Patents Issued in July 21, 2016
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Publication number: 20160207912Abstract: The present invention relates to certain heteroaryl amide compounds, pharmaceutical compositions containing them, and methods of using them, including methods for preventing, reversing, slowing, or inhibiting protein aggregation, and methods of treating diseases that are associated with protein aggregation, including neurodegenerative diseases such as Parkinson's disease, Alzheimer's disease, Lewy body disease, Parkinson's disease with dementia, fronto-temporal dementia, Huntington's Disease, amyotrophic lateral sclerosis, and multiple system atrophy, and cancer and melanoma.Type: ApplicationFiled: December 29, 2015Publication date: July 21, 2016Inventors: Wolfgang Wrasidlo, Emily M. Stocking
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Publication number: 20160207913Abstract: Disclosed are compounds having the formula: wherein X is as defined herein, and methods of making and using the same.Type: ApplicationFiled: March 25, 2016Publication date: July 21, 2016Inventor: Gren WANG
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Publication number: 20160207914Abstract: The invention provides novel compounds having the general formula: wherein R1, R2, R3, R4, R5 and R6 are as described herein, compositions including the compounds and methods of using the compounds.Type: ApplicationFiled: January 30, 2015Publication date: July 21, 2016Applicant: HOFFMANN-LA ROCHE INC.Inventors: Xingchun Han, Hassan Javanbakht, Min Jiang, Chungen Liang, Jianping Wang, Yongguang Wang, Zhanguo Wang, Robert James Weikert, Song Yang, Chengang Zhou
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Publication number: 20160207915Abstract: The present invention relates to prodrug derivatives of Mps-1 kinase inhibitors, processes for their preparation, and their use for the treatment and/or prophylaxis of diseases.Type: ApplicationFiled: June 6, 2014Publication date: July 21, 2016Inventors: Volker Schulze, Hans-Georg Lerchen, Donald Bierer, Antje Margret Wengner, Gerhard Siemeister, Philip Lienau, Ursula Krenz, Dirk Kosemund, Detlef Stockigt, Michael Bruning, Ulrich Lucking, Ildiko Terebesi
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Publication number: 20160207916Abstract: The present invention relates to naphthylurea derivatives. Such substances can significantly inhibit VEGFR2 and PDGFR-? receptor tyrosine kinase phosphorylation at nanomolar concentration levels.Type: ApplicationFiled: August 20, 2014Publication date: July 21, 2016Inventors: Yingjian HU, Zhibin LUO, Yanhong ZHANG, Li HAN, Yun WANG, Hongfei LU
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Publication number: 20160207917Abstract: The present invention relates to new benzoquinolone inhibitors of VMAT2, pharmaceutical compositions thereof, and methods of use thereof represented by structural Formula I.Type: ApplicationFiled: September 26, 2014Publication date: July 21, 2016Inventor: Chengzhi Zhang
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Publication number: 20160207918Abstract: This invention provides compounds having drug and bio-affecting properties, their pharmaceutical compositions and method of use. In particular, the invention is concerned with azaindoleoxoacetyl piperazine derivatives having the Formula I: wherein Q is These compounds possess unique antiviral activity, whether used alone or in combination with other antivirals, antiinfectives, immunomodulators or HIV entry inhibitors. More particularly, the present invention relates to the treatment of HIV and AIDS.Type: ApplicationFiled: March 16, 2016Publication date: July 21, 2016Inventors: Tao Wang, Zhongxing Zhang, Nicholas A. Meanwell, John F. Kadow, Zhiwei Yin, Qiufen May Xue, Alicia Regueiro-Ren, John D. Matiskella, Yasutsugu Ueda
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Publication number: 20160207919Abstract: The present invention relates to compounds that may be used for binding and imaging tau aggregates and related beta-sheet aggregates including, for example, beta-amyloid aggregates or alpha-synuclein aggregates.Type: ApplicationFiled: March 25, 2016Publication date: July 21, 2016Applicant: Hoffmann-La Roche Inc.Inventors: Luca GOBBI, Henner KNUST, Matthias KOERNER, Dieter MURI
