公开(公告)号：WO2008061029A1

公开(公告)日：2008-05-22

申请号：PCT/US2007/084321

申请日：2007-11-09

Applicant: WYETH ,  MEWSHAW, Richard, Eric ,  YANG, Cuijian ,  EDSALL, Richard ,  MOORE, William, Jay ,  KERN, Jeffrey, Curtis ,  DIFFENDAL, Jason, Michael ,  TRYBULSKI, Eugene, John ,  WILSON, Matthew, Alan ,  WELMAKER, Gregory, Scott

Inventor： MEWSHAW, Richard, Eric ,  YANG, Cuijian ,  EDSALL, Richard ,  MOORE, William, Jay ,  KERN, Jeffrey, Curtis ,  DIFFENDAL, Jason, Michael ,  TRYBULSKI, Eugene, John ,  WILSON, Matthew, Alan ,  WELMAKER, Gregory, Scott

IPC: C07D335/10 ,  C07D335/16 ,  C07D337/14 ,  C07D327/08 ,  C07D409/12 ,  C07D411/12 ,  C07D417/12 ,  A61K31/5415 ,  A61P19/00

CPC classification number: C07D335/10 ,  C07D327/08 ,  C07D335/16 ,  C07D337/14 ,  C07D409/12 ,  C07D411/12 ,  C07D417/12

Abstract: Compounds of formula (I) and pharmaceutically acceptable salt thereof, which are modulators of secreted frizzled related protein-1, are disclosed. The compounds, and compositions containing the compounds, can be used to treat various diseases and disorders, including osteoporosis, arthritis, chronic obstructive pulmonary disease, cartilage defects, bone fractures, leiomyoma, acute myeloid leukemia, wound healing, prostate cancer, autoimmune inflammatory disorders, such as Graves ophthalmopathy, and combinations thereof.

Abstract translation: 公开了式（I）化合物及其药学上可接受的盐，其是分泌的卷曲相关蛋白-1的调节剂。 化合物和含有这些化合物的组合物可用于治疗各种疾病和病症，包括骨质疏松症，关节炎，慢性阻塞性肺病，软骨缺损，骨折，平滑肌瘤，急性骨髓性白血病，伤口愈合，前列腺癌，自身免疫性炎症性疾病 ，如格雷夫斯眼病，及其组合。

公开(公告)号：WO2008073936A1

公开(公告)日：2008-06-19

申请号：PCT/US2007/087077

申请日：2007-12-11

Applicant: WYETH ,  ZELLE, Robert ,  MAZDIYASNI, Hormoz ,  GALULLO, Vincent ,  BAKER, Christopher, Todd ,  WILL, Paul ,  GUO, Jinsong ,  SOENEN, Danielle ,  FENSOME, Andrew ,  KERN, Jeffrey, Curtis ,  MOORE, William, Jay ,  MELENSKI, Edward, George ,  KAPLAN, Justin

Inventor： ZELLE, Robert ,  MAZDIYASNI, Hormoz ,  GALULLO, Vincent ,  BAKER, Christopher, Todd ,  WILL, Paul ,  GUO, Jinsong ,  SOENEN, Danielle ,  FENSOME, Andrew ,  KERN, Jeffrey, Curtis ,  MOORE, William, Jay ,  MELENSKI, Edward, George ,  KAPLAN, Justin

IPC: C07D213/36 ,  C07D213/74 ,  C07D277/42 ,  A61K31/435 ,  A61K31/426 ,  A61P9/00

CPC classification number: C07D213/36 ,  C07D213/74 ,  C07D277/42

Abstract: The present teachings provide compounds of Formula (I) wherein Ar, R 1 , R 2 , R 3 , X, p and n are defined herein. The present teachings also provide processes for producing said compounds and methods of treating a pathological condition or disorder, or alleviating a symptom thereof, using said compounds. The compounds can be useful in modulating ion channel activity including treating a variety of conditions associated with the abnormal modulation of one or more voltage-gated calcium channels.

