The Additional Unsaturated Hetero Ring And The Triazole Ring Are Attached To The Same Acyclic Atom Or To The Same Acyclic Chain Patents (Class 548/266.6)
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Patent number: 11465973Abstract: The invention relates to the compounds or its pharmaceutical acceptable polymorphs, solvates, enantiomers, stereoisomers and hydrates thereof. The pharmaceutical compositions comprising an effective amount of compounds of formula I, formula II, formula III, formula IV, formula V, formula VI, formula VII, formula VIII, formula IX, formula X, formula XI and formula XII and, the methods for the treatment of oral infectious diseases may be formulated for oral, buccal, rectal, topical, transdermal, transmucosal, lozenge, spray, intravenous, oral solution, buccal mucosal layer tablet, parenteral administration, syrup, or injection. Such compositions may be used to treatment of oral infectious diseases.Type: GrantFiled: October 8, 2020Date of Patent: October 11, 2022Assignee: Cellix Bio Private LimitedInventor: Mahesh Kandula
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Patent number: 10973804Abstract: The present application relates to compounded compositions, methods of making compounded compositions, kits comprising compounded compositions, containers comprising compounded compositions, and methods of using compounded compositions. For example, disclosed herein are compounded compositions comprising an anti-fungal agent and methods of using a compounded composition to treat or prevent a fungal infection or a suspected fungal infection. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.Type: GrantFiled: August 5, 2015Date of Patent: April 13, 2021Assignee: CMPD LICENSING, LLCInventor: Jay Richard Ray, II
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Publication number: 20150111893Abstract: The present invention relates to compounds of formula I: and pharmaceutically acceptable salts thereof, pharmaceutical compositions comprising the compounds of formula I, and methods of using said compounds, salts and compositions in the treatment of various disorders associated with CRM1 activity.Type: ApplicationFiled: May 9, 2013Publication date: April 23, 2015Inventors: Vincent P. Sandanayaka, Sharon Shechter, Sharon Shacham, Dilara McCauley, Erkan Baloglu
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Publication number: 20150105252Abstract: Disclosed is a method for controlling the growth of undesired vegetation comprising contacting the vegetation or its environment with a herbicidally effective amount of a compound of Formula 1, including all stereoisomers, N-oxides, and salts thereof, wherein A, R1, Q and J are as defined in the disclosure. Also disclosed is a method wherein the compound of Formula 1 (i.e. in a herbicidally effective amount) is comprised in a herbicidal composition further comprising at least one component selected from the group consisting of surfactants, solid diluents and liquid diluents. Also disclosed are compound of Formula 1 (including all stereoisomers), including N-oxides and salts thereof, their use as herbicides wherein A, R1, Q and J are as defined in the disclosure.Type: ApplicationFiled: October 15, 2014Publication date: April 16, 2015Inventor: THOMAS MARTIN STEVENSON
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Patent number: 8946236Abstract: The present invention relates to new insecticides of the formula (I) in which R1, R2, R3, R4, R5, R6, A, Q and n can have the definitions stated in the description, to a number of processes for preparing them and to their use as active compounds, more particularly to their use as pest control compositions.Type: GrantFiled: August 7, 2013Date of Patent: February 3, 2015Assignee: Bayer Cropscience AGInventors: Bernd Alig, Ruediger Fischer, Christian Funke, Rudolf F. Ernst Gesing, Achim Hense, Olga Malsam, Mark Wilhelm Drewes, Ulrich Goergens, Tetsuya Murata, Katsuaki Wada, Christian Arnold, Erich Sanwald
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Patent number: 8946231Abstract: The subject invention relates to novel P2X3 receptor antagonists that play a critical role in treating disease states associated with pain, in particular peripheral pain, inflammatory pain, or tissue injury pain that can be treated using a P2X3 receptor subunit modulator.Type: GrantFiled: March 15, 2010Date of Patent: February 3, 2015Assignee: Merck Sharp & Dohme Corp.Inventors: Christopher S. Burgey, Craig M. Potteiger
