Additional Hetero Ring Attached Directly Or Indirectly To The Diazole Ring By Nonionic Bonding (e.g., Methyl( 5-[2-(2-thienyl)-1,3-dioxolan -2-yl]-1h-benzimidazol-2-yl) Carbamate, Etc.) Patents (Class 548/304.7)
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Patent number: 7595330Abstract: The present invention provides benzimidazole thiophene compounds pharmaceutical compositions containing the same, processes for preparing the same and their use as pharmaceutical agents.Type: GrantFiled: August 28, 2006Date of Patent: September 29, 2009Assignee: SmithKline Beecham CorporationInventors: Mui Cheung, Kyle Allen Emmitte, James M. Salovich
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Patent number: 7595406Abstract: Compounds of Formula (I) inhibit the PARP enzyme and are useful for treating a disease or a disorder associated with PARP. Also disclosed are pharmaceutical compositions comprising compounds of Formula (I), methods of treatment comprising compounds of Formula (I), and methods of inhibiting the PARP enzyme comprising compounds of Formula (I).Type: GrantFiled: July 30, 2007Date of Patent: September 29, 2009Assignee: Abbott Laboratories Inc.Inventors: Thomas D. Penning, Sheela A. Thomas, Gui-Dong Zhu, Jianchun Gong, Vincent L. Giranda, Viraj B. Gandhi
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Patent number: 7582770Abstract: An enantiomer, diastereoisomer or tautomer of a compound, represented by formula I: wherein A, B, R1, R2, R3, R4, R5, R6, R7, R8, R9, and R10 are as defined herein, or a salt or ester thereof, as an inhibitor of HCV NS5B polymerase.Type: GrantFiled: February 18, 2005Date of Patent: September 1, 2009Assignee: Boehringer Ingelheim International GmbHInventors: Youla S. Tsantrizos, Catherine Chabot, Pierre Beaulieu, Christian Brochu, Timothy A. Stammers, Bounkham Thavonekham, Jean Rancourt
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Publication number: 20090202921Abstract: The present invention provides an optical recording composition comprising at least one compound denoted by general formula (I) and a holographic recording medium comprising a recording layer, wherein the recording layer comprises at least one compound denoted by general formula (I). In general formula (I), each of A1 and A2 independently denotes —CR4R5—, —O—, —NR6—, —S—, or —C(?O)—, each of R4, R5, and R6 independently denotes a hydrogen atom or a substituent, R1 denotes a substituent, n denotes an integer ranging from 0 to 4, each of R2 and R3 independently denotes a substituent having a Hammett substituent constant, ?p value, of greater than 0, R2 and R3 do not form a ring structure by bonding together, and at least one from among R1, R2, R3, A1, and A2 comprises at least one polymerizable group.Type: ApplicationFiled: February 10, 2009Publication date: August 13, 2009Applicant: FUJIFILM CorporationInventors: Hiroyuki SUZUKI, Satoru Yamada
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Publication number: 20090197910Abstract: The present invention relates to a pharmaceutical composition for the treatment or prevention of viral infections comprising as an active principle at least one benzimidazole conjugates derivative having the general formula (I). The invention also relates to processes for the preparation of compounds according to the invention having above mentioned general formula and their use as a medicine or to treat or prevent viral infections.Type: ApplicationFiled: May 7, 2007Publication date: August 6, 2009Applicants: KATHOLIEKE UNIVERSITEIT LEUVEN, NATIONAL TSING HUA UNIVERSITYInventors: Johan Neyts, Asish R. Das, Shih Ching Hung, Jih Ru Hwu, Raghunath Singha
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Patent number: 7569688Abstract: Provided is a pharmaceutical composition containing a propane-1,3-dione derivative as the active ingredient, particularly a GnRH receptor antagonist. Also, provided is a propane-1,3-dione derivative having a GnRH antagonistic effect.Type: GrantFiled: June 20, 2005Date of Patent: August 4, 2009Assignee: Astellas Pharma Inc.Inventors: Masaaki Hirano, Eiji Kawaminami, Akira Toyoshima, Hiroyuki Moritomo, Norio Seki, Ryutaro Wakayama, Minoru Okada, Toshiyuki Kusayama
