Ring Nitrogen Is Shared By The Cyclos Of The Bicyclo Ring System (e.g., Tetramisole, Etc.) Patents (Class 514/368)
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Publication number: 20100076036Abstract: The present invention relates to heterocyclyl-substituted sulfonamides with 5-HT6 receptor affinity, and compositions thereof, and the use of said compounds for the treatment or prophylaxis of various disorders.Type: ApplicationFiled: January 30, 2008Publication date: March 25, 2010Applicant: LABORATORIOS DEL DR. ESTEVE, S.A.Inventor: Jose-Luis Diaz-Fernandez
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Publication number: 20100069378Abstract: The present invention refers to new indanyl sulphonamide compounds with general formula (I), as well as to their preparation procedure, their application as medicine and the pharmaceuticals composition which they are made up of. The new compounds of formula (I) show affinity for 5-HT6 receptors and are, therefore, effective for treating diseases mediated by these receptors.Type: ApplicationFiled: July 25, 2007Publication date: March 18, 2010Applicant: LABORATORIOS DEL DR. ESTEVE, S.A.Inventors: Jordi Frigola-Constansa, Joerg Holenz, Ramon Merce-Vidal, Maria de las Ermitas Alcalde-Pais, Maria de les Neus Mesquida-Estevez, Sara Lopez-Perez
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Patent number: 7671078Abstract: The invention relates to isothiourea derivatives of formula I: wherein R1 is a residue of one of the following structures: where the variables are as defined in the claims of the invention, as well as processes for production of these compounds.Type: GrantFiled: February 25, 2005Date of Patent: March 2, 2010Assignee: Novartis AGInventors: Fraser Glickman, Markus Streiff, Gebhard Thoma, Hans-Günter Zerwes
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Publication number: 20100048555Abstract: Compounds of formula (I): are inhibitors of MARK, and hence useful for treatment of disorders involving 10 hyperphosphorylation of tau.Type: ApplicationFiled: July 20, 2007Publication date: February 25, 2010Inventors: Ian Churcher, Victoria Alexandra Doughty, Peter Hunt, Matthew Stanton
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Publication number: 20100048577Abstract: The invention relates to the discovery that resveratrol, and substituted forms of resveratrol, are effective in alleviating benign prostate hyperplasia. Formulations containing the resveratrol or resveratrol derivative, lack omega-3 fatty acids, and also contain no other compounds which activate SIRT1 and PGC?.Type: ApplicationFiled: August 21, 2009Publication date: February 25, 2010Inventors: Joerg R. Leheste, German Torres
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Patent number: 7662841Abstract: The present invention relates to compounds of formula (I) and a process for producing the same. In formula (I), X represents a halogen atom, and R1 represents group —COR2 wherein R2 represents group OM or C1-12 alkyloxy wherein M represents a hydrogen atom, an alkali metal, an alkaline earth metal, or quaternary ammonium. The use of this compound as a synthetic intermediate can realize the production of carbapenem derivatives having potent antimicrobial activity in an efficient and safe manner at low cost.Type: GrantFiled: January 19, 2006Date of Patent: February 16, 2010Assignees: Meiji Seika Kaisha, Ltd., Sagami Chemical Research CenterInventors: Eiki Shitara, Kunio Atsumi, Keiichi Ajito, Shinya Ikeda, Tadashi Katoh, Munenori Inoue, Mari Nakatani
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Publication number: 20100004159Abstract: The present invention relates to polysubstituted imidazolone derivatives, to the pharmaceutical compositions comprising them and to the therapeutic uses thereof in the human and animal health fields. The present invention also relates to a process for preparing these derivatives.Type: ApplicationFiled: July 24, 2007Publication date: January 7, 2010Applicant: GENFITInventors: Edith Bouey, Christophe Masson, Karine Bertrand
