Piperidinyl Or Tetrahydropyridyl Patents (Class 514/266.22)
  • Patent number: 10973823
    Abstract: Provided is a combined pharmaceutical composition of HF and an Artemisia annua sesquiterpene lactone compound for treating cancers. The active ingredients of the combined pharmaceutical composition consist of HF and an Artemisia annua sesquiterpene lactone compound. HF and ATS have significant synergistic effect. The activity of the combined pharmaceutical of HF and ATS is comparable or even higher than that of the anti-cancer drug 5-FU.
    Type: Grant
    Filed: September 27, 2016
    Date of Patent: April 13, 2021
    Assignee: Hong Kong Baptist University
    Inventors: Zhaoxiang Bian, Guoqing Chen, Ruihong Gong, Dajian Yang, Aiping Lyu
  • Patent number: 10874668
    Abstract: The invention relates to compositions for the treatment of obesity and related diseases comprising a) an active substance being not flibanserin, selected from the group consisting of active substances for the treatment of obesity and obesity related diseases and b) flibanserin, optionally in the form of pharmacologically acceptable acid addition salts thereof.
    Type: Grant
    Filed: June 3, 2019
    Date of Patent: December 29, 2020
    Assignee: Sprout Pharmaceuticals, Inc.
    Inventors: Angelo Ceci, Marcus Schindler
  • Patent number: 10821145
    Abstract: The present invention is based on a plurality of benefits from the extracts of mycelia of individual fungal species, and mixtures of species, to provide an armamentarium of defenses from multiple stressors in order to help bees survive a complex of symptoms collectively called colony collapse disorder (CCD). More particularly, the present invention utilizes specific concentrations of extracts from pure cultured mycelium from mushroom forming fungi to reduce harmful viruses in bees and to increase the longevity of bees.
    Type: Grant
    Filed: April 11, 2018
    Date of Patent: November 3, 2020
    Inventor: Paul E. Stamets
  • Patent number: 10646488
    Abstract: Conjugates of a cereblon-binding compound and compounds having modulatory activity against G12C mutant KRAS, HRAS or NRAS G12C proteins are provided. Methods associated with preparation and use of such conjugates, pharmaceutical compositions comprising such conjugates and methods to modulate the activity of G12C mutant KRAS, HRAS or NRAS G12C proteins for treatment of disorders, such as cancer, are also provided.
    Type: Grant
    Filed: July 13, 2017
    Date of Patent: May 12, 2020
    Assignee: ARAXES PHARMA LLC
    Inventors: Yi Liu, Liansheng Li, Pingda Ren
  • Patent number: 10633364
    Abstract: The invention relates to Crystal form I and Crystal form II of dihydrochloride of N-(4-((3-chloro-4-fluorophenyl)amino)-7-((7-methyl-7-azaspiro[3.5]nonan-2-yl)methoxy)quinazolin-6-yl)acrylamide represented by the following Formula (I), and preparation methods therefor, wherein the Crystal form I has an X-ray powder diffraction pattern having characteristic peaks at the 2? positions of 6.0±0.2°, 7.3±0.2°, 11.7±0.2°, 12.9±0.2°, 18.4±0.2°, 24.7±0.2°, and 26.3±0.2°, as determined by using Cu-K? radiation, and the Crystal form II has an X-ray powder diffraction pattern having characteristic peaks at the 2? positions of 5.0±0.2°, 7.0±0.2°, 10.1±0.2°, 17.0±0.2°, 26.0±0.2°, and 26.5±0.2°, as determined by using Cu-K? radiation.
    Type: Grant
    Filed: December 23, 2016
    Date of Patent: April 28, 2020
    Assignee: XUANZHU PHARMA CO., LTD.
    Inventors: Chutian Shu, Jinyuan Wang, Zhenhua Wang
  • Patent number: 10562889
    Abstract: This disclosure provides a process for preparing 1-(arylmethyl)quinazoline-2,4(1H,3H)-diones, specially provides a method for preparing the compound of Formula I, and the method comprises the step of reacting the compound of Formula II with the compound of Formula A in the presence of a condensation agent, an organic base and an organic solvent by condensation.
