Pyrimidines With Chalcogen Bonded Directly To A Ring Carbon Of Said Pyrimidine Moiety Patents (Class 514/269)
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Patent number: 9902712Abstract: The present invention relates to the field of medicine, provided herein are novel nitrogenous heterocyclic compounds, their preparation methods and their uses as drugs, especially for treatment and prevention of tissue fibrosis. Also provided herein are pharmaceutically acceptable compositions comprising the nitrogenous heterocyclic compounds and the uses of the compositions in the treatment of human or animal tissue fibrosis, especially for human or animal renal interstitial fibrosis, glomerular sclerosis, liver fibrosis, pulmonary fibrosis, IPF, peritoneal fibrosis, myocardial fibrosis, dermatofibrosis, postsurgical adhesion, benign prostatic hyperplasia, skeletal muscle fibrosis, scleroderma, multiple sclerosis, pancreatic fibrosis, cirrhosis, myosarcoma, neurofibroma, pulmonary interstitial fibrosis, diabetic nephropathy, alzheimer disease or vascular fibrosis.Type: GrantFiled: December 19, 2014Date of Patent: February 27, 2018Assignee: SUNSHINE LAKE PHARMA CO., LTD.Inventors: Jiancun Zhang, Xiaojun Wang, Yingjun Zhang, Runfeng Lin, Yi Yu, Liang Chen, Jihua Lin
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Patent number: 9873674Abstract: Compounds having a c-Rel inhibiting property according to the formula: (1) wherein R1 and R2 are each independently selected from hydrogen atom and hydrocarbon groups having at least one and up to thirty carbon atoms and optionally substituted with one or more heteroatoms selected from halogen, nitrogen, oxygen, and sulfur; R3 is selected from hydrocarbon groups having at least one and up to thirty carbon atoms and optionally substituted with one or more heteroatoms selected from halogen, nitrogen, oxygen, and sulfur; and X1, X2, and X3 are each independently selected from oxygen and sulfur atoms. Methods for treating diseases and conditions associated with c-Rel overexpression by administering compounds of Formula (1) or a pharmaceutical composition thereof to a subject afflicted with such a disease or condition are also described.Type: GrantFiled: September 19, 2013Date of Patent: January 23, 2018Assignee: CORNELL UNIVERSITYInventors: Hsiou-Chi Liou, Mei-Ling Liou, Samedy Ouk
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Patent number: 9856234Abstract: The present invention relates to a heterocyclic compound of the general formula (I) and their use and preparation, methods of making the compounds, compositions containing at least one of said compounds, and methods of treatment using at least one compound. In particular, compounds of the general formula (I) are useful for inhibiting glycogen synthase kinase 3 (GSK-3).Type: GrantFiled: January 31, 2014Date of Patent: January 2, 2018Assignees: ABBVIE DEUTSCHLAND GMBH & CO. KG, ABBVIE INC.Inventors: Sean Colm Turner, Margaretha Henrica Maria Bakker, Kent D. Stewart
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Patent number: 9850214Abstract: Disclosed are chemical entities which are inhibitors of Nedd8-activating enzyme (NAE), namely, the compound {(1S,2S,4R)-4-[(6-{[(1R,2S)-5-chloro-2-methoxy-2,3-dihydro-1H-inden-1-yl]amino}pyrimidin-4-yl)oxy]-2-hydroxycyclopentyl}methyl sulfamate and pharmaceutically acceptable salts thereof; solid state forms thereof; and prodrugs thereof. Also disclosed are methods of using the chemical entities to treat disorders such as cancer.Type: GrantFiled: July 8, 2014Date of Patent: December 26, 2017Assignee: MILLENNIUM PHARMACEUTICALS, INC.Inventors: Ashley Sue McCarron, Todd B. Sells, Matthew Stirling, Stephen G. Stroud
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Patent number: 9828383Abstract: Described herein is the Bruton's tyrosine kinase (Btk) inhibitor 1-((R)-3-(4-amino-3-(4-phenoxyphenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl)piperidin-1-yl)prop-2-en-1-one, including crystalline forms, solvates and pharmaceutically acceptable salts thereof. Also disclosed are pharmaceutical compositions that include the Btk inhibitor, as well as methods of using the Btk inhibitor, alone or in combination with other therapeutic agents, for the treatment of autoimmune diseases or conditions, heteroimmune diseases or conditions, cancer, including lymphoma, and inflammatory diseases or conditions.Type: GrantFiled: August 7, 2017Date of Patent: November 28, 2017Assignee: Pharmacyclic s LLCInventors: Norbert Purro, Mark Stephen Smyth, Erick Goldman, David D. Wirth
