Plural Acyclic Nitrogens Bonded Directly To The Same Carbon Or Single Bonded Directly To Each Other Patents (Class 546/306)
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Publication number: 20100184787Abstract: The invention relates to the hetaryl-substituted guanidine compounds of general formula (I), enantiomeres, diastereomeres and/or tautomeres thereof, in addition to the pharmaceutically acceptable salts thereof and the prodrugs of the known compounds. The invention also relates to the use of said hetaryl-substituted guanidine compounds as binding partners for 5-HT5-receptors for treating and/or for the prophylaxis of illnesses which are modulated by a 5-HT5-receptor activity, in particular, for treating and/or for the prophylaxis of neurodegenerative and neuropsychiatric disorders, and signs, symptoms and dysfunctions associated with said disorders.Type: ApplicationFiled: August 23, 2006Publication date: July 22, 2010Inventors: Wilhelm Amberg, Astrid Netz, Andreas Kling, Michael Ochse, Udo Lange, Charles W. Hutchins, Francisco Javier Garcia-Ladona, Wolfgang Wernet
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Publication number: 20100160300Abstract: Methods for treatment of depression-related mood disorders in mammals, particularly humans are disclosed. The methods of the invention include administration of compounds capable of enhancing glutamate transporter activity in the brain of mammals suffering from depression. ATP-sensitive K+ channel openers and ?-lactam antibiotics are used to enhance glutamate transport and to treat depression-related mood disorders and depressive symptoms.Type: ApplicationFiled: December 18, 2009Publication date: June 24, 2010Applicant: Brookhaven Science Associates, LLCInventor: Fritz Henn
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Publication number: 20100130736Abstract: Drug discovery is a complex undertaking facing many challenges, not the least of which is a high attrition rate as many promising candidates prove ineffective or toxic in the clinic owing to a poor understanding of the diseases, and thus the biological systems, they target. Therefore, it is broadly agreed that to increase the productivity of drug discovery one needs a far deeper understanding of the molecular mechanisms of diseases, taking into account the full biological context of the drug target and moving beyond individual genes and proteins. The present methods rely on the use of label-free cellular assays, particularly the DMR index, to systematically display the mode of actions, the toxicity, and the target(s) and pathway(s) of any molecules.Type: ApplicationFiled: November 23, 2009Publication date: May 27, 2010Inventors: Ye Fang, Ann M. Ferrie, Joydeep Lahiri, Elizabeth Tran
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Patent number: 7662822Abstract: This invention relates to substituted azaquinazolines, to a process for their preparation, to pharmaceutical compositions containing them, and to their use for the treatment and/or prophylaxis of diseases, especially for use as antiviral agents, in particular against cytomegaloviruses.Type: GrantFiled: April 23, 2005Date of Patent: February 16, 2010Assignee: Bayer Schering Pharma AktiengesellschaftInventors: Tobias Wunberg, Judith Baumeister, Mario Jeske, Frank Süβmeier, Holger Zimmermann, Kerstin Henninger, Dieter Lang
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Publication number: 20090298891Abstract: The present invention features methods of inhibiting ribonucleotide reductase and DNA synthesis after administration of a dose of ionizing radiation to cells. The present invention further features methods of treating patients suffering from cancer comprising contemporaneous or sequential administration of a radiosensitizing dose of a 2-carboxyaldehyde pyridine thiosemicarbazone compound and ionizing radiation.Type: ApplicationFiled: September 15, 2006Publication date: December 3, 2009Applicant: GOVERNMENT OF THE US, AS REPRESENTED BY THE SECRETADY OF HEALTH AND HUMAN SERVICESInventors: Philip Tofilon, Kevin Camphausen, David Gius
