Plural Hetero Atoms In The Polycyclo Ring System Patents (Class 514/338)
  • Triazole-substituted anthranilamides as pesticides
    Patent number: 8536202
    Abstract: The present invention constitutes new, triazole-substituted anthranilamides of the general formula (I), —in which R1, R2, R3, R4, R5, R6, Q, A and n have the definitions indicated in the description—, the application thereof as insecticides and acaricides for controlling animal pests, also in combination with further agents for activity boosting, and a number of processes for their preparation.
    Type: Grant
    Filed: April 14, 2011
    Date of Patent: September 17, 2013
    Assignee: Bayer Cropscience AG
    Inventors: Rüdiger Fischer, Christoph Grondal, Ernst Rudolf Gesing, Heinz-Juergen Wroblowsky, Achim Hense, Eva-Maria Franken, Arnd Voerste, Ulrich Görgens
  • MODULATORS OF ATP-BINDING CASSETTE TRANSPORTERS
    Publication number: 20130237568
    Abstract: Compounds of the present invention, and pharmaceutically acceptable compositions thereof, are useful as modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator (“CFTR”). The present invention also relates to methods of treating ABC transporter mediated diseases using compounds of the present invention.
    Type: Application
    Filed: April 26, 2013
    Publication date: September 12, 2013
    Inventors: Sara S. Hadida Ruah, Matthew Hamilton, Mark Miller, Peter D.J. Grootenhuis, Brian Bear, Jason McCartney, Jinglan Zhou
  • MODULATORS OF ATP-BINDING CASSETTE TRANSPORTERS
    Publication number: 20130237569
    Abstract: Compounds of the present invention, and pharmaceutically acceptable compositions thereof, are useful as modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator (“CFTC”). The present invention also relates to methods of treating ABC transporter mediated diseases using compounds of the present invention.
    Type: Application
    Filed: April 26, 2013
    Publication date: September 12, 2013
    Inventors: Sara S. Hadida Ruah, Matthew Hamilton, Mark Miller, Peter D.J. Grootenhuis, Brian Bear, Jason McCartney, Jinglan Zhou
  • NOVEL COMPOUNDS THAT ARE ERK INHIBITORS
    Publication number: 20130237518
    Abstract: Disclosed are the ERK inhibitors of formula (1): and the pharmaceutically acceptable salts thereof, wherein: A is a five membered monocyclic heteroaryl ring; and B is a monocyclic heterocycloalkyl ring, or a monocyclic heterocycloalkenyl ring, or a bridged monocyclic heterocycloalkyl ring, or a fused (monocyclic heterocycloalkyl ring) cyclopropyl ring. Also disclosed are methods of treating cancer using the compounds of formula (1).
    Type: Application
    Filed: October 24, 2011
    Publication date: September 12, 2013
    Inventors: Sobhana Babu Boga, Joseph M. Kelly, Hugh Y. Zhu, Abdul-Basit Alhassan, Xin Yao, Xiaolei Gao, James J-S Wang, Jagdish A. Desai, Subrahmanyam Gudipati, Sie-Mun Lo, Liang Zhu, Alan B. Cooper, Yongqi Deng, Gerald W. Shipps, JR.
  • USE OF MELANOMA INHIBITORY ACTIVITY (MIA) PROTEIN AS AN EARLY INDICATOR FOR THERAPEUTIC RESPONSE IN MELANOMA
    Publication number: 20130237546
    Abstract: The present invention provides a method for determining a response of a mammalian subject having melanoma tumor cells to treatment with a melanoma inhibitory agent. In one aspect, the method comprises (a) determining a first concentration of melanoma inhibitory activity protein (MIA) in a first biological sample taken from the mammalian subject before treatment with the melanoma inhibitory agent; (b) determining a second concentration of MIA in a second biological sample from the mammalian subject taken after treatment with the melanoma, inhibitory agent; and (c) comparing the first and second concentrations of MIA, wherein a decrease in the second concentration of MIA measured in the second biological sample as compared to the first concentration of MIA measured in the first biological sample indicates a positive response to the treatment with the melanoma inhibitory agent.
    Type: Application
    Filed: October 4, 2012
    Publication date: September 12, 2013
    Applicant: Novartis AG
    Inventors: Nguyen Tan, Eleni Venetsanakos, Michel Faure, Carla Heise
  • Crystalline (R)-(E)-2-(4-(2-(5-(1-(3,5-dichloropyridin-4-yl)ethoxy)-1H-indazol-3-yl)vinyl)-1H-pyrazol-1-yl)ethanol
    Patent number: 8530665
    Abstract: The present invention provides crystalline (R)-(E)-2-(4-(2-(5-(1-(3,5 -dichloropyridin-4-yl)ethoxy)-1H-indazol-3-yl)vinyl)-1H-pyrazol-1-yl)ethanol useful in the treatment of cancer.
