Ortho ester-substituted clorotriazines as capping agents for polyphenylene ethers

Lactide Production from Thermal Depolymerization of PLA with applications to Production of PLA or other bioproducts

Methods and systems are disclosed for producing lactide, which can be used for PLA production or other valuable bioproducts. PLA is heated to undergo thermal depolymerization to recover lactide. The lactide can be used for PLA production or other valuable bioproducts.

NEURO-PROTECTIVE EFFECTS OF ADELOSTEMMA GRACILLIMUM AND ITS ISOLATED COMPOUNDS

Isolated compounds from refined fractions and compositions containing the compounds are provided by the present invention. refined fractions and the extraction process thereof are also provided by the present invention. The uses of the compounds and the refined fractions for inhibiting the activities of NMDA receptor or amyloid-beta peptide, for improving memory, and for treating neurodegenerative diseases, neuropathological conditions or epilepsy are further provided by the present invention. 10. The compound of claim 9 , wherein Ris H.11. The compound of claim 9 , wherein{'sup': '1', 'Ris H;'}{'sup': 2', '3, 'each of Rand Rare Me; and'}subscript n is 10.1514. A pharmaceutical composition for treating a neurodegenerative disease or neuropathological condition in a subject claims 1 , the composition comprising a compound of any one of - and a pharmaceutically acceptable carrier or excipient.16Adelostemma gracillimum. A method of preparing a refined fraction claims 1 , the method comprising:{'i': 'Adelostemma gracillimum', 'contacting herb with an alcohol selected from the group consisting of methanol and ethanol, to form an alcohol extract;'}contacting the alcohol extract with an organic solvent to form an organic solvent fraction; and{'i': 'Adelostemma gracillimum', 'contacting the organic solvent fraction with a petroleum ether to form the refined fraction.'}17. The method of claim 16 , further comprising:{'i': 'Adelostemma gracillimum', 'eluting a first fraction of the refined fraction from a resin column with a solution of about 30% ethanol in water;'}eluting a second fraction from the resin column with a solution of about 60% ethanol in water; andeluting a third fraction from the resin column with a solution of about 96% ethanol in water.18Adelostemma gracillimum. An refined fraction prepared by the method of .19Adelostemma gracillimum. An refined fraction prepared by the method of .20Adelostemma gracillimum. A method of improving memory in a subject claim 17 , ...

COMPOSITION FOR THE TREATMENT OF ARTHRITIS CONTAINING A DIBENZO-P-DIOXIN DERIVATIVE AS THE ACTIVE INGREDIENT

Disclosed is a composition for treating arthritis containing a dibenzo-p-dioxin derivative as an active ingredient. This dibenzo-p-dioxin derivative is very effective in inhibiting NF-kB and AP-1 activity, alleviates the symptoms of degenerative arthritis and rheumatoid arthritis without irritating the skin or causing side effects, and can continue to exhibit improvement effects for a considerable period of time after discontinuation of treatment. Additionally, when the dibenzo-p-dioxin derivative is contained in liposomes, the composition of the invention exhibits much greater effects on treating arthritis by absorption through skin, and thus is useful for the treatment of degenerative arthritis and rheumatoid arthritis. 2. The method according to claim 1 , wherein each R in Formulas 1 to 10 is independently hydrogen claim 1 , methyl claim 1 , acetyl or oleoyl.3. The method according to claim 1 , wherein each R in Formulas 1 to 10 is independently hydrogen.4. The method according to claim 1 , wherein the total weight of the two or more selected compounds ranges from 0.2 to 2.0 wt % of the total weight of the composition.5. The method according to claim 1 , wherein the total weight of the two or more selected compounds ranges from 0.5 to 1.5 wt % of the total weight of the composition.6. The method according to claim 1 , wherein the composition is provided in a form selected from the group consisting of an ointment claim 1 , a lotion claim 1 , a cream claim 1 , a gel claim 1 , a skin emulsion claim 1 , a skin suspension claim 1 , a patch claim 1 , and a spray.7. The method according to claim 1 , wherein the composition further comprises a liposome carrying the composition.8. The method according to claim 7 , wherein the liposome comprises multi-lamella vesicles.9. The method according to claim 7 , wherein the liposome comprises unilamella vesicles.10. The method according to claim 1 , wherein the composition is applied in a dose of 1-1000 μg/cmper day.11. The method ...

Compounds, Compositions, And Methods For Reducing Or Eliminating Bitter Taste

The present invention provides edible compositions comprising a compound of the present invention, food products comprising such edible compositions and methods of preparing such food products. The present invention also provides methods of reducing the amount of NaCl in a food product, methods of reducing the sodium intake in a diet, and methods of reducing bitter taste in a food product. 710.-. (canceled)1355.-. (canceled)5661112. The composition of any one of - claims 1 , or claims 1 , further comprising a bitter tastant.576111256. The composition of any one of - claims 1 , claims 1 , or claims 1 , wherein the composition further comprises one or more components selected from the group consisting of: NaCl claims 1 , sodium lactate and sugar.58611125657. The composition of any one of - claims 1 , claims 1 , claims 1 , or claims 1 , wherein the composition is found in a food product or a consumer product.5961112. The composition of any one of - claims 1 , or claims 1 , wherein the composition further comprises a pharmaceutically active ingredient claims 1 , and optionally claims 1 , a bitter tastant.60. The composition of claim 59 , wherein the pharmaceutically active ingredient is bitter.61. The composition of or claim 59 , wherein the pharmaceutically active ingredient or bitter tastant is a potassium salt.62. The composition of any one of claim 59 , or claim 59 , wherein the bitter tastant is a potassium salt claim 59 , and wherein the potassium salt is potassium chloride or potassium lactate.6361112. A method of use of the composition of any one of - claims 1 , or claims 1 , wherein the method comprises:(a) providing a comestibly acceptable carrier; and{'claim-ref': {'@idref': 'CLM-00001', 'claims 1'}, 'b': '8', '(b) adding to the comestibly acceptable carrier, a composition as described in any of - or combinations thereof.'}64. The method of claim 63 , wherein the method further comprises adding a bitter tastant to the comestibly acceptable carrier.65. The ...

Process for the manufacture of a cyclic diester of an alpha-hydroxyacid

Process for the manufacture of a cyclic diester of an alpha-hydroxyacid comprising heating the alpha-hydroxyacid at a temperature from 100 to 250° C. in the presence of at least one polyol and of at least one catalyst selected from the group consisting carboxylates and alkoxides of Ti, Zr, Al and Sn. 1. A process for the manufacture of a cyclic diester of an alpha-hydroxyacid , comprising heating an alpha-hydroxyacid at a temperature from 100 to 250° C. in the presence of at least one polyol and of at least one catalyst selected from the group consisting carboxylates and alkoxides of Ti , Zr , Al and Sn.2. The process according to claim 1 , wherein said alpha-hydroxyacid is selected from the group consisting of lactic acid claim 1 , glycolic acid claim 1 , glutaric acid claim 1 , mandelic acid claim 1 , malic acid claim 1 , citric acid claim 1 , and tartaric acid.3. The process according to claim 1 , wherein said heating is conducted at a temperature from 150 to 240° C.4. The process according to claim 1 , wherein said heating is conducted under a pressure equal to or lower than 500 mbar.5. The process according to claim 1 , wherein said heating is initiated at atmospheric pressure claim 1 , then continues under a progressive vacuum until a pressure of from 10 to 200 mbar is attained.6. The process according to claim 1 , wherein said polyol is selected from the group consisting of ethylene glycol claim 1 , propylene glycol claim 1 , diethylene glycol claim 1 , glycerol claim 1 , erythritol claim 1 , mannitol claim 1 , sorbitol claim 1 , xylitol claim 1 , maltitol claim 1 , lactitol claim 1 , and volemitol.7. The process according to claim 1 , wherein said polyol is added in an amount of from 2 to 50 mol % of the alpha-hydroxyacid.8. The process according to claim 1 , wherein said catalyst is selected from the group consisting of carboxylates and alkoxides of titanium claim 1 , zirconium claim 1 , aluminum and tin claim 1 , particularly from titanium alkoxides.9. The ...

METHOD OF PRODUCING INGENOL-3-ANGELATE

The present invention relates to methods of producing ingenol-3-angelate (I) from ingenol (II). 4. The method according to claim 1 , wherein the method comprises the step of:(f) selective esterification of the 3-hydroxy group of compound (II) to obtain ingenol-3-angelate (I).5. The method according to claim 2 , wherein Rrepresents hydrogen or an ether claim 2 , acetal claim 2 , ketal claim 2 , silylether claim 2 , ester claim 2 , carbonate claim 2 , or a sulfenate derived hydroxyl protective group claim 2 , and Rrepresents hydrogen or an ether claim 2 , acetal claim 2 , ketal claim 2 , silylether claim 2 , ester claim 2 , carbonate claim 2 , or a sulfenate derived hydroxyl protective group.6. The method according to claim 2 , wherein D represents an acetal claim 2 , ketal- claim 2 , diacetal- claim 2 , diketal- claim 2 , ortho ester claim 2 , silyl claim 2 , boronate or a carbonate derived dihydroxyl protective group.7. The method according to claim 2 , wherein Ris selected from the group consisting of hydrogen or [(3 claim 2 ,4-dimethoxybenzyl)oxy]methyl claim 2 , guaiacolmethyl claim 2 , 2-methoxyethoxymethyl claim 2 , tetrahydropyranyl claim 2 , tetrahydrofuranyl claim 2 , 1-ethoxyethyl claim 2 , 1-methyl-1-methoxyethyl claim 2 , allyl claim 2 , prenyl claim 2 , p-methoxybenzyl claim 2 , triphenylmethyl claim 2 , 2-(trimethylsilyl)ethoxymethyl claim 2 , triethylsilyl claim 2 , triisopropylsilyl claim 2 , tert-butyldimethylsilyl claim 2 , dimethylisopropylsilyl claim 2 , diethylisopropylsilyl claim 2 , tert-butyldiphenylsilyl claim 2 , triphenylsilyl claim 2 , acetyl claim 2 , chloroacetyl claim 2 , phenoxyacetyl or angeloyl.8. The method according to claim 2 , wherein Ris selected from the group consisting of hydrogen or [(3 claim 2 ,4-dimethoxybenzyl)oxy]methyl claim 2 , guaiacolmethyl claim 2 , 2-methoxyethoxymethyl claim 2 , tetrahydropyranyl claim 2 , tetrahydrofuranyl claim 2 , 1-ethoxyethyl claim 2 , 1-methyl-1-methoxyethyl claim 2 , allyl claim 2 , prenyl ...

Esters of hexanoic acids as intermediates for the preparation of atorvastatin

The invention relates to compounds of general formula (3) wherein R 4 is allyl, 2-butyl, cyclohexyl, 3-methyl-2-butyl or 4-methyl-2-pentyl, a method for the preparation of compounds of general formula (3) and their use in the preparation of atorvastatin.

THERAPEUTICALLY ACTIVE COMPOSITIONS AND THEIR METHODS OF USE

Provided are methods of treating a cancer characterized by the presence of a mutant allele of IDH1 comprising administering to a subject in need thereof a compound described here. 2. The compound of claim 1 , wherein Ris 3-fluorophenyl.3. The compound of or claim 1 , wherein:{'sup': '1', 'Ris selected from cyclohexyl, cyclopentyl, cycloheptyl, 3,3-difluorocyclobutyl, 4,4,-difluorocyclohexyl, and bicyclo[2.2.1]heptanyl; and'}{'sup': '4', 'Ris selected from 1-(methylmethoxycarbonylamino)ethyl, 1,2,3,4-tetrahydroquinolin-1-yl, 1-ethoxycarbonylpiperidin-2-yl, 1-ethoxycarbonylpyrrolidin-2-yl, 1H-benzimidazol-1-ylmethyl, 1H-indazol-3-ylmethyl, indolin-1-ylmethyl, 1H-indol-3-ylmethyl, 1H-indol-5-ylmethyl, 1H-pyrrolo[2,3-b]pyridine-3-ylmethyl, 1H-pyrrolo[3,2-b]pyridin-3-ylmethyl, 1-methoxycarbonylpiperidin-2-yl, 1-methoxycarbonylpyrrolidin-2-yl, 2-fluoropyridin-3-ylaminomethyl, 2-imino-4-fluoropyridin-1-ylmethyl, 2-methoxyphenylaminomethyl, 2-methyl-1H-benzimidazol-1-ylmethyl, 2-methylimidazol-1-ylmethyl, 2-trifluoromethyl-1H-imidazol-1-yl, 3-cyanophenylaminomethyl, 3-fluoropyridin-2-ylaminomethyl, 3-methoxyphenylaminomethyl, 4-(1,3,4-oxadiazole-2-yl)phenylaminomethyl, 4-(dimethylaminocarbonyloxy)phenylmethyl, 4,5-dichloroimidazol-1-ylmethyl, 4-cyanophenylaminomethyl, 4-fluorophenylaminomethyl, 4-fluoropyridin-2-ylaminomethyl, 4-hydroxyphenylmethyl, 4-methoxycarbonylmorpholin-3-yl, 4-methoxycarbonylpiperazin-1-ylmethyl, 4-methoxyphenylaminomethyl, 4-methylcarbonyloxyphenylmethyl, 5-fluoropyridin-2-aminomethyl, 5-fluoropyridin-2-oxymethyl, 6-fluoropyridin-3-ylaminomethyl, benzomorpholin-4-ylmethyl, methoxycarbonylaminomethyl, methylmethoxycarbonylaminomethyl, methylphenylaminomethyl, phenylaminomethyl, pyridin-2-oxymethyl, pyridin-2-ylaminomethyl, pyridin-2-yloxymethyl, pyridin-3-oxymethyl, pyridin-3-ylmethyl, pyridin-4-ylmethyl, thiazol-4-ylmethyl, and thien-2-ylmethyl.'}4. The compound of claim 1 , wherein the compound is selected from any one of Compound numbers 104 claim ...

BENZODIOXANE INHIBITORS OF LEUKOTRIENE PRODUCTION

The present invention relates to compounds of formula (I): 2. The compound of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein group A is a group of formula —NRR.3. The compound of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein Ris —H or —(C-C)alkyl claim 1 , and Ris —(C-C)alkyl; wherein each —(C-C)alkyl of said Rand Rgroups claim 1 , when present claim 1 , is optionally independently substituted by one to three Rgroups.4. The compound of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein Ris —H or —(C-C)alkyl claim 1 , and Ris —(C-C)alkyl; wherein said —(C-C)alkyl of said Rgroup is substituted by —(C-C)cycloalkyl claim 1 , -(4- to 11-membered)heterocycloalkyl claim 1 , —(C-C)aryl claim 1 , or -(5- to 11-membered)heteroaryl; wherein each of said claim 1 , —(C-C)cycloalkyl claim 1 , -(4- to 11-membered)heterocycloalkyl claim 1 , —(C-C)aryl claim 1 , and -(5- to 11-membered)heteroaryl is optionally substituted with one to three groups independently selected from —(C-C)alkyl claim 1 , —CF claim 1 , and —C(O)OR.5. The compound of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein Ris —H or —(C-C)alkyl claim 1 , and Ris —(C-C)alkyl; wherein said —(C-C)alkyl of said Rgroup is independently substituted by one to three groups selected from —(C-C)alkyl claim 1 , —O(C-C)alkyl claim 1 , —C(O)R claim 1 , —C(O)OR claim 1 , —S(O)R claim 1 , and —NHC(O)R.6. The compound of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein Rand Rare each independently selected from —H or —(C-C)alkyl.7. The compound of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein Ris —H or —(C-C)alkyl claim 1 , and Ris —(C-C)cycloalkyl claim 1 , -(4- to 11-membered)heterocycloalkyl claim 1 , —(C-C)aryl claim 1 , and -(5- to 11-membered)heteroaryl; wherein each of the foregoing —(C-C)cycloalkyl claim 1 , -(4- to 11-membered)heterocycloalkyl claim 1 , —(C-C)aryl claim 1 ...

HETEROATOM CONTAINING CYCLIC DIMERS

The present invention provides cyclic dimers of alpha acids and polymers derived therefrom. Also provided are processes for preparing and methods of using the cyclic dimers and the polymers derived from the cyclic dimers. 2. The compound of claim 1 , wherein R claim 1 , R claim 1 , R claim 1 , R claim 1 , and Rare hydrogen; n is from 1 to 10; Z is chosen from sulfur claim 1 , sulfone claim 1 , sulfoxide claim 1 , and selenium; Ris lower chain alkyl claim 1 , and R claim 1 , if present claim 1 , is hydrogen or lower chain alkyl.4. The compound of claim 3 , wherein R claim 3 , R claim 3 , R claim 3 , R claim 3 , Rand Rare hydrogen;{'sup': 6', '10, 'each of n and m is from 1 to 10; Y and Z are independently chosen from sulfur, sulfone, sulfoxide, and selenium; Rand Rare lower chain alkyl; and'}{'sup': 7', '11, 'Rand R, if present, are independently hydrogen or lower chain alkyl.'}6. The compound of claim 5 , wherein R claim 5 , R claim 5 , R claim 5 , R claim 5 , and Rare hydrogen; n is from 1 to 10; Z is chosen from sulfur claim 5 , sulfone claim 5 , sulfoxide claim 5 , and selenium; Ris lower chain alkyl claim 5 , and R claim 5 , if present claim 5 , is hydrogen or lower chain alkyl.10. The compound of claim 9 , wherein R claim 9 , R claim 9 , R claim 9 , R claim 9 , Rand Rare hydrogen;{'sup': 6', '10, 'each of n and m is from 1 to 10; Y and Z are independently chosen from sulfur, sulfone, sulfoxide, and selenium; Rand Rare lower chain alkyl; and'}{'sup': 7', '11, 'Rand R, if present, are independently hydrogen or lower chain alkyl.'}12. The compound of claim 11 , wherein the compound comprises a racemic mixture.13. The compound of claim 11 , wherein ring atoms 3 and 6 have an L configuration.14. The compound of claim 11 , wherein ring atoms 3 and 6 have an D configuration.15. The compound of claim 11 , wherein ring atoms 3 and 6 have a meso configuration.17. The compound of claim 16 , wherein R claim 16 , R claim 16 , R claim 16 , R claim 16 , and Rare hydrogen; n ...

SKIN LIGHTENING COMPOSITIONS

Compositions and methods for lightening mammalian skin are described herein. 2. The composition of claim 1 , wherein Z is O.3. The composition of claim 1 , wherein A and B are taken together with the atoms to which they are attached to form an optionally substituted ring having from 4-9 member atoms.4. The composition of claim 1 , wherein A and B are taken to taken together with the atoms to which they are attached to form a ring having 6 member atoms.12. The composition of claim 1 , wherein the compound of formula I is 4-(tetrahydro-2H-pyran-2-yloxy)phenol.13. The composition of claim 1 , wherein the compound of formula I is present in the composition at a concentration of about 0.5 wt. % to about 10 wt. %.14. The composition of claim 1 , wherein the composition comprises an antioxidant and the antioxidant comprises at least one of ascorbic acid claim 1 , tocopherol claim 1 , butylated hydroxybenzoic acid claim 1 , butylated hydroxytoluene claim 1 , butylated hydroxyanisole claim 1 , uric acid claim 1 , gallic acid claim 1 , sorbic acid claim 1 , glutathione claim 1 , and esters and salts of any thereof.15. The composition of claim 1 , wherein the composition comprises an antioxidant and the antioxidant comprises at least one of ascorbic acid or a salt thereof claim 1 , ascorbyl phosphate or a salt thereof claim 1 , ascorbyl palmitate or a salt thereof claim 1 , tocopherol or a salt thereof claim 1 , tocopheryl acetate and sodium metabisulfite.16. The composition of claim 1 , comprising at least two antioxidants.17. The composition of claim 1 , comprising at least three antioxidants.18. The composition of claim 1 , comprising at least four antioxidants.19. The composition of claim 1 , comprising at least five antioxidants.20. The composition of claim 1 , wherein the composition comprises an antioxidant and the antioxidant is present in an amount of about 0.01 wt. % to about 3.0 wt. %.21. The composition of claim 1 , wherein the composition comprises an antioxidant ...

PROCESS FOR MANUFACTURING LACTIC ACID

A process for the preparation of lactic acid includes: 1. A process for the preparation of lactic acid comprising:a) providing an aqueous medium comprising magnesium lactate;b) adding to the aqueous medium comprising magnesium lactate a monovalent base to form an aqueous medium comprising a water soluble monovalent lactate salt and a solid magnesium base;c) separating the magnesium base from the aqueous medium comprising the water soluble monovalent lactate salt;d) adjusting the concentration of the monovalent lactate salt in the aqueous medium to a value between 10 and 30 wt. %,e) subjecting the aqueous medium comprising the monovalent lactate salt to water-splitting electrodialysis, to produce a first solution comprising monovalent base and a second solution comprising lactic acid and monovalent lactate salt, the electrodialysis being carried out to a partial conversion of 40 to 98 mole %;f) separating the second solution comprising lactic acid and monovalent lactate salt into lactic acid and a solution comprising the monovalent lactate salt by vapour-liquid separation;g) recycling the solution of step f) comprising the monovalent lactate salt to step d).2. The process according to claim 1 , wherein the vapour-liquid separation comprises distillation.3. The process according to claim 1 , wherein the electrodialysis is carried out to a partial conversion of 40 to 95 mole %.4. The process according to claim 3 , wherein the electrodialysis is carried out to a partial conversion of about 85 mole %.5. The process according to claim 1 , wherein concentration of the monovalent lactate salt in the aqueous medium of d) is adjusted to a value between 20 and 25 wt. %.6. The process according to claim 1 , wherein the first solution comprising the monovalent base produced by the water-splitting electrodialysis of step e) is recycled to step b).7. The process according to claim 1 , wherein the water-splitting electrodialysis is carried out in an electrodialysis apparatus ...

Condensation and washing device, polymerisation device and method for cleaning process steam during the production of polylactide

The present invention relates to a condensation and washing device with which in particular the process vapours which occur during the production of polylactide can be processed and cleaned. Furthermore, the present invention relates to a polymerisation device for the production of polylactide and also to a method for processing process vapours which occur during the production of polylactide; possibilities for use of both the condensation and washing devices and of the method are likewise mentioned.

TREATMENT OF MITOCHONDRIAL DISEASES

The invention relates the method of treatment or amelioration of mitochondrial disorders such as Alzheimer's disease, Parkinson's disease, Friedreich's ataxia (FRDA), cerebellar ataxias, Leber's hereditary optic neuropathy (LHON), mitochondrial myopathy, encephalopathy, lactacidosis, stroke (MELAS), Myoclonic Epilepsy with Ragged Red Fibers (MERFF), amyotrophic lateral sclerosis (ALS), motor neuron diseases, Huntington's disease, macular degeneration, and epilepsy, with chroman derivatives of Formula I or Formula II as described herein. 2. The method of claim 1 , comprising administering to said subject a therapeutically effective amount of a compound of Formula I.3. The method of claim 2 , comprising administering the compound of Formula I wherein Ris hydrogen claim 2 , Calkyl claim 2 , or Calkenyl.4. The method of claim 2 , comprising administering the compound of Formula I wherein Rand Rare independently of each other Calkyl or halogen.5. The method of claim 4 , comprising administering the compound of Formula I wherein Ris Calkyl and Ris Calkyl.6. The method of claim 2 , comprising administering the compound of Formula I wherein Ris Calkyl claim 2 , and Ris Calkyl or Calkenyl.7. The method of claim 2 , comprising administering the compound of Formula I wherein Rand Rtaken together with the carbon to which they are attached form a 5-6 membered carbocyclic ring claim 2 , optionally substituted with Calkyl claim 2 , Calkoxy claim 2 , hydroxy claim 2 , carboxy claim 2 , carboxyalkyl claim 2 , alkoxycarbonyl claim 2 , alkoxycarbonylalkyl claim 2 , aminocarbonyl claim 2 , aminocarbonylalkyl claim 2 , or hydroxyalkyl.8. The method of claim 1 , comprising administering to said subject a therapeutically effective amount of a compound of Formula II.9. The method of claim 8 , comprising administering the compound of Formula II claim 8 , wherein Ris —COOH claim 8 , or —COORand Ris Calkyl.11. The method of claim 1 , comprising administering a therapeutically effective amount ...

