Three Or More Ring Hetero Atoms In The Tetracyclo Ring System Patents (Class 544/247)
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Catalytic depolymerization of polymers containing electrophilic linkages using nucleophilic reagents
Patent number: 8492504Abstract: The disclosure relates to methods and materials useful for depolymerizing a polymer. In one embodiment, for example, the disclosure provides a method for depolymerizing a polymer containing electrophilic linkages, wherein the method comprises contacting the polymer with a nucleophilic reagent in the presence of a guanidine-containing compound. The methods and materials of the disclosure find utility, for example, in the field of waste reclamation and recycling.Type: GrantFiled: August 7, 2012Date of Patent: July 23, 2013Assignees: International Business Machines Corporation, The Board of Trustees of the Leland Stanford Junior UniversityInventors: James Lupton Hedrick, Russell Clayton Pratt, Robert M. Waymouth -
Patent number: 8486901Abstract: Novel sodium channel blocking compounds tetrodotoxm galactopyranosides of formula I were isolated and purified by HPLC and identified further through IR, NMR, GC, and MS. The compounds have a galactopyranosyl moiety attached to C11 of tetrodotoxin and retain the analgesic activity of the latter. Pharmaceutical compositions and medical uses thereof are further disclosed.Type: GrantFiled: March 26, 2010Date of Patent: July 16, 2013Assignee: Wex Medical LimitedInventor: Weiyang Lin
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Publication number: 20130172320Abstract: This disclosure is directed to pyrido[4,3-b]indole and pyrido[3,4-b]indole derivatives. Pharmaceutical compositions comprising the compounds are also provided, as are methods of using the compounds in a variety of therapeutic applications, including the treatment of a cognitive disorder, psychotic disorder, neurotransmitter-mediated disorder and/or a neuronal disorder.Type: ApplicationFiled: February 18, 2011Publication date: July 4, 2013Inventors: Sarvajit Chakravarty, Barry Patrick Hart, Rajendra Parasmal Jain
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Publication number: 20130156851Abstract: What is described are macrocyclic compounds formed by reaction of a cyclic compound, which contains an amine, with an epoxide. The macrocyclic compound has the following structure: When substituents R and R? that are hydrophobic substituents, the macrocyclic compound functions as a lipid and is compatible with lipid systems, including liposomes and lipid particles. When present in certain lipid systems, the macrocyclic compound enhances the ability of the lipid system to facilitate delivery of therapeutic molecules to target cells in a mammalian subject.Type: ApplicationFiled: August 26, 2011Publication date: June 20, 2013Inventors: Kunyuan Cui, Dong Liang
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Publication number: 20130092922Abstract: The present invention relates to an electronic device comprising anode, cathode and at least one organic layer which comprises a compound of the formula (I) to (IV). The invention furthermore encompasses the use of compounds of the formula (I) to (IV) in an electronic device and to a compound of the formula (Ic) to (IVc).Type: ApplicationFiled: May 30, 2011Publication date: April 18, 2013Applicant: Merck Patent GmbHInventors: Philipp Stoessel, Arne Buesing, Dominik Joosten
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Publication number: 20130085123Abstract: Optionally substituted 4,5,7,8-tetrahydro-(optionally 4-oxo, 4-thioxo or 4-imino)-(1H or 2H)-imidazo[1,2-a]pyrazolo[4,3-e]pyrimidine or 4,5,7,8,9-pentahydro-(optionally 4-oxo, 4-thioxo or 4-imino)-(1H or 2H)-pyrimido[1,2-a]pyrazolo[4,3-e]pyrimidine compounds, processes for their production, their use as pharmaceuticals and pharmaceutical compositions comprising them.Type: ApplicationFiled: May 31, 2011Publication date: April 4, 2013Applicant: INTRA-CELLULAR THERAPIES, INC.Inventors: Peng Li, Hailin Zheng, Jun Zhao, Lawrence P. Wennogle
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Patent number: 8367796Abstract: The disclosure relates to methods and materials useful for polymerizing a monomer. In one embodiment, for example, the disclosure provides a method for polymerizing a monomer containing a plurality of electrophilic groups, wherein the method comprises contacting the monomer with a nucleophilic reagent in the presence of a guanidine-containing catalyst. The methods and materials of the disclosure find utility, for example, in the field of materials science.Type: GrantFiled: July 1, 2009Date of Patent: February 5, 2013Assignees: International Business Machines Corporation, Stanford UniversityInventors: James Lupton Hedrick, Russell Clayton Pratt, Robert M. Waymouth
