Abstract: 2-(2-Oxo-1-pyrrolidinyl)acetic acids of the formula ##STR1## wherein R.sup.2 is hydrogen or lower alkyl and R.sup.11 is hydrogen, lower alkanoyl or another group readily cleavable by means of ammonia, are described. The compounds of formula III of the invention are useful to prepare the compound of formula I of the invention which are useful as medicaments, for example, in the form of pharmaceutical preparations.
Abstract: The disclosure provides an improved reactor/fermentor apparatus useful for carrying out cell culture and fermentation. The apparatus utilizes novel design features to provide optimum agitation of the cells while minimizing mechanical shear force. The reactor is composed of two chambers; an upper, wider chamber and a lower, small diameter chamber which are connected by inwardly sloping side walls. Agitation is accomplished by utilizing a gently flowing centrally disposed gas stream.
Abstract: Novel growth hormone releasing factor analogs in which glycine at position 15 is replaced by appropriately selected amino acids demonstrate enhanced potency for the release of growth hormone and the analogs can be administered to a subject having a deficiency of growth hormone.
Type:
Grant
Filed:
August 6, 1985
Date of Patent:
March 10, 1987
Assignee:
Hoffmann-La Roche Inc.
Inventors:
Arthur M. Felix, Edgar P. Heimer, Thomas F. Mowles
Abstract: Substituted phenoxy-aminopropanols of the formula ##STR1## wherein R is a branched-chain alkyl of 3 or 4 carbon atoms, R.sup.1 is hydrogen, halogen or lower alkyl and R.sup.2 and R.sup.3, independently, are hydrogen, halogen, lower alkyl, lower alkoxy or lower alkylthio, and pharmaceutically acceptable acid addition salts thereof, are described. A process for their preparation, as well as pharmaceutical preparations containing them are also described. The compounds of formula I and their salts possess cardioselective .beta.-adrenergic blocking activity and antihypertensive activity.
Abstract: Aqueous vitamin E solutions useful for parenteral adminstration are disclosed. The solution comprises phospholipid-cholanic acid mixed micelles in which the molar ratio of phospholipid: cholanic acid is about 0.2-0.9:1 and about 100 g or more of vitamin E per mol of phospholipid.
Abstract: The compounds 9-phenyl-3,7-dimethyl-2,4,6,8 nonatetraenoic acids wherein the phenyl group is substituted with an alkyl, aminoalkyl, hydroxyalkyl, alkoxy, hydroxyalkylamino, and a hydroxy alkoxy group, and derivatives thereof which are used as disease modifying anti-rheumatic agents and as immunosuppressants.
Type:
Grant
Filed:
June 20, 1985
Date of Patent:
March 10, 1987
Assignee:
Hoffmann-La Roche Inc.
Inventors:
Edward R. Aig, John W. Coffey, Allen J. Lovey, Michael Rosenberger
Abstract: A method for the photometric analysis of a liquid sample in which different path lengths of the sample are analyzed photometrically.In order to reduce the time needed for analyzing a large number of samples, the analysis is carried out with a light beam which is generated by an immobile light source; the sample is introduced into a cuvette which has at least two regions with different cross-section lengths; and the cuvette is continuously moved along a circular path in such a manner that in the course of the photometric measurement the light beam passes through at least two of the regions in succession.
Abstract: .beta.-lactams of the formula ##STR1## wherein R.sup.1 signifies hydrogen or a group readily cleavable by hydrolysis, A signifies the group R.sup.2 --N.dbd.C(CH.sub.3)--CH.dbd.C< or O.dbd.C(CH.sub.3)--CH.sub.2 --C(R.sup.3)<, R.sup.2 signifies hydroxy, lower alkoxy or arylamino and R.sup.3 signifies arylthio, lower alkanoylthio, lower alkoxycarbonylhydrazino or a N-containing saturated heterocycle attached via a N-atom, and pharmaceutically acceptable salts thereof, are disclosed. The compounds and their salts exhibit .beta.-lactamase inhibiting activities against .beta.-lactamases from bacteria.
Abstract: The total radiation load on a subject being treated for psoriasis with a psoralen in conjunction with ultraviolet A radiation (PUVA) can be substantially reduced by at least pretreating said subject with an anti-psoriatic effective polyene compound such as a retinoid, .beta.-carotene or phytoene.
