Nitrogen, Other Than As Nitro Or Nitroso, Attached Directly To The Six Membered Hetero Ring By Nonionic Bonding Patents (Class 546/159)
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Patent number: 8993767Abstract: The present invention relates to multiphoton activable organic compounds responding to the following formula (I). The present invention also relates to a method of synthesizing the compounds of the invention, to an aqueous solution comprising at least one compound of the invention, and to their specific uses. The present invention also concerns a method of liberating organic ligands, said method involving the step of irradiating a compound according to the invention.Type: GrantFiled: January 12, 2011Date of Patent: March 31, 2015Assignee: Centre National de la Recherche ScientifiqueInventors: Peter Dalko, Morgane Petit, David Ogden, Francine Acher
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Patent number: 8987456Abstract: The invention provides certain 3-pyridyl carboxamide-containing compounds of the Formula (I) (I) or pharmaceutically acceptable salts thereof, wherein A and B are as defined herein. The invention also provides pharmaceutical compositions comprising such compounds, and methods of using the compounds for treating diseases or conditions mediated by Spleen Tyrosine Kinase (Syk) kinase.Type: GrantFiled: October 1, 2012Date of Patent: March 24, 2015Assignee: Merck Sharp & Dohme Corp.Inventors: Michael D. Altman, Kaleen Konrad Childers, Anthony Donofrio, John Michael Ellis, Sandra Lee Knowles, Alan B. Northrup
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Patent number: 8987250Abstract: Compounds disclosed herein including compounds of formula I?: and salts thereof are provided. Pharmaceutical compositions comprising compounds disclosed herein, processes for preparing compounds disclosed herein, intermediates useful for preparing compounds disclosed herein and therapeutic methods for treating an HIV infection using compounds disclosed herein are also provided.Type: GrantFiled: April 19, 2013Date of Patent: March 24, 2015Assignee: Gilead Sciences, Inc.Inventors: Kerim Babaoglu, Gediminas Brizgys, Jake Cha, Xiaowu Chen, Hongyan Guo, Randall L. Halcomb, Xiaochun Han, Richard Huang, Hongtao Liu, Ryan McFadden, Michael L. Mitchell, Yingmei Qi, Paul A. Roethle, Lianhong Xu, Hong Yang
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Publication number: 20150073017Abstract: Compounds are provided that act as potent antagonists of the CCR(9) receptor. Animal testing demonstrates that these compounds are useful for treating inflammation, a hallmark disease for CCR(9). The compounds are generally aryl sulfonamide derivatives and are useful in pharmaceutical compositions, methods for the treatment of CCR(9)-mediated diseases, and as controls in assays for the identification of CCR(9) antagonists.Type: ApplicationFiled: November 14, 2014Publication date: March 12, 2015Inventors: Xi CHEN, Junfa FAN, Pingchen FAN, Antoni KRASINSKI, Lianfa LI, Rebecca M. LUI, Jeffrey P. McMAHON, Jay P. POWERS, Yibin ZENG, Penglie ZHANG
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Patent number: 8975278Abstract: The present invention describes a method for the treatment of a neurological condition in a subject which comprises administering to a subject in need thereof a therapeutically effect amount of a compound of the formula or pharmaceutically acceptable salts, hydrates, or solvates thereof.Type: GrantFiled: September 19, 2007Date of Patent: March 10, 2015Assignee: Prana Biotechnology LimitedInventors: Kevin Jeffrey Barnham, Elisabeth Colette Louise Gautier, Gaik Beng Kok, Guy Krippner
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Patent number: 8975408Abstract: Methods for producing moxifloxacin hydrochloride compounds having very low levels of impurities are provided. Compounds produced using such methods and pharmaceutical compositions including such compounds are also provided.Type: GrantFiled: January 20, 2014Date of Patent: March 10, 2015Assignee: F.I.S.—Fabbrica Italiana Sintetici S.p.A.Inventors: Gianni Gottardo, Pierluigi Padovan, Sergio Osti
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Patent number: 8969381Abstract: The disclosure relates to chemokine CXCR4 receptor modulators and uses related thereto. In certain embodiments, the disclosure relates to pharmaceutical compositions comprising compounds disclosed herein or pharmaceutically acceptable salts or prodrugs thereof. In certain embodiments, the compositions disclosed herein are used for managing CXCR4 related conditions, typically prevention or treatment of viral infections such as HIV or for managing cancer.Type: GrantFiled: December 2, 2011Date of Patent: March 3, 2015Assignee: Emory UniversityInventors: Lawrence J. Wilson, John Wiseman, Dennis C. Liotta, Michael G. Natchus
