349 results about "Aminothiazole" patented technology

The invention relates to processes for preparing compounds having the formula,

• • and crystalline forms thereof, wherein Ar is aryl or heteroaryl, L is an optional alkylene linker, and R₂, R₃, R₄, and R₅, are as defined in the specification herein, which compounds are useful as kinase inhibitors, in particular, inhibitors of protein tyrosine kinase and p38 kinase.

The invention relates to processes for preparing compounds having the formula,

and crystalline forms thereof, wherein Ar is aryl or heteroaryl, L is an optional alkylene linker, and R₂, R₃, R₄, and R₅, are as defined in the specification herein, which compounds are useful as kinase inhibitors, in particular, inhibitors of protein tyrosine kinase and p38 kinase.

The invention discloses 4-tert-butyl-5-(1,2,4-triazol-1-yl)-2-benzylimino thiazole (I) having the chemical structural formula shown rightwards. A method for preparing the 4-tert-butyl-5-(1,2,4-triazol-1-yl)-2-benzylimino thiazole is as follows: the step of reflux reaction is carried out on the 4-tert-butyl-5-(1,2,4-triazol-1-yl)-2-aminothiazole and aryl aldehyde in benzene, thereby preparing the 4-tert-butyl-5-(1,2,4-triazol-1-yl)-2-benzylimino thiazole. The 4-tert-butyl-5-(1,2,4-triazol-1-yl)-2-benzylimino thiazole can be used for preparing bactericide.

The invention discloses 4-(benzofuran-5-yl)-2-benzal aminothiazole as shown in a chemical structural formula I. The preparation method of the 4-(benzofuran-5-yl)-2-benzal aminothiazole is as follows: 1-(7-hydroxy/ alkoxy-2,2-dimethyl-2,3-dihydro-benzofuran-5-yl) butanone is subject to bromination and reacts with thiourea to obtain 4-(7-hydroxy/ alkoxy-2,2-dimethyl-2,3-dihydro-benzofuran-5-yl)-2-aminothiazole which reacts with aromatic aldehyde to prepare the 4-(benzofuran-5-yl)-2-benzal aminothiazole. The 4-(benzofuran-5-yl)-2-benzal aminothiazole has good activity inhabiting activity on Hela cells, human liver cancer cells (Bel 7402 cells) and lung carcinoma cells (A549 cells) and can be used for preparing the antineoplastic agent.

The invention discloses 4-(benzofuran-5-yl)-2-aromatic aminothiazole shown as a chemical structural formula I. The preparation method of the 4-(benzofuran-5-yl)-2-aromatic aminothiazole comprises the following steps of: heating and stirring 2-halogen-1-(7-hydroxyl/alkoxyl-2,2-dimethyl-2,3-dihydrobenzofuran-5-yl) butanone and arylthiourea in acetone for reaction to obtain 4-(benzofuran-5-yl)-2-aromatic aminothiazole salt; and neutralizing the 4-(benzofuran-5-yl)-2-aromatic aminothiazole salt with stronger ammonia water to obtain the 4-(benzofuran-5-yl)-2-aromatic aminothiazole. The 4-(benzofuran-5-yl)-2-aromatic aminothiazole has high insecticidal activity and is applied to the preparation of pesticides.

The invention is directed to processes for preparing 2-aminothiazole-5-carboxamides of formula I

• • wherein R₁, R₂, R₃, R₄ and R₅ are as defined as set forth in the specification herein.

The invention discloses 5-benzyl-4-alkyl-2-aminothiazole as shown in a chemical structure formula I and pharmaceutically acceptable salts of the 5-benzyl-4-alkyl-2-aminothiazole as shown in the specification. A preparation method of the 5-benzyl-4-alkyl-2-aminothiazole is as follows: heating 2-haslogen-1-aryl alkyl ketone, alkyl thiourea and ethanol, stirring, and reacting for a certain time; filtering, drying to obtain5-benzyl-4-alkyl-2-aminothiazole salts; and filtering the obtained filter cake and neutralizing with ammonia water, and then obtaining 5-benzyl-4-alkyl-2-aminothiazole. The invention also discloses application of the 5-benzyl-4-alkyl-2-aminothiazole or salts thereof in preparing antitumor medicaments.

The invention discloses a 4, 5-disubstituted-2-aminothiazole compound. The structural formula is shown in the specification, wherein R1 is 4-tolyl, 4-chlorophenyl, 4-methoxyphenyl, 4-nitrobenzene or propoxy, and R2 is phenyl, 4-tolyl, 4-fluorophenyl, 4-methoxyphenyl, 2-furyl, isopropyl, 4-nitrophenyl or n-propyl. The invention simultaneously provides a preparation method of the 4, 5-disubstituted-2-aminothiazole compound. The preparation method comprises the following steps: enabling an olefin azide type compound and potassium thiocyanate to react at the temperature of 75-85 DEG C in the presence of a solvent and a metal catalyst, concentrating an obtained reaction solution, then extracting with water and ethyl acetate, washing an obtained organic layer, then drying and concentrating by a rotary evaporator; performing silica gel column chromatography on an obtained concentrate to obtain the 4, 5-disubstituted-2-aminothiazole compound.

