Polycyclo Ring System Which Includes Ring Chalcogen Patents (Class 548/525)
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Patent number: 8217032Abstract: The present invention relates to a selective estrogen receptor modulator of formula I or Ia: (I) (Ia); or a pharmaceutical acid addition salt thereof; useful for treating vasomotor symptoms, in particular hot flashes, night sweats and other symptoms that affect women around menopause.Type: GrantFiled: June 23, 2011Date of Patent: July 10, 2012Assignee: Eli Lilly and CompanyInventors: Robert Dean Dally, Jeffrey Alan Dodge, Scott Alan Frank, Ronald Jay Hinklin, Timothy Alan Shepherd, Owen Brendan Wallace
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Publication number: 20120149732Abstract: In accordance with the present invention, novel multifunctional compounds have been developed which have orthogonal reactive groups thereon, thereby facilitating preparation of compounds having multiple functional properties (e.g., a targeting moiety and a biologically active moiety). Such constructs are useful for a variety of applications, e.g., for the delivery of biologically compatible materials, and release thereof in active form. Therefore, in accordance with the present invention, there are provided multifunctional linkers of defined structure, as well as various derivatives thereof bearing one or more biologically active components thereon. Also provided in accordance with the present invention are methods for the preparation of such constructs, as well as various uses thereof.Type: ApplicationFiled: August 22, 2011Publication date: June 14, 2012Inventors: Alexander Chucholowski, Alisher Khasanov, Gregory Parker, Tong Zhu
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Publication number: 20120101103Abstract: Compounds of Formula I: (I) in which A, A1, R1, R7a, R7b, R8 and R10 have the meanings given in the specification, are DP2 receptor inhibitors useful in the treatment of useful in the treatment and prevention of immunologic diseases, allergic diseases such as asthma, allergic rhinitis and atopic dermatitis, and other inflammatory diseases mediated by prostaglandin D2 (PGD2). The compounds of Formula I may also be useful in treating diseases or medical conditions involving the Th2 T cell via production of IL-4, IL-5 and/or IL-13.Type: ApplicationFiled: December 18, 2009Publication date: April 26, 2012Applicant: ARRAY BIOPHARMA INC.Inventors: Adam Cook, Kevin W. Hunt, Robert Kirk Delisle, Todd Romoff, Christopher T. Clark, Ganghyeok Kim, Christopher P. Corrette, George A. Doherty, Laurence E. Burgess
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Publication number: 20120088809Abstract: This invention provides new 1-(2-alkyl-2,3-dihydro-benzofuran-4-yl)-pyrrolidin-3-ylamine acyl compounds, their use for the treatment or prevention of melatoninergic disorders and its compositions.Type: ApplicationFiled: June 10, 2010Publication date: April 12, 2012Inventors: Josep Lluís Falcó, Albert Palomer
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Patent number: 8153797Abstract: This invention relates to novel 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: February 13, 2007Date of Patent: April 10, 2012Assignee: Neurosearch A/SInventors: Dan Peters, John Paul Redrobe, Elsebet Østergaard Nielsen
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Patent number: 8153682Abstract: Disclosed are compounds, compositions and methods for treating various diseases, syndromes, conditions and disorders, including pain. Such compounds are represented by Formula I as follows: wherein A, B, G, Y, R1, R2, R3, and R4 are defined herein.Type: GrantFiled: July 18, 2008Date of Patent: April 10, 2012Assignee: Janssen Pharmaceutica, NVInventors: Shawn T. Branum, Raymond W. Colburn, Scott L. Dax, Christopher M. Flores, Michele C. Jetter, Yi Liu, Donald Ludovici, Mark J. Macielag, Jay M. Matthews, James J. McNally, Laura M. Reaney, Ronald K. Russell, Ning Qin, Christopher Teleha, Kenneth M. Wells, Scott C. Youells, Mark A. Youngman
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Publication number: 20120083488Abstract: A compound represented by the general Formula (I) below, or a salt or solvate thereof, which is useful as an ALK inhibitor, and is useful for prophylaxis or treatment of a disease accompanied by abnormality in ALK, for example, cancer, cancer metastasis, depression or cognitive function disorder: (meanings of the symbols that are included in the formula are as given in the specification).Type: ApplicationFiled: June 9, 2010Publication date: April 5, 2012Inventors: Kazutomo Kinoshita, Kohsuke Asoh, Noriyuki Furuichi, Toshiya Ito, Hatsuo Kawada, Nobuya Ishii, Hiroshi Sakamoto, WooSang Hong, MinJeong Park, Yoshiyuki Ono, Yashuharu Kato, Kenji Morikami, Takashi Emura, Nobuhiro Oikawa
