Spiro Patents (Class 544/230)
  • Publication number: 20140275021
    Abstract: The present invention relates to compounds useful as inhibitors of ATR protein kinase. The invention also relates to pharmaceutically acceptable compositions comprising the compounds of this invention; methods of treating of various diseases, disorders, and conditions using the compounds of this invention; processes for preparing the compounds of this invention; intermediates for the preparation of the compounds of this invention; and methods of using the compounds in in vitro applications, such as the study of kinases in biological and pathological phenomena; the study of intracellular signal transduction pathways mediated by such kinases; and the comparative evaluation of new kinase inhibitors. The compounds of this invention have formula I: or a pharmaceutically acceptable salt, wherein the variables R1, R2, R3, and R4 are as defined herein.
    Type: Application
    Filed: December 6, 2013
    Publication date: September 18, 2014
    Inventors: Jean-Damien Charrier, Chris Davis, Steven Durrant, Damien Fraysse, Juan-Miguel Jimenez, David Kay, Ronald Knegtel, Michael O'Donnell, Francoise Pierard, Joanne Pinder, Pierre-Henri Storck, Heather Twin
  • Publication number: 20140275017
    Abstract: Compounds of Formula I: (wherein variables A1, A2, A3, ring-B, m, n, J, E1, E2, E3, R5, RPG and Y are as described herein), which are useful as antagonists of CGRP receptors, and useful in the treatment or prevention of diseases in which CGRP receptors are involved, such as headache, and in particular migraine and cluster headache. The invention is also directed to pharmaceutical compositions comprising the compounds of formula (I) and the use of these compounds and compositions in the prevention or treatment of diseases in which CGRP receptors are involved.
    Type: Application
    Filed: June 3, 2014
    Publication date: September 18, 2014
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Craig A. Stump, Amy G. Quigley, Cory R. Theberge, Michael R. Wood
  • Publication number: 20140275023
    Abstract: The present invention relates to substituted tricyclic pyrazolo-pyrimidine compounds and methods of synthesizing these compounds. The present invention also relates to pharmaceutical compositions containing substituted tricyclic pyrazolo-pyrimidine compounds and methods of treating cell proliferative disorders, such as cancer, by administering these compounds and pharmaceutical compositions to subjects in need thereof.
    Type: Application
    Filed: March 11, 2014
    Publication date: September 18, 2014
    Inventors: Nivedita Namdev, Jianqiang Wang
  • Patent number: 8834749
    Abstract: Disclosed are a photosensitive resin composition including (A) a binder resin including a cardo-based resin including a repeating unit represented by the following Chemical Formula 1, (B) a photopolymerizable monomer, (C) a photopolymerization initiator, (D) a colorant and (E) a solvent, and a light blocking layer using the same. In the above Chemical Formula 1, each substituent is the same as defined in the detailed description.
    Type: Grant
    Filed: July 22, 2013
    Date of Patent: September 16, 2014
    Assignee: Cheil Industries Inc.
    Inventors: Hyun-Moo Choi, Chang-Min Lee, Ji-Hye Kim, Kyung-Won Ahn, A-Rum Yu, Jae-Bum Yim, Hwan-Sung Cheon, Ju-Ho Jung
  • Publication number: 20140256546
    Abstract: The present invention provides a compound of Formula (I) or an agronomically acceptable salt thereof, wherein: R2 is selected from the group consisting of (A1), (A2) and (A3) wherein X1 is N or CR7X2 is N or CR8X3 is N or CR9X4 is N or CR6R1, R3, R4, R5 R6, R7, R8 and R9 are as defined herein. The invention further relates to herbicidal compositions which comprise a compound of Formula (I), and to their use for controlling weeds, in particular in crops of useful plants.
    Type: Application
    Filed: October 3, 2011
    Publication date: September 11, 2014
    Applicant: SYNGENTA LIMITED
    Inventors: Yunas Bhonoah, Alison Clare Elliott, Steven Gaulier, Kenneth Ling, Glynn Mitchell, James Alan Morris, Paula Rocha Rzepa, Russell Colin Viner
  • Publication number: 20140249135
    Abstract: New compounds, compositions and methods of inhibition of kinase activity associated with tumorigenesis in a human or animal subject are provided. In certain embodiments, the compounds and compositions are effective to inhibit the activity of at least one serine/threonine kinase or receptor tyrosine kinase. The new compounds and compositions may be used either alone or in combination with at least one additional agent for the treatment of a serine/threonine kinase- or receptor tyrosine kinase-mediated disorder, such as cancer.
