Nitrogen Attached Directly To The Diazole Ring By Nonionic Bonding Patents (Class 548/307.4)
  • Patent number: 10300045
    Abstract: A veterinary composition is disclosed and is based on anthelmintic compounds, particularly from the benzimidazole group, with delayed release properties, preferably in the form of granules or pellets, to be added to feed or feed supplements offered to ruminants in order to control eggs and larvae of helminths, preferably from the genus Haemonchus spp.
    Type: Grant
    Filed: November 28, 2017
    Date of Patent: May 28, 2019
    Assignee: Champion USA LLC
    Inventors: Flavia Sette da Rocha, Flavio Alves da Rocha
  • Patent number: 9512082
    Abstract: Compounds of formula (I), combinations and uses thereof for disease therapy, or a pharmaceutically acceptable salt, solvate or polymorph thereof, including all tautomers and stereoisomers thereof wherein: A represents and B, R1, R2, R3, R4, R5, R6 and Z are as defined throughout the description and the claims.
    Type: Grant
    Filed: April 18, 2008
    Date of Patent: December 6, 2016
    Assignee: PROBIODRUG AG
    Inventors: Mirko Buchholz, Ulrich Heiser, André J. Niestroj
  • Patent number: 9216968
    Abstract: The present invention provides a novel heterocyclic derivative or a pharmaceutically acceptable salt thereof. For example, the present invention provides a heterocyclic derivative of the general formula [1] or its tautomer, or a pharmaceutically acceptable salt thereof: wherein R1 and R2 are the same or different aromatic rings, etc., and ring A is a heterocyclic ring. The compound of the invention or a pharmaceutically acceptable salt thereof has potent mPGES-1 inhibiting activity and is useful as an agent for the treatment or prevention of a disease, such as rheumatoid arthritis, osteoarthritis, temporomandibular joint disorders, low back pain, endometriosis, dysmenorrhea, overactive bladder, malignant tumors or neurodegenerative disease.
    Type: Grant
    Filed: August 17, 2012
    Date of Patent: December 22, 2015
    Assignee: NIPPON SHINYAKU CO., LTD.
    Inventor: Hironori Otsu
  • Patent number: 9018393
    Abstract: A method for preparing 2-(N-substituted)-amino-benzimidazole derivatives is provided, which comprises the following steps: (1) reacting a compound of 2-(N-protecting group)-O-aryl diamine with a compound of N-phenoxycarbonyl monosubstituted amine to obtain a compound of 2-(N-protecting group)-amino aryl urea; (2) in a suitable organic solvent, performing dehydrating cyclization reaction of the compound of 2-(N-protecting group)-amino aryl urea in the presence of an organic base and dichloro triphenylphosphine prepared by triphenylphosphine oxide with oxalyl chloride or diphosgene or triphosgene, or dibromo triphenylphosphine prepared by triphenylphosphine oxide with bromine, to produce a compound of 1-protecting group-2-(N-substituted)-amino-benzimidazole; (3) deprotecting the resulting compound of 1-protecting group-2-(N-substituted)-amino-benzimidazole to obtain the compound 2-(N-substituted)-amino-benzimidazole.
    Type: Grant
    Filed: January 26, 2011
    Date of Patent: April 28, 2015
    Assignee: ABA Chemicals Corporation
    Inventors: Yueheng Jiang, Tong Cai, Limin Que, Zhigang Lin
  • Publication number: 20150086551
    Abstract: The present invention relates to a class of hydroxamic acid compounds of Formula (I), which act as alkylating agents and/or inhibitors of the HDAC pathway, having potential utility in the treatment of a neoplastic disease and immune diseases.
    Type: Application
    Filed: January 31, 2013
    Publication date: March 26, 2015
    Inventors: Yu Chen, Yi Chen
  • Publication number: 20150065495
    Abstract: The present invention provides compounds which are useful as inhibitors of lysine-specific demethylase 1 (“LSD1”). The present invention also relates to pharmaceutical compositions containing these compounds. The present invention also relates to a method for preparing these compounds. The present invention also relates to a method of treating a mammalian disorder in which LSD1 levels are elevated by administering these compounds and compositions to a patient in need thereof. The present invention also relates to a method for decreasing histone demethylase activity in a mammal comprising administering to the mammal an effective amount of these compounds and compositions.
