1,3-oxazoles (including Hydrogenated) Patents (Class 514/374)
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Patent number: 8946231Abstract: 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: GrantFiled: March 15, 2010Date of Patent: February 3, 2015Assignee: Merck Sharp & Dohme Corp.Inventors: Christopher S. Burgey, Craig M. Potteiger
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Patent number: 8946267Abstract: A therapeutic agent or a prophylactic agent for neuropathic pain provides a synergistically-enhanced analgesic effect at a dose at which a calcium channel ?2? ligand does not produce any side effects as well as which agent does not produce any new side effects on the central nervous system. The therapeutic agent or a prophylactic agent for neuropathic pain includes as effective ingredients a cyclohexane derivative, represented by the following formula, or a pharmaceutically acceptable salt thereof or a prodrug thereof, and a calcium channel ?2? ligand.Type: GrantFiled: July 29, 2011Date of Patent: February 3, 2015Assignee: Toray Industries, Inc.Inventors: Naoki Izumimoto, Hidenori Mochizuki
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Patent number: 8946426Abstract: The present invention is concerned with substituted bicyclic heterocyclic compounds of Formula (I) wherein Het1, Het2, A1, A2, A3 and A4 have the meaning defined in the claims. The compounds according to the present invention are useful as gamma secretase modulators. The invention further relates to processes for preparing such novel compounds, pharmaceutical compositions comprising said compounds as an active ingredient as well as the use of said compounds as a medicament.Type: GrantFiled: February 2, 2010Date of Patent: February 3, 2015Assignees: Janssen Pharmaceuticals, Inc., Cellzome LimitedInventors: Henricus Jacobus Maria Gijsen, Adriana Ingrid Velter, Gregor James MacDonald, François Paul Bischoff, Tongfei Wu, Sven Franciscus Anna Van Brandt, Michel Surkyn, Mirko Zaja, Serge Maria Aloysius Pieters, Didier Jean-Claude Berthelot, Michel Anna Jozef De Cleyn, Daniel Oehlrich
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Publication number: 20150031694Abstract: 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: ApplicationFiled: March 21, 2013Publication date: January 29, 2015Inventors: Edmond J. LaVoie, Ajit Parhi, Yongzheng Zhang, Daniel S. Pilch, Malvika Kaul
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Publication number: 20150031686Abstract: 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: ApplicationFiled: March 6, 2013Publication date: January 29, 2015Inventors: Zhaojin Zhong, Zhuorong Li, Dajun Zhang, Yuhuan Li, Zhen Wang, Rongmei Gao, Jiajia Shen
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Publication number: 20150018332Abstract: 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: ApplicationFiled: July 26, 2012Publication date: January 15, 2015Applicant: KARYOPHARM THERAPEUTICS INC.Inventors: Vincent P. Sandanayaka, Sharon Shacham, Michael Kauffman, Sharon Shechter, Dilara McCauley, Yosef Landesman, William Senapedis, Jean-Richard Saint-Martin
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Publication number: 20150011548Abstract: A compound of formula (I), wherein R3, R4, G, B, M, and Z are as defined in the claims, and pharmaceutically acceptable salts thereof are disclosed. The compounds of formula (I) possess utility as FGFR inhibitors and are useful in the treatment of a condition, where FGFR kinase inhibition is desired, such as cancer.Type: ApplicationFiled: October 9, 2012Publication date: January 8, 2015Inventors: Tero Linnanen, Gerd Wohlfahrt, Srinivas Nanduri, Ravi Ujjinamatada, Srinivasan Rajagopalan, Subhendu Mukherjee
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Publication number: 20150005320Abstract: 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: ApplicationFiled: September 27, 2013Publication date: January 1, 2015Applicant: 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
