134 results about "Diaminopyrimidine" patented technology

Methods for treating respiratory and gastrointestinal diseases mediated by a P2X₃ and/or a P2X_2/3 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 P2X_2/3 receptor antagonist and methods of making the compounds.

Compounds and methods for treating diseases mediated by a P2X₃ and/or a P2X_2/3 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 P2X_2/3 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.

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.

Methods for treating cough, chronic cough and urges to cough associated with respiratory diseases with 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 R¹ and R² are as defined herein.

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 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 1

or 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.

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.

Compounds of formula (I):

wherein R¹ and R² are as defined herein. Also disclosed are methods of making and using the subject compounds.

Novel compounds according to the formula

• • and pharmaceutically acceptable salts, solvates, or hydrates thereof; wherein
  • each 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; and
  • R¹, 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.

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.