    Type: Application
    Filed: August 28, 2014
    Publication date: March 5, 2015
    Applicant: UNIVERSITY OF UTAH
    Inventors: Hariprasad Vankayalapati, Sunil Sharma, Venkataswamy Sorna
  • Patent number: 8921405
    Abstract: The present invention relates to compounds of general formula I in which A, L, M, Q2, Q3, Q4, R1, R5, Ra, Rb, Rc, W, X, Y, Z1, Z2, Z3 are defined in the description, the salts thereof, particularly the physiologically acceptable salts thereof. The compounds are of potential utility in the treatment and/or prevention of inflammatory diseases and associated conditions, in particular, in the treatment and/or prevention of pain. The invention also relates to the use of such compounds as medicaments, to pharmaceutical compositions containing them, and to their preparation.
    Type: Grant
    Filed: July 15, 2013
    Date of Patent: December 30, 2014
    Assignee: Orexo AB
    Inventors: Roland Pfau, Kirsten Arndt, Henri Doods, Klaus Klinder, Raimund Kuelzer, Dimitrijs Lubriks, Juergen Mack, Benjamin Pelcman, Henning Priepke, Robert Roenn, Dirk Stenkamp, Edgars Suna
  • Patent number: 8895596
    Abstract: 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: Grant
    Filed: February 21, 2011
    Date of Patent: November 25, 2014
    Assignee: Merck Sharp & Dohme Corp
    Inventors: Jinlong Jiang, Andrew J. Kassick, Ahmet Kekec, Iyassu K. Sebhat
  • Patent number: 8865912
    Abstract: This invention relates to the use of benzimidazole derivatives for the modulation, notably the inhibition of the activity or function of the phosphoinositide 3? OH kinase family (hereinafter PI3 kinases), suitably, PI3K?, PI3K?, PI3K?, and/or PI3K?. Suitably, the present invention relates to the use of benzimidazoles in the treatment of one or more disease states selected from: autoimmune disorders, inflammatory diseases, cardiovascular diseases, neurodegenerative diseases, allergy, asthma, pancreatitis, multiorgan failure, kidney diseases, platelet aggregation, cancer, sperm motility, transplantation rejection, graft rejection and lung injuries. More suitably, the present invention relates to PI3K? selective benzimidazoles compounds for treating cancer.
    Type: Grant
    Filed: January 27, 2014
    Date of Patent: October 21, 2014
    Assignee: GlaxoSmithKline LLC
    Inventors: Junya Qu, Ralph A. Rivero, Robert Sanchez, Rosanna Tedesco
  • Publication number: 20140219960
    Abstract: The present invention relates a novel composition for preventing or treating hepatitis C virus, regulating the phosphorylation of a replicase. More specifically, it is possible to prevent or treat hepatitis C using a novel PRK2 inhibitor discovered through structure modeling, and to prevent or treat hepatitis C, particularly, interferon-insensitive hepatitis C through coadministration of an Hsp90 inhibitor.
    Type: Application
    Filed: April 23, 2012
    Publication date: August 7, 2014
    Applicant: Industry-Academic Cooperation Foundation, Yonsei University
    Inventor: Jong-Won Oh
  • Patent number: 8766001
    Abstract: The present invention relates to the improvement in organic electroluminescent devices by using compounds of the formula (1), in particular as hole-injection or hole-transport materials in a hole-injection or hole-transport layer.
    Type: Grant
    Filed: March 5, 2009
    Date of Patent: July 1, 2014
    Assignee: Merck Patent GmbH
    Inventors: Christof Pflumm, Arne Buesing, Amir Hossain Parham, Rocco Fortte, Holger Heil, Philipp Stoessel
  • Patent number: 8759537
    Abstract: This invention relates to compounds of formula I their use as inhibitors of the microsomal prostaglandin E2 synthase-1 (mPGES-1), pharmaceutical compositions containing them, and their use as medicaments for the treatment and/or prevention of inflammatory diseases and associated conditions. A, M, W, R1, R2, R6, R7, R8 have meanings given in the description.
