NOVEL PROCESS

The present invention relates to a process for the preparation of S-[2-[1-(2-ethylbutyl)cyclohexylcarbonylamino]-phenyl]2-methylthiopropionate which is a useful pharmaceutical active compound. 2. A process according to claim 1 , wherein said reaction is carried out with at least 0.10M of said reducing agent.3. A process according to claim 1 , wherein the said reducing agent is selected from the group consisting of: phosphines claim 1 , phosphinites claim 1 , phosphonites and phosphites.4. A process according to claim 1 , which further comprises the oxidation of excess reducing agent with an oxidizing agent.5. A process according to claim 4 , wherein the oxidizing agent is peroxymonosulfate or hydrogen peroxide.6. A process according to claim 1 , wherein the said reducing agent is a phosphine.7. A process according to claim 1 , wherein the said reducing agent is triphenyl phosphine.8. A process according to which further comprises the removal of the phosphine oxide claim 3 , phosphinate claim 3 , phosphonate or phosphate produced in said reaction using water/alcohol extraction from an organic solvent.9. A process according to claim 8 , wherein said reducing agent is a phosphine and the phosphine oxide produced in said reaction is removed using water/alcohol extraction from an organic solvent.10. A process according to which further comprises crystallizing the compound of formula (I) using a solvent-antisolvent process with water as the antisolvent and the solvent being a water-miscible solvent.1110. A process according to wherein the water miscible solvent is acetone claim 1 , ethanol claim 1 , isopropanol claim 1 , propanol or mixtures thereof.12. A process according to which further comprises crystallizing the compound of formula (I) by cooling a solution of said compound of formula (I) in a non-polar solvent.13. A process according to claim 1 , which further comprises the following steps:a) forming a solution of said compound of formula (I) in acetone, ethanol, ...

POLYMERIZABLE COMPOSITIONS CONTAINING (METH)ACRYLATE MONOMERS HAVING SULFIDE LINKAGES

Provided is a polymerizable composition including (meth)acrylate monomers having at least two sulfide (—S—) linkages in the monomer. The polymerizable compositions include a first (meth)acrylate monomer represented by the following Formula (I), 2. The polymerizable composition of wherein claim 1 ,{'sup': '1', 'sub': 1', '25', '3', '12, 'Lis selected from multivalent linear or branched optionally substituted C-Calkyl, multivalent optionally substituted C-Ccycloalkyl, multivalent optionally substituted aryl, and combinations thereof optionally interrupted with at least one of —C(O)—, —S—, —O— and combinations thereof, and'}{'sup': '2', 'sub': 1', '25', '3', '12, 'Lis independently for each n selected from divalent optionally substituted linear or branched C-Calkyl, divalent optionally substituted C-Ccycloalkyl, divalent optionally substituted aryl, and combinations thereof optionally interrupted with at least one of —O— and —S—.'}3. The polymerizable composition of wherein claim 2 ,{'sup': '1', 'sub': 1', '10, 'Lis selected from multivalent linear or branched C-Calkyl optionally interrupted with at least one of —C(O)—, —S—, —O— and combinations thereof, and'}{'sup': '2', 'sub': 1', '10, 'Lis independently for each n selected from divalent linear or branched C-Calkyl optionally interrupted with at least one —O—.'}4. The polymerizable composition of wherein claim 3 ,{'sup': '1', 'sub': 1', '10, 'claim-text': 'n is 2 or 3.', 'Lis selected from multivalent linear or branched C-Calkyl interrupted with at least one —S— group, and'}5. The polymerizable composition of wherein claim 1 ,n is 2, and{'sup': '1', 'Lis represented by the following Formula (B),'} {'br': None, 'sup': 2', '3, 'sub': 'p', '—(R—S)—R—\u2003\u2003(B)'}, 'wherein,'}wherein{'sup': '2', 'sub': 1', '10', '3', '12, 'Rfor each p is independently selected from linear or branched optionally substituted C-Calkyl, and optionally substituted C-Ccycloalkyl,'}{'sup': '3', 'sub': 1', '10', '3', '12, 'Ris selected from ...

Functionalized Polymers Using Protected Thiols

A process for the preparation of functional molecules using the thiol-ene coupling reaction and a process for the preparation of protected functional thiols, specifically thioesters is provided. The methods may be used to make functional polymers and other molecules. The method of making a functionalized polymer using a thiol-ene reaction comprises: providing a functionalized thioester having the following formula: 1. A functionalized thioester made by a method of preparing a functionalized thioester comprising:(a) reacting a nucleophilic starting material having a desired functional group with a nonsymmetrical bifunctional linker molecule, forming a functionalized intermediate; and (b) reacting the functionalized intermediate with a thiol acid to form a functionalized thioester.3. The functionalized thioester of claim 2 , wherein the protecting group is an acetyl or benzoyl group.4. The functionalized thioester of claim 2 , wherein the functional group is selected from the group consisting of: amino acid claim 2 , peptide claim 2 , polypeptide claim 2 , nucleic acid claim 2 , lipid claim 2 , carbohydrate claim 2 , carbazole claim 2 , benzoate claim 2 , phenol claim 2 , pyridine claim 2 , cyanobiphenyl claim 2 , perfluorocarbon claim 2 , polyethylene oxide (PEO) and polypropyleneoxide (PPO) groups This application is a divisional of application Ser. No. 12/961,136, filed Dec. 6, 2010, which is a divisional of application Ser. No. 12/251,708, filed Oct. 15, 2008, which takes priority from U.S. provisional application Ser. No. 60/998,980, filed Oct. 15, 2007, hereby incorporated by reference.Not applicable.This invention relates to functional polymers and functional protected thiol compounds, methods of preparation and use.Functionalization of polymers having pendant vinyl groups using thiol-ene coupling is a powerful and versatile method to prepare well-defined polymeric materials with tailored properties. However, commercially available mercaptans are limited to a ...

NEW PROCESS

A process for the preparation of a compound of formula (I): 2. A process according to claim 1 , wherein the coupling reaction is carried out in the presence of a secondary amine.3. A process according to claim 2 , wherein Ris pent-3-yl.9. A process according to claim 1 , wherein the coupling reaction is followed by a mineral acid quenching with hydrofluoric acid claim 1 , hydrochloric acid claim 1 , boric acid claim 1 , acetic acid claim 1 , formic acid claim 1 , nitric acid claim 1 , phosphoric acid or sulfuric acid.10. A process according to claim 1 , wherein the coupling reaction is followed by a hydrochloric acid quenching.11. A process according to claim 1 , wherein a nonprotic solvent is present.12. A process according to claim 11 , wherein the nonprotic solvent is tetrahydrofuran.13. A process according to claim 11 , wherein the alkylating agent is 1-halo-CHRor a sulfonate ester of RCH—OH wherein Ris defined in .14. A process according to claim 1 , wherein the alkylating agent is 1-halo-2-ethylbutane.15. A process according to claim 1 , wherein the alkylating agent is 2-ethyl-1-butanol.16. A process according to claim 1 , wherein the alkylating agent is 1-bromo-2-ethylbutane.17. A process according to claim 1 , wherein the Grignard reagent is a (C-C)alkyl-magnesium-halide claim 1 , phenyl-magnesium-halide claim 1 , heteroaryl-magnesium-halide or a (C-C)cycloakyl-magnesium-halide.18. A process according to claim 1 , wherein the Grignard reagent is methylmagnesiumchloride.19. A process according to claim 2 , wherein the secondary amine is diethylamine or diisopropylamine.20. A process according to claim 2 , wherein the secondary amine is diethylamine.21. A process according to claim 2 , wherein the secondary amine is in a catalytic amount.22. A process according to claim 2 , wherein 0.01 to 0.5 equivalents of the secondary amine is used.23. A process according to claim 2 , wherein the process is continuous.24. A process according to claim 8 , wherein the ...

DENDRIMERS AND METHODS OF PREPARING SAME THROUGH PROPORTIONATE BRANCHING

The present invention provides for monodispersed dendrimers having a core, branches and periphery ends, wherein the number of branches increases exponentially from the core to the periphery end and the length of the branches increases exponentially from the periphery end to the core, thereby providing for attachment of chemical species at the periphery ends without exhibiting steric hindrance. 1. A dendrimer comprising a generation (G) branching structure comprising a core , branches and periphery ends , wherein length of the branches increases exponentially from the periphery ends to the core and the number of branches increases exponentially from the core to the periphery ends.2. The dendrimer according to claim 1 , wherein the number of branches in a nth layer is defined as mand the number of bonds between the nth layer and n−1 layer is defined as lwherein n is defined as a value of 1≦n≦G claim 1 , wherein the increasing number of mfrom the core to the periphery is defined by the formula m=a×mand the increasing number of lfrom the periphery to the core is defined by the formula l=b×l claim 1 , wherein a is the branch multiplicity for growing the number of branches and b is the branch length multiplier for growth of the length of the branches and wherein the length multiplier b satisfies 1≦b≦a.3. The dendrimer according to claim 2 , wherein a has an integer value and b has an integer or non-integer value.4. The dendrimer according to claim 3 , wherein the value of a and b remain constant.6. The dendrimer according to claim 5 , wherein the proportionality constant is greater than 2%.7. The dendrimer according to claim 2 , wherein lis an integer.8. The dendrimer according to claim 2 , wherein the value of lfloats between [bl−1 claim 2 , bl+1] and is an integer.9. The dendrimer according to claim 2 , where the branch multiplicity a has a value of 2 claim 2 , 3 claim 2 , 4 or 5.10. The dendrimer according to claim 2 , wherein the branch length multiplier b has a non- ...

Preparation of methionine or selenomethionine from homoserine via a carbamate intermediate

Provided herein are processes for the production of methionine or selenomethionine from homoserine. In particular, the processes proceed via the production of carbamate intermediates.

COMPOUND, COMPOSITION AND USES THEREOF

The disclosure herein provides the compounds of Formulas 1 and its pharmaceutical acceptable salts, as well as polymorphs, solvates, and hydrates thereof. These salts may be formulated as pharmaceutical compositions. The pharmaceutical compositions may be formulated for oral administration, transdermal administration, and/or injection. Such compositions may be used for the treatment of metabolic conditions, cystinosis, non-alcoholic Steatohepatitis, hypertriglyceridemia, and/or neurodegenerative disorders, and/or their associated complications. 2. The method of claim 1 , further comprising administering the compound of comprising Formula 1 through at least one of a non-invasive peroral claim 1 , a topical ointment claim 1 , an enteral claim 1 , a gel solution claim 1 , a syrup claim 1 , a lotion claim 1 , a healing pad claim 1 , a transmucosal delivery claim 1 , a targeted delivery claim 1 , a sustained release delivery claim 1 , a delayed release delivery claim 1 , a pulsed release delivery claim 1 , a patch claim 1 , and a parenteral delivery.3. The method of claim 2 , wherein the method treats at least one of a hypertriglyceridemia disorder claim 2 , a stroke claim 2 , an atrial fibrillation claim 2 , a coronary heart disease claim 2 , a non-alcoholic Steatohepatitis claim 2 , cystinosis claim 2 , nephropathic cystinosis claim 2 , and Huntington's disease. This application is a continuation application claiming priority to co-pending U.S. non-provisional patent application Ser. No. 13/649,094 titled COMPOUND, COMPOSITION AND USES THEREOF filed on Oct. 10, 2012, which claimed priority to Ser. No. 13/152,864, filed on Jun. 3, 2011, India Provisional Patent Application No. 3947/CHE/2012, filed on Sep. 24, 2012 and is the national phase application of PCT application No. PCT/IN/2012/000668 filed on Oct. 9, 2012. These applications are hereby incorporated by reference in all of their entireties for all of their teachings.This disclosure generally relates to compounds ...

TRANS-2-DECENOIC ACID DERIVATIVE AND PHARMACEUTICAL AGENT CONTAINING THE SAME

An object of the present invention is to provide a novel trans-2-decenoic acid derivative or a pharmaceutically acceptable salt thereof and to provide a pharmaceutical agent which contains said compound as an active ingredient and has a highly safe neurotrophic factor-like activity or an alleviating action for side effect induced by administration of anti-cancer agents. The trans-2-decenoic acid derivative or a pharmaceutically acceptable salt thereof which is the compound of the present invention is specifically represented by the formula (1): 2. The trans-2-decenoic acid derivative or a pharmaceutically acceptable salt thereof according to claim 1 , wherein Y′ is —O— and W1′ is dialkylaminoalkyl group claim 1 , alkylthioalkyl group claim 1 , alkoxyalkyl group claim 1 , dialkoxyalkyl group or dialkylaminoalkoxyalkyl group.3. The trans-2-decenoic acid derivative or a pharmaceutically acceptable salt thereof according to claim 1 , wherein Y′ is —NR′—.4. The trans-2-decenoic acid derivative or a pharmaceutically acceptable salt thereof according to claim 3 , wherein R′ is dialkylaminoalkyl group and W2′ is hydrogen atom claim 3 , alkyl group or dialkylaminoalkyl group.5. The trans-2-decenoic acid derivative or a pharmaceutically acceptable salt thereof according to claim 3 , wherein R′ is alkyl group and W2′ is alkyl group which is same as or different from R′ (except the case where both R′ and W2′ are ethyl group).6. The trans-2-decenoic acid derivative or a pharmaceutically acceptable salt thereof according to claim 3 , wherein R′ is hydrogen atom and W2′ is alkyl group (except 2-methylpropyl group and 2-methylbutyl group) claim 3 , cyclohexyl group or pyrrolidinealkyl group.7. The trans-2-decenoic acid derivative or a pharmaceutically acceptable salt thereof according to claim 1 , wherein Y′ is —S— and W3′ is alkyl group claim 1 , cycloalkyl group claim 1 , phenylalkyl group or dialkylaminoalkyl group.9. The pharmaceutical agent according to claim 8 , wherein Y is ...

CONTROLLED CHEMICAL RELEASE OF HYDROGEN SULFIDE

Agents of formula: where R1 and R2 vary independently and are acyl, sulfonyl, phosphoryl, alkyl, substituted alkyl, halogen, aryl, arylalkyl, substituted aryl, heteroaryl, alkenyl, substituted alkenyl, alkynyl, substituted alkynyl, cycloalkyl, heterocycle, or heteroatoms; and R3 is H or a member of a ring structure which includes R2, are provided; as are agents of formula: where R1, R2 and R3 vary independently and: R1=OH, OR′, NHR′, NR′R″ (with R′ R″=alkyl, aryl, heteroaryl, etc); R=acyl, alkyl, aryl, sulfonyl, etc; R3=alkyl, aryl, substituted aryl, heteroaryl, etc; and R4 and R5 are (independently) H, methyl or alkyl, substituted alkyl, aryl, substituted aryl, etc. Methods of using the agents to treat e.g. cardiovascular disease, stroke, shock, injuries caused by hypoxia, male erectile dysfunction, and Alzheimer's are provided. 3. The agent of claim 1 , wherein R3 is a member of a ring structure which includes R2 claim 1 , andR1 and R2 are independently varied and are acyl, sulfonyl, phosphoryl, alkyl, substituted alkyl, halogen, aryl, substituted aryl, heteroaryl, alkenyl, substituted alkenyl, alkynyl, substituted alkynyl, cycloalkyl, heterocyclic, or are heteroatoms6. The method of claim 4 , wherein R3 is a member of a ring structure which includes R2 claim 4 , andR1 and R2 are independently varied and are acyl, sulfonyl, phosphoryl, alkyl, substituted alkyl, halogen, aryl, substituted aryl, heteroaryl, alkenyl, substituted alkenyl, alkynyl, substituted alkynyl, cycloalkyl, heterocyclic, or are heteroatoms.7. The method of claim 4 , wherein said patient is suffering from a disease or condition selected from the group consisting of: cardiovascular disease claim 4 , Alzheimer's claim 4 , and male erectile dysfunction.14. The method of claim 11 , wherein said patient is suffering from a disease or condition selected from the group consisting of: cardiovascular disease claim 11 , Alzheimer's claim 11 , and male erectile dysfunction. The invention generally relates ...

1,3-OXATHIOLANE DERIVATIVES, PROCESS FOR THE PREPARATION OF 1,3-OXATHIOLANE DERIVATIVES AND INTERMEDIATES THEREOF

This invention relates to 1,3-oxathiolane derivatives (I), processes for the preparation of 1,3-oxathiolane derivatives and intermediate compounds thereof. 5. The process of claim 1 , wherein the first acid is an organic sulfonic acid claim 1 , trifluoroacetic acid claim 1 , a phosphorous oxyacid claim 1 , sulfuric acid or a Lewis acid.6. The process of claim 4 , wherein the first acid is an organic sulfonic acid or trifluoroacetic acid.7. The process of claim 1 , wherein the first solvent is an aromatic hydrocarbon or an alcohol.9. The process of wherein the compound of Formula VII is not isolated.18. The process of claim 14 , wherein the compound of Formula IV is acetyl thioethoxyethylacetal.19. The process of claim 14 , wherein the compound of Formula IV is acetyl thiobutoxyethylacetal.20. The process of claim 14 , wherein the epoxidation is conducted in the presence of a sulfur ylide.21. The process of claim 14 , wherein the epoxidation is conducted in the predence of trimethylsulfoxonium iodide and dimethylsulfoxide.23. The process of wherein the second acid is an organic sulfonic acid or a Lewis acid.24. The process of wherein the Lewis acid is SnCl claim 23 , TiCl claim 23 , BF claim 23 , or OEt.25. The process of wherein the second acid is p-toluenesulfonic acid claim 22 , pyridinium toluenesulfonic acid or camphorsulfonic acid.26. The process of wherein the compound of Formula II is thioacetic acid claim 22 , and the compound of Formula III is ethyl vinyl ether.27. The process of wherein the compound of Formula II is thioacetic acid claim 22 , and the compound of Formula III is butyl vinyl ether.30. The compound of in acid addition salt form.31. The compound of wherein the acid addition salt is benzoic acid salt.33. The compound of in acid addition salt form. The invention relates to an improved process for the preparation of 1,3-oxathiolane derivatives and intermediates thereof.The 1,3-oxathiolane ring is a common feature of many useful compounds, ...

CYCLOALKYL GUANIDINE F1F0-ATPASE INHIBITORS AND THERAPEUTIC USES THEREOF

The invention provides cycloalkyl guanidine compounds that inhibit FF-ATPase, and methods of using cyclalkyl guanidine compounds as therapeutic agents in therapy, such as treating an immune disorder, inflammatory condition, or cancer. 2. The compound of claim 1 , wherein A is cycloalkylene claim 1 , that in addition to R claim 1 , is optionally substituted with 1 or 2 substituents independently selected from the group consisting of halogen claim 1 , alkyl claim 1 , haloalkyl claim 1 , cycloalkyl claim 1 , —N(R)COR claim 1 , —N(R)C(O)R claim 1 , —N(R)(R) claim 1 , —OR claim 1 , and —C(O)R.3. (canceled)4. The compound of claim 1 , wherein A is cyclobutylene claim 1 , cyclopentylene claim 1 , or cyclohexylene claim 1 , each of which is claim 1 , in addition to R claim 1 , optionally substituted with 1 or 2 substituents independently selected from the group consisting of halogen claim 1 , alkyl claim 1 , haloalkyl claim 1 , hydroxyl claim 1 , and —N(R)(R).5. The compound of claim 1 , wherein A is cyclohexylene.6. The compound of claim 1 , wherein Rrepresents independently for each occurrence halogen claim 1 , haloalkyl claim 1 , alkyl claim 1 , or C-Calkoxy.7. The compound of claim 1 , wherein Rrepresents independently for each occurrence chloro claim 1 , fluoro claim 1 , or trifluoromethyl.8. The compound of claim 1 , wherein Ris hydrogen.9. (canceled)10. The compound of claim 1 , wherein Ris —N(R)COR claim 1 , —N(R)C(O)R claim 1 , —N(R)C(O)N(R)(R) claim 1 , —N(R)SOR claim 1 , or —N(R)(R).11. The compound of claim 1 , wherein Ris —N(R)COR.12. The compound of claim 1 , wherein Ris —N(R)C(O)R.1316-. (canceled)17. The compound of claim 1 , wherein Ris aryl or aralkyl claim 1 , each of which is optionally substituted with 1 claim 1 , 2 claim 1 , or 3 substituents independently selected from the group consisting of halogen claim 1 , haloalkyl claim 1 , alkyl claim 1 , cycloalkyl claim 1 , and C-Calkoxy.18. The compound of claim 1 , wherein Ris phenyl optionally substituted ...

