3708 results about "Pyrimidine" patented technology

Provided are compounds of Formula I:nucleosides, nucleoside phosphates and prodrugs thereof, wherein R6 is CN, ethenyl, 2-haloethen-1-yl, or (C2-C8)-alkyn-1-yl. The compounds, compositions, and methods provided are useful for the treatment of Flaviviridae virus infections.

Provided herein are compounds of Formula (IV-b), or pharmaceutically acceptable salts thereof, that inhibit a KRas protein (e.g., a dysregulated KRas protein (e.g., a mutated or amplified KRas protein)). This disclosure also provides compositions containing the compounds as provided herein, or pharmaceutically acceptable salts thereof, as well as methods of using and making the same.

The present invention relates to crystalline forms of salts of the KRas G12C inhibitor 2-[(2b)-4- [7-(8-chloro-1-naphthyl)-2-[[(25)-1-methylpyrrolidin-2-yl]methoxy]-6,8-dihydro-5H -pyrido [3,4- d]pyrimidin-4-yl]-1-(2-fluoroprop-2-enoyl)piperazin-2-yl]acetonitrile, pharmaceutical compositions comprising the crystalline forms, processes for preparing the crystalline forms and methods of use thereof.

The present invention covers imidazo pyrimidine compounds of general formula (I), in which R1, R2, R3, R4 and Z are as defined herein, methods of preparing said compounds, intermediate compounds useful for preparing said compounds, pharmaceutical compositions and combinations comprising said compounds and the use of said compounds for manufacturing pharmaceutical compositions for the treatment or prophylaxis of diseases, in particular of neoplastic disorders, respectively cancer or conditions with dysregulated immune responses or other disorders associated with aberrant KRAS signaling, as a sole agent or in combination with other active ingredients.

The invention provides a pyridopyrimidine derivative as a small GTP enzyme KRAS mutation inhibitor, and particularly provides a pyridopyrimidine derivative with a structural formula as shown in a general formula (A) and pharmaceutically acceptable salts thereof, and the pyridopyrimidine derivative has inhibitory activity on mutants such as KRAS G12D and the like. The invention also provides a preparation method of the derivative, a pharmaceutical composition and a salifying compound of the derivative, and medical application of the derivative as a small GTP enzyme KRAS mutation inhibitor in treatment of different types of tumors.

The invention belongs to the technical field of medicines, and relates to tetrahydropyridopyrimidine compounds as well as a preparation method and application thereof, in particular to tetrahydropyridopyrimidine compounds or pharmaceutically acceptable salts thereof as well as a preparation method and application thereof in preparation of antitumor drugs. The structure of the tetrahydropyridopyrimidine compound or the pharmaceutically acceptable salt thereof is as shown in a general formula (I), and R1-R4 are as shown in the specification and claims. The compound provided by the invention can be used for preparing a KRAS G12C inhibitor, is used for inhibiting G12C mutation of KRAS, has an obvious inhibiting effect on lung cancer, pancreatic cancer or colon cancer, and can be used for preparing antitumor drugs. # imgabs0 #

Provided are a pyrimidine polycyclic derivative inhibitor, a preparation method therefor and the use thereof. In particular, provided are a compound as shown in the general formula, a preparation method therefor, a pharmaceutical composition comprising the compound, and the use thereof in the treatment of cancers and other related diseases.

The present disclosure relates generally to methods for treating or preventing central nervous system (CNS) metastases with a KRAS inhibitor, and more specifically to treating CNS metastases with a pyridopyrimidine derivative.

The present invention relates to a KRASG12D inhibitor and the use thereof. Specifically, provided in the present invention is a compound as shown in formula (I), and the definition of each substituent in the formula is as described in the description. In addition, the present invention further relates to a composition containing the inhibitor and the use thereof. The compound of the present invention has good tumor growth inhibitory activity, and has good safety.

The present invention belongs to the technical field of medicinal chemistry, and particularly relates to a pyrimidine macrocyclic compound. The compound has a good inhibitory effect on KRAS mutations, has a good inhibitory effect on the G12V mutation and other types of mutations of the KRAS gene, can be used as a general KRAS inhibitor, and can be used for the treatment of tumors driven by KRASG12V and other types of gene mutations.

Provided are a crystal form of a pyridopyrimidine derivative, a preparation method therefor, a pharmaceutical composition thereof and the use thereof. Specifically disclosed are a crystal form of a compound of formula (I), a preparation method therefor, a pharmaceutical composition thereof and the use thereof.

The present disclosure relates generally to methods for treating cancer with a KRAS inhibitor in combination with an immune checkpoint inhibitor, and more specifically to treating cancer with a pyridopyrimidine derivative in combination with a PD-1 or PD-L1 inhibitor.