    Type: Grant
    Filed: August 17, 2011
    Date of Patent: June 24, 2014
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Henning Priepke, Henri Doods, Raimund Kuelzer, Roland Pfau, Dirk Stenkamp, Benjamin Pelcman, Robert Roenn
  • Patent number: 8759520
    Abstract: Compounds of general formula (I): wherein R1, R2, R3, R4, R5, R6, X and Y are as defined herein are inhibitors of Bcl-2 and are useful for treating diseases characterized by abnormal cell growth and/or dysregulated apoptosis.
    Type: Grant
    Filed: December 8, 2009
    Date of Patent: June 24, 2014
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Stephen Peter East, Mark Whittaker, Osamu Ichihara, Adrian Kotei Kotey, Smantha Jayne Bamford
  • Publication number: 20140171363
    Abstract: The present invention provides compounds of formula (I); or pharmaceutically acceptable salts thereof, wherein the variables are defined as herein. The present invention provides a method for manufacturing the compounds of formula (I), their therapeutic uses, combinations with other of pharmacologically active agents, and a pharmaceutical compositions.
    Type: Application
    Filed: February 24, 2014
    Publication date: June 19, 2014
    Applicant: NOVARTIS AG
    Inventors: David Weninger BARNES, Gregory Raymond BEBERNITZ, Kevin CLAIRMONT, Scott Louis COHEN, Robert Edson DAMON, II, Robert Francis DAY, Stephanie Kay DODD, Christoph GAUL, Hatice Belgin GULGEZE EFTHYMIOU, Monish JAIN, Rajeshri Ganesh KARKI, Louise Clare KIRMAN, Kai LIN, Justin Yik Ching MAO, Tajesh Jayprakash PATEL, Brian Kenneth RAYMER, SU Liansheng
  • Publication number: 20140142117
    Abstract: The present invention relates to novel “reverse amide” compounds comprising a zinc chelator group, and the use of such compounds in the inhibition of HDAC6 and in the treatment of various diseases, disorders or conditions related to HDAC6.
    Type: Application
    Filed: November 11, 2013
    Publication date: May 22, 2014
    Inventors: John H. van Duzer, Ralph Mazitschek, Walter Ogier, James E. Bradner, Guoxiang Huang, Dejian Xie, Nan Yu
  • Patent number: 8722930
    Abstract: A compound of formula (I) wherein R1 to R15, P1, P2, A, B and Q are as defined in the claims and pharmaceutically acceptable salts and esters thereof, are disclosed. The compounds of formula (I) possess utility as matriptase inhibitors and are useful in the treatment of matriptase dependent conditions, particularly cancer.
    Type: Grant
    Filed: May 18, 2010
    Date of Patent: May 13, 2014
    Assignee: Orion Corporation
    Inventors: Rajeev Goswami, Anil Kumar Vuppala, Ramesh Veludandi, Ramesh Sistla, Chakshusmathi Ghadiyaram, Muralidhara Ramachandra
  • Publication number: 20140127273
    Abstract: Disclosure is provided for imidazole derivative compounds that prevent, remove and/or inhibit the formation of biofilms, compositions comprising these compounds, devices comprising these compounds, and methods of using the same.
    Type: Application
    Filed: January 8, 2014
    Publication date: May 8, 2014
    Applicant: North Carolina State University
    Inventors: Christian Melander, John Cavanagh, Robert W. Huigens, III, T. Eric Ballard, Justin J. Richards
  • Patent number: 8674113
    Abstract: This invention relates to compounds of formula I their use as inhibitors of the microsomal prostaglandin E2 synthase-1 (mPGES-1), pharmaceutical compositions containing them, and their use as medicaments for the treatment and/or prevention of inflammatory diseases and associated conditions. A, L, M, W, R1, R2, R3, R4, R6, R7, R9, Ra, Rb have meanings given in the description.
    Type: Grant
    Filed: December 8, 2011
    Date of Patent: March 18, 2014
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Henning Priepke, Henri Doods, Alexander Heim-Riether, Raimund Kuelzer, Roland Pfau, Klaus Rudolf, Dirk Stenkamp
  • Publication number: 20140066466
    Abstract: Described herein are compositions that inhibit the production of TNF? downstream of CD40 activation. As such, also described are various methods of using compositions exhibiting this activity for the treatment or prevention of inflammatory diseases associated with TNF? production or CD40 activation.
