Nitrogen Attached Indirectly To The Thiazole Ring By Nonionic Bonding Patents (Class 548/205)
  • Publication number: 20110207714
    Abstract: The biphenyic compounds of formula (I) are serotonin modulators useful in the treatment of serotonin-mediated diseases.
    Type: Application
    Filed: October 29, 2009
    Publication date: August 25, 2011
    Inventors: Nicholas I. Carruthers, Brock T. Shireman, Vi T. Tran, Victoria D. Wong, Jill A. Jablonowski, Wenying Chai
  • Publication number: 20110190335
    Abstract: 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: Application
    Filed: April 15, 2009
    Publication date: August 4, 2011
    Inventors: Tsuneo Yasuma, Osamu Ujikawa
  • Publication number: 20110184186
    Abstract: 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: Application
    Filed: April 1, 2011
    Publication date: July 28, 2011
    Applicant: Seoul National University Industry Foundation
    Inventors: Heon Joong Kang, Jung Yeob Ham
  • Publication number: 20110183953
    Abstract: 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: Application
    Filed: November 15, 2010
    Publication date: July 28, 2011
    Inventors: Marcus F. Boehm, Esther Martinborough, Enugurthi Brahmachary, Manisha Moorjani, Junko Tamiya, Liming Huang, Adam Richard Yeager
  • Publication number: 20110178133
    Abstract: 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: Application
    Filed: October 15, 2008
    Publication date: July 21, 2011
    Inventors: 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
  • Patent number: 7982036
    Abstract: 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: Grant
    Filed: October 17, 2008
    Date of Patent: July 19, 2011
    Assignee: Avila Therapeutics, Inc.
    Inventors: Juswinder Singh, Shomir Ghosh, Arthur F. Kluge, Russell C. Petter, Richland W. Tester
  • Publication number: 20110172434
    Abstract: 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: Application
    Filed: March 21, 2011
    Publication date: July 14, 2011
    Applicant: Ipsen Pharma S.A.S.
    Inventors: Pierre-Etienne CHABRIER DE LASSAUNIERE, Jeremiah Harnett, Dennis Bigg, Anne-Marie Liberatore, Jacques Pommier, Jacques Lannoy, Christophe Thurieau
  • Patent number: 7977332
    Abstract: 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: Grant
    Filed: December 2, 2004
    Date of Patent: July 12, 2011
    Assignee: FMC Corporation
    Inventors: David M. Roush, John F. Chiarello, Jianming Yu, Benjamin J. Dugan, George Theodoridis, Manorama M. Patel, Walter H. Yeager, Steven W. Szczepanski
  • Patent number: 7973045
    Abstract: The invention provides anhydrous forms of dasatinib, methods for their preparation, and pharmaceutical compositions thereof.
    Type: Grant
    Filed: June 14, 2010
    Date of Patent: July 5, 2011
    Assignee: 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
  • Publication number: 20110152232
    Abstract: Compounds that modulate GHS-R are described, for examples compounds formula (I)
    Type: Application
    Filed: October 26, 2010
    Publication date: June 23, 2011
    Inventors: Jeffrey O. Saunders, Thomas Coulter, Paul Mortenson, Manuel A. Navia, Jean-Francois Pons
  • Publication number: 20110136869
    Abstract: 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: Application
    Filed: June 1, 2010
    Publication date: June 9, 2011
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: Alessandra Bartolozzi, Eugene Richard Hickey, Doris Riether, Lifen Wu, Renee M. Zindell, Nigel James Blumire, Monika Ermann, Edward Thomas Glenn, Someina Khor, Przemyslaw Zawadzki
  • Patent number: 7956075
    Abstract: 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: Grant
    Filed: December 11, 2007
    Date of Patent: June 7, 2011
    Assignee: Ipsen Pharma S.A.S.
    Inventors: Pierre-Etienne Chabrier De Lassauniere, Jeremiah Harnett, Dennis Bigg, Anne-Marie Liberatore, Jacques Pommier, Jacques Lannoy, Christophe Thurieau
  • Patent number: 7943803
    Abstract: 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: Grant
    Filed: May 4, 2010
    Date of Patent: May 17, 2011
    Assignee: Nippon Soda Co., Ltd.
    Inventors: Natsuki Amanokura, Tetsuya Sahara, Hiroshi Suzuki, Yuichi Maekawa, Kiyoshi Katsuura, Yoshihiro Enomoto
  • Publication number: 20110105566
    Abstract: 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: Application
    Filed: March 18, 2009
    Publication date: May 5, 2011
    Inventors: 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
  • Publication number: 20110087030
    Abstract: A new technical process for preparation of enantiomerically pure antifungal compounds of formula I by resolution of the racemates has been disclosed.
