Carbon In The Ring Patents (Class 558/288)
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Patent number: 7635595Abstract: The spectroscopic and photophysical properties of fluorescent probes comprising donor-acceptor derivatives comprising the boric acid group or a derivative of boric acid, B(OH)3 (or borate ion, BO(OH)2?1), arsenious acid, H3 AsO3 (or arsenite ion, H2AsO3?1), telluric acid, H6TeO6 (or tellurate ion, H5 TeO6?1) or germanic acid, Ge(OH)6 (or germanate ion, GeO(OH)3?1) are described. Method of using said probes are also provided.Type: GrantFiled: March 10, 2005Date of Patent: December 22, 2009Inventors: Joseph R. Lakowicz, Nicolas Dicesare
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Patent number: 7582621Abstract: This invention relates to compounds useful for treating fungal infections, more specifically topical treatment of onychomycosis and/or cutaneous fungal infections. This invention is directed to compounds that are active against fungi and have properties that allow the compound, when placed in contact with a patient, to reach the particular part of the skin, nail, hair, claw or hoof infected by the fungus. In particular the present compounds have physiochemical properties that facilitate penetration of the nail plate.Type: GrantFiled: February 16, 2006Date of Patent: September 1, 2009Assignee: Anacor Pharmaceuticals, Inc.Inventors: Stephen J. Baker, Tsutomu Akama, Carolyn Bellinger-Kawahara, Vincent S. Hernandez, Karin M. Hold, James J. Leyden, Kirk R. Maples, Jacob J. Plattner, Virginia Sanders, Yong-Kang Zhang
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Publication number: 20080200672Abstract: Novel spiroborate esters derived from non-recemic 1,2-amino alcohols were examined as chiral catalyst in the borane reduction of acetophenone and other aromatic ketones at room temperature. The optically active alcohols were obtained in excellent chemical yields and up to 99% ee with less than 10% catalyst.Type: ApplicationFiled: August 30, 2006Publication date: August 21, 2008Inventors: Margarita Ortiz-Marciales, Viatcheslav Stepanenko, Wildeliz Correa-Ramirez, Melvin de Jesus
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Patent number: 7238826Abstract: The present invention relates to optically active boronate derivatives which are useful as intermediates for the synthesis of HMG-CoA enzyme inhibitors such as atorvastatin, cerivastatin, rosuvastatin, pitavastatin, and fluvastatin.Type: GrantFiled: August 23, 2004Date of Patent: July 3, 2007Assignee: Biocon LimitedInventors: Tom Thomas Puthiaparampil, Sumithra Srinath, Madhavan Sridharan, Sambasivam Ganesh
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Patent number: 7223745Abstract: The present invention provides boronic acid compounds, boronic esters, and compositions thereof that can modulate apoptosis such as by inhibition of proteasome activity. The compounds and compositions can be used in methods of inducing apoptosis and treating diseases such as cancer and other disorders associated directly of indirectly with proteasome activity.Type: GrantFiled: August 12, 2004Date of Patent: May 29, 2007Assignee: Cephalon, Inc.Inventors: Sankar Chatterjee, Mohamed Iqbal, Ernesto Menta, Ambrogio Oliva
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Patent number: 7078554Abstract: Compositions and methods for determining the presence or concentration of glucose in a sample which may also contain an alpha-hydroxy acid or a beta-diketone. The method uses a compound having at least two recognition elements for glucose, oriented such that the interaction between the compound and glucose is more stable than the interaction between the compound and the alpha-hydroxy acid or beta-diketone, such that the presence of the alpha-hydroxy acid or the beta-diketone does not substantially interfere with said determination.Type: GrantFiled: October 4, 2004Date of Patent: July 18, 2006Assignee: Sensors for Medicine and Science, Inc.Inventors: George Y. Daniloff, Aristotle G. Kalivretenos, Alexandre V. Nikolaitchik
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Patent number: 6939985Abstract: The invention provides a process for covalently coupling organic compounds which comprises reacting an aromatic ring compound having a halogen or halogen-like substituent at a coupling position with a diboron derivative in the presence of a Group VIII metal catalyst and a suitable base. The invention also provides useful arylboron intermediates.Type: GrantFiled: March 5, 2003Date of Patent: September 6, 2005Assignee: Commonwealth Scientific and Industrial Research OrganisationInventors: Sebastian Mario Marcuccio, Mary Rodopoulos, Helmut Weigold
