Patents by Inventor Andor Furst

Andor Furst has filed for patents to protect the following inventions. This listing includes patent applications that are pending as well as patents that have already been granted by the United States Patent and Trademark Office (USPTO).

  • Patent number: 4691032
    Abstract: The invention is concerned with a process for the preparation of 1 hydrogen or hydroxy cholesterol derivatives and intermediates therefor. The compounds of the present invention are useful as intermediates in the preparation of 24,25-dihydroxy and 1.alpha.,24,25-trihydroxycholecalciferol.
    Type: Grant
    Filed: November 1, 1985
    Date of Patent: September 1, 1987
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Andor Furst, Ludwig Labler, Werner Meier
  • Patent number: 4578475
    Abstract: The novel D-homosteroids of the formula ##STR1## wherein R.sup.1 represents a --CN, .dbd.NOH or .dbd.CH--NHOH group; R.sup.2 represents oxo or, where R.sup.1 represents a --CN group, R.sup.2 represents oxo or a --OAc group; or R.sup.1 and R.sup.2 together with carbon atoms 2 and 3 of the steroid skeleton represents a [2,3-d]-fused isoxazole ring, a [3,2-c]-fused pyrazole ring, a [3,2-c]-fused N-acylated pyrazole ring or a [2,3-c]-fused furazan ring; Ac represents an acyl group; R.sup.3 and R.sup.4 represent methyl and R.sup.5 and R.sup.6 together represent an additional bond between carbon atoms 5 and 6 of the steroid skeleton; or R.sup.4 and R.sup.5 together represent --O--, R.sup.3 represents hydrogen or methyl, and R.sup.6 represents hydrogen; R.sup.7 represents hydrogen, lower-alkyl or ethynyl; R.sup.8 represents hydroxy or acyloxy; or R.sup.7 and R.sup.
    Type: Grant
    Filed: January 26, 1984
    Date of Patent: March 25, 1986
    Assignee: Hoffman-La Roche Inc.
    Inventors: Andor Furst, Marcel Muller, Ulrich Kerb, Rudolf Wiechert
  • Patent number: 4568491
    Abstract: The invention is concerned with a process for the preparation of 1 hydrogen or hydroxy cholesterol derivatives and intermediates therefor. The compounds of the present invention are useful as intermediates in the preparation of 24,25-dihydroxy and 1.alpha., 24,25-trihydroxycholecalciferol.
    Type: Grant
    Filed: February 27, 1984
    Date of Patent: February 4, 1986
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Andor Furst, Ludwig Labler, Werner Meier
  • Patent number: 4492797
    Abstract: The present disclosure is directed to 5-oxo- or methylene 17.beta.-hydroxy saturated or unsaturated deA-steroids wherein the 17.alpha.-position contains a propionic acid or propanol substituent and derivatives thereof wherein the hydroxy group at the 17-position forms a lactone ring with the carboxy substituent when the substituent at position 21 is carboxy. The deA-steroids and derivatives of the present disclosure are useful as potassium-sparing diuretics or for flushing oedemas.
    Type: Grant
    Filed: October 4, 1982
    Date of Patent: January 8, 1985
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Andor Furst, Peter Keller, Marcel Muller
  • Patent number: 4361578
    Abstract: The invention is directed to 3-oxo-D-homosteroids and derivatives thereof which are useful as antiantigens.
    Type: Grant
    Filed: November 16, 1981
    Date of Patent: November 30, 1982
    Inventors: Leo Alig, Andor Furst, Peter Keller, Marcel Muller, Ulrich Kerb, Rudolf Wiechert
  • Patent number: 4348327
    Abstract: 17.alpha.-hyroxy- and 17a.alpha.-hydroxy-D-homoetiocarboxylic acids of the formula ##STR1## wherein n is 1 or 2,A is ##STR2## and R.sub.1 is H or CH.sub.3are prepared by hydrating the corresponding 17-nitriles with a mixture of a lower carboxylic acid and its anhydride in the presence of perchloric acid. The resultant 17.beta.-N-acylcarboxamide is then treated with an alkali metal hydroxide in a polyhydric alcohol at an elevated temperature. The product acids are intermediates, e.g., for the production of steroids having antiinflammatory activity.
    Type: Grant
    Filed: June 23, 1981
    Date of Patent: September 7, 1982
    Assignee: Schering Aktiengesellschaft
    Inventors: Robert Nickolson, Ulrich Kerb, Rudolf Wiechert, Leo Alig, Andor Furst, Marcel Muller
  • Patent number: 4312812
    Abstract: The present disclosure is directed to a process for the preparation of cholesterol derivatives from corresponding 21-hydroxymethyl steroidal compounds.
