Chalcogen Bonded Directly To Ring Carbon Of The Diazole Ring Patents (Class 548/306.4)
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Composition for treating cancer or inhibiting cancer metastasis, including TFG or TFMG nanoparticles
Patent number: 11638741Abstract: The present invention relates to a composition for preventing or treating cancer, a composition for inhibiting the metastasis of cancer, and the like, including TFG nanoparticles or TFMG nanoparticles, and more particularly, to a composition exhibiting effects of treating cancer, effects of inhibiting the metastasis of cancer, and the like by normalizing blood vessels inside a tumor.Type: GrantFiled: November 19, 2019Date of Patent: May 2, 2023Assignee: KYUNGPOOK NATIONAL UNIVERSITY INDUSTRY-ACADEMIC COOPERATION FOUNDATIONInventors: You-Mie Lee, Jong-Sup Bae -
Patent number: 10702504Abstract: The present application provides bifunctional compounds of Formula Ia or Ib: or a pharmaceutically acceptable salt, hydrate, solvate, prodrug, stereoisomer, or tautomer thereof, which act as protein degradation inducing moieties for tripartite motif-containing 24 (TRIM24). The present application also relates to methods for the targeted degradation of TRIM24 through the use of the bifunctional compounds that link a ubiquitin ligase-binding moiety to a ligand that is capable of binding to TRIM24 which can be utilized in the treatment of disorders modulated by TRIM24.Type: GrantFiled: June 23, 2017Date of Patent: July 7, 2020Assignee: DANA-FARBER CANCER INSTITUTE, INC.Inventors: James Bradner, Dennis Buckley, Lara Gechijian
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Patent number: 10357487Abstract: A method of treating one or more symptoms associated with underactive bladder in a patient suffering therefrom by administering to the patient a therapeutically effective amount of an acetylcholinesterase inhibitor (AChEI) and an amount of a muscarinic receptor agonist effective to reduce the volume of post void residual in the patient obtained by treatment with the AChEI alone.Type: GrantFiled: December 5, 2016Date of Patent: July 23, 2019Inventor: Sidney J. Goldfarb
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Patent number: 9890108Abstract: The present invention relates to a process for the preparation of amines, comprising the following steps: Reaction of a (i) amide acetal of the general formula (I), or (ii) ketene N,O-acetal of the general formula (II), or (iii) ester imide of the general formula (III) with H2 in the presence of a hydrogenation catalyst, where catalyst and amide acetal or ketene N,O-acetal or ester imide are used in a molar ratio of from 1:10 to 1:100 000 and where a hydrogen pressure of from 0.1 bar to 200 bar is established and where a temperature in the range of from 0° C. to 250° C. is established.Type: GrantFiled: October 15, 2014Date of Patent: February 13, 2018Assignee: Evonik Degussa GmbHInventor: Renat Kadyrov
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Publication number: 20150126553Abstract: The present disclosure is directed in part to bicyclic heterocycles, such as a compound represented by formula (I) or (II) as disclosed herein, and their use in treating medical disorders, such as immune inflammatory disorders such as Crohn's disease, ulcerative colitis, rheumatic disorders, psoriasis, and allergies. The compounds are contemplated to modulate T-Cell responses.Type: ApplicationFiled: May 31, 2013Publication date: May 7, 2015Inventors: Daan Hommes, Auke Verhaar, Gijs Van den Brink, Francesca Viti
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Patent number: 8993779Abstract: The present invention is directed to benzimidazolone derivatives which are positive allosteric modulators of the mGluR2 receptor, useful in the treatment or prevention of neurological and psychiatric disorders associated with glutamate dysfunction and diseases in which the mGluR2 receptor is involved. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which metabotropic glutamate receptors are involved, such as schizophrenia.Type: GrantFiled: August 5, 2011Date of Patent: March 31, 2015Assignee: Merck Sharp & Dohme Corp.Inventors: Vadim Y. Dudkin, Mark E. Fraley, Kenneth L. Arrington, Mark E. Layton, Alexander J. Reif, Kevin J. Rodzinak, Joseph E. Pero