    Type: Grant
    Filed: September 29, 2011
    Date of Patent: September 10, 2013
    Assignee: Eli Lilly and Company
    Inventor: Benjamin Alan Diseroad
  • Stable pharmaceutical omeprazole formulation for oral administration
    Patent number: 8530500
    Abstract: The present invention is directed to a pharmaceutical solution or syrup formulation for oral administration comprising; omeprazole, a solubilizing agent, a sweetening agent, a flavoring agent, and an antioxidant.
    Type: Grant
    Filed: July 20, 2010
    Date of Patent: September 10, 2013
    Assignee: Vetegen, LLC
    Inventors: Erik Juvonen, Louis Massimo Micolucci
  • Small Molecule Inhibitors Of P-type ATPases
    Publication number: 20130231372
    Abstract: Small, low molecular weight compounds of the formula I and/or the formula II, as defined herein, which inhibit Cu-ATPases, ATP7A and ATP7B. Compositions and methods therefore, are provided.
    Type: Application
    Filed: March 1, 2012
    Publication date: September 5, 2013
    Inventors: Mary Matsui, Daniel Yarosh
  • BIOMARKERS FOR RESPONSE TO TYROSINE KINASE PATHWAY INHIBITORS IN CANCER
    Publication number: 20130230511
    Abstract: Copy number gains detected in tumors and associated with drug sensitivity and resistance in vivo and in vitro can be used as biomarkers to select, predict and monitor drug treatment outcomes in cancer patients treated with tyrosine kinase inhibitors. Methods to identify patients with NSCLC or other malignancies who are more likely to benefit from tyrosine kinase inhibitors such as VEGF or VEGFR inhibitors when used either as monotherapy or in combination with other therapies such as chemotherapy or EGFR inhibitors, and who are in the advanced stages of disease and/or who have undergone adjuvant therapy are also provided herein.
    Type: Application
    Filed: February 4, 2013
    Publication date: September 5, 2013
    Applicant: BOARD OF REGENTS, THE UNIVERSITY OF TEXAS SYSTEM
    Inventor: Board of Regents, The University of Texas System
  • ESTROGEN RECEPTOR MODULATORS AND USES THEREOF
    Publication number: 20130231333
    Abstract: Described herein are compounds that are estrogen receptor modulators. Also described are pharmaceutical compositions and medicaments that include the compounds described herein, as well methods of using such estrogen receptor modulators, alone and in combination with other compounds, for treating diseases or conditions that are mediated or dependent upon estrogen receptors.
    Type: Application
    Filed: September 15, 2011
    Publication date: September 5, 2013
    Applicant: ARAGON PHARMACEUTICALS, INC.
    Inventors: Nicholas D. Smith, Mehmet Kahraman, Steven P. Govek, Johnny Y. Nagasawa, Andiliy G. Lai, Jackaline D. Julien, Mark R. Herbert, Celine Bonnefous, Karensa L. Douglas
  • Benzisothiazol-3(1H)-one-5-sulfonyl derivatives as chemokine receptor modulators
    Patent number: 8524745
    Abstract: The present invention relates to novel benzisothiazol-3(1H)-one-5-sulfonyl derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of chemokine receptors.
    Type: Grant
    Filed: December 11, 2012
    Date of Patent: September 3, 2013
    Assignee: Allergan, Inc.
    Inventors: Haiqing Yuan, Richard L. Beard, Xiaoxia Liu, John E. Donello, Veena Viswanath
  • Pyridyl derivatives as CFTR modulators
    Patent number: 8524910
    Abstract: The present invention relates to modulators of Formula I and the accompanying definitions herein of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator (“CFTR”), compositions thereof, and methods therewith. The present invention also relates to methods of treating ABC transporter mediated diseases such as cystic fibrosis using such modulators.
    Type: Grant
    Filed: June 26, 2012
    Date of Patent: September 3, 2013
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: Sara Hadida Ruah, Mark Miller, Jinglan Zhou, Brian Bear, Peter Grootenhuis
  • GLUCOSYLCERAMIDE SYNTHASE INHIBITION FOR THE TREATMENT OF COLLAPSING GLOMERULOPATHY AND OTHER GLOMERULAR DISEASE
    Publication number: 20130225573
    Abstract: A method of treating a glomerular disease selected from the group consisting of mesangial proliferative glomerulonephritis, collapsing glomerulopathy, proliferative lupus nephritis, crescentic glomerulonephritis and membranous nephropathy in a subject comprises administering to the subject an effective amount of a glucosylceramide synthase inhibitor.