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Publication number: 20150005319Abstract: The invention relates generally to macrocyclic compounds of formula I and their therapeutic use. More particularly, the invention relates to macrocyclic compounds that modulate the activity of IL-17 and/or are useful in the treatment of medical conditions, such as inflammatory diseases and other IL-17-associated disorders.Type: ApplicationFiled: February 1, 2013Publication date: January 1, 2015Inventors: Michael Taylor, Nicholas K. Terrett, William H. Connors, Cheri Snedeker, Kelley C. Shortsleeves, Benjamin A. Seigal, Stephen P. Hale, Timothy F. Briggs, Frank G. Favaloro, Jr., Tyler J. Cipriani, Dingxue Yan, Sethu L. Alexander, Atli Thorarensen, Li Xing
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Publication number: 20150005283Abstract: The present invention provides 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: ApplicationFiled: February 21, 2013Publication date: January 1, 2015Applicant: Hoffmann-La Roche Inc.Inventors: Adrian Wai-Hing Cheung, Ryan Craig Schoenfeld, Weiya Yun, Shu-Hai Zhao
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Publication number: 20140378474Abstract: The invention relates to a compound of the formula (I) in which the substituents are as defined in the specification; in free form or in salt form; to its preparation, to its use as medicament and to medicaments comprising it.Type: ApplicationFiled: January 25, 2013Publication date: December 25, 2014Applicant: NOVARTIS AGInventors: Stefanie Flohr, Christian Markert, Kenji Namoto, Bernard Pirard
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Publication number: 20140378445Abstract: Disclosed are methods for treating Vascular Leak Syndrome. Further disclosed are methods for treating vascular leakage due to inflammatory diseases, inter alia, sepsis, lupus, inflammatory bowel disease. Yet further disclosed are methods for treating renal cell carcinoma and melanoma. Still further disclosed are methods for reducing metastasis of malignant cells and/or preventing the proliferation of carcinoma cells via spreading due to vascular leakage.Type: ApplicationFiled: December 21, 2012Publication date: December 25, 2014Inventors: Robert Shalwitz, Kevin G. Peters
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Publication number: 20140370011Abstract: The present invention provides indane acetic acid and their derivatives and methods for the treating and/or preventing of cognitive disorders.Type: ApplicationFiled: September 4, 2014Publication date: December 18, 2014Applicant: DARA BIOSCIENCES, INC.Inventor: Mary Katherine Delmedico
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Publication number: 20140371274Abstract: 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: ApplicationFiled: June 13, 2014Publication date: December 18, 2014Inventors: Andrea Rosario BECCARI, Gianluca BIANCHINI, Chiara LIBERATI, Michela FANI', Mara ZIPPOLI
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Publication number: 20140356322Abstract: 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: ApplicationFiled: January 11, 2013Publication date: December 4, 2014Inventors: 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
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Publication number: 20140357650Abstract: 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: ApplicationFiled: January 17, 2013Publication date: December 4, 2014Applicant: Fox Chase Cancer CenterInventors: Koen Jansen, Ingrid De Meester, Leen Heirbaut, Jonathan D. Cheng, Jurgen Joossens, Koen Augustyns, Pieter Van Der Veken
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Patent number: 8901159Abstract: The present invention provides a method for treating inflammation in a patient in need thereof comprising administering to said patient an effective amount of a compound according to formula wherein R is H or lower alkyl, R1 is hydrocarbyl or substituted hydrocarbyl and the broken line represents a saturated or unsaturated bond, i.e a double bond. Preferably, R1 is an alkyl. More preferably, R1 is a n-alkyl or a cycloalkyl-n-alkyl, e.g. a cyclohexyl-n-alkyl, e.g. n-octyl, n-nonyl or cyclohexyl-n-butyl radical and prodrugs, isomers and pharmaceutically acceptable salts thereof.Type: GrantFiled: June 28, 2011Date of Patent: December 2, 2014Assignee: Allergan, Inc.Inventors: Jenny W. Wang, David F. Woodward, Ming Ni, Jose L. Martos, William R. Carling
