1,3-oxazoles (including Hydrogenated) Patents (Class 546/271.4)
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Publication number: 20110190282Abstract: The invention relates to compounds of general formula (I) wherein W, D, E, G, J, L, R1, R2, R3, R4, R5 and Y are as defined herein, and pharmaceutically acceptable salts, hydrates, or solvates thereof, for use—alone or in combination with one or more other pharmaceutically active compounds—in therapy, for treating diseases associated with deregulated angiogenesis, such as cancer and skin and eye diseases.Type: ApplicationFiled: August 27, 2009Publication date: August 4, 2011Applicant: LEO PHARMA A/SInventors: Jakob Felding, Xifu Liang, Anne Marie Horneman, Tina Dahlerup Poulsen, Jens Christian Højland Larsen
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Patent number: 7989449Abstract: The present invention relates to a compounds of formula I wherein R1, R1?, R2, R3, R4, X, Ar, and m are as defined in the specification and claims and pharmaceutically active acid addition salts thereof. Compounds of the invention have Asp2 (?-secretase, BACE 1 or Memapsin-2) inhibitory activity and are useful for the treatment of diseases characterized by elevated ?-amyloid levels or ?-amyloid deposits, particularly Alzheimer's disease.Type: GrantFiled: February 12, 2009Date of Patent: August 2, 2011Assignees: Hoffman-La Roche Inc., Siena Biotech S.p.A.Inventors: Matteo Andreini, Emanuele Gabellieri, Wolfgang Guba, Guido Marconi, Robert Narquizian, Eoin Power, Massimiliano Travagli, Thomas Woltering, Wolfgang Wostl
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Publication number: 20110184026Abstract: The invention provides a series of C4-substituted oxazole compounds having an alpha keto side chain at the 2 position, for example, compounds of formula I. The compounds can inhibit fatty acid amide hydrolase and can be useful for treatment of malconditions modulated by fatty acid amide hydrolase. The invention further provides methods of making compounds of formula I, useful intermediates in the preparation of compounds of formula I, and methods of using compounds of formula I and compositions thereof.Type: ApplicationFiled: June 19, 2009Publication date: July 28, 2011Inventor: Dale L. Boger
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Publication number: 20110183947Abstract: The invention provides a series of -?ketoheterocyclic compounds, for example, compounds of formula (I). The compounds can inhibit fatty acid amide hydrolase and can be useful for treatment of malconditions modulated by fatty acid amide hydrolase. The invention further provides methods of making compounds of formula (I), useful intermediates for the preparation of compounds of formula (I), and methods of using compounds of formula (I) and compositions thereof.Type: ApplicationFiled: July 8, 2009Publication date: July 28, 2011Applicant: THE SCRIPPS RESEARCH INSTITUTEInventor: Dale L. Boger
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Publication number: 20110178059Abstract: Compounds having the structure of Formula I, including pharmaceutically acceptable salts of the compounds, are CETP inhibitors, and are useful for raising HDL-cholesterol, reducing LDL-cholesterol, and for treating or preventing atherosclerosis. The compounds have 3 cyclic groups connected by single bonds, as for example triphenyl, which are attached directly to the ring of formula I or attached at the position B.Type: ApplicationFiled: March 28, 2011Publication date: July 21, 2011Applicant: Merck Sharp & Dohme Corp.Inventors: Amjad ALI, Zhijian Lu, Peter J. Sinclair, Yi-Heng Chen, Cameron J. Smith, Hong Li
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Publication number: 20110172223Abstract: A series of substituted aryl sulfone derivatives represented by Formula I, or pharmaceutically acceptable salts thereof. Pharmaceutical compositions comprise an effective amount of the instant compounds, either alone, or in combination with one or more other therapeutically active compounds, and a pharmaceutically acceptable carrier. Methods of treating conditions associated with, or caused by, calcium channel activity, including, for example, acute pain, chronic pain, visceral pain, inflammatory pain, neuropathic pain, urinary incontinence, itchiness, allergic dermatitis, epilepsy, diabetic neuropathy, irritable bowel syndrome, depression, anxiety, multiple sclerosis, sleep disorder, bipolar disorder and stroke, comprise administering an effective amount of the present compounds, either alone, or in combination with one or more other therapeutically active compounds.Type: ApplicationFiled: September 21, 2009Publication date: July 14, 2011Inventors: Prasun K. Chakravarty, Pengcheng Patrick Shao