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Patent number: 8969577Abstract: The present invention relates to curable compositions comprising a thermolatent amidine base and an organic material which is polymerizable or crosslinkable with a basic or nucleophilic catalyst. In particular, the invention relates to curable coating compositions, especially powder coating compositions, and curable adhesive compositions, as well as to the use a thermolatent amidine base as a curing catalyst for thermally induced base-catalyzed polymerization or crosslinking reactions.Type: GrantFiled: November 18, 2009Date of Patent: March 3, 2015Assignee: BASF SEInventors: Peter Nesvadba, Lucienne Bugnon Folger, Ralf Knischka
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Publication number: 20150057288Abstract: A pest control method for honeybee parasitic pests has been found, which is highly safe to honeybees and demonstrates excellent pest control effects against honeybee parasitic pests by using a honeybee parasitic pest control agent containing at least one of a compound represented by Formula (I) and acid addition salts thereof.Type: ApplicationFiled: November 10, 2014Publication date: February 26, 2015Applicant: MEIJI SEIKA PHARMA CO., LTD.Inventors: Ryo HORIKOSHI, Masaaki MITOMI
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Patent number: 8957091Abstract: The present invention relates to the use of quinolinone derivatives of general formula (I), ligands of the Smo receptor or of related receptors which target a binding site of the receptor which is different from the known ligand binding sites, as research tools for identifying modulators of the Smo receptor or of related receptors, characterizing the Hedgehog signalling pathway and diagnosis; the invention also relates to kits containing said derivatives of general formula (I).Type: GrantFiled: November 15, 2011Date of Patent: February 17, 2015Assignee: Centre National de la Recherche ScientifiqueInventors: Martial Ruat, Helene Faure, Tatiana Gorojankina
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Publication number: 20150041773Abstract: An anthracene-based compound is represented by Formula 1 as below: wherein Ar, R1 to R3, R11 to R13, L1, L2, a1 to a3, b1, b2, n1, n2, m1, m2, o1 and o2 are as defined in the specification. An organic light-emitting device includes the anthracene-based compound.Type: ApplicationFiled: May 21, 2014Publication date: February 12, 2015Applicant: SAMSUNG DISPLAY CO., LTD.Inventors: Jun-Ha PARK, Seok-Hwan HWANG, Young-Kook KIM, Hye-Jin JUNG, Eun-Young LEE, Jong-Woo KIM, Jin-O LIM, Sang-Hyun HAN, Kwang-Hyun KIM, Eun-Jae JEONG, Soo-Yon KIM
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Publication number: 20150038531Abstract: An aminopyridine derivative of Formula 1 and a method of preventing or treating cancer using the same. Formula 1: In Formula 1: X1 and X2 are each independently selected from the group consisting of carbon and nitrogen; R1 to R5 are each independently selected from the group consisting of a hydrogen, a straight, a branched, or cyclo alkyl of C1-C4, a halogen, and a hydroxyl; and R6 is a hydrogen or an alkyl of C1-C6.Type: ApplicationFiled: October 20, 2014Publication date: February 5, 2015Inventors: Sunghoon Kim, Hee Sook Lee, Young Sun Oh, Dae Gyu Kim
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Publication number: 20150038714Abstract: The present invention relates to novel and concise process for the construction of chiral 3-substituted tetrahyroquinoline derivatives based on proline catalyzed asymmetric ?-functionalization of aldehyde, followed by in situ reductive cyclization of nitro group under catalytic hydrogenation condition with high optical purities. Further the invention relates to conversion of derived chiral 3-substituted tetrahydroquinoline derivatives into therapeutic agents namely (?)-sumanirole (96% ee) and 1-[(S)-3-(di-methylamino)-3,4-dihydro-6,7-dimethoxy-quinolin-1(2H)-yl]propanone[(S)-903] (92% ee).Type: ApplicationFiled: March 19, 2013Publication date: February 5, 2015Applicant: Council of Scientific & Industrial ResearchInventors: Varun Rawat, Senthil Kumar Boopathi, Arumugam Sudalai