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Patent number: 8901156Abstract: 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: GrantFiled: January 13, 2011Date of Patent: December 2, 2014Assignee: Tempero Pharmaceuticals, Inc.Inventors: Erkan Baloglu, Shomir Ghosh, Mercedes Lobera, Darby Schmidt
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Patent number: 8901313Abstract: The invention relates to novel compounds of Formula I: wherein A, Y, R1, R2 and the subscript b each has the meaning as described herein and compounds of Formula I, and stereoisomers, geometric isomers, tautomers, solvates, metabolites, isotopes, pharmaceutically acceptable salts, or prodrugs thereof. Compounds of Formula I and pharmaceutical compositions thereof are useful in the treatment of disease and disorders in which undesired or over-activation of NF-kB signaling is observed.Type: GrantFiled: March 15, 2012Date of Patent: December 2, 2014Assignee: Genentech, Inc.Inventors: Steven Staben, Jianwen Feng, Pui Leng Loke, Christian A. G. N. Montalbetti
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Patent number: 8895535Abstract: Compounds of the formula I in which R1, R2, R3 and R4 have the meanings indicated in Claim 1, are inhibitors of methionine aminopeptidase and can be employed for the treatment of tumors.Type: GrantFiled: September 14, 2011Date of Patent: November 25, 2014Assignee: Merck Patent GmbHInventors: Timo Heinrich, Frank Zenke, Michel Calderini, Djordje Musil
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Publication number: 20140343109Abstract: Provision of an agent for promoting proliferation of meibomian gland epithelial cells or corneal epithelial cells, and a therapeutic agent for ocular diseases such as meibomian gland dysfunction, dry eye and the like. A preparation containing [3-[2-[4-isopropyl-2-(4-trifluoromethyl)phenyl-5-thiazolyl]ethyl]-5-methyl-1,2-benzisoxazol-6-yl]oxyacetic acid, [4-[3-[2-(4-trifluoromethyl)phenyl-4-isopropyl-5-thiazolyl]propionyl]-2-methylphenoxy]acetic acid or [4-[3-[2-(2-hydroxy-4-chlorophenyl)-5-isopropyl-4-oxazolyl]propionyl]-2-methylphenoxy]acetic acid, or a pharmacologically acceptable salt thereof as an active ingredient is used as an agent for promoting proliferation of meibomian gland epithelial cells or corneal epithelial cells, as well as a therapeutic agent for ocular diseases such as meibomian gland dysfunction, dry eye and the like.Type: ApplicationFiled: June 27, 2014Publication date: November 20, 2014Inventors: Yoshikuni NAKAMURA, Ikuko HANANO, Jun INOUE
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Publication number: 20140343017Abstract: 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: ApplicationFiled: January 24, 2013Publication date: November 20, 2014Applicant: Kabushiki Kaisha Yakult HonshaInventors: Takashi Ikeda, Masahiro Ono, Satoshi Ueno, Ryuta Yamazaki, Takashi Yaegashi, Takeshi Matsuzaki
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Patent number: 8889723Abstract: 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: GrantFiled: March 13, 2014Date of Patent: November 18, 2014Assignee: EMC microcollections GmbHInventors: Holger Eickhoff, Hubert Lowenheim
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Publication number: 20140336194Abstract: The present invention provides the use of a neutral endopeptidase inhibitor, in the manufacture of a medicament for the treatment, amelioration and/or prevention of contrast-induced nephropathy. The invention also relates to the use of a compound of Formula I: wherein R1, R2, R3, R5, X, A3, B1, s and n are defined herein, for the treatment, amelioration and/or prevention of contrast-induced nephropathy. The present invention further provides a combination of pharmacologically active agents for use in the treatment, amelioration and/or prevention of contrast-induced nephropathy.Type: ApplicationFiled: July 28, 2014Publication date: November 13, 2014Applicant: NOVARTIS AGInventor: Shi Yin FOO
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Patent number: 8883797Abstract: The instant invention describes compounds having metalloenzyme modulating activity, and methods of treating diseases, disorders or symptoms thereof mediated by such metalloenzymes.Type: GrantFiled: June 20, 2012Date of Patent: November 11, 2014Assignee: Viamet Pharmaceuticals, Inc.Inventors: William J. Hoekstra, Robert J. Schotzinger
