135 results about "Diaminopyrimidine" patented technology

Methods for treating respiratory and gastrointestinal diseases mediated by a P2X3 and / or a P2X2 / 3 receptor antagonist, the methods comprising administering to a subject in need thereof an effective amount of a compound of formula (I): or a pharmaceutically acceptable salt thereof, wherein D, X, Y, R1, R2, R3, R4, R5, R6, R7 and R8 are as defined herein.

Compounds of the formula I: or pharmaceutically acceptable salts thereof, wherein A, D, E, G, J, X, Y, Z R6, R7 and R8 are as defined herein. Also provided are methods of using the compounds for treating diseases mediated by a P2X3 and / or a P2X2 / 3 receptor antagonist and methods of making the compounds.

Compounds and methods for treating diseases mediated by a P2X3 and / or a P2X2 / 3 receptor antagonist, the methods comprising administering to a subject in need thereof an effective amount of a compound of formula (I): wherein D, X, R1, R2, R3, R4, R5, R6, R7 and R8 are as defined herein.

Compounds and methods for treating diseases mediated by a P2X3 and / or a P2X2 / 3 receptor antagonist, the compounds being of formula (I): wherein D, X, R1, R2, R3, R4, R5, R6, R7 and R8 are as defined herein.

Compounds and methods for treating diseases mediated by a P2X3 and / or a P2X2 / 3 receptor antagonist, the methods comprising administering to a subject in need thereof an effective amount of a compound of formula (I): or a pharmaceutically acceptable salt, solvate or prodrug thereof, wherein D, X, Y, R1, R2, R3, R4, R5, R6, R7 and R8 are as defined herein.

Compounds and methods for treating diseases mediated by a P2X3 and / or a P2X2 / 3 receptor antagonist, the methods comprising administering to a subject in need thereof an effective amount of a compound of formula (I):wherein D, X, R1, R2, R3, R4, R5, R6, R7 and R8 are as defined herein.

A method for inhibiting neoplasia, particularly cancerous and precancerous lesions by exposing the affected cells to 4,5-diaminopyrimidine derivatives.

The present invention is related to compounds of formula (I), or a therapeutically suitable salt or prodrug thereof, the preparation of the compounds, compositions containing the compounds and the use of the compounds in the prevention or treatment of disorders regulated by the action of ghrelin receptor, including Prader-Willi syndrome, eating disorder, weight gain, weight-loss maintainance following diet and exercise, obesity, and disorders associated with obesity such as noninsulin dependent diabetes mellitus.

Compounds and methods for treating diseases mediated by a P2X3 and / or a P2X2 / 3 receptor antagonist, the methods comprising administering to a subject in need thereof an effective amount of a compound of formula (I):or a pharmaceutically acceptable salt, solvate or prodrug thereof,wherein D, X, Y, R1, R2, R3, R4, R5, R6, R7 and R8 are as defined herein.

The present invention relates to a method of making a compound of the formulawherein X1, X2 and R3—R4 are as defined herein. The method includes reacting a compound of the formulawith an amine of formula 3 (HNR3R4) in the presence of a Lewis Acid and a non-nucleophilic base. The 2,4-diamino pyrimidine moiety is a common component in a variety of biologically active drug-like molecules and pyrimidine derivatives have been found to be useful in the treatment of abnormal cell growth, such as cancer, in mammals.

A process for preparing 4,6-diaminopyrimido[5,4-d]pyrimidines of formula I, wherein R1 denotes a hydrogen atom or a C1-C6 alkyl group, R2 denotes an optionally substituted C6-C10 aryl group, R3 denotes a hydrogen atom or a C1-C6 alkyl group, and R4 denotes a hydrogen atom or an optionally substituted C1-C6 alkyl, C3-C6 alkenyl, C3-C8cycloalkyl or a 4- to 7-membered, nitrogen-containing heterocyclyl group, or R3 and R4 together with the nitrogen atom linked to them denote an optionally substituted heterocyclyl group.

The invention provides series amiopyrimidine-modified gold nano particles. In the amiopyrimidine-modified gold nano particles, the amiopyrimidine may be one or more of 2-thiol-4,6-diamino-pyrimidine, 2-thiol-4-amino-pyrimidine and 2,4-diamino-6-mercaptopyrimidine. The particle size of the amiopyrimidine-modified gold nano particles is 1.5 to 10.0 nanometers; and the molar content ratio of amiopyrimidine molecules to gold element in the nano particles ranges from 0.1 to 0.9. The amiopyrimidine-modified gold nano particles have antibacterial effect, can be widely used for preparing antibacterial medicines such as anti-gram-negative bacilli penicillins medicines, anti-gram-positive bacterium medicines or / and anti-multi-medicine-resistance clinically isolated bacterium medicines. The invention also provides the preparation method and use of the amiopyrimidine-modified gold nano particles. The invention further provides antibacterial medicines containing the amiopyrimidine-modified gold nano particles.

