Patents by Inventor Michael R. Barbachyn
Michael R. Barbachyn 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: 7645781Abstract: The present invention provides antibacterial agents having the formulae I, II, and III described herein.Type: GrantFiled: September 21, 2006Date of Patent: January 12, 2010Assignee: Pfizer IncInventors: Richard C. Thomas, Toni-Jo Poel, Michael R. Barbachyn, Mikhail F. Gordeev, Gary W. Luehr, Adam Renslo, Upinder Singh, Vara Prasad Venkata Negandra Josyula
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Patent number: 6869965Abstract: Substituted quinolone derivatives in which an oxazolidinone, isoxazolinone, or isoxazoline is covalently bonded to a quinolone, methods of using the quinolone derivatives, and pharmaceutical compositions containing the quinolone derivatives are disclosed. Methods of synthesizing these substituted quinolone derivatives are also disclosed, and in particular a method of manufacturing a 7-(2-oxo-1,3-oxazolidin-3-yl)aryl-3-quinolinecarboxylic acid by condensing a 4-(2-oxo-1,3-oxazolidin-5-yl)aryl boronic acid with a 7-halo-quinolone derivative. The quinolone derivatives possess antibacterial activity, and are effective against a number of human and veterinary pathogens in the treatment of bacterial diseases.Type: GrantFiled: December 5, 2003Date of Patent: March 22, 2005Assignee: Pharmacia & Upjohn CompanyInventors: Mikhail F. Gordeev, Dinesh V. Patel, Michael R. Barbachyn, James R. Gage
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Publication number: 20040215017Abstract: Substituted quinolone derivatives in which an oxazolidinone, isoxazolinone, or isoxazoline is covalently bonded to a quinolone, methods of using the quinolone derivatives, and pharmaceutical compositions containing the quinolone derivatives are disclosed. Methods of synthesizing these substituted quinolone derivatives are also disclosed, and in particular a method of manufacturing a 7-(2-oxo-1,3-oxazolidin-3-yl)aryl-3-quinolinecarboxylic acid by condensing a 4-(2-oxo-1,3-oxazolidin-5-yl)aryl boronic acid with a 7-halo-quinolone derivative. The quinolone derivatives possess antibacterial activity, and are effective against a number of human and veterinary pathogens in the treatment of bacterial diseases.Type: ApplicationFiled: December 5, 2003Publication date: October 28, 2004Applicant: PHARMACIA & UPJOHN COMPANYInventors: Mikhail F. Gordeev, Dinesh V. Patel, Michael R. Barbachyn, James R. Gage
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Patent number: 6689769Abstract: Substituted quinolone derivatives in which an oxazolidinone, isoxazolinone, or isoxazoline is covalently bonded to a quinolone, methods of using the quinolone derivatives, and pharmaceutical compositions containing the quinolone derivatives are disclosed. Methods of synthesizing these substituted quinolone derivatives are also disclosed, and in particular a method of manufacturing a 7-(2-oxo-1,3-oxazolidin-3-yl)aryl-3-quinolinecarboxylic acid by condensing a 4-(2-oxo-1,3-oxazolidin-5-yl)aryl boronic acid with a 7-halo-quinolone derivative. The quinolone derivatives possess antibacterial activity, and are effective against a number of human and veterinary pathogens in the treatment of bacterial diseases.Type: GrantFiled: November 29, 2001Date of Patent: February 10, 2004Assignee: Pharmacia & Upjohn CompanyInventors: Mikhail F. Gordeev, Dinesh V. Patel, Michael R. Barbachyn, James R. Gage
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Publication number: 20030013737Abstract: Substituted quinolone derivatives in which an oxazolidinone, isoxazolinone, or isoxazoline is covalently bonded to a quinolone, methods of using the quinolone derivatives, and pharmaceutical compositions containing the quinolone derivatives are disclosed. Methods of synthesizing these substituted quinolone derivatives are also disclosed, and in particular a method of manufacturing a 7-(2-oxo-1,3-oxazolidin-3-yl)aryl-3-quinolinecarboxylic acid by condensing a 4-(2-oxo-1,3-oxazolidin-5-yl)aryl boronic acid with a 7-halo-quinolone derivative. The quinolone derivatives possess antibacterial activity, and are effective against a number of human and veterinary pathogens in the treatment of bacterial diseases.Type: ApplicationFiled: November 29, 2001Publication date: January 16, 2003Inventors: Mikhail F. Gordeev, Dinesh V. Patel, Michael R. Barbachyn, James R. Gage
