al Method for producing mono-aminofunctionalized dialkylphosphinic acids and esters and salts thereof by means of acrylnitriles and use thereof By www.freepatentsonline.com Published On :: Tue, 19 May 2015 08:00:00 EDT The invention relates to a method for producing mono-aminofunctionalized dialkylphosphinic acids and esters and salts thereof by means of acrylnitriles, characterized in that a) a phosphinic acid source (I) is reacted with olefins (IV) to yield an alkylphosphonic acid, salt or ester (II) thereof in the presence of a catalyst A, b) the thus obtained alkylphosphonic acid, salt or ester (II) thereof is reacted with an acrylnitrile of formula (V) to yield a mono-functionalized dialkylphosphinic acid derivative (VI) in the presence of a catalyst B, and c) the thus obtained mono-functionalized dialkylphosphinic acid derivative (VI) is reacted to yield a mono-aminofunctionalized dialkylphosphinic acid derivative (III) in the presence of a catalyst C or a reduction agent, wherein R1, R2, R3, R4, R5, R6, R7 are the same or different and stand independently of each other, among other things, for H, C1-C18 alkyl, C6-C18 aryl, C6-C18 aralkyl, C6-C18 alkylaryl and X stands for H, C1-C18 alkyl, C6-C18 aryl, C6-C18 aralkyl, C6-C18 alkylaryl, Mg, Ca, Al, Sb, Sn, Ge, Ti, Fe, Zr, Zn, Ce, Bi, Sr, Mn, Cu, Ni, Li, Na, K and/or a protonized nitrogen base, and Y stands for a mineral acid, a carboxylic acid, a Lewis acid or an organic acid, n=an integer or fractional number of 0 to 4 and the catalysts A and C are formed by transition metals, transition metal compounds and/or catalyst systems composed of a transition metal and/or a transition metal compound and at least one ligand, and catalyst B is formed by compounds forming peroxides, peroxo compounds, azo compounds, alkali metals, alkaline earth metals, alkali hydrides, alkaline earth hydrides and/or alkali alcoholates and alkaline earth alcoholates. Full Article
al Method of preparing an organohalosilane By www.freepatentsonline.com Published On :: Tue, 07 Jul 2015 08:00:00 EDT A method of preparing organohalosilanes comprising combining an organohalide having the formula RX (I), wherein R is a hydrocarbyl group having 1 to 10 carbon atoms and X is fluoro, chloro, bromo, or iodo, with a contact mass comprising at least 2% (w/w) of a palladium suicide of the formula PdxSiy (II), wherein x is an integer from 1 to 5 and y is 1 to 8, or a platinum suicide of formula PtzSi (III), wherein z is 1 or 2, in a reactor at a temperature from 250 to 700° C. to form an organohalosilane. Full Article
al Apparatus and methods to preserve catalyst activity in an epoxidation process By www.freepatentsonline.com Published On :: Tue, 05 May 2015 08:00:00 EDT Apparatus and methods are provided for forming and processing multiphasic systems. In one embodiment, the invention provides a process for the manufacture of an epoxide, including reacting an olefinically unsaturated compound with an oxidant in the presence of a buffer component and a water-soluble manganese complex disposed in an aqueous phase having a first pH level in a first multiphasic system, adjusting the pH of the aqueous phase to a second pH level less than the first pH level, isolating at least a portion of the aqueous phase from the first multiphasic system, adjusting the pH of the at least a portion of the aqueous phase to a third pH level greater than the second pH level, and introducing the at least a portion of the aqueous phase into a second multiphasic system. Full Article
al Photochromic materials that include indeno-fused naphthopyrans By www.freepatentsonline.com Published On :: Tue, 12 May 2015 08:00:00 EDT The present invention relates to photochromic materials that include one or more indeno-fused naphthopyrans that have particular groups at the 7, 11, and 13 positions thereof, and at the position alpha to the oxygen of the pyran ring thereof. With some embodiments, hydrogen or an alkoxy group is bonded to the 7 position, an optionally substituted phenyl is bonded to the 11 position, two alkyl groups are bonded to the 13 position, and two optionally substituted phenyl groups are bonded to the position alpha to the oxygen of the pyran ring of the indeno-fused naphthopyran compound. The 13 position of the indeno-fused naphthopyrans is free of ether groups in which an ether oxygen is bonded to the 13 position, and hydroxyl. The present invention also relates to photochromic articles and compositions that include such indeno-fused naphthopyrans. Full Article
