Nitrogen, Other Than As Nitro Or Nitroso, Attached Directly To The Six Membered Hetero Ring By Nonionic Bonding Patents (Class 514/313)
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Publication number: 20150004252Abstract: The invention relates to the use of choline kinase alpha as predictive marker for the determination of the response to a chemotherapeutic treatment in a subject suffering from cancer, particularly for predicting the clinical response of a subject suffering from non-small cell lung cancer to a platinum-based chemotherapeutic treatment. The invention relates to methods for designing a personalised therapy for subjects suffering from cancer, particularly from non-small cell lung cancer, based on the expression levels of choline kinase alpha as well as to methods for the treatment of non-small cell lung cancer using a platinum-based chemotherapeutic treatment based in a subject wherein the subject is selected based on the expression levels of choline kinase alpha.Type: ApplicationFiled: June 20, 2012Publication date: January 1, 2015Applicant: TRASLATIONAL CANCER DRUGS PHARMA, S.LInventor: Juan Carlos Lacal SanJuan
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Patent number: 8912218Abstract: The invention relates to the novel products of formula (I): in which: Ra represents H, Hal, aryl or heteroaryl, which is optionally substituted; Rb represents H, Rc, —COORc-CO—Rc or —CO—NRcRd; where Rc represents alkyl, cycloalkyl, heterocycloalkyl, aryl and heteroaryl, all optionally substituted; Rd represents H, alk or cycloalkyl; these products being in all the isomer forms and the salts, as medicaments, in particular as MET inhibitors.Type: GrantFiled: July 21, 2009Date of Patent: December 16, 2014Assignee: SanofiInventors: Ahmed Abouabdellah, Jochen Görlitzer, Peter Hamley, Antoine Ravet
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Patent number: 8912141Abstract: A combined therapy which utilizes hydroxychloroquine and GNS-227: for the treatment of an HCV-related disease, including HCV chronic infection, is disclosed. Further disclosed is pharmaceutical composition (e.g., as a unit dosage form) comprising hydroxychloroquine and GNS-227.Type: GrantFiled: June 21, 2012Date of Patent: December 16, 2014Assignee: Panmed Ltd.Inventor: Philippe Halfon
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Publication number: 20140364424Abstract: The present invention relates to novel hepcidin antagonists, pharmaceutical compositions comprising them and the use thereof as medicaments for the use in the treatment of iron metabolism disorders, such as, in particular, iron deficiency diseases and anemias, in particular anemias in connection with chronic inflammatory diseases.Type: ApplicationFiled: June 20, 2014Publication date: December 11, 2014Inventors: Wilm Buhr, Susanna Burckhardt, Franz Dürrenberger, Felix Funk, Peter O. Geisser, Vincent A. Corden, Stephen M. Courtney, Graham Dawson, Tara Davenport, Mark Slack, Mark P. Ridgill, Christopher J. Yarnold, Susan Boyce, Albertus A. Ellenbroek
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Publication number: 20140350048Abstract: Compounds, compositions and methods useful for treating infectious diseases are provided. In particular, 3-aryl quinoline compounds, their synthesis, pharmaceutical compositions thereof and methods of treating infectious diseases such as malaria, are disclosed.Type: ApplicationFiled: January 14, 2013Publication date: November 27, 2014Inventors: Michael K. Riscoe, Rolf W. Winter, Sovitj Pou, David J. Hinrichs, Jane Xu Kelly, Yuexin Li, Aaron Nilsen
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Publication number: 20140349937Abstract: Therapeutic methods for treating a subject with benign prostatic hypertrophy by inhibition of the activity of insulin-like growth factor-I (IGF-I) to reduce the amount of prostatic hyperplastic tissue in the subject are described herein.Type: ApplicationFiled: June 9, 2014Publication date: November 27, 2014Inventors: David L. Kleinberg, Sergio Vidal, Weifeng Ruan
