INHIBITORS OF THE INFLUENZA A VIRUS M2 PROTON CHANNEL

Provided are compounds that are capable of modulating the activity of the influenza A virus via interaction with the M2 transmembrane protein. Also provided are methods for treating an influenza A-affected disease state or infection comprising administering a composition comprising one or more compounds that have been identified as being capable of interaction with the M2 protein. 2. The compound according to wherein X and Y are each independently methylene or ethylene.3. The compound according to wherein X is methylene and Y is ethylene.4. The compound according to wherein at least one of Rand Ris hydrogen.5. The compound according to wherein one of Rand Ris carbonyl claim 4 , amino claim 4 , carboxyl claim 4 , cyano claim 4 , or —CH(R)(R).6. The compound according to wherein n is 1 or 2 claim 5 , except that if n is 1 claim 5 , both X and Y are methylene claim 5 , and both Rand Rare hydrogen claim 5 , then one of Rand Ris not carbonyl.7. The compound according to wherein one of Rand Ris —CH(R)(R).8. The compound according to wherein one of Rand Ris amino10. A composition comprising a compound according to and a pharmaceutically acceptable carrier claim 1 , diluent claim 1 , or excipient. This application is a divisional of U.S. Ser. No. 12/848,197, filed Aug. 1, 2010 (now allowed), the entire contents of which are hereby incorporated herein by reference.The present invention pertains to, among other things, compounds and methods for modulating the activity of the influenza virus.The M2 protein is found in the viral envelope of influenza A virus and functions as a highly selective, pH-regulated proton channel important for the life cycle of the virus. Unlike neuraminidase inhibitors, rimantadine and amantadine are anti-viral agents capable of blocking the tetrameric M2 channel. In 2006, the CDC issued an alert instructing clinicians to avoid using M2 ion-channel inhibitors during influenza season due to the extraordinarily high frequency of amantadine resistance in ...

PROCESS FOR THE PREPARATION OF 4-(8-(2-CHLOROPHENOXY)-[1,2,4]TRIAZOLO[4,3-A]PYRIDIN-3-YL)BICYCLO[2.2.1]HEPTAN-1-OL AND NOVEL INTERMEDIATES THEREFOR

A process is provided for preparing 4-(8-(2-chlorophenoxy)-[1,2,4]triazolo[4,3-a]pyridin-3-yl)bicyclo[2.2.1]heptan-1-ol and novel intermediates used in the process. The compound is a 11-beta hydroxysteroid dehydrogenase type I inhibitor which exhibits activity in the treatment of various metabolic diseases. 6. The process as defined in where the oxidation is carried out in the presence of sodium chlorite claim 4 , 2 claim 4 ,2 claim 4 ,6 claim 4 ,6-tetramethylpiperidine-N-oxide and sodium hypochlorite.8. The process as defined in wherein the reaction is carried out under an inert atmosphere at a temperature within the range from about 0 to about 5° C.10. The process as defined in wherein the carboxylic acid is benzoic acid and the reaction is carried out at a temperature within the range from about 105 to 110° C. This application claims priority to U.S. Provisional Application Ser. No. 62/033,695, filed Aug. 6, 2014; the entire content of which is incorporated herein reference.The invention generally relates to novel intermediates and an improved process for the preparation of 4-(8-(2-chlorophenoxy)-[1,2,4]triazolo[4,3-a]pyridin-3-yl)bicyclo[2.2.1]heptan-1-ol, a 11-beta hydroxysteroid dehydrogenase type I inhibitor which was recently in clinical trials for the treatment of type 2 diabetes, obesity, and the metabolic syndrome.The steroid hormone cortisol is a key regulator of many physiological processes. However, an excess of cortisol, as occurs in Cushing's Disease, provokes severe metabolic abnormalities including: type 2 diabetes, cardiovascular disease, obesity, and osteoporosis. Many patients with these diseases, however, do not show significant increases in plasma cortisol levels. In addition to plasma cortisol, individual tissues can regulate their glucocorticoid tone via the in situ conversion of inactive cortisone to the active hormone cortisol. Indeed, the normally high plasma concentration of cortisone provides a ready supply of precursor for conversion ...

HIGH ASPECT RATIO LAYERED DOUBLE HYDROXIDE MATERIALS AND METHODS FOR PREPARATION THEREOF

Embodiments are directed to adamantane-intercalated layered double-hydroxide (LDH) particles and the methods of producing adamantane-intercalated LDH particles. The adamantane-intercalated LDH particles have a general formula defined by [MAl(OH)](A).mHO, where x is from 0.14 to 0.33, m is from 0.33 to 0.50, M is chosen from Mg, Ca, Co, Ni, Cu, or Zn, and A is adamantane carboxylate. The adamantane-intercalated LDH particles further have an aspect ratio greater than 100. The aspect ratio is defined by the width of an adamantane-intercalated LDH particle divided by the thickness of the adamantane-intercalated LDH particle. 1. An adamantane-intercalated layered double-hydroxide (LDH) material in a form of adamantane-intercalated LDH particles , where the adamantane-intercalated LDH particles comprise:{'sub': 1-x', 'x', '2', 'x', '2, 'a general formula defined by [MAl(OH)](A).mHO, where x is from 0.14 to 0.33, m is from 0.33 to 0.50, M is chosen from Mg, Ca, Co, Ni, Cu, or Zn, and A is adamantane carboxylate; and'}an aspect ratio greater than 100, the aspect ratio defined by a width of an adamantane-intercalated LDH particle divided by a thickness of the adamantane-intercalated LDH particle.2. The adamantane-intercalated LDH material of where M is Mg.3. The adamantane-intercalated LDH material of where the aspect ratio is greater than 125.4. The adamantane-intercalated LDH material of where the aspect ratio is greater than 150.5. The adamantane-intercalated LDH material of where the aspect ratio is greater than 200.6. The adamantane-intercalated LDH material of where the adamantane-intercalated LDH particles have a particle diameter of 5 to 10 μm.7. The adamantane-intercalated LDH material of where the adamantane-intercalated LDH particles have characteristic peaks in an IR spectra at 1517 cm claim 1 , 1395 cm claim 1 , 2901 cm claim 1 , 2847 cm claim 1 , and 4302 cm. This application is a divisional application of U.S. patent application Ser. No. 15/449,207 filed Mar. ...

Radiolabelling Process

The present invention relates to a novel composition comprising 1-amino-3[F]-fluorocyclobutanecarboxylic acid ([F]-FACBC) wherein said composition has certain superior properties in comparison with known compositions comprising [F]-FACBC. Also provided by the invention is a method to obtain said composition. 2. The method as defined in wherein said concentration of MeCN in said composition is no greater than 20 μg/mL.3. The method as defined in either wherein said composition has a radioactive concentration (RAC) of between 500-5000 MBq/ml.4. The composition as defined in wherein said composition has a RAC of between 1000-5000 MBq/ml.5. The composition as defined in wherein said composition has a radiochemical purity of at least 99%.7. The method as defined wherein LG is a linear or branched Chaloalkyl sulfonic acid substituent claim 1 , a linear or branched Calkyl sulfonic acid substituent claim 1 , a fluorosulfonic acid substituent claim 1 , or an aromatic sulfonic acid substituent.8. The method as defined in wherein LG is methanesulfonic acid claim 7 , toluenesulfonic acid claim 7 , nitrobenzenesulfonic acid claim 7 , benzenesulfonic acid claim 7 , trifluoromethanesulfonic acid claim 7 , fluorosulfonic acid claim 7 , or perfluoroalkylsulfonic acid.9. The method as defined in wherein LG is trifluoromethanesulfonic acid.10. The method as defined in wherein PGis a linear or branched Calkyl chain or an aryl substituent.11. The method as defined in wherein PGis methyl claim 10 , ethyl claim 10 , t-butyl and phenyl.12. The method as defined in wherein PGis methyl or ethyl.13. The method as defined in wherein PGis ethyl.14. The method as defined in wherein PGis a carbamate substituent claim 1 , an amide substituent claim 1 , an imide substituents claim 1 , or an amine substituents.15. The method as defined in wherein PGis t-butoxycarbonyl claim 14 , allyloxycarbonyl claim 14 , phthalimide claim 14 , or N-benzylideneamine.16. The method as defined in wherein PGis t- ...

CYCLOALKYL-HYDROXYL COMPOUNDS AND COMPOSITIONS FOR CHOLESTEROL MANAGEMENT AND RELATED USES

The present invention relates to novel cycloalkyl-hydroxyl compounds, compositions comprising hydroxyl compounds, and methods useful for treating and preventing a variety of diseases and conditions such as, but not limited to aging, Alzheimer's Disease, cancer, cardiovascular disease, diabetic nephropathy, diabetic retinopathy, a disorder of glucose metabolism, dyslipidemia, dyslipoproteinemia, hypertension, impotence, inflammation, insulin resistance, lipid elimination in bile, obesity, oxysterol elimination in bile, pancreatitis, Parkinson's disease, a peroxisome proliferator activated receptor-associated disorder, phospholipid elimination in bile, renal disease, septicemia, Syndrome X, thrombotic disorder. Compounds and methods of the invention can also be used to modulate C reactive protein or enhance bile production in a patient. In certain embodiments, the compounds, compositions, and methods of the invention are useful in combination therapy with other therapeutics, such as hypocholesterolemic and hypoglycemic agents. 2. The compound of claim 1 , wherein each occurrence of Yand Yis independently OH claim 1 , COOR claim 1 , or COOH.3. The compound of claim 1 , wherein m is 0.4. The compound of claim 1 , wherein m is 1.5. The compound of claim 1 , wherein n is 4.6. The compound of claim 1 , wherein n is 5.7. The compound of claim 1 , wherein X is (CH)and z is 0.8. The compound of claim 1 , wherein each occurrence of Rand Rand the carbon to which they are both attached are taken together to form a (C-C)cycloakyl group.9. The compound of claim 1 , wherein Yand Yare each independently (C-C)alkyl.10. The compound of claim 1 , wherein Yand Yare each methyl.1157-. (canceled) This application claims the benefit of U.S. Provisional Application No. 60/441,795, filed Jan. 23, 2003, which is incorporated herein by reference in its entirety.The invention relates to cycloalkyl-hydroxyl compounds and pharmaceutically acceptable salts, hydrates, solvates, and mixtures thereof ...

MULTIPLE-COMPONENT SOLID PHASES CONTAINING AT LEAST ONE ACTIVE PHARMACEUTICAL INGREDIENT

The subject invention concerns a method for identifying complementary chemical functionalities to form a desired supramolecular synthon. The subject invention also pertains to binary phase compositions comprising one or more pharmaceutical entities and methods for producing such compositions. 136-. (canceled)37. A pharmaceutical composition comprising a pharmaceutically acceptable carrier and a therapeutically effective amount of a co-crystal comprising supramolecular synthons , each supramolecular synthon formed from stoichiometric amounts of at least one active pharmaceutical ingredient (API) and at least one co-former ,wherein the API has a first chemical functionality that permits formation of API homosynthons through non-covalent hydrogen bonding when the API is in its pure form,wherein the co-former has a second chemical functionality complimentary to the first chemical functionality via non-covalent hydrogen bonding,wherein said co-former is a solid at room temperature and atmospheric pressure when the co-former is in its pure form,wherein said co-former is not an API, andwherein supramolecular synthons are formed via non-covalent hydrogen bonding between the first chemical functionality of the API and the second chemical functionality of the co-former.38. The pharmaceutical composition of claim 37 , wherein the supramolecular synthon comprises a supramolecular heterosynthon dimer formed by non-covalent hydrogen bonding of the API to the co-former.39. The pharmaceutical composition of claim 37 , wherein the supramolecular synthon comprises a plurality of the API and a plurality of the co-former claim 37 , wherein the supramolecular synthon is a chain of supramolecular heterosynthons claim 37 , each supramolecular heterosynthon formed by non-covalent hydrogen bonding of one API to one co-former claim 37 , and wherein the supramolecular heterosynthons are bonded to one another by non-covalent hydrogen bonding.40. The pharmaceutical composition of claim 37 , ...

