Nitrogen Bonded Directly To The 1,3-diazine At 2-position Patents (Class 514/272)
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Patent number: 8957083Abstract: The present invention provides a new class of compounds useful for the modulation of beta-secretase enzyme (BACE) activity. The compounds have a general Formula I: wherein variables A1, A3, A4, A5, A6, A8, L, R2, R7, R9, W and Y of Formula I are defined herein. The invention also provides pharmaceutical compositions comprising the compounds, and corresponding uses of the compounds and compositions for treatment of disorders and/or conditions related to plaque formation and deposition, resulting from the activity of BACE. Such BACE mediated disorders include, for example, Alzheimer's Disease, cognitive deficits, cognitive impairments, schizophrenia and other central nervous system conditions. The invention further provides compounds of Formulas II and III, sub-Formula embodiments of Formulas I, II and III, intermediates and processes and methods useful for the preparation of compounds of Formulae I-III.Type: GrantFiled: November 18, 2011Date of Patent: February 17, 2015Assignee: Amgen Inc.Inventors: Ana Elena Minatti, Oleg Epstein, Ryan White, Matthew Weiss, Wenge Zhong, Jonathan D. Low
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Publication number: 20150045339Abstract: The object is to provide an Fms-like tyrosine kinase 3 (FLT3) inhibitor useful as a therapeutic agent for acute myeloid leukemia (AML). A novel nitrogen-containing heterocyclic compound represented by the general formula [1] or a salt thereof is provided. The compound or a salt thereof of the present invention can be used as an active ingredient of a pharmaceutical composition for a treatment of a disease or condition relating to FLT3, such as acute myeloid leukemia (AML) and acute promyelocytic leukemia (APL).Type: ApplicationFiled: October 16, 2014Publication date: February 12, 2015Applicant: FUJIFILM CORPORATIONInventors: Masaru TAKASAKI, Toshiaki TSUJINO, Shintarou TANABE, Megumi OOKUBO, Kimihiko SATO, Atsushi HIRAI, Daisuke TERADA, Shinsuke INUKI, Shinsuke MIZUMOTO
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Patent number: 8952027Abstract: The present invention is directed to compounds of formula I-V and tautomers thereof or 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 undesired thrombosis and Non Hodgkin's Lymphoma.Type: GrantFiled: October 23, 2012Date of Patent: February 10, 2015Assignee: Portola Pharmaceuticals, Inc.Inventors: Zhaozhong J. Jia, Chandrasekar Venkataramani, Wolin Huang, Mukund Mehrotra, Yonghong Song, Qing Xu, Shawn M. Bauer, Jack W. Rose, Brian Kane, Anjali Pandey
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Patent number: 8952025Abstract: The present disclosure provides biologically active compounds of formula (I): and pharmaceutically acceptable salts thereof: compositions comprising these compounds, and methods of using these compounds in a variety of applications, such as treatment or suppression of diseases associated with decreased mitochondrial function resulting in diminished ATP production and/or oxidative stress and/or lipid peroxidation.Type: GrantFiled: April 2, 2013Date of Patent: February 10, 2015Assignee: Arizona Board of Regents, A Body Corporate of the State of Arizona Acting for and on Behalf of Arizona State UniversityInventors: Sidney Hecht, Omar Khdour, Jun Lu, Pablo Arce
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Patent number: 8946249Abstract: Compound of Formula A and pharmaceutically acceptable salts thereof and crystalline Forms I and II of Compound of Formula A! Also, methods for the preparation of such compounds, pharmaceutical compositions comprising such compounds, and methods for their uses.Type: GrantFiled: December 12, 2013Date of Patent: February 3, 2015Assignee: Hutchison Medipharma LimitedInventors: Wei-Guo Su, Weihan Zhang, Hong Jia, Yumin Cui, Yongxin Ren, Yang Sai, Zhenping Wu, Wenji Li, Jiangyong Shao, Zhenping Tian
