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1. 发明申请

WO2008012110A2 ANNELLATED PYRROLE COMPOUNDS FOR CANCER MANAGEMENT 审中-公开
标题翻译：用于癌症管理的安息香精化合物
公开(公告)号：WO2008012110A2
公开(公告)日：2008-01-31
申请号：PCT/EP2007/006735
申请日：2007-07-30
申请人： MERCKLE GMBH , LAUFER, Stefan , GUARNIERI, Tiziana , TAVOLARI, Simona , TOMASI, Vittorio , PALAZZINI, Ernesto , BARBANTI, Miriam
发明人： LAUFER, Stefan , GUARNIERI, Tiziana , TAVOLARI, Simona , TOMASI, Vittorio , PALAZZINI, Ernesto , BARBANTI, Miriam
CPC分类号： A61K31/407
摘要： The present invention relates to the use of annellated pyrrole compounds and in particular ML3000 (licofelone), salts or derivatives thereof, for cancer management, and in general to the use of a compound of Formula (I): wherein the variables have the meanings given in the present description, for the prevention and/or treatment of neoplasia, in particular neoplasia selected from the group consisting of papilloma, carcinoma, adenoma and adenocarcinoma, e. g. human airway or colorectal carcinoma, preferably fast-growing, multidrug resistant and/or COX-2 negative neoplasia. The invention further relates to pharmaceutical compositions for the aforesaid purposes, comprising annellated pyrrole compounds and in particular ML3000 (licofelone), optical isomers, salts or derivatives thereof, as well as to a method of treating and/or preventing neoplasia and/or restoring the ability to undergo apoptosis in a cell having lost the same. This treatment ameliorates, diminishes, actively treats, reverses or prevents any disease related to insufficient apoptosis, in particular neoplasia, and it may be combined with irradiation, heating and treatment with a cytotoxic agent for preventive and/or curative purposes.
摘要翻译：本发明涉及环状吡咯化合物，特别是ML3000（licofelone），其盐或衍生物用于癌症治疗，通常涉及使用式（I）化合物的用途：其中变量具有给定的含义在本说明书中，为了预防和/或治疗肿瘤形成，特别是选自乳头瘤，癌，腺瘤和腺癌的瘤形成， G。人类气道或结肠直肠癌，优选快速生长，多药耐药和/或COX-2阴性瘤形成。本发明还涉及用于上述目的的药物组合物，其包含环状吡咯化合物，特别是ML3000（licofelone），旋光异构体，其盐或衍生物，以及治疗和/或预防肿瘤形成和/或恢复的方法在失去相同细胞的细胞凋亡的能力。该治疗改善，减少，积极治疗，逆转或预防与细胞凋亡不足有关的任何疾病，特别是瘤形成，并且可以与辐射，加热和用细胞毒性剂治疗相结合以用于预防和/或治疗目的。

2. 发明申请

WO2008012110A3 ANNELLATED PYRROLE COMPOUNDS FOR CANCER MANAGEMENT 审中-公开
标题翻译：新型吡咯类化合物用于癌症治疗
公开(公告)号：WO2008012110A3
公开(公告)日：2008-04-10
申请号：PCT/EP2007006735
申请日：2007-07-30
申请人： MERCKLE GMBH , LAUFER STEFAN , GUARNIERI TIZIANA , TAVOLARI SIMONA , TOMASI VITTORIO , PALAZZINI ERNESTO , BARBANTI MIRIAM
发明人： LAUFER STEFAN , GUARNIERI TIZIANA , TAVOLARI SIMONA , TOMASI VITTORIO , PALAZZINI ERNESTO , BARBANTI MIRIAM
IPC分类号： A61K31/407 , A61P35/00
CPC分类号： A61K31/407
摘要： The present invention relates to the use of annellated pyrrole compounds and in particular ML3000 (licofelone), salts or derivatives thereof, for cancer management, and in general to the use of a compound of Formula (I): wherein the variables have the meanings given in the present description, for the prevention and/or treatment of neoplasia, in particular neoplasia selected from the group consisting of papilloma, carcinoma, adenoma and adenocarcinoma, e. g. human airway or colorectal carcinoma, preferably fast-growing, multidrug resistant and/or COX-2 negative neoplasia. The invention further relates to pharmaceutical compositions for the aforesaid purposes, comprising annellated pyrrole compounds and in particular ML3000 (licofelone), optical isomers, salts or derivatives thereof, as well as to a method of treating and/or preventing neoplasia and/or restoring the ability to undergo apoptosis in a cell having lost the same. This treatment ameliorates, diminishes, actively treats, reverses or prevents any disease related to insufficient apoptosis, in particular neoplasia, and it may be combined with irradiation, heating and treatment with a cytotoxic agent for preventive and/or curative purposes.
摘要翻译：本发明涉及口服吡咯化合物，特别是ML3000（Licofelone），其盐或衍生物用于癌症治疗，并且一般涉及式（I）化合物的用途：其中变量具有给定的含义在本说明书中，用于预防和/或治疗瘤形成，特别是选自由乳头瘤，癌，腺瘤和腺癌组成的组的瘤形成， G。人气道或结直肠癌，优选快速生长，多药耐药性和/或COX-2阴性瘤形成。本发明进一步涉及用于上述目的的药物组合物，其包含螺化的吡咯化合物，特别是ML3000（Licofelone），其旋光异构体，盐或衍生物，以及治疗和/或预防瘤形成和/或恢复在失去细胞的细胞中发生细胞凋亡的能力。该治疗改善，减少，积极治疗，逆转或预防任何与细胞凋亡不足有关的疾病，特别是瘤形成，并且可以将其与辐射，加热和用细胞毒剂治疗组合用于预防和/或治疗目的。

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