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Patent number: 8987473Abstract: The present invention relates to a compound that has URAT1 inhibitory action, and a URAT1 inhibitor, a blood uric acid level-reducing agent and a pharmaceutical composition comprising the compound. More specifically, the present invention relates to a compound represented by Formula (I) below.Type: GrantFiled: January 30, 2012Date of Patent: March 24, 2015Assignee: Sato Pharmaceutical Co., Ltd.Inventors: Keita Nagai, Koh Nagasawa, Hirobumi Takahashi, Motoaki Baba, Shinichi Fujioka, Eri Kondoh, Kenichi Tanaka, Yoshiki Itoh
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Publication number: 20140323519Abstract: This invention relates to novel heterocyclic compounds that are useful for treating cancer and other cellular proliferative diseases and/or disorders associated with B-Raf activity. The compounds of the invention may be illustrated by the Formula (I).Type: ApplicationFiled: April 20, 2012Publication date: October 30, 2014Applicant: MERCK SHARP & DOHME CORP.Inventors: M. Arshad Siddiqui, Lianyun Zhao, Amit K. Mandal
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Publication number: 20140219995Abstract: Organic compounds showing the ability to inhibit effector toxin secretion or translocation mediated by bacterial type III secretion systems are disclosed. The disclosed type III secretion system inhibitor compounds are useful for combating infections by Gram-negative bacteria such as Salmonella spp., Shigella flexneri, Pseudomonas spp., Yersinia spp., enteropathogenic and enteroinvasive Escherichia coli, and Chlamydia spp. having such type III secretion systems.Type: ApplicationFiled: July 13, 2012Publication date: August 7, 2014Applicant: MICROBIOTIX, INC.Inventors: Donald T. Moir, Daniel Aiello, Norton P. Peet, John D. Williams, Matthew Torhan
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Patent number: 8658207Abstract: The present invention provides pharmaceutical release systems comprising an therapeutically effective amount of flibanserin and at least one pharmaceutically acceptable excipient, characterized in that said pharmaceutical release systems exhibit a pharmacokinetic profile that is characterized by an average maximum flibanserin plasma concentration Cmax lower than 300 ng/mL, preferably lower than 200 ng/mL after administration of a single dose to healthy volunteers in fasted state or directly after a meal.Type: GrantFiled: August 13, 2007Date of Patent: February 25, 2014Assignee: Boehringer Ingelheim International GmbHInventors: Wolfram Eisenreich, Thomas Friedl, Florian Sommer, Nantharat Pearnchob, Karl G. Wagner
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Publication number: 20140031403Abstract: The present invention provides forms of curcumin and the pharmaceutical compositions thereof. The forms of curcumin disclosed herein are curcumin polymorph Form III, curcumin-2-aminobenzimidazole co-crystal, and curcumin-L-lysine co-crystal. Further, the invention provides methods inhibiting cancer cells and HSV-1 using these curcumin novel solid forms.Type: ApplicationFiled: April 5, 2012Publication date: January 30, 2014Applicants: VAN ANDEL RESEARCH INSTITUTE, THE TRANSLATIONAL GENOMICS RESEARCH INSTITUTEInventors: Stephen T. Gately, Steven J. Triezenberg, Tong Wang
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Publication number: 20140005221Abstract: The present invention relates to a compound that has URAT1 inhibitory action, and a URAT1 inhibitor, a blood uric acid level-reducing agent and a pharmaceutical composition comprising the compound. More specifically, the present invention relates to a compound represented by Formula (I) below.Type: ApplicationFiled: January 30, 2012Publication date: January 2, 2014Applicant: SATO PHARMACEUTICAL CO., LTD.Inventors: Keita Nagai, Koh Nagasawa, Hirobumi Takahashi, Motoaki Baba, Shinichi Fujioka, Eri Kondoh, Kenichi Tanaka, Yoshiki Itoh
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Publication number: 20130306955Abstract: A specific nitrogen-containing heterocyclic compound having a urea structure, an electron transporting material containing the nitrogen-containing heterocyclic compound, and an organic electroluminescence device including a light emitting layer and an electron transporting layer between a cathode and an anode in which the electron transporting layer includes the electron transporting material or the nitrogen-containing heterocyclic derivative. An organic EL device exhibiting high emission efficiency even at low voltage and a material for organic EL devices are described.Type: ApplicationFiled: February 1, 2012Publication date: November 21, 2013Applicant: IDEMITSU KOSAN CO., LTD.Inventors: Sayaka Mizutani, Takayasu Sado, Hiroki Ishida
