Abstract: The vitamin D.sub.3 derivative 1.alpha.,25,26-trihydroxycholecalciferol which is useful for regulating the calcium metabolism or calcium transport in the body, cholestene intermediates and a process for their preparation are described.
Abstract: Compounds of the formula ##STR1## wherein A is methylene, ethylene or propylene which may be substituted by lower alkyl, B is carbonyl or methylene, R.sup.1 is halogen, carboxyl, lower alkoxycarbonyl, hydroxyaminocarbonyl, mercapto, lower alkanoylthio or aryl(lower alkylthio)--, R.sup.2 is hydroxy, lower alkoxy or amino, R.sup.3 is hydrogen, lower alkyl, aryl or aryl(lower alkyl)--, R.sup.4 is hydrogen, lower alkyl, aryl, aryl-(lower alkyl)-- or a group of the formula --A-R.sup.1 wherein A and R.sup.1 are as described above and the broken line denotes an optional carbon-carbon bond which can be present only when B is carbonyl,and salts of the acids of formula I with pharmaceutically acceptable bases, a process for the manufacture thereof and pharmaceutical preparations containing same, are described. The compounds of formula I and their salts are useful as antihypertensive agents.
Type:
Grant
Filed:
June 10, 1981
Date of Patent:
August 16, 1983
Assignee:
Hoffmann-La Roche Inc.
Inventors:
Cedric H. Hassall, Geoffrey Lawton, Christopher J. Moody
Abstract: The present invention relates to a method of treating osteoporosis by administering to a host suffering from osteoporosis an effective amount of 24,24-difluoro-1.alpha.,25-dihydroxycholecalciferol.
Type:
Grant
Filed:
May 17, 1982
Date of Patent:
August 9, 1983
Assignee:
Hoffmann-La Roche Inc.
Inventors:
Alfred Boris, John J. Partridge, Milan R. Uskokovic
Abstract: 2,3-Indoledione derivatives of the formula ##STR1## wherein R is isopropyl or tert.butyl, R.sup.1 is hydrogen or lower alkyl and R.sup.2 is lower alkyl or lower aralkyl, and their pharmaceutically acceptable acid addition salts, prepared from a compound of the formula ##STR2## wherein R.sup.3 is hydroxy and R.sup.4 is chlorine or bromine or R.sup.3 and R.sup.4, taken together, are oxygen, and R.sup.1 and R.sup.2 are as previously set forth, are described. The compounds of formula I and their pharmaceutically acceptable addition salts are useful as .beta.-adrenergic blocking agents and antihypertensive agents.
Abstract: Liquid crystal mixtures containing a coloring substance which comprise about 5 to about 40 weight % of trans-p-[5-(4-alkylcyclohexyl)-2-pyrimidinyl]benzonitriles, about 10 to about 60 weight % of trans-4-alkylcyclohexane carboxylic acid phenyl esters and about 0.1 to about 15 weight % of one or more coloring substances of the formula ##STR1## wherein m stands for the number 1 and X is alkoxy and Y is nitro; or m stands for the number 1 or 2; and X is p-alkoxyphenyl and Y is nitro or dialkylamino, or X is alkoxy and Y is -p-nitrophenyl or -(dialkylamino)phenyl; or m stands for the number 2, and X is alkoxy and Y is alkoxy, nitro or dialkylamino, or both X and Y are dialkylamino; and wherein the alkoxy denotes a straight-chain group containing 1 to 12 carbon atoms and the alkyl groups in the dialkylamino each denote a straight-chain alkyl group containing 1 to 4 carbon atoms are described.
Type:
Grant
Filed:
July 1, 1981
Date of Patent:
July 26, 1983
Assignee:
Hoffmann-La Roche Inc.
Inventors:
Arthur Boller, Alfred Germann, Martin Schadt, Alois Villiger
Abstract: Compounds of the formula ##STR1## wherein ring A is saturated or aromatic and a saturated ring A which may be present is trans-linked with the second ring; R.sup.1 is a straight-chain alkyl or alkoxy group containing 1 to 11 carbon atoms; R.sup.2 is cyano, a straight-chain alkyl group containing 1 to 11 carbon atoms, an ester group of the formula ##STR2## or, when ring A is saturated, additionally a straight-chain alkoxy group containing 1 to 11 carbon atoms; in the ester group of formula II ring B is either aromatic and X is oxygen or sulfur and R.sup.3 is cyano or a straight-chain alkyl or alkoxy group containing 1 to 10 carbon atoms, or ring B is a trans-1,4-disubstituted cyclohexane ring and X is oxygen and R.sup.3 is cyano or a straight-chain alkyl group containing 1 to 10 carbon atoms; and the total number of carbon atoms in the alkyl and/or alkoxy groups amounts to at most 12, are described. The compounds of formula I are useful in liquid crystal mixtures.
