Patents Represented by Attorney, Agent or Law Firm Robert A. Silverman
  • Patent number: 5389653
    Abstract: Catechol derivatives of the formula ##STR1## wherein Ra, Rb and Rc have the significance given herein, the ester and ether derivatives thereof which are hydrolyzable under physiological conditions and the pharmaceutically acceptable salts thereof are described and possess valuable pharmacological properties. In particular, they inhibit the enzyme catechol-O-methyltransferase (COMT), a soluble, magnesium-dependent enzyme which catalyses the transference of the methyl group of S-adenosylmethionine to a catechol substrate, whereby the corresponding methyl ethers are formed. Suitable substrates which can be O-methylated by COMT and which can thus be deactivated are, for example, extraneuronal catecholamines and exogeneously-administered therapeutically active substances having a catechol structure.Formula Ia above embraces not only compounds which form part of the invention, but also known compounds; the compounds which form part of the invention can be prepared according to known methods.
    Type: Grant
    Filed: April 16, 1993
    Date of Patent: February 14, 1995
    Assignee: Hoffman-La Roche Inc.
    Inventors: Karl Bernauer, Janos Borgulya, Hans Bruderer, Mose Da Prada, Gerhard Zurcher
  • Patent number: 5384314
    Abstract: This invention is for 1.alpha.-fluoro-25-hydroxy-16-ene-23-yne-cholecalciferol, which can be further characterized by the formula: ##STR1## and which is useful as an agent for the treatment of sebaceous gland diseases such as acne and sebhorreic dermatitis.
    Type: Grant
    Filed: March 11, 1994
    Date of Patent: January 24, 1995
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Thomas I. Doran, Shian-Jan Shiuey, Milan R. Uskokovic
  • Patent number: 5374727
    Abstract: A process for the asymmetric hydrogenation of 6,7-dihydropyrido[1,2-a]indole-8-methanol or its aromatically-substituted derivatives of the formula ##STR1## wherein R.sup.1, R.sup.2 and R.sup.3 each, independently, is hydrogen, halogen, C.sub.1-7 -alkyl, C.sub.1-7 -haloalkyl, hydroxy, C.sub.1-7 -alkoxy, C.sub.1-7 -alkylthio, C.sub.1-7 -alkylsulfinyl, C.sub.1-7 -alkylsulfonyl, nitro, amino or acylamino, to (S)- or (R)-compounds of the formula ##STR2## wherein R.sup.1, R.sup.2 and R.sup.3 have the significances given above and the asterisk (*) denotes the chiral center, carried out using optically active rhodium-diphosphine complexes as catalysts, is described. The production of the compounds II, which also form an object of the invention, is also described. The compounds I and II are valuable intermediates, for example, for the preparation of pharmaceutically active substances.
    Type: Grant
    Filed: May 27, 1993
    Date of Patent: December 20, 1994
    Assignee: Hoffmann-La Roche Inc.
    Inventor: Emil A. Broger
  • Patent number: 5371230
    Abstract: Compounds of the formula ##STR1## wherein R.sup.1 signifies a straight-chain alkyl group with 7 to 9 carbon atoms; and R.sup.2 represents a straight-chain alkyl group with 6 to 11 carbon atoms.their manufacture, liquid crystalline mixtures which contain these compounds and their use for electro-optical purposes.
    Type: Grant
    Filed: November 29, 1993
    Date of Patent: December 6, 1994
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Jurg Funfschilling, Stephen Kelly, Alois Villiger
  • Patent number: 5362738
    Abstract: The pyridone derivatives of the formula ##STR1## wherein Ra is hydrogen or halogen, Rb is --OR.sup.1 or --NR.sup.2 R.sup.3 ; R.sup.1 is an unsubstituted lower alkyl or a lower alkyl substituted by hydroxy, lower alkoxy, amino, lower alkylamino, di(lower alkyl)amino, di(lower alkyl)carbamoyl or lower alkoxycarbonylamino; R.sup.2 is hydrogen or a lower alkyl group which is unsubstituted or substituted by hydroxy, lower alkoxy, amino, lower alkylamino, di(lower alkyl)-amino, di(lower alkyl)carbamoyl or lower alkoxycarbonyl-amino; and R.sup.3 is hydrogen or lower alkyl optionally unsubstituted or mono- or disubstituted by lower alkyl, hydroxy, lower alkoxy, lower hydroxyalkyl, lower alkoxyalkyl or phenyl; B and the carbon atom denoted by .alpha. taken together is a group of the formula >C.sub..alpha. --CR.sup.4 .dbd.CH--CH.dbd.CH-- and R.sup.4 is hydrogen, fluorine or chlorine, that can be used for the control or treatment of muscle tension, stress, insomnia, anxiety and/or convulsions.
