The Polycyclo Ring System Is Quinazoline (including Hydrogenated) Patents (Class 514/252.17)
  • Patent number: 11033549
    Abstract: Disclosed herein are compounds for use in lightening skin, treating uneven skin pigmentation and/or improving the appearance of aging skin, as well as methods utilizing the compounds, and anti-aging compositions comprising the compounds and a pharmaceutically acceptable carrier. The compounds have the general Formula I: or a pharmaceutically acceptable salt thereof, wherein the dashed line, X, Y, Z, Ra-Rd, and R1-R3 are as defined herein.
    Type: Grant
    Filed: March 14, 2018
    Date of Patent: June 15, 2021
    Assignee: ATIR Holding S.A.
    Inventors: Izabella Munblit, Karina Tsipe
  • Patent number: 10927095
    Abstract: The present invention relates to novel procedures and novel intermediates useful in the synthesis of Niraparib or any salt thereof.
    Type: Grant
    Filed: August 14, 2018
    Date of Patent: February 23, 2021
    Inventors: Parven K. Luthra, Sanjay L. Vasoya, Bhatu T. Patil, Amit K. Taneja, Naveen C. Srivastav, Rinku Singh
  • Patent number: 10751324
    Abstract: Provided herein is technology relating to treating and/or ameliorating TNF? cytotoxicity and particularly, but not exclusively, to compositions, methods, and kits for specifically modulating BCL-2-associated death promoter (BAD) activity, for example, by modulating the activity of Src and/or p190GAP.
    Type: Grant
    Filed: September 1, 2017
    Date of Patent: August 25, 2020
    Assignee: The University of Chicago
    Inventor: Anning Lin
  • Patent number: 10392353
    Abstract: Disclosed herein is a novel process for preparing substituted quinazoline compounds of formula (I) using a hydrogen bonding catalyst.
    Type: Grant
    Filed: November 18, 2016
    Date of Patent: August 27, 2019
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Cheol K. Chung, Guy R. Humphrey, Zhijian Liu, Mark McLaughlin, Yingju Xu, Younong Yu
  • Patent number: 10316027
    Abstract: Disclosed are 1-(arylmethyl)quinazoline-2,4(1H,3H)-diones represented by the Formula (I): wherein Ar, R1-R6, are defined herein. Compounds having Formula (I) are PARP inhibitors. Therefore, compounds of the invention may be used to treat clinical conditions that are responsive to the inhibition of PARP activity.
    Type: Grant
    Filed: March 26, 2018
    Date of Patent: June 11, 2019
    Assignee: Impact Therapeutics, Inc.
    Inventors: Sui Xiong Cai, Ye Edward Tian, Haijun Dong, Qingbing Xu, Lizhen Wu, Lijun Liu, Yangzhen Jiang, Qingli Bao, Guoxiang Wang, Feng Yin, Chengyun Gu, Xiuhua Hu, Xiaozhu Wang, Sishun Kang, Shengzhi Chen
  • Patent number: 10287254
    Abstract: The invention relates to besylate and tosylate salts of {8-fluoro-2-[4-(3-methoxyphenyl)piperazin-1-yl]-3-[2-methoxy-5-(trifluoromethyl)phenyl]-3,4-dihydroquinazolin-4-yl} acetic acid and solvates thereof, to the use thereof in a method of treating and/or preventing virus infections, and to the use thereof to produce drugs for use in treating and/or preventing diseases, in particular use as antiviral agents, in particular against cytomegaloviruses (FIG. 1).
    Type: Grant
    Filed: October 31, 2016
    Date of Patent: May 14, 2019
    Assignee: AiCuris GmbH & Co. KG
    Inventors: Welljanne Maertens, Christian Schickaneder
  • Patent number: 10238627
    Abstract: Synthetic cremastranone and cremastranone analogs are disclosed. Additionally, methods for synthesizing cremastranone and cremastranone analogs are disclosed. Methods of treating ocular neovascularization disorders and treating angiogenesis-mediated disease are also disclosed.
