公开(公告)号：WO2006002185A8

公开(公告)日：2007-02-22

申请号：PCT/US2005021963

申请日：2005-06-21

Applicant: SMITHKLINE BEECHAM CORP ,  HEYER DENNIS ,  FANG JING ,  NAVAS III FRANK ,  KATAMREDDY SUBBA REDDY ,  PECKHAM JENNIFER POOLE ,  TURNBULL PHILIP STEWART ,  MILLER AARON BAYNE ,  AKWABI-AMEYAW ADWOA

Inventor： HEYER DENNIS ,  FANG JING ,  NAVAS III FRANK ,  KATAMREDDY SUBBA REDDY ,  PECKHAM JENNIFER POOLE ,  TURNBULL PHILIP STEWART ,  MILLER AARON BAYNE ,  AKWABI-AMEYAW ADWOA

IPC: C07C65/26 ,  A61K31/216 ,  A61K31/235 ,  A61P5/30 ,  C07C59/72 ,  C07C235/34 ,  C07C255/54 ,  C07C311/08 ,  C07C311/09 ,  C07C311/21 ,  C07D211/62 ,  C07D295/104 ,  C07F9/38

CPC classification number: C07D213/30 ,  C07C43/295 ,  C07C59/68 ,  C07C59/70 ,  C07C59/72 ,  C07C65/24 ,  C07C69/92 ,  C07C233/25 ,  C07C235/34 ,  C07C235/46 ,  C07C255/54 ,  C07C311/08 ,  C07C311/09 ,  C07C311/21 ,  C07C2601/02 ,  C07D211/62 ,  C07D295/108 ,  C07D295/185 ,  C07D307/42 ,  C07D333/16 ,  C07F9/3826 ,  C07F9/4006

Abstract: The present invention relates to novel compounds with a variety of therapeutic uses, more particularly novel naphthalene 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萘化合物。

公开(公告)号：WO2005012220A9

公开(公告)日：2005-05-19

申请号：PCT/US2004024308

申请日：2004-07-27

Applicant: SMITHKLINE BEECHAM CORP ,  BRITTON JONATHAN E ,  FANG JING ,  HEYER DENNIS ,  MILLER AARON BAYNE ,  NAVAS FRANK III ,  SMALLEY TERRENCE LEE JR ,  ZUERCHER WILLIAM J ,  KATAMREDDY SUBBA REDDY

Inventor： BRITTON JONATHAN E ,  FANG JING ,  HEYER DENNIS ,  MILLER AARON BAYNE ,  NAVAS FRANK III ,  SMALLEY TERRENCE LEE JR ,  ZUERCHER WILLIAM J ,  KATAMREDDY SUBBA REDDY

IPC: C07C39/23 ,  C07C39/42 ,  C07C43/23 ,  C07C45/45 ,  C07C45/46 ,  C07C45/59 ,  C07C45/62 ,  C07C45/67 ,  C07C45/71 ,  C07C47/57 ,  C07C49/403 ,  C07C49/83 ,  C07C49/835 ,  C07C49/84 ,  C07C59/54 ,  C07C59/56 ,  C07C233/25 ,  C07C235/34 ,  C07C235/42 ,  C07C255/13 ,  C07C255/53 ,  C07C311/08 ,  C07C311/21 ,  C07C317/22 ,  C07D207/16 ,  C07D207/32 ,  C07D207/333 ,  C07D211/60 ,  C07D211/62 ,  C07D213/30 ,  C07D239/26 ,  C07D261/08 ,  C07D263/32 ,  C07D295/096 ,  C07D307/42 ,  C07D309/20 ,  C07D309/22 ,  C07D335/02 ,  C07F9/40 ,  C07C59/72 ,  A61K31/165 ,  A61K31/192 ,  A61K31/382 ,  A61K31/40 ,  A61K31/44 ,  C07C43/295 ,  C07F9/142