Thioamide Compound, Method for Producing Thioamide Compound, Method for Producing [(4R,6R)-6-Aminoethyl-1,3-Dioxan-4-YL]Acetate Derivative, and Method for Producing Atorvastatin

A thioamide compound represented by the following general formula (1); 3. The method for producing the thioamide compound according to claim 2 , wherein the reacting is carried out with a copper complex.4. The method for producing the thioamide compound according to claim 3 , wherein the copper complex is a copper-optically active phosphine complex. This application is a continuation application of International Application PCT/JP2012/053323 filed on Feb. 14, 2012 and designated the U.S., the entire contents of which are incorporated herein by reference.1. Field of the InventionThe present invention relates to a thioamide compound useful for the synthesis of atorvastatin, a method for producing the thioamide compound, a method for producing a [(4R,6R)-6-aminoethyl-1,3-dioxan-4-yl]acetate derivative using the thioamide compound, and a method for producing atorvastatin using the thioamide compound.2. Description of the Related ArtConversion of 3-hydroxy-3-methylglutaryl-coenzyme A (HMG-CoA) into mevalonate is a rate-determining step in the initial stage of the cholesterol biosynthetic pathway. This step is catalyzed by the enzyme HMG-CoA reductase. Statins inhibit the catalytic action of HMG-CoA reductase on this conversion. In light of this, on the whole, statins are potent lipid lowering substances.Currently, atorvastatin calcium hydrate is commercially available as Lipitor (R), which has the following formula (see, for example, U.S. Pat. No. 5,273,995).Atorvastatin calcium is a selective, competitive HMG-CoA inhibitor. In light of this, atorvastatin is a potent lipid lowering substance, and therefore, is useful as a lipid lowering agent and/or cholesterol lowering agent. Further, atorvastatin is also useful for the treatment of osteoporosis, benign prostatic hyperplasia (BPH), and Alzheimer's disease.As a method for synthesizing atorvastatin calcium, a synthesis method shown in is known (see, for example, Roth B. D., et al., Progress in Medicinal Chemistry, 2002, ...

NOVEL PROCESS

The present invention relates to a process for the preparation of S-[2-[1-(2-ethylbutyl)cyclohexylcarbonylamino]-phenyl] 2-methylthiopropionate which is a useful pharmaceutical active compound. 2. A process according to claim 1 , wherein said reaction is carried out with at least 0.10 M of said reducing agent.3. A process according to claim 1 , wherein the said reducing agent is selected from the group consisting of: phosphines claim 1 , phosphinites claim 1 , phosphonites and phosphites.4. A process according to claim 1 , which further comprises the oxidation of excess reducing agent with an oxidizing agent.5. A process according to claim 4 , wherein the oxidizing agent is peroxymonosulfate or hydrogen peroxide.6. A process according to claim 1 , wherein the said reducing agent is a phosphine.7. A process according to claim 1 , wherein the said reducing agent is triphenyl phosphine.8. A process according to which further comprises the removal of the phosphine oxide claim 3 , phosphinate claim 3 , phosphonate or phosphate produced in said reaction using water/alcohol extraction from an organic solvent.9. A process according to claim 8 , wherein said reducing agent is a phosphine and the phosphine oxide produced in said reaction is removed using water/alcohol extraction from an organic solvent.10. A process according to which further comprises crystallizing the compound of formula (I) using a solvent-antisolvent process with water as the antisolvent and the solvent being a water-miscible solvent.11. A process according to 10 wherein the water miscible solvent is acetone claim 1 , ethanol claim 1 , isopropanol claim 1 , propanol or mixtures thereof.12. A process according to which further comprises crystallizing the compound of formula (I) by cooling a solution of said compound of formula (I) in a non-polar solvent.13. A process according to claim 1 , which further comprises the following steps:a) forming a solution of said compound of formula (I) in acetone, ethanol, ...

Process for producing thiophene compound and intermediate thereof

To provide a novel process for producing a 2-aryl-3-hydroxy-4-substituted carbonyl thiophene compound or an intermediate thereof useful as an intermediate for production of medicines and agricultural chemicals. A 2-aryl acetate compound represented by the formula (1): wherein R 1 is an aryl group or the like, R 4 is a C 1-3 alkyl group or the like, and X is a leaving group, is reacted with a thioacetic acid compound to form a thioacetyl compound (3), the thioacetyl compound (3) is reacted with a vinyl ketone compound to form a γ-ketosulfide compound (5), which is cyclized under basic conditions to form a dihydrothiophene compound (6), and the dihydrothiophene compound (6) is oxidized by using an oxidizing agent to produce a 2-aryl-3-hydroxy-4-substituted carbonyl thiophene compound (7).

Derivatives of tetracaine

Disclosed herein are derivatives of tetracaine that, among other things, block cyclic nucleotide gated (CNG) channels and are useful in the treatment of diseases characterized by overactive CNG channels such as retinal degeneration diseases.

THIOAMIDE-CONTAINING COMPOSITIONS AND METHODS OF USE THEREOF

Provided herein are compositions and methods for preparing albumin-targeting moieties that feature a thioamide linkage. Methods to use the albumin targeting molecules to generate drugs with improved in vivo pharmacodynamics and biodistribution are described. Therapeutic compounds incorporating these thioamide linked albumin-targeting moieties are disclosed. 2) The compound of claim 1 , wherein n is 2 or 3.4) The compound of claim 3 , wherein n is 3.6) The compound of claim 3 , wherein Lis Z claim 3 , and wherein:{'sub': 1', '12, 'Z is C-Calkyl, wherein any of the methylene groups in the alkyl group may be replaced with NH or carbonyl.'}9) The compound of claim 1 , wherein Lis —N(R)—C-Calkyl-C(O)—.11) The compound of claim 1 , wherein Lis —N(R)—C-Calkylcycloalkyl-C(O)—C-Calkylaryl-C(O)—.13) The compound of claim 1 , wherein Lis —N(R)—C-Calkylaryl-C(O)NH—C-Calkylaryl-C(O)NH—CH(COH)—C-Calkyl-NHC(O)—C-Calkyl-C(O)— claim 1 , wherein C-Calkylaryl is optionally substituted with halo or hydroxyl.17) The compound of claim 16 , wherein n is 3.22) The compound of claim 1 , wherein n is 2 or 3. This application claims the benefit of priority to U.S. Provisional Patent Application No. 62/767,151, filed Nov. 14, 2018. The contents of this related application is hereby incorporated by reference in its entirety.The invention relates generally to modified drugs and more particularly to thioamide-modified drugs.Several strategies are currently used to extend the serum lifetime of therapeutic drugs, including alteration of peptide sequence in peptide or polypeptide drugs and secondary structure to minimize protease activity. Another approach for extending biomolecule half-life is PEGylation. Yet another approach is to introduce albumin-targeting moieties on to drugs.This disclosure provides thioamide-modified amino acids useful as albumin-targeting moieties. These compounds offer tunable (and different) albumin binding and increased in vivo stability compared to the corresponding ...

DISULFIDE COMPOUNDS FOR DELIVERY OF PHARMACEUTICAL AGENTS

A compound of formula the following formula: (I). In this formula, moieties A, B, X, R, R, and Rare defined herein. Also disclosed are a nanocomplex that is formed of such a compound and a pharmaceutical agent, and a nanocomplex that is formed of a protein and a bioreducible compound. 7. The compound of claim 1 , wherein Ris a C-Cbivalent aliphatic radical or a C-Cbivalent heteroaliphatic radical; and the total carbon number of Rand Ris 14-18.11. A pharmaceutical composition comprising a pharmaceutically acceptable carrier and a nanocomplex formed of a compound of and a pharmaceutical agent claim 1 , wherein the nanocomplex has a particle size of 50 nm to 1000 nm; the compound binds to the pharmaceutical agent via a non-covalent interaction claim 1 , a covalent bond claim 1 , or both; and the pharmaceutical agent is a small molecule claim 1 , a protein claim 1 , a peptide claim 1 , a nucleic acid claim 1 , or a combination thereof.17. The pharmaceutical composition of claim 11 , wherein Ris a C-Cbivalent aliphatic radical or a C-Cbivalent heteroaliphatic radical; the total carbon number of Rand Ris 14-18.21. A pharmaceutical composition comprising a nanocomplex claim 11 , the nanocomplex formed of a protein and a bioreducible compound claim 11 , wherein the nanocomplex has a particle size of 50 nm to 1000 nm; the protein binds to the bioreducible compound via a non-covalent interaction claim 11 , a covalent bond claim 11 , or both; and the bioreducible compound contains a disulfide hydrophobic moiety claim 11 , a hydrophilic moiety claim 11 , and a linker joining the disulfide hydrophobic moiety and the hydrophilic moiety.24. The pharmaceutical composition of claim 23 , wherein each of X and Y is C-Calkylene. This application claims priority to U.S. Provisional Application No. 61/770,657, filed on Feb. 28, 2013, the contents of which are hereby incorporated by reference.To achieve therapeutic effect, a drug must be delivered to its target site. It is a challenge to ...

NOVEL HETERO-DIELS-ALDER CROSS-LINKER AND USE THEREOF IN REVERSIBLY CROSSLINKED POLYMER SYSTEMS

The invention relates to a novel hetero-Diels-Alder crosslinker, to a process for the production thereof and to the use thereof for reversibly crosslinking polymer systems. 2. The formulation according to claim 1 , wherein:at least one of the components A or B comprises more than two functionalities;at least one of the components A or B is present in the form of a polymer, andthe formulation is crosslinkable at room temperature, and the crosslinking is reversible to an extent of at least 50% at a higher temperature.3. The formulation according to claim 1 , wherein:{'sub': '1', 'the component A is a compound having a plurality of the structural unit (Z) and these are bonded to one another with alkylene groups Rhaving between 1 and 5 carbon atoms; and'}{'sub': '2', 'Rhas between 2 and 10 carbon atoms.'}5. The formulation according to claim 1 , wherein the component B is a polymer.6. The formulation according to claim 5 , wherein the polymer is selected from the group consisting of polyacrylates claim 5 , polymethacrylates claim 5 , polystyrenes claim 5 , mixed polymers made of acrylates claim 5 , methacrylates and/or styrenes claim 5 , polyacrylonitrile claim 5 , polyethers claim 5 , polyesters claim 5 , polylactic acids claim 5 , polyamides claim 5 , polyesteramides claim 5 , polyurethanes claim 5 , polycarbonates claim 5 , amorphous or semicrystalline poly-α-olefins claim 5 , EPDM claim 5 , EPM claim 5 , hydrogenated or non-hydrogenated polybutadienes claim 5 , ABS claim 5 , SBR claim 5 , polysiloxanes and block claim 5 , comb and/or star copolymers of these polymers.9. The formulation according to claim 1 , wherein the component B is a polyamide claim 1 , a polyester or a polycarbonate having at least one diene functionality.10. The formulation according to claim 1 , wherein the component A has one of the structural unit (Z) claim 1 , and the component B has one diene group.11. A process for reversible crosslinking claim 1 , the process comprising crosslinking the ...

METHOD FOR PRODUCING ORGANIC MERCAPTO COMPOUND OR INTERMEDIATE THEREOF, (POLY)THIOL COMPONENT, POLYMERIZABLE COMPOSITION FOR OPTICAL MATERIAL, MOLDED PRODUCT, OPTICAL MATERIAL, AND LENS

A method for producing an organic mercapto compound or an intermediate thereof according to the present invention has a reaction step of reacting an alcohol compound including a sulfur atom with a thioamide compound having a structure in which an organic group is bonded to at least one bonding hand of a thioamide group, under acidic conditions. 1. A method for producing an organic mercapto compound or an intermediate thereof , comprising:a reaction step of reacting an alcohol compound including a sulfur atom with a thioamide compound having a structure in which an organic group is bonded to at least one bonding hand of a thioamide group, under acidic conditions.2. The method for producing an organic mercapto compound or an intermediate thereof according to claim 1 ,{'sup': '2', 'wherein a topological polar surface area of the thioamide compound is 10.00 to 51.00 Å.'}4. The method for producing an organic mercapto compound or an intermediate thereof according to claim 3 ,{'sup': '1', 'wherein, in the compound represented by General Formula (2), Ris a monovalent aryl group having 6 to 10 carbon atoms, which optionally be substituted, a monovalent aliphatic group having 1 to 10 carbon atoms, which optionally be substituted, or a monovalent heteroaryl group having 3 to 10 carbon atoms, which optionally be substituted, and substituents of these groups optionally include a hetero atom, and'}{'sup': 2', '3', '2', '3, 'Rand Rare hydrogen atoms or Rand Rare bonded to each other to form a nitrogen-containing heterocyclic ring having 3 to 10 carbon atoms.'}5. The method for producing an organic mercapto compound or an intermediate thereof according to claim 1 , {'br': None, 'sup': '1', 'sub': 'n', 'Q\ue8a0OH\u2003\u2003(1)'}, 'wherein the alcohol compound is represented by General Formula (1),'}{'sup': '1', 'wherein in Formula (1), Qis an n-valent organic group including a sulfur atom and having 1 to 30 carbon atoms, and n is an integer of 1 to 10.'}7. The method for producing ...

PESTICIDAL COMPOSITIONS AND PROCESSES RELATED THERETO

This document discloses molecules having the following formula (“Formula One”): 2. A molecule according to wherein R1 is selected from H claim 1 , F claim 1 , Cl claim 1 , Br claim 1 , I claim 1 , CN claim 1 , NO claim 1 , methyl claim 1 , ethyl claim 1 , (C)alkyl claim 1 , (C)alkyl claim 1 , (C)alkyl claim 1 , (C)alkyl claim 1 , (C)alkyl claim 1 , (C)alkyl claim 1 , halomethyl claim 1 , haloethyl claim 1 , halo(C)alkyl claim 1 , halo(C)alkyl claim 1 , halo(C)alkyl claim 1 , halo(C)alkyl claim 1 , halo(C)alkyl claim 1 , halo(C)alkyl claim 1 , methoxy claim 1 , ethoxy claim 1 , (C)alkoxy claim 1 , (C)alkoxy claim 1 , (C)alkoxy claim 1 , (C)alkoxy claim 1 , (C)alkoxy claim 1 , (C)alkoxy claim 1 , halomethoxy claim 1 , haloethoxy claim 1 , halo(C)alkoxy claim 1 , halo(C)alkoxy claim 1 , halo(C)alkoxy claim 1 , halo(C)alkoxy claim 1 , halo(C)alkoxy claim 1 , and halo(C)alkoxy.3. A molecule according to wherein R2 is selected from H claim 1 , F claim 1 , Cl claim 1 , Br claim 1 , I claim 1 , CN claim 1 , NO claim 1 , methyl claim 1 , ethyl claim 1 , (C)alkyl claim 1 , (C)alkyl claim 1 , (C)alkyl claim 1 , (C)alkyl claim 1 , (C)alkyl claim 1 , (C)alkyl claim 1 , halomethyl claim 1 , haloethyl claim 1 , halo(C)alkyl claim 1 , halo(C)alkyl claim 1 , halo(C)alkyl claim 1 , halo(C)alkyl claim 1 , halo(C)alkyl claim 1 , halo(C)alkyl claim 1 , methoxy claim 1 , ethoxy claim 1 , (C)alkoxy claim 1 , (C)alkoxy claim 1 , (C)alkoxy claim 1 , (C)alkoxy claim 1 , (C)alkoxy claim 1 , (C)alkoxy claim 1 , halomethoxy claim 1 , haloethoxy claim 1 , halo(C)alkoxy claim 1 , halo(C)alkoxy claim 1 , halo(C)alkoxy claim 1 , halo(C)alkoxy claim 1 , halo(C)alkoxy claim 1 , and halo(C)alkoxy.4. A molecule according to wherein R3 is selected from H claim 1 , F claim 1 , Cl claim 1 , Br claim 1 , I claim 1 , CN claim 1 , NO claim 1 , methyl claim 1 , ethyl claim 1 , (C)alkyl claim 1 , (C)alkyl claim 1 , (C)alkyl claim 1 , (C)alkyl claim 1 , (C)alkyl claim 1 , (C)alkyl claim 1 , halomethyl claim 1 , ...

Retinoic acid receptor antagonists as chaperone-mediated authophagy modulators and uses thereof

Compounds, compositions and methods are provided for selectively activating chaperone-mediated autophagy (CMA), protecting cells from oxidative stress, proteotoxicity and lipotoxicity, and/or antagonizing activity of retinoic acid receptor alpha (RARα) in subjects in need thereof.

PHOTOACID GENERATOR COMPOUND, POLYMER COMPRISING END GROUPS CONTAINING THE PHOTOACID GENERATOR COMPOUND, AND METHOD OF MAKING

A compound has formula (I): 2. The compound of claim 1 , wherein{'sub': 1-20', '3-20', '6-20', '7-20, 'Z is a Calkyl, Ccycloalkyl, Caryl, or Caralkyl,'}y is an integer from 1 to 4,{'sup': '1', 'sub': 1-20', '3-20', '6-20', '7-20', '6-10', '2-10, 'Ais a Calkylene, Ccycloalkylene, Carylene, or Caralkylene substituted alpha to the point of attachment with sulfur with a CN, Caryl, or a Cester-containing organic group,'}{'sup': '2', 'sub': 1-20', '3-20', '6-20', '7-20, 'Ais fluorinated or non-fluorinated, and is Calkylene, Ccycloalkylene, Carylene, or Caralkylene,'}{'sup': '−', 'Q is sulfonate, sulfate, sulfonamide anion, or sulfonimide anion group, and'}G is an alkali metal cation, ammonium cation, alkylammonium cation, alkyl-aromatic ammonium cation, sulfonium cation, iodonium cation, phosphonium cation, or a carbonium cation.9. A polymer comprising end groups derived from the reaction product of the compound of claim 1 , an unsaturated monomer claim 1 , and optionally claim 1 , an initiator. Design rules for advanced generation microlithography (i.e., such as e-beam, X-ray, and extreme ultraviolet (EUV) lithography operating at a wavelength of 13.4 nm) are trending toward ever smaller dimensions of, for example, 30 nm and below. The narrower linewidths and thinner resist films used in advanced generation lithography can give rise to consistency issues such as line width roughness (LWR), where resolution takes on increasing significance and limits the performance and usefulness of photoresists. Excessive LWR can lead to poor etch and lack of linewidth control in, for example, transistor and gate architecture, potentially causing short circuits and signal delay in the final devices.Uneven distribution of photoacid generators (PAGs) for catalyzing deprotection of protected developable groups in photoresist films may contribute to increased LWR and hence poor resolution. PAGs may be incorporated into photoresist formulations by preparing a physical blend of the PAG and a ...

PROCESS FOR PREPARING AMINOTHIOL ESTER COMPOUNDS AND SALTS THEREOF

A process for preparing aminothiol ester compounds and salts thereof. The present invention relates to a process for preparing compounds of formula (I), (I) comprising the following steps: a) reacting a compound of formula (II) with an inorganic acid or an organic acid, (II) b) reacting the compound obtained in step a) with a base; c) reacting the compound obtained in step b) with CO; d) reacting the compound obtained in step c) with an alkyl chloroformate, a reagent capable of forming, with the compound obtained in step c), an acid halide, or a reagent capable of forming, with the compound obtained in step c), a mixed anhydride; e) reacting the compound obtained in step d) with an SMe anion precursor compound. 2. Method according to claim 1 , wherein the compound of formula (II) is obtained by a step a1) of reaction of 3-chloro-3-methylbut-1-yne with XXNH in an aqueous medium.3. Method according to claim 2 , wherein the compound obtained in step a1) is purified by one or more filtrations.4. Method according to claim 2 , wherein the 3-chloro-3-methylbut-1-yne is obtained by a step a0) of reaction of 2-methylbut-3-yn-2-ol with hydrochloric acid in the presence of a copper catalyst.5. Method according to claim 1 , wherein the acid is an inorganic acid selected from the group consisting of hydrochloric acid claim 1 , phosphoric acid claim 1 , nitric acid claim 1 , and sulfuric acid.6. Method according to claim 1 , wherein the base of step b) has a pKa greater than 25.7. Method according to claim 1 , wherein step d) is implemented with:an alkyl chloroformate having a 1-6 carbon alkyl, which may comprise at least one double bond; ora reagent capable of forming with the compound obtained in stage c) a mixed anhydride chosen from acid chlorides; or{'sub': 2', '2', '3', '5', '3', '3', '2, 'a reagent capable of forming with the compound obtained in stage c) an acid halide selected from the group consisting of SOCl, COCl, PCl, PCl, PBrand PPhBr.'}8. Method according to claim ...