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Publication number: 20110166358Abstract: The present invention offers compounds or their salts expressed by formula (I) (in the formula, X indicates an alkyl group, or the like; Y indicates an alkyl group; Z indicates a respectively independent nitro group, or the like; n indicates any integer from 0 to 3; A indicates carbon atom, or the like, and hydrogen atom is bonded thereto in the case where the carbon atom is not substituted with Z; D indicates oxygen atom, or the like; W indicates hydrogen atom, or the like; R1 and R2 indicate respectively independent hydrogen atoms, or the like; R1 and R2 may be bonded, and may form a heterocycle together with the nitrogen atom between R1 and R2).Type: ApplicationFiled: September 15, 2009Publication date: July 7, 2011Applicant: NIPPON SODA CO., LTD.Inventors: Jyun Iwata, Masahiro Kawaguchi
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Patent number: 7968572Abstract: It is intended to provide a compound represented by the formula (I): wherein all the symbols are as defined in the description; which has a p38 MAP kinase inhibitory activity, a salt thereof, an N-oxide thereof, a solvate thereof, or a prodrug thereof. The compound of the invention is useful for preventing or treating a disease in which the abnormal production of a cytokine such as an inflammatory cytokine or a chemokine or overreaction to them is considered to be involved in the cause and aggravation of pathological conditions, in other words, an inflammatory disease, a respiratory disease, a cardiovascular disease, a central nervous system disease or the like, which is a cytokine-mediated disease.Type: GrantFiled: October 2, 2006Date of Patent: June 28, 2011Assignee: Ono Pharmaceuticals Co., Ltd.Inventors: Hisao Nakai, Shingo Yamamoto, Shingo Nakatani, Tomomi Hirosaki
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Publication number: 20110144164Abstract: The present invention relates to compounds useful in therapy, in particular in the treatment of psychosis, to compositions comprising said compounds, and to methods of treating diseases comprising the administration of said compounds.Type: ApplicationFiled: December 14, 2010Publication date: June 16, 2011Applicant: H. LUNDBECK A/SInventors: Nikolay Khanzhin, Søren Møller Nielsen, Karsten Juhl, Lars Kyhn Rasmussen
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Publication number: 20110144128Abstract: Heterocyclic carboxamide compounds are described herein as being useful in modulating the activity of steroid nuclear receptors. Pharmaceutical compositions containing the compounds, methods of using the compounds and processes for making the compounds are also described.Type: ApplicationFiled: January 6, 2006Publication date: June 16, 2011Applicant: EXELIXIS, INC.Inventors: Brenton T. Flatt, Xiao-Hui Gu, Richard Martin, Raju Mohan, Brett Murphy, Michael C. Nyman, William C. Stevens, JR., Tie-Lin Wang
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Publication number: 20110144333Abstract: The invention relates to compounds of formula I wherein R1, R2, X, Y, and n are defined in the specification and to pharmaceutically acceptable acid addition salts thereof. The invention also provides pharmaceutical compositions and methods of manufacture of such compounds. The compounds are useful for the treatment of diseases related to the biological function of the trace amine associated receptors, which diseases are depression, anxiety disorders, bipolar disorder, attention deficit hyperactivity disorder, stress-related disorders, psychotic disorders, schizophrenia, neurological diseases, Parkinson's disease, neurodegenerative disorders, Alzheimer's disease, epilepsy, migraine, substance abuse and metabolic disorders, eating disorders, diabetes, diabetic complications, obesity, dyslipidemia, disorders of energy consumption and assimilation, disorders and malfunction of body temperature homeostasis, disorders of sleep and circadian rhythm, and cardiovascular disorders.Type: ApplicationFiled: February 24, 2011Publication date: June 16, 2011Inventors: Guido Galley, Annick Goergler, Katrin Groebke Zbinden, Roger Norcross
