公开(公告)号：WO2015095258A1

公开(公告)日：2015-06-25

申请号：PCT/US2014/070712

申请日：2014-12-17

Applicant: MERCK SHARP & DOHME CORP. ,  GRAHAM, Thomas, H. ,  LIU, Wensheng ,  YU, Tao ,  ZHANG, Yonglian ,  WADDELL, Sherman, T. ,  WAI, John, S. ,  COLEMAN, Paul, J. ,  SANDERS, John, M. ,  EMBREY, Mark, W. ,  WALJI, Abbas, M. ,  FERGUSON, Ronald Dale, II ,  DI MARCO, Christina Ng ,  STEELE, Thomas, G. ,  HU, Lihong ,  PENG, Xuanjia

Inventor： GRAHAM, Thomas, H. ,  LIU, Wensheng ,  YU, Tao ,  ZHANG, Yonglian ,  WADDELL, Sherman, T. ,  WAI, John, S. ,  COLEMAN, Paul, J. ,  SANDERS, John, M. ,  EMBREY, Mark, W. ,  WALJI, Abbas, M. ,  FERGUSON, Ronald Dale, II ,  DI MARCO, Christina Ng ,  STEELE, Thomas, G. ,  HU, Lihong ,  PENG, Xuanjia

IPC: C07D498/04 ,  A61K31/55

CPC classification number: A61K31/53 ,  A61K31/427 ,  A61K31/499 ,  A61K31/513 ,  A61K31/52 ,  A61K31/55 ,  A61K31/675 ,  A61K45/06 ,  C07D471/20 ,  C07D471/22 ,  C07D475/10 ,  C07D491/10 ,  C07D491/20 ,  C07D495/10 ,  C07D495/20 ,  C07F9/65616 ,  A61K2300/00

Abstract: The present invention relates to Spirocyclic Heterocycle Compounds of Formula (I): and pharmaceutically acceptable salts thereof, wherein A, B, X, Y, R 1 , R 2 and R 11 are as defined herein. The present invention also relates to compositions comprising at least one Spirocyclic Heterocycle Compound, and methods of using the Spirocyclic Heterocycle Compounds for treating or preventing HIV infection in a subject.

Abstract translation: 本发明涉及式（I）的螺环杂环化合物及其药学上可接受的盐，其中A，B，X，Y，R 1，R 2和R 11如本文所定义。 本发明还涉及包含至少一种螺环杂环化合物的组合物，以及使用螺环杂环化合物治疗或预防受试者中HIV感染的方法。

公开(公告)号：WO2012058173A1

公开(公告)日：2012-05-03

申请号：PCT/US2011/057557

申请日：2011-10-25

Applicant: MERCK SHARP & DOHME CORP. ,  MERCK CANADA INC. ,  BARBE, Guillaume ,  NGUYEN, Natalie, N., M. ,  BLOUIN, Marc ,  GAREAU, Yves ,  POWELL, David, A. ,  COTE, Bernard ,  HUMPHREY, Guy Roland ,  KUETHE, Jeffrey Thomas ,  CHILDERS, Karla Glaser ,  FARAND, Julie ,  TREPANIER, Vincent Hector Emile ,  LARIVEE, Alexandre ,  RADA, Vanessa Louise ,  EMBREY, Mark, W. ,  STEELE, Thomas, G. ,  SISKO, John, T. ,  BENNETT, David Jonathan ,  RAHEEM, Izzat Tiedje ,  SCHREIER, John David ,  HARTINGH, Timothy John ,  SHIPE, William, D. ,  BUNDA, Jaime Lynn

Inventor： BARBE, Guillaume ,  NGUYEN, Natalie, N., M. ,  BLOUIN, Marc ,  GAREAU, Yves ,  POWELL, David, A. ,  COTE, Bernard ,  HUMPHREY, Guy Roland ,  KUETHE, Jeffrey Thomas ,  CHILDERS, Karla Glaser ,  FARAND, Julie ,  TREPANIER, Vincent Hector Emile ,  LARIVEE, Alexandre ,  RADA, Vanessa Louise ,  EMBREY, Mark, W. ,  STEELE, Thomas, G. ,  SISKO, John, T. ,  BENNETT, David Jonathan ,  RAHEEM, Izzat Tiedje ,  SCHREIER, John David ,  HARTINGH, Timothy John ,  SHIPE, William, D. ,  BUNDA, Jaime Lynn

