Abstract: A stable ergot alkaloid soft gelatin capsule consisting essentially of a soft gelatin capsule shell and encapsulated therein a liquid center fill solution consisting essentially of a therapeutically effective amount of an ergot alkaloid of the formula ##STR1## wherein R.sub.1 is hydrogen or halogen,R.sub.2 is hydrogen or C.sub.1-4 alkyl,R.sub.3 is isopropyl, sec.-butyl, isobutyl or benzyl,R.sub.4 is methyl, ethyl or isopropyl, and eitherR.sub.5 is hydrogen andR.sub.6 is hydrogen or methoxy orR.sub.5 and R.sub.6 together is an additional bond,or mixtures thereof, dissolved in a pharmaceutically acceptable polar, hydrophilic soft gelatin capsule center fill solvent.
Type:
Grant
Filed:
June 24, 1981
Date of Patent:
December 28, 1982
Assignee:
Sandoz, Inc.
Inventors:
Samuel B. Stoopak, Saul S. Kornblum, Allen L. Jacobs
Abstract: Tropyl derivatives of the formula: ##STR1## in which R.sup.1 is (a) phenyl linked through a direct bond, --O--, ##STR2## (in which m=2 or 3); (b) diphenylmethyl; or (c) 10H-phenothiazin-10-yl; (each of which type may be substituted, or unsubstituted); R.sup.2 is --H, --OH, or --O Si (CH.sub.3).sub.3 ; and R.sup.3 is substituted or unsubstituted phenyl, e.g. 4-[3-(4-fluorobenzoyl)-8-azabicyclo [3.2.1]oct-8-yl]-1-(-4-fluorophenyl)-1-butanone, in free base form or pharmaceutically acceptable acid addition salts are useful as pharmaceuticals.
Abstract: Herbicidal and algaestatic and algaecidal compositions and use thereof comprising copper salts; both soluble acid salts as copper sulfate, chloride, nitrate, acetate, sulfamate, gluconate, citrate, etc. and basic copper salts such as basic copper sulfate, cupric hydroxide, basic copper carbonate, basic copper chloride and the like for a method for treating bodies of water to arrest or eliminate the growth of algae and aquatic weeds by giving a more efficient algaestat, algaecide and/or herbicide, when the copper salts or insoluble basic copper salts are used as a complex with an alkylene diamine, such as ethylenediamine, propylenediamine and substituted derivatives of these; or poly (aminoalkylene).sub.n --NH.sub.
Abstract: The invention discloses certain 1-phenyl-pyrazole derivatives having pharmacological activity in animals and useful as glucagon inhibiting agents. Nearly all of the compounds of this invention are prepared by cyclization of a phenyl hydrazine compound with a 1,1,3,3-tetra-C.sub.1-4 -alkoxy-propane compound.
Abstract: A liposome medicament delivery system wherein the medicament is encapsulated in a liposome comprising an aliphatic liquid-sterol-water lamellae. The lipid may be a sodium or potassium salt of a C.sub.4 to C.sub.18 fatty acid, and the sterol may be cholesterol.
Abstract: The compounds are 1-aryl-1-lower alkyl-substituted-1-buten-3-ols, butan-3-ols, and acylation products thereof, e.g., (p-biphenylyl)-2-penten-4-ol and are useful as pharmaceuticals.
Abstract: Compounds of the formula ##STR1## wherein R.sub.1 is C.sub.1-4 alkyl,R.sub.2 is hydrogen, C.sub.1-4 alkyl or C.sub.1-4 alkoxy,R.sub.3 is hydrogen or C.sub.1-4 alkyl, andM is hydrogen or a monovalent non-chromophoric cation,and mixtures of such compounds, stable, concentrated, aqueous compositions consisting essentially of, by weight,5-20% Compound of said formula in salt form or a mixture thereof2-25% 2-(2-Methoxyethoxy)ethanol0-8% Propylene glycolBalance Water,and the use of such compounds, mixtures and stable, concentrated, aqueous compositions for dyeing and printing anionically dyeable substrates such as natural and synthetic polyamides, especially nylon carpet.
Type:
Grant
Filed:
February 23, 1981
Date of Patent:
July 20, 1982
Assignee:
Sandoz, Inc.
