The Additional Hetero Ring Is One Of The Cyclos In A Polycyclo Ring System Patents (Class 514/337)
  • Patent number: 11098054
    Abstract: Disclosed is a compound of formula (I) in which a, R1-R5 and X1 are as described herein. Also disclosed are a pharmaceutical composition containing the compound and a method of using the compound for treating cancer, such as renal cancer.
    Type: Grant
    Filed: July 5, 2018
    Date of Patent: August 24, 2021
    Assignees: The United States of America, as represented by the Secretary, Department of Health and Human Sciences, Fundacio Institut Catala D'Investigacio Quimica, University of Delaware, University of Leeds, Universitat Rovira I Virgili
    Inventors: John A. Beutler, Antonio Echavarren, William Chain, David Beech, Zhenhua Wu, Jean-Simon Suppo, Fernando Bravo, Hussein Rubaiy
  • Patent number: 11001582
    Abstract: Processes for the preparation of Venetoclax and Venetoclax produced by the processes are disclosed.
    Type: Grant
    Filed: March 10, 2017
    Date of Patent: May 11, 2021
    Assignee: ASSIA CHEMICAL INDUSTRIES LTD.
    Inventors: Zsuzsa Potarine Juhasz, Szabolcs Struba, Csilla Nemethne Racz, Zoltan Gabor Toth, Andrea Szilagyi, Renata Kerti-Ferenczi, Sandor Janos Molnar, Nora Pasztor-Debreczeni, Janos Hajko
  • Patent number: 10947218
    Abstract: The invention relates to a compound of formula (I) in free form or in pharmaceutically acceptable salt form to pharmaceutical compositions comprising said compound and to the use of said compound in the treatment of heterotopic ossification and fibrodysplasia ossificans progressiva.
    Type: Grant
    Filed: May 27, 2020
    Date of Patent: March 16, 2021
    Assignee: NOVARTIS AG
    Inventors: Luca Arista, Sreehari Babu, Jianwei Bian, Kai Cui, Michael Patrick Dillon, Rene Lattmann, Jialiang Li, Lv Liao, Dimitrios Lizos, Rita Ramos, Nikolaus Johannes Stiefl, Thomas Ullrich, Peggy Usselmann, Xiaoyang Wang, Liladhar Murlidhar Waykole, Sven Weiler, Yubo Zhang, Yizong Zhou, Tingying Zhu
  • Patent number: 10939682
    Abstract: Pesticidally active bi- or tricyclic heterocycles with sulphur-containing substituents, stereoisomers and tautomeric forms thereof that can be used as insecticides and can be prepared in a manner known per se.
    Type: Grant
    Filed: June 19, 2014
    Date of Patent: March 9, 2021
    Assignee: Syngenta Participations AG
    Inventors: Andrew Edmunds, Michel Muehlebach, Andre Stoller, Olivier Loiseleur, Anke Buchholz, Ottmar Franz Hueter, Roger Graham Hall, Daniel Emery, Pierre Joseph Marcel Jung, Long Lu, Yaming Wu, Aurelien Bigot, Ruifang Chen
  • Patent number: 10668015
    Abstract: Disclosed herein are methods for prophylactic treatment of acute coronary syndrome (ACS) comprising administering, by inhalation, an effective amount of a pharmaceutical composition comprising at least one anticoagulant or antiplatelet agent to a subject in need thereof, wherein the anticoagulant or antiplatelet agent first enters the heart via the left atrium.
    Type: Grant
    Filed: January 20, 2016
    Date of Patent: June 2, 2020
    Assignees: InCarda Therapeutics, Inc., The Regents of the University of California
    Inventors: Rangachari Narasimhan, Gregory Marcus
  • Patent number: 10662171
    Abstract: Novel compounds of the structural formula (I), and the pharmaceutically acceptable salts thereof, are agonists of G-protein coupled receptor 40 (GPR40) and may be useful in the treatment, prevention and suppression of diseases mediated by the G-protein-coupled receptor 40. The compounds of the present invention may be useful in the treatment of Type 2 diabetes mellitus, and of conditions that are often associated with this disease, including obesity and lipid disorders, such as mixed or diabetic dyslipidemia, hyperlipidemia, hypercholesterolemia, and hypertriglyceridemia.