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Publication number: 20100004299Abstract: The present invention relates to derivatives of imidazo[2,1-b]thiazoles of formula I, in which R, R1 to R3 and n have the meanings indicated in the claims, which modulate the transcription of endothelial nitric oxide (NO) synthase and are valuable pharmacologically active compounds. Specifically, the compounds of formula I upregulate the expression of the enzyme endothelial NO synthase and can be applied in conditions in which an increased expression of said enzyme or an increased NO level or the normalization of a decreased NO level is desired.Type: ApplicationFiled: May 15, 2009Publication date: January 7, 2010Applicant: SANOFI-AVENTISInventors: Gerhard ZOLLER, Hartmut STROBEL, David William WILL, Paulus WOHLFART
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Publication number: 20090318391Abstract: The present invention relates to the treatment of a mammal with a pharmaceutical composition comprising an H2-blocker, at least one anti-inflammatory agent, a cytotoxic agent and, optionally, levamisole, a retinoid, an NFkB inhibitor, a redox quinone, an agent that enhances the intracellular accumulation of NADH+H+, a poly-alcohol, an inhibitor of pro-angiogenic growth factor(s) and an MMP inhibitor, such pharmaceutical composition allowing for the enhanced therapy and/or prevention of neoplastic diseases and disorders.Type: ApplicationFiled: July 4, 2007Publication date: December 24, 2009Applicant: TILTAN PHARMA LTD.Inventor: Shmuel A. Ben-Sasson
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Publication number: 20090312310Abstract: There is provided a novel compound that inhibits interaction between murine double minute 2 (Mdm2) protein and p53 protein and exhibits anti-tumor activity. The present invention provides an imidazothiazole derivative represented by the following formula (1) having various substituents that inhibits interaction between Mdm2 protein and p53 protein and exhibits anti-tumor activity: wherein R1, R2, R3, R4, and R5 in the formula (1) each has the same meaning as defined in the specification.Type: ApplicationFiled: June 11, 2009Publication date: December 17, 2009Inventors: Haruko Kawato, Masaki Miyazaki, Yuuichi Sugimoto, Hiroyuki Naito, Tooru Okayama, Tsunehiko Soga, Kouichi Uoto
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Publication number: 20090291948Abstract: Acyl sulfonamide, peri-substituted, fused bicyclic ring compounds useful for the treatment or prophylaxis of a prostaglandin-mediated disease or condition are disclosed.Type: ApplicationFiled: August 3, 2009Publication date: November 26, 2009Applicant: DECODE GENETICS EHFInventors: Jasbir Singh, Mark E. Gurney, Georgeta Hategan, Peng Yu, David Zembower, Nian Zhou
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Publication number: 20090264457Abstract: The present invention relates to a Combination of at least two 5HT6-Ligands of which one is a partial or agonist while the other is a full antagonist or an inverse agonist, a medicament comprising this comination, the use of the combiantion in the manufacture of a medicament for the treatment of memory disorders ADHD, and methods of treatment using the combination or its members.Type: ApplicationFiled: August 1, 2008Publication date: October 22, 2009Inventors: Xavier Codony-Soler, Jose-Miguel Vela-Hernandez, Helmut H. Buschmann
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Publication number: 20090252716Abstract: An in vitro method is provided for identifying nuclear receptors abnormally expressed by brain tumor stem cells and a corresponding ligand which, if administered to brain tumor stem cells (BTSC's), is capable of inhibiting cell proliferation. Once the nuclear receptor/ligand combination has been identified, it can be utilized in vitro and in vivo to inhibit the proliferation and survival of the cancerous stem cells and ultimately affect proliferation and survival of tumors. The method can be utilized alone or in combination with other treatment methods. The method can also be utilized with regard to other forms of cancer which have cancerous stem cells associated therewith and which abnormally express one or more nuclear receptors.Type: ApplicationFiled: April 3, 2009Publication date: October 8, 2009Applicant: Clarian Health Partners, Inc. d/b/a Methodist Research InstituteInventor: John J. Bright
