219 results about "Carbamic acid" patented technology

The present invention relates to novel synthetic methods for the preparation of intermediates of 3{5-[3-(4,6-Difluoro-1H-benzoimidazol-2-yl)-1H-indazol-5-yl]4-methyl-pyridin-3-yl methyl}-ethyl-amine.

This invention pertains to certain active carbamic acid compounds which inhibit HDAC activity and which have the following formula:

wherein: A is an aryl group; Q¹ is a covalent bond or an aryl leader group; J is an amide linkage selected from: —NR¹C(═O)— and —C(═O)NR¹—; R¹ is an amido substituent; X is an ether heteroatom, and is —O— or —S—; and, R² and R³ are each independently an ether group; and pharmaceutically acceptable salts, solvates, amides, esters, ethers, chemically protected forms, and prodrugs thereof. The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo, to inhibit HDAC, and, e.g., to inhibit proliferative conditions, such as cancer and psoriasis.

This invention pertains to certain active carbamic acid compounds which inhibit HDAC activity and which have the following formula: (I) A is an aryl group; Q¹ is a covalent bond or an aryl leader group; J is a sulfonamide linkage selected from: —S(═O)₂NR¹— and —NR¹S(═O)₂—; R¹ is a sulfonamido substituent; and, Q² is an acid leader group; with the proviso that if J is —S(═O)₂NR¹—, then Q¹ is an aryl leader group; and pharmaceutically acceptable salts, solvates, amides, esters, ethers, chemically protected forms, and prodrugs thereof. The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo, to inhibit HDAC, and, e.g., to inhibit proliferative conditions, such as cancer and psoriasis.

This invention pertains to certain carbamic acid compounds which inhibit HDAC (histone deacetylase) activity of the following formula:

wherein: Cy is independently a cyclyl group; Q¹ is independently a covalent bond or cyclyl leader group; the piperazin-1,4-diyl group is optionally substituted; J¹ is independently a covalent bond or —C(═;O)—; J² is independently —C(═O)— or —S(═O)₂—; Q₂ is independently an acid leader group; wherein: Cy is independently: C_3-20carbocyclyl, C_3-20heterocyclyl, or C_5-20aryl; and is optionally substituted; Q¹ is independently: a covalent bond; C_1-7alkylene; or C_1-7alkylene-X—C_1-7alkylene, —X—C^1-7alkylene, or C_1-7alkylene-X—, wherein X is —O— or —S—; and is optionally substituted; Q² is independently: C_4-8alkylene; and is optionally substituted; and has a backbone length of at least 4 atoms; or: Q² is independently: C_5-20arylene; C_5-20arylene-C_1-7alkylene; C_1-7alkylene-C_5-20arylene; or, C_1-7alkylene-C_5-20arylene-C_1-7alkylene; and is optionally substituted; and has a backbone length of at least 4 atoms; or a pharmaceutically acceptable salt, solvate, amide, ester, ether, chemically protected form, or prodrug thereof. The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo, to inhibit HDAC, and in the treatment of conditions mediated by HDAC, cancer, proliferative conditions, psoriasis, etc.

Compounds having somatostatin activity of the following Formula I,

wherein,

• • R¹ is aryl, substituted-aryl, and aryl-(lower-alkyl)-;
  • R² is lower alkyl, amino substituted lower alkyl, -carboxy-(lower-alkyl), -carbamic acid-(lower-alkyl) and -carboxy-(lower-alkyl)-aryl; and
  • R³ and R⁴ are independently, lower-alkyl, aryl, substituted-aryl, (substituted-aryl)-(lower-alkyl)-, heteroaryl, (heteroaryl)-(lower-alkyl)-, substituted-heteroaryl, (substituted heteroaryl)-(lower-alkyl)-, heterocyclic, heterocyclic-(lower-alkyl)-, substituted-heterocyclic, (substituted-heterocylic)-(lower alkyl)-, -carboxy-(lower-alkyl), and -carboxy-(lower-alkyl)-aryl; or a pharmaceutically acceptable, ester, ether, or salt thereof; methods for their use; and preparation.