    Type: Grant
    Filed: August 3, 2015
    Date of Patent: May 26, 2020
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Harry Chobanian, Duane DeMong, Yan Guo, Barbara Pio, Christopher W. Plummer
  • Patent number: 10654845
    Abstract: The invention relates to novel compounds of the formula (I) in which the R1, R2a, R2b, R3, A1, A2, A4 and n have the meanings given above, to their use as acaricides and/or insecticides for controlling animal pests and to processes and intermediates for their preparation.
    Type: Grant
    Filed: February 2, 2016
    Date of Patent: May 19, 2020
    Assignee: BAYER CROPSCIENCE AKTIENGESELLSCHAFT
    Inventors: Ruediger Fischer, David Wilcke, Kerstin Ilg, Daniela Portz, Ulrich Goergens, Sascha Eilmus, Olga Malsam, Andreas Turberg, Sebastian Horstmann
  • Patent number: 10383942
    Abstract: A topical pharmaceutical composition comprising tazarotene and one or more of an anti-inflammatory or anti-bacterial agent. Also provided is a method for treating skin conditions, such as acne utilizing the above topical pharmaceutical composition.
    Type: Grant
    Filed: July 20, 2015
    Date of Patent: August 20, 2019
    Assignee: Allergan, Inc.
    Inventors: Michael G. Oefelein, Jeffrey R. Ehrhardt, Gurpreet Ahluwalia
  • Patent number: 10385048
    Abstract: Compounds of formula (I), wherein the substituents are as defined in claim 1, and the agrochemically acceptable salts salts, stereoisomers, enantiomers, tautomers and N-oxides of those compounds, can be used as insecticides and can be prepared in a manner known per se.
    Type: Grant
    Filed: December 28, 2015
    Date of Patent: August 20, 2019
    Assignee: SYNGENTA PARTICIPATION AG
    Inventors: Andrew Edmunds, Pierre Joseph Marcel Jung, Michel Muehlebach, Long Lu, Yaming Wu, Ruifang Chen
  • Patent number: 10264976
    Abstract: Flavonoid compounds may be prepared that are selective for certain cell organelles, and may be used as biological imaging agents. Organelles that may be imaged with flavonoid compounds include mitochondria and lysosomes. Advantageously, the flavonoids show specificity to certain organelles and may exhibit a florescence “turn-on” mechanism, where the flavonoids that have target an organelle exhibit a florescence response when excited.
    Type: Grant
    Filed: November 6, 2015
    Date of Patent: April 23, 2019
    Assignee: The University of Akron
    Inventors: Yi Pang, Bin Liu
  • Patent number: 10172915
    Abstract: The present invention provides a method of treating, ameliorating or inhibiting sirtuin-associated disorders and/or conditions in a subject in need thereof, by administering to the subject an effective amount of an ANXA1 peptide.
    Type: Grant
    Filed: October 20, 2014
    Date of Patent: January 8, 2019
    Assignee: Duke University
    Inventors: Zhiquan Zhang, Mihai V. Podgoreanu, Qing Ma, David S. Warner, Mark F. Newman
  • Patent number: 9790231
    Abstract: The invention relates to compounds of Formula (I) and their pharmaceutically acceptable salts, wherein the substituents are as described herein, and their use in medicine for the treatment of diseases, disorders associated with the modulation of calcium release-activated calcium (CRAC) channel. The invention also relates to pharmaceutical compositions containing such compounds in treating diseases disorders associated with calcium release-activated calcium (CRAC) channel modulators.
    Type: Grant
    Filed: June 23, 2014
    Date of Patent: October 17, 2017
    Assignee: LUPIN LIMITED
    Inventors: Nageswara Rao Irlapati, Kiran Chandrashekhar Kulkarni, Vijay Pandurang Karche, Gokul Keruji Deshmukh, Neelima Sinha, Venkata P. Palle, Rajender Kumar Kamboj
  • Patent number: 9708268
    Abstract: The invention relates to ROR modulators; compositions comprising an effective amount of a ROR modulator; and methods for treating or preventing diseases associated with ROR.
    Type: Grant
    Filed: April 30, 2013
    Date of Patent: July 18, 2017
    Assignee: INNOV17 LLC
    Inventors: Anderson Gaweco, Jefferson W. Tilley, John Walker, Samantha Palmer, James Blinn
  • Patent number: 9676720
    Abstract: The present invention provides a substituted biaryl compound of general formula (I): wherein, R1, W, R2, and Z are as defined in the claims and the description, or a pharmacologically acceptable salt thereof. The compound according to the present invention has an excellent inhibition effect of pulmonary fibroblast proliferation, and is therefore useful as a therapeutic agent and/or a prophylactic agent for interstitial pneumonia and pulmonary fibrosis.
