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KIT FOR AUTOMATED RESOLVING AGENT SELECTION AND METHOD THEREOF

Application Number: 20120041225
Publication Date: 2012-02-16
Inventor: Vaidya, Niteen A.

The present invention provides a means for the rapid selection of optimum resolving agents and solvents, combinations and conditions to separate optical isomers. The present invention combinedly describes and automates a full lifecycle of chiral separation method development and optimization through a series of kits and procedures providing screening, automation for screening, racemate recovery, enantiomer preparation, and method ...

Process For The Iodination Of Aromatic Compounds

Application Number: 20120041224
Publication Date: 2012-02-16
Inventors: Lattuada, Luciano; Citterio, Attilio; Fretta, Roberta; Uggeri, Fulvio; Leonardi, Gabriella; Vignale, Evelin; Visigalli, Massimo; Ferrigato, Aurelia; Meli, Gabriele; Mazzon, Roberta

The present invention relates to a process for the preparation of iodinated anilines; in particular, it relates to a process including the direct iodination, with suitably activated iodine, of 3,5-disubstituted anilines to the corresponding 3,5-disubstituted-2,4,6-triiodoanilines, which are useful intermediates for the synthesis of x-ray contrast media, and to the preparation of the contrast media themselves.

PROCESS FOR PREPARING AROMATIC CARBAMATES

Application Number: 20120041223
Publication Date: 2012-02-16
Inventors: Wershofen, Stefan; Klein, Stephan; Vidal-Ferran, Anton; Reixach, Elisenda; Rius-Ruiz, Francese Xavier

The invention is directed to a process for preparing aromatic carbamates which comprises the reaction of an aromatic amine with an organic carbonate in the presence of a catalyst characterized in that Zn₄O(OAc)₆is used as ...

Proteasome Inhibitors and Methods of Using the Same

Application Number: 20120041196
Publication Date: 2012-02-16
Inventors: De Munari, Sergio; D'Arasmo, Germano; Menta, Ernesto; Bernardini, Raffaella; Bernareggi, Alberto; Chatterjee, Sankar; Oliva, Ambrogio; Iqbal, Mohamed; Ferretti, Edmondo; Cassará, Paolo G.; Messina McLaughlin, Patricia A.

The present invention provides boronic acid compounds, boronic esters, and compositions thereof that can modulate apoptosis such as by inhibition of proteasome activity. The compounds and compositions can be used in methods of inducing apoptosis and treating diseases such as cancer and other disorders associated directly of indirectly with proteasome ...

PHOSPHINATE RUTHENIUM COMPLEXES

Application Number: 20120041191
Publication Date: 2012-02-16
Inventors: Parsy, Christophe Claude; Alexandre, Francois-Rene; Surleraux, Dominique; Bonnaterre, Florence Marie-Emilie

Provided herein are ruthenium complexes of Formula (I), and processes of preparation thereof. Also provided are methods of their use as a metathesis catalyst.

ANTITUMORAL COMPOUNDS

Application Number: 20120041063
Publication Date: 2012-02-16
Inventors: Rodriguez Vicente, Alberto; Garranzo Garcia- Ibarrola, Maria; Murcia Perez, Carmen; Sanchez Sancho, Francisco; Cuevas Marchante, Maria del Carmen; Mateo Urbano, Cristina; Digon Juarez, Isabel

A compound of general formula (I)
wherein, R₁₁, R₁₂, R₁₃, R₁₄, R₁₅, W, Y, R₁, R₂, R₃, R₄, R₅, and R₆take various meanings for use in the treatment of cancer. ...

COMPOUND OF SALVIANOLIC ACID L, PREPARATION METHOD AND USE THEREOF

Application Number: 20120041062
Publication Date: 2012-02-16
Inventors: Zhou, Shuiping; Li, Wei; Jin, Yuanpeng; Ma, Xiaohui; Han, Jianping; Cui, Hongfang; Luo, Xuejun; Chen, Xiaopeng

The present invention relates to a new compound of salvianolic acid L, its preparation method, a pharmaceutical composition containing the salvianolic acid L, and its use for preparing a medicament for treating cardio-cerebrovascular ...

