Chalcogen Or Nitrogen Bonded Directly At 1-, 2- Or 3-position Of The Diazole Ring By Nonionic Bonding Patents (Class 514/395)
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Publication number: 20120277193Abstract: Combinations of compounds are provided that produce a synergistic effect when administered.Type: ApplicationFiled: September 20, 2010Publication date: November 1, 2012Applicant: PRESIDENT AND FELLOWS OF HARVARD COLLEGEInventors: Frederick P. Roth, Murat Cokol, Hon Nian Chua
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Patent number: 8293774Abstract: The present invention relates to an optically active (R)-aryloxypropionic acid amide compound which has high selectivity and safety for protecting a crop such as rice, wheat, barley and soy bean, and exhibits excellent herbicidal activity against weeds, and a herbicidal composition comprising the same.Type: GrantFiled: July 2, 2008Date of Patent: October 23, 2012Assignee: Kyung Nong CorporationInventors: Joo-kyung Kim, Dong-hoo Kim, Hyung-ho Kim, Kyung-hyun Kim, Cheol-su Yoon, In-cheon Hwang
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Publication number: 20120264760Abstract: One aspect of the present invention relates to compounds, and pharmaceutically acceptable salts and prodrugs thereof, that are useful as inhibitors of IMPDH. The invention also provides pharmaceutical compositions comprising the compounds of the invention which selectively inhibit parasitic IMPDH. In certain embodiments, the present invention relates to selective inhibition of C. parvum inosine-5?-monophosphate-dehydrogenase over human inosine-5?-monophosphate-dehydrogenase (IMPDH type I and type II). These compounds may be used alone or in combination with other therapeutic or prophylactic agents, such as anti-virals, anti-inflammatory agents, antimicrobials and immunosuppressants.Type: ApplicationFiled: June 6, 2012Publication date: October 18, 2012Applicants: University of Georgia Research Foundation, Inc., Brandeis UniversityInventors: Lizbeth K. Hedstrom, Boris Striepen
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Patent number: 8273740Abstract: The invention relates to 2-sulfanyl-benzoimidazol-1-yl-acetic acid derivatives and their use as potent “chemoattractant receptor-homologous molecule expressed on Th2 cells” antagonists in the treatment of prostaglandin mediated diseases, to pharmaceutical compositions containing these derivatives and to processes for their preparation.Type: GrantFiled: August 23, 2005Date of Patent: September 25, 2012Assignee: Actelion Pharmaceuticals, Ltd.Inventors: Heinz Fretz, Markus Gude, Kurt Hilpert, Julien Pothier, Markus Riederer, Matthias Steger
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Publication number: 20120238516Abstract: The present invention relates to anthelmintic compositions comprising two or more anthelmintic active agents selected from one or more of the following groups; imidazothiazoles such as levamisole, benzimidazoles such as oxfendazole, or fenbendazole, macrocylic lactones such as ivermectin or avermectin, salicylanilides, and praziquantel. The composition being in the form of stable granules that are readily dispersible in water so as to provide a homogenous mixture of the anthelmintic agents suitable for administration. Methods of preparing the composition are also described.Type: ApplicationFiled: March 7, 2012Publication date: September 20, 2012Inventors: Douglas Robert Cleverly, Debashis Mukhopadhyay
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Publication number: 20120214786Abstract: This invention relates to compounds of formula I their use as inhibitors of the microsomal prostaglandin E2 synthase-1 (mPGES-1), pharmaceutical compositions containing them, and their use as medicaments for the treatment and/or prevention of inflammatory diseases and associated conditions. A, M, W, R1, R2, R6, R7, R8 have meanings given in the description.Type: ApplicationFiled: August 17, 2011Publication date: August 23, 2012Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Henning PRIEPKE, Henri DOODS, Raimund KUELZER, Roland PFAU, Dirk STENKAMP, Benjamin PELCMAN, Robert ROENN
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Publication number: 20120213830Abstract: This invention is directed to a pharmaceutical composition for drinking water administration comprising benzimidazole carbamate particles having an effective average particle size of less than 450 mm and a Tween-type surfactant; a method for making the composition; use of the composition to make a medicament for controlling parasites; and use of said composition for the manufacture of a medicament or protecting animal from parasitic infection.Type: ApplicationFiled: March 19, 2012Publication date: August 23, 2012Inventors: Carsten SCHMIDT, Mark Allan, Elizabeth Benedicte Daniele Deschamps
