The Five-membered Hetero Ring Contains One Double Bond Only (i.e., Indolines) Patents (Class 548/490)
-
Publication number: 20110028468Abstract: This invention provides a compound of the formula (I): a pharmaceutically acceptable salt or solvate thereof, wherein R1 is substituted or unsubstituted alkyl or the like, R2 is hydrogen or substituted or unsubstituted alkyl, Ring A is monocyclic or bicyclic aromatic heterocycle, R3 is substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl or substituted or unsubstituted heterocycle, R4 is halogen, cyano, substituted or unsubstituted alkyl, substituted or unsubstituted cycloalkyl or the like, m is an integer between 0 and 2, n is an integer between 0 and 5, R is halogen, oxo, cyano, nitro, substituted or unsubstituted alkyl or the like, and p is an integer between 0 and 2 as novel compounds having NPY Y5 antagonistic activity.Type: ApplicationFiled: April 20, 2009Publication date: February 3, 2011Applicant: Shinonogi & Co., LtdInventors: Masahiro Sakagami, Hiroshi Hashizume, Satoru Tanaka, Takayuki Okuno, Hiroshi Yari, Keisuke Tonogaki, Naoki Kouyama
-
Publication number: 20110015375Abstract: Methods for identifying MarR family inhibiting compounds are described. The methods include the use of computer aided rational based drug design programs and three dimensional structures of MarR family polypeptides.Type: ApplicationFiled: June 18, 2009Publication date: January 20, 2011Applicant: Paratek Pharmaceuticals, Inc.Inventors: Michael N. Alekshun, Stuart B. Levy, Brent L. Podlogar, Roger Frechette
-
Publication number: 20100331540Abstract: A method for producing a compound having a deuterated aromatic ring or heterocyclic ring according to the invention includes heating a compound having an aromatic ring or heterocyclic ring in the presence of heavy water, a transition metal and a metal which generates deuterium. As the metal which generates deuterium, at least one metal selected from the group consisting of aluminum, magnesium, zinc, iron, lead and tin is preferred. As the transition metal, at least one metal selected from the group consisting of platinum, palladium, ruthenium and rhodium is preferred. The heating is preferably carried out by microwave irradiation.Type: ApplicationFiled: January 30, 2009Publication date: December 30, 2010Inventors: Haruki Shimodaira, Toshifumi Abe, Akira Miyazawa, Yuji Kawanishi, Taichi Abe
-
Publication number: 20100324130Abstract: Peripheral Benzodiazepine Receptor (PBR) is an attractive target for tumor imaging and treatment due to its up-regulation in numerous cancer cell types. DAA1 106 is a selective PBR ligand with high binding affinity. Aspects of the present invention are series of functionalized DAA1 106 analogs, which can be conjugated to a variety of signaling and treatment moieties, and are widely applicable in PBR targeted molecular imaging and drug delivery.Type: ApplicationFiled: December 5, 2007Publication date: December 23, 2010Inventors: Darryl J. Bornhop, Mingfeng Bai
-
Publication number: 20100320451Abstract: A fused aromatic ring derivative shown by the following formula (1): wherein Ra and Rb are independently a hydrogen atom or a substituent, m and n are independently an integer of 1 to 13, and when m and n are two or more, Ras and Rbs may be independently the same or different, and L1 is a single bond or a substituted or unsubstituted divalent linking group, provided that the fused aromatic ring derivative shown by the formula (1) does not have an anthracene ring.Type: ApplicationFiled: November 10, 2008Publication date: December 23, 2010Inventor: Masahiro Kawamura
-
Publication number: 20100304074Abstract: A novel indolium compound of general formula (I) and an optical recording material containing the indolium compound. In general formula (I), ring A is a benzene ring, etc.; R1 is a group of general formula (II), etc.; R2 is a C1-C30 organic group, etc.; Y1 is a C1-C10 alkyl group, etc.; Z1 is, e.g., a C1-C8 alkyl group optionally substituted with a halogen group and optionally interrupted by —O—, etc.; Z2 is, e.g., a C1-C8 alkyl group optionally substituted with a halogen group and optionally interrupted by —O—, etc.; a is an integer of 0 to 6; b is an integer of 0 to 5; Anq- is a q-valent anion; q is 1 or 2; and p is a number necessary to neutralize an electric charge.Type: ApplicationFiled: September 26, 2008Publication date: December 2, 2010Applicant: ADEKA CORPORATIONInventors: Toru Yano, Yohei Aoyama
