Abstract: N.sup.6 -2-hydroxypropylaryl-substituted adenosines and adenines represented by the formula ##STR1## wherein R.sub.1 is selected from the group consisting of naphthyl, phenyl, substituted phenyl or biphenyl; and R.sub.2 is hydrogen or 1-.beta.-ribosyl; and the pharmaceutically acceptable salts thereof. The compounds are anti-hypertensive agents.
Type:
Grant
Filed:
June 9, 1980
Date of Patent:
June 14, 1983
Assignee:
G.D. Searle & Co.
Inventors:
Robert W. Hamilton, Richard E. L. Henderson, Barnett S. Pitzele
Abstract: Hydroxy-substituted phosphoranes and salts thereof represented by Formulae I and II ##STR1## wherein R.sub.1, R.sub.2 and R.sub.3 are the same or different members of the group consisting of lower alkyl, C.sub.5 -C.sub.6 cycloalkyl, and ##STR2## wherein q is an integer from 0 to 4 and Y is selected from the group consisting of hydrogen, halogen, lower alkyl and lower alkoxy; R.sub.4 can be hydrogen or C.sub.1 -C.sub.3 straight or branched chain alkyl; the sum of n+m=3-5; R.sub.5 is hydrogen or lower alkyl; R.sub.6 and R.sub.7 are the same or different members of the group consisting of hydrogen, lower alkyl, and ##STR3## p is an integer of 0 or 1; and X is an anion. The compounds are useful as intermediates for the heterocyclic phosphonium salts disclosed and claimed in U.S. Pat. No. 4,075,407. An improved process for preparing the phosphonium salts of U.S. Pat. No. 4,075,407 is also provided by the present invention.
Abstract: 11-Amino-11-deoxydaunorubicin and analogs represented by the formula: ##STR1## wherein: R is hydrogen, hydroxy or methoxy; R.sub.1 is hydrogen or hydroxy; and the pharmaceutically acceptable salts thereof.The compounds are useful in ameliorating tumor growth.
Type:
Grant
Filed:
April 2, 1980
Date of Patent:
September 7, 1982
Assignee:
G.D. Searle & Co.
Inventors:
Robert B. Garland, Raphael Pappo, Paul B. Sollman
Abstract: Derivatives of .alpha.,.beta.-unsaturated ketones having anticonvulsant activity and methods of their preparation from heterocyclic phosphonium salts and acyclic phosphoranes are disclosed.
Abstract: 1-Cycloalkyl phosphonium salts represented by the formula ##STR1## wherein: R is selected from the group consisting of lower alkyl, hydroxy lower alkyl, halo lower alkyl, amino lower alkyl, cyano lower alkyl, lower alkenyl with the limitation that the double bond is not on the carbon atom attached to the oxygen atom, benzyl, substituted benzyl and ##STR2## wherein q is 0 or 1 and R.sub.4 is selected from the group consisting of hydroxy, loweralkoxy, phenyl, substituted phenyl, and ##STR3## wherein R.sub.5 and R.sub.6 are the same or different members of the group consisting of hydrogen and loweralkyl or taken together form a 5 or 6 membered ring; m is 1, 2 or 3; n is 0 or 1; o is 0 or 1; p is 0 or 1; R.sub.1, R.sub.2 and R.sub.3 are the same or different members of the group consisting of hydrogen, lower alkyl, lower alkoxy and halo; and X is a pharmaceutically acceptable anion. The compounds are useful as analgesic agents.
Abstract: The present invention provides a trans-dermal delivery pad for nitroglycerin administration, specifically a microsealed, trans-dermal nitroglycerin pad having a backing which is impervious to nitroglycerin absorption and transport and a silicon matrix affixed thereto, said silicone polymer matrix being of cross-linked silicone rubber having from about 10 to 200 micron microsealed compartments being formed by in situ cross-linking of the silicone rubber after it is mixed with a hydrophilic solvent system containing the nitroglycerin and a hydrophobic solvent which enhances nitroglycerin dispersion and transport.
