公开(公告)号：WO2010059627A1

公开(公告)日：2010-05-27

申请号：PCT/US2009/064791

申请日：2009-11-17

Applicant: WYETH LLC ,  TRAVINS, Jeremy, Mark ,  BERNOTAS, Ronald, Charles ,  WROBEL, Jay, Edward ,  KAUFMAN, David, Harry ,  HU, Baihua ,  JETTER, James, Winfield ,  O'NEILL, David, John ,  MANN, Charles, William

Inventor： TRAVINS, Jeremy, Mark ,  BERNOTAS, Ronald, Charles ,  WROBEL, Jay, Edward ,  KAUFMAN, David, Harry ,  HU, Baihua ,  JETTER, James, Winfield ,  O'NEILL, David, John ,  MANN, Charles, William

IPC: C07D239/72 ,  A61K31/517 ,  A61P3/00 ,  A61P9/10 ,  A61P29/00

CPC classification number: C07D239/72

Abstract: Disclosed are polar quinazoline-based modulators of Liver X receptors (LXRs) and related methods. The modulators include compounds of formula (I): INSERT FORMULA HERE AS IT APPEARS IN WRITTEN FORM IN THE SPECIFICATION (I) in which, R1, R2, R3, R4, R5, R6, R22, R23, R24, R25, R26, R27, R28, R29, W, W1, W2, Ra, Rb, Rc, Rd, Re, Rf, Rg, Rh, Ri, Rj, Rm, Rn, Ro, Rp, Rq, Rr, Rs, Rt, Ru, and n can be as defined anywhere herein. In general, these compounds can be used for treating or preventing one or more diseases, disorders, conditions or symptoms mediated by LXRs.

Abstract translation: 公开了基于极性喹唑啉的肝脏X受体调节剂（LXR）及相关方法。 调节剂包括式（I）化合物：其中R1，R2，R3，R4，R5，R6，R22，R23，R24，R25，R26， R 27，R 28，R 29，W，W 1，W 2，R a，R b，R c，R d，Re，R f，R g，Rh，R i，R j，R m，R n，R a，R p，R q，R r， 并且n可以如本文任何地方所定义。 通常，这些化合物可用于治疗或预防由LXR介导的一种或多种疾病，病症，病症或症状。

公开(公告)号：WO2009026326A1

公开(公告)日：2009-02-26

申请号：PCT/US2008/073655

申请日：2008-08-20

Applicant: WYETH ,  PELLETIER, Jeffrey Claude ,  FELIX, Luciana de Araujo ,  GREEN, Daniel Michael ,  HAUZE, Diane Barbara ,  LUNDQUIST IV, Joseph Theodore ,  MANN, Charles William ,  MEHLMANN, John Francis ,  ROGERS, JR., John Francis ,  VERA, Matthew Douglas ,  MOLINARI, Albert John

Inventor： PELLETIER, Jeffrey Claude ,  FELIX, Luciana de Araujo ,  GREEN, Daniel Michael ,  HAUZE, Diane Barbara ,  LUNDQUIST IV, Joseph Theodore ,  MANN, Charles William ,  MEHLMANN, John Francis ,  ROGERS, JR., John Francis ,  VERA, Matthew Douglas ,  MOLINARI, Albert John

IPC: C07D239/26 ,  C07D239/34 ,  C07D401/06 ,  C07D403/04 ,  C07D451/02 ,  C07D471/04 ,  C07D471/10 ,  C07D487/04 ,  C07D487/08 ,  A61K31/506 ,  A61P25/00

CPC classification number: C07D471/04 ,  C07D239/26 ,  C07D239/34 ,  C07D401/06 ,  C07D403/04 ,  C07D451/02 ,  C07D471/10 ,  C07D487/04 ,  C07D487/08

Abstract: The present invention relates to naphthylpyrimidine analogs, methods of making naphthylpyrimidine analogs, compositions comprising a naphthylpyrimidine analog, and methods for treating canonical Wnt-[beta-symbol]-catenin cellular messaging system-related disorders comprising administering to a subject in need thereof an effective amount of a naphthylpyrimidine, naphthylpyrazine and naphthylpyridazine analog.

