Polycyclo Ring System Having The Additional Six-membered Nitrogen Hetero Ring As One Of The Cyclos Patents (Class 514/253.02)
  • Patent number: 11154549
    Abstract: The invention provides pharmaceutical compositions comprising macromolecular gastrointestinal enzyme-labile opioid prodrugs, co-formulated with small-molecule and/or macromolecular gastrointestinal enzyme inhibitors. The macromolecular constructs are minimally absorbed from the GI tract, and can produce non-linear pharmacokinetic profiles of the delivered opioid agonist following oral ingestion. An optional macromolecular opioid antagonist may also be present in compositions of the invention to discourage tampering by potential abusers.
    Type: Grant
    Filed: April 17, 2019
    Date of Patent: October 26, 2021
    Assignee: ELYSIUM THERAPEUTICS, INC.
    Inventor: Thomas E. Jenkins
  • Patent number: 11129825
    Abstract: The invention provides compositions and methods for the treatment or prevention of pain. The invention provides constructs whereby hydrolysis of the construct by a specified gastrointestinal enzyme directly, or indirectly, releases an opioid when taken orally as prescribed. The gastrointestinal enzyme mediated release of opioid from constructs of the invention is designed to be attenuated in vivo via a saturation or inhibition mechanism when overdoses are ingested. The invention further provides constructs that are highly resistant to oral overdose, chemical tampering, and abuse via non-oral routes of administration.
    Type: Grant
    Filed: February 26, 2019
    Date of Patent: September 28, 2021
    Assignee: ELYSIUM THERAPEUTICS, INC.
    Inventor: Thomas E. Jenkins
  • Patent number: 10335406
    Abstract: The invention provides pharmaceutical compositions comprising macromolecular gastrointestinal enzyme-labile opioid prodrugs, co-formulated with small-molecule and/or macromolecular gastrointestinal enzyme inhibitors. The macromolecular constructs are minimally absorbed from the GI tract, and can produce non-linear pharmacokinetic profiles of the delivered opioid agonist following oral ingestion. An optional macromolecular opioid antagonist may also be present in compositions of the invention to discourage tampering by potential abusers.
    Type: Grant
    Filed: October 26, 2017
    Date of Patent: July 2, 2019
    Assignee: Elysium Therapeutics, Inc.
    Inventor: Thomas E. Jenkins
  • Patent number: 10251878
    Abstract: The invention provides compositions and methods for the treatment or prevention of pain. The invention provides constructs whereby hydrolysis of the construct by a specified gastrointestinal enzyme directly, or indirectly, releases an opioid when taken orally as prescribed. The gastrointestinal enzyme mediated release of opioid from constructs of the invention is designed to be attenuated in vivo via a saturation or inhibition mechanism when overdoses are ingested. The invention further provides constructs that are highly resistant to oral overdose, chemical tampering, and abuse via non-oral routes of administration.
    Type: Grant
    Filed: August 22, 2017
    Date of Patent: April 9, 2019
    Assignee: Elysium Therapeutics, Inc.
    Inventor: Thomas E. Jenkins
  • Patent number: 9382542
    Abstract: The present disclosure relates to methods of treating a patient suffering from or at risk of developing an ocular disease, disorder or injury, and includes treatment regimens using a double-stranded RNA compound that down-regulates CASP2 expression, or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: January 3, 2013
    Date of Patent: July 5, 2016
    Assignee: Quark Pharmaceuticals, Inc.
    Inventors: Shai Erlich, James D. Thompson, Rabia Ozden
  • Patent number: 9181193
    Abstract: An indenoquinolone compounds of Formula (A) is disclosed, wherein the definition of each group is described in the description. These compounds may specifically inhibit topoisomerase I, and they have good activities against many kinds of human tumor cells, such as lung cancer, colon cancer, breast cancer, liver cancer and the like. They can be used in the manufacture of antitumor drugs. The method for preparing the compound of formula (A), and pharmaceutical compositions containing such compounds and the use in the manufacture of antitumor drugs are also disclosed.
