1,3,4-oxadiazoles (including Hydrogenated) Patents (Class 548/143)
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Patent number: 9672990Abstract: An oxadiazole dye for use as an organic photosensitizer. The oxadiazole dye comprising donor-?-spacer-acceptor type molecules in which at least one of an oxadiazole group acts as a ?-conjugated bridge (spacer), a naphthyl unit acts as an electron-donating unit, a carboxyl group act as an electron acceptor group, and a cyano group acts as an anchor group. An optional thiophene group acts as part of the ?-conjugated bridge (spacer). The dye for use as organic photosensitizers in a dye-sensitized solar cell. The dye for use in photodynamic therapies. Computational DFT and time dependent DFT (TD-DFT) modeling techniques showing Light Harvesting Efficiency (LHE), Free Energy for Electron Injection (?Ginject), Excitation Energies, and Frontier Molecular Orbitals (FMOs) indicate that the series of dye comprise a more negative ?Ginject and a higher LHE value; resulting in a higher incident photon to current efficiency (IPCE).Type: GrantFiled: May 20, 2015Date of Patent: June 6, 2017Assignee: King Fahd University of Petroleum and MineralsInventors: Umer Mehmood, Shakeel Ahmed, Ibnelwaleed A. Hussein
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Patent number: 9126987Abstract: The present invention relates to compounds of formula (I), combinations and uses thereof for disease therapy, wherein R1 represents heteroaryl, -carbocyclyl-heteroaryl, -alkenylheteroaryl or -alkylheteroaryl; R2 represents alkyl; carbocyclyl which may optionally be substituted by alkyl; alkenyl; alkynyl, provided a triple bond is not adjacent to X; -alkyl-aryl; -alkyl-heteroaryl; -alkyl-heterocyclyl in which heterocyclyl may optionally be substituted by alkyl; -alkyl-carbocyclyl in which carbocyclyl may optionally be substituted by alkyl; aryl; heteroaryl; or H; X represents S or NR3; R3 represents H or C1-4 alkyl.Type: GrantFiled: November 28, 2007Date of Patent: September 8, 2015Assignee: PROBIODRUG AGInventors: Ulrich Heiser, Daniel Ramsbeck, Mirko Buchholz, Andre J. Niestroj
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Patent number: 9101141Abstract: N-(1,3,4-Oxadiazol-2-yl)arylcarboxamides of the general formula (I) are described as herbicides. In this formula (I) A is nitrogen or CY. R, X, Y and Z are each radicals such as hydrogen, organic radicals such as alkyl, and other radicals such as halogen.Type: GrantFiled: March 21, 2012Date of Patent: August 11, 2015Assignee: BAYER INTERLLECTUAL PROPERTY GMBHInventors: Arnim Köhn, Hartmut Ahrens, Ralf Braun, Simon Dörner-Rieping, Stefan Lehr, Ines Heinemann, Isolde Häuser-Hahn, Elmar Gatzweiler, Christopher Hugh Rosinger
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Publication number: 20150148384Abstract: Disclosed herein are novel A-ring epoxidized triterpenoid compounds and derivatives thereof, including those of the formula (I), wherein the variables are defined herein. Also provided are pharmaceutical compositions, kits, and articles of manufacture comprising such compounds. Methods and intermediates useful for making the compounds, and methods of using the compounds, for example as antioxidant inflammation modulators, and compositions thereof are also provided.Type: ApplicationFiled: June 14, 2013Publication date: May 28, 2015Applicant: REATA PHARMACEUTICALS, INC.Inventors: Eric Anderson, Christopher F. Bender, Xin Jiang, Xiaofeng Liu, Haizhou Sun, Melean Visnick
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Publication number: 20150141474Abstract: 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: ApplicationFiled: April 26, 2013Publication date: May 21, 2015Applicant: NOVARTIS AGInventors: Sejal Patel, Justin Mao, Qian Liu, Tyler Harrison, Rohit Duvadie, Xin Chen, Frederic Zecri