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Patent number: 7566789Abstract: Novel compounds of the formula I in which D, X, X?, W, Y, T and R1 are as defined in Patent claim 1, are inhibitors of coagulation factor Xa and can be employed for the prophylaxis and/or therapy of thromboembolic diseases and for the treatment of tumours.Type: GrantFiled: July 4, 2003Date of Patent: July 28, 2009Assignee: Merck Patent GmbHInventors: Dieter Dorsch, Bertram Cezanne, Wrner Mederski, Christos Tsaklakidis, Johannes Gleitz, Christopher Barnes
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Publication number: 20090181943Abstract: This invention relates to compounds for the inhibition of histone deacetylase. More particularly, the invention provides for compounds of formula compounds of the Formula (I) and N-oxides, hydrates, solvates, pharmaceutically acceptable salts, prodrugs and complexes thereof, and racemic and scalemic mixtures, diastereomers and enantiomers thereof, wherein groups L, M, X and Y are as defined herein.Type: ApplicationFiled: April 9, 2008Publication date: July 16, 2009Applicant: METHYLGENE INC.Inventors: Pierre Tessier, Silvana Leit, David Smil, Robert Deziel, Alain Ajamian, Yves Andre Chantigny, Celia Dominguez
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Publication number: 20090170842Abstract: A pharmaceutical composition for use in treating, inhibiting, and/or preventing breast and/or ovarian cancer can include: a molecule having a structure of one of Compounds 1-38, pharmaceutically acceptable salt thereof, or analog thereof, and a pharmaceutically acceptable carrier containing the compound. The pharmaceutically acceptable carrier can be configured for oral, systemic, transdermal, intranasal, suppository, parenteral, intramuscular, intravenous, or subcutaneous administration. The compound can be present in the composition in a therapeutically effective amount for treating, inhibiting, and/or preventing breast and/or ovarian cancer. Also, the compound can be present in a therapeutically effective amount for enhancing production of BRCA1.Type: ApplicationFiled: November 13, 2008Publication date: July 2, 2009Applicant: University of KansasInventors: Roy A. Jensen, Lisa M. Harlan-Williams, Frank J. Schoenen, Jeffrey Aube, Gerald H. Lushington
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Patent number: 7550603Abstract: Compounds of Formula (I) inhibit the PARP enzyme and are useful for treating a disease or a disorder associated with PARP. Also disclosed are pharmaceutical compositions comprising compounds of Formula (I), methods of treatment comprising compounds of Formula (I), and methods of inhibiting the PARP enzyme comprising compounds of Formula (I).Type: GrantFiled: April 11, 2006Date of Patent: June 23, 2009Assignee: Abbott Laboratories Inc.Inventors: Gui-Dong Zhu, Jianchun Gong, Virajkumar B. Gandhi, Thomas D. Penning, Vincent L. Giranda
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Publication number: 20090134783Abstract: The present invention provides for emissive materials comprising compounds of specific chemical structure, and electroluminescent devices comprising such emissive materials.Type: ApplicationFiled: November 14, 2008Publication date: May 28, 2009Inventors: Jiann T'suen Lin, Mei-Yi Lai, Chih-Hsin Chen
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Publication number: 20090131401Abstract: Substituted benzoimidazole compounds useful as anti-infectives that decrease resistance, virulence, or growth of microbes are provided. Methods of making and using substituted benzoimidazole compounds, as well as pharmaceutical preparations thereof, in, e.g., reducing antibiotic resistance and inhibiting biofilms.Type: ApplicationFiled: February 12, 2008Publication date: May 21, 2009Applicant: Paratek Pharmaceuticals, Inc.Inventors: Stuart B. Levy, Michael N. Alekshun, Brent L. Podlogar, Kwasi Ohemeng, Atul K. Verma, Tadeusz Warchol, Beena Bhatia, Todd Bowser, Mark Grier
