Additional Nitrogen Containing Unsaturated Hetero Ring (e.g., Thiazole, Etc.) Patents (Class 544/284)
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Patent number: 8883808Abstract: Patients suffering from serotonin-mediated diseases or conditions, such as depression, may be treated by administering an effective combined amount of a 5-HT7 receptor antagonist and a serotonin reuptake inhibitor.Type: GrantFiled: October 18, 2006Date of Patent: November 11, 2014Assignee: Janssen Pharmaceutica N.V.Inventors: Pascal Bonaventure, Christine Dugovic, Curt A. Dvorak, Dale A. Rudolph, Jonathan Edward Shelton
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Publication number: 20140326987Abstract: A compound represented by Formula 1. An organic electric element includes a first electrode, a second electrode, and an organic material layer between the first electrode and the second electrode. The organic material layer includes the compound represented by Formula 1. When the organic electric element includes the compound in the organic material layer, luminous efficiency, stability, and life span can be improved.Type: ApplicationFiled: November 13, 2012Publication date: November 6, 2014Inventors: Junghwan Park, Sunhee Lee, Soungyun Mun, Daesung Kim, Hwasoon Jung, Wonsam Kim, Jihun Byun, Bumsung Lee
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Publication number: 20140323447Abstract: The present invention relates to compounds of general formula (I) and the tautomers and the salts thereof, particularly the pharmaceutically acceptable salts thereof with inorganic or organic acids and bases, which have valuable pharmacological properties, particularly an inhibitory effect on epithelial sodium channels and the use thereof for the treatment of diseases, particularly diseases of the lungs and airways.Type: ApplicationFiled: April 28, 2014Publication date: October 30, 2014Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Joerg KLEY, Armin HECKEL
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Publication number: 20140315932Abstract: The present specification relates to the use of a quinazolinone compound of the formula (I) wherein R1, R2, R3, R4, R5 and m are as defined in the specification and in the claims, in free form or in salt form, and, where possible, in acid addition salt form.Type: ApplicationFiled: July 2, 2014Publication date: October 23, 2014Applicant: NOVARTIS AGInventors: Timothy John RITCHIE, Andrew James CULSHAW, Christopher Thomas BRAIN, Edward Karol DZIADULEWICZ, Terance William HART
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Publication number: 20140315886Abstract: Methods of treating disorders using compounds (I) that modulate stri-atal-enriched tyrosine phosphatase (STEP) are described herein. Exemplary disorders include schizophrenia and cognitive deficit. Formula (I).Type: ApplicationFiled: June 28, 2012Publication date: October 23, 2014Applicant: OTSUKA PHARMACEUTICAL CO., LTD.Inventors: Masaki Suzuki, Kazumi Kondo, Muneaki Kurimura, Krishna Reddy Valluru, Akira Takahahi, Takeshi Kuroda, Haruka Takahashi, Tae Fukushima, Shin Miyamura, Indranath Ghosh, Abhishek Dogra, Geraldine Harriman, Amy Elder, Satoshi Shimiza, Kevin J. Hodgetts, Jason S. Newcom
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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: 8865704Abstract: The present invention relates to known and novel compounds of formula (I) as herein described and pharmaceutical compositions thereof. The compounds of formula (I) have inhibitory effect on the Wnt pathway and are therefore useful in the preparation of a medicament, in particular for the treatment of cancer.Type: GrantFiled: October 6, 2010Date of Patent: October 21, 2014Assignee: Siena Biotech S.p.A.Inventors: Maurizio Varrone, Arianna Nencini, Joanna Margaret Quinn, Andrea Caricasole, Annette Cornelia Bakker, Giovanni Gaviraghi, Massimilano Salerno
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Patent number: 8865897Abstract: The invention relates to a new crystalline form of the acetate salt of which may be used, for example, for prevention or treatment of transplant rejection.Type: GrantFiled: October 18, 2007Date of Patent: October 21, 2014Assignee: Novartis AGInventors: Piotr Karpinski, Stéphanie Monnier, Elias Ndzie, Dimitris Papoutsakis, Paul A Sutton
