The Additional Six-membered Hetero Ring Is One Of The Cyclos In A Polycyclo Ring System Patents (Class 544/125)
  • Patent number: 9980953
    Abstract: The present invention relates to a pharmaceutical combined composition for preventing or treating cancer comprising a compound of formula 1 or a pharmaceutically acceptable salt thereof and topoisomerase inhibitor as active ingredients. The pharmaceutical combined composition of the present invention specifically inhibits cell proliferation and induces apoptosis as to various cancers such as colorectal cancer and ovarian cancer that a vascular disrupting agent cannot treat due to a complex inhibition mechanism of neoplasm of the compound of formula 1 and the pharmaceutically acceptable salt thereof and topoisomerase inhibitor, and thereby it can be usefully used for preventing and treating cancer.
    Type: Grant
    Filed: March 2, 2017
    Date of Patent: May 29, 2018
    Assignees: CHONG KUN DANG PHARMACEUTICAL CORP., NATIONAL CANCER CENTER
    Inventors: Soo Jin Kim, Young Sang Kim, MinChae Kim, Young-Whan Park, Jung-Yong Kim, In Chull Kim
  • Patent number: 9278969
    Abstract: The present invention provides a compound of formula I: Said compound is inhibitor of aldosterone synthase and aromatase, and thus can be employed for the treatment of a disorder or disease mediated by aldosterone synthase or aromatase. Accordingly, the compound of formula I can be used in treatment of hypokalemia, hypertension, congestive heart failure, atrial fibrillation, renal failure, in particular, chronic renal failure, restenosis, atherosclerosis, syndrome X, obesity, nephropathy, post-myocardial infarction, coronary heart diseases, inflammation, increased formation of collagen, fibrosis such as cardiac or myocardiac fibrosis and remodeling following hypertension and endothelial dysfunction, gynecomastia, osteoporosis, prostate cancer, endometriosis, uterine fibroids, dysfunctional uterine bleeding, endometrial hyperplasia, polycystic ovarian disease, infertility, fibrocystic breast disease, breast cancer and fibrocystic mastopathy.
    Type: Grant
    Filed: August 14, 2014
    Date of Patent: March 8, 2016
    Assignee: Novartis AG
    Inventors: Gary Michael Ksander, Erik Meredith, Lauren Monovich, Julien Papillon, Fariborz Firooznia, Qi-Ying Hu
  • 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: 9034870
    Abstract: The invention described herein pertains to substituted azaindenoisoquinoline compounds, in particular 7-, 8-, 9-, and 10-azaindenoisoquinoline compounds, which are inhibitors of topoisomerase I, processes and intermediates for their syntheses, pharmaceutical compositions of the compounds, and methods of using them in the treatment of cancer.
    Type: Grant
    Filed: March 6, 2014
    Date of Patent: May 19, 2015
    Assignees: Purdue Research Foundation, United States Government National Institutes of Health (NIH), U.S. Dept. of Health and Human Services (DHHS), NIH Division of Extramural Inventions and Technology Resources (DEITR)
    Inventors: Mark S. Cushman, Evgeny A. Kiselev, Andrew E. Morrell, Yves George Pommier
  • 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
  • Publication number: 20150133445
    Abstract: The invention described herein pertains to the synthesis and use of certain N-substituted indenoisoquinoline compounds which inhibit the activity Tyrosyl-DNA Phosphodiesterase I (Tdp1) or Topoisomerase I (Top1) or both, or otherwise demonstrate anticancer activity. Also disclosed are novel N-substituted indenoisoquinoline compounds and pharmaceutical compositions comprising the novel N-substituted indenoisoquinoline compounds.
    Type: Application
    Filed: November 10, 2014
    Publication date: May 14, 2015
    Inventors: Mark S. CUSHMAN, Trung X. Nguyen, Martin M. Conda-Sheridan, Yves George Pommier
  • Patent number: 9006234
    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: July 2, 2012
    Date of Patent: April 14, 2015
    Assignee: Medivation Technologies, Inc.
    Inventors: Rajendra Parasmal Jain, Sarvajit Chakravarty
  • 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
  • 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: 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: 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: 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
  • Patent number: 8853206
    Abstract: The invention relates to novel compounds of formula I where X, A?, Q1, Q2, Q3, R2, R3, R4, R5, R6, R7, R8 and R9 are each as defined below. The compounds of formula I have antithrombotic activity and inhibit especially protease-activated receptor 1 (PAR1). The invention further relates to a process for preparing the compound of formula I and to the use thereof as a medicament.
