Cyano Or -c(=x)-, Wherein X Is Chalcogen, Attached Directly Or Indirectly To The Oxazole Ring By Nonionic Bonding Patents (Class 548/236)
  • Patent number: 9757360
    Abstract: The invention relates to the use of pharmaceutical compositions containing as the active agent a compound of formula I in the treatment of dermal wounds. The compositions may be used for the promotion of healing of wounds affecting the deeper layers under the epithelium, including dermal- and sub dermal connective tissue, being cut, punctured, sliced wounds or originating in insufficient tissue perfusion, chronic diseases or other harms. The compositions are formulated for local application and may comprise other active agents contributing to wound healing in addition to a compound of formula (I).
    Type: Grant
    Filed: December 12, 2014
    Date of Patent: September 12, 2017
    Assignee: SZEGEDI TUDOMÁNYEGYETEM
    Inventors: Gábor Eros, Döníz Degovics, Petra Hartmann, Lajos Kemény
  • Publication number: 20150148301
    Abstract: The present invention relates to inhibitors of the activity of Complex (III) of the mitochondrial electron transport chain and use thereof in treatment and/or prevention of cancers presenting tumour-initiating cells. The present invention further relates to pharmaceutical compositions containing said inhibitors alone or in combination with other pharmaceutically active agents, and their use as medicaments or as agrochemicals where their properties as inhibitors of the mitochondrial respiration is of benefit.
    Type: Application
    Filed: May 23, 2013
    Publication date: May 28, 2015
    Inventors: Virginie Clement-Schatlo, Thomas Fessard, Damien Barbaras, Joana Matos, Erick Carreira
  • Publication number: 20150141474
    Abstract: The invention relates to compounds of formula (I): useful for treating disorders mediated by acyl coA-diacylglycerol acyl transferase 1 (DGAT1), e.g. metabolic disorders. The invention also provides methods of treating such disorders, and compounds and compositions etc. for their treatment.
    Type: Application
    Filed: April 26, 2013
    Publication date: May 21, 2015
    Applicant: NOVARTIS AG
    Inventors: Sejal Patel, Justin Mao, Qian Liu, Tyler Harrison, Rohit Duvadie, Xin Chen, Frederic Zecri
  • Publication number: 20150133451
    Abstract: The present invention provides a heterocyclic compound having an IRAK-4 inhibitory action, which is useful for the prophylaxis or treatment of inflammatory disease, autoimmune disease, osteoarticular degenerative disease, neoplastic disease and the like, and a medicament containing thereof. The present invention relates to a compound represented by the formula (I): wherein each symbol is as defined in the specification, or a salt thereof.
    Type: Application
    Filed: November 5, 2014
    Publication date: May 14, 2015
    Applicant: Takeda Pharmaceutical Company Limited
    Inventors: Masato Yoshida, Kazuaki TAKAMI, Yusuke TOMINARI, Zenyu SHIOKAWA, Akito SHIBUYA, Yusuke SASAKI, Tony GIBSON, Terufumi TAKAGI
  • Patent number: 9012445
    Abstract: In one aspect, the invention relates to substituted 4-(1H-pyrazol-4-yl)benzyl analogs compounds, derivatives thereof, and related compounds, which are useful as positive allosteric modulators of the muscarinic acetylcholine receptor M1 (mAChR M1); synthesis methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating neurological and psychiatric disorders associated with muscarinic acetylcholine receptor dysfunction using the compounds and compositions. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.
    Type: Grant
    Filed: January 12, 2013
    Date of Patent: April 21, 2015
    Assignee: Vanderbilt University
    Inventors: Craig W. Lindsley, P. Jeffrey Conn, Michael R. Wood, Bruce J. Melancon, Michael S. Poslusney, James C. Tarr
  • Publication number: 20150105253
    Abstract: Salts of N-(tetrazol-5-yl)- and N-(triazol-5-yl)arylcarboxamides of the general formula (I) are described as herbicides. In this formula (I), W, X, Z and R represent radicals such as hydrogen, organic radicals such as alkyl, and other radicals such as halogen. A and B each represent nitrogen or carbon. M+ represents a cation.
