Abstract: The tetradecapeptide ##STR1## is described along with corresponding non-toxic pharmaceutically-acceptable acid addition salts as well as intermediates useful in the synthesis of the tetradecapeptide. This tetradecapeptide as well as its pharmaceutically-acceptable acid addition salts exhibit various activities including inhibition of the release of gastric acid and reduction of gut motility.
Abstract: The tetradecapeptides ##STR1## in which Y is L-Asn or L-Ala are described along with corresponding non-toxic pharmaceutically-acceptable acid addition salts as well as intermediates useful in the synthesis of the tetradecapeptides. These tetradecapeptides as well as their pharmaceutically-acceptable acid addition salts exhibit various activities including inhibition of the release of gastric acid.
Abstract: A novel 4-(2'-benzothiazolyldithio)-3-imidoazetidin-2-one of the formula ##STR1## in which X is chloro or bromo and R.sub.2 is methylene or oxygen is ring-closed to the corresponding 3-exomethylenecepham or 3-"oxo" cepham by treatment with sodium or potassium iodide at a temperature of from about 40.degree. C. to about 80.degree. C.
Abstract: The tetradecapeptides ##STR1## in which Y is L-Asn or L-Ala are described along with corresponding non-toxic pharmaceutically-acceptable acid addition salts as well as intermediates useful in the synthesis of the tetradecapeptides. These tetradecapeptides as well as their pharmaceutically-acceptable acid addition salts exhibit various activities including inhibition of the release of gastric acid.
Abstract: N-Chlorophthalimide is prepared by contacting an alkali metal salt of phthalimide with chlorine under substantially non-aqueous conditions in the presence of a halogenated aliphatic hydrocarbon and at a temperature of from about -10.degree. C. to about +40.degree. C.
Abstract: Dihydrobenzopyranoxanthenones of the formula ##STR1## are electrolytically reduced to their corresponding hexahydrobenzopyranoxanthenones at a mercury cathode in the presence of a proton source and in the presence of an electrolyte selected from the group consisting of alkali metal salts, quaternary ammonium salts having a total of about 10 to about 28 carbon atoms in the cation moiety, and tertiary amine salts having a total of about 7 to about 21 carbon atoms in the cation moiety.
Abstract: Compounds of the formula ##STR1## in which each R is hydrogen, C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy, hydroxy, cyano, or halo, and both R groups are identical and are symmetrically located; R.sub.1 is C.sub.1 -C.sub.3 alkyl and R.sub.2 is methyl, or R.sub.1 and R.sub.2 taken together are (CH.sub.2 --.sub.n in which n is an integer from 4 to 6; and (1) X.sub.c and X.sub.d are hydrogen, and the combination of X.sub.a and Y.sub.a and of X.sub.b and Y.sub.b each represents a double bond, subject to the limitation that, when R.sub.1 is C.sub.1 -C.sub.3 alkyl and is other than methyl, X.sub.c, X.sub.d, and R.sub.1 are all in an .alpha.-configuration; or (2) X.sub.a, X.sub.b, X.sub.c, X.sub.d, Y.sub.a, and Y.sub.b are hydrogen, subject to the limitation that both X.sub.c and X.sub.d are in an .alpha.-configuration, both X.sub.a and X.sub.b are in an .alpha.-configuration or in a .beta.-configuration, and, R.sub.1, when it is C.sub.1 -C.sub.3 alkyl, is in an .alpha.
Abstract: A penicillin sulfoxide ester is reacted with an N-chloro halogenating agent at a temperature of from about 75.degree. C. to about 135.degree. C. to produce a novel 2-chlorosulfinylazetidin-4-one intermediate. The intermediate can be treated with stannic chloride to produce a 3-exomethylenecepham sulfoxide.
Abstract: The tetradecapeptide ##STR1## is described along with corresponding non-toxic pharmaceutically-acceptable acid addition salts as well as intermediates useful in the synthesis of the tetradecapeptide. This tetradecapeptide as well as its pharmaceutically acceptable acid addition salts inhibit the release of growth hormone and the release of gastric acid.