al Substituted phenoxyethyl (isopropyl) acyloxyalkyl phosphonate comprising phosphorusheterocyclic ring and having herbicidal activity, and preparation therefor By www.freepatentsonline.com Published On :: Tue, 12 May 2015 08:00:00 EDT A substituted phenoxyethyl(isopropyl)acyloxyalkyl phosphonate having phosphorusheterocyclic ring and having herbicidal activity, with a general formula of I, wherein R represents 5,5-dimethyl-1,3,2-dioxaphosphorinan-2-one-2-yl, or 1-oxo-1-phospha-2,6,7-trioxabicyclo[2,2,2]octan-4-yl, or 1-sulfo-1-phospha-2,6,7-trioxabicyclo 2,6,7-trioxabicyclo[2,2,2]octan-4-yl; R1 represents H, C1-C4 alkyl, phenyl, furyl, pyridyl, or phenyl substituted with methyl, methoxyl, nitro or chloro; R2 represents H, methyl, and methyl only if R in the general formula I is 1-sulfo-1-phospha-2,6,7-trioxabicyclo[2,2,2]octan-4-yl as phosphorusheterocyclic ring; X and Y represent H, halogen, C1-C4 alkyl or trifluoromethyl, and X and Y are the same or different. The compounds according to the present invention may be used as active component of dicotyledonous broadleaf weed herbicides. Full Article
al Device and method for evaluating organic material for organic solar cell By www.freepatentsonline.com Published On :: Tue, 12 May 2015 08:00:00 EDT Provided are a novel 1,2-bis(dialkylphosphino)-4,5-(methylenedioxy)benzene derivative that forms a metal complex having particularly high asymmetry induction capacity and catalytic activity on β-dehydroamino acids, a method for manufacturing the same, a metal complex having this 1,2-bis(dialkylphosphino)-4,5-(methylenedioxy)benzene derivative as a ligand, and an asymmetric hydrogenation method using this metal complex. A 1,2-bis(dialkylphosphino)-4,5-(methylenedioxy)benzene derivative represented by general formula (1). (In the formula, R1 and R2 represent an alkyl group having 1-10 carbon atoms, and R1 and R2 have different numbers of carbon atoms.) Full Article
al ***WITHDRAWN PATENT AS PER THE LATEST USPTO WITHDRAWN LIST***Halichondrin B analogs By www.freepatentsonline.com Published On :: Tue, 12 May 2015 08:00:00 EDT The invention includes halichondrin B analogs having pharmaceutical activity; in some cases, crystalline forms thereof, and in some cases, halichondrin B analogs having a further utility as synthetic intermediate. Full Article
al Bicyclic compound and use thereof for medical purposes By www.freepatentsonline.com Published On :: Tue, 12 May 2015 08:00:00 EDT Provided is a compound which has strong and sustaining intraocular pressure lowering action and, further, has no fear of side effect on eyes. Since a compound represented by the formula (I): wherein definition of each group is as described in the specification, or a salt thereof, a solvate thereof, or a prodrug thereof has strong and sustaining intraocular pressure lowering action and, further, has no side effect on eyes such as ocular stimulating property (hyperemia, corneal clouding etc.), aqueous humor protein rise etc., it has high safety, and can be an excellent agent for preventing and/or treating glaucoma etc. Full Article
al Process for preparation of acetals By www.freepatentsonline.com Published On :: Tue, 12 May 2015 08:00:00 EDT A process for the preparation of 1,3:2,4-bis(4-methylbenzylidene)sorbitol (MDBS) and 1,3:2,4-bis(3,4-dimethylbenzylidene)sorbitol (DMDBS) via a dehydrocondensation reaction is disclosed. The reaction is carried out between an aldehyde and an alditol in a mole ratio of 2:1 wherein ionic fluid is used as the acidic catalyst and/or reaction medium. The ionic fluid used in accordance with the present invention is quaternary ammonium salt based ionic liquid. Full Article
al Method for preparation of anhydrosugar alcohols By www.freepatentsonline.com Published On :: Tue, 12 May 2015 08:00:00 EDT A method is provided for the preparation of anhydrosugar alcohols. The method involves dehydration of a hexitol with a mixed acid of a first acid and second acid, in which the first acid is sulfuric acid and the second acid is at least one sulfur-containing acid or sulfur-containing acid salt selected from the group consisting of p-toluenesulfonic acid, methanesulfonic acid, ethanesulfonic acid, benzenesulfonic acid, naphthalenesulfonic acid and aluminum sulfate. Also provided are methods for purification of the resulting product. Full Article
