At Least Three Cyclos In The Polycyclo Ring System Patents (Class 514/224.5)
  • Patent number: 10675289
    Abstract: Described herein are methods and compositions for the treatment of pancreatic cancer in a subject in need thereof. The pancreatic cancer may be resistant to other therapeutic regimens. The methods may comprise administering ARDA compounds to the subject.
    Type: Grant
    Filed: October 2, 2015
    Date of Patent: June 9, 2020
    Assignee: University of Maryland, Baltimore
    Inventors: Vincent C. O. Njar, Puranik Purushottamachar, Andrew K. Kwegyir-Afful
  • Patent number: 10543200
    Abstract: Compositions and methods for inhibiting and/or sensitizing or re-sensitizing a parasite to an antiparasitic drug are provided. The compositions can comprise a an arylphenoxypropionate derivative, an aryloxyphenoxyacetate derivative, an aryloxyphenylacetate derivative, one or more substituted quinols, or a pharmaceutically acceptable salt, hydrate, or prodrug thereof, or a combination thereof in an amount and formulation sufficient to sensitize the parasite to the drug, treating infection of a patient by a parasite with a drug, or to prevent symptomatic infection of a patient by a parasite with a drug.
    Type: Grant
    Filed: August 26, 2016
    Date of Patent: January 28, 2020
    Assignee: The Texas A&M University System
    Inventors: Manchi C M Reddy, James C. Sacchettini, Nian E. Zhou, Billy F. McCutchen
  • Patent number: 10364247
    Abstract: The invention provides novel compounds and methods of using such compounds to treat or prevent cancer.
    Type: Grant
    Filed: April 21, 2015
    Date of Patent: July 30, 2019
    Assignees: Ruijin Hospital Affiliated to Shanghai Jiao Tong University School of Medicine, Xiamen University, Brandeis University
    Inventors: Ruibao Ren, Xianming Deng, Ping Liu, Bo Jiao, Wei Huang
  • Patent number: 10280177
    Abstract: Polyols stabilize polymorphous form of rifaximin, in particular the ? form. When polyols having at least two hydroxy groups are added to rifaximin powder, polymorph ? is stable and remains stable in time independently from the environment humidity. In this invention a method to prepare formulations constituted by pure and stable polymorphous forms able to give a pharmaceutical product is described.
    Type: Grant
    Filed: May 12, 2016
    Date of Patent: May 7, 2019
    Assignee: ALFASIGMA S.P.A.
    Inventors: Paola Maffei, Milena Bachetti, Giuseppe Bottoni, Giuseppe Claudio Viscomi
  • Patent number: 10278962
    Abstract: The present invention relates to a series of analogs of natural product Pyripyropene A represented by general formula I and a preparation method and use thereof. More particularly, the present invention relates to analogs of the natural product Pyripyropene A, a preparation method and use thereof as the acyl-CoA:cholesterol acyltransferase 2 (ACAT2) inhibitors for the treatment of cardiovascular diseases such as atherosclerosis and the like.
    Type: Grant
    Filed: March 3, 2016
    Date of Patent: May 7, 2019
    Assignee: SHANGHAI INSTITUTE OF MATERIA MEDICA, CHINESE ACADEMY OF SCIENCES
    Inventors: Fajun Nan, Boliang Li, Yang Zhan, Xiaowei Zhang, Ying Xiong, Xichan Hu, Yangming Zhang
  • Patent number: 9737610
    Abstract: The present invention relates to new rifaximin forms comprising solid dispersions of rifaximin, methods of making same and to their use in medicinal preparations and therapeutic methods.
    Type: Grant
    Filed: April 10, 2014
    Date of Patent: August 22, 2017
    Assignee: Salix Pharmaceuticals, Ltd
    Inventors: Jon Selbo, Jing Teng, Mohammed A. Kabir, Pam Golden
  • Patent number: 9741942
    Abstract: The present invention relates to compounds according to formula (1), a method for producing these compounds and electronic devices, in particular organic electroluminescent devices containing said compounds.
    Type: Grant
    Filed: September 13, 2013
    Date of Patent: August 22, 2017
    Assignee: Merck Patent GmbH
    Inventors: Philipp Stoessel, Amir Hossain Parham, Christof Pflumm, Anja Jatsch, Thomas Eberle, Jonas Valentin Kroeber
  • Patent number: 9216998
    Abstract: The present invention is directed to tricyclic indole derivatives, pharmaceutical compositions containing them and their use in the treatment of disorders and conditions modulated by endothelial lipase, for example, cardiovascular disorders.
