Patents Represented by Attorney, Agent or Law Firm Patricia S. Rocha
  • Hydroxymethylimidazodiazepines and their esters
    Patent number: 6174881
    Abstract: The invention is concerned with hydroxymethyl-imidazodiazepines and their esters of general formula I. These compounds can be used as anxiolytic and/or anticonvulsant and/or muscle relaxant and/or sedative-hypnotic active substances.
    Type: Grant
    Filed: September 4, 1997
    Date of Patent: January 16, 2001
    Assignee: Hoffman-La Roche Inc.
    Inventors: Ren{acute over (e)} Borer, Bernd B{umlaut over (u)}ttelmann, Andr{acute over (e)} Szente, Max Gerecke-Jecklin
  • Piperidine derivatives
    Patent number: 6166209
    Abstract: The present invention relates to compounds of the formula ##STR1## wherein X is --O-- or --CH.sub.2 --;Y is --C(O)--, --(CH.sub.2).sub.n -- or --N(CH.sub.3)--;n is 1 or 2 orX and Y taken together are --CH.dbd.CH--Z is --NH--, --CH.sub.2 --, --O-- or .dbd.CH--;A.sup.1 is a group ##STR2## B is --(CH.sub.2).sub.m --; m is 0, 1 or 2;R.sup.1 and R.sup.2 are each independently hydrogen or lower alkyl;R.sup.3 is hydrogen or halogen;R.sup.4 is hydrogen or hydroxy andthe dotted line is (--CH.sub.2 --CH.sub.2 --).sub.n, and n' is 0 or 1 and to pharmaceutically acceptable acid addition salts thereof.The compounds of the present invention are antagonists of the OFQ receptor.
    Type: Grant
    Filed: November 20, 1998
    Date of Patent: December 26, 2000
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Geo Adam, Andrea Cesura, Guido Galley, Fran.cedilla.ois Jenck, Stephan Rover, Jurgen Wichmann
  • 4,5-azolo-oxindoles
    Patent number: 6153634
    Abstract: Disclosed are novel 4,5-azolo-oxindoles having the formula ##STR1## These compounds inhibit cyclin-dependent kinases (CDKs), in particular CDK2. Thus, these compounds and their pharmaceutically acceptable salts, and prodrugs of said compounds, are anti-proliferative agents useful in the treatment or control of cell proliferative disorders, in particular cancer. Also disclosed are pharmaceutical compositions containing these compounds, and methods for the treatment and/or prevention of cancer, particularly in the treatment or control of solid tumors using these compounds, as well as intermediates useful in the preparation of compounds of formula I.
    Type: Grant
    Filed: December 15, 1999
    Date of Patent: November 28, 2000
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Kin-Chun Luk, Christophe Michoud, Steven Gregory Mischke
  • Arylsecocholadiene derivatives
    Patent number: 6153605
    Abstract: Compounds of formula (I) ##STR1## as defined by the specification. The compounds are useful in the treatment or prevention of vitamin D dependent disorders, particularly psoriasis, basal cell carcinomas, disorders of keratinization and keratosis, leukemia, osteoporosis, hyperparathyroidism accompanying renal failure, transplant rejection and graft vs. host disease.
    Type: Grant
    Filed: April 16, 1998
    Date of Patent: November 28, 2000
    Assignee: Hoffman-La Roche Inc.
    Inventors: Pierre Barbier, Franz Bauer, Peter Mohr, Marc Muller, Wolfgang Pirson
  • Antimicrobial compositions
    Patent number: 6150350
    Abstract: The invention relates to antimicrobial compositions comprising a combination of (1) a therapeutically effective amount of a compound of formula I ##STR1## with (2) a second ingredient selected from carbapenem antibiotics or with .beta.-lactamase inhibitors, to the use of the compositions for producing a medicament for the treatment and prophylaxis of infectious diseases, including MRSA infections, and to pharmaceutical compositions containing the combination.
    Type: Grant
    Filed: August 24, 1998
    Date of Patent: November 21, 2000
    Assignee: Hoffman-la Roche Inc.
    Inventors: Peter Angehrn, Ingrid Heinze-Krauss, Malcolm Page, Hans G. F. Richter
  • 4-Alkenyl- and 4-alkynyloxindoles
    Patent number: 6130239
    Abstract: Disclosed are novel 4-alkenyl- and 4-alkynyl oxindoles having the formula ##STR1## and the pharmaceutically acceptable salts thereof, wherein R.sup.1, R.sup.2, R.sup.3, a, b, and X are as defined herein. These compounds inhibit cyclin-dependent kinases (CDKs), in particular CDK2. These compounds and their pharmaceutically acceptable salts, and prodrugs of said compounds, are anti-proliferative agents useful in the treatment or control of cell proliferative disorders, in particular cancer, more particularly, the treatment or control of breast and colon tumors. Also disclosed are pharmaceutical compositions containing the compounds of formula I and II as well as intermediates useful in the preparation of the compounds of formula I and II.