    Type: Grant
    Filed: June 1, 1993
    Date of Patent: November 8, 1994
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Serge Burner, Ulrich Widmer
  • Patent number: 5356563
    Abstract: Optically active compounds of the formula ##STR1## wherein m stands for the number 1 and R.sup.2 is an unsubstituted or halogen-substituted alkyl or alkenyl group in which optionally one methylene group is replaced by oxygen and/or optionally one methylene group is replaced by an ester group --COO-- or --OOC--; or m stands for the number 0 or 1 and R.sup.2 denotes a group of the formula ##STR2## R.sup.1 and R.sup.3 each independently represent an alkyl or alkenyl group in which optionally one methylene group is replaced by oxygen; Z.sup.1, Z.sup.2 and Z.sup.3 each independently are a single covalent bond, --CH.sub.2 O--, --OCH.sub.2 --, --CH.sub.2 CH.sub.2 --, --COO-- or --OOC--; n stands for the number 0 or 1; rings A.sup.1 and A.sup.2 each independently are unsubstituted or halogen, cyano and/or methyl-substituted 1,4-phenylene in which optionally 1 CH group or 2 CH groups is/are replaced by nitrogen; and C.sup.* denotes a chiral carbon atom; with the proviso that simultaneously R.sup.
    Type: Grant
    Filed: June 9, 1993
    Date of Patent: October 18, 1994
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Richard Buchecker, Stephen Kelly, Frans Leenhouts
  • Patent number: 5344843
    Abstract: The invention relates to compounds of the formula ##STR1## wherein R.sub.1, R.sub.2, R.sub.2 ' X, Y, Z, A, B, Q and n are as described herein. Their pharmaceutically acceptable salts, and when appropriate, enantiomers, racemates, diastereomers or mixtures thereof or geometric isomer or mixtures thereof, and pharmaceutically acceptable salts thereof. The compounds of formula I inhibit enzyme carnitine acyltransferase 1 (CAT-1) and are therefore useful in the prevention of injury to ischemic tissue, and can limit infarct size, improve cardiac function and prevent arrhythmias during and following a myocardial infarction.
    Type: Grant
    Filed: March 13, 1992
    Date of Patent: September 6, 1994
    Assignee: Hoffman-La Roche Inc.
    Inventors: Robert W. Guthrie, John G. Mullin, Jr., David F. Kachensky, Richard W. Kierstead, Jefferson W. Tilley, Guy P. Heathers, Alan J. Higgins, Ronald A. LeMahieu
  • Patent number: 5335303
    Abstract: An optical frequency conversion element has a wave-guiding layer which consists of a .chi..sup.(2) -active ferroelectric liquid crystal. The monomeric or polymeric liquid crystal material has a periodic structure which permits the so-called quasi phase matching of a guided laser beam. The period length of the structure is equal to twice the coherence length l.sub.c =.pi./.DELTA..beta. of the material, whereby .DELTA..beta.=.beta..sub.o (2.omega.)-2.beta..sub.o (.omega.), with .omega.=angular frequency of the fundamental wave, 0=zero-order mode and .beta.=propagation constant of the mode.