Abstract translation: 本发明提供式（I）的化合物，其中Ar，R 1，R 2，R 3，X，p和n被定义 于此。 本教导还提供了使用所述化合物生产所述化合物的方法和治疗病理状况或病症或缓解其症状的方法。 该化合物可用于调节离子通道活性，包括治疗与一个或多个电压门控钙通道的异常调节相关的多种病症。

公开(公告)号：WO2008073929A1

公开(公告)日：2008-06-19

申请号：PCT/US2007/087060

申请日：2007-12-11

Applicant: WYETH ,  GALULLO, Vincent P. ,  ZELLE, Robert ,  SOENEN, Danielle ,  BAKER, Christopher, Todd ,  WILL, Paul ,  MAZDIYASNI, Hormoz ,  GUO, Jinsong ,  FENSOME, Andrew ,  KERN, Jeffrey, Curtis ,  MOORE, William, Jay ,  MELENSKI, Edward, George ,  KAPLAN, Justin

Inventor： GALULLO, Vincent P. ,  ZELLE, Robert ,  SOENEN, Danielle ,  BAKER, Christopher, Todd ,  WILL, Paul ,  MAZDIYASNI, Hormoz ,  GUO, Jinsong ,  FENSOME, Andrew ,  KERN, Jeffrey, Curtis ,  MOORE, William, Jay ,  MELENSKI, Edward, George ,  KAPLAN, Justin

IPC: C07D213/72 ,  C07D277/42 ,  A61K31/435 ,  A61K31/426 ,  A61P9/00

CPC classification number: C07D213/72 ,  C07D277/42

Abstract: The present teachings provide compounds of Formula (I): and pharmaceutically acceptable salts, hydrates, and esters thereof, wherein Ar, R 1 , R 2 , R 3 , p, and X are defined herein. The present teachings also provide processes for producing said compounds and their pharmaceutically acceptable salts, hydrates and esters, and methods of treating a pathological condition or disorder, or alleviating a symptom thereof, using said compounds including their pharmaceutically acceptable salts, hydrates and esters. The compounds can be useful in modulating ion channel activity including treating a variety of conditions associated with the abnormal modulation of one or more voltage-gated calcium channels.

Abstract translation: 本发明提供式（I）化合物及其药学上可接受的盐，水合物和酯，其中Ar，R 1，R 2，R 3， 这里定义了p，X。 本教导还提供使用所述化合物，包括其药学上可接受的盐，水合物和酯来制备所述化合物及其药学上可接受的盐，水合物和酯的方法，以及治疗病理状况或病症或减轻其症状的方法。 该化合物可用于调节离子通道活性，包括治疗与一个或多个电压门控钙通道的异常调节相关的多种病症。

公开(公告)号：WO2008060998A1

公开(公告)日：2008-05-22

申请号：PCT/US2007/084245

申请日：2007-11-09

Applicant: WYETH ,  WELMAKER, Gregory, Scott ,  WILSON, Matthew, Alan ,  MOORE, William, Jay ,  KERN, Jeffrey, Curtis ,  TRYBULSKI, Eugene, John

Inventor： WELMAKER, Gregory, Scott ,  WILSON, Matthew, Alan ,  MOORE, William, Jay ,  KERN, Jeffrey, Curtis ,  TRYBULSKI, Eugene, John

IPC: C07D209/30 ,  C07D401/12 ,  C07D403/12 ,  C07D405/12 ,  C07D409/12 ,  A61K31/404 ,  A61P19/00 ,  A61P19/02 ,  A61P19/10

CPC classification number: C07D401/12 ,  C07D209/30 ,  C07D403/12 ,  C07D405/12 ,  C07D409/12

Abstract: Indole sulfonamide compounds or pharmaceutically acceptable salts thereof, are provided, which are modulators of secreted frizzled related protein-1. The compounds, and compositions containing the compounds, can be used to treat a variety of disorders, including osteoporosis. (I) R 1 is alkyl, perfluoroalkyl, halo, cyano, or CO 2 alkyl; R 2 is optionally substituted alkyl, cycloalkyl, heterocycloalkyl, or spiroheterocycloalkyl; R 3 is optionally substituted aryl. R 4 is optionally substituted alkyl, cycloalkyl, or heterocycloalkyl; R 5 is hydrogen or alkyl; R 6 is optionally substituted aryl or heteroaryl; R 7 is alkyl, perfluoroalkyl, halo, cyano, or alkoxycarbonyl; and X is absent or SO 2 .

