Nitrogen, Other Than As Nitro Or Nitroso, Attached Directly To The Carbocyclic Ring Of The Quinoline Ring System By Nonionic Bonding Patents (Class 546/171)
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Publication number: 20090143354Abstract: The invention provides compounds of formula (IA), processes for their preparation, pharmaceutical compositions containing them, and their use in therapy.Type: ApplicationFiled: May 2, 2008Publication date: June 4, 2009Inventors: Richard Evans, Christine Eyssade, Rhonan Ford, Barrie Martin, Toby Thompson, Paul Willis
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Publication number: 20090118295Abstract: The use of a compound of formula I wherein Y is a single bond, C?O, C?S or S(O)m, where m is 0, 1 or 2; the ring is a 6-membered aromatic or is a 5 or 6 membered heteroaromatic ring; Z and Z? are joined by a single or a double bond and are ?C— or —N— provided that both are not N; Ra, R1, R2, R3, R3a, R4 and R8 are specified organic groups; n is 2, 3 or 4 and p is 0-4; or salts or N-oxides thereof or compositions containing them in controlling insects, acarines, nematodes or molluscs. Novel compounds are also provided.Type: ApplicationFiled: December 6, 2006Publication date: May 7, 2009Applicant: SYNGENTA CROP PROTECTION, INCInventors: Jerome Cassayre, Peter Maienfisch, Fredrik Cederbaum, Louis-Pierre Molleyres
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Publication number: 20090105474Abstract: The anthranilic acid derivative or the salt thereof represented by the general formula wherein R1 and R2 are hydrogen atom, or the like; R3 is a phenyl, cycloalkyl or bicyclic heterocyclic group which may be substituted, or the like; R4 is a phenyl, cycloalkyl or pyridyl group which may be substituted, or the like; X1 is an alkylene or alkenylene group which may be substituted or a bond; X2 is the general formula -X3-X4- or -X4-X3-, wherein X3 is a sulfur atom, an imino group or a bond, or the like; X4 means an alkylene or alkenylene group which may be substituted or a bond; is useful for a remedy such as rheumatoid arthritis, osteoarthritis and carcinoma, because it shows MMP-13 production inhibitory effect.Type: ApplicationFiled: March 14, 2006Publication date: April 23, 2009Applicant: Toyama Chemical Co., Ltd.Inventors: Junichi Yokotani, Yoichi Taniguchi, Eiji Hara, Hitoshi Akitsu, Hidehiko Tanaka, Shuzo Anzai
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Publication number: 20090105300Abstract: The present invention relates to compounds of Formula I as shown below, wherein the definitions of A, X, Y, R1 R2, R3, R4, R5, R6, R7, R8, and R9 are provided in the specification. Compounds of Formula I are useful for the treatment of diseases associated with ?-secretase activity, including Alzheimer's disease.Type: ApplicationFiled: October 17, 2008Publication date: April 23, 2009Inventor: Chih Yung HO
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Publication number: 20090099231Abstract: The present invention provides pyrrolidinone derivatives as Factor Xa inhibitors and pharmaceutical compositions comprising the same. The invention also relates to processes for the preparation of such compounds, and the use of such compounds in medicine, particularly in the amelioration of a clinical condition for which a Factor Xa inhibitor is indicated.Type: ApplicationFiled: April 7, 2006Publication date: April 16, 2009Inventors: John David Harling, Nigel Stephen Watson, Robert John Young
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Publication number: 20090082395Abstract: Disclosed are amide, thioamide, urea and thiourea 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, and diabetic-related diseases.Type: ApplicationFiled: September 9, 2008Publication date: March 26, 2009Inventor: Richard D. Gless, JR.
