SUPERACID FUNCTIONAL COMPOUNDS

The invention relates to a novel synthesis method for forming superacid functional molecules that include monomers, as well as new polymers and copolymers formed from the monomers, and uses for these superacid molecules, polymers, and copolymers. The superacid molecules have an alpha,alpha-difluorosulfonic acid functionality that can be obtained by a reaction between various Grignard reagents and an alkyl(2-fluorosulfonyl)-1,1-difluoroacetate, such as methyl(2-fluorosulfonyl-1,1-difluoroacetate. The molecules, polymers and copolymers would be expected to have enhanced ion conductivity, and would be useful in a variety of applications, including as ion-conductive materials, surfactants, and ion exchange resins. 3. The composition of where one of the groups claim 2 , R claim 2 , is vinylic claim 2 , and the other groups Rare hydrogen.4. The composition of where Ris chosen from: sulfonate claim 1 , sulfinate claim 1 , or sulfonyl halide.5. The composition of where one of the groups claim 2 , R claim 2 , is vinylic claim 2 , the other groups Rare hydrogen claim 2 , and Ris sulfonyl halide or sulfonate.7. The composition of where the group claim 6 , Ris selected from the group consisting of: sulfonate claim 6 , sulfinate claim 6 , and sulfonyl halide.9. The copolymer of having a weight average molecular weight of 500 kg/mol or less.10. The copolymer of claim 8 , comprising three or more monomer units.14. A polymer blend comprising from 5 to 95 weight percent of said homopolymer or copolymer composition of claim 8 , with from 5 to 95 weight percent of a matrix polymer.15. The polymer blend of claim 13 , comprising a blend of at least two different sulfonated polyelectrolytes claim 13 , each comprising from 5 to 95 weight percent of said blend.16. The polymer blend of claim 13 , wherein said matrix polymer is fluorinated.17. The polymer blend of claim 15 , wherein said matrix polymer comprises a poly(vinylidene fluoride) homopolymer or copolymer.18. The polymer blend of ...

Benzoxazine-thiol adducts

Novel benzoxazine-thiol adducts are described, which may be may be cured to produce compositions useful in coating, sealants, adhesive and many other applications.

DITHIOAMINE REDUCING AGENTS

Dithioamine reducing agents useful for the reduction of disulfide bonds. The reducing agents of this invention are useful, for example, to reduce disulfide bonds, particularly in proteins, or to prevent the formation of disulfide bonds, particularly in proteins and other biological molecules. Reducing agents of this invention are useful and suitable for application in a variety of biological applications, particularly as research and synthetic reagents. The invention provides S-acylated dithioamines which can be selectively activated reducing agents by removal of the S-acyl groups enzymatically or chemically. The invention further provides dithiane precursors of thioamino reducing agents. The invention provides dithioamine reducing agents, S-acylated dithioamines and dithianes which are immobilized on surfaces, including among others, glass, quartz, microparticles, nanoparticles and resins. 2. The compound of wherein neither Ror Ris an —NHgroup.3. The compound of wherein R claim 1 , Rand Rare all hydrogens.4. The compound of wherein R claim 1 , R claim 1 , R claim 1 , Rand Rare all hydrogens.5. The compound of wherein both Rare hydrogens.6. The compound of wherein both of Rare acyl groups.7. The compound of wherein one of Ror Ris an acyl group.8. The compound of wherein both of Ror Rare hydrogens.9. The compound of wherein Ror Ris -M.10. The compound of wherein Ror Ris -L-T.11. The compound of wherein R-Rare all hydrogens.12. The compound of wherein R-Rare all hydrogens and each Ris a —CO—Rwherein Ris an alkyl group having 1-6 carbon atoms claim 1 , a halogen-substituted alkyl group having 1-6 carbon atoms claim 1 , a hydroxy-substituted alkyl group having 1 to 6 carbon atoms claim 1 , an optionally substituted phenyl group or an optionally substituted benzyl group.13. The compound of wherein R claim 1 , R claim 1 , Rand one of Ror Rare all hydrogens and the other of Ror Ris an optionally substituted alkyl group having 1-3 carbons atoms claim 1 , a halogen claim 1 , ...

COPPER(I)-ION SELECTIVE FLUORESCENT PROBE, METHOD FOR PREPARING THE SAME, METHOD FOR DIAGNOSING MALIGNANT DISEASE AND DIAGNOSIS KIT USING THE PROBE

The present disclosure relates to a copper (I) ion-selective fluorescent probe, a method for preparing the same, and a method for diagnosing malignant disease and a diagnosis kit using the probe. The fluorescent probe according to the present disclosure is capable of detecting free copper (I) ions inside cells for a long time with high selectivity and sensitivity for copper (I) ion, with a penetration depth longer than 90 μm in living cells and tissues and without the problems of mistargeting and photobleaching. Accordingly, since a biological sample can be imaged for a long period of time with high resolution without damage, presence of malignance disease in the target biological sample can be diagnosed faster, more accurately and more easily. 2. The copper(I) ion-selective fluorescent probe of claim 1 , wherein Ris hydrogen claim 1 , methyl or methoxy.3. The copper(I) ion-selective fluorescent probe of claim 1 , wherein Ris hydrogen or methoxy.10. The method for diagnosing malignant disease as set forth in claim 8 , wherein the malignant disease is respiratory cancer claim 8 , gastrointestinal cancer or breast cancer.11. The method for diagnosing malignant disease as set forth in claim 8 , wherein the malignant disease is diagnosed when the ratio is between 1.657 and 2.169. This application claims priority under 35 U.S.C. §119 to Korean Patent Application Nos. 10-2011-0104150 and 10-2012-0015602, filed on Oct. 12, 2011 and Feb. 16, 2012, respectively, in the Korean Intellectual Property Office, the disclosure of which is incorporated herein by reference in its entirety.The present disclosure relates to a copper(I) ion-selective fluorescent probe, a method for preparing the same, and a method for diagnosing malignant disease and a diagnosis kit using the probe.Copper ion, existing either as oxidized copper(II) ion (Cu) or as reduced copper(I) ion (Cu), is the essential probing metal found in the organs of living organisms. It acts as cofactor in many reactions by ...

RHEUMATOID ARTHRITIS TREATMENT

A compound of formula (I) 2. A compound of formula (II){'br': None, 'R-L1-CO—X \u2003\u2003(II)'}(wherein R and X are as hereinbefore defined;{'sub': '2', 'L1 is a linking group forming a bridge of 1 to 5 atoms between the R group and the carbonyl CO, the atoms forming the backbone of said linking group being selected from carbon and/or the heteroatoms N, O, S, SO, SO,'}{'sub': '2', 'wherein the linking group L1 comprises a ring within the backbone or is linear and the backbone atoms of the linking group are substituted with at least one side chain (in addition to any oxo group of SO or SO) or a salt thereof.'}3. A compound as claimed in having the formula (IV){'br': None, 'R—Y3-Y4-CO—X \u2003\u2003(IV)'}wherein R and X are as hereinbefore defined;Y3 and Y4 taken together form a 5 or 6 membered homo or heterocyclic, saturated, unsaturated or aromatic ring; or{'sub': '2', 'Y3 forms a 5 or 6 membered homo or heterocyclic, saturated, unsaturated or aromatic ring and Y4 is (CH)n;'}where n is 1 to 3, preferably 1.7. A compound as claimed in any preceding claim wherein the group X is CN claim 2 , phenyl claim 2 , CHal claim 2 , CHalH claim 2 , CHalHwherein Hal represents a halogen claim 2 , e.g. fluorine claim 2 , chlorine claim 2 , bromine or iodine claim 2 , preferably fluorine.8. A compound as claimed in any preceding claim wherein the group X is CF.9. A compound as claimed in any preceding claim wherein the L or L1 group comprises an S atom claim 2 , especially β to the carbonyl.10. A compound as claimed in any preceding claim wherein R contains 5 non conjugated double bonds.12. A method of treating rheumatoid arthritis comprising administering to an animal claim 2 , preferably a mammal claim 2 , e.g. human claim 2 , an effective amount of a compound as claimed in any preceding claim.13. Use of a compound as claimed in any one of to for use in the manufacture of a medicament for treating rheumatoid arthritis.14. A compound of formula (I){'br': None, 'R-L-CO—X \u2003\ ...

6,7-DIHYDRO-5H-BENZO[7]ANNULENE DERIVATIVES, PROCESS FOR PREPARATION THEREOF, PHARMACEUTICAL PREPARATIONS COMPRISING THEM, AND THE USE THEREOF FOR PRODUCTION OF MEDICAMENTS

The invention relates to selective oestrogen receptor modulators (SERM) and methods of production thereof, use thereof for the treatment and/or prophylaxis of diseases and use thereof for the production of medicinal products for the treatment and/or prophylaxis of diseases, in particular of bleeding disorders, osteoporosis, endometriosis, myomata, hormone-dependent tumours, for hormone replacement therapy and for contraception. 6. A Compound according to that is8-(3,5-Difluorophenyl)-9-[6-(methyl{3-[(4,4,5,5,5-pentafluoropentyl)sulphonyl]propyl}amino)hexyl]-6,7-dihydro-5H-benzo[7]annulen-3-ol;8-(3,5-Difluorophenyl)-9-[6-(methyl{3-[(3,3,4,4,4-pentafluorobutyl)sulphinyl]propyl}amino)hexyl]-6,7-dihydro-5H-benzo[7]annulen-3-ol;8-(3,5-Difluorophenyl)-9-[6-(methyl{3-[(3,3,4,4,4-pentafluorobutyl)sulphonyl]propyl}amino)hexyl]-6,7-dihydro-5H-benzo[7]annulen-3-ol;8-(3,5-Difluorophenyl)-9-[6-(methyl{4-[(4,4,5,5,5-pentafluoropentyl)sulphinyl]butyl}amino)hexyl]-6,7-dihydro-5H-benzo[7]annulen-3-ol;8-(3,5-Difluorophenyl)-9-[6-(methyl{3-[(3,3,3-trifluoropropyl)sulphinyl]propyl}amino)hexyl]-6,7-dihydro-5H-benzo[7]annulen-3-ol;8-(3,5-Difluorophenyl)-9-[6-(methyl{3-[(3,3,3-trifluoropropyl)sulphonyl]propyl}amino)hexyl]-6,7-dihydro-5H-benzo[7]annulen-3-ol;8-(3,5-Difluorophenyl)-9-[6-(methyl{3-[(4,4,4-trifluorobutyl)sulphonyl]propyl}amino)hexyl]-6,7-dihydro-5H-benzo[7]annulen-3-ol;8-(3,5-Difluorophenyl)-9-[6-(methyl{3-[(4,4,5,5,5-pentafluoropentyl)sulphinyl]propyl}amino)hexyl]-6,7-dihydro-5H-benzo[7]annulen-3-ol;8-(3,5-Difluorophenyl)-9-[6-(methyl{4-[(4,4,5,5,5-pentafluoropentyl)sulphonyl]butyl}amino)hexyl]-6,7-dihydro-5H-benzo[7]annulen-3-ol;8-(3,5-Difluorophenyl)-9-{6-[(2-hydroxy-2-methylpropyl) {3-[(3,3,3-trifluoropropyl)sulphinyl]propyl}amino]hexyl}-6,7-dihydro-5H-benzo[7]annulen-3-ol;8-(3,5-Difluorophenyl)-9-{6-[(2-hydroxy-2-methylpropyl) {3-[(3,3,3-trifluoropropyl)sulphonyl]propyl}amino]hexyl}-6,7-dihydro-5H-benzo[7]annulen-3-ol;8-(3,5-Difluorophenyl)-9-{6-[(2-hydroxy-2- ...

4-(PHENOXYALKYL)THIO)-PHENOXYACETIC ACIDS AND ANALOGS

The invention features 4-((phenoxyalkyl)thio)-phenoxyacetic acids and analogs, compositions containing them, and methods of using them as PPAR delta modulators to treat or inhibit the progression of, for example, dyslipidemia. 195-. (canceled)97. The pharmaceutical composition of wherein the pharmaceutical composition is a tablet or a capsule.98. A method of treating a condition selected from the group consisting of diabetes claim 96 , cardiovascular diseases claim 96 , Metabolic X Syndrome claim 96 , hypercholesterolemia claim 96 , hypo-HDL-cholesterolemia claim 96 , hyper-LDL-cholesterolemia claim 96 , dyslipidemia claim 96 , atherosclerosis claim 96 , and obesity claim 96 , comprising administering to a patient in need of treatment a pharmaceutical composition of .100. The pharmaceutical composition of wherein the pharmaceutical composition is a tablet or a capsule.101. A method of treating a condition selected from the group consisting of diabetes claim 99 , cardiovascular diseases claim 99 , Metabolic X Syndrome claim 99 , hypercholesterolemia claim 99 , hypo-HDL-cholesterolemia claim 99 , hyper-LDL-cholesterolemia claim 99 , dyslipidemia claim 99 , atherosclerosis claim 99 , and obesity claim 99 , comprising administering to a patient in need of treatment a pharmaceutical composition of .103. The pharmaceutical composition of wherein the pharmaceutical composition is a tablet or a capsule.104. A method of treating a condition selected from the group consisting of diabetes claim 102 , cardiovascular diseases claim 102 , Metabolic X Syndrome claim 102 , hypercholesterolemia claim 102 , hypo-HDL-cholesterolemia claim 102 , hyper-LDL-cholesterolemia claim 102 , dyslipidemia claim 102 , atherosclerosis claim 102 , and obesity claim 102 , comprising administering to a patient in need of treatment a pharmaceutical composition of . This application claims priority to U.S. Provisional Patent Application No. 60/504,146, filed Sep. 19, 2003, which is hereby incorporated ...

Therapeutic polyamine compositions and their synthesis

This invention relates to a process of synthesis and composition of open chain (ring), closed ring, linear branched and or substituted polyamines, polyamine derived tyrosine phosphatase inhibitors and PPAR partial agonists/partial antagonists via a series of substitution reactions and optimizing the bioavailability and biological activities of the compounds. Polyamines prevent the toxicity of neurotoxins and diabetogenic toxins including paraquat, methyphenyl pyridine radical, rotenone, diazoxide, streptozotocin and alloxan. These polyamines can be utilized to treat neurological, cardiovascular, endocrine acquired and inherited mitochondrial DNA damage diseases and other disorders in mammalian subjects, and more specifically to the therapy of Parkinson's disease, Alzheimer's disease, Lou Gehrig's disease, Binswanger's disease, Olivopontine Cerebellar Degeneration, Lewy Body disease, Diabetes, Stroke, Atherosclerosis, Myocardial Ischemia, Cardiomyopathy, Nephropathy, Ischemia, Glaucoma, Presbycussis, Cancer, Osteoporosis, Rheumatoid Arthritis, Inflammatory Bowel Disease, Multiple Sclerosis and as Antidotes to Toxin Exposure. 1. A method of treating degenerative diseases due to acquired mitochondrial DNA damage , redox damage to mitochondrial macromolecules and inherited mitochondrial genetic defects said method comprising the steps of:selecting a composition from a group consisting of predominantly linear tetraamines and polyamines linked by 1,3-propylene and/or ethylene groups, predominately branched tetraamines and polyamines linked by 1,3-propylene and/or ethylene groups, cyclic polyamines linked by 1,3-propylene and/or ethylene groups, combinations of linear, branched and cyclic polyamines linked by one or more 1,3-propylene and/or ethylene groups, substituted polyamines, polyamines derivatized to form tyrosine phosphatase inhibitor molecules with linear or branched chains attached, polyamine derivatives of 2,2′-diaminobiphenyl with linear or branched chains ...

Perfluoroalkyl Composition with Reduced Chain Length

Novel fluorosurfactants are provided that contain perfluoroalkyl groups no longer than perfluorohexyl (C). The surfactants are useful in the preparation of aqueous film forming foams (AFFF) and alcohol-resistant film-forming foams (AR-AFFF) for firefighting. Unexpectedly, these compounds have activity in AFFF and AR-AFFF applications that is comparable and even superior to conventional surfactants that contain perfluoroalkyl groups that are perfluorooctyl (C) and longer. Also provided are methods of making the novel surfactants, as well as foam concentrates, methods of making foam and methods of fighting fires using foam containing the novel surfactants. 2. The composition according to wherein Ris CF(CF).3. The composition according to wherein A is —CHCH—S—.4. The composition according to wherein m is 4.5. The composition according to wherein X is —S—.6. The composition according to wherein the weight average molecular weight of said surfactant is 750-7500.8. The composition according to wherein p is 4-20.9. An aqueous firefighting composition concentrate comprising an effective amount of a composition according to claim 1 , wherein said firefighting composition is substantially free of any surfactant containing a perfluoroalkyl group containing more than 6 carbon atoms.10. (canceled)11. The composition according to claim 9 , wherein said composition further comprises an effective amount of one or more components selected from the group consisting of: an amphoteric hydrocarbon surfactant claim 9 , an anionic hydrocarbon surfactant claim 9 , a nonionic hydrocarbon surfactant claim 9 , a Cfluorochemical surfactant claim 9 , a foam aid claim 9 , a freeze protection composition claim 9 , a composition comprising ion sequestering claim 9 , buffer claim 9 , and anti-corrosion components claim 9 , a polymeric film forming composition claim 9 , a biocides and antimicrobial composition claim 9 , an electrolyte composition claim 9 , and a polysaccharide gum thickener.12. The ...

SYNTHESIS AND GROWTH REGULATORY ACTIVITY OF A PROTOTYPE MEMBER OF A NEW FAMILY OF AMlNOTHIOL RADIOPROTECTORS

The synthesis, growth inhibition and radioprotective activity of the PrC-210 aminothiol, 3-(methyl-amino)-2-((methylamino)methyl)propane-1-thiol, and its polyamine and thiolated polyamine progenitors are reported. All of the molecules significantly inhibited growth of cultured normal human fibroblasts. The combination of an ROS-scavenging thiol group and a positively charged alkyl-amine backbone provided the most radioprotective aminothiol molecule. 120.-. (canceled)21. A systemically administered radioprotector comprising a free thiol and a positively-charged backbone.22. The systemically administered radioprotector of wherein the positively-charged backbone comprises an amine.24. The systemically administered radioprotector of wherein administering systemically to a subject the systemically administered radioprotector does not cause a side effect of nausea claim 21 , vomiting claim 21 , hypotension claim 21 , or fainting in the subject.25. The systemically administered radioprotector of wherein the systemically administered radioprotector is sulfurous odor-free.26. A complex comprising the systemically administered radioprotector of bound to the positively-charged backbone of a DNA.27. The complex of wherein the systemically administered radioprotector displays the free thiol away from the DNA.28. A cell comprising the systemically administered radioprotector of .29. A cell comprising the complex of . This application claims priority to U.S. Pat. Appl. Ser. No. 61/713,050, which is incorporated herein by reference in its entirety.The synthesis, growth inhibition and radioprotective activity of the PrC-210 aminothiol, 3-(methyl-amino)-2-((methylamino)methyl)propane-1-thiol, and its polyamine and thiolated polyamine progenitors are reported. All of the molecules significantly inhibited growth of cultured normal human fibroblasts. The combination of an ROS-scavenging thiol group and a positively charged alkyl-amine backbone provided the most radioprotective ...