-
Patent number: 7834037Abstract: Described herein are compounds and pharmaceutical compositions containing such compounds, which modulate the activity of 5-lipoxygenase-activating protein (FLAP). Also described herein are methods of using such FLAP modulators, alone and in combination with other compounds, for treating respiratory, cardiovascular, and other leukotriene-dependent or leukotriene mediated conditions or diseases.Type: GrantFiled: October 27, 2007Date of Patent: November 16, 2010Assignee: Amira Pharmaceuticals, Inc.Inventors: John Howard Hutchinson, Nicholas Simon Stock, Jeffrey Roger Roppe
-
Publication number: 20100274023Abstract: The present invention provides new intermediate compounds enabling the preparation of N-meso substituted cyanine, merocyanine or oxonole dyes wherein the N-meso substituent comprises electron withdrawing groups and wherein such N-meso substituents are introduced at the intermediate level. These intermediates enable the formation of dyes having in the meso-position N-substituents comprising electron withdrawing groups without the need for further derivatization of the meso-substituent at the dye level.Type: ApplicationFiled: December 18, 2008Publication date: October 28, 2010Applicant: Agfa Graphics NVInventors: Paul Callant, Jos Louwet
-
Patent number: 7728023Abstract: The present invention relates to a compound represented by the formula (I), wherein all symbols are as defined in the description, a salt thereof, a solvate thereof, or a prodrug thereof, which has a leukotriene receptor antagonistic activity which is expected to be more effective than those of the leukotriene receptor antagonists currently used in clinical trials. Therefore, it is useful as an agent for the prevention and/or treatment of a leukotriene-mediated disease such as a respiratory diseases such as bronchial asthma, chronic obstructive pulmonary disease, pulmonary emphysema, chronic bronchitis, pneumonia (e.g. interstitial pneumonia etc.), severe acute respiratory syndrome (SARS), acute respiratory distress syndrome (ARDS), allergic rhinitis, sinusitis (e.g. acute sinusitis, chronic sinusitis, etc.), or the like, or as an expectorant or an antiitussive.Type: GrantFiled: February 24, 2006Date of Patent: June 1, 2010Assignee: Ono Pharmaceutical Co., Ltd.Inventors: Jun Takeuchi, Yoshisuke Nakayama, Manabu Fujita
-
Publication number: 20100130736Abstract: Drug discovery is a complex undertaking facing many challenges, not the least of which is a high attrition rate as many promising candidates prove ineffective or toxic in the clinic owing to a poor understanding of the diseases, and thus the biological systems, they target. Therefore, it is broadly agreed that to increase the productivity of drug discovery one needs a far deeper understanding of the molecular mechanisms of diseases, taking into account the full biological context of the drug target and moving beyond individual genes and proteins. The present methods rely on the use of label-free cellular assays, particularly the DMR index, to systematically display the mode of actions, the toxicity, and the target(s) and pathway(s) of any molecules.Type: ApplicationFiled: November 23, 2009Publication date: May 27, 2010Inventors: Ye Fang, Ann M. Ferrie, Joydeep Lahiri, Elizabeth Tran
-
Publication number: 20100130468Abstract: The invention is directed to novel indole carboxamide derivatives. Specifically, the invention is directed to compounds according to formula (I): wherein R1, R2, R3, R4, and m are as defined herein. The compounds of the invention are inhibitors of IKK2 and can be useful in the treatment of disorders associated with inappropriate IKK2 (also known as IKK?) activity, such as rheumatoid arthritis, asthma, rhinitis, and COPD (chronic obstructive pulmonary disease). Accordingly, the invention is further directed to pharmaceutical compositions comprising a compound of the invention. The invention is still further directed to methods of inhibiting IKK2 activity and treatment of disorders associated therewith using a compound of the invention or a pharmaceutical composition comprising a compound of the invention.Type: ApplicationFiled: March 20, 2008Publication date: May 27, 2010Inventors: Jeffrey Charles Boehm, Jakob Busch-Petersen, Wei Fu, Qi Jin, Jeffrey K. Kerns, Huijie Li, Guoliang Lin, Xichen Lin, Christopher E. Neipp