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Publication number: 20160207920Abstract: Provided herein are isoergoline compounds and pharmaceutical compositions thereof. In other embodiments, provided herein are methods of treatment, prevention, or amelioration of a variety of medical disorders such as, for example, migraine using the compounds and pharmaceutical compositions disclosed herein. In still other embodiments, provided herein are methods of agonizing receptors such as, for example, the 5-HT1A, 5-HT1B and 5-HT1D receptors without agonizing the 5-HT2B receptor using the compounds and pharmaceutical compositions disclosed herein. In still other embodiments, provided herein are methods of antagonizing the 5-HT2B adrenergic alpha2A and/or the alpha2B receptors using the compounds and pharmaceutical compositions disclosed herein. In still other embodiments, provided herein are methods of antagonizing the D2 and D3 receptor using the compounds and pharmaceutical compositions disclosed herein.Type: ApplicationFiled: January 20, 2016Publication date: July 21, 2016Inventors: THOMAS ARMER, GEOFF MCKINLEY, SCOTT BORLAND, MIGUEL GUZMAN
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Publication number: 20160207921Abstract: Provided herein are ergoline compounds and pharmaceutical compositions thereof. In some embodiments, provided herein are methods of treatment, prevention, or amelioration of a variety of medical disorders such as, for example, migraine using the compounds and pharmaceutical compositions disclosed herein. In still other embodiments, provided herein are methods of agonizing receptors such as, for example, the 5-HT1A, 5-HT1B and 5-HT1D receptors without agonizing the 5-HT2B receptor using the compounds and pharmaceutical compositions disclosed herein. In still other embodiments, provided herein are methods of antagonizing the 5-HT2B adrenergic alpha2A and/or the alpha2B receptors using the compounds and pharmaceutical compositions disclosed herein. In still other embodiments, provided herein are methods of antagonizing the D2 and D3 receptor using the compounds and pharmaceutical compositions disclosed herein.Type: ApplicationFiled: January 20, 2016Publication date: July 21, 2016Inventors: Thomas ARMER, Geoff MCKINLEY, Scott BORLAND, Miguel GUZMAN, Ármin SZABOLCS, János GERENCSER
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Publication number: 20160207922Abstract: The present invention provides compounds of Formula I and the pharmaceutically acceptable salts thereof, which are inhibitors of the ROMK (Kir1.1) channel. The compounds may be used as diuretic and/or natriuretic agents and for the therapy and prophylaxis of medical conditions including cardiovascular diseases such as hypertension, heart failure and chronic kidney disease and conditions associated with excessive salt and water retention.Type: ApplicationFiled: July 28, 2014Publication date: July 21, 2016Applicant: Merck Sharp & Dohme Corp.Inventors: Haifeng Tang, Barbara Pio, Jinlong Jiang, Alexander Pasternak, Shuzhi Dong, Ronald Dale Ferguson, II, Zack Zhiqiang Guo, Harry Chobanian, Jessica Frie, Yan Guo, Zhicai Wu, Yang Yu, Ming Wang
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Publication number: 20160207923Abstract: The invention provides azaspiro[4.5]decane derivatives of Formula (A): and pharmaceutically acceptable salts, solvates, hydrates, N-oxides, and diastereomers thereof, wherein A1, X, A2, Rr, R2?, W1, R3?, R4?, a, and b are defined in the disclosure. The invention also provides compounds of Formulae I, and B-G, and pharmaceutically acceptable salts, solvates, hydrates, N-oxides, and diastereomers thereof. Further, the invention provides use of the compounds of Formulae A-G and I, and the pharmaceutically acceptable salts, solvates, hydrates, N-oxides, and diastereomers thereof, to treat pain. In certain embodiments, Compounds of the Disclosure are useful for treating a disorder responsive to blockade of one or more sodium channels.Type: ApplicationFiled: August 11, 2014Publication date: July 21, 2016Inventors: Mark A. Youngman, Laykea Tafesse, Jae Hyun Park
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Publication number: 20160207924Abstract: The present invention provides a 2, 6-di-nitrogen-containing substituted purine derivative having a formula (I) structure, or pharmaceutical salt or hydrate thereof, and preparation method and use thereof. The compound is broad spectrum anticancer, low toxicity, high anticancer activity and good stability.Type: ApplicationFiled: August 27, 2014Publication date: July 21, 2016Applicant: Zhejiang Medicine Co., Ltd. Xinchang Pharmaceutical FactoryInventors: Guofeng Wu, Yongmei Xu, Wei Mao, Chunlin Chen, Zhanggui Wu, Xiaoqin Lin, Jun Wang, Jinna Cai, Sen Xiao, Lili Lv