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Patent number: 9828351Abstract: The present disclosure relates generally, but not exclusively, to compounds and their use as enzyme interacting agents, in particular, agents which interact with one or more enzymes in the sphingolipid biosynthesis pathway. The disclosure further relates to the use of such compounds as research tools, use in therapy, to compositions and agents comprising said compounds, and to methods of treatment using said compounds.Type: GrantFiled: June 26, 2015Date of Patent: November 28, 2017Assignees: MONASH UNIVERSITY, UNIVERSITY OF SOUTH AUSTRALIA, CENTRAL ADELAIDE LOCAL HEALTH NETWORK INCORPORATEDInventors: Bernard Luke Flynn, Luigi Aurelio, Carmen Vittoria Scullino, Bing Hui Wang, Stuart Maxwell Pitson, Melissa Rose Pitman
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Patent number: 9777001Abstract: The present invention provides compounds of Formula (I): or stereoisomers, tautomers, or pharmaceutically acceptable salts thereof, wherein all the variables are as defined herein. These compounds are selective factor XIa inhibitors or dual inhibitors of FXIa and plasma kallikrein. This invention also relates to pharmaceutical compositions comprising these compounds and methods of treating thromboembolic and/or inflammatory disorders using the same.Type: GrantFiled: January 30, 2015Date of Patent: October 3, 2017Assignee: Bristol-Myers Squibb CompanyInventors: James R. Corte, Indawati De Lucca, Tianan Fang, Wu Yang, Yufeng Wang, Andrew K. Dilger, Kumar Balashanmuga Pabbisetty, William R. Ewing, Yeheng Zhu, Ruth R. Wexler, Donald J. P. Pinto, Michael J. Orwat, Leon M. Smith, II
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Patent number: 9770023Abstract: The present invention relates to novel fungicidal active compound combinations or compositions comprising a phenylamidine compound of formula (I) and further active compounds (II) and (III) selected from the groups (A), (B) and/or (C), to a process for preparing these active compound combinations or compositions and to the use thereof as biologically active compound combinations or compositions, especially for the control of phytopathogenic fungi in plants and/or in the protection of materials and/or as plant growth regulators.Type: GrantFiled: February 10, 2015Date of Patent: September 26, 2017Assignee: BAYER CROPSCIENCE AKTIENGESELLSCHAFTInventors: Andreas Goertz, Thomas Seitz, Peter Dahmen, Ulrike Wachendorff-Neumann
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Patent number: 9763945Abstract: The present invention relates to compounds and pharmaceutically acceptable salts thereof and formulations comprising the compounds or a pharmaceutically acceptable salts thereof that are useful in modulating lyn kinase activity. In particular, the compounds or a pharmaceutically acceptable salts thereof are useful for treating or preventing a disease or disorder including cardiovascular disease, dyslipidemia, dyslipoproteinemia, a disorder of glucose metabolism, metabolic syndrome (i.e., Syndrome X), a peroxisome proliferator activated receptor-associated disorder, septicemia, a thrombotic disorder, type II diabetes, obesity, pancreatitis, hypertension, renal disease, inflammation, or impotence.Type: GrantFiled: November 13, 2015Date of Patent: September 19, 2017Assignee: Melior Pharmaceuticals I, Inc.Inventors: Andrew G. Reaume, Michael S. Saporito
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Patent number: 9750252Abstract: An arylalkyloxypyrimidine derivative represented by the formula (I) wherein R1 is an alkyl group, a cycloalkyl group, an alkenyl group, an alkynyl group, a haloalkyl group, a haloalkenyl group, a haloalkynyl group, an alkoxyalkyl group, a dioxolane group and the like; R2 and R3 are each a hydrogen atom, an alkyl group and the like; X is an alkyl group, a cycloalkyl group, an alkenyl group, an alkynyl group, a haloalkyl group, a haloalkenyl group, a haloalkynyl group, a trialkylsilyl group and the like; Y is CH or a nitrogen atom; q is an integer of 1 to 3; m is an integer of 0 to 5; and n is 0 or 1 or a salt thereof, and an agrohorticultural insecticide containing the compound as an active ingredient and a method of use thereof.Type: GrantFiled: February 1, 2013Date of Patent: September 5, 2017Assignee: Nihon Nohyaku., Ltd.Inventors: Eikou Satoh, Tetsuya Murata, Hiroto Harayama, Motofumi Nakano, Kosuke Fukatsu, Kayo Inukai, Ryota Kasahara, Yutaka Abe, Nobuyuki Hayashi, Naoya Fujita