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Patent number: 8865708Abstract: Compounds of Formulas I-XLIII are identified as direct inhibitors of p97 ATPase or of the degradation of a p97-dependent ubiquitin-proteasome system (UPS) substrate. Methods and compositions are disclosed for inhibiting p97 ATPase and the degradation of a p97-dependent UPS substrate, and for identifying inhibitors thereof.Type: GrantFiled: May 6, 2011Date of Patent: October 21, 2014Assignees: California Institute of Technology, The University of Kansas, Cleave Biosciences, Inc.Inventors: Raymond J. Deshaies, Tsui-Fen Chou, Frank J. Schoenen, Kelin Li, Kevin J. Frankowski, Jeffrey Aube, Samuel W. Gerritz, Han-Jie Zhou
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Publication number: 20140309246Abstract: This invention is in the fields of cancer therapy. More particularly it concerns compounds which are useful agents for inhibiting cell proliferative disorders, especially those disorders characterized by over activity and/or inappropriate activity of a EGFR, including EGFR-related cancers, and methods for treating these disorders.Type: ApplicationFiled: March 16, 2012Publication date: October 16, 2014Applicant: THE TRUSTEES OF THE UNIVERSITY OF PENNSYLVANIAInventors: Mark I. Greene, Hongtao Zhang, Alan Berezov, Zheng Cai
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Publication number: 20140309215Abstract: Aminoquinazolinyl compounds of formula (I) are described, which are useful as prolyl hydroxylase inhibitors. Such compounds may be used in pharmaceutical compositions and methods for the treatment of disease states, disorders, and conditions mediated by prolyl hydroxylase activity. Thus, the compounds may be administered to treat, e.g., anemia, vascular disorders, metabolic disorders, and wound healing.Type: ApplicationFiled: June 24, 2014Publication date: October 16, 2014Inventors: Michael H. RABINOWITZ, Mark D. ROSEN, Kyle T. TARANTINO, Hariharan VENKATESAN
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Patent number: 8859544Abstract: The invention relates to compounds corresponding to formula (I): in which R3 and R4 together form, with the carbon atoms of the phenyl nucleus to which they are attached, a 6-membered nitrogenous heterocycle corresponding to one of formula (A), (B) or (C) below: in which the wavy lines represent the phenyl nucleus to which R3 and R4 are attached. Preparation process and therapeutic use.Type: GrantFiled: July 4, 2011Date of Patent: October 14, 2014Assignee: SanofiInventors: Chantal Alcouffe, Corentin Herbert, Gilbert Lassalle
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Patent number: 8859571Abstract: Disclosed are compounds having the formula: wherein R1, R2, R3, R4, R5, R6 and R7 are as defined herein, and methods of making and using the same.Type: GrantFiled: November 1, 2010Date of Patent: October 14, 2014Assignee: GlaxoSmithKline LLCInventors: Lara S. Kallander, Brian Griffin Lawhorn, Joanne Philp
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Patent number: 8859570Abstract: The present invention relates to AZD2171 maleate salt, to particular crystalline forms of AZD2171 maleate salt, to processes for their preparation, to pharmaceutical compositions containing them as active ingredient, to their use in the manufacture of medicaments for use in the production of antiangiogenic and/or vascular permeability reducing effects in warm-blooded animals such as humans, and to their use in methods for the treatment of disease states associated with angiogenesis and/or increased vascular permeability.Type: GrantFiled: December 23, 2009Date of Patent: October 14, 2014Assignee: AstraZeneca ABInventor: James McCabe
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Publication number: 20140303164Abstract: Compounds of formula I: or salts thereof are disclosed. Also disclosed are pharmaceutical compositions comprising a compound of formula I, processes for preparing compounds of formula I, intermediates useful for preparing compounds of formula I and therapeutic methods for treating a Retroviridae viral infection including an infection caused by the HIV virus.Type: ApplicationFiled: February 28, 2014Publication date: October 9, 2014Inventors: Gediminas BRIZGYS, Eda CANALES, Chien-Hung CHOU, Michael GRAUPE, Yunfeng Eric HU, John O. LINK, Qi LIU, Yafan LU, Roland D. SAITO, Scott D. SCHROEDER, John R. SOMOZA, Winston C. TSE, Jennifer R. ZHANG