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Patent number: 8563746Abstract: Novel compounds of the structural formula (I) are activators of AMP-protein kinase and are useful in the treatment, prevention and suppression of diseases mediated by the AMPK-activated protein kinase. The compounds of the present invention are useful in the treatment of Type 2 diabetes, hyperglycemia, metabolic syndrome, obesity, hypercholesterolemia, and hypertension.Type: GrantFiled: October 19, 2009Date of Patent: October 22, 2013Assignees: Merck Sharp & Dohme Corp, Metabasis Therapeutics, Inc.Inventors: Qun Dang, De Michael Chung, Tony S. Gibson, Hongjian Jiang, Daniel K. Cashion, Jianming Bao, Ping Lan, Huagang Lu, Gergely M. Makara, F. Anthony Romero, Iyassu Sebhat, Dariusz Wodka
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Patent number: 8552019Abstract: The instant invention provides for compounds of formula A that inhibit PDK1 activity: The invention also provides for compositions comprising such inhibitory compounds and methods of inhibiting PDK1 activity by administering the compound to a patient in need of treatment of cancer.Type: GrantFiled: November 24, 2009Date of Patent: October 8, 2013Assignee: Merck Sharp & Dohme Corp.Inventors: Kevin A. Keenan, Alan B. Northrup
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Patent number: 8545886Abstract: The invention is directed to a Pharmaceutical extended release system, particularly for oral administration, of a pH-dependent water-soluble active substance, comprising or essentially consisting of a) flibanserin or a pharmaceutically acceptable derivative thereof as active substance; b) one or more pharmaceutically acceptable pH-dependent polymers; c) one or more pharmaceutically acceptable pH-independent polymers; d) one or more pharmaceutically acceptable acids; and e) optionally one or more additives. The present invention provides a release profile of flibanserin which is independent on the pH in the gastrointestinal tract when administered orally resulting in a significantly improved bioavailability.Type: GrantFiled: August 13, 2007Date of Patent: October 1, 2013Assignee: Boehringer Ingelheim International GmbHInventors: Wolfram Eisenreich, Thomas Friedl
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Publication number: 20130172335Abstract: The present invention relates to compounds of formula I wherein R1a to R1e, R2, R3 and R5 are as defined in the description and claims and R4 signifies a bicyclic heteroaryl group or a cyanophenyl group, as well as pharmaceutically acceptable salts thereof. The compounds are glucocorticoid receptor antagonists useful for the treatment and/or prevention of diseases such as diabetes, dyslipidemia, obesity, hypertension, cardiovascular diseases, adrenal imbalance or depression.Type: ApplicationFiled: February 22, 2013Publication date: July 4, 2013Applicant: Hoffmann-La Roche Inc.Inventor: Hoffmann-La Roche Inc.
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Patent number: 8461351Abstract: A sterically bulky stabilizer that includes an alkylated-benzimidazolone compound, where the sterically bulky stabilizer is associated non-covalently with a benzimidazolone pigment, and the presence of the sterically bulky stabilizer limits the extent of particle growth and aggregation, to afford nanoscale pigment particles.Type: GrantFiled: July 28, 2011Date of Patent: June 11, 2013Assignees: Xerox Corporation, National Research Council of CanadaInventors: Rina Carlini, Darren Andrew Makeiff
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Publication number: 20130143880Abstract: The present invention is directed to benzimidazolone derivatives which are positive allosteric modulators of the mGluR2 receptor, useful in the treatment or prevention of neurological and psychiatric disorders associated with glutamate dysfunction and diseases in which the mGluR2 receptor is involved. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which metabotropic glutamate receptors are involved, such as schizophrenia.Type: ApplicationFiled: August 5, 2011Publication date: June 6, 2013Inventors: Vadim Y. Dudkin, Mark E. Fraley, Kenneth L. Arrington, Mark E. Layton, Alexander J. Reif, Kevin J. Rodzinak, Joseph E. Pero