CYCLOALKYL-HYDROXYL COMPOUNDS AND COMPOSITIONS FOR CHOLESTEROL MANAGEMENT AND RELATED USES

The present invention relates to novel cycloalkyl-hydroxyl compounds, compositions comprising hydroxyl compounds, and methods useful for treating and preventing a variety of diseases and conditions such as, but not limited to aging, Alzheimer's Disease, cancer, cardiovascular disease, diabetic nephropathy, diabetic retinopathy, a disorder of glucose metabolism, dyslipidemia, dyslipoproteinemia, hypertension, impotence, inflammation, insulin resistance, lipid elimination in bile, obesity, oxysterol elimination in bile, pancreatitis, Parkinson's disease, a peroxisome proliferator activated receptor-associated disorder, phospholipid elimination in bile, renal disease, septicemia, Syndrome X, thrombotic disorder. Compounds and methods of the invention can also be used to modulate C reactive protein or enhance bile production in a patient. In certain embodiments, the compounds, compositions, and methods of the invention are useful in combination therapy with other therapeutics, such as hypocholesterolemic and hypoglycemic agents. 157-. (canceled)59. The method claim 58 , wherein each occurrence of Yand Yis independently COORor COOH.60. The method of claim 59 , wherein m is 0.61. The method of claim 59 , wherein m is 1.62. The method of claim 59 , wherein n is 4.63. The method of claim 59 , wherein n is 5.64. The method of claim 59 , wherein X is (CH2)and z is 0.67. The method of claim 58 , the method further comprising administering to a patient in need of such treatment a therapeutically effective amount of a second therapeutic agent.68. The method of claim 67 , wherein the second therapeutic agent is selected from the group consisting of a chemotherapeutic agent claim 67 , an alkylating agent claim 67 , a plant alkaloid claim 67 , a DNA topoisomerase inhibitor claim 67 , a mitomycin claim 67 , an anti-folate claim 67 , a pyrimidine analog claim 67 , a purine analog claim 67 , a hormonal therapy claim 67 , a retinoid claim 67 , a deltoid claim 67 , a vitamin D3 analog ...

RESIST COMPOSITION AND PATTERNING PROCESS

A resist composition comprising a base polymer and a quencher containing a sulfonium salt having an iodized benzene ring offers a high sensitivity, minimal LWR and improved CDU independent of whether it is of positive or negative tone. 2. The resist composition of wherein m is an integer of 2 to 5.3. The resist composition of claim 1 , further comprising an organic solvent.4. The resist composition of claim 1 , further comprising an acid generator capable of generating a fluorosulfonic acid claim 1 , fluoroimidic acid or fluoromethide acid.5. The resist composition of claim 1 , further comprising a base polymer.7. The resist composition of which is a chemically amplified positive resist composition.8. The resist composition of wherein the base polymer is free of an acid labile group.9. The resist composition of which is a chemically amplified negative resist composition.11. The resist composition of claim 1 , further comprising a surfactant.12. A process for forming a pattern comprising the steps of applying the resist composition of onto a substrate claim 1 , baking to form a resist film claim 1 , exposing the resist film to high-energy radiation claim 1 , and developing the exposed resist film in a developer.13. The process of wherein the high-energy radiation is ArF excimer laser radiation of wavelength 193 nm or KrF excimer laser radiation of wavelength 248 nm.14. The process of wherein the high-energy radiation is EB or EUV of wavelength 3 to 15 nm. This non-provisional application claims priority under 35 U.S.C. § 119(a) on Patent Application No. 2018-173598 filed in Japan on Sep. 18, 2018, the entire contents of which are hereby incorporated by reference.This invention relates to a resist composition and a pattern forming process.To meet the demand for higher integration density and operating speed of LSIs, the effort to reduce the pattern rule is in rapid progress. In particular, the enlargement of the logic memory market to comply with the wide-spread use ...

SALTS AND CRYSTALLINE FORMS OF A PD-1/PD-L1 INHIBITOR

This application relates to solid forms and salt forms of the PD-1/PD-L1 inhibitor 4,4′-(((((2,2′-dichloro-[1,1′-biphenyl]-3,3′-diyl)bis(azanediyl))bis(carbonyl))bis(1-methyl-1,4,6,7-tetrahydro-5H-imidazo[4,5-c]pyridine-2,5-diyl))bis(ethane-2,1-diyl))bis(bicyclo[2.2.1]heptane-1-carboxylic acid), including processes of preparation thereof, where the solid forms and salt forms are useful in the treatment of various diseases including infectious diseases and cancer. 1. A salt , which is 4 ,4′-(((((2 ,2′-dichloro-[1 ,1′-biphenyl]-3 ,3′-diyl)bis(azanediyl))bis(carbonyl))bis(1-methyl-1 ,4 ,6 ,7-tetrahydro-5H-imidazo[4 ,5-c]pyridine-2 ,5-diyl))bis(ethane-2 ,1-diyl))bis(bicyclo[2.2.1]heptane-1-carboxylic acid) di-hydrochloric acid salt.2. The salt of claim 1 , having Form I.3. The salt of claim 2 , having an X-ray powder diffraction pattern as substantially shown in .4. The salt of claim 2 , having a DSC thermogram substantially as depicted in .5. The salt of claim 2 , having a thermogravimetric analysis (TGA) thermogram substantially as depicted in .6. The salt of claim 2 , having at least one X-ray powder diffraction (XRPD) peak claim 2 , in terms of 2-theta (±0.2 degrees) claim 2 , selected from 5.7 claim 2 , 8.5 claim 2 , 9.6 claim 2 , 9.9 claim 2 , 11.8 claim 2 , 12.3 claim 2 , 13.1 claim 2 , 13.4 claim 2 , 13.8 claim 2 , 14.2 claim 2 , 14.5 claim 2 , 15.4 claim 2 , 15.8 claim 2 , 16.8 claim 2 , 17.3 and 17.6 degrees.7. The salt of claim 2 , having at least two X-ray powder diffraction (XRPD) peaks claim 2 , in terms of 2-theta (±0.2 degrees) claim 2 , selected from 5.7 claim 2 , 8.5 claim 2 , 9.6 claim 2 , 9.9 claim 2 , 11.8 claim 2 , 12.3 claim 2 , 13.1 claim 2 , 13.4 claim 2 , 13.8 claim 2 , 14.2 claim 2 , 14.5 claim 2 , 15.4 claim 2 , 15.8 claim 2 , 16.8 claim 2 , 17.3 and 17.6 degrees.8. The salt of claim 2 , having at least three X-ray powder diffraction (XRPD) peaks claim 2 , in terms of 2-theta (±0.2 degrees) claim 2 , selected from 5.7 claim 2 , 8.5 claim 2 , ...

Cycloalkyl-hydroxyl compounds and compositions for cholesterol management and related uses

The present invention relates to novel cycloalkyl-hydroxyl compounds, compositions comprising hydroxyl compounds, and methods useful for treating and preventing a variety of diseases and conditions such as, but not limited to aging, Alzheimer's Disease, cancer, cardiovascular disease, diabetic nephropathy, diabetic retinopathy, a disorder of glucose metabolism, dyslipidemia, dyslipoproteinemia, hypertension, impotence, inflammation, insulin resistance, lipid elimination in bile, obesity, oxysterol elimination in bile, pancreatitis, Parkinson's disease, a peroxisome proliferator activated receptor-associated disorder, phospholipid elimination in bile, renal disease, septicemia, Syndrome X, thrombotic disorder. Compounds and methods of the invention can also be used to modulate C reactive protein or enhance bile production in a patient. In certain embodiments, the compounds, compositions, and methods of the invention are useful in combination therapy with other therapeutics, such as hypocholesterolemic and hypoglycemic agents.

Multiple-component solid phases containing at least one active pharmaceutical ingredient

The subject invention concerns a method for identifying complementary chemical functionalities to form a desired supramolecular synthon. The subject invention also pertains to multiple-component phase compositions comprising one or more pharmaceutical entities and methods for producing such compositions.

Radiolabelling Process

The present invention relates to a novel composition comprising 1-amino-3-[F]-fluorocyclobutanecarboxylic acid ([F]-FACBC) wherein said composition has certain superior properties in comparison with known compositions comprising [F]-FACBC. Also provided by the invention is a method to obtain said composition. 1. A composition comprising 1-amino-3-[F] fluorocyclobutanecarboxylic acid ([F]-FACBC) and no greater than 50 μg/mL acetonitrile (MeCN).2. The composition of claim 1 , wherein said concentration of MeCN is no greater than 20 μg/mL.3. The composition of claim 1 , having a radioactive concentration (RAC) of between 500-5000 MBq/mL.4. The composition of claim 1 , having a RAC between 1000-5000 MBq/mL.5. The composition of claim 1 , having a radiochemical purity of at least 99%.7. The composition of claim 6 , wherein said concentration of MeCN is no greater than 20 μg/mL.8. The composition of claim 6 , having a radioactive concentration (RAC) of between 500-5000 MBq/mL.9. The composition of claim 6 , having a RAC between 1000-5000 MBq/mL.10. The composition of claim 6 , having a radiochemical purity of at least 99%. The invention relates to a method for the preparation of a radiopharmaceutical compound, in particular an amino acid derivative useful as a positron emission tomography (PET) tracer. The method of the invention is especially suitable when automated and offers advantages over known methods. Particularly, the invention relates to a method for preparation of [F]-1-amino-3-fluorocyclobutane-1-carboxylic acid ([F]-FACBC, also known as [F]-fluciclovine).The non-natural amino acid [F]-1-amino-3-fluorocyclobutane-1-carboxylic acid ([F]-FACBC, also known as [F]-Fluciclovine) is taken up specifically by amino acid transporters and has shown promise for tumour imaging with positron emission tomography (PET).A known synthesis of [F]-FACBC (EP2017258) begins with the provision of the protected precursor compound 1-(N-(t-butoxycarbonyl)amino)-3-[((trifluoromethyl) ...

NEUROACTIVE SUBSTITUTED CYCLOPENT[a]ANTHRACENES AS MODULATORS FOR GABA TYPE-A RECEPTORS

The present disclosure is generally directed to neuroactive substituted cyclopent[a]anthracenes as referenced herein, and pharmaceutically acceptable salts thereof, for use as, for example, an anesthetic, and/or in the treatment of disorders relating to GABA function and activity. The present disclosure is further directed to pharmaceutical compositions comprising such compounds. 2. The compound of claim 1 , wherein Ris H.3. The compound of claim 1 , wherein Ris ═O.4. The compound of claim 1 , wherein Ris spiroepoxy.5. The compound of claim 1 , wherein Ris β-CN.6. The compound of claim 1 , wherein R claim 1 , R claim 1 , R claim 1 , R claim 1 , R claim 1 , R claim 1 , and Rare H.7. The compound of claim 1 , wherein Ris methyl.8. The compound of claim 1 , wherein Ris H.9. The compound of claim 8 , wherein Ris in the alpha configuration.10. The compound of claim 1 , wherein a double bond is present between C-C.11. The compound of claim 10 , wherein Ris CN.17. A pharmaceutical composition comprising the compound of claim 1 , a pharmaceutically acceptable salt thereof claim 1 , or a combination of two or more thereof claim 1 , and a pharmaceutically acceptable carrier.18. A method of inducing anesthesia in a subject in need thereof claim 1 , said method comprising administering to the subject a therapeutically effective amount of the compound of claim 1 , or a pharmaceutically acceptable salt thereof.19. A method for treating disorders related to GABA function in a subject in need thereof claim 1 , said method comprising administering to the subject a therapeutically effective amount of the compound of claim 1 , or a pharmaceutically acceptable salt thereof.20. The method of claim 19 , wherein the disorder is selected from the group consisting of insomnia claim 19 , mood disorders claim 19 , convulsive disorders claim 19 , Fragile X syndrome claim 19 , anxiety claim 19 , or symptoms of ethanol withdrawal. This application claims priority benefit of U.S. Provisional ...