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Publication number: 20110144119Abstract: The present invention is directed to certain oxazole derivatives which are useful as inhibitors of Fatty Acid Amide Hydrolase (FAAH). The invention is also concerned with pharmaceutical formulations comprising these compounds as active ingredients and the use of the compounds and their formulations in the treatment of certain disorders, including osteoarthritis, rheumatoid arthritis, diabetic neuropathy, postherpetic neuralgia, skeletomuscular pain, and fibromyalgia, as well as acute pain, migraine, sleep disorder, Alzeimer Disease, and Parkinson's Disease.Type: ApplicationFiled: July 30, 2009Publication date: June 16, 2011Inventors: Harry Chobanian, Linus S. Lin, Ping Liu, Marc D. Chioda, Robert J. DeVita, Ravi P. Nargund, Yan Guo
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Publication number: 20110136833Abstract: The invention relates to tetrahydropyridinyl and dihydropyrrolyl compounds of Formula (I): and pharmaceutically acceptable salts, prodrugs, or solvates thereof, wherein X, Y, Z, R1, R2, m, and n are defined as set forth in the specification. The invention is also directed to the use of compounds of Formula (I) to treat a disorder responsive to the blockade of calcium channels, and particularly N-type calcium channels. Compounds of the present invention are especially useful for treating pain.Type: ApplicationFiled: August 3, 2009Publication date: June 9, 2011Applicant: Shinogi & Co., Ltd.Inventors: Hidenori Mikamiyama, Chiyou NI, Bin Shao, Laykea Tafesse
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Publication number: 20110136871Abstract: The present application relates to novel 2-alkoxy-substituted dicyanopyridines, to processes for their preparation, to their use for the treatment and/or prophylaxis of diseases and to their use for preparing medicaments for the treatment and/or prophylaxis of diseases, preferably for the treatment and/or prevention of cardiovascular disorders.Type: ApplicationFiled: May 22, 2009Publication date: June 9, 2011Applicant: BAYER SCHERING AKTIENGESELLSCHAFTInventors: Walter Hübsch, Daniel Meibom, Alexandros Vakalopoulos, Barbara albrecht-Küpper, Peter Nell, Katja Zimmermann, Frank Süssmeier, Joerg Keldenich
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Publication number: 20110136829Abstract: The invention provides new oxazolidinone compounds of formula (I) wherein R, R1, R2 and R3 have different meanings. Preparative processes, pharmaceutical compositions, and uses thereof in the treatment of bacterial infections are also provided.Type: ApplicationFiled: June 29, 2009Publication date: June 9, 2011Applicant: FERRER INTERNACIONAL, S.A.Inventors: Montserrat Cano, Albert Palomer, Antonio Guglietta
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Publication number: 20110130377Abstract: The present application relates to novel substituted aryloxazole derivatives, a method for the production thereof, the use thereof for the treatment and/or prophylaxis of diseases and the use thereof for the production of drugs for the treatment and/or prophylaxis of diseases, preferably for the treatment and/or prevention of cardiovascular and metabolic disorders.Type: ApplicationFiled: July 17, 2008Publication date: June 2, 2011Applicant: BAYER SCHERING PHARMA AKTIENGESELLSCHAFTInventors: Peter Nell, Walter Hübsch, Barbara Albrecht-Küpper, Jorg Keldenich, Alexandros Vakalopoulos, Frank Süssmeier, Katja Zimmermann, Dieter Lang, Daniel Meibom
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Publication number: 20110124647Abstract: The present invention relates to novel derivatives of substituted benzylamines, to processes for their preparation and to their use for controlling animal pests, especially arthropods, in particular insects.Type: ApplicationFiled: March 28, 2008Publication date: May 26, 2011Applicant: Bayer CropScience AGInventors: Christian Arnold, Ulrich Görgens, Hans-Georg Schwarz, Graham Holmwood, Roland Andree, Olga Malsam, Otto Schallner, Eva-Marie Franken, Horst-Peter Antonicek, Stefan Werner
