Patents Represented by Attorney Samuel L. Welt
  • Patent number: 4045475
    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: September 15, 1976
    Date of Patent: August 30, 1977
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Ka-Kong Chan, Gabriel Saucy
  • Patent number: 4045487
    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: August 30, 1977
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Roy Cleeland, Jr., Emanuel Grunberg, Willy Leimgruber, Manfred Weigele
  • Patent number: 4045452
    Abstract: A multi-step, stereospecific total synthesis of steroids utilizing intermediates having a cyanoalkyl A-ring precursor is disclosed. The initial starting materials for this process are the relatively inexpensive and commercially available reagents .gamma.-butyrolactone and sodium cyanide. The process is suitable for the preparation of racemic or optically active, medicinally valuable steroids, particularly 19-norsteroids. It is a feature of this process that conditions employed during the multiple step synthesis are selected so as to retain the normally labile nitrile group even during hydrogenation and hydrolysis steps. In this manner, it is possible to employ the nitrile group as an A-ring precursor without resorting to protective groups as wasl heretofore found necessary in previous steroid total synthesis processes.
    Type: Grant
    Filed: December 22, 1975
    Date of Patent: August 30, 1977
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Noal Cohen, Michael Rosenberger, Gabriel Saucy
  • Patent number: 4045476
    Abstract: A total synthesis of canthaxanthin or dinor-canthaxanthin, known food coloring agents, from pentols.
    Type: Grant
    Filed: September 15, 1976
    Date of Patent: August 30, 1977
    Assignee: Hoffmann-La Roche Inc.
    Inventor: Michael Rosenberger
  • Patent number: 4044051
    Abstract: 9-[2-(1-alkoxy-ethyl)-5,5-dimethyl-cyclopent-1-en-1-yl]-3,7-dimethyl-nona-2 ,4,6,8-tetraen acid compounds are disclosed which are useful for the topical or systemic treatment of dermatological disorders.
    Type: Grant
    Filed: July 16, 1975
    Date of Patent: August 23, 1977
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Werner Bollag, Norbert Rigassi, Ulrich Schwieter
  • Patent number: 4044004
    Abstract: The novel 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 novel 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 stereospecific 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: August 23, 1977
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Gabriel Saucy, John William Scott
  • Patent number: 4044005
    Abstract: The compounds 3,3,4,5,6,6-hexahydro-4-(3-esterified or etherified-1-octenyl)-2-oxo-2H-cyclopenta[b]furan-5-oyl peroxides useful as intermediates in the preparation of prostaglandins F.sub.2 .alpha. and E.sub.2 which are known agents for inducing labor and terminating pregnancy.
    Type: Grant
    Filed: October 6, 1976
    Date of Patent: August 23, 1977
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Frank Kienzle, Perry Rosen
  • Patent number: 4044016
    Abstract: Novel preparations of triazolobenzodiazepines are disclosed. Novel 6-pyridyl-4H-triazolo[4,3-a]-1,4-benzodiazepines and novel intermediates are also disclosed which are useful as anticonvulsants, muscle relaxants and sedative agents.
    Type: Grant
    Filed: May 7, 1976
    Date of Patent: August 23, 1977
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Leo Henryk Sternbach, Armin Walser
  • Patent number: 4044022
    Abstract: 15-Oxasteroids of the androstane, pregnane, estrane, and 19-norpregnane series are useful as hormonal agents.
    Type: Grant
    Filed: July 2, 1976
    Date of Patent: August 23, 1977
    Assignee: Hoffmann-La Roche Inc.
    Inventor: Perry Rosen
  • Patent number: 4043937
    Abstract: The halogen derivatives of ascorbic acid and D-araboascorbic acid useful as antioxidants as well as a method for stabilizing oxidation-sensitive organic materials by incorporating said derivatives in oxidation sensitive materials.
    Type: Grant
    Filed: April 28, 1976
    Date of Patent: August 23, 1977
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Joseph Kiss, Klaus Peter Berg
  • Patent number: 4044017
    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 groupAnd acid addition salts thereof.
    Type: Grant
    Filed: November 11, 1976
    Date of Patent: August 23, 1977
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Cedric Herbert Hassall, William Henry Johnson, Antonin Krohn, Carey Ernest Smithen, William Anthony Thomas
  • Patent number: 4044010
    Abstract: Compounds of the formfulas ##STR1## wherein R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, R.sub.6, m and n and X are as hereinafter set forth,Are described. The compounds of formulas I and Ia are useful as neuroleptic agents.