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Publication number: 20140249194Abstract: The invention discloses optically active compounds of Formula (1a) or Formula (1b), wherein R1 and R2 are independently selected from the group consisting of hydrogen and a halogen selected from the group consisting of fluorine, chlorine, bromine, and iodine; and wherein (a) R3 and R4 are independently selected from the group consisting of hydrogen and an alkyl group having a linear or branched chain having 1 to 20 carbon atoms, or (b) R3 and R4 together form a cycloalkyl ring having 3 to 10 carbon atoms fused to the thiophene ring; and wherein R5 is CN or COOR?, where R? is methyl or ethyl. The compounds of Formula (1a) or Formula (1b) may be used in pharmaceutical compositions for treating fungal infections.Type: ApplicationFiled: April 29, 2014Publication date: September 4, 2014Applicants: FDC LIMITED, COUNCIL OF SCIENTIFIC & INDUSTRIAL RESEARCHInventors: Hanumant Bapurao BORATE, SANGESHWER PRABHAKAR SAWARGAVE, SUBHASH PRATAPRAO CHAVAN, MOHAN ANAND CHANDAVARKAR, RAMAKRISHNAN RAMACAHNDRAN IYER, AMIT CHANDRAKANT TAWTE, DEEPALI DAMODAR RAO
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Publication number: 20140179733Abstract: Compounds are provided that act as potent antagonists of the CCR1 receptor, and have in vivo anti-inflammatory activity. The compounds are diazole lactam derivatives and are useful in pharmaceutical compositions, methods for the treatment of CCR1-mediated disease, and as controls in assays for the identification of competitive CCR1 antagonists.Type: ApplicationFiled: December 20, 2013Publication date: June 26, 2014Applicant: ChemoCentryx, Inc.Inventors: Xi Chen, Dean R. Dragoli, Pingchen Fan, Juan C. Jaen, Yandong Li, Jay P. Powers, Viengkham Malathong, Sreenivas Punna, Hiroko Tanaka, Penglie Zhang
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Publication number: 20140155370Abstract: The invention generally relates to the field of nuclear transport modulators, e.g., CRM1 inhibitors, and more particularly to new substituted-heterocyclic azole compounds, the synthesis and use of these compounds and their pharmaceutical compositions, e.g., in the treatment, modulation and/or prevention of physiological conditions associated with CRM1 activity such as in treating cancer and other neoplastic disorders, inflammatory diseases, disorders of abnormal tissue growth and fibrosis including cardiomyopathy, pulmonary fibrosis, hepatic fibrosis, glomerulonephritis, and other renal disorders, and for the treatment of viral infections (both acute and chronic).Type: ApplicationFiled: June 28, 2013Publication date: June 5, 2014Inventors: Sharon Shacham, Michael Kauffman, Vincent P. Sandanayaka, Sharon Shechter
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Publication number: 20140155440Abstract: The present invention provides cysteine and cystine bioisosteres for the treatment of schizophrenia and drug addiction. The invention further encompasses pharmaceutical compositions containing such bioisosteres and methods of using the bioisosteres for treatment of schizophrenia and drug addiction.Type: ApplicationFiled: January 7, 2014Publication date: June 5, 2014Applicants: MARQUETTE UNIVERSITY, UWM RESEARCH FOUNDATION, INC.Inventors: James M. Cook, David A. Baker, Edward Merle Johnson, II, Wenyuan Yin, Ranjit Singh Verma
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Patent number: 8729272Abstract: The present invention relates to a process using Grignard reagents for providing thio-triazolo group-containing compounds.Type: GrantFiled: March 15, 2011Date of Patent: May 20, 2014Assignee: BASF SEInventors: Maximilian Dochnahl, Michael Keil, Joachim Gebhardt, Uwe Josef Vogelbacher, Frederik Menges, Michael Rack, Jens Renner, Bernd Wolf
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Publication number: 20130324560Abstract: The present invention relates to new insecticides of the formula (I) in which R1, R2, R3, R4, R5, R6, A, Q and n can have the definitions stated in the description, to a number of processes for preparing them and to their use as active compounds, more particularly to their use as pest control compositions.Type: ApplicationFiled: August 7, 2013Publication date: December 5, 2013Applicant: BAYER CROPSCIENCE AGInventors: Bernd Alig, Ruediger Fischer, Christian Funke, Rudolf F. Ernst Gesing, Achim Hense, Olga Malsam, Mark Wilhelm Drewes, Ulrich Goergens, Tetsuya Murata, Katsuaki Wada, Christian Arnold, Erich Sanwald
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Publication number: 20130317031Abstract: The present invention relates to compounds of formula I: and pharmaceutically acceptable salts thereof, pharmaceutical compositions comprising the compounds of formula I, and methods of using said compounds, salts and compositions in the treatment of various disorders associated with CRM1 activity.Type: ApplicationFiled: May 9, 2013Publication date: November 28, 2013Applicant: Karyopharm Therapeutics Inc.Inventor: Karyopharm Therapeutics Inc.
