Having -c(=x)-, Wherein X Is Chalcogen, Bonded Directly To The Thiazole Ring Patents (Class 548/200)
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Publication number: 20100234431Abstract: A compound of the following formula: wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R11, R12, X, Y, and Z are as defined herein. Also disclosed is a method for inhibiting actively of fibroblast activation protein or for treating cancer or inflammation conditions with such a compound.Type: ApplicationFiled: February 19, 2010Publication date: September 16, 2010Applicant: National Health Research InstitutesInventors: Weir-Tong Jiaang, Xin Chen
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Publication number: 20100226882Abstract: The present invention discloses compounds of Formula (I), or pharmaceutically acceptable salts, esters, or prodrugs thereof: which inhibit RNA-containing virus, particularly the hepatitis C virus (HCV). Consequently, the compounds of the present invention interfere with the life cycle of the hepatitis C virus and are also useful as antiviral agents. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from HCV infection. The invention also relates to methods of treating an HCV infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention.Type: ApplicationFiled: February 17, 2010Publication date: September 9, 2010Inventors: Yat Sun Or, Xiaowen Peng, Ce Wang, Lu Ying, Datong Tang, Yao-Ling Qiu
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Publication number: 20100227892Abstract: Methods of using di, tri, and tetracyclic acylhydrazide derivatives and analogs, as well as pharmaceutical compositions containing the same, for the treatment or prophylaxis of viral infections and diseases associated therewith, particularly those viral infections and associated diseases caused by the orthopoxvirus.Type: ApplicationFiled: April 1, 2010Publication date: September 9, 2010Applicant: Siga Technologies Inc.Inventors: Robert Jordan, Thomas R. Bailey, Susan R. Rippin
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Publication number: 20100221215Abstract: The present invention discloses compounds of Formula (I), or pharmaceutically acceptable salts, esters, or prodrugs thereof: which inhibit RNA-containing virus, particularly the hepatitis C virus (HCV). Consequently, the compounds of the present invention interfere with the life cycle of the hepatitis C virus and are also useful as antiviral agents. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from HCV infection. The invention also relates to methods of treating an HCV infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention.Type: ApplicationFiled: February 9, 2010Publication date: September 2, 2010Inventors: Yao-Ling Qiu, Ce Wang, Xiaowen Peng, Lu Ying, Yat Sun Or
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Publication number: 20100221214Abstract: The present invention discloses compounds of Formula (I), or pharmaceutically acceptable salts, esters, or prodrugs thereof: which inhibit RNA-containing virus, particularly the hepatitis C virus (HCV). Consequently, the compounds of the present invention interfere with the life cycle of the hepatitis C virus and are also useful as antiviral agents. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from HCV infection. The invention also relates to methods of treating an HCV infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention.Type: ApplicationFiled: February 9, 2010Publication date: September 2, 2010Inventors: Yat Sun Or, Ce Wang, Xiaowen Peng, Lu Ying, Yao-Ling Qiu
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Publication number: 20100222389Abstract: Compounds of the formula (I), in which the substituents are as defined in claim 1 are suitable for use as microbiocides.Type: ApplicationFiled: June 13, 2008Publication date: September 2, 2010Applicant: SYNGENTA CROP PROTECTION, INC.Inventors: Harald Walter, Daniel Stierli, Hans Tobler
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Publication number: 20100216849Abstract: This invention relates to novel biphenylcarboxamides of the formula (I) in which R, Z, X, Y, m, n and A are as defined in the disclosure, to a plurality of processes for preparing these compounds and their use for controlling unwanted microorganisms, and to novel intermediates and their preparation.Type: ApplicationFiled: April 30, 2010Publication date: August 26, 2010Inventors: Ralf Dunkel, Hans-Ludwig Elbe, Heiko Rieck, Ulrike Wachendorff-Neumann, Peter Dahmen, Peter Lösel, Karl-Heinz Kuck, Astrid Mauler-Machnik, Jörg Nico Greul