Modulators of ATP-Binding Cassette Transporters

Compounds of the present invention and pharmaceutically acceptable compositions thereof, are useful as modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator (“CFTR”). The present invention also relates to methods of treating ABC transporter mediated diseases using compounds of the present invention. 171-. (canceled)7375-. (canceled)76. The method of claim 72 , wherein the one Rattached to the 3- or 4-position of the phenyl ring is an aryl optionally substituted with 1 claim 72 , 2 claim 72 , or 3 of R claim 72 , wherein Ris —ZR; in which each Zis independently a bond or an optionally substituted branched or straight Caliphatic chain wherein up to two carbon units of Zare optionally and independently replaced by —CO— claim 72 , —CS— claim 72 , —CONR— claim 72 , —CONRNR— claim 72 , —CO— claim 72 , —OCO— claim 72 , —NRCO— claim 72 , —O— claim 72 , —NRCONR— claim 72 , —OCONR— claim 72 , —NRNR— claim 72 , —NRCO— claim 72 , —S— claim 72 , —SO— claim 72 , —SO— claim 72 , —NR— claim 72 , —SONR— claim 72 , —NRSO— claim 72 , or —NRSONR—; each Ris independently R claim 72 , halo claim 72 , —B(OH) claim 72 , —OH claim 72 , —NH claim 72 , —NO claim 72 , —CN claim 72 , or —OCF; and each Ris independently hydrogen claim 72 , an optionally substituted Caliphatic group claim 72 , an optionally substituted cycloaliphatic claim 72 , an optionally substituted heterocycloaliphatic claim 72 , an optionally substituted aryl claim 72 , or an optionally substituted heteroaryl.77. The method of claim 76 , wherein the one Rattached to the 3- or 4-position of the phenyl ring is a phenyl optionally substituted with 1 claim 76 , 2 claim 76 , or 3 of R.78. The method of claim 72 , wherein Ris hydrogen or methyl.79. The method of claim 72 , wherein ring A is an unsubstituted Ccycloaliphatic.80. The method of claim 79 , wherein ring A is an unsubstituted cyclopropyl claim 79 , an unsubstituted cyclopentyl claim 79 ...

Liquid-crystalline compounds and liquid-crystalline media

The present invention relates to liquid-crystalline compounds containing an O-heterocyclic ring, three partially fluorinated benzene rings and a —CF 2 O— bridge between the rings. In addition, the invention relates to liquid-crystalline media prepared therewith and to liquid-crystal display devices (LC displays) containing these media.

HIV-1 INHIBITING PHARMACEUTICAL COMPOSITION CONTAINING AN ECKLONIA CAVA-DERIVED PHLOROGLUCINOL POLYMER COMPOUND

The present invention relates to a HIV-1 inhibiting pharmaceutical composition containing, as an active ingredient, 6,6′-bieckol which is a phloroglucinol polymer compound separated from Ecklonia cava. The Ecklonia cava-derived 6,6′-bieckol according to the present invention inhibits HIV-1 induced cell fusion, the cell lysis effect, and the cytopathogenic effect including virus p24 antibody production, exhibits RT enzyme inhibition activity and HIV-1 infection inhibition activity, and shows no cytotoxicity at the concentration that almost perfectly inhibits HIC-1 replication. 1. A method of treating an HIV-1 infected patient comprising:administering a pharmaceutical composition comprising a phloroglucinol polymer compound derived from Ecklonia cava as an active ingredient at a dose determined to be non-cytoxic and inhibit HIV-1 replication and reverse transcriptase activity in a patient.2. The method of claim 1 , wherein the phloroglucinol polymer compound is 6 claim 1 ,6′-bieckol. This application is a divisional of U.S. patent application Ser. No. 13/123,206, filed Jul. 1, 2011, which is a national stage application under 35 USC 371 of International Application No. PCT/KR2009/005354, filed Sep. 21, 2009, which claims the priority of Korean Patent Application No. 10-2008-0098327, filed Oct. 7, 2008, the contents of all of which prior applications are incorporated herein by reference.The present invention relates to a HIV-1 inhibiting pharmaceutical composition containing an Ecklonia cava-derived phloroglucinol polymer compound. More particularly, the present invention relates to a HIV-1 inhibiting pharmaceutical composition containing 6,6′-bieckol as an active ingredient which is a phloroglucinol polymer compound separated from Ecklonia cava.Human immunodeficiency virus type-1 (Human Immunodeficiency virus type-1; HIV-1) is identified as the causative agent of acquired immunodeficiency syndrome (AIDS) which is one of the most important diseases with about 33 ...

BENZODIOXANE INHIBITORS OF LEUKOTRIENE PRODUCTION

The present invention relates to compounds of formula (I): 120-. (canceled)21. A compound selected from the group consisting of:1-[4-(2,3-dihydro-1,4-benzodioxin-2-yl)benzyl]pyrrolidine;4-[4-(2,3-dihydro-1,4-benzodioxin-2-yl)benzyl]morpholine;1-[4-(2,3-dihydro-1,4-benzodioxin-2-yl)benzyl]-4,4-dimethylpiperidine;8-[4-(2,3-dihydro-1,4-benzodioxin-2-yl)benzyl]-2,8-diazaspiro[4.5]decan-1-one;1-[4-(2,3-dihydro-1,4-benzodioxin-2-yl)benzyl]-4-fluoropiperidine;(1s,4s)-7-[4-(2,3-dihydro-1,4-benzodioxin-2-yl)benzyl]-7-azabicyclo[2.2.1]heptane;4-[4-(2,3-dihydro-1,4-benzodioxin-2-yl)benzyl]thiomorpholine 1,1-dioxide;1-{4-[(2S)-2,3-dihydro-1,4-benzodioxin-2-yl]benzyl}-N,N-dimethylpiperidine-4-carboxamide;(3S)-1-[4-(2,3-dihydro-1,4-benzodioxin-2-yl)benzyl]pyrrolidin-3-ol;1-({1-[4-(2,3-dihydro-1,4-benzodioxin-2-yl)benzyl]piperidin-3-yl}methyl)pyrrolidin-2-one;1-{4-[4-(2,3-dihydro-1,4-benzodioxin-2-yl)benzyl]piperazin-1-yl}ethanone;2-{[4-(2,3-dihydro-1,4-benzodioxin-2-yl)benzyl]amino}-1-(pyrrolidin-1-yl)ethanone;N-{4-[(2S)-2,3-dihydro-1,4-benzodioxin-2-yl]benzyl}-N-methyl-1-(methylsulfonyl)piperidin-4-amine;1-{4-[{4-[(2S)-2,3-dihydro-1,4-benzodioxin-2-yl]benzyl}(methyl)amino]piperidin-1-yl}ethanone;3-[4-(pyrrolidin-1-ylmethyl)phenyl]-2,3-dihydro[1,4]dioxino[2,3-b]pyridine;7-[4-(2,3-dihydro-1,4-benzodioxin-2-yl)benzyl]-5,6,7,8-tetrahydro[1,2,4]triazolo[4,3-a]pyrazine;3-{4-[(1,1-dioxidothiomorpholin-4-yl)methyl]phenyl}-2,3-dihydro[1,4]dioxino[2,3-b]pyridine;3-[4-(morpholin-4-ylmethyl)phenyl]-2,3-dihydro[1,4]dioxino[2,3-b]pyridine;(3R)-1-{4-[(2S)-2,3-dihydro-1,4-benzodioxin-2-yl]benzyl}piperidine-3-carboxylic acid;(3S)-1-{4-[(2S)-2,3-dihydro-1,4-benzodioxin-2-yl]benzyl}piperidine-3-carboxylic acid;1-(1-{4-[(2S)-2,3-dihydro-1,4-benzodioxin-2-yl]benzyl}piperidin-4-yl)-2,2,2-trifluoroethanol;2-(1-{4-[(2S)-2,3-dihydro-1,4-benzodioxin-2-yl]benzyl}piperidin-4-yl)-1,1,1,3,3,3-hexafluoropropan-2-ol;N-[4-(2,3-dihydro-1,4-benzodioxin-2-yl)benzyl]-2-methylpropan-2-amine;(2R)—N-[4-(2,3-dihydro-1, ...

PROCESS FOR MAKING CHEMICAL DERIVATIVES

Process and methods for making glycolic acid chemical intermediates and derivatives from biomass are described herein. 1. A method of producing a glycolic acid monomer component product from a genetically modified polyhydroxyalkanoate (PHA) biomass , comprising:heating the biomass to release a glycolic acid monomer component from the PHA, optionally in the presence of a catalyst, wherein the glycolic acid monomer component yield is about 70% based on one gram of glycolic acid monomer component product per gram of polyhydroxyalkanoate.2. The method of claim 1 , further including producing a glycolide component.3. The method of claim 1 , wherein the biomass is dried prior to heating.4. The method of claim 1 , wherein the biomass is from a recombinant host selected from a plant crop claim 1 , bacteria claim 1 , a yeast claim 1 , a fungi claim 1 , an algae claim 1 , a cyanobacteria claim 1 , or a mixture of any two or more thereof.5. The method of claim 4 , wherein the host is bacteria.6Escherichia coli, Alcaligenes eutrophusRalstonia eutrophaBacillusAlcaligenes latus, Azotobacter, Aeromonas, Comamonas, Pseudomonads, Pseudomonas, Ralstonia, KlebsiellaSynechococcusSynechococcusSynechocystis, Thermosynechococcus elongatusChlorobium tepidum Chloroflexusauranticus, Chromatium tepidum, Chromatium vinosum Rhodospirillum rubrum, Rhodobacter capsulatusRhodopseudomonas palustris.. The method of claim 5 , wherein the bacteria is selected from (renamed as ) claim 5 , spp. claim 5 , ) claim 5 , sp PCC7002 claim 5 , sp. PCC 7942 claim 5 , sp. PCC 6803BP-I claim 5 , claim 5 , and7. The method of claim 4 , wherein the host is a plant crop.8. The method of claim 7 , wherein the plant crop is selected from tobacco claim 7 , sugarcane claim 7 , corn claim 7 , switchgrass claim 7 , miscanthus sorghum claim 7 , sweet sorghum claim 7 , or a mixture of any two or more thereof.9. The method of claim 1 , wherein the polyhydroxyalkanoate is a polyglycolic acid or a co-polymer thereof.10. The ...

RECOVERY OF LACTIC ACID VALUES FROM A MESO-LACTIDE STREAM

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. 1. A process for recovering lactic acid values from a starting lactide composition , comprisinga) subjecting a starting lactide composition to a temperature of up to 170° C. in the presence of a racemization catalyst for a time sufficient to racemize at least a portion of the lactide in the starting lactide composition to form a racemized lactide mixture that contains meso-lactide, S,S-lactide and R,R-lactide in relative proportions different than in the starting lactide composition.3. The process of claim 2 , wherein the racemization catalyst is 1 claim 2 ,4-dimethyl piperazine or 1 claim 2 ,4-diethyl piperazine.5. The process of claim 4 , wherein X is an —NR′R″ group claim 4 , wherein R′ and R″ are each alkyl or aryl-substituted alkyl claim 4 , or R′ and R″ together form a divalent group that forms a ring structure that includes the nitrogen atom of the —NR′R″ group.6. The process of claim 4 , wherein the racemization catalyst is 4-dimethylaminopyridine or 4-diethylaminopyridine.7. The process of claim 1 , wherein the racemization catalyst is an alkali metal salts of an alkanoic acid having one to 6 carbon atoms.8. The process of claim 7 , wherein the racemization ...

Bioavailable Diacylhydrazine Ligands for Modulating the Expression of Exogenous Genes via an Ecdysone Receptor Complex

The present invention relates to non-steroidal ligands for use in nuclear receptor-based inducible gene expression system and a method to modulate exogenous gene expression in which an ecdysone receptor complex comprising a DNA binding domain; a ligand binding domain; a transactivation domain; and a ligand is contacted with a DNA construct comprising: the exogenous gene and a response element; wherein the exogenous gene is under the control of the response element and binding of the DNA binding domain to the response element in the presence of the ligand results in activation or suppression of the gene. 114-. (canceled)15. A compound selected from the group consisting of:5-methyl-2,3-dihydro-benzo[1,4]dioxine-6-carboxylic acid N′-(3,5-dimethyl-benzoyl)-N′-(1-ethyl-2,2-dimethyl-propyl)-hydrazide;5-methyl-2,3-dihydro-benzo[1,4]dioxine-6-carboxylic acid N′-(3,5-dimethoxy-4-methyl-benzoyl)-N′-(1-ethyl-2,2-dimethyl-propyl)-hydrazide;5-methyl-2,3-dihydro-benzo[1,4]dioxine-6-carboxylic acid N′-(1-tert-butyl-butyl)-N′-(3,5-dimethyl-benzoyl)-hydrazide;5-methyl-2,3-dihydro-benzo[1,4]dioxine-6-carboxylic acid N′-(1-tert-butyl-butyl)-N′-(3,5-dimethoxy-4-methyl-benzoyl)-hydrazide;5-ethyl-2,3-dihydro-benzo[1,4]dioxine-6-carboxylic acid N′-(3,5-dimethyl-benzoyl)-N′-(1-ethyl-2,2-dimethyl-propyl)-hydrazide;5-ethyl-2,3-dihydro-benzo[1,4]dioxine-6-carboxylic acid N′-(3,5-dimethoxy-4-methyl-benzoyl)-N′-(1-ethyl-2,2-dimethyl-propyl)-hydrazide;5-ethyl-2,3-dihydro-benzo[1,4]dioxine-6-carboxylic acid N′-(1-tert-butyl-butyl)-N′-(3,5-dimethyl-benzoyl)-hydrazide;5-ethyl-2,3-dihydro-benzo[1,4]dioxine-6-carboxylic acid N′-(1-tert-butyl-butyl)-N′-(3,5-dimethoxy-4-methyl-benzoyl)-hydrazide;3,5-dimethoxy-4-methyl-benzoic acid N-(1-ethyl-2,2-dimethyl-propyl)-N′-(3-methoxy-2-methyl-benzoyl)-hydrazide;3,5-dimethyl-benzoic acid N-(1-tert-butyl-butyl)-N′-(3-methoxy-2-methyl-benzoyl)-hydrazide;3,5-dimethoxy-4-methyl-benzoic acid N-(1-tert-butyl-butyl)-N′-(3-methoxy-2-methyl-benzoyl)-hydrazide;3,5- ...

Spirocyclic nitriles as protease inhibitors

The invention relates to substituted carbo- and heterocyclic spiro compounds of the formula Ia which inhibit thiol proteases, to processes for their preparation and to the use thereof as medicaments. 2. A pharmaceutical composition comprising a therapeutically effective amount of the compound of or a physiologically tolerated salt thereof and a pharmaceutically acceptable carrier.4. The method of claim 3 , wherein the condition or disorder is osteoarthritis.5. The method of claim 3 , wherein the condition or disorder is bone loss. This application is a continuation of U.S. application Ser. No. 13/248,366, filed Sep. 29, 2011, which is a divisional of U.S. application Ser. No. 12/277,880, filed Nov. 25, 2008, which is a continuation of International Application No. PCT/EP2007/004550, filed May 23, 2007, which are incorporated herein by reference in their entirety; and claims the benefit of priority of German Patent Application No. 102006025630.1, filed Jun. 1, 2006.The invention relates to substituted carbo- and heterocyclic spiro compounds of the formula Ia which inhibit thiol proteases, to processes for their preparation and to the use thereof as medicaments.Proteolytic enzymes, known as proteases and peptidases, are very important enzymes which make up about 2% of the genes in the human organism, pathogenic microorganisms and also other life forms. Their particular significance is that they influence many physiological processes by playing an important role in the activation, synthesis or degradation of other proteins. This inevitably gives rise to a crucial regulatory function starting at conception, birth, growth, maturation, aging, diseases up to death.The balance of the different processes is of crucial significance for the life and survival of the organism. When there is an imbalance of protease-catalyzed processes as a result of endogenous or exogenous factors such as genetic predisposition or environmental factors, massive disruption can occur in the normal ...

B- AND y -DIKETONES AND y -HYDROXYKETONES AS WNT/ B -CATENIN SIGNALING PATHWAY ACTIVATORS

The present invention discloses β-diketones, γ-diketones or γ-hydroxyketones or analogs thereof, that activate Wnt/β-catenin signaling and thus treat or prevent diseases related to signal transduction, such as osteoporosis and osteoarthropathy; osteogenesis imperfecta, bone defects, bone fractures, periodontal disease, otosclerosis, wound healing, craniofacial defects, oncolytic bone disease, traumatic brain injuries related to the differentiation and development of the central nervous system, comprising Parkinson's disease, strokes, ischemic cerebral disease, epilepsy, Alzheimer's disease, depression, bipolar disorder, schizophrenia; eye diseases such as age related macular degeneration, diabetic macular edema or retinitis pigmentosa and diseases related to differentiation and growth of stem cell, comprising hair loss, hematopoiesis related diseases and tissue regeneration related diseases. 1. (canceled)4. The method of claim 2 , wherein Ris a substituted or unsubstituted phenyl.12. The method of claim 10 , wherein Ris a substituted or unsubstituted phenyl.19. The method of claim 17 , wherein Ris a substituted or unsubstituted phenyl.27. The method of claim 25 , wherein Ris a substituted or unsubstituted phenyl.32. The method of claim 2 , wherein the compound is topically administered to the mammal.33. The method of claim 10 , wherein the compound is topically administered to the mammal.34. The method of claim 17 , wherein the compound is topically administered to the mammal.35. The method of claim 25 , wherein the compound is topically administered to the mammal. This application is a continuation application of U.S. application Ser. No. 13/211,665, filed Aug. 17, 2011, and claims the benefit of U.S. Provisional Application No. 61/427,974, filed Dec. 29, 2010, and U.S. Provisional Application No. 61/374,687, filed Aug. 18, 2010, each of which is incorporated herein by reference in its entirety.1. Field of the InventionThis invention relates to activators of one or ...

Novel Ether Linked Compounds and Improved Treatments for Cardiac and Cardiovascular Disease

A compound of Formula (I), and its pharmaceutically acceptable salt or salts and physiologically hydrolysable derivatives in free form or salt form: 2. The compound as claimed in claim 1 , wherein Qand Qor Qand Qtogether form a Cheteroaryl or Cheterocylclic ring; optionally containing one or two heteroatoms selected from N and O claim 1 , optionally substituted by up to two groups selected from R.4. The compound as claimed in claim 1 , wherein Ris chloro claim 1 , bromo or fluoro claim 1 , Calkyl claim 1 , Calkoxy or cyano.5. The compound as claimed in claim 1 , wherein Ris CcycloalkylCalkyl or phenylCalkyl where the Calkyl optionally contains 1 or 2 heteroatoms selected from O.6. The compound as claimed in claim 1 , wherein Rand Rare both hydrogen.7. The compound as claimed in claim 1 , wherein Xis —O—.8. The compound as claimed in claim 1 , wherein Xis phenyl or a 9-10 membered heteroaryl ring.9. The compound as claimed in claim 1 , wherein Xis a 9-10 membered heterocyclic ring selected from isoindoline and 2 claim 1 ,3-dihydroxybenzimidazole10. The compound as claimed in claim 1 , wherein and Ris selected from amino claim 1 , carboxy claim 1 , halo claim 1 , Calkyl claim 1 , Calkoxy claim 1 , Cperfluoroalkyl claim 1 , oxo claim 1 , —NHC(O)Calkyl or —CONH.12. A composition comprising a therapeutically effective amount of a compound of Formula (I) or subformulae or its pharmaceutically acceptable salt and physiologically hydrolysable derivative as defined in in association with one or more pharmaceutical carriers or diluents.13. The compound as claimed in claim 1 , for in the prevention or treatment of a condition selected from ischaemic heart disease claim 1 , hypertension and heart failure claim 1 , more preferably with concomitant respiratory disease claim 1 , in particular asthma or COPD.15. A method for the treatment of a condition selected from ischaemic heart disease claim 1 , hypertension and heart failure claim 1 , more preferably with concomitant ...

METHOD FOR PRODUCING GLYCOLIDE

A method for producing glycolide (GL) by heating a glycolic acid oligomer (GAO) to depolymerize the GAO. The method for producing GL comprises: a step 1 of heating a mixture containing a GAO having a terminal COOH concentration of 400 eq/t or less and a polar organic solvent to a GAO depolymerization temperature under ambient pressure or reduced pressure; a step 2 of continuing the heating at the temperature for depolymerizing of the GAO and then codistilling out the produced GL and the solvent from the depolymerization reaction system to the outside the reaction system; and a step 3 of obtaining GL from the codistillation product. In the method for producing GL, the GAO is preferably prepared by a GAO production method which comprises a step of condensing glycolic acid (GA) and a dehydration step of continuing the heating together with a polar organic solvent or a depolymerization reaction solution to allow the GA condensation reaction to continue. 1. A method for producing glycolide by heating a glycolic acid oligomer to depolymerize , the method comprising steps below:I. a step 1 of heating a mixture containing a glycolic acid oligomer having a terminal carboxyl group concentration of 400 eq/t or less and a polar organic solvent to a temperature for depolymerizing the glycolic acid oligomer under ambient pressure or reduced pressure;II. a step 2 of continuing the heating at the temperature for depolymerizing the glycolic acid oligomer and then codistilling out, together with the polar organic solvent, glycolide produced by the depolymerization from a depolymerization reaction system containing the mixture; andIII. a step 3 of obtaining glycolide from the codistillation product.2. The method for producing glycolide according to claim 1 , wherein the glycolic acid oligomer is a glycolic acid oligomer having a terminal carboxyl group concentration of 250 eq/t or less.3. The method for producing glycolide according to claim 1 , wherein the glycolic acid oligomer ...

METHOD FOR PRODUCING GLYCOLIDE

A method for producing a GL comprising: (I) a heating step of heating a mixture either under normal pressure or reduced pressure at a temperature at which a polyglycolic acid (PGA) undergoes depolymerization, the mixture containing the PGA and a polyethylene glycol ether which is represented by the formula: X—O—(—CHCH—O—)—Y (wherein X and Y are each independently an alkyl group or an aryl group having from 2 to 20 carbon atoms, and p is an integer from 1 to 5) and which has a molecular weight of from 150 to 450 and a boiling point of from 130 to 220° C. at a pressure of 3 kPa; (II) a solution-forming step in which the mixture is rendered in a solution state in which a melt phase of the PGA and a liquid phase consisting of the polyethylene glycol ether essentially form a uniform phase; (III) a GL production step in which a glycolide (GL) is produced by a depolymerization reaction of the PGA by continuing to heat the mixture in the solution state; (IV) a distillation step of distilling off the produced GL together with the polyethylene glycol ether (B) from the depolymerization reaction system; and (V) a recovery step of recovering the GL from the distillate. 1. A method for producing a glycolide by depolymerizing a polyglycolic acid , the method comprising: {'br': None, 'sub': 2', '2', 'p, 'X—O—(—CHCH—O—)—Y\u2003\u2003(1)'}, '(I) a heating step of heating a mixture either under normal pressure or reduced pressure at a temperature at which a polyglycolic acid (A) undergoes depolymerization, the mixture containing the polyglycolic acid (A) and a polyethylene glycol ether (B) which is represented by the following formula (1)(wherein X and Y are each independently an alkyl group or an aryl group having from 2 to 20 carbon atoms, and p is an integer from 1 to 5)and which has a molecular weight of from 150 to 450 and a boiling point of from 130 to 220° C. at a pressure of 3 kPa;(II) a solution-forming step in which the mixture is rendered in a solution state in which a ...

