Polycyclo Ring System Having The Oxazole Ring As One Of The Cyclos Patents (Class 514/375)
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Patent number: 12042543Abstract: Disclosed are covalent inhibitors of enhancer zeste homolog 2 (EZH2) which may be utilized as EZH2 targeting agents. The disclosed compounds may be characterized as substituted 3-amino-5-phenylbenzamide compounds. The disclosed compounds may be utilized as covalent inhibitors of EZH2 and further may be derivatized to form proteolysis-targeting chimeric molecules (PROTACs) that target EZH2 for degradation. The disclosed compounds and PROTACs may be used in pharmaceutical compositions and methods for treating cell proliferative disorders associated with EZH2 activity, such as cancer.Type: GrantFiled: May 2, 2022Date of Patent: July 23, 2024Assignee: Northwestern UniversityInventors: Gary E. Schiltz, Jindan Yu
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Patent number: 11952371Abstract: A 2-[(1,3-benzoxazol-2-yl)imino]-5,5-diphenylimidazolidin-4-one compound, its synthesis, and its use as an antimicrobial agent.Type: GrantFiled: October 24, 2023Date of Patent: April 9, 2024Assignee: KING FAISAL UNIVERSITYInventors: Hany Mohamed Abd El-Lateef Ahmed, Mai Mostafa Khalaf Ali, Amer A. Amer, Antar Ahmed Abdelhamid Ahmed
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Patent number: 11786518Abstract: The present invention provides a reproxalap ophthalmic solution, and methods of using the same for treating a disease or disorder such as allergic conjunctivitis.Type: GrantFiled: March 20, 2020Date of Patent: October 17, 2023Assignee: Aldeyra Therapeutics, Inc.Inventors: David Clark, Susan Macdonald, Stephen Gitu Machatha, Lise Lund Kjems
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Patent number: 11759456Abstract: Provided is a pharmaceutical composition containing pemafibrate, a salt thereof or a solvate thereof and having excellent homogeneity. The pharmaceutical composition contains pemafibrate, a salt thereof or a solvate thereof in an amount of 0.017 to 4.2 mass % in terms of a free form of pemafibrate with respect to the total mass of the pharmaceutical composition.Type: GrantFiled: June 29, 2018Date of Patent: September 19, 2023Assignee: KOWA COMPANY, LTD.Inventors: Shin Sugimoto, Akito Minamizono
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Patent number: 11564899Abstract: It is provided a catechol-O-methyltransferase (COMT) inhibitor for use in the prevention and/or treatment of transthyretin-associated amyloidosis. It is also provided a catechol-O-methyltransferase (COMT) inhibitor for use in the prevention and/or treatment of transthyretin-associated amyloidosis in combination therapy with another COMT inhibitor, a benzoxazole derivative, iododiflunisal, diflunisal, resveratrol, tauroursodeoxycholic acid, doxocycline, or epigallocatechin-3-gallate.Type: GrantFiled: August 28, 2020Date of Patent: January 31, 2023Assignee: SOM Innovation Biotech, S.L.Inventors: Marc Centellas Casado, Raúl Insa Boronat, Nuria Reig Bolaño, Núria Gavaldà Batalla
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Patent number: 11554110Abstract: To provide a medicament for safely treating a patient in need of treatment with pemafibrate, a salt thereof, or a solvate of any of these (hereinafter also referred to as pemafibrate therapy). A medicament for treating a patient in need of pemafibrate therapy, the medicament comprising the step of avoiding or suspending concomitant use of pemafibrate, a salt thereof, or a solvate of any of these as an active ingredient in order to suppress an increase in plasma concentration of pemafibrate when the treatment is combined with a medicament containing an OATP1B inhibitor, or the step of reducing the dose of pemafibrate, a salt thereof, or a solvate of any of these.Type: GrantFiled: March 30, 2022Date of Patent: January 17, 2023Inventors: Ryu Oshima, Masatoshi Ito, Chisato Nagai