    Type: Grant
    Filed: April 20, 2012
    Date of Patent: October 7, 2014
    Assignee: Sanofi
    Inventors: Uwe Heinelt, Volkmar Wehner, Matthias Herrmann, Karl Schoenafinger, Henning Steinhagen
  • Publication number: 20140187547
    Abstract: The invention described herein pertains to substituted azaindenoisoquinoline compounds, in particular 7-, 8-, 9-, and 10-azaindenoisoquinoline compounds, which are inhibitors of topoisomerase I, processes and intermediates for their syntheses, pharmaceutical compositions of the compounds, and methods of using them in the treatment of cancer.
    Type: Application
    Filed: March 6, 2014
    Publication date: July 3, 2014
    Applicant: Purdue Research Foundation
    Inventors: Mark S. CUSHMAN, Evgeny A. KISELEV, Andrew E. MORRELL
  • Publication number: 20140187549
    Abstract: The application is directed to compounds of Formula I-A and pharmaceutically acceptable salts and solvates thereof, wherein , R1a, R3a, R4, Y and Za are defined as set forth in the specification. The invention is also directed to use of compounds of Formula I-A to treat disorders responsive to the modulation of one or more opioid receptors, or as synthetic intermediates. Certain compounds of the present invention are especially useful for treating pain.
    Type: Application
    Filed: December 13, 2013
    Publication date: July 3, 2014
    Applicant: Purdue Pharma L.P.
    Inventor: Laykea TAFESSE
  • Patent number: 8735424
    Abstract: New compounds, compositions and methods of inhibition of Provirus Integration of Maloney Kinase (PIM kinase) activity associated with tumorigenesis in a human or animal subject are provided. In certain embodiments, the compounds and compositions are effective to inhibit the activity of at least one PIM kinase. The new compounds and compositions may be used either alone or in combination with at least one additional agent for the treatment of a serine/threonine kinase- or receptor tyrosine kinase-mediated disorder, such as cancer.
    Type: Grant
    Filed: August 31, 2009
    Date of Patent: May 27, 2014
    Assignee: Novartis AG
    Inventors: Matthew Burger, Mika Lindvall
  • Publication number: 20140073637
    Abstract: The present invention relates to a new class of benzo[e]pyrido-indole, the amino-substituted-alkyloxy-benzo[e]pyrido[4,3-b]indole derivatives, having a particular kinase inhibition profile and useful as a therapeutic agent, in particular an anti-tumoral agent.
    Type: Application
    Filed: May 30, 2012
    Publication date: March 13, 2014
    Applicants: INSTITUT CURIE, INSERM (INSTITUT NATIONAL DE LA SANTE ET DE LA RECHERCHE MEDICALE, CENTRE NATIONAL DE LA RECHERCHE SCIENTIFIQUE
    Inventors: Chi-Hung N'Guyen, Annie Molla, Ly-Thuy-Tram Le
  • Patent number: 8664238
    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: Grant
    Filed: December 16, 2009
    Date of Patent: March 4, 2014
    Assignees: China Pharmaceutical University, Nanjing Medical University Affiliated Brain Hospital
    Inventors: Hua Xiang, Tianlin Wang, Hong Xiao, Qidong You, Yao Yao, Xiaobo Li, Qingjiang Liao
  • Publication number: 20140031543
    Abstract: The present invention provides (+)-morphinanium compounds comprising substituted 6-hydroxy or 6-amine groups. The invention also provides methods for inhibiting microglial activation by administering the compounds of the invention.
    Type: Application
    Filed: October 3, 2013
    Publication date: January 30, 2014
    Applicant: Mallinckrodt LLC
    Inventors: Christopher W. Grote, Amruta R. Poreddy
  • Publication number: 20140018360
    Abstract: The invention described herein pertains to substituted azaindenoisoquinoline compounds, in particular 7-, 8-, 9-, and 10-azaindenoisoquinoline compounds, which are inhibitors of topoisomerase I, processes and intermediates for their syntheses, pharmaceutical compositions of the compounds, and methods of using them in the treatment of cancer.
