Polycyclo Ring System Having The Six-membered Hetero Ring As One Of The Cyclos (e.g., 1,3- And 1,4- Benzothiazines, Etc.) Patents (Class 514/224.2)
  • Patent number: 8389511
    Abstract: The present invention relates to a compound of the following formula (I) or a pharmaceutically acceptable salt thereof, being useful as a renin inhibitor. [wherein R1a is halogen, etc.; R1m is H, etc.; G1 is —N(R1b)—, etc.; G2 is —CO—, etc.; G3 is —C(R1c)(R1d)—, etc.; G4 is oxygen, etc.; R1b is optionally substituted C1-6 alkyl, etc.; R1c and R1d are independently the same or different, H, etc.; R3 is H, optionally substituted C1-6 alkyl, etc.; R3a, R3b, R3c and R3d are independently the same or different, and a group: -A-B (said A is single bond, etc., and said B is H, etc.), etc.; and n is 1, etc.
    Type: Grant
    Filed: December 19, 2008
    Date of Patent: March 5, 2013
    Assignee: Dainippon Sumitomo Pharma Co., Ltd.
    Inventors: Hiroyuki Nakahira, Yohei Ikuma, Nobuhisa Fukuda, Kozo Yoshida, Hidenori Kimura, Satoshi Suetsugu, Akira Fusano, Kiyoto Sawamura, Junya Ikeda, Yoshio Nakai
  • Publication number: 20130053373
    Abstract: Compounds and pharmaceutically acceptable salts of the compounds are disclosed, wherein the compounds have the structure of Formula I, as defined in the specification. Corresponding pharmaceutical compositions, methods of treatment, methods of synthesis, and intermediates are also disclosed.
    Type: Application
    Filed: August 28, 2012
    Publication date: February 28, 2013
    Inventors: Michael Aaron BRODNEY, Christopher Ryan BUTLER, Christopher John HELAL, Brian Thomas O'NEILL
  • Publication number: 20130040935
    Abstract: The invention relates to 5?-biphenyl-substituted cyclic ketoenols for therapeutic purposes, to pharmaceutical compositions and to their use in therapy, in particular for the prophylaxis and therapy of tumour disorders.
    Type: Application
    Filed: February 8, 2011
    Publication date: February 14, 2013
    Applicant: BAYER INTELLECTUAL PROPERTY GMBH
    Inventors: Ningshu Liu, Kai Thede, Philip Lienau, Arne Scholz, Christoph-Stephan Hilger, Ulf Bömer, Maher Najjar, Knut Eis, Reiner Fischer, Wahed Ahmed Moradi
  • Publication number: 20130035327
    Abstract: The present invention relates to modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator, compositions thereof, and methods therewith. The present invention also relates to methods of treating ABC transporter mediated diseases using such modulators.
    Type: Application
    Filed: October 8, 2012
    Publication date: February 7, 2013
    Inventors: Sara Hadida-Ruah, Anna Hazlewood, Peter Grootenhuis, Fredrick Van Goor, Ashvani Singh, Jinglan Zhou, Jason McCartney
  • Publication number: 20130018041
    Abstract: This invention is directed to compounds of formula (I): where n, m, Y, R1, R2, R3, R4 and R5 are disclosed herein, as isolated stereoisomers or mixtures thereof, or pharmaceutically acceptable salts thereof; pharmaceutical compositions comprising the compounds of formula (I); and methods of using the compounds and the pharmaceutical compositions in treating diseases or conditions associated with JAK2 activity.
    Type: Application
    Filed: September 14, 2012
    Publication date: January 17, 2013
    Applicant: Rigel Pharmaceutical, Inc.
    Inventors: Somasekhar Bhamidipati, Jeffrey Clough, Ankush Argade, Rajinder Singh, Vadim Markovtosov, Pingyu Ding, Jiaxin Yu, Andy Atuegbu, Hui Hong, Ihab Darwish, Sambaiah Thota
  • Publication number: 20130012501
    Abstract: Disclosed embodiments provide pyrimidinediamine compounds useful for inhibiting kinase activity, including the activity of polo-like kinase 1 (PLK1). Also disclosed are pharmaceutical compositions comprising these compounds and methods of treating diseases associated with kinase activity, in particular enhanced PLK1 catalytic activity, such as diseases associated with abnormal cell proliferation, including neoplastic disorders.
    Type: Application
    Filed: September 11, 2012
    Publication date: January 10, 2013
    Inventors: Rajinder Singh, Andy Atuegbu, John Ramphal, Hui Li, Marina Gelman, Jeffrey Clough, Carlos Valdez, Somasekhar Bhamidipati, Sambaiah Thota, Darren McMurtrie
  • Patent number: 8349829
    Abstract: The invention relates to antibacterial compounds of formula I wherein R1 represents alkoxy or halogen; U, V and W each represent CH, or one of U, V and W represents N and the others each represent CH; A represents CH2 or O; G is CH?CH-E wherein E represents a phenyl group mono- or di-substituted with halogen, or G is a group of one of the formulae hereafter wherein Z represent CH or N, Q represents O or S and K represents O or S; and salts of such compounds.
    Type: Grant
    Filed: June 2, 2009
    Date of Patent: January 8, 2013
    Assignee: Actelion Pharmaceuticals Ltd.
