The Additional Hetero Ring Is A Diazine Patents (Class 514/252.02)
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Patent number: 12240831Abstract: Substituted pyridazinone compounds, conjugates, and pharmaceutical compositions for use in the treatment of neuromuscular diseases, such as Duchenne Muscular Dystrophy (DMD), are disclosed herein. The disclosed compounds are useful, among other things, in the treating of DMD and modulating inflammatory inhibitors IL-1, IL-6 or TNF-?.Type: GrantFiled: September 1, 2023Date of Patent: March 4, 2025Assignee: EDGEWISE THERAPEUTICS, INC.Inventors: Kevin Hunt, Kevin Koch, Alan Russell, Stephen Schlachter, Paul Winship, Chris Steele
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Patent number: 12202819Abstract: Substituted pyridazinone compounds, conjugates, and pharmaceutical compositions for use in the treatment of neuromuscular diseases, such as Duchenne Muscular Dystrophy (DMD), are disclosed herein. The disclosed compounds are useful, among other things, in the treating of DMD and modulating inflammatory inhibitors IL-1, IL-6 or TNF-?.Type: GrantFiled: September 1, 2023Date of Patent: January 21, 2025Assignee: EDGEWISE THERAPEUTICS, INC.Inventors: Kevin Hunt, Kevin Koch, Alan Russell, Stephen Schlachter, Paul Winship, Chris Steele
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Patent number: 12171229Abstract: The present invention relates to novel heteroaryl-triazole and heteroaryl-tetrazole compounds of the general formula (I), in which the structural elements Y, Q1, Q2, R1, R2, R3, R4 and R5 have the meaning given in the description, to formulations and compositions comprising such compounds and for their use in the control of animal pests including arthropods and insects in plant protection and to their use for control of ectoparasites on animals.Type: GrantFiled: August 11, 2023Date of Patent: December 24, 2024Assignee: BAYER AKTIENGESELLSCHAFTInventors: Alexander Arlt, Werner Hallenbach, Hans-Georg Schwarz, Martin Fuesslein, Heinz-Juergen Wroblowsky, Estella Buscato Arsequell, Marc Linka, Kerstin Ilg, Arunas Jonas Damijonaitis, Ulrich Ebbinghaus-Kintscher, Ulrich Goergens, Yolanda Cancho Grande, Peter Jeschke, Joachim Telser, Iring Heisler, Andreas Turberg
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Patent number: 12012395Abstract: Substituted pyridazinone compounds, conjugates, and pharmaceutical compositions for use in the treatment of neuromuscular diseases, such as Duchenne Muscular Dystrophy (DMD), are disclosed herein. The disclosed compounds are useful, among other things, in the treating of DMD and modulating inflammatory inhibitors IL-1, IL-6 or TNF-?.Type: GrantFiled: June 11, 2021Date of Patent: June 18, 2024Assignee: Edgewise Therapeutics, Inc.Inventors: Kevin Hunt, Kevin Koch, Alan Russell, Stephen Schlachter, Paul Winship, Chris Steele
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Patent number: 11873290Abstract: Substituted pyridazinone compounds, conjugates, and pharmaceutical compositions for use in the treatment of neuromuscular diseases, such as Duchenne Muscular Dystrophy (DMD), are disclosed herein. The disclosed compounds are useful, among other things, in the treating of DMD and modulating inflammatory inhibitors IL-1, IL-6 or TNF-?.Type: GrantFiled: June 11, 2021Date of Patent: January 16, 2024Assignee: Edgewise Therapeutics, Inc.Inventors: Kevin Hunt, Kevin Koch, Alan Russell, Stephen Schlachter, Paul Winship, Chris Steele
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Patent number: 11833144Abstract: A method for treating a mammal having an autoimmune disease, wherein said method comprises administering a SCD1 polypeptide inhibitor to said mammal, wherein said SCD1 polypeptide inhibitor is a compound having Formula (II): or a pharmaceutically acceptable salt thereof; wherein: R1 is halo; X is —(C?O)NR4—; Y is ?and R2, R3, and R4 are each independently H or an unsubstituted alkyl.Type: GrantFiled: August 24, 2021Date of Patent: December 5, 2023Assignee: Mayo Foundation for Medical Education and ResearchInventors: John A. Copland, III, Hu Zeng
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Patent number: 11786500Abstract: Disclosed herein are methods of treating a tumor or cancer in a subject whose tumor or cancer cells express low levels of asparagine synthetase (ASNS), and compounds and compositions useful in such treatment. Also disclosed herein are methods of evaluating whether to administer a compound that inhibits glutathione production or a glutaminase inhibitor to a subject with a tumor or cancer.Type: GrantFiled: May 21, 2021Date of Patent: October 17, 2023Assignee: Board of Regents, The University of Texas SystemInventors: Timothy Heffernan, Jeffrey Kovacs, Nakia Spencer, Christopher Bristow