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Publication number: 20150011551Abstract: Described herein are compounds that modulate the activity of TNAP. In some embodiments, the compounds described herein inhibit TNAP. In certain embodiments, the compounds described herein are useful in the treatment of conditions associated with hyper-mineralization.Type: ApplicationFiled: February 21, 2013Publication date: January 8, 2015Applicant: Sanford- Burnham Medical Reseach InstituteInventors: Anthony B. Pinkerton, Russell Dahl, Nicholas D.P. Cosford, Jose Luis Millan
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Patent number: 8927577Abstract: The present invention provides a compound of Formula I or a pharmaceutically acceptable salt thereof, wherein R1, R2, R3, A1, A2, A3, B1, B2, B3 and B4 are as defined herein. The compounds of Formula I have been found to act as glucagon antagonists or inverse agonists. Consequently, the compounds of Formula I and the pharmaceutical compositions thereof are useful for the treatment of diseases, disorders, or conditions mediated by glucagon.Type: GrantFiled: July 12, 2012Date of Patent: January 6, 2015Assignee: Pfizer Inc.Inventors: Mary Didiuk, Kevin J. Filipski, Angel Guzman-Perez, Esther C. Lee, Jeffrey A. Pfefferkorn, Benjamin Stevens, Meihua Tu
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Publication number: 20140371461Abstract: The present invention provides a process for effectively producing an N-(hetero)arylazole with high yield, which is useful as a medical or agrochemical product, an organic photoconductor material, an organic electroluminescent element material, or the like. The present invention relates to a process for producing an N-(hetero)arylazole, which includes reacting a (hetero)aryl (pseudo)halide with an NH-azole in the presence of: a catalyst including a palladium compound and a coordination compound; and a basic magnesium compound.Type: ApplicationFiled: August 31, 2012Publication date: December 18, 2014Applicant: TAKASAGO INTERNATIONAL CORPORATIONInventors: Yuji Nakayama, Tohru Kobayashi
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Publication number: 20140336178Abstract: The present invention is based, in part, on assays we conducted that revealed compounds that may be used to treat or prevent diseases characterized by an abnormal or undesirable association of one protein with another.Type: ApplicationFiled: April 29, 2014Publication date: November 13, 2014Applicants: The General Hospital Corporation, Massachusetts Institute of TechnologyInventors: Aleksey G. Kazantsev, Anne B. Young, David E. Housman, Steven M. Hersch
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Publication number: 20140329856Abstract: The instant application discloses methods of treating, reducing, or preventing pain in a mammal, which may include administering a compound capable of modulating a transient receptor potential channel. In one aspect, the TRP channel may be TRPC4. Types of pain contemplated by the present disclosure include acute, chronic, neuropathic, and nociceptive pain.Type: ApplicationFiled: June 13, 2014Publication date: November 6, 2014Inventors: Eric M. Ostertag, John Stuart Crawford
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Patent number: 8871937Abstract: The invention relates to compounds of the general formula (I) and their pharmaceutically acceptable salts (in which formula R1 represents a hydrogen atom, lower alkyl group, lower alkenyl group, lower cycloalkyl group, aryl group, aralkyl group or heterocyclic group, wherein, the above groups are optionally substituted in ortho, meta and/or para position with 1, 2, 3 or 4 electron withdrawing groups or electron donating groups; R2 represents a hydrogen atom, lower alkyl group, aryl group, aralkyl group or heterocyclic group wherein the above groups are optionally substituted with one or more halogen atoms; R3 represents a lower alkyl group, aryl group, aralkyl group or heterocyclic group wherein the above groups are optionally substituted in ortho, meta or para position with 1, 2, 3 or 4 electron withdrawing groups or electron donating groups; R4 represents a hydrogen atom, lower alkyl group or any acidic functional group; n is 1 or 2).Type: GrantFiled: May 6, 2011Date of Patent: October 28, 2014Assignees: “AVIDIN” Kutato, Fejleszto es Kereskedelmi Korlatolt Felelossegu Tarsasag, UBICHEM Kutato Korlatolt Felelossegu TarsasagInventors: Laszlo Puskas, Csaba Szabo, Ivan Kanizsai, Mario Gyuris, Ramona Madacsi, Bela Ozsvari, Liliana Feher, Gabor Tamas
