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公开(公告)号：US20100035826A1
公开(公告)日：2010-02-11
申请号：US12302764
申请日：2007-05-24
IPC分类号： A61K38/05 , C07D221/28 , C07K5/06 , C07D401/14 , A61K31/497 , A61K31/4748 , A61P25/04 , C07K5/062 , C07K5/068
CPC分类号： A61K31/485 , A61K47/542 , A61K47/545 , A61K47/556 , A61K47/64 , C07D489/02 , C07D489/08 , C07K5/06026
摘要： A method of providing a patient with controlled release of a phenolic opioid using a prodrug capable, upon enzymatic activation, of releasing the phenolic opioid through intra-molecular cyclization leading to formation of a cyclic urea, carbamate or thiocarbamate.
摘要翻译： 一种使用能够在酶活化时能够通过分子内环化释放酚类阿片样物质导致形成环状脲，氨基甲酸酯或硫代氨基甲酸酯的前体药物的前体药物为患者提供受控释放的酚类阿片样物质的方法。
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公开(公告)号：US20120142718A1
公开(公告)日：2012-06-07
申请号：US12524523
申请日：2008-02-15
IPC分类号： A61K31/46 , C07D489/02
CPC分类号： C07D489/04 , A61K47/54 , A61K47/542 , A61K47/65
摘要： Compounds of formula (II) R1R2R3N+—(C(R1a)(R2a))—Ar—Z—C(O)—Y—(C(R1)(R2))n—N—(R3)(R4)A−II, in which R1R2R3N+, R1a, R2a, Ar, Z, Y, R1, R2, n, R3, R4 and A− have the meanings given in the specification, are useful as prodrugs for opioids (Example 13).
摘要翻译： 式（II）化合物R1R2R3N + - （C（R1a）（R2a））-Ar-Z-C（O）-Y-（C（R1）（R2））n-N-（R3）（R4） II，其中R1R2R3N +，R1a，R2a，Ar，Z，Y，R1，R2，n，R3，R4和A具有说明书中给出的含义，可用作阿片类药物的前药（实施例13）。
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公开(公告)号：US08921418B2
公开(公告)日：2014-12-30
申请号：US13486613
申请日：2012-06-01
IPC分类号： A01N47/10 , A61K31/27 , C07C261/00 , C07C269/00 , C07C271/00 , A61K47/48
CPC分类号： A61K31/485 , A61K47/542 , A61K47/545 , A61K47/556 , A61K47/64 , C07D489/02 , C07D489/08 , C07K5/06026
摘要： A method of providing a patient with controlled release of a phenolic opioid using a prodrug capable, upon enzymatic activation, of releasing the phenolic opioid through intra-molecular cyclization leading to formation of a cyclic urea, carbamate or thiocarbamate.
摘要翻译： 一种使用能够在酶活化时能够通过分子内环化释放酚类阿片样物质导致形成环状脲，氨基甲酸酯或硫代氨基甲酸酯的前体药物的前体药物为患者提供受控释放的酚类阿片样物质的方法。
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公开(公告)号：US20120270894A1
公开(公告)日：2012-10-25
申请号：US13486613
申请日：2012-06-01
IPC分类号： C07D489/02 , A61P25/00 , A61K31/485
CPC分类号： A61K31/485 , A61K47/542 , A61K47/545 , A61K47/556 , A61K47/64 , C07D489/02 , C07D489/08 , C07K5/06026
摘要： A method of providing a patient with controlled release of a phenolic opioid using a prodrug capable, upon enzymatic activation, of releasing the phenolic opioid through intra-molecular cyclization leading to formation of a cyclic urea, carbamate or thiocarbamate.
摘要翻译： 一种使用能够在酶活化时能够通过分子内环化释放酚类阿片样物质导致形成环状脲，氨基甲酸酯或硫代氨基甲酸酯的前体药物的前体药物为患者提供受控释放的酚类阿片样物质的方法。
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公开(公告)号：US08217005B2
公开(公告)日：2012-07-10
申请号：US12302764
申请日：2007-05-24
IPC分类号： A61K38/00 , A61P3/04 , A61P25/00 , C07C261/00 , C07C269/00 , C07C271/00
CPC分类号： A61K31/485 , A61K47/542 , A61K47/545 , A61K47/556 , A61K47/64 , C07D489/02 , C07D489/08 , C07K5/06026
摘要： A method of providing a patient with controlled release of a phenolic opioid using a prodrug capable, upon enzymatic activation, of releasing the phenolic opioid through intra-molecular cyclization leading to formation of a cyclic urea, carbamate or thiocarbamate.