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Patent number: 6867306Abstract: The present invention discusses a novel process for the synthesis of [R-(R*,R*)]-2-(4-fluorophenyl)-B,D-dihydroxy-5-(1-methylethyl)-3-phenyl-4-[(phenylamino)carbonyl]-1H-pyrrole-1-heptanoic acid hemi calcium, atorvastatin. The compound so prepared is useful as inhibitor of the HMG-CoA reductase and may thus be used as hypolipidemic and hypocholesterolemic agent.Type: GrantFiled: June 14, 2001Date of Patent: March 15, 2005Assignee: Biocon LimitedInventors: Sumitra Srinath, Joy Mathew, Sandhya Ujire, Madhavan Sridharan, Ganesh Sambasivam
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Patent number: 6680401Abstract: The invention relates to processes for the synthesis of aryl or alkene borates which comprises reacting: (i) an olefinic compound having a halogen or halogen-like substituent in a vinylic substitution position, or (ii) an aromatic ring having a halogen or halogen-like substituent in a ring substitution position, with a disubstituted monohydroborane in the presence of a Group 8-11 metal catalyst. The invention also relates to the use of these borates in coupling reactions. The invention further relates to certain disubstituted monohydroboranes and aryl or alkene borates.Type: GrantFiled: August 13, 2001Date of Patent: January 20, 2004Assignee: Commonwealth Scientific and Industrial Research OrganisationInventors: Sebastian Mario Marcuccio, Mary Rodopoulos, Helmut Weigold
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Publication number: 20030220500Abstract: Novel polydioxaborines are prepared by polymerizing novel monomers that contain a dioxaborine group. Polydioxaborines are readily soluble, excellent film formers, and have semiconducting properties useful in various applications.Type: ApplicationFiled: September 3, 2002Publication date: November 27, 2003Inventors: J. Kevin Cammack, Seth R. Marder, Bernard Kippelen
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Patent number: 6630577Abstract: A reagent having the general formula of General Formula I: wherein group Z comprises a spacer selected from an aliphatic chain up to about 6 carbon equivalents in length, an unbranched aliphatic chain of from about 6 to 18 carbon equivalents in length with at least one of an intermediate amide and a disulfide moiety, and a polyethylene glycol chain of from about 3 to 12 carbon equivalents in length; wherein group R is an electrophilic or nucleophilic moiety suitable for reaction of the reagent with a biologically active species; and wherein group Q is one of nothing at all, an amide, a methyl amide, a methylene, an ether, a thioether, a methyl ether, and a methyl thioether moiety. Also, a conjugate, a bioconjugate and a method of conjugating.Type: GrantFiled: June 4, 2001Date of Patent: October 7, 2003Assignee: Prolinx, Inc.Inventors: Mark L. Stolowitz, Guisheng Li, Jean P. Wiley
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Patent number: 6586615Abstract: The present invention relates to a novel class of &agr;-aminoboronic acids of Formula (V), which are useful as intermediates in synthetic processes for inhibitors of the serine proteases, leukocyte elastase, pancreatic elastase, cathepsin G, and chymotrypsin. More specifically, the &agr;-aminoboronic acids are useful as intermediates for the synthesis of Hepatitis C Virus (HCV) protease inhibitors. This invention also generally relates to novel methods for the preparation of &agr;-aminoboronic acids.Type: GrantFiled: January 9, 2002Date of Patent: July 1, 2003Assignee: Bristol-Myers Squibb CompanyInventors: Charles A. Kettner, Sharada Jagannathan, Timothy Patrick Forsyth
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Patent number: 6559310Abstract: The invention provides a process for covalently coupling organic compounds which comprises reacting an aromatic ring compound having a halogen or halogen-like substituent at a coupling position with a diboron derivative in the presence of a Group VIII metal catalyst and a suitable base. The invention also provides useful arylboron intermediates.Type: GrantFiled: May 21, 2002Date of Patent: May 6, 2003Assignee: Commonwealth Scientific and Industrial Research OrganisationInventors: Sebastian Mario Marcuccio, Mary Rodopoulos, Helmut Weigold
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Publication number: 20020177725Abstract: This invention relates to a novel class of peptides having the Formula (I): 1Type: ApplicationFiled: October 28, 2001Publication date: November 28, 2002Inventor: E. Scott Priestley