Inventors:
Silvio A. Rodriguez, Sigmund C. Catino, deceased
Abstract: This disclosure describes compounds of the formula ##STR1## where R.sub.1 represents hydrogen, fluoro, chloro, lower alkyl having 1 to 4 carbon atoms or lower alkoxy having 1 to 4 carbon atoms, andR.sub.2 represents hydroxy, andR.sub.3 and R.sub.4 each independently represent lower alkyl as defined above, orR.sub.3 and R.sub.4 together with N represent ##STR2## wherein n is 1, 2 or 3, andR.sub.5 and R.sub.6 each independently represent hydrogen or lower alkyl as defined above,or a pharmaceutically acceptable acid addition salt thereof, which are useful as anti-diabetic agents, in particular as hypoglycemic agents and inhibiting or impeding post-prandial hyperglycemia.
Abstract: This disclosure describes compounds of the formula ##STR1## where R.sub.1 represents hydrogen, fluoro, chloro, lower alkyl having 1 to 4 carbon atoms or lower alkoxy having 1 to 4 carbon atoms, andR.sub.2 and R.sub.3 each independently represent lower alkyl as defined above, orR.sub.2 and R.sub.3 together with N represent ##STR2## wherein n is 1, 2 or 3, andR.sub.4 and R.sub.5 each independently represent hydrogen or lower alkyl as defined above,or a pharmaceutically acceptable acid addition salt thereof, which are useful as anti-diabetic agents in particular as hypoglycemic agents and inhibiting or impeding post-prandial hyperglycemia.
Abstract: This disclosure describes compounds of the formula ##STR1## wherein R.sub.1 represents hydrogen, fluoro, chloro, lower alkyl having 1 to 4 carbon atoms, or lower alkoxy having 1 to 4 carbon atoms, andR.sub.2 represents lower alkyl or ##STR2## where R.sub.5 represents hydrogen, fluoro, chloro, lower alkyl or lower alkoxy, andR.sub.3 and R.sub.4 each independently represent lower alkyl as defined above, andR.sub.3 and R.sub.4 together with N represent ##STR3## or pharmaceutically acceptable acid addition salts thereof, which are useful as anti-diabetic agents.
Abstract: The compounds are 4-phenyl-4-lower alkyl-substituted-3-buten-2-ones, and -2-halo-1,3-butadienes, e.g., 2-(p-biphenylyl)-2-penten-4-one, and are useful as pharmaceuticals.
Abstract: Compounds of the formula ##STR1## and pharmaceutically acceptable acid addition salts thereof, whereinR.sub.1 is C.sub.1-4 alkyl,R.sub.2 is hydrogen, C.sub.1-4 alkyl, C.sub.1-4 alkoxy, halo, trifluoromethyl, C.sub.1-4 alkylthio or --NR.sub.5 R.sub.6, wherein each of R.sub.5 and R.sub.6 is independently hydrogen or C.sub.1-3 alkyl,R.sub.3 is hydrogen, C.sub.1-3 alkyl, C.sub.1-3 alkoxy, halo or trifluoromethyl, andR.sub.4 is hydrogen, C.sub.1-3 alkyl, C.sub.1-3 alkoxy or halo,their use as muscle relaxants and as anti-inflammatory agents, pharmaceutical compositions comprising them, processes for their synthesis and compounds of the formulae ##STR2## wherein R.sub.1, R.sub.2, R.sub.3 and R.sub.4 are as defined above, useful as intermediates in their synthesis.
Abstract: Herbicides are of the formula ##STR1## wherein W is fluoro, bromo, chloro or CF.sub.3,each of X and X.degree. is independently H, fluoro, chloro, bromo, C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy, CF.sub.3 or nitro,Z and Z.sub.1 are independently oxygen or sulfur, with the proviso that at least one is oxygen,each of Y and Y.degree. is independently H, fluoro, chloro, bromo, C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy, CF.sub.3 or nitro,R.sub.1 and R.sub.4 are independently H, C.sub.1 -C.sub.4 alkyl and --COOR.sub.5 wherein R.sub.5 is H or C.sub.1 -C.sub.4 alkyl,R.sub.2 and R.sub.3 are independently H, C.sub.1 -C.sub.5 alkyl, fluoro, chloro, bromo or hydroxy, andR and R.degree. are independently H or C.sub.1 -C.sub.3 alkyl or both together form a covalent bond or an epoxy bridge (--O--),with the further proviso that no two adjacent ring members in either Rings A or B are from the group of t-butyl, t-butoxy and CF.sub.3.