GLYCOLIDE PRODUCTION METHOD

The object of the present invention is to provide a glycolide production method capable of further increasing the production rate of glycolide. The glycolide production method according to the present invention includes adding metal iron to an aqueous glycolic acid solution, subjecting glycolic acid contained in the aqueous glycolic acid solution to which the metal iron is added, to dehydrating polycondensation to obtain a glycolic acid oligomer, and heating and depolymerizing the glycolic acid oligomer to obtain glycolide. 1. A glycolide production method comprising:adding metal iron to an aqueous glycolic acid solution;subjecting glycolic acid contained in the aqueous glycolic acid solution to which the metal iron is added, to dehydrating polycondensation to obtain a glycolic acid oligomer; andheating and depolymerizing the glycolic acid oligomer to obtain glycolide.2. The glycolide production method according to claim 1 , wherein an addition amount of the metal iron is from 10 ppm to 1000 ppm relative to a total mass of the glycolic acid.3. The glycolide production method according to claim 1 , wherein the metal iron is iron powder.4. The glycolide production method according to claim 3 , wherein an average particle size of the iron powder is from 1 μm to 1000 μm.5. The glycolide production method according to claim 1 , wherein a dehydrating polycondensation temperature is from 50° C. to 300° C.6. The glycolide production method according to claim 1 , wherein the depolymerization is carried out in the presence of a polyalkylene glycol ether represented by Formula (1):{'br': None, '[Chemical Formula 1]'}{'br': None, 'i': 'p', 'X—O—(—R—O-)-Y\u2003\u2003(1)'}in Formula (1),R is a methylene group, or a linear or branched alkylene group having from 2 to 8 carbons,X and Y each independently denote an alkyl group or an aryl group having from 2 to 20 carbons,p is an integer from 1 to 5, andwhen p is 2 or greater, a plurality of R moieties may be the same or different. ...

Diacylhydrazine Ligands for Modulating the Expression of Exogenous Genes in Mammalian Systems via an Ecdysone Receptor Complex

The present invention relates to non-steroidal ligands for use in nuclear receptor-based inducible gene expression system, and a method to modulate exogenous gene expression in which an ecdysone receptor complex comprising: a DNA binding domain; a ligand binding domain; a transactivation domain; and a ligand is contacted with a DNA construct comprising: the exogenous gene and a response element; wherein the exogenous gene is under the control of the response element and binding of the DNA binding domain to the response element in the presence of the ligand results in activation or suppression of the gene. 15-. (canceled)7. The method of claim 6 , wherein the compound is of the specified formula and:X and X′ are O; [{'sub': 1', '4', '1', '4', '1', '4, '(a) substituted or unsubstituted phenyl wherein the substituents are independently 1-5 H, (C-C)alkyl, (C-C)alkoxy, halo (F, Cl, Br, I), (C-C)haloalkyl, cyano, or nitro; or'}, {'sub': 1', '4', '1', '4', '1', '4, '(b) substituted or unsubstituted 2-pyridyl, 3-pyridyl, or 4-pyridyl, wherein the substituents are independently 1-4 H, (C-C)alkyl, (C-C)alkoxy, halo (F, Cl, Br, I), (C-C)haloalkyl, cyano, or nitro;'}], 'Y is{'sup': '3', 'Ris H, methyl, ethyl, or cyano;'}{'sup': 4', '7', '8, 'sub': 1', '4', '1', '4', '1', '4, 'R, R, and Rare independently: H, (C-C)alkyl, (C-C)alkoxy, halo (F, Cl, Br, I), (C-C)haloalkyl, cyano, or nitro; and'}{'sup': 5', '6, 'sub': 1', '4', '1', '4', '1', '4, 'Rand Rare independently: H, (C-C)alkyl, halo (F, Cl, Br, I), C-Chaloalkyl, (C-C)alkoxy, hydroxy, amino, cyano, or nitro.'}8. (canceled)9. The method of claim 7 , wherein the compound is of the specified formula and: [{'sub': 1', '4', '1', '4', '1', '4, '(a) substituted or unsubstituted phenyl wherein the substituents are independently 1-5 H, (C-C)alkyl, (C-C)alkoxy, halo (F, Cl, Br, I), (C-C)haloalkyl; or'}, {'sub': 1', '4', '1', '4', '1', '4, '(b) substituted or unsubstituted 3-pyridyl, wherein the substituents are independently 1-4 H, (C- ...

RESIST COMPOSITION, METHOD OF FORMING RESIST PATTERN, COMPOUND, AND ACID DIFFUSION-CONTROLLING AGENT

A resist composition that contains a base material component exhibiting changed solubility in a developing solution under action of acid and a compound (D0) represented by General Formula (d0), in which R, R, R, and Reach independently represents a hydrogen atom, a hydroxy group, a halogen atom, or an alkyl group; alternatively, Rand R, Rand R, or Rand Rare bonded to each other to form an aromatic ring; Rrepresents a hydrogen atom or an alkyl group; Y represents a group that forms an alicyclic group together with a carbon atom *C; provided that at least one of the carbon atoms that form the alicyclic group is substituted with an ether bond, a thioether bond, a carbonyl group, a sulfinyl group, or a sulfonyl group; m represents an integer of 1 or more, and M represents an m-valent organic cation 2. The resist composition according to claim 1 , wherein a content of the compound (D0) is in a range of 1 to 35 parts by mass with respect to 100 parts by mass of the base material component (A).3. The resist composition according to claim 1 , further comprising an acid generator component (B) generating an acid upon exposure claim 1 , provided that the compound (D0) is excluded from the acid generator component (B).4. The resist composition according to claim 1 , wherein the base material component (A) contains a resin component (A1) claim 1 , and the resin component (A1) has a constitutional unit (a1) that contains an acid-decomposable group having a polarity which is increased by action of an acid.5. A method of forming a resist pattern claim 1 , comprising:{'claim-ref': {'@idref': 'CLM-00001', 'claim 1'}, 'forming a resist film on a support using the resist composition according to ;'}exposing the resist film; anddeveloping the exposed resist film to form a resist pattern.6. The method of forming a resist pattern according to claim 5 , wherein the resist film is exposed with extreme ultraviolet (EUV) rays or electron beam (EB).8. An acid diffusion-controlling agent ...

Process for Making Chemical Derivatives

Process and methods for making glycolic acid chemical intermediates and derivatives from biomass are described herein. 1. A continuous biorefinery process for the production of glycolide from a genetically engineered PHA biomass comprising ,a) culturing the genetically engineered PHA biomass to produce polyglycolide;b) heating the polyglycolide with a catalyst to produce a glycolide monomer component; andc) recovering the glycolide monomer, wherein the biomass is from a recombinant host selected from a plant crop, bacteria, yeast, fungi, algae, cyanobacteria, or a mixture of any two or more thereof.2. The process of claim 1 , wherein the biomass is dried prior to heating.3. The process of claim 1 , wherein the heating is pyrolysis claim 1 , torrefaction or flash pyrolysis.4. The process of claim 1 , wherein the weight percent of catalyst is about 5% to about 15%.5. A method of producing a glycolide component product from a genetically modified polyhydroxyalkanoate (PHA) biomass claim 1 , comprising:heating the biomass optionally in the presence of a catalyst to release a glycolide component from the PHA, wherein the glycolide component yield is about 70% based on one gram of glycolide component per gram of polyhydroxyalkanoate, wherein the biomass is from a recombinant host selected from a plant crop, bacteria, a yeast, a fungi, an algae, a cyanobacteria, or a mixture of any two or more thereof.6. The method of claim 5 , wherein the biomass is dried prior to heating.7. The method of claim 5 , wherein the host is bacteria.8Escherichia coli, Alcaligenes eutrophusRalstonia eutrophaBacillusAlcaligenes latus, Azotobacter, Aeromonas, Comamonas, Pseudomonads, Pseudomonas, Ralstonia, KlebsiellaSynechococcus, SynechococcusSynechocystisThermosynechococcus elongatusChlorobium tepidum Chloroflexusauranticus, Chromatium tepidum, Chromatium vinosum Rhodospirillum rubrum, Rhodobacter capsulatusRhodopseudomonas palustris.. The method of claim 7 , wherein the bacteria is selected ...

MANUFACTURING METHOD OF LACTIDE FROM LACTIC ACID

The present invention provides a method of producing D-type lactide from liquid D-type lactic acid, and a method for producing D-type polylactic acid having a weight average molecular weight of about 50,000˜20,000 g/mol from the produced D-type lactide. The method of the present invention is advantageous in that D-type lactide can be obtained at a high yield by a simple method, compared to the conventional production methods. Consequently, production cost of D-type polylactic acid that is finally obtained from D-type lactide can be reduced. 1. A method of producing D-type lactide , comprising the steps of:(a) converting liquid D-type lactic acid into D-type polylactic acid having a weight average molecular weight of about 600˜1200 g/mol at a temperature of about 130˜150° C. and a pressure of about 10˜200 torr;(b) converting the D-type polylactic acid having a weight average molecular weight of about 600˜1200 g/mol into gas stream by heating D-type polylactic acid in the presence of a zinc oxide catalyst at a temperature of about 230˜240° C. and at a pressure of 200 torr;(c) cooling the gas stream at a temperature of about −78˜10° C. to separate unreacted lactic acid from a mixture; and(d) mixing the mixture with water to separate D-type lactide.2. The method of claim 1 , wherein the zinc oxide catalyst exists in an amount of about 0.01˜1.5% by weight claim 1 , based on D-type polylactic acid.3. The method of claim 1 , wherein a carrier gas is added and the retention time is controlled from about 5˜10 sec in step (b).4. The method of claim 3 , wherein the carrier gas includes a nitrogen gas.5. The method of claim 1 , wherein the mixture and water are mixed at a volume ratio of about 1:0.5˜5 and at a temperature of about 5˜30° C.6. The method of claim 1 , wherein the unreacted lactic acid separated in step (c) is recycled to step (a) to create a continuous cycle.7. A method of producing D-type polylactic acid having a weight average molecular weight of about 50 claim ...

Synthesis of (2S,3R,4R)-4,5-Dihydroxyisoleucine and Derivatives

The invention relates to a method for the preparation of a 4,5-dihydroxyisoleucine derivative comprising the steps of asymmetric Claisen rearrangement of a Z-aminocrotyl-glycin ester and subsequent kinetic resolution of the product diastereomer mix by acylase, and subsequent Sharpless dihydroxylation of the resulting 2-amino-3-methylpent-4-enoic acid derivative. 2. The method of claim 1 , wherein said chiral ligand is selected from ephedrin claim 1 , valinol claim 1 , cinchonidine claim 1 , quinidine and cinchonine claim 1 , particularly wherein the chiral ligand is quinidine claim 1 , particularly wherein said chiral ligand is present in 2 to 3 molar equivalents in relation to compound 200.3. The method of claim 1 , wherein the Claisen rearrangement step proceeds in the presence of a strong non-nucleophilic base soluble in non-polar organic solvents claim 1 , particularly a lithium or potassium alkylamide or lithium or potassium silylalkylamide claim 1 , more particularly a base selected from LDA claim 1 , LiTMP and LiHMDS claim 1 , even more particularly in the presence of LiHMDS.4. The method of claim 1 , wherein Rand/or Ris/are CHF(CHF)CO— wherein n is 0 or 1 claim 1 , x is selected from 0 claim 1 , 1 claim 1 , 2 and 3 and y is selected from 0 claim 1 , 1 and 2 claim 1 , particularly Rand/or Ris/are selected from CFCO— claim 1 , CHFCO— claim 1 , CHFCO— claim 1 , CFCO and CFCFCO.5. The method of claim 1 , wherein the Claisen rearrangement step proceeds in the presence of LiHMDS and Ris CFCO—.6. The method of claim 1 , wherein Ris the same as Rand the enzymatic resolution step is performed directly after the Claisen rearrangement step.11. The method according to claim 7 , wherein{'sup': '1C', 'Ris a carboxylic acid moiety protecting group cleavable under acidic conditions,'}{'sup': 1', 'X', 'Y', 'Z', 'X', 'Y', 'Z, 'sub': 1', '4', '3', '6, 'particularly Ris —C(RRR) with R, Rand Rindependently selected from Cto Calkyl, Cto Ccycloalkyl or substituted or unsubstituted ...

PHOTOLABILE ACETAL AND KETAL COMPOUNDS FOR THE CONTROLLED RELEASE OF ACTIVE VOLATILE CARBONYL COMPOUNDS

The present invention relates to a delivery system based on photosensitive acetal or ketal compounds capable of liberating upon exposure to light an active volatile carbonyl compound in a controlled manner from a surface into the surrounding. The delivery system can be used to release active substances such as flavors, fragrances, malodor counteractants, insect attractants or insect repellents. The invention also relates to the use of said acetal or ketal compounds in perfumery, as well as in perfuming compositions or perfumed consumer articles. 2. The delivery system of claim 1 , wherein at least two Rand/or at least two Rare hydrogen atoms.3. The delivery system of claim 1 , wherein all of the groups Rand R claim 1 , which are not a hydrogen atom claim 1 , represent the same group selected from the group consisting of a linear C-Calkyl group claim 1 , a branched C-Calkyl group claim 1 , a methoxy group claim 1 , an ethoxy group claim 1 , a (OCHCH)OH group claim 1 , a (OCHCH)OCHgroup claim 1 , a methylthio group claim 1 , a dimethylamino group claim 1 , and a diethylamino group with n being an integer varying between 2 and 8.4. The delivery system of claim 1 , wherein the Rand Rgroup in ortho position with respect to the bond between the aromatic ring and the oxygenated ring are hydrogen atoms.5. The delivery system of claim 14 , wherein Rand Rare a hydrogen atom claim 14 , a methoxy group or a dimethylamino group.6. The delivery system of claim 1 , wherein Rrepresents a hydrogen atom claim 1 , a linear or branched C-Calkyl group claim 1 , a methoxy group claim 1 , a dimethylamino group or a diethylamino group.7. The delivery system of claim 1 , wherein the active volatile aldehyde or ketone is a perfuming ingredient.8. The delivery system of claim 7 , wherein the release of the perfuming compounds claim 7 , is triggered by light at a wavelength above 280 claim 7 , above 300 nm claim 7 , or above 330 nm.9. A perfuming composition comprising{'claim-ref': {'@idref': ...

COMPOUNDS

The present invention relates to compounds of Formula I as defined herein, and salts and solvates thereof. (I) The present invention also relates to pharmaceutical compositions comprising compounds of Formula (I), and to compounds of Formula (I) for use in the treatment of proliferative disorders, such as cancer, as well as other diseases or conditions in which inhibition of a RAS-effector protein-protein interaction is implicated. 2. A compound according to claim 1 , or a salt or solvate thereof claim 1 , wherein X is O.3. (canceled)4. A compound according to claim 1 , or a salt or solvate thereof claim 1 , wherein M is selected from phenyl optionally substituted by one or more Rand a 5-6 membered heteroaryl optionally substituted by one or more R.5. (canceled)6. A compound according to claim 1 , or a salt or solvate thereof claim 1 , wherein M is selected from phenyl optionally substituted by one or more Rand pyridyl optionally substituted by one or more R.8. A compound according to claim 1 , or a salt or solvate thereof claim 1 , wherein Ris independently selected from hydroxyl claim 1 , ═O claim 1 , halogen claim 1 , CN claim 1 , Chaloalkyl claim 1 , Chaloalkoxy claim 1 , Calkyl claim 1 , O—Calkyl claim 1 , Ccycloalkyl claim 1 , 3-10 membered heterocycloalkyl claim 1 , —NRR claim 1 , and a group of Formula II as defined in .911-. (canceled)12. A compound according to claim 7 , or a salt or solvate thereof claim 7 , wherein Ris independently selected from ═O claim 7 , Calkyl claim 7 , O—Calkyl and —NRR.13. A compound according to claim 7 , or a salt or solvate thereof claim 7 , wherein Ris independently selected from a group of Formula II as defined in .1419-. (canceled)2122-. (canceled)23. A compound according to claim 20 , or a salt or solvate thereof claim 20 , wherein Ris hydrogen and x is 1.2430-. (canceled)31. A compound according to claim 1 , or a salt or solvate thereof claim 1 , wherein Ris selected from hydrogen claim 1 , Calkyl optionally substituted ...

METHOD FOR PRODUCING LACTIDE DIRECTLY FROM LACTIC ACID AND A CATALYST USED THEREIN

The present invention provides a method for directly producing lactide by subjecting lactic acid to a dehydration reaction in the presence of a catalyst comprising a tin compound, preferably, a tin (IV) compound, wherein lactide can be produced directly or by one step from lactic acid, without going through the step of producing or separating lactic acid oligomer. The method of the present invention has advantages of causing no loss of lactic acid, having a high conversion ratio to lactic acid and a high selectivity to optically pure lactide, and maintaining a long life time of the catalyst. Further, since lactic acid oligomer is not or hardly generated and the selectivity of meso-lactide is low, the method also has an advantage that the cost for removing or purifying this can be saved.

METHOD OF RECOVERING LACTIDE

A method of recovering lactide which includes throwing a polylactic acid and a depolymerization catalyst into an extruder () communicated with a vent chamber () maintained under a reduced pressure, melt-kneading the polylactic acid and the depolymerization catalyst together in the extruder (), feeding the melt-kneaded product thereof into the vent chamber (), depolymerizing the polylactic acid in the vent chamber (), gasifying the formed lactide and recovering the gasified lactide from the vent chamber (). 1. A method of recovering lactide comprising throwing a polylactic acid and a depolymerization catalyst into an extruder , melt-kneading the polylactic acid and the depolymerization catalyst together in said extruder , feeding said melt-kneaded product thereof from said extruder into a vent chamber maintained under a reduced pressure , depolymerizing the polylactic acid in said vent chamber , gasifying the formed lactide therein , and recovering the gasified lactide from said vent chamber.2. The method of recovering lactide according to claim 1 , wherein the polylactic acid and the polymerization catalyst are thrown into said extruder hut without throwing the carrier resin therein claim 1 , and the melt-kneaded product of said polylactic acid is fed into said vent chamber without using the carrier resin.3. The method of recovering lactide according to claim 1 , wherein a trapping apparatus is linked to said vent chamber to trap the gasified lactide.4. The method of recovering lactide according to claim 1 , wherein said vent chamber is provided at the bottom portion thereof with a discharge pipe for discharging the residue from which the gasified lactide has been removed.5. The method of recovering lactide according to claim 1 , wherein said depolymerization catalyst is thrown into said extruder on the side downstream of the polylactic acid in the direction of extrusion in the extruder.6. The method of recovering lactide according to claim 1 , wherein the ...

Method for producing glycolide

The method for producing glycolide that achieves the object described above includes: an oligomer preparation step of heating an aqueous glycolic acid solution and subjecting glycolic acid contained in the aqueous glycolic acid solution to dehydrating polycondensation, to obtain a glycolic acid oligomer; and a depolymerization step of depolymerizing the glycolic acid oligomer in the presence of ferrous ions to obtain glycolide.

Process and Apparatus for Purification of a Stream Containing a Cyclic Ester of an Alpha-Hydroxycarboxylic Acid

The invention relates to a process for purification of a stream containing a cyclic ester of an alpha-hydroxycarboxylic acid of formula (I), wherein each R independently represents hydrogen or an aliphatic hydrocarbon having 1 to 6 carbon atoms comprising the steps of: (a) separating the cyclic ester-containing stream into one or more cyclic ester-containing vapour fractions and one or more cyclic ester-containing liquid fractions; (b) condensing a cyclic ester-containing vaporized fraction as obtained in step (a) to obtain a cyclic ester-containing condensate; (c) subjecting at least part of the cyclic ester-containing condensate as obtained in step (b) to melt crystallization to obtain a purified cyclic ester-containing stream and a residue stream; and (d) recovering the purified cyclic ester-containing stream as obtained in step (c). The invention further relates to an apparatus suitable for carrying out the present process. 122-. (canceled)24. The process according to claim 23 , wherein the cyclic ester is lactide.25. The process according to claim 23 , wherein the cyclic ester-containing condensate is undercooled in step (b) 5 to 10° C. above its freezing point before it is subjected to melt crystallization in a step (c).26. The process according to claim 23 , wherein step (a) is carried out in a distillation column.27. The process according to claim 26 , wherein the cyclic ester-containing vapour fraction to be condensed in step (b) is withdrawn from the distillation column via a side draw and introduced into a condensation unit.28. The process according to claim 26 , wherein a cyclic ester-containing liquid fraction as obtained in step (a) is subjected to a first evaporation treatment to obtain a first cyclic ester-containing vapour stream and a first cyclic ester-containing liquid stream claim 26 , and wherein the cyclic ester-containing vapour fraction which is to be condensed in step (b) is at least partly derived from the first cyclic ester-containing ...

COMPOUNDS FOR USE IN IMAGING, DIAGNOSING AND/OR TREATMENT OF DISEASES OF THE CENTRAL NERVOUS SYSTEM OR OF TUMORS

This invention relates to novel compounds suitable for labelling or already labelled by F, methods of preparing such a compound, compositions comprising such compounds, kits comprising such compounds or compositions and uses of such compounds, compositions or kits for diagnostic imaging by positron emission tomography (PET). 2. (canceled)3. The compound according to claim 1 , wherein A is substituted or unsubstituted phenyl claim 1 , substituted or unsubstituted furanyl claim 1 , (C-C)alkyl claim 1 , G-(C-C) claim 1 , alkynyl claim 1 , G-(C-C)alkoxy claim 1 , (G-(C-C)alkyl)phenyl claim 1 , or (G-(C-C)alkoxy)phenyl.4. The compound according to claim 3 , wherein A substituted or unsubstituted phenyl claim 3 , substituted or unsubstituted furanyl claim 3 , (G-(C-C)alkyl)phenyl claim 3 , (G-(C-C)alkoxy)phenyl claim 3 , hydroxy-phenyl claim 3 , halo-phenyl claim 3 , methoxy-phenyl claim 3 , dimethoxy-phenyl claim 3 , trifluormethyl-phenyl claim 3 , or ((C-C)alkyl)-phenyl.5. The compound according to claim 4 , wherein A is substituted or unsubstituted phenyl claim 4 , (G-(C-C)alkoxy)phenyl claim 4 , hydroxyl-phenyl claim 4 , fluorophenyl claim 4 , methoxyphenyl claim 4 , or methylphenyl.6. The compound according to claim 1 , wherein G claim 1 , G claim 1 , Gand Gare independently and individually claim 1 , at each occurrence claim 1 , hydrogen claim 1 , (C-C)alkyl claim 1 , L claim 1 , or —(C-C)alkyl-L claim 1 ,{'sup': 1', '4, 'sub': 1', '4, 'with the proviso that exactly one of G-Gis L or —(C-C)alkyl-L.'}7. The compound according to claim 6 , wherein G claim 6 , G claim 6 , Gand Gare independently and individually claim 6 , at each occurrence claim 6 , hydrogen claim 6 , methyl claim 6 , L claim 6 , or —(C-C)alkyl-L claim 6 , with the proviso that exactly one of G-Gis L or —(C-C)alkyl-L.8. The compound according to claim 7 , wherein G claim 7 , G claim 7 , Gand Gare independently and individually claim 7 , at each occurrence claim 7 , hydrogen claim 7 , methyl claim 7 , ...