    Type: Grant
    Filed: February 6, 2018
    Date of Patent: March 26, 2019
    Assignee: Indiana University Research and Technology Corporation
    Inventors: Timothy W. Corson, Halesha D. Basavarajappa, Seung-Yong Seo, Bit Lee, Xiang Fei
  • Patent number: 10126307
    Abstract: Methods are provided for quantifying the Androgen receptor protein (AR) protein directly in biological samples that have been fixed in formalin, using Selected Reaction Monitoring (SRM)/Multiple Reaction Monitoring (MRM) mass spectrometry. The biological samples are chemically preserved and fixed and can be, for example, tissues treated with formaldehyde containing agents/fixatives including formalin-fixed tissue/cells, formalin-fixed/paraffin embedded (FFPE) tissue/cells, FFPE tissue blocks and cells from those blocks. A protein sample is prepared from said biological sample using, for example, the Liquid Tissue protocol and the AR protein is quantitated in the Liquid Tissue sample by the method of SRM/MRM mass spectrometry by quantitating in the protein sample at least one or more of the peptides described.
    Type: Grant
    Filed: April 30, 2015
    Date of Patent: November 13, 2018
    Assignee: Expression Pathology, Inc.
    Inventors: David B. Krizman, Todd Hembrough, Sheeno Thyparambil, Eunkyung An
  • Patent number: 10086045
    Abstract: The present invention relates to the field of stem cells. In one aspect, the present invention provides methods of treating a subject with acute liver injury comprising administering to the subject a therapeutically effective amount of at least one stem cell mobilizer. In particular embodiments, the subject is treated with plerixafor and granulocyte colony-stimulating factor (G-CSF).
    Type: Grant
    Filed: September 1, 2016
    Date of Patent: October 2, 2018
    Assignee: The Johns Hopkins University
    Inventor: Andrew MacGregor Cameron
  • Patent number: 9895301
    Abstract: The invention provides for methods for treating a hair loss disorder in a subject by administering a Janus Kinase/Signal Transducers and Activators of Transcription inhibitor.
    Type: Grant
    Filed: August 7, 2015
    Date of Patent: February 20, 2018
    Assignee: The Trustees of Columbia University in The City of New York
    Inventors: Angela M. Christiano, Raphael Clynes
  • Patent number: 9868707
    Abstract: Provided herein are small molecule neurotensin receptor agonists, compositions comprising the compounds, and methods of using the compounds and compositions comprising the compounds.
    Type: Grant
    Filed: December 19, 2013
    Date of Patent: January 16, 2018
    Assignees: SANFORD-BURNHAM MEDICAL RESEARCH INSTITUTE, DUKE UNIVERSITY
    Inventors: Anthony Pinkerton, Patrick Maloney, Paul Hershberger, Satyamaheshwar Peddibhotla, Michael Hedrick, Lawrence Barak, Marc Caron
  • Patent number: 9512085
    Abstract: The invention relates to besylate and tosylate salts of {8-fluoro-2-[4-(3-methoxyphenyl)piperazin-1-yl]-3-[2-methoxy-5-(trifluoromethyl)phenyl]-3,4-dihydroquinazolin-4-yl}acetic acid and solvates thereof, to the use thereof in a method of treating and/or preventing virus infections, and to the use thereof to produce drugs for use in treating and/or preventing diseases, in particular use as antiviral agents, in particular against cytomegaloviruses.
    Type: Grant
    Filed: February 28, 2013
    Date of Patent: December 6, 2016
    Assignee: AICURIS GMBH & CO. KG
    Inventors: Welljanne Maertens, Christian Schickaneder
  • Patent number: 9273012
    Abstract: A straightforward single step method for the preparation and/or production of substituted quinazolines is disclosed, wherein said quinazolines preferably contain one substituent at position 4, and may contain other functional groups at various positions, such as 5, 6, 7, and/or 8 of quinazolines. In addition, the extension of this new method leads to the formation of different type of heterocyclic aromatic compounds, that include but are not limited to perimidines, anthrapyrimidin-7-ones (also known as anthrapyrimidinones), anthra[1,9:5,10]dipyrimidines (also known as quinazoline[5,4-ef]perimidines) and benzo[e]-pyrimido[4,5,6-gh]pyrimidines.
    Type: Grant
    Filed: April 30, 2012
    Date of Patent: March 1, 2016
    Assignee: University of Houston System
    Inventor: Zerong Daniel Wang
  • Patent number: 9260441
    Abstract: This invention relates to certain heteroaryl compounds for use as medicaments, more specifically as medicaments for treating animals. The medicament can be used for the treatment of helminth infections and the treatment of parasitosis caused by helminth infections. This invention also relates to uses of the compounds to make medicaments and treatments comprising the administration of the compounds to animals in need of the treatments. This invention also relates to pharmaceutical compositions and kits comprising the compounds.
