Patents by Inventor Adriano Indolese
Adriano Indolese 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: 8178670Abstract: The present disclosure provides a method that efficiently produces (6R)-tetrahydrobiopterin of Formula I in high yield and purity. The method includes the step of hydrolyzing diacetylbiopterin to biopterin under basic conditions in a biphasic mixture comprising an organic phase and an aqueous phase. After substantially complete hydrolysis of diacetylbiopterin, the aqueous phase containing biopterin can be separated from the organic phase containing most of the organic impurities, which avoids the time-consuming step of isolating biopterin as a solid. The aqueous solution containing biopterin is stereoselectively hydrogenated to (6R)-tetrahydrobiopterin under basic conditions and high hydrogen pressure in the presence of a metal catalyst (e.g., a platinum catalyst). To improve the purification of an acid addition salt of (6R)-tetrahydrobiopterin (e.g., (6R)-tetrahydrobiopterin dihydrochloride), any residual salts (e.g.Type: GrantFiled: January 6, 2009Date of Patent: May 15, 2012Assignee: BioMarin Pharmaceutical Inc.Inventors: Mark Henderson, Steven Jungles, Gabriele Roidl, Robert Baffi, Adriano Indolese, Christian Müller, Philipp Schmidt, Stefan Kaiser
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Publication number: 20090198055Abstract: The present disclosure provides a method that efficiently produces (6R)-tetrahydrobiopterin in high yield and purity. The method includes the step of hydrolyzing diacetylbiopterin to biopterin under basic conditions in a biphasic mixture comprising an organic phase and an aqueous phase. After substantially complete hydrolysis of diacetylbiopterin, the aqueous phase containing biopterin can be separated from the organic phase containing most of the organic impurities, which avoids the time-consuming step of isolating biopterin as a solid. The aqueous solution containing biopterin is stereoselectively hydrogenated to (6R)-tetrahydrobiopterin under basic conditions and high hydrogen pressure in the presence of a metal catalyst (e.g., a platinum catalyst). To improve the purification of an acid addition salt of (6R)-tetrahydrobiopterin (e.g., (6R)-tetrahydrobiopterin dihydrochloride), any residual salts (e.g.Type: ApplicationFiled: January 6, 2009Publication date: August 6, 2009Applicant: BioMarin Pharmaceutical Inc.Inventors: Mark Henderson, Steven Jungles, Gabriele Roidl, Robert Baffi, Adriano Indolese, Christian Muller, Philipp Schmidt, Stefan Kaiser
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Patent number: 7132569Abstract: From compounds of formula II wherein R1 and R2 are independently of one another H, C1–C6alkyl, C1–C6halogenalkyl, C1–C6alkoxy, C1–C6alkoxy-C1–C6alkyl, or C1–C6alkoxy-C1–C6alkyloxy, R3 is C1–C6alkyl, R4 is C1–C6alkyl, and R5 is C1–C6alkyl, C1–C6hydroxyalkyl, C1–C6alkoxy-C1–C6-alkyl, C1–C6alkanoyloxy-C1–C6alkyl, C1–C6aminoalkyl, C1–C6alkylamino-C1–C6-alkyl, C1–C6-dialkylamino-C1–C6-alkyl, C1–C6-alkanoylamido-C1–C6-alkyl, HO(O)C—C1–C6-alkyl, C1–C6alkyl-O—(O)C—C1–C6alkyl, H2N—C(O)—C1–C6alkyl, C1–C6alkyl-HN—C(O)—C1–C6alkyl or (C1–C6alkyl)2N—C(O)—C1–C6-alkyl, R6 is C1–C6alkyl, R7 is C1–C6alkyl or C1–C6alkoxy, or R6 and R7 together are tetramethylene, pentamethylene, 3-oxa-1,5-pentylene or —CH2CH2O— substituted, if necessary, with C1–C4-Alkyl, phenyl or benzyl, it is possible—through halolactonization, azidation of the halogen group, ring opening with an amine R5—NH2, and reduction of the azide group to form the amino group—to prepare compounds of formula I wherein R5 is C1–C6alkyl, C1–C6hydroxyalkyl, C1–C6Type: GrantFiled: October 21, 2005Date of Patent: November 7, 2006Assignee: Speedel Pharma AGInventors: Peter Herold, Stefan Stutz, Adriano Indolese
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Patent number: 7009078Abstract: From compounds of formula II wherein R1 and R2 are independently of one another H, C1–C6alkyl, C1–C6halogenalkyl, C1–C6alkoxy, C1–C6alkoxy-C1–C6alkyl, or C1–C6alkoxy-C1–C6alkyloxy, R3 is C1–C6alkyl, R4 is C1–C6alkyl, and R5 is C1–C6alkyl, C1–C6hydroxyalkyl, C1–C6alkoxy-C1–C6-alkyl, C1–C6alkanoyloxy-C1–C6alkyl, C1–C6aminoalkyl, C1–C6alkylamino-C1–C6-alkyl, C1–C6-dialkylamino-C1–C6-alkyl, C1–C6-alkanoylamido-C1–C6-alkyl, HO(O)C—C1–C6-alkyl, C1–C6alkyl-O—(O)C—C1–C6alkyl, H2N—C(O)—C1–C6alkyl, C1–C6alkyl-HN—C(O)—C1–C6alkyl or (C1–C6alkyl)2N—C(O)—C1–C6-alkyl, R6 is C1–C6alkyl, R7 is C1–C6alkyl or C1–C6alkoxy, or R6 and R7 together are tetramethylene, pentamethylene, 3-oxa-1,5-pentylene or —CH2CH2O— substituted, if necessary, with C1–C4-Alkyl, phenyl or benzyl, it is possible—through halolactonization, azidation of the halogen group, ring opening with an amine R5—NH2, and reduction of the azide group to form the amino group—to prepare compounds of formula I wherein R5 is C1–C6alkyl, C1–C6hydroxyalkyl, C1–C6aType: GrantFiled: July 13, 2000Date of Patent: March 7, 2006Assignee: Speedel Pharma AGInventors: Peter Herold, Stefan Stutz, Adriano Indolese
