Benzene Ring Bonded Directly To Ring Nitrogen Of The Five -membered Hetero Ring Patents (Class 548/563)
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Publication number: 20150133442Abstract: The invention features compositions and methods for inhibiting the Pin1 protein, and the treatment of disorders characterized by elevated Pin1 levels.Type: ApplicationFiled: June 7, 2013Publication date: May 14, 2015Inventors: Kun Ping Lu, Matthew Brian Boxer, Mindy Irene Emily Davis, Rajan Pragani, Min Shen, Anton Momtchilov Simeonov, Shuo Wei, Xiao Zhen Zhou
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Patent number: 9023882Abstract: 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: GrantFiled: June 12, 2012Date of Patent: May 5, 2015Assignee: Kissei Pharmaceutical Co., Ltd.Inventors: Kazuo Shimizu, Yasushi Takigawa, Hideki Fujikura, Masato Iizuka, Masahiro Hiratochi, Norihiko Kikuchi
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Patent number: 8921364Abstract: 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: GrantFiled: December 20, 2012Date of Patent: December 30, 2014Assignee: Rhizen Pharmaceuticals SAInventors: Meyyappan Muthuppalaniappan, Srikant Viswanadha, Gayatri Swaroop Merikapudi, Swaroop Kumar V. S. Vakkalanka
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Publication number: 20140128408Abstract: 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: ApplicationFiled: January 31, 2012Publication date: May 8, 2014Applicant: THE BOARD OF TRUSTEES OF THE UNIVERSITY OF ILLINOISInventors: Alan Kozikowski, Jay H. Kalin, Kyle V. Butier, Joel Bergman, Wayne W. Hancock
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Patent number: 8609713Abstract: 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: GrantFiled: May 7, 2010Date of Patent: December 17, 2013Assignee: 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
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Patent number: 8603646Abstract: 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: GrantFiled: March 2, 2011Date of Patent: December 10, 2013Assignee: Cheil Industries, Inc.Inventors: Sung-Hyun Jung, Hyung-Sun Kim, Ho-Jae Lee, Eun-Sun Yu, Mi-Young Chae, Ja-Hyun Kim
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Publication number: 20130310377Abstract: 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: ApplicationFiled: December 20, 2012Publication date: November 21, 2013Applicant: Rhizen Phamaceuticals SAInventor: Rhizen Phamaceuticals SA
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Publication number: 20130281453Abstract: 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: ApplicationFiled: October 21, 2011Publication date: October 24, 2013Applicant: The Scripps Research InstituteInventors: Benjamin Cravatt, Daniel Nomura, Jae W. Chang, Raymond E. Moellering, Dan Bachovehin, Weiwei Li
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Publication number: 20130224114Abstract: 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: ApplicationFiled: March 25, 2013Publication date: August 29, 2013Applicant: The University of SydneyInventor: The University of Sydney
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Publication number: 20130116227Abstract: 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: ApplicationFiled: July 12, 2011Publication date: May 9, 2013Applicant: DAINIPPON SUMITOMO PHARMA CO., LTD.Inventors: Seiji Katayama, Seiji Hori, Futoshi Hasegawa, Kuniko Suzuki
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Patent number: 8324125Abstract: 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: GrantFiled: September 3, 2009Date of Patent: December 4, 2012Assignee: The United States of America as represented by the Administrator of the U.S. Environmental Protection AgencyInventors: Rajender S. Varma, Vivek Polshettiwar
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Publication number: 20120220593Abstract: 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: ApplicationFiled: February 24, 2012Publication date: August 30, 2012Applicant: Daiichi Sankyo Company, LimitedInventors: Kazumasa Aoki, Koji Suda, Toshio Kaneko, Tomio Kimura
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Patent number: 8252833Abstract: 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: GrantFiled: February 1, 2007Date of Patent: August 28, 2012Assignee: Glaxo Group LimitedInventors: Andrew Billinton, Nicholas Maughan Clayton, Gerard Martin Paul Giblin, Mark Patrick Healy
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Publication number: 20120214785Abstract: 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: ApplicationFiled: August 17, 2011Publication date: August 23, 2012Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Gerald Juergen ROTH, Martin FLECK, Niklas HEINE, Joerg KLEY, Thorsten LEHMANN-LINTZ, Heike NEUBAUER, Bernd NOSSE
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Publication number: 20120196915Abstract: 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: ApplicationFiled: July 28, 2010Publication date: August 2, 2012Applicant: ARGON PHARMA, S.L.Inventors: Ramon Mangues Bafalluy, Isolda Casanova Rigalt, Fernando Albericio Palomera, Mercedes Álvarez, Svetlana Savina
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Patent number: 8217073Abstract: 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: GrantFiled: May 6, 2010Date of Patent: July 10, 2012Assignee: Myrexis, Inc.Inventors: Warren S. Weiner, Rachel M. Slade, Yevgeniya I. Klimova, Ruth J. Walton, Mark B. Anderson
