Abstract: A novel tyrosyl diester antibiotic is obtained from fermentation of a recombinant strain of Streptomyces lividans designated Stretomyces lividans WD 15684 (ATCC-202143). The new antibiotic, designated tyrissamycin, exhibits antibacterial activity, particularly against gram-positive bacteria.
Type:
Grant
Filed:
November 18, 2004
Date of Patent:
August 14, 2007
Assignee:
Bristol-Myers Squibb Company
Inventors:
Jingfang Q. Cutrone, Lyndon M. Foster, Kimberly D. Krampitz, Stephen W. Mamber, Grace A. McClure, Todd C. Peterson, Lisa C. Rupar, Katie A. Thompson
Abstract: A high drug load enteric coated pharmaceutical composition is provided which includes a core in the form of a tablet and which is comprised of a medicament which is sensitive to a low pH environment of less than 3, such as ddl, and having an enteric coating formed of methacrylic acid copolymer and a plasticizer. The tablets may be of varying sizes and may be orally ingested individually or a plurality of tablets sufficient to attain a desired dosage may be encapsulated in a dissolvable capsule. The tablets have excellent resistance to disintegration at pH less than 3 but have excellent drug release properties at pH greater than 4.5. A novel method of making said pharmaceutical composition is also disclosed.
Abstract: Inhibitors of the cytosolic phospholypase A2 enzymes are provided which are of use in controlling a wide variety of inflammatory diseases. The inhibitors of the present invention have the general formula
where X, Z, X1, R1, R2, Ra and Rb are as defined in the specification.
Type:
Grant
Filed:
February 8, 2001
Date of Patent:
December 10, 2002
Assignee:
Bristol-Myers Squibb Company
Inventors:
Jacques Banville, Serge Plamondon, Yonghua Gai, Neelakantan Balasubramanian
Abstract: Water-soluble prodrugs of triazole antifungal compounds having a secondary or tertiary hydroxy group are provided. More particularly, new water-soluble triazole antifungal compounds are provided having the general formula
wherein A is the non-hydroxy portion of a triazole antifungal compound of the type containing a secondary or tertiary hydroxyl group and n, R1 and R2 are as defined in the specification.
Type:
Grant
Filed:
February 21, 2001
Date of Patent:
November 26, 2002
Assignee:
Bristol-Myers Squibb Company
Inventors:
Thomas W. Hudyma, Oak K. Kim, Xiaofan Zheng
Abstract: This invention describes isoxazolinone derivatives which possess antibacterial activity and are useful in the treatment of bacterial diseases. More particularly, new isoxazolinones are provided having the general formula I
wherein R1, R2, R3, L and L1 are as described in the specification.
Type:
Grant
Filed:
June 28, 2001
Date of Patent:
October 15, 2002
Assignee:
Bristol-Myers Squibb Company
Inventors:
Dane M. Springer, Jason T. Goodrich, Zhaoxing Meng, Lawrence B. Snyder
Abstract: Water-soluble prodrugs of triazole antifungal compounds having a secondary or tertiary hydroxy group are provided. More particularly, new water-soluble triazole antifungal compounds are provided having the general formula
wherein A is the non-hydroxy portion of a triazole antifungal compound of the type containing a secondary or tertiary hydroxyl group and n, m, p, R1, R2, R3, and R4 are as defined in the specification.
Type:
Grant
Filed:
September 28, 2001
Date of Patent:
October 1, 2002
Assignee:
Bristol-Myers Squibb Company
Inventors:
Thomas W. Hudyma, Oak K. Kim, Xiaofan Zheng
Abstract: An improved process is provided for preparing water-soluble prodrugs of triazole antifungal compounds containing a secondary or tertiary hydroxyl group. More particularly, the improved process is directed toward preparation of water-soluble triazole antifungal compounds are provided having the general formula
wherein A is the non-hydroxy portion of a triazole antifungal compound of the type containing a secondary or tertiary hydroxyl group and R and R1 are as defined in the specification.
Type:
Grant
Filed:
October 16, 2001
Date of Patent:
September 10, 2002
Assignee:
Bristol-Myers Squibb Company
Inventors:
Chung-Pin Chen, Timothy Paul Connolly, Laxma Reddy Kolla, John D. Matiskella, Richard H. Mueller, Yadagiri Pendri, Dejah T. Petsch
Abstract: The present invention relates to antifungal compounds having the structural formula:
and pharmaceutically acceptable salts, solvates and prodrugs thereof. The present invention further relates to pharmaceutical compositions containing said compound, or a pharmaceutically acceptable salt, solvate or prodrug thereof, for use in the treatment of a fungal infection in an animal host.