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Publication number: 20160207925Abstract: The present invention provides salts of L-methylfolate of formula I, wherein X and Y both are elected from H, amino acids, and amine compounds, wherein both X and Y are not H in a single compound, i.e. when X?H, Y is not H and when Y?H, X is not H. The invention also relates to a process for the preparation of salts of l-methylfolate. Furthermore, the invention also relates to medicaments and nutritional supplements comprising salts of l-methylfolate.Type: ApplicationFiled: December 31, 2013Publication date: July 21, 2016Inventor: Gianni Fracchia
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Publication number: 20160207926Abstract: The instant invention provides compounds of formula I which are PI3K-delta inhibitors, and as such are useful for the treatment of PI3K-delta-mediated diseases such as inflamation, asthma, COPD and cancer.Type: ApplicationFiled: November 15, 2013Publication date: July 21, 2016Applicant: Merck Sharp & Dohme Corp.Inventors: Abdelghani Abe Achab, Michael D. Altman, Yongqi Deng, Solomon Kattar, Jason D. Katz, Joey L. Methot, Hua Zhou, Meredeth McGowan, Matthew P. Christopher, Yudith Garcia, Neville John Anthony, Francesc Xavier Fradera Llinas, Liping Yang, Changwei Mu, Xiaona Wang, Feng Shi, Baijun Ye, Sixing Zhang, Xiaoli Zhao, Rong Zhang, Kin Chiu Fong, Xiansheng Leng
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Publication number: 20160207927Abstract: The present invention relates to a purine compound useful as a kinase inhibitor.Type: ApplicationFiled: August 18, 2015Publication date: July 21, 2016Inventors: DiZhong Chen, Meredith Williams
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Publication number: 20160207928Abstract: The present invention relates to novel compounds showing an inhibitory effect on Mps-1 kinase, to methods of preparing said compounds, to pharmaceutical compositions and combinations comprising said compounds, to the use of said compounds for manufacturing a pharmaceutical composition for the treatment or prophylaxis of a disease, as well as to intermediate compounds useful in the preparation of said compounds.Type: ApplicationFiled: June 4, 2014Publication date: July 21, 2016Inventors: Volker SCHULZE, Hartmut SCHIROK, Dirk KOSEMUND, Hans BRIEM, Benjamin BADER, Ulf BÖMER, Antje Margret WENGNER, Gerhard SIEMEISTER, Philip LIENAU, Detlef STÖCKIGT, Ulrich LÜCKING, Andreas SCHALL
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Publication number: 20160207929Abstract: The present disclosure provides novel compounds useful as PI3K protein kinase modulators, in particular as PI3K delta (?) and/or gamma (?) protein kinase modulators. The present disclosure also provides methods for preparing PI3K protein kinase modulators, pharmaceutical compositions containing them, and methods of treatment, prevention and/or amelioration of PI3K kinase mediated diseases or disorders with them.Type: ApplicationFiled: July 1, 2014Publication date: July 21, 2016Applicant: RHIZEN PHARMACEUTICALS SAInventors: Prashant Kashinath Bhavar, Swaroop Kumar Venkata Satya Vakkalanka, Govindarajulu Babu
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Publication number: 20160207930Abstract: The invention relates novel NK1 receptor antagonists represented in formula A, wherein R1 and R2 independently are selected from the group consisting of (C1-4)alkyl, (C1-4)haloalkyl, (C1-4)alkoxy, CD3 or halogen; R3 is selected from the group consisting of hydrogen, (C1-4)alkyl, (C1-4)haloalkyl and (C1-4)hydroxyalkyl; R4 is selected from the group consisting of phenyl, 5-membered heteroaryl and 6-membered heteroaryl; R5 and R6 are independently selected from the group consisting of hydrogen, (C1-4)alkyl, (C1-4) hydroxyalkyl and (C1-4)haloalkyl and X and Y are independently selected from the group consisting of CH and N. The invention furthermore relates to intermediates for the preparation of said compounds, to their use in therapy, and to pharmaceutical compositions comprising said compounds.Type: ApplicationFiled: August 15, 2014Publication date: July 21, 2016Applicant: LEO PHARMA A/SInventors: Haakan BLADH, Jakob FELDING, Ding ZHOU, Zhen-wei CAI, Morten Dahl SØRENSEN
