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1. 发明授权

US07030242B2 Selective inhibition of aggrecanase in osteoarthritis treatment 失效
公开(公告)号：US07030242B2
公开(公告)日：2006-04-18
申请号：US11120376
申请日：2005-05-03
申请人： Mark C. Noe , Michael A. Letavic , Louis S. Chupak , Kim F. McClure
发明人： Mark C. Noe , Michael A. Letavic , Louis S. Chupak , Kim F. McClure
IPC分类号： C07D295/26 , A61K31/495
CPC分类号： C07D241/04 , C07D211/96 , C07D241/08
摘要： This invention relates to a method of treatment for osteoarthritis involving inhibitors of aggrecanase that demonstrate IC50s of less than 20 nM and demonstrate differential potency against matrix metalloproteinases (MMPs) and a disintegrin and metalloproteinases (ADAMs or reprolysins). This invention also relates to compounds, methods of treatment and composition of Formula I: or a therapeutically acceptable salt thereof, wherein X is carbon or nitrogen; R1 and R2 are independently selected from the group consisting of hydrogen, hydroxy, and methyl, wherein at least one of R1 and R2 is methyl; R3 and R4 are independently selected from the group consisting of hydrogen, hydroxy, and methyl, or R3 and R4 may be taken together to form a carbonyl group; and R5 and R6 are independent substituents in the ortho, meta, or para positions and are independently selected from the group consisting of hydrogen, halogen, cyano, methyl, and ethyl; with the provisos: when X is carbon, then R7 and R8 are both hydrogen and at least one of R1, R2, R3, and R4 is hydroxy; when X is carbon and R5 is para-halo, then at least one of R6, R3, and R4 is not hydrogen; when X is nitrogen, then R8 is not present and R7 is hydrogen or a group of the formula: wherein, Y is —CH2—NH2 or —NH—CH3; and when X is nitrogen and R7 is H, then R3 and R4 are taken together to form a carbonyl group.

2. 发明授权

US06599890B1 Arylsulfonyl hydroxamic acid derivatives 失效
标题翻译：芳基磺酰基异羟肟酸衍生物
公开(公告)号：US06599890B1
公开(公告)日：2003-07-29
申请号：US09708328
申请日：2000-11-08
申请人： Kim F. McClure , Mark C. Noe , Michael A. Letavic , Louis S. Chupak
发明人： Kim F. McClure , Mark C. Noe , Michael A. Letavic , Louis S. Chupak
IPC分类号： C07D21162
CPC分类号： C07D265/30 , C07D211/96 , C07D279/12
摘要： A compound of the formula wherein R1, R2 R3, R4 R5, R6, R7, R8, R9 and Q are as defined above, useful in the treatment of a condition selected from the group consisting of arthritis, cancer, tissue ulceration, macular degeneration, restenosis, periodontal disease, epidermolysis bullosa, scleritis, and other diseases characterized by matrix metalloproteinase activity, AIDS, sepsis, septic shock and other diseases involving the production of TNF. In addition, the compounds of the present invention may be used in combination therapy with standard non-steroidal anti-inflammatory drugs (NSAID'S) and analgesics, and in combination with cytotoxic drugs such as adriamycin, daunomycin, cis-platinum, etoposide, taxol, taxotere and other alkaloids, such as vincristine, in the treatment of cancer.
摘要翻译：式R 1，R 2，R 3，R 4，R 5，R 6，R 7，R 8，R 9和Q的化合物如上所定义，可用于治疗选自以下的病症：关节炎，癌症，组织溃疡，黄斑变性，再狭窄，牙周病，大疱性表皮松解症，巩膜炎等特征为基质金属蛋白酶活性，艾滋病，败血症，败血性休克等涉及TNF产生的疾病的疾病。此外，本发明的化合物可以与标准的非甾体抗炎药（NSAID'S）和止痛剂组合使用，并与细胞毒性药物如阿霉素，道诺霉素，顺铂，依托泊苷，紫杉醇，泰索帝等生物碱，如长春新碱，用于治疗癌症。

