580 results about "Propargyl" patented technology

The invention relates to posttranslational modification of phage-displayed polypeptides. These displayed polypeptides comprise at least one unnatural amino acid, e.g., an aryl-azide amino acid such as p-azido-L-phenylalanine, or an alkynyl-amino acid such as para-propargyloxyphenylalanine, which are incorporated into the phage-displayed fusion polypeptide at a selected position by using an in vivo orthogonal translation system comprising a suitable orthogonal aminoacyl-tRNA synthetase and a suitable orthogonal tRNA species. These unnatural amino acids advantageously provide targets for posttranslational modifications such as azide-alkyne [3+2] cycloaddition reactions and Staudinger modifications.

This invention is directed to compounds of the following formula:wherein when a is 0, b is 1 or 2; when a is 1, b is 1, m is from 0-3, X is 0 or S, Y is halogeno, R1 is hydrogen C1-4 alkyl, R2 is hydrogen, C1-4 alkyl, or optionally substituted propargyl and R1 and R4 are each independently hydrogen, C1-6 alkyl, C6-12 aryl, C6-12 aralkyl each optionally substituted.This invention is also directed to the use of these compounds for treating depression, Attention Deficit Disorder (ADD), Attention Deficit and Hyperactivity Disorder (ADHD), Tourette's Syndrome. Alzheimer's Disease and other dementia's such as senile dementia, dementia of the Parkinson's type, vascular dementia and Lewy body dementia.This invention is further directed to a pharmaceutical composition comprising a therapeutically effective amount of the above-defined compounds and a pharmaceutically acceptable carrier.

A process for isolating from a reaction mixture a salt of a mono-propargylated aminoindan, a process for isolating from a reaction mixture a crystalline diastereomeric salt of a mono-propargylated aminoindan, and a process for isolating from a reaction mixture a salt of enantiomerically pure N-propargyl-1-aminoindan or a salt of enantiomerically pure 6-(N-methyl, N-ethyl-carbamoyloxy)-N′-propargyl-1-aminoindan. The corresponding products are also disclosed.

Disclosed is crystalline R(+)-N-propargyl-1-aminoindan and racemic N-propargyl-1-aminoindan characterized by colorless crystals a pharmaceutical composition comprising the same, and the process for the manufacture and the validation thereof. Also disclosed is pure liquid R(+)-N-propargyl-1-aminoindan and a pharmaceutical composition comprising the same, and the process for the manufacture thereof.

Disclosed are pharmaceutical preparations of R(+)-N-propargyl-1-aminoindan salts having enhanced content uniformity, processes for preparation of the compositions, and their uses.

The present invention provides (1) a sulfone compounds having a propargyl group, (2) a nonaqueous electrolytic solution for lithium secondary batteries, which comprises an electrolyte salt dissolved in a nonaqueous solvent and contains a sulfone compound having a specific structure that has an SO2 group with a propargyl group or a vinyl group bonding thereto, in an amount of from 0.01 to 10% by weight of the nonaqueous electrolytic solution, and which can prevent gas generation and is excellent in battery characteristics such as cycle property and the like, and (3) a lithium secondary battery comprising a positive electrode, a negative electrode and a nonaqueous electrolytic solution of an electrolyte salt dissolved in a nonaqueous solvent, wherein the nonaqueous electrolytic solution contains a sulfone compound having a specific structure, in an amount of from 0.01 to 10% by weight of the nonaqueous electrolytic solution.

The subject invention provides crystalline R(+)-N-propargyl-1-aminoindan, pharmaceutical compositions and methods of manufacture thereof.

Novel iron chelators exhibiting neuroprotective and good transport properties are useful in iron chelation therapy for treatment of a disease, disorder or condition associated with iron overload and oxidative stress, eg. a neurodegenerative or cerebrovascular disease or disorder, a neoplastic disease, hemochromatosis, thalassemia, a cardiovascular disease, diabetes, a inflammatory disorder, anthracycline cardiotoxicity, a viral infection, a protozoal infection, a yeast infection, retarding ageing, and prevention and / or treatment of skin ageing and skin protection against sunlight and / or UV light. The iron chelator function is provided by a 8-hydroxyquinoline, a hydroxypyridinone or a hydroxamate moiety, the neuroprotective function is imparted to the compound e.g. by a neuroprotective peptide, and a combined antiapoptotic and neuroprotective function by a propargyl group.

