Patents by Inventor Vittorio Farina
Vittorio Farina 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: 9174971Abstract: The present invention is directed to a novel process for the preparation of compounds having inhibitory activity against sodium-dependent glucose transporter (SGLT) being present in the intestine or kidney.Type: GrantFiled: October 14, 2010Date of Patent: November 3, 2015Assignee: Janssen Pharmaceutica NVInventors: Vittorio Farina, Sebastien François Emmanuel Lemaire, Ioannis N. Houpis
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Publication number: 20110087017Abstract: The present invention is directed to a novel process for the preparation of compounds having inhibitory activity against sodium-dependent glucose transporter (SGLT) being present in the intestine or kidney.Type: ApplicationFiled: October 14, 2010Publication date: April 14, 2011Inventors: Vittorio FARINA, Sebastien François Emmanuel Lemaire, Ioannis N. Houpis
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Patent number: 7714127Abstract: Disclosed are processes to produce a compound of the formula (I):Type: GrantFiled: October 4, 2006Date of Patent: May 11, 2010Assignee: Boehringer Ingelheim Pharmaceuticals, Inc.Inventors: Guisheng Li, Jianxiu Liu, Zhi-Hui (Bruce) Lu, Ming Shen, Sonia Rodriguez, Vittorio Farina
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Patent number: 7544798Abstract: Disclosed is a multi-step process for preparing a macrocyclic compound of the formula (I): wherein Q is a radical of the following formula: and the other variables are as defined herein. The compounds of formula (I) are potent active agents for the treatment of hepatitis C virus (HCV) infection.Type: GrantFiled: February 1, 2007Date of Patent: June 9, 2009Assignee: Boehringer Ingelheim International GmbHInventors: Carl Alan Busacca, Vittorio Farina, Fabrice Gallou, Nizar Haddad, Xiao-jun Wang, Xudong Wei, Jinghua Xu, Yibo Xu, Nathan K. Yee, Li Zhang
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Publication number: 20080177029Abstract: Disclosed is a multi-step process for preparing a macrocyclic compound of the formula (I): wherein Q is a radical of the following formula: and the other variables are as defined herein. The compounds of formula (I) are potent active agents for the treatment of hepatitis C virus (HCV) infection.Type: ApplicationFiled: February 1, 2007Publication date: July 24, 2008Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Carl Alan Busacca, Vittorio Farina, Fabrice Gallou, Nizar Haddad, Xiao-Jun Wang, Xudong Wei, Jinghua Xu, Yibo Xu, Nathan K. Yee, Li Zhang
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Publication number: 20070105857Abstract: Disclosed are processes to produce a compound of the formula (I):Type: ApplicationFiled: October 4, 2006Publication date: May 10, 2007Inventors: Guisheng Li, Jianxiu Liu, Zhi-Hui (Bruce) Lu, Ming Shen, Sonia Rodriguez, Vittorio Farina
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Publication number: 20050209135Abstract: Disclosed is a multi-step process for preparing a macrocyclic compound of the formula (I): wherein Q is a radical of the following formula: and the other variables are as defined herein. The compounds of formula (I) are potent active agents for the treatment of hepatitis C virus (HCV) infection.Type: ApplicationFiled: March 11, 2005Publication date: September 22, 2005Applicant: Boehringer Ingelheim International GmbHInventors: Carl Busacca, Vittorio Farina, Fabrice Gallou, Nizar Haddad, Xiao-Jun Wang, Xudong Wei, Jinghua Xu, Yibo Xu, Nathan Yee, Li Zhang