Abstract: The compounds are 1-(3-halo-1,2-dioxopropyl)-cycloamines, eg 1-(3-chloro-1,2-dioxopropyl)-piperidine, and are useful as fungicides and bactericides. They can be prepared by halogenation of a corresponding 1-(1,2-dioxopropyl)-cycloamine.
Abstract: The compounds are free hydantoin derivatives of the formula: ##STR1## wherein X is a divalent radical consisting of from 2 to 5 linked units; one unit being --O--, and from one to 4 hydrocarbon units, independently, having the structure(a) --CH.sub.2 -- or (b) --C(R).sub.2 --in which R is alkyl having from 1 to 6 carbon atoms and being free of branching on the .alpha.-carbon atoms; provided that no more than 2 units are of type b; or a pharmaceutically acceptable salt form thereof with a suitable cation; e.g. 7-oxa-1,3-diazaspiro[4.4]nonane-2,4-dione, and are useful as pharmaceuticals.
Abstract: Compounds of the formula ##STR1## wherein R.sub.1 is hydrogen, alkyl of 1 to 6 carbon atoms or amino,R.sub.2 is hydrogen or alkyl of 1 to 6 carbon atoms, with the provisos that (1) at least one of R.sub.1 and R.sub.2 is not a tertiary alkyl group and (2) R.sub.2 is hydrogen when R.sub.1 is amino, orR.sub.1 and R.sub.2 taken together and with the nitrogen atom to which they are joined are pyrrolidino,piperidino or N'-2-hydroxyethylpiperazino,each X' is independently alkyl of 1 to 4 carbon atoms, alkoxy of 1 to 4 carbon atoms or halo or two X's on adjacent carbon atoms together are methylenedioxy, andn is 0, 1, 2 or 3,and the pharmaceutically acceptable acid addition salts thereof,are useful as anti-obesity and anti-diabetic agents.The compounds wherein R.sub.1 is alkyl and R.sub.2 is hydrogen are synthesized by a two-step synthesis from 2-alkyl-5-arylisoxazolium salts and ethylenediamine. The compounds wherein R.sub.1 and R.sub.
Abstract: Agents for lowering glucose levels in blood having the formula: ##STR1## wherein R.sub.o is bromo, chloro, fluoro, nitro or trifluoromethyl,R is hydrogen, C.sub.1-6 alkyl or C.sub.2-18 alkanoyl, andR.sub.1 is hydrogen or C.sub.1-12 alkyl,and the non-toxic, pharmaceutically acceptable salts thereof.
Abstract: Fungicides are of the formula: ##STR1## wherein R and R' are each independently alkyl of 1 to 4 carbon atoms,R.degree. is trihalomethyl in which the halo atoms are of atomic weight of from 18 to 36, e.g. trifluoromethyl or trichloromethyl, cyano or --SO.sub.2 NR"R"', andR" and R"' are each independently hydrogen or alkyl of 1 to 4 carbon atoms.
Abstract: This disclosure describes novel compounds of the formula ##STR1## wherein R.sub.1 and R.sub.2 each represent hydrogen, or ##STR2## and R.sub.3 is hydrogen or fluoro, andn is 1, 2 or 3, andprovided that one of R.sub.1 and R.sub.2 is other than hydrogen which are useful as anti-obesity agents.
Abstract: Compounds of the formula ##STR1## wherein R.sub.1 is hydrogen, alkyl of 1 to 6 carbon atoms or amino, R.sub.2 is hydrogen or alkyl of 1 to 6 carbon atoms, with the provisos that (1) at least one of R.sub.1 and R.sub.2 is not a tertiary alkyl group and (2) R.sub.2 is hydrogen when R.sub.1 is amino, orR.sub.1 and R.sub.2 taken together and with the nitrogen atom to which they are joined are pyrrolidino, piperidino or N'-2-hydroxyethylpiperazino,each X' is independently alkyl or 1 to 4 carbon atoms, alkoxy of 1 to 4 carbon atoms or halo, or two X's on adjacent carbon atoms together are methylenedioxy, andn is 0, 1, 2 or 3,and the pharmaceutically acceptable acid addition salts thereof, are useful as anti-obesity and anti-diabetic agents. The compounds wherein R.sub.1 is alkyl and R.sub.2 is hydrogen are synthesized by a two-step synthesis from 2-alkyl-5-arylisoxazolium salts and ethylenediamine. The compounds wherein R.sub.1 and R.sub.