Patents Represented by Attorney Samuel L. Welt
  • Patent number: 4105137
    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
  • Patent number: 4105681
    Abstract: Novel 9-phenyl 5,6-dimethyl-nona-2,4,6,8-tetraenoic acid,-tetraenal or tetraenol derivatives useful as anti-tumor agents.
    Type: Grant
    Filed: August 13, 1976
    Date of Patent: August 8, 1978
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Werner Bollag, Rudolf Ruegg, Gottlieb Ryser
  • Patent number: 4105852
    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
  • Patent number: 4105664
    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
  • Patent number: 4105652
    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.
    Type: Grant
    Filed: August 5, 1977
    Date of Patent: August 8, 1978
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Johannes A. Meienhofer, Su-Sun Wang
  • Patent number: 4105696
    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 7, 1976
    Date of Patent: August 8, 1978
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Zoltan G. Hajos, David R. Parrish
  • Patent number: 4104285
    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
  • Patent number: 4104367
    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
  • Patent number: 4104052
    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.
    Type: Grant
    Filed: February 13, 1976
    Date of Patent: August 1, 1978
    Assignee: Hoffmann-La Roche Inc.
    Inventor: William Szkrybalo
  • Patent number: 4104462
    Abstract: The present disclosure relates to adenosine nitrates having cardiac activity.
    Type: Grant
    Filed: July 5, 1977
    Date of Patent: August 1, 1978
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Ulf Fischer, Gunther Hausler
  • Patent number: 4102909
    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.
    Type: Grant
    Filed: May 16, 1977
    Date of Patent: July 25, 1978
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Ka-Kong Chan, Gabriel Saucy
  • Patent number: 4102925
    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.
    Type: Grant
    Filed: December 22, 1976
    Date of Patent: July 25, 1978
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Noal Cohen, Gabriel Saucy
  • Patent number: 4102929
    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
  • Patent number: 4103005
    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.
    Type: Grant
    Filed: October 20, 1977
    Date of Patent: July 25, 1978
    Assignee: Hoffmann-La Roche Inc.
    Inventor: Choh Hao Li
  • Patent number: 4102979
    Abstract: A radioimmunoassay for cocaine and the cocaine metabolite benzoylecgonine is described. The assay utilizes a novel labelled compound .sup.125 I-4-hydroxybenzoylecgonine.
    Type: Grant
    Filed: September 22, 1976
    Date of Patent: July 25, 1978
    Assignee: Hoffmann-La Roche Inc.
    Inventor: James Gordon Christenson
  • Patent number: 4101549
    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
  • Patent number: 4100173
    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
  • Patent number: 4100275
    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
  • Patent number: 4100171
    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.
    Type: Grant
    Filed: August 6, 1976
    Date of Patent: July 11, 1978
    Assignee: Hoffmann-La Roche Inc.
    Inventors: John Westley, Chao-Min Liu
  • Patent number: 4100598
    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