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Patent number: 8946248Abstract: HIV replication inhibitors of formula a N-oxide, a pharmaceutically acceptable addition salt, a quaternary amine or a stereochemically isomeric form thereof, wherein A is —CH2—CH2—, —CH?CH—, —C?C—; R1 is hydrogen, aryl, formyl, C1-6alkylcarbonyl, C1-6alkyl, C1-6alkyloxycarbonyl, R2 hydroxy, halo, C1-6alkyl, carboxyl, cyano, —C(?O)R6, nitro, amino, mono- or di(C1-6alkyl)amino, polyhalomethyl; X1 is —NR1—, —O—, —S—, —S(?O)p—; R3 is H, C1-6alkyl, halo; R4 is H, C1-6alkyl, halo; R5 is nitro, amino, mono- and diC1-4alkylamino, aryl, halo, —CHO, —CO—R6, —COOR7, —NH—C(?O)H, —NH—C(?O)R6, —CH?N—O—R8; R6 is C1-4alkyl, amino, mono- or di(C1-4alkyl)amino or polyhaloC1-4alkyl; R7 is hydrogen, C1-6alkyl, arylC1-6alkyl; R8 is hydrogen, C1-6alkyl, aryl; p is 1 or 2; aryl is optionally substituted phenyl; pharmaceutical compositions containing these compounds as active ingredient and processes for preparing said compounds and compositions.Type: GrantFiled: September 29, 2005Date of Patent: February 3, 2015Assignee: Janssen R&D IrelandInventors: Jerôme Emile Georges Guillemont, Jan Heeres, Paulus Joannes Lewi
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Publication number: 20150031533Abstract: A pesticidal mixture comprising as active ingredient a mixture of component A and component B, wherein component A is a compound of formula (I), in which Q is i or ii wherein X, Y and Z, m and n, A, G, and R, are as defined as in claim 1, and component B is a compound selected from the insecticides as defined in claim 1. The present invention also relates to methods of using said mixtures for the control of plant pests.Type: ApplicationFiled: January 17, 2013Publication date: January 29, 2015Applicant: SYNGENTA PARTICIPATIONS AGInventors: Anke Buchholz, Fabienne Hatt, Alfred Rindlisbacher, Michel Muehlebach
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Publication number: 20150025055Abstract: The present invention provides compounds, pharmaceutically acceptable compositions thereof, and methods of using the same.Type: ApplicationFiled: July 31, 2014Publication date: January 22, 2015Inventors: Kwangho Lee, Deqiang Niu, Russell C. Petter, Juswinder Singh, Matthew F. Baevsky, Bruce Eaton, Zhendong Zhu, Laura A. D'Agostino
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Publication number: 20150018351Abstract: The present invention provides pyridinonyl PDK1 inhibitors and methods of treating cancer using the same.Type: ApplicationFiled: July 10, 2014Publication date: January 15, 2015Inventors: Kenneth Egnard Lind, Kathy Cao, Edward Yin-shiang Lin, Thinh Ba Nguyen, Bradley T. Tangonan, Daniel A. Erlanson, Kevin Guckian, Robert Lowell Simmons, Wen-cherng Lee, Lihong Sun, Stig Hansen, Nuzhat Pathan, Lei Zhang
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Patent number: 8933090Abstract: The present invention relates to 1-aza-bicycloalkyl derivatives of Formula (I); wherein the substituents are as defined in the specification, to processes for their production, their use as pharmaceuticals and to pharmaceutical compositions comprising them. Formula (I), wherein A represents O or N(R1); Y represents a group of formula, or wherein the left bond is attached to the A group and the right bond is attached to the R group; R represents a substituted or unsubstituted C5-C10aryl, substituted or unsubstituted hetero-C5-C10aryl, a group N(R1)(R4), or a group N(R2)(CHP3R4); R represent a hydrogen, C1-C4alkyl, or CF3; R2 represents hydrogen, C1-C4alkyl, or CF3; R3 represents hydrogen, C1-C4alkyl, or CF3; R4 represents a substituted or unsubstituted C5-C10 aryl or a substituted or unsubstituted C5-C10heteroaryl; in free base or acid addition salt form.Type: GrantFiled: October 19, 2010Date of Patent: January 13, 2015Assignee: Novartis AGInventors: Dominik Feuerbach, Werner Müller, Bernard Lucien Roy, Thomas J. Troxler, Konstanze Hurth, Mathias Frederiksen
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Patent number: 8933089Abstract: This invention concerns pyrimidine derivatives of formula having HIV (Human Immunodeficiency Virus) replication inhibiting properties, the preparation thereof and pharmaceutical compositions comprising these compounds.Type: GrantFiled: March 30, 2007Date of Patent: January 13, 2015Assignee: Janssen R & D IrelandInventors: Jerôme Emile Georges Guillemont, Mikaël Paugam, Bruno François Marie Delest
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Publication number: 20150011574Abstract: The present invention provides a compound which enhances the production of erythropoietin. The present invention provides a compound represented by the formula (1) wherein R1: an aromatic hydrocarbon ring group or an aromatic heterocyclic group; R2: a hydrogen atom, an alkyl group, or a heterocycloalkyl group; R3: a hydrogen atom or an alkyl group; A: a hydrogen atom or a hydroxy group; L: —NHCO— or —OCH2—; and X: a nitrogen atom or ?CH—.Type: ApplicationFiled: September 24, 2014Publication date: January 8, 2015Applicant: DAIICHI SANKYO COMPANY, LIMITEDInventors: Tatsuya NISHI, Naoki TANAKA, Ryoko KITAZAWA, Riki GOTO, Takashi ISHIYAMA