    Type: Application
    Filed: April 30, 2013
    Publication date: April 16, 2015
    Applicant: Bayer Cropscience AG
    Inventors: Ralf Braun, Simon Doerner-Rieping, Hartmut Ahrens, Christian Waldraff, Arnim Koehn, Hansjoerg Dietrich, Elmar Gatzweiler, Christopher Hugh Rosinger
  • Publication number: 20150099696
    Abstract: The present invention relates to compounds of the general formula (I), their tautomeric forms, their stereoisomers, their pharmaceutically acceptable salts, pharmaceutical compositions containing them, methods for their preparation, use of these compounds in medicine and the intermediates involved in their preparation. The present invention is directed to compounds suitable for the treatment of Disease conditions such as hyperlipidemia.
    Type: Application
    Filed: June 26, 2012
    Publication date: April 9, 2015
    Applicant: Cadila Healthcare Limited
    Inventors: Harikishore Pingali, Pankaj Makadia, Vrajesh Pandya, Sairam V.V.M. Kalapatapu
  • Publication number: 20150099719
    Abstract: This invention relates to a novel class of compounds which are cysteine protease inhibitors, including but not limited to, inhibitors of cathepsins K, L, S and B. These compounds are useful for treating diseases in which inhibition of bone resorption is indicated, such as osteoporosis.
    Type: Application
    Filed: October 6, 2014
    Publication date: April 9, 2015
    Inventors: Shawn Stachel, Daniel V. Paone, Jing Li, Kausik Nanda
  • Patent number: 8993777
    Abstract: The present invention is a method for producing a phenyl-substituted heterocyclic derivative represented by general formula (1), which has a step wherein a heteroaromatic compound represented by general formula (2) is reacted with a phenol derivative represented by general formula (3) in the presence of a nickel compound, 1,2-bis(dicyclohexylphosphino)ethane, and a base.
    Type: Grant
    Filed: October 10, 2012
    Date of Patent: March 31, 2015
    Assignee: National University Corporation Nagoya University
    Inventors: Kenichiro Itami, Junichiro Yamaguchi, Kei Muto
  • Patent number: 8993619
    Abstract: The invention relates to compounds of formula (I): useful for treating disorders mediated by acyl coA-diacylglycerol acyl transferase 1 (DGAT1), e.g. metabolic disorders. The invention also provides methods of treating such disorders, and compounds and compositions etc. for their treatment.
    Type: Grant
    Filed: April 26, 2013
    Date of Patent: March 31, 2015
    Assignee: Novartis AG
    Inventors: Sejal Patel, Justin Mao, Qian Liu, Rui Zheng, Tyler Harrison, Rohit Duvadie, Xin Chen, Frederic Zecri, Jay Larrow, Xuchun Zheng, Yizong Zhou, Jiong Ye, Yiping Ding, Yu Gai
  • Publication number: 20150080576
    Abstract: Compounds, pharmaceutical compositions including the compounds, and methods of preparation and use thereof are disclosed. The compounds are amide compounds which can be prepared from certain heteroaryl carboxylic acids and certain diazabicycloalkanes. The compounds exhibit selectivity for, and bind with high affinity to, neuronal nicotinic receptors of the ?4?2 subtype in the central nervous system (CNS). The compounds and compositions can be used to treat and/or prevent a wide variety of conditions or disorders, particularly CNS disorders. The compounds can: (i) alter the number of nicotinic cholinergic receptors of the brain of the patient, (ii) exhibit neuroprotective effects, and (iii) when employed in effective amounts, not result in appreciable adverse side effects (e.g. side effects such as significant increases in blood pressure and heart rate, significant negative effects upon the gastrointestinal tract, and significant effects upon skeletal muscle).
    Type: Application
    Filed: November 24, 2014
    Publication date: March 19, 2015
    Inventors: Anatoly Mazurov, Lan Miao, Yunde Xiao, Philip S. Hammond, Craig H. Miller, Srinivasa Rao Akireddy, Srinivasa V. Murthy, Regina C. Whitaker, Scott R. Breining, Matt S. Melvin
  • Publication number: 20150065504
    Abstract: Disclosed herein are new antiviral compounds, together with pharmaceutical compositions that include one or more antiviral compounds, and methods of synthesizing the same. Also disclosed herein are methods of ameliorating and/or treating a paramyxovirus viral infection with one or more small molecule compounds. Examples of paramyxovirus infection include an infection caused by human respiratory syncytial virus (RSV).
