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).

  • Patent number: 9174971
    Abstract: 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: Grant
    Filed: October 14, 2010
    Date of Patent: November 3, 2015
    Assignee: Janssen Pharmaceutica NV
    Inventors: Vittorio Farina, Sebastien Fran├žois Emmanuel Lemaire, Ioannis N. Houpis
  • Publication number: 20110087017
    Abstract: 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: Application
    Filed: October 14, 2010
    Publication date: April 14, 2011
    Inventors: Vittorio FARINA, Sebastien Fran├žois Emmanuel Lemaire, Ioannis N. Houpis
  • Patent number: 7714127
    Abstract: Disclosed are processes to produce a compound of the formula (I):
    Type: Grant
    Filed: October 4, 2006
    Date of Patent: May 11, 2010
    Assignee: Boehringer Ingelheim Pharmaceuticals, Inc.
    Inventors: Guisheng Li, Jianxiu Liu, Zhi-Hui (Bruce) Lu, Ming Shen, Sonia Rodriguez, Vittorio Farina
  • Patent number: 7544798
    Abstract: 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: Grant
    Filed: February 1, 2007
    Date of Patent: June 9, 2009
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Carl Alan Busacca, Vittorio Farina, Fabrice Gallou, Nizar Haddad, Xiao-jun Wang, Xudong Wei, Jinghua Xu, Yibo Xu, Nathan K. Yee, Li Zhang
  • Publication number: 20080177029
    Abstract: 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: Application
    Filed: February 1, 2007
    Publication date: July 24, 2008
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: Carl Alan Busacca, Vittorio Farina, Fabrice Gallou, Nizar Haddad, Xiao-Jun Wang, Xudong Wei, Jinghua Xu, Yibo Xu, Nathan K. Yee, Li Zhang
  • Publication number: 20070105857
    Abstract: Disclosed are processes to produce a compound of the formula (I):
    Type: Application
    Filed: October 4, 2006
    Publication date: May 10, 2007
    Inventors: Guisheng Li, Jianxiu Liu, Zhi-Hui (Bruce) Lu, Ming Shen, Sonia Rodriguez, Vittorio Farina
  • Publication number: 20050209135
    Abstract: 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: Application
    Filed: March 11, 2005
    Publication date: September 22, 2005
    Applicant: Boehringer Ingelheim International GmbH
    Inventors: Carl Busacca, Vittorio Farina, Fabrice Gallou, Nizar Haddad, Xiao-Jun Wang, Xudong Wei, Jinghua Xu, Yibo Xu, Nathan Yee, Li Zhang
  • Patent number: 6407238
    Abstract: 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: Grant
    Filed: October 27, 2000
    Date of Patent: June 18, 2002
    Assignee: Boehringer Ingelheim Pharmaceuticals, Inc.
    Inventors: James A. Baron, Vittorio Farina, Nizar Haddad
  • Patent number: 5693666
    Abstract: The present invention provides paclitaxel derivatives of formula I ##STR1## and pharmaceutical compositions.
    Type: Grant
    Filed: January 3, 1996
    Date of Patent: December 2, 1997
    Assignee: Bristol-Myers Squibb Company
    Inventors: Shu-Hui Chen, Vittorio Farina, Gregory Roth, John Kadow
  • Patent number: 5478854
    Abstract: 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: Grant
    Filed: March 10, 1994
    Date of Patent: December 26, 1995
    Assignee: Bristol-Myers Squibb Company
    Inventors: Vittorio Farina, Shu-Hui Chen, David Langley, Mark D. Wittman, Joydeep Kant, Dolatrai M. Vyas
  • Patent number: 5380751
    Abstract: 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: Grant
    Filed: September 28, 1993
    Date of Patent: January 10, 1995
    Assignee: Bristol-Myers Squibb Company
    Inventors: Shu-Hui Chen, Vittorio Farina, Gregory Roth, John Kadow
  • Patent number: 5350866
    Abstract: 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: Grant
    Filed: September 22, 1992
    Date of Patent: September 27, 1994
    Assignees: Bristol-Myers Squibb Company, Florida State University
    Inventors: Robert A. Holton, Shu-Hui Chen, Vittorio Farina
  • Patent number: 5300638
    Abstract: 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: Grant
    Filed: July 16, 1992
    Date of Patent: April 5, 1994
    Assignee: Bristol-Myers Squibb Company
    Inventors: Vittorio Farina, Sheila I. Hauck
  • Patent number: 5294637
    Abstract: 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: Grant
    Filed: May 20, 1993
    Date of Patent: March 15, 1994
    Assignee: Bristol-Myers Squibb Company
    Inventors: Shu-Hui Chen, Vittorio Farina, Joydeep Kant, Dolatrai M. Vyas
  • Patent number: 5272171
    Abstract: 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: Grant
    Filed: November 24, 1992
    Date of Patent: December 21, 1993
    Assignee: Bristol-Myers Squibb Company
    Inventors: Yasutsugu Ueda, Henry Wong, Vittorio Farina, Amarendra Mikkilineni, Dolatrai M. Vyas, Terrence Doyle
  • Patent number: 5254580
    Abstract: 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: Grant
    Filed: March 11, 1993
    Date of Patent: October 19, 1993
    Assignee: Bristol-Myers Squibb Company
    Inventors: Shu-Hui Chen, Vittorio Farina
  • Patent number: 5248796
    Abstract: 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: Grant
    Filed: June 18, 1992
    Date of Patent: September 28, 1993
    Assignee: Bristol-Myers Squibb Company
    Inventors: Shu-Hui Chen, Vittorio Farina
  • Patent number: 5192796
    Abstract: 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: Grant
    Filed: July 1, 1992
    Date of Patent: March 9, 1993
    Assignee: Bristol-Myers Squibb Company
    Inventors: Shu-Hui Chen, Vittorio Farina
  • Patent number: 5162524
    Abstract: 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: Grant
    Filed: June 6, 1991
    Date of Patent: November 10, 1992
    Assignee: Bristol-Myers Squibb Company
    Inventors: Vittorio Farina, Joydeep Kant
  • Patent number: 5162521
    Abstract: 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: Grant
    Filed: June 6, 1991
    Date of Patent: November 10, 1992
    Assignee: Bristol-Myers Squibb Company
    Inventors: Vittorio Farina, Stephen R. Baker