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Patent number: 8927563Abstract: There is provided a compound of formula I, which compound has antiinflammatory activity (e.g. through inhibition of one or more of members of: the family of p38 mitogen-activated protein kinase enzymes; Syk kinase; and members of the Src family of tyrosine kinases, e.g., Src and Lck) and has use in therapy, including in pharmaceutical combinations, especially in the treatment of inflammatory diseases, including inflammatory diseases of the lung, eye and intestines.Type: GrantFiled: April 1, 2014Date of Patent: January 6, 2015Assignees: Respivert Limited, Topivert Pharma LimitedInventor: Matthew Colin Thor Fyfe
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Patent number: 8921359Abstract: The present invention is directed to a compound represented by the following structural formula: or a pharmaceutically acceptable salt thereof. Pharmaceutical composition comprising a compound represented by Structural Formula (I) and method of use of these compound for inhibiting BACE activity in a subject in need of such treatment are also described.Type: GrantFiled: April 22, 2013Date of Patent: December 30, 2014Assignee: Vitae Pharmaceuticals, Inc.Inventors: Lawrence W. Dillard, Jing Yuan, Lanqi Jia, Yajun Zheng
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Publication number: 20140378445Abstract: Disclosed are methods for treating Vascular Leak Syndrome. Further disclosed are methods for treating vascular leakage due to inflammatory diseases, inter alia, sepsis, lupus, inflammatory bowel disease. Yet further disclosed are methods for treating renal cell carcinoma and melanoma. Still further disclosed are methods for reducing metastasis of malignant cells and/or preventing the proliferation of carcinoma cells via spreading due to vascular leakage.Type: ApplicationFiled: December 21, 2012Publication date: December 25, 2014Inventors: Robert Shalwitz, Kevin G. Peters
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Publication number: 20140378489Abstract: The present invention provides methods and therapeutic agents for lowering serum or plasma serotonin levels in a patient in order to prevent or treat diabetes. In preferred embodiments, the patient is known to have, or to be at risk for, diabetes and the agents are TPH1 inhibitors.Type: ApplicationFiled: January 31, 2013Publication date: December 25, 2014Inventors: Gerard Karsenty, Grzegorz Sumara, Olga Sumara
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Publication number: 20140378488Abstract: Provided are derivatives substituted by urea associated with 4-substituted-(3-substituted-1H-pyrazole-5-amino)-pyrimidine-2-amino of formula (I), wherein these compounds may selectively regulate or inhibit an information transmission process controlled by natural or variant tyrosine kinase. Also provided are preparation methods and uses of the compounds.Type: ApplicationFiled: September 5, 2011Publication date: December 25, 2014Applicant: ZHEJIANG HISUN PHARMACEUTICAL CO., LTD.Inventors: Yili Ding, Xuan Yang, Qingyan Yan, Hua Bai, Lifeng Cai, Kenneth Smith, Jian Chai
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Patent number: 8916578Abstract: Pyrimidine compounds and their use in controlling pests such as insects and other invertebrates are provided. Further embodiments, forms, objects, features, advantages, aspects and benefits shall become apparent from the description.Type: GrantFiled: April 3, 2014Date of Patent: December 23, 2014Assignee: Dow AgroSciences, LLC.Inventors: Tony K. Trullinger, Timothy C. Johnson, Ricky Jim Hunter
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Publication number: 20140371205Abstract: The present invention encompasses compounds of general formula (1) wherein A, B, X, R1 to R3 are defined as in claim 1, which are suitable for the treatment of diseases characterised by excessive or abnormal cell proliferation, and their use for preparing a medicament having the above-mentioned properties.Type: ApplicationFiled: August 29, 2014Publication date: December 18, 2014Applicant: Boehringer Ingelheim International GmbHInventors: Heinz STADTMUELLER, Ioannis SAPOUNTZIS
