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)
  • Patent number: 7595330
    Abstract: The present invention provides benzimidazole thiophene compounds pharmaceutical compositions containing the same, processes for preparing the same and their use as pharmaceutical agents.
    Type: Grant
    Filed: August 28, 2006
    Date of Patent: September 29, 2009
    Assignee: SmithKline Beecham Corporation
    Inventors: Mui Cheung, Kyle Allen Emmitte, James M. Salovich
  • Patent number: 7595406
    Abstract: 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: Grant
    Filed: July 30, 2007
    Date of Patent: September 29, 2009
    Assignee: Abbott Laboratories Inc.
    Inventors: Thomas D. Penning, Sheela A. Thomas, Gui-Dong Zhu, Jianchun Gong, Vincent L. Giranda, Viraj B. Gandhi
  • Patent number: 7582770
    Abstract: 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: Grant
    Filed: February 18, 2005
    Date of Patent: September 1, 2009
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Youla S. Tsantrizos, Catherine Chabot, Pierre Beaulieu, Christian Brochu, Timothy A. Stammers, Bounkham Thavonekham, Jean Rancourt
  • Publication number: 20090202921
    Abstract: 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: Application
    Filed: February 10, 2009
    Publication date: August 13, 2009
    Applicant: FUJIFILM Corporation
    Inventors: Hiroyuki SUZUKI, Satoru Yamada
  • Publication number: 20090197910
    Abstract: 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: Application
    Filed: May 7, 2007
    Publication date: August 6, 2009
    Applicants: KATHOLIEKE UNIVERSITEIT LEUVEN, NATIONAL TSING HUA UNIVERSITY
    Inventors: Johan Neyts, Asish R. Das, Shih Ching Hung, Jih Ru Hwu, Raghunath Singha
  • Patent number: 7569688
    Abstract: 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: Grant
    Filed: June 20, 2005
    Date of Patent: August 4, 2009
    Assignee: Astellas Pharma Inc.
    Inventors: Masaaki Hirano, Eiji Kawaminami, Akira Toyoshima, Hiroyuki Moritomo, Norio Seki, Ryutaro Wakayama, Minoru Okada, Toshiyuki Kusayama
  • Patent number: 7566789
    Abstract: 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: Grant
    Filed: July 4, 2003
    Date of Patent: July 28, 2009
    Assignee: Merck Patent GmbH
    Inventors: Dieter Dorsch, Bertram Cezanne, Wrner Mederski, Christos Tsaklakidis, Johannes Gleitz, Christopher Barnes
  • Publication number: 20090181943
    Abstract: 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: Application
    Filed: April 9, 2008
    Publication date: July 16, 2009
    Applicant: METHYLGENE INC.
    Inventors: Pierre Tessier, Silvana Leit, David Smil, Robert Deziel, Alain Ajamian, Yves Andre Chantigny, Celia Dominguez
  • Publication number: 20090170842
    Abstract: 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: Application
    Filed: November 13, 2008
    Publication date: July 2, 2009
    Applicant: University of Kansas
    Inventors: Roy A. Jensen, Lisa M. Harlan-Williams, Frank J. Schoenen, Jeffrey Aube, Gerald H. Lushington
  • Patent number: 7550603
    Abstract: 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: Grant
    Filed: April 11, 2006
    Date of Patent: June 23, 2009
    Assignee: Abbott Laboratories Inc.
    Inventors: Gui-Dong Zhu, Jianchun Gong, Virajkumar B. Gandhi, Thomas D. Penning, Vincent L. Giranda
  • Publication number: 20090134783
    Abstract: The present invention provides for emissive materials comprising compounds of specific chemical structure, and electroluminescent devices comprising such emissive materials.
    Type: Application
    Filed: November 14, 2008
    Publication date: May 28, 2009
    Inventors: Jiann T'suen Lin, Mei-Yi Lai, Chih-Hsin Chen
  • Publication number: 20090131401
    Abstract: 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: Application
    Filed: February 12, 2008
    Publication date: May 21, 2009
    Applicant: 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
  • Patent number: 7531668
    Abstract: 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: Grant
    Filed: September 30, 2005
    Date of Patent: May 12, 2009
    Assignee: Banyu Pharmaceutical Co., Ltd.
    Inventors: Takao Suzuki, Minoru Moriya, Shunji Sakuraba, Sayaka Mizutani, Hisashi Iwaasa, Akio Kanatani
  • Publication number: 20090111865
    Abstract: 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: Application
    Filed: January 8, 2009
    Publication date: April 30, 2009
    Applicant: ASTRAZENECA AB
    Inventors: Ziping Liu, Daniel Page, Christopher Walpole, Hua Yang
  • Patent number: 7517893
    Abstract: 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: Grant
    Filed: May 16, 2006
    Date of Patent: April 14, 2009
    Assignees: 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
  • Patent number: 7514568
    Abstract: 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: Grant
    Filed: April 11, 2008
    Date of Patent: April 7, 2009
    Assignee: SmithKline Beecham Corporation
    Inventor: Stephen Freeman
  • Patent number: 7501448
    Abstract: 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: Grant
    Filed: October 13, 2005
    Date of Patent: March 10, 2009
    Assignee: Teva Pharmaceutical Industries, Ltd.