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Publication number: 20090082308Abstract: The present invention relates to a novel class of benzothiophene amide derivatives. The hydroxamic acid compounds can be used to treat cancer. The benzothiophene amide compounds can also inhibit histone deacetylase and are suitable for use in selectively inducing terminal differentiation, and arresting cell growth and/or apoptosis of neoplastic cells, thereby inhibiting proliferation of such cells. Thus, the compounds of the present invention are useful in treating a patient having a tumor characterized by proliferation of neoplastic cells. The compounds of the invention may also be useful in the prevention and treatment of TRX-mediated diseases, such as autoimmune, allergic and inflammatory diseases, and in the prevention and/or treatment of diseases of the central nervous system (CNS), such as neurodegenerative diseases.Type: ApplicationFiled: April 14, 2006Publication date: March 26, 2009Inventors: Jed Lee Hubbs, Dawn M. Mampreian, Joey L. Methot, Thomas A. Miller, Karin M. Otte, Phieng Siliphaivanh, David L. Sloman, Matthew G. Stanton, Kevin J. Wilson, David J. Witter
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Publication number: 20090048295Abstract: Substituted 5,6,7,8-tetrahydroquinoline derivatives, which are C5a receptor modulators, compositions containing these derivatives, and methods of their use for the prevention and treatment of conditions, including, inter alia, immune and inflammatory diseases and conditions, are disclosed.Type: ApplicationFiled: August 12, 2008Publication date: February 19, 2009Inventors: Joseph Kent Barbay, Wei He, Yong Gong, Jian Li, Jean Van Wauwe, Mieke Buntinx
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Publication number: 20090023718Abstract: The present invention relates to a novel class of hydroxamic acid derivatives having a diamine or iminodiacetic acid backbone. The hydroxamic acid compounds can be used to treat cancer. The hydroxamic acid compounds can also inhibit histone deacetylase and are suitable for use in selectively including terminal differentiation, arresting cell growth and/or apoptosis of neo-plastic cells, thereby inhibiting proliferation of such cells. Thus, the compounds of the present are useful in treating a patient having a tumor characterized by proliferation of neoplastic cells. The compound of the invention are also useful in the prevention and treatment of TRX-mediated diseases, such as autoimmune, allergic and inflammatory diseases, and in the prevention and/or treatment of diseases of the central nervous system (CNS), such as neurodegenerative diseases.Type: ApplicationFiled: November 23, 2004Publication date: January 22, 2009Applicant: Aton Pharma, Inc.Inventors: Thomas A. Miller, David J. Witter, Sandro Belvedere
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Publication number: 20090018133Abstract: The invention provides compounds of formula (I), in which m, A, R1 and Ar have the meanings defined in the specification; processes for their preparation; pharmaceutical compositions containing them; a process for preparing the pharmaceutical compositions; and their use in therapy.Type: ApplicationFiled: February 29, 2008Publication date: January 15, 2009Inventors: Rhonan Ford, Frederic Leroux, Michael Stocks
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Publication number: 20080312237Abstract: Compounds are disclosed that have a formula represented by the following: The compounds may be prepared as pharmaceutical compositions, and may be used for the prevention and treatment of a variety of conditions in mammals including humans, including by way of non-limiting example, pain, inflammation, traumatic injury, and others.Type: ApplicationFiled: July 18, 2008Publication date: December 18, 2008Inventors: Michael G. Kelly, Satyanarayana Janagani, Ravindra B. Upasani
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Publication number: 20080312273Abstract: The invention relates to compounds of formula (I) wherein: either any one of G1, G2, G3, G4 and G5 is nitrogen and the other four are —CH— or G1, G2, G3, G4 and G5 are all —CH—; Z is —O—, —NH—, —S—, —CH2— or direct bond; Z is linked to any one of G1, G2, G3, and G4; n is an integer from 0 to 5; m is an integer from 0 to 3; Ra represents hydrogen or fluoro; Rb, R1 and R2 are defined herein and salt thereof, process for the preparation so such compounds, pharmaceutical compositions containing a compound of formula I or a pharmaceutically acceptable salt thereof as active ingredient and the use of a compound of formula I in the manufacture of a medicament for the production of an antiangiogenic and/or vascular permeability reducing effect in warm-blooded animals. The compounds of formula I and the pharmaceutically acceptable salts thereof inhibit the effects of VEGF, a property of value in the treatment of a number of diseases states including cancer and rheumatoid arthritis.Type: ApplicationFiled: November 29, 2007Publication date: December 18, 2008Inventor: Laurent Francois Andre Hennequin
