Abstract: Steroids of the formula ##STR1## wherein n represents the number 2, 3 or 4; R.sup.1 represents hydrogen, lower-alkyl or lower-alkylidene; R.sup.2, R.sup.3 and R.sup.4 represent hydrogen or lower-alkyl and the dotted C--C bonds in the 5(6)-, 7(8)-, 22(23)-, 24(28)- and 25(26)-position are optional, whereby the B-ring can contain only one double bond and the side-chain is either saturated or is mono-unsaturated or is di-unsaturated in the 22(23), 25(26)-position; and whereby R.sup.1 is lower-alkyl or lower-alkylidene when a 5(6)-double bond is present, n is 2 and R.sup.2, R.sup.3 and R.sup.4 are methyl,and pharmaceutically acceptable salts of these steroids have activity inhibiting the intestinal resorption of cholesterol. They can be manufactured from steroids which are otherwise substituted in the 3.beta.-position.
Abstract: Disclosed herein are methods and means of microbially preparing novel human hybrid leukocyte interferons, useful in the treatment of viral and neoplastic diseases, by DNA recombination of parental interferon genes, taking advantage of common restriction endonuclease cleavage sites therein and in carrier expression plasmids.
Abstract: Novel pyridine, pyrazine and pyrimidine derivatives of the formula ##STR1## wherein R, R.sup.1, R.sup.2, R.sup.3 and R.sup.4 are as hereinafter set forth, and acid addition salts thereof, processes for their preparation, fungicidal compositions containing these compounds as the active ingredient as well as the use of such compounds or compositions for the control of fungi in agriculture and in horticulture are disclosed.
Type:
Grant
Filed:
October 1, 1984
Date of Patent:
July 7, 1987
Assignee:
Hoffman-La Roche Inc.
Inventors:
Franz Dorn, Albert Pfiffner, Beat Zehnder
Abstract: Novel p-[2(4,4-dimethyl-6-heterophenyl)substituted phenyl derivatives and salts thereof which are useful for combatting neoplasms and dermatoses including oral and topical compositions containing said derivatives which are suitable for such uses.
Abstract: Compounds of the formula ##STR1## wherein R.sup.1 is hydrogen or straight-chain alkyl; R.sup.2 is --CN, --R, --COR, --COOR or when R.sup.2 is positioned on an aromatic ring R.sup.2 also can be --OR, --OOCR or --F; R is alkyl; A is a group with 1 to 4 six-membered rings, these rings being linked directly with one another and with ring B in each case via a single covalent bond or being linked at one or two positions also via --COO--, --OOC-- or --CH.sub.2 CH.sub.
Abstract: Polycyclic salts of the formulaA-XN+CH.sub.2 --(Y).sub.n --(CH.sub.2).sub.p --(Z).sub.q --L--(T).sub.r --M IwhereinA.sup.- is the anion of a strong organic or inorganic acid;XN.sup.+ is pyridinium, pyrimidinium, thiazolium or imidazolium substituted by R.sup.1, R.sup.2 and R.sup.3 ;n, q and r individually are the integer 1 or 0 and p is an integer from 1 to 15;Y is CH.sub.2, C(H,OH) or C(O):Z is O, S, CH.sub.2, C(O), NQ.sup.1, SO.sub.2, C(O)O, OC(O), C(O)N(Q.sup.1) or N(Q.sup.1)C(O);L is p-phenylene substituted by R.sup.4 ; andM is phenyl substituted by R.sup.5 and R.sup.6,T has one of the meanings given above, for Z or is C(CH.sub.3).sub.2, C.sub.2 H.sub.4, C(Q.sup.2).dbd.C(Q.sup.3), C.tbd.C, CH.sub.2 C(O), C(O)CH.sub.2, CH.sub.2 O or OCH.sub.2,R.sup.1 is a group Ar, Ar-C.sub.1-4 -alkyl, ArO or ArC(O),Ar is phenyl substituted by R.sup.7, R.sup.8 and R.sup.9 ;R.sup.2 and R.sup.3 individually are H, C.sub.1-4 -alkyl, C.sub.1-4 -alkoxy or C.sub.6 H.sub.
Type:
Grant
Filed:
January 15, 1986
Date of Patent:
June 23, 1987
Assignee:
Hoffmann-LaRoche Inc.
Inventors:
Jean-Marie Cassal, Albrecht Edenhofer, Henri Ramuz
Abstract: A real-time method and appartus is disclosed for scanning large body areas to produce an ultrasound cross-sectional picture of the area in which at least two different and partially overlapping sector scans of the body are carried out in one scanning plane by the pulse-echo method utilizing an ultrasound transducer unit having a rigid transducer which is pivotable about an axis of oscillation perpendicular to the scanning plane, which performs an oscillatory movement about the axis of oscillation and between two end positions on each scan, and which is segmented into adjacent transducer elements. In performing the scans, at least two different transducer sets are used, each containing one or more transducer elements, each transducer set being used both for the emission of the ultrasound pulses and for the reception of echo waves. In all the scans the position of the axis of oscillation remains unchanged with respect to the body.