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Publication number: 20140343015Abstract: A morphinan derivative represented by the following general formula (I) (in the formula, R1 represents hydrogen, C1-6 alkyl, cycloalkylalkyl (the cycloalkyl moiety has 3 to 6 carbon atoms, and the alkylene moiety has 1 to 5 carbon atoms), aralkyl (the aryl moiety has 6 to 10 carbon atoms, and the alkylene moiety has 1 to 5 carbon atoms) and the like, R2 represents hydrogen, C1-6 alkyl, C3-6 cycloalkyl, C6-10 aryl, aralkyl (the aryl moiety has 6 to 10 carbon atoms, and the alkylene moiety has 1 to 5 carbon atoms) and the like, R3, R4 and R5 represent hydrogen, hydroxy, carbamoyl, C1-6 alkoxy, C6-10 aryloxy and the like, R6a, R6b, R7, R8, R9, and R10 represent hydrogen and the like, X represents O or CH2, and Y represents C?O, SO2, an atomic bond and the like), or an acid addition salt thereof is used as an analgesic.Type: ApplicationFiled: September 7, 2012Publication date: November 20, 2014Applicants: NIPPON CHEMIPHAR CO., LTD., THE KITASATO INSTITUTEInventors: Hiroshi Nagase, Hideaki Fujii, Eriko Nakata, Yoshikazu Watanabe, Toshihiro Takahashi
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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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Publication number: 20140329852Abstract: The present invention relates to novel N-(imidazolidin-2-ylidene)quinoline derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals.Type: ApplicationFiled: July 15, 2014Publication date: November 6, 2014Inventors: Liming Wang, Mohammed I. Dibas, Michael E. Garst, KEN CHOW, Santosh C. Sinha
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Publication number: 20140322193Abstract: Unexpectedly, disorders of the cornea and conjunctiva are found to be caused or to be exacerbated, at least in part, by extracellular ATP and P2X7 receptor activation. Therapeutic compositions for topical administration to the eye for the treatment of disorders of the cornea and conjunctiva include an entity that inhibits P2X7 receptor function, reduces the effective concentration of extracellular ATP, or both.Type: ApplicationFiled: December 1, 2012Publication date: October 30, 2014Inventor: Michael Kaleko
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Patent number: 8871228Abstract: The present invention relates to an injectable composition for local administration for treating hemorrhoids, which contains hydroxychloroquine. Specifically, the composition contains a solution of hydroxychloroquine in physiological saline for injection, together with a local anesthetic and an antioxidant.Type: GrantFiled: June 18, 2010Date of Patent: October 28, 2014Inventor: Oh-Young Yeo
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Publication number: 20140315899Abstract: Disclosed are compounds, compositions and methods for treating various diseases, syndromes, conditions and disorders, including pain. Such compounds are represented by Formula I as follows: wherein A, B, G, Y, R1, R2, R3, and R4 are defined herein.Type: ApplicationFiled: July 2, 2014Publication date: October 23, 2014Inventors: Shawn T. Branum, Raymond W. Colburn, Scott L. Dax, Christopher M. Flores, Michele C. Jetter, Yi Liu, Donald Ludovici, Mark J. Macielag, Jay M. Matthews, James J. McNally, Laura M. Andraka, Ronald K. Russell, Ning Qin, Christopher Teleha, Kenneth M. Wells, Scott C. Youells, Mark A. Youngman
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Patent number: 8865709Abstract: Oxazole derivatives are described. The inventive compounds are useful as kinase inhibitors, and may be used in the treatment of cancer, such as prostate cancer, lung cancer, breast cancer, colon cancer, leukemia, CNS cancer, melanoma, ovarian cancer, and renal cancer.Type: GrantFiled: September 24, 2013Date of Patent: October 21, 2014Assignee: Neosome Life Sciences, LLCInventors: Laxman S. Desai, Srinivas Chittaboina
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Patent number: 8865739Abstract: The present invention relates to sodium channel inhibitors of Formula (I): in which R1, R2, R3, R4, R5, X, Y, and Z are as defined herein, and to their use in the treatment of various disease states, including cardiovascular diseases and diabetes. The invention also relates to methods for the preparation of the compounds, and to pharmaceutical compositions containing such compounds.Type: GrantFiled: December 10, 2013Date of Patent: October 21, 2014Assignee: Gilead Sciences, Inc.Inventors: Matthew Abelman, Robert H. Jiang, Jeff Zablocki