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Patent number: 8450313Abstract: The present invention relates to compounds of formula I wherein R1a to R1e, R2, R3 and R5 are as defined in the description and claims and R4 signifies a bicyclic heteroaryl group or a cyanophenyl group, as well as pharmaceutically acceptable salts thereof. The compounds are glucocorticoid receptor antagonists useful for the treatment and/or prevention of diseases such as diabetes, dyslipidemia, obesity, hypertension, cardiovascular diseases, adrenal imbalance or depression.Type: GrantFiled: May 22, 2012Date of Patent: May 28, 2013Assignee: Hoffmann-La Roche Inc.Inventors: Daniel Hunziker, Christian Lerner, Werner Mueller, Ulrike Obst Sander, Philippe Pflieger, Pius Waldmeier
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Publication number: 20130109672Abstract: Disclosed are pyruvate kinase M2 activators which are compounds of Formula (I), including those of Formula (II), wherein A1, A2, L, R, R1 to R3, X1 to X3, k, n, and m are as defined herein, that are useful in treating a number of diseases that are treatable by the activation of PKM2, for example, cancer. A1-NR-L-A2 (I).Type: ApplicationFiled: April 26, 2011Publication date: May 2, 2013Applicant: The United States of America,as represented by the Secretary, Department of Health and Human ServiceInventors: Matthew B. Boxer, Min Shen, Douglas S. Auld, Craig J. Thomas, Martin J. Walsh
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Patent number: 8410284Abstract: Novel compounds of the structural formula (I) are activators of AMP-protein kinase and are useful in the treatment, prevention and suppression of diseases mediated by the AMPK-activated protein kinase. The compounds of the present invention are useful in the treatment of Type 2 diabetes, hyperglycemia, Metabolic Syndrome, obesity, hypercholesterolemia, and hypertension.Type: GrantFiled: October 12, 2009Date of Patent: April 2, 2013Assignees: Merck Sharp & Dohme Corp, Metabasis Therapeutics, Inc.Inventors: Qun Dang, Tony S. Gibson, Hongjian Jiang, De Michael Chung, Jianming Bao, Jinlong Jiang, Andy Kassick, Ahmet Kekec, Ping Lan, Huagang Lu, Gergely M. Makara, F. Anthony Romero, Iyassu Sebhat, David Wilson, Dariusz Wodka, Brett C. Bookser
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Patent number: 8410283Abstract: An electrolyte additive is selected from N-alkyl benzimidazole derivatives and is applicable to dye-sensitized solar cells. Accordingly, the electrolyte additive can be added to electrolyte at low concentration, and loss of function due to crystallization after long-term use can be prevented; in addition, short circuit photocurrent density and solar energy-to-electricity conversion efficiency of solar cells incorporating the electrolyte additive can be increased.Type: GrantFiled: July 15, 2010Date of Patent: April 2, 2013Assignee: National Taipei University of TechnologyInventors: Sheng-Tung Huang, Chung-Kuang Yang
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Publication number: 20130079339Abstract: The invention discloses compounds of formula I wherein Y is a group of formula A, B, C, D, or E: and W, Q, n, R1, R2, R3, U1-U5, J and K have the meanings given in the description. The compounds of formula I are TRPV1 antagonists and are useful as active ingredients of pharmaceutical compositions for the treatment of pain and other conditions ameliorated by the inhibition of the vanilloid receptor TRPV1.Type: ApplicationFiled: December 22, 2010Publication date: March 28, 2013Applicant: PHARMESTE S.R.L.Inventors: Mauro Napoletano, Marcello Trevisani, Maria Giovanna Pavani, Francesca Fruttarolo
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Patent number: 8394969Abstract: Novel compounds of the structural formula (I) are activators of AMP-protein kinase and are useful in the treatment, prevention and suppression of diseases mediated by the AMPK-activated protein kinase. The compounds of the present invention are useful in the treatment of Type 2 diabetes, hyperglycemia, metabolic syndrome, obesity, hypercholesterolemia, and hypertension.Type: GrantFiled: September 21, 2009Date of Patent: March 12, 2013Assignee: Merck Sharp & Dohme Corp.Inventors: Brett C. Bookser, Qun Dang, Tony S. Gibson, Hongjian Jiang, De Michael Chung, Jianming Bao, Jinlong Jiang, Andy Kassick, Ahmet Kekec, Ping Lan, Huagang Lu, Gergely M. Makara, F. Anthony Romero, Iyassu Sebhat, David Wilson, Dariusz Wodka