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Patent number: 8148422Abstract: Disclosed are compounds, compositions and methods for treating various diseases, syndromes, conditions and disorders, including pain. Such compounds are represented by Formula (I) and Formula (II) as follows: wherein Y, R1, R2, R3, R4, RA, and RB are defined herein.Type: GrantFiled: December 15, 2009Date of Patent: April 3, 2012Assignee: Janssen Pharmaceutica, NVInventors: Mark J. Macielag, James J. McNally
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Publication number: 20120077989Abstract: The present invention relates to a use of a cyclic imidate as a ligand for catalysis in which the ligand contains sub-structure (Y) as a minimal structural motive, wherein the carbon atoms and the nitrogen atom can be optionally substituted by a chemical substituent.Type: ApplicationFiled: April 6, 2010Publication date: March 29, 2012Inventors: Timothy Noël, Koen Vandyck, Johan Van Der Eycken
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Publication number: 20120077986Abstract: The present invention is directed to provide a novel preparation of anticancer-active tricyclic compounds via alkyne coupling reaction. The present invention provides a process for preparing a compound of formula (Ia) or (Ib): wherein R1 is optionally substituted C1-6 alkyl, etc.; W is O, S or NR2; R2 is hydrogen atom, etc., which comprises Step (a) in which a compound of formula (II): wherein R1 is the same as defined above, and a compound of formula (III) or (IV): wherein R2 is the same as defined above; R3 is hydrogen atom, etc.; X is halogen atom, etc., are reacted in the presence of a base, a copper catalyst and a palladium catalyst in an aprotic polar solvent.Type: ApplicationFiled: July 26, 2011Publication date: March 29, 2012Applicant: TAHEEBO JAPAN CO., LTD.Inventors: Akira IIDA, Kazunori UEDA, Mitsuaki YAMASHITA
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Patent number: 8129535Abstract: An alkyl ether derivative represented by the general formula: wherein each of R1 and R2 represents one or more groups selected from a hydrogen atom, a halogen atom, an alkyl group, an aryl group, an aralkyl group, an alkoxy group, an aryloxy group, an alkylthio group, an arylthio group, an alkenyl group, an alkenyloxy group, an amino group, an alkylsulfonyl group, an arylsulfonyl group, a carbamoyl group, a heterocyclic group, a hydroxyl group, a carboxyl group, a nitro group, an oxo group and the like; R3 is an alkylamino group, an amino group, a hydroxyl group or the like; the ring A is a 5-membered or 6-membered heteroaromatic ring or a benzene ring; each of m and n is an integer of 1 to 6; and p is an integer of 1 to 3, or its salt has activity to protect neurons, activity to accelerate nerve regeneration and activity to accelerate neurite extension and hence is useful as a therapeutic agent for diseases in central and peripheral nerves.Type: GrantFiled: October 17, 2008Date of Patent: March 6, 2012Assignee: Toyama Chemical Co., Ltd.Inventors: Akihito Saitoh, Noboru Iwakami, Tamotsu Takamatsu
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Publication number: 20120046334Abstract: The present invention relates to a combination for the treatment of cancer wherein the combination exhibits a synergistic effect. The combination comprises radiation and at least one cyclin dependent kinase (CDK) inhibitor selected from the compounds of formula I or a pharmaceutically acceptable salt or a solvate thereof. The present invention also relates to a method for the treatment of cancer, which method comprises administering to a patient in need of such a treatment, a therapeutically effective amount of the combination. The present invention also relates to the use of a CDK inhibitor selected from the compounds of formula I as a radiosensitizer that enhances the efficacy of radiotherapy for the treatment of cancer, particularly head and neck cancer.Type: ApplicationFiled: May 3, 2010Publication date: February 23, 2012Inventors: Maggie Joyce Rathos, Kalpana Sanjay Joshi, Nikhil Krishnamurthy Hebbar, Somesh Sharma
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Publication number: 20120035170Abstract: This invention concerns novel substituted unsaturated tetracyclic tetrahydrofuran derivatives with binding affinities towards serotonine receptors, in particular 5-HT2A and 5-HT2C receptors, and towards dopamine receptors, in particular dopamine D2 receptors and with norepinephrine reuptake inhibition properties, pharmaceutical compositions comprising the compounds according to the invention, the use thereof as a medicine, in particular for the prevention and/or treatment of a range of psychiatric and neurological disorders, in particular certain psychotic, cardiovascular and gastrokinetic disorders and processes for their production. The compounds according to the invention can be represented by general Formula (I) and comprises also the pharmaceutically acceptable acid or base addition salts thereof, the stereochemically isomeric forms thereof, the N-oxide form thereof and prodrugs thereof, wherein all substituents are defined as in claim 1.Type: ApplicationFiled: August 22, 2011Publication date: February 9, 2012Inventors: José Maria Núñez, Antonius Adrianus Hendrikus Petrus Megens, Andrés Avelino Trabanco-Suárez
