Hetero Ring In The Polycyclo Ring System Patents (Class 546/196)
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Publication number: 20140135298Abstract: This invention is in the fields of cancer therapy. More particularly it concerns compounds which are useful agents for treating cell proliferative disorders, especially those disorders characterized by over activity and/or inappropriate activity of a EGFR, including EGFR-related cancers, particularly for expanding the efficacy of drugs previously developed for this purpose, and for methods of treatments using the compounds for this purpose.Type: ApplicationFiled: March 16, 2012Publication date: May 15, 2014Applicant: THE TRUSTEES OF THE UNIVERSITY OF PENNSYLVANIAInventors: Alan Berezov, Mark I. Greene, Natalie Minkovsky, Zheng Cai, Hongtao Zhang
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Publication number: 20140114048Abstract: Dark quencher constructs, termed “multi-chromophoric quenchers” are described herein that comprise at least two dark quenching moieties, which can be the same or different, linked together by at least one multivalent linking moiety. The structure of the multi-chromophoric quenchers can be varied to selectively enhance quenching within a specific range of reporter emission wavelengths, to quench a broader range of reporter emission wavelengths than previously possible, or can combine both concepts. Multiple types of quenching moieties can be employed to increase the absorption range and a multiple number of each type of quenching moiety can be used to increase the total absorptivity within the absorption range. The multi-chromophoric quenchers can be tethered to probes for biomolecules, insoluble supports and/or fluorescent dyes for use in a wide variety of biomolecular assays.Type: ApplicationFiled: October 15, 2013Publication date: April 24, 2014Applicant: Applied Biosystems, LLCInventors: Scott BENSON, Steven MENCHEN, Krishna UPADHYA
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Patent number: 8698117Abstract: The present invention relates to compounds represented by the following Formulas (I) and (II), Ring-A of Formulas I and II can be, for example, an aryl group, and Q? and Q?? can each be independently selected from groups, such as, halogen, —OH, —CN, amine groups, amide groups, carboxylic acid ester groups, carboxylic acid groups, alkenyl groups, alkynyl groups, carbonate groups, sulfide groups, and sulfonic acid ester groups. The present invention also relates to photochromic compositions and photochromic articles that include one or more photochromic compounds, such as represented by Formula II.Type: GrantFiled: August 31, 2011Date of Patent: April 15, 2014Assignee: Transitions Optical, Inc.Inventors: Meng He, Anil Kumar, Darrin R. Dabideen
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Patent number: 8697890Abstract: A naphthopyran compound represented by the formula B1 and B2 are selected from a phenyl, naphthyl, or heterocyclic aromatic group, or may combine to form one or more aromatic rings. B1 and B2 are optionally substituted with one or more substituents. R3, R4, R5, R6, and R10 are selected independently from hydrogen, halogen, —Ra, —OH, —ORa, —O—CO—Ra, —CN, —NO2, —SO2Ra, —SORa, —SH, —SRa, —NH2, —NHRa, —NRaRa, and —NRbRc. Any two or more of R5, R6 or R10 may combine to form a cyclic group. R7 is a mesogenic group containing at least two rings connected to each other through a covalent bond or linking unit. The linking unit is an ester, —Rd—, —O—, —ORd—, —ORdO—, —OCORd—, —OCORdO—, —S—, —CH?CH—, —CH?N—, —C?C—, or —N?N—, where Rd is a linear or branched (C1-18)alkyl or a linear or branched (C1-18)haloalkyl group. The naphthopyran compound may be incorporated into an optical article.Type: GrantFiled: October 17, 2007Date of Patent: April 15, 2014Assignee: Alphamicron IncorporatedInventors: Ludmila Sukhomlinova, Linli Su, Tamas Kosa, Bahman Taheri
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Publication number: 20140088078Abstract: The invention provides tricyclic compounds and their use in treating medical disorders, such as obesity. Pharmaceutical compositions and methods of making various tricyclic compounds are provided. The compounds are contemplated to have activity against methionyl aminopeptidase 2.Type: ApplicationFiled: May 7, 2012Publication date: March 27, 2014Applicant: ZAFGEN, Inc.Inventors: Susan Mary Cramp, Hazel Joan Dyke, Thomas David Pallin, Robert Zahler
