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1. 发明申请

US20130177632A1 2,4,5-TRISUBSTITUTED IMIDAZOLES AND THEIR USE AS ANTI-MICROBIAL AGENTS 有权
标题翻译： 2,4,5-三唑基咪唑及其作为抗微生物剂的用途
公开(公告)号：US20130177632A1
公开(公告)日：2013-07-11
申请号：US13778458
申请日：2013-02-27
申请人： Raed H. Al-Qawasmeh , Aiping H. Young , Mario Huesca , Yoon S. Lee
发明人： Raed H. Al-Qawasmeh , Aiping H. Young , Mario Huesca , Yoon S. Lee
IPC分类号： A01N43/90 , A01N43/50 , C07D403/04 , C07D401/14 , C07D409/14 , C07D471/14 , A61K31/4164 , A61K31/4178 , A61K31/444 , A61K31/4439 , A61K31/4184 , A61K31/454 , A61K31/4375 , A61K45/06 , C07D233/64
CPC分类号： A01N43/90 , A01N43/50 , A01N43/52 , A23L3/3544 , A61K31/4164 , A61K31/4178 , A61K31/4184 , A61K31/4188 , A61K31/4375 , A61K31/4439 , A61K31/444 , A61K31/454 , A61K45/06 , A61L2/18 , C07D233/22 , C07D233/64 , C07D235/02 , C07D401/14 , C07D403/04 , C07D403/14 , C07D409/14 , C07D471/14 , E05B1/0069
摘要： The present invention provides therapeutically effective 2,4,5-trisubstituted imidazole compounds, methods of preparing the same, and compositions comprising the compounds alone or in combination with other agents. The present invention further provides for the use of the compounds as anti-microbial agents. The anti-microbial properties of the compounds include anti-bacterial and/or anti-fungal activity.
摘要翻译：本发明提供治疗有效的2,4,5-三取代的咪唑化合物，其制备方法，以及包含单独或与其它试剂组合的化合物的组合物。本发明还提供了化合物作为抗微生物剂的用途。化合物的抗微生物性质包括抗细菌和/或抗真菌活性。

2. 发明授权

US08969372B2 Aryl imidazoles and their use as anti-cancer agents 有权
标题翻译：芳基咪唑及其作为抗癌剂的用途
公开(公告)号：US08969372B2
公开(公告)日：2015-03-03
申请号：US10579149
申请日：2004-11-15
申请人： Mario Huesca , Raed Al-Qawasmeh , Aiping H. Young , Yoon Lee
发明人： Mario Huesca , Raed Al-Qawasmeh , Aiping H. Young , Yoon Lee
IPC分类号： A61K31/4745 , A61K31/4188 , A61K31/4178 , C07D233/64 , C07D235/02 , C07D401/14 , C07D403/04 , C07D403/14 , C07D409/14 , C07D495/04
CPC分类号： A61K31/4184 , A61K31/4178 , A61K31/4188 , A61K31/4745 , C07D233/64 , C07D235/02 , C07D401/14 , C07D403/04 , C07D403/14 , C07D409/14 , C07D495/04
摘要： Therapeutically effective 2,4,5-trisubstituted imidazole compounds are provided. Also provided are methods of preparing the compounds and pharmaceutical compositions comprising the compounds alone or in combination with other agents. The present invention further provides for the use of the compounds as anti-cancer agents; wherein: R1 is aryl, substituted aryl, heterocycle, substituted heterocycle, heteroaryl, substituted heteroaryl or amino; R2 and R3 are independently aryl, substituted aryl, heterocycle, heteroaryl, substituted heterocycle, or substituted heteroaryl or R2 and R3 when taken together along with the carbon atoms they are attached to, form aryl or substituted aryl, and R4 is hydrogen, halogen, hydroxyl, thiol, lower alkyl, substituted lower alkyl, lower alkenyl, substituted lower alkenyl, lower alkynyl, substituted lower alkynyl, alkylalkenyl, alkyl alkynyl, alkoxy, alkylthio, aryl, aryloxy, amino, amido, carboxyl, aryl, substituted aryl, heterocycle, heteroaryl, substituted heterocycle, heteroalkyl, cycloalkyl, substituted cycloalkyl, alkylcycloalkyl, alkylcycloheteroalkyl, nitro, cyano or —S(O)0-2R wherein R is alkyl, substituted alkyl, aryl, substituted aryl, heterocycle, heteroaryl, substituted heterocycle, or substituted heteroaryl.
摘要翻译：提供了治疗上有效的2,4,5-三取代的咪唑化合物。还提供了制备化合物和药物组合物的方法，其包含单独的化合物或与其它试剂组合。本发明还提供了化合物作为抗癌剂的用途; 其中：R1是芳基，取代的芳基，杂环，取代的杂环，杂芳基，取代的杂芳基或氨基; R2和R3独立地是芳基，取代的芳基，杂环，杂芳基，取代的杂环或取代的杂芳基，或者当R 2和R 3与它们连接的碳原子一起形成时，R 2和R 3，形成芳基或取代的芳基，且R 4是氢，卤素，羟基，硫醇，低级烷基，取代的低级烷基，低级烯基，取代的低级烯基，低级炔基，取代的低级炔基，烷基烯基，烷基炔基，烷氧基，烷硫基，芳基，芳氧基，氨基，酰胺基，羧基，芳基，取代的芳基，杂环，杂芳基，取代的杂环，杂烷基，环烷基，取代的环烷基，烷基环烷基，烷基环杂烷基，硝基，氰基或-S（O）0-2R，其中R是烷基，取代的烷基，芳基，取代的芳基，杂环，杂芳基，取代的杂环或取代的杂芳基。