Method for Preparation of Fluoro Alkylated 1,4-Dioxene by Homogeneous NI Catallysis

The invention discloses a method for the preparation of fluoro alkylated 1,4-dioxene by homogeneous Ni catalyzed fluoro alkylation with fluoro alkyl halides of -dioxane in the presence of a base. 2. The method according to claim 1 , wherein NISALT is NiCland LIG is compound of formula (dppb).3. The method according to claim 1 , wherein BAS is selected from the group consisting of CsCO claim 1 , NaCO claim 1 , KPO claim 1 , NaH and NaOtBu.4. The method according to claim 1 , wherein FAHALIDE is selected from the group consisting of perfluoro Calkyl-X1 claim 1 , Br—(CF)—Br claim 1 , and FHC—X1;with n3 being an integer of 2 to 10.5. The method according to claim 1 , wherein n3 is 2 claim 1 , 3 claim 1 , 4 claim 1 , 5 claim 1 , 6.6. The method according to claim 1 , wherein FAHALIDE is selected from the group consisting of FC—I claim 1 , FC—Br claim 1 , FC—I claim 1 , FC—Br claim 1 , FC—I claim 1 , FC—Br claim 1 , FC—I claim 1 , FC—Br claim 1 , FC—I claim 1 , FC—Br claim 1 , FC—I claim 1 , FC—Br claim 1 , Br—(CF)—Br claim 1 , FHC—I claim 1 , and FHC—Br.7. The method according to claim 1 , wherein FAHALIDE is selected from the group consisting of FC—I claim 1 , FC—I claim 1 , FC—I claim 1 , FC—I claim 1 , FC—I claim 1 , and FC—I.8. The method according to claim 7 , wherein the reaction is done neat or in a solvent SOL.9. The method according to claim 8 , wherein SOL is selected from the group consisting of alkanes claim 8 , chlorinated alkanes claim 8 , ketones claim 8 , ethers claim 8 , esters claim 8 , aliphatic nitrils claim 8 , aliphatic amides claim 8 , sulfoxides claim 8 , CFand mixtures thereof The invention discloses a method for the preparation of fluoro alkylated 1,4-dioxene by homogeneous Ni catalyzed fluoro alkylation with fluoro alkyl halides of 1,4-dioxane in the presence of a base.I. Hanna in Tetrahedron Letters, 1999, 40, 2521-2524 discloses that furans are important functional groups that can be found in many natural products and have frequently been ...

PRODUCTION METHOD FOR CYCLOPENTANONE DERIVATIVE, INTERMEDIATE COMPOUND, AND PRODUCTION METHOD FOR INTERMEDIATE COMPOUND

The present invention is a production method for a compound represented by the following general formula (V), the method comprising a step of obtaining a compound represented by the following general formula (II) by reacting a compound represented by the following general formula (I) with an acid: 4. The production method for a cyclopentanone derivative according to claim 3 , further comprising a step of obtaining a compound represented by general formula (V) above by dehydroxymethylating a compound represented by general formula (IV) above under basic conditions.6. The production method for a cyclopentanone derivative according to claim 5 , wherein Yand Yare each independently a hydrogen atom or an alkyl group having from 1 to 4 carbons.7. The production method for a cyclopentanone derivative according to claim 5 , wherein both Yand Yare methyl groups.9. The production method for a cyclopentanone derivative according to claim 1 , wherein in general formula (V) above claim 1 , m is an integer from 0 to 3 claim 1 , and when m is 1 or greater claim 1 , X is a halogen atom claim 1 , an alkyl group having from 1 to 3 carbons claim 1 , a haloalkyl group having from 1 to 3 carbons claim 1 , an alkoxy group having from 1 to 3 carbons claim 1 , or a haloalkoxy group having from 1 to 3 carbons.10. The production method for a cyclopentanone derivative according to claim 1 , wherein in general formula (V) above claim 1 , m is an integer from 0 to 2 claim 1 , and when m is 1 or 2 claim 1 , X is a halogen atom.11. (canceled)12. (canceled)13. (canceled)14. (canceled)15. (canceled)16. (canceled) The present invention relates to a novel production method for a cyclopentanone derivative, an intermediate compound of the cyclopentanone derivative, and a production method of the intermediate compound.A certain type of 2-(halogenated hydrocarbon substituted)-5-benzyl-1-azolylmethylcyclopentanol derivative is described in Patent Document 1 as a compound that can be used as an active ...

AZOLE DERIVATIVE, METHOD FOR PRODUCING AZOLE DERIVATIVE, AND INTERMEDIATE COMPOUND

In order to provide a novel azole derivative, an azole derivative of the present invention is an azole derivative represented by a general formula (V′). (where Rand Rindependently represent a hydrogen atom, a C-Calkyl group, a phenyl group, or a benzyl group; X represents a halogen atom, a C-Calkyl group, a haloalkyl group, an alkoxy group or a haloalkoxy group, a phenyl group, a cyano group, or a nitro group; m represents an integer of 0 to 5; and A represents a nitrogen atom or a methyne group.) 7. The method as set forth in claim 2 ,{'sup': 6', '7, 'sub': 1', '4, 'wherein Rand Rindependently represent a C-Calkyl group.'}11. An agro-horticultural agent containing the azole derivative recited in as an active constituent claim 1 , the agro-horticultural agent being used in a seed treatment.12. A seed treated by the agro-horticultural agent recited in .13. The method as set forth in claim 5 ,{'sup': 6', '7, 'sub': 1', '4, 'wherein Rand Rindependently represent a C-Calkyl group.'} The present invention relates to a novel azole derivative, a method for producing the same, a method for using the same, and an intermediate compound thereof.It is known that certain kinds of 2-substituted-5-benzyl-1-azolylmethylcyclopentanol derivative show biocidal activities (e.g., see Patent Literatures 1 and 2).Further, it is reported that some compounds encompassed in 2-(halogenated alkyl hydrocarbon)-5-benzyl-1-azolylmethylcyclopentanol derivative show an anticonvulsive property and an anti-anxiety fighting activity (see Patent Literature 3). Note that Patent Literature 3 does not disclose agro-horticultural agents or industrial material protecting agents, and does not specifically disclose compounds that are encompassed in the scope of the present invention.Patent Literature 1Patent Literature 2Patent Literature 3Patent Literature 4Patent Literature 5Conventionally, an agro-horticultural pesticide having a low toxicity to humans, capable of being handled safely, and exhibiting a high ...

DERIVATIVES OF DOCOSAHEXAENOYLETHANOLAMIDE AND USES THEREOF

The invention provides derivatives of DEA which have increased potency and hydrolysis resistance as compared to DEA, and compositions thereof, as well as methods of using these derivatives to promote neurogenesis, neurite growth and/or length, and/or promote synaptogenesis. 226-. (canceled) This patent application claims the benefit of U.S. Provisional Patent Application No. 61/624,741, filed Apr. 16, 2012, which is incorporated by reference in its entirety.Docosahexanenoic acid (DHA) is an n-3 essential fatty acid that is highly enriched in the brain, and which increases neurogenesis, neurite growth, and synaptogenesis. Docosahexaenoylethanolamide (DEA, also called “synaptamide”) is a DHA derivative that also has been shown to increase hippocampal development and synaptic function. Agents capable of neurogenesis, neurite growth, and synaptogenesis are desirable for use in treating central nervous system (CNS) conditions, especially conditions such as stroke, neurodegenerative diseases, and brain injuries.Additional DHA derivatives are needed which have increased potency and stability.In an aspect, the invention provides derivatives of synaptamide which have increased potency and hydrolysis resistance as compared to synaptamide, and compositions thereof.In another aspect, the invention provides a method of promoting neurite growth and/or length, and/or promoting synaptogenesis, comprising applying to a neuron a compound having the formula CHCHHC═CHCHHC═CHCHHC═CHCHHC═CHCHHC═CHCHHC═CHCHCHCO—NRR, wherein the group NRRis as provided in Table 1 below, and measuring the growth and/or length of a neurite of the neuron, wherein neurite growth and/or length is promoted if the length/growth of the neurite is greater than the length/growth of a control neurite of an untreated neuron and synaptogenesis is promoted if the number and/or percent increase of synapsin-positive puncta is greater than that of untreated control.In yet another aspect, the invention provides a method of ...

4,6-DIFLUORODIBENZOFURAN DERIVATIVES

4,6-difluorodibenzofuran derivatives of the formula I 2. (canceled)3. A compound according to claim 1 , wherein{'sup': 1', '2, 'Rand R, independently of one another, denote an alkyl radical having 1 to 7 carbon atoms or an alkenyl radical having 2 to 7 carbon atoms.'}4. A compound according to claim 1 , wherein the sum of the number of carbon atoms in Rand Ris 5 claim 1 , 6 claim 1 , 7 claim 1 , 8 or 9.7. A compound according to claim 1 , wherein{'sup': 1', '2, 'sub': '3', 'Rand R, independently of one another, denote an alkyl radical having 2 to 6 carbon atoms or an alkenyl radical having 3 to 6 carbon atoms or CF.'}8. (canceled)9. A compound according to claim 1 , wherein m=0 and n=1.10. A Liquid-crystalline medium comprising at least two compounds claim 1 , one of which is a compound according to .11. An electro-optical display element containing a liquid-crystalline medium according to .13. A compound according to claim 1 , wherein one of Rand Ris methyl or ethyl.14. A compound according to claim 1 , which has a negative dielectric anisotropy Δ∈.15. A compound according to claim 1 , which has a negative dielectric anisotropy of Δ∈<−8.18. A compound according to claim 1 , wherein{'sup': 1', '2, 'Rand Rindependently of one another, denote an alkyl radical having 1 to 15 C atoms, each of which are optionally mono- or polyhalogenated.'}19. A compound according to claim 1 , wherein{'sup': 1', '2, 'Rand Rindependently of one another, denote an alkyl radical having 1 to 15 C atoms.'}20. A compound according to claim 1 , wherein{'sup': 1', '2', '1', '2', '1', '2, 'Rand Rone of Rand Rdenotes an alkyl radical having 1 to 15 C atoms and the other of Rand Rdenotes an alkenyl or alkynyl radical having 2 to 15 C atoms, each of which are optionally mono- or polyhalogenated.'}21. A compound according to claim 1 , wherein{'sup': 1', '2', '1', '2', '1', '2, 'Rand Rone of Rand Rdenotes an alkyl radical having 1 to 15 C atoms and the other of Rand Rdenotes an alkenyl or alkynyl ...

METHOD FOR MANUFACTURING LACTIDE

A method for producing lactide including the steps of: providing a solution of lactic acid in a volatile organic solvent, subjecting the solution to an evaporation step to remove volatile organic solvent and water, resulting in the formation of a composition including lactic acid oligomer, adding catalyst to the composition including lactic acid oligomer, and bringing the mixture to reaction conditions, to form lactide. It has been found that the process results in the efficient production of lactide with a high production rate and a good product quality. 1. Method for producing lactide comprising the steps ofproviding a solution of lactic acid in a volatile organic solvent,subjecting the solution to an evaporation step to remove volatile organic solvent and water, resulting in the formation of a composition comprising lactic acid oligomer,adding catalyst to the composition comprising lactic acid oligomer, and bringing the mixture to reaction conditions, to form lactide.2. Method according to claim 1 , wherein the concentration of lactic acid in the solution of lactic acid in a volatile organic solvent is at least 5 wt. % and generally below 40 wt. %.3. Method according to wherein the solvent is selected from the group comprising C2-C10 ketones claim 1 , C2-C10 ethers.4. Method according to claim 1 , wherein the water content of the solution of lactic acid in a volatile organic solvent is below 15 wt. %.5. Method according to claim 1 , wherein in the composition comprising lactic acid oligomer claim 1 , the lactic acid oligomers have an average degree of polymerisation of between 2 and 30.6. Method according to claim 1 , wherein the composition comprising lactic acid oligomers formed after the evaporation step comprises a residual amount of solvent in the range of 0 to 5 wt. % and or water in the range of 0 to 5 wt. %.7. Method according to claim 1 , wherein the reaction conditions during the lactide formation step include a temperature in the range of 160 to 220° C ...

METHOD OF ISOLATING INGENOL

The present invention relates to a new method for isolating ingenol (CHO) from mixtures of diterpenoid esters and ingenol esters in a single step. Ingenol isolated by means of this method can be used as a precursor for the synthesis of biologically active ingenol derivatives, such as ingenol-3-angelate and ingenol-3-tigliate. 1. A method of isolating ingenol from plant material , said method comprising:a) subjecting said plant material to mechanical stirring in a solution of sodium methylate in methanol to obtain a solution containing hydrolyzed ingenol;b) extracting from the preceding solution a fraction containing ingenol with an acidified water and an organic solvent solution to obtain a fraction contain ingenol; andc) optionally purifying the ingenol to provide an isolated ingenol.2Euphorbia lathyris. The method according to claim 1 , wherein the plant material are seeds.3. The method according to claim 1 , wherein the concentration of sodium methylate in methanol is 0.20 N and the time for which the seeds are subjected to mechanical stirring is 4 hours.4. The method according to claim 1 , further comprising filtering or suctioning on celite the solution obtained in step a).5. The method according to claim 1 , wherein the acidified water solution consists of a combination of 2N HSOand HO plus NaCl at 35% weight/volume at a ratio of 1:1.6. The method according to wherein the step of purifying ingenol is performed by means of gravity column chromatography.7. The method according to claim 6 , wherein a silica gel column is used as a stationary phase with a petroleum ether-ethyl acetate as a mobile phase.8. The method according to claim 1 , wherein the purified isolated ingenol is subjected to an additional process of partial chemical synthesis to produce a derivative at position 3 selected from: ingenol-3-tigliate claim 1 , ingenol3-angelate or mixtures thereof.9. The method according to claim 8 , wherein the additional process of partial chemical synthesis for ...

TECHNOLOGICAL METHOD FOR SYNTHESIS OF OPTICALLY PURE L-/D-LACTIDE CATALYZED BY BIOGENIC GUANIDINE

A technological method for synthesizing optically pure L-/D-lactide by using a biogenic guanidine catalysis method. The method of the present invention comprises: by using biogenic guanidine creatinine (CR) as a catalyst and L-/D-lactic acid (90% of mass content) as a raw material, synthesizing optically pure L-/D-lactide by using a reactive reduced pressure distillation catalysis method. The method of the present invention has advantages that the used catalyst is biogenic guanidine creatinine and free of toxicity, metal, and cytotoxicity; the synthesized lactide is high in optical purity (the specific rotation of the L-lactide [α]25 D=−276˜−280, and the specific rotation of the D-lactide [α]25 D=280), and does not contain any metal; the amount of the catalyst used in reaction is low, the technological process is simplified (a process for rectifying and purifying a crude lactide product by using a conventional method is avoided); and the technological method is simple and convenient to operate and easy in industrial implementation. 1. A technological method for synthesizing optically pure L-/D-lactide by using biogenic guanidine catalysis method , wherein the optically pure L-/D-lactide is synthesized through the reactive reduced pressure distillation catalysis method using biogenic guanidine compound creatinine as a catalyst and L-/D-lactic acid (90% of mass content) as a raw material , comprising the following steps:(1) Under the condition of heating temperature of 130° C.-170° C., L-/D-lactate was firstly reacted under normal pressure conditions for 1-4 h, then reacted 2-8 h under reduced pressure 30-60 torr, to produce lactic acid oligomers with the weight -average molecular weight of 600-1500 Da by dehydration and polycondensation;(2) The lactic acid oligomers synthesized in step (1) was added to catalyst creatinine to react 1-4 h with the controlled temperature at 150-260° C. and degree of vacuum at 2-15 torr, and then the distilled white crude L-/D-lactide ...

INHIBITORS OF RAS-EFFECTOR PROTEIN INTERACTIONS

The present invention relates to compounds of Formula I as defined herein, and salts and solvates thereof. (I) The present invention also relates to pharmaceutical compositions comprising compounds of Formula (I), and to compounds of Formula (I) for use in the treatment of proliferative disorders, such as cancer, as well as other diseases or conditions in which inhibition of a RAS-effector protein-protein interaction is implicated. 3. A compound according to any one of the preceding claims , or a salt or solvate thereof , wherein X is O.4. A compound according to any one of the preceding claims , or a salt or solvate thereof , wherein Ris selected from hydrogen , Calkyl and halogen , suitably hydrogen.5. A compound according to any one of the preceding claims , or a salt or solvate thereof , wherein R , R , R , and Rare hydrogen.6. A compound according to any one of the preceding claims , or a salt or solvate thereof , wherein is 1 or 2 and is 0 , suitably is 1 and is 0.7. A compound according to any one of the preceding claims , or a salt or solvate thereof , wherein Jis selected from O and NR; where Ris selected from hydrogen and Calkyl , suitably hydrogen.9. A compound according to any one of the preceding claims , or a salt or solvate thereof , wherein Ais selected from Caryl optionally substituted by one or more R , 3-15 membered heterocycloalkyl optionally substituted by one or more R , and 5-15 membered heteroaryl optionally substituted by one or more R.10. A compound according to any one of the preceding claims , or a salt or solvate thereof , wherein Ais phenyl optionally substituted by one or more R.11. A compound according to any one of the preceding claims , or a salt or solvate thereof , wherein Ris selected from hydrogen , hydroxyl , ═O , halogen , CN , Chaloalkyl , Chaloalkoxy , Calkyl , and O—Calkyl; where said Calkyl and O—Calkyl are optionally substituted with one or more groups selected from hydroxyl , halogen , ═O , CN , Chaloalkyl , Chaloalkoxy ...

Novel Cyclic Phenoxy Compounds and Improved Treatments for Cardiac and Cardiovascular Disease

A compound of formula I, and its pharmaceutically acceptable salt or salts and physiologically hydrolysable derivatives in free form or salt form: 2. A compound as claimed in which comprises an optionally substituted bicyclic heteroaromatic ring system comprising benzene ring Yfused to a heterocyclic or heteroaromatic 5 or 6 membered ring claim 1 , comprising at least one O-heteroatom and optionally including an oxo (═O) moiety claim 1 , wherein the linking atom for the ring system to the remainder of the compound is a C atom of either ring claim 1 , and wherein the ring system optionally incorporates the OCRRmoiety.87. Novel intermediates as defined in Claim .9. A composition comprising a therapeutically effective amount of a compound of formula I or subformulae or its pharmaceutically acceptable salt and physiologically hydrolysable derivative as defined in in association with one or more pharmaceutical carriers or diluents.1014.-. (canceled)15. A method of treating a condition selected from ischaemic heart disease (also known as myocardial infarction or angina) claim 1 , hypertension claim 1 , and heart failure claim 1 , restenosis and cardiomyopathy claim 1 , said method comprising administering to a subject in need thereof claim 1 , a composition comprising a compound of formula I or subformulae or pharmaceutically acceptable salt or composition thereof as defined in in an amount sufficient to treat the condition.16. The method of claim 15 , wherein the subject has concomitant respiratory disease.17. The method of claim 16 , wherein the respiratory disease is selected from asthma and COPD.18. The method claim 15 , wherein the composition further comprises one or more pharmaceutical carriers or diluents. This invention relates to novel compounds and their preparation and use in treating cardiac and cardiovascular disease.β-adrenoceptor antagonists (β-blockers) are one of the most important therapies in the management of symptoms of, and for prolonging life in, ...

FLUOROLACTONE AND METHOD FOR PRODUCING SAME

The present disclosure provides, for example, a method that can produce a fluorolactone compound from hexafluoropropylene oxide or the like in a single step. The present disclosure relates to a method for producing a compound represented by formula (1):

PROCESSES FOR PREPARING HETEROATOM CONTAINING CYCLIC DIMERS

Processes for preparing heteroatom containing cyclic dimers that result in increased production efficiency and reduced waste production. 2. The process of claim 1 , wherein R claim 1 , R claim 1 , R claim 1 , and Rare hydrogen claim 1 , and Ris C-Calkyl.3. The process of claim 1 , wherein Ris (CRR)YR claim 1 ,wherein:{'sup': 8', '9, 'Rand Rindependently are hydrogen, alkyl, or substituted alkyl;'}{'sup': '10', 'Ris hydrogen, alkyl, substituted alkyl, aryl, or substituted aryl;'}Y is sulfur, sulfone, sulfoxide, or selenium; andm is an integer from 1 to 10.4. The process of claim 3 , wherein R claim 3 , R claim 3 , R claim 3 , R claim 3 , R claim 3 , and Rare hydrogen claim 3 , and each of Rand Rindependently is C-Calkyl.5. The process of claim 4 , wherein each of Rand Ris methyl claim 4 , each of n and m is 2 claim 4 , and each of Z and Y is sulfur or selenium.7. The process of claim 1 , wherein the nonpolar solvent used in steps (a) and (d) is anisole claim 1 , benzene claim 1 , chlorobenzene claim 1 , di-tert-butyl ether claim 1 , diethylene glycol claim 1 , diglyme claim 1 , diisopropyl ether claim 1 , ethyl tert-butyl ether claim 1 , fluorobenzene claim 1 , methyl tert-butyl ether claim 1 , toluene claim 1 , xylene claim 1 , or a combination thereof.8. The process of claim 7 , wherein the nonpolar solvent is toluene.9. The process of claim 1 , wherein the weight-to-weight ratio of the nonpolar solvent to the compounds of Formula (I) and Formula (II) at step (a) is less than 10:1.10. The process of claim 9 , wherein the weight-to-weight ratio is less than 5:1.11. The process of claim 10 , wherein the weight-to-weight ratio is less than 2.5:1.12. The process of claim 11 , wherein the weight-to-weight ratio is less than 1.5:1.13. The process of claim 1 , wherein the at least one acid catalyst at step (b) is para-toluenesulfonic acid claim 1 , sulfuric acid claim 1 , hydrochloric acid claim 1 , sodium bisulfate claim 1 , ammonium bisulfate claim 1 , or a combination ...

METHOD FOR SYNTHESIZING LACTIDE BY MEANS OF CATALYSIS OF LACTID ACID

The present invention relates to a method for the catalytic synthesis of lactide from lactic acid. The method relates to the synthesis of lactide from lactic acid under the catalysis of a zinc oxide nanoparticle aqueous dispersion as a catalyst. The present invention has four technical characteristics: I. the zinc oxide nanoparticle aqueous dispersion catalyst has a sufficient surface area, and the size of nanoparticles is merely 30-40 nm, providing a sufficient contact area between the substrate (lactic acid) and the catalyst; II. the new catalyst has a milder catalytic effect on polymerization, allowing the molecular weight distribution of a prepolymer within a range of 400-1500 g/mol, which is advantageous for depolymerization to proceed; III. the new catalyst is stable, thus avoiding oxidation or carbonization in a high temperature reaction; and IV. the new catalyst has a low toxicity and a small threat to human health. 1. A method for the catalytic synthesis of lactide from lactic acid , characterized in that the synthesis of lactide from lactic acid is under the catalysis of a zinc oxide aqueous nanoparticle dispersion as a catalyst.2. The method for the catalytic synthesis of lactide from lactic acid according to claim 1 , characterized in that said zinc oxide nanoparticle aqueous dispersion is a dispersion of zinc oxide nanoparticles in water; and in said zinc oxide nanoparticle aqueous dispersion claim 1 , the particle size of the zinc oxide nanoparticles is 30-40 nm claim 1 , and the mass percentage of the zinc oxide nanoparticles is 20%.3. The method for the catalytic synthesis of lactide from lactic acid according to claim 1 , characterized in that the method comprises the following steps:{'b': '100', 'S. Dehydration: lactic acid and a catalyst are mixed at a ratio under the conditions of 60-80° C. and 60 kPa, and subjected to a dehydration reaction for 2 hours to remove free water from the lactic acid to obtain a dehydration product;'}{'b': '200', 'S. ...