NEUROPROTECTIVE MULTIFUNCTIONAL COMPOUNDS AND PHARMACEUTICAL COMPOSITIONS COMPRISING THEM

Application Number: 20120040993
Publication Date: 2012-02-16
Inventors: Fridkin, Mati; Youdim, Moussa B. H.; Zheng, Hailin

Multifunctional compounds are provided, comprising two or more functional moieties selected from: (i) a moiety that imparts an iron chelator function; (ii) a moiety that imparts a neuroprotective function; (iii) a moiety that imparts combined antiapoptotic, neuroprotective and/or neurorestorative functions; (iv) a moiety that imparts brain MAO inhibition, preferably with little or no MAO inhibition in liver and small intestine; (v) a moiety that imparts cholinesterase inhibitory function; and ...

THIADIAZOLE AND OXADIAZOLE DERIVATIVES, PREPARATION THEREOF AND THERAPEUTIC USE THEREOF

Application Number: 20120040984
Publication Date: 2012-02-16
Inventors: Nicolai, Eric; Fett, Eykmar; Mougenot, Patrick; Namane, Claudie; Philippo, Christophe

The invention relates to compounds of the formula (I) either (i) in the state of a base or an acid addition salt, or (ii) in the state of an acid or a base addition salt, as well as to a method for preparing same and to the therapeutic applications thereof.

MEDICINAL USE OF 5-BENZYLAMINOSALICYLIC ACID DERIVATIVE OR ITS SALT

Application Number: 20120040939
Publication Date: 2012-02-16
Inventors: Gwag, Byoung-Joo; Son, Sun-Joo; Noh, Jae-Sung; Shin, Jin-Hee

The present invention relates to a pharmaceutical composition for treating or preventing stress disorder, depression, anxiety disorder, comprising 5-benzylaminosalicylic acid derivative or its pharmaceutically acceptable salt. The present invention relates to a method for treating or preventing stress disorder, depression, anxiety disorder, comprising 5-benzylaminosalicylic acid derivative or its pharmaceutically acceptable ...

SURFACE TREATING AGENT, ARTICLE AND FLUORINATED ETHER COMPOUND

Application Number: 20120040189
Publication Date: 2012-02-16
Inventors: Gozu, Yoshiyuki; Shirakawa, Daisuke; Hoshino, Taiki

To provide a surface treating agent and a composition for surface treatment capable of forming a coating film excellent in the water/oil repellency, the efficiency for removal of oil-and-fat stains, alkali resistance and heat resistance and having a low coefficient of friction; a method for treating the surface of an article by using the surface treating agent or the composition for surface treatment; an article having surface treatment applied; and a novel fluorinated ether compound useful as ...

ALKYNES AND METHODS OF REACTING ALKYNES WITH 1,3-DIPOLE-FUNCTIONAL COMPOUNDS

Application Number: 20120040011
Publication Date: 2012-02-16
Inventors: Boons, Geert-Jan; Guo, Jun; Ning, Xinghai; Wolfert, Margaretha

1,3-Dipole-functional compounds (e.g., azide functional compounds) can be reacted with certain alkynes in a cyclization reaction to form heterocyclic compounds. Useful alkynes (e.g., strained, cyclic alkynes) and methods of making such alkynes are also disclosed. The reaction of 1,3-dipole-functional compounds with alkynes can be used for a wide variety of applications including the immobilization of biomolecules on a ...

