Patents by Inventor Stuart J Mickel
Stuart J Mickel 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).
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Patent number: 7973175Abstract: The invention related to a novel process, novel process steps and novel intermediates useful in the synthesis of pharmaceutically active compounds, especially renin inhibitors, such as Aliskiren. Inter alia, the invention relates to a process for the manufacture of a compound of the formula III, wherein R, R1, and R? are as defined in the specification, or a salt thereof, and a compound of formula IV wherein R, R1, R2 and R? are as defined in the specification, and processes of manufacturing these.Type: GrantFiled: September 26, 2006Date of Patent: July 5, 2011Assignee: Novartis AGInventors: Stuart J Mickel, Wolfgang Marterer
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Patent number: 7767831Abstract: The present invention provides a novel process, novel process steps and novel intermediates useful in the synthesis of pharmaceutically active compounds, especially renin inhibitors, such as Aliskiren. Inter alia, the invention provides a process for the manufacture of a compound of the formula III, wherein R, R1, R2, R3 and PG are as defined in the specification, or a salt thereof. The manufacture comprises (preferably consists of) reacting a compound of the formula I, with a reagent able to transform hydroxy into X where X is for example a leaving group.Type: GrantFiled: June 6, 2006Date of Patent: August 3, 2010Assignee: Novartis AGInventors: Stuart J Mickel, Gottfried Sedelmeier, Hans Hirt, Frank Schäfer, Michael Foulkes, Walter Prikoszovich
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Patent number: 7119189Abstract: The present invention provides purified GABAB receptors and receptor proteins derived from rat and human sources, as well as nucleic acids which encode such proteins. The proteins and nucleic acids of the invention share significant homology with the GABAB receptor and the DNA encoding it as specifically disclosed herein. The invention moreover provides methods for isolating other members of the GABAB receptor family using DNA cloning technology and probes derived from the sequences provided herein, as well as novel members of the GABAB receptor family isolated by such methods.Type: GrantFiled: June 6, 2001Date of Patent: October 10, 2006Assignee: Novartis AGInventors: Klemens Kaupmann, Bernhard Bettler, Helmut Bittiger, Wolfgang Fröstl, Stuart J Mickel
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Publication number: 20020091250Abstract: The present invention provides purified GABAB receptors and receptor proteins derived from rat and human sources, as well as nucleic acids which encode such proteins. The proteins and nucleic acids of the invention share significant homology with the GABAB receptor and the DNA encoding it as specifically disclosed herein. The invention moreover provides methods for isolating other members of the GABAB receptor family using DNA cloning technology and probes derived from the sequences provided herein, as well as novel members of the GABAB receptor family isolated by such methods.Type: ApplicationFiled: June 6, 2001Publication date: July 11, 2002Inventors: Klemens Kaupmann, Bernhard Bettler, Helmut Bittiger, Wolfgang Frostl, Stuart J. Mickel
