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公开(公告)号:US5864033A
公开(公告)日:1999-01-26
申请号:US451236
申请日:1995-05-26
申请人: Clinton E. Browne , Bheemarao G. Ugarkar , Kevin M. Mullane , Harry E. Gruber , David A. Bullough , Mark D. Erion , Angelo Castellino
发明人: Clinton E. Browne , Bheemarao G. Ugarkar , Kevin M. Mullane , Harry E. Gruber , David A. Bullough , Mark D. Erion , Angelo Castellino
IPC分类号: A61K31/00 , C07D487/04 , C07D519/00 , C07H19/04 , C07H19/052 , C07H19/06 , C07H19/14 , C07H19/16
CPC分类号: A61K31/7064 , A61K31/00 , A61K31/7076 , C07D487/04 , C07H19/04 , C07H19/052 , C07H19/06 , C07H19/14 , C07H19/16
摘要: Novel compounds which selectively inhibit adenosine kinase and methods of preparing adenosine kinase inhibitors are provided. Also provided are methods of treating various conditions which may be ameliorated by increased local concentrations of adenosine using adenosine kinase inhibitors.
摘要翻译: 提供了选择性抑制腺苷激酶的新型化合物和制备腺苷激酶抑制剂的方法。 还提供了治疗各种病症的方法,其可以通过使用腺苷激酶抑制剂增加腺苷浓度来改善。
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公开(公告)号:US5646128A
公开(公告)日:1997-07-08
申请号:US349125
申请日:1994-12-01
申请人: Gary S. Firestein , Bheemarao G. Ugarkar , Leonard P. Miller , Harry E. Gruber , David A. Bullough , Mark D. Erion , Angelo J. Castellino , Clinton E. Browne
发明人: Gary S. Firestein , Bheemarao G. Ugarkar , Leonard P. Miller , Harry E. Gruber , David A. Bullough , Mark D. Erion , Angelo J. Castellino , Clinton E. Browne
IPC分类号: A61K31/00 , C07H19/04 , C07H19/052 , A61K31/70
CPC分类号: A61K31/7064 , A61K31/00 , A61K31/7076 , C07H19/04 , C07H19/052 , Y10S514/825 , Y10S514/885 , Y10S514/886
摘要: Novel compounds which selectively inhibit adenosine kinase and methods of preparing adenosine kinase inhibitors are provided. Also provided are methods of treating various inflammatory conditions, including arthritis and SIRS, which may be ameliorated by increased local concentrations of adenosine using adenosine kinase inhibitors.
摘要翻译: 提供了选择性抑制腺苷激酶的新型化合物和制备腺苷激酶抑制剂的方法。 还提供了治疗各种炎性病症(包括关节炎和SIRS)的方法,其可以通过使用腺苷激酶抑制剂增加腺苷浓度来改善。
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公开(公告)号:US5763597A
公开(公告)日:1998-06-09
申请号:US660506
申请日:1996-06-07
申请人: Bheemarao G. Ugarkar , Mark D. Erion , Jorge E. Gomez Galeno , Angelo J. Castellino , Clinton E. Browne
发明人: Bheemarao G. Ugarkar , Mark D. Erion , Jorge E. Gomez Galeno , Angelo J. Castellino , Clinton E. Browne
CPC分类号: C07H19/14
摘要: This invention relates to adenosine kinase inhibitors and to nucleoside analogs, specifically to orally active, substituted 5-aryl pyrrolo�2,3-d! pyrimidine and 3-aryl pyrazolo�3,4-d! pyrimidine nucleoside analogs having activity as adenosine kinase inhibitors. The invention also relates to the preparation and use of these and other adenosine kinase inhibitors in the treatment of cardiovascular and cerebrovascular diseases, inflammation and other diseases which can be regulated by increasing the local concentration of adenosine.