RETINOIC ACID RECEPTOR ANTAGONISTS AS CHAPERONE-MEDIATED AUTOPHAGY MODULATORS AND USES THEREOF

Compounds, compositions and methods are provided for selectively activating chaperone-mediated autophagy (CMA), protecting cells from oxidative stress, proteotoxicity and lipotoxicity, and/or antagonizing activity of retinoic acid receptor alpha (RARα) in subjects in need thereof. 2. The compound of claim 1 , wherein the halogen is Br claim 1 , Cl claim 1 , F or I.3. The compound of claim 1 , wherein the alkyl is C1-C3 alkyl.426-. (canceled)30. The compound or salt of claim 27 , wherein the any one or more halogen is Br claim 27 , Cl claim 27 , F claim 27 , or I independently of any other halogen.31. The compound or salt of claim 27 , wherein any one or more alkyl is a C-Calkyl independently of any other alkyl.32. The compound or salt of claim 27 , wherein any one or more aralkyl is C-Calkyl independently of any other aralkyl. This application is a continuation of U.S. patent application Ser. No. 15/298,280, filed Oct. 20, 2016, which is a divisional of U.S. patent application Ser. No. 14/566,762, filed Dec. 11, 2014, now U.S. Pat. No. 9,512,092 B2, issued Dec. 6, 2016, which claims the benefit of U.S. Provisional Patent Application No. 61/915,063, filed Dec. 12, 2013, the contents of which are incorporated herein by reference in their entirety.This invention was made with government support under grant numbers AG021904, AG031782, HL095929 and AA020630 awarded by the National Institutes of Health. The government has certain rights in the invention.The present invention relates to retinoic acid receptor antagonists as chaperone-mediated autophagy (CMA) modulators and uses thereof for treatment of diseases and disorders such as neurodegenerative diseases and diabetes and other diseases that could benefit by protecting cells from oxidative stress, proteotoxicity, and lipotoxicity.Throughout this application various publications are referred to in superscripts. Citations for these references may be found at the end of the specification immediately preceding the claims. ...

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. 1. A 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 comprising one VH and one VL and having specificity for an antigen of interest 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.2. The method according to claim 1 , wherein the reducing agent is selected from the group consisting of: glutathione (GSH) claim 1 , ethylsulfite claim 1 , 2-mercaptoethanol (BME) claim 1 , 2-mercaptoethylamine (BMEA) claim 1 , cysteine-HCl and dithiothreitol (DTT).3. The method according to claim 2 , wherein the reducing agent is selected from 2-mercaptoethanol (BME) and 2-mercaptoethylamine (BMEA).4. The method according to claim 3 , wherein the 2-mercaptoethylamine is 10 to 150 millimolar; 50 to 150 millimolar; or 95 to 135 millimolar.5. The method according to claim 1 , wherein the denaturant is urea and is at a concentration of 1 to 5 molar; a concentration of 3 ...

FUNCTIONALLY MODIFIED POLYPEPTIDES AND RADIOBIOSYNTHESIS

Provided herein are compositions and methods for generating polypeptides using non-natural amino acids (nnAAs) and genetic machinery, wherein the modified polypeptides, such as therapeutic polypeptides, bind to albumin, such as serum albumin. Methods of substituting a non-natural amino acid in a first polypeptide to obtain a modified polypeptide, the nnAA in some instances comprising an albumin targeting group, are disclosed, as are methods for making populations of such modified polypeptides. A therapeutic polypeptide, interleukin-1 receptor antagonist (IL-1RA) is exemplified using the disclosed methods. 1. A method of substituting a natural amino acid in a first polypeptide with a non-natural amino acid to obtain a modified polypeptide , wherein the non-natural amino acid comprises a moiety selected from the group consisting of: an albumin-targeting group , a radiolabel , and a radiolabelled albumin-targeting group , comprising:(a) selecting at least one amino acid residue in the first polypeptide to be substituted with the non-natural amino acid;(b) selecting a polynucleotide encoding the first polypeptide;(c) modifying the polynucleotide such that the amino acid residue to be substituted is encoded by a nonsense codon;(d) expressing the modified polynucleotide in a cell, wherein the cell is in the presence of the non-natural amino acid and expresses a suppressor tRNA and its cognate tRNA synthetase wherein the suppressor tRNA recognizes the nonsense codon of step (c), and the cell incorporates the non-natural amino acid into the modified polypeptide at the nonsense codon of step (c) during translation.2. The method of claim 1 , wherein the non-natural amino acid is represented by the formula:{'br': None, 'A-T'}wherein A is an amino acid selected from the group consisting of lysine, ornithine, arginine, serine, threonine, asparagine and glutamine, andT is a moiety selected from the group consisting of: an albumin-targeting group, a radiolabel, and a radiolabelled ...

KINETIC RESOLUTION

Whilst methodologies for the Kinetic Resolution of alcohols are well established, no analogous direct methods exist for the highly selective, direct catalytic Kinetic Resolution of thiols (i.e., R—SH). The present invention relates to a method for resolving stereoisomeric mixtures of thiols. In particular, the present invention relates to purely organocatalytic mediated resolution of enantiomeric mixtures of thiols without the need for enzymes. Also disclosed are some novel catalysts. Such catalysts may comprise a cinchona alkaloid-derived moiety. 2. A method according to wherein the mixture of stereoisomers of the thiol is an enantiomeric mixture of the thiol.3. A method according to wherein the thiols are selected from the group consisting of primary thiols and secondary thiols.4. A method according to wherein the bifunctional organocatalyst comprises a cinchona alkaloid.5. A method according to wherein the cinchona alkaloid is substituted with a urea claim 4 , thiourea or sulfonamide functional group.6. A method according to wherein the step of acylating the thiol comprises reacting the thiol with an organic anhydride.9. A process according to wherein the step of converting the thioester functional group into an amine comprises:iii) aminolysis of the thioester functional group to yield an amide; andiv) subjecting the amide product of step iii) to a Hofmann rearrangement.10. A method according to claim 1 , wherein the step of acylating the thiol comprises reacting the thiol with an organic anhydride claim 1 , wherein the organic anhydride is a prochiral anhydride and wherein acylation of the thiol with the prochiral anhydride in the presence of the bifunctional organocatalyst proceeds with desymmetrisation of the prochiral anhydride to afford a thioester.12. A method according to claim 1 , wherein the step of acylating the thiol comprises reacting the thiol with an organic anhydride claim 1 , wherein the organic anhydride is a meso anhydride and wherein acylation ...

BIODEGRADABLE COMPOUND, LIPID PARTICLE, COMPOSITION CONTAINING LIPID PARTICLE, AND KIT

The compound according to the present embodiment is represented by the following formula (1): 2. The compound according to claim 1 , wherein the L contains an ester structure selected from the group consisting of —C(═O)—O— claim 1 , —O—C(═O)—O— claim 1 , —O—C(═O)—O— claim 1 , —C(═S)—O— claim 1 , —O—C(═S)— claim 1 , —O—C(═S)—O— claim 1 , —S—C(═O)— claim 1 , —C(═O)—S— claim 1 , and —O—P(═O)OR′—O—(wherein R′ is hydrogen claim 1 , a non-cationic aliphatic group claim 1 , or —CHR).8. The compound according to claim 7 , wherein the c1 is a number from 4 to 8.9. The compound according to claim 1 , wherein the longest molecular chain contained in the R has 8 or more atoms.11. A lipid particle comprising the compound according to .12. The lipid particle according to claim 11 , further comprising a membrane-forming lipid and an aggregation-reducing lipid.13. The lipid particle according to claim 12 , wherein the membrane-forming lipid is selected from the group consisting of1,2-dioleoyl-sn-glycero-3-phosphoethanol amine (DOPE),1,2-stearoyl-sn-glycero-3-phosphoethanol amine (DSPE),1,2-dipalmitoyl-sn-glycero-3-phosphatidylcholine (DPPC),1-palmitoyl-2-oleoyl-sn-glycero-3-phosphatidylcholine (POPC),1,2-di—O—octadecyl-3-trimethylammonium propane (DOTMA),1,2-dioleoyl-3-dimethylammonium propane (DODAP),1,2-dimyristoyl-3-di methylammonium propane (14:0 DAP),1,2-dipalmitoyl-3-dimethylammonium propane (16:0 DAP),1,2-distearoyl-3-dimethylammonium propane (18:0 DAP),N-(4-carboxybenzyl)-N,N-dimethyl-2,3-bis(oleoyloxy)propane (DOBAQ),1,2-dioleoyl-3-trimethylammonium propane (DOTAP),1,2-dioleoyl-sn-glycero-3-phosphochlorine (DOPC),1,2-dilinoleoyl-sn-glycero-3-phosphochlorine (DLPC), 'wherein the aggregation-reducing lipid is a polyethylene glycol (PEG)-modified lipid.', '1,2-dioleoyl-sn-glycero-3-phospho-L-serine (DOPS), cholesterol, and the like; and'}14. The lipid particle according to claim 11 , further comprising an active agent.15. The lipid particle according to claim 14 , wherein the ...

2-CYANO-3-CYCLOPROPYL-3-HYDROXY-N-ARYL-THIOACRYLAMIDE DERIVATIVES

A compound of the formula (I) or a tautomeric isoform thereof wherein R1 is selected from the group consisting of halogen, nitro, lower alkyl sulfonyl, cyano, trifluromethyl lower alkyl, lower alkoxy, lower alkoxycarbonyl, carboxy, lower alkyl aminosulfonyl, perfluoro lower alkyl, lower alkylthio, hydroxy lower alkyl, alkoxy lower alkyl, lower alkylthio lower alkyl, lower alkylsulfinyl lower alkyl, lower alkylsulfonyl lower alkyl, lower alkylsulfonyl, lower alkanoyl, aroyl, aryl, aryloxy and R2 is selected from the group consisting of hydrogen, alkyl, alkoxy, alkylthio, and alkylcarbonyl, and their non-toxic, pharmaceutically acceptable base addition salts or pro-drugs thereof. The compounds of the invention are useful in the treatment of nervous system diseases and disorders, which are responsive to modulation of the GABAreceptor complex. 2. The compound according to claim 1 , wherein R1 is selected from a group consisting of fluorine claim 1 , chlorine claim 1 , jodine claim 1 , a trifluoromethyl claim 1 , a cyano claim 1 , a nitro claim 1 , a methansulfinyl claim 1 , a methansulfonyl claim 1 , a trifluoromethansulfinyl and a trifluoromethansulfonyl; and wherein R2 is selected from the group consisting of hydrogen claim 1 , ethyl claim 1 , and methyl.3. The compound according to claim 1 , wherein the compound is selected from the group consisting of 2-cyano-3-cyclopropyl-3-hydroxy-N-(3-methyl-4-trifluormethyl-phenyl)-thioacrylamide claim 1 , 2-cyano-3-cyclopropyl-3-hydroxy-N-(3-ethyl-4-trifluormethyl-phenyl)-thioacrylamide claim 1 , 2-cyano-3-cyclopropyl-N-(4-fluoro-3-methyl-phenyl)-3-hydroxy-thioacrylamide claim 1 , 2-cyano-3-cyclopropyl-N-(4-fluoro-3-ethyl-phenyl)-3-hydroxy-thioacrylamide claim 1 , 2-cyano-3-cyclopropyl-N-(4-fluoro-phenyl)-3-hydroxy-thioacrylamide 2-cyano-3-cyclopropyl-3-hydroxy-N-(3-methyl-4-nitro-phenyl)-thioacrylamide claim 1 , 2-cyano-3-cyclopropyl-3-hydroxy-N-(3-ethyl-4-nitro-phenyl)-thioacrylamide claim 1 , 2-cyano-3-cyclopropyl-3-hydroxy- ...

New Process

The present invention relates to a process for the preparation of S-[2-[1-(2-ethylbutyl)cyclohexylcarbonylamino]-phenyl] 2-methylthiopropionate which is useful as a pharmaceutically active compound. 5. The process according to claim 1 , wherein Ris (2-Ethyl-butyl)-cyclohexyl.6. The process according to claim 1 , wherein X claim 1 , Xand Xare each independently hydrogen or a (C-C)alkyl.7. The process according to claim 1 , wherein X claim 1 , X and X are each independently hydrogen or a (C-C)alkyl.13. The process according to wherein Ris isopropyl and the acylating agent is isobutyric anhydride or isobutyryl halide.14. The process according to wherein the acylating agent is isobutyric anhydride.15. The process according to claim 14 , wherein 2.0 to 4.0 equivalents of isobutyric anhydride with respect to the disulfide of formula (II) is used.16. The process according to in the presence of a solvent or a mixture of two or more solvents.17. The process according to claim 16 , wherein the solvent is an organic solvent.18. The process according to claim 16 , wherein the solvent is an ether like solvent claim 16 , ester like solvent claim 16 , aliphatic hydrocarbon solvent claim 16 , saturated alicyclic hydrocarbon solvent claim 16 , aromatic solvent or a mixture thereof.19. The process according to claim 16 , wherein the solvent is an aliphatic hydrocarbon solvent claim 16 , saturated alicyclic hydrocarbon solvent claim 16 , or aromatic solvent.20. The process according to wherein the acylating agent is an anhydride derivative which can act as a solvent or co-solvent with a molar ratio anhydride/amidodisulfide of 2 to 19.22. The process according to claim 21 , wherein the His added at a pressure of at least 0.1 bar.23. The process according to claim 1 , wherein the reaction is carried out at temperature up to 150° C.24. The process according to claim 1 , wherein the heterogeneous transition metal hydrogenation catalyst is a Raney catalyst claim 1 , Pd/C claim 1 , Pd(OH)/C ...

METHODS AND COMPOSITIONS RELATING TO SYNTHETIC BETA-1,6 GLUCOSAMINE OLIGOSACCHARIDES

The invention relates to the compositions of synthetic oligo-γ-(1→6)-2-amino-2-deoxy-D-glu-copyranosides conjugated to carriers, and methods for making and use same. 159-. (canceled)60. A method for stimulating an immune response in a subject comprisingadministering to a subject in need thereof the oligosaccharide-carrier conjugate in an amount effective to stimulate an immune response in the subject,wherein the oligosaccharide-carrier conjugated comprises an oligosaccharide conjugated to a protein or peptide carrier, through a linker, wherein the oligosaccharide is a β-1,6-linked glucosamine that is 0-40% acetylated and 4-20 monomers in length.61. The method of claim 60 , wherein the oligosaccharide is 5-11 monomers in length.62. The method of claim 60 , wherein the oligosaccharide is 5 monomers in length.63. The method of claim 60 , wherein the oligosaccharide is 0% acetylated.64. The method of claim 60 , wherein the protein or peptide carrier is tetanus toxoid.65. The method of claim 60 , wherein the oligosaccharide-carrier conjugate has an oligosaccharide to carrier ratio of 1:1 claim 60 , 2:1 claim 60 , 3:1 claim 60 , 4:1 claim 60 , 5:1 claim 60 , 6:1 claim 60 , 7:1 claim 60 , 8:1 claim 60 , 9:1 claim 60 , 10:1 claim 60 , 20:1 claim 60 , 30:1 claim 60 , 40:1 claim 60 , 50:1 claim 60 , 60:1 claim 60 , 70:1 claim 60 , 80:1 claim 60 , 90:1 or 100:1.66. The method of claim 60 , wherein the oligosaccharide-carrier conjugate has an oligosaccharide to carrier ratio in the range of 10:1 to 50:1.67. The method of claim 60 , wherein the oligosaccharide-carrier conjugate has an oligosaccharide to carrier ratio in the range of 40:1.68. The method of claim 60 , free of microbial contaminants other than tetanus toxoid or components thereof.69. The method of claim 60 , wherein the subject is human.70. The method of claim 60 , wherein the subject is non-human.71. The method of claim 60 , wherein the oligosaccharide-carrier conjugate is administered to the subject prior to ...

BIODEGRADABLE LIPIDS FOR THE DELIVERY OF ACTIVE AGENTS

The present invention relates to a cationic lipid having one or more biodegradable groups located in a lipidic moiety (e.g., a hydrophobic chain) of the cationic lipid. These cationic lipids may be incorporated into a lipid particle for delivering an active agent, such as a nucleic acid. The invention also relates to lipid particles comprising a neutral lipid, a lipid capable of reducing aggregation, a cationic lipid of the present invention, and optionally, a sterol. The lipid particle may further include a therapeutic agent such as a nucleic acid. 119-. (canceled)21. The lipid particle of claim 20 , wherein the biodegradable group is an ester.22. The lipid particle of claim 20 , wherein the head group comprises an aliphatic group and a hydroxyl group.23. The lipid particle of claim 20 , wherein the head group consists of a saturated aliphatic group and a hydroxyl group.24. The lipid particle of claim 20 , wherein the hydrophobic tails have different chemical formulas.25. The lipid particle of claim 20 , wherein claim 20 , in each hydrophobic tail claim 20 , Ris a saturated claim 20 , straight-chain C-Calkyl group.26. The lipid particle of claim 20 , wherein claim 20 , in each hydrophobic tail claim 20 , Ris n-hexyl.27. The lipid particle of claim 20 , wherein claim 20 , in each hydrophobic tail claim 20 , Ris branched.28. The lipid particle of claim 21 , wherein the ester group in each hydrophobic tail is —OC(O)—.29. The lipid particle of claim 21 , wherein the ester group in each hydrophobic tail is —C(O)O—.30. The lipid particle of claim 20 , wherein claim 20 , in each hydrophobic tail claim 20 , Ris a saturated claim 20 , branched C-Calkyl group claim 20 , where the branching occurs at the α-position relative to the biodegradable group claim 20 , and where the total carbon atom content of the tail is 21 to 26.31. The lipid particle of claim 20 , wherein claim 20 , in the at least one hydrophobic tail claim 20 , the biodegradable group is separated from a ...

BIODEGRADABLE LIPIDS FOR THE DELIVERY OF ACTIVE AGENTS

The present invention relates to a cationic lipid having one or more biodegradable groups located in a lipidic moiety (e.g., a hydrophobic chain) of the cationic lipid. These cationic lipids may be incorporated into a lipid particle for delivering an active agent, such as a nucleic acid. The invention also relates to lipid particles comprising a neutral lipid, a lipid capable of reducing aggregation, a cationic lipid of the present invention, and optionally, a sterol. The lipid particle may further include a therapeutic agent such as a nucleic acid. 119-. (canceled)20. A pharmaceutical composition comprising a lipid particle and a pharmaceutically acceptable diluent , wherein the lipid particle comprises:(i) a nucleic acid;(ii) 35-65 mol % of a lipid compound;(iii) 3-12 mol % of distearoylphosphatidylcholine (DSPC);(iv) 15-45 mol % of cholesterol; and(v) 0.5-10 mol % of 1-(monomethoxy-polyethylene glycol)-2,3-dimyristoyl glycerol (PEG-DMG) having an average molecular weight of 2,000 Da, wherein the lipid compound comprises a head group, two hydrophobic tails, and a central moiety to which the head group and the two hydrophobic tails are directly bonded, wherein:the central moiety is a nitrogen atom;{'sup': 12', '1', '13', '12', '1', '13, 'sub': 4', '14', '10', '20, 'each of the two hydrophobic tails independently has the formula —R-M-R, wherein Ris a C-Calkyl group, Mis a biodegradable group, and Ris a C-Calkyl group;'}in each hydrophobic tail, the biodegradable group is separated from a terminus of the hydrophobic tail by from 8 to 12 carbon atoms; and{'sup': '13', 'in at least one hydrophobic tail, Ris branched, where the branching occurs at the α-position relative to the biodegradable group, and where the total carbon atom content of the at least one tail is 21 to 26.'}21. The pharmaceutical composition of claim 20 , wherein the nucleic acid comprises RNA.22. The pharmaceutical composition of claim 20 , further comprising sodium acetate.23. The pharmaceutical ...