SYNTHESIS AND GROWTH REGULATORY ACTIVITY OF A PROTOTYPE MEMBER OF A NEW FAMILY OF AMlNOTHIOL RADIOPROTECTORS

The synthesis, growth inhibition and radioprotective activity of the PrC-210 aminothiol, 3-(methyl-amino)-2-((methylamino)methyl)propane-1-thiol, and its polyamine and thiolated polyamine progenitors are reported. All of the molecules significantly inhibited growth of cultured normal human fibroblasts. The combination of an ROS-scavenging thiol group and a positively charged alkyl-amine backbone provided the most radioprotective aminothiol molecule.

PREPARATION OF SULFONAMIDE HERBICIDE PROCESS INTERMEDIATES

Improved methods for preparing chemical precursors to sulfonyl chloride III, which are important intermediates in the preparation of pyroxsulam herbicide are provided. Specifically, these precursors are compounds of Formulas VII and/or VIII, and IX, wherein R is a C-Calkyl, Ris a C-Calkyl, X is Cl or OH, Y is halogen, OH, or OR, and Ris a C-Calkyl. 2. The method of claim 1 , further comprising preparing the compound of Formula IV by a method by combining an alkyl mercaptan RSH claim 1 , a haloacetonitrile Y—CHCN claim 1 , and a second base claim 1 , wherein R is a C-Calkyl claim 1 , and Y is a halogen.4. The method of claim 3 , wherein the acid is HSO claim 3 , HCl claim 3 , HBr claim 3 , HI or p-toluenesulfonic acid.5. The method of claim 3 , wherein the alcohol is a C-Calcohol.6. The method of claim 3 , wherein the alkoxide is a C-Csodium or potassium alkoxide.7. The method of claim 3 , wherein the dehydrative halogenating reagent is SOCl claim 3 , SOBr claim 3 , POCl claim 3 , POBr claim 3 , PCl claim 3 , PBr claim 3 , PClor PBr claim 3 , or oxalyl chloride claim 3 , and combinations thereof.8. The method of claim 3 , wherein the alcohol is methanol.9. The method of claim 3 , wherein the alkoxide is sodium methoxide or potassium methoxide.10. The method of claim 3 , wherein the combining includes the simultaneous combination of the acid and the alcohol with the compound of Formula VII or Formula VIII claim 3 , or mixtures thereof claim 3 , to provide the compound of Formula IX wherein R is a C-Calkyl claim 3 , and Y is OR claim 3 , wherein Ris a C-Calkyl.11. The method of claim 3 , wherein the combining includes the simultaneous combination of the acid and water with the compound of Formula VII or Formula VIII claim 3 , and mixtures thereof claim 3 , to provide the compound of Formula IX wherein R is a C-Calkyl claim 3 , and Y is OH.12. The method of claim 3 , wherein the combining includes the sequential combination of an acid that is HCl or HBr claim 3 , and ...

METHODS FOR REDUCING TRIGLYCERIDE, TOTAL CHOLESTEROL AND LOW DENSITY LIPOPROTEIN BLOOD LEVELS

A compound of Formula (I): 4. The method of claim 1 , in which the subject is diagnosed with hypertriglyceridemia.5. The method of claim 1 , in which the compound is administered orally.6. The method of claim 1 , in which the compound is administered once daily claim 1 , twice daily claim 1 , or thrice daily.7. The method of claim 1 , in which the compound is administered as a liquid or solid dosage form.8. The method of claim 1 , in which the compound is administered orally in a solid dosage form and is present in an orthorhombic crystalline form (“substantially free of other polymorphic forms”—mention in the specification but not in the claims).9. The method of claim 1 , in which the compound is administered in an amount ranging from 50 mg/day to 5 claim 1 ,000 mg/day claim 1 , optionally divided into one claim 1 , two claim 1 , or three portions.10. The method of claim 1 , in which the compound is administered at a dosage of 50 mg claim 1 , 75 mg claim 1 , 100 mg claim 1 , 200 mg claim 1 , 500 mg claim 1 , 750 mg claim 1 , or 1 claim 1 ,000 mg once a day claim 1 , twice a day claim 1 , or three times a day.14. The method of claim 11 , in which the subject is diagnosed with hypercholesterolemia.15. The method of claim 11 , in which the compound is administered orally.16. The method of claim 11 , in which the compound is administered once daily claim 11 , twice daily claim 11 , or thrice daily.17. The method of claim 11 , in which the compound is administered as a liquid or solid dosage form.18. The method of claim 11 , in which the compound is administered orally in a solid dosage form and is present in an orthorhombic crystalline form.19. The method of claim 11 , in which the compound is administered in an amount ranging from 50 mg/day to 5 claim 11 ,000 mg/day claim 11 , optionally divided into one claim 11 , two claim 11 , or three portions.20. The method of claim 11 , in which the compound is administered at a dosage of 50 mg claim 11 , 75 mg claim 11 , 100 mg ...

DETERMINATION OF AQUEOUS NITRATE CONCENTRATION

A method of measuring nitrate concentration in an aqueous sample includes mixing the aqueous sample with a water-soluble thioether chosen to reduce nitrate in the aqueous sample to nitrite in the presence of a water soluble catalyst, and a water soluble reagent system adapted to interact with nitrite to generate a color; measuring color generation, and correlating the color generation to nitrate concentration. 1. A method of measuring nitrate concentration in an aqueous sample , comprisinga. mixing the aqueous sample with a water-soluble thioether chosen to reduce nitrate in the aqueous sample to nitrite in the presence of a water soluble catalyst, and a water soluble reagent system adapted to interact with nitrite to generate a color,b. measuring color generation, andc. correlating the color generation to nitrate concentration.2. The method of wherein the water soluble thioether comprises a thioether-containing a five-membered claim 1 , aromatic heterocyclic compound claim 1 , a phenylalkyl thioether or a substituted phenylalkyl thioether.4. The method of wherein the hydrophilic polymer is a polyalkyleneoxide.5. The method of wherein at least one of R claim 3 , R claim 3 , R claim 3 , R claim 3 , and Ris —ORwherein Ris selected from the group consisting of H claim 3 , a C-Calkyl group claim 3 , a C-Csulfonate terminated alkyl group claim 3 , a phenyl group claim 3 , and a polyalkylene oxide group claim 3 , —NRRwherein RE and Rare selected independently from the group consisting of H claim 3 , a C-Calkyl group claim 3 , a C-Csulfonate terminated alkyl group claim 3 , and a polyalkylene oxide group claim 3 , a dihydroxybenzene group claim 3 , a phenyl diamine group claim 3 , a phenyl diether group claim 3 , a carboxy late group claim 3 , and a polyalkyleneoxide group; or Rand Rtogether form a chain of four or five members selected from the group of CH claim 3 , CH claim 3 , NH claim 3 , CC(O)OH or NR claim 3 , wherein Ris an C-Calkyl group or C-Csulfonate terminated ...

ALKYNYL PHENYL DERIVATIVE COMPOUNDS FOR TREATING OPHTHALMIC DISEASES AND DISORDERS

Provided are alkynyl phenyl derivative compounds, pharmaceutical compositions thereof, and methods of treating ophthalmic diseases and disorders, such as age-related macular degeneration and Stargardt's Disease, using said compounds and compositions. 190-. (canceled)92. The compound of claim 91 , or a pharmaceutically acceptable salt thereof claim 91 , wherein Ris alkyl.93. The compound of claim 92 , or a pharmaceutically acceptable salt thereof claim 92 , wherein m is 0.94. The compound of claim 93 , or a pharmaceutically acceptable salt thereof claim 93 , wherein Rand Rare each independently hydrogen or C-Calkyl.95. The compound of claim 91 , or a pharmaceutically acceptable salt thereof claim 91 , wherein Ris aryl.96. The compound of claim 95 , or a pharmaceutically acceptable salt thereof claim 95 , wherein m is 0.97. The compound of claim 96 , or a pharmaceutically acceptable salt thereof claim 96 , wherein Rand Rare each independently hydrogen or C-Calkyl.98. The compound of claim 91 , or a pharmaceutically acceptable salt thereof claim 91 , wherein Ris carbocyclyl.99. The compound of claim 98 , or a pharmaceutically acceptable salt thereof claim 98 , wherein m is 0.100. The compound of claim 99 , or a pharmaceutically acceptable salt thereof claim 99 , wherein Rand Rare each independently hydrogen or C-Calkyl.101. The compound of claim 91 , or a pharmaceutically acceptable salt thereof claim 91 , chosen from:3-amino-1-(3-(3-hydroxy-3-propylhex-1-ynyl)phenyl)propan-1-one oxime;4-((3-(2-aminoethylamino)-phenyl)ethynyl)heptan-4-ol;4-((3-(2-aminoethylthio)phenyl)ethynyl)heptan-4-ol;4-((3-(2-aminoethylsulfinyl)phenyl)ethynyl)heptan-4-ol; or4-((3-(2-aminoethylsulfonyl)phenyl)ethynyl)heptan-4-ol.1031. A pharmaceutical composition comprising a compound of Formula (A) claim 91 , or pharmaceutically acceptable salt thereof claim 91 , as described in claim claim 91 , and a pharmaceutically acceptable excipient.104. A pharmaceutical composition comprising a compound of ...

Compositions and Methods for the Treatment of Xerostomia

The invention relates to the compounds or its pharmaceutical acceptable polymorphs, solvates, enantiomers, stereoisomers and hydrates thereof. The pharmaceutical compositions comprising an effective amount of compounds of formula I, formula II, formula III, formula IV and formula V and the methods for the treatment of xerostomia may be formulated for oral, buccal, rectal, topical, transdermal, transmucosal, lozenge, spray, intravenous, oral solution, buccal mucosal layer tablet, parenteral administration, syrup, or injection. Such compositions may be used to treatment of oral mucosal inflammatory, dry mouth or oral dry mouth mediated infectious diseases. 6. A Pharmaceutical composition comprising a compound of and a pharmaceutically acceptable carrier.7. A Pharmaceutical composition comprising a compound of and a pharmaceutically acceptable carrier.8. A Pharmaceutical composition comprising a compound of and a pharmaceutically acceptable carrier.9. A Pharmaceutical composition comprising a compound of and a pharmaceutically acceptable carrier.10. A Pharmaceutical composition comprising a compound of and a pharmaceutically acceptable carrier.11. The pharmaceutical composition of claim 6 , which is formulated to treat the underlying etiology with an effective amount administering the patient in need by oral administration claim 6 , delayed release or sustained release claim 6 , transmucosal claim 6 , syrup claim 6 , topical claim 6 , parenteral administration claim 6 , injection claim 6 , subdermal claim 6 , oral solution claim 6 , rectal administration claim 6 , buccal administration or transdermal administration.12. The pharmaceutical composition of claim 7 , which is formulated to treat the underlying etiology with an effective amount administering the patient in need by oral administration claim 7 , delayed release or sustained release claim 7 , transmucosal claim 7 , syrup claim 7 , topical claim 7 , parenteral administration claim 7 , injection claim 7 , ...

LOW VISCOSITY LUBRICATING OIL BASE STOCKS AND PROCESSES FOR PREPARING SAME

A composition that includes one or more compounds represented by the formula 2. The composition of wherein Rand Rare selected from the residue of a mPAO dimer (C-C) claim 1 , trimer (C-C) claim 1 , tetramer (C-C) claim 1 , pentamer (C-C) claim 1 , and hexamer (C-C) claim 1 , or α-olefin (C-C) claim 1 , X is selected from the residue of 1 claim 1 ,2-ethanedithiol claim 1 , 3-mercaptopropionate claim 1 , pentaerythritoltetrakis(3-mercaptopropionate) claim 1 , and trimethylopropanetris(3-mercaptopropionate) claim 1 , a is a value from 1 to 4 claim 1 , and b is a value or 0 or 1.3. The composition of having a Noack volatility of no greater than 20 percent.4. The composition of which is selected from a heteroatom-containing mPAO dimer claim 1 , trimer claim 1 , tetramer claim 1 , pentamer claim 1 , hexamer and higher oligomer claim 1 , or one or more compounds represented by a formula of .5. A composition comprising me or more heteroatom-containing hydrocarbon compounds claim 1 , wherein said one or more heteroatom-containing hydrocarbon compounds are produced by a process comprising reacting a polyalphaolefin oligomer or α-olefin (C-C) with an aliphatic polythiol claim 1 , aromatic polythiol claim 1 , cycloaliphatic polythiol claim 1 , ester or acid containing thiol claim 1 , or ester or acid containing polythiol claim 1 , optionally in the presence of a catalyst claim 1 , under reaction conditions sufficient to produce said one or more heteroatom-containing hydrocarbon compounds.6. The composition of wherein the process is carried out under reaction conditions sufficient to couple the polyalphaolefin oligomer or α-olefin (C-C) with the aliphatic polythiol claim 5 , aromatic polythiol claim 5 , cycloaliphatic polythiol claim 5 , ester or acid containing thiol claim 5 , or ester or acid containing polythiol claim 5 , to produce said heteroatom-containing hydrocarbon compound.7. The composition of having a viscosity (Kv) from 2 to 30 at 100° C. claim 5 , a viscosity index ...

LIPID CONTAINING FORMULATIONS

Compositions and methods useful in administering nucleic acid based therapies, for example association complexes such as liposomes and lipoplexes are described. 2. The compound of claim 1 , wherein Ris H claim 1 , methyl claim 1 , ethyl claim 1 , isopropyl claim 1 , or 2-hydroxyethyl and Ris H claim 1 , methyl claim 1 , ethyl claim 1 , propyl claim 1 , or isopropyl.3. The compound of claim 1 , wherein both m and n are 1.4. The compound of claim 1 , wherein both Land Lare —OC(O)— or —C(O)O—.5. The compound of claim 1 , wherein both Land Lare —N(R)C(O)N(R)—.6. The compound of claim 1 , wherein both Land Lare —OC(O)N(R)— or —N(R)C(O)O—.7. The compound of claim 1 , wherein Lis —NRC(O)— and Lis —S—S—.8. The compound of claim 1 , wherein Lis —OC(O)— and Lis —S—S—.9. The compound of claim 1 , wherein Lis —OC(O)N(R) or —N(R)C(O)O— and Lis —S—S—.10. The compound of claim 1 , wherein Lis —N(R)C(O)N(R)— and L2 is —S—S—.11. The compound of claim 1 , wherein L-Rand L-Rare taken together to form an acetal claim 1 , a ketal claim 1 , or an orthoester.12. The compound of claim 1 , wherein both Rand Rare C-Calkyl.13. The compound of claim 12 , wherein each Land Lare independently —S—S— claim 12 , —OC(O)N(R)— or —N(R)C(O)O—.14. The compound of claim 1 , wherein each Rand Rare independently C-Calkenyl.19. A preparation comprising the compound of claim 1 , or a pharmaceutically acceptable salt thereof. This application is a divisional application of U.S. patent application Ser. No. 13/211,094, filed on Aug. 16, 2011, which is a continuation application of U.S. patent application Ser. No. 12/056,230, filed on Mar. 26, 2008, which application issued as U.S. Pat. No. 8,034,376 on Oct. 11, 2011, which is a continuation application of International Patent Application No. PCT/US2007/080331, filed on Oct. 3, 2007, and claims priority to U.S. Provisional Application No. 60/828,022 filed on Oct. 3, 2006 and U.S. Provisional Application No. 60/870,457 filed on Dec. 18, 2006. The entire content ...

LIPID CONTAINING FORMULATIONS

Compositions and methods useful in administering nucleic acid based therapies, for example association complexes such as liposomes and lipoplexes are described. 3. A preparation comprising a compound of .4. An association complex comprising a preparation of .5. An association complex comprising a preparation of .6. The association complex of claim 4 , further comprising a therapeutic agent.7. The association complex of claim 6 , wherein the therapeutic agent is nucleic acid.8. The association complex of claim 6 , wherein the therapeutic agent is siRNA.9. The association complex of claim 6 , wherein the therapeutic agent is mRNA.10. The association complex of claim 5 , further comprising a therapeutic agent.11. The association complex of claim 10 , wherein the therapeutic agent is nucleic acid.12. The association complex of claim 10 , wherein the therapeutic agent is siRNA.13. The association complex of claim 10 , wherein the therapeutic agent is mRNA.14. A method of treating a mammal comprising administering to said mammal a therapeutic amount of an association complex of .15. A method of treating a mammal comprising administering to said mammal a therapeutic amount of an association complex of . This application is a Continuation application of U.S. patent application Ser. No. 14/149,496, filed on Jan. 7, 2014, which is a Divisional application of U.S. patent application Ser. No. 13/211,094, filed on Aug. 16, 2011, issued as U.S. Pat. No. 8,642,076 on Feb. 4, 2014, which is a continuation application of U.S. patent application Ser. No. 12/056,230, filed on Mar. 26, 2008, issued as U.S. Pat. No. 8,034,376 on Oct. 11, 2011, which is a continuation application of International Patent Application No. PCT/US2007/080331, filed on Oct. 3, 2007, which claims priority to U.S. Provisional Application No. 60/828,022 filed on Oct. 3, 2006 and U.S. Provisional Application No. 60/870,457 filed on Dec. 18, 2006. The entire content of each of these applications is hereby ...

