Nitrogen Attached Indirectly To The Thiazole Ring By Nonionic Bonding Patents (Class 548/205)
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Publication number: 20110207714Abstract: The biphenyic compounds of formula (I) are serotonin modulators useful in the treatment of serotonin-mediated diseases.Type: ApplicationFiled: October 29, 2009Publication date: August 25, 2011Inventors: Nicholas I. Carruthers, Brock T. Shireman, Vi T. Tran, Victoria D. Wong, Jill A. Jablonowski, Wenying Chai
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Publication number: 20110190335Abstract: The purpose of the present invention is to provide a glucokinase activator which is useful as a pharmaceutical agent such as agents for the prophylaxis or treatment of diabetes, obesity and the like, and the like. The present invention is a compound represented by the formula (I): wherein each symbol is as defined in the specification, or a salt thereof.Type: ApplicationFiled: April 15, 2009Publication date: August 4, 2011Inventors: Tsuneo Yasuma, Osamu Ujikawa
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Publication number: 20110184186Abstract: The present invention provides a process for preparing thiazole derivatives of formula (I), that activate the delta subtype of the human Peroxisome Proliferator Activated Receptor (hPPAR ?), and also provides compounds of formula (II), (IV), (X), (XI) and (XII), intermediate compounds for preparation of the above compounds of formula (I).Type: ApplicationFiled: April 1, 2011Publication date: July 28, 2011Applicant: Seoul National University Industry FoundationInventors: Heon Joong Kang, Jung Yeob Ham
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Publication number: 20110183953Abstract: Compounds that selectively modulate the sphingosine 1 phosphate receptor are provided including compounds which modulate subtype 1 of the S1P receptor. Methods of chiral synthesis of such compounds is provided. Uses, methods of treatment or prevention and methods of preparing inventive compositions including inventive compounds are provided in connection with the treatment or prevention of diseases, malconditions, and disorders for which modulation of the sphingosine 1 phosphate receptor is medically indicated.Type: ApplicationFiled: November 15, 2010Publication date: July 28, 2011Inventors: Marcus F. Boehm, Esther Martinborough, Enugurthi Brahmachary, Manisha Moorjani, Junko Tamiya, Liming Huang, Adam Richard Yeager
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Publication number: 20110178133Abstract: The present invention relates generally to novel calcimimetic compounds and pharmaceutical compositions comprising them. The invention also relates to methods of treating of diseases or disorders related to the function of the calcium sensing receptor using the compounds represented in Formula I.Type: ApplicationFiled: October 15, 2008Publication date: July 21, 2011Inventors: Thomas S. Coulter, Christopher H. Fotsch, Chiara Ghiron, Paul E. Harrington, Michael G. Kelly, Philip Miller, Gilbert M. Rishton, David J. St.Jean, JR., David J. Semin
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Patent number: 7982036Abstract: The present invention provides compounds of formula I wherein Ring A, Ring B, m, Rx, Ry, W and R1 are as defined herein, pharmaceutically acceptable salts and compositions thereof, and methods of using the same.Type: GrantFiled: October 17, 2008Date of Patent: July 19, 2011Assignee: Avila Therapeutics, Inc.Inventors: Juswinder Singh, Shomir Ghosh, Arthur F. Kluge, Russell C. Petter, Richland W. Tester
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Publication number: 20110172434Abstract: The invention relates to thiazole, oxazole, imidazole, isoxazole and isoxazoline derivatives of general formula (I) wherein Het is thiazole, oxazole, imidazole, isoxazole or isoxazoline, n is an integer from 0 to 6, A is notably selected from various optionally substituted aromatic radicals, B is notably hydrogen, alkyl or phenyl, R1 and R2 are notably independently hydrogen, alkyl or cycloalkyl and ? is —NR46R47 or —OR48, R46 and R47 are notably independently hydrogen, alkyl, cycloalkyl or —(CH2)k—COOR51, R51 is notably alkyl or haloalkyl and R48 is notably hydrogen or alkyl. These compounds have advantageous pharmacological properties which allow their use in therapeutics, notably for treating neurodegenerative disorders or pain.Type: ApplicationFiled: March 21, 2011Publication date: July 14, 2011Applicant: Ipsen Pharma S.A.S.Inventors: Pierre-Etienne CHABRIER DE LASSAUNIERE, Jeremiah Harnett, Dennis Bigg, Anne-Marie Liberatore, Jacques Pommier, Jacques Lannoy, Christophe Thurieau