al Esterification of furan-2,5-dicarboxylic acid to a dialkyl-furan-2,5-dicarboxylate vapor with rectification By www.freepatentsonline.com Published On :: Tue, 12 May 2015 08:00:00 EDT A process for the manufacture of dialkyl furan-2,5-dicarboxylate (DAFD) vapor composition by feeding furan-2,5-dicarboxylic acid (“FDCA”) to an esterification reactor and in the presence of an alcohol compound such as methanol, conducting an esterification reaction to form an esterification vapor containing DAFD, unreacted alcohol compound, 5-(alkoxycarbonyl)furan-2-carboxylic acid (ACFC), and water, and continuously passing the esterification vapor through an ACFC condensing zone, that can be integral with the esterification reactor, in which at least a portion of the ACFC in the esterification vapor is converted to a liquid phase condensate, and continuously discharging the esterification vapor from the ACFC condensing zone as a DAFD vapor. There is also a DAFD vapor composition containing DAFD, water, unreacted alcohol, and by-products. Full Article
al Pharmaceutical composition comprising rotigotine salts (acid or Na), especially for iontophoresis By www.freepatentsonline.com Published On :: Tue, 19 May 2015 08:00:00 EDT The present invention relates to new salts of 6-(propyl-(2-thiophen-2-ylethyl)amino)tetralin-1-ol(rotigotine), their use as a medicament, for example for the treatment of CNS disorders like Parkinson Disease, RLS, fibromyalgia and/or depression, in particular through electromotive administration. The present invention relates to pharmaceutical formulations suitable for iontophoresis that provide enhanced iontophoretic delivery of rotigotine to at least one target tissue. The formulations are further characterized by good to excellent solubility of the salts in aqueous solutions. Full Article
al Catalyst for organic reaction and method of use thereof By www.freepatentsonline.com Published On :: Tue, 19 May 2015 08:00:00 EDT A catalyst for an organic reaction and a method of using a catalyst in an organic reaction are provided. The catalyst for an addition or condensation reaction includes a graphene oxide including an oxygen functional group, and the catalyst is configured to promote the addition or condensation reaction by bonding the oxygen functional group with an alkali metal ion or alkali earth metal ion during the addition or condensation reaction. Full Article
al Recovery of lactic acid values from a meso-lactide stream By www.freepatentsonline.com Published On :: Tue, 19 May 2015 08:00:00 EDT Lactic acid equivalents are recovered from a starting lactide stream by catalytically racemizing a portion of the lactide in the stream at a temperature of 180° C. or below. This increases the proportion of two species of lactide (i.e., at least two of S,S-, R,R- or meso-lactide) at the expense of the third species. The racemized mixture so obtained can be separated to recover some or all of one or more of the lactide species from the remaining lactide species, by a process such as melt crystallization or distillation. Impurities in the starting lactide stream usually are retained mostly in the remaining meso-lactide, so a highly purified S,S- and/or R,R-lactide stream can be produced in this manner. Such a purified S,S- and R,R-lactide stream is suitable for polymerization to form a polylactide. Full Article
al Total synthesis of artemisinin By www.freepatentsonline.com Published On :: Tue, 19 May 2015 08:00:00 EDT The present invention provides a method for manufacturing artemisinin and its congeners from cyclohexenone as a starting material. Full Article
al Liquid crystal composition, liquid crystal element, and liquid crystal display device By www.freepatentsonline.com Published On :: Tue, 26 May 2015 08:00:00 EDT A liquid crystal composition including a dioxolane compound represented by the general formula (G1) as a chiral agent is provided. In the general formula (G1), R1 and R2 individually represent any of hydrogen, an alkyl group having 1 to 6 carbon atoms, an alkoxy group having 1 to 20 carbon atoms, an aryl group having 6 to 12 carbon atoms, and an alkyl group having 1 to 20 carbon atoms and having a phenyl group as a substituent; R1 and R2 may be bonded to each other to form a ring; R3 and R4 individually represent any of hydrogen, an alkyl group having 1 to 6 carbon atoms, and a cycloalkyl group; and R5 to R40 individually represent any of hydrogen, an alkyl group having 1 to 4 carbon atoms, an alkoxy group having 1 to 4 carbon atoms, and an aryl group having 6 to 12 carbon atoms. Full Article