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Patent number: 8871938Abstract: The present invention relates to the field of synthesizing anti-infective compounds. More particularly, the invention relates to synthesizing a family of quinolone compounds useful as anti-infective agents. The invention includes a process for preparing a quinolone compound wherein less than about 0.40% of dimeric impurity of the quinolone is produced.Type: GrantFiled: July 9, 2013Date of Patent: October 28, 2014Assignee: Melinta Therapeutics, Inc.Inventors: Roger Hanselmann, Maxwell M. Reeve, Graham Johnson
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Patent number: 8865903Abstract: A continuous process for the alkylation of tertiary amines and, in particular, to a continuous process for the quaternization of cyclic tertiary amines useful for the preparation of cyclic quaternary ammonium salts with high purity is described.Type: GrantFiled: November 21, 2012Date of Patent: October 21, 2014Assignee: Cerbios-Pharma SAInventors: Andrea Mereu, Moreno Morosoli, Mauro Perseghini, Alessandro Spreafico
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Patent number: 8865738Abstract: The invention relates to compounds of the general formula (I) where: R2 is a hydrogen or fluorine atom or a hydroxyl, cyano, trifluoromethyl, C1-6-alkyl, C1-6-alkoxy, or NR8R9 group; m and p have a value of 1; n and o have the same value which is 0 or 1; A is a covalent bond or a C1-8-alkylene group; R1 is an optionally substituted aryl or heteroaryl group; R3 is a hydrogen or fluorine atom or a C1-6-alkyl group or a trifluoromethyl group; R4 is an optionally substituted 5-membered heterocyclic compound; wherein the compounds can be in the state of a base or an acid addition salt. The present invention can be used in therapeutics.Type: GrantFiled: May 11, 2010Date of Patent: October 21, 2014Assignee: SanofiInventors: Ahmed Abouabdellah, Aude Fayol, Alistair Lochead, Mourad Saady, Julien Vache, Philippe Yaiche
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Publication number: 20140296519Abstract: A 4-aminocarbazole compound represented by formula (1): wherein Ar1-Ar4 represent substituted or unsubstituted aryl, thienyl, pyridyl, benzothienyl, dibenzothienyl, dibenzofuranyl, 4-carbazolyl, dibenzothienylphenyl, dibenzofuranylphenyl or 9-carbazolylphenyl group; R1-R7 represent substituted or unsubstituted aryl, heteroaryl or heteroarylphenyl group, or alkyl, alkoxy, cyano group, or hydrogen or halogen atom; n is integer of 0-2; and X represents substituted or unsubstituted (n+1)-valent aromatic hydrocarbon, heteroaromatic or heteroarylphenyl group. The 4-aminocarbazole compound provides an organic EL device exhibiting enhanced emitting efficiency and durability.Type: ApplicationFiled: October 25, 2012Publication date: October 2, 2014Applicant: TOSOH CORPORATIONInventors: Naoki Matsumoto, Takanori Miyazaki
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Patent number: 8846928Abstract: The present invention is directed to compounds of formula I and pharmaceutically acceptable salts, esters, and prodrugs thereof which are inhibitors of Syk kinase. The present invention is also directed to intermediates used in making such compounds, the preparation of such a compound, pharmaceutical compositions containing such a compound, methods of inhibition Syk kinase activity, methods of inhibition the platelet aggregation, and methods to prevent or treat a number of conditions mediated at least in part by Syk kinase activity, such as Non Hodgkin's Lymphoma.Type: GrantFiled: November 1, 2011Date of Patent: September 30, 2014Assignee: Portola Pharmaceuticals, Inc.Inventors: Zhaozhong J. Jia, Yonghong Song, Qing Xu, Brian Kane, Shawn M. Bauer, Anjali Pandey
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Patent number: 8835458Abstract: Provided is a pharmaceutical composition comprising, as an active ingredient, a quinoline or quinazoline derivative of formula (I), a pharmaceutically acceptable salt, an isomer, a hydrate, and a solvate thereof, which is effective in the prevention and treatment of a cancer, inflammation, autoimmune diseases or neurodegenerative disorders which are induced by the overexpression of inhibitor of apoptosis proteins (IAPs).Type: GrantFiled: August 31, 2011Date of Patent: September 16, 2014Assignee: Hanmi Science Co., LtdInventors: In Hwan Bae, Eun Young Byun, Hae Kyoung Ju, Ji Young Song, Seung Hyun Jung, Seung Ah Jun, Ho Seok Kim, Young Hee Jung, Mi Yon Shim, Young Gil Ahn, Maeng Sup Kim