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Publication number: 20160207931Abstract: The present invention relates to a pyrrolopyridazine derivative represented by Formula 1 of the detailed description, or a pharmaceutically acceptable salt thereof. The compound according to the present invention and a pharmaceutically acceptable salt thereof can inhibit the activity of protein kinase(s), and thus are useful for preventing or treating diseases related thereto.Type: ApplicationFiled: August 29, 2014Publication date: July 21, 2016Applicant: CJ Healthcare CorporationInventors: Tae Gon BAIK, Won-Hyuk JUNG, Seung In KIM, Seung Chan KIM, Sook Kyung PARK, Su Yeon JUNG, Seung Hee JI, So Young KI, Min Cheol KIM, Eun Young LEE, Eun Mi HONG
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Publication number: 20160207932Abstract: The present invention relates to a compound of general Formula (VIII), the compound having a bowl-shaped conformation, its formation and its use in asymmetric catalysis. In Formula (VIII), M is a metal selected from the group consisting of Group 1 to Group 14 metals, lanthanides and actinides; R is one of —COOR3, —R4COOR3, —R4CHO, —R4COR3, —R4CONR5R6, —R4COX, —R4OP(?O)(OH)2, —R4P(?O)(OH)2), —R4C(O)C(R3)CR5R6 and R4CO2C(R3)O, wherein R1, R2, R3, R4, R5 and R6 are as defined herein.Type: ApplicationFiled: October 30, 2015Publication date: July 21, 2016Inventors: Teck Peng Loh, Jian Xiao
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Publication number: 20160207933Abstract: The invention relates to inhibitors of glucosylceramide synthase (GCS) useful for the treatment metabolic diseases, such as lysosomal storage diseases, either alone or in combination with enzyme replacement therapy, and for the treatment of cancer.Type: ApplicationFiled: August 25, 2015Publication date: July 21, 2016Inventors: Elyse BOURQUE, Mario CABRERA-SALAZAR, Cassandra CELATKA, Seng CHENG, Mary A. CROMWELL, Andrew GOOD, Bradford HIRTH, Katherine JANCSICS, John P. LEONARD, Lingyun LI, James LILLIE, Hanlan LIU, Elina MAKINO, John MARSHALL, Paul MASON, Markus METZ, Fazeela MORSHED, Thomas O'SHEA, Ronald SCHEULE, Renato SKERLJ, Bing WANG, Yibin XIANG, Zhong ZHAO
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Publication number: 20160207934Abstract: The present invention relates to a compound of formula (I): wherein: X is methyl or chlorine; R1 is fluorine or bromine; R2 is ethynyl, C1-C3alkoxy, C1-C3haloalkoxy, or C1-C3alkoxy-C1-C3alkoxy-; and Q is a pyran-3,5-dione-4-yl, a thiopyran-3,5-dione-4-yl, a piperidine-3,5-dione-4-yl, a cyclopentane-1,3-dione-2-yl, a cyclohexane-1,3, 5-trione-2-yl, a cyclohexane-1,3-dione-2-yl, or a cycloheptane-1,3-dione-2-yl, or a derivative thereof (e.g. a fused such as fused bicyclic derivative, and/or a spirocyclic derivative), or an enol ketone tautomer derivative thereof, wherein Q is further defined herein; and wherein the compound of formula (I) is optionally present as an agrochemically acceptable salt thereof. Preferably, X is methyl; and/or R1 is fluorine; and/or R2 is —O—R2A, wherein R2A is methyl, ethyl, trifluoromethyl, difluoromethyl, trifluoroethyl, or —CH2CH2OCH3. These compounds are suitable for use as herbicides.Type: ApplicationFiled: May 29, 2014Publication date: July 21, 2016Applicant: Syngenta LimitedInventors: Janice Black, James Nicholas Scutt, Louisa Whalley, Nigel James Willets
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Publication number: 20160207935Abstract: In one aspect, the invention relates to substituted 5-aminothieno[2,3-c]pyridazine-6-carboxamide analogs, derivatives thereof, and related compounds, which are useful as positive allosteric modulators of the muscarinic acetylcholine receptor M4 (mAChR M4); 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: ApplicationFiled: August 22, 2014Publication date: July 21, 2016Inventors: Craig W. Lindsley, P. Jeffrey Conn, Michael R. Wood, Michael S. Poslusney, James C. Tarr, Bruce J. Melancon
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Publication number: 20160207936Abstract: Compounds of the formula I or II: wherein X, m, Ar, R1 and R2 are as defined herein. The subject compounds are useful for treatment of IRAK-mediated conditions.Type: ApplicationFiled: December 18, 2015Publication date: July 21, 2016Inventors: Nidhi Arora, Shaoqing Chen, Johannes Cornelius Hermann, Andreas Kuglstatter, Sharada Shenvi Labadie, Ciara Jeou Jen Lin, Matthew C. Lucas, Amy Geraldine Moore, Eva Papp, Francisco Xavier Talamas, Jutta Wanner, Yansheng Zhai