al Crystalline molecular comlpexes of tadalafil By www.freepatentsonline.com Published On :: Tue, 26 May 2015 08:00:00 EDT Crystalline molecular complexes of tadalafil are disclosed. The crystalline molecular complexes include those of tadalafil and oxalic acid, tadalafil and 4-hydroxybenzoic acid, tadalafil and 3-phenylpropanoic acid, tadalafil and malonic acid, tadalafil and methylparaben, and tadalafil and propylparaben. Pharmaceutical compositions containing the crystalline molecular complexes are also disclosed. Full Article
al Process for the preparation of quaternary N-alkyl morphinan alkaloid salts By www.freepatentsonline.com Published On :: Tue, 26 May 2015 08:00:00 EDT An improved process for the N-alkylation of tertiary morphinan alkaloid bases to form the corresponding quaternary morphinan alkaloid derivatives. Full Article
al Process for producing 1,4-butanediol by hydrogenating dialkyl maleate in mixed liquid/vapor phase By www.freepatentsonline.com Published On :: Tue, 26 May 2015 08:00:00 EDT A process for the production of 1,4-butanediol and tetrahydrofuran by catalytic hydrogenation of dialkyl maleates includes the following steps: a) hydrogenating a stream of dialkyl maleate in a first stage of reaction over suitable catalysts to produce dialkyl succinate;b) further hydrogenating the dialkyl succinate in a second stage of reaction, by using a different suitable catalyst, for producing mainly 1,4-butanediol, together with gamma-butyrolactone and tetrahydrofuran as co-products. In both stages of reaction the conditions, as hydrogen/organic feed ratio, pressure and temperature, are such to maintain the reactors in mixed liquid/vapor phase. Full Article
al Halichondrin B analogs By www.freepatentsonline.com Published On :: Tue, 08 Dec 2015 08:00:00 EST The invention includes halichondrin B analogs having pharmaceutical activity; in some cases, crystalline forms thereof, and in some cases, halichondrin B analogs having a further utility as synthetic intermediate. Full Article
al Topical tetracycline compositions By www.freepatentsonline.com Published On :: Tue, 21 Oct 2014 08:00:00 EDT A topical therapeutic hydrophobic breakable composition includes a carrier comprising (a) about 60% to about 99% by weight of at least one hydrophobic oil; (b) at least one viscosity-modifying agents selected from the group consisting of a fatty alcohol, a fatty acid and a wax; and (c) a tetracycline antibiotic, characterized in that at least part of the tetracycline antibiotic is suspended in the composition; the viscosity of the composition is at least about 30% higher than the viscosity of the carrier without the tetracycline antibiotic; and is higher than the viscosity of the hydrophobic oil and the tetracycline antibiotic without the viscosity modifying agents. The tetracycline is chemically stable in the composition for at least six months; wherein more than about 90% of the tetracycline has not broken down. The composition is packaged as a breakable foam that breaks easily upon application of shear force. Full Article
al Topical tetracycline compositions By www.freepatentsonline.com Published On :: Tue, 28 Oct 2014 08:00:00 EDT A topical therapeutic hydrophobic breakable composition includes a carrier comprising (a) about 60% to about 99% by weight of at least one hydrophobic oil; (b) at least one viscosity-modifying agents selected from the group consisting of a fatty alcohol, a fatty acid and a wax; and (c) a tetracycline antibiotic, characterized in that at least part of the tetracycline antibiotic is suspended in the composition; the viscosity of the composition is at least about 30% higher than the viscosity of the carrier without the tetracycline antibiotic; and is higher than the viscosity of the hydrophobic oil and the tetracycline antibiotic without the viscosity modifying agents; and the amount of viscosity modifying agents can optionally be reduced by at least an amount by weight that would have increased the viscosity of the carrier without the tetracycline antibiotic by at least 30%; wherein the tetracycline is chemically stable in the composition for at least six months; wherein more than about 90% of the tetracycline has not broken down; wherein when packaged in an aerosol container to which is added a liquefied or compressed gas propellant the composition affords upon release from the container a breakable foam of at least good quality that breaks easily upon application of shear force. Full Article
