Abstract: Proteinaceous medicaments such as erythropoetin, insulin and calcitonin are formulated in a medium comprising a polyol pharmaceutical solvent combined as co-solvent with a lipid pharmaceutical solvent. The formulation is adapted for oral administration as a liquid as well as a filled hard or soft gelatin capsule. The preferred polyol solvent is polyethylene glycol/propylene glycol; the preferred lipid solvent is oleic acid.
Abstract: Pharmaceutically elegant oral compositions of non-steroidal anti-inflammatory drugs or their salts are prepared by adding selected dispersing agents such as a polyvinylpyrrolidone, hydroxypropyl-methylcellulose or hydroxypropylcellulose to the NSAIDs in a medium of polyol-glycol-alcohol. The compositions offer the formation of finely dispersed active ingredients upon dispersion in gastric juice.
Abstract: A sucralfate-like chemical compound which is free flowing but turns viscid upon contact with acid or non-acid aqueous liquid. The compound is prepared by adding an excess of aluminum chlorohydrate to sucrose octaammonium sulfate in aqueous alcohols.
Abstract: A one phase, liquid composition for oral administration comprises a NSAID such as an anthranilic acid derivative plus a di- or triglyceride of a medium chain fatty acid edible oil which has the characteristics of a pharmaceutical solvent carrier as known to those skilled in the art. Other pharmaceutical additives may be optionally added. An additional stipulation is that ethanol or other monohydric alcohol solvents should not be present.
Abstract: A one phase, liquid composition for oral administration comprises a NSAID such as an indoleacetic acid derivative or a pyrroleacetic acid derivative plus a di- or triglyceride of a medium chain fatty acid edible oil which has the characteristics of a pharmaceutical solvent carrier as known to those skilled in the art. Other pharmaceutical additives may be optionally added. An additional stipulation is that ethanol or other monohydric alcohol solvents should not be present.
Abstract: A pharmaceutically elegant, one phase, liquid composition for oral administration comprises a NSAID such as ibuprofen plus a di- or triglyceride of a medium chain fatty acid edible oil which has the characteristics of a pharmaceutical solvent carrier as known to those skilled in the art. Other pharmaceutical additives may be optionally added. An additional stipulation is that ethanol or other monohydric alcohol solvents should not be present.
Abstract: Pharmaceutically elegant oral liquid compositions of sulindac are prepared using calcium sulindac in a vehicle comprising a glycol, a polyol, optional ethanol and pharmaceutical additives.
Abstract: Selected pyridylalkylhydrazides are used as active ingredients in animal feed compositions and in methods for increasing the growth and feed efficiency of monogastric, meat-producing animals. A particularly useful active ingredient of this invention is 3-azabicyclo-[3.2.2]nonane-3-carbothioic acid 2-[1-(2-pyridyl)ethyl]-hydrazide.
Type:
Grant
Filed:
March 12, 1985
Date of Patent:
May 26, 1987
Assignee:
SmithKline Beckman Corporation
Inventors:
Alfred W. Chow, Thomas O. Lindsey, Winfred J. Sanders
Abstract: Certain vasopressin-like peptides, which have an acyclic unit at position 1 and which have an .omega.-amino- or guanidinoalkyl substituent attached to the cysteine in the 6-position of the ring, have V.sub.1 -vasopressin and oxytocin antagonist activity. A species of this series of new compounds is [1-desaminopenicillamine-2-(O-ethyl-D-tyrosine)-8-(1,4-diaminobutane)-9-de sglycinamide]-vasopressin.
Type:
Grant
Filed:
April 16, 1986
Date of Patent:
April 14, 1987
Assignee:
SmithKline Beckman Corporation
Inventors:
James F. Callahan, William F. Huffman, Michael L. Moore, Nelson C. Yim
Abstract: The preparation of [1-(.beta.-mercapto-.beta.,.beta.-cyclopentamethylenepropionic acid)-2-(O-ethyl-D-tyrosine)-4-valine-8-arginine-9-desglycine]vasopressin by oxidation of the corresponding dimercaptan is improved by using a copper II salt.
Abstract: Certain new vasopressin-like peptides which have structures characterized by having a bisaminoalkylbenzene present in the vasopressin tail at the 7- or 8-position retain vasopressin antagonist activity. A species of the invention is [1-.beta.-mercapto-.beta.,.beta.-cyclopentamethylenepropionic acid)-2-(O-ethyl)-D-tyrosine-4-valine-8-1',4'-bis(aminomethyl)benzene-9-de sglycinamide]-vasopressin.