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Patent number: 11702411Abstract: The present disclosure is directed to inhibitors of SHP2 and their use in the treatment of disease. Also disclosed are pharmaceutical compositions comprising the same.Type: GrantFiled: April 10, 2020Date of Patent: July 18, 2023Assignee: REVOLUTION MEDICINES, INC.Inventors: Jie Jack Li, Elena S. Koltun, Adrian Liam Gill, Andreas Buckl, Walter Won, Naing Aay, Kevin Mellem, Christos Tzitzilonis, Ashutosh Jogalekar, James Joseph Cregg
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Patent number: 11560390Abstract: Provided herein are compounds that inhibit the phosphorylation of MAPK and thus are useful in compositions and methods for treating cancer and inflammatory disease.Type: GrantFiled: September 16, 2020Date of Patent: January 24, 2023Assignee: SHY Therapeutics LLCInventors: Yaron R. Hadari, Luca Carta, Michael Schmertzler, Theresa M. Williams, Charles H. Reynolds
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Patent number: 11485740Abstract: The present invention relates to compounds of formula (I) and pharmaceutically acceptable salts therefore, wherein R1 to R6, A, U, V, W, X, Y, and Z are as defined herein. The invention also relates to pharmaceutical compositions comprising these compounds, methods of using these compounds in the treatment of various diseases and disorders, processes for preparing these compounds and intermediates useful in these processes.Type: GrantFiled: February 13, 2019Date of Patent: November 1, 2022Assignees: Boehringer Ingelheim International GmbH, Hydra Biosciences, LLCInventors: Steven Brunette, Jianwen Cui, Michael D. Lowe, Christopher Ronald Sarko, Simon Surprenant, Michael Robert Turner, Xinyuan Wu, Lana Louise Smith Keenan, Thierry Bouyssou, Paul Nicklin
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Patent number: 11369603Abstract: The invention relates to the use of a H3R inverse agonist for the treatment of shift work disorder.Type: GrantFiled: April 17, 2018Date of Patent: June 28, 2022Assignee: NOVARTIS AGInventors: Donald Johns, Klaus Kucher, Judit Sovago
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Patent number: 11185590Abstract: A preserved liquid aqueous pharmaceutical composition includes one or more etherified cyclodextrin derivatives, at least one water-soluble preservative, and at least one pharmaceutically active compound which is poorly water-soluble, very poorly water-soluble or water-insoluble. The liquid aqueous pharmaceutical composition provides an acceptable solubility of the pharmaceutically active compound, such as pimobendan, in aqueous solution whereby the water-soluble preservatives retain their effectiveness in the presence of the etherified cyclodextrin derivatives allowing the use in an oral administration form.Type: GrantFiled: July 27, 2018Date of Patent: November 30, 2021Assignee: BOEHRINGER INGELHEIM VETMEDICA GMBHInventors: Michael Aven, Tim Lukas
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Patent number: 11180502Abstract: The invention provides azaspiro[4.5]decane derivatives of Formula (A): and pharmaceutically acceptable salts, solvates, hydrates, N-oxides, and diastereomers thereof, wherein A1, X, A2, Rr, R2?, W1, W2, R3?, R4?, a, and b are defined in the disclosure. The invention also provides compounds of Formulae I, and B-G, and pharmaceutically acceptable salts, solvates, hydrates, N-oxides, and diastereomers thereof. Further, the invention provides use of the compounds of Formulae A-G and I, and the pharmaceutically acceptable salts, solvates, hydrates, N-oxides, and diastereomers thereof, to treat pain. In certain embodiments, Compounds of the Disclosure are useful for treating a disorder responsive to blockade of one or more sodium channels.Type: GrantFiled: January 12, 2018Date of Patent: November 23, 2021Assignee: Purdue Pharma L.P.Inventors: Mark A. Youngman, Laykea Tafesse, Jae Hyun Park
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Patent number: 11091464Abstract: Substituted pyridazinone compounds, conjugates, and pharmaceutical compositions for use in the treatment of neuromuscular diseases, such as Duchenne Muscular Dystrophy (DMD), are disclosed herein. The disclosed compounds are useful, among other things, in the treating of DMD and modulating inflammatory inhibitors IL-1, IL-6 or TNF-?.Type: GrantFiled: November 3, 2020Date of Patent: August 17, 2021Assignee: Edgewise Therapeutics, Inc.Inventors: Kevin Hunt, Kevin Koch, Alan Russell, Stephen Schlachter, Paul Winship, Chris Steele