CYCLOALKYL-HYDROXYL COMPOUNDS AND COMPOSITIONS FOR CHOLESTEROL MANAGEMENT AND RELATED USES

The present invention relates to novel cycloalkyl-hydroxyl compounds, compositions comprising hydroxyl compounds, and methods useful for treating and preventing a variety of diseases and conditions such as, but not limited to aging, Alzheimer's Disease, cancer, cardiovascular disease, diabetic nephropathy, diabetic retinopathy, a disorder of glucose metabolism, dyslipidemia, dyslipoproteinemia, hypertension, impotence, inflammation, insulin resistance, lipid elimination in bile, obesity, oxysterol elimination in bile, pancreatitis, Parkinson's disease, a peroxisome proliferator activated receptor-associated disorder, phospholipid elimination in bile, renal disease, septicemia, Syndrome X, thrombotic disorder. Compounds and methods of the invention can also be used to modulate C reactive protein or enhance bile production in a patient. In certain embodiments, the compounds, compositions, and methods of the invention are useful in combination therapy with other therapeutics, such as hypocholesterolemic and hypoglycemic agents. 157-. (canceled)59. The method claim 58 , wherein each occurrence of Yand Yis independently COORor COOH.60. The method of claim 58 , wherein Yand Yare each COOH.61. The method of claim 58 , wherein m is 0.62. The method of claim 58 , wherein m is 1.63. The method of claim 58 , wherein n is 4.64. The method of claim 58 , wherein n is 5.65. The method of claim 58 , wherein X is (CH)and z is 0.68. The method of claim 58 , wherein the compound of formula I is orally administered to the patient in the form of a pharmaceutical composition comprising the compound of formula I claim 58 , and a pharmaceutically acceptable vehicle.71. The method of claim 69 , wherein the compound of formula I is orally administered to the patient in the form of a pharmaceutical composition comprising the compound of formula I claim 69 , and a pharmaceutically acceptable vehicle.72. The method of claim 70 , wherein the compound is orally administered to the patient in the ...

Method for preparing 3(4),8(9)-bisformyltricyclo[5.2.1.0^2,6]decane

A method of preparing 3(4),8(9)-bisformyltricyclo[5.2.1.0 2,6 ]decane is provided. According to the present invention, 3(4),8(9)-bisformyltricyclo[5.2.1.0 2,6 ]decane (TCDDA) may be prepared with a high conversion rate and purity without a separate catalyst recovery process.

Polyphenolic selenium compound having functional group of alkali metal ion and selenium complex

A polyphenolic selenium compound having a functional group of alkali metal ion and selenium complex which has an aromatic ring is provided, wherein the aromatic ring comprises at least two functional groups, each of which is one member selected from the group consisting of oxygen functional group, sulphur functional group, phosphorus functional group and nitrogen functional group; and selenium complex functional group is formed by selenium, alkali metal ion and the functional group. The polyphenolic selenium compound having a functional group of alkali metal ion and selenium complex of the present invention has characteristics of over 20% selenium content and no toxicity. Because it has revolutionary effects in killing bacteria, virus and cancer cell, enhancing human immunity, removing oxygen free radicals and etc., it holds a vital medicinal value.

NANODIAMONDS HAVING ACID FUNCTIONAL GROUP AND METHOD FOR PRODUCING SAME

A nanodiamond according to the present invention has acidic functional groups, contains the acidic functional groups in a number density of 1 or more per square nanometer in the nanodiamond surface, and has a specific surface area of 150 m/g or more. Particles of the nanodiamond preferably have a D50 (median diameter) of 9 nm or less. The nanodiamond is preferably derived from a nanodiamond synthesized by a detonation technique (in particular, an air-cooling detonation technique). 1. A nanodiamond having acidic functional groups ,the nanodiamond comprising the acidic functional groups in a number density of 1 or more per square nanometer in a surface of the nanodiamond,{'sup': '2', 'the nanodiamond having a specific surface area of 150 m/g or more.'}2. The nanodiamond according to claim 1 ,wherein particles of the nanodiamond have a D50 of 9 nm or less.3. The nanodiamond according to one of and claim 1 ,wherein the nanodiamond is a detonation nanodiamond.4. The nanodiamond according to claim 1 ,wherein the nanodiamond is an air-cooled detonation nanodiamond.5. The nanodiamond according to claim 1 ,wherein the nanodiamond is a nanodiamond obtained by subjecting a nanodiamond having an acidic functional group content of 0.15 mmol/g or more to an oxidation treatment.6. A method for producing the nanodiamond according to claim 1 , the method comprising the step ofA) subjecting a material nanodiamond to an oxidation treatment with at least one oxidizer selected from the group consisting of chromic acid, chromic anhydride, dichromic acid, permanganic acid, perchloric acid, salts of these acids, and hydrogen peroxide, the material nanodiamond being synthesized by a detonation technique and having an acidic functional group content of 0.15 mmol/g or more.7. The method according to for producing a nanodiamond claim 6 ,wherein the oxidation treatment in the step A) is performed in coexistence of sulfuric acid.8. The method according to one of and for producing a nanodiamond ...

RESIST COMPOSITION AND PATTERN FORMING PROCESS

A resist composition comprising a quencher containing a sulfonium salt having the formula (A). 2. The resist composition of claim 1 , further comprising an organic solvent.3. The resist composition of claim 1 , further comprising an acid generator capable of generating fluorosulfonic acid claim 1 , fluoroimidic acid claim 1 , or fluoromethide acid.4. The resist composition of claim 1 , further comprising a base polymer.6. The resist composition of which is a chemically amplified positive resist composition.7. The resist composition of claim 4 , wherein the base polymer is free of an acid labile group.8. The resist composition of which is a chemically amplified negative resist composition.10. The resist composition of claim 1 , further comprising a surfactant.11. A pattern forming process comprising the steps of applying the resist composition of to form a resist film on a substrate claim 1 , exposing the resist film to high-energy radiation claim 1 , and developing the exposed resist film in a developer.12. The pattern forming process of claim 11 , wherein the high-energy radiation is ArF excimer laser radiation of wavelength 193 nm or KrF excimer laser radiation of wavelength 248 nm.13. The pattern forming process of claim 11 , wherein the high-energy radiation is electron beam or extreme ultraviolet of wavelength 3 to 15 nm. This non-provisional application claims priority under 35 U.S.C. § 119(a) on Patent Application No. 2020-031900 filed in Japan on Feb. 27, 2020, the entire contents of which are hereby incorporated by reference.This invention relates to a resist composition and a pattern forming process.As integration density and operating speed of LSIs become higher, the effort to make the pattern rule finer is in rapid progress. In particular, the enlargement of the logic memory market to comply with the wide-spread use of smartphones drives forward the miniaturization technology. As the advanced miniaturization technology, manufacturing of microelectronic ...

Synthesis of transition-metal adamantane salts and oxide nanocomposites, and systems and methods including the salts or the nanocomposites

A method for preparing a transition-metal adamantane carboxylate salt is presented. The method includes mixing a transition-metal hydroxide and a diamondoid compound having at least one carboxylic acid moiety to form a reactant mixture, where M is a transition metal. Further, the method includes hydrothermally treating the reactant mixture at a reaction temperature for a reaction time to form the transition-metal adamantane carboxylate salt.

Synthesis of magnesium adamantane salts and magnesium oxide nanocomposites, and systems and methods including the salts or the nanocomposites

A method for preparing a magnesium adamantane carboxylate salt is provided. The method includes mixing a magnesium salt and a diamondoid compound having at least one carboxylic acid moiety to form a reactant mixture and hydrothermally treating the reactant mixture at a reaction temperature for a reaction time to form the magnesium adamantane carboxylate salt.

HIGH ASPECT RATIO LAYERED DOUBLE HYDROXIDE MATERIALS AND METHODS FOR PREPARATION THEREOF

Embodiments are directed to adamantane-intercalated layered double-hydroxide (LDH) particles and the methods of producing adamantane-intercalated LDH particles. The method comprises adding to an aqueous solution a first precursor and a second precursor to form an initial mixture, where the first precursor is Al(OH)or AlO, the second precursor is a hydroxide M(OH)or an oxide MO, where M is a metal of oxidation state +2; and the initial mixture has a M/Al molar ratio of from 1 to 5. The method also comprises adding to the initial mixture an amount of adamantane to form a reaction mixture having an Al/adamantane molar ratio of from 0.5 to 2; and heating the reaction mixture to produce adamantane-intercalated LDH particles, where the adamantane-intercalated LDH particles have aspect ratios greater than 100.

Hydroxyl compounds and compositions for cholesterol management and related uses

The present invention relates to novel hydroxyl compounds, compositions comprising hydroxyl compounds, and methods useful for treating and preventing a variety of diseases and conditions such as, but not limited to aging, Alzheimer's Disease, cancer, cardiovascular disease, diabetic nephropathy, diabetic retinopathy, a disorder of glucose metabolism, dyslipidemia, dyslipoproteinemia, hypertension, impotence, inflammation, insulin resistance, lipid elimination in bile, obesity, oxysterol elimination in bile, pancreatitis, pancreatitius, Parkinson's disease, a peroxisome proliferator activated receptor-associated disorder, phospholipid elimination in bile, renal disease, septicemia, metabolic syndrome disorders (e.g., Syndrome X), thrombotic disorder. Compounds and methods of the invention can also be used to modulate C reactive protein or enhance bile production in a patient. In certain embodiments, the compounds, compositions, and methods of the invention are useful in combination therapy with other therapeutics, such as hypocholesterolemic and hypoglycemic agents.

CYCLOALKYL-HYDROXYL COMPOUNDS AND COMPOSITIONS FOR CHOLESTEROL MANAGEMENT AND RELATED USES

The present invention relates to novel cycloalkyl-hydroxyl compounds, compositions comprising hydroxyl compounds, and methods useful for treating and preventing a variety of diseases and conditions such as, but not limited to aging, Alzheimer's Disease, cancer, cardiovascular disease, diabetic nephropathy, diabetic retinopathy, a disorder of glucose metabolism, dyslipidemia, dyslipoproteinemia, hypertension, impotence, inflammation, insulin resistance, lipid elimination in bile, obesity, oxysterol elimination in bile, pancreatitis, Parkinson's disease, a peroxisome proliferator activated receptor-associated disorder, phospholipid elimination in bile, renal disease, septicemia, Syndrome X, thrombotic disorder. Compounds and methods of the invention can also be used to modulate C reactive protein or enhance bile production in a patient. In certain embodiments, the compounds, compositions, and methods of the invention are useful in combination therapy with other therapeutics, such as hypocholesterolemic and hypoglycemic agents. 2. The compound of claim 1 , wherein each occurrence of Yand Yis independently OH claim 1 , COOR claim 1 , or COOH.3. The compound of claim 1 , wherein m is 0.4. The compound of claim 1 , wherein m is 1.5. The compound of claim 1 , wherein n is 4.6. The compound of claim 1 , wherein n is 5.7. The compound of claim 1 , wherein X is (CH)and z is 0.8. The compound of claim 1 , wherein each occurrence of Rand Rand the carbon to which they are both attached are taken together to form a (C-C)cycloakyl group.9. The compound of claim 1 , wherein Yand Yare each independently (C-C)alkyl.10. The compound of claim 1 , wherein Y and Yare each methyl.1157-. (canceled) This application claims the benefit of U.S. Provisional Application No. 60/441,795, filed Jan. 23, 2003, which is incorporated herein by reference in its entirety.The invention relates to cycloalkyl-hydroxyl compounds and pharmaceutically acceptable salts, hydrates, solvates, and mixtures ...

