Nitrogen Attached Directly To The 1,3-thiazole Ring By Nonionic Bonding Patents (Class 546/270.7)
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Publication number: 20110281874Abstract: Provided are compounds that are useful in the treatment and/or prevention of diseases mediated by deficient levels of glucokinase activity, such as diabetes mellitus. Also provided are methods of treating or preventing diseases and disorders characterized by underactivity of glucokinase or which can be treated by activating glucokinase.Type: ApplicationFiled: July 27, 2011Publication date: November 17, 2011Applicant: ARRAY BIOPHARMA INC.Inventors: Thomas D. AICHER, Steven Armen BOYD, Mark Joseph CHICARELLI, Kevin Ronald CONDROSKI, Ronald Jay HINKLIN, Ajay SINGH
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Publication number: 20110263564Abstract: 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: October 29, 2009Publication date: October 27, 2011Applicant: Sirtris Pharmaceuticals, Inc.Inventors: Radha Narayan, Jeremy S. Disch, Robert B. Perni, Chi B. Vu
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Publication number: 20110257179Abstract: The present invention relates to novel compounds of Formula (I), wherein M, P, A and (B)n are defined as in Formula (I); invention compounds are modulators of metabotropic glutamate receptors—subtype 4 (“mGluR4”) which are useful for the treatment or prevention of central nervous system disorders as well as other disorders modulated by mGluR4 receptors. The invention is also directed to pharmaceutical compositions and the use of such compounds in the manufacture of medicaments, as well as to the use of such compounds for the prevention and treatment of such diseases in which mGluR4 is involved.Type: ApplicationFiled: January 12, 2010Publication date: October 20, 2011Inventor: Christelle Bolea
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Patent number: 8026367Abstract: The present invention relates to selected (R)-arylalkylamino derivatives of formula (I), in which R, R1 and Ar are as defined in the claims. These compounds show a surprising potent inhibitory effect on C5a induced human PMN chemotaxis. The compounds of the invention absolutely lack of CXCL8 inhibitory activity. Said compounds are useful in the treatment of pathologies depending on the chemotactic activation of neutrophils and monocytes induced by the fraction C5a of the complement. In particular, the compounds of the invention are useful in the treatment of sepsis, psoriasis, rheumatoid arthritis, ulcerative colitis, acute respiratory distress syndrome, idiopathic fibrosis, glomerulonephritis and in the prevention and treatment of injury caused by ischemia and reperfusion.Type: GrantFiled: November 24, 2006Date of Patent: September 27, 2011Assignee: Dompe PHA.R.MA S.p.A.Inventors: Marcello Allegretti, Alessio Moriconi, Andrea Aramini, Maria Candida Cesta, Andrea Beccari, Riccardo Bertini
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Publication number: 20110230477Abstract: The present invention is directed to novel compounds of formula (I) and their use in treating metabolic diseases.Type: ApplicationFiled: December 7, 2009Publication date: September 22, 2011Applicant: Euroscreen S.A.Inventors: Hamid Hoveyda, Cyrille Evangelos Brantis, Guillaume Dutheuil, Ludivine Zoute, Didier Schils, Jerome Bernard
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Publication number: 20110230486Abstract: Compounds, compositions, and methods for modulation of Hec1/Nek2 interaction are provided. Especially preferred compounds disrupt Nek2/Hec1 binding and are therefore useful as chemotherapeutic agent for neoplastic diseases.Type: ApplicationFiled: March 15, 2011Publication date: September 22, 2011Inventors: Johnson Lau, Jiann-Jyh Huang
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Patent number: 8022223Abstract: Provided are compounds of formula I that are useful in the treatment and/or prevention of diseases mediated by deficient levels of glucokinase activity, such as diabetes meilitus. Also provided are methods of treating or preventing diseases and disorders characterized by underactivity of glucokinase or which can be treated by activating glucokinase.Type: GrantFiled: March 23, 2007Date of Patent: September 20, 2011Assignee: Array Biopharma, Inc.Inventors: Thomas D. Aicher, Steven Armen Boyd, Mark Joseph Chicarelli, Kevin Ronald Condroski, Ronald Jay Hinklin, Ajay Singh
