Abstract: The invention is directed to a process and intermediates for the preparation of benzopyrans such as racemic-6-acetyl-7-[5-(4-acetyl-3-hydroxy-2-propylphenoxy)pentyloxy]-3, 4-dihydro-2H-1-benzopyran-2-carboxylic acid.
Abstract: The invention relates to compounds of the formula: ##STR1## wherein R is hydrogen or lower alkyl, R.sub.1, R.sub.2, R.sub.3 and R.sub.4, independently, are hydrogen, lower alkyl, lower alkenyl, cycloalkyl or phenyl unsubstituted or substituted by up to 3 substituents independently selected from lower alkyl, lower alkoxy or halogen, or R.sub.1 and R.sub.2 taken together with the carbon atom are alkylene of 2 to 5 carbon atoms unsubstituted or substituted by lower alkyl, and n is an integer of from 0 to 3,and, when R.sub.1 is different from R.sub.2 and/or when R.sub.3 is different from R.sub.4, enantiomers, diastereomers and racemates thereof and, when R is hydrogen, salts thereof with pharmaceutically acceptable bases.The compounds of formula I and, when R is hydrogen, pharmaceutically exceptable salts thereof are useful as bronchopulmonary agents, for example, in the relief of asthma and allergic reactions.
Type:
Grant
Filed:
June 13, 1989
Date of Patent:
March 19, 1991
Assignee:
Hoffmann-La Roche Inc.
Inventors:
George F. Field, John R. Vermeulen, William J. Zally
Abstract: A process for the manufacture of 6-aliphatic C.sub.2-20 -carboxylic acid esters of ascorbic acid by esterifying the ascorbic acid with an aliphatic C.sub.2-20 -carboxylic acid halide in the presence of a N,N-dialkyl-alkanecarboxylic acid amide, of a cyclic amide of the 1-methyl-2-pyrrolidone type, of a tetraalkylcarbamide such as tetramethylurea, of a cyclic carbamide of the 1,3-dimethyl-2-imidazolidinone type or of a phosphoric acid triamide of the hexamethylphosphoric acid triamide type. The 6-ascorbyl linolate which can be manufactured in this manner is novel and is likewise an object of the present invention. The thus-manufacturable 6-aliphatic C.sub.2-20 -carboxylic acid esters of ascorbic acid are important alternative application forms of L-ascorbic acid (vitamin C).
Abstract: An explosive and propellant composition is obtained by admixing finely divided particles of ascorbic acid and a nitrate-containing oxidation agent, such as potassium nitrate. Admixing can be carried out in the dry state, at room temperature. The composition upon ignition gives off no sulfurous fumes, and leaves little or no carbon residue; and causes no corrosion with contacted metal surfaces.
Abstract: Compounds of the formula ##STR1## wherein A is a group of the formula HN(OH)--CO-- or HCO--N(OH)--; R.sup.1 is a C.sub.2 -C.sub.5 -alkyl; R.sup.2 is the characterizing group of a natural .alpha.-amino acid in which any functional group present may be protected, any amino group present may be acylated and any carboxyl group present may be amidated, with the proviso that R.sup.2 is not hydrogen or methyl; R.sup.3 is hydrogen, amino, hydroxy, mercapto, C.sub.1 -C.sub.6 -alkyl, C.sub.1 -C.sub.4 -alkoxy, C.sub.1 -C.sub.6 -alkylamino, C.sub.1 -C.sub.6 -alkylthio or aryl-(C.sub.1 -C.sub.6 -alkyl), or amino-(C.sub.1 -C.sub.6 -alkyl), hydroxy-(C.sub.1 -C.sub.6 -alkyl), mercapto-(C.sub.1 -C.sub.6 -alkyl) or carboxy-(C.sub.1 -C.sub.6 -alkyl) in which the amino, hydroxy, mercapto or carboxyl group may be protected, the amino group may be acylated or the carboxyl group may be amidated; R.sup.4 is hydrogen or methyl; R.sup.5 is hydrogen or a C.sub.1 -C.sub.6 -alkyl, C.sub.1 -C.sub.6 -alkoxy-C.sub.1 -C.sub.6 -alkyl, di(C.