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Patent number: 9713617Abstract: Described herein is the Bruton's tyrosine kinase (Btk) inhibitor 1-((R)-3-(4-amino-3-(4-phenoxyphenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl)piperidin-1-yl)prop-2-en-1-one, including crystalline forms, solvates and pharmaceutically acceptable salts thereof. Also disclosed are pharmaceutical compositions that include the Btk inhibitor, as well as methods of using the Btk inhibitor, alone or in combination with other therapeutic agents, for the treatment of autoimmune diseases or conditions, heteroimmune diseases or conditions, cancer, including lymphoma, and inflammatory diseases or conditions.Type: GrantFiled: December 21, 2016Date of Patent: July 25, 2017Assignee: Pharmacyclics LLCInventors: Norbert Purro, Mark Stephen Smyth, Erick Goldman, David D. Wirth
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Patent number: 9700547Abstract: The use of at least one compound of formula I or II or pharmaceutically acceptable salts thereof, for preparing a pharmaceutical composition that acts by inhibiting the phosphorylase uridine enzyme, and the use of the compounds for preparing a pharmaceutical composition that acts by inhibiting the human phosphorylase uridine enzyme, which can be optionally used in combination with at least one antineoplastic, wherein the inhibition increases the effectiveness of antineoplastic and decreases the side effects caused by the administration of antineoplastics.Type: GrantFiled: September 2, 2014Date of Patent: July 11, 2017Assignee: União Brasileira de Educação e Assistência, Mantenedora da PucrsInventors: Luiz Augusto Basso, Pablo Machado, Daiana Renck, Diógenes Santiago Santos
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Patent number: 9695131Abstract: Substituted uracil derivatives of formula (I), processes for their preparation, their use alone or in combinations for the treatment and/or prophylaxis of diseases, and their use for preparing medicaments for the treatment and/or prophylaxis of diseases.Type: GrantFiled: November 5, 2014Date of Patent: July 4, 2017Assignee: Bayer Pharma AktiengesellschaftInventors: Chantal Fürstner, Jens Ackerstaff, Alexander Straub, Heinrich Meier, Hanna Tinel, Katja Zimmermann, Dmitry Zubov, Jens Schamberger
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Patent number: 9687486Abstract: This invention provides a method of treating a subject suffering from atherosclerosis or a myeloproliferative neoplasm which comprises administering to the subject an amount of a Lyn kinase activator effective to activate Lyn kinase so as to thereby treat the subject.Type: GrantFiled: December 20, 2013Date of Patent: June 27, 2017Assignee: THE TRUSTEES OF COLUMBIA UNIVERSITY IN THE CITY OF NEW YORKInventors: Alan R. Tall, Nan Wang
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Patent number: 9669034Abstract: The present invention relates to 4-aryl-N-phenyl-1,3,5-triazin-2-amines containing a sulfoximine group of general formula (I) or (Ia) as described and defined herein, and methods for their preparation, their use for the treatment and/or prophylaxis of disorders, in particular of hyper-proliferative disorders and/or virally induced infectious diseases and/or of cardiovascular diseases. The invention further relates to intermediate compounds useful in the preparation of said compounds of general formula (I) or (Ia).Type: GrantFiled: May 21, 2012Date of Patent: June 6, 2017Assignee: BAYER INTELLECTUAL PROPERTY GMBHInventors: Ulrich Lücking, Rolf Bohlmann, Arne Scholz, Gerhard Siemeister, Mark Jean Gnoth, Ulf Bömer, Dirk Kosemund, Philip Lienau, Gerd Rühter, Carsten Schultz-Fademrecht
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Patent number: 9662303Abstract: The present invention provides a compound for treating cancer including an isolated form of dibenzyl trisulfide (DTS) provided in an effective amount to act as an agent against human diseases, including various forms of cancer. The present invention also provides a compound for treating cancer including DTS isolated from Petiveria alliacea L. (guinea hen weed) for providing an effective, potent anti-proliferation and/or cytotoxic activity on a wide range of cancer cell lines. The present invention further provides DTS derivatives (e.g. DTS-albumin complexes) in effective dosage for providing a potent anti-proliferation and/or cytotoxic activity on a wide range of cancer cell lines. Additionally, the present invention provides methods of isolating and/or providing the DTS and/or its derivatives in an effective amount for providing a potent anti-proliferation and/or cytotoxic activity on cancer cell lines.Type: GrantFiled: May 18, 2007Date of Patent: May 30, 2017Assignee: PG-Pharma, LLCInventors: Lawrence A.D. Williams, H. George Levy
