Patents Represented by Attorney Samuel L. Welt
  • Patent number: 4083948
    Abstract: An improved radioimmunoassay for benzodiazepines such as diazepam, chlordiazepoxide, oxazepam, demoxepam and metabolites thereof is disclosed. Such immunoassay employs novel .sup.125 I-labelled 4'-hydroxy derivatives of these compounds as tracer.
    Type: Grant
    Filed: April 4, 1977
    Date of Patent: April 11, 1978
    Assignee: Hoffmann-La Roche, Inc.
    Inventors: Raymond Vincent Davis, Rodney Ian Fryer
  • Patent number: 4083741
    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. Inclued in the scope of the disclosed invention are certain apparatus and methods of manufacture.
    Type: Grant
    Filed: July 27, 1976
    Date of Patent: April 11, 1978
    Assignee: Hoffmann-La Roche, Inc.
    Inventor: Arthur H. Goldberg
  • Patent number: 4082188
    Abstract: Method and apparatus for high-speed automatic inspection and processing of large numbers of solid discrete particular objects such as multicolored capsule dose forms in regard to color and/or defect detection, in which virtually all unacceptable material is isolated and an accurate running and total count of acceptable material is provided. The objects are transported in a number of channels past respective optical heads comprising an electro-optics system, the transport mechanism being arranged to provide signals representative of relative object location. One or more rotary transport drums communicating with the front end of the transport mechanism are also provided to enable additional viewing of the capsules in either or both "end-on" orientations, in order to effect a more complete body of information for defect detection. The electro-optics system is comprised operatively of separate color recognition and shape inspection subsystems.
    Type: Grant
    Filed: June 23, 1976
    Date of Patent: April 4, 1978
    Assignee: Hoffmann-La Roche Inc.
    Inventors: William Charles Grimmell, Gilbert Carl Kaetzel, John Milton Moran, George Michael Zanko
  • Patent number: 4082737
    Abstract: Thymosin fraction 5 has been widely employed recently in the clinical investigation of this thymic hormone. This material is a hormonally active proteinaceous composition which is involved in the regulation of cell-mediated immunity. The present disclosure provides a solid, stable, endotoxin and pyrogen free thymosin fraction 5 composition suitable for reconstitution for injection.
    Type: Grant
    Filed: February 22, 1977
    Date of Patent: April 4, 1978
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Weldon Courtney McGregor, Harold Leon Newmark, Armin Hermann Ramel
  • Patent number: 4081434
    Abstract: Snythetic analogs of .beta.-endorphin having the sequence .beta.-endorphin-(1-5)-(16-31) are disclosed. These compounds are potent opiate agonists and analgesic agents, having activities in excess of the parent compounds. Moreover, the present analogs lack the antigenic determinent site which is believed to reside in residues 6-15 of .beta.-endorphin. Thus the analogs present a substantially reduced risk of inducing an anaphylactic response in a treated individual.
    Type: Grant
    Filed: March 11, 1977
    Date of Patent: March 28, 1978
    Assignee: Hoffmann-La Roche Inc.
    Inventor: Choh Hao Li
  • Patent number: 4081470
    Abstract: Polyene compounds such as vitamin A acetate are prepared by reacting triarylphosphonium salts with aldehydes in a two-phase aqueous-organic solvent system.
    Type: Grant
    Filed: August 4, 1976
    Date of Patent: March 28, 1978
    Assignee: Hoffman-La Roche Inc.
    Inventors: Kuno Schleich, Hansjorg Stoller
  • Patent number: 4080334
    Abstract: The intermediates and processes of this invention provide a new synthetic route for the preparation of pharmaceutically valuable 19-norsteroids. Further, the intermediates and processes of the invention provide a route for the preparation of pharmaceutically valuable estrones. The present invention provides a facile total synthesis of 19.beta.-alkyl-C/D-trans-steroidal materials. This desirable result is obtained via a unique asymmetric induction followed by subsequent stereo-specific reaction steps. As a precursor to the steroidal Ring A, a 3,5-disubstituted-4-isoxazolylmethylene group is employed in this synthesis.