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Patent number: 8362270Abstract: An alkylated benzimidazolone compound of the formula: wherein at least one of R1 to R4 is X—Rc, where X represents a linking group, and Ra, Rb, and Rc independently represents substituted or unsubstituted alkyl groups, provided that at least one of Ra and Rb represents H. The present disclosure provides alkylated benzimidazolone compounds and self-assembled nanostructures formed from alkylated benzimidazolone compounds.Type: GrantFiled: May 11, 2010Date of Patent: January 29, 2013Assignees: Xerox Corporation, National Research Council of CanadaInventors: Darren Andrew Makeiff, Rina Carlini, Hicham Fenniri
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Patent number: 8354434Abstract: The invention relates to cyclourea compounds of Formula I: or a pharmaceutically acceptable salt or solvate thereof, wherein R1-R3 and Z are defined as set forth in the specification. The invention is also directed to the use of compounds of Formula I to treat, prevent or ameliorate a disorder responsive to the blockade of calcium channels, and particularly N-type calcium channels. Compounds of the present invention are especially useful for treating pain.Type: GrantFiled: January 15, 2007Date of Patent: January 15, 2013Assignee: Purdue Pharma L.P.Inventor: Xiaoming Zhou
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Publication number: 20120322830Abstract: The invention relates to cyclourea compounds of Formula I: or a pharmaceutically acceptable salt or solvate thereof, wherein R1-R3 and Z are defined as set forth in the specification. The invention is also directed to the use of compounds of Formula I to treat, prevent or ameliorate a disorder responsive to the blockade of calcium channels, and particularly N-type calcium channels. Compounds of the present invention are especially useful for treating pain.Type: ApplicationFiled: June 11, 2012Publication date: December 20, 2012Applicant: Purdue Pharma L.P.Inventor: Xiaoming ZHOU
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Publication number: 20120309736Abstract: Novel compounds of the structural formula (I) are activators of AMP-protein kinase and are useful in the treatment, prevention and suppression of diseases mediated by the AMPK-activated protein kinase. The compounds of the present invention are useful in the treatment of Type 2 diabetes, hyperglycemia, metabolic syndrome, obesity, hypercholesterolemia, and hypertension.Type: ApplicationFiled: February 21, 2011Publication date: December 6, 2012Inventors: Jinlong Jiang, Andrew J. Kassick, Ahmet Kekec, Iyassu K. Sebhat
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Patent number: 8293777Abstract: A compound having the structure wherein R is an angiotensin receptor antagonist active group, and Y is Y is selected from the group consisting of R1 is selected from the group consisting of —O—C1-6 alkyl, —O-aryl, —O-heteroaryl, —O—C3-8 cycloalkyl, —C1-6 alkyl, -aryl, -heteroaryl, and —C3-8 cycloalkyl; R2 and R3 are independently selected from the group consisting of hydrogen and C1-4 alkyl, or a pharmaceutically acceptable salt or hydrate thereof, which is useful for treating hypertension.Type: GrantFiled: December 2, 2009Date of Patent: October 23, 2012Assignee: Merck Sharp & Dohme, Corp.Inventors: Michael Man-Chu Lo, Amjad Ali, Ravi P. Nargund
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Publication number: 20120232071Abstract: The present invention relates to compounds of formula I wherein R1a to R1e, R2, R3 and R5 are as defined in the description and claims and R4 signifies a bicyclic heteroaryl group or a cyanophenyl group, as well as pharmaceutically acceptable salts thereof. The compounds are glucocorticoid receptor antagonists useful for the treatment and/or prevention of diseases such as diabetes, dyslipidemia, obesity, hypertension, cardiovascular diseases, adrenal imbalance or depression.Type: ApplicationFiled: May 22, 2012Publication date: September 13, 2012Inventors: Daniel Hunziker, Christian Lerner, Werner Mueller, Ulrike Obst Sander, Philippe Pflieger, Pius Waldmeier