IPC: A61K31/235 ,  A61K31/66

CPC classification number: A61K31/235 ,  A61K31/66 ,  A61K45/06 ,  A61K2300/00

Abstract: Tricyclic compounds of Formula I are inhibitors of HIV integrase and inhibitors of HIV replication: (I), wherein R 1A, R 1B, R 1C, R 2A , R 2B , R 3A , R 3B , R 4 , R 5 and R 6 are defined herein. The compounds are useful for the prophylaxis or treatment of infection by HIV and the prophylaxis, treatment, or delay in the onset of AIDS. The compounds are employed against HIV infection and AIDS as compounds per se or in the form of pharmaceutically acceptable salts. The compounds and their salts can be employed as ingredients in pharmaceutical compositions, optionally in combination with other antivirals, immunomodulators, antibiotics or vaccines.

Abstract translation: 式I的三环化合物是HIV整合酶和HIV复制抑制剂的抑制剂：（I），其中R1A，R1B，R1C，R2A，R2B，R3A，R3B，R4，R5和R6如本文所定义。 该化合物可用于预防或治疗艾滋病毒感染以及艾滋病的预防，治疗或延迟。 这些化合物被用作抗HIV感染和艾滋病作为化合物本身或以药学上可接受的盐的形式。 化合物及其盐可以用作药物组合物中的成分，任选与其它抗病毒剂，免疫调节剂，抗生素或疫苗组合使用。

公开(公告)号：WO2011041280A2

公开(公告)日：2011-04-07

申请号：PCT/US2010050474

申请日：2010-09-28

Applicant: WILSON JOHN JR ,  BERGER RICHARD C ,  GIULIANO JOHN P ,  STEELE THOMAS C

Inventor： WILSON JOHN JR ,  BERGER RICHARD C ,  GIULIANO JOHN P ,  STEELE THOMAS C

IPC: F16M13/00

CPC classification number: F16M5/00 ,  F24F1/60 ,  F24F13/32

Abstract: An adjustable equipment curb has upper and lower frames, each having opposed first and second length-adjustable sides and opposed length-adjustable first and second ends interconnectable to form a rigid frame and height-adjustable mounting legs. The lower frame may be used alone, or may support the upper frame through a shock mount system having mounts affixed to both the upper and lower frames and shock absorbing springs between the mounts. The frames may be formed of interconnecting channel members, and the lower frame channel members may be of a perforated construction that, in conjunction with applied sheathing, provides acoustic damping. Seismic brackets may be affixed to the either of the frames to provide resist seismic shock and developed moment resistance.

Abstract translation: 可调设备路缘具有上框架和下框架，每个框架具有相对的第一和第二长度可调侧面，并且相对的长度可调节的第一和第二端部可互连以形成刚性框架和高度可调节的安装支腿。 下框架可以单独使用，或者可以通过具有固定到上框架和下框架上的安装件和安装件之间的减震弹簧的冲击安装系统来支撑上框架。 框架可以由互连通道构件形成，并且下框架通道构件可以是穿孔结构，其结合施加的护套提供声阻尼。 地震支架可以固定在任一框架上，以提供抗震震动和抗冲击力。

公开(公告)号：WO2005113484A1

公开(公告)日：2005-12-01

申请号：PCT/US2005/015949

申请日：2005-05-09

Applicant: MERCK & CO., INC. ,  COBURN, Craig, A. ,  STEELE, Thomas, G. ,  VACCA, Joseph, P. ,  ANNIS, David, Allen, Jr. ,  MAKARA, Gergely, M. ,  NASH, Huw, M. ,  TADIKONDA, Praveen, K. ,  WANG, Tong