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Patent number: 6407238Abstract: Disclosed is a process of making substituted pyrazoles from substituted benzophenone hydrazones with a variety of 1,3-bifunctional substrates under acid conditions. The pyrazole compounds are useful for making pharmaceutical compounds.Type: GrantFiled: October 27, 2000Date of Patent: June 18, 2002Assignee: Boehringer Ingelheim Pharmaceuticals, Inc.Inventors: James A. Baron, Vittorio Farina, Nizar Haddad
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Patent number: 5693666Abstract: The present invention provides paclitaxel derivatives of formula I ##STR1## and pharmaceutical compositions.Type: GrantFiled: January 3, 1996Date of Patent: December 2, 1997Assignee: Bristol-Myers Squibb CompanyInventors: Shu-Hui Chen, Vittorio Farina, Gregory Roth, John Kadow
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Patent number: 5478854Abstract: R.sup.g is C.sub.1-6 alkyl, C.sub.2-6 alkenyl, C.sub.2-6 alkynyl, C.sub.3-6 cycloalkyl, or a radical of the formula --W--R.sup.x in which W is a bond, C.sub.2-6 alkenediyl, or --(CH.sub.2).sub.t --, in which t is one to six; and R.sup.x is naphthyl, phenyl, or heteroaryl, and furthermore R.sup.x can be optionally substituted with one to three same or different C.sub.1-6 alkyl, C.sub.1-6 alkoxy, halogen or --CF.sub.3 groups;R.sup.2 is --OCOR, H, OH, --OR, --OSO.sub.2 R, --OCONR.sup.o R, --OCONHR, --OCOO(CH.sub.2).sub.t R, or --OCOOR; andR and R.sup.o are independently C.sub.1-6 alkyl, C.sub.2-6 alkenyl, C.sub.3-6 cycloalkyl, C.sub.2-6 alkynyl, or phenyl, optionally substituted with one to three same or different C.sub.1-6 alkyl, C.sub.1-6 alkoxy, halogen or --CF.sub.3 groups.Further provided by this invention are pharmaceutical formulations and intermediates for the the preparation of deoxy taxols of formula I. A method of treating mammalian tumors using a compound of formula I is also provided.Type: GrantFiled: March 10, 1994Date of Patent: December 26, 1995Assignee: Bristol-Myers Squibb CompanyInventors: Vittorio Farina, Shu-Hui Chen, David Langley, Mark D. Wittman, Joydeep Kant, Dolatrai M. Vyas
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Patent number: 5380751Abstract: The present invention provides paclitaxel derivatives of formula I ##STR1## in which R.sup.1 is --COR.sup.z in which R.sup.Z is RO-- or R;R.sup.2 is C.sub.1-6 alkyl, C.sub.2-6 alkenyl, C.sub.2-6 alkynyl, C.sub.3-6 cycloalkyl, or a radical of the formula --W--R.sup.x in which W is a bond, C.sub.2-6 alkenediyl, or --(CH.sub.2).sub.t --, in which t is one to six; and R.sup.x is naphthyl, phenyl, or heteroaryl, and furthermore R.sup.x can be optionally substituted with one to three same or different C.sub.1-6 alkyl, C.sub.1-6 alkoxy, halogen or --CF.sub.3 groups;R.sup.a is --OCOR, H, OH, --OR, --OSO.sub.2 R, --OCONR.sup.o R, --OCONHR, --OCOO(CH.sub.2).sub.t R, or --OCOOR;R.sup.b and R.sup.c are both hydroxy or together form a bond with the carbon atoms to which they are attached; andR and R.sup.o are independently C.sub.1-6 alkyl, C.sub.2-6 alkenyl, C.sub.3-6 cycloalkyl, C.sub.2-6 alkynyl, or phenyl, optionally substituted with one to three same or different C.sub.1-6 alkyl, C.sub.1-6 alkoxy, halogen or --CF.sub.Type: GrantFiled: September 28, 1993Date of Patent: January 10, 1995Assignee: Bristol-Myers Squibb CompanyInventors: Shu-Hui Chen, Vittorio Farina, Gregory Roth, John Kadow