    Type: Application
    Filed: May 9, 2014
    Publication date: September 4, 2014
    Applicant: NOVARTIS AG
    Inventors: Matthew Burger, Mika Lindvall, Wooseok Han, Jiong Lan, Gisele Nishiguchi, Cynthia Shafer, Cornelia Bellamacina, Kay Huh, Gordana Atallah, Christopher McBride, William Antonios-McCrea, JR., Tatiana Zavorotinskaya, Annette Walter, Pablo Dominguez Garcia
  • Publication number: 20140243306
    Abstract: The present invention describes new pyrrolo pyrimidine derivatives and pharmaceutically acceptable salts thereof which appear to interact with Bruton's tyrosine kinase (Btk). Accordingly, the novel pyrrolo pyrimidines may be effective in the treatment of autoimmune disorders, inflammatory diseases, allergic diseases, airway diseases, such as asthma and chronic obstructive pulmonary disease (COPD), transplant rejection, cancers e.g. of hematopoietic origin or solid tumors.
    Type: Application
    Filed: July 7, 2012
    Publication date: August 28, 2014
    Applicant: NOVARTIS AG
    Inventors: Richard Heng, Elizabeth Kate Hoegenauer, Guido Koch, Robert Alexander Pulz, Anna Vulpetti, Rudolf Waelchli
  • Publication number: 20140242027
    Abstract: The present invention provides compounds of Formula (I): and tautomers, isomers, and esters of said compounds, and pharmaceutically acceptable salts, solvates, and prodrugs of said compounds, wherein each of R, R1, X, Y, Z, R2, R3, R4, R5, R6, R7, R8, R9, R18, R19 and n is selected independently and as defined herein. Compositions comprising such compounds are also provided. The compounds of the invention are effective as inhibitors of HCV, and are useful, alone and together with other therapeutic agents, in treating or preventing diseases or disorders such as viral infections and virus-related disorders.
    Type: Application
    Filed: February 18, 2011
    Publication date: August 28, 2014
    Applicants: Southern Research Institute, Merck Sharp & Dohne Corp.
    Inventors: Ashok Arasappan, F. George Njoroge, Cecil D. Kwong, Subramaniam Ananthan, Frank Bennett, Francisco Velazquez, Vinay Girijavallabhan, Yuhua Huang, Hollis S. Kezer, Joseph Maddry, Robert C. REynold, Abhijit Roychowdhury, Anita T. Fowler, John A. Secrist, III, Ling Tong, Seong Heon Kim, Malcolm MacCoss, Srikanth Venkatraman, vishal Verma
  • Publication number: 20140243290
    Abstract: The present invention provides novel pyrimidine amines of formula (I) which are potent inhibitors of spleen tyrosine kinase, and are useful in the treatment and prevention of diseases mediated by said enzyme, such as asthma, COPD and rheumatoid arthritis.
    Type: Application
    Filed: April 17, 2014
    Publication date: August 28, 2014
    Inventors: Michael D. Altman, Brian M. Andresen, Kenneth L. Arrington, Sathesh Bhat, Jason Burch, Kaleen Konrad Childers, Bernard Cote, Maria Emilia Di Francesco, Anthony Donofrio, Kristina Dupont-Gaudet, John Michael Ellis, Christian Fischer, Jean-Francois Fournier, Jacques Yves Gauthier, Jonathan Grimm, Daniel Guay, David Joseph Guerin, Andrew M. Haidle, Solomon D. Kattar, Sandra Lee Knowles, Chaomin Li, Jongwon Lim, Michelle R. Machacek, Matthew L. Maddess, Alan B. Northrup, Brendan M. O'Boyle, Ryan D. Otte, Alessia Petrocchi, Michael H. Reutershan, Joel S. Robichaud, Eric T. Romeo, Adam J. Schell, Tony Siu, Kerrie B. Spencer, Brandon M. Taoka, B. Wesley Trotter, Hyun Chong Woo, Hua Zhou
  • Patent number: 8815412
    Abstract: An object is to provide a novel quinoxaline derivative, a light-emitting element with low driving voltage, and a light-emitting element which consumes low power. Another object is to provide a light-emitting device and an electronic appliance which consume low power by using the above light-emitting element. A quinoxaline derivative represented by a general formula (G11) is provided, in which at least one of carbon at a 2-position and carbon at a 3-position of quinoxaline, and carbon at a 2-position of a 1H-benzimidazole ring are bonded to each other via an arylene group.
    Type: Grant
    Filed: December 17, 2008
    Date of Patent: August 26, 2014
    Assignee: Semiconductor Energy Laboratory Co., Ltd.
