Abstract: The present invention provides a compound represented by the following general formula (A) wherein 1?-position is optically active; and one of R1 and R2 represents a methyl group and the other represents an ethyl group, or both R1 and R2 represent a methyl group.
Abstract: The present technology relates to a rhodium catalyzed carbonylation process of alcohols, ethers, and esters in the presence of phosphine oxide and ruthenium additives to produce carboxylic acids. In some embodiments, the technology provides for an improved method of preparing acetic acid from methyl acetate or methanol using a rhodium catalyst with a phosphine oxide and a ruthenium additive.
Type:
Application
Filed:
January 18, 2016
Publication date:
July 21, 2016
Applicant:
LyondellBasell Acetyls, LLC
Inventors:
Noel C. Hallinan, David L. Ramage, Daniel F. White
Abstract: An object is to provide a novel method for processing an organic substance with a catalyst under conditions in the presence of water. According to the present invention, there is provided a method of processing an organic substance under a hydrothermal condition by utilizing an oxidation-reduction cycle of a metal oxide catalyst, the method including: (i) oxidizing an organic substance with oxygen discharged from a metal oxide catalyst having an oxidized metal value so as to form a metal oxide catalyst having a reduced metal value and an oxidized organic substance; and (ii) oxidizing, simultaneously with the above (i), the metal oxide catalyst having the reduced metal value with oxygen discharged from water so as to reproduce the metal oxide catalyst having the oxidized metal value, where the metal oxide catalyst is a solid electrolyte.
Abstract: The present invention is in the field of producing bio-based commodity organic chemicals such as bio-acrylic acid, bio-acrylonitrile, and bio-1,4-butanediol using renewable carbon sources as feedstock. In the first stage of the present invention, bio-1,3-propanediol is derived from renewable carbon sources through microbial fermentation. In the second stage of the present invention, bio-1,3-propanediol is converted into bio-acrylic acid or bio-acrylonitrile or bio-1,4-butanediol.
Abstract: A process for the production of organic acids having at least three carbon atoms comprises the steps of forming an amount of carbon monoxide and reacting the amount of carbon monoxide with an amount of an unsaturated hydrocarbon. The reaction is preferably carried out in the presence of a supported palladium catalyst, a strong acid, and a phosphine. In some embodiments, the unsaturated hydrocarbon is one of acetylene and methylacetylene, and the organic acid is one of acrylic acid and methyl acrylic acid. The reacting step is preferably performed with carbon monoxide produced from carbon dioxide.
Type:
Application
Filed:
November 20, 2015
Publication date:
July 21, 2016
Inventors:
Richard I. Masel, Zheng Richard Ni, Qingmei Chen, Brian A. Rosen
Abstract: Disclosed is a method of making methacrylic acid, or a carboxylic derivative thereof, from itaconic acid, isomers, or precursors thereof. A starting material comprising an acid selected from the group consisting of itaconic acid, citraconic acid, mesaconic acid, citric acid, aconitic acid, isocitric acid and mixtures thereof, is subjected to contact with 0.1 eq. to 3.0 eq. of a base, at a temperature of 150° C. to 350° C., under the influence of a transition metal-containing heterogeneous catalyst. A better yield at lower temperatures is achieved.
Type:
Application
Filed:
August 26, 2014
Publication date:
July 21, 2016
Inventors:
Jerome Emile Lucien Le Notre, Elinor Lindsey Scott, Roeland Leo Croes, Jacobus Van Haveren
Abstract: A method of producing lactic acid includes filtering a lactic acid-containing aqueous solution through a nanofiltration membrane to recover an aqueous lactic acid solution from the permeate side (Step A); distilling the aqueous lactic acid solution to recover lactic acid from the vapor side (Step B); and crystallizing the lactic acid obtain in Step B, and performing solid-liquid separation to recover a lactic acid crystal(s) (Step C).