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Publication number: 20140051673Abstract: Disclosed are carboxamide, sulfonamide and amine compounds, as well as pharmaceutical compositions and methods of use. One embodiment is a compound having the structure in which R1, R2, R4, E, T, n and x are as described herein. In certain embodiments, a compound disclosed herein activates the AMPK pathway, and can be used to treat metabolism-related disorders and conditions.Type: ApplicationFiled: October 14, 2013Publication date: February 20, 2014Applicant: RIGEL PHARMACEUTICALS, INC.Inventors: Hui Hong, Xiang Xu, Jiaxin Yu, Rajinder Singh, Ihab S. Darwish, Sambaiah Thota
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Publication number: 20140045813Abstract: The present invention encompasses compounds of the formula (I) wherein the groups A, Cy, X1 and Y are defined herein, which are suitable for the treatment of diseases related to BTK, process of making, pharmaceutical preparations which contain compounds and their methods of use.Type: ApplicationFiled: August 8, 2013Publication date: February 13, 2014Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Joerg Martin BENTZIEN, Angela Kay BERRY, Todd BOSANAC, Michael Jason BURKE, Darren Todd DISALVO, Joshua Courtney HORAN, Shuang LIANG, Can MAO, Wang MAO, Yue SHEN, Fariba SOLEYMANZADEH, Renee M. ZINDELL
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Peperidine-flavan alkaloid compounds derived from African herb tea kinkeliba as anti-diabetic agents
Patent number: 8642769Abstract: This invention provides the methods of separation and identification of a novel type of piperidine flavan alkaloids from an African herbal tea, the leaves of Combretum micranthum commonly known as kinkeliba, and the procedures for preparing the total piperidine flavan alkaloids (TPFA). In particular, this invention relates to the use of the plant extract that may contain TPFA as anti-diabetic agents in treatment of metabolic disorders and other applications related to this new chemical structure and derivatives thereof.Type: GrantFiled: May 3, 2011Date of Patent: February 4, 2014Inventors: James E. Simon, Qingli Wu, Cara Welch -
Publication number: 20140031302Abstract: The present invention includes novel derivatives, analogs, and intermediates of the natural products radicicol, pochonins, pochoximes, and their syntheses. The present invention also provides a pharmaceutical composition comprising the present compound and the use of the compound as inhibitors of kinases and of the enzyme family known as heat shock protein 90 (HSP90).Type: ApplicationFiled: October 24, 2011Publication date: January 30, 2014Applicant: UNIVERSITE DE STRASBOURGInventors: Nicolas Winssinger, Sofia Barluenga
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Patent number: 8624032Abstract: A method for producing libraries of structurally and stereochemically diverse molecules that can be screened for biological or chemical activity. A library of 91 heterocyclic compounds composed of 16 distinct scaffolds was synthesized through a sequence of phosphine-catalyzed ring-forming reactions, Tebbe reactions, Diels-Alder reactions, and, in some cases, hydrolysis to illustrate the methods. Three compounds inhibiting migration of human breast cancer cells are identified from the library.Type: GrantFiled: November 9, 2012Date of Patent: January 7, 2014Assignees: The Regents of the University of California, The University of ConnecticutInventors: Ohyun Kwon, Gabriel Fenteany
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Publication number: 20130345199Abstract: The present invention relates to 1-[m-Carboxamido(hetero)aryl-methyl]-piperidine-4-carboxamide derivatives of formula (I) wherein X, Ar1, R1, R2, R3, R4, R5 and p are as described in the description, to their preparation, to pharmaceutically acceptable salts thereof, and to their use as pharmaceuticals, to pharmaceutical compositions containing one or more compounds of formula (I), and especially to their use as CXCR7 receptor modulators.Type: ApplicationFiled: June 21, 2013Publication date: December 26, 2013Applicant: Actelion Pharmaceuticals Ltd.Inventors: Heinz FRETZ, Markus Gude, Philippe Guerry, Thierry Kimmerlin, Francois Lehembre, Thomas Pfeifer, Anja Valdenaire
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Patent number: 8614231Abstract: The present invention relates to a compound of structural formula (I) and its derivatives for use as medicinal drugs. They are preferably immunosuppressive agents, with mechanism of action based on the blockage of TCR-Nck interaction.Type: GrantFiled: June 18, 2009Date of Patent: December 24, 2013Assignee: Consejo Superior de Investigaciones CientificasInventors: Balbino Alarcon Sanchez, Aldo Borroto Revuelta, Antonio Morreale de Leon, María del Carmen Fábregas Cleveria, Maria Luz Ortiz