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Patent number: 11465997Abstract: In one aspect, the present disclosure provides disorazole analogs of the formula: Formula (I) wherein the variables are as defined herein. In another aspect, the present disclosure also provides methods of preparing the compounds disclosed herein. In another aspect, the present disclosure also provides pharmaceutical compositions and methods of use of the compounds disclosed herein. Additionally, drug conjugates with cell targeting moieties of the compounds are also provided.Type: GrantFiled: June 21, 2018Date of Patent: October 11, 2022Assignee: William Marsh Rice UniversityInventors: Kyriacos C. Nicolaou, Gabriel Bellavance, Marek Buchman, Kiran Kumar Pulukuri, Stephan Rigol
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Patent number: 11298340Abstract: Provided is a pharmaceutical composition which contains pemafibrate, a salt thereof or a solvate thereof and has excellent stability. A pharmaceutical composition is provided containing pemafibrate, a salt thereof or a solvate thereof and having a moisture content of 2.4 mass % or less.Type: GrantFiled: June 29, 2018Date of Patent: April 12, 2022Assignee: KOWA COMPANY, LTD.Inventors: Shin Sugimoto, Akito Minamizono
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Patent number: 11091452Abstract: A polymerizable compound has a practical low melting point, excellent solubility in a general-purpose solvent, and can produce an optical film at low cost, exhibits low reflected luminance, and achieves uniform conversion of polarized light over a wide wavelength band, an optically anisotropic article.Type: GrantFiled: October 8, 2019Date of Patent: August 17, 2021Assignee: ZEON CORPORATIONInventors: Kei Sakamoto, Satoshi Kiriki, Kumi Okuyama, Kanako Taira
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Patent number: 10980810Abstract: The present disclosure provides methods and compositions for treating, stabilizing or lessening the severity or progression of a non-alcoholic fatty liver disease.Type: GrantFiled: October 5, 2018Date of Patent: April 20, 2021Assignee: Gilead Sciences, Inc.Inventors: Jamie Geier Bates, Adrian S. Ray
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Patent number: 10786473Abstract: It is provided a catechol-O-methyltransferase (COMT) inhibitor for use in the prevention and/or treatment of trans-thyretin-associated amyloidosis. It is also provided a catechol-O-methyltransferase (COMT) inhibitor for use in the prevention and/or treatment of transthyretin-associated amyloidosis in combination therapy with another COMT inhibitor, a benzoxazole derivative, iododiflunisal, diflunisal, resveratrol, tauroursodeoxycholic acid, doxocycline, or epigallocatechin-3-gallate.Type: GrantFiled: September 12, 2019Date of Patent: September 29, 2020Assignee: SOM Innovation Biotech, S.L.Inventors: Marc Centellas Casado, Raúl Insa Boronat, Nuria Reig Bolaño, Núria Gavaldà Batalla
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Patent number: 10759768Abstract: The present invention provides a prophylactic or therapeutic agent for an autism spectrum disorder containing compound (I) having melatonin receptor affinity. A compound represented by the formula: wherein each symbol is as described in the specification, or a salt thereof.Type: GrantFiled: January 5, 2017Date of Patent: September 1, 2020Assignee: TAKEDA PHARMACEUTICAL COMPANY LIMITEDInventors: Keisuke Hirai, Takashi Ishikawa
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Patent number: 10449169Abstract: It is provided a catechol-O-methyltransferase (COMT) inhibitor for use in the prevention and/or treatment of transthyretin-associated amyloidosis. It is also provided a catechol-O-methyltransferase (COMT) inhibitor for use in the prevention and/or treatment of transthyretin-associated amyloidosis in combination therapy with another COMT inhibitor, a benzoxazole derivative, iododiflunisal, diflunisal, resveratrol, tauroursodeoxycholic acid, doxocycline, or epigallocatechin-3-gallate.Type: GrantFiled: August 13, 2018Date of Patent: October 22, 2019Assignee: SOM Innovation Biotech, S.L.Inventors: Marc Centellas Casado, Raúl Insa Boronat, Núria Reig Bolano, Nuria Gavaldà Batalla