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Publication number: 20130029980Abstract: The present invention relates novel flavin derivatives, their use and compositions for use as riboswitch ligands and/or anti-infectives.Type: ApplicationFiled: April 6, 2011Publication date: January 31, 2013Inventors: Philip D. G. Coish, Brian R. Dixon, David Osterman, Paul Adrian Aristoff, Manuel Navia, Frank Sciavolino, Stephanie Avola, Nick Baboulas, Thomas R. Belliotti, Angelica Bello, Judd Berman, Robert A. Chrusciel, Bruce R. Evans, Harpreet Kaur, David Moon, Vinh Pham, Andrew Roughton, Phil Wickens, Jeffrey Wilson, Heinrich J. Schostarez
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Publication number: 20130018063Abstract: The invention provides novel 7,8-dihydro-imidazo[1,2-a]pyrazolo[4,3-e]pyrimidin-4-one compounds and 7,8,9-trihydro-[1H or 2H]-pyrimido[1,2-a]pyrazolo[4,3-e]pyrimidin-4(5H)-one compounds, substituted at the 1 or 2 position with C2-9 alkyl, C3-9 cycloalkyl, heteroarylalkyl, or substituted arylalkyl, in free, salt or prodrug form, processes for their production, their use as pharmaceuticals, particularly as PDE1 inhibitors, and pharmaceutical compositions comprising them.Type: ApplicationFiled: July 18, 2012Publication date: January 17, 2013Inventors: Peng LI, Haiyan Wu
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Publication number: 20120277224Abstract: Disclosed herein are new heterocyclic compounds and compositions and their application as pharmaceuticals for the treatment of disease. Methods of inhibiting PAS Kinase (PASK) activity in a human or animal subject are also provided for the treatment of diseases such as diabetes mellitus.Type: ApplicationFiled: April 26, 2012Publication date: November 1, 2012Applicant: BIOENERGENIXInventors: John M. McCall, Robert C. Kelly, Donna L. Romero
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Patent number: 8288396Abstract: The invention is to provide a novel anticancer agent or sensitizer for cancer chemotherapy or radiotherapy. A compound of a general formula (I): wherein A means an aryl group or a heteroaryl group, or a group of a formula (a): R1 means a —(C?O)aOb(C1-C6)alkyl group, a —(C?O)aOb(C2-C6)alkenyl group, a —(C?O)aOb(C3-C6)cycloalkyl group, an aryl group or a heteroaryl group; R2 and R3 each mean a hydrogen atom, a halogen atom, a hydroxyl group, a carboxyl group, a —(C?O)aOb(C1-C6)alkyl group or a group of —(C?O)aN(R1e)R2e; R4 means a hydrogen atom or a (C1-C6)alkyl group, and the like have an excellent Wee1-kinase-inhibitory effect, and are therefore useful in the field of medicine, especially in the field of various cancer treatments.Type: GrantFiled: February 18, 2010Date of Patent: October 16, 2012Assignee: MSDKKInventors: Yasuhiro Goto, Kenji Niiyama, Satoshi Sunami, Keiji Takahashi
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Patent number: 8288395Abstract: The invention relates to novel pyrimido-benzimidazole derivatives. Said products exhibit a good affinity for certain melanocortin receptor sub-types, in particular MC4 receptors. Said products represent a particular interest for treating pathological disorders and diseases associated with one or several melanocortin receptors. Pharmaceutical compositions containing said products and the use thereof for a drug preparation are also disclosed.Type: GrantFiled: June 17, 2010Date of Patent: October 16, 2012Assignee: Ipsen Pharma S.A.S.Inventors: Lydie Poitout, Carole Sackur, Valerie Brault, Pierre Roubert, Pascale Plas
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Publication number: 20120244182Abstract: The invention provides immunostimulatory compositions and methods of administration thereof. Also provided are methods of administering a tryptanthrin compound in an effective amount to enhance the immune response of a subject to an antigen. Also provided are methods of administering an effective amount of a tryptanthrin to stimulate the immune response in a subject for the treatment of cancer. Further provided are methods of administering a tryptanthrin compounds as an immunotherapeutic in the treatment of infectious diseases.Type: ApplicationFiled: June 4, 2012Publication date: September 27, 2012Applicant: NOVARTIS VACCINES AND DIAGNOSTICS, INC.Inventor: Nicholas M. VALIANTE
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Patent number: 8273877Abstract: Substituted tetraazapentalenes have two benzenoid rings and eight substitutable positions. Substitutions are made of hydrogen or C—H groups in favor of amino groups, nitro groups or nitrogen atoms. The tetraazapentalenes are synthesized through an intermediate azo, which is made from a 1:1:1 molar ratio of a nitroaniline, sodium nitrite and an amine.Type: GrantFiled: November 18, 2011Date of Patent: September 25, 2012Assignee: The United States of America as Represented by the Secretary of the NavyInventors: Alfred G. Stern, Patrick A. Caruana
