Nitrogen Bonded Directly To The 1,3-diazine At 2-position Patents (Class 514/272)
  • Patent number: 11370793
    Abstract: Pharmaceutical compounds, compositions, methods, and uses therefor are presented using selected triazolopyridines and triazolopyrimidines to inhibit or reduce phosphorylation of tau proteins or that act as antagonists of corticotropin-releasing factor. Viewed from another perspective, compounds, compositions, and methods are presented for treating or preventing symptoms of Alzheimer's disease by inhibiting or reducing the phosphorylation of tau proteins.
    Type: Grant
    Filed: August 29, 2016
    Date of Patent: June 28, 2022
    Assignee: NantNeuro, LLC
    Inventors: Varghese John, Oleksandr Buzko, Dale Bredesen, Patricia Spilman, Barbara Jagodzinska
  • Patent number: 11103507
    Abstract: Described herein are methods of treating cancers and other tumors related to the decreased proliferation, the depletion, or the repolarization of tumor-associated macrophages (TAMs) and treatment of associated disorders, including tenosynovial giant cell tumor (TGCT) and diffuse-type tenosynovial giant cell tumor (DTGCT).
    Type: Grant
    Filed: December 23, 2019
    Date of Patent: August 31, 2021
    Assignee: Deciphera Pharmaceuticals, LLC
    Inventors: Daniel L. Flynn, Bryan D. Smith, Rodrigo Ruiz Soto, Keisuke Kuida
  • Patent number: 11096923
    Abstract: The present invention features an antibacterial composition comprising 1) a composition A comprising polymyxin B and trimethoprim; and 2) an antibiotic agent selected from the group consisting of rifampicin, rifabutin, rifapentine, rifaximin, pefloxacin mesylate, sparfloxacin, sarafloxacin HCl, tobramycin, lomefloxacin, besifloxacin, danofloxacin mesylate, enrofloxacin, nadifloxacin and clinafloxacin, a topical pharmaceutical thereof, and a method of treating bacterial infections using mixtures of 1 and 2.
    Type: Grant
    Filed: August 16, 2017
    Date of Patent: August 24, 2021
    Assignee: University of Rochester
    Inventors: Paul M. Dunman, Rachel Wozniak
  • Patent number: 10752609
    Abstract: The disclosure generally relates to compounds of formula I, including their salts, as well as compositions and methods of using the compounds to treat disorders associated with GSK-3.
    Type: Grant
    Filed: November 27, 2017
    Date of Patent: August 25, 2020
    Assignee: Bristol-Myers Squibb Company
    Inventors: Richard A. Hartz, Vijay T. Ahuja, Guanglin Luo, Ling Chen, Prasanna Sivaprakasam, Gene M. Dubowchik, Swanee E. Jacutin-Porte, John E. Macor
  • Patent number: 10736692
    Abstract: Methods for treating a human patient diagnosed with cancer with therapeutic neuromodulation and associated systems are disclosed herein. Sympathetic nerve activity can contribute to several cellular and physiological processes associated with the progression of cancer. One aspect of the present technology is directed to methods that attenuate neural traffic along target sympathetic nerves innervating tissue proximate a primary malignant tumor. Other aspects are directed to methods that at least partially inhibit sympathetic neural activity in a renal nerve of a patient diagnosed with cancer or who has a high risk of developing cancer. Targeted sympathetic nerve activity can be attenuated to improve a measurable physiological parameter corresponding to the progression of cancer in the patient. The attenuation can be achieved, for example, using an intravascularly positioned catheter carrying a therapeutic assembly, e.g.
    Type: Grant
    Filed: June 27, 2016
    Date of Patent: August 11, 2020
    Assignee: MEDTRONIC ARDIAN LUXEMBOURG S.A.R.L.
    Inventors: Garrett Pilcher, Robert Melder
  • Patent number: 10676444
    Abstract: Provided are novel salts and polymorphs of 5-(2,4-diamino-pyrimidin-5-yloxy)-4-isopropyl-2-methoxy-benzenesulfonamide, which are potentially useful for modulating a condition mediated by a P2X3 or P2X2/3 receptor. Also provided are pharmaceutical formulations and methods of administration and dosing of these salts and polymorphs to subjects in need thereof.
    Type: Grant
    Filed: December 15, 2017
    Date of Patent: June 9, 2020
    Assignee: Afferent Pharmaceuticals, Inc.