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Patent number: 10251869Abstract: A method of treating a bacterial infection in a subject in need thereof includes administering to the subject therapeutically effective amounts of at least one ?-lactam antibiotic and at least one bisthiazolidine metallo-?-lactamase inhibitor.Type: GrantFiled: March 20, 2017Date of Patent: April 9, 2019Assignee: CASE WESTERN RESERVE UNIVERSITYInventors: Robert Bonomo, Alejandro Jose Vila, S. Graciela Mahler
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Patent number: 10213416Abstract: The present invention relates to substituted benzoxazolone derivatives as acid ceramidase inhibitors, pharmaceutical compositions containing these inhibitors and methods of inhibiting acid ceramidase for the treatment of disorders in which modulation of the levels of ceramide is clinically relevant. The invention also provides substituted benzoxazolone derivatives for use in the treatment of cancer, inflammation, pain, inflammatory pain or pulmonary diseases.Type: GrantFiled: November 8, 2016Date of Patent: February 26, 2019Assignees: The Regents of the University of Chicago, Fondazione Istituto Italiano di TechnologiaInventors: Daniele Piomelli, Daniela Pizzirani, Anders Bach, Rita Scarpelli, Laurin Melzig, Marco Mor
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Patent number: 10076504Abstract: Provided herein are compounds, including enantiomerically pure forms thereof, and pharmaceutically acceptable salts or co-crystals and prodrugs thereof which have glucagon receptor antagonist or inverse agonist activity. Further, provided herein are pharmaceutical compositions comprising the same as well as methods of treating, preventing, delaying the time to onset or reducing the risk for the development or progression of a disease or condition for which one or more glucagon receptor antagonist is indicated, including Type I and II diabetes, insulin resistance and hyperglycemia. Moreover, provided herein are methods of making or manufacturing compounds disclosed herein, including enantiomerically pure forms thereof, and pharmaceutically acceptable salts or co-crystals and prodrugs thereof.Type: GrantFiled: June 11, 2015Date of Patent: September 18, 2018Inventor: Lin Zhi
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Patent number: 10045956Abstract: It is provided a catechol-O-methyltransferase (COMT) inhibitor for use in the prevention and/or treatment of transthyretin-associated amyloidosis. It is also provided a catechol-O-methyltransferase (COMT) inhibitor for use in the prevention and/or treatment of transthyretin-associated amyloidosis in combination therapy with another COMT inhibitor, a benzoxazole derivative, iododiflunisal, diflunisal, resveratrol, tauroursodeoxycholic acid, doxocycline, or epigallocatechin-3-gallate.Type: GrantFiled: March 2, 2017Date of Patent: August 14, 2018Assignee: SOM Innovation Biotech, S.L.Inventors: Marc Centellas Casado, Raúl Insa Boronat, Núria Reig Bolano, Nuria Gavaldà Batalla
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Patent number: 9610270Abstract: It is provided a catechol-O-methyltransferase (COMT) inhibitor for use in the prevention and/or treatment of transthyretin-associated amyloidosis. It is also provided a catechol-O-methyltransferase (COMT) inhibitor for use in the prevention and/or treatment of transthyretin-associated amyloidosis in combination therapy with another COMT inhibitor, a benzoxazole derivative, iododiflunisal, diflunisal, resveratrol, tauroursodeoxycholic acid, doxocycline, or epigallocatechin-3-gallate.Type: GrantFiled: October 23, 2012Date of Patent: April 4, 2017Assignee: SOM INNOVATION BIOTECH, S.L.Inventors: Marc Centellas Casado, Raúl Insa Boronat, Nuria Reig Bolaño, Núria Gavaldà Batalla
