Chalcogen Bonded Directly To Pyrimidine At 2-position Patents (Class 514/274)
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Publication number: 20150148340Abstract: The present application relates to novel bicyclically substituted uracil derivatives, to processes for preparation thereof, to the use thereof alone or in combinations for treatment and/or prophylaxis of diseases, and to the use thereof for production of medicaments for treatment and/or prophylaxis of diseases.Type: ApplicationFiled: May 3, 2013Publication date: May 28, 2015Applicant: BAYER PHARMA AKTIENGESELLSCHAFTInventors: Chantal Fürstner, Jens Ackerstaff, Alexander Straub, Heinrich Meier, Hanna Tinel, Katja Zimmermann, Adrian Tersteegen, Dmitry Zubov, Raimund Kast, Jens Schamberger, Martina Schäfer, Kirsten Börngen
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Patent number: 9040516Abstract: The present invention provides: an uracil derivative represented by general formula (I) or a physiologically acceptable salt thereof (in the formula, R1 represents a hydrogen atom, a C1-10 alkyl group, a C2-6 alkene group or a 3- to 6-membered saturated or 4- to 6-membered unsaturated aliphatic ring group which may contain 1 to 2 hetero atoms independently selected from the group consisting of N, O and S; R2 represents a hydrogen atom, a halogen atom, a cyano group, —NRcRd, —N?CHN(CH3)2, or an C1-3 alkyl group; Ar1 and Ar2 independently represent a 5- to 6-membered aromatic ring group which may contain 1 to 3 hetero atoms independently selected from the group consisting of N, O and S; and L represents a 6-membered aromatic ring group which may contain 1 to 4 nitrogen atoms, a pyrazole group, a triazole group, or an imidazole group); and a therapeutic agent or prophylactic agent for various inflammatory diseases associated with elastase, comprises the compound or the like as an active ingredient.Type: GrantFiled: July 31, 2012Date of Patent: May 26, 2015Assignee: SUMITOMO DAINIPPON PHARMA CO., LTD.Inventors: Tomoya Shiro, Masanori Tobe, Katsumi Kubota, Yosuke Takanashi, Tomoaki Nakamura, Toshihiko Sone
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Patent number: 9040538Abstract: The present invention features compounds having the Formula (Ia) and (Ib) (e.g., a compound of any of Formulas ((Ia-2)-(Ia-21)), including other tautomers, stereoisomers, E/Z stereoisomers, prodrugs, pharmaceutically acceptable salts, and compositions thereof. The invention also features methods for treating or preventing pain (e.g., neuropathic pain), inflammation, or epilepsy in a patient by administering an effective amount of a compound of Formula (Ia) or (Ib). The invention also features a method for treating or preventing pain (e.g., neuropathic pain), inflammation, or epilepsy in a patient that includes administering to a patient in need thereof an effective amount of a compound of Formula (IIa) or (IIb) (e.g., a compound of any of Formulas ((IIa-2)-(IIa-6)). The compounds described herein (e.g., a compound of Formulas (Ia), (Ib), (IIa), or (IIb)) can also be used as anticonvulsants.Type: GrantFiled: May 21, 2010Date of Patent: May 26, 2015Assignee: Universite LavalInventors: Giorgio Attardo, Sasmita Tripathy, Martin Gagnon
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Patent number: 9040490Abstract: A cytosine analog, a method of preparation of a cytosine analog, a DNA methyltransferase 1 inhibitor, and a method for DNA methylation inhibition, is provided for the treatment of diseases associated with deviations from normal DNA methylation. The analog of cytosine may be comprised of 1, N4, 5 and 6-substituted derivatives of cytosine or 5,6-dihydrocytosine, wherein the analog can be described by the chemical formula where R1 is H, R3, R4, 2?-deoxyribosyl, R4 is alkyl or aryl, X is N or C, wherein if X in the analog of formula I is N, then R5 is no substituent and if X in the analog of formula I and/or II is C or if X in the analog of formula II is N, then R5 and R6 are independently alkyl, aryl, hydroxyalkyl, aminoalkyl, hydroxyl, carboxyl, amino group, alkoxyl, aryloxyl, aminoalkyl, aminoaryl, thio group, sulfonyl, sulfinyl or halogen.Type: GrantFiled: March 17, 2011Date of Patent: May 26, 2015Assignee: INSTYTUT CHEMII BIOORGANICZNEJ PANInventors: Jan Barciszewski, Wojciech T. Markiewicz, Ewelina Adamska, Beata Plitta, Malgorzata Giel-Pietraszuk, Eliza Wyszko, Maria Markiewicz, Agnieszka Fedoruk-Wyszomirska, Tadeusz Kulinski, Marcin Chmielewski