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Publication number: 20120157462Abstract: 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: ApplicationFiled: January 30, 2008Publication date: June 21, 2012Inventors: Alan T. Johnson, Guan-Sheng Jiao
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Publication number: 20120149910Abstract: 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: ApplicationFiled: August 3, 2010Publication date: June 14, 2012Applicant: Bayer CropScience AGInventors: Jun Mihara, Koichi Araki, Takuma Mori, Tetsuya Murata, Yasushi Yoneta, Yukiyoshi Watanabe, Eiichi Shimojo, Teruyuki Ichihara, Masashi Ataka, Katsuhiko Shibuya, Ulrich Gorgens
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Patent number: 8188144Abstract: 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: GrantFiled: April 9, 2010Date of Patent: May 29, 2012Assignee: Antoxis LimitedInventors: Donald Barton McPhail, Graeme James Cook, Andrew Scott Johnstone
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Publication number: 20110313158Abstract: 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: ApplicationFiled: February 26, 2010Publication date: December 22, 2011Inventors: Pravin R. Likhar, R. Arundhati, M. Lakshmi Kantam
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Publication number: 20110294818Abstract: 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: ApplicationFiled: July 28, 2011Publication date: December 1, 2011Inventors: Hans Allgeier, Yves Auberson, David Carcache, Philipp Floersheim, Christel Guibourdenche, Wolfgang Froestl, Jörg Kallen, Manuel Koller, Henri Mattes, Joachim Nozulak, David Orain, Johanne Renaud
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Publication number: 20110275669Abstract: 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: ApplicationFiled: April 25, 2011Publication date: November 10, 2011Applicant: Cadilla Healthcare LimitedInventors: Braj Bhushan Lohray, Vidya Bhushan Lohray, Vijay Kumar Barot, Saurin Khimshankar Raval, Preeti Saurin Raval, Sujay Basu
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Publication number: 20110266527Abstract: 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: ApplicationFiled: March 2, 2011Publication date: November 3, 2011Inventors: Sung-Hyun Jung, Hyung-Sun Kim, Ho-Jae Lee, Eun-Sun Yu, Mi-Young Chae, Young-Hoon Kim, Ja-Hyun Kim
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Publication number: 20110166349Abstract: 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: ApplicationFiled: May 8, 2009Publication date: July 7, 2011Applicant: The Regents of the University of CaliforniaInventors: Guy Bertrand, Vincent Lavallo, Guido D. Frey, Bruno Donnadieu, Michele Soleil-Havoup
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Publication number: 20110105554Abstract: 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, 7Type: ApplicationFiled: November 21, 2008Publication date: May 5, 2011Applicant: KINARIS BIOMEDICALS GMBHInventors: Dietmar Manstein, Roman Fedorov, Georgios Tsiavaliaris, Hans-Joachim Knölker, René Martin, Juliane Kirst, Herwig Gutzeit, Markus Böhl
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METHODS OF INHIBITING THE FORMATION OF AMYLOID-BETA DIFFUSABLE LIGANDS USING ACYLHYDRAZIDE COMPOUNDS
Publication number: 20110098309Abstract: 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: ApplicationFiled: July 11, 2008Publication date: April 28, 2011Applicant: 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: 7932403Abstract: 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: GrantFiled: December 16, 2005Date of Patent: April 26, 2011Assignee: ratiopharm GmbHInventors: Pavel Bobal, Jaroslav Frantisek, Jiri Stohandl, Kane Denike, Armin Boerner, Vitali Tararov, Andrei Korostylev, Gerd Koenig, Nicolas Jeker
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Publication number: 20110053974Abstract: 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: ApplicationFiled: September 29, 2010Publication date: March 3, 2011Applicant: DAIICHI SANKYO COMPANY, LIMITEDInventors: Narihiro TODA, Masao YOSHIDA, Rieko TAKANO, Masahiro INOUE, Takeshi HONDA, Koji MATSUMOTO, Ryutaro NAKASHIMA
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Publication number: 20110054180Abstract: 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: ApplicationFiled: September 3, 2009Publication date: March 3, 2011Applicant: USA as Represented by the Administrator of U.S. Environmental Protection AgencyInventors: Rajender S. Varma, Vivek Polshettiwar
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Publication number: 20110044898Abstract: 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: ApplicationFiled: December 2, 2008Publication date: February 24, 2011Applicant: University of SydneyInventors: Michael Kassiou, Michelle Louise James, Christopher Andrew Luus
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Publication number: 20110021528Abstract: 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: ApplicationFiled: October 1, 2010Publication date: January 27, 2011Applicant: PHARMACYCLICS, INC.Inventors: Erik J. Verner, Martin Sendzik, Chitra Baskaran, Joseph J. Buggy, James Robinson
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Publication number: 20100286109Abstract: 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: ApplicationFiled: July 22, 2010Publication date: November 11, 2010Applicant: ABBOTT LABORATORIESInventors: Michael R. Schrimpf, Kathleen H. Mortell, Diana L. Nersesian, Chih-Hung Lee, Bruce Clapham