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Patent number: 7531668Abstract: A compound represented by the formula [I]: [wherein R1 and R2 are the same or different and each represents C1-6 alkyl, C3-8 cycloalkyl, et al; R3a, R3b, and R4 are the same or different and each represents hydrogen, C1-6 alkyl, et al; X represents —N—, —CH—, et al; Y1 represents a single bond, C1-3 alkylene, et al; Y2 represents C1-4 alkylene, oxy(C1-4 alkylene), et al; Ar1 represents a monocyclic aromatic carbocyclic group, monocyclic aromatic heterocyclic group, et al; and Ar2 represents a 5- or 6-membered aromatic carbocyclic group, aromatic heterocyclic group, et al]. This compound functions as a melanin-concentrating hormone receptor antagonist and is useful as, e.g., a therapeutic agent for obesity, et al.Type: GrantFiled: September 30, 2005Date of Patent: May 12, 2009Assignee: Banyu Pharmaceutical Co., Ltd.Inventors: Takao Suzuki, Minoru Moriya, Shunji Sakuraba, Sayaka Mizutani, Hisashi Iwaasa, Akio Kanatani
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Publication number: 20090111865Abstract: Compounds of formula I or pharmaceutically acceptable salts thereof: wherein R1, R2, R3, R4 and Z are as defined in the specification as well as salts and pharmaceutical compositions including the compounds are prepared. They are useful in therapy, in particular in the management of pain.Type: ApplicationFiled: January 8, 2009Publication date: April 30, 2009Applicant: ASTRAZENECA ABInventors: Ziping Liu, Daniel Page, Christopher Walpole, Hua Yang
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Patent number: 7517893Abstract: Novel dicationic bichalcophene compounds are described. The presently disclosed novel dicationic bichalcophene compounds exhibit in vitro activity versus Trypanosoma brucei rhodesiense, Plasmodium falciparum, or Leishmania donovani comparable to that of pentamidine and furamidine. Some of the novel dicationic bichalcophene compounds displayed good activity in vivo in a murine model of a Trypanosoma brucei rhodesiense infection.Type: GrantFiled: May 16, 2006Date of Patent: April 14, 2009Assignees: The University of North Carolina at Chapel Hill, Georgia State University Research Foundation, Inc.Inventors: Richard R. Tidwell, David W. Boykin, Chad Stephens, Mohamed A. Ismail, W. David Wilson, Reto Brun, Karl Werbovetz
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Patent number: 7514568Abstract: The invention relates to new methods of preparing substituted benzimidazole compounds, such as 2-bromo-5,6-dichlorobenzimidazole, which are useful in the preparation of compounds having antiviral activity.Type: GrantFiled: April 11, 2008Date of Patent: April 7, 2009Assignee: SmithKline Beecham CorporationInventor: Stephen Freeman
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Patent number: 7501448Abstract: Provided are processes for preparing telmisartan alkyl ester and telmisartan using environmentally friendly organic solvents that are easily removed from the reaction mixture, wherein a telmisartan alkyl ester is isolated and hydrolyzed to form telmisartan or the telmisartan is prepared using a synthesis in a single reaction vessel.Type: GrantFiled: October 13, 2005Date of Patent: March 10, 2009Assignee: Teva Pharmaceutical Industries, Ltd.Inventors: Nurit Perlman, Eyal Gilboa
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Patent number: 7501447Abstract: Compounds of formula (I) or pharmaceutically acceptable salts thereof: wherein R1, R2, R3, R4 and Z are as defined in the specification as well as salts and pharmaceutical compositions including the compounds are prepared. They are useful in therapy, in particular in the management of pain.Type: GrantFiled: June 9, 2004Date of Patent: March 10, 2009Assignee: AstraZeneca ABInventors: Ziping Liu, Daniel Pagé, Christopher Walpole, Hua Yang
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Publication number: 20090054431Abstract: The present invention relates to novel compounds which are antagonist or inverse agonists at an opioid receptor. Such compounds are useful in the treatment of obesity and related diseases and/or conditions in mammals, particularly humans. Methods of making and using such compounds are also disclosed.Type: ApplicationFiled: October 12, 2006Publication date: February 26, 2009Inventors: Kevin Karl Barvian, Jason Daniel Speake, David John Cowan, Andrew Lamont Larkin, Jerzy Ryszard Szewczyk