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Publication number: 20140357616Abstract: The present invention relates to compounds of formula (I) or pharmaceutical acceptable salts, wherein R1a, R1b, R1c, X, and Y are defined in the description. The present invention relates also to compositions containing said compounds which are useful for inhibiting kinases such as Cdc7 and methods of treating diseases such as cancer.Type: ApplicationFiled: July 28, 2014Publication date: December 4, 2014Inventors: Thomas D. Penning, Keith W. Woods, Chunqiu Lai, Alan S. Florjancic, Yunsong Tong
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Publication number: 20140357629Abstract: Compounds and methods for treating diseases mediated by a P2X3 and/or a P2X2/3 receptor antagonist, the methods comprising administering to a subject in need thereof an effective amount of a compound of formula (I): or a pharmaceutically acceptable salt, solvate or prodrug thereof, wherein D, X, Y, R1, R2, R3, R4, R5, R6, R7 and R8 are as defined herein.Type: ApplicationFiled: August 6, 2014Publication date: December 4, 2014Applicant: ROCHE PALO ALTO LLCInventors: Chris Allen Broka, David Scott Carter, Michael Patrick Dillon, Ronald Charles Hawley, Alam Jahangir, Clara Jeou Jen Lin, Daniel Warren Parish
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Patent number: 8901143Abstract: A compound of the following formula: wherein R1, R2, R3, R4, R5, T, U, V, X, Y, Z, G, and Z are defined herein. It also discloses a method of treating an angiogenesis-related disorder, e.g., cancer or age-related macular degeneration, with such a compound.Type: GrantFiled: November 8, 2012Date of Patent: December 2, 2014Assignee: Hutchison MediPharma Enterprises LimitedInventors: Wei-Guo Su, Hong Jia, Weihan Zhang, Yumin Cui, Xiaoqiang Yan, Yongxin Ren, Jifeng Duan, Yang Sai
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Publication number: 20140350010Abstract: The invention relates to compounds of formula (I) as described herein, pharmaceutical preparations comprising such compounds, uses and methods of use for such compounds in the treatment of a disorder or a disease mediated by the activity of MDM2 and/or MDM4, and combinations comprising such compounds.Type: ApplicationFiled: November 28, 2012Publication date: November 27, 2014Applicant: NOVARTIS AGInventors: Pascal Furet, Vito Guagnano, Philipp Holzer, Robert Mah, Keiichi Masuya, Achim Schlapbach, Stefan Stutz, Andrea Vaupel
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Patent number: 8895573Abstract: 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 R1, Y, R2, R3, and Ra are defined herein.Type: GrantFiled: February 13, 2013Date of Patent: November 25, 2014Assignee: Janssen Pharmaceutica, NVInventors: Steven J Coats, Yue-Mei Zhang, Shu-Chen Lin, Li Liu, Tamara A Miskowski, Scott L. Dax, Henry J Breslin, Bart L. De Corte, Wei He
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Publication number: 20140343083Abstract: Pyrrolidine derivatives which are inhibitors of acetyl-CoA carboxylase(s) and their use in the treatment of obesity and type-2 diabetes. An exemplary compound is 2-(4-(1-[5-Chloro-6-(2-hydroxy-2-methyl-propoxy)-pyrimidin-4-yl]-(R)-pyrrolidin-3-yloxy)-phenyl)-N-cyclopropyl-propionamide.Type: ApplicationFiled: May 12, 2014Publication date: November 20, 2014Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Niklas HEINE, Martin FLECK, Bernd NOSSE, Gerald Juergen ROTH
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Publication number: 20140343070Abstract: A proton pump inhibitor containing a compound represented by the formula (I) wherein X and Y are the same or different and each is a bond or a spacer having 1 to 20 carbon atoms in the main chain, R1 is an optionally substituted hydrocarbon group or an optionally substituted heterocyclic group, R2, R3 and R4 are the same or different and each is a hydrogen atom, an optionally substituted hydrocarbon group, an optionally substituted thienyl group, an optionally substituted benzo[b]thienyl group, an optionally substituted furyl group, an optionally substituted pyridyl group, an optionally substituted pyrazolyl group, an optionally substituted pyrimidinyl group, an acyl group, a halogen atom, a cyano group or a nitro group, R5 and R6 are the same or different and each is a hydrogen atom or an optionally substituted hydrocarbon group, which has a superior proton pump action and shows an antiulcer activity and the like after conversion to a proton pump inhibitor in the body, or a salt thereof, or a prodrug theType: ApplicationFiled: August 1, 2014Publication date: November 20, 2014Applicant: TAKEDA PHARMACEUTICAL COMPANY LIMITEDInventors: Masahiro Kajino, Atsushi Hasuoka, Naoki Tarui, Terufumi Takagi
