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Небесная энциклопедия

Космические корабли и станции, автоматические КА и методы их проектирования, бортовые комплексы управления, системы и средства жизнеобеспечения, особенности технологии производства ракетно-космических систем

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Мониторинг СМИ

Мониторинг СМИ и социальных сетей. Сканирование интернета, новостных сайтов, специализированных контентных площадок на базе мессенджеров. Гибкие настройки фильтров и первоначальных источников.

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Поддерживает ввод нескольких поисковых фраз (по одной на строку). При поиске обеспечивает поддержку морфологии русского и английского языка
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Применить Всего найдено 22044. Отображено 100.
02-02-2012 дата публикации

Modified heparinase iii and methods of sequencing therewith

Номер: US20120027744A1
Автор: Dongfang Liu, Ganesh Venkataraman, Kevin Pojasek, Kristine Holley, Ram Sasisekharan, Yosuf El-Shabrawi, Zachary Shriver
Принадлежит: Massachusetts Institute of Technology

The invention relates to heparinase III and mutants thereof. Modified forms of heparinase III having reduced enzymatic activity which are useful for a variety of purposes, including sequencing of heparin-like glycosaminoglycans (HLGAGs), removing active heparan sulfate from a solution, inhibition of angiogenesis, etc. have been discovered according to the invention. The invention in other aspects relates to methods of treating cancer and inhibiting tumor cell growth and/or metastasis using heparinase III, or products produced by enzymatic cleavage by heparinase III of HLGAGs.

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Номер записи: 1
15-03-2012 дата публикации

Method for refining of high purity of tacrolimus

Номер: US20120065393A1
Автор: Byoung-Taek Choi, Byung-Sik Kim, Kyung-II Jeong, Seong-Seon Yu, Yun-Beom Ham
Принадлежит: Chongkundang Bio Corp

The present invention relates to a process of preparing a highly pure tacrolimus, which comprising a pre-purification process carried out by means of crystallization, and particularly to a process of preparing a highly pure tacrolimus, which comprises a pre-purification process comprising the steps of (a) extracting mycelia cake collected by filtering a tacrolimus-containing oily compound with an organic solvent, (b) concentrating the extract under reduced pressure and (c) crystallizing the concentrate. In addition, a highly pure tacrolimus can be obtained by dissolving the pre-purified crystals in an organic solvent, passing through the solution in an adsorption resin and concentrating the eluate under reduced pressure, followed by crystallization. According to a process of the present invention, Tacrolimus as pure as appropriate for a pharmaceutical purpose can be prepared by a simple process and at a relatively low cost.

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Номер записи: 2
29-03-2012 дата публикации

Antagonists of pcsk9

Номер: US20120076799A1
Автор: Ayesha Sitlani, Carl P. Sparrow, Holly A. Hammond, Jon H. Condra, Shilpa Pandit
Принадлежит: Merck Sharp and Dohme LLC

Antagonists of human proprotein convertase subtilisin-kexin type 9 (“PCSK9”) are disclosed. The disclosed antagonists are effective in the inhibition of PCSK9 function and, accordingly, present desirable antagonists for the use in the treatment of conditions associated with PCSK9 activity. The present invention also discloses nucleic acid encoding said antagonists, vectors, host cells, and compositions comprising the antagonists. Methods of making PCSK9-specific antagonists as well as methods of using the antagonists for inhibiting or antagonizing PCSK9 function are also disclosed and form important additional aspects of the present disclosure.

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Номер записи: 3
29-03-2012 дата публикации

Substituted Pyrazine (Thio)Pyrans with a Herbicidal Action

Номер: US20120077678A1
Автор: Anja Simon, Anna Aleksandra Michrowska, Bernd Sievernich, Dschun Song, Frank Stelzer, Johannes Hutzler, Julia Major, Klaus Grossmann, Klaus Kreuz, Liliana Parra Rapado, Matthias Witschel, Ricarda Niggeweg, Tao QU, Thomas Ehrhardt, Thomas Seitz, Trevor William Newton, William Karl Moberg
Принадлежит: BASF SE

Substituted pyrazines of the formula I in which the variables are defined according to the description, their agriculturally suitable salts, processes and intermediates for preparing the pyrazines of the formula I, compositions comprising them and their use as herbicides, i.e. for controlling harmful plants, and also a method for controlling unwanted vegetation which comprises allowing a herbicidally effective amount of at least one pyrazine compound of the formula I to act on plants, their seed and/or their habitat.

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Номер записи: 4
29-03-2012 дата публикации

Use of a growth-stimulating protein

Номер: US20120077750A1
Автор: Jukka Westermarck, Melissa Junttila, Pietri Puustinen
Принадлежит: Jukka Westermarck, Melissa Junttila, Pietri Puustinen

This invention relates to the inhibition of a newly discovered growth-stimulating protein in an individual. Further, the invention relates to a method for preventing or treating a cancer, or preventing or treating cancer growth, invasion or metastasis, or preventing or treating other hyperproliferative diseases in an individual, by down regulating the expression of said growth-stimulating protein or by inactivating said protein. Still further, the invention concerns a method for diagnosing cancer or other hyperproliferative diseases in an individual based on said growth-stimulating protein.

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Номер записи: 5
05-04-2012 дата публикации

Antagonists of pcsk9

Номер: US20120082680A1
Автор: Ayesha Sitlani, Carl P. Sparrow, Dana D. Wood, Jon H. Condra, Shilpa Pandit, Timothy S. Fisher
Принадлежит: Merck Sharp and Dohme LLC

Antagonists of human proprotein convertase subtilisin-kexin type 9 (“PCSK9”) are disclosed. The disclosed antagonists are effective in the inhibition of PCSK9 function and, accordingly, present desirable antagonists for the use in the treatment of conditions associated with PCSK9 activity. The present invention also discloses nucleic acid encoding said antagonists, vectors, host cells, and compositions comprising the antagonists. Methods of making PCSK9-specific antagonists as well as methods of using the antagonists for inhibiting or antagonizing PCSK9 function are also disclosed and form important additional aspects of the present disclosure.

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Номер записи: 6
10-05-2012 дата публикации

Nematocidal sulfonamides

Номер: US20120114624A1
Автор: Benjamin Kenneth Smith, Brenton Todd Smith, C. Anne Daly, George Philip Lahm, Renee M. Lett
Принадлежит: EI Du Pont de Nemours and Co

Disclosed are compounds of Formula 1, N-oxides, and salts thereof, wherein Z is O or S; and R 1 , R 2 , R 3 , Q and n are as defined in the disclosure. Also disclosed are compositions containing the compounds of Formula 1 and methods for controlling a parasitic nematode comprising contacting the parasitic nematode or its environment with a biologically effective amount of a compound or a composition of the invention.

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Номер записи: 7
10-05-2012 дата публикации

Porphyrin compounds comprising one or more pyridone moieties

Номер: US20120115901A1
Автор: Chuchawin Changtong, John L. Lombardi, Robert E. Connors
Принадлежит: VENTANA RESEARCH Corp

Various porphyrin compounds comprising one or more pyridone moieties, intermediates thereof, compositions thereof, and, methods of making and using thereof.

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Номер записи: 8
31-05-2012 дата публикации

Peptides whose uptake in cells is controllable

Номер: US20120134922A1
Автор: Emilia Olson, Mike Whitney, Quyen Nguyen, Roger Tsien, Tao Jiang
Принадлежит: UNIVERSITY OF CALIFORNIA

Disclosed herein, in certain embodiments, is a selective transport molecule with increased in vivo circulation. In some embodiments, a selective transport molecule disclosed herein has the formula (A—X—B—C)n—M, wherein C is a cargo moiety; A is a peptide with a sequence comprising 5 to 9 consecutive acidic amino acids, wherein the amino acids are selected from: aspartates and glutamates; B is a peptide with a sequence comprising 5 to 20 consecutive basic amino acids; X is a linker; and M is a macromolecular carrier.

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Номер записи: 9
31-05-2012 дата публикации

Synergistic antimicrobial composition

Номер: US20120136010A1
Автор: Emerentiana Sianawati, Sangeeta Ganguly
Принадлежит: Individual

A synergistic antimicrobial composition comprising: (a) 3-iodo-2-propynyl-butylcarbamate; and (b) flumetsulam. A synergistic antimicrobial composition comprising: (a) 3-iodo-2-propynyl-butylcarbamate; (b) diclosulam.

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Номер записи: 10
19-07-2012 дата публикации

Modulators of cell cycle checkpoints and their use in combination with checkpoint kinase inhibitors

Номер: US20120184505A1
Автор: Janeta Popovici-Muller, Kristin E. Rosner, Timothy J. Guzi
Принадлежит: Individual

In its many embodiments, the present invention provides a novel class of pyrimidine analogs as targeted mechanism-based modulators of cell cycle checkpoints. Cancers and/or malignancies can be treated by administration of a cell cycle checkpoint modulator of the invention. Also discussed are suitable combinations of the cell cycle checkpoint modulator with a checkpoint kinase inhibitor to produce synergistic apoptosis in cancer cells. The invention also includes methods of treating cancers by administering the combination of the cell cycle checkpoint modulator and the checkpoint kinase inhibitor, pharmaceutical compositions comprising the cell cycle checkpoint modulator as well as combinations and pharmaceutical kits. An example cell cycle checkpoint modulator is shown below: formula (I).

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Номер записи: 11
02-08-2012 дата публикации

Ubiquitin interacting motif peptides as cancer therapeutics

Номер: US20120197059A1
Автор: HONG Chen, Yunzhou DONG
Принадлежит: Oklahoma Medical Research Foundation

The present invention involves the use peptides comprising ubiquitin interacting motifs (UIMs) alone or in combination with other agents to treat diseases involving neovascularization, such as cancer.

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Номер записи: 12
13-09-2012 дата публикации

Organic compound and photovoltaic device comprising the same

Номер: US20120227802A1
Автор: Alexey Nokel, Pavel Ivan Lazarev, Pavel Khokhlov
Принадлежит: Cryscade Solar Ltd

The present invention provides a organic compound of the general structural formula 1 and photovoltaic device and photovoltaic layer comprising thereof Said organic compound forms rod-like supramolecules and absorbs electromagnetic radiation in at least one predetermined spectral subrange within a wavelength range from 400 to 3000 nm with excitation of electron-hole pairs. The polycyclic core Cor 1 , the bridging group B, and the polycyclic core Cor 2 form a molecular system selected from the list comprising donor-bridge-acceptor-bridge-donor and acceptor-bridge-donor-bridge-acceptor in which a dissociation of excited electron-hole pairs is carried out. A solution of the organic compound or its salt forms a solid photovoltaic layer on a substrate.

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Номер записи: 13
08-11-2012 дата публикации

Fungi antagonistic to xylella fastidiosa

Номер: US20120282233A1
Автор: Mary Caroline Roper, Philippe Rolshausen
Принадлежит: UNIVERSITY OF CALIFORNIA

The disclosure describes fungal organisms and preparations useful for inhibiting infection by Xylella sp. and in the treatment of Pierce's Disease.

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Номер записи: 14
22-11-2012 дата публикации

Device and method for combining a treatment agent and a gel

Номер: US20120296312A1
Автор: Charles D. Claude, Kimchi Tran, Paul J. Kawula, Syed Faiyaz Ahmed Hossainy
Принадлежит: Abbott Cardiovascular Systems Inc

A method including introducing a treatment agent at a treatment site within a mammalian host; and introducing a bioerodable gel material at the treatment site. An apparatus including a first annular member having a first lumen disposed about a length of the first annular member and a first entry port at a proximal end of the first annular member, and a second annular member coupled to the first annular member having a second lumen disposed about a length of the second annular member and a second entry port at a proximal end of the second annular member, wherein the first annular member and the second annular member are positioned to allow a combining of treatment agents introduced through each annular member at the treatment site.

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Номер записи: 15
03-01-2013 дата публикации

Substituted Pyridazines Having Herbicidal Action

Номер: US20130005576A1
Автор: Andree Van Der Kloet, Anja Simon, Anna Aleksandra Michrowska-Pianowska, Dschun Song, Frank Stelzer, Hans Wolfgang Hoeffken, Helmut Kraus, Johannes Hutzler, Julia Major, Klaus Grossmann, Klaus Kreuz, Liliana Parra Rapado, Matthias Witschiel, Ruediger Reingruber, Tao QU, Thomas Ehrhardt, Thomas Mietzner, Thomas Seitz, Trevor William Newton, William Karl Moberg
Принадлежит: BASF SE

Substituted pyridazines of the formula I in which the variables are defined according to the description, processes and intermediates for preparing the compounds of the formula I and their N-oxides, their agriculturally suitable salts, compositions comprising them and their use as herbicides, and also methods for controlling unwanted vegetation.

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Номер записи: 16
17-01-2013 дата публикации

New Chemical Entities To Be Used For Wee1 Inhibition For The Treatment Of Cancer

Номер: US20130018045A1
Автор: Chunqui Lai, Julie M. Miyashiro, Keith W. Woods, Thomas D. Penning
Принадлежит: ABBOTT LABORATORIES

The present invention relates to compounds of formula (I) or pharmaceutical acceptable salts, wherein R 1 , R 2 , R 3 , A, B, and n are defined in the description. The present invention relates also to compositions containing said compounds which are useful for inhibiting kinases such as wee-1 and methods of treating diseases such as cancer.

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Номер записи: 17
21-03-2013 дата публикации

MODULAR SUPRAMOLECULAR APPROACH FOR CO-CRYSTALLIZATION OF DONORS AND ACCEPTORS INTO ORDERED NETWORKS

Номер: US20130069010A1
Автор: Shveyd Alexander K., Stoddart J. Fraser, Stupp Samuel I., Sue Andrew C.H., Tayi Alok S.
Принадлежит: Northwestern University

Organic charge-transfer (CT) co-crystals in a mixed stack system are disclosed, wherein a donor molecule (D) and an acceptor molecule (A) occupy alternating positions (DADADA) along the CT axis. A platform is provided which amplifies the molecular recognition of donors and acceptors and produces co-crystals at ambient conditions, wherein the platform comprises (i) a molecular design of the first constituent (α-complement), (ii) a molecular design of the second compound (β-complement), and (iii) a solvent system that promotes co-crystallization. 1. An organic charge-transfer (CT) co-crystal consisting essentially of an electron acceptor molecule (A) and an electron donor molecule (D) , wherein one of A and D is an α-complement and the other one of A and D is a β-complement , such that the β-complement is incorporated into the α-complement through molecular linkages in a solvent system to form a co-crystalline supramolecular network , wherein one or more of the molecular linkages between the α-complement and the β-complement use adaptive intermolecular recognition to form the one or more molecular linkages , the co-crystal characterized by having a crystal superstructure comprising a mixed stack lattice (DADADA) and a topological hydrogen-bonded network.2. An organic CT co-crystal according to claim 1 , wherein A is a diimide.3. An organic CT co-crystal according to claim 2 , wherein A is selected from the group consisting of 1α claim 2 , 2α claim 2 , 3β and 4β; and D is selected from the group consisting of 5α claim 2 , 6α; 7β claim 2 , 8β claim 2 , 9β claim 2 , 10β claim 2 , 11β and 12β.4. An organic CT co-crystal according to claim 1 , wherein the solvent system is one or more organic solvents.5. An organic CT co-crystal according to claim 4 , wherein the solvent system is selected from the group consisting of dichloroethane/diethyl ether and N-methylpyrrolidone.6. An organic CT co-crystal according to claim 1 , wherein the α-complement has an α′-arm that is a ...

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Номер записи: 18
21-03-2013 дата публикации

5,5-FUSED ARYLENE OR HETEROARYLENE HEPATITIS C VIRUS INHIBITORS

Номер: US20130071352A1
Автор: Alexandre Francois-Rene, Brandt Guillaume, Convard Thierry, Da Costa Daniel, Derock Michel, Dousson Cyril B., Dukhan David, Paparin Jean-Laurent, Parsy Christophe Claude, Pierra Claire, Rahali Houcine, Surleraux Dominique
Принадлежит: IDENIX PHARMACEUTICALS, INC.

Provided herein are 5,5-fused heteroarylene hepatitis C virus inhibitor compounds, for example, of Formula I, IA, or IB, pharmaceutical compositions comprising the compounds, and processes of preparation thereof. Also provided are methods of their use for the treatment of an HCV infection in a host in need thereof. 6. The method of claim 1 , wherein Uis S.7. The method of claim 1 , wherein Wis S.8. The method of claim 1 , wherein Wis O.9. The method of claim 1 , wherein Wis N.10. The method of claim 1 , wherein U claim 1 , W claim 1 , Xand Xare C claim 1 , and Vand Vare each independently CR.17. The method of claim 1 , wherein u is 1.18. The method of claim 1 , wherein u is 2.26. The method of claim 1 , wherein Ris —C(O)R claim 1 , —C(O)CH(NRR)R claim 1 , —C(O)CH[N(C(O)R)R]R claim 1 , —C(O)CH[N(C(O)OR)R]R claim 1 , or —C(O)CH[N(C(O)NRR)R]R.27. The method of claim 26 , wherein Ris —C(O)CH[N(C(O)OR)R]R.28. The method of claim 1 , wherein Ris —C(O)R claim 1 , —C(O)CH(NRR)R claim 1 , —C(O)CH[N(C(O)R)R]R claim 1 , —C(O)CH[N(C(O)OR)R]R claim 1 , or —C(O)CH[N(C(O)NRR)R]R.29. The method of claim 28 , wherein Ris —C(O)CH[N(C(O)OR)R]R.30. The method of claim 3 , wherein each Ris independently hydrogen or —C(O)OR.31. The method of claim 1 , wherein each Ris independently hydrogen claim 1 , methyl claim 1 , isopropyl claim 1 , 2-methylpropyl claim 1 , 1-methylpropyl claim 1 , 2-methylthioethyl claim 1 , phenyl claim 1 , benzyl claim 1 , 3-indolylmethyl claim 1 , hydroxymethyl claim 1 , 1-hydroxyethyl claim 1 , sulfhydrylmethyl claim 1 , 4-hydroxybenzyl claim 1 , aminocarbonylmethyl claim 1 , 2-(aminocarbonyl)ethyl claim 1 , carboxymethyl claim 1 , 2-carboxyethyl claim 1 , 4-aminobutyl claim 1 , 3-guanidinopropyl claim 1 , or 5-imidazolylmethyl.32. The method of claim 1 , wherein Ris methyl claim 1 , ethyl claim 1 , propyl claim 1 , or butyl.33. The method of claim 1 , wherein Ris hydrogen.34. The method of claim 1 , wherein Rand Rtogether with the C and N atoms to which they ...

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Номер записи: 19
21-03-2013 дата публикации

Spirooxazine radical derivatives and reversible isomerization reaction

Номер: US20130072678A1
Автор: Atsumasa Sawada
Принадлежит: NEC Corp

The present invention can provide new spirooxazine radical derivatives of the following general formula (1) which have chromic property enabling the distinction between the radical species and the cation species on the basis of absorption wavelength:

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Номер записи: 20
21-03-2013 дата публикации

Method for optimising gene expression using synonymous codon optimisation

Номер: US20130074218A1
Автор: Ian Hector Frazer
Принадлежит: University of Queensland UQ

The present invention discloses a method for modulating the quality of a selected phenotype that is displayed by an organism or part thereof and that results from the expression of a polypeptide-encoding polynucleotide by replacing at least one codon of that polynucleotide with a synonymous codon that has a higher or lower preference of usage by the organism or part thereof to produce the selected phenotype than the codon it replaces. The present invention is also directed to the use of a codon-modified polynucleotide so constructed for modulating the quality of a selected phenotype displayed by an organism or part thereof.

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Номер записи: 21
28-03-2013 дата публикации

GYRASE INHIBITORS

Номер: US20130079323A1
Автор: Bensen Daniel, Chen Zhiyong, Creighton Christopher J., Finn John, Hilgers Mark, Lam Thanh To, Li Xiaoming, Tari Leslie William, Trzoss Michael, Zhang Junhu
Принадлежит: TRIUS THERAPEUTICS, INC.

Novel gyrase inhibitors and related compositions and methods are useful for impeding bacterial growth. Compounds of Formula (I), are disclosed: Formula (I), wherein Y is N or CH; Z is N or CR; Ris H, a substituted or unsubstituted hydrocarbyl residue (1-3C) containing 0-2 heteroatoms selected from O, S and N, or is an inorganic residue; L is O, S, NR, or CRR; Ris H or Calkyl; Rand Rare each independently H or Calkyl; Ris H, a hydrocarbyl residue (1-40C) containing 0-10 heteroatoms selected from O, S and N optionally substituted with an inorganic residue; Ris H, an inorganic residue, or a hydrocarbyl residue (1-30C) containing 0-12 heteroatoms selected from O, S and N and containing 0-10 inorganic residues, wherein Rand Rtogether may join to form a fused ring; and Ris selected from the group consisting of H, Calkyl, Calkenyl, Calkynyl, halo Calkyl, halo Calkenyl, halo Calkynyl, Chydroxyalkyl, Calkyl chloride, Calkenyl chloride, and Calkynyl chloride; or a pharmaceutically-acceptable salt, ester, or prodrug thereof. 2. The compound of claim 1 , whereinY is N; and{'sub': '2', 'L is O, S, NH, or CH.'}3. The compound of claim 1 , wherein Z is CR claim 1 , wherein Ris selected from the group consisting of hydrogen claim 1 , halo claim 1 , unsubstituted Calkyl claim 1 , and Calkyl substituted with one or more substituents selected from the group consisting of ═O claim 1 , halo claim 1 , NH claim 1 , NHCH claim 1 , ≡N claim 1 , and Calkenyl claim 1 , wherein Rand Rtogether may join to form a fused ring.4. The compound of claim 1 , wherein Ris methyl claim 1 , C(O)CH claim 1 , C(O)NH claim 1 , CHOH claim 1 , CF claim 1 , CN claim 1 , CHF claim 1 , CHO claim 1 , acetyl claim 1 , Cl or Br.5. The compound of claim 1 , wherein Rcomprises at least one aryl or heteroaryl moiety.6. The compound of claim 1 , wherein the at least one aryl or a heteraryl moiety of Ris directly linked to L.7. The compound of claim 1 , wherein the at least one aryl or heteraryl moiety of Ris substituted ...

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Номер записи: 22
28-03-2013 дата публикации

BICYCLIC METHYLENE AZIRIDINES AND REACTIONS THEREOF

Номер: US20130079511A1
Автор: ADAMS Christopher S., Boralsky Luke, Hershberger John, RIGOLI Jared, SCHOMAKER Jennifer
Принадлежит: WISCONSIN ALUMNI RESEARCH FOUNDATION

The oxidative functionalization of olefins is a common method for the formation of vicinal carbon-heteroatom bonds. However, oxidative methods to transform allenes into synthetic motifs containing three contiguous carbon-heteroatom bonds are much less developed. The use of bicyclic methylene aziridines (MAs), prepared via intramolecular allene aziridination, as scaffolds for functionalization of all three allene carbons, among other reactions, is described herein. 1. A method comprising forming a bicyclic methylene aziridine by an intramolecular allene aziridination reaction;{'sub': '2', 'wherein an allene group is tethered to an —NHgroup, and the amino group is separated from the proximal allene carbon by 3, 4, 5, or 6 atoms linearly;'}the method comprising combining the allene, an effective rhodium catalyst, a solvent, and an oxidant, to provide a reaction mixture, thereby initiating an intramolecular allene aziridination reaction, to provide a bicyclic methylene aziridine.2. The method of wherein the rhodium catalyst is Rh(esp)where esp is α claim 1 ,α claim 1 ,α′ claim 1 ,α′-tetramethyl-1 claim 1 ,3-benzenedipropionate claim 1 , or Rh(TPA)where TPA is triphenylacetate.3. The method of wherein the oxidant is a hypervalent iodide oxidant or a one-electron cerium or lead oxidant.4. The method of wherein the oxidant is PhIO claim 3 , PhI(OAc) claim 3 , PhI(OPiv) claim 3 , Ce(SO) claim 3 , or Pb(OAc).5. The method of wherein the reaction mixture further comprises a drying agent claim 4 , an acid neutralizing agent claim 4 , or a combination thereof.6. The method wherein the aziridine nitrogen of the bicyclic methylene aziridine is substituted by an electron-withdrawing group.7. The method of wherein the allene is mono-substituted claim 1 , di-substituted claim 1 , tri-substituted claim 1 , or tetra-substituted.9. The method of further comprising contacting the bicyclic methylene aziridine with a nucleophile to provide a nucleophile-addition product.10. The method of ...