-
Patent number: 7713996Abstract: The invention is concerned with novel heterobicyclic derivatives of formula (I): wherein R1, R2, R3, R4, R5, R6, R7, A, X and Y are as defined in the description and in the claims, as well as physiologically acceptable salts and esters thereof. These compounds inhibit L-CPT1 and can be used as medicaments.Type: GrantFiled: September 12, 2006Date of Patent: May 11, 2010Assignee: Hoffmann-La Roche Inc.Inventors: Jean Ackermann, Konrad Bleicher, Simona M Ceccarelli Grenz, Odile Chomienne, Patrizio Mattei, Tanja Schulz-Gasch
-
Publication number: 20100105924Abstract: The present invention relates to processes of producing glutamic acid compounds, for example, monatin, which are useful as, for example, production intermediates for sweetener or pharmaceutical products.Type: ApplicationFiled: November 6, 2009Publication date: April 29, 2010Applicant: AJINOMOTO CO. INC.Inventors: Shigeru KAWAHARA, Nao FUNAKOSHI
-
Patent number: 7705035Abstract: The invention is directed to indoline amide derivatives of formula I as EP4 receptor ligands, antagonists or agonists, useful for the treatment of EP4 mediated diseases or conditions, such as acute and chronic pain, osteoarthritis, rheumatoid arthritis, cancer and glaucoma. Pharmaceutical compositions and methods of use are also included.Type: GrantFiled: June 8, 2007Date of Patent: April 27, 2010Assignee: Merck Frosst Canada Ltd.Inventors: Michael Boyd, John Colucci
-
Publication number: 20100087484Abstract: The present invention relates to novel aminoalkoxy arylsulfonamide compounds of the formula (I), their derivatives, their stereoisomers, their pharmaceutically acceptable salts and pharmaceutically acceptable compositions containing them. The present invention also relates to a process for the preparation of above said novel compounds, their derivatives, their stereoisomers, their pharmaceutically acceptable salts and pharmaceutically acceptable compositions containing them. These compounds are useful in the treatment of various disorders that are related to 5-HT6 receptor functions. Specifically, the compounds of this invention are also useful in the treatment of various CNS disorders, hematological disorders, eating disorders, diseases associated with pain, respiratory diseases, genito-urological disorders, cardiovascular diseases and cancer.Type: ApplicationFiled: April 15, 2008Publication date: April 8, 2010Applicant: Suven Life Sciences LimitedInventors: Nirogi Ramakrishna, Rama Sastri Kambhampati, Anil Karbhari Shinde, Anand Vijaykumar Daulatabad, Adi Reddy Dwarampudi, Nagaraj Vishwottam Kandikere, Santosh Vishwakarma, Venkateswarlu Jasti
-
Publication number: 20100076041Abstract: The use of substituted amides of structure (I) for modulating the activity of 11 ?-hydroxysteroid dehydrogenase type 1 (11 ?HSD1) and the use of these compounds as pharmaceutical compositions, are described. Also a novel class of substituted amides, their use in therapy, pharmaceutical compositions comprising the compounds, as well as their use in the manufacture of medicaments are described. The present compounds are modulators and more specifically inhibitors of the activity of 11 ?HSD1 and may be useful in the treatment, prevention and/or prophylaxis of a range of medical disorders where a decreased intracellular concentration of active glucocorticoid is desirable.Type: ApplicationFiled: March 9, 2007Publication date: March 25, 2010Inventors: John Paul Kilburn, Henrik Sune Andersen, Gita Camilla Tejlgaard Kampen
-
Publication number: 20100075962Abstract: Disclosed are indole derivatives a preparation method thereof, and a composition for the prevention and treatment of metabolic diseases, containing the same as an active ingredient. The indole derivatives have inhibitory activity against DGAT (diacylglycerol acyltransferase), which causes metabolic diseases such as obesity and diabetes in the process of lipid metabolism. With the ability to effectively control lipid metabolism and energy metabolism, the composition is thus useful in the prevention and treatment of metabolic diseases, such as obesity and diabetes.Type: ApplicationFiled: September 27, 2007Publication date: March 25, 2010Applicant: Korea Research Institute of Bioscience and BiotechnologyInventors: Kyeong Lee, Hyun Sun Lee, Jung Joon Lee, Young Kook Kim, Mun-Chual Roh, Jeong Hyung Lee, Hye-Ran Park, Chul-Ho Lee, Yongseok Choi