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Patent number: 9586917Abstract: A polymerizable compound has a practical low melting point, excellent solubility in a general-purpose solvent, and can produce an optical film at low cost, exhibits low reflected luminance, and achieves uniform conversion of polarized light over a wide wavelength band, an optically anisotropic article. A carbonyl compound is useful as a raw material for producing the polymerizable compound. (In the formula (I), Y1 to Y8 represent —C(?O)—O—, G1 and G2 represent a C1-20 divalent linear aliphatic group, Z1 and Z2 represent a C2-10 alkenyl group that is unsubstituted, or substituted with a halogen atom, Ax represents a C2-30 organic group with at least one aromatic ring, Ay represents a hydrogen atom or C1-20 alkyl group, A1 represents a trivalent aromatic group, A2 and A3 represent a C3-30 divalent alicyclic hydrocarbon group, A4 and A5 represent a C6-30 divalent aromatic group or the like, and Q1 represents a hydrogen atom.Type: GrantFiled: May 30, 2013Date of Patent: March 7, 2017Assignee: ZEON CORPORATIONInventors: Kei Sakamoto, Satoshi Kiriki, Kumi Okuyama, Kanako Taira
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Patent number: 9404915Abstract: The disclosure provides methods for analysis of disease cell response to a therapeutic agent. In embodiments, a method comprises administering the therapeutic agent to a disease cell sample from the subject in a device that measures at least one physiological parameter of a cell; determining whether a change occurs in the physiologic parameter of the disease cell sample in response to the therapeutic agent as compared to a baseline measurement or the physiological parameter before administration of the therapeutic agent, and selecting the therapeutic agent that results in the change in the at least one physiologic parameter. In embodiments, the disease cells are whole, viable, and/or label free.Type: GrantFiled: January 6, 2015Date of Patent: August 2, 2016Assignee: Celcuity LLCInventors: Lance Gavin Laing, Brian Francis Sullivan
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Patent number: 9249112Abstract: The present invention relates to solid forms of the N-methyl-D-glucamine (meglumine) salt of 6-carboxy-2-(3,5-dichlorophenyl)-benzoxazole and to methods for their preparation. The invention is also directed to pharmaceutical compositions containing at least one solid form and to the therapeutic or prophylactic use of such solid forms and compositions.Type: GrantFiled: September 12, 2012Date of Patent: February 2, 2016Assignee: PFIZER INC.Inventors: Richard Frederic Labaudiniere, Michael Henry O'Neill
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Patent number: 9067905Abstract: The invention provides sulphone compounds and their use in treating medical disorders, such as obesity. Pharmaceutical compositions and methods of making various sulphone compounds are provided. The compounds are contemplated to have activity against methionyl aminopeptidase 2.Type: GrantFiled: April 23, 2012Date of Patent: June 30, 2015Assignee: Zafgen, Inc.Inventors: Hazel J. Dyke, Susan M. Cramp, Thomas D. Pallin, Janusz J. Kulagowski, John G. Montana, Robert Zahler
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Publication number: 20150148256Abstract: A bioluminescence imaging-based high-throughput assay for inhibitors of ABCG2 is described. Compositions of inhibitors of ABCG2 and methods of using ABCG2 inhibitors are also described.Type: ApplicationFiled: August 21, 2014Publication date: May 28, 2015Applicant: THE JOHNS HOPKINS UNIVERSITYInventors: MARTIN GILBERT POMPER, YIMAO ZHANG, JOHN LATERRA
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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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Publication number: 20150126567Abstract: The invention relates to the compounds of formula I or its pharmaceutical acceptable salts, as well as polymorphs, solvates, enantiomers, stereoisomers and hydrates thereof. The pharmaceutical compositions comprising an effective amount of compounds of formula I, and methods for the treatment of familial amyloid polyneuropathy may be formulated for oral, buccal, rectal, topical, transdermal, transmucosal, intravenous, parenteral administration, syrup, or injection. Such compositions may be used to treatment of transthyretin-related hereditary amyloidosis, neurodegenerative diseases, amyloidosis, neuropathic pain, amyloid fibril formation and cardiomyopathy related diseases.Type: ApplicationFiled: February 27, 2013Publication date: May 7, 2015Inventor: Mahesh Kandula