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Patent number: 6462179Abstract: Reagents suitable for the modification of a bioactive species for the purpose of incorporating one or more phenyldiboronic acid (PDBA) moieties for subsequent conjugation to a different (or the same) bioactive species having one or more pendant boronic compound complexing moieties of the general formula of General Formula I, wherein group R is a reactive electrophilic or nucleophilic moiety suitable for reaction of the PDBA reagent with a bioactive species. Group Z is a spacer selected from a saturated or unsaturated chain up to about 0 to 6 carbon equivalents in length, an unbranched saturated or unsaturated chain of from about 6 to 18 carbon equivalents in length with at least one intermediate amide or disulfide moiety, and a polyethylene glycol chain of from about 3 to 12 carbon equivalents in length. Group Q is a linkage that includes one of amide, ether and thioether moieties.Type: GrantFiled: July 25, 2000Date of Patent: October 8, 2002Assignee: Prolinx, Inc.Inventors: Mark L. Stolowitz, Edward A. Kesicki, Kevin P. Lund, Karin A. Hughes
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Patent number: 6414122Abstract: Embodiments include reagents to modify a bioactive species for incorporating a bifunctional boronic compound complexing moiety for subsequent conjugation to a different or same bioactive species having pendant phenylboronic acid moieties of General Formula I, wherein group R is an electrophilic or nucleophilic moiety suitable for reaction of the putative bifunctional boronic compound complexing reagent with a bioactive species, wherein group R2 is selected from one of H and OH moieties, and wherein group R3 is selected from one of an alkyl and a methylene bearing an electronegative substituent. Group Z is a spacer selected from (CH2)n and CH2O(CH2CH2O)n2, wherein n is an integer of from 1 to 5, and wherein n2 is an integer of from 1 to 4. Group Z2 and Z3 is a spacer and need not be the same.Type: GrantFiled: August 29, 2000Date of Patent: July 2, 2002Assignee: Prolinx, Inc.Inventors: Clarence N. Ahlem, Robert J. Kaiser, Kevin P. Lund, Mark L. Stolowitz
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Patent number: 6399779Abstract: The invention provides a process for covalently coupling organic compounds which comprises reacting an aromatic ring compound having a halogen substituent or other substituent which undergoes substitution with a diboronic acid ester at a coupling position with a diboron derivative in the presence of a Group VIII metal catalyst and a suitable base.Type: GrantFiled: December 18, 1998Date of Patent: June 4, 2002Assignee: Commonwealth Scientific and Industrial Research OrganisationInventors: Sebastian Mario Marcuccio, Mary Rodopoulos, Helmut Weigold
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Publication number: 20020038004Abstract: A reagent having the general formula of General Formula I: 1Type: ApplicationFiled: June 4, 2001Publication date: March 28, 2002Inventors: Mark L. Stolowitz, Guisheng Li, Jean P. Wiley
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Publication number: 20020032339Abstract: The invention provides a process for covalently coupling organic compounds which comprises reacting an aromatic ring compound having a halogen or halogen-like substituent at a coupling position with a diboron derivative in the presence of a Group VIII metal catalyst and a suitabIe base. The invention also provides useful arylboron intermediates.Type: ApplicationFiled: December 18, 1998Publication date: March 14, 2002Inventors: SEBASTIAN MARIO MARCUCCIO, MARY RODOPOULOS, HELMUT WEINGOLD
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Patent number: 6346639Abstract: This invention relates to a diboron derivative of formula (I) or a diboron derivative of formula (II) or a diboron derivative of formula (III) where R1, R2, R3 and R4 are each independently selected from the group consisting of optionally substituted alkyl, optionally substituted alkenyl, optionally substituted aryl, optionally substituted cycloalkyl, optionally substituted cycloalkenyl, a group of the formula —(R5Q)mR6 where Q is selected from O, S, NR7, optionally substituted arylene and optionally substituted cycloalkylene, m is an integer selected from 1 to 3, the or and each R5 is independently an optionally substituted C1-C3 alkylene, R6 is C1-C3 alkyl or hydrogen, and R7 is hydrogen or C1-C12 alkyl; each X is independently selected from O, S(O)n and NR7, where n is an integer from 0 to 3, R7 is hydrogen or C1-C12 alkyl, or one or more of —NR1R7, —NR2R7, —NR3R7 and —NR4R7 represent an optionally substituted 5 or 6 membered heterocyclyl group,and A, A1 and A2 are divalent grType: GrantFiled: June 22, 2000Date of Patent: February 12, 2002Assignee: The Commonwealth of Australia Commonwealth Scientific and Industrial Research OrganizationInventors: Sebastian Mario Marcuccio, Mary Rodopoulos, Helmut Weigold