BIODEGRADABLE LIPIDS FOR THE DELIVERY OF ACTIVE AGENTS

The present invention relates to a cationic lipid having one or more biodegradable groups located in a lipidic moiety (e.g., a hydrophobic chain) of the cationic lipid. These cationic lipids may be incorporated into a lipid particle for delivering an active agent, such as a nucleic acid. The invention also relates to lipid particles comprising a neutral lipid, a lipid capable of reducing aggregation, a cationic lipid of the present invention, and optionally, a sterol. The lipid particle may further include a therapeutic agent such as a nucleic acid. 119-. (canceled)20. A pharmaceutical composition comprising a lipid particle and a pharmaceutically acceptable diluent , wherein the lipid particle comprises:(i) a nucleic acid;(ii) 35-65 mol % of a lipid compound;(iii) 3-12 mol % of distearoylphosphatidylcholine (DSPC);(iv) 15-45 mol % of cholesterol; and(v) 0.5-10 mol % of a PEG-modified lipid, whereinthe lipid compound comprises a head group, two hydrophobic tails, and a central moiety to which the head group and the two hydrophobic tails are directly bonded, wherein:the central moiety is a nitrogen atom;{'sup': 12', '1', '13', '12', '1', '13, 'sub': 4', '14', '10', '20, 'each of the two hydrophobic tails independently has the formula —R-M-R, wherein Ris a C-Calkyl group, Mis a biodegradable group, and Ris a C-Calkyl group;'}in each hydrophobic tail, the biodegradable group is separated from a terminus of the hydrophobic tail by from 8 to 12 carbon atoms; and{'sup': '13', 'in at least one hydrophobic tail, Ris branched, where the branching occurs at the α-position relative to the biodegradable group, and where the total carbon atom content of the at least one tail is 21 to 26.'}21. The pharmaceutical composition of claim 20 , wherein the nucleic acid comprises RNA.22. The pharmaceutical composition of claim 20 , wherein the pharmaceutical composition is a vaccine.23. The pharmaceutical composition of claim 20 , further comprising sodium chloride.24. The pharmaceutical ...

PROCESS FOR THE PREPARATION OF A SULFUR-AMINE

The present invention relates to a process for the synthesis of cysteamine or a salt thereof. 2. A process according to wherein the cysteamine salt is a pharmaceutically acceptable salt thereof selected from the group consisting of hydrochloride claim 1 , hydrobromide claim 1 , tartrate claim 1 , bitartrate claim 1 , fumarate claim 1 , and succinate salt.3. A process according to wherein the cysteamine salt is hydrochloride or bitartrate salt.4. A process according to wherein in step a) the protection reaction is carried out in the presence of di-tert-butyl dicarbonate ((Boc)O) and in the presence of an apolar solvent selected from the group consisting of toluene claim 1 , tetrahydrofuran claim 1 , dichloromethane claim 1 , and ethyl acetate.5. A process according to wherein the apolar solvent is toluene.6. A process according to wherein in step b) the tosylation reaction is carried out with p-toluenesulfonyl chloride claim 1 , in the presence of a base and of an apolar solvent.7. A process according to wherein the base is an organic base selected from the group consisting of triethylamine claim 6 , tributylamine claim 6 , diisopropylamine claim 6 , pyridine claim 6 , or an inorganic base selected from the group consisting of potassium carbonate claim 6 , sodium carbonate claim 6 , and sodium bicarbonate.8. A process according to wherein the apolar solvent is selected from the group consisting of toluene claim 6 , tetrahydrofuran claim 6 , dichloromethane claim 6 , and ethyl acetate.9. A process according to wherein the base is triethylamine and the apolar solvent is toluene.10. A process according to wherein the nucleophilic substitution reaction at step c) is carried out with thioacetic acid claim 1 , potassium thioacetate or sodium thioacetate claim 1 , in the presence of a base and of a polar solvent.11. A process according to wherein the base is selected from the group consisting of potassium carbonate claim 10 , sodium carbonate and sodium bicarbonate.12. A ...

PROCESSES FOR CONVERTING CARBOXAMIDES TO THIOCARBOXAMIDES

Process for converting a carboxamide to a thiocarboxamide includes reacting (a) a substrate that comprises a heteroatom-containing moiety and a carboxamide moiety with (b) a dialkyl dithiophosphate and/or a salt thereof. The heteroatom-containing moiety includes a heteroatom selected from the group consisting of N, O, and S. Processes for preparing piperidine-4-thiocarboxamide are described. 1. A process for converting a carboxamide to a thiocarboxamide , the process comprising:reacting (a) a substrate that comprises a heteroatom-containing moiety and a carboxamide moiety with (b) a dialkyl dithiophosphate and/or a salt thereof;wherein the heteroatom-containing moiety comprises a heteroatom selected from the group consisting of N, O, and S.5. The process of claim 1 , wherein the heteroatom-containing moiety comprises a nitrogen atom.6. The process of claim 1 , wherein the heteroatom-containing moiety comprises a heterocyclic moiety selected from the group consisting of aziridine claim 1 , azirine claim 1 , diazirine claim 1 , oxaziridine claim 1 , azetidine claim 1 , azete claim 1 , diazetidine claim 1 , pyrrolidine claim 1 , pyrrole claim 1 , imidazolidine claim 1 , imidazole claim 1 , pyrazolidine claim 1 , pyrazole claim 1 , oxazolidine claim 1 , oxazole claim 1 , isoxazolidine claim 1 , isoxazole claim 1 , thiazolidine claim 1 , thiazole claim 1 , isothiazolidine claim 1 , isothiazole claim 1 , triazoles claim 1 , furazan claim 1 , oxadiazole claim 1 , thiadiazole claim 1 , dithiazole claim 1 , tetrazole claim 1 , piperidine claim 1 , pyridine claim 1 , piperazine claim 1 , diazines claim 1 , morpholine claim 1 , oxazine claim 1 , thiomorpholine claim 1 , thiazine claim 1 , triazine claim 1 , tetrazine claim 1 , azepane claim 1 , azepine claim 1 , homopiperazine claim 1 , diazepine claim 1 , thiazepine claim 1 , azocane claim 1 , azocine claim 1 , tetrahydropyran claim 1 , and combinations thereof.9. The process of claim 8 , wherein Rand Rare hydrogen.10. The ...

METHODS AND COMPOSITIONS RELATING TO SYNTHETIC BETA-1,6 GLUCOSAMINE OLIGOSACCHARIDES

The invention relates to the compositions of synthetic oligo-β-(1→6)-2-amino-2-deoxy-D-glucopyranosides conjugated to carriers, and methods for making and use same. 159.-. (canceled)60. An oligosaccharide-carrier conjugate comprising an oligosaccharide conjugated to a protein or peptide carrier through a linker , wherein the oligosaccharide is a β-1 ,6-linked glucosamine that is 0-40% acetylated.61. The oligosaccharide-carrier conjugate of claim 60 , wherein the protein or peptide carrier is tetanus toxoid.62. The oligosaccharide-carrier conjugate of claim 60 , wherein the oligosaccharide is 5-11 monomers in length.63. The oligosaccharide-carrier conjugate of claim 60 , wherein the oligosaccharide is 0% acetylated.64. The oligosaccharide-carrier conjugate of claim 60 , wherein the oligosaccharide-carrier conjugate has an oligosaccharide to carrier ratio of 1:1 claim 60 , 2:1 claim 60 , 3:1 claim 60 , 4:1 claim 60 , 5:1 claim 60 , 6:1 claim 60 , 7:1 claim 60 , 8:1 claim 60 , 9:1 claim 60 , 10:1 claim 60 , 20:1 claim 60 , 30:1 claim 60 , 40:1 claim 60 , 50:1 claim 60 , 60:1 claim 60 , 70:1 claim 60 , 80:1 claim 60 , 90:1 or 100:1.65. The oligosaccharide-carrier conjugate of claim 60 , wherein the oligosaccharide-carrier conjugate has an oligosaccharide to carrier ratio in the range of 10:1 to 50:1.66. A method for stimulating an immune response in a subject comprising administering to a subject in need thereof the oligosaccharide-carrier conjugate of in an amount effective to stimulate an immune response in the subject.67. The method of claim 66 , wherein the subject is human.68. The method of claim 66 , wherein the subject is non-human.69. A method for treating or preventing an infection in a subject comprising{'claim-ref': {'@idref': 'CLM-00060', 'claim 60'}, 'administering to a subject having or at risk of developing an infection by a bacterial species that produces poly-N-acetyl glucosamine (PNAG) an effective amount for inducing an immune response of the ...

SUBSTITUTED N-ACETYL-L-CYSTEINE DERIVATIVES AND RELATED COMPOUNDS

Novel substituted N-acetyl-L-cysteine (NAC) derivatives and related compounds and methods of using these compounds for the treatment of diseases and/or conditions, including but not limited to diseases and/or conditions of, or involving, the Central Nervous System (CNS), including schizophrenia adrenoleukodystrophy, mitochondrial diseases (e.g. Leigh syndrome, Alpers' disease, and MELAS), Huntington's disease, trichotillomania, HIV-associated neurocognitive disorder, hypoxic-ischemic encephalopathy, drug craving, and drug addiction. 3. (canceled)4. A pharmaceutical composition comprising the compound of and a pharmaceutically acceptable carrier.5. A method of treating central nervous system (CNS) disorders or conditions comprising administering to a subject in need thereof a therapeutically effective amount of the compound of .6. The method of wherein the CNS condition is drug addiction.7. The method of wherein the CNS disorder is selected from the group consisting of adrenoleukodystrophy claim 5 , Leigh syndrome claim 5 , Alpers' disease claim 5 , MELAS claim 5 , Huntington's disease claim 5 , trichotillomania claim 5 , HIV-associated neurocognitive disorder claim 5 , hypoxic-ischemic encephalopathy and schizophrenia.8. The method of wherein the CNS disorder is schizophrenia. This invention relates to novel substituted N-acetyl-L-cysteine (“NAC”) derivatives and related compounds and methods of using these compounds for the treatment of diseases and/or conditions, including but not limited to diseases and/or conditions of, or involving, the Central Nervous System (CNS), including schizophrenia adrenoleukodystrophy, mitochondrial diseases (e.g. Leigh syndrome, Alpers' disease, and MELAS), Huntington's disease, trichotillomania, HIV-associated neurocognitive disorder, hypoxic-ischemic encephalopathy, drug craving, and drug addiction.Schizophrenia is a debilitating disorder afflicting 1% of the world's population. The development of effective medications to treat ...

COMPOUND, COMPOSITION AND USES THEREOF

The disclosure herein provides the compounds of Formulas 1 and its pharmaceutical acceptable salts, as well as polymorphs, solvates, and hydrates thereof. These salts may be formulated as pharmaceutical compositions. The pharmaceutical compositions may be formulated for oral administration, transdermal administration, and/or injection. Such compositions may be used for the treatment of metabolic conditions, cystinosis, non-alcoholic Steatohepatitis, hypertriglyceridemia, and/or neurodegenerative disorders, and/or their associated complications. 2. The method of claim 1 , further comprising administering the compound of comprising Formula 1 through at least one of a non-invasive peroral claim 1 , a topical ointment claim 1 , an enteral claim 1 , a gel solution claim 1 , a syrup claim 1 , a lotion claim 1 , a healing pad claim 1 , a transmucosal delivery claim 1 , a targeted delivery claim 1 , a sustained release delivery claim 1 , a delayed release delivery claim 1 , a pulsed release delivery claim 1 , a patch claim 1 , and a parenteral delivery.3. The method of claim 2 , wherein the method treats at least one of a hypertriglyceridemia disorder claim 2 , a stroke claim 2 , an atrial fibrillation claim 2 , a coronary heart disease claim 2 , a non-alcoholic Steatohepatitis claim 2 , cystinosis claim 2 , nephropathic cystinosis claim 2 , and Huntington's disease. This application is a continuation application of U.S. non-provisional patent application Ser. No. 13/858,045 titled “COMPOUND, COMPOSITION AND USES THEREOF” filed on Apr. 6, 2013. Which is a continuation application claiming priority to co-pending U.S. non-provisional patent application Ser. No. 13/649,094 titled COMPOUND, COMPOSITION AND USES THEREOF filed on Oct. 10, 2012, which claimed priority to Ser. No. 13/152,864, filed on Jun. 3, 2011, India Provisional Patent Application No. 3947/CHE/2012, filed on Sep. 24, 2012 and is the national phase application of PCT application No. PCT/IN/2012/000668 filed on ...

Retinoic acid receptor antagonists as chaperone-mediated autophagy modulators and uses thereof

Compounds, compositions and methods are provided for selectively activating chaperone-mediated autophagy (CMA), protecting cells from oxidative stress, proteotoxicity and lipotoxicity, and/or antagonizing activity of retinoic acid receptor alpha (RARα) in subjects in need thereof.

COMPOUNDS AND METHODS OF TREATING CANCER

Presented herein inter alia are novel compounds and methods of using the same for the treatment of cancers. 2. The compound of having formula (I) claim 1 , wherein Lis a bond.3. The compound of claim 1 , wherein Land Lare bonds.411.-. (canceled)12. The compound of claim 1 , wherein Ris —NRRor substituted or unsubstituted heterocycloalkyl and Ris —NRRor substituted or unsubstituted heterocycloalkyl.13. (canceled)14. The compound of claim 12 , wherein Rand Rare joined to form a substituted or unsubstituted pyrrolidinyl claim 12 , substituted or unsubstituted imidazolidinyl claim 12 , substituted or unsubstituted oxazolidinyl claim 12 , substituted or unsubstituted thiazolidinyl claim 12 , substituted or unsubstituted dioxolanyl claim 12 , substituted or unsubstituted dithiolanyl claim 12 , substituted or unsubstituted piperidinyl claim 12 , substituted or unsubstituted morpholinyl claim 12 , substituted or unsubstituted dioxanyl claim 12 , or substituted or unsubstituted dithianyl claim 12 , substituted or unsubstituted aziridinyl claim 12 , substituted or unsubstituted azetidinyl claim 12 , substituted or unsubstituted azepinyl claim 12 , substituted or unsubstituted oxiranyl claim 12 , substituted or unsubstituted oxetanyl claim 12 , substituted or unsubstituted tetrahydrofuranyl claim 12 , substituted or unsubstituted tetrahydrothiophenyl claim 12 , or substituted or unsubstituted tetrahydropyranyl.15. The compound of claim 14 , wherein Ris —NRR claim 14 , and wherein Rand Rare joined to form a substituted or unsubstituted 5 to 8 membered heterocycloalkyl.16. The compound of claim 15 , wherein Rand Rare joined to form a substituted or unsubstituted pyrrolidine claim 15 , substituted or unsubstituted imidazolidine claim 15 , substituted or unsubstituted oxazolidine claim 15 , substituted or unsubstituted thiazolidine claim 15 , substituted or unsubstituted dioxolane claim 15 , or substituted or unsubstituted dithiolane claim 15 , substituted or unsubstituted ...

Photobase Generator, Compound, Photoreactive Composition, and Reaction Product

A photobase generator includes a compound including a first skeleton represented by the following formula (a), and a second skeleton including a nitrogen atom bonding to a bonding position of the first skeleton to form an amide group, wherein the compound generates a base, in which a hydrogen atom is bonding with the nitrogen atom of the second skeleton, by light irradiation, and the pKa of a conjugate acid of the base in water is 12 or more. In formula (a), G is a divalent aromatic group, and * represents the bonding position with the nitrogen atom. 5. (canceled)7. A photoreactive composition , comprising:{'claim-ref': {'@idref': 'CLM-00001', 'claim 1'}, 'the photobase generator according to ; and'}a base-reactive compound,wherein the base-reactive compound includes a functional group that is converted, by the action of a base, into a group exhibiting reactivity, or includes a group that reacts in response to the action of a base.8. A reaction product obtained by reacting the photoreactive composition according to .9. A photoreactive composition claim 7 , comprising:{'claim-ref': {'@idref': 'CLM-00002', 'claim 2'}, 'the photobase generator according to ; and'}a base-reactive compound,wherein the base-reactive compound includes a functional group that is converted, by the action of a base, into a group exhibiting reactivity, or includes a group that reacts in response to the action of a base.10. A photoreactive composition claim 7 , comprising:{'claim-ref': {'@idref': 'CLM-00003', 'claim 3'}, 'the photobase generator according to ; and'}a base-reactive compound,wherein the base-reactive compound includes a functional group that is converted, by the action of a base, into a group exhibiting reactivity, or includes a group that reacts in response to the action of a base. The present invention relates to a photobase generator, a compound, a photoreactive composition, and a reaction product.Photopolymerizable materials to be polymerized when irradiated with light are ...

RETINOIC ACID RECEPTOR ANTAGONISTS AS CHAPERONE-MEDIATED AUTOPHAGY MODULATORS AND USES THEREOF

Compounds, compositions and methods are provided for selectively activating chaperone-mediated autophagy (CMA), protecting cells from oxidative stress, proteotoxicity and lipotoxicity, and/or antagonizing activity of retinoic acid receptor alpha (RARα) in subjects in need thereof. 2. The compound of claim 1 , wherein the halogen is Br claim 1 , Cl claim 1 , F or I.3. The compound of claim 1 , wherein the alkyl is C1-C3 alkyl.6. A pharmaceutical composition comprising a compound of claim 1 , or a combination of any compounds thereof claim 1 , and a pharmaceutically acceptable carrier or diluent.8. The method of claim 7 , wherein the subject has a neurological disease or disorder claim 7 , a neurodegenerative disease claim 7 , a tauopathy claim 7 , Parkinson's Disease claim 7 , Alzheimer's Disease claim 7 , Huntington's Disease claim 7 , frontotemporal dementia claim 7 , retinal degeneration claim 7 , multiple sclerosis claim 7 , diabetes claim 7 , a lysosomal storage disorder claim 7 , a retinal disease claim 7 , a cardiovascular disease claim 7 , myocardial infarction claim 7 , cardiac hypertrophy or a cardiomyopathy.9. The method of claim 7 , wherein the subject has reduced CMA compared to a normal subject prior to administering the compound.10. The method of claim 7 , wherein the compound does not affect macroautophagy.12. The method of claim 11 , wherein the subject has one or more of a neurological disease or disorder claim 11 , a neurodegenerative disease claim 11 , a tauopathy claim 11 , Parkinson's Disease claim 11 , Alzheimer's Disease claim 11 , Huntington's Disease claim 11 , frontotemporal dementia claim 11 , retinal degeneration claim 11 , multiple sclerosis claim 11 , diabetes claim 11 , a lysosomal storage disorder claim 11 , a retinal disease claim 11 , a cardiovascular disease claim 11 , myocardial infarction claim 11 , cardiac hypertrophy and a cardiomyopathy.13. The method of claim 11 , wherein the cells being protected comprise cardiac cells claim ...