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Publication number: 20150119373Abstract: The invention relates to novel betulinic acid derivatives and related compounds, and pharmaceutical compositions useful for therapeutic treatment of viral diseases and particularly HIV mediated diseases.Type: ApplicationFiled: April 19, 2013Publication date: April 30, 2015Inventors: Bandi Parthasaradhi Reddy, Vedula Manohar Sharma, Kura Rathnakar Reddy, Mamnoor Prem Kumar, Kasireddy Bhaskar Reddy, Mogili Narsingam, Mukkera Venkati, Lanka VL Subrahmanyam, Ravi Mallikarjun Reddy
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Publication number: 20150105252Abstract: Disclosed is a method for controlling the growth of undesired vegetation comprising contacting the vegetation or its environment with a herbicidally effective amount of a compound of Formula 1, including all stereoisomers, N-oxides, and salts thereof, wherein A, R1, Q and J are as defined in the disclosure. Also disclosed is a method wherein the compound of Formula 1 (i.e. in a herbicidally effective amount) is comprised in a herbicidal composition further comprising at least one component selected from the group consisting of surfactants, solid diluents and liquid diluents. Also disclosed are compound of Formula 1 (including all stereoisomers), including N-oxides and salts thereof, their use as herbicides wherein A, R1, Q and J are as defined in the disclosure.Type: ApplicationFiled: October 15, 2014Publication date: April 16, 2015Inventor: THOMAS MARTIN STEVENSON
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Publication number: 20150099779Abstract: The invention relates to ROR modulators; compositions comprising an effective amount of a ROR modulator; and methods for treating or preventing diseases associated with ROR.Type: ApplicationFiled: April 30, 2013Publication date: April 9, 2015Inventors: Anderson Gaweco, Jefferson W. Tilley, John Walker, Samantha Palmer, James Blinn
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Patent number: 8993619Abstract: 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: GrantFiled: April 26, 2013Date of Patent: March 31, 2015Assignee: Novartis AGInventors: 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
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Publication number: 20150065482Abstract: The invention relates to compounds of Formula (0): wherein Q, A1-A8, R4 and R5 and each has the meaning as described herein. Compounds of Formula (0) and pharmaceutical compositions thereof are useful in the treatment of diseases and disorders in which undesired or over-activation of NF-kB signaling is observed.Type: ApplicationFiled: August 22, 2014Publication date: March 5, 2015Applicant: GENENTECH, INC.Inventors: Nicole Blaquiere, Georgette Castanedo, Jianwen A. Feng, Baihua Hu, Steven Staben, Po-wai Yuen, Guosheng Wu, Jason Burch
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Publication number: 20150053894Abstract: The present invention provides charge transporting molecular glass mixtures, luminescent molecular glass mixtures, or combinations thereof comprising at least two nonpolymeric compounds each independently corresponding to the structure (R1Y1)p[(Z1Y2)mR2Y3]nZ2Y4R3 wherein m is zero or one; n is zero up to an integer at which said compound starts to become a polymer; p is an integer of from one to eight; each R1 and R3 is independently a monovalent aliphatic or cycloaliphatic hydrocarbon group having 1 to 20 carbon atoms, an aromatic group or a multicyclic aromatic nucleus; R2, Z1, and Z2 each independently represent multivalent aliphatic or cycloaliphatic hydrocarbon groups having 1 to 20 carbon atoms or an aromatic group; and Y1, Y2, Y3, and Y4 each independently represent one or more linking groupsType: ApplicationFiled: August 25, 2014Publication date: February 26, 2015Inventor: Michel Frantz Molaire
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Patent number: 8957096Abstract: What is described are oxime ether-substituted benzoylamides of the general formula (I) as herbicides. In this formula (I), R, Y and Y are radicals such as hydrogen, organic radicals such as alkyl, and other radicals such as halogen. Q is a tetrazolyl, triazolyl or oxadiazolyl radical.Type: GrantFiled: October 29, 2012Date of Patent: February 17, 2015Assignee: Bayer Intellectual Property GmbHInventors: Andreas Van Almsick, Hartmut Ahrens, Hansjörg Dietrich, Isolde Häuser-Hahn, Ines Heinemann, Elmar Gatzweiler, Christopher Rosinger
