Benzene Ring Bonded Directly To Ring Nitrogen Of The Five -membered Hetero Ring Patents (Class 548/563)
  • Publication number: 20150133442
    Abstract: The invention features compositions and methods for inhibiting the Pin1 protein, and the treatment of disorders characterized by elevated Pin1 levels.
    Type: Application
    Filed: June 7, 2013
    Publication date: May 14, 2015
    Inventors: Kun Ping Lu, Matthew Brian Boxer, Mindy Irene Emily Davis, Rajan Pragani, Min Shen, Anton Momtchilov Simeonov, Shuo Wei, Xiao Zhen Zhou
  • Patent number: 9023882
    Abstract: 5-membered heterocyclic derivatives represented by general formula (I) having xanthine oxidase inhibitory activities and useful as agents for the prevention or treatment of a disease associated with abnormality of serum uric acid level, prodrugs thereof, or salts thereof. In the formula (I), T represents nitro, cyano and the like; ring J represents aryl or heteroaryl; Q represents carboxy, 5-tetazolyl and the like; Y represents H, OH, NH2, halogen, haloalkyl and the like; X1 and X2 independently represent CR2 or N; R2 represents H, alkyl and the like; R1 represents halogen, cyano, haloalkyl, A-D-E-G-L-M, —N(-D-L-M)2 and the like, A represents a single bond, O, S and the like; D, G and M independently represent optionally substituted alkylene, cycloalkylene, heterocycloalkylene, arylene, heteroarylene and the like; E and L independently represent a single bond, O, S, COO, SO2 and the like.
    Type: Grant
    Filed: June 12, 2012
    Date of Patent: May 5, 2015
    Assignee: Kissei Pharmaceutical Co., Ltd.
    Inventors: Kazuo Shimizu, Yasushi Takigawa, Hideki Fujikura, Masato Iizuka, Masahiro Hiratochi, Norihiko Kikuchi
  • Patent number: 8921364
    Abstract: Disclosed are novel calcium release-activated calcium (CRAC) channel inhibitors, methods for preparing them, pharmaceutical compositions containing them, and methods of treatment using them. The present disclosure also relates to methods for treating non-small cell lung cancer (NSCLC) with CRAC inhibitors, and to methods for identifying therapeutics for treating and of diagnosing cancer.
    Type: Grant
    Filed: December 20, 2012
    Date of Patent: December 30, 2014
    Assignee: Rhizen Pharmaceuticals SA
    Inventors: Meyyappan Muthuppalaniappan, Srikant Viswanadha, Gayatri Swaroop Merikapudi, Swaroop Kumar V. S. Vakkalanka
  • Publication number: 20140128408
    Abstract: Histone deacetylases inhibitors (HDACIs) and compositions containing the same are disclosed. Methods of treating diseases and conditions wherein inhibition of HDAC provides a benefit, like a cancer, a neurodegenerative disorder, a peripheral neuropathy, a neurological disease, traumatic brain injury, stroke, hypertension, malaria, an autoimmune disease, autism, autism spectrum disorders, and inflammation, also are disclosed.
    Type: Application
    Filed: January 31, 2012
    Publication date: May 8, 2014
    Applicant: THE BOARD OF TRUSTEES OF THE UNIVERSITY OF ILLINOIS
    Inventors: Alan Kozikowski, Jay H. Kalin, Kyle V. Butier, Joel Bergman, Wayne W. Hancock
  • Patent number: 8609713
    Abstract: The invention relates to a series of substituted pyrrole derivatives, compositions comprising the same, and methods of treating conditions and disorders using such compounds and compositions.
    Type: Grant
    Filed: May 7, 2010
    Date of Patent: December 17, 2013
    Assignee: AbbVie Inc.
    Inventors: Ramin Faghih, Gregory A. Gfesser, Christopher L. Lynch, Murali Gopalakrishnan, Sujatha Gopalakrishnan, John Malysz, Earl J. Gubbins, Rachid El Kouhen, Jinhe Li
  • Patent number: 8603646
    Abstract: A pyrrole compound for an organic photoelectric device and an organic photoelectric device including the same, the pyrrole compound being represented by the following General Formula 1:
    Type: Grant
    Filed: March 2, 2011
    Date of Patent: December 10, 2013
    Assignee: Cheil Industries, Inc.