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Patent number: 7977332Abstract: Certain noel N-(heteroarylalkyl)alkanediamine derivatives have provided unexpected insecticidal and acaricidal activity. These compounds are represented by formula I: wherein Ar, a, r, R, Ra, Rb, Rc, Rd, b, c, Re, Rf, Rg, Rh, R5, d, e, U, V, X, WR6 and R7 are fully described herein. In addition, compositions comprising an insecticidally effective amount of at least one compound of formula I, and optionally, an effective amount of at least one of a second compound, with at least one insecticidally compatible carrier are also disclosed; along with methods of controlling insects comprising applying said compositions to a locus where insects are present or are expected to be present.Type: GrantFiled: December 2, 2004Date of Patent: July 12, 2011Assignee: FMC CorporationInventors: David M. Roush, John F. Chiarello, Jianming Yu, Benjamin J. Dugan, George Theodoridis, Manorama M. Patel, Walter H. Yeager, Steven W. Szczepanski
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Patent number: 7973045Abstract: The invention provides anhydrous forms of dasatinib, methods for their preparation, and pharmaceutical compositions thereof.Type: GrantFiled: June 14, 2010Date of Patent: July 5, 2011Assignee: Teva Pharmaceutical Industries Ltd.Inventors: Ondrej {hacek over (S)}imo, Ji{hacek over (r)}í Filip{hacek over (c)}ík, Alexandr Martaus, Alexandr Jegorov, Ale{hacek over (s)} Gavenda, Judith Aronhime, Pavel Vraspír, Tamás Koltai, Ji{hacek over (r)}í Faustmann, Roman Gabriel
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Publication number: 20110152232Abstract: Compounds that modulate GHS-R are described, for examples compounds formula (I)Type: ApplicationFiled: October 26, 2010Publication date: June 23, 2011Inventors: Jeffrey O. Saunders, Thomas Coulter, Paul Mortenson, Manuel A. Navia, Jean-Francois Pons
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Publication number: 20110136869Abstract: 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: June 1, 2010Publication date: June 9, 2011Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Alessandra Bartolozzi, Eugene Richard Hickey, Doris Riether, Lifen Wu, Renee M. Zindell, Nigel James Blumire, Monika Ermann, Edward Thomas Glenn, Someina Khor, Przemyslaw Zawadzki
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Patent number: 7956075Abstract: The invention relates to thiazole, oxazole, imidazole, isoxazole and isoxazoline derivatives of general formula (I) wherein Het is thiazole, oxazole, imidazole, isoxazole or isoxazoline, n is an integer from 0 to 6, A is notably selected from various optionally substituted aromatic radicals, B is notably hydrogen, alkyl or phenyl, R1 and R2 are notably independently hydrogen, alkyl or cycloalkyl and ? is —NR46R47 or —OR48, R46 and R47 are notably independently hydrogen, alkyl, cycloalkyl or —(CH2)k—COOR51, R51 is notably alkyl or haloalkyl and R48 is notably hydrogen or alkyl. These compounds have advantageous pharmacological properties which allow their use in therapeutics, notably for treating neurodegenerative disorders or pain.Type: GrantFiled: December 11, 2007Date of Patent: June 7, 2011Assignee: Ipsen Pharma S.A.S.Inventors: Pierre-Etienne Chabrier De Lassauniere, Jeremiah Harnett, Dennis Bigg, Anne-Marie Liberatore, Jacques Pommier, Jacques Lannoy, Christophe Thurieau
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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: 20110105566Abstract: The present invention relates to hydroximoyl-tetrazole derivatives, their process of preparation, preparation intermediate compounds, 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.Type: ApplicationFiled: March 18, 2009Publication date: May 5, 2011Inventors: Christian Beier, Jurgen Benting, David Bernier, Isabelle Christian, Pierre-Yves Coqueron, Philippe Desbordes, Christophe Dubost, Pierre Genix, Benoit Hartmann, Andrew Pettinger, Daniela Portz, Arnd Voerste, Ulrike Wachendorff-Neumann