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Publication number: 20120232194Abstract: Provided is a phthalocyanine compound which is halogen-free and which has a green hue, excellent resistance to organic solvents and acids, and high chroma. Also provided are a metal-free phthalocyanine compound or a metal phthalocyanine compound represented by specified general formula (1-1) or (1-2) and having a N,N?-disubstituted imidazolone structure or piperazinedione structure introduced therein, and a coloring composition including the compound and a synthetic resin. The phthalocyanine compound of the present invention exhibits a clear green color and is halogen-free, and is thus useful as a clear green pigment for coloring materials such as a coating material, plastic, a printing ink, rubber, leather, textile printing, a color filter, a jet ink, a heat transfer ink, etc.Type: ApplicationFiled: August 6, 2010Publication date: September 13, 2012Inventors: Hitoshi Kondou, Yoshiyuki Sano, Yutaka Tachikawa
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Publication number: 20120225871Abstract: Provided are small-molecule Trp-p8 modulators, including Trp-p8 agonists and Trp-p8 antagonists, and compositions comprising small-molecule Trp-p8 agonists as well as methods for identifying and characterizing novel small-molecule Trp-p8 modulators and methods for decreasing viability and/or inhibiting growth of Trp-p8 expressing cells, methods for activating Trp-p8-mediated cation influx, methods for stimulating apoptosis and/or necrosis, and related methods for the treatment of diseases, including cancers such as lung, breast, colon, and/or prostate cancers as well as other diseases, such as benign prostatic hyperplasia, that are associated with Trp-p8 expression.Type: ApplicationFiled: June 8, 2010Publication date: September 6, 2012Applicant: Dendreon CorporationInventors: Ofir Moreno, Sateesh Natarajan, David F. Duncan
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Patent number: 8242284Abstract: The present disclosure relates to novel compounds having the structural Formulas (1a,1b), stereoisomers, tautomers, racemics, prodrugs, metabolites thereof, or pharmaceutically acceptable salt and/or solvate thereof as chemotherapy agents for treating of cancer, particularly androgen-independent prostate cancer. The disclosure also relates to methods for preparing said compounds, and to pharmaceutical compositions comprising said compounds.Type: GrantFiled: August 24, 2010Date of Patent: August 14, 2012Assignee: The United States of America as represented by the United States Department of EnergyInventors: Andrei A. Gakh, Mykhaylo V. Vovk, Nina V. Mel'nychenko, Volodymyr A. Sukach
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Patent number: 8232312Abstract: The present invention relates to substituted arylsulphonylglycines of general formula (I) wherein R, X, Y and Z are defined as in claim 1, the tautomers, enantiomers, diastereomers, mixtures thereof and salts thereof, which have valuable pharmacological properties, particularly the suppression of the interaction of glycogen phosphorylase a with the GL subunit of glycogen-associated protein phosphatase 1 (PP1), and their use as pharmaceutical compositions.Type: GrantFiled: March 14, 2008Date of Patent: July 31, 2012Assignee: Boehringer Ingelheim International GmbHInventors: Holger Wagner, Elke Langkopf, Matthias Eckhardt, Ruediger Streicher, Corinna Schoelch, Annette Schuler-Metz, Alexander Pautsch
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Patent number: 8207182Abstract: The present invention relates to substituted cyclic urea derivatives corresponding to formula I, to processes for the preparation thereof, to medicinal drugs containing such compounds, to the use of such compounds in the preparation of medicinal drugs and in related treatment methods.Type: GrantFiled: October 19, 2007Date of Patent: June 26, 2012Assignee: Gruenenthal GmbHInventors: Robert Frank, Bernd Sundermann, Hans Schick, Helmut Sonnenschein
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Patent number: 8173818Abstract: Disclosed herein, a process for producing sulphoxide compound of the Formula (I) by asymmetrically oxidizing a prochiral sulphide of the Formula (II) with an effective amount of oxidizing agent in the presence of a chiral transition metal complex without using an organic solvent and base.Type: GrantFiled: August 8, 2007Date of Patent: May 8, 2012Assignee: Jubilant Organosys LimitedInventors: Anand Singh, Khushwant Singh, Sushil Kumar Dubey