    Inventors: Prabha Ibrahim, Ronald Charles Hawley, Anthony P. Ford, Steven A. Smith
  • Patent number: 10543211
    Abstract: Provided herein include methods and compositions for treating diseases or conditions. In some embodiments provided are methods for treating one or more diseases or conditions selected from the group consisting of hypertension, heart failure, dyspnea, and sleep apnea. In certain embodiments provided are methods that include administering a compound of formula (I) as disclosed herein. In some embodiments provided are methods that include administering a P2X3 and/or a P2X2/3 receptor antagonist.
    Type: Grant
    Filed: December 6, 2018
    Date of Patent: January 28, 2020
    Assignee: Afferent Pharmaceuticals, Inc.
    Inventors: Anthony P. Ford, Julian Paton
  • Patent number: 10513509
    Abstract: Disclosed herein are nitrogen-containing bicyclic compounds, together with pharmaceutical compositions and methods of ameliorating and/or treating a cancer described herein with one or more of the compounds described herein.
    Type: Grant
    Filed: May 24, 2017
    Date of Patent: December 24, 2019
    Assignee: Recurium IP Holdings, LLC
    Inventors: Kevin Duane Bunker, Peter Qinhua Huang, Sunny Abraham, Joseph Robert Pinchman, Chad Daniel Hopkins, Deborah Helen Slee
  • Patent number: 10376512
    Abstract: The disclosure relates to a crystal of an aniline pyrimidine compound of trifluoroethyl substituted indole and a salt thereof as an EGFR inhibitor, specifically relates to a crystal of a compound represented by formula I, a crystal of monomethyl sulfonate of the compound represented by formula I or a crystal of dimethyl sulfonate of the compound represented by formula I, and further relates to a method for preparing the crystal, a crystalline composition comprising the crystal, or a pharmaceutical composition comprising the crystal or a crystalline composition thereof, and a medical use thereof.
    Type: Grant
    Filed: August 9, 2018
    Date of Patent: August 13, 2019
    Assignee: CHIA TAI TIANQING PHARMAEUTICAL GROUP CO., LTD.
    Inventors: Lulu Wang, Jianqiu Tang, Yizhong Zhu, Fei Liu, Yan Zhu, Chuanyu Zhang, Limin Yang
  • Patent number: 10280156
    Abstract: The present invention relates to heteroaromatic chalcone derivatives, particularly the compounds of formula (I) as described and defined herein, pharmaceutical compositions comprising these compounds, and their medical use, including their use in the treatment or prevention of cancer and, in particular, in the treatment or prevention of hematologic malignancies.
    Type: Grant
    Filed: August 28, 2015
    Date of Patent: May 7, 2019
    Assignees: Medizinische Universität Wien, Universität Wien
    Inventors: Katrina Vanura, Ulrich Jäger, Thomas Erker, Gerda Brunhofer-Bolzer
  • Patent number: 10189824
    Abstract: Provided are novel compounds of Formula (I): pharmaceutically acceptable salts thereof, and pharmaceutical composition thereof, which are useful as dual Hsp90/TRAP1 inhibitors. Also provided are pharmaceutical compositions comprising the novel compounds of Formula (I) and their use in treating one or more cancers.
    Type: Grant
    Filed: September 11, 2015
    Date of Patent: January 29, 2019
    Assignee: Calasia Pharmaceuticals, Inc.
    Inventors: Srinivasa Reddy Natala, Sridhar G. Prasad
  • Patent number: 9968592
    Abstract: This invention provides a combination-drug composition and a combination use of pharmaceuticals for preventing and/or treating dyslipidemic conditions such as hyper-LDL cholesterolemia in mammals, including humans. This invention pertains to a drug composition for preventing and/or treating dyslipidemia and the like, the drug composition including the following: (R)-2-[3-[[N-(benzoxazol-2-yl)-N-3-(4-methoxyphenoxy)propyl]aminomethyl]phenoxy] butyric acid, a salt thereof, or a solvate of either; and (S)-trans-{4-[({2-[({1-[3,5-bis(trifluoromethyl)phenyl]ethyl}{5-[2-(methyl sulfonyl)ethoxy]pyrimidin-2-yl}amino)methyl]-4-(trifluoromethyl)phenyl}(ethyl)amino)methyl]cyclohexyl} acetic acid, a salt thereof, or a solvate of either.
