Benzene Ring Bonded Directly To Guanidine Nitrogen Patents (Class 564/238)
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Patent number: 10759747Abstract: The present invention relates to a method of radiochemical synthesis. Novel methods useful in the synthesis of a positron emission tomography (PET) tracer, and novel intermediates useful in said method are provided that have advantages over known methods.Type: GrantFiled: May 2, 2017Date of Patent: September 1, 2020Assignees: GE HEALTHCARE LIMITED, KINGS COLLEGE LONDONInventors: Imtiaz Khan, Graeme McRobbie, Anna Kirjavainen
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Patent number: 9085518Abstract: The present invention provides a method for the synthesis of 18F-labelled biomolecules, which is amenable to automation. The present invention also provides a cassette for automating the method of the invention. The method of the present invention provides numerous advantages over the prior art methods. One less purification step is required as compared with known methods. Also, in a preferred embodiment, one less reagent is required as a particular reagent is employed in two different steps. The chemistry process is thereby simplified, the cost of goods is reduced and the burden of validation and documentation of reagents required for GMP clinical production is minimized.Type: GrantFiled: October 15, 2012Date of Patent: July 21, 2015Assignee: GE Healthcare LimitedInventors: Robert James Domett Nairne, Rajiv Bhalla, Imtiaz Khan, Jane Brown, Anthony Wilson, Andres Black
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Publication number: 20150051291Abstract: A composition and method of treating stroke by administration of a novel sigma agonist is presented. Twenty-four hours after MCAO, systemic administration of several novel sigma agonists including: Bromo-DTG; Chloro-DTG; N,N?-di-1-Naphthylguanidine hydrochloride (NAGH); N,N?-di-p-Nitrophenylguanidine HCL (NAD) or vehicle were injected subcutaneously daily for 3 days. Rats treated with Bromo-DTG and Chloro-DTG had no significant improvements in any of the motor or cognitive tests while NAGH treated rats showed improved vertical movement and had significantly less motor asymmetry and bias than vehicle treated rats. Sigma receptor agonist NAGH also was found to exert its long-term neuroprotective effects by preserving both gray matter and white matter tracts.Type: ApplicationFiled: November 3, 2014Publication date: February 19, 2015Applicant: UNIVERSITY OF SOUTH FLORIDAInventors: Keith R. Pennypacker, Alison Willing, Javier Cuevas, Jon C. Antilla, Michelle Cortes-Salva
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Publication number: 20140243555Abstract: The present invention provides a method for the synthesis of 18F-labelled biomolecules, which is amenable to automation. The present invention also provides a cassette for automating the method of the invention. The method of the present invention provides numerous advantages over the prior art methods. One less purification step is required as compared with known methods. Also, in a preferred embodiment, one less reagent is required as a particular reagent is employed in two different steps. The chemistry process is thereby simplified, the cost of goods is reduced and the burden of validation and documentation of reagents required for GMP clinical production is minimised.Type: ApplicationFiled: October 15, 2012Publication date: August 28, 2014Applicant: GE HEALTHCARE LIMITEDInventors: Robert James Domett Nairne, Rajiv Bhalla, Imtiaz Khan, Jane Brown, Anthony Wilson, Andres Black
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Publication number: 20140235861Abstract: The present invention provides a method for the synthesis of 18F-labelled biomolecules, which is amenable to automation. The present invention also provides a cassette for automating the method of the invention. The method of the present invention provides numerous advantages over the prior art methods. One less purification step is required as compared with known methods. Also, one less reagent is required as a particular reagent is employed in two different steps. The chemistry process is thereby simplified, the cost of goods is reduced and the burden of validation and documentation of reagents required for GMP clinical production is minimised.Type: ApplicationFiled: October 15, 2012Publication date: August 21, 2014Applicant: GE HEALTHCARE LIMITEDInventors: RAJIV Bhalla, Anthony Wilson, Imtiaz Khan, Janne Brown