    Inventors: Hiroshi Kadoma, Sachiko Kawakami, Satoko Shitagaki, Satoshi Seo
  • Publication number: 20140235615
    Abstract: Provided is a compound useful for the prophylaxis or treatment of cancer. The present invention relates to a compound represented by formula (I): wherein each symbol in the formula is as defined in the specification, or a salt thereof or a prodrug thereof, which is useful for the prophylaxis or treatment of cancer.
    Type: Application
    Filed: March 24, 2014
    Publication date: August 21, 2014
    Applicant: Takeda Pharmaceutical Company Limited
    Inventors: Misaki HOMMA, Toru MIYAZAKI, Yuya OGURO, Osamu KURASAWA
  • Publication number: 20140235657
    Abstract: 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: Application
    Filed: February 20, 2014
    Publication date: August 21, 2014
    Applicant: Kala Pharmaceuticals, Inc.
    Inventors: Winston Zapanta ONG, Pawel Wojciech Nowak, Ben C. Askew, Jinsoo Kim
  • Publication number: 20140235634
    Abstract: 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: Application
    Filed: February 14, 2014
    Publication date: August 21, 2014
    Applicant: Kala Pharmaceuticals, Inc.
    Inventors: Winston Zapanta ONG, Pawel Wojciech NOWAK, Ben C. ASKEW, Jinsoo KIM
  • Patent number: 8809364
    Abstract: Polycyclic aryl and polycyclic 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 catalytic activity are also disclosed.
    Type: Grant
    Filed: April 1, 2011
    Date of Patent: August 19, 2014
    Assignee: Rigel Pharmaceuticals, Inc.
    Inventors: Rajinder Singh, Dane Goff, Jiaxin Yu, Sacha Holland, Thilo J. Heckrodt, Pingyu Ding, Joane Litvak, Jing Zhang
  • Publication number: 20140228352
    Abstract: Provided is a compound useful for the prophylaxis or treatment of cancer. The present invention relates to a compound represented by formula (I): wherein each symbol in the formula is as defined in the specification, or a salt thereof or a prodrug thereof, which is useful for the prophylaxis or treatment of cancer.
    Type: Application
    Filed: March 24, 2014
    Publication date: August 14, 2014
    Applicant: Takeda Pharmaceutical Company Limited
    Inventors: Misaki HOMMA, Toru MIYAZAKI, Yuya OGURO, Osamu KURASAWA
  • Publication number: 20140227184
    Abstract: Methods of halogenating a carbon containing compound having an sp3 C—H bond are provided. Methods of fluorinating a carbon containing compound comprising halogenation with Cl or Br followed by nucleophilic substitution with F are provided. Methods of direct oxidative C—H fluorination of a carbon containing compound having an sp3 C—H bond are provided. The halogenated products of the methods are provided.
    Type: Application
    Filed: August 20, 2012
    Publication date: August 14, 2014
    Applicant: The Trustees of Princeton University
    Inventors: John T. Groves, Wei Liu, Xiongyi Huang
  • Publication number: 20140225040
    Abstract: The present invention relates to compounds for use in electronic devices, preferably organic electroluminescent devices. The invention furthermore relates to processes for the preparation of these compounds and to electronic devices comprising these compounds, preferably in a function as matrix materials and/or as electron-transport materials.
    Type: Application
    Filed: July 3, 2012
    Publication date: August 14, 2014
    Applicant: Merck Patent GmbH Patents & Scientific Information
    Inventors: Amir Hossain Parham, Christof Pflumm, Anja Jatsch
  • Publication number: 20140221347
    Abstract: Compounds of formula I: or pharmaceutically acceptable 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: Application
    Filed: January 9, 2014
    Publication date: August 7, 2014
    Applicant: Gilead Sciences, Inc.
    Inventors: Gediminas BRIZGYS, Chien-Hung CHOU, Randall L. HALCOMB, Yunfeng Eric HU, Qi LIU, John R. SOMOZA, Winston C. TSE, Jennifer R. ZHANG
  • Publication number: 20140221310
    Abstract: The present invention relates to compounds of Formula (I), or a form thereof, wherein ring A, R1, L and R2 are as defined herein, useful as FLAP modulators. The invention also relates to pharmaceutical compositions comprising compounds of Formula (I). Methods of making and using the compounds of Formula (I) are also within the scope of the invention.
    Type: Application
    Filed: January 31, 2014
    Publication date: August 7, 2014
    Applicant: JANSSEN PHARMACEUTICA NV
    Inventors: Wendy Eccles, Anne E. Fitzgerald, Michael D. Hack, Natalie A. Hawryluk, William M. Jones, John M. Keith, Paul Krawczuk, Alec D. Lebsack, Jing Liu, Neelakandha S. Mani, Kelly J. McClure, Steven P. Meduna, Mark D. Rosen
  • Publication number: 20140221346
    Abstract: 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: Application
    Filed: January 9, 2014
    Publication date: August 7, 2014
    Applicant: Gilead Sciences, Inc.
