Patents by Inventor Burton G. Christensen
Burton G. Christensen 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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Publication number: 20090111737Abstract: This invention relates to novel multibinding compounds (agents) that are antibacterial agents. The multibinding compounds of the invention comprise from 2-10 ligands covalently connected by a linker or linkers, wherein each of said ligands in their monovalent (i.e., unlinked) state have the ability to bind to a an enzyme involved in cell wall biosynthesis and metabolism, a precursor used in the synthesis of the bacterial cell wall and/or the bacterial cell surface thereby interfere with the synthesis and/or metabolism of the cell wall.Type: ApplicationFiled: April 11, 2008Publication date: April 30, 2009Inventors: Burton G. Christensen, Edmund J. Moran, John H. Griffin, J. Kevin Judice, YongQi Mu, John L. Pace, Mathai Mammen, James Aggen
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Publication number: 20040023290Abstract: Novel multi-binding compounds are disclosed that modulate enzymatic processes. The compounds of the invention comprise from 2-10 ligands covalently connected, each of said ligands being capable of binding to an enzyme, enzyme substrate or enzyme cofactor thereby modulating the biological processes/functions thereof.Type: ApplicationFiled: June 3, 2002Publication date: February 5, 2004Inventors: John H. Griffin, J. Kevin Judice, Burton G. Christensen, Thomas E. Jenkins
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Publication number: 20030087306Abstract: Disclosed are novel multi-binding compounds (agents) which bind cellular receptors. The compounds of this invention comprise a plurality of ligands each of which can bind to such cellular receptors thereby modulating the biological processes/functions thereof. Each of the ligands is covalently attached to a linker or linkers which may be the same of different to provide for the multi-binding compound. The linker is selected such that the multi-binding compound so constructed demonstrates increased modulation or disruption of the biological processes/functions of the cell. Also disclosed is a method for identifying such novel multi-binding compounds which bind cellular receptors and a method for generating a mixture of such novel multi-binding compounds.Type: ApplicationFiled: December 13, 2001Publication date: May 8, 2003Inventors: Burton G. Christensen, John H. Griffin, Thomas E. Jenkins, J. Kevin Judice
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Publication number: 20030060663Abstract: Disclosed are novel multibinding compounds (agents) which bind macromolecular structures including cellular, extracellular, and microbial components derived from vectors, viruses, fungi, yeasts, bacteria, and the like. The compounds of this invention comprise a plurality of ligands each of which can bind to such macromolecular structures thereby modulating the biological processes/functions thereof. Each of the ligands is covalently attached to a linker (framework) to provide for the multibinding compound. The linker is selected such that the multibinding compound so constructed demonstrates increased modulation or disruption of the biological processes/functions of cell as compared to the aggregate of the individual units of the ligand.Type: ApplicationFiled: March 8, 2002Publication date: March 27, 2003Inventors: John H. Griffin, Burton G. Christensen, Thomas E. Jenkins, J. Kevin Judice
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Publication number: 20030044845Abstract: Novel multi-binding compounds (agents) are disclosed which bind cell membrane transporters including ion channels, molecular transporters and ion pumps. The compounds of this invention comprise from 2 to 10 ligands each of which can bind to such cellular transporters to modulate the biological processes/functions thereof. Each of the ligands is covalently attached to a linker (framework) to provide for a multi-binding compound. The linker is selected such that the multi-binding compound exhibits increased modulation of the biological processes/functions of the transporter as compared to the aggregate of the individual ligand units made available for binding to the transporter.Type: ApplicationFiled: February 13, 2002Publication date: March 6, 2003Inventors: Thomas E. Jenkins, Burton G. Christensen, John H. Griffin, J. Kevin Judice