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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: 20110112080Abstract: The invention relates to compounds of formula I wherein the definitions of X, R and R1 are as defined herein. The compounds of formula I have a good affinity to the trace amine associated receptors (TAARs), especially for TAAR1. The compounds can be used for the treatment of depression, anxiety disorders, bipolar disorder, attention deficit hyperactivity disorder (ADHD), stress-related disorders, psychotic disorders such as schizophrenia, neurological diseases such as Parkinson's disease, neurodegenerative disorders such as Alzheimer's disease, epilepsy, migraine, hypertension, substance abuse and metabolic disorders such as eating disorders, diabetes, diabetic complications, obesity, dyslipidemia, disorders of energy consumption and assimilation, disorders and malfunction of body temperature homeostasis, disorders of sleep and circadian rhythm, and cardiovascular disorders.Type: ApplicationFiled: November 3, 2010Publication date: May 12, 2011Inventors: Guido Galley, Roger Norcross, Alessandra Polara
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Publication number: 20110105436Abstract: Provided herein are novel heteroaryl compounds, compositions comprising the compounds, and methods of treatment or prevention comprising administration of the compounds. The compounds are effective in the targeting of cells defective in the von Hippel-Lindau gene and in inducing autophagic cell death. The methods are directed to treating or preventing diseases such as cancer, and in particular cancers resulting from von Hippel-Lindau disease. The compounds of the invention may be administered in combination with another therapeutic agent.Type: ApplicationFiled: March 10, 2009Publication date: May 5, 2011Applicants: AUCKLAND UNISERVICES LIMITED, THE BOARD OF TRUSTEES OF THE LELAND STANFORD JUNIOR UNIVERSITYInventors: Sandra Turcotte, Denise A. Chan, Patrick D. Sutphin, Amato J. Giaccia, Michael P. Hay, William A. Denny, Muriel Marie Bonnet
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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: 20110105504Abstract: This invention relates to novel compounds of the Formula (I) and pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof which are useful for the therapeutic treatment of diseases associated with the modulation or inhibition of 11?-HSD1 in mammals.Type: ApplicationFiled: March 18, 2009Publication date: May 5, 2011Inventors: David A. Claremon, Linghang Zhuang, Yuanjle Ye, Suresh B. Singh, Colin M. Tice, Gerard McGeehan
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Publication number: 20110098302Abstract: Described herein are compounds that are antagonists of PGD2 receptors. Also described are pharmaceutical compositions and medicaments that include the antagonists of PGD2 receptors described herein, as well as methods of using such antagonists of PGD2 receptors, alone and in combination with other compounds, for treating respiratory, cardiovascular, and other PGD2-dependent or PGD2-mediated conditions or diseases.Type: ApplicationFiled: February 12, 2009Publication date: April 28, 2011Applicant: AMIRA PHARMACEUTICALS, INC.Inventors: John Howard Hutchinson, Thomas Jon Seiders, Brian Andrew Stearns, Bowei Wang, Yen Pham Truong, Jeannie M. Arruda
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Patent number: 7915271Abstract: Compounds having the structure of Formula I, including pharmaceutically acceptable salts of the compounds, are CETP inhibitors, and are useful for raising HDL-cholesterol, reducing LDL-cholesterol, and for treating or preventing atherosclerosis. The compounds have 3 cyclic groups connected by single bonds, as for example triphenyl, which are attached directly to the ring of formula I or attached at the position B.Type: GrantFiled: December 29, 2006Date of Patent: March 29, 2011Assignee: Merck Sharp & Dohme Corp.Inventors: Amjad Ali, Zhijian Lu, Peter J. Sinclair, Yi-Heng Chen, Cameron J. Smith, Hong Li
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Patent number: 7915270Abstract: Certain oxazole ketone compounds are useful as FAAH inhibitors. Such compounds may be used in pharmaceutical compositions and methods for the treatment of disease states, disorders, and conditions mediated by fatty acid amide hydrolase (FAAH) activity. Thus, the compounds may be administered to treat anxiety, pain, inflammation, sleep disorders, eating disorders, or movement disorders (such as MS).Type: GrantFiled: February 20, 2007Date of Patent: March 29, 2011Assignee: The Scripps Research InstituteInventor: Dale L. Boger