The invention discloses a hydrophobically-modified polyethyleneimine foaming agent capable of releasing carbon dioxide. The hydrophobically-modified polyethyleneimine foaming agent is prepared by reacting polyethyleneimine subjected to hydrophobic modification by a glycidyl ether compound or an alkyl carboxylic compound or a halogenated alkane compound with 0-31% of distilled water at the pressure of 0.1-1 MPa in carbon dioxide at the room temperature for 1-3 days; a 5-40.4 mol% hydrophobic chain is grafted on N atoms in a polyethyleneimine molecular chain of the foaming agent, and a carbamic acid anion (-NCOO-) characteristic absorption peak or a bicarbonate (HCO3-) characteristic absorption peak exists at the range of 159-165 ppm of a C Nuclear magnetic resonance of the foaming agent, and the foaming agent can release carbon dioxide CO2 at the temperature of 50-150 to prepare a polyurethane foam material. The foaming agent provided by the invention can be uniformly dispersed in a preparation raw material of hydrophobic polyurethane foam, can solve a series of problems caused by the fact that non-modified polyethyleneimine is used as a foaming agent, and is climate-friendly.

The invention discloses a 1, 5-pentyl diisocyanate preparation method which includes the steps: (1) mixing 1, 5-pentane diamine transfer solution and extracting solvents, extracting 1, 5-pentane diamine and dewatering extracting solution to obtain mixed solution of the 1, 5-pentane diamine transfer solution and the extracting solvents; (2) adding catalysts and urea into the mixed solution of the 1, 5-pentane diamine transfer solution and the extracting solvents, supplementing an appropriate quantity of extracting solvents to form a reaction system, performing carbamic acid esterification on the 1, 5-pentane diamine and recycling excessive extracting solvents in the reaction system by reduced pressure distillation to obtain PDU; (3) mixing the PDU, heat carriers and the catalysts and performing thermal cracking reaction and separation to obtain the extracting solvents and PDI. According to the method, a large quantity of salts in the transfer solution can be removed by extracting solvent extraction, the extracting solvents can serve as raw materials for synthesizing the PDU, the PDI can be prepared by thermal cracking, and the extracting solvents serving as by-products can be recycled.

This invention pertains to pharmaceutical compositions comprising certain carbamic acid compounds (e.g., which inhibit HDAC (histone deacetylase) activity) (e.g., PXD-101, N hydroxy-3-(3-phenylsulfamoyl-phenyl)-acrylamide)) and one or more additional ingredients selected from cyclodextrin, arginine, and meglumine. The present invention also pertains to the use of such compositions, for example, in the inhibition of HDAC, and in the treatment of conditions mediated by HDAC, cancer, proliferative conditions, psoriasis, etc.

The present invention describes carbamic acid ester-derived and valeric acid ester-derived polyfunctional cross-linker molecules, and methods for their synthesis and use. The inclusion of polymeric moieties such as poly(alkylene oxide) in the cross-linkers of the present invention can provide advantageous solubility properties in aqueous environments. Such cross-linkers may be used to form conjugates for use in a variety of assay formats.

Disclosed is a method for the preparation of carbamic acid (R)-1-aryl-2-tetrazolyl-ethyl esters, comprising the enantioselective enzyme reduction of a 1-aryl-2-tetrazolyl-ethyl ketone to form a (R)-1-aryl-2-tetrazolyl-ethyl alcohol and the carbamation of said alcohol.

This invention pertains to certain active carbamic acid compounds which inhibit HDAC activity and which have the formula (1) wherein: A is an aryl group; Q1 is an aryl leader group having a backbone of at least 2 carbon atoms; J is an amide linkage selected from: —NR1C(═O)— and —C(═O)NR1-; R1 is an amido substituent; and, Q2 is an acid leader group; and pharmaceutically acceptable salts, solvates, amides, esters, ethers, chemically protected forms, and prodrugs thereof. The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo, to inhibit HDAC, and, e.g., to inhibit proliferative conditions, such as cancer and psoriasis.