    Type: Grant
    Filed: March 31, 2017
    Date of Patent: February 18, 2020
    Assignee: IMPACT THERAPEUTICS, INC.
    Inventors: Suixiong Cai, Ping Huang
  • Patent number: 10335407
    Abstract: The invention relates to compositions for the treatment of obesity and related diseases comprising a) an active substance being not flibanserin, selected from the group consisting of active substances for the treatment of obesity and obesity related diseases and b) flibanserin, optionally in the form of pharmacologically acceptable acid addition salts thereof.
    Type: Grant
    Filed: July 31, 2017
    Date of Patent: July 2, 2019
    Assignee: Sprout Pharmaceuticals, Inc.
    Inventors: Angelo Ceci, Marcus Schindler
  • Patent number: 10155742
    Abstract: The present invention provides halofuginol, and derivatives and salts thereof, including diasteromerically enriched compositions thereof. The invention also provides pharmaceutical and cosmetic compositions thereof as well as methods for using halofuginol and derivatives thereof in treating chronic inflammatory diseases, autoimmune diseases, dry eye syndrome, fibrosis, scar formation, angiogenesis, viral infections, malaria, ischemic damage, transplant rejection, neurodegenerative diseases, T-cell neoplasms, and cosmetic conditions.
    Type: Grant
    Filed: January 11, 2013
    Date of Patent: December 18, 2018
    Assignees: President and Fellows of Harvard College, The General Hospital Corporation
    Inventors: Malcolm Whitman, Tracy Keller, Ralph Mazitschek
  • Patent number: 10011591
    Abstract: The present invention provides a crystalline Form I of afatinib dimaleate, its process for preparation and pharmaceutical composition thereof, and its use in the treatment of metastatic non-small cell lung cancer.
    Type: Grant
    Filed: October 1, 2015
    Date of Patent: July 3, 2018
    Assignee: Sun Pharmaceutical Industries Limited
    Inventors: Shravan Kumar Singh, Shyam Sunder Verma, Kaptan Singh, Mohan Prasad
  • Patent number: 9730927
    Abstract: The invention relates to compositions for the treatment of obesity and related diseases comprising a) an active substance being not flibanserin, selected from the group consisting of active substances for the treatment of obesity and obesity related diseases and b) flibanserin, optionally in the form of pharmacologically acceptable acid addition salts thereof.
    Type: Grant
    Filed: November 13, 2015
    Date of Patent: August 15, 2017
    Assignee: Sprout Pharmaceuticals, Inc.
    Inventors: Angelo Ceci, Marcus Schindler
  • Patent number: 9694015
    Abstract: Provided herein are methods of treating, preventing and/or managing locally advanced breast cancer, including inflammatory breast cancer, which comprise administering to a patient one or more immunomodulatory compounds or enantiomers or mixtures of enantiomers thereof, or pharmaceutically acceptable salts, solvates, hydrates, co-crystals, clathrates, or polymorphs thereof.
    Type: Grant
    Filed: September 9, 2013
    Date of Patent: July 4, 2017
    Assignee: Celgene Corporation
    Inventors: Anita Gandhi, Jorge Dimartino, Rajesh Chopra
  • Patent number: 9682955
    Abstract: The present invention is directed to quinazoline derivatives, pharmaceutical compositions containing said derivatives and their use in the treatment of disorders and conditions mediated by the CB-1 receptor; more particularly, in the treatment of disorders and conditions responsive to inverse agonism of the CB-1 receptor. For example, the compounds of the present invention are useful in the treatment of metabolic disorders.
    Type: Grant
    Filed: September 3, 2015
    Date of Patent: June 20, 2017
    Assignee: Janssen Pharmaceutica NV
    Inventors: Mark Joseph Macielag, Yue-Mei Zhang, Bart L. DeCorte, Michael N. Greco
  • Patent number: 9682952
    Abstract: Provided herein are deuterated isotopologues of 3-(5-amino-2-methyl-4-oxoquinazolin-3(4H)-yl)piperidine-2,6-dione, or enantiomers or mixtures of enantiomers thereof; or a pharmaceutically acceptable salt, solvate, cocrystal or polymorph thereof, and processes for making the same. Pharmaceutical compositions comprising the isotopes-enriched compounds, and methods of using such compounds are also provided.