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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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Patent number: 7777036Abstract: Methods of treating an SCD-mediated disease or condition in a mammal, preferably a human, are disclosed, wherein the methods comprise administering to a mammal in need thereof a compound of formula (I) where y, G, K, L, M, W, V, R2, R3, R4a, R6, R6a, R7, R7a, R8 and R8a are defined herein. Pharmaceutical compositions comprising the compounds of formula (I) are also disclosed.Type: GrantFiled: September 20, 2005Date of Patent: August 17, 2010Assignee: Xenon Pharmaceuticals Inc.Inventors: Rajender Kamboj, Zaihui Zhang, Jianmin Fu, Mehran Seid Bagherzadeh, Serguei Sviridov, Sultan Chowdhury, Shifeng Liu, Vishnumurthy Kodumuru
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Publication number: 20100204482Abstract: The invention relates to a fungicidally active compound of formula (I): where Het is a 5- or 6-membered heterocyclic ring containing one to three heteroatoms, each independently selected from oxygen, nitrogen and sulphur, the ring being substituted by the groups R6, R7 and R8; R1 is hydrogen, C1-4 alkyl, C1-4 haloalkyl, C1-4alkoxy, C1-4haloalkoxy, CH2C?CR9, CH2CR10?CHR11, CH?C?CH2 or COR12; R2 and R3 are each, independently, hydrogen, halo, C1-4 alkyl, C1-4 alkoxy, C1-4 haloalkyl or C1-4 haloalkoxy; R4 and R5 are each independently selected from halo, cyano and nitro; or one of R4 and R5 is hydrogen and the other is selected from halo, cyano and nitro; R6, R7 and R8 are each, independently, hydrogen, halo, cyano, nitro, C1-4 alkyl, C1-4 haloalkyl, C1-4 alkoxy(C1-4)alkyl, C1-4haloalkoxy(C1-4)alkyl or C1-4haloalkoxy, provided that at least one of R6, R7 and R8 is not hydrogen; R9, R10 and R11 are each, independently, hydrogen, halo, C1-4 alkyl, C1-4 haloalkyl or C1-4 alkoxy(C1-4)alkyl; and R12 is hydrogen,Type: ApplicationFiled: April 23, 2010Publication date: August 12, 2010Applicant: SYNGENTA CROP PROTECTION, INC.Inventors: Hans Tobler, Harald Walter, Josef Ehrenfreund, Camilla Corsi
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Publication number: 20100197644Abstract: Compounds of formula (I): The present invention relates to novel indazolyl ester or amide derivatives, to pharmaceutical compositions comprising such derivatives, to processes for preparing such novel derivatives and to the use of such derivatives as medicamentsType: ApplicationFiled: December 21, 2009Publication date: August 5, 2010Inventors: Markus Berger, Jan Dahmén, Karl Edman, Anders Eriksson, Balint Gabos, Thomas Hansson, Martin Hemmerling, Krister Henriksson, Svetlana Ivanova, Matti Lepistö, Darren McKerrecher, Magnus Munck af Rosenschöld, Stinabritt Nilsson, Hartmut Rehwinkel, Camilla Taflin
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Publication number: 20100190779Abstract: Compounds of formula I: wherein X, R2, R3, R5 and R6 are defined herein, are useful as inhibitors of the hepatitis C virus NS5B polymerase.Type: ApplicationFiled: July 31, 2008Publication date: July 29, 2010Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Pierre L. Beaulieu, Paul J. Edwards, Martin Poirier, Jean Rancourt, Timothy A. Stammers
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Publication number: 20100190688Abstract: Compounds, compositions and methods for treatment of hyperproliferative diseases, such as cancer are provided.Type: ApplicationFiled: July 12, 2005Publication date: July 29, 2010Inventors: Bin Chao, Thomas L. Deckwerth, Paul S. Furth, Steven D. Linton, Alfred P. Spada, Brett R. Ullman, Michael I. Weinhouse
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Publication number: 20100179119Abstract: Novel compounds inhibiting the integrin ?2?1/GPIa-IIa receptor are disclosed. Also disclosed are pharmaceutical compositions containing the compounds, as well as methods of their therapeutic use. The compounds disclosed are useful, inter alia, as inhibitors of integrin ?2?1/GPIa-IIa-mediated activity.Type: ApplicationFiled: September 24, 2009Publication date: July 15, 2010Inventors: William F. DeGrado, Meredith W. Miller, Sandeep Basra, Joel S. Bennett, Sungwook Choi