Type:
Grant
Filed:
September 14, 2001
Date of Patent:
August 20, 2002
Assignee:
Bristol-Myers Squibb Company
Inventors:
Michael Serrano-Wu, Xuhua Du, Neelakantan Balasubramanian, Denis R. St. Laurent
Abstract: Inhibitors of the cytosolic phospholipase A2 enzymes are provided which are of use in controlling a wide variety of inflammatory diseases. The inhibitors of the present invention have the general formula
where X, Z, R1, R2, R3, R4, Ra and Rb are as defined in the specification.
Type:
Grant
Filed:
March 23, 2001
Date of Patent:
July 2, 2002
Assignee:
Bristol-Myers Squibb Company
Inventors:
Jacques Banville, Anne Marinier, Yonghua Gai, Serge Plamondon, Stephan Roy, Neelakantan Balasubramanian
Abstract: There are provided in accordance with the present invention crystalline gatifloxacin pentahydrate represented by the formula
in a highly homogeneous form with respect to other crystalline forms thereof.
Type:
Grant
Filed:
August 17, 2001
Date of Patent:
July 2, 2002
Assignee:
Bristol-Myers Squibb Company
Inventors:
Krishnaswamy S. Raghavan, Sunanda A. Ranadive, Jack Z. Gougoutas, John D. DiMarco, William L. Parker, Martha Davidovich, Ann Newman
Abstract: The present invention relates to a process for the preparation of &agr;′ chloroketones, such as 4-phenyl-3-t-butyloxy-carbonylamino)-2-keto-1-chlorobutane by reacting certain aryl amino acid esters, e.g. N-(2-t-butoxycarbonyl)-L-phenylalanine-4-nitrophenyl ester, with a sulfur ylide compound to form the corresponding keto ylide compound which is then treated with a source of chloride and an organic acid.
Abstract: Water-soluble prodrugs of triazole antifungal compounds having a secondary or tertiary hydroxy group are provided. More particularly, new water-soluble triazole antifungal compounds are provided having the general formula
wherein A is the non-hydroxy portion of a triazole antifungal compound of the type containing a secondary or tertiary hydroxyl group and R and R1 are as defined in the specification.
Type:
Grant
Filed:
January 10, 2001
Date of Patent:
March 26, 2002
Assignee:
Bristol-Myers Squibb Company
Inventors:
Yasutsugu Ueda, John D. Matiskella, Jerzy Golik, Thomas W. Hudyma, Chung-Pin Chen
Abstract: Water-soluble prodrugs of triazole antifungal compounds having a secondary or tertiary hydroxy group are provided. More particularly, new water-soluble triazole antifungal compounds are provided having the general formula
wherein A is the non-hydroxy portion of a triazole antifungal compound of the type containing a secondary or tertiary hydroxyl group and n, R1 and R2 are as defined in the specification.
Type:
Grant
Filed:
February 21, 2001
Date of Patent:
March 19, 2002
Assignee:
Bristol-Myers Squibb Company
Inventors:
Thomas W. Hudyma, Oak K. Kim, Xiaofan Zheng
Abstract: Selective inhibitors of the cPLA2 enzymes are provided which are of use in controlling a wide variety of inflammatory diseases. The inhibitors of the present invention have the general formula
where (R′), p, D, Y, Z, Ra, Rb and A are as defined in the specification.
Type:
Grant
Filed:
February 18, 2000
Date of Patent:
February 26, 2002
Assignee:
Bristol-Myers Squibb Company
Inventors:
Jacques Banville, Yonghua Gai, Graham Johnson, Fred Christopher Zusi, James R. Burke
Abstract: Disclosed is the (R)-enantiomer of the formula
which has unexpectedly been found to possess all of the biological activity of the racemic compound disclosed in the prior art as an RAR&ggr;-specific agonist.
Type:
Grant
Filed:
September 21, 1999
Date of Patent:
December 18, 2001
Assignee:
Bristol-Myers Squibb Company
Inventors:
Makonen Belema, Fred C. Zusi, Kenneth M. Tramposch
Abstract: A novel tyrosyl diester antibiotic is obtained from fermentation of a recombinant strain of Streptomyces lividans designated Streptomyces lividans WD 15684 (ATCC-202143). The new antibiotic, designated tyrissamycin, exhibits antibacterial activity, particularly against gram-positive bacteria.
Type:
Grant
Filed:
August 20, 1999
Date of Patent:
December 11, 2001
Assignee:
Bristol-Myers Squibb Company
Inventors:
Jingfang Cutrone, Lyndon M. Foster, Kimberly Krampitz, Stephen W. Mamber, Grace McClure, Todd C. Peterson, Lisa C. Rupar, Katie A. Thompson
Abstract: An improved process is provided for synthesis of a halomethyl benzoic acid chloromethyl ester, a key intermediate for use in production of azole antifungal compounds and other pharmaceutical products.