    Inventors: Christian Hubschwerlen, Georg Rueedi, Jean-Philippe Surivet, Cornelia Zumbrunn-Acklin
  • Patent number: 8349828
    Abstract: The invention relates to antibacterial compounds of formula I wherein n is 0 or 1; R1 represents H or F; U represents CH2 or, provided n is 1, O or NH; “-----” is a bond or is absent; V represents CH or N when “-----” is a bond, or CH2 or NH when “-----” is absent; W represents CH or N; A represents —(CH2)p—NH—(CH2)q— wherein p is 1 and q is 1 or 2 or, provided U represents CH2 and n is 1, p may also be 0 and q is then 2; G represents one of the groups 1 wherein Z represents N or CH and Q represents O or S; and Z0, Z1 and Z2 each represent CH, or Z0 and Z1 each represent CH and Z2 represents N, or Z0 represents CH, Z1 represents N and Z2 represents CH or N, or Z0 represents N and Z1 and Z2 each represent CH; and to salts of such compounds.
    Type: Grant
    Filed: February 19, 2009
    Date of Patent: January 8, 2013
    Assignee: Actelion Pharmaceuticals Ltd.
    Inventors: Christian Hubschwerlen, Georg Rueedi, Jean-Philippe Surivet, Cornelia Zumbrunn-Acklin
  • Publication number: 20120329775
    Abstract: The present invention provides compounds of formula (I) in which y, m, n, R1, R2 and Q are as defined in the specification, a process for their preparation, pharmaceutical compositions containing them and their use in therapy.
    Type: Application
    Filed: June 4, 2012
    Publication date: December 27, 2012
    Inventors: Rhonan Ford, Andrew Mather, Antonio Mete, Ian Millichip
  • Patent number: 8338407
    Abstract: The present invention relates to a fused aminodihydrothiazine derivative of formula (I): wherein X is hydrogen or fluorine; A is CH or N; Y is methyl, ethyl, monofluoromethyl, difluoromethyl, trifluoromethyl, difluoroethyl, methoxy, ethoxy, methoxymethyl or —C?N; and pharmaceutically acceptable salts thereof; which compound has an A? production inhibitory effect or a BACE1 inhibitory effect and is useful as a prophylactic or therapeutic agent for a neurodegenerative disease caused by A? and typified by Alzheimer-type dementia.
    Type: Grant
    Filed: January 20, 2012
    Date of Patent: December 25, 2012
    Assignee: Eisai R&D Management Co., Ltd.
    Inventors: Adrian Hall, Christopher Neil Farthing
  • Publication number: 20120322791
    Abstract: The present invention provides Pyrazolopyrimidine Compounds of Formula (I): wherein L, T, Z, U, V, W, R3, R6, R7, R8, and m are as defined herein, and pharmaceutically acceptable salts of such Pyrazolopyrimidine Compounds. The Pyrazolopyrimidine Compounds are useful in the treatment of cancer and other diseases or disorders wherein mTOR is deregulated.
    Type: Application
    Filed: January 18, 2011
    Publication date: December 20, 2012
    Inventors: M. Arshad Siddiqui, Yang Nan, Mehul F. Patel, Panduranga Adulla P. Reddy, Umar Faruk Mansoor, Zhaoyang Meng, Lalanthi Dilrukshi Vitharana, Lianyun Zhao, Amit K. Mandal, Duan Liu, Shuyi Tang, Andrew McRiner, David B. Belanger, Patrick J. Curran, Chaoyang Dai, Angie R. Angeles, Liping Yang, Matthew Hersh Daniels
  • Publication number: 20120322792
    Abstract: The present invention relates to anti-cancer therapeutics. In certain aspects, cancers are treated with a combination of an anti-EGFR agent and an agent that increases the activity of the KLF6 tumor suppressor gene and/or an agent that increases activity of the FOXO1 tumor suppressor gene. In a preferred aspect, the anti-EGFR agent erlotinib a tricyclic agent compound, are used in combination to treat non-small cell lung cancer in a patient with primary or acquired drug resistance to erlotinib, and wherein the tricyclic agent is administered in an amount that does not lead to a substantial central nervous system effect. In additional aspects, the invention relates to compositions and kits useful for treating cancers, methods for screening for compounds that enhance the activity of anti-EGFR agent, and methods for determining whether a patient will respond to anti-EGFR therapy.
    Type: Application
    Filed: January 11, 2012
    Publication date: December 20, 2012
    Applicant: MOUNT SINAI SCHOOL OF MEDICINE
    Inventors: Goutham Narla, Michael Ohlmeyer, Matthew David Galsky
  • Publication number: 20120289493
    Abstract: The present disclosure relates to compounds that are sodium channel inhibitors and to their use in the treatment of various disease states, including cardiovascular diseases and diabetes. In particular embodiments, the structure of the compounds is given by Formula I: wherein Q, R1, X1, X2, Y and R2 are as described herein, to methods for the preparation and use of the compounds and to pharmaceutical compositions containing the same.
