August 27, 1985
Assignee:
Mead Johnson & Company
Inventors:
Robert L. Alexander, Robert J. Bequette, Terry T. Kensler, Joseph A. Scott
Abstract: Disubstituted N,N'-piperazinyl derivatives are disclosed wherein one substituent is heteroaryl and the other is alkylene attached to the ring nitrogen of substituted 2,5-pyrrolidinedion-1-yl moieties. The substitution pattern of the pyrrolidinedione ring involves either geminal disubstitution, including spiro ring fusion, or 3,4-phenyl ring fusion to give phthalimide derivatives. Heteroaryl substitution on the other piperazine nitrogen comprises pyridine, pyrimidine, and benzisothiazole ring systems. Representative examples of these compounds demonstrate useful central nervous system effects.
Abstract: 1-(4-Pyrimidinyloxy)-3-(hetarylalkylamino)-2-propanols are cardiovascular agents having a range of vasodilator and adrenergic beta-receptor blocking activities making these compounds useful anti-hypertensive agents. Preferred compounds bear a hydrazino or hydrazono substituent in the 2- position of the pyrimidine ring.
Type:
Grant
Filed:
May 9, 1983
Date of Patent:
May 14, 1985
Assignee:
Mead Johnson & Company
Inventors:
John E. Lawson, William L. Matier, Herbert R. Roth
Abstract: An improved tubing connector with a connecting tip designed to adapt all sizes of tubing commonly employed in nasogastric and gastrostomy feeding. This tubing connector comprises a one-piece hollow unit having at one end a smooth tapered sleeve with an outer concentric shielding member which end serves as means for permanent attachment to a standard sized supply tube such as an out-dwelling tube attached to a reservoir; and at the other end, representing the adaptable connecting tip, an outwardly flared portion where the flaring is accomplished first by smooth taper in the tip end area and then by multiple tapered flanges of increasing diameter as distance from the tip end lengthens. This novel embodiment of adaptable connecting tip features permits a secure fit regardless of tubing size, but with ease of connection and disconnection. These characteristics are highly desirable for use with in-dwelling surgical tubing which requires delicate manipulation.
Abstract: The invention provides 3-oxoisoindole compounds useful as diuretics of the general formula ##STR1## wherein X is halogen or trifluoromethyl, A is alkylene (C.sub.2 -C.sub.4), R.sub.1 is alkyl, R.sub.2 is alkyl or phenylalkyl, or R.sub.1 and R.sub.2 taken together with nitrogen are piperidino, morpholino or pyridinyl.
Abstract: A nutritionally complete ready-to-use liquid diet for providing total patient nourishment. This diet contains a source of protein equivalent comprised of free amino acids and small peptides; a carbohydrate source comprised of maltodextrin with a dextrose equivalent between 7 and 24 and a smaller amount of modified corn starch; a lipid component; nutritionally significant amounts of all essential vitamins and minerals; and stabilizers; all in an acidic aqueous emulsion which can be sterilized.
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:
December 3, 1981
Date of Patent:
January 22, 1985
Assignee:
Mead Johnson & Company
Inventors:
William E. Kreighbaum, William T. Comer
Abstract: Novel phthalimide intermediates are reduced to 5-sulfamoyl-6-halo-3-oxoisoindole compounds bearing a substituted 1-phenylalkyl-4-piperidinyl moiety as the isoindole N-substituent. Preferred compounds such as 6-chloro-2,3-dihydro-3-oxo-2-[1-(phenylmethyl)-4-piperidinyl]-1H-isoindole -5-sulfonamide exhibit diuretic and antihypertensive properties.
Abstract: 6-(1H-Tetrazol-5-yl)thiazolo[3,2-a]pyrimidin-5-ones, 3-(1H-tetrazol-5-yl)-4H-pyrimido[2,1-b]benzothiazol-4-ones, and the corresponding imidazo- and triazolo- pyrimidines, thiones, and imines are useful as antiallergy and antiasthmatic compounds by virtue of their inhibitory action on the immediate hypersensitivity reaction in mammals and relaxant action on the tracheal muscle. Intermediates in the synthesis of these substances from 2-aminoazoles and ethoxymethylene malononitrile also have smooth muscle relaxant and immediate hypersensitivity reaction inhibitory activity.
Type:
Grant
Filed:
July 11, 1980
Date of Patent:
January 1, 1985
Assignee:
Mead Johnson & Company
Inventors:
Robert R. Covington, Davis L. Temple, Jr., Joseph P. Yevich
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: Phenoxyalkyl substituted-1,2,4-triazolones having anti-depressant 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:
June 29, 1983
Date of Patent:
December 11, 1984
Assignee:
Mead Johnson & Company
Inventors:
Davis L. Temple, Jr., Walter G. Lobeck, Jr.