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Publication number: 20160207937Abstract: Provided are a compound having a novel mother nucleus, which can be a promising drug discovery seed compound, use thereof as an antifungal agent, and a production method thereof and the like. A compound represented by the following formula: or a pharmaceutically acceptable salt thereof, and an antifungal agent containing same, and the like.Type: ApplicationFiled: August 29, 2014Publication date: July 21, 2016Applicants: OP BIO FACTORY CO., LTD., SEED RESEARCH INSTITUTE CO., LTD.Inventors: Morita IWAMI, Sachi KATO, Yoshimi MATSUMOTO, Hideo NAOKI
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Publication number: 20160207938Abstract: The present invention concerns the compounds of formula the N-oxide forms, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein Z represents NH; Y represents —C3-9alkyl-, —C2-9alkenyl-, —C3-7alkyl-CO—NH optionally substituted with amino, mono- or di(C1-4alkyl)amino or C1-4alkyloxycarbonylamino-, —C3-7alkenyl-CO—NH— optionally substituted with amino, mono- or di(C1-4alkyl)amino- or C1-4alkyloxycarbonylamino-, C1-5alkyl-NR13—C1-5alkyl-, —C1-5alkyl-NR14—CO—C1-5alkyl-, —C1-6alkyl-CO—NH—, —C1-5alkyl-CO NR15—C1-5alkyl-, —C1-3alkyl-NH—CO-Het20-, —C1-2alkyl-CO-Het21-CO—, —C1-2alkyl-NH—CO—CR16R17—NH—, —C1-2alkyl-CO—NH—CR18R19—CO—, —C1-2alkyl-CO—NR20—C1-3alkyl-CO—, or —NR22—CO—C1-3alkyl-NH—; X1 represents a direct bond, O or —O—C1-2alkyl-; X2 represents a direct bond, —CO—C1-2alkyl-, NR12, —NR12—C1-2alkyl-, —O—N?CH— or —C1-2alkyl-; R1 and R2 each independently represents hydrogen or halo; R3 represents hydrogen; R4 represents hydrogen or C1-4alkyloxy; R12 and RType: ApplicationFiled: January 21, 2016Publication date: July 21, 2016Inventors: Eddy Jean Edgard FREYNE, Timothy Pietro Suren PERERA, Peter Jacobus Johannes Antonius BUIJNSTERS, Marc WILLEMS, Gaston Stanislas Marcella DIELS, Werner Constant Johan EMBRECHTS, Peter TEN HOLTE, Frederik Jan Rita ROMBOUTS, Carsten SCHULTZ-FADEMRECHT
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Publication number: 20160207939Abstract: The present invention is to provide a novel compound (I) shown below, having the anti-virus activity; particularly the HIV integrase inhibitory activity, and a drug containing the same, particularly an anti-HIV drug, as well as a process and an intermediate thereof. (wherein Z1 is NR4; R1 is hydrogen or lower alkyl; X is a single bond, a hetero atom group selected from O, S, SO, SO2 and NH, or lower alkylene or lower alkenylene in which the hetero atom group may intervene; R2 is optionally substituted aryl; R3 is hydrogen, a halogen, hydroxy, optionally substituted lower alkyl etc; and R4 and Z2 part taken together forms a ring, to form a polycyclic compound, including e.g., a tricyclic or tetracyclic compound.Type: ApplicationFiled: March 31, 2016Publication date: July 21, 2016Applicants: Shionogi & Co., Ltd., ViiV Healthcare CompanyInventors: Brian A. JOHNS, Takashi KAWASUJI, Teruhiko TAISHI, Yoshiyuki TAODA
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Publication number: 20160207940Abstract: Compounds and pharmaceutical compositions that modulate kinase activity, including PI3 kinase activity, and compounds, pharmaceutical compositions, and methods of treatment of diseases and conditions associated with kinase activity, including PI3 kinase activity, are described herein.Type: ApplicationFiled: December 16, 2015Publication date: July 21, 2016Inventors: Alfredo C. CASTRO, Katrina CHAN, Catherine A. EVANS, Somarajannair JANARDANANNAIR, Andre LESCARBEAU, Liansheng LI, Tao LIU, Yi LIU, Pingda REN, Daniel A. SNYDER, Martin R. TREMBLAY
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Publication number: 20160207941Abstract: The invention relates to a method for the cost-effective and environmentally friendly production of dialkyl indium chloride in high yield and with high selectivity and purity. The dialkyl indium chloride produced according to the invention is particularly suitable, also as a result of the high purity and yield, for the production, on demand, of indium-containing precursors in high yield and with high selectivity and purity. As a result of the high purity, the indium-containing precursors that can be produced are particularly suitable for metal organic chemical vapour deposition (MOCVD) or metal organic vapour phase epitaxy (MOVPE). The novel method according to the invention is characterised by the improved execution of the method, in particular a rapid process control. Owing to targeted and extensive use of raw materials that are cost-effective and have a low environmental impact, the method is also suitable for use on an industrial scale.Type: ApplicationFiled: August 18, 2014Publication date: July 21, 2016Applicant: UMICORE AG & CO. KGInventors: Joerg SUNDERMEYER, Annika FREY, Wolf SCHORN, David GROSSE-HAGENBROCK, Ralf KARCH, Andreas RIVAS-NASS, Eileen WOERNER, Angelino DOPPIU