    Type: Grant
    Filed: February 14, 2013
    Date of Patent: December 22, 2015
    Assignee: Janssen Pharmaceutica NV
    Inventors: Margery A. Connelly, Michael Greco, Hong Ye
  • Patent number: 9011882
    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: Grant
    Filed: February 13, 2013
    Date of Patent: April 21, 2015
    Assignee: The Board of Trustees of the Leland Stanford Junior University
    Inventors: Yohannes T. Ghebremariam, John P. Cooke
  • Patent number: 8957060
    Abstract: Disclosed herein are solutions and kits for tumescent antibiotic delivery. Embodiments of the solution comprise an antibiotic component, an anesthetic component and a vasoconstrictor component. In addition, a method of use is disclosed comprising subcutaneous delivery of the solution. The disclosed solution, kit and method of subcutaneous delivery can be used for a variety of surgical procedures including liposuction, mastectomy and others. The tumescent antibiotic solution can be administered to a patient in situations where establishing IV access is difficult, impossible, or undesirable. A variety of delivery methods appropriate for surgical settings, as well as for use by first responders are likewise disclosed.
    Type: Grant
    Filed: May 30, 2012
    Date of Patent: February 17, 2015
    Inventor: Jeffrey Alan Klein
  • Publication number: 20150031652
    Abstract: Disclosed are compounds of the following formula: in which R1, R2, R3, R4, R5, R6, R7, X, and t are defined in the specification. Also disclosed are pharmaceutical compositions, kits, and articles of manufacture, which contain the compounds, methods and intermediates useful for making the compounds, and methods of using the compounds to treat diseases, disorders, and conditions related to PARP activity.
    Type: Application
    Filed: August 1, 2014
    Publication date: January 29, 2015
    Applicant: TAKEDA PHARMACEUTICAL COMPANY LIMITED
    Inventors: Anthony R. Gangloff, Andrew John Jennings, Benjamin Jones, Andre A. Kiryanov
  • Publication number: 20150017263
    Abstract: The present disclosure is directed to methods of using fibroblast growth factor-inducible 14 (Fn14) antagonists to modulate activity at a TNF-like weak inducer of apoptosis (TWEAK) binding site on a cysteine-rich domain (CRD) of Fn14. The present disclosure also provides pharmaceutical compositions comprising synergistic combinations Fn14 antagonists and chemotherapeutic agents.
    Type: Application
    Filed: July 9, 2014
    Publication date: January 15, 2015
    Inventors: Nhan Tran, Nathalie Meurice, Harshil Dhruv
  • Publication number: 20140364424
    Abstract: The present invention relates to novel hepcidin antagonists, pharmaceutical compositions comprising them and the use thereof as medicaments for the use in the treatment of iron metabolism disorders, such as, in particular, iron deficiency diseases and anemias, in particular anemias in connection with chronic inflammatory diseases.
    Type: Application
    Filed: June 20, 2014
    Publication date: December 11, 2014
    Inventors: Wilm Buhr, Susanna Burckhardt, Franz Dürrenberger, Felix Funk, Peter O. Geisser, Vincent A. Corden, Stephen M. Courtney, Graham Dawson, Tara Davenport, Mark Slack, Mark P. Ridgill, Christopher J. Yarnold, Susan Boyce, Albertus A. Ellenbroek
  • Publication number: 20140336184
    Abstract: The present invention concerns methods and compositions regarding suppression of double stranded RNA-activated protein kinase (PKR) to enhance cognition in an individual. In specific cases, an inhibitor of PKR is provided to the individual such that cognition is enhanced thereby, including by enhancing memory, for example. Kits are encompassed in certain embodiments.
    Type: Application
    Filed: November 29, 2012
    Publication date: November 13, 2014
    Inventors: Mauro Costa-Mattioli, Ping Jun Zhu, Jeremy A. May
  • Publication number: 20140328795
    Abstract: In an embodiment of the present disclosure there is provided a method of inactivating enveloped DNA virus particles in a biological sample. In an embodiment, such a method comprises contacting the biological sample with an effective amount of an antiviral composition comprising PD 404,182 In some embodiments, the DNA virus is the Herpes Simplex virus-1 (HSV-1) or the Herpes Simplex Virus-2 (HSV-2). In another embodiment of the present disclosure, there is provided a method of treating, preventing, or reducing a viral infection caused by an enveloped DNA virus in a subject in need thereof. In yet another embodiment, there is provided a method of preventing transmission of a viral infection to a subject in need thereof.