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Patent number: 6288259Abstract: This invention describes a process for covalently coupling organic compounds which comprises reacting an olefinic compound having a halogen or halogen-like substituent at a coupling position with a diboron derivative in the presence of a Group VIII metal catalyst and a suitable base. The invention also describes a process for preparing alkene borate intermediates comprising reacting an olefinic compound having a halogen or halogen-like substituent with a diboron derivative in the presence of a Group VIII metal catalyst and a suitable base.Type: GrantFiled: March 6, 2000Date of Patent: September 11, 2001Assignee: Commonwealth Scientific and Industrial Research OrganisationInventors: Sebastian Mario Marcuccio, Mary Rodopoulos, Helmut Weigold
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Patent number: 6204405Abstract: New, economical and convenient procedures for the preparation of catecholborane in high chemically pure form using tri-O-phenylene bis borate readily prepared from the reaction of catechol with boric acid, and diborane or borane-Lewis base complexes.Type: GrantFiled: December 22, 1999Date of Patent: March 20, 2001Assignee: Sigma-Aldrich Co.Inventor: Herbert C. Brown
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Patent number: 6075126Abstract: Boron compound complexing reagents, boron compound complexes, and methods of synthesizing these reagents and complexes are disclosed. These reagents and complexes include those shown in General Formula CIII, General Formula CIV, and General Formula CVI. In one embodiment, the reagents of General Formula CIII may be used to produce, after condensation with a bioactive species (BAS), the reagent of General Formula CIV. The reagent of General Formula CIV may be used to form a complex with a boron compound, such as a complex shown in General Formula CVI.Type: GrantFiled: August 21, 1998Date of Patent: June 13, 2000Assignee: Prolinx, Inc.Inventors: Mark L. Stolowitz, Edward A. Kesicki, Kevin P. Lund, Karin A. Hughes
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Patent number: 6060462Abstract: This invention relates to electrophilic dipeptide analogs conjugated to an N,N-disubstituted .alpha.-amino acid as inhibitors of trypsin-like serine protease enzymes.Type: GrantFiled: August 1, 1997Date of Patent: May 9, 2000Assignee: DuPont Pharmaceuticals CompanyInventors: Robert Anthony Galemmo, Jr., Matthew Mark Abelman, Eugene Cruz Amparo, John Matthew Fevig, Robert Madara Knabb, William Henry Miller, Gregory James Pacofsky, Patricia Carol Weber, Joseph Cacciola
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Patent number: 6031117Abstract: The present invention provides arylboronic acid reagents useful for incorporation into modified oligonucleotides and polynucleotides. The modified oligonucleotides and polynucleotides thus produced are useful in bioconjugation reactions for the immobilization and purification of macromolecules.Type: GrantFiled: March 19, 1999Date of Patent: February 29, 2000Assignee: Prolinx IncorporatedInventors: Robert J. Kaiser, Mark L. Stolowitz
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Patent number: 5973185Abstract: A novel process for making compounds of Formula I, ##STR1## wherein X is a leaving group selected from the group Br, Cl, TsO, MsO, and TfO and R is a 1,2-diol, from a compound of Formula II: ##STR2## is described.Type: GrantFiled: July 7, 1997Date of Patent: October 26, 1999Assignee: DuPont Pharmaceuticals CompanyInventors: Philip Ma, Biao Jiang
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Patent number: 5880188Abstract: A method for the protection of a medium by susceptible to microbial attack by the treatment of the medium with an oxaborale or a salt of an oxaborale.Type: GrantFiled: December 9, 1996Date of Patent: March 9, 1999Assignee: Zeneca LimitedInventors: Peter William Austin, Christopher Juan Kneale, Patrick Jelf Crowley, John Martin Clough