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Publication number: 20090221645Abstract: Compounds of formula (I) or pharmaceutically acceptable salts thereof, exhibit 5-HT1A agonism in addition to noradrenaline reuptake inhibition and optionally also 5-HT reuptake inhibition are useful for the treatment of obesity.Type: ApplicationFiled: February 8, 2006Publication date: September 3, 2009Inventors: Oscar Barba, Graham John Dawson, Thomas Martin Krulle, Robert John Rowley, Donald Smyth, Gerard Hugh Thomas
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Patent number: 7563901Abstract: The present invention relates to compounds represented by formula (1) and a process for producing the same. The use of these compounds can realize the production of carbapenem derivatives having potent antimicrobial activity and a wide antimicrobial spectrum in a safe and cost-effective manner.Type: GrantFiled: February 15, 2008Date of Patent: July 21, 2009Assignee: Meiji Seika Kaisha, Ltd.Inventors: Toshiro Sasaki, Takashi Ando, Yasuo Yamamoto, Takahiro Imai, Dai Kubota, Katsuhiko Noguchi, Nobuyuki Hori, Eiki Shitara, Kunio Atsumi, Shohei Yasuda
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Publication number: 20090163547Abstract: The present invention makes reference to new indene derivatives with general formula (I), as well as to their preparation procedures, their application as medicament and the pharmaceutical compositions containing them. The new compounds of formula (I) show affinity for 5-HT6 receptors and are, therefore, effective for treating diseases mediated by these receptors.Type: ApplicationFiled: November 7, 2006Publication date: June 25, 2009Inventors: Maria De Las Ermitas Alcalde-Pais, Jordi Frigola-Constansa, Joerg Holenz, Ramon Merce-Vidal, Maria De Les Neus Mesquida-Estevez, Sara Lopez-Perez
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Publication number: 20090142347Abstract: This invention relates generally to the field of mineralization, and specifically to the role of TNAP in regulating the levels of extracellular inorganic pyrophosphate. The invention provides methods for modulating the activity of TNAP activity; methods for screening for modulators of TNAP activity; modulators of TNAP activity; and methods for treating pathologic conditions known of suspected to be affected by modulation of TNAP activity.Type: ApplicationFiled: September 29, 2005Publication date: June 4, 2009Applicant: THE BURNHAM INSTITUTE FOR MEDICAL RESEARCHInventor: José Luis Millan
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Publication number: 20090136448Abstract: Anti-viral agents of compounds of Formula (I): wherein A, R1, R2 and R3 are as defined in the specification, processes for their preparation and their use in HCV treatment are provided.Type: ApplicationFiled: December 20, 2006Publication date: May 28, 2009Inventors: John Andrew Corfield, Richard Martin Grimes, David Harrison, Charles David Hartley, Peter David Howes, Joelle Le, Malcolm Lees Meeson, Jacqueline Elizabeth Mordaunt, Pritom Shah, Martin John Slater, Gemma Victoria White
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Publication number: 20090111788Abstract: Novel modified release pharmaceutical compositions wherein the composition comprises at least one antibiotic(s) preferably amoxicillin or its pharmaceutically acceptable salts, esters, polymorphs, isomers, prodrugs, solvates, hydrates, or derivatives thereof either alone or in combination with other antibiotic(s) as active ingredient, with at least one release modifying agent(s) for controlling the release of the beta lactam antibiotic optionally with one or more other pharmaceutically acceptable excipient(s) is provided, wherein the dosage form provides a release of not more than about 60% of the antibiotic in about 30 minutes and not less than about 70% of the antibiotic after 8 hours when subjected to in vitro dissolution study or when tested in vivo. Further, the compositions of the present invention which when tested in a group of healthy humans provide a mean peak plasma concentration (Cmax) after at least about 0.5 hour of administration of the dosage form.Type: ApplicationFiled: March 7, 2007Publication date: April 30, 2009Inventors: Rajesh Jain, Kour Chand Jindal, Munish Talwar
