- Synthesis method of ribociclib intermediate product and intermediate compound thereof
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The invention discloses a synthesis method of a ribociclib intermediate product, which comprises the following steps: by using barbituric acid as a starting material, carrying out chlorination and formylation to obtain a compound 2; and performing condens
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Paragraph 0089-0091
(2020/05/14)
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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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Page/Page column 25-27
(2020/11/12)
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- CDK9 inhibitor, preparation method and application thereof
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The invention provides a CDK9 inhibitor, the CDK9 inhibitor is a pyrimidopyrrole kinase inhibitor, and the chemical structural general formula of the CDK9 inhibitor is shown as the formula I in the specification, the CDK9 inhibitor is the pyrimidopyrrole kinase inhibitor, the protein target adapted to the pyrimidopyrrole kinase is serine/threonine kinase CDK9. The CDK9 inhibitor shows relatively high specificity and low cytotoxicity, and the CDK9 inhibitor which is used for preventing or treating tumor growth and metastasis, has selectivity on CDK9, and is small in toxic and side effects and strong in action effect is provided, so that the CDK9 inhibitor is used for regulating and controlling the biological function of CDK9 and inhibiting the growth and proliferation processes of tumors.
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Paragraph 0106-0107; 0115-0116
(2021/01/04)
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- Synthesis method of antineoplastic drug ribociclib intermediate
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The invention relates to a synthesis method of an antineoplastic drug ribociclib intermediate. The synthesis method includes the following steps that the electrophilic addition reaction is conducted on N,N-dimethylacrylamide and bromine to obtain N,N-dime
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Paragraph 0032; 0061-0078
(2019/11/13)
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- Synthesis method of anti-tumor drug ribociclib
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The invention relates to a synthesis method of an anti-tumor drug ribociclib. The method mainly comprises the steps of carrying out a reaction between 4-(6-amino-3-pyridyl)-1-piperazinyl tert-butyl formate and 2-chloro-7-cyclopentyl-N,N-dimethyl-7H-pyrrol
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Paragraph 0041; 0081-0098
(2019/11/14)
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- SUBSTITUTED PYRROLOPYRIMIDINE CDK INHIBITOR, PHARMACEUTICAL COMPOSITION CONTAINING SAME AND USE THEREOF
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The present invention belongs to the field of pharmaceutical chemistry, and relates to a substituted pyrrolopyrimidine CDK inhibitor, in particular to a compound as shown in formula I or a pharmaceutically acceptable salt or solvate thereof, as well as a preparation method thereof and a pharmaceutical composition thereof. The present invention also relates to the use of the compound and the pharmaceutical composition thereof in the preparation of a drug for treating diseases associated with CDK inhibition. The compound according to the present invention has a marked inhibitory effect on CDK, excellent drug absorption and significantly superior oral absorption effect.
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Paragraph 0109; 0114; 0115
(2019/02/09)
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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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Page/Page column 19-20
(2019/08/08)
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- Key intermediate for synthesis of CDK 4/6 dual inhibitor and preparation method and application of key intermediate
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The invention discloses a 2-chloro-7-cyclopentyl-N,N-dimethyl-7H-pyrrolo[2,3-d]pyrimidine-6-methanamide intermediate and a preparation method and application thereof. The intermediate is the compoundI, and the preparation method comprises the following st
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Paragraph 0119; 0122-0125; 0128-0131; 0134-0137; 0141-0143
(2019/08/20)
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- New intermediate of ribociclib, and synthetic method for preparing ribociclib by using new intermediate
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The invention provides a new intermediate compound 6 of ribociclib, and a preparation method thereof, and a synthetic method for preparing ribociclib by using the new intermediate compound 6, whereinthe structure of the compound 6 is defined in the specif
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Paragraph 0106; 0107
(2018/10/19)
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- THIENOPYRANONES AND FURANOPYRANONES AS KINASE, BROMODOMAIN, AND CHECKPOINT INHIBITORS
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The invention relates to compounds and methods of treating diseases including but not limited to, cancer, non-cancer proliferative disease, sepsis, autoimmune disease, viral infaction, atheroscleosis. Type 1 or 2 diabetes, obesity, inflammatory disease, o
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Paragraph 0218
(2018/08/20)
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- Synthesis technology of ribociclib
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The invention discloses a synthesis technology of ribociclib. The synthesis technology comprises the following steps: 1) in the presence of cesium carbonate, 2-chloro-4-cyclopentylaminopyrimidine and 3-bromo-2-oxo-N,N-dimethylpropionamide react under the
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Paragraph 0030-0035; 0036-0041; 0042-0047; 0048-0053
(2017/08/31)
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- New synthesis method of ribociclib intermediate
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The invention discloses preparation of a ribociclib key intermediate A; propiolic acid ester or amide 2 is directly used as a Sonogashira coupling side chain, coupling conditions are optimized, an intermediate 3 is obtained with relatively high yield, the intermediate 3 is directly subjected to ring closing under simple conditions to complete construction of a mother ring molecule, to obtain a structural formula A or a precursor ester 4 of the structural formula A, and the precursor ester 4 is subjected to hydrolysis and condensation to obtain the structural formula A. The route has simple operation, reaction steps are shorted, the yield is relatively high, and the purity of the obtained product is relatively high, and the method is suitable for enlarged production, wherein the reaction route is described in the specification.
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Paragraph 0050; 0051; 0052
(2017/08/27)
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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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Page/Page column 7-8
(2012/05/20)
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- PYRROLOPYRIMIDINE COMPOUNDS AS CDK INHIBITORS
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The disclosed compounds relate to treatments and therapies for protein kinase-associated disorders. There is also a need for compounds useful in the treatment or prevention or amelioration of one or more symptoms of cancer, transplant rejections, and autoimmune diseases. Furthermore, there is a need for methods for modulating the activity of protein kinases, such as CDK1, CDK2, CDK4, CDK5, CDK6, CDK7, CDK8 and CDK9, using the compounds provided herein
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Page/Page column 89; 91
(2010/04/03)
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