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Publication number: 20150139905Abstract: The present invention provides pharmacological compounds including an effector moiety conjugated to a binding moiety that directs the effector moiety to a biological target of interest. Likewise, the present invention provides compositions, kits, and methods (e.g., therapeutic, diagnostic, and imaging) including the compounds. The compounds can be described as a protein interacting binding moiety-drug conjugate (SDC-TRAP) compounds, which include a protein interacting binding moiety and an effector moiety. For example, in certain embodiments directed to treating cancer, the SDC-TRAP can include an Hsp90 inhibitor conjugated to a cytotoxic agent as the effector moiety.Type: ApplicationFiled: October 9, 2014Publication date: May 21, 2015Inventors: Dinesh Chimmanamada, Weiwen Ying
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Publication number: 20150141428Abstract: The present invention is directed to benzyl urea compounds, which are tropomyosin-related kinase (Trk) family protein kinase inhibitors, and hence may be useful in the treatment of pain, inflammation, cancer, restenosis, atherosclerosis, psoriasis, thrombosis, a disease, disorder, injury, or malfunction relating to dysmyelination or demyelination or a disease or disorder associated with abnormal activities of nerve growth factor (NGF) receptor Trk-A, Trk-B and/or Trk-C.Type: ApplicationFiled: May 17, 2013Publication date: May 21, 2015Applicant: Merck Sharp & Dohme Corp.Inventors: Shawn J. Stachel, Melissa Egbertson, Edward Brnardic, Kristen G. Jones, John M. Sanders, Darrell Henze
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Publication number: 20150141434Abstract: The invention provides compounds that are useful as sodium channel blockers. In one aspect, the invention provides compounds of Formula I: or pharmaceutically acceptable salts, solvates, hydrates, or diastereomers thereof, wherein R1, R4, X, G, n, p, W1, W2, W3, W4, and the E ring are defined in the disclosure. In certain embodiments, the invention provides compounds of Formulae II-XIII as set forth supra. The invention also provides the use of compounds of any of the above discussed formulae to treat a disorder responsive to blockade of sodium channels. In one embodiment, Compounds of the Invention are useful for treating pain.Type: ApplicationFiled: September 5, 2014Publication date: May 21, 2015Inventor: Jae Hyun Park
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Publication number: 20150141342Abstract: The differential expression of select miRNA in plasma and bile among patients with PDAC, chronic pancreatitis (CP), and controls were measured. Patients (n=215) with treatment-naïve PDAC (n=77), CP with bile or pancreatic duct pathology (n=67), and controls (n=71) that had been prospectively enrolled in a Pancreatobiliary Disease Biorepository at the time of endoscopic retrograde cholangiopancreatography (ERCP) or endoscopic ultrasound (EUS) were identified. Controls were patients with choledocholithiasis but normal pancreata. The sample was separated into training (n=95) and validation (n=120) cohorts to establish and then test the performance of PDAC Signature Panels in diagnosing PDAC. The training cohort (n=95) included age-matched patients with CP and controls. Panels were derived from the differential expression of 10-candidate miRNA in plasma or bile.Type: ApplicationFiled: November 14, 2014Publication date: May 21, 2015Inventors: Murray Korc, A. Jesse Gore, Gregory A. Cote, Stuart Sherman