    Type: Application
    Filed: August 19, 2014
    Publication date: March 5, 2015
    Inventors: Guangyi Wang, Leonid Beigelman, Anh Truong, Carmela Napolitano, Daniele Andreotti, Haiying He, Karin Ann Stein
  • Publication number: 20150057282
    Abstract: The invention provides a compound which is an amide of the formula (1), or a salt, solvate, N-oxide or tautomer thereof; wherein: a is 0 or 1; b is 0 or 1: provided that the sum of a and b is 0 or 1; T is O or NH Ar1 is a monocyclic or bicyclic 5- to 10-membered aryl or heteroaryl group containing up to 4 heteroatoms selected from O, N and S, and being optionally substituted by one or more substituents R1; Ar2 Js a monocyclic or bicyclic 5- to 10-membered aryl or heteroaryl group containing up to 4 heteroatoms selected from O, N and S and being optionally substituted by one or more substituents R2; and R1 and R2 are as defined in the claims. The compounds are inhibitors of kinases and in particular FLT3, FLT4 and Aurora kinases.
    Type: Application
    Filed: October 31, 2014
    Publication date: February 26, 2015
    Applicant: SAREUM LIMITED
    Inventors: John Charles READER, John Mark ELLARD, Helen BOFFEY, Susanne TAYLOR, Andrew David CARR, Michael CHERRY, Michelle WILSON, Richard Boakye OWOARE
  • Publication number: 20150038534
    Abstract: Disclosed are compounds having the formula: wherein X1, X2, X3, R1, R2, R3, R4, Y, A, Z, L and n are as defined herein, and methods of making and using the same.
    Type: Application
    Filed: October 22, 2014
    Publication date: February 5, 2015
    Inventors: Erkan BALOGLU, Shomir Ghosh, Mercedes Lobera, Darby R. Schmidt
  • Patent number: 8946231
    Abstract: The subject invention relates to novel P2X3 receptor antagonists that play a critical role in treating disease states associated with pain, in particular peripheral pain, inflammatory pain, or tissue injury pain that can be treated using a P2X3 receptor subunit modulator.
    Type: Grant
    Filed: March 15, 2010
    Date of Patent: February 3, 2015
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Christopher S. Burgey, Craig M. Potteiger
  • Publication number: 20150031686
    Abstract: Disclosed are phenyl-oxazolyl derivatives having a general formula (I), a preparation method thereof, and an application of the phenyl-oxazolyl derivatives as an inosine monophosphate dehydrogenase (IMPDH) inhibitor.
    Type: Application
    Filed: March 6, 2013
    Publication date: January 29, 2015
    Inventors: Zhaojin Zhong, Zhuorong Li, Dajun Zhang, Yuhuan Li, Zhen Wang, Rongmei Gao, Jiajia Shen
  • Publication number: 20150031694
    Abstract: The invention provides compounds of formula (I): wherein R1-R7 and W have any of the values defined in the specification, and salts thereof. The compounds have good solubility and are useful for treating bacterial infections.
    Type: Application
    Filed: March 21, 2013
    Publication date: January 29, 2015
    Inventors: Edmond J. LaVoie, Ajit Parhi, Yongzheng Zhang, Daniel S. Pilch, Malvika Kaul
  • Publication number: 20150025249
    Abstract: The invention relates to a process for the preparation of a compound of formula (I) or a salt thereof.
    Type: Application
    Filed: October 8, 2014
    Publication date: January 22, 2015
    Applicant: Hoffmann-La Roche Inc.
    Inventors: Kurt Puentener, Michelangelo Scalone
  • Publication number: 20150018332
    Abstract: The invention generally relates to nuclear transport modulators, e.g CRM1 inhibitors, and more particularly to a compound represented by formula (I): or a pharmaceutically acceptable salt thereof, wherein the variables are as defined and described herein. The invention also includes the synthesis and use of a compound of structural formula (I), or a pharmaceutically acceptable salt or composition thereof, e.g, in the treatment, modulation and/or prevention of physiological conditions associated with CRM1 activity.
    Type: Application
    Filed: July 26, 2012
    Publication date: January 15, 2015
    Applicant: KARYOPHARM THERAPEUTICS INC.