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Patent number: 9657001Abstract: There is provided compounds of formula I, wherein E1, E2, E3, E4, L1, Y1, Y2, Y3, Ra and z have meanings provided in the description, and pharmaceutically-acceptable salts thereof, which compounds are useful in the treatment of diseases in which inhibition of leukotriene C4 synthase is desired and/or required, and particularly in the treatment of respiratory diseases and inflammation.Type: GrantFiled: May 4, 2016Date of Patent: May 23, 2017Assignee: ASTRAZENECA ABInventors: Robert Ronn, Carl Jonas Lindh, Erik Ringberg, Hanna Birgitta Ellinor Andersson, Peter Nilsson, Wesley Ralph Schaal, Magnus Munck af Rosenschöld, Antonios Nikitidis, Grigorios Nikitidis, Petra Johannesson, Christian Tyrchan
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Patent number: 9649311Abstract: Compressed tablets for oral administration containing raltegravir in the form of a pharmaceutically acceptable salt are described. The tablets comprise: (A) an intragranular component comprising (i) an effective amount of an alkali metal salt of raltegravir, (ii) optionally a first superdisintegrant, and (iii) a binder; and (B) an extragranular component comprising (i) a second superdisintegrant, (ii) a filler, and (iii) a lubricant. Methods for preparing the tablets and the use of the tablets, optionally in combination with other anti-HIV agents, for the inhibition of HIV integrase, for the treatment or prophylaxis of HIV infection, or for the treatment, delay in the onset, or prophylaxis of AIDS are also described.Type: GrantFiled: October 21, 2010Date of Patent: May 16, 2017Assignee: Merck Sharp & Dohme Corp.Inventors: Majid Mahjour, Feng Li, Decheng Ma, Sutthilug Sotthivirat
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Method of treating and preventing brain impairment using Na-K-2Cl-cotransporter isoform 1 inhibitors
Patent number: 9616075Abstract: The disclosure relates to a method of treating and/or preventing brain impairment in a subject that has or is susceptible to ammonia neurotoxicity (increased plasma ammonia), by administering a Na-; —K+-2CI- cotransporter isoform 1 (“NKCC1”) inhibitor to the selected subject under conditions effective to treat and/or prevent brain impairment. The disclosure further relates to methods of maintaining the fundamental function of astrocytic potassium buffering and inhibiting accumulation of potassium star rounding astrocytes, both of which involve contacting astrocytes with a NKCC 1 inhibitor.Type: GrantFiled: March 15, 2013Date of Patent: April 11, 2017Assignee: University of RochesterInventors: Maiken Nedergaard, Alexander Stanley Thrane, Vinita Rangroo Thrane -
Patent number: 9539221Abstract: The use of ?-adrenergic inverse agonists provides a new and highly efficient way of treating a number of pulmonary airway diseases, including asthma, emphysema, and chronic obstructive pulmonary diseases. In general, such a method comprises administering a therapeutically effective amount of a ?-adrenergic inverse agonist to the subject to treat the pulmonary airway disease. Particularly preferred inverse agonists include nadolol and carvedilol.Type: GrantFiled: October 8, 2004Date of Patent: January 10, 2017Assignees: EGB ADVISORS, LLC, INVION, INC.Inventor: Richard A. Bond
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Patent number: 9540382Abstract: Described herein is the Bruton's tyrosine kinase (Btk) inhibitor 1-((R)-3-(4-amino-3-(4-phenoxyphenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl)piperidin-1-yl)prop-2-en-1-one, including crystalline forms, solvates and pharmaceutically acceptable salts thereof. Also disclosed are pharmaceutical compositions that include the Btk inhibitor, as well as methods of using the Btk inhibitor, alone or in combination with other therapeutic agents, for the treatment of autoimmune diseases or conditions, heteroimmune diseases or conditions, cancer, including lymphoma, and inflammatory diseases or conditions.Type: GrantFiled: June 3, 2013Date of Patent: January 10, 2017Assignee: Pharmacyclics LLCInventors: Norbert Purro, Mark Smyth, Erick Goldman, David D. Wirth