-
Patent number: 7671080Abstract: The present invention relates to i-benzylindole-2-carboxamide derivatives of formula I, or a pharmaceutically acceptable salt or solvate thereof. The invention also relates to pharmaceutical compositions comprising said 1-benzylindole-2-carboxamide derivatives and to their use in therapy, particularly for the treatment of obesity or nicotine dependence.Type: GrantFiled: March 17, 2006Date of Patent: March 2, 2010Assignee: N.V. OrganonInventors: Phillip Martin Cowley, Samuel George Gibson, Grant Wishart
-
Patent number: 7662824Abstract: The invention is directed to acylhydrazones compounds of Formula I: where R1, R2 and A are as defined herein, the use of such compounds as protein tyrosine kinase modulators, particularly inhibitors of c-Met, and the use of such compounds to reduce or inhibit kinase activity of c-Met in a cell or a subject, and modulate c-Met expression in a cell or subject, and the use of such compounds for preventing or treating in a subject a cell proliferative disorder and/or disorders related to c-Met. The present invention is further directed to pharmaceutical compositions comprising the compounds of the present invention and to methods for treating conditions such as cancers and other cell proliferative disorders.Type: GrantFiled: March 16, 2006Date of Patent: February 16, 2010Assignee: Janssen Pharmaceutica NVInventors: Kristi Leonard, Tianbao Lu, Robert W. Tuman, Dana L. Johnson, Anna C. Maroney, Jan L. Sechler, Richard W. Connors, Richard S. Alexander, Maxwell D. Cummings, Robert A. Galemmo, Thomas P. Markotan
-
Patent number: 7655680Abstract: Thiazole compounds for inhibiting the activity of phosphodiesterase 4, the production of tumor necrosis factor alpha, and the production of interleukin 4. The compounds of the invention are represented by general formula (1): wherein A is any one of the following groups (i) and (ii): (i) —CO—B— wherein B is a C1-6 alkylene group and (ii) —CO—Ba— wherein Ba is a C2-6 alkenylene group, and include optical isomers and salts of the compounds.Type: GrantFiled: May 16, 2005Date of Patent: February 2, 2010Assignee: Otsuka Pharmaceutical Co., Ltd.Inventors: Isao Takemura, Kenji Watanabe, Kunio Oshima, Nobuaki Ito, Junpei Haruta, Hidetaka Hiyama, Masatoshi Chihiro, Hideki Kawasome, Yoko Sakamoto, Hironobu Ishiyama, Takumi Sumida, Kazuhiko Fujita, Hideki Kitagaki
-
Publication number: 20090298905Abstract: This invention is related to new nitrogenated trans-stilbene analog compounds, more specifically, imine, pyrrol and Indole derivatives, with procedures for the preparation and use thereof as pharmaceutical compositions for the treatment and/or chemoprevention of those mammalian diseases such as cancer, fibrosclerosis and acute/chronic inflammation, graft-versus-host reaction, ischemic-reperfusion tissue injury in stroke and heart attack, neurodegeneration, and during organ transplantation, whose pathogenic and pathophysiological mechanisms depend on or are significantly contributed by undesirable oxidative stress, angiogenic and proliferative responses.Type: ApplicationFiled: April 12, 2006Publication date: December 3, 2009Inventors: Fernando Pedro Cossio, Eneko Aldaba Arevalo, Yosu Ion Vara Salazar, Aizpea Zubia Olascoaga, Silvia Vivanco Amato, Miren Lorea Mendoza Arteche, Clarisa Salado Pogonza, Natalia Gallot Escobal, Fernando Vidal Vanaclocha
-
Publication number: 20090264653Abstract: Indoles that have activity as inhibitors of FAAH are described as are indoles and indole derivatives that have activity as inhibitors of DAO.Type: ApplicationFiled: December 18, 2006Publication date: October 22, 2009Inventors: Wilmin Bartolini, Brian M Cali, Barbara Chen, Yueh-Tyng Chien, Mark G. Currie, G. Todd Milne, James Philip Pearson, John Jeffrey Talley, Jane Yang, Craig Zimmerman, Charles Kim, Kevin Sprott, Timothy Barden, Regina Lundigran, Ara Mermerian