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Publication number: 20120003270Abstract: The present invention relates to 6-substituted isoflavonoid compounds and compositions comprising same. The invention further relates to the use of 6-substituted isoflavonoid compounds for the treatment of various diseases and conditions.Type: ApplicationFiled: July 30, 2009Publication date: January 5, 2012Inventors: Alan James Husband, Michael James, Naresh Kumar
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Publication number: 20120004255Abstract: The present invention relates to conjugate comprising a carrier substituted with one or more occurrences of a moiety having the structure: wherein each occurrence of M is independently a modifier having a molecular weight ?10 kDa; denotes direct of indirect attachment of M to linker LM; and each occurrence of LM is independently an optionally substituted succinamide-containing linker, whereby the modifier M is directly or indirectly attached to the succinamide linker through an amide bond, and the carrier is linked directly or indirectly to each occurrence of the succinamide linker through an ester bond. In another aspect, the invention provides compositions comprising the conjugates, methods for their preparation, and methods of use thereof in the treatment of various disorder, including, but not limited to cancer.Type: ApplicationFiled: June 3, 2011Publication date: January 5, 2012Applicant: THE GENERAL HOSPITAL CORPORATIONInventors: Mikhail I. Papisov, Alexander Yurkovetskiy
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Publication number: 20110318772Abstract: Chemically reactive 7-hydroxycoumarin derivatives and their application for analyzing cell function, for example in combination with additional fluorescent labels. The coumarin derivatives exhibit a strong absorption at 405 nm and high fluorescence quantum yields.Type: ApplicationFiled: June 23, 2010Publication date: December 29, 2011Applicant: AAT BIOQUEST, INC.Inventors: Zhenjun DIWU, Chunmei WEI, Qinglin MENG, Haitao GUO, Jingfang LIAO
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Patent number: 8084612Abstract: The invention relates to compounds of Formulae I(a) to XI and pharmaceutically acceptable salts and solvates thereof (Proline Analog Compounds), that are useful, e.g., as ligands for cannabinoid receptors, as compositions comprising a Proline Analog Compound and a pharmaceutically acceptable carrier, in methods of making such Proline Analog Compounds, and in methods for treating or preventing a Condition, such as pain, nausea, vomiting and an eating disorder, comprising administering an effective amount of a Proline Analog Compound to an animal in need thereof.Type: GrantFiled: January 8, 2009Date of Patent: December 27, 2011Assignee: Purdue Pharma L.P.Inventors: Bin Shao, Jiangchao Yao
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Publication number: 20110294827Abstract: IAP binding molecules and compositions including these are disclosed. The IAP binding molecules interact with IAPs (inhibitor of apoptosis proteins) in cells and may be used to modify apoptosis in cells treated with such molecules. Embodiments of these compounds have a Kd of less that 0.1 micromolar. Methods of using these IAP binding molecules for therapeutic, diagnostic, and assay purposes are also disclosed.Type: ApplicationFiled: June 3, 2011Publication date: December 1, 2011Applicant: TETRALOGIC PHARMACEUTICALS CORPORATIONInventors: Stephen M. Condon, Matthew G. LaPorte, Yijun Deng, Susan R. Rippin
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Patent number: 8058454Abstract: A process for preparing substituted pyrrolidine compounds, including (5)-2-{1-[2-(2,3-dihydrobenzofuran-5-yl)ethyl]-3-pyrrolidinyl}-2,2-diphenylacetamide hydrobromide, commonly known in the art as darifenacin, comprising reacting a pyrrolidine compound with a benzofuran derivative in the presence of a phase-transfer catalyst.Type: GrantFiled: September 7, 2007Date of Patent: November 15, 2011Assignee: Medichem, S.A.Inventors: Núria Soldevilla Madrid, Ernesto Durán López, Jordi Puig Serrano