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Patent number: 8273750Abstract: The invention provides novel 7,8-dihydro-imidazo[1,2-?]pyrazolo[4,3-e]pyrimidin-4-one compounds and 7,8,9-trihydro-[1H or 2/f]-pyrimido[1,2-a]pyrazolo[4,3-e]pyrimidin-4(5H)-one compounds, substituted at the 1 or 2 position with C2-g allcyl, C3-9 cycloalkyl, heteroarylalkyl, or substituted arylalkyl, in free, salt or prodrug form, processes for their production, their use as pharmaceuticals, particularly as PDE1 inhibitors, and pharmaceutical compositions comprising them.Type: GrantFiled: June 6, 2006Date of Patent: September 25, 2012Assignee: Takeda Pharmaceutical Company LimitedInventors: Peng Li, Haiyan Wu
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Publication number: 20120214824Abstract: The present invention is directed to compounds of Formulae (I), (II), (III), (IV), (V), (VI), (VII), and (VIII), pharmaceutical compositions thereof and methods of use thereof in the treatment of conditions associated with a dysfunction in proteostasis.Type: ApplicationFiled: December 8, 2011Publication date: August 23, 2012Inventors: Bradley Tait, Christopher Borella, Robert Chambers, Matthew Cullen
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Publication number: 20120196880Abstract: Disclosed herein are novel antioxidant inflammation modulators, including those of the formula: wherein the variables are defined herein. Also provided are pharmaceutical compositions, kits and articles of manufacture comprising such compounds. Methods and intermediates useful for making the compounds, and methods of using the compounds and compositions thereof are also provided.Type: ApplicationFiled: December 19, 2011Publication date: August 2, 2012Inventors: Eric Anderson, Gary L. Bolton, Bradley Caprathe, Xin Jiang, Chitase Lee, William H. Roark, Melean Visnick
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Publication number: 20120190673Abstract: The invention provides a compound of the formula (I): or a salt, solvate, tautomer or N-oxide thereof, wherein M is selected from a group D1 and a group D2: and R?, E, A and X are as defined in the claims. Also provided are pharmaceutical compositions containing the compounds, processes for making the compounds and the use of the compounds in the prophylaxis or treatment of a disease state mediated by a CDK kinase, GSK-3 kinase or Aurora kinase.Type: ApplicationFiled: December 19, 2011Publication date: July 26, 2012Applicant: ASTEX THERAPEUTICS LIMITEDInventors: Valerio BERDINI, Maria Grazia CARR, Adrian Liam GILL, Steven HOWARD, Eva Figueroa NAVARRO, Gary TREWARTHA, David Charles REES, Mladen VINKOVIC, Paul Graham WYATT
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Patent number: 8222259Abstract: Compounds of the Formula I wherein R1 and R2 together with the carbon atoms to which they are bonded optionally form a further heteroaromatic ring of the formula (II) as well as pharmaceutically acceptable salts, solvates, esters and prodrugs thereof are adenosine A2a receptor antagonists and, therefore, are useful in the treatment of central nervous system diseases, in particular Parkinson's disease.Type: GrantFiled: March 3, 2009Date of Patent: July 17, 2012Assignee: Schering CorporationInventors: Joel M. Harris, Bernard R. Neustadt, Jinsong Hao, Andrew W. Stamford
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Publication number: 20120178915Abstract: This invention relates with the arylheterocycle-fused pyrimidines, derivatives and analogs of formula I: or stereoisomers, tautoers, prodrugs, pharmaceutically acceptable salts, complex salts or solvates thereof, wherein: A-cycle is of 3-8 saturated or unsaturated arylheterocycles or aliheterocyclic, containing 1-4 heteroatoms, B-cycle 5-8 member saturated or unsaturated heterocycle containing 1-4 heteroatoms; X1, X2, X3, X4 are, independently at each occurrence, C, O, S, Se, N and P elements; R1, R2, R3 is a substituent containing alicyclic group, arylcycle group, heterocyclic group, adamantane alkyl, adamantane heterocycle, adamantane analogs, sugar group, hydroxyl group, amino acid group or a combination of the above substituents. This invention also relates with their preparative methods and applications.Type: ApplicationFiled: December 24, 2009Publication date: July 12, 2012Inventor: Lifeng Xu
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Patent number: 8207172Abstract: The invention relates to novel heterocycles of formula (I) processes for their preparation and their use for preparing medicaments for the treatment or prophylaxis of disorders, especially of hyperproliferative disorders.Type: GrantFiled: August 19, 2005Date of Patent: June 26, 2012Assignee: Bayer Intellectual Property GmbHInventors: Chengzhi Zhang, Jacques Dumas, Qingming Zhu, Roger Smith, Qingjie Liu, Sharad Verma, Jason Duquette, Qian Zhao, Dongping Fan, Georgiy Bondar, Philip Coish