    Type: Grant
    Filed: March 28, 2014
    Date of Patent: June 13, 2017
    Assignee: UBE INDUSTRIES, LTD.
    Inventors: Nobuhiko Shibakawa, Kenji Yoneda, Tetsushi Katsube, Tomoko Kanda, Koji Ito, Kiyoshi Yamamoto, Noriaki Iwase, Shigeru Ushiyama
  • Patent number: 9670190
    Abstract: The present invention relates to novel pyridine or pyrimidine derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of chemokine receptors. The invention relates specifically to the use of these compounds and their pharmaceutical compositions to treat disorders associated with chemokine receptor modulation.
    Type: Grant
    Filed: March 12, 2014
    Date of Patent: June 6, 2017
    Assignee: Allergan, Inc.
    Inventors: Richard L. Beard, John E. Donello, Veena Viswanath, Michael E. Garst, Haiqing Yuan, Xiaoxia Liu
  • Patent number: 9611243
    Abstract: An improved method is described for making single isomers of synthetic benzoprostacyclin analogue compounds, in particular the pharmacologically active 314-d isomer of beraprost. In contrast to the prior art, the method is stereoselective and requires fewer steps than the known methods for making these compounds.
    Type: Grant
    Filed: April 8, 2016
    Date of Patent: April 4, 2017
    Assignee: Lung Biotechnology PBC
    Inventors: Vijay Sharma, Hitesh Batra, Sudersan Tuladhar
  • Patent number: 9532973
    Abstract: A compound of formula (I-1) wherein n equals 0 or 1, Z represents O or S, R1 represents one group chosen among the group consisting of hydrogen, C1-C7 alkyl, substituted, or not, by a halogen, a hydroxyl or a —O—R12 group, wherein R12 is a C1-C7 alkyl, a group —CH2—O—CO—R5 wherein R5 is chosen among a hydrogen atom and a C1-C7 alkyl, substituted or not by at least one halogen, a group —O—R13, wherein R13 is chosen among hydrogen and a C1-C7 alkyl, an amine or a —CH2-amine, R?1 represents a group chosen among hydrogen and —O—R14, wherein R14 is chosen among hydrogen and a C1-C7 alkyl, and R2 is chosen among the group consisting of a C1-C7 alkyl, a C3-C6 cycloalkyl, an aryl group, and an heteroaryl group for the treatment of pathologies involving excess activity of at least one member of the kallikrein family.
    Type: Grant
    Filed: March 10, 2015
    Date of Patent: January 3, 2017
    Assignees: UNIVERSITE PIERRE ET MARIE CURIE (PARIS 6), UNIVERSITE DE LIEGE
    Inventors: Michele Reboud-Ravaux, Chahrazade Yerroum-El Amri, Xiao Tan, Lixian Qin, Maurice Pagano, Alain Hovnanian, Laetitia Furio, Bernard Pirotte
  • Patent number: 9469651
    Abstract: The invention includes halichondrin B analogs having pharmaceutical activity; in some cases, crystalline forms thereof, and in some cases, halichondrin B analogs having a further utility as synthetic intermediates.
    Type: Grant
    Filed: May 8, 2015
    Date of Patent: October 18, 2016
    Assignee: Eisai R&D Management Co., Ltd.
    Inventor: Yongbo Hu
  • Patent number: 9463504
    Abstract: A curing agent composition for making foundry molds, comprising 2,6-dihydroxybenzoic acid. In a sand composition for making foundry molds, it is preferable to use simultaneously: an acid-hardening resin which contains both a binder composition for making foundry molds which comprises one or more 5-position-substituted furfural compounds selected from the group consisting of 5-hydroxymethylfurfural and 5-acetoxymethylfurfural, and the curing agent composition for making foundry molds which comprises 2,6-dihydroxybenzoic acid. It is preferable that the content of 2,6-dihydroxybenzoic acid in the curing agent composition is 10 to 80 wt %.