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Publication number: 20080312270Abstract: Compounds, compositions and methods that are useful in the treatment of inflammatory and immune-related diseases and conditions are provided herein. In particular, the invention provides compounds which modulate the function and/or expression of proteins involved in atopic diseases, inflammatory conditions and cancer. The subject compounds are carboxylic acid derivatives.Type: ApplicationFiled: April 30, 2008Publication date: December 18, 2008Inventors: Matthew Brown, Michael G. Johnson, An-Rong Li, Jiwen Liu, Sarah E. Lively, Julio C. Medina, Wang Shen, Xuemei Wang, Yingcai Wang
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Publication number: 20080312278Abstract: Compounds of the formula I in which X, Y, R1, R1?, R2, R3 have the meanings indicated in claim 1, are inhibitors of cell proliferation and can be employed for the treatment of tumours.Type: ApplicationFiled: November 14, 2006Publication date: December 18, 2008Inventors: Oliver Schadt, Dieter Dorsch, Claus Fittschen, Matthias Grell
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Publication number: 20080300243Abstract: Compounds are disclosed that have a formula represented by the following: The compounds may be prepared as pharmaceutical compositions, and may be used for the prevention and treatment of a variety of conditions in mammals including humans, including by way of non-limiting example, pain, inflammation, traumatic injury, and others.Type: ApplicationFiled: February 24, 2006Publication date: December 4, 2008Inventors: Michael G. Kelly, John Kincaid, Matthew Duncton, Kiran Sahasrabudhe, Satyanarayana Janagani, Ravindra B. Upasani, Guoxian Wu, YunFeng Fang, Zhi-Liang Wei, Carl Kaub, Jianhua He
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Publication number: 20080293766Abstract: The present invention provides a method of inhibiting an androgen receptor by administering a compound of Formula I: or a compound of Formula II: wherein R1, R2, R3 and R8 are each independently hydrogen or C1-6 alkyl. R4 is absent or is hydrogen, C1-6 alkyl or C1-6 alkyl-OH. R5 is hydrogen, C1-6 alkyl or —NR6R7. R6 and R7 are each independently hydrogen or C1-6 alkyl, or are combined with the nitrogen to which they are attached to form a heterocycloalkyl having from 5 to 7 ring members. L is a linker of C1-6 alkylene, C2-6 alkenylene, C2-6 alkynylene or C3-6 cycloalkylene. The compounds of Formula I include the salts, hydrates and prodrugs thereof. Each R9 is H, C1-6 alkyl, —OH or —O—C1-6 alkyl. The compounds of Formulas I and II include the salts, hydrates and prodrugs thereof. By administering the compound of Formula I or II, the method inhibits the androgen receptor.Type: ApplicationFiled: April 11, 2008Publication date: November 27, 2008Applicant: REGENTS OF THE UNIVERSITY OF CALIFORNIAInventors: Marc Diamond, Jeremy Jones, Adam Renslo
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Publication number: 20080286607Abstract: It is an object of the present invention to provide a novel triazole derivative. Further, it is another object of the present invention to provide a light-emitting element having high luminous efficiency with the use of the novel triazole derivative. Moreover, it is still another object of the present invention to provide a light-emitting device and electronic devices which have low power consumption. A light-emitting element having high luminous efficiency can be manufactured with the use of a triazole derivative which is a 1,2,4-triazole derivative, in which an aryl group or a heteroaryl group is bonded to each of 3-position, 4-position, and 5-position, and in which any one of the aryl group or heteroaryl group has a 9H-carbazol-9-yl group.Type: ApplicationFiled: May 15, 2008Publication date: November 20, 2008Applicant: Semiconductor Energy Laboratory Co., Ltd.Inventors: Hiroko Nomura, Sachiko Kawakami, Nobuharu Ohsawa, Satoshi Seo