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Patent number: 9024038Abstract: Inhibitors of HIV-1 protease and compositions containing them are described. Use of the inhibitors and compositions containing them to treat HIV, AIDS, and AIDS-related diseases is described.Type: GrantFiled: June 27, 2013Date of Patent: May 5, 2015Assignee: Purdue Research FoundationInventors: Arun K. Ghosh, Bruno D. Chapsal, Hiroaki Mitsuya, Cuthbert D. Martyr
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Publication number: 20150111935Abstract: The present invention relates to a novel class of 1,3-benzoxazol-2(3H)-ones and their use as a medicament, preferably as a dermatologic agent, and as a cosmetic. These novel compounds are particularly useful in treating and/or preventing inflammation, irritation, itching, pruritus, pain, oedema and/or pro-allergic or allergic conditions in a patient. Usually they are topically applied to the skin or mucosa in the form of a pharmaceutical or cosmetic composition comprising the compound and a pharmaceutically and/or cosmetically acceptable carrier.Type: ApplicationFiled: May 21, 2013Publication date: April 23, 2015Applicant: DR. AUGUST WOLFF GMBH & CO. KG ARZNEIMITTELInventors: Chrsitoph Abels, Ulrich Knie, Michael Soeberdt
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Patent number: 9012481Abstract: Novel benzoarylureido compounds and a use thereof for prevention and/or treatment of the neurodegenerative brain disease are provided. The neurodegenerative brain diseases may include Alzheimer's disease, dementia, Parkinson's disease, stroke, amyloidosis, Pick's disease, Lou Gehrig's disease, Huntington's disease, Creutzfeld-Jakob disease, and the like.Type: GrantFiled: December 29, 2009Date of Patent: April 21, 2015Assignee: Korea Institute of Science and TechnologyInventors: Hoh-Gyu Hahn, Kee-Dal Nam, Dong-Yun Shin, Chan-Ho Park, Sung-Woo Cho, Eun-A Kim, Ghil-Soo Nam, Kyung-Il Chol, Seon-Hee Seo, Hee-Sup Shin, Dong-Jin Kim, Ae-Nim Pae, Hye-Jin Chung, Hyun-Ah Choo, Hye-Whon Rhim, Yong-Seo Cho, Eun-Joo Roh, Gyo-Chang Keum, Kee-Hyun Choi, Kye-Jung Shin, Chan-Seong Cheong, Jae-Kyun Lee, Yong-Koo Kang, Young-Soo Kim, Woong-Seo Park, Key-Sun Kim, He-Sson Chung, Chi-Man Song, Sun-Joon Min, Eunice Eun-Kyeong Kim, Cheol-Ju Lee, Soon-Bang Kang
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Publication number: 20150105403Abstract: Described herein are compounds that are estrogen receptor modulators. Also described are pharmaceutical compositions and medicaments that include the compounds described herein, as well as methods of using such estrogen receptor modulators, alone and in combination with other compounds, for treating diseases or conditions that are mediated or dependent upon estrogen receptors.Type: ApplicationFiled: March 14, 2013Publication date: April 16, 2015Inventors: Nicholas D. Smith, Steven P. Govek, Mehmet Kahraman, Jackaline D. Julien, Johnny Y. Nagasawa, Karensa L. Douglas, Celine Bonnefous, Andiliy G. Lai
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Publication number: 20150099730Abstract: Disclosed are compounds, compositions and methods for treating various diseases, syndromes, conditions and disorders, including those mediated by inhibition of fatty acid synthase (FASN) enzyme, such as, cancer, obesity or related discorders, and liver related disorders. Such compounds are represented by formula (I) as follows: wherein L1, a, b, m, n, R1, R2, R3, R4, and R5 are defined herein.Type: ApplicationFiled: September 6, 2013Publication date: April 9, 2015Applicant: Janssen Pharmaceutica, NVInventor: Peter J. Connolly
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Publication number: 20150094329Abstract: A compound represented by formula (1) and an N-oxide thereof have excellent pest control effect. (In the formula, Het to which R1—S(O)n is bonded represents a five-membered aromatic heterocyclic ring represented by formula H1, H2, H3 or H4 (wherein Y1 represents an oxygen atom or the like; Y2 represents an oxygen atom or the like; G1, G2 and G3 may be the same or different and each represents a nitrogen atom or the like; R1 represents a C1-C6 alkyl group which may have one or more atoms or groups selected from the group X, or the like; and n represents 0, 1 or 2); A1 represents an oxygen atom or the like; A2 represents a nitrogen atom or the like; A3 represents a nitrogen atom or the like; and R2 and R3 may be the same or different and each represents a C1-C6 chain hydrocarbon group which may have one or more atoms or groups selected from the group X, or the like.Type: ApplicationFiled: May 23, 2013Publication date: April 2, 2015Inventors: Yoshihiko Nokura, Mai Ito, Chie Shimizu, Hajime Mizuno