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Patent number: 8022222Abstract: Provided are compounds of formula I wherein R2, L, Z, Y, G and R1 are as defined herein, that are useful in the treatment and/or prevention of diseases or disorders mediated by deficient levels of glucokinase activity or which can be treated by activating glucokinase including, but not limited to, diabetes mellitus, impaired glucose tolerance, IFG (impaired fasting glucose) and IFG (impaired fasting glycemia), as well as other diseases and disorders such as those discussed herein.Type: GrantFiled: January 24, 2007Date of Patent: September 20, 2011Assignee: Array Biopharma, Inc.Inventors: Thomas D. Aicher, Steven Armen Boyd, Mark Joseph Chicarelli, Kevin Ronald Condroski, Rustam Ferdinand Garrey, Ronald Jay Hinklin, Ajay Singh, Timothy M. Turner
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Publication number: 20110224225Abstract: Compounds of general Formula (I): wherein R1, R2, R3, Ra, A, B and x are as defined herein are inhibitors of protein kinases in particular members of the cyclin-dependent kinase family and/or the glycogen synthase kinase 3 family and are useful in preventing and/or treating any type of pain, inflammatory disorders, cancer, immunological diseases, proliferative diseases, infectious diseases, cardiovascular diseases, metabolic disorders, renal diseases, neurologic and neuropsychiatric diseases and neurodegenerative diseases.Type: ApplicationFiled: March 10, 2011Publication date: September 15, 2011Inventors: Lutz Zeitlmann, Andre Niestroj, Ulrich Heiser
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Publication number: 20110200586Abstract: The present invention relates to compounds of Formula (I), methods for preparing these compounds, compositions, intermediates and derivatives thereof and for treating a condition including but not limited to ankylosing spondylitis, artherosclerosis, arthritis (such as rheumatoid arthritis, infectious arthritis, childhood arthritis, psoriatic arthritis, reactive arthritis), bone-related diseases (including those related to bone formation), breast cancer (including those unresponsive to anti-estrogen therapy), cardiovascular disorders, cartilage-related disease (such as cartilage injury/loss, cartilage degeneration, and those related to cartilage formation), chondrodysplasia, chondrosarcoma, chronic back injury, chronic bronchitis, chronic inflammatory airway disease, chronic obstructive pulmonary disease, diabetes, disorders of energy homeostasis, gout, pseudogout, lipid disorders, metabolic syndrome, multiple myeloma, obesity, osteoarthritis, osteogenesis imperfecta, osteolytic bone metastasis, osteomalacType: ApplicationFiled: February 16, 2011Publication date: August 18, 2011Inventors: Gilles BIGNAN, Micheal Gaul, Guozhang Xu, Bao-Ping Zhao
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Publication number: 20110201613Abstract: The present invention relates to hydroximoyl-tetrazole derivatives of formula (I), their process of preparation, their use as fungicide active agents, particularly in the form of fungicide compositions and methods for the control of phytopathogenic fungi, notably of plants, using these compounds or compositions. wherein A represents a tetrazoyl group, Het represents a pyridyl group or a thiazolyl group and X represents various substituents.Type: ApplicationFiled: July 3, 2009Publication date: August 18, 2011Inventors: Christian Beier, Jürgen Benting, David Bernier, Isabelle Christian, Pierre-Yves Coqueron, Philippe Desbordes, Christophe Dubost, Pierre Genix, Daniela Portz, Ulrike Wachendorff-Neumann
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Publication number: 20110200587Abstract: The present invention relates to compounds of Formula (I), methods for preparing these compounds, compositions, intermediates and derivatives thereof and for treating a condition including but not limited to ankylosing spondylitis, artherosclerosis, arthritis (such as rheumatoid arthritis, infectious arthritis, childhood arthritis, psoriatic arthritis, reactive arthritis), bone-related diseases (including those related to bone formation), breast cancer (including those unresponsive to anti-estrogen therapy), cardiovascular disorders, cartilage-related disease (such as cartilage injury/loss, cartilage degeneration, and those related to cartilage formation), chondrodysplasia, chondrosarcoma, chronic back injury, chronic bronchitis, chronic inflammatory airway disease, chronic obstructive pulmonary disease, diabetes, disorders of energy homeostasis, gout, pseudogout, lipid disorders, metabolic syndrome, multiple myeloma, obesity, osteoarthritis, osteogenesis imperfecta, osteolytic bone metastasis, osteomalacType: ApplicationFiled: February 16, 2011Publication date: August 18, 2011Inventors: Gilles Bignan, Micheal Gaul, Guozhang Xu, Bao-Ping Zhao