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Publication number: 20080281105Abstract: The present invention relates generally to the synthesis of novel quinolinium salts and derivative compounds. Such salts and compounds are useful for inhibiting the growth of cancer cells.Type: ApplicationFiled: January 18, 2006Publication date: November 13, 2008Applicant: IMMUSOL INCORPORATEDInventors: James E. Macdonald, Michelle K. Hysell, Dehua Yu, Henry Li, Flossie Wong-Staal
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Publication number: 20080255345Abstract: The invention relates to iRNA agents that preferably include a modification that targets CC chemokine receptor 5 (CCR5). The invention also relates to methods of making and using such modified iRNA agents.Type: ApplicationFiled: November 21, 2007Publication date: October 16, 2008Inventors: Muthiah Manoharan, Kallanthottahil G. Rajeev
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Publication number: 20080254318Abstract: The present invention provides a material having excellent hole injecting and hole transporting properties. Moreover, the present invention provides a light-emitting element and a light-emitting device using the material having excellent hole injecting and hole transporting properties. The present invention provides a carbazole derivative represented by the general formula (1). By applying the carbazole derivative of the present invention to a light-emitting element or a light-emitting device, a lower driving voltage, enhanced emission efficiency, a longer lifetime and enhanced reliability of the light-emitting element or the light-emitting device can be realized.Type: ApplicationFiled: December 26, 2005Publication date: October 16, 2008Applicant: Semiconductor Energy Laboratory Co., Ltd.Inventors: Harue Nakashima, Daisuke Kumaki, Kumi Kojima, Satoshi Seo, Sachiko Kawakami
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Patent number: 7429667Abstract: The invention concerns compounds which inhibit MEK and which have activity as anti-neoplastic agents. These compounds include N-substituted-3-hydroxy-5-arylamino-isothiazole-4-carboxamidines. Also included are the tautomeric isothiazol-3(2H)-ones.Type: GrantFiled: January 20, 2006Date of Patent: September 30, 2008Assignee: Ardea Biosciences, Inc.Inventors: Hassan Abdellaoui, Robert Tam, Huanming Chen, Varaprasad Chamakura, Dinesh Barawkar, Andreas Maderna, Zhi Hong, Stanley Lang
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Publication number: 20080220003Abstract: The present invention is related to a compound, preferably a C5a receptor antagonist, having the following structure, R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R11, R12, R13, R14, R15, R16, R17, R18, R19, R20, R21 and R22 are individually and independently selected from the group comprising H, alkyl, substituted alkyl, alkenyl, substituted alkenyl, alkynyl, substituted alkynyl, cycloalkyl, substituted cycloalkyl, heterocyclyl, substituted heterocyclyl, aryl, substituted aryl, heteroaryl, substituted heteroaryl, arylalkyl, substituted arylalkyl, heteroarylalkyl, substituted heteroarylalkyl, alkoxyl, substituted alkoxyl, aryloxy, substituted aryloxy, arylalkyloxy, substituted arylalkyloxy, acyloxy, substituted acyloxy, halogen, hydroxyl, nitro, cyano, acyl, substituted acyl, mercapto, alkylthio, substituted alkylthio, amino, substituted amino, alkylamino, substituted alkylamino, bisalkyl amino, substituted bisalkyl amino, cyclic amino, substituted cyclic amino, carbamoyl (—CONH2), substituted carbamoyl, carboxylType: ApplicationFiled: May 30, 2006Publication date: September 11, 2008Applicant: Jerini AGInventors: Karsten Schnatbaum, Dirk Scharn, Elsa Locardi, Thomas Polakowski, Uwe Richter, Ulrich Reineke, Gerd Hummel
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Publication number: 20080188490Abstract: The invention provides compounds of formula (I) wherein the substituents are as defined in the specification, to processes for their preparation and corresponding intermediates, and their use as pharmaceuticals.Type: ApplicationFiled: April 24, 2006Publication date: August 7, 2008Inventors: Ralf Glatthar, Thomas J. Troxler