    Inventors: Vincent P. Sandanayaka, Sharon Shacham, Michael Kauffman, Sharon Shechter, Dilara McCauley, Yosef Landesman, William Senapedis, Jean-Richard Saint-Martin
  • Publication number: 20150011754
    Abstract: The present disclosure relates to compounds, compositions and methods for the treatment of hepatitis C virus (HCV) infection. Also disclosed are pharmaceutical compositions containing such compounds and methods for using these compounds in the treatment of HCV infection.
    Type: Application
    Filed: September 17, 2014
    Publication date: January 8, 2015
    Inventors: Carol Bachand, Makonen Belema, Daniel H. Deon, Andrew C. Good, Jason Goodrich, Clint A. James, Rico Lavoie, Omar D. Lopez, Alain Martel, Nicholas A. Meanwell, Van N. Nguyen, Jeffrey Lee Romine, Edward H. Ruediger, Lawrence B. Snyder, Denis R. St. Laurent, Fukang Yang, David R. Langley, Lawrence G. Hamann
  • Publication number: 20150005320
    Abstract: The invention relates to compounds of formula (I): or a pharmaceutically acceptable salt, solvate, clathrate, or prodrug thereof wherein X, Y, A, Z, L and n are defined herein. These compounds are useful as immunosuppressive agents and for treating and preventing inflammatory conditions and immune disorders.
    Type: Application
    Filed: September 27, 2013
    Publication date: January 1, 2015
    Applicant: Synta Pharmaceuticals Corp.
    Inventors: Yu Xie, Mats Holmqvist, Jerome Mahiou, Mitsunori Ono, Lijun Sun, Shoujun Chen, Shijie Zhang, Jun Jiang, Dinesh Chimmanamada, Chih-Yi Yu
  • Patent number: 8916715
    Abstract: A process for the preparation of 4-methyl-oxazole-5-carboxamide, an intermediate in the synthesis of pyridoxine, by reacting lower alkyl 4-methyl-oxazole-5-carboxy-late with a molar excess of anhydrous, liquid ammonia.
    Type: Grant
    Filed: May 31, 2012
    Date of Patent: December 23, 2014
    Assignee: DSM IP Assets B.V.
    Inventors: Werner Bonrath, Jocelyn Fischesser, Hongyan Shen
  • Publication number: 20140371274
    Abstract: The present invention relates to novel compounds, their use in the prevention or treatment of symptoms and disorders associated with the bradykinin B1 pathway and pharmaceutical compositions containing them.
    Type: Application
    Filed: June 13, 2014
    Publication date: December 18, 2014
    Inventors: Andrea Rosario BECCARI, Gianluca BIANCHINI, Chiara LIBERATI, Michela FANI', Mara ZIPPOLI
  • Publication number: 20140357650
    Abstract: The present invention relates to novel inhibitors having high selectivity and specificity for FAP (fibroblast activation protein). Said inhibitors are useful as a human and/or veterinary medicine, in particular for the treatment and/or prevention of FAP-related disorders such as but not limited to proliferative disorders.
    Type: Application
    Filed: January 17, 2013
    Publication date: December 4, 2014
    Applicant: Fox Chase Cancer Center
    Inventors: Koen Jansen, Ingrid De Meester, Leen Heirbaut, Jonathan D. Cheng, Jurgen Joossens, Koen Augustyns, Pieter Van Der Veken
  • Publication number: 20140356322
    Abstract: The present invention relates to bifunctional compounds, which find utility as modulators of targeted ubiquitination, especially inhibitors of a variety of polypeptides and other proteins that are degraded and/or otherwise inhibited by bifunctional compounds of the present invention. In particular, the present invention is directed to compounds, which contain on one end a VHL ligand that binds to the ubiquitin ligase and on the other end a moiety that binds a target protein, such that the target protein is placed in proximity to the ubiquitin ligase to effect degradation (and inhibition) of that protein. The present invention exhibits a broad range of pharmacological activities associated with compounds of the present invention, consistent with the degradation/inhibition of targeted polypeptides.