    Inventors: Nurit Perlman, Eyal Gilboa
  • Patent number: 7501447
    Abstract: 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: Grant
    Filed: June 9, 2004
    Date of Patent: March 10, 2009
    Assignee: AstraZeneca AB
    Inventors: Ziping Liu, Daniel Pagé, Christopher Walpole, Hua Yang
  • Publication number: 20090054431
    Abstract: 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: Application
    Filed: October 12, 2006
    Publication date: February 26, 2009
    Inventors: Kevin Karl Barvian, Jason Daniel Speake, David John Cowan, Andrew Lamont Larkin, Jerzy Ryszard Szewczyk
  • Patent number: 7495109
    Abstract: 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: Grant
    Filed: January 11, 2005
    Date of Patent: February 24, 2009
    Assignee: Purdue Pharma L.P.
    Inventors: Qun Sun, R. Richard Goehring, Donald Kyle, Zhengming Chen, Sam Victory, John Whitehead
  • Publication number: 20090042931
    Abstract: 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: Application
    Filed: April 12, 2006
    Publication date: February 12, 2009
    Applicant: Vicore Pharma AB
    Inventors: Mathias Alterman, Anders Hallberg, Xiongyu Wu
  • Publication number: 20090030016
    Abstract: 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: Application
    Filed: July 15, 2008
    Publication date: January 29, 2009
    Applicant: ABBOTT LABORATORIES
    Inventors: Virajkumar B. Gandhi, Vincent L. Giranda, Jianchun Gong, Thomas D. Penning, Gui-Dong Zhu
  • Patent number: 7479502
    Abstract: 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: Grant
    Filed: December 3, 2003
    Date of Patent: January 20, 2009
    Assignee: Pharmacyclics, Inc.
    Inventors: Aleksandr Kolesnikov, Roopa Rai, William Dvorak Shrader, Steven M. Torkelson, Kieron E. Wesson, Wendy B. Young
  • Patent number: 7465807
    Abstract: The present invention provides a process for preparing benzimidazole thiophene compounds.
    Type: Grant
    Filed: October 12, 2004
    Date of Patent: December 16, 2008
    Assignee: SmithKline Beecham Corporation
    Inventors: Mui Cheung, Kyle Allen Emmitte
  • Patent number: 7462724
    Abstract: 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: Grant
    Filed: November 15, 2006
    Date of Patent: December 9, 2008
    Assignee: Abbott Laboratories
    Inventors: Thomas D. Penning, Sheela A. Thomas, Gui-Dong Zhu, Jianchun Gong, Vincent L. Giranda, Viraj B. Gandhi
  • Patent number: 7459566
    Abstract: 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: Grant
    Filed: March 2, 2007
    Date of Patent: December 2, 2008
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Georg Zerban, Arndt Hausherr, Kerstin Schlarb, Heinz-Peter Schmitt, Bjoern Weyell, Gunter Koch, Rainer Hamm
  • Publication number: 20080269298
    Abstract: 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: Application
    Filed: May 1, 2008
    Publication date: October 30, 2008
    Inventors: 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
  • Patent number: 7439258
    Abstract: 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: Grant
    Filed: May 21, 2004
    Date of Patent: October 21, 2008
    Assignee: Boehringer Ingelheim (Canada) Ltd
    Inventors: Pierre Louis Beaulieu, Gulrez Fazal, James Gillard, George Kukolj, Volkhard Austel
  • Publication number: 20080249301
    Abstract: The present invention provides a process for preparing benzimidazole thiophene compounds of formula (I). Intermediates used in the process are also claimed.
    Type: Application
    Filed: August 28, 2006
    Publication date: October 9, 2008
    Inventors: Keith Hornberger, Mui Cheung, Mark Andrew Pobanz, Kyle Allen Emmitte, Kevin Wayne Kuntz, Jennifer Gabriel Badiang
  • Patent number: 7425637
    Abstract: 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: Grant
    Filed: February 18, 2005
    Date of Patent: September 16, 2008
    Assignee: Array BioPharma Inc.
    Inventors: Eli M. Wallace, Joseph P. Lyssikatos, Allison L. Marlow, T. Brian Hurley
  • Patent number: 7414046
    Abstract: 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: Grant
    Filed: May 23, 2003
    Date of Patent: August 19, 2008
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: Anne-Laure Grillot, Paul Charifson, Dean Stamos, Yusheng Liao, Michael Badia, Martin Trudeau
  • Patent number: 7410989
    Abstract: 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: Grant
    Filed: November 20, 2006
    Date of Patent: August 12, 2008
    Assignees: The University of North Carolina at Chapel Hill, Georgia State University Research Foundation, Inc., Auburn University
    Inventors: Christine C. Dykstra, Maurice Daniel Givens, David A. Stringfellow, Kenny Brock, David Boykin, Arvid Kumar, W. David Wilson, Richard R. Tidwell, Chad F. Stephens
  • Patent number: 7410990
    Abstract: 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: Grant
    Filed: October 3, 2006
    Date of Patent: August 12, 2008
    Assignee: Synta Pharmaceuticals Corp.