    Type: Grant
    Filed: March 27, 2013
    Date of Patent: February 16, 2016
    Assignee: Intervet Inc.
    Inventors: Michael Berger, Marko Eck, Christopher Kern
  • Patent number: 9133138
    Abstract: Disclosed is a use of a quinazoline compound of Formula I having 2,4-diaminoquinazoline as a parent nucleus in preparation of a medicament for treating diseases caused by flaviviridae infection, especially a use in combating Hepatitis C virus infection and Dengue fever virus infection.
    Type: Grant
    Filed: December 2, 2011
    Date of Patent: September 15, 2015
    Assignee: SHANGHAI INSTITUTE OF MATERIA MEDICA, CHINESE ACADEMY OF SCIENCES
    Inventors: Jianping Zuo, Youhong Hu, Wei Tang, Bo Chao, Xiankun Tong, Dewen Li, Feihong Ji, Peilan He
  • Publication number: 20150147379
    Abstract: The embodiments relate generally to medical devices and to methods of their manufacture. One aspect provides devices including chitosan fibers that are a free of chemical cross linking. Another aspect provides a method of manufacturing such devices.
    Type: Application
    Filed: November 18, 2014
    Publication date: May 28, 2015
    Applicant: COOK MEDICAL TECHNOLOGIES LLC
    Inventor: Mohammad Z. Albanna
  • Publication number: 20150148256
    Abstract: A bioluminescence imaging-based high-throughput assay for inhibitors of ABCG2 is described. Compositions of inhibitors of ABCG2 and methods of using ABCG2 inhibitors are also described.
    Type: Application
    Filed: August 21, 2014
    Publication date: May 28, 2015
    Applicant: THE JOHNS HOPKINS UNIVERSITY
    Inventors: MARTIN GILBERT POMPER, YIMAO ZHANG, JOHN LATERRA
  • Publication number: 20150141400
    Abstract: The present invention relates to quinazolinedione derivatives represented by formula (I) or pharmaceutically acceptable salts thereof.
    Type: Application
    Filed: April 24, 2013
    Publication date: May 21, 2015
    Inventors: Takeshi Murata, Hatsuo Kawada, Satoshi Niizuma, Sousuke Hara, Kihito Hada, Hideaki Shimada, Hiroshi Tanaka, Toshiyuki Mio
  • Publication number: 20150133414
    Abstract: It was determined whether SNPs in SLC4A5 are associated with salt sensitivity of blood pressure (BP). Subjects consumed an isocaloric constant diet with a randomized order of 7 days low Na+ (10 mmol/d) and 7 days high Na+ (300 mmol/d) intake. Salt sensitivity was defined as a ?7 mm Hg increase in mean arterial pressure (MAP). 35 polymorphisms in 17 candidate genes were assayed. Association analyses with salt sensitivity revealed three variants that associated with salt sensitivity, two in SLC4A5 (rs7571842, rs10177833; P<0.001), and one in GRK4 (rs1801058; P=0.020). Paradoxical changes in blood pressure in response to changes in salt intake were also found associated with a SNP for DRD2 (rs6276). In conclusion, SLC4A5 variants are strongly associated with salt sensitivity of BP in Caucasian and a DRD2 SNP is a marker for paradoxical response to salt intake.
    Type: Application
    Filed: April 22, 2013
    Publication date: May 14, 2015
    Applicant: University of Virginia Patent Foundation
    Inventors: Robin A. Felder, Robert M. Carey, John E. Jones, Pedro A. Jose, Scott M. Williams
  • Publication number: 20150133460
    Abstract: This invention provides a compound of formula (I): or a crystalline form thereof, or a pharmaceutical composition thereof, or an oral pharmaceutical dosage form thereof; processes for the synthesis or manufacture of the compound of formula (I), or a crystalline form thereof, or a pharmaceutical composition thereof, or an oral pharmaceutical dosage form thereof; and the use of said compound, or a crystalline form thereof, or a pharmaceutical composition thereof, or an oral pharmaceutical dosage form thereof, for the treatment of patients suffering from or subject to diseases, disorders or conditions involving cell survival, proliferation, and migration, including cardiovascular disease (e.g., arteriosclerosis and vascular reobstruction), cancer, (e.g., AML and malignant glioma) glomerulosclerosis, fibrotic disease and inflammation.