    Type: Grant
    Filed: August 5, 1993
    Date of Patent: August 2, 1994
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Richard Buchecker, Xin H. Chen, Jurg Funfschilling, Rolf-Peter Herr, Martin Schadt, Klaus Schmitt
  • Patent number: 5333717
    Abstract: An apparatus for automatically separating cuvettes supplied in bulk form to an analytical instrument, the cuvettes being suitable for the performance of photometric measurements on samples contained in the cuvettes. To automatically separate cuvettes, the apparatus contains a receiving station for receiving the cuvettes in bulk form. It also includes a device for separating cuvettes, the device having an inlet through which disordered cuvettes can be supplied to the device, and an outlet through which individual cuvettes successively leave the device. A device is provided for conveying disordered cuvettes from the receiving station to the inlet of the device for separation of the cuvettes.
    Type: Grant
    Filed: April 19, 1993
    Date of Patent: August 2, 1994
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Burkard Rosenberg, Gottlieb Schacher
  • Patent number: 5328637
    Abstract: Compounds of the formula ##STR1## and liquid crystalline mixtures containing same.
    Type: Grant
    Filed: February 18, 1992
    Date of Patent: July 12, 1994
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Richard Buchecker, Martin Schadt
  • Patent number: 5326769
    Abstract: The compound (S)-1-[(10-chloro-6,7-dihydro-4-oxo-3-phenyl-4H-benzo[a]quino-lizin-1-yl)c arbonyl]-3-ethoxypyrrolidine of the formula ##STR1## which has valuable pharmacological properties, is described. In particular, the compound of formula I has a non-sedating, hypnotic, that is, sleep-promoting, activity and can accordingly be used for the treatment of sleep disorders.
    Type: Grant
    Filed: March 24, 1993
    Date of Patent: July 5, 1994
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Richard R. Scherschlicht, Ulrich Widmer
  • Patent number: 5326497
    Abstract: Compounds of the general formula ##STR1## wherein R.sup.1 is C.sub.5-12 -alkyl or C.sub.5-12 -alkenyl;R.sup.2 is C.sub.1-9 -alkyl or C.sub.2-9 -alkenyl; provided that at least one of groups R.sup.1 and R.sup.2 is alkenyl;X is a CH group or nitrogen;n is either 0 or 1;q is a whole number between 2 to 6 inclusive;r is either 0 or 1 provided that the sum of q and r at least 3,s is either 0 or 1; andp is either 1 or 2, provided that n is zero when p is 2;mixtures which contain these compounds as well as the use of these compounds for electro-optical purposes.
    Type: Grant
    Filed: October 2, 1992
    Date of Patent: July 5, 1994
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Richard Buchecker, Stephen Kelly, Martin Schadt
  • Patent number: 5326498
    Abstract: Compounds of the general formula ##STR1## wherein R.sup.1 signifies alkyl or alkenyl with 1 to 12 and, respectively, 2 to 12 carbon atoms, which is unsubstituted or mono- or multiply-substituted with halogen and in which one methylene group can be replaced by --O--;R.sup.2 signifies alkyl or alkenyl with 1 to 12 and, respectively, 2 to 12 carbon atoms, which is unsubstituted or mono- or multiply-substituted with halogen and in which one or more methylene groups can be replaced by --O-- and/or --COO-- or --OOC--;Z.sup.1 signifies a single covalent bond or --CH.sub.2 CH.sub.2 --;A.sup.1, A.sup.2 each independently represent 1,4-phenylene, which is unsubstituted or mono- or multiply-substituted with halogen, or pyridine-2,5-diyl or pyrimidine-2,5-diyl;A.sup.3 represents 1,4-phenylene, which is unsubstituted or mono- or multiply-substituted with halogen, or pyridine-2,5-diyl, pyrimidine-2,5-diyl or trans-1,4-cyclohexylene;n is 0 or 1;with the proviso that at least one of rings A.sup.1, A.sup.2 or A.sup.
    Type: Grant
    Filed: October 30, 1992
    Date of Patent: July 5, 1994
    Assignee: Hoffmann-La Roche Inc.