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Patent number: 5545631Abstract: Compounds having GABA.sub.B -antagonistic properties, for example those of formula I ##STR1## wherein one of the radicals R.sub.1, R.sub.2 and R.sub.3 is hydrogen or an aliphatic, cycloaliphatic, araliphatic or aromatic radical, another is hydrogen or, in the case of R.sub.1 or R.sub.2, hydroxy or, in the case of R.sub.1, halogen or, in the case of R.sub.2 together with R.sub.2 ', oxo, and the remaining radical is hydrogen, R.sub.1 ' is hydrogen or halogen, R.sub.2 ' is hydrogen, hydroxy or, together with R.sub.2, is oxo, R.sub.4 and R.sub.5 are hydrogen or R.sub.4 is an araliphatic or heteroarylaliphatic radical and R.sub.5 is hydrogen or an aliphatic radical, and R is an aliphatic, cycloaliphatic, cycloaliphatic-aliphatic, araliphatic, heteroarylaliphatic or aromatic radical having at least 2 carbon atoms or, when R.sub.1 is hydrogen or hydroxy, R.sub.2 is an aromatic radical and R.sub.1 ', R.sub.2 ' and R.sub.3 are hydrogen.Type: GrantFiled: January 20, 1995Date of Patent: August 13, 1996Assignee: Ciba-Geigy CorporationInventors: Christian Marescaux, Raymond Bernasconi, Markus Schmutz, Wolfgang Fr ostl, Stuart J. Mickel
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Patent number: 5500418Abstract: Compounds of formula I ##STR1## wherein R is diethoxymethyl, R.sub.1 is hydrogen, R.sub.2 is pyrid-3-ylmethyl and R.sub.3 is hydrogen, or R is cyclohexylmethyl, R.sub.1 is hydrogen and R.sub.2 is quinolin-4-ylmethyl, or R.sub.1 is hydroxy and R.sub.2 is 3,4-methylenedioxybenzyl, 1-(3,4-methylenedioxyphenyl)ethyl, and R.sub.3 is hydrogen, or R is benzyl, R.sub.1 is hydroxy, R.sub.2 is 1-(3,4-methylenedioxyphenyl)ethyl, and R.sub.3 is hydrogen, and salts thereof have GABA.sub.B -antagonistic properties and can be used for the treatment of diseases responsive to GABA.sub.B -antagonists.Type: GrantFiled: September 16, 1994Date of Patent: March 19, 1996Assignee: Ciba-Geigy CorporationInventor: Stuart J. Mickel
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Patent number: 5424441Abstract: N-aralkyl- and N-heteroaralkyl-aminoalkanephosphinic acids of formula I ##STR1## wherein R is an aliphatic, cycloaliphatic, cycloaliphatic-aliphatic, araliphatic or heteroarylaliphatic radical having at least 2 carbon atoms, R.sub.1 is hydrogen or hydroxy, R.sub.2 is an araliphatic or heteroarylaliphatic radical substituted by free or functionally modified carboxy that is bonded directly or by way of a spacer, and R.sub.3 is hydrogen, lower alkyl or a group R.sub.2, and the salts thereof have valuable nootropic and anti-epileptic properties and can be used in the preparation of a nootropic or anti-epileptic medicament.Type: GrantFiled: May 4, 1994Date of Patent: June 13, 1995Assignee: Ciba-Geigy CorporationInventors: Stuart J. Mickel, Wolfgang Frostl, Pascal Furet
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Patent number: 5407922Abstract: Compounds having GABA.sub.B -antagonistic properties, for example those of formula I ##STR1## wherein one of the radicals R.sub.1, R.sub.2 and R.sub.3 is hydrogen or an aliphatic, cycloaliphatic, araliphatic or aromatic radical, another is hydrogen or, in the case of R.sub.1 or R.sub.2, hydroxy or, in the case of R.sub.1, halogen or, in the case of R.sub.2 together with R.sub.2 ', oxo, and the remaining radical is hydrogen, R.sub.1 ' is hydrogen or halogen, R.sub.2 ' is hydrogen, hydroxy or, together with R.sub.2, is oxo, R.sub.4 and R.sub.5 are hydrogen or R.sub.4 is an araliphatic or heteroarylaliphatic radical and R.sub.5 is hydrogen or an aliphatic radical, and R is an aliphatic, cycloaliphatic, cycloaliphatic-aliphatic, araliphatic, heteroarylaliphatic or aromatic radical having at least 2 carbon atoms or, when R.sub.1 is hydrogen or hydroxy, R.sub.2 is an aromatic radical and R.sub.1 ', R.sub.2 ' and R.sub.Type: GrantFiled: May 3, 1993Date of Patent: April 18, 1995Assignee: Ciba-Geigy CorporationInventors: Christian Marescaux, Raymond Bernasconi, Markus Schmutz, Wolfgang Frostl, Stuart J. Mickel