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Patent number: 8536092Abstract: The present invention relates to new insecticides of the formula (I) in which R1, R2, R3, R4, R5, R6, A, Q and n can have the definitions stated in the description, to a number of processes for preparing them and to their use as active compounds, more particularly to their use as pest control compositions.Type: GrantFiled: December 14, 2011Date of Patent: September 17, 2013Assignee: Bayer Cropscience AGInventors: Bernd Alig, Rüdiger Fischer, Christian Funke, Rudolf F. Ernst Gesing, Achim Hense, Olga Malsam, Mark Wilhelm Drewes, Ulrich Görgens, Tetsuya Murata, Katsuaki Wada, Christian Arnold, Erich Sanwald
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Publication number: 20130190330Abstract: The present application relates to novel bisaryl-linked 5-aryl-1,2,4-triazolone derivatives, to processes for preparing them, to their use alone or in combinations for the treatment and/or prevention of diseases and also to their use for the production of medicaments for the treatment and/or prevention of diseases, more particularly for the treatment and/or prevention of cardiovascular disorders.Type: ApplicationFiled: February 25, 2011Publication date: July 25, 2013Applicant: BAYER INTELLECTUAL PROPERTY GMBHInventors: Chantal Furstner, Joerg Keldenich, Martina Delbeck, Peter Kolkhof, Axel Kretschmer, Ingo Pluschkell, Elisabeth Pook, Carsten Schmeck, Hubert Trubel
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Publication number: 20130059833Abstract: The present invention relates to compounds of formula (I) wherein R1, R2, R3, R5, W, X, X1, Y, Y1, Z and Z1 are as defined in the description and in the claims, as well as physiologically acceptable salts thereof. These compounds inhibit PDE10A and can be used in the treatment of CNS disorders such as schizophrenia, Alzheimer's disease, and Parkinson's disease.Type: ApplicationFiled: August 30, 2012Publication date: March 7, 2013Inventors: Stephan Bachmann, Alexander Flohr, Katrin Groebke Zbinden, Matthias Koerner, Bernd Kuhn, Jens-Uwe Peters, Markus Rudolph
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Publication number: 20130005985Abstract: The present invention relates to a process using Grignard reagents for providing thio-triazolo group-containing compounds.Type: ApplicationFiled: March 15, 2011Publication date: January 3, 2013Applicant: BASF SEInventors: Maximilian Dochnahl, Michael Keil, Joachim Gebhardt, Uwe Josef Vogelbacher, Frederik Menges, Michael Rack, Jens Renner, Bernd Wolf
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Publication number: 20120322827Abstract: Disclosed are compounds having the formula: wherein X1, X2, X3, R1, R2, R3, R4, Y, A, n and L are as defined herein, and methods of making and using the same.Type: ApplicationFiled: January 13, 2011Publication date: December 20, 2012Inventors: Erkan Baloglu, Shomir Ghosh, Mercedes Lobera, Darby Schmidt
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Patent number: 8318789Abstract: The present invention relates to co-crystals of propiconazole and a co-crystal forming compound.Type: GrantFiled: March 20, 2008Date of Patent: November 27, 2012Assignee: Syngenta LimitedInventors: Neil George, James Forrest, Paul Edward Bonnett, Pauline Theresa Gavin
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Patent number: 8309103Abstract: The present invention refers to a treatment for mixed infectious diseases in the human reproductive system, wherein an association of compounds containing fluconazole and either tinidazole or secnidazole is used, the same being associated in doses lower to those commonly used therapeutically. The combination has proven to be highly efficacious and shown a good degree of tolerance.Type: GrantFiled: January 22, 2004Date of Patent: November 13, 2012Assignee: Alparis, S.A. DE C.V.Inventors: Luisa Hernandez-Ramirez, Angelica Arzola-Paniagua, Raul E. Garcia-Salgado-Lopez, Fernando Poot-Lopez