    Type: Grant
    Filed: January 19, 1981
    Date of Patent: January 26, 1982
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Andor Furst, Ludwig Labler, Werner Meier
  • Patent number: 4305881
    Abstract: A process for the synthesis of 1.alpha.,3.beta.-dihydroxy-.DELTA..sup.5 -steroids from steroids such as 1.alpha.,2.alpha.-epoxy-cholesta-4,6-dien-3-one, which is reacted with lithium in liquid ammonia in the absence of a proton donator and subsequently reduced by repeated alternative additions of a proton donator, said additions being followed in each case by an equivalent amount of lithium. The final product, a 1.alpha.,3.beta.-dihydorxy-.DELTA..sup.5 -steroid, is useful in the synthesis of derivatives of cholecalciferol.
    Type: Grant
    Filed: November 13, 1979
    Date of Patent: December 15, 1981
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Andor Furst, Ludwig Labler, Werner Meier
  • Patent number: 4285880
    Abstract: D-Homopregnanes of the formula ##STR1## wherein X is hydrogen, Y is hydroxy or X and Y taken together denote an oxygen to carbon bond; R.sup.6 is hydrogen, R.sup.7 is hydrogen, lower alkanoylthio or aroylthio, or R.sup.6 and R.sup.7 taken together denote a carbon to carbon bond and the dotted line in the 1,2-position of the A-ring together with the corresponding solid line denotes a single or double carbon to carbon bond or a pharmaceutically acceptable basic addition salt thereof when Y is hydroxy having diuretic activity are disclosed.
    Type: Grant
    Filed: October 5, 1979
    Date of Patent: August 25, 1981
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Andor Furst, Peter Keller, Marcel Muller
  • Patent number: 4272630
    Abstract: The present invention is directed to 3-oxo, 6,9-hydro or halo, 11-oxo or (.alpha.--H,.beta.--OH), 17a-alkanoyloxy, 17a.beta.-carboxylate D-homosteroids which are useful as antiinflammatory agents.
    Type: Grant
    Filed: January 11, 1980
    Date of Patent: June 9, 1981
    Inventors: Leo Alig, Andor Furst, Marcel Muller, Ulrich Kerb, Klaus Kieslich, Rudolf Wiechert
  • Patent number: 4252729
    Abstract: The present disclosure is concerned with 9.alpha.-chloro-17-(m-iodobenzyloxy) steroids and a process for their manufacture. The subject compounds are useful as intermediates in the synthesis of pharmacologically-active substances and have themselves been found to exhibit pharmacological activity.
    Type: Grant
    Filed: May 7, 1979
    Date of Patent: February 24, 1981
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Leo Alig, Andor Furst, Marcel Muller, Ulrich Kerb, Rudolf Wiechert
  • Patent number: 4202823
    Abstract: D-Homopregnanes of the formula ##STR1## wherein X is hydrogen, Y is hydroxy or X and Y taken together denote an oxygen to carbon bond; R.sup.6 is hydrogen, R.sup.7 is hydrogen, lower alkanoylthio or aroylthio, or R.sup.6 and R.sup.7 taken together denote a carbon to carbon bond and the dotted line in the 1,2-position of the A-ring together with the corresponding solid line denotes a single or double carbon to carbon bondor a pharmaceutically acceptable basic addition salt thereof when Y is hydroxy having diuretic activity are disclosed.
    Type: Grant
    Filed: June 30, 1978
    Date of Patent: May 13, 1980
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Andor Furst, Peter Keller, Marcel Muller
  • Patent number: 4202841
    Abstract: D-Homopregnanes of the formula ##STR1## wherein the dotted line in the 1,2-position together with the corresponding solid line denotes a single or double carbon-carbon bond; R.sup.6 is hydrogen, fluoro, chloro or methyl; R.sup.9 is hydrogen, fluoro, chloro or bromo; R.sup.11 is hydroxyl, acyloxy, fluoro or chloro; and R.sup.17a is hydroxyl or acyloxy with the proviso that when R.sup.9 is fluoro, chloro or bromo and R.sup.11 is fluoro or chloro, the atomic number of R.sup.11 is less than or equal to that of R.sup.9 ; and with the further proviso that when R.sup.6 is hydrogen, and R.sup.11 and R.sup.17a are hydroxy or when R.sup.6 is fluoro, R.sup.11 and R.sup.17a are hydroxyl and the dotted line in the 1,2-position together with the corresponding solid line denotes a single carbon-carbon bond, R.sup.9 is fluoro, chloro or bromo and processes for the preparation thereof are disclosed.