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Publication number: 20060041169Abstract: From compounds of formula II wherein R1 and R2 are independently of one another H, C1-C6alkyl, C1-C6halogenalkyl, C1-C6alkoxy, C1-C6alkoxy-C1-C6alkyl, or C1-C6alkoxy-C1-C6alkyloxy, R3 is C1-C6alkyl, and R5 is C1-C6alkyl, C1-C6hydroxyalkyl, C1-C6alkoxy-C1-C6-alkyl, C1-C6alkanoyloxy-C1-C6alkyl, C1-C6aminoalkyl, C1-C6alkylamino-C1-C6-alkyl, C1-C6-dialkylamino-C1-C6-alkyl, C1-C6-alkanoylamido-C1-C6-alkyl, HO(O)C—C1-C6-alkyl, C1-C6alkyl-O—(O)C—C1-C6alkyl, H2N—C(O)—C1-C6alkyl, C1-C6alkyl-HN—C(O)—C1-C6alkyl or (C1-C6alkyl)2N—C(O)—C1-C6-alkyl, R6 is C1-C6alkyl, R7 is C1-C6alkyl or C1-C6alkoxy, or R6 and R7 together are tetramethylene, pentamethylene, 3-oxa-1,5-pentylene or —CH2CH2O— substituted, if necessary, with C1-C4-Alkyl, phenyl or benzyl, it is possible—through halolactonization, azidation of the halogen group, ring opening with an amine R5—NH2, and reduction of the azide group to form the amino group—to prepare compounds of formula I wherein R5 is C1-C6alkyl, C1-C6hydroxyalkyl, C1-C6alkoxy-C1-C6alkyl,Type: ApplicationFiled: October 21, 2005Publication date: February 23, 2006Inventors: Peter Herold, Stefan Stutz, Adriano Indolese
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Patent number: 6784295Abstract: Process for the coupling of a) nucleophiles selected from the group alcohols, thioles, amines, metallised hydrocarbons, CH-acidic compounds and metal cyanides, or of b) carbon monoxide mixed with water, alcohols, ammonia, primary or secondary amines, to organic compounds selected from the group of leaving-group-containing aromatics, hetero-aromatics with a C-bonded leaving group, aromatic or hetero-aromatic methyl compounds with a leaving group bonded to the methyl group, ethylenically unsaturated organic compounds with a C-bonded leaving group, or organic allyl compounds with a leaving group in allyl position, or c) vinyl compounds with leaving-group-containing aromatics, whilst cleaving the leaving group in the presence of Pd complexes with monophospholine ligands as the catalyst, whereby variants b) and c) are carried out in the presence of an inorganic base or organic nitrogen base, the process being characterised in that the Pd complex contains secondary monophosphines with aliphatic, branched or cyclType: GrantFiled: March 3, 2003Date of Patent: August 31, 2004Assignee: Solvias AGInventors: Adriano Indolese, Anita Schnyder
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Publication number: 20030181688Abstract: Process for the coupling ofType: ApplicationFiled: March 3, 2003Publication date: September 25, 2003Inventors: Adriano Indolese, Anita Schnyder
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Patent number: 6548684Abstract: Process for the coupling of a) nucleophiles selected from the group alcohols, thioles, amines, metallised hydrocarbons, CH-acidic compounds and metal cyanides, or of b) carbon monoxide mixed with water, alcohols, ammonia, primary or secondary amines, to organic compounds selected from the group of leaving-group-containing aromatics, hetero-aromatics with a C-bonded leaving group, aromatic or hetero-aromatic methyl compounds with a leaving group bonded to the methyl group, ethylenically unsaturated organic compounds with a C-bonded leaving group, or organic allyl compounds with a leaving group in allyl position, or c) vinyl compounds with leaving-group-containing aromatics, whilst cleaving the leaving group in the presence of Pd complexes with monophospholine ligands as the catalyst, whereby variants b) and c) are carried out in the presence of an inorganic base or organic nitrogen base, the process being characterised in that the Pd complex contains secondary monophosphines with aliphatic, branched or cycType: GrantFiled: March 6, 2001Date of Patent: April 15, 2003Assignee: Solvias AGInventors: Adriano Indolese, Anita Schnyder
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Patent number: 6441233Abstract: A process for the preparation of primary aromatic carboxamides by the carbonylation of an aromatic compound, which contains at least one leaving group, with carbon monoxide, in the presence of a homogeneous or heterogeneous Pd catalyst and at least stoichiometric amounts of an amidation agent at elevated temperatures, which is characterized in that a primary carboxamide or a primary urethane is used as the amidation agent, and the reaction is carried out in the presence of an acylation catalyst.Type: GrantFiled: June 21, 2001Date of Patent: August 27, 2002Assignee: Solvias AGInventors: Anita Schnyder, Adriano Indolese, Gerald Mehltretter