    Type: Application
    Filed: May 8, 2012
    Publication date: November 15, 2012
    Inventors: Britton Kenneth Corkey, Elfatih Elzein, Robert H. Jiang, Rao V. Kalla, Tetsuya Kobayashi, Dmitry Koltun, Xiaofen Li, Ruben Martinez, Gregory Notte, Eric Q. Parkhill, Thao Perry, Jeff Zablocki, Chandrasekar Venkataramani, Michael Graupe, Juan Guerrero
  • Publication number: 20120270863
    Abstract: The present invention relates to arylcarbonyl and heteroarylcarbonyl anthranilate compounds that may be useful as anti-fibrotic agents. The present invention also relates to methods for their preparation, pharmaceutical compositions containing these compounds and uses of these compounds in the treatment disorders.
    Type: Application
    Filed: October 21, 2010
    Publication date: October 25, 2012
    Applicant: Fibrotech Therapeutics Pty Ltd
    Inventors: Spencer John Williams, Steven Zammit, Darren James Kelly
  • Publication number: 20120270864
    Abstract: The present invention relates to compounds of Formula (I): and pharmaceutically acceptable salts thereof, to their use in the treatment of bacterial infections, and to their methods of preparation.
    Type: Application
    Filed: May 18, 2012
    Publication date: October 25, 2012
    Inventors: Andrew Aydon Godfrey, Janelle Comita-Prevoir, Mark Cronin, Bolin Geng, Folkert Reck
  • Publication number: 20120258961
    Abstract: The present invention provide a medicament for treating the diseases induced by production, secretion or deposition of amyloid-? proteins, for example, a compound of the following formula (I) wherein R1, R2a, R2b, R3a, R3b, R4a, R4b, ring A, Y and the dotted line are defined in the specification, its pharmaceutically acceptable salt or a solvate thereof.
    Type: Application
    Filed: December 22, 2010
    Publication date: October 11, 2012
    Applicant: SHIONOGI & CO., LTD.
    Inventors: Shinji Suzuki, Yuuji Kooriyama
  • Patent number: 8278441
    Abstract: The present invention provides BACE inhibitors of Formula I: methods for their use, intermediates, and methods for their preparation.
    Type: Grant
    Filed: July 6, 2010
    Date of Patent: October 2, 2012
    Assignee: Eli Lilly and Company
    Inventors: Dustin James Mergott, Grant Mathews Vaught
  • Publication number: 20120245127
    Abstract: The present disclosure provides methods for the treatment of cell proliferative disorders by administration of a Syk kinase or Syk/Flt-3 kinase inhibitor. Cell proliferative disorders treatable by the methods include, hematopoietic neoplasms and virally associated tumors. The compounds are also directed to therapeutic or prophylactic inhibition of tumor metastasis.
    Type: Application
    Filed: June 4, 2012
    Publication date: September 27, 2012
    Applicant: Rigel Pharmaceuticals, Inc.
    Inventors: Esteban Masuda, Donald G. Payan, Elliot B. Grossbard, Somasekhar Bhamidipati, Rajinder Singh
  • Publication number: 20120245154
    Abstract: The present invention relates to an agent for treating or preventing disease induced by production, secretion and/or deposition of amyloid ? protein, for example, a compound of formula (I), wherein, R1, R2a, R2b R3, R4a, R4b, ring A, and dashed line are described in this specification, its pharmaceutically acceptable salt or a solvate thereof.
    Type: Application
    Filed: December 8, 2010
    Publication date: September 27, 2012
    Applicant: SHIONOGI & CO., LTD.
    Inventors: Kousuke Anan, Yukio Tada, Akihiro Hori, Moriyasu Masui
  • Publication number: 20120245153
    Abstract: Compounds useful as allosteric potentiators/positive allosteric modulators of the metabotropic glutamate receptor subtype 4 (mGluR4) and use thereof.
    Type: Application
    Filed: September 7, 2010
    Publication date: September 27, 2012
    Applicant: VANDERBILT UNIVERSITY
    Inventors: P. Jeffrey Conn, Craig W. Lindsley, Corey R. Hopkins, Charles David Weaver, Colleen M. Niswender, Darren W. Engers, Patrick R. Gentry, Yiu-Yin Cheung, James M. Salovich, Rocco D. Gogliotti
  • Publication number: 20120245152
    Abstract: A compound of the general formula (I): [wherein, R1 represents a halogen atom, or the like, R2 represents a hydrogen atom, or the like, R3 and R4, each independently, represent a hydrogen atom, a C1-4 alkyl group, or the like, R5 represents a hydrogen atom, a halogen atom, or the like, R6 represents a hydrogen atom, a halogen atom, or the like, R7 and R8, each independently, represent a hydrogen atom, a halogen atom, or the like, R9 and R10, each independently, represent a hydrogen atom, a C1-4 alkyl group, R11 and R12, each independently, represent a hydrogen atom, a C1-4 alkyl group, or the like, X represents an oxygen atom, a group —CH2—, or the like, Y represents a nitrogen atom, a group ?CH—, or the like, and Z represents a nitrogen atom, or the like] or a pharmacologically acceptable salt thereof, which has an excellent suppressive action on platelet aggregation, and is useful for prevention and/or treatment of thromboembolism.
