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51. 发明申请

US20140005174A1 INDOLE DERIVATIVES USEFUL AS CCR2 ANTAGONISTS 审中-公开
标题翻译：内含衍生物作为CCR2拮抗剂有用
公开(公告)号：US20140005174A1
公开(公告)日：2014-01-02
申请号：US14004464
申请日：2012-03-14
申请人： Anilkumar G. Nair , Joseph A. Kozlowski , Jose S. Duca , Stuart B. Rosenblum
发明人： Anilkumar G. Nair , Joseph A. Kozlowski , Jose S. Duca , Stuart B. Rosenblum
IPC分类号： C07D401/12 , C07D491/048 , C07D403/12
CPC分类号： C07D401/12 , C07D403/12 , C07D491/04 , C07D491/048
摘要： Disclosed are the CCR2 antagonists of Formula I: I or pharmaceutically acceptable salt thereof wherein R7, A, X, B, and n are defined herein. Also disclosed are pharmaceutical compositions containing the compounds, methods of treatment using the compounds, and compositions to treat diseases or disorders associated with CCR2 activity.
摘要翻译：公开了式I的CCR2拮抗剂：I或其药学上可接受的盐，其中R7，A，X，B和n如本文所定义。还公开了含有化合物的药物组合物，使用该化合物的治疗方法和用于治疗与CCR2活性相关的疾病或病症的组合物。

52. 发明申请

US20120251491A1 FUSED TRICYCLIC ARYL COMPOUNDS USEFUL FOR THE TREATMENT OF VIRAL DISEASES 有权
标题翻译：用于治疗病毒性疾病的融合的三酰甘油化合物
公开(公告)号：US20120251491A1
公开(公告)日：2012-10-04
申请号：US13320427
申请日：2010-05-12
申请人： Stuart B. Rosenblum , Kevin X. Chen , Joseph A. Kozlowski , F. George Njoroge , Craig A. Coburn
发明人： Stuart B. Rosenblum , Kevin X. Chen , Joseph A. Kozlowski , F. George Njoroge , Craig A. Coburn
IPC分类号： A61K31/4178 , C07D487/04 , C07D493/04 , A61K31/4184 , A61K31/4188 , C07D471/04 , A61K31/4745 , C07D491/044 , A61K31/55 , C07D401/14 , A61K31/473 , A61K31/498 , A61K38/21 , A61K31/7088 , A61K39/12 , A61K39/395 , A61K31/7056 , A61P31/14 , A61P37/04 , A61P31/12 , C07D403/14
CPC分类号： C07D403/14 , C07C403/04 , C07D403/04 , C07D471/04 , C07D487/04 , C07D491/044 , C07D493/04
摘要： The present invention relates to novel Fused Tricyclic Aryl Compounds, compositions comprising at least one Fused Tricyclic Aryl Compound, and methods of using the Fused Tricyclic Aryl Compounds for treating or preventing HCV infection in a patient.
摘要翻译：本发明涉及新的熔融三环芳基化合物，包含至少一种稠合三环芳基化合物的组合物，以及使用稠合三环芳基化合物治疗或预防患者HCV感染的方法。

53. 发明申请

US20140170111A1 FUSED TETRACYCLE DERIVATIVES AND METHODS OF USE THEREOF FOR THE TREATMENT OF VIRAL DISEASES 有权
标题翻译：融合的四氢吡啶衍生物及其用于治疗病毒的方法
公开(公告)号：US20140170111A1
公开(公告)日：2014-06-19
申请号：US13876931
申请日：2011-09-28
申请人： Craig A. Coburn , Brian J. Lavey , Michael P. Dwyer , Joseph A. Kozlowski , Stuart B. Rosenblum
发明人： Craig A. Coburn , Brian J. Lavey , Michael P. Dwyer , Joseph A. Kozlowski , Stuart B. Rosenblum
IPC分类号： A61K31/553 , A61K31/4178 , C07D493/04 , A61K45/06 , C07D498/04 , C07D487/04 , A61K31/5517 , C07D403/14 , C07D405/14
CPC分类号： A61K31/553 , A61K31/4178 , A61K31/5517 , A61K45/06 , C07D403/14 , C07D405/14 , C07D487/04 , C07D493/04 , C07D498/04 , Y02A50/385 , Y02A50/387 , Y02A50/389 , Y02A50/395
摘要： The present invention relates to novel Fused Tetracycle Derivatives of Formula (I): and pharmaceutically acceptable salts thereof, wherein A, A′, B, G, R1, U, V, W, W′, X, X′, Y and Y′ are as defined herein. The present invention also relates to compositions comprising at least one Fused Tetracycle Derivative, and methods of using the Fused Tetracycle Derivatives for treating or preventing HCV infection in a patient.
摘要翻译：本发明涉及式（I）的新型熔融四环衍生物及其药学上可接受的盐，其中A，A'，B，G，R 1，U，V，W，W'，X，X'，Y和Y '如本文所定义。本发明还涉及包含至少一种熔融四环衍生物的组合物，以及使用熔融四环衍生物治疗或预防患者HCV感染的方法。