    Inventors: Lijun Sun, Mitsunori Ono, Yumiko Wada, Weiwen Ying, Teresa Przewloka, Elena Kostik
  • Publication number: 20080188668
    Abstract: 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: Application
    Filed: April 11, 2008
    Publication date: August 7, 2008
    Inventor: Stephen Freeman
  • Publication number: 20080146797
    Abstract: 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: Application
    Filed: February 6, 2008
    Publication date: June 19, 2008
    Applicant: SANOFI-AVENTIS DEUTSCHLAND GMBH
    Inventors: Uwe HEINELT, Hans-Jochen LANG
  • Patent number: 7371870
    Abstract: 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: Grant
    Filed: June 23, 2004
    Date of Patent: May 13, 2008
    Assignee: Dainippon Ink and Chemicals, Inc.
    Inventors: Masaki Hosaka, Toshio Takei
  • Patent number: 7368467
    Abstract: 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: Grant
    Filed: March 7, 2005
    Date of Patent: May 6, 2008
    Assignee: Wyeth
    Inventors: Robert Zelle, Vincent P. Galullo, Hormoz Mazdiyasni
  • Patent number: 7335777
    Abstract: This invention relates to novel benzimidazole derivatives of formula (I), pharmaceutical compositions containing these compounds, and methods of treatment therewith.
    Type: Grant
    Filed: April 1, 2004
    Date of Patent: February 26, 2008
    Assignee: Neurosearch A/S
    Inventors: Lene Teuber, Janus S. Larsen
  • Patent number: 7309716
    Abstract: 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: Grant
    Filed: October 28, 2004
    Date of Patent: December 18, 2007
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: Dean M. Wilson, Andreas P. Termin, Jesus E. Gonzalez, III, Nicole Zimmermann, Yulian Zhang, Lev T. D. Fanning
  • Patent number: 7300928
    Abstract: 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: Grant
    Filed: May 3, 2006
    Date of Patent: November 27, 2007
    Assignee: Acadia Pharmaceuticals, Inc.
    Inventors: Nicholas Michael Kelly, Kristian Norup Koch, Bo-Ragnar Tolf
  • Patent number: 7291611
    Abstract: 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: Grant
    Filed: July 21, 2005
    Date of Patent: November 6, 2007
    Assignee: ACADIA Pharmaceuticals Inc.
    Inventors: Nicholas Michael Kelly, Kristian Norup Koch, Bo-Ragnar Tolf
  • Patent number: 7271271
    Abstract: 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: Grant
    Filed: June 27, 2005
    Date of Patent: September 18, 2007
    Assignee: Amgen SF, LLC
    Inventors: 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
  • Patent number: 7271270
    Abstract: 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: Grant
    Filed: May 24, 2004
    Date of Patent: September 18, 2007
    Assignee: Neurogen Corporation
    Inventors: Andrew Thurkauf, Xiao-shu He, He Zhao
  • Patent number: 7268255
    Abstract: 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: Grant
    Filed: February 19, 2004
    Date of Patent: September 11, 2007
    Assignee: Lonza AG
    Inventors: Ulrich Kampfen, Dario Veghini, Dominique Roberge, Jared Randall
  • Patent number: 7250427
    Abstract: 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: Grant
    Filed: June 27, 2005
    Date of Patent: July 31, 2007
    Assignee: Janssen Pharmaceutica, N.V.
    Inventors: J. Guy Breitenbucher, Alice Lee-Dutra, Danielle K. Neff
  • Patent number: 7235558
    Abstract: 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: Grant
    Filed: June 4, 2003
    Date of Patent: June 26, 2007
    Assignees: Sanofi-Aventis Deutschland GmbH, Ajinomoto Co., Inc
    Inventors: Otmar Klingler, Melitta Just, Kuniya Sakurai, Naoyuki Fukuchi
  • Patent number: 7202368
    Abstract: 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: Grant
    Filed: June 9, 2005
    Date of Patent: April 10, 2007
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Georg Zerban, Arndt Hausherr, Kerstin Schlarb, Heinz-Peter Schmitt, Bjoern Weyell, Gunter Koch, Rainer Hamm
  • Patent number: 7183286
    Abstract: 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: Grant
    Filed: March 9, 2004
    Date of Patent: February 27, 2007
    Assignees: 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
  • Patent number: 7148226
    Abstract: 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: Grant
    Filed: November 19, 2003
    Date of Patent: December 12, 2006
    Assignee: Agouron Pharmaceuticals, Inc.
    Inventors: Allen Borchardt, Javier Gonzalez, Hui Li, Maria Angelica Linton, John Howard Tatlock
  • Patent number: RE40245
    Abstract: 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: Grant
    Filed: April 28, 2004
    Date of Patent: April 15, 2008
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: Anne-Laure Grillot, Paul S. Charifson, Dean Stamos, Yusheng Liao, Michael C. Badia, Martin Trudeau