    Type: Application
    Filed: February 7, 2013
    Publication date: August 29, 2013
    Applicant: GENZYME CORPORATION
    Inventor: Genzyme Corporation
  • SUBSTITUTED BENZAZOLES AND METHODS OF THEIR USE AS INHIBITORS OF RAF KINASE
    Publication number: 20130224195
    Abstract: New substituted benzazole compounds, compositions and methods of inhibition of Raf kinase activity in a human or animal subject are provided. The new compounds compositions may be used either alone or in combination with at least one additional agent for the treatment of a Raf kinase mediated disorder, such as cancer.
    Type: Application
    Filed: April 3, 2013
    Publication date: August 29, 2013
    Inventors: Abran Costales, Teresa Hansen, Barry H. Levine, Christopher McBride, Daniel J. Poon, Savithri Ramurthy, Paul A. Renhowe, Cynthia M. Shafer, Sharadha Subramanian, Joelle Verhagen
  • Dimethylarginine Dimethylaminohydrolase Inhibitors and Methods of Use Thereof
    Publication number: 20130224259
    Abstract: The present disclosure provides DDAH modulators. Thus, the present disclosure provides a method of treating a patient suffering from a disorder characterized by excessive NO production and/or elevated DDAH activity, the method comprising administering to said patient an effective amount of a compound of one of formulae I-X. The present disclosure also provides a pharmaceutical composition comprising a compound of one of formulae I-X.
    Type: Application
    Filed: February 13, 2013
    Publication date: August 29, 2013
    Applicant: The Board of Trustees of the Leland Stanford Junior University
    Inventor: The Board of Trustees of the Leland Stanford Junior University
  • IMIDOTHIAZOLE KINASE INHIBITORS
    Publication number: 20130225591
    Abstract: The present invention is directed to novel kinase inhibitors of general formula (I) and pharmaceutically acceptable salts thereof, and to the use of the kinase inhibitors of general formula (I) for treating diseases or disorders in which tau phosphorylation and cell cycle regulation is implicated, such as Alzheimer's Disease and cancer.
    Type: Application
    Filed: September 14, 2010
    Publication date: August 29, 2013
    Inventors: Michelle R. Machacek, Sean P. Ahearn, Eric Romeo, Tony Siu, Stephanie Chichetti, Gabriela de Almeida, Alexey A. Rivkin
  • Tricyclic compounds as mPGES-1 inhibitors
    Patent number: 8519149
    Abstract: The present invention relates to tricyclic compounds of formula (I) or pharmaceutically acceptable salt thereof as mPGES-1 inhibitors. These compounds are inhibitors of the microsomal prostaglandin E synthase-1 (mPGES-1) enzyme and are therefore useful in the treatment of pain and/or inflammation from a variety of diseases or conditions, such as asthma, osteoarthritis, rheumatoid arthritis, acute or chronic pain and neurodegenerative diseases.
    Type: Grant
    Filed: October 28, 2011
    Date of Patent: August 27, 2013
    Assignee: Glenmark Pharmaceuticals S.A.
    Inventors: Laxmikant A. Gharat, Nagarajan Muthukaman, Lakshminarayana Narayana, Neelima Khairatkar-Joshi, Vidya G. Kattige
  • Aryl pyridine as aldosterone synthase inhibitors
    Patent number: 8519142
    Abstract: The present invention provides a compound of formula I; a method for manufacturing the compounds of the invention, and its therapeutic uses. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.
    Type: Grant
    Filed: September 14, 2012
    Date of Patent: August 27, 2013
    Assignee: Novartis AG
    Inventors: Sylvie Chamoin, Qi-Ying Hu, Julien Papillon
  • NOVEL BIARYL BENZOIMIDAZOLE DERIVATIVES AND PHARMACEUTICAL COMPOSITION COMPRISING THE SAME
    Publication number: 20130217684
    Abstract: Disclosed are biaryl benzoimidazole derivatives. They have an inhibitory effect on calcium influx in HEK cells, thereby showing a powerful antagonistic effect on a vanilloid receptor, and further have an analgesic effect, thereby being useful for preventing or treating pain, acute pain, chronic pain, neuropathic pain, postoperative pain, migraine, arthralgia, neuropathies, nerve injury, diabetic neuropathy, neurological illness, neurodermatitis, stroke, bladder hypersensitivity, irritable bowel syndrome, a respiratory disorder such as cough, asthma, and chronic obstructive pulmonary disease, burning, psoriasis, itching, vomiting, irritation of the skin, eyes, and mucous membranes, gastric-duodenal ulcers, inflammatory intestinal diseases, and inflammatory diseases.