    Type: Application
    Filed: March 12, 2012
    Publication date: March 6, 2014
    Applicant: President and Fellows of Harvard College
    Inventor: Junying Yuan
  • Patent number: 8653259
    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: Grant
    Filed: February 6, 2008
    Date of Patent: February 18, 2014
    Assignee: Sanofi-Aventis Deutschland GmbH
    Inventors: Uwe Heinelt, Hans-Jochen Lang
  • Publication number: 20130345436
    Abstract: A method for preparing 2-(N-substituted)-amino-benzimidazole derivatives is provided, which comprises the following steps: (1) reacting a compound of 2-(N-protecting group)-O-aryl diamine with a compound of N-phenoxycarbonyl monosubstituted amine to obtain a compound of 2-(N-protecting group)-amino aryl urea; (2) in a suitable organic solvent, performing dehydrating cyclization reaction of the compound of 2-(N-protecting group)-amino aryl urea in the presence of an organic base and dichloro triphenylphosphine prepared by triphenylphosphine oxide with oxalyl chloride or diphosgene or triphosgene, or dibromo triphenylphosphine prepared by triphenylphosphine oxide with bromine, to produce a compound of 1-protecting group-2-(N-substituted)-amino-benzimidazole; (3) deprotecting the resulting compound of 1-protecting group-2-(N-substituted)-amino-benzimidazole to obtain the compound 2-(N-substituted)-amino-benzimidazole.
    Type: Application
    Filed: January 26, 2011
    Publication date: December 26, 2013
    Applicant: ABA CHEMICALS CORPORATION
    Inventors: Yueheng Jiang, Tong Cai, Limin Que, Zhigang Lin
  • Patent number: 8614213
    Abstract: There are described cyclohexyl amide derivatives useful as corticotropin releasing (CRF1) receptor antagonists.
    Type: Grant
    Filed: August 5, 2009
    Date of Patent: December 24, 2013
    Assignee: Novartis AG
    Inventors: David Beattie, Andrew James Culshaw, Lisa Rooney, Emily Stanley
  • Publication number: 20130324537
    Abstract: The present invention relates to guanidine compounds of the general formula I corresponding enantiomeric, diastereomeric and/or tautomeric forms thereof as well as pharmaceutically acceptable salts thereof. The present compound further relates to the use of guanidine compounds as binding partners for 5-HT5 receptors for the treatment of diseases which are modulated by a 5-HT5 receptor activity, in particular for the treatment of neurodegenerative and neuropsychiatric disorders as well as the associated signs, symptoms and dysfunctions.
    Type: Application
    Filed: November 21, 2012
    Publication date: December 5, 2013
    Applicants: Abbott Laboratories, Abbott GmbH & Co. KG
    Inventors: Abbott GmbH & Co. KG, Abbott Laboratories, Andrea Hager-Wernet
  • Publication number: 20130303571
    Abstract: The present invention relates to compounds of general formula I in which A, L, M, Q2, Q3, Q4, R1, R5, Ra, Rb, Rc, W, X, Y, Z1, Z2, Z3 are defined in the description, the salts thereof, particularly the physiologically acceptable salts thereof. The compounds are of potential utility in the treatment and/or prevention of inflammatory diseases and associated conditions, in particular, in the treatment and/or prevention of pain. The invention also relates to the use of such compounds as medicaments, to pharmaceutical compositions containing them, and to their preparation.
    Type: Application
    Filed: July 15, 2013
    Publication date: November 14, 2013
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: Roland PFAU, Kirsten ARNDT, Henri DOODS, Klaus KLINDER, Raimund KUELZER, Dimitrijs LUBRIKS, Juergen MACK, Benjamin PELCMAN, Henning PRIEPKE, Robert ROENN, Dirk STENKAMP, Edgars SUNA
  • Publication number: 20130245257
    Abstract: The invention provides a compound having a heterocyclic skeleton of formula (I): wherein the substituents are as defined in the specification, as well as a tautomer thereof or a salt thereof. The invention also provides asymmetric synthesis methods involving the use of such a compound, tautomer thereof, or salt thereof, as a catalyst.
    Type: Application
    Filed: March 14, 2013
    Publication date: September 19, 2013
    Applicants: Sumitomo Chemical Company, Limited, Kyoto University
    Inventors: Yoshiji TAKEMOTO, Kazuo MURAKAMI
  • Publication number: 20130217668
    Abstract: Compounds of Formula (I) are useful inhibitors of anaplastic lymphoma kinase. Compounds of Formula (I) have the following structure: where the definitions of the variables are provided herein.