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Patent number: 5376684Abstract: Novel compounds of formula I ##STR1## wherein R is selected from butyl, diethoxymethyl, cyclohexylmethyl, cyclohex-3-enylmethyl, benzyl, 4-chlorobenzyl, 4-methylbenzyl and 4-methoxybenzyl, R.sub.1 is selected from hydrogen and hydroxy, R.sub.2 is selected from hydrogen, chlorobenzyl, dichlorobenzyl, .alpha.-cyclopropyl-dichloro-benzyl, dichlorophenyl-2-hydroxy-ethyl, dimethylbenzyl, trimethoxybenzyl, methylenedioxybenzyl, chlorophenylethyl, dichlorophenylethyl, chloro-iodo-phenylethyl, dimethoxyphenylethyl, methylenedioxyphenylethyl, trimethoxyphenylethyl, 3-phenylprop-2-yl, 3-phenyl-3-hydroxy-prop-2-yl, dichlorophenylpropyl, dichlorophenyl-3-hydroxyprop-2-yl, dichlorophenylbutyl and quinolin-4-ylmethyl, and R.sub.3 is selected from hydrogen and methyl, and salts thereof, have GABA.sub.B -antagonistic properties and can be used for the treatment of diseases responsive to GABA.sub.B -antagonists.Type: GrantFiled: November 19, 1992Date of Patent: December 27, 1994Assignee: Ciba-Geigy CorporationInventor: Stuart J. Mickel
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Patent number: 5332729Abstract: N-aralkyl- and N-heteroaralkyl-aminoalkanephosphinic acids of formula I ##STR1## wherein R is an aliphatic, cycloaliphatic, cycloaliphatic-aliphatic, araliphatic or heteroarylaliphatic radical having at least 2 carbon atoms,R.sub.1 is hydrogen or hydroxy,R.sub.2 is an araliphatic or heteroarylaliphatic radical substituted by free or functionally modified carboxy that is bonded directly or by way of a spacer, andR.sub.3 is hydrogen, lower alkyl or a group R.sub.2, and the salts thereof have valuable nootropic and anti-epileptic properties and can be used in the preparation of a nootropic or anti-epileptic medicament.Type: GrantFiled: May 3, 1993Date of Patent: July 26, 1994Assignee: Ciba-Geigy CorporationInventors: Stuart J. Mickel, Wolfgang Frostl, Pascal Furet
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Patent number: 5300679Abstract: Compounds of the formula I ##STR1## wherein R denotes an aliphatic, cycloaliphatic, cycloaliphatic-aliphatic or araliphatic radical having 2 or more carbon atoms, and wherein one of the groups R.sup.1, R.sup.2 and R.sup.3 represents hydrogen or an aliphatic, cycloaliphatic, araliphatic or aromatic radical, another one of R.sup.1, R.sup.2 and R.sup.3 is hydrogen or, in the case of R.sup.1 and R.sup.2, is hydroxy, and the remaining one of R.sup.1, R.sup.2 and R.sup.3 is hydrogen, or wherein R denotes methyl, R.sub.1 denotes hydrogen or hydroxy, R.sub.2 denotes an aromatic radical and R.sub.3 represents hydrogen, and their salts have GABA.sub.B -antagonistic properties and can be used as GABA.sub.B -antagonists. They are obtained when in a compound of formula II ##STR2## in which R, R.sup.1, R.sup.2 and R.sup.3 have their previous significances, Z represents --NH.sub.2 and R.sup.4 denotes a hydroxy-protective group R.sup.5 or, when R.sup.1 and R.sup.3 denote hydrogen and R.sup.Type: GrantFiled: October 29, 1992Date of Patent: April 5, 1994Assignee: Ciba-Geigy CorporationInventors: Eric K. Baylis, Helmut Bittiger, Wolfgang Frostl, Roger G. Hall, Ludwig Maier, Stuart J. Mickel, Hans-Rudolf Olpe