54. 发明授权

US08377928B2 3-aminosulfonyl substituted indole derivatives and methods of use thereof 有权
标题翻译： 3-氨基磺酰基取代的吲哚衍生物及其使用方法
公开(公告)号：US08377928B2
公开(公告)日：2013-02-19
申请号：US12743023
申请日：2008-11-13
申请人： Kevin X. Chen , Stuart B. Rosenblum , F. George Njoroge , Joseph A. Kozlowski
发明人： Kevin X. Chen , Stuart B. Rosenblum , F. George Njoroge , Joseph A. Kozlowski
IPC分类号： A61K31/404 , A61K31/549
CPC分类号： C07D417/14
摘要： The present invention relates to 3-Aminosulfonyl Substituted Indole Derivatives of Formula (I): The invention also relates to compositions comprising at least one 3-Aminosulfonyl Substituted Indole Derivative, and methods of using the 3-Aminosulfonyl Substituted Indole Derivatives for treating or preventing a viral infection or a virus-related disorder in a patient.
摘要翻译：本发明涉及式（I）的3-氨基磺酰基取代的吲哚衍生物：本发明还涉及包含至少一种3-氨基磺酰基取代的吲哚衍生物的组合物，以及使用3-氨基磺酰基取代的吲哚衍生物用于治疗或预防病毒感染或病毒相关疾病。

55. 发明申请

US20100322901A1 5, 6-RING ANNULATED INDOLE DERIVATIVES AND USE THEREOF 有权
标题翻译： 5，6环结构的吲哚衍生物及其用途
公开(公告)号：US20100322901A1
公开(公告)日：2010-12-23
申请号：US12519975
申请日：2007-12-17
申请人： Frank Bennett , Srikanth Venkatraman , F. George Njoroge , Kevin X. Chen , Neng-Yang Shih , Stuart B. Rosenblum , Joseph A. Kozlowski
发明人： Frank Bennett , Srikanth Venkatraman , F. George Njoroge , Kevin X. Chen , Neng-Yang Shih , Stuart B. Rosenblum , Joseph A. Kozlowski
IPC分类号： A61K31/4439 , C07D401/04 , C07D491/048 , C07D513/04 , C07D417/14 , C07D401/14 , C07D471/04 , A61K31/444 , A61K31/4709 , A61K31/519 , A61K31/517 , A61K31/4375 , A61K31/437 , A61K38/21 , A61K31/7088 , A61K39/00 , A61K39/395 , A61P31/12
CPC分类号： C07D513/04 , C07D401/04 , C07D471/04 , C07D491/04
摘要： The present invention relates to 5,6-ring annulated indole derivatives of the formula (I), compositions comprising at least one 5,6-ring annulated indole derivatives, and methods of using the 5,6-ring annulated indole derivatives for treating or preventing a viral infection or a virus-related disorder in a patient.
摘要翻译：本发明涉及式（I）的5,6环环状吲哚衍生物，包含至少一种5,6环环状吲哚衍生物的组合物，以及使用5,6环环状吲哚衍生物用于治疗或预防患者的病毒感染或病毒相关疾病。