LOW FREE 2-MERCAPTOETHANOL ESTER AND USES THEREOF

A novel Low Free 2-MercaptoEthanol Ester has been used to prepare Alkyl Tin Reverse Ester Stabilizers as well as used to enhance the thermal performance of those Alkyl Tin Reverse Ester Stabilizers or Alkyl Tin Thioglycolate Stabilizers or Alkyl Tin Mercaptides for PVC applications where odor during PVC compounding, processing, or of the final PVC article has prevented widespread use of Alkyl Tin Reverse Ester Stabilizers. 13-. (canceled)4. A method of using a Low Free 2-MercaptoEthanol Ester (LFMEE) that is obtained through removal of 2-MercaptoethylEthanol from a standard 2-MercaptoEthanol Ester , wherein the resulting LFMEE have residual 2-Mercaptoethanol below 1.0 wt % to enhance thermal performance of alkyl tin thioglycolate ester stabilizers.5. A method of using a Low Free 2-MercaptoEthanol Ester (LFMEE) that is obtained through removal of 2-MercaptoethylEthanol from a standard 2-MercaptoEthanol Ester , wherein the resulting LFMEE have residual 2-Mercaptoethanol below 1.0 wt % to enhance thermal performance of alkyl tin reverse ester stabilizers.6. A method of using a Low Free 2-MercaptoEthanol Ester (LFMEE) that is obtained through removal of 2-MercaptoethylEthanol from a standard 2-MercaptoEthanol Ester , wherein the resulting LFMEE have residual 2-Mercaptoethanol below 1.0 wt % to enhance thermal performance of alkyl tin mercaptide and carboxylate stabilizers.7. The method of wherein the mercaptide can be dodocylmercaptan or carboxylates.8. The method of wherein the carboxylate is Maleates.9. The method of wherein the stabilizer further includes sulfide bridging for alkyl groups ranging of C1-C8.10. The method of wherein the mono and di components of alkyl tin groups are in ratios ranging from 100% di to 100% mono and all combinations between.11. The method of wherein the amount of LFMEE can range from 5 wt % to 75 wt %.12. The method of wherein the amount of LFMEE can range from 10 wt % to 40 wt %.13. The method of wherein the resulting stabilizer further ...

METHODS OF TREATMENT USING MODULATORS OF SIRT2

The instant application describes novel compounds that modulate (in particular, inhibit) Sirt2, with structures according to Formulas (1) and (2) provided herein. The invention is also directed to pharmaceutical compositions thereof, methods of treatment (i.e., cancer and neurodegenerative disease) by administration of the modulating compounds, assay methods for finding modulators of Sirt2, and kits for practicing the assay method. 2. The compound of claim 1 , wherein said hydrocarbon group for Rhas at least five carbon atoms connected by carbon-carbon bonds in the absence of heteroatom substitution claim 1 , except that one or more hydrogen atoms are optionally replaced with fluoro atoms.3. The compound of claim 1 , wherein said hydrocarbon group for Rhas at least six carbon atoms.4. The compound of claim 1 , wherein said hydrocarbon group for Rhas at least seven carbon atoms.5. The compound of claim 1 , wherein said hydrocarbon group for Rhas at least eight carbon atoms.6. The compound of claim 1 , wherein said hydrocarbon group for Rhas up to twenty carbon atoms.7. The compound of claim 1 , wherein each of X claim 1 , X claim 1 , and Xis —(CH)— claim 1 , wherein n is independently 1 claim 1 , 2 claim 1 , or 3.8. The compound of claim 1 , wherein each of X claim 1 , X claim 1 , and Xis —CH—.9. The compound of claim 1 , wherein Yis an —O— atom.10. The compound of claim 1 , wherein Yis an —NR— group.11. The compound of claim 1 , wherein Yis an —O— atom and Yis an —NR— group.12. The compound of claim 1 , wherein Rand Rare independently selected from hydrogen atom claim 1 , unsubstituted hydrocarbon groups having up to three carbon atoms claim 1 , alkoxy groups —OR claim 1 , amide groups —NR′C(O)R or —C(O)NR′R claim 1 , ketone groups —C(O)R claim 1 , ester groups C(O)OR or —OC(O)R claim 1 , carbamate groups —OC(O)NR′R or —NR′C(O)OR claim 1 , and urea groups —NR′C(O)NR claim 1 , wherein R is a hydrocarbon group having up to three carbon atoms claim 1 , and R′ is a ...

Bimesogenic Compounds and Mesogenic Media

The invention relates to bimesogenic compounds of formula I 4. Bimesogenic compounds according to claim 1 , characterized in that Ris selected from OCF claim 1 , CF claim 1 , F claim 1 , Cl and CN.5. Bimesogenic compounds according to claim 1 , characterized in that Spis —(CH)— and o is 1 claim 1 , 3 or an integer from 5 to 15.6. (canceled)7. Liquid-crystalline medium claim 1 , characterised in that it comprises one or more bimesogenic compounds according to .9. (canceled)10. Liquid crystal device comprising a liquid crystalline medium comprising two or more components claim 1 , one or more of which is a bimesogenic compound of formula I according to .11. Liquid crystal device according to claim 10 , characterized in that it is a flexoelectric device. The invention relates to bimesogenic compounds of formula Iwherein R, R, MG, MGand Sphave the meaning given herein below, to the use of bimesogenic compounds of formula I in liquid crystal media and particular to flexoelectric liquid crystal devices comprising a liquid crystal medium according to the present invention.Liquid Crystal Displays (LCDs) are widely used to display information. LCDs are used for direct view displays, as well as for projection type displays. The electro-optical mode which is employed for most displays still is the twisted nematic (TN)-mode with its various modifications. Besides this mode, the super twisted nematic (STN)-mode and more recently the optically compensated bend (OCB)-mode and the electrically controlled birefringence (ECB)-mode with their various modifications, as e. g. the vertically aligned nematic (VAN), the patterned ITO vertically aligned nematic (PVA)-, the polymer stabilized vertically aligned nematic (PSVA)-mode and the multi domain vertically aligned nematic (MVA)-mode, as well as others, have been increasingly used. All these modes use an electrical field, which is substantially perpendicular to the substrates, respectively to the liquid crystal layer. Besides these ...

RAPID CURE POLYMERIC RESINS

A polysulfide material having reactive vinyl end groups and a method of making a vinyl end-capped polysulfide material are described. The vinyl end-capped polysulfide material has potential applications as a sealant, an adhesive, a coating, a caulking, or the like. In a specific example, the polysulfide material may be used as a precursor material for a sealant resin in the manufacturing of an integral fuel tank of an aircraft. An example method for making polysulfide materials includes contacting a vinyl-functionalized aryl halide and/or a vinyl-functionalized heteroaryl halide with dithiols and/or trithiols in the presence of an organic solvent. 2. The polymer of claim 1 , wherein each instance of Ris the same or different and is selected from -aryl-alkyl- or -aryl-.3. The polymer of claim 2 , wherein each instance of Ris the same or different and is selected from -benzyl- or -phenyl-.4. The polymer of claim 3 , wherein each instance of Ris -ethyl-O-methyl-O-ethyl-.5. The polymer of claim 1 , wherein each instance of Ris -heteroaryl-.6. The polymer of claim 1 , wherein each instance of Ris -heteroaryl-alkyl-.7. The polymer of claim 1 , wherein each instance of -alkyl- of Ris selected from the group consisting of -methyl- claim 1 , -ethyl- claim 1 , and -propyl-.9. The polymer of claim 8 , wherein each instance of Ris -ethyl-O-methyl-O-ethyl- and each instance of Ris -benzyl-.10. The polymer of claim 8 , wherein each instance of -alkyl- of Ris selected from the group consisting of -methyl- claim 8 , -ethyl- claim 8 , and -propyl-.14. The method of claim 13 , wherein X is chlorine claim 13 , Ris -benzyl- claim 13 , and at least one instance of Ris -ethyl-O-methyl-O-ethyl-.15. The method of claim 13 , wherein the organic solvent is N claim 13 ,N-dimethylformamide. This application claims benefit from U.S. Provisional Patent Application No. 62/095,371, filed Dec. 22, 2014, which is incorporated by reference in its entirety.The present disclosure relates generally to ...

POLYMERIZABLE COMPOSITION COMPRISING AN OXIME SULFONATE AS THERMAL CURING AGENT

The present invention relates to a polymerizable composition comprising at least one ethylenically unsaturated, polymerizable compound and at least one oxime sulfonate compound of the formula I 144-. (canceled)47: The compound of formula I according to claim 45 , where{'sup': '14', 'X is S or NRand'}{'sup': 14', '6', '14a', '8', '9', '10', '11', '4', '5', '6', '7', '8', '9', '10', '11, 'sub': 1', '12', '3', '8', '1', '8', '1', '4', '2, 'Ris C-C-alkyl, which may be interrupted by one or more O, S, NRor CO and/or may be substituted by one or more identical or different radicals Rselected from CN, COR, COOR, CONRR, phenyl and C-C-cycloalkyl which may interrupted by one or two CO groups and where the two last-mentioned radicals may be substituted by one or more identical or different radicals selected from C-C-alkyl, C-C-haloalkyl, F, Cl, Br, I, CN, NO, SR, OR, NRR, COR, COORand CONRR;'}{'sub': 2', '12', '3', '8', '1', '8', '1', '4', '2, 'sup': 6', '14a', '8', '9', '10', '11', '4', '5', '6', '7', '8', '9', '10', '11, 'C-C-alkenyl, which may be interrupted by one or more O, S, NRor CO and/or may be substituted by one or more identical or different radicals Rselected from CN, COR, COOR, CONRR, phenyl and C-C-cycloalkyl which may interrupted by one or two CO groups and where the two last-mentioned radicals may be substituted by one or more identical or different radicals selected from C-C-alkyl, C-C-haloalkyl, F, Cl, Br, I, CN, NO, SR, OR, NRR, COR, COORand CONRR;'}{'sub': 3', '12', '1', '8, 'sup': 14b', '8', '9', '10', '11, 'C-C-cycloalkyl, which may be interrupted by one or more CO and/or may be substituted by one or more identical or different radicals Rselected from C-C-alkyl, CN, COR, COOR, CONRR;'}{'sup': 14c', '4', '5', '6', '7', '8', '9', '10', '11, 'sub': 1', '8', '1', '4', '2, 'phenyl, which may be substituted by one or more identical or different radicals Rselected from C-C-alkyl, C-C-haloalkyl, F, Cl, Br, I, CN, NO, SR, OR, NRR, COR, COOR, CONRRand phenyl,'}or ...

Stabilized Multi-Functional Antioxidant Compounds and Methods of Use

Disclosed are novel stable compounds having anti-oxidant properties and methods of using the compounds for the treatment of diseases or injuries associated with oxidative stress. 120-. (canceled)22. (canceled)23. The compound according to claim 21 , wherein{'sub': '2', 'L is CH;'}{'sup': '4', 'Ris H;'}{'sup': '6', 'Ris —C(O)Me;'}{'sup': '9', 'Ris H, —C(O)Me, or —C(O)Et;'}{'sup': 1', '5, 'Lis —CHR; and'}{'sup': '5', 'sub': '2', 'Ris —COOH or —C(O)NH.'}24. The compound according to claim 21 , wherein the compound is selected from:(2R)-4-(2-acetamido-2-carboxyethylthio)-2-hydroxy-N,N,N-trimethyl-4-oxobutan-1-aminium;(2R)-4-(2-acetamido-3-amino-3-oxopropylthio)-2-hydroxy-N,N,N-trimethyl-4-oxobutan-1-aminium;(2R)-4-(2-acetamido-2-carboxyethylthio)-2-acetoxy-N,N,N-trimethyl-4-oxobutan-1-aminium;(2R)-4-(2-acetamido-3-amino-3-oxopropylthio)-2-acetoxy-N,N,N-trimethyl-4-oxobutan-1-aminium;(2R)-4-(2-acetamido-2-carboxyethylthio)-N,N,N-trimethyl-4-oxo-2-(propionyloxy)butan-1-aminium;(2R)-4-(2-acetamido-3-amino-3-oxopropylthio)-N,N,N-trimethyl-4-oxo-2-(propionyloxy)butan-1-aminium.2536-. (canceled)37. The compound according to claim 24 , wherein the compound is (2R)-4-(2-acetamido-2-carboxyethylthio)-2-hydroxy-N claim 24 ,N claim 24 ,N-trimethyl-4-oxobutan-1-aminium.38. The compound according to claim 24 , wherein the compound is (2R)-4-(2-acetamido-3-amino-3-oxopropylthio)-2-hydroxy-N claim 24 ,N claim 24 ,N-trimethyl-4-oxobutan-1-aminium.39. The compound according to claim 24 , wherein the compound is (2R)-4-(2-acetamido-2-carboxyethylthio)-2-acetoxy-N claim 24 ,N claim 24 ,N-trimethyl-4-oxobutan-1-aminium.40. The compound according to claim 24 , wherein the compound is ((2R)-4-(2-acetamido-3-amino-3-oxopropylthio)-2-acetoxy-N claim 24 ,N claim 24 ,N-trimethyl-4-oxobutan-1-aminium.41. The compound according to claim 24 , wherein the compound is (2R)-4-(2-acetamido-2-carboxyethylthio)-N claim 24 ,N claim 24 ,N-trimethyl-4-oxo-2-(propionyloxy)butan-1-aminium.42. The compound ...

SUBSTITUTED N-ACETYL-L-CYSTEINE DERIVATIVES AND RELATED COMPOUNDS

Novel substituted N-acetyl-L-cysteine (NAC) derivatives and related compounds and methods of using these compounds for the treatment of diseases and/or conditions, including but not limited to diseases and/or conditions of, or involving, the Central Nervous System (CNS), including schizophrenia adrenoleukodystrophy, mitochondrial diseases (e.g. Leigh syndrome, Alpers' disease, and MELAS), Huntington's disease, trichotillomania, HIV-associated neurocognitive disorder, hypoxic-ischemic encephalopathy, drug craving, and drug addiction. 2. A pharmaceutical composition comprising the compound of and a pharmaceutically acceptable carrier.3. A pharmaceutical composition comprising a therapeutically effective amount of the compound of and a pharmaceutically acceptable carrier.4. A method of treating a central nervous system (CNS) disorder or condition selected from the group consisting of trichotillomania claim 1 , schizophrenia claim 1 , drug addiction claim 1 , inherited mitochondrial disease claim 1 , adrenoleukodystrophy claim 1 , Huntington's disease claim 1 , HIV-associated neurocognitive disorder claim 1 , and hypoxic-ischemic encephalopathy comprising administering a therapeutically effective amount of the compound of to a subject in need thereof.5. The method of claim 4 , wherein the CNS disorder or condition is trichotillomania.6. The method of claim 4 , wherein the CNS disorder or condition is schizophrenia.7. The method of claim 4 , wherein the CNS disorder or condition is drug addiction.8. The method of claim 4 , wherein the CNS disorder or condition is an inherited mitochondrial disease.9. The method of claim 8 , wherein the inherited mitochondrial disease is (a) Leigh syndrome claim 8 , (b) Alpers' disease claim 8 , or (c) mitochondrial encephalomyopathy claim 8 , lactic acidosis claim 8 , and stroke-like episodes (MELAS).10. The method of claim 4 , wherein the CNS disorder or condition is adrenoleukodystrophy claim 4 , Huntington's disease claim 4 , HIV- ...

METHOD FOR PRODUCING POLYTHIOL COMPOUND, METHOD FOR PRODUCING CURABLE COMPOSITION, AND METHOD FOR PRODUCING CURED PRODUCT

A method for producing a polythiol compound, the method including reacting a halide represented by Formula (1) with an alkali metal compound selected from the group made of an alkali metal sulfide and an alkali metal hydroxide to obtain a polyol compound selected from the group made of a polyol compound represented by Formula (2) and a polyol compound represented by Formula (3), in which a content of iron in the alkali metal compound is 100 ppm or less on a mass basis. 2. The method for producing a polythiol compound according to claim 1 , wherein the alkali metal compound is sodium sulfide.3. The method for producing a polythiol compound according to claim 1 , wherein the polythiol salt is a salt selected from the group consisting of a polythiol alkali metal salt and a polythiol ammonium salt.4. A method for producing a curable composition claim 1 , the method comprising:{'claim-ref': {'@idref': 'CLM-00001', 'claim 1'}, 'producing a polythiol compound by the production method according to ; and'}mixing the produced polythiol compound with a polyiso(thio)cyanate compound to prepare a curable composition.5. A method for producing a cured product claim 1 , the method comprising:{'claim-ref': {'@idref': 'CLM-00004', 'claim 4'}, 'producing a curable composition by the production method according to ; and'}curing the produced curable composition to obtain a cured product.6. The method for producing a cured product according to claim 5 , wherein the curing the produced curable composition to obtain a cured product is performed by subjecting the curable composition to cast polymerization.7. The method for producing a cured product according to claim 5 , wherein the cured product is a spectacle lens substrate. The present invention relates to a method for producing a polythiol compound, a method for producing a curable composition, and a method for producing a cured product.A polythiol compound is widely used as a synthetic raw material for obtaining various resins. For ...

NEW PROCESS

A process for the preparation of a compound of formula (I): 2. A process according to claim 1 , wherein the coupling reaction is carried out in the presence of a secondary amine.3. A process according to claim 2 , wherein Ris pent-3-yl.9. A process according to claim 1 , wherein the coupling reaction is followed by a mineral acid quenching with hydrofluoric acid claim 1 , hydrochloric acid claim 1 , boric acid claim 1 , acetic acid claim 1 , formic acid claim 1 , nitric acid claim 1 , phosphoric acid or sulfuric acid.10. A process according to claim 1 , wherein the coupling reaction is followed by a hydrochloric acid quenching.11. A process according to claim 1 , wherein a nonprotic solvent is present.12. A process according to claim 11 , wherein the nonprotic solvent is tetrahydrofuran.13. A process according to claim 11 , wherein the alkylating agent is 1-halo-CHRor a sulfonate ester of RCH—OH wherein Ris defined in .14. A process according to claim 1 , wherein the alkylating agent is 1-halo-2-ethylbutane.15. A process according to claim 1 , wherein the alkylating agent is 2-ethyl-1-butanol.16. A process according to claim 1 , wherein the alkylating agent is 1-bromo-2-ethylbutane.17. A process according to claim 1 , wherein the Grignard reagent is a (C-C)alkyl-magnesium-halide claim 1 , phenyl-magnesium-halide claim 1 , heteroaryl-magnesium-halide or a (C-C)cycloakyl-magnesium-halide.18. A process according to claim 1 , wherein the Grignard reagent is methylmagnesiumchloride.19. A process according to claim 2 , wherein the secondary amine is diethylamine or diisopropylamine.20. A process according to claim 2 , wherein the secondary amine is diethylamine.21. A process according to claim 2 , wherein the secondary amine is in a catalytic amount.22. A process according to claim 2 , wherein 0.01 to 0.5 equivalents of the secondary amine is used.23. A process according to claim 2 , wherein the process is continuous.24. A process according to claim 8 , wherein the ...

Lipids for the delivery of active agents

The present invention relates to novel cationic lipids that can be used in combination with other lipid components such as cholesterol and PEG-lipids to form lipid nanoparticles with oligonucleotides, to facilitate the cellular uptake and endosomal escape, and to knockdown target mRNA both in vitro and in vivo. The invention also relates to lipid particles comprising a neutral lipid, a lipid capable of reducing aggregation, a cationic lipid of the present invention, and optionally, a sterol. The lipid particle may further include a therapeutic agent such as a nucleic acid.

PHARMACEUTICAL COMPOSITIONS FOR THE TREATMENT OF LEFT VENTRICULAR DIASTOLIC DYSFUNCTION COMPRISING AN APOLIPOPROTEIN PEPTIDE/PHOSPHOLIPID COMPLEX

The present invention features pharmaceutical compositions and methods of using pharmaceutical compositions for treating left ventricular diastolic dysfunction. In particular, the pharmaceutical compositions include an apolipoprotein complex comprising a lipid fraction and a protein fraction. 1. A pharmaceutical composition for the treatment of left ventricular diastolic dysfunction (LVDD) comprising a CETP inhibitor selected from:propanethioic acid, 2-methyl-, S-[2-[[[1-(2-ethylbutyl)cyclohexyl]carbonyl]amino]phenyl]ester (Dalcetrapib),S-[2-(1-isopentylcyclohexanecarbonylamino)phenyl]2,2-dimethylthiopropionate;S-[2-(1-isopentylcyclohexanecarbonylamino)phenyl]2-acetylamino-3-phenylthiopropionate;S-[2-(1-isopentylcyclohexanecarbonylamino)phenyl]3-pyridinethiocarboxylate;S-[2-(1-isopentylcyclohexanecarbonylamino)phenyl]chlorothioacetate;S-[2-(1-isopentylcyclohexanecarbonylamino)phenyl]methoxythioacetate;S-[2-(1-isopentylcyclohexanecarbonylamino)phenyl]thiopropionate;S-[2-(1-isopentylcyclohexanecarbonylamino)phenyl]phenoxy-thioacetate;S-[2-(1-isopentylcyclohexanecarbonylamino)phenyl]2-methylthiopropionate;S-[2-(1-isopentylcyclohexanecarbonylamino)phenyl]4-chlorophenoxythioacetate;S-[2-(1-isopentylcyclohexanecarbonylamino)phenyl]cyclopropanethiocarboxylate;S-[2-(1-isopentylcyclohexanecarbonylamino)phenyl]2-acetylamino-4-carbamoylthiobutyrate;S-[2-(1-isopentylcyclohexanecarbonylamino)phenyl]2-hydroxy-2-methylthiopropionate;S-[2-(1-isopentylcyclopentanecarbonylamino)phenyl]2,2-dimethylthiopropionate;S-[2-(1-isopentylcyclopentanecarbonylamino)phenyl]thioacetate;S-[4,5-dichloro-2-(1-isopentylcyclohexanecarbonylamino)-phenyl]2,2-dimethylthiopropionate;S[4,5-dichloro-2-(1-isopentylcyclopentanecarbonylamino)-phenyl]2,2-dimethylthiopropionate;S-[2-(1-isopentylcyclohexanecarbonylamino)-4-trifluoromethylphenyl]2,2-dimethylthiopropionate;O-methyl S-[2-(1-isopentylcyclohexanecarbonylaminophenyl monothiocarbonate;S-[2-(1-methylcyclohexanecarbonylamino)phenyl]S-phenyldithiocarbonate; ...