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Publication number: 20120214769Abstract: The present invention provides for novel compounds of Formula (I) and pharmaceutically acceptable salts and co-crystals thereof which have glucagon receptor antagonist or inverse agonist activity. The present invention further provides for pharmaceutical compositions comprising the same as well as methods of treating, preventing, delaying the time to onset or reducing the risk for the development or progression of a disease or condition for which one or more glucagon receptor antagonist is indicated, including Type I and II diabetes, insulin resistance and hyperglycemia. The present invention also provides for processes of making the compounds of Formula I, including salts and co-crystals thereof, and pharmaceutical compositions comprising the same.Type: ApplicationFiled: April 8, 2011Publication date: August 23, 2012Applicant: METABASIS THERAPEUTICS, INC.Inventors: Jorge E. Gomez-Galeno, K. Raja Reddy, Paul D. van Poelje, Robert Huerta Lemus, Thanh Huu Nguyen, Matthew P. Grote, Qun Dang, Scott J. Hecker, Venkat Reddy Mali, Mingwei Chen, Zhili Sun, Serge Henri Boyer, Haiqing Li, William Craigo
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Publication number: 20120214856Abstract: The present invention provides methods for the treatment of tumors, comprising administration of an effective amount of at least one taxoid and an effective amount of at least one benzimidazol carbamate compound of formula (I). The invention also provides a method for the treatment of tumors insensitive to one or more anti-mitotic drugs, the method comprising administering a effective amount of at least one benzimidazole carbamate compound of formula (I). Also provide are compositions for carrying out methods of the invention.Type: ApplicationFiled: April 27, 2012Publication date: August 23, 2012Applicant: NEWSOUTH INNOVATIONS PTY LIMITEDInventors: David L. Morris, Mohammad Hossein Pourgholami
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Patent number: 8247440Abstract: The present disclosure relates to pharmaceutical compositions comprising omeprazole, lansoprazole and at least one buffering agent.Type: GrantFiled: February 19, 2009Date of Patent: August 21, 2012Assignee: Curators of the University of MissouriInventor: Jeffrey O. Phillips
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Patent number: 8242157Abstract: Disclosed are compounds, compositions and methods for treating various diseases, syndromes, conditions and disorders, including pain. Such compounds are represented by Formula I as follows: wherein R0, R1, R2, R3, R4 and a are defined herein.Type: GrantFiled: June 10, 2010Date of Patent: August 14, 2012Assignee: Janssen Pharmaceutica NVInventors: Michele C. Jetter, Mark J. Macielag, Mingde Xia, Xiaoqing Xu
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Publication number: 20120202840Abstract: Provided are methods for treating a hematological malignancy comprising administering an effective amount of flubendazole alone or in combination with a vinca alkaloid. Also provided are compositions and kits comprising an effective amount of flubendazole and/or a vinca alkaloid for use in the methods of the disclosure.Type: ApplicationFiled: October 8, 2010Publication date: August 9, 2012Applicant: UNIVERSITY HEALTH NETWORKInventors: Aaron David Schimmer, Jiayi Hu, Paul Anthony Spangnuolo
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Publication number: 20120196897Abstract: The present invention relates to compounds of general formula I in which A, L, M, Q2, Q3, Q4, R1, R5, Ra, Rb, Rc, W, X, Y, Z1, Z2, Z3 are defined in the description, the salts thereof, particularly the physiologically acceptable salts thereof. The compounds are of potential utility in the treatment and/or prevention of inflammatory diseases and associated conditions, in particular, in the treatment and/or prevention of pain. The invention also relates to the use of such compounds as medicaments, to pharmaceutical compositions containing them, and to their preparation.Type: ApplicationFiled: April 6, 2012Publication date: August 2, 2012Applicant: Boehringer Ingelheim International GmbHInventors: Roland PFAU, Kirsten ARNDT, Henri DOODS, Klaus KLINDER, Raimund KUELZER, Dimitrijs LUBRIKS, Juergen MACK, Benjamin PELCMAN, Henning PRIEPKE, Robert ROENN, Dirk STENKAMP, Edgars SUNA