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Patent number: 6420608Abstract: A process for the preparation of a compound of formula I wherein Y is a group that is inert during preparation of the compound and m is from 0 to 4 is described. The process broadly involves the steps of a) reacting a compound of formula II wherein X is chlorine, bromine or iodine, and Y and m are as defined above, with a vinylether or an enamide in a solvent, a base and a catalytic amount of a palladium compound and a phosphine ligand. The resulting intermediate is then hydrolyzed to the compound of formula I.Type: GrantFiled: December 16, 1999Date of Patent: July 16, 2002Assignee: Bayer AktiengesellschaftInventor: Adriano Indolese
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Patent number: 6417389Abstract: This invention relates to a novel advantageous process for the stereoselective preparation of 2-hydroxy-4-phenylbutyrates (HPB esters) and of their precursors. This is done by starting from readily accessible &agr;-unsaturated &agr;-hydroxy-&ggr;-keto esters which can be prepared by Claisen condensation.Type: GrantFiled: September 25, 2000Date of Patent: July 9, 2002Assignee: Ciba Specialty Chemicals CorporationInventors: Martin Studer, Peter Herold, Adriano Indolese, Stefan Burckhardt
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Publication number: 20010037042Abstract: Process for the coupling ofType: ApplicationFiled: March 6, 2001Publication date: November 1, 2001Inventors: Adriano Indolese, Anita Schnyder
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Patent number: 6031126Abstract: A process for the production of a fluorescent whitening agent of formula: ##STR1## in which X and Z are as defined herein, comprising A) rearranging a hydrazobenzene compound having the formula: ##STR2## in which Z is as defined herein, to produce in situ a compound having the formula: ##STR3## B) diazotising the compound of formula (3) to produce a compound having the formula: ##STR4## in which Z has its previous significance and G.sub.1 is a counter ion; and C) reacting the compound of formula (4) with 2 moles of a compound having the formula: ##STR5## in which X and n have their previous significance, in the presence of an inorganic or organic palladium salt, or a mixture thereof, as catalyst-precursor, to produce a compound having the formula (1).Type: GrantFiled: April 23, 1998Date of Patent: February 29, 2000Assignee: Ciba Specialty Chemicals CorporationInventors: Victor Eliu, Werner Kanert, Adriano Indolese, Philipp Wyser, Anita Schnyder
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Patent number: 5952524Abstract: The present invention provides a process for the production of a compound of formula: ##STR1## in which X and Y, independently, are hydrogen, halogen, NO.sub.2, CF.sub.3, CN, C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy, COO--C.sub.1 -C.sub.4 alkyl, CO--C.sub.1 -C.sub.4 alkyl, NH--(C.sub.1 -C.sub.4 alkyl), N(C.sub.1 -C.sub.4 alkyl).sub.2, NH(C.sub.1 -C.sub.4 alkyl-OH), N(C.sub.1 -C.sub.4 alkyl-OH).sub.2, COOH or SO.sub.3 H or an ester or amide thereof, or COOM or SO.sub.3 M in which M is Na, K, Ca, Mg, ammonium, mono-, di-, tri- or tetra-C.sub.1 -C.sub.4 alkylammonium, mono-, di- or tri-hydroxyalkylammonium or ammonium that is di- or tri-substituted with a mixture of C.sub.1 -C.sub.4 alkyl and C.sub.1 -C.sub.4 hydroxyalkyl groups;Z is hydrogen, C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy, CF.sub.3, halogen (F, Cl, Br, I), SO.sub.3 H or SO.sub.Type: GrantFiled: April 23, 1998Date of Patent: September 14, 1999Assignee: Ciba Specialty Chemicals CorporationInventors: Victor Eliu, Werner Kanert, Adriano Indolese, Ian John Fletcher, Julia Volkel, Anita Schnyder
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Patent number: 5883283Abstract: The invention relates to a process for the preparation of substituted 3-amninobenzonitriles, which comprises reacting the appropriate substituted 3-aminochlorobenzene with a cyano-donating reagent, and to the compounds thereby produced. The compounds are intermediates, which after further reaction, produce 1,2,3-benzothiadiazole-derivatives having plant immunizing properties.Type: GrantFiled: August 1, 1997Date of Patent: March 16, 1999Assignee: Novartis Finance CorporationInventors: Richard Breitschuh, Benoit Pugin, Adriano Indolese, Verena Gisin