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Publication number: 20140228388Abstract: Provided herein are phenyl-guanidine derivatives for the inhibition of Rac1 which blocks its interaction with guanosine exchange factors (GEFs) belonging to the DBL family as agents for the treatment of aggressive and/or resistant tumours, as well as pharmaceutical compositions comprising them, their use in therapy and processes for their preparation.Type: ApplicationFiled: October 10, 2012Publication date: August 14, 2014Applicants: Universidad Nacional de Quilmes, Chemo Research, S.L.Inventors: Pablo Lorenzano Menna, Julieta Comín, Daniel Eduardo Gómez, Daniel Fernando Alonso
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Publication number: 20140154182Abstract: The invention is directed to a N,N-substituted guanidine compound or a salt or solvate thereof according to formula (1), R1RNC(NH)NR2R3, wherein R1 is methyl and R2 is hydrogen. R3 is a organic group comprising a halogen and thiomethyl substituted phenyl group. R is an organic group comprising a substituted aryl group Z wherein the substituent group is —Y—R4, wherein Y is a heteroatom chosen from the group consisting of O, S and N and R4 is a fluorinated organic group.Type: ApplicationFiled: May 30, 2012Publication date: June 5, 2014Applicant: STICHTING VU-VUMCInventors: Pieter Jacob Klein, Athansios Metaxas, Albert Dirk Windhorst, Johannes Antonius Maria Christiaans, Bart Nicolaas Maria van Berckel
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Patent number: 8633337Abstract: The present invention provides a method for the preparation of a radiolabeled guanidine derivative, in particular wherein the radiolabeled guanidine derivative is a positron emission tomography (PET) tracer. Certain intermediates useful in said method are also provided, as well as means for carrying out said method in an automated fashion. The method of the invention provides advantages over known methods for the preparation of radiolabeled guanidine derivatives.Type: GrantFiled: May 13, 2011Date of Patent: January 21, 2014Assignee: GE Healthcare LimitedInventors: Anders Brathe, Andreas Olsson, Mikkel Thaning, Steffen Bugge
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Catalytic depolymerization of polymers containing electrophilic linkages using nucleophilic reagents
Patent number: 8492504Abstract: The disclosure relates to methods and materials useful for depolymerizing a polymer. In one embodiment, for example, the disclosure provides a method for depolymerizing a polymer containing electrophilic linkages, wherein the method comprises contacting the polymer with a nucleophilic reagent in the presence of a guanidine-containing compound. The methods and materials of the disclosure find utility, for example, in the field of waste reclamation and recycling.Type: GrantFiled: August 7, 2012Date of Patent: July 23, 2013Assignees: International Business Machines Corporation, The Board of Trustees of the Leland Stanford Junior UniversityInventors: James Lupton Hedrick, Russell Clayton Pratt, Robert M. Waymouth -
Publication number: 20130060064Abstract: The present invention provides a method for the preparation of a radiolabeled guanidine derivative, in particular wherein the radiolabeled guanidine derivative is a positron emission tomography (PET) tracer. Certain intermediates useful in said method are also provided, as well as means for carrying out said method in an automated fashion. The method of the invention provides advantages over known methods for the preparation of radiolabeled guanidine derivatives.Type: ApplicationFiled: May 13, 2011Publication date: March 7, 2013Applicant: GE HEALTHCARE LIMITEDInventors: Anders Brathe, Andreas Olsson, Mikkel Thaning, Steffen Bugge
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Publication number: 20130046092Abstract: A solvent that reversibly converts from a nonionic liquid mixture to an ionic liquid upon contact with a selected trigger, e.g., contact with CO2, is described. In preferred embodiments, the ionic solvent is readily converted back to the nonionic liquid mixture. The nonionic liquid mixture includes an amidine or guanidine or both, and water, alcohol, or a combination thereof. Single component amine solvents that reversibly convert between ionic and non-ionic states are also described. Some embodiments require increased pressure to convert; others convert at 1 atmosphere.Type: ApplicationFiled: June 29, 2011Publication date: February 21, 2013Applicants: QUEEN'S UNIVERSITY AT KINGSTON, GEORGIA TECH RESEARCH CORPORATIONInventors: Philip JESSOP, Charles ECKERT, Charles LIOTTA, David HELDEBRANT