56. 发明申请

US20080119487A1 NOVEL NON-IMIDAZOLE COMPOUNDS 审中-公开
标题翻译：新型非咪唑化合物
公开(公告)号：US20080119487A1
公开(公告)日：2008-05-22
申请号：US11943315
申请日：2007-11-20
申请人： Robert G. Aslanian , Neng-Yang Shih , Pauline C. Ting , Michael Y. Berlin , Stuart B. Rosenblum , Kevin D. McCormick , Wing C. Tom , Christopher W. Boyce , Pietro Mangiaracina , Mwangi W. Mutahi , John J. Piwinski
发明人： Robert G. Aslanian , Neng-Yang Shih , Pauline C. Ting , Michael Y. Berlin , Stuart B. Rosenblum , Kevin D. McCormick , Wing C. Tom , Christopher W. Boyce , Pietro Mangiaracina , Mwangi W. Mutahi , John J. Piwinski
IPC分类号： A61K31/495 , A61K31/445 , A61K31/435 , A61P27/14 , A61P11/02
CPC分类号： C07D213/73 , A61K31/435 , A61K31/445 , A61K31/495 , C07D401/12 , C07D401/14 , C07D409/14 , C07D413/14 , C07D417/14 , C07D498/04
摘要： Disclosed are novel compounds of the formula Also disclosed are pharmaceutical compositions comprising the compounds of Formula I.Also disclosed are methods of treating various diseases or conditions, such as, for example, allergy, allergy-induced airway responses, and congestion (e.g., nasal congestion) using the compounds of Formula I.Also disclosed are methods of treating various diseases or conditions, such as, for example, allergy, allergy-induced airway responses, and congestion (e.g., nasal congestion) using the compounds of Formula I in combination with a H1 receptor antagonist.
摘要翻译：公开的是式的新化合物还公开了包含式I化合物的药物组合物。还公开了治疗各种疾病或病症的方法，例如过敏，过敏诱发的气道反应和充血（例如，鼻拥塞）。还公开了使用组合式I化合物来治疗各种疾病或病症的方法，例如过敏，过敏诱发的气道反应和充血（例如，鼻塞）具有H 1受体拮抗剂。

57. 发明授权

US6130229A Tricyclic compounds having activity as RAS-FPT inhibitors 失效
标题翻译：具有作为RAS-FPT抑制剂的活性的三环化合物
公开(公告)号：US6130229A
公开(公告)日：2000-10-10
申请号：US946527
申请日：1997-10-07
申请人： Adriano Afonso , Joseph M. Kelly , Stuart B. Rosenblum , Ronald L. Wolin , Jay Weinstein
发明人： Adriano Afonso , Joseph M. Kelly , Stuart B. Rosenblum , Ronald L. Wolin , Jay Weinstein
IPC分类号： C07D491/04 , C07D495/04 , A61K31/445
CPC分类号： C07D491/04 , C07D495/04
摘要： Compounds of Formula I: ##STR1## wherein: X.sup.1 is hydrogen, halogen, CF.sub.3, nitro, NH.sub.2 or lower alkyl;each X.sup.2 is independently selected from the group consisting of hydrogen, halogen, lower alkoxy and lower alkyl;n is 1 or 2;Y is selected from the group consisting of S(O).sub.p, O, and NR.sup.5, wherein p is 0, 1 or 2, and R.sup.5 is hydrogen, alkyl, aryl, cycloalkyl, loweralkoxycarbonyl, aminocarbonyl or acyl;R.sup.1 and R.sup.2, which may be the same or different, are selected from the group consisting of hydrogen and lower alkyl groups, or taken together can form an oxygen atom when Y is NR.sup.5 ;A . . . is C=, CH-- or N--;R is --CZ--Y.sup.1 --Y.sup.2 --R.sup.3, wherein:Z is O, =CH--CN, or =N--CN;one of Y.sup.1 and Y.sup.2 is a bond, --CO--, O, S, or --NR.sup.4 --, and the other is (CH.sub.2).sub.m, where m is 0 or an integer of 1 to 4, and R.sup.4 is H or alkyl, with the proviso that when Z is O and m is 0 then Y.sup.1 or Y.sup.2 is selected from --CO--, O, S, or --NR.sup.4 ;R.sup.3 is aryl, heteroaryl or heterocycloalkyl, with the proviso that R.sup.3 can also be lower alkyl when Z is =N--CN;and their pharmaceutically acceptable acid addition salts; have activity as Ras-FPT inhibitors. They can be used, e.g., in pharmaceutical compositions, for inhibiting the abnormal growth of cells and for inhibiting proliferative diseases. Processes for their preparation, and useful intermediates, are also disclosed.
摘要翻译：式I化合物：其中：X 1是氢，卤素，CF 3，硝基，NH 2或低级烷基; 每个X 2独立地选自氢，卤素，低级烷氧基和低级烷基; n为1或2; Y选自S（O）p，O和NR5，其中p为0,1或2，R5为氢，烷基，芳基，环烷基，低级烷氧羰基，氨基羰基或酰基; R 1和R 2可以相同或不同，选自氢和低级烷基，或者当Y是NR 5时可以一起形成氧原子; 一个。。。是C =，CH-或N-; R为-CZ-Y1-Y2-R3，其中：Z为O，= CH-CN或= N-CN; Y1和Y2之一是键，-CO-，O，S或-NR4-，另一个是（CH2）m，其中m是0或1-4的整数，R4是H或烷基，条件是当Z为O且m为0时，则Y1或Y2选自-CO-，O，S或-NR4; R3是芳基，杂芳基或杂环烷基，条件是当Z = N-CN时，R3也可以是低级烷基; 及其药学上可接受的酸加成盐; 具有作为Ras-FPT抑制剂的活性。它们可以用于例如药物组合物中，用于抑制细胞异常生长和抑制增殖性疾病。还公开了它们的制备方法和有用的中间体。

