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21. 发明授权

US07700601B2 Substituted indazoles of formula 1.0 that are kinase inhibitors 失效
标题翻译：式1.0的取代的吲唑是激酶抑制剂
公开(公告)号：US07700601B2
公开(公告)日：2010-04-20
申请号：US11729020
申请日：2007-03-28
申请人： Tin-Yau Chan , Brian A. McKittrick , Haiyan Pu , Liwu Hong , Andrew J. Prongay , Li Xiao , Mark A. McCoy
发明人： Tin-Yau Chan , Brian A. McKittrick , Haiyan Pu , Liwu Hong , Andrew J. Prongay , Li Xiao , Mark A. McCoy
IPC分类号： A61K31/4965
CPC分类号： C07D403/14 , C07D401/14 , C07D403/04
摘要： Disclosed is a compound of the formula: and the pharmaceutically acceptable salts thereof. Also disclosed are methods of treating protein kinase mediated diseases using the compound of formula 1.0. Also disclosed are methods of treating cancer using a compound of formula 1.0. The disclosed methods also include combination therapies wherein the compound of formula 1.0 is administered in combination with at least one addition pharmaceutically active ingredient.
摘要翻译：公开了下式的化合物及其药学上可接受的盐。还公开了使用式1.0化合物治疗蛋白激酶介导的疾病的方法。还公开了使用式1.0化合物治疗癌症的方法。所公开的方法还包括联合治疗，其中式1.0化合物与至少一种加成药物活性成分组合施用。

22. 发明申请

US20080070890A1 Spirocyclic Azetidinone Compounds and Methods of Use Thereof 审中-公开
标题翻译：螺环氮杂环丁酮化合物及其使用方法
公开(公告)号：US20080070890A1
公开(公告)日：2008-03-20
申请号：US11854746
申请日：2007-09-13
申请人： Duane A. Burnett , Brian A. McKittrick
发明人： Duane A. Burnett , Brian A. McKittrick
IPC分类号： A61K31/00 , A61P1/16 , A61P3/00 , A61P7/12 , C07D205/12
CPC分类号： C07D471/10
摘要： The present invention relates to Spirocyclic Azetidinone Compounds, compositions comprising a Spirocyclic Azetidinone Compound and methods for treating or preventing a disorder of lipid metabolism, pain, diabetes, a vascular condition, demyelination or nonalcoholic fatty liver disease, comprising administering to a patient an effective amount of a Spirocyclic Azetidinone Compound.
摘要翻译：本发明涉及螺环氮杂环丁酮化合物，包含螺环氮杂环丁酮化合物的组合物和治疗或预防脂质代谢紊乱，疼痛，糖尿病，血管病症，脱髓鞘或非酒精性脂肪性肝病的方法，包括向患者施用有效量的螺环氮杂环丁酮化合物。