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Patent number: 8853225Abstract: The present invention relates to a compound of formula (I), which has valuable pharmacological properties, particularly an inhibiting effect on signal transduction mediated by tyrosine kinases, processes for stereoselectively preparing these compounds, particularly pharmaceutical formulations suitable for inhalation and their use for the treatment of diseases, particularly tumoral diseases, benign prostatic hyperplasia and diseases of the lungs and airways.Type: GrantFiled: January 27, 2012Date of Patent: October 7, 2014Assignee: Boehringer Ingelheim International GmbHInventors: Waldermar Pfrengle, Guenther Huchler, Markus Ostermeier, Peter Sieger
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Publication number: 20140296206Abstract: Compounds and compositions useful for treating disorders related to Kit are described herein.Type: ApplicationFiled: March 14, 2014Publication date: October 2, 2014Applicant: BLUEPRINT MEDICINES CORPORATIONInventors: Lucian V. DiPietro, Brian L. Hodous, Joseph L. Kim, Chandrasekhar V. Miduturu, Steven Mark Wenglowsky, Douglas Wilson, Yulian Zhang
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Publication number: 20140296260Abstract: The invention relates to novel quinazolinone compounds and their use as inhibitors of PI3 kinases, for example, PI3K?, for treating and/or preventing diseases, disorder, and conditions associated with modulating PI3 kinase activity. Novel 3-aryl-2-((arylamino)methyl)quinazolin-4(3H)-one derivatives and pharmaceutically acceptable salts or solvates thereof and their use for the treatment or prevention of diseases, disorders, and conditions associated with the activity of one or more PI3 kinase, such as PI3K?, are disclosed.Type: ApplicationFiled: March 28, 2014Publication date: October 2, 2014Inventors: Ben C. Askew, Takeru Furuya
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Publication number: 20140296247Abstract: Biologically active compounds, which are useful for treating a sexual disorder, are provided herein. Further provided are pharmaceutical compositions formulated for transdermal composition, which comprise a biologically active compound useful for treating a sexual disorder. The compounds and pharmaceutical compositions allow for a prolonged presence of a biologically active compound in plasma. Further provided herein are methods and uses of the compounds and pharmaceutical compositions described herein in the treatment of a sexual disorder, including female sexual disorders.Type: ApplicationFiled: December 26, 2011Publication date: October 2, 2014Inventors: Vladimir Kogan, Leonid Lurya, Lev Tabachnik
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Publication number: 20140296266Abstract: Compounds of formula I: or salts thereof are disclosed. Also disclosed are pharmaceutical compositions comprising a compound of formula I, processes for preparing compounds of formula I, intermediates useful for preparing compounds of formula I and therapeutic methods for treating a Retroviridae viral infection including an infection caused by the HIV virus.Type: ApplicationFiled: February 28, 2014Publication date: October 2, 2014Inventors: Yunfeng Eric HU, John O. LINK, Qi LIU, Winston C. TSE, Jennifer R. ZHANG
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Publication number: 20140296230Abstract: The present invention encompasses compounds of general formula (I) wherein the groups R1 to R4 and A1 to A5 have the meanings given in the claims and in the specification. The compounds of the invention are suitable for the treatment of diseases characterized by excessive or abnormal cell proliferation pharmaceutical preparations containing such compounds and their uses as a medicament.Type: ApplicationFiled: March 26, 2014Publication date: October 2, 2014Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Christian SMETHURST, Harald ENGELHARDT, Davide GIANNI, Ulrich REISER
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Patent number: 8846654Abstract: A subject-matter of the present invention is the use of compounds of formula (I) in the base, hydrate or solvate form or in the form of their mixtures, as medicaments or for the preparation of medicaments intended for the treatment of at least one cardiovascular disease and/or to prevent the appearance of at least one cardiovascular disease.Type: GrantFiled: October 7, 2011Date of Patent: September 30, 2014Assignee: SanofiInventors: Philip Janiak, Gilbert Marciniak, Jean-Francois Nave, Fabrice Viviani