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Publication number: 20030008812Abstract: Disclosed are derivatives of glycopeptide antibiotic compounds having at least one substituent of the formula:Type: ApplicationFiled: February 2, 2001Publication date: January 9, 2003Inventors: Burton G. Christensen, J. Kevin Judice, YongQi Mu
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Patent number: 5789584Abstract: The present invention includes (7R)-7-(acylamino)-3-(substituted-pyridinyl)-3-cephem-4-carboxylic acids or their pharmacologically acceptable salts which exhibit antibiotic activity against methicillin-resistant bacteria and are therefore useful as antibacterial agents.Type: GrantFiled: March 29, 1995Date of Patent: August 4, 1998Assignee: Microcide Pharmaceuticals, Inc.Inventors: Burton G. Christensen, In-Seop Cho, Tomasz W. Glinka, Scott J. Hecker
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Patent number: 5607926Abstract: The present invention includes novel (7R)-7-(acylamino)-3-(arylthio)-3-cephem-4-carboxylic acids or their pharmacologically acceptable salts which exhibit antibiotic activity against a wide spectrum of organisms including organisms which are resistant to .beta.-lactam antibiotics and are useful as antibacterial agents. The invention also relates to novel intermediates useful for making the novel compounds of the present invention and to novel methods for producing the novel compounds and intermediate compounds.Type: GrantFiled: March 29, 1995Date of Patent: March 4, 1997Assignee: Microcide Pharmaceuticals, Inc.Inventors: Scott J. Hecker, In-Seop Cho, Burton G. Christensen, Tomasz W. Glinka
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Patent number: 5593986Abstract: The present invention includes novel (7R)-7-(acylamino)-3-(arylthio)-3-cephem-4-carboxylic acids or their pharmacologically acceptable salts which exhibit antibiotic activity against a wide spectrum of organisms including organisms which are resistant to .beta.-lactam antibiotics and are useful as antibacterial agents. The invention also relates to novel intermediates useful for making the novel compounds of the present invention and to novel methods for producing the novel compounds and intermediate compounds.Type: GrantFiled: March 29, 1995Date of Patent: January 14, 1997Assignee: Microcide Pharmaceuticals, Inc.Inventors: Burton G. Christensen, In-Seop Cho, Tomasz W. Glinka, Scott J. Hecker
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Patent number: 5547978Abstract: The invention relates to derivatives of pyrrolidin-2-ylcarbonylheterocyclic compound of the general formula ##STR1## in which R.sup.1 represents C.sub.1-6 alkyl, C.sub.1-20 cycloalkyl, aryl or heteroaryl,R.sup.2 represents a heterocyclic compound selected from the group consisting of 2-thiazole, 2-oxazole, 2-imidazole, 2-pyrrole, 2-thiophene, 2-benzothiazole, 2-benzoxazole, 2-benzimidazole, 2-indole, 2-thiazolo[5,4-b]pyridine, 2-oxazolo[4,5-b]pyridine, 2-imidazo[4,5-b]pyridine, 5-thiazole, 2-thiazoline, 2-pyridine, 3-pyridine, 5-pyrimidine, 2-pyrazine, 2-triazole or 2-pyrazole wherein the heterocyclic compound may be unsubstituted or substituted independently with R.sup.4 or R.sup.5 wherein R.sup.4 and R.sup.5 are H, C.sub.1-5 alkyl, aryl or R.sup.4 and R.sup.Type: GrantFiled: November 23, 1994Date of Patent: August 20, 1996Assignee: Meiji Seika Kaisha, Ltd.Inventors: Burton G. Christensen, Takashi Egawa, Yasuyuki Ichimaru, Shokichi Ohuchi, Tsuneo Okonogi, Arthur A. Patchett, Seiji Shibahara, Seiji Tsutsumni