The invention discloses a flame retardant containing phosphorus, nitrogen and sulfur and used for epoxy resin and a preparation method of the flame retardant. Firstly, DOPO and aminothiazole are taken as reaction raw materials and subjected to an Atherton-Todd reaction for preparation of the flame retardant containing phosphorus, nitrogen and sulfur. The process steps of the method are simple, the yield and the purity of the flame retardant are high, and the post-treatment process is simple and convenient. The flame retardant containing phosphorus, nitrogen and sulfur and prepared with the method is used for modifying cured epoxy resin and has good compatibility with epoxy resin, and the obtained cured flame-retardant epoxy resin has excellent flame retardancy; when the phosphorus content of the epoxy curing system reaches 0.43wt%-1.23wt%, the vertical burning grade can pass UL-94 V-0 level, and the limit oxygen index is as high as 36%.

The polishing solution for CMP of the invention comprises abrasive grains, a first additive and water, wherein the first additive is at least 1,2-benzoisothiazole-3(2H)-one or 2-aminothiazole. The polishing method of the invention is a polishing method for a substrate having a silicon oxide film on the surface, and the polishing method comprises a step of polishing the silicon oxide film with a polishing pad while supplying the polishing solution for CMP between the silicon oxide film and the polishing pad.

The present invention provides a reagent composition for detecting β-lactamase including as a β-lactamase detection substrate 3-[2,4-dinitrostyryl]-7-(2-thienylacetamido]-3-cephem-4-carboxylic acid, or 7-[2-(2-aminothiazol-4-yl)-2-(1-carboxy-1-methylethoxy-imino)acetamido]-3-(2,4-dinitrostyryl)-3-cephem-4-carboxylic acid, and at least one β-lactamase inhibitor selected from the group consisting of clavulanic acid, aztreonam, ethylenediaminetetraacetic acid, and cloxacillin, which composition can detect β-lactamases rapidly and easily with high sensitivity. The present invention also provides a detection kit including the detecting reagent composition. Further, the present invention provides a β-lactamase detection method where a liquid specimen containing a target substance to be analyzed is brought into contact with the composition.

A pharmaceutical composition for modified release, comprising (1) (R)-2-(2-aminothiazol-4-yl)-4′-[2-[(2-hydroxy-2-phenylethyl)amino]ethyl]acetic acid anilide, or a pharmaceutically acceptable salt thereof, (2) at least one additive which ensures penetration of water into the pharmaceutical composition and which has a solubility such that the volume of water required for dissolving 1 g of the additive is 5 mL or less, and (3) a hydrogel-forming polymer having an average molecular weight of approximately 100,000 or more, or a viscosity of 12 mPa·s or more at a 5% aqueous solution at 25° C. is disclosed.

2-Acylaminothiazole derivatives or salts thereof which have a platelet increasing activity based on an excellent human c-mpl-Ba/F3 cell growth function and a function of accelerating formation of megakaryocytic colonies and which are useful for treating thrombocytopenia are provided.

The invention provides a method for catalyzing gamma-valerolactone to be subjected to ring-opening polymerization by utilizing a biomimetic catalyst and belongs to the field of biomass high molecular materials. According to the method, the gamma-valerolactone is used as a monomer, the biomimetic catalyst is used as a catalyst and an alcohol compound is used as an initiator, and the gamma-valerolactone is subjected to the ring-opening polymerization in a solvent to obtain poly-gamma-valerolactone; the biomimetic catalyst is one or a mixture of more of a thioureaamide type dihydrogen bond donor catalyst, an aminothiazole type dihydrogen bond donor catalyst and a phenyl phosphate type dihydrogen bond donor catalyst. Compared with a traditional catalyst, the aminothiazole type biomimetic catalyst, the thioureaamide type biomimetic catalyst and the phenyl phosphate type biomimetic catalyst have no metal and the utilization amount is small; the catalysis effect is higher under the action of a dihydrogen bond.

The invention relates to 3-[[2-(benzylamino) thiazole-5-yl]-methyl] quinolone-2(1H)-ketone as shown in chemical structural formulas I and II or a salt thereof. In the chemical structural formulas, R, X<1> and X<2> are selected from hydrogen, deuterium, C1-C2 alkyl, C3-C4 linear-chain alkyl or branched-chain alkyl; X<3> is selected from hydroxyl, methoxyl and ethyoxyl; is selected from hydrogen, deuterium, C1-C2 alkyl, fluorine, fluorine or bromine; X4 and X6 are selected from hydrogen, deuterium, C1-C2 alkyl, fluorine, fluorine, bromine or nitryl; X5 and X7 are selected from hydrogen, deuterium and C1-C2 alkyl. The invention also provides an application of the 3-[[2-(benzylamino) thiazole-5-yl]-methyl] quinolone-2(1H)-ketone in preparation of an influenza virus neuraminidase inhibitor.