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Patent number: 7514458Abstract: Disclosed compounds of formula (I) which inhibit production of cytokines involved in inflammatory processes and are thus useful for treating diseases and pathological conditions involving inflammation such as chronic inflammatory disease. Also disclosed are processes for preparing these compounds and pharmaceutical compositions comprising these compounds.Type: GrantFiled: January 30, 2007Date of Patent: April 7, 2009Assignee: Boehringer Ingelheim Pharmaceuticals, Inc.Inventors: Derek Cogan, Ming-Hong Hao, Victor Marc Kamhi, Craig Andrew Miller, Matthew Russell Netherton, Alan David Swinamer
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Publication number: 20090075918Abstract: Veterinarian composition comprising an organic salt of levamisole in combination with at least one avermectine and/or milbemycine. A veterinarian formulation comprising of organics salts of levamisole, more specifically to the disophenolat salt of levamisole and the nitroxynil-salt of levamisole with avermectines and milbemycines and its use in treatment of helminthiasis in mammals, in particular in bovines, swines, caprines, equines, ovines, canines and felines.Type: ApplicationFiled: December 18, 2006Publication date: March 19, 2009Inventors: Dolivar Coracci Neto, Nelson Henriques Fernandes Filho, Ricardo da Silva Sercheli
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Patent number: 7498327Abstract: The present invention provides a compound of formula I and the use thereof for the therapeutic treatment of disorders relating to or affected by the 5-HT6 receptor.Type: GrantFiled: June 22, 2005Date of Patent: March 3, 2009Assignee: WyethInventors: Youchu Wang, Chia-Cheng Shaw, Ronald Charles Bernotas, Chung-Chiee Paul Wang, Ping Cai, Zhi Wang
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Publication number: 20090054463Abstract: The present invention relates generally to compounds represented in Formula I, pharmaceutical compositions comprising them and methods of treating of diseases or disorders related to the function of the calcium sensing receptor. The invention also relates to processes for making such compounds and to intermediates useful in these processes.Type: ApplicationFiled: July 10, 2008Publication date: February 26, 2009Inventors: Pierre Deprez, Christopher Fotsch, Paul Harrington, Sarah Lively, Kanaka Pattabiraman, David St. Jean, Taoues Temal-Laib
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Publication number: 20090048271Abstract: Novel compounds having a fused bicyclic heteroaromatic ring system substituted with a heteroaryl five-membered ring are disclosed. The compounds inhibit growth of a variety of types of cancer cells, and are thus useful for treating cancer. Efficacy of these compounds is demonstrated with a system for monitoring cell growth/migration, which shows they are potent inhibitors of growth and/or migration of cancer cells. In addition, compounds of the invention were shown to stop growth of tumors in vivo, and to reduce the size of tumors in vivo. Compositions comprising these compounds, and methods to use these compounds and compositions for treatment of cancers, are disclosed.Type: ApplicationFiled: July 17, 2008Publication date: February 19, 2009Inventors: Haoyun An, Biao Xi, Yama Abassi, Xiaobo Wang, Xiao Xu
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Publication number: 20090011975Abstract: The invention provides a method of inhibiting cell death in a mammal. The method comprises administering to a mammal an effective amount of a composition comprising a cell protection factor covalently linked to a bone targeting agent via a linkage that is cleaved under physiological conditions, whereby the cell protection factor is released from the bone targeting agent in vivo to inhibit cell death. The invention further provides a compound comprising a cell protection factor covalently attached to a bone targeting agent via a linker that is cleaved under physiological conditions.Type: ApplicationFiled: July 31, 2008Publication date: January 8, 2009Applicant: Semafore Pharmaceuticals Inc.Inventors: Joseph R. Garlich, Donald L. Durden, Tim C. Smith