    Type: Application
    Filed: November 11, 2013
    Publication date: May 14, 2015
    Applicant: Millennium Phamaceuticals, Inc.
    Inventors: Ian Armitage, Abu J. Ferdous, Michael E. Bourland, Craig S.J. Boyle, Martin Ian Cooper, Marianne Langston
  • Publication number: 20150133461
    Abstract: The invention relates to pharmaceutical compositions, particularly for intravenous administration, containing {8-fluoro-2-[4-(3-methoxyphenyl)piperazine-1-yl]-3-[2-methoxy-5-(trifluoromethyl)phenyl]-3,4-dihydroquinazoline-4-yl}acetic acid in combination with at least one of the cyclodextrin excipients, lysine and arginine; the method for its production; and its use in methods of treatment of and/or as a prophylactic for illnesses, particularly its use as an antiviral, preferably against cytomegaloviruses.
    Type: Application
    Filed: February 28, 2013
    Publication date: May 14, 2015
    Applicant: AICURIS GMBH & CO. KG
    Inventors: Kerstin Paulus, Wilfried Schwab, Dominique Grunder, Peter Van Hoogevest
  • Publication number: 20150133439
    Abstract: The Present invention relates to nitrogen-containing heterocyclic compounds and pharmaceutically acceptable salts thereof which have inhibitory activity on the phosphorylation of kinases, which inhibits the activity of such kinases. The invention is also related to a method of inhibiting kinases and treating disease states in a mammal by inhibiting the phosphorylation of kinases. In a particular aspect the present invention provides nitrogen-containing heterocyclic compounds and pharmaceutically acceptable salts thereof which inhibit phosphorylation of a PDGF receptor to hinder abnormal cell growth and cell wandering, and a method for preventing or treating cell-proliferative diseases such as arteriosclerosis, vascular reobstruction, cancer and glomerulosclerosis.
    Type: Application
    Filed: July 9, 2014
    Publication date: May 14, 2015
    Inventors: Anjali Pandey, Robert M. Scarborough, Kenji Matsuno, Michio Ichimura, Yuji Nomoto, Shinichi Ide, Eiji Tsukuda, Junko Sasaki, Shoji Oda
  • Publication number: 20150126492
    Abstract: The present invention provides a compound of formula I a method for manufacturing the compounds of the invention, and its therapeutic uses as inhibitor of the complement alternative pathway and particularly as inhibitor of Factor B for the treatment of e.g. age-related macular degeneration and diabetic retinopathy. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.
    Type: Application
    Filed: June 19, 2013
    Publication date: May 7, 2015
    Applicant: NOVARTIS AG
    Inventors: Michael Dechantsreiter, Jonathan E. Grob, Aengus Macsweeney, Wolfgang Miltz, Stefan Andreas Randl, Richard Sedrani, Holger Sellner, Finton Sirockin, Eric Valeur
  • Publication number: 20150110723
    Abstract: The disclosure relates to quinazoline derivatives, compositions, and methods related thereto. In certain embodiments, the disclosure relates to inhibitors of NADPH-oxidases (Nox enzymes) and/or myeloperoxidase.
    Type: Application
    Filed: May 28, 2013
    Publication date: April 23, 2015
    Applicant: EMORY UNIVERSITY
    Inventors: John David Lambeth, Thota Ganesh, Susan M. Smith, Aiming Sun
  • Publication number: 20150080409
    Abstract: Embodiments of the present disclosure, in one aspect, relate to a 2,4-diaminoquinazoline compound, pharmaceutical compositions including a 2,4-diaminoquinazoline compound, methods of treatment of a condition (e.g., infection) or disease, methods of treatment using compositions or pharmaceutical compositions, and the like.
    Type: Application
    Filed: October 31, 2014
    Publication date: March 19, 2015
    Applicant: University of South Florida (A Florida Non-Profit Corporation)
    Inventors: Roman Manetsch, Lindsey Neil Shaw, Kurt Steven Van Horn, Whittney Nicole Burda
  • Publication number: 20150080392
    Abstract: A class of quinazoline derivatives or pharmaceutically acceptable salts or solvates thereof with novel structures is provided; meanwhile, a pharmaceutical composition comprising a pharmaceutically effective amount of said quinazoline derivatives or pharmaceutically acceptable salts or solvates thereof, and pharmaceutically acceptable excipients or additives is also provided. By modifying and transforming the quinazoline and screening of the transformed compounds on the activity of tyrosine kinase inhibition, most of the compounds have been found to possess inhibitory activity against one or several of EGFR, VEGFR-2, c-erbB-2, c-erbB-4, c-met, tie-2, PDGFR, c-src, lck, Zap70 and fyn kinases. The present invention has the advantages of reasonable design, broad source of and easy access to the raw materials, simple and easy operation of the preparation methods, mild reaction conditions, high yield of the products and being beneficial for industrial-scale production.