58. 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。

59. 发明授权

US07300941B2 Non-imidazole compounds 失效
标题翻译：非咪唑化合物
公开(公告)号：US07300941B2
公开(公告)日：2007-11-27
申请号：US10699189
申请日：2003-10-31
申请人： Robert G. Aslanian , Neng-Yang Shih , Pauline C. Ting , Michael Y. Berlin , Stuart B. Rosenblum , Kevin D. McCormick , Wing C. Tom , Christopher W. Boyce , Pietro Mangiaracina , Mwangi W. Mutahi , John J. Piwinski
发明人： Robert G. Aslanian , Neng-Yang Shih , Pauline C. Ting , Michael Y. Berlin , Stuart B. Rosenblum , Kevin D. McCormick , Wing C. Tom , Christopher W. Boyce , Pietro Mangiaracina , Mwangi W. Mutahi , John J. Piwinski
IPC分类号： A61K31/44
CPC分类号： C07D213/73 , A61K31/435 , A61K31/445 , A61K31/495 , C07D401/12 , C07D401/14 , C07D409/14 , C07D413/14 , C07D417/14 , C07D498/04
摘要： Disclosed are novel compounds of the formula Also disclosed are pharmaceutical compositions comprising the compounds of Formula I.Also disclosed are methods of treating various diseases or conditions, such as, for example, allergy, allergy-induced airway responses, and congestion (e.g., nasal congestion) using the compounds of Formula I.Also disclosed are methods of treating various diseases or conditions, such as, for example, allergy, allergy-induced airway responses, and congestion (e.g., nasal congestion) using the compounds of Formula I in combination with a H1 receptor antagonist.
摘要翻译：公开的是式的新化合物还公开了包含式I化合物的药物组合物。还公开了治疗各种疾病或病症的方法，例如过敏，过敏诱发的气道反应和充血（例如，鼻拥塞）。还公开了使用组合式I化合物来治疗各种疾病或病症的方法，例如过敏，过敏诱发的气道反应和充血（例如，鼻塞）具有H 1受体拮抗剂。

60. 发明授权

US06720328B2 Non-imidazole compounds 失效
标题翻译：非咪唑化合物
公开(公告)号：US06720328B2
公开(公告)日：2004-04-13
申请号：US09978267
申请日：2001-10-15
申请人： Robert G. Aslanian , Neng-Yang Shih , Pauline C. Ting , Michael Y. Berlin , Stuart B. Rosenblum , Kevin D. McCormick , Wing C. Tom , Christopher W. Boyce , Pietro Mangiaracina , Mwangi W. Mutahi , John J. Piwinski
发明人： Robert G. Aslanian , Neng-Yang Shih , Pauline C. Ting , Michael Y. Berlin , Stuart B. Rosenblum , Kevin D. McCormick , Wing C. Tom , Christopher W. Boyce , Pietro Mangiaracina , Mwangi W. Mutahi , John J. Piwinski
IPC分类号： C07D40114
CPC分类号： C07D213/73 , A61K31/435 , A61K31/445 , A61K31/495 , C07D401/12 , C07D401/14 , C07D409/14 , C07D413/14 , C07D417/14 , C07D498/04
摘要： Disclosed are novel compounds of the formula In Formula I, M1 is carbon, M2, M3 and M4 are carbon or nitrogen and the remaining variables are as defined in the specification. Also disclosed are pharmaceutical compositions comprising the compounds of Formula I. Also disclosed are methods of treating various diseases or conditions, such as, for example, allergy, allergy-induced airway responses, and congestion (e.g., nasal congestion) using the compounds of Formula I. Also disclosed are methods of treating various diseases or conditions, such as, for example, allergy, allergy-induced airway responses, and congestion (e.g., nasal congestion) using the compounds of Formula I in combination with a H1 receptor antagonist.
摘要翻译：公开了式I的新化合物，式I中M 1是碳，M 2，M 3和M 4是碳或氮，其余的变量如说明书中所定义。还公开了包含式I化合物的药物组合物。还公开了使用式（I）的化合物治疗各种疾病或病症例如过敏，过敏诱发的气道反应和充血（例如，鼻塞）的方法还公开了使用式I化合物与H1受体拮抗剂组合来治疗各种疾病或病症的方法，例如过敏，过敏诱导的气道反应和充血（例如，鼻塞）。

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