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Publication number: 20150141447Abstract: The present invention provides a solid preparation excellent in disintegration property and preservation stability. The present invention relates to a solid preparation containing (1) 2-[[6-[(3R)-3-amino-1-piperidinyl]-3,4-dihydro-3-methyl-2,4-dioxo-1(2H)-pyrimidinyl]methyl]-4-fluorobenzonitrile (compound (A)) or a salt thereof, (2) a saccharide, and (3) sodium stearyl fumarate. In addition, the present invention relates to a solid preparation containing (1) compound (A) or a salt thereof, (2) a saccharide, and (3) stearic acid or talc in a naked tablet part.Type: ApplicationFiled: June 4, 2013Publication date: May 21, 2015Applicant: Takeda Pharmaceutical Company LimitedInventors: Maiko Harada, Ikurou Yamane, Masafumi Misaki
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Publication number: 20150141427Abstract: The present invention relates to compounds of formula I: in which Y, Y1, Y4, Y5, Y6, R1, R2, R3 and R4 are defined in the Summary of the Invention; capable of inhibiting the activity of BCR-ABL1 and mutants thereof. The invention further provides a process for the preparation of compounds of the invention, pharmaceutical preparations comprising such compounds and methods of using such compounds in the treatment of cancers.Type: ApplicationFiled: May 9, 2013Publication date: May 21, 2015Applicant: Novartis AGInventors: Pascal Furet, Robert Martin Grotzfeld, Wolfgang Jahnke, Darryl Brynley Jones, Paul William Manley, Andreas Marzinzik, Saliha Moussaoui, Xavier Francois Andre Pelle, Bahaa Salem, Joseph Schoepfer
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Patent number: 9034888Abstract: Compounds of formula (I): wherein R1, R2, R3, R4, R7, R6, R7, R8, R9, A, X and Y as defined herein are provided as useful for the treatment of cancer or for the manufacture of anti-cancer agents.Type: GrantFiled: February 16, 2011Date of Patent: May 19, 2015Assignee: Universite LavalInventors: René C. Gaudreault, Sébastien Fortin
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Patent number: 9034850Abstract: Disclosed are compounds useful as gonadotrophin-releasing hormone (“GnRH”) receptor antagonist.Type: GrantFiled: November 19, 2010Date of Patent: May 19, 2015Assignee: SK Chemicals Co., Ltd.Inventors: Seon Mi Kim, Min Hee Lee, Jae Sun Kim, Hoe Chul Jung, So Young Lee, Soo Min Lee, Eun Jeong Kim, Eui Sun Park, Sung Hoon Park, Bong Yong Lee, Key An Um
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Publication number: 20150132258Abstract: Provided herein are compounds useful for the treatment of HBV infection in a subject in need thereof, pharmaceutical compositions thereof, and methods of inhibiting, suppressing, or preventing HBV infection in the subject.Type: ApplicationFiled: November 14, 2014Publication date: May 14, 2015Inventor: George D. Hartman
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Publication number: 20150133449Abstract: The present invention provides, inter alia, compounds of formula I as protein kinase modulators, methods of preparing them, pharmaceutical compositions containing them and methods of treatment, prevention and/or amelioration of kinase mediated diseases or disorders with them.Type: ApplicationFiled: November 6, 2014Publication date: May 14, 2015Inventors: Meyyappan MUTHUPPALANIAPPAN, Srikant Viswanadha, Govindarajulu Babu, Swaroop K. Vakkalanka
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Publication number: 20150133477Abstract: Methods for reducing uric acid levels in blood or serum of a subject employing metabolites of merbarone as active agents. Methods for treating or preventing disorders of uric acid metabolism are also provided. The metabolites can be formulated as pharmaceutical compositions comprising the metabolites and a pharmaceutically acceptable carrier for use in these methods.Type: ApplicationFiled: November 13, 2013Publication date: May 14, 2015Inventor: Raymond P. Warrell, JR.