Novel chain transfer agent and emulsion polymerization using the same

To provide a novel compound having both a surface-activating ability and a polymerization controlling ability. A compound represented by the following general formula (1) or (2): wherein, R 1 and R 3 are an organic group having the hydrophile-lipophile balance (HLB) determined by Griffin's method of 3 or more. The definitions of R 1 , R 2 , R 3 , R 4 , Z, p and q are described in the Description.

RETINOIC ACID RECEPTOR ANTAGONISTS AS CHAPERONE-MEDIATED AUTOPHAGY MODULATORS AND USES THEREOF

Compounds, compositions and methods are provided for selectively activating chaperone-mediated autophagy (CMA), protecting cells from oxidative stress, proteotoxicity and lipotoxicity, and/or antagonizing activity of retinoic acid receptor alpha (RARα) in subjects in need thereof. 118-. (canceled)2027-. (canceled)30. The compound of claim 29 , wherein any one or more alkyl is C1-C3 alkyl independently of any other alkyl.33. A method of selectivity activating chaperone-mediated autophagy (CMA) in a subject in need thereof claim 31 , comprising administering to the subject a compound or salt of claim 31 , in an amount effective to activate CMA claim 31 ,wherein the subject has Parkinson's Disease, Huntington's Disease, frontotemporal dementia, retinal degeneration, multiple sclerosis, diabetes, a lysosomal storage disorder, a retinal disease, a cardiovascular disease, mycardial infarcation, cardiac hypertrophy, or a cardiomyopathy.34. The method of claim 33 , wherein the subject has reduced CMA compared to a normal subject prior to administering the compound.35. A method of protecting cells from oxidative stress claim 31 , proeotoxicity claim 31 , and/or lipotoxicity in a subject in need thereof claim 31 , comprising administering to the subject a compound or salt claim 31 , in an amount effective to protect cells from oxidative stress claim 31 , proeotoxicity claim 31 , and/or lipotoxicity claim 31 ,wherein the subject has Parkinson's Disease, Huntington's Disease, frontotemporal dementia, retinal degeneration, multiple sclerosis, diabetes, a lysosomal storage disorder, a retinal disease, a cardiovascular disease, mycardial infarcation, cardiac hypertrophy, or a cardiomyopathy.36. The method of claim 35 , wherein the cells being protected comprise cardiac cells claim 35 , liver cells neurons claim 35 , myocytes claim 35 , fibroblasts claim 35 , and/or immune cells.37. A method of antagonizing activity of retinoic acid receptor alpha (RARα) in need thereof comprising ...

ADMINISTRATION OF A BIS(THIOHYDRAZIDE AMIDE) COMPOUND FOR TREATING CANCERS

Administration of a bis(thiohydrazide amide) compound is found to be surprisingly effective at treating subjects with cancer. Methods of treating a subject with cancer comprising continuously administering a bis(thiohydrazide amide) compound, or administering a bis(thiohydrazide amide) compound such that a constant concentration of the compound is achieved in the subject, are disclosed. 2. The method of claim 1 , wherein the cancer is selected from the group consisting of:i) human sarcoma or carcinoma, selected from the group consisting of fibrosarcoma, myxosarcoma, liposarcoma, chondrosarcoma, osteogenic sarcoma, chordoma, angiosarcoma, endotheliosarcoma, lymphangio sarcoma, lymphangioendotheliosarcoma, synovioma, mesothelioma, Ewing's tumor, leiomyosarcoma, rhabdomyosarcoma, anal carcinoma, esophageal cancer, gastric cancer, hepatocellular cancer, bladder cancer, endometrial cancer, pancreatic cancer, breast cancer, ovarian cancer, prostate cancer, stomach cancer, atrial myxomas, squamous cell carcinoma, basal cell carcinoma, adenocarcinoma, sweat gland carcinoma, sebaceous gland carcinoma, thyroid and parathyroid neoplasms, papillary carcinoma, papillary adenocarcinomas, cystadenocarcinoma, medullary carcinoma, bronchogenic carcinoma, hepatoma, bile duct carcinoma, choriocarcinoma, seminoma, embryonal carcinoma, Wilms' tumor, cervical cancer, testicular tumor, lung carcinoma, small cell lung carcinoma, bladder carcinoma, epithelial carcinoma, glioma, pituitary neoplasms, astrocytoma, medulloblastoma, craniopharyngioma, ependymoma, pinealoma, hemangioblastoma, acoustic neuroma, schwannomas, oligodendroglioma, meningioma, spinal cord tumors, melanoma, neuroblastoma, pheochromocytoma, Types 1-3 endocrine neoplasia, retinoblastoma; andii) leukemia, selected from the group consisting of acute lymphocytic leukemia, acute myelocytic leukemia; chronic leukemia, polycythemia vera, multiple myeloma, Waldenstrobm's macroglobulinemia, heavy chain disease, T-cell leukemias, B ...

THIOCARBONYLTHIO COMPOUNDS AS CHAIN TRANSFER AGENTS SUITABLE FOR RAFT POLYMERIZATION

The present invention relates to a compound having the structure of formula (I), wherein R, R, R, R, R, R, and Rare as described herein. The present invention also relates to a process for the preparation of a compound of formula (I) and to a process for the synthesis of a polymer using the compound of formula (I) through controlled free radical polymerization. 4. The process according to claim 3 , wherein Ais selected from the group consisting of K claim 3 , Na claim 3 , Li claim 3 , triethyl ammonium cation claim 3 , and piperidinium cation.6. The process according to claim 5 , wherein X is a halogen.7. The process according to claim 6 , wherein X is Cl.9. The process according to claim 8 , wherein Ais selected from the group consisting of K claim 8 , Na claim 8 , Li claim 8 , triethyl ammonium cation claim 8 , and piperidinium cation.10. The process according to claim 8 , wherein said forming the first intermediate compound of formula (II) comprises:reacting the second intermediate compound of formula (IV) with carbon disulfide under conditions effective to produce the first intermediate compound of formula (II).11. The process according to further comprising: {'br': None, 'sup': '1', 'RH\u2003\u2003(V), and'}, 'providing a compound of formula (V)reacting the compound of formula (V) with a base to form the second intermediate compound of formula (IV).12. The process according to claim 11 , wherein the base is selected from the group consisting of KPO*xHO claim 11 , NaPO*xHO claim 11 , LiPO claim 11 , NaH claim 11 , EtN claim 11 , piperidine claim 11 , morpholine claim 11 , alkali hydroxides; and wherein x is 0 to 10.13. The process according to claim 12 , wherein the base is KPO*3HO.17. The process of claim 14 , wherein said monomer composition comprises one or more monomers.18. The process of claim 17 , wherein the one or more monomers is selected from the group consisting of vinyl aromatics and acrylate.19. The process of claim 17 , wherein the one or more ...

POLYTHIOLS WITH CARBAMATE GROUPS

The present invention discloses polythiol compositions containing sulfur-containing compounds with carbamate groups, and to methods for producing such polythiol compositions. These polythiol compositions can be synthesized via the reaction of an isocyanate with an allyl ether alcohol, followed by thiolation with HS, and these polythiol compositions are often used in formulations for adhesives, paints, and coatings. 2. The composition of claim 1 , wherein:{'sub': 3', '15, 'each R independently is a Cto Calkane group;'}{'sup': '1', 'sub': 5', '20, 'each Rindependently is a substituted or unsubstituted Cto Ccycloalkane group;'}n is an integer from 2 to 4; andm is an integer from 0 to 4, wherein an average value of m in the composition is from greater than 0 to 2.3. The composition of claim 1 , wherein:{'sub': 3', '12, 'each R is the same and is a Cto Calkane group;'}{'sup': '1', 'sub': 6', '12, 'each Ris the same and is a substituted or unsubstituted Cto Ccycloalkane group;'}n is an integer from 2 to 4; andm is an integer from 0 to 3, wherein an average value of m in the composition is from greater than 0 to 1.4. The composition of claim 3 , wherein n is equal to 2.5. The composition of claim 1 , wherein the sulfur-containing compounds are characterized by:an average thiol sulfur to sulfide sulfur molar ratio in a range from 2:1 to 500:1;an average of from 0.05 wt. % to 10 wt. % sulfide sulfur;an average of from 12.5 wt. % to 16.2 wt. % thiol sulfur;a thiol equivalent weight in a range from 198 to 300 g/eq; andan average thiol functionality in a range from 4.05 to 6.6. The composition of claim 1 , wherein the sulfur-containing compounds are characterized by:an average thiol sulfur to sulfide sulfur molar ratio in a range from 3:1 to 100:1;an average of from 0.1 wt. % to 5 wt. % sulfide sulfur;an average of from 13 wt. % to 16 wt. % thiol sulfur;a thiol equivalent weight in a range from 200 to 250 g/eq; andan average thiol functionality in a range from 4.05 to 5.7. The ...

Thioether-containing phenolic compounds

Thioether-substituted phenols that are the reaction product of a thioether-substituted alcohol or thioether-substituted amine and a phenol with at least one pendant acyl group and have a ratio of sulfur groups to phenol groups of at least 1:1 and uses for thioether-substituted phenols. Methods of lubricating an internal combustion engine by contacting the internal combustion engine with a lubricating composition comprising a thioether-substituted phenol. Methods of reducing deposit formation and/or corrosion in an engine using a lubricating composition comprising a thioether-substituted phenol.

Polymorphs of n-malonyl-bis(n`-methyl-n`-thiobenzoylhydrazide)

At least 70% by weight of Compound 1 is the single crystalline form, Form A, Form C, or Form D, of the compound. A pharmaceutical composition comprises a pharmaceutically acceptable carrier or diluent, and compound 1, wherein at least 70% by weight of the compound is the single crystalline form, Form A, Form C, or Form D, of the compound. A method of treating a subject with cancer comprises administering to the subject an effective amount of compound 1 or the pharmaceutical composition.

OXIME SULFONATE DERIVATIVES

Oxime sulfonate compounds of the formula (I), wherein Ris O(CO)R, COORor CONRR; n is 1 or 2; Rfor example is C-Calkyl, C-Ccycloalkyl or benzyl; Ris for example C-Calkyl, C-Ccycloalkyl, C-Chaloalkyl, C-Calkenyl, benzyl, phenyl or naphthyl, which optionally are substituted; Ris for example C-Calkyl, C-Ccycloalkyl, C-Chaloalkyl, C-Calkenyl, benzyl, phenyl or naphthyl, which optionally are substituted; Ris for example C-Calkyl, C-Ccycloalkyl, C-Calkenyl, C-Calkyl which is substituted for example by one or more halogen; or Ris phenyl or naphthyl, which are unsubstituted; Rand Reach independently of one another for example are hydrogen, C-Calkyl, C-Chaloalkyl, phenyl-C-Calkyl, C-Calkenyl or C-Ccycloalkyl, phenyl or naphthyl; or Rand R, together with the N-atom to which they are attached, form a 5- or 6-membered ring; are suitable as thermal radical initiators. 2. The compound according to claim 1 , wherein{'sub': 1', '4', '5', '6', '7, 'Ris O(CO)R, COORor CONRR,'}n is 1 or 2;{'sub': 2', '1', '4, 'Ris C-Calkyl or benzyl;'}{'sub': 3', '1', '6, 'Ris benzyl, phenyl or phenyl substituted by one or more C-Calkyl;'}{'sub': 4', '1', '6, 'Ris benzyl, phenyl or phenyl substituted by one or more C-Calkyl;'}{'sub': 5', '3', '18', '3', '12, 'Ris C-Calkyl or C-Ccycloalkyl,'}{'sub': 5', '2', '12, 'or Ris C-Calkyl which is interrupted by one or more O,'}{'sub': 5', '1', '6', '1', '6', '2', '2', '1', '12, 'or Ris C-Calkyl substituted by phenylsulfanyl, phenoxy, N(C-Calkyl), N(phenyl), phthalimido, phenyl or phenyl substituted by one or more C-Calkyl;'}{'sub': 6', '7', '1', '6', '6', '7, 'Rand Reach independently are hydrogen, C-Calkyl or phenyl, or together with the N-atom to which Rand Rare attached form a morpholino ring.'}3. The compound according to claim 1 , wherein{'sub': 1', '4', '5', '6', '7, 'Ris O(CO)R, COORor CONRR;'}n is 1 or 2{'sub': '2', 'Ris methyl, ethyl or benzyl'}{'sub': 3', '1', '6, 'Ris benzyl, phenyl or phenyl substituted by C-Calkyl;'}{'sub': 4', '1', '6, 'Ris benzyl ...

ANTIVIRAL COMPOUNDS AND METHODS

The invention relates to compounds having antiviral and methods utilizing the compounds to treat viral infections. 1168-. (canceled)170. The method according to wherein the compound is selected from the group consisting of:(2-Bromocinnamoyl)guanidine,(2-Chlorocinnamoyl)guanidine,(2-Furanacryloyl)guanidine,(2-Methoxycinnamoyl)guanidine,(2-Nitrocinnamoyl)guanidine,(3-Bromocinnamoyl)guanidine,(3-Chlorocinnamoyl)guanidine,(3-Methoxycinnamoyl)guanidine,(3-Nitrocinnamoyl)guanidine,(3-phenylpropanoyl)guanidine,(4-Bromocinnamoyl)guanidine,(4-Chlorocinnamoyl)guanidine,(4-Hydroxycinnamoyl)guanidine,(4-Methoxycinnamoyl)guanidine,(4-Phenoxybenzoyl)guanidine,(5-Phenyl-penta-2,4-dienoyl)guanidine,(a-Methylcinnamoyl)guanidine,(Phenylacetyl)guanidine,(Quinoline-2-carbonyl)guanidine,(trans-2-Phenylcyclopropanecarbonyl)guanidine,[(4-Chlorophenoxy-acetyl]guanidine,[(E)-3-(4-Dimethylaminophenyl)-2-methylacryloyl]guanidine,[3-(3-Pyridyl)acryloyl]guanidine,1-bromo-2-naphthoylguanidine,1-naphthoylguanidine,2-(1-naphthyl)acetoylguanidine,2-(2-naphthyl)acetoylguanidine,2-(cyclohex-1-en-lyl)cinnamoylguanidine,2-(trifluoromethyl)cinnamoylguanidine,2,3,5,6-tetramethylcinnamoylguanidine,2,3-difluorocinnamoylguanidine,2,3-dimethylcinnamoylguanidine,2,4,6-trimethylcinnamoylguanidine,2,4-dichlorocinnamoylguanidine,2,5-dimethylcinnamoylguanidine,2,6-dichlorocinnamoylguanidine,2′4 DichloroBenazamil HCl,2-chloro-6-fluorocinnamoylguanidine,2-cyclohexylcinnamoylguanidine,2-ethoxycinnamoylguanidine,2-ethylcinnamoylguanidine,2-fluorocinnamoylguanidine,2-methylcinnamoylguanidine,2-naphthoylguanidine,2-phenylcinnamoylguanidine,2-t-butylcinnamoylguanidine,3-(2-naphthyl)acryloylguanidine,3-(cyclohex-1-en-1-yl)cinnamoylguanidine,3-(trans-hept-1-en-1-yl)cinnamoylguanidine,3-(trifluoromethoxy)cinnamoylguanidine,3-(trifluoromethyl)cinnamoylguanidine,3,4-(methylenedioxy)cinnamoylguanidine,3,4,5-trimethoxycinnamoylguanidine,3,4-dichlorocinnamoylguanidine,3,4-difluorocinnamoylguanidine,3-ethoxycinnamoylguanidine,3- ...

Method for Producing Carboxylic Acid Thioester

According to the present invention, there is provided a method for producing carboxylic acid thioester, comprising reacting a compound represented by the following formula (I), carboxylic acid and thiol in the presence of a catalyst including at least one Group 2 metal compound. The production method is a production method which is simple in reaction operation, which places a small load on the environment and the human body and which enables carboxylic acid thioester to be catalytically obtained at a high yield even at a normal temperature and a normal pressure (25° C., 1 atm). In the formula (I), R 1 and R 2 each independently represent a hydrocarbon group having 1 to 20 carbon atoms.

SULPHUR CONTAINING HIGH REFRACTIVE INDEX MONOMER

This invention discloses aromatic based sulfur containing hydrophobic acrylate monomer with high refractive index. The invention further discloses process for the preparation of 2-phenyl-2-(phenylthio)ethyl acrylate of the formula (I). This monomer can be polymerized to take the form of an optical products having high refractive index. Optical products made from this monomer having high refractive index can be thinner and provide same refractive power as product made from a material having a relatively low refractive index. In particular the polymeric material prepared from the novel monomer can be used for making intraocular lenses that are thinner than the conventionally used ones offering advantages of reduced volume of space and light weight materials. 2. The compound as claimed in claim 1 , wherein a refractive index of the compound is 1.584.4. The process as claimed in step (i) and step (iii) of claim 3 , wherein the solvent is selected from the group consisting of water claim 3 , esters claim 3 , ketones claim 3 , ethers claim 3 , alcohols claim 3 , aromatic hydrocarbons claim 3 , haloalkanes claim 3 , heterocyclic compounds and combinations thereof.5. The process as claimed in claim 4 , wherein the solvent is selected from the group consisting of dichloromethane claim 4 , tetrahydrofuran claim 4 , toluene claim 4 , ethyl methyl ketone claim 4 , chloroform claim 4 , ethyl acetate petroleum ether and combinations thereof.6. The process as claimed in step (i) of claim 3 , wherein the solvent is 1 to 10 times claim 3 , preferably 1 to 5 times by weight with respect to the total amount of the acryloyl chloride and the 2-phenyl-2-(phenylthio)ethanol.7. The process as claimed in claim 3 , wherein the dehydrohalogenating agent is selected from the group consisting of triethylamine claim 3 , trimethylamine claim 3 , pyridine claim 3 , sodium carbonate claim 3 , potassium carbonate and combinations thereof.8. The process as claimed in claim 3 , wherein the ...