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Patent number: 7994174Abstract: The present invention relates to pyridyl sulfonamide derivatives useful as inhibitors of ion channels. The invention also provides pharmaceutically acceptable compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various disorders.Type: GrantFiled: September 17, 2008Date of Patent: August 9, 2011Assignee: Vertex Pharmaceuticals IncorporatedInventors: Esther Martinborough, Nicole Zimmermann, Timothy Neubert, Tara Hampton
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Publication number: 20110190279Abstract: The following compound is provided as an agent for treating a disease induced by production, secretion and/or deposition of amyloid ? protein, for example, a compound represented by the formula (I): wherein ring A is an optionally substituted carbocyclic group or an optionally substituted heterocyclic group, R1 is optionally substituted lower alkyl or the like, R2a and R2b are each independently hydrogen, optionally substituted lower alkyl or the like, R3a and R3c are each independently hydrogen, halogen, hydroxy, optionally substituted lower alkyl or the like, or a pharmaceutically acceptable salt thereof, or a solvate thereof.Type: ApplicationFiled: June 11, 2009Publication date: August 4, 2011Applicant: SHIONOGI & CO., LTD.Inventors: Akihiro Hori, Shuji Yonezawa, Chiaki Fujikoshi, Sae Matsumoto, Yuuji Kooriyama, Tatsuhiko Ueno, Terukazu Kato
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Publication number: 20110183992Abstract: Provided are therapeutic and/or preventive agents for migraine which comprise, as an active ingredient, a compound having a selective adenosine A2A receptor antagonistic activity or a pharmaceutically acceptable salt thereof; therapeutic and/or preventive agents for migraine which comprise, as an active ingredient, a compound having a selective adenosine A2A receptor antagonistic activity, which has an affinity for the adenosine A2A receptor 10 times or higher than that for the adenosine A1 receptor, or a pharmaceutically acceptable salt thereof; and the like.Type: ApplicationFiled: July 23, 2009Publication date: July 28, 2011Applicant: KYOWA HAKKO KIRIN CO., LTD.Inventors: Junichi Ikeda, Shunji Ichikawa, Masako Kurokawa, Tomoyuki Kanda
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Publication number: 20110172276Abstract: A carboxamide compound represented by the formula (I): [wherein Q represents a nitrogen-containing 5-membered heterocyclic group optionally fused with a benzene ring, R1 represents a C1-C3 alkyl group or the like, R2 represents a hydrogen atom or the like, and R3 represents a hydrogen atom.] has an excellent plant disease controlling effect.Type: ApplicationFiled: March 25, 2011Publication date: July 14, 2011Inventors: Sadayuki Arimori, Yoshiharu Kinoshita
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Patent number: 7977328Abstract: Compounds of formula (I) wherein R1, HET-1 and HET-2 are as described in the specification, and their salts and pro-drugs, are activators of glucokinase (GLK) and are thereby useful in the treatment of, for example, type 2 diabetes. Processes for preparing compounds of formula (I) are also described.Type: GrantFiled: October 22, 2008Date of Patent: July 12, 2011Assignee: AstraZeneca ABInventors: Darren McKerrecher, Kurt Gordon Pike, Michael James Waring
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Publication number: 20110166129Abstract: The instant invention provides for compounds that inhibit the four known mammalian JAK kinases (JAK1, JAK2, JAK3 and TYK2) and PDK1. The invention also provides for compositions comprising such inhibitory compounds and methods of inhibiting the activity of JAK1, JAK2, JAK3, TYK2 and PDK1 by administering the compound to a patient in need of treatment for myeloproliferative disorders or cancer.Type: ApplicationFiled: April 9, 2009Publication date: July 7, 2011Inventors: Michelle R. Machacek, Andrew Haidle, Anna A. Zabierek, Kaleen M. Konrad, Michael D. Altman
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Patent number: 7968577Abstract: Novel non-steroidal compounds are provided which are useful in treating diseases associated with modulation of the glucocorticoid receptor, AP-1, and/or NF-?B activity including inflammatory and immune diseases, obesity and diabetes having the structure of formula (I) an enantiomer, diastereomer, tautomer, solvate (e.g.Type: GrantFiled: October 31, 2007Date of Patent: June 28, 2011Assignee: Bristol-Myers Squibb CompanyInventors: Bingwei Vera Yang, Lidia M. Doweyko, Wayne Vaccaro, Tram N. Huynh, David R. Tortolani, T. G. Murali Dhar