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Publication number: 20160207942Abstract: The invention relates to a method for the cost-effective and environmentally friendly production of alkyl indium sesquichloride in high yield and with high selectivity and purity. The alkyl indium sesquichloride produced according to the invention is particularly suitable, also as a result of the high purity and yield, for the production, on demand, of indium-containing precursors in high yield and with high selectivity and purity. As a result of the high purity, the indium-containing precursors that can be produced are particularly suitable for metal organic chemical vapour deposition (MOCVD) or metal organic vapour phase epitaxy (MOVPE). The novel method according to the invention is characterised by the improved execution of the method, in particular a rapid process control. Owing to targeted and extensive use of raw materials that are cost-effective and have a low environmental impact, the method is also suitable for use on an industrial scale.Type: ApplicationFiled: August 18, 2014Publication date: July 21, 2016Applicant: UMICORE AG & CO. KGInventors: Joerg Sundermeyer, Annika Frey, Wolf Schorn, Ralf Karch, Andreas Rivas-Nass, Eileen Woerner, Angelino Doppiu
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Publication number: 20160207943Abstract: Provided are methods for purifying N-methyliminodiacetic acid (MIDA) boronates from solution. Also provided are methods for deprotection of boronic acids from their MIDA ligands. The purification and deprotection methods can be used in conjunction with methods for coupling or otherwise reacting boronic acids. Iterative cycles of deprotection, coupling, and purification can be performed to synthesize chemical compounds of interest. The methods are suitable for use in an automated chemical synthesis process. Also provided is an automated small molecule synthesizer apparatus for performing automated synthesis of small molecules using iterative cycles of deprotection, coupling, and purification in accordance with methods of the invention.Type: ApplicationFiled: January 15, 2016Publication date: July 21, 2016Applicant: The Board of Trustees of the University of IllinoisInventors: Martin D. Burke, Eric P. Gillis, Steven G. Ballmer
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Publication number: 20160207944Abstract: Methods for producing functionalized graphene from graphite oxide or graphite are disclosed in which ionic liquids are used as a reaction medium to promote chemical functionalization of the graphene through electrochemically interacted exfoliation of graphene sheets.Type: ApplicationFiled: December 29, 2015Publication date: July 21, 2016Applicant: WASHINGTON STATE UNIVERSITYInventors: Jinwen ZHANG, Yu FU
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Publication number: 20160207945Abstract: The invention includes processes for the synthesis of amphetamine, dexamphetamine, methamphetamine, derivatives of these, including their salts, and novel precursors and intermediates obtained thereby, by synthesizing aziridine phosphoramidate compounds in specified solvents at specified temperatures, and then converting to a novel aryl or aryl-alkyl phosphoramidate precursors using an organometallic compound such as a copper salt, where the novel aryl or aryl-alkyl phosphoramidate precursor is then easily converted to the target compounds using known reactions,Type: ApplicationFiled: March 7, 2016Publication date: July 21, 2016Inventors: HAROLD MECKLER, BRIAN GREGG, JIE YANG
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Publication number: 20160207946Abstract: This disclosure relates to a ligand compound, a catalyst system for olefin oligomerization, and a method for olefin oligomerization using the same. The catalyst system for olefin oligomerization according to the present invention has excellent catalytic activity, and yet, exhibits high selectivity to 1-hexene or 1-octene, thus enabling more efficient preparation of alpha-olefin.Type: ApplicationFiled: November 10, 2014Publication date: July 21, 2016Inventors: Eun Ji SHIN, Yong Ho LEE, Seok Pil SA, Ki Soo LEE