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Publication number: 20090005399Abstract: Substituted imidazo[2,1-b]thiazole compounds corresponding to formula I, a method for producing them, pharmaceutical compositions containing them, and the use thereof for regularing mGluR5 receptors, or for treating or inhibiting disorders or disease states at least partially mediated by mGluR5 receptor such as pain, anxiety attacks, drug or alcohol dependency, and others.Type: ApplicationFiled: September 9, 2008Publication date: January 1, 2009Applicant: Gruenenthal GmbHInventors: Sven KUEHNERT, Saskia ZEMOLKA, Michael HAURAND, Klaus SCHIENE
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Publication number: 20090005417Abstract: The present invention relates to substituted indazolyl sulfonamide and 2,3-dihydroindolyl sulfonamide compounds of general formula I, a process for their preparation, medicaments comprising said substituted indazolyl sulfonamide and 2,3-dihydro-indolyl sulfonamide compounds as well as the use of said substituted indazolyl sulfonamide and 2,3-dihydro-indolyl sulfonamide compounds for the preparation of medicaments, which are particularly suitable for the prophylaxis and/or treatment of disorders or diseases that are at least partially mediated via 5-HT6 receptors.Type: ApplicationFiled: December 29, 2005Publication date: January 1, 2009Applicant: LABORATORIOS DEL DR. ESTEVE S.A.Inventors: Ramon Merce Vidal, Xavier Codony-Soler, Alberto Dordal-Zueras
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Publication number: 20080293645Abstract: This invention relates an antiparasitic combination for conveniently treating multiple types of parasites in domestic animals. Specifically, this invention provides a convenient combination and a method for removing worms from a gastrointestinal tract of a domestic animal while also preventing heartworm. The antiparasitic combination for the treatment of domestic animals may include an effective amount of praziquantel, an effective amount of pyrantel pamoate, an effective amount of febantel, and an effective amount of ivermectin. Typical worms removed may include tapeworms, hookworms, whipworms and ascarids.Type: ApplicationFiled: May 25, 2007Publication date: November 27, 2008Inventor: Lawrence F. Schneider
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Publication number: 20080287511Abstract: The present invention relates to the novel anthelmintic compound tetrahydro-furan-2-carboxylic acid-[3-(2,3,5,6-tetrahydro-imidazo[2,1-b]thiazol-6-yl)-phenyl]-amide and the pharmaceutically acceptable acid addition salts and the stereochemically isomeric forms thereof, as well as pharmaceutical compositions comprising said novel compound, processes for preparing said compound and compositions, and the use thereof as a medicine, in particular in treatment, control and prevention of endo- and ectoparasite infections in warm-blooded animals.Type: ApplicationFiled: January 26, 2006Publication date: November 20, 2008Inventors: Jan Heeres, Paulus Joannes Lewi, Paul Adriaan Jan Janssen, Kathleen Marie Jeanne Alice Vlaminck, Pierre Josef Hektor Valere Ottevaere, Oscar Franz Joseph Vanparijs, Frank Xavier Jozef Herwig Arts
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Publication number: 20080255062Abstract: A method for rapidly screening small molecules to identify small molecules that stimulate axon regeneration and outgrowth from adult sensory neurons. The method generally comprises preparing a purified individualized dorsal root ganglia cell suspension (DRG), coating well surfaces of a suitably prepared multi-well microplate with the DRG, then dispensing dosages of selected small molecules into selected wells. The microplates are incubated under sterile conditions at about 37° C. for at least 24 hours. The DRG suspension in each well is then morphometrically assessed to assess the extent of axon regeneration and outgrowth that occurred, and the effects of the selected small molecules are determined by comparison to control treatments. The method is suitable for screening chemically derived small molecules and biologically derived small molecules.Type: ApplicationFiled: February 13, 2008Publication date: October 16, 2008Applicant: UNIVERSITY OF MANITOBAInventor: Paul FERNYHOUGH