摘要翻译： 一种使用能够在酶活化时能够通过分子内环化释放酚类阿片样物质导致形成环状脲，氨基甲酸酯或硫代氨基甲酸酯的前体药物的前体药物为患者提供受控释放的酚类阿片样物质的方法。
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![PYRAZOLO[3,4-c]PYRIDINE COMPOUNDS AND METHODS OF USE](/abs-image/US/2013/02/14/US20130039906A1/abs.jpg.150x150.jpg)
公开(公告)号：US20130039906A1
公开(公告)日：2013-02-14
申请号：US13571595
申请日：2012-08-10
申请人： Steven Do , Huiyong Hu , Aleksandr Kolesnikov , Wendy Lee , Vickie H. Tsui , Xiaojing Wang , Zhaoyang Wen
发明人： Steven Do , Huiyong Hu , Aleksandr Kolesnikov , Wendy Lee , Vickie H. Tsui , Xiaojing Wang , Zhaoyang Wen
IPC分类号： C07D471/04 , A61K31/497 , A61K31/55 , A61K31/496 , A61K31/551 , A61K31/5377 , C07D471/10 , A61K31/506 , A61K31/438 , A61P35/00 , A61P37/00 , A61P9/00 , A61P31/12 , A61P29/00 , A61P3/00 , A61P5/00 , A61P25/00 , A61P35/02 , A61K31/573 , A61K31/675 , A61K31/704 , A61K31/4745 , A61K39/395 , A61K31/664 , A61K31/69 , A61K31/436 , A61K31/7068 , A61K31/437
CPC分类号： C07D471/04 , A61K31/437 , A61K31/496 , A61K31/497 , A61K31/4995 , A61K31/506 , A61K31/55 , A61K31/551 , A61K45/06 , C07D231/00 , C07D519/00
摘要： Pyrazolo[3,4-c]pyridine compounds of Formula I, including stereoisomers, geometric isomers, tautomers, and pharmaceutically acceptable salts thereof, wherein R1 and R2 are as defined herein, are useful for inhibiting Pim kinase, and for treating disorders such as cancer mediated by Pim kinase. Methods of using compounds of Formula I for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed.
摘要翻译： 式I的吡唑并[3,4-c]吡啶化合物，包括立体异构体，几何异构体，互变异构体及其药学上可接受的盐，其中R 1和R 2如本文所定义，可用于抑制Pim激酶， 由Pim激酶介导的癌症。 公开了使用式I化合物在体外，原位和体内诊断，预防或治疗哺乳动物细胞或相关病理状况中的这种病症的方法。
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公开(公告)号：US20120244149A1
公开(公告)日：2012-09-27
申请号：US13477587
申请日：2012-05-22
申请人： Nicole Blaquiere , Steven Do , Danette Dudley , Adrian Folkes , Robert Heald , Timothy Heffron , Mark Jones , Aleksandr Kolesnikov , Chudi Ndubaku , Alan G. Olivero , Stephen Price , Steven Staben , Lan Wang
发明人： Nicole Blaquiere , Steven Do , Danette Dudley , Adrian Folkes , Robert Heald , Timothy Heffron , Mark Jones , Aleksandr Kolesnikov , Chudi Ndubaku , Alan G. Olivero , Stephen Price , Steven Staben , Lan Wang
IPC分类号： A61K31/553 , A61K31/565 , A61P35/00 , A61P29/00 , A61P37/02 , A61P37/04 , A61P9/00 , A61P31/12 , A61P7/00 , A61P3/10 , A61P1/16 , A61K39/395 , A61P25/00
CPC分类号： C07D498/04 , A61K31/553 , A61K45/06 , C07D491/044 , C07D498/14 , C07D519/00
摘要： Benzoxazepin compounds of Formula I, including stereoisomers, geometric isomers, tautomers, solvates, metabolites and pharmaceutically acceptable salts thereof, wherein: Z1 is CR1 or N; Z2 is CR2 or N; Z3 is CR3 or N; Z4 is CR4 or N; and B is a pyrazolyl, imidazolyl, or triazolyl ring fused to the benzoxepin ring, are useful for inhibiting lipid kinases including p110 alpha and other isoforms of PI3K, and for treating disorders such as cancer mediated by lipid kinases. Methods of using compounds of Formula I for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed.
