Patents Represented by Attorney David M. Morse
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Patent number: 5760084Abstract: Retinoid-like activity is exhibited by compounds of the formula ##STR1## wherein X is F, Cl, OH or CH.sub.3, Y is H or F, R.sub.1 -R.sub.6 are each independently hydrogen or C.sub.1 -C.sub.6 alkyl, n is an integer of 1 to 4 and R.sub.7 is hydrogen or a carboxyl-protecting group, and pharmaceutically acceptable salts thereof. The compounds of the formula I selectively interact with the retinoic acid subtype RAR.gamma. and have been found to lack the liver toxicity associated with systemic administration of non-relative retinoids.Type: GrantFiled: October 4, 1996Date of Patent: June 2, 1998Assignee: Bristol-Myers Squibb CompanyInventors: R. Thomas Swann, Daniel Smith, Kenneth M. Tramposch, Fred Christopher Zusi
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Patent number: 5736578Abstract: Novel substituted fluorene compunds of Formula I are active as melatonergic agents: ##STR1## wherein: X=H, halogen, OH or OZ;Z=C.sub.1-6 alkyl; --(CH.sub.2).sub.m --CF.sub.3 (m=0-2); CD.sub.3 ; or ##STR2## n=1 or 2; and R=C.sub.1-6 alkyl, C.sub.3-6 cycloalkyl, C.sub.2-4 alkenyl, halogen substituted C.sub.1-6 alkyl, or C.sub.1-6 alkoxy substituted C.sub.1-6 alkyl.Type: GrantFiled: May 10, 1996Date of Patent: April 7, 1998Assignee: Bristol-Myers Squibb CompanyInventors: Brett T. Watson, Katherine S. Takaki, Joseph P. Yevich, James R. Epperson, George N. Karageorge, Karen L. Leboulluec
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Patent number: 5734047Abstract: Novel cephem derivatives represented by the general formula ##STR1## wherein Ar is an optionally substituted lipophilic phenyl, naphthyl, benzthiazolyl or pyridyl group; R.sup.1 represents a group of the formula ##STR2## in which R.sup.8 and R.sup.9 are each independently hydrogen, C.sub.1 -C.sub.6 alkyl or (C.sub.1 -C.sub.6)alkoxycarbonyl, said C.sub.1 -C.sub.6 alkyl group being optionally substituted by 1-5 hydroxy or C.sub.1 -C.sub.6 alkoxy groups; m is either 0 or 1; A is a C.sub.2 -C.sub.10 alkyl group optionally substituted by 1-5 hydroxy groups; and R.sup.2 and R.sup.3 are each independently hydrogen or C.sub.1 -C.sub.6 alkyl. The derivatives are gram-positive antibacterial agents especially useful in the treatment of diseases caused by methicillin-resistant Staphylococcus aureus.Type: GrantFiled: December 5, 1996Date of Patent: March 31, 1998Assignee: Bristol-Myers Squibb CompanyInventors: Choung U. Kim, Muzammil M. Mansuri, Peter F. Misco, John A. Wichtowski
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Patent number: 5668290Abstract: Novel cephem derivatives represented by the general formula ##STR1## in which the Acyl substituent is a group of the formula ##STR2## wherein Ar is a lipophilic optionally substituted phenyl, naphthyl or pyridyl group; R.sup.1 represents either the residue of a heterocyclic amino acid or a C.sub.2 -C.sub.10 alkyl group substituted by both a carboxyl group and a group of the formula --NR.sup.9 R.sup.10 or ##STR3## in which R.sup.9 and R.sup.10 are each independently hydrogen or C.sub.1 -C.sub.6 alkyl, said C.sub.2 -C.sub.10 alkyl group being optionally interrupted by one or more nitrogen atoms or carbonyl groups, and R.sup.2 and R.sup.3 are each independently hydrogen, alkyl or aminoalkyl are gram-positive antibacterial agents, especially useful in the treatment of diseases caused by methicillin-resistant Staphylococcus aureus (also referred to below as MRSA or methicillin-resistant S. aureus).Type: GrantFiled: August 23, 1996Date of Patent: September 16, 1997Assignee: Bristol-Myers Squibb CompanyInventors: Joanne J. Bronson, Stanley V. D'Andrea, Shelley E. Hoeft, John D. Matiskella, Peter F. Misco, Jr., Bing Yu Luh, Dane M. Springer, Yasutsugu Ueda, John A. Wichtowski