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Patent number: 5229379Abstract: Compounds having GABA.sub.B -antagonistic properties, for example those of formula I ##STR1## wherein one of the radicals R.sub.1, R.sub.2 and R.sub.3 is hydrogen or an aliphatic, cycloaliphatic, araliphatic or aromatic radical, another is hydrogen or, in the case of R.sub.1 or R.sub.2, hydroxy or, in the case of R.sub.1, halogen or, in the case of R.sub.2 together with R.sub.2 ', oxo, and the remaining radical is hydrogen, R.sub.1 ' is hydrogen or halogen, R.sub.2 ' is hydrogen, hydroxy or, together with R.sub.2, is oxo, R.sub.4 and R.sub.5 are hydrogen or R.sub.4 is an araliphatic or heteroarylaliphatic radical and R.sub.5 is hydrogen or an aliphatic radical, and R is an aliphatic, cycloaliphatic, cycloaliphatic-aliphatic, araliphatic, heteroarylaliphatic or aromatic radical having at least 2 carbon atoms or, when R.sub.1 is hydrogen or hydroxy, R.sub.2 is an aromatic radical and R.sub.1 ', R.sub.2 ' and R.sub.Type: GrantFiled: June 20, 1991Date of Patent: July 20, 1993Assignee: Ciba-Geigy CorporationInventors: Christian Marescaux, Raymond Bernasconi, Markus Schmutz, Wolfgang Frostl, Stuart J. Mickel
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Patent number: 5190933Abstract: Compounds of the formula I ##STR1## wherein R denotes an aliphatic, cycloaliphatic, cycloaliphatic-aliphatic or araliphatic radical having 2 or more carbon atoms, and wherein one of the groups R.sup.1, R.sup.2 and R.sup.3 represents hydrogen or an aliphatic, cycloaliphatic, araliphatic or aromatic radical, another one of R.sup.1, R.sup.2 and R.sup.3 is hydrogen or, in the case of R.sup.1 and R.sup.2, is hydroxy, and the remaining one of R.sup.1, R.sup.2 and R.sup.3 is hydrogen, or wherein R denotes methyl, R.sub.1 denotes hydrogen or hydroxy, R.sub.2 denotes an aromatic radical and R.sub.3 represents hydrogen, and their salts have GABA.sub.B -antagonistic properties and can be used as GABA.sub.B -antagonists. They are obtained when in a compound of formula II ##STR2## in which R, R.sup.1, R.sup.2 and R.sup.3 have their previous significances, Z represents --NH.sub.2 and R.sup.4 denotes a hydroxy-protective group R.sup.5 or, when R.sup.1 and R.sup.3 denote hydrogen and R.sup.Type: GrantFiled: March 3, 1992Date of Patent: March 2, 1993Assignee: Ciba-Geigy CorporationInventors: Eric K. Baylis, Ludwig Maier, Stuart J. Mickel, Hans-Rudolf Olpe, Helmut Bittiger, Wolfgang Frostl, Roger G. Hall
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Patent number: 5190934Abstract: Compounds of the formula I ##STR1## wherein either R.sub.1 is halogen, R.sub.1 ' is halogen or hydrogen and R.sub.2 and R.sub.2 ' denote hydrogen or R.sub.1 and R.sub.1 ' represent hydrogen, R.sub.2 is an aliphatic or aromatic radical and R.sub.2 ' is hydroxy or R.sub.2 and R.sub.2 ' together represent oxo, and wherein R denotes an aliphatic, cycloaliphatic, cycloaliphatic-aliphatic or araliphatic radical having 2 or more carbon atoms or, if R.sub.1 and R.sub.1 ' denote hydrogen, R.sub.2 represents an aromatic radical and R.sub.2 ' is hydroxy, R represents methyl, and their salts are useful as nootropics, antidepressants and/or anxiolytics. The can be manufacture by replacing any group R.sub.5 by hydrogen and/or converting any group Z.sub.0 into amino in a compound of formula II ##STR2## in which R, R.sub.1, R.sub.1 ', R.sub.2 and R.sub.2 ' have their previous significances, Z represents a protected or latent amino group Z.sub.0 and R.sub.4 denotes hydrogen or a hyddroxy-protective group R.sub.Type: GrantFiled: March 3, 1992Date of Patent: March 2, 1993Assignee: Ciba-Geigy CorporationInventors: Stuart J. Mickel, Georg von Sprecher