    Type: Grant
    Filed: February 4, 1976
    Date of Patent: August 23, 1977
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Max Gerecke, Jean-Pierre Kaplan, Emilio Kyburz
  • Patent number: 4044028
    Abstract: Homologation of .alpha.,.beta.-polyene unsaturated aldehydes and ketones to form .alpha.,.beta.-unsaturated aldehydes via epoxidation of the ketone or aldehyde and intermediates in this process such as .beta.,.gamma.-unsaturated polyene aldehydes.
    Type: Grant
    Filed: September 15, 1976
    Date of Patent: August 23, 1977
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Michael Rosenberger, Gabriel Saucy
  • Patent number: 4042920
    Abstract: A multiplexed electrical control circuit is provided for use with optical display devices of the type wherein electrical intelligence is translated into optical images of letters or numbers or other patterns through the use of a liquid crystal shutter device fully described in a copending application Ser. No. 136,441, filed Apr. 22, 1971. The shutter device comprises a layer of liquid crystal material sandwiched between opposing parallel plates coated with transparent conducting films. The shutter device, or liquid crystal cell, is disposed between a pair of polarizers such that the application of electrical potential across a character, digit, or other image-defining segment and an opposing position-designating film will cause light to be transmitted or to be cut off, depending upon the orientation of the two polarizers.
    Type: Grant
    Filed: August 12, 1976
    Date of Patent: August 16, 1977
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Thomas B. Harsch, Edd Dems
  • Patent number: 4042682
    Abstract: A morphine-like compound (MLC) can be extracted from the brain of various species by utilizing morphine specific antibodies. MLC shows great similarities to morphine in immunological, chemical and chromatographic tests. The compound has biological activity as it inhibits the electrically induced contractions both of the guinea pig ileum and mouse vas deferens but the inhibition is not reversed by naloxone or naltrexone.
    Type: Grant
    Filed: April 7, 1976
    Date of Patent: August 16, 1977
    Assignee: Hoffmann-La Roche Inc.
    Inventor: Sidney Spector
  • Patent number: 4042597
    Abstract: A method for preparing 2-(2-hydroxy-2-propyl-1-methyl-5-nitroimidazole by the autoxidation of 1-methyl-2-isopropyl-5-nitroimidazole is disclosed.
    Type: Grant
    Filed: March 22, 1976
    Date of Patent: August 16, 1977
    Assignee: Hoffmann-La Roche Inc.
    Inventor: Werner Hofheinz
  • Patent number: 4041058
    Abstract: A synthesis of 2,6,10-trimethyl-undecan-1-ol, an intermediate for producing vitamin E, from methacrolein, crotonaldehyde, .beta.-hydroxy-isobutyric acid including intermediates in this synthesis.
    Type: Grant
    Filed: December 8, 1975
    Date of Patent: August 9, 1977
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Noal Cohen, Gabriel Saucy
  • Patent number: 4041076
    Abstract: New hapten compositions useful in preparing antigens which may be employed in eliciting antibodies useful in an improved radioimmunoassay for pharmacologically active phenethylamines are disclosed. Particular phenethylamins which are preferably detected by the present radioimmunoassay include the catecholamines such as norepinephrine, dopamine and epinephrine, and the amphetamines.
    Type: Grant
    Filed: March 9, 1976
    Date of Patent: August 9, 1977
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Richard William Avenia, James Gordon Christenson, Benjamin Pecherer
  • Patent number: 4041040
    Abstract: A novel derivative of ecgonine is described. This compound, 4-hyroxy-benzoyl ecgonine, is useful as a substrate for iodination with a radioactive isotope of iodine such as .sup.125 I. The resulting radiolabeled compound is useful in a radioimmunoassay for benzoyl ecgonine.
    Type: Grant
    Filed: September 22, 1976
    Date of Patent: August 9, 1977
    Assignee: Hoffmann-La Roche Inc.
    Inventors: James Gordon Christenson, Harvey Gurien, Sidney Teitel
  • Patent number: 4041023
    Abstract: Radiolabelled and isotopically labelled peptides are prepared in a convenient and efficient manner by catalytically tritiating or deuterating an analog of the desired peptide containing one or more amino acid residues having an ethylenic type unsaturated bond therein. Preferred amino acid residues for this purpose include 3,4-dehydroproline (.DELTA..sup.3 -proline) and trans-4,5-dehydrolysine (.DELTA..sup.4 -lysine).
    Type: Grant
    Filed: April 14, 1976
    Date of Patent: August 9, 1977
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Arthur Martin Felix, Arnold Alvin Liebman