    Type: Grant
    Filed: September 28, 2015
    Date of Patent: May 15, 2018
    Assignee: KOWA COMPANY, LTD.
    Inventors: Yuta Inokuchi, Haruki Shibata, Toshiaki Takizawa
  • Patent number: 9907795
    Abstract: This invention relates to the new use of the compound 2-(R)-(4-Fluoro-2-methyl-phenyl)-4-(S)-((8aS)-6-oxo-hexahydro-pyrrolo[1,2-?]-pyrazin-2-yl)-piperidine-1-carboxylic acid [1-(R)-(3,5-bis-trifluoromethyl-phenyl)-ethyl]-methylamide (orvepitant) or pharmaceutically acceptable salts thereof and pharmaceutical compositions containing it and one or more therapeutic agents for the treatment of chronic cough, including chronic refractory cough and to combinations for such a use.
    Type: Grant
    Filed: August 2, 2017
    Date of Patent: March 6, 2018
    Assignee: NeRRe Therapeutics Limited
    Inventor: Mike Trower
  • Patent number: 9901591
    Abstract: Disclosed are methods and preparations useful for reducing fat at a targeted area(s) on a human. The preparations comprise as an active ingredient an adipolysis enhancing (i.e., fat-melting) amount of an active ingredient, paeoniflorin (PF). The preparations may be provided as an injectable preparation or as a topically applied preparation, such as in the form of a crème or lotion. In topical preparations, the active ingredient paeoniflorin may be contained within nanospheres, such as albumin nanospheres. The PF-containing preparations may also include a permeant, such as azone. The method may be accompanied by the application of ultrasound to the area being treated prior to, during or after, or prior to, during, and after application of the paeoniflorin preparation to an area of the body in which fat reduction is desired.
    Type: Grant
    Filed: July 10, 2013
    Date of Patent: February 27, 2018
    Inventor: Bakr Rabie
  • Patent number: 9883909
    Abstract: Methods for treating hyperaldosteronism with therapeutic renal neuromodulation and associated systems and methods are disclosed herein. One aspect of the present technology, for example, is directed to methods that at least partially inhibit sympathetic neural activity in renal nerves proximate a renal blood vessel of a human patient. One or more measurable physiological parameters corresponding to hyperaldosteronism of the patient can thereby be improved. Moreover, central sympathetic drive in the patient can be reduced in a manner that treats the patient for hyperaldosteronism. Renal sympathetic nerve activity can be modulated along the afferent and/or efferent pathway. The modulation can be achieved, for example, using an intravascularly positioned catheter carrying a neuromodulation assembly, e.g., a neuromodulation assembly configured to use electrically-induced, thermally-induced, and/or chemically-induced approaches to modulate the renal nerve.
    Type: Grant
    Filed: March 7, 2013
    Date of Patent: February 6, 2018
    Assignee: Medtronic Ardian Luxembourg S.a.r.l.
    Inventor: Gabriel Brennan
  • Patent number: 9580439
    Abstract: The invention provides inhibitors of focal adhesion kinase, an enzyme involved in the attachment of the cytoskeleton of a cell to an extracellular matrix, which has been implicated in processes such as cell migration, cell proliferation, and cell survival. The inhibitors are derivatives of a 5-substituted 2,4-diaminopyridine wherein the substituents are as defined herein. The invention also provides a method of using the inhibitors in treatment of cancer, and methods of preparation of the inhibitors by use of coupling reactions.
    Type: Grant
    Filed: June 19, 2013
    Date of Patent: February 28, 2017
    Assignee: The Scripps Research Institute
    Inventors: Congxin Liang, Marcel Koenig, Yuanjun He, Par Holmberg
  • Patent number: 9481648
    Abstract: 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: Grant
    Filed: April 1, 2014
    Date of Patent: November 1, 2016
    Assignees: Respivert Limited, Topivert Pharma Limited
    Inventors: Thomas Matthew Baker, Matthew Colin Thor Fyfe, Gareth William Harbottle, Vedran Hasimbegovic, Premji Meghani, Aaron Rigby, Colin Sambrook-Smith, Stephen Malcolm Thom
  • Patent number: 9422250
    Abstract: This invention relates to pyrimidine derivatives, processes for their preparation, pharmaceutical compositions, and their use in treating viral infections such as HCV or HBV.
