Abstract: Benzylpyrimidines of the formula ##STR1## wherein R.sup.1 and R.sup.2 each, independently, is amino, optionally C.sub.1.sub.-3 -alkyl-substituted pyrrolo, pyrrolidino, piperidino, -NHR.sup.3, -N(R.sup.3).sub.2, -NHR.sup.4, -N(R.sup.3)(R.sup.4),-NR.sup.3 COOR.sup.3, -NHCOOR.sup.3, -NHCONHR.sup.3, -NHCONH.sub.2 or -N(NO)R.sup.3 or wherein R.sup.3 is C.sub.1.sub.-4 -alkyl or C.sub.2.sub.-4 -alkenyl, R.sup.4 is acyl; Z is hydrogen, chlorine, bromine, pyrrolo, pyrrolidino, piperidino or morpholino or R.sup.3, OR.sup.3 or -N(R.sup.3).sub.2 ; A is an oxygen atom bonded to one of the cyclic nitrogen atoms; and n is 0 or 1 are prepared. The benzylpyrimidines are useful as potentiators of the activity of the sulfonamides.
Type:
Grant
Filed:
December 19, 1975
Date of Patent:
August 2, 1977
Assignee:
Hoffmann-La Roche Inc.
Inventors:
Ivan Kompis, Gerald Rey-Bellet, Guido Zanetti
Abstract: An untriakontapeptide having significant opiate agonist activity has been isolated from camel pituitary glands. The structure of this peptide has been determined and this peptide was then synthesized utilizing solid phase peptide synthesis. Both natural and synthetic material show identical physical and biological properties.
Abstract: Compounds of the formula ##STR1## wherein R.sub.1 is lower alkyl or phenyl lower alkyl: R.sub.2 is phenyl or substituted phenyl: and R.sub.3 is substituted or unsubstituted phenyl, naphthyl or indolyl;Are fluorogenic reagents which react with primary amino groups to form fluorophors. The above compounds are useful for fluorescent labeling of materials of biological importance.
Type:
Grant
Filed:
March 18, 1976
Date of Patent:
July 26, 1977
Assignee:
Hoffmann-La Roche Inc.
Inventors:
Roy Cleeland, Jr., Emanuel Grunberg, Willy Leimgruber, Manfred Weigele
Abstract: Stereospecific syntheses of 24R,25- and 24S,25-dihydroxycholesterol and alkanoyl derivatives thereof, intermediates in the preparation of biologically important metabolites of Vitamin D.sub.3, are described.
Type:
Grant
Filed:
October 20, 1975
Date of Patent:
July 26, 1977
Assignee:
Hoffmann-La Roche Inc.
Inventors:
John Joseph Partridge, Jr., Milan Radoje Uskokovic
Abstract: D-homosteroids of the formula ##STR1## wherein R.sup.6 is hydrogen, fluorine, chlorine or methyl; R.sup.9 is hydrogen, fluorine, chlorine or bromine; R.sup.17 and R.sup.21 each independently are hydroxy or acyloxy, and U represents optional olefinic unsaturation are endocrine agents having anti-inflammatory properties.
Abstract: 11-Substituted prostaglandins E.sub.1, E.sub.2 and F.sub.2.alpha. useful as cardiovascular agents and as agents for inducing labor in pregnant females and for the termination of pregnancy and a process for preparing these prostaglandins.
Type:
Grant
Filed:
September 17, 1975
Date of Patent:
July 19, 1977
Assignee:
Hoffmann-La Roche Inc.
Inventors:
George William Holland, Jane Liu Jernow, Perry Rosen
Abstract: Compounds of the formulas ##STR1## WHEREIN R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, R.sub.6, R.sub.7, R.sub.8 and X are as hereinafter set forth, are described. The compounds of formulas I and Ia are useful as neuroleptic agents.
Abstract: Compounds of the formulas ##STR1## WHEREIN R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, R.sub.6, R.sub.7, R.sub.8 and X are as hereinafter set forth,Are described. The compounds of formulas I and Ia are useful as neuroleptic agents.
Abstract: The present invention relates to a new synthesis for the preparation of 5-(substituted benzyl)-2,4-diamino-pyrimidines, including new pyrimidine derivatives. More particularly, a new synthesis of ormetoprin, diaveridine and related compounds, including novel derivatives, is disclosed. The synthesis involves the condensation of a substituted benzene and an acrylonitrile derivative to directly give enol ether intermediates, which upon subsequent reaction by known techniques with guanidine, provides the desired 5-(substituted benzyl)-2,4-diamino-pyrimidines, including novel compounds. The pyrimidine end products are useful as potentiators of sulfonamides and as antibacterial agents.
