Discovery of 4-Hydrazinyl-1-methylpiperidine

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A class of pyrazole derivatives is described for use in treating p38 kinase mediated disorders. Compounds of particular interest are defined by Formula I

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Reference:
Piperidine – Wikipedia,
Piperidine | C5H5718N – PubChem

 

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Aberrant Class I PI3K signaling is a key factor contributing to many immunological disorders and cancers. We have identified 4-amino pyrrolotriazine as a novel chemotype that selectively inhibits PI3Kdelta signaling despite not binding to the specificity pocket of PI3Kdelta isoform. Structure activity relationship (SAR) led to the identification of compound 30 that demonstrated efficacy in mouse Keyhole Limpet Hemocyanin (KLH) and collagen induced arthritis (CIA) models.

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Reference:
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Abnormal proliferation mediated by disruption of the mechanisms that keep the cell cycle under control is a hallmark of virtually all cancer cells. Compounds targeting complexes between cyclin-dependent kinases (CDKs) and cyclins (Cy) and inhibiting their activity are regarded as promising antitumor agents to complement the existing therapies. An expansion of pyrazolo[4,3-h]quinazoline chemical class oriented to the development of three points of variability was undertaken leading to a series of compounds able to inhibit CDKs both in vitro and in vivo. Starting from the CDK selective but poorly soluble hit compound 1, we succeeded in obtaining several compounds showing enhanced inhibitory activity both on CDKs and on tumor cells and displaying improved physical properties and pharmacokinetic behavior. Our study led to the identification of compound 59 as a highly potent, orally bioavailable CDK inhibitor that exhibited significant in vivo efficacy on the A2780 ovarian carcinoma xenograft model. The demonstrated mechanisms of action of compound 59 on cancer cell lines and its ability to inhibit tumor growth in vivo render this compound very interesting as potential antineoplastic agent.

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Reference:
Piperidine – Wikipedia,
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1(2H)-Phthalazinones as cytoprotective agents

1(2H)-Phthalazinones such as trans-6-[2-(4-methoxy-phenyl)ethenyl]-2-(3-aminopropyl)phthalazin-1(2H)-one hydrobromide, trans-6-[2-(4-methoxyphenyl)ethenyl]-2-[3–(dimethylamino)propyl]phthalazin-1(2H)-one hydrobromide, and trans-6-[2-(4-hydroxphenyl)ethenyl]-2-[3-(dimethyl-amino)propyl]phthalazin-1(2H)-one hydrochloride are useful as cytoprotective agents in mammals.

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Piperidine – Wikipedia,
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New learning discoveries about 51304-64-4

51304-64-4 4-Hydrazinyl-1-methylpiperidine 10920535, apiperidines compound, is more and more widely used in various fields.

51304-64-4, 4-Hydrazinyl-1-methylpiperidine is a piperidines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated,51304-64-4

Example 6 Trans-6-[2-(4-methoxyphenyl)ethenyl]-2-(1-methyl-4-piperidinyl)phthalazin-1(2H)-one 1-Methyl-4-hydrazinopiperidine (41.2 gm) was dissolved in 1000 ml of ethanol. To this was added 90 gm trans-5-[2-(4-methoxyphenyl)ethenyl]-3-hydroxyphthalide (refer to U.S. patent 4,665,181). The resulting mixture was refluxed for 5 hours, then concentrated to dryness and the product taken up in 2000 ml of 2.5 normal HCl and extracted three times with 700 ml ethyl acetate. The product was basified, extracted into chloroform, and concentrated to dryness. The product was dissolved in isopropanol, acidified with HCl, heated to reflux, charcoaled and allowed to cool and crystallize. After three more crystallizations 3.7 gm of pure material was obtained melting at 297 to 298C.

51304-64-4 4-Hydrazinyl-1-methylpiperidine 10920535, apiperidines compound, is more and more widely used in various fields.

Reference£º
Patent; FISONS CORPORATION; EP309765; (1990); A3;,
Piperidine – Wikipedia
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