    Type: Grant
    Filed: September 3, 2013
    Date of Patent: June 20, 2017
    Assignee: Celgene Corporation
    Inventors: Hon-Wah Man, William W. Leong
  • Patent number: 9606089
    Abstract: Impurities of lapatinib such as N-{3-chloro-4-[(2-fluorobenzyl)oxy]phenyl}-6-[5-({[2-(methylsulfonyl)ethyl]amino}methyl)furan-2-yl]quinazoline-4-amine compound of formula (I) or a salt thereof: and analytical methods for identifying and quantifying such impurities of Lapatinib and salts thereof are provided. Also provided is Lapatinib containing less than about 0.05 percent of this and related impurities and methods for preparing such pure forms of Lapatinib.
    Type: Grant
    Filed: September 10, 2014
    Date of Patent: March 28, 2017
    Assignee: F.I.S.—FABBRICA ITALIANA SINTETICI S.P.A.
    Inventors: Francesco Fontana, Alessandro Leganza, Sergio Osti
  • Patent number: 9586939
    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: Grant
    Filed: May 28, 2012
    Date of Patent: March 7, 2017
    Assignee: XUANZHU PHARMA CO., LTD.
    Inventors: Frank Wu, Aichen Wang
  • Patent number: 9540340
    Abstract: The invention provides 3-deuterium-enriched 3-(5-substituted-4-oxoquinazolin-3(4H)-yl)-piperidine-2,6-diones, deuterated derivatives thereof, stereoisomers thereof, pharmaceutically acceptable salt forms thereof, and methods of treatment using the same, such as in the treatment of cancer, an immune-related disease, or an inflammatory disease.
    Type: Grant
    Filed: January 14, 2014
    Date of Patent: January 10, 2017
    Assignee: DeuteRx, LLC
    Inventor: Sheila DeWitt
  • Patent number: 9474757
    Abstract: Provided herein are methods for treating or preventing a cancer, comprising administering an effective amount of a TOR kinase inhibitor and an effective amount of a 5-Substituted Quinazolinone Compound to a patient having a cancer.
    Type: Grant
    Filed: April 16, 2014
    Date of Patent: October 25, 2016
    Assignee: Signal Pharmaceuticals, LLC
    Inventors: Kristen Mae Hege, Rajesh Chopra
  • Patent number: 9339503
    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: Grant
    Filed: January 14, 2013
    Date of Patent: May 17, 2016
    Assignee: MERCK PATENT GMBH
    Inventors: Hans-Peter Buchstaller, Christina Esdar, Birgitta Leuthner
  • Patent number: 9303014
    Abstract: Provided herein are processes for the preparation of 3-(5-amino-2-methyl-4-oxoquinazolin-3(4H)-yl)piperidine-2,6-dione, or an enantiomer or a mixture of enantiomers thereof; or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: September 24, 2015
    Date of Patent: April 5, 2016
    Assignee: Celgene Corporation
    Inventors: Alexander L. Ruchelman, Benjamin M. Cohen, Anusuya Choudhury, Matthew M. Kreilein, William W. Leong, Hon-Wah Man
  • Patent number: 9284297
    Abstract: The present invention provides novel analogs and derivatives of halofuginone. The invention also provides pharmaceutical and cosmetic compositions thereof and methods for using halofuginone analogs in treating chronic inflammatory diseases, autoimmune diseases, dry eye syndrome, fibrosis, scar formation, angiogenesis, viral infections, ischemic damage, transplant and implant rejection, neurodegenerative diseases, and cosmetic applications.
    Type: Grant
    Filed: August 11, 2009
    Date of Patent: March 15, 2016
    Assignees: President and Fellows of Harvard College, Children's Medical Center Corporation
    Inventors: Tracy Keller, Ralph Mazitschek, Malcolm Whitman, Jinbo Lee, Mark S. Sundrud, Anjana Rao
  • Patent number: 9119854
    Abstract: Provided herein are methods for treating or preventing a cancer, comprising administering an effective amount of a substituted quinazolinone compound and an effective amount of N-(3-(5-fluoro-2-(4-(2-methoxyethoxy)phenylamino)pyrimidin-4-ylamino)phenyl)acrylamide to a patient having a cancer.