CPC classification number: C07D207/333 ,  C07C39/23 ,  C07C39/42 ,  C07C43/23 ,  C07C45/45 ,  C07C45/46 ,  C07C45/59 ,  C07C45/62 ,  C07C45/673 ,  C07C45/71 ,  C07C47/57 ,  C07C49/403 ,  C07C49/83 ,  C07C49/835 ,  C07C49/84 ,  C07C59/54 ,  C07C59/56 ,  C07C65/19 ,  C07C233/25 ,  C07C235/34 ,  C07C235/42 ,  C07C255/13 ,  C07C255/53 ,  C07C311/08 ,  C07C311/21 ,  C07C317/22 ,  C07C2601/08 ,  C07C2601/14 ,  C07C2601/18 ,  C07D207/16 ,  C07D211/60 ,  C07D211/62 ,  C07D213/30 ,  C07D239/26 ,  C07D261/08 ,  C07D263/32 ,  C07D295/096 ,  C07D307/42 ,  C07D309/20 ,  C07D309/22 ,  C07D335/02 ,  C07F9/4015

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. Formula (I) including salts, solvates, and pharmacologically functional derivatives thereof wherein R is OH; each of R and R independently are selected from OH, alkyl, or halogen; each of p and q independently are selected from 0, 1, or 2; R is -(Y)z-R ; z is 0 or 1; Y is -C=C- or CR =CR -; X is -(CH2)n- where n is 0, 1, 2, or 3, -C(R )2-, -O-,or -S-.

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。 式（I）包括盐，溶剂合物和其药理学功能衍生物，其中R 1是OH; R 2和R 4各自独立地选自OH，烷基或卤素; p和q各自独立地选自0,1或2; R 3是 - （Y）z -R 6; z为0或1; Y是-C = C-或CR 6 = CR 1 - ; X是 - （CH 2）n - ，其中n是0,1,2或3，-C（R 9）2 - ， - O-或-S-。

公开(公告)号：WO2003027090A3

公开(公告)日：2003-04-03

申请号：PCT/US2002/029298

申请日：2002-09-16

Applicant: SMITHKLINE BEECHAM CORPORATION ,  HAFFNER, Curt, Dale ,  KALDOR, Istvan ,  MCDOUGALD, Darryl, Lynn ,  MILLER, Aaron, Bayne

Inventor： HAFFNER, Curt, Dale ,  KALDOR, Istvan ,  MCDOUGALD, Darryl, Lynn ,  MILLER, Aaron, Bayne

IPC: C07D307/80

Abstract: The present invention includes novel retinoid compounds that have selectivity as RXR agonists on one or more isoforms of RXR, currently, RXRα RXRβ, or RXRγ. The present compounds, an d ph armaceutical compositions incorporating these compounds, therefore, are effective in treating conditions mediated by RXRs. Among other physiological responses, the compounds of the present invention reduce blood glucose and maintain body weight, and, thus, are useful for the treatment of diabetes (NIDDIM) and obesity

公开(公告)号：WO2006002185A1

公开(公告)日：2006-01-05

申请号：PCT/US2005/021963

申请日：2005-06-21

Applicant: SMITHKLINE BEECHAM CORPORATION ,  HEYER, Dennis ,  FANG, Jing ,  NAVAS III, Frank ,  KATAMREDDY, Subba, Reddy ,  PECKHAM, Jennifer, Poole ,  TURNBULL, Philip, Stewart ,  MILLER, Aaron, Bayne ,  AKWABI-AMEYAW, Adwoa

Inventor： HEYER, Dennis ,  FANG, Jing ,  NAVAS III, Frank ,  KATAMREDDY, Subba, Reddy ,  PECKHAM, Jennifer, Poole ,  TURNBULL, Philip, Stewart ,  MILLER, Aaron, Bayne ,  AKWABI-AMEYAW, Adwoa

IPC: C07C65/26

CPC classification number: C07D213/30 ,  C07C43/295 ,  C07C59/68 ,  C07C59/70 ,  C07C59/72 ,  C07C65/24 ,  C07C69/92 ,  C07C233/25 ,  C07C235/34 ,  C07C235/46 ,  C07C255/54 ,  C07C311/08 ,  C07C311/09 ,  C07C311/21 ,  C07C2601/02 ,  C07D211/62 ,  C07D295/108 ,  C07D295/185 ,  C07D307/42 ,  C07D333/16 ,  C07F9/3826 ,  C07F9/4006