    Type: Application
    Filed: July 28, 2011
    Publication date: August 22, 2013
    Applicant: AMGEN INC.
    Inventors: Christiane M. Boezio, Alan C. Cheng, Deborah Choquette, Richard T. Lewis, Michele H. Potashman, Karina Romero, John C. Stellwagen, Douglas A. Whittington
  • Publication number: 20130136782
    Abstract: Compounds described herein inhibit biofilm formation or disperse pre-formed biofilms of Gram-negative bacteria. Biofilm-inhibitory compounds can be encapsulated or contained in a polymer matrix for controlled release. Coatings, films, multilayer films, hydrogels, microspheres and nanospheres as well as pharmaceutical compositions and disinfecting compositions containing biofilm-inhibitory compounds are also provided. Methods for inhibiting formation of biofilms or dispersing already formed biofilms are provided. Methods for treating infections of gram-negative bacteria which form biofilms, particularly those of Pseudomonas and more particularly P. aeruginosa.
    Type: Application
    Filed: November 5, 2012
    Publication date: May 30, 2013
    Inventors: Helen BLACKWELL, Reto Frei, Anthony Breitbach, David M. Lynn, Adam H. Broderick
  • Patent number: 8426607
    Abstract: The present invention relates to substituted amino-benzimidazoles of general formula (1) wherein the groups R1 to R14 and A, are defined as in the specification and claims and the use thereof for the treatment of Alzheimer's disease (AD) and similar diseases.
    Type: Grant
    Filed: January 21, 2009
    Date of Patent: April 23, 2013
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Klaus Fuchs, Cornelia Dorner-Ciossek, Sandra Handschuh, Niklas Heine, Stefan Hoerer, Klaus Klinder
  • Publication number: 20130090342
    Abstract: The invention relates to new derivatives of formula (I), wherein the substituents are as defined in the specification; to processes for the preparation of such derivatives; pharmaceutical compositions comprising such derivatives; such derivatives as a medicament; such derivatives for the treatment of one or more IGF-1R mediated disorders or diseases.
    Type: Application
    Filed: June 16, 2011
    Publication date: April 11, 2013
    Applicant: NOVARTIS AG
    Inventors: Frederic Berst, Pascal Furet, Andreas Marzinzik
  • Publication number: 20130079376
    Abstract: Compounds are provided according to formula I: where R, R?, R3, R4, R5, and R6 are as defined herein. Provided compounds and pharmaceutical compositions thereof are useful for the prevention and treatment of a variety of conditions in mammals including humans, including by way of non-limiting example, Alzheimer' s Disease, Down's syndrome, Parkinson's Disease, and others.
    Type: Application
    Filed: July 6, 2012
    Publication date: March 28, 2013
    Inventors: Bijan Almassian, Martin J. Sadowski, Xu Kevin Lin
  • Publication number: 20130059852
    Abstract: Some embodiments of this invention include methods for treating disease and methods for administering a compound of Formula (I). In some aspects of the invention, diseases can be treated by administration of compositions comprising a compound of Formula (I). Pharmaceutical compositions of some embodiments of the present invention comprise a compound of Formula (I).
    Type: Application
    Filed: April 8, 2011
    Publication date: March 7, 2013
    Applicant: UNIVERSITY OF LOUISVILLE RESEARCH FOUNDATION, INC.
    Inventors: John O. Trent, Jason B. Meier, Kelby B. Napier
  • Publication number: 20120309738
    Abstract: This invention relates to compounds of formula I their use as inhibitors of the microsomal prostaglandin E2 synthase-1 (mPGES-1), to pharmaceutical compositions containing them, and their use as medicaments for the treatment and/or prevention of inflammatory diseases and associated conditions. A, M, W, R1, R2, R3, R4, R6, R2, R7, R8, R9, Ra, Rb have meanings given in the description.
    Type: Application
    Filed: December 8, 2011
    Publication date: December 6, 2012
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: Henning Priepke, Raimund Kuelzer, Juergen Mack, Roland Pfau, Dirk Stenkamp, Benjamin Pelcman, Robert Roenn, Dimitrijs Lubriks, Edgars Suna
  • Patent number: 8293774
    Abstract: The present invention relates to an optically active (R)-aryloxypropionic acid amide compound which has high selectivity and safety for protecting a crop such as rice, wheat, barley and soy bean, and exhibits excellent herbicidal activity against weeds, and a herbicidal composition comprising the same.