Abstract: A cardiogenin major isomer is obtained from a methanol extract of Geum japonicum and separated from its minor isomer. The separation of the two isomers can be achieved by chiral phase chromatography, e.g., using a Chiralpak® IC™ column. The purity of the isolated cardiogenin major isomer can be further increased by crystallization, yielding isolated cardiogenin major isomer having HPLC purity as high as 98.97% (a/a) at 210 nm and a potency of 95.50%) (w/w).
Type:
Application
Filed:
August 28, 2015
Publication date:
July 21, 2016
Inventors:
Andreas KYAS, Ernst FREUND, Oliver SCHLÖRKE, Joerg LILL, Lars ROGALL, Dario MENIA, Gary ELLIOTT, James PATERNITI
Abstract: A process for producing methyl methacrylate, the process comprising contacting reactants comprising methacrolein, methanol and an oxygen-containing gas, under reaction conditions in the presence of a solid catalyst comprising palladium, bismuth and at least one third element X selected from the group consisting of Fe, Zn, Ge, and Pb, wherein the solid catalyst further comprises a support selected from at least one member of the group consisting of silica and alumina.
Type:
Application
Filed:
July 29, 2014
Publication date:
July 21, 2016
Inventors:
Kirk K. Limbach, Dmitri A. Kraptchetov, Christopher D. Frick
Abstract: A batchwise process for aftertreatment of polyol esters prepared by reacting polyols of the general formula (II) H—(—O—[—CR1R2—]m—)o—OH ??(II) in which R1 and R2 are each independently hydrogen, an alkyl radical having 1 to 5 carbon atoms, preferably methyl, ethyl or propyl, or a hydroxyalkyl radical having 1 to 5 carbon atoms, preferably the hydroxymethyl radical, m is an integer from 1 to 10, preferably 1 to 8 and especially 1, 2, 3 or 4, o is an integer from 2 to 15, preferably 2 to 8 and especially 2, 3, 4 or 5, with excess linear or branched aliphatic monocarboxylic acids having 3 to 20 carbon atoms and having a lower boiling point than the polyols used.
Abstract: Disclosed herein are new mixed metal oxide catalysts suitable as heterogeneous catalysts for catalyzing the transesterification process of aromatic alcohols with a dialkyl carbonate to form aromatic carbonates. The heterogeneous catalyst comprises a combination of two, three, four, or more oxides of Mo, V, Nb, Ce, Cu, Sn, or an element selected from Group IA or Group IIA of the periodic table.
Abstract: The present invention includes DNP derivatives of formula (I) that are useful for preventing or treating a metabolic disease or disorder in a subject in need thereof. In certain embodiments, the subject is further administered at least one additional therapeutic agent.
Abstract: Disclosed is a process for performing a chemical reaction selected from reductive amination and hydrogenation of a first functional group in an organic feed substrate, which feed substrate comprises at least one further functional group containing a halogen atom, wherein the halogen atom is selected from the list consisting of chlorine, bromine, iodine, and combinations thereof, in the presence of hydrogen and a heterogeneous catalyst comprising at least one metal from the list of Pd, Rh, and Ru, together with at least a second metal from the list consisting of Ag, Ni, Co, Sn, Cu and Au. The process is preferably applied for the reductive amination of 2-chloro-benzaldehyde to form 2-chloro-benzyldimethylamine, as an intermediate in the production of agrochemically active compounds and microbiocides of the methoximinophenylglyoxylic ester series.
Type:
Application
Filed:
August 26, 2014
Publication date:
July 21, 2016
Applicant:
Taminco BVBA
Inventors:
Kristof Moonen, Bart Vandeputte, Daan Scheldeman, Kim Dumoleijn
Abstract: A method for producing trans-bis(aminomethyl)cyclohexane includes a trans-isomerization step in which cis-dicyanocyclohexane is isomerized into trans-dicyanocyclohexane by heating dicyanocyclohexane containing cis-dicyanocyclohexane in the presence of a tar component produced by distillation of dicyanocyclohexane; and an aminomethylation step in which trans-dicyanocyclohexane produced by the trans-isomerization step is allowed to contact with hydrogen to produce trans-bis(aminomethyl)cyclohexane.