Abstract: The present invention relates to novel compounds with a variety of therapeutic uses, more particularly novel naphthalene 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萘化合物。

公开(公告)号：WO2002061089A2

公开(公告)日：2002-08-08

申请号：PCT/US2002/002992

申请日：2002-01-31

Applicant: SMITHKLINE BEECHAM CORPORATION ,  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: C12N15/12

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：WO2005012220A3

公开(公告)日：2005-02-10

申请号：PCT/US2004/024308

申请日：2004-07-27

Applicant: SMITHKLINE BEECHAM CORPORATION ,  BRITTON, Jonathan, E. ,  FANG, Jing ,  HEYER, Dennis ,  MILLER, Aaron, Bayne ,  NAVAS, Frank, III ,  SMALLEY, Terrence, Lee, Jr. ,  ZUERCHER, William, J. ,  KATAMREDDY, Subba, Reddy

Inventor： BRITTON, Jonathan, E. ,  FANG, Jing ,  HEYER, Dennis ,  MILLER, Aaron, Bayne ,  NAVAS, Frank, III ,  SMALLEY, Terrence, Lee, Jr. ,  ZUERCHER, William, J. ,  KATAMREDDY, Subba, Reddy

IPC: C07C59/72

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. Formula (I) including salts, solvates, and pharmacologically functional derivatives thereof wherein R 1 is OH; each of R 2 and R 4 independently are selected from OH, alkyl, or halogen; each of p and q independently are selected from 0, 1, or 2; R 3 is -(Y) z -R 6 ; z is 0 or 1; Y is -C=C- or CR 6 =CR 1 -; X is -(CH 2 ) n - where n is 0, 1, 2, or 3, -C(R 9 ) 2 -, -O-,or -S-.

公开(公告)号：WO2005012220A2

公开(公告)日：2005-02-10

申请号：PCT/US2004024308

申请日：2004-07-27

Applicant: SMITHKLINE BEECHAM CORP ,  BRITTON JONATHAN E ,  FANG JING ,  HEYER DENNIS ,  MILLER AARON BAYNE ,  NAVAS FRANK III ,  SMALLEY TERRENCE LEE JR ,  ZUERCHER WILLIAM J ,  KALAMREDDY SUBBA REDDY

Inventor： BRITTON JONATHAN E ,  FANG JING ,  HEYER DENNIS ,  MILLER AARON BAYNE ,  NAVAS FRANK III ,  SMALLEY TERRENCE LEE JR ,  ZUERCHER WILLIAM J ,  KALAMREDDY SUBBA REDDY

IPC: C07C39/23 ,  C07C39/42 ,  C07C43/23 ,  C07C45/45 ,  C07C45/46 ,  C07C45/59 ,  C07C45/62 ,  C07C45/67 ,  C07C45/71 ,  C07C47/57 ,  C07C49/403 ,  C07C49/83 ,  C07C49/835 ,  C07C49/84 ,  C07C59/54 ,  C07C59/56 ,  C07C233/25 ,  C07C235/34 ,  C07C235/42 ,  C07C255/13 ,  C07C255/53 ,  C07C311/08 ,  C07C311/21 ,  C07C317/22 ,  C07D207/16 ,  C07D207/32 ,  C07D207/333 ,  C07D211/60 ,  C07D211/62 ,  C07D213/30 ,  C07D239/26 ,  C07D261/08 ,  C07D263/32 ,  C07D295/096 ,  C07D307/42 ,  C07D309/20 ,  C07D309/22 ,  C07D335/02 ,  C07F9/40 ,  C07C59/00