Inventor： COBURN, Craig, A. ,  STEELE, Thomas, G. ,  VACCA, Joseph, P. ,  ANNIS, David, Allen, Jr. ,  MAKARA, Gergely, M. ,  NASH, Huw, M. ,  TADIKONDA, Praveen, K. ,  WANG, Tong

IPC: C07C233/05

CPC classification number: C07C235/84 ,  C07C255/57 ,  C07C309/67

Abstract: The present invention is directed to phenyl carboxamide compounds which are inhibitors of the beta-secretase enzyme and that are useful in the treatment of diseases in which the beta-secretase enzyme is involved, such as Alzheimer's disease. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the treatment of such diseases in which the beta-secretase enzyme is involved.

Abstract translation: 本发明涉及作为β-分泌酶的抑制剂并且可用于治疗其中涉及β-分泌酶的疾病如阿尔茨海默氏病的苯甲酰胺化合物。 本发明还涉及包含这些化合物的药物组合物以及这些化合物和组合物在治疗涉及β-分泌酶的疾病中的用途。

公开(公告)号：WO1994028230A1

公开(公告)日：1994-12-08

申请号：PCT/US1994006191

申请日：1994-06-01

Applicant: BIOCONVERSION TECHNOLOGIES, INC. ,  FUQUA, Clark ,  STEELE, Thomas, D.

Inventor： BIOCONVERSION TECHNOLOGIES, INC.

IPC: D06M16/00

CPC classification number: G05D21/02 ,  A61L2/18 ,  A61L11/00 ,  B09B3/0075

Abstract: Microorganisms, including both viruses and bacteria, which are found in or on infectious waste (12) are destroyed via enzymatic activity in an enzyme tank (10). A system controller (14) is used to adjust the pH and temperature conditions within the enzyme tank (10) to optimize the killing capacity for the enzymes used in tank (10). Treated waste has zero or substantially reduced numbers of viable microorganisms and can safely be disposed of using sewage systems and landfilling. In addition, the treatment process can substantially reduce the volume of waste material.

Abstract translation: 在酶罐（10）中通过酶活性破坏在感染性废物（12）中或其上发现的包括病毒和细菌在内的微生物。 系统控制器（14）用于调节酶罐（10）内的pH和温度条件，以优化用于罐（10）中的酶的杀伤能力。 经处理的废物的活微生物数量零或大幅度减少，并且可以安全地使用污水系统和填埋进行处置。 此外，处理过程可以显着地减少废料的体积。

公开(公告)号：WO2014099586A1

公开(公告)日：2014-06-26

申请号：PCT/US2013/074590

申请日：2013-12-12

Applicant: MERCK SHARP & DOHME CORP. ,  EMBREY, Mark, W. ,  GRAHAM, Thomas, H. ,  WALJI, Abbas ,  WADDELL, Sherman, T. ,  YU, Tao ,  ZHANG, Yonglian ,  LIU, Wensheng ,  COLEMAN, Paul, J. ,  WAI, John ,  STEELE, Thomas ,  DI MARCO, Christina

Inventor： EMBREY, Mark, W. ,  GRAHAM, Thomas, H. ,  WALJI, Abbas ,  WADDELL, Sherman, T. ,  YU, Tao ,  ZHANG, Yonglian ,  LIU, Wensheng ,  COLEMAN, Paul, J. ,  WAI, John ,  STEELE, Thomas ,  DI MARCO, Christina

IPC: C07D498/04

CPC classification number: C07D471/04 ,  A61K31/4985 ,  A61K31/53 ,  A61K31/55 ,  A61K31/675 ,  A61K45/06 ,  C07D471/10 ,  C07D471/14 ,  C07D471/20 ,  C07D491/20 ,  C07D495/20 ,  C07D498/14 ,  C07F9/6521

Abstract: The present invention relates to 4-Pyridinonetriazine Derivatives of Formula (I); and pharmaceutically acceptable salts thereof, wherein A, X, Y, R 1 , R 2 , R 3 and R 5 are as defined herein. The present invention also relates to compositions comprising at least one 4-Pyridinonetriazine Derivative, and methods of using the 4-Pyridinonetriazine Derivatives for treating or preventing HIV infection in a subject.