4-(3-BENZYLOXYPHENYLTHIO)-2-CHLORO-1-(3-NITROPROPYL)BENZENE CRYSTAL

[Problem] For example, 4-(3-benzyloxyphenylthio)-2-chloro-1-(3-nitropropyl)benzene (compound 1) is used as an intermediate for producing a 2-amino-2-[2-[4-(3-benzyloxyphenylthio)-2-chlorophenyl]ethyl]-1,3-propanediol hydrochloride which has excellent immunosuppressive activity. This compound 1 is traditionally obtained only as an oil and thus handling and refining were difficult. 1. A crystal of 4-(3-benzyloxyphenylthio)-2-chloro-1-(3-nitropropyl)benzene , wherein , in powder X-ray diffraction using CuKα radiation with 2θ representing a diffraction angle , a powder X-ray diffraction image including the following 2θ peaks is observed: 2θ: 9.7 , 12.9 , 16.4 , 16.8 , 17.6 , 19.5 , 21.7 , 22.6 , 22.9 , 23.3 , 24.5 , 24.8 , 26.0 , 26.4 , 27.2.2. A crystal of 4-(3-benzyloxyphenylthio)-2-chloro-1-(3-nitropropyl)benzene , wherein a powder X-ray diffraction image substantially the same as an image in is obtained by powder X-ray diffraction using CuKα radiation with 2θ representing a diffraction angle.3. The crystal of 4-(3-benzyloxyphenylthio)-2-chloro-1-(3-nitropropyl)benzene according to claim 1 , wherein a melting point of the crystal measured by a hot plate method is 46° C. to 49° C.4. The crystal of 4-(3-benzyloxyphenylthio)-2-chloro-1-(3-nitropropyl)benzene according to claim 1 , wherein claim 1 , in thermogravimetric/differential thermal analysis (TG/DTA) of the crystal claim 1 , no reduction in weight is observed until 49° C. claim 1 , and a single endothermic peak is observed at around 50° C.5. A production method of the crystal according to claim 1 , the method including the step of mixing 4-(3-benzyloxyphenylthio)-2-chloro-1-(3-nitropropyl)benzene with an alcohol.6. The production method of the crystal according to claim 5 , wherein the 4-(3-benzyloxyphenylthio)-2-chloro-1-(3-nitropropyl)benzene is dissolved in a soluble solvent that can dissolve the compound to obtain a solution claim 5 , and the obtained solution of the 4-(3-benzyloxyphenylthio)-2-chloro-1-(3- ...

METHODS FOR REDUCING TRIGLYCERIDE, TOTAL CHOLESTEROL AND LOW DENSITY LIPOPROTEIN BLOOD LEVELS

A compound of Formula (I): 4. The method of claim 1 , in which the subject is diagnosed with hypertriglyceridemia.5. The method of claim 1 , in which the compound is administered orally.6. The method of claim 1 , in which the compound is administered once daily claim 1 , twice daily claim 1 , or thrice daily.7. The method of claim 1 , in which the compound is administered as a liquid or solid dosage form.8. The method of claim 2 , in which the compound is administered orally in a solid dosage form and is present in an orthorhombic crystalline form.9. The method of claim 1 , in which the compound is administered in an amount ranging from 50 mg/day to 5 claim 1 ,000 mg/day claim 1 , optionally divided into one claim 1 , two claim 1 , or three portions.10. The method of claim 1 , in which the compound is administered at a dosage of 50 mg claim 1 , 75 mg claim 1 , 100 mg claim 1 , 200 mg claim 1 , 500 mg claim 1 , 750 mg claim 1 , or 1 claim 1 ,000 mg once a day claim 1 , twice a day claim 1 , or three times a day.14. The method of claim 11 , in which the subject is diagnosed with hypercholesterolemia.15. The method of claim 11 , in which the compound is administered orally.16. The method of claim 11 , in which the compound is administered once daily claim 11 , twice daily claim 11 , or thrice daily.17. The method of claim 11 , in which the compound is administered as a liquid or solid dosage form.18. The method of claim 12 , in which the compound is administered orally in a solid dosage form and is present in an orthorhombic crystalline form.19. The method of claim 11 , in which the compound is administered in an amount ranging from 50 mg/day to 5 claim 11 ,000 mg/day claim 11 , optionally divided into one claim 11 , two claim 11 , or three portions.20. The method of claim 11 , in which the compound is administered at a dosage of 50 mg claim 11 , 75 mg claim 11 , 100 mg claim 11 , 200 mg claim 11 , 500 mg claim 11 , 750 mg claim 11 , or 1 claim 11 ,000 mg once a day ...

SUBSTITUTED AMINO-THIOL AND AMINO-DISULFIDE COMPOUNDS, AND USES THEREOF

The disclosure provides for new substituted cysteamine and cystamine compounds, pharmaceutical compositions made thereof, and methods thereof including the treatment of any disease or disorder in a subject that can benefit from one or more of the bioprotective effects of the compounds, including but not limited to, binding of cystine, reducing oxidative stress, increasing adiponectin levels and/or increasing brain-derived neurotrophic factors. Examples of such disease and disorders, include but are not limited to, cystinosis, and fatty liver diseases.

2-MERCAPTO-5-METHYL-4-HEPTANONE AND ITS USE IN FLAVOR AND FRAGRANCE COMPOSITIONS

The present invention is directed to a novel compound, 2-mercapto-5-methyl-4-heptanone, a process of augmenting, enhancing or imparting taste to a material selected from the group consisting of a foodstuff, a chewing gum, a medicinal product, and toothpaste comprising the step of incorporating an olfactory acceptable amount of 2-mercapto-5-methyl-4-heptanone, and a process of improving, enhancing or modifying a fragrance formulation through the addition of an olfactory acceptable amount of 2-mercapto-5-methyl-4-heptanone. 1. A compound , 2-mercapto-5-methyl-4-heptanone.2. A composition comprising an olfactory effective amount of 2-mercapto-5-methyl-4-heptanone.3. The composition of further comprising a material selected from the group consisting of foodstuff claim 2 , a chewing gum claim 2 , a dental or oral hygiene product claim 2 , and a medicinal product.4. The composition of claim 2 , wherein the olfactory effective amount is greater than about 0.5 parts per billion by weight.5. The composition of claim 2 , wherein the olfactory effective amount is from about 1 part per billion to about 1 part per million by weight.6. The composition of claim 2 , wherein the olfactory effective amount is from about 5 parts per billion to about 500 parts per billion by weight.7. A process of augmenting claim 2 , enhancing or imparting a taste to a material selected from the group consisting of foodstuff claim 2 , a chewing gum claim 2 , a dental or oral hygiene product claim 2 , and a medicinal product comprising the step of incorporating a composition comprising an olfactory effective amount of 2-mercapto-5-methyl-4-heptanone.8. The process of claim 7 , wherein the olfactory effective amount is greater than about 0.5 parts per billion by weight.9. The process of claim 7 , wherein the olfactory effective amount is from about 1 part per billion to about 1 part per million by weight.10. The process of claim 7 , wherein the olfactory effective amount is from about 5 parts per ...

Polymerizable compound and liquid crystal composition

A compound represented by formula (i) has, as Ki1 in the formula (i), a structure represented by any one of formula (K-1) to formula (K-3). When used in a liquid crystal composition, it adheres to substrates which hold the liquid crystal composition (liquid crystal layer) therebetween, thereby permitting liquid crystal molecules to be maintained in the state of being aligned in the vertical direction. The liquid crystal composition using the compound enables liquid crystal molecules to be aligned even when the PI layer is not provided (vertical alignment of liquid crystal molecules is induced without the voltage applied and horizontal alignment of liquid crystal molecules is realized with the voltage applied). It is possible to provide a polymerizable compound being excellent in storability and capable of uniform vertical alignment of liquid crystal molecules with no PI layer provided.

LIGAND AND METHOD OF MANUFACTURING THE SAME, QUANTUM DOT FILM AND METHOD OF MANUFACTURING THE SAME, AND DISPLAY APPARATUS

A ligand includes a molecular skeleton, a first coordinating group connected to the molecular skeleton, at least one initial group connected to the molecular skeleton, and a protecting group connected to an end of each initial group away from the molecular skeleton. Each initial group is capable of forming a second coordinating group after deprotection. 1. A ligand , comprising:a molecular skeleton;a first coordinating group connected to the molecular skeleton;at least one initial group connected to the molecular skeleton; anda protecting group connected to an end of each initial group away from the molecular skeleton; whereineach initial group is capable of forming a second coordinating group after deprotection.2. The ligand according to claim 1 , wherein for a same central atom claim 1 , a coordination capability of the second coordinating group to the central atom is stronger than a coordination capability of the first coordinating group to the central atom.3. The ligand according to claim 1 , whereinthe first coordinating group includes one of an amino group, an imino group, a carboxyl group, or a sulfhydryl group;or,the second coordinating group formed after each initial group is deprotected includes one of an amino group, an imino group, a carboxyl group, or a sulfhydryl group;or,the first coordinating group includes one of an amino group, an imino group, a carboxyl group or a sulfhydryl group, and the second coordinating group formed after each initial group is deprotected includes one of an amino group, an imino group, a carboxyl group, or a sulfhydryl group.4. The ligand according to claim 1 , wherein a decomposable bond formed between each initial group and the protecting group includes a photolytic chemical bond or a pyrolytic chemical bond; whereinthe photolytic chemical bond is capable of being broken under ultraviolet (UV) light irradiation; andthe pyrolytic chemical bond is capable of being broken by heating.5. The ligand according to claim 4 , ...

Use of Cysteamine in Treating Infections caused by Yeasts/Moulds

The present invention relates to compositions comprising cysteamine or a derivative thereof for use in treating infections caused by yeasts or moulds. 1. A composition comprising cysteamine or a derivative thereof for use in the treatment or prevention of an infection caused by yeasts and/or moulds.2CandidaC. albicansAspergillusEpidermophytonExophialaMicrosporumTrichophytonT. rubrumT. interdigitaleTineaBlastomycesBlastoschizomycesCoccidioidesCryptococcusCryptococcus neoformansHistoplasmaParacoccidiomycesSporotrixAbsidiaCladophialophoraFonsecaeaPhialophoraLacaziaArthrographisAcremoniumActinomaduraApophysomycesEmmonsiaBasidiobolusBeauveriaChrysosporiumConidiobolusCunninghamellaFusariumGeotrichumGraphiumLeptosphaeriaMalasseziaMalassezia furfurMucorNeotestudinaNocardiaNocardiopsisPaecilomycesPhomaPiedraiaPneumocystisPseudallescheriaPyrenochaetaRhizomucorRhizopusRhodotorulaSaccharomycesScedosporiumScopulariopsisSporobolomycesSyncephalastrumTrichodermaTrichosporonUlocladiumUstilagoVerticilliumWangiella. A composition according to wherein the infection is caused by one or more of the group consisting of: spp. claim 1 , (e.g. ) claim 1 , spp. claim 1 , spp. claim 1 , spp. claim 1 , spp. claim 1 , spp. claim 1 , (e.g and ) claim 1 , spp. claim 1 , spp. claim 1 , spp. claim 1 , spp. claim 1 , spp. (e.g. ) claim 1 , spp. claim 1 , spp. claim 1 , spp. claim 1 , spp. claim 1 , spp. claim 1 , spp. claim 1 , spp. claim 1 , spp. claim 1 , spp. claim 1 , spp. claim 1 , spp. claim 1 , spp. claim 1 , spp. claim 1 , spp. claim 1 , spp. claim 1 , spp. claim 1 , spp. claim 1 , spp. claim 1 , spp. claim 1 , spp. claim 1 , spp. claim 1 , spp. claim 1 , spp. (e.g ) claim 1 , spp. claim 1 , spp. claim 1 , spp. claim 1 , spp. claim 1 , spp. claim 1 , spp. claim 1 , spp. claim 1 , spp. claim 1 , spp. claim 1 , spp. claim 1 , spp. claim 1 , spp. claim 1 , spp. claim 1 , spp. claim 1 , spp. claim 1 , spp. claim 1 , spp. claim 1 , spp. claim 1 , spp. claim 1 , spp. claim 1 , spp. claim 1 , spp. c ...

IONIZABLE CATIONIC LIPID FOR RNA DELIVERY

What is described is a compound of formula I 2. The compound of claim 1 , wherein X is —CO—O—.3. The compound of claim 1 , wherein X is —O—CO—.4. The compound of claim 1 , wherein Y is S.5. The compound of claim 1 , wherein Y is O.6. The compound of claim 1 , wherein n is 1.7. The compound of claim 1 , wherein R is an alkenyl.8. The compound of claim 1 , wherein L is an alkylene.9. The compound of claim 1 , wherein L is an alkenylene.10. The compound of claim 1 , wherein L and R together have 14 to 20 carbons.11. The compound of claim 1 , wherein L and R together have 16 carbons.12. The compound of claim 1 , wherein Ris a C2 or a C3.13. The compound of claim 1 , wherein Rand Rtogether have 2 to 4 carbons.15. A composition of the compound of claim 1 , further comprising a lipid particle.16. A composition of the compound of claim 1 , further comprising an RNA claim 1 , wherein the RNA is encapsulated.17. A composition of the compound of claim 1 , further comprising a lipid conjugate.18. A composition of the compound of claim 1 , further comprising a non-cationic lipid. This application a divisional of U.S. patent application Ser. No. 14/707,796, filed May 8, 2015, which is a continuation-in-part and claims benefit under 35 U.S.C. §120 to U.S. patent application Ser. No. 14/546,105 filed on Nov. 18, 2014, which claims benefit under 35 U.S.C. §119(e) of Provisional U.S. Patent Application No. 61/905,724, filed Nov. 18, 2013, the contents of which are incorporated herein by reference in its entirety.The description of U.S. patent application Ser. No. 14/707,876, entitled “IONIZABLE CATIONIC LIPID FOR RNA DELIVERY,” filed May 8, 2015, now U.S. Pat. No. 9,365,610, issued Jun. 14, 2016, is hereby incorporated by reference in its entirety.A number of different types of nucleic acids are currently being developed as therapeutics for the treatment of a number of diseases. These nucleic acids include DNA in gene therapy, plasmids-based interfering nucleic acids, small ...

CONTACT-KILLING, QAC FUNCTIONALIZED THERMOPLASTIC POLYURETHANE FOR CATHETER APPLICATIONS

In various embodiments, the present invention provides a functionalized thermoplastic polyurethane (TPU) containing bulk incorporated or surface-grafted quaternary ammonium compounds (QAC)s for contact-killing of a variety of microbes, where the QACs are on the surface of TPU to provide a sterile surface material that prevents bacteria commonly involved in device-associated infections (DAIs) from proliferating. The functionalized TPUs of the present invention can be formed into a wide variety of 3-dimensional shapes, such as catheters, medical tubing, laryngeal or tracheal stents, sutures, prosthetics, wound dressings, and/or a coating for medical devices and contains the residue of either a QAC containing diol monomer or an alkene functional diol monomer, which then allows the TPU to be functionalized with a QAC containing disulfide or free thiol compound, to form a quaternary ammonium functionalized thermoplastic polyurethane compound having antimicrobial properties for use in medical devices. 1) A quaternary ammonium functionalized thermoplastic polyurethane compound having antimicrobial properties for use in medical devices comprising:a polyurethane polymer backbone;a plurality of side chains, said side chains extending from said polyurethane polymer backbone and comprising a quaternary ammonium functional group.2) The quaternary ammonium functionalized thermoplastic polyurethane compound of wherein:said polyurethane polymer backbone comprises the residues of one or more diisocyanates, one or more soft segment diols, one or more functionalized diols, and one or more diol chain extenders; andsaid plurality of side chains comprise a quaternary ammonium functional group connected to said polyurethane polymer backbone through said one or more functionalized diols.3) The quaternary ammonium functionalized thermoplastic polyurethane compound of wherein the residues of one or more functionalized diols comprises from 0.5 to 50 mole percent of said polyurethane polymer ...

BIODEGRADABLE COMPUTED TOMOGRAPHY CONTRAST AGENTS

Biodegradable computed tomography (CT) contrast agents comprising a polyiodinated aryl contrast agent that is crosslinked by an organic disulfide are described herein. The contrast agents can be used to image a tissue region by administering an effective amount of the biodegradable CT contrast agent to a subject, allowing a sufficient amount of time for the biodegradable CT contrast agent to enter the tissue region, and performing x-ray computed tomography imaging of the tissue region of the subject. 1. A biodegradable macromolecular computed tomography (CT) contrast agent comprising a polyiodinated aryl contrast agent crosslinked by an organic disulfide.4. The biodegradable macromolecular CT contrast agent of claim 1 , wherein the polyiodinated aryl contrast agent is PEGylated.5. The biodegradable macromolecular CT contrast agent of claim 1 , wherein the polyiodinated aryl contrast agent is 5-amino-2 claim 1 ,4 claim 1 ,6-triiodoisophthalic acid (ATIPA).6. The biodegradable macromolecular CT contrast agent of claim 1 , wherein the organic disulfide is cystamine.8. The biodegradable macromolecular CT contrast agent of claim 1 , wherein the organic disulfide is cystine.10. A method for imaging a tissue region of a subject comprising:(a) administering an effective amount of a biodegradable macromolecular computed tomography (CT) contrast agent comprising a polyiodinated aryl contrast agent that is crosslinked by an organic disulfide to the subject;(b) allowing a sufficient amount of time for the macromolecular biodegradable CT contrast agent to enter the tissue region; and(c) performing x-ray computed tomography imaging of the tissue region of the subject.13. The method of claim 10 , wherein the polyiodinated aryl contrast agent is 5-amino-2 claim 10 ,4 claim 10 ,6-triiodoisophthalic acid (ATIPA).16. The method of claim 10 , wherein the tissue region is a blood vessel.17. The method of claim 10 , wherein the tissue region is a tumor.18. A method of making a ...

TETRADENTATE ORGANIC LIGAND H3-MN-16Bn CONTAINING LONG ALKYL GROUP, PRECURSOR THEREOF, AND METHOD FOR PREPARING THE SAME

A tetradentate organic ligand H-MN-16Bn containing a long alkyl group, a precursor thereof, and a method for preparing the same are revealed. A precursor of H-MN-16Bn, benzyl 16-bromohexadecanate, is obtained by esterification reaction of 16-bromohexadecanoic acid. Then bimolecular nucleophilic substitution reaction (S2) of Benzyl 16-bromohexadecanate with nitrogen sulfide (NS) is carried out to get H-MN-16Bn that is used as a standard hydrolysis metabolites of non-radioactive Re-complex compound. 2. A method for preparing a tetradentate organic ligand H-MN-16Bn containing a long alkyl group comprising the steps of:dissolving 16-bromohexadecanoic acid and thionyl chloride in a first solvent to get a first solution;heating the first solution under reflux;cooling the first solution, and concentrating the first solution by removing excess thionyl chloride and excess first solution to form a second solution;adding phenylmethanol into the second solution to form benzyl 16-bromohexadecanate in a solid form;{'sub': 2', '2, 'mixing the benzyl 16-bromohexadecanate, nitrogen sulfide (NS), a dehydrogenating agent, a molecular sieve and a second solvent to form a third solution;'}heating the third solution under reflux; and{'sub': '3', 'filtering the third solution to get a crude product and then purifying the crude product to get the tetradentate organic ligand H-MN-16Bn containing a long alkyl group.'}3. The method as claimed in claim 2 , wherein the first solvent is hexane.4. The method as claimed in claim 2 , wherein the second solvent is acetonitrile.5. The method as claimed in claim 2 , wherein the first solution is heated under reflux at 75˜85° C. for 2 hours in the step of heating the first solution under reflux.6. The method as claimed in claim 2 , wherein the first third solution is heated under reflux at 80˜90° C. for 48 hours in the step of heating the third solution under reflux.7. The method as claimed in claim 2 , wherein the dehydrogenating agent is potassium ...