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Publication number: 20110087030Abstract: A new technical process for preparation of enantiomerically pure antifungal compounds of formula I by resolution of the racemates has been disclosed.Type: ApplicationFiled: October 8, 2009Publication date: April 14, 2011Inventor: Milan Soukup
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Publication number: 20110070297Abstract: Compounds, pharmaceutical compositions, kits and methods are provided for use with glucokinase that comprise a compound selected from the group consisting of: wherein the variables are as defined herein.Type: ApplicationFiled: December 1, 2010Publication date: March 24, 2011Applicants: Takeda San Diego, Inc., Takeda Pharmaceutical Company LimitedInventors: Sheldon X. Cao, Jun Feng, Yasuhiro Imaeda, Stephen L. Gwaltney, David J. Hosfield, Nobuyuki Takakura, Mingnam Tang
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Publication number: 20110060018Abstract: N-Substituted (2-substituted-1,3-thiazol)alkyl sulfoximines are effective at controlling insects.Type: ApplicationFiled: November 18, 2010Publication date: March 10, 2011Inventors: Michael R. Loso, Benjamin M. Nugent, Yuanming Zhu, Thomas L. Siddall, Francis E. Tisdell, Jim X. Huang, Zoltan L. Benko
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Publication number: 20110059970Abstract: The present invention relates to new 4-phenyl-1,3-azole derivatives having the general formula (I) wherein R1, R2, R3, R4, X, A, B, and n are variable, in a racemic form, an enantiomeric form or any combinations thereof. These compounds exhibit affinity for cannabinoid receptors and may therefore be used as drugs to treat or prevent pathological states and diseases in which one or more of these receptors are involved. The invention also relates to pharmaceutical compositions containing said products and to the use thereof to prepare a drug.Type: ApplicationFiled: September 11, 2008Publication date: March 10, 2011Applicant: IPSEN PHARMA S.A.S.Inventor: Jeremiah Harnett
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Publication number: 20110053987Abstract: Pegylated pyridinium and thiazolium compounds and methods of their use in medicine, research, industry, agriculture and recreational activities are disclosed. The present invention also provides methods of controlling microbial growth and infection. Additionally, the present invention provides methods of controlling microbial infestations relating to industrial and agricultural uses. The present invention can also be used to control insects.Type: ApplicationFiled: November 8, 2006Publication date: March 3, 2011Inventors: Jeffrey L. Selph, Richard B. Klein, John J. Partridge
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Patent number: 7897782Abstract: N-Substituted sulfoximines are effective at controlling insects.Type: GrantFiled: November 11, 2009Date of Patent: March 1, 2011Assignee: Dow AgroSciences LLCInventors: Yuanming Zhu, Richard B. Rogers, Jim X. Huang
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Publication number: 20110028468Abstract: This invention provides a compound of the formula (I): a pharmaceutically acceptable salt or solvate thereof, wherein R1 is substituted or unsubstituted alkyl or the like, R2 is hydrogen or substituted or unsubstituted alkyl, Ring A is monocyclic or bicyclic aromatic heterocycle, R3 is substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl or substituted or unsubstituted heterocycle, R4 is halogen, cyano, substituted or unsubstituted alkyl, substituted or unsubstituted cycloalkyl or the like, m is an integer between 0 and 2, n is an integer between 0 and 5, R is halogen, oxo, cyano, nitro, substituted or unsubstituted alkyl or the like, and p is an integer between 0 and 2 as novel compounds having NPY Y5 antagonistic activity.Type: ApplicationFiled: April 20, 2009Publication date: February 3, 2011Applicant: Shinonogi & Co., LtdInventors: Masahiro Sakagami, Hiroshi Hashizume, Satoru Tanaka, Takayuki Okuno, Hiroshi Yari, Keisuke Tonogaki, Naoki Kouyama
