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Novel heterocyclic compounds as HSP90-inhibitors

A kind of compound, the technology of heterocyclic group, be applied in the field of heterocyclic compound, can solve the problem such as not being reported

Inactive Publication Date: 2010-06-09
CONFORMAL THERAPEUTICS CORP (US)
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, compounds with desirable potency, selectivity, and pharmaceutical properties required to effectively inhibit HSP90 in vivo have not been reported

Method used

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  • Novel heterocyclic compounds as HSP90-inhibitors
  • Novel heterocyclic compounds as HSP90-inhibitors
  • Novel heterocyclic compounds as HSP90-inhibitors

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[1221] Example 1. 2-Chloro-1-chloromethyl-3,4,5-trimethoxy-benzene

[1222]

[1223] According to the general procedure 3.1, 5-chloromethyl-1,2,3-trimethoxy-benzene was chlorinated with NCS to obtain the title compound.

[1224] 1 H-NMR(CDCl 3 ): δ 6.82 (s, 1H), 4.70 (s, 1H), 3.93 (s, 3H), 3.90 (s, 3H) 3.87 (s, 3H).

Embodiment 2

[1225] Example 2. 2-Chloro-6-chloromethyl-4-methoxy-3,5-dimethyl-pyridine

[1226]

[1227] Step 1: 2-Chloromethyl-4-methoxy-3,5-dimethylpyridine-1-oxide

[1228] Follow general procedure 2.1 to oxidize 2-chloromethyl-4-methoxy-3,5-dimethyl-pyridine to obtain the title compound. HPLC Rt: 4.46 minutes. 1 H-NMR(CDCl 3 ): δ 8.05 (s, 1H), 4.93 (s, 2H), 3.77 (s, 3H), 2.37 (s, 3H), 2.24 (s, 3H).

[1229] Step 2: 2-Chloro-6-chloromethyl-4-methoxy-3,5-lutidine

[1230] Follow the general step 2.6 with POCl 3 Treatment of 2-chloromethyl-4-methoxy-3,5-lutidine-1-oxide gave the title compound. HPLC Rt: 6.757 minutes. 1 H-NMR(CDCl 3 ): δ 4.64 (s, 2H), 3.79 (s, 3H), 2.35 (s, 3H), 2.33 (s, 3H).

Embodiment 3

[1231] Example 3. 4-Chloro-2-chloromethyl-3,5-dimethyl-pyridine

[1232]

[1233] Use POCl in the same way as in the general step 2.6 3 Treatment of 2-chloromethyl-3,5-lutidine-4-ol (Tarbit, et al., WO 99 / 10326) gave the title compound (74% yield). HPLC Rt: 5.54 minutes. 1 H-NMR(CDCl 3 ): δ 8.24 (s, 1H), 4.71 (s, 2H), 2.48 (s, 3H), 2.36 (s, 3H).

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Abstract

Novel heterocyclic compounds are described and demonstrated to have utility as Heat Shock Protein 90 (HSP90) inhibiting agent. Method of synthesis and use of such compounds are also described.

Description

Invention field [0001] In general, the present invention relates to heterocyclic compounds and related compounds and their broad-spectrum uses, for example, to inhibit heat shock protein 90 (HSP90) to treat or prevent HSP90-mediated diseases. Background of the invention [0002] HSP90 is a ubiquitous chaperone protein, which participates in the folding, activation and combination of various proteins, including the main proteins involved in signal transduction, cell cycle control and transcription regulation. Researchers have reported that HSP90 chaperone proteins and important signaling proteins, such as steroid hormone receptors and protein kinases, including, for example, Raf-1, EGFR, v-Src family kinases, Cdk4 and ErbB-2 (Buchner J. TIBS 1999, 24, 136-141; Stepanova, L. et al., Genes Dev. 1996, 10, 1491-502; Dai, K. et al., J. Biol. Chem. 1966, 271, 22030-4). Studies have further shown that certain co-chaperones, such as HSP70, p60 / Hop / Stil, Hip, Bag1, HSP40 / Hdj2 / Hsj1, immuno...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07D487/04C07D471/04C07D473/32C07D473/40C07D473/18C07D473/24A61K31/519A61K31/522A61K31/52A61P35/00A61P37/06
Inventor 斯里尼瓦斯·R·卡西布哈特拉马库斯·F·贝姆凯文·D·翁马科·A·比亚蒙特史建栋让·伊夫·勒布拉齐代克张琳戴维·赫斯特
Owner CONFORMAL THERAPEUTICS CORP (US)
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