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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

US07259171B2 Di and trifluoro-triazolo-pyridines anti-inflammatory compounds 失效
标题翻译：二和三氟 - 三唑并 - 吡啶抗炎化合物
公开(公告)号：US07259171B2
公开(公告)日：2007-08-21
申请号：US10649236
申请日：2003-08-27
申请人： Mark A. Dombroski , Michael A. Letavic , Kim F. McClure
发明人： Mark A. Dombroski , Michael A. Letavic , Kim F. McClure
IPC分类号： A61K31/4745 , C07D471/02
CPC分类号： C07D471/04
摘要： The present invention relates to novel triazolo-pyridines of the formula I wherein R1 is fluoro;s is an integer from two to three;R2 is (C3-C6)cycloalkyl optionally substituted by one or two moieties independently selected from the group consisting of halo, (C1-C4)alkyl, hydroxy, (C1-C6)alkoxy and (C1-C6)alkyl-(C═O)—O—;or R2 is (C1-C6)alkyl optionally substituted by one or two moieties independently selected from the group consisting of halo, (C1-C6)alkyl, hydroxy, (C1-C6)alkoxy and (C1-C6)alkyl-(C═O)—O—;with the proviso that said compound of formula I cannot be6-[4-(2,4-Difluoro-phenyl)-oxazol-5-yl]-3-isopropyl-[1,2,4]triazolo[4,3-a]pyridine; or6-[4-(3,4-Difluoro-phenyl)-oxazol-5-yl]-3-isopropyl-[1,2,4]triazolo[4,3-a]pyridine;to intermediates for their preparation, to pharmaceutical compositions containing them and to their medicinal use. The compounds of the present invention are potent inhibitors of MAP kinases, preferably p38 kinase. They are useful in the treatment of inflammation, osteoarthritis, rheumatoid arthritis, cancer, repurfusion or ischemia in stroke or heart attack, autoimmune diseases and other disorders.
摘要翻译：本发明涉及式I的新的三唑并 - 吡啶，其中R 1是氟; s是从2到3的整数; R 2是任选被一个或两个独立地选自以下的部分取代的（C 1 -C 6 -C 6）环烷基：卤素，（C C 1 -C 4烷基，羟基，（C 1 -C 6 -C 6）烷氧基和（C

5. 发明授权

US06664395B2 Benzotriazoles anti-inflammatory compounds 失效
标题翻译：苯并三唑抗炎化合物
公开(公告)号：US06664395B2
公开(公告)日：2003-12-16
申请号：US10115952
申请日：2002-04-04
申请人： Michael A. Letavic , Mark A. Dombroski , Kim F. McClure , Ellen R. Laird
发明人： Michael A. Letavic , Mark A. Dombroski , Kim F. McClure , Ellen R. Laird
IPC分类号： C07D40304
CPC分类号： C07D401/14 , C07D403/04 , C07D403/14 , C07D413/04
摘要： The present invention relates to novel benzotriazoles of the formula I wherein Het is an optionally substituted 5-membered heterocycle containing one to two heteroatoms selected from nitrogen, sulfur and oxygen wherein at least one of said heteroatoms atoms must be nitrogen; R2 is selected from the group consisting of hydrogen, (C1-C6)alkyl or other suitable substituents; R3 is selected from the group consisting of hydrogen, (C1-C6)alkyl or other suitable substituents; s is an integer from 0-5; to intermediates for their preparation, to pharmaceutical compositions containing them and to their medicinal use. The compounds of the present invention are potent inhibitors of MAP kinases, preferably p38 kinase. They are useful in the treatment of inflammation, osteoarthritis, rheumatoid arthritis, cancer, repurfusion or ischemia in stroke or heart attack, autoimmune diseases and other disorders.
摘要翻译：本发明涉及式I的新型苯并三唑，其中Het是含有一至二个选自氮，硫和氧的杂原子的任选取代的五元杂环，其中至少一个所述杂原子必须是氮;选择R 2 由（C 1 -C 6）烷基或其它合适的取代基组成的组; R 3选自氢，（C 1 -C 6）烷基或其它合适的取代基; s为0-5的整数 ;用于制备的中间体，含有它们的药物组合物及其药物用途。本发明的化合物是MAP激酶的有效抑制剂，优选p38激酶。它们可用于治疗炎症，骨关节炎，类风湿性关节炎，癌症，中风或心脏病发作中的再灌注或缺血，自身免疫疾病和其他疾病。