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Publication number: 20100216862Abstract: 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: ApplicationFiled: May 6, 2010Publication date: August 26, 2010Applicant: Myriad Pharmaceuticals, Inc.Inventors: Warren S. Weiner, Rachel M. Slade, Yevgeniya I. Klimova, Ruth J. Walton, Mark B. Anderson
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Patent number: 7745481Abstract: Certain cyclooxygenase-2 inhibitors are useful for the treatment and prevention of tumors and tumor-related disorders and cachexia.Type: GrantFiled: August 13, 2004Date of Patent: June 29, 2010Assignee: Daiichi Sankyo Company, LimitedInventors: Shinichi Kurakata, Masaharu Hanai, Saori Kanai, Tomio Kimura
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Publication number: 20100160327Abstract: 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: ApplicationFiled: June 21, 2006Publication date: June 24, 2010Inventors: 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
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Patent number: 7714022Abstract: 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: GrantFiled: March 27, 2008Date of Patent: May 11, 2010Assignee: Myriad Pharmaceuticals, Inc.Inventors: Warren S. Weiner, Rachel M. Slade, Yevgeniya I. Klimova, Ruth J. Walton, Mark B. Anderson
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Patent number: 7628938Abstract: 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: GrantFiled: March 21, 2007Date of Patent: December 8, 2009Assignee: National University Corporation Nara Institute of Science and TechnologyInventors: Tsuyoshi Kawai, Takuya Nakajima, Shigekazu Kawai
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Patent number: 7618995Abstract: 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: GrantFiled: December 7, 2007Date of Patent: November 17, 2009Assignee: Sanofi-AventisInventors: Francis Barth, Christian Congy, Laurent Hortala, Murielle Rinaldi-Carmona
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Publication number: 20090281094Abstract: 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: ApplicationFiled: March 3, 2006Publication date: November 12, 2009Inventors: Mariangela Biava, Fabrizio Manetti, Delia Deidda, Raffaello Pompei, Maurizio Botta, Giulio Cesare Porretta
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Patent number: 7615647Abstract: 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: GrantFiled: August 5, 2005Date of Patent: November 10, 2009Assignee: Apotex Pharmachem Inc.Inventors: K.S. Keshava Murthy, Yajun Zhao, Daqing Che, Bhaskar Reddy Guntoori, Sammy Chris Duncan, Stephen E. Horne
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Publication number: 20090163715Abstract: 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: ApplicationFiled: May 25, 2006Publication date: June 25, 2009Applicant: EISAI R&D MANAGEMENT CO., LTD.Inventors: Mitsuo Nagai, Kazumasa Nara, Kazunori Wakasugi, Toshihiko Naito
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Patent number: 7524971Abstract: 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: GrantFiled: August 2, 2007Date of Patent: April 28, 2009Assignee: Sanofi - AventisInventors: Francis Barth, Christian Congy, Laurent Hortala, Murielle Rinaldi-Carmona
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Publication number: 20090005410Abstract: 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: ApplicationFiled: June 17, 2008Publication date: January 1, 2009Applicant: 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
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Publication number: 20080275053Abstract: 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: ApplicationFiled: October 6, 2004Publication date: November 6, 2008Inventors: Gerard Martin Paul Giblin, Adrian Hall, Ian Reginald Kilford, Xiao Qing Lewell, Neil Derek Miller, Alan Naylor
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Publication number: 20080261952Abstract: 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: ApplicationFiled: August 16, 2005Publication date: October 23, 2008Inventors: 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
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Patent number: 7323490Abstract: 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: GrantFiled: May 17, 2004Date of Patent: January 29, 2008Assignee: Ambit Biosciences CorporationInventors: 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
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Publication number: 20080006797Abstract: 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: ApplicationFiled: March 21, 2007Publication date: January 10, 2008Applicant: NATIONAL UNIVERSITY CORPORATION NARA INSTITUTE OF SCIENCE AND TECHNOLOGYInventors: Tsuyoshi Kawai, Takuya Nakajima, Shigekazu Kawai
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Patent number: 7314885Abstract: 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: GrantFiled: March 22, 2006Date of Patent: January 1, 2008Assignee: Vertex Pharmaceuticals IncorporatedInventors: Alex Aronov, Upul K. Bandarage, David J. Lauffer, Pan Li, Ronald C. Tomlinson
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Patent number: 7241803Abstract: 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: GrantFiled: November 12, 2003Date of Patent: July 10, 2007Assignee: New York Blood CenterInventors: Shibo Jiang, Asim Kumar Debnath
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Patent number: 7186749Abstract: 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: GrantFiled: August 22, 2005Date of Patent: March 6, 2007Assignee: WyethInventors: Thomas J. Commons, Douglas John Jenkins