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Patent number: 7495109Abstract: A compound of the formula (I), (II), (III) or (IV) wherein Z, A, B, C, R, R1, R2, Q, and n are as described herein.Type: GrantFiled: January 11, 2005Date of Patent: February 24, 2009Assignee: Purdue Pharma L.P.Inventors: Qun Sun, R. Richard Goehring, Donald Kyle, Zhengming Chen, Sam Victory, John Whitehead
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Publication number: 20090042931Abstract: There is provided compounds of formula I, wherein A, X1, X2, X3, X4, Y1, Y2, Y3, Y4, Z1, Z2, R4 and R5 have meanings given in the description, and pharmaceutically-acceptable salts thereof, which compounds are useful as selective agonists of the AT2 receptor, and thus, in particular, in the treatment of inter alia gastrointestinal conditions, such as dyspepsia, IBS and MOF, and cardiovascular disorders.Type: ApplicationFiled: April 12, 2006Publication date: February 12, 2009Applicant: Vicore Pharma ABInventors: Mathias Alterman, Anders Hallberg, Xiongyu Wu
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Publication number: 20090030016Abstract: Compounds which inhibit the activity of poly(ADP-ribose)polymerase (PARP), compositions containing the compounds and methods of treating diseases using them are disclosed.Type: ApplicationFiled: July 15, 2008Publication date: January 29, 2009Applicant: ABBOTT LABORATORIESInventors: Virajkumar B. Gandhi, Vincent L. Giranda, Jianchun Gong, Thomas D. Penning, Gui-Dong Zhu
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Patent number: 7479502Abstract: The present invention relates to novel inhibitors of Factors VIIa, IXa, Xa, XIa, in particular Factor VIIa, pharmaceutical compositions comprising these inhibitors, and methods for using these inhibitors for treating or preventing thromboembolic disorders, cancer or rheumatoid arthritis. Processes for preparing these inhibitors are also disclosed.Type: GrantFiled: December 3, 2003Date of Patent: January 20, 2009Assignee: Pharmacyclics, Inc.Inventors: Aleksandr Kolesnikov, Roopa Rai, William Dvorak Shrader, Steven M. Torkelson, Kieron E. Wesson, Wendy B. Young
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Patent number: 7465807Abstract: The present invention provides a process for preparing benzimidazole thiophene compounds.Type: GrantFiled: October 12, 2004Date of Patent: December 16, 2008Assignee: SmithKline Beecham CorporationInventors: Mui Cheung, Kyle Allen Emmitte
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Patent number: 7462724Abstract: Compounds of Formula (I) inhibit the PARP enzyme and are useful for treating a disease or a disorder associated with PARP. Also disclosed are pharmaceutical compositions comprising compounds of Formula (I), methods of treatment comprising compounds of Formula (I), and methods of inhibiting the PARP enzyme comprising compounds of Formula (I).Type: GrantFiled: November 15, 2006Date of Patent: December 9, 2008Assignee: Abbott LaboratoriesInventors: Thomas D. Penning, Sheela A. Thomas, Gui-Dong Zhu, Jianchun Gong, Vincent L. Giranda, Viraj B. Gandhi
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Patent number: 7459566Abstract: A process for preparing an optionally substituted 4-benzimidazol-2-ylmethylamino)benzamidine, the process comprising: (a) condensing an optionally suitably substituted diaminobenzene with 2-[4-(1,2,4-oxadiazol-5-on-3-yl)phenylamino]acetic acid; (b) hydrogenating the product obtained from step (a); and (c) optionally carboxylating the amidino group of the product obtained from step (b).Type: GrantFiled: March 2, 2007Date of Patent: December 2, 2008Assignee: Boehringer Ingelheim International GmbHInventors: Georg Zerban, Arndt Hausherr, Kerstin Schlarb, Heinz-Peter Schmitt, Bjoern Weyell, Gunter Koch, Rainer Hamm
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Publication number: 20080269298Abstract: The present invention provides compounds of formula (I): pharmaceutical compositions containing the same, processes for preparing the same and their use as pharmaceutical agents.Type: ApplicationFiled: May 1, 2008Publication date: October 30, 2008Inventors: Clarence W. Andrews, Mui Cheung, Ronda G. Davis-Ward, David Harold Drewry, Kyle Allen Emmitte, Robert Dale Hubbard, Kevin W. Kuntz, James Andrew Linn, Robert Anthony Mook, Gary Keith Smith, James Marvin Veal