    Type: Application
    Filed: July 13, 2012
    Publication date: January 16, 2014
    Inventors: Mark S. CUSHMAN, Evgeny A. KISELEV, Andrew E. MORRELL
  • Patent number: 8575188
    Abstract: Various 14-nitro, 14-amino, and 14-substituted amino camptothecin derivatives are useful in the treatment of cancer and other hyperproliferative diseases. 14-Nitro camptothecin derivatives are conveniently prepared by reacting a camptothecin derivative with fuming nitric acid, optionally employing acetic anhydride as a solvent.
    Type: Grant
    Filed: June 16, 2010
    Date of Patent: November 5, 2013
    Assignee: Threshold Pharmaceuticals, Inc.
    Inventors: Xiaohong Cai, Jian-Xin Duan, Mark Matteucci, Yeyu Cao, Hailong Jiao
  • Patent number: 8546381
    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 24, 2009
    Date of Patent: October 1, 2013
    Assignee: Medivation Technologies, Inc.
    Inventors: David T. Hung, Andrew Asher Protter, Sarvajit Chakravarty, Rajendra Parasmal Jain
  • 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.
  • Publication number: 20130143878
    Abstract: The invention described herein pertains to substituted dibenzonaphthyridine compounds, pharmaceutical compositions, and formulations comprising the dibenzonaphthyridine compounds, their synthesis, and methods for their use in the treatment and/or prevention of cancer.
    Type: Application
    Filed: August 17, 2011
    Publication date: June 6, 2013
    Applicant: PURDUE RESEARCH FOUNDATION
    Inventors: Mark S. Cushman, Evgeny A. Kiselev
  • Publication number: 20130121986
    Abstract: The present invention concerns nitrogenated derivatives of narciclasine and pancratistatin of the following general formula (I) as well as their pharmaceutically acceptable salts. The present invention also concerns the use of these compounds in cancer therapy as well as a method for their preparation.
    Type: Application
    Filed: December 26, 2012
    Publication date: May 16, 2013
    Inventors: Frederic MARION, Jean-Philippe ANNEREAU, Jacques FAHY
  • Publication number: 20130102598
    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: Application
    Filed: May 17, 2011
    Publication date: April 25, 2013
    Applicant: SECOND MILITARY MEDICAL UNIVERSITY, PLA
    Inventors: Yunlong Song, Xiaodan Fu, Yunpeng Qi
  • 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: 20130065875
    Abstract: The invention provides derivatives and analogues of triazatetracyclo[7.7.0.01,13,02,7]-hexadeca-2,4,6,10,12-pentaenes, 5,7,11-triazatetracyclo[8.7.0.01,6,012,17]-heptadeca-6,8,12,14,16-pentaenes, pharmaceutical compositions comprising these compounds and methods for treatment of hepatitis C viral infections using these compounds.
    Type: Application
    Filed: October 27, 2010
    Publication date: March 14, 2013
    Applicants: THE SCRIPPS RESEARCH INSTITUTE, TRUSTEES OF BOSTON UNIVERSITY
    Inventors: John K. Snyder, Wanguo Wei, Feng Ni, Arthur Donny Strosberg, Smitha Kota, Virginia Takahashi
  • 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.
  • 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
  • Patent number: 8299056
    Abstract: Provided herein are Heteroaryl Compounds of formula (I): wherein R1 and R2 are as defined herein, compositions comprising an effective amount of a Heteroaryl Compound and methods for treating or preventing inflammatory conditions or cancer, and conditions treatable or preventable by inhibition of a kinase or a kinase pathway comprising administering an effective amount of a Heteroaryl Compound to a subject in need thereof.
    Type: Grant
    Filed: September 8, 2009
    Date of Patent: October 30, 2012
    Assignee: Signal Pharmaceuticals, LLC
    Inventors: Sogole Bahmanyar, R.J. Bates, Kate Blease, Andrew Calabrese, Thomas Daniel, Mercedes Delgado, Jan Elsner, Paul Erdman, Bruce Fahr, Gregory Ferguson, Branden Lee, Lisa Nadolny, Garrick Packard, Patrick Papa, Veronique Plantevin-Krenitsky, Jennifer Riggs, Patricia Rohane, Sabita Sankar, John Sapienza, Yoshitaka Satoh, Victor Sloan, Randall Stevens, Lida Tehrani, Jayashree Tikhe, Eduardo Torres, Andrew Wallace, Brandon Wade Whitefield, Jingjing Zhao
  • Patent number: 8288538
    Abstract: A compound represented by the following formula, or a salt thereof or a hydrate of the foregoing, has excellent hepatocyte growth factor receptor (HGFR) inhibitory activity, and exhibits anti-tumor activity, angiogenesis inhibitory activity, and cancer metastasis inhibitory activity. R1 represents a 3- to 10-membered non-aromatic heterocyclic group or the like; R2 and R3 represent hydrogen; R4, R5, R6, and R7 may be the same or different and each represents hydrogen, halogen, C1-6 alkyl or the like; R8 represents hydrogen or the like; R9 represents a 3- to 10-membered non-aromatic heterocyclic group or the like; n represents an integer of 1 or 2; X represents —CH?, nitrogen or the like.