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Patent number: 8993607Abstract: The invention provides compounds of formula I, II, and III as defined herein, as well as salts thereof. The compounds may have activity as anti-proliferative agents.Type: GrantFiled: August 1, 2008Date of Patent: March 31, 2015Assignee: Rutgers, The State University of New JerseyInventors: Edmond J. LaVoie, Joseph E. Rice
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Publication number: 20150087680Abstract: Provided herein are compounds, including enantiomerically pure forms thereof, and pharmaceutically acceptable salts or co-crystals and prodrugs thereof which have glucagon receptor antagonist or inverse agonist activity. Further, provided herein are pharmaceutical compositions comprising the same as well as methods of treating, preventing, delaying the time to onset or reducing the risk for the development or progression of a disease or condition for which one or more glucagon receptor antagonist is indicated, including Type I and II diabetes, insulin resistance and hyperglycemia. Moreover, provided herein are methods of making or manufacturing compounds disclosed herein, including enantiomerically pure forms thereof, and pharmaceutically acceptable salts or Co-crystals and prodrugs thereof.Type: ApplicationFiled: November 26, 2014Publication date: March 26, 2015Inventors: Jorge E. Gomez-Galeno, Scott J. Hecker, Qun Dang, Mali Venkat Reddy, Zhili Sun, Matthew P. Grote, Thanh Huu Nguyen, Robert Huerta Lemus, Haiqing Li
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Publication number: 20150072958Abstract: Various embodiments of the present invention relate to, among other things, compounds and methods of using those compounds to treat an HIV infection. The compounds of the various embodiments of the present invention provide, among other things, therapeutic agents having enhanced penetration capability across the blood-brain barrier, such that they can enter the CNS to treat an HIV-1 infection in the CNS.Type: ApplicationFiled: September 10, 2014Publication date: March 12, 2015Inventors: Arun K. Ghosh, Hiroaki Mitsuya, Sofiya Yashchuk
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Publication number: 20150057320Abstract: A method for treating a disease characterized by excessive lipofuscin accumulation in the retina of a mammal afflicted therewith comprising administering to the mammal an effective amount of a transthyretin (TTR) ligand.Type: ApplicationFiled: October 31, 2014Publication date: February 26, 2015Applicant: The Trustees of Columbia University in the City of New YorkInventor: Konstantin PETRUKHIN
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Patent number: 8957097Abstract: The present invention is directed to hemi phorboxazole A: and its stereoisomers, as well as derivatives of hemi phorboxazole A of formula I: wherein ring A is aryl or a 5- or 6-membered heteroaryl optionally substituted with one or more of halogen, —OH, or —C1-6alkyl; and R is —CN, a 5- or 6-membered heteroaryl, or halogen; and the pharmaceutically acceptable salt forms thereof, in addition to methods of using these compounds.Type: GrantFiled: July 23, 2010Date of Patent: February 17, 2015Assignees: The Trustees Of The University Of Pennsylvania, The Regents Of The University Of CaliforniaInventors: Amos B. Smith, III, Zhuqing Liu, Anne-Marie L. Hogan, Doralyn S. Dalisay, Tadeusz F. Molinski