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Patent number: 7745464Abstract: The present invention relates to heterocyclic compounds that bind to Bcl proteins and inhibit Bcl function, compositions comprising such compounds, and methods for treating and modulating disorders associated with hyperproliferation, such as cancer.Type: GrantFiled: December 15, 2006Date of Patent: June 29, 2010Inventors: Alfredo C. Castro, Michael J. Grogan, Edward B. Holson, Brian T. Hopkins, Nii O. Koney, Stephane Peluso, Daniel A. Snyder
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Publication number: 20100158996Abstract: A novel therapeutic agent for hyperlipidemia, which is an ester compound represented by the formula (1?) (wherein R1 and R2 are each hydrogen atom or optionally substituted aryl, etc.; X is —COO— or —CON(R10)—; R3 and R4 are each hydrogen atom, C1-C6 alkyl or C1-C6 alkoxy, etc.; R5, R6 and R7 are each hydrogen atom, C1-C6 alkyl or C1-C6 alkoxy, etc.; R9 and R9 are each independently hydrogen atom, C1-C6 alkyl, —CON(R18) (R19) or —COO(R20), etc.; ring A, ring B and ring C are each independently aryl or heterocycle residue, etc.; Alk1 and Alk2 are each independently alkanediyl, etc.; l and m are each an integer of 0 or 1 to 3) or a prodrug thereof, or a pharmaceutically acceptable salt of either. The therapeutic agent selectively inhibits MTP in the small intestine, thus causes no such side effect as a fatty liver.Type: ApplicationFiled: February 12, 2010Publication date: June 24, 2010Inventors: Atsushi Hagiwara, Yasuhiro Ohe, Naoya Odani, Shizue Watanabe, Taku Ikenogami, Takashi Kawai, Kenya Madono, Toshio Taniguchi
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Publication number: 20100160327Abstract: The present invention relates to a novel class of modified malonate derivatives. The modified malonate compounds can be used to treat cancer. The modified malonate compounds can also inhibit histone deacetylase and are suitable for use in selectively inducing terminal differentiation, and arresting cell growth and/or apoptosis of neoplastic cells, thereby inhibiting proliferation of such cells. Thus, the compounds of the present invention are useful in treating a patient having a tumor characterized by proliferation of neoplastic cells. The compounds of the invention may also be useful in the prevention and treatment of TRX-mediated diseases, such as autoimmune, allergic and inflammatory diseases, and in the prevention and/or treatment of diseases of the central nervous system (CNS), such as neurodegenerative diseases.Type: ApplicationFiled: June 21, 2006Publication date: June 24, 2010Inventors: Jonathan Grimm, Paul Harrington, Richard Heidebrecht, JR., Thomas Miller, Karin Otte, Phieng Siliphaivanh, David Sloman, Matthew Stanton, Kevin Wilson, David Witter, Solomon Kattar, Paul Tempest
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Publication number: 20100160302Abstract: The present invention relates to novel compounds representated by formula (I), where R, R1, R2, R3, X, Y, m, n are as defined. The present invention relates to compounds of the general formula I their derivatives, their analogs, their tautomeric forms, their stereoisomers, their diastereomers, their bioisosteres, their polymorphs, their pharmaceutically acceptable salts and pharmaceutically acceptable compositions containing them which are predominantly dipeptidyl peptidase IV inhibitors. The present invention also relates to the processes for the preparation of novel compounds of formula (I) and their use in treating type II diabetes and diabetic complications thereof and also for treating dislipidemia, hypercholesterolemia, obesity and hyperglycemia.Type: ApplicationFiled: March 30, 2007Publication date: June 24, 2010Inventors: Balasubramanian Gopalan, Dhamjewar Ravi, Mohammed Rasheed, Swamy Hosamane Keshavapura HosamaneSreedhara, Ahmad Ishtiyaque