3. 发明授权

US06329397B1 Hydroxy pipecolate hydroxamic acid derivatives 失效
标题翻译：羟基哌啶酸异羟肟酸衍生物
公开(公告)号：US06329397B1
公开(公告)日：2001-12-11
申请号：US09372946
申请日：1999-08-12
申请人： Kim F. McClure , Mark C. Noe , Michael A. Letavic , Louis S. Chupak
发明人： Kim F. McClure , Mark C. Noe , Michael A. Letavic , Louis S. Chupak
IPC分类号： A61K31445
CPC分类号： C07D401/12 , C07D211/96 , C07D405/12 , C07D409/12 , C07D413/12
摘要： A compound of the formula wherein R1, R2 R3, R4 R5, R6, R7, R8, R9 and Ar are as defined above, useful in the treatment of a condition selected from the group consisting of arthritis, cancer, and other diseases characterized by matrix metalloproteinase or mammalian reprolysin activity. In addition, the compounds of the present invention may be used in combination therapy with standard non-steroidal anti-inflammatory drugs (NSAID'S), COX-2 inhibitors and analgesics, and in combination with cytotoxic drugs such as adriamycin, daunomycin, cis-platinum, etoposide, taxol, taxotere and other alkaloids, such as vincristine, in the treatment of cancer.
摘要翻译：式R 1，R 2，R 3，R 4，R 5，R 6，R 7，R 8，R 9和Ar的化合物如上所定义，可用于治疗选自以下的病症：关节炎，癌症和其它以基质为特征的疾病金属蛋白酶或哺乳动物生殖毒素活性。此外，本发明的化合物可以与标准非甾体抗炎药（NSAID'S），COX-2抑制剂和镇痛药组合使用，并与细胞毒性药物如阿霉素，道诺霉素，顺式铂，依托泊苷，紫杉醇，泰索帝等生物碱，如长春新碱，用于治疗癌症。

4. 发明授权

US07462600B2 Macrolides 失效
标题翻译：大环内酯类
公开(公告)号：US07462600B2
公开(公告)日：2008-12-09
申请号：US11313523
申请日：2005-12-21
申请人： Louis S. Chupak , Mark E. Flanagan , Takushi Kaneko , Thomas V. Magee , Mark C. Noe , Usa Reilly
发明人： Louis S. Chupak , Mark E. Flanagan , Takushi Kaneko , Thomas V. Magee , Mark C. Noe , Usa Reilly
IPC分类号： A61K31/70 , C07H17/08
CPC分类号： C07H17/08
摘要： Macrolide compounds per se, as shown below and defined herein, and their use, e.g., as antibacterial and antiprotozoal agents in animals, including humans: Also disclosed are methods of preparing the compounds, intermediates, and pharmaceutical compositions thereof, and methods of treating or preventing disease by administering the compounds to subjects in need. This abstract is only an excerpt and is not limiting of the invention.
摘要翻译：大环内酯类化合物本身，如下文所示和定义，以及它们在动物（包括人）中作为抗细菌剂和抗原虫药的用途：还公开了制备化合物，中间体及其药物组合物的方法，以及治疗或通过将化合物给予需要的受试者来预防疾病。该摘要仅是摘录而不是本发明的限制。

5. 发明授权

US06916807B2 Triaryl-oxy-aryl-spiro-pyrimidine-2,4,6-trione metalloproteinase inhibitors 失效
标题翻译：三芳基氧基 - 芳基 - 螺 - 嘧啶-2,4,6-三酮金属蛋白酶抑制剂
公开(公告)号：US06916807B2
公开(公告)日：2005-07-12
申请号：US10423671
申请日：2003-04-25
申请人： Kevin D. Freeman-Cook , Mark C. Noe
发明人： Kevin D. Freeman-Cook , Mark C. Noe
IPC分类号： A61K31/527 , A61P1/00 , A61P1/16 , A61P3/00 , A61P9/00 , A61P11/00 , A61P13/12 , A61P15/00 , A61P17/00 , A61P19/02 , A61P25/00 , A61P27/02 , A61P29/00 , A61P31/00 , A61P35/00 , A61P37/00 , A61P37/02 , A61P37/08 , C07D487/10 , A61K31/547
CPC分类号： C07D487/10
摘要： The present invention relates to triaryl-oxy-aryl-spiro-pyrimidine-2,4,6-trione metalloproteinase inhibitors of the formula wherein said ring X is a 5-7 membered heterocyclic ring, and wherein A, Y, B, G, and W are as defined in the specification; and to pharmaceutical compositions and methods of treating inflammation, cancer and other disorders.
摘要翻译：本发明涉及下式的三芳基 - 氧 - 芳基 - 螺 - 嘧啶-2,4,6-三酮金属蛋白酶抑制剂，其中所述环X为5-7元杂环，其中A，Y，B，G，和W如说明书中所定义; 以及治疗炎症，癌症和其他疾病的药物组合物和方法。

