Patents by Inventor Alexander Fassler

Alexander Fassler 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: 6451973
    Abstract: The invention relates to compounds of the formula I, in which R1 and R2 are, independently of each other, lower alkyl or lower alkoxy-lower alkyl; R3 and R4 are, independently of each other, sec-lower alkyl or tert-lower alkyl; R5 is phenyl or cyclohexyl; and R6 and R7 are, independently of each other, lower alkyl, or, together with the linking nitrogen atom, pyrrolidino, piperidino, 4-lower alkylpiperidino, 1,2,4-triazol-1-yl or 1,2,4-triazol-4-yl; or a salt thereof, provided that at least one salt-forming group is present. These compounds are inhibitors of HIV protease and are therefore suitable, for example, for treating AIDS or its preliminary stages.
    Type: Grant
    Filed: February 1, 1999
    Date of Patent: September 17, 2002
    Assignee: Novatis AG
    Inventors: Alexander Fässler, Guido Bold, Hans-Georg Capraro, Marc Lang
  • Patent number: 6300519
    Abstract: There are described compounds of formula I*, wherein R1 is lower alkoxycarbonyl, R2 is secondary or tertiary lower alkyl or lower alkylthio-lower alkyl, R3 is phenyl that is unsubstituted or substituted by one or more lower alkoxy radicals, or C4-C8cycloalkyl, R4 is phenyl or cyclohexyl each substituted in the 4-position by unsaturated heterocyclyl that is bonded by way of a ring carbon atom, has from 5 to 8 ring atoms, contains from 1 to 4 hetero atoms selected from nitrogen, oxygen, sulfur, suffinyl (—SO—) and sulfonyl (—SO2—) and is unsubstituted or substituted by lower alkyl or by phenyl-lower alkyl, R5, independently of R2, has one of the meanings mentioned for R2, and R6, independently of R1, is lower alkoxycarbonyl, or salts thereof, provided that at least one salt-forming group is present. The compounds are inhibitors of retroviral aspartate protease and can be used, for example, in the treatment of AIDS.
    Type: Grant
    Filed: November 23, 1999
    Date of Patent: October 9, 2001
    Assignee: Novartis Finance Corporation
    Inventors: Alexander Fässler, Guido Bold, Hans-Georg Capraro, Marc Lang, Satish Chandra Khanna
  • Patent number: 6225345
    Abstract: The invention relates to compounds of formula (I): wherein R1 and R10 are each independently of the other lower alkoxycarbonyl; either R2, R3 and R4 are each independently of the other C1-C4alkyl and R7, R8 and R9 are each selected from hydrogen and C1-C4alkyl, with not more than 2 of the radicals being hydrogen; or R7, R8 and R9 are each independently of the other C1-C4alkyl and R2, R3 and R4 are each selected from hydrogen and C1-C4alkyl, with 1 or 2 of the radicals being hydrogen; R5 is phenyl or cyclohexyl; and R6 is phenyl or cyanophenyl; or salts thereof; those compounds are inhibitors of retroviral aspartate proteases and are effective, for example, against HIV.
    Type: Grant
    Filed: May 21, 1998
    Date of Patent: May 1, 2001
    Assignee: Novartis AG
    Inventors: Alexander Fässler, Guido Bold, Hans-Georg Capraro, Marc Lang
  • Patent number: 6166004
    Abstract: There are described compounds of formula I*, ##STR1## wherein R.sub.1 is lower alkoxycarbonyl,R.sub.2 is secondary or tertiary lower alkyl or lower alkylthio-lower alkyl,R.sub.3 is phenyl that is unsubstituted or substituted by one or more lower alkoxy radicals, or C.sub.4 -C.sub.8 cycloalkyl,R.sub.4 is phenyl or cyclohexyl each substituted in the 4-position by unsaturated heterocyclyl that is bonded by way of a ring carbon atom, has from 5 to 8 ring atoms, contains from 1 to 4 hetero atoms selected from nitrogen, oxygen, sulfur, sulfinyl (--SO--) and sulfonyl (--SO.sub.2 --) and is unsubstituted or substituted by lower alkyl or by phenyl-lower alkyl,R.sub.5, independently of R.sub.2, has one of the meanings mentioned for R.sub.2, andR.sub.6, independently of R.sub.1, is lower alkoxycarbonyl,or salts thereof, provided that at least one salt-forming group is present.The compounds are inhibitors of retroviral aspartate protease and can be used, for example, in the treatment of AIDS.
