1233145-65-7

Upstream product

• 321-23-3 4-bromo-2-fluoronitrobenzene 
• 103966-66-1 4-bromo-2-methoxy-1-nitro-benzene 
• 375853-82-0 tert-Butyl 4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-3,6-dihydro-1(2H)-pyridinecarboxylate 
• 6627-53-8 1-chloro-3-methoxy-4-nitrobenzene 

Downstream Products

• 1246533-06-1 tert-butyl 4-(4-amino-3-methoxy-phenyl)-3,6-dihydro-2H-pyridine-1-carboxylate 
• 1089280-53-4 tert-butyl 4-(4-amino-3-methoxyphenyl)piperidine-1-carboxylate 
• 1314996-83-2 7-Amino-2-[4-(1-cyclopropylpiperid-4-yl)-2-methoxyphenylamino]-8-ethyl-5-oxo-5,8-dihydropyrido[2,3-d]pyrimidine-6-carboxamide 
• 1314997-78-8 tert-Butyl 4-[4-(7-amino-6-carbamoyl-8-ethyl-5-oxo-5,8-dihydropyrido[2,3-d]pyrimidin-2-ylamino)-3-methoxyphenyl]piperidine-1-carboxylate 
• 1233182-00-7 4-(3-Methoxy-4-nitrophenyl)-1,2,3,6-tetrahydropyridine hydrochloride 
• 1315513-42-8 tert-Butyl 4-[4-(7-amino-6-carbamoyl-8-(2-hydroxy-2-methylpropyl)-5-oxo-5,8-dihydropyrido[2,3-d]pyrimidin-2-ylamino)-3-methoxyphenyl]piperidine-1-carboxylate 
• 1315513-49-5 tert-Butyl 4-[4-(7-amino-6-carbamoyl-5-oxo-8-phenyl-5,8-dihydropyrido[2,3-d]pyrimidin-2-ylamino)-3-methoxyphenyl]piperidine-1-carboxylate 
• 1315513-76-8 7-Amino-2-[4-(1-cyclopropylpiperid-4-yl)-2-methoxyphenylamino]-8-(2-hydroxy-2-methylpropyl)-5-oxo-5,8-dihydropyrido[2,3-d]pyrimidine-6-carboxamide 
• 1315513-52-0 7-amino-2-{4-[1-(2-chloroethyl)piperid-4-yl]-2-methoxyphenylamino}-8-(2-hydroxy-2-methylpropyl)-5-oxo-5,8-dihydropyrido[2,3-d]pyrimidine-6-carboxamide 
• 1315513-77-9 7-amino-8-(2-hydroxy-2-methylpropyl)-2-{2-methoxy-4-[1-(2-methoxyethyl)piperid-4-yl]phenylamino}-5-oxo-5,8-dihydropyrido[2,3-d]pyrimidine-6-carboxamide 
• 1315304-56-3 C₂₂H₂₇N₇O₃ 
• 1315514-19-2 7-amino-8-(2-hydroxy-2-methylpropyl)-2-[4-(1-ethylpiperid-4-yl)-2-methoxyphenylamino]-5-oxo-5,8-dihydropyrido[2,3-d]pyrimidine-6-carboxamide 
• 1233146-37-6 C₁₅H₂₃N₃O₂ 
• 1353898-52-8 C₁₅H₁₉N₃O₄ 

Relevant academic research and scientific papers

PYRIMIDINE DERIVATIVE AND USE THEREOF

The present invention provides a pyrimidine derivative and a use thereof. The pyrimidine derivative is the compound shown in formula I or a pharmaceutically acceptable salt, hydrate, solvate, metabolite or prodrug thereof, wherein, R1, R2, R3, R4 and R5 are, for example, as defined in the specification. The compound can act as an ALK inhibitor, and is for preparing an anti-tumor medicament for suppressing an anaplastic lymphoma kinase.

HETEROCYCLIC COMPOUND

The present invention provides a compound having a CaMKII inhibitory action, which is expected to be useful as an agent for the prophylaxis or treatment of cardiac diseases (particularly catecholaminergic polymorphic ventricular tachycardia, postoperative atrial fibrillation, heart failure, fatal arrhythmia) and the like. The present invention relates to a compound represented by the formula (I): wherein each symbol is as defined in the specification, or a salt thereof.