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Patent number: 7598277Abstract: The present invention relates to inhibitors of p38, a mammalian protein kinase involved cell proliferation, cell death and response to extracellular stimuli. The invention also relates to inhibitors of ZAP70. The invention also relates to methods for producing these inhibitors. The invention also provides pharmaceutical compositions comprising the inhibitors of the invention and methods of utilizing those compositions in the treatment and prevention of various disorders.Type: GrantFiled: February 5, 2007Date of Patent: October 6, 2009Assignee: Vertex Pharmaceuticals IncorporatedInventors: John Cochran, Vincent Galullo, Guy W. Bemis
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Publication number: 20090215780Abstract: This invention relates to certain aryl alkyl acid compounds, compositions, and methods for treating or preventing obesity and related diseases.Type: ApplicationFiled: April 18, 2006Publication date: August 27, 2009Applicant: Bayer Pharmaceuticals CorporationInventors: Roger Smith, Derek Lowe, Philip Coish, Ann-Marie Campbell, Gan Wang, Manoj Patel, Gerogiy Bondar
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Publication number: 20090156825Abstract: The present invention relates to a novel class of fluorescent compounds that bind to histone deacetylases. The fluorescent compounds can be used to determine binding association and dissociation rates of histone deacetylase inhibitors via fluorescence polarization.Type: ApplicationFiled: November 25, 2008Publication date: June 18, 2009Inventors: Richard W. Heidebrecht, JR., Astrid M. Kral, Thomas A. Miller
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Publication number: 20090149510Abstract: The invention relates to compounds and methods for modulating one or more components of a kinase cascade.Type: ApplicationFiled: July 7, 2008Publication date: June 11, 2009Inventor: David G. Hangauer, JR.
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Publication number: 20090136473Abstract: The present invention relates to a genus of biaryl compounds containing at least one further ring. The compounds are PDE4 inhibitors useful for the treatment and prevention of stroke, myocardial infarct and cardiovascular inflammatory diseases and disorders.Type: ApplicationFiled: November 20, 2008Publication date: May 28, 2009Applicant: DECODE GENETICS EHFInventors: Jasbir Singh, Mark E. Gurney, Alex Burgin, Alexander Kiselyov, Munagala Rao, Timothy Hagen
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Publication number: 20090082350Abstract: Disclosed are heterocylic or heteroaryl compounds and compositions that inhibit soluble epoxide hydrolase (sEH), methods for preparing the compounds and compositions, and methods for treating patients with such compounds and compositions. The compounds, compositions, and methods are useful for treating a variety of sEH mediated diseases, including hypertensive, cardiovascular, inflammatory, pulmonary, and diabetic-related diseases.Type: ApplicationFiled: September 10, 2008Publication date: March 26, 2009Inventors: Sampath-Kumar Anandan, Richard D. Gless, JR.
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Publication number: 20090075981Abstract: The present invention relates to inhibitors of p38, a mammalian protein kinase involved cell proliferation, cell death and response to extracellular stimuli. The invention also relates to methods for producing these inhibitors. The invention also provides pharmaceutical compositions comprising the inhibitors of the invention and methods of utilizing those compositions in the treatment and prevention of various disorders.Type: ApplicationFiled: August 1, 2008Publication date: March 19, 2009Applicant: VERTEX PHARMACEUTICALS INCORPORATEDInventors: Francesco Salituro, Vincent Galullo, Steven Bellon, Guy Bemis, John Cochran
