- TRIFLUOROMETHYL-SUBSTITUTED SULFONAMIDE AS BCL-2-SELECTIVE INHIBITOR
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Disclosed is a trifluoromethyl-substituted sulfonamide BCL-2-selective inhibitor, in particular disclosed are a compound of formula I, a stereoisomer or a pharmaceutically acceptable salt thereof, a preparation method therefor, and a pharmaceutical composition thereof. Also disclosed are the uses of said compound and of a pharmaceutical composition comprising same for treating anti-apoptotic BCL-2-related diseases, such as cancer.
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Paragraph 0120-0121
(2021/08/05)
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- BCL-2 INHIBITORS AND THEIR USE AS PHARMACEUTICALS
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The disclosure is directed to, in part, to BCL-2 inhibitors, pharmaceutical compositions comprising the same, as well as methods of their use and preparation.
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Paragraph 0449-0450
(2021/11/13)
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- PROCESS FOR THE PREPARATION OF 4-(4-{[2-(4-CHLOROPHENYL)-4,4-DIMETHYLCYCLOHEX-1-EN-1- YL]METHYL}PIPERAZIN-1-YL)-N-({3-NITRO-4-[(TETRAHYDRO-2H-PYRAN-4-YLMETHYL)AMINO] PHENYL}SULFONYL)-2-(1H-PYRROLO[2,3-B]PYRIDIN-5-YLOXY)BENZAMIDE)
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The present invention relates to novel crystalline forms of 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-({3-nitro-4-[(tetrahydro-2H-pyran -4-ylmethyl)amino]phenyl}sulfonyl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide compound of formula-1 represented by the following structural formula-1, which is referred to as Venetoclax Formula-1 The present invention also relates to an improved process for the preparation of Venetoclax compound of formula-1 which is free of Impurity-I, Impurity-II, Impurity-III and Impurity-IV.
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Page/Page column 28
(2020/03/29)
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- Venetoclax and dihydroartemisinin compound and preparation method and application thereof
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The invention belongs to the technical field of medicines, and relates to a Venetoclax and dihydroartemisinin compound, pharmaceutically acceptable salts, hydrates and optical isomers thereof, a pharmaceutical composition taking the compound as an active component, and an application of the compound in preparation of medicines for treating cancers. The structure of the Venetoclax and dihydroartemisinin compound is as shown in a general formula I in the specification, wherein L is as described in the claims and the specification.
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Paragraph 0050; 0089-0092
(2021/03/05)
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- Solid dispersions containing an apoptosis-inducing agent
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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.
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Page/Page column 211
(2019/03/15)
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- Bcl-2 INHIBITORS
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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.
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Paragraph 1099; 1100
(2019/11/19)
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- Preparation method of B cell lymphoma factor-2 inhibitor ABT-199
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The invention discloses a preparation method of a B cell lymphoma factor-2 inhibitor ABT-199, and belongs to the field of pharmaceutical synthesis. The method comprises the following steps: substituting a starting material methyl 4-fluorosalicylate that is compound II with tert-butyl-1-piperazinecarboxylate that is compound III in the presence of a phase transfer catalyst, then de-protecting underthe acidic condition to obtain a compound IV, performing reductive amination on the compound IV and a synthesized key intermediate compound V in the presence of a catalyst (sodium triacetoxyborohydride) to obtain an intermediate VI, substituting the intermediate VI with a raw material VII that is 5-bromo-azaindole, then directly hydrolyzing and acidifying the obtained esterified product to obtainan intermediate VIII, and finally amidating the intermediate VIII and a raw material compound IX to obtain a target product compound I. The raw materials are easy to purchase or synthesize, the synthesis steps are short, the total yield is more than or equal to 40%, the use of expensive or difficult-to-purchase raw materials is avoided, and the method is suitable for industrial production.
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Paragraph 0055; 0058; 0059
(2019/01/08)
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- PROCESS FOR THE PREPARATION OF VENETOCLAX
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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.
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Page/Page column 27
(2018/03/06)
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- Processes For The Preparation Of An Apoptosis-Inducing Agent
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Provided herein is a process for the preparation of an apoptosis-inducing agent, and chemical intermediates thereof. Also provided herein are novel chemical intermediates related to the process provided herein.
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Paragraph 0142; 0143
(2014/09/30)
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- APOPTOSIS-INDUCING AGENTS FOR THE TREATMENT OF CANCER AND IMMUNE AND AUTOIMMUNE DISEASES
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Disclosed are compounds which inhibit the activity of anti-apoptotic Bcl-2 proteins, compositions containing the compounds and methods of treating diseases during which is expressed anti-apoptotic Bcl-2 protein.
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Page/Page column 106; 107
(2010/07/04)
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