    Type: Grant
    Filed: April 10, 2012
    Date of Patent: August 23, 2016
    Assignee: Janssen Sciences Ireland UC
    Inventors: David Mc Gowan, Pierre Jean-Marie Bernard Raboisson, Werner Embrechts, Tim Hugo Maria Jonckers, Stefaan Julien Last, Serge Maria Aloysius Pieters, Jaromir Vlach
  • Patent number: 9409887
    Abstract: The present invention provides compounds, pharmaceutically acceptable compositions thereof, and methods of using the same.
    Type: Grant
    Filed: July 31, 2014
    Date of Patent: August 9, 2016
    Assignee: Celgene Avilomics Research, Inc.
    Inventors: Kwangho Lee, Deqiang Niu, Matthew F. Baevsky
  • Patent number: 9259399
    Abstract: The invention involves methods of inhibiting the cancer cell cycle to make cancer cells more susceptible to chemotherapeutic agents. In particular, inhibition of CDK4 and/or CDK6 inhibits cell cycle progression in cancer cells. When combined with chemotherapy such cell cycle inhibition can effectively treat even aggressive cancer types that are drug-resistant and intractable to most chemotherapies.
    Type: Grant
    Filed: October 1, 2008
    Date of Patent: February 16, 2016
    Assignee: Cornell University
    Inventors: Selina Chen-Kiang, Maurizio Di Liberto, Xiangao Huang
  • Patent number: 9238629
    Abstract: The present invention provides compounds, pharmaceutically acceptable compositions thereof, and methods of using the same.
    Type: Grant
    Filed: October 31, 2011
    Date of Patent: January 19, 2016
    Assignee: Celgene Avilomics Research, Inc.
    Inventors: Kwangho Lee, Deqiang Niu, Russell C. Petter, Juswinder Singh
  • Patent number: 9212186
    Abstract: Compounds of formula I: or pharmaceutically acceptable salts thereof, wherein X, R1, R2, R3 and A are as defined herein. Also disclosed are methods of making the compounds and using the compounds for treatment of diseases associated with LRRK2 receptor, such as Parkinson's disease.
    Type: Grant
    Filed: November 3, 2014
    Date of Patent: December 15, 2015
    Assignee: Genentech, Inc.
    Inventors: Charles Baker-Glenn, Bryan K. Chan, Jennafer Dotson, Anthony Estrada, Timothy Heffron, Joseph Lyssikatos, Zachary Sweeney
  • Patent number: 9179671
    Abstract: The present invention provides a composition having an excellent controlling activity on a pest. The composition comprising a compound represented by Formula (1) and the cyanamide compound represented by Formula (2) shows an excellent controlling activity on a pest.
    Type: Grant
    Filed: October 13, 2011
    Date of Patent: November 10, 2015
    Assignee: SUMITOMO CHEMICAL COMPANY, LIMITED
    Inventors: So Kiguchi, Soichi Tanaka
  • Patent number: 9150521
    Abstract: 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: Grant
    Filed: January 31, 2013
    Date of Patent: October 6, 2015
    Assignee: The Trustees of Columbia University in the City of New York
    Inventors: Gerard Karsenty, Grzegorz Sumara, Olga Sumara
  • Publication number: 20150148358
    Abstract: The present invention provides compounds of the Formula below: where R is H or —CH3; methods of treating patients for hypertriglyceridemia and cardiovascular disease including dyslipidemia and atherosclerosis, and processes for preparing the compounds.
    Type: Application
    Filed: November 19, 2014
    Publication date: May 28, 2015
    Applicant: Eli Lilly and Company
    Inventors: Manisha NAIK, Nicholas Paul CAMP
  • Publication number: 20150148327
    Abstract: The invention provides certain substituted pyridines of the Formula (I) or pharmaceutically acceptable salts thereof, wherein R1, R2, R3, R4, Rcy, Cy, and t 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: Application
    Filed: June 17, 2013
    Publication date: May 28, 2015
    Applicant: Merck Canada Inc.
    Inventors: Andrew M. Haidle, Sandra Lee Knowles, Solomon D. Kattar, Denis Deschenes, Jason Burch, Joel Robichaud, Matthew Christopher, Michael D. Altman, James P. Jewell, Alan B. Northrup, Marc Blouin, John Michael Ellis, Hua Zhou, Christian Fischer, Adam J. Schell, Michael H. Reutershan, Brandon M. Taoka, Anthony Donofrio, Joel Robichaud
  • Patent number: 9040549
    Abstract: 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: Grant
    Filed: April 11, 2013
    Date of Patent: May 26, 2015
    Assignee: YM Biosciences Australia Pty Ltd.