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Publication number: 20110275673Abstract: The invention relates to compounds of Formula (I). Compounds of the present invention are inhibitors of sphingosine kinase 3, and are useful in the treatment of various disorders and conditions, such as inflammatory disorders.Type: ApplicationFiled: September 17, 2009Publication date: November 10, 2011Inventors: Yibin Xiang, Bradford Hirth, John L. Kane, Junkai Liao, Kevin Noson, Christopher Yee
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Publication number: 20110263672Abstract: Novel metabolites of wortmannin and wortmannin analogs and their use in inhibiting PI-3 kinase activity in mammals and the treatment and prevention of cancer or tumor formation in a subject are described herein.Type: ApplicationFiled: June 10, 2011Publication date: October 27, 2011Applicant: Arizona Board of Regents on behalf of the University of ArizonaInventor: Garth Powis
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Publication number: 20110257164Abstract: Described are novel compounds of the Formula (I), their derivatives, analogs, tautomeric forms, regioisomers, stereoisomers, polymorphs, solvates, intermediates, pharmaceutically acceptable salts, pharmaceutical compositions, metabolites and prodrugs thereof. These compounds are effective in lowering blood glucose, serum insulin, free fatty acids, cholesterol, triglyceride levels; treatment of obesity, inflammation, autoimmune diseases such as multiple sclerosis, rheumatoid arthritis; treatment and/or prophylaxis of type II diabetes. These compounds are more particularly dipeptidyl peptidase (DPP IV) inhibitors.Type: ApplicationFiled: January 7, 2010Publication date: October 20, 2011Applicant: ORCHID RESEARCH LABORATORIES LIMITEDInventors: Gopalan Balasubramanian, Sukumar Sakamuri, Gajendra Singh, Sivanesan Dharmalingam, Franklin Pooppady Xavier, Shridhar Narayanan, Jeyamurugan Mookkan, Jeganatha Sivakumar Balasubramanian, Agneeswari Rajalingam, Jayanarayan Kulathingal
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Publication number: 20110257174Abstract: Provided herein are novel sirtuin-modulating compounds and methods of use thereof. The sirtuin-modulating compounds may be used for increasing the lifespan of a cell, and treating and/or preventing a wide variety of diseases and disorders including, for example, diseases or disorders related to aging or stress, diabetes, obesity, neurodegenerative diseases, cardiovascular disease, blood clotting disorders, inflammation, cancer, and/or flushing as well as diseases or disorders that would benefit from increased mitochondrial activity. Also provided are compositions comprising a sirtuin-modulating compound in combination with another therapeutic agent.Type: ApplicationFiled: September 29, 2009Publication date: October 20, 2011Applicant: Sirtris Pharmaceuticals, Inc.Inventors: Christopher Oalmann, Robert B. Perni, Chi B. Vu
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Patent number: 8039489Abstract: The invention provides compounds of formula I: or a pharmaceutically acceptable salt thereof, wherein R1-3, R5-7, a, X, Y, Y?, Y?, and Z 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: GrantFiled: April 28, 2011Date of Patent: October 18, 2011Assignee: Theravance, Inc.Inventors: YuHua Ji, Craig Husfeld, YongQi Mu, Rick Lee, Li Li
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Publication number: 20110245244Abstract: Novel compounds of the general formula (I), the use of these compounds as pharmaceutical compositions, pharmaceutical compositions comprising the compounds and methods of treatment employing these compounds and compositions. The present compounds are activators of PPAR? and should be useful for treating conditions mediated by the same.Type: ApplicationFiled: April 4, 2011Publication date: October 6, 2011Applicant: HIGH POINT PHARMACEUTICALS, LLCInventors: Per Sauerberg, Pavel Pihera, Zdenek Polivka, Miroslav Havranek, Ingrid Pettersson, John Patrick Mogensen
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Publication number: 20110230463Abstract: [Object] Provided is a compound which has an excellent S1P1 agonist action, and is useful particularly as an active ingredient for an agent for preventing and/or treating a disease induced by undesirable lymphocyte infiltration or a disease induced by abnormal proliferation or accumulation of cells. [Means for Solution] According to the present invention, a 2H-chromene compound or a derivative thereof which has an excellent S1P1 agonist action, and is useful particularly as an active ingredient of an agent for preventing and/or treating a disease induced by undesirable lymphocyte infiltration or a disease induced by abnormal proliferation or accumulation of cells can be provided. The 2H-chromene compound and a derivative thereof which are the compounds of the present invention have an S1P1 agonist action, and can be used particularly for prevention and/or treatment of a disease induced by undesirable lymphocyte infiltration or a disease induced by abnormal proliferation or accumulation of cells.Type: ApplicationFiled: December 4, 2009Publication date: September 22, 2011Applicant: ASTELLAS PHARMA INC.Inventors: Hironori Harada, Kazuyuki Hattori, Kazuya Fujita, Sunao Imada, Tatsuaki Morokata
