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: 6451973Abstract: 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: GrantFiled: February 1, 1999Date of Patent: September 17, 2002Assignee: Novatis AGInventors: Alexander Fässler, Guido Bold, Hans-Georg Capraro, Marc Lang
-
Patent number: 6300519Abstract: 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: GrantFiled: November 23, 1999Date of Patent: October 9, 2001Assignee: Novartis Finance CorporationInventors: Alexander Fässler, Guido Bold, Hans-Georg Capraro, Marc Lang, Satish Chandra Khanna
-
Patent number: 6225345Abstract: 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: GrantFiled: May 21, 1998Date of Patent: May 1, 2001Assignee: Novartis AGInventors: Alexander Fässler, Guido Bold, Hans-Georg Capraro, Marc Lang
-
Patent number: 6166004Abstract: 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: GrantFiled: September 20, 1999Date of Patent: December 26, 2000Assignee: Novartis Finance CorporationInventors: Alexander Fassler, Guido Bold, Hans-Georg Capraro, Marc Lang, Satish Chandra Khanna
-
Patent number: 6110946Abstract: 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: GrantFiled: July 1, 1998Date of Patent: August 29, 2000Assignee: Novartis Finance CorporationInventors: Alexander Fassler, Guido Bold, Hans-Georg Capraro, Marc Lang, Satish Chandra Khanna
-
Patent number: 5935976Abstract: Antiretroviral compounds (which are effective, for example, against HIV) of the formula I ##STR1## in which R.sub.Type: GrantFiled: August 21, 1998Date of Patent: August 10, 1999Assignee: Novartis CorporationInventors: Guido Bold, Hans-Georg Capraro, Alexander Fassler, Marc Lang, Shripad Subray Bhagwat, Satish Chandra Khanna, Janis Karlis Lazdins, Jurgen Mestan
-
Patent number: 5912352Abstract: 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: GrantFiled: May 30, 1997Date of Patent: June 15, 1999Assignee: Novartis Finance CorporationInventors: Alexander Fassler, Guido Bold, Hans-Georg Capraro, Heinz Steiner
-
Patent number: 5849911Abstract: 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: GrantFiled: April 9, 1997Date of Patent: December 15, 1998Assignee: Novartis Finance CorporationInventors: Alexander Fassler, Guido Bold, Hans-Georg Capraro, Marc Lang, Satish Chandra Khanna
-
Patent number: 5807891Abstract: Antiretroviral compounds (which are effective, for example, against HIV) of the formula I ##STR1## in which R.sub.Type: GrantFiled: April 8, 1997Date of Patent: September 15, 1998Assignee: Novartis AGInventors: Guido Bold, Hans-Georg Capraro, Alexander Fassler, Marc Lang, Shripad Subray Bhagwat, Satish Chandra Khanna, Janis Karlis Lazdins, Jurgen Mestan
-
Patent number: 5753652Abstract: The invention relates to compounds of formula ##STR1## and salts, pharmaceutical compositions, intermediates and processes of preparation thereof.Type: GrantFiled: April 4, 1995Date of Patent: May 19, 1998Assignee: Novartis CorporationInventors: Alexander Fassler, Guido Bold, Marc Lang, Shripad Bhagwat, Peter Schneider
-
Patent number: 5670497Abstract: 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: GrantFiled: January 11, 1996Date of Patent: September 23, 1997Assignee: Ciba-Geigy CorporationInventors: Guido Bold, Shripad S. Bhagwat, Alexander Fassler, Marc Lang
-
Patent number: 5663200Abstract: Antiretroviral compounds (which are effective, for example, against HIV) of the formula I ##STR1## in which R.sub.Type: GrantFiled: October 19, 1995Date of Patent: September 2, 1997Assignee: Ciba-Geigy CorporationInventors: Guido Bold, Hans-Georg Capraro, Alexander Fassler, Marc Lang, Shripad Subray Bhagwat, Satish Chandra Khanna, Janis Karlis Lazdins, Jurgen Mestan
-
Patent number: 5643878Abstract: 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: GrantFiled: March 8, 1994Date of Patent: July 1, 1997Assignee: Ciba-Geigy CorporationInventors: Guido Bold, Marc Lang, Alexander Fassler, Hans-Georg Capraro, Shripad Bhagwat, Peter Schneider, Peter van Hoogevest
-
Patent number: 5409927Abstract: 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: GrantFiled: March 25, 1993Date of Patent: April 25, 1995Assignee: Ciba-Geigy CorporationInventors: Guido Bold, Alexander Fassler, Marc Lang, Peter Schneider