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Publication number: 20140309257Abstract: The invention provides methods of inhibiting the growth or metastasis of cancer in a mammal by inhibiting TopoIIa in the mammal. The invention also provides small molecule inhibitors of TopoIIa useful in the methods of the invention and pharmaceutical compositions containing the therapeutically effective compounds and methods of using the same.Type: ApplicationFiled: November 13, 2012Publication date: October 16, 2014Inventor: Daniel V. Labarbera
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Publication number: 20140303206Abstract: 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: ApplicationFiled: October 1, 2012Publication date: October 9, 2014Inventors: Michael D. Altman, Kaleen Konrad Childers, Anthony Donofrio, John Michael Ellis, Sandra Lee Knowles, Alan B. Northrup
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Publication number: 20140296215Abstract: The present disclosure provides pharmaceutical compositions, pharmaceutical preparations and methods for increasing activity of a mutant cystic fibrosis transmembrane conductance regulator protein (mutant-CFTR). The pharmaceutical compositions, pharmaceutical preparations and methods are useful for the study and treatment of disorders associated with mutant-CFTR, such as cystic fibrosis. The pharmaceutical compositions and pharmaceutical preparations may include one or more cyanoquinoline-containing compounds of the embodiments, or an analog or derivative thereof.Type: ApplicationFiled: May 25, 2012Publication date: October 2, 2014Applicant: The Regents of the University of CaliforniaInventors: Alan S. Verkman, Puay-Wah Phuan, Mark J. Kurth, John Knapp
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Publication number: 20140294767Abstract: A method of treating an Hepatitis C Virus infection in a patient, comprising providing a therapeutically effective amount, to a patient in need thereof, of a compound of Formula (I) or a pharmaceutically acceptable salt thereof, wherein: G1 is a group of the formula or where n is 0, 1, 2, 3, or 4 and Het is a 5- or 6-membered heteroaryl group containing 1 to 4 heteroatoms independently chosen from N, O, and S, which Het is optionally substituted.Type: ApplicationFiled: October 26, 2012Publication date: October 2, 2014Inventors: David Waugh, Christopher Self, Guangtao Zhang, Yves Pommier, Robert H. Shoemaker, Michael Currens, John Cardellina, Andrew Jobson, George Lountos, Dominic Scudiero
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Patent number: 8846675Abstract: Compounds and methods are provided for the treatment of, inter alia, Type II diabetes and other diseases associated with poor glycemic control.Type: GrantFiled: May 3, 2012Date of Patent: September 30, 2014Assignee: Cymabay Therapeutics, Inc.Inventors: Jingyuan Ma, Christopher J. Rabbat, Jiangao Song, Xin Chen, Imad Nashashibi, Zuchun Zhao, Aaron Novack, Dong Fang Shi, Peng Cheng, Yan Zhu, Alison Murphy
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Publication number: 20140288032Abstract: Agents that inhibit or prevent restenosis are identified by assaying test agents in a battery of assays to measure the effect of the test agent on cell proliferation, thrombosis, tissue modeling, and inflammation. Treatment for restenosis is provided using compositions of the invention.Type: ApplicationFiled: March 18, 2014Publication date: September 25, 2014Applicant: DiscoveRx CorporationInventors: Eric J. Kunkel, Evangelos Hytopoulos, Ivan Plavec