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Publication number: 20140343056Abstract: Herein are disclosed azaindazoles of formula (I) where the various groups are defined herein, and which are useful for treating cancer.Type: ApplicationFiled: September 12, 2012Publication date: November 20, 2014Applicant: GlaxoSmithKline LLCInventors: Joelle Lorraine Burgess, Neil W. Johnson, Steven David Knight, Louis Vincent LaFrance, III, William Henry Miller, Kenneth Allen Newlander, Stuart Paul Romeril, Meagan B. Rouse, Dominic Suarez, Xinrong Tian, Sharad Kumar Verma
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Publication number: 20140343006Abstract: This invention concerns HIV replication inhibitors of formula the N-oxides, the pharmaceutically acceptable addition salts, the quaternary amines and the stereochemically isomeric forms thereof, wherein the ring containing -a1=a2-a3=a4- and -b1=b2-b3=b4- represents phenyl, pyridyl, pyrimidinyl, pirazinyl, pyridazinyl; n is 0 to 5; m is 1 to 4; R1 is hydrogen; aryl; formyl; C1-6alkylcarbonyl; C1-6alkyl; C1-6alkyloxycarbonyl; substituted C1-6alkyl, C1-6alkylcarbonyl, C1-6alkyloxycarbonyl, C1-6alkylcarbonyloxy; substituted C1-6alkyloxyC1-6alkylcarbonyl; R2 is hydroxy, halo, optionally substituted C1-6alkyl, C3-7cycloalkyl, optionally substituted C2-6alkenyl, optionally substituted C2-6alkynyl, C1-6alkyloxy, C1-6alkyloxycarbonyl, carboxyl, cyano, nitro, amino, mono- or di(C1-6alkyl)amino, polyhalomethyl, polyhalomethyloxy, polyhalomethylthio, —S(?O)pR6, —NH—S(?O)pR6, —C(?O)R6, —NHC(?O)H, —C(?O)NHNH2, —NHC(?O)R6, —C(?NH)R6 or a 5-membered heterocycle; X1 is —NR5—, —NH—NH—, —N?N—, —O—, —C(?O)—, C1-4alkanediyl,Type: ApplicationFiled: August 5, 2014Publication date: November 20, 2014Inventors: Jerome Emile Georges Guillemont, Patrice Palandijian, Marc Rene DeJonge, Lucien Maria Henricus Koymans, Hendrik Maarten Vinkers, Frederik Frans Desire Daeyaert, Jan Heeres, Koen Jeanne Alfons Van Aken, Paulus Joannes Lewi, Frank Xavier Jozef Herwig Arts
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Publication number: 20140336208Abstract: This invention relates to compounds of the formula wherein R1 to R9 are as described below, or to pharmaceutically acceptable salts thereof. These compounds are BACE2 inhibitors and can be used as medicaments for the therapeutic and/or prophylactic treatment of diseases such as diabetes, particularly type 2 diabetes, and other metabolic disorders.Type: ApplicationFiled: July 9, 2014Publication date: November 13, 2014Inventors: David Banner, Emanuele Gabellieri, Wolfgang Guba, Hans Hilpert, Benoit Hornsperger, Roland Humm, Harald Mauser, Alexander V. Mayweg, Robert Narquizian, Emmanuel Pinard, Mark Rogers-Evans, Thomas Woltering, Wolfgang Wostl
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Publication number: 20140329799Abstract: This invention relates to aminopyrimidinone compounds of Formula (I) that are inhibitors of Interleukin receptor-associated kinases, in particular IRAK-4, and are useful in the treatment or prevention of inflammatory diseases, including rheumatoid arthritis and inflammatory bowel disease.Type: ApplicationFiled: October 26, 2012Publication date: November 6, 2014Inventors: W. Michael Seganish, Stephanie Nicole Brumfield, Jongwon Lim, Julius J. Matasi, William T. Mcelroy, Deen B. Tulshian, Brian J. Lavey, Michael D. Altman, Criag R. Gibeau, John William Lampe, Joey Methot, Liang Zhu
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Publication number: 20140329816Abstract: Certain chemical entities are provided herein. Also provided are pharmaceutical compositions comprising at least one chemical entity and one or more pharmaceutically acceptable vehicle. Methods of treating patients suffering from certain diseases and disorders responsive to the inhibition of KMO activity are described, which comprise administering to such patients an amount of at least one chemical entity effective to reduce signs or symptoms of the disease or disorder are disclosed. These diseases include neurodegenerative disorders such as Huntington's disease. Also described are methods of treatment include administering at least one chemical entity as a single active agent or administering at least one chemical entity in combination with one or more other therapeutic agents. Also provided are methods for screening compounds capable of inhibiting KMO activity.Type: ApplicationFiled: July 26, 2012Publication date: November 6, 2014Inventors: Celia Dominguez, Leticia M. Toledo-Sherman, Stephen Martin Courtney, Michael Prime, William Mitchell, Christopher John Brown, Paula C. De Aguiar Pena, Peter Johnson