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Patent number: 5968962Abstract: A compound of the formula (I): ##STR1## or pharmaceutical acceptable salts thereof wherein X is NR.sub.1, S(O).sub.g, or O; R.sub.1 is H, C.sub.1-6 alkyl optionally substituted with one or more OH, CN, or halo, or R.sub.1 is --(CH.sub.2).sub.h -- aryl, --COR.sub.1--1, --COOR.sub.1-2, --CO--(CH.sub.2).sub.h --COR.sub.1--1, C.sub.1-6 alkyl sulfonyl, --SO.sub.2 --(CH.sub.2).sub.h --aryl, or --(CO).sub.i --Het; R.sub.2 is H, C.sub.1-6 alkyl, --(CH.sub.2).sub.h --aryl, or halo; R.sub.3 and R.sub.4 are the same or different and are H or halo; R.sub.5 is H, C.sub.1-12 alkyl optionally substituted with one or more halo, C.sub.3-12 cycloalkyl, C.sub.1-6 alkoxy. The compounds are useful antimicrobial agents.Type: GrantFiled: August 13, 1996Date of Patent: October 19, 1999Assignee: Pharmacia & Upjohn CompanyInventors: Richard C. Thomas, Toni-Jo Poel, Michael R. Barbachyn
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Patent number: 5958983Abstract: The present invention relates to polyaromatic compounds having useful antiviral activity against viruses of the herpes family, to a composition containing them, and to a method of using them for the treatment of herpes viruses infections.Type: GrantFiled: April 1, 1998Date of Patent: September 28, 1999Assignee: Pharmacia & Upjohn CompanyInventors: Michael R. Barbachyn, Fred L. Homa, Antonio Monge, Esteban Santiago, Juan J. Martinez-Irujo, Maria Font
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Patent number: 5952324Abstract: Phenyloxazolidinone compound of formula (I)or a pharmaceutically acceptable salt thereof characterized by a bicyclic thiazine or oxazine substituent. The compounds are useful antimicrobial agents, effective against a number of human and veterinary pathogens, including gram-positive aerobic bacteria such as multiply-resistant staphylococci, streptococci and enterococci as well as anaerobic organisms such as Bacteroides spp. and Clostridia spp. species, and acid-fast organisms such as Mycobacterium tuberculosis, Mycobacterium avium and Mycobacterium spp.Type: GrantFiled: May 14, 1997Date of Patent: September 14, 1999Assignee: Pharmacia & Upjohn CompanyInventors: Michael R. Barbachyn, Richard C. Thomas, Gary L. Cleek, Lisa M. Thomasco, Robert C. Gadwood
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Patent number: 5929248Abstract: The present invention discloses novel substituted aryl- and heteroarylphenyloxazolidinones which are useful as anti-bacterial agents. More specifically, the substituted aryl- and heteroarylphenyloxazolidinones of the invention are characterized by oxazolidinones having an aryl or heteroaryl group at the p-position of the 3-phenyl ring and additional substitutions at the m-position(s) of the 3-phenyl ring. A compound representative of this new class of oxazolidinones is (.+-.)-5-(acetamidomethyl)-3-?4-(3-pyridyl)-3,5-difluorophenyl!-2-oxazolid inone.Type: GrantFiled: April 23, 1997Date of Patent: July 27, 1999Assignee: Pharmacia & Upjohn CompanyInventors: Michael R. Barbachyn, Steven J. Brickner
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Patent number: 5883093Abstract: The present invention relates to antimicrobial phenyloxazolidinone compounds having a pyrrolidinyl or azetidinyl moiety.Type: GrantFiled: April 23, 1997Date of Patent: March 16, 1999Assignee: Pharmacia & Upjohn CompanyInventors: Douglas K. Hutchinson, Steven J. Brickner, Michael R. Barbachyn, Mikio Taniguchi, Kiyotaka Munesada, Hiroyoshi Yamada
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Patent number: 5880118Abstract: A compound of the Formula I: ##STR1## or pharmaceutically acceptable salts thereof wherein X, R, R.sup.1, R.sup.2, R.sup.3 and n are as defined in the disclosure. The oxazine and thiazine oxazolidinone derivatives are useful antimicrobial agents effective against a number of human and veterinary pathogens, including gram-positive aerobic bacteria such as multiply-resistant staphylococci, streptococci, and enterococci as well as anaerobic organisms such as Bacteroides spp. and Clostridia spp. species, and acid-fast organisms such as Mycobacterium tuberculosis, Mycobacterium avium and Mycobacterium spp.Type: GrantFiled: July 2, 1997Date of Patent: March 9, 1999Assignee: Pharmacia & Upjohn CompanyInventors: Michael R. Barbachyn, Steven J. Brickner, Douglas K. Hutchinson