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Publication number: 20150045399Abstract: Described herein are liver X receptor (LXR) modulators and methods of utilizing LXR modulators in the treatment of dermal diseases, disorders or conditions. Also described herein are pharmaceutical compositions containing such compounds.Type: ApplicationFiled: September 2, 2014Publication date: February 12, 2015Applicant: Alexar Therapeutics, Inc.Inventor: Raju Mohan
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Publication number: 20150045554Abstract: The present invention relates to a novel synthetic route for the preparation of raltegravir and pharmaceutically acceptable salts, starting from 2-amino-2-methylpropanenitrile and oxadiazole carbonyl chloride, through the formation of a pyrimidinone intermediate of formula (V).Type: ApplicationFiled: December 21, 2012Publication date: February 12, 2015Inventors: Mukund Keshav Gurjar, Swapnil Panditrao Sonawane, Golakchandra Sudarshan Maikap, Gulabrao Dagadu Patil, Shivnath Bhaupatil Shinde, Pankaj Shalikrao, Samit Satish Mehta
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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: 20150030618Abstract: The present application relates to new binder-drug conjugates (ADCs) of N,N-dialkylauristatins that are directed against the target C4.4a, to active metabolites of these ADCs, to processes for preparing these ADCs, to the use of these ADCs for treating and/or preventing illnesses, and also to the use of these ADCs for producing medicaments for treating and/or preventing illnesses, more particularly hyperproliferative and/or angiogenic diseases such as, for example, cancer diseases. Such treatments may be practised as a monotherapy or else in combination with other medicaments or further therapeutic measures.Type: ApplicationFiled: May 5, 2014Publication date: January 29, 2015Applicant: SEATTLE GENETICS, INC.Inventors: Hans-Georg LERCHEN, Lars Linden, Sherif El Sheikh, Jörg Willuda, Charlotte C. Kopitz, Joachim Schuhmacher, Simone Greven, Christoph Mahlert, Beatrix Stelte-Ludwig, Sven Golfier, Rudolf Beier, Iring Heisler, Axel Harrenga, Karl-Heinz Thierauch, Sandra Bruder, Heike Petrul, Hannah Jörissen, Sandra Borkowski
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Publication number: 20150031537Abstract: There are described 4-nitro-substituted N-(tetrazol-5-yl)-, N-(triazol-5-yl)- and N-(1,3,4-oxadiazol-2-yl)arylcarboxamides of the general formula (I) as herbicides. In this formula (I), X, Y and W are radicals such as hydrogen, organic radicals such as alkyl, and other radicals such as halogen. A is N and CY.Type: ApplicationFiled: February 18, 2013Publication date: January 29, 2015Inventors: Simon Dörner-Rieping, Ralf Braun, Arnin Köhn, Hartmut Ahrens, Stefan Lehr, Hansjörg Dietrich, Elmar Gatzweiler, Christopher Hugh Rosinger, Dirk Schmutzler
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Publication number: 20150025042Abstract: Disclosed are compounds of formulae (I), (III), (IV), (VII), (X), (XI), (XII), (XIII) and (XIV), wherein the variables are as defined in the claims, and methods of using compounds of the invention for treating a subject with a proliferative disorder, such as cancer, and methods for treating disorders responsive to Hsp70 induction and/or natural killer induction. Also disclosed are pharmaceutical compositions comprising compounds of the invention and a pharmaceutically acceptable carrier.Type: ApplicationFiled: December 16, 2013Publication date: January 22, 2015Applicant: SYNTA PHARMACEUTICALS CORP.Inventors: Shoujun Chen, Keizo Koya, Zachary Demko, Lijun Sun