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Publication number: 20110226610Abstract: Inventors have developed a chromophore (nitrodibenzylfuranyl, or NBDF) for ultra efficient uncaging of a caged substrate (e.g., an organic molecule such as, for example, an amino acid, a biological molecules, such as, for example, second messengers inside cells). Photolysis of a NBDF derivative of EGTA (i.e. caged calcium) is about 50 times more efficient than others calcium cages (the quantum yield of photolysis is 0.6 and the extinction coefficient is 18,400. NDBF-EGTA has a 2-photon cross section of about 0.3-0.6 GM).Type: ApplicationFiled: February 18, 2011Publication date: September 22, 2011Applicant: Philadelphia Health & Education Corporation d/b/a Drexel University College of MedicineInventors: Graham Ellis-Davies, Atsuya Momotake
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Patent number: 8022203Abstract: New aminoalkoxyimino derivatives at position 3 of substituted B-homoandrostanes and B-heteroandrostanes, processes for their preparation, and to pharmaceutical compositions containing them for the treatment of cardiovascular disorders, such as heart failure and hypertension. In particular compounds having the general formula (I) are described, where the radicals have the meanings described in detail in the application.Type: GrantFiled: May 31, 2007Date of Patent: September 20, 2011Assignee: Sigma-Tau Industrie Farmaceutiche Riunite S.p.A.Inventors: Alberto Cerri, Barbara Moro, Maco Torri, Giulio Carzana, Giuseppe Bianchi, Mara Ferrandi, Patrizia Ferrari, Maria Pia Zappavigna, Leonardo Banfi, Giuseppe Giacalone
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Publication number: 20110223677Abstract: The present invention relates to carboxamide-substituted dyes, the production and use of such dyes as labeling groups in analytics.Type: ApplicationFiled: March 18, 2011Publication date: September 15, 2011Applicant: ATTO-TEC GmbHInventors: Jutta Arden-Jacob, Karl-Heinz Drexhage, Monika Hamers-Schneider, Norbert Këmnitzer, Alexander Zilles
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Publication number: 20110217335Abstract: Disclosed are macrocyclic compounds of formulae I, I?, II, II?, III, III?, IV, and V, which are analogs of the pochonin resorcylic acid lactones, pharmaceutical compositions comprising the compounds, and methods and uses comprising the compounds for the treatment of diseases mediated by kinases and Heat Shock Protein 90 HSP90.Type: ApplicationFiled: January 15, 2009Publication date: September 8, 2011Applicant: UNIVERSITE DE STRASBOURGInventors: Nicolas Winssinger, Sofia Barluenga, Martin Karplus
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Publication number: 20110212940Abstract: The present invention relates to compounds of the general formula (I) that have activity as S1P receptor modulating agents and the use of such compounds to treat diseases associated with inappropriate S1P receptor activity. The compounds may be used as immunomodulators, e.g., for treating or preventing diseases such as autoimmune and related immune disorders including systemic lupus erythematosus, inflammatory bowel diseases such as Crohn's disease and ulcerative colitis, type I diabetes, uveitis, psoriasis, myasthenia gravis, rheumatoid arthritis, non-glomerular nephrosis, hepatitis, Behçet's disease, glomerulonephritis, chronic thrombocytopenic purpura, hemolytic anemia, hepatitis and Wegner's granuloma; and for treating other conditions.Type: ApplicationFiled: February 25, 2011Publication date: September 1, 2011Applicant: EPIX PHARMACEUTICALS, INC.Inventors: Roland Burli, Victor J. Cee, Jennifer Golden, Brian Alan Lanman, Susana Neira, Ashis Saha, Nili Schutz, Xiang Yu, Dilara McCauley, Mercedes Lobera, Yael Marantz, Jian Lin, Srinivasa R. Cheruku, Pini Orbach, Anurag Sharadendu, Robert C. Penland, Kimberley Gannon, Sharon Shacham, Silvia Noiman, Oren Becker, Zhaoda Zhang
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Publication number: 20110212955Abstract: The present invention relates to a new class of rosamine derivatives, in one embodiment, the compounds have the structure (I) or any pharmaceutically acceptable salt or solvate thereof, wherein: R1 represents aryl, Het1 or C1-6 alkyl, which latter group is optionally substituted by aryl or Het2; R2a and R2b together form C3.8 n-alkylene, which alkylene group is optionally substituted by one or more substituents selected from halo, C1-4 alkyl, C(O)OH and C(O)O—C1-4, alkyl and which alkylene group is optionally interrupted by X1; R3a and R3b together form C3-6 /7-alkylene, which alkylene group is optionally substituted by one or more substituents selected from halo.Type: ApplicationFiled: July 2, 2009Publication date: September 1, 2011Applicant: CANCER RESEARCH INITIATIVES FOUNDATIONInventors: Hong Boon Lee, Kevin Burgess, Siang Hui Lim, Liangxing Wu