Abstract: Derivatives of 2-aroyl-3-phenylindenes, 3-aroyl-4-phenyl-1,2-dihydronaphthalenes, and 1-phenyl-2-aroyl-naphthalenes are useful as antifertility agents.
Abstract: A penicillin sulfoxide ester is reacted with an N-chloro halogenating agent at a temperature of from about 75.degree. C. to about 135.degree. C. and in the presence of an alkylene oxide and calcium oxide to produce a 2-chlorosulfinylazetidin-4-one intermediate. The intermediate, upon separation from the alkylene oxide, calcium oxide, and any conversion products of both the alkylene oxide and calcium oxide, can be treated with stannic chloride to produce a 3-exomethylenecepham sulfoxide.
Abstract: The tetradecapeptide ##STR1## is described along with corresponding non-toxic pharmaceutically-acceptable acid addition salts as well as intermediates useful in the synthesis of the tetradecapeptide. This tetradecapeptide as well as its pharmaceutically acceptable acid addition salts inhibit the secretion of gastric acid.
Abstract: The tetradecapeptides ##STR1## in which Y is L-Cha, L-Leu, or D-Phe are described along with corresponding non-toxic pharmaceutically-acceptable acid addition salts as well as intermediates useful in the synthesis of the tetradecapeptides. These tetradecapeptides as well as their pharmaceutically-acceptable acid addition salts inhibit the release of growth hormone.
Abstract: The tetradecapeptides ##STR1## in which Y is Gly or D-Ala are described along with corresponding non-toxic pharmaceutically-acceptable acid addition salts as well as intermediates useful in the synthesis of the tetradecapeptides. The tetradecapeptide in which Y is Gly as well as its pharmaceutically acceptable acid addition salts exhibit as their principal activity the in vivo inhibition of the release of gastric acid. The tetradecapeptide in which Y is D-Ala as well as its pharmaceutically acceptable acid addition salts exhibit as their principal activity the in vivo stimulation of the release of growth hormone.
Abstract: Cephalosporin antibiotics of the formula ##STR1## in which, for example, R is phenyl, hydroxyphenyl, halophenyl, thienyl, or furyl; R.sub.1 is hydrogen, carbamoyloxy, acetoxy, a lower alkyl substituted 1H-tetrazol-5-ylthio or 1,3,4-thiadiazol-5-ylthio group; and R.sub.2 is hydrogen or methyl; are highly active broad spectrum antibiotics especially useful in the treatment of infections attributable to the gram-negative microorganisms.
Abstract: Certain halogenated phenylthioacetamido cephalosporanic acids and derivatives thereof, e.g., 7-[2'-(2",5"-dichlorophenylthio)acetamido]cephalosporanic acid, are effective antibiotics against Staphylococcus aureus cultures which show heterogeneous resistance to methicillin.
Abstract: The proteinase plasmin is assayed either colorimetrically or fluorometrically with a tripeptidyl-4-methoxy-2-naphthylamide substrate having the following general formula: ##STR1## The substrate is useful for either routine clinical assays or kinetic studies.
Type:
Grant
Filed:
May 10, 1976
Date of Patent:
November 1, 1977
Assignee:
Eli Lilly and Company
Inventors:
Jesse L. Bobbitt, Edward L. Smithwick, Jr.
Abstract: Cephalosporin antibiotics of the formula ##STR1## in which, for example, R is phenyl, hydroxyphenyl, halophenyl, thienyl, or furyl; R.sub.1 is hydrogen, carbamoyloxy, acetoxy, a lower alkyl substituted 1H-tetrazol-5-ylthio or 1,3,4-thiadiazol-5-ylthio group; and R.sub.2 is hydrogen, C.sub.1 -C.sub.3 alkyl, C.sub.1 -C.sub.3 alkoxy, chloro, bromo, or fluoro; are highly active broad spectrum antibiotics especially useful in the treatment of infections attributable to the gram-negative microorganisms.