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Patent number: 7404962Abstract: A combination kit for the treatment of malaria caused by Plasmodium vivax (P. vivax) having individual doses of an anti-malarial agent, 3-[1-[[4-[(6-methoxy-8-quinolinyl)amino]pentyl]amino]ethylidene]-dihydro-2(3H)-furanone (I) in the form of capsules; individual doses of the anti-malarial agent, chloroquine in the form of tablets; and instruction material for the administration of the two anti-malarial drugs. The combination kit is particularly suited for a 6 days treatment regimen where the treatment is rendered by five tablets containing 500 mg of chloroquine phosphate (equivalent to 300 mg base), three to be taken on day one and one each on days two and three; and five capsules containing 25 mg of 3-[1-[[4-[(6-methoxy-8-quinolinyl)amino]pentyl]amino]ethylidene]-dihydro-2(3H)-furanone (I), one each to be taken on days two to six.Type: GrantFiled: August 30, 2000Date of Patent: July 29, 2008Assignees: Nicholas Piramal India Limited, Council of Scientific and Industrial ResearchInventors: Francis Joseph Pinto, Swati Ajay Piramal, Ram Pratap, Amiya Prasad Bhaduri, Harsh Pati Thapliyal, Sunil Kumar Puri, Guru Prasad Dutta, Anil Kumar Dwivedi, Satyawan Singh, Pratima Srivastava, Vikash Chandra Pandey, Sudhir Srivastava, Shio Kumar Singh, Ram Chandra Gupta, Jagdishwar Sahai Srivastava, Omkar Prasad Asthana
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Publication number: 20080161575Abstract: The present invention provides a process for the preparation of 6-amino-4-(3-chloro-4-fluoro-phenylamino)-7-ethoxy-quinoline-3-carbonitrile comprising the steps and products disclosed within this application.Type: ApplicationFiled: March 10, 2008Publication date: July 3, 2008Applicant: WyethInventors: Sylvain Daigneault, Ronald Stanley Michalak, Michel Bernatchez
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Publication number: 20080153875Abstract: The invention relates to novel indole derivatives of the general formula 1, to their preparation and to their use as medicaments, in particular for treating tumors.Type: ApplicationFiled: March 6, 2008Publication date: June 26, 2008Applicant: AEterna Zentaris GmbHInventors: Peter Emig, Gerald Bacher, Dietmar Reichert, Silke Basner, Beate Aue, Bernd Nickel, Eckhard Gunther
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Publication number: 20080114172Abstract: A process for producing one selected stereoisomer of a substituted alcohol comprises reacting a stereoisomeric epoxide with an amine, a carboxylic acid, an amide, a sulfonyl, or a cyanide. The process avoids the production of a racemic mixture of stereoisomers of the prior art. Such a stereoisomeric substituted alcohol can be used for anti-inflammatory therapy.Type: ApplicationFiled: October 19, 2007Publication date: May 15, 2008Inventor: Arthur E. Harms
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Patent number: 7365081Abstract: The invention relates to novel indole derivatives of the general formula 1, to their preparation and to their use as medicaments, in particular for treating tumorsType: GrantFiled: July 20, 2001Date of Patent: April 29, 2008Assignee: AEterna Zentaris GmbHInventors: Peter Emig, Gerald Bacher, Dietmar Reichert, Silke Basner, Beate Aue, Bernd Nickel, Eckhard Günther
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Patent number: 7354932Abstract: The invention relates to heterocyclic compounds consisting of a core nitrogen atom surrounded by three pendant groups, wherein two of the three pendant groups are preferably benzimidazolyl methyl and tetrahydroquinolyl, and the third pendant group contains N and optionally contains additional rings. The compounds bind to chemokine receptors, including CXCR4 and CCR5, and demonstrate protective effects against infection of target cells by a human immunodeficiency virus (HIV).Type: GrantFiled: June 6, 2003Date of Patent: April 8, 2008Assignee: Anormed, Inc.Inventors: Gary Bridger, Al Kaller, Curtis Harwig, Renato Skerlj, David Bogucki, Trevor R. Wilson, Jason Crawford, Ernest J. McEachern, Bem Atsma, Siqiao Nan, Yuanxi Zhou, Dominique Schols, Christopher Dennis Smith, Maria Rosaria Di Fluri
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Publication number: 20080081907Abstract: The present invention relates to compounds of the formula (I): or pharmaceutically acceptable salts thereof, wherein X, Y, Ar1, and Ar2 are as defined in the specification.Type: ApplicationFiled: September 21, 2007Publication date: April 3, 2008Inventors: Sabine Kolczewski, Claus Riemer, Lucinda Steward, Juergen Wichmann, Thomas Woltering