    Type: Grant
    Filed: March 14, 2013
    Date of Patent: October 11, 2016
    Assignee: KAO CORPORATION
    Inventors: Takashi Joke, Toshiki Matsuo
  • Patent number: 9364468
    Abstract: The present invention relates to a pharmaceutical composition for preventing or treating tuberculosis, comprising: (a) a pharmaceutically effective amount of a compound represented by the following chemical formula 1; and (b) a pharmaceutically acceptable carrier. Chemical formula 1 The compound contained as an active ingredient of the present invention inhibits the expression and activity of CO-DH in tubercle bacillus so as to effectively block the detoxification of carbon monoxide, which is an important survival factor of tubercle bacillus, and is safe for the human body since the compound targets CO-DH which does not exist in the human body. In addition, the compound creates a synergistic effect when combined with a conventional tuberculostatic drug, and thus can be more effective for treating tuberculosis.
    Type: Grant
    Filed: February 13, 2013
    Date of Patent: June 14, 2016
    Assignee: INDUSTRY-ACADEMIC COOPERATION FOUNDATION, YONSEI UNIVERSITY
    Inventors: Young Min Kim, Seung Jung Han, Tae Gwon Oh, Sae Woong Park, Sang Nae Cho, Mi Young Hahn, Jee Hee Suh, Kyu Yang Yi
  • Patent number: 9334255
    Abstract: An improved method is described for making single isomers of synthetic benzoprostacyclin analogue compounds, in particular the pharmacologically active 314-d isomer of beraprost. In contrast to the prior art, the method is stereoselective and requires fewer steps than the known methods for making these compounds.
    Type: Grant
    Filed: March 12, 2015
    Date of Patent: May 10, 2016
    Assignee: Lung Biotechnology PBC
    Inventors: Vijay Sharma, Hitesh Batra, Sudersan Tuladhar
  • Patent number: 9248111
    Abstract: The present invention relates to compositions and methods for the treatment of Parkinson's disease and related disorders. More specifically, the present invention relates to novel combinatorial therapies of Parkinson's disease and related disorders targeting the alpha-synuclein aggregation network. In particular, the invention relates to compounds which, alone or in combination(s), can effectively protect neuronal cells from alpha-synuclein aggregates. The invention also relates to methods of producing a drug or a drug combination for treating Parkinson's disease and to methods of treating Parkinson's disease or a related disorder.
    Type: Grant
    Filed: August 29, 2014
    Date of Patent: February 2, 2016
    Assignee: PHARNEXT
    Inventors: Daniel Cohen, Serguei Nabirochkin, Ilya Chumakov, Rodolphe Hajj
  • Patent number: 9181231
    Abstract: Described herein are methods for using compounds that activate pyruvate kinase.
    Type: Grant
    Filed: May 3, 2012
    Date of Patent: November 10, 2015
    Assignee: AGIOS PHARMACEUTICALS, INC
    Inventor: Shin-San M. Su
  • Patent number: 9120814
    Abstract: The present invention relates to a compound having benzopyran core, a preparation method of the derivatives by liquid phase synthesis and solid phase synthesis through diversity-oriented synthesis, and an anticancer agent comprising the compound that exhibit excellent cytotoxicity against cancer cells.
    Type: Grant
    Filed: June 9, 2009
    Date of Patent: September 1, 2015
    Assignee: SNU R&DB FOUNDATION
    Inventors: Seung Bum Park, Hwan Jong Jang, Sung Kon Ko, EunHa Kim, Sangmi Oh, Jongmin Park
  • Patent number: 9120728
    Abstract: The present invention relates to novel substituted phenoxyethylamine derivatives, useful as modulators of cortical and basal ganglia dopaminergic and N-methyl-D-aspartate (NMDA) receptor-mediated glutamatergic neurotransmission. In other aspects the invention relates to the use of these compounds in a method for therapy and to pharmaceutical compositions comprising the compounds of the invention.
    Type: Grant
    Filed: January 23, 2015
    Date of Patent: September 1, 2015
    Assignee: Integrative Research Laboratories Sweden AB
    Inventors: Clas Sonesson, Jonas Karlsson, Peder Svensson
  • Publication number: 20150148334
    Abstract: This invention provides compounds of formula I-A or I-B: wherein HY, G1, G2, R2, R12, W1, W2, n, and Ring A are as described in the specification. The compounds are inhibitors of PI3K and/or mTor and are thus useful for treating proliferative, inflammatory, or cardiovascular disorders.