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Publication number: 20110172225Abstract: Novel derivatives of enfumafungin are disclosed herein, along with their, pharmaceutically acceptable salts, hydrates and prodrugs. Also disclosed are compositions comprising such compounds, methods of preparing such compounds and methods of using such compounds as antifungal agents and/or inhibitors of (1,3)-?-D-glucan synthase. The disclosed compounds, their pharmaceutically acceptable salts, hydrates and prodrugs, as well as compositions comprising such compounds, salts, hydrates and prodrugs, are useful for treating and/or preventing fungal infections and associated diseases and conditions.Type: ApplicationFiled: September 25, 2008Publication date: July 14, 2011Applicants: Merck Sharp & Dohme Corp., Scynexis, Inc.Inventors: James M. Balkovec, Phieng Siliphaivanh, Frances A. Bouffard, Roland A. Bouffard, Michael R. Peel, Weiming Fan, Ahmed Mamai, Sarah Dimick Gray
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Publication number: 20110166142Abstract: 2-Substituted isoflavonoid compounds and pharmaceutical compositions containing same are useful as anti-inflammatory agents and antioxidants and for the treatment of related diseases and conditions.Type: ApplicationFiled: June 30, 2008Publication date: July 7, 2011Inventors: Eleanor Eiffe, Andrew Heaton, Catherine Walker, Alan James Husband
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Patent number: 7973030Abstract: A pharmaceutical useful as a therapeutic agent and a preventive agent for hyperlipemia, and a pharmaceutical useful as a therapeutic agent and a preventive agent for hepatic disorders associated with cholestasis, particularly, primary biliary cirrhosis and primary sclerosing cholangitis, and a pharmaceutical useful as a therapeutic agent and a preventive agent for obesity, fatty liver and steatohepatitis are provided.Type: GrantFiled: February 25, 2005Date of Patent: July 5, 2011Assignee: Asahi Kasei Pharma CorporationInventors: Takehiko Sasahara, Mitsunobu Mohri, Ken-Ichi Kasahara
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Publication number: 20110152234Abstract: The invention relates to thiophene carboxamides of formula (I), wherein A, R1, R2, R3, n and X are as defined in the specification, processes and intermediates used in their preparation, pharmaceutical compositions containing them and their use in therapy.Type: ApplicationFiled: December 23, 2010Publication date: June 23, 2011Inventors: Alan Faull, Craig Johnstone, Andrew Morley, Jeffrey Philip Poyser
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Publication number: 20110144096Abstract: Novel compounds and methods for activating the TrkB receptor are provided. The methods include administering in vivo or in vitro a therapeutically effective amount of a compound containing four six-membered rings and a substituted or unsubstituted C5 or C6 heteroaryl or hetero-cycloalkyl ring and pharmaceutically acceptable salts, prodrugs, and derivatives thereof. Specifically, methods and compounds for the treatment of disorders including neurologic, neuropsychiatric, and metabolic disorders are provided. For example, a method is provided of treating or reducing the risk of depression, anxiety, or obesity in a subject, which includes selecting a subject with or at risk of developing depression, anxiety, or obesity, and administering to the subject a therapeutically effective amount of the described compounds.Type: ApplicationFiled: July 28, 2009Publication date: June 16, 2011Applicant: EMORY UNIVERSITYInventor: Keqiang Ye
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Patent number: 7960385Abstract: The invention provides compounds of formula I: or a pharmaceutically acceptable salt thereof, wherein R1-3, R5-7, a, X, Y, Y?, Y?, and Z 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: GrantFiled: September 5, 2008Date of Patent: June 14, 2011Assignee: Theravance, Inc.Inventors: YuHua Ji, Craig Husfeld, YongQi Mu, Rick Lee, Li Li