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Publication number: 20120136062Abstract: Disclosed are complexes of an antipneumocystic compound and an antimalarial compound, processes for their preparation, pharmaceutical compositions and methods of using said complexes or compositions for the treatment and/or prophylaxis of parasitic infections.Type: ApplicationFiled: August 20, 2010Publication date: May 31, 2012Applicant: IPCA Laboratories Ltd.Inventors: Ashok Kumar, Dharmendra Singh, Pramilkumar Mathur, Vitthal Syryabhan Buchude
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Publication number: 20120116076Abstract: A solvent that reversibly converts from a nonionic liquid mixture to an ionic liquid upon contact with a selected trigger, e.g., contact with CO2, is described. In preferred embodiments, the ionic solvent is readily converted back to the nonionic liquid mixture. The nonionic liquid mixture includes an amidine or guanidine or both, and water, alcohol, or a combination thereof. Single component amine solvents that reversibly convert between ionic and non-ionic states are also described. Some embodiments require increased pressure to convert; others convert at 1 atmosphere.Type: ApplicationFiled: June 29, 2011Publication date: May 10, 2012Applicants: GEORGIA TECH RESEARCH CORPORATION, QUEEN'S UNIVERSITY AT KINGSTONInventors: Philip G. JESSOP, Charles A. ECKERT, Charles L. LIOTTA, David J. HELDEBRANT
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Patent number: 8058311Abstract: The invention provides a compound of formula (I); or a salt or solvate thereof, wherein: R1 is hydrogen or C1-4 alkyl; R2 and R4 are each independently selected from C1-4 alkyl, [11C]C1-4 alkyl, and [18F]—C1-4 fluoroalkyl provided that at least one of R2 and R4 is [11C]C1-4 alkyl or [18F]—C1-4 fluoroalkyl; and R3 is halo. Such compounds having use for imaging central nervous system receptors.Type: GrantFiled: June 23, 2006Date of Patent: November 15, 2011Assignee: Hammersmith Imanet LimitedInventors: Edward George Robins, Erik Arstad
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Publication number: 20110201688Abstract: 1,3 di-o-tolylguanidine (DTG) was examined as anti-stroke drug with a broad therapeutic window. DTG activates sigma 1 and 2 receptors. Administration of DTG at 24 hours post-stroke to rats reduces neurodegeneration by 85%; this is the only pharmacological agent that has been used successfully at this delayed timepoint. Treatment with DTG provides protection of neurons exposed to hypoxia and blocks activation of immune cells that are responsible for delayed neurodegeneration associated with stroke. Disclosed is an altered DTG structure, placing a bromide at the para position to increase tissue penetrance and efficacy. Results show that N,N?-di-p-bromophenyl guanidine protects cultured neurons under hypoxic conditions but is more potent than DTG. Moreover, N,N?-di-p-bromophenyl guanidine is as least as efficacious as DTG in treating rats 24 hours after experimental stroke.Type: ApplicationFiled: April 20, 2011Publication date: August 18, 2011Applicant: UNIVERSITY OF SOUTH FLORIDAInventors: Keith Pennypacker, Javier Cuevas, Jon Antilla, Michelle Cortes-Salva
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Patent number: 7982069Abstract: A solvent that reversibly converts from a nonionic liquid mixture to an ionic liquid upon contact with a selected trigger, e.g., contact with CO2, is described. In preferred embodiments, the ionic solvent is readily converted back to the nonionic liquid mixture. The nonionic liquid mixture includes an amidine or guanidine or both, and water, alcohol, or a combination thereof. Single component amine solvents that reversibly convert between ionic and non-ionic states are also described. Some embodiments require increased pressure to convert; others convert at 1 atmosphere.Type: GrantFiled: March 13, 2007Date of Patent: July 19, 2011Assignees: Queen's University at Kingston, Georgia Tech Research CorporationInventors: Philip G. Jessop, Charles A. Eckert, Charles L. Liotta, David J. Heldebrant
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Patent number: 7960459Abstract: The present invention has its object to provide a curable composition which comprises a reactive silyl group-containing organic polymer, does not contain, as a silanol condensation catalyst, any organotin type curing catalyst currently of concern because of the toxic feature thereof, is excellent in surface curability and depth curability and, further, can provide cured products excellent in adhesiveness; the above object can be achieved by a curable composition which comprises: an organic polymer (A) containing a silicon-containing group capable of crosslinking under siloxane bond formation; and a guanidine compound (B-1), as a silanol condensation catalyst (B), represented by the general formula (1): R1N?C(NR12)2??(1) (wherein one of the five R1s is an aryl group and the other four R1s each independently is a hydrogen atom or a hydrocarbon group in which the carbon atom at position 1 is saturated).Type: GrantFiled: February 9, 2007Date of Patent: June 14, 2011Assignee: Kaneka CorporationInventors: Noriko Noro, Toshihiko Okamoto, Ayako Yano, Yoshikazu Morii