    Type: Grant
    Filed: September 20, 1999
    Date of Patent: December 26, 2000
    Assignee: Novartis Finance Corporation
    Inventors: Alexander Fassler, Guido Bold, Hans-Georg Capraro, Marc Lang, Satish Chandra Khanna
  • Patent number: 6110946
    Abstract: There are described compounds of formula I*, ##STR1## wherein R.sub.1 is lower alkoxycarbonyl,R.sub.2 is secondary or tertiary lower alkyl or lower alkylthio-lower alkyl,R.sub.3 is phenyl that is unsubstituted or substituted by one or more lower alkoxy radicals, or C.sub.4 -C.sub.8 cycloalkyl,R.sub.4 is phenyl or cyclohexyl each substituted in the 4-position by unsaturated heterocyclyl that is bonded by way of a ring carbon atom, has from 5 to 8 ring atoms, contains from 1 to 4 hetero atoms selected from nitrogen, oxygen, sulfur, sulfinyl (--SO--) and sulfonyl (--SO.sub.2 --) and is unsubstituted or substituted by lower alkyl or by phenyl-lower alkyl,R.sub.5, independently of R.sub.2, has one of the meanings mentioned for R.sub.2, andR.sub.6, independently of R.sub.1, is lower alkoxycarbonyl,or salts thereof, provided that at least one salt-forming group is present.The compounds are inhibitors of retroviral aspartate protease and can be used, for example, in the treatment of AIDS.
    Type: Grant
    Filed: July 1, 1998
    Date of Patent: August 29, 2000
    Assignee: Novartis Finance Corporation
    Inventors: Alexander Fassler, Guido Bold, Hans-Georg Capraro, Marc Lang, Satish Chandra Khanna
  • Patent number: 5935976
    Abstract: Antiretroviral compounds (which are effective, for example, against HIV) of the formula I ##STR1## in which R.sub.
    Type: Grant
    Filed: August 21, 1998
    Date of Patent: August 10, 1999
    Assignee: Novartis Corporation
    Inventors: Guido Bold, Hans-Georg Capraro, Alexander Fassler, Marc Lang, Shripad Subray Bhagwat, Satish Chandra Khanna, Janis Karlis Lazdins, Jurgen Mestan
  • Patent number: 5912352
    Abstract: The invention relates to a novel process for the preparation of compounds of formula I ##STR1## wherein R.sub.1 is hydrogen or a suitable amino-protecting group,R.sub.2 is unsubstituted or substituted alkyl,R.sub.3 is hydrogen, aryl, heterocyclyl, unsubstituted or substituted alkyl or unsubstituted or substituted cycloalkyl,R.sub.4, independently of R.sub.1, is hydrogen or a suitable amino-protecting group andm is a number from 1 to 7; and wherein further suitable protecting groups for functional groups may be present; which compounds are antivirally active or can be used as starting materials for pharmaceutically active, especially antiviral compounds.
    Type: Grant
    Filed: May 30, 1997
    Date of Patent: June 15, 1999
    Assignee: Novartis Finance Corporation
    Inventors: Alexander Fassler, Guido Bold, Hans-Georg Capraro, Heinz Steiner
  • Patent number: 5849911
    Abstract: There are described compounds of formula I*, ##STR1## wherein R.sub.1 is lower alkoxycarbonyl,R.sub.2 is secondary or tertiary lower alkyl or lower alkylthio-lower alkyl,R.sub.3 is phenyl that is unsubstituted or substituted by one or more lower alkoxy radicals, or C.sub.4 -C.sub.8 cycloalkyl,R.sub.4 is phenyl or cyclohexyl each substituted in the 4-position by unsaturated heterocyclyl that is bonded by way of a ring carbon atom, has from 5 to 8 ring atoms, contains from 1 to 4 hetero atoms selected from nitrogen, oxygen, sulfur, sulfinyl (--SO--) and sulfonyl (--SO.sub.2 --) and is unsubstituted or substituted by lower alkyl or by phenyl-lower alkyl,R.sub.5, independently of R.sub.2, has one of the meanings mentioned for R.sub.2, andR.sub.6, independently of R.sub.1, is lower alkoxycarbonyl,or salts thereof, provided that at least one salt-forming group is present.The compounds are inhibitors of retroviral aspartate protease and can be used, for example, in the treatment of AIDS.
    Type: Grant
    Filed: April 9, 1997
    Date of Patent: December 15, 1998
    Assignee: Novartis Finance Corporation
    Inventors: Alexander Fassler, Guido Bold, Hans-Georg Capraro, Marc Lang, Satish Chandra Khanna
  • Patent number: 5807891
    Abstract: Antiretroviral compounds (which are effective, for example, against HIV) of the formula I ##STR1## in which R.sub.