    Type: Application
    Filed: August 27, 2010
    Publication date: September 27, 2012
    Applicant: DAIICHI SANKYO COMPANY, LIMITED
    Inventors: Tatsuya Nishi, Masashi Hasegawa, Yumi Shinagawa-ku, Yuichi Ochiai, Ryoko Kitazawa, Hiroshi Susaki
  • Publication number: 20120245155
    Abstract: The present invention provides, for example, a compound mentioned below as a medicament for treating or preventing the diseases induced by production, secretion or deposition of amyloid-?proteins. A compound of the formula (I): wherein R1, R2a, R2b, R3, R4, R5a, R5b, R6a, R6b, X, Y, Z, ring A and the dashed lines are defined in the specification, its pharmaceutically acceptable salt or a solvate thereof.
    Type: Application
    Filed: December 9, 2010
    Publication date: September 27, 2012
    Applicant: Shionogi & Co., Ltd.
    Inventors: Syuhei Yoshida, Issei Kato, Kouki Fuchino, Yuuji Kooriyama, Yoshiyasu Baba, Norihiko Tanimoto
  • Publication number: 20120232059
    Abstract: Compounds of the present invention, and pharmaceutically acceptable compositions thereof, are useful as modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator (“CFTR”). The present invention also relates to methods of treating ABC transporter mediated diseases using compounds of the present invention.
    Type: Application
    Filed: May 18, 2012
    Publication date: September 13, 2012
    Applicant: Vertex Pharmaceuticals Incorporated
    Inventors: Sara Hadida-Ruah, Matthew Hamilton, Mark Miller, Peter D.J. Grootenhuis, Brian Bear, Jason McCartney, Jinglan Zhou, Frederick van Goor
  • Publication number: 20120220574
    Abstract: The present invention provides arylpiperazine derivatives which can be advantageously used for treating schizophrenia and related psychoses such as acute manic, bipolar disorder, autistic disorder, and depression.
    Type: Application
    Filed: May 7, 2012
    Publication date: August 30, 2012
    Inventors: Laxminarayan Bhat, Prabhu Prasad Mohapatra, Kouacou Adiey
  • Patent number: 8232391
    Abstract: Antibacterial compounds, compositions containing them, and methods of use for the inhibition of bacterial activity and the treatment, prevention or inhibition of bacterial infection.
    Type: Grant
    Filed: July 9, 2010
    Date of Patent: July 31, 2012
    Assignee: Janssen Pharmaceutica NV
    Inventors: Brett D. Allison, Laurent Gomez, Cheryl A. Grice, Michael D. Hack, Brian J. Morrow, S. Timothy Motley, Alejandro Santillan, Jr., Karen J. Shaw, Kimberly L. Schwarz, Liu Y. Tang, Hariharan Venkatesan, John J. M. Wiener
  • Publication number: 20120190672
    Abstract: The present invention relates to a fused aminodihydrothiazine derivative of formula (I): wherein X is hydrogen or fluorine; A is CH or N; Y is methyl, ethyl, monofluoromethyl, difluoromethyl, trifluoromethyl, difluoroethyl, methoxy, ethoxy, methoxymethyl or —C?N; and pharmaceutically acceptable salts thereof; which compound has an A? production inhibitory effect or a BACE1 inhibitory effect and is useful as a prophylactic or therapeutic agent for a neurodegenerative disease caused by A? and typified by Alzheimer-type dementia.
    Type: Application
    Filed: January 20, 2012
    Publication date: July 26, 2012
    Applicant: EISAI R&D MANAGEMENT CO., LTD.
    Inventors: Adrian Hall, Christopher Neil Farthing, Jose Luis Castro Pineiro
  • Publication number: 20120184518
    Abstract: Methods for the treatment and/or prevention of an inflammatory disease or disorder through administration of an inhibitor of a glutaminyl peptide cyclotransferase. Inflammatory diseases or disorders treated or prevented by methods disclosed herein include mild cognitive impairment (MCI), rheumatoid arthritis, atherosclerosis, restenosis, pancreatitis, sepsis and peritonitus. Further provided are respective diagnostic methods, assays and kits.
    Type: Application
    Filed: January 20, 2012
    Publication date: July 19, 2012
    Applicant: PROBIODRUG AG
    Inventors: Stephan Schilling, Holger Cynis, Torsten Hoffman, Hans-Ulrich Demuth
  • Patent number: 8217029
    Abstract: The invention relates to compounds of formula (I) wherein U, V, W, X, R1, R2, R3, R4, R5, R6, A, B, D, E, G, m, and n are as defined in the description, to pharmaceutically acceptable salts of such compounds for use in the manufacture of a medicament for the prevention or treatment of a bacterial infection. Certain compounds of formula (I) are new and are also part of this invention.
    Type: Grant
    Filed: April 11, 2008
    Date of Patent: July 10, 2012
    Assignee: Actelion Pharmaceuticals Ltd
    Inventors: Daniel Bur, Christian Hubschwerlen, Georg Rueedi, Jean-Philippe Surivet, Cornelia Zumbrunn-Acklin
  • Publication number: 20120165322
    Abstract: The present invention relates to compounds of formula (I): and pharmaceutically acceptable salts thereof, wherein R1 and R2 are as defined herein. The invention also relates to pharmaceutical compositions comprising these compounds, methods of using these compounds in the treatment of various diseases and disorders, processes for preparing these compounds and intermediates useful in these processes.