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Patent number: 8236840Abstract: The present invention discloses novel compounds of the Formula (1), containing thiophene moieties and pharmaceutically acceptable salts thereof, methods for preparing these compounds, the use of these compounds in prevention and treatment of fungal infections, and pharmaceutical preparations containing these novel compounds.Type: GrantFiled: October 1, 2009Date of Patent: August 7, 2012Assignees: Council of Scientific & Industrial Research, FDC LimitedInventors: Hanumant Bapurao Borate, Sangmeshwer Prabhakar Sawargave, Suleman Riyajsaheb Maujan, Mohan Anand Chandavarkar, Sharangi Ravinda Vaiude, Vinay Anant Joshi
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Patent number: 8236788Abstract: The present invention relates to azolylmethyloxiranes of the general formula I in which A or B is phenyl which is substituted by one CN and optionally by one to three of the following substituents: halogen, NO2, amino, C1-C4-alkyl, C1-C4-alkoxy, C1-C4-haloalkyl, C1-C4-haloalkoxy, C1-C4-alkylamino, C1-C4-dialkylamino, thio or C1-C4-alkylthio, and the respective other substituent A or B is phenyl or 5-membered or 6-membered heteroaryl, these substituents optionally being substituted by one to three of the following substituents: halogen, CN, NO2, amino, C1-C4-alkyl, C1-C4-alkoxy, C1-C4-haloalkyl, C1-C4-haloalkoxy, C1-C4-alkylamino, C1-C4-dialkylamino, thio or C1-C4-alkylthio, and to the plant-compatible acid addition salts or metal salts thereof, to the use of the compounds of the formula I for controlling phytopathogenic fungi and to compositions comprising these compounds.Type: GrantFiled: July 18, 2007Date of Patent: August 7, 2012Assignee: BASF SEInventors: Jochen Dietz, Thomas Grote, Bernd Müller, Jan Klaas Lohmann, Jens Renner, Sarah Ulmschneider, Alice Glättli
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Patent number: 8207352Abstract: A new technical process for preparation of enantiomerically pure antifungal compounds of formula I by resolution of the racemates has been disclosed.Type: GrantFiled: October 8, 2009Date of Patent: June 26, 2012Assignee: Drug Process Licensing Associates LLCInventor: Milan Soukup
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Publication number: 20120094830Abstract: The present invention relates to new insecticides of the formula (I) in which R1, R2, R3, R4, R5, R6, A, Q and n can have the definitions stated in the description, to a number of processes for preparing them and to their use as active compounds, more particularly to their use as pest control compositions.Type: ApplicationFiled: December 14, 2011Publication date: April 19, 2012Applicant: BAYER CROPSCIENCE AGInventors: Bernd ALIG, Rüdiger FISCHER, Christian FUNKE, Ernst Rudolf F. GESING, Achim HENSE, Olga MALSAM, Mark Wilhelm DREWES, Ulrich GÖRGENS, Tetsuya MURATA, Katsuaki WADA, Christian ARNOLD, Erich SANWALD
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Publication number: 20120088747Abstract: Compounds, compositions and methods for treating GHS-R mediated disorders are described herein.Type: ApplicationFiled: October 30, 2009Publication date: April 12, 2012Inventor: Jeffrey O. Saunders
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Publication number: 20120088663Abstract: The present invention relates to novel triazole compounds of the formulae I and II as defined below which carry a sulfur substituent, to agricultural compositions containing them, to their use as fungicides and to intermediate compounds used in the method of producing them.Type: ApplicationFiled: June 17, 2010Publication date: April 12, 2012Applicant: BASF SEInventors: Sarah Uluschneider, Jochen Dietz, Jens Renner, Thomas Grote, Wassilios Grammenos, Bernd Mueller, Jan Klaas Lohmann, Marianna Vrettou-Schultes, Richard Riggs
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Publication number: 20120022083Abstract: Compounds, particularly compounds having activity as modulators of cadherin-mediated cell adhesion having the following structure: or a pharmaceutically acceptable salt, stereoisomer or prodrug thereof, wherein R1, R2, R3, R4, R5, R6, A, X, Y, Z, m and n are as defined herein. Methods associated with preparation and use of the same, as well as pharmaceutical compositions containing the same, are also disclosed.Type: ApplicationFiled: February 9, 2011Publication date: January 26, 2012Applicant: ADHEREX TECHNOLOGIES, INC.Inventors: Mukur Gupta, Brian Huber, Orest W. Blaschuk