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Publication number: 20080319028Abstract: This invention relates to dicycloalkylcarbamoyl ureas of formula (I), which are activators of glucokinase and thus may be useful for the management, treatment, control, or adjunct treatment of diseases, where increasing glucokinase activity is beneficial.Type: ApplicationFiled: July 7, 2006Publication date: December 25, 2008Applicant: Novo Nordisk A/SInventors: Anthony Murray, Jesper Lau, Per Vedso, Lone Jeppesen, Marit Kristiansen
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Publication number: 20080312161Abstract: The invention relates to novel compounds with formula I and their use in stabilization of Factor Vila or other Factor VII polypeptides, particularly in aqueous liquid compositions thereof.Type: ApplicationFiled: February 24, 2006Publication date: December 18, 2008Inventors: Anders Klarskov Petersen, Andrew Neil Bowler
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Publication number: 20080261952Abstract: A method of treating a condition associated with the CB-1 receptor, in particular obesity, by administering an effective amount of an aryl urea CB-1 receptor modulating compound to a subject in need of such treatment.Type: ApplicationFiled: August 16, 2005Publication date: October 23, 2008Inventors: Jason Bloxham, Matthew Colin Thor Fyfe, James Horswill, Revathy Perpetua Jeevaratnam, John Keily, Martin James Procter, Karen Lesley Schofield, Salam Shaaban, Andrew Simon Swain, Phillppe Wong-Kai-In
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Publication number: 20080132507Abstract: A compound represented by the following general formula (1) or a salt thereof or a hydrate of the foregoing is safe while exhibiting suitable physicochemical stability, and is useful as therapeutic or prophylactic agents for diseases associated with thrombus formation. wherein R1a, R1b, R1c and R1d each independently represent hydrogen, etc., R2 represents optionally substituted phenyl, etc., R3 represents optionally substituted C6-10 aryl, etc., Z1, Z2 and Z3 each independently represent hydrogen, etc., Z4 represents hydrogen, etc. and X represents a single bond or —CO—, etc.Type: ApplicationFiled: October 13, 2005Publication date: June 5, 2008Applicant: Eisai R&D Management Co., Ltd.Inventors: Richard Clark, Shinsuke Hirota, Hiroshi Azuma, Kazunobu Kira, Nobuhisa Watanabe, Tadashi Nagakura, Tatsuo Horizoe
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Patent number: 7317104Abstract: Chelants and macrocyclic metal complexes thereof, methods of preparing the chelants and macrocyclic metal complexes, and radiopharmaceutical compositions comprising the macrocyclic metal complexes are disclosed. Methods of using the macrocyclic metal complexes as radiopharmaceuticals for the diagnosis of cardiovascular disorders, infectious diseases and cancer are also disclosed. Chelants as bifunctional chelators (BFCs) for the radiolabeling of target-specific biomolecules, such as proteins, peptides, peptidomimetics, non-peptide receptor ligands, enzyme inhibitors, and enzyme substrates are disclosed. Methods of using macrocyclic metal complexes containing the chelant-biomolecule conjugates as target-specific diagnostic radiopharmaceuticals that selectively localize at sites of disease and allow an image to be obtained of the loci using gamma scintigraphy are disclosed.Type: GrantFiled: June 9, 2004Date of Patent: January 8, 2008Assignee: Bristol-Myers Squibb Pharma CompanyInventor: Shuang Liu
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Patent number: 7253193Abstract: Pyridyl cyanoguanidine compounds of the general formula I wherein A, X1, X2, X3, Y1, Y2, Y3, R1, R2, R5, R6 and n are as indicated in the description are suitable as prodrugs in human and veterinary therapy of proliferative diseases such as cancers.Type: GrantFiled: May 15, 2003Date of Patent: August 7, 2007Assignee: LEO Pharma A/SInventors: Ernst Torndal Binderup, Tore Duvold