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Publication number: 20130337536Abstract: The present disclosure is directed to a reactive ester agent capable of conjugating a reporter molecule to a carrier molecule or solid support. The reactive ester agent has the general formula: wherein the variables are described throughout the application.Type: ApplicationFiled: August 21, 2013Publication date: December 19, 2013Applicant: LIFE TECHNOLOGIES CORPORATIONInventors: Evan Antoulinakis, Kyle Gee, Aleksey Rukavishnikov
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Publication number: 20130331578Abstract: Iminosugar compounds are described that have inbuilt delivery features by virtue of covalent incorporation of a tocopherol moiety, or alternative moieties that are analogues of tocopherol or select analogues of cholesterol, or its antagonist “Ezitimibe”; and are likely to have broad spectrum antiviral activity. The compounds differ from previous iminosugar compounds, even lipophillic ones, being more hydrophobic and resembling fats and oils in their partition behavior in vivo into lipid phases of lipoproteins, cellular lipid droplet organelles and biological membranes. These features confer a number of unique delivery attributes in vivo, favorable to the therapy of virus infections involving cells of the lymphoid system and the liver, in particular, but these features are also favorable in general for the treatment of virus infections of man and animals.Type: ApplicationFiled: June 5, 2013Publication date: December 12, 2013Inventors: J. L. Kiappes, Peter Laing, Raymond Dwek, Nicole Zitzmann, Stephanie Pollock
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Patent number: 8569282Abstract: Chemokine receptor antagonists, in particular, compounds of Formula (I-A) that act as antagonists of the chemokine CCR2 receptor, including pharmaceutical compositions and uses thereof to treat or prevent diseases associated with monocyte accumulation, lymphocyte accumulation or leukocyte accumulation are described herein.Type: GrantFiled: December 11, 2008Date of Patent: October 29, 2013Assignee: CytoPathfinder, Inc.Inventors: Efrat Ben-Zeev, Dongli Chen, Merav Fichman, Shomir Ghosh, Steffi Koerner, Jian Lin, Yael Marantz, Rosa E. Melendez, Pradyumna Mohanty, Sharon Shacham, Zhaoda Zhang
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Publication number: 20130281489Abstract: The invention provides compounds of the formula: in salt or zwitterionic form or a pharmaceutically acceptable salt thereof, wherein R1-6, a, Z and Q are as defined in the specification. These compounds are muscarinic receptor antagonists. The invention also provides pharmaceutical compositions containing such compounds, processes for preparing such compounds and methods of using such compounds to, for example, treat pulmonary disorders such as chronic obstructive pulmonary disease and asthma.Type: ApplicationFiled: June 19, 2013Publication date: October 24, 2013Applicant: THERAVANCE, INC.Inventors: Craig Husfeld, YuHua Ji, Rick Lee, Li Li, YongQi Mu, Cameron Smith, Johnny Uy
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Publication number: 20130273380Abstract: The present invention relates to controlled radical polymerization (CRP) initiators that include at least one radically transferable group. The CRP initiators include at least one of the following, (a) a spirooxazine compound represented by the following Formula (I), and (b) an indenonaphthopyran represented by the following Formula (II), One or more of R1, R2, R3, R4, R5, and R6 of the spirooxazine, and one or more of R7, R8, R9, R10, B, and B? independently include the radically transferable group. The present invention also relates to polymers, such as mechanochromic polymers, that are prepared from such CRP initiators, polymer compositions that include such polymers, and mechanochromic articles that include such polymer compositions.Type: ApplicationFiled: March 15, 2013Publication date: October 17, 2013Inventors: Charles R. Hickenboth, Cynthia Kutchiko, Matthew J. Kryger