    Type: Grant
    Filed: May 17, 2011
    Date of Patent: November 10, 2015
    Assignee: Second Military Medical University, PLA
    Inventors: Yunlong Song, Xiaodan Fu, Yunpeng Qi, Yves G. Pommier
  • Publication number: 20150139905
    Abstract: The present invention provides pharmacological compounds including an effector moiety conjugated to a binding moiety that directs the effector moiety to a biological target of interest. Likewise, the present invention provides compositions, kits, and methods (e.g., therapeutic, diagnostic, and imaging) including the compounds. The compounds can be described as a protein interacting binding moiety-drug conjugate (SDC-TRAP) compounds, which include a protein interacting binding moiety and an effector moiety. For example, in certain embodiments directed to treating cancer, the SDC-TRAP can include an Hsp90 inhibitor conjugated to a cytotoxic agent as the effector moiety.
    Type: Application
    Filed: October 9, 2014
    Publication date: May 21, 2015
    Inventors: Dinesh Chimmanamada, Weiwen Ying
  • Publication number: 20150141419
    Abstract: The present invention relates to a diarylo[a,g]quinolizidine compound of formula (I), enantiomer, diastereoisomer, racemate, mixture, pharmaceutically acceptable salt, crystalline hydrate or solvate thereof; the preparation method thereof, and uses thereof in preparing an experimental model drugs related to dopamine receptors and 5-HT receptors or a medicament for treating or preventing a disease related to dopamine receptors and 5-HT receptors.
    Type: Application
    Filed: May 9, 2013
    Publication date: May 21, 2015
    Inventors: Hong Liu, Xuechu Zhen, Haifeng Sun, Liyuan Zhu, Wangke Qian, Leiping Yu, Zeng Li, Shengbin Zhou, Wenxian Cai, Hualiang Jiang, Kaixian Chen
  • Patent number: 9034869
    Abstract: This disclosure relates to new compounds that may be used to modulate a histamine receptor in an individual. Novel compounds are described, including new bridged heterocyclic[4,3-b]indole compounds. Pharmaceutical compositions are also provided. Pharmaceutical compositions comprising the compounds are also provided, as are methods of using the compounds in a variety of therapeutic applications, including the treatment of a cognitive disorder, psychotic disorder, neurotransmitter-mediated disorder and/or a neuronal disorder.
    Type: Grant
    Filed: March 7, 2013
    Date of Patent: May 19, 2015
    Assignee: Medivation Technologies, Inc.
    Inventors: David T. Hung, Andrew Asher Protter, Sarvajit Chakravarty, Rajendra Parasmal Jain
  • Patent number: 8999977
    Abstract: This disclosure relates to new compounds that may be used to modulate a histamine receptor in an individual. Novel compounds are described, including new bridged heterocyclic [4,3-b]indole compounds. Pharmaceutical compositions are also provided. Pharmaceutical compositions comprising the compounds are also provided, as are methods of using the compounds in a variety of therapeutic applications, including the treatment of a cognitive disorder, psychotic disorder, neurotransmitter-mediated disorder and/or a neuronal disorder.
    Type: Grant
    Filed: March 8, 2013
    Date of Patent: April 7, 2015
    Assignee: Medivation Technologies, Inc.
    Inventors: David T. Hung, Andrew Asher Protter, Sarvajit Chakravarty, Rajendra Parasmal Jain
  • Patent number: 8980909
    Abstract: The disclosure includes hydroxamic compounds of Formula I: (Formula I) wherein Z, L, R1, R2, and R3 are defined herein. Also disclosed is a method for treating a neoplastic disease or an immune disease with these compounds.
    Type: Grant
    Filed: January 6, 2012
    Date of Patent: March 17, 2015
    Assignee: Crystal Biopharmaceutical LLC
    Inventors: Yi Chen, Yu Chen
  • Publication number: 20150038438
    Abstract: The present description relates to compounds and forms and pharmaceutical compositions thereof and methods for use thereof to treat or ameliorate bacterial infections caused by wild-type and multi-drug resistant Gram-negative and Gram-positive pathogens.
    Type: Application
    Filed: August 29, 2012
    Publication date: February 5, 2015
    Inventors: Arthur Branstrom, Vara Prasad Venkata Nagendra Josyula, Michael Andrew Arnold, Aleksey I. Gerasyuto, Gary Karp, Jiashi Wang, Guangming Chen, Olya Ginzburg, Song Huang, Jana Narasimhan, Srinivasa Peddi, Sean Wesley Smith, Anthony Allan Turpoff, Matthew G. Woll, Nanjing Zhang, Xiaoyan Zhang
  • Publication number: 20140357647
    Abstract: The present invention belongs to the field of natural medicine and pharmaceutical chemistry and specifically relates to novel 7-substituted fangchinoline derivatives of formula (I) and a pharmaceutically acceptable adduct, complex and salt thereof, to a process for the preparation of these compounds, pharmaceutical compositions containing such compounds and their use in preparing antineoplastic medicaments.