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Publication number: 20140256724Abstract: The present application relates to cycloalkylpyridin-2-amines derivates of formula (1) or stereoisomers thereof or pharmaceutically acceptable salts thereof. The present application also relates to the process for the preparation of compounds of formula (I). The present application further describes the compounds of formula (1) as cholesteryl ester-transfer protein (CETP) inhibitors. The present application further relates to pharmaceutical compositions comprising compounds of formula (1) or stereoisomers thereof or pharmaceutically acceptable salts thereof.Type: ApplicationFiled: August 17, 2012Publication date: September 11, 2014Applicant: DR. REDDY'S LABORATORIES LTD.Inventors: Anima Boruah, Shanavas Alikunju
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Patent number: 8829196Abstract: The present invention relates to compositions and methods that modulate at least one TRP family member. Specifically, the present invention relates to novel TRPA1 antagonists and their use in the treatment of pain such as chronic inflammatory and neuropathic pain. Compounds that can modulate one or more TRPA1 functions are useful in many aspects including, but not limited to, maintaining calcium homeostasis; maintaining sodium homeostasis; modulating intracellular calcium levels; modulating membrane polarization (membrane potential); modulating cation levels; and/or treating or preventing diseases, disorders, or conditions associated with calcium homeostasis, sodium homeostasis, calcium or sodium dyshomeostasis, or membrane polarization/hyperpolarization (including hypo and hyperexcitability), and/or treating or preventing diseases, disorders, or conditions associated with regulation or misregulation of TRPA1 expression or function.Type: GrantFiled: September 28, 2010Date of Patent: September 9, 2014Assignee: Merck Sharp & Dohme Corp.Inventors: Mark T. Bilodeau, Melissa Egbertson, Ahren Green, John C. Hartnett, Yiwei Li
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Publication number: 20140243286Abstract: Described herein are monomers capable of forming a biologically useful multimer when in contact with one, two, three or more other monomers in an aqueous media. In one aspect, such monomers may be capable of binding to another monomer in an aqueous media (e.g. in vivo) to form a multimer (e.g. a dimer). Contemplated monomers may include a ligand moiety, a linker element, and a connector element that joins the ligand moiety and the linker element. In an aqueous media, such contemplated monomers may join together via each linker element and may thus be capable of modulating one or more biomolecules substantially simultaneously, e.g., modulate two or more binding domains on a protein or on different proteins.Type: ApplicationFiled: February 28, 2014Publication date: August 28, 2014Applicant: Coferon, Inc.Inventors: Lee Daniel Arnold, Kenneth W. Foreman, Douglas S. Werner
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Publication number: 20140243321Abstract: Described herein are monomers capable of forming a biologically useful multimer when in contact with one, two, three or more other monomers in an aqueous media. In one aspect, such monomers may be capable of binding to another monomer in an aqueous media (e.g. in vivo) to form a multimer, (e.g. a dimer). Contemplated monomers may include a ligand moiety, a linker element, and a connector element that joins the ligand moiety and the linker element. In an aqueous media, such contemplated monomers may join together via each linker element and may thus be capable of modulating one or more biomolecules substantially simultaneously, e.g., modulate two or more binding domains on a protein or on different proteins.Type: ApplicationFiled: February 28, 2014Publication date: August 28, 2014Applicant: Coferon, Inc.Inventors: Lee Daniel Arnold, Kenneth W. Foreman, Douglas S. Werner
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Patent number: 8815956Abstract: The present invention includes compounds having structural formula (I), or salts or solvates thereof. These compounds are useful as sweet flavor modifiers. The present invention also includes compositions comprising the present compounds and methods of enhancing the sweet taste of compositions.Type: GrantFiled: August 10, 2012Date of Patent: August 26, 2014Assignee: Senomyx, Inc.Inventors: Catherine Tachdjian, Xiao-Qing Tang, Donald S. Karanewsky, Guy Servant, Xiaodong Li, Feng Zhang, Qing Chen, Hong Zhang, Timothy James Davis, Vincent Darmohusodo, Melissa Sue Wong, Victor Selchau