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Patent number: 7732469Abstract: The invention relates to a fungicidally active compound of formula (I): where Het is a 5- or 6-membered heterocyclic ring containing one to three heteroatoms, each independently selected from oxygen, nitrogen and sulphur, the ring being substituted by the groups R6, R7 and R8; R1 is hydrogen, C1-4 alkyl, C1-4 haloalkyl, C1-4 alkoxy, C1-4 haloalkoxy, CH2 C?CR9, CH2 CR10?CHR11, CH?C?CH2 or COR12; R2 and R3 are each, independently, hydrogen, halo, C1-4 alkyl, C1-4 alkoxy, C1-4 haloalkyl or C1-4 haloalkoxy; R4 and R5 are each independently selected from halo, cyano and nitro; or one of R4 and R5 is hydrogen and the other is selected from halo, cyano and nitro; R6, R7 and R8 are each, independently, hydrogen, halo, cyano, nitro, C1-4 alkyl, C1-4 haloalkyl, C1-4 alkoxy(C1-4)alkyl, C1-4 haloalkoxy(C1-4)alkyl or C1-4 haloalkoxy, provided that at least one of R6, R7 and R8 is not hydrogen; R9, R10 and R11 are each, independently, hydrogen, halo, C1-4 alkyl, C1-4 haloalkyl or C1-4 alkoxy(C1-4)alkyl; and R12 is hydrogenType: GrantFiled: October 23, 2006Date of Patent: June 8, 2010Assignee: Syngenta Crop Protection, Inc.Inventors: Hans Tobler, Harald Walter, Josef Ehrenfreund, Camilla Corsi
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Publication number: 20100137336Abstract: The present invention relates to novel compounds of Formula (I), wherein X1, X2, X3, X4, Am and Bn are defined as in Formula (I); invention compounds are modulators of metabotropic glutamate receptors—subtype 4 (“mGluR4”) which are useful for the treatment or prevention of central nervous system disorders as well as other disorders modulated by mGluR4 receptors. The invention is also directed to pharmaceutical compositions and the use of such compounds in the manufacture of medicaments, as well as to the use of such compounds for the prevention and treatment of such diseases in which mGluR4 is involved.Type: ApplicationFiled: July 10, 2008Publication date: June 3, 2010Inventor: Christelle Boléa
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Publication number: 20100137298Abstract: The present invention relates to biaryl sulfonamides and their use as, for example, metalloproteinase inhibitors.Type: ApplicationFiled: June 13, 2008Publication date: June 3, 2010Applicant: WyethInventors: Jeremy Ian Levin, Thomas Saltmarsh Rush, III, Frank Lovering, Yonghan Hu, Jianchang Li, Wei Li, Jun Jun Wu, Rajeev Hotchandani, Jason Shaoyun Xiang, Xuemei Du, Derek Cecil Cole, Steve Yikkai Tam
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Patent number: 7728019Abstract: This invention relates to novel biphenylcarboxamides of the formula (I) in which R, Z, X, Y, m, n and A are as defined in the disclosure, to a plurality of processes for preparing these compounds and their use for controlling unwanted microorganisms, and to novel intermediates and their preparation.Type: GrantFiled: December 1, 2003Date of Patent: June 1, 2010Assignee: Bayer CropScience AGInventors: Ralf Dunkel, Hans-Ludwig Elbe, Heiko Rieck, Ulrike Wachendorff-Neumann, Peter Dahmen, Peter Lösel, Karl-Heinz Kuck, Astrid Mauler-Machnik, Jörg Nico Greul
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Patent number: 7714126Abstract: Provided herein are compounds of the formula (I): as well as pharmaceutically acceptable salts thereof, wherein the substituents are as those disclosed in the specification. These compounds, and the pharmaceutical compositions containing them, are useful for the treatment of diseases such as, for example, obesity, type II diabetes mellitus and metabolic syndrome.Type: GrantFiled: November 17, 2006Date of Patent: May 11, 2010Assignee: Via Pharmaceuticals, Inc.Inventors: David Robert Bolin, Adrian Wai-Hing Cheung, Fariborz Firooznia, Matthew Michael Hamilton, Shiming Li, Lee Apostle McDermott, Yimin Qian, Weiya Yun
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Publication number: 20100113531Abstract: The invention relates to novel thiazolidine derivatives of the formula (I) wherein A and R1 are as described in the description and their use as medicaments, especially as orexin receptor antagonists.Type: ApplicationFiled: March 25, 2008Publication date: May 6, 2010Inventors: Hamed Aissaoui, Christoph Boss, Markus Gude, Ralf Koberstein, Thierry Sifferlen
