1374639-75-4

Usage

Uses

Used in Pharmaceutical Industry:
LEE011 (succinate) is used as an anti-cancer agent for its ability to inhibit the CDK4/6 proteins, which are commonly overactive in cancer cells. This inhibition can help control the unregulated cell division and growth associated with cancer.
Used in Combination Therapy for Melanoma and Breast Cancer:
In combination with LGX818 (a V600E BRAF specific inhibitor) or BYL719 (a PIK3CA specific inhibitor), LEE011 (succinate) is used to enhance anti-tumor activity in melanoma and breast cancer tumor models. The synergistic effect of these drugs can lead to more robust anti-cancer responses and potentially improve patient outcomes.

Upstream product

• 110-15-6 succinic acid 
• 1211441-98-3 (7-cyclopentyl-Ν,Ν-dimethyl-2-[(5-piperazin-1-ylpyridin-2-yl)amino]pyrrolo [2,3-d]pyrimidine-6-carboxamide) 
• 571188-59-5 tert-butyl 4-(6-aminopyridin-3-yl)piperazine-1-carboxylate 
• 1211443-61-6 2-chloro-7-cyclopentyl-7H-pyrrolo[2,3-d]pyrimidine-6-carboxylic acid dimethylamide 
• 1374639-77-6 (2-chloro-7-cyclopentyl-7H-pyrrolo[2,3-d]pyrimidin-6-yl)methanol 
• 1374639-76-5 3-(2-chloro-4-(cyclopentylamino)pyrimidin-5-yl)prop-2-yn-1-ol 
• 733039-20-8 5-bromo-2-chloro-N-cyclopentylaminopyrimidine-4-amine 
• 571189-16-7 4-(6-nitropyridin-3-yl)-piperazine-1-carboxylic acid tert-butyl ester 
• 1003-03-8 Cyclopentamine 
• 52092-47-4 5-chloro-2-nitropyridine 
• 775288-71-6 1-(6-nitropyridin-3-yl)piperazine 
• 1195-08-0 2,4-dioxo-1,2,3,4-tetrahydropyrimidine-5-carbaldehyde 
• 1211443-58-1 2-chloro-7-cyclopentyl-7H-pyrrolo[2,3-d]pyrimidine-6-carboxylic acid 
• 1374639-78-7 N,N‐dimethyl‐7‐cyclopentyl‐2‐{[5‐(4-tert-butoxycarbonylpiperazin‐1‐yl)pyridin‐2‐yl]amino}‐7H‐pyrrolo[2,3‐d]pyrimidine‐6‐carboxamide 

Relevant academic research and scientific papers

RIBOCICLIB INTERMEDIATE AND PROCESS FOR PREPARATION THEREOF

The present invention relates to the process for the preparation of ribociclib succinate by making use of novel intermediates. The invention also relates to the process for the preparation of novel intermediates.

POLYMORPHS OF 7-CYCLOPENTYL-N,N-DIMETHYL-2-{[5-(PIPERAZIN-1-YL) PYRIDIN-2-YL]-AMINO}-7H-PYRROLO[2,3-D]PYRIMIDINE-6-CARBOXAMIDE AND ITS PHARMACEUTICALLY ACCEPTABLE SALTS AND PROCESS FOR THE PREPARATION THEREOF

The present invention relates to novel crystalline forms of butanedioic acid 7-cyclopentyl-N,N-dimethyl-2-{[5-(piperazin-1-yl) pyridin-2-yl]amino}-7H-pyrrolo[2,3-d] pyrimidine-6-carboxamide of formula-1a and process for preparation thereof. The present invention also relates to a process for the preparation of 7-cyclopentyl-N,N-dimethyl-2-{[5-(piperazin-1-yl)pyridin-2-yl]amino}-7H-pyrrolo[2,3-d] pyrimidine-6-carboxamide. Further, the present application also relates to acid addition salts of 7-cyclopentyl-N,N-dimethyl-2-{[5-(piperazin-1-yl)pyridin-2-yl]amino}-7H-pyrrolo[2,3-d] pyrimidine-6-carboxamide and process for the preparation thereof.