    Type: Application
    Filed: April 5, 2013
    Publication date: August 22, 2013
    Applicant: DAEWOONG PHARMACEUTICAL CO., LTD.
    Inventor: Daewoong Pharmaceutical Co., Ltd.
  • TRICYCLIC COMPOUNDS AND METHODS OF USE THEREFOR
    Publication number: 20130217666
    Abstract: The invention relates to novel compounds of Formula I: wherein A1, A2, A3, A4, A5, A6, R2, R4, R5, R6, R7, R8 and subscripts m and n each has the meaning as described herein. Compounds of Formula I and pharmaceutical compositions thereof are useful in the treatment of disease and disorders in which undesired or over-activation of NF-kB signaling is observed.
    Type: Application
    Filed: February 15, 2013
    Publication date: August 22, 2013
    Applicant: Genentech, Inc.
    Inventor: Genentech, Inc.
  • PHARMACEUTICAL COMPOSITIONS OF (R)-LANSOPRAZOLE
    Publication number: 20130216617
    Abstract: The present invention relates to stable pharmaceutical compositions of (R)-lansoprazole or pharmaceutically acceptable salts thereof and process of preparing the same. The invention particularly provides pharmaceutical compositions of optically active (R)-isomer of lansoprazole with at least two functional coating layers.
    Type: Application
    Filed: June 28, 2011
    Publication date: August 22, 2013
    Applicant: CADILA HEALTHCARE LIMITED
    Inventors: Sunilendu Bhushan Roy, Sushrut Krishnaji Kulkarni, Manohar Vishwanath Lalge, Vaibhav Panditrao Deshmukh
  • Use of epothilones in the treatment of neuronal connectivity defects such as schizophrenia and autism
    Patent number: 8513280
    Abstract: The present invention is about the use of at least one epothilone or derivative thereof as an active ingredient for manufacturing a medicament for use in the treatment of disease(s) involving a neuronal connectivity defect.
    Type: Grant
    Filed: September 9, 2010
    Date of Patent: August 20, 2013
    Assignees: Institut National de la Sante et de la Recherche Medicale, Commissariat a l'Energie Atomique, Gesellschaft fur Biotechnologische Forschung mbH (GBF)
    Inventors: Annie Andrieux, Didier Job, Annie Schweitzer, Gerhard Höfle
  • COMPOSITIONS OF SMALL MOLECULE THERAPEUTICS
    Publication number: 20130210766
    Abstract: Compositions containing a small molecule therapeutic and an alkyl N,N-disubstituted amino acetate are disclosed. Inclusion of the alkyl N,N-disubstituted amino acetate enhances the pharmacokinetic properties of the small molecule therapeutic.
    Type: Application
    Filed: May 4, 2011
    Publication date: August 15, 2013
    Applicant: NEXMED HOLDINGS, INC.
    Inventors: Bassam B. Damaj, Richard Martin
  • Novel Heterocyclic Compounds and Uses Thereof
    Publication number: 20130210818
    Abstract: New substituted heterocyclic compounds, compositions containing them, and methods of using them for the inhibition of Raf kinase activity are provided. The new compounds and compositions may be used either alone or in combination with at least one additional agent for the treatment of a Raf kinase mediated disorder, such as cancer.
    Type: Application
    Filed: February 14, 2012
    Publication date: August 15, 2013
    Inventors: Zilin Huang, Jeff Jin, Timothy Machajewski, William R. Antonios-McCrea, Maureen McKenna, Daniel Poon, Paul A. Renhowe, Martin Sendzik, Cynthia Shafer, Aaron Smith, Yongjin Xu, Qiong Zhang, Zheng Chen
  • SULFAMOYL BENZOIC ACID HETEROBICYCLIC DERIVATIVES AS TRPM8 ANTAGONISTS
    Publication number: 20130210858
    Abstract: The present invention relates to sulfamoyl benzoic acid heterobicyclic derivatives of the formula (I) or a pharmaceutically acceptable salt thereof or a prodrug thereof, processes for their preparation, pharmaceutical compositions containing them and their use in the treatment of various disorders which are mediated via the TRPM8 receptor.
    Type: Application
    Filed: October 3, 2011
    Publication date: August 15, 2013
    Applicant: Raqualia Pharma Inc.