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Patent number: 7884244Abstract: Disclosed herein is compound having a formula as described herein. Therapeutic methods, compositions, and medicaments related thereto are also disclosed.Type: GrantFiled: March 28, 2008Date of Patent: February 8, 2011Assignee: Allergan, Inc.Inventors: Ken Chow, Wenkui K. Fang, Evelyn G. Corpuz, Daniel W. Gil, Michael E. Garst
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Publication number: 20100331384Abstract: The adrenergic receptors or adrenoceptors are a family of G-protein coupled receptors split into ? and ? subclasses. The adrenoceptors have important roles in regulating a myriad of physiological conditions and their malfunction has been implicated in the pathophysiology of a number of diseases. Disclosed herein are a series of novel guanidine and 2-aminoimidazoline compounds which are ligands of the alpha2-adrenoceptor (?2-ARs) subclass of adrenergic receptors. The invention also provides for pharmaceutical compositions comprising the novel compounds. The compounds are suitable for use in the manufacture of medicaments for the treatment of ?2-ARs associated disorders, such as depression, schizophrenia, glaucoma and analgesia.Type: ApplicationFiled: December 22, 2008Publication date: December 30, 2010Applicants: UNIVERSIDAD DEL PAIS VASCO/EUSKAL HERRIKO UNIBERTSITATEA, UNIDIVIDED TRINITY OF QUEEN ELIZABETHInventors: Maria Isabel Rozas Hernando, Fernando Rodriguez Royo, Javier Meana, Luis Callado
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Patent number: 7825279Abstract: Novel fused ring dicationic anti-protozoan compounds. Representative protozoan species include but are not limited to Trypanosoma brucei rhodesiense (T.b.r.) and Plasmodium falciparum. Prodrugs of these compounds can be used as an oral treatment for malaria and human African trypanosomiasis.Type: GrantFiled: November 18, 2004Date of Patent: November 2, 2010Assignees: The University of North Carolina at Chapel Hill, Georgia State University Research Foundation, Inc.Inventors: David W. Boykin, Richard R. Tidwell, W. David Wilson, Reto Brun, Reem K. Arafa, Chad E. Stephens
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Publication number: 20100143252Abstract: The invention provides a compound of formula (I); or a salt or solvate thereof, wherein: R1 is hydrogen or C1-4alkyl; R2 and R4 are each independently selected from C1-4 alkyl, [11C] C1-4alkyl, and [18F]—C1-4 fluoroalkyl provided that at least one of R2 and R4 is [11C] C1-4alkyl or [18F]—C1-4 fluoroalkyl; and R3 is halo. Such compounds having use for imaging central nervous system receptors.Type: ApplicationFiled: June 23, 2006Publication date: June 10, 2010Inventors: Edward George Robins, Erik Arstad
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Patent number: 7582656Abstract: Compounds of the formula (I): in which the radicals R and R1 to R10 are as defined in the description, processes for the preparation of them, use thereof for the treatment of cardiovascular diseases, and pharmaceutical compositions comprising them.Type: GrantFiled: June 28, 2005Date of Patent: September 1, 2009Assignee: Merck Patent GesellschaftInventors: Didier Roche, Bruno Roux, Isabelle Berard
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Publication number: 20080249121Abstract: This invention relates to a process for the preparation of (3-trifluoromethylsulfonyl)-N-[4-methyl-3-(4-pyridin-3yl-pyrimidin-2ylamino)-phenyl]-benzamide (formula (I)) starting from 4-methyl-2-nitro-aniline (formula (II)) through intermediates (3-trifluoromethylsulfonyl)-N-[4-methyl-3-nitrophenyl]-benzamide (formula (III)), (3-trifluoromethylsulfonyl)-N-[3-amino-4-methylphenyl]-benzamide (formula (IV)) and (3-trifluoromethylsulfonyl)-N-[3-guanidino-4-methylphenyl]-benzamide (formula (V)). This invention also relates to processes for the preparation of these intermediates.Type: ApplicationFiled: March 4, 2008Publication date: October 9, 2008Applicant: Natco Pharma LimitedInventors: Amala Kishan Kompella, Bhujanga rao Adibhatla Kali Satya, Sreenivas Rachakonda, Nannapaneni Venkaiah Chowdary