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Patent number: 7705025Abstract: The present invention provides a novel compound of Formula (I) or a pharmaceutically acceptable salt thereof, having histamine-H3 receptor antagonist or inverse agonist activity, as well as methods for preparing such compounds. In another, embodiment, the invention discloses pharmaceutical compositions comprising compounds of Formula (I) as well as methods of using them to treat obesity, cognitive deficiencies, narcolepsy, and other histamine H3 receptor-related diseases.Type: GrantFiled: August 15, 2005Date of Patent: April 27, 2010Assignee: Eli Lilly and CompanyInventors: Don Richard Finley, Terry Patrick Finn, Philip Arthur Hipskind, William Joseph Hornback, Cynthia Darshini Jesudason, Takako Takakuwa
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Publication number: 20100099677Abstract: The present invention relates to compositions and methods for treating a disease in an animal, which disease is responsive to inhibiting of functional cystic fibrosis transmembrane conductance regulator (CFTR) polypeptide by administering to a mammal in need thereof an effective amount of a compound defined herein (including those compounds set forth in Tables 1-2 or encompassed by formulas I-V) or compositions thereof, thereby treating the disease. The present invention particularly, relates to a method of treating diarrhea and polycystic kidney disease.Type: ApplicationFiled: April 20, 2009Publication date: April 22, 2010Inventor: Kevin James Doyle
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Publication number: 20100093733Abstract: Compounds of formula (I): or pharmaceutically acceptable salts and esters thereof, are useful for the treatment of obesity, type II diabetes and the metabolic syndrome.Type: ApplicationFiled: February 15, 2008Publication date: April 15, 2010Applicant: PROSIDION LIMITEDInventors: Oscar Barba, Graham Dawson, William Gattrell, Martin James Procter, Chrystelle Marie Rasamison, Colin Peter Sambrook-Smith, Philippe Wong-Kai-In
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Publication number: 20100087494Abstract: A compound of general formula (I): A process for preparing this compound. A fungicidal composition comprising a compound of general formula (I). A method for treating plants by applying a compound of general formula (I) or a composition comprising it.Type: ApplicationFiled: February 21, 2008Publication date: April 8, 2010Inventors: Pierre-Yves Coqueron, Rudiger Fischer, Oliver Gaertzen, Marie-Claire Grosjean-Cournoyer, Benoit Hartmann, Klaus Kunz, Darren Mansfield, Amos Mattes, Oswald Ort, Philippe Desbordes
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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: 20100056786Abstract: The present invention relates to a novel process for preparing known fungicidally active alkylanilides from 2-alkylhaloaromatics and heterocyclylamides.Type: ApplicationFiled: July 12, 2007Publication date: March 4, 2010Applicant: Bayer CropScience AGInventor: Alexander Straub
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Patent number: 7671076Abstract: The present invention relates to compounds of formula (I), which inhibit dipeptidyl peptidase IV (DPP-IV) and are useful for the prevention or treatment of diabetes, especially type II diabetes, as well as hyperglycemia, syndrome X, hyperinsulinemia, obesity, atherosclerosis, and various immunomodulatory diseases.Type: GrantFiled: January 30, 2008Date of Patent: March 2, 2010Assignee: Abbott LaboratoriesInventors: Irini Akritopoulou-Zanze, Daria Darczak, Jürgen Dinges, Stevan W. Djuric, Ethan D. Hoff, Hana A. Kopecka, Jyoti R. Patel, Zhonghua Pei, Qi Shuai, Kathy Sarris, Hing L. Sham, Paul E. Wiedeman
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Publication number: 20100048570Abstract: The present invention relates to novel 2-carbonyl-3-acyl-1,3-thiazolidines having a ?-amino group on the acyl chain, in free, prodrug form or pharmaceutically acceptable salt thereof, including their enantiomers, diastereomers and racemates, as efficient inhibitors against DPP-IV. The invention further relates to the pharmaceutical compositions comprising the disclosed compounds. The present invention also relates to methods for preparing the disclosed compounds and for treating DPP-IV-mediated diseases.Type: ApplicationFiled: January 16, 2008Publication date: February 25, 2010Applicants: Kainos Medicine, Inc, Korea Research Institute of Chemical Technology, Yungjin Pharmaceutical Company, LtdInventors: Sung Soo Kim, Jin Hee Ahn, Hyae Gyeong Cheon, Sang Dal Rhee, Nam Sook Kang, Ki Young Kim, Seung Kyu Kang, Won Hoon Jung, Sung Gyu Kim, Sun Young Kim, Jae Hong Kweon, Sang Kwon Sohn, Min Ki Shin, Ni Na Ha