Type:
Grant
Filed:
August 3, 1981
Date of Patent:
July 5, 1983
Assignee:
Hoffmann-La Roche Inc.
Inventors:
Arthur Boller, Martin Schadt, Alois Villiger
Abstract: Phenyl-quinolizidines of the general formula ##STR1## wherein X is hydrogen, fluorine, chlorine, lower-alkoxy, lower-alkyl or trifluoromethyl; Y is hydrogen, fluorine, chlorine, lower-alkoxy or lower-alkyl; and R.sup.1 is acyl, acylamino or a group A of the formula ##STR2## wherein R.sup.2 is oxygen or sulfur; R.sup.3 is hydrogen or lower-alkyl; and one of R.sup.4 and R.sup.5 is hydrogen and the other is bromine, iodine, cyano, lower-alkoxycarbonyl or sulfamoyl,as racemates or enatiomers, as well as acid addition salts thereof, utilizing various intermediates, are described. The foregoing compounds are useful as neuroleptic, antiemetic and analgesic agents.
Abstract: Imidazoquinazolines of the formula ##STR1## wherein R.sup.1, R.sup.2 and R.sup.3 are hydrogen, halogen, C.sub.1-4 -alkyl, C.sub.1-4 -alkoxy or C.sub.2-5 -alkoxyalkyl; or two of R.sup.1, R.sup.2 and R.sup.3 on adjacent carbon atoms taken together are methylenedioxy or ethylenedioxy; and R.sup.4 and R.sup.5 are hydrogen or C.sub.1-4 -alkyl,and their tautomers, as well as their physiologically compatible acid addition salts, are described.The compounds of formula I inhibit the aggregation of the blood platelets, as well as gastric acid secretion, and have activity on the circulatory system.
Type:
Grant
Filed:
August 12, 1981
Date of Patent:
June 28, 1983
Assignee:
Hoffmann-La Roche Inc.
Inventors:
Madhukar S. Chodnekar, Ado Kaiser, Frank Kienzle
Abstract: Pyrimidine derivatives of the formula ##STR1## wherein at least one of rings A and B is a trans-1,4-disubstituted cyclohexane ring and the other, optionally, may be aromatic and R is straight-chain alkyl or alkoxy of 1 to 10 carbon atoms or a branched-chain alkyl group of the formula C.sub.2 H.sub.5 --CH(CH.sub.3)--(CH.sub.2).sub.n -- wherein n is 1, 2 or 3, are described. Processes for the preparation of the compounds of formula I as well as their uses in liquid crystalline mixtures are also described.
Type:
Grant
Filed:
January 30, 1981
Date of Patent:
June 21, 1983
Assignee:
Hoffmann-La Roche Inc.
Inventors:
Arthur Boller, Martin Schadt, Alois Villiger
Abstract: Neuroleptically active cycloalka[4,5]pyrrolo[2,3-g]isoquinolines of the formula ##STR1## wherein n, R.sub.1, R.sub.2 and X are as hereinafter set forth, and intermediates therefore are described.
Abstract: Phenoxy-aminopropanol derivatives of the formula ##STR1## wherein R is lower alkyl, X is oxygen or sulfur, n is the integer zero or 1, Y is methylene, ethylene or propylene or, when n is zero, Y can also be a group of the formula--CH.dbd.CH--C*H.sub.2 -- (a), wherein the double-bond is trans and the carbon atom marked with an asterisk is linked to Z, and Z is a 5-membered aromatic heterocyclic ring which contains one or more nitrogen atoms as the sole hetero atom (s), said heterocyclic ring is linked to Y via a nitrogen atom, and may be substituted by halogen, lower alkyl, lower alkoxy, aryl, cyano or carboxamido, or on adjacent carbon atoms by a group of the formula ##STR2## and pharmaceutically acceptable acid addition salts thereof are described. A process for the preparation of the compound of formula I and pharmaceutical preparations containing them are also described. The aforementioned compounds and salts possess .beta.-adrenergic blocking activity and antihypertensive activity.
Abstract: Imidazole derivatives of the formula ##STR1## wherein X is hydrogen or C.sub.1-4 -alkyl, Y is sulfur, sulfinyl or sulfonyl and Z is thienyl, optionally substituted by methyl or fluorine, or a group of the formula ##STR2## wherein R.sup.1, R.sup.2 and R.sup.3 are hydrogen, methyl, fluorine, hydroxy, methoxy, methylthio or two of R.sup.1, R.sup.2 and R.sup.3 on adjacent carbon atoms taken together are methylenedioxy or ethylenedioxy or one of R.sup.1, R.sup.2 and R.sup.3 is mono- or di-(C.sub.1-4 -alkyl)-amino and the other two are hydrogen,and physiologically or pharmaceutically compatible or acceptable acid addition salts thereof, are described. The compounds of formula I inhibit the aggregation of the blood platelets and have antihyperglycemic activity.