CREATINE ANALOGS AND THE USE THEREOF

The present invention provides novel creatine analogs useful for treating any creatine deficiency disorders and methods of treating and preventing creatine deficiencies utilizing the present compounds and the pharmaceutical compositions or formulations thereof. Certain embodiments seek to increase the lipophilicty of novel creatine analogs with the goal of improving their bioavailability. 2. The compound of claim 1 , when Ris not hydrogen claim 1 , then at least one of Rand Ris hydrogen.3. The compound of or claim 1 , which demonstrates increased hydrophobicity or increased uptake by a carrier-mediated transporter as compared to the uptake of creatine claim 1 , wherein the carrier-mediated transporter is selected from the group consisting of amino acid transporter claim 1 , monocarboxylic acid transporter claim 1 , small peptide transporter claim 1 , glucose transporter claim 1 , glutathione transporter claim 1 , ascorbic acid transporter claim 1 , and nucleoside transporter.5. The compound of claim 4 , wherein Rand Rare both hydrogen.6. The compound of claim 5 , wherein X is O or NH; and Zis an amino acid residue.7. The compound of claim 5 , wherein X is O or NH; and Zis a dipeptide residue or a tripeptide residue.8. The compound of claim 4 , wherein{'sup': 1', '4', '4, 'Ris —C(O)—NH—R, or —C(O)—O—R;'}{'sup': '2', 'Ris hydrogen;'}{'sup': '4', 'Ris alkyl, substituted alkyl, alkenyl, substituted alkenyl, alkynyl, substituted alkynyl, heteroalkyl, substituted heteroalkyl, aryl, substituted aryl, heteroaryl, substituted heteroaryl, carbocyclyl, substituted carbocyclyl, heterocyclyl, substituted heterocyclyl;'}X is O or NH;{'sup': '1', 'Lis alkylene, substituted alkylene, arylene, substituted arylene; aralkylene, or substituted aralkylene; and'}{'sup': '1', 'Zis OH.'}9. The compound of claim 4 , wherein{'sup': '1', 'Ris hydrogen;'}{'sup': 2', '5', '5, 'Ris —C(O)—NH—R, or —C(O)—O—R;'}{'sup': '5', 'Ris alkyl, substituted alkyl, alkenyl, substituted alkenyl, alkynyl, ...

Dye-Sensitized Solar Cell

The purpose of the present invention is to provide a dye-sensitized solar cell which has excellent photoelectric conversion efficiency and excellent durability. Disclosed is a dye-sensitized solar cell which comprises: a first conductive supporting body which has a semiconductor-containing layer that is sensitized by a dye; a second conductive supporting body which has a counter electrode and is disposed at a position where the semiconductor-containing layer and the counter electrode face each other at a predetermined distance; a charge transfer layer which is sandwiched between the first and second conductive supporting bodies; and a sealing agent which is provided in the peripheral portions of the first and second conductive supporting bodies for the purpose of sealing the charge transfer layer. The dye is an organic non-ruthenium dye; the counter electrode contains platinum; and the charge transfer layer is composed of an electrolyte solution that contains iodine, iodine ions and a compound which has both a thioester bond and a positively charged nitrogen atom in each molecule. 1. A dye-sensitized solar cell comprising: a first conductive support having a dye-sensitized semiconductor-containing layer; a second conductive support having a counter electrode provided in a position where the semiconductor-containing layer and the counter electrode are opposite to each other at a predetermined interval; a charge transfer layer sandwiched in a gap between the first and the second conductive supports; and a sealing agent provided in a peripheral part of the first and the second conductive supports in order to seal the charge transfer layer , wherein the dye is an organic non-ruthenium dye; the counter electrode contains platinum; and the charge transfer layer comprises an electrolyte solution containing iodine , iodide ions , and a compound having , in a molecule thereof , both a thioester bond and a positively charged nitrogen atom.3. The dye-sensitized solar cell ...

Beta-Mercaptoethanol Synthesis

A process includes reacting, in a reactor having a fixed bed containing a solid catalyst which contains a heterogeneous ion exchange resin, hydrogen sulfide and ethylene oxide in the presence of the solid catalyst to yield a reaction product which contains beta-mercaptoethanol. A reactor system includes the reactor, an ethylene oxide stream, a hydrogen sulfide stream, a fixed bed containing the solid catalyst placed in the reactor, and an effluent stream containing the reaction product. During steady state operation of the reactor in the process and the reactor system, the hydrogen sulfide and the ethylene oxide are present in a mole ratio in a range of about 9:1 to about 20:1. 1. A reactor system for producing beta-mercaptoethanol , comprising:a reactor;an ethylene oxide stream feeding ethylene oxide to the reactor;a hydrogen sulfide stream feeding hydrogen sulfide to the reactor;a fixed bed containing a solid catalyst placed in the reactor; andan effluent stream flowing from the reactor, wherein the effluent stream comprises a reaction product comprising beta-mercaptoethanol yielded in the reactor by a reaction of hydrogen sulfide and ethylene oxide in presence of the solid catalyst;wherein the solid catalyst comprises a heterogeneous ion exchange resin, andwherein the hydrogen sulfide and the ethylene oxide are present in the reactor during steady state operation in a mole ratio ranging from about 9:1 to about 20:1.2. The reactor system of claim 1 , which includes no internal and/or external source for cooling the reactor.3. The reactor system of claim 1 , wherein the fixed bed of the solid catalyst comprises a top zone claim 1 , a middle zone claim 1 , and a bottom zone; and wherein the top zone includes about 66% of a chemically inert solid diluent and about 33% solid catalyst by volume claim 1 , the middle zone includes about 50% of the chemically inert solid diluent and about 50% solid catalyst by volume claim 1 , and the bottom zone includes 100% solid ...

NOVEL BENZYLAMIDE COMPOUND, METHOD FOR PRODUCING THE SAME, AND MITICIDE

An object of the present invention is to provide a benzylamide compound or a salt thereof that controls a mite. The present invention provides a benzylamide compound represented by Formula (1): or a salt thereof, wherein Rrepresents Calkyl or Chaloalkyl; Rand Rare identical or different and each represent hydrogen, halogen, cyano, nitro, Calkyl, or the like; Rrepresents hydrogen, formyl Calkyl, or the like; Rand Rare identical or different and each represent hydrogen, halogen, or Calkyl, or the like; R, R, R, R, and Rare identical or different and each represent hydrogen, halogen, or the like; X represents oxygen or sulfur; and n represents an integer of 0 to 2. 2. The benzylamide compound or the salt thereof according to claim 1 , wherein Ris Chaloalkyl.3. The benzylamide compound or the salt thereof according to or claim 1 , wherein Rand Rare identical or different and each represent halogen claim 1 , cyano claim 1 , or Calkyl.4. The benzylamide compound or the salt thereof according to any one of to claim 1 , wherein Ris hydrogen claim 1 , or Calkyl.5. The benzylamide compound or the salt thereof according to any one of to claim 1 , wherein R claim 1 , R claim 1 , R claim 1 , R claim 1 , and Rare identical or different and each represent hydrogen claim 1 , halogen claim 1 , nitro claim 1 , Calkyl claim 1 , Chaloalkyl claim 1 , Calkoxy claim 1 , Chaloalkoxy claim 1 , Calkylsulfonyl claim 1 , Chaloalkylsulfonyl claim 1 , Calkylsulfinyl claim 1 , Chaloalkylsulfinyl claim 1 , Calkylthio claim 1 , Chaloalkylthio claim 1 , substituted or unsubstituted amino claim 1 , aryl claim 1 , or heterocyclic.10. A pesticide containing the benzylamide compound or the salt thereof of according to any one of to .11. A miticide containing the benzylamide compound or the salt thereof of according to any one of to . The present invention relates to a novel benzylamide compound, method for producing the same, and miticide containing the compound.Due to the emergence of mites resistant ...

ETHYNYL COMPOUNDS, THEIR PREPARATION AND THEIR THERAPEUTIC USE FOR THE TREATMENT OF MALARIA

The present disclosure relates to compounds of formula (I) or a pharmaceutically acceptable salt thereof wherein Rmeans a fluorine atom or a perhalogeno linear alkyl radical containing 1, 2 or 3 carbon atoms; Rmeans a chlorine atom, a linear alkyl radical containing 1, 2 or 3 carbon atoms or a perhalogeno linear alkyl radical containing 1, 2 or 3 carbon atoms, and R means a hydrogen atom or a radical of formula (Ia). The present disclosure also relates to processes for their preparation as well their therapeutic uses, in particular such as for use in the treatment of malaria. 120-. (canceled)22. The compound according to claim 21 , wherein Ris a fluorine atom or a trifluoromethyl radical.23. The compound according to claim 21 , wherein Ris a chlorine atom claim 21 , a methyl radical or a perhalogeno linear alkyl radical containing 1 claim 21 , 2 or 3 carbon atoms.24. The compound according to claim 21 , wherein R is the radical of formula (Ia).25. The compound according to claim 21 , wherein R is a radical of formula (Ia) and Ris in position 5 or 6 of said radical of formula (Ia).26. The compound according to claim 21 , wherein R is the radical of formula (Ia) and Ris a hydrogen atom claim 21 , a hydroxyl radical or a methyl radical.27. The compound according to claim 25 , wherein R is the radical of formula (Ia) and Ris a hydroxyl radical in position 5 of said radical of formula (Ia).28. The compound according to claim 25 , wherein R is the radical of formula (Ia) and Ris a linear or branched alkyl radical containing 1 claim 25 , 2 or 3 carbon atoms in position 6 of said radical of formula (Ia).29. The compound according to claim 21 , wherein at least one of Rand Ris a perfluoromethyl radical.30. The compound according to claim 21 , wherein both Rand Rare a perfluoromethyl radical.31. The compound according to claim 21 , said compound being selected from:5-((3-(carbamimidoylcarbamoyl)-5-(trifluoromethyl)phenyl)ethynyl)-N-(pyridin-2-yl)-2-(trifluoromethyl)benzamide, ...

COMPOSITIONS AND METHODS FOR THE TREATMENT OF MUCOSITIS

The invention relates to the compounds of formula I or its pharmaceutical acceptable salts, as well as polymorphs, solvates, enantiomers, stereoisomers and hydrates thereof. The pharmaceutical compositions comprising an effective amount of compounds of formula I, and methods for the treatment of mucositis may be formulated for oral, buccal, rectal, topical, transdermal, transmucosal, intravenous, parenteral administration, syrup, or injection. Such compositions may be used to treatment of mucus diseases related to painful inflammation and ulceration of the digestive tract lining and in the mouth. 2. A pharmaceutical composition comprising a compound of and a pharmaceutically acceptable carrier.3. The pharmaceutical composition of claim 2 , wherein said pharmaceutical composition is formulated to treat the underlying etiology with an effective amount administering the patient in need by oral administration claim 2 , delayed release or sustained release claim 2 , transmucosal claim 2 , syrup claim 2 , topical claim 2 , parenteral administration claim 2 , injection claim 2 , subdermal claim 2 , oral solution claim 2 , rectal administration claim 2 , buccal administration or transdermal administration.4. A method of treating mucositis as the underlying etiology claim 3 , the method comprising administering to a patient in need thereof an effective amount of .5. The method of claim 4 , wherein the mucositis as the underlying etiology is selected from mucus diseases related to painful inflammation and ulceration of the digestive tract lining and in the mouth.6. The pharmaceutical composition of claim 2 , further comprising a molecular conjugate of 2-(2 claim 2 ,6-dichlorophenyl)guanidine and carboxylic acid compounds selected from a group consisting of R-Lipoic acid claim 2 , acetyl cysteine claim 2 , caprylic acid claim 2 , and salsalate.7. The molecular conjugate of claim 6 , wherein the carboxylic acid compound is R-Lipoic acid.8. The molecular conjugate of claim 6 , ...

Novel alkanethioic acid derivative and perfume composition containing the same

An alkanethioic acid derivative capable of imparting a characteristic aroma or flavor to fragrances and cosmetics, and foods and beverages; and a perfume composition comprising the alkanethioic acid derivative as an active ingredient. S-alkyl 5-[(1-alkoxy)ethoxy]alkanethioate represented by formula (1), and a perfume composition comprising the S-alkyl 5-[(1-alkoxy)ethoxy]alkanethioate represented by formula (1) as an active ingredient. In the formula (1), R1 represents an alkyl group having 1 to 9 carbon atoms, R2 represents an alkyl group having 2 to 4 carbon atoms, and R3 represents a methyl group or an ethyl group.

Thioamides and Amides for Controlling Animal Pests

The invention relates to the use of a compound of formula (I) 136-. (canceled)38. The method of claim 37 , wherein{'sup': 5', '5, 'Y is phenyl unsubstituted or substituted with 1, 2, 3, 4 or 5 substituents R; or naphthyl unsubstituted or substituted with 1 or 2 substituents R;'}{'sup': 6', '6', '6', '6, 'Q is phenyl unsubstituted or substituted with 1, 2, 3 or 4 substituents R; cyclohexyl unsubstituted or substituted with 1 or 2 substituents R; cyclopentyl unsubstituted or substituted with 1 or 2 substituents R; or a 6-membered aromatic heterocyclic ring containing 1, 2 or 3 nitrogen atoms in the ring, wherein the aforementioned ring is unsubstituted or substituted with 1, 2, 3 or 4 substituents R;'}{'sup': '1', 'sub': 1', '6', '2', '6', '2', '6', '3', '6', '1', '6', '1', '6', '3', '1', '6', '2', '6', '2', '6', '3', '6', '1', '6', '1', '6, 'Ris selected from the group consisting of H, halogen, cyano, C-C-alkyl, C-C-alkenyl, C-C-alkynyl, C-C-cycloalkyl or (C-C-alkoxy)carbonyl, wherein the five radicals last mentioned are unsubstituted or substituted with 1, 2 or 3 substituents selected from halogen, cyano, hydroxy, OSi(C-C-alkyl), C-C-alkyl, C-C-alkenyl, C-C-alkynyl, C-C-cycloalkyl, C-C-alkoxy and (C-C-alkoxy)carbonyl,'}wherein the six radicals last mentioned are unsubstituted or partially or fully halogenated;{'sup': '2', 'Ris selected from the group consisting of H and halogen;'}or{'sup': 1', '2, 'Rand Rform together with the carbon atom to which they are attached a methylene group;'}{'sup': '3', 'sub': 1', '6', '2', '6', '2', '6', '3', '6', '1', '6', '1', '6', '3', '1', '6', '2', '6', '2', '6', '3', '6', '1', '6', '1', '6, 'Ris selected from the group consisting of H, halogen, cyano, C-C-alkyl, C-C-alkenyl, C-C-alkynyl, C-C-cycloalkyl or (C-C-alkoxy)carbonyl, wherein the five radicals last mentioned are unsubstituted or substituted with 1, 2 or 3 substituents selected from halogen, cyano, hydroxy, OSi(C-C-alkyl), C-C-alkyl, C-C-alkenyl, C-C-alkynyl, C-C-cycloalkyl ...

SUBSTITUTED N-ACETYL-L-CYSTEINE DERIVATIVES AND RELATED COMPOUNDS

Novel substituted N-acetyl-L-cysteine (NAC) derivatives and related compounds and methods of using these compounds for the treatment of diseases and/or conditions, including but not limited to diseases and/or conditions of, or involving, the Central Nervous System (CNS), including schizophrenia adrenoleukodystrophy, mitochondrial diseases (e.g. Leigh syndrome, Alpers' disease, and MELAS), Huntington's disease, trichotillomania, HIV-associated neurocognitive disorder, hypoxic-ischemic encephalopathy, drug craving, and drug addiction. 2. The method of claim 1 , wherein the compound of formula I is administered orally.3. The method of claim 1 , wherein the compound of formula I is administered rectally claim 1 , parenterally claim 1 , intracisternally claim 1 , intravaginally claim 1 , transdermally claim 1 , transmucosally claim 1 , sublingually claim 1 , pulmonarily claim 1 , intraperitoneally claim 1 , topically claim 1 , intranasally claim 1 , or bucally.4. The method of claim 1 , wherein the compound of formula I is administered in a solid form.5. The method of claim 1 , wherein the compound of formula I is administered in a capsule.6. The method of claim 1 , wherein the compound of formula I is administered in a soft gelatin capsule.7. The method of claim 1 , wherein the compound of formula I is administered in a hard gelatin capsule.8. The method of claim 1 , wherein the compound of formula I is administered as a tablet.9. The method of claim 1 , wherein the compound of formula I is administered with an enteric coating.10. The method of claim 1 , wherein the compound of formula I is administered in a solid form with an enteric coating.11. The method of claim 1 , wherein the compound of formula I is administered as an enteric formulation.12. The method of claim 1 , wherein the compound of formula I is administered in a composition that releases the compound in a delayed manner.13. The method of claim 1 , wherein the compound of formula I is administered in a ...

Propionic acids, propionic acid esters, and related compounds

The invention relates to compounds of the following formula: and their pharmaceutically acceptable salts, pharmaceutical compositions containing this compounds, and methods of using this compound for the treatment of various diseases or conditions, including but not limited to diseases and/or conditions of, or involving, the Central Nervous System (CNS), including schizophrenia adrenoleukodystrophy, mitochondrial diseases (e.g. Leigh syndrome, Alpers' disease, and MELAS), Huntington's disease, trichotillomania, HIV-associated neurocognitive disorder, hypoxic-ischemic encephalopathy, drug craving, and drug addiction.

PACLITAXEL ENHANCER COMPOUNDS

Disclosed is a compound represented by the Structural Formula (I): 1. A compound represented by the following structural formula:Y is a covalent bond, a phenylene group or a substituted or unsubstituted straight chained hydrocarbyl group, or, Y, taken together with both >C═Z groups to which it is bonded, is a substituted or unsubstituted aromatic group;{'sub': 1', '2, 'Rand Rare independently an aryl group or a substituted aryl group;'}{'sub': 3', '4, 'Rand Rare independently —H, an aliphatic group, a substituted aliphatic group, an aryl group or a substituted aryl group;'}{'sub': 5', '6, 'R-Rare independently —H, an aliphatic group, a substituted aliphatic group, an aryl group or a substituted aryl group; and'}Z is ═O or ═S;{'sub': 2', '3', '4', '5', '6', '1', '2, 'provided that when Y is —CH—, Rand Rare both phenyl and R-Rare all —H, then Rand Rare not both phenyl.'}or a pharmaceutically acceptable salt thereof, wherein: This application is a continuation of U.S. application Ser. No. 12/692,895, filed on Jan. 25, 2010, now U.S. Pat. No. 9,107,955, issuing on Aug. 18, 2015; which is a continuation of U.S. application Ser. No. 12/009,641, filed on Jan. 18, 2008, now U.S. Pat. No. 7,671,092, issued on Mar. 3, 2010; which is a continuation of U.S. application Ser. No. 11/244,324, filed on Oct. 5, 2005, now U.S. Pat. No. 7,345,094, issued on Mar. 18, 2008; which is a continuation of U.S. application Ser. No. 10/846,152, filed on May 14, 2004, now U.S. Pat. No. 7,037,940, issued on May 2, 2006; which is a continuation of U.S. application Ser. No. 10/193,075, filed on Jul. 10, 2002, now U.S. Pat. No. 6,800,660, issued on Oct. 5, 2004; which claims the benefit of U.S. Provisional Application No. 60/304,252, filed on Jul. 10, 2001, and U.S. Provisional Application No. 60/361,946, filed on Mar. 6, 2002. The entire teachings of all of these applications are incorporated herein by reference in their entirety.Many new drugs are now available to be used by oncologists in ...

Method for Synthesizing of Thioesters by Using Compound as Catalyst

A method for synthesizing of thioesters by using a compound as a catalyst is disclosed. The compound is represented by formula I below: 3. The method as in claim 2 , wherein one or more substituents of the substituted alkyl claim 2 , the substituted aryl claim 2 , and the substituted heteroaryl is selected from the group consisting of: a halogen atom claim 2 , a hydroxyl claim 2 , a cyano claim 2 , a nitro claim 2 , a thiohydroxy claim 2 , an amino claim 2 , a carbonyl claim 2 , a carbamoyl claim 2 , a sulfamoyl claim 2 , a Calkyl claim 2 , a C-Calkenyl claim 2 , a C-Calkynyl claim 2 , a C-Calkoxy claim 2 , Calkyl alcohol claim 2 , Chaloalkyl claim 2 , Chaloalkylthio claim 2 , Calkylamino claim 2 , Calkylamido claim 2 , Calkylsulfonyl claim 2 , Chaloalkylsulfonyl claim 2 , Calkoxycarbonyl claim 2 , Calkylcarbamoyl claim 2 , Caryl claim 2 , Ccycloalkyl claim 2 , Cheteroaryl claim 2 , and Cheterocycloalkyl.4. The method as in claim 2 , wherein Rin Formula I represents a substituted or unsubstituted phenyl claim 2 , a substituted or unsubstituted thienyl claim 2 , or a substituted or unsubstituted pyridinyl; One of X and Y is H and another is a Calkyl; and n is 2.5. The method as in claim 2 , wherein Rin Formula I represents a phenyl claim 2 , one of X and Y is H and another is methyl; and n is 2.7. The method as in claim 6 , wherein molar ratio of compound 1:compound 2:compound 3:catalyst is 1-1.5:1-1.5:1-1.5:0.1-0.5.8. The method as in claim 6 , wherein one or more substituents of the substituted alkyl claim 6 , the substituted alkoxy claim 6 , the substituted aryl claim 6 , and the substituted heteroaryl is selected from the group consisting of: a halogen atom claim 6 , a hydroxyl claim 6 , a cyano claim 6 , a nitro claim 6 , a thiohydroxy claim 6 , an amino claim 6 , a carbonyl claim 6 , a carbamoyl claim 6 , a sulfamoyl claim 6 , a Calkyl claim 6 , a C-Calkenyl claim 6 , a C-Calkynyl claim 6 , a C-Calkoxy claim 6 , Calkyl alcohol claim 6 , Chaloalkyl claim 6 , ...