6. 发明授权

US06900201B2 N-substituted-heteroaryloxy-aryl-spiro-pyrimidine-2,4,6-trione metalloproteinase inhibitors 失效
标题翻译： N-取代 - 杂芳氧基 - 芳基 - 螺 - 嘧啶-2,4,6-三酮金属蛋白酶抑制剂
公开(公告)号：US06900201B2
公开(公告)日：2005-05-31
申请号：US10423779
申请日：2003-04-25
申请人： Mark C. Noe , Kevin Freeman-Cook
发明人： Mark C. Noe , Kevin Freeman-Cook
IPC分类号： A61K31/527 , A61P1/16 , A61P3/00 , A61P9/00 , A61P11/00 , A61P13/12 , A61P17/00 , A61P19/02 , A61P25/02 , A61P27/02 , A61P29/00 , A61P31/00 , A61P35/00 , A61P37/00 , A61P37/08 , A61P43/00 , C07D487/10
CPC分类号： C07D487/10
摘要： The present invention relates to N-substituted-heteroaryloxy-aryl-spiro-pyrimidine-2,4,6-trione metalloproteinase inhibitors of the formula wherein ring X is a 5-7 membered heterocyclic ring, and wherein A, Y, B, and G are as defined in the specification; and to pharmaceutical compositions and methods of treating inflammation, cancer and other disorders.
摘要翻译：本发明涉及下式的N-取代杂芳氧基 - 芳基 - 螺 - 嘧啶-2,4,6-三酮金属蛋白酶抑制剂，其中环X是5-7元杂环，其中A，Y，B和 G如规范中所定义; 以及治疗炎症，癌症和其他疾病的药物组合物和方法。

7. 发明授权

US06841671B2 Spiro-pyrimidine-2,4,6-trione metalloproteinase inhibitors 失效
标题翻译：螺 - 嘧啶-2,4,6-三酮金属蛋白酶抑制剂
公开(公告)号：US06841671B2
公开(公告)日：2005-01-11
申请号：US10047592
申请日：2001-10-23
申请人： Mark C. Noe , Martin J. Wythes , Brian S. Bronk
发明人： Mark C. Noe , Martin J. Wythes , Brian S. Bronk
IPC分类号： C07D471/10 , C07D487/10
CPC分类号： C07D471/10 , C07D487/10
摘要： The present invention relates to 5-spiro-pyrimidine-2,4,6-trione metalloproteinase inhibitors of the formula wherein said “A” is a 5-7 membered heterocyclic ring as defined in the specification and to pharmaceutical compositions and methods of treating inflammation, cancer and other disorders.
摘要翻译：本发明涉及式Ⅳ所示的5-螺 - 嘧啶-2,4,6-三酮金属蛋白酶抑制剂，所述“A”是本说明书中定义的5-7元杂环，以及治疗炎症的药物组合物和方法，癌症等疾病。