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Patent number: 5872224Abstract: Boron compound complexing reagents, boron compound complexes, and methods of synthesizing these reagents and complexes are disclosed. These reagents and complexes include those shown in General Formula CIV, and General Formula CVI. In one embodiment, the reagent of General Formula CIV may be used to form a complex with a boron compound, such as a complex shown in General Formula CVI. ##STR1## In one embodiment, group Z comprises a spacer selected from a saturated or unsaturated chain of up to about 6 carbon equivalents in length, an unbranched saturated or unsaturated chain of from about 6 to 18 carbon equivalents in length with at least one of intermediate amide and disulfide moieties, and a polyethylene glycol chain of from about 3 to 12 carbon equivalents in length; group R.sub.3 is selected from one of an H, an alkyl, and a methylene or ethylene moiety with an electronegative substituent; and BAS and BAS* are biologically active species.Type: GrantFiled: October 22, 1997Date of Patent: February 16, 1999Assignee: Prolinx, Inc.Inventors: Mark L. Stolowitz, Robert J. Kaiser, Kevin P. Lund
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Patent number: 5859210Abstract: Boron compound complexing reagents, boron compound complexes, and methods of synthesizing these reagents and complexes are disclosed. These reagents and complexes include those shown in General Formula IV and General Formula VI. In one embodiment, the reagent of General Formula IV may be used to form a complex with a boron compound, such as a complex shown in General Formula VI. ##STR1## In one embodiment, group Z comprises a spacer selected from a saturated or unsaturated chain of up to about 6 carbon equivalents in length, an unbranched saturated or unsaturated chain of from about 6 to 18 carbon equivalents in length with at least one of intermediate amide or disulfide moieties, and a polyethylene glycol chain of from about 3 to 12 carbon equivalents in length; group R.sub.3 is selected from one of an H, an alkyl, and a methylene or ethylene moiety with an electronegative substituent; and BAS and BAS* are biologically active species.Type: GrantFiled: October 22, 1997Date of Patent: January 12, 1999Assignees: Prolinx, Inc., SystemixInventors: Mark L. Stowolitz, Robert J. Kaiser, Kevin P. Lund, Steven M. Torkelson
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Patent number: 5705704Abstract: Novel tricyclic compounds of formula I as defined in the specification, a process for their preparation and their use for the preparation of optically active or racemic colchicine and thiocolchicine derivatives.Type: GrantFiled: March 1, 1996Date of Patent: January 6, 1998Assignee: Roussel UclafInventors: Francis Brion, Bernadette Chappert, Christian Diolez, Christian Marie, Alain Mazurie, Michel Middendorp, Didier Pronine, Edmond Toromanoff
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Patent number: 5698538Abstract: Novel boronic acid and ester and carboxyl-modified amino acid compounds of the Formula I, which are inhibitors of trypsin-like enzymes, are disclosed :R.sup.1 --Z--CHR.sup.2 --A,where R.sup.1, Z, R.sup.2 arid A are defined within.Type: GrantFiled: July 26, 1996Date of Patent: December 16, 1997Assignee: The DuPont Merck Pharmaceutical CompanyInventors: Eugene Cruz Amparo, William Henry Miller, Gregory James Pacofsky, John Wityak, Patricia Carol Weber, John Jonas Vytautas Duncia, Joseph Basil Santella, III
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Patent number: 5688928Abstract: The present invention relates to a novel class of phenylboronic acid complexing reagents useful for the preparation of bioconjugates, and the method of making and using such reagents. In the present invention, in the place of prior art Avidin-Biotin and Digoxigenin-anti-Digoxigenin systems, phenylboronic acid complexing reagents are utilized in conjunction with phenylboronic acid reagents (many of which are known in the prior art) to facilitate chemical conjugation without the use of intermediary biological macromolecules. Reagents suitable for the modification of bioactive species for the purpose of incorporating a phenylboronic acid complexing moiety for subsequent conjugation to a different bioactive species having pendant phenylboronic acid moieties are of General Formula I or General Formula II. ##STR1## wherein group X is selected from either H, OH, NH.sub.2, NHCH.sub.3, NHOH and NHOCH.sub.Type: GrantFiled: June 7, 1995Date of Patent: November 18, 1997Assignee: Prolinx, Inc.Inventor: Mark L. Stolowitz