    Type: Grant
    Filed: December 26, 1978
    Date of Patent: May 13, 1980
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Leo Alig, Andor Furst, Marcel Muller, Ulrich Kerb, Klaus Kieslich, Rudolf Wiechert
  • Patent number: 4197406
    Abstract: The present disclosure is concerned with 17a-(m-iodobenzoyloxy) substituted D-homosteroids and a process for their manufacture. The compounds are useful as intermediates and also as hormonal agents, particularly progestational agents.
    Type: Grant
    Filed: May 7, 1979
    Date of Patent: April 8, 1980
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Leo Alig, Andor Furst, Marcel Muller, Ulrich Kerb, Rudolf Wiechert
  • Patent number: 4193921
    Abstract: The present invention relates to pregnane derivatives of the formula ##STR1## wherein R.sup.1 and R.sup.3 are hydroxyl groups or readily cleavable etherified or esterified hydroxyl groups and R.sup.20 is hydroxymethyl or readily cleavable etherified or esterified hydroxy methyl, formyl, carboxyl or carbalkoxy useful as intermediates for the preparation of 1.alpha.-hydroxycholecalciferols. The present invention also relates to processes for the preparation of the pregnane derivatives and the intermediates thereof.
    Type: Grant
    Filed: October 12, 1977
    Date of Patent: March 18, 1980
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Andor Furst, Ludwig Labler, Werner Meier
  • Patent number: 4155918
    Abstract: The present disclosure relates to novel D-homosteroids. More particularly, the invention is concerned with hormonally active novel D-homosteroids, a process for the manufacture thereof and pharmaceutical preparations containing same.
    Type: Grant
    Filed: March 16, 1978
    Date of Patent: May 22, 1979
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Andor Furst, Marcel Muller, Ulrich Kerb, Rudolf Wiechert
  • Patent number: 4140700
    Abstract: D-Homopregnanes of the formula ##STR1## wherein X is hydrogen, Y is hydroxy or X and Y taken together denote an oxygen to carbon bond and the dotted line in the 1,2-position of the A-ring together with the corresponding solid line denotes a single or double carbon-to-carbon bond or a pharmaceutically acceptable basic addition salt thereof when Y is hydroxy having diuretic activity are disclosed.
    Type: Grant
    Filed: December 16, 1977
    Date of Patent: February 20, 1979
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Andor Furst, Peter Keller, Marcel Muller
  • Patent number: 4139716
    Abstract: The present disclosure relates to D-homosteroids. More particularly, the disclosure is concerned with 19-nor-D-homopregnanes, a process for the manufacture thereof and pharmaceutical preparations containing same.
    Type: Grant
    Filed: March 25, 1976
    Date of Patent: February 13, 1979
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Andor Furst, Jurg A. W. Gutzwiller, Marcel Muller, Ulrich Kerb, Rudolf Wiechert
  • Patent number: 4137269
    Abstract: The present disclosure relates to steroids. More particularly, the disclosure is concerned with D-homosteroids, a process for the manufacture thereof and pharmaceutical preparations containing same. The subject D-homosteroids have high endocrinal activity and are particularly active as anti-inflammatory agents.
    Type: Grant
    Filed: October 12, 1976
    Date of Patent: January 30, 1979
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Leo Alig, Andor Furst, Marcel Muller, Ulrich Kerb, Klaus Kieslich, Rudolf Wiechert
  • Patent number: 4131655
    Abstract: D-homopregnanes of the formula ##STR1## wherein R.sup.6 is hydrogen, chloro, fluoro or methyl; X is .beta.-hydroxymethylene or carbonyl; R.sup.17a is hydroxy, lower alkanoyloxy or aroyloxy; R.sup.21 is hydrogen, chloro, fluoro, hydroxy, lower alkanoyloxy, aroyloxy, sulfate or phosphate; and the dotted line in the 1,2-position of the A-ring denotes an additional carbon-carbon bondAnd pharmaceutically acceptable salts thereof, processes for the preparation thereof and pharmaceutical compositions containing them as the active ingredient are disclosed. The D-homopregnanes of the present invention exhibit hormonal activity and are useful for the treatment of inflammation.
    Type: Grant
    Filed: April 20, 1978
    Date of Patent: December 26, 1978
    Assignee: Hoffman-La Roche Inc.
    Inventors: Leo Alig, Andor Furst, Marcel Muller, Ulrich Kerb, Rudolf Wiechert