3. 发明申请

US20100168417A1 2-Indolyl Imidazo [4,5-d] Phenanthroline Derivatives and Their Use in the Treatment for Cancer 有权
标题翻译： 2-吲哚咪唑并[4,5-d]菲咯啉衍生物及其在癌症治疗中的应用
公开(公告)号：US20100168417A1
公开(公告)日：2010-07-01
申请号：US11915257
申请日：2006-05-25
申请人： Mario Huesca , Aiping H. Young , Yoon Lee , Aye Aye Khine , Jim A. Wright , Lisa Lock , Raed Al-Qawasmeh
发明人： Mario Huesca , Aiping H. Young , Yoon Lee , Aye Aye Khine , Jim A. Wright , Lisa Lock , Raed Al-Qawasmeh
IPC分类号： C07D401/14 , C07D471/16 , C07D413/14
CPC分类号： C07D471/14
摘要： 2-indolyl imidazo[4,5-d]phenanthroline compounds of Formula I that are capable of intracellular chelation of transition metals and of exerting antiproliferative effects in cancer cells, that are cytostatic and/or cytotoxic, are provided. Compounds of Formula I can also induce apoptosis in cancer cells and are thus capable of exerting a cytotoxic effect on cancer cells. The compounds of Formula I are also capable of selectively inhibiting the proliferation of one or more of prostate cancer cells, colon cancer cells, non-small lung cancer cells and leukemia cells. The compounds of Formula I are also capable of increasing the expression of the zinc-regulated tumour suppressor, KLF4 and thus are useful in inhibiting the proliferation of cancer cells in which KLF4 functions as a tumour-suppressor, including, but not limited to, bladder cancer, cancers of the gastrointestinal tract and various leukemias.
摘要翻译：提供能够细胞内螯合过渡金属并且在细胞抑制和/或细胞毒性的癌细胞中发挥抗增殖作用的式I的2-吲哚基咪唑并[4,5-d]菲咯啉化合物。式I的化合物还可以诱导癌细胞凋亡，因此能够对癌细胞发挥细胞毒性作用。式I的化合物还能够选择性地抑制一种或多种前列腺癌细胞，结肠癌细胞，非小细胞肺癌细胞和白血病细胞的增殖。式I的化合物还能够增加锌调节的肿瘤抑制因子KLF4的表达，因此可用于抑制KLF4作为肿瘤抑制剂的癌细胞的增殖，包括但不限于膀胱癌症，胃肠道癌症和各种白血病。