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Publication number: 20120008228Abstract: This invention provides a magnetic recording medium excellent in terms of corrosion resistance. The magnetic recording medium comprises a magnetic recording layer, a protective layer and a lubricant layer provided on a nonmagnetic substrate, and the lubricant layer comprises a compound having a heterocyclic ring.Type: ApplicationFiled: July 8, 2011Publication date: January 12, 2012Inventors: Katsumi MABUCHI, Kyoko Honbo, Mina Amo
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Publication number: 20110295019Abstract: The present invention relates to a method for producing 1-hydroxymethyl-1,2-diphenyloxiranes from 2,3-diphenylpropenals by means of epoxidation and reduction. The formation of objectionable by-products can be suppressed in that the reduction is started before the 2,3-5 diphenylpropenal is completely converted. The hydroxymethyl diphenyloxiranes represent valuable intermediate products for producing 1-azolylmethyl-1,2-diphenyloxiranes, wherein the latter can be easily produced from said intermediate products by introducing the azolyl group.Type: ApplicationFiled: February 4, 2010Publication date: December 1, 2011Applicant: BASF SEInventors: Rainer Noack, Clemens Palm, Carsten Gröning, Gunter Lipowsky
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Publication number: 20110281879Abstract: The present invention is directed to compounds that are inhibitors of cysteine proteases, in particular, cathepsins B, K, L, F, and S and are therefore useful in treating diseases mediated by these proteases. The present invention is directed to pharmaceutical compositions comprising these compounds and processes for preparing them.Type: ApplicationFiled: January 12, 2011Publication date: November 17, 2011Applicant: ViroBay, Inc.Inventor: Craig Mossman
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Publication number: 20110275607Abstract: The invention generally relates to the field of nuclear transport modulators, e.g., CRM1 inhibitors, and more particularly to new substituted-heterocyclic azole compounds, the synthesis and use of these compounds and their pharmaceutical compositions, e.g., in the treatment, modulation and/or prevention of physiological conditions associated with CRM1 activity such as in treating cancer and other neoplastic disorders, inflammatory diseases, disorders of abnormal tissue growth and fibrosis including cardiomyopathy, pulmonary fibrosis, hepatic fibrosis, glomerulonephritis, and other renal disorders, and for the treatment of viral infections (both acute and chronic).Type: ApplicationFiled: March 5, 2011Publication date: November 10, 2011Applicant: KARYOPHARM THERAPEUTICS, INC.Inventors: Sharon Shacham, Michael Kauffman, Vincent P. Sandanayaka, Sharon Shechter
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Publication number: 20110257235Abstract: The present disclosure relates to certain new and known triazolium and/or imidazolium salts and to their therapeutic use, for example in methods of treating or preventing an infection by a Plasmodium or Babesia parasite in a subject in need thereof. The triazolium and imidazolium salts are compounds of the Formula (I) or (II): wherein R1-R4, R1?-R3?, R8-R11, X, X?, X?, Y, Y? and Y? are as defined in the disclosure.Type: ApplicationFiled: September 4, 2009Publication date: October 20, 2011Inventors: Ian E. Crandall, Walter A. Szarek, Jason Z. Vlahakis
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Publication number: 20110223093Abstract: This invention relates to sulfur functionalized ionic liquid compounds that are useful in methods of carbon dioxide or sulfur dioxide removal to which they may be applied.Type: ApplicationFiled: March 11, 2011Publication date: September 15, 2011Applicant: E.I. DU PONT DE NEMOURS AND COMAPNYInventor: MARK A. SCIALDONE