INTEGRATED PROCESS FOR PRODUCING ALCOHOLS FROM A MIXED ACID FEED

Application Number: 20120036769
Publication Date: 2012-02-16
Inventors: Horton, Trinity; JOHNSTON, Victor; SARAGER, Lincoln; JEVTIC, Radmila; WARNER, R. Jay; Lee, David; WEINER, Heiko; SCATES, Mark; SHAVER, Ronald David; TORRENCE, G. Paull; Zink, James

Processes for producing alcohols such as ethanol and propanol from a mixed acid feedstock in an integrated process. In one embodiment, the process comprises the step of carbonylating methanol in the presence of a carbonylation catalyst to form a mixed acid feedstock comprising acetic acid and one or more higher acids, preferably comprising propionic acid. The mixed acid feed is hydrogenated in the presence of a hydrogenation catalyst to form a crude alcohol product comprising ethanol and one or ...

PROCESS FOR THE PREPARATION OF POLYISOCYANATES AND USE THEREOF

Application Number: 20120035391
Publication Date: 2012-02-09
Inventors: Richter, Frank; Brahm, Martin

The invention relates to a process for isocyanate modification which includes reacting a) at least one organic isocyanate having an NCO functionality greater than or equal to 1, b) a catalyst comprising at least one phosphonium salt comprising at least one cycloalkyl substituent bonded directly to a P atom of a phosphonium cation, c) optionally a solvent, and d) optionally additives. The present invention also relates to a catalyst for isocyanate modification comprising at least one phosphonium ...

Ethyl acetate production

Application Number: 20120035390
Publication Date: 2012-02-09
Inventor: Gadewar, Sagar B.

A process for the production of high purity ethyl acetate from ethanol is described. The process involves reacting ethanol over a suitable catalyst in a reactive distillation column. The reactive distillation setup allows overcoming the reaction equilibrium for increased conversion of ethanol. Hydrogen is removed as the distillate and ethyl acetate is obtained as a bottoms product from the reactive distillation column. A feed of hydrogen at the bottom of the column and a suitable hydrogenation ...

METHOD FOR PURIFYING THE AZEOTROPIC FRACTION GENERATED DURING THE SYNTHESIS OF N,N-DIMETHYL AMINOETHYL ACRYLATE

Application Number: 20120035389
Publication Date: 2012-02-09
Inventors: Paul, Jean-Michel; Graire, Coralie; Riehl, Audrey

The invention relates to a method for producing N,N-dimethylaminoethyl acrylate by the transesterification reaction of an alykl acrylate by N1N-dimethylaminoethanol, and more particularly relates to a method for purifying the azeotropic fraction generated during said reaction, thereby enabling the recycling thereof on the alkyl acrylate production unit. The aim of the method of the invention is in particular to remove the acetaldehyde and the dialkoxyethane contained in the azeotropic ...

PLATINUM/CARBON NANOTUBE CATALYST, THE PREPARATION PROCESS AND USE THEREOF

Application Number: 20120035388
Publication Date: 2012-02-09
Inventors: Chen, Zhijian; Li, Can

This invention provides a platinum/carbon nanotube catalyst applicable to heterogeneous asymmetric hydrogenation, which is fabricated by supporting platinum on carbon nanotube carriers. The catalyst is prepared by the steps of: heating purified carbon nanotubes in nitric acid, filtering and washing the same with water until pH value of the filtrate becomes neutral, drying the carbon nanotubes; immersing the carbon nanotube carriers obtained in an aqueous chloroplatinic acid solution and ...

METHOD FOR PRODUCING OPTICALLY ACTIVE DIAMINE DERIVATIVE

Application Number: 20120035369
Publication Date: 2012-02-09
Inventor: Kawanami, Koutarou

The problem to be solved is to provide an important intermediate for production of an FXa inhibitor. The solution thereto is a method for industrially producing a compound (1) or a compound (4), comprising: [Step 1]: adding a quaternary ammonium salt and a metal azide salt to water to prepare an aqueous solution of an azidification reagent complex comprising quaternary ammonium salt-metal azide salt, and subsequently dehydrating the aqueous solution using an aromatic hydrocarbon solvent to form ...