4. 发明授权

US08148392B2 2-indolyl imidazo [4,5-d] phenanthroline derivatives and their use in the treatment of cancer 有权
标题翻译： 2-吲哚基咪唑并[4,5-d]菲咯啉衍生物及其在治疗癌症中的应用
公开(公告)号：US08148392B2
公开(公告)日：2012-04-03
申请号：US11915257
申请日：2006-05-25
申请人： Mario Huesca , Aiping H. Young , Yoon Lee , Aye Aye Khine , Jim A. Wright , Lisa Lock , Raed Al-Qawasmeh
发明人： Mario Huesca , Aiping H. Young , Yoon Lee , Aye Aye Khine , Jim A. Wright , Lisa Lock , Raed Al-Qawasmeh
IPC分类号： A61K31/4745 , C07D471/12
CPC分类号： C07D471/14
摘要： 2-indolyl imidazo[4,5-d]phenanthroline compounds of Formula (I) and methods of using same in the treatment of cancer, in particular, solid cancers and leukemia are provided. Pharmaceutical compositions comprising the compounds are also provided.
摘要翻译：提供式（I）的2-吲哚基咪唑并[4,5-d]菲咯啉化合物及其在治疗癌症中的用途，特别是固体癌症和白血病。还提供了包含该化合物的药物组合物。

5. 发明申请

US20110152337A1 2,4,5-TRISUBSTITUTED IMIDAZOLES AND THEIR USE AS ANTI-MICROBIAL AGENTS 有权
标题翻译： 2,4,5-三唑基咪唑及其作为抗微生物剂的用途
公开(公告)号：US20110152337A1
公开(公告)日：2011-06-23
申请号：US12976122
申请日：2010-12-22
申请人： RAED H. AL-QAWASMEH , AIPING H. YOUNG , MARIO HUESCA , YOON S. LEE
发明人： RAED H. AL-QAWASMEH , AIPING H. YOUNG , MARIO HUESCA , YOON S. LEE
IPC分类号： A61K31/4178 , C07D403/04 , A61P31/04 , A61P31/10
CPC分类号： A01N43/90 , A01N43/50 , A01N43/52 , A23L3/3544 , A61K31/4164 , A61K31/4178 , A61K31/4184 , A61K31/4188 , A61K31/4375 , A61K31/4439 , A61K31/444 , A61K31/454 , A61K45/06 , A61L2/18 , C07D233/22 , C07D233/64 , C07D235/02 , C07D401/14 , C07D403/04 , C07D403/14 , C07D409/14 , C07D471/14 , E05B1/0069
摘要： The present invention provides therapeutically effective 2,4,5-trisubstituted imidazole compounds, methods of preparing the same, and compositions comprising the compounds alone or in combination with other agents. The present invention further provides for the use of the compounds as anti-microbial agents. The anti-microbial properties of the compounds include anti-bacterial and/or anti-fungal activity.
摘要翻译：本发明提供治疗有效的2,4,5-三取代的咪唑化合物，其制备方法，以及包含单独或与其它试剂组合的化合物的组合物。本发明还提供了化合物作为抗微生物剂的用途。化合物的抗微生物性质包括抗细菌和/或抗真菌活性。

6. 发明授权

US07884120B2 2,4,5-trisubstituted imidazoles and their use as anti-microbial agents 有权
标题翻译： 2,4,5-三取代的咪唑及其作为抗微生物剂的用途
公开(公告)号：US07884120B2
公开(公告)日：2011-02-08
申请号：US10525690
申请日：2003-08-19
申请人： Raed Al-Qawasmeh , Aiping H. Young , Mario Huesca , Yoon Lee
发明人： Raed Al-Qawasmeh , Aiping H. Young , Mario Huesca , Yoon Lee
IPC分类号： C07D403/04 , A61K31/4184 , C07D401/14 , A61K31/435
CPC分类号： A01N43/90 , A01N43/50 , A01N43/52 , A23L3/3544 , A61K31/4164 , A61K31/4178 , A61K31/4184 , A61K31/4188 , A61K31/4375 , A61K31/4439 , A61K31/444 , A61K31/454 , A61K45/06 , A61L2/18 , C07D233/22 , C07D233/64 , C07D235/02 , C07D401/14 , C07D403/04 , C07D403/14 , C07D409/14 , C07D471/14 , E05B1/0069
摘要： The present invention provides therapeutically effective 2,4,5-trisubstituted imidazole compounds, methods of preparing the same, and compositions comprising the compounds alone or in combination with other agents. The present invention further provides for the use of the compounds as anti-microbial agents. The anti-microbial properties of the compounds include anti-bacterial and/or anti-fungal activity.
摘要翻译：本发明提供治疗有效的2,4,5-三取代的咪唑化合物，其制备方法，以及包含单独或与其它试剂组合的化合物的组合物。本发明还提供了化合物作为抗微生物剂的用途。化合物的抗微生物性质包括抗细菌和/或抗真菌活性。