    Type: Application
    Filed: September 10, 2013
    Publication date: November 6, 2014
    Applicants: The Texas A&M University System, The Scripps Research Institute
    Inventors: Zhilei Chen, Karrupiah Chockalingam, Ana M. Chamoun-Emanuelli, Rudo Simeon, Michael Bobardt, Philippe Gallay
  • Publication number: 20140315896
    Abstract: This invention relates to the field of biologically active compounds and specifically to phaeofungins, of the general formula (I) or a pharmacologically acceptable salt, solvate, hydrate or a pharmacologically acceptable formulation thereof, pharmaceutical compositions comprising these compounds, methods for the production of the phaeofungins and their use as fungicide, antibiotic as well as antitumor agent.
    Type: Application
    Filed: June 15, 2012
    Publication date: October 23, 2014
    Applicant: Leibniz-Institut fuer Naturstoff-Forschung und Infektionsbiologie E.V. Hans-Knoell-Institut (HKI)
    Inventors: Axel Brakhage, Hans-Martin Dahse, Christian Hertweck, Hans-Wilhelm Nuetzmann, Kirstin Scherlach
  • Publication number: 20140303144
    Abstract: Hydrogenated pyrido[4,3-b]indoles, pyrido[3,4-b]indoles and azepino[4,5-b]indoles are described. The compounds may bind to and are adrenergic receptor ?2B antagonists. The compounds may also bind to and antagonize adrenergic receptor ?2B. The compounds may find use in therapy, e.g., to (i) reduce blood pressure and/or (ii) promote renal blood flow and/or (iii) decrease or inhibit sodium reabsorption. The compounds may also be used to treat diseases or conditions that are, or are expected to be, responsive to a decrease in blood pressure. Use of the compounds to treat cardiovascular and renal disorders is particularly described.
    Type: Application
    Filed: February 17, 2012
    Publication date: October 9, 2014
    Applicant: Medivation Technologies, Inc.
    Inventors: Andrew Asher Protter, Sarvajit Chakravarty
  • Publication number: 20140227335
    Abstract: In some embodiments the present disclosure provides a method of inactivating a RNA virus of the family retroviridae in a biological sample. Such a method comprises contacting the biological sample with an effective amount of an antiviral composition comprising PD 404,182. In an embodiment of the present disclosure the RNA virus is selected from the group consisting of HIV pseudotyped lentiviruses, primary human immunodeficiency virus-1 isolates (HIV-1), human immunodeficiency virus-2 (HIV-2), and simian immunodeficiency virus (SIV). Further embodiments of the present disclosure pertain to a method of treating a subject infected by a RNA virus of the family retroviridae. Another embodiment of the present invention pertains to a method of preventing transmission of a RNA virus of the family retroviridae in a subject in need thereof.
    Type: Application
    Filed: September 10, 2013
    Publication date: August 14, 2014
    Inventors: Zhilei Chen, Karrupiah Chockalingam, Ana M. Chamoun-Emanuelli, Rudo Simeon, Michael Bobardt, Philippe Gallay
  • Publication number: 20140228353
    Abstract: Hydrogenated pyrido[4,3-b]indoles, pyrido[3,4-b]indoles and azepino[4,5-b]indoles are described. The compounds may bind to and are antagonists of the adrenergic receptor ?2A. The compounds may also bind to and are an antagonist of the adrenergic receptor ?2B; or the compounds are not antagonists of the adrenergic receptor ?2B and the compounds are administered in conjunction with a second agent that reduces, or is expected to reduce, blood pressure in an individual. The compounds may find use in therapy, e.g., to regulate blood glucose level, increase insulin secretion and treat diseases or conditions that are, or are expected to be, responsive to an increase in insulin production. Use of the compounds to treat type 2 diabetes is particularly described.
    Type: Application
    Filed: February 17, 2012
    Publication date: August 14, 2014
    Applicant: Medivation Technologies, Inc.
