1235865-75-4

Usage

Uses

Used in Oncology:
ABT199 INT 2 is used as an intermediate for ABT 199, a potent and selective BCL-2 inhibitor, for its potent antitumor activity while sparing platelets. This makes it a valuable compound in the development of treatments for various types of cancer.
Used in Chronic Lymphocytic Leukemia Treatment:
ABT199 INT 2 is used as an intermediate for ABT 199, which is employed as a treatment for chronic lymphocytic leukemia cells. Its selective BCL-2 inhibition helps in targeting and eliminating cancer cells while minimizing harm to healthy cells.
Used in Estrogen Receptor-Positive Breast Cancer Treatment:
ABT199 INT 2 is used as an intermediate for ABT 199, which is utilized in the treatment of estrogen receptor-positive breast cancer. Its potent antitumor activity and platelet-sparing properties make it a promising option for patients with this type of cancer.

Upstream product

• 106614-28-2 methyl 2,4-difluorobenzoate 
• 685514-01-6 1-[tris(propan-2-yl)silyl]-1H-pyrrolo[2,3-b]pyridin-5-ol 
• 858116-66-2 5-bromo-1-(triisopropylsilyl)-1H-pyrrolo[2,3-b]pyridine 
• 1583-58-0 2,4-difluoro-benzoic acid 
• 67-56-1 methanol 
• 98549-88-3 5-hydroxypyrrolo[2,3-b]pyridine 

Downstream Products

• 1235865-77-6 [2-((1H-pyrrolo [2,3-b]pyridin-5-yl)oxy)-4-(4-((4’-chloro-5,5-dimethyl-3,4,5,6-tetrahydro-[1,1’-biphenyl]-2-yl)methyl)piperazin-1-yl)benzoic acid] 
• 1257044-40-8 2-((1H-pyrrolo[2,3-b]pyridin-5-yl)oxy)-4-(4-((4'-chloro-5,5-dimethyl-3,4,5,6-tetrahydro-[1,1-biphenyl]-2-yl)methyl)piperazin-1-yl)-N-((3-nitro-4-(((tetrahydro-2H-pyran-4-yl)methyl)amino)phenyl)sulfonyl)benzamide 
• 1235865-76-5 2-((1H-pyrrolo[2,3-b]pyridin-5-yl)oxy)-4-(4-((4’-chloro-5,5-dimethyl-3,4,5,6-tetrahydro-[1,1’-biphenyl]-2-yl)methyl)piperazin-1-yl)benzoic acid methyl ester 

Relevant academic research and scientific papers

Heterocyclic compounds as BCL-2 inhibitor

The present invention relates to a compound, a pharmaceutical composition containing the same, preparation method of the compound and thepharmaceutical composition, and uses ofthe compound and the pharmaceutical compositionas B-cell lymphoma-2 (BCL-2) inhibitors, wherein the compound is a compound shown as a formula I, or an isomer, a prodrug, a solvate, a stable isotope derivative or a pharmaceutically acceptable salt thereof. The invention also relates to the uses of the compound or the composition containing the same in treatment or prophylaxis of BCL2-mediated related diseases such as tumours.

Bcl-2 INHIBITORS

Disclosed herein is a compound of Formula (I) for inhibiting Bcl-2 and treating disease associated with undesirable bcl-2 activity (Bcl-2 related diseases), a method of using the compounds disclosed herein for treating dysregulated apoptotic diseases including cancers and treating autoimmune disease, and a pharmaceutical composition comprising the same.

Solid dispersions containing an apoptosis-inducing agent

A pro-apoptotic solid dispersion comprises, in essentially non-crystalline form, a Bcl-2 family protein inhibitory compound of Formula I as defined herein, dispersed in a solid matrix that comprises (a) a pharmaceutically acceptable water-soluble polymeric carrier and (b) a pharmaceutically acceptable surfactant. A process for preparing such a solid dispersion comprises dissolving the compound, the polymeric carrier and the surfactant in a suitable solvent, and removing the solvent to provide a solid matrix comprising the polymeric carrier and the surfactant and having the compound dispersed in essentially non-crystalline form therein. The solid dispersion is suitable for oral administration to a subject in need thereof for treatment of a disease characterized by overexpression of one or more anti-apoptotic Bcl-2 family proteins, for example cancer.

