Benzene Ring Containing Patents (Class 564/237)
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Publication number: 20150093365Abstract: Provided herein are compositions containing photoactivatable caged tamoxifen and tamoxifen derivative molecules. Also provided are kits containing one of these compositions and a light source. Also provided are methods of optically inducing nuclear translocation of a fusion protein containing a mammalian estrogen receptor ligand binding domain in a eukaryotic cell and methods of optically inducing recombination in a eukaryotic cell that include contacting a eukaryotic cell with at least one of these compositions. Also provided are methods of treating breast cancer in a subject that include administering a photoactivatable caged tamoxifen or tamoxifen derivative molecule to a subject having breast cancer.Type: ApplicationFiled: March 14, 2013Publication date: April 2, 2015Inventors: Xin Lu, Sarit S. Agasti, Ronald A. DePinho, Ralph Weissleder
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Publication number: 20150056305Abstract: Provided are dithiol mucolytic agents. These agents increase the liquefaction of mucus in a patient with excessive mucus or mucus with increased viscoelastic, cohesive, or adhesive properties. Also provided are a variety of methods of treatment using these inventive mucolytic agents.Type: ApplicationFiled: August 13, 2014Publication date: February 26, 2015Applicant: PARION SCIENCES, INC.Inventors: Michael R. Johnson, William R. Thelin, Ronald A. Aungst, JR.
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Publication number: 20140322304Abstract: Anti-cancer compositions and methods are described herein. In particular, compositions including one or more of leelamine, a leelamine derivative, abietylamine, an abietylamine derivative, and an abietic acid derivative are described. Methods for treatment of pathological conditions particularly cancer, in a subject using one or more of leelamine, a leelamine derivative, abietylamine, an abietylamine derivative, and an abietic acid derivative are described herein.Type: ApplicationFiled: July 10, 2014Publication date: October 30, 2014Inventors: Gavin P. Robertson, Raghavendra Gowda Chandagalu D., Subbarao V. Madhunapantula, Gajanan S. Inamdar, Omer F. Kuzu
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Publication number: 20140275539Abstract: Provided herein are stabilized radioiodinated and astatinated compounds, and to methods for their preparation.Type: ApplicationFiled: March 14, 2014Publication date: September 18, 2014Applicant: Ground Fluor Pharmaceuticals, Inc.Inventor: Stephen G. DiMagno
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Publication number: 20140221658Abstract: The disclosed modulators of Rb:Raf-1 interactions are potent, selective disruptors of Rb:Raf-1 binding, with IC50 values ranging from 80 nM to 500 nM. Further, these compounds are surprisingly effective in inhibiting a wide variety of cancer cells, including osteosarcoma, epithelial lung carcinoma, non-small cell lung carcinoma, three different pancreatic cancer cell lines, two different glioblastoma cell lines, metastatic breast cancer, melanoma, and prostate cancer. Moreover, the disclosed compounds effectively disrupt angiogenesis and significantly inhibited tumors in nude mice derived from human epithelial lung carcinoma tumors. Accordingly, the disclosed compounds, pharmaceutical compositions comprising the compounds, methods of inhibiting cell proliferation, methods of treating subjects with cancer, and methods of preparing the disclosed compounds are provided.Type: ApplicationFiled: February 3, 2014Publication date: August 7, 2014Applicant: University of South FloridaInventors: Said M. Sebti, Srikumar Chellappan, Nicholas James Lawrence
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Publication number: 20140039184Abstract: The present disclosure relates to a compound of formula (1): where R1 through R8, which can be identical or different from each other, each are selected from of the group comprising hydrogen and the radical —(CH2)k—X, where k is a whole number from 1 to 20 and where X is an organic radical comprising a) at least one neutral, protonizable nitrogen atom and/or b) at least one positively charged nitrogen atom, under the provision that at least 1 radical R1 through R8 is not hydrogen. The invention further relates to the production and use of said compound.Type: ApplicationFiled: February 23, 2012Publication date: February 6, 2014Inventors: Wolfgang Bäumler, Ariane Felgenträger, Karin Lehner, Tim Maisch, Johannes Regensburger, Francesco Santarelli, Andreas Spath