    Inventors: Andrew Asher Protter, Sarvvajit Chakravarty
  • Publication number: 20140213581
    Abstract: The present invention provides a new class of compounds useful for the modulation of beta-secretase enzyme (BACE) activity. The compounds have a general Formula I: wherein variables A5, A6, A8, R1, R2, R3, R7, X, Y, n and o of Formula I, independently, are defined herein. The invention also provides pharmaceutical compositions comprising the compounds, and corresponding uses of the compounds and compositions for treatment of disorders and/or conditions related to A-beta plaque formation and deposition, resulting from the biological activity of BACE. Such BACE mediated disorders include, for example, Alzheimer's Disease, cognitive deficits, cognitive impairments, schizophrenia and other central nervous system conditions. The invention further provides compounds of Formula II and sub-formula embodiments thereof, compounds of Formula III, intermediates and processes and methods useful for the preparation of compounds of Formulas I-III, and sub-Formulas thereof.
    Type: Application
    Filed: January 28, 2014
    Publication date: July 31, 2014
    Inventors: Ryan WHITE, Jennifer R. ALLEN, Oleg EPSTEIN, Fang-Tsao HONG, Zihao HUA, Jason Brooks HUMAN, Patricia LOPEZ, Philip R. OLIVIERI, Karina ROMERO, Laurie SCHENKEL, John STELLWAGEN, Nuria A. TAMAYO, Xiao Mei ZHENG
  • Publication number: 20140206663
    Abstract: The invention provides a compound of Formula (I) pharmaceutically acceptable salts, pro-drugs, biologically active metabolites, stereoisomers and isomers thereof wherein the variable are defined herein. The compounds of the invention are useful for treating immunological and oncological conditions.
    Type: Application
    Filed: March 19, 2014
    Publication date: July 24, 2014
    Inventors: Jianfei Wang, Eric C. Breinlinger, Martine Barth, Michael M. Friedman, Fabrice Guillier, Maria A. Argiriadi, Jeremy Edmunds, Dominique Potin, Adrian D. Hobson, Wentao Wu, Dominique Bonafoux, Didier Thomas, Dawn M. George, Linlin Dai, Yang Zhang
  • Publication number: 20140178503
    Abstract: The present invention relates to new cyclohexyl urea modulators of D2 receptors and/or modulators of D3 receptors, pharmaceutical compositions thereof, and methods of use thereof.
    Type: Application
    Filed: February 26, 2014
    Publication date: June 26, 2014
    Applicant: Auspex Pharmaceuticals, Inc.
    Inventors: Ronald C. Newbold, Chengzhi Zhang
  • Publication number: 20140171417
    Abstract: The present invention provides a compound of formula I or a pharmaceutically acceptable salt thereof; and its therapeutic uses. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.
    Type: Application
    Filed: December 17, 2013
    Publication date: June 19, 2014
    Applicant: NOVARTIS AG
    Inventors: Mahbub AHMED, Alexander ASHALL-KELLY, Louisa GUERITZ, Jeffrey MCKENNA, Joseph MCKENNA, Simon MUTTON, Rakesh PARMAR, Jon SHEPHERD, Paul WRIGHT
  • Publication number: 20140155369
    Abstract: An agent for the prophylaxis or treatment of stress urinary incontinence, which contains a substance that activates a serotonin 5-HT2C receptor, an agent for the prophylaxis or treatment of stress urinary incontinence, which contains a substance that stimulates an androgen binding site, and a method of screening for a drug for the prophylaxis or treatment of abdominal pressure incontinence, which includes electrostimulating the abdominal muscles or a nerve controlling them of an animal to increase the abdominal pressure, and measuring the leak point pressure at that time.
    Type: Application
    Filed: January 16, 2014
    Publication date: June 5, 2014
    Applicant: Takeda Pharmaceutical Company Limited
    Inventors: Izumi KAMO, Tadatoshi HASHIMOTO
  • Patent number: 8685963
    Abstract: The present invention relates to compounds with activity as BACE1 and NF?B modulators, and methods for treating, preventing, or ameliorating neurodegenerative diseases, such as Alzheimer's disease. The present invention is also directed to the treatment of diseases related to dysfunction of cell proliferation, the immune system and/or inflammation using such compounds or pharmaceutical compositions containing such candidate compounds.
    Type: Grant
    Filed: April 26, 2011
    Date of Patent: April 1, 2014
    Assignee: The Trustees of Columbia University in the city of New York
    Inventors: Donald W. Landry, Shi Xian Deng, Gangli Gong, Yuli Xie, Yidong Liu, K. Alison Rinderspacher
  • Publication number: 20140073631
    Abstract: Disclosed are guanidine and biguanidine derivatives which have anti-viral and antibacterial activity. Also disclosed are pharmaceutical compositions containing such compounds as an active ingredient, and anti-viral and anti-bacterial methods utilizing such compounds. Methods of treating infections using the guanidine and biguanidine derivatives are also disclosed.