    Type: Application
    Filed: January 21, 2013
    Publication date: December 4, 2014
    Applicant: HANGZHOU BENSHENG PHARMACEUTICAL CO., LTD.
    Inventors: Frank Rong, Rongzhen Xu, Hongxi Lai, Fuwen Xie
  • Publication number: 20140343015
    Abstract: A morphinan derivative represented by the following general formula (I) (in the formula, R1 represents hydrogen, C1-6 alkyl, cycloalkylalkyl (the cycloalkyl moiety has 3 to 6 carbon atoms, and the alkylene moiety has 1 to 5 carbon atoms), aralkyl (the aryl moiety has 6 to 10 carbon atoms, and the alkylene moiety has 1 to 5 carbon atoms) and the like, R2 represents hydrogen, C1-6 alkyl, C3-6 cycloalkyl, C6-10 aryl, aralkyl (the aryl moiety has 6 to 10 carbon atoms, and the alkylene moiety has 1 to 5 carbon atoms) and the like, R3, R4 and R5 represent hydrogen, hydroxy, carbamoyl, C1-6 alkoxy, C6-10 aryloxy and the like, R6a, R6b, R7, R8, R9, and R10 represent hydrogen and the like, X represents O or CH2, and Y represents C?O, SO2, an atomic bond and the like), or an acid addition salt thereof is used as an analgesic.
    Type: Application
    Filed: September 7, 2012
    Publication date: November 20, 2014
    Applicants: NIPPON CHEMIPHAR CO., LTD., THE KITASATO INSTITUTE
    Inventors: Hiroshi Nagase, Hideaki Fujii, Eriko Nakata, Yoshikazu Watanabe, Toshihiro Takahashi
  • Publication number: 20140343047
    Abstract: The present invention belongs to the field of natural medicine and pharmaceutical chemistry and specifically relates to novel 5-substituted tetrandrine derivatives of formula (I) and a pharmaceutically acceptable adduct, complex and salt thereof, to a process for the preparation of these compounds, pharmaceutical compositions containing such compounds and their use in preparing antineoplastic medicaments.
    Type: Application
    Filed: August 20, 2012
    Publication date: November 20, 2014
    Applicant: HANGZHOU BENSHENG PHARMACEUTICAL CO., LTD.
    Inventors: Rongzhen Xu, Frank Rong, Fuwen Xie, Hongxi Lai
  • Publication number: 20140336188
    Abstract: N-Substituted indenoisoquinoline compounds, and pharmaceutical formulations of N-substituted indenoisoquinoline compounds are described. Also described are processes for preparing N-substituted indenoisoquinoline compounds. Also described are methods for treating cancer in mammals using the described N-substituted indenoisoquinoline compounds or pharmaceutical formulations thereof.
    Type: Application
    Filed: July 24, 2014
    Publication date: November 13, 2014
    Applicants: PURDUE RESEARCH FOUNDATION, THE GOVERNMENT OF THE UNITED STATES OF AMERICA AS REPRESENTED BY THE SECRETSR
    Inventors: Mark S. CUSHMAN, Andrew E. MORRELL, Muthukaman NAGARAJAN, Yves G. POMMIER, Keli K. AGAMA, Smitha ANTONY
  • Publication number: 20140308360
    Abstract: The invention provides multivalent surface-crosslinked micelle (SCM) particles, crosslinked reverse micelle (CRM) particles, and methods of making and using them. The SCM particles can be used, for example, to inhibit a virus or bacteria from binding to a host cell. The inhibition can be used in therapy for the flu, cancer, or AIDS. The CRM particles can be used, for example, to prepare metal nanoparticles or metal alloy nanoparticles, or they can be used in catalytic reactions.
    Type: Application
    Filed: June 26, 2014
    Publication date: October 16, 2014
    Inventor: Yan Zhao
  • Patent number: 8841300
    Abstract: A new treatment methodology and pharmacological composition for the treatment and remission of Parkinson's Disease and other neurological diseases are provided. The medication and treatment are based on the use of a combination of a phosphodiesterase inhibitor medication, commonly used to treat male erectile dysfunction, and a high-dose of serotonergic synaptic reuptake inhibitor medication, commonly used to treat depression, anxiety disorders, obsessive compulsive disorder and various panic phobias. The treatment regime is based upon the discovery that the primary cause of PD and various other related neurological conditions is dysfunction in the serotonergic pathways involving the brainstem, nucleus of Raphe, and various projecting serotonergic fibers.