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Publication number: 20160207947Abstract: A method for preparing trishydroxymethyl phosphine from tetrakishydroxymethyl phosphonium salt, the method including at least the steps of continuously feeding a first reaction chamber with, from one hand, at least one tetrakishydroxymethyl phosphonium salt and, from another hand, at least one base, under conditions suitable for a reaction of the tetrakishydroxymethyl phosphonium salt(s) with the base(s), to form a mixture of trishydroxymethyl phosphine and formaldehyde; and continuously removing the formaldehyde.Type: ApplicationFiled: September 17, 2014Publication date: July 21, 2016Applicant: MAGPIE POLYMERSInventors: Steven VAN ZUTPHEN, Vladica BOCOKIC
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Publication number: 20160207948Abstract: The invention relates to phosphohistidine analogues. The invention also relates to antibodies that specifically bind to the analogues and methods of generating said antibodies. In one embodiment of the invention there is provided a phosphohistidine analogue of Formula V: (V) wherein W is selected from H, CO2H or CONH2; and X is selected from CH or N.Type: ApplicationFiled: September 2, 2014Publication date: July 21, 2016Applicant: University of SheffieldInventors: Richard Jackson, Richard Muimo, Matthew Lilley
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Publication number: 20160207949Abstract: The present invention is related to novel cytotoxic agents, pyrrolo[2,1-c][1,4]benzodiazepine (PBD) derivatives, their conjugates with a cell-binding agent, the preparation and the therapeutic uses in the targeted treatment of cancers, autoimmune disorders, and infectious diseases.Type: ApplicationFiled: September 2, 2013Publication date: July 21, 2016Applicant: Hangzhou DAC Biotech Co., LtdInventor: Robert Yongxin Zhao
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Publication number: 20160207950Abstract: The invention relates to a compound characterized by a general formula, wherein OM is an organometallic compound independently selected from the group of an unsubstituted or substituted metal sandwich compound, an unsubstituted or substituted half metal sandwich compound or a metal carbonyl compound, wherein Z is a group described by a general formula wherein with i being or, is a -alkyl with r being or, is a alkyl with t being or, and wherein each RX1 independently from any other is or, and wherein n of and with each independently from any other being hydrogen or an unsubstituted or substituted alkyl and their use in a method for treatment of infections by helminths.Type: ApplicationFiled: September 26, 2014Publication date: July 21, 2016Inventors: Gilles GASSER, Robin B. GASSER, Jeanníne HESS, Abdul JABBAR, Malay PATRA
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Publication number: 20160207951Abstract: The Invention comprises a compound characterized by a general formula (1), RL—OM-RR?? (1) wherein OM is an organometallic compound independently selected from the group of an unsubstituted or substituted metal sandwich compound, an unsubstituted or substituted half metal sandwich compound or a metal carbonyl compound, and wherein at least one of RL and RR is selected from and their use for in a method of treatment of disease, in particular their use against helminths.Type: ApplicationFiled: September 26, 2014Publication date: July 21, 2016Inventors: Gilles GASSER, Robin B. GASSER, Jeannine HESS, Abdul JABBAR, Malay PATRA
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Publication number: 20160207952Abstract: Provided are methods of making compounds having an inhibitory effect on sodium-dependent glucose cotransporter SGLT. The invention also provides synthetic intermediates useful for preparing such compounds.Type: ApplicationFiled: November 19, 2015Publication date: July 21, 2016Inventors: Baihua Xu, Binhua Lv, Ge Xu, Brian Seed, Jacques Roberge
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Publication number: 20160207953Abstract: Compounds of Formula (A) are described herein and the uses thereof for the treatment of diseases, conditions and/or disorders mediated by pharmaceutical compositions and the uses thereof as asialoglycoprotein receptor (ASGPR) targeting agents.Type: ApplicationFiled: April 7, 2016Publication date: July 21, 2016Applicant: Pfizer Inc.Inventors: Spiros Liras, Vincent Mascitti, Benjamin Thuma