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Номер записи: 23
04-04-2013 дата публикации

AMINOACID DERIVATIVES, THEIR PROCESS OF PREPARATION AND THEIR THERAPEUTICAL USES AS INHIBITORS OF ONCOGENIC SIGNALS BY THE MET FAMILY

Номер: US20130085143A1
Автор: BOSCH Joan, COLOMBO Francesco, DONO Rosanna, LEROUX Vincent, MAIGRET Bernard, MAINA Flavio, PASSARELLA Daniele, PICCOLO Oreste
Принадлежит:

Novel amino acids derivatives, in particular some amino acid amides derivatives, their process of preparation and their use for inhibiting Met-triggered disorders, in particular cancer. 2. The compounds according to in which m=0 or 1 claim 1 , p=0 claim 1 , r=0 and T=H.4. The compounds according to claim 1 , in which W═W═H.5. The compounds according to claim 1 , in which n=0 or 1 and X is H or an optionally substituted aryl or heteroaryl.6. The compounds according to claim 1 , in which X is phenyl.7. The compounds according to claim 1 , in which Y is an -alkylaryl claim 1 , such as —CHaryl claim 1 , where the aryl is optionally substituted by one or more identical or different substituents chosen from halogen claim 1 , OR claim 1 , NRR′ claim 1 , SR claim 1 , alkyl claim 1 , CN claim 1 , perhalogenoalkyl.13. The process according to claim 10 , further comprising the step of isolating the obtained compound.14. A pharmaceutical composition comprising a compound of formula (I) as defined in and a pharmaceutically acceptable carrier.15. The composition according to where said carrier is a cyclodextrin.16. A compound of formula (I) as defined in for inhibiting the Met family.17. A compound of formula (I) as defined in for treating and/or preventing Met family-triggered disorders.18. A compound of formula (I) according to for treating and/or preventing cancer(s) claim 17 , infections diseases and pain.19. A combination of a compound as defined in with one or more agent(s) and/or pharmaceutical composition(s) useful for the treatment and/or prevention of cancer(s) claim 1 , infections diseases and pain.20. A compound of formula (I) as defined in for treating and/or preventing distinct tumours characterised by alteration of selective signals. The present invention is related to novel aminoacids derivatives, pharmaceutical compositions comprising the same, processes for the preparation of said derivatives and uses of said compositions. Particularly, the present invention ...

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Номер записи: 24
04-04-2013 дата публикации

THIAZOLOPYRIDINE SIRTUIN MODULATING COMPOUNDS

Номер: US20130085155A1
Автор: Disch Jeremy, Ng Pui Yee, OALMANN Christopher, Perni Robert
Принадлежит: Sirtris Pharmaceuticals

Provided herein are novel sirtuin-modulating compounds of Structural Formula (Ia) and methods of use thereof. The sirtuin-modulating compounds may be used for increasing the lifespan of a cell, and treating and/or preventing a wide variety of diseases and disorders including, for example, diseases or disorders related to aging or stress, diabetes, obesity, neurodegenerative diseases, cardiovascular disease, blood clotting disorders, inflammation, cancer, and/or flushing as well as diseases or disorders that would benefit from increased mitochondrial activity. Also provided are compositions comprising a sirtuin-modulating compound in combination with another therapeutic agent. 110-. (canceled)12. The pharmaceutical composition for topical administration of claim 11 , comprising 0.001 to 10% by weight of the compound.13. The pharmaceutical composition for topical administration of claim 12 , comprising 0.1 to 5% by weight of the compound.14. The pharmaceutical composition for topical administration of claim 11 , comprising 0.25 to 75% by weight of the compound.15. The pharmaceutical composition for topical administration of claim 14 , comprising 0.25 to 30% by weight of the compound.16. The pharmaceutical composition for topical administration of claim 15 , comprising 0.25 to 15% by weight of the compound.17. The pharmaceutical composition for topical administration of claim 16 , comprising 1.0 to 10% by weight of the compound.18. The pharmaceutical composition for topical administration of claim 11 , wherein the topical carrier is selected from water claim 11 , alcohol claim 11 , glycerin claim 11 , mineral oil claim 11 , silicone claim 11 , petroleum jelly claim 11 , lanolin claim 11 , fatty acids claim 11 , vegetable oil claim 11 , paraben claim 11 , and wax.19. The pharmaceutical composition for topical administration of claim 11 , wherein the composition is in a form selected from an ointment claim 11 , a lotion claim 11 , a cream claim 11 , a microemulsion claim ...

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Номер записи: 25
11-04-2013 дата публикации

POLYMORPHIC FORMS OF RIFAXIMIN

Номер: US20130090348A1
Автор: Kothakonda Kiran Kumar, Rey Allan W.
Принадлежит: APOTEX PHARMACHEM INC.

Provided for in the instant application are two additional polymorphic forms of rifaximin; namely substantially pure APO-I and APO-II. Also provided are processes for preparing substantially pure APO-I and APO-II. Rifaximin is a non-aminoglycoside antibiotic that has previously been found to be useful for the treatment of traveller's diarrhea caused by bacteria, as well as in the treatment of irritable bowel syndrome, diverticular disease, hepatic encephalopathy, pyogenic skin infections and as an antibacterial prophylactic prior to colon surgery. 1. Substantially pure polymorphic form APO-I of Rifaximin.2. The polymorphic form APO-I of Rifaximin of having a PXRD diffractogram comprising peaks claim 1 , in terms of degrees 2-theta claim 1 , at approximately 6.32 claim 1 , 6.70 claim 1 , 8.36 claim 1 , 9.57 claim 1 , 12.67 and 18.733. The polymorphic form APO-I of Rifaximin of having a PXRD diffractogram comprising peaks claim 1 , in terms of degrees 2-theta claim 1 , at approximately 6.32 claim 1 , 6.52 claim 1 , 6.54 claim 1 , 6.70 claim 1 , 8.36 claim 1 , 8.38 claim 1 , 9.57 claim 1 , 12.67 claim 1 , 12.68 claim 1 , 18.73 and 24.94.4. (canceled)5. The polymorphic form APO-I of Rifaximin of having a PXRD diffractogram as depicted in .6. The polymorphic form APO-I of Rifaximin of having a 1% KBr FTIR spectrum comprising peaks claim 1 , in terms of cm claim 1 , at approximately 3427.9 claim 1 , 2968.1 claim 1 , 2934.1 claim 1 , 1714.2 1647.7 claim 1 , 1587.3 claim 1 , 1507.1 claim 1 , 1373.7 claim 1 , 1338.1 claim 1 , 1226.4 claim 1 , 1157.0 claim 1 , and 1124.1.78.-. (canceled)9. The polymorphic form APO-I of Rifaximin of having a FTIR spectrum as depicted in .10. A pharmaceutical formulation comprising the polymorphic form APO-I of Rifaximin of and a pharmaceutically acceptable excipient.11. A process for preparation of a substantially pure polymorphic form APO-I of Rifaximin comprising:dissolving Rifaximin in a first organic solvent thereby forming a Rifaximin ...

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Номер записи: 26
11-04-2013 дата публикации

Method for protecting rice from being infected by fungi

Номер: US20130090360A1
Автор: Stierl Reinhard
Принадлежит: BASF SE

Method for protecting rice from being infected by harmful fungi, wherein the fungi, their habitat, rice plants, their seed, rice plant propagation material or the soil on which rice is grown or intended to be grown, is treated with epoxiconazole and tricyclazole in synergistically effective amounts; use of a composition comprising epoxiconazole, tricyclazole and optionally a further commercially available fungicide, for preparing a composition suitable for protecting rice from being infected by harmful fungi. 17-. (canceled)8. A method for protecting rice from being infected by phytopathogenic harmful fungi , wherein the fungi , their habitat , rice plants , their seed , rice plant propagation material or the soil on which rice is grown or intended to be grown , is treated with epoxiconazole and tricyclazole in synergistically effective amounts.9Pyricularia griseaPyricularia oryzaeRhizoctonia solaniPellicularia sasakiiBipolaris oryzae, Microdochium oryzae, Ustilaginoidea virens, Curvularia lunata, Cercospora orzyae, Helminthosporium oryzaeFusarium. The method according to claim 8 , wherein the phytopathogenic harmful fungi to be controlled are selected from the group (syn. ). (syn in rice ) claim 8 , and spp.10. The method according to claim 8 , wherein an aqueous preparation of a formulation comprising epoxiconazole and tricyclazole is applied to the above-ground parts of the rice plants.11. A method according to claim 8 , whereas plant propagation material is treated.12. The method according to claim 8 , wherein a combination of epoxiconazole claim 8 , tricyclazole and a further claim 8 , commercially available fungicide is employed.13. The method according to claim 8 , wherein the active ingredients are applied simultaneously claim 8 , that is jointly or separately claim 8 , or in succession.14. The method according to claim 8 , wherein the combination is applied in an amount of from 20 g/ha to 1000 g/ha.15. A method for protecting rice from being infected by ...

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Номер записи: 27
18-04-2013 дата публикации

Nematicidal Mixtures for Use in Sugar Cane

Номер: US20130096077A1
Автор: Azenha Antonio Cesar, Prade Alexander Guttenkunst
Принадлежит: BASF SE

A method for the synergistic plant nematode control in sugar cane with a mixture of fipronil and abamectin comprising fipronil and abamectin in a ratio by weight of from 1:10 to 10:1, wherein the mixture is applied to sugar cane in furrow, a method for the synergistic plant nematode control in sugar cane with a mixture of fipronil and abamectin comprising fipronil and abamectin in a ratio by weight of from 1:10 to 10:1, wherein the mixture is applied to plant propagation materials of sugar cane, and a method which combines synergistic plant nematode control with (preferably synergistic) improvement of the plant health of sugar cane plants. 114-. (canceled)15. A method for the synergistic plant nematode control in sugar cane with a mixture of fipronil and abamectin comprising fipronil and abamectin in a ratio by weight of from 1:10 to 10:1 , wherein the mixture is applied to sugar cane in furrow.16. A method for the synergistic plant nematode control in sugar cane with a mixture of fipronil and abamectin comprising fipronil and abamectin in a ratio by weight of from 1:10 to 10:1 , wherein the mixture is applied to plant propagation materials of sugar cane.17MeloidogynePratilenchusHelicotylencusParatrichodorus. The method according to claim 15 , wherein the plant nematodes are selected from the group consisting of species claim 15 , species claim 15 , species claim 15 , and species.18. The method according to claim 15 , wherein the plant health of sugar cane is improved.19. The method according to wherein the plant health of sugar cane is improved synergistically.20. The method according to wherein improved plant health is an improved sugar cane plant property selected from the group consisting of more developed root system claim 15 , improved root growth claim 15 , improved root size maintenance claim 15 , improved root effectiveness claim 15 , and tillering increase.21. The method according to wherein improved plant health is an improved sugar cane plant property ...

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Номер записи: 28
18-04-2013 дата публикации

BICYCLIC HETEROCYCLE DERIVATIVES AND METHODS OF USE THEREOF

Номер: US20130096141A1
Автор: Liu Hong, Neustadt Bernard R.
Принадлежит:

Compounds of structural formula I: are GPR119 agonists and are useful for the treatment, control or prevention of disorders responsive to agonism of GPR119, such as metabolic-related disorders such as type I diabetes, type II diabetes, inadequate glucose tolerance, insulin resistance, hyperglycemia, hyperlipidemia, hypertriglyceridemia, hypercholesterolemia, dyslipidemia or syndrome X. The compounds are also reported as being useful for controlling weight gain, controlling food intake, and inducing satiety in mammals. 142-. (canceled)44. The compound of claim 43 , wherein A is —O—.47. The compound of claim 43 , wherein W is —C(O)O— or —C(O)—.48. The compound of claim 43 , wherein W is a bond.49. The compound of claim 43 , wherein Ris C-Calkyl claim 43 , haloalkyl claim 43 , heteroaryl or cycloalkyl.50. The compound of claim 43 , wherein Ar is aryl or heteroaryl.51. The compound of claim 43 , wherein Ar is phenyl.52. The compound of claim 43 , wherein Ar is pyridyl.54. The compound of claim 43 , wherein J and M are each —N—.55. The compound of claim 43 , wherein A is —O— and W is —C(O)O— claim 43 , a bond or —CH—.58. A compound of or pharmaceutically acceptable salt thereof claim 57 , wherein X is —S—.59. A compound of or pharmaceutically acceptable salt thereof claim 57 , wherein X is —NC-Calkyl-.61. A pharmaceutical composition comprising a compound of claim 43 , or a pharmaceutically acceptable salt thereof claim 43 , and a pharmaceutically acceptable carrier.62. A method for the treatment of a condition selected from the group consisting of obesity and diabetes comprising administering to an individual a pharmaceutical composition comprising the compound of . The present invention relates to bicyclic heterocycle derivatives, compositions comprising a bicyclic heterocycle derivative, and methods of using the bicyclic heterocycle derivatives for treating or preventing obesity, diabetes, a diabetic complication, a metabolic disorder, a cardiovascular disease or a ...

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Номер записи: 29
18-04-2013 дата публикации

DUAL-ACTING ANTIHYPERTENSIVE AGENTS

Номер: US20130096162A1
Автор: Allegretti Paul, Choi Seok-ki, Fatheree Paul R., Gendron Roland, Jendza Keith, McKinnell Robert Murray, McMurtrie Darren, Olson Brooke
Принадлежит:

The invention is directed to compounds having the formula: 2. The compound of claim 1 , wherein r is 1.3. (canceled)5. The compound of claim 4 , wherein Ris selected from —COOH claim 4 , —SONHR claim 4 , and tetrazol-5-yl.711-. (canceled)12. The compound of claim 1 , wherein Ris selected from —Calkyl and —Calkylene-O—Calkylene-R claim 1 , where Ris —Calkyl.13. The compound of claim 12 , wherein Ris selected from —Calkyl and —O—Calkyl.14. The compound of claim 1 , wherein X is —Calkylene- claim 1 , 1 to 4-CH-moieties in the alkylene are replaced with a —NR—C(O)— or —C(O)—NR— moiety claim 1 , and Ris selected from H and —OH.15. The compound of wherein X is selected from: —C(O)NH—; —CH—NHC(O)—; —C(O)NH—CH—; —C(O)NH—NHC(O)—; —CH═C(—CH-2-thiophene)-C(O)NH—; —(CH)—NHC(O)—; —C(O)NH—CH—CH(COOH)—CH—; —C(O)NH—CH(benzyl)-CH—NHC(O)—; —C(O)NH—CH(benzyl)-CH—C(O)NH—; —CH—NHC(O)—CH—NHC(O)—; —CH—NHC(O)-cyclohexylene-NHC(O)—; —CH—N(OH)C(O)-cyclohexylene-NHC(O)—; —CH—NHC(O)—CH—CH(COOH)—NHC(O)—; —CH—NHC(O)—(CH)—NHC(O)—; —C(O)NH—(CH)—C(O)N(OH)—CH—; —C(O)NH—(CH)—CH(COOH)—NHC(O)—; —C(O)NH—(CH)—NHC(O)—; —CH—NHC(O)—(CH)—CH(COOH)—NHC(O)—; —C(O)NH—(CH)—CH(COOH)—NHC(O)—; —C(O)NH—(CH)—NHC(O)—CH—NHC(O)—; —C(O)NH—(CH)—NHC(O)-cyclohexylene-NHC(O)—; —CH—NHC(O)—(CH)—NHC(O)—; —C(O)NH—(CH)—CH(COOH)—NHC(O)—; —CH—NHC(O)—(CH)—NHC(O)-cyclohexylene-NHC(O)—; —CH—C(O)NH—(CH)—NHC(O)-cyclohexylene-NHC(O)—; —C(O)NH—(CH)—NHC(O)—CH—NHC(O)—; —C(O)NH—(CH)—NHC(O)-cyclohexylene-NHC(O)—; —CH—NHC(O)—(CH)—NHC(O)—; —CH—NHC(O)—(CH)—NHC(O)-cyclohexylene-NHC(O)—; —C(O)NH—(CH)—NHC(O)-cyclohexylene-NHC(O)—; and —CH—NHC(O)—(CH)—NHC(O)-cyclohexylene-NHC(O)—.16. The compound of claim 15 , wherein X is selected from —C(O)NH— and —CH—NHC(O)—.17. The compound of claim 1 , wherein Ris selected from —Calkylene-SR claim 1 , —Calkylene-C(O)NRR claim 1 , —Calkylene-NR—C(O)R claim 1 , —NH—Calkylene-P(O)(OR) claim 1 , —Calkylene-P(O)ORR claim 1 , —Calkylene-CHR—COOH claim 1 , and —Calkylene-C(O)NR—CHR—COOH; Ris H claim 1 , Ris —OH claim 1 ...

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Номер записи: 30
18-04-2013 дата публикации

ORGANIC SEMICONDUCTIVE MATERIAL PRECURSOR CONTAINING DITHIENOBENZODITHIOPHENE DERIVATIVE, INK, INSULATING MEMBER, CHARGE-TRANSPORTING MEMBER, AND ORGANIC ELECTRONIC DEVICE

Номер: US20130096320A1
Автор: Goto Daisuke, Kato Takuji, Matsumoto Shinji, Mohri Masataka, Okada Takashi, Sagisaka Toshiya, Shinoda Masato, TANO Takanori, YAMAMOTO Satoshi, Yutani Keiichiro
Принадлежит:

An organic semiconductive material precursor containing a dithienobenzodithiophene derivative expressed by General Formula I: in General Formula I, X and Y represent groups bonded together, upon application of external stimulus, to form X—Y which is eliminated from the compound expressed by General Formula I; Rand Reach represent a substituted or unsubstituted alkyl group, or a substituted or unsubstituted aryl group; and Rto Reach represent a hydrogen atom, a substituted or unsubstituted alkyl group, a substituted or unsubstituted alkoxy group, a substituted or unsubstituted alkylthio group, or a substituted or unsubstituted aryl group. 2. The organic semiconductive material precursor according to claim 1 ,wherein a first group of either X or Y is a hydrogen atom, anda second group of either X or Y that is different from the first group is a hydroxyl group or a group having an ether structure, an ester structure, or a thioester structure.67-. (canceled)8. The organic semiconductive material precursor of claim 1 , wherein the precursor is soluble in at least one solvent selected from the group consisting of dichloromethane claim 1 , tetrahydrofuran claim 1 , chloroform claim 1 , toluene claim 1 , mesitylene claim 1 , ethyl benzoate claim 1 , dichlorobenzene claim 1 , and xylene.9. The organic semiconductive material precursor of claim 1 , wherein Rand Rare each independently a substituted or unsubstituted aryl group.10. The ink of claim 4 ,wherein a first group of either X or Y is a hydrogen atom, anda second group of either X or Y that is different from the first group is a hydroxyl group or a group having an ether structure, an ester structure, or a thioester structure.12. The insulating member of claim 5 ,wherein a first group of either X or Y is a hydrogen atom, anda second group of either X or Y that is different from the first group is a hydroxyl group or a group having an ether structure, an ester structure, or a thioester structure. The present invention ...

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Номер записи: 31
25-04-2013 дата публикации

USE OF A NATURAL METABOLITE TO INCREASE CROP PRODUCTION

Номер: US20130102465A1
Автор: Lovatt Carol J.
Принадлежит: The Regents of the University of California

Described are compositions and methods to increase bud break in order to increase aspects of one or both of plant vegetative and reproductive growth, by use of a natural metabolite. In particular, the present disclosure provides a natural metabolite either alone or as part of a fertilizer blend to increase crop production. Additionally the present disclosure provides a natural metabolite in combination with one or both of a plant growth regulator and a bio stimulant to increase crop production. 1. A method of increasing crop production , comprising administering to a crop plant a composition comprising an effective amount of a purified natural compound to increase the crop production of the crop plant , wherein the natural compound is selected from the group consisting of adenosine , an adenosine phosphate , inosine , an inosine phosphate , adenine , hypoxanthine , xanthine , and combinations thereof.2. The method of claim 1 , wherein the natural compound comprises 9-beta-D-adenosine.3. The method of claim 1 , wherein the natural compound comprises one or more of the group consisting of adenosine monophosphate claim 1 , adenosine diphosphate claim 1 , adenosine triphosphate claim 1 , inosine claim 1 , inosine monophosphate claim 1 , inosine diphosphate claim 1 , inosine triphosphate claim 1 , adenine claim 1 , hypoxanthine claim 1 , and xanthine.4. The method of claim 2 , wherein the composition further comprises one or more of a fertilizer claim 2 , a plant growth regulator claim 2 , and a biostimulant.5. The method of claim 4 , wherein the fertilizer is selected from the group consisting of nitrogen claim 4 , potassium claim 4 , magnesium claim 4 , phosphorus claim 4 , calcium claim 4 , sulfur claim 4 , iron claim 4 , boron claim 4 , chlorine claim 4 , manganese claim 4 , zinc claim 4 , copper claim 4 , molybdenum claim 4 , nickel claim 4 , cobalt claim 4 , silicon claim 4 , selenium claim 4 , and combinations thereof.6. The method of claim 2 , wherein the crop ...

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Номер записи: 32
02-05-2013 дата публикации

MITOTIC KINESIN INHIBITORS AND METHODS OF USE THEREOF

Номер: US20130109656A1
Автор: Allen Shelley, Corrette Christopher P., DeLisle Robert Kirk, Hans Jeremy, Laird Ellen, Lyssikatos Joseph P., Robinson John E., Voegtli Walter C., Wallace Eli M., Zhao Qian
Принадлежит:

This invention relates to inhibitors of mitotic kinesins, particularly KSP, and methods for producing these inhibitors. The invention also provides pharmaceutical compositions comprising the inhibitors of the invention and methods of utilizing the inhibitors and pharmaceutical compositions in the treatment and prevention of various disorders. 23. The compound of claim 1 , wherein Ris alkyl optionally substituted with OR claim 1 , NRR claim 1 , NRC(═O)(CH)R claim 1 , NRSOR claim 1 , heterocyclyl claim 1 , —OP(═O)(OR) claim 1 , an amino acid residue claim 1 , a dipeptide or a tripeptide claim 1 , or Ris a heterocyclyl.24. The compound of claim 1 , wherein Ris (CH)—OH claim 1 , (CH)—OH claim 1 , (CH)—NH claim 1 , (CH)—NH claim 1 , (CH)—NH claim 1 , (CH)—NHCH(CH) claim 1 , (CH)—NHMe claim 1 , (CH)—NMe claim 1 , (CH)—NMe claim 1 , (CH)—NHMe claim 1 , (CH)NHC(═O)Me claim 1 , (CH)NHC(═O)CH(CH) claim 1 , (CH)NHC(═O)CHCHNMe claim 1 , (CH)NHSOMe claim 1 , (CH)-(pyrrolidin-1-yl) claim 1 , (CH)-(piperidin-1-yl) claim 1 , (CH)-(4-methylpiperidin-1-yl) claim 1 , (CH)-(morpholin-4-yl) claim 1 , (CH)-(pyrrolidin-2-yl) claim 1 , (CH)NH(C═O)CH(Me)NH(C═O)CH(Me)NH claim 1 , (CH)—OPOH claim 1 , CH—O—CHOMe or piperidin-4-yl.25. The compound of claim 1 , wherein Ris (CH)—NH.26. The compound of claim 1 , wherein Ris Z—NR—C(═NR)R claim 1 , Z—NR—C(═NR)NRR claim 1 , Z—C(═NR)NRR claim 1 , Z—O—NRC(═NR)NRR claim 1 , Z—O—NR claim 1 , —C(═NR)R claim 1 , Z—NR—NR—C(═NR)R claim 1 , or Z—NR—NR—C(═NR)NRR.27. The compound of claim 1 , wherein Aris phenyl optionally substituted with one or more groups independently selected from halogen claim 1 , alkyl claim 1 , —ORor —NROR; or Aris a heteroaryl selected from thiophenyl or pyridyl claim 1 , wherein said pyridyl is optionally substituted independently with one or more halogen.28. The compound of claim 1 , wherein Aris phenyl claim 1 , 2 claim 1 ,4-difluorophenyl claim 1 , 2-fluorophenyl claim 1 , 3-fluorophenyl claim 1 , 2-chlorophenyl claim 1 , 3- ...

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Номер записи: 33
02-05-2013 дата публикации

PROCESS FOR MAKING THIENOPYRIMIDINE COMPOUNDS

Номер: US20130109852A1
Автор: Babu Srinivasan, CHENG Zhigang, REYNOLDS Mark E., SAVAGE Scott J., Tian Qingping, Yajima Herbert
Принадлежит: Genentech, Inc.

The invention provides processes of preparing, separating, and purifying PI3K inhibitor, Formula I and II compounds, and novel intermediates for preparing Formula I and II compounds. 1. The compound selected from 14 and 14A This application is a divisional of U.S. Ser. No. 12/739,434 filed 29 Jul. 2010, which is a National Stage Application under 35 U.S.C. §371 and claims the benefit of priority to International Application No. PCT/US2008/081204 filed on 24 Oct. 2008, which claims the benefit under 35 USC §119(e) of U.S. Provisional Application Ser. No. 60/982,562 filed on 25 Oct. 2007, each of which are incorporated by reference in entirety.The invention relates generally to processes for making and purifying thienopyrimidine compounds with anti-cancer activity and more specifically to compounds which inhibit PI3 kinase activity.Phosphatidylinositol (hereinafter abbreviated as “PI”) is one of a number of phospholipids found in cell membranes. In recent years it has become clear that PI plays an important role in intracellular signal transduction. Cell signaling via 3′-phosphorylated phosphoinositides has been implicated in a variety of cellular processes, e.g., malignant transformation, growth factor signaling, inflammation, and immunity (Rameh et al (1999) J. Biol Chem, 274:8347-8350). The enzyme responsible for generating these phosphorylated signaling products, phosphatidylinositol 3-kinase (also referred to as PI 3-kinase or PI3K), was originally identified as an activity associated with viral oncoproteins and growth factor receptor tyrosine kinases that phosphorylate phosphatidylinositol (PI) and its phosphorylated derivatives at the 3′-hydroxyl of the inositol ring (Panayotou et al (1992) Trends Cell Biol 2:358-60).Phosphoinositide 3-kinases (PI3K) are lipid kinases that phosphorylate lipids at the 3-hydroxyl residue of an inositol ring (Whitman et al (1988) Nature, 332:664). The 3-phosphorylated phospholipids (PIP3s) generated by PI3-kinases act as second ...