    Type: Grant
    Filed: October 2, 2006
    Date of Patent: September 23, 2014
    Inventor: Jerry M. Held
  • Publication number: 20140275017
    Abstract: Compounds of Formula I: (wherein variables A1, A2, A3, ring-B, m, n, J, E1, E2, E3, R5, RPG and Y are as described herein), which are useful as antagonists of CGRP receptors, and useful in the treatment or prevention of diseases in which CGRP receptors are involved, such as headache, and in particular migraine and cluster headache. The invention is also directed to pharmaceutical compositions comprising the compounds of formula (I) and the use of these compounds and compositions in the prevention or treatment of diseases in which CGRP receptors are involved.
    Type: Application
    Filed: June 3, 2014
    Publication date: September 18, 2014
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Craig A. Stump, Amy G. Quigley, Cory R. Theberge, Michael R. Wood
  • Patent number: 8828988
    Abstract: The present invention is directed to a compound represented by Structural Formula (I): or a pharmaceutically acceptable salt thereof. The variables for Structural Formula I are defined herein. Also described is a pharmaceutical composition comprising the compound of Structural Formula I and its therapeutic use.
    Type: Grant
    Filed: December 31, 2012
    Date of Patent: September 9, 2014
    Assignee: Tetraphase Pharmaceuticals, Inc.
    Inventors: Roger B. Clark, Minsheng He, Louis Plamondon, Xiao-Yi Xiao, Magnus P. Rönn
  • Patent number: 8809326
    Abstract: Disclosed are novel substituted 2H-isoquinolin-1-one and 3H-quinazolin-4-one derivatives useful as inhibitors of Rho kinase and for treating a variety of diseases and disorders that are mediated or sustained through the activity of Rho kinase, including cardiovascular diseases, pharmaceutical compositions comprising such compounds, methods for using such compounds and processes for making such compounds.
    Type: Grant
    Filed: September 18, 2007
    Date of Patent: August 19, 2014
    Assignee: Aerie Pharmaceuticals, Inc.
    Inventors: Todd Bosanac, John David Ginn, Eugene Richard Hickey, Thomas Martin Kirrane, Jr., Weimin Liu, Anthony S. Prokopowicz, Sabine K. Schlyer, Cheng-Kon Shih, Roger John Snow, Michael Robert Turner, Frank Wu, Erick Richard Young
  • Patent number: 8802681
    Abstract: Pharmaceutical compositions and their methods of use are provided, where the pharmaceutical compositions comprise a phenolic opioid prodrug that provides enzymatically-controlled release of a phenolic opioid, and an enzyme inhibitor that interacts with the enzyme(s) that mediates the enzymatically-controlled release of the phenolic opioid from the prodrug so as to attenuate enzymatic cleavage of the prodrug.
    Type: Grant
    Filed: October 16, 2009
    Date of Patent: August 12, 2014
    Assignee: Signature Therapeutics, Inc.
    Inventors: Thomas E. Jenkins, Julie D. Seroogy, Jonathan W. Wray
  • Publication number: 20140031362
    Abstract: The present invention relates to compounds of following general formula (I): and to the pharmaceutically acceptable salts of same, the tautomers of same, the stereoisomers or mixture of stereoisomers in any proportions of same, such as a mixture of enantiomers, notably a racemic mixture, as well as to methods for preparing same and uses of same, notably as an antineoplastic agent.
    Type: Application
    Filed: April 12, 2012
    Publication date: January 30, 2014
    Applicant: PIERRE FABRE MEDICAMENT
    Inventors: Rémi Rabot, Karim Bedjeguelal, El Bachir Kaloun, Philippe Schmitt, Nicolas Rahier, Patrice Mayer, Emmanuel Fournier
  • Publication number: 20140024643
    Abstract: This disclosure relates to new compounds that may be used to modulate a histamine receptor in an individual. Novel compounds are described, including new bridged heterocyclic [4,3-b]indole compounds. Pharmaceutical compositions are also provided. Pharmaceutical compositions comprising the compounds are also provided, as are methods of using the compounds in a variety of therapeutic applications, including the treatment of a cognitive disorder, psychotic disorder, neurotransmitter-mediated disorder and/or a neuronal disorder.