    Type: Application
    Filed: June 29, 2011
    Publication date: June 28, 2012
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: Brian Nicholas Cook, Jennifer A. Kowalski, Xiang Li, Daniel Richard Marshall, Sabine Schlyer, Robert Sibley, Lana Louise Smith-Keenan, Fariba Soleymanzadeh, Ronald John Sorcek, Erick Richard Roush Young, Yunlong Zhang
  • Publication number: 20120149691
    Abstract: The invention provides compounds of formula I: or a salt thereof as described herein. The invention also provides pharmaceutical compositions comprising a compound of formula I, processes for preparing compounds of formula I, intermediates useful for preparing compounds of formula I, and therapeutic methods for suppressing an immune response or treating cancer or a hematologic malignancy using compounds of formula I.
    Type: Application
    Filed: July 30, 2010
    Publication date: June 14, 2012
    Applicant: BioCryst Pharmaceuticals, Inc.
    Inventors: Yarlagadda S. Babu, Yarlagadda S. Babu, Pravin L. Kotian, V. Satish Kumar, Minwan Wu, Tsu-Hsing Lin
  • Publication number: 20120148689
    Abstract: The present invention is related to the composition and methods of manufacture of orally-dissolvable, edible films as a vehicle for the non-invasive administration of active drugs through the mucosal tissues of the oral cavity. The films include a water soluble film-forming polymer such as pullulan. Methods for producing the films are also disclosed.
    Type: Application
    Filed: February 17, 2012
    Publication date: June 14, 2012
    Inventor: Todd Maibach
  • Patent number: 8198269
    Abstract: A compound represented by the general formula: wherein Ring A is a C6-14 aryl group or the like, L is —NRLCO— or the like (wherein RL is a hydrogen atom or the like), Ring B is a C6-14 aryl group or the like, X is a C1-3 alkylene group or the like, Y is a C1-3 alkylene group or the like, Z is an oxygen atom or the like, R1 and R2 are each independently a hydrogen atom or the like, and R3, R4, R5 and R6 are independently a hydrogen atom, a halogen atom or the like, or a pharmaceutically acceptable salt thereof, or a solvate thereof, has an A? production inhibitory effect or a BACE1 inhibitory effect and is useful as a therapeutic agent for a neurodegenerative disease caused by A? and typified by Alzheimer-type dementia.
    Type: Grant
    Filed: September 28, 2009
    Date of Patent: June 12, 2012
    Assignee: Eisai R&D Management Co., Ltd.
    Inventors: Takafumi Motoki, Kunitoshi Takeda, Yoichi Kita, Mamoru Takaishi, Yuichi Suzuki, Tasuku Ishida
  • Patent number: 8193179
    Abstract: Antibacterial compounds including 3-amino-6-(1-amino-ethyl)-tetrahydropyran derivatives are provided, and methods of treatment or prevention of bacterial infection with such compounds are provided.
    Type: Grant
    Filed: June 13, 2008
    Date of Patent: June 5, 2012
    Assignee: Actelion Pharmaceuticals, Ltd
    Inventors: Christian Hubschwerlen, Georg Rueedi, Jean-Philippe Surivet, Cornelia Zumbrunn-Acklin
  • Patent number: 8188073
    Abstract: The present invention relates to a compound, useful as a mineralocorticoid receptor-modulating agent, of the following formula [I]: wherein Ring A is a benzene ring optionally having a substituent(s) other than R1 etc, R1 is a group of the formula: RaSO2NH— etc, Ra is an alkyl group etc, R2 and R3 are each a hydrogen atom, a phenyl group, an optionally substituted alkyl group etc, X is an oxygen atom etc, Y is a group of the formula: —C(?O)— etc, Ar is an optionally substituted aryl group or an optionally substituted heteroaryl group, Q is a single bond, an alkylene group etc, or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: June 24, 2011
    Date of Patent: May 29, 2012
    Assignee: Mitsubishi Tanabe Pharma Corporation
    Inventors: Toru Iijima, Yasuo Yamamoto, Hidenori Akatsuka, Takayuki Kawaguchi
  • Publication number: 20120122773
    Abstract: The present invention provides a compound of formula (I): wherein R1a is optionally substituted C1-6 alkyl, etc.; R1m is hydrogen atom, etc.; G1, G2, G3 and G4 are (i), etc. ((i) G1 is —N(R1b)—, G2 is —CO—, G3 is —C(R1c)(R1d)—, and G4 is oxygen, etc.); R1b is optionally substituted C1-6 alkyl, etc.; R1c and R1d are each independently optionally substituted C1-6 alkyl, etc.; R2 is optionally substituted C1-6 alkyl, etc.; R3a, R3b, R3c and R3d are each independently a group: -A-B (A is a single bond, etc., B is hydrogen atom, etc.), etc.; n is 1, etc.; R5 is C1-4 alkoxycarbonyl, etc., or a pharmaceutically acceptable salt thereof, which is useful as a renin inhibitor.
    Type: Application
    Filed: June 24, 2010
    Publication date: May 17, 2012
    Applicant: DAINIPPON SUMITOMO PHARMA CO., LTD.