Abstract translation: 本发明涉及萘基嘧啶类似物，制备萘基嘧啶类似物的方法，包含萘基嘧啶类似物的组合物，以及治疗经典Wnt-β-连环蛋白细胞通讯系统相关病症的方法，其包括给药 给有此需要的对象有效量的萘基嘧啶，萘基吡嗪和萘基哒嗪类似物。

公开(公告)号：WO2009026319A1

公开(公告)日：2009-02-26

申请号：PCT/US2008/073644

申请日：2008-08-20

Applicant: WYETH ,  PELLETIER, Jeffrey Claude ,  FELIX, Luciana De Araujo ,  GREEN, Daniel Michael ,  HAUZE, Diane Barbara ,  LUNDQUIST IV, Joseph Theodore ,  MANN, Charles William ,  MEHLMANN, John Francis ,  ROGERS, JR., John Francis ,  VERA, Matthew Douglas ,  MOLINARI, Albert John

Inventor： PELLETIER, Jeffrey Claude ,  FELIX, Luciana De Araujo ,  GREEN, Daniel Michael ,  HAUZE, Diane Barbara ,  LUNDQUIST IV, Joseph Theodore ,  MANN, Charles William ,  MEHLMANN, John Francis ,  ROGERS, JR., John Francis ,  VERA, Matthew Douglas ,  MOLINARI, Albert John

IPC: C07D239/26 ,  C07D239/34 ,  C07D401/06 ,  C07D403/04 ,  C07D451/02 ,  C07D471/04 ,  C07D471/10 ,  C07D487/04 ,  C07D487/08 ,  A61K31/506 ,  A61P25/00

CPC classification number: C07D471/04 ,  C07D239/26 ,  C07D239/34 ,  C07D401/06 ,  C07D403/04 ,  C07D451/02 ,  C07D471/10 ,  C07D487/04 ,  C07D487/08

Abstract: The present invention relates to naphthylpyrimidine analogs, methods of making naphthylpyrimidine analogs, compositions comprising a naphthylpyrimidine analog, and methods for treating canonical Wnt-[beta-symbol]-catenin cellular messaging system-related disorders comprising administering to a subject in need thereof an effective amount of a naphthylpyrimidine, naphthylpyrazine and naphthylpyridazine analog.

Abstract translation: 本发明涉及萘基嘧啶类似物，制备萘基嘧啶类似物的方法，包含萘基嘧啶类似物的组合物，以及用于治疗典型的Wnt- [β-符号] - 连环蛋白细胞消化系统相关疾病的方法，其包括向有需要的受试者施用有效的 萘基嘧啶，萘基吡嗪和萘基哒嗪类似物的量。

公开(公告)号：WO2008073956A2

公开(公告)日：2008-06-19

申请号：PCT/US2007/087171

申请日：2007-12-12

Applicant: WYETH ,  FENSOME, Andrew ,  GOLDBERG, Joel Adam ,  MCCOMAS, Casey Cameron ,  MANN, Charles William ,  MELENSKI, Edward George ,  SABATUCCI, Joseph P. ,  WOODWORTH, Richard Page, Jr.

Inventor： FENSOME, Andrew ,  GOLDBERG, Joel Adam ,  MCCOMAS, Casey Cameron ,  MANN, Charles William ,  MELENSKI, Edward George ,  SABATUCCI, Joseph P. ,  WOODWORTH, Richard Page, Jr.

IPC: C07D279/02 ,  C07D291/08 ,  C07D417/06 ,  C07D419/06 ,  C07D285/15 ,  A61K31/5415 ,  A61P5/24

CPC classification number: C07D279/02 ,  C07D285/15 ,  C07D291/08 ,  C07D417/04 ,  C07D419/04 ,  C07D419/06 ,  C07D487/08

Abstract: The present invention is directed to cyclic sulfonamide derivatives of formula (I): or a pharmaceutically acceptable salt thereof, which are monoamine reuptake inhibitors, compositions containing these derivatives, and methods of their use for the prevention and treatment of conditions, including, inter alia, vasomotor symptoms, sexual dysfunction, gastrointestinal disorders and genitourinary disorder, depression disorders, endogenous behaviorial disorder, cognitive disorder, diabetic neuropathy, pain, and other diseases or disorders.