The present invention provides an acid sensitive doxorubicin prodrug based on polyethylene glycol, and a method and an application of the acid sensitive doxorubicin prodrug based on polyethylene glycol. The preparation method comprises: preparing a polyethylene glycol whose end contains an acid sensitive acetal group and a p-nitrophenyl ester azide group by a reaction of a polyethylene glycol whose double ends contain diazido ethyl diacetal groups with a p-nitro phenyl propargyl carbonate; preparing the acid sensitive doxorubicin prodrug based on the polyethylene glycol by the reaction of the prepared polyethylene glycol with doxorubicin hydrochloride. The acid sensitive and water soluble doxorubicin prodrug has good biocompatibility and acid sensitivity, thereby being used as a stimulation sensitive antineoplastic prodrug.

The invention relates to 2-[4-(quinoxaline-2-oxygroup) phenoxy] alkylamide shown as a chemical structural formula I or an optical isomer thereof. In the formula, R1 is selected from H, C1-C1alkyl, C3-C4 straight-chain or branch-chain alkyl; R2 is selected from allyl, propargyl, halogenated allyl, halogenated propargyl; and X1-X6 are selected from hydrogen, C1-C2 alkyl, trifluoromethyl, fluorine, chlorine, bromine, nitryl or trifluoromethoxy. The invention further discloses an application of 2-[4-(quinoxaline-2-oxygroup) phenoxy] alkylamide or the optical isomer thereof in preparation of anti-lung adenocarcinoma drugs.

The invention belongs to the field of pharmacy, and relates to application of a hydrogen sulfide donor to the preparation of a medicine for treating central nervous system disease, in particular to application of the hydrogen sulfide donor, namely sodium hydrosulfide, or allyl cysteine and analogues thereof to the preparation of the medicine for treating the central nervous system disease. Integral animal model experiments prove that the sodium hydrosulfide and propargyl cysteine can reduce the learning and memory impairment of rats, increase the content of hydrogen sulfide in hippocampus tissues of the rats, inhibit the messenger ribonucleic acid (mRNA) expression of a tumor necrosis factor alpha and a receptor I thereof, inhibit an inflammatory mediator in the hippocampus tissues of rats with dementia and inhibit inflammation-related enzymes in the hippocampus tissues of the rats, and can be used as a medicine for treating Alzheimer disease and other inflammation-related central nervous system degenerative diseases such as Parkinson disease.

The invention provides branched copolymers as precursors for preparing silicon carbide (SiC) ceramics represented by the general formulae:[Si(˜)RC(˜)H]xn[SiR1R2CH2]yn,Formula Type-Iwherein n is the degree of polymerization, 0.1≦x<0.8, 0.2≦y<0.9 and x+y=1; and R=methyl or H, R1 and R2 are randomly composed of hydrogen (H), allyl, methyl (Me), phenyl (Ph), propargyl or vinyl. Another branched copolymer is represented by the general formula:[Si(˜)RC(˜)H]xn[SiR1R2CH2]yn[SiR3R4CH2]znFormula Type-IIwherein n is the degree of polymerization, 0.1≦x<0.8, 0≦y<0.8, 0.2≦z<0.8 and x+y+z=1; and R=methyl or H, R1 and R2 are randomly composed of hydrogen (H), methyl (Me) and phenyl; R3 and R4 are randomly composed of H, allyl, methyl, phenyl (Ph), propargyl, and vinyl. The invention also provides methods for the preparation of such branched copolymers.

The present invention relates to a method for assessing the sensitivity of a patient's cancer to treatment with 10-propargyl-10-deazaminopterin and a method for selecting a patient for treatment of cancer with 10-propargyl-10-deazaminopterin, by determining the amount of a EGFR or other growth factor expressed by the cancer and comparing the amount with the amount of EGFR or other growth factor expressed by a reference cancer.

The invention relates to 2-(4-aryloxyphenoxy)alkylamide represented by a chemical structural formula I or an optical isomer thereof, wherein R1 is selected from H, C1-C1 alkyl, and C3-C4 straight-chain or branched-chain alkyl; R2 is selected from allyl, propargyl, halogenated allyl, and halogenated propargyl; X1-X6 are selected from hydrogen, C1-C2 alkyl, fluoro, chloro, bromo, or cyan. The invention also relates to the application of the 2-(4-aryloxyphenoxy)alkylamide or the optical isomer thereof in preparing anti-lung-adenocarcinoma medicines.