Type:
Grant
Filed:
March 20, 1985
Date of Patent:
November 25, 1986
Assignee:
SmithKline Beckman Corporation
Inventors:
James F. Callahan, Michael L. Moore, Nelson C. Yim
Abstract: Certain vasopressin-like peptides, which have an acyclic unit at position 1 and which have an .omega.-amino- or guanidinoalkyl substituent attached to the cysteine in the 6-position of the ring, have V.sub.1 -vasopressin and oxytocin antagonist activity. A species of this series of new compounds is [1-desaminopenicillamine-2-(O-ethyl-D-tyrosine)-8-(1,4-diaminobutane)-9-de sglycinamide]-vasopressin.
Type:
Grant
Filed:
November 21, 1984
Date of Patent:
August 5, 1986
Assignee:
SmithKline Beckman Corporation
Inventors:
James F. Callahan, William F. Huffman, Michael L. Moore, Nelson C. Yim
Abstract: Vasopressin derivatives having V.sub.1 and oxytocin antagonist activity whose structures are characterized by a Mpa unit at position 1 and a des-Pro unit at position 7 are prepared by standard peptide synthetic methods also using an oxidative cyclization of a dimercaptan. Representative species are [1-deaminopenicillamine-2-(O-methyl)-tyrosine-7-desproline-8-arginine-9-de sglycine]vasopressin or [1-.beta.-mercaptopropionic acid-2-D-(O-ethyl)tyrosine-3-isoleucine-4-threonine-7-desproline-8-arginin e-9-desglycine]-vasopressin.
Abstract: 2- or 3-.beta.-Indolylalanyl and .beta.-indolylglycyl vasopressins are prepared by standard peptide synthetic methods. These 2- or 3-TRP vasopressins have vasopressin antagonist activity.
Abstract: A series of pharmaceutical compositions which contain 4-aminoalkyl-2(3H)-indolones has been demonstrated to have D.sub.2 -agonist activity useful for treating congestive heart failure and hypertension. A representative ingredient of the compositions is 4-di-n-propylaminoethyl-2(3H)-indolone or a salt thereof.
Abstract: Flukicidal N-[4-(1-phenylethenyl)phenyl]-2-hydroxy-3,5-dihalobenzamides are prepared by reacting a halosalicylic acid with a 1-(4-aminophenyl)-1-phenylethylene in the presence of a halo condensing agent. A species of the invention is N-[4-(1-phenylethenyl)phenyl]-2-hydroxy-3,5-diiodobenzamide.
Type:
Grant
Filed:
May 7, 1984
Date of Patent:
May 6, 1986
Assignee:
SmithKline Beckman Corporation
Inventors:
Alfred W. Chow, Vassilios J. Theodorides
Abstract: Certain octapeptides, which have structures characterized by being a six unit cyclic peptide ring with a dipeptide tail which lacks a glycine unit at position 9, have potent vasopressin antagonist activity. The compounds here claimed are in general characterized by having an amino acid unit at position 4 which is other than valine. An important species of the group is [1-(.beta.-mercapto-.beta.,.beta.-cyclopentamethylenepropionic acid)-2-(O-ethyl-D-tyrosine)-4-.alpha.-aminobutyric acid-8-arginine-9-desglycine]vasopressin.
Abstract: New intermediates and processes for preparing 6-halo-7,8-dihydroxy-1-(p-hydroxyphenyl)-2,3,4,5-tetrahydro-1H-3-benzazepi nes involve the reaction of a p-methoxyphenylglyoxal, lower alkyl hemimercaptal with a 2-chloro-3,4-dimethoxyphenethylamine, followed by a borohydride reduction.
Abstract: A device for effecting the delayed release of an active ingredient comprises a container and, within, a dispersible unit of ingredient, a removable closure and a electrical control circuit for removal of said closure at a designated time to release the active ingredient. Several assemblies are combined to control the administration of veterinary medicaments to ruminant animals as a specific application of the invention.
Abstract: Certain aminoethyl substituted 1,3-benzthiazol- and 1,3-benzoxazol-2(3H)-ones are D.sub.2 -dopamine agonists. These compounds are prepared by reacting an appropriate o-aminophenol or thiophenol with phosgene.