23. 发明授权

US5633246A Sulfur-substituted azetidinone compounds useful as hypocholesterolemic agents 失效
公开(公告)号：US5633246A
公开(公告)日：1997-05-27
申请号：US463619
申请日：1995-06-05
申请人： Brian A. McKittrick , Sundeep Dugar , Duane A. Burnett
发明人： Brian A. McKittrick , Sundeep Dugar , Duane A. Burnett
IPC分类号： A61K31/395 , A61K31/397 , A61K31/44 , A61K31/4427 , A61K31/4433 , A61P3/06 , A61P9/10 , C07D205/08 , C07D401/12 , C07D409/12
CPC分类号： C07D401/12 , C07D205/08 , C07D409/12
摘要： Sulfur-substituted azetidinone hypocholesterolemic agents of the formula ##STR1## or a pharmaceutically acceptable salt thereof, wherein: Ar.sup.1 is aryl, R.sup.10 -substituted aryl or heteroaryl;Ar.sup.2 is aryl or R.sup.4 -substituted aryl;Ar.sup.3 is aryl or R.sup.5 -substituted aryl;X and Y are --CH.sub.2 --, --CH(lower alkyl)-- or --C(dilower alkyl)--;R is --OR.sup.6, --O(CO)R.sup.6, --O(CO)OR.sup.9 or --O(CO)NR.sup.6 R.sup.7 ; R.sup.1 is hydrogen, lower alkyl or aryl; or R and R.sup.1 together are .dbd.O;q is 0 or 1; r is 0, 1 or 2; m and n are 0-5; provided that the sum of m, n and q is 1-5;R.sup.4 is selected from lower alkyl, --OR.sup.6, --O(CO)R.sup.6, --O(CO)OR.sup.9, --O(CH.sub.2).sub.1-5 OR.sup.6, --O(CO)NR.sup.6 R.sup.7, --NR.sup.6 R.sup.7, --NR.sup.6 (CO)R.sup.7, --NR.sup.6 (CO)OR.sup.9, --NR.sup.6 (CO)NR.sup.7 R.sup.8, --NR.sup.6 SO.sub.2 R.sup.9, --COOR.sup.6, --CONR.sup.6 R.sup.7, --COR.sup.6, --SO.sub.2 NR.sup.6 R.sup.7, S(O).sub.0-2 R.sup.9, --O(CH.sub.2).sub.1-10 --COOR.sup.6, --O(CH.sub.2).sub.1-10 CONR.sup.6 R.sup.7, --(lower alkylene)--COOR.sup.6 and --CH.dbd.CH--COOR.sup.6 ;R.sup.5 is selected from --OR.sup.6, --O(CO)R.sup.6, --O(CO)OR.sup.9, --O(CH.sub.2).sub.1-5 OR.sup.6, --O(CO)NR.sup.6 R.sup.7, --NR.sup.6 R.sup.7, --NR.sup.6 (CO)R.sup.7, --NR.sup.6 (CO)OR.sup.9, --NR.sup.6 (CO)NR.sup.7 R.sup.8, --NR.sup.6 SO.sub.2 R.sup.9, --COOR.sup.6, --CONR.sup.6 R.sup.7, --COR.sup.6, --SO.sub.2 NR.sup.6 R.sup.7, S(O).sub.0-2 R.sup.9, --O(CH.sub.2).sub.1-10 --COOR.sup.6, --O(CH.sub.2).sub.1-10 CONR.sup.6 R.sup.7, --CF.sub.3, --CN, --NO.sub.2, halogen, --(lower alkylene)COOR.sup.6 and --CH.dbd.CH--COOR.sup.6 ;R.sup.6, R.sup.7 and R.sup.8 are H, lower alkyl, aryl or aryl-substituted lower alkyl;R.sup.9 is lower alkyl, aryl or aryl-substituted lower alkyl; andR.sup.10 is selected from lower alkyl, --OR.sup.6, --O(CO)R.sup.6, --O(CO)OR.sup.9, --O(CH.sub.2).sub.1-5 OR.sup.6, --O(CO)NR.sup.6 R.sup.7, --NR.sup.6 R.sup.7, --NR.sup.6 (CO)R.sup.7, --NR.sup.6 (CO)OR.sup.9, --NR.sup.6 (CO)NR.sup.7 R.sup.8, --NR.sup.6 SO.sub.2 R.sup.9, --COOR.sup.6, --CONR.sup.6 R.sup.7, --COR.sup.6, --SO.sub.2 NR.sup.6 R.sup.7, S(O).sub.0-2 R.sup.9, --O(CH.sub.2).sub.1-10 --COOR.sup.6, --O(CH.sub.2).sub.1-10 CONR.sup.6 R.sup.7, --CF.sub.3, --CN, --NO.sub.2 and halogen;are disclosed, as well as pharmaceutical compositions containing them, and a method of lowering serum cholesterol by administering said compounds, alone or in combination with a cholesterol biosynthesis inhibitor.

24. 发明授权

US4904799A Preparation of tryptophols 失效
标题翻译： tryptophols的制备
公开(公告)号：US4904799A
公开(公告)日：1990-02-27
申请号：US390801
申请日：1989-08-08
申请人： Brian A. McKittrick , Alan H. Katz
发明人： Brian A. McKittrick , Alan H. Katz
IPC分类号： A61K31/40 , A61P25/04 , A61P29/00 , C07D491/04 , C07D491/052
CPC分类号： C07D491/04
摘要： Indole derivatives characterized by having a 1,3,4,9-tetrahydropyrano[3,4-b]indole-1-acetic acid nucleus bearing a substituent in position 1-, 4-, 5-, 6-, 7- and 8- are disclosed. The derivatives are useful anti-inflammatory and analgesic agents and methods for their preparation and use are also disclosed.