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Publication number: 20150132352Abstract: The present invention relates to chemical compounds, methods for their discovery, and their therapeutic and research use. In particular, the present invention provides compounds as therapeutic agents against bacterial infections (e.g., biofilms).Type: ApplicationFiled: May 2, 2013Publication date: May 14, 2015Inventors: Hongmin Sun, Bryan Yestrepsky, David Ginsburg, Scott D. Larsen
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Publication number: 20150132327Abstract: It has been desired to develop a pharmaceutical composition, which is used in agents for preventing and/or treating various diseases related to PDE10 (e.g. mental disorder and neurodegenerative disorder). The present invention provides: compounds having PDE10 inhibitory effect, in particular, compounds having a 4-heteroarylpyrazole-5-carboxylic acid amide structure represented by the following formula (I), or their pharmaceutically acceptable salts, or their solvates; pharmaceutical compositions comprising, as active ingredients, the compounds, or their pharmaceutically acceptable salts, or their solvates; and medical use of the compounds, or their pharmaceutically acceptable salts, or their solvates.Type: ApplicationFiled: January 21, 2015Publication date: May 14, 2015Applicant: MOCHIDA PHARMACEUTICAL CO., LTD.Inventors: Akihiro OKANO, Muneyoshi MAKABE, Kouki OGAWA
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Publication number: 20150125546Abstract: Method of treating and/or preventing pulmonary arterial hypertension comprising administering effective amounts of ambrisentan or a pharmaceutically acceptable salt thereof and riociguat or a pharmaceutically acceptable salt thereof.Type: ApplicationFiled: November 6, 2014Publication date: May 7, 2015Applicant: Gilead Sciences, Inc.Inventors: Luiz Belardinelli, Hunter Campbell Gillies, Faquan Liang, Lina Yao
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Publication number: 20150125559Abstract: A method of constructing a data architecture for use in identifying connections between perturbagens and genes associated with a type of periorbital dyschromia. The method includes providing a gene expression profile for a keratinocyte, fibroblast, melanocyte or melanoma cell, which has been exposed to at least one perturbagen, and comparing the gene expression profile to a control cell from the same cell line. Genes that are differentially expressed in response to the perturbagen are identified by comparing the gene expression profiles of the control cell and the test cell. An ordered list of identifiers representing the differentially expressed genes is created according to the differential expression of the genes. The ordered list is stored as an instance on a computer readable medium. The steps are then repeated to construct a data architecture of stored instances.Type: ApplicationFiled: August 29, 2014Publication date: May 7, 2015Inventors: Karen Marie OSORIO, Wenzhu ZHAO
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Publication number: 20150126523Abstract: The present invention relates to novel and inventive isoxazoline of formula (I) and salts thereof: wherein variables D1, D2, D3, D4, D5, R1, B1, B2, B3, R2, R3, R4, R5, R6, Y, Z, L, a and b are described herein are as defined in the description. The invention also relates to parasiticidal and pesticidal compositions comprising the isoxazoline compounds of formula (I), processes for their preparation and their uses to prevent or treat parasitic infections or infestations in animals and as pesticides.Type: ApplicationFiled: October 30, 2014Publication date: May 7, 2015Applicant: MERIAL LIMITEDInventor: Charles Q. Meng
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Publication number: 20150126436Abstract: The present invention provides a method of treatment of Scedosporium spp.Type: ApplicationFiled: May 13, 2013Publication date: May 7, 2015Applicant: BIODIEM LIMITEDInventors: Julie Phillips, Tania Sorrell, Sharon Chen
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Publication number: 20150126585Abstract: Described herein is the discovery that miR-21 targets and down-regulates the core mismatch repair (MMR) recognition protein complex hMSH2 and hMSH6. Anti-sense miR-21 is therefore proven as therapeutic herein. Therefore, compositions, kits, therapies and other methods, including methods of treatment/amelioration of symptoms, are disclosed herein.Type: ApplicationFiled: December 31, 2014Publication date: May 7, 2015Applicant: THE OHIO STATE UNIVERSITYInventors: Carlo M. Croce, Nicola Valeri
