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The novel compound represented by Chemical Formula, according to the present invention can be used as an active ingredient for preventing or treating 1-bromodomain,containing protein-related diseases or conditions, comprising the novel compound represented by Chemical Formula (cereblon) E3 according to the present invention as an active ingredient, which can be used (Degraducer)-fold, ubiquitin ligase as an active ingredient for inducing degradation of a (cereblon) E3,target protein-related disease or a, condition, as an 1 active ingredient, to provide a, health – functional food composition for prevention or treatment of diseases or conditions associated with various diseases as an active ingredient. KIPO & WIPO & WIPL- for prevention or treatment of diseases or conditions associated with various diseases as an active ingredient. (by machine translation)

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Reference:
Piperidine – Wikipedia,
Piperidine | C5H9479N – PubChem

 

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Provided are 5-substituted quinazolinone compounds, and pharmaceutically acceptable salts, solvates, clathrates, stereoisomers, and prodrugs thereof. Methods of use, and pharmaceutical compositions of these compounds are disclosed.

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Reference:
Piperidine – Wikipedia,
Piperidine | C5H9518N – PubChem

 

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We previously disclosed the identification of cereblon modulator 3 (CC-885), with potent antitumor activity mediated through the degradation of GSPT1. We describe herein the structure-activity relationships for analogs of 3 with exploration of the structurally related dioxoisoindoline class. The observed activity of protein degradation could in part be rationalized through docking into the previously disclosed 3-CRBN-GSPT1 cocrystal ternary complex. For SAR that could not be rationalized through the cocrystal complex, we sought to predict SAR through a QSAR model developed in house. Through these analyses, selective protein degradation could be achieved between the two proteins of interest, GSPT1 and Aiolos.

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Reference:
Piperidine – Wikipedia,
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Substituted 1,3-dioxo-2-(2,6-dioxopiperidin-3-yl)isoindolines and 1-oxo-2-(2,6-dioxo-piperidin-3-yl)isoindolines reduce the levels of TNFa in a mammal and are useful in treating oncogenic conditions, inflammation, and autoimmune diseases. Typical embodiments are 1-oxo-2-(2,6-dioxo-3-methylpiperidin-3-yl)-4,5,6,7-tetrafluoroiso-indoline and 1,3-dioxo-2-(2,6-dioxo-3-methylpiperidin-3-yl)-4-aminoisoindoline.

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Reference:
Piperidine – Wikipedia,
Piperidine | C5H9561N – PubChem

 

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The compound shown, by the invention is a compound I shown in the formula, I shown in the formula I, or, a, stereoisomer, of the, compound shown in the formula shown in the formula I, a tautomer of a solvate BTK thereof, a salt, or a prodrug thereof EGFR, ITK, TEC, a pharmaceutically acceptable salt thereof, or a prodrug thereof BTK .X – Y – Z I. (by machine translation)

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Reference:
Piperidine – Wikipedia,
Piperidine | C5H9500N – PubChem

 

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The invention discloses a method for the preparation of amine to that, which belongs to the field of organic synthesis. Through to 2 – methyl – 3 – nitro-benzoic acid methyl ester and 3 – N – benzyloxy carbonyl – L – glutamine as the starting material, 2 – methyl – 3 – nitro-benzoic acid methyl ester after bromo reaction, to obtain the important intermediate 2 – bromomethyl – 3 – nitro-benzoic acid methyl ester. 3 – N – benzyloxy carbonyl – L – glutamine in under the catalytic action of the cyclization reaction, generating 3 – N – benzyloxycarbonyl amino – 2, 6 – dioxopiperidin, amino deprotected to produce 3 – amino – 2, 6 – piperidine dione hydrohalide salt, then with 2 – bromomethyl – 3 – nitro-benzoic acid methyl ester by the ammonolysis reaction to obtain 3 – (4 – nitro – 1 – oxo – 1, 3 – ISO-Indol – 2 – yl) piperidine – 2, 6 – dione, by reduction reaction to that amine. The route has the low cost of raw materials, easy post treatment, the yield and the like, so that the amine to greatly reduce the production cost of the raw material. This invention is a convenient, efficient and suitable for industrial production of synthetic method to that amine. (by machine translation)

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Reference:
Piperidine – Wikipedia,
Piperidine | C5H9491N – PubChem

 

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Processes for the preparation of substantially pure lenalidomide. The application also relates to an enriched, substantially pure, and pure amorphous form of lenalidomide and solid dispersions containing amorphous lenalidomide.

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The present application provides bifunctional compounds of Formula (I), or Targeting Ligand, or a pharmaceutically acceptable salt, hydrate, solvate, prodrug, stereoisomer, or tautomer thereof, which act as protein degradation inducing moieties for cyclin-dependent kinase 4 (CDK4) and/or cyclin-dependent kinase 6 (CDK6). The present application also relates to methods for the targeted degradation of CDK4 and/or CDK6 through the use of the bifunctional compounds that link a ubiquitin ligase-binding moiety to a ligand that is capable of binding to CDK4 and/or CDK6 which can be utilized in the treatment of disorders modulated by CDK4 and/or CDK6.

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Piperidine – Wikipedia,
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The invention discloses a method for the preparation of amine to that, the specific step includes: to 2 – methyl – 3 – nitro benzoic acid as the raw material, to obtain 2 – bromomethyl – 3 – nitro-benzoic acid methyl ester; L – glutamic acid as the raw material to make the N – CBZ – L – glutamic acid; to N – CBZ – L – glutamic acid as the raw material to make the 3 – amino – 2, 6 – piperidine dione hydrochloride; to 2 – methyl – 3 – nitro-benzoic acid methyl ester with 3 – amino – 2, 6 – piperidine dione hydrochloride as the raw material to make the 3 – (4 – nitro – 1, 3 dihydro – 1 – oxo – 2 hydrogen – isoindol – 2 – yl) piperidine – 2, 6 – dione; to 3 – (4 – nitro – 1, 3 dihydro – 1 – oxo – 2 hydrogen – isoindol – 2 – yl) piperidine – 2, 6 – dione as raw materials to that amine. The method of the invention has simple technological process, raw material economic, few by-products, and purification is simple, high yield, environment-friendly and the like, after treatment is simple, has better practicability and application value, has great industrial prospects. (by machine translation)

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Piperidine – Wikipedia,
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Proteolysis targeting chimeras (PROTACs) are bispecific molecules containing a target protein binder and an ubiquitin ligase binder connected by a linker. By recruiting an ubiquitin ligase to a target protein, PROTACs promote ubiquitination and proteasomal degradation of the target protein. The generation of effective PROTACs depends on the nature of the protein/ligase ligand pair, linkage site, linker length, and linker composition, all of which have been difficult to address in a systematic way. Herein, we describe a “click chemistry” approach for the synthesis of PROTACs. We demonstrate the utility of this approach with the bromodomain and extraterminal domain-4 (BRD4) ligand JQ-1 (3) and ligase binders targeting cereblon (CRBN) and Von Hippel-Lindau (VHL) proteins. An AlphaScreen proximity assay was used to determine the ability of PROTACs to form the ternary ligase-PROTAC-target protein complex and a MSD assay to measure cellular degradation of the target protein promoted by PROTACs.

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Reference:
Piperidine – Wikipedia,
Piperidine | C5H9522N – PubChem