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Publication number: 20110136794Abstract: A compound represented by the following formula (1) or a salt thereof: The compound has an inhibitory activity on the production of interleukin-6, and is therefore useful as a preventive and/or therapeutic agent for a disease associated with interleukin-6, ocular inflammatory diseases and the like. In the formula, R1 represents a halogen atom, a hydrogen atom, a lower alkyl group which may have a substituent, a formyl group, or a lower alkylcarbonyl group which may have a substituent, R2 represents a bicyclic hydrocarbon group which may have a substituent or a bicyclic heterocyclic group which may have a substituent, R3 represents a hydrogen atom, a lower alkyl group which may have a substituent, an aryl group which may have a substituent, or an acyl group.Type: ApplicationFiled: August 25, 2009Publication date: June 9, 2011Inventors: Kenji Kawashima, Noriko Kawashima, Hiroshi Enomoto, Minoru Yamamoto, Massaaki Murai
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Patent number: 7951822Abstract: The object is to provide a novel LXR? agonist that is useful as a preventative and/or therapeutic agent for atherosclerosis; arteriosclerosis such as those resulting from diabetes; dyslipidemia; hypercholesterolemia; lipid-related diseases; inflammatory diseases that are caused by inflammatory cytokines; skin diseases such as allergic skin diseases; diabetes; or Alzheimer's disease. The solving means is a 1,3-dihydroisobenzofuran derivative represented by the following general formula (1) or salt thereof, or their solvate.Type: GrantFiled: March 30, 2009Date of Patent: May 31, 2011Assignee: Kowa Company, Ltd.Inventors: Ayumu Okuda, Takayuki Matsuda, Toru Miura, Koichi Yamazaki, Yuki Yamaguchi, Minoru Koura, Sayaka Kurobuchi, Yuichiro Watanabe, Kimiyuki Shibuya
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Publication number: 20110122475Abstract: A naphthopyran compound represented by the formulae (I) to (II) wherein:—mi, Hi2, p, q are each an integer comprised from O to 4 or 5 inclusive;—Ri, R2 and R4, represent a group selected from halogen, H, —Ra, aryl, —OH, —ORa, —SH, —SRa, —NH2, —NR8RaI, —NRbRc, —NRaI-CORa, —NRaiCO(aryl), —NRai aryl, —N-aryfe, —N(aryl)CO(aryl), —CO—R3, —CO2R3I, —OC(O)—Rd, and —X—(Re)—Y, and linear or branched (Ci-Ci8) perfluoroalkyl group, wherein R3, RaI, Rb, Rc, X, Y, Re, Rd are as defined into the description;—Zi re resent a group selected from: (formules)Type: ApplicationFiled: March 2, 2009Publication date: May 26, 2011Applicant: Essilor International (compagnie Generale D'optique)Inventors: Stuart Aiken, Christopher David Gabbutt, Bernard Mark Heron, Christopher Stephen Kershaw, Nicola Jane Smith, Jean-Paul Cano
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Publication number: 20110105463Abstract: Compounds of Formula (I): in which A1, A2, W, L, G, R7a, R7b, R8, R9 and R10 have the meanings given in the specification, are DP2 receptor modulators useful in the treatment of immunologic diseases.Type: ApplicationFiled: June 24, 2009Publication date: May 5, 2011Applicant: ARRAY BIOPHARMA INC.Inventors: Laurence E. Burgess, Christopher T. Clark, Adam Cook, Christopher P. Corrette, Robert Kirk DeLisle, George A. Doherty, Kevin W. Hunt, Todd T. Romoff
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Publication number: 20110092700Abstract: The present invention provides a compound represented by general formula (1) below or a pharmaceutically acceptable salt thereof: wherein: X is selected from heteroaryl etc., Y1 and Y2 are selected from —N? etc., Y3 and Y4 are selected from —CH? etc., A is selected from sulfamide etc., R1 is selected from hydrogen etc., and R2 is selected from C1-6 alkyl etc. The compound or salt has sufficiently high antitumor activity, and is useful in the treatment of cell proliferative disorders, particularly cancers. The present invention also provides a pharmaceutical composition containing the compound or salt as an active ingredient.Type: ApplicationFiled: December 3, 2010Publication date: April 21, 2011Inventors: Hitoshi Iikura, Ikumi Hyoudoh, Toshihiro Aoki, Noriyuki Furuichi, Masayuki Matsushita, Fumio Watanabe, Sawako Ozawa, Masahiro Sakaitani, Pil-Su Ho, Yasushi Tomii, Kenji Takanashi, Naoki Harada
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Patent number: 7923558Abstract: The invention relates to a method for obtaining pure tetrahydrocannabinol from reaction mixtures containing tetrahydrocannabinol compounds or from raw products containing tetrahydrocannabinol compounds. According to said method, the tetrahydrocannabinol compounds in the reaction mixture or in the raw product are converted into crystallisable derivatives, preferably using a suitable solvent, said derivatives are then crystallised and isolated, and the pure tetrahydrocannabinol compounds are then obtained from the crystallised derivatives. The invention also related to the use of compounds produced in this way for the production of a medicament for human therapy, and to the medicaments thus produced.Type: GrantFiled: July 19, 2004Date of Patent: April 12, 2011Assignee: Cilag Ltd.Inventors: Enver Arslantas, Ulrich Weigl