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Patent number: 8642278Abstract: The disclosed modulators of Rb:Raf-1 interactions are potent, selective disruptors of Rb:Raf-1 binding, with IC50 values ranging from 80 nM to 500 nM. Further, these compounds are surprisingly effective in inhibiting a wide variety of cancer cells, including osteosarcoma, epithelial lung carcinoma, non-small cell lung carcinoma, three different pancreatic cancer cell lines, two different glioblastoma cell lines, metastatic breast cancer, melanoma, and prostate cancer. Moreover, the disclosed compounds effectively disrupt angiogenesis and significantly inhibited tumors in nude mice derived from human epithelial lung carcinoma tumors. Accordingly, the disclosed compounds, pharmaceutical compositions comprising the compounds, methods of inhibiting cell proliferation, methods of treating subjects with cancer, and methods of preparing the disclosed compounds are provided.Type: GrantFiled: November 22, 2006Date of Patent: February 4, 2014Assignee: University of South FloridaInventors: Said M. Sebti, Srikumar Chellappan, Nicholas James Lawrence
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Publication number: 20140030189Abstract: Novel compounds that find use as imaging agents within nuclear medicine applications (PET imaging) for imaging of cardiac innervation are disclosed. These PET based radiotracers may exhibit increased stability, decreased NE release (thereby reducing side effects), improved quantitative data, and/or high affinity for VMAT over prior radiotracers. Methods of using the compounds to image cardiac innervation are also provided. In some instances the compounds are developed by derivatizing certain compounds with 18F in a variety of positions: aryl, alkyl, a keto, benzylic, beta-alkylethers, gamma-propylalkylethers and beta-proplylalkylethers. Alternatively or additionally, a methyl group a is added to the amine, and/or the catechol functionality is either eliminated or masked as a way of making these compounds more stable.Type: ApplicationFiled: June 12, 2013Publication date: January 30, 2014Inventors: Ajay Purohit, Thomas D. Harris, Heike S. Radeke, Simon P. Robinson, Ming Yu, David S. Casebier, Michael T. Azure
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Patent number: 8404893Abstract: Pentafluorosulfanylbenzoylguanidines of the formula I and II in which R1 to R4 have the meanings stated in the claims, are suitable as antiarrhythmic medicaments with a cardioprotective component for the prophylaxis of infarction and treatment of infarction and for the treatment of angina pectoris. They also inhibit preventively the pathophysiological processes associated with the development of ischemia-induced damage, especially in the triggering of ischemia-induced cardiac arrhythmias.Type: GrantFiled: August 25, 2011Date of Patent: March 26, 2013Assignee: Sanofi-Aventis Deutschland GmbHInventor: Heinz-Werner Kleemann
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Publication number: 20120196819Abstract: Compositions and methods for the treatment and control of various conditions in an animal which comprises administering to said animal an effective amount of a immediate release composition of about 0.5% to 50% wt/wt of active ingredient together with excipients to a total of about 100%, wherein said compositon dissolves in a relatively short period of time, e.g., 75 seconds or less, 5 seconds or less, or 3 seconds or less, upon administration to said animal.Type: ApplicationFiled: January 4, 2012Publication date: August 2, 2012Applicant: NEWMARKET PHARMACEUTICALS LLCInventors: David ROCK, Mark RIDALL
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Patent number: 8188296Abstract: The present invention relates to stabilized 123I-labelled radiopharmaceutical compositions having a stabilizer which comprises gentisic acid or a salt thereof with a biocompatible cation. Methods of preparation of the stabilized radioiodine compositions as well as the use of gentisic acid to stabilize 123I-labelled radiopharmaceutical at a specified radioactive concentration range are also described.Type: GrantFiled: March 31, 2006Date of Patent: May 29, 2012Assignee: GE Healthcare LimitedInventors: Ton Janssen, Jan Van Den Bos
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Publication number: 20120129894Abstract: The present invention relates generally to compositions and methods for treating neurodegenerative diseases and disorders, particularly ophthalmic diseases and disorders. Provided herein are alkoxyl derivative compounds and pharmaceutical compositions comprising these compounds. The subject compositions are useful for treating and preventing ophthalmic diseases and disorders, including age-related macular degeneration (AMD) and Stargardt's Disease.Type: ApplicationFiled: May 19, 2011Publication date: May 24, 2012Applicant: Acucela Inc.Inventors: Ian L. Scott, Vladimir A. Kuksa, Mark W. Orme, Thomas Little, Anna Gall, Feng Hong