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Patent number: 7439258Abstract: A compound of the formula I: wherein: X is CH or N; Y is O or S; Z is OH, NH2, NMeR3, NHR3; OR3 or 5- or 6-membered heterocycle, having 1 to 4 heteroatoms selected from O, N and S, said heterocycle being optionally substituted with from 1 to 4 substituents; A is N, COR7 or CR5, wherein R5 is H, halogen, or (C1-6) alkyl and R7 is H or (C1-6 alkyl), with the proviso that X and A are not both N; R6 is H, halogen, (C1-6 alkyl) or OR7, wherein R7 is H or (C1-6 alkyl); R1 is selected from the group consisting of 5- or 6-membered heterocycle having 1 to 4 heteroatoms selected from O, N, and S, phenyl, phenyl(C1-3)alkyl, (C2-6)alkenyl, phenyl(C2-6)alkenyl, (C3-6)cycloalkyl, (C1-6)alkyl, CF3, 9- or 10-membered heterobicycle having 1 to 4 heteroatoms selected from O, N and S, wherein said heterocycle, phenyl, phenyl(C2-6)alkenyl and phenyl(C1-3)alkyl), alkenyl, cycloalkyl, (C1-6)alkyl, and heterobicycle are all optionally substituted with from 1 to 4 substituents; R2 is selected from (C1-6)alkyl, (C3-7)cycloalkyl,Type: GrantFiled: May 21, 2004Date of Patent: October 21, 2008Assignee: Boehringer Ingelheim (Canada) LtdInventors: Pierre Louis Beaulieu, Gulrez Fazal, James Gillard, George Kukolj, Volkhard Austel
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Publication number: 20080249301Abstract: The present invention provides a process for preparing benzimidazole thiophene compounds of formula (I). Intermediates used in the process are also claimed.Type: ApplicationFiled: August 28, 2006Publication date: October 9, 2008Inventors: Keith Hornberger, Mui Cheung, Mark Andrew Pobanz, Kyle Allen Emmitte, Kevin Wayne Kuntz, Jennifer Gabriel Badiang
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Patent number: 7425637Abstract: Disclosed are compounds of the Formula I and pharmaceutically acceptable salts and prodrugs thereof, wherein W, R1, R2, R7, R8, R9 and R10 are as defined in the specification. Such compounds are MEK inhibitors and useful in the treatment of hyperproliferative diseases, such as cancer and inflammation, in mammals. Also disclosed is a method of using such compounds in the treatment of hyperproliferative diseases in mammals, and pharmaceutical compositions containing such compounds.Type: GrantFiled: February 18, 2005Date of Patent: September 16, 2008Assignee: Array BioPharma Inc.Inventors: Eli M. Wallace, Joseph P. Lyssikatos, Allison L. Marlow, T. Brian Hurley
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Patent number: 7414046Abstract: The present invention relates to compounds of the formula I: or a pharmaceutically acceptable derivative or prodrug thereof. The compounds are useful as inhibitors of bacterial gyrase activity. The present invention also relates to methods for treating bacterial infections in mammala. The present invention also relates to methods for decreasing bacterial quantity in a biological sample.Type: GrantFiled: May 23, 2003Date of Patent: August 19, 2008Assignee: Vertex Pharmaceuticals IncorporatedInventors: Anne-Laure Grillot, Paul Charifson, Dean Stamos, Yusheng Liao, Michael Badia, Martin Trudeau
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Patent number: 7410989Abstract: The present invention relates to novel compounds and methods that are useful in treating members of the Flaviviridae family of viruses. Compounds of the present invention will have a structure according to Formulas (I)-(VI) as recited throughout the application.Type: GrantFiled: November 20, 2006Date of Patent: August 12, 2008Assignees: The University of North Carolina at Chapel Hill, Georgia State University Research Foundation, Inc., Auburn UniversityInventors: Christine C. Dykstra, Maurice Daniel Givens, David A. Stringfellow, Kenny Brock, David Boykin, Arvid Kumar, W. David Wilson, Richard R. Tidwell, Chad F. Stephens