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Patent number: 5837870Abstract: The present invention includes processes for producing 5-hydroxymethyl substituted oxazolidinone alcohols (III) from carbamates (IIA) or a trifluoroacetamide (IIB) using a dihydroxy compound (I) or glycidol (IV) starting material and for the transformation of the hydroxymethyl substituted oxazolidinone alcohols (III) to the corresponding amino compounds, 5-aminomethyl substituted oxazolidinone amines (VII) which are acylated to form commercially useful antibacterial 5-acylamidomethyl substituted oxazolidinone (VIII).Type: GrantFiled: March 28, 1997Date of Patent: November 17, 1998Assignee: Pharmacia & Upjohn CompanyInventors: Bruce A. Pearlman, William R. Perrault, Michael R. Barbachyn, Peter R. Manninen, Dana S. Toops, David J. Houser, Thomas J. Fleck
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Patent number: 5801246Abstract: The present invention discloses novel substituted aryl- and heteroarylphenyloxazolidinones which are useful as anti-bacterial agents. More specifically, the substituted aryl- and heteroarylphenyloxazolidinones of the invention are characterized by oxazolidinones having an aryl or heteroaryl group at the p-position of the 3-phenyl ring and additional substitutions at the m-position(s) of the 3-phenyl ring. A compound representative of this new class of oxazolidinones is (.+-.)-5-(acetamidomethyl)-3-?4-(3-pyridyl)-3,5-difluorophenyl!-2-oxazolid inone.Type: GrantFiled: June 6, 1995Date of Patent: September 1, 1998Assignee: Pharmacia & Upjohn CompanyInventors: Michael R. Barbachyn, Steven J. Brickner
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Patent number: 5756732Abstract: The present invention discloses novel substituted aryl- and heteroarylphenyloxazolidinones which are useful as anti-bacterial agents. More specifically, the substituted aryl- and heteroarylphenyloxazolidinones of the invention are characterized by oxazolidinones having an aryl or heteroaryl group at the p-position of the 3-phenyl ring and additional substitutions at the m-position(s) of the 3-phenyl ring. A compound representative of this new class of oxazolidinones is (.+-.)-5-(acetamidomethyl)-3-?4-(3-pyridyl)-3,5-difluorophenyl!-2-oxazolid inone.Type: GrantFiled: June 6, 1995Date of Patent: May 26, 1998Assignee: Pharmacia & Upjohn CompanyInventors: Michael R. Barbachyn, Steven J. Brickner
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Patent number: 5700799Abstract: A compound of structural Formula I: ##STR1## or pharmaceutically acceptable salts thereof wherein: each n is independently 1 to 3; Y is choosen from a-n as defined herein; wherein each occurrence of said C.sub.1-6 alkyl may be substituted with one or more F, Cl, Br, I, OR.sup.1, CO.sub.2 R.sup.1, CN, SR.sup.1, or R.sup.1 (where R.sup.1 is a hydrogen or C.sub.1-4 alkyl); X and Z are independently C.sub.1-6 alkyl, C.sub.3-12 cycloalkyl or hydrogen, or X and Z form a C.sub.0-3 bridging group, preferably X and Z are hydrogen; U, V and W are independently C.sub.1-6 alkyl, F, Cl, Br, hydrogen or a C.sub.1-6 alkyl substituted with one or more of F, Cl, Br or I, preferably U and V are F and W is hydrogen; R is hydrogen, C.sub.1-12 alkyl, C.sub.3-12 cycloalkyl, C.sub.1-6 alkoxy, C.sub.1-6 alkyl substituted with one or more F, Cl, Br, I or OH; and q is 0 to 4 inclusive.Type: GrantFiled: March 4, 1996Date of Patent: December 23, 1997Assignee: Pharmacia & Upjohn CompanyInventors: Douglas K. Hutchinson, Michael R. Barbachyn, Steven J. Brickner, Ronald B. Gammill, Mahesh V. Patel
