Abstract: Process and device for the automatic dilution of solutions using a peristaltic pump. Successive dilution processes can be carried out with a relative precision that remains high for a long time and without manual interference, with the advantage that the device is easily adjustable to any desired degrees of dilution. The peristaltic pump rotates continuously at a constant rate in one direction and the suction line immerses alternately, in each case during a certain number of pump strokes, in the solution to be diluted and in a diluent. A dilution operation is comprised of three stages, in which the suction tube is immersed in the diluent in the first and last stages and in the solutions to be diluted in the middle stage.
Type:
Grant
Filed:
June 23, 1976
Date of Patent:
August 8, 1978
Assignee:
Hoffmann-La Roche Inc.
Inventors:
Rudolf Bernet, Hans Koller, Eugen Wachberger
Abstract: This invention is directed toward pharmacologically active compounds of the formula ##STR1## wherein A represents a nitrogen atom which may be substituted by a methyl, cyclopropylmethyl, di(C.sub.1-4 alkyl)aminoethyl, methoxymethyl or hydroxyethyl group and B represents a carbonyl group or A and B together represent a grouping of the formula ##STR2## in which R.sup.a represents a hydrogen atom or a lower alkyl or hydroxymethyl group and X represents a nitrogen atom or C--R.sup.b wherein R.sup.b represents a hydrogen atom or a lower alkyl or hydroxymethyl group; R represents a halogen atom or a nitro or trifluoromethyl group; R.sup.1 represents a hydrogen atom or a lower alkyl group; R.sup.2 represents an acyl group derived from a naturally occurring amino acid (all such groups which contain an asymmetric carbon atom having the L- or D,L-configuration) and R.sup.3 represents a phenyl, halophenyl or 2-pyridyl group and acid addition salts thereof.
Type:
Grant
Filed:
November 11, 1976
Date of Patent:
August 8, 1978
Assignee:
Hoffmann-La Roche Inc.
Inventors:
Cedric H. Hassall, William H. Johnson, Antonin Krohn, Carey E. Smithen, William A. Thomas
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:
March 18, 1977
Date of Patent:
August 8, 1978
Assignee:
Hoffmann-La Roche Inc.
Inventors:
Max Gerecke, Emilio Kyburz, Jean-Pierre Kaplan
Abstract: Human .beta.-endorphin (.beta..sub.h -endorphin) is prepared by solution phase peptide synthesis. Synthesis proceeded via the protected .beta.-endorphin fragments 1-9, 10-18, 19-21 and 22-31.
Abstract: Optically active organic compounds are prepared starting from optically inactive reactants by means of an optically active agent which influences the course of the reaction. In particular optically active compounds having a "meso" type carbon atom undergo an intramolecular ring closure in the presence of an optically active agent to yield an optically active product having one additional ring. The present process is particularly useful in the preparation of optically active bicyclic diketones which are important intermediates in the total synthesis of steroids.
Abstract: Taurine and glycine derivatives of nor or bisnorcholanic acid or etiocholanic acid which are useful in increasing bile flow or decreasing lipid levels and their method of production from deoxycholic acid, including intermediates thereof.
Type:
Grant
Filed:
April 22, 1977
Date of Patent:
August 1, 1978
Assignee:
Hoffmann-La Roche Inc.
Inventors:
Hugo Gallo-Torres, Robert William Guthrie, James Guthrie Hamilton, Richard Wightman Kierstead, Ann Clare Sullivan
Abstract: An improved immunoassay for methadone is disclosed. The subject radioimmunoassay utilizes a novel antigen, antibody and novel labelled methadone derivatives.
Type:
Grant
Filed:
October 13, 1976
Date of Patent:
August 1, 1978
Assignee:
Hoffmann-La Roche Inc.
Inventors:
Magdalena Usategui Gomez, Harvey Gurien, John Edward Heveran, Manfred Weigele
Abstract: Plant growth regulant compounds represented by the formula: ##STR1## wherein, when n is 1, R is hydrogen, sodium, potassium, ammonium, substituted ammonium, straight or branched chain aliphatic hydrocarbyl or halo-lower alkyl and, when n is 2, R is calcium, magnesium or lower alkylene, R.sub.1, R.sub.2, R.sub.3 and R.sub.4 are hydrogen, straight or branched chain aliphatic lower hydrocarbyl, halo-lower alkyl, aryl or R.sub.1 and R.sub.2 together and R.sub.3 and R.sub.4 together are each a saturated ring containing from 3 to 8 carbon atoms, n is an integer from 1 to 2 and X is a number from 0 to 1; enantiomers and racemic mixtures.These compounds are useful as post-emergence and pre-emergence plant growth regulants and herbicides.
Abstract: Asymmetric synthesis of optically active 3,7,11-trimethyl-dodecan-1-ol, an intermediate for producing optically active vitamin E, from isovaleraldehyde or prenal including intermediates in this synthesis.
Abstract: A multi-step, stereospecific total synthesis of steroids is disclosed. The starting materials for this process are the relatively inexpensive and readily available m-alkoxy acetophenones. The process is suitable for the preparation of racemic or optically active, medicinally valuable steroids, particularly A-ring aromatic steroids. This process features an early optical resolution and a unique asymmetric induction which insures the correct stereochemistry of the final steroidal product.