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Patent number: 5668284Abstract: Novel cephem derivatives represented by the general formula ##STR1## in which the Acyl substituent is a group of the formula ##STR2## wherein Ar is a lipophilic optionally substituted phenyl, naphthyl, pyridyl or benzthiazolyl group; R.sup.1 is selected from certain optionally substituted aliphatic, aromatic, arylaliphatic or sugar moieties and R.sup.2 and R.sup.3 are each independently hydrogen, alkyl or aminoalkylcarbonylamino are gram-positive antibacterial agents, especially useful in the treatment of infectious diseases caused by methicillin-resistant Staphylococcus aureus (MRSA).Type: GrantFiled: May 8, 1996Date of Patent: September 16, 1997Assignee: Bristol-Myers Squibb CompanyInventors: Choung U. Kim, Peter F. Misco, Jr., John A. Wichtowski, Yasutsugu Ueda, Thomas W. Hudyma, John D. Matiskella, Stanley V. D'Andrea, Shelley E. Hoeft, Raymond F. Miller, Muzammil M. Mansuri, Joanne J. Bronson
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Patent number: 5648385Abstract: The present invention relates to a compound of formula ##STR1## or a nontoxic pharmaceutically acceptable salt, physiologically hydrolyzable ester or solvate thereof, in whichX is --O--CO--, --NH--CO--, --CS--NH--, --CO--O--, --CO--NH--, --COS--, --SCO--, --SCH.sub.2 --, --CH.sub.2 --CH.sub.2 --, --C.tbd.C--, --CH.sub.2 --NH--, --COCH.sub.2 --, --NHCS--, --CH.sub.2 S--, --CH.sub.2 O--, --OCH.sub.2 --, --NHCH.sub.2 -- or --CR.sup.5 .dbd.CR.sup.6 --;R.sup.m and R.sup.k are independently hydrogen, halogen, C.sub.1-6 alkyl, hydroxy, C.sub.1-6 alkyloxy or nitro;n is zero or one;R.sup.4 is --(CH.sub.2).sub.t --Y, C.sub.1-6 alkyl, or C.sub.3-6 cycloalkyl;R.sup.1 is --CO.sub.2 Z, C.sub.1-6 alkyl, CH.sub.2 OH, --CONHR.sup.y, or CHO;R.sup.2 and R.sup.3 are independently hydrogen or C.sub.1-6 alkyl;R.sup.a and R.sup.b are independently hydrogen or C.sub.1-6 alkyl; but when n is one, R.sup.a and R.sup.Type: GrantFiled: June 5, 1995Date of Patent: July 15, 1997Assignee: Bristol-Myers Squibb Co.Inventors: John E. Starrett, Jr., Kuo-Long Yu, Muzammil M. Mansuri, David R. Tortolani, Peter R. Reczek
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Patent number: 5637694Abstract: This invention relates to a method of producing 3-alkanoyloxymethyl-3-cephem-4-carboxylic acids from 3-hydroxymethyl-3-cephem-4-carboxylic acids in an aqueous medium for a practical, large-scale production. Moreover, the invention provides an ideal intermediate for the process.Type: GrantFiled: April 5, 1996Date of Patent: June 10, 1997Assignee: Briston-Myers Squibb CompanyInventors: J. Gregory Reid, Paul R. Brodfuehrer, Patrick R. Smith
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Patent number: 5624957Abstract: Retinoid-like activity is exhibited by compounds of the formula ##STR1## wherein X is F, Cl, OH or CH.sub.3, Y is H or F, R.sub.1 -R.sub.6 are each independently hydrogen or C.sub.1 -C.sub.6 alkyl, n is an integer of 1 to 4 and R.sub.7 is hydrogen or a carboxyl-protecting group, and pharmaceutically acceptable salts thereof. The compounds of formula I selectively interact with the retinoic acid subtype RAR.gamma. and have been found to lack the liver toxicity associated with systemic administration of non-selective retinoids.Type: GrantFiled: June 6, 1995Date of Patent: April 29, 1997Assignee: Bristol-Myers Squibb CompanyInventors: R. Thomas Swann, Daniel Smith, Kenneth M. Tramposch, Fred C. Zusi
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Patent number: 5620969Abstract: Novel cephem derivatives represented by the general formula ##STR1## in which the Acyl substituent is a group of the formula ##STR2## wherein Ar is a lipophilic optionally substituted phenyl, naphthyl or pyridyl group; R.sup.1 represents either the residue of a heterocyclic amino acid or a C.sub.2 -C.sub.10 alkyl group substituted by both a carboxyl group and a group of the formula --NR.sup.9 R.sup.10 or ##STR3## in which R.sup.9 and R.sup.10 are each independently hydrogen or C.sub.1 -C.sub.6 alkyl, said C.sub.2 -C.sub.10 alkyl group being optionally interrupted by one or more nitrogen atoms or carbonyl groups, and R.sup.2 and R.sup.3 are each independently hydrogen, alkyl or aminoalkyl are gram-positive antibacterial agents, especially useful in the treatment of diseases caused by methicillin-resistant Staphylococcus aureus (also referred to below as MRSA or methicillin-resistant S. aureus).Type: GrantFiled: April 25, 1995Date of Patent: April 15, 1997Assignee: Bristol-Myers Squibb CompanyInventors: Joanne J. Bronson, Stanley V. D'Andrea, Shelley E. Hoeft, John D. Matiskella, Peter F. Misco, Jr., Bing Y. Luh, Dane M. Springer, Yasutsugu Ueda, John A. Wichtowski
