公开(公告)号：WO2005082857A1

公开(公告)日：2005-09-09

申请号：PCT/US2005/005467

申请日：2005-02-22

Applicant: SMITHKLINE BEECHAM CORPORATION ,  HOEKSTRA, William, Joel ,  MILLER, Aaron, Bayne ,  ZUERCHER, William, John ,  PATEL, Harikrishna, Suryakant

Inventor： HOEKSTRA, William, Joel ,  MILLER, Aaron, Bayne ,  ZUERCHER, William, John ,  PATEL, Harikrishna, Suryakant

IPC: C07D215/36

CPC classification number: C07D215/233 ,  C07C59/68 ,  C07D215/36

Abstract: The present invention relates to novel compounds of Formula (I) with a variety of therapeutic uses, more particularly novel substituted quinoline compounds particularly useful for selective estrogen receptor modulation.

Abstract translation: 本发明涉及具有多种治疗用途的新型式（I）化合物，更特别地涉及特别用于选择性雌激素受体调节的新颖取代的喹啉化合物。

公开(公告)号：WO2003086385A1

公开(公告)日：2003-10-23

申请号：PCT/US2003/009893

申请日：2003-04-01

Applicant: SMITHKLINE BEECHAM CORPORATION ,  BARRETT, David, Gene ,  CATALANO, John, G. ,  DEATON, David, Norman ,  MILLER, Aaron, Bayne ,  RAY, John, A ,  SAMANO, Vicente

Inventor： BARRETT, David, Gene ,  CATALANO, John, G. ,  DEATON, David, Norman ,  MILLER, Aaron, Bayne ,  RAY, John, A ,  SAMANO, Vicente

IPC: A61K31/341

CPC classification number: C07D207/27 ,  C07D207/12 ,  C07D207/273 ,  C07D207/48 ,  C07D307/20 ,  C07D307/33 ,  C07D401/06 ,  C07D403/06 ,  C07D403/12 ,  C07D405/06 ,  C07D405/12 ,  C07D409/06 ,  C07D409/12 ,  C07D413/06 ,  C07D413/12 ,  C07D413/14 ,  C07D417/06 ,  C07D417/12 ,  C07D417/14

Abstract: Heterocycle substituted ketoamide derivatives of Formula (I), wherein the substitutes A, D, Z and R are defined as in claim 1, which are useful as cathepsin K inhibitors are described herein. The described invention also includes methods of making such heterocycle substituted ketoamide derivatives as well as methods of using the same in the manufacture of medicaments for the treatment of disorders, including osteoporosis, associated with an imbalance between bone resorption and formation which can ultimately lead to fracture.

Abstract translation: 式（I）的杂环取代的酮酰胺衍生物，其中取代基A，D，Z和R如权利要求1中所定义，其可用作组织蛋白酶K抑制剂。 所描述的发明还包括制备这种杂环取代的酮酰胺衍生物的方法以及在制备用于治疗与骨吸收和形成之间的不平衡相关的障碍（包括骨质疏松症）的药物中的药物的方法，其可能最终导致骨折 。

公开(公告)号：WO2003034028A3

公开(公告)日：2003-04-24

申请号：PCT/US2002/032917

申请日：2002-10-16

Applicant: SMITHKLINE BEECHAM CORPORATION ,  BLANCHARD, Steven, G. ,  MILLER, Aaron, Bayne ,  ORBAND-MILLER, Lisa, A.

Inventor： BLANCHARD, Steven, G. ,  MILLER, Aaron, Bayne ,  ORBAND-MILLER, Lisa, A.

IPC: C12N15/12

Abstract: Methods of identifying compounds that interact with ERRy and are useful in the treatment of ERRy- and ER-mediated diseases, risk factors, and conditions are provided. Pharmaceutical compositions containing compounds that interact directly with ERRy and methods of using these compositions in the treatment of ERRy- and ER-mediated diseases, risk factors, and conditions are also provided.

公开(公告)号：WO2008030771A8

公开(公告)日：2008-05-15

申请号：PCT/US2007077356

申请日：2007-08-31

Applicant: SMITHKLINE BEECHAM CORP ,  ZUERCHER WILLIAM JOHN ,  HEYER DENNIS ,  MILLER AARON BAYNE

Inventor： ZUERCHER WILLIAM JOHN ,  HEYER DENNIS ,  MILLER AARON BAYNE

IPC: C07C39/42 ,  C07C43/20 ,  C07C217/12

CPC classification number: C07C217/18 ,  C07C2601/14 ,  C07C2601/18

Abstract: The present invention relates to novel compounds with a variety of therapeutic uses, more particularly novel substituted cyclic alkylidene compounds that are particularly useful for selective estrogen receptor modulation.