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Publication number: 20150023913Abstract: The present disclosure is generally directed to antiviral compounds, and more specifically directed to combinations of compounds which can inhibit the function of the NS5A protein encoded by Hepatitis C virus (HCV), compositions comprising such combinations, and methods for inhibiting the function of the NS5A protein.Type: ApplicationFiled: July 2, 2013Publication date: January 22, 2015Inventors: Piyasena Hewawasam, Omar D. Lopez, Yong Tu, Alan Xiangdong Wang, Ningning Xu, John F. Kadow, Nicholas A. Meanwell, Samayamuthula Venkata Satya Arun Kumar Gupta, Indasi J. Gopi Kumar, Suresh Kumar Ponugupati, Makonen Belema
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Publication number: 20150025235Abstract: Benzamide compounds and derivatives thereof, as can be used for selective inhibition of the SIRT2 enzyme and/or therapeutic use in the treatment of Huntington's disease.Type: ApplicationFiled: May 30, 2014Publication date: January 22, 2015Inventors: Richard B. Silverman, Hua Wang, Mohammad Khanfar, Aleksey G. Kazantsev
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Publication number: 20150018210Abstract: Sulfinylaminobenzamides of the general formula (I) as herbicides are described. In this formula (I), R, R?, R?, X, W and Z are radicals such as hydrogen, organic radicals such as alkyl, and other radicals such as halogen. Q is a tetrazolyl, triazolyl or oxadiazolyl radical.Type: ApplicationFiled: February 18, 2013Publication date: January 15, 2015Inventors: Hartmut Ahrens, Ralf Braun, Arnim Koehn, Stefan Lehr, Hansjoerg Dietrich, Dirk Schmutzler, Elmar Gatzweiler, Christopher Hugh Rosinger
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Publication number: 20150018209Abstract: The invention relates to sulfin- and sulfonimidoylbenzamides of general formula (S) used as herbicides. In said formula (I), R, R?, R?, X, W and Z represent radicals such as hydrogen, organic radicals such as alkyl, and other radicals such as halogens. Q represents a tetrazolyl-, triazolyl or oxadiazolyl radicals.Type: ApplicationFiled: February 18, 2013Publication date: January 15, 2015Inventors: Hartmut Ahrens, Ralf Braun, Simon Doerner-Rieping, Arnim Koehn, Stefan Lehr, Hansjoerg Dietrich, Dirk Schmutzler, Elmar Gatzweiler, Christopher HUGH Rosinger
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Publication number: 20150011517Abstract: The present invention relates to a lupane triterpenoid derivatives and pharmaceutical use thereof, specifically relates to a lupane triterpenoid derivatives of formula (I)˜(III), a pharmaceutical composition and a combination preparation comprising a lupane triterpenoid derivatives or a pharmaceutically acceptable salt thereof in a therapeutically-effective dose, particularly relates to the use in preparation of a medicament for the treatment of HIV-1/AIDS.Type: ApplicationFiled: January 30, 2013Publication date: January 8, 2015Inventor: Feng Lu
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Publication number: 20150005232Abstract: Disclosed are compounds of Formula 1, and pharmaceutically acceptable salts thereof, wherein R1, R2, R3, R4, R5, and R6 are defined in the specification. This disclosure also relates to materials and methods for preparing compounds of Formula 1, to pharmaceutical compositions which contain them, and to their use for treating obesity and related diseases, disorders, and conditions associated with MetAP2.Type: ApplicationFiled: February 28, 2013Publication date: January 1, 2015Applicant: Takeda Pharmaceutical Company LimitedInventors: Zacharia Cheruvallath, Philip Erickson, Jun Feng, Mallareddy Komandla, John David Lawson, Christopher McBride, Joanne Miura, Sean Murphy, Mingnam Tang, Huong-Thu Ton-Nu