25. 发明申请

US20110165118A1 3-HETEROCYCLIC SUBSTITUTED INDOLE DERIVATIVES AND METHODS OF USE THEREOF 有权
标题翻译： 3-杂环取代的吲哚衍生物及其使用方法
公开(公告)号：US20110165118A1
公开(公告)日：2011-07-07
申请号：US12743016
申请日：2008-11-13
申请人： Tin-Yau Chan , Jose S. Duca , Liwu Hong , Charles A. Lesburg , Brian A. McKittrick , Haiyan Pu , Li Wang , Henry M. Vaccaro
发明人： Tin-Yau Chan , Jose S. Duca , Liwu Hong , Charles A. Lesburg , Brian A. McKittrick , Haiyan Pu , Li Wang , Henry M. Vaccaro
IPC分类号： A61K31/519 , C07D495/04 , C07D403/04 , A61K31/517 , C07D487/04 , C07D473/04 , A61K31/522 , C07D471/04 , A61K31/513 , A61K31/5377 , A61K31/4178 , A61K38/21 , A61K31/7088 , A61K39/395 , A61P31/14
CPC分类号： C07D403/04 , C07D401/04 , C07D403/14 , C07D487/04 , C07D495/04
摘要： The present invention relates to 3-Heterocyclic Substituted Indole Derivatives, compositions comprising at least one 3-Heterocyclic Substituted Indole Derivative, and methods of using the 3-Heterocyclic Substituted Indole Derivatives for treating or preventing a viral infection or a virus-related disorder in a patient.
摘要翻译：本发明涉及3-杂环取代的吲哚衍生物，包含至少一种3-杂环取代的吲哚衍生物的组合物，以及使用3-杂环取代的吲哚衍生物用于治疗或预防病毒感染或病毒相关病症的方法患者。

26. 发明授权

US07528132B2 Kinase inhibitors 有权
标题翻译：激酶抑制剂
公开(公告)号：US07528132B2
公开(公告)日：2009-05-05
申请号：US11338501
申请日：2006-01-24
申请人： Tin-Yau Chan , Thierry O. Fischmann , Mark A. McCoy , Brian A. McKittrick , Andrew J. Prongay , Haiyan Pu , Li Wang , Li Xiao
发明人： Tin-Yau Chan , Thierry O. Fischmann , Mark A. McCoy , Brian A. McKittrick , Andrew J. Prongay , Haiyan Pu , Li Wang , Li Xiao
IPC分类号： C07D403/12 , C07D403/14 , A61K31/53 , A61P35/00
CPC分类号： C07D403/04
摘要： A compound having the general structure of Formula (I): or a pharmaceutically acceptable salt, solvate, or ester thereof, are useful in treating diseases, disorders, or conditions such as immunodeficiencies, cancers, cardiovascular diseases, endocrine disorders, Parkinson's disease, metabolic diseases, tumorigenesis, Alzheimer's disease, heart disease, diabetes, neurodegeneration, inflammation, kidney disease, atherosclerosis and airway disease.
摘要翻译：具有式（I）的通式结构的化合物或其药学上可接受的盐，溶剂化物或酯可用于治疗疾病，病症或病症，例如免疫缺陷，癌症，心血管疾病，内分泌紊乱，帕金森病，代谢疾病，肿瘤发生，阿尔茨海默病，心脏病，糖尿病，神经变性，炎症，肾脏疾病，动脉粥样硬化和气道疾病。

