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1. 发明授权

US5521156A Cyclic neurokinin A antagonists 失效
标题翻译：循环神经激肽A拮抗剂
公开(公告)号：US5521156A
公开(公告)日：1996-05-28
申请号：US191571
申请日：1994-02-03
申请人： Thomas J. Owen , Elizabeth M. Kudlacz , Scott L. Harbeson , Stephen H. Buck
发明人： Thomas J. Owen , Elizabeth M. Kudlacz , Scott L. Harbeson , Stephen H. Buck
IPC分类号： A61K38/00 , A61K38/55 , A61P11/00 , A61P11/06 , A61P25/04 , A61P29/00 , A61P43/00 , C07K7/22 , C07K7/64 , A61K38/12
CPC分类号： C07K7/22 , A61K38/00 , Y10S930/27
摘要： Antagonists of neurokinin A which are novel cyclic hexapeptide and octapeptide compounds are described. The antagonism is confirmed using conventional competitive binding and biochemical assays as well as conventional physiological tests and the use of these derivatives in a variety of conditions in which neurokinin A is implicated is also described.
摘要翻译：描述了新型环状六肽和八肽化合物的神经激肽A的拮抗剂。使用常规竞争性结合和生物化学测定以及常规生理测试证实拮抗作用，并且还描述了在涉及神经激肽A的各种情况下使用这些衍生物。

2. 发明授权

US5830863A Neurokinin A antagonists 失效
标题翻译：神经激肽A拮抗剂
公开(公告)号：US5830863A
公开(公告)日：1998-11-03
申请号：US764157
申请日：1996-12-13
申请人： Stephen H. Buck , Scott L. Harbeson , John L. Krstenansky , Chester F. Hassman, III , James R. McCarthy
发明人： Stephen H. Buck , Scott L. Harbeson , John L. Krstenansky , Chester F. Hassman, III , James R. McCarthy
IPC分类号： A61K38/00 , C07K5/02 , C07K7/22
CPC分类号： C07K7/22 , C07K5/0207 , C07K5/0212 , A61K38/00 , Y10S514/826
摘要： Antagonists of neurokinin A which are derivatives of naturally occurring neurokinin A in which the amide bond connecting the two amino acids on the carboxy terminal end is modified are described. The antagonism is confirmed using conventional competitive binding and biochemical assays as well as conventional physiological tests and the use of these derivatives in a variety of conditions in which neurokinin A is implicated is also described.
摘要翻译：描述了神经激肽A的拮抗剂，其是连接羧基末端上的两个氨基酸的酰胺键被修饰的天然存在的神经激肽A的衍生物。使用常规竞争性结合和生物化学测定以及常规生理测试证实拮抗作用，并且还描述了在涉及神经激肽A的各种情况下使用这些衍生物。

3. 发明授权

US5731286A Cyclic neurokinin A antagonists 失效
标题翻译：循环神经激肽A拮抗剂
公开(公告)号：US5731286A
公开(公告)日：1998-03-24
申请号：US811913
申请日：1997-03-05
申请人： Scott L. Harbeson , Stephen H. Buck
发明人： Scott L. Harbeson , Stephen H. Buck
IPC分类号： A61K38/00 , A61K38/04 , A61P1/12 , A61P9/12 , A61P11/00 , A61P11/08 , A61P13/02 , A61P15/00 , A61P17/00 , A61P25/00 , A61P25/04 , A61P29/00 , A61P31/12 , A61P35/00 , A61P37/06 , A61P37/08 , A61P43/00 , C07K1/113 , C07K5/02 , C07K5/10 , C07K7/06 , C07K7/22 , C07K7/64 , A61K38/12 , C07K5/00 , C07K7/00
CPC分类号： C07K7/22 , A61K38/00
摘要： Antagonists of neurokinin A which are derivatives of naturally occurring neurokinin A in which the amide bond connecting the two amino acids on the carboxy terminal end is modified are described. The antagonism is confirmed using conventional competitive binding and biochemical assays as well as conventional physiological tests and the use of these derivatives in a variety of conditions in which neurokinin A is implicated is also described.
摘要翻译：描述了神经激肽A的拮抗剂，其是连接羧基末端上的两个氨基酸的酰胺键被修饰的天然存在的神经激肽A的衍生物。使用常规竞争性结合和生物化学测定以及常规生理测试证实拮抗作用，并且还描述了在涉及神经激肽A的各种情况下使用这些衍生物。