    Type: Application
    Filed: June 27, 2014
    Publication date: May 28, 2015
    Inventors: Brian S. Freeze, Masaaki Hirose, Hong Myung Lee, Todd B. Sells, Zhan Shi, Leo R. Takaoka, Stepan Vyskocil, Tianlin Xu
  • Publication number: 20150148343
    Abstract: The present invention relates to novel sirtuin-modulating compounds, corresponding pharmaceutical compositions comprising a sirtuin-modulating compound, alone and/or in combination with another therapeutic agent, and methods of use thereof. Sirtuin-modulating compounds of the present invention may be used for increasing the lifespan of a cell, and treating and/or preventing a wide variety of diseases and disorders including, for example, diseases or disorders related to aging or stress, diabetes, obesity, neurodegenerative diseases, cardiovascular disease, blood clotting disorders, inflammation, cancer, and/or flushing as well as diseases or disorders that would benefit from increased mitochondrial activity.
    Type: Application
    Filed: January 29, 2015
    Publication date: May 28, 2015
    Inventors: Robert B. PERNI, Christopher Oalmann, Chi B. Vu
  • Publication number: 20150126529
    Abstract: Disclosed are azaindazole compounds of Formula (I): or a pharmaceutically acceptable salt thereof, wherein: X is O and Y is N; or X is S and Y is CH; Z is CR2 or N; Q is a heteroaryl; and R1 is defined herein. Also disclosed are methods of using such compounds in the treatment of at least one CYP17 associated condition, such as, for example, cancer, and pharmaceutical compositions comprising such compounds.
    Type: Application
    Filed: January 16, 2015
    Publication date: May 7, 2015
    Inventors: Upender Velaparthi, Peiying Liu
  • Patent number: 9023837
    Abstract: Described herein are pharmaceutical compositions and medicaments, and methods of using such pharmaceutical compositions and medicaments in the treatment of cancer.
    Type: Grant
    Filed: April 15, 2011
    Date of Patent: May 5, 2015
    Assignee: Colby Pharmaceutical Company
    Inventors: Hirak S. Basu, David A. Zarling, George Wilding, Farideh Mehraein-Ghomi, Dawn R. Church
  • Publication number: 20150119397
    Abstract: The present invention relates generally to compositions and methods for treating cancer and neoplastic disease. Provided herein are substituted amidopyridine or amidopyridazine derivative compounds and pharmaceutical compositions comprising said compounds. The subject compounds and compositions are useful for inhibition histone demethylase. Furthermore, the subject compounds and compositions are useful for the treatment of cancer, such as prostate cancer, breast cancer, bladder cancer, lung cancer and/or melanoma and the like.
    Type: Application
    Filed: January 8, 2015
    Publication date: April 30, 2015
    Inventors: Young K. Chen, Toufike Kanouni, Zhe Nie, Jeffrey Alan Stafford, James Marvin Veal, Michael Brennan Wallace
  • Publication number: 20150111910
    Abstract: Compounds of formula (I) are of use in the modulation of Kv3.1, Kv.3.2 and Kv3.3 channels and have utility in the treatment or prevention of related disorders.
    Type: Application
    Filed: May 22, 2013
    Publication date: April 23, 2015
    Applicant: AUTIFONY THERAPEUTICS LIMITED
    Inventors: Agostino Marasco, Giuseppe Alvaro, Anne Dècor, Dieter Hamprecht, Paolo Dambruoso, Simona Tommasi
  • Publication number: 20150111888
    Abstract: The present invention provides a small compound targeting at TACC3. The present invention further provides a drug, particularly, an anticancer agent, comprising the small compound targeting at TACC3. A compound represented by the general formula (I) or a pharmaceutically acceptable salt, solvate, or ester derivative thereof binds to TACC3 and inhibits cell growth. Thus, these compounds can be used as drugs, particularly, anticancer agents.
    Type: Application
    Filed: April 30, 2013
    Publication date: April 23, 2015
    Inventors: Ryoji Yao, Hiroyuki Osada, Yasumitsu Kondoh
  • Publication number: 20150098918
    Abstract: Stable cream gel dermatological/cosmetic compositions useful, e.g., for the treatment of acne vulgaris, contain, formulated into a physiologically acceptable medium, a homogeneous dispersion of at least one dispersed retinoid, dispersed benzoyl peroxide, at least one lipophilic compound and at least one gelling agent.
    Type: Application
    Filed: December 15, 2014
    Publication date: April 9, 2015
    Inventors: Claire MALLARD, Fabienne LOUIS, Emmanuelle At GUILLET
  • Publication number: 20150094281
    Abstract: The invention relates to macrocyclic picolinamides of Formula I and their use as fungicides.