Preparation method of Venetoclax intermediate and product

The invention discloses a preparation method of a Venetoclax intermediate. 5-bromine-7-azaindole (II) is used as a raw material; an upper protecting group generates 5-bromine-1-(Triisopropyl silicyl)-1H-pyrrolo[2,3-b]pyridine (III); a compound (III) and T

PROCESS FOR THE PREPARATION OF VENETOCLAX

The present disclosure provides novel synthetic process for the preparation of venetoclax. The disclosed processes involve the use of novel intermediates. Processes for the preparation of these intermediates are also disclosed as well as methods for the preparation of particularly useful salts thereof.

N-benzenesulfonyl benzamide compound for inhibiting Bcl-2 proteins as well as composition and application thereof

The invention relates to a compound capable of inhibiting the activity of Bcl-2 anti-apoptosis protein as well as a preparation and application thereof, in particular to an N-benzenesulfonyl benzamidecompound for inhibiting Bcl-2 proteins as shown in formula (I), or a medicine composition of a crystal form, a precursor, a pharmaceutically-acceptable salt, a three-dimensional isomer, a solvent composition or a hydrate of the N-benzenesulfonyl benzamide compound. The compound and the composition containing the compound have excellent rejection capability for Bcl-2 proteins, have better pharmacokinetics parameter characteristics, can increase the medicine concentration of the compound in animal bodies, and can improve the drug curative effect and safety. (The formula (I) is shown in the description).

A ABT - 199 intermediate preparation method (by machine translation)

The invention discloses a ABT - 199 intermediate preparation method, the intermediate structure correspond to the formula I: The method comprises the compound of formula II 5 - bromo - 7 - azaindole as raw materials, through the protection, copper catalytic hydroxylation reaction, substituted, to protect 4 step reaction, the final formula I of ABT - 199 intermediate. The method of the invention cheap raw material, mild reaction conditions, the problem of non-selective, high yield, is more suitable for industrial production. (by machine translation)

Compound, preparation method and applications thereof

The invention relates to a new diaryl ether alkynyl compound I and a synthesis method thereof, provide a synthesis method for obtaining a compound II from the compound I through a cyclization reaction, and relates to the field of pharmaceutical intermediate synthesis. According to the present invention, the synthesis of an anticancer drug key intermediate is completed through the designed completely-new synthesis path; and the synthesis method comprises the coupling reaction between the aryl group and the terminal alkyne and the cyclization reaction of the five-membered nitrogen-containing heterocyclic ring, and has characteristics of easily available raw materials, mild reaction conditions, and simple operation.

Synthesis method for BCL-2 inhibitor Venetoclax

The invention discloses a new synthesis method for a BCL-2 inhibitor Venetoclax. The synthesis method includes the steps that 2,4-difluoro methyl benzoate serves as a raw material, the 2,4-difluoro methyl benzoate and 5-hydroxy-7-azaindole are subjected to a condensation reaction, Ven-16 is obtained, and 4-substituted isomer and other impurities are removed through recrystallization; the product and N-Boc-piperazine are reacted and hydrolyzed, and Ven-18 is obtained; Ven-18 and Ven-21 are condensed, Boc of trifluoroacetic acid is removed, and Ven-20 is obtained; the product and Ven-7 are reacted, reaction intermediates in all the steps have the good crystal forms, purification can be carried out through crystal to achieve the center control requirements of the technology, and a final product Venetoclax can also be subjected to recrystallization to obtain the product Venetoclax, wherein the HPLC purity of the Venetoclax is larger than 99.5%, and the individual impurity of the Venetoclax is smaller than 0.1%; the Venetoclax has the industrialized application value.

Sulfonamide derivative and application thereof in pharmacy

The invention relates to a sulfonamide derivative and a pharmaceutical composition containing the same, and an application of the sulfonamide derivative and the pharmaceutical composition of the sulfonamide derivative in drug preparation, specifically the application in drug preparation of a BCL-2 family protein antagonist and the application in treatment of cancers.