Type:
Grant
Filed:
April 11, 1989
Date of Patent:
February 26, 1991
Assignee:
Hoffmann-La Roche Inc.
Inventors:
Balraj K. Handa, William H. Johnson, Peter J. Machin
Abstract: A process for preparing optically active naphtho[1,2-b][1,4]thiazepin-4(5H)-ones comprising resolution of rac-.beta.-[(2-amino-1-naphthalenyl)thio]-.alpha.- hydroxy-4-methoxybenzenepropanoic acid and converting the optically active acids so obtained into final products is described. The end product naphtho[1,2-b][1,4]thiazepin- 4(5H)-ones have activity as calcium channel blockers and accordingly are useful as agents for lowering blood pressure, and as agents for treating ischemia.
Abstract: Compositions comprising a mixture of a 2,4-diamino-5-(trisubstituted)benzyl-pyrimidine potentiated sulfonamide antibiotic with an ionophorous polyether anticoccidial agent are useful for the treatment and prevention of coccidiosis in animals.
Type:
Grant
Filed:
July 11, 1988
Date of Patent:
February 26, 1991
Assignee:
Hoffmann-La Roche Inc.
Inventors:
Eugene G. Schildknecht, Govind G. Untawale
Abstract: Dihydropyridine derivatives of the formula ##STR1## wherein the symbols R and R.sup.1 to R.sup.6 have the significance given in claim 1, have a pronounced calcium-antagonist activity and can accordingly be used as medicaments, especially in the control or prevention of angina pectoris, ischemia, high blood pressure and/or migraine.
Abstract: A compound of the formula ##STR1## wherein R.sup.1 is hydroxy, lower-alkoxy, amino, mono- or di-lower-alkylamino;R.sup.2 is hydrogen, alkyl, akoxy or halogen;R.sup.3, R.sup.4, R.sup.5, R.sup.6, R.sup.11 and R.sup.12 independently are hydrogen or lower-alkyl;R.sup.3 and R.sup.5 taken together are methylene or hydroxymethylene;R.sup.7, R.sup.8, R.sup.9 and R.sup.10 independently are hydrogen or lower-alkyl;R.sup.11 and R.sup.12 taken together are oxo or spiro-cyclo-lower alkyl; or R.sup.11 is hydrogen and R.sup.12 is hydroxy or acetoxy; and one of the residues R.sup.13 and R.sup.14 is hydrogen and the other is lower-alkyl or trifluoromethyl, as well as physiologically compatible salts of carboxylic acids of formula I, which can be used as medicaments, especially for the treatment of neoplasms, acne and psoriasis, are described. The compounds of the invention can be prepared by the synthesis of the C(R.sup.13).dbd.C(R.sup.
Abstract: Methods and compositions are provided for the high level expression of human interleukin-2 in mammalian cells. This high level expression is produced by the substitution of the normal human 5' noncoding sequences and the AUG initiation codon of the interleukin-2 gene by heterologous corresponding sequences. The expression product is a glycosylated polypeptide which is similar to the natural product and which can be purified to a high degree of purity for use as a therapeutic agent.
Abstract: Compounds of the formula ##STR1## wherein R.sub.1 is phenyl substituted with 1 to 3 substituents selected from the group consisting of halogen and lower alkoxy; R.sub.2 is hydrogen, lower alkyl, lower alkanoyl, lower cycloalkanoyl, ##STR2## R.sub.3 and R.sub.4 are independently lower alkyl, phenyl lower alkyl or together form a piperidine or pyrrolidine ring; n is 2 ro 4; m is 1 to 2; and pharmaceutically acceptable acid addition salts thereof, with the proviso that when R.sub.1 is 4-methoxyphenyl, R.sub.2 is hydrogen and R.sub.3 and R.sub.4 are methyl; and n is 2, the compound of formula I cannot be in the (-)-cis form,are described. The compounds of formula I are active as calcium channel blockers and accordingly, are useful as agents for treating ischemia.