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Patent number: 9471130Abstract: The described embodiments include a computing device with an entity (a processor, a processor core, etc.) and a controller. In these embodiments, the controller, using an idle duration history, predicts a duration of a next idle period for the entity. Based on the predicted duration of the next idle period, the controller configures the entity to operate in a corresponding idle state.Type: GrantFiled: October 25, 2013Date of Patent: October 18, 2016Assignee: ADVANCED MICRO DEVICES, INC.Inventors: Manish Arora, Nuwan S. Jayasena, Michael J. Schulte
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Patent number: 9428499Abstract: The present disclosure is related to heteroaryl compounds as MEK inhibitors. These compounds include heteroaryl compounds of formula I, their pharmaceutically acceptable salts, combinations with suitable medicament and pharmaceutical compositions thereof. The present disclosure also includes processes of preparation of the compounds and their use in methods of treatment.Type: GrantFiled: March 11, 2013Date of Patent: August 30, 2016Assignee: LUPIN LIMITEDInventors: Bhavesh Dave, Rakesh Kumar Banerjee, Samiron Phukan, Abhijit Datta Khoje, Rajkumar Hangarge, Jitendra Sambhaji Jadhav, Venkata P. Palle, Rajender Kumar Kamboj
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Patent number: 9382214Abstract: The present invention relates to processes and intermediates for preparing Gonadotropin-Releasing Hormone (GnRH) receptor antagonists of structure (VI); and stereoisomers and pharmaceutically acceptable salts thereof.Type: GrantFiled: June 19, 2014Date of Patent: July 5, 2016Assignee: Neurocine Biosciences, Inc.Inventors: Donald J. Gallagher, Laszlo R. Treiber, Robert Michael Hughes, Onorato Campopiano, Peng Wang, Yuxin Zhao, Shine K. Chou, Michael Allen Ouellette, Donald Nicholas Hettinger
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Patent number: 9376450Abstract: Heteroaryloxyheterocyclyl compounds, and compositions containing them, and processes for preparing such compounds. Provided herein also are methods of treating disorders or diseases treatable by inhibition of PDE10, such as obesity, non-insulin dependent diabetes, schizophrenia, Huntington's Disease, bipolar disorder, obsessive-compulsive disorder, and the like.Type: GrantFiled: May 10, 2013Date of Patent: June 28, 2016Assignee: AMGEN INC.Inventors: Jennifer R. Allen, Daniel B. Horne, Essa Hu Harrington, Matthew R. Kaller, Holger Monenschein, Thomas T. Nguyen, Andreas Reichelt, Robert M. Rzasa
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Patent number: 9370578Abstract: The present invention relates to an oral dosage form comprising crystalline lopinavir and crystalline ritonavir. The invention further relates to methods of preparing said oral dosage forms containing the above pharmaceutical active agents.Type: GrantFiled: March 6, 2013Date of Patent: June 21, 2016Assignee: ratiopharm GmbHInventors: Dominique Meergans, Konstantin Holfinger
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Patent number: 9326509Abstract: The present invention relates to plant-protecting active ingredient mixtures comprising, as active components, a neonicotinoid and one or two fungicides selected from pyraclostrobin and boscalid, in synergistically effective amounts and to a method of improving the health of plants by to the plants or the locus thereof by applying said mixtures.Type: GrantFiled: February 20, 2006Date of Patent: May 3, 2016Assignee: BASF SEInventors: Dirk Voeste, Martin P. Mascianica, Hendrik Ypema, Henry Van Tuyl Cotter
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Patent number: 9315493Abstract: The present invention provides: a compound represented by general formula (I) below, that has both angiotensin II receptor antagonism and a PPAR? activation effect and that is useful as a preventative and/or therapeutic agent for high blood pressure, cardiac disease, arteriosclerosis, type-2 diabetes, and the like; and a drug composition containing the compound. General formula (I) (in the formula: ring A represents a pyridine ring; ring B represents a tetrazole ring or an oxadiazol-5(4H)-one ring; X represents C—R5 or a nitrogen atom; R1 represents an alkyl group; R2 represents an alkyl group or a cycloalkyl group; and R3, R4, and R5 each independently represents a hydrogen atom, a halogen atom, an alkyl group, an alkoxy group or similar.Type: GrantFiled: March 13, 2012Date of Patent: April 19, 2016Assignee: KOWA COMPANY, LTD.Inventors: Toru Miura, Seiichi Sato, Hajime Yamada, Junya Tagashira, Toshiaki Watanabe, Ryohei Sekimoto, Rie Ishida, Hitomi Aoki, Tadaaki Ohgiya
