938443-20-0

Basic information

• Product Name: 2,4,7-Trichloropyrido[2,3-d]pyrimidine
• Synonyms: 2,4,7-Trichloropyrido[2,3-d]pyrimidine;2,4,7-Trichloropyrido[2,3...;Pyrido[2,3-d]pyriMidine, 2,4,7-trichloro-
• CAS NO: 938443-20-0
• Molecular Formula: C₇H₂Cl₃N₃
• Molecular Weight: 234.473
• Mol File: 938443-20-0.mol

Chemical Properties

• Boiling Point: 316.4±42.0 °C(Predicted)
• Appearance: /
• Density: 1.686 g/cm³
• Refractive Index: 1.688
• Storage Temp.: under inert gas (nitrogen or Argon) at 2-8°C
• PKA: -2.53±0.30(Predicted)
• CAS DataBase Reference: 2,4,7-Trichloropyrido[2,3-d]pyrimidine(CAS DataBase Reference)
• NIST Chemistry Reference: 2,4,7-Trichloropyrido[2,3-d]pyrimidine(938443-20-0)
• EPA Substance Registry System: 2,4,7-Trichloropyrido[2,3-d]pyrimidine(938443-20-0)

Safety Data

• Hazard Codes: T
• Statements: 25-41
• Safety Statements: 26-39-45
• RIDADR: UN 2811 6.1 / PGIII
• WGK Germany: 3
• Hazardous Substances Data: 938443-20-0(Hazardous Substances Data)

Usage

Uses

Used in Pharmaceutical Industry:
2,4,7-Trichloropyrido[2,3-d]pyrimidine is used as a synthetic intermediate for the development of dual mTORC1/mTORC2 inhibitors. These inhibitors are designed to target the mechanistic target of rapamycin complex 1 and 2, which play a crucial role in regulating cell growth, proliferation, and survival. By inhibiting these complexes, the dual inhibitors can potentially suppress tumor growth and treat various types of cancer.
In the context of antitumor research, 2,4,7-Trichloropyrido[2,3-d]pyrimidine has been instrumental in the discovery of compounds such as AZD8055 and AZD2014. These compounds have demonstrated promising antitumor activity in preclinical studies, making them potential candidates for further development as therapeutic agents in cancer treatment.

InChI:InChI=1/C7H2Cl3N3/c8-4-2-1-3-5(9)12-7(10)13-6(3)11-4/h1-2H

Upstream product

• 38496-18-3 2,6-dichloropyridine-3-carboxylic acid 
• 64321-24-0 2-amino-6-chloro-pyridine-3-carboxamide 
• 58584-92-2 2-amino-6-chloronicotinic acid 
• 258282-54-1 C₇H₅N₃O₃ 
• 938443-19-7 7-chloropyrido[2,3-d]pyrimidine-2,4(1H,3H)-dione 

Downstream Products

• 938440-64-3 KU-63794 
• 1009302-61-7 C₂₄H₂₉N₅O₄ 
• 1009302-80-0 C₂₅H₃₂N₆O₃ 
• 1009302-46-8 C₂₄H₃₁N₅O₄ 
• 1009302-47-9 C₂₃H₂₄N₆O₃ 
• 1009298-09-2 AZD₈₀₅₅ 
• 938443-23-3 7-chloro-2-((2S,6R)-2,6-dimethyl-morpholin-4-yl)-4-morpholin-4-yl-pyrido[2,3-d]pyrimidine 
• 938443-29-9 7-(3-chloromethyl-4-methoxy-phenyl)-2-((2S,6R)-2,6-dimethyl-morpholin-4-yl)-4-morpholin-4-yl-pyrido[2,3-d]pyrimidine 
• 1424432-35-8 C₂₆H₃₄N₆O₃ 
• 1424432-36-9 C₂₅H₃₂N₆O₂ 
• 1424432-37-0 C₂₆H₃₄N₆O₂ 
• 1009303-44-9 (3S)-4-[7-chloro-2-[(3S)-3-methylmorpholin-4-yl]pyrido[2,3-d] pyrimidin-4-yl] 3-methyl-morpholine 
• 1424432-38-1 C₂₅H₃₁N₅O₃S 

Relevant articles and documents

HETEROCYCLIC COMPOUNDS AS MTOR INHIBITORS

The present disclosure describes novel heterocyclic mTOR inhibitors and methods for preparing them. The pharmaceutical compositions comprising such mTOR inhibitors and methods of using them for treating cancer, infectious diseases, and other mTOR associated disorders are also described.