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Patent number: 7910592Abstract: Compounds having the structure of Formula (I), including pharmaceutically acceptable salts of the compounds, are CETP inhibitors and are useful for raising HDL-cholesterol, reducing LDL-cholesterol, and for treating or preventing atherosclerosis. In the compounds of Formula (I), B is a cyclic group other than phenyl, and B has a cyclic substituent at a position that is ortho to the position at which B is connected to the remainder of the structure of Formula (I). The 5-membered ring of Formula (I) has a second cyclic substituent in addition to B.Type: GrantFiled: December 29, 2006Date of Patent: March 22, 2011Assignee: Merck Sharp & Dohme Corp.Inventors: Amjad Ali, Zhijian Lu, Peter J. Sinclair, Yi-Heng Chen, Cameron J. Smith, Hong Li, Christopher F. Thompson
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Publication number: 20110065129Abstract: This invention relates to novel indane acetic acid derivatives which are useful in the treatment of diseases such as diabetes, obesity, hyperlipidemia, and atherosclerotic diseases. The invention also relates to intermediates useful in preparation of indane acetic derivatives and to methods of preparation.Type: ApplicationFiled: February 11, 2009Publication date: March 17, 2011Inventors: Derek B. Lowe, Philip L. Wickens, Xin Ma, Mingbao Zhang, William H. Bullock, Philip D. G. Coish, Ingo A. Mugge, Andreas Stolle, Ming Wang, Yamin Wang, Chengzhi Zhang, Hai-Jun Zhang, Lei Zhu, Manami Tsutsumi, James N. Livingston
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Publication number: 20110060011Abstract: The present invention relates generally to compounds represented in Formula (I), pharmaceutical compositions comprising them and methods of treating of diseases or disorders such as cancer.Type: ApplicationFiled: March 13, 2009Publication date: March 10, 2011Applicant: Amgen Inc.Inventors: Matthew Brown, Michael Johnson
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Publication number: 20110046162Abstract: The present application relates to novel substituted fused cyanopyridine 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 disorders.Type: ApplicationFiled: December 9, 2008Publication date: February 24, 2011Applicant: BAYER SCHERING PHARMAInventors: Peter Nell, Alexandros Vakalopoulos, Frank Süssmeier, Barbara Albrecht-Küpper, Katja Zimmermann, Jörg Keldenich, Daniel Meibom
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Publication number: 20110039846Abstract: The present invention aims to provide an iminopyridine derivative compound having an ?1D adrenergic receptor antagonistic action, which is useful as an agent for the prophylaxis or treatment of a lower urinary tract disease and the like. The present invention provides a compound represented by the formula wherein each symbol is as defined in the specification, or a salt thereof.Type: ApplicationFiled: April 22, 2009Publication date: February 17, 2011Applicant: TAKEDA PHARMACEUTICAL COMPANY LIMITEDInventors: Masato Yoshida, Nobuki Sakauchi, Ayumu Sato
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Publication number: 20110034483Abstract: The present invention is directed to 2-aminoimidazole compounds of formula (I) which are inhibitors of the beta-secretase enzyme and that are useful in the treatment of diseases in which the beta-secretase enzyme is involved, such as Alzheimer's disease. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the treatment of such diseases in which the beta-secretase enzyme is involved.Type: ApplicationFiled: February 18, 2009Publication date: February 10, 2011Inventors: Ivory D. Hills, Craig A. Coburn, Samuel L. Graham, Keith P. Moore, Philippe G. Nantermet, Hemaka A. Rajapakse, Shawn J. Stachel, Hong Zhu
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Publication number: 20110034517Abstract: The invention provides well-defined heterocyclic compounds 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: February 10, 2011Applicant: ALLERGAN, INC.Inventors: 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: 20110021527Abstract: In one aspect, the invention relates to compounds having the formula: wherein: Ar, Z, R3, R4 and R5 are as defined in the specification, or a pharmaceutically acceptable salt thereof. These compounds have AT1 receptor antagonist activity and neprilysin inhibition activity. In another aspect, the invention relates to pharmaceutical compositions comprising such compounds; methods of using such compounds; and process and intermediates for preparing such compounds.Type: ApplicationFiled: July 14, 2010Publication date: January 27, 2011Inventors: Paul R. FATHEREE, Ryan HUDSON, Robert Murray MCKINNELL