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Patent number: 7432397Abstract: The invention relates to compounds of formula: (I) or a salt or solvate thereof, wherein: R1 is —11CH2R5 or [18F]—C1-4 fluoroalkyl wherein R5 is hydrogen or C1-4 alkyl; R2 is hydrogen or C1-4 alkyl; R3 is halo; and R4 is halo, C1-4 alkylthio, or C1-4 alkyl; and their use for imaging central nervous system (CNS) receptors.Type: GrantFiled: July 16, 2003Date of Patent: October 7, 2008Assignee: Hammersmith Imanet Ltd.Inventors: Frank Brady, Sajinder Kaur Luthra
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Patent number: 7351743Abstract: The present invention provides therapeutically useful substituted guanidines, and methods of treatment and pharmaceutical compositions that utilize or comprise one or more of such guanidines.Type: GrantFiled: August 11, 2000Date of Patent: April 1, 2008Assignee: WyethInventors: Stanley M. Goldin, James B. Fischer, Andrew Gannett Knapp, N. Laxma Reddy, David Berlove, Graham J. Durant, Subbarao Katragadda, Lain-Yen Hu, Sharad Magar, Wenhong Fan, Elizabeth Yost, Juo Qing Guo
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Patent number: 7078566Abstract: This invention relates to salts of guanidine derivatives of formula R—X—C(?NH)NH3+Z?, wherein X represents a valence bond, —CH2—NH—, —CH2—NH—NH— or —CH?N—NH—; R represents a linear or branched C1–C30 alkyl, C3–C20 cycloalkyl, adamantyl, norbornyl, tricyclodecyl, benzyl, furyl, pyridyl, anthracyl, naphthyl, phenanthryl, perinaphthyl or quinuclidinyl residue, which can be substituted by one or more hydroxyl groups, C1–C4 alkoxy groups, C1–C4 alkyl groups and/or one or more halogen atoms or one or more amino groups; Z represents O—CO—Y, O—S(O)2—Y, or O—P(O)(OH)—Y; and Y represents a linear or branched C1–C12 alkyl, C3–C8 cycloalkyl, benzyl, furyl or pyridyl residue, which can be substituted by one or more hydroxyl groups, carboxylic acid groups, C1–C4 alkoxy groups, C1–C4 alkyl groups and/or one or more halogen atoms or one or more amino groups. These compounds are useful for treating tumor diseases, autoimmune diseases, cardiovascular diseases, infections, and viral diseases.Type: GrantFiled: April 8, 2004Date of Patent: July 18, 2006Assignee: Biosphinks AktiengesellschaftInventor: Eberhard Amtmann
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Patent number: 7049460Abstract: The present invention relates to novel selective inhibitors of the urokinase plasminogene activator (uPA, EC 3.4.21.31) of the aryl guanidine type.Type: GrantFiled: August 23, 2000Date of Patent: May 23, 2006Assignee: Wilex AGInventors: Viktor Magdolen, Luis Moroder, Stefan Sperl, Jörg Stürzebecher, Olaf Wilhelm
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Patent number: 6949567Abstract: The invention relates to new diphenylurea having the formula (I) or a salt thereof, where Y is C?O, C?S, C?NH, (C?O)2 or SO2; and to processes for the preparation of these compounds and to their use in the treatment of protozoal diseases and to diseases where the inhibition of intracellular protein-degradation pathways is of benefit.Type: GrantFiled: February 26, 2002Date of Patent: September 27, 2005Assignee: 4SC AGInventors: Andrea Aschenbrenner, Katharina Aulinger Fuchs, Matthias Dormeyer, Gabriel Garcia, Bernd Kramer, Jürgen Kraus, Rolf Krauss, Johan Leban, Stefano Pegoraro, Wael Saeb, Kristina Wolf
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Patent number: 6927218Abstract: Compounds, compositions and methods treating arthritic disorders such as osteoarthritis or rheumatoid arthritis, and for treating other diseases associated with altered mitochondrial function, such as cancer, psoriasis, stroke, Alzheimer's Disease and diabetes. The compounds of this invention have the following structure (I): including stereoisomers, prodrugs and pharmaceutically acceptable salts thereof, wherein R1-5 are as defined herein. The methods of this invention are directed to administering to a warm-blooded animal in need thereof an effective amount of a compound of structure (I), typically in the form of a pharmaceutical composition.Type: GrantFiled: March 11, 2003Date of Patent: August 9, 2005Assignee: Migenix Corp.Inventors: Soumitra S. Ghosh, Tomas R. Szabo
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Patent number: 6911477Abstract: This invention relates to a novel class of partial or full muscarinic receptor agonists intermediates for their preparation, and pharmaceutical compositions and methods of use for the treatment or prevention of diseases the treatment or prevention of which is mediated by muscarinic receptor agonism.Type: GrantFiled: February 28, 2003Date of Patent: June 28, 2005Assignee: Pfizer Inc.Inventors: Anabella Villalobos, Daniel Yohannes, Jolanta Nowakowski, Dane R. Liston