    Type: Grant
    Filed: September 14, 2009
    Date of Patent: October 16, 2012
    Assignee: Eisai R&D Management Co., Ltd.
    Inventors: Tomohiro Matsushima, Keiko Takahashi, Setsuo Funasaka, Hiroshi Obaishi, Shuji Shirotori
  • 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
  • Publication number: 20120135978
    Abstract: A novel compound which is useful as an agent for treating and/or preventing emesis, vomiting and/or constipation. A compound represented by the formula (I): wherein R1 and R2 are each independently hydrogen, optionally substituted lower alkyl, optionally substituted lower alkenyl, optionally substituted cycloalkyl, optionally substituted aryl etc., R3 is hydrogen, hydroxy, optionally substituted lower alkyl, optionally substituted lower alkenyl, optionally substituted lower alkynyl, optionally substituted lower alkoxy etc., R4 is hydrogen or lower alkyl, R5 is hydrogen, lower alkyl, cycloalkyl lower alkyl or lower alkenyl, or a pharmaceutically acceptably salt, or a solvate thereof is provided.
    Type: Application
    Filed: November 30, 2011
    Publication date: May 31, 2012
    Inventors: Masanao INAGAKI, Shin-ichiro Hara, Nobuhiro Haga, Yoshinori Tamura, Yoshihisa Goto, Tsuyoshi Hasegawa
  • 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: 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
  • Patent number: 8119654
    Abstract: The present invention relates to Indenoisoquinolinone Analogs, compositions comprising an effective amount of an Indenoisoquinolinone Analog and methods for treating or preventing an inflammatory disease, a reperfusion injury, diabetes mellitus, a diabetic complication, reoxygenation injury resulting from organ transplantation, an ischemic condition, a neurodegenerative disease, renal failure, a vascular disease, a cardiovascular disease, cancer, a complication of prematurity, cardiomyopathy, retinopathy, nephropathy, neuropathy, erectile dysfunction or urinary incontinence, comprising administering to a subject in need thereof an effective amount of an Indenoisoquinolinone Analog.
    Type: Grant
    Filed: February 28, 2008
    Date of Patent: February 21, 2012
    Assignee: Inotek Pharmaceuticals Corporation
    Inventors: Prakash Jagtap, Duy-Phong Pham-Huu, Frederick Cohen, Xiaojing Wang
  • Publication number: 20120022061
    Abstract: The present invention provides compounds of formula I: formula (I) wherein X1-X4 and R1-R12 have any of the values defined in the specification, as well as salts and prodrugs thereof, which inhibit major molecular mechanisms associated with bacterial cell division and proliferation so as to be useful for the treatment and/or prevention of bacterial infections. The invention also provides compositions comprising these compounds as well as methods for using these compounds to inhibit bacterial cell division and proliferation and to treat bacterial infections.
    Type: Application
    Filed: January 15, 2010
    Publication date: January 26, 2012
    Inventors: Edmond J. LaVoie, Ajit Parhi, Daniel S. Pilch, Malvika Kaul
  • Publication number: 20120004223
    Abstract: The present technology relates to compounds of Formulas (V) and (VI) and methods of making and using such compounds. Methods of use include prevention and treatment of hyperlipidemia, hypercholesterolemia, hypertriglyceridemia, hepatic steatosis, and metabolic syndrome. Compounds disclosed herein also lower total cholesterol, LDL-cholesterol, and triglycerides and increase hepatic LDL receptor expression, inhibit PCSK9 expression, and activate AMP-activated protein kinase.
