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1. 发明申请

WO2008064318A3 PERIPHERAL OPIOID RECEPTOR ACTIVE COMPOUNDS 审中-公开
标题翻译：外用阿片受体活性化合物
公开(公告)号：WO2008064318A3
公开(公告)日：2008-08-21
申请号：PCT/US2007085396
申请日：2007-11-21
申请人： UNIV NEW JERSEY MED , WELSH WILLIAM J , ARORA SONIA , YANG KAIPEEN
发明人： WELSH WILLIAM J , ARORA SONIA , YANG KAIPEEN
IPC分类号： C07D233/61
CPC分类号： C07D249/08 , C07D207/333 , C07D231/12 , C07D263/32 , C07D277/24
摘要： Substituted pyrazoles, imidazoles, triazoles, other 5-membered heteroaromatic ring compounds, substituted 6-membered heteroaromatic ring compounds, fluorene and carbazole compounds, and pyrazoles, imidazoles, triazoles, and other 5- membered heteroaromatic ring compounds substituted with two phenyl groups, may be used as selective peripheral opioid-receptor agonists and antagonist that are designed to elicit the pharmacological effects through the peripheral opioid receptors. These compounds compete with opioid analgesics for binding sites on opioid receptors and particularly the delta and mu opioid receptors, but are unable to cross the blood-brain barrier. Such compounds and pharmaceutical compositions comprising such compounds offer methods of treatment of conditions mediated by opioid receptors, including postoperative and chronic pain, and cytoprotection.
摘要翻译：取代的吡唑，咪唑，三唑，其它5元杂芳环化合物，取代的6元杂芳环化合物，芴和咔唑化合物，以及吡唑，咪唑，三唑和其它被两个苯基取代的5元杂芳环化合物用作选择性周边阿片受体激动剂和拮抗剂，其被设计为通过外周阿片受体诱发药理作用。这些化合物与阿片类镇痛药竞争阿片受体特别是δ和μ阿片受体的结合位点，但不能穿过血脑屏障。包含这些化合物的这些化合物和药物组合物提供治疗由阿片受体介导的病症的方法，包括术后和慢性疼痛以及细胞保护。

2. 发明申请

WO2008064318A2 PERIPHERAL OPIOID RECEPTOR ACTIVE COMPOUNDS 审中-公开
标题翻译：外周阿片受体活性化合物
公开(公告)号：WO2008064318A2
公开(公告)日：2008-05-29
申请号：PCT/US2007/085396
申请日：2007-11-21
申请人： UNIVERSITY OF MEDICINE AND DENTISTRY OF NEW JERSEY , WELSH, William, J. , ARORA, Sonia , YANG, Kaipeen
发明人： WELSH, William, J. , ARORA, Sonia , YANG, Kaipeen
IPC分类号： A61K31/4245
CPC分类号： C07D249/08 , C07D207/333 , C07D231/12 , C07D263/32 , C07D277/24
摘要： Substituted pyrazoles, imidazoles, triazoles, other 5-membered heteroaromatic ring compounds, substituted 6-membered heteroaromatic ring compounds, fluorene and carbazole compounds, and pyrazoles, imidazoles, triazoles, and other 5- membered heteroaromatic ring compounds substituted with two phenyl groups, may be used as selective peripheral opioid-receptor agonists and antagonist that are designed to elicit the pharmacological effects through the peripheral opioid receptors. These compounds compete with opioid analgesics for binding sites on opioid receptors and particularly the delta and mu opioid receptors, but are unable to cross the blood-brain barrier. Such compounds and pharmaceutical compositions comprising such compounds offer methods of treatment of conditions mediated by opioid receptors, including postoperative and chronic pain, and cytoprotection.
摘要翻译：取代的6-元杂芳环化合物，芴和咔唑化合物以及吡唑，咪唑，三唑和其它5-元杂芳环被两个苯基取代的化合物可用作选择性外周阿片受体激动剂和拮抗剂，其被设计为通过外周阿片受体引发药理作用。这些化合物与阿片类镇痛药竞争阿片受体特别是δ阿片受体和μ阿片受体的结合位点，但不能穿过血脑屏障。这种化合物和包含这种化合物的药物组合物提供了治疗由阿片受体介导的病症的方法，包括术后和慢性疼痛以及细胞保护。