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Patent number: 6849733Abstract: There are disclosed novel neuropeptide Y ligands having the general formula I Wherein the symbols W, A, D, R1, R2, R3, R4 are further defined in the description. Compounds of formula I are agonists and antagonists of neuropeptide Y, and are therefore useful as regulators.Type: GrantFiled: August 22, 1997Date of Patent: February 1, 2005Assignee: Agouron Pharmaceuticals, Inc.Inventors: Yufeng Hong, Vlad Edward Gregor, Anthony Lai Ling, Eileen Valenzuela Tompkins
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Patent number: 6787569Abstract: The present invention provides therapeutically useful substituted guanidines, and methods of treatment and pharmaceutical compositions that utilize or comprise one or more of such guanidines.Type: GrantFiled: August 11, 2000Date of Patent: September 7, 2004Assignee: Cambridge NeuroScience, Inc.Inventors: Stanley M. Goldin, James B. Fischer, Andrew Gannett Knapp, N. Laxma Reddy, David Berlove, Graham J. Durant, Subbarao Katragadda, Lain-Yen Hu, Sharad Magar, Wenhong Fan, Elizabeth Yost, Jun Qing Guo
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Patent number: 6774263Abstract: This invention relates to racemic and optically active N-(2-chloro-5-methylthiophenyl)-N′-(3-methylsulfinylphenyl)-N′-methylguanidine, N-(2-chloro-5-methylsulfinylphenyl)-1-(7-trifluoromethyl- 1,2,3,4-tetrahydroquinolinyl)carboximidamide, and N-(3-methylsulfinylphenyl)-N-methyl-N′-(2-chloro-5-methoxyphenyl)guanidine and pharmaceutically acceptable salts thereof, and pharmaceutical compositions and therapeutic methods of treatment that comprise such compounds. Compounds of the invention are particularly useful for the treatment or prophylaxis of neurological injury and neurodegenerative disorders.Type: GrantFiled: October 9, 1998Date of Patent: August 10, 2004Assignee: Cambridge Neuroscience, Inc.Inventors: Graham J. Durant, Michael Perlman, James B. Fischer, Seetharamaiyer Padmanabhan
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Patent number: 6706765Abstract: Aminoguanidine and alkoxyguanidine compounds, including compounds of the formula: wherein X is O or NR9 and R1-R4, R6-R9, R11, R12, Ra, Rb, Rc, Y, Z, n and m are set forth in the specification, as well as hydrates, solvates or pharmaceutically acceptable salts thereof, that inhibit proteolytic enzymes such as thrombin are described. Also described are methods for preparing the compounds of Formula I. The novel compounds of the present invention are potent inhibitors of proteases, especially trypsin-like serine proteases, such as chymotrypsin, trypsin, thrombin, plasmin and factor Xa. Certain of the compounds exhibit antithrombotic activity via direct, selective inhibition of thrombin, or are intermediates useful for forming compounds having antithrombotic activity.Type: GrantFiled: February 6, 2003Date of Patent: March 16, 2004Assignee: 3-Dimensional Pharmaceuticals, Inc.Inventors: Bruce E. Tomczuk, Richard M. Soll, Tianbao Lu, Cynthia L. Fedde, Carl R. Illig, Thomas P. Markotan, Thomas P. Stagnaro
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Patent number: 6673557Abstract: Methods are provided for treatment of eye disorders and injury, including methods for treatment of reduced flow of blood or other nutrients to retinal tissue and/or optic nerve, methods for treatment of retinal ischemia and trauma and methods for treatment for optic nerve injury/damage.Type: GrantFiled: January 29, 2002Date of Patent: January 6, 2004Inventor: Robert N. McBurney
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Patent number: 6656967Abstract: The invention provides fungicidal compounds of formula I and salts thereof: wherein the various radicals and substituents are as defined in the description, fungicidal compositions containing them and method for combating fungi which comprises applying these.Type: GrantFiled: August 6, 2001Date of Patent: December 2, 2003Assignee: Bayer Cropscience SAInventors: Vincent Gerusz, Darren James Mansfield, Joseph Perez, Jean-Pierre Vors