Abstract translation: 本发明涉及式（I）的4-吡啶酮三嗪衍生物; 其中A，X，Y，R 1，R 2，R 3和R 5如本文所定义。 本发明还涉及包含至少一种4-吡啶酮三嗪衍生物的组合物，以及使用4-吡啶酮三嗪衍生物治疗或预防受试者中HIV感染的方法。

公开(公告)号：WO2012082578A2

公开(公告)日：2012-06-21

申请号：PCT/US2011/064320

申请日：2011-12-12

Applicant: CYTEC TECHNOLOGY CORP. ,  SAMUELS, Sari-Beth ,  STEELE, Thomas ,  ENG, J. Mon, Hei ,  GUPTA, Ram ,  PENG, Lingqing

Inventor： SAMUELS, Sari-Beth ,  STEELE, Thomas ,  ENG, J. Mon, Hei ,  GUPTA, Ram ,  PENG, Lingqing

IPC: C08J3/20

CPC classification number: B29C41/04 ,  C08K5/00 ,  C08K5/005 ,  C08K5/1545 ,  C08K5/34 ,  C08K5/51 ,  C08L23/0815 ,  Y02P20/124 ,  C08L23/02

Abstract: The cycle time of polymer compositions subjected to a rotomolding process is improved {i.e., reduced), while the processing window is simultaneously enlarged through the use of a polymer-stabilizing amount of a processing stabilizer system having at least one chroman-based compound according to Formula V:

Abstract translation: 经受滚塑过程的聚合物组合物的循环时间得到改善（即减少），同时通过使用聚合物稳定化量的具有至少一种苯并二氢吡喃基化合物的加工稳定剂体系同时扩大加工窗口，根据 公式V：

公开(公告)号：WO2012054366A3

公开(公告)日：2012-04-26

申请号：PCT/US2011/056504

申请日：2011-10-17

Applicant: MERCK SHARP & DOHME CORP. ,  SHIPPS, Gerald, W., Jr. ,  SAUVAGNAT, Berenegere ,  BRACKEN, Jack ,  MCELROY, William, T. ,  COX, Christopher, D. ,  HO, Ginny ,  MCGAUGHEY, Georgia ,  DENG, Yongqi ,  ZHU, Liang ,  DUDKIN, Vadim ,  STEELE, Thomas, G. ,  STEEN, Justin, T.

Inventor： SHIPPS, Gerald, W., Jr. ,  SAUVAGNAT, Berenegere ,  BRACKEN, Jack ,  MCELROY, William, T. ,  COX, Christopher, D. ,  HO, Ginny ,  MCGAUGHEY, Georgia ,  DENG, Yongqi ,  ZHU, Liang ,  DUDKIN, Vadim ,  STEELE, Thomas, G. ,  STEEN, Justin, T.

IPC: A01N43/64 ,  A61K31/41

Abstract: The present invention is directed to substituted amino-triazolyl compounds which are useful as therapeutic agents for the treatment of central nervous system disorders associated with phosphodiesterase 10 (PDE10). The present invention also relates to the use of such compounds for treating neurological and psychiatric disorders, such as schizophrenia, psychosis or Huntington's disease, and those associated with striatal hypofunction or basal ganglia dysfunction.