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Publication number: 20110020566Abstract: A charge transporting, liquid crystal photoalignment material comprising a charge transporting moiety connected through covalent chemical bonds to a surface derivatising moiety, and a photoalignment moiety connected through covalent chemical bonds to a surface derivatising moiety.Type: ApplicationFiled: February 16, 2009Publication date: January 27, 2011Inventor: Gene Carl Koch
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Publication number: 20110015236Abstract: The present invention relates to hydroximoyl-tetrazole derivatives of formula (I), their process of preparation, preparation intermediate compounds, 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.Type: ApplicationFiled: March 18, 2009Publication date: January 20, 2011Inventors: Christian Beier, Jurgen Benting, Isabelle Christian, Pierre-Yves Coqueron, Christophe Dubost, Pierre Genix, Benoit Hartmann, Daniela Portz, Arnd Voerste, Ulrike Wachendorff-Neumann
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Publication number: 20110003992Abstract: A quaternary nitrogen-containing corrosion inhibitor of formula wherein is an aromatic, nitrogen-containing ring of 5 to 14 ring atoms, optionally containing an additional N, O or S ring atom and optionally substituted with one or more alkyl, alkenyl, aryl, arylalkyl, cycloalkyl, amino, aminoalkyl, alkoxy, hydroxylalkyl, or cyano groups, or a mixture thereof; Y is a group of formula —OC(O)R1 or —C(O)R1; L is C1-C10 alkyl, C2-C10 alkenyl or a group of formula —CH2CH(OR2)CH2—; R1 is C8-C20 alkyl or C8-C20 alkenyl; R2 is H or —C(O)R1; R3 and R4 are independently selected from H, alkyl, alkenyl, amino, alkoxy, hydroxylalkyl and cyano; and X is Br, Cl or I is particularly useful for inhibiting corrosion in oil and gas field applications.Type: ApplicationFiled: September 15, 2010Publication date: January 6, 2011Inventor: Laxmikant Tiwari
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Publication number: 20110003827Abstract: A compound of the formula is disclosed as an HIV protease inhibitor. Methods and compositions for inhibiting an HIV infection are also disclosed.Type: ApplicationFiled: December 10, 2004Publication date: January 6, 2011Inventors: Charles A. Flentge, Hui-Ju Chen, David A. DeGoey, William J. Flosi, David J. Grampovnik, Peggy P. Huang, Dale J. Kempf, Larry L. Klein, Allan C. Krueger, Darold L. Madigan, John T. Randolph, Minghua Sun, Ming C. Yeung, Chen Zhao
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Patent number: 7863303Abstract: N-Substituted (2-substituted-1,3-thiazol)alkyl sulfoximines are effective at controlling insects.Type: GrantFiled: August 30, 2007Date of Patent: January 4, 2011Assignee: Dow AgroSciences LLCInventors: Michael R. Loso, Benjamin M. Nugent, Yuanming Zhu, Thomas L. Siddall, Francis E. Tisdell, Jim X. Huang, Zoltan L. Benko
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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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Publication number: 20100311709Abstract: The present invention is directed to 2-[1-phenyl-5-hydroxy or methoxy-4alpha-methyl-hexahydrocyclopenta[f]indazol-5-yl]ethyl phenyl derivatives of formula I (I) as glucocorticoid receptor ligands useful for treating a variety of autoimmune and inflammatory diseases or conditions. Pharmaceutical compositions and methods of use are also included.Type: ApplicationFiled: October 23, 2007Publication date: December 9, 2010Inventors: Christopher J. Bungard, Jesse J. Manikowski, James J. Perkins, Robert Meissner
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Publication number: 20100298346Abstract: The present invention relates to nitro-containing heterocyclic or ring-opening nitrogenous compounds of formula (A), wherein R1, R2, R3, R4, R5, Y, Z, and W are as defined in the specification. The present invention discloses the preparation and the uses of a novel insecticide. Said compound and the derivatives thereof have high insecticidal activity to farm insects including homoptera and Lepidoptera pests, such as aphis, fulgorides, aleyrodids, leafhopper, commom thrips, cotton bollworm, cabbage caterpillar, cabbage moth, cotton leafworm, armyworn and so on.Type: ApplicationFiled: May 28, 2008Publication date: November 25, 2010Applicant: EAST CHINA UNIVERSITY OF SCIENCE AND TECHNOLOGYInventors: Zhong Li, Xuhong Qian, Xusheng Shao, Xiaoyong Xu, Liming Tao, Gonghua Song, Qingchun Huang