    Type: Application
    Filed: September 29, 2014
    Publication date: April 2, 2015
    Inventors: Fangzheng Li, Kevin G. Meyer, James M. Renga, Chenglin Yao, Jeremy Wilmot, Jessica Herrick, Karla Bravo-Altamirano, Timothy Boebel
  • Patent number: 8993619
    Abstract: The invention relates to compounds of formula (I): useful for treating disorders mediated by acyl coA-diacylglycerol acyl transferase 1 (DGAT1), e.g. metabolic disorders. The invention also provides methods of treating such disorders, and compounds and compositions etc. for their treatment.
    Type: Grant
    Filed: April 26, 2013
    Date of Patent: March 31, 2015
    Assignee: Novartis AG
    Inventors: Sejal Patel, Justin Mao, Qian Liu, Rui Zheng, Tyler Harrison, Rohit Duvadie, Xin Chen, Frederic Zecri, Jay Larrow, Xuchun Zheng, Yizong Zhou, Jiong Ye, Yiping Ding, Yu Gai
  • Publication number: 20150087676
    Abstract: Methods of inhibiting cytochrome P450 enzymes are provided that can be used for improving the treatment of diseases by preventing degradation of drugs or other molecules by cytochrome P450. Pharmaceutical compositions are provided that can act as boosters to improve the pharmacokinetics, enhance the bioavailability, and enhance the therapeutic effect of drugs that undergo in vivo degradation by cytochrome P450 enzymes.
    Type: Application
    Filed: December 9, 2014
    Publication date: March 26, 2015
    Inventors: Michael Eissenstat, Dehui Duan
  • Patent number: 8987258
    Abstract: The present invention relates to novel chromenone analog sirtuin modulator compounds of Formula (I): or pharmaceutically acceptable salts thereof, corresponding pharmaceutical compositions and treatment methods and combination therapies thereof for use in increasing the lifespan of a cell, and treating and/or preventing a wide variety of diseases and disorders including, for example, diseases or disorders related to aging or stress, diabetes, obesity, neurodegenerative diseases, cardiovascular disease, blood clotting disorders, inflammation, cancer, and/or flushing as well as diseases or disorders that would benefit from increased mitochondrial activity.
    Type: Grant
    Filed: September 29, 2009
    Date of Patent: March 24, 2015
    Inventors: Christopher Oalmann, Robert B. Perni, Chi B. Vu
  • Publication number: 20150079182
    Abstract: A topical composition which includes a silica microspheres and an active ingredient in the amount of 0.01 to 15.0% w/w wherein the active ingredient is selected from adapalene, an antibiotic, tazarotene, tretinoin, a retinoid, or any combination thereof. The topical composition may also include benzoyl peroxide as an active ingredient. The topical compositions provide sustained release of the active ingredient so as to reduce skin irritation.
    Type: Application
    Filed: November 24, 2014
    Publication date: March 19, 2015
    Inventors: Marina Shevachman, Amira Ze' Evi, Eilon Asculai, Batella Binyaminovich, Nir Avram
  • Patent number: 8975263
    Abstract: The present invention relates to a compound or a pharmacologically acceptable salt thereof having an excellent glucose lowering effect. A compound represented by the following general formula (I) or a pharmacologically acceptable salt thereof: wherein R1 represents a C1-C3 alkyl group, each substituent R2 may be the same or different and may each represent a C1-C3 alkyl group, R3 represents an optionally substituted pyridyl group or the like, R4 and R5, which are the same or different, each represent a C1-C3 alkyl group, R6 and R7, which are the same or different, each represent a C1-C3 alkyl group, and n represents 0 to 3.
    Type: Grant
    Filed: May 30, 2014
    Date of Patent: March 10, 2015
    Assignee: Daiichi Sankyo Company, Limited
    Inventors: Shigeo Yamanoi, Katsuji Kagechika, Tsuyoshi Soneda, Yuichi Ochiai, Hidenori Namiki, Fuminao Doi, Madoka Hoshino, Shoko Yoshida
  • Publication number: 20150065504
    Abstract: Disclosed herein are new antiviral compounds, together with pharmaceutical compositions that include one or more antiviral compounds, and methods of synthesizing the same. Also disclosed herein are methods of ameliorating and/or treating a paramyxovirus viral infection with one or more small molecule compounds. Examples of paramyxovirus infection include an infection caused by human respiratory syncytial virus (RSV).