Type:
Application
Filed:
July 25, 2014
Publication date:
July 21, 2016
Inventors:
Takeshi FUKUDA, Kazuhiro KOSUMI, Jun TAKAHASHI, Keita TAKUNO, Ryo SHINAGAWA, Masashi SHIMAMOTO, Gran Martinez Alejandro, Satoshi YAMASAKI, Goro KUWAMURA
Abstract: The present invention relates to a catalyst for fixed bed aniline rectification residue recycling and preparation method thereof. Based on the total weight of the catalyst, the catalyst comprises the following components in percentage by weight: 5-40% of an active component, 2-30% of a first cocatalyst component, 10-30% of a second cocatalyst component and the balance of carrier, wherein the active component is NiO; the first cocatalyst component is one or more of Fe, Mo, Cr or Co oxide; and the second cocatalyst component is one or more of La, Zr, Y or Ce oxide. The catalyst is prepared through co-precipitation. The catalyst shows high activity and stability in the waste liquid treatment process, and can still maintain high rectification residue cracking rate after reaction of 200 hours.
Abstract: A method for isomerizing a bis(aminomethyl)cyclohexane, including an isomerization step of isomerizing the bis(aminomethyl)cyclohexane in the presence of an imine compound represented by the following general formula (1) and at least one compound selected from the group consisting of an alkali metal, an alkali metal-containing compound, an alkaline earth metal and an alkaline earth metal-containing compound: wherein R1 and R2 each independently represent a hydrogen atom or a monovalent group selected from the group consisting of a substituted or unsubstituted hydrocarbon group, a substituted or unsubstituted alkoxy group, and an acyl group (R1 and R2 may mutually bind to form a ring); R3 represents a hydrogen atom or an n-valent group selected from the group consisting of substituted or unsubstituted hydrocarbon groups; and n represents an integer of 1 to 10.
Abstract: Described herein are a series of compounds having the structure of Formula I: for use in the inhibition of MAO and uses thereof for the treatment of a barrier disease, obesity, solid epithelial cell tumor metastasis, diabetes, an auto-immune and inflammatory disease or a cardiometabolic disorder.
Type:
Application
Filed:
August 29, 2014
Publication date:
July 21, 2016
Inventors:
Edward Ewald Putnins, David Scott Grierson, Ronan F.B. Gealageas, Alice Andree Valentine Devineau, Edith Mary Dullaghan
Abstract: This invention generally relates to the generation of free fatty acids and/or derivatives thereof, e.g. fatty alkyl esters, and/or fatty amides, from feedstocks comprising phospholipids. In alternative embodiments, the invention provides methods and industrial processes for generating free fatty acids and/or fatty acid derivatives from a feedstock comprising phospholipids by combining the feedstock with one or more reactants to form a reaction mixture and reacting the mixture at a temperature and pressure sufficient to provide for the separation of the free fatty acids from their phosphatide structures.
Type:
Application
Filed:
August 29, 2014
Publication date:
July 21, 2016
Inventors:
William W. BERRY, William Rusty SUTTERLIN, Mark G. TEGEN, Cory BLANCHARD
Abstract: The present invention provides compounds of formula (I) and pharmaceutically acceptable salts thereof, wherein R1, X, m, R2, Y, R3, Z, n, R4, A and B are as defined in the specification, processes for their preparation, pharmaceutical compositions containing them and their use in therapy.
Type:
Application
Filed:
August 20, 2014
Publication date:
July 21, 2016
Inventors:
William BUFFHAM, Hannah CANNING, Richard DAVENPORT, William FARNABY, Stephen MACK, Alka PARMAR, Susanne WRIGHT
Abstract: The present invention is directed to a method of treating an inflammatory skin disease or disorder, such as dermatitis, psoriasis, acne, or rosacea. The method comprises administering to the subject 4-methylsulfonyl-2-butenenitrile, in an amount effective to reduce or eliminate the symptoms of the inflammatory skin disease or disorder. Topical administration and oral administration are preferred routes of administration.