Abstract translation: 本发明涉及式（I）的环磺酰胺衍生物或其药学上可接受的盐，它们是单胺再摄取抑制剂，含有这些衍生物的组合物，以及它们用于预防和治疗 尤其包括血管舒缩症状，性功能障碍，胃肠疾病和泌尿生殖系统疾病，抑郁症，内源性行为障碍，认知障碍，糖尿病性神经病，疼痛和其他疾病或病症的治疗。

公开(公告)号：WO2008073956A3

公开(公告)日：2008-07-24

申请号：PCT/US2007087171

申请日：2007-12-12

Applicant: WYETH CORP ,  FENSOME ANDREW ,  GOLDBERG JOEL ADAM ,  MCCOMAS CASEY CAMERON ,  MANN CHARLES WILLIAM ,  MELENSKI EDWARD GEORGE ,  SABATUCCI JOSEPH P ,  WOODWORTH RICHARD PAGE JR

Inventor： FENSOME ANDREW ,  GOLDBERG JOEL ADAM ,  MCCOMAS CASEY CAMERON ,  MANN CHARLES WILLIAM ,  MELENSKI EDWARD GEORGE ,  SABATUCCI JOSEPH P ,  WOODWORTH RICHARD PAGE JR

IPC: C07D279/02 ,  A61K31/5415 ,  A61P5/24 ,  C07D285/15 ,  C07D291/08 ,  C07D417/06 ,  C07D419/06

CPC classification number: C07D279/02 ,  C07D285/15 ,  C07D291/08 ,  C07D417/04 ,  C07D419/04 ,  C07D419/06 ,  C07D487/08

Abstract: The present invention is directed to cyclic sulfonamide derivatives of formula (I): or a pharmaceutically acceptable salt thereof, which are monoamine reuptake inhibitors, compositions containing these derivatives, and methods of their use for the prevention and treatment of conditions, including, inter alia, vasomotor symptoms, sexual dysfunction, gastrointestinal disorders and genitourinary disorder, depression disorders, endogenous behaviorial disorder, cognitive disorder, diabetic neuropathy, pain, and other diseases or disorders.

Abstract translation: 本发明涉及式（I）的环状磺酰胺衍生物：或其药学上可接受的盐，其为单胺再摄取抑制剂，含有这些衍生物的组合物，及其用于预防和治疗病症的方法， ，血管舒缩症状，性功能障碍，胃肠道疾病和泌尿生殖器疾病，抑郁症，内源性行为障碍，认知障碍，糖尿病性神经病，疼痛和其他疾病或障碍。

公开(公告)号：WO2010054229A1

公开(公告)日：2010-05-14

申请号：PCT/US2009/063596

申请日：2009-11-06

Applicant: WYETH LLC ,  HU, Baihua ,  WROBEL, Jay, Edward ,  JETTER, James, Winfield ,  O'NEILL, David, John ,  MANN, Charles, William ,  UNWALLA, Rayomand, Jal

Inventor： HU, Baihua ,  WROBEL, Jay, Edward ,  JETTER, James, Winfield ,  O'NEILL, David, John ,  MANN, Charles, William ,  UNWALLA, Rayomand, Jal

IPC: C07D241/42 ,  C07D241/44 ,  A61K31/498 ,  A61P3/06 ,  A61P9/10

CPC classification number: C07D241/44 ,  C07D241/42

Abstract: Disclosed are quinoxaline-based modulators of Liver X receptors (LXRs) and related methods. The modulators include compounds of formula (I): wherein: each of L1 and L2 is, independently, a bond, -O- or -NH-; R2 is C6-C10 aryl or heteroaryl including 5-10 ring atoms, each of which is (i) substituted with 1 R9, and (ii) optionally further substituted with from 1-4 Re; and each of R4 and R5 is, independently (i) hydrogen; or (ii) halo; or (iii) C1-C6 alkyl or C1-C6 haloalkyl, each of which is optionally substituted with from 1-3 Ra; and R1, R3, R6, R9, Ra and Re are defined herein. In general, these compounds can be used for treating or preventing one or more diseases, disorders, conditions or symptoms mediated by LXRs.