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Publication number: 20110021573Abstract: Described herein are compounds that are antagonists of PGD2 receptors. Also described are pharmaceutical compositions and medicaments that include the antagonists of PGD2 receptors described herein, as well as methods of using such antagonists of PGD2 receptors, alone and in combination with other compounds, for treating respiratory, cardiovascular, and other PGD2-dependent or PGD2-mediated conditions or diseases.Type: ApplicationFiled: February 25, 2009Publication date: January 27, 2011Applicant: AMIRA PHARMACEUTICALS, INC.Inventors: John Howard Hutchinson, Brian Andrew Stearns, Thomas Jonathan Seiders, Jill Melissa Scott, Jeannie M. Arruda, Bowei Wang
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Publication number: 20110021523Abstract: Compounds are provided that act as potent antagonists of the CCR9 receptor, and which have been further confirmed in animal testing for inflammation, one of the hallmark disease states for CCR9. The compounds are generally aryl sulfonamide derivatives and are useful in pharmaceutical compositions, methods for the treatment of CCR9-mediated diseases, and as controls in assays for the identification of CCR9 antagonists.Type: ApplicationFiled: October 1, 2010Publication date: January 27, 2011Applicant: CHEMOCENTRYX, INC.Inventors: Solomon Ugashe, Zheng Wei, J.J. Wright, Andrew Pennell
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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: 20110003826Abstract: This invention relates to new chemical compounds, application of these compounds as anticoagulants, pharmaceutical compositions, and plasma-substituting solutions on their basis, and can be used for treating thromboembolic complications of diseases such as myocardial infarction, stroke, and thrombosis of deep veins or a pulmonary artery; and for preventing hypercoagulation conditions in consequence of injuries, surgeries, sepsis, various obstetric pathologies, in disaster medicine, resuscitation, and so on.Type: ApplicationFiled: June 27, 2008Publication date: January 6, 2011Applicant: Obschestvo S Organichennoi Otvetsttvennoctiyu "BioInventors: Elena Ivanovna Sinauridze, Fazoil Inoyatovich Ataullakhanov, Andrey Alexandrovich Butylin, Vladimir Borisovich Sulimov, Alexey Nickolayevich Romanov, Alexey Alexeevich Bogolyubov, Yury Vladimirovich Kuznetsov, Irina Vladimirovna Gribkova, Alexander Sergeevich Gorbatenko, Olga Anatolievna Kondakova
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Publication number: 20110003787Abstract: The present invention relates to a compound or a pharmacologically acceptable salt thereof having superior glucokinase activating activity, and is a compound represented by general formula (I), or pharmacologically acceptable salt thereof: [wherein, A represents, for example, an oxygen atom or sulfur atom, R1 represents, for example, a C1-C6 alkyl group, a C1-C6 alkoxy group or a C1-C6 halogenated alkyl group, A and R1 together with the carbon atom bonded thereto form a heterocyclic group that may be substituted with 1 to 3 group(s) independently selected from Substituent Group ?, R2 represents a phenyl group that may be substituted with 1 to 5 group(s) independently selected from Substituent Group ? or a heterocyclic group that may be substituted with 1 to 3 group(s) independently selected from Substituent Group ?, R3 represents a hydroxy group or a C1-C6 alkoxy group, and Substituent Group ? consists of, for example, a halogen atom, a C1-C6 alkyl group, a C1-C6 alkyl group substituted with 1 or 2 hydType: ApplicationFiled: July 26, 2010Publication date: January 6, 2011Inventors: Akihiro Furukawa, Takehiro Fukuzaki, Yukari Onishi, Hideki Kobayashi, Takeshi Honda, Yumi Matsui, Masahiro Konishi, Kenjiro Ueda, Tetsuyoshi Matsufuji
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Publication number: 20110003815Abstract: The present invention provides compounds of Formula I which are FLAP inhibitors useful as anti-atherosclerotic, anti-asthmatic, anti-allergic, anti-inflammatory and cytoprotective agents.Type: ApplicationFiled: October 6, 2008Publication date: January 6, 2011Inventors: Anthony Ogawa, Feroze Ujjainwalla, Bing Li, Lin Chu, Minal Patel, Helen M. Armstrong, Hyun O. Ok, Rosemary Sisco, Dwight MacDonald, John Hutchinson, Helene Perrier