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Publication number: 20140235548Abstract: Compounds, pharmaceutical compositions, and methods of using such compounds to treat or prevent diseases or disorders associated with or mediated by JAMM proteins are disclosed. The compounds and compositions inhibit the enzymatic activity of a JAMM domain, including the JAMM domain of the CSN5 subunit of the COP9-signalsome (CSN), the JAMM domain of the Rpn11/Poh1/Psmd14 subunit of the 26S proteasome, the JAMM domain of AMSH, the JAMM domain of AMSH-LP, the JAMM domain of BRCC36, among other JAMM domains.Type: ApplicationFiled: May 10, 2012Publication date: August 21, 2014Applicant: Cleave Biosciences, Inc.Inventors: Han-Jie Zhou, Francesco Parlati, Matthieu Roufflet, Ethan D. Emberley, Raymond J. Deshaies, Seth Cohen
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Patent number: 8802700Abstract: The present invention relates to modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator, compositions thereof, and methods therewith. The present invention also relates to methods of treating ABC transporter mediated diseases using such modulators.Type: GrantFiled: June 8, 2012Date of Patent: August 12, 2014Assignee: Vertex Pharmaceuticals IncorporatedInventors: Urvi Sheth, Lev T. D. Fanning, Mehdi Numa, Hayley Binch, Dennis James Hurley, Jinglan Zhou, Sara S. Hadida Ruah, Anna R. Hazlewood, Alina Silina, Rajendran Vairagoundar, Fredrick F. Van Goor, Peter Diederik Jan Grootenhuis, Martyn C. Botfield
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Patent number: 8802697Abstract: Described herein are inhibitors of FGFR, pharmaceutical compositions including such compounds, and methods of using such compounds and compositions to inhibit the activity of tyrosine kinases.Type: GrantFiled: July 11, 2013Date of Patent: August 12, 2014Assignee: Blueprint Medicines CorporationInventors: Neil Bifulco, Jr., Natasja Brooijmans, Brian L. Hodous, Joseph L. Kim, Chandrasekhar V. Miduturu
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Publication number: 20140219989Abstract: The present invention provides a compound of Formula (I) as described herein, or a pharmaceutically acceptable salt thereof. The present invention also provides pharmaceutical compositions comprising one or more said compounds, and methods for using said compounds for treating or preventing a thromboses, embolisms, hypercoagulability or fibrotic changes.Type: ApplicationFiled: July 3, 2012Publication date: August 7, 2014Inventors: Craig Boyle, William Greenlee, Samuel Chackalamannil, Claire Lankin
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Publication number: 20140221371Abstract: The invention relates to compounds of general formula (I), corresponding enantiomeric, diastereomeric and/or tautomeric forms thereof as well as pharmaceutically acceptable salts thereof and the prodrugs of said compounds. The invention also relates to the use of said compounds as binding partners for 5-HT5 receptors for treating diseases that are modulated by a 5-HT5 receptor activity, in particular, for treating neurodegenerative and neuropsychiatric disorders as well as signs, symptoms and dysfunctions.Type: ApplicationFiled: December 23, 2013Publication date: August 7, 2014Inventors: Wilhelm Amberg, Astrid Netz, Andreas Kling, Michael Ochse, Udo Lange, Charles W. Hutchins, Franciso Javier Garcia-Ladona, Wolfgang Wernet
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Patent number: 8791275Abstract: Psoralen compounds of Formula (I): wherein (N+ Aryl) is a member selected from the group consisting of nitrogen containing aromatic heterocycles of formulae (i)-(iii): wherein Z is a group of formula: wherein R is C1-C30 hydrocarbyl, which may be linear, branched or cyclic and contains from 1 to 15 carbon-carbon double bonds, which may be conjugated or unconjugated with one another or may include an aryl ring, and may contain one or more substituents; R1 is hydrogen, aryl, heteroaryl, alkyl, cycloalkyl, heterocyclyl, alkenyl, alkynyl, alkene-aryl, alkene-heteroaryl, alkene-heterocyclyl, alkene-cycloalkyl, fused cycloalkylaryl, fused cycloalkylheteroaryl, fused heterocyclylaryl, fused heterocyclyheteroaryl, alkylene-fused cycloalkylaryl, alkylene-fused cycloalkylheteroaryl, alkylene-fused heterocyclylaryl, alkylene-fused heterocyclyheteroaryl; n is an integer from 1 to 8 and X is a pharmaceutically acceptable counter ion; and their use in methods for the treatment of a cell proliferatType: GrantFiled: January 11, 2013Date of Patent: July 29, 2014Assignees: Duke University, Immunolight, LLCInventors: Eric Toone, David Gooden, Tuan Vo-Dinh, Frederic A. Bourke, Jr.