    Type: Application
    Filed: September 20, 2013
    Publication date: January 23, 2014
    Applicant: MEDIVATION TECHNOLOGIES, INC.
    Inventors: David T. HUNG, Andrew Asher PROTTER, Sarvajit CHAKRAVARTY, Rajendra Parasmal JAIN
  • Patent number: 8580792
    Abstract: A synergistically effective combination of an anti-cancer agent and a therapeutic compound, such as an mTOR-Rictor complex inhibitor, a Serine 473 phosphorylation inhibitor, an AKT2 inhibitor, or a combination thereof, for use in the treatment of cancer, and methods and uses thereof. Also included are methods and uses of a thiosemicarbazone for treating a cancer in a mammal in need thereof characterized by over-expression of RAS, by an EGFR mutation, and/or by over-expression of AKT2.
    Type: Grant
    Filed: February 1, 2012
    Date of Patent: November 12, 2013
    Assignee: Critical Outcome Technologies Inc.
    Inventor: Wayne R. Danter
  • Publication number: 20130281402
    Abstract: The disclosure includes hydroxamic compounds of Formula I: (Formula I) wherein Z, L, R1, R2, and R3 are defined herein. Also disclosed is a method for treating a neoplastic disease or an immune disease with these compounds.
    Type: Application
    Filed: January 6, 2012
    Publication date: October 24, 2013
    Applicant: CRYSTAL BIOPHARMACEUTICAL LLC
    Inventors: Yi Chen, Yu Chen
  • Publication number: 20130190308
    Abstract: This disclosure relates to new heterocyclic compounds that may be used to modulate a histamine receptor in an individual. Pyrido[3,4-b]indoles are described, as are pharmaceutical compositions comprising the compounds and methods of using the compounds in a variety of therapeutic applications, including the treatment of a cognitive disorder, psychotic disorder, neurotransmitter-mediated disorder and/or a neuronal disorder.
    Type: Application
    Filed: March 8, 2013
    Publication date: July 25, 2013
    Applicant: MEDIVATION TECHNOLOGIES, INC.
    Inventor: Medivation Technologies, Inc.
  • Publication number: 20130190303
    Abstract: This disclosure relates to new compounds that may be used to modulate a histamine receptor in an individual. Novel compounds are described, including new bridged heterocyclic [4,3-b]indole compounds. Pharmaceutical compositions are also provided. Pharmaceutical compositions comprising the compounds are also provided, as are methods of using the compounds in a variety of therapeutic applications, including the treatment of a cognitive disorder, psychotic disorder, neurotransmitter-mediated disorder and/or a neuronal disorder.
    Type: Application
    Filed: March 8, 2013
    Publication date: July 25, 2013
    Applicant: MEDIVATION TECHNOLOGIES, INC.
    Inventor: MEDIVATION TECHNOLOGIES, INC.
  • Publication number: 20130184269
    Abstract: This disclosure relates to new compounds that may be used to modulate a histamine receptor in an individual. Novel compounds are described, including new bridged heterocyclic[4,3-b]indole compounds. Pharmaceutical compositions are also provided. Pharmaceutical compositions comprising the compounds are also provided, as are methods of using the compounds in a variety of therapeutic applications, including the treatment of a cognitive disorder, psychotic disorder, neurotransmitter-mediated disorder and/or a neuronal disorder.
    Type: Application
    Filed: March 7, 2013
    Publication date: July 18, 2013
    Applicant: MEDIVATION TECHNOLOGIES, INC.
    Inventor: Medivation Technologies, Inc.
  • Patent number: 8440671
    Abstract: The invention relates generally to novel pharmaceutical methods for the treatment of various conditions. Compositions comprising: at least one phosphodiesterase-5-inhibitor in combination with one or more of the following medications: a selective serotonin reuptake inhibitor; a serotonin-norepinephrine reuptake inhibitor; a cholinesterase inhibitor; a dopamine agonist; or a medication suitable to increase the chemical concentrations of the neurotransmitters, selected from amino acids, monoamines, neuropeptides and other agents capable of primary neurotransmission in the synaptic clefts, and their use for treating a neurodegenerative disease in a subject. The invention also relates to: Compositions comprising: at least one phosphodiestersa-5-inhibitor in combination with one or more of the following medications: a selective serotonin reuptake inhibitor; or a cholinesterase inhibitor, and their use for treating damaged skin in a subject.