摘要翻译： 式I的苯并氧氮杂化合物，包括立体异构体，几何异构体，互变异构体，溶剂合物，代谢物及其药学上可接受的盐，其中：Z1是CR1或N; Z2为CR2或N; Z3为CR3或N; Z4是CR4或N; B是与苯并氧杂环环稠合的吡唑基，咪唑基或三唑基环，可用于抑制脂质激酶，包括p110α和PI3K的其他同种型，并用于治疗由脂质激酶介导的癌症等疾病。 公开了使用式I化合物在体外，原位和体内诊断，预防或治疗哺乳动物细胞或相关病理状况中的这种病症的方法。
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公开(公告)号：US08263633B2
公开(公告)日：2012-09-11
申请号：US12890810
申请日：2010-09-27
申请人： Nicole Blaquiere , Steven Do , Danette Dudley , Adrian Folkes , Richard Goldsmith , Robert Heald , Timothy Heffron , Aleksandr Kolesnikov , Chudi Ndubaku , Alan G. Olivero , Stephen Price , Steven Staben , BinQing Wei
发明人： Nicole Blaquiere , Steven Do , Danette Dudley , Adrian Folkes , Richard Goldsmith , Robert Heald , Timothy Heffron , Aleksandr Kolesnikov , Chudi Ndubaku , Alan G. Olivero , Stephen Price , Steven Staben , BinQing Wei
IPC分类号： A61K31/41 , C07D249/14
CPC分类号： C07D495/04 , A61K31/381 , A61K31/41 , A61K31/4196 , A61K31/4245 , A61K31/429 , A61K31/4365 , A61K31/4439 , A61K31/454 , A61K31/4545 , A61K31/496 , A61K31/4985 , A61K31/506 , A61K31/5377 , A61K31/541 , A61K31/551 , A61K45/06 , C07D249/14 , C07D495/14 , C07D513/04 , C07D513/14
摘要： Benzoxepin compounds of Formula I, and including stereoisomers, geometric isomers, tautomers, solvates, metabolites and pharmaceutically acceptable salts thereof, wherein: Z1 is CR1 or N; Z2 is CR2 or N; Z3 is CR3 or N; Z4 is CR4 or N; and where (i) X1 is N and X2 is S, (ii) X1 is S and X2 is N, (iii) X1 is CR7 and X2 is S, (iv) X1 is S and X2 is CR7; (v) X1 is NR8 and X2 is N, (vi) X1 is N and X2 is NR8, (vii) X1 is CR7 and X2 is O, (viii) X1 is O and X2 is CR7, (ix) X1 is CR7 and X2 is C(R7)2, (x) X1 is C(R7)2 and X2 is CR7; (xi) X1 is N and X2 is O, or (xii) X1 is O and X2 is N, are useful for inhibiting lipid kinases including p110 alpha and other isoforms of PI3K, and for treating disorders such as cancer mediated by lipid kinases. Methods of using compounds of Formula I for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed.