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Patent number: 8552032Abstract: The present invention is directed to novel bicyclic derivatives, pharmaceutical compositions containing them and their use in the treatment of disorders and conditions modulated by DPP-1.Type: GrantFiled: December 16, 2010Date of Patent: October 8, 2013Assignee: Janssen Pharmaceutica NVInventors: Edward C. Lawson, Dennis J. Hlasta, Shyamali Ghosh, Renee L. DesJarlais, Carsten Schubert
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Patent number: 8551982Abstract: The present invention relates to compounds of formula (I): wherein R1 to R3, A, X and n are as defined herein. The compounds of formula (I) are useful as inhibitors of leukotriene A4 hydrolase (LTA4H) and treating LTA4H related disorder. The present invention also relates to pharmaceutical compositions comprising the compounds of formula (I), methods of using these compounds in the treatment of various diseases and disorders, and processes for preparing these compounds.Type: GrantFiled: March 13, 2012Date of Patent: October 8, 2013Assignee: Boehringer Ingelheim International GmbHInventors: Asitha Abeywardane, Michael J. Burke, Thomas Martin Kirrane, Matthew Russell Netherton, Anil Kumar Padyana, Lana Louise Smith Keenan, Hidenori Takahashi, Michael Robert Turner, Qiang Zhang, Qing Zhang
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Patent number: 8545984Abstract: Described herein are compounds generally comprising an indeno[2?,3?:3,4]naptho[1,2-b]pyran structure. Such compounds may be useful for their photochromic properties, and be used in certain photochromic compositions. Such compositions may further comprise other photochromic compositions and/or materials. Additionally, such compounds and/or compositions may be suitable for preparing certain photochromic articles. Also described herein are methods for preparing certain photochromic compounds, compositions, and articles.Type: GrantFiled: December 16, 2010Date of Patent: October 1, 2013Assignee: Transitions Optical, Inc.Inventors: Meng He, Darrin R. Dabideen, Anil Kumar, Ruisong Xu
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Publication number: 20130252937Abstract: The present invention relates to compounds of general formula I, wherein the groups R1, R2 and m are defined as in claim 1, which have valuable pharmacological properties, in particular bind to the GPR40 receptor and modulate its activity. The compounds are suitable for treatment and prevention of diseases which can be influenced by this receptor, such as metabolic diseases, in particular diabetes type 2.Type: ApplicationFiled: March 14, 2013Publication date: September 26, 2013Applicant: Boehringer Ingelheim International GmbHInventors: Matthias ECKHARDT, Sara FRATTINI, Dieter HAMPRECHT, Frank HIMMELSBACH, Elke LANGKOPF, Iain LINGARD, Stefan PETERS, Holger WAGNER
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Publication number: 20130237536Abstract: Heterocyclic compounds which modulate cannabinoid receptors are presented. Pharmaceutical compositions containing these compounds, methods of using these compounds as modulators of cannabinoid receptors and processes for synthesizing these compounds are also described herein.Type: ApplicationFiled: April 26, 2013Publication date: September 12, 2013Applicant: The Cleveland Clinic FoundationInventors: Mohamed Naguib Attala, Philippe Diaz
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Publication number: 20130237566Abstract: Disclosed are compounds of Formula (I) or stereoisomers, salts, or prodrugs thereof, wherein: W is CH2 or O; Q is Formula (II), Formula (III) or Formula (IV); and R1, R2, R3, R4, n, and G are defined herein. Also disclosed are methods of using such compounds as selective agonists for G protein-coupled receptor S1P1, and pharmaceutical compositions comprising such compounds. These compounds are useful in treating, preventing, or slowing the progression of diseases or disorders in a variety of therapeutic areas, such as autoimmune diseases and vascular disease.Type: ApplicationFiled: November 2, 2011Publication date: September 12, 2013Inventors: Robert J. Cherney, Zhongyu Wang
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Publication number: 20130231338Abstract: The present invention relates to novel benzofuran-2-sulfonamide derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of chemokine receptors.Type: ApplicationFiled: March 1, 2013Publication date: September 5, 2013Applicant: ALLERGAN, INC.Inventors: HAIQING YUAN, RICHARD L. BEARD, XIAOXIA LIU, JOHN E. DONELLO, VEENA VISWANATH, MICHAEL E. GARST