Abstract translation: 本发明涉及具有多种治疗用途的新化合物，更特别地涉及特别适用于选择性雌激素受体调节的新型取代的环亚烷基化合物。

公开(公告)号：WO02061089A3

公开(公告)日：2003-10-16

申请号：PCT/US0202992

申请日：2002-01-31

Applicant: SMITHKLINE BEECHAM CORP ,  DAVIS RODERICK GERALD ,  JOHNSON ROBERT LLOYD JR ,  MILLER AARON BAYNE ,  MILLER ANN BRIER ,  WAY JAMES M ,  WILLIAMS SHAWN P ,  WILLSON TIMOTHY MARK ,  WISELY GEORGE BRUCE

Inventor： DAVIS RODERICK GERALD ,  JOHNSON ROBERT LLOYD JR ,  MILLER AARON BAYNE ,  MILLER ANN BRIER ,  WAY JAMES M ,  WILLIAMS SHAWN P ,  WILLSON TIMOTHY MARK ,  WISELY GEORGE BRUCE

IPC: C07K14/47 ,  C07K14/72 ,  C12N15/12 ,  G01N33/48 ,  G01N33/50 ,  G06F19/00 ,  G01N33/68

CPC classification number: C07K14/4702 ,  C07K2299/00

Abstract: A solved three-dimensional crystal structure of an HNF4g ligand binding domain polypeptide is disclosed, along with a crystal form of the HNF4g ligand binding domain. Methods of designing modulators of the biological activity of HNF4g, and other HNF4 ligand binding domain polypeptides are also disclosed

Abstract translation: 公开了HNF4g配体结合结构域多肽的解决的三维晶体结构以及HNF4g配体结合结构域的晶体形式。 还公开了设计HNF4g和其他HNF4配体结合域多肽的生物学活性调节剂的方法

公开(公告)号：WO2003034028A2

公开(公告)日：2003-04-24

申请号：PCT/US2002/032917

申请日：2002-10-16

Applicant: SMITHKLINE BEECHAM CORPORATION ,  BLANCHARD, Steven, G. ,  MILLER, Aaron, Bayne ,  ORBAND-MILLER, Lisa, A.

Inventor： BLANCHARD, Steven, G. ,  MILLER, Aaron, Bayne ,  ORBAND-MILLER, Lisa, A.

IPC: G01N

CPC classification number: G01N33/743 ,  G01N33/574 ,  G01N2333/70567 ,  G01N2500/04 ,  G01N2800/108 ,  G01N2800/32 ,  G01N2800/362

Abstract: Methods of identifying compounds that interact with ERRy and are useful in the treatment of ERRy- and ER-mediated diseases, risk factors, and conditions are provided. Pharmaceutical compositions containing compounds that interact directly with ERRy and methods of using these compositions in the treatment of ERRy- and ER-mediated diseases, risk factors, and conditions are also provided.

Abstract translation: 提供了识别与ERRy相互作用并可用于治疗ERR-和ER介导的疾病，危险因素和病症的化合物的方法。 还提供了含有与ERRy直接相互作用的化合物的药物组合物和使用这些组合物治疗ERR-和ER介导的疾病，危险因素和病症的方法。

公开(公告)号：WO2003013518A1

公开(公告)日：2003-02-20

申请号：PCT/US2002/023255

申请日：2002-07-23

Applicant: SMITHKLINE BEECHAM CORPORATION ,  SAMANO, Vicente ,  BARRETT, David, Gene ,  DEATON, David, Norman ,  MCFADYEN, Robert, Blount ,  MILLER, Aaron, Bayne ,  RAY, John, Albert ,  TAVARES, Francis, Xavier ,  ZHOU, Huiqiang

Inventor： BARRETT, David, Gene ,  DEATON, David, Norman ,  MCFADYEN, Robert, Blount ,  MILLER, Aaron, Bayne ,  RAY, John, Albert ,  TAVARES, Francis, Xavier ,  ZHOU, Huiqiang

IPC: A61K31/4245

CPC classification number: C07D233/64 ,  C04B35/632 ,  C07D231/12 ,  C07D231/40 ,  C07D233/56 ,  C07D249/08 ,  C07D271/10 ,  C07D285/12 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D409/12 ,  C07D413/12 ,  C07D413/14 ,  C07D417/12 ,  C07D417/14

Abstract: Biaryl ketoamide derivatives (I), which are useful as cathepsin K inhibitors are described herein. The described invention also includes methods of making such biaryl ketoamide derivatives as well as methods of using the same in the treatment of disorders, including osteoporosis, associated with enhanced bone turnover which can ultimately lead to fracture.

Abstract translation: 本文描述了可用作组织蛋白酶K抑制剂的双芳酮酮酰胺衍生物（I）。 所描述的发明还包括制备这种联芳基酮酰胺衍生物的方法以及用于治疗与骨质疏松增加相关的障碍（包括骨质疏松症）的方法，其可能最终导致骨折。