    Type: Application
    Filed: July 21, 2012
    Publication date: March 19, 2015
    Applicants: HANGZHOU MINSHENG PHARMACEUTICAL CO. LTD, HANGZHOU MINSHENG INSTITUTES FOR PHARMA RESEARCH
    Inventors: Shulong Wang, Jian Cai, Qiufu Ge, Dianwu Guo, Lan Yang, Binnan Huang, Zhenhua Liu, Zhonghua Peng, Ximing Shen, Feiyu Feng
  • Publication number: 20150072955
    Abstract: The present disclosure relates to compounds, which are useful for regulating the expression of apolipoprotein A-I (ApoA-I), and their use for treatment and prevention of cardiovascular disease and related disease states, including cholesterol- or lipid-related disorders, such as, for example, atherosclerosis.
    Type: Application
    Filed: October 14, 2014
    Publication date: March 12, 2015
    Applicant: Resverlogix Corp.
    Inventor: Henrik C. Hansen
  • Publication number: 20150071874
    Abstract: Methods and compositions containing a phorbol ester or a derivative of a phorbol ester are provided for the treatment of chronic and acute conditions. Such conditions may be caused by disease, be symptoms or sequelae of disease. Chronic and acute conditions may be due to viral infections such as HIV and AIDS, neoplastic diseases stroke, kidney disease, urinary incontinence, autoimmune disorders, Parkinson's disease, prostate hypertrophy, aging, or the treatment of such diseases. Additional compositions and methods are provided which employ a phorbol ester or derivative compound in combination with at least one additional agent to yield more effective treatment tools against acute and chronic conditions in mammalian subjects.
    Type: Application
    Filed: September 12, 2013
    Publication date: March 12, 2015
    Applicant: Biosuccess Biotech Co. Ltd.
    Inventors: Zheng Tao Han, Hung-Fong Chen
  • Publication number: 20150057263
    Abstract: This invention relates to quinazoline compounds of Formula (I) which are inhibitors of the histone lysine methyltransferase (HKMTase) EZH2, and to uses of such compounds as medicaments, in particular in the treatment of a disease or disorder in which inhibition of EZH2 provides a therapeutic or prophylactic effect.
    Type: Application
    Filed: March 19, 2013
    Publication date: February 26, 2015
    Inventors: Robert Brown, Matthew John Fuchter, Nadine Chapman-Rothe, Nitipol Srimongkolpithak, Joachim Caron, James Synder, Thota Ganesh, Jin Liu, Aiming Sun
  • Publication number: 20150050241
    Abstract: The present invention is directed to methods and compositions employing 9-(4-hydroxy-2-(hydroxymethyl)butyl)guanine (“H2G”) or derivatives or analogs thereof for the treatment of viral diseases, as well as for the treatment of other conditions, including, but not limited to, cancer, chronic fatigue syndrome, Alzheimer's disease, multiple sclerosis and Graves' disease. The H2G or derivative or analog thereof can be administered in a pharmaceutical composition and can be administered with an additional antiviral therapeutic agent or another agent for the treatment of other conditions.
    Type: Application
    Filed: October 30, 2014
    Publication date: February 19, 2015
    Inventors: Fred VOLINSKY, Steven Daniel DONG
  • Publication number: 20150045371
    Abstract: The invention relates to besylate and tosylate salts of {8-fluoro-2-[4-(3-methoxyphenyl)piperazin-1-yl]-3-[2-methoxy-5-(trifluoromethyl)phenyl]-3,4-dihydroquinazolin-4-yl}acetic acid and solvates thereof, to the use thereof in a method of treating and/or preventing virus infections, and to the use thereof to produce drugs for use in treating and/or preventing diseases, in particular use as antiviral agents, in particular against cytomegaloviruses.