AN IMPROVED PROCESS FOR DIASTEREOSELECTIVE SYNTHESIS OF VICINAL DIAMINES

The present invention relates to an improved process for diastereoselective synthesis of vicinal diamines (1). The process involves highly regio- and diastereoselective addition of 2-azaallyl anions (4) to N-tert-butanesulfinylimines (5) to produce vicinal diamines (1). 2. The process according to claim 1 , wherein solvent(s) used in step (a) and (b) is selected from an ether; alcohol; halogenated; ketone solvent; aprotic solvent such as acetonitrile claim 1 , N claim 1 ,N-dimethyl formamide (DMF) claim 1 , N claim 1 ,N-dimethyl acetamide claim 1 , dimethyl sulfoxide (DMSO) and N-methylpyrrolidone (NMP); an aromatic solvent; water or a mixture thereof.3. The process according to claim 1 , wherein in step (a) and step (b) claim 1 , the solvent is an ether solvent selected from the group consisting of tetrahydrofuran claim 1 , cyclopentyl methyl ether claim 1 , 2-methyltetrahydrofuran and diethyl ether.4. The process according to claim 1 , wherein in step (a) the base is selected from potassium hydride (KH) claim 1 , potassium tert-butoxide (tert-BuOK) claim 1 , sodium amide (NaNH) claim 1 , sodium hexamethyldisilazide (NaHMDS) or a lithium amide base.5. The process according to claim 1 , wherein in step (a) the base is a lithium amide base selected from the group consisting of lithium diethylamide claim 1 , lithium diisopropylamide (LDA) claim 1 , lithium pyrrolidinamide claim 1 , lithium piperidinamide claim 1 , lithium isopropylcyclohexylamide claim 1 , lithium tetramethylpiperidide (LiTMP) and lithium hexamethyl disilazide (LiHMDS).6. The process according to claim 1 , wherein step (a) is carried out at temperature in the range of −70° C. to −90° C. The present invention relates to an improved process for the preparation of diastereoselective synthesis of vicinal diamines of compound of formula (I).The following discussion of the prior art is intended to present the invention in an appropriate technical context, and allows its significance to be properly ...

DIOXIN DERIVATIVES, PREPARATION METHODS THEREOF, ELECTRON TRANSPORT LAYERS, OLED DEVICES AND DISPLAY PANELS

The present application provides a dioxin derivative, a preparation method thereof, an electron transport layer, an OLED device and a display panel. The dioxin derivative has a formula of 2. The dioxin derivative of claim 1 , wherein at least one of R4 claim 1 , R5 or R6 is substituted by R3.3. The dioxin derivative of claim 1 , wherein the first heteroatom is at least one of N claim 1 , O claim 1 , S or Si.4. The dioxin derivative of claim 1 , wherein the second heteroatom is at least one of N claim 1 , O or S.5. The dioxin derivative of claim 1 , wherein at least one of R4 claim 1 , R5 or R6 comprises a third heteroatom claim 1 , and the third heteroatom is at least one of N claim 1 , S or B.6. The dioxin derivative of claim 5 , wherein a first group and a second group bonded to a same third heteroatom are bonded with each other through a single bond claim 5 , or the first group and the second group are bridged with B(R3) claim 5 , C(R3) claim 5 , Si(R3) claim 5 , C═O claim 5 , C═N(R3) claim 5 , C═C(R3) claim 5 , O claim 5 , S claim 5 , S═O claim 5 , SO claim 5 , N(R3) claim 5 , P(R3) or P(═O)R3.7. The dioxin derivative of claim 6 , wherein the first group and the second group independently are phenyl claim 6 , aryl or alkyl.10. An electron transport layer claim 1 , comprising the dioxin derivative of .11. An OLED device claim 10 , comprising the electron transport layer of .12. A display panel claim 11 , comprising the OLED device of . This application claims priority to Chinese Patent Application No. 202010931127.0, titled “DIOXIN DERIVATIVES, PREPARATION METHODS AND APPLICATIONS THEREOF”, filed on Sep. 7, 2020, the contents of all of which are incorporated herein by reference.This application relates to the field of material technology, and in particular, to a dioxin derivative and a preparation method thereof, an electron transport layer, an OLED device and a display panel.OLED (Organic Light-Emitting Diode) is a display technology emerged in recent years. It ...

PRODUCTION OF MESO-LACTIDE, D-LACTIDE AND L-LACTIDE BY BACK BITING OF POLYLACTIDE

Process for increasingly producing D-Lactide and meso lactide by depolymerizing by back biting polylactide (PLA) said process which comprises: 1. Process for increasingly producing D-Lactide and meso lactide by depolymerizing by back biting polylactide (PLA) said process which comprises:{'img': [{'@id': 'CUSTOM-CHARACTER-00009', '@he': '2.46mm', '@wi': '1.78mm', '@file': 'US20180057476A1-20180301-P00001.TIF', '@alt': 'custom-character', '@img-content': 'character', '@img-format': 'tif'}, {'@id': 'CUSTOM-CHARACTER-00010', '@he': '2.46mm', '@wi': '1.78mm', '@file': 'US20180057476A1-20180301-P00002.TIF', '@alt': 'custom-character', '@img-content': 'character', '@img-format': 'tif'}, {'@id': 'CUSTOM-CHARACTER-00011', '@he': '2.46mm', '@wi': '1.78mm', '@file': 'US20180057476A1-20180301-P00001.TIF', '@alt': 'custom-character', '@img-content': 'character', '@img-format': 'tif'}, {'@id': 'CUSTOM-CHARACTER-00012', '@he': '2.46mm', '@wi': '1.78mm', '@file': 'US20180057476A1-20180301-P00002.TIF', '@alt': 'custom-character', '@img-content': 'character', '@img-format': 'tif'}], 'sub': '2', '(i) Depolymerizing polylactide into its corresponding dimeric cyclic esters by heating the polylactide in the presence of a catalyst system which comprises a catalyst and a co-catalyst, the catalyst of general formula (M)(X1, X2, . . . Xm)n wherein M of the catalyst is selected from the group consisting of Sn, Zn and Mg, and X1, X2, . . . Xm are each substituents selected from one of the classes of alkyls, aryls, oxides, carboxylates, halogenides, alkoxides as well as elements of columns 15 and/or 16 of the periodic table, m is an integer ranging from 1 to 6 and n is an integer ranging from 0 to 6 ; the co-catalyst is selected from the group comprising an organosilane aliphatic or cycloaliphatic selected from the group comprising alkylalkoxysilane or the cycloalkylalkoxysilane represented by the general formula QQ′Si(O-alkyle), where the Q and Q′ are the same or different and are alkyle or ...

AN IMPROVED ASYMMETRIC SYNTHESIS OF alpha-(DIARYLMETHYL) ALKYL AMINES

The present invention relates to an improved asymmetric synthesis of alpha-(diarylmethyl) alkyl amines (hereafter referred to as the compound (1)) or its pharmaceutically acceptable salt and derivatives. The process comprises an unusual substrate specific regioselective lithiation of alpha-diarylmethanes, followed by its highly diastereoselective addition to N-tert-butanesulfinylimines resulting in the selective formation of chiral alpha-(diarylmethyl) alkyl amines 4 and chiral amine 5; which on subsequently removing the sulfinyl group provides corresponding alpha-(diarylmethyl) alkyl amines (1) or relative chiral amines (1″). 3. The process according to claim 1 , wherein the lithiating agent used at step (a) is an organolithium compound selected from n-butyl lithium (n-BuLi) claim 1 , phenyllithium claim 1 , methyllithium claim 1 , tert-butyllithium or mixture thereof.4. The process according to claim 1 , wherein the step (b) involves the cleaving of the sulfinyl substitution of the amine by treatment of the alpha-(diarylmethyl) alkyl amine compound (4) with an acid claim 1 , such as hydrochloric acid claim 1 , hydrobromic acid claim 1 , hydrofluoric acid claim 1 , nitric acid claim 1 , sulfuric acid claim 1 , phosphoric acid or a mixture thereof.7. The process according to claim 5 , wherein the lithiating agent used at step (x) is an organolithium compound selected from n-butyl lithium (n-BuLi) claim 5 , phenyllithium claim 5 , methyllithium claim 5 , tert-butyllithium or mixture thereof.8. The process according to claim 5 , wherein the step (y) involves the cleaving of the sulfinyl substitution of the amine by treatment of the sulfinyl amine compound (5) with an acid claim 5 , such as hydrochloric acid claim 5 , hydrobromic acid claim 5 , hydrofluoric acid claim 5 , nitric acid claim 5 , sulfuric acid claim 5 , phosphoric acid or a mixture thereof. The present invention relates to an improved asymmetric synthesis of alpha-(diarylmethyl) alkyl amines (hereafter ...

METHOD FOR PREPARING REFINED LACTIDE FROM RECOVERED POLYLACTIC ACID

A method for preparing lactide from recovered polylactic acid, the method including the following steps: A. pretreating the recovered polylactic acid; B. extruding the treated polylacitc acid from a twin screw extruder to yield a polylacitc acid melt, and introducing the polylacitc acid melt to a pre-depolymerization kettle; C. carrying out a chain scission reaction to break molecular chains in the polylactic acid melt and to decrease the number-average molecular weight of the polylactic acid melt to below 5000; D. conducting depolymerization reaction to yield a crude lactide; and E. purifying the crude lactide and crystallizing the purified lactide. 1. A method for preparing a refined lactide from recovered polylactic acid , the method comprising:a) crushing recovered polylactic acid by a crusher, washing and filtrating the polylactic acid to remove impurities, and desiccating the polylactic acid to remove water;b) transporting the polylactic acid after the pretreatment to a hopper of a twin screw extruder, extruding the treated polylacitc acid from the twin screw extruder to yield a polylacitc acid melt, and introducing the polylacitc acid melt to a pre-depolymerization kettle;c) stirring the polylactic acid melt in the presence of a catalyst at a temperature of between 180 and 250° C. for carrying out a chain scission reaction to break molecular chains of the polylactic acid melt and to decrease a number-average molecular weight of the polylactic acid melt to below 5000;d) transporting the polylactic acid melt after the chain scission to a depolymerization system via a first delivery pump, and conducting depolymerization reaction at a temperature of between 150 and 250° C. and at a vacuum between 0.1 and 0.09 MPa to yield a crude lactide; ande) transporting the crude lactide to a purification system via a second delivery pump, and crystallizing the purified lactide, whereby yielding a refined lactide.2. The method of claim 1 , wherein the recovered polylactic ...

Process for Recovering and Improving Production of Meso-Lactide from a Crude Lactide Containing Stream

A process for the recovery and production of meso-lactide from a crude lactide containing stream may include subjecting a starting crude lactide stream to a first distillation step to obtain: a top stream mainly containing meso-lactide; a bottom stream; and a side stream mainly containing L-lactide and meso-lactide. The process may include recovering the side stream and subjecting the side stream to a melt crystallization step to obtain: a first purified stream mainly containing L-lactide; and a drain stream mainly containing meso-lactide and L-lactide. The process may include recovering the top stream and drain stream, and subjecting the top stream and drain stream to a second distillation step to obtain a second purified stream containing L-lactide and meso-lactide. 116-. (canceled)17. A process for the recovery and production of meso-lactide from a crude lactide containing stream , the process comprising: a top stream (B) containing meso-lactide;', 'a bottom stream (C); and', 'a side stream (D) containing L-lactide and meso-lactide;, 'subjecting a starting crude lactide stream (A) to a first distillation step to obtain a first purified stream (E) containing L-lactide; and', 'a drain stream (F) containing meso-lactide and L-lactide;, 'recovering the side stream (D) and subjecting the side stream (D) to a melt crystallization step to obtainrecovering the top stream (B) and the drain stream (F); andsubjecting the top stream (B) and the drain stream (F) to a second distillation step to obtain a second purified stream (G) containing L-lactide and meso-lactide.18. The process according to claim 17 , wherein the first distillation step is carried out in a distillation column.19. The process according to claim 17 , wherein the first distillation of step is carried out at a temperature of from 80 to 180° C. and a pressure of from 3 to 50 mbara.20. The process according to claim 17 , wherein the side stream (D) is subjected to a melt crystallization step operated in the ...

METHODS OF USING PYRUVATE KINASE ACTIVATORS

Described herein are compounds that activate pyruvate kinase, for use in a method for increasing lifetime of the red blood cells, for regulating 2,3-diphosphoglycerate levels in blood and for treating sickle cell anemia. 2. The method of claim 1 , wherein the compound is added directly to whole blood or packed cells extracorporeally.3. The method of claim 1 , wherein the pharmaceutical composition is administered to a patient in need thereof.7. The method of claim 1 , wherein Rand Rare phenyl substituted with one or more substituents selected from the group consisting of C-Calkyl claim 1 , C-Ctrihaloalkyl claim 1 , heterocyclyl claim 1 , heteroaryl claim 1 , alkylenedioxy claim 1 , OR claim 1 , SR claim 1 , NRR claim 1 , NCOR claim 1 , OCOR claim 1 , SCOR claim 1 , SOR claim 1 , SOR claim 1 , SONRR claim 1 , NO claim 1 , B(OH) claim 1 , CN claim 1 , and halogen claim 1 ,{'sup': 3', '4, 'sub': 1', '10, 'Rand Rare independently selected from the group consisting of H, C-Calkyl, and F, or, taken together, form C═O, and'}{'sup': 5', '7', '10, 'sub': 1', '10, 'Rand Rto Rare independently H, C-Calkyl, or F.'}8. The method of claim 1 , wherein Rand Rare phenyl substituted with one or more substituents selected from the group consisting of C-Calkyl claim 1 , C-Ctrihaloalkyl claim 1 , heterocyclyl claim 1 , heteroaryl claim 1 , alkylenedioxy claim 1 , CN claim 1 , and halogen claim 1 , and Rto Rare H.9. The method of claim 1 , wherein X is N.10. The method of claim 1 , wherein n is 1.11. The method of claim 1 , wherein Ris selected from the group consisting of phenyl claim 1 , 4-methylphenyl claim 1 , 2-methylphenyl claim 1 , 2-fluorophenyl claim 1 , 4-chlorophenyl claim 1 , 4-fluorophenyl claim 1 , 4 claim 1 ,2-difluorophenyl claim 1 , 2 claim 1 ,6-difluorophenyl claim 1 , 2 claim 1 ,4 claim 1 ,5-trifluorophenyl claim 1 , 4-chloro-2-fluorophenyl claim 1 , 3-chloro-2-fluorophenyl claim 1 , 4-trifluoromethylphenyl claim 1 , 3-trifluoromethylphenyl claim 1 , 2 claim 1 ,6- ...

Low-Toxicity Olefinic Ester Compositions and Methods of Using the Same

Compositions including certain olefinic ester compounds are generally disclosed. In some embodiments, such compositions are compositions having low toxicity, such as low aquatic toxicity. Therefore, in some embodiments, such compositions can be suitable used as solvents or as part of a solvent system for applications where low toxicity is desirable. Such uses include, but are not limited to, cleaning applications on or near waterways, use in oil or gas recovery, and the like. In some other embodiments, such compositions are treatment fluids for oil wells, and can therefore be introduced into an oil well to remove buildup and other deposits. In some embodiments, the olefinic ester compounds are derived from a natural oil or a natural oil derivative. 2. The compound of claim 1 , wherein Ris Calkenyl claim 1 , which is optionally substituted.3. The compound of claim 1 , wherein Ris —(CH)—CH═CH—CH.3. (canceled)4. The compound of claim 1 , wherein Ris —(CH)—CH═CH—CH—CH═CH claim 1 , —(CH)—CH═CH—CH—CH—CH claim 1 , or —(CH)—CH═CH.5. The compound of claim 4 , wherein Ris —(CH)—CH═CH—CH—CH═CH.6. The compound of claim 1 , wherein Ris —(CH)—CH═CH—CH—CH═CH—CH claim 1 , —(CH)—CH═CH—CH—CH—CH—CH claim 1 , or —(CH)—CH═CH—CH.7. The compound of claim 6 , wherein Ris —(CH)—CH═CH—CH—CH═CH—CH.8. The compound of claim 1 , wherein Ris —(CH)—CH═CH—CH—CH═CH—CH—CH claim 1 , —(CH)—CH═CH—(CH)—CH claim 1 , or —(CH)—CH═CH—CH—CH.9. The compound of claim 8 , wherein Ris —(CH)—CH═CH—CH—CH═CH—CH—CH.10. The compound of claim 1 , wherein Ris -G-R.11. The compound of claim 1 , wherein Ris R.12. (canceled)13. The compound of claim 10 , wherein Gis —CH— or —CH—CH.14. (canceled)15. (canceled)16. The compound of claim 11 , wherein Ris Ccycloalkyl claim 11 , which is optionally substituted.17. (canceled)18. (canceled)19. The compound of claim 16 , wherein Ris cyclopentyl claim 16 , cyclohexyl claim 16 , norbornyl claim 16 , or adamantyl.20. The compound of claim 19 , wherein Ris cyclohexyl.21. The compound ...

FACILE AND SELECTIVE PERFLUORO-AND POLYFLUOROARYLATION OF MELDRUMS ACID

This disclosure relates generally to the facile and selective mono-perfluoro and polyfluoroarylation of Meldrum's acid to generate a versatile synthon for highly fluorinated alpha-phenyl acetic acid derivatives which provide straightforward access to fluorinated building blocks. The reaction takes place quickly and all products were isolated without the need for chromatography. An embodiment provides an alternative strategy to access alpha-arylated Meldrum's acids which avoids the need for aryl-Pb(IV) salts or diaryliodonium salts and provides access to the tertiary product which was not previously synthetically accessible. The synthetic versatility and utility of the Meldrum's acid products is demonstrated by subjecting the products to several derivatizations of the Meldrum's acid products as well as photocatalytic hydrodefluorination which provide access to difficult but valuable synthetic targets such as multifluorinated aromatics. 1. A process for the substitution of Meldrum's acid , said process comprising reacting fluoroarene compounds of the general formula ,{'br': None, 'ArFn'}whereAr is a mono aromatic radical;F is fluorine;n is ≧1;with Meldrum's acid.2. The process of wherein said Meldrum's acid comprises any analog varied at the O claim 1 ,O-carbon.3. The process of claim 2 , wherein said Meldrum's acid analog is selected from a group consisting of at least one alkyl group claim 2 , at least one cyclic alkyl group claim 2 , and at least one aryl group.4. The process of wherein said Meldrum's acid is unsubstituted.5. The process of wherein said Meldrum's acid is 1 claim 1 ,5-dioxaspiro[5.5]undecane-2 claim 1 ,4-dione.6. The process of wherein ArFn is pentafluoropyridine.7. The process of wherein said ArFn is selected from the group consisting of perfluoroarenes and polyfluoroarenes.8. The process of wherein n is 1≦n≦5.9. The process of wherein said fluoroarene contains an activating functional group.10. The process of wherein said fluoroarene contains an ...

3-SUBSTITUTED PHENYLAMIDINE COMPOUNDS, PREPARATION AND USE THEREOF

The present invention disclosed 3-substituted phenylamidine compounds of general formula (I), wherein R, R, R, R, R, R, A and E have the same meanings as defined in description. The present invention further discloses methods for their preparation and use of the compounds of general formula (I) as a crop protection agent. 2. The compound of formula (I) as claimed in claim 1 , wherein{'sup': '1', 'sub': 1', '6', '2', '6', '2', '6', '1', '6', '1', '6', '3', '5', '4', '8, 'Ris selected from the group consisting of C-C-alkyl, C-C-alkenyl, C-C-alkynyl, C-C-haloalkyl, C-C-alkoxy, C-C-cycloalkyl and C-C-cycloalkylalkyl;'}{'sup': '2', 'sub': 1', '6', '2', '6', '2', '6', '3', '8', '1', '6, 'Ris selected from the group consisting of C-C-alkyl, C-C-alkenyl, C-C-alkynyl, C-C-cycloalkyl and C-C-haloalkyl;'}{'sup': 3', '4, 'sub': 1', '6', '2', '6', '2', '6', '1', '6', 'n', '3', '8, 'Rand Rare independently selected from the group consisting of X, cyano, C-C-alkyl, C-C-alkenyl, C-C-alkynyl, C-C-haloalkyl, N(R′R′″), OR″, S(O)R′″, (C═O)—R″ and C-C-cycloalkyl;'}{'sup': '5', 'sub': 1', '6', '2', '6', '2', '6', '1', '6', '3', '8, 'Ris selected from the group consisting of hydrogen, C-C-alkyl, C-C-alkenyl, C-C-alkynyl, C-C-haloalkyl, C-C-cycloalkyl and OR′;'}{'sup': 6', '7, 'sub': 1', '4', '2', '4', '2', '4', '1', '4', '3', '4', 'm, 'Rand Rare independently selected from the group consisting of hydrogen, X, cyano, C-C-alkyl, C-C-alkenyl, C-C-alkynyl, C-C-haloalkyl and C-C-cycloalkyl; wherein one or more carbon atoms in cycloalkyl ring may be replaced by heteroatoms selected from the group consisting of N, O, S(O)and optionally including 1 to 3 ring members selected from the group consisting of C(═O) or C(═S);'}{'sub': 3', '10', '5', '10, 'sup': '8', 'ring E is selected from the group consisting of fused or non-fused C-C-carbocyclyl and C-C-heterocyclyl, which may optionally be substituted by one or more groups of R;'}or agriculturally acceptable salts, isomers/structural isomers, stereo ...

METHOD FOR PREPARING 3-SUBSTITUTED 2-VINYLPHENYL SULFONATES

The present invention relates to a method for preparing 3-substituted 2-vinylphenyl sulfonates. 2. Method according to claim 1 , wherein a) and b) are carried out in a one-pot process.3. Method according to claim 1 , wherein one or more bases selected from the group consisting of trialkylamines claim 1 , pyridyl bases claim 1 , alkoxide bases and amidine bases is used in (a) and (b).4. Method according to claim 3 , wherein the base used is tributylamine.5. Method according to claim 1 , wherein one or more solvents are used in (a) and (b) selected from the group consisting of petroleum ether claim 1 , n-hexane claim 1 , n-heptane claim 1 , cyclohexane claim 1 , methylcyclohexane claim 1 , toluene claim 1 , o-xylene claim 1 , m-xylene claim 1 , p-xylene claim 1 , decaline claim 1 , chlorobenzene claim 1 , 1 claim 1 ,2-dichlorobenzene claim 1 , dichloromethane claim 1 , chloroform claim 1 , tetrachloromethane claim 1 , dichloroethane claim 1 , trichloroethane claim 1 , diethyl ether claim 1 , diisopropyl ether claim 1 , methyl tert-butyl ether claim 1 , methyl tert-amyl ether claim 1 , 1 claim 1 ,4-dioxane claim 1 , tetrahydrofuran claim 1 , 2-methyltetrahydrofuran claim 1 , 1 claim 1 ,2-dimethoxyethane claim 1 , 1 claim 1 ,2-diethoxyethane claim 1 , diglyme claim 1 , anisole claim 1 , acetonitrile claim 1 , propionitrile claim 1 , n-butyronitrile claim 1 , isobutyronitrile claim 1 , benzonitrile claim 1 , ethyl acetate claim 1 , N claim 1 ,N-dimethylformamide claim 1 , N claim 1 ,N-dimethylacetamide claim 1 , dimethylsulfoxide.6. Method according to claim 1 , wherein the solvent used is toluene or methyl tert-butyl ether.7. Method according to claim 1 , wherein{'sup': '1', 'Ris methyl, ethyl, n-propyl, isopropyl, n-butyl, phenyl, 4-methylphenyl or benzyl,'}{'sup': '2', 'Ris Cl, F, Br, I or methyl, and'}{'sup': 3', '1, 'sub': '2', 'Ris F, Cl or OSOR.'}9. Method according to claim 8 , wherein a deprotonating agent is first added to the compound of the formula (IV) ...