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Patent number: 8846700Abstract: Disclosed are compounds of the following formula and their pharmaceutically-acceptable salts, which have an effect of glucokinase activation and are useful in the field of medicines for treatment for diabetes, obesity, etc. (wherein ring A represents a pyrazolyl group optionally having a lower alkyl group, etc.; ring B represents a heteroaryl group; R represents a lower alkyl group, etc.; R1 represents a group of a formula: (wherein R11 and R12 each independently represent a hydrogen atom, etc.; m indicates an integer of from 2 to 6), etc.; R2 represents a lower alkyl group, etc.; r indicates an integer of from 0 to 3; k indicates an integer of from 0 to 4).Type: GrantFiled: September 9, 2013Date of Patent: September 30, 2014Assignee: MSD K.K.Inventors: Tomoharu Iino, Akio Ohno, Norikazu Otake, Takuya Suga, Masanori Asai
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Patent number: 8846000Abstract: The present invention is directed to radiolabeled pyrimidinone compounds of general structural formula I which are useful as radiotracers for quantitative imaging of PDE10 in mammals.Type: GrantFiled: May 26, 2010Date of Patent: September 30, 2014Assignee: Merck Sharp & Dohme Corp.Inventors: Christopher D. Cox, Broc A. Flores, Eric Hostetler, Hong Fan
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Publication number: 20140288048Abstract: Compounds and pharmaceutical compositions that modulate kinase activity, including PI3 kinase activity, and compounds, pharmaceutical compositions, and methods of treatment of diseases and conditions associated with kinase activity, including P13 kinase activity, are described herein.Type: ApplicationFiled: June 5, 2014Publication date: September 25, 2014Inventors: Alfredo C. CASTRO, Catherine A. EVANS, Somarajannair JANARDANANNAIR, Andre LESCARBEAU, Tao LIU, Daniel A. SNYDER, Martin R. TREMBLAY, Pingda REN, Yi LIU, Liansheng LI, Katrina CHAN
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Publication number: 20140283218Abstract: Compounds of formula I wherein the substituents are as defined in claim 1, and the agrochemically acceptable salts and all stereoisomers and tautomeric forms of the compounds of formula I can be used as insecticides and can be prepared in a manner known per se.Type: ApplicationFiled: June 27, 2012Publication date: September 18, 2014Applicant: SYNGENTA PARTICIPATIONS AGInventors: Roger Graham Hall, Andrew Edmunds, Andre Jeanguenat, Thomas Pitterna, Sebastian Rendler
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Publication number: 20140275095Abstract: The present invention is directed to compounds of Formula I: wherein X is CR1 or N; Y is CR2 or N; Z is NH or O; R1 is alkoxy, triazolyl, oxazolyl, isoxazolyl, oxadiazolyl, or pyrimidinyl; R2 is H, alkyl, or halo; R3 is H, alkyl, alkoxy, halo, triazolyl, oxazolyl, or pyrimidinyl; R4 is alkyl; R5 is pyridyl; benzoxazolyl; pyrimidinyl; pyridazinyl; quinoxalinyl; pyrazinyl; or quinazolinyl; wherein the pyridyl; benzoxazolyl; pyrimidinyl; pyridazinyl; quinoxalinyl; pyrazinyl; or quinazolinyl is optionally substituted with one or two substituents independently selected from the group consisting of alkyl, halo, or phenyl; and R6 is H or alkyl. Methods of making the compounds of Formula I are also described. The invention also relates to pharmaceutical compositions comprising compounds of Formula I. Methods of using the compounds of the invention are also within the scope of the invention.Type: ApplicationFiled: March 12, 2014Publication date: September 18, 2014Applicant: JANSSEN PHARMACEUTICA NVInventors: Curt A. Dvorak, Brock T. Shireman
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Publication number: 20140275129Abstract: Tetrahydroisoquinolin-2-yl-(quinazolin-4-yl)methanone derivatives represented by formula (I), pharmacologically acceptable salts thereof, and compositions containing such compounds are described. Methods for treating hyperproliferative disorders by administering the compounds are also described. 1,2,3,4-tetrahydroisoquinoline derivatives for making tetrahydroisoquinolin-2-yl-(quinazolin-4-yl)methanone compounds are also described.Type: ApplicationFiled: March 14, 2014Publication date: September 18, 2014Applicant: Rexahn Pharmaceuticals, Inc.Inventors: Young Bok Lee, Jae Min Kim, Deog Joong Kim, Chang-Ho Ahn