The invention discloses a preparation method of a non-additive nitrogen-phosphorus-cerium synergistic flame-retardant polyurethane elastomer, and the polyurethane elastomer is prepared by taking isocyanate as a hard segment and poly (1, 4-butanediol adipate) as a soft segment, and compounding the hard segment and the soft segment with 2-amino-4-hydroxy-6-methylpyrimidine, a phosphorus reactive flame retardant and cerium oxide. The preparation method is simple, the process is easy to control, and the prepared polyurethane elastomer has good tensile strength; besides, the limit oxygen index of the polyurethane elastomer reaches 27.4, the polyurethane elastomer meets commercial standards of flame-retardant materials and UL-94 V-0 flame-retardant grade requirements, the ultraviolet band light transmittance is 0%, ultraviolet rays can be completely isolated, and the polyurethane elastomer has a good anti-oxidation function and can be applied to the industries of wires, cables, pipe profiles, films, general molding and the like.

Methods for treating prostate cancer, including advanced prostate cancer, in a subject in need thereof, include administering once-daily to the subject, at least 80 mg of N-(4-(1-(2,6-difluorobenzyl)-5-((dimethylamino)methyl)-3-(6-methoxy-3-pyridazinyl)-2,4-dioxo-1,2,3,4-tetrahydrothieno[2,3-d]pyrimidin-6-yl)phenyl)-N′-methoxyurea, or a corresponding amount of a pharmaceutically acceptable salt thereof. Another method includes: administering once-daily to the subject in need thereof, an oral load dose formulation having from 240 mg to 480 mg of N-(4-(1-(2,6-difluorobenzyl)-5-((dimethylamino)methyl)-3-(6-methoxy-3-pyridazinyl)-2,4-dioxo-1,2,3,4-tetrahydrothieno[2,3-d]pyrimidin-6-yl)phenyl)-N′-methoxyurea, or a corresponding amount of a pharmaceutically acceptable salt thereof, and thereafter administering once-daily to the subject, an oral maintenance dose formulation having 80 mg to 160 mg of N-(4-(1-(2,6-difluorobenzyl)-5-((dimethylamino)methyl)-3-(6-methoxy-3-pyridazinyl)-2,4-dioxo-1,2,3,4-tetrahydrothieno[2,3-d]pyrimidin-6-yl)phenyl)-N′-methoxyurea, or a corresponding amount of a pharmaceutically acceptable salt thereof.

The present disclosure relates generally to polymorphic forms of a KRAS inhibitor, and more specifically to polymorphic forms of a pyridopyrimidine derivative, and uses thereof.

Disclosed herein are novel methods for preparing 2-[(3R)-2-[4-amino-3-(2-fluoro-4-phenoxy-phenyl)pyrazolo[3,4-d]pyrimidin-1-yl]piperidine-1-carbonyl]-4-methyl-4[4-(oxetan-3-yl)piperazin-1-yl]-pent-2-enenitrile, including various solvate forms and intermediates thereof. Also disclosed herein are novel solvate forms and intermediates of 2-[(3R)-2-[4-amino-3-(2-fluoro-4-phenoxy-phenyl)pyrazolo[3,4-d]pyrimidin-1-yl]piperidine-1-carbonyl]-4-methyl-4[4-(oxetan-3-yl)piperazin-1-yl]-pent-2-enenitrile.

The invention provides a pyrimidino heterocyclic compound as well as a pharmaceutical composition and application thereof. The invention provides a pyrimidino heterocyclic compound as shown in a formula I, and a stereoisomer, a tautomer, an atropisomer or a pharmaceutically acceptable salt of the pyrimidino heterocyclic compound. The compound disclosed by the invention has good proliferation inhibition activity on NCI-H358 cells, AsPC-1 cells and Capan-1 cells containing KRAS mutation, and has relatively weak proliferation inhibition activity on PC-9 cells wild in KRAS. # imgabs0 #

The present invention provides a production method of a thienopyrimidine derivative or a salt thereof which has a gonadotropin releasing hormone (GnRH) antagonistic action with high quality in high yield. The present invention provides a method of producing a thienopyrimidine derivative, which comprises reacting 6-(4-aminophenyl)-1-(2,6-difluorobenzyl)-5-dimethylaminomethyl-3-(6-methoxypyridazin-3-yl)thieno[2,3-d]pyrimidine-2,4(1H,3H)-dione or salt thereof, 1,1′-carbonyldiimidazole or a salt thereof and methoxyamine or a salt thereof, and the like.