The invention relates to a lubricating grease additive, which has a structure as shown in a general formula, wherein R1, R2, R3 and R4 are selected from C4-C15 straight chain and branched chain alkyl group; R1 is different from R2; R3 is the same with R4; R1 and R2 can be the same with or different from R3 and R4; Z equals to 1-3, W equals to 1-3; and x+y=3-7. The invention also provides a methodfor preparing the above additive by a reaction of a dialkylamine mixture, comprising the following steps of: mixing water, the dialkylamine mixture, cycloalkyl base oil and molybdenum resource with uniformly stirring, cooling to 15-20DEG C, pressurizing to 830-900mmHg, adding dropwisely carbon disulfide, heating up to 60-80DEG C, followed by reflux reaction for 3-5 hours, reducing pressure to 760-800mmHg for water evaporation, completely vacuumizing at low speed, heating to 120-140DEG C, continuously reacting for 1-3 hours, cooling, and filtering. The additive provided by the invention contains no phosphorus, and has not only excellent antifriction and anti-wear performance but also improved oil dissolving performance and antioxidation performance.

The invention discloses a preparation method of a 6-bromoindole derivative: tertiary butyl 2-(6-bromo-1H-indole-3-yl) ethyl carbamic acid. The preparation method comprises the following steps: by using 6-bromoindole as an initial raw material, carrying out Friedel-Craft reaction; carrying out amidation; reducing; and carrying out t-butyloxycarboryl protective reaction to obtain the target product. The compound is an important medical intermediate.

Amorphous and crystalline solid forms of the anti-HCV compound (1-{3-[6-(9,9-difluoro-7-{2-[5-(2-methoxycarbonylamino-3-methyl-butyryl)-5-aza-spiro[2.4]hept-6-yl]-3H-imidazol-4-yl}-9H-fluoren-2-yl)-1H-benzoimidazol-2-yl]-2-aza-bicyclo[2.2.1]heptane-2-carbonyl}-2-methyl-propyl)-carbamic acid methyl ester (Compound I) were prepared and characterized in the solid state: Also provided are processes of manufacture and methods of using the amorphous and crystalline forms.

The invention relates to novel trans N-{4-{2-[4-(2, 3-dichlorophenyl)-piperazine-1-il]-ethyl}-cyclohexylamine dihydrochloride monohydrate and a process for the preparation of the trans N-{4-{2-[4-(2,3-dichlorophenyl)-piperazine-1-il]-ethyl}-cyclohexylamine dihydrochloride monohydrate, said process comprising the steps

• • a) reacting trans 2-{1-[4-(N-tert-butoxycarbonyl) amino]-cyclohexyl}-acetic acid ester with sodium borohydride and aluminium trichloride to give trans 2-{1-[4-(N-tert-butoxycarbonyl)-amino]-cyclohexyl}-ethanol;
  • b) reacting trans 2-{1-[4-(N-tert-butoxycarbonyl)-amino]cyclohexyl}-ethanol obtained with methanesulfonic acid chloride in the presence of an acid binding agent to give trans 2-{1-[4-(N-tert-butoxycarbonyl)-amino]-cyclohexyl}-ethyl methanesulfonate;
  • c) reacting trans 2-{1-[4-(N-tert-butoxycarbonyl)-amino]-cyclohexyl}-ethyl methanesulfonate obtained with 2,3-dichlorophenyl-piperazine in the presence of an acid binding agent to give trans 2-{1-[4-(N-tert-butoxycarbonyl)-amino]-cyclohexyl}-carbamic acid tert-butylester;
  • d) heating trans 2-{1-[4-(N-tert-butoxycarbonyl)-amino]-cyclohexyl}-carbamic acid tert-butylester obtained to a temperature between 40-100° C. in a mixture of aqueous hydrochloric acid/methanol to give trans N-{4-{2-[4-(2,3-dichlorophenyl) piperazine-1-il]-ethyl}-cyclohexylamine dihydrochloride monohydrate.

A composition for forming a coating film, comprising a reaction product of a tantalum alkoxide and at least one compound selected from carbamic acid, carboxylic acid and carboxylic anhydride and a solvent. A tantalum oxide film is obtained by forming a coating film of this composition and thermally and/or optically treating the coating film. This tantalum oxide film has a large dielectric constant and a small leak current.