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Patent number: 7410990Abstract: This invention features a compound of formula (I): R1 is aryl or heteroaryl; each of R2 and R4, independently, is H, halogen, CN, alkyl, ORa, or NRaRb; R3 is H, halogen, CN, alkyl, alkenyl, alkynyl, aryl, heteroaryl, cyclyl, heterocyclyl, ORa, OC(O)Ra, OC(O)NRaRb, NRaRb, NRaC(O)Rb, NRaS(O)RbNRaS(O)2Rb, NRaC(O)NRbRc, NRaC(S)NRbRc, NRaC(NRb)NRcRd, NRaC(O)ORb, S(O)NRaRb, S(O)2NRaRb, S(O)Ra, S(O)2Ra, C(O)Ra, C(O)ORa, or C(O)NRaRb; R5 is H or alkyl; n is 0, 1, 2, 3, 4, 5, or 6; A is O, S, S(O), S(O)2, or NRe; B is N or CRf; X is O, S, S(O), S(O)2, NRe, or C(O); Y is a covalent bond, C(O), C?NRa, O, S, S(O), S(O)2, or NRe; Z is N or CH; each of U and V, independently, is N or CR; and W is O, S, or NRe; in which each of Ra, Rb, Rc, and Rd, independently, is H, alkyl, aryl, heteroaryl, cyclyl, or heterocyclyl; Re is H, alkyl, aryl, acyl, or sufonyl; and Rf is H, alkyl, aryl, acyl, sulfonyl, alkoxyl, amino, ester, amide, CN, or halogen.Type: GrantFiled: October 3, 2006Date of Patent: August 12, 2008Assignee: Synta Pharmaceuticals Corp.Inventors: Lijun Sun, Mitsunori Ono, Yumiko Wada, Weiwen Ying, Teresa Przewloka, Elena Kostik
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Publication number: 20080188668Abstract: The invention relates to new methods of preparing substituted benzimidazole compounds, such as 2-bromo-5,6-dichlorobenzimidazole, which are useful in the preparation of compounds having antiviral activity.Type: ApplicationFiled: April 11, 2008Publication date: August 7, 2008Inventor: Stephen Freeman
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Publication number: 20080146797Abstract: The invention provides the process illustrated in scheme 1 for synthesizing heterocyclic compounds of formula I. In the process, an isothiocyanate of formula II is initially reacted with a primary amine or formula III to give a thiourea of formula IV. Subsequently, the thiourea of formula IV is converted to the corresponding heterocycle of formula I using a base and a sulfonyl chloride.Type: ApplicationFiled: February 6, 2008Publication date: June 19, 2008Applicant: SANOFI-AVENTIS DEUTSCHLAND GMBHInventors: Uwe HEINELT, Hans-Jochen LANG
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Patent number: 7371870Abstract: There are provided benzimidazolone compounds that provide a plurality of hues from a single structural formula, and are useful as pigments that offer superior dispersibility in binder resins, as well as benzimidazolone compounds that are useful as pigments, and show minimal flocculation when pigments of two or more different hues are blended together to produced a desired hue. A benzimidazolone compound represented by a general formula (1) shown below. (wherein, R1, R2, R3 and R4 each represent, independently, a hydrogen atom, an alkyl group of 1 to 5 carbon atoms, or an alkoxy group of 1 to 5 carbon atoms, and R5 and R6 each represent, independently, an alkyl group of 1 to 5 carbon atoms).Type: GrantFiled: June 23, 2004Date of Patent: May 13, 2008Assignee: Dainippon Ink and Chemicals, Inc.Inventors: Masaki Hosaka, Toshio Takei
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Patent number: 7368467Abstract: The invention relates to compounds, compositions comprising the compounds, and methods of using the compounds and compound compositions. The compounds, compositions, and methods described herein can be used for the therapeutic modulation of ion channel function, and treatment of disease and disease symptoms, particularly those mediated by certain calcium channel subtype targets.Type: GrantFiled: March 7, 2005Date of Patent: May 6, 2008Assignee: WyethInventors: Robert Zelle, Vincent P. Galullo, Hormoz Mazdiyasni
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Patent number: 7335777Abstract: This invention relates to novel benzimidazole derivatives of formula (I), pharmaceutical compositions containing these compounds, and methods of treatment therewith.Type: GrantFiled: April 1, 2004Date of Patent: February 26, 2008Assignee: Neurosearch A/SInventors: Lene Teuber, Janus S. Larsen