METHODS OF MAKING 6-HYDROXYHEXANOPHENONE AND 5-BENZOYLPENTANOIC ACID AND MONO OR DIESTERS THEREOF

Application Number: 20120035308
Publication Date: 2012-02-09
Inventors: Godwin, Allen David; Mozeleski, Edmund John; Smirnova, Diana S.; Baugh, Lisa Saunders; Zushma, Stephen; Dakka, Jihad Mohammed; Benitez, Francisco Manuel; Wang, Kun

Mono- or diester plasticizers of the formula:

wherein A is either —OC(O)R′ or ═O, and X is either —COC(O)R or —C(O)OR, and R and R′ are C₃to C₁₃alkyl, which are the same or different, formed from cyclohexylbenzene and processes of making ...

METHOD FOR INHIBITING CRYSTAL GROWTH RATE OF AMIDE COMPOUND AND METHOD FOR PRODUCING MOLDED ARTICLE OF POLYOLEFIN-BASED RESIN

Application Number: 20120035304
Publication Date: 2012-02-09
Inventors: Uchiyama, Yohei; Ikoma, Reira; Iwasaki, Shohei

A method for inhibiting the crystal growth rate of an amide compound present in a molten polyolefin-based resin and a method for producing a polyolefin-based resin molded article are provided.

A phenol compound is incorporated into an amide compound-containing polyolefin-based resin such that a weight ratio, amide compound:phenol compound, is 60:40 to ...

DEUTERIUM-ENRICHED SAXAGLIPTIN

Application Number: 20120035261
Publication Date: 2012-02-09
Inventor: Czarnik, Anthony W.

The present application describes deuterium-enriched saxagliptin, pharmaceutically acceptable salt forms thereof, and methods of treating using the ...

TELLURIUM-CONTAINING COMPOUNDS FOR AFFECTING FEMALE"S REPRODUCTIVE SYSTEM FOLLOWING CHEMOTHERAPY AND/OR RADIOTHERAPY

Application Number: 20120035260
Publication Date: 2012-02-09
Inventors: Albeck, Michael; Sredni, Benjamin; Meirow, Dror; Ron, Benjamin

Use of tellurium-containing compounds in a method of conception and/or for maintaining and/or augmenting fertility in female following chemotherapy and/or radiotherapy is disclosed. The tellurium-containing compound is utilized in combination with a chemotherapeutic agent and/or radiation, such that the female treated by the chemotherapeutic agent and/or radiation and by the tellurium-containing compound is instructed to refrain from conceptive sex for a pre-determined time period, following ...

OXADIAZOLE DERIVATIVES

Application Number: 20120035226
Publication Date: 2012-02-09
Inventors: Crosignani, Stefano; Sauer, Wolfgang; Quattropani, Anna; Montagne, Cyril; Bombrun, Agnés

The invention relates to oxadiazole compounds of formula I. The compounds are useful e.g. in the treatment of autoimmune disorders, such as multiple ...

Betulin derived compounds as anti-feedants for plant pests

Application Number: 20120035224
Publication Date: 2012-02-09
Inventors: Yli-Kauhaluoma, Jari; Bergström, Pia; Alakurtti, Sami; Mäkelä, Taru; Koskimies, Salem; Hokkanen, Heikki; Menzler-Hokkanen, Ingeborg

The invention relates to compounds derived from betulin, and to the use thereof in plant pest control, particularly as antifeedants for butterfly larvae, beetles and snails. Further, the invention relates to novel betulin derivatives and methods for the production thereof either directly from betulin, or via intermediates derived ...

CARBOXYLIC ACID COMPOUND

Application Number: 20120035196
Publication Date: 2012-02-09
Inventors: Watanabe, Hideyuki; Ohnuki, Kei; Urano, Yasuharu; Kuramoto, Kazuyuki; Yonetoku, Yasuhiro; Negoro, Kenji

[Problem]

The present invention has an object to provide a compound having a GPR40 agonistic activity, which is useful as a pharmaceutical composition, an insulin secretion promoter, or an agent for preventing/treating diabetes.