    Type: Application
    Filed: February 28, 2013
    Publication date: February 12, 2015
    Applicant: AiCuris GmbH & Co. KG
    Inventors: Welljanne Maertens, Christian Schickaneder
  • Publication number: 20150038514
    Abstract: The invention relates to sodium and calcium salts of {8-fluoro-2-[4-(3-methoxyphenyl)piperazine-1-yl]-3-[2-methoxy-5-(trifluoromethyl)phenyl]-3,4-dihydroquinazoline-4-yl}acetic acid and solvates thereof, to the use thereof in a method of treatment and/or prophylaxis of virus infections and to the use thereof for producing drugs for use in methods of treatment and/or prophylaxis of diseases, more particularly the use thereof as antiviral agents, more particularly against cytomegaloviruses.
    Type: Application
    Filed: February 28, 2013
    Publication date: February 5, 2015
    Inventors: Alfons Grunenberg, Mathias Berwe, Birgit Keil, Edwin Aret, Kerstin Paulus, Wilfried Schwab
  • Publication number: 20150031705
    Abstract: Ophthalmic formulations are provided. The ophthalmic formulations include one or more active agents that act to optimize pupil light reflex while minimizing, or effectively eliminating, any undesired eye redness in response to application thereof. The active agents include, for example, alpha 1 antagonists, such as alpha 1a selective antagonists.
    Type: Application
    Filed: October 14, 2014
    Publication date: January 29, 2015
    Inventor: Gerald Horn
  • Publication number: 20150030588
    Abstract: The present invention provides for a method for treating a disease condition associated with PI3-kinase a and/or a receptor tyrosine kinase (RTK) in a subject. In another aspect, the invention provides for a method for treating a disease condition associated with PI3-kinase ? and/or an RTK in a subject. In yet another aspect, a method of inhibiting phosphorylation of Akt (S473) in a cell is set forth.
    Type: Application
    Filed: November 12, 2012
    Publication date: January 29, 2015
    Inventors: Katayoun Jessen, Xin Guo, Pingda Ren, Christian Rommel, Yi Liu
  • Publication number: 20150025071
    Abstract: Compounds of the formula I in which U, V and W have the meanings indicated in claim 1, are inhibitors of Tankyrase, and can be employed, inter alia, for the treatment of diseases such as cancer, cardiovascular diseases, central nervous system injury and different forms of inflammation.
    Type: Application
    Filed: January 14, 2013
    Publication date: January 22, 2015
    Applicant: MERCK PATENT GMBH
    Inventors: Hans-Peter Buchstaller, Christina Esdar, Birgitta Leuthner
  • Publication number: 20150025072
    Abstract: The present invention relates to quinazolinone compounds, processes for their preparation and their use as pharmaceutical agents for the treatment of Parkinson's disease (PD). The quinazolinone compounds are of general formula (I).
    Type: Application
    Filed: October 7, 2014
    Publication date: January 22, 2015
    Applicant: PRANA BIOTECHNOLOGY LIMITED
    Inventors: Penelope Jane HUGGINS, Jack Gordon PARSONS
  • Publication number: 20150018365
    Abstract: The present invention relates to a method for treating comorbid anxiety disorders and depression disorders, as well as for preventing depression disorders in individuals affected by anxiety disorders, by administering a therapeutically effective amount of the compound of general formula (I): wherein R1 is —OCH3 or —CN or suitable pharmaceutical salts, hydrates or anhydrates thereof.
    Type: Application
    Filed: April 14, 2014
    Publication date: January 15, 2015
    Applicants: ACHÉ LABORATÓRIOS FARMACÊUTICOS S.A., ACHÉ INTERNATIONAL (BVI) LTD.
    Inventors: Valter FREIRE TORRES RUSSO, Elisa MANNOCHIO DE SOUZA RUSSO
  • Publication number: 20150011542
    Abstract: Methods of treating adverse intestinal effects of a non-steroidal anti-inflammatory drugs (NSAID) in a subject by administering to the subject a therapeutically effective amount of a selective bacterial beta-glucuronidase inhibitor. The adverse intestinal effects to be treated include the formation or growth of an intestinal ulcer, increased intestinal permeability, the loss of intestinal villi, bleeding of the intestinal mucosa, and an increased intestinal inflammatory response. The methods are useful for treating the adverse effects of any NSAID such as propionic acid derivatives, carboxylic acid derivatives, enolic acid derivatives, fenamic acid derivatives, sulphonanilidies, and selective COX-2 inhibitors. The bacterial beta-glucuronidase inhibitors are selective for the inhibition of bacterial beta-glucuronidase enzymes and do not inhibit mammalian beta-glucuronidase.