RESORCYLIC ACID LACTONE COMPOUNDS

Disclosed are a novel resorcyclic acid lactone compound with inhibitory activity against protein kinases, a pharmaceutically acceptable salt thereof, a method for the synthesis thereof, and a pharmaceutical composition for the treatment and prevention of various cancer diseases comprising the same as an active ingredient. The novel resorcyclic acid lactone compound is useful as a therapeutic for cancer diseases, especially blood cancer, inter alia, acute myeloid leukemia (AML). 2. The compound of claim 1 , being in an optically pure form or as a racemate.3. The compound of claim 2 , wherein Ris C1˜C10 alkyl claim 2 , and Rand Rare each a hydrogen atom.4. The compound of claim 3 , being (7S claim 3 ,12S claim 3 ,13R claim 3 ,Z)-4 claim 3 ,12 claim 3 ,13-trihydroxy-2-methoxy-7-methyl-7 claim 3 ,8 claim 3 ,13 claim 3 ,14-tetrahydro-5H-dibenzo[c claim 3 ,e][1]oxacyclotetradecen-5 claim 3 ,11(12H)-dione.5. An anti-cancer composition comprising the compound defined in .6. The anti-cancer composition of claim 5 , having inhibitory activity against a kinase selected from the group consisting of FLT3 (D835Y) claim 5 , FLT3 (ITD) claim 5 , FLT3 claim 5 , FLT1/VEGFR1 claim 5 , FLT4/VEGFR3 claim 5 , PDGFRa claim 5 , PDGFRb claim 5 , PDGFRa (D842V) claim 5 , PDGFRa (T674I) claim 5 , and PDGFRa (V561 D).7. The anti-cancer composition of for use in treatment and prevention of blood cancer.8. The anti-cancer composition of claim 7 , wherein the blood cancer is acute myeloid leukemia (AML).10. An intermediate compound for use in synthesis of the resorcyclic acid lactone compound of claim 1 , selected from the group consisting of:5-(3-(hydroxymethyl)phenyl)-7-methoxy-2,2-dimethyl-4H-benzo[d][1,3]dioxin-4-one);3-(7-methoxy-2,2-dimethyl-4-oxo-4H-benzo[d][1,3]dioxin-5-yl)benzaldehyde;(E)-methyl 3-(3-(7-methoxy-2,2-dimethyl-4-oxo-4H-benzo[d][1,3]dioxin-5-yl)phenyl)acrylate;(2S,3R)-methyl 2,3-dihydroxy-3-(3-(7-methoxy-2,2-dimethyl-4-oxo-4H-benzo[d][1,3]dioxin-5-yl)phenyl)propanoate;(4S,5R ...

NON-AQUEOUS ELECTROLYTE AND NON-AQUEOUS ELECTROLYTE SECONDARY BATTERY

A non-aqueous electrolyte includes a lithium salt, and a non-aqueous solvent dissolving the lithium salt. The non-aqueous solvent contains a fluorinated cyclic carbonic acid ester, a carboxylic anhydride A having a structure represented by a general formula (1) below, and a carboxylic anhydride B having a structure represented by a general formula (2) below. (In the general formula (1), n represents 0 or 1, and Rto Reach independently represent a hydrogen atom, an alkyl group, an alkenyl group, or an aryl group.) (In the general formula (2), Rto Reach independently represent a hydrogen atom, an alkyl group, an alkenyl group, or an aryl group.) 2. The non-aqueous electrolyte of claim 1 , wherein an amount of the fluorinated cyclic carbonic acid ester in the non-aqueous solvent is 0.1 to 50 vol %.3. The non-aqueous electrolyte of claim 1 , wherein an amount of the carboxylic anhydride A in the non-aqueous electrolyte is 0.1 to 2.0 mass %.4. The non-aqueous electrolyte of claim 1 , wherein an amount of the carboxylic anhydride B in the non-aqueous electrolyte is 0.1 to 2.0 mass %.5. The non-aqueous electrolyte of claim 1 , wherein the amount of the carboxylic anhydride B in the non-aqueous electrolyte is greater than the amount of the carboxylic anhydride A in the non-aqueous electrolyte.6. The non-aqueous electrolyte of claim 1 , wherein the amount of the carboxylic anhydride A in the non-aqueous electrolyte is greater than the amount of the carboxylic anhydride B in the non-aqueous electrolyte.7. The non-aqueous electrolyte of claim 1 , wherein the carboxylic anhydride A includes at least one selected from the group consisting of succinic anhydride and glutaric anhydride.8. The non-aqueous electrolyte of claim 1 , wherein the carboxylic anhydride B includes at least one selected from the group consisting of diglycolic anhydride claim 1 , methyldiglycolic anhydride claim 1 , dimethyldiglycolic anhydride claim 1 , ethyldiglycolic anhydride claim 1 , methoxydiglycolic ...

GLYCOLIDE PRODUCTION METHOD

The object of the present invention is to provide a glycolide production method capable of sufficiently increasing the production rate of glycolide. The glycolide production method according to the present invention includes: adding metal titanium to an aqueous glycolic acid solution; subjecting glycolic acid contained in the aqueous glycolic acid solution to which the metal titanium is added, to dehydrating polycondensation to obtain a glycolic acid oligomer; and heating and depolymerizing the glycolic acid oligomer to obtain glycolide. 1. A glycolide production method comprising:adding metal titanium to an aqueous glycolic acid solution;subjecting glycolic acid contained in the aqueous glycolic acid solution to which the metal titanium is added, to dehydrating polycondensation to obtain a glycolic acid oligomer; andheating and depolymerizing the glycolic acid oligomer to obtain glycolide; wherein the metal titanium is a titanium powder.2. The glycolide production method according to claim 1 , wherein an addition amount of the metal titanium is from 1 ppm to 10000 ppm relative to a total mass of the glycolic acid.3. (canceled)4. The glycolide production method according to claim 1 , wherein an average particle size of the titanium powder is equal to or less than 100 μm.5. The glycolide production method according to claim 1 , wherein a dehydrating polycondensation temperature is from 50° C. to 300° C.6. The glycolide production method according to claim 1 , wherein the depolymerization is performed in an organic solvent.7. The glycolide production method according to claim 6 , wherein the organic solvent comprises a polyalkylene glycol ether represented by Formula (1) below:{'br': None, '[Chemical Formula 1]'}{'br': None, 'i': 'p', 'X—O—(—R—O—)—Y\u2003\u2003(1)'}where R denotes a methylene group or a linear or branched alkylene group having from 2 to 8 carbons,X and Y each independently denote an alkyl group or an aryl group having from 2 to 20 carbons,p is an ...

Cyclic Acetals and Ketals and Use Thereof as Fragrance

The present invention relates to compounds of the formula (I) and use thereof as fragrance. In a further aspect the present invention relates to compositions and fragrance mixtures containing compounds of the formula (I) and the products perfumed with these compositions and fragrance mixtures. 5. A composition comprising(i) one or more 3,6,8,8-tetramethyl-octahydro-3a,7-methano-azulen-5,6-diol ketal(s), and{'claim-ref': {'@idref': 'CLM-00001', 'claim 1'}, '(ii) one or more compound(s) of the formula (I) as claimed in , wherein'}the total content of the compounds of the formula (I) is greater than 40 wt. %, preferably greater than 55 wt. %, preferably greater than 70 wt. %, more preferably greater than 85 wt. %, and especially preferably greater than 95 wt. %, based on the total quantity of the 3,6,8,8-tetramethyl-octahydro-3a,7-methano-azulen-5,6-diol ketals contained in the composition.6. A method for intensifying an odor claim 1 , comprising using a compound as claimed in as afragrance or fragrance mixture, preferably as a fragrance or fragrance mixture with the fragrance notes ambergris and/or wood,means for increasing substantivity and/or retention of a fragrance mixture, orfixative.7. A fragrance mixture claim 1 , preferably perfume oil claim 1 , comprising{'claim-ref': {'@idref': 'CLM-00001', 'claim 1'}, 'one or more compound(s) of the formula (I) as claimed in and'}one or more (further) fragrance(s) not corresponding to the formula (I), wherein(i) the quantity of the compound(s) of the formula (I) suffices to procure an ambergris note and/or wood note, in particular a white ambergris note (“white amber”), and/or(ii) the (further) fragrance(s) not corresponding to the formula (I) procure one, several or all of the notes fruity, floral, spicy, woody, musk and ambrette and the quantity of the compound(s) of the formula (I) suffices to modify and/or to intensify one, several or all of the notes fruity, floral, spicy, woody, musk and ambrette, and/or(iii) the ...

AMINO, AMIDO AND HETEROCYCLIC COMPOUNDS AS MODULATORS OF RAGE ACTIVITY AND USES THEREOF

Amino, amido, and heterocyclic compounds are disclosed. The compounds may be prepared as pharmaceutical compositions, and may be used for the prevention and treatment of a variety of conditions in mammals including humans, including by way of non-limiting example, diabetes complications, inflammation, and neurodegeneration, obesity, cancer, ischemia/reperfusion injury, cardiovascular disease and other diseases related to RAGE activity. 3. (canceled)4. (canceled)5. (canceled)6. (canceled)7. (canceled)8. (canceled)9. (canceled)10. (canceled)11. (canceled)12. (canceled)13. (canceled)14. (canceled)15. (canceled)16. (canceled)17. (canceled)18. (canceled)19. (canceled)20. (canceled)21. (canceled)22. (canceled)23. (canceled)24. (canceled)25. (canceled)26. (canceled)30. (canceled)31. (canceled)32. (canceled)33. (canceled)34. (canceled)35. (canceled)36. (canceled)37. (canceled)38. (canceled)39. (canceled)40. (canceled)41. (canceled)42. (canceled)44. The method according to claim 1 , wherein the compound is according to formula A-XIVa claim 1 , A-XIVb claim 1 , A-XIVc claim 1 , A-XIVd claim 1 , A-XV claim 1 , A-XVIb claim 1 , or A-XXa.47. (canceled)48. (canceled)49. (canceled)50. (canceled)51. (canceled)52. (canceled)53. (canceled)54. (canceled)55. (canceled)57. (canceled)58. (canceled)59. (canceled)60. (canceled)61. (canceled)62. (canceled)63. (canceled)64. (canceled)65. (canceled)66. (canceled)68. (canceled)69. (canceled)70. (canceled)71. (canceled)72. (canceled)74. (canceled)75. (canceled)76. (canceled)77. (canceled)78. (canceled)79. (canceled)80. (canceled)81. (canceled)82. (canceled)84. (canceled)85. The method according to claim 45 , wherein Ris OH claim 45 , alkoxy claim 45 , or acyloxy.86. (canceled)87. The method according to claim 45 , wherein Ris substituted or unsubstituted alkyl.88. (canceled)89. The method according to claim 45 , wherein Ris substituted or unsubstituted aryl.90. (canceled)91. (canceled)92. The method according to claim 45 , wherein m is 1; and n ...

PROCESS FOR MAKING N-SULFINYL a-AMINO AMIDES

Disclosed is a process for making diastereomeric N-sulfinyl α-amino amides by reaction of chiral sulfinimines with formamides and lithium diisopropylamide. The process of the invention provides the N-sulfinyl α-amino amides in high yields and with high diastereoselectivity.

CYCLIC POLY L-LACTIC ACID

A cyclic poly L-lactic acid composition having a pH of 6 to 7 by the polymer itself. 1. A cyclic poly L-lactic acid composition having a pH of 6 to 7 by the polymer itself.2. The cyclic poly L-lactic acid composition according to claim 1 , wherein the cyclic poly L-lactic acid has a cyclic polymerization degree (n) of 5 to 30.3. The cyclic poly L-lactic acid composition according to claim 2 , wherein the cyclic poly L-lactic acid having the cyclic polymerization degree (n) of 5 to 10 shows an ionic strength of 50% or more.4. The cyclic poly L-lactic acid composition according to claim 2 , further comprising a chain poly L-lactic acid having a chain polymerization degree (n) of 2 to 30.5. A cyclic poly L-lactic acid composition having a pH of 6 to 7 by the polymer itself claim 2 , wherein molecules having a polymerization degree (n) of 5 to 10 show an ionic strength of 50% or more claim 2 , and molecules having a polymerization degree (n) of 11 to 30 are further comprised.6. A pharmaceutical product in which the cyclic poly L-lactic acid composition according to is compounded.7. A pharmaceutical product in which the cyclic poly L-lactic acid composition according to is compounded.8. A pharmaceutical product in which the cyclic poly L-lactic acid composition according to is compounded.9. A pharmaceutical product in which the cyclic poly L-lactic acid composition according to is compounded.10. A pharmaceutical product in which the cyclic poly L-lactic acid composition according to is compounded. The present invention relates to a cyclic poly L-lactic acid (composition) having a specific pH by the polymer itself (alone), a method for producing the same, a pharmaceutical product containing the cyclic poly L-lactic acid (composition), and the like.L-lactic acid is one of the products of glycolysis in vivo. When rapid exercise is performed, sugar is decomposed as an energy source in muscle cells to produce lactic acid via pyruvic acid. Microorganisms that synthesize L- ...

Arthropod controlling composition

Described herein are an arthropod controlling composition including a compound according to a formula (I), methods, and uses to control arthropods as well as arthropod controlling articles including the same.

METHOD OF PREPARING INTERMEDIATE OF SALMETEROL

A method of preparing an intermediate of salmeterol (Compound 1, 2-amino-1-(2,2-dimethyl-4H-1,3-benzodioxin-6-yl)ethanol) includes: reacting compound 2 with 2-methoxypropene in a first organic solvent to produce a reaction solution including compound 3, compound 2 including a 2-bromo precursor of Compound 1; reacting compound 3 with a nitrogen source to produce compound 4; reacting compound 4 with sodium borohydride in a second organic solvent to produce compound 5; and debenzylating compound 5 by ammonium formate/palladium-carbon catalytic transfer hydrogenation in a third organic solvent to produce Compound 1. A method of preparing salmeterol includes preparing Compound 1, and reacting Compound 1 to prepare salmeterol. 1. A method of preparing Compound 1 , 2-amino-1-(2 ,2-dimethyl-4H-1 ,3-benzodioxin-6-yl)ethanol , the method comprising:reacting compound 2 with 2-methoxypropene in a first organic solvent to produce a reaction solution comprising compound 3, compound 2 comprising a 2-bromo precursor of Compound 1;reacting compound 3 with a nitrogen source in the reaction solution to produce compound 4;reacting compound 4 with sodium borohydride in a second organic solvent to produce compound 5; anddebenzylating compound 5 by ammonium formate/palladium-carbon catalytic transfer hydrogenation in a third organic solvent to produce Compound 1.2. The method of claim 1 , wherein the first organic solvent comprises tetrahydrofuran claim 1 , dichloromethane claim 1 , acetic ether claim 1 , methyl tert-butyl ether claim 1 , chloroform claim 1 , methyl acetate claim 1 , or a mixture thereof.3. The method of claim 1 , wherein the first organic solvent comprises tetrahydrofuran.4. The method of claim 1 , wherein the reacting of compound 2 with 2-methoxypropene is conducted in the presence of a catalyst.5. The method of claim 4 , wherein the catalyst comprises p-Toluenesulfonic acid.6. The method of claim 1 , wherein the nitrogen source comprises α-phenylethylamine.7. The ...

CATIONIC POLYGLYCERYL COMPOSITIONS AND COMPOUNDS

Provided are polyglyceryl compositions comprising one or more polyglyceryl compounds having: (a) a node structure comprising at least three contiguous glyceryl remnant units; (b) one or more cationic groups each linked to the node structure by an independently selected linking group; and (c) one or more hydrophobic moieties each independently (i) linked to the node structure by a linking group, or (ii) constituting a portion of one of the one or more cationic groups, wherein the composition has an average degree of polymerization determined by hydroxyl value testing (DP) of from about 3 to about 20. Also provided are polyglyceryl compounds which may compose such compositions, and uses of the polyglyceryl compositions and compounds. 120-. (canceled)22. The composition of wherein the one or more compounds have a DPof from about 3 to about 20.23. The composition of wherein the one or more compounds have a DPof from about 5 to about 10.24. The composition of wherein the one or more compounds have a DPof about 10.25. The composition of wherein the one or more compounds have an average degree of substitution c of cationic groups of greater than zero to less than five.26. The composition of wherein the one or more compounds have an average degree of substitution c of cationic groups of greater than zero to about three.27. The composition of wherein the one or more compounds have an average degree of substitution b of cationic-hydrophobic groups of greater than zero to less than five.28. The composition of wherein the one or more compounds have an average degree of substitution b of cationic-hydrophobic groups of greater than 0.5 to less than 3.29. A personal care composition comprising:a solvent,{'claim-ref': {'@idref': 'CLM-00021', 'claim 21'}, 'a composition of , and'}at least one material selected from the group consisting of surfactants, chelating agents, emollients, humectants, conditioners, preservatives, opacifiers, fragrances, and combinations of two or more ...

CATIONIC POLYGLYCERYL COMPOSITIONS AND COMPOUNDS

Provided are polyglyceryl compositions comprising one or more polyglyceryl compounds having: (a) a node structure comprising at least three contiguous glyceryl remnant units; (b) one or more cationic groups each linked to the node structure by an independently selected linking group; and (c) one or more hydrophobic moieties each independently (i) linked to the node structure by a linking group, or (ii) constituting a portion of one of the one or more cationic groups, wherein the composition has an average degree of polymerization determined by hydroxyl value testing (DP) of from about 3 to about 20. Also provided are polyglyceryl compounds which may compose such compositions, and uses of the polyglyceryl compositions and compounds. 120.-. (canceled)22. The composition of wherein the one or more compounds have a DPof from about 3 to about 20.23. The composition of wherein the one or more compounds have a DPof from about 5 to about 10.24. The composition of wherein the one or more compounds have a DPof about 10.25. The composition of having an average degree of substitution a of hydrophobic groups of greater than zero to less than one.26. The composition of having an average degree of substitution c of cationic groups of equal to or greater than zero to less than five.27. The composition of having an average degree of substitution c of cationic groups of equal to or greater than zero to about 3.28. The composition of having an average degree of substitution b of cationic-hydrophobic groups of equal to or greater than zero to less than five.29. The composition of having an average degree of substitution b of cationic-hydrophobic groups of equal to or greater than 0.5 to less than 3.30. A personal care composition comprising:a solvent,{'claim-ref': {'@idref': 'CLM-00021', 'claim 21'}, 'a composition of , and'}at least one material selected from the group consisting of surfactants, chelating agents, emollients, humectants, conditioners, preservatives, opacifiers, ...

Methods for making and using novel semi-synthetic small molecules for the treatment parasitic disease

Small molecule therapeutics for the treatment of parasitic diseases, in particular, semi-synthetic derivatives of the fugally-derived natural product merulin A for the treatment of African Sleeping Sickness. 4. The method of wherein the compound demonstrates endoperoxide activity.5. The method of wherein the compound demonstrates an IC50 of 56 nM claim 1 , a selectivity index greater than 250-fold.6. The method of wherein the compound demonstrates a half-life greater than 12 hours.'8. The method of claim 7 , wherein the disease is African Sleeping Sickness claim 7 , The present invention is a divisional application of and claims the benefit of and priority to U.S. application Ser. No. 14/236,030 filed 29 Jan. 2014 titled “Novel semi-synthetic small molecules for the treatment parasitic disease” which application is incorporated by reference for all purposes. U.S. application Ser. No. 14/236,030 itself claims the benefit of and priority to U.S. application No. 61/513,027 filed 29 Jul. 2011 which application is incorporated by reference for all purposes.This work was sponsored by US government grant NIH 1R56AI08517701A1 (RGL), the Government has certain rights in the inventionSmall molecule therapeutics for the treatment of parasitic diseases, in particular, semi-synthetic derivatives of the fugally-derived natural compound Merulin A for the treatment of African Sleeping Sickness.1. BackgroundHuman African Trypanosomiasis (HAT) is transmitted by the tsetse fly vector, and , and if untreated, is lethal. Current treatments are poor. In particular, the side effects for the treatment of the second stage infection (CNS infection) are very serious. There is therefore an unmet need for the development of new approaches to the development of endoperoxide-containing compounds as lead compounds for HAT.The invention encompasses semi-synthetic derivatizations of the fungally-derived natural product, Merulin.Semi-synthetic derivatization of the fungally-derived natural product ...

METHOD AND APPARATUS FOR PREPARATION OF LACTIDE USING LACTIDE PURIFICATION PROCESS

The present invention relates to a method and apparatus for preparation of lactide using a lactide purification process, comprising introducing an aqueous solution comprising lactic acid into a reactor filled with a catalyst and reacting the same to produce crude lactide vapor; and purifying the crude lactide vapor to produce lactide crystals, wherein a first purification comprises collecting and crystallizing the crude lactide vapor using a first solvent to produce lactide crystals, and separating the lactide crystal from a residue through filtration. 1. A method for preparing lactide comprising:(i) introducing an aqueous solution comprising lactic acid into a reactor filled with a catalyst and reacting the same to produce crude lactide vapor; and(ii) purifying the crude lactide vapor produced in the step (i) to produce lactide crystals, wherein the step (ii) comprises:(ii-a) collecting and crystallizing the crude lactide vapor using a first solvent to produce lactide crystals, and (ii-b) separating the lactide crystals from a residue through filtration.2. The method of claim 1 , wherein the first solvent is at least one selected from the group consisting of ethanol claim 1 , propanol claim 1 , and butanol.3. The method of claim 1 , wherein the first solvent cools claim 1 , collects claim 1 , and crystallizes the crude lactide vapor at a temperature between 5° C. and 20° C.4. The method of claim 1 , wherein the solubility of lactide in the first solvent is 0.1 or less at a temperature between 5° C. and 20° C.5. The method of claim 1 , wherein the vapor pressure of the first solvent is between 5 hPa and 70 hPa at 20° C.6. The method of claim 1 , wherein the steps (ii-a) and (ii-b) are conducted simultaneously.7. The method of claim 1 , further comprising (iii) re-purifying the lactide crystals after the step (ii) claim 1 ,wherein the step (iii) comprises:(iii-a) dissolving the lactide crystals in a second solvent which has the same components as the first solvent,( ...

Benzo[1,3]Dioxine Derivatives And Their Use As LPAR5 Antagonists

The present invention relates to compounds of the formula (I), wherein the residues A, Rto R, Zand Zhave the meanings indicated in the claims. The compounds of the formula (I) are valuable pharmacologically active compounds for use in the treatment of diverse disorders, for example cardiovascular disorders like thromboembolic diseases or restenoses. The compounds of the invention are effective antagonists of the platelet LPA receptor LPAR5 (GPR92) and can in general be applied in conditions in which an undesired activation of the platelet LPA receptor LPAR5, the mast cell LPA receptor LPAR5 or the microglia cell LPA receptor LPAR5 is present or for the cure or prevention of which an inhibition of the platelet, mast cell or microglia cell LPA receptor LPAR5 is intended. The invention furthermore relates to processes for the preparation of compounds of the formula (I), their use, in particular as active ingredients in medicaments, and pharmaceutical compositions comprising them. 6. A compound of the formula I or a pharmaceutically acceptable salt thereof according to for use as medicament.7. A compound of the formula I or a pharmaceutically acceptable salt thereof according to for use in the treatment of a disease responsive to the inhibition of the LPA receptor LPAR5 or the reduction or inhibition of platelet aggregation or thrombus formation or the reduction or inhibition of the activation of mast cells or for reduction or inhibition of the activation of microglial cells.8. A compound of the formula I or a pharmaceutically acceptable salt thereof according to for use in the treatment of thromboembolic diseases claim 1 , deep vein thrombosis claim 1 , venous or arterial thromboembolism claim 1 , thrombophlebitis claim 1 , coronary or cerebral arterial thrombosis claim 1 , cerebral embolism claim 1 , renal embolism claim 1 , pulmonary embolism claim 1 , disseminated intravascular coagulation claim 1 , cardiovascular disorders claim 1 , transient ischemic attacks claim ...