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Publication number: 20150119390Abstract: The present invention provides imidazothiadiazole compounds of Formula (I); Wherein W, Y, R0, R2, R4, Ra, Rb, X1, X2, X3 and X4 are as defined herein, or a stereoisomer, tautomer, pharmaceutically acceptable salt, prodrug ester or solvate form thereof, wherein all of the variables are as defined herein. These compounds are inhibitors of platelet aggregation and thus can be used as medicaments for treating or preventing thromboembolic disorders.Type: ApplicationFiled: April 24, 2013Publication date: April 30, 2015Inventors: Alain Martel, François Tremblay, Anne Marinier, Eldon Scott Priestley, Shoshana L. Posy, R. Michael Lawrence, Michael M. Miller
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Publication number: 20150119389Abstract: Compounds of the formula Ia***** in which the substituents have the definitions provided in the specification, are novel, effective PDE4 inhibitors, useful in the treatment of psoriasis.Type: ApplicationFiled: October 7, 2014Publication date: April 30, 2015Inventor: Ulrich KAUTZ
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Publication number: 20150119382Abstract: The present invention relates to compounds of Formula (I), and solvates, hydrates, and pharmaceutically acceptable salts thereof, wherein X1, X1?, X1?, R1, R2 and R3 are as defined herein, useful as FLAP modulators. The invention also relates to pharmaceutical compositions comprising compounds of Formula (I). Methods of making and using the compounds of Formula (I) are also within the scope of the invention.Type: ApplicationFiled: December 29, 2014Publication date: April 30, 2015Inventors: Wenying Chai, Curt A. Dvorak, Wendy Eccles, James P. Edwards, Steven D. Goldberg, Paul J. Krawczuk, Alec D. Lebsack, Jing Liu, Daniel J. Pippel, Zachary S. Sales, Virginia M. Tanis, Mark S. Tichenor, John J. M. Wiener
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Publication number: 20150111909Abstract: The present invention relates to an oral dosage form comprising non-crystalline lopinavir and crystalline ritonavir. The invention further relates to methods of preparing said oral dosage forms containing the above pharmaceutical active agents.Type: ApplicationFiled: March 6, 2013Publication date: April 23, 2015Inventors: Dominique Meergans, Ralph Stefan
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Publication number: 20150111891Abstract: The invention provides compounds and salts thereof as d herein. The invention also provides pharmaceutical compositions comprising a compound disclosed herein, processes for preparing compounds disclosed herein, intermediates useful for preparing compounds disclosed herein and therapeutic methods for treating an HIV infection, treating the proliferation of the HIV virus, treating AIDS or delaying the onset of AIDS or ARC symptoms in a mammal using compounds disclosed herein.Type: ApplicationFiled: January 3, 2013Publication date: April 23, 2015Applicant: Gilead Sciences, Inc.Inventors: Kerim Babaoglu, Gediminas Brizgys, Hongyan Guo, Paul Hrvatin, Eric Lansdon, John O. Link, Hongtao Liu, Ryan McFadden, Michael L. Mitchell, Yingmei Qi, Paul A. Roethle, Randall W. Vivian, Lianhong Xu, Hong Yang
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Publication number: 20150111851Abstract: This present disclosure is related to the field of 5-fluoropyrimidinones and their derivatives and to the use of these compounds as fungicides.Type: ApplicationFiled: December 22, 2014Publication date: April 23, 2015Inventors: Timothy Boebel, Kristy Bryan, Peter Lee Johnson, Beth Lorsbach, Kevin G. Meyer, W. John Owen, Michael T. Sullenberger, Jeffery D. Webster, Chenglin Yao
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Publication number: 20150111910Abstract: Compounds of formula (I) are of use in the modulation of Kv3.1, Kv.3.2 and Kv3.3 channels and have utility in the treatment or prevention of related disorders.Type: ApplicationFiled: May 22, 2013Publication date: April 23, 2015Applicant: AUTIFONY THERAPEUTICS LIMITEDInventors: Agostino Marasco, Giuseppe Alvaro, Anne Dècor, Dieter Hamprecht, Paolo Dambruoso, Simona Tommasi