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Publication number: 20110144171Abstract: The present invention discloses novel compounds of the Formula (1), containing thiophene moieties and pharmaceutically acceptable salts thereof, methods for preparing these compounds, the use of these compounds in prevention and treatment of fungal infections, and pharmaceutical preparations containing these novel compounds.Type: ApplicationFiled: October 1, 2009Publication date: June 16, 2011Applicants: COUNCIL OF SCIENCE & INDUSTRIAL RESEARCH, FDC LIMITEDInventors: Hanumant Bapurao Borate, Sangmeshwer Prabhakar Sawargave, Suleman Ruyajsaheb Maujan, Mohan Anand Chandavarkar, Sharangi Ravinda Vaiude, Vinay Anant Joshi
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Publication number: 20110077409Abstract: Cyano-substituted sulfilimines are produced efficiently and in high yield from the corresponding sulfides by reaction with cyanamide and hypochlorite.Type: ApplicationFiled: November 18, 2010Publication date: March 31, 2011Inventors: David E. Podhorez, Ronald Ross, JR., James R. McConnell
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Patent number: 7910614Abstract: The present invention relates to azolylmethyloxiranes of the general formula I in which A or B is benzodioxolyl which is optionally substituted by one to five of the following substituents: halogen, CN, NO2, amino, C1-C4-alkyl, C1-C4-alkoxy, C1-C4-haloalkyl, C1-C4-haloalkoxy, C1-C4-alkylamino, C1-C4-dialkylamino, thio or C1-C4-alkylthio, and the respective other substituent A or B is phenyl or 5-membered or 6-membered heteroaryl, these substituents optionally being substituted by one to three of the following substituents: halogen, CN, NO2, amino, C1-C4-alkyl, C1-C4-alkoxy, C1-C4-haloalkyl, C1-C4-haloalkoxy, C1-C4-alkylamino, C1-C4-dialkylamino, thio or C1-C4-alkylthio, and to the plant-compatible acid addition salts or metal salts thereof, to the use of the compounds of the formula I for controlling phytopathogenic fungi and to compositions comprising these compounds.Type: GrantFiled: July 17, 2007Date of Patent: March 22, 2011Assignee: BASF SEInventors: Jochen Dietz, Thomas Grote, Bernd Müller, Jan Klaas Lohmann, Jens Renner, Sarah Ulmschneider, Alice Glättli
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Publication number: 20110003799Abstract: The invention provides compounds of the formula (0) or salts or tautomers or N-oxides or solvates thereof for use in the prophylaxis or treatment of disease states and conditions such as cancers mediated by cyclin-dependent kinase and glycogen synthase kinase-3. In formula (0): X is a group R1-A-NR4— or a 5- or 6-membered carbocyclic or heterocyclic ring; A is a bond, SO2, C?O, NRg(C?O) or O(C?O) wherein Rg is hydrogen or C1-4 hydrocarbyl optionally substituted by hydroxy or C1-4 alkoxy; Y is a bond or an alkylene chain of 1, 2 or 3 carbon atoms in length; R1 is hydrogen; a carbocyclic or heterocyclic group having from 3 to 12 ring members; or a C1-8 hydrocarbyl group optionally substituted by one or more substituents selected from halogen (e.g.Type: ApplicationFiled: September 8, 2010Publication date: January 6, 2011Applicant: ASTEX THERAPEUTICS, LTD.Inventors: Valerio BERDINI, Michael Alistair O'BRIEN, Maria Grazia CARR, Theresa Rachel EARLY, Adrian Liam GILL, Gary TREWARTHA, Alison Jo-Anne WOOLFORD, Andrew James WOODHEAD, Paul Graham WYATT
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Publication number: 20100298394Abstract: Provided herein are compounds, compositions and methods for protecting neuronal and glial cells.Type: ApplicationFiled: June 14, 2010Publication date: November 25, 2010Applicant: THE JOHNS HOPKINS UNIVERSITYInventors: Joseph P. Steiner, Avindra Nath, Norman Haughey
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Patent number: 7803786Abstract: The present invention comprises pharmaceutical compositions comprising a co-crystal of an API and a co-crystal former, and methods of making and using the same.Type: GrantFiled: June 16, 2005Date of Patent: September 28, 2010Assignees: Transform Pharmaceuticals, Inc., University of South FloridaInventors: Jennifer McMahon, Matthew Peterson, Michael J. Zaworotko, Tanise Shattock, Magali Bourghol Hickey