    Inventors: 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
  • Publication number: 20150141446
    Abstract: 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: Application
    Filed: November 19, 2014
    Publication date: May 21, 2015
    Inventors: Tony K. Trullinger, Timothy C. Johnson, Ricky Jim Hunter
  • Publication number: 20150141427
    Abstract: The present invention relates to compounds of formula I: in which Y, Y1, Y4, Y5, Y6, R1, R2, R3 and R4 are defined in the Summary of the Invention; capable of inhibiting the activity of BCR-ABL1 and mutants thereof. The invention further provides a process for the preparation of compounds of the invention, pharmaceutical preparations comprising such compounds and methods of using such compounds in the treatment of cancers.
    Type: Application
    Filed: May 9, 2013
    Publication date: May 21, 2015
    Applicant: Novartis AG
    Inventors: Pascal Furet, Robert Martin Grotzfeld, Wolfgang Jahnke, Darryl Brynley Jones, Paul William Manley, Andreas Marzinzik, Saliha Moussaoui, Xavier Francois Andre Pelle, Bahaa Salem, Joseph Schoepfer
  • Publication number: 20150132258
    Abstract: Provided herein are compounds useful for the treatment of HBV infection in a subject in need thereof, pharmaceutical compositions thereof, and methods of inhibiting, suppressing, or preventing HBV infection in the subject.
    Type: Application
    Filed: November 14, 2014
    Publication date: May 14, 2015
    Inventor: George D. Hartman
  • Publication number: 20150133457
    Abstract: The present invention relates to pharmaceutical compounds, compositions and methods, especially as they are related to compositions and methods for the treatment and/or prevention of a proliferation disorder, a cancer, a tumor, an inflammatory disease, an autoimmune disease, psoriasis, dry eye or an immunologically related disease, and in some embodiments diseases or disorders related to the dysregulation of kinase such as, but not limited to, EGFR (including HER), Alk, PDGFR, BLK, BMX/ETK, FLT3(D835Y), ITK, TEC, TXK, BTK, or JAK, and the respective pathways.
    Type: Application
    Filed: July 11, 2014
    Publication date: May 14, 2015
    Inventors: Xiao XU, Xiaobo WANG, Long MAO, Li ZHAO, Biao XI
  • Publication number: 20150126473
    Abstract: The present disclosure provides an isolated particle comprising very high density, ultra small, lipid depleted apo B containing particles, and may also contain cytokeratin 8. The isolated particle is useful in diagnostic assays, which are also provided.
    Type: Application
    Filed: June 14, 2012
    Publication date: May 7, 2015
    Applicant: Children's Hospital & Research Center at Oakland
    Inventors: Ronald M. Krauss, Mohmed Elfatih Ashmaig
  • Patent number: 9018218
    Abstract: The invention relates to substituted pyrimidine ammonia compounds. The structure of the compounds is represented as the general formula (I): The groups are as defined as specification. The compound represented by formula (I) can be used in the prevention of plants diseases caused by a plurality of pathogenic bacteria such as oomycota, basidiomycota, ascomycota, and fungi imperfecti, and due to these compounds have good bioactivity, which make them have very good effects at very low doses, especially more effective to powdery mildew of wheat. Therefore, the present invention relates to the use of the compounds having general formula I as fungicides, both in agriculture and other fields.
    Type: Grant
    Filed: November 18, 2011
    Date of Patent: April 28, 2015
    Assignees: Sinochem Corporation, Shenyang Research Institute of Chemical Industry Co., Ltd.
    Inventors: Changling Liu, Baoshan Chai, Zhinian Li, Xufeng Sun, Zhonggang Shan
  • Publication number: 20150110809
    Abstract: Embodiments of the invention are directed to compounds that inhibit an activity of EP AC proteins and methods of using the same. The inventors have developed a sensitive and robust high throughput screening (HTS) assay for the purpose of identifying EPAC specific inhibitors (Tsalkova et al. (2012) PLOS ONE 7 (1):e30441).