Methods for treating respiratory and gastrointestinal diseases mediated by a P2X3 and / or a P2X2 / 3 receptor antagonist, the methods comprising administering to a subject in need thereof an effective amount of a compound of formula (I):or a pharmaceutically acceptable salt thereof,wherein D, X, Y, R1, R2, R3, R4, R5, R6, R7 and R8 are as defined herein.

The invention provides a diaminopyrimidine compound and a composition containing the same and discloses the diaminopyrimidine compound shown as in a formula (I) and a drug combination containing the compound or salt thereof acceptable in crystal form and pharmacy, hydrate or solvent complex, stereoisomer, pro-drug or isotope variant. The diaminopyrimidine compound and the composition containing the same have excellent inhibition effect on protein kinase and have better pharmacokinetic parameter characteristics, and drug concentration of the compound in animal bodies can be increased to improve drug efficacy and safety.

Compounds within the scope of the present invention have a Formula 1or a salt or prodrug thereof, where ring A is selected from cycloaliphatic; ring B is aryl; R1 is selected from (C1-C10)alkyl, (C3-C10)cycloalkyl, halo, aryl, and heteroaryl; and R2 and R3 are independently selected from hydrogen and (C1-C6)alkyl. Disclosed compounds may have an IRAK4 IC50 of from 0.003 μM to 3.7 μM; a TAK1 IC50 of from 0.008 μM to 132 μM; and / or an IRAK4 / TAK1 selectivity of from 1 to 450. Particular compounds may have an IRAK4 / TAK1 selectivity of from 100 to 500. Disclosed compositions may be formulated as pharmaceutical compositions. A method for using the compounds and / or compositions also are disclosed. The method may comprise administering to a subject an effective amount of a compound within the scope of the present invention, particularly to selectively inhibit IRAK 1 and / or IRAK4 over TAK1.

The invention discloses a hair-growing composition and application thereof. The hair-growing composition is mainly prepared from the following components in parts by mass: 0.1 to 5 parts of pyrrolidyldiaminopyrimidine oxide and 0.1 to 5 parts of dimethyl sulfone, wherein the pyrrolidyl diaminopyrimidine oxide can promote the telophase in the hair life cycle to be changed into anagen; the dimethylsulfone provides an organic sulfur nutrient source as a necessary condition for the synthesis of keratin fibers and also can remove free radicals and inhibit inflammation; by combined use of the twosubstances, multiple effects of promoting blood circulation, opening potassium channels, and promoting the proliferation of hair follicle cells and the expression of human keratin fibers can be realized; a good hair growth effect is achieved from inside to outside.

A method for preparing a compound of formula kor a salt or solvate thereof,wherein R1 is as defined herein,the method comprising treating a compound of formula jor a salt or solvate thereof,with ammonia, to form the compound of formula k.

Compounds and methods for treating diseases mediated by a P2X3 and / or a P2X2 / 3 receptor antagonist, the compounds being of formula (I):wherein D, X, R1, R2, R3, R4, R5, R6, R7 and R8 are as defined herein.

The present invention relates to a novel production method of a diaminopyrimidine compound useful as an intermediate for various compounds having a pharmacological activity, a novel intermediate useful for producing said compound, and a production method of the intermediate.The present invention provides a novel 5-aminopyrimidine compound represented by the following formula (2) and a novel 4,5-diaminopyrimidine compound represented by the formula (3), as well as production methods of the compounds of the following formulas (2) to (6).wherein each symbol is as defined in the specification.

The invention provides substituted diaminopyrimidine compound, a composition comprising the compound and application of the compound. The substituted diaminopyrimidine compound is diaminopyrimidine compound shown as in formula (I) or its crystal-form pharmaceutically acceptable salts and prodrugs, and stereoisomer, hydrate or solvent compound. The substituted diaminopyrimidine compound disclosed herein and the composition comprising the compound have excellent inhibitory action on EGFR (epidermal growth factor receptor) kinase, have better pharmacokinetics parameter characteristics, and can increase the drug concentration of the compound in an animal body to provide improved drug therapeutic effect and safety.

The invention provides a substituted diaminopyrimidine compound and medicinal salt thereof. The structure of the substituted diaminopyrimidine compound is as shown in a general formula (I). A pharmacodynamic test proves that the compound is capable of effectively inhibiting growth of multiple tumor cells and can be used for preparing anti-tumor drugs, and meanwhile, the drug resistance of EGFR T790M can be overcome.