The invention relates to a method for preparing 1-propene-3-sultone, and the technical field of preparation of organic materials. The method mainly comprises the processes of addition, acidation and cyclization: a, addition, namely an addition reaction of propargyl ethanol and alkali metal sulphite or hydrosulfite is carried out in an aqueous solution, the molar ratio of the propargyl alcohol to the alkali metal sulphite or the hydrosulfite is 1:1-10, and inorganic acid or organic acid is added to stop reaction after the addition reaction is ended; and b, a product of the addition reaction isseparated out, and then the separated product is subjected to cyclization and separation to obtain a 1-propene-3-sultone product. The PST product can be refined. The method overcomes the defect of the prior art, and has the remarkable advantages of unique method, simple manufacturing process, easy operation, mild reaction conditions, cheap and easily-obtained raw materials, higher yield, good selectivity, high and stable quality of products, few three wastes, lower cost, remarkable economic benefit, and the like.

Process for the preparation of unsaturated 4,5-allene ketones by reaction of tertiary propargyl alcohols with alkenyl alkyl ethers or ketals in the presence of aliphatic sulfonic acids or sulfonic acid salts.

Disclosed is crystalline R(+)-N-propargyl-1-aminoindan and racemic N-propargyl-1-aminoindan characterized by colorless crystals a pharmaceutical composition comprising the same, and the process for the manufacture and the validation thereof. Also disclosed is pure liquid R(+)-N-propargyl-1-aminoindan and a pharmaceutical composition comprising the same, and the process for the manufacture thereof.

The invention relates to a method for synthesizing chiral beta-acetenyl ketone by catalytic intermolecular decarboxylation from beta-ketonic acid and a propargyl compound. A chiral copper catalyst adopted in the invention is synthesized in stiu from a copper salt and a chiral P,N,N-tridentate ligand in various polar solvents and nonpolar solvents. According to the invention, various chiral beta-acetenyl ketone compounds with substituent groups can be synthesized conveniently, and can obtain a percent enantiomeric excess as high as 95%. The method in the invention is advantaged by operational simplicity, available raw materials, wide substrate application range, high enantioselectivity, and the like.

The invention provides a method for synthesizing 1,6-eneyne compounds. The method is an effective method which synthesizes the optically active 1,6-eneyne compounds with high regioselectivity and enantioselectivity by using iridium complex as a catalyst as well as allyl carbonate compounds and a propargyl nucleophilic reagent as raw materials. The method has the advantages of readily available catalyst, high catalytic activity, mild reaction temperature, wide substrate application range and high product regioselectivity and enantioselectivity.

The invention provides poly (gamma-propargyl-L-glutamate)-polyamino acid segmented copolymer. The poly (gamma-propargyl-L-glutamate)-polyamino acid segmented copolymer is presented as the formula (I). Small molecules containing primary amino radical serve as an initiator, and the poly (gamma-propargyl-L-glutamate)-polyamino acid segmented copolymer is obtained through the gradual ring cleavage reaction of gamma- propargyl-L-glutamate-N-carboxylic acid anhydride and amino acid-N- carboxylic acid anhydride. The side chain of the segmented copolymer is propargyl which is easy to modify, has high reactivity and is beneficial to functional small molecules which are subjected to bonded azide and have biological activity or environmental responsiveness, and the bonding process cannot lead to the breakage of amino acid backbones and is not affected by the amount and steric hindrance of functional small molecules. The segmented copolymer has good biocompatibility after being functionalized and can be applied in fields such as targeted drug delivery, organizational projects and protein separation and detection.

The invention discloses a method for catalytic synthesis of a chiral propargylamine compound by a chiral copper catalyst. The method comprises the following steps that a copper salt and a chiral P, N, N-ligand undergo an in-suit reaction in the presence of an alcohol solvent to produce a chiral copper catalyst; and a propargyl compound and primary amine or secondary amine undergo a displacement reaction in the presence of the chiral copper catalyst to produce the chiral propargylamine compound. The method can realize convenient synthesis of various propargylamine compounds, and has the maximum yield of 92% and enantioselectivity (ee) of 97%. The method has simple processes, strong catalytic system universality and high enantioselectivity.