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Номер записи: 34
09-05-2013 дата публикации

FUSED POLYHETEROAROMATIC COMPOUND, ORGANIC THIN FILM INCLUDING THE COMPOUND, AND ELECTRONIC DEVICE INCLUDING THE ORGANIC THIN FILM

Номер: US20130116447A1
Автор: Chung Jong Won, Lee Bang Lin, Lee Ji Youl, Park Jeong il
Принадлежит: SAMSUNG ELECTRONICS CO., LTD.

A low-molecular-weight fused polycyclic heteroaromatic compound may have a compact planar structure in which seven or more rings are fused together. The compound may exhibit a relatively high charge mobility and enable the use of a deposition process or a room-temperature solution process when applied to devices, therefore realizing improved processibility. An organic thin film and electronic device may include the fused polycyclic heteroaromatic compound. 2. The fused polycyclic heteroaromatic compound of claim 1 , wherein the R claim 1 , R claim 1 , R claim 1 , R claim 1 , R claim 1 , or Rthat is not linked to provide the aromatic ring claim 1 , the heteroaromatic ring claim 1 , or the alicyclic ring fused with the X-containing ring or the X-containing ring is a substituted or unsubstituted C10 to C30 alkyl group or a substituted or unsubstituted C10 to C30 alkenyl group.3. The fused polycyclic heteroaromatic compound of claim 1 , wherein X claim 1 , X claim 1 , X claim 1 , and Xare sulfur (S).5. The fused polycyclic heteroaromatic compound of claim 4 , wherein X claim 4 , X claim 4 , X claim 4 , and Xare sulfur (S).7. The fused polycyclic heteroaromatic compound of claim 6 , wherein X claim 6 , X claim 6 , X claim 6 , and Xare sulfur (S).9. The fused polycyclic heteroaromatic compound of claim 8 , wherein X claim 8 , X claim 8 , X claim 8 , X claim 8 , X claim 8 , X claim 8 , X claim 8 , and Xare sulfur (S).11. The fused polycyclic heteroaromatic compound of claim 10 , wherein X claim 10 , X claim 10 , X claim 10 , X claim 10 , X claim 10 , and Xare sulfur (S).12. The fused polycyclic heteroaromatic compound of claim 1 , wherein the compound has an average molecular weight of about 350 to about 3000.13. An organic thin film comprising the fused polycyclic heteroaromatic compound according to .14. An electronic device comprising the fused polycyclic heteroaromatic compound according to .15. The electronic device of claim 14 , wherein the electronic device is a ...

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Номер записи: 35
16-05-2013 дата публикации

PHOTOELECTRIC CONVERSION DEVICE, PRODUCTION METHOD THEREOF, PHOTOSENSOR, IMAGING DEVICE AND THEIR DRIVE METHODS

Номер: US20130122276A1
Автор: FUKUZAKI Eiji, MITSUI Tetsuro, NOMURA Kimiatsu
Принадлежит: FUJIFILM Corporation

A photoelectric conversion device comprising a transparent electrically conductive film, a photoelectric conversion film and an electrically conductive film in this order, wherein the photoelectric conversion film comprises a photoelectric conversion layer, and an electron blocking layer, wherein the electron blocking layer contains a compound represented by the specific formula. 2. An electron blocking material comprising the compound according to .3. A film comprising the compound according to claim 1 , wherein the film has a thickness of 1 to 1 claim 1 ,000 nm.4. The compound according to claim 1 , wherein Rand R′in formula (F-10) are the same.5. The compound according to claim 1 , wherein Aand Ain formula (F-10) are the same.6. The compound according to claim 1 , wherein Xa in formula (A-1) represents a single bond.7. The compound according to claim 1 , wherein the compound represented by formula (F-10) has a molecular weight of 500 to 2000.8. The compound according to claim 1 , wherein the compound represented by formula (F-10) has an ionization potential of 5.8 eV or less. 1. Field of the InventionThe present invention relates to a photoelectric conversion device, a production method thereof, a photosensor, an imaging device and their driving methods.2. Description of the Related ArtAs for the solid-state imaging device, there is widely used a flat light-receiving device where photoelectric conversion sites are two-dimensionally arrayed in a semiconductor to form pixels and a signal generated by photoelectric conversion in each pixel is charge-transferred and read out through a CCD or CMOS circuit. The conventional photoelectric conversion site generally used is a photodiode part formed using PN junction in a semiconductor such as Si.In recent years, fabrication of a multipixel device is proceeding, and the pixel size and in turn, the area of a photodiode part become small, which brings about problems of reduction in the aperture ratio, reduction in the light ...

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Номер записи: 36
16-05-2013 дата публикации

Herbicidal Isoxazolo[5,4-B]pyridines

Номер: US20130123105A1
Автор: EVANS Richard Roger, Grossmann Klaus, Hutzler Johannes, Kraus Helmut, Kreuz Klaus, Major Julia, Michrowska-Pianowska Anna Aleksandra, Moberg William Karl, NEWTON Trevor William, PARRA RAPADO Liliana, QU Tao, Reingruber Ruediger, SEITZ Thomas, SIMON Anja, Song Dschun, Stelzer Frank, Van Der Kloet Andree, WITSCHEL Matthias
Принадлежит: BASF SE

The invention relates to isoxazolo[5,4-b]pyridine compounds of formula I, 116-. (canceled)18. The method as claimed in claim 17 , wherein in formula I{'sup': '1', 'sub': 1', '6', '1', '6, 'Ris hydrogen, halogen, C-C-alkyl, or C-C-haloalkyl.'}19. The method as claimed in claim 17 , wherein in formula I{'sup': '2', 'sub': 1', '6', '1', '6', '1', '6', '3', '6', '3', '6', '2', '6', '2', '6, 'Ris hydrogen, C-C-alkyl, C-C-haloalkyl, C-C-hydroxyalkyl, C-C-cycloalkyl, C-C-halocycloalkyl, C-C-alkenyl, or C-C-alkynyl.'}20. The method as claimed in claim 17 , wherein in formula I{'sup': '1', 'Ris hydrogen;'}{'sup': '2', 'sub': 1', '6', '1', '6', '1', '6', '3', '6', '3', '6', '2', '6', '2', '6, 'Ris hydrogen, C-C-alkyl, C-C-haloalkyl, C-C-hydroxyalkyl, C-C-cycloalkyl, C-C-halocycloalkyl, C-C-alkenyl, or C-C-alkynyl;'}{'sup': 3', '3, 'sub': 1', '6', '1', '6', '3', '6', '1', '6', '3', '6', '1', '6', '3', '6', '3', '6', '1', '4', '3', '6', '1', '6', '1', '6', '1', '4', '1', '4', '1', '4', '1', '4', '3', '6', '2', '6', '2', '6', '1', '4', '1', '4', '1', '4', '1', '4', '1', '4', '1', '4', '1', '4, 'Ris C-C-alkyl, C-C-haloalkyl, C-C-cycloalkyl-C-C-alkyl, C-C-halocycloalkyl-C-C-alkyl, C-C-cycloalkyl, C-C-halocycloalkyl, C-C-alkyl-C-C-cycloalkyl, C-C-alkoxy, C-C-haloalkoxy, or phenyl; wherein the phenyl moieties of Rcan be unsubstituted or substituted with one or more radicals selected from the group consisting of halogen, hydroxy, nitro, cyano, C-C-alkyl, C-C-haloalkyl, C-C-alkoxy-C-C-alkyl, C-C-cycloalkyl, C-C-alkenyl, C-C-alkynyl, C-C-alkoxy, C-C-haloalkoxy, C-C-alkoxycarbonyl, C-C-alkylsulfinyl, C-C-alkylsulfonyl, amino, C-C-alkylamino, N,N-di-(C-C)-alkylamino, heterocyclyl, or phenyl;'}{'sup': 4', '5, 'X is ORor SR.'}21. The method as claimed in claim 17 , wherein in formula I{'sup': '4', 'X is OR;'}{'sup': '4', 'sub': 1', '6', '1', '6', '1', '6', '1', '6', '1', '6', '1', '6', '1', '6', '2', '6', '2', '6', '2', '6, 'Ris hydrogen, C-C-alkyl, C-C-haloalkyl, C-C-cyanoalkyl, C-C- ...

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Номер записи: 37
23-05-2013 дата публикации

SUBSTITUTED 6-(ALKYLBENZYLAMINO) PURINE DERIVATIVES FOR USE AS CYTOKININ RECEPTOR ANTAGONISTS AND PREPARATIONS CONTAINING THESE DERIVATIVES

Номер: US20130130906A1
Автор: Dolezal Karel, POPA IGOR, Schmulling Thomas, Spichal Lukas, Strnad Miroslav, Voller Jiri, Werner Tomàs
Принадлежит:

6-(alkylbenzylamino)purine derivatives of the general formula I for use as cytokinin receptor antagonists. R1 is selected from a group which includes, but is not limited to, hydroxyl, amino, nitro, thio and alkyl group. R2 denotes one to four alkyl groups. The invention also relates to preparations containing these derivatives and methods of using the derivatives. 4. A method of claim 1 , wherein the substituted 6-(alkylbenzylamino)purine derivatives are selected from the group consisting of 6-(2-amino-3-methylbenzylamino)purine claim 1 , 6-(2-amino-4-methylbenzylamino)purine claim 1 , 6-(2-amino-5-methylbenzylamino)purine claim 1 , 6-(2-amino-3-ethylbenzylamino)purine claim 1 , 6-(2-amino-5-ethylbenzylamino)purine claim 1 , 6-(2-amino-3-isopropylbenzylamino)purine claim 1 , 6-(2-amino-5-isopropylbenzylamino)purine claim 1 , 6-(2-hydroxy-3-methylbenzylamino)purine claim 1 , 6-(2-hydroxy-4-methylbenzylamino)purine claim 1 , 6-(2-hydroxy-5-methylbenzylamino)purine claim 1 , 6-(2-hydroxy-6-methylbenzylamino)purine claim 1 , 6-(2-hydroxy-3-ethylbenzylamino)purine claim 1 , 6-(2-hydroxy-4-ethylbenzylamino)purine claim 1 , 6-(2-hydroxy-5-ethylbenzylamino)purine claim 1 , 6-(2-hydroxy-6-ethylbenzylamino)purine claim 1 , 6-(2-hydroxy-3-isopropylbenzylamino)purine claim 1 , 6-(2-hydroxy-5-isopropylbenzylamino)purine claim 1 , 6-(2-nitro-3-methylbenzylamino)purine claim 1 , 6-(2-nitro-4-methylbenzylamino)purine claim 1 , 6-(2-thio-3-methylbenzylamino)purine claim 1 , 6-(2-thio-5-methylbenzylamino)purine claim 1 , 6-(2-thio-3-ethylbenzylamino)purine 6-(2-hydroxy-3 claim 1 ,5-dimethylbenzylamino)purine claim 1 , 6-(2-hydroxy-3 claim 1 ,4-dimethylbenzylamino)purine claim 1 , 6-(2-hydroxy-3 claim 1 ,6-dimethylbenzylamino)purine claim 1 , 6-(2-hydroxy-3 claim 1 ,4 claim 1 ,5-trimethylbenzylamino)purine claim 1 , 6-(2-amino-3 claim 1 ,5-dimethylbenzylamino)purine claim 1 , 6-(2-amino-3 claim 1 ,6-dimethylbenzylamino)purine claim 1 , 6-(2-hydroxy-3 claim 1 ,5-diethylbenzylamino) ...

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Номер записи: 38
23-05-2013 дата публикации

SPIROXAZOLIDINONE COMPOUNDS

Номер: US20130131042A1
Автор: Bao Jianming, Duffy Joseph L., Finke Paul E., Hussain Zahid, Katipally Revathi, Liu Weiguo, Moningka Remond, Ondeyka Debra L., Plotkin Michael A., Romero F. Anthony, Shao Patrick, Sherer Edward C., Tyagarajan Sriram, Ujjainwalla Feroze, Wood Harold B., Ye Feng, Zang Yi, Zwicker Aaron
Принадлежит: Merck Sharp & Dohme Corp.

Substituted spirocyclic amines of structural formula (I) are selective antagonists of the somatostatin subtype receptor 5 (SSTR5) and are useful for the treatment, control or prevention of disorders responsive to antagonism of SSTR5, such as Type 2 diabetes, insulin resistance, lipid disorders, obesity, atherosclerosis, Metabolic Syndrome, depression, and anxiety. 2. A compound of or a pharmaceutically acceptable salt thereof claim 1 , wherein at each occurrence of Ra claim 1 , Ra is hydrogen.3. A compound of or a pharmaceutically acceptable salt thereof claim 1 , wherein Ris phenyl.4. A compound of or a pharmaceutically acceptable salt thereof claim 1 , wherein Ris pyridine.5. A compound of or a pharmaceutically acceptable salt thereof claim 1 , wherein Ris substituted with OH claim 1 , —C-Calkyl claim 1 , —COOH claim 1 , COO—C-Calkyl claim 1 , —O—C-Calkyl —C-Ccycloalkyl claim 1 , —CON(C-Calkyl)NH(C-Calkyl) or heterocycle claim 1 , wherein the —C-Calkyl claim 1 , —C-Ccycloalkyl or —OC-Calkyl is unsubstituted or substituted with 1-4 substituents selected from the group consisting of halogen and —COOH.6. A compound of or a pharmaceutically acceptable salt thereof claim 1 , wherein Ris imidazole claim 1 , naphthalene claim 1 , phenyl claim 1 , pyridine claim 1 , benzimidazole claim 1 , indole claim 1 , oxazole claim 1 , thiazole claim 1 , benzofuran claim 1 , benzocyclopentane claim 1 , benzotetrahydropyran or pyrazole.7. A compound of or a pharmaceutically acceptable salt thereof claim 1 , wherein Ris phenyl.8. A compound of or a pharmaceutically acceptable salt thereof claim 1 , wherein Ris pyridine.9. A compound of or a pharmaceutically acceptable salt thereof claim 1 , wherein Ris imidazole.10. A compound of or a pharmaceutically acceptable salt thereof claim 1 , wherein Ris substituted with two substituents independently selected from α.11. A compound of or a pharmaceutically acceptable salt thereof claim 1 , wherein Ris substituted with three substituents ...

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Номер записи: 39
23-05-2013 дата публикации

COMPOUNDS FOR THE REDUCTION OF BETA-AMYLOID PRODUCTION

Номер: US20130131049A1
Автор: Wu Yong-Jin
Принадлежит:

Compounds of formula (I), including pharmaceutically acceptable salts thereof, are set forth herein: 2. The compound of claim 1 , wherein:{'sub': 1', '2', '3', '4', '5', '6', '1', '6', '1', '6, 'R, R, R, R, R, and Rare independently hydrogen, C-Calkyl or C-Ccycloalkyl;'}{'sub': 1-4', '1-4', '1-4', '1', '6', '1', '6', '2', '4, 'Y is phenyl or thiophenyl and Z is a pyridyl, pyrimidinyl or pyrazinyl, wherein each Y and Z group can be optionally substituted with from 0-3 substituents selected from hydrogen, halogen, amino, Calkylamino, Cdialkylamino, haloCalkyl, OH, CN, C-Calkyl or cycloalkyl, C-Calkoxy, or C-Calkynyl;'}L is either a bond or is —NHCO—; andm is 1 or 2.3. The compound of claim 2 , wherein:{'sub': 1', '2', '3', '4', '5', '6, 'R, R, R, R, R, and Rare hydrogen;'}{'sub': 2', '4, 'Y is phenyl and Z is a pyridyl, wherein each Y and Z group can be optionally substituted with from 0-3 halogen substituents and Z can be optionally substituted with from 0-3 halogen, cyano, or C-Calkynyl substituents;'}L is either a bond or is —NHCO—; andm is 1 or 2.4. The compound of claim 2 , wherein:{'sub': 1', '2', '3', '4', '5', '6, 'R, R, R, R, R, and Rare hydrogen;'}{'sub': 2', '4, 'Y is phenyl optionally substituted with from 0-3 halogen, cyano, or C-Calkynyl substituents;'}L and Z together can be absent; andm is 1 or 2.5. A compound of any claims of 1 to 3 claim 2 , wherein the configuration of the chiral center adjacent to the nitrogen of the aminothiazine is (R) or a pharmaceutically acceptable salt thereof.6. The compound of claim 4 , which is selected from the group consisting of:N-(3-((4aR,7aR)-2-amino-4-a,5,6,7a-tetrahydro-4H-furo[2,3-d][1,3]thiazin-7a-yl)-4-fluorophenyl)-5-chloropicolinamide;N-(3-((4aR,7aR)-2-amino-4-a,5,6,7a-tetrahydro-4H-furo[2,3-d][1,3]thiazin-7a-yl)-4-cyanophenyl)-5-chloropicolinamide;N-(3-((4aR,7aR)-2-amino-4-a,5,6,7a-tetrahydro-4H-furo[2,3-d][1,3]thiazin-7a-yl)-4-cyanophenyl)-5-bromopicolinamide;N-(3-((4aR,7aR)-2-amino-4a,5,6,7a-tetrahydro-4H- ...

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Номер записи: 40
23-05-2013 дата публикации

FUSED HETEROCYCLIC COMPOUND AND APPLICATION THEREOF

Номер: US20130131050A1
Автор: Asano Kouhei, MATSUNAGA Nobuyuki, OKAMOTO Rei, Suzuki Hideo, Tokuhara Hidekazu, YAMAMOTO Takeshi
Принадлежит: Takeda Pharmaceutical Company Limited

The present invention provides a compound useful for the prophylaxis or treatment of eicosanoid-associated diseases such as atherosclerosis, atherothrombosis, diabetes, obesity, asthma, fever, pain, cancer, rheumatism, osteoarthritis, atopic dermatitis and the like, and having superior pharmacological action, physicochemical properties and the like. 2. The compound or salt of claim 1 , wherein{'sup': '2', 'Xis 0; and'}{'sup': '4', 'sub': '1-6', 'Ris a Calkyl group optionally substituted by 1 to 3 halogen atoms.'}6. 2-(2 claim 1 ,2 claim 1 ,2-Trifluoroethoxy)-3-[4-(2 claim 1 ,2 claim 1 ,2-trifluoroethoxy)phenyl]-5 claim 1 ,6-dihydropyrido[2 claim 1 ,3-d]pyrimidine-4 claim 1 ,7(3H claim 1 ,8H)-dione or a salt thereof.7. 2-Ethoxy-3-[4-(2 claim 1 ,2 claim 1 ,2-trifluoroethoxy)phenyl]-5 claim 1 ,6-dihydropyrido[2 claim 1 ,3-d]pyrimidine-4 claim 1 ,7(3H claim 1 ,8H)-dione or a salt thereof.8. 3-[4-(2 claim 1 ,2 claim 1 ,2-Trifluoroethoxy)phenyl]-2-(3 claim 1 ,3 claim 1 ,3-trifluoropropyl)-5 claim 1 ,6-dihydropyrido[2 claim 1 ,3-d]pyrimidine-4 claim 1 ,7(3H claim 1 ,8H)-dione or a salt thereof.9. A medicament comprising the compound or salt of .10. The medicament of claim 9 , which is a delta-5-desaturase inhibitor.11. The medicament of claim 9 , which is an agent for the prophylaxis or treatment of eicosanoid-associated diseases.12. The medicament of claim 9 , which is an agent for the prophylaxis or treatment of arteriosclerosis.13. The medicament of claim 9 , which is an agent for the prophylaxis or treatment of diabetes or obesity.14. A method for the prophylaxis or treatment of arteriosclerosis in a mammal claim 1 , comprising administering an effective amount of the compound or salt of to the mammal.15. A method for the prophylaxis or treatment of diabetes or obesity in a mammal claim 1 , comprising administering an effective amount of the compound or salt of to the mammal.1617-. (canceled)18. The compound or salt of for use in the prophylaxis or treatment of ...

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Номер записи: 41
23-05-2013 дата публикации

COMPOUNDS FOR THE REDUCTION OF BETA-AMYLOID PRODUCTION

Номер: US20130131051A1
Автор: Higgins Mendi A., III Lorin A., MARCIN Lawrence R., Rajamani Ramkumar, Shi Jianliang, Thompson, Wu Yong-Jin
Принадлежит:

Compounds of formula (I), including pharmaceutically acceptable salts thereof, are set forth herein: 2. The compound of claim 1 , wherein:{'sub': '2', 'X is selected from CHand O;'}m=0 or 1;n=0 to 3;{'sup': '1', 'sub': 1-4', '1-4', '1-4', '1', '6', '1', '6', '2', '4, 'Rat each instance is selected from the group of halogen, hydroxy, amino, Calkylamino, Cdialkylamino, haloCalkyl, CN, C-Calkyl or cycloalkyl, C-Calkoxy, or C-Calkynyl;'}L is either a bond or is —NHCO—;{'sub': 1-4', '1-4', '1-4', '1', '6', '1', '6', '2', '4, 'Z is a phenyl, pyridyl, pyrimidinyl, or pyrazinyl group which can be further substituted with from 0-3 substituents selected from the group of halogen, hydroxy, amino, Calkylamino, Cdialkylamino, haloCalkyl, CN, C-Calkyl or cycloalkyl, C-Calkoxy, and C-Calkynyl;'}{'sup': 3', '4', '5, 'sub': '1-4', 'and R, Rand Rare independently selected from hydrogen or Calkyl.'}3. The compound of claim 2 , wherein:{'sub': '2', 'X is selected from CHand O;'}m=0 or 1;n=0 to 3;{'sup': '1', 'Rat each instance is selected from halogen,'}L is either a bond or is —NHCO—;{'sub': 2', '4, 'Z is a phenyl, pyridyl, pyrimidinyl, or pyrazinyl group which can be further substituted with from 0-3 substituents selected from halogen, CN, or C-Calkynyl;'}{'sup': '3', 'sub': '1-4', 'Ris selected from hydrogen or Calkyl;'}{'sup': 4', '5, 'and Rand Rare hydrogen.'}4. A compound of any claims of 1 to 3 wherein the configuration of the chiral center adjacent to the nitrogen of the aminothiazine is (S) or a pharmaceutically acceptable salt thereof.5. The compound of claim 4 , which is 5-Chloro-pyridine-2-carboxylic acid ((4aS claim 4 ,11bS)-2-amino-11b-methyl-4 claim 4 ,4a claim 4 ,5 claim 4 ,6 claim 4 ,7 claim 4 ,11b-hexahydro-3-thia-1-aza-dibenzo[a claim 4 ,c]cyclohepten-10-yl)-amide.6. A pharmaceutical composition which comprises one or more of the compounds as claimed in claim 1 , together with one or more pharmaceutically acceptable carriers claim 1 , excipients or diluents.7. A ...

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Номер записи: 42
30-05-2013 дата публикации

OXOPYRAZINE DERIVATIVE AND HERBICIDE

Номер: US20130137577A1
Автор: Ito Minoru, Kobayashi Masami, Mitsunari Takashi, Nakano Yuki, Tamai Ryuji
Принадлежит:

The present invention is to provide an oxopyrazine derivative having an excellent herbicidal activity and besides exhibiting high safety for useful crops and the like, or a salt thereof, and a herbicide containing the same. 2. (canceled)3. (canceled)4. The oxopyrazine derivative or the agrochemically acceptable salt thereof according to claim 1 , wherein Ris hydroxyl group; or OM (wherein M is an alkali metal cation or an ammonium cation).5. The oxopyrazine derivative or the agrochemically acceptable salt thereof according to claim 1 , wherein{'sup': '2', 'Xis a nitrogen atom;'}{'sup': 1', '6', '7', '8', '1', '9', '10', '11', '12', '1', '13, 'sub': 1', '12', '2', '6', '2', '6', '3', '8', '1', '6', '2', '6', '1', '6', '1', '6', '1', '6', '1', '6', '1', '6', '1', '6', '1', '6', '1', '6', '1', '6', '1', '6', '1', '6', '1', '6', '1', '6', '1', '6', '1', '6', '1', '6', '1', '6', '1', '6', '1', '6', '1', '6', '1', '6', '1', '6', '1', '6', '1', '6', '1', '6', '1', '6', '1', '6', '6', '10', '1', '6', '1', '6', '6', '10, 'Rrepresents a hydrogen atom; a C-Calkyl group; a C-Calkenyl group; a C-Calkynyl group; a C-Ccycloalkyl group; a C-Chaloalkyl group; a C-Chaloalkenyl group; a C-Calkylthio-C-Calkyl group; a C-Calkylsulfonyl-C-Calkyl group; a C-Calkoxy-C-Calkyl group; a C-Calkoxy-C-Calkoxy-C-Calkyl group; a phenoxy-C-Calkyl group; a C-Chaloalkoxy-C-Calkyl group; a tetrahydrofuran-C-Calkoxy-C-Calkyl group; a C-Calkylsulfonyl-C-Calkoxy-C-Calkyl group; a cyano-C-Calkoxy-C-Calkyl group; a cyano-C-Calkyl group; a C-Calkylcarbonyloxy-C-Calkyl group; a C-Cacyl-C-Calkyl group; a C-Calkoxycarbonyl-C-Calkyl group; a (RRN—C═O)—C-Calkyl group; a C-Caryl-C-Calkyl group (the aryl moiety of the group may be substituted with one or two or more identical or different Rs); a Het-C-Calkyl group (the group may be substituted with one or two or more identical or different Rs); a NRRgroup; a C-Caryl group (the group may be substituted with one or two or more identical or different Rs); or a ...