Abstract: Antiallergically-active pyrimidine derivatives of the formula ##STR1## wherein R.sup.1 is hydrogen, chlorine, bromine or C.sub.1-4 -alkyl, and R.sup.2 is hydrogen or methyl, prepared starting from corresponding 4-oxothieno-[3,2-d]pyrimidine derivatives, are described.
Abstract: Levorotatory N-substituted acylmorphinans of the formula ##STR1## wherein R.sub.1 is hydrogen, lower alkyl, lower alkenyl, cycloalkyl-lower alkyl, cyano-lower alkyl, aryl-lower alkyl, or 5- or 6-membered heterocyclic-lower alkyl, and one of R.sub.2 or R.sub.3 is hydrogen and the other of R.sub.2 or R.sub.3 is alkanoyl of 2 to 7 carbon atoms, aroyl, trifluoromethylcarbonyl or ##STR2## wherein R is hydrogen or lower alkyl and n is an integer of 0 to 6, and salts thereof with pharmaceutically acceptable acid addition salts, are described. The compounds of formula I are useful as analgesic agents.
Abstract: 1-Ethyl-1,4-dihydro-6-(2-naphthyl)-4-oxonicotinic acid and C.sub.1-6 -alkyl esters thereof as well as their alkali metal, alkaline earth metal or ammonium salts are described. The foregoing compounds are useful as central nervous system stimulants. Also described are 1-ethyl-6-(2-naphthyl)-4-oxo-1,4,5,6-tetrahydronicotinic acid and C.sub.1-6 -alkyl esters thereof, which are useful as intermediates.
Abstract: Imidazole derivatives of the formula ##STR1## wherein R.sup.1, R.sup.2 and R.sup.3, independently, are hydrogen, halogen, trifluoromethyl, nitro, lower alkyl or lower alkylthio; one of R.sup.4 and R.sup.5 is hydrogen and the other is hydrogen, halogen, hydroxy or lower alkoxy; R.sup.6 is hydrogen or lower alkyl; R.sup.7 is hydrogen, hydroxy, lower alkyl or lower alkoxy; and either R.sup.8 is hydrogen, lower alkyl, lower alkenyl, aryl(lower alkyl) or acyl and R.sup.9 taken together with R is an additional bond, or R.sup.9 is lower alkyl, lower alkenyl or aryl(lower alkyl) and R.sup.8 taken together with R is an additional bond; provided that R.sup.4 or R.sup.5 is not hydroxy when R.sup.7 is lower alkoxy and/or R.sup.8 is acyl, and that R.sup.7 is not hydroxy when R.sup.4 or R.sup.5 is lower alkoxy and/or R.sup.8 is acyl, and their pharmaceutically acceptable acid addition salts are described, the compounds of formula I have valuable therapeutic properties and are especially useful as analgesics.
Abstract: Compounds of the formula ##STR1## wherein R.sup.1 and R.sup.2, independently, are hydrogen, halogen or lower alkyl; R.sup.3, R.sup.4, R.sup.5, R.sup.6 and R.sup.7, independently, are hydrogen or lower alkyl; R.sup.8 is hydrogen, lower alkyl or formyl; R.sup.9 and R.sup.10, independently, are methyl or trifluoromethyl; and n is 0 (zero) or, when both R.sup.7 and R.sup.8 are lower alkyl, n is 0 (zero) or 1, prepared, inter alia, from p-aminobenzaldehydes which may be N-alkyl substituted, are described. The compounds of formula I are orally active antidiabetic agents.
Abstract: Oxadiazolo[2,3-c]pyrimidine derivatives of the formula ##STR1## wherein R is alkyl, alkenyl, alkynyl or alkoxyalkyl, as well as their salts, are described. The compounds of formula I have valuable, long-lasting vasodilating and/or blood pressure-lowering properties and are useful for the treatment of vascular-conditioned hypertensions or as vasodilators in peripheral blood supply disorders. The compounds are prepared, inter alia, by carbamoylating the corresponding derivative containing a free amino group and optional salt formation.
Type:
Grant
Filed:
December 4, 1982
Date of Patent:
November 23, 1982
Assignee:
Hoffmann-La Roche Inc.
Inventors:
Urs Hengartner, Jean-Claude Muller, Henri Ramuz
Abstract: 2-Imino-imidazolidine derivatives of the formula ##STR1## wherein R.sup.1, R.sup.2, R.sup.3 and R.sup.4 are as hereinafter set forth, and pharmaceutically acceptable acid addition salts thereof, are described. The 2-imino-imidazolidine derivatives are useful in the treatment of hypertension.
Abstract: Neuroleptically active octahydro-1H-pyrrolo[2,3-g]isoquinolines of the formula ##STR1## wherein R.sub.1, R.sub.2, R.sub.3, R.sub.4 and X are as hereinafter set forth, are described.