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Patent number: 8207173Abstract: Provided are compounds of the formula: wherein RN1 is a substituent of formula G1-NX1X2, wherein G1 is an optionally further substituted alkylene, which optionally forms, together with RN2, a cyclic group, and each of X1 and X2 is independently H or an N-substituent, or X1 and X2 together form a heterocyclic ring, or X1 together with G1 forms a cyclic group and X2 is H or an N-substituent; and each of Z1, Z2, Z3 and Z4 is H or a substituent, or two of Z1, Z2, Z3 and Z4 together form an optionally substituted ring, and further wherein at least one of Z1, Z2, Z3 and Z4 is other than H, and salts thereof, pharmaceutical compositions and methods of using the compounds. The compounds have antiviral activity.Type: GrantFiled: November 17, 2009Date of Patent: June 26, 2012Assignee: Isis Pharmaceuticals, Inc.Inventors: Punit P. Seth, Elizabeth Anne Jefferson, Richard H. Griffey, Eric E. Swayze
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Patent number: 8193528Abstract: The present invention relates to electronic devices, especially electroluminescent devices, comprising azapyrenes of formula (I), or formula (III), wherein Y1, Y2, Y3, Y4, X1, X2 and X3 are independently each other N, or CR4, with the proviso that at least one of the groups X1, X2 and X3 is a group CR4, R1 is hydrogen, F, —SiR100R101R102, or an organic substituent, R4 is hydrogen, F, —SiR100R101R102, or an organic substituent, or any of the substituents R1, R1? and R4, which are adjacent to each other, together form an aromatic, or heteroaromatic ring, or ring system, which can optionally be substituted, m is an integer of 1 to 6, and R100, R101 and R102 are independently of each other a C1-C8alkyl group, a C6-C24aryl group, or a C7-C12aralkyl group, which may optionally be substituted, and Q is a linking group; with the proviso that in the compound of formula (III) at least one of the substituents R1, or R4 is a group Q; especially as host for phosphorescent emitters, electron transporting materials, or emitType: GrantFiled: June 23, 2009Date of Patent: June 5, 2012Assignee: BASF SEInventors: Thomas Schäfer, Thomas Eichenberger, Kristina Bardon, Andrea Ricci, Natalia Chebotareva
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Publication number: 20120134955Abstract: The invention is to provide a novel anticancer agent or sensitizer for cancer chemotherapy or radiotherapy. A compound of a general formula (I): wherein A means an aryl group or a heteroaryl group, or a group of a formula (a):; R1 means a —(C?O)aOb(C1-C6)alkyl group, a —(C?O)aOb(C2-C6)alkenyl group, a —(C?O)aOb(C3-C6)cycloalkyl group, an aryl group or a heteroaryl group; R2 and R3 each mean a hydrogen atom, a halogen atom, a hydroxyl group, a carboxyl group, a —(C?O)aOb(C1-C6)alkyl group or a group of —(C?O)aN(R1e)R2e; R4 means a hydrogen atom or a (C1-C6)alkyl group, and the like have an excellent Wee 1-kinase-inhibitory effect, and are therefore useful in the field of medicine, especially in the field of various cancer treatments.Type: ApplicationFiled: February 18, 2010Publication date: May 31, 2012Inventors: Yasuhiro Goto, Kenji Niyama, Satoshi Sunami, Keiji Takahashi
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Publication number: 20120115848Abstract: The present invention provides compounds having a structure according to Formula (I): or a salt or solvate thereof, wherein ring A, U1, U2, U3, R2, R3 and R4 are defined herein. The invention further provides pharmaceutical compositions including the compounds of the invention and methods of making and using the compounds and compositions of the invention, e.g., in the treatment and prevention of various disorders, such as Parkinson's disease.Type: ApplicationFiled: October 6, 2011Publication date: May 10, 2012Applicant: ELAN PHARMACEUTICALS, INC.Inventors: Robert A. Galemmo, JR., Dean Richard Artis, I, Xiaocong Michael Ye, Danielle L. Aubele, Anh P. Truong, Simeon Bowers, Roy K. Hom, Yong-Liang Zhu, R. Jeffrey Neitz, Jennifer Sealy, Marc Adler, Paul Beroza, John P. Anderson
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Publication number: 20120094987Abstract: The invention relates to compounds of general formula (I); 1a, 1b, 1c and 1d. The invention also relates to a method for the production thereof, pharmaceutical preparations containing said compounds and/or physiologically compatible salts thereof which can be produced therefrom and/or solvates thereof, and to the pharmaceutical use of said compounds, salts or solvates thereof as inhibitors of phosphodiesterase 4. The compounds comprise active ingredients for the treatment of diseases which can have a positive influence by inhibiting the activity of phosphodiesterase 4 and/or TNF?-release, for example, in lymphocytes, eosinophile and basophile granulocytes, macrophages and mastocytes.Type: ApplicationFiled: October 3, 2011Publication date: April 19, 2012Inventors: Claudia Reichelt, Alexander Ludwig, Alexander Schulze, Mohammed Daghish, Siegfried Leistner, Andreas Krödel, Jochen Heinicke