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Patent number: 9315521Abstract: 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: April 22, 2015Date of Patent: April 19, 2016Assignee: Université LavalInventors: Giorgio Attardo, Sasmita Tripathy, Martin Gagnon
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Patent number: 9241939Abstract: The invention relates to a pharmaceutical combination which comprises (a) a phosphoinositide 3-kinase inhibitor compound and (b) a compound which modulates the Ras/Raf/Mek pathway for the treatment of a proliferative disease, especially a solid tumor disease; a pharmaceutical composition comprising such a combination; the use of such a combination for the preparation of a medicament for the treatment of a proliferative disease; a commercial package or product comprising such a combination as a combined preparation for simultaneous, separate or sequential use; and to a method of treatment of a warm-blooded animal, especially a human.Type: GrantFiled: December 19, 2014Date of Patent: January 26, 2016Assignee: Novartis AGInventors: Carlos Garcia-Echeverria, Sauveur-Michel Maira, Darrin Stuart, Susan Wee, Christine Fritsch, Tobi Nagel
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Patent number: 9216959Abstract: The present invention relates to compounds and pharmaceutically acceptable salts thereof and formulations comprising the compounds or a pharmaceutically acceptable salts thereof that are useful in modulating lyn kinase activity. In particular, the compounds or a pharmaceutically acceptable salts thereof are useful for treating or preventing a disease or disorder including cardiovascular disease, dyslipidemia, dyslipoproteinemia, a disorder of glucose metabolism, metabolic syndrome (i.e., Syndrome X), a peroxisome proliferator activated receptor-associated disorder, septicemia, a thrombotic disorder, type II diabetes, obesity, pancreatitis, hypertension, renal disease, inflammation, or impotence.Type: GrantFiled: February 18, 2014Date of Patent: December 22, 2015Assignee: Melior Pharmaceuticals I, Inc.Inventors: Andrew G. Reaume, Michael S. Saporito
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Patent number: 9167815Abstract: A composition having a stable and high fungicidal effect against a cultivated crop infected by a plant pathogen is provided. An agricultural or horticultural fungicide composition containing, as active ingredients, (a) fluazinam or its salt and (b) a strobilurin compound or its salt is provided; in addition, a method for controlling a plant pathogen by applying the subject agricultural or horticultural fungicide composition to a plant or a soil is provided; and furthermore, a method for controlling a plant pathogen by applying (a) fluazinam or its salt and (b) a strobilurin compound or its salt to a plant or a soil is provided.Type: GrantFiled: May 25, 2012Date of Patent: October 27, 2015Assignee: ISHIHARA SANGYO KAISHA, LTD.Inventors: Koji Sugimoto, Takanori Suzuki, Koudai Yamamoto
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Patent number: 9168291Abstract: ?-mannosylceramides or salts or solvates thereof in a pharmaceutically acceptable carrier, for use as a Type I NKT cell agonist in conjunction with a therapeutically effective amount of ?-galactosylceramide or a salt or a solvate thereof, and/or at least one or more T-cell co-stimulatory molecules, disclosed. Compositions comprising ?-mannosylceramide, as well as methods of treatment of tumors are also provided.Type: GrantFiled: August 7, 2014Date of Patent: October 27, 2015Assignees: The United States of America, as represented by the Secretary, Department of Health and Human Services, The University of BirminghamInventors: Jay A. Berzofsky, Jessica J. O'Konek, Masaki Terabe, Petr A. Illarionov, Gurdyal S. Besra
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Patent number: 9156817Abstract: Compounds of Formula (I) promote axonal outgrowth angiogenesis and can therefore be used to reduce central nerve injuries such as head injury and spinal cord injury, cerebral infarction, ischemic heart diseases, peripheral arterial occlusive diseases, or after-effects of these diseases. in which Nx group is preferably a 6-membered aromatic ring containing two nitrogen atoms; R0, R1 and R2 are each independently a hydrogen atom, an alkyl group, or an amino group; E is an oxygen atom or an —NR8 group (wherein R8 is an alkyl group or the like); n is an integer of 0 to 5; X and Y are each a connecting bond, a cycloalkyl group, or —CO—; and Q is a hydrogen atom or a phenyl group.Type: GrantFiled: July 22, 2014Date of Patent: October 13, 2015Assignee: DAIICHI SANKYO COMPANY, LIMITEDInventors: Naohiro Takemoto, Kenji Murata, Norihito Murayama, Chikaomi Yamada