    Type: Application
    Filed: September 10, 2013
    Publication date: March 13, 2014
    Applicant: Vymed Corporation
    Inventor: B. Vithal SHETTY
  • Patent number: 8658639
    Abstract: The present invention provides a compound of formula (I): wherein R1a is optionally substituted C1-6 alkyl, etc.; R1m is hydrogen atom, etc.; G1, G2, G3 and G4 are (i), etc. ((i) G1 is —N(R1b)—, G2 is —CO—, G3 is —C(R1c)(R1d)—, and G4 is oxygen, etc.); R1b is optionally substituted C1-6 alkyl, etc.; R1c and R1d are each independently optionally substituted C1-6 alkyl, etc.; R2 is optionally substituted C1-6 alkyl, etc.; R3a, R3b, R3c and R3d are each independently a group: -A-B (A is a single bond, etc., B is hydrogen atom, etc.), etc.; n is 1, etc.; R5 is C1-4 alkoxycarbonyl, etc., or a pharmaceutically acceptable salt thereof, which is useful as a renin inhibitor.
    Type: Grant
    Filed: June 24, 2010
    Date of Patent: February 25, 2014
    Assignee: Dainippon Sumitomo Pharma Co., Ltd
    Inventors: Satoshi Suetsugu, Nobuhisa Fukuda, Yoshio Nakai, Takashi Takada, Yohei Ikuma, Hiroyuki Nakahira
  • Publication number: 20140045687
    Abstract: The present invention relates to the use of dithiine-dicarboximide compounds of formula I as defined in the description, and the N-oxides, and salts thereof for combating harmful fungi and seed coated with at least one such compound. The invention also relates to novel dithiine-dicarboximides, processes and intermediates for preparing these compounds and also to compositions comprising at least one such compound.
    Type: Application
    Filed: April 10, 2012
    Publication date: February 13, 2014
    Applicant: BASF SE
    Inventors: Wassilios Grammenos, Nadege Boudet, Richard Riggs, Jochen Dietz, Egon Haden, Marcus Fehr
  • Publication number: 20140044789
    Abstract: This invention provides melanin nanoshells and their use for protection against radiation, particularly ionizing radiation, and electronic pulses, and methods of making materials comprising melanin nanoshells.
    Type: Application
    Filed: October 22, 2013
    Publication date: February 13, 2014
    Applicant: Albert Einstein College of Medicine of Yeshiva University
    Inventors: Ekaterina Dadachova, Arturo Casadevall
  • Patent number: 8604024
    Abstract: Compounds of formula (I), including pharmaceutically acceptable salts thereof, are set forth herein: wherein X is selected from the group of CH2, O, and NR2; m=0 or 1; R1 at each instance is selected from the group of halogen, hydroxy, amino, C1-4alkylamino, C1-4dialkylamino, haloC1-4 alkyl, CN, C1-C6 alkyl or cycloalkyl, C1-C6 alkoxy, and C2-C4 alkynyl; L is a bond, —NHCO—, —NH—, or L and Z together can be absent; Z is a C6-C10-aryl group or a 5-10 membered heterocyclic group which can be further substituted with from 0-3 substituents selected from the group of halogen, haloC1-4 alkoxy, 4-methoxyphenyl, hydroxy, amino, C1-4alkylamino, C1-4dialkylamino, haloC1-4 alkyl, CN, C1-C6 alkyl or cycloalkyl, C1-C6 alkoxy, and C2-C4 alkynyl; R2 is selected from the group of hydrogen, benzyl, C1-C6 alkyl or cycloalkyl, C1-C6 alkoxy, acetyl, and methanesulfonyl; and R3, R4 and R5 are independently selected from hydrogen or C1-4alkyl.
    Type: Grant
    Filed: May 22, 2012
    Date of Patent: December 10, 2013
    Assignee: Bristol-Myers Squibb Company
    Inventors: Lorin A. Thompson, III, Jianliang Shi, Yong-Jin Wu, Lawrence R. Marcin, Ramkumar Rajamani, Mendi A. Higgins
  • Publication number: 20130315825
    Abstract: Derivatives of phenothiazine, phenoxazine, and phenazine compounds and their use as ?-synuclein ligands are described. Also described are methods of using these compounds and their radiolabeled analogs for the detection, monitoring, and treatment of synucleinopathies, including Parkinson's disease.