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Patent number: 8153632Abstract: The present invention relates to pyrimidine compounds that are useful as anti-proliferative agents. More particularly, the present invention relates to oxygen linked and substituted pyrimidine compounds, methods for their preparation, pharmaceutical compositions containing these compounds and uses of these compounds in the treatment of proliferative disorders. These compounds may be useful as medicaments for the treatment of a number of proliferative disorders including tumors and cancers as well as other disorders or conditions related to or associated with kinases.Type: GrantFiled: November 15, 2006Date of Patent: April 10, 2012Assignee: S*BIO Pte Ltd.Inventors: Stephanie Blanchard, Cheng Hsia Angeline Lee, Harish Kumar Mysore Nagaraj, Anders Poulsen, Eric T. Sun, Yee Ling Evelyn Tan, Anthony Deodaunia William
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Publication number: 20120071450Abstract: Optionally substituted 4,5,7,8-tetrahydro-(optionally 4-thioxo or 4-imino)-(1H or 2H)-imidazo[1,2-a]pyrazolo[4,3-e]pyrimidine or 4,5,7,8,9-pentahydro-(optionally 4-thioxo or 4-imino)-(1H or 2H)-pyrimido[1,2-a]pyrazolo[4,3-e]pyrimidine compounds or Compounds of Formula (I), processes for their production, their use as pharmaceuticals and pharmaceutical compositions comprising them.Type: ApplicationFiled: December 7, 2009Publication date: March 22, 2012Inventors: Peng Li, Jun Zhao, Hailin Zheng, Lawrence Wennogle
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Patent number: 8134146Abstract: The present invention relates to heterocyclic radicals or diradicals, the dimers, oligomers, polymers, dispiro compounds and polycycles thereof, to the use thereof to organic semiconductive materials and to electronic and optoelectronic components.Type: GrantFiled: March 20, 2007Date of Patent: March 13, 2012Assignee: Novaled AGInventors: Michael Limmert, Olaf Zeika, Martin Ammann, Horst Hartmann, Ansgar Werner
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Publication number: 20120046282Abstract: The present invention provides Wall Teichoic Acid biosynthesis inhibitors such as compound 1835F03 (targocil) and related synthetic analogs. The invention also provides pharmaceutical compositions thereof and methods for treating bacterial infection and the suppression of growth of bacterial cells by administering a Wall Teichoic Acid biosynthesis inhibitor. The invention is particularly useful for the treatment of Methicillin-resistant Staphylococcus aureus (MRSA). The invention further provides procedures for the syntheses of Wall Teichoic Acid biosynthesis inhibitors. The invention also provides methods for the identification of antibacterial therapeutic agents.Type: ApplicationFiled: June 5, 2009Publication date: February 23, 2012Applicant: President and Fellows of Harvard CollegeInventors: Suzanne Walker Kahne, Jonathan G. Swoboda, Timothy C. Meredith, Kyungae Lee, Jennifer Campbell
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Publication number: 20120039913Abstract: The invention relates to Histamine H4 receptor antagonists or inhibitors of Histamine H4 receptor gene expression for the treatment and/or the prevention of vestibular disorders.Type: ApplicationFiled: December 23, 2009Publication date: February 16, 2012Applicant: INSERM (institut National de la Sante de la Recher Medicale)Inventors: Gilles Desmadryl, Christian Chabbert
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Patent number: 8093254Abstract: Disclosed are compounds of formula I (Chemical formula should be inserted here as it appears on abstract in paper form) Formula I or a stereoisomer, tautomer, or pharmaceutically acceptable salt or solvate thereof, wherein R1, R2, R3, R4, R14, V, W, X, Y, Z, p, and ring A are as described in the specification. Also disclosed is the method of inhibiting aspartyl protease, and in particular, the methods of treating cardiovascular diseases, cognitive and neurodegenerative diseases. Also disclosed are methods of treating cognitive or neurodegenerative diseases using the compounds of formula I in combination with a cholinesterase inhibitor or a muscarinic m1 agonist or m2 antagonist.Type: GrantFiled: December 10, 2007Date of Patent: January 10, 2012Assignee: Schering CorporationInventors: Zhaoning Zhu, Andrew Stamford, Mihirbaran Mandal, Xiaoxiang Liu