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Publication number: 20080249103Abstract: Provided herein are methods for diagnosis and prognosis using polymorphic variants of sirtuins. Such polymorphic may be used, for example, to identify subjects that would be responsive to treatment with a sirtuin modulating compound and/or subjects that are suffering from or susceptible to a disease mediated by a sirtuin. Also provided are methods for determining the predictive value of a sirtuin polymorphic variant, methods for evaluating sirtuin modulating compounds, and methods for determining appropriate dosage and/or treatment regimens for subjects having one or more sirtuin polymorphic variants. Screening methods for identifying sirtuin modulating compounds using polymorphic variants of a sirtuin are also provided.Type: ApplicationFiled: October 30, 2007Publication date: October 9, 2008Applicant: Sirtris Pharmaceuticals, Inc.Inventors: Markku Laakso, Teemu Kuulasmaa, Johan Auwerx, Christoph Westphal, Peter Elliott, Karl D. Normington, Olivier Boss, Andre Iffland, Siva Lavu
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Publication number: 20080249146Abstract: The present invention relates to compounds of the formula (I), wherein R1, R2, A, B, D, E, F, G and Ar are as defined herein, and pharmaceutically acceptable salts thereof, useful in the prevention and treatment of hepatitis C infections.Type: ApplicationFiled: July 14, 2005Publication date: October 9, 2008Inventors: Immacolata Conte, Jose Ignacio Martin Hernando, Savina Malancona, Jesus Maria Ontoria Ontoria, Ian Stansfield
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Patent number: 7419993Abstract: The invention relates to triazolo-thiazole analogues of epothilone A and epothilone B.Type: GrantFiled: February 9, 2005Date of Patent: September 2, 2008Assignee: Helmholtz Center of Infection Research GmbHInventors: Gerhard Hoefle, Nicole Glaser
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Publication number: 20080161341Abstract: The present invention is directed to novel compounds of formula (I) wherein the variables are as defined herein. The compounds of formula (I) are useful as kinase inhibitors and as such would be useful in treating certain conditions and diseases, especially inflammatory conditions and diseases and proliferative disorders and conditions, for example, cancers.Type: ApplicationFiled: October 5, 2007Publication date: July 3, 2008Inventors: David J. Calderwood, Kristine E. Frank, David W. Borhani, Heather M. Davis, Nathan S. Josephsohn, Barbara S. Skinner
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Patent number: 7351732Abstract: New cycloalkanedione derivatives that are serotonin (5-hydroxytriptamine, 5-HT) 5-HT1A receptor subtype agonists and, consequently, they are useful in the treatment of pathological states for which an agonist of these receptors is indicated. They are particularly useful as neuroprotective agents, of special interest in the treatment and prophylaxis of cerebral damage produced by traumatic or ischemic stroke.Type: GrantFiled: July 29, 2003Date of Patent: April 1, 2008Assignee: Schwarz Pharma S.L.Inventors: Joaquin Del Río Zambrana, Diana Frechilla Manso, M. Luz López Rodríguez, Bellinda Benhamú Salama, José Ángel Fuentes Cubero, Mercedes Delgado Wallace
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Patent number: 7345069Abstract: The present invention relates to TG-25 and/or analogs thereof and their use of TG-25 in the treatment of cancer. TG-25 inhibits the growth of prostate cells by inhibiting DNA synthesis, more particularly by DNA cleavage.Type: GrantFiled: April 1, 2005Date of Patent: March 18, 2008Assignee: Wisconsin Alumni Research FoundationInventor: Ben Shen