    Type: Application
    Filed: January 11, 2013
    Publication date: December 4, 2014
    Inventors: Craig M. Crews, Dennis Buckley, Alessio Ciulli, William Jorgensen, Peter C. Gareiss, Inge Van Molle, Jeffrey Gustafson, Hyun-Seop Tae, Julien Michel, Dentin Wade Hoyer, Anke G. Roth, John David Harling, Ian Edward David Smith, Afjal Hussain Miah, Sebastien Andre Campos, Joelle Le
  • Publication number: 20140343017
    Abstract: Provided is a highly safe and effective compound represented by the following general formula (1) or a salt thereof which acts on tubulin and has an anticancer effect, wherein Ar represents an aryl group or a heteroaryl group; Z1, Z2, Z3, and Z4 each independently represent CH, a nitrogen atom, an oxygen atom, or a sulfur atom; R1 represents a hydrogen atom, a halogen atom, an alkyl group, or the like; R2 and R3 are the same or different and each represent a hydrogen atom, a halogen atom, a carboxyl group, or the like; n units of R4 are the same or different and each represent a hydrogen atom, an alkyl group, or the like; and n represents a number of 0 to 4.
    Type: Application
    Filed: January 24, 2013
    Publication date: November 20, 2014
    Applicant: Kabushiki Kaisha Yakult Honsha
    Inventors: Takashi Ikeda, Masahiro Ono, Satoshi Ueno, Ryuta Yamazaki, Takashi Yaegashi, Takeshi Matsuzaki
  • Patent number: 8889723
    Abstract: A method of treating inner ear hardness of hearing and restoring hearing of humans and animals after damage and loss of sensory hair cells in an organ of Corti based on regeneration biology includes administering a therapeutically effective amount of a compound including aminoalkyloxazole and aminoalkylthiazole carboxylic acid amides, or a pharmaceutically acceptable salt, a stereoisomer, a stereoisomer mixture, a tautomer or a prodrug compound thereof, directly or indirectly to damaged tissue structures in a cochlea, optionally, by transtympanal injection into a middle ear, by application to a round or oval window of an inner ear or by injection into the inner ear.
    Type: Grant
    Filed: March 13, 2014
    Date of Patent: November 18, 2014
    Assignee: EMC microcollections GmbH
    Inventors: Holger Eickhoff, Hubert Lowenheim
  • Patent number: 8884029
    Abstract: A photoelectric conversion device capable of improving conversion efficiency is provided. The photoelectric conversion device includes a work electrode, an opposed electrode, and an electrolyte-containing layer. In the work electrode, a metal oxide semiconductor layer supporting a dye is provided. The dye contains a cyanine compound that has a methine chain, an indolenine skeleton bonded with both ends of the methine chain, and anchor groups introduced to a nitrogen atom included in the indolenine skeleton. Electron injection efficiency to the metal oxide semiconductor layer is improved, and the dye is hardly exfoliated from the metal oxide semiconductor layer.
    Type: Grant
    Filed: September 9, 2009
    Date of Patent: November 11, 2014
    Assignee: Adeka Corporation
    Inventors: Junji Tanabe, Atsushi Monden, Masahiro Shinkai, Mitsuhiro Okada, Toru Yano, Yohei Aoyama, Yusuke Kubota
  • Publication number: 20140329796
    Abstract: The present invention aims to provide a novel compound having a TRPA1 antagonist activity, and a medicament containing the compound. Moreover, the present invention aims to provide a TRPA1 antagonist and a medicament useful for the prophylaxis or treatment of diseases involving TRPA1. A medicament containing a compound represented by the formula (I): wherein each symbol is as defined in the DESCRIPTION, or a pharmaceutically acceptable salt thereof, and the like.
    Type: Application
    Filed: July 16, 2014
    Publication date: November 6, 2014
    Applicant: Ajinomoto Co., Inc.
    Inventors: Tamotsu SUZUKI, Kaori Kobayashi, Sayaka Asari, Seiji Shiraishi, Tatsuya Okuzumi
  • Patent number: 8877741
    Abstract: The invention relates to new pyrrolidine derivatives of the formula to their use as medicaments, to methods for their therapeutic use and to pharmaceutical compositions containing them.
    Type: Grant
    Filed: January 22, 2014
    Date of Patent: November 4, 2014
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Martin Fleck, Niklas Heine, Bernd Nosse, Gerald Juergen Roth
  • Patent number: 8877754
    Abstract: The invention relates to new compounds of the formula I to their use as medicaments, to methods for their therapeutic use and to pharmaceutical compositions containing them.