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Publication number: 20140329796Abstract: 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: ApplicationFiled: July 16, 2014Publication date: November 6, 2014Applicant: Ajinomoto Co., Inc.Inventors: Tamotsu SUZUKI, Kaori Kobayashi, Sayaka Asari, Seiji Shiraishi, Tatsuya Okuzumi
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Patent number: 8877741Abstract: 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: GrantFiled: January 22, 2014Date of Patent: November 4, 2014Assignee: Boehringer Ingelheim International GmbHInventors: Martin Fleck, Niklas Heine, Bernd Nosse, Gerald Juergen Roth
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Patent number: 8877754Abstract: 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: GrantFiled: August 17, 2011Date of Patent: November 4, 2014Assignee: Boehringer Ingelheim International GmbHInventors: Gerald Juergen Roth, Martin Fleck, Heike Neubauer, Bernd Nosse
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Publication number: 20140323458Abstract: The present disclosure provides substituted aliphanes, cyclophanes, heteraphanes, heterophanes, hetero-heteraphanes and metallocenes, of Formula I D-M-D??(Formula I) useful as antiviral agents. In certain embodiments disclosed herein M is a group —P-A-P— where A is Certain substituted aliphanes, cyclophanes, heteraphanes, heterophanes, hetero-heteraphanes and metallocenes disclosed herein are potent and/or selective inhibitors of viral replication, particularly Hepatitis C virus replication. Pharmaceutical compositions/and combinations containing one or more substituted aliphanes, cyclophanes, heteraphanes, heterophanes, hetero-heteraphanes and metallocenes and a pharmaceutically acceptable carrier are also provided by this disclosure. Methods for treating viral infections, including Hepatitis C viral infections are provided by the disclosure.Type: ApplicationFiled: July 10, 2014Publication date: October 30, 2014Inventors: Jason Allan Wiles, Qiuping Wang, Akihiro Hashimoto, Godwin Pais, Xiangzhu Wang, Venkat Gadhachanda, Avinash Phadke, Milind Deshpande, Dawei Chen
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Publication number: 20140323501Abstract: Immune-modulators of formula (I) below are prepared: A pharmaceutical composition contains the immune-modulators. The pharmaceutical composition is used as a drug, especially as an immune-modulating drug. The compound can be used in treatment of immune disorders and for immune suppression. Thus, for example, the compound can be used in treating hypo-immunity, rejection after organ transplantation and auto-immune disease.Type: ApplicationFiled: July 5, 2012Publication date: October 30, 2014Applicant: INSTITUTE OF MATERIA MEDICA, CHINESE ACADEMY OF MEDICAL SCIENCESInventors: Weijuan Han, Haijing Zhang, Xiaojian Wang, Jing Jin, Gang Li, Yi Zhang, Qiong Xiao, Wanqi Zhou, Xiaoguang Chen, Dali Yin
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Publication number: 20140315946Abstract: 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: ApplicationFiled: July 2, 2014Publication date: October 23, 2014Inventor: Arun K. Ghosh
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Publication number: 20140315721Abstract: This document discloses molecules having the following formulas (“Formula One” & “Formula Two” and “Formula Three”) The Ar1, Het, Ar2, R1, R2, R3, R4, and R5 are further described herein.Type: ApplicationFiled: June 25, 2014Publication date: October 23, 2014Applicant: DOW AGROSCIENCES LLCInventors: Gary D. Crouse, Thomas C. Sparks, William H. Dent, III, CaSandra L. McLeod, Lawrence C. Creemer, David A. Demeter, Amanda E. Fritz, Lindsey G. Fischer, Erich W. Baum
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Publication number: 20140315961Abstract: 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: ApplicationFiled: March 14, 2014Publication date: October 23, 2014Applicant: Epizyme, Inc.Inventors: Richard Chesworth, Lorna Helen Mitchell, Gideon Shapiro