-
Patent number: 7592343Abstract: Compounds of formula (Ia): where x, y, G, L, M, W, R2, R3, R5, R5a, R6, R6a, R7, R7a, R8 and R8a are defined herein, are disclosed, as well as pharmaceutical compositions comprising the compounds. These compounds and pharmaceutical compositions are useful in treating SCD-mediated diseases or conditions.Type: GrantFiled: September 20, 2005Date of Patent: September 22, 2009Assignee: Xenon Pharmaceuticals Inc.Inventors: Rajender Kamboj, Zaihui Zhang, Jianmin Fu, Vandna Raina, Serguei Sviridov, Vishnumurthy Kodumuru, Nagasree Chakka, Shifeng Liu, Shaoyi Sun, Duanjie Hou
-
Publication number: 20090233979Abstract: The invention provides compounds of formula (I) or pharmaceutically acceptable esters, amides, solvates or salts thereof, including salts of such esters or amides, and solvates of such esters, amides or salts, (I) wherein R1, R2, R3, R4, R5, R6, Y and W are as defined in the specification. The invention also provides the use of such compounds in the treatment or prophylaxis of a condition that may be treated with a thyroid receptor agonist or partial agonist.Type: ApplicationFiled: May 24, 2007Publication date: September 17, 2009Applicant: KARO BIO ABInventors: Ana Maria Garcia Collazo, Eva Kristina Koch, Lars Johan Malm, Aiping Cheng, Tomas Fredrik Hansson
-
Publication number: 20090227571Abstract: Provided herein are compounds that bind to androgen receptors and modulate the activity and/or the amount of androgen receptors and to methods for making and using such compounds. Also provided are compositions including such compounds and methods for making and using such compositions.Type: ApplicationFiled: June 30, 2006Publication date: September 10, 2009Inventors: Jon C. Loren, Todd Miller, Bijan Pedram, Charlene V. Rowley, Yixing Shen, Cornelis Arjan Van Oeveren, Lin Zhi
-
Patent number: 7566716Abstract: Compounds of Formula I are useful for inhibiting Raf kinase and for treating disorders mediated thereby. Methods of using compounds of Formula I, and stereoisomers, tautomers, solvates and pharmaceutically acceptable salts thereof, for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions are disclosed.Type: GrantFiled: May 18, 2006Date of Patent: July 28, 2009Assignee: Array Biopharma Inc.Inventors: Ellen Laird, George Topalov, Joseph P. Lyssikatos, Mike Welch, Jonas Grina, Josh Hansen, Brad Newhouse
-
Publication number: 20090184235Abstract: A merocyanine dye is provided. The merocyanine dye is represented by formula (1). In the formula (1), A1 represents a divalent atomic group, n represents an integer of 1 to 3, A2 and A3 each independently represent an aromatic hydrocarbon ring or a heterocyclic ring having 3 to 18 carbon atoms, and R11 and R12 each independently represent a hydrogen atom, an alkyl group having 1 to 18 carbon atoms, an aryl group having 6 to 18 carbon atoms, or a heterocyclic group having 3 to 18 carbon atoms.Type: ApplicationFiled: January 16, 2009Publication date: July 23, 2009Applicant: FUJIFILM CORPORATIONInventors: Kimiatsu NOMURA, Rui SHEN, Hideyuki SUZUKI
-
Patent number: 7531577Abstract: Compounds of the formula I: or pharmaceutically acceptable salts thereof, wherein Ar, X, m, R1, R2 are as defined herein. Also provided are methods for preparing, compositions comprising, and methods for using compounds of formula I for treatment of 5-HT6-mediated diseases.Type: GrantFiled: June 20, 2007Date of Patent: May 12, 2009Assignee: Roche Palo Alto LLCInventors: Ralph New Harris, III, James M. Kress, David Bruce Repke, Russell Stephen Stabler
-
Patent number: 7524878Abstract: Disclosed are compounds and pharmaceutically acceptable salts of formula (A): which are useful in the treatment of metabolic disorders related to insulin resistance, leptin resistance, or hyperglycemia. Compounds of the invention include inhibitors of Protein tyrosine phosphatases, in particular Protein tyrosine phosphatase-1B (PTP-1B), that are useful in the treatment of diabetes and other PTP mediated diseases, such as cancer, neurodegenerative diseases and the like. Also disclosed are pharmaceutical compositions comprising compounds of the invention and methods of treating the aforementioned conditions using such compounds.Type: GrantFiled: April 30, 2004Date of Patent: April 28, 2009Assignee: The Institute for Pharmaceuticals Discovery LLCInventors: Darren Whitehouse, Shaojing Hu, Haiquan Fang, Michael C. Van Zandt