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Publication number: 20100298384Abstract: The present invention relates to novel oxazolidinone compounds of formula (I) with antibacterial activity, their pharmaceutically acceptable salts, their stereoisomers, their prodrugs, pharmaceutical compositions comprising the same and to their use as therapeutic agentsType: ApplicationFiled: December 4, 2007Publication date: November 25, 2010Inventors: Mohamed Takhi, Jagattaran Das, Javed Iqbal, Natesan Selvakumar, Sreenivas Kandepu, M. Sitaram Kumar
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Publication number: 20100292187Abstract: The present invention provides compounds, pharmaceutical compositions, and methods of using such compounds or compositions for treating infection by a virus, or for affecting viral IRES activity.Type: ApplicationFiled: June 14, 2010Publication date: November 18, 2010Applicant: PTC THERAPEUTICS, INC.Inventors: Gary M. Karp, Peter Seongwoo Hwang, James J. Takasugi, Hongyu Ren, Richard Gerald Wilde, Anthony A. Turpoff, Alexander Arefolov, Guangming Chen, Jeffrey A. Campbell, Chunshi Li, Steven Paget, Nanjing Zhang, Xiaoyan Zhang, Jin Zhu
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Patent number: 7825155Abstract: Disclosed is a compound represented by the formula (1) below, a prodrug thereof or a pharmaceutically acceptable salt of either, which is useful as a therapeutic, preventive or ameliorating agent for diabetes and the like. (In the formula, R3 represents an optionally substituted carbamoyl group or the like; X represents a hydroxyl group or the like; W1 and W2 independently represent a single bond or methylene; R7 and R8 independently represent a hydrogen atom, an optionally substituted alkyl group or the like; and Ar represents an optionally substituted aryl group or the like.Type: GrantFiled: September 13, 2006Date of Patent: November 2, 2010Assignee: Dainippon Sumitomo Pharma Co., Ltd.Inventors: Teruhisa Tokunaga, Tsuyoshi Takasaki, Kozo Yoshida, Ryu Nagata
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Publication number: 20100274006Abstract: 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: ApplicationFiled: May 4, 2010Publication date: October 28, 2010Applicant: NIPPON SODA CO., LTDInventors: Natsuki Amanokura, Tetsuya Sahara, Hiroshi Suzuki, Yuichi Maekawa, Kiyoshi Katsuura, Yoshihiro Enomoto
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Publication number: 20100267698Abstract: This invention relates to benzimidazoles, pyridylimidazoles and related bicyclic heteroaryl compounds, all of which may be described by of Formula I The invention is particularly related to such compounds that bind with high selectivity and high affinity to the benzodiazepine site of GABAA receptors. This invention also relates to pharmaceutical compositions comprising such compounds and to the use of such compounds in treatment of certain central nervous system (CNS) diseases. Novel processes for preparing compounds of Formula I are disclosed. This invention also relates to the use of benzimidazoles, pyridylimidazoles and related bicyclic heteroaryl compounds of Formula I in combination with one or more other CNS agents to potentiate the effects of the other CNS agents. Additionally this invention relates to the use such compounds as probes for the localization of GABAA receptors in tissue sections.Type: ApplicationFiled: January 5, 2010Publication date: October 21, 2010Inventors: Guiying Li, Pamela Albaugh, Kevin S. Currie, Guolin Cai, Linda M. Gustavson, Kyungae Lee, Alan Hutchison, George D. Maynard, Jun Yuan, Ling Hong Xie, Manuka Ghosh, Nian Liu, George P. Luke, Scott Mitchell, Martin Patrick Allen, Spiros Liras