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Publication number: 20140315965Abstract: 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: ApplicationFiled: December 20, 2012Publication date: October 23, 2014Inventors: James L. Gleason, John H. White, Dainis Kaldre, Joshua Fischer
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Patent number: 8865754Abstract: Compounds and their pharmaceutically acceptable salts for treatment of synucleinopathies, such as Parkinson's disease and tauopathies.Type: GrantFiled: March 1, 2012Date of Patent: October 21, 2014Assignee: Proteotech Inc.Inventors: Luke A. Esposito, Marisa C. Yadon, Joel Cummings, F. Michael Hudson, Thomas Lake, Franz F. Hefti, Geoffrey Golding, Seok-Rye Choi, Ximin Li, Alan D. Snow, Qubai Hu, Judy Cam
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Publication number: 20140308243Abstract: The present invention discloses compounds of Formula (I), and pharmaceutically acceptable salts, esters, or prodrugs thereof: Q-G-A-L-B—Z—W??(I), which inhibit RNA-containing virus, particularly the hepatitis C virus (HCV). Consequently, the compounds of the present invention interfere with the life cycle of the hepatitis C virus and are also useful as antiviral agents. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from HCV infection. The invention also relates to methods of treating an HCV infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention.Type: ApplicationFiled: April 16, 2014Publication date: October 16, 2014Applicant: ENANTA PHARMACEUTICALS, INC.Inventors: Yao-Ling Qiu, Hui Cao, Xiaowen Peng, Zhigang Chen, Yat Sun Or
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Patent number: 8859768Abstract: This invention provides compounds of formula IA or IB: wherein HY, R1, R2, and G1, are as described in the specification. The compounds are inhibitors of VPS34 and/or PI3K and are thus useful for treating proliferative, inflammatory, or cardiovascular disorders.Type: GrantFiled: August 10, 2011Date of Patent: October 14, 2014Assignee: Millennium Pharmaceuticals, Inc.Inventors: Courtney A. Cullis, Krista E. Granger, Jianping Guo, Masaaki Hirose, Gang Li, Miho Mizutani, Tricia J. Vos
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Publication number: 20140302010Abstract: 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: ApplicationFiled: March 28, 2012Publication date: October 9, 2014Applicant: BAYER INTELLECTUAL PROPERTY GMBHInventors: Ulrich Klar, Marcus Koppitz, Duy Nguyen, Dirk Kosemund, Roland Neuhaus, Gerhard Siemeister
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Publication number: 20140302069Abstract: 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: ApplicationFiled: November 7, 2012Publication date: October 9, 2014Inventors: David Fairlie, Robert C. Reid
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Publication number: 20140303175Abstract: The present invention relates to 2-(substituted sulphur, sulphone or sulphoxide)-3-(substituted phenyl)propionic acid derivatives, 2-(substituted oxygen)-3-(substituted phenyl)propionic acid derivatives, benzoic acid derivatives, and derivatives of 2-methyl-2-(phenoxy or phenylthio)propanoic acid and 2-(methyl or ethyl)-2-(phenoxy or phenylthio)butanoic acid, to processes for preparing such compounds, to their use in the treatment of inflammatory conditions, and to pharmaceutical compositions containing them.Type: ApplicationFiled: June 11, 2014Publication date: October 9, 2014Inventors: Anders Broo, Johan Gottfries, Michael Kossenjans, Li Lanna, Eva-Lotte Lindstedt-Alstermark, Kristina A. Nilsson, Bengt Ohlsson, Maria Thorstensson, Maria Boije
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Publication number: 20140296239Abstract: 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: ApplicationFiled: March 27, 2014Publication date: October 2, 2014Applicant: SANOFIInventors: Sven Ruf, Thorsten Sadowski, Klaus Wirth, Herman Schreuder, Christian Buning, Christopher Kallus, Hartmut Strobel, Hermut Wehlan
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Publication number: 20140296296Abstract: 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: ApplicationFiled: March 27, 2014Publication date: October 2, 2014Inventors: Sven Ruf, Thorsten Sadowski, Klaus Wirth, Herman Schreuder, Christian Buning, Christopher Kallus, Hartmut Strobel, Hermut Wehlan