    Inventors: Sung-Hyun Jung, Hyung-Sun Kim, Ho-Jae Lee, Eun-Sun Yu, Mi-Young Chae, Ja-Hyun Kim
  • Publication number: 20130310377
    Abstract: Disclosed are novel calcium release-activated calcium (CRAC) channel inhibitors, methods for preparing them, pharmaceutical compositions containing them, and methods of treatment using them. The present disclosure also relates to methods for treating non-small cell lung cancer (NSCLC) with CRAC inhibitors, and to methods for identifying therapeutics for treating and of diagnosing cancer.
    Type: Application
    Filed: December 20, 2012
    Publication date: November 21, 2013
    Applicant: Rhizen Phamaceuticals SA
    Inventor: Rhizen Phamaceuticals SA
  • Publication number: 20130281453
    Abstract: Serine hydrolases are implicated in malconditions such as cancer, central nervous system disorders, cardiovascular disorders, obesity, and metabolic disorders. Many serine hydrolases expressed in proteomic libraries are of unknown function in vivo. Compounds identified through library versus library screening can be used for treatment of malconditions associated with the specific serine hydrolase KIAA1363 (also known as AADACL1). A library of inhibitors of KIAA1363 was prepared and candidate compounds were identified as a potent inhibitors having submicromolar IC50 values. An exemplary compound of the invention was shown to be an effective inhibitor of prostate cancer pathogenesis. Other inhibitory compounds of the invention comprising fluorophore groups are shown to be effective in spatial and temporal localization of the serine hydrolase in cells and tissues.
    Type: Application
    Filed: October 21, 2011
    Publication date: October 24, 2013
    Applicant: The Scripps Research Institute
    Inventors: Benjamin Cravatt, Daniel Nomura, Jae W. Chang, Raymond E. Moellering, Dan Bachovehin, Weiwei Li
  • Publication number: 20130224114
    Abstract: The present invention relates to compounds and methods for imaging translocator protein (18 kDa) (TSPO) expression in a subject. This invention also relates to compounds and methods for the treatment of neurodegenerative disorders, inflammation or anxiety in a subject.
    Type: Application
    Filed: March 25, 2013
    Publication date: August 29, 2013
    Applicant: The University of Sydney
    Inventor: The University of Sydney
  • Publication number: 20130116227
    Abstract: Disclosed is a novel biaryl amide derivative represented by formula (1) and having an affinity for the aldosterone receptor; also disclosed is a pharmaceutically acceptable salt thereof. (In the formula, A is any of the groups represented by formula (a); L is —CONH—, etc.; R1 is a substitutable aminosulfonyl group, etc.; R2 is a hydrogen atom, etc.; R3 is a hydrogen atom, etc.; R4 is a hydrogen atom, a halogen atom, hydroxy group, a substitutable amino group, a substitutable C1-6 alkoxy group, a substitutable 4- to 7-membered cyclic amino group, etc.; R5a, R5b and R5c are each independently hydrogen atoms, etc.; R6 is a halogen atom, a cyano group, etc.; R7 and R8 are each independently a hydrogen atom, etc.; and m is an integer such as 0.
    Type: Application
    Filed: July 12, 2011
    Publication date: May 9, 2013
    Applicant: DAINIPPON SUMITOMO PHARMA CO., LTD.
    Inventors: Seiji Katayama, Seiji Hori, Futoshi Hasegawa, Kuniko Suzuki
  • Patent number: 8324125
    Abstract: This invention relates to the use of nano-organocatalysts, and, more specifically, to the use of magnetic nanomaterial-supported organocatalysts. It is an object of the present invention to provide “green” catalysts and protocols. According to one embodiment of the invention, a nano-organocatalyst in the form of a magnetic nanomaterial-supported organocatalyst is provided. According to other embodiments of the invention, glutathione and cysteine are provided as organocatalysts and magnetic nanomaterial-supported glutathione and magnetic nanomaterial-supported cysteine are provided for use as nano-organocatalysts. According to another embodiment of the invention, a method of using a recyclable magnetic nanomaterial-supported organocatalyst using a totally benign aqueous protocol, without using any organic solvent in the reaction or during the workup, is provided.
    Type: Grant
    Filed: September 3, 2009
    Date of Patent: December 4, 2012
    Assignee: The United States of America as represented by the Administrator of the U.S. Environmental Protection Agency
    Inventors: Rajender S. Varma, Vivek Polshettiwar
  • Publication number: 20120220593
    Abstract: A pharmaceutical composition comprising a compound having Formula (I) or a pharmacologically acceptable salt thereof as an active ingredient: [wherein, R1 is, for example, a C6-C10 aryl group which may be substituted with one group or more than one group selected from substituent group ?; R2 is, for example, a C6-C10 aryl group which may be substituted with one group or more than one group selected from substituent group ?; and X is, for example, a hydroxyl group or a C1-C6 alkoxy group].