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Publication number: 20140315882Abstract: The invention relates to new pyrrolidine derivatives of the formula wherein R1 to R3, Ar, L T and n are as defined in the description and claims, to their use as medicaments, to methods for their therapeutic use and to pharmaceutical compositions containing them.Type: ApplicationFiled: April 7, 2014Publication date: October 23, 2014Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Martin FLECK, Annekatrin HEIMANN, Niklas HEINE, Bernd NOSSE, Gerald Juergen ROTH
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Publication number: 20140315917Abstract: Described are compounds of Formula I which find utility in the treatment of cancer, autoimmune diseases and metabolic bone disorders through inhibition of c-FMS (CSF-1R), c-KIT, and/or PDGFR kinases. These compounds also find utility in the treatment of other mammalian diseases mediated by c-FMS, c-KIT, or PDGFR kinases.Type: ApplicationFiled: March 14, 2014Publication date: October 23, 2014Applicant: Deciphera Pharmaceuticals, LLCInventors: Daniel L. Flynn, Michael D. Kaufman, Thiwanka Samarakoon, Timothy Malcolm Caldwell, Lakshminarayana Vogeti, YuMi Ahn, William C. Patt, Karen M. Yates
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Patent number: 8859591Abstract: The present invention provides a compound of Formula (I) or a pharmaceutically acceptable salt thereof wherein R1, R2, R3, A1, A2, A3, A4, L, 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 3, 2013Date of Patent: October 14, 2014Assignee: Pfizer Inc.Inventors: Gary Erik Aspnes, Mary Theresa Didiuk, Kevin James Filipski, Angel Guzman-Perez, Esther Cheng Yin Lee, Jeffrey Allen Pfefferkorn, Benjamin Dawson Stevens, Meihua Mike Tu
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Patent number: 8859529Abstract: This invention relates to compounds of the Formula (I) as described herein, or a pharmaceutically acceptable salt, solvate or ester thereof, which can be useful for the treatment of diseases or conditions mediated by MMPs, ADAMs, TACE, aggrecanase, TNF- or combinations thereof.Type: GrantFiled: September 22, 2009Date of Patent: October 14, 2014Assignee: Merck Sharp & Dohme Corp.Inventors: Bandarpalle B. Shankar, Seong Heon Kim, Wensheng Yu, Ling Tong, Michael K. C. Wong, Brian J. Lavey, Joseph A. Kozlowski, Lei Chen, Razia K. Rizvi, Aneta Maria Kosinski, De-Yi Yang, Guowei Zhou, Kristen E. Rosner, Luke Fire, Judson E. Richard, Dansu Li
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Publication number: 20140303198Abstract: Provided is an agent for treating and/or preventing obesity. An agent for suppressing expression of NPC1L1 (Niemann-Pick disease, type C1, gene-like 1) and/or LIPG (Lipase, endothelial) mRNA, and an agent for preventing and/or treating obesity, each comprising, as an active ingredient, a compound having CETP inhibitory activity, or a salt thereof, or a solvate thereof.Type: ApplicationFiled: November 28, 2012Publication date: October 9, 2014Applicant: KOWA COMPANY, LTD.Inventors: Takeshi Murakami, Kentaro Murakami, Tadaaki Ohgiya, Kimiyuki Shibuya
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Publication number: 20140303197Abstract: The present invention relates to preventing and treating leukemia and other cancers of the blood and bone, as well as disorders of the blood, by inhibiting gut-derived serotonin. The inhibition of the gut-derived serotonin is accomplished by inhibiting Tph1, an enzyme responsible for the production of gut-derived serotonin. The present invention also relates to preventing and treating leukemia and other cancers of the blood and bone, as well as disorders of the blood, by increasing the number, growth and proliferation of osteoblasts.Type: ApplicationFiled: November 16, 2012Publication date: October 9, 2014Applicant: The Trustees of Columbia University in the City of New YorkInventor: Stavroula Kousteni