    Type: Application
    Filed: October 8, 2009
    Publication date: April 14, 2011
    Inventor: Milan Soukup
  • Publication number: 20110070297
    Abstract: 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: Application
    Filed: December 1, 2010
    Publication date: March 24, 2011
    Applicants: Takeda San Diego, Inc., Takeda Pharmaceutical Company Limited
    Inventors: Sheldon X. Cao, Jun Feng, Yasuhiro Imaeda, Stephen L. Gwaltney, David J. Hosfield, Nobuyuki Takakura, Mingnam Tang
  • Publication number: 20110060018
    Abstract: N-Substituted (2-substituted-1,3-thiazol)alkyl sulfoximines are effective at controlling insects.
    Type: Application
    Filed: November 18, 2010
    Publication date: March 10, 2011
    Inventors: Michael R. Loso, Benjamin M. Nugent, Yuanming Zhu, Thomas L. Siddall, Francis E. Tisdell, Jim X. Huang, Zoltan L. Benko
  • Publication number: 20110059970
    Abstract: 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: Application
    Filed: September 11, 2008
    Publication date: March 10, 2011
    Applicant: IPSEN PHARMA S.A.S.
    Inventor: Jeremiah Harnett
  • Publication number: 20110053987
    Abstract: 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: Application
    Filed: November 8, 2006
    Publication date: March 3, 2011
    Inventors: Jeffrey L. Selph, Richard B. Klein, John J. Partridge
  • Patent number: 7897782
    Abstract: N-Substituted sulfoximines are effective at controlling insects.
    Type: Grant
    Filed: November 11, 2009
    Date of Patent: March 1, 2011
    Assignee: Dow AgroSciences LLC
    Inventors: Yuanming Zhu, Richard B. Rogers, Jim X. Huang
  • Publication number: 20110028468
    Abstract: 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: Application
    Filed: April 20, 2009
    Publication date: February 3, 2011
    Applicant: Shinonogi & Co., Ltd
    Inventors: Masahiro Sakagami, Hiroshi Hashizume, Satoru Tanaka, Takayuki Okuno, Hiroshi Yari, Keisuke Tonogaki, Naoki Kouyama
  • Publication number: 20110020566
    Abstract: 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: Application
    Filed: February 16, 2009
    Publication date: January 27, 2011
    Inventor: Gene Carl Koch
  • Publication number: 20110015236
    Abstract: 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: Application
    Filed: March 18, 2009
    Publication date: January 20, 2011
    Inventors: Christian Beier, Jurgen Benting, Isabelle Christian, Pierre-Yves Coqueron, Christophe Dubost, Pierre Genix, Benoit Hartmann, Daniela Portz, Arnd Voerste, Ulrike Wachendorff-Neumann
  • Publication number: 20110003992
    Abstract: 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: Application
    Filed: September 15, 2010
    Publication date: January 6, 2011
    Inventor: Laxmikant Tiwari
  • Publication number: 20110003827
    Abstract: A compound of the formula is disclosed as an HIV protease inhibitor. Methods and compositions for inhibiting an HIV infection are also disclosed.
    Type: Application
    Filed: December 10, 2004
    Publication date: January 6, 2011
    Inventors: 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
  • Patent number: 7863303
    Abstract: N-Substituted (2-substituted-1,3-thiazol)alkyl sulfoximines are effective at controlling insects.
    Type: Grant
    Filed: August 30, 2007
    Date of Patent: January 4, 2011
    Assignee: Dow AgroSciences LLC
    Inventors: Michael R. Loso, Benjamin M. Nugent, Yuanming Zhu, Thomas L. Siddall, Francis E. Tisdell, Jim X. Huang, Zoltan L. Benko
  • Publication number: 20100331302
    Abstract: 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: Application
    Filed: July 8, 2010
    Publication date: December 30, 2010
    Applicant: 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
  • Publication number: 20100311709
    Abstract: 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: Application
    Filed: October 23, 2007
    Publication date: December 9, 2010
    Inventors: Christopher J. Bungard, Jesse J. Manikowski, James J. Perkins, Robert Meissner
  • Publication number: 20100298346
    Abstract: 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: Application
    Filed: May 28, 2008
    Publication date: November 25, 2010
    Applicant: EAST CHINA UNIVERSITY OF SCIENCE AND TECHNOLOGY
    Inventors: Zhong Li, Xuhong Qian, Xusheng Shao, Xiaoyong Xu, Liming Tao, Gonghua Song, Qingchun Huang
  • Publication number: 20100298384
    Abstract: 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 agents
    Type: Application
    Filed: December 4, 2007
    Publication date: November 25, 2010
    Inventors: Mohamed Takhi, Jagattaran Das, Javed Iqbal, Natesan Selvakumar, Sreenivas Kandepu, M. Sitaram Kumar
  • Publication number: 20100292187
    Abstract: 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: Application
    Filed: June 14, 2010
    Publication date: November 18, 2010
    Applicant: 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
  • Patent number: 7825155
    Abstract: 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: Grant
    Filed: September 13, 2006
    Date of Patent: November 2, 2010
    Assignee: Dainippon Sumitomo Pharma Co., Ltd.