摘要翻译: 本发明涉及腺苷激酶抑制剂和核苷类似物,特别是具有作为腺苷激酶活性的口服活性的取代的5-芳基吡咯并[2,3-d]嘧啶和3-芳基吡唑并[3,4-d]嘧啶核苷类似物 抑制剂。 本发明还涉及这些和其它腺苷激酶抑制剂在治疗心血管和脑血管疾病,炎症等疾病中的制备和应用,可以通过增加腺苷的局部浓度来调节。
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公开(公告)号:US5721356A
公开(公告)日:1998-02-24
申请号:US473491
申请日:1995-06-07
申请人: Bheemarao G. Ugarkar , Mark D. Erion , Jorge E. Gomez Galeno , Angelo J. Castellino , Clinton E. Browne
发明人: Bheemarao G. Ugarkar , Mark D. Erion , Jorge E. Gomez Galeno , Angelo J. Castellino , Clinton E. Browne
IPC分类号: C12N9/99 , A61K31/00 , A61K31/70 , A61K31/7042 , A61K31/7052 , A61K31/7064 , A61P25/04 , A61P25/08 , A61P29/00 , A61P43/00 , C07D487/04 , C07D519/00 , C07H19/04 , C07H19/052 , C07H19/06 , C07H19/14 , C07H19/16 , C07H19/23
CPC分类号: C07H19/04 , A61K31/00 , A61K31/7064 , A61K31/7076 , C07D487/04 , C07H19/052 , C07H19/06 , C07H19/14 , C07H19/16
摘要: This invention relates to adenosine kinase inhibitors and to nucleoside analogs, specifically to orally active, substituted 5-aryl pyrrolo�2,3-d!pyrimidine and 3-aryl pyrazolo�3,4-d! pyrimidine nucleoside analogs having activity as adenosine kinase inhibitors. The invention also relates to the preparation and use of these and other adenosine kinase inhibitors in the treatment of cardiovascular and cerebrovascular diseases, inflammation and other diseases which can be regulated by increasing the local concentration of adenosine.
摘要翻译: 本发明涉及腺苷激酶抑制剂和核苷类似物,特别是具有作为腺苷激酶活性的口服活性的取代的5-芳基吡咯并[2,3-d]嘧啶和3-芳基吡唑并[3,4-d]嘧啶核苷类似物 抑制剂。 本发明还涉及这些和其它腺苷激酶抑制剂在治疗心血管和脑血管疾病,炎症等疾病中的制备和应用,可以通过增加腺苷的局部浓度来调节。
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公开(公告)号:US5506347A
公开(公告)日:1996-04-09
申请号:US191282
申请日:1994-02-03
IPC分类号: C07D473/40 , A61K31/505 , A61K31/52 , A61K31/70 , A61K31/7042 , A61K31/7052 , A61K31/7076 , A61P7/02 , A61P9/00 , A61P25/00 , A61P29/00 , A61P43/00 , C07D487/04 , C07H19/04 , C07H19/06 , C07H19/14 , C07H19/16 , C07G3/00
摘要: Novel lyxose derivatives which selectively inhibit adenosine kinase and methods of preparing these compounds are provided. These compounds are useful in treating certain conditions in vivo which may be ameliorated by increased local concentrations of adenosine.
摘要翻译: 提供了选择性抑制腺苷激酶的新型赖索糖衍生物和制备这些化合物的方法。 这些化合物可用于治疗体内某些条件,这可以通过增加局部腺苷浓度而改善。
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公开(公告)号:US07351399B2
公开(公告)日:2008-04-01
申请号:US11145194
申请日:2005-06-03
CPC分类号: C07H19/10 , A61K31/7056 , A61K31/7072 , A61K31/7076 , C07F9/657154 , C07F9/657181 , C07F9/65742 , C07F9/65744 , C07H19/20 , C07H19/207 , Y02A50/411
摘要: Prodrugs of formula I, their uses, their intermediates, and their method of manufacture are described: and pharmaceutically acceptable prodrugs and salts thereof.
摘要翻译: 描述了式I的前药,其用途,其中间体及其制备方法及其药学上可接受的前药和盐。
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公开(公告)号:US5763596A
公开(公告)日:1998-06-09
申请号:US660505
申请日:1996-06-07
IPC分类号: C07H19/044
CPC分类号: C07H19/044
摘要: This invention relates to adenosine kinase inhibitors and to nucleoside analogs, C-4' modified pyrrolo�2,3-d!pyrimidine and pyrazolo�3,4-d!pyrimidine nucleoside analogs having activity as adenosine kinase inhibitors. The invention relates to nucleoside analogs of this kind, having zero substitutions or two substitutions at the C-4' position of the furanose (sugar) moiety. The invention also relates to the preparation and use of these adenosine kinase inhibitors in the treatment of cardiovascular, and cerebrovascular diseases, inflammation and other diseases which can be regulated by increasing the local concentration of adenosine.