    Type: Grant
    Filed: June 14, 1976
    Date of Patent: March 21, 1978
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Gabriel Saucy, John William Scott
  • Patent number: 4080323
    Abstract: The present invention concerns compounds of the formula ##STR1## wherein X is hydrogen or halogen; R.sub.1 is hydrogen, halogen or trifluoromethyl; R.sub.2 is hydrogen or lower alkyl; and R.sub.3 is hydrogen, --COO lower alkyl or CON(R.sub.4).sub.2 wherein R.sub.4 is lower alkyl or hydrogen and may be differentAnd the pharmaceutically acceptable salts thereof.Also provided are methods for the preparation of these compounds as well as pharmaceutical formulations which contain the active compounds of this invention. The compounds of the formula illustrated above are useful as anxiolytics, anticonvulsants, muscle relaxants and sedative agents.
    Type: Grant
    Filed: March 7, 1977
    Date of Patent: March 21, 1978
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Armin Walser, Rodney Ian Fryer
  • Patent number: 4079127
    Abstract: The amino acid sequence of a biologically active polypeptide hormone isolated from calf thymus termed thymosin .alpha..sub.1 has been determined. Thymosin .alpha..sub.1 is a heat stable acidic molecule composed of 28 amino acid residues. This peptide is one of several present in thymosin fraction 5 which participate in the regulation, differentiation and function of thymic dependent lymphocytes (T cells).
    Type: Grant
    Filed: February 8, 1977
    Date of Patent: March 14, 1978
    Assignees: Board of Regents of the University of Texas, Hoffmann-La Roche, Inc.
    Inventors: Allan L. Goldstein, Teresa L. K. Low, Chun-Yen Lai, Su-Sun Wang
  • Patent number: 4079076
    Abstract: A novel conjugated diene bisfunctionalization process wherein a nitro group and a hydroxyl group in the form of an ester are introduced into the conjugated diene molecule by treatment of conjugated dienes with nitric acid in the presence of an acid anhydride. The novel compounds produced by this process and transformation products thereof, are useful as bactericides and fungicides and valuable organic synthesis intermediates, A novel procedure for the production of nitriles and .gamma.-acetoxytiglic aldehyde is disclosed.
    Type: Grant
    Filed: March 17, 1976
    Date of Patent: March 14, 1978
    Assignee: Hoffmann-La Roche, Inc.
    Inventor: Pius Anton Wehrli
  • Patent number: 4079124
    Abstract: A method of preparing enteric X-ray contrast media particularly suited to the use of high energy X-ray sources are disclosed. The disclosed media comprise hafnium, tantalum, tungsten, oxides or insoluble salts thereof in purified form, mixtures thereof and, more particularly, partially purified ores containing one or more of them in combination with a suitable carrier.
    Type: Grant
    Filed: April 21, 1976
    Date of Patent: March 14, 1978
    Assignee: Medi-Physics, Inc.
    Inventor: Harry S. Winchell
  • Patent number: 4079352
    Abstract: An ultrasonic echo sounding technique for reducing unwanted echoes from reflectors outside the focal line of a focused ultrasonic field is disclosed. In this technique at least two pulse-defined ultrasonic waves are successively transmitted. The amplitudes of the said waves are functions of an angle .phi. which is generated about the axis of the source of ultrasound. Echoes from the reflected waves are received from reflectors both on and outside the focal line and multiplied by an amplitude factor which is a function of the above mentioned angle .phi.. Echo signals associated with echoes having the same transit time are then added together.
    Type: Grant
    Filed: February 23, 1977
    Date of Patent: March 14, 1978
    Assignee: Hoffmann-La Roche, Inc.