Process for Preparing Chiral Compounds

The present invention is directed to a 2-deoxyribose-5-phosphate aldolase (DERA) chemoenzymatic process for making chiral compounds. 131-. (canceled)32. 2-[2-(4 ,6-Dihydroxy-tetrahydro-pyran-2-yl)ethyl]-isoindole-1 ,3-dione.43. A crystalline form of 4-fluoro-alpha-[2-methyl-1-oxopropyl]-gamma-oxo-N , beta-diphenylbenzenebutanamide characterized as having X-ray diffraction peaks of about 9.0 , 12.7 , 20.2 , 22.6 , and 25.2 degrees two theta.44. A crystalline form of (2R-trans)-5-(4-fluorophenyl)-2-(1-methylethyl)-N ,4-diphenyl-1-[2-(tetrahydro-4-hydroxy-6-oxo-2H-pyran-2-yl)ethyl]-1H-3-carboxamide characterized as having powder X-ray diffraction peaks of about 6.3 , 12.7 , 16.8 , 21.1 and 25.5 degrees two theta. The present invention is directed to a 2-deoxyribose-5-phosphate aldolase (DERA) chemoenzymatic process for making chiral compounds.The use of DERA (deoxyribose aldolase) family of aldolases in chemoenzymatic processes has been described. See U.S. Pat. No. 5,795,749, WO 03/006656, WO 2004/027075, WO 2005/012246; Gijsen, H. J. M., et al. JACS, 1994, 116, 8422-8423; Gijsen, H. J. M., et al., JACS, 1995, 117, 7585-7591; Greenberg, W. A., et al., PNAS, 2004, 101, 5788-5793, U.S. Pat. No. 6,964,863 and Biotechonol J, 101, pgs 537-548 (2006). However, some of the processes provided poor overall yield as well as a mixture of products. In addition, the processes were limited to specific substrates. Accordingly, there exists a need in the art for a chemoenzymatic process that is effective and efficient for alternative substrates.The present invention relates to a process comprising the step of reacting acetaldehyde with an N-protected aminoaldehyde substrate selected from the group consisting of 3-phthalimidopropionaldehyde, N-formyl-3-aminopropionaldehyde, 3-succinimido-propionaldehyde or N-diBoc-3-aminopropionaldehyde under aldolase-catalyzed aldol condensation conditions to form the corresponding lactol.The present invention also relates to a process wherein said ...

METHOD FOR PREPARING LACTIDE USING AN IONIC SOLVENT

Disclosed is a method for preparing lactide by using a solvent. According to the method, since an ionic liquid is used as a solvent in a second step in the course of preparing lactide, it is possible to secure mobility of the resulting reactant, and decrease a reaction temperature. In addition, the ionic liquid absorbs moisture generated during the reaction, and thus prevents degradation of lactide which is susceptible to moisture. Furthermore, to the present method allows for the preparation of lactide successively through the continuous supply of lactic acid oligomers. Because the use of an ionic liquid minimizes the contamination of a reactive group with by-products, the use of a solvent for reactor washing is unnecessary. Further, owing to a high boiling point of the ionic liquid, the ionic liquid can be easily harvested and recycled. 1. A method for preparing lactide , comprising:(a) adding an ionic solvent to one or more lactic acid oligomers, the one or more lactic acid oligomers being synthesized through polymerization of at least one lactic acid monomer; and(b) synthesizing lactide from the one or more lactic acid oligomers added to the ionic solvent by regulating temperature and pressure conditions.2. The method of claim 1 , wherein the polymerization of the lactic acid monomer in the step (a) is carried out at a temperature of about 120 to 300° C. under a pressure of about 1 to 500 atm for about 1 to 5 hours.3. The method of claim 1 , wherein the synthesis of lactides in the step (b) is carried out at a temperature of about 100 to 1000° C. under a pressure of about 1 to 600 atm for about 1 to 5 hours.4. The method of claim 1 , wherein the one or more lactic acid oligomers have a molecular weight of about 600 to 9000 g/mol.5. The method of claim 1 , wherein the ionic solvent is selected from the group consisting of 1-butyl-1-methyl-azepanum bis(trifluoromethylsulfonyl)imide; 1-butyl-1-methyl-azepanum dicyanamide; 6-azonia-spiro[5 claim 1 ,6]dodecan bis( ...

HETEROATOM CONTAINING CYCLIC DIMERS

The present invention provides cyclic dimers of alpha acids and polymers derived therefrom. Also provided are processes for preparing and methods of using the cyclic dimers and the polymers derived from the cyclic dimers. 2. The process of claim 1 , wherein Ris hydrogen claim 1 , alkyl claim 1 , or substituted alkyl claim 1 , R claim 1 , R claim 1 , R claim 1 , and Rare hydrogen; Ris C-Calkyl; and n is from 1 to 10.4. The process of claim 3 , wherein R claim 3 , R claim 3 , R claim 3 , R claim 3 , Rand Rare hydrogen; Rand Rare C-Calkyl; and each of n and m is from 1 to 10.5. The process of claim 4 , wherein Rand Rare methyl; Y and Z are sulfur claim 4 , and each of n and m is 2.6. The process of claim 1 , wherein the polymer comprising repeat units of Formula (XX) has a number average molecular weight of at least about 2 claim 1 ,000 Da claim 1 , at least about 10 claim 1 ,000 Da claim 1 , at least about 100 claim 1 ,000 Da claim 1 , or at least about 1 claim 1 ,000 claim 1 ,000 Da.7. The process of claim 1 , wherein the polymer comprising repeat units of Formula (XX) contains less than about 5% by weight of free monomer.8. The process of claim 1 , wherein the reaction is conducted in the absence or presence of a catalyst.9. The process of claim 1 , wherein the temperature is from about 120° C. to about 180° C.10. The process of claim 1 , wherein the heating occurs in an extruder claim 1 , the extruder being a twin screw extruder claim 1 , a single screw extruder claim 1 , or an extruder thermoforming machine.11. An extrudate prepared by the process of .12. The process of claim 1 , wherein the process further comprises heating in the presence of a plurality of additional monomers to form a copolymer.13. The process of claim 12 , wherein the plurality of additional monomers is chosen from acrylates claim 12 , aminoacrylates claim 12 , alkylene succinates claim 12 , alkylene oxalates claim 12 , amides claim 12 , amino acids claim 12 , anhydrides claim 12 , arylates ...

PHOTOREACTIVE COMPOUNDS

The present invention relates to photoreactive compounds that are particularly useful in materials for the alignment of liquid crystals. 3. The compound comprising a group terminal group of formulae (I) or (Ia) according to claim 1 , wherein the polymerizable group is “D” claim 1 , which is preferably selected from acrylate claim 1 , methacrylate claim 1 , 2-chloroacrylate claim 1 , 2-phenylacrylate claim 1 , optionally N-lower alkyl substituted acrylamide claim 1 , methacrylamide claim 1 , 2-chloroacrylamide claim 1 , 2-phenylacrylamide claim 1 , vinyl ether and ester claim 1 , allyl ether and ester epoxy claim 1 , styrene and styrene derivatives claim 1 , for example alpha-methylstyrene claim 1 , p-methylstyrene claim 1 , p-tert-butyl styrene claim 1 , p-chlorostyrene claim 1 , etc. claim 1 , siloxanes claim 1 , diamines claim 1 , imide monomers claim 1 , amic acid monomers and their esters claim 1 , amidimide monomers claim 1 , maleic acid and maleic acid derivatives claim 1 , for example claim 1 , di-n-butyl maleate claim 1 , dimethyl maleate claim 1 , diethyl maleate claim 1 , etc claim 1 , fumaric acid and fumaric acid derivatives claim 1 , for example claim 1 , di-n-butyl fumarate claim 1 , di-(2-ethylhexyl) fumarate claim 1 , etc claim 1 , urethanes or their corresponding homo- and co-polymers.4. The compound comprising a group terminal group of formulae (I) or (Ia) according to claim 1 , wherein the spacer unit is Sand/or Seach independently from each other represents a single bond or a cyclic claim 1 , straight-chain or branched claim 1 , substituted or unsubstituted C-Calkylen claim 1 , in which one or more claim 1 , preferably non-adjacent claim 1 , C-atom claim 1 , CH— or CH— claim 1 , group unreplaced or replaced by a linking group claim 1 , and/or a non-aromatic claim 1 , aromatic claim 1 , unsubstituted or substituted carbocyclic or heterocyclic group of formula (V):{'br': None, 'sup': 2a', '1', '1', '2', '2', '1a, 'sub': a4', 'a1', 'a2', 'a3, '—(Z ...

LIQUID CRYSTAL COMPOUNDS OF CYCLOALKYL-CONTAINING DIBENZOFURAN DERIVATIVES, PREPARATION METHOD THEREFOR AND USE THEREOF

Disclosed are liquid crystal compounds of cycloalkyl-containing dibenzofuran derivatives, a preparation method therefor and use thereof. The compounds are as represented by formula I. In the molecular structures of the compounds of formula I provided by the present invention, liquid crystal compounds of cycloalkyl terminal group-containing dibenzofuran derivatives, compared with those having flexible alkyl chains as terminal groups, exhibit better intersolubility, and thus the use of a compound as represented by formula I provided by the present invention can improve the intersolubility of a liquid crystal compound and extend the application range of a liquid crystal mixture, producing an important application value. 4. A liquid crystal medium claim 1 , wherein said liquid crystal medium comprises one or more compounds as represented by formula I in .7. The liquid crystal medium according to claim 6 , wherein in said liquid crystal medium claim 6 , the total content in weight percentage of one or more compounds as represented by formula I is 1-24% claim 6 , the total content in weight percentage of one or more compounds as represented by formula IV is 35-58% claim 6 , and the total content in weight percentage of one or more compounds as represented by formula V is 30-46%.10. Use of any one or more compounds of in the preparation of a liquid crystal mixture claim 1 , a liquid crystal display device material or an electro-optical display device material. The present invention belongs to the technical field of liquid crystal compounds and applications, and relates to liquid crystal compounds of cycloalkyl-containing dibenzofuran derivatives, a preparation method therefor and use thereof.Since the Austrian scientist Reinitzer first synthesized a liquid crystal in 1888, the actual development of the liquid crystal industry is in the recent more than 30 years; since liquid crystal display materials have obvious advantages, such as a low drive voltage, a small power ...

Process for Preparing Cyclic Esters and Cyclic Amides

The invention relates to a process for preparing a cyclic ester or a cyclic amide, comprising the step of: 115-. (canceled)17. The process according to claim 16 , wherein at least one of said interconnected and non-parallel channel systems comprises 12- or more-membered ring channels.18. The process according to claim 16 , wherein said zeolite has a Brønsted acid density between 0.05 and 6.5 mmol/g dry weight.19. The process according to claim 16 , wherein said zeolite comprises a BEA topology claim 16 , a MFI topology claim 16 , a FAU topology claim 16 , a MEL topology claim 16 , a FER topology claim 16 , and a MWW topology.20. The process according to claim 16 , wherein said zeolite comprises a BEA topology.21. The process according to claim 16 , wherein X is Al.22. The process according to claim 16 , wherein said zeolite comprises at least three interconnecting and non-parallel channel systems.23. The process according to claim 16 , wherein said aminocarboxylic acid is provided in a composition comprising said amino-carboxylic acid in a concentration of at least 1 wt % based on a total weight of the composition.24. The process according to claim 16 , wherein said process is performed under conditions of water removal.25. The process according to claim 24 , wherein said water removal is performed via azeotropic distillation. The invention relates to a process for preparing cyclic esters and cyclic amides, which may be used as starting products for the preparation of polymers such as biopolymers.Cyclic esters are useful compounds that can be polymerized into polymeric materials. Such polymeric materials are useful in the preparation of biodegradable plastic materials and other plastic materials. Cyclic esters are also useful as plasticizers and as intermediates for production of surface-active agents and plasticizers.Cyclic esters are usually prepared by condensing hydroxy acids to an oligomeric prepolymer. The prepolymer is then depolymerized to a cyclic ester. ...

SALT AND PHOTORESIST COMPOSITION CONTAINING THE SAME

A salt comprising a group represented by the formula (aa): 2. The salt according to claim 1 , which comprises a cation and an anion having the group represented by formula (aa).3. The salt according to claim 2 , wherein the anion having the group represented by formula (aa) further has a sulfonate.6. The salt according towherein the ring W1 represents an adamantane ring or a cyclohexane ring.8. The salt according towherein the ring W represents 1,3-dioxan-2-one ring.9. An acid generator comprising the salt according to .10. A photoresist composition comprising the acid generator according to and a resin which comprises a structural unit having an acid-labile group.11. The photoresist composition according to which further comprises a salt generating an acid weaker in acidity than an acid generated from the acid generator.12. A process for producing a photoresist pattern comprising the following steps (1) to (5):{'claim-ref': [{'@idref': 'CLM-00010', 'claim 10'}, {'@idref': 'CLM-00011', '11'}], '(1) a step of applying the photoresist composition according to or on a substrate,'}(2) a step of forming a composition film by conducting drying,(3) a step of exposing the composition film to radiation,(4) a step of baking the exposed composition film, and(5) a step of developing the baked composition film thereby forming a photoresist pattern. This nonprovisional application claims priority under 35 U.S.C. § 119(a) on Patent Application No. 2017-200113 filed in JAPAN on Oct. 16, 2017, the entire contents of which are hereby incorporated by reference.The invention of the disclosure relates to a salt, and acid generator comprising the same, a photoresist composition and a method for producing a photoresist pattern.US2011/014568A1 mentions the following salt and a photoresist composition comprising the same as an acid generator.JP2013-256496A1 mentions the following salt and a photoresist composition comprising the same as an acid generator.US2017/0247323A1 mentions the ...

METHOD OF FLUORINATION USING IODONIUM YLIDES

A process for fluorination of aromatic compounds employing iodonium ylides and applicable to radiofluorination using F is described. Processes, intermediates, reagents and radiolabelled compounds are described. 2. (canceled)3. The process of claim 1 , wherein step (a) is performed in the presence of an oxidizing agent selected from the group consisting of sodium perborate claim 1 , urea-hydrogen peroxide adduct claim 1 , 1-chloromethyl-4-fluoro-1 claim 1 ,4-diazoniabicyclo[2.2.2]octane bis(tetrafluoroborate) (Selectfluor®) claim 1 , potassium peroxymonosulfate (OXONE®) claim 1 , dimethyldioxirane claim 1 , or meta-chloroperoxybenzoic acid claim 1 , and a carboxylate salt that is an acetate source or a trifluoroacetate source.410-. (canceled)11. The process of claim 1 , wherein step (b) is carried out in the presence of a carbonate base.12. (canceled)1418-. (canceled)2227-. (canceled)28. The process of claim 1 , wherein said fluoride source comprises [F] fluoride.2931-. (canceled)33. The compound of claim 32 , wherein Zis O and Zis O.3437-. (canceled)4083-. (canceled)86. A process for preparing an aromatic fluoride compound (Ar—F) comprising:{'claim-ref': {'@idref': 'CLM-00032', 'claim 32'}, '(c) reacting a compound according to with a fluoride source to form an aromatic fluoride compound (Ar—F).'}87. (canceled)88. The process of claim 86 , wherein said fluoride source comprises [F] fluoride.8991-. (canceled)92. An [F] radiolabelled compound claim 86 , wherein the compound is selected from filorexant claim 86 , mosapride claim 86 , lapatinib claim 86 , risperidone claim 86 , ezetimibe claim 86 , astemizole claim 86 , paroxetine claim 86 , pitvastatin claim 86 , crizotinib claim 86 , safinamide claim 86 , 6-fluoro-meta-tyrosine claim 86 , and meta-fluorobenzylguanidine. This application claims the benefit of U.S. Provisional Application Ser. No. 62/248,060, filed Oct. 29, 2015, the disclosure of which is incorporated herein by reference in its entirety.This disclosure ...

HIGH YIELD, ECO-FRIENDLY RECYCLING METHOD OF POLYLACTIC ACID USING SUPERCRITICAL OR DENSE GAS CARBON DIOXIDE

A recycling method of polylactic acid in a single step by using supercritical or dense gas carbon dioxide is provided. The recycling method includes the steps of adjusting a temperature of a reactor to at least 120° C., and adjusting a pressure to values above or below a critical pressure of carbon dioxide, wherein the critical pressure is 73.8 bar. 1. A method for a conversion of polylactic acid into lactide in a single step , wherein a reaction is performed in a carbon dioxide medium.2. The method according to claim 1 , wherein the carbon dioxide medium is a supercritical carbon dioxide medium.3. The method according to claim 1 , wherein the carbon dioxide medium is a dense gas carbon dioxide medium.4. The method according to claim 2 , comprising the following steps of:a) adjusting a temperature of a reactor to at least 120° C.,b) adjusting a reactor pressure to values above a critical pressure of carbon dioxide, wherein the critical pressure is 73.8 bar,wherein the steps of a) and b) are applied at a desired sequence.5. The method according to claim 3 , comprising the following steps of:a) adjusting a temperature of a reactor to at least 120° C.,b) adjusting a reactor pressure to values less than a critical pressure of carbon dioxide, wherein the reactor pressure is in a range of 10 bar to 73 bar,wherein the steps of a) and b) are applied at a desired sequence.6. The method according to claim 1 , comprising the following steps of:a) carrying out a heating and a pressurization gradually,b) filling a reactor with carbon dioxide at a temperature and a pressure ensuring a loaded carbon dioxide remains in a gas phase,c) increasing a temperature of the reactor to a reaction temperature,d) filling the reactor with the carbon dioxide to a reaction pressure.7. The method according to claim 1 , wherein a reaction time is at least 10 minutes.8. The method according to claim 2 , wherein a reactor pressure is in a range of 74-300 bar claim 2 , and a maximum pressure does not ...

MATERIAL FOR FORMING ORGANIC FILM, SUBSTRATE FOR MANUFACTURING SEMICONDUCTOR DEVICE, METHOD FOR FORMING ORGANIC FILM, PATTERNING PROCESS, AND COMPOUND FOR FORMING ORGANIC FILM

The present invention is a material for forming an organic film, containing: (A) a compound for forming an organic film shown by the following general formula (1A); and (B) an organic solvent, where Wi represents a tetravalent or hexavalent organic group, n1 represents an integer of 1 or 2, n2 represents 2 or 3, each Rindependently represents any in the following formula (1B), and a hydrogen atom of a benzene ring in the formula (1A) is optionally substituted with a fluorine atom. This provides: a compound having a dioxin structure, which is cured even under film formation conditions in inert gas, and which is capable of forming an organic underlayer film having not only excellent heat resistance and properties of filling and planarizing a pattern formed on a substrate, but also favorable film formability and adhesiveness to a substrate; and an organic film material containing the compound. 4. The material for forming an organic film according to claim 1 , wherein the component (A) satisfies 1.00≤Mw/Mn≤1.10 claim 1 , where Mw is a weight-average molecular weight and Mn is a number-average molecular weight measured by gel permeation chromatography in terms of polystyrene.5. The material for forming an organic film according to claim 1 , wherein the component (B) is a mixture of one or more kinds of organic solvent having a boiling point of lower than 180° C. and one or more kinds of organic solvent having a boiling point of 180° C. or higher.6. The material for forming an organic film according to claim 1 , further comprising at least one of (C) an acid generator claim 1 , (D) a surfactant claim 1 , (E) a crosslinking agent claim 1 , and (F) a plasticizer.7. A substrate for manufacturing a semiconductor device claim 1 , comprising an organic film on the substrate claim 1 , the organic film being a cured film of the material for forming an organic film according to .8. A method for forming an organic film employed in a semiconductor device manufacturing process claim ...

ECKOL DERIVATIVES, METHODS OF SYNTHESIS AND USES THEREOF

Provided herein are eckol derivatives, methods of synthesis thereof and pharmaceutical compositions thereof. In other embodiments, provided herein are methods of treatment, prevention, or amelioration of a variety of medical disorders such as, for example, Alzheimer's disease, microbial infections, obesity, diabetes, cancer or inflammation using the compounds and pharmaceutical compositions disclosed herein. 10. The compound of claim 1 , wherein R{'sub': 3', '3', '2', '3', '2', '3', '2, 'is —CH, —CF, —CHPh, —C(O)OCH, —C(O)OPh, —CHOCHor —CHC≡CH.'}11. The compound of claim 2 , wherein Ris{'sub': 3', '3', '2', '3', '2', '3', '2', '9', '3', '3', '2', '3', '2', '3', '2', '1', '9, 'hydrogen, —CH, —CF, —CHPh, —C(O)OCH, —C(O)OPh, —CHOCHor —CHC≡CH and Ris hydrogen, —CH, —CF, —CHPh, —C(O)OCH, —C(O)OPh, —CHOCHor —CHC≡CH with the proviso that Rand Rare not both hydrogen.'}12. The compound of claim 3 , wherein R{'sub': 3', '3', '2', '3', '2', '3', '2, 'is —CH, —CF, —CHPh, —C(O)OCH, —C(O)OPh, —CHOCHor —CHC≡CH.'}13. The compound of claim 4 , wherein Ris{'sub': 3', '3', '2', '3', '2', '3', '2', '1', '3', '3', '2', '3', '2', '3', '2', '7', '1, 'hydrogen, —CH, —CF, —CHPh, —C(O)OCH, —C(O)OPh, —CHOCHor —CHC≡CH and Ris hydrogen, —CH, —CF, —CHPh, —C(O)OCH, —C(O)OPh, —CHOCHor —CHC≡CH with the proviso that Rand Rare not both hydrogen.'}14. The compound of claim 5 , wherein Ris{'sub': 3', '3', '2', '3', '2', '3', '2', '1', '3', '3', '2', '3', '2', '3', '2', '6', '1, 'hydrogen, —CH, —CF, —CHPh, —C(O)OCH, —C(O)OPh, —CHOCHor —CHC≡CH and Ris hydrogen, —CH, —CF, —CHPh, —C(O)OCH, —C(O)OPh, —CHOCHor —CHC≡CH with the proviso that Rand Rare not both hydrogen.'}15. The compound of claim 6 , wherein R{'sub': 3', '3', '2', '3', '2', '3', '2, 'is —CH, —CF, —CHPh, —C(O)OCH, —C(O)OPh, —CHOCHor —CHC≡CH.'}16. The compound of claim 7 , wherein R{'sub': 3', '3', '2', '3', '2', '3', '2, 'is —CH, —CF, —CHPh, —C(O)OCH, —C(O)OPh, —CHOCHor —CHC≡CH.'}17. The compound of claim 8 , wherein R{'sub': 3', '3', '2', '3', ...