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Publication number: 20140275711Abstract: Disclosed are novel 1-(arylmethyl)-5,6,7,8-tetrahydroquinazoline-2,4-diones and analogs thereof, represented by the Formula I, wherein Ar, A, B, R3-R6 are defined herein. Compounds having Formula I are PARP inhibitors. Therefore, compounds of the invention may be used to treat clinical conditions that are responsive to the inhibition of PARP activity, such as cancer.Type: ApplicationFiled: November 1, 2012Publication date: September 18, 2014Inventors: Suixiong Cai, Ye Edward Tian, Lizhen Wu, Lijun Liu, Xiaozhu Wang, Yangzhen Jiang, Guoxiang Wang, Xiuyan Zhang, Qingbing Xu, Zheng Meng
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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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Patent number: 8835445Abstract: The present disclosure provides compounds of Formula I: or a pharmaceutically acceptable salt thereof, wherein R5, R6 and Z are as described herein. The disclosure also provides pharmaceutical compositions thereof; and methods for inhibiting DHFR activity; and methods for treating cell proliferative diseases, autoimmune disease, inflammatory disease or bacterial, fungal or parasitic infection by administering a compound of Formula I.Type: GrantFiled: June 2, 2011Date of Patent: September 16, 2014Assignee: Trius Therapeutics, Inc.Inventors: Zhiyong Chen, Christopher J. Creighton, Mark Cunningham, John Finn, Mark Hilgers, Michael Jung, Lucy Aguirre Kohnen, Thanh Lam, Xiaoming Li, Mark Stidham, Les Tari, Michael Trzoss, Junhu Zhang
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Publication number: 20140256753Abstract: Provided is a process for treating or preventing a viral infection in a subject, wherein the viral infection is from a flavivirus selected from the group consisting of Hepatitis C Virus (genotypes 1-7) and Japanese Encephalitis Virus.Type: ApplicationFiled: August 10, 2012Publication date: September 11, 2014Applicants: Sanford-Burnham Medical Research Institute, Southern Research InstituteInventors: Marintha L. Heil, Nicholas D.P. Cosford, Robert Ardecky, Jiwen Zou
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Publication number: 20140256711Abstract: Disclosed are an anti-angiogenic compound, represented by Chemical Formula I, or a pharmaceutically acceptable salt thereof, a preparation method thereof, and a pharmaceutically acceptable composition including the same. Because the compound of Chemical Formula I potently suppresses the angiogenesis, the compound of Chemical Formula I is applicable to the prevention and treatment of diseases caused by aberrant activity of vascular endothelial growth factor, and available as an anti-angiogenic agent.Type: ApplicationFiled: July 27, 2012Publication date: September 11, 2014Applicant: Boryung Pharmaceutical Co., Ltd.Inventors: Ji Han Kim, Je Hak Kim, Joon Kwang Lee, Hahn-Sun Jung, Nam Seok Han, Yong Park, Seung-Hoon Kang, Hee Jin Jeong, Kyung-Tae Lee, Hye Eun Choi, Yong Ha Chi, Joo Han Lee, Soo Heui Paik
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Patent number: 8829014Abstract: Thiazole and thiophene compounds are disclosed having utility in treating inflammatory conditions, immunoinflammatory conditions, autoimmune diseases, and cancers. Methods for the synthesis of these compounds are also disclosed.Type: GrantFiled: June 15, 2012Date of Patent: September 9, 2014Assignees: Board of Supervisors of Louisiana State University and Agricultural and Mechanical College, B.V. Patel Pharmaceutical Education & Research Development (PERD) CentreInventors: Anthony Giordano, Kamala K. Vasu, Hardik M. Thakar, Rajan S. Giri, Vasudevan Sudarsanam, Swapnil G. Yerande, Gajanan S. Inamdar
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Publication number: 20140249139Abstract: The invention relates to substituted quinazoline derivative of the formula (I), wherein A, X1, X2, X3, X4 and R5 are as defined in the description. Such compounds are suitable for the treatment of a disorder or disease which is mediated by the activity of the PI3K enzymes.Type: ApplicationFiled: October 19, 2012Publication date: September 4, 2014Applicant: NOVARTIS AGInventors: Pascal Furet, Christina Hebach, Klemens Hogenauer, Gregory Hollingworth, Ian Lewis, Alexander Baxter Smith, Nicolas Solvermann, Frederic Stauffer, Romain Wolf, Frederic Zecri
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Publication number: 20140249129Abstract: This invention relates to substituted bicyclic dihydropyrimidinones of formula 1 and their use as inhibitors of neutrophil elastase activity, pharmaceutical compositions containing the same, and methods of using the same as agents for treatment and/or prevention of pulmonary, gastrointestinal and genitourinary diseases, inflammatory diseases of the skin and the eye and other autoimmune and allergic disorders, allograft rejection, and oncological diseases.Type: ApplicationFiled: February 20, 2014Publication date: September 4, 2014Applicant: Boehringer Ingelheim International GmbHInventors: Christian GNAMM, Thorsten OOST, Stefan PETERS, Klaus RUDOLF