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Patent number: 11066396Abstract: The present invention is directed to substituted 5-trifluoromethyl oxadiazole compounds of generic formula (I) or a pharmaceutically acceptable salt thereof. In particular, the invention is directed to a class of aryl and heteroaryl substituted 5-trifluoromethyl oxadiazole compounds of formula I which may be useful as HDAC6 inhibitors for treating cellular proliferative diseases, including cancer, neurodegenerative diseases, such as schizophrenia and stroke, as well as other diseases.Type: GrantFiled: June 19, 2017Date of Patent: July 20, 2021Assignee: MERCK SHARP & DOHME CORP.Inventors: Abbas Walji, Richard Berger, Craig A. Stump, Kelly-Ann S. Schlegel, James J. Mulhearn, Thomas J. Greshock, Deping Wang, Mark E. Fraley, Kristen G. Jones
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Patent number: 11045443Abstract: Disclosed herein are methods of treating a tumor or cancer in a subject whose tumor or cancer cells express low levels of asparagine synthetase (ASNS), and compounds and compositions useful in such treatment. Also disclosed herein are methods of evaluating whether to administer a compound that inhibits glutathione production or a glutaminase inhibitor to a subject with a tumor or cancer.Type: GrantFiled: June 3, 2020Date of Patent: June 29, 2021Assignee: Board of Regents, The University of Texas SystemInventors: Timothy Heffernan, Jeffrey Kovacs, Nakia Spencer, Christopher Bristow
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Patent number: 11020397Abstract: Bifunctional barbiturate-derivative compounds that increase uric acid excretion and reduce uric acid production, and monofunctional barbiturate-derivative compounds that either increase uric acid excretion or reduce uric acid production are provided. Methods of using these compounds for reducing uric acid levels in blood or serum, for treating disorders associated with excess uric acid, and for maintaining normal uric acid levels in blood or serum, or the whole body, are also provided. Pharmaceutical compositions comprising the bifunctional and monofunctional compounds are also provided.Type: GrantFiled: May 12, 2020Date of Patent: June 1, 2021Assignee: Acquist LLCInventors: Raymond P. Warrell, Jr., John J. Piwinski, Alexandre Larivée, Arshad Siddiqui, Karen Thai
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Patent number: 10973810Abstract: The present disclosure provides compounds and methods useful in the treatment of neurological disorders. The compounds of the invention, alone or in combination with other pharmaceutically active agents, can be used for treating or preventing neurological disorders.Type: GrantFiled: January 5, 2018Date of Patent: April 13, 2021Assignee: Yumanity Therapeutics, Inc.Inventors: Benjamin Vincent, Daniel Tardiff, Jeff Piotrowski, Eric Solis, Robert Scannevin, Chee-Yeun Chung, Rebecca Aron, Bertrand Le Bourdonnec, Matthew Lucas, Kenneth Rhodes
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Patent number: 10935526Abstract: A minimum peak is determined from analysis results, a correction wavelength at which an S/N ratio of the minimum peak is greatest is determined, and the determined correction wavelength is used to execute correction of the minimum peak. A plurality of detector output value correction method are registered in a processor, correction method is selected from default correction method or from among a plurality of preset correction methods according to an object to perform correction.Type: GrantFiled: December 16, 2019Date of Patent: March 2, 2021Assignee: HITACHI HIGH-TECH SCIENCE CORPORATIONInventors: Shuhei Yamamura, Daisuke Akieda, Ayumi Nakaogami, Katsutoshi Shimizu
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Patent number: 10899744Abstract: Provided are a compound as represented by structural formula (I) ({5-[(1R)-1-(2,6-dichloro-3-fluorophenyl)ethoxy]-6-aminopyridazin-3-yl}-N-{4-[((3S,5R)-3,5-di methylpiperazinyl)carbonyl]phenyl}carboxamide hydrochloride) and a novel crystalline form of a hydrate or solvate of the compound. Further provided are a manufacturing method of the compound and crystalline form, a related intermediate, a pharmaceutical composition comprising the compound, an application using the compound or the crystalline form for preparing a pharmaceutical product for treating a disease, symptom, or disorder, and a therapeutic method for treating a disease, symptom, or disorder.Type: GrantFiled: June 1, 2017Date of Patent: January 26, 2021Assignee: XCOVERY HOLDINGS, INC.Inventors: Congxin Liang, Yongbin Ma, Wei He