    Type: Application
    Filed: January 11, 2013
    Publication date: January 8, 2015
    Inventor: Urs A. Boelsterli
  • Patent number: 8921321
    Abstract: The invention relates to therapeutic agents for use in the prevention or treatment of Alzheimer's disease. In particular the invention relates to use of inhibitors of cell cycle reentry and progression to the G1/S transition or inhibitors of progression of the cell cycle through the G1/S transition point in the prevention or treatment of Alzheimer's disease.
    Type: Grant
    Filed: November 30, 2012
    Date of Patent: December 30, 2014
    Assignee: Isis Innovation Ltd.
    Inventor: Zsuzsanna Nagy
  • Patent number: 8921362
    Abstract: Compounds of formula (I) in which: R1 is: R2 is —CH3 or —CH2CH3; or a pharmaceutically acceptable salt thereof. Pharmaceutical compositions including the compound of formula (I) and a pharmaceutically acceptable carrier. Processes for preparing the compound of formula (I). Methods of inhibiting a receptor tyrosine kinase in a subject in need thereof. Methods of inhibiting the growth of a tumor cell in a subject in need thereof. Methods of treating pancreatic cancer in a subject in need of treatment for pancreatic cancer. Methods of treating HER2 positive breast cancer in a subject in need of treatment for HER2 positive breast cancer. Methods of treating drug resistant non-small cell lung cancer in a subject in need of treatment for drug resistant non-small cell lung cancer. Each of these methods can include administering to the subject an effective amount of a compound of formula (I) or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: July 9, 2010
    Date of Patent: December 30, 2014
    Assignee: Natco Pharma Limited
    Inventors: Bhujanga rao Adibhatla Kali Satya, Ramanadham Jyothi Prasad, Bollepalli Nageshwara Rao, Nannapaneni Venkaiah Chowdary
  • Publication number: 20140378469
    Abstract: LKB1 mutation status and/or expression, YES expression and phosphorylation level; and/or CD24 expression are employed to predict melanoma prognosis and response to therapeutics. Inhibitors (including targeted inhibitors) of SRC family kinases (especially YES) are employed to treat melanoma.
    Type: Application
    Filed: February 6, 2013
    Publication date: December 25, 2014
    Inventors: Norman Edward Sharpless, Wenjin Liu, James Bear, Kimberly Monahan, Kwok-Kin Wong
  • Publication number: 20140371233
    Abstract: The present invention provides compositions and methods for treating and preventing an A?-modulated disease. In certain embodiments, the invention provides an inhibitor of Fyn tyrosine kinase, and methods of using the same. In certain embodiments, the inhibitor of the invention inhibits A? oligomer induced signaling and reduces or halts the progression of Alzheimer's Disease.
    Type: Application
    Filed: May 8, 2014
    Publication date: December 18, 2014
    Applicant: Yale University
    Inventor: Stephen M. Strittmatter
  • Publication number: 20140364420
    Abstract: The present invention relates to compounds useful as Chemokine Receptor antagonists. Compounds of general formula I are provided: or pharmaceutically acceptable salts thereof. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compounds and compositions for the inhibition of Chemokine Receptors and also for the treatment of various diseases, conditions, or disorders, including acute or chronic inflammatory disease, cancer or osteolytic bone disorders.
    Type: Application
    Filed: January 13, 2014
    Publication date: December 11, 2014
    Applicant: Millennium Pharmaceuticals, Inc.
    Inventors: Kenneth G. Carson, Shomir Ghosh, Prakash Raman, Francois Soucy, Qing Ye
  • Publication number: 20140357646
    Abstract: The invention relates to polymorphous crystal modifications of a DPP-IV inhibitor, the preparation thereof and the use thereof for preparing a medicament.
    Type: Application
    Filed: August 19, 2014
    Publication date: December 4, 2014
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: Peter SIEGER, Dirk KEMMER, Peter KOHLBAUER, Thomas NICOLA, Martin RENZ
  • Publication number: 20140343054
    Abstract: The invention relates to the use of compounds corresponding to formula (I) in which R2 and R3 together form, with the carbon atoms of the phenyl nucleus to which they are attached, a 6-membered nitrogenous heterocycle corresponding to one of the formulae (A), (B) and (C) in which the wavy lines represent the phenyl nucleus to which R2 and R3 are attached, or of a pharmaceutically acceptable salt thereof, for preparing a medicament for the treatment of bladder cancer.