    Type: Application
    Filed: February 8, 2013
    Publication date: April 23, 2015
    Applicant: The Board of Regents of the University of Texas System
    Inventors: Xiaodong Cheng, Jia Zhou, Tamara Tsalkova, Fang Mei, Haijun Chen
  • Publication number: 20150111908
    Abstract: The present invention provides methods and therapeutic agents for lowering or increasing serum serotonin levels in a patient in order to increase or decrease bone mass, respectively. In preferred embodiments, the patient is known to have, or to be at risk for, a low bone mass disease such as osteoporosis and the agents are TPH1 inhibitors or serotonin receptor antagonists.
    Type: Application
    Filed: May 20, 2014
    Publication date: April 23, 2015
    Inventors: Gerard Karsenty, Patricia F. Ducy, Yuli Xie, Donald Landry, Vijay Yadav
  • Publication number: 20150099756
    Abstract: The present invention relates to novel compounds that inhibit Lp-PLA2 activity, processes for their preparation, to compositions containing them and to their use in the treatment of diseases associated with the activity of Lp-PLA2, for example atherosclerosis, Alzheimer's disease, and/or diabetic macular edema.
    Type: Application
    Filed: December 15, 2014
    Publication date: April 9, 2015
    Inventors: Yun JIN, Zehong WAN, Qing ZHANG
  • Patent number: 8987250
    Abstract: Compounds disclosed herein including compounds of formula I?: and salts thereof are provided. Pharmaceutical compositions comprising compounds disclosed herein, processes for preparing compounds disclosed herein, intermediates useful for preparing compounds disclosed herein and therapeutic methods for treating an HIV infection using compounds disclosed herein are also provided.
    Type: Grant
    Filed: April 19, 2013
    Date of Patent: March 24, 2015
    Assignee: Gilead Sciences, Inc.
    Inventors: Kerim Babaoglu, Gediminas Brizgys, Jake Cha, Xiaowu Chen, Hongyan Guo, Randall L. Halcomb, Xiaochun Han, Richard Huang, Hongtao Liu, Ryan McFadden, Michael L. Mitchell, Yingmei Qi, Paul A. Roethle, Lianhong Xu, Hong Yang
  • Patent number: 8987251
    Abstract: Provided herein is a method of treating a PIM-1 and/or PIM-2 and/or PIM-3 kinase-mediated condition in a mammal, which comprises administering to said mammal a therapeutically effective amount of a compound of Formula I: in which A, B, R1, R1a, R2, R3, R4, R5, R6, and R7 have the meanings given in the specification.
    Type: Grant
    Filed: October 18, 2013
    Date of Patent: March 24, 2015
    Assignee: Array BioPharma Inc.
    Inventors: Shelley Allen, Laura L. Celeste, T. Gregg Davis, Robert Kirk DeLisle, Julie Marie Hicks, Stefan D. Gross, Erik James Hicken, Leila J. Jackson, Nicholas C. Kallan, Joseph P. Lyssikatos, Fredrik P. Marmsater, Mark C. Munson, Jed Pheneger, Bryson Rast, John E. Robinson, Stephen T. Schlachter, George T. Topalov, A. Dale Wright, Qian Zhao
  • Publication number: 20150080393
    Abstract: The present invention is directed to spirocyclic compounds which are inhibitors of tryptophan hydroxylase (TPH), particularly isoform 1 (TPH1), that are useful in the treatment of diseases or disorders associated with peripheral serotonin including, for example, gastrointestinal, cardiovascular, pulmonary, inflammatory, metabolic, and low bone mass diseases, as well as serotonin syndrome, and cancer.
    Type: Application
    Filed: September 5, 2014
    Publication date: March 19, 2015
    Inventors: Stéphane De Lombaert, Daniel R. Goldberg, Kenneth Brameld, Eric Brian Sjogren, Andrew Scribner
  • Publication number: 20150079154
    Abstract: The invention provides a pharmaceutical composition comprising Sorafenib in combination with an inhibitor of a specific kinase inhibitor as a medicament for the treatment or prevention of liver cancer.
    Type: Application
    Filed: July 9, 2012
    Publication date: March 19, 2015
    Applicant: HELMHOLTZ-ZENTRUM FUER INFEKTIONSFORSCHUNG GMBH
    Inventors: Lars Zender, Ramona Rudalska, Daniel Dauch
  • Publication number: 20150065530
    Abstract: The present invention provides compositions and methods for characterizing irritable bowel syndrome. In particular, the present invention provides compositions and methods for determining polymorphisms associated with IBS-D and Crohn's disease. The present invention further provides compositions and methods for determining a treatment course of action in subjects with IBS-D and Crohn's disease.