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Patent number: 5681978Abstract: A method of synthesis of (2S,3R,1'R)-stegobinone(I) using borane intermediates and methods for the use of stegobinone (I) for attracting beetles of the Anobium species.Type: GrantFiled: August 2, 1995Date of Patent: October 28, 1997Assignee: Washington State University Research FoundationInventors: Donald S. Matteson, Hon-Wah Man, Oliver Ho
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Patent number: 5677431Abstract: The present invention relates to a novel class of phenylboronic acid bioconjugate complexes derived from aminosalicylic acid, and the method of making and using such bioconjugate complexes. The bioconjugate complexes are in the form of the following general formulas; ##STR1## wherein group X is selected from the group consisting of O, NH, N-alkyl, NC.sub.6 H.sub.5, N-aryl, NCH.sub.2 -aryl, NCH.sub.2 CH.sub.2 OH, NCOCH.sub.2 CH.sub.2 OH, NOH, NO-alkyl and NOCH.sub.2 -aryl, wherein alkyl denotes a hydrocarbon moiety of from 1 to 4 carbons in length and which may be linear or branched, wherein aryl is selected from the group consisting of an aromatic ring, a substituted aromatic ring and a fused aromatic ring,wherein group Y is selected from the group consisting of O, S, NH, N-alkyl, N-aryl and NCH.sub.Type: GrantFiled: June 7, 1995Date of Patent: October 14, 1997Assignee: Prolinx, Inc.Inventor: Mark L. Stolowitz
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Patent number: 5668258Abstract: The present invention relates to a novel class of phenylboronic acid complexing reagents useful for the preparation of bioconjugates, and the method of making and using such reagents. In the present invention, in the place of prior art Avidin-Biotin and Digoxigenin-anti-Digoxigenin systems, phenylboronic acid complexing reagents are utilized in conjunction with phenylboronic acid reagents (many of which are known in the prior art) to facilitate chemical conjugation without the use of intermediary biological macromolecules. Reagents suitable for the modification of a bioactive species for the purpose of incorporating a phenylboronic acid complexing moiety for subsequent conjugation to a different bioactive species having pendant phenylboronic acid moieties are of General Formula I or General Formula II. ##STR1## wherein group X is selected from either H, OH, NH.sub.2, NHCH.sub.3, NHOH and NHOCH.sub.Type: GrantFiled: June 7, 1995Date of Patent: September 16, 1997Assignee: Prolinx, Inc.Inventor: Mark L. Stolowitz
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Patent number: 5648470Abstract: The present invention relates to a novel class of phenylboronic acid complexing reagents useful for the preparation of bioconjugates, and the method of making and using such reagents. In the present invention, in the place of prior art Avidin-Biotin and Digoxigenin-anti-Digoxigenin systems, phenylboronic acid complexing reagents are utilized in conjunction with phenylboronic acid reagents (many of which are known in the prior art) to facilitate chemical conjugation without the use of intermediary biological macromolecules. Reagents suitable for the modification of a bioactive species for the purpose of incorporating a phenylboronic acid complexing moiety for subsequent conjugation to a different bioactive species having pendant phenylboronic acid moieties are of General Formula I or General Formula II. ##STR1## wherein group X is selected from either H, OH, NH.sub.2, NHCH.sub.3, NHOH and NHOCH.sub.Type: GrantFiled: June 7, 1995Date of Patent: July 15, 1997Assignee: Prolinx, Inc.Inventor: Mark L. Stolowitz
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Patent number: 5623055Abstract: The present invention relates to a novel class of bioconjugates derived from phenylboronic acid complexes, and the method of making and using such bioconjugate complexes. The complexes are in the form of the following general formulas. ##STR1## wherein group Q is selected from either O, S, NH, N-alkyl and N-aryl, wherein alkyl denotes a hydrocarbon moiety, wherein aryl is selected from either an aromatic ring, a substituted aromatic ring and fused aromatic rings, wherein group R is preferably selected from either O, NH, CH.sub.2, alkyl and aryl, wherein alkyl and aryl are as were previously defined,wherein group X is selected from either H, CH.sub.3 and C.sub.6 H.sub.5, wherein group Y is selected from either O, NH, CH.sub.Type: GrantFiled: January 28, 1994Date of Patent: April 22, 1997Assignee: Prolinx, Inc.Inventor: Mark L. Stolowitz