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Publication number: 20120101287Abstract: The invention related to an optically active compound of formula (I) or a salt thereof: wherein the various symbols are as defined in the description, to processes for their preparation, to compositions thereof, and to their use as herbicides or plant growth regulators. The invention also relates to novel intermediates of formula (III), (V) and (XIII) as defined in the description.Type: ApplicationFiled: December 28, 2011Publication date: April 26, 2012Applicant: Bayer CropScience AGInventors: Hartmut Ahrens, Hansjöerg Dietrich, Klemens Minn, Thomas Auler, Hermann Bieringer, Martin Hills, Heinz Kehne, Hubert Menne
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Patent number: 8153647Abstract: Disclosed are compounds according to formula (I): wherein A, Q, X, Y, Z, R1, R2, R3, R4, R5, R6, R7, R8, R9, R10 and R11 are as defined herein. The disclosure also relates to pharmaceutical compositions containing a compound of formula (I), to processes for preparing the compounds of formula (I), and to methods of using the compounds of formula (I).Type: GrantFiled: December 15, 2008Date of Patent: April 10, 2012Assignee: Sanofi-AventisInventors: Jozsef Zsolt Bocskei, Gary McCort, Hans Matter, Henning Steinhagen, Bérangère Thiers
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Patent number: 8148577Abstract: Polyamine, polyamine/guanidino, and polyamine/biguanide compounds are disclosed. The compounds are useful as anti-cancer and anti-parasitic treatments. The compounds are also useful as inhibitors of the enzyme lysine-specific demethylase-1.Type: GrantFiled: April 20, 2010Date of Patent: April 3, 2012Assignees: The Johns Hopkins University, Wayne State UniversityInventors: Patrick M. Woster, Tracey Boncher, Robert A. Casero
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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: 20110196149Abstract: A method for the fluoridation of an iodonium salt with a fluoride ion source which can be carried out in an aqueous reaction solvent.Type: ApplicationFiled: April 18, 2011Publication date: August 11, 2011Applicant: GE HEALTHCARE LIMITEDInventors: HARRY JOHN WADSWORTH, PETER ANTHONY DEVENISH
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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: 7932422Abstract: The invention relates to chlorine Guanabenz derivatives for treating Huntington's disease and other polyglutamine expansion associated diseases. More specifically, it relates to the use of the molecule of formula (I) wherein R?H or Cl and the phenyl group is at least substituted twice, or a pharmaceutically acceptable salt thereof, for the manufacture of a medicament for treating polyglutamine expansion associated diseases.Type: GrantFiled: October 3, 2007Date of Patent: April 26, 2011Inventors: Anne Bertolotti, Marc Blondel
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Patent number: 7847124Abstract: Disclosed is an alanine racemase chiral binaphthol derivative having the ability to recognize amino alcohols selectively on the basis of chirality and transform amino acids from an L-form into a D-form. Methods for the optical resolution of amino acid or amino alcohol and for the optical transformation of D- and L-forms of amino acids using the binaphthol derivative are also provided.Type: GrantFiled: February 8, 2008Date of Patent: December 7, 2010Assignee: Green Formula Co., Ltd.Inventors: Kwan Mook Kim, Lijun Tang
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Publication number: 20100274052Abstract: According to a first aspect of the invention, a process is disclosed for the preparation of radiolabelled haloaromatic compounds. According to a second aspect of the invention, intermediate precursor insoluble polymer compounds used in the preparation of the radiolabelled haloaromatics are disclosed, as well as processes for the preparation of the intermediate precursor insoluble polymer compounds.Type: ApplicationFiled: February 8, 2010Publication date: October 28, 2010Inventors: Duncan H. Hunter, Xizhen Zhu
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Publication number: 20100221182Abstract: Novel compounds that find use as imaging agents within nuclear medicine applications (PET imaging) for imaging of cardiac innervation are disclosed. These PET based radiotracers may exhibit increased stability, decreased NE release (thereby reducing side effects), improved quantitative data, and/or high affinity for VMAT over prior radiotracers. Methods of using the compounds to image cardiac innervation are also provided. In some instances the compounds are developed by derivatizing certain compounds with 18F in a variety of positions: aryl, alkyl, a keto, benzylic, beta-alkylethers, gamma-propylalkylethers and beta-proplylalkylethers. Alternatively or additionally, a methyl group a is added to the amine, and/or the catechol functionality is either eliminated or masked as a way of making these compounds more stable.Type: ApplicationFiled: December 21, 2007Publication date: September 2, 2010Inventors: Ajay Purohit, Thomas D, Harris, Heike S. Radeke, Simon P. Robinson, Ming Yu, David S. Casebier, Michael T. Azure