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Patent number: 7241780Abstract: Compounds are provided which have the structure wherein Q is C or N, A is O or S, Z is O or a bond, X is CH or N and R1, R2, R2a, R2b, R2c, R3, Y, x, m, and n are as defined herein, which compounds are useful as antidiabetic, hypolipidemic, and antiobesity agents.Type: GrantFiled: October 13, 2004Date of Patent: July 10, 2007Assignee: Bristols-Myers Squibb CompanyInventors: Peter T. Cheng, Pratik Devasthale, Yoon Jeon, Sean Chen, Hao Zhang
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Patent number: 7186737Abstract: The present invention relates to inhibitors of p38, a mammalian protein kinase involved cell proliferation, cell death and response to extracellular stimuli. The invention also relates to inhibitors of ZAP70. The invention also relates to methods for producing these inhibitors. The invention also provides pharmaceutical compositions comprising the inhibitors of the invention and methods of utilizing those compositions in the treatment and prevention of various disorders.Type: GrantFiled: February 11, 2003Date of Patent: March 6, 2007Assignee: Vertex Pharmaceuticals IncorporatedInventors: John Cochran, Vincent Galullo, Guy W. Bemis
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Patent number: 7056925Abstract: Compounds having the formula are useful for inhibiting protein kinases. Also disclosed are methods of making the compounds, compositions containing the compounds, and methods of treatment using the compounds.Type: GrantFiled: August 13, 2003Date of Patent: June 6, 2006Assignee: Abbott LaboratoriesInventors: Gaoquan Li, Qun Li, Tongmei Li, Nan-Horng Lin, Robert A. Mantei, Hing L. Sham, Gary T. Wang
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Patent number: 7045512Abstract: A fungicidally active compound of the formula: a) wherein Q is —NY—NH—, —N?N—, or X is oxygen, sulfur, sulfoxide, or sulfone; n is 0 or 1; Y is hydrogen, C1–C4 alkanoyl, C1–C4 haloalkanoyl, C1–C6 straight chain or branched alkoxycarbonyl, C1–C4 alkoxy(C1–C4)alkoxycarbonyl, C1–C4 alkyl, or C1–C4 haloalkyl; R1 is C1–C6 alkoxy, C3–C6 branched alkoxy, C3–C6 cycloalkoxy, phenoxy, benzyloxy, C2–C6 alkenyloxy, C2–C6 alkynyloxy, C1–C6 haloalkoxy, silyloxy, (C1–C6 alkoxy)-carbonylmethoxy, C1–C6 thioalkoxy, C1–C6 alkylamino, C1–C6 alkyl, C3–C6 branched alkyl, (C1–C6 alkoxy) C1–C6 alkoxy, or (C1–C6 alkoxy)carbonyl; R2 and R3 are each, independently, hydrogen, halogen, C1–C6 alkyl, C3–C6 branched alkyl, C1–C6 haloalkyl, C1–C6 alkoxy, C1–C6 haloalkoxy, cyano, or (C1–C6 alkoxy)carbonyl; R4 is C1–C6 alkyl; and Z1 and Z2 are each independently, carbon or nitrogen, with the proviso that when Z1 is carbon, X is oxygen, and R2 is hydrogen, then R3 cannot be hydrogen; b) wherein R5 is C1–C6 alkoxy; and R6 andType: GrantFiled: May 27, 2004Date of Patent: May 16, 2006Assignees: Uniroyal Chemical Company, Inc., Crompton Co./CiieInventors: Gaik-Lean Chee, Mark A. Dekeyser, Kenneth W. Seebold, Jr., Ewa Maria Osika, Walter G. Brouwer, Sheldon B. Park, Hoi Kiong Lai
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Patent number: 7022695Abstract: Thioether-substituted benzamide compounds having the formula: are provided that exhibit exceptionally strong inhibition of Factor Xa in combination with weak hERG binding.Type: GrantFiled: October 5, 2004Date of Patent: April 4, 2006Assignee: Millennium Pharmaceuticals, Inc.Inventors: Bing-Yan Zhu, Erick A. Goldman, Wenrong Huang, Penglie Zhang
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Patent number: 6989398Abstract: Benzanilides are provided which are voltage-dependent potassium channel openers. Methods of using the benzanilides of the invention are also provided.Type: GrantFiled: February 2, 2004Date of Patent: January 24, 2006Assignee: ICAgen, Inc.Inventors: Grant A. McNaughton-Smith, Michael F. Gross, Alan D. Wickenden