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Patent number: 9145374Abstract: The present invention relates to methods of inhibiting shikimate pathway, comprising administering to a subject a pharmaceutically acceptable composition comprising a compound having a formula: or pharmaceutically acceptable salts thereof.Type: GrantFiled: January 10, 2014Date of Patent: September 29, 2015Assignee: NATIONAL TSING HUA UNIVERSITYInventors: Wen-Ching Wang, Shih-Ching Chou, Ming-Hua Hsu
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Patent number: 9139564Abstract: Compound of Table I are described. They are useful as stimulators of sGC, particularly NO-independent, heme-dependent stimulators. These compounds may be useful for treating, preventing or managing various disorders that are herein disclosed.Type: GrantFiled: December 26, 2012Date of Patent: September 22, 2015Assignee: IRONWOOD PHARMACEUTICALS, INC.Inventors: Charles Kim, Takashi Nakai, Joel Moore, Nicholas Robert Perl, G-yoon Jamie Im, Timothy Claude Barden, Rajesh R. Iyengar, Daniel P. Zimmer, Angelika Fretzen, Paul Allan Renhowe
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Patent number: 9139518Abstract: A compound of the formula (I): a pharmaceutically acceptable salt or solvate thereof, where R1 is optionally substituted lower alkyl, Y is —S(O)2—, R2 is hydrogen or optionally substituted lower alkyl, R7 is hydrogen or optionally substituted lower alkyl, X is a group of the formula: where R5 and R6 are each independently hydrogen, a group of the formula: is optionally substituted cycloalkylene, p is 0, and q is 1 or 2, Z is optionally substituted carbocyclyl or optionally substituted heterocyclyl, and provided that a compound wherein Z is fused heterocyclyl consisting of three rings or optionally substituted pyrimidinyl is excluded.Type: GrantFiled: June 25, 2010Date of Patent: September 22, 2015Assignee: SHIONOGI & CO., LTD.Inventors: Takayuki Okuno, Naoki Kouyama, Masahiro Sakagami
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Patent number: 9132097Abstract: Described herein are carrier nanoparticles comprising a polymer containing a polyol coupled to a polymer containing a boronic acid, configured to present the polymer containing a boronic acid to an environment external to the nanoparticle. Targeted versions of the described nanoparticles are also described, as are related compositions, methods and systems.Type: GrantFiled: March 1, 2013Date of Patent: September 15, 2015Assignee: California Institute of TechnologyInventors: Mark E. Davis, Han Han
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Patent number: 9078437Abstract: This invention provides a composition comprising a first compound selected from Formula 1, an N-oxide or an agriculturally suitable salt thereof; and a second compound selected from pyrethroids, wherein R1, R2, R3, R4a, R4b and R5 are as defined in the disclosure.Type: GrantFiled: March 8, 2013Date of Patent: July 14, 2015Assignee: E I DU PONT DE NEMOURS AND COMPANYInventors: George Philip Lahm, Thomas Paul Selby, Thomas Martin Stevenson
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Patent number: 9067945Abstract: The invention relates to the use of selective phosphodiesterase 9A (PDE9A) inhibitors for producing medicaments for improving perception, concentration, cognitive processes, learning and/or memory.Type: GrantFiled: May 3, 2013Date of Patent: June 30, 2015Assignee: Boehringer Ingehleim International GmbHInventors: Frank-Gerhard Böss, Christina Erb, Martin Hendrix, Marja Van Kampen, Frank Wunder
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Publication number: 20150148308Abstract: A harmful arthropod control composition comprising a compound represented by the following Formula (1) wherein each symbol represents definitions described in the specification, and one or more fungicidal compounds, which are selected from among azoles, strobilurins, phenylamides, rice blast controlling compounds, rice sheath blight disease controlling compounds, and other fungicidal compounds. The composition has an excellent controlling effect against harmful arthropods.Type: ApplicationFiled: June 5, 2013Publication date: May 28, 2015Applicant: Sumitomo Chemical Company, LimitedInventors: Tatsuya Suzuki, Atsushi Iwata, Yoshihiko Nokura