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Publication number: 20100267743Abstract: In one aspect, the invention relates to compounds of formula I: where RA and RB are as defined in the specification, or a pharmaceutically acceptable salt thereof. The compounds of formula I are serotonin and norepinephrine reuptake inhibitors. 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: April 14, 2010Publication date: October 21, 2010Inventors: Eric L. Stangeland, Priscilla Van Dyke, Daisuke Roland Saito, Jane Schmidt, Lori Jean Patterson, Timothy J. Church, Adam Hughes
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Patent number: 7816537Abstract: Disclosed is a process for the manufacture of a compound of formula (I) wherein Hal represents fluoro or chloro, and R1 and R2 represent, independently from one another, hydrogen or Hal; in which process a compound of formula (II) is converted to a corresponding alkyl, fluoroalkyl or aryl sulfonic acid ester, which is then reacted with an alkali metal nitrite in the presence of a suitable crown ether in a polar non-nucleophilic solvent at a temperature of ?10 to 50° C. to give the compound of formula (I).Type: GrantFiled: November 29, 2006Date of Patent: October 19, 2010Assignee: Basilea Pharmaceutica AGInventors: Marc Muller, Lin Xu
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Publication number: 20100261757Abstract: Certain novel N-(heteroarylalkyl)alkanediamine derivatives have provided unexpected insecticidal and acaricidal activity. These compounds are represented by formula I: wherein Ar, a, b, c, T, W, Y R, Rf, Rg, Rh, Ri, Rj, Rk, Rm, Rn, and R are fully described herein. In addition, compositions comprising an insecticidally effective amount of at least one compound of formula I, and optionally, an effective amount of at least one of a second compound, with at least one insecticidally compatible carrier are also disclosed; along with methods of controlling insects comprising applying said compositions to a locus where insects are present or are expected to be present.Type: ApplicationFiled: January 15, 2007Publication date: October 14, 2010Inventors: John F. Chiarello, Harvey R. Wendt, Najing Zhang, George Theodoridis
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Publication number: 20100249101Abstract: The present invention relates to compounds of formula I, The compounds of formula I are valuable pharmacologically active compounds. They exhibit a strong anti-thrombotic effect and are suitable, for example, for the therapy and prophylaxis of cardio-vascular disorders like thromboembolic diseases or restenoses. They are inhibitors of the blood clotting enzymes, especially factor VIIa and can in general be applied in conditions in which an undesired activity of factor VIIa is present or for the cure or prevention of which an inhibition of factor VIIa is intended. The invention furthermore relates to processes for the preparation of compounds of formula I, their use, in particular as active ingredients in pharmaceuticals, and pharmaceutical preparations comprising them.Type: ApplicationFiled: January 7, 2010Publication date: September 30, 2010Applicant: SANOFI-AVENTISInventors: Henning STEINHAGEN, Hauke SZILLAT, Markus FOLLMANN, Reinhard KIRSCH, Volkmar WEHNER, Hans MATTER, Martin LORENZ, Kent W. Neuenschwander, Anthony C. SCOTESE
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Publication number: 20100240890Abstract: The present invention relates to novel benzamidine derivatives, process for the preparation thereof and pharmaceutical composition comprising the same. The novel benzamidine derivatives of the present invention are useful for the prevention and treatment of osteoporosis, bone fractures and allergic inflammatory diseases.Type: ApplicationFiled: August 4, 2005Publication date: September 23, 2010Inventors: Jin Soo Lee, Seok Hoon Ahn, Young Goo Jin, Sang Mi Jin, Whui-Jung Park, Sae Kwang Ku, Yu Ha Hwang, Pan Soo Kim, Sun Shin Yi, Jei Man Ryu
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Publication number: 20100234398Abstract: N-Substituted (heteroaryl)alkyl sulfilimines are effective at controlling insects.Type: ApplicationFiled: May 26, 2010Publication date: September 16, 2010Applicant: DOW AGROSCIENCES LLCInventors: Michael R. Loso, Benjamin M. Nugent, Yuanming Zhu, Richard B. Rogers, Jim X. Huang, James M. Renga, Zoltan L. Benko, Gregory T. Whiteker, John F. Daeuble, SR.