HYDROXYL COMPOUNDS AND COMPOSITIONS FOR CHOLESTEROL MANAGEMENT AND RELATED USES

The present invention relates to novel hydroxyl compounds, compositions comprising hydroxyl compounds, and methods useful for treating and preventing a variety of diseases and conditions such as, but not limited to aging, Alzheimer's Disease, cancer, cardiovascular disease, diabetic nephropathy, diabetic retinopathy, a disorder of glucose metabolism, dyslipidemia, dyslipoproteinemia, hypertension, impotence, inflammation, insulin resistance, lipid elimination in bile, obesity, oxysterol elimination in bile, pancreatitis, pancreatitius, Parkinson's disease, a peroxisome proliferator activated receptor-associated disorder, phospholipid elimination in bile, renal disease, septicemia, metabolic syndrome disorders (e.g., Syndrome X), thrombotic disorder. Compounds and methods of the invention can also be used to modulate C reactive protein or enhance bile production in a patient. In certain embodiments, the compounds, compositions, and methods of the invention are useful in combination therapy with other therapeutics, such as hypocholesterolemic and hypoglycemic agents. 12-. (canceled)46-. (canceled)7. The method of claim 3 , wherein each occurrence of Yand Yis independently OH claim 3 , COOR claim 3 , or COOH.8. The method of claim 3 , wherein m is 0.9. The method of claim 3 , wherein n is 5.10. The method of claim 3 , wherein z is 0.11. The method of claim 10 , wherein R claim 10 , R claim 10 , R claim 10 , and Rare (C-C)alkyl.12. The method of claim 11 , wherein Yand Yis COOH.16. The method of claim 15 , wherein each occurrence of Yand Yis independently OH claim 15 , COOR claim 15 , or COOH.17. The method of claim 15 , wherein m is 0.18. The method of claim 15 , wherein n is 5.19. The method of claim 15 , wherein z is 0.20. The method of claim 19 , wherein R claim 19 , R claim 19 , R claim 19 , and Rare (C-C)alkyl.21. The method of claim 20 , wherein Yand Yis COOH.24. The method of claim 15 , wherein the compound of formula I is orally administered to the human ...

Method for producing acid halide solution, mixed solution, and method for producing monoester compound

The present disclosure provides a method for producing an acid halide solution that is useful as a production intermediate or the like that allows industrially advantageous production of a polymerizable liquid crystal compound. The method for producing an acid halide solution of the present disclosure includes a step α of reacting a halogenating agent and a dicarboxylic acid compound in a water-immiscible organic solvent in the presence of a tetraalkylammonium salt to obtain a water-immiscible organic solvent solution including an acid halide, and a step β of concentrating the obtained water-immiscible organic solvent solution.

Multiple-component solid phases containing at least one active pharmaceutical ingredient

The subject invention concerns a method for identifying complementary chemical functionalities to form a desired supramolecular synthon. The subject invention also pertains to multiple-component phase compositions comprising one or more pharmaceutical entities and methods for producing such compositions.

NEW METHOD FOR SYNTHESIZING 2-FLUOROCYCLOPROPANE CARBOXYLIC ACID

Disclosed is a new method for synthesizing 2-fluorocyclopropanecarboxylic acid comprising: 1) performing reaction of 1,1-dichloro-1-fluoroethane with thiophenol in the presence of an alkali, to produce a phenyl sulfide intermediate; 2) performing oxidation reaction of the phenyl sulfide intermediate with Oxone; 3) performing elimination reaction of the product of Step 2) in the presence of an alkali, to obtain 1-fluoro-1-benzenesulfonyl ethylene; 4) performing addition reaction of the 1-fluoro-benzenesulfonyl ethylene with ethyl diazoacetate in the presence of a catalyst, to obtain a cyclopropane intermediate; 5) performing elimination reaction of the cyclopropane intermediate in the presence of an alkali before acidification, to obtain 2-fluorocyclopropanecarboxylic acid. Herein, the synthetic route is short, used materials are bulk commodities, and raw materials are inexpensive and readily available. The process can be safely scaled up by replacing commonly used mCPBA reagents with Oxone. Further, reaction yield is improved, production cost is greatly reduced, and operation is simplified. 1: A new method for synthesizing 2-fluorocyclopropanecarboxylic acid ,comprising the following steps:1) performing a reaction of 1,1-dichloro-1-fluoroethane with thiophenol in the presence of an alkali, to produce a phenyl sulfide intermediate;2) performing an oxidation reaction of the phenyl sulfide intermediate with Oxone;3) performing an elimination reaction of a product obtained in Step 2) in the presence of an alkali, to obtain 1-fluoro-1-benzenesulfonyl ethylene;4) performing an addition reaction of the 1-fluoro-1-benzenesulfonyl ethylene and ethyl diazoacetate in the presence of a catalyst, to obtain a cyclopropane intermediate;5) performing an elimination reaction of the cyclopropane intermediate in the presence of an alkali before an acidification, to obtain 2-fluorocyclopropanecarboxylic acid.2: The new method for synthesizing 2-fluorocyclopropanecarboxylic acid of ...

Receptor ligands

Non-antibody multimeric receptor ligands, methods for making and identifying them and their use for agonizing or antagonizing multimeric receptors.

Unsaturated polyester resin composition

Highly versatile thermoplastic nucleators

Bicyclic nucleator compounds that provide highly versatile nucleation benefits for different polyolefins are provided. Such nucleator compounds provide very high peak crystallization temperatures and significantly reduced crystallization cycle time for certain thermoplastic formulations with or without the presence of other calcium stearate and/or peroxide components within the same type of formulation. Furthermore, such inventive nucleator compounds exhibits very little if any fugitivity from such thermoplastic formulations thereby providing excellent processing characteristics as well as excellent nucleation capabilities for a variety of different thermoplastic resins, independent of the presence of different, potentially necessary, additives (such as calcium stearate). Thermoplastic compositions as well as thermoplastic additive packages comprising such inventive nucleator compounds are also contemplated within this invention.

Polymer additive compositions comprising highly versatile thermoplastic nucleators

Bicyclic nucleator compounds that provide highly versatile nucleation benefits for different polyolefins are provided. Such nucleator compounds provide very high peak crystallization temperatures and significantly reduced crystallization cycle time for certain thermoplastic formulations with or without the presence of other calcium stearate and/or peroxide components within the same type of formulation. Furthermore, such inventive nucleator compounds exhibits very little if any fugitivity from such thermoplastic formulations thereby providing excellent processing characteristics as well as excellent nucleation capabilities for a variety of different thermoplastic resins, independent of the presence of different, potentially necessary, additives (such as calcium stearate). Thermoplastic compositions as well as thermoplastic additive packages comprising such inventive nucleator compounds are also contemplated within this invention.

Novel fluorinated adamantane derivatives

新規なフッ素化されたアダマンタン誘導体を提供する。式ＡＦ（−ＣＯＦ）ｎで表される化合物。ただしＡＦ、およびｎは以下の意味を示す。ＡＦ：アダマンタンから水素原子をｎ個を除いた（ただし、ｎが２以上の場合除かれる水素原子は異なる炭素原子に結合した水素原子である）ｎ価の基であり、残余の水素原子の少なくとも１個はフッ素原子に置換され、さらに残余の水素原子は炭素数１〜６のアルキル基またはフルオロアルキル基で置換されていてもよい、含フッ素アダマンタン残基。ｎ：１〜４の整数。ただし、ｎが１の場合は、前記ＡＦは少なくとも１個の水素原子を有する。 Novel fluorinated adamantane derivatives are provided. A compound represented by the formula AF (-COF) n. However, AF and n have the following meanings. AF: n-valent group obtained by removing n hydrogen atoms from adamantane (provided that when n is 2 or more, the hydrogen atom is a hydrogen atom bonded to a different carbon atom), at least the remaining hydrogen atoms A fluorine-containing adamantane residue in which one is substituted with a fluorine atom and the remaining hydrogen atoms may be substituted with an alkyl group or fluoroalkyl group having 1 to 6 carbon atoms. n: An integer of 1 to 4. However, when n is 1, the AF has at least one hydrogen atom.

The method of obtaining cyclopropane carboxylic acids

Bicyclo[2.2.1]heptane dicarboxylate salts as polyolefin nucleators

Compounds and compositions comprising specific metal salts of bicyclo[2.2.1 ]heptane dicarboxylate salts in order to provide highly desirable properties within polyolefin articles are provided. The inventive salts and derivatives thereof are useful as nucleating and/or clarifying agents for such polyolefin, provide excellent crystallization temperatures, stiffness, and calcium stearate compatibility within target polyolefin. Also, such compounds exhibit very low hygroscopicity and therefore excellent shelf stability as powdered or granular formulations. Polyolefin additive compositions and methods of producing polyolefin with such compounds are also contemplated within this invention.

Highly nucleated thermoplastic articles

Compounds and compositions comprising specific metal salts of bicyclo[2.2.1 ]heptane dicarboxylate salts in order to provide highly desirable properties within polyolefin articles are provided. The inventive salts and derivatives thereof are useful as nucleating and/or clarifying agents for such polyolefin, provide excellent crystallization temperatures, stiffness, and calcium stearate compatibility within target polyolefin. Also, such compounds exhibit very low hygroscopicity and therefore excellent shelf stability as powdered or granular formulations. Polyolefin additive compositions and methods of producing polyolefin with such compounds are also contemplated within this invention.

Thermoplastic articles with high degree of structural formation

FIELD: chemical technology. SUBSTANCE: invention relates to technology for making articles from thermoplastics, in particular, to compounds and compositions comprising specific metal salts and bicyclo[2.2.1]heptane dicarboxylates providing suitable high indices of articles made of polyolefins. Proposed salts and their derivatives are used as cross-linking agents and/or clearing agents for such polyolefins and provide the excellent crystallization point values, rigidity (density) and compatibility with calcium stearate in the end polyolefin. Also, proposed compound possess very low hygroscopicity and, therefore, the excellent stability in storing as powder-like or granulated compositions. Also, invention considers additive compositions prepared from polyolefins and methods for synthesis of polyolefin with such compounds. EFFECT: improved and valuable properties of thermoplastics. 20 cl, 13 tbl, 11 ex ÐÎÑÑÈÉÑÊÀß ÔÅÄÅÐÀÖÈß RU (19) (11) 2 289 597 (13) C2 (51) ÌÏÊ C08K C07C C08K C08K C08K ÔÅÄÅÐÀËÜÍÀß ÑËÓÆÁÀ C07C ÏÎ ÈÍÒÅËËÅÊÒÓÀËÜÍÎÉ ÑÎÁÑÒÂÅÍÍÎÑÒÈ,C07C ÏÀÒÅÍÒÀÌ È ÒÎÂÀÐÍÛÌ ÇÍÀÊÀÌ (12) 5/09 13/40 5/092 5/095 5/098 69/75 69/753 (2006.01) (2006.01) (2006.01) (2006.01) (2006.01) (2006.01) (2006.01) ÎÏÈÑÀÍÈÅ ÈÇÎÁÐÅÒÅÍÈß Ê ÏÀÒÅÍÒÓ (21), (22) Çà âêà: 2003131268/04, 05.03.2002 (24) Äàòà íà÷àëà îòñ÷åòà ñðîêà äåéñòâè ïàòåíòà: 05.03.2002 (73) Ïàòåíòîîáëàäàòåëü(è): ÌÈËËÈÊÅÍ ÝÍÄ ÊÎÌÏÀÍÈ (US) (43) Äàòà ïóáëèêàöèè çà âêè: 20.03.2005 2 2 8 9 5 9 7 (45) Îïóáëèêîâàíî: 20.12.2006 Áþë. ¹ 35 (56) Ñïèñîê äîêóìåíòîâ, öèòèðîâàííûõ â îò÷åòå î ïîèñêå: US 4647581 À, 03.03.1987. US 4442025 A, 10.04.1984. RU 2072363 C1, 27.01.1997. SU 956275 A1, 07.09.1982. US 3207735 A, 21.09.1965. (85) Äàòà ïåðåâîäà çà âêè PCT íà íàöèîíàëüíóþ ôàçó: 24.10.2003 2 2 8 9 5 9 7 R U (87) Ïóáëèêàöè PCT: WO 02/077092 (03.10.2002) C 2 C 2 (86) Çà âêà PCT: US 02/06493 (05.03.2002) Àäðåñ äë ïåðåïèñêè: 129010, Ìîñêâà, óë. Á.Ñïàññêà , 25, ñòð.3, ÎÎÎ "Þðèäè÷åñêà ôèðìà Ãîðîäèññêèé è Ïàðòíåðû", ïàò.ïîâ. Å.Å.Íàçèíîé (54) ÈÇÄÅËÈß ÈÇ ...