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Patent number: 7288559Abstract: The present invention is directed to compounds that are antagonists of CGRP receptors and that are useful in the treatment or prevention of diseases in which the CGRP is involved, such as headache, migraine and cluster headache. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which CGRP is involved.Type: GrantFiled: March 10, 2004Date of Patent: October 30, 2007Assignee: Merck + Co, Inc.Inventors: Ian M. Bell, Steven N. Gallicchio, Craig A. Stump, C. Blair Zartman
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Patent number: 7230021Abstract: The present invention provides a compound of Formula I, all of its related stereoisomers, and their pharmaceutically acceptable salts, wherein A—B, K, Q, X, Y, Z, R and R1 are as defined in Claim 1.Type: GrantFiled: March 13, 2003Date of Patent: June 12, 2007Assignee: The Texas A&M University SystemInventors: Daniel Romo, Jun Liu, Nam Song Choi, Zonggao Shi
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Patent number: 7220756Abstract: The present invention provides a compound of formula I and the use thereof for the therapeutic treatment of a CNS disorder relating to or affected by the 5-HT6 receptorType: GrantFiled: February 1, 2006Date of Patent: May 22, 2007Assignee: WyethInventor: Derek Cecil Cole
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Patent number: 7214802Abstract: Disclosed compounds of formula (I) which inhibit production of cytokines involved in inflammatory processes and are thus useful for treating diseases and pathological conditions involving inflammation such as chronic inflammatory disease. Also disclosed are processes for preparing these compounds and pharmaceutical compositions comprising these compounds.Type: GrantFiled: March 7, 2005Date of Patent: May 8, 2007Assignee: Boehringer Ingelheim Pharmaceuticals, Inc.Inventors: Derek Cogan, Ming-Hong Hao, Victor Marc Kamhi, Craig Andrew Miller, Matthew Russell Netherton, Alan David Swinamer
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Patent number: 7153873Abstract: Salts of a bicyclic, N-acylated imidazo-3-amine or an imidazo-5-amine of the formula: addition products thereof with acids, and methods for preparing the salts and addition products. Also disclosed are pharmaceutical compositions comprising the same and methods using the pharmaceutical compositions for the treatment or prophylaxis of pain, drug or alcohol abuse, diarrhoea, gastritis, ulcers, urinary incontinence, depression, narcolepsy, overweight, asthma, glaucoma, tinnitus, itching, hyperkinetic syndrome, epilepsy, or schizophrenia, for inducing anesthesia, and for anxiolysis.Type: GrantFiled: June 6, 2006Date of Patent: December 26, 2006Assignee: Gruenenthal GmbHInventors: Matthias Gerlach, Corinna Sundermann
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Patent number: 7125863Abstract: Compounds according to formula (1), wherein R1 is H or CN, X1 is S, O, SO2 or CH2, X2 is CO, CH2 or a covalent bond, Het is a nitrogen-containing heterocycle and n is 1–5 are new. The compounds of the invention are inhibitors of dipeptidyl peptidase IV.Type: GrantFiled: April 26, 2001Date of Patent: October 24, 2006Assignee: Ferring BVInventors: David Michael Evans, Gary Robert William Pitt
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Patent number: 7105550Abstract: This invention concerns the use of a compound of formula (I?) a N-oxide, pharmaceutically acceptable addition salt, quaternary amine and stereochemically isomeric form thereof, wherein Q is optionally substituted C3-6cycloalkyl, phenyl, naphthyl, pyridyl, pyrimidinyl, pyrazinyl, pyridazinyl, benzthiazolyl, benzoxazolyl, benzimidazolyl, indazolyl, or imidazopyridyl; or Q is a radical of formula wherein X and Y each independently are O, NR3, CH2 or S, with R3 being hydrogen or C1-4alkyl; q is 1 to 4; Z is O or NR4 with R4 being hydrogen or C1-4alkyl; r is 1 to 3; L is optionally substituted phenyl or L is Het with Het being an optionally substituted five- or six-membered heterocyclic ring or an optionally substituted bicyclic heterocyclic ring; for the manufacture of a medicament for the prevention or the treatment of diseases mediated through cytokines.Type: GrantFiled: February 20, 2001Date of Patent: September 12, 2006Inventors: Christopher Love, Jean Pierre Frans Van Wauwe, Marc De Brabander, Ludwig Cooymans, Nele Vandermaesen, Ludo Edmond Josephine Kennis