al Crystallization of (20R) and (20S) analogs of 2-methylene-19-nor-24-dimethyl-1α,25-dihydroxyvitamin D3 By www.freepatentsonline.com Published On :: Tue, 11 Nov 2014 08:00:00 EST Disclosed are methods of purifying (20R) and (20S) analogs of 2-methylene-19-nor-22-dimethyl-1α,25-dihydroxyvitamin D3 to obtain the (20R) and (20S) analogs in crystalline form. The method includes the steps of preparing a solvent of either diethyl ether or a mixture of 2-propanol and hexane, dissolving a product containing the (20R) and (20S) analog to be purified in the solvent, cooling the solvent and dissolved product below ambient temperature for a sufficient amount of time to form a precipitate of crystals, and recovering the crystals. Full Article
al Oral dosage form of 25-hydroxyvitamin D By www.freepatentsonline.com Published On :: Tue, 09 Dec 2014 08:00:00 EST Methods and compositions for treating 25-hydroxyvitamin D insufficiency and deficiency in a patient are described herein. The method includes orally administering to the patient a delayed, sustained release formulation including a first ingredient selected from the group consisting of 25-hydroxyvitamin D2, 25-hydroxyvitamin D3, or a combination of 25-hydroxyvitamin D2 and 25-hydroxyvitamin D3, or it includes gradually administering to the patient a sterile intravenous formulation including a first ingredient selected from the group consisting of 25-hydroxyvitamin D2, 25-hydroxyvitamin D3, or a combination of 25-hydroxyvitamin D2 and 25-hydroxyvitamin D3. Full Article
al Low-calcemic 16,23-diene 25-oxime analogs of 1α,25-dihydroxy vitamin D3 By www.freepatentsonline.com Published On :: Tue, 09 Dec 2014 08:00:00 EST The present invention provides novel 16,23-diene 25-oxime ether analogs of 1,25-dihydroxy vitamin D3, compositions comprising these compounds and methods of using these compounds as inhibitors of CYP24. In particular, the novel compound of the invention are useful for treating diseases which benefit from a modulation of the levels of 1,25-dihydroxy vitamin D3, for example, cell-proliferative disorders. Full Article
al C-3 cycloalkenyl triterpenoids with HIV maturation inhibitory activity By www.freepatentsonline.com Published On :: Tue, 09 Dec 2014 08:00:00 EST Compounds having drug and bio-affecting properties, their pharmaceutical compositions and methods of use are set forth. In particular, C-3 cycloalkenyl triterpenoids that possess unique antiviral activity are provided as HIV maturation inhibitors, as represented by compounds of Formulas I, II, III and IV: wherein X can be a C4-8 cycloalkyl, C4-8 cycloalkenyl, C4-9 spirocycloalkyl, C4-9 spirocycloalkenyl, C4-8 oxacycloalkyl, C4-8 dioxacycloalkyl, C6-8 oxacycloalkenyl, C6-8 dioxacycloalkenyl, C6-9 oxaspirocycloalkyl, or C6-9 oxaspirocycloalkenyl ring. These compounds are useful for the treatment of HIV and AIDS. Full Article
al Pyrrolysine analogs By www.freepatentsonline.com Published On :: Tue, 30 Dec 2014 08:00:00 EST Several different pyrrolysine analogs are disclosed in this application. Those analogs have distinct chemical and biophysical properties. Some analogs are useful in chemical ligation applications. Methods of making and using are also disclosed. Full Article
al Preparation of a crystalline antibiotic substance By www.freepatentsonline.com Published On :: Tue, 13 Jan 2015 08:00:00 EST The present invention relates to processes for the crystallisation and for the preparation and isolation of a novel crystalline form of fusidic acid, to the use of said processes in the manufacture of pharmaceutical formulation or medicament, and to the use of said crystalline fusidic acid form for the treatment of bacterial infections. Full Article
al Crystallization of (20R)-2-methylene-19-nor-24-difluoro-1α,25-dihydroxyvitamin D3 By www.freepatentsonline.com Published On :: Tue, 27 Jan 2015 08:00:00 EST Disclosed are methods of purifying the compound (20R)-2-methylene-19-nor-24-difluoro-1α,25-dihydroxyvitamin D3 to obtain the compound in crystalline form. The methods typically include the steps of dissolving a product containing the compound in a solvent comprising hexane and 2-propanol, cooling the solvent and dissolved product below ambient temperature for a sufficient amount of time to form a precipitate of crystals, and recovering the crystals. Full Article
al Methods for synthesizing and purifying aminoalkyl tetracycline compounds By www.freepatentsonline.com Published On :: Tue, 03 Feb 2015 08:00:00 EST Methods for the synthesis and purification of 9-amino alkyl tetracycline compounds are described. Full Article