27. 发明授权

US06458812B1 Muscarinic antagonists 失效
标题翻译：毒蕈碱拮抗剂
公开(公告)号：US06458812B1
公开(公告)日：2002-10-01
申请号：US10023277
申请日：2001-12-17
申请人： Brian A. McKittrick , Guihua Guo , Zhaoning Zhu , Yuanzan Ye
发明人： Brian A. McKittrick , Guihua Guo , Zhaoning Zhu , Yuanzan Ye
IPC分类号： A61K31445
CPC分类号： C07D451/04 , C07D211/34 , C07D405/04
摘要： Amide derivatives of 1,4 di-substituted piperidine compounds of the formula: or a pharmaceutically acceptable salt, ester or solvate thereof, wherein R1 is optionally substituted cycloalkyl, cycloalkylalkyl, aryl, arylalkyl or heteroaryl; R2 is H, alkyl, or optionally substituted cycloalkyl, cycloalkylalkyl, heterocycloalkyl, bridged cycloalkyl, or bridged heterocycloalkyl; R3 is alkyl or —CH2OH; and R4 is H or alkyl; are muscarinic antagonists useful for treating cognitive disorders such as Alzheimer's disease. Pharmaceutical compositions and methods of preparation are also disclosed.
摘要翻译：其中R1是任选取代的环烷基，环烷基烷基，芳基，芳基烷基或杂芳基; R2是H，烷基或任意取代的环烷基环烷基烷基，杂环烷基，桥连环烷基或桥连杂环烷基; R3是烷基或-CH2OH; 和R 4是H或烷基;是可用于治疗认知障碍如阿尔茨海默氏病的毒蕈碱拮抗剂。还公开了药物组合物和制备方法。

28. 发明授权

US5846966A Combinations of hydroxy-substituted azetidinone compounds and HMG CoA Reductase Inhibitors 失效
标题翻译：羟基取代的氮杂环丁酮化合物与HMG CoA还原酶抑制剂的组合
公开(公告)号：US5846966A
公开(公告)日：1998-12-08
申请号：US953825
申请日：1997-10-14
申请人： Stuart B. Rosenblum , Sundeep Dugar , Duane A. Burnett , John W. Clader , Brian A. McKittrick
发明人： Stuart B. Rosenblum , Sundeep Dugar , Duane A. Burnett , John W. Clader , Brian A. McKittrick
IPC分类号： A61K31/21 , A61K31/35 , A61K31/395 , A61K31/397 , A61K31/40 , A61P3/06 , A61P7/00 , A61P9/10 , C07D205/08
CPC分类号： A61K45/06 , A61K31/21 , A61K31/35 , A61K31/395 , A61K31/40 , A61K9/2018 , A61K9/4858 , Y10S514/824
摘要： Hydroxy-substituted azetidinone hypocholesterolemic agents of the formula ##STR1## or a pharmaceutically acceptable salt thereof, wherein: Ar.sup.1 and Ar.sup.2 are aryl or R.sup.4 -substituted aryl; Ar.sup.3 is aryl or R.sup.5 -substituted aryl; X, Y and Z are --CH.sub.2 --, --CH(lower alkyl)-- or --C(dilower alkyl)--; R and R.sup.2 are --OR.sup.6, --O(CO)R.sup.6, --O(CO)OR.sup.9 or --O(CO)NR.sup.6 R.sup.7 ; R.sup.1 and R.sup.3 are H or lower alkyl; q is 0 or 1; r is 0 or 1; m, n and p are 0-4; provided that at least one of q and r is 1, and the sum of m, n, p, q and r is 1-6; and provided that when p is 0 and r is 1, the sum of m, q and n is 1-5; R.sup.4 is selected from lower alkyl, R.sup.5, --CF.sub.3, --CN, --NO.sub.2 and halogen; R.sup.5 is selected from --OR.sup.6, --O(CO)R.sup.6, --O(CO)OR.sup.9, --O(CH.sub.2).sub.1-5 OR.sup.6, --O(CO)NR.sup.6 R.sup.7, --NR.sup.6 R.sup.7, --NR.sup.6 (CO)R.sup.7, --NR.sup.6 (CO)OR.sup.9, --NR.sup.6 (CO)NR.sup.7 R.sup.8, --NR.sup.6 SO.sub.2 R.sup.9, --COOR.sup.6, --CONR.sup.6 R.sup.7, --COR.sup.6, --SO.sub.2 NR.sup.6 R.sup.7, S(O).sub.0-2 R.sup.9, --O(CH.sub.2).sub.1-10 --COOR.sup.6, --O(CH.sub.2).sub.1-10 CONR.sup.6 R.sup.7, --(lower alkylene)COOR.sup.6 and --CH.dbd.CH--COOR.sup.6 ; R.sup.6, R.sup.7 and R.sup.8 are H, lower alkyl, aryl or aryl-substituted lower alkyl; R.sup.9 is lower alkyl, aryl or aryl-substituted lower alkyl; are disclosed, as well as a method of lowering serum cholesterol by administering said compounds, alone or in combination with a cholesterol biosynthesis inhibitor, pharmaceutical compositions containing them, and a process for preparing them.
摘要翻译：式（I）的羟基取代的氮杂环丁酮降胆固醇剂或其药学上可接受的盐，其中：Ar 1和Ar 2是芳基或R 4取代的芳基; Ar 3是芳基或者R 5取代的芳基; X，Y和Z是-CH 2 - ， - CH（低级烷基） - 或-C（二卤代烷基） - 。 R和R 2为-OR 6，-O（CO）R 6，-O（CO）OR 9或-O（CO）NR 6 R 7; R1和R3是H或低级烷基; q为0或1; r为0或1; m，n和p为0-4; 条件是q和r中的至少一个是1，m，n，p，q和r的和是1-6; 并且当p为0且r为1时，m，q和n的和为1-5; R4选自低级烷基，R5，-CF3，-CN，-NO2和卤素; R5选自-OR6，-O（CO）R6，-O（CO）OR9，-O（CH2）1-5OR6，-O（CO）NR6R7，-NR6R7，-NR6（CO）R7，-NR6（ CO）OR 9，-NR 6（CO）NR 7 R 8，-NR 6 SO 2 R 9，-COOR 6，-CONR 6 R 7，-COR 6，-SO 2 NR 6 R 7，S（O）0-2R 9，-O（CH 2）1-10 -COOR 6，-O 1-10CONR6R7， - （低级亚烷基）COOR6和-CH = CH-COOR6; R6，R7和R8是H，低级烷基，芳基或芳基取代的低级烷基; R9是低级烷基，芳基或芳基取代的低级烷基; 以及通过单独或与胆固醇生物合成抑制剂组合使用所述化合物，含有它们的药物组合物及其制备方法来降低血清胆固醇的方法。