摘要翻译： 式I的苯并氧杂环己烯化合物，包括立体异构体，几何异构体，互变异构体，溶剂合物，代谢物及其药学上可接受的盐，其中：Z1是CR1或N; Z2为CR2或N; Z3为CR3或N; Z4是CR4或N; 并且其中（i）X1为N且X2为S，（ii）X1为S且X2为N，（iii）X1为CR7，X2为S，（iv）X1为S且X2为CR7; （ⅴ）X1为NR8，X2为N，（vi）X1为N，X2为NR8，i X1为CR7，X2为O，（ii）X1为O，X2为CR7，ix为CR7 X2为C（R7）2，（x）X1为C（R7）2，X2为CR7; （xi）X1是N，X2是O，或（xii）X1是O，X2是N，可用于抑制脂质激酶，包括p110α和PI3K的其他同种型，并用于治疗由脂质激酶介导的癌症等疾病。 公开了使用式I化合物在体外，原位和体内诊断，预防或治疗哺乳动物细胞或相关病理状况中的这种病症的方法。
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9.发明申请2-(2-HYDROXYBIPHENYL-3-YL)-1H-BENZOIMIDAZOLE-5-CARBOXAMIDINE DERIVATIVES AS FACTOR VIIA INHIBITORS 有权作为因子VIIA抑制剂的2-（2-羟基联苯-3-基）-1H-苯并咪唑-5-羧酰胺衍生物公开(公告)号：US20110269806A1
公开(公告)日：2011-11-03
申请号：US13100107
申请日：2011-05-03
申请人： Aleksandr Kolesnikov , Roopa Rai , William Dvorak Shrader , Steven M. Torkelson , Kieron E. Wesson , Wendy B. Young
发明人： Aleksandr Kolesnikov , Roopa Rai , William Dvorak Shrader , Steven M. Torkelson , Kieron E. Wesson , Wendy B. Young
IPC分类号： A61K31/4184 , A61P7/00
CPC分类号： C07D235/18 , C07D235/12 , C07D235/16 , C07D401/12 , C07D403/10 , C07F9/094 , C07F9/12 , C07F9/65128 , C12Q1/56
摘要： The present invention relates to novel inhibitors of Factors VIIa, IXa, Xa, XIa, in particular Factor VIIa, pharmaceutical compositions comprising these inhibitors, and methods for using these inhibitors for treating or preventing thromboembolic disorders, cancer or rheumatoid arthritis. Processes for preparing these inhibitors are also disclosed.
摘要翻译： 本发明涉及因子VIIa，IXa，Xa，XIa，特别是因子VIIa的新型抑制剂，包含这些抑制剂的药物组合物，以及使用这些抑制剂治疗或预防血栓栓塞性疾病，癌症或类风湿性关节炎的方法。 还公开了制备这些抑制剂的方法。
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10.发明申请公开(公告)号：US20110130363A1
公开(公告)日：2011-06-02
申请号：US13018068
申请日：2011-01-31
申请人： Steven Do , Richard Goldsmith , Tim Heffron , Aleksandr Kolesnikov , Steven Staben , Alan G. Olivero , Michael Siu , Daniel P. Sutherlin , Bing-Yan Zhu , Paul Goldsmith , Tracy Bayliss , Adrian Folkes , Neil Pegg
发明人： Steven Do , Richard Goldsmith , Tim Heffron , Aleksandr Kolesnikov , Steven Staben , Alan G. Olivero , Michael Siu , Daniel P. Sutherlin , Bing-Yan Zhu , Paul Goldsmith , Tracy Bayliss , Adrian Folkes , Neil Pegg
IPC分类号： A61K31/69 , C07D313/06 , C07D333/00 , C07D491/14 , C07F5/02 , C07D249/10 , C07D405/14 , A61K31/335 , A61K31/381 , A61K31/4196 , A61K31/443 , A61K31/497 , C12N9/99 , A61P35/00 , A61P35/02
CPC分类号： C07F5/02 , A61K31/381 , A61K31/4155 , A61K31/4196 , A61K31/4245 , A61K31/427 , A61K31/429 , A61K31/4365 , A61K31/4436 , A61K31/496 , A61K31/53 , C07D495/04 , C07D495/14 , C07D513/14
摘要： Benzopyran and benzoxepin compounds of Formulas I and II, and including stereoisomers, geometric isomers, tautomers, solvates, metabolites and pharmaceutically acceptable salts thereof, are useful for inhibiting lipid kinases including p110 alpha and other isoforms of PI3K, and for treating disorders such as cancer mediated by lipid kinases. Methods of using compounds of Formulas I and II for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed.
摘要翻译： 式I和II的苯并吡喃和苯并辛菌素化合物，包括立体异构体，几何异构体，互变异构体，溶剂合物，代谢物和药学上可接受的盐，可用于抑制脂质激酶，包括p110α和PI3K的其他同种型，并用于治疗疾病如癌症 由脂质激酶介导。 公开了使用式I和II的化合物在体外，原位和体内诊断，预防或治疗哺乳动物细胞或相关病理状况中的这种病症的方法。
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