    Inventors: Randall L. HALCOMB, Yunfeng Eric HU, Qi LIU, Jennifer R. ZHANG
  • Publication number: 20140221333
    Abstract: Provided are 6-5 membered fused pyridine ring compounds according to Formula (I) or pharmaceutically acceptable salts thereof, pharmaceutical compositions comprising these compounds and their use in therapy. In particular, provided is the use of membered fused pyridine ring compounds in the treatment of Bruton's Tyrosine Kinase (Btk) mediated disorders.
    Type: Application
    Filed: July 19, 2012
    Publication date: August 7, 2014
    Inventors: Adrianus Petrus Antonius De Man, Jan-Gerard Sterrenburg, Han C.A. Raaijmakers, Allard Kaptein, Arthura A. Oubrie, Johannes Bernardus Maria Rewinkel, Christiaan Gerardus Johannes Maria Jans, Jacobus C.H.M. Wijkamans, Tjeerd A. Barf, Alan B. Cooper, Ronald M. Kim, Sobhana Babu Boga, Hugh Y. Zhu, Xiaolei Gao, Xin Yao, Rajan Anand, Hao Wu, Shilan Liu, Chundao Yang, Abdul-Basit Alhassan, James Wang, Younong Yu, Jian Liu, Henry M. Vaccaro
  • Publication number: 20140221352
    Abstract: Disclosed are compounds of formula I, compositions containing them, and methods of use for the compounds and compositions in the treatment of conditions in which modulation of the JAK pathway or inhibition of JAK kinases, particularly JAK 2 and JAK3, are therapeutically useful.
    Type: Application
    Filed: April 10, 2014
    Publication date: August 7, 2014
    Applicant: Rigel Pharmaceuticals, Inc.
    Inventors: Yan Chen, Vanessa Taylor, Hui Li, Rajinder Singh
  • Publication number: 20140209884
    Abstract: The present disclosure provides a nitrogen-containing heterocyclic compound and an organic electronic device comprising the same. The organic electronic device according to the present disclosure shows excellent characteristics in terms of efficiency, driving voltage and lifespan.
    Type: Application
    Filed: June 18, 2013
    Publication date: July 31, 2014
    Applicant: LG Chem Ltd.
    Inventors: Tae Yoon Park, Minseung Chun, Sung Kil Hong, Dong Hoon Lee, Dongheon Kim
  • Publication number: 20140206664
    Abstract: Heterocycle amino alkyloxy substituted quinazoline derivatives as represented by the structural Formula (I) and pharmaceutically acceptable salts thereof, capable of inhibiting the activity of receptor tyrosine kinase EGFR, and being used to treat cancers related to the expression of the receptor tyrosine kinase of the ErbB family are provided.
    Type: Application
    Filed: December 13, 2012
    Publication date: July 24, 2014
    Inventor: Wei Qian
  • Publication number: 20140200209
    Abstract: The present invention is to provide a novel compound (I) shown below, having the anti-virus activity; particularly the HIV integrase inhibitory activity, and a drug containing the same, particularly an anti-HIV drug, as well as a process and an intermediate thereof. (wherein Z1 is NR4; R1 is hydrogen or lower alkyl; X is a single bond, a hetero atom group selected from O, S, SO, SO2 and NH, or lower alkylene or lower alkenylene in which the hetero atom group may intervene; R2 is optionally substituted aryl; R3 is hydrogen, a halogen, hydroxy, optionally substituted lower alkyl etc; and R4 and Z2 part taken together forms a ring, to form a polycyclic compound, including e.g., a tricyclic or tetracyclic compound.
    Type: Application
    Filed: March 14, 2014
    Publication date: July 17, 2014
    Applicants: ViiV Healthcare Company, Shionogi & Co., Ltd.
    Inventors: Brian A. JOHNS, Takashi KAWASUJI, Teruhiko TAISHI, Yoshiyuki TAODA
  • Publication number: 20140200223
    Abstract: The present invention is directed to a compound represented by the following structural formula or a pharmaceutically acceptable salt thereof. Pharmaceutical compositions and method of use of the compounds are also described.
    Type: Application
    Filed: December 18, 2013
    Publication date: July 17, 2014
    Inventors: Salvacion Cacatian, David A. Claremon, Lawrence Wayne Dillard, Klaus Fuchs, Niklas Heine, Lanqi Jia, Katerina Leftheris, Brian Mckeever, Angel Morales-Ramos, Suresh B. Singh, Shankar Venkatraman, Guosheng Wu, Zhongren Wu, Zhenrong Xu, Jing Yuan, Yajun Zheng
  • Patent number: 8778938
    Abstract: The present invention discloses compounds of Formula (I), or pharmaceutically acceptable salts, esters, or prodrugs thereof: which inhibit RNA-containing virus, particularly the Hepatitis C Virus (HCV). Consequently, the compounds of the present invention interfere with the life cycle of the Hepatitis C Virus and are also useful as antiviral agents. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from HCV infection. The invention also relates to methods of treating an HCV infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention.