AROMATIC AMIDES HAVING A FUNGICIDAL ACTIVITY, THEIR AGRONOMIC COMPOSITIONS AND RELATIVE PREPARATION METHOD

Aromatic amides are described, having general formula (I): 2. The amide according to claim 1 , wherein:{'sup': 1', '4', '5, 'sub': 1', '6', '1', '6', '3', '12, 'Rrepresents a C-Calkoxyl, a C-Chaloalkoxyl, a C-Ccycloalkoxyl, a —NRRgroup;'}{'sup': '2', 'sub': 2', '7', '2', '7', '1', '6', '2', '7', '1', '6', '1', '6', '1', '6', '1', '6', '1', '6', '1', '6', '1', '6', '3', '12', '1', '6', '1', '6', '1', '6', '1', '6', '1', '6', '1', '6', '4', '12', '1', '6', '1', '6', '1', '6', '1', '6', '1', '6', '1', '6', '1', '6', '1', '6', '1', '6', '1', '6', '1', '6', '1', '6', '1', '6', '1', '6', '3', '12', '1', '6', '1', '6', '1', '6', '1', '6', '1', '6', '1', '6', '3', '12', '1', '6', '1', '6', '1', '6', '1', '6', '4', '6', '1', '6', '2', '6', '1', '6', '4', '12', '1', '6', '1', '6', '1', '6', '1', '6', '1', '6', '1', '6', '1', '6', '1', '6', '1', '6', '1', '6', '1', '6', '1', '6', '1', '6', '1', '6', '3', '12', '1', '6', '1', '6', '1', '6', '1', '6', '1', '6', '1', '6', '3', '12', '1', '6', '1', '6', '1', '6', '1', '6', '2', '6', '1', '6', '2', '6', '1', '6', '4', '12', '1', '6', '1', '6', '1', '6', '1', '6', '1', '6', '4', '12', '1', '6', '1', '6', '1', '6, 'Rrepresents a hydrogen atom, a C-Cacyl, a C-Calkanoyloxyalkyl C-C, a C-Chaloalkanoyloxyalkyl C-C, a C-Calkoxy-C-C-alkanoyloxyalkyl C-C, a C-Chaloalkoxy-C-C-alkanoyloxyalkyl C-C, a C-Ccycloalkoxy-C-C-alkanoyloxyalkyl C-C, an aryloxy C-Calkanoyloxyalkyl C-C, a benzyloxy C-Calkanoyloxyalkyl C-C, a C-Ccycloalkanoyloxyalkyl C-C, a C-Caroyloxyalkyl, a C-Cbenzoyloxyalkyl, a C-Cheterocyclylcarbonyloxyalkyl, a C-Calkyloxyalkyl C-C, a C-Chaloalkyloxyalkyl C-C, a C-Calkoxy-C-C-alkyloxyalkyl C-C, a C-Chaloalkoxy-C-C-alkyloxyalkyl C-C, a C-Ccycloalkoxy C-C-alkyloxyalkyl C-C, an aryloxy C-C-alkyloxyalkyl C-C, a benzyloxy C-C-alkyloxyalkyl C-C, a C-Ccycloalkyloxyalkyl C-C, a C-Caryloxyalkyl, a C-Cbenzyloxyalkyl; a C-Cheterocyclyloxyalkyl, a C-Calkanoylthioalkyl C-C, a C-Chaloalkanoylthioalkyl C-C, a C-Ccycloalkanoylthioalkyl C-C, a C- ...

ADDITIVE FOR RUBBER

Provided is an additive for rubber that contains a sulfide composition, wherein the sulfide composition in the additive for rubber contains a sulfide compound having the repeating units shown by formula (1), the amount of repeating units (1) in which X=2 is at least 45 molar parts per 100 molar parts of repeating units (1) in the sulfide compound, and the number n of repeating units (1) in the sulfide compound is from 1 to 400, whereby an additive for rubber capable of imparting excellent heat resistance is provided. Also provided is a rubber composition that contains said additive for rubber. 2. The additive for rubber according to claim 1 ,wherein, in the sulfide compound, the amount of repeating unit (1) having X=2 is at least 50 parts by mol per 100 parts by mol of the total amount of repeating unit (1).3. The additive for rubber according to claim 1 ,wherein, in the sulfide compound, the amount of repeating unit (1) having X=1 is 1 parts by mol to 40 parts by mol per 100 parts by mol of the total amount of repeating unit (1).5. A rubber composition comprising the additive for rubber according to and natural rubber and/or synthetic rubber.6. The additive for rubber according to claim 2 ,wherein, in the sulfide compound, the amount of repeating unit (1) having X=1 is 1 parts by mol to 40 parts by mol per 100 parts by mol of the total amount of repeating unit (1).9. A rubber composition comprising the additive for rubber according to and natural rubber and/or synthetic rubber.10. A rubber composition comprising the additive for rubber according to and natural rubber and/or synthetic rubber.11. A rubber composition comprising the additive for rubber according to and natural rubber and/or synthetic rubber. The present invention relates to an additive for rubber and a rubber composition comprising the additive for rubber.For improving performance of rubber products, for example, use of sulfur as a vulcanizing agent is known. In recent years, an additive comprising ...

BIODEGRADABLE LIPIDS FOR THE DELIVERY OF ACTIVE AGENTS

The present invention relates to a cationic lipid having one or more biodegradable groups located in a lipidic moiety (e.g., a hydrophobic chain) of the cationic lipid. These cationic lipids may be incorporated into a lipid particle for delivering an active agent, such as a nucleic acid. The invention also relates to lipid particles comprising a neutral lipid, a lipid capable of reducing aggregation, a cationic lipid of the present invention, and optionally, a sterol. The lipid particle may further include a therapeutic agent such as a nucleic acid. 134-. (Canceled)42. The process of claim 39 , wherein the reaction is performed in dichloromethane.43. The process of claim 40 , wherein the reaction is performed in dichloromethane.44. The process of claim 41 , wherein the reaction is performed in dichloromethane. This application is a continuation of U.S. patent application Ser. No. 13/708,383, filed Dec. 7, 2012, which claims the benefit of U.S. Provisional Application No. 61/568,133, filed Dec. 7, 2011, and U.S. Provisional Application No. 61/623,274, filed Apr. 12, 2012, each of which is hereby incorporated by reference.The present invention relates to biodegradable lipids and to their use for the delivery of active agents such as nucleic acids.Therapeutic nucleic acids include, e.g., small interfering RNA (siRNA), micro RNA (miRNA), antisense oligonucleotides, ribozymes, plasmids, immune stimulating nucleic acids, antisense, antagomir, antimir, microRNA mimic, supermir, U1 adaptor, and aptamer. In the case of siRNA or miRNA, these nucleic acids can down-regulate intracellular levels of specific proteins through a process termed RNA interference (RNAi). The therapeutic applications of RNAi are extremely broad, since siRNA and miRNA constructs can be synthesized with any nucleotide sequence directed against a target protein. To date, siRNA constructs have shown the ability to specifically down-regulate target proteins in both in vitro and in vivo models. In addition, ...

ANTIVIRAL COMPOUNDS AND METHODS

The invention relates to compounds having antiviral and methods utilizing the compounds to treat viral infections. 2. The compound according to wherein the compound is selected from:(2-Bromocinnamoyl)guanidine,(2-Chlorocinnamoyl)guanidine,(2-Furanacryloyl)guanidine,(2-Methoxycinnamoyl)guanidine,(2-Nitrocinnamoyl)guanidine,(3-Bromocinnamoyl)guanidine,(3-Chlorocinnamoyl)guanidine,(3-Methoxycinnamoyl)guanidine,(3-Nitrocinnamoyl)guanidine,(3-phenylpropanoyl)guanidine,(4-Bromocinnamoyl)guanidine,(4-Chlorocinnamoyl)guanidine,(4-Hydroxycinnamoyl)guanidine,(4-Methoxycinnamoyl)guanidine,(4-Phenoxybenzoyl)guanidine,(5-Phenyl-penta-2,4-dienoyl)guanidine,(a-Methylcinnamoyl)guanidine,(Phenylacetyl)guanidine,(Quinoline-2-carbonyl)guanidine,(trans-2-Phenylcyclopropanecarbonyl)guanidine,[(4-Chlorophenoxy-acetyl]guanidine,[(E)-3-(4-Dimethylaminophenyl)-2-methylacryloyl]guanidine,[3-(3-Pyridyl)acryloyl]guanidine,1-bromo-2-naphthoylguanidine,1-naphthoylguanidine,2-(1-naphthyl)acetoylguanidine,2-(2-naphthyl)acetoylguanidine,2-(cyclohex-1-en-1yl)cinnamoylguanidine,2-(trifluoromethyl)cinnamoylguanidine,2,3,5,6,-tetramethylcinnamoylguanidine,2,3-difluorocinnamoylguanidine,2,3-dimethylcinnamoylguanidine,2,4,6-trimethylcinnamoylguanidine,2,4-dichlorocinnamolyguanidine,2,5-dimethylcinnamoylguanidine,2,6-dichlorocinnamoylguanidine,2-chloro-6-fluorocinnamoylguanidine,2-cyclohexylcinnamoylguanidine,2-ethoxycinnamoylguanidine,2-ethylcinnamoylguanidine,2-fluorocinnamoylguanidine,2-methylcinnamoylguanidine,2-naphthoylguanidine,2-phenylcinnamoylguanidine,2-t-butylcinnamoylguanidine,3-(2-naphthyl)acryloylguanidine,3-(cyclohex-1-en-1-yl)cinnamoylguanidine,3-(trans-hept-1-en-1-yl)cinnamoylguanidine,3-(trifluoromethoxy)cinnamoylguanidine,3-(trifluoromethyl)cinnamoylguanidine,3,4-(methylenedioxy)cinnamoylguanidine,3,4,5-trimethoxycinnamoylguanidine,3,4-dichlorocinnamoylguanidine,3,4-difluorocinnamoylguanidine,3-ethoxycinnamoylguanidine,3-fluorocinnamoylguanidine,3-isopropylcinnamoylguanidine ...

Latent thiol monomers

This invention relates to latent thiol monomers and their use in the synthesis of polymers. In addition, this invention relates to novel polymers and graft copolymers formed with these latent thiol monomers.

Thiol and Sulfur-containing O-(meth) acrylate compounds and use thereof

A sulfur-containing O-(meth)acrylate compound of the following formula (1) is useful as a starting material for a resin composition used in optical applications such as a lens; ##STR1## wherein R represents hydrogen atom or methyl group; 1 represents an integer from 1 to 3; B is ##STR2## n is 1 or 2, m is 1, 2 or 3 and A is selected from certain arylene, aralkylene, thioether, dithioether or thiopheneylene radicals.

BIODEGRADABLE LIPIDS FOR THE DELIVERY OF ACTIVE AGENTS

The present invention relates to a cationic lipid having one or more biodegradable groups located in a lipidic moiety (e.g., a hydrophobic chain) of the cationic lipid. These cationic lipids may be incorporated into a lipid particle for delivering an active agent, such as a nucleic acid. The invention also relates to lipid particles comprising a neutral lipid, a lipid capable of reducing aggregation, a cationic lipid of the present invention, and optionally, a sterol. The lipid particle may further include a therapeutic agent such as a nucleic acid. 1. A cationic lipid comprising a primary group and two biodegradable hydrophobic tails , wherein (a) the primary group comprises a protonatable group having a pKof from about 4 to about 13 , (b) the cationic lipid has an in vivo half life (t) of less than about 3 hours , and (c) at least one of the hydrophobic tails has the formula -(hydrophobic chain)-(biodegradable group)-(hydrophobic chain) where the terminal hydrophobic chain in the hydrophobic tail is a branched alkyl group. where the branching occurs at the α-position relative to the biodegradable group.2. The cationic lipid of claim 1 , wherein the primary group includes (i) a head group claim 1 , and (ii) a central moiety to which both the biodegradable hydrophobic tails are directly bonded.3. The cationic lipid of claim 2 , wherein the central moiety is selected from the group consisting of a central carbon atom claim 2 , a central nitrogen atom claim 2 , a central carbocyclic group claim 2 , a central aryl group claim 2 , a central heterocyclic and a central heteroaryl group.4. The cationic lipid of claim 1 , wherein at least one biodegradable hydrophobic tail has the formula —R-M-R claim 1 , where Ris a C-Calkylene or C-Calkenylene claim 1 , Mis a biodegradable group claim 1 , and Ris a branched alkyl or branched alkenyl.5. The cationic lipid of claim 4 , wherein Ris a branched C-Calkyl or C-Calkenyl.6. The cationic lipid of claim 4 , wherein the chain length ...

Polymerization with living characteristics

This invention concerns a free radical polymerization process, selected chain transfer agents employed in the process and polymers made thereby, in which the process comprises preparing polymer of general Formula (A) and Formula (B) comprising contacting: (i) a monomer selected from the group consisting of vinyl monomers (of structure CH2 = CUV), maleic anhydride, N-alkylmaleimide, N-arylmaleimide, dialkyl fumarate and cyclopolymerizable monomers; (ii) a thiocarbonylthio compound selected from Formula (C) and Formula (D) having a chain transfer constant greater than about 0.1; and (iii) free radicals produced from a free radical source; the polymer of Formula (A) being made by contacting (i), (ii) C and (iii) and that of Formula (B) by contacting (i), (ii) D, and (iii); and (iv) controlling the polydispersity of the polymer being formed by varying the ratio of the number of molecules of (ii) to the number of molecules of (iii); wherein Q, R, U, V, Z, Z', m, p and q are as defined in the text.

Purification of bis(thiohydrazide amides)

Disclosed herein is a method for the purification of bis(thiohydrazide amide) compounds of formula I, wherein R1, R2, R3, R4, R7, R8, Z and Y are defined herein, by dissolving the compound in a solvent selected from the group consisting of tetrahydrofuran-acetone, tetrahydrofuran-acetonitrile, tetrahydrofuran, acetone, acetonitrile, tetrahydrofuran-ethanol and acetone-ethanol and precipitating the compound with water.

Oxime sulfonate derivatives

SULFUR COMPOUNDS AND METHOD FOR THEIR PRODUCTION

PROCESS FOR THE PREPARATION OF AMINOTHIOLESTER COMPOUNDS AND THEIR SALTS

La présente invention concerne un procédé de préparation de composés de formule (I) comprenant les étapes suivante : a) réaction d'un composé de formule (II) avec un acide inorganique ou un acide organique b) réaction du composé obtenu à l'étape a) avec une base ; c) réaction du composé obtenu à l'étape b) avec du CO2 ; d) réaction du composé obtenu à l'étape c) avec un chloroformiate d'alkyle, un réactif susceptible de former, avec le composé obtenu à l'étape c) un halogénure d'acide ou un réactif susceptible de former, avec le composé obtenu à l'étape c), un anhydride mixte ; e) réaction du composé obtenu à l'étape d) avec un composé précurseur d'anion The present invention relates to a process for the preparation of compounds of formula (I) comprising the following steps: a) reaction of a compound of formula (II) with an inorganic acid or an organic acid b) reaction of the compound obtained in step a) with a base; c) reaction of the compound obtained in step b) with CO2; d) reaction of the compound obtained in step c) with an alkyl chloroformate, a reagent capable of forming, with the compound obtained in step c), an acid halide or a reagent capable of forming, with the compound obtained in step c), a mixed anhydride; e) reaction of the compound obtained in step d) with an anion precursor compound

New amino acid derivatives, their preparation processes and their therapeutic application.

PROCESS FOR THE PRODUCTION OF DITHIOUSTERN

Latent thiol monomers and their use in the synthesis of polymers

ABSTRACT OF THE DISCLOSURE This invention relates to latent thiol monomers and their use in the synthesis of polymers. In addition, this invention relates to novel polymers and graft copolymers formed with these latent thiol monomers.

Water-soluble dithioesters and method for polymerization thereof

具有活性特征的聚合作用

本发明涉及一种自由基聚合方法,涉及选择该方法中使用的链转移剂和由该方法制得的聚合物;其中该方法包括制备通式(A)和通式(B)的聚合物;包括使下还组分进行接触:(i)选自乙烯基单体(结构式为CH 2 =CUV)、马来酸酐、N－烷基马来酰亚胺、N－芳基马来酰亚胺、富马酸二烷基酯和可环化聚合的单体的单体;(ii)选自通式(C)和通式(D)的硫代羰基硫化合物,其链转移常数大于约0.1;和(iii)由自由基源生成的自由基;通式(A)的聚合物是由(i)、(ii)C和(iii)进行接触制得的,通式(B)的聚合物是由(i)、(ii)D和(iii)进行接触制得的;以及(iv)通过改变(ii)与(iii)的分子数的比值,来控制形成的聚合物的多分散性指数;其中Q、R、U、V、Z、Z’、m、p和q如说明书所定义。

Latent thiol monomers

Latent thiol monomers and their use in the synthesis of polymers and graft copolymers are described. The latent thiol monomers comprise at least one polymerizable functional group and at least one protected thiol group. The polymers or copolymers may be used in adhesive, caulk, or mastic compositions. The copolymer may also be used as a compatiblizer for physical blends of at least two polymers.

Thiol and sulfur-containing O-(meth)acrylate counpounds and use thereof

A sulfur-containing O-(meth)acrylate compound of the following formula (1) is useful as a starting material for a resin composition used in optical applications such as a lens; wherein R represents hydrogen atom or methyl group; l represents an integer from 1 to 3; B is when B is n is 2; m is 1 or 2; A is selected from the following groups: wherein m represents 1 or 2; each ring may be substituted by one or more alkyl, alkylthio or alkoxy groups having 1 or 2 carbon atoms; p and q are 0 or 1, while m is 1 when p is 1; when B is n is 1; m is 2 or 3; A is selected from the following groups: —(CH 2 ) r —S—(CH 2 ) r —, —(CH 2 ) r —S—S—(CH 2 ) r —, —(CH 2 ) r —S—(CH 2 ) s —S—(CH 2 ) r — and wherein r and s are an integer from 1 to 3; when B is n is 1; m is 2; A is selected from the following groups: —(CH 2 ) r —S—(CH 2 ) r —, —(CH 2 ) r —S—S—(CH 2 ) r — and —(CH 2 ) r —S—(CH 2 ) s —S—(CH 2 ) r — wherein r and s are an integer from 1 to 3.

硫醇和含硫o－(甲基)丙烯酸酯化合物及其应用

本发明涉及下列式(1)的化合物及其制备方法和作为树脂组合物的原料在光学上的用途，其中R、A、B、m、n和l的定义见说明书。

制备氨基硫醇酯化合物及其盐的方法

制备氨基硫醇酯化合物及其盐的方法。本发明涉及制备式(I)化合物的方法，包括以下步骤：a)式(II)化合物与无机酸或有机酸的反应；b)步骤a)中获得的化合物与碱的反应；c)步骤b)中获得的化合物与CO 2 的反应；d)步骤c)中获得的化合物与氯甲酸烃基酯(即可能与步骤c)中获得的化合物可能形成酰卤的试剂，或者与步骤c)中获得的化合物可能形成混合酸酐的试剂)的反应；e)步骤d)中获得的化合物与SMe ‑ 阴离子前体化合物的反应。

Optically active derivative of d-2-(6-methoxy-2-naphthyl)-propionic acid and pharmaceutical compositions containing it

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Method of preparation of symmetric oxythioalcanes