6. 发明授权

US07005523B2 Cycloalkyl-[4-(trifluorophenyl)-oxazol-5yl]-triazolo-pyridines 失效
标题翻译：环烷基 - [4-（三氟苯基） - 恶唑-5-基] - 三唑并 - 吡啶
公开(公告)号：US07005523B2
公开(公告)日：2006-02-28
申请号：US10649216
申请日：2003-08-27
申请人： Mark A. Dombroski , Michael A. Letavic , Kim F. McClure
发明人： Mark A. Dombroski , Michael A. Letavic , Kim F. McClure
IPC分类号： C07D471/02 , A61K31/44
CPC分类号： C07D471/04
摘要： The present invention relates to novel cycloalkyl-[4-(trifluorophenyl)-oxazol-5-yl]-triazolo-pyridines, to intermediates for their preparation, to pharmaceutical compositions containing them and to their medicinal use. The compounds of the present invention are potent inhibitors of MAP kinases, preferably p38 kinase. They are useful in the treatment of inflammation, osteoarthritis, rheumatoid arthritis, cancer, reperfusion or ischemia in stroke or heart attack, autoimmune diseases and other disorders.
摘要翻译：本发明涉及新的环烷基 - [4-（三氟苯基） - 恶唑-5-基] - 三唑并 - 吡啶，其制备中间体，含有它们的药物组合物及其药物用途。本发明的化合物是MAP激酶的有效抑制剂，优选p38激酶。它们可用于治疗炎症，骨关节炎，类风湿性关节炎，癌症，中风或心脏病发作中的再灌注或缺血，自身免疫性疾病和其他疾病。

7. 发明授权

US06696464B2 Triazolo-pyridines anti-inflammatory compounds 失效
标题翻译：三唑并吡啶抗炎化合物
公开(公告)号：US06696464B2
公开(公告)日：2004-02-24
申请号：US10094760
申请日：2002-03-11
申请人： Kim F. McClure , Michael A. Letavic , Mark A. Dombroski , Allen J. Duplantier , Ellen R. Laird
发明人： Kim F. McClure , Michael A. Letavic , Mark A. Dombroski , Allen J. Duplantier , Ellen R. Laird
IPC分类号： A61K3144
CPC分类号： C07D471/04
摘要： The present invention relates to novel triazolo-pyridines of the formula I wherein Het is an optionally substituted 5-membered heterocycle containing one to two heteroatoms selected from nitrogen, sulfur and oxygen wherein at least one of said heteroatoms atoms must be nitrogen; R2 is selected from the group consisting of hydrogen, (C1-C6)alkyl or other suitable substituents; R3 is selected from the group consisting of hydrogen, (C1-C6)alkyl or other suitable substituents; s is an integer from 0-5; to intermediates for their preparation, to pharmaceutical compositions containing them and to their medicinal use. The compounds of the present invention are potent inhibitors of MAP kinases, preferably p38 kinase. They are useful in the treatment of inflammation, osteoarthritis, rheumatoid arthritis, cancer, repurfusion or ischemia in stroke or heart attack, autoimmune diseases and other disorders.
摘要翻译：本发明涉及式I的新型三唑并 - 吡啶，其中Het是含有一至二个选自氮，硫和氧的杂原子的任选取代的五元杂环，其中至少一个所述杂原子必须是氮; R 2，选自氢，（C 1 -C 6）烷基或其它合适的取代基; R 3选自氢，（C 1 -C 6）烷基或其它合适的取代基; s是0的整数 -5;用于制备的中间体，含有它们的药物组合物及其药物用途。本发明的化合物是MAP激酶的有效抑制剂，优选p38激酶。它们可用于治疗炎症，骨关节炎，类风湿性关节炎，癌症，中风或心脏病发作中的再灌注或缺血，自身免疫疾病和其他疾病。

8. 发明授权

US07037923B2 Alkyl-[4-(trifluorophenyl)-oxazol-5-yl]-triazolo-pyridines 失效
标题翻译：烷基 - [4-（三氟苯基） - 恶唑-5-基] - 三唑并 - 吡啶
公开(公告)号：US07037923B2
公开(公告)日：2006-05-02
申请号：US10649265
申请日：2003-08-27
申请人： Mark A. Dombroski , Michael A. Letavic , Kim F. McClure
发明人： Mark A. Dombroski , Michael A. Letavic , Kim F. McClure
IPC分类号： A61K31/44 , C07D471/02
CPC分类号： C07D471/04
摘要： The present invention relates to novel alkyl-[4-(trifluorophenyl)-oxazol-5-yl]-triazolo-pyridines, to intermediates and methods for their preparation, to pharmaceutical compositions containing them and to their medicinal use. The compounds of the present invention are potent inhibitors of MAP kinases, preferably p38 kinase. They are useful in the treatment of inflammation, osteoarthritis, rheumatoid arthritis, cancer, reperfusion or ischemia in stroke or heart attack, autoimmune diseases and other disorders.
摘要翻译：本发明涉及新的烷基 - [4-（三氟苯基） - 恶唑-5-基] - 三唑并 - 吡啶，其中间体及其制备方法，含有它们的药物组合物及其医药用途。本发明的化合物是MAP激酶的有效抑制剂，优选p38激酶。它们可用于治疗炎症，骨关节炎，类风湿性关节炎，癌症，中风或心脏病发作中的再灌注或缺血，自身免疫性疾病和其他疾病。