Pyridopyrimidine KRAS G12C mutant protein inhibitor

The invention belongs to the technical field of medicines, and particularly relates to a pyridopyrimidine KRAS G12C mutant protein inhibitor shown in a general formula (I), pharmaceutically acceptable salts, stereoisomers and deuterated substances thereof. The invention also relates to a preparation method of the compounds, and a preparation method of the pharmaceutically acceptable salts, pharmaceutical preparations and pharmaceutical compositions containing the compounds. The invention also relates to the application of the compounds, pharmaceutically acceptable salts containing the compounds, pharmaceutical preparations and pharmaceutical compositions of the compounds in treatment of cancer proliferative diseases caused by KRAS G12C mutant protein.

PYRIDOPYRIMIDINE COMPOUNDS ACTING AS MTORC 1/2 DOUBLE-KINASE INHIBITORS

Disclosed are a series of pyridopyrimidine compounds and a use of same in the preparation of drugs associated with mTORC 1/2 dual complex inhibitors, and specifically disclosed is a use of the compounds as shown in formula (IV), tautomers thereof or pharmaceutically acceptable salts thereof in the preparation of drugs associated with mTORC 1/2 dual complex inhibitors.

Pyridine and miazines mTOR inhibitors

The invention belongs to the technical field of medicines, and particularly relates to a pyridopyrimidine mammalian target of rapamycin (mTOR) inhibitor which is shown as a general formula (I), pharmaceutically acceptable salts and stereoisomers thereof, and deuterated pyridopyrimidine mammalian mTOR inhibitors, wherein Z, Z, Z, R, R, R, X and W are defined in the specifications. The invention also relates to preparation methods for the compounds, medicinal inhibitors and medicinal compositions which contain the compounds, and the application of the compounds to preparation of medicines for treating and/or preventing post-transplant lymphoproliferative diseases which have response to inhibition of mTOR activity.

Discovery of 1-methyl-1 H-imidazole derivatives as potent Jak2 inhibitors

Structure based design, synthesis, and biological evaluation of a novel series of 1-methyl-1H-imidazole, as potent Jak2 inhibitors to modulate the Jak/STAT pathway, are described. Using the C-ring fragment from our first clinical candidate AZD1480 (24), optimization of the series led to the discovery of compound 19a, a potent, orally bioavailable Jak2 inhibitor. Compound 19a displayed a high level of cellular activity in hematopoietic cell lines harboring the V617F mutation and in murine BaF3 TEL-Jak2 cells. Compound 19a demonstrated significant tumor growth inhibition in a UKE-1 xenograft model within a well-tolerated dose range.

Optimization of potent and selective dual mTORC1 and mTORC2 inhibitors: The discovery of AZD8055 and AZD2014

The optimization of a potent and highly selective series of dual mTORC1 and mTORC2 inhibitors is described. An initial focus on improving cellular potency whilst maintaining or improving other key parameters, such as aqueous solubility and margins over hERG IC50, led to the discovery of the clinical candidate AZD8055 (14). Further optimization, particularly aimed at reducing the rate of metabolism in human hepatocyte incubations, resulted in the discovery of the clinical candidate AZD2014 (21).

HETEROCYCLIC JAK KINASE INHIBITORS

The present invention relates to compounds of Formula (I) and to their salts, pharmaceutical compositions, methods of use, and methods for their preparation. These compounds provide a treatment for myeloproliferative disorders and cancer

The discovery and optimisation of pyrido[2,3-d]pyrimidine-2,4-diamines as potent and selective inhibitors of mTOR kinase

We describe a novel series of potent inhibitors of the kinase activity of mTOR. The compounds display good selectivity relative to other PI3K-related kinase family members and, in cellular assays, inhibit both mTORC1 and mTORC2 complexes and exhibit good antiproliferative activity.

COMBINATION 059

This invention relates to a combination product, as defined herein, comprising a MEK inhibitor and a mTOR-selective inhibitor, and to methods for the production of an anti-cancer effect in a patient, which is accordingly useful in the treatment of cancer in a patient. More specifically the present invention relates to; a combination product, as defined herein, comprising a MEK inhibitor and a mTOR-selective inhibitor; a combination product, as defined herein, comprising a kit of parts comprising a MEK inhibitor and a mTOR-selective inhibitor; use of the combination product, as defined herein, in the treatment of cancer; a method of treating cancer comprising administering the combination product, as defined herein, to a patient. The combination product, as defined herein, and methods of the invention are also useful in the treatment of other diseases associated with the activity of MEK, and/or mTOR.

2-METHYLMORPHOLINE PYRIDO-, PYRAZO- AND PYRIMIDO-PYRIMIDINE DERIVATIVES AS MTOR INHIBITORS

There is provided a compound of Formula (I), or a pharmaceutically acceptable salt thereof. There are also provided processes for the manufacture of a compound of Formula (1), and the use of a compound of Formula (1) as a medicament and in the treatment of cancer