Abstract translation: 提供了吲哚磺酰胺化合物或其药学上可接受的盐，其是分泌的卷曲相关蛋白-1的调节剂。 化合物和含有这些化合物的组合物可用于治疗多种疾病，包括骨质疏松症。 （I）R 1是烷基，全氟烷基，卤素，氰基或CO 2烷基; R 2是任选取代的烷基，环烷基，杂环烷基或螺杂环烷基; R 3是任选取代的芳基。 R 4是任选取代的烷基，环烷基或杂环烷基; R 5是氢或烷基; R 6是任选取代的芳基或杂芳基; R 7是烷基，全氟烷基，卤素，氰基或烷氧基羰基; 并且X不存在或者是SO 2。

公开(公告)号：WO2006028875A1

公开(公告)日：2006-03-16

申请号：PCT/US2005/031053

申请日：2005-08-30

Applicant: WYETH ,  STEFFAN, Robert, John ,  MOORE, William, Jay ,  TRYBULSKI, Eugene, J. ,  MOLINARI, Albert, John

Inventor： STEFFAN, Robert, John ,  MOORE, William, Jay ,  TRYBULSKI, Eugene, J. ,  MOLINARI, Albert, John

IPC: C07D221/12 ,  A61K31/473 ,  A61P29/00 ,  A61P19/02 ,  A61P3/06 ,  A61P3/10 ,  A61P9/10 ,  A61P17/06

CPC classification number: C07D221/12

Abstract: The present invention provides phenanthridine carbonyl compounds and compositions, particularly those that find use as ligands for the estrogen receptor. Representative compounds of the invention include those of formula 1.

Abstract translation: 本发明提供菲啶羰基化合物和组合物，特别是可用作雌激素受体配体的那些。 本发明的代表性化合物包括式1的化合物。

公开(公告)号：WO2008073461A2

公开(公告)日：2008-06-19

申请号：PCT/US2007/025416

申请日：2007-12-11

Applicant: WYETH ,  GALULLO, Vincent ,  ZELLE, Robert ,  MAZDIYASNI, Hormoz ,  BAKER, Christopher, Todd ,  WILL, Paul ,  GUO, Jinsong ,  FENSOME, Andrew ,  SOENEN, Danielle ,  KERN, Jeffrey, Curtis ,  MOORE, William, Jay ,  MELENSKI, Edward, George ,  KAPLAN, Justin ,  SABATUCCI, Joseph, Peter

Inventor： GALULLO, Vincent ,  ZELLE, Robert ,  MAZDIYASNI, Hormoz ,  BAKER, Christopher, Todd ,  WILL, Paul ,  GUO, Jinsong ,  FENSOME, Andrew ,  SOENEN, Danielle ,  KERN, Jeffrey, Curtis ,  MOORE, William, Jay ,  MELENSKI, Edward, George ,  KAPLAN, Justin ,  SABATUCCI, Joseph, Peter

IPC: C07D207/34 ,  C07D233/90 ,  C07D249/04 ,  C07D277/56 ,  C07D307/68 ,  C07D307/71 ,  C07D333/70 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D405/12 ,  C07D405/14 ,  C07D409/12 ,  C07D409/14 ,  C07D417/12 ,  C07D417/14 ,  A61K31/341 ,  A61K31/381 ,  A61K31/415 ,  A61K31/4192 ,  A61K31/427 ,  A61K31/428 ,  A61K31/44 ,  A61K31/4965 ,  A61K31/50 ,  A61K31/505 ,  A61P9/10 ,  A61P9/12 ,  A61P25/00 ,  A61P25/08 ,  A61P25/14 ,  A61P25/16 ,  A61P25/32 ,  A61P25/34 ,  A61P25/36 ,  A61P29/00

CPC classification number: C07D417/12 ,  C07D207/34 ,  C07D233/90 ,  C07D249/04 ,  C07D277/56 ,  C07D307/68 ,  C07D307/71 ,  C07D333/70 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D405/12 ,  C07D405/14 ,  C07D409/12 ,  C07D409/14 ,  C07D417/14

Abstract: The present teachings provide carboxylic amide compounds that can modulate the activity of ion channels in a mammal. The present teachings also provide processes for producing said compounds and their pharmaceutically acceptable salts, hydrates and esters, and methods of treating a pathological condition or disorder, or alleviating a symptom thereof, using said compounds including their pharmaceutically acceptable salts, hydrates and esters. The compounds can be useful in modulating ion channel activity including treating a variety of conditions associated with the abnormal modulation of one or more voltage-gated calcium channels.