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Patent number: 8785640Abstract: The present invention relates to modulators of cystic fibrosis transmembrane conductance regulator (“CFTR”), compositions thereof, and methods therewith. The present invention also relates to methods of treating diseases using modulators of CFTR.Type: GrantFiled: July 17, 2013Date of Patent: July 22, 2014Assignee: Vertex Pharmaceuticals IncorporatedInventors: Hayley Binch, Lev T. D. Fanning, Dennis Hurley, Urvi Sheth, Alina Silina, Xiaoqing Yang, Martyn Botfield, Peter D. J. Grootenhuis, Fredrick Van Goor, Mehdi Michel Djamel Numa
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Publication number: 20140200216Abstract: The present disclosure describes bicyclic aromatic carboxamide derivatives, as well as their compositions and methods of use. The compounds inhibit the activity of the Pim kinases, and are useful in the treatment of diseases related to the activity of Pim kinases including, e.g., cancer and other diseases.Type: ApplicationFiled: January 14, 2014Publication date: July 17, 2014Applicant: INCYTE CORPORATIONInventors: Yun-Long Li, David M. Burns, Hao Feng, Chu-Biao Xue, Anlai Wang, Jun Pan
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Patent number: 8779146Abstract: The invention relates to improvements of the physiochemical and/or the pharmaceutical properties of cilostazol. Disclosed herein are several new compositions and cocrystals of cilostazol, including: a 1:1 cilostazol gentisic acid cocrystal, a 1:1:1 cilostazol gentisic acid H2O cocrystal, a 1:1 cilostazol 4-hydroxybenzoic acid cocrystal, and a 1:1 cilostazol 2,4-dihydroxybenzoic acid cocrystal. The therapeutic methods and uses of these cilostazol cocrystals are described as well as therapeutic compositions containing them.Type: GrantFiled: April 28, 2011Date of Patent: July 15, 2014Assignee: Nuformix LimitedInventors: Alan Chorlton, Christopher Frampton, Daniel Gooding, Joanne Holland
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Patent number: 8772200Abstract: Provided is an agricultural fungicide that contains at least one selected from the group consisting of a novel nitrogen-containing heterocyclic compound represented by Formula (I), a salt thereof, or an N-oxide compound thereof. In Formula (I), R represents a group represented by CR1R2R3 or a cyano group. R1 to R3 each independently represents a hydrogen atom, an unsubstituted or substituted C1-8 alkyl group, an unsubstituted or substituted hydroxyl group, or the like. R4 or R5 represents a halogeno group or the like. Y or Z represents a carbon atom or the like, and A or D represents a benzene ring or the like. X represents an oxygen atom or a nitrogen atom or the like.Type: GrantFiled: December 28, 2010Date of Patent: July 8, 2014Assignee: Nippon Soda Co., Ltd.Inventors: Kotaro Shibayama, Jun Inagaki, Yuto Saiki, Akira Mitani, Raito Kuwahara, Motoaki Sato, Satoshi Nishimura, Mami Kuboki
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Patent number: 8754224Abstract: The present invention relates to solid state forms of N-[2,4-bis(1,1-dimethylethyl)-5-hydroxyphenyl]-1,4-dihydro-4-oxoquinoline-3-carboxamide (Compound 1), pharmaceutical compositions thereof and methods therewith.Type: GrantFiled: March 5, 2013Date of Patent: June 17, 2014Assignee: Vertex Pharmaceuticals IncorporatedInventors: Patricia Hurter, William Rowe, Christopher R. Young, Adriana Costache, Patrick R. Connelly, Mariusz Krawlec, Yuchuan Gong, Yushi Feng, Martin Trudeau
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Publication number: 20140162980Abstract: The present invention provides compounds of formula (I) wherein G1, G2, G3, G4, G5, G6, Y1, Y2, Y3, Y4, Y5 and Y6 and p and q are as defined in the claims. The invention further relates to compositions which comprise these compounds and to their use in agriculture or horticulture for controlling or preventing infestation of plants by phytopathogenic microorganisms, preferably fungi.Type: ApplicationFiled: July 28, 2011Publication date: June 12, 2014Applicant: SYNGENTA CROP PROTECTION LLCInventors: Daniel Stierli, Kurt Nebel, Werner Zambach, Andrea Bortolato
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Patent number: 8748458Abstract: Compounds of the invention are of the formula (I); wherein: is a double bond and X is C; or is a single bond and X is N, CH or CQR1; and wherein: n is 1 to 10; R is H or QR1; each R? is independently selected from H and QR1; each Q is independently selected from a bond, CO, NH, S, SO, SO2 or O; each R1 is independently selected from C1-C10 alkyl, C2-C10 alkenyl, C2-C10 alkynyl, substituted or unsubstituted aryl or heteroaryl, acyl, C1-C10 cycloalkyl, halogen, C1-C10 alkylaryl or C1-C10 heterocycloalkyl; L is a nitrogen-containing heteroaryl; and W is a zinc-chelating residue; or a pharmaceutically acceptable salt thereof. The compounds are useful in therapy.Type: GrantFiled: January 26, 2010Date of Patent: June 10, 2014Assignee: Karus Therapeutics LimitedInventors: Stephen Joseph Shuttleworth, Cyrille Davy Tomassi