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Patent number: 6936719Abstract: Compounds of formula (I) are useful as inhibitors of trypsin like serine protease enzymes such as thrombin, factor VIIa, factor Xa, TF/FVIIa, and trypsin. These compounds could be useful to treat and/or prevent clotting disorders, and as anticoagulating agents.Type: GrantFiled: December 18, 2003Date of Patent: August 30, 2005Assignee: BioCryst Pharmaceuticals, Inc.Inventors: Yarlagadda S. Babu, R. Scott Rowland, Pooran Chand, Pravin L. Kotian, Yahya El-Kattan, Shri Niwas
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Patent number: 6897209Abstract: A complex of a radiometal or paramagnetic metal ion with a metal chelating agent such as a diaminedioxime has attached thereto a substituent of formula (Y)m-A-NHR)k can function as a substrate for the fibrin-stabilizing Factor XIIIa. The complex is useful for the diagnosis or therapy of thrombosis, embolism, atherosclerosis, inflammation or cancer.Type: GrantFiled: August 22, 2003Date of Patent: May 24, 2005Assignee: GE Healthcare LimitedInventors: Alan Michael Forster, Peter Knox, Marivi Mendizabal, Timothy Charles Richardson, Anthony Eamon Storey, Ian Andrew Wilson, Susan Champion, Alex Gibson, Benedicte Guilbert
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Patent number: 6875764Abstract: The present invention relates to novel compounds, pharmaceutical compositions containing the same as well as a method for treatment of parasitic disorders, wherein said compounds are administered. The present compounds are especially well suited for treatment of coccidiosis, particularly in poultry, and they have general formula (I): where Y is S or O and R is as defined in the specification.Type: GrantFiled: October 27, 2000Date of Patent: April 5, 2005Assignee: New Pharma Research Sweden ABInventors: Sabrina Muzi, Shoaá Abdul Rahman
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Patent number: 6838472Abstract: The current invention provide novel compounds, methods of treating or preventing emphysema, cancer and dermatological disorders, pharmaceutical compositions suitable for the treatment or prevention of emphysema, cancer and dermatological disorders and methods for delivering formulations into the lung of a mammal suffering from emphysema, cancer and dermatological disorders.Type: GrantFiled: September 17, 2002Date of Patent: January 4, 2005Assignee: Syntex (U.S.A.) LLCInventors: Michael Klaus, Jean-Marc Lapierre
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Publication number: 20040259885Abstract: Compounds having the formula 1Type: ApplicationFiled: August 13, 2003Publication date: December 23, 2004Inventors: Gaoquan Li, Qun Li, Tongmei Li, Nan-Horng Lin, Robert A. Mantei, Hing L. Sham, Gary T. Wang
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Publication number: 20040220408Abstract: Compounds according to formula (I) 1Type: ApplicationFiled: December 16, 2003Publication date: November 4, 2004Inventor: Fredrik Bjorkling
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Patent number: 6803486Abstract: Peptidomimetic compositions for selective inhibition of neuronal nitric oxide synthase.Type: GrantFiled: June 24, 2002Date of Patent: October 12, 2004Assignee: Northwestern UniversityInventors: Richard B. Silverman, Jung-Mi Hah, Jose Antonio Gomez Vidal
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Publication number: 20040192717Abstract: 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.Type: ApplicationFiled: April 8, 2004Publication date: September 30, 2004Inventor: Eberhard Amtmann
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Publication number: 20040152715Abstract: This invention provides a compound of the formula (I): 1Type: ApplicationFiled: December 16, 2003Publication date: August 5, 2004Inventors: Makoto Kawai, Hiroshi Nakamura, Hiroshia Shimokawa