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Publication number: 20140243361Abstract: Polymorphs of N4-(4-([1,2,4]triazolo[1,5-a]pyridin-7-yloxy)-3-methylphenyl)-N6-(4,4-dimethyl-4,5-dihydrooxazol-2-yl)quinazoline-4,6-diamine are provided herein. Processes for preparing the polymorphs and pharmaceutical composition comprising the polymorphs are also disclosed.Type: ApplicationFiled: October 12, 2012Publication date: August 28, 2014Applicant: Array BioPharma Inc.Inventors: Donald T. Corson, Christopher M. Lindemann, Daniel J. Watson
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Patent number: 8815878Abstract: Substituted spiro hemiaminals and methods for their use in the treatment of viral diseases, including hepatitis C viral infections, are described herein.Type: GrantFiled: July 27, 2011Date of Patent: August 26, 2014Assignee: NovaDrug, LLCInventor: Eliezer Huberman
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Patent number: 8815849Abstract: Inhibitors of HCV replication of formula I including stereochemically isomeric forms, and salts, hydrates, solvates thereof, wherein R and R? have the meaning as defined herein. The present invention also relates to processes for preparing said compounds, pharmaceutical compositions containing them and their use, alone or in combination with other HCV inhibitors, in HCV therapy.Type: GrantFiled: July 26, 2011Date of Patent: August 26, 2014Assignee: Janssen R&D IrelandInventors: Koen Vandyck, Wim Gaston Verschueren, Pierre Jean-Marie Bernard Raboisson
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Publication number: 20140235634Abstract: Described herein are compounds of Formula (I) or Formula (VI), pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof. Also provided are particles (e.g., nanoparticles) comprising compounds of Formula (I) or Formula (VI) and pharmaceutical compositions thereof that are mucus penetrating. Methods of using the compounds or pharmaceutical compositions thereof for treating diseases are also provided.Type: ApplicationFiled: February 14, 2014Publication date: August 21, 2014Applicant: Kala Pharmaceuticals, Inc.Inventors: Winston Zapanta ONG, Pawel Wojciech NOWAK, Ben C. ASKEW, Jinsoo KIM
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Publication number: 20140235657Abstract: Described herein are compounds of Formula (I)-(III), pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof. Also provided are particles (e.g., nanoparticles) comprising compounds of Formula (I)-(III) and pharmaceutical compositions thereof that are mucus penetrating. Methods of using the compounds or pharmaceutical compositions thereof for treating and/or preventing diseases are also provided.Type: ApplicationFiled: February 20, 2014Publication date: August 21, 2014Applicant: Kala Pharmaceuticals, Inc.Inventors: Winston Zapanta ONG, Pawel Wojciech Nowak, Ben C. Askew, Jinsoo Kim
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Publication number: 20140235633Abstract: The present invention provides a 4-aminoquinazoline derivative having the chemical structure of the following formula, and the use thereof. It is demonstrated by the pharmacological experiment that, the compound or a salt thereof according to the present invention not only has distinct inhibitory effect on histone deacetylases, but also has stronger differentiation induction and anti-proliferative activities for certain tumor cells. It can be used in the treatment of cancers and diseases related to cell differentiation and proliferation. Excellent efficacy is observed especially for leukemia and a solid tumor. As demonstrated by the animal test, the compound or a salt thereof according to the present invention is less toxic.Type: ApplicationFiled: May 10, 2012Publication date: August 21, 2014Applicants: SHANGHAI INSTITUTE OF PHARMACEUTICAL INDUSTRY, JIANGSU HENGYI PHARMACEUTICAL CO. LTD.Inventors: Jianqi Li, Qingwei Zhang, Wangping Cai