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Patent number: 5350866Abstract: The present invention relates to 10-desacetoxytaxol and derivatives thereof, which are useful as antitumor agents. These compounds have the formula ##STR1## wherein R.sub.2 is hydrogen, hydroxy or a protected hydroxy group; R.sub.3 and R.sub.4 are independently hydrogen, hydroxy, a protected hydroxy group, methyl, --SH, --NH.sub.2, or --NR.sub.8 R.sub.9 ; R.sub.5 is R.sub.10, or --OR.sub.10 ; R.sub.6 and R.sub.7 are independently hydrogen, alkyl, or aryl; R.sub.8 and R.sub.9 are independently hydrogen, alkyl, alkenyl, alkynyl, or aryl; and R.sub.10 is alkoxy, alkyl, alkenyl, alkynl, or aryl.Type: GrantFiled: September 22, 1992Date of Patent: September 27, 1994Assignees: Bristol-Myers Squibb Company, Florida State UniversityInventors: Robert A. Holton, Shu-Hui Chen, Vittorio Farina
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Patent number: 5300638Abstract: The present invention relates to a process for the preparation of (3R, 4S)-3-hydroxy-4-phenyl-2-azetidinone derivatives which are useful intermediates in the synthesis of taxol from baccatin III, said process comprises reacting an acyloxyacetyl halide with an imine derived from L-threonine; and to compounds of formula (III) which are produced in said process: ##STR1## wherein Ar is phenyl; R.sup.1 is hydrogen, an acyl radical of a carboxylic acid, or a carbonic acid ester radical; R.sup.2 is hydrogen or a carboxy protecting group; and R.sup.3 is hydrogen or a hydroxy protecting group.Type: GrantFiled: July 16, 1992Date of Patent: April 5, 1994Assignee: Bristol-Myers Squibb CompanyInventors: Vittorio Farina, Sheila I. Hauck
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Patent number: 5294637Abstract: This invention relates to a fluorinated taxol of formula I ##STR1## in which R.sup.1 is --COR.sup.z in which R.sup.z is RO-- or R;R.sup.g is C.sub.1-6 alkyl, C.sub.2-6 alkenyl, C.sub.2-6 alkynyl, C.sub.3-6 cycloalkyl, or a radical of the formula --W--R.sup.x in which W is a bond, C.sub.2-6 alkenediyl, or --(CH.sub.2).sub.t --, in which t is one to six; and R.sup.x is naphthyl, furyl, thienyl or phenyl, and furthermore R.sup.x can be optionally substituted with one to three same or different C.sub.1-6 alkyl, C.sub.1-6 alkoxy, halogen or --CF.sub.3 groups;R.sup.2 is --OCOR, H, OH, --OR, --OSO.sub.2 R, --OCONR.sup.o R, --OCONHR, --OCOO(CH.sub.2).sub.t R, or --OCOOR; andR and R.sup.o are independently C.sub.1-6 alkyl, C.sub.2-6 alkenyl, C.sub.3-6 cycloalkyl, C.sub.2-6 alkynyl, or phenyl, optionally substituted with one to three same or different C.sub.1-6 alkyl, C.sub.1-6 alkoxy, halogen or --CF.sub.3 groups.Type: GrantFiled: May 20, 1993Date of Patent: March 15, 1994Assignee: Bristol-Myers Squibb CompanyInventors: Shu-Hui Chen, Vittorio Farina, Joydeep Kant, Dolatrai M. Vyas
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Patent number: 5272171Abstract: The present invention is directed to novel taxol derivatives useful as anti-tumor agents. Also provided by this invention is pharmaceutical formulations and methods of treating mammalian tumors with the compounds of this invention.Type: GrantFiled: November 24, 1992Date of Patent: December 21, 1993Assignee: Bristol-Myers Squibb CompanyInventors: Yasutsugu Ueda, Henry Wong, Vittorio Farina, Amarendra Mikkilineni, Dolatrai M. Vyas, Terrence Doyle
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Patent number: 5254580Abstract: An antitumor compound of formula I ##STR1## in which R.sup.1 is --COR.sup.z in which R.sup.z is t-butyloxy, C.sub.1-6 alkyl, C.sub.2-6 alkenyl, C.sub.2-6 alkynyl, C.sub.3-6 cycloalkyl, or phenyl, optionally substituted with one to three same or different C.sub.1-6 alkyl, C.sub.1-6 alkoxy, halogen or --CF.sub.3 groups;R.sup.2 is C.sub.1-6 alkyl, C.sub.2-6 alkenyl, C.sub.2-6 alkynyl, C.sub.3-6 cycloalkyl, or a radical of the formula --W--R.sup.x in which W is a bond, C.sub.2-6 alkenediyl, or --(CH.sub.2).sub.t --, in which t is one to six; and R.sup.x is naphthyl, furyl, thienyl or phenyl, and furthermore R.sup.x can be optionally substituted with one to three same or different C.sub.1-6 alkyl, C.sub.1-6 alkoxy, halogen or --CF.sub.3 groups;R.sup.3 is OCOR, --OCOOR, H, or OH; R.sup.4 is hydrogen; or R.sup.3 and R.sup.4 jointly form a carbonyl group; and R is C.sub.1-6 alkyl.Type: GrantFiled: March 11, 1993Date of Patent: October 19, 1993Assignee: Bristol-Myers Squibb CompanyInventors: Shu-Hui Chen, Vittorio Farina