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Patent number: 7309716Abstract: The present invention relates to compounds of Formula I: or a pharmaceutically acceptable salt thereof, wherein the R1, Z, Y, RA, and W groups of formula I are as defined herein. The invention also provides pharmaceutically acceptable compositions and methods of using the compositions in the treatment of various disorders.Type: GrantFiled: October 28, 2004Date of Patent: December 18, 2007Assignee: Vertex Pharmaceuticals IncorporatedInventors: Dean M. Wilson, Andreas P. Termin, Jesus E. Gonzalez, III, Nicole Zimmermann, Yulian Zhang, Lev T. D. Fanning
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Patent number: 7300928Abstract: Benzimidazolidinone derivative compounds, which increase acetylcholine signaling or effect in the brain, and highly selective muscarinic agonists, particularly for the M1 and/or M4 receptor subtypes, pharmaceutical compositions comprising the same, as well as methods of treating psychosis using these compounds are disclosed.Type: GrantFiled: May 3, 2006Date of Patent: November 27, 2007Assignee: Acadia Pharmaceuticals, Inc.Inventors: Nicholas Michael Kelly, Kristian Norup Koch, Bo-Ragnar Tolf
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Patent number: 7291611Abstract: Benzimidazolidinone derivative compounds, which increase acetylcholine signaling or effect in the brain, and highly selective muscarinic agonists, particularly for the M1 and/or M4 receptor subtypes, pharmaceutical compositions comprising the same, as well as methods of treating psychosis using these compounds are disclosed.Type: GrantFiled: July 21, 2005Date of Patent: November 6, 2007Assignee: ACADIA Pharmaceuticals Inc.Inventors: Nicholas Michael Kelly, Kristian Norup Koch, Bo-Ragnar Tolf
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Patent number: 7271271Abstract: Compounds are provided having the formula: wherein variables R0, R1, R2, R3, R4, Q, L and subscript n are as described herein. The subject compounds are useful for treatment of infammatory and immune conditions and diseases. Compositions and methods of treatment using the subject compounds are also provided. For example, the subject methods are useful for treatment of inflammatory and immune disorders and disease such as multiple sclerosis, rheumatoid arthritis, psoriasis, and inflammatory bowel disease.Type: GrantFiled: June 27, 2005Date of Patent: September 18, 2007Assignee: Amgen SF, LLCInventors: Zice Fu, Michael G. Johnson, An-Rong Li, Andrew P. Marcus, Julio C. Medina, Philippe Bergeron, Xiaoqi Chen, Xiaohui Du, Jeffrey Deignan, Jason A. Duquette, Darin Gustin, Jeffrey T. Mihalic
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Patent number: 7271270Abstract: This invention relates to low molecular weight, non-peptidic, non-peptidomimetic, organic molecules that act as modulators of mammalian complement C5a receptors, preferably ones that act as high affinity C5a receptor ligands and also to such ligands that act as antagonists or inverse agonists of complement C5a receptors. Preferred compounds of the invention possess some or all of the following properties in that they are: 1) multi-aryl in structure, 2) heteroaryl in structure, 3) a pharmaceutically acceptable oral dose can provide a detectable in vitro effect, 4) comprise fewer than four or preferably no amide bonds, and 5) capable of inhibiting leukocyte chemotaxis at nanomolar or sub-nanomolar concentrations. This invention also relates to pharmaceutical compositions comprising such compounds and the use of such compounds in treating a variety of inflammatory and immune system disorders. Additionally, this invention relates to the use such compounds as probes for the localization of C5a receptors.Type: GrantFiled: May 24, 2004Date of Patent: September 18, 2007Assignee: Neurogen CorporationInventors: Andrew Thurkauf, Xiao-shu He, He Zhao
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Patent number: 7268255Abstract: N-Aryl or N-heteroarylformamides are prepared by hydrogenating a corresponding nitroarene or nitroheteroarene with formic acid and/or ammonium formate as hydrogen donor and formylating agent in the presence of at least one noble metal-based hydrogenation catalyst and a vanadium or molybdenum compound as co-catalyst.Type: GrantFiled: February 19, 2004Date of Patent: September 11, 2007Assignee: Lonza AGInventors: Ulrich Kampfen, Dario Veghini, Dominique Roberge, Jared Randall