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Patent number: 7781431Abstract: The present invention relates to thienopyrrole compounds of formula (I); wherein A, B, Y, Ar, n, Z and X1 are as defined herein, and pharmaceutically acceptable salts thereof, useful in the prevention and treatment of hepatitis C infections.Type: GrantFiled: September 7, 2004Date of Patent: August 24, 2010Assignee: Istituto di Ricerche di Biologia Molecolare P Angeletti SpAInventors: Barbara Attenni, Jose Ignacio Martin Hernando, Savina Malancona, Frank Narjes, Jesus Maria Ontoria Ontoria, Michael Rowley
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Patent number: 7696352Abstract: The present invention is directed to compounds represented by Formula (I) or a pharmaceutically acceptable salt, ester, or prodrug thereof which are inhibitors of Factor Xa. The present invention is also directed to and intermediates used in making such compounds, pharmaceutical compositions containing such compounds, methods to prevent or treat a number of conditions characterized by undesired thrombosis and methods of inhibiting the coagulation of a blood sample.Type: GrantFiled: January 5, 2007Date of Patent: April 13, 2010Assignee: Millennium Pharmaceuticals, Inc.Inventors: Bing-Yan Zhu, Shawn M. Bauer, Zhaozhong J. Jia, Yonghong Song, Gary D. Probst, Yanchen Zhang, Robert M. Scarborough, Carroll Anna Crew Scarborough, legal representative
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Publication number: 20100063285Abstract: The present invention relates to triazole derivaties, a method for the preparation thereof, and a pharmaceutical composition containing the same as an active ingredient. The inventive triazole derivaties have an excellent antifungal activity against various pathogens.Type: ApplicationFiled: December 28, 2007Publication date: March 11, 2010Applicant: DAEWOONG PHARMACEUTICAL CO., LTD.Inventors: Joon Seok Park, Kyung A Yu, Yun Soo Yoon, Mi Ryeong Han
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Publication number: 20090186924Abstract: This invention relates to a range of 1-aryl-4-cyclopropylpyrazoles in which the cyclopropyl ring is substituted at the angular position, and pharmaceutically acceptable salts and solvates thereof, to compositions comprising such compounds, processes to their synthesis and their use as parasiticides.Type: ApplicationFiled: March 19, 2009Publication date: July 23, 2009Applicants: Pfizer Inc., Pfizer Products Inc..Inventors: Denis Billen, Jessica Boyle, Douglas James Critcher, David Morris Gethin, Kim Thomas Hall, Graham Michael Kyne
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Publication number: 20090099209Abstract: Compounds of formula (I), or pharmaceutically acceptable derivatives thereof, wherein: R1 represents H, C1-6alkyl, C1-6alkyloxy, C3-8cycloalkyl, or halo; R2 represents H, C1-6alkyl (optionally substituted by R3), phenyl (optionally substituted by CN), or Het; R3 represents OH, CN, Het, —R4—C1-6alkyl, or CONR5R6; R4 represents —CO2—, or —O—; R5 and R6 independently represent H, C1-6alkyl (optionally substituted by OR7) or C3-8cycloalkyl; R7 represents H or C1-6alkyl; Het represents a five or six membered aromatic heterocyclic group containing (i) from one to four nitrogen heteroatom(s) or (ii) one or two nitrogen heteroatom(s) and one oxygen or one sulphur heteroatom or (iii) one or two oxygen or sulphur heteroatom(s), said heterocyclic group being optionally substituted by one or more groups selected from CN and C1-6alkyl; R8 represents C1-6alkyl, C1-6alkyloxy, C3-8cycloalkyl, or halo; and R9 and R10 independently represent H, C1-6alkyl, C1-6alkyloxy, CN, CF3 or halo; may be useful for treatiType: ApplicationFiled: December 12, 2008Publication date: April 16, 2009Inventors: Paul Anthony Bradley, Kevin Neil Dack, Ian Roger Marsh