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Patent number: 5621133Abstract: Novel compounds having the formula ##STR1## and the pharmaceutically acceptable salts, esters and amides thereof, whereinA is --O--, --S-- or --CR.sup.2 R.sup.8 --;R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6, R.sup.7, R.sup.8, R.sup.9, R.sup.10, X and Y are specifically defined; andup to one combination of (a) R.sup.2 and R.sup.5, (b) R.sup.5 and R.sup.6, (c) R.sup.5 and R.sup.7, (d) R.sup.6 and R.sup.7, and (e) R.sup.7 and Y, taken together with the atoms to which they are attached, may form a ring, the compounds being useful for treating dopamine-related neurological, psychological and cardiovascular disorders as well as in the treatment of cognitive impairment, attention deficit disorder, and substance abuse and other addictive behavior disorders.Also disclosed are intermediates and processes useful in the preparation of the above compounds.Type: GrantFiled: June 5, 1995Date of Patent: April 15, 1997Inventors: Michael P. DeNinno, Richard J. Perner
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Patent number: 5596123Abstract: Stable .alpha.-substituted boronic esters, e.g. for use in peptide synthesis, are prepared by reacting a substituted alkene of the formula: ##STR1## with a disubstituted borane of the formula: ##STR2## wherein: (i) R.sup.1 and R.sup.2 are each selected from various groups which are preferably not leaving groups;(ii) X is halogen or other leaving group;(iii) Y is H or lower alkyl;(iv) Q.sup.1 and Q.sup.2 are each selected from various groups which are preferably such that the borane is non-hydrolyzable, and particularly Q.sup.1 and Q.sup.2 together may represent a residue of a diol such as catechol or pinanediol.Type: GrantFiled: June 2, 1995Date of Patent: January 21, 1997Assignee: Thrombosis Research InstituteInventors: Said M. A. Elgendy, John J. Deadman, Geeta Patel, Donovan S. Green, Jehan A. Baban, Vijay V. Kakkar, Goran K. Claeson
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Patent number: 5594111Abstract: The present invention relates to a novel class of phenylboronic acid bioconjugate complexes derived from aminosalicylic acid, and the method of making and using such bioconjugate complexes. The bioconjugate complexes are in the form of the following general formulas; ##STR1## wherein group X is selected from the group consisting of O, NH, N-alkyl, NC.sub.6 H.sub.5, N-aryl, NCH.sub.2 -aryl, NCH.sub.2 CH.sub.2 OH, NCOCH.sub.2 CH.sub.2 OH, NOH, NO-alkyl and NOCH.sub.2 -aryl, wherein alkyl denotes a hydrocarbon moiety of from 1 to 4 carbons in length and which may be linear or branched, wherein aryl is selected from the group consisting of an aromatic ring, a substituted aromatic ring and a fused aromatic ring,wherein group Y is selected from the group consisting of O, S, NH, N-alkyl, N-aryl and NCH.sub.Type: GrantFiled: January 28, 1994Date of Patent: January 14, 1997Assignee: Prolinx, Inc.Inventor: Mark L. Stolowitz
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Patent number: 5591884Abstract: Novel compounds having the formula ##STR1## and the pharmaceutically acceptable salts, esters and amides thereof, whereinA is --O--, --S-- or --CR.sup.2 R.sup.8 --;R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6, R.sup.7, R.sup.8, R.sup.9, R.sup.10, X and Y are specifically defined; andup to one combination of (a) R.sup.2 and R.sup.5, (b) R.sup.5 and R.sup.6, (c) R.sup.5 and R.sup.7, (d) R.sup.6 and R.sup.7, and (e) R.sup.7 and Y, taken together with the atoms to which they are attached, may form a ring, the compounds being useful for treating dopamine-related neurological, psychological and cardiovascular disorders as well as in the treatment of cognitive impairment, attention deficit disorder, and substance abuse and other addictive behavior disorders.Also disclosed are intermediates and processes useful in the preparation of the above compounds.Type: GrantFiled: June 5, 1995Date of Patent: January 7, 1997Assignee: Abbott LaboratoriesInventors: Michael P. DeNinno, Richard J. Perner
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Patent number: 5543526Abstract: A compound of formula (I) ##STR1## in which R.sub.3 and R.sub.4 together represent the residue of a dihydroxy compound, andR.sub.5 represents a hydrogen atom or a (C.sub.1 -C.sub.4) alkyl group, or a salt thereof, and its use as a synthetic intermediate.Type: GrantFiled: April 11, 1995Date of Patent: August 6, 1996Assignee: SynthelaboInventors: Sergio Mallart, Gilbert Lassalle, Thomas Andrew Purcell, Jean Claude Muller