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Patent number: 7667044Abstract: The present invention relates to novel inhibitors of prolyl endopeptidase of formula 1 W—KCONH—X—CON—Y—CO—Z??(1) wherein K, W, X, Y and Z are specified in the description. The compounds are useful for the treatment of diseases such as mild cognitive impairment (MCI), Alzheimer's disease, Down Syndrome, Parkinson disease and Chorea Huntington.Type: GrantFiled: November 30, 2005Date of Patent: February 23, 2010Assignee: Probiodrug AGInventors: André Niestroj, Ulrich Heiser, Ingo Schulz, Jens-Ulrich Rahfeld, Joachim Baer, Hans-Ulrich Demuth
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Patent number: 7666866Abstract: This application relates to a compound of formula (I) (or a pharmaceutically acceptable salt of the compound) as defined herein, pharmaceutical compositions thereof, and its use as an inhibitor of factor Xa and/or thrombin, as well as a process for its preparation and intermediates therefor.Type: GrantFiled: November 15, 2005Date of Patent: February 23, 2010Assignee: Eli Lilly and CompanyInventors: Jeffry Bernard Franciskovich, David Kent Herron, Valentine Joseph Klimkowski, Angela Lynn Marquart, John Joseph Masters, David Mendel, Andrew Michael Ratz, Gerald Floyd Smith, Michael Robert Wiley, Ying Kwong Yee
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Publication number: 20100035929Abstract: Disclosed are dispyrin analogue compounds useful as H3 receptor activity modulators, methods of making same, pharmaceutical compositions comprising same, and methods of treating neurological and psychiatric disorders associated with histamine H3 receptor activity using same. In one aspect, the disclosed analogues can have a structure represented by a formula: This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.Type: ApplicationFiled: June 8, 2009Publication date: February 11, 2010Inventors: Craig W. Lindsley, P. Jeffrey Conn, J. Phillip Kennedy, John T. Brogan
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Publication number: 20100029730Abstract: The invention relates to novel thiazolylbiphenylamides of the formula (I) in which R1, R2, R3, R4, R5 and R6 are as defined in the disclosure, to a process for preparing these compounds and to their use for controlling unwanted micro-organisms.Type: ApplicationFiled: October 1, 2009Publication date: February 4, 2010Inventors: Ralf Dunkel, Hans-Ludwig Elbe, Heiko Rieck, Ulrike Wachendorff-Neumann, Karl-Heinz Kuck
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Publication number: 20100022605Abstract: Described herein are N-hydroxyamlde antibacterial compounds, methods for making the compounds, pharmaceutical compositions containing the compounds and methods of treating bacterial infections utilizing the compounds and pharmaceutical compositions compound of Formula (I): or a salt, solvate ti hydrate thereof, wherein A is (a) eachindicates a point of attachment.Type: ApplicationFiled: December 4, 2006Publication date: January 28, 2010Inventors: Rakesh Kumar Jain, Mikhail Fedorovich Gordeev, Jason Gustaf Lewis, Charles Francavilla
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Publication number: 20100016550Abstract: The present invention relates to methods for the chemo-selective pegylation of the cysteine residue having unoxidized sulfhydryl side-chain and free ?-amino group in proteins, peptides and other molecules. Similar methods are provided for the chemo-selective pegylation of the homocysteine, selenocysteine, penicillamine, and N-methyl-cysteine residues.Type: ApplicationFiled: May 25, 2007Publication date: January 21, 2010Inventors: Zheng Xin Dong, John S. Eynon