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Publication number: 20110152299Abstract: Disclosed are negative allosteric modulators of the metabotropic glutamate receptor subtype 5 (mGluR5); synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating neurological and psychiatric disorders associated with glutamate dysfunction using the compounds and compositions.Type: ApplicationFiled: September 17, 2010Publication date: June 23, 2011Inventors: P. Jeffrey Conn, Craig W. Lindsley, Kyle A. Emmitte, Charles David Weaver, Alice L. Rodriguez, Andrew S. Felts, Carrie K. Jones
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Patent number: 7960392Abstract: Nitrogen-containing heterocyclic compounds represented by the following Formula (1) are provided. The compounds or salts thereof have a strong EP1 antagonistic activity when they are administered to a human or an animal, and they are useful as an effective component of a pharmaceutical agent for prophylaxis and/or treatment of an overactive bladder, for example. Furthermore, they are useful as an effective component of a pharmaceutical agent for the prophylaxis and/or treatment of symptoms including frequent urination, urinary urgency and urinary incontinence.Type: GrantFiled: July 14, 2009Date of Patent: June 14, 2011Assignee: Asahi Kasei Pharma CorporationInventors: Masakazu Atobe, Kenji Naganuma, Akifumi Morimoto, Teruki Kobayashi
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Patent number: 7951824Abstract: The present invention relates to novel pyridine-2-carboxyamide derivatives of formula (I) useful as metabotropic glutamate receptor antagonists: wherein Y, Z, R1, R2 and R3 are as defined in the specification herein.Type: GrantFiled: January 30, 2007Date of Patent: May 31, 2011Assignee: Hoffman-La Roche Inc.Inventors: Georg Jaeschke, Will Spooren, Eric Vieira
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Publication number: 20110124637Abstract: Provided herein are sirtuin-modulating compounds of formula (II). 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 relating 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: July 2, 2009Publication date: May 26, 2011Inventors: Chi B Vu, Jeremy S. Disch, Pui Yee Ng, Charles A. Blum, Robert B. Perni
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Publication number: 20110124624Abstract: Compounds of Formula I: in free or salt form, wherein Ra, Rb, R2, R3, R4 and R5 have the meanings as indicated in the specification, are useful for treating conditions that are mediated by phosphatidylinositol 3-kinase. Pharmaceutical compositions that contain the compounds and a process for preparing the compounds are also described.Type: ApplicationFiled: February 3, 2011Publication date: May 26, 2011Inventors: Graham Charles Bloomfield, Ian Bruce, Judy Fox Hayler, Catherine LeBlanc, Darren Mark Le Grand, Clive McCarthy
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Publication number: 20110118248Abstract: Compounds are provided that act as potent antagonists of the CCR2 receptor. Animal testing demonstrates that these compounds are useful for treating inflammation, a hallmark disease for CCR2. The compounds are generally aryl sulfonamide derivatives and are useful in pharmaceutical compositions, methods for the treatment of CCR2-mediated diseases, and as controls in assays for the identification of CCR2 antagonists.Type: ApplicationFiled: January 13, 2009Publication date: May 19, 2011Inventors: Solomon Ungashe, Zheng Wei, Arindrajit Basak, Trevor T. Charvat, Wei Chen, Jeff Jin, Jimmie Moore, Yibin Zeng, Sreenivas Punna, Daniel Dairaghi, Derek Hansen, Andrew M. K. Pennell, John J. Wright, Antoni Krasinski, Qiang Wang
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Publication number: 20110118470Abstract: Compounds represented by the following general formula: wherein Ag is an optionally substituted 5- to 14-membered heterocyclic group, etc.; Xg is —O—, —S—, etc.; Yg is an optionally substituted C6-14 aryl group, an optionally substituted 5- to 14-membered heterocyclic group, etc.; and Tg1 is a group represented by the following general formula: (wherein Eg is a single bond or —N(Rg2)—), Rg1 and Rg2 each independently represent a hydrogen atom, an optionally substituted C1-6 alkyl group, etc. and Zg represents a C1-8 alkyl group, a C3-8 alicyclic hydrocarbon group, a C6-14 aryl group, etc.), salts thereof or hydrates of the foregoing.Type: ApplicationFiled: January 7, 2011Publication date: May 19, 2011Inventors: Yasuhiro FUNAHASHI, Akihiko Tsuruoka, Masayuki Matsukura, Toru Haneda, Yoshio Fukuda, Junichi Kamata, Keiko Takahashi, Tomohiro Matsushima, Kazuki Miyazaki, Ken-ichi Nomoto, Tatsuo Watanabe, Hiroshi Obaishi, Atsumi Yamaguchi, Sachi Suzuki, Katsuji Nakamura, Fusayo Mimura, Yuji Yamamoto, Junji Matsui, Kenji Matsui, Takako Yoshiba, Yasuyuki Suzuki, Itaru Arimoto