-
Publication number: 20090088577Abstract: Methods for the preparation of the high intensity sweetener, monatin, 3-(1-amino-1,3-dicarboxy-3-hydroxy-but-4-yl)indole, its salts and internal condensation products thereof, including methods applicable to the large-scale production of monatin are described.Type: ApplicationFiled: October 1, 2007Publication date: April 2, 2009Inventors: Subash Buddoo, Amanda Louise Rousseau, Gregory E.R. Gordon
-
Publication number: 20090088578Abstract: Imaging agents for magnetic resonance imaging are disclosed. Also disclosed are methods of non-invasively generating a visible image of a target tissue. In some embodiments, the discloses methods include the steps of (a) providing a contrast enhancement agent comprising a small molecule that binds to a biomolecule present in the target tissue; (b) introducing the contrast enhancement agent into the target tissue; and (c) scanning the target tissue using magnetic resonance imaging, whereby a visible image of the target tissue is non-invasively generated. Further discloses are methods for monitoring a response to a therapy, methods for selecting a therapy for a subject, methods for delineating a boundary between a diseased cell and a non-diseased cell in a tissue, and methods for assessing the degree to which a target tissue has been removed from a subject.Type: ApplicationFiled: January 22, 2008Publication date: April 2, 2009Inventors: Christopher D. Lascola, Allen W. Song, Timothy A. Haystead
-
Publication number: 20090082418Abstract: The present application describes deuterium-enriched fluvastatin, pharmaceutically acceptable salt forms thereof, and methods of treating using the same.Type: ApplicationFiled: August 22, 2008Publication date: March 26, 2009Applicant: PROTIA, LLCInventor: Anthony W. Czarnik
-
Publication number: 20090075938Abstract: There are disclosed compound of Formula (1): A1, A2, A3 and A4 which may be the same or different, represent N or CR1, X is a divalent group selected from O, S(O)n, C?W, NR4, NC(?O)R5 and CR6R7, W is O, S, NR20, Y is N or CR8, one of R4, R5, R6, R8, R9 and NR20 represents -L-R3, in which L is a single bond or a linker group, additionally, R1, R3-R9, which may be the same or different, independently represent hydrogen or a substituent and R20 represents hydrogen, hydroxyl, alkyl optionally substituted by aryl, alkoxy optionally substituted by aryl, aryl, CN, optionally substituted alkoxy, optionally substituted aryloxy, optionally substitute alkanoyl, optionally substituted aroyl, NO2, NR30R31, in which R30 and R31, which may be the same or different, represent hydrogen, optionally substituted alkyl or optionally substituted aryl; additionally, one of R30 and R31 may represent optionally substituted alkanoyl or optionally substituted aroyl, n represents an integer from 0 to 2, in addition, when an adjacent paiType: ApplicationFiled: February 9, 2007Publication date: March 19, 2009Inventors: Graham Michael Wynne, Stephen Paul Wren, Peter David Johnson, Paul Damien Price, Olivier De Moor, Gary Nugent, Richard Storer, Richard Joseph Pye, Colin Richard Dorgan
-
Publication number: 20090076271Abstract: The present invention relates to intermediates of rosuvastatin and processes for the production thereof.Type: ApplicationFiled: April 18, 2008Publication date: March 19, 2009Inventors: Vinod Kumar Kansal, Brijnath P. Chaurasia, Hitesh K. Patel, Vrajlal Gothalia, Hiren Gandhi
-
Patent number: 7473786Abstract: A copper(I)-catalyzed procedure for the synthesis of benzo[b]heterocycles. This protocol can be used to synthesize a variety of 2-arylbenzo[b]furans and indoles in good to excellent yields. This method can tolerate a variety of functional groups, does not require the use of expensive additives and is palladium-free.Type: GrantFiled: December 6, 2004Date of Patent: January 6, 2009Assignee: University of MassachusettsInventors: Dhandapani Venkataraman, Craig G. Bates, Pranorm Saejueng
-
