Abstract: A family of three 8-alkyl boron dipyrromethenes 1, 2, and 3 has been prepared. These compounds are characterized by emission in the green region of the electromagnetic radiation spectrum and exhibit an almost double laser efficiency than other commercial dyes and much greater photostability. The 8-alkyl boron dipyrromethenes are prepared by catalytic hydrogenation (reduction) of the corresponding 8-alkenyl boron dipyrromethenes, which are obtained by Liebeskind-Srogl coupling of thiomethylboron dipyrromethene with an alkenyl boronic acid.
Abstract: The disclosure provides fluorescence probe compounds of formula I, their preparation methods and applications. These compounds are useful in detecting mercury ions.
Type:
Grant
Filed:
December 3, 2010
Date of Patent:
March 4, 2014
Assignees:
Dalian University of Technology, Dalian Chromas Bioscience Co., Ltd.
Inventors:
Xiaojun Peng, Jiangli Fan, Jianjun Du, Jingyun Wang, Jianzhou Zhang, Shiguo Sun
Abstract: In a process for making an N-substituted phthalimide compound, an amine is contacted with a carboxylic acid anhydride and allowed to react in an aqueous solution at a pH of about 2 to about 6. Optionally, the reactants are combined with an acid to lower the pH of the reaction solution wherein the lowering of the pH optimizes the yield of the desired N-substituted phthalimide product. The N-substituted phthalimide may be, for example, N-hydroxyphthalimide, and the reactants may be phthalic anhydride and hydroxylamine or a salt thereof. The N-substituted phthalimide compound is useful for, among other things, the oxidation of various hydrocarbons.
Abstract: Novel silicone compounds containing a siloxane moiety and at least one terpenyl moiety, such as limonenyl or valencenyl, and methods for their synthesis, are provided. The novel compounds are appropriate for incorporation into cosmetic formulations due to their low aroma, resistance to deterioration, and favorable solubility properties.
Type:
Grant
Filed:
February 14, 2012
Date of Patent:
February 18, 2014
Assignee:
Gelest Technologies, Inc.
Inventors:
Barry C. Arkles, Rudolph Cameron, Youlin Pan, Gerald L. Larson
Abstract: A process for the manufacture of agomelatine and its intermediate N-[2-(7-methoxy- 1-naphthy)ethyl]phthalimide is provided and inclues reacting 7-methoxy-1-naphthyl ethanol (III) with benzenesulfonyl chloride to obtain 7-methoxy-1 -naphthylethyl benzene sulfonate (IV), which is reacted with potassium phthalimide to produce N-[2-(7-methoxy-1-naphthy)ethyl]phthalimide (II); and subjecting N-[2-(7-methoxy-1-naphthy)ethyl]phthalimide (II) to alkaline hydrolysis and acetylation, to obtain agomelatine.
Abstract: Disclosure is provided for imidazole derivative compounds that prevent, remove and/or inhibit the formation of biofilms, compositions comprising these compounds, devices comprising these compounds, and methods of using the same.
Type:
Grant
Filed:
February 2, 2011
Date of Patent:
February 18, 2014
Assignee:
North Carolina State University
Inventors:
Christian Melander, John Cavanagh, Robert W. Huigens, III, T. Eric Ballard, Justin J. Richards
Abstract: Compounds of the formula (I): in which A, R1, R2, X, Y and Z are defined in the description, the processes for the preparation of these compounds, the uses thereof for the treatment of dyslipidaemia, atherosclerosis and diabetes, and the pharmaceutical compositions comprising them.
Type:
Grant
Filed:
December 22, 2005
Date of Patent:
February 18, 2014
Assignee:
Merck Patent GmbH
Inventors:
Catherine Vidal, Nathalie Adje, Stéphane Yvon, Jean Jacques Zeiller
Abstract: The present invention relates to an azeotropic or azeotrope-like mixture consisting essentially of 1,1,1,2,3,3-hexafluoropropane, hexafluoropropene and hydrogen fluoride.
Type:
Grant
Filed:
April 11, 2013
Date of Patent:
February 18, 2014
Assignee:
Honeywell International Inc.