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Patent number: 7790728Abstract: The present disclosure relates to a compound of formula (I) wherein: A is an optionally substituted monocyclic or polycyclic aryl or heteroaryl group; B is an optionally substituted monocyclic nitrogen-containing heteroaryl group; and either a) R1 and R2 are chosen from a hydrogen atom and specified substituents, or b) R2, R1 and the —NH— group to which R1 is attached, form a moiety chosen from the moiety of formulae (IIa) and (IIb): or a pharmaceutically acceptable salt thereof, or a N-oxide thereof. The present disclosure also relates to a method for treating a subject afflicted with a pathological condition or disease susceptible to amelioration by antagonism of the A2B adenosine receptor.Type: GrantFiled: July 25, 2006Date of Patent: September 7, 2010Assignee: Laboratorios Almirall, S.A.Inventors: Bernat Vidal Juan, Christina Esteve Trias, Lidia Soca Pueyo, Paul Robert Eastwood
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Publication number: 20100216787Abstract: A thiazolylimidazole derivative represented by the formula or a pharmaceutically acceptable salt thereof, and an ALK5 inhibitor, an therapeutic agent for alopecia or a hair growth agent having the above as an active ingredient, wherein: X1 and X2 are different from each other and represent a sulfur atom or a carbon atom; R1 represents a phenyl group; a substituted phenyl group; a phenyl group condensed with a hetero aromatic ring; a pyridyl group; or a pyridyl group condensed with a hetero aromatic ring; R2 represents a hydrogen atom, a halogen atom, an alkyl group having 1 to 6 carbon atoms, an alkyl group having 1 to 6 carbon atoms substituted with 1 to 5 halogen atoms, an alkoxy group having 1 to 6 carbon atoms, an alkanoyl group having 1 to 5 carbon atoms, or a hydroxyalkyl group having 1 to 6 carbon atoms, A represents a group which is represented by the formula.Type: ApplicationFiled: December 22, 2009Publication date: August 26, 2010Applicant: TAISHO PHARMACEUTICAL CO., LTD.Inventors: Masakazu Sato, Yuko Matsunaga, Hajime Asanuma, Hideaki Amada, Takeshi Koami, Tetsuo Takayama, Tetsuya Yabuuchi, Fumiyasu Shiozawa, Hironori Katakai, Hiroki Umemiya, Akiko Ikeda
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Publication number: 20100204480Abstract: The present invention relates to a process for preparing 4-aminobut-2-enolides and also corresponding intermediates and starting compounds which are passed through or used in the process according to the invention.Type: ApplicationFiled: September 5, 2008Publication date: August 12, 2010Applicant: BAYER CROPSCIENCEInventors: Norbert Lui, Jens-Dietmar Heinrich
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Patent number: 7763640Abstract: The present application relates to new substituted oxyguanidines of structure (I) a method for their preparation and their use for the control of animal pests, mainly arthropods, in particular insects.Type: GrantFiled: November 12, 2005Date of Patent: July 27, 2010Assignee: Bayer CorpScience AGInventors: Peter Jeschke, Peter Lösel, Ralf Nauen, Peter Marczok, Christian Arnold, Erich Sanwald