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Номер записи: 43
06-06-2013 дата публикации

ORGANIC SEMICONDUCTOR COMPOSITION, ORGANIC THIN FILM, AND ORGANIC THIN FILM TRANSISTOR HAVING SAME

Номер: US20130140548A1
Автор: Kohiro Kenji, Okachi Takayuki
Принадлежит: Sumitomo Chemical Company, Limited

To provide an organic semiconductor composition that can exhibit a high carrier transport property and give uniform characteristics. An organic semiconductor composition characterized by containing a high molecular weight compound having a carrier transport property and a low molecular weight compound, in which the low molecular weight compound has a structure represented by Formula (1) and a content ratio of the low molecular weight compound is from 5 to 95 parts by mass relative to a total of 100 parts by mass of the high molecular weight compound and the low molecular weight compound, 2. The organic semiconductor composition according to claim 1 , wherein the high molecular weight compound has a repeating unit containing at least one kind of structures of an arylamine structure claim 1 , a fluorene structure claim 1 , and a thiophene structure.3. The organic semiconductor composition according to claim 1 , wherein a content ratio of the high molecular weight compound is either from not less than 5 parts by mass to less than 30 parts by mass or from more than 70 parts by mass to not more than 95 parts by mass relative to a total of 100 parts by mass of the high molecular weight compound and the low molecular weight compound.4. The organic semiconductor composition according to claim 1 , wherein the content ratio of the high molecular weight compound is from not less than 5 parts by mass to less than 30 parts by mass relative to a total of 100 parts by mass of the high molecular weight compound and the low molecular weight compound.5. An organic thin film claim 1 , comprising the organic semiconductor composition according to .6. An organic thin film transistor comprising:a source electrode and a drain electrode;an organic semiconductor layer that serves as a current path between these electrodes; anda gate electrode that controls an amount of current flowing through the current path,{'claim-ref': {'@idref': 'CLM-00005', 'claim 5'}, 'wherein the organic ...

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Номер записи: 44
06-06-2013 дата публикации

MODIFIED SOPHOROLIPIDS COMBINATIONS AS ANTIMICROBIAL AGENTS

Номер: US20130142855A1
Автор: Gross Richard A., Thavasi Thavasi Renga
Принадлежит: Polytechnic Institute of New York University

A method to control, inhibit, and kill pathogens and normal microbial strains that includes, but not limited to plant, animal and human pathogens, biofilm forming microbes, biofouling microbes, algae, fungi, bacteria, virus and protozoa using natural SL, MSL derivative and combinations thereof encompassed by the combination invention. 1. A method for controlling , inhibiting the growth of , or killing live cells and/or spores , comprising:a) providing an admixture of compounds that consist of at least two constituents selected from the group consisting of natural sophorolipids, natural sophorolipid mixture, and modified sophorolipids; andb) applying the admixture to undesirable microbial cells, plants, surface, device, or any system containing undesirable microbes, live cells, and/or spores that have grown or might grow,whereby the admixture controls, inhibits the growth of, or kills the live cells and/or spores.2. The method of where the microbe is selected from the group consisting of plant pathogens claim 1 , human pathogens claim 1 , microbes claim 1 , or combination of microbes.3. The method of claim 2 , wherein the microbe is a microbe grows on surfaces causing fouling or contamination of that surface.4. The method of claim 3 , wherein the microbe has accumulated in excess due to some shift in an ecosystem selected from the group consisting of a non-natural chemical in lakes claim 3 , catheters claim 3 , medical dives claim 3 , walls claim 3 , shower curtains claim 3 , shower rooms claim 3 , swimming pools claim 3 , pipelines claim 3 , water filters claim 3 , cooling towers claim 3 , marine structures claim 3 , ships claim 3 , boats claim 3 , navigational aids claim 3 , channel markers claim 3 , buoys claim 3 , oil exploration plat forms claim 3 , oil wells claim 3 , oil pipelines claim 3 , and surface of equipment.5. The method of claim 1 , wherein the modified sophorolipids are synthesized by methods using natural sophorolipids produced by fermentation from ...

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Номер записи: 45
06-06-2013 дата публикации

SEMICONDUCTOR MATERIALS PREPARED FROM BRIDGED BITHIAZOLE COPOLYMERS

Номер: US20130144065A1
Автор: Basuki Johan Sebastian, Doetz Florian, Mishra Ashok Kumar, Noguchi Hiroyoshi, Vaidyanathan Subramanian, ZHU Bo
Принадлежит:

The present invention provides semiconducting compounds, oligomers and polymers of formula wherein Aand Acan be the same or different and are S or Se, E is selected from the group consisting of The compounds, oligomers and polymers of formula of formula (1) are suitable for use in electronic devices such as organic field effect transistors. 2. The compound of claim 1 , wherein Aand Aare S.6. The compound of claim 1 , wherein Rand Rare independently H claim 1 , C-alkyl claim 1 , C-haloalkyl claim 1 , —X—Ror —X—Ar claim 1 ,wherein{'sup': 1', '1', '1', '1, 'sub': a', 'a', 'a, 'claim-text': wherein', {'sup': '1', 'sub': 1-6', '1-6, 'Zis C-alkylene or C-haloalkylene, and'}, 'a is an integer of from 1 to 10,, 'Xis —[Z—O]—, —[Z—S—]—, or —[S—Z]—S—,'}{'sup': '6', 'sub': 1-30', '1-30, 'Ris C-alkyl or C-haloalkyl,'}{'sup': 2', '3', '4', '3', '4, 'sub': 1-30', '1-30, 'claim-text': {'sup': 3', '4, 'sub': 1-6', '1-6, 'wherein Zand Zare independently C-alkylene or C-haloalkylene,'}, 'Xis —Z—O—Z—, —Z—S—Z—, C-alkylene or C-haloalkylene,'}and{'sup': 1', 'a', 'a, 'sub': 6-14', '1-6', '1-6, 'Aris C-aryl, optionally substituted with 1 to 5 substituents R, wherein Ris selected from the group consisting of a halogen, a C-alkyl, and a C-alkoxy.'}7. The compound of claim 1 , wherein Rand Rare independently a C-alkyl.8. The compound of claim 1 , wherein Ris —X—Ar claim 1 , —X—Ar—Ar claim 1 , —X—Ar—Ror —X—Ar—Ar—R claim 1 ,wherein{'sup': '5', 'Xis a covalent bond,'}{'sup': 7', 'e', 'e, 'sub': 6-14', '1-6', '1-6', '1-6, 'Aris C-aryl or monovalent 5 to 14 membered aromatic heterocyclic residue, each optionally substituted with 1 to 5 substituents R, wherein Ris selected from the group consisting of a halogen, a CN, a C-alkyl, a C-alkoxy and a C-haloalkyl,'}{'sup': 8', '9', 'f', 'f, 'sub': 6-14', '1-6', '1-6', '1-6, 'Arand Arare independently C-arylene or bivalent 5 to 14 membered aromatic heterocyclic residue, each optionally substituted with 1 to 4 substituents R, wherein Ris selected from the ...

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Номер записи: 46
13-06-2013 дата публикации

NOVEL COMPOUNDS

Номер: US20130150347A1
Автор: BISCHOFF Daniel, DAHMANN Georg, GRAUERT Matthias, KUELZER Raimund, RUDOLF Klaus, WELLENZOHN Bernd
Принадлежит:

This invention relates to compounds of formula I 2. The compound according to claim 1 , wherein{'sup': '1', 'sub': 1-4', '3-6', '1-3', '1-3, 'Rrepresents phenyl, Calkyl or Ccycloalkyl which latter three groups are optionally substituted with one or more substituents selected from fluoro, Calkyl and —O—Calkyl.'}12. A pharmaceutical composition comprising a therapeutically effective amount of a compound according to or a pharmaceutically acceptable salt thereof in admixture with a pharmaceutically acceptable adjuvant claim 1 , diluent and/or carrier.13. A method of treating schizophrenia claim 1 , schizoaffective disorder and substance induced psychotic disorder; cognitive disorders and dementias including age-associated learning and memory impairments or losses claim 1 , post stroke dementia claim 1 , deficits in concentration claim 1 , mild cognitive impairment claim 1 , the cognitive dysfunction in Alzheimers disease or the cognitive dysfunction of schizophrenia comprising administering to a patient a therapeutically effective amount of a compound according to . This invention relates to substituted imidazoles and their use as positive allosteric modulators of mGlu5 receptor activity, pharmaceutical compositions containing the same, and methods of using the same as agents for treatment and/or prevention of neurological and psychiatric disorders associated with glutamate dysfunction such as schizophrenia or cognitive decline such as dementia or cognitive impairment.Glutamate is the primary excitatory amino acid in the mammalian central nervous system. Neurotransmission mediated by glutamate has been demonstrated to be critical in many physiological processes, such as synaptic plasticity, long term potentiation involved in both learning and memory as well as sensory perception (Riedel et al., Behay. Brain Res. 2003, 140:1-47). Furthermore, it has been demonstrated that an imbalance of glutamate neurotransmission plays a critical role in the pathophysiology of various ...

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Номер записи: 47
13-06-2013 дата публикации

CHEMICAL COMPOUNDS

Номер: US20130150366A1
Автор: BASARAB Gregory Steven, Dangel Brian, FLEMING Paul Robert, GRAVESTOCK Michael Barry, GREEN Oluyinka, HAUCK Sheila Irene, HILL Pamela, HULL Kenneth Gregory, MULLEN George, Ni Haihong, SHERER Brian, Zhou Fei
Принадлежит: ASTRAZENECA, INTELLECTUAL PROPERTY

Compounds of formula (I) and their pharmaceutically acceptable salts are described. Processes for their preparation, pharmaceutical compositions containing them, their use in the treatment of bacterial infections are also described. 7. The compound of claim 1 , or a pharmaceutically acceptable salt thereof wherein Ris methyl.8. The compound of claim 7 , or a pharmaceutically acceptable salt thereof wherein Ris chloro.9. The compound of claim 8 , or a pharmaceutically acceptable salt thereof wherein Ris chloro.10. The compound of claim 9 , or a pharmaceutically acceptable salt thereof wherein Ris a substituent on carbon and is selected from methoxy claim 9 , hydroxy claim 9 , methoxycarbonyl claim 9 , fluoro claim 9 , allyloxy claim 9 , propoxy claim 9 , N claim 9 ,N-dimethylcarbamoyl claim 9 , morpholinocarbonyl claim 9 , N-ethylcarbamoyl claim 9 , N-(2-hydroxyethyl)carbamoyl claim 9 , dimethylaminomethyl claim 9 , N-methyl-N-methoxycarbamoyl claim 9 , methoxymethyl claim 9 , methylaminomethyl and carboxy.11. The compound of claim 1 , or a pharmaceutically acceptable salt thereof wherein Ris a substituent on carbon and is selected from halo claim 1 , carboxy claim 1 , carbamoyl claim 1 , Calkyl claim 1 , Calkoxy claim 1 , N—(Calkyl)carbamoyl claim 1 , N—(Calkoxy)carbamoyl or Calkoxycarbonyl; wherein Rmay be optionally substituted on carbon by one or more R; wherein Ris selected from Calkoxy or carbocyclyl-R—; and Ris a direct bond.12. The compound claim 1 , or a pharmaceutically acceptable salt thereof wherein Ris hydrogen.13. A compound which is2-((3S,4R)-4-{[(3,4-dichloro-5-methyl-1H-pyrrol-2-yl)carbonyl]amino}-3-fluoropiperidin-1-yl)-1,3-thiazole-5-carboxylic acid;2-((3S,4R)-4-{[(3,4-dichloro-5-methyl-1H-pyrrol-2-yl)carbonyl]amino}-3-methoxypiperidin-1-yl)-4-{[(2-methoxyethyl)amino]carbonyl}-1,3-thiazole-5-carboxylic acid;2-((3S,4R)-4-{[(3,4-dichloro-5-methyl-1H-pyrrol-2-yl)carbonyl]amino}-3-methoxypiperidin-1-yl)-4-{[(1S)-2-methoxy-1-methylethyl]amino}carbonyl)- ...

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Номер записи: 48
13-06-2013 дата публикации

Novel Sultam Compounds

Номер: US20130150376A1
Автор: "ONeill Brian Thomas", Brodney Michael Aaron, Efremov Ivan Viktorovich, Helal Christopher John
Принадлежит: PFIZER INC.

Compounds and pharmaceutically acceptable salts of the compounds are disclosed, wherein the compounds have the structure of Formula I (I) as defined in the specification. Corresponding pharmaceutical compositions, methods of treatment, methods of synthesis, and intermediates are also disclosed. 2. A compound of wherein A is Ccycloalkyl claim 1 , Caryl claim 1 , 4- to 10-membered heterocycloalkyl claim 1 , or 5- to 10-membered heteroaryl and A is optionally substituted with one to three Rsubstituents selected from the group consisting of Calkyl claim 1 , halogen claim 1 , cyano claim 1 , —COR claim 1 , —CON(R) claim 1 , —N(R)COR claim 1 , —N(R)COR claim 1 , —N(R)CON(R) claim 1 , —N(R)SOR claim 1 , —SOR claim 1 , —SON(R) claim 1 , —(C(R))—Ccycloalkyl claim 1 , —(C(R))-(4- to 10-membered heterocycloalkyl) claim 1 , —(C(R))—Caryl claim 1 , —(C(R))-(5- to 10-membered heteroaryl) claim 1 , —(C(R))—N(R) claim 1 , or —(C(R))—OR; wherein each Ralkyl claim 1 , cycloalkyl claim 1 , heterocycloalkyl claim 1 , aryl claim 1 , or heteroaryl is optionally substituted by one to three cyano claim 1 , Calkyl claim 1 , Ccycloalkyl claim 1 , halogen claim 1 , —CFor —OR; and pharmaceutically acceptable salts thereof.3. A compound of wherein A is Caryl and A is optionally substituted with one to three Rsubstituents selected from the group consisting of Calkyl claim 2 , halogen claim 2 , cyano claim 2 , —COR claim 2 , —CON(R) claim 2 , —(C(R))Ccycloalkyl claim 2 , —(C(R))-(4- to 10-membered heterocycloalkyl) claim 2 , —(C(R))—Caryl claim 2 , —(C(R))-(5- to 10-membered heteroaryl) claim 2 , or —(C(R))—OR; wherein each Ralkyl claim 2 , cycloalkyl claim 2 , heterocycloalkyl claim 2 , aryl claim 2 , or heteroaryl is optionally substituted by one to three cyano claim 2 , Calkyl claim 2 , Ccycloalkyl claim 2 , halogen claim 2 , —CFor —OR; and pharmaceutically acceptable salts thereof.4. A compound of wherein t is 0 or 1; B is —(C(R))—Caryl claim 3 , or —(C(R))-(5- to 10-membered heteroaryl); ...

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Номер записи: 49
13-06-2013 дата публикации

PESTICIDAL COMPOSITIONS

Номер: US20130150394A1
Автор: Buchholz Anke, Grimm Christoph
Принадлежит: SYNGENTA CROP PROTECTION LLC

A pesticidal composition comprising a pesticidal effective amount of at least one compound of formula (I) in which the substituents are as defined as in claim , and a safener. 2. A composition according to claim 1 , wherein the safener is cloquintocet-mexyl claim 1 , cloquintocet acid or salts thereof claim 1 , mefenpyr-diethyl claim 1 , mefenpyr diacid claim 1 , isoxadifen-ethyl claim 1 , isoxadifen acid claim 1 , cyprosulfamide or N-(2-methoxybenzoyl)-4-[(methylaminocarbonyl)amino]-benzenesulfonamide.3. A composition according to claim 2 , wherein the safener is cloquintocet-mexyl claim 2 , cloquintocet acid or salts thereof claim 2 , mefenpyr-diethyl claim 2 , mefenpyr diacid or N-(2-methoxybenzoyl)-4-[(methylaminocarbonyl)amino]-benzenesulfonamide.4. A composition according to claim 1 , wherein the ratio compound of formula I to safener is from 15:1 to 1:105. A method of combating and controlling pests which comprises treating the pests or the locus of the pests or the plant susceptible to attack by a pest or the seeds thereof with an insecticidally claim 1 , nematicidally or mollusicidally effective amount of a composition according to . The present invention relates to new pesticidal, in particular insecticidal, acaricidal, molluscicidal and nematicidal compositions and to methods of using them to combat and control pests such as insect, acarine, mollusc and nematode pests.The application of pesticidal compositions to crop plants or the locus thereof can result in considerable damage being caused to crop plants, for example in dependence upon the concentration of the pesticide and the mode of its application, the crop plant, the nature of the soil and the climatic conditions, such as period of exposure to light, temperature and amounts of precipitation. In order to counter those problems, various substances have already been proposed as safeners that are capable of protecting the crop plant against the damaging action of the pesticide. It has been found that a ...

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Номер записи: 50
13-06-2013 дата публикации

SALTS, PRODRUGS AND POLYMORPHS OF FAB I INHIBITORS

Номер: US20130150400A1
Автор: Pauls Henry, Ramnauth Jailall
Принадлежит: Affinium Pharmaceuticals, Inc.

In part, the present invention is directed to antibacterial compounds and salts thereof. 2. The compound of claim 1 , wherein the compound is in a crystalline form.3. The compound of claim 1 , wherein n equals 1 claim 1 , m equals 1 and X is HSOAr.4. The compound of claim 1 , wherein n equals 1 claim 1 , m equals 0 and X is HSOAr.5. The compound of claim 1 , wherein Ar is benzene or toluene.6. The compound of claim 1 , wherein the compound is an anhydrous p-toluenesulfonic salt.7. The salt according to with characteristic peaks in the powder X-ray diffraction pattern at values of 2θ as depicted in .8. The compound of claim 1 , wherein the compound is a mono claim 1 , di claim 1 , tri or fractional hydrate form of a p-toluenesulfonic salt.9. The salt of claim 8 , wherein the monohydrate form has characteristic peaks in the powder X-ray diffraction pattern at values of 20 substantially the same as depicted in .10. The compound of claim 1 , wherein the compound is a hydrochloric acid salt.11. The salt of claim 10 , wherein said salt has a powder X-ray diffraction pattern substantially that same as that depicted in .12. The compound of claim 1 , wherein the compound is a methane sulfonate salt.13. The salt of claim 12 , wherein said salt has a powder X-ray diffraction pattern substantially that same as that depicted in .14. The compound of claim 1 , wherein the compound is a benzenesulfonic salt.15. The salt according to claim 14 , wherein said salt has a powder X-ray diffraction pattern substantially that same as that depicted in .16. The salt according to claim 15 , wherein said salt has a powder X-ray diffraction pattern substantially that same as that depicted in .17. The compound of claim 1 , wherein the compound is a sulfate salt.18. The salt according to claim 17 , wherein said salt has a powder X-ray diffraction pattern substantially that same as that depicted in .19. A compound selected from the group consisting of:(E)-N-methyl-N-((3-methylbenzofuran-2-yl) ...

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Номер записи: 51
13-06-2013 дата публикации

NITROGEN-CONTAINING AROMATIC COMPOUND, ORGANIC SEMICONDUCTOR MATERIAL, AND ORGANIC ELECTRONIC DEVICE

Номер: US20130150576A1
Автор: Hotta Masanori, Jikumaru Masana, Kawada Atsushi, Matsumoto Megumi, Sawada Yuichi
Принадлежит:

Provided are a nitrogen-containing aromatic heterocyclic compound useful as an organic semiconductor material and an organic electronic device using this compound. The nitrogen-containing aromatic heterocyclic compound has a fused indole skeleton represented by the following formula (1), the organic semiconductor material contains the said compound, and the organic electronic device uses the said organic semiconductor material. In general formula (1), X is N-A′, O, S, or Se; A is an alkyl group, a cycloalkyl group, an alkenyl group, an alkynyl group, an aromatic hydrocarbon group, or an aromatic heterocyclic group exclusive of a fused heterocycle consisting of 4 rings or more; and R is a hydrogen atom, an alkyl group, a cycloalkyl group, an alkenyl group, an alkynyl group, an aromatic hydrocarbon group, or an aromatic heterocyclic group exclusive of a fused heterocycle consisting of 4 rings or more. 2. An organic electronic dcvice as described in wherein claim 1 , in general formula (1) claim 1 , Xis N—A′.3. (canceled)4. (canceled)5. (canceled)6. An organic electronic device as described in wherein the organic electronic device is a light-emitting device claim 1 , a thin film transistor claim 1 , or a photovoltaic device.7. An organic electronic device as described in wherein the light-emitting device is an organic electroluminescent device. This invention relates to a novel nitrogen-containing aromatic compound and an organic electronic device using the said compound and, further, to a light-emitting device, a thin film transistor, and a photovoltaic device utilizing the said compound as an organic semiconductor material.In recent years, organic electronic devices in which organic compounds are used as semiconductor materials have enjoyed remarkable prosperity. Typical examples of their applications include organic electroluminescent devices (hereinafter referred to as organic EL device) that are expected to become next generation flat panel displays, organic thin ...

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Номер записи: 52
20-06-2013 дата публикации

Compounds for photovoltaics

Номер: US20130157403A1
Автор: Sheena Zuberi, Tania Zuberi
Принадлежит: Cambridge Display Technology Ltd

A species for use, for example, in a charge transfer layer of a photovoltaic device, the species comprising an acceptor group to which is fused a tuning group. The species can be a small molecule, polymer or oligomer, and monomers for producing said polymer, photovoltaic devices comprising said species, and methods for producing said device, are also provided.

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Номер записи: 53
20-06-2013 дата публикации

AZOLOPYRIDIN-3-ONE DERIVATIVES AS INHIBITORS OF LIPASES AND PHOSPHOLIPASES

Номер: US20130157941A1
Автор: Baringhaus Karl-Heinz, Petry Stefan, Tennagels Norbert
Принадлежит: SANOFI

The present invention relates to azolopyridin-3-one derivatives of the general formula (I) with the meanings specified in the description, to their pharmaceutically usable salts and to their use as drug substances. 5. A compound of the formula I as claimed in claim 1 , in which{'sub': 1', '6', '3', '8, 'R2 is hydrogen, —(C-C)-alkyl, (C-C)-cycloalkyl or phenyl;'}R3 is hydrogen;{'sub': 1', '6, 'R4 is hydrogen or —(C-C)-alkyl.'}6. A pharmaceutical composition comprising one or more of the compounds of the formula I as claimed in together with a pharmaceutically acceptable carrier.7. The pharmaceutical composition as claimed in claim 6 , which comprises claim 6 , as a further active ingredient claim 6 , metformin claim 6 , arcabose claim 6 , glibenclamide claim 6 , glimepiride claim 6 , gliclazide claim 6 , gliquidone claim 6 , pioglitazone claim 6 , rosiglitazone claim 6 , exenatide claim 6 , miglitol claim 6 , vildagliptin claim 6 , sitagliptin claim 6 , repaglinide claim 6 , nateglinide or mitiglinide.8. The pharmaceutical composition as claimed in claim 6 ,which comprises, as a further active ingredient, one or more antidiabetics, active hypoglycemic ingredients, HMG-CoA reductase inhibitors, cholesterol absorption inhibitors, PPAR gamma agonists, PPAR alpha agonists, PPAR alpha/gamma agonists, fibrates, MTP inhibitors, bile acid absorption inhibitors, CETP inhibitors, polymeric bile acid adsorbers, LDL receptor inducers, ACAT inhibitors, antioxidants, lipoprotein lipase inhibitors, ATP citrate lyase inhibitors, squalene synthetase inhibitors, lipoprotein(a) antagonists, lipase inhibitors, insulins, sulfonylureas, biguanides, meglitinides, thiazolidinediones, α-glucosidase inhibitors, active ingredients which act on the ATP-dependent potassium channel of the beta cells, CART agonists, NPY agonists, MC4 agonists, orexin antagonists, H3 agonists, TNF agonists, CRF antagonists, CRF BP antagonists, urocortin agonists, β3 agonists, MSH (melanocyte-stimulating hormone) ...

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Номер записи: 54
27-06-2013 дата публикации

PROCESS FOR PREPARATION OF OPTICALLY ACTIVE DIAMINE DERIVATIVE SALT

Номер: US20130165657A1
Автор: Ishikawa Hideaki, Kawanami Koutarou, Shoji Masahiro
Принадлежит: Daiichi Sankyo Company, Limited

The problem to be solved is to produce, at high yields with high purity, anhydrous crystals of a compound represented by formula (1) that is an important intermediate for preparation of FXa inhibitor compound (X) or a pharmacologically acceptable salt thereof, or a hydrate thereof. The solution thereto is an industrial preparation process that provides, with high purity, anhydrous crystals of a compound represented by the following formula (1), which is an intermediate for the production of FXa inhibitor compound (X) or a pharmacologically acceptable salt thereof, or a hydrate thereof, wherein Boc represents a tert-butoxycarbonyl group. 3. The preparation process according to claim 1 , wherein the heating is performed at 50 to 80° C.4. The preparation process according to claim 1 , wherein the heating is performed at 70 to 75° C.5. The preparation process according to claim 1 , wherein the stirring step further comprises distilling off the organic solvent by 1/2 to 4/7 of the total volume of the organic solvent under reduced pressure in the range of 40 to 75° C. and then re-adding an organic solvent in an amount corresponding to the amount distilled off.6. The preparation process according to claim 5 , wherein the water content of the organic solvent is kept at less than 0.2% by weight in the distilling off of the organic solvent under reduced pressure and the re-addition.8. The preparation process according to claim 2 , wherein the hydrous organic solvent is a hydrous organic solvent containing 4% or more water.9. The preparation process according to claim 2 , wherein the hydrous organic solvent is a hydrous organic solvent containing 4 to 10% water.10. The preparation process according to claim 2 , wherein the treatment with anhydrous oxalic acid comprises adding dropwise a solution of anhydrous oxalic acid in an organic solvent.11. The preparation process according to claim 10 , wherein the dropwise addition is performed at 50 to 80° C.12. The preparation process ...