    Type: Grant
    Filed: May 2, 2014
    Date of Patent: September 1, 2015
    Assignee: Celgene Corporation
    Inventors: Rajesh Chopra, Kristen M. Hege
  • 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
  • Patent number: 9029378
    Abstract: Substituted bicyclic aromatic carboxamide and urea compounds as vanilloid receptor ligands, pharmaceutical compositions containing these compounds, and a method of using these compounds in the treatment and/or inhibition of pain and further diseases and/or disorders mediated at least in part via the vanilloid receptor 1 (VR1/TRPV1).
    Type: Grant
    Filed: July 25, 2012
    Date of Patent: May 12, 2015
    Assignee: Gruenenthal GmbH
    Inventors: Robert Frank, Thomas Christoph, Bernhard Lesch, Jeewoo Lee
  • Publication number: 20150125535
    Abstract: Described herein is certain crystalline forms of Compound 3, as well as pharmaceutical compositions employing the crystalline forms. Also provided are particles (e.g., nanoparticles) comprising such crystalline forms or pharmaceutical compositions. In certain examples, the particles are mucus penetrating particles (MPPs). The present invention further relates to methods of treating or preventing diseases using crystalline forms or pharmaceutical compositions.
    Type: Application
    Filed: October 31, 2014
    Publication date: May 7, 2015
    Inventors: Elizabeth Enlow, Mint Ngoc Nguyen, Winston Ong
  • Publication number: 20150126538
    Abstract: Provided herein are methods of treating, preventing and/or managing cancers, which comprise administering to a patient 3-(5-amino-2-methyl-4-oxo-4H-quinazolin-3-yl)-piperidine-2,6-dione, or an enantiomer or a mixture of enantiomers thereof, or a pharmaceutically acceptable salt, solvate, hydrate, co-crystal, clathrate, or polymorph thereof.
    Type: Application
    Filed: November 5, 2014
    Publication date: May 7, 2015
    Inventors: George W. MULLER, Peter H. SCHAFER, Hon-Wah MAN, Ling-Hua ZHANG, Anita GANDHI, Rajesh CHOPRA
  • Patent number: 9023859
    Abstract: A compound in combination with a pharmaceutically acceptable carrier, the compound having a formula: wherein: R1 is a member of the group consisting of hydrogen, halogen, nitro, benzo, lower alkyl, phenyl, and lower alkoxy; R2 is a member of the group consisting of hydroxy, acetoxy, and lower alkoxy; and R3 is a member of the group consisting of hydrogen and lower alkenoxy-carbonyl; and n is either 1 or 2; and pharmaceutically acceptable salts thereof; for use in treatment of or prevention of skeletal muscle fibrosis and/or for inducing skeletal muscle regeneration.
    Type: Grant
    Filed: March 1, 2013
    Date of Patent: May 5, 2015
    Assignees: State of Israel, Ministry of Agriculture, Agricultural Research Organization, Hadasit Medical Research Services and Development Company
    Inventors: Mark Pines, Arnon Nagler
  • Publication number: 20150119405
    Abstract: Described herein are inhibitors of FGFR-4, pharmaceutical compositions including such compounds, and methods of using such compounds and compositions.
    Type: Application
    Filed: October 23, 2014
    Publication date: April 30, 2015
    Applicant: BLUEPRINT MEDICINES CORPORATION
    Inventors: Neil Bifulco, Jr., Lucian V. DiPietro, Brian L. Hodous, Chandrasekhar V. Miduturu
  • Patent number: 9018191
    Abstract: Quinazoline derivatives of formula (I): wherein A is 5-membered heteroaryl containing a nitrogen atom and one or two further nitrogen atoms; compositions containing them, processes for their preparation and their use in therapy.