    Inventor: Stephen Kelly
  • Patent number: 5322638
    Abstract: Compounds of the formula ##STR1## wherein A.sup.1 denotes a single covalent bond and A.sup.2 denotes 1,4-phenylene or trans-1,4-cyclohexylene or A.sup.1 denotes trans-1,4-cyclohexylene and A.sup.2 denotes a single covalent bond; X.sup.1 signifies fluorine or chlorine; X.sup.2 represents fluorine or, when X.sup.1 signifies chlorine, also hydrogen or chlorine; and R.sup.1 signifies 1E-alkenyl with 2 to 12 carbon atoms,their manufacture, liquid crystalline mixtures which contain such compounds and their use for electro-optical purposes.
    Type: Grant
    Filed: March 26, 1992
    Date of Patent: June 21, 1994
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Martin Schadt, Alois Villiger
  • Patent number: 5321021
    Abstract: The compounds are of the class of bi- and tricyclic pyridone derivatives of the formula ##STR1## wherein various substituents are as described in the specification, useful in the control of prevention of muscle tensions, stress conditions, insomnia, anxiety states and/or convulsions.
    Type: Grant
    Filed: April 24, 1991
    Date of Patent: June 14, 1994
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Ulf Fischer, Fernand Schneider, Ulrich Widmer
  • Patent number: 5318964
    Abstract: Hydroxamic acid derivatives of the formula ##STR1## and pharmaceutically acceptable salts thereof, which are collagenase inhibitors useful for the control or prevention of degenerative joint diseases, such as, rheumatoid arthritis and osteoarthritis or for the treatment of invasive tumors, atherosclerosis or multiple sclerosis, are described. Said compounds can be prepared either by hydroxamidating a corresponding carboxylic acid or deprotecting a corresponding benzyloxycarbamoyl compound.
    Type: Grant
    Filed: May 24, 1993
    Date of Patent: June 7, 1994
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Michael J. Broadhurst, Paul A. Brown, William H. Johnson, Geoffrey Lawton
  • Patent number: 5304549
    Abstract: Compounds of the formula ##STR1## wherein A is the group ##STR2## R.sup.1 is hydrogen, amino, protected amino, acylamino or lower alkyl optionally substituted by aryl, hydroxy, protected hydroxy, amino, protected amino, acylamino, maleimido, succinimido, naphthalimido, 2,3-dihydro-1,3-dioxo-1H-benz[d,e]isoquinol-2-yl, carboxy, protected carboxy, carbamoyl, mono(lower alkyl)carbamoyl, di(lower alkyl)carbamoyl, di(lower alkyl)amino, carboxy-lower alkanoylamino, pyrrolidino or morpholino; R.sup.2 is hydrogen or lower alkyl optionally substituted by aryl, amino, protected amino, di(lower alkyl)- amino, guanidino, carboxyl, protected carboxyl, carbamoyl, mono(lower alkyl) carbamoyl, di(lower alkyl)carbamoyl, di(lower alkoxy)phosphinyl, dihydroxyphosphinyl, pyrrolidino, piperidino or morpholino; R.sup.3 is hydrogen or lower alkyl optionally substituted by hydroxy, protected hydroxy, amino or protected amino; R.sup.4 is hydrogen, hydroxy, lower alkoxy or benzyloxy; and R.sup.
    Type: Grant
    Filed: January 21, 1992
    Date of Patent: April 19, 1994
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Michael J. Broadhurst, Paul A. Brown, William H. Johnson, Geoffrey Lawton
  • Patent number: 5297599
    Abstract: A closure or cap for a reagent container for use in an analysis system in which an automatic pipetting device is used for transferring small quantities of reagent from the reagent container to reaction cells. In order to simplify the process of handling the reagent container in an automatic analysis system, the closure is characterized in that it is formed in one piece from a plastic and it has a cylindrical side wall and an annular top wall adjacent the side wall and merging into a conical wall which extends inwards from the inner circle of the top wall and ends in a piercable tip situated on the axis of symmetry of the cylindrical wall.
    Type: Grant
    Filed: March 10, 1992
    Date of Patent: March 29, 1994
    Assignee: Hoffmann-LaRoche Inc.
    Inventor: Rudolf Bucheli