3. 发明申请

WO2008064317A1 LIPOPHILIC OPIOID RECEPTOR ACTIVE COMPOUNDS 审中-公开
标题翻译： LIPOPHILIC OPIOID RECEPTOR活性化合物
公开(公告)号：WO2008064317A1
公开(公告)日：2008-05-29
申请号：PCT/US2007/085394
申请日：2007-11-21
申请人： UNIVERSITY OF MEDICINE AND DENTISTRY OF NEW JERSEY , WELSH, William, J. , ARORA, Sonia , YANG, Kaipeen
发明人： WELSH, William, J. , ARORA, Sonia , YANG, Kaipeen
IPC分类号： A01N57/00 , A61K31/675
CPC分类号： C07D249/08
摘要： Substituted pyrazoles, imidazoles, triazoles, other 5-membered heteroaromatic ring compounds, substituted 6-membered heteroaromatic ring compounds, and fluorene and carbazole compounds, may be included in pharmaceutical central nervous system drug compositions to treat a condition mediated by an opioid receptor in a patient. Such compounds are designed to possess improved transport across the blood-brain barrier. These compounds possess an optimal combination of high lipophilicity, low polarity, limited conformational flexibility, and few hydrogen bonding groups. Such lipophilic opioid receptor active compounds are useful for treating pain, inflammation, arthritis, central nervous system disorders, and other diseases.
摘要翻译：取代的吡唑，咪唑，三唑，其它5元杂芳环化合物，取代的6元杂芳环化合物，以及芴和咔唑化合物可以包括在药物中枢神经系统药物组合物中，以治疗由阿片受体介导的病症患者。这些化合物被设计成具有穿过血脑屏障的改善的运输。这些化合物具有高亲油性，低极性，有限的构象柔性和少量氢键基团的最佳组合。这样的亲脂性阿片受体活性化合物可用于治疗疼痛，炎症，关节炎，中枢神经系统疾病和其他疾病。

4. 发明申请

WO2008064310A3 MIXED OPIOID RECEPTOR ACTIVE COMPOUNDS 审中-公开
标题翻译：混合的阿片受体活性化合物
公开(公告)号：WO2008064310A3
公开(公告)日：2008-08-21
申请号：PCT/US2007085384
申请日：2007-11-21
申请人： UNIV NEW JERSEY MED , WELSH WILLIAM J , ARORA SONIA , YANG KAIPEEN
发明人： WELSH WILLIAM J , ARORA SONIA , YANG KAIPEEN
IPC分类号： A61K31/53
CPC分类号： C07D249/10
摘要： Pyrazoles, imidazoles, triazoles, other 5-membered heteroaromatic ring compounds substituted with two phenyl groups, and like compounds, may be included in pharmaceutical compositions to treat a condition mediated by an opioid receptor in a patient. The compounds possess a high binding affinity and high selectivity for delta, kappa and mu opioid receptors. Such mixed opioid receptor active compounds are useful for treating pain, inflammation, arthritis, central nervous system disorders, and other diseases.
摘要翻译：吡唑，咪唑，三唑，被两个苯基取代的其它5元杂芳环化合物和类似化合物可以包括在药物组合物中以治疗患者中由阿片受体介导的病症。该化合物对δ，κ和μ阿片受体具有高结合亲和力和高选择性。这样的混合阿片受体活性化合物可用于治疗疼痛，炎症，关节炎，中枢神经系统疾病和其它疾病。

5. 发明申请

WO2008064310A2 MIXED OPIOID RECEPTOR ACTIVE COMPOUNDS 审中-公开
标题翻译：混合阿片类药物受体活性化合物
公开(公告)号：WO2008064310A2
公开(公告)日：2008-05-29
申请号：PCT/US2007/085384
申请日：2007-11-21
申请人： UNIVERSITY OF MEDICINE AND DENTISTRY OF NEW JERSEY , WELSH, William, J. , ARORA, Sonia , YANG, Kaipeen
发明人： WELSH, William, J. , ARORA, Sonia , YANG, Kaipeen
IPC分类号： A01N43/66
CPC分类号： C07D249/10
摘要： Pyrazoles, imidazoles, triazoles, other 5-membered heteroaromatic ring compounds substituted with two phenyl groups, and like compounds, may be included in pharmaceutical compositions to treat a condition mediated by an opioid receptor in a patient. The compounds possess a high binding affinity and high selectivity for delta, kappa and mu opioid receptors. Such mixed opioid receptor active compounds are useful for treating pain, inflammation, arthritis, central nervous system disorders, and other diseases.
摘要翻译：吡唑类，咪唑类，三唑类，被两个苯基取代的其它5元杂芳族环化合物和类似化合物可包含在药物组合物中以治疗患者中由阿片受体介导的病症。这些化合物对δ，κ和μ阿片受体具有高结合亲和力和高选择性。这种混合的阿片受体活性化合物可用于治疗疼痛，炎症，关节炎，中枢神经系统疾病和其他疾病。

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