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Publication number: 20150111865Abstract: An object of the present invention is to provide a drug containing a compound having Trk-inhibiting activity as an active ingredient in prophylaxis and/or therapy of diseases such as pain, pruritus, lower urinary tract dysfunction, asthma, allergic rhinitis, inflammatory bowel disease or Chagas disease. A compound represented by the general formula (I): (wherein all symbols represent the same meanings as described in the specification), a salt thereof, an N-oxide thereof, a solvate thereof or a prodrug thereof is useful as a drug component having Trk-inhibiting activity in prophylaxis and/or therapy of diseases such as pain, pruritus, lower urinary tract dysfunction, asthma, allergic rhinitis, inflammatory bowel disease or Chagas disease.Type: ApplicationFiled: April 25, 2013Publication date: April 23, 2015Applicant: ONO PHARMACEUTICAL CO., LTD.Inventors: Jun Takeuchi, Masahiro Ikura, Masato Higashino, Maki Iwahashi, Kazuya Hashimura
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Publication number: 20150111911Abstract: Discovery of a new Bax isoform, Bax?2, in cancer cell lines and primary tumors is described. The Bax?2 isoform resulted from combination of Bax microsatellite mutation and alternative splicing Bax exon 2. It is also discovered that Bax?2 renders cancer cells sensitive to certain chemotherapeutic drugs that target caspase 8. Also provided are methods for treating colorectal cancer by administering to a colorectal cancer patient a chemotherapeutic agent that is capable of activating caspase 8, wherein the patient contains a cancer cell that expresses a Bax?2 protein (SEQ ID NO. 2).Type: ApplicationFiled: August 14, 2014Publication date: April 23, 2015Applicant: Mumetel, LLCInventors: Jialing Xiang, Li Ma
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Publication number: 20150111892Abstract: The present invention concerns, in a first aspect, compounds of Formula I as defined herein, pharmaceutically acceptable salts thereof and pharmaceutical compositions containing such compounds. The present invention also relates to compounds of Formula I for use as acid ceramidase inhibitors, and in the treatment of cancer and other disorders in which modulation of the levels of ceramide is clinically relevant.Type: ApplicationFiled: May 27, 2013Publication date: April 23, 2015Inventors: Daniele Piomelli, Natalia Realini, Marco Mor, Chiara Pagliuca, Daniela Pizzirani, Rita Scarpelli, Tiziano Bandiera
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Publication number: 20150110809Abstract: Embodiments of the invention are directed to compounds that inhibit an activity of EP AC proteins and methods of using the same. The inventors have developed a sensitive and robust high throughput screening (HTS) assay for the purpose of identifying EPAC specific inhibitors (Tsalkova et al. (2012) PLOS ONE 7 (1):e30441).Type: ApplicationFiled: February 8, 2013Publication date: April 23, 2015Applicant: The Board of Regents of the University of Texas SystemInventors: Xiaodong Cheng, Jia Zhou, Tamara Tsalkova, Fang Mei, Haijun Chen
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Patent number: 9012467Abstract: The present disclosure describes compositions for intratumoral administration which include a tissue-stabilizing agent and a therapeutic agent.Type: GrantFiled: October 15, 2010Date of Patent: April 21, 2015Assignee: Covidien LPInventor: Joshua Stopek
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Patent number: 9012444Abstract: Tumor growth and metastases in cancer patients are inhibited by administration of a combination therapy including effective amounts of 5-Fluorouracil and a methylol transfer agent such as taurolidine, taurultam or mixtures thereof.Type: GrantFiled: March 21, 2011Date of Patent: April 21, 2015Assignee: Ed. Geistlich Soehne AG fuer Chemische IndustrieInventors: H. Paul Redmond, Rolf W. Pfirrmann
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Publication number: 20150105389Abstract: Provided herein are 3,5-diaminopyrazoles, for example, compounds of Formula IA, that are useful for modulating regulated-in-COPD kinase activity, and pharmaceutical compositions thereof. Also provided herein are methods of their use for treating, preventing, or ameliorating one or more symptoms of a RC kinase-mediated disorder, disease, or condition.Type: ApplicationFiled: December 17, 2014Publication date: April 16, 2015Inventors: Erik Dean RAAUM, Garrett Thomas POTTER, Tai Wei LY
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Publication number: 20150105351Abstract: The present invention is directed to novel nanomolar and picomolar inhibitors of HIV reverse transcriptase, pharmaceutical compositions therefrom and methods for inhibiting reverse transcriptase and treating HIV infections, especially included drug resistant strains of HIV-1 and HIV-2 and/or secondary disease states and/or conditions which occur as a consequence of HIV infection.Type: ApplicationFiled: October 8, 2014Publication date: April 16, 2015Inventors: William L. Jorgensen, Karen S. Anderson