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Publication number: 20140288120Abstract: A compound having the following formula or a pharmaceutically acceptable salt thereof: where: R? is a hydrogen atom or a (C1-C4)alkyl group; n? is 1 or 2; n is 1, 2, or 3; R independently represents a hydrogen atom, a halogen atom, or a group selected from a (C1-C3)alkyl group, a —CN group, a hydroxyl group, a —NR1R2 group, a —COOR1 group, a (C1-C3)fluoroalkyl group, a —NO2 group, a (C1-C3)fluoroalkoxy, and a (C1-C4)alkoxy group; R? is a hydrogen atom, a halogen atom, or a group selected from a (C1-C3)alkyl group, a —COOR1 group, a —NO2 group, a —NR1R2 group, a (C1-C4)alkoxy group, and a CN group; R1 and R2 are a hydrogen atom or a (C1-C3)alkyl group; with the proviso that when R and R? are not simultaneously a hydrogen atom: when n is 1, R is not a methyl group in an ortho or para position with respect to N, when R? is a hydrogen atom, R is not a bromine atom or a chlorine atom, and when R is a hydrogen atom, R is not a methyl or ethyl group, a —COOH group, a —COOC2H5 group, or a bromine atom that isType: ApplicationFiled: April 18, 2014Publication date: September 25, 2014Applicants: SOCIETE SPLICOS, CENTRE NATIONAL DE LA RECHERCHE SCIENTIFIQUE, INSTITUT CURIE, UNIVERSITE MONTPELLIER 2Inventors: Jamal TAZI, Florence MAHUTEAU, Romain NAJMAN, Didier SCHERRER, Noelie CAMPOS, Aude GARCEL
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Patent number: 8841321Abstract: Use of a compound for the manufacture of a medicament for the treatment of a bacterial infection provided that the bacterial infection is other than a Mycobacterial infection, said compound being a compound of formula (Ia) or (Ib) a pharmaceutically acceptable acid or base addition salt thereof, a stereochemically isomeric form thereof, a tautomeric form thereof or a N-oxide form thereof, wherein R1 is hydrogen, halo, haloalkyl, cyano, hydroxy, Ar, Het, alkyl, alkyloxy, alkylthio, alkyloxyalkyl, alkylthioalkyl, Ar-alkyl or di(Ar)alkyl; p is 1, 2, 3 or 4; R2 is hydrogen, hydroxy, mercapto, alkyloxy, alkyloxyalkyloxy, alkylthio, mono or di(alkyl)amino or a radical of formula; R3 is alkyl, Ar, Ar-alkyl, Het or Het-alkyl; q is 1, 2 or 3; R4 and R5 are hydrogen, alkyl or benzyl; or R4 and R5 together and including the N to which they are attached may form a ring; R6 is hydrogen, halo, haloalkyl, hydroxy, Ar, alkyl, alkyloxy, alkylthio, alkyloxyalkyl, alkythioalkyl, Ar-alkyl or di(Ar)alkyl; or two vicinal R6 radicaType: GrantFiled: June 26, 2006Date of Patent: September 23, 2014Assignee: Janssen Pharmaceutica NVInventors: Koenraad Jozef Lodewijk Marcel Andries, Anil Koul, Jérôme Emile Georges Guillemont, David Francis Alain Lançois, Magali Madeleine Simone Motte, Ismet Dorange, Leo Jacobus Jozef Backx, Lieven Meerpoel
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Publication number: 20140275164Abstract: Compositions and methods are provided for inhibiting or treating the early and established stages of inflammatory diseases by administration of an effective dose of the desethylhydroxychloroquine (DHCQ). A benefit of the methods is the ability to deliver a dose of agent that is effective in treating inflammation while sparing the individual from retinal toxicity.Type: ApplicationFiled: March 14, 2014Publication date: September 18, 2014Inventors: William H. Robinson, Jeremy Sokolove, Qian Wang
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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: 20140256619Abstract: The present invention relates to the use of avermectin derivative as a drug for the treatment of parasitic infections. The avermectin derivative is represented by the formula (I) wherein: (i) R1 is chosen from the group constituted of —CH(CH3)2, —CH(CH3)CH2CH3, or cyclohexyle, (ii) X represents —CH2CH2—, or —CH?CH—, (iii) R2 is chosen from the group constituted of or —OH group, (iv) R3 is OH or NOH, (v) represents a single bond when R3 is OH, or a double bond when R3 is NOH, as an inhibitor of a membrane-bound protein which transports exogenous compounds out of target cells.Type: ApplicationFiled: October 18, 2012Publication date: September 11, 2014Inventors: Anne Lespine, Roger Prichard, Cecile Menez