Patent number: 7462640Abstract: The present invention refers to new sulfonamide derivatives, of general formula (Ia, Ib, Ic) optionally in form of one of their stereoisomers, preferably enantiomers or diastereomers, their racemate, or in form of a mixture of at least two of their stereoisomers, preferably enantiomers or diastereomers, at any mixing ratio or their salts, preferably the corresponding, physiologically acceptable salts, or corresponding solvates; to the process for their preparation, to their application as medicaments in human and/or veterinary therapeutics, and to the pharmaceutical compositions containing them.Type: GrantFiled: July 29, 2004Date of Patent: December 9, 2008Assignee: Laboratorios del Dr. Esteve S.A.Inventors: Ramon Merce Vidal, Xavier Codony Soler, Alberto Dordal Zueras
-
Publication number: 20080275224Abstract: The present invention relates to dyes of the general formula CAT+ Y? (I), where Y? is an anion selected from the group of the cyanoborates, fluoroalkylphosphates, fluoroalkylborates or imidates and CAT+ is a cation selected from the group of the azine, xanthene, polymethine, styryl, azo, tetrazolium, pyrylium, benzopyrylium, thiopyrylium, benzothiopyrylium, thiazine, oxazine, triarylmethane, diarylmethane, methine, acridine, quinoline, isoquinoline or quaternary azafluorenone dyes, for colouring plastics and plastic fibres, for the preparation of flexographic printing inks, as ball-point pen pastes, as stamp ink, for colouring leather and paper, for use in data acquisition systems, reprography, in ink microfilters, in photogalvanics, laser technology and the photo industry.Type: ApplicationFiled: July 22, 2004Publication date: November 6, 2008Inventors: Nikolai (Mykola) Ignatyev, Urs Weiz-Biermann, Helge Willner, Maik Finze, Eduard Bernhardt, Andriy Kucheryna
-
Publication number: 20080274907Abstract: A new class of pH sensitive fluorescent dyes and assays relating thereto are described. The dyes and assays are particularly suited for biological applications including phagocytosis and monitoring intracellular processes. The pH sensitive fluorescent dyes of the present invention include compounds of Formula I: wherein the variables are described throughout the application.Type: ApplicationFiled: October 29, 2007Publication date: November 6, 2008Applicant: INVITROGEN CORPORATIONInventors: Daniel Beacham, Jeffrey Dzubay, Kyle Gee, Vladimir Martin, Aleksey Rukavishnikov
-
Publication number: 20080275102Abstract: The invention relates to compounds of formula (I), wherein X, R1, R2, R3, R4 and R5 are as described herein. The invention also includes preparative methods for the preparation of compounds of formula (I). A method for the therapeutic use of the inventive compounds is also disclosed and claimed.Type: ApplicationFiled: May 14, 2008Publication date: November 6, 2008Applicant: SANOFI-AVENTISInventors: Francis BARTH, Claude VERNHET, Murielle RINALDI-CARMONA, Carole Elisabeth GUILLAUMONT-LEGEAY
-
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
-
Patent number: 7429612Abstract: The present invention provides an indoline compound represented by the formula (I) wherein each symbol is as defined in the DESCRIPTION, or a pharmaceutically acceptable salt thereof, and a pharmaceutical composition containing this indoline compound or a pharmaceutically acceptable salt thereof. The compound of the present invention shows superior ACAT inhibitory effect and superior lipoperoxidation inhibitory effect and is useful as an ACAT inhibitor or a lipoperoxidation inhibitor.Type: GrantFiled: July 16, 2003Date of Patent: September 30, 2008Assignee: Kyoto Pharmaceutical Industries, Ltd.Inventors: Shouji Kamiya, Miho Ikai, Kenji Takahash, Tadatsugu Tarumi, Masayasu Kasai, Akihisa Yoshimi, Hiroaki Shirahase
-
Publication number: 20080227684Abstract: The present invention relates to compositions for use in the modulation of PDZ domain interactions with cognate ligands. Methods of assessing and characterizing PDZ domain interactions from various polypeptides also are provided.Type: ApplicationFiled: December 29, 2006Publication date: September 18, 2008Inventors: MICHAEL P. BELMARES, Peter S. Lu, Kenneth A. Mendoza
-
