- RIBOCICLIB INTERMEDIATE AND PROCESS FOR PREPARATION THEREOF
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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.
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- 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
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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.
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- PREPARATION METHOD OF RIBOCICLIB AND ITS SALT AND CRYSTALLINE FORM THEREOF
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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.
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Paragraph 0044-0045
(2021/02/20)
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- Polymorphic substances of ribosinil monosuccinate and preparation method and use thereof
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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.
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Paragraph 0151-0153
(2020/04/17)
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- Crystal form of and preparation method and application thereof (by machine translation)
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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)
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Paragraph 0184-0188
(2020/10/14)
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- NOVEL POLYMORPHS OF RIBOCICLIB SUCCINATE
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The present invention relates to novel crystalline forms of Ribociclib Succinate and its preparation process.
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Page/Page column 10-12
(2020/11/23)
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- AN IMPROVED PROCESS FOR THE PREPARATION OF RIBOCICLIB SUCCINATE AND ITS NOVEL CRYSTALLINE FORMS THEREOF
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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
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- IMPROVED PROCESS FOR THE PREPARATION OF 7-CYCLOPENTYL-N, N-DIMETHYL-2-(5-(PIPERAZIN-1-YL) PYRIDIN-2-YLAMINUTESO)-7H-PYRROLO[2,3-D] PYRIMIDINE-6-CARBOXAMIDE SUCCINATE (RIBOCICLIB SUCCINATE) AND ITS CRYSTALLINE FORMS THEREOF
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The present invention relates to an improved process for the preparation of Ribociclib succinate (1) and the novel crystalline forms thereof. More particularly the invention relates to the process for the preparation of novel crystalline forms of Ribociclib succinate (1).
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Page/Page column 15; 16
(2019/08/26)
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- AN IMPROVED PROCESS FOR THE PREPARATION OF RIBOCICLIB AND ITS SALTS
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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.
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- Preparation method of ribociclib and product and use thereof
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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.
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- CRYSTALLINE FORMS OF RIBOCICLIB SUCCINATE
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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.
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Page/Page column 2; 14; 15
(2019/06/23)
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- NOVEL POLYMORPHS OF RIBOCICLIB MONO SUCCINATE
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The present invention relates to novel crystalline and amorphous polymorphic forms of Ribociclib(l) mono succinate. (I) Said crystalline forms may be useful in the improved preparation of oral dosage forms for the treatment of cancer.
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Page/Page column 15; 16
(2019/07/13)
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- NOVEL POLYMORPHS OF RIBOCICLIB SUCCINATE
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The present invention discloses novel crystalline polymorphic forms of ribociclib succinate, methods of preparation, pharmaceutical compositions and methods of therapeutic treatment involving polymorphic forms thereof.
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Page/Page column 33
(2019/09/18)
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- RIBOCICLIB SALTS AND SOLID STATE FORMS THEREOF
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The present disclosure relates to Ribociclib solid state forms, Ribociclib salts including Ribociclib succinate and solid state forms thereof, as well as processes for preparation thereof and pharmaceutical compositions thereof.
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- Salt of Pyrrolo[2,3-D]pyrimidine Compound and Novel Polymorph of Salt
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The present invention relates to novel crystalline forms of 7-cyclopentyl-2-(5-piperazin-1-yl-pyridin-2-ylamino)-7H-pyrrolo[2,3-d]pyrimidine-6-car boxylic acid dimethylamide(compound I), its salts, and process for preparation thereof. Crystalline forms in the present invention have good stability, low hygroscopicity, good processability, easy treatability and other favorable properties. In addition, the process is simple, low cost, and has an important value for future optimization and development of the drug.
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Paragraph 0130; 0131; 0132
(2018/01/04)
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- SALT(S) OF 7-CYCLOPENTYL-2-(5-PIPERAZIN-1-YL-PYRIDIN-2-YLAMINO)-7H-PYRROLO[2,3-D]PYRIMIDINE-6-CARBOXYLIC ACID DIMETHYLAMIDE AND PROCESSES OF MAKING THEREOF
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This invention relates to (1) process of making 7-Cyclopentyl-2-(5-piperazin-1-yl-pyridin-2-ylamino)-7H-pyrrolo[2,3-d]pyrimidine-6-carboxylic acid dimethylamide and salts thereof; (2) novel salt(s) of 7-Cyclopentyl-2-(5-piperazin-1-yl-pyridin-2-ylamino)-7H-pyrrolo[2,3-d]pyrimidine-6-carboxylic acid dimethylamide; (3) pharmaceutical compositions comprising the same; and (4) methods of treatment using the same.
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