    Type: Application
    Filed: February 24, 2012
    Publication date: August 30, 2012
    Applicant: Daiichi Sankyo Company, Limited
    Inventors: Kazumasa Aoki, Koji Suda, Toshio Kaneko, Tomio Kimura
  • Patent number: 8252833
    Abstract: A compound of formula (I) or a pharmaceutically acceptable derivative thereof, wherein, R1 R2 R3, R4, R5, R6, X and Y are as defined in the specification; a process for preparing such compounds; a pharmaceutical composition comprising such compounds; and the use of such compounds in medicine.
    Type: Grant
    Filed: February 1, 2007
    Date of Patent: August 28, 2012
    Assignee: Glaxo Group Limited
    Inventors: Andrew Billinton, Nicholas Maughan Clayton, Gerard Martin Paul Giblin, Mark Patrick Healy
  • Publication number: 20120214785
    Abstract: The invention relates to new compounds of the formula I to their use as medicaments, to methods for their therapeutic use and to pharmaceutical compositions containing them.
    Type: Application
    Filed: August 17, 2011
    Publication date: August 23, 2012
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: Gerald Juergen ROTH, Martin FLECK, Niklas HEINE, Joerg KLEY, Thorsten LEHMANN-LINTZ, Heike NEUBAUER, Bernd NOSSE
  • Publication number: 20120196915
    Abstract: The present invention relates to a new series of 1,2-diphenylpyrroles of formula (I) or their pharmaceutically acceptable salts, or their pharmaceutically acceptable solvates, having antitumor activity, wherein R1 and R2 are individually selected from the group consisting of halogen, optionally substituted O(C1-C4)alkyl and optionally substituted (C1-C4)alkyl; and R3 is selected from the group consisting of H, (C1-C4)alkyl, CONH2 and (C?NH)NH2. It also relates to a process for preparing them, to pharmaceutical compositions containing them, and to their use for the treatment of cancer, in particular lung carcinoma, colorectal carcinoma, breast carcinoma and/or prostate carcinoma.
    Type: Application
    Filed: July 28, 2010
    Publication date: August 2, 2012
    Applicant: ARGON PHARMA, S.L.
    Inventors: Ramon Mangues Bafalluy, Isolda Casanova Rigalt, Fernando Albericio Palomera, Mercedes Álvarez, Svetlana Savina
  • Patent number: 8217073
    Abstract: Novel pyrrole derivatives are disclosed as A?42-lowering agents for the treatment and prevention of neurodegenerative disorders characterized by the formation or accumulation of amyloid plaques comprising the A?42 peptide.
    Type: Grant
    Filed: May 6, 2010
    Date of Patent: July 10, 2012
    Assignee: Myrexis, Inc.
    Inventors: Warren S. Weiner, Rachel M. Slade, Yevgeniya I. Klimova, Ruth J. Walton, Mark B. Anderson
  • Publication number: 20120157462
    Abstract: Compounds having the formula wherein the symbols have the meaning described in the specification are hydroxamic acid derivatives of aniline and capable of inhibiting the lethal effects of infection by anthrax bacteria and are useful in the treatment of poisoning by anthrax.
    Type: Application
    Filed: January 30, 2008
    Publication date: June 21, 2012
    Inventors: Alan T. Johnson, Guan-Sheng Jiao
  • Publication number: 20120149910
    Abstract: The object of the present invention is to provide novel carboxamides which exhibit an excellent pesticidal activity as pesticides. Disclosed are the carboxamides represented by the following Formula (I): wherein each substituent is as defined in the specification, and use thereof as pesticides and animal parasite controlling agents.
    Type: Application
    Filed: August 3, 2010
    Publication date: June 14, 2012
    Applicant: Bayer CropScience AG
    Inventors: Jun Mihara, Koichi Araki, Takuma Mori, Tetsuya Murata, Yasushi Yoneta, Yukiyoshi Watanabe, Eiichi Shimojo, Teruyuki Ichihara, Masashi Ataka, Katsuhiko Shibuya, Ulrich Gorgens
  • Patent number: 8188144
    Abstract: The invention is directed to compounds of Formula (I) or salts thereof. The invention is also directed to use of the compounds of formula (I) in the in vitro preservation of living animal cells. The living cells can be isolated cells, such as stem cells, or groups of cells such as tissue or an organ.