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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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Publication number: 20150141372Abstract: Compounds of formula (I), processes for their production and their use as Bub1 kinase inhibitors for the treatment of hyperproliferative diseases and/or disorders responsive to induction of cell death.Type: ApplicationFiled: May 8, 2013Publication date: May 21, 2015Inventors: Marion Hitchcock, Christoph-Stephan Hilger, Anne Mengel, Hans Briem, Simon Holton, Vera Pütter, Gerhard Siemeister, Stefan Prechtl, Amaury Ernesto Fernández-Montalván, Christian Stegmann, Cornelia Preuße, Mark Jean Gnoth
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Publication number: 20150141403Abstract: The present invention relates to novel triazolo[4,3-a]pyridine derivatives of Formula (I) wherein all radicals are as defined in the claims. The compounds according to the invention are positive allosteric modulators of the metabotropic glutamate receptor subtype 2 (“mGluR2”), which are useful for the treatment or prevention of neurological and psychiatric disorders associated with glutamate dysfunction and diseases in which the mGluR2 subtype of metabotropic receptors is involved. The invention is also directed to pharmaceutical compositions comprising such compounds, to processes to prepare such compounds and compositions, and to the use of such compounds for the prevention or treatment of neurological and psychiatric disorders and diseases in which mGluR2 is involved.Type: ApplicationFiled: December 1, 2014Publication date: May 21, 2015Inventors: Jose Maria CID-NUNEZ, Daniel OEHLRICH, Andres Avelino TRABANCO-SUAREZ, Gary John TRESADERN, Juan Antonio VEGA RAMIRO, Gregor James MACDONALD
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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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Patent number: 9034851Abstract: The present invention relates to substituted pyrimidines useful as HIF prolyl hydroxylase inhibitors to treat anemia and like conditions.Type: GrantFiled: September 19, 2012Date of Patent: May 19, 2015Assignee: MERCK SHARP & DOHME CORP.Inventors: Qun Dang, Changyou Zhou, Wuxin Zou, Yuxia Hua
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Patent number: 9029538Abstract: The present application provides compounds of Formula I or salt forms thereof, wherein Ra, Rb, Rc, Rd, D, W, R1a, R1b, R1c, Y, R3, X, E and G are as defined herein, compositions, methods of treatment and uses thereof.Type: GrantFiled: May 13, 2014Date of Patent: May 12, 2015Assignee: Ignyta, Inc.Inventors: Reddeppa Reddy Dandu, Robert L. Hudkins, Kurt A. Josef, Catherine P. Prouty, Rabindranath Tripathy
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Publication number: 20150126513Abstract: The present invention provides for compounds of formula (I): wherein R1-R4 and n are defined herein. The present invention also provides for pharmaceutical compositions and combinations comprising a compound of formula (I) as well as for the use of such compounds as tankyrase inhibitors and in the treatment of Wnt signaling and tankyrase 1 and 2 signaling related disorders which include, but are not limited to, cancer.Type: ApplicationFiled: July 13, 2012Publication date: May 7, 2015Applicant: Novartis AGInventors: Christine Hiu-Tung Chen, Donovan Noel Chin, Lucian V. DiPietro, Jianmei Fan, Mark G. Palermo, Michael David Shultz, Bakary-Barry Toure
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Publication number: 20150119412Abstract: A compound having an SSTR5 antagonist action and use of the compound as a medicament are provided. Specifically, a compound represented by the following formula: wherein each symbol is as defined herein, or a salt thereof, a medicament comprising the compound or a salt thereof, and use of the compound or a salt thereof as an agent the prophylaxis or treatment of diabetes mellitus are provided.Type: ApplicationFiled: October 28, 2014Publication date: April 30, 2015Applicant: Takeda Pharmaceutical Company LimitedInventors: Shizuo Kasai, Takashi Nakahata, Asato Kina, Hideki Hirose, Takeshi Yamasaki, Tohru Yamashita, Yoichi Nishikawa
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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