    Inventors: Teruhisa Tokunaga, Tsuyoshi Takasaki, Kozo Yoshida, Ryu Nagata
  • Publication number: 20100274006
    Abstract: 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: Application
    Filed: May 4, 2010
    Publication date: October 28, 2010
    Applicant: NIPPON SODA CO., LTD
    Inventors: Natsuki Amanokura, Tetsuya Sahara, Hiroshi Suzuki, Yuichi Maekawa, Kiyoshi Katsuura, Yoshihiro Enomoto
  • Publication number: 20100267698
    Abstract: 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: Application
    Filed: January 5, 2010
    Publication date: October 21, 2010
    Inventors: 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
  • Publication number: 20100267743
    Abstract: 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: Application
    Filed: April 14, 2010
    Publication date: October 21, 2010
    Inventors: Eric L. Stangeland, Priscilla Van Dyke, Daisuke Roland Saito, Jane Schmidt, Lori Jean Patterson, Timothy J. Church, Adam Hughes
  • Patent number: 7816537
    Abstract: 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: Grant
    Filed: November 29, 2006
    Date of Patent: October 19, 2010
    Assignee: Basilea Pharmaceutica AG
    Inventors: Marc Muller, Lin Xu
  • Publication number: 20100261757
    Abstract: 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: Application
    Filed: January 15, 2007
    Publication date: October 14, 2010
    Inventors: John F. Chiarello, Harvey R. Wendt, Najing Zhang, George Theodoridis
  • Publication number: 20100249101
    Abstract: 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: Application
    Filed: January 7, 2010
    Publication date: September 30, 2010
    Applicant: SANOFI-AVENTIS
    Inventors: Henning STEINHAGEN, Hauke SZILLAT, Markus FOLLMANN, Reinhard KIRSCH, Volkmar WEHNER, Hans MATTER, Martin LORENZ, Kent W. Neuenschwander, Anthony C. SCOTESE
  • Publication number: 20100240890
    Abstract: 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: Application
    Filed: August 4, 2005
    Publication date: September 23, 2010
    Inventors: 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
  • Publication number: 20100234398
    Abstract: N-Substituted (heteroaryl)alkyl sulfilimines are effective at controlling insects.
    Type: Application
    Filed: May 26, 2010
    Publication date: September 16, 2010
    Applicant: DOW AGROSCIENCES LLC
    Inventors: 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.
  • Patent number: 7790728
    Abstract: 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: Grant
    Filed: July 25, 2006
    Date of Patent: September 7, 2010
    Assignee: Laboratorios Almirall, S.A.
    Inventors: Bernat Vidal Juan, Christina Esteve Trias, Lidia Soca Pueyo, Paul Robert Eastwood
  • Publication number: 20100216787
    Abstract: 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: Application
    Filed: December 22, 2009
    Publication date: August 26, 2010
    Applicant: 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
  • Publication number: 20100204480
    Abstract: 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: Application
    Filed: September 5, 2008
    Publication date: August 12, 2010
    Applicant: BAYER CROPSCIENCE
    Inventors: Norbert Lui, Jens-Dietmar Heinrich
  • Patent number: 7763640
    Abstract: 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: Grant
    Filed: November 12, 2005
    Date of Patent: July 27, 2010
    Assignee: Bayer CorpScience AG
    Inventors: Peter Jeschke, Peter Lösel, Ralf Nauen, Peter Marczok, Christian Arnold, Erich Sanwald
  • Publication number: 20100130446
    Abstract: 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: Application
    Filed: April 25, 2008
    Publication date: May 27, 2010
    Applicant: TAKEDA PHARMACEUTICAS COMPANY LIMITED
    Inventors: Tsuneo Yasuma, Kentaro Hashimoto, Masahiro Ito
  • Publication number: 20100113538
    Abstract: 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: Application
    Filed: April 21, 2008
    Publication date: May 6, 2010
    Applicant: 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
  • Publication number: 20100105744
    Abstract: 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: Application
    Filed: June 24, 2009
    Publication date: April 29, 2010
    Applicant: BAYER SCHERING PHARMA AKTIENGESELLSCHAFT
    Inventors: 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
  • Patent number: 7687490
    Abstract: 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: Grant
    Filed: April 12, 2006
    Date of Patent: March 30, 2010
    Assignee: Meiji Seika Kaisha, Ltd.
    Inventors: Takahisa Maruyama, Yuko Kano, Takashi Ando, Takehiko Sawabe, Nobuyoshi Baba, Hiromi Takata, Hisashi Suzuki, Kazuhiro Aihara, Toshiki Fujita
  • Publication number: 20100076032
    Abstract: N-Substituted sulfoximines are effective at controlling insects.
    Type: Application
    Filed: November 11, 2009
    Publication date: March 25, 2010
    Applicant: DOW AGROSCIENCES LLC
    Inventors: Yuanming Zhu, Richard Brewer Rogers, Jim Xinpei Huang
  • Publication number: 20100056579
    Abstract: N-Substituted sulfoximines are effective at controlling insects.
    Type: Application
    Filed: November 11, 2009
    Publication date: March 4, 2010
    Applicant: DOW AGROSCIENCES LLC
    Inventors: Yuanming Zhu, Richard Brewer Rogers, Jim Xinpei Huang