    Type: Grant
    Filed: May 19, 2008
    Date of Patent: May 14, 2013
    Assignee: Vivus, Inc.
    Inventor: Jerry M. Held
  • Publication number: 20130085140
    Abstract: Indenoisoquinolinone derivatives (I), the manufacturing method and the medical use thereof, which belong to pharmaceutical chemistry and organic chemistry field, are disclosed. These compounds can be used for treating several medical symptoms related to postmenopausal syndrome, uterine fibers deterioration and aortic smooth muscle cells proliferation, especially ER-(+) depend breast cancer. Meanwhile, these compounds can also be used for treating glioma and lung cancer, and have inhibiting effect on tumor metastasis effect on tumor metastasis.
    Type: Application
    Filed: December 16, 2009
    Publication date: April 4, 2013
    Applicant: CHINA PHARMACEUTICAL UNIVERSITY
    Inventors: Hua Xiang, Tianlin Wang, Hong Xiao, Qidong You, Yao Yao, Xiaobo Li, Qingjiang Liao
  • Publication number: 20130053363
    Abstract: [Problem] To provide a compound useful as medicine having PDE4B inhibitory activity, in particular, as an active ingredient of a composition for treating or preventing schizophrenia, Alzheimer's disease, dementia, depression and the like. [Measures for Solution] The present inventors examined compounds having PDE4B inhibitory activity and found that a tricyclic or tetracyclic imidazo[1,2-a]pyridine derivative or salts thereof had a superior PDE4B inhibitory activity, thereby completing the present invention. The imidazo[1,2-a]pyridine derivative can be used as an agent for treating or preventing schizophrenia, Alzheimer's disease, dementia, depression and the like.
    Type: Application
    Filed: October 26, 2012
    Publication date: February 28, 2013
    Applicant: Astellas Pharma Inc.
    Inventor: Astellas Pharma Inc.
  • Patent number: 8367836
    Abstract: The present invention provides compounds that are alpha4 integrin antagonists having a structure according to the following formula: or a tautomer, mixture of tautomers, salt or solvate thereof, wherein Cy, ring A, m, n, p, R1, R2, R3, R4, R5 and R6 are defined in the specification. The invention further provides pharmaceutical compositions including the compounds of the invention as well as methods of making and using the compounds and compositions of the invention, e.g., in the treatment and prevention of various conditions and disorders, such as Crohn's disease and ulcerative colitis.
    Type: Grant
    Filed: April 27, 2010
    Date of Patent: February 5, 2013
    Assignee: Elan Pharmaceuticals, Inc.
    Inventors: Ying-zi Xu, Shendong Yuan, David Wone, Andrei Konradi
  • Patent number: 8367654
    Abstract: The present invention is directed to a compound represented by Structural Formula (I) or a pharmaceutically acceptable salt thereof. The variables for Structural Formula I are defined herein. Also described is a pharmaceutical composition comprising the compound of Structural Formula I and its therapeutic use.
    Type: Grant
    Filed: May 7, 2010
    Date of Patent: February 5, 2013
    Assignee: Tetraphase Pharmaceuticals, Inc.
    Inventors: Roger B. Clark, Minsheng He, Louis Plamondon, Xiao-Yi Xiao, Magnus P. Rönn
  • Publication number: 20120302563
    Abstract: Described herein are substituted norindenoisoquinoline compounds, and pharmaceutical compositions and formulations comprising the norindenoisoquinoline compounds. Also described herein are methods for using the compounds for the treatment and/or prevention of topoisomerase mediated diseases, such as cancer.
    Type: Application
    Filed: January 27, 2011
    Publication date: November 29, 2012
    Applicant: PURDUE RESEARCH FOUNDATION
    Inventors: Mark S. Cushman, Yunlong Song
  • Publication number: 20120295856
    Abstract: The invention relates to novel fredericamycin derivatives, to drugs containing said derivatives or the salts thereof, and to the use of the fredericamycin derivatives for treating diseases, especially cancer diseases.