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Patent number: 7943803Abstract: A clathrate compound containing a polymolecular host compound as a host compound and an agricultural chemical active ingredient having a saturated solubility in water at 25° C. of not less than 500 ppm as a guest compound.Type: GrantFiled: May 4, 2010Date of Patent: May 17, 2011Assignee: Nippon Soda Co., Ltd.Inventors: Natsuki Amanokura, Tetsuya Sahara, Hiroshi Suzuki, Yuichi Maekawa, Kiyoshi Katsuura, Yoshihiro Enomoto
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Publication number: 20110112110Abstract: Inhibitors of the oncogenic tyrosine kinase ALK and of the Bcr-Abl mutant T315I Bcr-Abl, pharmaceutical compositions containing the same and their use for the treatment of hyper-proliferative diseases.Type: ApplicationFiled: March 30, 2009Publication date: May 12, 2011Applicants: UNIVERSITA' DEGLISTUDI DI MILANO- BICOCCA, UNIVERSITE ' DE GENEVE, UNIVERSITE ' CLAUDE BERNARD DE LYON 1Inventors: Carlo Gambacorti Passerini, Rosalind Helen Gunby, Alfonso Zambon, Leonardo Scapozza, Shaheen Ahmed, Peter G. Goekjian, David Gueyrard, Florence Popowycz, Cerric Schneider
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Publication number: 20110105526Abstract: The invention provides oxazolidine and thiazolidine derivatives that are useful as subtype selective alpha 2 adrenergic agonists. As such, the compounds described herein are useful in treating a wide variety of disorders associated with selective subtype modulation of alpha 2 adrenergic receptors.Type: ApplicationFiled: January 14, 2009Publication date: May 5, 2011Inventors: Todd M. Heidelbaugh, Ken Chow, Santosh C. Sinha, Phong X. Nguyen, Wenkui K. Fang, Ling Li, Janet A. Takeuchi, Smita S. Bhat
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Publication number: 20110104110Abstract: The present invention relates to Substituted Indole Derivatives, compositions comprising at least one Substituted Indole Derivative, and methods of using these Substituted Indole Derivatives for treating or preventing a viral infection or a virus-related disorder in a patient.Type: ApplicationFiled: August 27, 2008Publication date: May 5, 2011Inventors: Gopinadhan N. Anikumar, Frank Bennett, Tin-Yau Chan, Kevin X. Chen, Mousumi Sannigrahi, Francisco Velazquez, Srikanth Venkatraman, Qingbei Zeng, Jose S. Duca, Charles A. Lesburg, Joseph A. Kozlowski, F. George Njoroge, Stuart B. Rosenblum, Neng-Yang Shih
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Publication number: 20110082144Abstract: This invention relates to compounds that are activators of glucokinase and thus may be useful for the management, treatment, control, or adjunct treatment of diseases, where increasing glucokinase activity is beneficial. The compounds are of the general formula (I) wherein A and B are further defined in the application.Type: ApplicationFiled: September 30, 2010Publication date: April 7, 2011Applicant: TransTech Pharma, Inc.Inventors: Jesper F. Lau, Per Vedsø, János Tibor Kodra, Anthony Murray, Lone Jeppesen, Michael Ankersen, Govindan Subramanian, Adnan M. M. Mjalli, Robert Carl Andrews, Dharma Rao Polisetti, Daniel Peter Christen
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Publication number: 20110082107Abstract: The present invention relates to compounds with the formula (I), (II), (III) or (IV): wherein R1, R2, R3, R4, R5, R6, R7, X and Z are as defined herein, and also to pharmaceutical compositions comprising the compounds, as well as methods of use of the compounds for treatment of disorders associated with human 11-?-hydroxysteroid dehydrogenase type 1 enzyme and for the preparation of a medicament which acts on the human 11-?-hydroxysteroid dehydrogenase type 1 enzyme.Type: ApplicationFiled: October 5, 2010Publication date: April 7, 2011Inventors: Martin Henriksson, Evert Homan, Lars Johansson, Jerk Vallgarda, Meredith Williams, Eric A. Bercot, Christopher H. Fotsch, Aiwen Li, Guolin Cai, Randall W. Hungate, Chester Chenguang Yuan, Christopher Tegley, David J.St. Jean, JR., Nianhe Han, Qi Huang, Qingyian Liu, Michael D. Bartberger, George A. Moniz, Matthew J. Frizzle