    Type: Grant
    Filed: April 9, 2010
    Date of Patent: May 29, 2012
    Assignee: Antoxis Limited
    Inventors: Donald Barton McPhail, Graeme James Cook, Andrew Scott Johnstone
  • Publication number: 20110313158
    Abstract: The invention describes the development of highly efficient, recyclable two component system, CuAl-hydrotalcite/rac 1,1?-Binaphthalene-2,2?-diol catalytic system for the N-alkylation of electron deficient aryl chlorides in presence of potassium carbonate as a base at room temperature in 3-6 h, wherein the process is provided for the preparation of various secondary amines via C—N coupling reaction of aliphatic amines(aliphatic open chain, acyclic, benzyl amines and heterocyclic amines) with various aryl chlorides.
    Type: Application
    Filed: February 26, 2010
    Publication date: December 22, 2011
    Inventors: Pravin R. Likhar, R. Arundhati, M. Lakshmi Kantam
  • Publication number: 20110294818
    Abstract: The present invention relates to 1H-Quinazoline-2,4-diones of formula (I) wherein R1 and R2 are as defined in the specification, their preparation, their use as pharmaceuticals, and pharmaceutical compositions containing them. Further, intermediates for the manufacture of compounds of formula (I) are and combinations comprising compounds of formula (I) are disclosed.
    Type: Application
    Filed: July 28, 2011
    Publication date: December 1, 2011
    Inventors: Hans Allgeier, Yves Auberson, David Carcache, Philipp Floersheim, Christel Guibourdenche, Wolfgang Froestl, Jörg Kallen, Manuel Koller, Henri Mattes, Joachim Nozulak, David Orain, Johanne Renaud
  • Publication number: 20110275669
    Abstract: The present invention relates to compounds of the general formula (I) their derivatives, their analogs, their tautomeric forms, their pharmaceutically acceptable salts, wherein all variables are as defined in the specification.
    Type: Application
    Filed: April 25, 2011
    Publication date: November 10, 2011
    Applicant: Cadilla Healthcare Limited
    Inventors: Braj Bhushan Lohray, Vidya Bhushan Lohray, Vijay Kumar Barot, Saurin Khimshankar Raval, Preeti Saurin Raval, Sujay Basu
  • Publication number: 20110266527
    Abstract: A pyrrole compound for an organic photoelectric device and an organic photoelectric device including the same, the pyrrole compound being represented by the following General Formula 1:
    Type: Application
    Filed: March 2, 2011
    Publication date: November 3, 2011
    Inventors: Sung-Hyun Jung, Hyung-Sun Kim, Ho-Jae Lee, Eun-Sun Yu, Mi-Young Chae, Young-Hoon Kim, Ja-Hyun Kim
  • Publication number: 20110166349
    Abstract: Methods are provided for the catalytic hydroamination of compounds having an alkyne or allene functional group, in which the compound is contacted with ammonia or an amine in the presence of a catalytic amount of a gold complex under conditions sufficient for hydroamination to occur.
    Type: Application
    Filed: May 8, 2009
    Publication date: July 7, 2011
    Applicant: The Regents of the University of California
    Inventors: Guy Bertrand, Vincent Lavallo, Guido D. Frey, Bruno Donnadieu, Michele Soleil-Havoup
  • Publication number: 20110105554
    Abstract: The present invention provides a method of designing a modulator of a myosin, the method comprising molecular modeling of a compound such that the modeled compound interacts with at least three amino acid residues of said myosin, said residues being selected from (a) ranges K265-V268, V411-L441, N588-Q593, D614-T629, and V630-E646 of SEQ ID NO: 2, said myosin comprising or consisting of (i) the sequence of SEQ ID NO: 2; (ii) the sequence encoded by the sequence of SEQ ID NO: 1; (iii) a sequence being at least 40% identical to the sequence of SEQ ID NO: 2 or to the sequence encoded by the sequence of SEQ ID NO: 1; or (iv) a sequence encoded by a sequence being at least 40% identical to the sequence of SEQ ID NO: 1; wherein said sequence of (iii) or (iv) comprises said three amino acid residues, and wherein said residues comprise K265; or (b) ranges of any one of SEQ ID NOs: 4, 6, 8, 10, 12, 14, 16, 18, 20, 22, 24, 26, 28, 30, 32, 34, 36, 38, 40, 42, 44, 46, 48, 50, 52, 54, 56, 58, 60, 62, 64, 66, 68, 70, 72, 7
    Type: Application
    Filed: November 21, 2008
    Publication date: May 5, 2011
    Applicant: KINARIS BIOMEDICALS GMBH
    Inventors: Dietmar Manstein, Roman Fedorov, Georgios Tsiavaliaris, Hans-Joachim Knölker, René Martin, Juliane Kirst, Herwig Gutzeit, Markus Böhl
  • Publication number: 20110098309
    Abstract: Disclosed are methods of inhibiting, regulating, and/or modulating the formation of soluble, globular, non-fibrillar, neurotoxic amyloid ?1-42 oligomers from amyloid ?1-42 monomers using acylhydrazide compounds. Also disclosed are methods of treating a patient suffering from diseases associated with the formation of soluble, globular, non-fibrillar, neurotoxic amyloid ?1-42 oligomers using acylhydrazide compounds.