4. 发明授权

US08889687B2 Deuterated pyrazinoisoquinoline compounds 有权
标题翻译：氘化吡嗪异喹啉化合物
公开(公告)号：US08889687B2
公开(公告)日：2014-11-18
申请号：US13411198
申请日：2012-03-02
申请人： Julie F. Liu , Roger Tung , Scott L. Harbeson
发明人： Julie F. Liu , Roger Tung , Scott L. Harbeson
IPC分类号： A61K31/4985 , C07D471/04 , C07B59/00
CPC分类号： C07D471/04 , A61K31/4184 , A61K31/4985 , C07B59/002 , Y02A50/411 , Y02A50/423
摘要： This invention in one embodiment is directed to a compound of Formula Ia; where the designation (R) indicates that the designated carbon has the (R) stereochemistry; and wherein Z1 is hydrogen or fluorine; Z2 is hydrogen, deuterium, or fluorine; Z3 is deuterium; Z4 is fluorine; m is an integer from 0 to 10; n is an integer from 0 to 2; provided that: the sum of m+n does not exceed 10; and when both Z1 and Z2 are hydrogen, the sum of m+n is greater than 0, and pharmaceutically acceptable salts thereof. This invention also provides compositions comprising one or more compounds of this invention and a carrier and the use of the disclosed compounds and compositions in methods of treating diseases and conditions that are beneficially treated by administering an antihelminthic agent, such as praziquantel.
摘要翻译：本发明在一个实施方案中涉及式Ia化合物; 其中指定（R）表示指定的碳具有（R）立体化学; 并且其中Z1是氢或氟; Z2是氢，氘或氟; Z3是氘; Z4是氟; m为0〜10的整数; n为0〜2的整数; 条件是：m + n的和不超过10; 并且当Z1和Z2均为氢时，m + n的和大于0，以及其药学上可接受的盐。本发明还提供包含一种或多种本发明化合物和载体的组合物，以及所述化合物和组合物在治疗通过施用抗栓剂如吡喹酮有益治疗的疾病和病症的方法中的用途。

5. 发明授权

US08563554B2 Deuterated pyrazinoisoquinoline compounds 有权
标题翻译：氘化吡嗪异喹啉化合物
公开(公告)号：US08563554B2
公开(公告)日：2013-10-22
申请号：US13256787
申请日：2010-03-16
申请人： Julie F. Liu , Scott L. Harbeson , Roger Tung
发明人： Julie F. Liu , Scott L. Harbeson , Roger Tung
IPC分类号： A61K31/495
CPC分类号： C07D471/04 , A61K31/4184 , A61K31/4985 , A61K45/06 , Y02A50/411 , Y02A50/423 , A61K2300/00
摘要： This invention relates to novel compounds that are pyrazinoisoquinoline derivatives, and pharmaceutically acceptable salts thereof. More specifically, this invention relates to novel pyrazinoisoquinoline derivatives that are derivatives of praziquantel, such as compounds of formula (I): or pharmaceutically acceptable salts thereof. This invention also provides compositions comprising one or more compounds of this invention and a carrier and the use of the disclosed compounds and compositions in methods of treating diseases and conditions that are beneficially treated by administering an antihelminthic agent, such as praziquantel.
摘要翻译：本发明涉及吡嗪并异喹啉衍生物的新化合物及其药学上可接受的盐。更具体地，本发明涉及作为吡喹酮的衍生物的新的吡嗪并喹啉衍生物，例如式（I）的化合物或其药学上可接受的盐。本发明还提供包含一种或多种本发明化合物和载体的组合物，以及所述化合物和组合物在治疗通过施用抗栓剂如吡喹酮有益治疗的疾病和病症的方法中的用途。

6. 发明授权

US08557815B2 Substituted triazolophthalazine derivatives 有权
标题翻译：取代的三唑并恶嗪衍生物
公开(公告)号：US08557815B2
公开(公告)日：2013-10-15
申请号：US12856360
申请日：2010-08-13
申请人： Scott L. Harbeson
发明人： Scott L. Harbeson
IPC分类号： A61K31/5025 , C07D487/04
CPC分类号： A61K45/06 , A61K31/5025 , A61K31/535 , C07B59/002 , C07D487/04
摘要： This invention relates to novel substituted triazolophthalazines and pharmaceutically acceptable salts thereof. This invention also provides compositions comprising a compound of this invention and the use of such compositions in methods of treating diseases and conditions that are beneficially treated by administering selective α5 receptor partial or full inverse agonists.
摘要翻译：本发明涉及新的取代的三氮杂印hthal嗪及其药学上可接受的盐。本发明还提供了包含本发明化合物的组合物和这些组合物在治疗通过施用选择性α5受体部分或完全反向激动剂有益治疗的疾病和病症的方法中的用途。