[Means for Solution]

The present inventors have extensively studied a compound having a GPR40 agonistic activity, and as a result, they have found that the compound (I) of the ...

PROCESS FOR PRODUCING OPTICALLY ACTIVE SUCCINIMIDE DERIVATIVES AND INTERMEDIATES THEREOF

Application Number: 20120034660
Publication Date: 2012-02-09
Inventors: Kasai, Masaji; Kita, Shinji; Ogawa, Tadashi; Tokai, Hideaki

A process for producing optically active succinimide derivatives as key intermediates of (3R)-2′-(4-bromo-2-fluorobenzyl)spiro{pyrrolidine-3,4′(1H)-pyrrolo[1,2-a]pyrazine}-1′,2,3′,5(2′H)-tetraone, which comprises the following reaction steps.

PHARMACEUTICAL COMPOSITION COMPRISING ONE OR MORE FUMARIC ACID ESTERS

Application Number: 20120034274
Publication Date: 2012-02-09
Inventors: Rupp, Roland; Nilsson, Henrik

A pharmaceutical controlled release composition comprising one or more fumaric acid ...

SULPHURATED DERIVATIVES OF RESORCINOL, PREPARATION OF SAME AND COSMETIC USES THEREOF

Application Number: 20120034176
Publication Date: 2012-02-09
Inventor: Poigny, Stéphane

The present invention relates to a compound of the general formula (I) where: X═S, SO or SO₂; and one of the radicals R₁and R₂is a hydrogen atom and the other is a radical: a C₁to C₁₈linear or branched alkyl, optionally substituted by one or more halogen atom(s); a C₂to C₁₈linear or branched alkenyl, optionally substituted by one or more halogen atom(s); an aralkyl, optionally substituted by one or more C_{1 ...}

PREPARATION OF MONOBASIC PHOSPHATE IONOPHORES

Application Number: 20120031775
Publication Date: 2012-02-09
Inventor: Ahmad, Mohd Rais

The present invention relates to the synthesis of lipophilic or immobilized monobasic phosphate (H₂PO₄) ionophores (7, 8a, 8b and 11) to be used as ion recognition molecules for monobasic phosphate (H2PO₄″) in the cocktail preparation of hydrophobic polymer membranes in ion selective electrode (ISE) or ion-sensitive field effect transistor (ISFET) chemical sensors for detection of monobasic phosphate (H₂PO₄) ionic species in soil, ...

METHOD FOR STORING TRANSDERMALLY/TRANSMUCOSALLY ABSORBABLE PREPARATION AND PACKAGE OF TRANSDERMALLY/TRANSMUCOSALLY ABSORBABLE PREPARATION

Application Number: 20120031047
Publication Date: 2012-02-09
Inventors: SHINODA, Tomohiro; Yasukouchi, Takashi; Takada, Yasunori

A method for storing a transdermally/transmucosally absorbable preparation, comprising keeping a transdermally/transmucosally absorbable preparation enclosed in a container in a low oxygen atmosphere, the transdermally/transmucosally absorbable preparation comprising a drug whose molecule has an amino group substituted with a lower alkyl ...

PROCESSES FOR PRODUCING ALCOHOLS FROM A MIXED ACID FEED

Application Number: 20120030995
Publication Date: 2012-02-09
Inventors: HORTON, Trinity; JEVTIC, Radmila; WARNER, R. Jay; JOHNSTON, Victor J.; WEINER, Heiko

Processes for producing alcohols such as ethanol and propanol from a mixed acid feedstock. In one embodiment, the process comprises the steps of hydrogenating a mixed acid feedstock comprising acetic acid and one or more higher acids, preferably comprising propionic acid, in the presence of a catalyst to form a crude alcohol product comprising ethanol and one or more higher alcohols, preferably including ...