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Patent number: 10722487Abstract: Disclosed herein are methods of treating a tumor or cancer in a subject whose tumor or cancer cells express low levels of asparagine synthetase (ASNS), and compounds and compositions useful in such treatment. Also disclosed herein are methods of evaluating whether to administer a compound that inhibits glutathione production or a glutaminase inhibitor to a subject with a tumor or cancer.Type: GrantFiled: October 18, 2018Date of Patent: July 28, 2020Assignee: Board of Regents, The University of Texas SystemInventors: Timothy Heffernan, Jeffrey Kovacs, Nakia Spencer, Christopher Bristow
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Patent number: 10703752Abstract: The present invention relates to novel integrin antagonists of Formula I and their use as a medicament, in particular for inhibiting neovascularization.Type: GrantFiled: August 19, 2019Date of Patent: July 7, 2020Assignee: OXURION NVInventors: Ove Pedersen, Elke Vermassen
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Patent number: 10676538Abstract: Compounds inhibitory to Staphylococcus pseudintermedius Sortase A (SrtA) are identified. The compounds inhibit cell wall-associated protein anchoring to the bacterial cell wall, thus potentially reducing bacterial virulence.Type: GrantFiled: August 28, 2018Date of Patent: June 9, 2020Inventors: Stephen Anthony Kania, David Allen Bemis, Jerome Baudry, Manasi Balachandran
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Patent number: 10624948Abstract: The present invention refers to the use of protein kinase inhibitors and more specifically to the use of inhibitors of the protein kinase c-Jun amino terminal kinase, JNK inhibitor sequences, chimeric peptides, or of nucleic acids encoding same as well as pharmaceutical compositions containing same, for the treatment of various diseases or disorders strongly related to JNK signaling.Type: GrantFiled: June 26, 2014Date of Patent: April 21, 2020Assignee: XIGEN INFLAMMATION LTD.Inventors: Jean-Marc Combette, Catherine Deloche
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Patent number: 10414727Abstract: The present invention provides compounds, compositions thereof, and methods of using the same.Type: GrantFiled: November 8, 2017Date of Patent: September 17, 2019Assignee: Navitor Pharmaceuticals, Inc.Inventors: David John O'Neill, Eddine Saiah, Seong Woo Anthony Kang, Andrew Brearley, Jonathan Bentley
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Patent number: 10335416Abstract: The disclosure provides a method for treating NPM1-mutated acute myeloid leukemia (AML) by administration of a composition comprising dactinomycin.Type: GrantFiled: September 13, 2016Date of Patent: July 2, 2019Inventors: Brunangelo Falini, Maria Paola Martelli
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Patent number: 10287269Abstract: The present invention is directed to pyrimidine carboxamide compounds of formula I which are useful as therapeutic agents for the treatment of central nervous system disorders associated with phosphodiesterase 2 (PDE2). The present invention also relates to the use of such compounds for treating neurological and psychiatric disorders, such as schizophrenia, psychosis, Parkinson's disease, Parkinson's disease dementia (PDD), or Huntington's disease, and those associated with striatal hypofunction or basal ganglia dysfunction.Type: GrantFiled: March 21, 2016Date of Patent: May 14, 2019Assignee: Merck Sharp & Dohme Corp.Inventors: Dong-Ming Shen, Jonathan E. Wilson, Meng Yang, Dann Parker, Zack Zhiqiang Guo, Alejandro Crespo, Deping Wang, Troy McCracken
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Dendrogenin A and antineoplastic agents for the treatment of chemosensitive or chemoresistant tumors
Patent number: 10188666Abstract: Dendrogenin A and antineoplastic agents for the treatment of chemosensitive or chemoresistant tumors. The invention concerns a kit-of-parts comprising 5?-hydroxy-6?-[2-(1H-imidazol-4-yl)ethylamino]cholestan-3?-ol (Dendrogenin A) or a pharmaceutically acceptable salt thereof and an antineoplastic agent for use in the treatment of cancer. Furthermore, the invention concerns Dendrogenin A or a pharmaceutically acceptable salt thereof for use for treating a chemoresistant cancer.Type: GrantFiled: September 3, 2014Date of Patent: January 29, 2019Assignees: AFFICHEM, INSERM (INSTITUT NATIONAL DE LA SANTE ET DE LA RECHERCHE MEDICALE), CENTRE HOSPITALIER UNIVERSITAIRE DE TOULOUSEInventors: Philippe de Medina, Michael Paillasse, Christian Recher, Marc Poirot, Sandrine Silvente Poirot -