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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: 8828438Abstract: A solid amorphous dispersion comprises a cholesteryl ester transfer protein (CETP) inhibitor, an inhibitor of 3-hydroxy-3-methylglutaryl-coenzyme A reductase (HMG-CoA reductase inhibitor), and a concentration enhancing polymer. At least a major portion of the CETP inhibitor in the dispersion is amorphous. The solid amorphous dispersion provides concentration-enhancement of the CETP inhibitor when administered to an aqueous use environment.Type: GrantFiled: May 22, 2006Date of Patent: September 9, 2014Assignee: Bend Research, Inc.Inventors: Dwayne Thomas Friesen, Bruno Caspar Hancock, Rodney James Ketner, David Keith Lyon, James Alan Shriver Nightingale, Ravi Mysore Shanker
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Publication number: 20140249144Abstract: Disclosed is a compound which has a low molecular weight and has an activity of enhancing the production of EPO and/or an activity of enhancing the production of hemoglobin.Type: ApplicationFiled: May 12, 2014Publication date: September 4, 2014Applicant: KOWA COMPANY, LTD.Inventors: Masanori Ashikawa, Junya Tagashira, Akiyasu Koketsu, Toshiharu Morimoto, Takahiro Kitamura, Syunji Takemura, Gen Watanabe, Tatsuaki Nishiyama, Satoshi Goda, Masaki Yamabi, Takeshi Doi, Hiroyuki Ishiwata
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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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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: 20140243337Abstract: The invention provides certain phenyl carboxamide-containing compounds of the Formula (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: ApplicationFiled: October 1, 2012Publication date: August 28, 2014Inventors: Michael D. Altman, Maria Emilia Di Francesco, John Michael Ellis, Sandra Lee Knowles, Alan B. Northrup
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Patent number: 8815903Abstract: The present invention provides a compound represented by the general formula (I) of the present invention, which has EP1 receptor antagonism: wherein A represents a benzene ring, a pyridine ring, or the like; Y1 represents a C1-6 alkylene group or the like; Y2 represents a single bond or the like; Z represents —C(?O)—NHSO2R6, an acidic 5-membered hetero ring group, or the like; R1 represents a hydrogen atom or the like; R2 represents a phenyl group, a 5-membered aromatic heterocyclic group, or the like; R3 represents a halogen atom, a C1-6 alkoxy group, or the like; R4 represents a hydrogen atom, a halogen atom, or the like; R5 represents a hydrogen atom or the like; and R6 represents a C1-6 alkyl group or the like], or a pharmaceutically acceptable salt thereof. Furthermore, the compound (I) of the present invention can be used as an agent for treating or preventing LUTS, in particular, various symptoms of OABs.Type: GrantFiled: January 24, 2012Date of Patent: August 26, 2014Assignees: Kissei Pharmaceutical Co., Ltd., Kyorin Pharmaceutical Co., Ltd.Inventors: Kazuya Tatani, Atsushi Kondo, Tatsuhiro Kondo, Naohiro Kawamura, Shigeki Seto, Yasushi Kohno
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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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Publication number: 20140235671Abstract: Compounds of the invention are of the formula 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: ApplicationFiled: April 30, 2014Publication date: August 21, 2014Applicant: Karus Therapeutics LimitedInventors: Stephen Joseph SHUTTLEWORTH, Cyrille Davy TOMASSI
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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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Patent number: 8802701Abstract: The present invention refers to new compounds represented by the general formula (I) where X is represented by the general formula (II) and Y is represented by the general formula (III). The relation X to Y may vary from 1:1 to 1:7. The radicals R1, R2, R3, R4, R5, and R6 in formula (II) are represented by: R1=H, CF3, CH3, OCH3, NH2, halogen; R2=H, CH3, NH2, halogen, NH—CHCH3(CH2)3N(C2H5)(CH2CH2OH), CH(OH)-2(C5H11N), NH—R7—N—(C2H5)2; R3=H, m-OC6H4CF3, NH2; R4=H, CH3, OCH3, NH2, halogen; R5=H, CH3, CF3, NH2, halogen; R6=H, CF3, CH3, NH2, halogen, NH—R8—N—(C2H5)2, NHCH(CH3)(CH2)3NH2; R7=(CH2)2, (CH2)3, CHCH3CH2, (CH2)4, (CH2)5, CHCH3(CH2)3, (CH2)6, (CH2)8, (CH2)10, (CH2)12; R8=CHCH3(CH2)3, CHCH3(CH2)CHCH3, (CH2)2, (CH2)3, (CH2)6, (CH2)3O(CH2)3. This invention also refers to a process of preparation of these compounds (formula I), and antiparasitic pharmaceutical compositions thereof.Type: GrantFiled: November 27, 2012Date of Patent: August 12, 2014Assignee: Fundação Oswaldo CruzInventors: Nubia Boechat, Marcus Vinicius Nora de Souza, Alessandra Leda Valverde, Antoniana Ursine Krettli