Provided is a cephem compound which has a wide antimicrobial spectrum, and in particular exhibit potent antimicrobial activity against beta-lactamase producing Gram negative bacteria, and pharmaceutical composition comprising the same.

A Compound of the formula (I):

wherein

• • W and U are as defined in the specification;
  • R¹ is as defined in the specification;
  • R^2A and R^2B are as defined in the specification, provided that R^2A and R^2B are not taken together to form an optionally substituted oxime group when R¹ is aminothiazole or aminothiadiazole optionally protected at the amino group;
  • ring A is a benzene ring or a 6-membered aromatic heterocyclic group having 1-3 nitrogen atoms;
  • R³ is a hydrogen atom, —OCH₃ or —NH—CH(═O);
  • k is an integer from 0 to 2;
  • R⁴ is as defined in the specification; and
  • D and E are as defined in accordance with a) or b) described in the specification.

The present invention relates to compounds of Formula (I),

methods for preparing these compounds, compositions, intermediates and derivatives thereof and for treating a condition including but not limited to ankylosing spondylitis, artherosclerosis, arthritis (such as rheumatoid arthritis, infectious arthritis, childhood arthritis, psoriatic arthritis, reactive arthritis), bone-related diseases (including those related to bone formation), breast cancer (including those unresponsive to anti-estrogen therapy), cardiovascular disorders, cartilage-related disease (such as cartilage injury/loss, cartilage degeneration, and those related to cartilage formation), chondrodysplasia, chondrosarcoma, chronic back injury, chronic bronchitis, chronic inflammatory airway disease, chronic obstructive pulmonary disease, diabetes, disorders of energy homeostasis, gout, pseudogout, lipid disorders, metabolic syndrome, multiple myeloma, obesity, osteoarthritis, osteogenesis imperfecta, osteolytic bone metastasis, osteomalacia, osteoporosis, Paget's disease, periodontal disease, polymyalgia rheumatica, Reiter's syndrome, repetitive stress injury, hyperglycemia, elevated blood glucose level, and insulin resistance.

This invention is directed to aminothiazole compounds of formula (I) wherein R<1> is a substituted or unsubstituted group selected from: C1-6-alkyl; C1-6-alkenyl; C1-6-alkynyl; C1-6-alkoxyl; C1-6-alcohol; carbocyclic or heterocyclic, monocyclic or fused or non-fused polycyclic, cycloalkyl; carbocyclic or heterocyclic, monocyclic or fused or non-fused polycyclic, aryl; carbonyl; ether; (C1-6-alkyl)-carbonyl; (C1-6-alkyl)-aryl; (C1-6-alkyl)-cycloalkyl; (C1-6-alkyl)-(C1-6-alkoxyl); aryl-(C1-6-alkoxyl); thioether; thiol; and sulfonyl; wherein when R<1> is substituted, each substituent independently is a halogen; haloalkyl; C1-6-alkyl; C1-6-alkenyl; C1-6-alkynyl; hydroxyl; C1-6-alkoxyl; amino; nitro; thiol; thioether; imine; cyano; amido; phosphonato; phosphine; carboxyl; thiocarbonyl; sulfonyl; sulfonamide; ketone; aldehyde; ester; oxygen; carbocyclic or heterocyclic, monocyclic or fused or non-fused polycyclic, cycloalkyl; or carbocyclic or heterocyclic, monocyclic or fused or non-fused polycyclic, aryl; and R<2 >is a carbocyclic or heterocyclic, monocyclic or fused or non-fused polycyclic, ring structure having a substituent at the position adjacent to the point of attachment, which ring structure is optionally further substituted, where each substituent of R<2> independently is a halogen; haloalkyl; C1-6-alkyl; C1-6-alkenyl; C1-6-alkynyl; hydroxyl; C1-6-alkoxyl; amino; nitro; thiol; thioether; imine; cyano; amido; phosphonato; phosphine; carboxyl; thiocarbonyl; sulfonyl; sulfonamide; ketone; aldehyde; ester; oxygen; carbocyclic or heterocyclic, monocyclic or fused or non-fused polycyclic, cycloalkyl; or carbocyclic or heterocyclic, monocyclic or fused or non-fused polycyclic, aryl; or a pharmaceutically acceptable salt of a compound of formula (I), or a prodrug or pharmaceutically active metabolite of a compound of formula (I) or pharmaceutically acceptable salt thereof, for inhibiting cyclin-dependent kinases (CDKs), such as CDK1, CDK2, CDK4, and CDK6.

The invention provides a compound of aztreonam and a synthetic method thereof. In the method, general solvents are used, suitable amines are chosen, (2-aminothiazole-4-group)-2-(tert-butoxycarbonyl)-iminodiacetic acid isopropoxide acid-2-ester mercaptobenzothiazole and (3-S-trans form)-3-amino-4-methyl-2-oxo-1-sulfonic acid azetidine are used as intermediates; therefore, the method simplifies reaction and has good effect on depriving protecting groups by the mixed aqueous solution of acetic acid and hydrochloric acid.