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Patent number: 8853228Abstract: The compositions and methods described herein disclose the design, synthesis and testing of compounds that act as inhibitors of DHFR. The basic scaffold of these inhibitors includes a 2,4-diaminopyrimidine ring with a propargyl linker to another substituted aryl, bicyclo or heteroaryl ring. These DHFR inhibitors are potent and selective for many different pathogenic organisms, including the DHFR enzyme from bacteria such as Bacillus anthracis and methicillin-resistant Staphylococcus aureus, fungi such as Candida glabrata, Candida albicans and Cryptococcus neoformans and protozoa such as Cryptosporidium hominis and Toxoplasma gondii. These compounds and other similar compounds are also potent against the mammalian enzyme and may be useful as anti-cancer therapeutics.Type: GrantFiled: November 7, 2011Date of Patent: October 7, 2014Assignee: University of ConnecticutInventors: Amy C. Anderson, Dennis L. Wright, Kathleen Mary Frey, Janet Leigh Paulsen, Eric William Scocchera, Kishore Viswanathan
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Publication number: 20140296208Abstract: There are provided compounds of formula I, wherein R1A to R1E, R2 to R5, L and X1 to X3 have meanings given in the description, which compounds have antiinflammatory activity (e.g. through inhibition of one or more of members of: the family of p38 mitogen-activated protein kinase enzymes; Syk kinase; and members of the Src family of tyrosine kinases) and have use in therapy, including in pharmaceutical combinations, especially in the treatment of inflammatory diseases, including inflammatory diseases of the lung, eye and intestines.Type: ApplicationFiled: April 1, 2014Publication date: October 2, 2014Applicants: Topivert Pharma Limited, Respivert LimitedInventors: Thomas Matthew BAKER, Matthew Colin Thor FYFE, Gareth William HARBOTTLE, Vedran HASIMBEGOVIC, Premji MEGHANI, Aaron RIGBY, Colin SAMBROOK-SMITH, Stephen Malcolm THOM
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Publication number: 20140296271Abstract: There is provided a compound of formula I, which compound has antiinflammatory activity (e.g. through inhibition of one or more of members of: the family of p38 mitogen-activated protein kinase enzymes; Syk kinase; and members of the Src family of tyrosine kinases, e.g., Src and Lck) and has use in therapy, including in pharmaceutical combinations, especially in the treatment of inflammatory diseases, including inflammatory diseases of the lung, eye and intestines.Type: ApplicationFiled: April 1, 2014Publication date: October 2, 2014Applicants: Topivert Pharma Limited, Respivert LimitedInventor: Matthew Colin Thor FYFE
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Patent number: 8846704Abstract: The present invention relates to thiopyrimidine-based compounds that are inhibitors of protein kinases including JAK kinases. In particular, the compounds are selective for JAK1, JAK2 or JAK3 kinases and combinations thereof such as JAK1 and JAK2. The kinase inhibitors can be used in the treatment of kinase associated diseases such as immunological and inflammatory diseases including organ transplants; hyperproliferative diseases including cancer and myeloproliferative diseases; viral diseases; metabolic diseases and vascular diseases.Type: GrantFiled: January 31, 2008Date of Patent: September 30, 2014Assignee: YM Biosciences Austraila Pty LtdInventors: David Gerard Bourke, Xianyong Bu, Christopher John Burns, Anthony Nicholas Cuzzupe, John Thomas Feutrill, Tracy Leah Nero, Beata Maria Blannin, Jun Zeng, Shaun Patrick Gaynor
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Publication number: 20140288017Abstract: The present invention is directed to novel catechol diether compounds, pharmaceutical compositions therefrom and methods for inhibiting reverse transcriptase and treating HIV infections, especially included drug resistant strains of HIV 1 and 2 and/or secondary disease states and/or conditions which occur as a consequence of HIV infection.Type: ApplicationFiled: October 12, 2012Publication date: September 25, 2014Inventors: William L. Jorgensen, Karen S. Anderson
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Publication number: 20140288065Abstract: The present invention provides a pyrrolidine compound of General Formula (1) or a salt thereof, wherein R101 and R102 are each independently a phenyl group or a pyridyl group, the phenyl group or the pyridyl group may have one or more substituents selected from halogen atoms and lower alkyl groups optionally substituted with one or more halogen atoms, etc. The pyrrolidine compound or a salt thereof of the present invention is usable to produce a pharmaceutical preparation having a wider therapeutic spectrum and being capable of exhibiting sufficient therapeutic effects after short-term administration.Type: ApplicationFiled: June 10, 2014Publication date: September 25, 2014Applicant: OTSUKA PHARMACEUTICAL CO., LTD.Inventors: Muneaki KURIMURA, Shinichi TAIRA, Takahiro TOMOYASU, Nobuaki ITO, Kuninori TAI, Noriaki TAKEMURA, Takayuki MATSUZAKI, Yasuhiro MENJO, Shin MIYAMURA, Yohji SAKURAI, Akihito WATANABE, Yasuyo SAKATA, Takumi MASUMOTO, Kohei AKAZAWA, Haruhiko SUGINO, Naoki AMADA, Satoshi OHASHI, Tomoichi SHINOHARA, Hirofumi SASAKI, Chisako MORITA, Junko YAMASHITA, Satoko NAKAJIMA