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Publication number: 20110082133Abstract: [Problems] A useful compound which can be used as a pharmaceutical, in particular, an agent for treating peripheral arterial occlusive disease is provided. [Means for Solution] The present inventors have conducted extensive studies on EP4 receptor agonists, and as a result, have found that a novel pyridone compound, in which a group having an acidic group is substituted at the 1-position of the pyridone ring, the 6-position is bonded with an aromatic ring group via a linking part, and the linking part contains a nitrogen atom, has an excellent EP4 receptor agonistic action, thereby completing the present invention. Since the compound of the present invention has an excellent EP4 receptor agonistic action, it is useful as a pharmaceutical, in particular, as an agent for treating peripheral arterial occlusive disease.Type: ApplicationFiled: June 16, 2009Publication date: April 7, 2011Inventors: Takashi Kamikubo, Masanori Miura, Takao Okuda, Keisuke Maki, Fukushi Hirayama, Ayako Moritomo, Yuriko Komiya, Keisuke Matsuura, Ryotaro Ibuka
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Publication number: 20110077244Abstract: The present invention relates to synthetic studies of a novel thiophenediamine derivative having a urea structure and to finding pharmaceutical actions thereof. The present invention provides a compound represented by the following general formula (1) or a salt thereof. In the formula (1), R1 and R2 are the same or different and represent a hydrogen atom, a lower alkyl group which may have a substituent, etc. R3 represents a hydroxy group, a lower alkoxy group which may have a substituent, a lower cycloalkyloxy group which may have a substituent, etc. R4 and R5 are the same or different and represent a halogen atom, a lower alkyl group, a hydroxy group, etc. X represents a lower alkylene group which may have a substituent, etc. Y represents a single bond or a lower alkylene group which may have a substituent, etc. W1-W2 represents N—CH, CH—N, etc. and l and m are the same or different and represent 0, 1, etc.Type: ApplicationFiled: May 25, 2009Publication date: March 31, 2011Applicant: Santen Pharmaceutical Co., Ltd.Inventors: Hiroyaki Mogi, Hisashi Tajima, Noriko Mishina, Yusuke Yamazaki, Shinji Yoneda, Katsuhiko Watanabe
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Publication number: 20110077234Abstract: The invention provides a compound of general formula (I) wherein the substituents are defined further in the application, as well as further embodiments hereof described in the attached embodiments. The present invention also provides use of the compounds of the invention for preparation of a medicament for the treatment of various diseases, e.g. for the treatment of type 2 diabetes.Type: ApplicationFiled: December 7, 2010Publication date: March 31, 2011Applicant: Novo Nordisk A/SInventors: Jesper Lau, Anthony Murray, Per Vedso, Marit Kristiansen, Lone Jeppesen
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Patent number: 7915263Abstract: The present invention relates to a compound of formula I: wherein: R1 is a hydrogen atom, F, CN, etc.; R1? is a hydrogen atom or lower alkyl which may be substituted; R2 is O, S, SO, SO2, etc.; R3 is a phenyl which may be substituted; X1, X2, and X3 each independently CH, N, etc. provided, however, that among X1, X2 and X3, the number of nitrogen is 0 or 1; W is the following residue: wherein: W1, W2, and W3 each independently CH, N, etc., or a pharmaceutically acceptable salt or ester thereof.Type: GrantFiled: August 29, 2007Date of Patent: March 29, 2011Assignee: Banyu Pharmaceutical Co., Ltd.Inventors: Yoshikazu Iwasawa, Tetsuya Kato, Nobuhiko Kawanishi, Kouta Masutani, Takashi Mita, Katsumasa Nonoshita, Mitsuru Ohkubo
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Patent number: 7915405Abstract: Disclosed herein are 2,4-disubstituted-5-aminocarbonyl-1,3-thiazole derivatives, a preparation method thereof, and a therapeutic agent for treating inflammatory diseases induced by SPC, which contains the derivative as an active ingredient. The anti-inflammatory effect of the 2,4-disubstituted-5-aminocarbonyl-1,3-thiazole derivatives was analyzed through a test employing human dermal cells and an animal test using mice and, as a result, it was found that the derivatives showed excellent inhibitory activity on SPC receptor compared to thiazole derivatives known in the prior art. Thus, the 2,4-disubstituted-5-aminocarbonyl-1,3-thiazole derivatives or pharmaceutically acceptable salts thereof are useful as active ingredients in therapeutic agents for treating inflammatory diseases, such as inflammation, pruritus and skin infection, which appear in atopic dermatitis and other diseases induced by SPC activity. wherein R1, R2, R3 and R4 are as defined in the specification.Type: GrantFiled: September 30, 2009Date of Patent: March 29, 2011Assignee: Korea Research Institute of Chemical TechnologyInventors: Young-Dae Gong, Taeho Lee, Moon-Kook Jeon, Heeyeong Cho, Jae Yang Kong, Gildon Choi, Dae Young Jeong, Soon-Hee Hwang