Abstract translation: 本教导提供了可调节哺乳动物离子通道活性的羧酸酰胺化合物。 本教导还提供了使用所述化合物（包括它们的药学上可接受的盐，水合物和酯）来制备所述化合物及其药学上可接受的盐，水合物和酯以及治疗病理学症状或病症或缓解其症状的方法。 该化合物可用于调节离子通道活性，包括治疗与一种或多种电压门控钙通道的异常调节有关的多种病症。

公开(公告)号：WO2008061016A1

公开(公告)日：2008-05-22

申请号：PCT/US2007/084285

申请日：2007-11-09

Applicant: WYETH ,  MOORE, William, Jay ,  KERN, Jeffrey, Curtis ,  TRYBULSKI, Eugene, John ,  WILSON, Matthew, Alan ,  WELMAKER, Gregory, Scott

Inventor： MOORE, William, Jay ,  KERN, Jeffrey, Curtis ,  TRYBULSKI, Eugene, John ,  WILSON, Matthew, Alan ,  WELMAKER, Gregory, Scott

IPC: C07D211/58 ,  C07D211/96 ,  C07D401/06 ,  C07D407/06 ,  A61K31/4523 ,  A61K31/445 ,  A61P11/06 ,  A61P19/00 ,  A61P35/00 ,  C07D401/04 ,  C07D401/12 ,  C07D401/14

CPC classification number: C07D211/58 ,  C07D211/96 ,  C07D401/06

Abstract: Compounds of formula (I): Chemical formula should be inserted here as it appears on the abstract in paper form. and pharmaceutically acceptable salt thereof, which are modulators of secreted frizzled related protein-1, are disclosed. The compounds, and compositions containing the compounds, can be used to treat various diseases and disorders, including osteoporosis, arthritis, chronic obstructive pulmonary disease, cartilage defects, bone fractures, leiomyoma, acute myeloid leukemia, wound healing, prostate cancer, autoimmune inflammatory disorders, such as Graves ophthalmopathy, and combinations thereof.

Abstract translation: 式（I）化合物：化学式应在纸上以抽象形式出现。 和其药学上可接受的盐，其是分泌的卷曲相关蛋白-1的调节剂。 化合物和含有这些化合物的组合物可用于治疗各种疾病和病症，包括骨质疏松症，关节炎，慢性阻塞性肺病，软骨缺损，骨折，平滑肌瘤，急性骨髓性白血病，伤口愈合，前列腺癌，自身免疫性炎症性疾病 ，如格雷夫斯眼病，及其组合。

公开(公告)号：WO2006124875A3

公开(公告)日：2007-01-18

申请号：PCT/US2006018886

申请日：2006-05-12

Applicant: WYETH CORP ,  GOPALSAMY ARIAMALA ,  MOORE WILLIAM JAY ,  KERN JEFFERY CURTIS ,  MOLINARI ALBERT JOHN ,  SHI MENGXIAO ,  WELMAKER GREGORY SCOTT ,  WILSON MATTHEW ALLAN ,  KRISHNAMURTHY GIRIJA ,  COMMONS THOMAS JOSEPH ,  WEBB MICHAEL BYRON ,  WOODWORTH RICHARD P

Inventor： GOPALSAMY ARIAMALA ,  MOORE WILLIAM JAY ,  KERN JEFFERY CURTIS ,  MOLINARI ALBERT JOHN ,  SHI MENGXIAO ,  WELMAKER GREGORY SCOTT ,  WILSON MATTHEW ALLAN ,  KRISHNAMURTHY GIRIJA ,  COMMONS THOMAS JOSEPH ,  WEBB MICHAEL BYRON ,  WOODWORTH RICHARD P

IPC: C07C317/20 ,  A61K31/445 ,  C07C317/22 ,  C07C317/26 ,  C07C317/38

CPC classification number: C07F9/3882 ,  C07C317/14 ,  C07C317/22 ,  C07C2601/02 ,  C07C2601/04 ,  C07C2601/08 ,  C07C2601/14 ,  C07C2602/08 ,  C07D213/42 ,  C07D233/54 ,  C07D401/04 ,  C07F9/4056

Abstract: Compounds of Formula (I), or pharmaceutically acceptable salts thereof, are provided, which are modulators of secreted frizzled related protein-1. The compounds, and compositions containing the compounds, can be used to treat a variety of disorders, including osteoporosis.