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Patent number: 7342026Abstract: The invention relates to the use of quinolines having general formula (I), wherein R1 denotes H; alkyl C1-C15; alkenyl or alkynyl C2-C15; —CHO; heteroaryl; alkyl C1-C15 or alkenyl or alkynyl C2-C7 comprising at least one substituent selected from among O, halogen, —OH, —CHO, —COOH, aryloxycarbonyl, alkyloxycarbonyl C2-C8, alkenyloxycarbonyl C3-C9, nitrile, aryl, heteroaryl, arylsulphone, alkylsulphone C1-C7, thioalkyl or aminoalkyl C1-C7; alkenyl C2-C 7 bearing at least one substituent selected from among NH2, aleoxy C1-C7, phenoxy, cycloakyl C3-C6 or heteroaryloxy, alkenyl or alkynyl C2-C15 comprising at least one trialkylsilyl C1-C7; R2, in position 3, 6 or 8, denotes H; halogen; —OH; —CHO; —COOH; alkyl or aleoxy C1-C7; —NH2; alkenyl C2-C7; or alkynyl C2-C10; R1 and R2 do not both denote H.Type: GrantFiled: January 15, 2002Date of Patent: March 11, 2008Assignees: Institut de Recherche pour le Developpement, Centre National de la Recherche ScientifiqueInventors: Mohamed Fakhfakh, Bruno Figadere, Alain Fournet, Xavier Franck, Reynald Hocquemiller, Eric Prina
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Publication number: 20080058293Abstract: The invention provides compounds of formula (I) wherein n, p, q, X, R1, R2, R3, R4, R5 and R6 are as defined in the specification; processes for their preparation, pharmaceutical compositions containing them and their use in therapy.Type: ApplicationFiled: July 21, 2004Publication date: March 6, 2008Inventors: Rhonan Ford, Toby Thompson, Paul Willis
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Patent number: 7332605Abstract: This invention relates to a process for synthesizing heterocyclic pharmaceutical compound which binds to the CXCR4 chemokine receptor.Type: GrantFiled: March 11, 2005Date of Patent: February 19, 2008Assignee: AnorMED, Inc.Inventors: Jason B. Crawford, Gang Chen, David Gauthier, Renato Skerlj, Ian R. Baird, Trevor R. Wilson
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Patent number: 7329753Abstract: The invention relates to quinoline and isoquinoline derivatives of general formula I and a process for their production, and their use as inflammation inhibitors.Type: GrantFiled: June 13, 2006Date of Patent: February 12, 2008Assignee: Schering AGInventors: Stefan Jaroch, Manfred Lehmann, Norbert Schmees, Markus Berger, Hartmut Rehwinkel, Konrad Krolikiewicz, Werner Skuballa, Heike Schaecke, Arndt J. G. Schottelius
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Publication number: 20080021063Abstract: The present invention is based, in part, on our discovery of compounds that inhibit an activity of a sirtuin (e.g., compounds that inhibit or preferentially inhibit an activity of SIRT2) and are therefore believed useful in the treatment or prevention of diseases associated with sirtuin activity. These diseases include, but are not limited to, neurological disorders such as Parkinson's Disease (PD).Type: ApplicationFiled: July 18, 2006Publication date: January 24, 2008Inventor: Aleksey G. Kazantsev
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Patent number: 7312234Abstract: Tertiary amines containing a multiplicity of heteroaromatic substituents are useful as chemokine receptor modulators.Type: GrantFiled: August 9, 2004Date of Patent: December 25, 2007Assignee: AnorMEDInventors: Gary Bridger, Renato Skerlj, Al Kaller, Curtis Harwig, David Bogucki, Trevor R. Wilson, Jason Crawford, Ernest J. McEachern, Bem Atsma, Siqiao Nan, Yuanxi Zhou, Dominique Schols, Christopher Dennis Smith, Maria Rosaria Di Fluri
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Patent number: 7291631Abstract: The present invention relates to compounds that bind to chemokine receptors, and having the formula wherein each A, X, Y, R1, R2 and R3 are substituents. The present invention also relates to methods of using such compounds, such as in treating HIV infection and inflammatory conditions such as rheumatoid arthritis. Furthermore, the present invention relates to methods to elevate progenitor and stem cell counts, as well as methods to elevate white blood cell counts, using such compounds.Type: GrantFiled: April 12, 2004Date of Patent: November 6, 2007Assignee: Genzyme CorporationInventors: Gary J. Bridger, Ernest J. McEachern, Renato Skerlj, Dominique Schols, Ian Baird, Al Kaller, Curtis Harwig, Yongbao Zhu, Gang Chen, Krystyna Skupinska
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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: 7265115Abstract: Compounds of formula I: or pharmaceutically acceptable salts thereof, are useful for controlling synaptic transmission in mammals.Type: GrantFiled: April 11, 2003Date of Patent: September 4, 2007Assignee: Abbott LaboratoriesInventors: William H. Bunnelle, Daniela Barlocco Cristina, Jerome F. Daanen, Michael J. Dart, Michael D. Meyer, Keith B. Ryther, Michael R. Schrimpf, Kevin B. Sippy, Richard B. Toupence