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Patent number: 8163935Abstract: There is provided a CRF receptor antagonist comprising a compound of the formula (I): wherein R1 is an optionally substituted hydrocarbyl, an optionally substituted C-linked heterocyclic group, an optionally substituted N-linked heteroaryl group, a cyano or an acyl; R2 is an optionally substituted cyclic hydrocarbyl or an optionally substituted heterocyclic group; X is oxygen, sulfur or —NR3— (wherein R3 is a hydrogen, an optionally substituted hydrocarbyl or an acyl); Y1, Y2 and Y3 are each an optionally substituted carbon or a nitrogen, provided that one or less of Y1, Y2 and Y3 is nitrogen; and Z is a bond, —CO—, oxygen, sulfur, —SO—, —SO2—, —NR4—, —NR4-alk-, —CONR4— or —NR4CO— (wherein alk is an optionally substituted C1-4 alkylene and R4 is a hydrogen, an optionally substituted hydrocarbyl or an acyl); or a salt thereof or a prodrug thereof.Type: GrantFiled: April 26, 2006Date of Patent: April 24, 2012Assignee: Takeda Pharmaceutical Company LimitedInventors: Kazuyoshi Aso, Michiyo Mochizuki, Albert Charles Gyorkos, Christopher Peter Corrette, Suk Young Cho, Scott Alan Pratt, Christopher Stephen Siedem
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Patent number: 8119676Abstract: The present invention relates to novel benzimidazolone derivatives of the general formula (I) in which the substituents R1, R2, R3, A1, A2, and B are as defined in claim 1, medicaments comprising these, and the use thereof for the prophylaxis and/or treatment of vasopressin-dependent diseases.Type: GrantFiled: August 24, 2007Date of Patent: February 21, 2012Assignee: Abbott GmbH & Co. HGInventors: Torsten Arndt, Thorsten Oost, Wilfried Lubisch, Wolfgang Wernet, Alfred Hahn, legal representative, Wilfried Hornberger, Liliane Unger, Juliana Ruiz Caro
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Publication number: 20110301156Abstract: Vanilloid receptor ligand compounds corresponding to formula I: pharmaceutical compositions containing such compounds, a process for producing such compounds, and methods of using such compounds for treating or inhibiting pain and various other disorders or conditions.Type: ApplicationFiled: August 16, 2011Publication date: December 8, 2011Applicant: Gruenenthal GmbHInventors: Robert Frank, Gregor Bahrenberg, Thomas Christoph, Klaus Schiene, Jean De Vry, Derek Saunders, Bernd Sundermann, Jeewoo Lee
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Publication number: 20110282072Abstract: An alkylated benzimidazolone compound of the formula: wherein at least one of R1 to R4 is X—Rc, where X represents a linking group, and Ra, Rb, and Rc independently represents substituted or unsubstituted alkyl groups, provided that at least one of Ra and Rb represents H. The present disclosure provides alkylated benzimidazolone compounds and self-assembled nanostructures formed from alkylated benzimidazolone compounds.Type: ApplicationFiled: May 11, 2010Publication date: November 17, 2011Applicants: NATIONAL RESEARCH COUNCIL OF CANADA, XEROX CORPORATIONInventors: Darren Andrew MAKEIFF, Rina Carlini, Hicham Fenniri
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Publication number: 20110281879Abstract: The present invention is directed to compounds that are inhibitors of cysteine proteases, in particular, cathepsins B, K, L, F, and S and are therefore useful in treating diseases mediated by these proteases. The present invention is directed to pharmaceutical compositions comprising these compounds and processes for preparing them.Type: ApplicationFiled: January 12, 2011Publication date: November 17, 2011Applicant: ViroBay, Inc.Inventor: Craig Mossman
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Patent number: 8044078Abstract: The invention relates to a compound of the general formula (I), as defined herein which is useful for the treatment of a pathology in a patient wherein a CCR3 receptor plays a role in the development of the pathology, and pharmaceutical preparations containing such compound. The invention is also directed to a process for preparing the compound of the general formula (I), and intermediate useful in the preparation.Type: GrantFiled: March 19, 2008Date of Patent: October 25, 2011Assignee: Sanofi-AventisInventors: Agnes Pappne Behr, Zoltan Kapui, Peter Aranyi, Sandor Batori, Veronika Bartane Bodor, Lajos T. Nagy, Mihalyne Santa, legal representative, Marton Varga, Endre Mikus, Katalin Urban-Szabo, Judit Vargane Szeredi, Tibor Szabo, Edit Susan, Marianna Kovacs
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Publication number: 20110251200Abstract: The invention provides to a family of aryl guanidine-based F1F0-ATPase inhibitors, e.g., mitochondrial F1F0-ATPase inhibitors, methods for their discovery, and their use as therapeutic agents for treating certain disorders.Type: ApplicationFiled: September 11, 2009Publication date: October 13, 2011Applicant: THE REGENTS OF THE UNIVERSITY OF MICHIGANInventors: Gary D. Glick, Peter Toogood, Gina Ney