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Patent number: 8088788Abstract: [1,2]Imidazo[4,5-c] ring compounds (e.g., imidazo[4,5-c]quinolines, imidazo[4,5-c]naphthyridines, and imidazo[4,5-c]pyridines) substituted with a fused ring containing an oxygen and/or nitrogen atom attached at the 1- and/or 2-position, pharmaceutical compositions containing the compounds, intermediates, methods of making the compounds, and methods of use of these compounds as immunomodulators, for inducing cytokine biosynthesis in animals and in the treatment of diseases including viral and neoplastic diseases, are disclosed.Type: GrantFiled: March 14, 2007Date of Patent: January 3, 2012Assignee: 3M Innovative Properties CompanyInventors: Tushar A. Kshirsagar, Karl J. Manske, Larry R. Krepski, Joan T. Moseman, George W. Griesgraber, Sarah Johannessen Slania, Scott E. Langer, Philip D. Heppner
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Publication number: 20110288086Abstract: At least one active pharmaceutical ingredient is chosen from polycyclic quinazolines of formula V, pharmaceutically acceptable salts thereof, and hydrates of the pharmaceutically acceptable salts. The active pharmaceutical ingredients disclosed may be inhibitors of protein tyrosine kinase inhibitors and/or aurora kinase. The active pharmaceutical ingredients can be used for treating cancers susceptible to treatment with protein tyrosine kinase inhibitors and/or aurora kinase inhibitors.Type: ApplicationFiled: May 20, 2011Publication date: November 24, 2011Inventors: Jianqi Li, Zixue Zhang, Peng Xie, Qingwei Zhang
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Publication number: 20110272685Abstract: The present invention describes indenofluorene derivatives containing a heteroaromatic bridge atom as a novel class of materials having emitting and hole-transporting properties, in particular for use in the emission and/or charge-transport layer of electroluminescent devices. The invention furthermore relates to a process for the preparation of the compounds according to the invention and to electronic devices comprising same.Type: ApplicationFiled: December 22, 2009Publication date: November 10, 2011Applicant: Merck Patent GmbHInventors: Amir Hossain Parham, Christof Pflumm, Philipp Stoessel, Holger Heil, Arne Buesing
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Publication number: 20110272684Abstract: The present invention describes indenofluorene derivatives of the general formula I, II, III or IV having emitting and hole-transporting properties, in particular for use in the emission and/or charge-transport layer of electro-luminescent devices. The invention furthermore relates to a process for the preparation of the compounds according to the invention and to electronic devices comprising same.Type: ApplicationFiled: December 22, 2009Publication date: November 10, 2011Inventors: Amir Hossain Parham, Christof Pflumm, Arne Buesing, Holger Heil, Philipp Stoessel
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Publication number: 20110263616Abstract: The present invention relates to certain salts of a 11-(2-pyrrolidin-1-yl-ethoxy)-14,19-dioxa-5,7,26triaza-tetra-cyclo[19.3.1.1(2,6).1(8,12)]heptacosa-1(25),2(26),3,5,8,10,12(27),16,21,23-decaene (Compound I) which have been found to have improved properties. In particular the present invention relates to the maleate salt of this compound. The invention also relates to pharmaceutical compositions containing this salt and methods of use of the salt in the treatment of certain medical conditions.Type: ApplicationFiled: December 9, 2009Publication date: October 27, 2011Applicant: S*BIO Pte Ltd.Inventors: Brian Dymock, Cheng H. Lee, Anthony D. William
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Publication number: 20110245214Abstract: Optionally substituted 3-(thio, sulfonyl or sulfonyl)-7,8-dihydro-(1H or 2H)-imidazo[1,2-a]pyrazolo[4,3-e]pyrimidin-4(5H)-one or a substituted 3-(thio, sulfinyl or sulfonyl)-7,8,9-trihydro-(1H or 2H)-pyrimido[1,2-a]pyrazolo[4,3-e]pyrimidin-4(5H)-one compounds or Compounds of Formula (I), processes for their production, their use as pharmaceuticals and pharmaceutical compositions comprising them.Type: ApplicationFiled: December 7, 2009Publication date: October 6, 2011Inventors: Peng Li, Jun Zhao, Hailin Zeng, Lawrence Wennogle