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Номер записи: 55
04-07-2013 дата публикации

EVAPORABLE ORGANIC SEMICONDUCTIVE MATERIAL AND USE THEREOF IN AN OPTOELECTRONIC COMPONENT

Номер: US20130167930A1
Автор: Gerdes Olga, Hildebrandt Dirk, Mattersteig Gunter, Vetter Serge, Weiss André
Принадлежит: HELIATEK GMBH

The invention relates to compounds of general formula IIIa and their use in optoelectronic components. 2. A compound according to claim 1 , wherein said compounds of the formula IIIa have point or mirror symmetry at least in relation to the main chain.11. A compound according to where o and p=0 and W═C—R.14. A compound according to where X═S claim 13 , and Y═S and W═C—R.16. A compound according to claim 15 , where additionally p=0.17. A compound according to wherein R9 and R10 form a 5 membered or 6-membered ring.18. A compound according to claim 1 , in which W is selected from: C(CN) claim 1 , CHCN claim 1 , and R1 and R6 are each selected from: H and CN.194. An optoelectronic component having an electrode and a counterelectrode and at least one organic light-sensitive layer between the electrode and the counterelectrode claim 1 , wherein the organic light-sensitive layer () comprises at least one compound according to .20. (canceled)21. A compound according to wherein R′ is selected from C(CN)and CHCN. The invention relates to an organic semiconductive material of the general formulae I and II, and also IIIa.Research and development in organic solar cells has increased significantly, particularly in the last ten years. The maximum efficiency reported to date for what are called “small molecules” is 5.7% [Jiangeng Xue, Soichi Uchida, Barry P. Rand, and Stephen R. Forrest, Appl. Phys. Lett. 85 (2004) 5757]. Small molecules are understood in the context of the present invention to mean nonpolymeric organic monodisperse molecules in the mass range between 100 and 2000 grams/mol. These have to date been unable to achieve the efficiencies of 10-20% typical of inorganic solar cells. Organic solar cells, however, are subject to the same physical limitations as inorganic solar cells, and therefore, at least theoretically, similar efficiencies are to be expected after corresponding development work.Organic solar cells consist of a sequence of thin layers (each typically of ...

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Номер записи: 56
04-07-2013 дата публикации

OPTOELECTRONIC COMPONENT WITH ORGANIC LAYERS

Номер: US20130167931A1
Автор: Gerdes Olga, Hildebrandt Dirk, Mattersteig Gunter, Pfeiffer Martin, Uhrich Christian, Vetter Serge, Weiss André
Принадлежит:

The present disclosure relates to an optoelectronic component having an electrode (), a counter electrode () and at least one organic light-sensitive layer () between the electrode and counter electrode. The organic light-sensitive layer () contains at least one compound of the general formula EWG (electron withdrawing group)-D (donor block)-EWG with at least one substituent on the extended donor block D. 1. An optoelectronic component having an electrode and a counterelectrode and at least one organic light-sensitive layer between the electrode and the counterelectrode , said layer comprising a compound EWG-D-EWG as the main component , in which EWG has electron-withdrawing properties with respect to the extensive donor block D , wherein the extensive donor block D has not more than 9 conjugated double bonds in linear succession and is formed from heterocyclic 5-membered rings and/or from vinylene and/or systems of the same type or mixed types which are fused thereto , and in that the donor block D has at least one substituent.2. The component according to claim 1 , wherein the heterocyclic 5-membered rings of the extensive donor block D are each independently selected from thiophene claim 1 , selenophene claim 1 , furan and pyrrole and/or from systems of the same kind or mixed kinds fused thereto.3. The component according to claim 1 , wherein the at least one substituent of the extensive donor block D has π electrons claim 1 , for example as a free electron pair or in a multiple bond.4. The component according to claim 1 , wherein the at least one substituent of the extensive donor block D is selected from the group of the ethers claim 1 , thioethers claim 1 , amines claim 1 , or from substituted or unsubstituted aromatics or heteroaromatics having 4 to 10 atoms claim 1 , or from alkenyl having at least one double bond in the α position claim 1 , or claim 1 , in the case of 2 adjacent substituents claim 1 , form a heterocyclic 5- claim 1 , 6- or 7-membered ring.5 ...

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Номер записи: 57
04-07-2013 дата публикации

LIGHT EMITTING ELEMENT, LIGHT EMITTING DEVICE AND ELECTRONIC APPARATUS

Номер: US20130168654A1
Автор: Fujita Tetsuji, Yamamoto Hidetoshi
Принадлежит: SEIKO EPSON CORPORATION

The light emitting element of the embodiment includes an anode; a cathode; a visible light emitting layer provided between the anode and the cathode and emitting visible light; and a carrier trapping layer containing a thiadiazole based compound represented by the following formula (1). 5. The light emitting element according to claim 1 , wherein the carrier trapping layer is positioned at an anode side relative to the light emitting layer.6. The light emitting element according to claim 5 ,wherein the carrier trapping layer further contains a host material in addition to the thiazole based compound, andwherein the host material is at least one type from among amine based material, anthracene based material, and napthacene based material.7. The light emitting element according to claim 1 , wherein the carrier trapping layer is positioned at a cathode side relative to the light emitting layer.8. The light emitting element according to claim 7 ,wherein the carrier trapping layer further contains a host material in addition to the thiazole based compound, andwherein the host material is at least one type from among anthracene based material, napthacene based material, and a quinolinolato based metal complex.9. The light emitting element according to claim 1 , wherein the light emitting layer is a single layer.10. The light emitting element according to claim 9 , wherein the light emitting layer emits a blue luminescent color as visible light.11. The light emitting element according to claim 9 , wherein the light emitting layer emits a yellow luminescent color as visible light.12. The light emitting element according to claim 1 , wherein the light emitting layer is formed of at least two layers.13. A light emitting device comprising the light emitting element according to .14. A light emitting device comprising the light emitting element according to .15. A light emitting device comprising the light emitting element according to .16. A light emitting device comprising ...

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Номер записи: 58
04-07-2013 дата публикации

ORGANOSELENIUM MATERIALS AND THEIR USES IN ORGANIC LIGHT EMITTING DEVICES

Номер: US20130168660A1
Автор: Kwong Raymond, LIN Chun, Ma Bin, Xia Chuanjun
Принадлежит: UNIVERSAL DISPLAY CORPORATION

The present invention provides organoselenium compounds comprising dibenzoselenophene, benzo[b]selenophene or benzo[c]selenophene and their uses in organic light emitting devices. 1. An organic light emitting device , comprising an organic layer positioned between an anode layer and a cathode layer , said organic layer comprising an organoselenium material selected from the group consisting of a compound comprising a dibenzoselenophene , a compound comprising a benzo[b]selenophene , and a compound comprising benzo[c]selenophene.46-. (canceled)73. The organic light emitting device of any of to claims 1 , wherein said organoselenium material is a host material claims 1 , and wherein said organic layer further comprises a dopant material.8. The organic light emitting device of claim 7 , wherein said organic layer is an emissive layer claim 7 , and wherein said dopant material is a phosphorescent or fluorescent dopant material.9. The organic light emitting device of claim 8 , wherein said dopant material is a phosphorescent dopant material.13. The organic light emitting device of claim 9 , further comprising one or more organic layers selected from the group consisting of a hole injecting layer claim 9 , an electron injecting layer claim 9 , a hole transporting layer claim 9 , an electron transporting layer claim 9 , a hole blocking layer claim 9 , an exciton blocking layer claim 9 , and an electron blocking layer.14. The organic light emitting device of claim 13 , wherein said hole transporting layer comprises an organoselenium material.15. The organic light emitting device of claim 13 , wherein said electron transporting layer comprises an organoselenium material.163. The organic light emitting device of any of to claims 1 , wherein said organic layer is a hole transporting layer or an electron transporting layer.17. (canceled)2022-. (canceled) This application claims the benefit under 35 U.S.C. §119(e) of U.S. Provisional Application No. 61/100,229, filed Sep. 25, ...

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Номер записи: 59
04-07-2013 дата публикации

OXYGEN LINKED PYRIMIDINE DERIVATIVES

Номер: US20130172338A1
Автор: Blanchard Stephanie, Lee Cheng Hsia Angeline, Nagaraj Harish Kumar Mysore, Poulsen Anders, SUN Eric T., Tan Yee Ling Evelyn, William Anthony Deodaunia
Принадлежит: CELL THERAPEUTICS, INC.

The present invention relates to pyrimidine compounds that are useful as anti-proliferative agents. More particularly, the present invention relates to oxygen linked and substituted pyrimidine compounds, methods for their preparation, pharmaceutical compositions containing these compounds and uses of these compounds in the treatment of proliferative disorders. These compounds may be useful as medicaments for the treatment of a number of proliferative disorders including tumours and cancers as well as other disorders or conditions related to or associated with kinases. 1138-. (canceled)140. The method according to wherein the one or more protein kinase(s) is a cyclin-dependent protein kinase.141. The method according to wherein the cyclin-dependent kinase is a Group I CMCG kinase.142. The method according to wherein the Group I CMCG kinase is selected from the group consisting of CDC2Hs claim 141 , CDK2 claim 141 , CDK3 claim 141 , CDK4 claim 141 , CDK5 claim 141 , CDK6 claim 141 , CDK9 claim 141 , PCTAIRE1 claim 141 , PCTAIRE2 claim 141 , PCTAIRE3 claim 141 , CAK/MO15 claim 141 , Dm2 claim 141 , Dm2c claim 141 , Ddcdc2 claim 141 , DdPRK claim 141 , LmmCRK1 claim 141 , PfC2R claim 141 , EhC2R claim 141 , CfCdc2R claim 141 , cdc2+ claim 141 , CDC28 claim 141 , PHO85 claim 141 , KIN28 claim 141 , FpCdc2 claim 141 , MsCdc2B claim 141 , and OsC2R or a functional equivalent thereof.143. The method according to wherein the Group I CMCG kinase is CDK2 or a functional equivalent thereof.144. The method according to wherein the condition is selected from the group consisting of prostate cancer claim 139 , retinoblastoma claim 139 , malignant neoplasm of breast claim 139 , malignant tumour of colon claim 139 , endometrial hyperplasia claim 139 , osteosarcoma claim 139 , squamous cell carcinoma claim 139 , non-small cell lung cancer claim 139 , melanoma claim 139 , liver cell carcinoma claim 139 , malignant neoplasm of pancreas claim 139 , myeloid leukemia claim 139 , cervical ...

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Номер записи: 60
04-07-2013 дата публикации

Pyrrolopyrrole derivatives, their manufacture and use

Номер: US20130172575A1
Автор: AEBISCHER OLIVER FREDERIC, BIENEWALD FRANK, BUDRY JEAN-LUC, Duggeli Mathias, FONDRODONA TURON MARTA, Fontana Margherita, HAO ZHIMIN, Hayoz Pascal, Schmidhalter Beat, TURBIEZ MATHEIU G.R.
Принадлежит: BASF SE

The present invention relates to compounds of the formula I 9. A semiconductor device according to comprising as a semiconducting effective means a compound of the formula I as defined in with the proviso that at least one of R , R , R , Rand Ris different from hydrogen.10. A semiconductor device according to in the form of a diode claim 8 , a photodiode claim 8 , a sensor claim 8 , an organic field effect transistor claim 8 , a transistor for flexible displays claim 8 , or a heterojunction solar cell.11. A p-type transistor comprising the compound of formula I as defined in . The present invention relates to 1,4-diketopyrrolo[3,4-c]pyrrole (DPP) derivatives of the below formula I, wherein the substituents are as defined herein below, to their manufacture; to their use as organic semiconductors, e.g. in semiconductor devices, especially a sensor, a diode, a photodiode, an organic field effect transistor, a transistor for flexible displays, and/or a solar cell (photovoltaic cell); to such semiconductor devices comprising diketopyrrolopyrrol derivatives of the formula I as a semiconducting effective means, and to devices containing said semiconductor devices.JP 2006117591-A to Toyo Ink Manufacturing Co. discloses diketopyrrolopyrrol derivatives for use in organic electroluminescent elements, like flat panel displays and liquid crystal displays, but not for use as organic semiconductors.WO 2004/090046 A1 to Ciba discloses fluorescent diketopyrrolopyrrol (DPP) derivatives, mainly for use in inks, toners, colorants, pigmented plastics, color changing media, solid dye lasers and electroluminescent devices. Said DPP derivatives have a smaller or shorter side chain on both sides of the diketopyrrolopyrrol moiety than the diketopyrrolopyrrol derivatives claimed per se in the present specification. In addition, specifically disclosed, i.e. individualized, compounds include only those derivatives wherein the DPP nitrogen atoms are substituted by alkyl groups having no more ...

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Номер записи: 61
11-07-2013 дата публикации

BENZO-FUSED THIOPHENE / TRIPHENYLENE HYBRID MATERIALS

Номер: US20130175510A1
Автор: Kwong Raymond, LIN Chun, Ma Bin, WU Yonggang
Принадлежит: UNIVERSAL DISPLAY CORPORTION

Triphenylene containing benzo-fused thiophene compounds are provided. Additionally, triphenylene containing benzo-fused furan compounds are provided. The compounds may be useful in organic light emitting devices, particularly as hosts in the emissive layer of such devices, or as materials for enhancement layers in such devices, or both. 1. A compound comprising a triphenylene containing benzo-fused thiophene or benzo-fused furan , wherein any substituent in the compound is an unfused substituent independently selected from the group consisting of CH , OCH , OAr , N(CH) , N(Ar)(Ar) , CH═CH—CH , C≡CHCH , Ar , Ar—Ar , CH—Ar , or no substitution , wherein n is 1 , 2 , 3 , 4 , 5 , 6 , 7 , 8 , 9 , or 10 , and wherein Arand Arare independently selected from the group consisting of benzene , biphenyl , naphthalene , triphenylene , carbazole , and heteroaromatic analogs thereof.3. The compound of claim 2 , wherein X is S.4. The compound of claim 2 , wherein X is O.6. The compound of claim 5 , wherein X is S.7. The compound of claim 5 , wherein X is O.9. The compound of claim 8 , wherein X is S.10. The compound of claim 8 , wherein X is O.12. The compound of claim 11 , wherein X is S.13. The compound of claim 11 , where X is O.1419-. (canceled)20. The compound of claim 1 , wherein Arand Arare independently selected from the group consisting of benzene claim 1 , biphenyl claim 1 , naphthalene claim 1 , triphenylene claim 1 , and carbazole.21. An organic light emitting device claim 1 , comprising:an anode;a cathode; and{'sub': n', '2n+1', 'n', '2n+1', '1', 'n', '2n+1', '2', '1', '2', 'n', '2n+1', 'n', '2n+1', '1', '1', '2', 'n', '2n', '1', '1', '2, 'an organic layer disposed between the anode and the cathode, wherein the organic layer comprises a compound comprising a triphenylene containing benzo-fused thiophene or benzo-fused furan, wherein any substituent in the compound is an unfused substituent independently selected from the group consisting of CH, OCH, OAr, N(CH), N(Ar)( ...

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Номер записи: 62
11-07-2013 дата публикации

SYNTHESIS OF 4H-BENZO[D]PYRROLO[1,2-A]THIAZOLES AND INDOLIZINO[6,7-b]INDOLE DERIVATIVES AND THEIR USE AS ANTITUMOR THERAPEUTIC AGENTS

Номер: US20130178629A1
Автор: Chou Ting-Chao, Lee Te-Chang, Su Tsann-Long
Принадлежит: Academia Sinica

The present invention provides a series of 2,3-bis(hydroxymethyl)-4H-benzo[d]pyrrolo-[1,2-a]thiazoles and 1,2-bis(hydroxymethyl)indolizino[6,7-b]indole derivatives and their bis(alkylcarbamates) derivatives. These derivatives were designed as bi-functional DNA cross-linking agents. The in vitro cytotoxicity study of these compounds revealed that they exhibit significant anti-proliferative activity in inhibiting human lymphoblastic leukemia and various solid tumor cell growth. The compounds also exhibit therapeutic efficacy against human breast carcinoma and lung cancer in xenograft model. The compounds generally possess potent antitumor activity to kill various human solid tumors and have high potential for clinical applications. 2. The compound of wherein the unsubstituted or substituted aryl group is selected from the group consisting of unsubstituted or substituted phenyl claim 1 , naphthyl claim 1 , pyrenyl claim 1 , anthryl claim 1 , phenanthryl claim 1 , furyl claim 1 , pyrrolyl claim 1 , thienyl claim 1 , oxazoyl claim 1 , imidazoyl claim 1 , thiazoyl claim 1 , pyridyl claim 1 , pyrimidinyl claim 1 , quinazolinyl and indolyl.3. The compound of wherein the substituent of the aryl or benzyl is selected from the group consisting of C-Calkyl claim 1 , OR; halo claim 1 , cyano claim 1 , nitro claim 1 , NH claim 1 , NHR claim 1 , N(R) claim 1 , a C-Ccyclic alkylamino group claim 1 , a methylenedioxy and ethylenedioxy group; wherein Ris hydrogen or C-Calkyl claim 1 , and Ris hydrogen or C-Calkyl.4. The compound of that is selected from the group consisting of(1-Methylbenzo[d]pyrrolo[2,1-b]thiazole-2,3-diyl)dimethanol;(1-(4-Fluorophenyl)benzo[d]pyrrolo[2,1-b]thiazole-2,3-diyl)dimethanol;(1-(4-Chlorophenyl)benzo[d]pyrrolo[2,1-b]thiazole-2,3-diyl)dimethanol;(1-(3,4-Difluorophenyl)benzo[d]pyrrolo[2,1-b]thiazole-2,3-diyl)dimethanol;(1-(3,4-Dichlorophenyl)benzo[d]pyrrolo[2,1-b]thiazole-2,3-diyl)dimethanol;(1-(3-Chloro-4-fluorophenyl)benzo[d]pyrrolo[2,1-b]thiazole-2,3-diyl ...

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Номер записи: 63
18-07-2013 дата публикации

Herbicidal Benzoxazinones

Номер: US20130184155A1
Автор: EVANS Richard Roger, NEWTON Trevor William, SEITZ Thomas, SIMON Anja, Walter Helmut, WITSCHEL Matthias
Принадлежит:

The present invention provides benzoxazinones of formula I 19-. (canceled)11. The compound of claim 10 , wherein Ris halogen.12. The compound of claim 10 , wherein Ris C-C-alkynyl or C-C-haloalkynyl.13. The compound of claim 10 , wherein Y is Y claim 10 , Yor Y.14. A herbicidal composition comprising a herbicidal active amount of a compound of and at least one further active compound selected from the group of the herbicides B and/or safeners C.15. The composition according to comprising at least two further active compounds selected from the group of the herbicides B and/or safeners C.16. The composition according to further comprising at least one inert liquid and/or solid carrier and claim 15 , if appropriate claim 15 , at least one surface-active substance.17. The composition of wherein Ris halogen.18. The composition of wherein Ris C-C-alkynyl or C-C-haloalkynyl.19. The composition of wherein Y is Y claim 15 , Yor Y.20. A herbicidal composition comprising a herbicidal active amount of a compound of and at least one inert liquid and/or solid carrier and claim 10 , if appropriate claim 10 , at least one surface-active substance.21. A process for the preparation of herbicidal active compositions claim 10 , which comprises mixing a herbicidal active amount of a compound of and at least one inert liquid and/or solid carrier and claim 10 , if desired claim 10 , at least one surface-active substance.22. A method of controlling undesired vegetation claim 10 , which comprises allowing a composition comprising a herbicidal active amount of a compound of to act on plants claim 10 , their environment or on seed.23. The method of claim 22 , wherein the composition further comprises at least two further active compounds selected from the group of the herbicides B and/or safeners C.24. The method of claim 23 , wherein the composition further comprises at least one inert liquid and/or solid carrier and claim 23 , if appropriate claim 23 , at least one surface-active substance. ...

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Номер записи: 64
18-07-2013 дата публикации

HETEROCYCLIC COMPOUND AND USE THEREOF

Номер: US20130184266A1
Автор: ASANO Yasutomi, Honda Eiji, IMAEDA Toshihiro, KORI Masakuni, Mochizuki Michiyo, Nakamura Shinji, TOYOFUKU Masashi, Ujikawa Osamu
Принадлежит: Takeda Pharmaceutical Company Limited

Provided is a compound represented by the formula (I): 123-. (canceled)24. 9-[4-(Cyclohexyloxy)phenyl]-7-methyl-3 ,4-dihydropyrazino[2 ,1-c][1 ,2 ,4]thiadiazine 2 ,2-dioxide or a pharmaceutically acceptable salt thereof.25. A medicament comprising 9-[4-(cyclohexyloxy)phenyl]-7-methyl-3 ,4-dihydropyrazino[2 ,1-c][1 ,2 ,4]thiadiazine 2 ,2-dioxide or a pharmaceutically acceptable salt thereof and a pharmaceutically acceptable carrier. The present invention relates to a heterocyclic compound, particularly a heterocyclic compound having an AMPA (α-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid) receptor potentiating action.Glutamate is the most abundant excitatory neurotransmitter in the mammalian central nervous system. Glutamate plays a pivotal role in cognition, mood, and motor function, and its neurotransmission becomes unstable in psychiatric diseases and neurological disorder. Glutamate receptors are divided into ligand gated ion channels and G protein-coupled receptors, and the ligand gated ion channels are further divided into α-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid (AMPA) receptors, N-methyl-D-aspartic acid (NMDA) receptors, and kainic acid (KA) receptors. (non-patent document 1)AMPA receptor is one kind of receptor for excitatory neurotransmitter glutamate, and was named for the selective activation of the receptor by AMPA. AMPA receptors are composed of 4 subunits (GluR1, GluR2, GluR3, GluR4). Each subunit exists in flip and flop alternatively spliced variants. AMPA receptors form homo- or hetero-tetramers composed of these subunits in vivo. The physiological property of AMPA receptor has been reported to change depending on the subunit composition. (non-patent documents 1, 2, 3)The importance of AMPA receptor in cerebrophysiology is well known, and a compound having an AMPA receptor potentiating action is expected to be useful as a prophylactic or therapeutic drug for psychiatric diseases, neurodegenerative diseases, cognitive disorders, ...

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Номер записи: 65
18-07-2013 дата публикации

NITROGENATED AROMATIC COMPOUND, ORGANIC SEMICONDUCTOR MATERIAL, AND ORGANIC ELECTRONIC DEVICE

Номер: US20130184458A1
Автор: Hotta Masanori, Matsumoto Megumi, Sawada Yuichi
Принадлежит:

Provided are a novel nitrogen-containing aromatic heterocyclic compound and an organic electronic device using the compound. This nitrogen-containing aromatic compound is represented by the general formula (1). Further, the present invention relates to organic electronic devices such as a light-emitting device, a thin-film transistor, and a photovoltaic device each using the nitrogen-containing aromatic compound. 2. A nitrogen-containing aromatic compound according to . claim 1 , wherein the n in the general formula (1) represents 0.3. A nitrogen-containing aromatic compound according to claim 1 , wherein the X's in the general formula (1) each represent N-A.4. A compound according to claim 1 , wherein the m in the general formula (1) represents 2 or 3.5. An organic semiconductor material claim 1 , comprising the nitrogen-containing aromatic compound according to .6. An organic semiconductor thin film claim 5 , which is formed of the organic semiconductor material according to .7. An organic electronic device claim 5 , which is obtained by using the organic semiconductor material according to .8. An organic electronic device according to claim 7 , wherein the organic electronic device is selected from a light-emitting device claim 7 , a thin-film transistor claim 7 , and a photovoltaic device.9. An organic electronic device according to claim 8 , wherein the light-emitting device comprises an organic electroluminescence device.10. An organic semiconductor material claim 2 , comprising the nitrogen-containing aromatic compound according to .11. An organic semiconductor material claim 3 , comprising the nitrogen-containing aromatic compound according to .12. An organic semiconductor material claim 4 , comprising the nitrogen-containing aromatic compound according to .13. An organic semiconductor thin film claim 10 , which is formed of the organic semiconductor material according to .14. An organic semiconductor thin film claim 11 , which is formed of the organic ...