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Publication number: 20040127477Abstract: The present invention relates to a class of compounds represented by the Formula I 1Type: ApplicationFiled: November 20, 2003Publication date: July 1, 2004Applicant: G. D. Searle & Co.Inventors: Nizal Samuel Chandrakumar, Bipinchandra Nanubhai Desai, Balekudru Devadas, Alan Frank Gasiecki, Renee Huff, Ish K. Khanna, James W. Malecha, Julie M. Miyashiro, Shashidhar N. Rao, Joseph Gerace Rico, Thomas Edward Rogers, Peter Gerrard Ruminski, Mark Andrew Russell, Yi Yu
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Publication number: 20040122017Abstract: The present invention discloses compounds which, are novel antagonists for melanin-concentrating hormone (MCH), as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising such MCH antagonists as well as methods of using them to treat obesity, metabolic disorders, eating disorders such as hyperphagia, and diabetes.Type: ApplicationFiled: December 3, 2002Publication date: June 24, 2004Applicant: Schering CorporationInventors: John W. Clader, Anandan Palani, Ruo Xu, Mark D. McBriar, Jing Su, Haiqun Tang
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Publication number: 20040106795Abstract: PDF inhibitors and novel methods for their use are provided.Type: ApplicationFiled: September 29, 2003Publication date: June 3, 2004Inventors: Ajita Bhat, Siegfried B. Christensen IV, James S. Frazee, Martha S. Head, Jack D. Leber, Mei Li
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Publication number: 20040102636Abstract: This invention relates to the use of a group of aryl ureas in treating cytokine mediated diseases and proteolytic enzyme mediated diseases, and pharmaceutical compositions for use in such therapy.Type: ApplicationFiled: February 1, 2002Publication date: May 27, 2004Applicant: BAYER CORPORATIONInventors: Scott Miller, Martin Osterhout, Jacques Dumas, Uday Khire, Timothy B. Lowinger, William J. Scott, Roger A. Smith, Jill E. Wood, David E. Gunn, Holia Hatoum-Mokdad, Marell Rodriguez, Robert Sibley, Ming Wang, Tiffany Turner, Catherine Brennan
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Publication number: 20040082550Abstract: Tropolone derivatives represented by the formula (I), which have retinoid actions and are useful as active ingredients of medicaments [R1 to R4 represent hydrogen atom, an alkyl group, or an alkoxyl group; the ring represented by Ar represents an aryl ring or a heteroaryl ring; X represents a single bond, —N═N—, —CON(R5)—, —(C═C)nCON(R6)—, —N(R7)CON(R8)—, —SO2N(R9)—, —N(R10)— (R5 to R9 represent hydrogen atom or an alkyl group, n represents 1 to 3, R10 represents hydrogen atom, an alkyl group, or an acyl group), an alkylene group, an aryldiyl group, or a heterocyclic diyl group; Y represents hydrogen atom, —OR11 (R11 represents hydrogen atom, an alkyl group, or an acyl group), —NHR12 (R12 represents hydrogen atom, an alkyl group, an acyl group, or amino group), or a halogen atom.Type: ApplicationFiled: December 16, 2003Publication date: April 29, 2004Inventor: Hiroyuki Kagechika
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Patent number: 6727265Abstract: The invention provides compounds which inhibit reverse transcriptase (RT) and which inhibit replication of a retrovirus, such as human immunodeficiency virus-1 (HIV-1). The compound of the invention are phenoxyethyl-thiourea-pyridines. The invention additionally provides a method for inhibiting reverse transcriptase activity of a retrovirus, such as HIV-1, comprising contacting the retrovirus with a compound of the invention. The invention additionally provides a method for inhibiting replication of a retrovirus, such as HIV-1, comprising contacting the retrovirus with a compound of the invention.Type: GrantFiled: April 15, 2003Date of Patent: April 27, 2004Assignee: Parker Hughes InstituteInventors: Fatih M. Uckun, Taracad K. Venkatachalam