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Patent number: 5064819Abstract: Compounds of the formula I ##STR1## wherein R denotes an aliphatic, cycloaliphatic, cycloaliphatic-aliphatic or araliphatic radical having 2 or more carbon atoms, and wherein one of the groups R.sup.1, R.sup.2 and R.sup.3 represents hydrogen or an aliphatic, cycloaliphatic, araliphatic or aromatic radical, another one of R.sup.1, R.sup.2 and R.sup.3 is hydrogen or, in the case of R.sup.1 and R.sup.2, is hydroxy, and the remaining one of R.sup.1, R.sup.2 and R.sup.3 is hydrogen, or wherein R denotes methyl, R.sub.1 denotes hydrogen or hydroxy, R.sub.2 denotes an aromatic radical and R.sub.3 represents hydrogen, and their salts have GABA.sub.B -antagonistic properties and can be used as GABA.sub.B -antagonists. They are obtained when in a compound of formula II ##STR2## in which R, R.sup.1, R.sup.2 and R.sup.3 have their previous significances, Z represents --NH.sub.2 and R.sup.4 denotes a hydroxy-protective group R.sup.5 or, when R.sup.1 and R.sup.3 denote hydrogen and R.sup.Type: GrantFiled: March 30, 1990Date of Patent: November 12, 1991Assignee: Ciba-Geigy CorporationInventors: Eric K. Baylis, Helmut Bittiger, Wolfgang Frostl, Roger G. Hall, Ludwig Maier, Stuart J. Mickel, Hans-Rudolf Olpe
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Patent number: 5051524Abstract: Compounds of the formula I ##STR1## wherein R denotes an aliphatic, cycloaliphatic, cycloaliphatic-aliphatic or araliphatic radical having 2 or more carbon atoms, and wherein one of the groups R.sup.1, R.sup.2 and R.sup.3 represents hydrogen or an aliphatic, cycloaliphatic, araliphatic or aromatic radical, another one of R.sup.1, R.sup.2 and R.sup.3 is hydrogen or, in the case of R.sup.1 and R.sup.2, is hydroxy, and the remaining one of R.sup.1, R.sup.2 and R.sup.3 is hydrogen, or wherein R denotes methyl, R.sub.1 denotes hydrogen or hydroxy, R.sub.2 denotes an aromatic radical and R.sub.3 represents hydrogen, and their salts have GABA.sub.B -antagonistic properties and can be used as GABA.sub.B -antagonists. They are obtained when in a compound of formula II ##STR2## in which R, R.sup.1, R.sup.2 and R.sup.3 have their previous significances, Z represents --NH.sub.2 and R.sup.4 denotes a hydroxy-protective group R.sup.5 or, when R.sup.1 and R.sup.3 denote hydrogen and R.sup.Type: GrantFiled: February 26, 1990Date of Patent: September 24, 1991Assignee: Ciba-Geigy CorporationInventors: Eric K. Baylis, Helmut Bittiger, Wolfgang Frostl, Roger G. Hall, Ludwig Maier, Stuart J. Mickel, Hans-Rudolf Olpe
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Patent number: 5013863Abstract: Compounds of the formula I ##STR1## wherein R denotes an aliphatic, cycloaliphatic, cycloaliphatic-aliphatic or araliphatic radical having 2 or more carbon atoms, and wherein one of the groups R.sup.1, R.sup.2 and R.sup.3 represents hydrogen or an aliphatic, cycloaliphatic, araliphatic or aromatic radical, another one of R.sup.1, R.sup.2 and R.sup.3 is hydrogen or, in the case of R.sup.1 and R.sup.2, is hydroxy, and the remaining one of R.sup.1, R.sup.2 and R.sup.3 is hydrogen, and their salts have GABA.sub.B -antagonistic properties and can be used as GABA.sub.B -antagonists. They are obtained when in a compound of formula II ##STR2## in which R, R.sup.1, R.sup.2 and R.sup.3 have their previous significances, Z represents --NH.sub.2 and R.sup.4 denotes a hydroxy-protective group R.sup.5 or, when R.sup.1 and R.sup.3 denote hydrogen and R.sup.2 denotes hydrogen or alkyl, denotes an alkali metal or ammonium ion R.sup.6, or Z represents a protected or latent amino group Z.sup.0 and R.sup.Type: GrantFiled: July 12, 1989Date of Patent: May 7, 1991Assignee: Ciba-Geigy CorporationInventors: Eric K. Baylis, Helmut Bittiger, Wolfgang Froostl, Roger G. Hall, Ludwig Maier, Stuart J. Mickel, Hans-Rudolf Olpe