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Номер записи: 66
25-07-2013 дата публикации

MESOIONIC PYRIDO [1, 2-A] PYRIMIDINE PESTICIDES

Номер: US20130190171A1
Автор: JR. Thomas Francis, Pahutski
Принадлежит: E I DU PONT DE NEMOURS AND COMPANY

Disclosed are compounds of Formula 1, 2. A compound of wherein{'sup': 1', '2, 'Ris phenyl optionally substituted with Q and up to 3 substituents independently selected from R; and'}{'sub': 1', '4', '1', '4', '1', '4', '1', '4, 'Q is phenyl or pyridinyl, each optionally substituted with up to 3 substituents independently selected from the group consisting of halogen, cyano, C-Calkyl, C-Chaloalkyl, C-Calkoxy and C-Chaloalkoxy.'}3. A compound of wherein{'sup': '1', 'sub': 1', '4', '1', '4', '1', '4', '1', '4, 'Ris phenyl optionally substituted with up to 3 substituents independently selected from the group consisting of halogen, C-Calkyl, C-Chaloalkyl, C-Calkoxy and C-Chaloalkoxy.'}4. A compound of that is selected from the group consisting of:2-hydroxy-4-oxo-3-phenyl-1-(5-pyrimidinylmethyl)-4H-pyrido[1,2-a]pyrimidinium inner salt;3-(4-fluorophenyl)-2-hydroxy-4-oxo-1-(5-pyrimidinylmethyl)-4H-pyrido[1,2-a]pyrimidinium inner salt;2-hydroxy-4-oxo-1-(5-pyrimidinylmethyl)-3-[3-(trifluoromethyl)phenyl]-4H-pyrido[1,2-a]pyrimidinium inner salt;2-hydroxy-3-(2-methoxyphenyl)-4-oxo-1-(5-pyrimidinylmethyl)-4H-pyrido[1,2-a]pyrimidinium inner salt;2-hydroxy-3-(3-methoxyphenyl)-4-oxo-1-(5-pyrimidinylmethyl)-4H-pyrido[1,2-a]pyrimidinium inner salt;3-(2,4-difluorophenyl)-2-hydroxy-4-oxo-1-(5-pyrimidinylmethyl)-4H-pyrido[1,2-a]pyrimidinium inner salt;2-hydroxy-4-oxo-1-(5-pyrimidinylmethyl)-3-[3-(trifluoromethoxy)phenyl]-4H-pyrido[1,2-a]pyrimidinium inner salt;3-(2-bromophenyl)-2-hydroxy-4-oxo-1-(5-pyrimidinylmethyl)-4H-pyrido[1,2-a]pyrimidinium inner salt;3-(2-fluorophenyl)-2-hydroxy-4-oxo-1-(5-pyrimidinylmethyl)-4H-pyrido[1,2-a]pyrimidinium inner salt;3-[2-fluoro-5-(trifluoromethyl)phenyl]-2-hydroxy-4-oxo-1-(5-pyrimidinylmethyl)-4H-pyrido[1,2-a]pyrimidinium inner salt;2-hydroxy-3-(3-methylphenyl)-4-oxo-1-(5-pyrimidinylmethyl)-4H-pyrido[1,2-a]pyrimidinium inner salt;3-[4-fluoro-3-(trifluoromethyl)phenyl]-2-hydroxy-4-oxo-1-(5-pyrimidinylmethyl)-4H-pyrido[1,2-a]pyrimidinium inner salt (i. ...

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Номер записи: 67
25-07-2013 дата публикации

NEMATOCIDAL SULFONAMIDES

Номер: US20130190172A1
Автор: JR. Thomas Francis, Lahm George Philip, Pahutski
Принадлежит: E I DU PONT DE NEMOURS AND COMPANY

Disclosed are compounds of Formula 1, N-oxides, and salts thereof, 2. A compound of wherein:Z is O; and{'sup': 4', '5', '6', '7', '8', '11', '12', '9', '11', '12', '7', '10', '7, 'sub': 1', '6', '1', '6', '2', '6', '2', '6', '2', '6', '2', '6', 'm', '2, 'Q is phenyl or a 5- or 6-membered heteroaromatic ring, each optionally substituted with 1 to 3 substituents independently selected from the group consisting of halogen, cyano, nitro, OR, NRR, C-Calkyl, C-Chaloalkyl, C-Calkenyl, C-Chaloalkenyl, C-Calkynyl, C-Chaloalkenyl, C(X)R, C(O)OR, C(X)NRR, S(O)R, S(O)NRR, OC(O)Rand N(R)C(O)R.'}3. A compound of wherein:{'sup': 4', '5', '6', '7', '8', '11', '12', '9', '11', '12', '7', '10', '7, 'sub': 1', '6', '1', '6', '2', '6', '2', '6', '2', '6', '2', '6', 'm', '2, 'Q is phenyl, pyridinyl, pyrazolyl, oxazolyl, thiazolyl, isoxazolyl, isothiazolyl, furanyl or thienyl, each optionally substituted with 1 to 3 substituents independently selected from the group consisting of halogen, cyano, nitro, OR, NRR, C-Calkyl, C-Chaloalkyl, C-Calkenyl, C-Chaloalkenyl, C-Calkynyl, C-Chaloalkynyl, C(X)R, C(O)OR, C(X)NRR, S(O)R, S(O)NRR, OC(O)Rand N(R)C(O)R.'}4. A compound of or wherein:{'sup': 1', '4, 'sub': 1', '6', '1', '6, 'each Ris independently halogen, cyano, nitro, OR, C-Calkyl or C-Chaloalkyl;'}{'sup': '2', 'sub': 1', '6, 'Ris H, halogen or C-Calkyl; and'}{'sup': 3', '7', '8', '9, 'sub': m', '1', '6, 'Ris H, C(X)R, C(O)ORor S(O)R; or C-Calkyl optionally substituted with 1 to 4 substituents independently selected from halogen.'}5. A compound of that is selected from the group consisting of:N-[(2-chloro-5-methoxyphenyl)sulfonyl]-6-(trifluoromethyl)imidazo[1,2-a]pyrazine-2-carboxamide;6-bromo-N-[[2-chloro-5-(trifluoromethyl)phenyl]sulfonyl]imidazo[1,2-a]pyrimidine-2-carboxamide; andN-[[2-chloro-5-(trifluoromethyl)phenyl]sulfonyl]-6-(trifluoromethyl)imidazo[1,2-a]pyrimidine-2-carboxamide.6. A composition comprising a compound of and at least one additional component selected from the group ...

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Номер записи: 68
25-07-2013 дата публикации

USE OF ALS INHIBITOR HERBICIDES FOR CONTROL OF UNWANTED VEGETATION IN ALS INHIBITOR HERBICIDE TOLERANT BETA VULGARIS PLANTS

Номер: US20130190179A1
Автор: Donn Guenter, Hain Ruediger, Johann Gerhard
Принадлежит: Bayer Intellectual Property GmbH

The present invention relates generally to the use of biological or chemical control agents with for controlling insects and nematodes and to methods particularly useful for combating insects or nematodes and/or increasing crop yield in plants that are at least partially resistant to one or more parasitic nematodes or insects. 1Beta vulgarisBeta vulgaris. An ALS inhibitor herbicide capable of being used for controlling unwanted vegetation in a growing area in which the plant comprises a mutation in codon 1705-1707 of an endogenous ALS gene encoding an ALS protein containing an amino acid that is different from tryptophan at position 569.3. The ALS inhibitor herbicide according to claim 1 , wherein the ALS herbicide belongs to the group comprising: amidosulfuron [CAS RN 120923-37-7] (=A1-1);chlorimuron-ethyl [CAS RN 90982-32-4] (=A1-4);ethametsulfuron-methyl [CAS RN 97780-06-8] (=A1-8);ethoxysulfuron [CAS RN 126801-58-9] (=A1-9);flupyrsulfuron-methyl-sodium [CAS RN 144740-54-5] (=A1-12); foramsulfuron [CAS RN 173159-57-4] (=A1-13);iodosulfuron-methyl-sodium [CAS RN 144550-36-7] (=A1-16);mesosulfuron-methyl [CAS RN 208465-21-8] (=A1-17);metsulfuron-methyl [CAS RN 74223-64-6] (=A1-18);monosulfuron [CAS RN 155860-63-2] (=A1-19);nicosulfuron [CAS RN 111991-09-4] (=A1-20);sulfosulfuron [CAS RN 141776-32-1] (=A1-28);thifensulfuron-methyl [CAS RN 79277-27-3] (=A1-29);tribenuron-methyl [CAS RN 101200-48-0] (=A1-31);2-iodo-N-[(4-methoxy-6-methyl-1,3,5-triazinyl)carbamoyl]benzene-sulfonamide (=A1-39);2-iodo-N-[(4-methoxy-6-methyl-1,3,5-triazinyl)carbamoyl]benzene-sulfonamide sodium salt (=A1-41);(A1-83) or its sodium salt (=A1-87);propoxycarbazone-sodium [CAS RN 181274-15-7] (=A2-2);thiencarbazone-methyl [CAS RN 317815-83-1] (=A2-3);florasulam [CAS RN 145701-23-1] (=A3-3);metosulam [CAS RN 139528-85-1] (=A3-5);pyroxsulam [CAS RN 422556-08-9] (=A3-7)(A4-1);(A4-2);(A4-3);imazamox [CAS RN 114311-32-9] (=B1-2); and/orbispyribac-sodium [CAS RN 125401-92-5] (=C1-1).4. The ALS ...

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Номер записи: 69
25-07-2013 дата публикации

HETEROCYCLIC COMPOUND AND USE THEREOF

Номер: US20130190291A1
Автор: ASANO Yasutomi, Honda Eiji, IMAEDA Toshihiro, KORI Masakuni, Mochizuki Michiyo, Nakamura Shinji, TOYOFUKU Masashi, Ujikawa Osamu
Принадлежит: Takeda Pharmaceutical Company Limited

Provided is a compound represented by the formula (I): 5. The compound according to claim 2 , wherein L is a bond claim 2 , or a salt thereof.6. The compound according to claim 2 , wherein ring D is an optionally substituted 3-8-membered monocyclic non-aromatic hydrocarbon ring claim 2 , an optionally substituted 6-14-membered aromatic hydrocarbon ring claim 2 , an optionally substituted 6-14-membered non-aromatic hydrocarbon ring claim 2 , an optionally substituted 5-6-membered monocyclic aromatic heterocycle claim 2 , an optionally substituted 3-8-membered monocyclic non-aromatic heterocycle claim 2 , an optionally substituted 8-14-membered condensed aromatic heterocycle or an optionally substituted 6-14-membered condensed non-aromatic heterocycle claim 2 , or a salt thereof.7. The compound according to claim 2 , wherein ring D is{'sub': '3-7', 'optionally substituted Ccycloalkane,'}{'sub': '6-14', 'optionally substituted Carene,'}optionally substituted dihydronaphthalene,optionally substituted tetrahydronaphthalene,optionally substituted dihydroinden,optionally substituted thiophene,optionally substituted azetidine,optionally substituted piperidine,optionally substituted furan,optionally substituted pyridine,optionally substituted pyrazole,optionally substituted 1,2,4-oxadiazole,optionally substituted dihydrobenzodioxin,optionally substituted dihydrobenzofuran,optionally substituted benzodioxole,optionally substituted benzofuran,optionally substituted indole,optionally substituted quinoline,optionally substituted benzimidazole,optionally substituted benzothiazole,optionally substituted indazole, oroptionally substituted dibenzothiophene,or a salt thereof.8. The compound according to claim 2 , wherein ring D is Ccycloalkane claim 2 , Carene claim 2 , dihydronaphthalene claim 2 , tetrahydronaphthalene claim 2 , dihydroinden claim 2 , thiophene claim 2 , azetidine claim 2 , piperidine claim 2 , furan claim 2 , pyridine claim 2 , pyrazole claim 2 , 1 claim 2 ,2 claim ...

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Номер записи: 70
25-07-2013 дата публикации

Compositions Containing a Pyripyropene Insecticide and an Adjuvant

Номер: US20130190360A1
Автор: Anspaugh Douglas D., Benton Kara, BERGHAUS Rainer, Ch. Kierkus Paul, Dieleman Cedric, Fletcher William Maurice, Levy Tatjana, Neese Paul, Saxell Heidi Emilia, Weishaar Walter, Xu Wen
Принадлежит: BASF SE

Pesticidal composition containing a pyripyropene insecticide and an adjuvant 139-. (canceled)41. The composition according to claim 40 , wherein the pyripyropene pesticide is the pesticide of formula I.42. The composition according to claim 40 , wherein the surfactant which carries at least one poly-C-C-alkyleneoxide moiety is selected from polyethoxylated sorbitan fatty acid esters claim 40 , poly(ethyleneoxide-co-propylenoxide) copolymers and poly-C-C-alkyleneoxide modified polydimethylsiloxanes.43. The composition according to claim 40 , wherein the adjuvant comprises a silicone-based adjuvant.44. The composition according to claim 40 , wherein the silicone-based adjuvant comprises a poly-C-C-alkyleneoxide modified polydimethylsiloxane.45. The composition according to claim 40 , wherein the adjuvant comprises a crop oil concentrate.46. The composition according to claim 40 , wherein the crop oil concentrate contains at least one hydrocarbon solvent and at least one non-ionic surfactant.47. The composition according to claim 40 , wherein the adjuvant comprises an alkoxylated aliphatic alcohol.48. The composition according to claim 47 , wherein the alkoxylated aliphatic alcohol is selected from alkoxylates of the formula (A){'br': None, 'sup': a', 'b, 'sub': m', '2m', 'x', 'n', '2n', 'y', 'p', '2p', 'z, 'R—O—(CHO)—(CHO)—(CHO)—R\u2003\u2003(A)'}in which{'sup': 'a', 'sub': 5', '36', '5', '36, 'Rrepresents C-C-alkyl, C-C-alkenyl or a mixture thereof;'}{'sup': 'b', 'sub': 1', '12, 'Rrepresents H or C-C-alkyl;'}m,n,p represent, independently of one another, an integer from 2 to 16;x, y, z represent, independently of one another, a number from 0 to 100; andx+y+z corresponds to a value from 1 to 100.49. The composition according to claim 48 , wherein Rrepresents a linear C-C-alkyl claim 48 , C-C-alkenyl claim 48 , or a mixture thereof.50. The composition according to claim 48 , wherein Rrepresents a linear C-C-alkyl claim 48 , C-C-alkenyl claim 48 , or a mixture thereof. ...

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Номер записи: 71
01-08-2013 дата публикации

ORGANIC ELECTROLUMINESCENT ELEMENT

Номер: US20130193429A1
Автор: Hotta Masanori, Matsumoto Megumi, Sawada Yuichi
Принадлежит:

Provided are a novel nitrogen-containing aromatic heterocyclic compound and an organic electronic device using the compound. Specifically provided is an organic electroluminescent device, including a plurality of organic layers between an anode and a cathode laminated on a substrate, in which at least one of the organic layers contains a nitrogen-containing aromatic compound represented by the following formula (1). In the formula, L represents an n+m-valent group arising from an alkane, a cycloalkane, an aromatic hydrocarbon, an aromatic heterocyclic compound, a triarylamine, or a diarylsulfone, A represents an alkyl group, a cycloalkyl group, an alkenyl group, an alkynyl group, a silyl group, an acyl group, an aromatic hydrocarbon group, or an aromatic heterocyclic group, X represents C(R), oxygen, S, or Se, R represents H, an alkyl group, a cycloalkyl group, an alkenyl group, an alkynyl group, an aromatic hydrocarbon group, or an aromatic heterocyclic group, m represents an integer of 1 to 4, and n represents an integer of 0 to 3. The total number of m and n is 2 to 4. 3. An organic electroluminescent device according to claim 2 , wherein p in the general formula (2) represents 2 or 3.4. An organic electroluminescent device according to claim 1 , wherein the layer which contains the compound represented by the general formula (1) comprises at least one layer selected from the group consisting of a light-emitting layer claim 1 , a hole-transporting layer claim 1 , and an electron-blocking layer.5. An organic electroluminescent device according to claim 4 , wherein the layer which contains the compound represented by the general formula (1) comprises a light-emitting layer containing a phosphorescent light-emitting dopant.6. An organic electroluminescent device according to claim 2 , wherein the layer which contains the compound represented by the general formula (1) comprises at least one layer selected from the group consisting of a light-emitting layer claim 2 , ...

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Номер записи: 72
01-08-2013 дата публикации

Cannabinoid Receptor Agonists

Номер: US20130196960A1
Автор: Carey Galen John, Kim Charles, Nakai Takashi, Rohde Jason
Принадлежит: Ironwood Pharmaceuticals, Inc.

The present disclosure relates to compounds useful as agonists of cannabinoid receptors. The disclosure also provides pharmaceutically acceptable compositions comprising the compounds of the disclosure and methods of using the compositions in the treatment of various disorders either alone or in combination therapy. The compounds have Formula (I), or are pharmaceutically acceptable salts thereof: 2. The compound according to claim 1 , wherein V is a Calkylene linker wherein up to two methylene units of said Calkylene linker are optionally and independently replaced by —O— claim 1 , —C(O)— claim 1 , —C(O)O— claim 1 , —N(R)S(O)— claim 1 , —S(O)N(R)— or —S(O)—.3. The compound according to claim 2 , wherein R is hydrogen.4. The compound according to claim 1 , wherein Ris hydrogen claim 1 , a monocyclic 3-8-membered cycloaliphatic ring or a monocyclic 3-8-membered heterocyclyl ring claim 1 , wherein said cycloaliphatic or heterocyclyl ring is optionally and independently substituted with one instance of a Calkyl claim 1 , —OR claim 1 , —C(O)OR claim 1 , —C(O)R claim 1 , —S(O)Ror —SON(R).5. The compound according to claim 4 , wherein Ris hydrogen claim 4 , a monocyclic 3-8-membered cycloaliphatic ring or a monocyclic 3-8-membered heterocyclyl ring claim 4 , herein each said cycloaliphatic or heterocyclyl ring is optionally and independently substituted with one instance of methyl.7. The compound according to claim 1 , wherein Ris selected from hydrogen claim 1 , halogen claim 1 , —CN or Calkyl.8. The compound according to claim 7 , wherein Ris methyl.9. The compound according to claim 1 , wherein Ring A is pyridyl claim 1 , phenyl or a 3-6-membered cycloalkyl ring.10. The compound according to claim 9 , wherein each Ris independently selected from halogen claim 9 , —OR claim 9 , —C(O)OR claim 9 , —C(O)R claim 9 , or a Caliphatic claim 9 , wherein each of said aliphatic groups is optionally and independently substituted with up to 6 instances of R; or two instances of ...

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Номер записи: 73
01-08-2013 дата публикации

NOVEL COMPOUND OF A REVERSE-TURN MIMETIC AND A PRODUCTION METHOD AND USE THEREFOR

Номер: US20130196972A1
Автор: Cho Young-Seok, Chung Jae-Uk, Kang Myoung-Joo, Kim Mi-Jung, Lee Sang-Hak, Lee Yong-Sil, Ma Sang-Ho, Na Young-Jun, Park Woul-Seong
Принадлежит: JW Pharmaceutical Corporation

This invention relates to novel compounds of reverse-turn mimetics, having pyrazino-triazinone as a basic framework, and a method of preparing the same, and the use thereof to treat diseases such as cancer, in particular, acute myeloid leukemia. 2. The compound or pharmaceutically acceptable salt thereof of claim 1 , wherein Ris C-Calkyl group or C-Calkenyl group; and Ris H.3. The compound or pharmaceutically acceptable salt thereof of claim 1 , wherein Ris a methyl group.8. A method of treating cancer comprising administering to a subject in need thereof a pharmaceutical composition comprising a compound or a pharmaceutically acceptable salt thereof according to .9. The method of claim 8 , wherein the cancer is acute myeloid leukemia.10. A method of treating cancer comprising administering to a subject in need thereof an injectable pharmaceutical composition comprising a compound or a pharmaceutically acceptable salt thereof according to .11. The method of claim 10 , wherein the cancer is acute myeloid leukemia.12. A method of preparing the compound of claim 1 , comprising:introducing a cyano group (—CN) to position 3 of indole-7-carbaldehyde;introducing a methyl group and an aminoacetal group to the indole-7-carbaldehyde in which a cyano group (—CN) is introduced;performing stereoselective amidation with Cbz-tyrosine-OtBu and 2-(1-allyl-4-benzylsemicarbazido)acetic acid for the indole-7-carbaldehyde in which a cyano group (—CN), a methyl group and an aminoacetal group are introduced;performing cyclization using formic acid for the amidated compound; andconverting the cyano group (—CN) of the resulting compound into a carboxyl group and then performing amidation.13. A method of preparing the compound of claim 1 , comprising:iodizing indole-7-carbaldehyde so that iodine is introduced to position 3 of the indole-7-carbaldehyde;introducing a methyl group and an aminoacetal group to the indole-7-carbaldehyde in which a iodine is introduced;performing stereoselective ...

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Номер записи: 74
08-08-2013 дата публикации

MITIGATION OF ALTERNATE BEARING

Номер: US20130203596A1
Автор: Lovatt Carol J.
Принадлежит:

Described are compositions and methods to mitigate alternate bearing of perennial crops by use of a natural metabolite. In particular, the present disclosure provides a natural metabolite in the presence or absence of an auxin transport inhibitor to increase floral intensity (flower number) of the return bloom in the spring following the setting of a heavy on-crop to increase the yield of the putative off-crop year and, thus, increase cumulative crop yield. Additionally the present disclosure provides a natural metabolite in combination with one or both of a growth promoting type of plant growth regulator, and a hormone biosynthesis, transport or function inhibiting type of plant growth regulator. 1. A method of mitigating alternate bearing in a perennial crop plant , comprising administering to the perennial crop plant a composition comprising an effective amount of a purified natural compound to mitigate alternate bearing , wherein the natural compound is selected from the group consisting of adenosine , an adenosine phosphate , inosine , an inosine phosphate , adenine , hypoxanthine , xanthine , and combinations thereof.2. The method of claim 1 , wherein the natural compound comprises 9-beta-D-adenosine.3. The method of claim 1 , wherein the natural compound comprises one or more of the group consisting of adenosine monophosphate claim 1 , adenosine diphosphate claim 1 , adenosine triphosphate claim 1 , inosine claim 1 , inosine monophosphate claim 1 , inosine diphosphate claim 1 , inosine triphosphate claim 1 , adenine claim 1 , hypoxanthine claim 1 , and xanthine.44. The method of claim 2 , wherein the composition further comprises a plant growth regulator selected from the group consisting of 6-benzylaminopurine claim 2 , zeatin claim 2 , zeatinriboside claim 2 , kinetin claim 2 , isopentenyladenine claim 2 , isopentenyladenosine claim 2 , 1-(2-chloro-4-pyridynl)-3-phenyluea claim 2 , gibberellic acid claim 2 , 6-benzyladenine claim 2 , 6-benzyladenosine claim ...

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Номер записи: 75
08-08-2013 дата публикации

FUSED HETEROCYCLIC DERIVATIVES AS S1P MODULATORS

Номер: US20130203737A1
Автор: Coolen Hein K.A.C., den Hartog Jacobus A.J., Iwema Bakker Wouter I., Sliedregt Leonardus A.J.M., Smid Pieter, van Dongen Maria J.P.
Принадлежит: AbbVie B.V.

The present invention relates to a fused heterocyclic derivative of the formula (I) 2. The compound of claim 1 , wherein 'a group selected from a (3-6C)cycloalkyl group and a (8-10C)bicyclic group wherein the group is optionally substituted with a halogen atom, (1-4C)alkyl, and a phenyl group wherein the phenyl group is optionally substituted with at least one substituent independently selected from a halogen atom, cyano, (1-4C)alkyl, (1-4C)alkoxy, a trifluoromethyl, and a trifluoromethoxy;', 'R1 is selected from'}{'sub': '2', 'W is selected from a bond, —O—, —CO—, —S—, —SO—, —SO—, —NH—, —CH═CH—, —C≡C—, and a trans-cyclopropylene;'}n is an integer from 0 to 4; andR2 is selected from H and at least one substituent independently selected from a halogen atom, (1-4C)alkyl optionally substituted with at least one fluoro and (1-4C)alkoxy optionally substituted with at least one fluoro atom.5. The compound of claim 1 , wherein Y is O.6. The compound of claim 1 , wherein R4 is selected from —(CH)—COOH claim 1 , —(CH)—COOH claim 1 , —CH—CHCH—COOH claim 1 , —CH—C(CH)—COOH claim 1 , —CHCH—CH—COOH claim 1 , —CH—CF—COOH claim 1 , and 1 claim 1 ,3-cyclobutylene-COOH.7. The compound of claim 1 , wherein R1 is a phenyl group optionally substituted with at least one substituent independently selected from halogen claim 1 , cyano claim 1 , (1-4C)alkyl optionally substituted with at least one halogen atom claim 1 , (1-4C)alkoxy optionally substituted with at least one halogen atom claim 1 , amino claim 1 , dimethylamino claim 1 , and (3-6C)cycloalkyl optionally substituted with a phenyl group wherein the phenyl group is optionally substituted with a substituent selected from (1-4C)alkyl and a halogen atom.8. The compound of claim 7 , wherein R1 is a phenyl group optionally substituted with at least one substituent independently selected from a halogen atom claim 7 , cyano claim 7 , (1-4C)alkyl claim 7 , (1-4C)alkoxy claim 7 , a trifluoromethyl claim 7 , and a trifluoromethoxy.9. The ...

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Номер записи: 76
08-08-2013 дата публикации

FUSED AMINODIHYDROTHIAZINE DERIVATIVES

Номер: US20130203740A1
Автор: Farthing Christopher Neil, Hall Adrian
Принадлежит: Eisai R&D Management Co., Ltd.