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Patent number: 7087626Abstract: Novel pyrrazole derivative compounds and their use as pharmaceutical agents, in particular their use as TGF-beta signal transduction inhibitors.Type: GrantFiled: May 13, 2002Date of Patent: August 8, 2006Assignee: Eli Lilly and CompanyInventors: Douglas Wade Beight, Todd Vincent DeCollo, Alexander Glenn Godfrey, Theodore Goodson, Jr., Hong-Yu Li, William Thomas McMillen, Shawn Christopher Miller, Jason Scott Sawyer, Edward C. R. Smith, Jonathan Michael Yingling
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Patent number: 7022701Abstract: The present invention provides a compound of formula I and the use thereof for the therapeutic treatment of disorders relating to or affected by the 5-HT6 receptor.Type: GrantFiled: April 20, 2004Date of Patent: April 4, 2006Assignee: WyethInventors: Derek Cecil Cole, Joseph Raymond Stock, William Joseph Lennox, Ping Zhou
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Patent number: 7012087Abstract: The therapeutic use of temporary p53 inhibitors in the treatment of p53-mediated diseases, conditions, and injuries is disclosed.Type: GrantFiled: June 13, 2001Date of Patent: March 14, 2006Assignee: The Board of Trustees of the University of IllinoisInventors: Andrei V. Gudkov, Pavel G. Komarov, Elena A. Komarova
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Patent number: 7008957Abstract: The invention relates to compounds of the formula I in which the radicals have the stated meanings, their stereoisomeric forms and their physiologically tolerated salts and process for their preparation. The compounds are suitable for the treatment of metabohlic disorders such as type 2 diabetes.Type: GrantFiled: July 26, 2004Date of Patent: March 7, 2006Assignee: Sanofi-Aventis Deutschland GmbHInventors: Holger Wagner, Karl Schoenafinger, Gerhard Jaehne, Holger Gaul, Christian Buning, Georg Tschank, Ulrich Werner
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Patent number: 6900160Abstract: The invention relates to triazolo-thiazole analogues of epothilone A and epothilone B.Type: GrantFiled: September 21, 2001Date of Patent: May 31, 2005Assignee: Gesellschaft fuer Biotechnologische Forschung mbHInventors: Gerhard Hoefle, Nicole Glaser
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Patent number: 6875765Abstract: The novel arylsulfonamide ether compounds, pharmaceutical compositions and uses thereof as inhibitors of interleukin-1? converting enzyme and other cysteine proteases in the ICE family are described. In one embodiment, the compound is described by the generalized structure: and pharmaceutically acceptable salts, esters, amides, and prodrugs thereof. In addition, methods of treating stroke, inflammatory diseases, septic shock, repurfusion injury, Alzheimer's disease, and shigellosis, using a compound of the invention or a pharmaceutical composition thereof, are described.Type: GrantFiled: May 10, 2002Date of Patent: April 5, 2005Assignee: Warner-Lambert CompanyInventors: James Knobelsdorf, Sheryl Hays, Charles J. Stankovic, Kimberly S. Para, Michael K. Connolly, Paul Galatsis, William Harter, Aurash B. Shahripour, Mark Stephen Plummer, Beth Lunney, Bernd Janssen, Jay Bradford Fell
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Patent number: 6838462Abstract: The present invention relates to novel heterocyclic compounds of formula (I) where A, R1, R2, Y, Z, and n are defined in the disclosure, to processes for their preparation, and to their use as crop protection agents, in particular for controlling animal pests.Type: GrantFiled: April 16, 2002Date of Patent: January 4, 2005Assignee: Bayer CropScience LPInventors: Peter Jeschke, Michael Beck, Wolfgang Krämer, Detlef Wollweber, Angelika Lubos-Erdelen, Andreas Turberg, Olaf Hansen, Hans-Dieter Martin, Piet Sauer, Christoph Erdelen