    Inventors: Satoshi Suetsugu, Nobuhisa Fukuda, Yoshio Nakai, Takashi Takada, Yohei Ikuma, Hiroyuki Nakahira
  • Publication number: 20120122855
    Abstract: The present invention features benzoxazines, benzothiazines, and related compounds that inhibit nitric oxide synthase (NOS), particularly those that selectively inhibit neuronal nitric oxide synthase (nNOS) in preference to other NOS isoforms. The NOS inhibitors of the invention, alone or in combination with other pharmaceutically active agents, can be used for treating or preventing various medical conditions.
    Type: Application
    Filed: January 27, 2012
    Publication date: May 17, 2012
    Applicant: NeurAxon, Inc.
    Inventors: Jailall RAMNAUTH, Subhash C. Annedi, Sarah Silverman, Peter Dove, Shawn Maddaford, Suman Rakhit
  • Publication number: 20120108576
    Abstract: The present invention provides compounds, salts and hydrates of Formula I, wherein the variables Ar1, R2, R3, R4, r, q, and t are defined herein. Certain compounds of Formula I described herein possess potent antiviral activity. The invention also provides compounds of Formula I that are potent and/or selective inhibitors of Hepatitis C virus replication. Certain compounds described herein inhibit assembly of the HCV replication complex. The invention also provides pharmaceutical compositions containing one or more compounds of Formula I, or a salt, solvate, or acylated prodrug of such compounds, and one or more pharmaceutically acceptable carriers, excipients, or diluents. The invention further comprises methods of treating patients suffering from certain infectious diseases by administering to such patients an amount of a compound of Formula I effective to reduce signs or symptoms of the disease. These infectious diseases include viral infections, particularly HCV infections.
    Type: Application
    Filed: November 30, 2011
    Publication date: May 3, 2012
    Applicant: ACHILLION PHARMACEUTICALS, INC.
    Inventors: Suoming Zhang, Avinash Phadke, Cuixian Liu, Xiangzhu Wang, Jesse Quinn, Dawei Chen, Venkat Gadhachanda, Shouming Li, Milind Deshpande
  • Publication number: 20120108577
    Abstract: The present invention relates to compounds that demonstrate antibacterial activity, processes for their preparation, pharmaceutical compositions containing them as the active ingredient, to their use as medicaments and to their use in the manufacture of medicaments for use in the treatment of bacterial infections in warm-blooded animals such as humans. In particular this invention relates to compounds useful for the treatment of bacterial infections in warm-blooded animals such as humans, more particularly to the use of these compounds in the manufacture of medicaments for use in the treatment of bacterial infections in warm-blooded animals such as humans.
    Type: Application
    Filed: January 11, 2012
    Publication date: May 3, 2012
    Applicant: ASTRAZENECA AB
    Inventors: Gloria Breault, Charles Joseph Eyermann, Bolin Geng, Marshall Morningstar, Folkert Reck
  • Publication number: 20120094972
    Abstract: Substituted bicyclic heteroaryls and compositions containing them, for the treatment of general inflammation, arthritis, rheumatic diseases, osteoarthritis, inflammatory bowel disorders, inflammatory eye disorders, inflammatory or unstable bladder disorders, psoriasis, skin complaints with inflammatory components, chronic inflammatory conditions, including but not restricted to autoimmune diseases such as systemic lupus erythematosis (SLE), myestenia gravis, rheumatoid arthritis, acute disseminated encephalomyelitis, idiopathic thrombocytopenic purpura, multiples sclerosis, Sjoegren's syndrome and autoimmune hemolytic anemia, allergic conditions including all forms of hypersensitivity, The present invention also enables methods for treating cancers that are mediated, dependent on or associated with p110 activity, including but not restricted to leukemias, such as Acute Myeloid leukaemia (AML) Myelo-dysplastic syndrome (MDS) myelo-proliferative diseases (MPD) Chronic Myeloid Leukemia (CML) T-cell Acute Lymphob
    Type: Application
    Filed: June 25, 2010
    Publication date: April 19, 2012
    Applicant: AMGEN INC.
    Inventors: Matthew Brown, Yi Chen, Timothy David Cushing, Felix Gonzalez Lopez De Turiso, Xiao He, Todd J. Kohn, Julia Winslow Lohman, Vatee Pattaropong, Jennifer Seganish, Youngsook Shin, Jillian L. Simard
  • Publication number: 20120094984
    Abstract: A compound represented by the general formula: or a pharmaceutically acceptable salt thereof or a solvate thereof, wherein Ring A is a C6-14 aryl group or the like, L is —NReCO— or the like (wherein Re is a hydrogen atom or the like), Ring B is a C6-14 aryl group or the like, X is a C1-3 alkylene group or the like, Y is a single bond or the like, Z is a C1-3 alkylene group or the like, R1 and R2 are each independently a hydrogen atom or the like, and R3, R4, R5 and R6 are independently a hydrogen atom, a halogen atom or the like, has an A? production inhibitory effect or a BACE1 inhibitory effect and is useful as a prophylactic or therapeutic agent for a neurodegenerative disease caused by A? and typified by Alzheimer-type dementia.
    Type: Application
    Filed: December 21, 2011
    Publication date: April 19, 2012
    Applicant: EISAI R&D MANAGEMENT CO., LTD.