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Publication number: 20100331302Abstract: Compounds are provided that act as potent antagonists of the CCR9 receptor. Animal testing demonstrates that these compounds are useful for treating inflammation, a hallmark disease for CCR9. The compounds are generally aryl sulfonamide derivatives and are useful in pharmaceutical compositions, methods for the treatment of CCR9-mediated diseases, and as controls in assays for the identification of CCR9 antagonists.Type: ApplicationFiled: July 8, 2010Publication date: December 30, 2010Applicant: Chemocentryx, Inc.Inventors: Trevor T. Charvat, Cheng Hu, Anita Melikian, Aaron Novack, Andrew M.K. Pennell, Edward J. Sullivan, William D. Thomas, Solomon Ungashe, Penglie Zhang, Jay Powers, Sreenivas Punna
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Patent number: 7842706Abstract: Pharmaceutical composition which comprises an insulin sensitivity enhancer in combination with other antidiabetics differing from the enhancer in the mechanism of action, which shows a potent depressive effect on diabetic hyperglycemia and is useful for prophylaxis and treatment of diabetes.Type: GrantFiled: March 20, 2009Date of Patent: November 30, 2010Assignee: Takeda Pharmaceutical Company LimitedInventors: Hitoshi Ikeda, Takashi Sohda, Hiroyuki Odaka
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Publication number: 20100298558Abstract: There is provided a novel pest control agent, particularly an insecticide or miticide. A substituted dihydroazole compound of General Formula (1) or a salt thereof: where A1, A2, A3 and A4 are independently C—Y or N, A5 is —CH2—, etc., G1 is a benzene ring, etc., G2 is G2-1, G2-6, G2-9, etc., X is a halogen atom, C1-2haloalkyl, etc., Z is methyl, —NH2, etc., R1 is —C(O)R1a, etc., R1a is C1-4alkyl, etc., R2 is H, C1-4alkyl, etc., R3 is C1-2haloalkyl, etc., R4 is H, cyano, methyl, etc., m is an integer of 1, 2, 3, etc., n is an integer of 0 or 1; and a pest control agent comprising the compound or the salt thereof.Type: ApplicationFiled: December 5, 2008Publication date: November 25, 2010Applicant: NISSAN CHEMICAL INDUSTRIES, LTD.Inventors: Takeshi Mita, Eitatsu Ikeda, Hiroaki Takahashi, Mitsuaki Komoda
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Publication number: 20100298293Abstract: The invention relates to novel substituted oxazolidinones, to processes for preparation thereof, to the use thereof for treatment and/or prophylaxis of diseases, and to the use thereof for producing medicaments for treatment and/or prophylaxis of diseases, especially of thromboembolic disorders.Type: ApplicationFiled: June 13, 2008Publication date: November 25, 2010Applicant: BAYER SCHERING PHARMA ATIENGESELLSCHAFTInventors: Swen Allerheiligen, Marcus Bauser, Hartmut Schirok, Michael Härter, Stephan Siegel, Ulrich Rester, Christoph Gerdes, Stefan Heitmeier, Georges Von Degenfeld, Anja Buchmüller, Elke Dittrich-Wengenroth, Uwe Saatman, Julia Strassburger, Mark Jean Gnoth, Dieter Lang
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Publication number: 20100298301Abstract: The invention provides a compound which is an amide of the formula (1), or a salt, solvate, N-oxide or tautomer thereof; wherein: a is 0 or 1; b is 0 or 1: provided that the sum of a and b is 0 or 1; T is O or NH Ar1 is a monocyclic or bicyclic 5- to 10-membered aryl or heteroaryl group containing up to 4 heteroatoms selected from O, N and S, and being optionally substituted by one or more substituents R1; Ar2 Js a monocyclic or bicyclic 5- to 10-membered aryl or heteroaryl group containing up to 4 heteroatoms selected from O, N and S and being optionally substituted by one or more substituents R2; and R1 and R2 are as defined in the claims. The compounds are inhibitors of kinases and in particular FLT3, FLT4 and Aurora kinases.Type: ApplicationFiled: May 9, 2008Publication date: November 25, 2010Applicant: SAREUM LIMITEDInventors: John Charles Reader, John Mark Ellard, Helen Boffey, Susanne Taylor, Andrew David Carr, Michael Cherry, Michelle Wilson, Richard Boakye Owoare