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Patent number: 6562821Abstract: Compounds, compositions and methods treating arthritic disorders such as osteoarthritis or rheumatoid arthritis, and for treating other diseases associated with altered mitochondrial function, such as cancer, psoriasis, stroke, Alzheimer's Disease and diabetes. The compounds of this invention have the following structure (I): including stereoisomers, prodrugs and pharmaceutically acceptable salts thereof, wherein R1-5 are as defined herein. The methods of this invention are directed to administering to a warm-blooded animal in need thereof an effective amount of a compound of structure (I), typically in the form of a pharmaceutical composition.Type: GrantFiled: February 27, 2002Date of Patent: May 13, 2003Assignee: MitoKorInventors: Soumitra S. Ghosh, Tomas R. Szabo
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Publication number: 20030045556Abstract: Compounds, compositions and methods treating arthritic disorders such as osteoarthritis or rheumatoid arthritis, and for treating other diseases associated with altered mitochondrial function, such as cancer, psoriasis, stroke, Alzheimer's Disease and diabetes.Type: ApplicationFiled: February 27, 2002Publication date: March 6, 2003Applicant: MitoKorInventors: Soumitra S. Ghosh, Tomas R. Szabo
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Publication number: 20020198392Abstract: This invention relates to a leather that contains scent-containing microcapsules in its cross section, wherein the walls of the microcapsules comprise reaction products of guanidine compounds and polyisocyanates.Type: ApplicationFiled: April 3, 2002Publication date: December 26, 2002Inventors: Martin Kleban, Jurgen Weisser, Friedrich Koch, Wolfgang Schwaiger
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Publication number: 20020103194Abstract: This invention relates to a novel class of partial or full muscarinic receptor agonists intermediates for their preparation, and pharmaceutical compositions and methods of use for the treatment or prevention of diseases the treatment or prevention of which is mediated by muscarinic receptor agonismType: ApplicationFiled: February 15, 2000Publication date: August 1, 2002Inventors: Anabella Villalobos, Daniel Yohannes, Jolanta Nowakowski, Dane Liston
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Patent number: 6420556Abstract: The subject invention involves novel acyl isothiocyanate resins of formula (I) and processes for making them: (a) starting with a phenyl carboxy resin, treating the resin with any reagent that converts the carboxy to an acyl halide, followed by treatment with tetranikylammonium thiocyanate or an alkali metal salt thereof, to provide the acyl isothiocyanate resin. The subject invention also involves processes for making guanidine compounds and related cyclized compounds using an acyl isothiocyanate resin, comprising the following steps: (b) reacting the acyl isothiocyanate resin with a primary amine; (c) reacting the product from Step (b) with a sulfur activating agent and ammonia or a primary or secondary amine; (d) treating the product from Step (c) with a strong base or medium strength acid to cleave product from the resin, providing the guanidine compound or/and the related cyclized compound.Type: GrantFiled: June 12, 2001Date of Patent: July 16, 2002Assignee: The Procter & Gamble CompanyInventor: Lawrence Joseph Wilson
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Patent number: 6358696Abstract: Methods are provided for treatment of eye disorders and injury, including methods for treatment of reduced flow of blood or other nutrients to retinal tissue and/or optic nerve, methods for treatment of retinal ischemia and trauma and methods for treatment for optic nerve injury/damage.Type: GrantFiled: August 9, 2000Date of Patent: March 19, 2002Inventor: Robert N. McBurney
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Patent number: 6348529Abstract: An object of the present invention is to provide a heat sensitive recording material which can develop color at high density by the inclusion of a novel guanidine compound which is strongly basic and superior in diffusion resistance. The present invention for attaining the above-described object is a heat sensitive recording material comprising a substrate supporting thereon a heat sensitive recording layer containing a diazonium salt compound, a coupler which reacts with the diazonium salt compound when heated to develop color, and abase, wherein the heat sensitive recording layer includes as the base at least one of the guanidine compounds represented by the general formula (1): wherein, in the general formula (1), R1 and R2 represent an alkyl group or aryl group and may be the same or different, R3 and R4 represent a hydrogen atom, alkyl group or halogen atom and may be the same or different, and X represents a divalent connecting group.Type: GrantFiled: January 4, 2000Date of Patent: February 19, 2002Assignee: Fuji Photo Film Co., Ltd.Inventors: Naoto Yanagihara, Hisao Yamada, Mitsuyuki Tsurumi