    Type: Grant
    Filed: June 3, 2011
    Date of Patent: July 15, 2014
    Assignee: Enanta Pharmaceuticals, Inc.
    Inventors: Yao-Ling Qiu, Ce Wang, Hui Cao, Xiaowen Peng, Datong Tang, Yat Sun Or
  • Publication number: 20140194404
    Abstract: This invention relates to amidopyrazole compounds that are inhibitors of Interleukin receptor-associated kinases, in particular IRAK-4, and are useful in the treatment of cellular proliferative diseases, for example, cancer, hyperplasia, restenosis, cardiac hypertrophy, immune disorders and inflammation.
    Type: Application
    Filed: March 21, 2012
    Publication date: July 10, 2014
    Inventors: William T. McElroy, Guoqing Li, Ginny Dai Ho, Zheng Tan, Sunil Paliwal, William Michael Seganish, Deen Tulshian, John Lampe, Joey L. Methot, Hua Zhou, Michael D. Altman, Liang Zhu
  • Patent number: 8772301
    Abstract: Provided herein are compounds and methods of synthesis thereof. The compounds set forth herein are useful for the treatment, prevention, and/or management of various disorders, such as neurological disorders, neurodegenerative disorders, neuropsychiatric disorders, disorders of cognition, learning or memory, gastrointestinal disorders, lower urinary tract disorder, and cancer. Compounds set forth herein modulate the activity of metabotropic glutamate receptor 5 (mGluR5) in the central nervous system or the periphery. Pharmaceutical formulations containing the compounds and their methods of use are also provided herein.
    Type: Grant
    Filed: December 17, 2010
    Date of Patent: July 8, 2014
    Assignee: Sunovion Pharmaceuticals, Inc.
    Inventors: Larry Wendell Hardy, Michele L. R. Heffernan, Frank Xinhe Wu, Kerry L. Spear, Lakshmi D. Saraswat
  • Patent number: 8772288
    Abstract: The present disclosure is directed to new inhibitors of the p38 mitogen-activated protein kinase having the general formula (I), processes for preparation thereof, pharmaceutical compositions thereof, and methods of use thereof.
    Type: Grant
    Filed: April 3, 2009
    Date of Patent: July 8, 2014
    Assignee: Almirall, S.A.
    Inventors: Paul Robert Eastwood, Jacob Gonzalez Rodriguez, Bernet Vidal Juan, Nuria Aguilar Izquierdo
  • Patent number: 8772286
    Abstract: The present invention relates to compounds of general Formula (I) or a pharmaceutically acceptable salt thereof. The compounds can be used in the treatment of immune, autoimmune, inflammatory diseases, cardiovascular diseases, infectious diseases, bone resorption disorders, neurodegenerative diseases or proliferative diseases.
    Type: Grant
    Filed: December 13, 2010
    Date of Patent: July 8, 2014
    Assignee: Merck Sharp & Dohme B.V.
    Inventors: Tjeerd Andries Barf, Arthur Oubrie, Carsten Schultz-Fademrecht, Eduard Willem Zwart, Niels Hoogenboom, Sander Martijn De Wilde, Allard Kaptein
  • Publication number: 20140187534
    Abstract: A compound of the following general formula [I]: wherein each symbol has the same meaning as defined herein, or a pharmaceutically acceptable salt thereof, or a solvate thereof, and a pharmaceutical use of the same in treating organ transplant rejection, graft versus host reaction after transplantation, autoimmune disease, allergic disease and chronic myeloproliferative disease.
    Type: Application
    Filed: November 12, 2013
    Publication date: July 3, 2014
    Applicant: Japan Tobacco Inc.
    Inventors: Satoru Noji, Makoto Shiozaki, Tomoya Miura, Yoshinori Hara, Hiroshi Yamanaka, Katsuya Maeda, Akimi Hori, Masafumi Inoue, Yasunori Hase
  • Publication number: 20140187530
    Abstract: The present invention provides a compound of Formula I or Formula II: enantiomer, diastereomer, prodrug, solvate, metabolite, or pharmaceutically acceptable salt thereof, wherein constituent variables are provided herein. The compounds of Formula I and II are modulators of metalloproteases and are useful in treating diseases associated with metalloprotease activity such as arthritis, cancer, cardiovascular disorders, skin disorders, inflammation and allergic conditions.