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Patent number: 7205299Abstract: The invention relates to indole derivatives which are used as drugs for treating tumor diseases, in particular when there is drug resistance against other active compounds and where there is a metastasizing carcinoma.Type: GrantFiled: June 2, 2004Date of Patent: April 17, 2007Assignee: Zentaris GmbHInventors: Matthias Gerlach, Tilmann Schuster, Peter Ernig, Peter Schmidt, Silke Baasner, Eckhard Günther
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Patent number: 7199134Abstract: The present invention relates to a novel class of hydroxamic acid derivatives having at least two aryl containing groups, at least one of which is a quinolinyl, isoquinolinyl or benzyl moiety, linked to the hydroxamic acid group through a methylene chain. The hydroxamic acid compounds can be used to treat cancer, for example, brain cancer. The hydroxamic acid compounds can also inhibit histone deacetylase and are suitable for use in selectively inducing terminal differentiation, and arresting cell growth and/or apoptosis of neoplastic cells, thereby inhibiting proliferation of such cells. Thus, the compounds of the present are useful in treating a patient having a tumor characterized by proliferation of neoplastic cells. The compounds of the invention are also useful in the prevention and treatment of TRX-mediated diseases, such as autoimmune, allergic and inflammatory diseases, and in the prevention and/or treatment of diseases of the central nervous system (CNS), such as neurodegenerative diseases.Type: GrantFiled: April 1, 2004Date of Patent: April 3, 2007Assignees: Sloan-Kettering Institute for Cancer Research, The Trustees of Columbia University in the City of New YorkInventors: Ronald Breslow, Thomas A. Miller, Sandro Belvedere, Paul A. Marks, Victoria M. Richon, Richard A. Rifkind
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Patent number: 7183415Abstract: A compound, which has a melanin-concentrating hormone antagonistic action and useful as an agent for preventing or treating obesity, and which is represented by the formula: wherein Ar is a cyclic group optionally having substituent(s); X is a bond or a spacer having a main chain of 1 to 6 atoms; R1 and R2 are the same or different and each is a hydrogen atom or a hydrocarbon group optionally having substituent(s), or R1 and R2 may form, together with the adjacent nitrogen atom, a nitrogen-containing heterocycle optionally having substituent(s); Y is a divalent hydrocarbon group optionally having substituent(s) (except CO); R3 is a hydrogen atom or a hydrocarbon group optionally having substituent(s); and ring A and ring B may further have substituents, and when ring B further has a substituent, the substituent may be linked to R1 to form a ring, or a salt thereof, or a prodrug thereof, is provided.Type: GrantFiled: October 24, 2002Date of Patent: February 27, 2007Assignee: Takeda Pharmaceutical Company LimitedInventors: Yuji Ishihara, Makoto Kamata, Shiro Takekawa, Nobuhiro Suzuki, Koki Kato
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Patent number: 7183291Abstract: The present invention a novel use of primaquine derivative N1-(3-ethylidinotetrahydrofuran-2-one)-N4-(6-methoxy-8-quinolinyl)-1,4-pentanediamine in the treatment and controlling the spread of malaria. In particular, the present invention discloses a method of treatment of malaria by the use of primaquine derivative N1-(3-ethylidinotetrahydrofuran-2-one)-N4-(6-methoxy-8-quinolinyl)-1,4-pentanediamine as a gametocytocidal agent.Type: GrantFiled: May 21, 1999Date of Patent: February 27, 2007Assignee: Council of Scientific and Industrial ResearchInventors: Ram Pratap, Amiya Prasad Bhaduri, Harsh Pati Thapliyal, Sunil Kumar Puri, Guru Prasad Dutta, Anil Kumar Dwivedi, Satyawan Singh, Pratima Srivastava, Vikash Chandra Pandey, Sudhir Srivastava, Shio Kumar Singh, Ram Chandra Gupta, Jagdishwar Sahai Srivastava, Omkar Prasad Asthana
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Patent number: 7176312Abstract: General methods for the solution phase as well as solid phase synthesis of various substituted heteroaryls has been demonstrated. These substituted heteroaryls can be further elaborated by aromatic substitution with amines at elevated temperature or by anilines, boronic acids and phenols via palladium catalyzed cross-coupling reactions.Type: GrantFiled: October 12, 2002Date of Patent: February 13, 2007Assignees: The Scripps Research Institute, IRM LLCInventors: Sheng Ding, Qiang Ding, Nathanael S. Gray