    Type: Grant
    Filed: July 2, 2008
    Date of Patent: October 23, 2012
    Assignee: Kyung Nong Corporation
    Inventors: Joo-kyung Kim, Dong-hoo Kim, Hyung-ho Kim, Kyung-hyun Kim, Cheol-su Yoon, In-cheon Hwang
  • Publication number: 20120214786
    Abstract: This invention relates to compounds of formula I their use as inhibitors of the microsomal prostaglandin E2 synthase-1 (mPGES-1), pharmaceutical compositions containing them, and their use as medicaments for the treatment and/or prevention of inflammatory diseases and associated conditions. A, M, W, R1, R2, R6, R7, R8 have meanings given in the description.
    Type: Application
    Filed: August 17, 2011
    Publication date: August 23, 2012
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: Henning PRIEPKE, Henri DOODS, Raimund KUELZER, Roland PFAU, Dirk STENKAMP, Benjamin PELCMAN, Robert ROENN
  • Patent number: 8236965
    Abstract: A subject of the present application is new benzimidazole derivatives of formula in which A, Y, R1, R2, R3 and R4 represent different variable groups. These products have an antagonist activity of GnRH (Gonadotropin-Releasing Hormone). The invention also relates to pharmaceutical compositions containing said products and their use for the preparation of a medicament.
    Type: Grant
    Filed: December 23, 2008
    Date of Patent: August 7, 2012
    Assignee: IPSEN Pharma S.A.S.
    Inventors: Lydie Poitout, Valérie Brault, Eric Ferrandis, Christophe Thurieau
  • Publication number: 20120196897
    Abstract: The present invention relates to compounds of general formula I in which A, L, M, Q2, Q3, Q4, R1, R5, Ra, Rb, Rc, W, X, Y, Z1, Z2, Z3 are defined in the description, the salts thereof, particularly the physiologically acceptable salts thereof. The compounds are of potential utility in the treatment and/or prevention of inflammatory diseases and associated conditions, in particular, in the treatment and/or prevention of pain. The invention also relates to the use of such compounds as medicaments, to pharmaceutical compositions containing them, and to their preparation.
    Type: Application
    Filed: April 6, 2012
    Publication date: August 2, 2012
    Applicant: Boehringer Ingelheim International GmbH
    Inventors: Roland PFAU, Kirsten ARNDT, Henri DOODS, Klaus KLINDER, Raimund KUELZER, Dimitrijs LUBRIKS, Juergen MACK, Benjamin PELCMAN, Henning PRIEPKE, Robert ROENN, Dirk STENKAMP, Edgars SUNA
  • Publication number: 20120171129
    Abstract: Disclosure is provided for benzimidazole derivative compounds that prevent, remove and/or inhibit the formation of biofilms, compositions including these compounds, devices including these compounds, and methods of using the same.
    Type: Application
    Filed: June 10, 2010
    Publication date: July 5, 2012
    Inventors: Christian Melander, Steven A. Rogers, Robert W. Huigens, III
  • Publication number: 20120149676
    Abstract: This invention relates to compounds of formula I their use as inhibitors of the microsomal prostaglandin E2 synthase-1 (mPGES-1), pharmaceutical compositions containing them, and their use as medicaments for the treatment and/or prevention of inflammatory diseases and associated conditions. A, L, M, W, R1, R2, R3, R4, R6, R7, R9, Ra, Rb have meanings given in the description.
    Type: Application
    Filed: December 8, 2011
    Publication date: June 14, 2012
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: Henning PRIEPKE, Henri DOODS, Alexander HEIM-RIETHER, Raimund KUELZER, Roland PFAU, Klaus RUDOLF, Dirk STENKAMP
  • Publication number: 20120142922
    Abstract: Disclosed are benzamide derivatives useful in slowing the expansion of cancer cells.