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Patent number: 8227476Abstract: The invention relates to a method for the treatment of obesity and related diseases comprising the administration of a therapeutically effective amount of Flibanserin.Type: GrantFiled: July 31, 2006Date of Patent: July 24, 2012Assignee: Sprout Pharmaceuticals, Inc.Inventors: Angelo Ceci, Marcus Schindler
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Publication number: 20120184535Abstract: A compound, a process for its preparation, a pharmaceutical composition, use of a compound, a method for modulating or regulating serine/threonine and tyrosine kinases and a serine/threonine and tyrosine kinases modulating agent. Novel small-molecule compounds with kinase inhibitory activity, having superior properties as pharmaceutical agents, production method thereof and uses thereof. In particular, new derivatives of tetrahalogenated benzimidazole with serine/threonine and tyrosine kinases inhibitory properties, preferably selected from the group of PIM, HIPK, DYRK, CLK, CDK, FLT, PKG, Haspin, MER, TAO, MNK, TRK kinases which exhibit superior pharmacological actions, and can be useful for the treatment of disease conditions, especially cancers depending on serine/threonine and tyrosine kinases, such as but not limited to leukemias and solid tumors.Type: ApplicationFiled: December 28, 2011Publication date: July 19, 2012Applicant: SELVITA S.A.Inventors: Krzysztof BRZÓZKA, Wojciech CZARDYBON, Aleksandra SABINIARZ, Mariusz MILLIK, Renata WINDAK, Adrian ZAREBSKI, Nicolas BEUZEN
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Publication number: 20120178785Abstract: Compounds, compositions and methods are provided which are useful in the treatment of conditions such as central or peripheral nervous system disorders through the modulation of potassium ion flux through voltage-dependent potassium channels and/or depressing cortical and/or peripheral neuron activity are disclosed. Novel derivatives of N-phenylanthranilic acid are also disclosed.Type: ApplicationFiled: March 20, 2012Publication date: July 12, 2012Applicant: Ramot at Tel-Aviv University Ltd.Inventors: Bernard ATTALI, Asher Peretz
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Publication number: 20120171129Abstract: Disclosure is provided for benzimidazole derivative compounds that prevent, remove and/or inhibit the formation of biofilms, compositions including these compounds, devices including these compounds, and methods of using the same.Type: ApplicationFiled: June 10, 2010Publication date: July 5, 2012Inventors: Christian Melander, Steven A. Rogers, Robert W. Huigens, III
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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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Publication number: 20120148530Abstract: An inexpensive, easily available, and convenient method of treating or preventing a virus infection is provided. The present invention relates to a method for the treatment or prevention of virus infections using polybiguanide-based compounds administering a therapeutically effective amount of a compound or a pharmaceutically acceptable salt thereof The invention relies on the unique biochemical reaction in which polybiguanide-based compounds interfere with the spread of virus within or between organisms. The compositions and formulations described in the present invention are effective means to reduce the infectivity of the human immunodeficiency virus type 1 (HIV-1), and human herpes simplex viruses, and also to kill the causative organisms of many other sexually transmitted diseases (STDs).Type: ApplicationFiled: June 21, 2010Publication date: June 14, 2012Applicant: Novaflux Biosciences, Inc.Inventors: Mohammed E. Labib, Richard F. Stockel
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Publication number: 20120149676Abstract: This invention relates to compounds of formula I their use as inhibitors of the microsomal prostaglandin E2 synthase-1 (mPGES-1), pharmaceutical compositions containing them, and their use as medicaments for the treatment and/or prevention of inflammatory diseases and associated conditions. A, L, M, W, R1, R2, R3, R4, R6, R7, R9, Ra, Rb have meanings given in the description.Type: ApplicationFiled: December 8, 2011Publication date: June 14, 2012Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Henning PRIEPKE, Henri DOODS, Alexander HEIM-RIETHER, Raimund KUELZER, Roland PFAU, Klaus RUDOLF, Dirk STENKAMP