    Type: Application
    Filed: August 19, 2014
    Publication date: March 5, 2015
    Inventors: Guangyi Wang, Leonid Beigelman, Anh Truong, Carmela Napolitano, Daniele Andreotti, Haiying He, Karin Ann Stein
  • Publication number: 20150065494
    Abstract: The present invention provides an aminostyrylbenzofuran compound of Formula (I), and a pharmaceutical composition comprising same. The pharmaceutical composition of the present invention comprising the compound of Formula (I), a pharmaceutically acceptable salt, an isomer, a hydrate, and a solvate thereof as an active ingredient can be useful for the prevention and treatment of degenerative brain diseases caused by accumulation of beta-amyloid.
    Type: Application
    Filed: April 1, 2013
    Publication date: March 5, 2015
    Inventors: Dong Jin Kim, Kyung Ho Yoo, Young Soo Kim, Woong Seo Park, Yong Koo Kang, Hye Yun Kim, Yun Kyung Kim, Ki Duk Park, Maeng Sup Kim, Kwee Hyun Suh, Young Gil Ahn
  • Patent number: 8969352
    Abstract: The present invention is directed to compounds of Formula I: wherein X is N or CR1; Y is N or CR2; R1 is H, alkoxy, halo, triazolyl, pyrimidinyl, oxazolyl, isoxazole, oxadiazolyl, or pyrazolyl; R2 is H, alkyl, alkoxy, or halo; Z is NH or O; R3 is H, alkyl, alkoxy, halo, or triazolyl; R4 is H or alkyl; or R3 and R4, together with the atoms to which they are attached, form a 6-membered aryl ring or a 5- or 6-membered heteroaryl ring; R5 is pyridyl, pyrazinyl, or pyrimidinyl, wherein the pyridyl, pyrazinyl, or pyrimidinyl is optionally substituted with halo or alkyl; and n is 1 or 2. Methods of making the compounds of Formula I are also described. The invention also relates to pharmaceutical compositions comprising compounds of Formula I. Methods of using the compounds of the invention are also within the scope of the invention.
    Type: Grant
    Filed: March 12, 2014
    Date of Patent: March 3, 2015
    Assignee: Janssen Pharmaceutica NV
    Inventors: Christine F. Gelin, Terry P. Lebold, Brock T. Shireman
  • Patent number: 8969345
    Abstract: A dibenzoxepin derivative represented by the following general formula (I) wherein Y is a hydrogen atom and the like, RA is a hydrogen atom and the like, X is the formula (b3) wherein RB is a hydrogen atom and the like, and the like, A is the formula (a18) wherein R1 is a hydrogen atom and the like, and RC and RD are the same or different and each is a hydrogen atom and the like, and the like, which has a PPAR? agonist activity and the like, and useful as a therapeutic agent and/or prophylaxis agent and the like for type 2 diabetes and the like, or a pharmaceutically acceptable salt thereof and the like is provided.
    Type: Grant
    Filed: August 3, 2012
    Date of Patent: March 3, 2015
    Assignee: Kyowa Hakko Kirin Co., Ltd.
    Inventors: Keisuke Yamamoto, Tomohiro Tamura, Rina Nakamura, Kimihisa Ueno, Shintaro Hosoe
  • Publication number: 20150056141
    Abstract: It has been found that efficient screening for a compound having anticancer activity can be achieved by selecting a compound having activity to induce alternative autophagy using, as an index, formation of fluorescent bright spots due to aggregation of a lysosomal protein to which a fluorescent protein is attached in cells expressing the lysosomal protein.
    Type: Application
    Filed: February 7, 2013
    Publication date: February 26, 2015
    Applicant: National University Corporation Tokyo Medical and Dental University
    Inventors: Shigeomi Shimizu, Takamitsu Hosoya, Michiko Murohashi, Suguru Yoshida
  • Publication number: 20150056166
    Abstract: The present invention relates to flavone derivatives and to compositions containing one or more of these flavone derivatives. The present invention further relates to flavone derivatives or compositions for use in the treatment and/or prevention of a viral infection, and to a method of preventing or treating these infections.