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Patent number: 8916592Abstract: Compounds of formula I wherein X is O or S(?O)n; n is 0, 1 or 2; R1 is optionally substituted alkyl, haloalkyl, alkenyl, haloalkenyl, alkynyl, haloalkynyl, cycloalkyl, halocycloalkyl, cycloalkenyl, halocycloalkenyl, phenyl, hetaryl, phenylalkyl, hetaryl alkyl, optionally fused to phenyl, hetaryl or heterocyclyl; A is —NRb2, —C(=G)GRb, —C(=G)NRb2, —C(?NORb)Rb, C(=G)[N?SRb2], —C(=G)NRb—NRb2, C2-C6-alkandiyl, C2-C6-alkenediyl, C1-C3-alkyl-G-C1-C3-alkyl, wherein Rb is as defined in the description, or optionally substituted phenyl, hetaryl, heterocyclyl, optionally fused to phenyl or heterocyclyl; B is an optionally substituted saturated or partially unsaturated hydrocarbon chain with 1 to 3 carbon chain atoms; D is an optionally substituted saturated or partially unsaturated hydrocarbon chain with 1 to 5 carbon chain atoms or C3-C6-cycloalkyl; G is oxygen or sulfur; or the enantiomers or diastereomers or salts or N-oxides thereof, processes for preparing the compounds I, pesticidal compositions and synergistic mType: GrantFiled: December 13, 2006Date of Patent: December 23, 2014Assignee: Merial LimitedInventors: Matthias Pohlman, Michael Hofmann, Henricus Maria Martinus Bastiaans, Michael Rack, Deborah L. Culbertson, Hassan Oloumi-Sadeghi, Takeo Hokama, Christopher Palmer, Jürgen Langewald
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Publication number: 20140371068Abstract: N-(1,2,5-Oxadiazol-3-yl)-, N-(1,3,4-oxadiazol-2-yl)-, N-(tetrazol-5-yl)- or N-(triazol-5-yl)arylcarboxamides of the general formula (I) are described as herbicides. In this formula (I), R, V, X, Y and Z are radicals such as hydrogen, organic radicals such as alkyl, and other radicals such as halogen. Q is a tetrazolyl, triazolyl or oxadiazolyl radical. W is CY or N.Type: ApplicationFiled: December 10, 2012Publication date: December 18, 2014Inventors: Armin Koehn, Stefan Lehr, Ralf Braun, Simon Doerner-Rieping, Hartmut Ahrens, Hansjoerg Dietrich, Isolde Haeuser-Hahn, Christopher Hugh Rosinger, Elmar Gatzweiler
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Publication number: 20140371276Abstract: The invention relates to compounds acting as selective antagonists of Transient Receptor Potential cation channel subfamily M member 8 (TRPM8), and having formula (I). Said compounds are useful in the treatment of diseases associated with activity of TRPM8 such as pain, inflammation, ischaemia, neurodegeneration, stroke, psychiatric disorders, itch, irritable bowel diseases, cold induced and/or exhacerbated respiratory disorders and urological disorders.Type: ApplicationFiled: December 19, 2012Publication date: December 18, 2014Inventors: Alessio Moriconi, Gianluca Bianchini, Sandro Colagioia, Laura Brandolini, Andrea Aramini, Chiara Liberati, Silvia Bovolenta
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Patent number: 8901119Abstract: The present invention relates to a compound of Formula (I): or a pharmaceutically acceptable salt thereof, corresponding pharmaceutical compositions, compound preparation and treatment methods directed to bacterial infections and inhibition of bacterial peptide deformylase (PDF) activity.Type: GrantFiled: March 9, 2012Date of Patent: December 2, 2014Assignee: GlaxoSmithKline Intellectual Property (No. 2) LimitedInventors: Kelly M. Aubart, Andrew B. Benowitz, Yuhong Fang, James Hoffman, Joseph M. Karpinski, Andrew Nicholson Knox, Xiangmin Liao, Donghui Qin, Dongchuan Shi, Jared T. Spletstoser
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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: 8883801Abstract: The present invention relates to certain pyrazolo[1,5-a]pyrimidine compounds of Formula (I) as inhibitors of mammalian Target Of Rapamycin (mTOR) kinase, which is also known as FRAP, RAFT, RAPT or SEP. The compounds may be used in the treatment of cancer and other disorders where mTOR is deregulated. The present invention further provides pharmaceutical compositions comprising the pyrazolo[1,5-a]pyrimidine compounds.Type: GrantFiled: August 22, 2011Date of Patent: November 11, 2014Assignee: Merck Sharp & Dohme Corp.Inventors: Lianyun Zhao, Duan Liu, Shuyi Tang, Amit K. Mandal, Umar Faruk Mansoor, Lalanthi Dilrukshi Vitharana, Panduranga Adulla P. Reddy, M. Arshad Siddiqui