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Publication number: 20130225530Abstract: The present invention relates to a pharmaceutical composition for use as a medicament for the treatment or prophylaxis of cardiac hypertrophy, comprising at least one compound of formula (I), wherein: R1 is e.g. hydrogen, —CH3, R2 is e.g. hydrogen, —CH3, R4 is hydrogen, —OH, —NH2; R5 is hydrogen, —OH; R6 is hydrogen, —OH; R3 is e.g. —OCH3 or a pharmaceutically acceptable salt, and at least one pharmaceutical excipient.Type: ApplicationFiled: July 6, 2011Publication date: August 29, 2013Applicant: DKFZ DEUTSCHES KREBSFORSCHUNGSZENTRUMInventors: Min Li-Weber, H. Peter Krammer, Gernot Polier
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Patent number: 8518546Abstract: The present invention relates to compounds represented by the following Formula I, Ring-A of the Formula I can be, for example an aryl group, and L1 is a chiral or achiral lengthening group. The compound represented by Formula I can be a photochromic compound. The present invention also relates to photochromic compositions and photochromic articles that include one or more photochromic compounds, such as represented by Formula I.Type: GrantFiled: December 16, 2010Date of Patent: August 27, 2013Assignee: Transitions Optical, Inc.Inventors: Meng He, Sujit Mondal, Darrin R. Dabideen, Anil Kumar, Xiao-Man Dai
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Publication number: 20130197033Abstract: A compound represented by Formula (1), or a pharmacologically acceptable salt thereof retains the principal therapeutic effect of paroxetine and has an improved CYP inhibitory effect: wherein R1 is a hydrogen atom or C1-6 alkyl group.Type: ApplicationFiled: January 29, 2013Publication date: August 1, 2013Applicant: EISAI R&D MANAGEMENT CO., LTD.Inventor: EISAI R&D MANAGEMENT CO., LTD.
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Publication number: 20130196987Abstract: The present invention provides compounds, methods for the synthesis thereof and methods for the use thereof in the treatment of various disorders including inflammatory or autoimmune disorders, and disorders involving malignancy or increased angiogenesis.Type: ApplicationFiled: October 30, 2012Publication date: August 1, 2013Applicant: EISAI CO., LTD.Inventors: Roch Boivin, Kenichi Chiba, Jesse Chow, Hong Du, Yoshihito Eguchi, Masanori Fujita, Masaki Goto, Fabian Gusovsky, Jean-Christophe Harmange, Atsushi Inoue, Yimin Jiang, Megumi Kawada, Takatoshi Kawai, Yoshiyuki Kawakami, Akifumi Kimura, Makoto Kotake, Yoshikazu Kuboi, Charles-Andre Lemelin, Xiang-Yi Li, Tomohiro Matsushima, Yoshiharu Mizui, Kenzo Muramoto, Hideki Sakurai, Yong-Chun Shen, Hiroshi Shirota, Mark Spyvee, Isao Tanaka, John (Yuan) Wang, Satoshi Yamamoto, Naoki Yoneda
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Publication number: 20130150401Abstract: The present invention relates to compounds of formula I, wherein R1, LP, LQ, X, A, and n are as defined in the application, which have valuable pharmacological properties, and in particular bind to the GPR119 receptor and modulate its activity.Type: ApplicationFiled: December 6, 2012Publication date: June 13, 2013Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventor: Boehringer Ingelheim International GmbH
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Publication number: 20130143921Abstract: This invention provides the methods of separation and identification of a novel type of piperidine flavan alkaloids from an African herbal tea, the leaves of Combretum micranthum commonly known as kinkeliba, and the procedures for preparing the total piperidine flavan alkaloids (TPFA). In particular, this invention relates to the use of the plant extract that may contain TPFA as anti-diabetic agents in treatment of metabolic disorders and other applications related to this new chemical structure and derivatives thereof.Type: ApplicationFiled: May 3, 2011Publication date: June 6, 2013Applicant: RUTGERS, THE STATE UNIVERSITY OF NEW JERSEYInventors: James E. Simon, Qingli Wu, Cara Welch
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Patent number: 8440832Abstract: Heterocyclic compounds which modulate cannabinoid receptors are presented. Pharmaceutical compositions containing these compounds, methods of using these compounds as modulators of cannabinoid receptors and processes for synthesizing these compounds are also described herein.Type: GrantFiled: July 14, 2008Date of Patent: May 14, 2013Assignee: Board of Regents, The University of Texas SystemInventors: Mohamed Naguib Attala, Philippe Diaz