CONDENSED-RING PYRIMIDYLAMINO DERIVATIVE, PREPARATION METHOD THEREFOR, AND INTERMEDIATE, PHARMACEUTICAL COMPOSITION AND APPLICATIONS THEREOF

Disclosed are a condensed-ring pyrimidylamino derivative, a preparation method therefor, and an intermediate, a pharmaceutical composition and applications thereof. The method for preparing the condensed-ring pyrimidylamino derivative comprises: in a solvent, in the presence of a palladium-containing catalyst, allowing a compound represented by formula I-a and a compound represented by formula I-b' to have a coupling reaction, and then preparing a compound represented by formula I by means of a deprotection reaction. Also disclosed applications of the condensed-ring pyrimidylamino derivative in the preparation of drugs for preventing, relieving and/or treating tumors or diseases caused by an anaplastic lymphoma kinase. The condensed-ring pyrimidylamino derivative of the present invention has an obvious restraint effect on the anaplastic lymphoma kinase.

Tyrosine Kinase Inhibitor And Uses Thereof

Disclosed is a compound of Formula (I) or a pharmaceutically acceptable salt, ester, or solvate thereof, or their stereoisomers, which can be used as tyrosine kinase inhibitor. Also disclosed is a method for preparing the compound, a pharmaceutical composition and a kit comprising the compound, and uses of the compound. The compound can be used as tyrosine kinase inhibitor, or can be used to reduce or inhibit activity of EGFR or mutant thereof, such as EGFR mutant comprising T790M mutation, in a cell, or to treat and/or prevent a disease associated with overactivity of EGFR, such as cancer.

Heterocyclic derivate tyrosine kinase inhibitor

The invention belongs to the technical field of medicine and particularly relates to a heterocyclic derivate tyrosine kinase inhibitor shown in the formula (I), a pharmaceutically acceptable salt and ester thereof and stereoisomers thereof, wherein Y, W, Q m, L, R1, R2, R3, R4, R5, R6, R7, R7', R8 and R8' are defined in the specification. The invention further relates to a preparation method of the compounds and a pharmaceutical preparation and pharmaceutical compositions containing the compounds, and application of the compounds as the tyrosine kinase inhibitor for preparing medicine for preventing and/or treating cancer diseases caused by EGFR mutation and drug resistance diseases caused by EGFR T790M mutation.

PYRROLOTRIAZINES AS ALK INHIBITORS

This application provides compounds of the general formula (I) and/or a salt thereof, where X, R1 and R2 are as defined herein. Compositions and therapeutic uses are also described.

5 OXO-5,8-DIHYDROPYRIDO[2,3-d]PYRIMIDINE DERIVATIVES AS CAMKII KINASE INHIBITORS FOR TREATING CARDIOVASCULAR DISEASES

The present invention relates to 5-oxo-5,8-dihydropyrido[2,3-d]pyrimidine derivatives, to their preparation and to their therapeutic use.

Strategies to mitigate the bioactivation of 2-anilino-7-aryl-pyrrolo[2,1-f ][1,2,4]triazines: Identification of orally bioavailable, efficacious ALK inhibitors

Chemical strategies to mitigate cytochrome P450-mediated bioactivation of novel 2,7-disubstituted pyrrolo[2,1-f][1,2,4]triazine ALK inhibitors are described along with synthesis and biological activity. Piperidine-derived analogues showing minimal microsomal reactive metabolite formation were discovered. Potent, selective, and metabolically stable ALK inhibitors from this class were identified, and an orally bioavailable compound (32) with antitumor efficacy in ALK-driven xenografts in mouse models was extensively characterized.

PYRIMIDINE INHIBITORS OF KINASE ACTIVITY

The present invention relates to compounds of formula (I) or pharmaceutical acceptable salts or solvates thereof, wherein G1, R2, R3, R4, R5, n, p, q, Ar1, and Ar2 are defined in the description. The present invention relates also to methods of making said compounds, and compositions comprising said compounds which are useful for inhibiting kinases such as IGF-IR.

COMPOUNDS AND THERAPEUTIC USES THEREOF

The invention relates to compounds, pharmaceutical compositions, and uses thereof, including therapeutic uses thereof, such as methods useful for treating cancer.