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Publication number: 20140323722Abstract: A compound represented by formula: its pharmaceutically acceptable salt, or a solvate thereof. Ring B is substituted or unsubstituted nitrogen-containing hetero ring, R2 and R3 are each independently hydrogen, halogen, hydroxy, cyano, nitro, carboxy, substituted or unsubstituted alkyl or substituted or unsubstituted alkyloxy, R2 and R3 taken together may form oxo, R4 is a group represented by the formula: —(CR6R7)n—R8, R6 and R7 are each independently hydrogen, halogen, hydroxy, carboxy, substituted or unsubstituted alkyl or substituted or unsubstituted alkyloxy, R6 and R7 taken together with the adjacent carbon atom to which they are attached may form a substituted or unsubstituted ring, and n is an integer of 0 to 3.Type: ApplicationFiled: April 29, 2014Publication date: October 30, 2014Applicant: Shionogi & Co., Ltd.Inventors: Koji MASUDA, Shiro Kida, Naoki Yoshikawa, Manabu Katou, Terukazu Kato, Mado Nakajima, Eiichi Kojima, Mitsuhiro Yonehara
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Publication number: 20140309112Abstract: What is described are oxime ether-substituted benzoylamides of the general formula (I) as herbicides. In this formula (I), R, Y and Y are radicals such as hydrogen, organic radicals such as alkyl, and other radicals such as halogen. Q is a tetrazolyl, triazolyl or oxadiazolyl radical.Type: ApplicationFiled: October 29, 2012Publication date: October 16, 2014Inventors: Andreas Van Almsick, Hartmut Ahrens, Hansjörg Dietrich, Isolde Häuser-Hahn, Ines Heinemann, Elmar Gatzweiler, Christopher Rosinger
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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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Publication number: 20140296177Abstract: A new class of biotin protein ligase (BPL) inhibitors that have antibacterial activity against multiple Staphylococcus aureus isolates, including clinically important methicillin-resistant S. aureus (MRSA) are disclosed that are non-toxic.Type: ApplicationFiled: September 21, 2012Publication date: October 2, 2014Inventors: Andrew Abel, Steven Polyak, Grant Booker, John Wallace, Tatiana Soares Da Costa, Angie Jarrad, William Tieu, Kelly Lee Keeling, Daniel Sejer Pederson, Nicole Pendini, Matthew Wilce, Min Yin Yap
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Patent number: 8846727Abstract: A new class of haloalkyl heteroaryl benzamides is described. These compounds show strong activity against hepatitis viruses.Type: GrantFiled: May 11, 2010Date of Patent: September 30, 2014Assignee: Romark Laboratories, L.C.Inventors: Jean-Francois Rossignol, J. Edward Semple
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Publication number: 20140275133Abstract: The present invention is directed to compounds of the Formula (I) as well as pharmaceutically acceptable salts thereof that are possible useful for treating aldosterone-mediated diseases. The invention furthermore relates to processes for preparing compounds of the Formula (I), to their possible use for the treatment of the above mentioned diseases and for preparing pharmaceuticals for this purpose, and to pharmaceutical compositions which comprise compounds of the Formula (I).Type: ApplicationFiled: October 8, 2012Publication date: September 18, 2014Inventors: Hong Shen, Jason M. Cox, Hong Dong Chu
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Patent number: 8835469Abstract: The present invention relates to substituted benzamide derivatives of the Formula I and their pharmaceutically acceptable salts, pharmaceutically acceptable solvates, enantiomers, diastereomers, prodrugs, metabolites, and polymorphs and can be useful for treating disease states mediated by glucokinase. Compounds disclosed herein can be used for reducing blood glucose levels and for increasing insulin secretion for treating type II diabetes. The invention also relates to processes for the preparation of the compounds of invention, pharmaceutical compositions containing the compounds, and their use.Type: GrantFiled: July 22, 2010Date of Patent: September 16, 2014Assignee: Cadila Healthcare LimitedInventors: Rajendra Kharul, Mukul R. Jain, Pankaj R. Patel