Highly nucleated thermoplastic articles

본 발명은 폴리올레핀 제품 내에서 매우 바람직한 특성을 제공하기 위한, 비사이클로[2.2.1]헵탄 디카복실레이트 염의 특정 금속 염을 포함하는 화합물 및 조성물의 제공에 관한 것이다. 본 발명의 염 및 이의 유도체는 상기 폴리올레핀의 핵형성화 및/또는 투명화제로서 유용하며, 탁월한 결정화 온도, 견고성, 및 표적 폴리올레핀 내에서의 칼슘 스테아레이트 혼화성을 제공한다. 또한, 상기 화합물은 매우 낮은 흡습성을 나타내어, 분말 또는 과립 제제로서 우수한 보존 안정성을 나타낸다. 또한, 본 발명은 상기 화합물을 사용하는 폴리올레핀 첨가제 조성물 및 폴리올레핀의 제조방법을 포함한다. The present invention relates to the provision of compounds and compositions comprising certain metal salts of bicyclo [2.2.1] heptane dicarboxylate salts to provide very desirable properties in polyolefin articles. Salts and derivatives thereof of the present invention are useful as nucleation and / or clearing agents of such polyolefins and provide excellent crystallization temperature, robustness, and calcium stearate miscibility in the target polyolefin. In addition, the compounds exhibit very low hygroscopicity, which shows good storage stability as powder or granule formulations. The present invention also encompasses polyolefin additive compositions and methods for preparing polyolefins using the compounds.

Polymer additive compositions comprising highly versatile thermoplastic nucleators

Bicyclic nucleator compounds that provide highly versatile nucleation benefits for different polyolefins are provided. Such nucleator compounds provide very high peak crystallization temperatures and significantly reduced crystallization cycle time for certain thermoplastic formulations with or without the presence of other calcium stearate and/or peroxide components within the same type of formulation. Furthermore, such inventive nucleator compounds exhibits very little if any fugitivity from such thermoplastic formulations thereby providing excellent processing characteristics as well as excellent nucleation capabilities for a variety of different thermoplastic resins, independent of the presence of different, potentially necessary, additives (such as calcium stearate). Thermoplastic compositions as well as thermoplastic additive packages comprising such inventive nucleator compounds are also contemplated within this invention.

Thermoplastic nucleating compounds

Compounds and compositions comprising specific metal salts of bicyclo[2.2.1]heptane dicarboxylate salts in order to provide highly desirable properties within polyolefin articles are provided. The inventive salts and derivatives thereof are useful as nucleating and/or clarifying agents for such polyolefin, provide excellent crystallization temperatures, stiffness, and calcium stearate compatibility within target polyolefin. Also, such compounds exhibit very low hygroscopicity and therefore excellent shelf stability as powdered or granular formulations. Polyolefin additive compositions and methods of producing polyolefin with such compounds are also contemplated within this invention.

Nanodiamonds having acid functional group, and method for production thereof

FIELD: chemistry.SUBSTANCE: invention relates to nanotechnology. Nanodiamond obtained by detonation synthesis containing 0.15 mmol/g or more of acid functional groups, oxidative treatment is carried out with at least one oxidant selected from a group consisting of chromic acid, chromic anhydride, dichromic acid, manganic acid, perchloric acid, salts of said acids and hydrogen peroxide. Oxidative treatment can be carried out in the presence of sulphuric acid at temperature 130 °C or higher. If nanodiamonds do not contain acidic functional groups as a result of detonation synthesis, nanodiamond blend can be treated with mineral acid. Suspension of nanodiamonds after oxidative treatment can be subjected to disaggregating treatment. Obtained nanodiamonds have specific surface area of 150 m/g or more and carboxyl functional groups with numerical density of 1 or more groups per square nanometer of the surface. Nanodiamond particles have d50 of 9 nm or less. High dispersibility of nanodiamond in dispersion media, for example in water, to obtain a stable dispersion.EFFECT: invention can be used in production of lubricating, abrasive or insulating materials.9 cl, 2 ex РОССИЙСКАЯ ФЕДЕРАЦИЯ (19) RU (11) (13) 2 696 439 C2 (51) МПК C01B 32/15 (2017.01) C01B 32/28 (2017.01) B82B 1/00 (2006.01) B82B 3/00 (2006.01) B82Y 40/00 (2011.01) ФЕДЕРАЛЬНАЯ СЛУЖБА ПО ИНТЕЛЛЕКТУАЛЬНОЙ СОБСТВЕННОСТИ (12) ОПИСАНИЕ ИЗОБРЕТЕНИЯ К ПАТЕНТУ (52) СПК C01B 32/15 (2019.02); C01B 32/28 (2019.02); B82B 1/008 (2019.02); B82B 3/0076 (2019.02); B82Y 40/00 (2019.02) (21)(22) Заявка: 2017119669, 31.08.2015 31.08.2015 (73) Патентообладатель(и): ДАЙСЕЛ КОРПОРЭЙШН (JP) Дата регистрации: 01.08.2019 07.11.2014 JP 2014-226656 (43) Дата публикации заявки: 07.12.2018 Бюл. № 34 (45) Опубликовано: 01.08.2019 Бюл. № 22 (86) Заявка PCT: JP 2015/074654 (31.08.2015) C 2 C 2 (85) Дата начала рассмотрения заявки PCT на национальной фазе: 07.06.2017 (87) Публикация заявки PCT: 2 6 9 6 4 3 9 WO 2016/072138 (12.05.2016) R U 2 6 ...

Method for preparing intermediate compound for synthesis of medicinal agent

FIELD: chemistry.SUBSTANCE: present invention relates to a method of producing a compound of chemical formula 1comprising a step of selectively deprotecting a protective group of carboxylic acid (P2) from P1and P2protective groups on a compound of chemical formula 2where when removing protection, a solid base is used as a reaction base, and a lower alcohol is used as a reaction solvent. Where R1, R2, R3 and R4 are independently hydrogen or halogen, P1is a carbonyl group, an acyl group, a sulfonyl group, an acetyl group or a benzyl group as an amine protecting group, P2is a benzyl group, an ethyl group, an isopropyl group or a tert-butyl group.EFFECT: technical result is described is having high economic feasibility and efficiency, a method of producing a compound which is an intermediate compound for oral medications for non-insulin dependent diabetes, which can significantly improve the yield of the end product even under moderate conditions.9 cl, 6 ex, 1 tbl РОССИЙСКАЯ ФЕДЕРАЦИЯ (19) RU (11) (13) 2 741 389 C1 (51) МПК C07D 211/74 (2006.01) C07C 27/02 (2006.01) C07C 31/04 (2006.01) C07C 51/09 (2006.01) C07C 51/42 (2006.01) C07C 61/13 (2006.01) ФЕДЕРАЛЬНАЯ СЛУЖБА C07C 67/10 (2006.01) ПО ИНТЕЛЛЕКТУАЛЬНОЙ СОБСТВЕННОСТИ C07D 211/36 (2006.01) (12) ОПИСАНИЕ ИЗОБРЕТЕНИЯ К ПАТЕНТУ (52) СПК C07D 211/74 (2020.08); C07C 31/04 (2020.08); C07C 31/04 (2020.08); C07C 51/09 (2020.08); C07C 51/42 (2020.08); C07C 61/13 (2020.08); C07C 67/10 (2020.08); C07D 211/36 (2020.08) (21)(22) Заявка: 2020114746, 23.10.2018 23.10.2018 Дата регистрации: 25.01.2021 Приоритет(ы): (30) Конвенционный приоритет: (56) Список документов, цитированных в отчете о поиске: KR 10-1378984 B1, 27.03.2014. JP 04316526 A, 06.11.1992. JP 2008-201719 A, 04.09.2008. US 4256907 A, 17.03.1981. KR 10-20010079823 A, 22.08.2001. EA 200701854 D1, 28.02.2008. 16.11.2017 KR 10-2017-0153334; 23.10.2018 KR 10-2018-0126663 (45) Опубликовано: 25.01.2021 Бюл. № 3 (85) Дата начала рассмотрения заявки PCT на национальной фазе: ...

Polyhalosubstituted polyhydropolycyclicdicarboxylic acid and anhydride

NOVEL COMPOUNDS COMPRISING POLYHALO-SUBSTITUTED POLYHYDROPOLYCYCLICDICARBOXYLIC ACIDS OR ANHYDRIDES THEREOF AS EXEMPLIFIED BY 5,6,7,8,9,9-HEXACHLORO-6,7-DIBROMOMETHYLENE - 1,2,3,4,4A,5,8,8A-OCTAHYDRO-5,8-METHANO-2,3NAPHTHALENEDICARBOXYLIC ANHYDRIDE POSSESSING CERTAIN PHYSICAL PROPERTIES SUCH AS BEING FLAMEPROOF OR FIRE RESISTANT.

Highly nucleated thermoplastic articles

Compounds and compositions comprising specific metal salts of bicyclo[2.2.1]heptane dicarboxylate salts in order to provide highly desirable properties within polyolefin articles are provided. The inventive salts and derivatives thereof are useful as nucleating and/or clarifying agents for such polyolefin, provide excellent crystallization temperatures, stiffness, and calcium stearate compatibility within target polyolefin. Also, such compounds exhibit very low hygroscopicity and therefore excellent shelf stability as powdered or granular formulations. Polyolefin additive compositions and methods of producing polyolefin with such compounds are also contemplated within this invention.

Novel highly versatile thermoplastic nucleators

Bicyclic nucleator compounds that provide highly versatile nucleation benefits for different polyolefins are provided. Such nucleator compounds provide very high peak crystallization temperatures and significantly reduced crystallization cycle time for certain thermoplastic formulations with or without the presence of other calcium stearate and/or peroxide components within the same type of formulation. Furthermore, such inventive nucleator compounds exhibits very little if any fugitivity from such thermoplastic formulations thereby providing excellent processing characteristics as well as excellent nucleation capabilities for a variety of different thermoplastic resins, independent of the presence of different, potentially necessary, additives (such as calcium stearate). Thermoplastic compositions as well as thermoplastic additive packages comprising such inventive nucleator compounds are also contemplated within this invention.

Novel thermoplastic nucleating compounds

Compounds and compositions comprising specific metal salts of bicyclo[2.2.1]heptane dicarboxylate salts in order to provide highly desirable properties within polyolefin articles are provided. The inventive salts and derivatives thereof are useful as nucleating and/or clarifying agents for such polyolefin, provide excellent crystallization temperatures, stiffness, and calcium stearate compatibility within target polyolefin. Also, such compounds exhibit very low hygroscopicity and therefore excellent shelf stability as powdered or granular formulations. Polyolefin additive compositions and methods of producing polyolefin with such compounds are also contemplated within this invention.