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Publication number: 20150105404Abstract: The present invention comprises compounds of Formula I. wherein: R1, R2, R3, R4, R5, R6, R7, R8, and R9 are defined in the specification. The invention also comprises a method of treating or ameliorating a syndrome, disorder or disease, wherein said syndrome, disorder or disease is rheumatoid arthritis or psoriasis. The invention also comprises a method of modulating ROR?t activity in a mammal by administration of a therapeutically effective amount of at least one compound of claim 1.Type: ApplicationFiled: October 15, 2013Publication date: April 16, 2015Applicant: Janssen Pharmaceutica NVInventors: Kristi A. Leonard, Kent Barbay, James P. Edwards, Kevin D. Kreutter, David A. Kummer, Umar Maharoof, Rachel Nishimura, Maud Urbanski, Hariharan Venkatesan, Aihua Wang, Ronald L. Wolin, Craig R. Woods, Anne Fourie, Xiaohua Xue, Maxwell D. Cummings
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Patent number: 9006259Abstract: This present disclosure is related to the field of N1-sulfonyl-5-fluoropyrimidinones and their derivatives and to the use of these compounds as fungicides.Type: GrantFiled: August 5, 2010Date of Patent: April 14, 2015Assignee: Dow AgroSciences LLCInventors: Timothy A. Boebel, Kristy Bryan, Beth Lorsbach, Timothy P. Martin, W. John Owen, Mark A. Pobanz, Scott Thornburgh, Jeffery D. Webster, Chenglin Yao
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Patent number: 9006249Abstract: The present invention provides a compound of formula I?; or a pharmaceutically acceptable salt thereof, wherein R1, R2, R3, X and n are defined herein. The invention also relates to a method for manufacturing the compounds of the invention, and its therapeutic uses. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.Type: GrantFiled: June 7, 2012Date of Patent: April 14, 2015Assignee: Novartis AGInventors: Gary Mark Coppola, Yuki Iwaki, Rajeshri Ganesh Karki, Toshio Kawanami, Gary Michael Ksander, Muneto Mogi, Robert Sun
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Patent number: 9006232Abstract: A compound represented by the formula (I) or a pharmaceutically acceptable salt thereof: wherein Z represents nitrogen atom or C—X; X represents hydrogen atom or fluorine atom; R1 is hydrogen atom or a C1-C3 alkyl group; L represents single bond or a C1-C6 alkylene group which may be substituted; Y represents single bond, sulfur atom, oxygen atom, NH, or the like; R2 represents hydrogen atom or a cyclic group which may be substituted, which is used for preventive and/or therapeutic treatment of a disease caused by abnormal activity of tau protein kinase 1 such as a neurodegenerative diseases (e.g. Alzheimer disease).Type: GrantFiled: August 11, 2010Date of Patent: April 14, 2015Assignee: Mitsubishi Tanabe Pharma CorporationInventors: Kazuki Nakayama, Daiki Sakai, Kazutoshi Watanabe, Toshiyuki Kohara, Keiichi Aritomo
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Publication number: 20150099766Abstract: The invention relates to compounds of the general formula (I), in which the radicals A1, A2, A3, A4, Lm, Q, R1, T and U have the meaning given in the description and to the use of the compounds for controlling animal pests. In addition, the invention relates to processes and intermediates for the preparation of the compounds according to formula (I).Type: ApplicationFiled: December 15, 2014Publication date: April 9, 2015Inventors: Michael MAUE, Isabelle ADELT, Wolfgang GIENCKE, Markus HEIL, Peter JESCHKE, Bernd-Wieland KRÜGER, Friedrich August MÜHLTHAU, Alexander SUDAU, Klaus RAMING, Ulrich EBBINGHAUS-KINTSCHER, Martin ADAMCZEWSKI, Arnd VOERSTE, Ulrich GÖRGENS, Tobias KAPFERER, Mark Wilhelm DREWES, Angela BECKER, Eva-Maria FRANKEN
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Publication number: 20150099748Abstract: Multiheteroaryl compounds, their preparation, pharmaceutical compositions comprising these compounds, and their pharmaceutical use in the prevention and treatment of prostaglandin D2 mediated diseases and conditions that may be modulated by the inhibition of hematopoietic prostaglandin D synthase (H-PGDS).Type: ApplicationFiled: September 29, 2014Publication date: April 9, 2015Inventors: Gregory W. Endres, Pil Heui Lee, Kirk Lang Olson, James Bernard Kramer, Fred Lawrence Ciske, Stephen Douglas Barrett