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Publication number: 20140255850Abstract: A method for fabricating a semiconductor product includes applying a photo-resist layer to a substrate, the photo-resist layer including a higher acid concentration at an upper portion of the photo-resist layer than at a lower portion of the photo-resist layer. The method also includes exposing the photo-resist layer to a light source through a mask including a feature, the photo-resist layer including a floating, diffusing acid that will diffuse into a region of the photo-resist layer affected by the feature while not diffusing into a feature formed by the mask.Type: ApplicationFiled: March 9, 2013Publication date: September 11, 2014Applicant: Taiwan Semiconductor Manufacturing Company, Ltd.Inventors: Ching-Yu Chang, Ming-Feng Shieh, Wen-Hung Tseng
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Publication number: 20140256744Abstract: Described herein are compounds that are antagonists of lysophosphatidic receptor(s). Also described are pharmaceutical compositions and medicaments that include the compounds described herein, as well as methods of using such antagonists, alone and in combination with other compounds, for treating LPA-dependent or LPA-mediated conditions or diseases.Type: ApplicationFiled: May 21, 2014Publication date: September 11, 2014Inventors: Ryan Clark, Brian Andrew Stearns, Lucy Zhao, Thomas Jon Seiders, Deborah Volkots, Jeannie M. Arruda
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Publication number: 20140249159Abstract: The invention relates to compounds of Formula I: wherein Ar1, Ar2, Ar3, L1, L2, Y, Z and v are defined in the specification, and pharmaceutically acceptable derivatives thereof, compositions comprising an effective amount of a compound of Formula I or a pharmaceutically acceptable derivative thereof, and methods for treating or preventing a condition such as pain, UI, an ulcer, IBD and IBS, comprising administering to an animal in need thereof an effective amount of a compound of Formula I or a pharmaceutically acceptable derivative thereof.Type: ApplicationFiled: May 16, 2012Publication date: September 4, 2014Inventors: Noriyuki Kurose, Kayoko Hata, Yasuyoshi Iso, Naoko Yamaguchi, Bin Shao, Laykea Tafesse, Xiaoming Zhou, Jianming Yu
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Publication number: 20140243334Abstract: This invention provides compounds of formula (I): wherein R1a, R1b, R1c, R2a, R2b, R2c, and R2d have values as described in the specification, useful as inhibitors of HDAC6. The invention also provides pharmaceutical compositions comprising the compounds of the invention and methods of using the compositions in the treatment of proliferative, inflammatory, infectious, neurological or cardiovascular diseases or disorders.Type: ApplicationFiled: May 5, 2014Publication date: August 28, 2014Applicant: Millennium Pharmaceuticals, Inc.Inventors: Emily F. Calderwood, Dylan B. England, Alexandra E. Gould, Sean J. Harrison, Liting Ma
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Publication number: 20140234939Abstract: Benzamide compounds and derivatives thereof, as can be used for selective inhibition of the SIRT2 enzyme and/or therapeutic use in the treatment of Huntington's disease.Type: ApplicationFiled: December 23, 2013Publication date: August 21, 2014Applicant: Northwestern UniversityInventors: Richard B. Silverman, Hua Wang, Mohammad Khanfar
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Publication number: 20140235660Abstract: The present invention relates to compounds of formula I: in which n, m, X, Y1, R1, R2, R3, R4 and R5 are defined in the Summary of the Invention; capable of being both potent antagonists and degraders of estrogen receptors. The invention further provides a process for the preparation of compounds of the invention, pharmaceutical preparations comprising such compounds and methods of using such compounds and compositions in the management of diseases or disorders associated with aberrant estrogen receptor activity.Type: ApplicationFiled: February 12, 2014Publication date: August 21, 2014Applicant: NOVARTIS AGInventors: Heather Elizabeth BURKS, Michael A. DECHANTSREITER, Guo HE, Jill NUNEZ, Stefan PEUKERT, Clayton SPRINGER, Yingchuan SUN, Noel Marie-France THOMSEN, George Scott TRIA, Bing YU