    Type: Application
    Filed: July 27, 2012
    Publication date: November 22, 2012
    Applicant: ZENTOPHARM GmbH
    Inventors: Ulrich Abel, Werner Simon
  • Publication number: 20120165522
    Abstract: Various 14-Nitro, 14-amino, and 14-substituted amino camptothecin derivatives are useful in the treatment of cancer and other hyperproliferative diseases. Various 14-nitro camptothecin derivatives are conveniently prepared by reacting a camptothecin derivative with fuming nitric acid, optionally employing acetic anhydride as a solvent.
    Type: Application
    Filed: June 16, 2010
    Publication date: June 28, 2012
    Inventors: Xiaohong Cai, Jian-Xin Duan, Mark Matteucci, Yeyu Cao, Hailong Jiao
  • Patent number: 8188284
    Abstract: The present invention relates to compounds of formula (I) wherein A, R1, R2, R3, R4, and R5 are as described herein, pharmaceutical compositions containing them, and methods for their manufacture. These compounds are 5-HT5A receptor antagonists and are useful in the prevention and/or treatment of depression, anxiety disorders, schizophrenia, panic disorders, agoraphobia, social phobia, obsessive compulsive disorders, post-traumatic stress disorders, pain, memory disorders, dementia, disorders of eating behaviors, sexual dysfunction, sleep disorders, abuse of drugs, motor disorders such as Parkinson's disease, psychiatric disorders or gastrointestinal disorders.
    Type: Grant
    Filed: February 27, 2009
    Date of Patent: May 29, 2012
    Assignee: Hoffman-La Roche Inc.
    Inventors: Sabine Kolczewski, Claus Riemer, Olivier Roche, Lucinda Steward, Juergen Wichmann, Thomas Woltering
  • Publication number: 20120122848
    Abstract: A novel (+)-3-hydroxymorphinan derivatives and a pharmaceutical composition comprising the same as an active ingredient, which are useful for preventing or treating a neurodegenerative disease, are provided.
    Type: Application
    Filed: July 28, 2010
    Publication date: May 17, 2012
    Applicant: GREEN CROSS CORPORATION
    Inventors: Jinhwa Lee, Jong Yup Kim, Kwang-Seop Song, Jeongmin Kim, Kwang Woo Ahn, Yonggyu Kong
  • Publication number: 20120108569
    Abstract: The present invention is directed to a compound represented by Structural Formula (I) or a pharmaceutically acceptable salt thereof. The variables for Structural Formula I are defined herein. Also described is a pharmaceutical composition comprising the compound of Structural Formula I and its therapeutic use.
    Type: Application
    Filed: May 7, 2010
    Publication date: May 3, 2012
    Inventors: Roger B. Clark, Minsheng He, Louis Plamondon, Xiao-Yi Xiao, Magnus P. Rönn
  • Publication number: 20120083488
    Abstract: A compound represented by the general Formula (I) below, or a salt or solvate thereof, which is useful as an ALK inhibitor, and is useful for prophylaxis or treatment of a disease accompanied by abnormality in ALK, for example, cancer, cancer metastasis, depression or cognitive function disorder: (meanings of the symbols that are included in the formula are as given in the specification).
    Type: Application
    Filed: June 9, 2010
    Publication date: April 5, 2012
    Inventors: Kazutomo Kinoshita, Kohsuke Asoh, Noriyuki Furuichi, Toshiya Ito, Hatsuo Kawada, Nobuya Ishii, Hiroshi Sakamoto, WooSang Hong, MinJeong Park, Yoshiyuki Ono, Yashuharu Kato, Kenji Morikami, Takashi Emura, Nobuhiro Oikawa
  • Publication number: 20120058939
    Abstract: Novel MCH-1 receptor antagonists are disclosed. These compounds are used in the treatment of various disorders, including obesity, anxiety, depression, non-alcoholic fatty liver disease, and psychiatric disorders. Methods of making these compounds are also described in the present invention.
    Type: Application
    Filed: July 1, 2010
    Publication date: March 8, 2012
    Applicant: ALBANY MOLECULAR RESEARCH, INC.
    Inventors: Peter R. GUZZO, Matthew David SURMAN, Alan John HENDERSON, Mark HADDEN, Emily Elizabeth FREEMAN
  • Publication number: 20120022030
    Abstract: The present invention describes tetracyclic compounds of formula (IA) or (IB), wherein the symbols R, X, A, Y, R2, R3 and D are as defined in the specification, their use in the treatment of certain diseases, e.g. depending on MK-2 or TNF activity, and ways of manufacturing them.