Patent number: 10149840Abstract: To provide an OCT3 activity inhibitor having a different basic skeleton than that of conventional OCT3 activity inhibitors. This inhibitor of organic cation transporter 3 (OCT3) contains, as an active component, an imidazo[1,2-a]pyridine derivative, a pharmaceutically acceptable salt thereof, or a pharmaceutically acceptable solvate thereof.Type: GrantFiled: September 15, 2017Date of Patent: December 11, 2018Assignee: SHIN NIPPON BIOMEDICAL LABORATORIES, LTD.Inventors: Hidetoshi Yamashita, Nobuyuki Suzuki
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Patent number: 10071162Abstract: The present invention is directed to a preserved liquid aqueous pharmaceutical composition comprising one or more etherified cyclodextrin derivatives; one or more water-soluble preservatives; preferably selected from the group consisting of sorbic acid or salts thereof, preferably sodium sorbate, potassium sorbate, calcium sorbate; benzoic acid or salts thereof, preferably sodium benzoate; benzalkonium chloride; benzethonium chloride; cetylpyridinium chloride; sodium metabisulfite; sodium acetate; parabenes and salts thereof, preferably methylparabene, ethylparabene, propylparabene, butylparabene, butylparabene sodium; or combinations thereof; and at least one pharmaceutically active compound which is poorly water-soluble, very poorly water-soluble or water-insoluble.Type: GrantFiled: July 18, 2014Date of Patent: September 11, 2018Assignee: BOEHRINGER INGELHEIM VETMEDICA GMBHInventors: Michael Aven, Tim Lukas
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Patent number: 9938265Abstract: A compound of Formula (I): or a pharmaceutically acceptable salt thereof, where: Q can be 5-methylpyridazin-3-yl,5-chloropyridazin-3-yl, 6-methylpyridazin-3-yl, or 6-fluoropyridazin-3-yl; R can be hydrogen, fluoro, or methoxy; R1 can be hydrogen, methoxy, difluoromethoxy, or trifluoromethoxy; and R2 can be methyl or ethyl. The compound of formula (I) can inhibit glutaminase, e.g., GLS1.Type: GrantFiled: November 29, 2016Date of Patent: April 10, 2018Assignees: AstraZeneca AB, Cancer Research Technology LimitedInventors: Johannes Wilhelmus Maria Nissink, Maurice Raymond Verschoyle Finlay, Mark David Charles, Matt Wood
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Patent number: 9839636Abstract: Disclosed herein are analogues of itraconazole that are both angiogenesis and hedgehog signaling pathway inhibitors. The compounds are expected to be useful in the treatment of cancer, particularly cancers that are dependent upon the hedgehog signaling pathway such as basal cell carcinoma and medulloblastoma.Type: GrantFiled: April 7, 2017Date of Patent: December 12, 2017Assignee: UNIVERSITY OF CONNECTICUTInventors: Matthew Kyle Hadden, Upasana Banerjee
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Patent number: 9708290Abstract: Compounds of Formula I or a stereoisomer, tautomer, prodrug or pharmaceutically acceptable salt thereof are provided, which are useful for the treatment of hyperproliferative, pain and inflammatory diseases. Methods of using compounds of Formula I or a stereoisomer, tautomer, prodrug or pharmaceutically acceptable salt thereof, for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions are disclosed.Type: GrantFiled: January 12, 2016Date of Patent: July 18, 2017Assignees: Array BioPharma Inc., Genentech, Inc.Inventors: James F. Blake, Mark Joseph Chicarelli, Rustam Ferdinand Garrey, John Gaudino, Jonas Grina, David A. Moreno, Peter J. Mohr, Li Ren, Jacob Schwarz, Huifen Chen, Kirk Robarge, Aihe Zhou
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Patent number: 9682083Abstract: The present invention relates to 6-amino-7-deaza-purine derivatives which modulate the activity of protein kinases and are therefore useful in treating diseases caused by dysregulated protein kinase activity, in particular RET family kinases. The present invention also provides methods for preparing these compounds, pharmaceutical compositions comprising these compounds, and methods of treating diseases utilizing pharmaceutical compositions containing these compounds.Type: GrantFiled: May 7, 2014Date of Patent: June 20, 2017Assignee: NERVIANO MEDICAL SCIENCES S.R.L.Inventors: Mauro Angiolini, Laura Buffa, Maria Menichincheri, Ilaria Motto, Paolo Polucci, Gabriella Traquandi, Fabio Zuccotto