    Type: Grant
    Filed: August 21, 2012
    Date of Patent: April 28, 2015
    Assignee: AstraZeneca AB
    Inventors: Nicola Murdoch Heron, Andrew Austen Mortlock, Frederic Henri Jung, Georges Rene Pasquet
  • 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
  • Patent number: 9006240
    Abstract: The present invention provides a method of predicting the antitumor effect of an angiogenesis inhibitor. It is possible to predict the antitumor effect of an angiogenesis inhibitor by evaluating the EGF dependency of a tumor cell for proliferation and/or survival and using the EGF dependency as an indicator. Since the antitumor effect of an angiogenesis inhibitor correlates with the EGF dependency of a tumor cell for proliferation and/or survival, the angiogenesis inhibitors is capable of producing excellent antitumor effect when combined with a substance having EGF inhibitory activity.
    Type: Grant
    Filed: August 2, 2006
    Date of Patent: April 14, 2015
    Assignee: Eisai R&D Management Co., Ltd.
    Inventors: Toshimitsu Uenaka, Yuji Yamamoto, Junji Matsui
  • Publication number: 20150079079
    Abstract: The present invention provides compositions and methods of use in the treatment/prevention of chlamydial infection and/or diseases and disorders associated with chlamydial infection in a subject.
    Type: Application
    Filed: September 11, 2014
    Publication date: March 19, 2015
    Inventors: Allen W. Tsang, Cristina M. Furdui
  • Publication number: 20150080419
    Abstract: Provided are 5-substituted quinazolinone compounds, for example, of formula (I), and pharmaceutically acceptable salts, solvates, clathrates, stereoisomers, and prodrugs thereof. Methods of use for treating angiogenesis or cytokine related disorders, and pharmaceutical compositions of these compounds are disclosed.
    Type: Application
    Filed: November 24, 2014
    Publication date: March 19, 2015
    Inventors: George W. MULLER, Hon-Wah MAN
  • Patent number: 8969344
    Abstract: The present invention provides a method of predicting the antitumor effect of an angiogenesis inhibitor. It is possible to predict the antitumor effect of an angiogenesis inhibitor by evaluating the EOF dependency of a tumor cell for proliferation and/or survival and using the EGF dependency as an indicator. Since the antitumor effect of an angiogenesis inhibitor correlates with the EGF dependency of a tumor cell for proliferation and/or survival, the angiogenesis inhibitors is capable of producing excellent antitumor effect when combined with a substance having EGF inhibitory activity.
    Type: Grant
    Filed: September 21, 2012
    Date of Patent: March 3, 2015
    Assignee: Eisai R&D Management Co., Ltd.
    Inventors: Junji Matsui, Yuji Yamamoto, Toshimitsu Uenaka
  • 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: 20150057335
    Abstract: [PROBLEMS] To identify mutations that can serve as indicators for predicting the effectiveness of drug treatments in cancers such as lung cancer; to provide a means for detecting said mutations; and to provide a means for identifying, based on said mutations, patients with cancer or subjects with a risk of cancer, in which drugs targeting genes having said mutations or proteins encoded by said genes show a therapeutic effect. [MEANS FOR SOLVING] A method for detecting a gene fusion serving as a responsible mutation (driver mutation) for cancer, the method comprising the step of detecting any one of an EZR-ERBB4 fusion polynucleotide, a KIAA1468-RET fusion polynucleotide, a TRIM24-a BRAF fusion polynucleotide, a CD74-NRG1 fusion polynucleotide, and an SLC3A2-NRG1 fusion polynucleotide, or a polypeptide encoded thereby, in an isolated sample from a subject with cancer.
    Type: Application
    Filed: August 20, 2014
    Publication date: February 26, 2015
    Inventors: Takashi Kohno, Koji Tsuta, Kazuki Yasuda
  • Publication number: 20150056193
    Abstract: The present disclosure provides methods of that include detecting in a biological sample from a patient having or suspected of having cancer the presence of a polypeptide having ROS1 kinase activity or a polynucleotide encoding the same and detecting in the biological sample the presence of a mutant EGFR polypeptide or a polynucleotide encoding the same. In some aspects, the disclosure provides methods of treating a patient for cancer that include determining that a biological sample from a tumor in the patient includes a polypeptide having ROS1 kinase activity or a polynucleotide encoding the same and a mutant EGFR polypeptide or a polynucleotide encoding the same and administering to the patient a therapeutically effective amount of a ROS1 inhibitor and an EGFR inhibitor, thereby treating the patient for cancer.