The present invention provides a production method of a thienopyrimidine derivative or a salt thereof which has a gonadotropin releasing hormone (GnRH) antagonistic action with high quality in high yield. The present invention provides a method of producing a thienopyrimidine derivative, which comprises reacting 6-(4-aminophenyl)-1-(2,6-difluorobenzyl)-5-dimethylaminomethyl-3-(6-methoxypyridazin-3-yl)thieno[2,3-d]pyrimidine-2,4(1H,3H)-dione or salt thereof, 1,1′-carbonyldiimidazole or a salt thereof and methoxyamine or a salt thereof, and the like.

The invention relates to a pyrimidine-containing polybasic ring derivative inhibitor as well as a preparation method and application thereof. In particular, the invention relates to a pyrimidine-containing multi-element fused ring compound or a stereoisomer thereof, a preparation method thereof, a pharmaceutical composition containing the compound, and an application of the compound or the stereoisomer thereof in preparation of drugs for treating cancers and other related diseases.

The invention belongs to the technical field of pesticides, and particularly relates to a mesoionic pyrimidinium compound, and an N-oxide or salt and application thereof. The compound is shown as a general formula I: # imgabs0 #, wherein X represents a cyano group, a cyano alkyl group, an aryl group or a heterocyclic group; q1 and Q2 independently represent O or S respectively; m1, M2, M3, M4 and M5 respectively and independently represent CR9 or N, and at least two of the M1, M2, M3, M4 and M5 are N; r1, R2, R3, R4, R5, R6, R7, R8 and R9 independently represent hydrogen, nitro, amino, cyano, halogen and the like respectively. The compound has excellent prevention and control effects on pests such as chilo suppressalis, spodoptera frugiperda, armyworm, prodenia litura, peanut aphid and rice planthopper, and is safe to bees.

The present disclosure relates generally to polymorphic forms of a KRAS inhibitor, and more specifically to polymorphic forms of a pyridopyrimidine derivative, and uses thereof.

Provided is a method for treating and / or preventing of cancer using Compound A or a pharmaceutically acceptable salt thereof.

The invention relates to a low-temperature curing polyimide precursor solution and a preparation method thereof. The method comprises the following steps: carrying out condensation polymerization reaction on a dianhydride monomer and a diamine monomer in a reaction solvent to obtain a polyamide acid solution; and adding an amino compound containing one or more special functional groups of pyridine, imidazole, quinoline, pyrimidine and azine into the polyamide acid solution, and fully stirring to enable amino in the compound to fully react with carboxyl in a polyamide acid molecular chain, thereby obtaining the polyimide precursor solution capable of being cured at low temperature. According to the preparation method, the curing temperature of polyimide can be greatly reduced, meanwhile, the mechanical property of the material can be improved, the thermal expansion coefficient can be reduced, and the preparation method can be used for preparing polyimide binders, photoresist, electronic packaging, resin, films, fibers and aerogel.

The present disclosure is directed to compounds of Formula (I):which modulate PD-1 / PD-L1 protein / protein interaction, compositions, and methods of treating various diseases, including infectious diseases and cancer.

The invention relates to a conjugated microporous polymer based on a dicarbazole structure and a preparation method and application thereof, the conjugated microporous polymer has a dicarbazole structure unit and a nitrogen-containing aromatic structure unit, the dicarbazole monomer structure is represented by the formula (I): # imgabs0 #, in the structure represented by the formula (I): R = H, R1 = C = H or R1 = H, R = C = H; the structure of the nitrogen-containing aromatic monomer is shown as a formula (II): # imgabs 1 #, wherein the aromatic structure in the structure shown as the formula (II) is any one of benzene, pyridine, pyrimidine, pyrazine and pyridazine. A plurality of conjugated microporous polymers with excellent photocatalytic performance are obtained by changing aromatic monomers with different nitrogen contents, and the conjugated microporous polymers can be applied to high-efficiency production of hydrogen peroxide under photocatalytic conditions.

The disclosure relates to a particulate composition comprising ensifentrine, wherein the particulate composition further comprises: from greater than 0.00 wt % to 0.60 wt % of 1,3-bis(2-(2-(mesitylimino)-9,10-dimethoxy-4-oxo-6,7-dihydro-2H-pyrimido[6,1-a]isoquinolin-3(4H)-yl)ethyl)urea (BMIQU) relative to the total weight of ensifentrine; and from 0.00 wt % to 0.50 wt % of a biuret impurity of formula (A) relative to the total weight of ensifentrine. Further disclosed herein are liquid pharmaceutical compositions comprising the particulate composition, and a process for producing the particulate composition are also described.

Provided herein is a process comprising heating a composition comprising (P)-compound A or a salt thereof and a solvent to a temperature of 250° C. to 350° C. to form racemized compound A. Also provided is a process for isolating (P)-compound A from a composition comprising (P)-compound A and a tartrate, as described herein. Further provided herein, is a process for isolating a free acid of a tartrate or a hydrate thereof from a composition comprising a tartrate, (P)-compound A, and an organic solvent.