    Type: Application
    Filed: April 3, 2013
    Publication date: March 5, 2015
    Applicant: THE REGENTS OF THE UNIVERSITY OF MICHIGAN
    Inventors: Juanita L. Merchant, Helmut Grasberger
  • Patent number: 8969341
    Abstract: 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: Grant
    Filed: November 28, 2012
    Date of Patent: March 3, 2015
    Assignee: Novartis AG
    Inventors: Pascal Furet, Vito Guagnano, Philipp Holzer, Robert Mah, Keiichi Masuya, Achim Schlapbach, Stefan Stutz, Andrea Vaupel
  • Patent number: 8969336
    Abstract: Provided is a compound useful as an inhibitor against the kinase activity of EML4-ALK fusion protein. As a result of intensive and extensive studies on compounds having inhibitory activity against the kinase activity of EML4-ALK fusion protein, the present inventors found that the diamino heterocyclic carboxamide compounds of the present invention had inhibitory activity against the kinase activity of EML4-ALK fusion protein. By this finding, the present invention was completed. The compounds of the present invention can be used as a pharmaceutical composition for preventing and/or treating cancer, such as lung cancer, non-small cell lung cancer, and small cell lung cancer.
    Type: Grant
    Filed: May 6, 2010
    Date of Patent: March 3, 2015
    Assignees: Astellas Pharma Inc., Kotobuki Pharmaceutical Co., Ltd.
    Inventors: Itsuro Shimada, Kazuo Kurosawa, Takahiro Matsuya, Kazuhiko Iikubo, Yutaka Kondoh, Akio Kamikawa, Hiroshi Tomiyama, Yoshinori Iwai
  • Publication number: 20150057299
    Abstract: Methods for treating cough, chronic cough and urges to cough associated with respiratory diseases with 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 thereof, wherein R1 and R2 are as defined herein.
    Type: Application
    Filed: August 22, 2014
    Publication date: February 26, 2015
    Inventors: Anthony P. Ford, Bruce G. McCarthy
  • Publication number: 20150051232
    Abstract: The invention relates to the use of (R)—S-cyclopropyl-S-(4-{[4-{[(1R,2R)-2-hydroxy-1-methylpropyl]oxy}-5-(trifluoromethyl)pyrimidin-2-yl]amino}phenyl)sulphoximide and/or (S)—S-cyclopropyl-S-(4-{[4-{[(1R,2R)-2-hydroxy-1-methylpropyl]oxy}-5-(trifluoromethyl)pyrimidin-2-yl]amino}phenyl)sulphoximide for the treatment of specific tumours.
    Type: Application
    Filed: March 18, 2013
    Publication date: February 19, 2015
    Inventor: Martin Kornacker
  • Patent number: 8957083
    Abstract: 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: Grant
    Filed: November 18, 2011
    Date of Patent: February 17, 2015
    Assignee: Amgen Inc.
    Inventors: Ana Elena Minatti, Oleg Epstein, Ryan White, Matthew Weiss, Wenge Zhong, Jonathan D. Low
  • Publication number: 20150045339
    Abstract: 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: Application
    Filed: October 16, 2014
    Publication date: February 12, 2015
    Applicant: FUJIFILM CORPORATION
    Inventors: Masaru TAKASAKI, Toshiaki TSUJINO, Shintarou TANABE, Megumi OOKUBO, Kimihiko SATO, Atsushi HIRAI, Daisuke TERADA, Shinsuke INUKI, Shinsuke MIZUMOTO
  • Patent number: 8952027
    Abstract: 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: Grant
    Filed: October 23, 2012
    Date of Patent: February 10, 2015
    Assignee: 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
  • Patent number: 8952025
    Abstract: 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: Grant
    Filed: April 2, 2013
    Date of Patent: February 10, 2015
    Assignee: Arizona Board of Regents, A Body Corporate of the State of Arizona Acting for and on Behalf of Arizona State University
    Inventors: Sidney Hecht, Omar Khdour, Jun Lu, Pablo Arce
  • Patent number: 8946248
    Abstract: 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: Grant
    Filed: September 29, 2005
    Date of Patent: February 3, 2015
    Assignee: Janssen R&D Ireland
    Inventors: Jerôme Emile Georges Guillemont, Jan Heeres, Paulus Joannes Lewi