    Type: Application
    Filed: May 3, 2013
    Publication date: November 28, 2013
    Applicant: Washington University
    Inventors: Zhude Tu, Robert Mach, Lihai Yu, Paul Kotzbauer
  • Publication number: 20130274239
    Abstract: Disclosed are compounds of the following formula: in which R1, R2, R3, R4, R5, R6, R7, X, and t are defined in the specification. Also disclosed are pharmaceutical compositions, kits, and articles of manufacture, which contain the compounds, methods and intermediates useful for making the compounds, and methods of using the compounds to treat diseases, disorders, and conditions related to PARP activity.
    Type: Application
    Filed: May 8, 2013
    Publication date: October 17, 2013
    Inventors: Anthony R. Gangloff, Andrew John Jennings, Benjamin Jones, Andre A. A. Kiryanov
  • 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
  • Publication number: 20130225558
    Abstract: This disclosure is directed to fused tetracyclic pyrido[4,3-b>]indole and pyrido[3,4-b]indole derivatives. 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: February 18, 2011
    Publication date: August 29, 2013
    Inventors: Sarvajit Chakravarty, Barry Patrick Hart, Rajendra Parasmal Jain
  • Publication number: 20130210806
    Abstract: The present invention is directed to tricyclic indole derivatives, pharmaceutical compositions containing them and their use in the treatment of disorders and conditions modulated by endothelial lipase, for example, cardiovascular disorders.
    Type: Application
    Filed: February 14, 2013
    Publication date: August 15, 2013
    Applicant: Janssen Pharmaceutica, NV
    Inventor: Janssen Pharmaceutica, NV
  • Publication number: 20130210803
    Abstract: This disclosure is directed to fused tetracyclic pyrido[4,3-b]indoles and pyrido[3,4-b]indoles. 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: February 18, 2011
    Publication date: August 15, 2013
    Inventors: Sarvajit Chakravarty, Barry Patrick Hart, Rajendra Parasmal Jain
  • Patent number: 8501733
    Abstract: A compound represented by the general formula (I): or a pharmaceutically acceptable salt thereof, has an A? production inhibitory effect or a BACE1 inhibitory effect and is useful as a prophylactic or therapeutic agent for a neurodegenerative disease caused by A? and typified by Alzheimer-type dementia.
    Type: Grant
    Filed: July 24, 2009
    Date of Patent: August 6, 2013
    Assignee: Eisai R&D Management Co., Ltd.
    Inventors: Takafumi Motoki, Toshihiko Kaneko, Noboru Yamamoto, Afzal Khan
  • Publication number: 20130131051
    Abstract: Compounds of formula (I), including pharmaceutically acceptable salts thereof, are set forth herein: wherein X is selected from the group of CH2, O, and NR2; m=0 or 1; R1 at each instance is selected from the group of halogen, hydroxy, amino, C1-4alkylamino, C1-4dialkylamino, haloC1-4 alkyl, CN, C1-C6 alkyl or cycloalkyl, C1-C6 alkoxy, and C2-C4 alkynyl; L is a bond, —NHCO—, —NH—, or L and Z together can be absent; Z is a C6-C10-aryl group or a 5-10 membered heterocyclic group which can be further substituted with from 0-3 substituents selected from the group of halogen, haloC1-4 alkoxy, 4-methoxyphenyl, hydroxy, amino, C1-4alkylamino, C1-4dialkylamino, haloC1-4 alkyl, CN, C1-C6 alkyl or cycloalkyl, C1-C6 alkoxy, and C2-C4 alkynyl; R2 is selected from the group of hydrogen, benzyl, C1-C6 alkyl or cycloalkyl, C1-C6 alkoxy, acetyl, and methanesulfonyl; and R3, R4 and R5 are independently selected from hydrogen or C1-4alkyl.
    Type: Application
    Filed: May 22, 2012
    Publication date: May 23, 2013
    Inventors: LORIN A. THOMPSON, III, Jianliang Shi, Yong-Jin Wu, Lawrence R. Marcin, Ramkumar Rajamani, Mendi A. Higgins
  • Patent number: 8389511
    Abstract: The present invention relates to a compound of the following formula (I) or a pharmaceutically acceptable salt thereof, being useful as a renin inhibitor. [wherein R1a is halogen, etc.; R1m is H, etc.; G1 is —N(R1b)—, etc.; G2 is —CO—, etc.; G3 is —C(R1c)(R1d)—, etc.; G4 is oxygen, etc.; R1b is optionally substituted C1-6 alkyl, etc.; R1c and R1d are independently the same or different, H, etc.; R3 is H, optionally substituted C1-6 alkyl, etc.; R3a, R3b, R3c and R3d are independently the same or different, and a group: -A-B (said A is single bond, etc., and said B is H, etc.), etc.; and n is 1, etc.