METHOD FOR PRODUCING HIGH PURITY TERMINAL OLEFIN COMPOUND

Application Number: 20120029229
Publication Date: 2012-02-02
Inventors: Miyoshi, Kei; Asanuma, Goro

An industrially advantageous method for producing a high purity terminal olefin is disclosed, comprising the steps of (a) contacting a mixture comprising a terminal olefin represented by formula (1):

and one or more corresponding internal olefins as impurities, with a brominating agent in the presence of water or an alcohol, to convert the internal olefin(s) to compound(s) having a higher boiling point than the terminal olefin; and ...

CHEMICAL RECYCLING OF PLA BY ALCOHOLYSIS

Application Number: 20120029228
Publication Date: 2012-02-02
Inventors: Bogaert, Jean-Christophe; Coszach, Philippe; Willocq, Jonathan

A process for recycling a polymer blend necessarily containing PLA, comprising grinding, compacting, dissolving in a solvent of PLA, removing the undissolved contamining polymers, alcoholysis depolymerisation reaction and purification ...

METHOD FOR PRODUCING CYCLOPROPANECARBOXYLIC ACID ESTER

Application Number: 20120029227
Publication Date: 2012-02-02
Inventors: Uekawa, Toru; Ohshita, Jun

A method for producing a cyclopropanecarboxylate represented by formula (III):

wherein, R represents a chain hydrocarbon group having 1 to 10 carbon atoms optionally having at least one member selected from the group consisting of halogen atoms, acyl groups having 2 to 7 carbon atoms optionally having a substituent, alkoxy groups having 1 to 7 carbon atoms optionally having a substituent, alkylthio groups having 1 to 3 carbon atoms ...

METHOD FOR THE SYNTHESIS OF CHIRAL ALPHA-ARYL PROPIONIC ACID DERIVATIVES

Application Number: 20120029226
Publication Date: 2012-02-02
Inventors: Kaptein, Bernardus; Vlieg, Elias; Noorduin, Willem Lieuwe

The present invention provides a method for the synthesis of optically pure α-aryl propionic acid derivatives comprising subjecting the corresponding racemic α-aryl propionic acid derivatives to high sheer or impact forces, such as ...

Catalytic Wittig and Mitsunobu Reactions

Application Number: 20120029211
Publication Date: 2012-02-02
Inventor: O'Brien, Christopher J.

A catalytic Wittig method utilizing a phosphine including the steps of providing a phosphine oxide precatalyst and reducing the phosphine oxide precatalyst to produce the phosphine; forming a phosphonium ylide precursor from the phosphine and a reactant; generating a phosphonium ylide from the phosphonium ylide precursor; reacting the phosphonium ylide precursor with the aldehyde, ketone, or ester to form the olefin and the phosphine oxide which then reenters the cycle. The invention is also ...

ESTERS OF O-SUBSTITUTED HYDROXY CARBOXYLIC ACIDS AND PREPARATIONS THEREOF

Application Number: 20120029198
Publication Date: 2012-02-02
Inventors: Deng, Liu; Boaz, Neil Warren

Esters of O-substituted hydroxy carboxylic acids are provided having Formula 1, or 2, or both Formulas 1 and 2:

wherein R and R¹are independently selected from the group consisting of substituted and unsubstituted, branched- and straight-chain, saturated, unsaturated, and polyunsaturated C₁-C₂₂alkyl, substituted and unsubstituted C₃-C₈cycloalkyl, substituted and unsubstituted ...

METHOD FOR PRODUCING ALCOHOL COMPOUND AND CATALYST THEREFOR

Application Number: 20120029195
Publication Date: 2012-02-02
Inventors: Hagiya, Koji; Souda, Hiroshi; Aoyagi, Yasutaka

A method for producing an alcohol compound, wherein a carboxylic acid ester compound is reduced with hydrogen in the presence of a ruthenium complex which is obtained by reacting a pyridine compound having at least one optionally substituted amino group with a ruthenium ...