    Type: Application
    Filed: July 11, 2008
    Publication date: April 28, 2011
    Applicant: ACUMEN PHARMACEUTICALS, INC.
    Inventors: Gary Charles Look, Lauri Schultz, Alexandre Mikhaylovich Polozov, Nikhil Bhagat, Jian Wang, David E. Zembower, William F. Goure, Todd Pray, Grant A. Krafft
  • Patent number: 7932403
    Abstract: The present invention relates to a process for preparing pyrrole derivatives of a class that is effective at inhibiting the biosynthesis of cholesterol in humans, and more particularly to improved synthetic methods for preparing 3,5-dihydroxy-7-pyrrol-1-yl heptanoic acids from 1,4-diketo starting materials. The invention further relates to intermediates in this process formula (I).
    Type: Grant
    Filed: December 16, 2005
    Date of Patent: April 26, 2011
    Assignee: ratiopharm GmbH
    Inventors: Pavel Bobal, Jaroslav Frantisek, Jiri Stohandl, Kane Denike, Armin Boerner, Vitali Tararov, Andrei Korostylev, Gerd Koenig, Nicolas Jeker
  • Publication number: 20110054180
    Abstract: This invention relates to the use of nano-organocatalysts, and, more specifically, to the use of magnetic nanomaterial-supported organocatalysts. It is an object of the present invention to provide “green” catalysts and protocols. According to one embodiment of the invention, a nano-organocatalyst in the form of a magnetic nanomaterial-supported organocatalyst is provided. According to other embodiments of the invention, glutathione and cysteine are provided as organocatalysts and magnetic nanomaterial-supported glutathione and magnetic nanomaterial-supported cysteine are provided for use as nano-organocatalysts. According to another embodiment of the invention, a method of using a recyclable magnetic nanomaterial-supported organocatalyst using a totally benign aqueous protocol, without using any organic solvent in the reaction or during the workup, is provided.
    Type: Application
    Filed: September 3, 2009
    Publication date: March 3, 2011
    Applicant: USA as Represented by the Administrator of U.S. Environmental Protection Agency
    Inventors: Rajender S. Varma, Vivek Polshettiwar
  • Publication number: 20110053974
    Abstract: To find a therapeutic agent and/or a preventive agent for diabetes mellitus or the like having excellent activity and safety. A compound represented by the following general formula (I), or a pharmacologically acceptable salt thereof. In the formula, X represents ?C(R5)- or ?N—; Y represents —O— or —NH—; L represents a bond or a substitutable C1-C3 alkylene group; M represents a substitutable C3-C10 cycloalkyl group, a substitutable C6-C10 aryl group, or a substitutable heterocyclic group; R1 represents a C1-C6 alkyl group, a C3-C10 cycloalkyl group, a C1-C6 haloalkyl group, a C2-C6 alkenyl group, a C2-C6 alkynyl group, a C1-C6 aliphatic acyl group, a C1-C6 alkoxy C1-C6 alkyl group, or a C6-C10 aryl group; and R2, R3, R4, and R5 may be the same or different and each represent a hydrogen atom, a halogen atom, a C1-C3 alkyl group, a C1-C3 haloalkyl group, a C1-C3 alkoxy group, or a nitro group.
    Type: Application
    Filed: September 29, 2010
    Publication date: March 3, 2011
    Applicant: DAIICHI SANKYO COMPANY, LIMITED
    Inventors: Narihiro TODA, Masao YOSHIDA, Rieko TAKANO, Masahiro INOUE, Takeshi HONDA, Koji MATSUMOTO, Ryutaro NAKASHIMA
  • Publication number: 20110044898
    Abstract: The present invention relates to compounds and methods for imaging translocator protein (18 kDa) (TSPO) expression in a subject. This invention also relates to compounds and methods for the treatment of neurodegenerative disorders, inflammation or anxiety in a subject.