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Patent number: 6335303Abstract: The present invention describes methods of making a series of amine-containing organic compounds which are used as ligands for group 3-10 and lanthanide metal compounds. The ligands have electron-withdrawing groups bonded to them. The metal compounds, when combined with a cocatalyst, are catalysts for the polymerization of olefins.Type: GrantFiled: February 16, 2000Date of Patent: January 1, 2002Assignee: The Regents of the University of CaliforniaInventors: John G. Watkin, Damon R. Click
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Patent number: 6288123Abstract: The present invention provides therapeutically useful substituted guanidines, and methods of treatment and pharmaceutical compositions that utilize or comprise one or more of such guanidines.Type: GrantFiled: June 5, 1995Date of Patent: September 11, 2001Assignee: Cambridge NeuroSciences, Inc.Inventors: Stanley M. Goldin, James B. Fischer, Andrew Gannett Knapp, N. Laxma Reddy, David Berlove, Graham J. Durant, Subbarao Katragadda, Lain-Yen Hu, Sharad Magar, Wenhong Fan, Elizabeth Yost, Jun Qing Guo
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Patent number: 6251948Abstract: Tri- and tetra-substituted guanidines which exhibit a high binding affinity to phencyclidine (PCP) receptors and, more preferably, low affinity to the brain sigma receptors. These guanidine derivatives act as non-competitive inhibitors of glutamate induced responses of the NMDA receptor by acting as blockers for the ion channel of the NMDA receptor-ion channel complex. These compounds thus exert neuroprotective activity and are useful in the therapeutic treatment of neuronal loss in hypoxia, hypoglycemia, brain or spinal cord ischemia, and brain or spinal chord trauma as well as being useful for the treatment of epilepsy, Alzheimer's disease, Amyotrophic Lateral Sclerosis, Parkinson's disease, Huntington's disease, Down's Syndrome, Korsakoff's disease and other neurodegenerative disorders.Type: GrantFiled: June 6, 1995Date of Patent: June 26, 2001Assignee: State of Oregon, acting by and through the Oregon State Board of Higher Education, acting for and on behalf of the Oregon Health Sciences University and the University of OregonInventors: Eckard Weber, John F. W. Keana
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Patent number: 6242198Abstract: Methods are provided for treatment of eye disorders and injury, including methods for treatment of reduced flow of blood or other nutrients to retinal tissue and/or optic nerve, methods for treatment of retinal ischemia and trauma and methods for treatment for optic nerve injury/damage.Type: GrantFiled: July 25, 1996Date of Patent: June 5, 2001Assignee: Cambridge Neuroscience, Inc.Inventor: Robert N. McBurney
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Patent number: 6174924Abstract: The present invention provides therapeutically useful substituted guanidines, and methods of treatment and pharmaceutical compositions that utilize or comprise one or more of such guanidines.Type: GrantFiled: June 5, 1995Date of Patent: January 16, 2001Assignee: Cambridge NeuroScience, Inc.Inventors: Stanley M. Goldin, James B. Fischer, Andrew Gannett Knapp, N. Laxma Reddy, David Berlove, Graham J. Durant, Subbarao Katragadda, Lain-Yen Hu, Sharad Magar, Wenhong Fan, Elizabeth Yost, Jun Qing Guo
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Patent number: 6153604Abstract: The present invention provides therapeutically useful substituted guanidines of the following Formula: ##STR1## and methods of treatment and pharmaceutical compositions that utilize or comprise one or more of such guanidines.Type: GrantFiled: June 2, 1995Date of Patent: November 28, 2000Assignee: Cambridge NeuroScience, Inc.Inventors: Graham J. Durant, Sharad Magar, Lain-Yen Hu
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Patent number: 6150382Abstract: This invention is directed to monocyclic N-heterocyclics which are substituted by acyclic or cyclic thio derivatives which are useful as anti-coagulants. This invention is also directed to pharmaceutical compositions containing the compounds of the invention, and methods of using the compounds to treat disease-states characterized by thrombotic activity.Type: GrantFiled: May 21, 1999Date of Patent: November 21, 2000Assignee: Berlex Laboratories, Inc.Inventors: Monica J. Kochanny, Michael M. Morrissey, Howard P. Ng