    Type: Application
    Filed: April 18, 2013
    Publication date: February 26, 2015
    Applicant: CELL SIGNALING TECHNOLOGY, INC.
    Inventors: Katherine Eleanor Crosby, Victoria McGuinness Rimkunas, Matthew Ren Silver, Herbert Haack
  • Publication number: 20150057297
    Abstract: The present invention provides halofuginol, and derivatives and salts thereof, including diasteromerically enriched compositions thereof. The invention also provides pharmaceutical and cosmetic compositions thereof as well as methods for using halofuginol and derivatives thereof in treating chronic inflammatory diseases, autoimmune diseases, dry eye syndrome, fibrosis, scar formation, angiogenesis, viral infections, malaria, ischemic damage, transplant rejection, neurodegenerative diseases, T-cell neoplasms, and cosmetic conditions.
    Type: Application
    Filed: January 11, 2013
    Publication date: February 26, 2015
    Applicants: President and Fellows of Harvard College, The General Hospital Corporation d/b/a Massachusetts General Hospital
    Inventors: Malcolm Whitman, Tracy Keller, Ralph Mazitschek
  • Publication number: 20150050239
    Abstract: The present invention provides novel substituted pyrazolone compounds, pharmaceutical acceptable salts and formulations thereof useful in modulating the protein tyrosine kinase activity, and in modulating cellular activities such as proliferation, differentiation, apoptosis, migration and invasion. The invention also provides pharmaceutically acceptable compositions comprising such compounds and methods of using the compositions in the treatment of hyperproliferative disorders in mammals, especially humans.
    Type: Application
    Filed: July 19, 2013
    Publication date: February 19, 2015
    Applicants: Calitor Sciences, LLC, Sunshine Lake Pharma Co., Ltd.
    Inventors: Ning Xi, Yanjun Wu, Min Liao, Yanming Feng
  • Patent number: 8957081
    Abstract: The invention provides novel pyrimidine and pyridine derivatives and pharmaceutical compositions thereof, and methods for using such compounds. For example, the pyrimidine and pyridine derivatives of the invention may be used to treat, ameliorate or prevent a condition which responds to inhibition of anaplastic lymphoma kinase (ALK) activity, focal adhesion kinase (FAK), zeta-chain-associated protein kinase 70 (ZAP-70), insulin-like growth factor (IGF-1R), or a combination thereof.
    Type: Grant
    Filed: September 11, 2012
    Date of Patent: February 17, 2015
    Assignee: IRM LLC
    Inventors: Pierre-Yves Michellys, Wei Pei, Thomas H. Marsilje, III, Bei Chen, Tetsuo Uno, Yunho Jin, Tao Jiang
  • Publication number: 20150031677
    Abstract: Monomeric and dimeric trioxane thioacetals and methods of their use for treating subjects infected with malaria or other parasitic infectious diseases including, but not limited to, toxoplasmic infection; subjects afflicted with psychiatric conditions associated with toxoplasmic infection; and subjects afflicted with cancer.
    Type: Application
    Filed: February 28, 2013
    Publication date: January 29, 2015
    Applicant: THE JOHNS HOPKINS UNIVERSITY
    Inventors: Gary H. Posner, Alexander M. Jacobine, Rachel D. Slack, Jennifer R. Mazzone
  • Publication number: 20150025070
    Abstract: The present invention provides for compounds of formula (I): wherein R1-R5 and L are defined herein. The present invention also provides for pharmaceutical compositions and combinations comprising a compound of formula (I) as well as for the use of such compounds as tankyrase inhibitors and in the treatment of Wnt signaling and tankyrase 1 and 2 signaling related disorders which include, but are not limited to, cancer.