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Publication number: 20160207954Abstract: Disclosed is a steviol glycoside referred to as rebaudioside D2. Rebaudioside D2 has five ?-D-glucosyl units connected to the aglycone steviol. Also disclosed are methods for producing rebaudioside D2, a UDP-glycosyltransferase fusion enzyme, and methods for producing rebaudioside D and rebaudioside E.Type: ApplicationFiled: February 5, 2016Publication date: July 21, 2016Inventors: Guohong Mao, Venkata Sai Prakash Chaturvedula, Oliver Yu
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Publication number: 20160207955Abstract: Disclosed is tri- or tetravalent sialic acid derivatives comprising a core moiety to which 3 or 4 sialic acid residues are connected via a linker. Such derivatives inhibit the binding of adenovirus to human cells, whereby infections, such as epidemic keratoconjunctivitis, may be treated or prevented by administration of the tri- or tetravalent sialic acid derivatives.Type: ApplicationFiled: August 28, 2014Publication date: July 21, 2016Applicant: Adenovir Pharma ABInventors: Niklas Arnberg, Rémi Caraballo, Mikael Elofsson
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Publication number: 20160207956Abstract: SCY-078 is a glucan synthase inhibitor with antimicrobial activity. Novel salts and polymorph forms of SCY-078 are disclosed herein. The disclosure also relates to pharmaceutical compositions, methods of use, and methods of preparing the novel salts and polymorphs of SCY-078.Type: ApplicationFiled: January 14, 2016Publication date: July 21, 2016Applicant: SCYNEXIS, INC.Inventor: Yi Zhang
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Publication number: 20160207957Abstract: The present invention relates to peptide modifier compounds of Formula (1), or a salt thereof, wherein: a is an integer from 1 to 10, more preferably from 1 to 3; b is an integer from 0 to 7; Z is a terminal group and Y is a bivalent group. Further aspects of the invention relate to intermediates in the preparation of compounds of Formula (1), and the use of compounds of Formula 1 in the synthesis of peptide derivatives.Type: ApplicationFiled: August 28, 2014Publication date: July 21, 2016Inventors: Kleomenis Barlos, Dimitrios Gatos, Kostas K. Barlos, Zoi Vasileiou
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Publication number: 20160207958Abstract: A method for producing a dipeptide that has a protected N-terminal and is represented by formula (1) or a salt of the dipeptide, said method comprising condensing an ?-monosubstituted amino acid that has a protected N-terminal and is represented by formula (2) or glycine or a salt thereof with a disubstituted amino acid that is represented by formula (3) or a salt thereof in the presence of a condensing agent [in each of the formulae, substituents are as defined in the description or the like].Type: ApplicationFiled: August 20, 2014Publication date: July 21, 2016Applicant: NAGASE & CO., LTD.Inventors: Keisuke MATSUYAMA, Kazuya KODAMA
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Publication number: 20160207959Abstract: An isolated polypeptide comprising a peptide selected from: i) DHX1SDNYT, wherein X1 is L or H (SEQ ID NO:3); ii) a conservative variant of i) iii) a fragment of i) or ii); wherein the conservative variant and/or fragment retains biological activity and the peptide is 15 or less amino acids as well as recombinant cells, and uses thereof.Type: ApplicationFiled: August 27, 2014Publication date: July 21, 2016Inventors: Fackson MWALE, John ANTONIOU, Lisbet HAGLUND, Peter J. ROUGHLEY, Rahul GAWRI, Laura M. EPURE, Michael P. GRANT
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Publication number: 20160207960Abstract: Disclosed are pharmaceutical compositions comprising a CIRP inhibitor. Methods of treating a subject suffering from an inflammatory condition comprising administering to said subject a CIRP inhibitor are also described herein.Type: ApplicationFiled: September 24, 2014Publication date: July 21, 2016Inventor: Ping Wang
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Publication number: 20160207961Abstract: Analogues of cyclosporin-A are disclosed comprising modifications of the substituents as the positions of amino acids 1 and 3, according to the following Formula. The disclosed compounds include compounds having affinity for cyclophilin, including cyclophilin-A, and reduced immunosuppressivity in comparison with cyclosporin-A and analogs thereof modified solely at position 1.Type: ApplicationFiled: October 30, 2015Publication date: July 21, 2016Inventors: Alexander Hegmans, Bruce W. Fenske, Dan J. Trepanier, Mark D. Abel, Daren R. Ure, Shin Sugiyama