    Inventors: Yuichi Suzuki, Takafumi Motoki, Toshihiko Kaneko, Mamoru Takaishi, Tasuku Ishida, Kunitoshi Takeda, Yoichi Kita, Noboru Yamamoto, Afzal Khan, Paschalis Dimopoulos
  • Patent number: 8158620
    Abstract: A compound represented by the general formula: or a pharmaceutically acceptable salt thereof or a solvate thereof, wherein Ring A is a C6-14 aryl group or the like, L is —NReCO— or the like (wherein Re is a hydrogen atom or the like), Ring B is a C6-14 aryl group or the like, X is a C1-3 alkylene group or the like, Y is a single bond or the like, Z is a C1-3 alkylene group or the like, R1 and R2 are each independently a hydrogen atom or the like, and R3, R4, R5 and R6 are independently a hydrogen atom, a halogen atom or the like, has an A? production inhibitory effect or a BACE1 inhibitory effect and is useful as a prophylactic or therapeutic agent for a neurodegenerative disease caused by A? and typified by Alzheimer-type dementia.
    Type: Grant
    Filed: January 16, 2009
    Date of Patent: April 17, 2012
    Assignee: Eisai R&D Management Co., Ltd.
    Inventors: Yuichi Suzuki, Takafumi Motoki, Toshihiko Kaneko, Mamoru Takaishi, Tasuku Ishida, Kunitoshi Takeda, Yoichi Kita, Noboru Yamamoto, Afzal Khan, Paschalis Dimopoulos
  • Publication number: 20120065189
    Abstract: The present invention provides a novel heterocyclic compound. A heterocyclic compound represented by general formula (1) wherein, R1 and R2, each independently represent hydrogen; a phenyl lower alkyl group that may have a substituent(s) selected from the group consisting of a lower alkyl group and the like on a benzene ring and/or a lower alkyl group; or a cyclo C3-C8 alkyl lower alkyl group; or the like; R3 represents a lower alkynyl group or the like; R4 represents a phenyl group that may have a substituent(s) selected from the group consisting of a 1,3,4-oxadiazolyl group that may have e.g., halogen or a heterocyclic group selected from pyridyl group and the like; the heterocyclic group may have at least one substituent(s) selected from a lower alkoxy group and the like or a salt thereof.
    Type: Application
    Filed: May 27, 2010
    Publication date: March 15, 2012
    Inventors: Akira Takahashi, Masaki Suzuki, Yuichi Nakamura, Yohji Sakurai
  • Patent number: 8129369
    Abstract: The present invention discloses novel compounds of the Formula (1), comprising benzothiazinone, benzoxazinone or benzoxazolinone moieties having antifungal activity, method for preparing these compounds and the use of these compounds as antifungal agents in prevention and treatment of fungal infections, and pharmaceutical preparations containing these novel compounds.
    Type: Grant
    Filed: October 16, 2009
    Date of Patent: March 6, 2012
    Assignees: Council of Scientific & Industrial Research;, FDC Ltd.
    Inventors: Hanumant Bapurao Borate, Suleman Riyasaheb Maujan, Sangmeshwer Prabhakar Sawargave, Ramesh Ganesh Kelkar, Radhika Dilip Wakharkar, Mohan Anand Chandavarkar, Sharangi Ravinda Vaiude, Vinay Anant Joshi
  • Patent number: 8124602
    Abstract: The present invention relates to compounds of Formula V(A): that demonstrate antibacterial activity, processes for their preparation, pharmaceutical compositions containing them as the active ingredient, to their use as medicaments and to their use in the manufacture of medicaments for use in the treatment of bacterial infections in warm-blooded animals such as humans. In particular this invention relates to compounds of Formula V(A) useful for the treatment of bacterial infections in warm-blooded animals such as humans, more particularly to the use of these compounds in the manufacture of medicaments for use in the treatment of bacterial infections in warm-blooded animals such as humans.
    Type: Grant
    Filed: December 9, 2010
    Date of Patent: February 28, 2012
    Assignee: AstraZeneca AB
    Inventors: Gloria Breault, Charles Joseph Eyermann, Bolin Geng, Marshall Morningstar, Folkert Reck
  • Publication number: 20120040957
    Abstract: Compounds of formula (I) wherein X1, X3; X4 and X6, each independently of the others, represents a nitrogen atom or CR2, with the proviso that at least one of X1, X3; X4 and X6 represents a nitrogen atom; X2 represents C—H, C—(C1-C6alkyl), C—(C1-C6alkoxy), C-halogen, C—COOH; X5 represents C—H or C—(C1-C6alkyl), C-halogen; R1 and R2, independently of one another, represent hydrogen or a substituent selected from hydroxy, halogen, carboxy, amino, C1-C6alkylamino, di(C1-C6alkyl)amino, mercapto, cyano, nitro, C1-C6alkyl, C1-C6alkoxy, C1-C6alkylthio, C1-C6alkylamino-carbonyloxy, C2-C6alkenyl, C2-C6alkynyl, C1-C6alkylcarbonyloxy, C1-C6alkyl-sulfonyloxy, C1-C6heteroalkylcarbonyloxy, C5-C6heterocyclyl-carbonyloxy, C1-C6heteroalkyl, C1-C6heteroalkoxy, wherein heteroalkyl, heteroalkoxy groups or heterocyclyl comprise 1, 2 or 3 heteroatoms selected from nitrogen, oxygen and sulphur, in which substituents the alkyl moieties are unsubstituted or further substituted by halogeno, cyano, hydroxy, C1-C4alkoxy, C1-C4alkylcarbo