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Publication number: 20120136002Abstract: A compound of formula (I) wherein R1 to R15, P1, P2, A, B and Q are as defined in the claims and pharmaceutically acceptable salts and esters thereof, are disclosed. The compounds of formula (I) possess utility as matriptase inhibitors and are useful in the treatment of matriptase dependent conditions, particularly cancer.Type: ApplicationFiled: May 18, 2010Publication date: May 31, 2012Inventors: Rajeev Goswami, Anil Kumar Vuppala, Ramesh Veludandi, Ramesh Sistla, Chakshusmathi Ghadiyaram, Muralidhara Ramachandra
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Publication number: 20120135987Abstract: This invention is directed to compounds, which are PDE10A enzyme inhibitors. The invention provides a pharmaceutical composition comprising a therapeutically effective amount of a compound of the invention and a pharmaceutically acceptable carrier. The present invention also provides processes for the preparation of the compounds of formula I. The present invention further provides a method of treating a subject suffering from a neurodegenerative disorder comprising administering to the subject a therapeutically effective amount of a compound of formula I. The present invention also provides a method of treating a subject suffering from a drug addiction comprising administering to the subject a therapeutically effective amount of a compound of formula I. The present invention further provides a method of treating a subject suffering from a psychiatric disorder comprising administering to the subject a therapeutically effective amount of a compound of formula I.Type: ApplicationFiled: February 3, 2012Publication date: May 31, 2012Applicant: H. Lundbeck A/SInventors: Andreas Ritzén, Jan Kehler, Morten Langgård, Jacob Nielsen, John Paul Kilburn, Mohamed M. Farah
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Publication number: 20120121664Abstract: An oral pharmaceutical dosage form comprises pharmacologically effective amounts of an acid-susceptible proton pump inhibitor and an H2 receptor antagonist in combination with at least on pharmacologically acceptable excipient which causes a delayed release and/or an extended release of the proton pump inhibitor. The H2 receptor antagonist is included in the dosage for in such a way that it is rapidly released after administration. This dosage form is suitable for the treatment of conditions associated with an excessive secretion of gastric acid and provides a suitable combination of a rapid onset and a long-lasting duration of the effect. The invention also relates to a method for manufacturing such a dosage form and to a method for the treatment of conditions associated with the secretion of gastric acid.Type: ApplicationFiled: January 23, 2012Publication date: May 17, 2012Applicant: OREXO ABInventors: Anders Pettersson, Christer Nyström, Yvonne Hakansson
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Publication number: 20120122852Abstract: The invention concerns tricyclic N-heteroaryl-carboxamide derivatives containing a benzimidazole unit of general formula (I): Wherein A, P, Y, R1, R2 and R3 are as defined herein. The invention also concerns a method of preparing the compounds and their therapeutic use.Type: ApplicationFiled: January 24, 2012Publication date: May 17, 2012Applicant: SANOFI-AVENTISInventors: Laurent DUBOIS, Yannick EVANNO, Luc EVEN, Catherine GILLE, Andre MALANDA, David MACHNIK, Nathalie RAKOTOARISOA
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Patent number: 8178694Abstract: Heterocyclylaminoalkyl Substituted Benzimidazoles Inhibitors of RSV replication of formula (I): The salts and stereochemically isomeric forms thereof, wherein Q is hydrogen, C1-6alkyl optionally substituted with a heterocycle or Q is C1-6alkyl substituted with both —OR4 and a heterocycle; wherein said heterocycle is oxazolidine, thiazolidine, 1-oxo-thiazolidine, 1,1-dioxothiazolidine, morpholinyl, thiomorpholinyl, 1-oxo-thiomorpholinyl, 1,1-dioxothiomorpholinyl, hexahydrooxazepine, hexahydrothiazepine, 1-oxo-hexahydrothiazepine, 1,1-dioxo-hexahydrothiazepine, pyrrolidine, piperidine, homopiperidine, piperazine; which heterocyle may be substituted with 1-2 substituents; each Alk is C1-6alkanediyl; R1 is Ar or optionally substituted piperidinyl, piperazinyl, morpholinyl, thiomorpholinyl, pyridyl, pyrazinyl, pyridazinyl, pyrimidinyl, furanyl, tetrahydrofuranyl, thienyl, pyrrolyl, thiazolyl, oxazolyl, imidazolyl, isothiazolyl, pyrazolyl, isoxazo lyl, oxadiazolyl, quinolinyl, quinoxalinyl, benzofuranyl, benzothienType: GrantFiled: June 20, 2006Date of Patent: May 15, 2012Assignee: Tibotec Pharmaceuticals Ltd.Inventors: Jean-François Bonfanti, Philippe Muller, Jérôme Michel Claude Fortin, Frédéric Marc Maurice Doublet