Type:
Application
Filed:
March 30, 2016
Publication date:
July 21, 2016
Inventors:
Joseph P. ST. LAURENT, Gerald S. JONES, David M. BRESSE, Scott A. GOODRICH
Abstract: A method for preparing peroxide, including a step of treating, in a reaction medium, a component having at least one tertiary alcohol grouping with a compound having at least one tertiary hydroperoxide function in the presence of a catalyst, said method being characterised in that the catalyst includes a sulphonic acid and a inorganic acid, the molar ratio between the sulphonic acid and the aforementioned component including at least one tertiary alcohol grouping ranges from 0.05 to 0.8, and the molar ratio between the inorganic acid and the aforementioned component including at least one tertiary alcohol grouping ranges from 0.05 to 0.8. Also, to the peroxide resulting directly from said preparation method.
Abstract: Provided is a compound showing a bone formation promoting action (and/or bone resorption suppressive action). A compound of the formula (I) or a pharmacologically acceptable salt: [wherein each substituent is as defined in the DESCRIPTION], has low toxicity, shows good pharmacokinetics, has an action to promote bone formation, and is useful for the prophylaxis or To treatment of metabolic bone diseases (osteoporosis, fibrous osteitis (hyperparathyroidism), osteomalacia, Paget's disease that influences the systemic bone metabolism parameter etc.) associated with a decrease in the bone formation ability as compared to the bone resorption capacity.
Abstract: The present invention relates to Saroglitazar free acid of Formula (IA) or its pharmaceutically acceptable salts, pharmaceutically acceptable solvates, pharmaceutically acceptable esters, stereoisomers, tautomers, analogs and derivatives thereof. The present invention also provides an amorphous form of saroglitazar free acid and processes of preparation thereof. The present invention also provides pharmaceutical composition comprising an amorphous form saroglitazar magnesium.
Abstract: The present invention relates to compounds of formula wherein A is R is lower alkyl, —(CH2)z-C3-7-cycloalkyl or —(CH2)z—C4-6-heterocycloalkyl, which are optionally substituted by one to three hydroxy, lower alkyl, lower alkoxy or halogen, or is (endo)-7-oxabicyclo[2.2.
Type:
Application
Filed:
March 28, 2016
Publication date:
July 21, 2016
Applicant:
Hoffmann-La Roche Inc.
Inventors:
Theresa M. Ballard, Katrin Groebke Zbinden, Emmanuel Pinard, Thomas Ryckmans, Herve Schaffhauser
Abstract: The invention relates to the compounds of formula V or its pharmaceutical acceptable polymorphs, solvates, enantiomers, stereoisomers and hydrates thereof. The pharmaceutical compositions comprising an effective amount of compounds of formula V and methods for the treatment of inflammation and pain may be formulated for oral, buccal, rectal, topical, transdermal, transmucosal, lozenge, spray, intravenous, oral solution, buccal mucosal layer tablet, parenteral administration, syrup, or injection. Such compositions may be used to treatment of pain, oral mucosal inflammatory or oral infectious diseases.
Abstract: Novel compounds of the structural formula (I), and the pharmaceutically acceptable salts thereof, are agonists of G-protein coupled receptor 40 (GPR40) and may be useful in the treatment, prevention and suppression of diseases mediated by the G-protein-coupled receptor 40. The compounds of the present invention may be useful in the treatment of Type 2 diabetes mellitus, and of conditions that are often associated with this disease, including obesity and lipid disorders, such as mixed or diabetic dyslip idemia, hyperlipidemia, hypercholesterolemia, and hypertriglyceridemia.
Type:
Application
Filed:
September 30, 2014
Publication date:
July 21, 2016
Inventors:
Tesfaye Biftu, Purakkattle Biju, Steven L. Colletti, Mingxiang Cui, William K. Hagmann, Bin Hu, Hubert Josien, Nam Fung Kar, Anilkumar Nair, Ravi Nargund, Donald M. Sperbeck, Cheng Zhu
Abstract: The present invention relates to a pyrazolochalcone of formula A useful as potential antitumor agent against human cancer cell lines and a process for the preparation thereof. Formula A wherein, R1, R2, R3, R4, R5=H, Cl, F, CH3, OCH3, 3,4(OCH2O) X=H, Cl, CH3, OCH3, 3,4(OCH2O), NH2, NO2, OH, dotted line indicates optionally cyclic structure.