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Publication number: 20100292241Abstract: The present invention is directed to 3,5-disubstituted-1,3-oxazolidin-2-one derivatives which are potentiators of metabotropic glutamate receptors, including the mGluR2 receptor, and which are useful in the treatment or prevention of neuro-ological and psychiatric disorders associated with glutamate dysfunction and diseases in which metabotropic glutamate receptors are involved. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which metabotropic glutamate receptors are involved.Type: ApplicationFiled: January 14, 2009Publication date: November 18, 2010Applicant: Merck Sharp & Dohme Corp.Inventors: Edward Brnardic, Mark Fraley, Mark Layton, Robert Garbaccio
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Publication number: 20100286210Abstract: An object of the present invention is to provide novel carbazole derivatives, solvates thereof, or pharmaceutically acceptable salts thereof having an excellent adipose tissue weight reducing effect, hypoglycemic effect, and hypolipidemic effect, which are useful as a preventive and/or therapeutic agent for fatty liver, obesity, lipid metabolism abnormality, visceral adiposity, diabetes, hyperlipemia, impaired glucose tolerance, hypertension, non-alcoholic fatty liver disease, non-alcoholic steatohepatitis, and the like.Type: ApplicationFiled: October 28, 2005Publication date: November 11, 2010Applicant: Zeria Pharmaceutical Co., Ltd.Inventors: Masakazu Murata, Yoshihiko Itokazu, Ryu Nakao
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Publication number: 20100286211Abstract: The present invention relates to certain substituted phenyl oxazolidinones and to processes for the synthesis of the same. This invention also relates to pharmaceutical compositions containing the compounds of the present invention as antimicrobials. The compounds are useful antimicrobial agents, effective against a number of human and veterinary pathogens, including gram-positive aerobic bacteria, for example, multiple-resistant staphylococci, streptococci and enterococci as well as anaerobic organisms, for example, Bacterioides spp. and Clostridia spp. species, and acid fast organisms, for example, Mycobacterium tuberculosis, Mycobacterium avium and Mycobacterium spp.Type: ApplicationFiled: October 6, 2005Publication date: November 11, 2010Inventors: Biswajit Das, Shahadal Ahmed, Ajay Singh Yadav, Soma Ghosh, Arti Gujrati, Pankaj Sharma, Ashok Rattan
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Publication number: 20100286170Abstract: The present invention provides novel beta-secretase inhibitors and methods for their use, including methods of treating of Alzheimer's disease.Type: ApplicationFiled: September 24, 2008Publication date: November 11, 2010Inventors: Arun K. Ghosh, Chunfeng Liu, Thippeswamy Devasamudram, Hui Lei, Lisa M. Swanson, Sudha V. Ankala, John C. Lilly, Geoffrey M. Bilcer
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Publication number: 20100286103Abstract: The invention relates to compounds that are useful as immunosuppressive agents and for treating and preventing inflammatory conditions, allergic disorders, and immune disorders.Type: ApplicationFiled: July 31, 2008Publication date: November 11, 2010Inventor: Shoujun Chen
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Patent number: 7816379Abstract: The present invention relates to novel derivatives of oxazolidinone, a method thereof and pharmaceutical compositions comprising the derivatives for use in an antibiotic. The oxazolidinone derivatives of the present invention show inhibitory activity against a broad spectrum of bacteria and lower toxicity. The prodrugs, prepared by reacting the compound having hydroxyl group with amino acid or phosphate, have an excellent efficiency on solubility thereof against water. Further, the derivatives of the present invention may exert potent antibacterial activity versus various human and animal pathogens, including Gram-positive bacteria such as Staphylococi, Enterococci and Streptococi, anaerobic microorganisms such as Bacteroides and Clostridia, and acid-resistant microorganisms such as Mycobacterium tuberculosis and Mycobacterium avium. Accordingly, the compositions comprising the oxazolidinone are used in an antibiotic.Type: GrantFiled: December 17, 2004Date of Patent: October 19, 2010Assignee: Dong-A Pharm. Co., Ltd.Inventors: Jae Keol Rhee, Weon Bin Im, Chong Hwan Cho, Sung Hak Choi, Tae Ho Lee