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Publication number: 20130116247Abstract: Compounds which directly inhibit IRE-1? activity in vitro, prodrugs, and pharmaceutically acceptable salts there-of. Such compounds and prodrugs are useful for treating diseases associated with the unfolded protein response or with regulated IRE1-dependent decay (RIDD) and can be used as single agents or in combination therapies.Type: ApplicationFiled: April 5, 2011Publication date: May 9, 2013Applicant: MANNKIND CORPORATIONInventors: Qingping Zeng, Andras Toro, John Bruce Patterson, Warren Stanfield Wade, Zoltan Zubovics, Yun Yang, Zhipeng Wu
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Publication number: 20130116232Abstract: Described herein are compounds that are estrogen receptor modulators. Also described are pharmaceutical compositions and medicaments that include the compounds described herein, as well methods of using such estrogen receptor modulators, alone and in combination with other compounds, for treating diseases or conditions that are mediated or dependent upon estrogen receptors.Type: ApplicationFiled: June 8, 2011Publication date: May 9, 2013Applicant: ARAGON PHARMACEUTICALS, INC.Inventors: Mehmet Kahraman, Steven P. Govek, Johnny Y. Nagasawa, Nicholas D. Smith
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Patent number: 8436184Abstract: A naphthopyran compound represented by the formula (I) wherein: n1, n2, p, m and q represent an integer; R1, R2 and R4, represent a group selected from halogen, —Ra, —OH, —ORa, —SH, —SRa, —NH2, —NRaRa1, —NRbRc, —CO—Ra, —CO2Ra1, —OC(O)—Rd, —X—(Re)—Y, linear or branched (C1-C18) perfluoroalkyl group, wherein Ra, Ra1, Rb, Rc, X, Y, Re, and Rd are as defined in the description; Z represents a group selected from CO, CS, SO, SO2, CO2, C(O)S, CS2, C(O)NH, C(O)NRa, C(S)NH, C(S)NRa and C?NRa; R3 represents a group selected from halogen, —Ra, linear or branched (C1-18) perfluoroalkyl group —OH, —ORa, —SH, —SRa, —NH2, and —NRaRa1; R6 represents a group selected from —Ra which may be optionally substituted, linear or branched (C1-18) perfluoroalkyl, cycloalkyl, heterocycloalkyl, aryl, and heteroaryl, which may be optionally substituted; R5 represents a group selected from: halogen, —Ra, linear or branched (C1-18) perfluoroalkyl group, —OH, —ORa, —SH, —SRa, —NH2, —NRaRa1, —CO—Ra, —O—C(O)—Ra and —CO2Ra1; or when q is equaType: GrantFiled: September 5, 2007Date of Patent: May 7, 2013Assignee: Essilor International (Compagnie Generale d'OptiqueInventors: Stuart Aiken, Jean-Paul Cano, Christopher David Gabbutt, Bernard Mark Heron
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Patent number: 8410271Abstract: This invention relates to chromen-2-one derivatives useful as monoamine neurotransmitter re-uptake inhibitors. In other aspects the invention relates to the use of these compounds in a method for therapy and to pharmaceutical compositions comprising the compounds of the invention.Type: GrantFiled: November 10, 2009Date of Patent: April 2, 2013Assignee: Neurosearch A/SInventors: Dan Peters, Gunnar M. Olsen, Jorgen Scheel-Kruger, Elsebet Ostergaard Nielsen
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Publication number: 20130065056Abstract: The present invention provides ophthalmic devices comprising at least one photochromic material which is an indeno-fused naphthopyran having a pi-conjugation extending group bonded to the 11-position of the indeno-fused naphthopyran, the pi-conjugation extending group having at least one pendent halo-substituted group bonded thereto. The pi-conjugation extending group extends the pi-conjugation system of said indeno-fused naphthopyran. The 13-position of the indeno-fused naphthopyran is substantially free of spiro-substituents. The invention further provides photochromic materials of specified structure, photochromic compositions, photochromic articles and optical elements that include the photochromic materials. Other non-limiting embodiments relate to methods of making the ophthalmic devices comprising photochromic materials.Type: ApplicationFiled: March 12, 2012Publication date: March 14, 2013Inventors: Anu Chopra, Jun Deng, Beon-Kyu Kim, David B. Knowies, Frank F. Molock, JR., Victor A. Montes, Stephen D. Straight, Wenjing Xiao, Huayun Yu