29. 发明授权

US5744467A Sulfur-substituted azetidinone compounds useful as hypocholesterolemic agents 失效
标题翻译：可用作降胆固醇药的硫取代的氮杂环丁酮化合物
公开(公告)号：US5744467A
公开(公告)日：1998-04-28
申请号：US813585
申请日：1997-01-08
申请人： Brian A. McKittrick , Sundeep Dugar , Duane A. Burnett
发明人： Brian A. McKittrick , Sundeep Dugar , Duane A. Burnett
IPC分类号： A61K31/395 , A61K31/397 , A61K31/44 , A61K31/4427 , A61K31/4433 , A61P3/06 , A61P9/10 , C07D205/08 , C07D401/12 , C07D409/12
CPC分类号： C07D401/12 , C07D205/08 , C07D409/12
摘要： Sulfur-substituted azetidinone hypocholesterolemic agents of the formula ##STR1## or a pharmaceutically acceptable salt thereof are disclosed, as well as pharmaceutical compositions containing them, and a method of lowering serum cholesterol by administering said compounds, alone or in combination with a cholesterol biosynthesis inhibitor.
摘要翻译：公开了具有式“IMAGE”I的硫取代的氮杂环丁酮降胆固醇药或其药学上可接受的盐，以及含有它们的药物组合物，以及通过单独或与胆固醇生物合成组合施用所述化合物来降低血清胆固醇的方法抑制剂。