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Publication number: 20150045402Abstract: A compound which is useful as a dopamine D1 receptor positive allosteric modulator (D1 PAM) is provided. The present inventors have studied a compound which has a dopamine D1 receptor positive allosteric modulating activity and is useful as an active ingredient of a pharmaceutical composition for preventing and/or treating cognitive impairment, negative symptoms of schizophrenia, Parkinson's disease, Alzheimer's disease, Huntington's disease, drug addictions, or the like, and they have thus found that a heterocyclic acetamide compound has a dopamine D1 receptor positive allosteric modulating activity, thereby completing the present invention. The heterocyclic acetamide compound of the present invention has a dopamine D1 receptor positive allosteric modulating activity and can be used as an agent for preventing and/or treating cognitive impairment, negative symptoms of schizophrenia, Parkinson's disease, Alzheimer's disease, Huntington's disease, drug addictions, or the like.Type: ApplicationFiled: October 28, 2014Publication date: February 12, 2015Applicant: ASTELLAS PHARMA INC.Inventors: Ryota Shiraki, Takahiko TOBE, Shimpei KAWAKAMI, Hiroyuki MORITOMO, Makoto OHMIYA
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Publication number: 20150045346Abstract: The invention provides compounds for selectively inhibiting glycosidases, prodrugs of the compounds, and pharmaceutical compositions including the compounds or prodrugs of the compounds. The invention also provides methods of treating diseases and disorders related to deficiency or overexpression of O-GlcNAcase, accumulation or deficiency of O-GlcNAc.Type: ApplicationFiled: June 27, 2012Publication date: February 12, 2015Applicants: MERCK SHARP & DOHME CORP., ALECTOS THERAPEUTICS INC.Inventors: Tong-Shuang Li, Ernest J. McEachern, David J. Vocadlo, Yuanxi Zhou, Harold G. Selnick
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Publication number: 20150045368Abstract: Compounds of Formula (I) and Formula (II) are useful inhibitors of tankyrase. Compounds of Formula (I) and Formula (II) have the following structure: where the definitions of the variables are provided herein.Type: ApplicationFiled: March 1, 2013Publication date: February 12, 2015Inventors: Howard Bregman, John L. Buchanan, Nagasree Chakka, Erin F. Dimauro, Hakan Gunaydin, Angel Guzman-Perez, Zihao Hua, Hongbing Huang, Xin Huang, Matthew W. Martin, Vinod F. Patel
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Patent number: 8952058Abstract: Provided herein are heterocyclic compounds for treatment of CSF1R, FLT3, KIT, and/or PDGFR? kinase mediated diseases. Also provided are pharmaceutical compositions comprising the compounds and methods of using the compounds and compositions.Type: GrantFiled: October 12, 2012Date of Patent: February 10, 2015Assignee: Ambit Biosciences CorporationInventors: Michael J. Hadd, Michael D. Hocker, Mark W. Holladay, Gang Liu, Martin W. Rowbottom, Shimin Xu
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Publication number: 20150031735Abstract: The present invention relates to solid forms of the N-methyl-D-glucamine (meglumine) salt of 6-carboxy-2-(3,5-dichlorophenyl)-benzoxazole and to methods for their preparation. The invention is also directed to pharmaceutical compositions containing at least one solid form and to the therapeutic or prophylactic use of such solid forms and compositions.Type: ApplicationFiled: September 12, 2012Publication date: January 29, 2015Inventors: Richard Frederic Labaudiniere, MICHAEL HENRY O'Neill
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Publication number: 20150031694Abstract: The invention provides compounds of formula (I): wherein R1-R7 and W have any of the values defined in the specification, and salts thereof. The compounds have good solubility and are useful for treating bacterial infections.Type: ApplicationFiled: March 21, 2013Publication date: January 29, 2015Inventors: Edmond J. LaVoie, Ajit Parhi, Yongzheng Zhang, Daniel S. Pilch, Malvika Kaul
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Patent number: 8940764Abstract: Compositions and methods for treating macular degeneration and other forms of retinal disease whose etiology involves the accumulation of A2E and/or lipofuscin, and, more specifically, for preventing the formation and/or accumulation of A2E are disclosed.Type: GrantFiled: May 26, 2006Date of Patent: January 27, 2015Assignee: Aldexa Therapeutics, Inc.Inventors: Thomas A. Jordan, John E. Dowling, John Clifford Chabala