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Publication number: 20130065859Abstract: The present invention relates to substituted 2-(chroman-6-yloxy)-thiazoles of the formula I, in which Ar, R2, R3 and R4 are as defined in the claims. The compounds of the formula I are inhibitors of the sodium-calcium exchanger (NCX), especially of the sodium-calcium exchanger of subtype 1 (NCX1), and are suitable for the treatment of diverse disorders in which intracellular calcium homeostasis is disturbed, such as arrhythmias, heart failure and stroke. The invention furthermore relates to processes for the preparation of the compounds of the formula I, their use as pharmaceuticals, and pharmaceutical compositions comprising them.Type: ApplicationFiled: September 12, 2011Publication date: March 14, 2013Applicant: SANOFIInventors: Werngard CZECHTIZKY, John WESTON, Nils RACKELMANN, Michael PODESCHWA, Petra ARNDT, Klaus WIRTH, Heinz GOEGELEIN, Olaf RITZELER, Volker KRAFT, Patrice BELLEVERGUE, Gary MCCORT
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Patent number: 8394794Abstract: The invention provides compounds of Formula (I) and (IV): as described herein, as well as salts thereof. The compounds have anti-cancer properties and/or chemosensitization properties.Type: GrantFiled: March 21, 2008Date of Patent: March 12, 2013Assignee: Regents of The University of MinnesotaInventors: Chengguo Xing, Jignesh Doshi
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Patent number: 8388872Abstract: The present invention provides a photochromic material which is an indeno-fused naphthopyran of structural formulas I or II, having a pi-conjugation extending group bonded to the 11-position of the indeno-fused naphthopyran, the pi-conjugation extending group having at least one pendent halo-substituted group bonded thereto. The pi-conjugation extending group extends the pi-conjugation system of said indeno-fused naphthopyran. The 13-position of the indeno-fused naphthopyran is substantially free of spiro-substituents. The invention further provides photochromic materials of specified structure, photochromic compositions, photochromic articles and optical elements that include the photochromic material.Type: GrantFiled: February 21, 2012Date of Patent: March 5, 2013Assignee: Transitions Optical, Inc.Inventors: Anu Chopra, Jun Deng, Beon-Kyu Kim, David B. Knowles, Frank F. Molock, Jr., Victor A. Montes, Stephen D. Straight, Wenjing Xiao, Huayun Yu
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Publication number: 20130035323Abstract: The present invention relates to aminochromane, aminothiochromane and amino-1,2,3,4-tetrahydroquinoline derivatives of the formula (I) or a physiologically tolerated salt thereof. The invention relates to pharmaceutical compositions comprising such aminochromane, aminothiochromane and amino-1,2,3,4-tetrahydroquinoline derivatives, and the use of such aminochromane, aminothiochromane and amino-1,2,3,4-tetrahydroquinoline derivatives for therapeutic purposes. The aminochromane, aminothiochromane and amino-1,2,3,4-tetrahydroquinoline derivatives are GlyT1 inhibitors.Type: ApplicationFiled: August 3, 2012Publication date: February 7, 2013Applicant: Abbott GmbH & Co. KGInventors: Wilhelm AMBERG, Udo LANGE, Frauke POHLKI
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Publication number: 20130018030Abstract: The present invention relates to compounds of general formula I, wherein the groups R1, LP, LQ, X1, X2, X3, A, n and m are as defined in the application. The compounds of formula I have valuable pharmacological properties, and in particular bind to the GPR119 receptor and modulate its activity.Type: ApplicationFiled: January 20, 2012Publication date: January 17, 2013Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Frank HIMMELSBACH, Elke LANGKOPF, Bernd NOSSE
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Publication number: 20120329832Abstract: This invention relates to novel coumarin derivative, formulations comprising same, and to methods of making and using these compounds and formulations, which are useful as repellents against insects and/or pests. The compounds also prevent illness and disease caused by insect/pest-borne vectors, and provide safer, more effective alternatives to existing repellents.Type: ApplicationFiled: June 21, 2012Publication date: December 27, 2012Inventors: Jean Delaveau, Emile Vialle, Marc Lemaire, Stephane Pellet-Rostaing, Bruno Andrioletti
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Publication number: 20120328661Abstract: The present invention relates to novel 2-oxo-2H-chromene-3-carboxamide derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of sphingosine-1-phosphate receptors.Type: ApplicationFiled: October 20, 2010Publication date: December 27, 2012Applicant: ALLERGAN, INC.Inventors: Todd M. Heidelbaugh, John R. Cappiello, Phong X. Nguyen, Dario G. Gomez