    Type: Application
    Filed: December 2, 2008
    Publication date: February 24, 2011
    Applicant: University of Sydney
    Inventors: Michael Kassiou, Michelle Louise James, Christopher Andrew Luus
  • Publication number: 20110021528
    Abstract: The present invention is directed to certain hydroxamate derivatives that are useful in the treatment of hepatitis C. These compounds are also inhibitors of histone deacetylase and are therefore useful in the treatment of diseases associated with histone deacetylase activity. Pharmaceutical compositions and processes for preparing these compounds are also disclosed.
    Type: Application
    Filed: October 1, 2010
    Publication date: January 27, 2011
    Applicant: PHARMACYCLICS, INC.
    Inventors: Erik J. Verner, Martin Sendzik, Chitra Baskaran, Joseph J. Buggy, James Robinson
  • Publication number: 20100286109
    Abstract: The invention relates to novel amide derivatives that are positive allosteric modulators of neuronal nicotinic receptors, compositions comprising the same, processes for preparing such compounds, and methods for using such compounds and compositions.
    Type: Application
    Filed: July 22, 2010
    Publication date: November 11, 2010
    Applicant: ABBOTT LABORATORIES
    Inventors: Michael R. Schrimpf, Kathleen H. Mortell, Diana L. Nersesian, Chih-Hung Lee, Bruce Clapham
  • Publication number: 20100216862
    Abstract: Novel pyrrole derivatives are disclosed as A?42-lowering agents for the treatment and prevention of neurodegenerative disorders characterized by the formation or accumulation of amyloid plaques comprising the A?42 peptide.
    Type: Application
    Filed: May 6, 2010
    Publication date: August 26, 2010
    Applicant: Myriad Pharmaceuticals, Inc.
    Inventors: Warren S. Weiner, Rachel M. Slade, Yevgeniya I. Klimova, Ruth J. Walton, Mark B. Anderson
  • Patent number: 7745481
    Abstract: Certain cyclooxygenase-2 inhibitors are useful for the treatment and prevention of tumors and tumor-related disorders and cachexia.
    Type: Grant
    Filed: August 13, 2004
    Date of Patent: June 29, 2010
    Assignee: Daiichi Sankyo Company, Limited
    Inventors: Shinichi Kurakata, Masaharu Hanai, Saori Kanai, Tomio Kimura
  • Publication number: 20100160327
    Abstract: The present invention relates to a novel class of modified malonate derivatives. The modified malonate compounds can be used to treat cancer. The modified malonate compounds can also inhibit histone deacetylase and are suitable for use in selectively inducing terminal differentiation, and arresting cell growth and/or apoptosis of neoplastic cells, thereby inhibiting proliferation of such cells. Thus, the compounds of the present invention are useful in treating a patient having a tumor characterized by proliferation of neoplastic cells. The compounds of the invention may also be useful in the prevention and treatment of TRX-mediated diseases, such as autoimmune, allergic and inflammatory diseases, and in the prevention and/or treatment of diseases of the central nervous system (CNS), such as neurodegenerative diseases.
    Type: Application
    Filed: June 21, 2006
    Publication date: June 24, 2010
    Inventors: Jonathan Grimm, Paul Harrington, Richard Heidebrecht, JR., Thomas Miller, Karin Otte, Phieng Siliphaivanh, David Sloman, Matthew Stanton, Kevin Wilson, David Witter, Solomon Kattar, Paul Tempest
  • Patent number: 7714022
    Abstract: Novel pyrrole derivatives are disclosed as A?42-lowering agents for the treatment and prevention of neurodegenerative disorders characterized by the formation or accumulation of amyloid plaques comprising the A?42 peptide.
    Type: Grant
    Filed: March 27, 2008
    Date of Patent: May 11, 2010
    Assignee: Myriad Pharmaceuticals, Inc.
    Inventors: Warren S. Weiner, Rachel M. Slade, Yevgeniya I. Klimova, Ruth J. Walton, Mark B. Anderson
  • Patent number: 7628938
    Abstract: The present invention provides a photochromic compound that is colored when irradiated with visible light and quickly faded when set in a dark place. The photochromic compound according to the present invention is expressed by the following general formula (I): where each of A1, A2 and A3 is a five-member rings forming a 6?-electron system, the three rings being identical, partially identical or totally different from each other, and each ring may have a substituent; B1 and B2 are functional groups, each having an atomic number of five or larger, including a ring compound, and bonded to the 2-carbon of each of A2 and A3, respectively; and R1, R2 and R3 are substituents identical to or different from each other. This compound is highly colorable and durable even when it is dispersed into plastic macromolecular materials. Therefore, it is suitable as a dye material for sunglasses or similar products.