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Patent number: 9611262Abstract: The present invention is directed to compounds of Formula I: Methods of making the compounds of Formula I are also described. The invention also relates to pharmaceutical compositions comprising compounds of Formula I. Methods of using the compounds of the invention are also within the scope of the invention.Type: GrantFiled: September 11, 2015Date of Patent: April 4, 2017Assignee: Janssen Pharmaceutica NVInventors: Brock T. Shireman, Terry P. Lebold, Curt A. Dvorak, Heather R. Coate, Jeannie M. Ziff, Cathy Preville, Christine Gelin, Gang Chen
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Patent number: 9604962Abstract: Disclosed are compounds of Formulae 1, 1A, 1B and 1C including all geometric and stereoisomers, N-oxides, and salts thereof, wherein R1, R2, R4a1, R4a2, A, Aa, G, M, W, Z1, Z3, X, J, J1 and n are as defined in the disclosure. Also disclosed are compositions containing the compounds of Formula 1 and methods for controlling plant disease caused by a fungal pathogen comprising applying an effective amount of a compound or a composition of the invention.Type: GrantFiled: June 24, 2015Date of Patent: March 28, 2017Assignee: E I DU PONT DE NEMOURS AND COMPANYInventors: Robert James Pasteris, Rafael Shapiro
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Patent number: 9505752Abstract: Compounds of Formula I, including pharmaceutically acceptable salts thereof: formula (I): wherein A is selected from the group consisting of: formula (II) and wherein Z is selected from the group consisting of: formula (III): and. are useful as HIV attachment inhibitors.Type: GrantFiled: August 7, 2013Date of Patent: November 29, 2016Assignee: ViiV Healthcare UK (No. 5) LimitedInventors: Tao Wang, Zhongxing Zhang, John F. Kadow, Nicholas A. Meanwell, Edward H. Ruediger, Clint A. James, Daniel H. Deon, David J. Carini, Barry L. Johnson
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Patent number: 9499567Abstract: The invention further relates to a DGAT inhibitor of formula including any stereochemically isomeric form thereof, wherein A represents CH or N; the dotted line represents an optional bond in case A represents a carbon atom; X represents —NRx—C(?O)—; —Z—C(?O)—; —Z—NRx—C(?O)—; —S(?O)p-; —C(?S)—; —NRx—C(?S)—; —Z—C(?S)—; —Z—NRx—C(?S)—; —O—C(?O)—; —C(?O)—C(?O)—; R1 represents a 5-membered monocyclic heterocycle containing at least 2 heteroatoms; a 6-membered aromatic monocyclic heterocycle; or a 5-membered heterocycle containing at least 2 heteroatoms fused with phenyl, cyclohexyl or a 5- or 6-membered heterocycle; wherein each of said heterocycles may optionally be substituted; R2 represents R3; R3 represents C3-6cycloalkyl, phenyl, naphtalenyl, 2,3-dihydro-1,4-benzodioxinyl, 1,3-benzodioxolyl, 2,3-dihydrobenzofuranyl or a 6-membered aromatic heterocycle containing 1 or 2 N atoms, wherein said C3-6cycloalkyl, phenyl, naphtalenyl, 2,3-dihydro-1,4-benzodioxinyl, 1,3-benzodioxolyl, 2,3-dihydrobenzofuranyl or 6-Type: GrantFiled: July 20, 2015Date of Patent: November 22, 2016Assignee: Janssen Pharmaceutica N.V.Inventors: Jean-Pierre Andre Marc Bongartz, Lieven Meerpoel, Gustaaf Maria Boeckx, Guy Rosalia Eugeen Van Lommen, Christophe Francis Robert Nestor Buyck, Daniel Obrecht, Philipp Ermert, Anatol Luther
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Patent number: 9463199Abstract: The invention relates to the use of a phosphodiesterase type III (PDE III) inhibitor or Ca2+-sensitizing agent or a pharmaceutically acceptable derivative thereof for the preparation of a medication for the reduction of the heart size of a patient suffering from heart failure.Type: GrantFiled: March 23, 2005Date of Patent: October 11, 2016Assignee: Boehringer Ingelheim Vetmedica GmbHInventors: Juergen Daemmgen, Olaf Joens, Rainer Kleemann