    Type: Grant
    Filed: December 15, 1999
    Date of Patent: October 10, 2000
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Yi Chen, Wendy Lea Corbett, Apostolos Dermatakis, Jin-Jun Liu, Kin-Chun Luk, Paige E. Mahaney, Steven Gregory Mischke
  • Process for the preparation of shikimic acid and its derivatives
    Patent number: 6130354
    Abstract: The present invention discloses a process for the preparation of shikimic acid or its derivatives from quinic acid or its derivatives by dehydration with Vilsmeier reagent. The present invention further discloses intermediates produced by this process and their use in the synthesis of shikimic acid or its derivatives.
    Type: Grant
    Filed: May 10, 1999
    Date of Patent: October 10, 2000
    Assignee: Hoffman-La Roche Inc.
    Inventor: Hans-Jurgen Mair
  • Azulene derivatives
    Patent number: 6121322
    Abstract: The invention provides novel azulene derivatives of general formula I ##STR1## wherein R.sub.1 to R.sub.6 have the significance given in the description, as well as their tautomers, enantiomers, diastereomers, racemates and physiologically compatible salts or esters and substances which are hydrolyzed or metabolized in vivo to compounds of formula I.The invention is also concerned with a process and intermediates for the manufacture of the above compounds, pharmaceutical compositions which contain such compounds as well as the use of these compounds in the treatment of inflammatory conditions.
    Type: Grant
    Filed: November 24, 1998
    Date of Patent: September 19, 2000
    Assignee: Boehringer Mannheim GmbH
    Inventors: Joachim Dickhaut, Walter-Gunar Friebe, Frank Grams, Rainer Haag, Herbert Leinert
  • Method for the preparation of .alpha.-Bromo-Lactam derivatives
    Patent number: 6114541
    Abstract: The invention is concerned with a new process for the preparation of compounds of formula ##STR1## wherein R is hydrogen, lower alkyl, lower alkoxy, cycloalkyl, cycloalkenyl, cycloalkyl-lower alkyl, lower alkenyl, lower alkynyl, aryl, aryl-lower alkyl, heterocyclyl or heterocyclyl-lower alkyl; the lower alkyl, cycloalkyl, lower alkenyl, cycloalkenyl, lower alkynyl, aryl-lower alkyl, aryl and the heterocyclyl moieties being unsubstituted or substituted with at least one group selected from carboxy, amino, carbamoyl, nitro, cyano, lower alkyl, lower alkoxy, hydroxy, halogen, aminomethyl, mercapto, trifluoromethyl and trichloroethyl.The compounds prepared according to above mentioned process are useful in the preparation of cephem, isoxacephem and carbacephem derivatives.
    Type: Grant
    Filed: February 6, 1998
    Date of Patent: September 5, 2000
    Assignee: Hoffmann-La Roche Inc.
    Inventor: Stefan Abrecht
  • Substituted 2,4-diaminopyrimidines
    Patent number: 6114330
    Abstract: The invention is concerned with compounds of formula ##STR1## wherein R.sup.1 is lower-alkoxy, R.sup.2 is hydroxy or lower-alkoxy, R.sup.3 is hydrogen, cyano, alkyl, alkenyl, cycloalkyl, aryl, heterocycyl, aryl-Q-alkyl, or a group of the formula --CR.sup.4 R.sup.4 'COR.sup.5 --, Q is --SO-- or --SO.sub.2 --; R.sup.4, R.sup.4 ' are each independently hydrogen, alkyl, aryl or heterocyclyl, R.sup.5 is hydrogen, alkyl, alkoxy, hydroxy, aryl or heterocycyl, or R.sup.4 and R.sup.5 together form --(CH.sub.2).sub.n --, and n is a whole number between 2 to 5 inclusive and the enantiomers, epimers, and diastereomers thereof, as well as pharmaceutically acceptable salts thereof. These compounds have valuable antibacterial activity.