Abstract translation: 提供式（I）化合物或其药学上可接受的盐，其是分泌性卷曲相关蛋白-1的调节剂。 化合物和含有这些化合物的组合物可用于治疗多种疾病，包括骨质疏松症。

公开(公告)号：WO2006124875A2

公开(公告)日：2006-11-23

申请号：PCT/US2006/018886

申请日：2006-05-12

Applicant: WYETH ,  GOPALSAMY, Ariamala ,  MOORE, William, Jay ,  KERN, Jeffery, Curtis ,  MOLINARI, Albert, John ,  SHI, Mengxiao ,  WELMAKER, Gregory, Scott ,  WILSON, Matthew, Allan ,  KRISHNAMURTHY, Girija ,  COMMONS, Thomas, Joseph ,  WEBB, Michael, Byron ,  WOODWORTH, Richard, P.

Inventor： GOPALSAMY, Ariamala ,  MOORE, William, Jay ,  KERN, Jeffery, Curtis ,  MOLINARI, Albert, John ,  SHI, Mengxiao ,  WELMAKER, Gregory, Scott ,  WILSON, Matthew, Allan ,  KRISHNAMURTHY, Girija ,  COMMONS, Thomas, Joseph ,  WEBB, Michael, Byron ,  WOODWORTH, Richard, P.

IPC: C07C317/20 ,  C07C317/22 ,  C07C317/26 ,  C07C317/38 ,  A61K31/445

CPC classification number: C07F9/3882 ,  C07C317/14 ,  C07C317/22 ,  C07C2601/02 ,  C07C2601/04 ,  C07C2601/08 ,  C07C2601/14 ,  C07C2602/08 ,  C07D213/42 ,  C07D233/54 ,  C07D401/04 ,  C07F9/4056

Abstract: Compounds of Formula (I), or pharmaceutically acceptable salts thereof, are provided, which are modulators of secreted frizzled related protein-1. The compounds, and compositions containing the compounds, can be used to treat a variety of disorders, including osteoporosis.

Abstract translation: 提供式（I）化合物或其药学上可接受的盐，其是分泌性卷曲相关蛋白-1的调节剂。 化合物和含有这些化合物的组合物可用于治疗多种疾病，包括骨质疏松症。

公开(公告)号：WO2005037207A2

公开(公告)日：2005-04-28

申请号：PCT/US2004/033730

申请日：2004-10-13

Applicant: WYETH ,  TRYBULSKI, Eugene, John ,  MAHANEY, Paige, Erin ,  KRIM, Lori, Danielle ,  MOORE, William, Jay ,  SABATUCCI, Joseph, Peter

Inventor： TRYBULSKI, Eugene, John ,  MAHANEY, Paige, Erin ,  KRIM, Lori, Danielle ,  MOORE, William, Jay ,  SABATUCCI, Joseph, Peter

IPC: A61K

CPC classification number: C07D295/073 ,  C07D207/14 ,  C07D209/14 ,  C07D211/46 ,  C07D211/48 ,  C07D211/56 ,  C07D211/58 ,  C07D213/38 ,  C07D215/12 ,  C07D215/14 ,  C07D243/08 ,  C07D295/088 ,  C07D295/092 ,  C07D295/096 ,  C07D295/155 ,  C07D307/52 ,  C07D307/81 ,  C07D309/10 ,  C07D317/58 ,  C07D333/20 ,  C07D333/38 ,  C07D333/58 ,  C07D409/06 ,  C07D471/04

Abstract: The present invention is directed to alkanoyl and cycloalkanoyl-amine derivatives, compositions containing these derivatives, and methods of their use for the prevention and treatment of conditions ameliorated by monoamine reuptake including, inter alia , vasomotor symptoms (VMS), sexual dysfunction, nc gastrointestinal and genitourinary disorders, chronic fatigue syndrome, fibromylagia syndrome, nervous system disorders, and combinations thereof, particularly those conditions selected from the group consisting of major depressive disorder, vasomotor symptoms, stress and urge urinary incontinence, fibrornyalgia, pain, diabetic neuropathy, and combinations thereof.

Abstract translation: 本发明涉及烷酰基和环烷酰胺衍生物，含有这些衍生物的组合物及其用于预防和治疗由单胺再摄取改善的病症的方法，其中尤其包括血管舒缩症状（VMS），性功能障碍，胃肠道疾病 特别是选自重度抑郁症，血管舒缩症状，压力和急迫性尿失禁，纤维肌痛，疼痛，糖尿病性神经病变和组合的那些病症，这些疾病包括：泌尿生殖系统疾病，慢性疲劳综合征，纤维肉瘤病综合征，神经系统疾病及其组合 它们。