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Publication number: 20090082367Abstract: [Problem] To provide a compound which may be used in treating diseases in which 11?-hydroxysteroid dehydrogenase type 1 (11?-HSD1) is concerned, especially diabetes and insulin resistance. [Means for Solution] It was found that a triazole derivative or a pharmaceutically acceptable salt thereof, in which the 3-position of triazole ring is substituted with a trisubstituted methyl group and the 5-position is substituted with a lower alkyl, cycloalkyl or the like, has a strong 11?-HSD1-inhibitory activity. In addition, since the triazole derivative of the present invention shows excellent blood glucose-lowering action, it may be used in the treatment of diabetes and insulin resistance.Type: ApplicationFiled: March 14, 2007Publication date: March 26, 2009Applicant: ASTELLAS PHARMA INC.Inventors: Seiji Yoshimura, Ryota Shiraki, Tomoaki Kawano, Daisuke Sasuga, Mitsuru Hosaka, Hiroki Fukudome, Kazuo Kurosawa, Hirofumi Ishii, Takanori Koike
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Publication number: 20090062357Abstract: The present application describes deuterium-enriched fluconazole, pharmaceutically acceptable salt forms thereof, and methods of treating using the same.Type: ApplicationFiled: August 21, 2008Publication date: March 5, 2009Applicant: PROTIA, LLCInventor: Anthony W. Czarnik
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Publication number: 20080287440Abstract: Disclosed herein are antifungal triazole derivatives or pharmaceutically acceptable salts thereof, a preparation method thereof, and a pharmaceutical composition comprising the same. The triazole derivatives of Chemical Formula 1 or pharmaceutically acceptable salts thereof according to the present invention have excellent inhibitory activity against a broad spectrum of fungi, in addition to being safe to the body, and thus are very useful in the treatment and prevention of fungal infection.Type: ApplicationFiled: October 31, 2006Publication date: November 20, 2008Applicant: Daewoong Pharmaceutidcal Co., Ltd.Inventors: Joon Seok Park, Kyung A Yu, Sun Young Kim, Yeon Jung Song, Kang-Pil Kim, Yun Soo Yoon, Mi Ryeong Han
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Patent number: 7348440Abstract: The present invention relates to dihydropyrrole compounds that are useful for treating cellular proliferative diseases, for treating disorders associated with KSP kinesin activity, and for inhibiting KSP kinesin. The invention also related to compositions which comprise these compounds, and methods of using them to treat cancer in mammals.Type: GrantFiled: June 12, 2003Date of Patent: March 25, 2008Assignee: Merck & Co., Inc.Inventors: Kenneth L. Arrington, Paul J. Coleman, Christopher D. Cox, Mark E. Fraley, Robert M. Garbaccio, George D. Hartman, William F. Hoffman, Edward S. Tasber
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Publication number: 20080027117Abstract: An azole derivative of formula (I) having a fluorovinyl moiety or a pharmaceutically acceptable salt thereof is superior to the conventional antifungal drugs in antifungal activity against a wide spectrum of pathogenic fungi, and has advantageously low toxicity.Type: ApplicationFiled: August 9, 2004Publication date: January 31, 2008Applicant: KOREA RESERACH INSTIITUTE OF CHEMICAL TECHNOLOGYInventors: Bum Tae Kim, Yong Ki Min, Yeon Soo Lee, No Kyun Park, Woo Jung Kim
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Patent number: 7223780Abstract: The present invention is directed to the compound of formula I which is useful for inhibiting the activity of blood clotting enzyme Factor Xa. The present invention is also directed to compositions containing said compounds, processes for their preparation, their use, such as for inhibiting the formation of thrombin or for therapeutically treating a patient suffering from, or subject to, a disease state associated with a cardiovascular disorder.Type: GrantFiled: May 19, 2004Date of Patent: May 29, 2007Assignee: Sanofi-Aventis Deutschland GmbHInventors: Marc Nazare, Volker Laux, Armin Bauer, Michael Wagner