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Publication number: 20090326016Abstract: The present invention relates to N-cycloalkyl-thiocarboxamide or N-cycloalkyl-N-substituted carboximidamide derivatives of formula (I) wherein A and B represent a 5-membered heterocyclyl groups, T represents an oxygen, sulphur or amino derivatives, Z1 represents a cycloalkyl group and Z2 and Z3 represent various substituents, their process of preparation, their use as fungicide active agents, particularly in the form of fungicide compositions, and methods for the control of phytopathogenic fungi, notably of plants, using these compounds or compositions.Type: ApplicationFiled: July 30, 2007Publication date: December 31, 2009Inventors: Ralf Dunkel, Stephanie Gary, Marie-Claire Grosjean-Cournoyer, Philippe Rinolfi, Arounarith Tuch
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Publication number: 20090326020Abstract: Compounds according to formula (I) are disclosed where Q is S, N, or O; X is optional, and can be O?, S?, ?N—NH2, ?N—OH, or —OH; Y is optional and can be —N(H)—, O, or C1 to C20 hydrocarbon; and R1 and R2 are each independently substituted or unsubstituted single-, fused- or multiple-ring aryl or (hetero)cyclic ring systems. Methods of making these compounds, pharmaceutical compositions containing the compounds, and their use, particularly for treating or preventing cancer, are also disclosed.Type: ApplicationFiled: June 16, 2009Publication date: December 31, 2009Applicants: UNIVERSITY OF TENNESSEE RESEARCH FOUNDATION, OHIO STATE UNIVERSITY RESEARCH FOUNDATIONInventors: Duane D. Miller, Wei Li, Zhao Wang, Yan Lu, Jianjun Chen, James T. Dalton, Chien-Ming Li
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Publication number: 20090306155Abstract: The present invention relates to compounds useful as inhibitors of protein kinase. The invention also relates to pharmaceutically acceptable compositions comprising said compounds and methods of using the compounds and the compositions in the treatment of various disease, conditions, or disorders. The invention also relates to processes for preparing compounds of the inventions.Type: ApplicationFiled: August 10, 2009Publication date: December 10, 2009Applicant: Vertex Pharmaceuticals IncorporatedInventors: Juan-Miguel Jimenez, Ronald Knegtel, Daniel Robinson, Philip Collier
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Patent number: 7625944Abstract: The present invention provides compounds that inhibit the activity of plasma kallikrein (PK) and methods of preventing and treating the formation of thrombin during or after a PK dependent disease or condition, for example, after fibrinolysis treatment.Type: GrantFiled: July 30, 2007Date of Patent: December 1, 2009Assignee: Activesite Pharmaceuticals, Inc.Inventors: Sukanto Sinha, Tamie Jo Chilcote
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Publication number: 20090281138Abstract: The invention provides compounds of formula wherein R1, R3, L1, L2, G1, G2, A and m are as defined in the specification and optical isomers, racemates and tautomers thereof, and pharmaceutically acceptable salts thereof; together with processes for their preparation, pharmaceutical compositions containing them and their use in therapy. The compounds are inhibitors of microsomal prostaglandin E synthase-1.Type: ApplicationFiled: November 14, 2008Publication date: November 12, 2009Applicant: AstraZeneca ABInventors: Johan Bylund, Marie E. Ek, Annika Kers, Gunnar Nordvall, Liselotte Ohberg, Jenny Viklund, Stefan Von Berg, Jorg Holenz, Katja Narhi, Daniel Sohn, Martin H. Johansson
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Publication number: 20090274655Abstract: Anti-viral agents of compounds of Formula (I): wherein A, R1, R2 and R3 are as defined in the specification, processes for their preparation and their use in HCV treatment are provided.Type: ApplicationFiled: November 15, 2007Publication date: November 5, 2009Inventors: Richard Martin Grimes, Charles David Hartley, Jacqueline Elizabeth Mordaunt, Pritom Shah, Martin John Slater, Gemma Victoria White
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Patent number: 7612059Abstract: N-[1-oxo-(optionally 2-aza)-2-alkyl-3-(carboxyl or thiol or hydroxyaminocarbonyl or N-hydroxyformamido)-propyl]-(aryl or heteroaryl)-azacyclo4-7alkanes or thiazacyclo4-7alkanes, salts or prodrugs thereof have interesting properties, e.g., in the treatment or prevention of disorders amenable to treatment by PDF inhibitors, such as treatment of bacterial infections.Type: GrantFiled: June 13, 2005Date of Patent: November 3, 2009Assignee: Vicuron Pharmaceuticals, Inc.Inventors: Jeffrey Jacobs, Rakesh K Patel, Jason G Lewis, Dinesh V Patel, Zhengyu Yuan