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Patent number: 8841301Abstract: The disclosure generally relates to compounds of formula I, including their salts, as well as compositions and methods of using the compounds. The compounds are ligands, antagonists of the NR2B receptor and may be useful for the treatment of various disorders of the central nervous system.Type: GrantFiled: September 24, 2012Date of Patent: September 23, 2014Assignee: Bristol-Myers Squibb CompanyInventors: Dalton King, John E. Macor, Richard E. Olson, Christiana I. Iwuagwu, George N. Karageorge
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Publication number: 20140275085Abstract: Described are compounds of Formula I which find utility in the treatment of cancer, autoimmune diseases and metabolic bone disorders through inhibition of c-FMS (CSF-1R), c-KIT, and/or PDGFR kinases. These compounds also find utility in the treatment of other mammalian diseases mediated by c-FMS, c-KIT, or PDGFR kinases.Type: ApplicationFiled: March 14, 2014Publication date: September 18, 2014Applicant: Deciphera Pharmaceuticals, LLCInventors: Michael D. Kaufman, Daniel L. Flynn, YuMi Ahn, Lakshminarayana Vogeti, Timothy Malcolm Caldwell
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Publication number: 20140275088Abstract: In one aspect, the present invention relates to a method of identifying compounds useful in modifying the activity of Aldolase.Type: ApplicationFiled: October 25, 2012Publication date: September 18, 2014Inventors: Timothy J. Cardozo, Jürgen Bosch, Sondra Maureen Nemetski
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Publication number: 20140256756Abstract: Compounds of Formula (I) and pharmaceutically acceptable salts thereof in which X1, X2, X3, L, R3, R4, R5, R7 and n have the meanings given in the specification, are modulators of GPR119 and are useful in the treatment or prevention of diseases such as, but not limited to, type 2 diabetes, diabetic complications, symptoms of diabetes, metabolic syndrome, obesity, dyslipidemia, and related conditions.Type: ApplicationFiled: October 30, 2012Publication date: September 11, 2014Inventors: Thomas Daniel Aicher, Josef Roland Benscik, Steven Armen Boyd, Kevin Ronald Condroski, Jay Bradford Fell, John Peter Fischer, Ronald Jay Hinklin, Scott Pratt, Ajay Singh, Timothy M. Turner
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Publication number: 20140249169Abstract: There is provided a compound of formula (I) which is an inhibitor of the family of p38 mitogen-activated protein kinase enzymes, and to its use in therapy, including in pharmaceutical combinations, especially in the treatment of inflammatory diseases, including inflammatory diseases of the lung, such as asthma and COPD.Type: ApplicationFiled: October 3, 2012Publication date: September 4, 2014Inventors: Kazuhiro Ito, Catherine Elisabeth Charron, John King-Underwood, Stuart Thomas Onions, Alistair Ian Longshaw, Rudy Broeckx, Walter Filliers, Alex Copmans
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Patent number: 8822446Abstract: The present invention relates to compounds of formula (I) or pharmaceutical acceptable salts, wherein R1a, R1b, R1c, X, and Y are defined in the description. The present invention relates also to compositions containing said compounds which are useful for inhibiting kinases such as Cdc7 and methods of treating diseases such as cancer.Type: GrantFiled: April 14, 2011Date of Patent: September 2, 2014Assignee: AbbVie Inc.Inventors: Thomas D. Penning, Keith W. Woods, Chunqiu Lai, Yunsong Tong, Alan S. Florjancic
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Patent number: 8815883Abstract: Compounds having the structures below that are TPH1 inhibitors are provided: The compounds are useful of, e.g., to increase bone mass. In preferred embodiments, the patient is known to have, or to be at risk for, a low bone mass disease such as osteoporosis.Type: GrantFiled: November 2, 2010Date of Patent: August 26, 2014Assignee: The Trustees of Columbia Unviersity in the City of New YorkInventors: Donald Landry, Shi-Xian Deng