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Publication number: 20120322784Abstract: The present invention relates to compounds of formula I, wherein the groups R1, LP, LQ, X1, X2, X3, Ar and n are as defined in the application, which have valuable pharmacological properties, and in particular bind to the GPR119 receptor and modulate its activity.Type: ApplicationFiled: December 16, 2011Publication date: December 20, 2012Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Frank HIMMELSBACH, Matthias ECKHARDT, Niklas HEINE, Elke LANGKOPF, Bernd NOSSE
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Publication number: 20120302539Abstract: Certain compounds and pharmaceutically acceptable salts are provided herein. Also provided are pharmaceutical compositions comprising at least one compound or pharmaceutically acceptable salt therein and one or more pharmaceutically acceptable vehicle. Methods of treating patients suffering from certain disease states responsive to the inhibition of transglutaminase TG2 activity are described. These disease states include neurodegenerative disorders such as Huntington's disease. Also described are methods of treatment include administering at least one compound or pharmaceutically acceptable salt thereof as a single active agent or administering at least one compound or pharmaceutically acceptable salt thereof in combination with one or more other therapeutic agents.Type: ApplicationFiled: May 7, 2012Publication date: November 29, 2012Inventors: Michael Prime, Stephen Martin Courtney, Richard Marston, Celia Dominguez, Douglas Macdonald, John Wityak
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Patent number: 8309596Abstract: The present invention relates to the crystal structure of the serine protease kallikrein 7 and to the use of this crystal structure in drug discovery. The present invention also relates to compounds binding specifically to this active site of kallikrein 7.Type: GrantFiled: June 26, 2008Date of Patent: November 13, 2012Assignee: Novartis AGInventors: Stefanie Flohr, Stefan Andreas Randl, Nils Ostermann, Ulrich Hassiepen, Frederic Berst, Ursula Bodendorf, Bernd Gerhartz, Andreas Marzinzik, Claus Ehrhardt, Josef Gottfried Meingassner
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Patent number: 8308996Abstract: A photochromic chromene compound which develops a color of a neutral tint, has high color optical density, a high fading speed and high durability, and has an indeno(2,1-f)naphtho(1,2-b)pyran structure represented by the following formula as the basic skeleton, wherein a sulfur-containing substituent selected from thiol group, alkylthio group, alkoxyalkylthio group, haloalkylthio group, cycloalkylthio group, arylthio group and heteroarylthio group is bonded to the 6-position and/or 7-position carbon atom(s).Type: GrantFiled: August 4, 2010Date of Patent: November 13, 2012Assignee: Tokuyama CorporationInventors: Toshiaki Takahashi, Junji Takenaka, Junji Momoda, Kazuhiro Teranishi
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Patent number: 8308995Abstract: A chromene compound represented by the following formula (1): wherein R1, R2, R3, R4, R5, R6, m, and n are defined in the specification. The chromene compound is rarely deteriorated by exposure.Type: GrantFiled: February 9, 2012Date of Patent: November 13, 2012Assignee: Tokuyama CorporationInventors: Soko Kasai, Shinobu Izumi
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Publication number: 20120283254Abstract: The present invention is concerned with novel selective dual modulators of the 5-HT2A and D3 receptors of formula (I) wherein R1, R2, R3, n, and Y are as described herein, as well as pharmaceutically acceptable salts and esters thereof. Further the present invention is concerned with the manufacture of the compounds of formula (I), pharmaceutical compositions comprising them and their use as pharmaceuticals.Type: ApplicationFiled: April 27, 2012Publication date: November 8, 2012Inventors: Rosa Maria Rodriguez Sarmiento, Juergen Wichmann
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Publication number: 20120270736Abstract: This invention provides compounds having the structure which may be used for the treatment of tumors.Type: ApplicationFiled: June 30, 2011Publication date: October 25, 2012Applicant: Lixte Biotechnology, Inc.Inventors: John S. Kovach, Francis Johnson