Type:
Grant
Filed:
May 4, 1981
Date of Patent:
June 22, 1982
Assignee:
G. D. Searle & Co.
Inventors:
Dilip R. Sanvordeker, James G. Cooney, Ronald C. Wester
Abstract: 7-[5-oxo-3-hydroxy-2-(3-substituted)-3-hydroxypropyl)-1-cyclopentene]-hepta noic acids having the following general formula ##STR1## wherein X is oxygen or hydroxyl, R.sub.1 and R.sub.3 are independently hydrogen or methyl, and R.sub.2 is --(CH.sub.2)n-Y where n is an integer from 0 through 4 inclusive, and Y is phenyl, or a cycloalkyl group having 4 to 6 carbon atoms. Said acids as well as certain derivatives thereof are useful as nasal decongestants, inhibitors of gastric secretion, inhibitors of platelet aggregation, blood additives, smooth muscle stimulators, hypotensive agents, labor inducers, and in controlling ovulation.
Abstract: Method of determining the quality of fish prior to processing and packaging thereof which comprises measuring the quantitative distribution of trimethylamine in the fish and more particularly, the extent of migration of trimethylamine from dark to light meat in the fish.
Abstract: A stable solid dosage form of the compound .+-.methyl(7-[3(.alpha.)-hydroxy-2-.beta.-(4(RS)-4-hydroxy-4-methyl-trans- 1-octen-1-yl)-oxycyclopent-1.alpha.-yl]heptanoate, said solid dosage form comprising from about 50 to about 500 parts of a polymer selected from the group consisting of hydroxypropylmethyl cellulose and polyvinylpyrolidone per part of said compound.
Abstract: 25-Alkylcholest-5-ene-3.beta.,22-diols and esters thereof adapted to inhibit the activity of 3-hydroxy-3-methylglutaryl coenzyme A reductase are disclosed.
Abstract: Phosphonium salts represented by the formula ##STR1## wherein: R is selected from the group consisting of lower alkyl, phenyl, substituted phenyl, benzyl and substituted benzyl; R.sub.1 is hydrogen or lower alkyl; R.sub.2 is hydrogen or loweralkyl; or R.sub.1 and R.sub.2 taken together form a 5 or 6 membered saturated or unsaturated carbocyclic ring with the limitation that R.sub.1 is on the carbon atom adjacent the carbon atom bearing R.sub.2, m is 1,2 or 3; n is 0 or 1; o is 0 or 1; p is 0 or 1; R.sub.3, R.sub.4 and R.sub.5 are the same or different members of the group consisting of hydrogen, lower alkyl, lower alkoxy and halo; R.sub.6 is hydrogen or C.sub.1 --C.sub.3 straight or branched chain alkyl; and X is a pharmaceutically acceptable anion. Compounds wherein R is phenyl, substituted phenyl, benzyl or substituted benzyl are narcotic antagonists. Compounds wherein R.sub.1 and R.sub.2 are hydrogen or lower alkyl when R is lower alkyl are mixed agonist/antagonist analgesic agents and compounds where R.
Abstract: A new, hybrid carnation, distinguished by its profuse production of Tyrian Purple flowers of medium size, each petal of which is bordered with a ruffled margin of a light color, approaching white, the flowers being borne singly on strong, upright pedicels, which are carried on sturdy, upright peduncles about 45-60 cm. long.
Abstract: A new and distinct carnation cultivar characterized by its profuse production of generally white flowers having deeply indented margins. The petals exhibits a slightly yellow coloration at the level of the claw of the petals, and their margins are deeply indented.
Abstract: A new variety of carnation of the closed calyx or non-splitting type, characterized by a vigorous growth and precocious blooming habit of very large flowers having dark red and violet coloration of its petals which are bordered by white margins.
Abstract: A new and distinct lily cultivar of the Oriental hybrid type characterized by its very large, somewhat upward facing, oval shaped flowers with an unusual and distinctive color pattern, the midrib of each flower tepal being colored a rich red-purple color which suffuses outwardly through a light pink to a pure white margin, each tepal being copiously marked on each side of the midrib with maculae of red-purple color over the middle 12 cm. of each tepal.
Abstract: A new and distinct lily cultivar of the Oriental hybrid type particularly characterized by its very short stature and its relatively large bowl-shaped flowers of rich magenta-rose coloration borne as a compact raceme, and by its deep rose pink bud coloration before the flowers open, the compact inflorescence being borne on an unusually short peduncle.
Abstract: A new and distinct lily cultivar of the Oriental hybrid type characterized by its short stature and silhouette and a compact raceme of large, light pink flowers of good form and substance, with abundant foliage, the plant also having a sturdy and vigorous growth habit and being capable of forced out-of-season production with reliable performance.