    Type: Application
    Filed: November 27, 2013
    Publication date: July 3, 2014
    Applicant: INCYTE CORPORATION
    Inventors: Wenqing Yao, Jincong Zhuo, Meizhong Xu, Fenglei Zhang, Brian W. Metcalf
  • Patent number: 8765744
    Abstract: The present invention relates to compounds defined by formula I wherein the variables R1, R2, R3, R4, R7, A, Z and m are as defined herein. The compounds of formula (I) are inhibitors of 11-beta-hydroxysteroid dehydrogenase 1 (11beta-HSD1) and thus are suitable for treatment and prevention of diseases which can be influenced by inhibition of this enzyme, such as metabolic diseases, in particular diabetes type 2, obesity, and dyslipidemia.
    Type: Grant
    Filed: June 23, 2011
    Date of Patent: July 1, 2014
    Assignee: Boehringer Ingelheim International GmbH
    Inventor: Frank Himmelsbach
  • Publication number: 20140179666
    Abstract: The invention relates to bicyclic heterocycle compounds of formula (I): or tautomeric or stereochemically isomeric forms, N-oxides, pharmaceutically acceptable salts or the solvates thereof; wherein R1, R2a, R2b, R3a, R3b, R5, R6, R7, R8, R9, p and E are as defined herein; to pharmaceutical compositions comprising said compounds and to the use of said compounds in the treatment of diseases, e.g. cancer.
    Type: Application
    Filed: April 20, 2012
    Publication date: June 26, 2014
    Applicant: ASTEX THERAPEUTICS LIMITED
    Inventors: Alison Jo-Anne Woolford, Steven Howard, Ildiko Maria Buck, Gianni Chessari, Christopher Norbert Johnson, Emiliano Tamanini, James Edward Harvey Day, Elisabetta Chiarparin, Thomas Daniel Heightman, Martyn Frederickson, Charlotte Mary Griffiths-Jones
  • Publication number: 20140179668
    Abstract: Fused pyrimidine compounds as kinase inhibitors, such as multi-kinase inhibitors, are provided. Fused pyrimidine compounds as IGF-IR inhibitors are provided. The compounds may be used in a method of treating cancer. Pharmaceutical compositions containing a fused pyrimidine compound and a pharmaceutically acceptable carrier are also provided, as are kits containing a fused pyrimidine compound or salt thereof and instructions for use, e.g., in a method of treating cancer.
    Type: Application
    Filed: December 26, 2013
    Publication date: June 26, 2014
    Applicant: MEDIVATION TECHNOLOGIES, INC.
    Inventors: Sarvajit CHAKRAVARTY, Roopa RAI, Michael John GREEN
  • Publication number: 20140179682
    Abstract: Compounds that modulate GluR5 activity and methods of using the same are disclosed.
    Type: Application
    Filed: June 8, 2012
    Publication date: June 26, 2014
    Applicant: SUNOVION PHARMACEUTICALS INC.
    Inventors: Michele L. R. Heffernan, Larry Wendell Hardy, Frank Xinhe Wu, Lakshmi D. Saraswat, Kerry L. Spear
  • Publication number: 20140179695
    Abstract: The present invention provides a compound which is useful as an active ingredient of a pharmaceutical composition, in particular, a pharmaceutical composition for preventing or treating diseases or conditions associated with and/or mediated by ?-secretase activity, hydrolysis of a ?-secretase site of a ?-amyloid precursor protein, and/or ?-amyloid protein accumulation, including a pharmaceutical composition for preventing or treating diseases including, but not limited to, Glaucoma, MCI (Mild cognitive impairment) or Alzheimer's disease, especially, Alzheimer's disease.
    Type: Application
    Filed: February 27, 2014
    Publication date: June 26, 2014
    Applicants: CoMentis, Inc., ASTELLAS PHARMA INC.
    Inventors: Ryosuke MUNAKATA, Makoto INOUE, Hiroaki TOMINAGA, Shingo YAMASAKI, Yasuhiro SHIINA, Kiyohiro SAMIZU, Hisao HAMAGUCHI, Lin HONG
  • Patent number: 8754096
    Abstract: The present invention is directed to piperidinone carboxamide azaindane derivatives which are antagonists of CGRP receptors and useful in the treatment or prevention of diseases in which the CGRP is involved, such as migraine. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which CGRP is involved.