30. 发明授权

US5624920A Sulfur-substituted azetidinone compounds useful as hypocholesterolemic agents 失效
公开(公告)号：US5624920A
公开(公告)日：1997-04-29
申请号：US342197
申请日：1994-11-18
申请人： Brian A. McKittrick , Sundeep Dugar , Duane A. Burnett
发明人： Brian A. McKittrick , Sundeep Dugar , Duane A. Burnett
IPC分类号： C07D205/08 , C07D401/12 , C07D409/12 , A61K31/395
CPC分类号： C07D401/12 , C07D205/08 , C07D409/12
摘要： Sulfur-substituted azetidinone hypocholesterolemic agents of the formula ##STR1## or a pharmaceutically acceptable salt thereof, wherein: Ar.sup.1 is aryl or R.sup.10 -substituted aryl;Ar.sup.2 is aryl or R.sup.4 -substituted aryl;Ar.sup.3 is aryl or R.sup.5 -substituted aryl;X and Y are --CH.sub.2 --, --CH(lower alkyl)-- or --C(dilower alkyl)--;R is --OR.sup.6, --O(CO)R.sup.6, --O(CO)OR.sup.9 or --O(CO)NR.sup.6 R.sup.7 ; R.sup.1 is hydrogen, lower alkyl or aryl; or R and R.sup.1 together are .dbd.O;q is 0 or 1; r is 0, 1 or 2; m and n are 0-5; provided that the sum of m, n and q is 1-5;R.sup.4 is selected from lower alkyl, --OR.sup.6, --O(CO)R.sup.6, --O(CO)OR.sup.9, --O(CH.sub.2).sub.1-5 OR.sup.6, --O(CO)NR.sup.6 R.sup.7, --NR.sup.6 R.sup.7, --NR.sup.6 (CO)R.sup.7, --NR.sup.6 (CO)OR.sup.9, --NR.sup.6 (CO)NR.sup.7 R.sup.8, --NR.sup.6 SO.sub.2 R.sup.9, --COOR.sup.6, --CONR.sup.6 R.sup.7, --COR.sup.6, --SO.sup.2 NR.sup.6 R.sup.7, S(O).sub.0-2 R.sup.9, --O(CH.sub.2).sub.1-10 --COOR.sup.6, --O(CH.sub.2).sub.1-10 CONR.sup.6 R.sup.7, --(lower alkylene)--COOR.sup.6 and --CH.dbd.CH--COOR.sup.6 ;R.sup.5 is selected from --OR.sup.6, --O(CO)R.sup.6, --O(CO)OR.sup.9, --O(CH.sub.2).sub.1-5 OR.sup.6, --O(CO)NR.sup.6 R.sup.7, --NR.sup.6 R.sup.7, --NR.sup.6 (CO)R.sup.7, --NR.sup.6 (CO)OR.sup.9, --NR.sup.6 (CO)NR.sup.7 R.sup.8, --NR.sup.6 SO.sub.2 R.sup.9, --COOR.sup.6, --CONR.sup.6 R.sup.7, --COR.sup.6, --SO.sub.2 NR.sup.6 R.sup.7, S(O).sub.0-2 R.sup.9, --O(CH.sub.2).sub.1-10 --COOR.sup.6, --O(CH.sub.2).sub.1-10 CONR.sup.6 R.sup.7, --CF.sub.3, --CN, --NO.sub.2, halogen, --(lower alkylene)COOR.sup.6 and --CH.dbd.CH--COOR.sup.6 ;R.sup.6, R.sup.7 and R.sup.8 are H, lower alkyl, aryl or aryl-substituted lower alkyl;R.sup.9 is lower alkyl, aryl or aryl-substituted lower alkyl; andR.sup.10 is selected from lower alkyl, --OR.sup.6, --O(CO)R.sup.6, --O(CO)OR.sup.9, --O(CH.sub.2).sub.1-5 OR.sup.6, --O(CO)NR.sup.6 R.sup.7, --NR.sup.6 R.sup.7, --NR.sup.6 (CO)R.sup.7, --NR.sup.6 (CO)OR.sup.9, --NR.sup.6 (CO)NR.sup.7 R.sup.8, --NR.sup.6 SO.sub.2 R.sup.9, --COOR.sup.6, --CONR.sup.6 R.sup.7, --COR.sup.6, --SO.sub.2 NR.sup.6 R.sup.7, S(O).sub.0-2 R.sup.9, --O(CH.sub.2).sub.1-10 --COOR.sup.6, --O(CH.sub.2).sub.1-10 CONR.sup.6 R.sup.7, --CF.sub.3, --CN, --NO.sub.2 and halogen;are disclosed, as well as pharmaceutical compositions containing them, and a method of lowering serum cholesterol by administering said compounds, alone or in combination with a cholesterol biosynthesis inhibitor.

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