摘要翻译: 本发明涉及具有作为腺苷激酶抑制剂活性的腺苷激酶抑制剂和核苷类似物C-4'修饰的吡咯并[2,3-d]嘧啶和吡唑并[3,4-d]嘧啶核苷类似物。 本发明涉及这样的核苷类似物,其在呋喃糖(糖)部分的C-4'位置具有零取代或两个取代。 本发明还涉及这些腺苷激酶抑制剂在治疗心血管和脑血管疾病,炎症等疾病中的制备和应用,可以通过增加腺苷的局部浓度来调节。
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公开(公告)号:US5726302A
公开(公告)日:1998-03-10
申请号:US473492
申请日:1995-06-07
IPC分类号: A61K31/00 , A61K31/70 , A61K31/7042 , A61K31/7052 , A61K31/7064 , A61P25/04 , A61P25/08 , A61P29/00 , A61P43/00 , C07D487/04 , C07D519/00 , C07H19/04 , C07H19/052 , C07H19/06 , C07H19/14 , C07H19/16 , C07H19/23
CPC分类号: C07H19/04 , A61K31/00 , A61K31/7064 , A61K31/7076 , C07D487/04 , C07H19/052 , C07H19/06 , C07H19/14 , C07H19/16
摘要: This invention relates to adenosine kinase inhibitors and to nucleoside analogs, specifically to water soluble, aryl substituted 4-amino pyrrolo�2,3-d! pyrimidine and pyrazolo�3,4-d! pyrimidine nucleoside analogs having activity as adenosine kinase inhibitors. The invention also relates to the preparation and use of these adenosine kinase inhibitors in the treatment of cardiovascular, and cerebrovascular diseases, inflammation and other diseases which can be regulated by increasing the local concentration of adenosine.
摘要翻译: 本发明涉及腺苷激酶抑制剂和核苷类似物,具体涉及具有作为腺苷激酶抑制剂活性的水溶性芳基取代的4-氨基吡咯并[2,3-d]嘧啶和吡唑并[3,4-d]嘧啶核苷类似物。 本发明还涉及这些腺苷激酶抑制剂在治疗心血管和脑血管疾病,炎症等疾病中的制备和应用,可以通过增加腺苷的局部浓度来调节。
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公开(公告)号:US06946115B2
公开(公告)日:2005-09-20
申请号:US09978454
申请日:2001-10-15
IPC分类号: A61K31/7056 , A61K31/7072 , A61K31/7076 , C07F9/6571 , C07F9/6574 , C07H19/10 , C07H19/20 , C07H19/207 , A61K51/00 , A61M36/14
CPC分类号: C07H19/10 , A61K31/7056 , A61K31/7072 , A61K31/7076 , C07F9/657154 , C07F9/657181 , C07F9/65742 , C07F9/65744 , C07H19/20 , C07H19/207 , Y02A50/411
摘要: Prodrugs of formula I, their uses, their intermediates, and their method of manufacturing are described: and pharmaceutically acceptable prodrugs and salts thereof.
摘要翻译: 描述了式I的前药,其用途,其中间体及其制备方法及其药学上可接受的前药和盐。
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公开(公告)号:US06312662B1
公开(公告)日:2001-11-06
申请号:US09392352
申请日:1999-09-08
IPC分类号: A61K4900
CPC分类号: C07H19/10 , A61K31/7056 , A61K31/7072 , A61K31/7076 , C07F9/657154 , C07F9/657181 , C07F9/65742 , C07F9/65744 , C07H19/20 , C07H19/207 , Y02A50/411
摘要: Prodrugs of formula I, their uses, their intermediates, and their method of manufacture are described:
摘要翻译: 描述了式I的前药,其用途及其中间体及其制备方法:
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