8. 发明授权

US06548526B2 Isothiazole derivatives useful as anticancer agents 有权
标题翻译：异噻唑衍生物可用作抗癌剂
公开(公告)号：US06548526B2
公开(公告)日：2003-04-15
申请号：US09803296
申请日：2001-03-09
申请人： Eric R. Larson , Mark C. Noe , Thomas G. Gant
发明人： Eric R. Larson , Mark C. Noe , Thomas G. Gant
IPC分类号： A61K31426
CPC分类号： C07D275/03 , C07C33/46 , C07C327/58 , C07D231/12 , C07D233/56 , C07D249/08 , C07D417/12 , C07D487/08
摘要： The present invention relates to compounds of the formula 1 and to pharmaceutically acceptable salts, prodrugs and solvates thereof, wherein X1, R1, R2 and R3 are as defined herein. The invention also relates to pharmaceutical compositions containing the above compounds and to methods treating hyperproliferative disorders in mammals by administering the above compounds.
摘要翻译：本发明涉及式1的化合物及其药学上可接受的盐，前药和溶剂合物，其中X1，R1，R2和R3如本文所定义。本发明还涉及含有上述化合物的药物组合物和通过施用上述化合物治疗哺乳动物过度增殖性疾病的方法。

9. 发明授权

US06919332B2 N-substituted-heteroaryloxy-aryloxy-pyrimidine-2,4,6-trione metalloproteinase inhibitors 失效
标题翻译： N-取代 - 杂芳氧基 - 芳氧基 - 嘧啶-2,4,6-三酮金属蛋白酶抑制剂
公开(公告)号：US06919332B2
公开(公告)日：2005-07-19
申请号：US10424382
申请日：2003-04-28
申请人： Mark C. Noe , Lilli Ann Wolf-Gouveia
发明人： Mark C. Noe , Lilli Ann Wolf-Gouveia
IPC分类号： A61K31/513 , A61P1/00 , A61P1/16 , A61P3/00 , A61P9/00 , A61P11/00 , A61P13/12 , A61P15/00 , A61P17/00 , A61P25/00 , A61P27/02 , A61P29/00 , A61P31/00 , A61P35/00 , A61P37/02 , A61P37/08 , C07D401/14 , C07D403/12 , C07D403/14 , A61K31/515
CPC分类号： C07D401/14 , C07D403/12 , C07D403/14
摘要： The present invention relates to N-substituted-heteroaryloxy-aryloxy-2,4,6-trione metalloproteinase inhibitors of the formula wherein X, A, Y, B, G, and R1 are as defined in the specification, and to pharmaceutical compositions and methods of treating inflammation, cancer and other disorders.
摘要翻译：本发明涉及下式的N-取代 - 杂芳氧基 - 芳氧基-2,4,6-三酮金属蛋白酶抑制剂，其中X，A，Y，B，G和R 1如说明书，以及治疗炎症，癌症和其它疾病的药物组合物和方法。

10. 发明授权

US06608104B2 Gem substituted hydroxamic acids 失效
标题翻译： Gem取代的异羟肟酸
公开(公告)号：US06608104B2
公开(公告)日：2003-08-19
申请号：US09818056
申请日：2001-03-27
申请人： Mark C. Noe
发明人： Mark C. Noe
IPC分类号： A61K3135
CPC分类号： C07D309/10
摘要： A compound of the formula wherein R1-R13, X, Z and Q are as defined above, useful in the treatment of arthritis, cancer, and other diseases involving the dysregulated production/release of reprolysins such as Aggrecanase and other diseases characterized by matrix metalloproteinase activity. In addition, the compounds of the present invention may be used in combination therapy with standard non-steroidal anti-inflammatory drugs (NSAID's), COX-2 inhibitors and analgesics, and in combination with cytotoxic drugs such as adriamycin, daunomycin, cis-platinum, etoposide, taxol, taxotere and other alkaloids, such as vincristine, in the treatment of cancer.
摘要翻译： R1-R13，X，Z和Q的化合物如上所定义，可用于治疗关节炎，癌症以及涉及生殖细胞失调产生/释放的其他疾病，例如聚集蛋白聚糖酶和其他以基质金属蛋白酶活性为特征的疾病。此外，本发明的化合物可以与标准非甾体抗炎药（NSAID），COX-2抑制剂和镇痛药组合使用，并与细胞毒性药物如阿霉素，道诺霉素，顺式铂，依托泊苷，紫杉醇，泰索帝等生物碱，如长春新碱，用于治疗癌症。

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