Method for producing cyclopropilcarbonic acids

Изобретение относится к органической химии, конкретно к получению циклопропилкарбоновых кислот, производные которых находят применение в качестве пластификаторов и поверхностно-активных веществ. Способ заключается в том, что проводят окисление олефинов циклопропанового ряда в смеси с гидроксидом натрия, метанолом и хлористым метиленом, озоном при температуре -50°С. Технический результат - увеличение выхода целевого продукта при повышении его качества. 1 з.п. ф-лы, 1 табл., 2 пр. РОССИЙСКАЯ ФЕДЕРАЦИЯ (19) RU (11) (13) 2 620 268 C1 (51) МПК C07C 51/34 (2006.01) C07C 61/15 (2006.01) ФЕДЕРАЛЬНАЯ СЛУЖБА ПО ИНТЕЛЛЕКТУАЛЬНОЙ СОБСТВЕННОСТИ (12) ФОРМУЛА (21)(22) Заявка: ИЗОБРЕТЕНИЯ К ПАТЕНТУ РОССИЙСКОЙ ФЕДЕРАЦИИ 2016113879, 11.04.2016 (24) Дата начала отсчета срока действия патента: 11.04.2016 Дата регистрации: Приоритет(ы): (22) Дата подачи заявки: 11.04.2016 (45) Опубликовано: 24.05.2017 Бюл. № 15 (56) Список документов, цитированных в отчете о поиске: US 3462453 A, 19.08.1969. US C 1 (57) Формула изобретения 1. Способ получения циклопропилкарбоновых кислот окислением олефинов циклопропанового ряда в смеси с гидроксидом натрия, метанолом и хлористым метиленом, озоном при температуре -50°С. 2. Способ по п. 1, отличающийся тем, что процесс озонирования проводят при следующем соотношении компонентов, мас.%: 1,1-дихлор-2-винил-2-циклопропан 1; гидроксид натрия 1,6; метанол 12,6; хлористый метилен 84,8. R U 2 6 2 0 2 6 8 (54) Способ получения циклопропилкарбоновых кислот Стр.: 1 C 1 3341611 A, 12.09.1967. US 2002/0169329 A1, 14.11.2002. Арбузова Т.В. "Синтез замещенных гем.-дихлорциклопропанов и реакции их основе" Диссертация на соискание ученой степени кандидата химических наук, Уфа, 2006, 111с. 2 6 2 0 2 6 8 Адрес для переписки: 450062, г. Уфа, ул. Космонавтов, 1, Уфимский государственный нефтяной технический университет, патентный отдел (73) Патентообладатель(и): Федеральное государственное бюджетное образовательное учреждение высшего профессионального образования "Уфимский ...

Molecule clathrate compound and the preparation method and application thereof

本发明属于超分子材料技术领域，尤其是涉及一类分子笼化合物及其制备方法与应用。本发明的分子笼化合物可以显著改善笼状化合物在有机溶剂甚至水中的溶解性；本发明的分子笼化合物具有和金刚烷及其衍生物相匹配的空间尺寸，可以为某些不稳定的金刚烷衍生物提供一个封闭性空间，提高其化学稳定性；本发明的分子笼化合物能够选择性的络合金刚烷及其衍生物，同时在特定条件下可以定量释放，并且实现对主体分子的高效回收，这在药物的传输和释放领域具有很大的应用前景。

Synthesis of magnesium adamantane carboxylate and oxide nanocomposite

마그네슘 아다만탄 카복실레이트염의 제조 방법이 제공된다. 상기 방법은 적어도 1종의 카복실산 모이어티를 갖는 다이아몬드형 화합물과 마그네슘염을 혼합하여 반응물 혼합물을 형성시키는 단계 및 반응 온도에서 반응 시간 동안 상기 반응물 혼합물을 열수 처리하여 마그네슘 아다만탄 카복실레이트염을 형성시키는 단계를 포함한다.

METHODS AND COMPOSITIONS FOR TREATMENT OF DIABETES MELLITUS AND DYSLIPIDEMIA

1. Композиция, содержащая по меньшей мере одно соединение в соответствии с формулой I:,его стереоизомеры и/или фармацевтически приемлемые соли, гдеRвыбран из группы, состоящей из гидрокси, алкокси, амина, алкила, галогеналкила, NHSOR или NHCOR, где R выбран из алкила или циклоалкила, NHR', где R' обозначает алкил или циклоалкил, необязательно замещенный гидрокси или алкокси группой;nи nнезависимо выбраны из 0, 1 и 2;по меньшей мере один из Rи Rи/или Rи Rобразуют циклическое кольцо, содержащее 3-8 атомов углерода, необязательно содержащее алкильные группы, гетероатомы или функциональные группы, такие как O, N, SO;Rи Rили Rи R, когда они не образуют циклическое кольцо, то они необязательно независимо выбраны из водорода, алкила, разветвленного алкила и циклоалкила;Lобозначает линейную алифатическую цепь, необязательно содержащую от 4 до 16 атомов углерода, необязательно замещенную один или более раз алкилом, разветвленным алкилом, циклоалкилом или арилом;Rнезависимо выбран из водорода, алкокси, гидрокси, алкила, галогеналкила, циклоалкила, гетероциклоалкила, гетероарила, циано или COR, где Rвыбран из гидрокси, алкила, алкокси или амина, NHR', NHSOR или NHCOR;Yобозначает кислород или водород;Yявляется необязательным, причем когда Yприсутствует, то Yи Yобозначают водород, а когда Yне присутствует, то Yобозначает карбонильную группу.2. Композиция по п. 1, где соединение имеет формулу II:,его стереоизомеры и/или фармацевтически приемлемые соли, гдеRи Rнезависимо выбраны из группы, состоящей из гидрокси, алкокси, алкила, амина, NHR', где R' обозначает алкил или циклоалкил, необязательно замещенный гидрокси или алкокси группой, NHSOR или NHCOR, где R выбран из алкила или ц РОССИЙСКАЯ ФЕДЕРАЦИЯ (19) RU (11) (13) 2013 118 021 A (51) МПК A61K 31/225 (2006.01) ФЕДЕРАЛЬНАЯ СЛУЖБА ПО ИНТЕЛЛЕКТУАЛЬНОЙ СОБСТВЕННОСТИ (12) ЗАЯВКА НА ИЗОБРЕТЕНИЕ (21)(22) Заявка: 2013118021/15, 20.09.2011 (71) Заявитель(и): КАРЕУС ТЕРАПЬЮТИКС, СА (CH) Приоритет(ы): (30) ...

Method for producing norbornane dicarboxylic acid

본 발명은 노르보르난 카르복실산의 제조방법에 관한 것으로, 보다 상세하게는 디사이클로펜타디엔을 열분해하여 얻어진 사이클로펜타디엔과 말레산 무수물을 반응시키는 단계를 포함하여 제조하는 것을 특징으로 하는 노르보르난 카르복실산의 제조방법에 관한 것이다. 본 발명에 따른 제조방법은 디사이클로펜타디엔을 활용하며, 반응 효율이 우수하고, 전체 반응 공정이 공업적으로 유용하기 때문에 고수율의 노르보르난 디카르복실산의 대량생산이 가능하며, 산업적으로 다양한 분야에 응용을 가능케 한다. The present invention relates to a method for preparing norbornane carboxylic acid, and more particularly, to a method for preparing norbornane carboxylic acid, comprising the step of reacting cyclopentadiene obtained by thermal decomposition of dicyclopentadiene with maleic anhydride. I relate to a process for the preparation of carboxylic acids. The production method according to the present invention utilizes dicyclopentadiene, has excellent reaction efficiency, and because the entire reaction process is industrially useful, it is possible to mass-produce norbornane dicarboxylic acid in high yield, and industrially It enables application in various fields.

Tricycloundecane derivatives

Electrolyte for electrolytic capacitor and electrolytic capacitor using the same

다음 일반식(I) 또는 (II)로 표시되는 3급 디카르복실산의 염을 함유함을 특징으로하는 전해 콘덴서용 전해액: An electrolytic solution for an electrolytic capacitor, comprising a salt of a tertiary dicarboxylic acid represented by the following general formula (I) or (II): (식중 n은 1 내지 5의 정수이고, R 1 내지 R 4 는 탄소수 4이하인 알킬기임) Wherein n is an integer of 1 to 5 and R 1 to R 4 are alkyl groups having 4 or less carbon atoms. (식중 n은 상기 정의한 바와 같고, ℓ및 m은 각각 정수 4 또는 5를 나타내며, R 5 및 R 6 은 각각 수소원자, 메틸기 또는 에틸기를 표시한다) (Wherein n is as defined above, l and m each represent an integer of 4 or 5, and R 5 and R 6 each represent a hydrogen atom, a methyl group or an ethyl group) 및 이를 이용한 전해 콘덴서가 개시된다. And an electrolytic capacitor using the same.

Radiolabelling process

本发明涉及包含1-氨基-3-[ 18 F]-氟代环丁烷羧酸([ 18 F]-FACBC)的新的组合物，其中所述组合物相较于包括[ 18 F]-FACBC的已知组合物具有某些优越的性质。本发明还提供获得所述组合物的方法。

The seperation method of alpha-halo alkanoic acid optical isomers composition

A method for the separation of a recemic mixture of alpha- haloalkanoic acid comprises reacting a metal salt of a cpd. of formula (II) with a cpd. of formula (III) to obtain a pair of diastereoisomers of formula (IV), separating the diastereoisomers by column chromatography, esterifying the obtd. cpd., and reducing the optically pure cpd. of formula (V). In the formulas, R=C1-10 alkyl or C6-12 aryl; X=Cl, Br or I; R1=C1-10 alkyl or C6-12 aryl; R2=H, C1-10 alkyl or C6-12 aryl. The optically pure alpha- haloalkanoic acids are useful as intermediates in the mfr. of medicines or agricultural chemicals.

Process for the preparation of 2,4-dibromo-5-fluorobenroicacid

A process for preparing 2,4-dibromo-5-fluorobenzoic acid of formula (I) comprises (A) obtaining 2,4-dibromo-5-fluorotoluene (II) 3- fluorotoluene (B) reacting (II) with Br2 in the presence of UV to form 3-fluoro-alpha, alpha, 4,5-tetrabromotoluene (IV) (C) hydrolyzing (IV) and reacting with Jones reagent to obtain (I). (I) is an intermediate in the synthesis of a potent antibacterial compound.

Patent RU2017119669A3

NANODIAMONDS WITH AN ACID FUNCTIONAL GROUP AND METHOD FOR PRODUCING THEM

РОССИЙСКАЯ ФЕДЕРАЦИЯ (19) RU (11) (13) 2017 119 669 A (51) МПК C01B 31/06 (2006.01) ФЕДЕРАЛЬНАЯ СЛУЖБА ПО ИНТЕЛЛЕКТУАЛЬНОЙ СОБСТВЕННОСТИ (12) ЗАЯВКА НА ИЗОБРЕТЕНИЕ (21)(22) Заявка: 2017119669, 31.08.2015 (71) Заявитель(и): ДАЙСЕЛ КОРПОРЭЙШН (JP) Приоритет(ы): (30) Конвенционный приоритет: (72) Автор(ы): ЯМАКАВА Акира (JP) 07.11.2014 JP 2014-226656 34 (85) Дата начала рассмотрения заявки PCT на национальной фазе: 07.06.2017 JP 2015/074654 (31.08.2015) (87) Публикация заявки PCT: R U Адрес для переписки: 129090, Москва, ул. Б. Спасская, 25, стр. 3, ООО "Юридическая фирма Городисский и Партнеры" (54) НАНОАЛМАЗЫ, ИМЕЮЩИЕ КИСЛОТНУЮ ФУНКЦИОНАЛЬНУЮ ГРУППУ, И СПОСОБ ИХ ПОЛУЧЕНИЯ (57) Формула изобретения 1. Наноалмаз, имеющий кислотные функциональные группы, причем наноалмаз содержит кислотные функциональные группы с численной плотностью 1 или более групп на квадратный нанометр на поверхности наноалмаза, и при этом наноалмаз имеет удельную поверхность 150 м2/г или более. 2. Наноалмаз по п. 1, в котором частицы наноалмаза имеют D50, составляющий 9 нм или менее. 3. Наноалмаз по одному из пп. 1-2, где наноалмаз представляет собой наноалмаз, полученный детонационным синтезом. 4. Наноалмаз по любому из пп. 1-3, где наноалмаз представляет собой наноалмаз, полученный детонационным синтезом с воздушным охлаждением. 5. Наноалмаз по любому из пп. 1-4, где наноалмаз представляет собой наноалмаз, полученный подверганием наноалмаза, имеющего содержание кислотных функциональных групп 0,15 ммоль/г или более, окислительной обработке. 6. Способ получения наноалмаза, предназначенный для получения наноалмаза по любому из пп. 1-5, причем способ включает этап, на котором: А) подвергают материал наноалмаза окислительной обработке по меньшей мере одним окислителем, выбираемым из группы, состоящей из хромовой кислоты, хромового Стр.: 1 A 2 0 1 7 1 1 9 6 6 9 A WO 2016/072138 (12.05.2016) 2 0 1 7 1 1 9 6 6 9 (86) Заявка PCT: R U (43) Дата публикации заявки: 07.12.2018 Бюл. № R U ангидрида, ...