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Publication number: 20150018398Abstract: Disclosed herein are methods useful for treating radiation damage in a subject.Type: ApplicationFiled: July 15, 2014Publication date: January 15, 2015Inventors: Richard J. Pietras, Michael E. Jung
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Publication number: 20150018388Abstract: The present invention relates to the identification of compounds and pharmaceutical compositions thereof for treating subjects with amyotrophic lateral sclerosis (ALS) and other neurodegenerative diseases. The invention also provides methods of preparing the provided compounds.Type: ApplicationFiled: December 11, 2013Publication date: January 15, 2015Inventors: Richard B. Silverman, Yinan Zhang
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Publication number: 20150005283Abstract: The present invention provides compounds, compositions and methods for the treatment of hepatitis C virus (HCV) infection. Also disclosed are pharmaceutical compositions containing such compounds and methods for using these compounds in the treatment of HCV infection.Type: ApplicationFiled: February 21, 2013Publication date: January 1, 2015Applicant: Hoffmann-La Roche Inc.Inventors: Adrian Wai-Hing Cheung, Ryan Craig Schoenfeld, Weiya Yun, Shu-Hai Zhao
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Publication number: 20140378493Abstract: Compounds having the structure of Formula I, including pharmaceutically acceptable salts of the compounds, are CETP inhibitors and are useful for raising HDL-cholesterol, reducing LDL-cholesterol, and for treating or preventing atherosclerosis.Type: ApplicationFiled: September 8, 2014Publication date: December 25, 2014Inventors: Pengcheng Patrick Shao, Wanying Sun, Revathi Reddy Katipally, Petr Vachal, Feng Ye, Jian Liu, Deyou Sha
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Publication number: 20140378421Abstract: The present invention relates to novel compounds having ?2 adrenergic agonist and M3 muscarinic antagonist dual activity, to pharmaceutical compositions containing them, to the process for their preparation and to their use in respiratory therapies.Type: ApplicationFiled: November 9, 2012Publication date: December 25, 2014Inventors: Jose Aiguade Bosch, Silvia Gual Roig, Maria Prat Quinones, Carlos Puig Duran
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Publication number: 20140371278Abstract: Disclosed are compound of formula (I) and pharmaceutically accepted salts and prodrugs thereof, wherein each of R1, R2, R3, R4, R5, R6, X1 and X2 is as defined in the description. These compounds are protein kinases inhibitors, especially the inhibitors of Mek, which are useful in the treatment of cancers and inflammation of mammals. Disclosed are the treatment methods of cancers and inflammation of mammals as well as pharmaceutical compositions comprising the compounds described herein. The preparation of benzoheterocyclic compounds are disclosed. Disclosed are the preparation of potential drug candidates, such as benzooxazol, benzothiazol, benzothiadiazol and the like.Type: ApplicationFiled: January 16, 2013Publication date: December 18, 2014Applicant: TIANJIN BINJIANG PHARMA, INC.Inventors: Hongqi Tian, Conghui Ji, Chunlei Liu, Li Kong, Ying Cheng, Gongchao Huang
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Patent number: 8912186Abstract: The invention provides specific small molecule compounds that allosterically regulate the activity or modulate protein-protein interactions of AGC protein kinases and the Aurora family of protein kinases, methods for their production, pharmaceutical compositions comprising same, and their use for preparing medicaments for the treatment and prevention of diseases related to abnormal activities of AGC protein kinases or of protein kinases of the Aurora family.Type: GrantFiled: October 16, 2009Date of Patent: December 16, 2014Assignee: Universitaet des SaarlandesInventors: Matthias Engel, Wolfgang Fröhner, Adriane Stroba, Ricardo M. Biondi