IONIZABLE CATIONIC LIPID FOR RNA DELIVERY

What is described is a compound of formula III or IV 2. The compound of claim 1 , wherein X is S.3. The compound of claim 1 , wherein Ris ethylene.4. The compound of claim 1 , wherein Ris n-propylene or isopropylene.5. The compound of claim 1 , wherein Rand Reach is methyl claim 1 , ethyl claim 1 , or isopropyl.6. The compound of claim 1 , wherein Land Leach is a bond.7. The compound of claim 1 , wherein Land Leach is a methylene.8. The compound of claim 1 , wherein Rand Reach is a branched alkyl.9. The compound of claim 1 , wherein Ris an alkyl.10. The compound of claim 1 , wherein Rand Reach is a branched alkyl of 19 or 20 carbon atoms.11. The compound of claim 1 , wherein Ror Reach is a branched alkyl of 13 or 14 carbon atoms.12. The compound of claim 1 , wherein Ris ethylene claim 1 , X is S claim 1 , and Rand Reach is a methyl.13. The compound of claim 1 , wherein Ris n-propylene claim 1 , X is S claim 1 , and Rand Reach is a methyl.14. The compound of claim 1 , wherein Ris isopropylene claim 1 , X is S claim 1 , and Rand Reach is a methyl.17. The compound of claim 16 , wherein X is S.18. The compound of claim 16 , wherein Ris ethylene claim 16 , n-propylene claim 16 , or isopropylene.19. The compound of claim 16 , wherein Rand Reach is methyl claim 16 , ethyl claim 16 , or isopropyl.20. The compound of claim 16 , wherein L is a bond.21. The compound of claim 16 , wherein L is a methylene.22. The compound of claim 16 , wherein R is a branched alkyl of 19 or 20 carbons.23. The compound of claim 16 , wherein R is a branched alkyl of 13 or 14 carbons. This application a divisional of U.S. patent application Ser. No. 14/707,796, filed May 8, 2015, which is a continuation-in-part and claims benefit to U.S. patent application Ser. No. 14/546,105 filed on Nov. 18, 2014, which claims benefit of Provisional U.S. Patent Application No. 61/905,724, filed Nov. 18, 2013, the contents of which are incorporated herein by reference in its entirety.The description of U.S. ...

SULFIDE-BASED COMPOUNDS AND USES THEREOF

Disclosed are sulfide-based compounds which are a product of a Michael addition reaction between a sulfur-containing donor group and an unsaturated hydrocarbon moiety. The sulfide-based compounds may be used in compositions and methods for inhibiting corrosion. 1. A composition comprising at least one sulfide-based compound , the at least one sulfide-based compound formed by a Michael addition reaction between a sulfa-Michael donor and an olefin as a Michael acceptor.2. The composition of of claim 1 , wherein the sulfa-Michael donor comprises a mercaptoalcohol.3. The composition of claim 1 , wherein the olefin comprises α claim 1 ,β-unsaturated carbonyl compounds.4. The composition of claim 3 , wherein the α claim 3 ,βunsaturated carbonyl compounds comprises a vinyl ketone claim 3 , a vinyl sulfone claim 3 , a quinone claim 3 , an enamine claim 3 , a ketimine claim 3 , an aldimine claim 3 , an oxazolidine claim 3 , and an acrylate claim 3 , acrylate esters claim 3 , acrylonitrile claim 3 , acrylamides claim 3 , maleimides claim 3 , alkyl methacrylates claim 3 , cyanoacrylates claim 3 , vinyl ketones claim 3 , α claim 3 ,β-unsaturated aldehydes claim 3 , vinyl phosphonates claim 3 , acrylonitrile claim 3 , vinyl pyridines claim 3 , azo compounds claim 3 , β-keto acetylenes claim 3 , acetylene esters claim 3 , nitro ethylenes.6. The composition of claim 1 , further comprising a solvent claim 1 , wherein the solvent is present in the composition at about 10 wt % to 99 wt % of the composition.7. A fluid source comprising one or more corrodents and at least one sulfide-based compound as in .8. The composition of claim 7 , wherein the fluid source comprises about 0.1% to about 25% weight/weight total dissolved solids.9. The composition of claim 1 , wherein the sulfide-based compound is about is about 0.1 ppm to 10 claim 1 ,000 ppm by weight or volume of the composition.12. A method of inhibiting corrosion of metal containments in contact with a fluid source comprising the ...

CHROMENE COMPOUND AND CURABLE COMPOSITION

A chromene compound which has a sulfur-containing substituent represented by the following formula (2) at the 6-position and/or 7-position carbon atom of an indeno (2,1-f)naphtho(1,2-b)pyran structure and is excellent in photochromic properties and stability at a high temperature. 3. The chromene compound according to claim 2 , wherein claim 2 , in the above formula (3) claim 2 , Rand Rform an aliphatic hydrocarbon ring together with the 13-position carbon atom bonded thereto claim 2 , and the aliphatic hydrocarbon ring has 3 to 20 ring member carbon atoms and may have at least one substituent selected from the group consisting of alkyl group claim 2 , haloalkyl group claim 2 , cycloalkyl group claim 2 , alkoxy group claim 2 , amino group claim 2 , aralkyl group claim 2 , aryl group and halogen atom.4. A photochromic curable composition comprising the chromene compound of and a polymerizable monomer.5. A photochromic optical article having a polymer molded product comprising the chromene compound of dispersed therein as a constituent member.6. The photochromic optical article according to which has a yellowness index change (ΔYI) after it is kept at 110° C. for 12 hours of 2 or less and does not substantially change in developed hue at the time of exposure.7. An optical article having an optical substrate all or part of at least one surface of which is covered with a polymer film comprising the chromene compound of dispersed therein as a constituent member.9. A photochromic curable composition comprising the chromene compound of and a polymerizable monomer.10. A photochromic curable composition comprising the chromene compound of and a polymerizable monomer.11. A photochromic optical article having a polymer molded product comprising the chromene compound of dispersed therein as a constituent member.12. A photochromic optical article having a polymer molded product comprising the chromene compound of dispersed therein as a constituent member.13. An optical article ...

ACTIVE INGREDIENTS WHICH IMPROVE PRIMARY DETERGENT POWER

The aim of the invention is to improve the primary detergent power of washing and cleaning agents, in particular with respect to bleach-sensitive or enzyme-sensitive soiling. This is substantially achieved by the incorporation of alkoxy group-carrying sulfocalixarenes or carboxycalixarenes. 2. The agent according to claim 1 , wherein it contains the compound of the general formula (I) in amounts of 0.1% by weight to 10% by weight.3. The agent according to claim 1 , wherein in the compound of general formula (I) n denotes a number from 3 to 7.4. The agent according to claim 1 , wherein in the compound of general formula (I) R denotes hydrogen or an alkyl group having 6 to 12 C atoms.5. The agent according to claim 1 , wherein in the compound of general formula (I) all substituents X are not hydrogen.7. The method according to claim 6 , wherein the compound of general formula (I) is added to a liquor containing washing or cleaning agent or is introduced into the liquor as a constituent of a washing or cleaning agent.8. The method according to claim 6 , wherein the concentration of the compound of general formula (I) in liquor containing the agent is in the range from 0.1 mmol/l to 2.5 mmol/l.9. The method according to claim 6 , wherein it is carried out by means of a domestic washing machine or dishwasher. The present invention generally relates to the use of certain macrocyclic oligomers of the calixarene type to enhance the primary detergent power of washing or cleaning agents when washing textiles or cleaning hard surfaces with respect to in particular bleach-sensitive or enzyme-sensitive soiling, and to washing and cleaning agents which contain such macrocyclic oligomers.Besides the ingredients essential for the washing process, such as surfactants and builder materials, washing agents usually contain further constituents which can be collectively referred to as washing auxiliaries and which include such diverse groups of active substances as foam regulators, anti ...

Compounds and Methods for Use in Detecting Gabapentin

Compounds and methods for use in detecting gabapentin in a sample suspected of containing gabapentin are disclosed. Gabapentin derivatives are used to produce gabapentin conjugates. A gabapentin-immunogenic carrier conjugate may be used as an immunogen for the preparation of an anti-gabapentin antibody. A gabapentin-detectable label may be used in a signal producing system in gabapentin assays. 2. The compound of claim 1 , wherein said linker comprises 0 to 40 carbon atoms and 0-6 heteroatoms.3. The compound of claim 2 , wherein W is a lower alkyl and said linker is selected from the group consisting of:{'sub': 2', 'n, '—(CH)C(O)—;'}{'sub': 2', 'n, '—C(O)(CH)—;'}{'sub': 2', 'n, '—C(O)(CH)NH—C(O)—;'}{'sub': 2', 'm', '2', 'n, '—C(O)(CH)NH—C(O)(CH)—;'}{'sub': 2', 'n', '2, '—(CH)SCHC(O)—;'}{'sub': 2', 'm', '2', '2', 'n, '—(CH)SCHC(O)(CH)—;'}{'sub': 2', 'm', '2', 'n, '—(CH)C(O)NH(CH)—;'}{'sub': 2', 'n, '—(CH)NH—C(O)—;'}{'sub': 2', 'm', '2', 'n, '—(CH)NH—C(O)(CH)—;'}{'sub': 2', 'n, '—C(O)—(CH)—; and'}{'sub': 2', 'n, '—(CH)—, and'}wherein m, n, o, and p are independently selected from an integer from 0 to 10.4. The compound of claim 2 , wherein W is a carbonyl and said linker is selected from the group consisting of:{'sub': 2', 'n, '—(CH)C(O)—;'}{'sub': 2', 'n', '2, '—(CH)SCHC(O)—;'}{'sub': 2', 'm', '2', '2', 'n, '—(CH)SCHC(O)(CH)—;'}{'sub': 2', 'm', '2', 'n, '—(CH)C(O)NH(CH)—;'}{'sub': 2', 'n, '—(CH)NH—C(O)—;'}{'sub': 2', 'm', '2', 'n, '—(CH)NH—C(O)(CH)—; and'}{'sub': 2', 'n, '—(CH)—, and'}wherein m, n, o, and p are independently selected from an integer from 0 to 10.5. The compound of claim 1 , wherein W is a lower alkyl group and the lower alkyl group is a methyl group.6. The compound of claim 1 , wherein said reactive functional group is selected from the group consisting of halogen claim 1 , OH claim 1 , SH claim 1 , NH claim 1 , O-lower alkyl claim 1 , epoxy claim 1 , S-acyl claim 1 , carboxyl claim 1 , maleimidyl claim 1 , haloacetamide claim 1 , hydroxysuccinimidyl ...

THIOL-FORMYL HEMIACETAL CORROSION INHIBITORS

The present invention generally relates to compositions and methods for inhibiting corrosion at a surface in the production, transportation, storage, and separation of crude oil and natural gas. 2. (canceled)4. An anti-corrosion composition comprising the compound of formula (I) claim 3 , (II) claim 3 , (III) or (IV) of .5. The method of claim 1 , wherein the anti-corrosion composition comprises the compound of formula (I).8. (canceled)9. The method of claim 1 , wherein Rof Formula (I) claim 1 , (IA) or (IB) is either:{'sub': 1', '24', '1', '24', '6', '12', '3', '8', '2', '2', '1', '6', '1', '6', '2', '10', '11', '2', '10', '11', '1', '6', '2', '1, 'C-Calkyl, C-Calkenyl, C-Caryl, monocyclic or bicyclic heteroaryl, or C-Ccycloalkyl, wherein said alkyl, alkenyl, aryl, heteroaryl, or cycloalkyl are each independently unsubstituted or substituted with 1 to 3 substituents independently selected from —F, —Cl, —NO, —CN, —OH, —NH, C-Chaloalkyl, C-Calkoxy, —COR, and —CON(R), wherein Rand R, at each occurrence, are each independently hydrogen or C-Calkyl; or optionally one or more of the —CH— groups of Ris replaced with a —C(O)O— group; or'}{'sub': 1', '18', '3', '8', '1', '6', '2', '10', '10', '1', '6', '2', '1, 'C-Calkyl, or C-Ccycloalkyl, wherein said alkyl, or cycloalkyl are each independently unsubstituted or substituted with 1 to 3 substituents independently selected from —OH, C-Calkoxy, or —CORwherein Rat each occurrence, is independently hydrogen or C-Calkyl; or optionally one or more of the —CH— groups of Ris replaced with a —C(O)O— group.'}10. (canceled)11. The method of claim 1 , wherein Rof Formula (I) claim 1 , (IA) or (IB) is either:{'sub': 1', '18', '3', '8, 'C-Calkyl or C-Ccycloalkyl; or'}{'sub': 1', '12', '2', '1', '1', '12', '2, 'C-Calkyl optionally substituted with 1 to 3 substituents of —OH or —COH; or Ris C-Calkyl wherein one or more of the —CH— groups is replaced with a —C(O)O— group; or'}{'sub': 1', '12', '2', '1', '1', '12', '2, 'C-Calkyl substituted ...

Dithioamine Reducing Agents

Dithioamine reducing agents useful for the reduction of disulfide bonds. The reducing agents of this invention are useful, for example, to reduce disulfide bonds, particularly in proteins, or to prevent the formation of disulfide bonds, particularly in proteins and other biological molecules. Reducing agents of this invention can be employed to regulate protein function in proteins in which a sulfhydryl group is associated with biological activity. Reducing agents of this invention can prevent inactivation of a given protein or enhance activation of a given protein or other biological molecule in vitro and/or in vivo. Reducing agents of this invention can prevent or reduce oxidation of cysteine residues in proteins and prevent the formation of reduced activity protein dimers (or other oligomers). Reducing agents of this invention are useful and suitable for application in a variety of biological applications, particularly as research and synthetic reagents. The invention provides S-acylated dithioamines which can be selectively activated reducing agents by removal of the S-acyl groups enzymatically or chemically. The invention further provides dithiane precursors of thioamino reducing agents. The invention provides dithioamine reducing agents, S-acylated dithioamines and dithianes which are immobilized on surfaces, including among others, glass, quartz, microparticles, nanoparticles and resins. 2. The compound of wherein neither Ror Ris an —NHgroup.3. The compound of wherein one of Ror Ris a —CORgroup.4. The compound of wherein R claim 3 , Rand Rare all hydrogens.5. The compound of wherein R claim 3 , R claim 3 , R claim 3 , Rand Rare all hydrogens.6. The compound of wherein both Rare hydrogens or both Rare acyl groups.7. (canceled)8. The compound of wherein Ris independently hydrogen claim 3 , a 1-12 carbon alkyl group claim 3 , an aryl group claim 3 , a heterocyclic group claim 3 , or a heteroaryl group.9. The compound of wherein R-Rare all hydrogens and each Ris ...

Styrenyl Derivative Compounds for Treating Ophthalmic Diseases and Disorders

The present invention relates generally to compositions and methods for treating neurodegenerative diseases and disorders, particularly ophthalmic diseases and disorders. Provided herein are styrenyl derivative compounds, including but not limited to stilbene derivative compounds, and compositions comprising these compounds, that are useful for treating and preventing ophthalmic diseases and disorders, including age-related macular degeneration (AMD) and Stargardt's Disease. 184.-. (canceled)86. The compound of claim 85 , or the pharmaceutically acceptable salt thereof claim 85 , wherein Ris cyclohexyl.87. The compound of claim 85 , or the pharmaceutically acceptable salt thereof claim 85 , wherein R claim 85 , R claim 85 , Rand Rare each independently hydrogen claim 85 , halogen claim 85 , alkyl claim 85 , fluoroalkyl claim 85 , —OR claim 85 , or —NRR claim 85 , wherein each Ris independently hydrogen or alkyl.88. The compound of claim 85 , or the pharmaceutically acceptable salt thereof claim 85 , wherein R claim 85 , R claim 85 , Rand Rare each the same or different and independently hydrogen claim 85 , halogen claim 85 , —OR claim 85 , or alkyl.89. The compound of claim 85 , or the pharmaceutically acceptable salt thereof claim 85 , selected from:(E)-3-(3-(2-cyclohexylvinyl)phenyl)propan-1-amine;(E)-1-(3-(3-amino-1-hydroxypropyl)styryl)cyclohexanol;(E)-1-(3-((1R,2R)-3-amino-1-hydroxy-2-methylpropyl)styryl)cyclohexanol;(E)-1-(3-(3-amino-1-hydroxypropyl)-5-fluoro styryl)cyclohexanol;(E)-1-(3-(3-amino-1-hydroxypropyl)-2-fluoro styryl)cyclohexanol;(1S,2S)-3-amino-1-(3-((E)-2-(1-hydroxycyclohexyl)vinyl)phenyl)propane-1,2-diol;(1R,2R)-3-amino-1-(3-((E)-2-(1-hydroxycyclohexyl)vinyl)phenyl)propane-1,2-diol;(E)-1-(5-(3-amino-1-hydroxypropyl)-2-methoxystyryl)cyclohexanol;(E)-1-(3-(3-amino-1-hydroxypropyl)-4-chloro styryl)cyclohexanol;(E)-1-(3-(3-amino-1-hydroxypropyl)-4-methylstyryl)cyclohexanol;(E)-1-(3-(3-amino-1-hydroxypropyl)-5-methylstyryl)cyclohexanol;(1S,2R)-3- ...

GLYCOSIDE COMPOUND, METHOD FOR PRODUCING THIOETHER, ETHER, METHOD FOR PRODUCING ETHER, METHOD FOR PRODUCING GLYCOSIDE COMPOUND, METHOD FOR PRODUCING NUCLEIC ACID

The invention provides a glucoside compound, which is capable of providing a phosphoramidite, which can be produced at low cost and can produce a nucleic acid in high yield and with high purity. The glycoside compound has the formula 2. The production method according to claim 1 , wherein claim 1 , in the aforementioned chemical formulas (101a) claim 1 , (101b) and (103) claim 1 , Rand Rare each a methyl group.4. The production method according to claim 3 , wherein claim 3 , in the aforementioned chemical formulas (103b) claim 3 , (104) and (103) claim 3 , R claim 3 , Rand Rare each a methyl group.5. The production method according to claim 3 , wherein the aforementioned halogenating agent is at least one selected from the group consisting of N-chlorosuccinimide claim 3 , N-bromosuccinimide claim 3 , N-iodosuccinimide claim 3 , iodine claim 3 , bromine and chlorine.6. The production method according to claim 3 , wherein the aforementioned Lewis acid is at least one selected from the group consisting of perfluoroalkylcarboxylic acid claim 3 , perfluoroalkylsulfonic acid claim 3 , alkylsulfonic acid and a salt thereof.7. The production method according to claim 3 , wherein the aforementioned Lewis acid is a silver salt of trifluoromethanesulfonic acid.8. The production method according to claim 3 , wherein the aforementioned coupling reaction is performed in the co-presence of molecular sieve.11. The production method according to claim 10 , wherein the aforementioned halogenating agent is at least one selected from the group consisting of N-chlorosuccinimide claim 10 , N-bromosuccinimide claim 10 , N-iodosuccinimide claim 10 , iodine claim 10 , bromine and chlorine.12. The production method according to claim 10 , wherein the aforementioned Lewis acid is at least one selected from the group consisting of perfluoroalkylcarboxylic acid claim 10 , perfluoroalkylsulfonic acid claim 10 , alkylsulfonic acid and a salt thereof.13. The production method according to claim 10 ...