Publication number: 20080221322Abstract: The present invention relates to chemical processes for the manufacture of certain quinazoline derivatives, or pharmaceutically acceptable salts thereof. The invention also relates to processes for the manufacture of certain intermediates useful in the manufacture of the quinazoline derivatives and to processes for the manufacture of the quinazoline derivatives utilising said intermediates. In particular, the present invention relates to chemical processes and intermediates useful in the manufacture of the compound 4-(4-fluoro-2-methylindol-5-yloxy)-6-methoxy-7-(3-pyrrolidin-1-ylpropoxy)quinazoline.Type: ApplicationFiled: October 31, 2007Publication date: September 11, 2008Applicant: AstraZeneca ABInventors: Euan Alexander Arnott, John Crosby, Mathew Charles Evans, James Gair Ford, Martin Francis Jones, Kevin William Leslie, Ian Michael McFarlane, George Joseph Sependa
-
Publication number: 20080153875Abstract: The invention relates to novel indole derivatives of the general formula 1, to their preparation and to their use as medicaments, in particular for treating tumors.Type: ApplicationFiled: March 6, 2008Publication date: June 26, 2008Applicant: AEterna Zentaris GmbHInventors: Peter Emig, Gerald Bacher, Dietmar Reichert, Silke Basner, Beate Aue, Bernd Nickel, Eckhard Gunther
-
Publication number: 20080139637Abstract: The present invention discloses a method for forming indole-based compounds, wherein the method comprises a reaction of ?,?-unsaturated ketone or aldehyde with indole or its derivative in the presence of at least one kind of Lewis acid. The Lewis acid comprises one of the following groups: metal halides, halogens, inorganic ammonia salts, organic sulfonate and sulfonic acid. Furthermore, this invention discloses 3-indole based compounds applied as anticancer agents.Type: ApplicationFiled: December 6, 2006Publication date: June 12, 2008Applicant: NATIONAL TAIWAN NORMAL UNIVERSITYInventors: Ching-Fa Yao, Yi-Ching Wang
-
Patent number: 7384973Abstract: The subject invention provides novel HMG-CoA-reductase inhibitors. In a preferred embodiment, the HMG-CoA reductase inhibitors of the subject invention can be deactivated to a primary inactive metabolite by hydrolytic enzymes. Compounds of the present invention can be advantageously used to treat patients suffering hypercholesterolemia.Type: GrantFiled: September 6, 2005Date of Patent: June 10, 2008Assignee: ARYx Therapeutics, Inc.Inventors: Pascal Druzgala, Xiaoming Zhang, Jurg R. Pfister
-
Patent number: 7381739Abstract: The present invention provides a compound of the formula: a pharmaceutically acceptable salt or a prodrug thereof, where R1, R2, R3, R4, p and n are those defined herein. The present invention also provides compositions comprising, methods for using, and methods for preparing Compound of Formula I.Type: GrantFiled: September 16, 2003Date of Patent: June 3, 2008Assignee: Roche Palo Alto LLCInventors: Ann Marie Madera, Robert James Weikert
-
Publication number: 20080124577Abstract: A novel organic compound and a high-performance organic light-emitting element containing the same. The organic light-emitting element contains a novel compound having a fluoranthene structure.Type: ApplicationFiled: April 18, 2007Publication date: May 29, 2008Applicant: CANON KABUSHIKI KAISHAInventors: Akihito Saitoh, Keiji Okinaka, Satoshi Igawa, Naoki Yamada, Chika Negishi, Takao Takiguchi, Shinjiro Okada
-
Patent number: 7375118Abstract: The present invention is directed to small molecule inhibitors of the IgE response to allergens, which are useful in the treatment of allergy and/or asthma or any diseases where IgE is pathogenic. This invention also relates to phenyl-indole molecules that are cellular proliferation inhibitors and thus are useful as anticancer agents. This invention further relates to small molecules which suppress cytokines and leukocytes.Type: GrantFiled: September 12, 2003Date of Patent: May 20, 2008Assignee: Avanir PharmaceuticalsInventors: Jagadish C. Sircar, Jailall Ramnauth, Mark L. Richards
-
Patent number: 7371865Abstract: The invention relates to a process for the manufacture of a compound of formula or a salt, especially a pharmaceutically acceptable salt with a base, thereof or a lactone thereof wherein the element represents —CH2—CH2— or —CH?CH— and R represents a cyclic residue.Type: GrantFiled: January 30, 2003Date of Patent: May 13, 2008Assignee: Novartis Pharmaceuticals CorporationInventors: Murat Acemoglu, Bernhard Riss