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Publication number: 20150099756Abstract: The present invention relates to novel compounds that inhibit Lp-PLA2 activity, processes for their preparation, to compositions containing them and to their use in the treatment of diseases associated with the activity of Lp-PLA2, for example atherosclerosis, Alzheimer's disease, and/or diabetic macular edema.Type: ApplicationFiled: December 15, 2014Publication date: April 9, 2015Inventors: Yun JIN, Zehong WAN, Qing ZHANG
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Publication number: 20150099743Abstract: The present invention relates to compounds and pharmaceutically acceptable salts of Formulas A and B: wherein A, B, R1, R2, R3, R4, R5, R6, R7, R8, R9 and R10 are as defined above. The invention further relates to pharmaceutical compositions comprising the compounds and pharmaceutically acceptable salts and to methods of treating diabetes mellitus and its complications, cancer, ischemia, inflammation, central nervous system disorders, cardiovascular disease, Alzheimer's disease and dermatological disease pression, virus diseases, inflammatory disorders, or diseases in which the liver is a target organ.Type: ApplicationFiled: October 3, 2014Publication date: April 9, 2015Inventors: Hui LI, Seiji NUKUI, Stephanie Anne SCALES, Min TENG, Chunfeng YIN
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Patent number: 8999934Abstract: The disclosure relates to an endothelin receptor antagonist for use in the prevention or treatment of brain metastases in combination with a cytotoxic chemotherapy agent, radiotherapy or both. The endothelin receptor antagonist may for example be bosentan, macitentan or a mixture of bosentan and macitentan.Type: GrantFiled: August 9, 2010Date of Patent: April 7, 2015Assignee: Board of Regents, The University of Texas SystemInventors: Isaiah Fidler, Sun-jin Kim
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Patent number: 9000002Abstract: This present disclosure is related to the field of N1-substituted-5-fluoro-2-oxopyrimidinone-1-(2H)-carboxamides and their derivatives and to the use of these compounds as fungicides.Type: GrantFiled: September 12, 2013Date of Patent: April 7, 2015Assignee: Dow AgroSciences LLCInventors: Timothy A. Boebel, Kristy Bryan, Beth Lorsbach, Timothy P. Martin, W. John Owen, Mark A. Pobanz, Scott Thornburgh, Jeffery D. Webster, Chenglin Yao
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Publication number: 20150093338Abstract: There is provided compositions and methods for the treatment of respiratory conditions such as pulmonary hypertension and sickle-cell disease in a patient in need thereof. The composition and method are for treating a patient in need thereof by inhalation of a composition containing amino acid ester compounds comprising at least one nitric oxide releasing group and pharmaceutical salts thereof.Type: ApplicationFiled: October 8, 2014Publication date: April 2, 2015Inventor: Michael Farber
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Publication number: 20150094294Abstract: The present disclosure provides compounds, specifically pyrimidin-4,6-dicarboxylic acid amide derivatives, or pharmaceutically acceptable salts thereof and pharmaceutical compositions containing said compounds. Also provided are methods for treating a mammal having malaria, or killing or inhibiting the growth of a Plasmodium species, comprising administering to said mammal or contacting said Plasmodium species with, an effective amount of a pyrimidin-4,6-dicarboxylic acid amide derivative.Type: ApplicationFiled: February 28, 2013Publication date: April 2, 2015Inventors: Richard W. Scott, Robert W. Kavash, Wenxi Pan, Katie Freeman, Michael J. Costanzo, Doron Greenbaum, Yongjiang Xu, Trevor Young
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Patent number: 8993779Abstract: The present invention is directed to benzimidazolone derivatives which are positive allosteric modulators of the mGluR2 receptor, useful in the treatment or prevention of neurological and psychiatric disorders associated with glutamate dysfunction and diseases in which the mGluR2 receptor is involved. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which metabotropic glutamate receptors are involved, such as schizophrenia.Type: GrantFiled: August 5, 2011Date of Patent: March 31, 2015Assignee: Merck Sharp & Dohme Corp.Inventors: Vadim Y. Dudkin, Mark E. Fraley, Kenneth L. Arrington, Mark E. Layton, Alexander J. Reif, Kevin J. Rodzinak, Joseph E. Pero