    Type: Application
    Filed: September 13, 2010
    Publication date: January 26, 2012
    Inventors: Achim SCHLAPBACH, Lászlo RÉVÉSZ, Guido KOCH
  • Publication number: 20110306604
    Abstract: Compounds of Formula (I): (where variables R1A, R1B, R2, R3, R4, A, and Z are as defined herein) which are useful as antagonists of CGRP receptors, and useful in the treatment or prevention of diseases in which CGRP receptors are involved, such as headache, and in particular migraine and cluster headache. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which CGRP receptors are involved.
    Type: Application
    Filed: August 14, 2009
    Publication date: December 15, 2011
    Inventors: Michael R. Wood, Ian M. Bell, June J. Kim, Harold G. Selnick, Craig A. Stump
  • Publication number: 20110281886
    Abstract: Pharmaceutical compositions and their methods of use are provided, where the pharmaceutical compositions comprise a phenolic opioid prodrug that provides enzymatically-controlled release of a phenolic opioid, and an enzyme inhibitor that interacts with the enzyme(s) that mediates the enzymatically-controlled release of the phenolic opioid from the prodrug so as to attenuate enzymatic cleavage of the prodrug.
    Type: Application
    Filed: October 16, 2009
    Publication date: November 17, 2011
    Inventors: Thomas E. Jenkins, Julie D. Seroogy, Jonathan W. Wray
  • Publication number: 20110237582
    Abstract: This disclosure relates to new heterocyclic compounds that may be used to modulate a histamine receptor in an individual. Pyrido[3,4-b]indoles are described, as are pharmaceutical compositions comprising the compounds and 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: September 23, 2010
    Publication date: September 29, 2011
    Inventors: Rajendra Parasmal JAIN, Sarvajit Chakravarty
  • Publication number: 20110223241
    Abstract: Compositions which comprise a liposomal water-soluble camptothecin and optionally a liposomal fluoropyrimidine in combination with a vascular epithelial growth factor (VEGF) inhibitor such as cetuximab or an epidermal growth factor receptor (EGFR) inhibitor such as bevacizumab are useful in achieving enhanced therapeutic effects for the treatment of cancer.
    Type: Application
    Filed: October 16, 2009
    Publication date: September 15, 2011
    Applicant: Celator Pharmaceuticals, Inc.
    Inventors: Paul Tardi, Lawrence Mayer, David Bermudes
  • Patent number: 8017612
    Abstract: The present invention relates to a compound represented by the following formula [I] wherein each symbol is as defined in the specification, or a pharmaceutically acceptable salt thereof, or a solvate thereof and an anti-HCV agent and an HCV polymerase inhibitor 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: Grant
    Filed: April 17, 2007
    Date of Patent: September 13, 2011
    Assignee: Japan Tobacco Inc.
    Inventors: Hiroyuki Abe, Masahiro Tanaka, Kazuyuki Sugimoto, Akira Suma, Masahiro Yokota, Makoto Shiozaki, Kiyosei Iio, Kazuhito Ueyama, Dai Motoda, Toru Noguchi, Tsuyoshi Adachi, Junichiro Tsuruha, Satoki Doi
  • Publication number: 20110218184
    Abstract: The present invention provides novel quinolone compounds and pharmaceutical composition thereof which may inhibit cell proliferation and/or induce cell apoptosis. The present invention also provides methods of preparing such compounds and compositions, and methods of making and using the same.
    Type: Application
    Filed: March 9, 2011
    Publication date: September 8, 2011
    Applicant: CYLENE PHARMACEUTICALS, INC.
    Inventors: Johnny Yasuo NAGASAWA, Fabrice Pierre, Mustapha Haddach, Michael Schwaebe, Levan Darjania, Jeffrey P. Whitten
  • Patent number: 7977337
    Abstract: Disclosed are quinoline compounds having affinity for the 5-HT6 receptor and having the formula: where R1, R2, R3, R4, R5, n, m, p and A are defined herein, and salts thereof, compositions containing these compounds and salts and processes for making and using the same.
    Type: Grant
    Filed: July 30, 2010
    Date of Patent: July 12, 2011
    Assignee: Glaxo Group Limited
    Inventors: Mahmood Ahmed, Christopher Norbert Johnson, Martin C Jones, Gregor James MacDonald, Stephen Frederick Moss, Mervyn Thompson, Charles Edward Wade, David R Witty