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Publication number: 20040063765Abstract: The present invention relates to the use of compounds of the general Formula (I): 1Type: ApplicationFiled: May 6, 2003Publication date: April 1, 2004Applicant: 4 SC AGInventors: Aldo Ammendola, Katharina Aulinger-Fuchs, Astrid Gotschlich, Bernd Kramer, Martin Lang, Wael Saeb, Udo Sinks, Andreas Wuzik
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Patent number: 6699994Abstract: Compounds of formula (I) are useful as inhibitors of trypsin like serine protease enzymes such as thrombin, factor VIIa, factor Xa, TF/FVIIa, and trypsin. These compounds could be useful to treat and/or prevent clotting disorders, and as anticoagulating agents.Type: GrantFiled: April 23, 2002Date of Patent: March 2, 2004Assignee: BioCryst Pharmaceuticals, Inc.Inventors: Yarlagadda S. Babu, R. Scott Rowland, Pooran Chand, Pravin L. Kotian, Yahya El-Kattan, Shri Niwas
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Publication number: 20040034027Abstract: Compounds of formula I, 1Type: ApplicationFiled: August 6, 2003Publication date: February 19, 2004Applicant: Aventis Pharma Deutschland GmbHInventors: Manfred Schudok, Otmar Klingler, Hans-Peter Nestler, Hans Matter, Herman Schreuder
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Publication number: 20040034038Abstract: Compounds having the formula 1Type: ApplicationFiled: August 13, 2002Publication date: February 19, 2004Inventors: Goaquan Li, Qun Li, Tongmei Li, Nan-Horng Lin, Robert A. Mantei, Hing L. Sham, Gary T. Wang
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Patent number: 6693122Abstract: The present invention describes novel nitrosated and/or nitrosylated potassium channel activators, and novel compositions comprising at least one nitrosated and/or nitrosylated potassium channel activator, and, optionally, at least one compound that donates, transfers or releases nitric oxide, elevates endogenous levels of endothelium-derived relaxing factor, stimulates endogenous synthesis of nitric oxide or is a substrate for nitric oxide synthase and/or at least one vasoactive agent. The present invention also provides novel compositions comprising at least one potassium channel activator, and at least one compound that donates, transfers or releases nitric oxide, elevates endogenous levels of endothelium-derived relaxing factor, stimulates endogenous synthesis of nitric oxide or is a substrate for nitric oxide synthase and/or at least one vasoactive agent.Type: GrantFiled: May 28, 2002Date of Patent: February 17, 2004Assignee: NitroMed, Inc.Inventors: David S. Garvey, Inigo Saenz de Tejada
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Patent number: 6677353Abstract: The invention relates to substituted polycyclic aryl and heteroaryl tertiary-heteroalkylamine compounds useful as inhibitors of cholesteryl ester transfer protein (CETP; plasma lipid transfer protein-I) and compounds, compositions and methods for treating atherosclerosis and other coronary artery diseases. Preferred tertiary-heteroalkylamine compounds are substituted N-phenyl-N-heteroaralkyl aminoalcohols.Type: GrantFiled: May 23, 2002Date of Patent: January 13, 2004Assignee: Pharmacia CorporationInventors: James A. Sikorski, Richard C. Durley, Deborah A. Mischke, Emily J. Reinhard, Yvette M. Fobian, Michael B. Tollefson, Lijuan Wang, Margaret L. Grapperhaus, Brian S. Hickory, Mark A. Massa, Monica B. Norton, William F. Vernier, Barry L. Parnas, Michele A. Promo, Ashton T. Hamme, Dale P. Spangler, Melvin L. Rueppel