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Publication number: 20100190766Abstract: Antibacterial compounds of formula (I) are provided: as well as stereoisomers, pharmaceutically acceptable salts, esters, and prodrugs thereof; pharmaceutical compositions comprising such compounds; methods of treating bacterial infections by the administration of such compounds; and processes for the preparation of such compounds.Type: ApplicationFiled: December 10, 2009Publication date: July 29, 2010Applicant: Achaogen, Inc.Inventors: Heinz E. Moser, Qing Lu, Phillip A. Patten, Dan Wang, Ramesh Kasar, Stephen Kaldor, Brian D. Patterson
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Publication number: 20100056641Abstract: There are described compounds of general formula (I) and isomeric forms thereof wherein n is 0, 1, 2 or 3, saturated or unsaturated; most preferably at least one of R1 to R5 represents halogen; at least one of R1, R2, R3, R4 and R5 is selected from —S—R or —COOR, or two or more Of R1-R5 comprise a linking group such as —S—(CH2)mS—, where m is 1, 2 or 3 and R is selected from alkyl having 1 to 5 carbon atoms, cycloalkyl having 3-6 carbon atoms, hydroxy, and aryl having 6 to 10 carbon atoms, such groups being optionally substituted, and when R1 is selected from —S—R, then at least one of R2, R3 and R5 is most preferably selected from halogen; and R1, R2, R3, R4 and R5 are otherwise the same or different and are selected from hydrogen, halogen, alkyl having 1 to 5 carbon atoms, electron donor groups such as alkoxy having 1-5 carbon atoms or hydroxy, electron acceptor groups selected from cyano, nitro, trifluoroalkyl or amide; alkylamino, benzoyloxy, nitroxy, phenyl or sulpho; and pharmacologically acceptable salType: ApplicationFiled: December 13, 2007Publication date: March 4, 2010Applicant: ACURE PHARMA ABInventors: Torbjorn Lundstedt, Elisabeth Seifert, Per Lek, Arne Boman
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Patent number: 7629493Abstract: The invention relates to a process for the crystallization of the compounds of the formula (I) or acid-addition salts thereof, in which R1, R2 and R3 have the meaning indicated in Claim 1.Type: GrantFiled: April 10, 2004Date of Patent: December 8, 2009Assignee: Merck Patent GmbHInventors: Michael Kirschbaum, Ekkehard Bartmann, Dieter Bensinger, Alexander Haas, Ricky Lippert
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Publication number: 20090099239Abstract: The present invention relates to novel compounds and compositions having antiviral activity. The invention also relates to methods for the therapeutic or prophylactic treatment of viral infections in mammals.Type: ApplicationFiled: June 23, 2006Publication date: April 16, 2009Inventors: Gary Dinneen Ewart, Wayne Morris Best
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Publication number: 20090005595Abstract: The present invention relates to stabilised 123I-labelled radiopharmaceutical compositions having a stabiliser which comprises gentisic acid or a salt thereof with a biocompatible cation. Methods of preparation of the stabilised radioiodine compositions as well as the use of gentisic acid to stabilise 123I-labelled radiopharmaceutical at a specified radioactive concentration range are also described.Type: ApplicationFiled: March 31, 2006Publication date: January 1, 2009Inventors: Ton Janssen, Jan Van Den Bos
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Publication number: 20080293751Abstract: Compounds of the formula I: or pharmaceutically acceptable salts thereof, wherein m, p, q, Ar, R1 and R2 are as defined herein. Also provided are methods for preparing, compositions comprising, and methods for using compounds of formula I.Type: ApplicationFiled: November 15, 2007Publication date: November 27, 2008Inventors: Robert Greenhouse, Ralph New Harris, III, Saul Jaime-Figueroa, James M. Kress, David Bruce Repke, Russell Stephen Stabler
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Publication number: 20080214797Abstract: Disclosed herein is a method for the preparation of radioisotope-labeled compounds using CNT. It comprises filling the carbon nanotube with a radioisotope; and labeling a physiologically active material with the radioisotope charged in the carbon nanotube. Taking advantage of CNT, the method can prepare a radioisotope-labeled compound invention at a high yield and in a simple manner. Also, the radioisotope, when remaining unreacted, can be recovered by the filtration of the CNT, thereby achieving the prevention of radioactive contamination and the reduction of radioactive waste. Further, the radioisotope-labeled compound is useful as a contrast medium for imaging the hepatobiliary system.Type: ApplicationFiled: April 20, 2007Publication date: September 4, 2008Inventors: Sang Hyun Park, Hui Jeong Gwon, Myung Woo Byun