7. 发明授权

US08394815B2 2,4,5-trisubstituted imidazoles and their use as anti-microbial agents 有权
公开(公告)号：US08394815B2
公开(公告)日：2013-03-12
申请号：US12976122
申请日：2010-12-22
申请人： Raed H. Al-Qawasmeh , Aiping H. Young , Mario Huesca , Yoon S. Lee
发明人： Raed H. Al-Qawasmeh , Aiping H. Young , Mario Huesca , Yoon S. Lee
IPC分类号： C07D471/12 , A61K31/435 , A61P31/04
CPC分类号： A01N43/90 , A01N43/50 , A01N43/52 , A23L3/3544 , A61K31/4164 , A61K31/4178 , A61K31/4184 , A61K31/4188 , A61K31/4375 , A61K31/4439 , A61K31/444 , A61K31/454 , A61K45/06 , A61L2/18 , C07D233/22 , C07D233/64 , C07D235/02 , C07D401/14 , C07D403/04 , C07D403/14 , C07D409/14 , C07D471/14 , E05B1/0069
摘要： The present invention provides therapeutically effective 2,4,5-trisubstituted imidazole compounds, methods of preparing the same, and compositions comprising the compounds alone or in combination with other agents. The present invention further provides for the use of the compounds as anti-microbial agents. The anti-microbial properties of the compounds include anti-bacterial and/or anti-fungal activity.

8. 发明申请

US20080262015A9 Aryl imidazoles and their use as anti-cancer agents 有权
标题翻译：芳基咪唑及其作为抗癌剂的用途
公开(公告)号：US20080262015A9
公开(公告)日：2008-10-23
申请号：US10579149
申请日：2004-11-15
申请人： Mario Huesca , Raed Al-Qawasmeh , Aiping Young , Yoon Lee
发明人： Mario Huesca , Raed Al-Qawasmeh , Aiping Young , Yoon Lee
IPC分类号： A61K31/4745 , A61K31/4188 , A61K31/4178
CPC分类号： A61K31/4184 , A61K31/4178 , A61K31/4188 , A61K31/4745 , C07D233/64 , C07D235/02 , C07D401/14 , C07D403/04 , C07D403/14 , C07D409/14 , C07D495/04
摘要： Therapeutically effective 2,4,5-trisubstituted imidazole compounds are provided. Also provided are methods -of preparing the compounds and pharmaceutical compositions comprising the compounds alone or in combination with other agents. The present invention further provides for the use of the compounds as anti-cancer agents; wherein: R1 is aryl, substituted aryl, heterocycle, substituted heterocycle, heteroaryl, substituted heteroaryl or amino; R2 and R3 are independently aryl, substituted aryl, heterocycle, heteroaryl, substituted heterocycle, or substituted heteroaryl or R2 and R3 when taken together along with the carbon atoms they are attached to, form aryl or substituted aryl, and R4 is hydrogen, halogen, hydroxyl, thiol, lower alkyl, substituted lower alkyl, lower alkenyl, substituted lower alkenyl, lower alkynyl, substituted lower alkynyl, alkylalkenyl, alkyl alkynyl, alkoxy, alkylthio, aryl, aryloxy, amino, amido, carboxyl, aryl, substituted aryl, heterocycle, heteroaryl, substituted heterocycle, heteroalkyl, cycloalkyl, substituted cycloalkyl, alkylcycloalkyl, alkylcycloheteroalkyl, nitro, cyano or —S(O)o.2R wherein R is alkyl, substituted alkyl, aryl, substituted aryl, heterocycle, heteroaryl, substituted heterocycle, or substituted heteroaryl.
摘要翻译：提供了治疗上有效的2,4,5-三取代的咪唑化合物。还提供了制备化合物和药物组合物的方法，所述药物组合物包含单独的化合物或与其它药剂组合。本发明还提供了化合物作为抗癌剂的用途; 其中：R1是芳基，取代的芳基，杂环，取代的杂环，杂芳基，取代的杂芳基或氨基; R2和R3独立地是芳基，取代的芳基，杂环，杂芳基，取代的杂环或取代的杂芳基，或者当R 2和R 3与它们连接的碳原子一起形成时，R 2和R 3，形成芳基或取代的芳基，且R 4是氢，卤素，羟基，硫醇，低级烷基，取代的低级烷基，低级烯基，取代的低级烯基，低级炔基，取代的低级炔基，烷基烯基，烷基炔基，烷氧基，烷硫基，芳基，芳氧基，氨基，酰胺基，羧基，芳基，取代的芳基，杂环，杂芳基，取代的杂环，杂烷基，环烷基，取代的环烷基，烷基环烷基，烷基环杂烷基，硝基，氰基或-S（O）o2R其中R是烷基，取代的烷基，芳基，取代的芳基，杂环，杂芳基，取代的杂环或取代的杂芳基。