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Patent number: 5384410Abstract: A method for the removal of ester protecting groups from .alpha.-amino boronic acid is disclosed for the preparation of compounds of formula (II) belowR.sup.1 -X.sub.n -NHCH (R.sup.2)-B(OH).sub.Type: GrantFiled: March 24, 1993Date of Patent: January 24, 1995Assignee: The Du Pont Merck Pharmaceutical CompanyInventor: Charles A. Kettner
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Patent number: 5382672Abstract: Derivatives of benzeneborinic acid, preparation thereof and use thereof as synthetic intermediates.Type: GrantFiled: November 19, 1993Date of Patent: January 17, 1995Assignee: SynthelaboInventors: Isaac Chekroun, Jose Ruiz-Montes, Manuel Bedoya-Zurita, Guy Rossey
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Patent number: 5262556Abstract: The invention relates to a process for the reaction of fluorinated or chlorinated aromatics with electrophiles at the ortho position relative to the fluorine or chlorine atom, characterized in that a strong base is added to a mixture of the fluorinated or chlorinated aromatic and the electrophile.Type: GrantFiled: May 6, 1992Date of Patent: November 16, 1993Assignee: Merck Patent Gesellschaft mit beschrankter HaftungInventors: Bernard Riefling, Jurgen Seubert, Volker Reiffenrath, Reinhard Hittich
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Patent number: 5250720Abstract: Intermediates for the preparation of Peptides comprising C-terminal boronic acid derivatives of lysine, ornithine, and arginine, homoarginine and corresponding isothiouronium analogs thereof, are reversible inhibitors of trypsin-like serine proteases such as thrombin, plasma kallikrein and plasmin.Type: GrantFiled: March 9, 1992Date of Patent: October 5, 1993Assignee: The Dupont Merck Pharmaceutical CompanyInventors: Charles A. Kettner, Ashokkumar B. Shenvi
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Patent number: 5221758Abstract: A method of preparing a compound or formulation having biocidal or preservative properties, or both comprises reacting an organic complexing agent, preferably a selected organic alcohol, with a borate or boric acid to produce a borate organic complex ion. The complex ion is preferably further reacted with a suitable cationic species. A compound or formulation so prepared is also claimed.Type: GrantFiled: September 28, 1989Date of Patent: June 22, 1993Inventor: Nigel P. Maynard
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Patent number: 5169841Abstract: The invention relates to compounds of the formula 1 ##STR1## in which A.sup.1 denotes a radical of the formulae ##STR2## A.sup.2 is absent or represents a radical of the formula ##STR3## R.sup.2, R.sup.3 and R.sup.4 are as defined in the specification, and X and Y, independently of one another, represent --O-- or --NR.sup.13 --, and to the salts thereof. Also described is a process for the preparation of the compounds of the formula 1, corresponding pharmaceutical products, and the use thereof as medicines, and intermediates for the preparation of these compounds.Type: GrantFiled: November 3, 1988Date of Patent: December 8, 1992Assignee: Hoechst AktiengesellschaftInventors: Heinz-Werner Kleeman, Hansjorg Urbach, Dieter Ruppert, Bernward Scholkens
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Patent number: 5105003Abstract: A process for the separation of a compound comprising a 1,2-dihydroxycyclohexa-3,5-diene ring from a medium containing it in which the compound reacts with a phenylboronate ion to form a phenylboronate ester which is insoluble in the medium. Novel phenylboronate esters formed during the separation process are also claimed.Type: GrantFiled: January 16, 1990Date of Patent: April 14, 1992Assignee: Imperial Chemical Industries PLCInventors: Andrew B. Herbert, Gary N. Sheldrake, Peter J. Somers, John A. Meredith
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Patent number: RE37133Abstract: A method of preparing a compound or formulation having biocidal or preservative properties, or both comprises reacting an organic complexing agent, preferably a selected organic alcohol, with a borate or boric acid to produce a borate organic complex ion. The complex ion is preferably further reacted with a suitable cationic species. A compound or formulation so prepared is also claimed.Type: GrantFiled: August 18, 1997Date of Patent: April 10, 2001Assignee: Fernz Timber Protection LimitedInventor: Nigel P. Maynard