IONIZABLE CATIONIC LIPID FOR RNA DELIVERY

What is described is a compound of formula I 2. The compound of claim 1 , wherein Ris a linear alkyl claim 1 , alkenyl claim 1 , or alkynyl.3. The compound of claim 1 , wherein Ris a linear alkyl.4. The compound of claim 1 , wherein Ris a branched alkyl claim 1 , consisting of a linear alkyl of 1-18 carbons and a single alkyl substituent.5. The compound of claim 1 , wherein Rconsisting of a linear alkyl of 1-18 carbons and a single alkyl substituent.6. The compound of claim 1 , wherein Land Lare the same.7. The compound of claim 6 , wherein Land Lare linear alkylenes.8. The compound of claim 1 , wherein Lor Lor both is an alkenylene.9. The compound of claim 1 , wherein Rand Rare the same or different claim 1 , each a methyl claim 1 , ethyl claim 1 , n-propyl claim 1 , isopropyl claim 1 , n-butyl claim 1 , t-butyl claim 1 , n-pentyl claim 1 , or hexyl.10. The compound of claim 1 , wherein Rand Rare the same or different claim 1 , each a methyl claim 1 , ethyl claim 1 , n-propyl claim 1 , or isopropyl.11. The compound of claim 1 , wherein Lis a bond.12. The compound of claim 1 , wherein X is S.13. A lipid particle comprising the compound of .14. The lipid particle of claim 13 , wherein the lipid particle is a nucleic-acid lipid particle.15. The lipid particle of claim 13 , further comprising a bilayer of lipid molecules.16. The lipid particle of claim 15 , further comprising a lipid encapsulated nucleic acid.17. The lipid particle of claim 16 , wherein the nucleic acid is RNA.18. The lipid particle of claim 13 , further comprising a lipid conjugate.19. The lipid particle of claim 13 , further comprising a phospholipid.20. The lipid particle of claim 13 , further comprising a neutral lipid. This application is a continuation of U.S. patent application Ser. No. 15/614,499, filed Jun. 5, 2017, now U.S. Pat. No. 9,896,413, issued Feb. 20, 2018, which is a continuation of U.S. patent application Ser. No. 15/347,647, filed Nov. 9, 2016, now U.S. Pat. No. 9,670,152, granted ...

Vitamin Cationic Lipids

Disclosed are cationic lipids comprising a vitamin substructure and an ionizable nitrogen-containing group. Cationic lipids provided herein can be useful for delivery and expression of mRNA and encoded protein, e.g., as a component of liposomal delivery vehicle, and accordingly can be useful for treating various diseases, disorders and conditions, such as those associated with deficiency of one or more proteins. 1. A liposome encapsulating an mRNA encoding a peptide or polypeptide , wherein the liposome comprisesone or more cationic lipids, andoptionally one or more non-cationic lipids, optionally one or more cholesterol-based lipids and optionally one or more PEG-modified lipids; and{'sup': 1', '1, 'wherein the liposome comprises at least one cationic lipid that comprises the structure of Vitamin A, D, E, or K, and also comprises a moiety X, wherein Xis an ionizable nitrogen-containing group.'}13. The liposome of any one of - , wherein Xis O.14. The liposome of any one of - , wherein Ris C-C-alkylene.15. The liposome of any one of - , wherein Ris C-C-alkylene.16. The liposome of claim 14 , wherein Ris unsubstituted C-C-alkylene.17. The liposome of claim 15 , wherein Ris unsubstituted C-C-alkylene.18. The liposome of any one of - claim 15 , wherein Ris —CH— claim 15 , —CH— claim 15 , —CH— claim 15 , —CH— claim 15 , —CH— claim 15 , —CH— claim 15 , —CH— claim 15 , —CH— claim 15 , —CH— claim 15 , —CH— claim 15 , —CH— claim 15 , —CH— claim 15 , —CH— claim 15 , —CH— claim 15 , —CH— claim 15 , —CH— claim 15 , —CH— claim 15 , —CH— claim 15 , —CH— claim 15 , or —CH—.19. The liposome of any one of - claim 15 , wherein Ris —CH— claim 15 , —CH— claim 15 , or CH—.20. The liposome of claim 14 , wherein Ris substituted C-C-alkylene with one or substituents selected from halogen claim 14 , hydroxyl claim 14 , amino claim 14 , thiol claim 14 , ester claim 14 , and thioester.21. The liposome of any one of - claim 14 , wherein Ris C-C-alkenylene or C-C-alkenylene.22. The liposome of ...

Multicomponent Degradable Cationic Polymers

Degradable polymers were synthesized that self-assemble with DNA to form particles that are effective for gene delivery. Small changes to polymer synthesis conditions, particle formulation conditions, and polymer structure provides significant changes to efficacy in a cell-type dependent manner. Polymers presented here are more effective than commercially available materials, such as LIPOFECTAMINE 2000™, FUGENE®, or polyethylenimine (PEI), for gene delivery to cancerous fibroblasts or human primary fibroblasts. The presently disclosed materials may be useful for cancer therapeutics and regenerative medicine. 157-. (canceled)60. The polymer or particle of claim 58 , wherein R forms a butyl diester group.61. The polymer or particle of claim 58 , wherein side chain R′ forms a butyl alcohol.62. The polymer or particle of claim 58 , wherein end group R″ comprises a heterocyclic group selected from pyrrolidinyl claim 58 , pyrrolinyl claim 58 , imidazolidinyl claim 58 , imidazolinyl claim 58 , indolinyl claim 58 , quinuclidinyl claim 58 , morpholinyl claim 58 , thiomorpholinyl claim 58 , thiadiazinanyl claim 58 , and tetrahydrofuranyl.63. The polymer or particle of claim 58 , wherein acrylate-terminated polymer is first synthesized by reaction of the diacrylate backbone and amine side chain at a molar ratio of 1:1.1 to 1.2:1; followed by end-capping with amine-containing end groups.64. The polymer or particle of claim 58 , wherein n is an integer of from 1 to 1000.65. The polymer or particle of claim 58 , wherein n is an integer of from 1 to 100.66. The polymer or particle of claim 58 , wherein n is an integer of from 5 to 20.67. The polymer or particle of claim 58 , wherein the polymer has a molecular weight of from 5 to 10 kDa.68. The polymer or particle of claim 58 , wherein the polymer has a molecular weight of from 10 to 15 kDa.69. The polymer or particle of claim 58 , wherein the polymer has a molecular weight of from 15 to 25 kDa.70. The polymer or particle of claim ...

Storage of 3-methylthiopropionaldehyde and methyl mercaptan

A compound, which is 1-(1,3-bis(methylthio)propoxy)-3-(methylthio)propan-1-ol, a composition containing the compound, a method for the preparation thereof, a method for preparing 3-methylthiopropionaldehyde by reacting 1-(1,3-bis(methylthio)propoxy)-3-(methylthio)propan-1-ol with acrolein, and also to the use of 1-(1,3-bis(methylthio)propoxy)-3-(methylthio)propan-1-ol or compositions containing the compound for the storage and/or transport of 3-methylthiopropionaldehyde and/or methyl mercaptan.

Process for preparation of cysteamine bitartrate

The present invention provides process for preparation of cysteamine bitartrate comprising reacting cysteamine or its salt with tartaric acid. The present invention further provides crystalline form L1 of cysteamine bitartrate having characteristic diffraction peaks at 10.36, 14.54, 17.23, 18.03, 19.24, 20.76, 21.20, 22.02, 23.37, 23.64, 27.71, 28.28, 29.26, 31.33, 32.84, 33.83, 35.51, 36.74±0.2 degree two theta in an X-ray diffraction pattern and process for preparation thereof. The present invention provides crystalline form L2 of cysteamine bitartrate having characteristic diffraction peaks at 7.4, 10.3, 11.0, 11.4, 14.4, 14.9, 18.6, 19.4, 20.1, 20.8, 21.9, 22.3, 22.5, 23.5±0.2 degree two theta in an X-ray diffraction pattern and process for preparation thereof.

Method for preparing an aromatic sulfide or salt thereof

A method for preparing an aromatic sulfide or a salt thereof is provided. The method for preparing an aromatic sulfide or a salt thereof includes reacting a compound having a structure represented by Formula (I) to a compound having a structure represented by Formula (III) in the presence of a compound having a structure represented by Formula (II) to obtain a compound having a structure represented by Formula (IV) wherein R 1 and R 2 are independently C 1-6 alkyl group, or C 5-7 cycloalkyl group; R 3 is independently C 1-6 alkyl group, C 5-7 cycloalkyl group, C 1-6 haloalkyl group, or aryl group; R 4 is independently H, or C 1-6 alkyl group; Y is H, aryl group, or —X—R 5 ; X is —O—, —NH—, —PH—, or —S—, or Y and an adjacent R 4 are optionally combined with the carbon atoms to which they are attached, to form an aryl group; and R 5 is H, C 1-6 alkyl group, C 5-7 cycloalkyl group, or aryl group; and Z − is R 3 SO 3 − .

CLEAVABLE LIPIDS

Disclosed herein are novel compounds, pharmaceutical compositions comprising such compounds and related methods of their use. The compounds described herein are useful, e.g., as liposomal delivery vehicles to facilitate the delivery of encapsulated polynucleotides to target cells and subsequent transfection of said target cells, and in certain embodiments are characterized as having one or more properties that afford such compounds advantages relative to other similarly classified lipids. 268-. (canceled)70. The compound of claim 69 , wherein Ris imidazole.72. The compound of claim 69 , wherein Ris guanidinium.75. The compound of claim 74 , wherein Rand Rare each an optionally substituted claim 74 , variably saturated or unsaturated C-Calkyl.76. The compound of claim 74 , wherein Rand Rare each an optionally substituted claim 74 , polyunsaturated C-Calkyl.77. The compound of claim 74 , wherein Rand Rare each an optionally substituted claim 74 , polyunsaturated Calkyl.78. The compound of claim 74 , wherein Rand Rare each an unsubstituted polyunsaturated Calkyl.79. The compound of claim 74 , wherein Ris amino.80. The compound of claim 79 , wherein Rand Rare each an unsubstituted claim 79 , polyunsaturated Calkyl.81. The compound of claim 80 , wherein n is 1.83. The compound of claim 74 , wherein Ris imidazole.84. The compound of claim 83 , wherein Rand Rare each an unsubstituted claim 83 , polyunsaturated Calkyl.85. The compound of claim 84 , wherein n is 1.87. The compound of claim 74 , wherein Ris guanidinium.88. The compound of claim 87 , wherein Rand Rare each an unsubstituted claim 87 , polyunsaturated Calkyl.89. The compound of claim 88 , wherein n is 1.96. A nanoparticle comprising the compound .97. The nanoparticle of claim 96 , further comprising one or more compounds selected from the group consisting of a cationic lipid claim 96 , a PEG-modified lipid claim 96 , a non-cationic lipid and a helper lipid.98. The nanoparticle of claim 96 , further comprising ...

AMINO MERCAPTAN COMPOUND AND PREPARATION METHOD THEREFOR AND USE THEREOF IN PROTECTION AGAINST RADIATION

The present invention discloses an amino mercaptan compound, preparation method thereof and use thereof in radiation protection. The compound has the structure of formula I, wherein Ais selected from: —C(O)NR—, —S(O)—NR—, —S(O)NR—, and —R—NR—; Ais selected from: carbonyl, sulfonyl, sulfinyl, substituted or unsubstituted Calkyl; R, R, R, and Rmay be the same or different and are selected from: hydrogen, substituted or unsubstituted C-Calkyl or heteroalkyl; n is an integer from 0 to 20,000; Rand Rare independently selected from: hydrogen, X, substituted or unsubstituted Calkyl; X is selected from: F, Cl, Br and I; Ris selected from: substituted or unsubstituted C-Calkyl; and Ris selected from: hydrogen, substituted or unsubstituted C-Calkyl. The compound has the effects of reducing the biological damage caused by ionizing radiation, extending the survival period and survival rate of the radiated animals, and significantly alleviating the side effects of radiotherapy, and has a low toxicity. The present invention opens up a new way for protection and treatment of ionizing radiation damage. 2. The compound of claim 1 , wherein Ais selected from: carbonyl claim 1 , sulfonyl claim 1 , sulfinyl claim 1 , substituted or unsubstituted Calkyl; and/or{'sup': 1', '2', '5', '6, 'sub': 1-3', '1', '3, 'R, R, R, and Rmay be the same or different and are selected from: hydrogen, Calkyl, and hydroxy or amino-substituted C-Calkyl or heteroalkyl; and/or'}n is an integer from 0 to 2,000; and/or{'sup': 3', '4, 'sub': '1-3', 'Rand Rare independently selected from: hydrogen, X, substituted or unsubstituted Calkyl; and/or'}X is selected from: F and Cl; and/or{'sup': '7', 'sub': 1', '3, 'Ris selected from: substituted or unsubstituted C-Calkyl; and/or'}{'sup': '8', 'sub': 1', '3, 'Ris selected from: hydrogen, substituted or unsubstituted C-Calkyl; and/or'}{'sup': 3', '4, 'wherein the chiral carbon directly attached to Rand Ris in R configuration or S configuration.'}3. The compound of claim ...

PHARMACEUTICAL COMPOUNDS

Therapeutically-effective amounts of novel analogs or derivatives of alkyl fatty acids, such as but not limited to lipoic acid, and pharmaceutical formulations comprising such analogs or derivatives and pharmaceutically-acceptable carriers therefor, are useful for the treatment, prevention, imaging, and/or diagnosis of medical disorders. 3. A pharmaceutical formulation comprising a therapeutically-effective amount of at least one alkyl fatty acid analog or derivative of and at least one pharmaceutically-acceptable carrier or excipient therefor.4. The pharmaceutical formulation of claim 3 , wherein the at least one alkyl fatty acid analog or derivative is present in an amount to provide from about 0.001 mg/mto about 10 g/m.5. A method of treating claim 1 , preventing claim 1 , imaging claim 1 , or diagnosing a disease characterized by diseased cells or tissues that are sensitive to alkyl fatty acid analogs or derivatives comprising administering to a patient in need thereof a therapeutically-effective amount of at least one alkyl fatty acid analog or derivative according to .6. The method of claim 5 , wherein the at least one alkyl fatty acid analog or derivative is in a pharmaceutical formulation further comprising at least one pharmaceutically-acceptable additive. This invention relates to pharmaceutical agents, and more particularly to therapeutic agents comprising novel analogs and derivatives of alkyl fatty acids, such as but not limited to lipoic acid, and pharmaceutically-acceptable formulations and methods of use therefor.The precise mechanism by which cancer arises continues to be the subject of intense investigation, and thus a unifying theory of the origin of cancer remains elusive. Recent research has confirmed that cancer is a disease arising from a patient's own cells and tissue. Indeed, it is now known that an individual patient may possess multiple tumor cell types, which may not be the same across patients with the same diagnosis or even in the same ...

METHODS AND COMPOSITIONS FOR DELIVERY OF ACTIVE AGENTS

A lipid particle can include a cationic lipid. The cationic lipid can include one or more hydrophobic tails, which can include one or more sites of unsaturation. The sites of unsaturation can include cycloalkyl groups, e.g., cyclopropyl, cyclobutyl, cyclopentyl, or cyclohexyl groups. The lipid particle is suitable for delivering an active agent. 35-. (canceled)6. The cationic lipid of claim 1 , wherein -L-(CRR)— is —(CH)—.9. The cationic lipid of claim 7 , wherein L-Ris —(CH)—CHor —CH.1011-. (canceled)12. The cationic lipid of claim 1 , wherein Hdhas the formula —X—(CRR)—N(R)(R)(R).13. The cationic lipid of claim 12 , wherein Hdis H claim 12 , X is O claim 12 , and Ris absent.14. (canceled)16. The cationic lipid of claim 15 , wherein X and Y are each independently 0 claim 15 , and m is 0 claim 15 , 1 claim 15 , or 2.17. The cationic lipid of claim 16 , wherein n is 1 claim 16 , 2 claim 16 , 3 claim 16 , 4 claim 16 , or 5.18. The cationic lipid of claim 17 , wherein Ris absent; and Rand Rare each independently alkyl optionally substituted by halo; hydroxy; cyano; oxo claim 17 , nitro; C-Ccycloalkyl optionally substituted by halo claim 17 , hydroxy claim 17 , or alkoxy; aryl; heteroaryl; or heterocyclyl.19. (canceled)20. The compound of claim 1 , wherein the compound is in the form of a cationic lipid.21. A lipid particle comprising a neutral lipid claim 20 , a lipid capable of reducing aggregation claim 20 , and a cationic lipid of .2223-. (canceled)24. The lipid particle of claim 21 , further comprising an active agent.25. (canceled)26. A pharmaceutical composition comprising a lipid particle of and a pharmaceutically acceptable carrier.27. A method of modulating the expression of a target gene in a cell claim 21 , comprising providing to the cell a lipid particle of .28. (canceled)29. A method of treating a disease or disorder characterized by the overexpression of a polypeptide in a subject claim 26 , comprising providing to the subject the pharmaceutical ...