The present invention relates to a fused aminodihydrothiazine derivative of formula (I): 15-. (canceled)6. A compound which is N-(3-((4aS ,5S ,7aS)-2-amino-5-(trifluoromethyl)-4-a ,5 ,7 ,7a-tetrahydro-4H-furo[3 ,4-d][1 ,3]thiazin-7a-yl)-4-fluorophenyl)-5-methoxypyrazine-2-carboxamide , or a pharmaceutically acceptable salt thereof.713-. (canceled)14. A pharmaceutical composition comprising the compound according to claim 6 , or a pharmaceutically acceptable salt thereof claim 6 , as an active ingredient in association with a pharmaceutically acceptable carrier.15. (canceled)16. A method of treating Down's syndrome claim 6 , comprising administering to a human subject suffering from Down's syndrome an effective amount of the compound according to claim 6 , or a pharmaceutically acceptable salt thereof.17. A method of treating Alzheimer-type dementia claim 6 , comprising administering to a human subject suffering from Alzheimer-type dementia an effective amount of the compound according to claim 6 , or a pharmaceutically acceptable salt thereof. The present invention relates to a fused aminodihydrothiazine derivative and pharmaceutical use thereof. More particularly, the present invention relates to a fused aminodihydrothiazine derivative which has an amyloid-β (hereinafter referred to as Aβ) protein production inhibitory effect or a beta-site amyloid-β precursor protein cleavage enzyme 1 (hereinafter referred to as BACE1 or beta-secretase) inhibitory effect and is effective for treating a neurodegenerative disease caused by Aβ protein, in particular, Alzheimer-type dementia, Down's syndrome or the like, and to a pharmaceutical composition comprising the fused aminodihydrothiazine derivative as an active ingredient.Alzheimer's disease is a disease characterized by degeneration and loss of neurons as well as formation of senile plaques and neurofibrillary tangles. Currently, only the symptoms of Alzheimer's disease are treated using a symptom-improving agent typified ...

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Номер записи: 77
08-08-2013 дата публикации

PHARMACEUTICAL COMPOSITION COMPRISING A PYRIMIDINEONE DERIVATIVE

Номер: US20130203778A1
Автор: CHAUDHARI Sunil, Dhuppad Ulhas
Принадлежит: Glenmark Pharmaceuticals S.A.

The present patent application relates to a pharmaceutical composition comprising a fused pyrimidineone derivative having transient receptor potential modulating activity and a hydrophilic carrier. 1. A pharmaceutical composition comprising a solid dispersion that includes an active ingredient 7-{(E)-2-[2-(cyclopropylmethoxy)-3-methoxyphenyl]vinyl}-6-(4-trifluoromethoxy-phenyl)-5H-[1 ,3]thiazolo-[3 ,2-a]pyrimidin-5-one (“Compound I”) or its salt; and a hydrophilic carrier.2. (canceled)3. A pharmaceutical composition according to claim 1 , wherein the hydrophilic carrier includes surfactant claim 1 , complexing agent claim 1 , cosolvent claim 1 , polymer and mixtures thereof.4. A pharmaceutical composition according to claim 1 , wherein the hydrophilic carrier is a surfactant selected from poloxamer claim 1 , polyoxyethylene sorbitan ester claim 1 , polyoxyethylene sorbitan ester claim 1 , polyglyceryl-6-dioleate claim 1 , polyethylene glycol 15 hydroxy stearate claim 1 , diethylene glycol monoethyl ether claim 1 , propylene glycol dicaprylocaprate claim 1 , lecithin claim 1 , phospholipid claim 1 , lauroyl macrogolglycerides claim 1 , oleoyl macrogolglycerides claim 1 , and caprylocaproyl macrogolglycerides claim 1 , or mixtures thereof.5. A pharmaceutical composition according to claim 1 , wherein the hydrophilic carrier is a complexing agent selected from alpha-cyclodextrin claim 1 , beta-cyclodextrin claim 1 , gamma-cyclodextrin claim 1 , hydroxypropyl beta-cyclodextrin claim 1 , sulphobutyl ether beta cyclodextrin neutralized poly(acrylic acid) claim 1 , and crosslinked acrylic acid copolymers claim 1 , or mixtures thereof.6. A pharmaceutical composition according to claim 1 , wherein the hydrophilic carrier is a cosolvent selected from ethanol claim 1 , propanol claim 1 , isopropanol claim 1 , propylene glycol claim 1 , polyethylene glycol claim 1 , dichloromethane claim 1 , dimethylisosorbide claim 1 , ethyl lactate claim 1 , N-methylpyrrolidones claim 1 , ...

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Номер записи: 78
08-08-2013 дата публикации

PESTICIDE AND A METHOD OF CONTROLLING A WIDE VARIETY OF PESTS

Номер: US20130203842A1
Автор: Bain Oakford George, DYER Chad Douglas, NEWBERRY George David, Sterzi Dario
Принадлежит: GOWAN COMERCIO INTERNACIONAL E SERVICOS LIMITADA

A pesticidal composition including at least one substance derived from plant, at least one metal salt of a fatty acid and at least one excipient. The present disclosure also relates to a kit including the pesticidal composition. The present disclosure further relates to use of pesticidal composition/kit in controlling a wide variety of pests. 1. A pesticidal composition comprising:{'i': 'Azadirachta indica', 'i. at least one substance derived from plant;'}ii. at least one metal salt of a fatty acid; andiii. at least one excipient.2Azadirachta indica. The pesticidal composition as claimed in claim 1 , wherein the substance is selected from the group comprising powder claim 1 , extract and oil derived from plant material and azadirachtins.3. The pesticidal composition as claimed in claim 1 , wherein the metal salt of a fatty acid is at least one selected from the group consisting of a potassium salt of a fatty acid claim 1 , a sodium salt of a fatty acid claim 1 , a calcium salt of a fatty acid claim 1 , a magnesium salt of a fatty acid claim 1 , an aluminium salt of a fatty acid and a manganese salt of a fatty acid claim 1 , preferably claim 1 , a potassium salt of a fatty acid.4Azadirachta indica. The pesticidal composition as claimed in claim 1 , wherein the proportion of the substance derived from plant and the metal salt of a fatty acid ranges between 3000:1 and 1:3000 claim 1 , preferably 100:1 and 1:100 and most preferably 50:1 and 1:50.5. The pesticidal composition as claimed in claim 1 , wherein the amount of the metal salt of a fatty acid ranges between 0.01 w/w % and 30.0 w/w %.6. The pesticidal composition as claimed in claim 1 , further comprises at least one oil selected from the group consisting of isopropyl myristate claim 1 , myristyl myristate claim 1 , isopropyl palmitate claim 1 , isopropyl stearate claim 1 , isopropyl oleate claim 1 , n-butyl stearate claim 1 , n-hexyl laurate claim 1 , n-decyl oleate claim 1 , isooctyl stearate claim 1 , isononyl ...

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Номер записи: 79
15-08-2013 дата публикации

Use of 6- substituted 9 - halogenalkyl purines for regulation of growth and development of whole plants, plant cells and plant organs; novel 6 - substituted 9 - halogenalkyl purines

Номер: US20130210632A1
Автор: Jiri Gruz, Karel Dolezal, Lucie Szucova, Lukas Spichal, Miroslav Strnad, Petr Galuszka, Vaclav Mik
Принадлежит: Palackeho Univerzita v Olomouci

The invention relates to 6-substituted 9-halogenalkyl purine derivatives of the general formula I wherein R6 is selected from the group comprising —NH-furfuryl, —NH-(4-hydroxy-3-methylbut-2-en-1-yl), —NH-(3-methylbut-2-en-1-yl), —NH-(4-hydroxy-3-methylbutyl), —NH-(4-hydroxy-1,3-dimethylbut-2-en-1-yl), —NH-(4-hydroxy-1,3-dimethylbutyl), —NH-benzyl, —NH-phenyl, wherein benzyl, furfuryl and phenyl can be unsubstituted or optionally substituted with 1 to 3 substituents selected from the group comprising hydroxy, halogen, methyl and methoxy, and R9 is selected from the group comprising C 1 -C 3 alkyl or C 1 -C 3 alkenyl wherein each of the groups is substituted with one or more halogen atoms, for use in the regulation of growth and development of plant cells, organs and/or whole plants. The invention also relates to preparations containing these derivatives and to novel to 6-substituted 9-halogenalkyl purines.

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Номер записи: 80
15-08-2013 дата публикации

POSITIVE ALLOSTERIC MODULATORS OF MGLUR2

Номер: US20130210768A1
Автор: Arrington Kenneth L., Dudkin Vadim, Layton Mark E., Pero Joseph E., Reif Alexander J.
Принадлежит:

The present invention is directed to 5-substituted 1,3-dihydro-2H-imidazo[4,5-b]pyridine-2-one derivatives which are positive allosteric modulators of the mGluR2 receptor, useful in the treatment or prevention of neurological and psychiatric disorders associated with glutamate dysfunction and diseases in which the mGluR2 receptor is involved. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which metabotropic glutamate receptors are involved, such as schizophrenia. 2. The compound according to wherein Y is methyl.3. The compound according to wherein Ris selected from the group consisting of: cyclopropylmethyl claim 1 , 2 claim 1 ,2-difluorocyclopropylmethyl claim 1 , 2 claim 1 ,2-difluoro-1-methylcyclopropylmethyl claim 1 , 1-(trifluoromethyl)cyclopropylmethyl claim 1 , 4 claim 1 ,4 claim 1 ,4-trifluoro-2 claim 1 ,2-dimethylbutyl claim 1 , cyclobutylmethyl claim 1 , 2 claim 1 ,2-dimethylpropyl claim 1 , prop-2-enyl claim 1 , biphenyl and benzyl claim 1 , optionally substituted with methoxy or —OCF.5. The compound according to wherein Ris selected from the group consisting of: halo claim 4 , —CN claim 4 , —N(O) claim 4 , amino claim 4 , —N(Calkyl) claim 4 , —C(O)—O—Calkyl claim 4 , —C(O)—Calkyl claim 4 , —S(O)—Calkyl claim 4 , Ccycloalkyl claim 4 , —C(Calkyl)-NHC(O)—O—Calkyl and Calkyl optionally substituted with 1 to 4 substituents independently selected from hydroxy and halo.7. The compound according to wherein Ris selected from the group consisting of: halo claim 6 , —CN claim 6 , —N(O) claim 6 , amino claim 6 , —N(Calkyl) claim 6 , —C(O)—O—Calkyl claim 6 , —C(O)—Calkyl claim 6 , —S(O)—Calkyl claim 6 , Ccycloalkyl and Calkyl optionally substituted with 1 to 4 substituents independently selected from hydroxy and halo.9. The compound according to wherein ring B is pyridyl.11. The compound according to wherein ring C is ...

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Номер записи: 81
15-08-2013 дата публикации

TRICYCLIC MGLUR5 RECEPTOR MODULATORS

Номер: US20130210804A1
Автор: Anthony Neville J., Gomez Robert P., LI Jing, Mercer Swati P., Roecker Anthony J., Stump Craig A., Williams Theresa M.
Принадлежит:

The present invention is directed to tricyclic compounds which are positive allosteric modulators of metabotropic glutamate receptors, particularly the mGluR5 receptor, and which are useful in the treatment or prevention of neurological and psychiatric disorders associated with glutamate dysfunction and diseases in which metabotropic glutamate receptors are involved. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which metabotropic glutamate receptors are involved. 5. The compound of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein A is selected from the group consisting of phenyl claim 1 , pyridyl and pyrrolyl.6. The compound of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein Q is C and V is C.7. The compound of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein Z is —CH—.8. The compound of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein R claim 1 , Rand Rare independently selected from the group consisting of:(1) hydrogen,(2) halogen,(3) hydroxyl,{'sub': '1-6', '(4) Calkyl, which is unsubstituted or substituted with halogen, hydroxyl, phenyl or napthyl,'}{'sub': '1-6', '(5) —O—Calkyl, which is unsubstituted or substituted with halogen, hydroxyl or phenyl,'}{'sub': 1-6', '1-6', '2, '(6) heteroaryl, wherein heteroaryl is selected from pyrrolyl, imidazolyl, indolyl, pyridyl, and pyrimidinyl, which is unsubstituted or substituted with halogen, hydroxyl, Calkyl, —O—Calkyl or —NO,'}{'sub': 1-6', '1-6', '2, '(7) phenyl, which is unsubstituted or substituted with halogen, hydroxyl, Calkyl, —O—Calkyl or —NO,'}{'sub': 1-6', '1-6', '2, '(8) —O-phenyl, which is unsubstituted or substituted with halogen, hydroxyl, Calkyl, —O—Calkyl or —NO, and'}{'sub': 1-6', '1-6', '1-6', '1-6', '1-6, '(9) —NH—Calkyl, or —N(Calkyl)(Calkyl), which is ...

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Номер записи: 82
15-08-2013 дата публикации

TRICYCLIC INDOLE DERIVATIVES USEFUL ENDOTHELIAL LIPASE INHIBITORS

Номер: US20130210806A1
Автор: Connelly Margery A., Greco Michael, Ye Hong
Принадлежит: Janssen Pharmaceutica, NV

The present invention is directed to tricyclic indole derivatives, pharmaceutical compositions containing them and their use in the treatment of disorders and conditions modulated by endothelial lipase, for example, cardiovascular disorders. 13. A pharmaceutical composition comprising a pharmaceutically acceptable carrier and a compound of .14. A pharmaceutical composition made by mixing a compound of and a pharmaceutically acceptable carrier.15. A process for making a pharmaceutical composition comprising mixing a compound of and a pharmaceutically acceptable carrier.16. A method of treating a disorder mediated by the endothelial lipase claim 1 , comprising administering to a subject in need thereof a therapeutically effective amount of the compound of .17. The method of claim 16 , wherein the disorder mediated by the endothelial lipase is selected from the group consisting of atherosclerosis claim 16 , dyslipidemia claim 16 , low HDL and high LDL.18. A method of treating a disorder selected from the group consisting of atherosclerosis claim 13 , dyslipidemia claim 13 , low HDL and high LDL comprising administering to the subject in need thereof a therapeutically effective amount of the composition of .19. A method of treating a disorder selected from the group consisting of atherosclerosis claim 1 , dyslipidemia claim 1 , low HDL and high LDL comprising administering to the subject in need thereof a therapeutically effective amount of the compound of . The present application claims benefit of U.S. Provisional Patent Application Ser. No. 61/599,066, filed on Feb. 15, 2012, which is incorporated herein by reference in its entirety and for all purposes.The present invention is directed to tricyclic indole derivatives, pharmaceutical compositions containing them and their use in the treatment of disorders and conditions modulated by endothelial lipase. More particularly, the compounds of the present invention are endothelial lipase inhibitors, useful in the treatment ...

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Номер записи: 83
15-08-2013 дата публикации

Tricyclic Compounds as Allosteric Modulators of Metabotropic Glutamate Receptors.

Номер: US20130210807A1
Автор: Boléa Christelle, Celanire Sylvain, Liverton Nigel J, Luo Yunfu
Принадлежит:

The present invention describes and claims compounds of the Structural Formula I, Structural Formula II, or Structural Formula III: wherein R, R, Rand R are —H or methyl, or Rand Rtaken together form a double bond, or R is —H and Rand Rtaken together form a spiro-cyclopropyl substituent, Ris —H or —F, and R5 is —H, methyl, —CI or —Br, Formula II wherein Ris —H, ethyl-, isopropyl-, cyclopropyl-, methyl- or methoxy-, Ris —H or —F, and “Y” is: (a) —CH—; (b) —CRH-0-CRR—, wherein R, R, and Rare independently —H or methyl; (c) —CRH—N(R)—CRR—, wherein R, R, and Rare independently —H or methyl; (d) —CH—C(R)(R)—C(R)(R)—, wherein R, R, Rand Rare independently —H or -methyl, or both Rand Rare —F, Rand Rare independently —H or -methyl, or both Rand Rare —F, or Rand Rtaken together are (0=), which together with the carbon to which they are attached forms a carbonyl group. 2) A pharmaceutical formulation comprising at least one compound of or a pharmaceutically acceptable salt thereof.3) Use of a compound of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , in the provision of a medicament for treating claim 1 , preventing claim 1 , or managing a disorder or disease which can be treated claim 1 , prevented claim 1 , or managed by administering an effective amount of an mGluR4 positive allosteric modulating compound.4) A medicament of formulated for use in the treatment or management of Parkinson's disease.5) A method of treating claim 3 , preventing claim 3 , or managing a disorder or disease which can be treated claim 3 , prevented claim 3 , or managed by administering an effective amount of an mGluR4 positive allosteric modulating compound comprising administering to a mammalian patient in need of such a medicament of in an effective amount in combination with an agent selected from the group consisting of: levodopa claim 3 , levodopa with a selective extracerebral decarboxylase inhibitor claim 3 , carbidopa claim 3 , entacapone claim 3 , a COMT inhibitor claim ...

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Номер записи: 84
22-08-2013 дата публикации

CRTH2 MODULATORS

Номер: US20130216552A1
Автор: Graul Regina, Jia James, Mermerían Ara, Nakai Takashi, Rohde Jason
Принадлежит: Ironwood Pharmaceuticals, Inc.

Modulators of CRTH2, particularly antagonists of CRTH2, that are useful for treating various disorders, including asthma and respiratory disorders are disclosed herein. The compounds are described by structural Formula I:

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Номер записи: 85
22-08-2013 дата публикации

Growth inhibition of perennial forage grasses with Pyroxsulam

Номер: US20130217578A1
Автор: Hare Donald Douglas
Принадлежит: DOW AGROSCIENCES LLC

Pyroxsulam inhibits the grown of perennial forage grasses, reducing the need for mowing. 1. A method of inhibiting the growth of perennial forage grasses which comprises contacting the perennial forage grass or the locus thereof with a growth inhibiting amount of pyroxsulam.2. The method of in which pyroxsulam is applied at a rate from about 7.5 grams per hectare (g ai/ha) to about 50 g ai/ha. This application is a continuation of U.S. patent application Ser. No. 13/270,281, filed Oct. 11, 2011 and claims the benefit of U.S. Provisional Patent Application Ser. No. 61/392,142 filed Oct. 12, 2010.This invention concerns the use of pyroxsulam as a plant growth regulator.The present invention concerns a method of controlling or inhibiting the growth of certain perennial forage grasses, particularly in areas covered by perennial forage grass cover, including non-crop areas and range and pasture. The use of ground cover is highly desirable in areas such as parkland, rights-of-way, roadsides, pipelines, transmission lines, airports and other areas considered as industrial vegetation management areas for prevention of erosion and for aesthetic reasons. Grasses are often the cover of choice, as they grow well in a range of sunlight availability, can use relatively little water, and are perennial. They do suffer from the problem of needing to be mowed or cut frequently in order to keep their height to a desired level for safety and aesthetic reasons, which can result in increased labor costs for agencies managing these areas.The plant growth regulating compound forming the composition of this invention is known in the art for its effect as an herbicide. Pyroxsulam, N-(5,7-dimethoxy[1,2,4]-triazolo[1,5-α]pyrimidin-2-yl)-2-methoxy-4-(trifluoromethyl)-3-pyridinesulfonamide, is a triazolopyrimidine sulfonamide herbicide, and its herbicidal activity is described in , Fifteenth Edition, 2009. Pyroxsulam provides broad-spectrum, post-emergence annual grass and broadleaf weed control ...

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Номер записи: 86
29-08-2013 дата публикации

THIADIAZOLE, COMPOUND FOR LIGHT-EMITTING ELEMENTS, LIGHT-EMITTING ELEMENT, LIGHT-EMITTING APPARATUS, AUTHENTICATION APPARATUS, AND ELECTRONIC DEVICE

Номер: US20130221334A1
Автор: Fujita Tetsuji, Yamamoto Hidetoshi
Принадлежит: SEIKO EPSON CORPORATION

The thiadiazole represented by formula (1), when used as a light-emitting material in a light-emitting element, allows the light-emitting element to emit near-infrared light. 4. The compound for light-emitting elements according to used as a light-emitting material.8. The light-emitting element according to claim 5 , further comprising an electron transport layer claim 5 , which is a layer having the capability of transporting electrons claim 5 , provided between the cathode and the light-emitting layer so as to be in contact with the light-emitting layer claim 5 ,wherein the electron transport layer contains a compound having an azaindolizine skeleton and an anthracene skeleton in the molecule as an electron transport material.12. The light-emitting element according to claim 9 , further comprising an electron transport layer claim 9 , which is a layer having the capability of transporting electrons claim 9 , provided between the cathode and the light-emitting layer so as to be in contact with the light-emitting layer claim 9 ,wherein the electron transport layer contains a compound having an azaindolizine skeleton and an anthracene skeleton in the molecule as an electron transport material.14. A light-emitting apparatus comprising the light-emitting element according to .15. A light-emitting apparatus comprising the light-emitting element according to .16. A light-emitting apparatus comprising the light-emitting element according to .17. An authentication apparatus comprising the light-emitting element according to .18. An authentication apparatus comprising the light-emitting element according to .19. An authentication apparatus comprising the light-emitting element according to .20. An electronic device comprising the light-emitting element according to .21. An electronic device comprising the light-emitting element according to .22. An electronic device comprising the light-emitting element according to . The present application claims priority to Japanese ...

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Номер записи: 87
29-08-2013 дата публикации

BISMUTH-THIOLS AS ANTISEPTICS FOR AGRICULTURAL, INDUSTRIAL AND OTHER USES

Номер: US20130224258A1
Автор: Baker Brett Hugh James
Принадлежит: MICROBION CORPORATION

Compositions and methods, including novel homogeneous microparticulate suspensions, are described for treating natural and artificial surfaces that contain bacterial biofilm, including unexpected synergy or enhancing effects between bismuth-thiol (BT) compounds and certain antibiotics, to provide formulations including antiseptic formulations. Previously unpredicted antibacterial properties and anti-biofilm properties of disclosed BT compounds and BT compound-plus-antibiotic combinations are also described, including preferential efficacies of certain such compositions for treating certain gram-positive bacterial infections, and distinct preferential efficacies of certain such compositions for treating certain gram-negative bacterial infections. 1. A method for protecting a plant against a bacterial , fungal or viral pathogen , comprising:contacting the plant with an effective amount of a bismuth-thiol (BT) composition under conditions and for a time sufficient for one or more of:(i) prevention of infection of the plant by the bacterial, fungal or viral pathogen,(ii) inhibition of cell viability or cell growth of substantially all planktonic cells of the bacterial, fungal or viral pathogen,(iii) inhibition of biofilm formation by the bacterial, fungal or viral pathogen, and(iv) inhibition of biofilm viability or biofilm growth of substantially all biofilm-form cells of the bacterial, fungal or viral pathogen,wherein the BT composition comprises a substantially monodisperse suspension of microparticles that comprise a BT compound, said microparticles having a volumetric mean diameter of from about 0.4 μm to about 10 μm.2Erwinia amylovora. The method of wherein the bacterial pathogen comprises cells.3Erwinia amylovora, Xanthomonas campestrisdieffenbachiae, Pseudomonas syringae, Xylella fastidiosa; Xylophylus ampelinus; Monilinia fructicola, Pantoea stewartiiStewartii, Ralstonia solanacearumClavibacter michiganensissepedonicus.. The method of wherein the bacterial ...

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Номер записи: 88
29-08-2013 дата публикации

FUSED TETRACYCLIC PYRIDO [4,3-B] INDOLE AND PYRIDO [3,4-B] INDOLE DERIVATIVES AND METHODS OF USE

Номер: US20130225558A1
Автор: CHAKRAVARTY Sarvajit, Hart Barry Patrick, JAIN Rajendra Parasmal
Принадлежит:

This disclosure is directed to fused tetracyclic pyrido[4,3-b>]indole and pyrido[3,4-b]indole derivatives. Pharmaceutical compositions comprising the compounds are also provided, as are methods of using the compounds in a variety of therapeutic applications, including the treatment of a cognitive disorder, psychotic disorder, neurotransmitter-mediated disorder and/or a neuronal disorder. 4. The compound of claim 3 , wherein Ris H or methyl.5. The compound of claim 3 , wherein each R claim 3 , R claim 3 , R claim 3 , R claim 3 , R claim 3 , R claim 3 , R claim 3 , R claim 3 , Rand R claim 3 , where applicable claim 3 , is independently H claim 3 , hydroxyl claim 3 , substituted or unsubstituted C-Calkyl claim 3 , substituted or unsubstituted aryl claim 3 , substituted or unsubstituted heteroaryl claim 3 , substituted or unsubstituted heterocyclyl claim 3 , substituted or unsubstituted aralkyl claim 3 , or acylamino claim 3 , or Rand Rare taken together with the carbon to which they are attached to form a carbonyl moiety claim 3 , or Rand a vicinal R claim 3 , where applicable claim 3 , are taken together to form a bond.6. The compound of claim 3 , wherein at least one of R claim 3 , R claim 3 , R claim 3 , R claim 3 , R claim 3 , R claim 3 , R claim 3 , R claim 3 , Rand Ris a group containing a cyclic moiety.7. The compound of claim 6 , wherein the group containing a cyclic moiety is selected from the group consisting of substituted or unsubstituted aryl claim 6 , substituted or unsubstituted heteroaryl claim 6 , substituted or unsubstituted cycloalkyl claim 6 , and substituted or unsubstituted heterocyclyl.8. The compound of claim 6 , wherein the group containing a cyclic moiety is a C-Calkyl claim 6 , or a C-Calkenyl claim 6 , substituted with a group selected from the group consisting of substituted or unsubstituted aryl claim 6 , substituted or unsubstituted heteroaryl claim 6 , substituted or unsubstituted cycloalkyl claim 6 , and substituted or unsubstituted ...