al Construction of a multivalent scFv through alkyne-azide 1,3-dipolar cycloaddition By www.freepatentsonline.com Published On :: Tue, 03 Feb 2015 08:00:00 EST The present invention provides for a practical, universal and efficient method to ligate two large macromolecules (e.g., proteins) using the alkyne-azide 1,3-dipolar cycloaddition reaction to produce a conjugated macromolecule, such as a multivalent scFv. The present invention also provides for conjugate macromolecules comprising a plurality of macromolecule components cross-linked through at least one linking group comprising at least one 1,2,3-triazole moiety, wherein at least 50 percent of the macromolecule components in the conjugate macromolecule has only one site available for cross-linking. Full Article
al N-cyclopropyl-(20R)-2-methylene-19,26,27-trinor-25-aza-vitamin D analogs and their uses By www.freepatentsonline.com Published On :: Tue, 24 Mar 2015 08:00:00 EDT This invention discloses N-cyclopropyl-(20R)-2-methylene-19,26,27-trinor-25-aza-vitamin D analogs, and specifically N-cyclopropyl-(20R)-2-methylene-19,26,27-trinor-25-aza-1α-hydroxyvitamin D3 and pharmaceutical uses therefor. This compound exhibits relatively high binding activity and pronounced activity in arresting the proliferation of undifferentiated cells and inducing their differentiation to the monocyte thus evidencing use as an anti-cancer agent especially for the treatment or prevention of leukemia, colon cancer, breast cancer, skin cancer or prostate cancer. Full Article
al Topical tetracycline compositions By www.freepatentsonline.com Published On :: Tue, 31 Mar 2015 08:00:00 EDT A topical therapeutic hydrophobic breakable composition includes a carrier comprising (a) about 60% to about 99% by weight of at least one hydrophobic oil; (b) at least one viscosity-modifying agents selected from the group consisting of a fatty alcohol, a fatty acid and a wax; and (c) a tetracycline antibiotic, characterized in that at least part of the tetracycline antibiotic is suspended in the composition; the viscosity of the composition is at least about 30% higher than the viscosity of the carrier without the tetracycline antibiotic; and is higher than the viscosity of the hydrophobic oil and the tetracycline antibiotic without the viscosity modifying agents. The tetracycline is chemically stable in the composition for at least six months; wherein more than about 90% of the tetracycline has not broken down. The composition is packaged as a breakable foam that breaks easily upon application of shear force. Full Article
al 3-desoxy-2-methylene-19-nor-vitamin D analogs and their uses By www.freepatentsonline.com Published On :: Tue, 31 Mar 2015 08:00:00 EDT This invention discloses 3-desoxy-2-methylene-19-nor-vitamin D analogs, and specifically (20S)-3-desoxy-2-methylene-1α,25-dihydroxy-19-nor-vitamin D3 and (20R)-3-desoxy-2-methylene-1α,25-dihydroxy-19-nor-vitamin D3 as well as pharmaceutical uses therefor. These compounds exhibit relatively high binding activity and pronounced activity in arresting the proliferation of undifferentiated cells and inducing their differentiation to monocytes thus evidencing use as anti-cancer agents especially for the treatment or prevention of osteosarcoma, leukemia, colon cancer, breast cancer, skin cancer or prostate cancer. These compounds also exhibit relatively high calcemic activity evidencing use in the treatment of bone diseases. Full Article
al Method for producing 30-halogenated betulinic acid By www.freepatentsonline.com Published On :: Tue, 21 Apr 2015 08:00:00 EDT The invention discloses a method for producing 30-halogenated betulinic acid. Betulin is used as a raw material and selectively oxidized and halogenated to generate 30-betulinic acid, and the selected oxidation and halogenation agent has high selectivity and does not affect C-3 hydroxyl or carbon-carbon double bonds. Oxidation and halogenation are completed in one step, so the process route is short, the treatment method is simple, and the product is purified easily. Full Article
al Vitamin D receptor modulators with partial agonist activity By www.freepatentsonline.com Published On :: Tue, 28 Apr 2015 08:00:00 EDT The present invention provides a compound which functions as a selective vitamin D receptor modulator and has action-selectivity or tissue-selectivity such that it does not induce hypercalcemia but causes other effects. There is provided a compound represented by formula (I), a solvate thereof or a prodrug thereof. wherein m and n each independently represent 1 or 0;R represents a hydrogen atom or an alkyl group;Y represents an ethane-1,1-diyl group or an ethyne-1,2-diyl group; andZ1 represents a hydrogen atom and Z2 represents a hydroxyalkoxy group, orZ1 and Z2 jointly form a methylene group. Full Article