    Type: Grant
    Filed: November 10, 2011
    Date of Patent: June 17, 2014
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Ian M. Bell, Mark E. Fraley, Steven N. Gallicchio, Anthony Ginnetti, Helen J. Mitchell, Daniel V. Paone, Donnette D. Staas, Heather E. Stevenson, Cheng Wang, C. Blair Zartman
  • Patent number: 8754107
    Abstract: The present invention is directed to novel aminopyrrolidines of formula I pharmaceutically acceptable salts thereof, metabolites thereof, isomers thereof, stereoisomers thereof or pro-drugs thereof, wherein the variables are as defined herein. The compounds of formula (I) are useful as chemokine receptor antagonists and as such would be useful in treating certain conditions and diseases, especially inflammatory conditions and diseases and proliferative disorders and conditions, for example, cancers.
    Type: Grant
    Filed: November 16, 2007
    Date of Patent: June 17, 2014
    Assignee: AbbVie Inc.
    Inventors: Dawn M. George, Richard W. Dixon, Michael Friedman, Adrian D. Hobson, Biqin Li, Lu Wang, Xiaoyun Wu, Neil Wishart
  • Publication number: 20140161801
    Abstract: The invention relates to a quinazoline derivative represented by the general formula (I), a pharmaceutical acceptable salt and a stereoisomer thereof as tyrosine kinase inhibitor, wherein R1, R2, R3, R3?, R4, R5, R6, X, L, T, Z and q are as defined in the specification. The invention also relates to a process for preparing the same, a pharmaceutical composition and a pharmaceutical formulation containing the derivative, use of the derivative for treating excessive proliferative diseases and chronic obstructive pulmonary disease and use of the derivative in the manufacture of a medicament for treating excessive proliferative diseases and chronic obstructive pulmonary disease.
    Type: Application
    Filed: May 28, 2012
    Publication date: June 12, 2014
    Applicant: XUANZHU PHARMA CO., LTD.
    Inventors: Frank Wu, Aichen Wang
  • Publication number: 20140162983
    Abstract: The present invention provides novel pyrimidine and pyridine compounds according to Formula (I), Formula (II), Formula (III), Formula (IV) and Formula (V) their manufacture and use for the treatment of hyperproliferative diseases including, but not limited to, cancer, lupus, allergic disorders, Sjogren's disease and rheumatoid arthritis. In preferred embodiments, the present invention describes irreversible kinase inhibitors including, but not limited to, inhibitors of Bruton's tyrosine kinase.
    Type: Application
    Filed: June 10, 2012
    Publication date: June 12, 2014
    Applicant: Merck Patent GmbH
    Inventors: Brian L. Hodous, Lesley Liu-Bujalski, Reinaldo Jones, Donald Bankston, Theresa L. Johnson, Igor Mochalkin, Ngan Nguyen, Hui Qiu, Andreas Goutopoulos, Nadia Brugger
  • Publication number: 20140148474
    Abstract: The present invention provides novel pyrimidine amines of formula I which are potent inhibitors of spleen tyrosine kinase, and are useful in the treatment and prevention of diseases mediated by said enzyme, such as asthma, COPD, rheumatoid arthritis and cancer.
    Type: Application
    Filed: May 4, 2012
    Publication date: May 29, 2014
    Inventors: Michael D. Altman, Kaleen Konrad Childers, Maria Emilia Di Francesco, John Michael Ellis, Christian Fischer, Jonathan Grimm, Andrew M. Haidle, Solomon D. Kattar, Alan B. Northrup, Ryan D. Otte, Alessia Petrocchi, Adam J. Schell, Hua Zhou
  • Publication number: 20140140958
    Abstract: Compounds, methods, and compositions for the treatment of infections in or exposure to humans and other host animals of Flaviviridae viruses, including HCV, that includes the administration of an effective amount of a spiro[2.4]heptane as described herein or a pharmaceutically acceptable salt or prodrug thereof, optionally in a pharmaceutically acceptable carrier, are provided. The spiro[2.4]heptane compounds either possess antiviral activity, or are metabolized to a compound that exhibits such activity.
    Type: Application
    Filed: January 23, 2014
    Publication date: May 22, 2014
    Applicant: University of Georgia Research Foundation, Inc.
    Inventor: Chung K. Chu
  • Publication number: 20140142084
    Abstract: Provided is a compound useful as a prophylactic and/or therapeutic agent for bladder cancer. As a result of studies on compounds having FGFR inhibitory action, the present inventors have found that the nitrogen-containing aromatic heterocyclic compounds of the present invention have inhibitory action on FGFR1, FGFR2, and/or FGFR3, particularly, mutant FGFR3, and thus, the present invention has been accomplished. The nitrogen-containing aromatic heterocyclic compound of the present invention can be used as a therapeutic agent for various cancers related to FGFR1, FGFR2, and/or FGFR3, such as lung cancer and hormone therapy-resistant breast cancer, stomach cancer, triple negative breast cancer, endometrial cancer, bladder cancer, and glioblastoma, particularly as a prophylactic and/or therapeutic agent for mutant FGFR3-positive bladder cancer.