    Type: Grant
    Filed: February 25, 1998
    Date of Patent: September 5, 2000
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Philippe Guerry, Christian Hubschwerlen, Synese Jolidon, Jean-Luc Specklin, Pierre-Charles Wyss
  • 5'-deoxy-cytidine derivatives
    Patent number: 6114520
    Abstract: Novel 5'-deoxy-cytidine derivatives represented by the general formula (I) ##STR1## wherein R.sup.1 is a hydrogen atom or a group easily hydrolyzable under physiological conditions; R.sup.2 is a hydrogen atom, or --CO--OR.sup.4 group [wherein R.sup.4 is a saturated or unsaturated, straight or branched hydrocarbon group consisting of one to fifteen carbon atoms, or a group of the formula --(CH.sub.2).sub.n --Y (in which Y is cyclohexyl or phenyl; n is an integer from 0 to 4)]; R.sup.3 is a hydrogen atom, bromo, iodo, cyano, a C.sub.1-4 alkyl group [which may be substituted with halogen atom(s)], a vinyl or ethynyl group [which may be substituted with halogen atom(s), C.sub.1-4 alkyl, cycloalkyl, aralkyl, or aromatic ring which may have one or more hetero atom(s)], or an aralkyl group which may be substituted for use in medical therapy, especially tumor therapy.
    Type: Grant
    Filed: January 14, 2000
    Date of Patent: September 5, 2000
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Kazuo Hattori, Tohru Ishikawa, Hideo Ishitsuka, Yasunori Kohchi, Nobuhiro Oikawa, Nobuo Shimma, Hitomi Suda
  • 2-amino-bicyclo[3.1.0]hexane-2,6-dicarboxylic acid derivatives and a process for the preparation thereof
    Patent number: 6107342
    Abstract: The present invention relates to the compound of formulae ##STR1## and to a process for the manufacture of compounds of the general formula ##STR2## which are ligands for the metabotropic glutamate receptors of group II, whereinT is tritium;R.sup.1 is hydroxy, lower alkoxy, lower alkenyloxy, benzyloxy, hydrogen, deuterium or tritium;R.sup.11 is hydrogen, deuterium or tritium, hydroxy or amino, andR.sup.2 is hydrogen or tritium, orR.sup.1 and R.sup.2 form a bond.
    Type: Grant
    Filed: August 30, 1999
    Date of Patent: August 22, 2000
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Geo Adam, Philippe Nicolas Huguenin-Virchaux, Vincent Mutel, Heinz Stadler, Thomas Johannes Woltering
  • .beta.-Alkoxyacrylates against malaria
    Patent number: 6084120
    Abstract: The present invention relates to compounds having the formulae ##STR1## wherein R, R.sup.1, R.sup.6, R.sup.7, Rn.sup.8, X, and Z are defined herein, which are useful in the treatment or prophylaxis of malaria. The compounds of the present invention are especially useful in the treatment or prophylaxis of chloroquine-sensitive and chloroquine-resistant malaria.
    Type: Grant
    Filed: June 22, 1998
    Date of Patent: July 4, 2000
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Jawad Alzeer, Jacques Chollet, Christian Hubschwerlen, Hugues Matile, Robert George Ridley
  • Octahydro phenanthridine derivatives useful as NMDA-R receptor subtype blockers
    Patent number: 6071929
    Abstract: The present invention relates to the use of tetrahydroisoquinoline derivatives of the general formula: ##STR1## wherein: A is arylR.sup.1 is hydrogen, hydroxy, lower alkyl, lower alkoxy, R--CO-- or R--COO--, wherein R is lower alkyl;R.sup.2 is hydrogen, lower alkyl or cycloalkylR.sup.3 -R.sup.7 are independently hydrogen, lower alkyl, lower alkoxy, hydroxy orR.sup.3 and R.sup.4 taken together are --(CH.sub.2).sub.n -- orR.sup.6 and R.sup.7 taken together are --OCH.sub.2 O-- andn is 3 or 4,as well as pharmaceutically acceptable salts for the manufacture of medicaments for the control or treatment of diseases which represent therapeutic indications for NMDA receptor subtype specific blockers.
    Type: Grant
    Filed: May 26, 1999
    Date of Patent: June 6, 2000
    Assignee: Hoffman-La Roche Inc.
    Inventors: Alexander Alanine, Anne Bourson, Bernd Buttelmann, Gunther Fischer, Marie-Paule Heitz Neidhart, Vincent Mutel, Emmanuel Pinard, Stephan Rover, Gerhard Trube, Rene Wyler
  • 1,3,8-triazaspiro[4,5]decan-4-one derivatives
    Patent number: 6071925
    Abstract: The present invention relates to compounds of the formula ##STR1## wherein R.sup.1 and R.sup.2 are each independently hydrogen, lower alkyl, lower alkoxy or halogen;R.sup.3 is phenyl, which is unsubstituted or substituted by lower alkyl, CF.sub.3, lower alkoxy or halogen;R.sup.4 is hydrogen, lower alkyl, lower alkenyl, --C(O)-lower alkyl, --C(O)-phenyl, lower alkyl-C(O)-phenyl, lower alkylene-C(O)O-lower alkyl, lower alkantriyl-di-C(O)O-lower alkyl, hydroxy-lower alkyl, lower alkyl-O-lower alkyl, lower alkyl-CH(OH)CF.sub.3, phenyl or benzyl,R.sup.5 and R.sup.6 are each independently hydrogen, phenyl, lower alkyl or di-lower alkyl or R.sup.5 and R.sup.6 together with the carbon atoms to which they are bound form a phenyl ring, orR.sup.5 and one of R.sup.1 or R.sup.