    Type: Grant
    Filed: March 21, 2007
    Date of Patent: December 8, 2009
    Assignee: National University Corporation Nara Institute of Science and Technology
    Inventors: Tsuyoshi Kawai, Takuya Nakajima, Shigekazu Kawai
  • Patent number: 7618995
    Abstract: The invention relates to compounds having formula (I): Wherein X, R1, R2, R3, R4 and R5 are as defined herein. The invention also relates to the preparation method thereof and the use of same in therapeutics.
    Type: Grant
    Filed: December 7, 2007
    Date of Patent: November 17, 2009
    Assignee: Sanofi-Aventis
    Inventors: Francis Barth, Christian Congy, Laurent Hortala, Murielle Rinaldi-Carmona
  • Publication number: 20090281094
    Abstract: The present invention concerns pyrrole compounds, derivatives of 1-{[1,5-bis(4-chlorophenyl)-2-methyl-1H-pyrrol-3-yl]methyl}-4-methylpiperazine (BM212). The invention concerns the use of the described compounds as antitubercular agents having high activity and low toxicity and process to obtain intermediates and final compounds.
    Type: Application
    Filed: March 3, 2006
    Publication date: November 12, 2009
    Inventors: Mariangela Biava, Fabrizio Manetti, Delia Deidda, Raffaello Pompei, Maurizio Botta, Giulio Cesare Porretta
  • Patent number: 7615647
    Abstract: A process is provided for preparing pharmaceutical grade atorvastatin hemicalcium salt comprising: (a) deesterifying, wherein R is an ester protecting group to (b) extracting R(R*,R*)-3 into an organic solvent or mixture of solvents, (c) adding a base of formula NR1R2R3 wherein R1, R2 and R3 are independently selected from H, substituted or non-substituted C1 to C7 alkyl, C6 to C9 aryl, C8 to C10 aralkyl or aminoalkyl to form atorvastatin base salt, (d) isolating by precipitation of the above atorvastatin base salt and purifying when necessary, (e) converting atorvastatin base salt to atorvastatin hemicalcium salt by treatment with a calcium salt solution, and (f) isolating the atorvastatin hemicalcium salt.
    Type: Grant
    Filed: August 5, 2005
    Date of Patent: November 10, 2009
    Assignee: Apotex Pharmachem Inc.
    Inventors: K.S. Keshava Murthy, Yajun Zhao, Daqing Che, Bhaskar Reddy Guntoori, Sammy Chris Duncan, Stephen E. Horne
  • Publication number: 20090163715
    Abstract: A compound represented by the general formula below or a salt thereof is a useful intermediate in the production of a [2-(3,3,5,5-tetramethylcyclohexyl)phenyl]piperazine compound that has excellent cell adhesion inhibitory effect and cell invasion inhibitory effect and therefore is useful as a therapeutic or prophylactic agent for various inflammatory diseases and autoimmune diseases induced by the adhesion and invasion of leukocytes, such as inflammatory bowel diseases (particularly ulcerative colitis or Crohn's disease), irritable bowel syndrome, rheumatoid arthritis, psoriasis, multiple sclerosis, asthma and atopic dermatitis. wherein R1 and R2 independently represent hydrogen or a protecting group for an amino group, or R1 and R2 bond together to form an optionally substituted pyrrole ring.
    Type: Application
    Filed: May 25, 2006
    Publication date: June 25, 2009
    Applicant: EISAI R&D MANAGEMENT CO., LTD.
    Inventors: Mitsuo Nagai, Kazumasa Nara, Kazunori Wakasugi, Toshihiko Naito
  • Patent number: 7524971
    Abstract: The invention relates to compounds having formula (I): Wherein X, R1, R2, R3, R4, R5 and R6 are as defined herein. The invention also relates to a method of preparing said compounds and to die application thereof in therapeutics.
    Type: Grant
    Filed: August 2, 2007
    Date of Patent: April 28, 2009
    Assignee: Sanofi - Aventis
    Inventors: Francis Barth, Christian Congy, Laurent Hortala, Murielle Rinaldi-Carmona
  • Publication number: 20090005410
    Abstract: Compounds are provided that act as potent antagonists of the CCR9 receptor. Animal testing demonstrates that these compounds are useful for treating inflammation, a hallmark disease for CCR9. The compounds are generally aryl sulfonamide derivatives and are useful in pharmaceutical compositions, methods for the treatment of CCR9-mediated diseases, and as controls in assays for the identification of CCR9 antagonists.
    Type: Application
    Filed: June 17, 2008
    Publication date: January 1, 2009
    Applicant: CHEMOCENTRYX, INC.