CARBON NANOTUBES COMPRISING HYDROXY GROUPS, METHOD FOR THE PRODUCTION THEREOF AND POLYURETHANE POLYMERS COMPRISING SAID CARBON NANOTUBES

Application Number: 20120029162
Publication Date: 2012-02-02
Inventors: Hofmann, Jörg; Vogel, Stephanie; Nefzger, Hartmut

The invention relates to carbon nanotubes comprising hydroxy groups, wherein the surface thereof comprises hydroxy alkyl ester groups covalently bound thereon, chosen from the group according to the general formula (1) and/or the general formula (2), wherein (CNT) stands for the surface of the carbon nanotube and R1 and R2 are independently from each other hydrocarbon, an alkyl radical or an aryl radical. The invention further relates to a method for the production thereof by means of reaction ...

HIGH-FUNCTIONALITY POLYISOCYANATES CONTAINING URETHANE GROUPS

Application Number: 20120029144
Publication Date: 2012-02-02
Inventors: Steinbrecher, Angelika Maria; Elizalde, Oihana; Lucas, Frederic; Tuchbreiter, Lydie

The present invention relates to new, urethane-group-containing polyisocyanates based on aliphatic and/or cycloaliphatic diisocyanates, and to their ...

NOVEL OLIGOFUNCTIONAL PHOTOINITIATORS

Application Number: 20120029107
Publication Date: 2012-02-02
Inventors: Birbaum, Jean-Luc; Berens, Ulrich; Studer, Katia

The invention pertains to novel oligofunctional photoinitiators of the formula (1) or (1A). R₁and R₂are methyl or together are —(CH₂)₅—; and n is 2 or 3, and the solvent in (1A) is water or an organic solvent; and their use in photopolymerizable compositions, in particular inks.

PLEUROMUTILIN DERIVATIVES FOR THE TREATMENT OF DISEASES MEDIATED BY MICROBES

Application Number: 20120029072
Publication Date: 2012-02-02
Inventors: Ferencic, Mathias; Mang, Rosemarie; Novak, Rodger; Heilmayer, Werner; Badegruber, Rudolf; Strickmann, Dirk B.; Murty Bulusu, Atchyuta Rama Chandra

Disclosed are pleuromutilin derivatives of formula (I)

an their use in the treatment of diseases mediated by ...

Polyphenol Proteasome Inhibitors, Synthesis, and Methods of Use

Application Number: 20120029067
Publication Date: 2012-02-02
Inventors: DOU, Q. Ping; CHAN, Tak-Hang; SMITH, David M.

The present invention relates to synthetic green tea derived polyphenolic compounds, their modes of syntheses, and their use in inhibiting proteasomal activity and in treating cancers. The present invention is also directed to pharmaceutical compositions useful in methods of inhibiting proteasomes and of treating ...

2-AMINO-BICYCLO[3.1.0]HEXANE-2, 6-DICARBOXYLIC ESTER DERIVATIVE

Application Number: 20120028982
Publication Date: 2012-02-02
Inventors: Sakagami, Kazunari; Nakazato, Atsuro; YASUHARA, Akito; Ohta, Hiroshi

A drug effective for the treatment and prevention of psychiatric disorders such as schizophrenia, anxiety and related ailments thereof, depression, bipolar disorder and epilepsy. The drug antagonizes the action of group II metabotropic glutamate receptors and shows high activity in oral administration. A 2-amino-bicyclo[3.1.0]hexane-2,6-dicarboxylic ester derivative represented by formula [I]

[wherein R¹and R^{2 ...}

ABUSE DETERRENT AND ANTI-DOSE DUMPING PHARMACEUTICAL SALTS USEFUL FOR THE TREATMENT OF ATTENTION DEFICIT/HYPERACTIVITY DISORDER

Application Number: 20120028960
Publication Date: 2012-02-02
Inventors: King, Clifford Riley; D'Ambrosio, Stephen G.; Bristol, David W.