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Patent number: 5688792Abstract: A compound of structural Formula I: ##STR1## or pharmaceutically acceptable salts thereof wherein: X is O, S, SO, SO.sub.2, SNR.sup.10 or S(O)NR.sup.10 ;R is (a) hydrogen,(b) C.sub.1 -C.sub.8 alkyl optionally substituted with one or more of the following: F, Cl, hydroxy, C.sub.1 -C.sub.8 alkoxy, C.sub.1 -C.sub.8 acyloxy or --O--CH.sub.2 --Ph,(c) C.sub.3 -C.sub.6 cycloalkyl,(d) amino,(e) C.sub.1 -C.sub.8 alkylamino,(f) C.sub.1 -C.sub.8 dialkylamino or(g) C.sub.1 -C.sub.8 alkoxy;R.sup.1 is H, except when X is O then R.sup.1 can be H, CH.sub.3, CN, CO.sub.2 H, CO.sub.2 R or (CH.sub.2).sub.m R.sup.11 (m is 1 or 2);R.sup.2 is independently H, F or Cl;R.sup.3 is H except when X is O and R.sup.1 is CH.sub.3 then R.sup.3 can be H or CH.sub.3 ;R.sup.10 is independently H, C.sub.1 -C.sub.4 alkyl (optionally substituted with chloro, fluoro, hydroxy, C.sub.1 -C.sub.8 alkoxy, amino, C.sub.1 -C.sub.8 alkylamino, or C.sub.1 -C.sub.8 dialkylamino) or p-toluenesulfonyl;R.sup.11 is hydrogen, OH, OR, OCOR, NH.sub.Type: GrantFiled: March 5, 1996Date of Patent: November 18, 1997Assignee: Pharmacia & Upjohn CompanyInventors: Michael R. Barbachyn, Steven J. Brickner, Douglas K. Hutchinson
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Patent number: 5654428Abstract: The present invention discloses novel substituted aryl- and heteroarylphenyloxazolidinones which are useful as anti-bacterial agents. More specifically, the substituted aryl- and heteroarylphenyloxazolidinones of the invention are characterized by oxazolidinones having aryl or heteroaryl group at the p-position of the 3-phenyl ring and additional substitutions at the m-position(s) of the 3-phenyl ring. A compound representative of this new class of oxazolidinones is (.+-.)-5-(acetamidomethyl)-3-[4-(3-pyridyl)-3,5-difluorophenyl]-2-oxazolid inone.Type: GrantFiled: June 6, 1995Date of Patent: August 5, 1997Assignee: Pharmacia & Upjohn CompanyInventors: Michael R. Barbachyn, Steven J. Brickner
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Patent number: 5654435Abstract: The present invention discloses novel substituted aryl- and heteroarylphenyloxazolidinones which are useful as anti-bacterial agents. More specifically, the substituted aryl- and heteroarylphenyloxazolidinones of the invention are characterized by oxazolidinones having an aryl or heteroaryl group at the p-position of the 3-phenyl ring and additional substitutions at the m-position(s) of the 3-phenyl ring. A compound representative of this new class of oxazolidinones is (.+-.)-5-(acetamidomethyl)-3-[4-(3-pyridyl)-3,5-difluorophenyl]-2-oxazolid inone.Type: GrantFiled: June 6, 1995Date of Patent: August 5, 1997Assignee: Pharmacia & Upjohn CompanyInventors: Michael R. Barbachyn, Steven J. Brickner
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Patent number: 5652238Abstract: A compound of structural Formula (I) or pharmaceutically acceptable salts thereof wherein: R is --C(O)--R.sup.1, --PO.sub.3 .dbd. or --P(O)(OH).sub.2 ; R.sup.1 is C.sub.1-6 alkyl, --N(R.sup.4).sub.2, C.sub.1-6 alkyl-N(R.sup.4).sub.2, --phenyl--N(R.sup.4).sub.2, --phenyl-NHC(O)CH.sub.2 NH.sub.2, --C.sub.2 H.sub.4 -morpholinyl, pyridinyl, C.sub.1-6 alkyl-OH, C.sub.1-6 alkyl-OCH.sub.3, C.sub.1-6 alkyl C(O)CH.sub.3, --O--C.sub.1-6 alkyl-OCH.sub.3, C.sub.0-3 alkyl-piperazinyl (optionally substituted with C.sub.1-3 alkyl), imidazolyl, C.sub.1-6 alkyl-COOH, --C(CH.sub.2 OH).sub.2 CH.sub.3 ; R.sup.2 and R.sup.3 are independently selected from hydrogen or F except at least one of R.sup.2 or R.sup.3 is F; R.sup.4 are independently selected from hydrogen or C.sub.1-6 alkyl.Type: GrantFiled: May 9, 1996Date of Patent: July 29, 1997Assignee: Pharmacia & Upjohn CompanyInventors: Steven J. Brickner, Michael R. Barbachyn, Douglas K. Hutchinson
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Patent number: 5565571Abstract: The present invention discloses novel substituted aryl- and heteroarylphenyloxazolidinones which are useful as anti-bacterial agents. More specifically, the substituted aryl- and heteroarylphenyloxazolidinones of the invention are characterized by oxazolidinones having an aryl or heteroaryl group at the p-position of the 3-phenyl ring and additional substitutions at the m-position(s) of the 3-phenyl ring. A compound representative of this new class of oxazolidinones is (.+-.)-5-(acetamidomethyl)-3-[4-(3-pyridyl)-3,5-difiuorophenyl]-2-oxazolid inone.Type: GrantFiled: April 28, 1994Date of Patent: October 15, 1996Assignee: The Upjohn CompanyInventors: Michael R. Barbachyn, Steven J. Brickner