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Patent number: 5140030Abstract: Disclosed are 2-aza-substituted 1-carbadethiapen-2-em-3-carboxylic acids. I, where the generic 2-aza group includes azido, acylamino, amino, alkylamino, dialkylamino, triazolyl, triazolinyl, aziridinyl, and their pharmaceutically acceptable salt, ester, anhydride and amide derivatives which are useful as antibiotics. Also disclosed are processes for the preparation of I from the known, appropriately substituted bicyclic keto ester II via the 2-azido central intermediate III: ##STR1## wherein R.sup.16 is H or CH.sub.3, preferably beta-methyl; R.sup.6, and R.sup.7 are independently hydrogen, linear, branched or cyclic C.sub.1 -C.sub.5 alkyl, which can be substituted with fluoro, hydroxy, protected hydroxy, sulfoxy, amino, protected amino, wherein R.sup.6 and R.sup.7 taken together can also be C.sub.2 -C.sub.4 alkylidene, similarly substituted; with the proviso that both R.sup.6 and R.sup.7 are not unsubstituted alkyl, R.sup.1 and R.sup.Type: GrantFiled: August 16, 1990Date of Patent: August 18, 1992Assignee: MerckInventors: Burton G. Christensen, Ronald W. Ratcliffe, John C. Chabala
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Patent number: 5137884Abstract: N-tetrazolyl beta-lactams of the Formula: ##STR1## and the pharmaceutically acceptable salts thereof wherein R.sup.2 is hydrogen, alkyl having 1 to 6 carbon atoms or carboalkoxy having 2 to 7 carbon atoms; andZ is ##STR2## and W is ##STR3## thus forming a zwitterion, or Z is ##STR4## wherein R.sup.1 is benzyl, phenyloxymethyl or ##STR5## wherein Y is alkoxy or substituted alkoxy having 1 to 6 carbon atoms wherein the substituent on the alkoxy group is --COOH; andW is ##STR6## wherein R.sup.3 is H, M or --CH.sub.2 COOM, wherein M is a pharmaceutically acceptable cation are disclosed. The compounds are useful as antibiotics.Type: GrantFiled: November 16, 1983Date of Patent: August 11, 1992Assignee: Merck & Co., Inc.Inventors: W. Alexander Andrus, Burton G. Christensen, James V. Heck
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Patent number: 5055573Type: GrantFiled: August 24, 1990Date of Patent: October 8, 1991Assignee: Merck & Co., Inc.Inventors: Lovji D. Cama, Burton G. Christensen
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Patent number: 5021566Abstract: Disclosed are 6- and 6,6-disubstituted-3-substituted-1-azabicyclo[3.2.0]hept-2-en-7-one-2-carbo xylic acids (I): ##STR1## wherein R.sup.1 and R.sup.2 are, inter alia, independently selected from the group consisting of hydrogen (both are not hydrogen at the same time), substituted and unsubstituted: alkyl, aryl and aralkyl; X is halo, oxygen (the 2-3 bond is saturated and the species I exists as carboxylate salt or ester), or --OR wherein R is, inter alia, acyl, alkyl, or aralkyl. Such compounds and their pharmaceutically acceptable salt, ester and amide derivatives are useful as antibiotics. Also disclosed are processes for the preparation of such compounds, pharmaceutical compositions comprising such compounds and methods of treatment comprising administering such compounds and compositions when an antibiotic effect is indicated.Type: GrantFiled: February 15, 1990Date of Patent: June 4, 1991Assignee: Merck & Co. Inc.Inventors: Burton G. Christensen, Ronald W. Ratcliff
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Patent number: 4997936Abstract: Disclosed are 2- and 6-substituted-1-carbadethiapen-2-em-3-carboxylic acids having the structure: ##STR1## wherein R.sup.6, and R.sup.7 are, inter alia, independently selected from the group consisting of hydrogen, alkyl, alkenyl, aryl and aralkyl; A is a direct, single bond connecting the indicated S and C atoms, or A is a cyclic or acyclic connecting group selected, inter alia, from alkyl, cyclalkyl, aryl, heteroaryl, heteroalkyl; R.sup.1 and R.sup.2 inter alia, independently selected from hydrogen, alkyl, aryl; additionally, said carbamimidoyl is characterized by cyclic structures achieved by the joinder of the two nitrogen atoms via their substituents and by their joinder to connecting group A; additionally, "carbamimidiums" are disclosed by quarternization of one of the nitrogen atoms of said carbammidoyl. Such compounds as well as their pharmaceutically acceptable salt, ester and amide derivatives are useful as antibiotics.Type: GrantFiled: August 21, 1986Date of Patent: March 5, 1991Assignee: Merck & Co., Inc.Inventors: Burton G. Christensen, David B. R. Johnston, Susan M. Schmitt