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Publication number: 20120115903Abstract: Substituted heteroaromatic carboxamide and urea compounds corresponding to formula (i) processes for the preparation thereof, pharmaceutical compositions containing these compounds and also a method of using these compounds in pharmaceutical compositions for treating or inhibiting pain and other conditions mediated at least in part via the vanilloid receptor 1.Type: ApplicationFiled: November 9, 2011Publication date: May 10, 2012Applicant: Gruenenthal GmbHInventors: Robert Frank, Thomas Christoph, Bernhard Lesch, Jeewoo Lee
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Patent number: 8163935Abstract: There is provided a CRF receptor antagonist comprising a compound of the formula (I): wherein R1 is an optionally substituted hydrocarbyl, an optionally substituted C-linked heterocyclic group, an optionally substituted N-linked heteroaryl group, a cyano or an acyl; R2 is an optionally substituted cyclic hydrocarbyl or an optionally substituted heterocyclic group; X is oxygen, sulfur or —NR3— (wherein R3 is a hydrogen, an optionally substituted hydrocarbyl or an acyl); Y1, Y2 and Y3 are each an optionally substituted carbon or a nitrogen, provided that one or less of Y1, Y2 and Y3 is nitrogen; and Z is a bond, —CO—, oxygen, sulfur, —SO—, —SO2—, —NR4—, —NR4-alk-, —CONR4— or —NR4CO— (wherein alk is an optionally substituted C1-4 alkylene and R4 is a hydrogen, an optionally substituted hydrocarbyl or an acyl); or a salt thereof or a prodrug thereof.Type: GrantFiled: April 26, 2006Date of Patent: April 24, 2012Assignee: Takeda Pharmaceutical Company LimitedInventors: Kazuyoshi Aso, Michiyo Mochizuki, Albert Charles Gyorkos, Christopher Peter Corrette, Suk Young Cho, Scott Alan Pratt, Christopher Stephen Siedem
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Publication number: 20120083463Abstract: The present invention relates to active compound combinations consisting, firstly, of a known halogen-substituted derivative (component A) and, secondly, of further known pesticidally active compounds (component B), which active compound combinations are suitable for controlling animal and microbial pests.Type: ApplicationFiled: July 8, 2011Publication date: April 5, 2012Applicant: Bayer CropScience AGInventors: Michael MAUE, Friedrich August MÜHLTHAU, Isabelle ADELT, Markus HEIL, Peter JESCHKE, Tobias KAPFERER, Alexander SUDAU, Heike HUNGENBERG
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Publication number: 20120070413Abstract: Selected compounds are effective for prophylaxis and treatment of diseases, such as HGF mediated diseases. 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, cancer and the like. The subject invention also relates to processes for making such compounds as well as to intermediates useful in such processes.Type: ApplicationFiled: November 30, 2011Publication date: March 22, 2012Inventors: Tae-Seong KIM, David Bauer, Steven Bellon, Alessadro Boezio, Shon Booker, Deborah Choquette, Derin C. D'Amico, Noel D'Angelo, Celia Dominguez, Ingrid M. Fellows, Julie Germain, Russell Graceffa, Jean-Christophe Harmange, Satoko Hirai, Daniel La, Matthew Lee, Longbin Liu, Mark H. Norman, Michele Potashman, Philip Roveto, Aaron C. Siegmund, Ning Xi, Kevin Yang
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Patent number: 8138177Abstract: This invention relates to compounds of the formula (I): or pharmaceutically acceptable salts thereof, wherein: A, B, R1, R2 and R3 are each as described herein, and compositions containing such compounds and the use of such compounds in the treatment of a condition mediated by CB2 receptor binding activity such as, but not limited to, inflammatory pain, nociceptive pain, neuropathic pain, fibromyalgia, chronic low back pain, visceral pain, acute cerebral ischemia, pain, chronic pain, acute pain, post herpetic neuralgia, neuropathies, neuralgia, diabetic neuropathy, HIV-related neuropathy, nerve injury, rheumatoid arthritic pain, osteoarthritic pain, back pain, cancer pain, dental pain, fibromyalgia, neuritis, sciatica, inflammation, neurodegenerative disease, cough, broncho constriction, irritable bowel syndrome (IBS), inflammatory bowel disease (IBD), colitis, cerebrovascular ischemia, emesis such as cancer chemotherapy-induced emesis, rheumatoid arthritis, asthma, Crohn's disease, ulcerative colitis, asthmaType: GrantFiled: March 2, 2006Date of Patent: March 20, 2012Assignee: Pfizer Inc.Inventors: Kazuo Ando, Makoto Kawai, Tsutomu Masuda, Hirofumi Omura