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Publication number: 20090258912Abstract: A compound of general formula (I): A process for preparing this compound. A fungicidal composition comprising a compound of general formula (I). A method for treating plants by applying a compound of general formula (I) or a composition comprising it.Type: ApplicationFiled: November 21, 2006Publication date: October 15, 2009Inventors: Pierre-Yves Coqueron, Darren James Mansfield, Philippe Desbordes, Heiko Rieck, Pierre Genix, Alain Villier, Marie-Claire Grosjean-Cournoyer
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Publication number: 20090258868Abstract: Disclosed are compounds of the formula I or a stereoisomer, tautomer, or pharmaceutically acceptable salt or solvate thereof, wherein W is a bond, —C(?S)—, —S(O)—, —S(O)2—, —C(?O)—, —O—, —C(R6)(R7)—, —N(R5)— or —C(?N(R5))—; X is —O—, —N(R5)— or —C(R6)(R7)—; provided that when X is —O—, U is not —O—, —S(O)—, —S(O)2—, —C(?O)— or —C(?NR5)—; U is a bond, —S(O)—, —S(O)2—, —C(O)—, —O—, —P(O)(OR15)—, —C(?NR5)—, —(C(R6)(R7))b— or —N(R5)—; wherein b is 1 or 2; provided that when W is —S(O)—, —S(O)2—, —O—, or —N(R5)—, U is not —S(O)—, —S(O)2—, —O—, or —N(R5)—; provided that when X is —N(R5)— and W is —S(O)—, —S(O)2—, —O—, or —N(R5)—, then U is not a bond; and R1, R2, R3, R4, R5, R6, and R7 are as defined in the specification; and pharmaceutical compositions comprising the compounds of formula I.Type: ApplicationFiled: December 10, 2008Publication date: October 15, 2009Inventors: Zhaoning Zhu, Brian A. McKittrick, Zhong-Yue Sun, Yuanzan C. Ye, Johannes H. Voigt, Corey Strickland, Elizabeth M. Smith, Andrew Stamford, William J. Greenlee, Robert Mazzola, John Caldwell, Jared N. Cumming, Lingyan Wang, Yusheng Wu, Ulrich Iserloh, Tao Guo, Thuy X.H. Le, Kurt W. Saionz, Suresh D. Babu, Rachael C. Hunter, Michelle L. Morris, Huizhong Gu, Gang Qian, Dawit Tadesse
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Publication number: 20090253673Abstract: Certain novel N-acylated spiropiperidine derivatives are ligands of the human ghrelin receptor(s) and, in particular, are antagonists/inverse agonists of the human ghrelin receptor. They are therefore useful for the treatment, control, or prevention of diseases and disorders responsive to the modulation of the ghrelin receptor, such as obesity, diabetes, and metabolic syndrome.Type: ApplicationFiled: July 6, 2007Publication date: October 8, 2009Inventors: Min Ge, Eric Cline, Lihu Yang, Sander G. Mills
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Publication number: 20090233972Abstract: The present invention discloses compounds of Formulae (I), or pharmaceutically acceptable salts, esters, or prodrugs thereof: which inhibit RNA-containing viruses, particularly the hepatitis C virus (HCV). Consequently, the compounds of the present invention interfere with the life cycle of the hepatitis C virus and are also useful as antiviral agents. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from HCV infection. The invention also relates to methods of treating an HCV infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention. The present invention relates to novel antiviral compounds represented herein above, pharmaceutical compositions comprising such compounds, and methods for the treatment or prophylaxis of viral (particularly HCV) infection in a subject in need of such therapy with said compounds.Type: ApplicationFiled: March 12, 2009Publication date: September 17, 2009Inventors: YAT SUN OR, LU YING, CE WANG, JIANG LONG, YAO-LING QIU
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Patent number: 7589216Abstract: The present invention is directed to a process for preparing intermediates that are useful to prepare certain antibacterial N-formyl hydroxylamine compounds which are peptide deformylase inhibitors. The process makes use ? ?-lactarn intermediate. Certain optically pure intermediates are also claimed.Type: GrantFiled: September 18, 2003Date of Patent: September 15, 2009Assignee: Novartis AGInventors: Prasad Koteswara Kapa, Xinglong Jiang, Eric M. Loeser, Joel Slade, Mahavir Prashad, George Tien-San Lee