    Inventors: Kiyoshi Kawamura, Yuji Shishido, Masashi Ohmi
  • Solid forms of 3-(6-(1-(2,2-difluorobenzo[d][1,3]dioxol-5-yl) cyclopropanecarboxamido)-3-methylpyridin-2-yl)benzoic acid
    Patent number: 8507534
    Abstract: The present invention relates to a substantially crystalline and free solid state form of 3-(6-(1-(2,2-difluorobenzo[d][1,3]dioxol-5-yl)cyclopropanecarboxamido)-3-methylpyridin-2-yl)benzoic acid (Form I), pharmaceutical compositions thereof, and methods of treatment therewith.
    Type: Grant
    Filed: December 4, 2008
    Date of Patent: August 13, 2013
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: Ali Keshavarz-Shokri, Beili Zhang, Mariusz Krawiec
  • Bicyclic pyridinylpyrazoles
    Patent number: 8507472
    Abstract: Bicyclic pyridinylpyrazoles of the formula (I) in which the symbols have the meanings given in the description and agrochemically active salts thereof and their use for controlling unwanted microorganisms in crop protection and the protection of materials and for reducing mycotoxins in plants and plant parts, and also processes for preparing compounds of the formula (I).
    Type: Grant
    Filed: April 5, 2011
    Date of Patent: August 13, 2013
    Assignee: Bayer CropScience AG
    Inventors: Amos Mattes, Hendrik Helmke, Stefan Hillebrand, Gorka Peris, Alexander Sudau, Lars Rodefeld, Stefan Gauger, Jürgen Benting, Peter Dahmen, Ruth Meissner, Ulrike Wachendorff-Neumann, Hiroyuki Hadano
  • SUBSTITUTED SEVEN-MEMBERED HETEROCYCLIC COMPOUNDS AS DIPEPTIDYL PEPTIDASE-IV INHIBITORS FOR THE TREATMENT OF DIABETES
    Publication number: 20130203786
    Abstract: The present invention is directed to novel amino-substituted seven-membered heterocyclic compounds of structural formula (I) which are inhibitors of the dipeptidyl peptidase-IV enzyme and which are useful in the treatment or prevention of diseases in which the dipeptidyl peptidase-IV enzyme is involved, such as diabetes and particularly Type 2 diabetes. 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 the dipeptidyl peptidase-IV enzyme is involved.
    Type: Application
    Filed: May 16, 2011
    Publication date: August 8, 2013
    Inventors: Jacqueline D. Hicks, Tesfaye Biftu, Ping Chen, Xiaoxia Qian, Robert R. Wilkening
  • BENZOTHIAZOLES AS GHRELIN RECEPTOR MODULATORS
    Publication number: 20130203730
    Abstract: A compound of formula I or a pharmaceutically acceptable salt thereof in which R1, R2, R3, R4 and m are as described in the specification for use in the treatment of obesity and/or diabetes.
    Type: Application
    Filed: March 13, 2013
    Publication date: August 8, 2013
    Applicant: AstraZeneca AB
    Inventor: AstraZeneca AB
  • THIOACETATE COMPOUNDS, COMPOSITIONS AND METHODS OF USE
    Publication number: 20130202573
    Abstract: Described herein are compounds useful in the modulation of blood uric acid levels, formulations containing them and methods of using them. In some embodiments, the compounds described herein are used in the treatment or prevention of disorders related to aberrant levels of uric acid.
    Type: Application
    Filed: June 15, 2011
    Publication date: August 8, 2013
    Applicant: Ardea Biosciences, Inc.
    Inventors: Samedy Ouk, Esmir Gunic, Jean-Michel Vernier, Chixu Chen
  • DELAYED RELEASE ORAL DISINTEGRATING PHARMACEUTICAL COMPOSITIONS OF LANSOPRAZOLE
    Publication number: 20130202688
    Abstract: The present invention relates to delayed release oral disintegrating pharmaceutical compositions of lansoprazole or pharmaceutically acceptable salts thereof. The invention also relates to processes for the preparation of such compositions.
    Type: Application
    Filed: May 3, 2011
    Publication date: August 8, 2013
    Inventors: Sunilendu Bhushan Roy, Sushrut Krishnaji Kulkarni, Hemant Manilal Mamania
  • IDENTIFICATION OF GENETIC VARIANTS
    Publication number: 20130202587
    Abstract: The present disclosure provides a method for identifying whether a subject is more or less likely to be responsive to VEGF-based therapy, comprising screening a nucleic acid sample obtained from the subject to provide output information which identifies the presence or absence of an allelic variant, wherein the presence or absence of an allelic variant indicates whether the subject is more or less likely to be responsive to VEGF-based therapy.