    Type: Grant
    Filed: January 20, 1998
    Date of Patent: June 6, 2000
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Geo Adam, Andrea Cesura, Guido Galley, Fran.cedilla.ois Jenck, Frederick Monsma, Jr., Stephan Rover, Jurgen Wichmann
  • Heterocyclic vinyl ethers
    Patent number: 6054588
    Abstract: The compounds of the formula ##STR1## wherein R signifies halogen or lower alkyl;n signifies 0-3;R.sup.1 signifies lower alkyl; cycloalkyl; benzyl optionally substituted by hydroxy, halogen, lower alkoxy or lower alkyl; benzoyl optionally substituted by amino, lower alkyl-amino or di-lower alkylamino; acetyl or cycloalkyl-carbonyl; and ##STR2## signifies an aromatic 5-membered residue which is bonded via a N-atom and which contains further 1-3 N atoms in addition to the linking N atom,as well as their pharmaceutically acceptable salts as therapeutically active substances, especially for the control or prevention of acute and/or chronic neurological disorders.
    Type: Grant
    Filed: May 4, 1999
    Date of Patent: April 25, 2000
    Assignee: Hoffman-La Roche Inc.
    Inventors: Geo Adam, Sabine Kolczewski, Vincent Mutel, Heinz Stadler, Jurgen Wichmann, Thomas Johannes Woltering
  • Substituted pyrroles
    Patent number: 6048887
    Abstract: Certain substituted pyrroles are antiproliferative agents useful in the treatment of cancer.
    Type: Grant
    Filed: March 16, 1999
    Date of Patent: April 11, 2000
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Urvashi Hooda Dhingra, Donna Mary Huryn, June Ke, Giuseppe Federico Weber
  • Vitamin D derivatives
    Patent number: 6043385
    Abstract: The present invention relates to vitamin D derivatives of the formula I ##STR1## wherein X is C.dbd.CH.sub.2 or CH.sub.2 ;Y is hydrogen, fluorine or hydroxyZ is hydroxyn is 1 or 2R.sup.1 is lower alkyl,R.sup.2 is a branched alkyl having 3 to 8 carbon atoms which is unsubstituted or substituted with one or more halogen or OH substituents, or is a phenyl group which is unsubstituted or substituted with a branched alkyl having 3 to 8 carbon atoms which is unsubstituted or substituted with one or more halogen or OH substituents;and the dotted carbon-carbon bond in ring D is --C--C-- or --C.dbd.C--; or a pharmaceutically usable salt thereof.
    Type: Grant
    Filed: December 1, 1998
    Date of Patent: March 28, 2000
    Assignee: Hoffman-La Roche Inc.
    Inventors: Pierre Barbier, Franz Bauer, Peter Mohr, Marc Muller, Wolfgang Pirson
  • 1,3,8,-triaza spiro (4,5)decan-4-on derivatives
    Patent number: 6043366
    Abstract: The present invention relates to compounds of formula I and pharmaceutically acceptable acid addition salts thereof.
    Type: Grant
    Filed: December 3, 1998
    Date of Patent: March 28, 2000
    Assignee: Hoffman-La Roche Inc.
    Inventors: Geo Adam, Andrea Cesura, Caido Galley, Fran.cedilla.ois Jenck, Stephan Rover, Jurgen Wichmann
  • Synthesis of 3-epi vitamin D.sub.3 metabolites and analogs
    Patent number: 6040461
    Abstract: The invention relates to a process for the preparation of vitamin D.sub.3 compounds of formula I. ##STR1## Wherein A is a single or a double bond; B is a single, cis-double, trans double or a triple bond; R.sub.1 and R.sub.2 are independently hydrogen, a lower alkyl, e.g., a C.sub.1 -C.sub.4 alkyl; R.sub.3 and R.sub.4 are independently a lower alkyl, e.g., C.sub.1 -C.sub.4 alkyl, a hydroxyalkyl, and a haloalkyl, e.g., a fluoroalkyl; and X and Y are independently hydrogen or hydroxy in the case when B is a single or a double bond.
    Type: Grant
    Filed: May 11, 1999
    Date of Patent: March 21, 2000
    Assignees: Hoffmann-La Roche Inc., Syntex (U.S.A.)
    Inventors: Andrew David Batcho, Percy Sarwood Manchand, Milan Radoje Uskokovic