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Publication number: 20120064008Abstract: An in vivo assay for assessing the metastatic potential of cancer cells has been developed. This is a functional assay that also allows for screening of compounds that are selective for metastatic cancer. Metastatic cancer is established in animals by intravenous injection of metastatic cancer cells before treatments are tested. This assay has been used to identify benzimidazoles for the treatment of metastatic prostate cancers. The benzimidazole(s) can be formulated for enteral or parenteral administration. In one embodiment, the compositions are formulated for parenteral administration. Compositions containing a benzimidazole exhibit greater cytotoxicity against cell lines prone to metastasis than against cells lines that are less prone to metastasis in vitro. The benzimidazoles described herein were effective at treating metastatic prostate cancer in bone.Type: ApplicationFiled: May 20, 2010Publication date: March 15, 2012Inventors: Bruce Zetter, Ivy Chung, Courtney Barrows
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Publication number: 20120064052Abstract: Three types of trisiloxane surfactants having the basic formula: MDM? are described wherein the substituents on the differing M and M? groups, in conjunction with pendant polyalkylene oxide substituents on the D group render the surfactant resistant to hydrolysis under either basic or acidic conditions outside the pH range of 6.0 to 7.5. The compositions are useful in agricultural, household and cosmetic applications.Type: ApplicationFiled: June 22, 2011Publication date: March 15, 2012Applicant: Momentive Performance Materials Inc.Inventors: George A. Policello, Mark D. Leatherman, Wenqing Peng, Suresh K. Rajaraman, Sophia Xia
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Publication number: 20120046329Abstract: Disclosed herein are compositions and methods relating to modulators of Nod-like Receptors NOD1 (NLRC1) and NOD2 (NLRC2) signaling. Further provided are methods of identifying modulators of Nod-like Receptors NOD1 and NOD2 activity. Further provided are compositions and methods for treating or preventing inflammation, including diseases associated with inflammation such as inflammatory bowel diseases (Crohn's disease, ulcerative colitis), pancreatitis, arthritis, asthma, psoriasis. Alzheimer's disease, cardiovascular disease (arteritis), diabetes, and sepsis.Type: ApplicationFiled: August 10, 2011Publication date: February 23, 2012Inventors: Gregory Paul Roth, Ricardo Garcia Correa, Pasha Moeenuddin Khan, John Christian Reed
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Patent number: 8119676Abstract: The present invention relates to novel benzimidazolone derivatives of the general formula (I) in which the substituents R1, R2, R3, A1, A2, and B are as defined in claim 1, medicaments comprising these, and the use thereof for the prophylaxis and/or treatment of vasopressin-dependent diseases.Type: GrantFiled: August 24, 2007Date of Patent: February 21, 2012Assignee: Abbott GmbH & Co. HGInventors: Torsten Arndt, Thorsten Oost, Wilfried Lubisch, Wolfgang Wernet, Alfred Hahn, legal representative, Wilfried Hornberger, Liliane Unger, Juliana Ruiz Caro
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Patent number: 8110571Abstract: This invention relates to benzimidazole and benzothiazole compounds of formula (I) to methods of preparing such compounds, pharmaceutical compositions comprising such compounds, and to methods of treatment comprising administering of such compounds.Type: GrantFiled: March 25, 2008Date of Patent: February 7, 2012Assignee: Aventis Pharma S.A.Inventors: Conception Nemecek, Francois Clerc
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Publication number: 20120024743Abstract: The present invention relates to semisolid transdermal pharmaceutical preparation having enhanced stability and bioavailability, wherein the particles are coated by a volatile silicon oil component and the thus obtained suspension is dispersed in a gel or cream base.Type: ApplicationFiled: February 5, 2010Publication date: February 2, 2012Applicant: EGIS GYOGYSZERGYAR NYILVANOSAN MUKODO RESZVENYTARSASAGInventors: Endre Mikulasik, Patrik Fazekas
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Publication number: 20120022121Abstract: Indole derivatives and analogous compounds and pharmaceutical compositions comprising the same are provided. Also provided are methods of using these compounds to inhibit tubulin polymerization in a cell associated with a proliferative disease or to treat cancer, metastatic cancer, resistant cancer or multidrug resistant cancer, including inter-alia: prostate cancer, breast cancer, melanoma, colon cancer and bladder cancer.Type: ApplicationFiled: July 25, 2011Publication date: January 26, 2012Inventors: James T. DALTON, Duane D. MILLER, Sunjoo AHN, Charles DUKE, Dong Jin HWANG, Jun YANG