    Type: Grant
    Filed: August 17, 2011
    Date of Patent: November 4, 2014
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Gerald Juergen Roth, Martin Fleck, Heike Neubauer, Bernd Nosse
  • Publication number: 20140315961
    Abstract: Described herein are compounds of Formula (I), pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof. Compounds of the present invention are useful for inhibiting arginine methyltransferase activity. Methods of using the compounds for treating arginine methyltransferase-mediated disorders are also described.
    Type: Application
    Filed: March 14, 2014
    Publication date: October 23, 2014
    Applicant: Epizyme, Inc.
    Inventors: Richard Chesworth, Lorna Helen Mitchell, Gideon Shapiro
  • Publication number: 20140315946
    Abstract: Novel compounds and compositions for treating patients in need of relief from HIV, AIDS and AIDS-related diseases are described. Methods for treating HIV, AIDS, and AIDS-related diseases using the compounds described herein are also described.
    Type: Application
    Filed: July 2, 2014
    Publication date: October 23, 2014
    Inventor: Arun K. Ghosh
  • Publication number: 20140315965
    Abstract: The present disclosure relates to novel compounds having vitamin D receptor agonist and histone deacetylase inhibitory efficacy as well as methods for reducing or inhibiting the proliferation of cancer cells or for treating cancer.
    Type: Application
    Filed: December 20, 2012
    Publication date: October 23, 2014
    Inventors: James L. Gleason, John H. White, Dainis Kaldre, Joshua Fischer
  • Publication number: 20140302069
    Abstract: Heterocyclic compounds that modulate C3a receptors and their use in the treatment or prevention of inflammatory diseases, infectious diseases, cancers, metabolic disorders, obesity, type 2 diabetes, metabolic syndrome and associated cardiovascular diseases are described. The use of the compounds in stimulating or suppressing an immune response is also described together with pharmaceutical compositions comprising the compounds or their pharmaceutically acceptable salts.
    Type: Application
    Filed: November 7, 2012
    Publication date: October 9, 2014
    Inventors: David Fairlie, Robert C. Reid
  • Publication number: 20140302010
    Abstract: The present invention relates to substituted benzimidazole compounds of general formula (I) in which R3, R5 and A are as defined in the claims, to methods of preparing said compounds, to pharmaceutical compositions and combinations comprising said compounds and to the use of said compounds for manufacturing a pharmaceutical composition for the treatment or prophylaxis of a disease, in particular of a hyper-proliferative and/or angiogenesis disorder, as a sole agent or in combination with other active ingredients.
    Type: Application
    Filed: March 28, 2012
    Publication date: October 9, 2014
    Applicant: BAYER INTELLECTUAL PROPERTY GMBH
    Inventors: Ulrich Klar, Marcus Koppitz, Duy Nguyen, Dirk Kosemund, Roland Neuhaus, Gerhard Siemeister
  • Publication number: 20140296296
    Abstract: The present invention relates to compounds of the formula I, wherein X, R, R1, R2, D, E1, E2, E3, E4, G1, G2, G3 and G4 have the meanings indicated in the claims, which are valuable pharmaceutical active compounds. They are inhibitors of the protease cathepsin A, and are useful for the treatment of diseases such as atherosclerosis, heart failure, renal diseases, liver diseases or inflammatory diseases, for example. The invention furthermore relates to processes for the preparation of the compounds of the formula I, their use and pharmaceutical compositions comprising them.
    Type: Application
    Filed: March 27, 2014
    Publication date: October 2, 2014
    Inventors: Sven Ruf, Thorsten Sadowski, Klaus Wirth, Herman Schreuder, Christian Buning, Christopher Kallus, Hartmut Strobel, Hermut Wehlan
  • Publication number: 20140296239
    Abstract: The present invention relates to compounds of the formula I, wherein X, R, R1, R2, D, E1, E2, E3, E4, G1, G2, G3 and G4 have the meanings indicated in the claims, which are valuable pharmaceutical active compounds. They are inhibitors of the protease cathepsin A, and are useful for the treatment of diseases such as atherosclerosis, heart failure, renal diseases, liver diseases or inflammatory diseases, for example. The invention furthermore relates to processes for the preparation of the compounds of the formula I, their use and pharmaceutical compositions comprising them.