Abstract: A method is disclosed for controlling liver fluke infections comprising orally administering to host animals an anthelmintically effective amount of a compound selected from a group of halogen-substituted-benzenesulfonanilides represented by the formula: ##STR1## wherein each of R.sub.1 and R.sub.2 are independently chlorine or bromine, R.sub.3 is hydrogen or chlorine and each of R.sub.4 through R.sub.7 is independently hydrogen, halogen or trifluoromethyl, with the proviso that at least 2 of R.sub.3 through R.sub.7 is other than hydrogen and X is hydrogen or lower alkanoyl.
Abstract: Arrangement for coordinating and documenting the handling of material between at least two sites remote from one another, which is useful particularly in inventory control situations and the movement of bulk pharmaceuticals. There is provided at a first site a master data communicator unit whereby an operator may, upon preliminarily addressing the programmable data lock portion of the master unit with the correct code, enter data, for example, alphanumeric data, into the master unit. This information is automatically forwarded to one or more slave units associated with respective slave sites, wherein the information entered at the master unit is continuously displayed on both the master and slave units. The information forwarded to the slave unit is passed through an information distribution control arrangement situated at the master site by which an operator may control the dissemination of the data entered in the master unit to the slave units on a need-to-know basis.
Type:
Grant
Filed:
April 28, 1976
Date of Patent:
July 5, 1977
Assignee:
Hoffmann-La Roche Inc.
Inventors:
John Marshall Free, Charles William Jeunelot
Abstract: A fermentation process is disclosed wherein the known antibiotic lysocellin is produced by the fermentation of a new species of Streptomyces denominated as Streptomyces longwoodensis (X-14537).
Type:
Grant
Filed:
August 12, 1976
Date of Patent:
July 5, 1977
Assignee:
Hoffmann-La Roche Inc.
Inventors:
Chao-Min Liu, Norberto Palleroni, Theron Hermann, Barbara Prosser
Abstract: 6-Phenyl-S-triazolo[4,3-a][1,4]benzodiazepines bearing in the 8-position a hydroxyamino or azoxy substituent are disclosed together with processes for preparing these compounds and intermediates used in these processes. These triazolobenzodiazepines are useful as muscle relaxant, anti-convulsant and sedative agents.
Abstract: Dibenz[b,f]oxepins of the formula ##STR1## wherein R, R.sub.1, R.sub.2, R.sub.3 and R.sub.4 are as hereinafter described. The foregoing compounds exhibit strong central depressant and neuroleptic properties, and are useful, for example, in the treatment of acute or chronic schizophrenia and also as tranquilizers.
Type:
Grant
Filed:
December 18, 1974
Date of Patent:
June 28, 1977
Assignee:
Hoffmann-La Roche Inc.
Inventors:
Max Gerecke, Emilio Kyburz, Jean-Pierre Kaplan
Abstract: This invention relates to a process for the preparation of 2-alkenyl-4-hydroxy-3-methyl-2-cyclopenten-1-ones from the reaction product of 2,4-pentane dione and a 2-propen-or 2-propyn-1-ol derivative including intermediates therein.
Abstract: Process for synthesizing the lactone, (dl) 3,3a beta-4,5-6,6a beta-hexahydro-4beta(3-hydroxyl-1-trans-octenyl)-5alpha-hydroxy-2-oxo-2H-c yclopenta[b]furan, a known intermediate for producing prostaglandin E.sub.2 and F.sub.2.sub..alpha. and a process for preparing 11-desoxy and 11-alkyl prostaglandins from dihydroresorcyclic acid.
Abstract: This invention is directed toward pharmacologically active compounds of the formula ##STR1## wherein R represents a hydrogen atom or a lower alkyl group and R.sub.1 represents a hydrogen or halogen atom or a trifluoromethyl group which have the absolute configuration S at the 3-position carbon atom.Also presented is a process to produce the above benzodiazepine derivatives and pharmaceutical preparations therefor. The above benzodiazepine derivatives exhibit pronounced anthelmintic, especially schistosomicidal, activity and muscle relaxant, anticonvulsant and sedative activities.
Abstract: There is disclosed instrumentation for use in connection with one or more tablet presses of various types, and in particular rotary tablet presses, for virtually any reasonable combination and number of such tablet presses. Tablet formation information, in particular compression and ejection force information, tablet capping information and force information related to the time of occurrence of punch withdrawal is provided and processed by such instrumentation. This information is selectively applied to converting means which renders the selected information in a convenient data form for processing. Selection of the information may be made for example based on the need or desire to monitor a particular tablet press, tablet press station and/or individual tablet die/punch set combination.
Abstract: Pharmaceutical dosage forms comprising an edible web having deposited thereon or at least partially thereon a particulate medicament, the webs being thereafter fabricated and finished to pharmaceutically elegant solid dosage forms having no medicament exposed on an exterior surface. The dosage forms have a consistency of release of medicament which can be controlled to exacting specifications. The disclosed solid dosage forms are prepared by high speed automated equipment and the process by which they are made is characterized by non-destructive quality control analysis and performance evaluation both conducted on-line and integrated into the manufacturing operation. Included in the scope of the disclosed invention are certain apparatus and methods of manufacture.