    Inventors: Trevor T. Charvat, Cheng Hu, Anita Melikian, Aaron Novack, Andrew M.K. Pennell, Edward J. Sullivan, William D. Thomas, Solomon Ungashe, Penglie Zhang, Jay Powers, Sreenivas Punna
  • Publication number: 20080275053
    Abstract: Compounds of formula (I) or a pharmaceutically acceptable derivative thereof: wherein A, B, D, Z, R1, R2a, R2b, and Rx are as defined in the specification, a process for the preparation of such compounds, pharmaceutical compositions comprising such compounds and the use of such compounds in medicine.
    Type: Application
    Filed: October 6, 2004
    Publication date: November 6, 2008
    Inventors: Gerard Martin Paul Giblin, Adrian Hall, Ian Reginald Kilford, Xiao Qing Lewell, Neil Derek Miller, Alan Naylor
  • Publication number: 20080261952
    Abstract: A method of treating a condition associated with the CB-1 receptor, in particular obesity, by administering an effective amount of an aryl urea CB-1 receptor modulating compound to a subject in need of such treatment.
    Type: Application
    Filed: August 16, 2005
    Publication date: October 23, 2008
    Inventors: Jason Bloxham, Matthew Colin Thor Fyfe, James Horswill, Revathy Perpetua Jeevaratnam, John Keily, Martin James Procter, Karen Lesley Schofield, Salam Shaaban, Andrew Simon Swain, Phillppe Wong-Kai-In
  • Patent number: 7323490
    Abstract: The invention provides pyrrole-containing compounds and methods of use thereof. Kits and pharmaceutical compositions comprising the pyrrole compounds of the invention are also provided. The compounds and compositions disclosed herein are preferably used in the treatment of neurodegenerative diseases, cardiovascular diseases, proliferative diseases, and visual disorders. In particular, methods and compositions for the treatment of stroke are disclosed herein.
    Type: Grant
    Filed: May 17, 2004
    Date of Patent: January 29, 2008
    Assignee: Ambit Biosciences Corporation
    Inventors: David J. Lockhart, Hitesh K. Patel, Zdravko V. Milanov, Shamal Anil Mehta, Patrick Parvis Zarrinkar, William H. Biggs, III, Pietro Ciceri, Miles A. Fabian, Daniel K. Treiber
  • Publication number: 20080006797
    Abstract: The present invention provides a photochromic compound that is colored when irradiated with visible light and quickly faded when set in a dark place. The photochromic compound according to the present invention is expressed by the following general formula (I): where each of A1, A2 and A3 is a five-member rings forming a 6?-electron system, the three rings being identical, partially identical or totally different from each other, and each ring may have a substituent; B1 and B2 are functional groups, each having an atomic number of five or larger, including a ring compound, and bonded to the 2-carbon of each of A2 and A3, respectively; and R1, R2 and R3 are substituents identical to or different from each other. This compound is highly colorable and durable even when it is dispersed into plastic macromolecular materials. Therefore, it is suitable as a dye material for sunglasses or similar products.
    Type: Application
    Filed: March 21, 2007
    Publication date: January 10, 2008
    Applicant: NATIONAL UNIVERSITY CORPORATION NARA INSTITUTE OF SCIENCE AND TECHNOLOGY
    Inventors: Tsuyoshi Kawai, Takuya Nakajima, Shigekazu Kawai
  • Patent number: 7314885
    Abstract: The present invention relates to compounds useful of inhibitors of protein kinases. The invention also provides pharmaceutically acceptable compositions comprising said compounds, processes for making the compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders.
    Type: Grant
    Filed: March 22, 2006
    Date of Patent: January 1, 2008
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: Alex Aronov, Upul K. Bandarage, David J. Lauffer, Pan Li, Ronald C. Tomlinson
  • Patent number: 7241803
    Abstract: A group of compounds that inhibit HIV replication by blocking HIV entry was identified. Two representative compounds, designated NB-2 and NB-64, inhibited HIV replication (p24 production) with IC50 values <0.5 ?g/ml.
    Type: Grant
    Filed: November 12, 2003
    Date of Patent: July 10, 2007
    Assignee: New York Blood Center
    Inventors: Shibo Jiang, Asim Kumar Debnath
  • Patent number: 7186749
    Abstract: The present invention relates to pyrrolo-naphthyl compounds of the formula and methods of using them to modulate PAI-1 expression and to treat PAI-1 related disorders.
    Type: Grant
    Filed: August 22, 2005
    Date of Patent: March 6, 2007
    Assignee: Wyeth
    Inventors: Thomas J. Commons, Douglas John Jenkins