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Publication number: 20140151548Abstract: Provided is a matrix for MALDI mass spectrometry that has a high ability of ionizing low-molecular-weight compounds, and makes it possible to make measurement in a negative ion mode. The matrix is a matrix for mass spectrometry that contains one or more compounds selected from the group consisting of compounds each represented by the following general formula (I), (II) or (III), and their salts thereof.Type: ApplicationFiled: July 5, 2012Publication date: June 5, 2014Inventors: Mitsuru Shindo, Hiroyuki Wariishi, Daisuke Miura, Yoshinori Fujimura
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Publication number: 20140128481Abstract: The present invention includes compounds having structural formula (I), or pharmaceutically acceptable salts, solvate, and/or ester thereof. These compounds are useful as sweet flavor modifiers. The present invention also includes compositions comprising the present compounds and methods of enhancing the sweet taste of ingestible compositions. Furthermore, the present invention provides methods for preparing the compounds.Type: ApplicationFiled: October 23, 2013Publication date: May 8, 2014Applicant: SENOMYX, INC.Inventors: Catherine TACHDJIAN, Xiao Qing TANG, Donald S. KARANEWSKY, Guy SERVANT, Xiaodong LI, Feng ZHANG, Qing CHEN, Hong ZHANG, Timothy DAVIS, Vincent DARMOHUSODO, Melissa WONG, Victor Selchau
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Patent number: 8716285Abstract: The present invention provides a compound of formula (I) or a pharmaceutically acceptable salt, ester or stereoisomer thereof, wherein R1 to R3 and X have the significances given herein. The present invention is also directed to processes for making said compounds and uses of said compounds, in particular their use as medicaments, more particularly their use as medicaments in the treatment of cancer.Type: GrantFiled: September 7, 2011Date of Patent: May 6, 2014Assignee: Hoffmann-La Roche Inc.Inventors: Lei Guo, Guozhi Tang, Zhanguo Wang, Jason Christopher Wong, Weixing Zhang
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Patent number: 8716307Abstract: The present invention is directed to methods of using a sirolimus drug and chloroquine or a quinoline derivative in combination. Methods of use are also described.Type: GrantFiled: May 4, 2010Date of Patent: May 6, 2014Assignee: The Trustees Of The University of PennsylvaniaInventors: Ravi Kumar Amaravadi, Craig B. Thompson
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Patent number: 8716310Abstract: Provided are compounds that are inhibitors of both rho kinase and of a monoamine transporter (MAT) act to improve the disease state or condition. Further provided are compositions comprising the compounds. Further provided are methods for treating diseases or conditions, the methods comprising administering compounds according to the invention. One such disease may be glaucoma for which, among other beneficial effects, a marked reduction in intraocular pressure (IOP) may be achieved.Type: GrantFiled: February 15, 2013Date of Patent: May 6, 2014Assignee: Aerie Pharmaceuticals, Inc.Inventors: Mitchell A. deLong, Jill Marie Sturdivant, Susan M. Royalty
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Patent number: 8710079Abstract: Quinoline compounds of formula (I): in which A, B, D, E, F, G, R1, R2, R3, X, Y, n, p, and q are defined herein. Also disclosed is a method for treating a viral infection with a compound of formula (I).Type: GrantFiled: April 21, 2011Date of Patent: April 29, 2014Assignee: National Health Research InstitutesInventors: Hsing-Pang Hsieh, Tsu-An Hsu, Jiann-Yih Yeh, Yu-Sheng Chao
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Patent number: RE45108Abstract: The present invention provides a quinolone compound that inhibits the chronic progression of Parkinson's disease or protects dopamine neurons from disease etiology, thereby suppressing the progression of neurological dysfunction, so as to prolong the period of time until L-dopa is administered while also improving neuronal function; the quinolone compound of the invention is represented by Formula (1): wherein: R1 represents hydrogen or the like; R2 represents hydrogen or the like; R3 represents substituted or unsubstituted phenyl or the like; R4 represents halogen or the like; R5 represents hydrogen or the like; R6 represents hydrogen or the like; and R7 represents hydrogen or the like.Type: GrantFiled: September 27, 2013Date of Patent: September 2, 2014Assignee: Otsuka Pharmaceutical Co., Ltd.Inventors: Kenji Otsubo, Takahito Yamauchi, Yuji Ochi