    Type: Application
    Filed: March 22, 2013
    Publication date: February 26, 2015
    Inventors: Thomas Pietschmann, Sibylle Haid, Juliane Gentzsch, Christina Grethe, Elisabeth Davioud-Charvet, Don Antoine Lanfranchi, Mourad Elhabiri, Xavier Benlloch-Martin
  • Patent number: 8962660
    Abstract: The present invention provides compounds of Formula (I): or a stereoisomer, or a pharmaceutically acceptable salt thereof, wherein all of the variables are as defined herein. These compounds are GPR120 G protein-coupled receptor modulators which may be used as medicaments.
    Type: Grant
    Filed: March 12, 2014
    Date of Patent: February 24, 2015
    Assignee: Bristol-Myers Squibb Company
    Inventors: Hao Zhang, Peter T. W. Cheng, Sean Chen, Shiwei Tao, Shung C. Wu, Lidet A Negash
  • Patent number: 8952003
    Abstract: The present invention provides a sterol derivative or a pharmaceutically acceptable salt thereof having an activity to promote proliferation of neural stem cells. Namely, the present invention provides a sterol derivative represented by the general formula (I) (wherein Y represents optionally substituted lower alkyl or the like; Xa and Xb are the same or different, and represent a bond or the like; R1, R2, R3, R4, R7 and R8 are the same or different, and represent a hydrogen atom or the like; R5 and R6 are the same or different, and represent a hydrogen atom or the like; R9 represents a hydrogen atom or the like; R10 and R11 together represent a bond or the like; and R12 represents a hydrogen atom or the like) or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: July 22, 2010
    Date of Patent: February 10, 2015
    Assignee: Kyowa Hakko Kirin Co., Ltd
    Inventors: Kenji Uchida, Tsutomu Agatsuma, Kazuhiro Hibino, Setsuya Sasho, Kyoichiro Iida, Hideyuki Onodera
  • Publication number: 20150031727
    Abstract: [Problem] To provide a compound that has an intestinal phosphate transporter (NPT-IIb) inhibitory action and is useful as an active ingredient of an agent for treating and/or preventing hyperphosphatemia. [Means for Solution] The present inventors conducted their studies on a compound that has an NPT-IIb inhibitory action and is useful as an active ingredient of an agent for treating and/or preventing hyperphosphatemia. As a result, they created an aminoalkyl-substituted N-thienylbenzamide derivative which has NPT-IIb inhibitory action, thereby completing the present invention. The aminoalkyl-substituted N-thienylbenzamide derivative of the present invention has an NPT-IIb inhibitory action and can be used as an agent for preventing and/or treating hyperphosphatemia.
    Type: Application
    Filed: October 25, 2012
    Publication date: January 29, 2015
    Applicant: ASTELLAS PHARMA INC.
    Inventors: Masanori Miura, Daisuke Kaga, Susumu Watanuki, Shunichiro Hachiya, Takao Okuda, Ippei Sato, Mai Isomura, Kazuhiro Terai, Yoh Terada
  • Publication number: 20150025046
    Abstract: The present invention relates to bicyclic himbacine derivatives of the formula or a pharmaceutically acceptable salt thereof, wherein: X is —O—, —N(R), —C(R8)(R9) or —C(O)—; and Y is —O—, —N(R), —C(R8)(R9) or —C(O)— and the remaining variables are described herein. The compounds of the invention are effective inhibitors of the PAR-1 receptor. The inventive compounds may be used for the treatment or prophylaxis of disease states such as ACS, secondary prevention of myocardial infarction or stroke, or PAD.
    Type: Application
    Filed: February 27, 2013
    Publication date: January 22, 2015
    Inventors: Mihir Mandal, Timothy A. Blizzard, Helen Chen, Harry Chobanian, Yan Guo, Barbara Pio, Zhicai Wu, Tesfaye Biftu, William J. Greenlee, Johnny Zhaoning Zhu
  • Patent number: 8937055
    Abstract: The present invention provides a compound having a muscle cell or adipocyte differentiation regulating action, useful for the prophylaxis or treatment of diseases such as diabetes, obesity, dyslipidemia and the like, and the like, and having superior efficacy. The present invention provides a compound represented by the formula: wherein each symbol is as defined in the description, or a salt thereof.
    Type: Grant
    Filed: July 14, 2011
    Date of Patent: January 20, 2015
    Assignee: Takeda Pharmaceutical Company Limited
    Inventors: Osamu Ujikawa, Kazuaki Takami, Nobuyuki Takakura, Nozomu Sakai