Abstract: It has been surprisingly been found that the compounds of general formula I are positive allosteric modulators (PAMs) of metabotropic glutamate receptor 4 (mGluR4), useful for the treatment of Parkinson's disease, anxiety, emesis, obsessive compulsive disorder, autism, neuroprotection, cancer, depression and diabetes type 2.
Type:
Application
Filed:
March 25, 2016
Publication date:
July 21, 2016
Applicant:
Hoffmann-La Roche Inc.
Inventors:
Barbara BIEMANS, Wolfgang GUBA, Georg JAESCHKE, Antonio RICCI, Daniel RUEHER, Eric VIEIRA
Abstract: The present disclosure describes new inhibitors or antagonists of Ras useful for the treatment of conditions resulting from Ras-induced or mediated cellular processes, including cellular proliferation, differentiation, apoptosis, senescence, and survival. These cellular processes may be associated with a non-malignant or malignant disease, disorder, or pathological condition. The present disclosure also describes a method for inhibiting such Ras-induced or mediated cellular processes. The method entails administering a Ras antagonist in an amount effective to inhibit such cellular processes.
Abstract: Described are methods for preparing salts of 5-nitrotetrazolate that include reacting aqueous solutions of 5-aminotetrazole, an acid, and sodium nitrite in a continuous flow system at an ambient temperature.
Type:
Application
Filed:
January 19, 2016
Publication date:
July 21, 2016
Applicant:
Pacific Scientific Energetic Materials Company
Inventors:
Jon G. Bragg, Jason B. Pattison, John W. Fronabarger, Michael D. Williams
Abstract: Disclosed are novel calcium modulators having formula I: or a pharmaceutically acceptable salt, and including deuterated forms thereof, wherein: Z1, Z2, Z3, Z4 Z5, R1, R1?, R2, R3, R3? R4, and R4?, are as defined throughout the specification; pharmaceutical compositions thereof; and methods of use thereof.
Abstract: A simple and elegant chemical process for the synthesis of oxygenated products, such as acids and aldehydes, or other derivative products, such as amines and nitriles, of cyclic bifunctional molecules made from renewable, bio-based sources such as HMF and/or its reduction product, 2,5-bis(hydroxymethyl)-tetrahydrofuran (bHMTHF) is described. In general, the process involves: a) generating a tetrahydrofuran-2,5-diyl-bis(methylene)-bis(sulfonate) from bHMTHFs using a sulfonate; b) displacing nucleophilically at least a sulfonate leaving group from the tetrahydrofuran-2,5-diyl-bis(methylene)-bis(sulfonate) to form a THF-dinitrile; and either c) oxidizing the THF-dinitrile with an acid having a pKa of ?0 to generate a di-acid, or d) reducing partially the THF-dinitrile to generate a di-aldehyde, or e) reducing fully the THF-dinitrile to generate a di-amine.
Abstract: The invention provides a method for preparing a 2,5-dialkyl furan. The method includes forming a reaction mixture containing a catalyst, a hydrogen source, and 2-haloalkylfuran starting material under conditions sufficient to form the 2,5-dialkyl furan. The 2-haloalkylfuran starting material can be derived from biomass, and the 2,5-dialkyl furan product can be used as a biofuel or as a chemical feedstock.
Abstract: Provided is a method for preparing 5-hydroxymethyl-2-furfural using an acid catalyst in the presence of an ethylene glycol-based solvent. The method for preparing the 5-hydroxymethyl-2-furfural involves using a linear or cyclic ethylene glycol-based compound as a solvent and producing the 5-hydroxymethyl-2-furfural from fructose, in the presence of the acid catalyst, thereby reducing the dependency on petroleum in response to greenhouse gas emission regulations. Also, a high yield of the 5-hydroxymethyl-2-furfural can be obtained from fructose, and the solvent and the catalyst can be efficiently separated, collected, and reused after a reaction has completed.