Inventors:
Ryan Hulse, Hang T. Pham, Rajiv R. Singh, Hsueh S. Tung, Daniel C. Merkel, Konstantin A. Pokrovski
Abstract: The present invention relates to the field of organic chemistry and in particular to organic free radicals used as polarizing agents in the technique of Dynamic Nuclear Polarization (DNP), which involves transferring the polarization of electron spins to the nuclei of a compound whose Nuclear Magnetic Resonance (NMR) is being observed. It concerns dinitroxide-type biradical polarizing agents characterized by a rigid linkage between the nitroxide units that enables optimal orientation and distance to be maintained between the aminoxyl groups of said nitroxide units. This particular structure enables, at low temperatures and high fields, optimal transfer of polarization and optimal enhancement of NMR/MAS signals of the polarized nuclei of the compound studied.
Type:
Grant
Filed:
May 29, 2009
Date of Patent:
February 11, 2014
Assignee:
Universite d'Aix Marseille
Inventors:
Olivier Ouari, Hakim Karoui, Francois Le Moigne, Paul Tordo, Robert G. Griffin, Yoh Matsuki, Thorsten Maly
Abstract: Alkoxy-substituted phenyltetraene nonlinear optically active compounds, films and devices that include the compounds, and methods for making and using the compounds, films, and devices.
Type:
Grant
Filed:
May 28, 2009
Date of Patent:
February 11, 2014
Assignee:
University of Washington
Inventors:
Kwan-Yue Jen, Jingdong Luo, Su Huang, Yen-Ju Cheng, Tae-Dong Kim, Zhengwei Shi, Xinghua Zhou, Brent M. Polishak, Yanqing Tian
Abstract: The present invention relates to chemical-pharmaceutical industry and medicine. The present invention relates to N-[3-(4-nitrophenylamino)-indole-2-ilmethylene]aminoguanidine hydrochloride of formula (2) having anti-inflammatory and chondroprotective activity. The compound does not exhibit adverse effects.
Type:
Grant
Filed:
March 11, 2011
Date of Patent:
February 4, 2014
Assignee:
Obschestvo S Ogranichennoy Otvetstvennostyu “Polyar” (OOO Polyar)
Abstract: The present invention relates to photolabile or photoreleasable compounds including a caging moiety linked to an effector moiety, wherein the compounds are capable of releasing the effector moiety on irradiation, typically by flash irradiation with UV light. These compounds are particularly suitable for focal 2-photon uncaging The photoreleasable compounds can be used to deliver effector moieties such as carboxylic acids, preferably, neuroactive amino acids to sites where their activity is required. In preferred embodiments of the invention, the caging moiety is based on 4-carboxymethoxy-5,7-dinitroinlinyl and derivatives thereof.
Type:
Grant
Filed:
January 29, 2008
Date of Patent:
February 4, 2014
Assignee:
Philadelphia Health & Education Corporation
Abstract: The present invention relates to two main components, mahanine and mahanimbine (dehydroxy-mahanine) from Murraya koenigii for the treatment of glioblastoma and cervical carcinoma. Mahanimbine exhibited anti-cancer activity against lymphoid leukemia, myeloid leukemia, glioma, cervical carcinoma, pancreatic, colon and lung cancers in nineteen cells of different genetic status. C-3 hydroxy and NH groups are responsible contributing groups for their cytotoxicity. Mahanine reduced the doses of cisplatin and paclitaxel in cervical cancer showing better efficacy and useful as an adjunct chemotherapeutic agent to reduce toxicity these two drugs. A new cheap process for this preparation was established. EtOAc extract containing alkaloids enriched with mahanimbine and mahanine, is active against glioma and cervical cancers.
Type:
Grant
Filed:
March 9, 2012
Date of Patent:
January 28, 2014
Assignee:
Council of Scientific and Industrial Research
Abstract: The present invention provides novel lactams extracted from an alcohol extract of dehulled adlay seeds. The present invention also provides a process for the preparation of the lactams and a method for treating breast cancer in a subject, which method comprises administering to said subject an effective amount of the lactam and a pharmaceutically acceptable carrier or excipient.
Abstract: Provided herein are compounds, compositions, and methods in the field of medicinal chemistry. The compounds and compositions provided herein relate to spiro-oxindoles which function as antagonists of the interaction between p53 and MDM2, and their use as therapeutics for the treatment of cancer and other diseases.