    Type: Grant
    Filed: December 19, 2008
    Date of Patent: March 5, 2013
    Assignee: Dainippon Sumitomo Pharma Co., Ltd.
    Inventors: Hiroyuki Nakahira, Yohei Ikuma, Nobuhisa Fukuda, Kozo Yoshida, Hidenori Kimura, Satoshi Suetsugu, Akira Fusano, Kiyoto Sawamura, Junya Ikeda, Yoshio Nakai
  • Publication number: 20130018045
    Abstract: The present invention relates to compounds of formula (I) or pharmaceutical acceptable salts, wherein R1, R2, R3, A, B, and n are defined in the description. The present invention relates also to compositions containing said compounds which are useful for inhibiting kinases such as wee-1 and methods of treating diseases such as cancer.
    Type: Application
    Filed: July 12, 2012
    Publication date: January 17, 2013
    Applicant: ABBOTT LABORATORIES
    Inventors: Keith W. Woods, Chunqui Lai, Thomas D. Penning, Julie M. Miyashiro
  • Patent number: 8288378
    Abstract: The present invention relates to the use of agents that inhibit the toxic effects of amyloid oligomers by increasing intracellular levels of phosphoinositol 4-phosphate (PI(4)P, or “PIP”) and/or phosphotidylinositol 4,5-biphosphate (PI(4,5)P2 or “PIP2”), the use of such agents for the treatment of neurodegenerative diseases, methods of treating neurodegenerative diseases by administration of agents which alter lipid metabolism, and methods of identifying agents which alter the association of presenilins with ?-secretase and lipid rafts.
    Type: Grant
    Filed: May 18, 2009
    Date of Patent: October 16, 2012
    Assignee: The Trustees of Columbia University in the City of New York
    Inventors: Tae-Wan Kim, Gilbert Di Paolo, Min Suk Kang, Diego Berman, Laura Beth Johnson McIntire
  • Publication number: 20120214803
    Abstract: The present invention relates to novel hepcidin antagonists, pharmaceutical compositions comprising them and the use thereof as medicaments for the use in the treatment of iron metabolism disorders, such as, in particular, iron deficiency diseases and anemias, in particular anemias in connection with chronic inflammatory diseases.
    Type: Application
    Filed: February 2, 2012
    Publication date: August 23, 2012
    Applicant: VIFOR (INTERNATIONAL) AG
    Inventors: Wilm Buhr, Susanna Burckhardt, Franz Dürrenberger, Felix Funk, Peter O. Geisser, Vincent A. Corden, Stephen M. Courtney, Graham Dawson, Tara Davenport, Mark Slack, Mark P. Ridgill, Chrostopher J. Yarnold, Susan Boyce, Albertus A. Ellenbroek
  • Publication number: 20120122804
    Abstract: The present invention relates to quinobenzoxazines analogs having the general formula: and pharmaceutically acceptable salts, esters and prodrugs thereof; wherein A, U, V, W, X and Z are substituents. The present invention also relates to methods for using such compounds.
    Type: Application
    Filed: March 30, 2007
    Publication date: May 17, 2012
    Applicant: Cylene Pharmaceuticals, Inc.
    Inventors: Jeffrey P. Whitten, Michael Schwaebe, Adam Siddiqui-Jain, Terrance Moran
  • Publication number: 20120122835
    Abstract: Disclosed are compounds of the following formula: in which R1, R2, R3, R4, R5, R6, R7, X, and t are defined in the specification. Also disclosed are pharmaceutical compositions, kits, and articles of manufacture, which contain the compounds, methods and intermediates useful for making the compounds, and methods of using the compounds to treat diseases, disorders, and conditions related to PARP activity.
    Type: Application
    Filed: January 18, 2012
    Publication date: May 17, 2012
    Applicant: TAKEDA PHARMACEUTICAL COMPANY LIMITED
    Inventors: Anthony R. Gangloff, Andrew John Jennings, Benjamin Jones, Andre A. Kiryanov
  • Publication number: 20120114740
    Abstract: Disclosed are formulations comprising multivesicular liposomes and one or more non-steroidal anti-inflammatory drugs which minimize the side effects of unencapsulated non-steroidal anti-inflammatory drugs while maintaining or improving efficacy. Methods of making and administering the formulations comprising multivesicular liposomes and one or more non-steroidal anti-inflammatory drugs and their use as medicaments are also provided.