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Publication number: 20100130446Abstract: The present invention provides a compound represented by the formula (I): wherein each symbol is as defined in the specification, or a salt thereof. The compound of the present invention has a glucokinase activity, and is useful as a medicament such as an agent for the prophylaxis or treatment of diabetes, obesity and the like, and the like.Type: ApplicationFiled: April 25, 2008Publication date: May 27, 2010Applicant: TAKEDA PHARMACEUTICAS COMPANY LIMITEDInventors: Tsuneo Yasuma, Kentaro Hashimoto, Masahiro Ito
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Publication number: 20100113538Abstract: N-hydroxy-4-{5-[4-(5-isopropyl-2-methyl-1,3-thiazol-4-yl)phenoxy]pentoxy}benzamidine 2 ethansulfonic acid salt, a process for the preparation thereof, a pharmaceutical composition for preventing and treating osteoporosis, bone fractures or allergic inflammatory diseases, comprising the same, and an oral formulation for preventing and treating osteoporosis, bone fractures or allergic inflammatory diseases, comprising the same are described.Type: ApplicationFiled: April 21, 2008Publication date: May 6, 2010Applicant: DONG WHA PHARMACEUTICAL CO., LTD.Inventors: Jin Soo Lee, Soon Ki Cho, Seoung Kyoo Sung, Young Goo Jin, Jae Hoon Park, Bo Kyung Kim, Ja Hyun Cha, Eun Hee Cho, Jei Man Ryu
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Publication number: 20100105744Abstract: The present application relates to novel 7-sulfanylmethyl-, 7-sulfinylmethyl- and 7-sulfonylmethylindole derivatives, processes for the preparation thereof, the use thereof alone or in combinations for the treatment and/or prevention of diseases, and the use thereof for the manufacture of medicaments for the treatment and/or prevention of diseases, especially for the treatment and/or prevention of cardiovascular disorders.Type: ApplicationFiled: June 24, 2009Publication date: April 29, 2010Applicant: BAYER SCHERING PHARMA AKTIENGESELLSCHAFTInventors: Peter Kolkhof, Astrid Brüns, Kai Thede, Karl-Heinz Schlemmer, Alexander Hillisch, Dieter Lang, Michael Gerisch, Andreas Göller, Rolf Grosser, Carsten Schmeck, Elisabeth Woltering, Olaf Prien, Holger Paulsen, Armin Kern
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Patent number: 7687490Abstract: An objective of the present invention is to provide compounds that are effective against various resistant bacteria which cause current clinical problems, for example, pneumococci including penicillin resistant Streptococcus pneumoneae (PRSP), Haemophilus influenzae including bata-lactamase-nonproducing ampicillin-resistant Haemophilus influenzae (BLNAR), and Moraxella (Branhamella) catarrhalis.Type: GrantFiled: April 12, 2006Date of Patent: March 30, 2010Assignee: Meiji Seika Kaisha, Ltd.Inventors: Takahisa Maruyama, Yuko Kano, Takashi Ando, Takehiko Sawabe, Nobuyoshi Baba, Hiromi Takata, Hisashi Suzuki, Kazuhiro Aihara, Toshiki Fujita
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Publication number: 20100076032Abstract: N-Substituted sulfoximines are effective at controlling insects.Type: ApplicationFiled: November 11, 2009Publication date: March 25, 2010Applicant: DOW AGROSCIENCES LLCInventors: Yuanming Zhu, Richard Brewer Rogers, Jim Xinpei Huang
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Publication number: 20100056579Abstract: N-Substituted sulfoximines are effective at controlling insects.Type: ApplicationFiled: November 11, 2009Publication date: March 4, 2010Applicant: DOW AGROSCIENCES LLCInventors: Yuanming Zhu, Richard Brewer Rogers, Jim Xinpei Huang