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Patent number: 5618839Abstract: The present invention relates to a compound of formula I ##STR1## or a nontoxic pharmaceutically acceptable salt, physiologically hydrolyzable ester or solvate thereof, in whichX is --O--CO--, --NH--CO--, --CS--NH--, --CO--O--, --CO--NH--, --COS--, --SCO--, --SCH.sub.2 --, --CH.sub.2 --CH.sub.2 --, --C.tbd.C--, --CH.sub.2 --NH--, --COCH.sub.2 --, --NHCS--, --CH.sub.2 S--, --CH.sub.2 O--, --OCH.sub.2 --, --NHCH.sub.2 -- or --CR.sup.5 .dbd.CR.sup.6 --;R.sup.m and R.sup.k are independently hydrogen, halogen, C.sub.1-6 alkyl, hydroxy, C.sub.1-6 alkyloxy or nitro;n is zero or one;R.sup.4 is --(CH.sub.2).sub.t --Y, C.sub.1-6 alkyl, or C.sub.3-6 cycloalkyl;R.sup.1 is --CO.sub.2 Z, C.sub.1-6 alkyl, CH.sub.2 OH, --CONHR.sup.y, or CHO;R.sup.2 and R.sup.3 are independently hydrogen or C.sub.1-6 alkyl;R.sup.a and R.sup.b are independently hydrogen or C.sub.1-6 alkyl; but when n is one, R.sup.a and R.sup.Type: GrantFiled: May 2, 1996Date of Patent: April 8, 1997Assignee: Bristol-Myers Squibb CompanyInventors: John E. Starrett, Jr., Kuo-Long Yu, Muzammil M. Mansuri, David R. Tortolani, Peter R. Reczek
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Patent number: 5567698Abstract: Novel cephem derivatives represented by the general formula ##STR1## in which the Acyl substituent is a group of the formula ##STR2## wherein Ar is a lipophilic optionally substituted phenyl, naphthyl, pyridyl or benzthiazolyl group; R.sup.1 is selected from certain optionally substituted aliphatic, aromatic, arylaliphatic or sugar moieties and R.sup.2 and R.sup.3 are each independently hydrogen, alkyl or aminoalkylcarbonylamino are gram-positive antibacterial agents, especially useful in the treatment of infectious diseases caused by methicillin-resistant Staphylococcus aureus (MRSA).Type: GrantFiled: May 30, 1995Date of Patent: October 22, 1996Assignee: Bristol-Myers Squibb CompanyInventors: Choung U. Kim, Peter F. Misco, Jr., John A. Wichtowski, Yasutsugu Ueda, Thomas W. Hudyma, John D. Matiskella, Stanley V. D'Andrea, Shelley E. Hoeft, Raymond F. Miller, Muzammil M. Mansuri, Joanne J. Bronson
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Patent number: 5559248Abstract: This invention relates to a compound of formula I ##STR1## in which T is --CONH-- or --CH.dbd.CH--;R.sup.a and R.sup.b are independently C.sub.1-6 alkyl;R.sup.c is C.sub.1-6 alkyl or hydrogen; andR is heteroaryl and these compounds are useful in preventing and treating skin disorders.Type: GrantFiled: April 5, 1995Date of Patent: September 24, 1996Assignee: Bristol-Myers Squibb Co.Inventors: John E. Starrett, Jr., David R. Tortolani, Muzammil M. Mansuri, Nicholas A. Meanwell
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Patent number: 5559108Abstract: Novel cephem derivatives represented by the general formula ##STR1## in which the Acyl substituent is a group of the formula ##STR2## where Ar is a substituted phenyl or optionally substituted naphthyl or benzthiazolyl group and A is a substituted-pyridinium group are gram-positive antibiotics, especially useful in the treatment of diseases caused by methicillin-resistant Staphylococcus aureus.Type: GrantFiled: May 22, 1995Date of Patent: September 24, 1996Assignee: Bristol-Myers Squibb CompanyInventors: Choung U. Kim, Muzammil M. Mansuri, Peter F. Misco, Jr., John A. Wichtowski, Joanne J. Bronson, Stanley V. D'Andrea, Thomas W. Hudyma
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Patent number: 5552542Abstract: This invention relates to a method of producing 3-alkanoyloxymethyl-3-cephem-4-carboxylic acids from 3-hydroxymethyl-3-cephem-4-carboxylic acids in an aqueous medium for a practical, large-scale production. Moreover, the invention provides an ideal intermediate for the process.Type: GrantFiled: May 10, 1995Date of Patent: September 3, 1996Assignee: Bristol-Myers Squibb CompanyInventors: J. Gregory Reid, Paul R. Brodfuehrer, Patrick R. Smith