    Type: Application
    Filed: October 27, 2011
    Publication date: May 10, 2012
    Applicant: PACIRA PHARMACEUTICALS, INC
    Inventors: Louie Daniel Garcia, Liangjin Zhu, William Joseph Lambert, Gary Patou
  • Publication number: 20120070409
    Abstract: The present invention relates to a tetracyclic fused heterocyclic compound represented by the following formula [I] wherein each symbol is as defined in the specification, or a pharmaceutically acceptable a salt thereof, and a hepatitis C virus (HCV) polymerase inhibitor and a therapeutic agent for hepatitis C containing this compound. The compound of the present invention shows an anti-HCV activity based on the HCV polymerase inhibitory activity, and useful as an agent for the prophylaxis or treatment of hepatitis C.
    Type: Application
    Filed: February 3, 2011
    Publication date: March 22, 2012
    Applicant: Japan Tobacco Inc.
    Inventors: Takahiro Oka, Kazutaka Ikegashira, Shintaro Hirashima, Hiroshi Yamanaka, Satoru Noji, Yasushi Niwa, Yoko Matsumoto, Toshihiro Sato, Izuru Ando, Yukihiro Nomura
  • Publication number: 20120064099
    Abstract: The present invention relates to compounds with activity as BACE1 and NF?B modulators, and methods for treating, preventing, or ameliorating neurodegenerative diseases, such as Alzheimer's disease. The present invention is also directed to the treatment of diseases related to dysfunction of cell proliferation, the immune system and/or inflammation using such compounds or pharmaceutical compositions containing such candidate compounds.
    Type: Application
    Filed: April 26, 2011
    Publication date: March 15, 2012
    Applicant: The Trustees of Columbia University in The City of New York
    Inventors: Donald W. Landry, Tae-Wan Kim, Shi Xian Deng, Gangli Gong, Jeremy C. Hwang, Yuli Xie, Yidong Liu, K. Alison Rinderspacher
  • Publication number: 20110319398
    Abstract: The disclosure relates to compounds and methods of inhibiting type three secretion system effector molecules, to methods of detecting compounds that inhibit Yops translocation, and to methods of treating or preventing infections by administering compounds described herein to a subject in need thereof.
    Type: Application
    Filed: June 1, 2011
    Publication date: December 29, 2011
    Applicant: TUFTS UNIVERSITY
    Inventor: Joan Mecsas
  • Publication number: 20110281855
    Abstract: The present invention provides a dosage form comprising at least one form of tapentadol, with or without a second analgesic, and at least one opioid antagonist, wherein tapentadol is present in an optimal or suboptimal amount and the said antagonist is present in an amount effective to improve the efficacy and or reduce the side effects of tapentadol. The present invention further provides a method of treating pain and pain related conditions by administering to a patient in need thereof, a dosage form comprising at least one form of tapentadol, with or without a second analgesic, and at least one opioid antagonist, wherein tapentadol is present in an optimal or suboptimal amount and the said antagonist is present in an amount effective to improve the efficacy and or reduce the side effects of tapentadol.
    Type: Application
    Filed: April 21, 2011
    Publication date: November 17, 2011
    Applicant: GRUENENTHAL GMBH
    Inventor: RAMESH SESHA
  • Publication number: 20110195950
    Abstract: The invention relates to compound of the formula I in which R1 represents an optionally substituted aryl group or an optionally substituted heteroaryl group; R2 represents hydrogen or a substituent different from hydrogen; R3 represents an optionally substituted aryl group, cycloalkyl group, heteroaryl group, heterocyclyl group; X1 represents O, S, NR4, CR42; X2 represents O, S, NR4, CR42; X3 represents O, S, NR4, CR42; X4 represents O, S, NR4, CR42; R4 represents hydrogen or a substituent different from hydrogen; R5 represents hydrogen or alkyl; Y represents O or S; m represents 0, 1, 2 or 3; n represents 0, 1, 2 or 3 in free base form or in acid addition salt form; to its preparation, to its use as medicament and to medicaments comprising it.
    Type: Application
    Filed: August 12, 2008
    Publication date: August 11, 2011
    Inventors: Samuel Hintermann, Konstanze Hurth, Marina Tintelnot-Blomley