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Patent number: 7923562Abstract: Bifunctional linkers are provided that comprise a photocleavable moiety flanked by two different amine reactive moieties. In some embodiments the photocleavable moiety is a dimethoxynitrobenzyl moiety. In other embodiments the photocleavable moiety is 8-bromo-7-hydroxyquinoline. In other embodiments the photocleavable moiety is nitrodibenzofuran. In other embodiments the photocleavable moiety is 6-bromo-7-hydroxycoumarin-4-ylmethyl. The linkers find use in synthetic methods, including the generation of photocleavable oligonucleotides, e.g. caged morpholinos.Type: GrantFiled: June 16, 2009Date of Patent: April 12, 2011Assignee: The Board of Trustees of the Leland Stanford Junior UniversityInventors: James K. Chen, Surajit Sinha, Ilya Shestopalov, Xiaohu Ouyang
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Patent number: 7919509Abstract: To provide a novel LXR? agonist that is useful as a preventative and/or therapeutic agent for atherosclerosis; arteriosclerosis such as those resulting from diabetes; dyslipidemia; hypercholesterolemia; lipid-related diseases; inflammatory diseases that are caused by inflammatory cytokines; skin diseases such as allergic skin diseases; diabetes; or Alzheimer's disease. [Solving Means] A 2-oxochromene derivative represented by the following general formula (1) or salt thereof, or their solvate.Type: GrantFiled: February 27, 2009Date of Patent: April 5, 2011Assignee: Kowa Company, Ltd.Inventors: Ayumu Okuda, Takayuki Matsuda, Toru Miura, Hidefumi Ozawa, Ayako Tosaka, Koichi Yamazaki, Yuki Yamaguchi, Sayaka Kurobuchi, Yuichiro Watanabe, Kimiyuki Shibuya
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Patent number: 7915301Abstract: The present invention relates to novel compounds for the inhibition of cyclin-dependent kinases, and more particularly, to chromenone derivatives of formula (Ia), wherein R1, R2, R3, R4, R5, R6, R7 and A have the meanings indicated in the claims. The invention also relates to processes for the preparation of the compounds of formula (Ia), to methods of inhibiting cyclin-dependent kinases and of inhibiting cell proliferation, to the use of the compounds of formula (Ia) in the treatment and prophylaxis of diseases, which can be treated or prevented by the inhibition of cyclin-dependent kinases such as cancer, to the use of the compounds of formula (Ia) in the preparation of medicaments to be applied in such diseases.Type: GrantFiled: July 18, 2007Date of Patent: March 29, 2011Assignee: Piramal Life Science LimitedInventors: Bansi Lal, Kalpana Joshi, Sanjeev Kulkarni, Malcolm Mascarenhas, Shrikant Kamble, Maggie Joyce Rathos, Rajendrakumar Joshi
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Publication number: 20110054165Abstract: The invention provides a novel class of xanthene dyes, some of which are functionalized to allow their coupling to conjugation partners of interest, e.g. biomolecules, drugs, toxins and the like. Also provided are conjugates of the dyes, methods of preparing and using the dyes and their conjugates and kits including the dyes and their conjugates.Type: ApplicationFiled: November 8, 2010Publication date: March 3, 2011Applicant: BIOSEARCH TECHNOLOGIES, INC.Inventors: MARK REDDINGTON, MATT LYTTLE
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Publication number: 20110040103Abstract: The subject invention pertains to pentafluorosulfonyl (SF5) substituted pyrroles, thiophenes, 3-pyrrolines and 2,5-dihydrothiophenes, as well as methods for their synthesis.Type: ApplicationFiled: June 17, 2010Publication date: February 17, 2011Applicant: UNIVERSITY OF FLORIDA RESEARCH FOUNDATION, INC.Inventors: Zhaoyun Zheng, William R. Dolbier, JR.
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Patent number: 7884127Abstract: The present invention relates to novel compounds for the inhibition of cyclin-dependent kinases, and more particularly, to chromenone derivatives of formula (Ic) wherein R1, R2, R3, R4, R5, R6, R7 and A have the meanings indicated in the claims. The invention also relates to processes for the preparation of the compounds of formula (Ia), to methods of inhibiting cyclin-dependent kinases and of inhibiting cell proliferation, to the use of the compounds of formula (Ic) in the treatment and prophylaxis of diseases, which can be treated or prevented by the inhibition of cyclin-dependent kinases such as cancer, to the use of the compounds of formula (Ic) in the preparation of medicaments to be applied in such diseases.Type: GrantFiled: September 8, 2006Date of Patent: February 8, 2011Assignee: Pirimal Life Sciences Ltd.Inventors: Bansi Lal, Kalpana Joshi, Sanjeev Kulkarni, Malcolm Mascarenhas, Shrikant Kamble, Maggie Joyce Rathos, Rajendrakumar Joshi, Meenakshi Sivakumar