    Type: Application
    Filed: June 11, 2010
    Publication date: June 7, 2012
    Applicant: TRANSLATIONAL GENOMICS RESEARCH INSTITUTE
    Inventors: Tong Wang, Stephen Gately
  • Publication number: 20120136002
    Abstract: A compound of formula (I) wherein R1 to R15, P1, P2, A, B and Q are as defined in the claims and pharmaceutically acceptable salts and esters thereof, are disclosed. The compounds of formula (I) possess utility as matriptase inhibitors and are useful in the treatment of matriptase dependent conditions, particularly cancer.
    Type: Application
    Filed: May 18, 2010
    Publication date: May 31, 2012
    Inventors: Rajeev Goswami, Anil Kumar Vuppala, Ramesh Veludandi, Ramesh Sistla, Chakshusmathi Ghadiyaram, Muralidhara Ramachandra
  • Patent number: 8178694
    Abstract: Heterocyclylaminoalkyl Substituted Benzimidazoles Inhibitors of RSV replication of formula (I): The salts and stereochemically isomeric forms thereof, wherein Q is hydrogen, C1-6alkyl optionally substituted with a heterocycle or Q is C1-6alkyl substituted with both —OR4 and a heterocycle; wherein said heterocycle is oxazolidine, thiazolidine, 1-oxo-thiazolidine, 1,1-dioxothiazolidine, morpholinyl, thiomorpholinyl, 1-oxo-thiomorpholinyl, 1,1-dioxothiomorpholinyl, hexahydrooxazepine, hexahydrothiazepine, 1-oxo-hexahydrothiazepine, 1,1-dioxo-hexahydrothiazepine, pyrrolidine, piperidine, homopiperidine, piperazine; which heterocyle may be substituted with 1-2 substituents; each Alk is C1-6alkanediyl; R1 is Ar or optionally substituted piperidinyl, piperazinyl, morpholinyl, thiomorpholinyl, pyridyl, pyrazinyl, pyridazinyl, pyrimidinyl, furanyl, tetrahydrofuranyl, thienyl, pyrrolyl, thiazolyl, oxazolyl, imidazolyl, isothiazolyl, pyrazolyl, isoxazo lyl, oxadiazolyl, quinolinyl, quinoxalinyl, benzofuranyl, benzothien
    Type: Grant
    Filed: June 20, 2006
    Date of Patent: May 15, 2012
    Assignee: Tibotec Pharmaceuticals Ltd.
    Inventors: Jean-François Bonfanti, Philippe Muller, Jérôme Michel Claude Fortin, Frédéric Marc Maurice Doublet
  • Patent number: 8163935
    Abstract: 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: Grant
    Filed: April 26, 2006
    Date of Patent: April 24, 2012
    Assignee: Takeda Pharmaceutical Company Limited
    Inventors: Kazuyoshi Aso, Michiyo Mochizuki, Albert Charles Gyorkos, Christopher Peter Corrette, Suk Young Cho, Scott Alan Pratt, Christopher Stephen Siedem
  • Publication number: 20120095227
    Abstract: The present invention provides a compound having a heterocyclic skeleton, which is represented by of the formula (I): wherein R1 and R2 are the same or different and each is a lower alkyl group optionally having substituent(s), an aralkyl group optionally having substituent(s) or an aryl group optionally having substituent(s), or R1 and R2 in combination form, together with the nitrogen atom they are bonded to, a heterocycle optionally having substituent(s) (the heterocycle is optionally condensed with an aromatic hydrocarbon ring); ring A is an imidazole ring condensed with an aromatic ring optionally having substituent(s), or a pyrimidin-4-one ring condensed with an aromatic ring optionally having substituent(s); R3 and R4 are the same or different and each is a lower alkyl group optionally having substituent(s), a lower alkenyl group optionally having substituent(s), a lower alkynyl group optionally having substituent(s), an aralkyl group optionally having substituent(s) or an aryl group optionally h
    Type: Application
    Filed: April 9, 2010
    Publication date: April 19, 2012
    Applicants: SUMITOMO CHEMICAL COMPANY, LIMITED, KYOTO UNIVERSITY
    Inventors: Yoshiji Takemoto, Kazuo Murakami
  • Patent number: 8097758
    Abstract: The invention relates to the compounds of formula (I) having antithrombotic activity which especially inhibit blood clotting factor IXa, to methods for producing the same and to the use thereof as drugs.