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Patent number: 8846733Abstract: 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: GrantFiled: December 6, 2011Date of Patent: September 30, 2014Assignee: Actelion Pharmaceuticals Ltd.Inventors: Daniel Bur, Olivier Corminboeuf, Sylvaine Cren, Corinna Grisostomi, Xavier Leroy, Sylvia Richard-Bildstein
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Publication number: 20140288065Abstract: The present invention provides a pyrrolidine compound of General Formula (1) or a salt thereof, wherein R101 and R102 are each independently a phenyl group or a pyridyl group, the phenyl group or the pyridyl group may have one or more substituents selected from halogen atoms and lower alkyl groups optionally substituted with one or more halogen atoms, etc. The pyrrolidine compound or a salt thereof of the present invention is usable to produce a pharmaceutical preparation having a wider therapeutic spectrum and being capable of exhibiting sufficient therapeutic effects after short-term administration.Type: ApplicationFiled: June 10, 2014Publication date: September 25, 2014Applicant: OTSUKA PHARMACEUTICAL CO., LTD.Inventors: Muneaki KURIMURA, Shinichi TAIRA, Takahiro TOMOYASU, Nobuaki ITO, Kuninori TAI, Noriaki TAKEMURA, Takayuki MATSUZAKI, Yasuhiro MENJO, Shin MIYAMURA, Yohji SAKURAI, Akihito WATANABE, Yasuyo SAKATA, Takumi MASUMOTO, Kohei AKAZAWA, Haruhiko SUGINO, Naoki AMADA, Satoshi OHASHI, Tomoichi SHINOHARA, Hirofumi SASAKI, Chisako MORITA, Junko YAMASHITA, Satoko NAKAJIMA
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Publication number: 20140288135Abstract: 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: ApplicationFiled: March 13, 2014Publication date: September 25, 2014Applicant: EMC microcollections GmbHInventors: Holger Eickhoff, Hubert Lowenheim
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Publication number: 20140287011Abstract: Disclosed is an arthropod pest control composition comprising 2-(2,6-difluorophenyl)-4-[4-(1,1-dimethylethyl)-2-ethoxyphenyl]-4,5-dihydrooxazole and an inert carrier, wherein the volume median diameter of 2-(2,6-difluorophenyl)-4-[4-(1,1-dimethylethyl)-2-ethoxyphenyl]-4,5-dihydrooxazole is from 1.5 to 5.Type: ApplicationFiled: November 2, 2012Publication date: September 25, 2014Inventors: Katsuya Natsuhara, Yusuke Kimura, Mamoru Takiuchi
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Publication number: 20140274952Abstract: The present invention relates to novel heterocyclic alkanol derivatives, to processes for these compounds, to compositions comprising these compounds and to their use as biologically active compounds, in particular for controlling harmful microorganisms in crop protection and in the protection of materials and as plant growth regulators.Type: ApplicationFiled: November 23, 2012Publication date: September 18, 2014Applicant: BAYER INTELLCTUAL PROPERTY GMBHInventors: Sebastian Hoffmann, Hendrik Helmke, Gorka Peris, Friedrich Carl Nising, Tomoki Tsuchiya, Alexander Sudau, Jürgen Benting, David Bernier
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Publication number: 20140275191Abstract: The present invention relates to novel oxazolidinone compounds of general formula (I) having antibiotic activity also against multiresistant bacterial strains.Type: ApplicationFiled: March 15, 2013Publication date: September 18, 2014Inventors: I.E.ME.S.T-ISTITUTO EURO MEDITERRANEO DI SCIENZA E TECNOLOGIA, UNIVERSITA DEGLI STUDI DI MILANO-BICOCCA
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Publication number: 20140256740Abstract: 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: ApplicationFiled: July 27, 2012Publication date: September 11, 2014Applicant: Tempero Pharmaceuticals, Inc.Inventors: Erkan Baloglu, Shomir Ghosh, Mercedes Lobera, Darby R. Schmidt
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Patent number: 8828908Abstract: Bicyclic dione compounds of formula (I), and derivatives thereof, which are suitable for use as herbicides.Type: GrantFiled: May 27, 2008Date of Patent: September 9, 2014Assignee: Syngenta LimitedInventors: Christopher John Mathews, Matthew Brian Hotson, Alan John Dowling, James Nicholas Scutt, Mangala Govenkar, Lee Challinor