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Patent number: 8022617Abstract: An organic compound having excellent heat resistance, an excellent amorphous nature, an excellent ability to transport charges, highly excited singlet and triplet states, and excellent solubility in an organic solvent is an organic compound represented by Formula (I): wherein Ar1 represents an optionally-substituted aromatic hydrocarbon group, an optionally-substituted aromatic heterocyclic group, or an optionally-substituted alkyl group; Ar2 represents an optionally-substituted aromatic hydrocarbon group or an optionally-substituted aromatic heterocyclic group; R1 and R2 each represent a hydrogen atom or a substituent, and R1 and R2 may be bonded to each other to form a ring; and Q is represented by Formula (I-1) or (I-2): wherein Ar3 to Ar5 each represent an optionally-substituted aromatic hydrocarbon group or an optionally-substituted aromatic heterocyclic group, and Ar3 and Ar4 may be bonded to each other to form a ring.Type: GrantFiled: November 22, 2006Date of Patent: September 20, 2011Assignee: Mitsubishi Chemical CorporationInventors: Koichiro Iida, Yuichiro Kawamura, Tomoyuki Ogata, Masayoshi Yabe, Misako Okabe, Masako Takeuchi, Kazuki Okabe
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Publication number: 20110190509Abstract: New methods for the preparation of bendamustine, and the pharmaceutical salts thereof, are described. Novel compounds useful for the preparation of bendamustine are also described.Type: ApplicationFiled: April 5, 2011Publication date: August 4, 2011Applicant: Cephalon, Inc.Inventors: Jian Chen, Katrin Przyuski, Renee Caroline Roemmele
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Patent number: 7951955Abstract: This invention relates to compounds of formula I their salts, and pharmaceutically acceptable derivatives thereof, pharmaceutical compositions comprising these compounds and their use in the treatment of picornavirus infections in mammals, as well as novel intermediates useful in the preparation of the compounds of formula I.Type: GrantFiled: May 1, 2008Date of Patent: May 31, 2011Assignee: Biota Scientific Management Pty LtdInventors: Keith Watson, Guy Krippner, Pauline Stanislawski, Darryl McConnell
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Patent number: 7947709Abstract: Compounds of formula I, wherein R1, R2, R3, X and Ar, are as defined herein or pharmaceutically acceptable salts thereof, inhibit HIV-1 reverse transcriptase and afford a method for prevention and treatment of HIV-1 infections and the treatment of AIDS and/or ARC. The present invention also relates to compositions containing compounds of formula I useful for the prevention and treatment of HIV-1 infections and the treatment of AIDS and/or ARC.Type: GrantFiled: June 20, 2008Date of Patent: May 24, 2011Assignee: Roche Palo Alto LLCInventors: Todd Richard Elworthy, Joan Heather Hogg, Joshua Kennedy-Smith, Counde O'Yang, Mark Smith, Zachary Kevin Sweeney, Jeffrey Wu
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Patent number: 7906541Abstract: The invention relates to a new process leading to new substituted 1H-benzo[d]imidazol-2(3H)-ones of formula III and III?, to pharmaceutical compositions comprising them and to their use as therapeutic agents, particularly as BACE 1 inhibitors in the treatment of Alzheimer disease.Type: GrantFiled: December 8, 2008Date of Patent: March 15, 2011Assignee: Universite Paul Cezanne-Aix Marseille IIIInventors: Christian Roussel, Frederico Andreoli, Nicolas Daniel Pierre Vanthuyne
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Patent number: 7897619Abstract: The invention relates to heterocyclic compounds of Formula I and compositions thereof useful for treating diseases mediated by protein kinase B (PKB) where the variables have the definitions provided herein. The invention also relates to the therapeutic use of such compounds and compositions thereof in treating disease states associated with abnormal cell growth, cancer, inflammation, and metabolic disorders.Type: GrantFiled: July 16, 2008Date of Patent: March 1, 2011Assignee: Amgen Inc.Inventors: Qingping Zeng, Dawei Zhang, Guomin Yao, George E. Wohlhieter, Xianghong Wang, James Rider, Andreas Reichelt, Holger Monenschein, Fang-Tsao Hong, James R. Falsey, Celia Dominguez, Matthew P. Bourbeau, John G. Allen