    Type: Application
    Filed: August 24, 2012
    Publication date: August 8, 2013
    Applicant: Randox Laboratories Ltd.
    Inventor: John Lamont
  • PROLYL HYDROXYLASE INHIBITORS AND METHODS OF USE
    Publication number: 20130203816
    Abstract: The present disclosure relates to HIF-1? prolyl hydroxylase inhibitors, compositions which comprise the HIF-1? prolyl hydroxylase inhibitors described herein and to methods for controlling, inter alia, Peripheral Vascular Disease (PVD), Coronary Artery Disease (CAD), heart failure, ischemia, and anemia.
    Type: Application
    Filed: November 20, 2012
    Publication date: August 8, 2013
    Applicant: Akebia Therapeutics Inc.
    Inventors: Richard Masaru Kawamoto, Shengde Wu, Namal C. Warshakoon, Artem G. Evdokimov, Kenneth D. Greis, Angelique Sun Boyer
  • INHIBITORS OF HUMAN IMMUNODEFICIENCY VIRUS REPLICATION
    Publication number: 20130203747
    Abstract: Compounds of formula I: wherein a, R1, R2, R3, R4, R5 and R6 are defined herein, are useful as inhibitors of HIV replication.
    Type: Application
    Filed: November 21, 2012
    Publication date: August 8, 2013
    Applicant: Gilead Sciences, Inc.
    Inventor: Gilead Sciences, Inc.
  • Salts of benzimidazolyl pyridyl ethers and formulations thereof
    Patent number: 8501785
    Abstract: Salts of benzimidazolyl pyridyl ethers are provided, particularly salts of {1-methyl-5-[2-(5-trifluoromethyl-1H-imidazol-2-yl)-pyridin-4-yloxy]-1H-benzoimidazol-2-yl}-(4-trifluoromethyl-phenyl)amine. Compositions and formulations including such salts and surfactants as well as methods of preparing such compositions and formulations are provided.
    Type: Grant
    Filed: June 4, 2012
    Date of Patent: August 6, 2013
    Assignee: Novartis AG
    Inventors: Rampurna Gullapalli, Ahmad Hashash, Piotr Karpinski, Kangwen L. Lin, Eric M. Loeser, Augustus O. Okhamafe, Paul Allen Sutton, Eduardo Sy
  • CYCLOPROPYLAMINE DERIVATIVES USEFUL AS LSD1 INHIBITORS
    Publication number: 20130197013
    Abstract: The invention relates to cyclopropylamine compounds, in particular the compounds of Formula (I), and their use in therapy, including e.g. in the treatment or prevention of cancer, a neurological disease or condition, or viral infection.
    Type: Application
    Filed: July 27, 2011
    Publication date: August 1, 2013
    Inventors: Mathew Colin Thor Fyfe, Alberto Ortega Muñoz, Julio Castro-Palomino Laria, Marc Martinell Pedemonte, Maria de los Ángeles Estiarte-Martínez, Nuria Valls Vidal
  • HETEROCYCLIC DERIVATIVES FOR THE TREATMENT OF DISEASES
    Publication number: 20130196952
    Abstract: The invention relates to compounds of Formula (1) and to processes for the preparation of intermediates used in the preparation of compositions containing and the uses of such derivatives. The compounds according to the present invention are useful in numerous diseases in which ALK protein is involved or in which inhibition of ALK activity may induce benefit, especially for the treatment of cancer mediated by a mutated EML4-ALK fusion protein.
    Type: Application
    Filed: May 4, 2011
    Publication date: August 1, 2013
    Applicant: PFIZER INC.
    Inventors: Mark Edward Bunnage, Andrew Simon Cook, Jingrong Jean Cui, Kevin Nell Dack, Judith Gail Deal, Danlin Gu, Mingying He, Patrick Stephen Johnson, Ted William Johnson, Phuong Thi Quy Le, Cynthia Louise Palmer, Hong Shen
  • 3-AMINOCYCLOPENTANECARBOXAMIDES AS CHEMOKINE RECEPTOR AGONISTS
    Publication number: 20130197008
    Abstract: There is provided a compound of Formula I(a) or I(b): or a pharmaceutically acceptable salt thereof, wherein the various substitutents are defined herein.
    Type: Application
    Filed: September 14, 2012
    Publication date: August 1, 2013
    Applicant: Pfizer Inc.