al Pharmaceutical composition By www.freepatentsonline.com Published On :: Tue, 12 May 2015 08:00:00 EDT The invention relates to a solid pharmaceutical composition comprising solid amorphous fulvestrant, said composition being formulated in combination with a solubilizing composition. The invention also relates to a method for preparing said composition and a kit including the composition. Full Article
al Crystallization of (20R) 19-nor-24-difluoro-1α,25-dihydroxyvitamin D3 By www.freepatentsonline.com Published On :: Tue, 26 May 2015 08:00:00 EDT Disclosed are methods of purifying the compound (20R)-19-nor-24-difluoro-1α,25-dihydroxyvitamin D3 to obtain the compound in crystalline form. The methods typically include the steps of dissolving a product containing the compound in a solvent comprising hexane and 2-propanol, cooling the solvent and dissolved product below ambient temperature for a sufficient amount of time to form a precipitate of crystals, and recovering the crystals. Full Article
al Agrochemical formulations comprising 1-vinyl-2-pyrrolidinone co-polymers By www.freepatentsonline.com Published On :: Tue, 14 Apr 2015 08:00:00 EDT The present invention comprises formulations comprising at least one pesticide and at least one co-polymer comprising a) 1-vinyl-2-pyrrolidinone as comonomer a); and b) 60-99 wt % at least one comonomer b) chosen from the group of laurylacrylate and vinyl ester of neodecanoic acid in polymerized form, methods of combating harmful insects and/or phytopathogenic fungi, a method of controlling undesired vegetation and methods of improving the health of plants based on the afore-mentioned formulations. Full Article
al Synergistic fungicidal active substance combinations By www.freepatentsonline.com Published On :: Tue, 14 Apr 2015 08:00:00 EDT Novel active compound combinations comprising a carboxamide of the general formula (I) (group 1) in which A, R1, R2 and R3 are as defined in the description,and the active compound groups (2) to (23) listed in the description have very good fungicidal properties. Full Article
al Glyphosate formulations based on compositions derived from natural oil metathesis By www.freepatentsonline.com Published On :: Tue, 14 Apr 2015 08:00:00 EDT Aqueous glyphosate formulations comprising a surfactant derived from metathesized natural oil feedstocks are disclosed. The formulations comprise a glyphosate salt, water, and a surfactant derived from a metathesis-derived C10-C17 monounsaturated acid, octadecene-1,18-dioic acid, or their ester derivatives. The surfactant is selected from C10 or C12 amine oxides, C10 or C12 quats, C10, C12, or C16 amidoamines, C10 or C12 amidoamine oxides, C10 imidazoline quats, C10 or C12 amidoamine quats, C10, C12, or C16 betaines, C16 amidoamine betaines, C18 diamidoamines, C18 diamidoamine oxides, C18 diamidoamine diquats, C18 diamidoamine oxide quats, C18 diamidoamine oxide betaines, Cis diamidoamine monobetaines, C18 diamidoamine monobetaine quats, C18 ester amidoamine quats, and amidoamines and their oxidized or quaternized derivatives made from self- or cross-metathesized palm or soybean oil. The surfactants noted above impart substantial stability to highly concentrated glyphosate formulations at, above, and below room temperature and perform as well or better than commercial alternatives. Full Article
al Agrochemical formulations of microcapsules for compounds containing carboxamide groups By www.freepatentsonline.com Published On :: Tue, 14 Apr 2015 08:00:00 EDT The present invention is directed towards microcapsules, uses and methods of microencapsulation with improved properties regarding agglomeration, bleeding and control of the reaction. The invention is especially suitable for chemical compounds with at least one carboxamide group, preferably for microencapsulation of those compounds wherein the carbonyl group is attached to a nitrogen atom or nitrogenated heterocycle and wherein the microencapsulation reaction may be too vigorous. The microcapsules are characterized by a mixed glycoluril-polyurea polymer wall, wherein the polyurea groups come from a urea-formaldehyde resin and not from isocyanate monomers or prepolymers. The process of making such microcapsules a dispersant in the oil phase of the type of block copolymer of vinylpyrrolidone/vinylalkene and/or vinylpyrrolidone/vinyl acetate and the microencapsulation reaction may be carried out without the presence of any polyamine/polyol acting as a catalyst. Full Article