    Type: Application
    Filed: March 27, 2014
    Publication date: October 2, 2014
    Applicant: SANOFI
    Inventors: Sven Ruf, Thorsten Sadowski, Klaus Wirth, Herman Schreuder, Christian Buning, Christopher Kallus, Hartmut Strobel, Hermut Wehlan
  • Patent number: 8846733
    Abstract: The invention relates to oxazolyl-methylether derivatives of formula (I), wherein R1, R2, R3, R4 and R5 are as defined in the description, their preparation and their use as pharmaceutically active compounds.
    Type: Grant
    Filed: December 6, 2011
    Date of Patent: September 30, 2014
    Assignee: Actelion Pharmaceuticals Ltd.
    Inventors: Daniel Bur, Olivier Corminboeuf, Sylvaine Cren, Corinna Grisostomi, Xavier Leroy, Sylvia Richard-Bildstein
  • Publication number: 20140275549
    Abstract: The present invention is a method for producing a phenyl-substituted heterocyclic derivative represented by general formula (1), which has a step wherein a heteroaromatic compound represented by general formula (2) is reacted with a phenol derivative represented by general formula (3) in the presence of a nickel compound, 1,2-bis(dicyclohexylphosphino)ethane, and a base.
    Type: Application
    Filed: October 10, 2012
    Publication date: September 18, 2014
    Applicant: National University Corporation Nagoya University
    Inventors: Kenichiro Itami, Junichiro Yamaguchi, Kei Muto
  • Publication number: 20140256740
    Abstract: The present invention relates to novel retinoid-related orphan receptor gamma (ROR?) modulators and their use in the treatment of diseases mediated by ROR?.
    Type: Application
    Filed: July 27, 2012
    Publication date: September 11, 2014
    Applicant: Tempero Pharmaceuticals, Inc.
    Inventors: Erkan Baloglu, Shomir Ghosh, Mercedes Lobera, Darby R. Schmidt
  • Patent number: 8822444
    Abstract: This disclosure concerns novel compounds of Formula (I) as defined in the specification and compositions comprising such novel compounds. These compounds are useful antiviral agents, especially in inhibiting the function of the NS5A protein encoded by Hepatitis C virus (HCV). Thus, the disclosure also concerns a method of treating HCV related diseases or conditions by use of these novel compounds or a composition comprising such novel compounds.
    Type: Grant
    Filed: July 13, 2012
    Date of Patent: September 2, 2014
    Assignee: Bristol-Myers Squibb Company
    Inventors: Omar D. Lopez, Qi Chen, Makonen Belema, Lawrence G. Hamann
  • Patent number: 8822514
    Abstract: The present invention relates to compounds of Formulas I and II, wherein B1, B2, B3, B4, C1, C2, ring D, L1, L2 and R1-4 are defined herein, synthetic intermediates, and pharmaceutical compositions, comprising such compounds. The compounds and compositions are capable of modulating various protein kinase receptors such as Tie-2 and Aurora and, therefore, influencing kinase related disease states and conditions. The compounds, for example, are capable of treating cancer caused by unregulated angiogenesis, and inflammation as well as other proliferative disorders.
    Type: Grant
    Filed: June 6, 2012
    Date of Patent: September 2, 2014
    Assignee: Amgen Inc.
    Inventors: Brian L. Hodous, Stephanie D. Geuns-Meyer, Philip R. Olivieri, Vinod F. Patel, Paul A. Tempest
  • Patent number: 8822519
    Abstract: The present invention provides a novel compound of formula I, which has an agitation effect on the peroxisome proliferator-activated receptor subtype ? (PPAR?), to a pharmaceutical composition comprising the compound, to a process for preparation of the compound and to use of the compound in the manufacture of a medicament for treating or preventing a disease which could be treated or prevented by activating PPAR? thereof, said disease is one or more from the group comprising metabolic syndrome, obesity, dyslipidemia, pathoglycemia, insulin resistance, senile dementia and tumors. The present invention also relates to a new intermediate used in the preparation of the novel compound and a process for preparation of the intermediate.
    Type: Grant
    Filed: August 7, 2009
    Date of Patent: September 2, 2014
    Assignee: Zhejiang Hisun Pharmaceutical Co., Ltd.
    Inventors: Chunhua Jin, Xiaoyu Liu, Zhenliang Chen, Xiaohe Zheng, Shoufeng Ming
  • Patent number: 8815924
    Abstract: Novel heterocyclic compounds of the formula (I), in which R1, D, W, T and T? have the meanings indicated in Claim 1, are SGK inhibitors and can be used for the treatment of SGK-induced diseases and conditions, such as diabetes, obesity, metabolic syndrome (dyslipidaemia), systemic and pulmonary hypertonia, cardiovascular diseases and kidney diseases, generally in fibroses and inflammatory processes of any type.