9. 发明授权

US07056918B2 Benzimidazole anti-inflammatory compounds 失效
标题翻译：苯并咪唑抗炎化合物
公开(公告)号：US07056918B2
公开(公告)日：2006-06-06
申请号：US10094717
申请日：2002-03-11
申请人： Mark A. Dombroski , Michael A. Letavic , Kim F. McClure
发明人： Mark A. Dombroski , Michael A. Letavic , Kim F. McClure
IPC分类号： A61K31/4184 , C07D403/04 , C07D403/14
CPC分类号： C07D401/14 , C07D403/04 , C07D403/14 , C07D405/14 , C07D409/14 , C07D413/04 , C07D487/04
摘要： The present invention relates to novel triazolo-pyridines of the formula I wherein Het is an optionally substituted 5-membered heterocycle containing one to two heteroatoms selected from nitrogen, sulfur and oxygen wherein at least one of said heteroatoms atoms must be nitrogen; R2 is selected from the group consisting of hydrogen, (C1–C6)alkyl or other suitable substituents; R3 is selected from the group consisting of hydrogen, (C1–C6)alkyl or other suitable substituents; s is an integer from 0–5; to intermediates for their preparation, to pharmaceutical compositions containing them and to their medicinal use. The compounds of the present invention are potent inhibitors of MAP kinases, preferably p38 kinase. They are useful in the treatment of inflammation, osteoarthritis, rheumatoid arthritis, cancer, repurfusion or ischemia in stroke or heart attack, autoimmune diseases and other disorders.
摘要翻译：本发明涉及式I的新型三唑并 - 吡啶，其中Het是含有一至二个选自氮，硫和氧的杂原子的任选取代的5元杂环，其中至少一个所述杂原子必须是氮; R 2选自氢，（C 1 -C 6 -C 6）烷基或其它合适的取代基; R 3选自氢，（C 1 -C 6 -C 6）烷基或其它合适的取代基; s是0-5的整数; 制备中间体，含有它们的药物组合物及其药物用途。本发明的化合物是MAP激酶的有效抑制剂，优选p38激酶。它们可用于治疗炎症，骨关节炎，类风湿性关节炎，癌症，中风或心脏病发作中的再灌注或缺血，自身免疫疾病和其他疾病。

10. 发明授权

US07012143B2 Cycloalkyl-[4-(difluorophenyl)-oxazol-5-yl]-triazolo-pyridines 失效
标题翻译：环烷基 - [4-（二氟苯基） - 恶唑-5-基] - 三唑并 - 吡啶
公开(公告)号：US07012143B2
公开(公告)日：2006-03-14
申请号：US10649255
申请日：2003-08-27
申请人： Mark A. Dombroski , Michael A. Letavic , Kim F. McClure
发明人： Mark A. Dombroski , Michael A. Letavic , Kim F. McClure
IPC分类号： C07D47/02 , A61K31/44
CPC分类号： C07D471/04
摘要： The present invention relates to novel cycloalkyl-[4-(difluorophenyl)-oxazol-5-yl]-triazolo-pyridines, to intermediates for their preparation, to pharmaceutical compositions containing them and to their medicinal use. The compounds of the present invention are potent inhibitors of MAP kinases, preferably p38 kinase. They are useful in the treatment of inflammation, osteoarthritis, rheumatoid arthritis, cancer, reperfusion or ischemia in stroke or heart attack, autoimmune diseases and other disorders.
摘要翻译：本发明涉及新的环烷基 - [4-（二氟苯基） - 恶唑-5-基] - 三唑并 - 吡啶，其制备中间体，含有它们的药物组合物及其医药用途。本发明的化合物是MAP激酶的有效抑制剂，优选p38激酶。它们可用于治疗炎症，骨关节炎，类风湿性关节炎，癌症，中风或心脏病发作中的再灌注或缺血，自身免疫性疾病和其他疾病。

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