Sensitivity of a patient's cancer to treatment with 10-propargyl-10-deazaaminopterin is assessed and patients are selected for treatment of cancer with 10-propargyl-10-deazaaminopterin, by determining the amount of a selected polypeptide expressed by the cancer and comparing the amount with the amount of the selected polypeptide expressed by a reference cancer. The polypeptide includes a member of a folate pathway polypeptide within a cell and may include at least one of reduced folate carrier-1 enzyme (RFC-1), dihydrofolate reductase (DHFR), folylpoly-gamma-glutamate synthetase (FPGS), thymidylate synthase (TS), γ-glutamyl hydrolase (GGH), and glycinamide ribonucleotide formyltransferase (GARFT).

The invention discloses a lithium iron phosphate power battery with an improved low temperature charge performance, belongs to the technical field of lithium iron phosphate power batteries, and aims to solve the problem that the negative pole can easily reach a cut-off voltage, and the charge capacity is reduced therefore. The lithium iron phosphate power battery is characterized by comprising a positive plate, a negative plate, and electrolyte. The lithium salt is lithium hexafluorophosphate (11.5-15.0%). The organic solvent is a four component mixed solvent, which is composed of propylene carbonate, methyl carbonate, ethyl carbonate, and diethyl carbonate according to a ratio of 10-40: 1-10: 20-50: 10-30. The additive is one or more of vinylene carbonate, fluoroethylene carbonate, propargyl sulfonate, lithium difluorophosphate, lithium difluoro(oxalato)borate, and lithium tetrafluoro(oxalato)phosphate. The interface impedance of the negative pole can be reduced, the low temperature properties of the lithium iron phosphate power battery are obviously improved, and the low temperature charge performance of the lithium iron phosphate power battery is improved.

The invention discloses 1-(1,2,4-triazole triazole-1- group)ketoxime ether or its nitrate as shown in the chemical structure formula I, wherein R<1> is selected from the group consisting of C1-2alkyl, C3-4straight chain or branched alkyl; R is selected from the group consisting of C1-C2alkyl, C3-C18 straight chain or branched alkyl or alicyclic groups; allyl, propargyl, 2-methyl allyl, 2-chlorallyl, (Z)-3-chlorallyl, (E)-3-chlorallyl, or ArCH2; or Y(CH2)n:Y equals to fluorine, chlorine, bromine or iodine, n equals to 1,2,3,4,5 or 6. The application of 1-(1,2,4-triazole triazole-1- group)ketoxime ether or its nitrate as shown in the formula I in the preparation of a bactericide for killing wheat powdery mildew or Botrytis cinerea.

Compounds of Formula I and Formula IA are inhibitors of dihydrofolate reductase and are suitable for use in compositions and methods for dihydrofolate reductase inhibition or, more specifically, treatment of a fungal infection, a bacterial infection or a protozoal infection, and, in specific embodiments, treatment of a fungal infection caused by C. albicans or C. glabrata:wherein R, R1, R2, R3, R4, A, B, E, V, W, X, Y and Z are as defined herein.

The invention discloses quaternary ammonium salt type hyperbranched polythioether modified polymer microspheres and a preparation method thereof. The preparation method comprises the following steps of: under a photo-initiation condition, taking polyethylene glycol as a pore-foaming agent, taking alkyl dithiol, propargyl glycidyl ether and 1,7-octadiyne as raw materials, and preparing epoxy groupmicroporous polymer spheres by using a sulfydryl-alkyne addition suspension polymerization method; then, under the condition of 0 DEG C, taking methanol as a solvent, and initiating allyl glycidyl ether and a cysteamine compound by ultraviolet light to react to synthesize an [alpha]-epoxy-[omega]-ammonium-based intermediate; and, in a solvent and under the condition of 60 DEG C, synthesizing the hyperbranched ammonium polythioether modified polymer microspheres from the epoxy group microporous polymer spheres, the [alpha]-epoxy-[omega]-ammonium-based intermediate and sodium methoxide in one step. The obtained product has a good killing effect on escherichia coli, and the modified polymer microspheres can be recycled through simple filtration.