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Publication number: 20110071113Abstract: The present invention is related to thiazole derivatives of Formula (I) in particular for the treatment and/or prophylaxis of autoimmune disorders and/or inflammatory diseases, cardiovascular diseases, neurodegenerative diseases, bacterial or viral infections, kidney diseases, platelet aggregation, cancer, transplantation, graft rejection or lung injuries.Type: ApplicationFiled: November 23, 2010Publication date: March 24, 2011Applicant: MERCK SERONO SAInventors: Anna Quattropani, David Covini, Vincent Pomel, Jérôme Dorbais, Thomas Rueckle
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Publication number: 20110071127Abstract: Compounds of formula (I) are disclosed. Compounds according to the invention bind to and are agonists, antagonists or inverse agonists of the CB2 receptor, and are useful for treating inflammation. Those compounds which are agonists are additionally useful for treating pain.Type: ApplicationFiled: November 30, 2010Publication date: March 24, 2011Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Angela BERRY, Pier Francesco CIRILLO, Eugene Richard HICKEY, Doris RIETHER, David THOMSON, Monika ERMANN, James Edward JENKINS, Innocent MUSHI, Malcolm TAYLOR, Chandana CHOWDHURY, Christopher Francis PALMER, Nigel BLUMIRE
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Publication number: 20110061723Abstract: The present invention pertains to an electrode layer comprising a porous film made of oxide semiconductor fine particles sensitized with certain methin dyes. Moreover the present invention pertains to a photoelectric conversion device comprising said electrode layer, a dye sensitized solar cell comprising said photoelectric conversion device and to novel methin dyes.Type: ApplicationFiled: February 26, 2009Publication date: March 17, 2011Applicant: BASF SEInventors: Kazuhiko Kunimoto, Hiroshi Yamamoto, Shinji Nakamichi, Ryuichi Takahashi, Junichi Tanabe
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Publication number: 20110059973Abstract: The present invention relates to novel pyrazole compounds of the formulae I and II, to their salts and their N-oxides which can be used for combating or controlling invertebrate pests, in particular arthropod pests. The invention also relates to a method for controlling invertebrate pests by using these compounds. The present invention also relates to seed and to an agricultural and veterinary composition comprising said compounds. wherein A is a pyrazole radical of the formulae A1, A2 or A3 # denotes the binding site to the remainder of formulae I or II; X1 is S, O or NR1a; X2 is OR2a, NR2bR2c, S(O)mR2d; X3 is a lone pair or oxygen; R1, R2 and R3 are, inter alia, hydrogen, and wherein R41, R42, R43, R51, R52, R53, R61, R62, R63, are as defined in claim 1.Type: ApplicationFiled: August 26, 2008Publication date: March 10, 2011Applicant: BASF SEInventors: Steffen Gross, Delphine Breuninger, Henricus Maria Martinus Bastiaans, Wolfgang von Deyn, Michael Puhl, Karsten Koerber, Douglas D. Anspaugh, Deborah L. Culbertson, Hassan Oloumi-Sadeghi
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Publication number: 20110060013Abstract: The present invention relates to compounds useful as inhibitors of Aurora protein kinases. The invention also provides pharmaceutically acceptable compositions comprising those compounds and methods of using the compounds and compositions in the treatment of various disease, conditions, and disorders. The invention also provides processes for preparing compounds of the invention.Type: ApplicationFiled: November 20, 2009Publication date: March 10, 2011Applicant: VERTEX PHARMACEUTICALS INCORPORATEDInventors: Michael Paul Mortimore, Christopher John Davis, Julian M.C. Golec, John Studley, Daniel David Robinson
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Publication number: 20110059961Abstract: The invention relates to compounds of formula (I) which are useful as kinase inhibitors, more specifically useful as PIM kinase inhibitors, thus useful as cancer therapeutics. The invention also relates to compositions, more specifically pharmaceutical compositions comprising these compounds and methods of using the same, either alone or in combination, to treat various forms of cancer and hyperproliferative disorders, as well as methods of using the compounds for in vitro, in situ, and in vivo diagnosis or treatment of mammalian cells, or associated pathological conditions.Type: ApplicationFiled: September 8, 2010Publication date: March 10, 2011Inventors: Xiaojing Wang, Allen J. Ebens, JR.
