2158302-00-0

Usage

Chemical structure

A complex chemical compound with a piperazine ring and two carboxylate groups.

Building block

Often used in medicinal chemistry as a building block for the synthesis of pharmaceuticals and potential drug candidates.

Presence of benzyl and tert-butyl groups

These groups can affect the compound's pharmacokinetic properties, such as solubility and bioavailability.

Cyanomethyl group

This group may lend the compound reactive and pharmacological qualities.

Importance

An important intermediate in the development of new therapeutic agents.

Applications

Potential applications in drug discovery and medicinal research.

Upstream product

• 301673-16-5 tert-butyl 3-(hydroxymethyl)piperazine-1-carboxylate 
• 317365-33-6 1-(benzyloxycarbonyl)-2-hydroxymethyl-4-(tert-butyloxycarbonyl)-piperazine 
• 773837-37-9 sodium cyanide 
• 501-53-1 benzyl chloroformate 
• 529516-61-8 O₁-benzyl O₄-tert-butyl (2S)-2-(hydroxymethyl)piperazine-1,4-dicarboxylate 
• 1589082-06-3 (S)-3-cyanomethylpiperazine-1-carboxylic acid tert-butyl ester 
• 7677-24-9 trimethylsilyl cyanide 
• 1217813-68-7 O¹-benzyl O⁴-(tert-butyl) (R)-2-(hydroxymethyl)piperazine-1,4-dicarboxylate 
• 278788-66-2 (R)-tert-butyl 3-(hydroxymethyl)piperazine-1-carboxylate 

Downstream Products

• 2502156-03-6 (2S,4R)-1-((S)-2-(3-(3-((S)-2-(((7-(8-chloronaphthalen-1-yl)-4-((S)-3-(cyanomethyl)-4-(2-fluoroacryloyl)piperazin-1-yl)-5,6,7,8-tetrahydropyrido[3,4-d]pyrimidin-2-yl)oxy)methyl)pyrrolidin-1-yl)propoxy)propanamido)-3,3-dimethylbutanoyl)-4-hydroxy-N-(4-(4-methylthiazol-5-yl)benzyl)pyrrolidine-2-carboxamide 
• 2502156-03-6 (2S,4S)-1-((S)-2-(3-(3-((S)-2-(((7-(8-chloronaphthalen-1-yl)-4-((S)-3-(cyanomethyl)-4-(2-fluoroacryloyl)piperazin-1-yl)-5,6,7,8-tetrahydropyrido[3,4-d]pyrimidin-2-yl)oxy)methyl)pyrrolidin-1-yl)propoxy)propanamido)-3,3-dimethylbutanoyl)-4-hydroxy-N-(4-(4-methylthiazol-5-yl)benzyl)pyrrolidine-2-carboxamide 
• 2306248-13-3 tert-butyl (R)-3-(cyanomethyl)piperazine-1-carboxylate 
• 1589082-06-3 (S)-3-cyanomethylpiperazine-1-carboxylic acid tert-butyl ester 

Relevant academic research and scientific papers

TRICYCLIC PYRIDONES AND PYRIMIDONES

A compound of Formula (I) is provided: (I) where the variables are defined herein.

Heterocyclic compound, pharmaceutical composition and application

The invention discloses a heterocyclic compound which is a heterocyclic compound shown as a formula I, a pharmaceutically acceptable salt, a stereoisomer, a tautomer, a hydrate, a solvate, a metabolite or a prodrug thereof. The heterocyclic compound can be used for preparing medicines for treating and/or preventing cancers related to KRAS G12C mutation. The invention also discloses a pharmaceutical composition containing the heterocyclic compound, and application of the compound shown in the formula I, or pharmaceutically acceptable salt, stereoisomer, tautomer, hydrate, solvate, metabolite, prodrug or pharmaceutical composition thereof in preparation of drugs.

COMPOUNDS AND METHODS FOR TARGETED DEGRADATION OF KRAS

Bifunctional compounds, which find utility as modulators of Kirsten ras sarcoma protein (KRas or KRAS), are described herein. In particular, the hetero-bifunctional compounds of the present disclosure contain on one end a moiety that binds to the Von Hippel-Lindau E3 ubiquitin ligase and on the other end a moiety which binds KRas, such that the target protein is placed in proximity to the ubiquitin ligase to effect degradation (and inhibition) of target protein. The heterobifunctional compounds of the present disclosure exhibit a broad range of pharmacological activities associated with degradation/inhibition of target protein. Diseases or disorders that result from aberrant regulation of the target protein are treated or prevented with compounds and compositions of the present disclosure.

Tetrahydropyrido [3, 4-d] pyrimidine derivative and medical application thereof

The invention relates to a compound as shown in a general formula (I) or a stereoisomer, a deuterated compound, a solvate, a prodrug, a metabolite, a pharmaceutically acceptable salt or eutectic crystal thereof, an intermediate and a preparation method thereof, and application of the compound in preparation of drugs for treating diseases related to KRas-G12C activity or expression quantity.

Compound for inhibiting KRASG12C mutant protein, preparation method and application thereof

The present invention discloses a compound represented by the following formula (I), and an isomer or a pharmaceutically acceptable salt thereof. The compound can be used for inhibiting KRASG12C mutant protein and treating related cancers.

RAS INHIBITORS AND METHODS OF USING THE SAME

Provided herein are compounds identified as inhibitors of KRAS protein activity that can be used to treat various diseases and disorders, such as cancer.

KRAS G12C INHIBITORS

The present invention relates to compounds that, inhibit KRas G12C, In particular, the present invention relates to compounds that irreversibly inhibit the activity of KRas G12C, pharmaceutical compositions comprising the compounds and methods of use therefor.

KRAS G12C INHIBITORS

The present invention relates to compounds that inhibit KRas G12C. In particular, the present invention relates to compounds that irreversibly inhibit the activity of KRas G12C, pharmaceutical compositions comprising the compounds and methods of use therefor.

KRAS G12C INHIBITORS

The present invention relates to compounds that inhibit KRas G12C. In particular, the present invention relates to compounds that irreversibly inhibit the activity of KRas G12C, pharmaceutical compositions comprising the compounds and methods of use therefor.

MODULATORS OF PROTEOLYSIS AND ASSOCIATED METHODS OF USE

The present disclosure relates to bifunctional compounds, which find utility as modulators of Kirsten rat sarcoma protein (target protein). In particular, the present disclosure is directed to bifunctional compounds, which contain on one end a Von Hippel-Lindau, cereblon, Inhibitors of Apotosis Proteins or mouse double-minute homolog 2 ligand which binds to the respective E3 ubiquitin ligase and on the other end a moiety which binds the target protein, such that the target protein is placed in proximity to the ubiquitin ligase to effect degradation (and inhibition) of target protein. The present disclosure exhibits a broad range of pharmacological activities associated with degradation/inhibition of target protein. Diseases or disorders that result from aggregation, accumulation, and/or overactivation of the target protein are treated or prevented with compounds and compositions of the present disclosure.