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Patent number: 4994568Abstract: Disclosed are 6- and 4-substituted-1-azabicyclo[3.2.0]heptan-3,7-dione-2-carboxylic acid esters and salts (I) which are useful in the preparation of 6-, 1- and 2-substituted carbapenem antibiotics. ##STR1## wherein R.sup.5 is a pharmaceutically acceptable ester moiety or a removable protecting group or an alkali or alkaline earth metal cation such as sodium or potassium and wherein R.sup.1, R.sup.2, Rhu 3 and R.sup.4 are, inter alia, independently selected from the group consisting of hydrogen, alkyl, aryl and aralkyl. Another embodiment disclosed is a group of compounds having the formula ##STR2## where X is a leaving group.Type: GrantFiled: February 15, 1990Date of Patent: February 19, 1991Assignee: Merck & Co., Inc.Inventor: Burton G. Christensen
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Patent number: 4992542Abstract: Disclosed are 2- and 6-substituted-1-carbadethiapen-2-em-3-carboxylic acids having the structure: ##STR1## wherein R.sup.6, R.sup.7 and R.sup.8 are inter alia, independently selected from the group consisting of hydrogen, alkyl, alkenyl, aryl and aralkyl. Such compounds as well as their pharmaceutically acceptable salt, ester and amide derivatives are useful as antibiotics. Also disclosed are processes for the preparation of such compounds, pharmaceutical compositions comprising such compounds and methods of treatment comprising administering such compounds and compositions when an antibiotic effect is indicated.Type: GrantFiled: February 26, 1987Date of Patent: February 12, 1991Assignee: Merck & Co., Inc.Inventors: Burton G. Christensen, David B. R. Johnston, Susan M. Schmitt
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Patent number: 4892869Abstract: Disclosed are 2-aza-substituted 1-carbadethiapen-2-em-3-carboxylic acids I, where the generic 2-aza group includes azido, acylamino, amino, alkylamino, dialkylamino, triazolyl, triazolinyl, aziridinyl, and their pharmaceutically acceptable salt, ester, anhydride and amide derivatives which are useful as antibiotics. Also disclosed are processes for the preparation of 1 from the known, appropriately substituted bicyclic keto ester II via the 2-azido central intermediate III: ##STR1## wherein R.sup.16 is H or CH.sub.3, preferably beta-methyl; R.sup.6, and R.sup.7 are independently hydrogen, linear, branched or cyclic C.sub.1 -C.sub.5 alkyl, which can be substituted with fluoro, hydroxy, protected hydroxy, sulfoxy, amino, protected amino, wherein R.sup.6 and R.sup.7 taken together can also be C.sub.2 -C.sub.4 alkylidene, similarly substituted; with the proviso that both R.sup.6 and R.sup.7 are not unsubstituted alkyl, R.sup.1 and R.sup.Type: GrantFiled: January 19, 1989Date of Patent: January 9, 1990Assignee: Merck & Co., Inc.Inventors: Burton G. Christensen, Ronald W. Ratcliffe, John C. Chabala
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Patent number: 4873324Abstract: Compounds are disclosed of the structural formula: ##STR1## wherein R.sup.2 is independently selected from hydrogen, linear or branched C.sub.1 -C.sub.3 alkyl, which can be substituted with fluoro, hydroxy, or protected hydroxy, R.sup.3 is hydrogen or a protecting group, X is sulfur or selenium, Q is hydroxymethyl, carboxy or C.sub.1 -C.sub.4 alkoxycarbonyl, and R.sup.1 is C.sub.1 -C.sub.4 alkyl, C.sub.6 -C.sub.10 aryl, or pyridyl which can be substituted with C.sub.1 -C.sub.4 alkyl, alkoxy and nitro; such compound are useful for selectively obtaining 1-.beta.-methylcarbapenem intermediates.Type: GrantFiled: February 6, 1989Date of Patent: October 10, 1989Assignee: Merck & Co., Inc.Inventors: Burton G. Christensen, Lovji D. Cama, Susan M. Schmitt
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Patent number: 4839352Abstract: Disclosed are N-acyl derivatives of the antibiotic thienamycin having the following structural formula: ##STR1## wherein R.sup.1 and R.sup.2 are independently selected from the group consisting of hydrogen and acyl. Such derivatives and their pharmaceutically acceptable salts, are useful as antibiotics. Also disclosed are processes for the preparation of such derivatives, pharmaceutical compositions comprising such derivatives, and methods of treatment comprising administering such derivatives and compositions when an antibiotic effect is indicated.Type: GrantFiled: August 27, 1987Date of Patent: June 13, 1989Assignee: Merck & Co., Inc.Inventors: Louis Barash, Burton G. Christensen, John Hannah, William J. Leanza, David H. Shih