Derivatives of n-(pyrid-5-yl)cyclopropanecarboxamide and their stereoisomers and fungicide composition

FIELD: applicable in agriculture. SUBSTANCE: the present invention offers derivatives of N-(pyrid-5- yl)cyclopropanecarboxamide of general formula 1 and their stereoisomers, where R' is halogen, (C'- C 4 )aloxy; R 2 is hydrogen, halogen, methyl; R 3 and R 4 are, independently of each other, hydrogen or halogen, provided that R 2 , R 3 and R 4 are not hydrogen simultaneously, and provided that when R 2 is methyl, then one or R 3 or R 4 is other than hydrogen; X is group N(RS)-C(= Y)-, where R5 is hydrogen, (C'-C<Mv>4>D>)-alkyl, benzyl, (C 2 -C 4 ) alkenyl, (C 2 -C 4 ) alkynyl, and Y is oxygen, and fungicide composition containing active ingredient in form of 0.0005-96 mas.% of compound with formula 1 in mixture with fungicide-tolerable carrier or diluent. The structure of compounds of formula 1 is given in the invention description. EFFECT: higher efficiency. 5 cl, 3 tbl г; 990с ПЧ Го РОССИЙСКОЕ АГЕНТСТВО ПО ПАТЕНТАМ И ТОВАРНЫМ ЗНАКАМ (19) ВИ” 2 066 314. (51) МПК 13) СЛ С 070 213/75, А 01 М 43/40 12) ОПИСАНИЕ ИЗОБРЕТЕНИЯ К ПАТЕНТУ РОССИЙСКОЙ ФЕДЕРАЦИИ (21), (22) Заявка: 4894320/04, 04.01.1991 (30) Приоритет: 04.01.1990 СВ 9000130.6 (46) Дата публикации: 10.09.1996 (56) Ссылки: Патент США М 4766134, кл. 514/346, 1998. Патент США М 47677711, кл. 514/346, 1989. Европейская заявка М 190036, кл. С 07 О 213/15, 1986. (71) Заявитель: Империал Кемикал Индастриз ПЛС (СВ), АЙ-Си-Ай Америказ Инк. (Ц$) (72) Изобретатель: Дон Роберт Бейкер[Ц$], Карл Джозеф Фишер[Ц$], Пол Энтони Вортингтон[ СВ], Ян Ричард Мэттьюз[СВ], Дэвид Бартоломеу[СВ], Патрик Джелф Кроули[СВ] (73) Патентообладатель: Империал Кемикал Индастриз ПЛС (СВ), АЙ-Си-Ай Америказ Инк. (Ц$) (54) ПРОИЗВОДНЫЕ М-(ПИРИД-5-ИЛ)ЦИКЛОПРОПАНКАРБОКСАМИДА И ИХ СТЕРЕОИЗОМЕРЫ И ФУНГИЦИДНАЯ КОМПОЗИЦИЯ (57) Реферат: Использование: в сельском хозяйстве. Сущность — изобретения: производные М-(пирид-5-ил)циклопропанкарбоксамида общей формулы [ и их стереоизомеры, где В 1 - галоген, (С1-Са)алкокси, В? - водород, ...

Patent JPS5810371B2

1-methyl-2-chlorocyclopropane carboxylic acid, ester thereof and manufacture

Methods and compositions for inhibiting 5α-reductase activity

Disclosed are a novel class of antiandrogenic compounds including saturated and unsaturated fatty acids, catechin gallates, their derivatives, and synthetic analogs, their method of synthesis, and their use in treating disorders associated with androgenic activities. Also disclosed is the use of known compounds not previously known for their antiandrogenic activity in treating disorders related to androgenic activities and cancers.

Adamantyl-s-triazines

Chemically-amplified positive resist composition and resist patterning process using the same

An object of the present invention is to provide a chemically amplified positive resist composition using a sulfonium salt having a very high resolution and capable of imparting a small pattern of line edge roughness and a method of forming a resist pattern using the chemically amplified positive resist composition. (A) a salt represented by the following formula (1), (B) a resin which is decomposed by the action of an acid containing a repeating unit represented by the following formula (U-1) and whose solubility in an alkali developer is increased And a resist pattern forming method using the chemically amplified positive resist composition.

The method of radioactive labeling

РОССИЙСКАЯ ФЕДЕРАЦИЯ (19) RU (11) (13) 2015 138 540 A (51) МПК A61K 51/04 (2006.01) ФЕДЕРАЛЬНАЯ СЛУЖБА ПО ИНТЕЛЛЕКТУАЛЬНОЙ СОБСТВЕННОСТИ (12) ЗАЯВКА НА ИЗОБРЕТЕНИЕ (21)(22) Заявка: 2015138540, 28.03.2014 (71) Заявитель(и): ДжиИ Хелткер Лимитед (GB) Приоритет(ы): (30) Конвенционный приоритет: (72) Автор(ы): ВИКСТРОМ Торильд (NO) 28.03.2013 GB 1305687.4 (85) Дата начала рассмотрения заявки PCT на национальной фазе: 28.10.2015 R U (43) Дата публикации заявки: 03.05.2017 Бюл. № 13 (86) Заявка PCT: (87) Публикация заявки PCT: WO 2014/154886 (02.10.2014) A Адрес для переписки: 191036, Санкт-Петербург, а/я 24, "НЕВИНПАТ" (54) Способ радиоактивного мечения R U 1. Способ получения композиции, содержащей 1-амино-3-[18F]фторциклобутанкарбоновую кислоту ([18F]-FACBC), где указанная композиция содержит ацетонитрил (MeCN) в концентрации не более 50 мкг/мл и где указанная композиция имеет концентрацию радиоактивности (RAC) между 500 и 5000 МБк/мл, включающий: (1) взаимодействие [18F]фторида с соединением-предшественником формулы I: , где LG представляет собой уходящую группу; PG1 представляет собой карбокси-защитную группу; и PG2 представляет собой амин-защитную группу; где указанную стадию взаимодействия проводят в ацетонитриле; с получением реакционной смеси, содержащей соединение формулы II: , где PG1 и PG2 являются такими, как определено для формулы I; Стр.: 1 A 2 0 1 5 1 3 8 5 4 0 (57) Формула изобретения 2 0 1 5 1 3 8 5 4 0 EP 2014/056344 (28.03.2014) (2) перенос указанного соединения формулы II из реакционного сосуда с осуществлением удаления PG1 и, таким образом, получением соединения формулы III: , где PG2 является такой, как определено для формулы I; (3) одновременно со стадией (2) подведение тепла к указанному реакционному сосуду; (4) перенос указанного соединения формулы III обратно в указанный реакционный 5. Способ по п. 1, где указанная [18F]FACBC представляет собой транс-1-амино- R U сосуд с осуществлением удаления PG2 и, таким образом, получением [18F]-FACBC. 2. ...

Method of radioactive labeling

FIELD: medicine; pharmaceuticals.SUBSTANCE: invention relates to a method for producing a radiopharmaceutical composition comprising [F]-1-amino-3-fluorocyclobutane-1-carboxylic acid ([F]-FACBC, also known as [F]-fluciclovine), useful as an indicator for positron emission tomography (PET).EFFECT: method of the invention is particularly suitable for automation and provides advantages over other methods.16 cl, 2 ex, 2 tbl РОССИЙСКАЯ ФЕДЕРАЦИЯ (19) RU (11) (13) 2 675 371 C2 (51) МПК A61K 51/04 (2006.01) ФЕДЕРАЛЬНАЯ СЛУЖБА ПО ИНТЕЛЛЕКТУАЛЬНОЙ СОБСТВЕННОСТИ (12) ОПИСАНИЕ ИЗОБРЕТЕНИЯ К ПАТЕНТУ (52) СПК A61K 51/00 (2006.01); A61K 51/04 (2006.01) (21)(22) Заявка: 2015138540, 28.03.2014 (24) Дата начала отсчета срока действия патента: (73) Патентообладатель(и): ДжиИ Хелткер Лимитед (GB) Дата регистрации: 19.12.2018 (56) Список документов, цитированных в отчете о поиске: WO 2012089594 A1, 05.07.2012. RU 2476423 C2, 27.02.2013. RU 2445120 C2, 20.03.2012. 28.03.2013 GB 1305687.4 (43) Дата публикации заявки: 03.05.2017 Бюл. № 13 (45) Опубликовано: 19.12.2018 Бюл. № 35 (86) Заявка PCT: C 2 C 2 (85) Дата начала рассмотрения заявки PCT на национальной фазе: 28.10.2015 EP 2014/056344 (28.03.2014) (87) Публикация заявки PCT: WO 2014/154886 (02.10.2014) 2 6 7 5 3 7 1 2 6 7 5 3 7 1 Приоритет(ы): (30) Конвенционный приоритет: Адрес для переписки: 191036, Санкт-Петербург, а/я 24, "НЕВИНПАТ" (54) Способ радиоактивного мечения (57) Реферат: Изобретение относится к способу получения радиофармацевтической композиции, содержащей [18F]-1-амино-3-фторциклобутан-1-карбоновую R U R U 28.03.2014 (72) Автор(ы): ВИКСТРОМ Торильд (NO) кислоту ([18F]-FACBC, также известную как [18F] -флуцикловин), полезной в качестве индикатора Стр.: 1 для позитронно-эмиссионной томографии (ПЭТ). Способ по изобретению особенно подходит при автоматизации и предоставляет преимущества по сравнению с другими способами. 15 з.п. ф-лы, 2 пр., 2 табл. RUSSIAN FEDERATION (19) RU (11) (13) 2 675 371 C2 (51) Int. Cl. A61K 51/04 ...

Method for preparing 3(4),8(9)-bisformyltricyclo[5.2.1.02,6]decane

The present invention relates to a method for preparing 3(4),8(9)-bisformyltricyclo[5.2.1.0 2,6 ]decane. According to the present invention, a separate catalyst recovery process is not required, and 3(4),8(9)-bisformyltricyclo[5.2.1.0 2,6 ]decane (TCDDA) having a high conversion rate and purity can be prepared.

Attractants for the Mediterranean fruit fly

Novel attractants for the Mediterrean Fruit fly, "Medfly" comprise isomeric blends of C l -C₅ alkyl esters of iodo- trans -2-methylcyclohexanecarboxylic acid.

Acetylcycloundecane and acetylcycloundecenes, their preparation and use in perfumery composition and as an odorant

A B S T R A C T Cyclic compounds adapted for perfumery use selected from the group consisting of acetylcycloundecane having the formula: , an acetylcycloundecene having the formula: where the double bond is in one of the three positions designated by the dashed lines, and mixtures of said three acetylcycloundecene isomers; their synthesis, their use as a perfumery agent and as an olefactant component in perfumery compositions and as an odorant for technical products. The compounds are perfumes with strong, woody-earthy lonone-ambergris odor nuances. They are used in perfume combinations in an amount of from 1% to 5% by weight.

LIQUID CRYSTALLINE SUBSTANCES AND PROCESS FOR THEIR MANUFACTURE

Patent FR6596M

DERIVATIVES OF BICYCLO ACID (3.2.1.) CARBOXYLIC OCTANE, THEIR PREPARATION PROCESS AND THEIR THERAPEUTIC APPLICATION

Patent FR2345423B1

PROCESS FOR PRODUCING 4-HOMOISOTWISTANE-3-CARBOXYLIC ACID

Fungicidal bactericidal cyclopropane carboxylic acid derivs. - are intermediates in prepn. of insecticidal, acaricidal, nematocidal and antifungal ester(s)

Cyclopropanecarboxylic acid derivs. of formula (I) and their functional derivs. are new. In (I), X1 is H, F, Cl or Br; X2 is F, Cl or Br; and X3 is Cl, Br or I. (I) have fungicidal properties and are partic. suitable for combatting phytopathogenic fungi, e.g. on vines, tomatoes and cucumbers. They also have bactericidal properties and can be used as industrial biocides. (I) and their functional derivs. are also useful as intermediates for esters of the acids (I) which have insecticidal, acaricidal, nematocidal and antifungal properties. Specific (I) is (1R-cis)-2,2-dimethyl-3-(1,2,2,2-tetrabromoethyl)-cyclopropane-1-- carboxylic acid.

