222 results about "Carbamic acid" patented technology

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 carbamic acid compounds of the following formula, which inhibit HDAC (histone deacetylase) activity wherein: A is independently an unsubstituted or substituted bicyclic C9-10heteroaryl group (e.g., quinolinyl; quinoxalinyl; benzoxazolyl; benzothiazolyl); Q is an acid leader group, and is independently an unsubstituted or substituted, saturated or unsaturated C17alkylene group having a backbone length of 4 or less; with the proviso that if A is unsubstituted benzothiazol-2-yl, then Q is an unsaturated group; and with the proviso that if A is unsubstituted quinolin-6-yl, then Q is unsubstituted at the a-position; and with the proviso that A is not benzimidazol-2-yl; 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 in the treatment of conditions mediated by HDAC, cancer, proliferative conditions, psoriasis, etc.

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: C3-20carbocyclyl, C3-20heterocyclyl, or C5-20aryl; and is optionally substituted; Q1 is independently: a covalent bond; C1-7alkylene; or C1-7alkylene-X—C1-7alkylene, —X—C1-7alkylene, or C1-7alkylene-X—, wherein X is —O— or —S—; and is optionally substituted; Q2 is independently: C4-8alkylene; and is optionally substituted; and has a backbone length of at least 4 atoms; or: Q2 is independently: C5-20arylene; C5-20arylene-C1-7alkylene; C1-7alkylene-C5-20arylene; or, C1-7alkylene-C5-20arylene-C1-7alkylene; 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; andR3 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.

Disclosed is a method for the preparation of carbamic acid (R)-1-aryl-2-tetrazolyl-ethyl ester, comprising the asymmetric reduction of arylketone and the carbamation of alcohol.

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.

A catalyst of the invention includes an imide compound having a N-substituted cyclic imide skeleton represented by following Formula (I):wherein R is a hydroxyl-protecting group. Preferred R is a hydrolyzable protecting group. R may be a group obtained from an acid by eliminating an OH group therefrom. Such acids include, for example, carboxylic acids, sulfonic acids, carbonic acid, carbamic acid, sulfuric acid, nitric acid, phosphoric acids and boric acids. The catalyst may include the imide compound and a metallic compound in combination. In the presence of the catalyst, (A) a compound capable of forming a radical is allowed to react with (B) a radical scavenging compound and thereby yields an addition or substitution reaction product of the compound (A) and the compound (B) or a derivative thereof. This catalyst can produce an organic compound with a high selectivity in a high yield as a result of, for example, an addition or substitution reaction under mild conditions.

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 psorias

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.

A medicinal composition combining paclitaxel with a novel phthalazinone compound, provided by the invention, comprises an active component and a pharmaceutically-acceptable auxiliary material, the active component is composed of paclitaxel and the phthalazinone compound with an N crystal form, represented by formula I, and a mass ratio of the paclitaxel to the phthalazinone compound of the formulaI in the active component is (0.1-0.3):1, wherein the chemical name of the phthalazinone compound of the formula I is [2(1H)-butyl-2-enoyl-3,4-dihydroisoquinolin-5-yl]-carbamic acid-4-[8-fluoro-(2H)-phthalazin-1-one]benzyl ester mesylate. The medicinal composition has a good anticancer effect. It is found that the paclitaxel and the phthalazinone compound with an N crystal form, represented by formula I, are combined to greatly enhance the antitumor growth bioactivity and achieve antitumor proliferation synergistic effects, so the medicinal composition is expected to be developed into clinically anti-pancreatic cancer first-line drugs.

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 stepsa) 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.

The invention relates to a material chitosan-bi(aryl-carbamate)-(amide) for preparing a chiral stationary phase and a preparation method of the chitosan-bi(aryl-carbamate)-(amide). The preparation method comprises the following steps: 1) acylating chitosan amino, namely enabling chitosan with the deacetylation degree of over 98 percent to be reacted with excessive anhydride, thereby obtaining acylated N-chitosan; and 2) performing carbamic acid esterification on acylated N-chitosan, namely dissolving the acylated N-chitosan in N,N-dimethylacetamide solution of lithium chloride, adding excessive isocyanate containing different substituent groups on the benzene ring, and reacting at the temperature of 80-95 DEG C for 24-36 hours, thereby generating a chitosan derivative, namely the chitosan-bi(aryl-carbamate)-(amide). The structural formula is as shown in the specification.

Zinc carbonates such as carbonic acid zinc salt, zinc carbonate hydroxide monohydrate, zinc bicarbonate, zinc tetraamine carbonate, zinc ammonium carbonate, carbamic acid zinc salt and zinc carbamate can initiate hardening of polyurethane coatings and decrease the coating tack-free time. The decreased tack-free times facilitate earlier application of additional polyurethane layers and earlier return of a coated article to service, and can provide improved floor finishes.

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 invention discloses novel high-strength foam concrete and a preparation method for the same. The novel high-strength foam concrete is characterized in that the novel high-strength foam concrete is prepared from the following raw materials in parts by weight: 300 to 800 parts of a gel material, 250 to 850 parts of a fine aggregate, 375 to 1,250 parts of a coarse aggregate, 4 to 8 parts of a water reducing agent, 250 to 850 parts of water, 20 to 40 parts of a foaming agent and 10 to 20 parts of a foam stabilizer, wherein the foaming agent is an isocyanate derivative. According to the novel high-strength foam concrete and the preparation method for the same, the following principle is utilized: isocyanate adopted as the foaming agent is reacted with the water to generate unstable carbamic acid at first, the unstable carbamic acid is rapidly decomposed into amine and carbon dioxide, and the discharged carbon dioxide acts for foaming to generate a foam body; a prepared foam concrete material is favorable for making a heat insulation, soundproof and high-strength foam concrete building block on one hand, and on the other hand, the construction engineering cost is reduced, and the high-strength foam concrete can be widely applied to construction engineering.

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.