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Patent number: 9434721Abstract: A compound of formula: wherein Ar1, A, R3, x, and m are as disclosed herein and Ar2 is a benzothiazolyl, benzooxazolyl, or benzoimidazolyl group or a pharmaceutically acceptable salt thereof (a “Benzoazolylpiperazine Compound”), compositions comprising a Benzoazolylpiperazine Compound, and methods for treating or preventing pain, UI, an ulcer, IBD, IBS, an addictive disorder, Parkinson's disease, parkinsonism, anxiety, epilepsy, stroke, a seizure, a pruritic condition, psychosis, a cognitive disorder, a memory deficit, restricted brain function, Huntington's chorea, amyotrophic lateral sclerosis, dementia, retinopathy, a muscle spasm, a migraine, vomiting, dyskinesia, or depression in an animal comprising administering to an animal in need thereof an effective amount of a Benzoazolylpiperazine Compound are disclosed.Type: GrantFiled: December 6, 2013Date of Patent: September 6, 2016Assignee: Purdue Pharma L.P.Inventors: Qun Sun, Laykea Tafesse, Sam Victory
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Patent number: 9422296Abstract: The present invention relates to 4-aryl-6-piperazin-1-yl-3-substituted-pyridazines that are fast dissociating dopamine 2 receptor antagonists, processes for preparing these compounds, pharmaceutical compositions comprising these compounds as an active ingredient. The compounds find utility as medicines for treating or preventing central nervous system disorders, for example schizophrenia, by exerting an antipsychotic effect without motor side effects.Type: GrantFiled: July 28, 2014Date of Patent: August 23, 2016Assignee: JANSSEN PHARMACEUTICA NVInventors: Gregor James Macdonald, Xavier Jean Michel Langlois, José Manuel Bartolomé-Nebreda, Michiel Luc Maria Van Gool
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Patent number: 9409871Abstract: The present invention relates to compounds of formula I: in which L, W, X, Y, Z, m, p, R1, R2, R3, R4 and R7 are defined in the Summary of the Invention; capable of inhibiting the Hedgehog and Smo signaling pathway. 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 and compositions in the diagnosis and treatment of pathologies relating to the Hedgehog and Smo signaling pathway, for example, tumor formation, cancer, neoplasia and non-malignant hyperproliferative disorders.Type: GrantFiled: May 30, 2013Date of Patent: August 9, 2016Assignee: NOVARTIS AGInventors: Feng He, Stefan Peukert, Karen Marie Miller-Moslin, Naeem Yusuff, Zhuoliang Chen, Bharat Lagu
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Patent number: 9353104Abstract: The present invention is directed to substituted pyridizinone compounds of formula I which are useful as therapeutic agents for the treatment of central nervous system disorders associated with phosphodiesterase 10 (PDE10). The present invention also relates to the use of such compounds for treating neurological and psychiatric disorders, such as schizophrenia, psychosis or Huntington's disease, and those associated with striatal hypofunction or basal ganglia dysfunction.Type: GrantFiled: March 10, 2014Date of Patent: May 31, 2016Assignee: Merck Sharp & Dohme Corp.Inventors: Scott D. Kuduk, Casey C. McComas, Thomas S. Reger, Changhe Qi
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Patent number: 9315381Abstract: To provide a catalyst for dehydrogenation of formic acid which allows hydrogen, heavy hydrogen gas or heavy-hydrogenated hydrogen containing no carbon monoxide to be produced through dehydrogenation of formic acid in a highly efficient manner. A catalyst for dehydrogenation of formic acid, including: a multinuclear metal complex represented by the following Formula (1), a tautomer or stereoisomer thereof, or a salt thereof, where M1 and M2 denote transition metals and may be the same as or different from each other; Q1 to Q6 each independently denote carbon or nitrogen; R1 to R6 each independently denote, for example, a hydrogen atom, an alkyl group, a phenyl group, a nitro group, a halogen group, a sulfonate group (sulfo group); L1 and L2 each independently denote an aromatic anionic ligand or an aromatic ligand, and may be substituted by one or more substituents; Y1 and Y2 each independently denote any ligand or are absent; and m denotes a positive integer, 0, or a negative integer.Type: GrantFiled: January 25, 2013Date of Patent: April 19, 2016Assignee: NATIONAL INSTITUTE OF ADVANCED INDUSTRIAL SCIENCE AND TECHNOLOGYInventors: Yuichiro Himeda, Wan-Hui Wang
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Patent number: 9289427Abstract: The present invention relates to 3-(1-{3-[5-(1-methyl-piperidin-4-ylmethoxy)-pyrimidin-2-yl]-benzyl}-6-oxo-1,6-dihydro-pyridazin-3-yl)-benzonitrile hydrochloride solvates and crystalline modifications thereof. The present invention further relates to processes of manufacturing these crystalline modifications as well as their use in the treatment and/or prophylaxis of physiological and/or pathophysiological conditions, which are caused, mediated and/or propagated by the inhibition, regulation and/or modulation of signal transduction of kinases, in particular by the inhibition of tyrosine kinases, e.g. pathophysiological conditions such as cancer.Type: GrantFiled: January 17, 2014Date of Patent: March 22, 2016Assignee: MERCK PATENT GMBHInventors: Axel Becker, Clemens Kuehn, Christoph Saal, Oliver Schadt, Dieter Dorsch, Heinz-Hermann Bokel, Frank Stieber, Cristina Donini