    Inventors: Robert O. HUGHES, Rajesh V. Devraj, Donald J. Rogier, John I. Trujillo, Steve R. Turner, Wei Huang
  • Heterocyclic compound and use thereof
    Patent number: 8497274
    Abstract: Provided is a fused heterocycle derivative showing a strong Raf inhibitory activity. A compound represented by the formula wherein each symbol is as defined in the present specification, or a salt thereof.
    Type: Grant
    Filed: January 10, 2012
    Date of Patent: July 30, 2013
    Assignee: Takeda Pharmaceutical Company Limited
    Inventors: Masanori Okaniwa, Terufumi Takagi, Masaaki Hirose
  • Hexahydropyrroloimidazolone compounds
    Patent number: 8497288
    Abstract: The invention provides novel compounds having the general formula (I), wherein R1, R2, R3 and A are as described herein, compositions including the compounds and methods of using the compounds. These compounds are useful as inhibitors of hormone sensitive lipase (HSL) and may be used in the treatment of diabetes, metabolic syndrome, dyslipidemia, atherosclerosis, obesity, cardiovascular diseases, myocardial dysfunction, inflammation, non-alcoholic fatty liver disease and non-alcoholic steatohepatitis.
    Type: Grant
    Filed: May 2, 2012
    Date of Patent: July 30, 2013
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Aurelia Conte, Daniel Hunziker, Werner Neidhart, Matthias Nettekoven, Tanja Schulz-Gasch
  • Pyrrolinone derivative and pharmaceutical composition comprising the same
    Patent number: 8497263
    Abstract: The present invention provides a compound represented by the formula (I): wherein R1, R2, R3, Z1, Z2, Ra, Rb, q, A and n are as defined in the description, a pharmaceutically acceptable salt or solvate thereof. The compound is useful as P2X3 and/or P2X2/3 receptor antagonist.
    Type: Grant
    Filed: September 23, 2011
    Date of Patent: July 30, 2013
    Assignee: Shionogi & Co., Ltd.
    Inventors: Hiroyuki Kai, Shunji Shinohara, Takayuki Kameyama
  • FUSED HETEROCYCLIC COMPOUNDS AND USES THEREOF
    Publication number: 20130190271
    Abstract: Disclosed is a harmful arthropod control composition comprising, as an active ingredient, a fused heterocyclic compound represented by formula (1) [wherein A1 and A2 independently represent a nitrogen atom or the like; R1 and R4 independently represent a halogen atom or the like; R2 and R3 independently represent a halogen atom or the like; R5 and R6 independently represent a linear C1-C6 hydrocarbon group which may be substituted, or the like (provided that both R5 and R6 cannot represent a hydrogen atom simultaneously); and n represents 0 or 1]. The harmful arthropod control composition has an excellent efficacy to control harmful arthropods.
    Type: Application
    Filed: March 8, 2013
    Publication date: July 25, 2013
    Applicant: SUMITOMO CHEMICAL COMPANY, LIMITED
    Inventor: Sumitomo Chemical Company, Limited
  • FORMULATIONS OF 3-(6-(1-(2,2-DIFLUOROBENZO[D][1,3]DIOXOL-5-YL) CYCLOPROPANECARBOXAMIDO)-3-METHYLPYRIDIN-2-YL)BENZOIC ACID
    Publication number: 20130186801
    Abstract: A pharmaceutical composition comprising Compound 1, (3-(6-(1-(2,2-difluorobenzo[d][1,3]dioxol-5-yl)cyclopropanecarboxamido)-3-methylpyridin-2-yl)benzoic acid), and at least one excipient selected from: a filler, a disintegrant, a surfactant, a binder, and a lubricant, the composition being suitable for oral administration to a patient in need thereof to treat a CFTR mediated disease such as Cystic Fibrosis. Processes of preparing pharmaceutical compositions comprising Compound 1 are also disclosed.
    Type: Application
    Filed: January 25, 2013
    Publication date: July 25, 2013
    Applicant: Vertex Pharmaceuticals Incorporated
    Inventor: Marinus Jacoubus Verwijs
  • NOVEL ORALLY ADMINISTERED DABIGATRAN FORMULATION
    Publication number: 20130190358
    Abstract: The invention relates to a new medicament formulation of the active substance dabigatran etexilate of formula I optionally in the form of the pharmaceutically acceptable salts thereof, as well as the preparation thereof.