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Publication number: 20030224940Abstract: The invention relates to novel pesticidally active &agr;-sulfin and &agr;-sulfonamino acid amides of the general formula (I) including the optical isomers thereof and mixtures of such isomers, wherein n is a number zero or one; R1, R2, R3, R4, R5, R6 and R7 have the meanings given in the specification, and R8 is either hydrogen, (a), (b), (c), (d) or (e) wherein R11, R12, R13, R15 and R17 are each independently hydrogen or C1-C4 alkyl, R13 is C4-C12 alkyl, C1-C12 halogenalkyl; C3-C8 cycloalkyl; optionally substituted aryl or optionally substituted heteroaryl, R16 is optionally substituted aryl or optionally substituted heteroaryl; and Z is oxygen, sulfur —CR18R19— or —NR2O—, wherein R18, R19 and R20 independently of each other are hydrogen or C1-C4 alkyl. The novel compounds possess plant-protecting properties and are suitable for protecting plants against infestation by phytopathogenic microorganisms.Type: ApplicationFiled: May 6, 2003Publication date: December 4, 2003Inventors: Martin Zeller, Clemens Lamberth, Henry Szczepanski, Alain De Mesmaeker
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Patent number: 6653299Abstract: A complex of a radiometal or paramagnetic metal ion with a metal chelating agent such as a diaminedioxime has attached thereto a substituent of formula —(Y)m—A—NHR, can function as a substrate for the fibrin-stabilizing Factor XIIIa. The complex is useful for the diagnosis or therapy of thrombosis, embolism, atherosclerosis, inflammation or cancer.Type: GrantFiled: October 4, 1999Date of Patent: November 25, 2003Assignee: Nycomed Amersham PLCInventors: Alan Michael Forster, Peter Knox, Marivi Mendizabal, Timothy Charles Richardson, Anthony Eamon Storey, Ian Andrew Wilson, Susan Champion, Alex Gibson, Benedicte Guilbert
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Patent number: 6649613Abstract: Diacylhydrazine derivatives of general formula (I) wherein X, Y, Z, R1, 2 and R3 are as defined herein, and their physiologically acceptable salts or solvates thereof, are integrin inhibitors and can be used to combat thromboses, myocardial infarcts, coronary cardiac diseases, arteriosclerosis, inflammations, tumors, osteoporosis, infections, and restenosis following angioplasty or during pathological processes that are maintained or propagated by angiogenesis.Type: GrantFiled: January 14, 2002Date of Patent: November 18, 2003Assignee: Merck Patent GmbHInventors: Günter Hölzemann, Simon Goodman, Horst Kessler, Christoph Gibson, Gabór Sulyok
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Patent number: 6646129Abstract: The present invention relates to hitherto unknown compounds of formula (I) or their tautomeric forms, the attachment to the pyridine ring being in the 3- or 4-position, in which formula R stands for one or more substituents which can be the same or different and are selected from the group consisting of: hydrogen, halogen, trifluoromethyl, carboxy, C1-C4 alkyl, alkoxy or alkoxycarbonyl, nitro, amino or cyano and Q stands for C5-C14 divalent hydrocarbon radical which can be straight, branched, cyclic, saturated or unsaturated and X stands for carboxy, C1-C4 alkoxycarbonyl, di(C1-C4 alkoxy)-phosphinoyloxy, amino, C1-C4 alkoxycarbonylamino or tetrahydropyranyloxy; and pharmaceutically acceptable, non-toxic salts and N-oxides thereof. The present compounds are of value in the human and veterinary practice.Type: GrantFiled: February 4, 2002Date of Patent: November 11, 2003Assignee: Leo Pharmaceutical Products Ltd. A/SInventors: Charlotte Schou Hunneche, Erik Rytter Ottosen
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Patent number: 6645968Abstract: Compounds of formula I: are useful in treating diseases prevented by or ameliorated with potassium channel openers. Also disclosed are potassium channel opening compositions and a method of opening potassium channels in a mammal.Type: GrantFiled: February 5, 2001Date of Patent: November 11, 2003Assignee: Abbott LaboratoriesInventors: Robert J. Altenbach, Hao Bai, Jorge D. Brioni, William A. Carroll, Murali Gopalakrishnan, Robert J. Gregg, Mark W. Holladay, Peggy P. Huang, John F. Kincaid, Michael E. Kort, Philip R. Kym, John K. Lynch, Arturo Perez-Medrano, Henry Q. Zhang