公开(公告)号：WO2009120652A2

公开(公告)日：2009-10-01

申请号：PCT/US2009/038013

申请日：2009-03-24

Applicant: MERCK & CO., INC. ,  SELNICK, Harold, G. ,  BELL, Ian, M. ,  MCWHERTER, Melody ,  STAAS, Donnette, D. ,  STACHEL, Shawn, J. ,  STEELE, Thomas ,  STUMP, Craig ,  WOOD, Michael, R. ,  ZARTMAN, C., Blair

Inventor： SELNICK, Harold, G. ,  BELL, Ian, M. ,  MCWHERTER, Melody ,  STAAS, Donnette, D. ,  STACHEL, Shawn, J. ,  STEELE, Thomas ,  STUMP, Craig ,  WOOD, Michael, R. ,  ZARTMAN, C., Blair

IPC: C07D491/10

CPC classification number: C07D471/10 ,  C07D403/06 ,  C07D471/20 ,  C07D519/00

Abstract: The present invention is directed to compounds of the formula (I) : (wherein variables A 1 , A 2 , A 3 , A 4 , A 5 , A 6 , A 7 , A 8 , G 1 , G 2 , G 3 , G 4 , J, Q, E a , E b , E c , R 6 , R 7 , R PG and Y are as described herein) which are antagonists of CGRP receptors and which are useful in the treatment or prevention of diseases in which CGRP is involved, such as migraine. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which CGRP is involved.

Abstract translation: 本发明涉及式（I）的化合物：（其中变量A1，A2，A3，A4，A5，A6，A7，A8，G1，G2，G3，G4，J，Q，Ea，Eb，Ec ，R6，R7，RPG和Y如本文所述），其是CGRP受体的拮抗剂，其可用于治疗或预防涉及CGRP的疾病，例如偏头痛。 本发明还涉及包含这些化合物的药物组合物以及这些化合物和组合物在预防或治疗涉及CGRP的疾病中的用途。

公开(公告)号：WO2015089847A1

公开(公告)日：2015-06-25

申请号：PCT/CN2013/090156

申请日：2013-12-20

Applicant: MERCK SHARP & DOHME CORP. ,  GRAHAM, Thomas H. ,  LIU, Wensheng ,  YU, Tao ,  ZHANG, Yonglian ,  WADDELL, Sherman T. ,  WAI, John S. ,  COLEMAN, Paul J. ,  SANDERS, John M. ,  EMBREY, Mark W. ,  WALJI, Abbas ,  FERGUSON, Ronald Dale II ,  MARCO, Christina Ng Di ,  STEELE, Thomas ,  HU, Lihong ,  PENG, Xuanjia

Inventor： GRAHAM, Thomas H. ,  LIU, Wensheng ,  YU, Tao ,  ZHANG, Yonglian ,  WADDELL, Sherman T. ,  WAI, John S. ,  COLEMAN, Paul J. ,  SANDERS, John M. ,  EMBREY, Mark W. ,  WALJI, Abbas ,  FERGUSON, Ronald Dale II ,  MARCO, Christina Ng Di ,  STEELE, Thomas ,  HU, Lihong ,  PENG, Xuanjia

IPC: C07D471/20 ,  C07D493/20 ,  C07D495/20 ,  C07D471/22 ,  A61K31/499 ,  A61K31/53 ,  A61K31/55 ,  A61P31/18

CPC classification number: A61K31/53 ,  A61K31/427 ,  A61K31/499 ,  A61K31/513 ,  A61K31/52 ,  A61K31/55 ,  A61K31/675 ,  A61K45/06 ,  C07D471/20 ,  C07D471/22 ,  C07D475/10 ,  C07D491/10 ,  C07D491/20 ,  C07D495/10 ,  C07D495/20 ,  C07F9/65616 ,  A61K2300/00

Abstract: Disclosed are Spirocyclic Heterocycle Compounds of Formula (I) and pharmaceutically acceptable salts thereof, where A, B, X, Y, R 1 , R 2 and R 11 are as defined herein. Composition comprising at least one Spirocyclic Heterocycle Compound, and methods of using the Spirocyclic Heterocycle Compounds for treating or preventing HIV infection in a subject are also disclosed.

Abstract translation: 公开了式（I）的螺环杂环化合物及其药学上可接受的盐，其中A，B，X，Y，R 1，R 2和R 11如本文所定义。 还公开了包含至少一种螺环杂环化合物的组合物，以及使用螺环杂环化合物治疗或预防受试者中HIV感染的方法。