9. 发明申请

US20070123553A1 Aryl imidazoles and their use as anti-cancer agents 有权
标题翻译：芳基咪唑及其作为抗癌剂的用途
公开(公告)号：US20070123553A1
公开(公告)日：2007-05-31
申请号：US10579149
申请日：2004-11-15
申请人： Mario Huesca , Raed Al-Qawasmeh , Aiping Young , Yoon Lee
发明人： Mario Huesca , Raed Al-Qawasmeh , Aiping Young , Yoon Lee
IPC分类号： A61K31/4745 , A61K31/4188 , A61K31/4178
CPC分类号： A61K31/4184 , A61K31/4178 , A61K31/4188 , A61K31/4745 , C07D233/64 , C07D235/02 , C07D401/14 , C07D403/04 , C07D403/14 , C07D409/14 , C07D495/04
摘要： Therapeutically effective 2,4,5-trisubstituted imidazole compounds are provided. Also provided are methods -of preparing the compounds and pharmaceutical compositions comprising the compounds alone or in combination with other agents. The present invention further provides for the use of the compounds as anti-cancer agents; wherein: R1 is aryl, substituted aryl, heterocycle, substituted heterocycle, heteroaryl, substituted heteroaryl or amino; R2 and R3 are independently aryl, substituted aryl, heterocycle, heteroaryl, substituted heterocycle, or substituted heteroaryl or R2 and R3 when taken together along with the carbon atoms they are attached to, form aryl or substituted aryl, and R4 is hydrogen, halogen, hydroxyl, thiol, lower alkyl, substituted lower alkyl, lower alkenyl, substituted lower alkenyl, lower alkynyl, substituted lower alkynyl, alkylalkenyl, alkyl alkynyl, alkoxy, alkylthio, aryl, aryloxy, amino, amido, carboxyl, aryl, substituted aryl, heterocycle, heteroaryl, substituted heterocycle, heteroalkyl, cycloalkyl, substituted cycloalkyl, alkylcycloalkyl, alkylcycloheteroalkyl, nitro, cyano or —S(O)o.2R wherein R is alkyl, substituted alkyl, aryl, substituted aryl, heterocycle, heteroaryl, substituted heterocycle, or substituted heteroaryl.
摘要翻译：提供了治疗上有效的2,4,5-三取代的咪唑化合物。还提供了制备化合物和药物组合物的方法，所述药物组合物包含单独的化合物或与其它药剂组合。本发明还提供了化合物作为抗癌剂的用途; 其中：R1是芳基，取代的芳基，杂环，取代的杂环，杂芳基，取代的杂芳基或氨基; R2和R3独立地是芳基，取代的芳基，杂环，杂芳基，取代的杂环或取代的杂芳基，或者当R 2和R 3与它们连接的碳原子一起形成时，R 2和R 3，形成芳基或取代的芳基，且R 4是氢，卤素，羟基，硫醇，低级烷基，取代的低级烷基，低级烯基，取代的低级烯基，低级炔基，取代的低级炔基，烷基烯基，烷基炔基，烷氧基，烷硫基，芳基，芳氧基，氨基，酰胺基，羧基，芳基，取代的芳基，杂环，杂芳基，取代的杂环，杂烷基，环烷基，取代的环烷基，烷基环烷基，烷基环杂烷基，硝基，氰基或-S（O）o2R其中R是烷基，取代的烷基，芳基，取代的芳基，杂环，杂芳基，取代的杂环或取代的杂芳基。

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