PH-SENSITIVE COMPOUND, USE, COMPOSITION AND TREATMENT PROCESS USING SAME

The subject of the present invention is a compound of formula (I) below, the addition salts thereof, the dimer thereof and also the organic or inorganic acid salts thereof, the optical isomers thereof, the geometric isomers thereof, and the solvates thereof such as hydrates: (I) These compounds are sensitive to pH and of use for the treatment of keratin fibres, such as human keratin fibres and in particular the hair. 5. Use according to or , for modulating the hydrophobic nature of keratin fibres , such as human keratin fibres and in particular the hair.6. Cosmetic composition comprising , in an aqueous or aqueous-alcoholic cosmetically acceptable medium , one or more compounds of formula (II) as defined in or .7. Composition according to claim 6 , characterized in that the total concentration of compounds of formula (II) preferably ranges from 0.05 to 20% by weight claim 6 , more preferentially from 0.1 to 15% by weight and even more preferentially from 0.25 to 10% by weight relative to the total weight of the composition.8. Process for treating keratin fibres claim 6 , such as human keratin fibres and in particular the hair claim 6 , comprising a step of applying the composition as defined in or to said fibres.9. Process according to claim 8 , characterized in that the composition contains one or more reducing agents.10. Process according to or claim 8 , characterized in that it comprises an additional step of applying an oxidizing agent claim 8 , after the step of applying the composition.11. Use of the composition as defined in or claim 8 , for the cosmetic treatment of keratin fibres claim 8 , such as human keratin fibres and in particular the hair.12. Multi-compartment device or kit claim 8 , comprising:{'claim-ref': [{'@idref': 'CLM-00006', 'claim 6'}, {'@idref': 'CLM-00007', '7'}], 'a first compartment comprising a composition as defined in or ,'}a second compartment comprising an oxidizing composition. The subject of the invention is pH-sensitive compounds, ...

MULTICOMPONENT DEGRADABLE CATIONIC POLYMERS

Degradable polymers were synthesized that self-assemble with DNA to form particles that are effective for gene delivery. Small changes to polymer synthesis conditions, particle formulation conditions, and polymer structure provides significant changes to efficacy in a cell-type dependent manner. Polymers presented here are more effective than commercially available materials, such as LIPOFECTAMINE 2000™, FUGENE®, or polyethylenimine (PEI), for gene delivery to cancerous fibroblasts or human primary fibroblasts. The presently disclosed materials may be useful for cancer therapeutics and regenerative medicine. 157.-. (canceled)59. The compound of claim 58 , wherein n is an integer selected from the group consisting of from 1 to 1000 claim 58 , from 1 to 100 claim 58 , and from 5 to 20.60. The compound of claim 58 , wherein the polymer has a molecular weight selected from the group consisting of from 5 to 10 kDa claim 58 , from 10 to 15 kDa claim 58 , from 15 to 25 kDa claim 58 , and from 25 to 50 kDa.61. The compound of claim 58 , wherein the polymer is formulated as a particle encapsulating a nucleic acid.624. The compound of claim claim 58 , wherein the nucleic acid is selected from the group consisting of a gene claim 58 , DNA claim 58 , RNA claim 58 , siRNA claim 58 , miRNA claim 58 , isRNA claim 58 , agRNA claim 58 , smRNA claim 58 , and combinations thereof.66. The compound of claim 58 , wherein at least one R″ comprises a biomolecule selected from the group consisting of poly(ethyleneglycol) (PEG) claim 58 , a targeting ligand claim 58 , and a labeling molecule.67. The compound of claim 58 , wherein at least one R″ comprises an C-Calkyl chain claim 58 , wherein the alkyl chain is terminated with a functional group selected from the group consisting of —OH and —NH.72. The compound of claim 58 , wherein R is derived from a C-Cdiacrylate monomer claim 58 , R′ is derived from a C-Camino-alcohol monomer claim 58 , and R″ comprises a 1-(3-aminopropyl)pyrrolidine end ...

SYMMETRIC IONIZABLE CATIONIC LIPID FOR RNA DELIVERY

What are described are compounds of formulas II, III, and IV. The compound of formula II 2. The compound of claim 1 , wherein Land Lboth consist of a linear alkylene consisting of five carbons.3. The compound of claim 1 , wherein Rconsists of ethylene or propylene.4. The compound of claim 1 , wherein Rand Rare the same or different claim 1 , each consisting of hydrogen claim 1 , methyl claim 1 , or ethyl.5. The compound of claim 1 , wherein Lconsists of a bond.6. The compound of claim 1 , wherein Rand Rboth consist of a linear alkenyl consisting of ten carbons.9. The compound of claim 8 , wherein Lconsists of a bond.10. The compound of claim 8 , wherein X consists of S.11. The compound of claim 8 , wherein Rconsists of ethylene.12. The compound of claim 8 , wherein Rconsists of n-propylene or isopropylene.13. The compound of claim 8 , wherein Rand Rseparately consist of methyl claim 8 , ethyl claim 8 , or isopropyl.14. The compound of claim 8 , wherein Land Lconsists of a bond.15. The compound of claim 8 , wherein Land Lconsist of a methylene.16. The compound of claim 8 , wherein Rand Reach consist of branched alkyl.17. The compound of claim 8 , wherein Rconsists of an alkyl.18. The compound of claim 8 , wherein Rand Reach consists of 19 or 20 carbon atoms.19. The compound of claim 8 , wherein Ror Reach consists of 13 or 14 carbon atoms.20. The compound of claim 8 , wherein Lconsists of methylene claim 8 , Rconsists of ethylene claim 8 , Xconsists of S claim 8 , and R4 and R5 each consist of methyl.21. The compound of claim 8 , wherein Lconsists of a bond claim 8 , Rconsists of ethylene claim 8 , X consists of S claim 8 , and Rand Reach consist of methyl.22. The compound of claim 8 , wherein Lconsists of a bond claim 8 , Rconsists of n-propylene claim 8 , X consists of S claim 8 , and Rand Reach consist of methyl.23. The compound of claim 8 , wherein Lconsists of a bond claim 8 , Rconsists of isopropylene claim 8 , X consists of S claim 8 , and Rand Reach consist of ...

COMPOSITION, SYNTHESIS, AND USE OF A NEW CLASS OF ISONITRILES

This invention relates to novel isonitriles, including arylthio isonitriles, and methods for their preparation. The isonitriles include a conjugated ring system. The structure is designed with the flexibility to have multiple substitution patterns. The isonitriles may be used in applications including, but not limited to, pharmaceutical compositions. 2. The compound of claim 1 , wherein Ris selected from alkyl and a cyclic six-membered ring.3. The compound of claim 1 , wherein Ris selected from C-Calkyl and aryl.4. The compound of claim 1 , wherein Ris selected from C-Calkyl and aryl.5. The compound of claim 1 , wherein Rand Rcome together to form a benzo ring.10. The method of claim 9 , wherein the electrophile is selected from the group consisting of diphenyl disulfide claim 9 , methyl iodide claim 9 , propyl bromide claim 9 , propylene oxide claim 9 , cyclohexanone claim 9 , propyl iodide claim 9 , cyclohexenone claim 9 , and mixtures thereof.11. The method of claim 9 , wherein Ris selected from C-Calkyl and aryl.12. The method of claim 9 , wherein Ris selected from C-Calkyl and aryl.13. The method of claim 1 , wherein Rand Rcome together to form a benzo ring. This application claims priority under 35 U.S.C. §119(e) to U.S. Provisional Patent Application Ser. No. 61/942,843, filed Feb. 21, 2014, entitled “Composition, Synthesis, and Use of a New Class of Isonitriles”, which is herein incorporated by reference.Portions of this invention were made with Government support by the National Institutes of Health (NIH), No. 2R15AI051352-04. The Government may have certain rights in the invention.The invention relates to arylthio isonitrile compounds and their synthesis. The invention also relates to new arylthio isonitriles as intermediates for synthesizing isonitriles and nitriles.Isonitrile compounds and derivatives thereof are known in the art and can be used in various applications, including the fields of medicine and pharmaceuticals. For example, bioactive ...

POLYCATIONIC AMPHIPHILES AS ANTIMICROBIAL AGENTS

The present disclosure provides an antimicrobial composition including a polycationic amphiphile compound, and the method of making and the method of using such a compound or composition. The compound having the formula 3. The antimicrobial composition of claim 1 , wherein{'sub': 1', '2', '3', '4', '5', '6', '10', '11', '1-4, 'R, R, R, R, R, R, Ror Ris H or a Calkyl; and'}{'sub': 7', '8', '9', '2-5, 'R, Ror Ris a Calkyl unsubstituted or optionally substituted.'}4. The antimicrobial composition of claim 1 , wherein{'sub': 1', '2', '3', '4', '5', '6', '10', '11', '1-12, 'at least one of R, R, R, R, R, R, R, or Ris a Calkyl substituted with a functional group selected from the group consisting of —SH, allyl, and substituted allyl.'}5. The antimicrobial composition of claim 1 , whereinX or Y is chlorine or bromine; andm and n are integers in the range from 10 to 16.7. The antimicrobial composition of claim 6 , wherein each of m and n is 10 claim 6 , 11 or 12 claim 6 , and each of R claim 6 , R claim 6 , R claim 6 , Rand Ris methyl or ethyl claim 6 , and Ris hydrogen claim 6 , methyl or ethyl.9. The antimicrobial composition of claim 7 , wherein the middle nitrogen (N) atom of the compound (10 claim 7 , 3 claim 7 , 0 claim 7 , 3 claim 7 , 10) is further substituted and ionized.11. A method of making the antimicrobial composition of comprising mixing an effective amount of a compound having the formula (I) or (II) and a carrier.12. A method of killing or inhibiting microbial growth claim 1 , comprising applying the antimicrobial composition of comprising a compound having the formula (I) or (II).13. The method of claim 12 , wherein the antimicrobial composition is used to kill or inhibit growth of at least one group of microorganisms selected from the group consisting of bacteria claim 12 , viruses claim 12 , yeast claim 12 , fungi claim 12 , and protozoa claim 12 , or to inhibit formation of a biofilm or eradicate a pre-established biofilm.15. The method of claim 14 , ...

Synthesis and growth regulatory activity of a prototype member of a new family of aminothiol radioprotectors

The synthesis, growth inhibition and radioprotective activity of the PrC-210 aminothiol, 3-(methyl-amino)-2-((methylamino)methyl)propane-l-thiol, and its polyamine and thiolated polyamine progenitors are reported. All of the molecules significantly inhibited growth of cultured normal human fibroblasts. The combination of an ROS-scavenging thiol group and a positively charged alkyl-amine backbone provided the most radioprotective aminothiol molecule.

Multicomponent Degradable Cationic Polymers

Degradable polymers were synthesized that self-assemble with DNA to form particles that are effective for gene delivery. Small changes to polymer synthesis conditions, particle formulation conditions, and polymer structure provides significant changes to efficacy in a cell-type dependent manner. Polymers presented here are more effective than commercially available materials, such as LIPOFECTAMINE 2000™, FUGENE®, or polyethylenimine (PEI), for gene delivery to cancerous fibroblasts or human primary fibroblasts. The presently disclosed materials may be useful for cancer therapeutics and regenerative medicine. 59. The compound of claim 58 , wherein n is an integer selected from the group consisting of: an integer from 1 to 1 claim 58 ,000; an integer from 1 to 100; an integer from 1 to 30; an integer from 5 to 20; an integer from 10 to 15; and an integer from 1 to 10.62. A pharmaceutical composition comprising a compound of .63. The pharmaceutical composition of further comprising a therapeutic agent.64. The pharmaceutical composition of claim 63 , wherein the therapeutic agent is selected from the group consisting of a gene claim 63 , DNA claim 63 , RNA claim 63 , siRNA claim 63 , miRNA claim 63 , isRNA claim 63 , agRNA claim 63 , smRNA claim 63 , a nucleic acid claim 63 , a peptide claim 63 , a protein claim 63 , a chemotherapeutic agent claim 63 , a hydrophobic drug claim 63 , and a small molecule drug.65. The pharmaceutical composition of further comprising a nanoparticle or microparticle comprising a compound of formula (I).67. The copolymer of claim 66 , wherein n is an integer selected from the group consisting of: an integer from 1 to 1 claim 66 ,000; an integer from 1 to 100; an integer from 1 to 30; an integer from 5 to 20; an integer from 10 to 15; and an integer from 1 to 10.71. A pharmaceutical composition comprising a copolymer of .72. The pharmaceutical composition of further comprising a therapeutic agent.73. The pharmaceutical composition of claim 71 ...

PROCESS FOR THE PREPARATION OF FREEZE-DRIED 2-[(3-AMINOPROPYL)AMINO]ETHANETHIOL FORMULATION

A process for the preparation of freeze-dried 2-[(3-aminopropyl)amino]ethanethiol including the following steps: a) the reaction of a solution of amifostine with a strong acid, to obtain a solution of 2-[(3-aminopropyl)amino]ethanethiol, and b) the freeze-drying of the solution of 2-[(3-aminopropyl)amino]ethanethiol, with or without addition of excipients. 1. A process for the preparation of freeze-dried 2-[(3-aminopropyl) amino]ethanethiol comprising the following steps:a) the reaction of a solution of amifostine with a strong acid, to obtain a solution of 2-[(3-aminopropyl)amino]ethanethiol, andb) the freeze-drying of the solution of 2-[(3-aminopropyl)amino]ethanethiol, with or without addition of excipients.2. The process of claim 1 , wherein the strong acid is chosen from the group consisting of: hydrochloric acid claim 1 , phosphoric acid claim 1 , sulfuric acid claim 1 , and mixtures thereof.3. The process of claim 1 , wherein the strong acid is hydrochloric acid.4. The process of claim 1 , wherein step a) is carried out at a temperature comprised between 50° C. and 90° C.5. The process of claim 1 , wherein step a) is carried out for 30 minutes to 24 hours.6. The process of claim 1 , wherein the concentration of amifostine is comprised between 80 mg/ml and 500 mg/ml.7. The process of claim 1 , wherein the molarity of the acid is comprised between 1M and 4M.8. The process of claim 1 , wherein the molar ratio between the amount of amifostine and the amount of acid is comprised between 1:0.5 and 1:3.9. The process of claim 1 , further comprising a step a1) claim 1 , after step a) and before step b) claim 1 , for diluting the solution of 2-[(3-aminopropyl)amino]ethanethiol claim 1 , with or without addition of excipients in the solution.10. The process of claim 9 , wherein step a1) consists in the addition of an aqueous solution comprising water or at least one poloxamer into the solution of 2-[(3-aminopropyl)amino]ethanethiol.11. A lyophilisate of 2-[(3- ...

Method for Preparation of N-Acetyl Cysteine Amide and Derivatives Thereof

The present invention includes methods for making and isolating N-acetylcysteine amide, (2R,2R′)-3,3′-disulfanediyl bis(2-acetamidopropanamide, diNACA), intermediates and derivatives thereof comprising: contacting cystine with an alcohol and a chlorinating reagent to form an organic solution containing L-cystine dimethylester dihydrochloride; combining dried or undried L-cystine dimethylester dihydrochloride with a triethylamine, an acetic anhydride, and an acetonitrile to form a di-N-acetylcystine dimethylester; mixing dried di-N-acetylcystine dimethylester with ammonium hydroxide to form a di-N-acetylcystine amide (diNACA); and separating dried di-N-acetylcystine dimethylester into N-acetylcysteine amide with dithiothreitol, triethylamine and an alcohol. 1. A process for making N-acetylcysteine amide comprising:contacting cystine with an alcohol and a chlorinating reagent to form an organic solution containing L-cystine dimethylester dihydrochloride;combining dried or undried L-cystine dimethylester dihydrochloride with a triethylamine, an acetic anhydride, and an acetonitrile to form a di-N-acetylcystine dimethylester;mixing dried di-N-acetylcystine dimethylester with ammonium hydroxide to form a di-N-acetylcystine amide; andseparating dried di-N-acetylcystine dimethylester into N-acetylcysteine amide with dithiothreitol, triethylamine and an alcohol.2. The process of claim 1 , wherein the alcohol is an organic alcohol selected from an alkyl alcohol claim 1 , methanol claim 1 , ethanol claim 1 , propanol claim 1 , isopropanol or butanol.3. The process of claim 1 , wherein the step of contacting L-cysteine with an alcohol and a chlorinating reagent to form an organic solution containing L-cystine dimethylester dihydrochloride is conducted at −10 to 10° C. and then heated to reflux at 65 to 70° C. to completion.4. The process of claim 1 , wherein the chlorinating agent is thionyl chloride.5. The process of claim 1 , further comprising a solvent exchange between the ...

Phenolic resin composition and the use thereof in a rubber composition to reduce hysteresis

This invention relates to a phenolic resin composition comprising a phenolic resin admixed with and/or modified by one or more functionalized organosulfur compounds. This invention also relates to a rubber composition comprising (i) a natural rubber, a synthetic rubber, or a mixture thereof; (ii) one or more phenolic resins; and (iii) one or more functionalized organosulfur compounds. The interaction between the component (i) and the components (ii) and (iii) reduces the hysteresis increase compared to a rubber composition without the component (iii), upon curing the rubber composition. The invention also relates to a process for preparing the phenolic resin composition, a process for preparing the rubber composition, and a process for reducing the hysteresis increase caused in a rubber composition when a phenolic resin is added to a rubber composition.

DITHIOAMINE REDUCING AGENTS

Dithioamine reducing agents useful for the reduction of disulfide bonds. The reducing agents of this invention are useful, for example, to reduce disulfide bonds, particularly in proteins, or to prevent the formation of disulfide bonds, particularly in proteins and other biological molecules. Reducing agents of this invention can be employed to regulate protein function in proteins in which a sulfhydryl group is associated with biological activity. Reducing agents of this invention can prevent inactivation of a given protein or enhance activation of a given protein or other biological molecule in vitro and/or in vivo. Reducing agents of this invention can prevent or reduce oxidation of cysteine residues in proteins and prevent the formation of reduced activity protein dimers (or other oligomers). Reducing agents of this invention are useful and suitable for application in a variety of biological applications, particularly as research and synthetic reagents. The invention provides S-acylated dithioamines which can be selectively activated reducing agents by removal of the S-acyl groups enzymatically or chemically. The invention further provides dithiane precursors of thioamino reducing agents. The invention provides dithioamine reducing agents, S-acylated dithioamines and dithianes which are immobilized on surfaces, including among others, glass, quartz, microparticles, nanoparticles and resins. 2. The compound of wherein neither Ror Ris an —NHgroup.3. The compound of wherein one of Ror Ris a —CORgroup.4. The compound of wherein R claim 3 , Rand Rare all hydrogens.5. The compound of wherein R claim 3 , R claim 3 , R claim 3 , Rand Rare all hydrogens.6. The compound of wherein both Rare hydrogens.7. The compound of wherein both of Rare acyl groups.8. The compound of wherein Ris independently hydrogen claim 3 , a 1-12 carbon alkyl group claim 3 , an aryl group claim 3 , a heterocyclic group claim 3 , or a heteroaryl group.9. The compound of wherein R-Rare all hydrogens ...