A method for preparing a compound of formula Ithe method comprising treating a compound of formula dwith an iodination reagent, to form the compound of formula I, wherein R1, R2 and R3 are as defined herein.

The invention relates to an anti-hair loss and hair-strengthening nutrient solution and a preparation method thereof. The anti-hair loss and hair-strengthening nutrient solution is prepared from the following raw material components in parts by weight: 80 to 90 parts of compound plant extract, 5 to 9 parts of a hair conditioner, 3.5 to 10 parts of a humectant and 0.2 to 0.4 part of a thickening agent, wherein the composite plant extract is a mixture of water, a cacumen biotae extract, a radix polygoni multiflori extract, a ginger root extract, a folium mori extract, a black mulberry fruit extract, a sesame seed extract and a ginseng root extract, and the hair conditioner is a mixture of water, propylene glycol, glycerol, 1, 2-hexanediol, diaminopyrimidine oxide, polyglycerol-6 myristate, caprylic / capric triglyceride, pyrrolidinyl diaminopyrimidine oxide, lecithin, hydroxylated lecithin and cholesterin. The anti-hair loss and hair-strengthening nutrient solution has good effects of strengthening and toughening hair roots, preventing hair loss and promoting hair growth.

The present invention encompasses compounds of general formula (1) wherein Q and R1 to R4 are defined as in claim 1, which are suitable for the treatment of diseases characterised by excessive or anomalous cell proliferation, and their use for preparing a pharmaceutical composition having the above-mentioned properties.

Novel compounds according to the formula and pharmaceutically acceptable salts, solvates, or hydrates thereof; whereineach occurrence of A is independently selected from CH or N;X is selected from the group consisting of —CH2—, —O—, —NH—, (C1-C6)alkylamino-, (C1-C6)alkylaminocarbonylamino-, (C1-C6)alkylcarbonylamino-, (C1-C6)alkylsulfonylamino-, phenylsulfonylamino-, carbonyl, —NH—C(O)—, —N(C1-C6)alkyl-C(O)—, —S(O)y— where y is 0, 1 or 2, and;n in —(CH2)n— is 1, 2 or 3; andR1, R2, and R3 are as described herein; pharmaceutical compositions that including these compounds, and methods for the treatment of autoimmune disease, inflammation, allergy, transplant rejection, and other circumstances where administration of an immunosuppressive agent is of therapeutic benefit.

Methods for treating respiratory and gastrointestinal diseases mediated by a P2X3 and / or a P2X2 / 3 receptor antagonist, the methods comprising administering to a subject in need thereof an effective amount of a compound of formula (I):or a pharmaceutically acceptable salt thereof,wherein D, X, Y, R1, R2, R3, R4, R5, R6, R7 and R8 are as defined herein.

The invention discloses an anti-loss hair-growth liquid and a preparation method thereof, a composition thereof comprises: a phase A comprising adenosine, nicotinamide, and water; a phase B comprisingdipotassium glycyrrhizinate and pyridoxine HCl; a phase C comprising an acrylate copolymer and water; a phase D comprising sodium hydroxide and water; a phase E comprising water, beeswax, hydroxyethyl behenamide propyl dimethyl ammonium chloride, behenyl alcohol, an avocado fruit extract, phenoxyethanol, ethylhexylglycerin, an apple fruit extract, a biota orientalis extract, a leaf extract of Ilex aquifolium, a mulberry leaf extract, and propylene glycol; a phase F comprising propylene glycol, the avocado extract, caffeine, beeswax, hydroxyethyl behenamide propyl dimethyl ammonium chloride, behenyl alcohol, phenoxyethanol, ethylhexyl glycerol, and water; a phase G comprising ethanol, biotin, pyrrole alkyl diaminopyrimidine oxide, and water; and a phase H comprising phenoxyethanol. The invention also provides a preparation method of the anti-loss hair-growth liquid. The anti-loss hair-growth liquid has the advantages of scientific ratio, safety, and non-toxic side effects, and can effectively promote hair growth.

The invention relates to a pyrimidopyrimidine compound and a nucleoside analog derivative thereof. The pyrimidopyrimidine compound and the nucleoside analog derivative thereof prepared in the invention have certain hepatitis virus inhibition activities, and 4,7-diamino-1-(beta-2-deoxy-D-ribofuranose)pyrimido[4,5-d]pyrimidine-2,5(1H,6H)-dione and 4,7-diaminopyrimido[4,5-d]pyrimidine-2,5(1H,6H)-dione perform obvious virus copying inhibition potentials and are better than ribavirin, so a new selection is provided for clinical medicines.