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Publication number: 20140219957Abstract: The invention features methods of treating an immune disorder characterized by elevated Pin1 marker levels in a subject by administering a retinoic acid compound. Additionally, the invention features methods of treating immune disorders (e.g., immune disorders characterized by elevated Pin1 marker levels) by administering a retinoic acid compound in combination with an anti-inflammatory, anti-viral, or anti-microbial compound.Type: ApplicationFiled: May 29, 2012Publication date: August 7, 2014Applicant: Beth Israel Deaconess Medical Center, Inc.Inventors: Kun Ping Lu, Adrian Tun-Kyi, Greg Finn
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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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Publication number: 20140221411Abstract: The present invention relates to a 2-hydroxyarylamide derivative or a pharmaceutically acceptable salt thereof, a preparation method thereof, and a pharmaceutical composition for preventing or treating cancer comprising the same as an active ingredient. The 2-hydroxyarylamide derivative prepared by the present invention is excellent in the inhibition of the activity of TMPRSS4 serine protease and the suppression of the infiltration of TMPRSS4-expressed cancer cells, and thus can be useful as a composition for preventing or treating cancer by inhibiting TMPRSS4 over-expressed in cancer cells, particularly, colorectal cancer, lung cancer, breast cancer, prostate cancer, ovarian cancer, pancreatic cancer, or stomach cancer cells.Type: ApplicationFiled: April 18, 2014Publication date: August 7, 2014Applicant: Korea Research Institute of Bioscience and BiotechnologyInventors: Semi KIM, Ill Young LEE, Hye-Jin MIN, Eun-Hee NAM, Pilho KIM, Chang Soo YUN, Dong Joon KO
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Patent number: 8791090Abstract: Disclosed is a compound which has a low molecular weight and has an activity of enhancing the production of EPO and/or an activity of enhancing the production of hemoglobin.Type: GrantFiled: March 31, 2010Date of Patent: July 29, 2014Assignee: Kowa Company, Ltd.Inventors: Masanori Ashikawa, Junya Tagashira, Akiyasu Koketsu, Toshiharu Morimoto, Takahiro Kitamura, Syunji Takemura, Gen Watanabe, Tatsuaki Nishiyama, Satoshi Goda, Masaki Yamabi, Takeshi Doi, Hiroyuki Ishiwata
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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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Publication number: 20140200227Abstract: The present disclosure describes thiazole and pyridine carboxamide derivatives, 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: Chu-Biao Xue, Yun-Long Li, Hao Geng, Jun Pan, Anlai Wang, Ke Zhang, Wenqing Yao, Fenglei Zhang, Jincong Zhuo
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Patent number: 8778967Abstract: The invention relates to heterocyclic compounds consisting of a core nitrogen atom surrounded by three pendant groups, wherein two of the three pendant groups are preferably benzimidazolyl methyl and tetrahydroquinolyl, and the third pendant group contains N and optionally contains additional rings. The compounds bind to chemokine receptors, including CXCR4 and CCR5, and demonstrate protective effects against infection of target cells by a human immunodeficiency virus (HIV).Type: GrantFiled: January 25, 2012Date of Patent: July 15, 2014Assignee: Genzyme CorporationInventors: Gary Bridger, Renato T Skelj, Al Kaller, Curtis Harwig, David Bogucki, Trevor R Wilson, Jason B Crawford, Ernest J McEachern, Bem Atsma, Siqiao Nan, Yuanxi Zhou, Dominique Schols, Christopher Dennis Smith, Maria R Di Fluri