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Publication number: 20080200553Abstract: Pentafluorosulfanylbenzoylguanidines of the formula I and II in which R1 to R4 have the meanings stated in the claims, are suitable as antiarrhythmic medicaments with a cardioprotective component for the prophylaxis of infarction and treatment of infarction and for the treatment of angina pectoris. They also inhibit preventively the pathophysiological processes associated with the development of ischemia-induced damage, especially in the triggering of ischemia-induced cardiac arrhythmias.Type: ApplicationFiled: April 14, 2008Publication date: August 21, 2008Applicant: SANOFI-AVENTIS DEUTSCHLAND GMBHInventor: Heinz-Werner KLEEMANN
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Publication number: 20080146673Abstract: Pentafluorosulfanylbenzoylguanidines of formula I wherein R1 to R4 have the meanings stated in the claims, are suitable, for example, as antiarrhythmic medicaments with a cardioprotective component for the prophylaxis of infarction and treatment of infarction and for the treatment of angina pectoris. They also inhibit preventively the pathophysiological processes associated with the development of ischemia-induced damage, especially in the triggering of ischemia-induced cardiac arrhythmias.Type: ApplicationFiled: January 11, 2008Publication date: June 19, 2008Applicant: sanofi-aventis Deutschland GmbHInventor: Heinz-Werner KLEEMANN
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Patent number: 7285682Abstract: The present invention provides terphenyl guanidine compounds of formula I The present invention also provides methods for the use thereof to inhibit ?-secretase (BACE) and treat ?-amyloid deposits and neurofibrillary tangles.Type: GrantFiled: February 13, 2006Date of Patent: October 23, 2007Assignee: WyethInventor: Baihua Hu
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Patent number: 7153881Abstract: The present invention provides novel compounds and use of compounds of general formula (I) as ligands to the melanocortin receptors and/or for treatment of disorders in the melanocortin system: Wherein X and Y are independently chosen from O, N, S and (CH2)n, where n is 0, 1, 2, 3, 4, or 5, or a combination of these and may contain carbon-carbon multiple bonds and branched chains as well as alicyclic and heterocyclic groups; Q is H or OH; R1 and R2 can be either the same or different and are chosen from hydrogen or the residue of an aromatic group as listed in Scheme 1 and the pharmacologically active salts thereofType: GrantFiled: August 7, 2001Date of Patent: December 26, 2006Assignee: Acure Pharma ABInventors: Torbjörn Lundstedt, Anna Skottner, Arne Boman, Per Andersson, Victor Andrianov, Ivars Kalvins
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Patent number: 7109329Abstract: This invention provides pharmacologically active compounds having neurological and other bio-active capability. These active compounds comprise the derivatives of guanidino, aminoguanidino, 2-imadazolino, 2-hydrazinoimidazolino or 2-guanidinobenzimidazolino groups.Type: GrantFiled: July 1, 2002Date of Patent: September 19, 2006Inventor: N. Eric Naftchi
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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: 6906076Abstract: The present invention concerns alkyl aryl carbonyl compounds that possess anti-infective activity. The compounds of the invention can be used to target specific nuclear localization signal, thereby blocking importation of specific proteins or molecular complex into the nucleus of a cell. The invention encompasses methods of use of such compounds for treatment or prevention of infectious diseases, such as parasitic and viral diseases, including, for example, malaria and acquired immunodeficiency syndrome. The use of the compounds to detect certain specific protein structures which are present in nuclear localization sequences is also taught.Type: GrantFiled: September 12, 2003Date of Patent: June 14, 2005Assignee: Cytokine Pharmasciences, Inc.Inventors: Michael I. Bukrinsky, Anthony Cerami, Peter Ulrich, Bradley Berger
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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: 6768024Abstract: The invention provides triamine derivative melanocortin receptor ligands of the formula: wherein R1 to R8 and n have the meanings provided herein. The invention further provides methods of using the ligands to alter or regulate the activity of a melanocortin receptor.Type: GrantFiled: August 4, 2000Date of Patent: July 27, 2004Assignee: Lion Bioscience AGInventors: Karen J. Watson-Straughan, Timothy C. Gahman, Ming Qi, Christa Hamashin, James E. Macdonald, Michael J. Green, Kevin R. Holme, Michael C. Griffith
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Publication number: 20040132782Abstract: The present invention provides compounds having formula (I): 1Type: ApplicationFiled: June 16, 2003Publication date: July 8, 2004Inventors: Wenjin Yang, Douglas R. Cary, Jeffrey W. Jacobs, Wanli Lu, Yafan Lu, Jian Sun, Min Zhong