    Type: Application
    Filed: January 23, 2013
    Publication date: July 25, 2013
    Applicant: Boehringer Ingelheim International GmbH
    Inventor: Georg BOECK
  • BRIDGED HETEROCYCLIC COMPOUNDS AND METHODS OF USE
    Publication number: 20130190359
    Abstract: This disclosure relates to new compounds that may be used to modulate a histamine receptor in an individual. Novel compounds are described, including new bridged heterocyclic [4,3-b]indole compounds. Pharmaceutical compositions are also provided. Pharmaceutical compositions comprising the compounds are also provided, as are methods of using the compounds in a variety of therapeutic applications, including the treatment of a cognitive disorder, psychotic disorder, neurotransmitter-mediated disorder and/or a neuronal disorder.
    Type: Application
    Filed: March 8, 2013
    Publication date: July 25, 2013
    Applicant: MEDIVATION TECHNOLOGIES, INC.
    Inventor: MEDIVATION TECHNOLOGIES, INC.
  • Mediators of Hedgehog Signaling Pathways, Compositions and Uses Related Thereto
    Publication number: 20130190350
    Abstract: The present invention makes available methods and reagents for inhibiting aberrant growth states resulting from hedgehog gain-of-function, ptc loss-of-function or smoothened gain-of-function comprising contacting the cell with a hedgehog antagonist, such as a small molecule, in a sufficient amount to aberrant growth state, e.g., to agonize a normal ptc pathway or antagonize smoothened or hedgehog activity.
    Type: Application
    Filed: December 12, 2012
    Publication date: July 25, 2013
    Applicant: CURIS, INC.
    Inventor: Curis, Inc.
  • Substituted phenylimidazopyrazoles and their use
    Publication number: 20130190290
    Abstract: The present application relates to novel 1-phenyl-1H-imidazo[1,2-b]pyrazole derivatives, to processes for their preparation, to their use for the treatment and/or prevention of diseases and to their use for preparing medicaments for the treatment and/or prevention of diseases, in particular angiogenic disorders and hyperproliferative disorders, where neovascularization plays a role, such as, for example, neoplastic disorders and tumour disorders. Such treatments can be carried out as monotherapy or else in combination with other medicaments or further therapeutic measures.
    Type: Application
    Filed: January 23, 2013
    Publication date: July 25, 2013
    Applicant: BAYER INTELLECTUAL PROPERTY GMBH
    Inventor: BAYER INTELLECTUAL PROPERTY GmbH
  • Compositions Containing a Pyripyropene Insecticide and an Adjuvant
    Publication number: 20130190360
    Abstract: Pesticidal composition containing a pyripyropene insecticide and an adjuvant The present invention relates to a compositions comprising a pyripyropene pesticide of the formula (I) or (II) as defined below and an adjuvant. The present invention relates also to methods of preparing and applying such compositions, as well as several uses thereof, and finally seeds, comprising said composition. The invention also relates to an aqueous pesticide formulation comprising a pesticide compound of the formula I as defined in claim 1 in the form of fine particles suspended in an aqueous liquid.
    Type: Application
    Filed: September 13, 2011
    Publication date: July 25, 2013
    Applicant: BASF SE
    Inventors: Wen Xu, Paul Neese, William Maurice Fletcher, Douglas D. Anspaugh, Heidi Emilia Saxell, Cedric Dieleman, Walter Weishaar, Paul Ch. Kierkus, Kara Benton, Rainer Berghaus, Tatjana Levy
  • COMPOSITIONS AND METHODS FOR ASSESSING AND TREATING A PRECURSOR LESION AND/OR ESOPHAGEAL CANCER
    Publication number: 20130190357
    Abstract: One aspect of the present disclosure relates to a method for predicting a subject's risk of developing an esophageal cancer, a precursor lesion, or both. One step of the method includes obtaining a biological sample from the subject. Next, the presence of at least one germline mutation is determined in the biological sample. The subject is at an increased risk of an esophageal cancer, a precursor lesion, or both, where the presence of at least one germline mutation is determined.
    Type: Application
    Filed: July 26, 2012
    Publication date: July 25, 2013
    Inventor: Charis Eng
  • Composition containing a pyripyropene insecticide and a base
    Publication number: 20130184153
    Abstract: The present invention relates to a composition comprising a pyripyropene pesticide of the formula (I) or (II) as defined below and a base. The present invention relates also to methods of preparing and applying such compositions, as well as several uses thereof, and finally seeds, comprising said composition.
    Type: Application
    Filed: September 13, 2011
    Publication date: July 18, 2013
    Applicant: BASF SE
    Inventors: Cedric Dieleman, Torsten Knieriem, Michael Krapp, Paul Ch. Kierkus, Wen Xu, Kara Benton