Type:
Grant
Filed:
September 23, 1985
Date of Patent:
June 23, 1987
Assignee:
Kontron Holding AG
Inventors:
John G. Abbott, Christoph B. Burckhardt, Pierre-Andre Grandchamp, Peter Krummenacher, Claude Schlaepfer
Abstract: The crystallization of human leukocyte interferon is described. In a preferred embodiment crystalline recombinant human leukocyte interferon A (IFL-rA) is prepared.
Type:
Grant
Filed:
July 3, 1985
Date of Patent:
June 9, 1987
Assignee:
Hoffmann-La Roche Inc.
Inventors:
Hsiang-Fu Kung, David L. Miller, Sidney Pestka
Abstract: There is presented antibiotic compounds designated as Antibiotics X-14889 A, C and D of the formulas ##STR1## wherein (for X-14889A) R.sub.1 is methyl, R.sub.2 is methyl, R.sub.3 is hydrogen, R.sub.4 is methyl and R.sub.5 is hydrogen or (for X-14889C) R.sub.1 is hydrogen, R.sub.2 is methyl, R.sub.3 is hydrogen, R.sub.4 is methyl and R.sub.5 is CO.sub.2 H or ##STR2## and the pharmaceutically acceptable salts thereof. The compounds exhibit antimicrobial activity and one of the compounds X-14889C also exhibits activity against Treponema hyodysenteriae (in vitro), Plasmodium berghei and as food efficiency enhancers in ruminants.Also presented is a process to produce the above compounds and another known component Antibiotic X-14889B.
Abstract: The invention relates to compounds of the formula ##STR1## wherein R is hydrogen or lower alkyl, Y is alkylene; Z is alkylene, ##STR2## the asterisk herein denotes bonding to the substituted acetophenone; R.sub.2 is hydrogen or lower alkoxy; and n is an integer of 1 to 3; A is ##STR3## and HET is a 5-or 6- membered nitrogen containing heterocyclic group, and their acid addition salts. The compounds of formula I of the invention are useful for the treatment of allergic conditions, such as, asthma and cardiovascular diseases, such as, angina and arrhythmias.
Type:
Grant
Filed:
April 22, 1985
Date of Patent:
June 9, 1987
Assignee:
Hoffmann-La Roche Inc.
Inventors:
Matthew Carson, Ru-Jen L. Han, Ronald A. LeMahieu
Abstract: A process is described for the preparation of fat-soluble vitamin active beadlet compositions which exhibit superior stability when exposed to the feed pelleting process. The process includes forming an aqueous emulsion of a fat-soluble vitamin-active material, gelatin, and a sugar converting the emulsion to dry particulate form containing the non-aqueous constituents of the emulsion and heat treating the resulting product to form water insoluble beadlets.
Abstract: The prostacyclins 7-fluoro-6,9-epoxy-16-substituted-15-hydroxyprost-[4 or 5,13]-dienoic acids and esters useful as anti-secretory agents, blood pressure lowering agents, anti-ulcerogenic agents, anti-hypertensive agents, bronchodilation agents and for combating gastro-hyperacidity and as anti-blood platelet aggregating agents.
Type:
Grant
Filed:
September 9, 1985
Date of Patent:
May 12, 1987
Assignee:
Hoffmann-La Roche Inc.
Inventors:
George W. Holland, Perry Rosen, Hans Maag
Abstract: A novel process for the manufacture of quinone derivatives which are suitable as intermediates for the manufacture of (2RS,4'R,8'R)-tocopherol is described. In this process a quinone of the formula ##STR1## is reacted with a phytyl derivative of the formula ##STR2## If desired, the thus-obtained compound of the formula ##STR3## is subsequently converted into the compound of the formula ##STR4## and, if desired, this compound is converted into the compound of the formula ##STR5## The compound of formula V is known and can be converted into (2RS,4'R,8'R)-tocopherol in a known manner.
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--(CH.sub.2).sub.4 -- (b)or--CH.dbd.CH--CH.dbd.CH--, (c)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.
Abstract: The invention relates to an analytical rotor comprising a set of analytical cells disposed at its periphery, a central distribution chamber, portioning cavities corresponding to the respective cells and disposed between the cells and the chamber periphery, the cavities each having an inlet connected to the chamber and an outlet connected to one of the cells by a transfer passage, and at least one overflow reservoir connected to the inlets of the cavities by at least one communication passage.
Abstract: Compounds of the formula ##STR1## wherein R.sub.1, R.sub.2, R.sub.3, and A are as described herein, are set forth.These compounds are useful as anti-allergic agents and agents for the treatment of cardiovascular diseases.
Abstract: A novel enantiomeric systhesis from ascorbic acid of (3S,4S)-3-amino-4-carbamoyloxymethyl-2-azetidinone-1-sulfate, an intermediate for an antibiotic compound.
Abstract: The present disclosure relates to novel liposome compositions and methods for their preparation. Utilization of the present invention provides an efficient reconstitution of membrane proteins into large (0.1 to 2 micron diameter) phospholipid vesicles with a large, internal aqueous space. The method has been exemplified with the use of glycoproteins of influenza (A/PR8/34) and Sendai (parainfluenza type I) viruses.
Abstract: A DNA-directed in vitro assay for measuring the formation of the initial NH.sub.2 -terminal dipeptides or tripeptides which are characteristic of a particular gene product is disclosed. This invention also encompasses a kit consisting of the reagents necessary to perform this method so as to measure or identify a product of gene expression.