    Type: Application
    Filed: December 22, 2009
    Publication date: January 5, 2012
    Inventors: Haiyan Liu, Gaoping Li, Junbo Wang, Jingwen Liu
  • 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: 20110123516
    Abstract: The present invention concerns nitrogenated derivatives of narciclasine and pancratistatin of the following general formula (I) as well their pharmaceutically acceptable salts. The present invention also concerns the use of these compounds in cancer therapy as well as a method for their preparation.
    Type: Application
    Filed: July 28, 2009
    Publication date: May 26, 2011
    Applicant: PIERRE FABRE MEDICAMENT
    Inventors: Frédéric Marion, Jean-Philippe Annereau, Jacques Fahy
  • Publication number: 20110112086
    Abstract: The present invention provides pyridinone analogs which may inhibit cell proliferation and/or induce cell apoptosis. The present invention also provides methods of preparing pyridinone analogs, and methods of using the same.
    Type: Application
    Filed: June 8, 2007
    Publication date: May 12, 2011
    Applicant: CYLENE PHARMACEUTICALS, INC.
    Inventors: Fabrice Pierre, Michael Schwaebe
  • Publication number: 20110105470
    Abstract: The present invention provides novel tricyclic spiro-oxathiine naphthoquinone derivatives, a synthetic method for making the derivatives, and the use of the derivatives to induce cell death and/or to inhibit proliferation of cancer or precancerous cells. The naphthoquinone derivatives of the present invention are related to the compound known as ?-lapachone (3,4-dihydro-2,2-dimethyl-2H-naphtho(1,2-b)pyran-5,6-dione).
    Type: Application
    Filed: January 11, 2011
    Publication date: May 5, 2011
    Applicant: ArQule, Inc.
    Inventors: Mark A. Ashwell, Manish Tandon, Jean-Marc Lapierre, Syed Ali, David Vensel, Chiang J. Li
  • Publication number: 20110081482
    Abstract: The present invention relates to photochromic naphthopyrancs having a double-bridged terphenyl sub-unit, and to the use thereof in plastics of all types, particularly for ophthalmic purposes.
    Type: Application
    Filed: April 29, 2009
    Publication date: April 7, 2011
    Inventors: Manfred Melzig, Yven Rohlfing, Udo Weigand
  • Patent number: 7919487
    Abstract: This invention relates to compounds of formula (I): their compositions and methods of use thereof. The compounds (and compositions) are useful in modulating IL-12 production and processes mediated by IL-12.
    Type: Grant
    Filed: November 10, 2005
    Date of Patent: April 5, 2011
    Assignee: Synta Pharmaceuticals Corporation
    Inventors: Lijun Sun, Shijie Zhang, Keizo Koya, Dinesh Chimmanamada, Hao Li, David James, Elena Kostik
  • Publication number: 20110065687
    Abstract: This application relates to certain novel polycyclic compounds that interact with quadruplex-forming regions of polynucleotides and thereby inhibit translation of genetic information into polypeptides. These compounds can thus provide anticancer and antibacterial and antiviral effects. The invention includes novel compounds and pharmaceutical compositions, and methods of using them to treat cancer and other conditions.
    Type: Application
    Filed: April 17, 2008
    Publication date: March 17, 2011
    Inventors: Michael Schwaebe, Johnny Yasuo Nagasawa, Mustapha Haddach
  • Publication number: 20110027226
    Abstract: Compounds of a certain formula I, in which R1, R2, R3 and R4 have the meanings indicated in the description, are effective Eg5-inhibiting compounds with anti-proliferative and/or apoptosis inducing activity.
    Type: Application
    Filed: August 22, 2007
    Publication date: February 3, 2011
    Applicant: 4SC AG
    Inventors: Matthias Vennemann, Juergen Braugner, Petra Gimmnich, Thomas Baer
  • Publication number: 20110009628
    Abstract: The present technology relates to compounds of Formulas I-VI and methods of making and using such compounds. Methods of use include prevention and treatment of hyperlipidemia, hypercholesterolemia, hypertriglyceridemia, hepatic steatosis, and metabolic syndrome. Compounds disclosed herein also increase HDL-C, lower total cholesterol, LDL-cholesterol, and triglycerides and increase hepatic LDL receptor expression, inhibit PCSK9 expression, and activate AMP-activated protein kinase.
    Type: Application
    Filed: July 8, 2010
    Publication date: January 13, 2011
    Inventors: Haiyan Liu, Gaoping Li, Junbo Wang, Jingwen Liu