7. 发明授权

US08354557B2 Synthesis of deuterated morpholine derivatives 有权
标题翻译：氘代吗啉衍生物的合成
公开(公告)号：US08354557B2
公开(公告)日：2013-01-15
申请号：US12456507
申请日：2009-06-17
申请人： Julie F. Liu , Xuejun Tang , Scott L. Harbeson , Craig E. Masse
发明人： Julie F. Liu , Xuejun Tang , Scott L. Harbeson , Craig E. Masse
IPC分类号： C07C215/68
CPC分类号： C07D413/10 , A61K31/5377 , A61K45/06 , C07B2200/05 , C07C215/12 , C07D263/06 , C07D295/02 , C07D295/033 , C07D295/06 , C07D295/12 , C07D295/135 , C07D413/14
摘要： The present invention is directed to a process for preparing a 2,26,6-d4-morpholine derivative represented by Structural Formula (I): or a salt thereof.
摘要翻译：本发明涉及一种制备由结构式（I）表示的2,26,6-d4-吗啉衍生物或其盐的方法。

8. 发明授权

US08258309B2 Azapeptide derivatives 有权
标题翻译： Azapeptide衍生物
公开(公告)号：US08258309B2
公开(公告)日：2012-09-04
申请号：US13411089
申请日：2012-03-02
申请人： Scott L. Harbeson , Roger D. Tung
发明人： Scott L. Harbeson , Roger D. Tung
IPC分类号： A61K31/44 , C07D213/00
CPC分类号： C07D213/42 , C07F9/58
摘要： This invention relates to novel compounds that are azapeptides, and pharmaceutically acceptable salts thereof. More specifically, the invention relates to novel azapeptide compounds that are derivatives of the HIV protease inhibitor atazanavir sulfate. This invention also provides pyrogen-free compositions comprising one or more compounds of the invention and a carrier, and the use of the disclosed compounds and compositions in methods of treating diseases and conditions that are treated by administering HIV protease inhibitors. The invention also relates to the use of one or more of the disclosed compounds as reagents in analytical studies involving atazanavir.
摘要翻译：本发明涉及作为氮杂肽的新化合物及其药学上可接受的盐。更具体地，本发明涉及作为HIV蛋白酶抑制剂阿扎那韦硫酸盐的衍生物的新型氮杂肽化合物。本发明还提供了包含一种或多种本发明化合物和载体的无热原组合物，以及所公开的化合物和组合物在治疗通过施用HIV蛋白酶抑制剂治疗的疾病和病症的方法中的用途。本发明还涉及一种或多种所公开的化合物在涉及阿扎那韦的分析研究中作为试剂的用途。

9. 发明申请

US20100160247A1 Synthesis of deuterated morpholine derivatives 有权
标题翻译：氘代吗啉衍生物的合成
公开(公告)号：US20100160247A1
公开(公告)日：2010-06-24
申请号：US12456507
申请日：2009-06-17
申请人： Julie F. Liu , Xuejun Tang , Scott L. Harbeson , Craig E. Masse
发明人： Julie F. Liu , Xuejun Tang , Scott L. Harbeson , Craig E. Masse
IPC分类号： A61K31/5377 , C07C215/68 , C07D265/30 , C07D413/10 , A61K31/7036 , A61K31/397 , A61P31/06 , A61P31/04 , A61P31/10 , A61K31/546 , A61K31/5383
CPC分类号： C07D413/10 , A61K31/5377 , A61K45/06 , C07B2200/05 , C07C215/12 , C07D263/06 , C07D295/02 , C07D295/033 , C07D295/06 , C07D295/12 , C07D295/135 , C07D413/14
摘要： The present invention is directed to a process for preparing a 2,26,6-d4-morpholine derivative represented by Structural Formula (I): or a salt thereof.
摘要翻译：本发明涉及一种制备由结构式（I）表示的2,26,6-d4-吗啉衍生物或其盐的方法。

10. 发明申请

US20100113589A1 Deuterated darunavir 有权
标题翻译：氘代地瑞那韦
公开(公告)号：US20100113589A1
公开(公告)日：2010-05-06
申请号：US12387327
申请日：2009-04-28
申请人： Scott L. Harbeson
发明人： Scott L. Harbeson
IPC分类号： A61K31/34 , C07D493/04
CPC分类号： C07B59/002 , C07D493/04
摘要： This invention relates to novel compounds that are hydroxyethylamino sulfonamide derivatives and pharmaceutically acceptable salts thereof. More specifically, this invention relates to novel hydroxyethylamino sulfonamide derivatives that are derivatives of darunavir. This invention also provides compositions comprising one or more compounds of this invention and a carrier and the use of the disclosed compounds and compositions in methods of treating diseases and conditions that are beneficially treated by administering a human immunodeficiency virus (HIV) protease inhibitor, such as darunavir.
摘要翻译：本发明涉及羟乙基氨基磺酰胺衍生物及其药学上可接受的盐的新型化合物。更具体地，本发明涉及作为地瑞那韦衍生物的新的羟乙基氨基磺酰胺衍生物。本发明还提供了包含本发明的一种或多种化合物和载体的组合物，以及所公开的化合物和组合物在治疗通过施用人类免疫缺陷病毒（HIV）蛋白酶抑制剂有益治疗的疾病和病症的方法中的用途，例如地瑞那韦

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