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Patent number: 8809354Abstract: Surprising antiviral activity of 3-amino-2-(4-nitrophenyl)-4-(3H)-quinazolinone (Compound 1) was reported in the treatment or prevention of viral infections, particularly in combination with other antiviral agents such as interferon and/or ribavarin.Type: GrantFiled: December 31, 2011Date of Patent: August 19, 2014Inventors: Sheikh Riazuddin, Osman Ali, Usman Ashfaq, Shaheen N. Khan, Javed Akram, Atta-ur Rahman, M. Iqbal Choudhary, Khalid M. Khan, Zulfiqar Ali Khan
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Publication number: 20140228361Abstract: The present invention relates to the field of medicine. Provided herein are aminoquinazoline derivatives, their salts and pharmaceutical formulations useful in modulating the protein tyrosine kinase activity, and in modulating inter- and/or intra-cellular signaling. Also provided herein are pharmaceutically acceptable compositions comprising the aminoquinazoline compounds and methods of using the compositions in the treatment of hyperproliferative disorders in mammals, especially humans.Type: ApplicationFiled: November 14, 2012Publication date: August 14, 2014Applicant: SUNSHINE LAKE PHARMA CO., LTD.Inventors: Jiancun Zhang, Yingjun Zhang, Weihong Zhang, Bing Liu, Jiquan Zhang, Jinlei Liu, Lu Zhang
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Publication number: 20140228367Abstract: The present disclosure relates to compounds of the Formula (I): and pharmaceutically acceptable salts, as kinase modulators, compatible with the Type-II inhibition of kinases.Type: ApplicationFiled: February 5, 2014Publication date: August 14, 2014Inventor: Gary A. Flynn
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Patent number: 8802659Abstract: Compounds that have agonist activity at one or more of the S1P receptors are provided. The compounds are sphingosine analogs that, after phosphorylation, can behave as agonists at S1P receptors.Type: GrantFiled: August 5, 2010Date of Patent: August 12, 2014Assignee: Biogen Idec MA Inc.Inventors: Jermaine Thomas, Xiaogao Liu, Edward Yin-Shiang Lin, Guo Zhu Zheng, Bin Ma, Richard D. Caldwell, Kevin M. Guckian, Gnanasambandam Kumaravel, Arthur G. Taveras
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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: 20140221402Abstract: This invention provides a class of quinazoline compounds, as represented by formula (I), and their pharmaceutically acceptable salts, wherein: each of R1 and R2 independently, is selected from H, C1-C6 alkoxy, halo-C1-C6 alkoxy, C1-C6-alkoxy-C1-C6 alkoxy, C3-C8 cycloalkoxy, C3-C8 heterocycloalkoxy containing at least one of heteroatoms selected from N, O, S; Z is —NR4—, C(R5)2, S or —O—, wherein R4 is H or C1-C3 alkyl, R5 is the same or different, selected from H or C1-C3 alkyl; R3 is selected from H, halogen, C1-C6 alkyl, C1-C6 alkoxy or halo-C1-C6 alkyl; n is an integer from 0 to 5. This invention also provides methods of preparation and medical uses of the compounds of formula (I) and their pharmaceutically acceptable salts. These compounds have the activity of inhibiting EGFR-TK, and can be used as drugs for the treatment of protein tyrosine kinase related diseases such as tumours, cancers, etc.Type: ApplicationFiled: March 26, 2012Publication date: August 7, 2014Applicant: FUJIAN INSTITUTE OF RESEARCH ON THE STRUCTURE OF MATTER, CHINESE ACADEMY OF SCIENCESInventors: Canzhong Lu, Jianping Yong
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Publication number: 20140221403Abstract: The present invention relates to quinazoline containing zinc-binding moiety based derivatives of Formula (IV) below. These compounds have enhanced and unexpected properties as inhibitors of epidermal growth factor receptor tyrosine kinase (EGFR-TK) and are useful in the treatment of EGFR-TK related diseases and disorders such as cancer. These compounds may further act as HDAC inhibitors.Type: ApplicationFiled: November 25, 2013Publication date: August 7, 2014Applicant: Curis, Inc.Inventors: Changgeng Qian, Xiong Cai, Stephen Gould, Haixiao Zhai
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Patent number: 8796259Abstract: N3-Heteroaryl substituted triazoles and N5-heteroaryl substituted triazoles and pharmaceutical compositions containing the compounds are disclosed as being useful in inhibiting the activity of the receptor protein tyrosine kinase Axl. Methods of using the compounds in treating diseases or conditions associated with Axl activity are also disclosed.Type: GrantFiled: October 4, 2012Date of Patent: August 5, 2014Assignee: Rigel Pharmaceuticals, Inc.Inventors: Pingyu Ding, Dane Goff, Jing Zhang, Rajinder Singh, Sacha Holland, Jiaxin Yu, Thilo J. Heckrodt, Joane Litvak