MULTICOMPONENT DEGRADABLE CATIONIC POLYMERS

Degradable polymers were synthesized that self-assemble with DNA to form particles that are effective for gene delivery. Small changes to polymer synthesis conditions, particle formulation conditions, and polymer structure provides significant changes to efficacy in a cell-type dependent manner. Polymers presented here are more effective than commercially available materials, such as LIPOFECTAMINE 2000™, FUGENE®, or polyethylenimine (PEI), for gene delivery to cancerous fibroblasts or human primary fibroblasts. The presently disclosed materials may be useful for cancer therapeutics and regenerative medicine. 2. The compound of claim 1 , under the further proviso that if at least one R group comprises an ester linkage claim 1 , then the R″ groups impart one or more of the following characteristics to the compound of formula (I): independent control of cell-specific uptake and/or intracellular delivery of a particle; independent control of endosomal buffering and endosomal escape; independent control of DNA release; triggered release of an active agent; modification of a particle surface charge; increased diffusion through a cytoplasm of a cell; increased active transport through a cytoplasm of a cell; increased nuclear import within a cell; increased transcription of an associated DNA within a cell; increased translation of an associated DNA within a cell; increased persistence of an associated therapeutic agent within a cell claim 1 , wherein the therapeutic agent is selected from the group consisting of DNA claim 1 , RNA claim 1 , a peptide or a protein.3. The compound of claim 1 , wherein n is an integer from 1 to 1 claim 1 ,000.4. The compound of claim 1 , wherein n is an integer from 1 to 100.5. The compound of claim 1 , wherein n is an integer from 1 to 30.6. The compound of claim 1 , wherein n is an integer from 5 to 20.7. The compound of claim 1 , wherein n is an integer from 10 to 15.8. The compound of claim 1 , wherein n is an integer from 1 to 10.9. The ...

INDUSTRIAL PROCESS FOR THE PREPARATION OF (5S, 10S)-10-BENZYL-16-METHYL-11, 14, 18-TRIOXO-15, 17, 19-TRIOXA-2,7,8-TRITHIA-12-AZAHENICOSAN-5-AMINIUM(E)-3-CARBOXYACRYLATE SALT

The present invention relates to an industrial process for the preparation of (5S,10S)-10-benzyl-16-methyl-11,14,18-trioxo-15,17,19-trioxa-2,7,8-trithia-12-azahenicosan-5-aminium (E)-3-carboxyacrylate salt of following formula (I): wherein X is fumarate. This process comprises the following successive key steps: a kinetic resolution, formation of disulfide compound, peptide coupling, and anion exchange reaction to obtain the desired product of formula (I). 2. Industrial process according to claim 1 , wherein crystallization in step 1b comprises the following successive steps:1b.1) dissolution of quinine salt at solubilizing temperature, then;1b.2) cooling the mixture obtained in step 1 b.1, until temperature ranging from 10° C. to 20° C.;1b.3) isolating quinine salt obtained after step 1 b.2 by filtration.3. Industrial process claim 1 , according to claim 1 , wherein in step 1a is solvent is ethyl acetate.5. Industrial process claim 1 , according to claim 1 , further comprising after step 1d.1 claim 1 , the following successive steps:1d.2.1) Alkaline hydrolysis in polar and protic solvent, then1d.2.2) Acidic treatment, then;1d.2.3) Extraction of compound (E) with organic solvent.6. Industrial process according to claim 1 , wherein the recovering of quinine in step 1e comprises the following successive steps:1e.1) Combining the aqueous phases obtained in step 1d.2.1 and in step 1d.2.2, then;1e.2) Adding 20% by weight of aqueous solution of NaOH in water to adjust the pH to 12, then;1e.3) Extracting the resulting mixture obtained in step 1e.2 with AcOEt, then;1e.4) Concentrating under vacuum the resulting organic layer obtained in step 1e.3, then;1e.5) Adding petroleum ether at temperature ranging from 10° C. to 20° C., then;1e.6) Filtrating the resulting solid obtained at the end of step 1e.5 and recovering quinine.7. Industrial process according to claim 1 , further comprising after step 2b and before step 3 the following successive steps:2b.1) adding water ...

METHOD OF TREATING ADVANCED NON-ALCOHOLIC STEATOHEPATITIS

A compound of Formula (I): 4. The method of claim 1 , wherein the compound is administered orally.5. The method of claim 4 , wherein the compound is administered as a tablet or a capsule.6. The method of claim 2 , wherein the compound is present in an orthorhombic crystalline form.7. The method of claim 1 , wherein the compound is administered as a liquid dosage form.8. The method of claim 1 , wherein the compound is administered in an amount from about 100 to about 4 claim 1 ,000 mg/day claim 1 , divided into one claim 1 , two claim 1 , or three portions.9. The method of claim 1 , wherein the patient diagnosed with advanced NASH exhibits one or more of hepatic fibrosis claim 1 , spider angiomata claim 1 , ascites claim 1 , splenomegaly claim 1 , hard liver border claim 1 , palmar erythema claim 1 , asterixis claim 1 , or portal hypertension.10. The method of claim 9 , wherein the patient's hepatic fibrosis is reduced.11. The method of claim 1 , wherein the patient diagnosed with advanced NASH exhibits one or more of hepatic scarring claim 1 , cirrhosis claim 1 , or hepatocellular carcinoma (HCC).12. The method of claim 11 , wherein the patient's hepatic scarring is reduced.13. The method of claim 1 , wherein the patient is a pediatric patient.15. The method of claim 14 , wherein the compound is administered orally.16. The method of claim 14 , wherein the compound is administered as a tablet or a capsule.17. The method of claim 14 , wherein the compound is administered as a liquid dosage form.18. The method of claim 13 , wherein the compound is administered in an amount from about 100 to about 4 claim 13 ,000 mg/day claim 13 , divided into one claim 13 , two claim 13 , or three portions.19. The method of claim 14 , wherein the patient diagnosed with advanced NASH exhibits one or more of hepatic fibrosis claim 14 , spider angiomata claim 14 , ascites claim 14 , splenomegaly claim 14 , hard liver border claim 14 , palmar erythema claim 14 , asterixis claim 14 , or ...

PRECURSOR FOR LABELING THERAPEUTIC AGENT FOR LIVER CANCER AND METHOD FOR MANUFACTURING THE SAME

A precursor for labeling therapeutic agents for liver cancer and a method for manufacturing the same are revealed. The chemical structure of the precursor has a ligand linked to complex compounds of radioisotopes. Moreover, the chemical structure of the precursor further includes a specific functional group soluble in Lipiodol or having properties of Lipiodol. Thus the radioisotopes attached to the precursor are allowed to retain in hepatic tissues of patients with liver cancer for internal radiation therapy of liver cancer. 2. The precursor as claimed in claim 1 , wherein the precursor is linked to a radioisotope to form a labeling substance for therapeutic agents for liver cancer;{'sup': 188', '99m, 'the radioisotope is Rhenium-188 (Re) or technetium-99m (Tc).'}3. A method for manufacturing a precursor for labeling therapeutic agents of liver cancer comprising the steps of:producing L-Nε-tert-butoxycarbonyl-Nα-[2-(triphenylmethyl)thioacetyl]lysine methyl ester (hereafter called compound 1) by an amidation reaction between L-Nε-tert-butoxycarbonyllysine methyl ester and triphenylmethyl thio glycolic acid;hydrolyzing the compound 1 to produce L-Nε-tert-butoxycarbonyl-Nα-[2-(triphenylmethyl)thioacetyl]lysine (hereafter called compound 2);producing L-Nε-tert-butoxycarbonyl-Nα-[2-(triphenylmethyl)thioacetyl]-6-aza-5-oxo-9-(triphenyl methyl)thio-1,5-nonanediamine (hereafter called compound 3) by an amidation reaction between the compound 2 and 2-(triphenylmethyl)thio]ethylamine;decomposing the compound 3 by acid to produce L-Nε-[2-(triphenylmethyl)thioacetyl]-6-aza-5-oxo-9-(triphenylmethyl) thio-1,5-nonanediamine (hereafter called compound 4); and L-Nε-[2-(Triphenylmethyl)thioacetyl]-Nα-8-heptadecenylcarbonyl-6-aza-5-oxo-9-(triphenyl methyl) thio-1,5-nonanediamine (hereafter called HOC-NODA)/or', 'L-Nε-[2-(Triphenylmethyl)thioacetyl]-Nα-5,6-diiodotetradecylcarbonyl-6-aza-5-oxo-9-(triphenylmethyl) thio-1,5-nonanediamine (hereafter called TDI-NODA)., 'carrying out an ...

METHOD FOR PREPARING 3-METHYLTHIOPROPIONALDEHYDE

The present invention relates to a method for preparing 3-methylthiopropionaldehyde by reacting methyl mercaptan with acrolein, in which deviations in the stoichiometry of methyl mercaptan to acrolein in the reaction to give 3-methylthiopropionaldehyde are compensated for by supplying or by forming 1,3-bis(methylthio)-1-propanol, and also to the use of 1,3-bis(methylthio)-1-propanol as a storage form of methyl mercaptan and/or 3-methylthiopropionaldehyde. 1: A method for continuously preparing 3-methylthiopropionaldehyde , the method comprising:reacting methyl mercaptan with acrolein, to obtain the 3-methylthiopropionaldehyde,wherein deviations in a stoichiometry of the methyl mercaptan to the acrolein during the reacting to obtain the 3-methylthiopropionaldehyde are compensated for by supplying or forming 1,3-bis(methylthio)-1-propanol, andwhereinif the methyl mercaptan is present in excess with respect to the acrolein, an excess methyl mercaptan is converted to the 1,3-bis(methylthio)-1-propanol with the 3-methylthiopropionaldehyde,orif the acrolein is present in excess with respect to the methyl mercaptan, the 1,3-bis(methylthio)-1-propanol is supplied to the reacting of the methyl mercaptan with the acrolein.2: The method according to claim 1 , wherein a molar ratio of the methyl mercaptan to the 3-methylthiopropionaldehyde during the reacting to obtain the 1 claim 1 ,3-bis(methylthio)-1-propanol is from 0.1:1 (mol/mol) to 1:1 (mol/mol).3: The method according to claim 1 , wherein an excess acrolein is present and the excess acrolein is reacted with the 1 claim 1 ,3-bis(methylthio)-1-propanol to obtain the 3-methylthiopropionaldehyde.4: The method according to claim 1 , wherein a portion of a stream comprising the methyl mercaptan is branched off before the reacting to obtain the 3-methylthiopropionaldehyde and is supplied to the forming of the 1 claim 1 ,3-bis(methylthio)-1-propanol by reacting the 3-methylthiopropionaldehyde with the methyl mercaptan.5: The ...

Processes for the preparation of enamines

The invention disclosed in this document is related to the field of processes for the preparation of enamines wherein R1, R2, R3, R4, R5, and further information are disclosed herein.

THIOL-FORMYL HEMIACETAL CORROSION INHIBITORS

The present invention generally relates to compositions and methods for inhibiting corrosion at a surface in the production, transportation, storage, and separation of crude oil and natural gas. 2. (canceled)4. An anti-corrosion composition comprising the compound of formula (I) claim 3 , (II) claim 3 , (III) or (IV) of .5. The method of claim 1 , wherein the anti-corrosion composition comprises the compound of formula (I).8. (canceled)9. The method of claim 1 , wherein Rof Formula (I) claim 1 , (IA) or (IB) is either:{'sub': 1', '24', '1', '24', '6', '12', '3', '8', '2', '2', '1', '6', '1', '6', '2', '10', '11', '2', '10', '11', '1', '6', '2', '1, 'C-Calkyl, C-Calkenyl, C-Caryl, monocyclic or bicyclic heteroaryl, or C-Ccycloalkyl, wherein said alkyl, alkenyl, aryl, heteroaryl, or cycloalkyl are each independently unsubstituted or substituted with 1 to 3 substituents independently selected from —F, —Cl, —NO, —CN, —OH, —NH, C-Chaloalkyl, C-Calkoxy, —COR, and —CON(R), wherein Rand R, at each occurrence, are each independently hydrogen or C-Calkyl; or optionally one or more of the —CH— groups of Ris replaced with a —C(O)O— group; or'}{'sub': 1', '18', '3', '8', '1', '6', '2', '10', '10', '1', '6', '2', '1, 'C-Calkyl, or C-Ccycloalkyl, wherein said alkyl, or cycloalkyl are each independently unsubstituted or substituted with 1 to 3 substituents independently selected from —OH, C-Calkoxy, or —CORwherein Rat each occurrence, is independently hydrogen or C-Calkyl; or optionally one or more of the —CH— groups of Ris replaced with a —C(O)O— group.'}10. (canceled)11. The method of claim 1 , wherein Rof Formula (I) claim 1 , (IA) or (IB) is either:{'sub': 1', '18', '3', '8, 'C-Calkyl or C-Ccycloalkyl; or'}{'sub': 1', '12', '2', '1', '1', '12', '2, 'C-Calkyl optionally substituted with 1 to 3 substituents of —OH or —COH; or Ris C-Calkyl wherein one or more of the —CH— groups is replaced with a —C(O)O— group; or'}{'sub': 1', '12', '2', '1', '1', '12', '2, 'C-Calkyl substituted ...

FLUOROUS COMPOUND, METHOD OF PREPARING FLUOROUS TAGGED PROTEIN, AND METHOD OF IMMOBILIZING PROTEIN

A fluorous compound, a method of preparing a fluorous tagged protein, and a method of immobilizing protein are provided. The fluorous compound is represented by Y-L-R, wherein Y is a fluorous group; L is a linker, and the linker includes a bivalent group having a sulfo group, a bivalent group having a carboxyl group, or a bivalent group of hydrophilic amino acid; and R is a functional group capable of bonding to protein. 1. A fluorous compound represented by Y-L-R , wherein Y is a fluorous group; L is a linker , and the linker comprises a bivalent group having a sulfo group , a bivalent group having a carboxyl group , or a bivalent group of a hydrophilic amino acid; and R is a functional group capable of bonding to a protein.2. The fluorous compound of claim 1 , wherein the linker further comprises a C1 to C12 alkylene group claim 1 , a C6 to C15 arylene group claim 1 , a C2 to C12 heteroarylene group claim 1 , a C1 to C12 alkyleneoxy group claim 1 , a C1 to C12 alkylene sulfide group claim 1 , a C3 to C12 cycloalkylene group claim 1 , an amide group claim 1 , a bivalent group of ethylene glycol claim 1 , or a combination thereof.3. The fluorous compound of claim 1 , wherein the bivalent group having the sulfo group is a bivalent group of cysteic acid.4. The fluorous compound of claim 1 , wherein the bivalent group of the hydrophilic amino acid comprises a bivalent group of aspartic acid claim 1 , a bivalent group of glutamic acid claim 1 , or a bivalent group of arginine.5. The fluorous compound of claim 1 , wherein the fluorous group comprises a straight or branched C3 to C8 fluoroalkyl group.6. The fluorous compound of claim 1 , wherein the functional group capable of bonding to the protein comprises a group having a thiol group and an amine group claim 1 , a group having a thioester group claim 1 , or a group having a boric acid group.9. A method of preparing a fluorous tagged protein claim 1 , comprising:providing a protein; andbonding a fluorous compound to ...

LIPID CONTAINING FORMULATIONS

Compositions and methods useful in administering nucleic acid based therapies, for example association complexes such as liposomes and lipoplexes are described. 2138-. (canceled)140324-. (canceled)326349-. (canceled) This application is a continuation application of U.S. application Ser. No. 15/492,898, filed Apr. 20, 2017, which is a continuation application of U.S. application Ser. No. 14/149,496, filed Jan. 7, 2014, now abandoned, which is a divisional application of U.S. application Ser. No. 13/211,094, filed Aug. 16, 2011, issued as U.S. Pat. No. 8,642,076 on Feb. 4, 2014, which is a continuation application of U.S. application Ser. No. 12/056,230, filed Mar. 26, 2008, issued as U.S. Pat. No. 8,034,376 on Oct. 11, 2011, which is a continuation application of International Application No. PCT/US2007/080331, filed Oct. 3, 2007, which claims priority to U.S. Provisional Application No. 60/828,022 filed Oct. 3, 2006 and U.S. Provisional Application No. 60/870,457 filed Dec. 18, 2006. The entire content of each of these applications is hereby incorporated by reference.This invention relates to compositions and methods useful in administering nucleic acid based therapies, for example association complexes such as liposomes and lipoplexes.The opportunity to use nucleic acid based therapies holds significant promise, providing solutions to medical problems that could not be addressed with current, traditional medicines. The location and sequences of an increasing number of disease-related genes are being identified, and clinical testing of nucleic acid-based therapeutics for a variety of diseases is now underway.One method of introducing nucleic acids into a cell is mechanically, using direct microinjection. However this method is not generally effective for systemic administration to a subject.Systemic delivery of a nucleic acid therapeutic requires distributing nucleic acids to target cells and then transferring the nucleic acid across a target cell membrane intact ...

NUCLEIC ACID-CONTAINING LIPID NANOPARTICLE

The present invention provides a nucleic acid-containing lipid nanoparticle comprising an analog of a fatty acid ester of glycerol, and a nucleic acid, wherein the analog is not hydrolyzable by a lipase. 127-. (canceled)29. The nucleic acid-containing lipid nanoparticle according to claim 28 , wherein the analog of the fatty acid ester of glycerol is an analog of a glycerophospholipid.30. The nucleic acid-containing lipid nanoparticle according to claim 28 , wherein the lipase is phospholipase A2.32. The nucleic acid-containing lipid nanoparticle according to claim 28 , further comprising a cationic lipid.34. The nucleic acid-containing lipid nanoparticle according to claim 33 , wherein the cationic lipid is the lipid B.35. The nucleic acid-containing lipid nanoparticle according to claim 28 , further comprising a lipid derivative or a fatty acid derivative of a water-soluble polymer.36. The nucleic acid-containing lipid nanoparticle according to claim 28 , further comprising a neutral lipid.37. The nucleic acid-containing lipid nanoparticle according to claim 28 , wherein the nucleic acid is a nucleic acid having a silencing effect on a target gene through the use of RNA interference (RNAi).38. A method for stabilizing a nucleic acid-containing lipid nanoparticle using an analog of a fatty acid ester of glycerol claim 28 , wherein the analog is not hydrolyzable by a lipase.39. A method for introducing a nucleic acid into a cell using the nucleic acid-containing lipid nanoparticle according to .40. The method according to claim 39 , wherein the cell is a cell residing at a mammalian tumor or inflammation site.41. The method according to claim 39 , wherein a method for the introduction into the cell is a method of introduction into the cell by intravenous administration or subcutaneous administration.42. A method for treating a cancer or an inflammatory disease claim 28 , comprising administering the nucleic acid-containing lipid nanoparticle according to to a mammal ...