al Compatibility agents for herbicidal formulations comprising 2,4-(Dichlorophenoxy) acetic acid salts By www.freepatentsonline.com Published On :: Tue, 21 Apr 2015 08:00:00 EDT The present invention generally relates to a method for minimizing the formation of insoluble salts of phenoxy herbicides. The method comprises (1) mixing a compatibility agent, amine salts of phenoxy acid herbicides, and a chemical containing non-amine cations in a aqueous system to form a stable and non-nozzle plugging solution; and (2) application of said stable and non-nozzle plugging solution onto target plants. Full Article
al Insecticidal N-substituted (6-haloalkylpyridin-3-yl)-alkyl sulfoximines By www.freepatentsonline.com Published On :: Tue, 21 Apr 2015 08:00:00 EDT N-Substituted (6-haloalkylpyridin-3-yl)alkyl sulfoximines are effective at controlling insects. Full Article
al Pesticidal composition comprising sulphur, an insecticide and an agrochemical excipient By www.freepatentsonline.com Published On :: Tue, 28 Apr 2015 08:00:00 EDT The present invention relates to an pesticidal composition comprising an effective amount of a sulphur; an effective amount of at least one insecticide selected from the group consisting of cartap fipronil, pirimicarb, buprofezine, thiachloprid, acetamiprid, clothianidin, diafenthiuron, novaluron, flubendiamide, spirotetramat, thiamethoxam, imidacloprid or salts thereof, and at least one agrochemically acceptable excipient. Full Article
al Pesticidal compositions By www.freepatentsonline.com Published On :: Tue, 28 Apr 2015 08:00:00 EDT A pesticidal composition comprising (a) a pesticidal effective amount of at least one compound of formula I in which Q is i or ii or iii or an agrochemically acceptable salt or an N-oxide thereof, and (b) a plant growth regulator, where the ratio of compound of formula I to plant growth regulator is from 20:1 to 1:25. Full Article
al Pesticidal compositions and processes related thereto By www.freepatentsonline.com Published On :: Tue, 28 Apr 2015 08:00:00 EDT This document discloses molecules having the following formulas (“Formula One” & “Formula Two” and “Formula Three”) The Ar1, Het, Ar2, R1, R2, R3, R4, and R5 are further described herein. Full Article
al Methods for promoting plant health By www.freepatentsonline.com Published On :: Tue, 05 May 2015 08:00:00 EDT A method for promoting the health of a plant comprises administering malic acid to the plant or the soil in an amount effective to recruit plant growth promoting rhizobacteria (PGPR) to the plant. Administration of malic acid promotes biofilm formation of PGPR on the plant's roots, thereby restricting entry of a foliar pathogen through stomatal pores present in the leaves. Another method for promoting the health of a plant comprises administering acetoin to the plant or the soil in an amount effective to increase pathogen resistance in aerial parts of the plant. Full Article
al Compositions and methods for blocking ethylene response in plants using 3-cyclopropyl-1-enyl-propanoic acid salt By www.freepatentsonline.com Published On :: Tue, 05 May 2015 08:00:00 EDT The present invention discloses a method of inhibiting an ethylene response in a plant, comprising step of applying to at least one portion of the plant an effective ethylene response-inhibiting amount of a H1-cyclopropene-1-propanoic acid salt (CPAS). A method of prolonging the life of a cut flower, comprising applying to the cut flower an effective life-prolonging amount of CPAS and a method for the production a CPAS, comprising steps of (i) preparing 4-bromo-4-pentenoic acid or derivatives thereof; (ii) producing 1-cyclopropene-1-propanoic acid; and (iii), converting this acid into its water soluble salt, especially its sodium salt are presented. Additionally, a new family of water soluble CPAS inhibitors for ethylene response in a plant is disclosed. Full Article
al Modification of trehalose-6-phosphate levels in plants By www.freepatentsonline.com Published On :: Tue, 05 May 2015 08:00:00 EDT Compounds which are trehalose-6-phosphate or trehalose-6-phosphonate precursors of formula (I) or agriculturally acceptable salts thereof are provided: (I) The compounds are useful in increasing starch production in plants. Full Article