    Inventors: Christoph Benedikt Burckhardt, Pierre-Andre Grandechamp, Heinz Hoffmann
  • Patent number: 4077983
    Abstract: Total synthesis of known progestationally active steroidal materials. The steroids can be synthesized depending on the particular starting reactants selected by employing as intermediates bicyclic compounds of the formula ##STR1## wherein m is an integer having a value of 1 or 2; R.sub.4 is hydrogen or lower alkyl; Z is lower alkylenedioxy, CH(OR.sub.2 ) and carbonyl; R.sub.8 when taken alone is hydrogen; R.sub.9 when taken alone is lower alkoxycarbonyl, aryloxy-carbonyl, lower cycloalkyloxycarbonyl, carbonyl-halide, hydrogen, carboxy, formyl and methylene-X, where X is a leaving group and when taken together are methylene; with the proviso that when Z is carbonyl R.sub.8 when taken alone is hydrogen; R.sub.9 when taken alone is carbonyl halide, hydrogen, carboxy, formyl and methylene-X where X is a leaving group and when taken together are methylene and R.sub.
    Type: Grant
    Filed: July 14, 1976
    Date of Patent: March 7, 1978
    Assignee: Hoffmann-La Roche, Inc.
    Inventor: Zoltan George Hajos
  • Patent number: 4078049
    Abstract: A sensitive immunoassay for acetylcholine is described. To prepare the acetylcholine selective antiserum, an antigen is made comprising 6-aminocaproic acid (2-trimethylaminoethyl) ester covalently bonded to an immunogenic carrier material through a peptide bond formed from said 6-amino group and carboxyl groups contained in said immunogenic carrier material and the antigen is injected into a suitable host animal to elicit the desired antiserum.
    Type: Grant
    Filed: February 28, 1977
    Date of Patent: March 7, 1978
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Arthur Martin Felix, Sidney Spector
  • Patent number: 4077985
    Abstract: Dienylphosphates of the formula ##STR1## wherein each of R.sub.1 and R.sub.1 ' is lower alkyl, aryl or benzyl and each of R.sub.2, R.sub.3 and R.sub.4 is hydrogen or lower alkyl,Are useful as anthelmintic agents and as intermediates for enolphosphates having anthelmintic activity.
    Type: Grant
    Filed: February 7, 1977
    Date of Patent: March 7, 1978
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Kaspar F. Burri, Frank Kienzle, Perry Rosen
  • Patent number: 4077978
    Abstract: Isoindole derivatives of the formula ##STR1## wherein R.sub.1 -R.sub.6, A and Z are as hereinafter described. The isoindole derivatives are useful as appetite suppressants.
    Type: Grant
    Filed: August 25, 1976
    Date of Patent: March 7, 1978
    Assignee: Hoffmann-La Roche Inc.
    Inventor: Roland Jaunin
  • Patent number: 4076797
    Abstract: A radioimmunoassay for syphilis using Treponema pallidum reiter variant as the antigen in an indirect procedure is disclosed.
    Type: Grant
    Filed: September 28, 1976
    Date of Patent: February 28, 1978
    Assignee: Hoffmann-La Roche Inc.
    Inventor: Raymond Vincent Davis
  • Patent number: 4076834
    Abstract: Methods of, and compositions for, improving cardiovascular function utilizing as the active agent certain polyether antibiotics, their pharmaceutically acceptable salts and derivatives are disclosed.
    Type: Grant
    Filed: December 19, 1975
    Date of Patent: February 28, 1978
    Assignee: Hoffmann-La Roche Inc.
    Inventor: John Westley
  • Patent number: 4076810
    Abstract: N-oxides of benyzlpyrimidines of the formula ##STR1## wherein R.sup.1, R.sup.2 and R.sup.3 are as set forth hereinafter, ARE DESCRIBED. The 2,4-diamino-5-(4-bromo-3,5-dimethoxybenzyl)-pyrimidine is also described. The compounds referred to above are useful as potentiators of the antibacterial activity of sulfonamides.
    Type: Grant
    Filed: February 18, 1977
    Date of Patent: February 28, 1978
    Assignee: Hoffmann-La Roche Inc.
    Inventor: Ivan Kompis
  • Patent number: 4076739
    Abstract: A synthesis of Vitamin E in racemic or optically active forms from 6-methyl-2-hepten-4-ol; 6,10-dimethyl-2-undecen-4-ol or 6-benzyloxy-2,5,7,8-tetramethyl-chroman-2-acetaldehyde including intermediates in this synthesis.
    Type: Grant
    Filed: December 8, 1976
    Date of Patent: February 28, 1978
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Ka-Kong Chan, Gabriel Saucy