Abstract translation: 公开了基于喹喔啉的肝脏X受体调节剂（LXR）和相关方法。 调节剂包括式（I）的化合物：其中：L1和L2各自独立地是键，-O-或-NH-; R 2是包括5-10个环原子的C 6 -C 10芳基或杂芳基，其各自为（i）被1个R 9取代，和（ii）任选进一步被1-4个Re取代; 并且R 4和R 5各自独立地是（i）氢; 或（ii）卤素; 或（iii）C 1 -C 6烷基或C 1 -C 6卤代烷基，其各自任选被1-3个R a取代; 并且R1，R3，R6，R9，Ra和Re在本文中定义。 通常，这些化合物可用于治疗或预防由LXR介导的一种或多种疾病，病症，病症或症状。

公开(公告)号：WO2003103660A1

公开(公告)日：2003-12-18

申请号：PCT/US2003/018198

申请日：2003-06-09

Applicant: WYETH ,  ARQULE, INC. ,  KREFT, Anthony, Frank ,  COLE, Derek, Cecil ,  WOLLER, Kevin, Roger ,  STOCK, Joseph, Raymond ,  KUTTERER, Kristina, Martha ,  KUBRAK, Dennis, Martin ,  MANN, Charles, William ,  MOORE, William, Jay ,  CASEBIER, David, Scott

Inventor： KREFT, Anthony, Frank ,  COLE, Derek, Cecil ,  WOLLER, Kevin, Roger ,  STOCK, Joseph, Raymond ,  KUTTERER, Kristina, Martha ,  KUBRAK, Dennis, Martin ,  MANN, Charles, William ,  MOORE, William, Jay ,  CASEBIER, David, Scott

IPC: A61K31/18

CPC classification number: C07C311/40 ,  A61K31/18 ,  A61K31/335 ,  A61K31/34 ,  A61K31/357 ,  A61K31/4245 ,  A61K31/655 ,  C07C311/17 ,  C07C311/18 ,  C07C311/20 ,  C07C311/29 ,  C07C323/49 ,  C07C2601/04 ,  C07C2601/08 ,  C07C2601/14 ,  C07C2602/08 ,  C07C2602/42 ,  C07D209/16 ,  C07D307/52 ,  C07D319/06

Abstract: Compounds of Formula I, wherein R 1 -R 8 are defined herein are provided, together with pharmaceutically acceptable salts, hydrates, metabolites, and/or prodrugs thereof. Uses of these compounds for inhibiting beta amyloid production and for the prevention and treatment of Alzheimer’s Disease and Down’s syndrome are described.

Abstract translation: 提供其中R 1 -R 8在本文中定义的式I化合物及其药学上可接受的盐，水合物，代谢物和/或前药。 描述了这些化合物用于抑制β淀粉样蛋白生成和预防和治疗阿尔茨海默病和唐氏综合征的用途。

公开(公告)号：WO2008073459A1

公开(公告)日：2008-06-19

申请号：PCT/US2007/025405

申请日：2007-12-12

Applicant: WYETH ,  MC COMAS, Casey, Cameron ,  COHN, Stephen, Todd ,  CRAWLEY, Matthew, L. ,  FENSOME, Andrew ,  GOLDBERG, Joel, Adam ,  JENKINS, Douglas, John ,  KIM, Callain, Younghee ,  MAHANEY, Paige, Erin ,  MANN, Charles, William ,  MARELLA, Michael, Anthony ,  O'NEILL, David, John ,  SABATUCCI, Joseph, P. ,  TEREFENKO, Eugene, Anthony ,  TRYBULSKI, Eugene, John ,  VU, An, Thien ,  WOODWORTH, Richard, Page, Jr. ,  ZHANG, Puwen