Type:
Application
Filed:
August 28, 2014
Publication date:
July 21, 2016
Inventors:
JIN KU CHO, SANG YONG KIM, BO RA KIM, SEUNG HAN SHIN
Abstract: The present disclosure provides methods to produce 5-(halomethyl)furfural, including 5-(chloromethyl)furfural, by acid-catalyzed conversion of C6 saccharides, including isomers thereof, polymers thereof, and certain derivatives thereof. The methods make use of acids with lower concentrations, and allows for conversion of sugars into 5-(halomethyl)furfural at higher temperatures and faster reaction or residence times.
Type:
Application
Filed:
September 19, 2014
Publication date:
July 21, 2016
Applicant:
MICROMIDAS, INC.
Inventors:
Alex B. WOOD, Makoto N. MASUNO, Ryan L. SMITH, John BISSEL, Dimitri A. HIRSCH-WEIL, Robert Joseph ARAIZA, Daniel R. HENTON, James H. PLONKA
Abstract: An acid composition comprising 2-formyl-furan-5-carboxylic acid and 2,5-furandicarboxylic acid is purified in a process which comprises; contacting the acid composition with an alcohol to obtain an esterified composition; and separating the ester of 2-formyl-furan-5-carboxylic acid from the esterified composition to obtain a purified esterified product; and contacting the purified esterified composition with water for saponification or hydrolysis, to obtain a product composition, comprising 2,5-furandicarboxylic acid and a reduced amount of 2-formyl-furan-5-carboxylic acid.
Type:
Application
Filed:
August 29, 2014
Publication date:
July 21, 2016
Applicant:
FURANIX TECHNOLOGIES B.V.
Inventors:
Jagdeep SINGH, Benjamin MCKAY, Bing WANG, Matheus Adrianus DAM, Gerardus Johannes Maria GRUTER, Ana Sofia Vagueiro DE SOUSA DIAS
Abstract: The present invention relates to a method for synthesizing an optionally substituted furoic acid by dehydrating a biomass and oxidizing the optionally substituted furan derived from the dehydration reaction. Water extraction has been incorporated as a step between the dehydration and the oxidation in order to purify the intermediate optionally substituted furan before having it oxidized. Prior to this water extraction, the organic solvent used for dehydration may be separated by evaporation. The provision of the water extraction allows impurities to be separated from the intermediate optionally substituted furan.
Abstract: The invention relates to compounds of Formula (I) and their use as selective dipeptidyl peptidase I inhibitors, as well as pharmaceutical compositions comprising said compounds, and methods of treatment involving said compounds.
Abstract: A compound is represented by Formula (I) or (II) described below. A medicine includes, as an active ingredient, a compound represented by Formula (I), (II), or (III) described below.
Abstract: The subject invention relates to improved tocopheryl quinone derivatives and tocopherol derivatives having improved pharmacokinetics in vivo that can, in some embodiments, be useful in the treatment of Lysosomal Storage Disorders, restoration of normal mitochondrial ATP production, modulation of intracellular calcium ion concentration and other treatments or therapies. The tocopheryl quinone derivatives and tocopherol derivatives have side chains that have terminally halogenated carbon atoms.
Type:
Application
Filed:
November 14, 2013
Publication date:
July 21, 2016
Inventors:
Juan Jose MARUGAN, Wei ZHENG, Jingbo XIAO, John MCKEW
Abstract: Described are novel photochromic naphthopyran compounds which exhibit a red coloring when in a red-colored state achieved upon exposure to ultraviolet light, whereby the red coloring has a lambda max in a range of between about 490 nanometers to about 510 nanometers or between about 490 nanometers to about 500 nanometers.
Abstract: Disclosed are crystalline ansolvate salts of 2-hydroxy-6-((2-(1-isopropyl-1H-pyrazol-5-yl)pyridin-3-yl)methoxy)benzaldehyde (or Compound 1), such as the hydrochloride Form I.