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Publication number: 20140221421Abstract: Compounds of formula I: or salts thereof are disclosed. Also disclosed are pharmaceutical compositions comprising a compound of formula I, processes for preparing compounds of formula I, intermediates useful for preparing compounds of formula I and therapeutic methods for treating a Retroviridae viral infection including an infection caused by the HIV virus.Type: ApplicationFiled: January 9, 2014Publication date: August 7, 2014Applicant: GILEAD SCIENCES, INC.Inventors: Steven S. BONDY, Carina E. CANNIZZARO, Chien-Hung CHOU, John O. LINK, Qi LIU, Scott D. SCHROEDER, Winston C. TSE, Jennifer R. ZHANG
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Publication number: 20140221332Abstract: Compounds that modulate GluR5 activity and methods of using the same are disclosed.Type: ApplicationFiled: May 25, 2012Publication date: August 7, 2014Applicant: SUNOVION PHARMACEUTICALS INC.Inventors: Michele L. R. Heffernan, Larry Wendell Hardy, Frank Xinhe Wu, Lakshmi D. Saraswat
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Patent number: 8796320Abstract: Provided is a 1,3,4-oxadiazole-2-carboxamide compound which has STAT3 inhibitory activity and is useful as an anticancer agent. Provided is a 1,3,4-oxadiazole-2-carboxamide compound represented by formula (I) or a pharmacologically acceptable salt thereof (in the formula, Ar represents a furyl group or the like; R1 represents a hydrogen atom or the like; and —X—Y represents a diaryl group such as a biphenyl group).Type: GrantFiled: December 28, 2010Date of Patent: August 5, 2014Assignees: General Incorporated Association Pharma Valley Project Supporting Organization, Pharma Design, Shizuoka Prefecture, Kumamoto Health Science University, Kabushiki Kaisha Yakult HonshaInventors: Akira Asai, Kenji Matsuno, Naohisa Ogo, Osamu Takahashi, Yoshiaki Masuda, Ayumu Muroya, Yasuto Akiyama, Tadashi Ashizawa, Tadashi Okawara
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Publication number: 20140199263Abstract: The present invention relates to compounds of formula (I) that are useful as hepatitis C virus (HCV) NS5B polymerase inhibitors, the synthesis of such compounds, and the use of such compounds for inhibiting HCV NS5B polymerase activity, for treating or preventing HCV infections and for inhibiting HCV viral replication and/or viral production in a cell-based system.Type: ApplicationFiled: August 16, 2012Publication date: July 17, 2014Inventors: Casey Cameron McComas, Nigel J. Liverton, Joerg Habermann, Uwe Koch, Frank Narjes, Peng Li, Xuanjia Peng, Richard Soll, Hao Wu, Anandan Palani, Xing Dai, Hong Liu, Shuwen He, Zhong Lai, Qun Dang, Nicolas Zorn
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Patent number: RE45288Abstract: This invention provides, but is not limited to, novel oleanolic acid derivatives having the formula: wherein the variables are defined herein. Also provided are pharmaceutical compositions, kits and articles of manufacture comprising such compounds, methods and intermediates useful for making the compounds, and methods of using the compounds and compositions.Type: GrantFiled: November 14, 2013Date of Patent: December 9, 2014Assignee: Reata Pharmaceuticals, Inc.Inventors: Eric Anderson, Xin Jiang, Xiaofeng Liu, Melean Visnick
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Patent number: RE45325Abstract: This invention provides, but is not limited to, novel oleanolic acid derivatives having the formula: wherein the variables are defined herein. Also provided are pharmaceutical compositions, kits and articles of manufacture comprising such compounds, methods and intermediates useful for making the compounds, and methods of using the compounds and compositions.Type: GrantFiled: November 14, 2013Date of Patent: January 6, 2015Assignee: Reata Pharmaceuticals, Inc.Inventors: Eric Anderson, Xin Jiang, Xiaofeng Liu, Melean Visnick