Inventor： MC COMAS, Casey, Cameron ,  COHN, Stephen, Todd ,  CRAWLEY, Matthew, L. ,  FENSOME, Andrew ,  GOLDBERG, Joel, Adam ,  JENKINS, Douglas, John ,  KIM, Callain, Younghee ,  MAHANEY, Paige, Erin ,  MANN, Charles, William ,  MARELLA, Michael, Anthony ,  O'NEILL, David, John ,  SABATUCCI, Joseph, P. ,  TEREFENKO, Eugene, Anthony ,  TRYBULSKI, Eugene, John ,  VU, An, Thien ,  WOODWORTH, Richard, Page, Jr. ,  ZHANG, Puwen

IPC: C07D285/14 ,  C07D417/04 ,  C07D417/06

CPC classification number: C07D417/04 ,  C07D285/14 ,  C07D417/06

Abstract: The present invention is directed to aryl sulfamide derivatives of formula (I): or a pharmaceutically acceptable salt, stereoisomer or tautomer thereof, which are monoamine reuptake inhibitors, compositions containing these derivatives, and methods of their use for the prevention and treatment of conditions, including, inter alia, vasomotor symptoms, sexual dysfunction, gastrointestinal disorders and genitourinary disorder, depression disorders, endogenous behavioral disorders, cognitive disorders, diabetic neuropathy, pain, and other diseases or disorders.

Abstract translation: 本发明涉及式（I）的芳基磺酰胺衍生物：或其药学上可接受的盐，立体异构体或互变异构体，它们是单胺再摄取抑制剂，含有这些衍生物的组合物及其用于预防和治疗病症的方法， 包括血管舒缩症状，性功能障碍，胃肠道疾病和泌尿生殖器疾病，抑郁症，内源性行为障碍，认知障碍，糖尿病性神经病，疼痛和其他疾病或病症。

公开(公告)号：WO0043413A3

公开(公告)日：2000-11-30

申请号：PCT/US0001537

申请日：2000-01-21

Applicant: ELAN PHARM INC ,  AMERICAN HOME PROD ,  DRESSEN DARREN B ,  KREFT ANTHONY ,  KUBRAK DENNIS ,  MANN CHARLES WILLIAM ,  PLEISS MICHAEL A ,  STACK GARY PAUL ,  THORSETT EUGENE D

Inventor： DRESSEN DARREN B ,  KREFT ANTHONY ,  KUBRAK DENNIS ,  MANN CHARLES WILLIAM ,  PLEISS MICHAEL A ,  STACK GARY PAUL ,  THORSETT EUGENE D

IPC: A61K38/00 ,  A61P1/04 ,  A61P3/10 ,  A61P9/10 ,  A61P11/06 ,  A61P13/12 ,  A61P17/00 ,  A61P17/06 ,  A61P25/28 ,  A61P27/00 ,  A61P29/00 ,  A61P35/04 ,  C07K5/06 ,  C07K5/078 ,  A61K38/05

CPC classification number: C07K5/06173 ,  C07K5/06139 ,  C07K5/06165 ,  C07K5/06191

Abstract: Disclosed are pyroglutamic acid derivatives and related compounds which bind VLA-4. Certain of these compounds also inhibit leukocyte adhesion and, in particular, leukocyte adhesion mediated by VLA-4. Such compounds are useful in the treatment of inflammatory diseases in a mammalian patient, e.g., human, such as asthma, Alzheimer's disease, atherosclerosis, AIDS dementia, diabetes, inflammatory bowel disease, rheumatoid arthritis, tissue transplantation, tumor metastasis and myocardial ischemia. The compounds can also be administered for the treatment of inflammatory brain diseases such as multiple sclerosis.

Abstract translation: 公开了结合VLA-4的焦谷氨酸衍生物和相关化合物。 这些化合物中的某些还抑制白细胞粘附，特别是抑制由VLA-4介导的白细胞粘附。 此类化合物可用于治疗哺乳动物患者例如人的炎性疾病，例如哮喘，阿尔茨海默氏病，动脉粥样硬化，AIDS痴呆，糖尿病，炎性肠病，类风湿性关节炎，组织移植，肿瘤转移和心肌缺血。 该化合物也可以用于治疗炎症性脑疾病如多发性硬化症。