Abstract: Optically active organic compounds are prepared starting from optically inactive reactants by means of an optically active agent which influences the course of the reaction. In particular optically active compounds having a "meso" type carbon atom undergo an intramolecular ring closure in the presence of an optically active agent to yield an optically active product having one additional ring. The present process is particularly useful in the preparation of optically active bicyclic diketones which are important intermediates in the total synthesis of steroids.
Type:
Grant
Filed:
September 14, 1976
Date of Patent:
July 25, 1978
Assignee:
Hoffmann-La Roche Inc.
Inventors:
Zoltan George Hajos, David Richard Parrish
Abstract: Two enkephalin analogs, [D-Met.sup.2, Thz.sup.5 ]-enkephalinamide and [D-Thr.sup.2, Thz.sup.5 ]-enkephalinamide have been found to be potent analgesic agents.
Abstract: A radioimmunoassay for cocaine and the cocaine metabolite benzoylecgonine is described. The assay utilizes a novel labelled compound .sup.125 I-4-hydroxybenzoylecgonine.
Abstract: Aminoaryl esters and amino-lower alkyl amides of carboxy substituted barbiturates are linked via an amide linkage to carboxylated latex polymers to form reagents which are useful in a sensitive diagnostic test to detect the presence of barbiturates in body fluids.The large increase in the abuse of therapeutic agents, particularly the barbiturates, by the general population as well as military personnel, has brought with it a substantial need to improve analytical techniques for the determination of such agents in biological fluids. In many instances, medical treatment centers are faced with the immediate need for determining the identity of a barbiturate taken by a patient who is unable, being in a comatose condition, or unwilling to supply such information to the treating physician. Early procedures involved the identification of barbiturates by extraction and thin-layer, gas chromatographic and spectrophotometric methods.
Type:
Grant
Filed:
May 26, 1976
Date of Patent:
July 18, 1978
Assignee:
Hoffmann-La Roche Inc.
Inventors:
Antonino Focella, John Edward Heveran, Sidney Teitel, Manfred Weigele
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,Are 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:
March 18, 1977
Date of Patent:
July 11, 1978
Assignee:
Hoffmann-La Roche Inc.
Inventors:
Max Gerecke, Emilio Kyburz, Jean-Pierre Kaplan
Abstract: Compositions having antibiotic properties containing as antibiotic potentiators peptides of the formula ##STR1## wherein R.sup.1 represents a hydrogen atom or a lower alkyl, lower cycloalkyl, (lower cycloalkyl)-(lower alkyl), aryl or aryl(lower alkyl) group (said group being optionally substituted as the case may require by one or more amino, hydroxy, thio, methylthio, carboxy or guanidino groups so as to form the characterizing group of a naturally occurring L .alpha.-amino acid); R.sup.2 and R.sup.3 each represent the characterizing group of an .alpha.-amino acid of the type normally found in proteins with the proviso that R.sup.3 cannot represent a hydrogen atom when n is zero and R.sup.1 is a hydrogen atom or the phenyl group; R.sup.4 represents a hydroxy or methyl group; n stands for zero, 1, 2 or 3; and single asterisks denote that the configuration at the carbon atom so-marked is L when R.sup.2 or R.sup.
Type:
Grant
Filed:
July 21, 1976
Date of Patent:
July 11, 1978
Assignee:
Hoffmann-La Roche Inc.
Inventors:
Frank Ratcliffe Atherton, Michael John Hall, Cedric Herbert Hassall, Peter Stuart Ringrose, Robert Wilson Lambert
Abstract: The invention relates to a new and useful antibiotic substance which is of the formula ##STR1## and to processes for its production and recovery. The antibiotic which exhibits ionophoric properties, is classified as a polyether group antibiotic. The antibiotic of formula I is effective in inhibiting the growth of gram positive bacteria and exhibits utility as an antihypertensive agent and as a compound to improve ruminant feed utilization. The antibiotic of Formula I is prepared by cultivating a strain of Streptomyces sp. X-14547 in an aqueous carbohydrate solution containing nitrogenous nutrients and mineral salts and thereafter isolating the antibiotic from the fermentation broth.
Abstract: There is disclosed a method and apparatus for developing and controlling pharmaceutical granulations from a tabletting characteristics standpoint, involving instrumenting a tablet press to derive both the peak compression force and peak ejection force information for each tabletting event in convenient digital form. The thusly derived compression and ejection force information is automatically scaled to desired units of force and utilized in compression and ejection profiles and in the calculation of the average and standard deviations for both compression and ejection in the pursuit of optimization of the tabletted granulation regarding such tabletting characteristics as compressibility, lubricity, relative flow, compression failure point, and tendency of the formed tablets to adhere to the tablet press punches.
Type:
Grant
Filed:
August 13, 1976
Date of Patent:
July 11, 1978
Assignee:
Hoffmann-La Roche Inc.
Inventors:
Donald Melvyn Stiel, Charles Robert Browski, Eric Neugroschel, Joseph James Williams