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Publication number: 20120015910Abstract: Novel active compound combinations comprising a carboxamide of the general formula (I) (group 1) in which A, R1, R2 and R3 are as defined in the description, and the active compound groups (2) to (23) listed in the description have very good fungicidal properties.Type: ApplicationFiled: September 23, 2011Publication date: January 19, 2012Applicant: Bayer CropScience AGInventors: Ulrike Wachendorff-Neumann, Peter Dahmen, Ralf Dunkel, Hans-Ludwig Elbe, Anne Suty-Heinze, Heiko Rieck
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Publication number: 20120015911Abstract: Methods, compounds, pharmaceutical compositions and kits are described for treating or preventing amyloid-related disease.Type: ApplicationFiled: September 20, 2011Publication date: January 19, 2012Applicant: Bellus Health Inc.Inventors: Xianqi Kong, Xinfu Wu, Abderrahim Bouzide, Isabelle Valade, David Migneault, Francine Gervais, Daniel Delorme, Benoit Bachand, Mohamed Atfani, Sophie Levesque, Bita Samim
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Patent number: 8097758Abstract: The invention relates to the compounds of formula (I) having antithrombotic activity which especially inhibit blood clotting factor IXa, to methods for producing the same and to the use thereof as drugs.Type: GrantFiled: March 9, 2009Date of Patent: January 17, 2012Assignee: Sanofi-AventisInventors: Henning Steinhagen, Markus Follmann, Jochen Goerlitzer, Herman Schreuder
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Publication number: 20120010222Abstract: The present invention relates to methods of treating, preventing, or lessening the severity of resistant bacterial infections in mammals, utilizing compounds of formula I or formula VII or pharmaceutically salts thereof. The present invention also relates to methods of using compounds of formula I or formula VII in combination with one or more additional antibacterial agents and/or one or more additional therapeutic agents that increase the susceptibility of bacterial organisms to antibiotics.Type: ApplicationFiled: September 16, 2011Publication date: January 12, 2012Applicant: VERTEX PHARMACEUTICALS INCORPORATEDInventors: Paul Charifson, David Deininger, Anne-Laure Grillot, Yusheng Liao, Steven Ronkin, Dean Stamos, Emanuele Perola, Tiansheng Wang, Arnaud Le Tiran, Joseph Drumm
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Patent number: 8088767Abstract: This invention relates to the field of protein tyrosine kinases and inhibitors thereof. In particular, the invention relates to inhibitors of JAK-2, pharmaceutical compositions of the compounds for inhibiting JAK-2, methods of inhibiting JAK-2 in a cell, comprising contacting a cell in which inhibition of JAK-2 is desired with a compound or pharmaceutical composition comprising a compound according to the invention. The also comprises methods of treating a disease or condition that involves JAK-2 comprising administering to a patient a pharmaceutical composition comprising a compound according to the invention.Type: GrantFiled: September 28, 2007Date of Patent: January 3, 2012Assignee: Exelixis, Inc.Inventors: Adam Antoni Galan, Jeff Chen, Hongwang Du, Timothy Forsyth, Tai Phat Huynh, Henry William Beecroft Johnson, Patrick Kearney, James W. Leahy, Matthew Sangyup Lee, Grace Mann, Brian Hugh Ridgway, Craig Stacy Takeuchi, Peiwen Zhou
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Publication number: 20110319456Abstract: Novel benzoarylureido compounds and a use thereof for prevention and/or treatment of the neurodegenerative brain disease are provided. The neurodegenerative brain diseases may include Alzheimer's disease, dementia, Parkinson's disease, stroke, amyloidosis, Pick's disease, Lou Gehrig's disease, Huntington's disease, Creutzfeld-Jakob disease, and the like.Type: ApplicationFiled: December 29, 2009Publication date: December 29, 2011Applicant: KOREA INSTITUTE OF SCIENCE AND TECHNOLOGYInventors: Hoh-Gyu Hahn, Kee-Dal Nam, Dong-Yun Shin, Chan-Ho Park, Sung-Woo Cho, Eun-A Kim, Ghil-Soo Nam, Kyung-Il Chol, Seon-Hee Seo, Hee-Sup Shin, Dong-JIn Kim, Ae-Nim Pae, Hye-JIn Chung, Hyun-Ah Choo, Hye-Whon Rhim, Yong-Seo Cho, Eun-Jon Roh, Gyo-Chang Keum, Kee-Hyun Choi, Kye-Jung Shin, Chan-Seong Cheong, Jae-Kyun Lee, Yong-Koo Kang, Young-Soo Kim, Woong-Seo Park, Key-Sun Kim, He-Sson Chung, Chi-Man Song, Sun-Joon Min, Eunlce Eun-Kyeong Kim, Cheol-Ju Lee, Soon-Bang Kang