Compounds and Methods for Use in Detecting Gabapentin

Compounds and methods for use in detecting gabapentin in a sample suspected of containing gabapentin are disclosed. Gabapentin derivatives are used to produce gabapentin conjugates. A gabapentin-immunogenic carrier conjugate may be used as an immunogen for the preparation of an anti-gabapentin antibody. A gabapentin-detectable label may be used in a signal producing system in gabapentin assays. 2. The compound of claim 1 , wherein said linker comprises 0 to 40 carbon atoms and 0-6 heteroatoms.3. The compound of claim 2 , wherein W is a lower alkyl and said linker is selected from the group consisting of:{'sub': 2', 'n, '—(CH)C(O)—;'}{'sub': 2', 'n, '—C(O)(CH)—;'}{'sub': 2', 'n, '—C(O)(CH)NH—C(O)—;'}{'sub': 2', 'm', '2', 'n, '—C(O)(CH)NH—C(O)(CH)—;'}{'sub': 2', 'n', '2, '—(CH)SCHC(O)—;'}{'sub': 2', 'm', '2', '2', 'n, '—(CH)SCHC(O)(CH)—;'}{'sub': 2', 'm', '2', 'n, '—(CH)C(O)NH(CH)—;'}{'sub': 2', 'n, '—(CH)NH—C(O)—;'}{'sub': 2', 'm', '2', 'n, '—(CH)NH—C(O)(CH)—;'}{'sub': 2', 'n, '—C(O)—(CH)—; and'}{'sub': 2', 'n, '—(CH)—, and'}wherein m, n, o, and p are independently selected from an integer from 0 to 10.4. The compound of claim 2 , wherein W is a carbonyl and said linker is selected from the group consisting of:{'sub': 2', 'n, '—(CH)C(O)—;'}{'sub': 2', 'n', '2, '—(CH)SCHC(O)—;'}{'sub': 2', 'm', '2', '2', 'n, '—(CH)SCHC(O)(CH)—;'}{'sub': 2', 'm', '2', 'n, '—(CH)C(O)NH(CH)—;'}{'sub': 2', 'n, '—(CH)NH—C(O)—;'}{'sub': 2', 'm', '2', 'n, '—(CH)NH—C(O)(CH)—; and'}{'sub': 2', 'n, '—(CH)—, and'}wherein m, n, o, and p are independently selected from an integer from 0 to 10.5. The compound of claim 1 , wherein W is a lower alkyl group and the lower alkyl group is a methyl group.6. The compound of claim 1 , wherein said reactive functional group is selected from the group consisting of halogen claim 1 , OH claim 1 , SH claim 1 , NH claim 1 , O-lower alkyl claim 1 , epoxy claim 1 , S-acyl claim 1 , carboxyl claim 1 , maleimidyl claim 1 , haloacetamide claim 1 , hydroxysuccinimidyl ...

Polythiol for epoxy resin curing agent

Polythiols and use as epoxy resin curing agents

Polythiols prepared by the reaction of hydrogen sulfide or organic dithiols with polyglycidyl substituted amines have been found to be outstanding curing agents for epoxy resins. Epoxy resins cured with these polythiols are characterized by not only improved gel times, but also improved cure rates, better heat resistance and greater resistance to absorption of water. A useful polythiol is the reaction product of N,N,N',N'-tetraglycidyl-m-xylylenediamine with hydrogen sulfide.

Polythiols and use as epoxy resin curing agents

A process for curing polyepoxide comprising mixing together and reacting together (a) at least one polyepoxide and (b) at least one polythiol having the structure: (XSCH₂CHOH₂CH₂) b -A-R-N (CH₂CHOHCH₂SX)₂ wherein: R is aromatic, substituted aromatic, methylene bis-diphenyl, xylylene, cycloaliphatic, substituted cycloaliphatic, methylene bis-dicyclohexyl, dimethylene cyclohexyl, methylene cyclohexyl or aliphatic, A is N or O X is -H or -R′SH, R′ is alkylene, cycloalkylene or alkylene substituted aromatic, and when A is O, b is 1 and when A is N, b is 2.

New Α-aminoacetophenone photoinitiators and photopolymerizable compositions comprising these photoinitiators

Nitrogen containing anti-oxidant compositions

This invention describes compositions containing nitrogen, sulfur and optionally oxygen which are useful as antioxidants for lubricants.

Photocurable resin compositi0n containing anthraquinone derivative

본 발명은 장파장의 자외광이나 가시광에 대해 고감도인 광경화성 수지 조성물, 특히 실링제로서 유용한 광경화성 수지 조성물을 제공한다. 보다 구체적으로 본 발명은 하기 화학식 Ⅰ로 표시되는 안트라퀴논 유도체로 이루어지는 성분(a), 및 분자 내에 (메트)아크릴로일기를 갖는 화합물로 이루어지는 성분(b)를 함유하는 광경화성 수지 조성물로서, 상기 성분(b)에 포함되는 성분의 일부 또는 전부는 분자 내에 옥시란일기를 추가로 갖고, 상기 성분(a)의 함유량은 상기 성분(b)의 함유량에 대해 0.01 내지 10질량%인 광경화성 수지 조성물에 관한 것이다. 화학식 I (화학식 I에서, X는 페닐기 또는 탄소수 1 내지 8의 알킬기, 당해 페닐기 또는 알킬기의 알코올체, 또는 당해 알코올체의 유도체를 나타낸다) The present invention provides a photocurable resin composition which is highly sensitive to ultraviolet light and visible light having a long wavelength, particularly a photocurable resin composition useful as a sealing agent. More specifically, the present invention provides a photocurable resin composition containing a component (a) consisting of an anthraquinone derivative represented by the following formula (I) and a component (b) consisting of a compound having a (meth) acryloyl group in a molecule thereof. Part or all of the component contained in component (b) further has an oxiranyl group in a molecule | numerator, and content of the said component (a) is 0.01-10 mass% with respect to content of the said component (b), The photocurable resin composition It is about. Formula I (Wherein X represents a phenyl group or an alkyl group having 1 to 8 carbon atoms, an alcohol of the phenyl group or an alkyl group, or a derivative of the alcohol)

1,4-dihydrothionapthoquinone and heterocyclic congeners which inhibit lipoxygenase enzymes

The present invention provides certain novel 1,4-dihydrothionapthoquinone and heterocyclic cogeners of Formula (I), which are useful as inhibitors of leukotriene biosynthesis and as inhibitors of lipoxygenase. They are thus employed wherever it is medically necessary or desirable to inhibit these systems.

Process for the preparation of thioalkylamine derivatives

반응 증류를 이용한 3-머캅토프로피온산의 제조 방법

본 발명은 3-머캅토프로피온산의 제조 방법에 관한 것이다. 본 발명에 따르면, 반응 증류를 이용하여 보다 단순화된 공정과 우수한 반응 효율로 3-머캅토프로피온산을 대량 생산할 수 있는 제조 방법이 제공된다.

Lipid containing formulations

핵산계 치료제, 예를 들면, 리포솜 및 리포플렉스와 같은 회합 복합체의 투여에 유용한 조성물 및 방법에 관한 것이다. The present invention relates to compositions and methods useful for the administration of association complexes, such as nucleic acid-based therapeutics such as liposomes and lipoplexes. 핵산, 리포솜, 회합 복합체 Nucleic Acids, Liposomes, Association Complexes

Phenoxyalkylcarboxylic acid derivatives and process of preparing the same

Phenoxyalkylcarboxylic acid derivatives represented by the following formula (I) ##STR1## having a strong and selective leukotriene antagonistic action and useful for prophylaxis and therapy of allergic diseases as asthma and processes of preparing the same.

Process for making polymorphic form A of 4-[6-acetyl-3-[3-(4-acetyl-3-hydroxy-2-propylphenylthio)propoxy]-2-propylphenoxy]butyric acid

Process for making a pharmaceutical composition, comprising: a compound of formula (1) in crystalline form: together with a pharmaceutically acceptable carrier or excipient, wherein the compound of formula (1) is present in polymorphic crystal form A substantially free of other polymorphs, and methods for making this polymorph.

Alpha-diketones for led photocuring

The present invention relates to substituted derivatives of alpha-diketones which can be used as photoinitiators in LED photocuring and to a process for curing compositions comprising said alpha-diketones.

Process for making polymorphic form a of 4-[6-acetyl-3-[3-(4-acetyl-3-hydroxy-2-propylphenythio)propoxy]-2-propylphenoxy]butyric acid

본 발명은 약학적으로 허용가능한 담체 또는 부형제와 함께 사용되는, 결정형의 화학식 1의 화합물로 이루어지는 약학적 조성물의 제조방법에 관한 것이며, 화학식 1의 화합물은 실질적으로 다른 다형이 없는 A형 다형 결정으로 존재하고, 이 다형의 제조방법도 제공된다. [화학식 1] 다형, 화합물, 결정화, 사방정계결정구조

A kind of preparation method of β-carbonyl thioether

本发明公开了一种β‑羰基硫醚的制备方法。该制备方法以芳环取代的丙炔醇和硫醇为原料，在酸作用下进行串联的Meyer‑Schuster重排反应和1,4‑加成反应，从而实现β‑羰基硫醚的一锅法合成。本发明的制备方法最高产率可达99％，具有操作简单和100％原子经济等优点，为β‑羰基硫醚类化合物的构建提供了一种全新的合成方法。

Processes for preparing 3-Arylsulfur hydroxamic acids

This invention provides processes for the preparation of a compound of Formula I:wherein:Y is hydroxy or XONX, where each X is independently hydrogen, lower alkyl or lower acyl;R1 is hydrogen or lower alkyl;R2 is hydrogen, lower alkyl, aryl, aralkyl, cycloalkyl, cycloalkylalkyl, or R1 and R2 together with the carbon atom to which they are attached form a cycloalkyl or heterocyclo group;R3 is aryl; andn is 0, 1 or 2.The invention also provides novel aryl haloalkyl sulfide intermediates useful for the preparation of compounds of Formula I and novel methods of preparing aryl alkyl sulfides.

Processes for preparing 3-arylsulfur hydroxamic acids

This invention provides processes for the preparation of a compound of Formula I: Y—C(═O)—C(R 1 )(R 2 )—CH 2 —S(O) n R 3 wherein: Y is hydroxy or XONX, where each X is independently hydrogen, lower alkyl or lower acyl; R 1 is hydrogen or lower alkyl; R 2 is hydrogen, lower alkyl, aryl, aralkyl, cycloalkyl, cycloalkylalkyl, or R 1 and R 2 together with the carbon atom to which they are attached form a cycloalkyl or heterocyclo group; R 3 is aryl; and n is 0, 1 or 2. The invention also provides novel aryl haloalkyl sulfide intermediates useful for the preparation of compounds of Formula I and novel methods of preparing aryl alkyl sulfides.

Processes for preparing 3-arylsulfur hydroxamic acids

This invention provides processes for the preparation of a compound of Formula I:wherein:Y is hydroxy or XONX, where each X is independently hydrogen, lower alkyl or lower acyl;R1 is hydrogen or lower alkyl;R2 is hydrogen, lower alkyl, aryl, aralkyl, cycloalkyl, cycloalkylalkyl, or R1 and R2 together with the carbon atom to which they are attached form a cycloalkyl or heterocyclo group;R3 is aryl; andn is 0, 1 or 2.The invention also provides novel aryl haloalkyl sulfide intermediates useful for the preparation of compounds of Formula I and novel methods of preparing aryl alkyl sulfides.

Stabilized elastomer composition, stabilizer, elastomer stabilization process, and a method for preventing decoloration of substrates

FIELD: polymer materials. SUBSTANCE: invention relates to compositions containing (i) elastomer sensitive to oxidative, thermal, dynamic, or light- and/or ozone-induced degradation and (ii), as stabilizer, at least one compound belonging to type of S-substituted 4-(3-mercaptosulfinyl-2-hydroxypropylamino)diphenylamine, as well as to a method for preventing decoloration of substrates coming into contact with elastomers and to a method for stabilizing elastomers consisting in introducing into the latter or coating them with at least one compound belonging to type of S-substituted 4-(3-mercaptosulfinyl-2-hydroxypropylamino)diphenylamine. Composition of stabilized elastomer comprises (a) natural-origin or synthetic elastomer sensitive to degradation as mentioned above and (b) stabilizer, in particular at least one compound having following general formula 1: [R-S(=O) m CH 2 -CH(OH)-CH 2 ] n -N(R 1 ) 2-n -R 2 (1), where R represents C 4 -C 20 -alkyl, hydroxy-substituted C 4 -C 20 -alkyl, phenyl, benzyl, α-methylbenzyl, α,α-dimethykbenzyl, cyclohexyl, or -(CH 2 ) q COOR 3 , and, when m=0, R can be and, when n=1 and R 4 is hydrogen, can also be R 2 -R 1 N-CH 2 -CH(OH)-CH 2 -S(=O) m (CH 2 ) x - or R 2 -R 1 N-CH 2 -CH(OH)-CH 2 -S(=O) m -CH 2 -CH 2 -(O-CH 2 -CH 2 ) y -; R 1 represents hydrogen, cyclohexyl, or C 3 -C 12 -alkyl; R 2 represents group ; R 3 C 1 -C 18 -alkyl; R 4 hydrogen or CH 2 -CH(OH)-CH 2 -S(=O) m -R; X C 1 -C 8 -alkyl; Y C 1 -C 8 -alkyl; m=0 or 1, n=1 or 2, q=1 or q=2-6, and y=1 or 2. Compounds of formula 1 stabilize elastomers, especially low-colored ones, prevent oxidative, thermal, dynamic, or light- and/or ozone-induced degradation thereof, and prevent decoloration of substrates coming into contact with elastomers. EFFECT: enlarged assortment of elastomer-conditioning reagents. 16 cl, 3 tbl, 6 ex ÐÎÑÑÈÉÑÊÀß ÔÅÄÅÐÀÖÈß (19) RU (51) ÌÏÊ 7 (11) 2 261 258 (13) C2 C 08 L 21/00, C 08 K 5/375, 5/41, C 07 C 323/25, 323/11 ÔÅÄÅÐÀËÜÍÀß ÑËÓÆÁÀ ÏÎ ÈÍÒÅËËÅÊÒÓÀËÜÍÎÉ ...

Process for preparing 2-mercaptoethylamine hydrogalogenides and its modification

2-Mercaptoethylamine hydrohalides of the formula …<CHEM>… wherin R1, R2, R3 and R4 are identical or different, and each represents a hydrogen atom, a lower alkyl group, a hydroxy-substituted lower alkyl group or a phenyl group, and X represents a halogen atom.… are produced by reacting …<CHEM>… in the presence of water. The process may proceed via the intermediate …<CHEM>… which is hydrolysed to give compound III.

Phenoxyalkylcarboxylacid acid derivatives and preparation method thereof

具有强的选择性白三烯拮抗作用，可用于预防和 治疗过敏反应性疾病如哮喘的以通式(1)表示的苯氧 基烷基羧酸衍生物及其制备方法。 其中R 1 为氢原子、甲基或乙基。

Application of composition of salviskinone A derivatives to drugs used for preventing and treating renal fibrosis

本发明公开了一种Salviskinone A的苯并咪唑基和二(2‑甲硫基乙基)胺基衍生物的组合物在治疗或预防肾纤维化药物中的应用，本发明涉及有机合成和药物化学领域，具体涉及一种Salviskinone A的苯并咪唑基和二(2‑甲硫基乙基)胺基衍生物的组合物、制备方法及其在制备预防或治疗肾纤维化药物上的用途。本发明公开了一种Salviskinone A的苯并咪唑基和二(2‑甲硫基乙基)胺基衍生物的组合物及其制备方法。药理学实验表明，本发明的组合物具有预防或治疗肾纤维化的作用，具有开发预防或治疗肾纤维化药物的价值。

Method of preparing oxime derivatives or their salts

A hydrazone-based charge transport material, a method of preparing the same and a method of using the same

본 발명은 도전성 기재 및 상기 도전성 기재 상의 광도전 요소를 포함하는 유기감광체로서, 상기 광도전 요소는, The present invention provides an organophotoreceptor comprising a conductive substrate and a photoconductive element on the conductive substrate, wherein the photoconductive element is (a) 하기 화학식 1을 갖는 전하 수송 물질; 및 (a) a charge transport material having Formula 1; And (b) 전하 생성 화합물 (b) charge generating compounds 을 포함하는 개선된 유기감광체에 관한 것이다: An improved organophotoreceptor comprising: <화학식 1> <Formula 1> 상기 화학식 1 중, R 1 및 R 2 는 독립적으로, 알킬기, 알케닐기, 알키닐기, 방향족기 또는 헤테로사이클릭기이고; R 3 및 R 4 는 독립적으로, 수소, 알킬기, 알케닐기, 알키닐기, 방향족기 또는 헤테로사이클릭기이고; X 1 및 X 2 는 독립적으로, 연결기이고; Y 1 및 Y 2 는 독립적으로, 아릴아민기를 포함하고; Z는 연결기이다. 이를 이용한 전자사진 화상형성 장치 및 전자사진 화상형성 방법도 기재되어 있다. In Formula 1, R 1 and R 2 are independently an alkyl group, an alkenyl group, an alkynyl group, an aromatic group or a heterocyclic group; R 3 and R 4 are independently hydrogen, alkyl group, alkenyl group, alkynyl group, aromatic group or heterocyclic group; X 1 and X 2 are independently a linking group; Y 1 and Y 2 independently include an arylamine group; Z is a linking group. An electrophotographic image forming apparatus and an electrophotographic image forming method using the same are also described.

METHOD FOR OBTAINING DICHLORBENZYLTHYOETHYLAMINES

Pharmaceutical lipid nanoparticles

Method

Compounds and methods for use in detecting gabapentin

Compounds and methods for use in detecting gabapentin in a sample suspected of containing gabapentin are disclosed. Gabapentin derivatives are used to produce gabapentin conjugates. A gabapentin-immunogenic carrier conjugate may be used as an immunogen for the preparation of an anti-gabapentin antibody. A gabapentin-detectable label may be used in a signal producing system in gabapentin assays.

Method of monomerisation of recombinant antibody molecules

The present invention provides method of increasing the percentage of monomer in a composition of recombinantly expressed antibody molecules characterised in that the antibody molecule comprises at least one Fv with specificity for an antigen of interest comprising one VH and one VL wherein said VH and VL are connected directly or indirectly via one or more linkers and are stabilised by a disulfide bond therebetween, said method comprises: a) a conversion step of treating the composition with a denaturant selected from urea and/or Guanidine hydrochloride; b) wherein step a) is performed in the presence of a reducing agent or after treatment with a reducing agent.