PREPARATION METHOD OF RIBOCICLIB AND ITS SALT AND CRYSTALLINE FORM THEREOF

The present invention provides a preparation method of ribociclib and its salt and a novel crystalline form of ribociclib succinate. The conditions of the preparation method of the present invention are easier than the conventional process, and the yield is higher as well. The purity of ribociclib in crude product stage meets the requirement for quality of active pharmaceutical ingredient (API), so that no further purification is required. The crystalline form of ribociclib succinate in the present invention has outstanding storage stability.

Polymorphic substances of ribosinil monosuccinate and preparation method and use thereof

The invention relates to novel crystal forms of a compound mono-succinate represented by a formula I and a preparation method of the novel crystal. Specifically, the invention provides a plurality ofnew crystal forms of the compound mono-succinate represented by the formula I and a preparation method thereof, and the new crystal forms have the properties of excellent solubility, lower hygroscopicity, better stability and the like.

Crystal form of and preparation method and application thereof (by machine translation)

The invention relates to a crystal form of, a preparation method and an application thereof. , The invention provides a plurality of novel crystal forms and a preparation method thereof, and the novel crystal forms disclosed by the invention have excellent solubility and the like. (by machine translation)

NOVEL POLYMORPHS OF RIBOCICLIB SUCCINATE

The present invention relates to novel crystalline forms of Ribociclib Succinate and its preparation process.

AN IMPROVED PROCESS FOR THE PREPARATION OF RIBOCICLIB AND ITS SALTS

The invention relates to a process for the preparation of ribociclib of formula V or its salts. The invention provides novel crystalline forms of ribociclib succinate and ribociclib trifluoroacetate. The present invention also relates to pharmaceutical compositions comprising a crystalline form of ribociclib succinate and at least a pharmaceutically acceptable carrier. It further relates to the use of such compositions in the treatment of cancer.

AN IMPROVED PROCESS FOR THE PREPARATION OF RIBOCICLIB SUCCINATE AND ITS NOVEL CRYSTALLINE FORMS THEREOF

The present invention relates to an improved process for the preparation of 7-cyclopentyl-N,N-dimethyl-2-{[5-(piperazin-1-yl)pyridin-2-yl]amino}-7H-pyrrolo[2,3-d]pyrimidine-6-carboxamide succinate (1/1) compound of formula-1a and its novel crystalline for

Preparation method of ribociclib and product and use thereof

A preparation method of ribociclib comprises the following steps: 1) utilizing 4-(6-aminopyridine-3-yl)piperazine-1-carboxylic acid tert-butyl ester and 2-chloro-4-cyclopentyl-N,N-dimethyl-7H-pyrrole[2,3-d]pyrimidine-6-formamide as raw materials and conducting reaction in a protective atmosphere with palladium acetate/ BINAP as a catalyst, cesium carbonate as an acid absorber and 4-methyl-2-pentanone as a solvent to obtain 4-(6-(7-cyclopentyl-6-(dimethylaminoformyl)-7H-pyrrolo[2,3-d]pyrimidine-2-yl)aminopyridine-3-yl)piperazine-1-carboxylic acid tert-butyl ester); 2) dissolving the4-(6-(7-cyclopentyl-6-(dimethylaminoformyl)-7H-pyrrolo[2,3-d]pyrimidine-2-yl)aminopyridine-3-yl)piperazine-1-carboxylic acid tert-butyl ester) obtained in step 1) in an organic solvent, adding acid dropwise at the room temperature to remove tert-butyl formate, conducting liquid separation, adding a water-soluble organic solvent to an aqueous layer, separating solids and filtering to obtain ribociclib acid salt; 3) adding water to the ribociclib acid salt for dissolving, adding an adsorbent, filtering and adding alkali to the filtrate to obtain the ribociclib.

CRYSTALLINE FORMS OF RIBOCICLIB SUCCINATE

The present invention relates to crystalline Forms S1 and S2 of ribociclib succinate, processes for their preparation, a pharmaceutical composition comprising these crystalline forms, and their use for the treatment of postmenopausal women with hormone receptor (HR)-positive, human epidermal growth factor receptor 2 (HER2)-negative advanced or metastatic breast cancer.