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Patent number: 7250427Abstract: Aryl substituted benzimidazole and imidazo[4,5]pyridine ethers are described as inhibitors of Cds1 and useful as adjuvants to chemotherapy or radiation therapy in the treatment of cancer.Type: GrantFiled: June 27, 2005Date of Patent: July 31, 2007Assignee: Janssen Pharmaceutica, N.V.Inventors: J. Guy Breitenbucher, Alice Lee-Dutra, Danielle K. Neff
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Patent number: 7235558Abstract: The present invention relates to compounds of the formula I, in which R1, R2, A, B, D, F, n, m and o have the meanings indicated herein. The compounds of the formula I are valuable pharmacologically active compounds. They are reversible inhibitors of the interaction between the plasma protein von Willebrand factor (vWF) and the blood platelet receptor glycoprotein Ib-IX-V complex (GPIb).Type: GrantFiled: June 4, 2003Date of Patent: June 26, 2007Assignees: Sanofi-Aventis Deutschland GmbH, Ajinomoto Co., IncInventors: Otmar Klingler, Melitta Just, Kuniya Sakurai, Naoyuki Fukuchi
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Patent number: 7202368Abstract: A process for preparing an optionally substituted 4-benzimidazol-2-ylmethylamino)benzamidine, the process comprising: (a) condensing an optionally suitably substituted diaminobenzene with 2-[4-(1,2,4-oxadiazol-5-on-3-yl)phenylamino]acetic acid; (b) hydrogenating the product obtained from step (a); and (c) optionally carboxylating the amidino group of the product obtained from step (b).Type: GrantFiled: June 9, 2005Date of Patent: April 10, 2007Assignee: Boehringer Ingelheim International GmbHInventors: Georg Zerban, Arndt Hausherr, Kerstin Schlarb, Heinz-Peter Schmitt, Bjoern Weyell, Gunter Koch, Rainer Hamm
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Patent number: 7183286Abstract: The present invention relates to novel compounds and methods that are useful in treating members of the Flaviviridae family of viruses. Compounds of the present invention will have a structure according to Formulas (I)–(VI) as recited throughout the application.Type: GrantFiled: March 9, 2004Date of Patent: February 27, 2007Assignees: The University of North Carolina at Chapel Hill, Auburn University, Georgia State University Research Foundation, Inc.Inventors: Christine C. Dykstra, Maurice Daniel Givens, David A. Stringfellow, Kenny Brock, David W. Boykin, Arvid Kumar, W. David Wilson, Richard R. Tidwell, Chad F. Stephens
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Patent number: 7148226Abstract: The invention relates to compounds of the formula 1 and to pharmaceutically acceptable salts, solvates, prodrugs and metabolites thereof, wherein W, Z, R1 and R2, are as defined herein. The invention also relates to methods of treating Hepatitis C virus in mammals by administering the compounds of formula 1, and to pharmaceutical compositions for treating such disorders, which contain the compounds of formula 1. The invention also relates to methods of preparing the compounds of formula 1.Type: GrantFiled: November 19, 2003Date of Patent: December 12, 2006Assignee: Agouron Pharmaceuticals, Inc.Inventors: Allen Borchardt, Javier Gonzalez, Hui Li, Maria Angelica Linton, John Howard Tatlock
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Patent number: RE40245Abstract: The present invention relates to compounds of the formula I: or a pharmaceutically acceptable derivative or prodrug thereof. The compounds are useful as inhibitors of bacterial gyrase activity. The present invention also relates to methods for treating bacterial infections in mammala. The present invention also relates to methods for decreasing bacterial quantity in a biological sample.Type: GrantFiled: April 28, 2004Date of Patent: April 15, 2008Assignee: Vertex Pharmaceuticals IncorporatedInventors: Anne-Laure Grillot, Paul S. Charifson, Dean Stamos, Yusheng Liao, Michael C. Badia, Martin Trudeau