    Type: Application
    Filed: February 26, 2013
    Publication date: May 22, 2014
    Applicants: KOTOBUKI PHARMACEUTICAL CO., LTD., Astellas Pharma Inc.
    Inventors: Minoru Kameda, Ikumi Kuriwaki, Kazuhiko Iikubo, Hiroyuki Hisamichi, Yuichiro Kawamoto, Hiroyuki Moritomo, Tomoyuki Suzuki, Takashi Futami, Atsushi Suzuki, Kazuhisa Tsunoyama, Makoto Asaumi, Hiroshi Tomiyama, Atsushi Noda, Yoshinori Iwai, Kazuo Tokuzaki, Haruki Okada, Kozo Miyasaka
  • Patent number: 8729079
    Abstract: The present application provides novel pyrimido-pyridazinone compounds and methods for preparing and using these compounds. These compounds are useful in treating inflammation in patients by administering one or more of the compounds to a patient. In one embodiment, the novel pyrimido-pyridazinone compound is of Formula (I) and R1 and R2 are defined herein.
    Type: Grant
    Filed: August 23, 2012
    Date of Patent: May 20, 2014
    Assignee: Endo Pharmaceuticals Inc.
    Inventors: Aranapakam Venkatesan, Roger Astbury Smith, Subramanya Hosahalli, Vijay Potluri, Sunil Kumar Panigrahi, Vishnu Basetti, Karunasree Kunta
  • Publication number: 20140134193
    Abstract: The present invention is directed to novel cytotoxic spliceostatin analogs and derivatives, to antibody drug conjugates thereof, and to methods for using the same to treat medical conditions including cancer.
    Type: Application
    Filed: October 31, 2013
    Publication date: May 15, 2014
    Applicant: PFIZER INC.
    Inventors: Chakrapani SUBRAMANYAM, Frank Erich KOEHN, Kenneth John DIRICO, Alessandra S. EUSTAQUIO, Michael Eric GREEN, Haiyin HE, Min HE, Christopher John O'DONNELL, Sujiet PUTHENVEETIL, Anokha RATNAYAKE, Jesse Alexander TESKE, Hui Yu YANG
  • Publication number: 20140121206
    Abstract: The present invention relates to spirocarbamate compounds of Formula (I) in which R1, (R2)Y, R3, R4, X and A have the meanings given in the specification. The invention further provides pharmaceutical compositions containing the compounds or pharmaceutically acceptable salts thereof and relates to their use of these compounds as TRPV4 antagonists in treating or preventing conditions associated with TRPV4 imbalance.
    Type: Application
    Filed: June 15, 2012
    Publication date: May 1, 2014
    Applicant: GlaxoSmithKliine, LLC
    Inventors: Carl Brooks, Mui Cheung, Hilary Schenck Eidam, Krista B. Goodman, Marlys Hammond, Mark A. Hilfiker, Tram H. Hoang, Jaclyn R. Patterson, Patrick Stoy, Guosen Ye
  • Publication number: 20140113882
    Abstract: The present application provides a compound of formula (I) or a salt thereof, wherein R7, R8, R9, G, and X are as defined herein. This application further describes compositions comprising the same. Compounds of formula (I) and their salts have aPKC inhibitory activity, and may be used to treat proliferative disorders.
    Type: Application
    Filed: September 27, 2013
    Publication date: April 24, 2014
    Applicants: Cancer Research Technology Limited, Cephalon, Inc.
    Inventors: Henry J. Breslin, Bruce D. Dorsey, Benjamin J. Dugan, Katherine M. Fowler, Robert L. Hudkins, Eugen F. Mesaros, Nathaniel J.T. Monck, Emma L. Morris, Ikeoluwa Olowoye, Gregory R. Ott, Gregoire A. Pave, Jonathan R. Roffey, Christelle N. Soudy, Ming Tao, Craig A. Zificsak, Allison L. Zulli
  • Publication number: 20140113914
    Abstract: Compounds of Formula I: and pharmaceutically acceptable salts and solvates thereof, wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, and R10 have the meanings as indicated in the specification, are useful for treating diseases mediated by blockade of the epithelial sodium channel. Pharmaceutical compositions that contain the compounds and processes for preparing the compounds are also described.
    Type: Application
    Filed: October 22, 2012
    Publication date: April 24, 2014
    Applicant: NOVARTIS AG
    Inventors: Gurdip BHALAY, Lee EDWARDS, Catherine HOWSHAM, Peter HUNT, Nichola SMITH