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Publication number: 20140194464Abstract: The present invention relates to the use of crenolanib, in a pharmaceutically acceptable salt form for the treatment of FLT3 mutated proliferative disorders driven by constitutively activated mutant FLT3, and to a method of treatment of warm-blooded animals, preferably humans, in which a therapeutically effective dose of crenolanib is administered to an animal suffering from said disease or condition:Type: ApplicationFiled: October 14, 2013Publication date: July 10, 2014Inventor: Vinay K. Jain
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Patent number: 8765781Abstract: The present invention is a DNA intercalating agent represented by the structure Y—Z—Y, wherein Y is an antitumor bis-carbazole and Z is a linear arrangement of multiple aromatic rings, containing at least two aromatic rings, or at least two alicyclic rings, said rings being linked in a 1,4 or 1,3 manner. Methods of inhibiting cancer cells and treating subjects having cancer with these agents are also provided.Type: GrantFiled: July 2, 2009Date of Patent: July 1, 2014Assignee: Trustees of Dartmouth CollegeInventors: Gordon W. Gribble, Dmity A. Androsov
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Publication number: 20140179697Abstract: Disubstituted octahydropyrrolo[3,4-c]pyrrole compounds are described, which are useful as orexin receptor modulators. Such compounds may be useful in pharmaceutical compositions and methods for the treatment of diseased states, disorders, and conditions mediated by orexin activity, such as insomnia.Type: ApplicationFiled: December 23, 2013Publication date: June 26, 2014Applicant: JANSSEN PHARMACEUTICA NVInventors: Wenying Chai, Michael A. Letavic, Kiev S. Ly, Daniel J. Pippel, Dale A. Rudolph, Kathleen C. Sappey, Brad M. Savall, Chandravadan R. Shah, Brock T. Shireman, Akinola Soyode Johnson, Emily M. Stocking, Devin M. Swanson
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Publication number: 20140171441Abstract: Pharmaceutical compositions of a low-solubility drug and lower alkanoate-, phthalate- and trimellitate esters of hydroxypropyl methyl cellulose and lower alkanoate- and succinate esters of cellulose and methyl cellulose are disclosed that provide enhanced concentrations of the drug in a use environment.Type: ApplicationFiled: December 17, 2013Publication date: June 19, 2014Applicant: BEND RESEARCH, INC.Inventors: Walter C. Babcock, Dwayne T. Friesen, Warren K. Miller, Daniel T. Smithey
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Publication number: 20140170162Abstract: The invention relates to treatment and/or prevention of nerve injury. In one embodiment, the present invention provides a method of preserving the neuromuscular junction (NMJ) in an individual by administering a therapeutically effective dosage of a composition comprising an inhibitor of Wnt3a, and an inhibitor of MMP3 to the individual. In another embodiment, the present invention provides a method of stabilizing NMJ after nerve injury by inhibiting the WNT and beta-catenin signaling pathway and preserving agrin.Type: ApplicationFiled: December 18, 2013Publication date: June 19, 2014Applicant: THE REGENTS OF THE UNIVERSITY OF CALIFORNIAInventor: Ranjan Gupta
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Patent number: 8754053Abstract: The present invention relates to compounds formula (I), wherein P is P1, P2, heterocyclyl or heterocyclyl substituted by one to five Z; and wherein A1, A2, A3, A4, G1, R1, R2, R3, R4, R5, R6, R17, R18, R19 and R20 are as defined in claim 1; or a salt or N-oxide thereof. Furthermore, the present invention relates to processes and intermediates for preparing compounds of formula (I), to insecticidal, acaricidal, nematicidal and molluscicidal compositions comprising the compounds of formula (I) and to methods of using the compounds of formula (I) to control insect, acarine, nematode and mollusc pests.Type: GrantFiled: February 17, 2011Date of Patent: June 17, 2014Assignee: Syngenta Crop Protection LLCInventors: Thomas Pitterna, Myriem El Qacemi, Jerome Yves Cassayre, Peter Renold, Vladimir Bobosik