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Номер записи: 89
29-08-2013 дата публикации

FUROPYRIDINE DERIVATIVES

Номер: US20130225569A1
Автор: Burgdorf Lars, Hodous Brian, Huck Bayard R., Potnick Justin, Ross Tatjana, SCHULTZ Melanie, Sutton Amanda E.
Принадлежит: Merck Patent Gesellschaft Mit Beschrankter Haftung

Compounds of the formula I 2. Compounds according to in which{'sup': 1', '4, 'sub': 2', 'n', '2', 'n, 'Hetdenotes furyl, thienyl, pyrrolyl, imidazolyl, pyrazolyl, oxazolyl, isoxazolyl, thiazolyl, isothiazolyl, pyridyl, pyrimidinyl, triazolyl, tetrazolyl, oxadiazolyl, thiadiazolyl, pyridazinyl, pyrazinyl, quinolyl, isoquinolyl, benzimidazolyl, benzotriazolyl, indolyl, benzo-1,3-dioxolyl, 2,3-dihydro-benzo[1,4]dioxinyl, indazolyl or benzothiadiazolyl, each of which is unsubstituted or mono-, di- or trisubstituted by Het, A, benzyl, (CH)OH and/or (CH)OA,'}and pharmaceutically acceptable solvates, salts, tautomers and stereoisomers thereof, including mixtures thereof in all ratios.3. Compounds according to in which{'sup': 2', '4', '4', '4, 'sub': 2', 'n', '2', 'n', '2', 'n', '2', 'n', '2', 'p', '2', 'p', '2', 'p', '2', 'p', '2', 'n', '2', 'n', '2', '2', 'n', '2', 'n', '2', '2', 'p', '2', '2', '2', '2, 'Hetdenotes piperidinyl, piperazinyl, pyrrolidinyl, morpholinyl, furyl, thienyl, pyrrolyl, imidazolyl, pyrazolyl, oxazolyl, isoxazolyl, thiazolyl, isothiazolyl, pyridyl, pyrimidinyl, triazolyl, tetrazolyl, oxadiazolyl, thiadiazolyl, pyridazinyl, pyrazinyl, quinolyl, isoquinolyl, benzimidazolyl, benzothiophenyl, benzotriazolyl, indolyl, indolinyl, benzo-1,3-dioxolyl, 2,3-dihydro-benzo[1,4]dioxinyl, 1,3-dihydro-indolyl, 1,3-dihydrobenzimidazolyl, dihydropyranyl, 3,4-dihydro-2H-pyrano[2,3-b]pyridinyl, 1,2,3,4-tetrahydro-[1,8]naphthyridinyl, furopyridinyl, indazolyl, benzo[1,4]oxazinyl, pyrido[3,2-b][1,4]oxazinyl or benzothiadiazolyl, each of which is unsubstituted or mono-, di- or trisubstituted by Hal, (CH)Het, NH(CH)Het, OHet, A, (CH)OH, (CH)OA, (CH)CH(OH)(CH)OH, (CH)CH(OH)(CH)OA, (CH)COOA, phenyl, benzyl, CHO, COA, (CH)NH, (CH)NHA, (CH)NA, NH(CH)NH, CN, NHSOA, NASOA, SOA and/or ═O,'}and pharmaceutically acceptable solvates, salts, tautomers and stereoisomers thereof, including mixtures thereof in all ratios.4. Compounds according to in which{'sup': 3', '3, 'sub': 2', 'n', ...

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Номер записи: 90
29-08-2013 дата публикации

BICYCLIC HETEROCYCLIC SPIRO COMPOUNDS

Номер: US20130225624A1
Автор: BAR-NER Nira, FISHER Abraham, NACHUM Victoria
Принадлежит:

There are provided certain bicyclic heterocyclic compounds that act as M1 muscarinic receptor modulators. Compositions containing these compounds and their use are also disclosed. 2. A compound according to wherein R is methyl.3. A compound according to wherein p and n are each 1.58-. (canceled)9. A compound according to wherein Ris methyl.10. A compound according to wherein Ris H.11. A compound according to wherein Rand Rare each H.12. A compound according to wherein Ris H.13. A compound according to any wherein Y is S.14. A compound according to wherein Y is O.15. A compound according to wherein Ris optionally substituted —C(O)—(C)-indol-3-yl.16. A compound according to wherein Ris selected from the group consisting of —C(O)—CH-indol-3-yl claim 15 , —C(O)—CHCH-indol-3-yl claim 15 , —C(O)—CHCHCH-indol-3-yl claim 15 , trans —C(O)—CH═CH-indol-3-yl and —C(O)—CH(NH)—CH-indol-3-yl.1720-. (canceled)22. A compound according to wherein Ris selected from the group consisting of —SO-4-fluorophenyl claim 1 , —C(O)CH(n-propyl) claim 1 , —C(O)-(4-hydroxy-3 claim 1 ,5-di-tertbutylphenyl) and —C(O)—CHCH.2325-. (canceled)27. A compound according to which is selected from the group consisting of (1-(2 claim 1 ,8-dimethyl-1-thia-3 claim 1 ,8-diazaspiro[4.5]dec-3-yl)-3-(1H-indol-3-yl)propan-1-one) claim 1 , (+)-(1-(2 claim 1 ,8-dimethyl-1-thia-3 claim 1 ,8-diazaspiro[4.5]dec-3-yl)-3-(1H-indol-3-yl)propan-1-one) claim 1 , (−)-(1-(2 claim 1 ,8-dimethyl-1-thia-3 claim 1 ,8-diazaspiro[4.5]dec-3-yl)-3-(1H-indol-3-yl)propan-1-one) claim 1 , 1-(2 claim 1 ,8-dimethyl-1-oxa-3 claim 1 ,8-diazaspiro[4.5]dec-3-yl)-3-(1H-indol-3-yl)-propan-1-one claim 1 , (+)-1-(2 claim 1 ,8-dimethyl-1-oxa-3 claim 1 ,8-diazaspiro[4.5]dec-3-yl)-3-(1H-indol-3-yl)-propan-1-one claim 1 , and (−)-1-(2 claim 1 ,8-dimethyl-1-oxa-3 claim 1 ,8-diazaspiro[4.5]dec-3-yl)-3-(1H-indol-3-yl)-propan-1-one.28. A pharmaceutical composition comprising the compound AF710B and a pharmaceutically acceptable carrier claim 1 , excipient ...

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Номер записи: 91
05-09-2013 дата публикации

QUINOLINO[3,2,1-KL]PHENOXAZINE COMPOUND AND ORGANIC LIGHT EMITTING ELEMENT USING THE SAME

Номер: US20130228768A1
Автор: Abe Shigemoto, Kamatani Jun, Kishino Kengo, Kosuge Tetsuya
Принадлежит: CANON KABUSHIKI KAISHA

Provided is an excellent organic light emitting element having high emission efficiency and a low drive voltage. The organic light emitting element includes an anode, a cathode, and an organic compound layer disposed between the anode and the cathode, in which the organic compound layer includes a quinolino[3,2,1-kl]phenoxazine compound represented by the following general formula [1]: 3. An organic light emitting element comprising:an anode;a cathode; andan organic compound layer disposed between the anode and the cathode,{'claim-ref': {'@idref': 'CLM-00001', 'claim 1'}, 'wherein the organic compound layer comprises the quinolino[3,2,1-kl]phenoxazine compound according to .'}4. The organic light emitting element according to claim 3 , wherein:the organic compound layer comprises an emission layer and a hole transport layer adjacent to the emission layer; andthe hole transport layer comprises the quinolino[3,2,1-kl]phenoxazine compound.5. The organic light emitting element according to claim 4 , wherein:the emission layer comprises a host and a guest;the host comprises the quinolino[3,2,1-kl]phenoxazine compound; andthe guest comprises a phosphorescent light emitting material.6. The organic light emitting element according to claim 5 , wherein the phosphorescent light emitting material comprises an iridium complex.7. A display device comprising multiple pixels claim 3 , wherein the pixels each comprise the organic light emitting element according to and a switching element connected to the organic light emitting element.8. An image input device comprising:a display unit for displaying an image; andan input unit for inputting image information,wherein:the display unit comprises multiple pixels; and{'claim-ref': {'@idref': 'CLM-00003', 'claim 3'}, 'the pixels each comprise the organic light emitting element according to and a switching element connected to the organic light emitting element.'}9. A display device comprising multiple pixels claim 4 , wherein the pixels ...

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Номер записи: 92
05-09-2013 дата публикации

INDOLOPHENOXAZINE COMPOUND AND ORGANIC LIGHT EMITTING DEVICE USING THE SAME

Номер: US20130228770A1
Автор: Abe Shigemoto, Kamatani Jun, Kishino Kengo, Kosuge Tetsuya
Принадлежит: CANON KABUSHIKI KAISHA

Provided is an organic light emitting device having high emission efficiency and excellent driving durability. The organic light emitting device includes an anode, a cathode, and an organic compound layer disposed between the anode and the cathode, in which the organic compound layer includes an indolophenoxazine compound represented by the following general formula [1]: 2. The indolophenoxazine compound according to claim 1 , wherein each of Rto Rrepresents a hydrogen atom.4. An organic light emitting device comprising:an anode;a cathode; andan organic compound layer disposed between the anode and the cathode,{'claim-ref': {'@idref': 'CLM-00001', 'claim 1'}, 'wherein the organic compound layer comprises the indolophenoxazine compound according to .'}5. The organic light emitting device according to claim 4 , wherein the indolophenoxazine compound is contained in one of a hole injection layer and a hole transport layer.6. The organic light emitting device according to claim 5 , wherein:the organic compound layer comprises a light emitting layer; andthe light emitting layer comprises a phosphorescent light emitting material.7. The organic light emitting device according to claim 6 , wherein the phosphorescent light emitting material comprises an iridium complex.8. An image display apparatus comprising:{'claim-ref': {'@idref': 'CLM-00004', 'claim 4'}, 'the organic light emitting device according to ; and'}a switching element connected to the organic light emitting device.9. An image display apparatus comprising:{'claim-ref': {'@idref': 'CLM-00005', 'claim 5'}, 'the organic light emitting device according to ; and'}a switching element connected to the organic light emitting device.10. An image display apparatus comprising:{'claim-ref': {'@idref': 'CLM-00006', 'claim 6'}, 'the organic light emitting device according to ; and'}a switching element connected to the organic light emitting device.11. An image display apparatus comprising:{'claim-ref': {'@idref': 'CLM-00007', ...

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Номер записи: 93
05-09-2013 дата публикации

ENTERIC-COATED SODIUM METABISULFITE LIVESTOCK FEED ADDITIVE FOR VOMITOXIN DETOXIFICATION

Номер: US20130230597A1
Автор: Adams Keith, Cook Douglas R.
Принадлежит: Cargill, Incorporated

A livestock feed supplement in which a core particle containing sodium metabisulfite and at least one binder is enrobed with an enteric coating, wherein the thickness and composition of the coating protects the sodium metabisulfite from decomposition to sulfur dioxide in an aqueous acid stomach environment. Also disclosed are a method of delivering sodium metabisulfite to the lower gastrointestinal tract of an animal, and a method of delivering an antidote to relieve the toxic effect of vomitoxin in an animal, by administering to the animal the livestock feed supplement. 1. A livestock feed supplement comprising:(a) a core particle comprising sodium metabisulfite and at least one binder, and(b) an enteric coating enrobing said core particle,wherein the thickness and composition of said coating protects said sodium metabisulfite from decomposition to sulfur dioxide in an aqueous acid stomach environment.2. The livestock feed supplement of claim 1 , wherein said binder comprises a pellet binder claim 1 , a starch binder claim 1 , or a fiber binder.3. The livestock feed supplement of claim 1 , wherein said binder is a water-soluble binder selected from the group consisting of starch claim 1 , sodium caseinate claim 1 , gelatin claim 1 , soybean protein claim 1 , molasses claim 1 , lactose claim 1 , dextrin claim 1 , carboxymethyl cellulose salt claim 1 , alginates claim 1 , methyl cellulose claim 1 , ethyl cellulose claim 1 , hydroxypropyl cellulose claim 1 , starch glycolic acid salt claim 1 , polymethacrylates claim 1 , polyvinyl alcohol and polyvinyl pyrrolidone.4. The livestock feed supplement of claim 1 , wherein said binder is a hydrophobic binder selected from the group consisting of natural waxes claim 1 , shellac resin claim 1 , rosin claim 1 , bees wax claim 1 , paraffin wax claim 1 , cetanol claim 1 , higher fatty acids claim 1 , stearic acid claim 1 , stearic acid metal salts claim 1 , animal fats claim 1 , animal oils claim 1 , vegetable fats claim 1 , ...

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Номер записи: 94
05-09-2013 дата публикации

SYNERGISTIC HERBICIDAL COMPOSITION CONTAINING PENOXSULAM AND ORYZALIN

Номер: US20130231245A1
Автор: Mann Richard K.
Принадлежит: DOW AGROSCIENCES LLC

An herbicidal synergistic composition containing (a) penoxsulam and (b) oryzalin provides improved post-emergence herbicidal weed control in tree and vine crops, turf, sugar cane, range and pasture, parks and alleyways, and IVM. 1. A synergistic herbicidal composition comprising a herbicidally effective amount of (a) penoxsulam and (b) oryzalin.2. The composition of in which the weight ratio of oryzalin to penoxsulam on an active ingredient (ai) basis is from about 40:1 to about 960:1.3. The composition of claim 2 , wherein the weight ratio is from about 343:1 to about 536:1.4. The composition of claim 2 , wherein the weight ratio is about 343:1 or 536:1.5. The composition of claim 2 , wherein the weight ratio is about 300:1.6. The composition of further comprising an agriculturally acceptable adjuvant or carrier.7. A method of controlling undesirable vegetation comprising contacting the vegetation or the locus thereof with a herbicidally effective amount the composition of .8. A method of controlling undesirable vegetation comprising contacting the vegetation or the locus thereof with a herbicidally effective amount of (a) penoxsulam and (b) oryzalin.9. The method of claim 8 , wherein the weight ratio of oryzalin to penoxsulam on an active ingredient (ai) basis is from about 40:1 to about 960:1.10. The method of claim 9 , wherein the weight ratio is about 343:1 or 536:1.11. The method of claim 9 , wherein the weight ratio is about 300:1.12. The method of claim 8 , wherein the undesirable vegetation is Solanum nigrum claim 8 , Chenopodium album claim 8 , Portulaca oleracea claim 8 , Kickxia spuria claim 8 , or Senecio vulgaris.13. The method of claim 8 , wherein the undesirable vegetation is controlled in fruit trees claim 8 , grapevines claim 8 , turf claim 8 , sugar cane claim 8 , parks and alleyways claim 8 , range and pasture claim 8 , or industrial vegetation management.14. The method of claim 13 , wherein the fruit tree is pome claim 13 , stone claim 13 , tree ...

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Номер записи: 95
05-09-2013 дата публикации

Methods for reducing nematode damage

Номер: US20130231299A1
Автор: Adel Morcos, Elmar Kerber, Max Angst
Принадлежит: SYNGENTA CROP PROTECTION LLC

A method of reducing damage to plant propagation material and plant organs which grow at a later time by a representative of the class Nematoda, which method comprises (i) treating the propagation material with (A) a chelating agent, and optionally (B) a macrocyclic lactone compound or another pesticide, before the material is sown or planted, or (ii) applying (A) a chelating agent, and optionally (B) a macrocyclic lactone compound or another pesticide, to the locus of the material or the treated material defined in (i) before its planting, and/or at its planting and/or during its growth.

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Номер записи: 96
05-09-2013 дата публикации

IMIDAZOPYRIZINE SYK INHIBITORS

Номер: US20130231330A1
Автор: BLOMGREN Peter A., CURRIE Kevin S., KROPF JEFFREY E., LEE SEUNG H., MITCHELL Scott A., STAFFORD Douglas G., XU JIANJUN
Принадлежит: Gilead Connecticut, Inc.

Certain imidazopyrazines and pharmaceutical compositions thereof are provided herein. Methods of treating patients suffering from certain diseases and disorders responsive to the inhibition of Syk activity, which comprises administering to such patients an amount of at least one chemical entity effective to reduce signs or symptoms of the disease or disorder are provided. Also provided are methods for determining the presence or absence of Syk kinase in a sample. 2: At least one chemical entity of claim 1 , wherein Ris pyridinyl substituted with one or more groups chosen fromhydroxy;{'sup': b', 'c', 'b', 'c, 'sub': 1', '6', '1', '4', '1', '4', '1', '4, '—NRRwherein Ris chosen from hydrogen and C-Calkyl optionally substituted with one or two groups chosen from hydroxy and —OC-Calkyl and Ris independently chosen from hydrogen and C-Calkyl optionally substituted with one or two groups chosen from hydroxy and —OC-Calkyl;'}{'sub': 3', '6', '1', '4', '1', '4', '1', '4', '1', '4', '1', '4', '2', '1', '4', '1', '4', '1', '4', '1', '4, 'heterocycloalkyl optionally substituted with one or two groups chosen from hydroxy, C-Ccycloalkyl, C-Calkyl, —C-Calkyl-OH, —C-Calkyl-O—C-Calkyl, —C-Calkyl-NH, —N(C-Calkyl)(C-Calkyl), —NH(C-Calkyl), and —OC-Calkyl;'}{'sub': 1', '6', '3', '6', '1', '4', '1', '4', '1', '4', '1', '4', '1', '4', '2', '1', '4', '1', '4', '1', '4', '1', '4, '—OC-Calkyl optionally substituted with one or two groups chosen from hydroxy, C-Ccycloalkyl, C-Calkyl, —C-Calkyl-OH, —C-Calkyl-O—C-Calkyl, —C-Calkyl-NH, —N(C-Calkyl)(C-Calkyl), —NH(C-Calkyl), and —OC-Calkyl;'}{'sub': 1', '6', '3', '6', '1', '4', '1', '4', '1', '4', '1', '4', '1', '4', '2', '1', '4', '1', '4', '1', '4', '1', '4, 'C-Calkyl optionally substituted with one or two groups chosen from hydroxy, C-Ccycloalkyl, C-Calkyl, —C-Calkyl-OH, —C-Calkyl-O—C-Calkyl, —C-Calkyl-NH, —N(C-Calkyl)(C-Calkyl), —NH(C-Calkyl), and —OC-Calkyl; and'}{'sub': 3', '6', '1', '4', '1', '4', '1', '4', '1', '4', '1', '4', '2', '1', ...

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Номер записи: 97
12-09-2013 дата публикации

MATERIAL FOR ORGANIC ELECTROLUMINESCENCE DEVICE AND ORGANIC ELECTROLUMINESCENCE DEVICE

Номер: US20130234119A1
Автор: HIBINO Kumiko, INOUE Tetsuya, Ito Mitsunori, MIZUKI Yumiko, Nishimura Kazuki
Принадлежит: IDEMITSU KOSAN CO., LTD.

An organic electroluminescence device employing a specific biscarbazole derivative having a cyano group as a first host and a compound having both a carbazole structure and a nitrogen-containing aromatic heteroring as a second host. The organic electroluminescence device has a prolonged lifetime. 2. The organic electroluminescence device according to claim 1 , wherein the first host material satisfies at least one of the requirements (i) and (ii).3. The organic electroluminescence device according to claim 1 , wherein Aof formula (A) represents a substituted or unsubstituted divalent monocyclic hydrocarbon group having 6 or less ring carbon atoms or a substituted or unsubstituted divalent monocyclic heterocyclic group having 6 or less ring atoms.6. The organic electroluminescence device according to claim 1 , wherein the first host material satisfies only the requirement (i).8. The organic electroluminescence device according to claim 1 , wherein at least one of Aand Arepresents a cyano-substituted phenyl group claim 1 , a cyano-substituted naphthyl group claim 1 , a cyano-substituted phenanthryl group claim 1 , a cyano-substituted dibenzofuranyl group claim 1 , a cyano-substituted dibenzothiophenyl group claim 1 , a cyano-substituted biphenyl group claim 1 , a cyano-substituted terphenyl group claim 1 , a cyano-substituted 9 claim 1 ,9-diphenylfluorenyl group claim 1 , a cyano-substituted 9 claim 1 ,9′-spirobi[9H-fluorene]-2-yl group claim 1 , a cyano-substituted 9 claim 1 ,9′-dimethylfluorenyl group claim 1 , or a cyano-substituted triphenylenyl group.9. The organic electroluminescence device according to claim 1 , wherein the light emitting material comprises a phosphorescent emitting material selected from ortho metallated complexes of a metal selected from iridium (Ir) claim 1 , osmium (Os) claim 1 , and platinum (Pt).10. The organic electroluminescence device according to claim 1 , wherein a peak of emission wavelength of the phosphorescent emitting material ...

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Номер записи: 98
12-09-2013 дата публикации

COGNITIVE FUNCTION

Номер: US20130236447A1
Автор: ROSENBLUM Yaacov, SEGEV Yifat, STERN Elad
Принадлежит: CARMEL-HAIFA UNIVERSITY ECONOMIC CORP., LTD.

Inhibition of eIF-2α phosphorylation can be used to improve cognitive function and/or to treat dementia, including Alzheimer's Disease. In particular, this can be achieved by inhibiting the kinase activity of PKR in a non-toxic manner. 1. A method for improving cognitive function , said method comprising administering to a patient in need a therapeutically effective amount of an inhibitor of eIF-2α phosphorylation or a pharmaceutically acceptable salt thereof such as to improve cognitive function in said patient.2. The method according to claim 1 , for improving learning claim 1 , improving memory formation claim 1 , or both.3. The method according to claim 2 , for treating dementia in said patient.4. The method according to claim 3 , for treating Alzheimer's Disease.5. The method according to claim 1 , wherein the inhibitor of eIF-2α phosphorylation inhibits a kinase.6. The method according to claim 5 , wherein the inhibitor is an inhibitor of the kinase activity of PKR.7. The method according to claim 5 , wherein the inhibitor acts to inhibit the ATP-binding site of a kinase.8. The method according to claim 1 , wherein the inhibitor is administered orally or by injection.9. The method according to claim 1 , wherein the inhibitor is a small molecule.11. The method according to claim 1 , wherein the inhibitor is a protein claim 1 , a peptide claim 1 , an antibody or a nucleic acid.12. The method according to claim 11 , wherein the nucleic acid is an antisense RNA or a double stranded RNA.13. The method according to claim 1 , including inhibiting an eIF-2α kinase.14. The method according to claim 1 , including inhibiting the kinase activity of PKR.15. The method according to claim 1 , wherein the patient is human. The present application is a Continuation-in-Part of U.S. patent application Ser. No. 12/827,935, filed Jun. 30, 2010, which is a National stage and Continuation-in-Part of International Application No. PCT/IB2009/007857, filed Dec. 21, 2009, in which the ...

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Номер записи: 99
12-09-2013 дата публикации

Antipathogenic Surfaces Having Selenium Nanoclusters

Номер: US20130236523A1
Автор: Tran Phong Anh, Webster Thomas J.
Принадлежит: BROWN UNIVERSITY

The present invention is directed to methods for inhibiting growth of pathogens and to substrates with selenium nanoparticles or selenium nanoclusters having antipathogenic properties. 1. A method of inhibiting growth of a pathogen comprising contacting the pathogen to selenium nanoclusters or selenium nanoparticles and inhibiting growth of the pathogen.2. The method of wherein the pathogen is on a substrate.3. The method of wherein the substrate includes a metal claim 2 , a polymer claim 2 , a ceramic or composites thereof.4. The method of wherein the metal is titanium claim 3 , aluminum claim 3 , platinum claim 3 , niobium claim 3 , tantalum claim 3 , tin claim 3 , nickel claim 3 , cobalt claim 3 , chromium claim 3 , molybdenum claim 3 , stainless steel claim 3 , nitinol claim 3 , Ti6Al4V claim 3 , SiN claim 3 , CoCrMo claim 3 , zinc claim 3 , silver claim 3 , gold or alloys thereof.5. The method of wherein the polymer is polycarbonate claim 3 , polyethyleneimine claim 3 , isoplast claim 3 , polyvinyl chloride claim 3 , silicone claim 3 , polyurethane claim 3 , polyether imide claim 3 , polycaprolactone claim 3 , poly-lactic-co-glycolic acid claim 3 , poly-lactic acid claim 3 , poly-glycolic acid claim 3 , polyethylene claim 3 , polyethylene glycol claim 3 , polydimethylsiloxane claim 3 , polyacrylamide claim 3 , polypropylene claim 3 , polystyrene claim 3 , polyether ether ketone (PEEK) claim 3 , ultra high molecular weight polyethylene (UHMWPE) claim 3 , hydrogels claim 3 , or composites thereof.6. The method of wherein the ceramic is alumina claim 3 , titania claim 3 , hydroxyapatite claim 3 , silica claim 3 , calcium phosphates claim 3 , bone cements claim 3 , metal oxides or composites therefore.7. A substrate surface having antipathogenic properties including selenium nanoclusters produced by the method of contacting the substrate with a liquid medium including a selenium precursor and a reducing agent for a time sufficient to form selenium nanoclusters on ...

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Номер записи: 100