Type:
Grant
Filed:
May 11, 2012
Date of Patent:
January 14, 2014
Assignees:
The Regents of the University of Michigan, Sanofi
Inventors:
Shaomeng Wang, Wei Sun, Angelo Aguilar, Carlos Garcia-Echeverria
Abstract: A process for preparing optically active 2-methylalkan-1-ol of the general formula (III) comprising the following steps: (i) carbonyl-selective reduction of 2-methylalk-2-en-1-al of the general formula (I) to 2-methylalk-2-en-1-ol of the general formula (II), (ii) enantioselective hydrogenation of 2-methylalk-2-en-1-ol to the general formula (iii), (iii) increasing the optical yield of the optically active 2-methylalkan-1-ol (III) obtained in step (ii) by a lipase-catalyzed acylation reaction, where the radical R means C1-C10-alkyl.
Type:
Grant
Filed:
October 18, 2010
Date of Patent:
January 7, 2014
Assignee:
BASF SE
Inventors:
Christoph Jäkel, Gunnar Heydrich, Rainer Stürmer, Rocco Paciello
Abstract: Protein tyrosine phosphatase (PTP) Shp2 is a non-receptor PTP that involved in cell signaling and regulation of cell proliferation, differentiation, and migration. Shp2 mediates activation of kinases that are involved in the pathogenesis of human carcinoma. A high throughput screen identified compounds that inhibit the PTP Shp2. Several compounds were identified that selectively inhibit Shp2 over Shp1 with low to sub-micromolar activity. Also disclosed are methods of inhibiting a protein tyrosine phosphatase in a cell and treating cancer through selective inhibition of Shp2.
Type:
Grant
Filed:
October 17, 2011
Date of Patent:
January 7, 2014
Assignee:
H. Lee Moffitt Cancer Center and Research Institute, Inc.
Inventors:
Jie Wu, Nicholas James Lawrence, Said M. Sebti, Harshani Rithma Lawrence
Abstract: The present invention provides an indolecarboxylic acid derivative having DP receptor antagonistic activity and a pharmaceutical composition comprising the said compound as an active ingredient, and further a therapeutic agent for treating allergic diseases. A compound of the general formula (I): wherein the ring A is an aromatic carbocyclic ring etc.; the ring B is a nitrogen-containing non-aromatic heterocyclic ring etc.; the formula of —X1?X2—X3?X4— is a formula of —C(R1)?C(R2)—C(R3)?C(R4)— etc.; X5 is C(R5) or N; R1, R2, R3, R4 and R5 is independently a hydrogen atom, a halogen atom etc; R6 is a formula of —Z—R10 etc. wherein Z is alkylene etc., and R10 is carboxy etc.; R7 is optionally substituted alkyloxy etc.; R8 is independently a halogen atom etc.; R9 is independently optionally substituted alkyl etc.; Y is a single bond etc.; n is 0 etc.; q is 0 etc.; a pharmaceutically acceptable salt or a solvate thereof.
Abstract: Compounds of the present invention and pharmaceutically acceptable compositions thereof, are useful as modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator (“CFFR”). The present invention also relates to methods of treating ABC transporter mediated diseases using compounds of the present invention.
Type:
Grant
Filed:
April 26, 2010
Date of Patent:
January 7, 2014
Assignee:
Vertex Pharmaceuticals Incorporated
Inventors:
Sara S. Hadida Ruah, Peter D. J. Grootenhuis, Fredrick F. van Goor, Jinglan Zhou, Brian Bear, Mark T. Miller, Jason McCartney, Mehdi Michel Djamel Numa
Abstract: A compound of formula (I) or a compound of formula (II) or pharmaceutically acceptable salts thereof, wherein R1-R7 and X are as defined in the description, and the use of these compounds in therapy, in particular in treating cancer or as an inhibitor of the interaction of the MDM2 protein with p53.
Type:
Grant
Filed:
June 25, 2009
Date of Patent:
December 31, 2013
Assignee:
Cancer Research Technology Limited
Inventors:
Bernard Thomas Golding, Christiane Riedinger, Roger John Griffin, Ian Robert Hardcastle, Eric Valeur, Anna Frances Watson, Martin Noble