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Publication number: 20110039849Abstract: A method for inhibiting Gram-negative bacterial pathogenesis, a method of screening for compounds that inhibit type III secretion in Gram-negative bacteria, and compounds that inhibit type III secretion in Gram-negative bacteria.Type: ApplicationFiled: August 16, 2010Publication date: February 17, 2011Applicant: UNIVERSITY OF WASHINGTONInventors: Heather B. Felise, Samuel I. Miller, Toni Kline
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Publication number: 20110028461Abstract: The present invention provides compounds of Formula I, pharmaceutical compositions thereof, and method of using the same in the treatment or prevention of diseases mediated by the activation of ?3-adrenoceptor.Type: ApplicationFiled: March 23, 2009Publication date: February 3, 2011Inventors: Richard Berger, Lehua Chang, Scott D. Edmondson, Stephen D. Goble, Bart Harper, Nam Fung Kar, Ihor E. Kopka, Bing Li, Gregori J. Morriello, Chris R. Moyes, Dong-Ming Shen, Liping Wang, Harvey Wendt, Cheng Zhu
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Patent number: 7880013Abstract: (Wherein n is an integer of from 0 to 3; R1 is substituted or unsubstituted cycloalkyl, substituted or unsubstituted aryl, a substituted or unsubstituted alicyclic heterocyclic group, or a substituted or unsubstituted aromatic heterocyclic group; R2 is halogen, substituted or unsubstituted lower alkyl, substituted or unsubstituted aryl, a substituted or unsubstituted alicyclic heterocyclic group, a substituted or unsubstituted aromatic heterocyclic group, —COR8, or the like; R3 and R4 may be the same or different, and each represents a hydrogen atom, substituted or unsubstituted lower alkyl, substituted or unsubstituted aralkyl, —COR12, or the like) For example, provided are adenosine A2A receptor antagonists comprising, as the active ingredient, a thiazole derivative represented by a general formula (I), or a pharmaceutically acceptable salt thereof, and the like.Type: GrantFiled: April 26, 2010Date of Patent: February 1, 2011Assignee: Kyowa Hakko Kirin Co., Ltd.Inventors: Takao Nakajima, Masamori Sugawara, Yuji Nomoto, Noriaki Uesaka, Yoshisuke Nakasato
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Publication number: 20110021487Abstract: The present application relates to novel cycloalkoxy-substituted 4-phenyl-3,5-dicyanopyridine derivatives, to processes for their preparation, to their use for the treatment and/or prevention of diseases and to their use for preparing medicaments for the treatment and/or prevention of diseases, preferably for the treatment and/or prevention of cardiovascular and metabolic disorders.Type: ApplicationFiled: January 31, 2009Publication date: January 27, 2011Applicant: BAYER SCHERING PHARMA AKTIENGESELLSCHAFTInventors: Walter Hübsch, Peter Nell, Frank Süssmeier, Alexandros Vakalopoulos, Daniel Meibom, Barbara Albrecht-Küpper, Katja Zimmermann
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Publication number: 20110021559Abstract: The present invention relates to compounds useful as inhibitors of protein kinases. The invention also provides pharmaceutically acceptable compositions comprising those compounds and methods of using the compounds and compositions in the treatment of various disease, conditions, and disorders. The invention also provides processes for preparing compounds of the invention.Type: ApplicationFiled: June 2, 2010Publication date: January 27, 2011Applicant: VERTEX PHARMACEUTICALS INCORPORATEDInventors: Juan-Miguel Jimenez, Philip Collier, Jeremy Green, Gregory Henkel, Michael Liu, Timothy Neuberger
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Patent number: 7871999Abstract: The present invention relates to substituted thiazoles, to methods for the production thereof, to medicaments containing these compounds and to the use thereof for producing medicaments.Type: GrantFiled: June 26, 2008Date of Patent: January 18, 2011Assignee: Gruenenthal GmbHInventors: Michael Haurand, Klaus Schiene, Sven Kühnert, Melanie Reich
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Publication number: 20110003806Abstract: This invention provides compounds of formula IA or IB: wherein R1, R2, G1 and HY are as described in the specification. The compounds are inhibitors of PI3K and/or mTor and are thus useful for treating proliferative, inflammatory, or cardiovascular disorders.Type: ApplicationFiled: January 28, 2010Publication date: January 6, 2011Applicants: Millennium Pharmaceuticals, Inc., Takeda Pharmaceutical Company LimitedInventors: Masaaki Hirose, Steven P. Langston, Hirotake Mizutani, Stepan Vyskocil