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Patent number: 9283208Abstract: Medicaments and methods for treating cancer are disclosed.Type: GrantFiled: May 17, 2012Date of Patent: March 15, 2016Assignee: NIIKI PHARMA INC.Inventor: Hooshmand Sheshbaradaran
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Patent number: 9095846Abstract: The invention relates to a ligand that may be used to create a catalyst including a coordination complex is formed by the addition of two metals; Cp, Cp* or an unsubstituted or substituted ?-arene; and two coordinating solvent species or solvent molecules. The bimetallic catalyst may be used in the hydrogenation of CO2 to form formic acid and/or salts thereof, and in the dehydrogenation of formic acid and/or salts thereof to form H2 and CO2.Type: GrantFiled: September 12, 2012Date of Patent: August 4, 2015Assignees: Brookhaven Science Associates, LLC, National Institute of Advanced Industrial Science and Technology (AIST)Inventors: Jonathan F. Hull, Yuichiro Himeda, Etsuko Fujita, James T. Muckeman
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Publication number: 20150148351Abstract: The present invention relates to 3-(1-{3-[5-(1-methyl-piperidin-4-ylmethoxy)-pyrimidin-2-yl]-benzyl}-6-oxo-1,6-dihydro-pyridazin-3-yl)-benzonitrile hydrochloride solvates and crystalline modifications thereof. The present invention further relates to processes of manufacturing these crystalline modifications as well as their use in the treatment and/or prophylaxis of physiological and/or pathophysiological conditions, which are caused, mediated and/or propagated by the inhibition, regulation and/or modulation of signal transduction of kinases, in particular by the inhibition of tyrosine kinases, e.g. pathophysiological conditions such as cancer.Type: ApplicationFiled: January 29, 2015Publication date: May 28, 2015Applicant: MERCK PATENT GMBHInventors: Axel BECKER, Clemens KUEHN, Christoph SAAL, Oliver SCHADT, Dieter DORSCH, Heinz-Hermann BOKEL, Frank STIEBER, Cristina DONINI
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Patent number: 9040537Abstract: The present invention relates to pyridazine compounds of formulae I or II and the salts thereof, the N-oxides thereof and the salts of the N-oxides thereof, where the radical A is of the formula A, wherein # denotes the point of attachment to the remainder of formulae I or II, and wherein A1 is N or C—RA1, A2 is N or C—RA2, A3 is N or C—RA3, A4 is N or C—RA4 and A5 is N or C—RA5, provided that one or two of the variables A1, A2, A3, A4 or A5 is N; RA1, RA5, if present, are H, halogen, CN, NO2, C1-C6-alkyl, C1-C6-haloalkyl and the like; RA2, RA4, if present, are H, halogen, CN, NO2, C1-C10-alkyl, C1-C10-haloalkyl and the like; RA3, if present, is H, halogen, CN, NO2, C1-C10-alkyl, C1-C10-haloalkyl and the like; where W is N or C—RW and V is N or C—RV, provided that one of the variables W or V is N; Rt and Rw, if present, are H, halogen, methyl, C1-haloalkyl and the like; Ru and Rv, if present, are H, halogen, C1-C4-alkyl, C1-C3-haloalkyl and the like; X1 is S, O or NR1a, wherein R1a is H, C1-C10-alkylType: GrantFiled: March 23, 2011Date of Patent: May 26, 2015Assignee: BASF SEInventors: Ronan Le Vezouet, Sebastian Soergel, Christian Defieber, Steffen Gross, Karsten Koerber, Wolfgang Von Deyn, Douglas D. Anspaugh, Deborah L. Culbertson
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Patent number: RE48622Abstract: A series of pyrazolo[3,4-d]pyrimidine derivatives that are substituted at the 4-position by a diaza monocyclic, bridged bicyclic or spirocyclic moiety, are beneficial in the treatment and/or prevention of various human ailments, including inflammatory, autoimmune and oncological disorders; viral diseases and malaria; and organ and cell transplant rejection.Type: GrantFiled: July 22, 2019Date of Patent: July 6, 2021Assignees: UCB Biopharma SRL, Katholieke Universiteit Leuven, K.U. Leuven R&DInventors: Daniel James Ford, Richard Jeremy Franklin, Anant Ramrao Ghawalkar, Helen Tracey Horsley, Qiuya Huang, James Thomas Reuberson, Bart Vanderhoydonck