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Patent number: 5248796Abstract: The present invention relates to 10-desacetoxy-11,12-dihydrotaxol-10,12(18)-diene derivatives which are useful as antitumor agents and as intermediates for the preparation of 10-desacetoxytaxol. Also disclosed is a novel process for the preparation of 10-desacetoxytaxol which comprises treating hydroxy protected 10-deacetyltaxol with 1,1,2-trifluoro-2-chlorotriethylamine followed by catalytic hydrogenation.Type: GrantFiled: June 18, 1992Date of Patent: September 28, 1993Assignee: Bristol-Myers Squibb CompanyInventors: Shu-Hui Chen, Vittorio Farina
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Patent number: 5192796Abstract: This invention relates to a fluorinated taxol of formula I ##STR1## in which R.sup.1 is benzoyl or t-butyloxycarbonyl; R.sup.2 is acetoxy, hydrogen or hydroxy; and the wavy line indicates either the .alpha.- or the .beta.-configuration.Further provided by this invention are pharmaceutical formulations and useful intermediates for the fluorinated taxols of formula I. A method of treating mammalian tumors using a compound of formula I is also provided.Type: GrantFiled: July 1, 1992Date of Patent: March 9, 1993Assignee: Bristol-Myers Squibb CompanyInventors: Shu-Hui Chen, Vittorio Farina
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Patent number: 5162521Abstract: This invention relates to a novel process for making a cephem of formula II from 2-(3-amino-2-oxo-azetidin-1-yl)-2,3-butadienoate of formula I. In another aspect, this invention is concerned with a process of further converting a compound of formula II into an antibacterial cephem of formula III. ##STR1## In formulae I, II and III, R.sup.1 is hydrogen, a conventional amino protecting group or an acyl group; R.sup.2 is an aromatic heterocyclic or aryl group; R.sup.3 is a conventional carboxy protecting group or --CO.sub.2 R.sup.3 taken together forms a physiologically hydrolyzable ester; and R.sup.4 is a group selected from the group consisting of C.sub.1-6 alkyl, C.sub.2-6 alkenyl, C.sub.2-6 alkynyl, cyclic C.sub.3-6 alkyl, and aryl; and n is 0 or 2.Type: GrantFiled: June 6, 1991Date of Patent: November 10, 1992Assignee: Bristol-Myers Squibb CompanyInventors: Vittorio Farina, Stephen R. Baker
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Patent number: 5162524Abstract: This invention relates to a novel process for making a cephem of formula II from a 2-(3-amino-2-oxo-azetidin-1-yl)-2,3-butadienoate intermediate of formula I using an organo-copper reagent. In another aspect, this invention is concerned with said intermediate. ##STR1## In the compounds of Scheme (A), R.sup.1 is a conventional amino protecting group or an acyl group; R.sup.2 is an aromatic heterocyclic or aryl group; R.sup.3 is a conventional carboxy protecting group or --CO.sub.2 R.sup.3 taken together forms a physiologically hydrolyzable ester; and R.sup.4 is a group selected from the group consisting of C.sub.1-6 alkyl, C.sub.2-6 alkenyl, C.sub.2-6 alkynyl, cyclic C.sub.3-6 alkyl, and aryl; and n is 0 or 2.This invention also relates to an intermediate represented by formula ##STR2## in which R.sup.1, R.sup.2, R.sup.3 and n are as defined above.Type: GrantFiled: June 6, 1991Date of Patent: November 10, 1992Assignee: Bristol-Myers Squibb CompanyInventors: Vittorio Farina, Joydeep Kant