    Type: Grant
    Filed: April 8, 1997
    Date of Patent: September 15, 1998
    Assignee: Novartis AG
    Inventors: Guido Bold, Hans-Georg Capraro, Alexander Fassler, Marc Lang, Shripad Subray Bhagwat, Satish Chandra Khanna, Janis Karlis Lazdins, Jurgen Mestan
  • Patent number: 5753652
    Abstract: The invention relates to compounds of formula ##STR1## and salts, pharmaceutical compositions, intermediates and processes of preparation thereof.
    Type: Grant
    Filed: April 4, 1995
    Date of Patent: May 19, 1998
    Assignee: Novartis Corporation
    Inventors: Alexander Fassler, Guido Bold, Marc Lang, Shripad Bhagwat, Peter Schneider
  • Patent number: 5670497
    Abstract: This invention relates to substituted cyclic carbonyls and derivatives thereof useful as retroviral protease inhibitors to pharmaceutical compositions comprising such compounds, and to methods of using these compounds for treating vital infection.
    Type: Grant
    Filed: January 11, 1996
    Date of Patent: September 23, 1997
    Assignee: Ciba-Geigy Corporation
    Inventors: Guido Bold, Shripad S. Bhagwat, Alexander Fassler, Marc Lang
  • Patent number: 5663200
    Abstract: Antiretroviral compounds (which are effective, for example, against HIV) of the formula I ##STR1## in which R.sub.
    Type: Grant
    Filed: October 19, 1995
    Date of Patent: September 2, 1997
    Assignee: Ciba-Geigy Corporation
    Inventors: Guido Bold, Hans-Georg Capraro, Alexander Fassler, Marc Lang, Shripad Subray Bhagwat, Satish Chandra Khanna, Janis Karlis Lazdins, Jurgen Mestan
  • Patent number: 5643878
    Abstract: Compounds of formula I ##STR1## or their hydroxy-protected derivatives, and compounds of formula I' ##STR2## wherein T is an acyl radical of formula Z ##STR3## wherein R.sup.z is unsubstituted or substituted hydrocarbyl wherein at least one carbon atom has been replaced by a hetero atom with the proviso that a hetero atom is not bonded directly to the carbonyl to which the radical R.sup.z is bonded, alkyl having two or more carbon atoms, lower alkenyl, lower alkynyl, aryl or unsubstituted or substituted amino, and wherein the radicals R.sub.1, B.sub.1, R.sub.2, R.sub.3, A.sub.1, A.sub.2 and NR.sub.4 R.sub.5 are as defined in the description, and precursors thereof, are described. The compounds have pharmaceutical activity, for example in the treatment of retroviral diseases, such as AIDS.
    Type: Grant
    Filed: March 8, 1994
    Date of Patent: July 1, 1997
    Assignee: Ciba-Geigy Corporation
    Inventors: Guido Bold, Marc Lang, Alexander Fassler, Hans-Georg Capraro, Shripad Bhagwat, Peter Schneider, Peter van Hoogevest
  • Patent number: 5409927
    Abstract: There are described compounds of formula I ##STR1## wherein R.sub.1 is hydrogen or lower alkyl,R.sub.2 is hydrogen, lower alkyl, lower alkoxycarbonyl, phenyl- or naphthyl-lower alkoxycarbonyl, heterocyclylcarbonyl wherein heterocyclyl contains 5 or 6 ring atoms, is saturated and is bonded to the carbonyl group via a ring nitrogen atom and, in addition to the bonding nitrogen atom, contains as ring member one or more further hetero atoms selected from unsubstituted or C.sub.1 -C.sub.4 alkyl-substituted NH, O, S, S.dbd.O and SO.sub.2, or is lower alkanoyl, phenyl- or naphthyl-lower alkanoyl or lower alkanesulfonyl,R.sub.3 is morpholino, thiomorpholino, S-oxothiomorpholino or S,S-dioxothiomorpholino, the heterocyclyl radical in heterocyclylcarbonyl R.sub.2 having the same definition as R.sub.3 or having a definition other than R.sub.3, andR.sub.4 is hydrogen, hydroxy, C.sub.1 -C.sub.4 alkoxy, cyano, trifluoromethyl or fluorine, and salts of those compounds where salt-forming groups are present.
    Type: Grant
    Filed: March 25, 1993
    Date of Patent: April 25, 1995
    Assignee: Ciba-Geigy Corporation
    Inventors: Guido Bold, Alexander Fassler, Marc Lang, Peter Schneider