NEW SIGMA-RECEPTORS LIGANDS WITH ANTI-APOPTOTIC AND/OR PRO-APOPTOTIC PROPERTIES, OVER CELLULAR BIOCHEMICAL MECHANISMS WITH NEUROPROTECTIVE, ANTI-CANCER, ANTI-METASTATIC AND ANTI-(CHRONIC) INFLAMMATORY ACTION

The present invention involves new and original sigma receptors ligands: (Mono-or di-alkylaminoalkyl)-γ-butyrolactones, their analogues aminotetrahydrofuranes, the (1-adamantyl) phenyl(s) alkylamines, the N,N Dialkyl α-[(adamantyl-l)benzyloxy-2] alkylamines and the 3-cyclopentyl adamantyl-amines or alkylamines or alkyl phenylamines, their enantiomers or diastereoisomers and their pharmaceutically acceptable salts, with pro-apoptotic and/or anti-apoptotic properties over cellular biochemical mechanisms, with anti-cancer, anti-metastatic, anti-(chronic) inflammatory, neuro-protective, anticonvulsive, antidepressive and nooanaleptic or sedative action. 1. A sigma(σ)-receptor ligand with anti-apoptotic and/or pro-apoptotic properties said compound consisting essentially of:a sigma(σ)-receptor ligand compound consisting essentially of tetrahydro-N,N-dimethyl-2,2-diphenyl-3-furanomethanamine, enantiomers or diastereoisomers of tetrahydro-N,N-dimethyl-2,2-diphenyl-3-furanomethanamine, and pharmacologically acceptable salts of tetrahydro-N,N-dimethyl-2,2-diphenyl-3-furanomethanamine.24-. (canceled)5. The compound according to wherein said tetrahydro-N claim 1 ,N-dimethyl-2 claim 1 ,2-diphenyl-3-furanomethanamine is a metabolite of said tetrahydro-N claim 1 ,N-dimethyl-2 claim 1 ,2-diphenyl-3-furanomethanamine.6. The compound of wherein said metabolite is tetrahydro-N-methyl-2 claim 5 ,2-diphenyl-3-furanomethanamine This application is a continuation and claims priority to U.S. Ser. No. 12/522,761, filed Jul. 10, 2009, which is a U.S. national phase application under 35 U.S.C. §371 based upon International Application No. PCT/GR2008/000002 filed on Jan. 14, 2008. Additionally, this U.S. national phase application claims the benefit of priority of International Application No. PCT/GR2008/000002 filed on Jan. 14, 2008, and Greece Application No. 20070100020 filed on Jan. 17, 2007. The entire disclosures of the prior applications are incorporated herein by reference. The ...

AMORPHOUS FORM OF ELIGLUSTAT HEMITARTARATE

The present application relates to the solid state forms of Eliglustat hemitartrate and the processes for the preparation thereof. The application further provides solid dispersion of Eliglustat hemitartrate having Eliglustat hemitartrate in amorphous form. 2: A process for preparing amorphous form of Eliglustat hemitartrate comprising:a) providing a solution of Eliglustat hemitartrate in a solvent;b) removing the solvent from the solution obtained in step a), andc) recovering amorphous form of Eliglustat hemitartrate.3: The process of wherein suitable solvent in step a) is selected from alcohols claim 2 , esters claim 2 , ketones claim 2 , hydrocarbons claim 2 , water or mixtures thereof.4: The process of wherein suitable solvent in step a) is selected from methanol claim 2 , isopropyl alcohol claim 2 , ethyl acetate claim 2 , acetone claim 2 , dichloromethane or mixtures thereof.5: The process of wherein removal of solvent in step b) is affected by evaporation claim 2 , freeze drying claim 2 , spray drying claim 2 , lyophilization claim 2 , by addition of suitable anti-solvent or any combination thereof.6: The process of wherein step c) involves an additional step of drying the isolated Eliglustat hemitartrate.7: A solid dispersion comprising amorphous Eliglustat hemitartrate in a dispersing agent.8: The solid dispersion of claim 7 , wherein the dispersing agent comprises hydroxypropyl methyl cellulose (HPMC) claim 7 , Polyvinyl pyrrolidone (PVP) claim 7 , Colloidal silicon dioxide and the like.9: The solid dispersion of claim 8 , wherein PVP is of different grades like K-15 claim 8 , K-30 claim 8 , K-60 and like.10: The solid dispersion of claim 8 , wherein colloidal silicon dioxide like Syloid 244 FP is employed.11: A pharmaceutical composition comprising solid dispersion of . The present application relates to the solid state forms of Eliglustat hemitartrate and the processes for the preparation thereof.Chemically Eliglustat is named N-[(1R,2R)-2-(2,3-dihydro-1 ...

DUAL MODULATOR OF MGLUR5 AND 5-HT2A RECEPTOR, AND USE THEREOF

Disclosed are a dual modulator of mGluR5 and 5-HT2AR (5-HT2A receptor), and use thereof. More specifically, disclosed are a compound which acts as modulator of mGluR5 and an antagonist of 5-HT2AR at the same time, and use thereof as therapeutic agent for pain. 2. The compound or pharmaceutically acceptable salt thereof according to claim 1 , wherein{'sub': 1', '2', '4', '7, 'Xand Xtogether with carbon atom to which they are attached form C-Ccycloalkyl or 4- to 6-membered heterocycloalkyl;'}{'sub': '3', 'Xis CH or N;'}{'sub': 1', '1', '8, 'Ris hydroxy, halo or C-Calkyl;'}{'sub': 2', '1', '8', '1', '5', '1', '5', '1', '5', '1', '5', '3', '6', '1', '5', '3', '6', '1', '5', '1', '5', '1', '5', '1', '5', '1', '8', '1', '8', '1', '8', '1', '8', '1', '5', '1', '5', '1', '5, 'Ris hydroxy, halo, C-Calkyl, C-Calkoxy, 4- to 6-membered heterocycloalkyl, hydroxy-C-Calkyl, halo-C-Calkyl, C-Calkylamino, C-Ccycloalkyl-C-Calkyl, C-Ccycloalkylamino, halo-C-Calkylamino, C-Calkylaminocarbonyl, C-Calkoxycarbonyl-C-Calkyl, carboxy-C-Calkyl, aminocarbonyl-C-Calkyl, hydroxyaminocarbonyl-C-Calkyl, C-Calkylaminocarbonyl-C-Calkyl, di(C-Calkyl)aminocarbonyl-C-Calkyl or pyridyl;'}{'sub': 3', '1', '8, 'Ris deuterium, fluoro or C-Calkyl;'}{'sub': 4', '5', '1', '5, 'Rand Rare each independently halo or C-Calkyl;'}m is an integer of 0 to 2;n is 0 or 1; andl, p and q are each independently an integer of 0 to 2;wherein the heterocycloalkyl has 1 to 3 heteroatoms selected from the group consisting of N and O.3. The compound or pharmaceutically acceptable salt thereof according to claim 1 , wherein the 4- to 7-membered aliphatic ring is cyclobutane claim 1 , cyclopentane claim 1 , cyclohexane or cycloheptane.4. The compound or pharmaceutically acceptable salt thereof according to claim 1 , wherein the 4- to 6-membered heteroaliphatic ring is oxetane claim 1 , tetrahydrofuran claim 1 , tetrahydropyran claim 1 , dioxane or piperidine.5. The compound or pharmaceutically acceptable salt thereof according ...

INHIBITORS OF BACTERIAL TYPE III SECRETION SYSTEM

Organic compounds showing the ability to inhibit effector toxin secretion or translocation mediated by bacterial type III secretion systems are disclosed. The disclosed type III secretion system inhibitor compounds are useful for combating infections by Gram-negative bacteria such as spp., spp., spp., enteropathogenic and enteroinvasive , and spp. having such type III secretion systems. 3. A compound according to claim 1 , comprising the R-isomer in substantially pure form.5. A pharmaceutical composition comprising one or more bacterial T3SS inhibitor compounds according to and a pharmaceutically acceptable carrier or excipient.6. The pharmaceutical composition according to claim 5 , wherein said one or more T3SS inhibitor compounds is the R-isomer in substantially pure form.710-. (canceled)11. A method for treating an individual infected with or exposed to a Gram-negative bacterium comprising administering to said individual an effective amount to inhibit T3SS-mediated effector secretion of a compound according to .12. The method according to claim 11 , wherein said individual is human.13Pseudomonas, Salmonella, YersiniaChlamydia.. The method according to claim 12 , wherein said Gram-negative bacterium is of the genus claim 12 , or14Pseudomonas aeruginosa, Yersinia pestisChlamydia trachomatis.. The method according to claim 13 , wherein said Gram-negative bacterium is or15Pseudomonas aeruginosa.. The method according to claim 14 , wherein said Gram-negative bacterium is16. The method according to claim 11 , further comprising administering an additional active ingredient selected from the group consisting of an antibiotic claim 11 , an antibody claim 11 , an antiviral agent claim 11 , an anticancer agent claim 11 , an analgesic claim 11 , an immunostimulatory agent claim 11 , a natural claim 11 , synthetic or semisynthetic hormone claim 11 , a central nervous system stimulant claim 11 , an antiemetic agent claim 11 , an anti-histamine claim 11 , an erythropoietin ...

MODULATORS OF THE INTEGRATED STRESS PATHWAY

Provided herein are compounds, compositions, and methods useful for modulating the integrated stress response (ISR) and for treating related diseases, disorders and conditions. 2. The compound of claim 1 , wherein D is a bridged bicyclic cycloalkyl optionally substituted with 1-4 R.3. The compound of any one of - claim 1 , wherein D is a bridged bicyclic 5-8 membered cycloalkyl optionally substituted with 1-4 R.4. The compound of any one of - claim 1 , wherein D is bicyclo[1.1.1]pentane claim 1 , bicyclo[2.2.1]heptane claim 1 , bicyclo[2.1.1]hexane claim 1 , bicyclo[2.2.2]octane claim 1 , bicyclo[3.2.1]octane claim 1 , or 2-azabicyclo[2.2.2]octane claim 1 , each of which is optionally substituted with 1-4 Rgroups.8. The compound of any one of - claim 1 , wherein D is substituted with 0 R.10. The compound of any one of - claim 1 , wherein D is substituted with 1 or 2 R.12. The compound of any one of - claim 1 , wherein each Ris independently selected from the group consisting of oxo claim 1 , —OH claim 1 , —C(O)OH claim 1 , —C(O)OR claim 1 , halo claim 1 , and hydroxy-C-Calkyl.13. The compound of any one of - claim 1 , wherein Lis a bond claim 1 , 2-7 membered heteroalkylene claim 1 , —NR— claim 1 , or —O— claim 1 , wherein 2-7 membered heteroalkylene is optionally substituted by 1-5R.14. The compound of any one of - claim 1 , wherein Lis a bond claim 1 , 2-7 membered heteroalkylene claim 1 , —NR— claim 1 , or —O— claim 1 , wherein 2-7 membered heteroalkylene is substituted by 0 R.15. The compound of any one of - claim 1 , wherein Lis selected from a bond claim 1 , CHO—* claim 1 , CHOCH—* claim 1 , —NCH— claim 1 , —NH— claim 1 , or —O— claim 1 , wherein “-*” indicates the attachment point to A.16. The compound of any one of - claim 1 , wherein Ris hydrogen or CH.17. The compound of any one of - claim 1 , wherein Ris hydrogen or CH.18. The compound of any one of - claim 1 , wherein A is phenyl or 5-6-membered heteroaryl; wherein phenyl or 5-6-membered heteroaryl is ...

Substituted Azoanthracene Derivatives and Intermediates for Preparation Thereof

The present invention relates to substituted azoanthracene derivatives and intermediates for the preparation thereof. The substituted azoanthracene derivatives and associated intermediates may be useful for the preparation of pharmaceutical compositions for the treatment or prevention of diseases, disorders, and conditions wherein modulation of the human GLP-1 receptor is beneficial. 2. The compound of claim 1 , wherein Ris —(R)-1-phenyl-propyl.3. The compound of claim 1 , wherein Ris —(S)-1-phenyl-propyl.6. The compound of claim 5 , wherein Ris —(R)-1-phenyl-propyl.7. The compound of claim 5 , wherein Ris —(S)-1-phenyl-propyl.9. The compound of claim 8 , wherein Ris —(R)-1-phenyl-propyl.10. The compound of claim 8 , wherein Ris —(S)-1-phenyl-propyl. 1. Field of InventionThe present invention relates to substituted azoanthracene derivatives and intermediates for the preparation thereof. The substituted azoanthracene derivatives and associated intermediates may be useful for the preparation of pharmaceutical compositions for the treatment or prevention of diseases, disorders, and conditions wherein modulation of the human GLP-1 receptor is beneficial.2. Description of Related ArtDiabetes mellitus type 2 is a metabolic disorder where the disease progression may be characterized by one or more of peripheral tissue insulin resistance, hyperglycemia, islet b-cell compensation, hyperinsulinemia, dyslipidemia, increased liver gluconeogenesis, and ultimate loss of b-cell mass and function. The pathophysiological consequences of aberrant glucose and lipid metabolism are toxicity to organs such as the kidney, eye, peripheral neurons, vasculature and heart. Thus, there is a need for agents that may delay disease progression by improving glycemic control and by improving b-cell mass and function.Glucagon-like peptide-1 (GLP-1) is a member of the incretin family of neuroendocrine peptide hormones secreted from L-cells of the intestine in response to food ingestion. GLP-1 has ...

SYNTHESIS OF UDP-GLUCOSE: N-ACYLSPHINGOSINE GLUCOSYLTRANSFERASE INHIBITORS

Disclosed is a novel enantiomeric synthesis ceramide-like inhibitors of UDP-glucose:N-acylsphingosine glucosyltransferase. Also disclosed are novel intermediates formed during the synthesis. 123-. (canceled)25. The method of claim 24 , wherein the hydrolysis is carried out using methanol as solvent.26. The method of claim 24 , wherein the compound of formula (1) is prepared by reacting (5S)-5-phenylmorpholin-2-one with 1 claim 24 ,4-benzodioxan-6-carboxaldehyde.29. The method of claim 28 , wherein the reduction is carried out using lithium aluminum hydride.31. The method of claim 30 , wherein the reduction is carried out using lithium aluminum hydride.33. The method of claim 32 , wherein the hydrolysis is carried out using methanol as solvent.34. The method of claim 32 , wherein the compound of formula (1) is prepared by reacting (5S)-5-phenylmorpholin-2-one with 1 claim 32 ,4-benzodioxan-6-carboxaldehyde. This application is a divisional of U.S. patent application Ser. No. 10/916,824, filed Aug. 12, 2004, which is a divisional of U.S. patent application Ser. No. 10/197,227, filed Jul. 16, 2002, which claims the benefit of U.S. Provisional Application No. 60/305,814, filed Jul. 16, 2001. The entire teachings of these applications are incorporated herein by reference.Glycosphingolipids (GSLs) are a class of naturally occurring compounds which have a multitude of biological functions, including the ability to promote cell growth, cell differentiation, adhesion between cells or between cells and matrix proteins, binding of microorganisms and viruses to cells, and metastasis of tumor cells. GSLs are derived from glucosylceramide (GlcCer), which is produced from ceramide and UDP-glucose by the enzyme UDP-glucose:N-acylsphingosine glucosyltransferase (GlcCer synthase). The structure of ceramide is shown below:The accumulation of GSLs has been linked to a number of diseases, including Tay-Sachs, Gaucher's, and Fabry's diseases (see, for example, U.S. Pat. No. 6,051,598). ...

CONDENSED-CYCLIC COMPOUND AND ORGANIC LIGHT-EMITTING DEVICE INCLUDING THE SAME

A condensed cyclic compound and an organic light-emitting device including the same. The a condensed cyclic compound represented by Formula 1: 2. The condensed cyclic compound of claim 1 , wherein{'sub': 1', '2, 'Xand Xare each O.'}3. The condensed cyclic compound of claim 1 , wherein{'sub': 1', '2', '11, 'L, L, and Lare each independently selected froma phenylene group, a pentalenylene group, an indenylene group, a naphthylene group, an azulenylene group, a heptalenylene group, an indacenylene group, an acenaphthylene group, a fluorenylene group, a spiro-bifluorenylene group, a benzofluorenylene group, a dibenzofluorenylene group, a phenalenylene group, a phenanthrenylene group, an anthracenylene group, a fluoranthenylene group, a triphenylenylene group, a pyrenylene group, a chrysenylene group, a naphthacenylene group, a picenylene group, a perylenylene group, a pentaphenylene group, a hexacenylene group, a pentacenylene group, a rubicenylene group, a coronenylene group, an ovalenylene group, a pyrrolylene group, a thiophenylene group, a furanylene group, an imidazolylene group, a pyrazolylene group, a thiazolylene group, an isothiazolylene group, an oxazolylene group, an isoxazolylene group, a pyridinylene group, a pyrazinylene group, a pyrimidinylene group, a pyridazinylene group, an isoindolylene group, an indolylene group, an indazolylene group, a purinylene group, a quinolinylene group, an isoquinolinylene group, a benzoquinolinylene group, a phthalazinylene group, a naphthyridinylene group, a quinoxalinylene group, a quinazolinylene group, a cinnolinylene group, a carbazolylene group, a phenanthridinylene group, an acridinylene group, a phenanthrolinylene group, a phenazinylene group, a benzimidazolylene group, a benzofuranylene group, a benzothiophenylene group, an benzoisothiazolylene group, a benzoxazolylene group, an benzoisoxazolylene group, a triazolylene group, a tetrazolylene group, an oxadiazolylene group, a triazinylene group, a dibenzofuranylene ...

Lactate Production Process

A process for producing alkyl R-lactate from an initial compound comprising substructure (I) is provided. The process involves producing an intermediate comprising R,R- and S,S-lactide from the initial compound, wherein the initial compound is subjected to stereoisomerisation conditions; and reacting at least a portion of the intermediate with an alkyl alcohol to produce a product comprising alkyl R-lactate, wherein alkyl R-lactate is produced in the presence of an enzyme. Also provided are processes for the production of R-lactic acid, oligomeric R-lactic acid, R,R-lactide, poly-R-lactic acid and stereocomplex lactic acid. 2. The process as claimed in claim 1 , wherein the initial compound is contacted with a tertiary amine stereoisomerisation catalyst.3. The process as claimed in claim 1 , wherein the initial compound comprises oligomeric S-lactic acid claim 1 , S-lactic acid or a salt thereof claim 1 , alkyl S claim 1 ,S-lactyllactate and/or alkyl S-lactate claim 1 , and wherein the intermediate is produced by:(i) subjecting the initial compound to stereoisomerisation conditions; and(ii) converting at least a portion of the product of step (i) into the intermediate.4. The process as claimed in claim 3 , wherein the initial compound comprises oligomeric-S-lactic acid claim 3 , wherein the oligomeric S-lactic acid is produced from S-lactic acid claim 3 , and wherein step (i) comprises contacting the oligomeric S-lactic acid with a tertiary amine stereoisomerisation catalyst at a temperature of from about 100° C. to about 200° C. to produce oligomeric lactic acid.5. The process as claimed in claim 4 , wherein step (ii) comprises converting at least a portion of the oligomeric lactic acid into R claim 4 ,R- and S claim 4 ,S-lactide by heating at a temperature of from about 160° C. to about 240° C. in the presence of a Lewis acid catalyst comprising an oxide claim 4 , alkoxide or carboxylate salt of a metal.6. The process as claimed in claim 2 , wherein tertiary amine ...

PROCESS FOR THE PRODUCTION OF FURANIC COMPOUNDS COMPRISING AT LEAST ONE AMINE FUNCTION

Disclosed is a process for the production of furanic compound comprising at least one amine function, comprising reacting a furanic compound having at least one hydroxyl function or at least one aldehyde function with a second reactant having an amine function, in the presence of an iridium catalyst. 2. The process according to claim 1 , wherein the first reactant is selected from the group consisting of: furfuryl alcohol claim 1 , furfural claim 1 , 2 claim 1 ,5-bis(hydroxymethyl)furan claim 1 , 5-hydroxymethyl furfural (HMF) claim 1 , furan-2 claim 1 ,5-dicarbaldehyde and furanose.3. The process according to claim 1 , wherein R represents an alkyl claim 1 , alkenyl claim 1 , aryl claim 1 , cycloalkyl or heterocyclic group.4. The process according to claim 1 , wherein the second reactant is selected from the group consisting of: n-heptylamine claim 1 , methylamine claim 1 , allylamine claim 1 , benzylamine claim 1 , 3-phenylprop-2-enylamine claim 1 , cyclohexanamine claim 1 , and (tetrahydrofuran-2-yl)methanamine.5. The process according to claim 1 , wherein the molar ratio of first reactant to second reactant is from 1 to 5.6. The process according to claim 1 , wherein the reductant agent is hydrogen or a secondary alcohol.7. The process according to claim 1 , wherein molar ratio of first reactant to the reductant agent is from 1 to 10.8. The process according to claim 1 , wherein the compound of formula (III) is a (pentamethylcyclopentadienyl)-iridium-ammine iodide claim 1 , chloride or bromide complex.9. The process according to claim 1 , wherein molar amount of catalyst of formula (II) or (III) is from 0.1 to 10 molar % claim 1 , in relation with the molar amount of first reactant.10. The process according to claim 1 , wherein the furanic compound comprising at least one amine function is selected from the group consisting of: N-phenylbenzylamine claim 1 , (tetrahydrofuran-2 claim 1 ,5-diyl) dimethanamine claim 1 , (furan-2 claim 1 ,5-diyl) dimethanamine claim ...

LIQUID CRYSTAL COMPOUND HAVING 2, 6-DIFLUOROPHENYL ETHER STRUCTURE AND LIQUID CRYSTAL COMPOSITION THEREOF

The present invention relates to a compound having 2,6-difluorophenyl ether structure and useful as an organic electronic material and a medicine/agrochemical, particularly a material for liquid crystal display devices, and also relates to an effective method for producing the same. The present invention provides a compound represented by general formula (1) 3. The compound according to claim 1 , wherein in the general formula (1) claim 1 , Z claim 1 , Z claim 1 , Z claim 1 , and Zeach independently represent —OCF— claim 1 , —CFO— claim 1 , —CHCH— claim 1 , —C≡C— claim 1 , or a single bond.4. The compound according to claim 1 , wherein in the general formula (I) W represents a fluorine atom a cyano group claim 1 , or —OCF.8. A liquid crystal composition comprising one or two or more compounds according to .9. A liquid crystal display device using the liquid crystal composition according to . The present invention relates to a compound having a 2,6-difluorophenyl ether structure useful as an organic electronic material and a medicine/agrochemical, particularly a material for liquid crystal display devices, and also relates to an effective, method for producing the same.Liquid crystal display devices have been used for watches and electronic calculators, various measuring apparatuses, automotive panels, word processors, electronic notebooks, printers, computers, televisions, watches, advertising displays, etc. Typical examples of a liquid crystal display mode include a TN (twisted nematic) mode, a STN (super twisted nematic) mode, a vertical alignment mode using TFT (thin-film transistor), an IPS (in-plane switching) mode, and the like. Liquid crystal compositions used for these liquid crystal display devices are required to have stability to external factors such as moisture, air, heat, light, and the like, exhibit a liquid crystal phase (a nematic phase, a smectic phase, a blue, phase, and the like) within as wide a temperature range as possible including room ...

METHOD AND DEVICE FOR MANUFACTURING LACTIDE

A method and a device for manufacturing lactide, whereby crude lactide, being prepared by means of depolymerization of lactic acid oligomers, is purified by means of a distillation step. The prepared crude lactide is maintained for a period of at least 5 hours in a reaction vessel at a temperature between 97° C. and 200° C. prior to the distillation step. Keeping the lactide during a period of time in a reaction vessel leads to a decrease of the lactic acid content and an increase of the lactic acid oligomer concentration, so that the resulting crude lactide can be more efficiently purified during subsequent distillation. A pre-distilling step gives additional advantages. 1. Method for manufacturing lactide , whereby crude lactide , being prepared by means of depolymerization of lactic acid oligomers , is purified by means of a distillation step , wherein , prior to the distillation step , the prepared crude lactide is maintained for a period of at least 5 hours in a reaction vessel at a temperature between 97° C. and 200° C.2. Method according to claim 1 , wherein the crude lactide is maintained for at least 10 hours in the reaction vessel.3. Method according to claim 1 , wherein the reaction vessel is designed as a continuous stirred-tank reactor.4. Method according to claim 3 , wherein the reaction vessel is designed as a series of at least two continuous stirred-tank reactors claim 3 , and that the crude lactide is transported through this series of reactors.5. Method according to claim 1 , wherein the reaction vessel is designed as a plug flow reactor.6. Method according to claim 1 , wherein the crude lactide is maintained in the reaction vessel under ambient pressure.7. Method according to claim 1 , wherein the temperature of the lactide in the reaction vessel(s) ranges between 100° C. and 150° C.8. Method according to claim 1 , wherein a pre-distillation step is performed on the crude lactide between the preparation of the crude lactide and the maintenance of ...