A pharmaceutical composition comprising a drug substance consisting essentially of a pharmaceutically acceptable organic acid addition salt of an amine containing pharmaceutically active compound wherein the amine containing pharmaceutical active compound is selected from the group consisting of racemic or single isomer ritalinic acid or phenethylamine derivatives and the drug substance has a physical form selected from amorphous and ...

ENZYMATIC PROCESS FOR THE PREPARATION OF (S)-5-(4-FLUORO-PHENYL)-5-HYDROXY- 1MORPHOLIN-4-YL-PENTAN-1-ONE, AN INTERMEDIATE OF EZETIMIBE AND FURTHER CONVERSION TO EZETIMIBE

Application Number: 20120028316
Publication Date: 2012-02-02
Inventors: Husain, Mofazzal; Srikanth, G.S.C; Thorpunuri, Swapna; Debashish, Datta

The present invention provides an enzymatic process for the preparation of (S)-5-(4-Fluoro-phenyl)-5-hydroxy-1morpholin-4-yl-pentan-1-one by the reduction of 1-(4-Fluoro-phenyl)-5-morpholin-4-yl-pentane-1,5-dione by using a suitable enzyme or by the resolution of (R,S)-5-(4-Fluoro-phenyl)-5-hydroxy-1morpholin-4-yl-pentan-1-one by using an enzyme. The present invention also provides process for the preparation of Ezetimibe comprising the steps of a) protecting the compound ...

RADIATION-SENSITIVE RESIN COMPOSITION, METHOD FOR FORMING RESIST PATTERN, POLYMER AND COMPOUND

Application Number: 20120028189
Publication Date: 2012-02-02
Inventors: Sato, Mitsuo; Asano, Yusuke

A radiation-sensitive resin composition includes (A) a fluorine-containing compound that includes a group shown by the following formula (1), and (B) a photoacid generator.

wherein R^Crepresents a (p+1)-valent aromatic ring group, Q represents a linking group obtained by removing one hydrogen atom from a monovalent hydrophilic group, R^Erepresents a hydrogen atom or a hydrocarbon group having 1 to 10 carbon ...

ELECTROLYTE, AND SECONDARY BATTERY COMPRISING SAME

Application Number: 20120028133
Publication Date: 2012-02-02
Inventors: Kim, Yo Jin; Choi, Seung Don; Lee, Han Ho

Provided are an electrolyte which may prevent the degradation of the battery performance by including a functional group which can react with a side reaction site which is responsible for decomposition of negative electrode material components and a functional group which can react with moisture which is responsible for decomposition of positive electrode material components in an electrolyte of the battery to ensure the stability of the battery at high temperatures, and a secondary battery ...

Polyester Based Degradable Materials and Implantable Biomedical Articles Formed Therefrom

Application Number: 20120027719
Publication Date: 2012-02-02
Inventors: Ashby, Valerie; Olson, David

A method of making an aliphatic polyester prepolymer, comprising: reacting, alone or in combination with other reactants, a diol with at least a first diacid (or a diester of said first diacid) to produce an aliphatic polyester prepolymer. The first diacid is preferably a trans-beta-hydromuconic acid (HMA). In some embodiments, the diol contains at least one ether linkage. In some embodiments the diol is further reacted with at a second diacid, or a diester of said second diacid, wherein said ...

OXIME CONJUGATES AND METHODS FOR THEIR FORMATION AND USE

Application Number: 20120027680
Publication Date: 2012-02-02
Inventors: Yurkovetskiy, Alexander; Papisov, Mikhail I.

The present invention relates to biodegradable biocompatible polyketals, methods for their preparation, and methods for treating animals by administration of biodegradable biocompatible polyketals. In one aspect, a method for forming the biodegradable biocompatible polyketals comprises combining a glycol-specific oxidizing agent with a polysaccharide to form an aldehyde intermediate, which is combined with a reducing agent to form the biodegradable biocompatible polyketal. The resultant ...