Abstract: The present disclosure relates to pyrimidine compounds of formula (I), their stereoisomers, tautomers, pharmaceutically acceptable salts, polymorphs, solvates, and hydrates thereof. The present disclosure also relates to process of preparation of these pyrimidine compounds, and to pharmaceutical compositions containing them. The compounds of the present disclosure are useful in the treatment, prevention or suppression of diseases and disorders mediated by epidermal growth factor receptor (EGFR) family kinases.
Abstract: To provide a novel 2,6-diaminopyrimidine derivative by the following formula (I): A 2,6-diaminopyrimidine derivative is represented by the formula (I): wherein R1 represents a substituted or unsubstituted lower alkyl group, or a substituted or unsubstituted alkoxy group, Ar represents a substituted or unsubstituted aryl group, or a substituted or unsubstituted heteroaryl group, Z1 and Z2 represent carbon atoms, or either 1 or 2 of the Z1 and Z2 represent nitrogen atoms, Q is selected from a structure (a) or (b) described below: R2 represents a substituted or unsubstituted lower alkyl group, or a substituted or unsubstituted cycloalkyl group, R3 represents a hydrogen atom or a halogen atom, Y represents a nitrogen atom or a carbon atom, and the bond drawn with a dotted line parallel to a solid line on structure (a) represents either double bond or single bond.
Type:
Application
Filed:
September 1, 2014
Publication date:
July 21, 2016
Inventors:
Wataru KAWAHATA, Tokiko ASAMI, Masaaki SAWA, Takayuki IRIE
Abstract: The present invention relates to the novel solid forms of Afatinib monomaleate and preparation methods thereof; the solid forms of Afatinib monomaleate of the present invention have many improved properties as compared to the known crystalline form of Afatinib salt; and the present invention also relates to pharmaceutical compositions containing the novel solid forms of Afatinib monomaleate as well as the uses thereof for treating terminal non-small cell lung cancer (NSCLS) and HER2 positive advanced breast cancer.
Abstract: The invention provides compounds represented by the formulae: (I) and (II) where the compounds are useful in treating, for example, viral and/or parasitic infections. Also provided are pharmaceutical compositions comprising the compounds and methods of treatment using the compounds.
Type:
Application
Filed:
September 16, 2015
Publication date:
July 21, 2016
Inventors:
Benhur Lee, Michael E. Jung, Jihye Lee, Frederic Vigant, Peter J. Bradley, Michael C. Wolf, Bettina E. Hajagos
Abstract: A synthesis method of anti-cancer drug UK-1 includes: mixing methyl 2-amino-3-hydroxybenzoate, aldehyde and molecular sieves to form a mixture and firstly refluxing the mixture to form a first reactant; hydrolyzing the first reactant in a basic solution to form a hydrolyzed solution and secondly refluxing the hydrolyzed solution to form a second reactant; and dehydrating the second reactant and the methyl 2-amino-3-hydroxybenzoate in an acidic solution to form a dehydrated solution and thirdly refluxing the dehydrated solution to form an anti-cancer drug UK-1 or at least one derivative thereof.
Abstract: A fluorinated 2-arylbenzo heterocyclic compound with high affinity to A? plaques and containing a chiral side chain substituent, has a general formula (I) as follows: wherein X is N; Y is S or O; Z is N or CH; R1 is a 5 or 6-substituent and is F is 19F or 18F; R2 is NHCH3 or N(CH3)2. The compound of the present invention has high affinity to A? plaques and can be used to make appropriate radioactive nuclide labeling probes for early diagnosis of AD.
Abstract: The invention relates to a new crystal form of dabrafenib and preparation method thereof. With respect to known crystal forms, the new crystal form has the advantage of being more stable at room temperature or in aqueous systems, and has low hygroscopicity, and thus is more suitable for a wet granulation process or being prepared into a suspension. The present invention also relates to a pharmaceutical composition and formulations comprising the new crystal form, and their use in the treatment of Raf family kinase-related diseases.