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Patent number: 5162330Abstract: The novel antitumor antibiotic designated herein as dynemicin C is produced by fermentation of Micromonospora chersina M956-1 mutant F1085 (ATCC-55077). Dynemicin C and its triacetate derivative possess antibacterial and antifungal activity and also inhibit the growth of mammalian tumors.Type: GrantFiled: November 5, 1990Date of Patent: November 10, 1992Assignee: Bristol-Myers Squibb Co.Inventors: Kyoichiro Saitoh, Takeo Miyaki, Haruaki Yamamoto, Nahomi Oda
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Patent number: 5143906Abstract: Kedarcidin chromophore, a non-protein chromophore isolated from kedarcidin antitumor antibiotic, is obtained from purified or partially purified kedarcidin by solvent extraction and chromatographic procedures. The chromophore is characterized and found to contain substantially all of the antitumor activity of kedarcidin.Type: GrantFiled: September 26, 1991Date of Patent: September 1, 1992Assignee: Bristol-Myers Squibb CompanyInventor: John E. Leet
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Patent number: 5124150Abstract: Production of an antiviral antibiotic complex, BU-3889V and its bioactive components A.sub.1, A.sub.2, A.sub.3, D.sub.1, D.sub.2 and D.sub.3, by fermentation of a BU-3889V producing strain of the new microorganism Amycolatopsis orientalis ATCC-53884 is disclosed. Complex BU-3889V is recovered and the components separated by the use of ion exchange chromatography techniques. The bioactive components are characterized by their physico-chemical characterizing properties. The products have been found to be effective to inhibit viruses including herpes simplex virus, human immunodeficiency virus (HIV) and influenza virus.Type: GrantFiled: March 11, 1991Date of Patent: June 23, 1992Assignee: Bristol-Myers Squibb Co.Inventors: Masataka Konishi, Mitsuaki Tsunakawa, Osamu Tenmyo, Takeo Miyaki, Toshikazu Oki
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Patent number: 5116845Abstract: The novel antitumor antibiotic designated herein as BU-3420T is produced by fermentation of Micromonospora chersina strain M956-1 (ATCC 53710). BU-3420T and its triacetate derivative possess antibacterial and antifungal activity and also inhibit the growth of mammalian tumors such as P388 leukemia in mice.Type: GrantFiled: May 4, 1990Date of Patent: May 26, 1992Assignee: Bristol-Myers CompanyInventors: Hiroaki Ohkuma, Masataka Konishi, Kiyoshi Matsumoto, Toshikazu Oki, Yutaka Hoshino
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Patent number: 5098708Abstract: Production of an antiviral antibiotic complex, BU-3889V and its bioactive components A.sub.1, A.sub.2, A.sub.3, D.sub.1, D.sub.2 and D.sub.3, by fermentation of a BU-3889V producing strain of the new microorganism Amycolatopsis orientalis ATCC-53884 is disclosed. Complex BU-3889V is recovered and the components separated by the use of ion exchange chromatography techniques. The bioactive components are characterized by their physico-chemical characterizing properties. The products have been found to be effective to inhibit viruses including herpes simplex virus, human immunodeficiency virus (HIV) and influenza virus.Type: GrantFiled: July 6, 1990Date of Patent: March 24, 1992Assignee: Bristol-Myers Squibb CompanyInventors: Masataka Konishi, Mitsuaki Tsunakawa, Osamu Tenmyo, Takeo Miyaki, Toshikazu Oki
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Patent number: H1649Abstract: Combinations of certain HIV-1 protease inhibitors are provided which effectively inhibit the HIV-1 protease enzyme while eliminating or substantially reducing the viral cross-resistance seen with use of individual HIV-1 protease inhibitors. Such combinations are useful in the treatment of diseases associated with the AIDS virus.Type: GrantFiled: May 17, 1995Date of Patent: May 6, 1997Inventors: Joel C. Barrish, Richard J. Colonno, Pin-Fang M. Lin