    Type: Grant
    Filed: April 4, 2005
    Date of Patent: August 26, 2014
    Assignee: Merck Patent GmbH
    Inventors: Dieter Dorsch, Rolf Gericke, Werner Mederski, Norbert Beier, Florian Lang
  • Publication number: 20140213588
    Abstract: The present invention provides compounds of Formula (I): as defined in the specification and compositions comprising any of such novel compounds. These compounds are endothelial lipase inhibitors which may be used as medicaments. The disclosure also provides a novel method of treating diseases or conditions related to the activity of endothelial lipase by use of compounds according to Formula (II): as defined in the specification and compositions comprising any of the compounds.
    Type: Application
    Filed: September 26, 2012
    Publication date: July 31, 2014
    Applicant: Bristol-Myers Squibb Company
    Inventors: Lynn Abell, Leonard Adam, Cullen L. Cavallaro, Heather Finlay, Todd J. Friends, Jon J. Hangeland, Ji Jiang, R. Michael Lawrence, Jennifer X. Qiao, Carol Hui Hu, Tammy C. Wang
  • Publication number: 20140206880
    Abstract: A process for the preparation of 4-methyl-oxazole-5-carboxamide, an intermediate in the synthesis of pyridoxine, by reacting lower alkyl 4-methyl-oxazole-5-carboxy-late with a molar excess of anhydrous, liquid ammonia.
    Type: Application
    Filed: May 31, 2012
    Publication date: July 24, 2014
    Applicant: DSM IP ASSETS B.V.
    Inventors: Werner Bonrath, Jocelyn Fischesser, Hongyan Shen
  • Publication number: 20140206676
    Abstract: In one aspect, the invention relates to substituted 4-(1H-pyrazol-4-yl)benzyl analogs compounds, derivatives thereof, and related compounds, which are useful as positive allosteric modulators of the muscarinic acetylcholine receptor M1 (mAChR M1); synthesis methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating neurological and psychiatric disorders associated with muscarinic acetylcholine receptor dysfunction using the compounds and compositions. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.
    Type: Application
    Filed: January 12, 2013
    Publication date: July 24, 2014
    Applicant: Vanderbilt University
    Inventors: Craig W. Lindsley, P. Jeffrey Conn, Michael R. Wood, Bruce J. Melancon, Michael S. Poslusney, James C. Tarr
  • Publication number: 20140206706
    Abstract: The present invention provides a method for treating a thrombotic or an inflammatory disorder administering to a patient in need thereof a therapeutically effective amount of at least one compound of Formula (I) or Formula (V): or a stereoisomer or pharmaceutically acceptable salt or solvate form thereof, wherein the variables A, L, Z, R3, R4, R6, R11, X1, X2, and X3 are as defined herein. The compounds of Formula (I) are useful as selective inhibitors of serine protease enzymes of the coagulation cascade and/or contact activation system; for example thrombin, factor Xa, factor XIa, factor IXa, factor VIIa and/or plasma kallikrein. In particular, it relates to compounds that are selective factor XIa inhibitors. This invention also provides compounds within the scope of Formula I and relates to pharmaceutical compositions comprising these compounds.
    Type: Application
    Filed: March 19, 2014
    Publication date: July 24, 2014
    Inventors: Jon J. Hangeland, Mimi L. Quan, Joanne M. Smallheer, Gregory S. Bisacchi, James R. Corte, Todd J. Friends, Zhong Sun, Karen A. Rossi, Cullen L. Cavallaro
  • Publication number: 20140194443
    Abstract: The invention relates to pyrazolyl-based carboxamide compounds useful as ICRAC inhibitors, to pharmaceutical compositions containing these compounds and to these compounds for the use in the treatment and/or prophylaxis of diseases and/or disorders, in particular inflammatory diseases and/or inflammatory disorders.
    Type: Application
    Filed: January 10, 2014
    Publication date: July 10, 2014
    Applicant: Grünenthal GmbH
    Inventors: Sonja Nordhoff, Sebastian Wachten, Achim Kless, Felix Voss, Stefanie Ritter