CPC classification number: C07D207/333 ,  C07C39/23 ,  C07C39/42 ,  C07C43/23 ,  C07C45/45 ,  C07C45/46 ,  C07C45/59 ,  C07C45/62 ,  C07C45/673 ,  C07C45/71 ,  C07C47/57 ,  C07C49/403 ,  C07C49/83 ,  C07C49/835 ,  C07C49/84 ,  C07C59/54 ,  C07C59/56 ,  C07C65/19 ,  C07C233/25 ,  C07C235/34 ,  C07C235/42 ,  C07C255/13 ,  C07C255/53 ,  C07C311/08 ,  C07C311/21 ,  C07C317/22 ,  C07C2601/08 ,  C07C2601/14 ,  C07C2601/18 ,  C07D207/16 ,  C07D211/60 ,  C07D211/62 ,  C07D213/30 ,  C07D239/26 ,  C07D261/08 ,  C07D263/32 ,  C07D295/096 ,  C07D307/42 ,  C07D309/20 ,  C07D309/22 ,  C07D335/02 ,  C07F9/4015

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：WO2003062192A1

公开(公告)日：2003-07-31

申请号：PCT/US2003/001271

申请日：2003-01-15

Applicant: SMITHKLINE BEECHAM CORPORATION ,  CATALANO, John, George ,  DEATON, David, Norman ,  MILLER, Aaron, Bayne ,  TAVARES, Francis, Xavier

Inventor： CATALANO, John, George ,  DEATON, David, Norman ,  MILLER, Aaron, Bayne ,  TAVARES, Francis, Xavier

IPC: C07C271/34

CPC classification number: C07D213/30 ,  C07C271/22 ,  C07C271/34 ,  C07C275/16 ,  C07C2601/04 ,  C07C2601/08 ,  C07C2601/14 ,  C07D213/40 ,  C07D231/40 ,  C07D233/84 ,  C07D237/14 ,  C07D239/34 ,  C07D239/38 ,  C07D239/42 ,  C07D263/58 ,  C07D277/24 ,  C07D277/34 ,  C07D285/08 ,  C07D295/215 ,  C07D417/12 ,  C07D495/04

Abstract: Cycloalkyl ketoamide derivatives, which are useful as cathepsin K inhibitors are described herein. The described invention also includes methods of making such cycloalkyl 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抑制剂的环烷基酮酰胺衍生物。 所描述的发明还包括制备这种环烷酮酮酰胺衍生物的方法以及使用该方法来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。

公开(公告)号：WO2003027090A2

公开(公告)日：2003-04-03

申请号：PCT/US2002/029298

申请日：2002-09-16

Applicant: SMITHKLINE BEECHAM CORPORATION ,  HAFFNER, Curt, Dale ,  KALDOR, Istvan ,  MCDOUGALD, Darryl, Lynn ,  MILLER, Aaron, Bayne

Inventor： HAFFNER, Curt, Dale ,  KALDOR, Istvan ,  MCDOUGALD, Darryl, Lynn ,  MILLER, Aaron, Bayne

IPC: C07D307/80

CPC classification number: C07D263/56 ,  C07D307/54 ,  C07D333/24 ,  C07D333/60 ,  C07D409/04 ,  C07D491/04

Abstract: The present invention includes novel retinoid compounds that have selectivity as RXR agonists on one or more isoforms of RXR, currently, RXRα RXRβ, or RXRγ. The present compounds, an d ph armaceutical compositions incorporating these compounds, therefore, are effective in treating conditions mediated by RXRs. Among other physiological responses, the compounds of the present invention reduce blood glucose and maintain body weight, and, thus, are useful for the treatment of diabetes (NIDDIM) and obesity

Abstract translation: 本发明包括在RXR，目前为RXRαRRRβ或RXRγ的一种或多种异构体上具有选择性作为RXR激动剂的新型维甲酸化合物。 因此，本发明化合物是掺入这些化合物的d药物组合物可有效治疗RXR介导的病症。 在其他生理反应中，本发明的化合物降低血糖并维持体重，因此可用于治疗糖尿病（NIDDIM）和肥胖

公开(公告)号：WO2008030771A1

公开(公告)日：2008-03-13

申请号：PCT/US2007/077356

申请日：2007-08-31

Applicant: SMITHKLINE BEECHAM CORPORATION ,  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颖化合物，更具体地涉及对选择性雌激素受体调节特别有用的新型取代的环状亚烷基化合物。