    Type: Application
    Filed: January 3, 2013
    Publication date: November 20, 2014
    Inventors: Chantal Alcouffe, Corentin Herbert
  • Publication number: 20140336199
    Abstract: This invention is related to the alkyl-piperazine-phenyl 4(3H)-quinazolinones compounds of general formula (I) below: which are pharmacologicaly active and able to act on the 5-HT1A and 5-HT2A serotonin receptors in a manner that promotes the control, relief or cure of disorders associated with these receptors, and pharmaceutical compositions containing the compounds for the treatment of disorders associated with these receptors. These compounds and their pharmaceutical compositions are useful in the treatment of conditions such as depression, anxiety, phobias, addictions, aggressiveness, impulsiveness, panic, psychotic, eating and sleep disorders, obsessive-compulsive disorder and female sexual dysfunctions, among other disorders associated with these receptors.
    Type: Application
    Filed: May 5, 2014
    Publication date: November 13, 2014
    Applicants: ACHE LABORATORIOS FARMACEUTICOS S.A., ATC Trustees Abbot Building, 2nd FLoor, Road Town, ACHE INTERNATIONAL (BVI) LTD.
    Inventors: Valter FREIRE TORRES RUSSO, Elisa Mannochio De Souza Russo
  • Publication number: 20140309184
    Abstract: Embodiments of the present disclosure relate to methods and compositions for treating a subject with ovarian cancer. Some embodiments include treating a subject with a particular combination of chemotherapeutic agents.
    Type: Application
    Filed: July 20, 2012
    Publication date: October 16, 2014
    Applicant: UNIVERSITY OF SOUTH ALABAMA
    Inventors: Rodney P. Rocconi, Lalita Samant
  • Publication number: 20140303179
    Abstract: This invention is related to the alkyl-piperazine-phenyl 4 (3H)-quinazolinones general formula (I) compounds, pharmacologicaly active and able to act on the 5-HT1A and 5-HT2A serotonin receptors in a manner that promotes the control, relief or cure of disorders associated with these receptors, and pharmaceutical compositions containing the compounds for the treatment of disorders associated with these receptors. These compounds and their pharmaceutical compositions are useful in the treatment of conditions such as depression, anxiety, phobias, addictions, aggressiveness, impulsiveness, panic, psychotic, eating and sleep disorders, obsessive-compulsive disorder and female sexual dysfunctions, among other disorders associated with these receptors.
    Type: Application
    Filed: March 27, 2014
    Publication date: October 9, 2014
    Applicants: ACHÉ INTERNATIONAL (BVI) LTD., ACHÉ LABORATÓRIOS FARMACÊUTICOS S.A. ATC Trustees, Abbot Building, 2nd Floor, Road Town
    Inventors: Valter FREIRE TORRES RUSSO, Elisa MANNOCHIO DE SOUZA RUSSO
  • Publication number: 20140296247
    Abstract: Biologically active compounds, which are useful for treating a sexual disorder, are provided herein. Further provided are pharmaceutical compositions formulated for transdermal composition, which comprise a biologically active compound useful for treating a sexual disorder. The compounds and pharmaceutical compositions allow for a prolonged presence of a biologically active compound in plasma. Further provided herein are methods and uses of the compounds and pharmaceutical compositions described herein in the treatment of a sexual disorder, including female sexual disorders.
    Type: Application
    Filed: December 26, 2011
    Publication date: October 2, 2014
    Inventors: Vladimir Kogan, Leonid Lurya, Lev Tabachnik
  • Publication number: 20140296233
    Abstract: The present invention provides compounds, pharmaceutically acceptable compositions thereof, and methods of using the same.
    Type: Application
    Filed: March 14, 2014
    Publication date: October 2, 2014
    Applicants: Sanofi, Celgene Avilomics Research, Inc.
    Inventors: Laura Akullian D'Agostino, Robert Tjin Tham Sjin, Deqiang Niu, Joseph John McDonald, Zhendong Zhu, Haibo Liu, Hormoz Mazdiyasni, Russell C. Petter, Juswinder Singh, Matthieu Barrague, Alexandre Gross, Mark Munson