Abstract: Pyridine-ethanolamines of the formula ##STR1## wherein n, X, Y, R.sup.1, R.sup.2 and R.sup.3 have the significances given in the description, their corresponding enantiomers, diastereomers, and racemates as well as the physiologically compatible salts thereof are described. The compounds of formula I have catabolic activity and can be used for the treatment of obesity and of diabetes mellitus or of conditions which are associated with an increased protein breakdown, or as feed additives for fattening animals. The compounds of formula I can be prepared by alkylating the primary or secondary amines corresponding to the secondary or tertiary amines of formula I.
Abstract: There is described a unique instrument system employing a laser, having a polarized and collimated beam of radiation, which is split into a multitude of primary and secondary beams containing the same desirable properties of high collimation and monochromaticity. The secondary beams are used to measure simultaneously multiple antigen-antibody (Ag-Ab) agglutinations reactions involving latex particles.
Abstract: Tricyclic imidazole derivatives of formula I ##STR1## wherein one of R.sup.1 and R.sup.3 is lower alkyl and the other is hydrogen or lower alkyl, R.sup.2 is lower alkyl, n is the number 0 or 1, A is ##STR2## R.sup.4, R.sup.5, R.sup.6 and R.sup.7 each is lower alkyl land R.sup.8 is hydrogen nor lower alkyl,and their acid addition salts are described. These compounds are useful as agents for control or prevention of ulcers and of increaased gastric acid secretion.
Type:
Grant
Filed:
January 5, 1990
Date of Patent:
January 1, 1991
Assignee:
Hoffmann-La Roche Inc.
Inventors:
Albert Fischli, Anna Krasso, Henri Ramuz, Andre Szente
Abstract: This invention concerns compounds of the formula: ##STR1## wherein X is a single covalent bond, --CH.sub.2 CH.sub.2 --, 1,4-phenylene, a 2,5-disubstituted pyrimidine ring or a group of the formula: ##STR2## ring A is trans-1,4-cyclohexylene or, when X is a single covalent bond, ring A may also be 1,4-phenylene, a 2,5-disubstituted pyrimidine ring or a trans-2,5-disubstituted m-dioxane ring; andR.sup.1 is straight-chain trans-1-alkenyl having 2 to 12 carbon atoms or straight-chain trans-3-alkenyl having 4 to 12 carbon atoms or, when X is --CH.sub.2 CH.sub.2 --, R.sup.1 may also be 1,4-phenylene, a 2,5-disubstituted pyrimidine ring or a group of formula IA or when ring A is a 2,5-disubstituted pyrimidine ring of a trans-2,5-disubstituted m-dioxane ring, R.sup.1 may also be straight-chain alkyl with 1 to 12 carbon atoms; and one of the benzene rings may have a lateral fluorine substituent;their manufacture, and liquid crystalline mixtures and electro-optical device containing same.
Type:
Grant
Filed:
April 3, 1987
Date of Patent:
December 25, 1990
Assignee:
Hoffmann-La Roche Inc.
Inventors:
Martin Petrzilka, Martin Schadt, Alois Villiger
Abstract: Novel 4-substituted-4,8-dimethyl-2,3-dioxabicyclo[3.3.1] nonan-7-ones which have a pronounced activity against the causative organism of malaria and can be used for the prevention and control of malaria.
Type:
Grant
Filed:
September 29, 1988
Date of Patent:
December 11, 1990
Assignee:
Hoffmann-La Roche Inc.
Inventors:
Werner Hofheinz, Gerard Schmid, Harro Stohler
Abstract: Tetracyclic compounds of the formula ##STR1## wherein R.sup.1, R.sup.2, X, Y, Z and n are as hereinafter described, and salts thereof, prepared starting from corresponding tricyclic compounds, are described. The compounds I and some of the said tricyclic compounds have antibacterial activity, and are therefore useful as antibacterial agents.