    Type: Application
    Filed: July 13, 2012
    Publication date: January 22, 2015
    Applicant: Novartis AG
    Inventors: Atwood Kim Cheung, Donovan Noel Chin, Jianmei Fan, Karen Marie Miller-Moslin, Michael David Shultz, Troy D. Smith, Ronald Charles Tomlinson, Bakary-Barry Toure, Michael Scott Visser
  • 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: 20150005278
    Abstract: This invention relates to novel sulfoximine substituted quinazoline derivatives of formula I wherein Ar, R1 and R2 are as defined in the description and claims, and their use as MNK1 (MNK1a or MNK1b) and/or MNK2 (MNK2a or MNK2b) kinase inhibitors, pharmaceutical compositions containing the same, and methods of using the same as agents for treatment or amelioration of MNK1 (MNK1a or MNK1b) and/or MNK2 (MNK2a or MNK2b) mediated disorders.
    Type: Application
    Filed: June 26, 2014
    Publication date: January 1, 2015
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: Andreas BLUM, Dirk GOTTSCHLING, Armin HECKEL, Joerg P. HEHN, Bernhard SCHMID, Dieter WIEDENMAYER
  • Patent number: 8921385
    Abstract: Provided are 5-substituted quinazolinone compounds, for example, of formula (I), and pharmaceutically acceptable salts, solvates, clathrates, stereoisomers, and prodrugs thereof. Methods of use for treating angiogenesis or cytokine related disorders, and pharmaceutical compositions of these compounds are disclosed.
    Type: Grant
    Filed: December 11, 2009
    Date of Patent: December 30, 2014
    Assignee: Celgene Corporation
    Inventors: George W. Muller, Hon-Wah Man
  • Publication number: 20140378484
    Abstract: Solid forms comprising 3-(5-amino-2-methyl-4-oxo-4H-quinazolin-3-yl)-piperidine-2,6-dione, compositions comprising the solid forms, methods of making the solid forms and methods of their uses are disclosed
    Type: Application
    Filed: June 27, 2014
    Publication date: December 25, 2014
    Inventors: George W. MULLER, Hon-Wah MAN, Benjamin M. COHEN, Ying LI, Jean XU, William W. LEONG
  • Publication number: 20140371243
    Abstract: The present invention relates to the use of a certain DPP-4 inhibitor along with angioplasty or stenting, and/or to its use for treating and/or preventing restenosis from angioplasty or stenting.
    Type: Application
    Filed: June 13, 2014
    Publication date: December 18, 2014
    Applicant: Boehringer Ingelheim International GmbH
    Inventors: Thomas KLEIN, Takashi NOMIYAMA, Yuichi TERAWAKI, Toshihiko YANASE
  • Publication number: 20140371247
    Abstract: The present invention relates to quinazolin-4-one compounds of formula (I?), their process of preparation and uses thereof. These compounds are useful as selective and reversible inhibitors of ubiquitin specific proteases, particularly USP7, for treating e.g. cancer, neurodegenerative diseases, inflammatory disorders and viral infections.
    Type: Application
    Filed: August 29, 2012
    Publication date: December 18, 2014
    Applicant: HYBRIGENICS SA
    Inventors: Frédéric Colland, Marie-Edith Gourdel
  • Publication number: 20140371209
    Abstract: Compounds of formula (I) or (II) can modulate the activity of SIP receptors.
    Type: Application
    Filed: February 3, 2012
    Publication date: December 18, 2014
    Inventors: Jermaine Thomas, Sha Mi, Edward Yin-Shiang Lin, Guo Zhu Zheng, Bin Ma, Kevin Guckian, Gnanasambandam Kumaravel
  • Patent number: 8906932
    Abstract: Provided herein are methods of treating, preventing and/or managing cancers, which comprise administering to a patient 3-(5-amino-2-methyl-4-oxo-4H-quinazolin-3-yl)-piperidine-2,6-dione, or an enantiomer or a mixture of enantiomers thereof, or a pharmaceutically acceptable salt, solvate, hydrate, co-crystal, clathrate, or polymorph thereof.
    Type: Grant
    Filed: March 9, 2012
    Date of Patent: December 9, 2014
    Assignee: Celgene Corporation
    Inventors: George W. Muller, Peter H. Schafer, Hon-Wah Man, Ling-Hua Zhang, Anita Gandhi, Rajesh Chopra