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Patent number: 7138376Abstract: A compound, method and composition for treating a host infected with a hepatitis C viral comprising administering an effective hepatitis C treatment amount of a described 4?-disubstituted nucleoside or a pharmaceutically acceptable salt or prodrug thereof, is provided.Type: GrantFiled: September 30, 2002Date of Patent: November 21, 2006Assignees: Idenix Pharmaceuticals, Inc., Centre National de la Recherche ScientifiqueInventors: Gilles Gosselin, Jean-Louis Imbach, Jean-Pierre Sommadossi
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Patent number: 7126001Abstract: The present invention provides the compound having the formula: wherein each of R1 and R2 is, substituted or unsubstituted, aryl, cycloalkyl, cycloalkylamino, naphtha, pyridineamino, piperidino, t-butyl, aryloxy, arylalkyloxy, or pyridine group; wherein A is an amido moiety, —O—, —S—, —NH—, or —CH2—; and wherein n is an integer from 3 to 8. The present invention also provides a method of selectively inducing growth arrest, terminal differentiation and/or apoptosis of neoplastic cells and thereby inhibiting proliferation of such cells. Moreover, the present invention provides a method of treating a patient having a tumor characterized by proliferation of neoplastic cells. Lastly, the present invention provides a pharmaceutical composition comprising a pharmaceutically acceptable carrier and a therapeutically acceptable amount of the compound above.Type: GrantFiled: October 25, 2002Date of Patent: October 24, 2006Assignees: Sloan-Kettering Institute for Cancer Research, The Trustees of Columbia University in the City of New YorkInventors: Ronald Breslow, Sandro Belvedere, Leland Gershell, Thomas A. Miller, Paul A. Marks, Victoria M. Richon, Richard A. Rifkind
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Patent number: 7109212Abstract: The invention relates to quinoline and isoquinoline derivatives of general formula I and a process for their production, and their use as inflammation inhibitors.Type: GrantFiled: February 17, 2005Date of Patent: September 19, 2006Assignee: Schering AGInventors: Stefan Jaroch, Manfred Lehmann, Norbert Schmees, Markus Berger, Hartmut Rehwinkel, Konrad Krolikiewicz, Werner Skuballa, Heike Schaecke, Arndt. J. G. Schottelius
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Patent number: 7084155Abstract: Novel compounds that are useful for targeting chemokine receptors are disclosed. These compounds are complex tertiary amines.Type: GrantFiled: June 1, 2004Date of Patent: August 1, 2006Assignee: AnorMEDInventors: Gary Bridger, Renato Skerlj, Al Kaller, Curtis Harwig, David Bogucki, Trevor R. Wilson, Jason Crawford, Ernest J. McEachern, Bem Atsma, Siqiao Nan, Yuanxi Zhou, Dominique Schols, Christopher Dennis Smith, Maria Rosaria Di Fluri
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Patent number: 7041809Abstract: A light-resistant, metal complex dye for inkjet printing comprising a substituted 8-heterocyclic azo-5-aminoquinoline of the following structural formula:Type: GrantFiled: June 25, 2004Date of Patent: May 9, 2006Assignee: Lexmark International, Inc.Inventors: Bradley Leonard Beach, James F. Feeman, Kelly Ann Killeen
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Patent number: RE40525Abstract: A racemate diastereoisomer and optical isomer of a compound of formula (I): wherein B is H, a C6 or C10 aryl, C7-16 aralkyl; Het or (lower alkyl)-Het, all of which may be optionally substituted with C1-6 alkyl; C1-6 alkoxy; C1-6 alkanoyl; hydroxy; hydroxyalkyl; halo; haloalkyl; nitro; cyano; cyanoalkyl; amino optionally substituted with C1-6 alkyl; amido; or (lower alkyl)amide; or B is an acyl derivative of formula R4—C(O)—; a carboxyl derivative of formula R4—O—C(O)—; an amide derivative of formula R4—N(R5)—C(O)—; a thioamide derivative of formula R4—N(R5)—C(S)—; or a sulfonyl of formula R4—SO2; R5 is H or C1-6 alkyl; and Y is H or C1-6 alkyl; R3 is C1-8 alkyl, C3-7 cycloalkyl, or C4-10 alkylcycloalkyl, all optionally substituted with hydroxy, C1-6 alkoxy, C1-6 thioalkyl, amido, (lower alkyl)amido, C6 or C10 aryl, or C7-16 aralkyl; R2 is C2—R20, NH—R20, O—R20 or S—R20, wherein R20 is a saturated or unsaturated C3-7 cycloalkyl or C4-10 (alkylcycloalkyl), all of which being optionally mono-, di- or tri-Type: GrantFiled: September 30, 2005Date of Patent: September 30, 2008Assignee: Boehringer Ingelheim (Canada) Ltd.Inventors: Montse Llinas-Brunet, Murray D. Bailey, Dale R. Cameron, Anne-Marie Faucher, Elise Ghiro, Nathalie Goudreau, Teddy Halmos, Marc-André Poupart, Jean Rancourt, Youla S. Tsantrizos, Dominik M. Wernic