Patent JPH0226617B2

CARBOXYL DISPIROCYCLOPROPANE ESTERS WITH PESTICIDE PROPERTIES

LIQUID CRYSTALLINE SUBSTANCES FOR THE DISPLAY OF INFORMATION AND METHOD FOR THE PRODUCTION THEREOF

Patent FR2395247B1

New dicarboxy-adamantanes and their manufacturing process

Patent FR2398714B1

Patent FR8413M

ADAMANTANE DERIVATIVES AND THEIR APPLICATION

PROCESS FOR THE PRODUCTION OF TRICYCLO (5.2.1.02,6) DECANE-2-CARBOXYLIC ACID

PROCEDE DE PRODUCTION DE L'ACIDE TRICYCLO 5.2.1.0 DECANE-2-CARBOXYLIQUE. POUR OBTENIR L'ACIDE TRICYCLO 5.2.1.0 DECANE-2-CARBOXYLIQUE, ON MET EN CONTACT LE TRICYCLO 5.2.1.0 DEC-8-YL FORMATE (II) AVEC UN CATALYSEUR MINERAL DE CARACTERE FORTEMENT ACIDE. (CF DESSIN DANS BOPI) LES DERIVES ESTERS ET ALCOOLS DE CET ACIDE SONT DES PARFUMS. PROCESS FOR THE PRODUCTION OF TRICYCLO 5.2.1.0 DECANE-2-CARBOXYLIC ACID. TO OBTAIN TRICYCLO 5.2.1.0 DECANE-2-CARBOXYLIC ACID, THE TRICYCLO 5.2.1.0 DEC-8-YL FORMATE (II) IS IN CONTACT WITH A MINERAL CATALYST OF STRONG ACID CHARACTER. (CF DRAWING IN BOPI) ESTERS AND ALCOHOLS DERIVATIVES OF THIS ACID ARE PERFUMES.

BICYCLO (3.2.1.) OCTANE CARBOXYLIC ACID DERIVATIVES, PROCESS FOR THEIR PREPARATION AND THEIR THERAPEUTIC APPLICATION

La présente invention est relative à des dérivés de l'acide bicyclo(3.2.1.)octane carboxylique de formule générale suivante : " cf. formule dans BOPI " dans laquelle R représente un radical alcoyle inférieur droit ou ramifié, Z représente le groupement OX dans lequel X est l'hydrogène ou une base alcaline, ou Z représente encore le groupe N-(R1)(R2) dans lequel R1 et R2, identiques ou différents , sont l'hydrogène ou un radical alcoyle inférieur. Ces composés sont utilisables en thérapeutique notamment en raison de leurs activités anticonvulsivante et antianoxique.

Process for the preparation of steroid analogues

Patent FR2019929A1

TRICYCLO ACID (4.3.1.1 2,5) UNDECANE-1-CARBOXYLIC, ITS DERIVATIVES AND THEIR PREPARATION PROCESS

a. Acide tricyclo Ø4.3.1.1 ** 2,5õ undécane-1-carboxylique, ses dérivés et leur procédé de préparation. b. Ces composés répondent à la formule : at. Tricyclo acid Ø4.3.1.1 ** 2,5õ undecane-1-carboxylic, its derivatives and process for their preparation. b. These compounds correspond to the formula:

Process for the production of adamantane-carboxaldehydes and intermediate products obtained in the implementation of this process

Vicinal cyclanicarboxylic acids

Patent FR2409997A1

L'INVENTION A TRAIT AU DOMAINE DE LA CHIMIE PHARMACEUTIQUE. ELLE CONCERNE DE NOUVEAUX ANALOGUES, 5,6-DIHYDRO DE PROSTAGLANDINE I ET UN PROCEDE PERMETTANT DE LES OBTENIR. LES COMPOSES DE L'INVENTION INHIBENT L'AGREGATION DES PLAQUETTES OU L'ACIDITE GASTRIQUE CHEZ LES PATIENTS DONT L'ETAT NECESSITE CE TYPE DE TRAITEMENT. THE INVENTION RELATES TO THE FIELD OF PHARMACEUTICAL CHEMISTRY. IT CONCERNS NEW ANALOGUES, 5,6-DIHYDRO OF PROSTAGLANDIN I AND A PROCESS FOR OBTAINING THEM. THE COMPOUNDS OF THE INVENTION INHIBIT PLATELET AGGREGATION OR GASTRIC ACIDITY IN PATIENTS WHOSE CONDITION REQUIRES THIS TYPE OF TREATMENT.

Disubstituted pyrimidines

Pyrimidines of the formula: ##STR1## wherein Y is nitrogen and Z is ═CH--, or Z is nitrogen and Y is ═CH--; R 1 is alkyl and R 2 is cyano, alkyl, p-alkylphenyl or trans-4-alkylcyclohexyl; where each alkyl denotes either a straight chain alkyl group of 1 to 12 carbon atoms or a branched chain alkyl group of the formula C 2 H 5 --CH(CH 3 )--(CH 2 ) n , n is 1, 2 or 3; with the proviso that the compound contains at most only one of said branched chain alkyl group and with the further proviso that the sum of the carbon atoms in all of the alkyl groups within the compound is at most 14 are described. Liquid crystalline mixtures comprising Compound I as well as their use in electro-optical devices also are disclosed.

PROCEDURE FOR THE PREPARATION OF PSYCHOTROPIC POLYCLIC IMIDES.

LAS AMIDAS SUSTITUIDAS DE FORMULA (I) DONDE X, R, R1 Y R2 REPRESENTAN SUSTANCIAS CUYA FORMULA SE DESCRIBE SON AGENTES ANTOPSICOTICOS Y ANSIOLITICOS CON MUY PEQUEÑOS EFECTOS SECUNDARIOS EXTRAPIRAMIDALES. THE SUBSTITUTED AMIDES OF FORMULA (I) WHERE X, R, R1 AND R2 REPRESENT SUBSTANCES WHOSE FORMULA IS DESCRIBED ARE ANTOPSYCHOTIC AND ANSIOLITICAL AGENTS WITH VERY SMALL EXTRAPIRAMIDAL SIDE EFFECTS.

Purification of bicyclic acid c10h16o2

Salts and crystalline forms of a pd-1/pd-l1 inhibitor

This application relates to solid forms and salt forms of the PD-1/PD-L1 inhibitor 4,4'-(((((2,2'-dichloro-[1,1'-biphenyl]-3,3'-diyl)bis(azanediyl))bis(carbonyl))bis(1-methyl-1,4,6,7-tetrahydro-5H-imidazo[4,5-c]pyridine-2,5-diyl))bis(ethane-2,1-diyl))bis(bicyclo[2.2.1]heptane-1-carboxylic acid), including processes of preparation thereof, where the solid forms and salt forms are useful in the treatment of various diseases including infectious diseases and cancer.

Magnesium adamantane carboxylate and magnesium oxide nanocomposite

Adamantylamino-tetrahydronaphthyl-oxypropanols and ester derivatives

CH(-R4)-N(-R3)-(CH2)M-)ADAMANTANE AND TO SALTS OF SUCH COMPOUNDS, PRODUCTS WHICH ARE USEFUL IN CORONARY DISEASES AND AS ANTIVIRAL AGENTS. THIS INVENTION RELATES TO NEW ADAMANTYLAMINO-5,6,7,8,TETRAHYDRONAPHTHYLOXYPROPANOLS AND RELATED COMPOUNDS OF THE FORMULA 3-R1,5-R2,7-((TETRAHYDRONAPHTHYL)-O-C(-R5)(-R6)-CH(-O-R7)-

Preparation of 1, 4-cyclohexadiene-1-carboxylic acid

Patent RU2015138540A3

`”ВУ“” 2015138540'`” АЗ Дата публикации: 01.03.2018 Форма № 18 ИЗ,ПМ-2011 Федеральная служба по интеллектуальной собственности Федеральное государственное бюджетное учреждение «Федеральный институт промышленной собственности» ж 9 (ФИПС) ОТЧЕТ О ПОИСКЕ 1. . ИДЕНТИФИКАЦИЯ ЗАЯВКИ Регистрационный номер Дата подачи 2015138540/15(059157) 28.03.2014 РСТ/ЕР2014/056344 28.03.2014 Приоритет установлен по дате: [ ] подачи заявки [ ] поступления дополнительных материалов от к ранее поданной заявке № [ ] приоритета по первоначальной заявке № из которой данная заявка выделена [ ] подачи первоначальной заявки № из которой данная заявка выделена [ ] подачи ранее поданной заявки № [Х] подачи первой(ых) заявки(ок) в государстве-участнике Парижской конвенции (31) Номер первой(ых) заявки(ок) (32) Дата подачи первой(ых) заявки(ок) (33) Код страны 1. 1305687.4 28.03.2013 ОВ Название изобретения (полезной модели): [Х] - как заявлено; [ ] - уточненное (см. Примечания) Способ радиоактивного мечения Заявитель: ДжиИ Хелткер Лимитед, СВ 2. ЕДИНСТВО ИЗОБРЕТЕНИЯ [Х] соблюдено [ ] не соблюдено. Пояснения: см. Примечания 3. ФОРМУЛА ИЗОБРЕТЕНИЯ: [Х] приняты во внимание все пункты (см. Примечания) [ ] приняты во внимание следующие пункты: [ ] принята во внимание измененная формула изобретения (см. Примечания) 4. КЛАССИФИКАЦИЯ ОБЪЕКТА ИЗОБРЕТЕНИЯ (ПОЛЕЗНОЙ МОДЕЛИ) (Указываются индексы МПК и индикатор текущей версии) Аб/1К 51/04 (2006.01) 5. ОБЛАСТЬ ПОИСКА 5.1 Проверенный минимум документации РСТ (указывается индексами МПК) Аб1К 51/00, Аб1К 51/02, Аб1К 51/04 5.2 Другая проверенная документация в той мере, в какой она включена в поисковые подборки: 5.3 Электронные базы данных, использованные при поиске (название базы, и если, возможно, поисковые термины): Езрасепе, Соозе, Ра еагсв, РиБМеа, КОРТО 6 ДОКУМЕНТЫ, ОТНОСЯЩИЕСЯ К ПРЕДМЕТУ ПОИСКА Кате- Наименование документа с указанием (где необходимо) частей, Относится к гория* относящихся к предмету поиска пункту формулы № 1 2 3 х \/О 2012089594 АТ ( ...

Resist composition, method of forming resist pattern, acid generator, photoreactive quencher, and compound

A resist composition which generates acid upon exposure and exhibits changed solubility in a developing solution under action of acid, and which includes a base component which exhibits changed solubility in a developing solution under action of acid and an acid-generator component including a compound (B0-1) represented by general formula (b0) shown below in which Ra 1 represents an aromatic ring; Ra 01 represents an alkyl group of 5 or more carbon atoms optionally having a substituent; Ra 02 and Ra 03 each independently represents an alkyl group of 1 to 10 carbon atoms optionally having a substituent; n1 represents an integer of 1 to 5; n2 represents an integer of 0 to 2; n3 represents an integer of 0 to 4; and X − represents a counteranion.

Preparation of bicyclohexane derivative

A process for the preparation of (+)-2-amino-bicyclo¢3.1.0!-hexane-2-6-dicarboxylic acid, or a pharmaceutically acceptable salt thereof, which comprises hydrolysing (-)-2-spiro-5'-hydantoinbicyclo¢3.1.0!hexane-6-carboxylic acid or a salt thereof, and optionally forming a pharmaceutically acceptable salt. Also disclosed are novel intermediates useful in the process.