    Type: Grant
    Filed: March 9, 2009
    Date of Patent: January 17, 2012
    Assignee: Sanofi-Aventis
    Inventors: Henning Steinhagen, Markus Follmann, Jochen Goerlitzer, Herman Schreuder
  • Publication number: 20110312969
    Abstract: Compounds of general formula (I): wherein R1, R2, R3, R4, R5, R6, X and Y are as defined herein are inhibitors of Bcl-2 and are useful for treating diseases characterised by abnormal cell growth and/or dysregulated apoptosis.
    Type: Application
    Filed: December 8, 2009
    Publication date: December 22, 2011
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: Stephen Peter East, Mark Whittaker, Osamu Ichihara, Adrian Kotei Kotei, Smantha Jayne Bamford
  • Publication number: 20110312935
    Abstract: There are provided compounds of formula (I), wherein R1, R6, R8, Q2, Q3, Q3a, Q4, L and A have meanings given in the description, and pharmaceutically-acceptable salts thereof, which compounds are useful in the treatment of diseases in which inhibition of the activity of a member of the MAPEG family is desired and/or required, and particularly in the treatment of inflammation and/or cancer.
    Type: Application
    Filed: September 25, 2009
    Publication date: December 22, 2011
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: Roland Pfau, Kirsten Arndt, Henri Doods, Norbert Hauel, Klaus Klinder, Raimund Kuelzer, Juergen Mack, Henning Priepke, Dirk Stenkamp
  • Patent number: 8067614
    Abstract: This invention is directed to the compound of formula (I), compositions containing said compounds to inhibit the sodium-proton exchanger of subtype 3 (NHE3) which are useful in the prevention or treatment of various disorders in a patient suffering from a disease state, such as, renal disorders including acute or chronic renal failure, disorders of biliary function and for respiratory disorders such as snoring or sleep apnea or for stroke.
    Type: Grant
    Filed: March 12, 2010
    Date of Patent: November 29, 2011
    Assignee: Sanofi-Aventis Deutschland GmbH
    Inventors: Uwe Heinelt, Hans-Jochen Lang, Armin Hofmeister, Klaus Wirth, Martin Hug
  • Publication number: 20110288139
    Abstract: The present invention relates to substituted amino-benzimidazoles of general formula (1) wherein the groups R1 to R14 and A, are defined as in the specification and claims and the use thereof for the treatment of Alzheimer's disease (AD) and similar diseases.
    Type: Application
    Filed: January 21, 2009
    Publication date: November 24, 2011
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: Klaus Fuchs, Cornelia Dorner-Ciossek, Sandra Handschuh, Niklas Heine, Stefan Hoerer, Klaus Klinder
  • Patent number: 8039500
    Abstract: There is provided a compound of the formula: wherein R1 is an optionally substituted hydrocarbyl, a substituted amino, etc.; R2 is an aromatic group substituted with one or two substituents at the positions adjacent to the position bonded to Z, and said aromatic group may have additional substituent(s); X is —NR3— wherein R3 is a hydrogen, an optionally substituted hydrocarbyl or an acyl, or sulfur; Y1, Y2 and Y3 are an optionally substituted methine or a nitrogen, etc.; and Z is an optionally substituted methylene, provided that carbonyl is excluded; or a salt thereof or a prodrug thereof, which have CRF receptor antagonist activity and use thereof.
    Type: Grant
    Filed: December 28, 2007
    Date of Patent: October 18, 2011
    Assignee: Takeda Pharmaceutical Company Limited
    Inventors: Kazuyoshi Aso, Michiyo Mochizuki, Katsumi Kobayashi
  • Publication number: 20110237589
    Abstract: The present invention relates to guanidine compounds of the general formula I corresponding enantiomeric, diastereomeric and/or tautomeric forms thereof as well as pharmaceutically acceptable salts thereof. The present compound further relates to the use of guanidine compounds as binding partners for 5-HT5 receptors for the treatment of diseases which are modulated by a 5-HT5 receptor activity, in particular for the treatment of neurodegenerative and neuropsychiatric disorders as well as the associated signs, symptoms and dysfunctions.
    Type: Application
    Filed: February 4, 2011
    Publication date: September 29, 2011
    Inventors: Astrid Netz, Wilhelm Amberg, Udo Lange, Michael Ochse, Charles W. Hutchins, Francisco-Xavier Garcia-Ladona, Wolfgang Wernet, Andreas Kling, Andrea Hager-Wernet