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Publication number: 20110312935Abstract: There are provided compounds of formula (I), wherein R1, R6, R8, Q2, Q3, Q3a, Q4, L and A have meanings given in the description, and pharmaceutically-acceptable salts thereof, which compounds are useful in the treatment of diseases in which inhibition of the activity of a member of the MAPEG family is desired and/or required, and particularly in the treatment of inflammation and/or cancer.Type: ApplicationFiled: September 25, 2009Publication date: December 22, 2011Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Roland Pfau, Kirsten Arndt, Henri Doods, Norbert Hauel, Klaus Klinder, Raimund Kuelzer, Juergen Mack, Henning Priepke, Dirk Stenkamp
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Publication number: 20110306614Abstract: The invention relates to N-hydroxysulfonamide derivatives that donate nitroxyl (HNO) under physiological conditions and are useful in treating and/or preventing the onset and/or development of diseases or conditions that are responsive to nitroxyl therapy, including heart failure and ischemia/reperfusion injury. Novel N-hydroxysulfonamide derivatives release NHO at a controlled rate under physiological conditions, and the rate of HNO release is modulated by varying the nature and location of functional groups on the N-hydroxysulfonamide derivatives.Type: ApplicationFiled: August 19, 2011Publication date: December 15, 2011Applicants: THE JOHNS HOPKINS UNIVERSITY, CARDIOXYL PHARMACEUTICALS, INC.Inventors: John P. Toscano, Frederick Arthur Brookfield, Andrew D. Cohen, Stephen Martin Courtney, Lisa Marie Frost, Vincent Jacob Kalish
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Publication number: 20110305640Abstract: Soluble adenylyl cyclase (sAC) is implicated in proliferation of keratinocytes. Inhibitors of sAC are useful for the treatment and/or prevention of psoriasis and other hyperproliferative skin disorders. Assays to identify such compounds are also described.Type: ApplicationFiled: February 23, 2010Publication date: December 15, 2011Applicant: CORNELL UNIVERSITYInventors: Jochen Buck, Lonny Levin, Jonathan Zippin
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Patent number: 8067454Abstract: A series of novel thio-substituted anthra[1,2-d]imidazole-6,11-dione derivatives, and the preparation method and application of said derivatives, said application having a pharmaceutical composition containing said derivatives with therapeutically effective amount for treating cancer, and said application involves effects of said derivatives for inhibiting telomerase activity, inhibiting the growth of cancer cell, treating cancer and the like.Type: GrantFiled: February 25, 2010Date of Patent: November 29, 2011Assignee: National Defense Medical CenterInventor: Hsu-Shan Huang
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Patent number: 8067614Abstract: This invention is directed to the compound of formula (I), compositions containing said compounds to inhibit the sodium-proton exchanger of subtype 3 (NHE3) which are useful in the prevention or treatment of various disorders in a patient suffering from a disease state, such as, renal disorders including acute or chronic renal failure, disorders of biliary function and for respiratory disorders such as snoring or sleep apnea or for stroke.Type: GrantFiled: March 12, 2010Date of Patent: November 29, 2011Assignee: Sanofi-Aventis Deutschland GmbHInventors: Uwe Heinelt, Hans-Jochen Lang, Armin Hofmeister, Klaus Wirth, Martin Hug
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Patent number: 8067382Abstract: The invention relates to a novel formulation having the advantage of including triclabendazole in solution. In addition a further anthelmintic may be included. The formulation is made by mixing the abamectin and benzyl alcohol and mixing this with triclabendazole and butyl dioxitol. The mix is then heated to dissolve the active, and allowed to cool at which stage the solution is diluted to volume with PEG 4000. The present invention overcomes the solubility difficulties of triclabendazole and presents the triclabendazole in a solution.Type: GrantFiled: December 7, 2009Date of Patent: November 29, 2011Assignee: Merial LimitedInventor: Colin Manson Harvey
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Publication number: 20110288139Abstract: The present invention relates to substituted amino-benzimidazoles of general formula (1) wherein the groups R1 to R14 and A, are defined as in the specification and claims and the use thereof for the treatment of Alzheimer's disease (AD) and similar diseases.Type: ApplicationFiled: January 21, 2009Publication date: November 24, 2011Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Klaus Fuchs, Cornelia Dorner-Ciossek, Sandra Handschuh, Niklas Heine, Stefan Hoerer, Klaus Klinder