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Patent number: 7994187Abstract: HIV inhibitory compounds of formula: salts, hydrates, solvates, N-oxides, or stereoisomers thereof, wherein A forms pyridine, pyrimidine, pyrazine, pyridazine, triazine, imidazole, pyrazole, triazole, tetrazole, oxazole, isoxazole, oxadiazole, thiazole, isothiazole, and thiadiazole; R1 is halo, cyano, nitro, C1-6alkyl, polyhaloC1-6alkyl, —C1-6alkyl-OR4, —C(?O)—R5, —C(?O)—OR4, —C(?O)—NR6R7, —OR4, —O—C(?O)—C1-6alkyl, —O—C1-6alkyl-OR4, —O—C1-6alkyl-NR6R7, —O—C1-6alkyl-O—C(?O)—C1-6alkyl, —O—C1-6alkyl-C(?O)—OR4, —O—C1-6alkyl-C(?O)—NR6R7, —NR6R7, —NR8—C(?O)—R5, —NR8—C(?O)—OR4, —NR8—C(?O)—NR6R7, —NR8—C(?O)—C1-6alkyl-C(?O)—OR4, —NR8—C1-6alkyl-OR4, —NR8—C1-6alkyl-NR6R7, —NR8—C1-6alkyl-imidazolyl, —NR8—SO2R9, —N?CH—NR6R7, —NH—C(?NH)—NH2, —SO2NR6R7, and —O—PO(OR8)2; D forms pyridine, pyrimidine, pyrazine, pyridazine, pyrrole, imidazole, pyrazole, furane, oxazole, isoxazole, thiophene, thiazole, and isothiazole; R2 is C1-6alkyl, polyhaloC1-6alkyl, halo, cyano, —COOR4, —OR4, and —NR6R7; R3 is phenyl, pyridyl, pyrimidType: GrantFiled: April 3, 2007Date of Patent: August 9, 2011Assignee: Tibotec Pharmaceuticals Ltd.Inventors: Bart Rudolf Romanie Kesteleyn, Wim Bert Griet Schepens
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Publication number: 20110186821Abstract: The present invention relates to electronic devices, especially electroluminescent devices, comprising azapyrenes of formula (I), or formula (III), wherein Y1, Y2, Y3, Y4, X1, X2 and X3 are independently each other N, or CR4, with the proviso that at least one of the groups X1, X2 and X3 is a group CR4, R1 is hydrogen, F, —SiR100R101R102, or an organic substituent, R4 is hydrogen, F, —SiR100R101R102, or an organic substituent, or any of the substituents R1, R1? and R4, which are adjacent to each other, together form an aromatic, or heteroaromatic ring, or ring system, which can optionally be substituted, m is an integer of 1 to 6, and R100, R101 and R102 are independently of each other a C1-C8alkyl group, a C6-C24aryl group, or a C7-C12aralkyl group, which may optionally be substituted, and Q is a linking group; with the proviso that in the compound of formula (III) at least one of the substituents R1, or R4 is a group Q; especially as host for phosphorescent emitters, electron transporting materials, or emitType: ApplicationFiled: June 23, 2009Publication date: August 4, 2011Applicant: BASF SEInventors: Thomas Schäfer, Thomas Eichenberger, Kristina Bardon, Andrea Ricci, Natalia Chebotareva
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Publication number: 20110172224Abstract: The invention relates to novel heterocycles of formula (I) processes for their preparation and their use for preparing medicaments for the treatment or prophylaxis of disorders, especially of hyperproliferative disorders.Type: ApplicationFiled: August 19, 2005Publication date: July 14, 2011Applicant: Bayer Pharmaceuticals CorporationInventors: Chengzhi Zhang, Jacques Dumas, Qingming Zhu, Roger Smith, Qingjie Liu, Sharad Verma, Jason Duquette, Qian Zhao, Dongping Fan, Georgiy Bondar, Philip Coish
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Publication number: 20110152256Abstract: Compounds of the Formula I wherein R1 and R2 together with the carbon atoms to which they are bonded optionally form a further heteroaromatic ring of the formula (II) as well as pharmaceutically acceptable salts, solvates, esters and prodrugs thereof are adenosine A2a receptor antagonists and, therefore, are useful in the treatment of central nervous system diseases, in particular Parkinson's disease.Type: ApplicationFiled: March 3, 2009Publication date: June 23, 2011Inventors: Joel M. Harris, Bernard R. Neustadt, Hong Liu, Jinsong Hao, Andrew W. Stamford
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Publication number: 20110143387Abstract: Luminescent labels based on aromatic and heterocyclic compounds, including reactive intermediates used to synthesize these compounds, and methods of synthesizing and using these reporter compounds. These labels combine high photostabilities, large Stokes' shifts and contain a pyrimidinium moiety as a water-soluble group. These luminescent compounds relate generally to the following structure: The methods relate generally to the synthesis and/or use of reporter compounds for fluorescence lifetime or fluorescence polarization based applications.Type: ApplicationFiled: October 18, 2010Publication date: June 16, 2011Inventors: Leonid D. Patsenker, Inna G. Yermolenko, Iryna A. Fedyunyaeva, Yelena N. Obukhova, Olga N. Semenova, Ewald A. Terpetschnig
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Publication number: 20110127513Abstract: The present invention provides a novel nitrogen-containing heterocyclic derivative and an organic electronic device using the same. The organic electronic device according to the present invention has excellent properties in terms of efficiency, driving voltage, and a life span.Type: ApplicationFiled: November 3, 2009Publication date: June 2, 2011Applicant: LG CHEM, LTD.Inventors: Dong-Hoon Lee, Tae-Yoon Park, Jae-Soon Bae, Hyun Nam, Jun-Gi Jang, Sung-Kil Hong