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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: 6680408Abstract: Processes for preparing &agr;-substituted benzylnitroguanidines include the steps of providing a reaction mixture comprising water, alcohol, an S-alkyl nitroisothiourea, and an &agr;-substituted benzylamine; heating the reaction mixture; steam distilling the alcohol from the reaction mixture; and isolating an &agr;-substituted benzylnitroguanidine from the remaining water layer.Type: GrantFiled: June 20, 2002Date of Patent: January 20, 2004Assignee: Bayer Cropscience LPInventors: David M. Mayes, Vijay C. Desai, Eric Rivadeneira
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Patent number: 6673968Abstract: The present invention relates to an NHE-1 selective Na+/H+ antiporter inhibitor N-(4,5-bismethanesulfonyl-2-methylbenzoyl)guanidine, hydrochloride, to its hydrochloride hydrate, and to a process for the preparation.Type: GrantFiled: September 4, 2002Date of Patent: January 6, 2004Assignee: Merck Patent Gesellschaft mit beschränkter HaftungInventors: Rolf Gericke, Manfred Baumgarth, Hans Markus Bender, Bernhard Ladstetter
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Publication number: 20030203969Abstract: The present invention relates to aromatic guanylhydrazone compounds and their use as pharmaceutically active agents, especially for prophylaxis and treatment of virally caused diseases and infections, including opportunistic infections. The inventive guanylhydrazone compounds are also useful as inhibitors of deoxyhypusine synthase and as inhibitors for nuclear export in infectious diseases and may be used to regulate bacterially induced TNF-&agr; production. Furthermore, the aromatic guanylhydrazones exhibit antibacterial activity against Gram positive and Gram negative bacteria and can be regarded as a novel class of antibiotics. In addition, methods for prophylaxis and treatment of virally or bacterially induced infections and diseases are disclosed together with pharmaceutical compositions useful within said methods containing at least one aromatic guanylhydrazone of the present invention as active ingredient.Type: ApplicationFiled: January 7, 2003Publication date: October 30, 2003Inventors: Dorian Bevec, Joachim Hauber, Sabine Obert, Gyorgy Keri, Laszlo Orfi, Istvan Szekely, Axel Choidas, Gerald Bacher
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Patent number: 6632840Abstract: Monoacyl-substituted guanidines of formula III, or a salt or acid thereof, and their use as medicine or diagnostic aid: in which X(2) isType: GrantFiled: March 24, 2000Date of Patent: October 14, 2003Assignee: Hoechst AktiengesellschaftInventors: Heinz-Werner Kleemann, Hans-Jochen Lang, Andreas Weichert, Peter Crause, Wolfgang Scholz, Udo Albus, Jan-Robert Schwark
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Publication number: 20030119876Abstract: The invention relates to new diphenylurea having the formula (I) 1Type: ApplicationFiled: February 26, 2002Publication date: June 26, 2003Inventors: Andrea Aschenbrenner, Katharina Aulinger Fuchs, Matthias Dormeyer, Gabriel Garcia, Bernd Kramer, Jurgen Kraus, Rolf Krauss, Johan Leban, Stefano Pegoraro, Wael Saeb, Kristina Wolf
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Publication number: 20030119855Abstract: There is provided an excellent novel analgesic having an analgesic effect which is effective widely against a pain including a chronic pain or an allodynia accompanied with herpes zoster by acting on a nociceptin receptor.Type: ApplicationFiled: September 25, 2002Publication date: June 26, 2003Inventors: Masahiko Okano, Kazuya Mori
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Patent number: 6573404Abstract: The invention relates to a process for the preparation of ortho-alkylated benzoic acid derivatives of the formula I characterized in that an aryl bromide of the formula II is reacted with a secondary or tertiary organolithium compound and CO2.Type: GrantFiled: October 8, 2002Date of Patent: June 3, 2003Assignee: Merck Patent GmbHInventors: Ekkehard Bartmann, Ingeborg Stein
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Patent number: 6570038Abstract: Hexasubstituted guanidinium chlorides are prepared by a method which affords them in high yield as aqueous solutions, optionally also containing alkali metal chlorides. The solutions may be employed as sources of hexasubstituted guanidinium salts useful as phase transfer catalysts for the reaction of alkali metal salts of dihydroxyaromatic compounds with substituted imides to form polyetherimides or their intermediates.Type: GrantFiled: June 9, 2000Date of Patent: May 27, 2003Inventors: Joseph John Caringi, Peter David Phelps, Thomas Link Guggenheim, Daniel Joseph Brunelle