    Type: Application
    Filed: January 21, 2010
    Publication date: February 16, 2012
    Inventors: Berangere Gaucher, Franck Hubert Danel, Patrick Roussel
  • Patent number: 8114867
    Abstract: The invention relates to antibacterial compounds of formula I wherein R1 is hydrogen, halogen, hydroxy, alkoxy or cyano; Y1 and Y2 each represent CH, one or two of U, V, W and X represent(s) N and the remaining each represent CH or, in the case of X, may also represent CRa, Ra being halogen, and, in the case of W, may also represent CRb, or each of U, V, W, X, Y1 and Y2 represents CH, or each of U, V, W, X and Y1 represents CH and Y2 represents N, or also one or, provided R1 is hydrogen, two of U, V, W, X, Y1 and Y2 represent(s) CRC and the remaining each represent CH, Rb being alkoxy, alkoxycarbonyl or alkoxyalkoxy and Rc being, each time it occurs, independently represents hydroxy or alkoxy; A-B-D represents a chain of 4 to 6 atoms, which 4 to 6 atoms are selected from carbon, oxygen and nitrogen and may be substituted; E is one of the following groups: in which Z is CH or N and Q is O or S, or E is a phenyl group which is substituted once or twice in the meta and/or para position(s); and to salts
    Type: Grant
    Filed: April 10, 2008
    Date of Patent: February 14, 2012
    Assignee: Actelion Pharmaceuticals Ltd
    Inventors: Markus Gude, Christian Hubschwerlen, Georg Rueedi, Jean-Philippe Surivet, Cornelia Zumbrunn-Acklin
  • Publication number: 20120028969
    Abstract: The present invention provides compounds of formula (I); or pharmaceutically acceptable salts thereof, wherein the variables are defined as herein. The present invention provides a method for manufacturing the compounds of formula (I), their therapeutic uses, combinations with other of pharmacologically active agents, and a pharmaceutical compositions.
    Type: Application
    Filed: July 25, 2011
    Publication date: February 2, 2012
    Applicant: NOVARTIS AG
    Inventors: David Weninger BARNES, Gregory Raymond BEBERNITZ, Kevin CLAIRMONT, Scott Louis COHEN, Robert Edson DAMON, Robert Francis DAY, Stephanie Kay DODD, Christoph GAUL, Hatice Belgin GULGEZE EFTHYMIOU, Monish JAIN, Rajeshri Ganesh KARKI, Louise Clare KIRMAN, Kai LIN, Justin Yik Ching MAO, Tajesh Jayprakash PATEL, Brian Kenneth RAYMER, Liansheng SU
  • Publication number: 20120028920
    Abstract: A heterocyclic compound or a salt thereof represented by the formula (1): where R2 represents a hydrogen atom or a lower alkyl group; A represents a lower alkylene group or lower alkenylene group; and R1 represents an aromatic group or a heterocyclic group. The compound of the present invention has a wide treatment spectrum for mental disorders including central nervous system disorders, no side effects and high safety.
    Type: Application
    Filed: October 11, 2011
    Publication date: February 2, 2012
    Inventors: Hiroshi YAMASHITA, Hideaki Kuroda, Nobuaki Ito, Shin Miyamura, Kunio Oshima, Jun Matsubara, Haruka Takahashi, Tae Fukushima, Satoshi Shimizu, Kazumi Kondo, Yohji Sakurai, Takeshi Kuroda, Shinichi Taira, Motohiro Itotani, Tatsuyoshi Tanaka
  • Patent number: 8106043
    Abstract: The present invention features benzothiazines that inhibit nitric oxide synthase (NOS), particularly those that selectively inhibit neuronal nitric oxide synthase (nNOS) in preference to other NOS isoforms, and that have the formula: The NOS inhibitors of the invention, alone or in combination with other pharmaceutically active agents, can be used for treating or preventing various medical conditions.
    Type: Grant
    Filed: July 6, 2009
    Date of Patent: January 31, 2012
    Assignee: NeurAxon, Inc.
    Inventors: Jailall Ramnauth, Subhash C. Annedi, Sarah Silverman, Peter Dove, Shawn Maddaford, Suman Rakhit
  • Patent number: 8097614
    Abstract: The invention includes compositions for transmucosal administration to an animal comprising at least one active agent and a pharmaceutically acceptable carrier. A preferred active agent is selected from the group consisting of meloxicam, carprofen, enrofloxacin, clemastine, diphenhydramine, digoxin, levothyroxine, cyclosporine, ondansetron, lysine, zolpidem, propofol, nitenpyram, ivermectin, milbemycin, and pharmaceutically acceptable salts, solvates and esters thereof. In another embodiment, the invention includes methods of treating or preventing a condition in an animal comprising transmucosally administering a composition comprising a therapeutically or prophylactically effective amount of an active agent and a pharmaceutically acceptable carrier.
    Type: Grant
    Filed: February 17, 2006
    Date of Patent: January 17, 2012
    Assignees: Velcera Pharmaceuticals, Inc., NovaDel Pharma, Inc.
    Inventors: Mark C. Heit, Antonio M. Benitz, Dennis F. Steadman, David M. Petrick