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Publication number: 20110130305Abstract: Provided are dyes and compositions which are useful in a number of applications, such as the detection and monitoring protein aggregation, kinetic studies of protein aggregation, neurofibrillary plaques analysis, evaluation of protein formulation stability, protein thermal stability shift assay and analysis of molecular chaperone activity. These dyes and compositions are also useful as probes in nucleic acid and protein detection.Type: ApplicationFiled: November 30, 2009Publication date: June 2, 2011Inventors: Wayne Forrest Patton, Sergiy M. Yarmoluk, Praveen Pande, Vladyslava Kovalska, Lijun Dai, Kateryna Volkova, Jack Coleman, Mykhaylo Losytskyy, Anthony Ludlum, Anatoliy Balanda
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BENZENESULFONYL-CHROMANE, THIOCHROMANE, TETRAHYDRONAPHTHALENE AND RELATED GAMMA SECRETASE INHIBITORS
Publication number: 20110110948Abstract: Disclosed are novel gamma secretase inhibitors of the formula (I): or a pharmaceutically acceptable salt, solvate, or ester thereof, wherein L1, n, X, Ar, Y, Z, Q, and Q1 are as defined herein. Also disclosed are methods for inhibiting gamma secretase, methods for treating Alzheimer's disease, methods of treating one or more neurodegenerative diseases, and methods of inhibiting the deposition of amyloid protein (e.g., amyloid beta protein) in, on or around neurological tissue (e.g., the brain) using the compounds of formula 1.0.Type: ApplicationFiled: July 15, 2008Publication date: May 12, 2011Applicant: SCHERING CORPORATIONInventors: Thavalakulamgara K. Sasikumar, Duane A. Burnett, Theodros Asberom, Wen-Lian Wu, Hongmei Li, Ruo Xu, Hubert B. Josien -
Publication number: 20110092701Abstract: The invention relates to the improvement of organic electroluminescent devices, in which compounds that are represented by formula (1) are used, in particular as hole injection materials or hole transport materials in a hole injection layer or hole transport layer.Type: ApplicationFiled: March 5, 2009Publication date: April 21, 2011Applicant: Merck Patent GmbHInventors: Christof Pflumm, Arne Buesing, Amir Hossain, Rocco Fortte, Holger Heil, Philipp Stoessel
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Publication number: 20110086834Abstract: Selected compounds are effective for prophylaxis and treatment of inflammation and inflammatory disorders, such as NIK-mediated disorders. The invention encompasses novel compounds, analogs, prodrugs and pharmaceutically acceptable salts thereof, pharmaceutical compositions and methods for prophylaxis and treatment of diseases and other maladies or conditions involving, inflammation and the like.Type: ApplicationFiled: June 26, 2009Publication date: April 14, 2011Applicant: AMGEN INC.Inventors: Guoqing Chen, Timothy D. Cushing, Paul Faulder, Benjamin Fisher, Xiao He, Kexue Li, Zhihong Li, Wen Liu, Lawrence R. Mcgee, Vatee Pattaropong, Jennifer L. Seganish, Youngshook Shin, Zhulun Wang
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Patent number: 7888505Abstract: The present invention relates to a 6,7-dihydrobenzimidazo[1,2-c]quinazolin-6-one carboxylic acid and its esters of the general structural formula (I), and provides a method for their synthesis (I) where R and each R? are selected independently from the list comprising —H—CH3, —C2H5, —C3H7, -iso-C3H7, —CH2CH2CH2CH3, —CH(CH3)CH2CH3, —CH2CH(CH3)CH3 and —C(CH3)3; n is 1, 2, 3 or 4; Y is a substituent selected from the list comprising —CH3, —C2H5, —NO2, —Cl, —Br, —F, —CF3, —CN, —OH, —OCH3, —OC2H5, —OCOCH3, —OCN, —SCN, —NH2, —NHCOCH3; and z is 0, 1, 2, 3 or 4.Type: GrantFiled: January 15, 2007Date of Patent: February 15, 2011Assignee: Crysoptix, KKInventors: Tatyana Doutova, Pavel I. Lazarev, Elena N. Sidorenko, Valery S. Kuzmin
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Publication number: 20110009404Abstract: The present invention relates to compounds of Formula (Ia) or (Ib), the N-oxide forms, pharmaceutically acceptable addition salts, quaternary amines, stereoisomers, tautomers, racemics, metabolites, prodrugs, hydrates, or solvates thereof, wherein Y1, m, n, R1; X1; X2; R2; X3; X4; R3; and R4 have the meaning defined in the claims. The present invention also relates to processes for preparing said compounds, pharmaceutical compositions containing them and their use in therapy. The invention particularly relates to compounds that are kinase inhibitors useful for the treatment of disease states mediated by kinase, especially PLK4, in particular such compounds that are useful in the treatment of pathological processes which involve an aberrant cellular proliferation, such as tumor growth, rheumatoid arthritis, restenosis and atherosclerosis.Type: ApplicationFiled: March 9, 2009Publication date: January 13, 2011Inventors: Peter Jacobus Johannes Buijnsters, Marc Gustaaf Celine Verdonck, Kristof Van Emelen, Pascal Ghislain André Bonnet