Abstract: Unsaturated eicosanoic acids and derivatives thereof which inhibit the synthesis of SRS-A are useful for treating and preventing asthma and allergic responses caused by SRS-A as well as useful in inhibiting inflammation.
Type:
Grant
Filed:
March 17, 1986
Date of Patent:
February 10, 1987
Assignee:
Hoffmann-La Roche Inc.
Inventors:
Ka-Kong Chan, George W. Holland, Perry Rosen
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.
Abstract: A compound of the formula ##STR1## wherein R.sub.1 is phenyl substituted with 1 to 3 lower alkoxy groups, or 1 to 3 halogens; R.sub.2 is hydroxy or lower alkanoyloxy; R.sub.3 and R.sub.4 are each independently lower alkyl or together form a pyrrolidine or piperidine ring; and n is 2 to 4, and pharmaceutically acceptable acid addition salts thereof are described. The compounds of formula I are active as calcium channel blockers and accordingly, are useful as agents for lowering blood pressure, and as agents for treating ischemia.
Abstract: The compounds of the formula ##STR1## wherein one of the symbols Q and Q' is the group --CH.dbd. and the other is the group --CH.dbd. or --N.dbd., R.sup.1, R.sup.2 and R.sup.3 each independently are hydrogen or halogen and n is the integer 0, 1 or 2,and their pharmaceutically acceptable acid addition salts, which have valuable antimycotic properties and can be used for the control of infections caused by pathogenic fungi, are described.
Abstract: A marking device for marking a sheet mounted on a digitizer board includes a measuring coil inductively coupled to the digitizer board when the coil is operatively positioned relative to the board. A switch on the marking device is operable to cause current pulses to be applied to the conductors on the digitizer board producing magnetic flux which couples the conductors on the board to the coil. A marker on the marking device is responsive to operation of the switch for marking a thermosensitive sheet on which the measuring coil is placed thereby marking on the sheet the position of the marking device when the switch was closed.
Abstract: A cuvette arrangement for use in a chemical analysis system, which cuvette arrangement comprises an integrally constructed unit which defines separate chambers, for the receipt of sample-reagent mixtures.
Abstract: A process for the manufacture of intermediates in the synthesis of biotin as well as of biotin itself is described. In this process the side chain is attached to the ring system by means of a Grignard reaction, the resulting compound is then dehydrated and subsequently reduced.
Abstract: 1.alpha.,25-Dihydroxy-24R-fluorocholecalciferol and 1.alpha.,25-dihydroxy-24S-fluorocholecalciferol, analogs of 1.alpha.,25-dihydroxy-cholecalciferol which is physiologically the most active metabolite of vitamin D.sub.3, are synthesized in a multistep process from the known substance 1.alpha.,3.beta.-dihydroxyandrost-5-en-17-one. The new analogs are characterized by the ability to increase intestinal calcium transport, increase serum calcium and phosphate concentrations and to increase the deposition of these minerals in bones. These compounds will find a ready application as substitutes for natural 1.alpha.,25-dihydroxycholecalciferol in the treatment of disease states characterized by metabolic calcium and phosphate deficiencies.
Type:
Grant
Filed:
April 11, 1984
Date of Patent:
January 6, 1987
Assignee:
Hoffmann-La Roche Inc.
Inventors:
John J. Partridge, Shian-Jan Shiuey, Milan R. Uskokovic
Abstract: 7-fluoro-16-substituted 15-hydroxy PGI.sub.2 compounds which have saturated bond of the 13 position and which are useful as blood platelet anti-aggregating agents.
Type:
Grant
Filed:
June 24, 1985
Date of Patent:
January 6, 1987
Assignee:
Hoffmann-La Roche Inc.
Inventors:
George W. Holland, Hans Maag, Perry Rosen
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 and R.sup.8 is hydrogen or lower alkyl, and their acid addition salts are described. These compounds are useful as agents for control or prevention of ulcers and of increased gastric acid secretion.
Type:
Grant
Filed:
April 8, 1985
Date of Patent:
January 6, 1987
Assignee:
Hoffmann-La Roche Inc.
Inventors:
Albert Fischli, Anna Krasso, Henri Ramuz, Andre Szente