公开(公告)号：WO2003042164A1

公开(公告)日：2003-05-22

申请号：PCT/US2002/036237

申请日：2002-11-12

Applicant: THERAVANCE, INC ,  MORAN, Edmund, J. ,  JACOBSEN, John, R. ,  LEADBETTER, Michael, R. ,  NODWELL, Matthew, B. ,  TRAPP, Sean, G. ,  AGGEN, James ,  CHURCH, Timothy, J.

Inventor： MORAN, Edmund, J. ,  JACOBSEN, John, R. ,  LEADBETTER, Michael, R. ,  NODWELL, Matthew, B. ,  TRAPP, Sean, G. ,  AGGEN, James ,  CHURCH, Timothy, J.

IPC: C07C229/60

CPC classification number: C07D213/75 ,  C07C215/60 ,  C07C217/84 ,  C07C229/38 ,  C07C233/43 ,  C07C317/36 ,  C07D213/76 ,  C07D215/227 ,  C07D215/26 ,  C07D231/22 ,  C07D239/38 ,  C07D239/42 ,  C07D239/47 ,  C07D277/46 ,  C07D277/52 ,  C07D295/26 ,  C07D311/80 ,  C07D319/18 ,  C07D321/10 ,  C07D401/12 ,  C07D409/12 ,  C07D413/12

Abstract: The invention provides novel β 2 adrenergic receptor agonist compounds of formula (I): wherein R 1 -R 13 and w have any of the values described in the specification. The invention also provides pharmaceutical compositions comprising such compounds, methods of using such compounds to treat diseases associated with β 2 adrenergic receptor activity, and processes and intermediates useful for preparing such compounds.

Abstract translation: 本发明提供式（I）的新型β2肾上腺素能受体激动剂化合物：其中R 1 -R 13和w具有说明书中描述的任何值。 本发明还提供包含这些化合物的药物组合物，使用这些化合物治疗与β2肾上腺素能受体活性有关的疾病的方法，以及可用于制备这些化合物的方法和中间体。

公开(公告)号：WO2012024682A1

公开(公告)日：2012-02-23

申请号：PCT/US2011/048650

申请日：2011-08-22

Applicant: THE UNIVERSITY OF BRITISH COLUMBIA ,  WANG, Xiaoxia ,  MEIMETIS, Labros, George ,  NODWELL, Matthew, Bruce ,  ANDERSEN, Raymond

Inventor： WANG, Xiaoxia ,  MEIMETIS, Labros, George ,  NODWELL, Matthew, Bruce ,  ANDERSEN, Raymond

IPC: A61K31/045

CPC classification number: C07C43/23 ,  A61K31/045 ,  C07B2200/07 ,  C07C37/50 ,  C07C39/17 ,  C07C41/18 ,  C07C45/30 ,  C07C45/65 ,  C07C49/747 ,  C07C49/753 ,  C07C67/08 ,  C07C69/65 ,  C07C69/734 ,  C07C213/02 ,  C07C215/44 ,  C07C215/64 ,  C07C249/08 ,  C07C251/44 ,  C07C2603/40 ,  C07D223/32

Abstract: Compounds of structure (I): including stereoisomers and pharmaceutically acceptable salts thereof, wherein R 1 , R 2 and A are as defined herein are disclosed. Such compounds have enhanced water solubility and have activity as SHIP1 modulators, and thus may be used to treat any of a variety of diseases, disorders or conditions that would benefit from SHIP1 modulation. Enantioselective methods for preparation of compounds of structure (I), compositions comprising a compound of structure (I) in combination with a pharmaceutically acceptable carrier or diluents and methods of SHIP1 modulation by administration of such compounds to an animal in need thereof are also disclosed.

Abstract translation: 结构（I）的化合物：包括立体异构体及其药学上可接受的盐，其中R1，R2和A如本文所定义。 这些化合物具有增强的水溶性并且具有作为SHIP1调节剂的活性，因此可用于治疗将受益于SHIP1调节的各种疾病，病症或病症中的任何一种。 还公开了用于制备结构（I）化合物的对映选择性方法，包含结构（I）化合物与药学上可接受的载体或稀释剂的组合物的组合物以及通过将这些化合物施用于有需要的动物的SHIP1调节方法。

公开(公告)号：WO2007147252A1

公开(公告)日：2007-12-27

申请号：PCT/CA2007/001106

申请日：2007-06-21

Applicant: THE UNIVERSITY OF BRITISH COLUMBIA ,  ANDERSEN, Raymond ,  NODWELL, Matthew ,  MUI, Alice

Inventor： ANDERSEN, Raymond ,  NODWELL, Matthew ,  MUI, Alice

IPC: C07C219/28 ,  A61K31/222 ,  A61K31/417 ,  A61K31/661 ,  C07C235/74 ,  C07C237/12 ,  C07C279/14 ,  C07C323/52 ,  C07D233/64 ,  C07F9/12

CPC classification number: C07C39/17 ,  C07C43/23 ,  C07C45/29 ,  C07C47/57 ,  C07C65/17 ,  C07C229/08 ,  C07C229/24 ,  C07C229/26 ,  C07C279/14 ,  C07C323/52 ,  C07C2603/40 ,  C07F9/12 ,  C07J61/00

Abstract: The present invention provides the use of prodrugs of pelorol and homopelorol, related compounds and pharmaceutical compositions thereof as modulators of SHIPl activity. A compound or a pharmaceutical composition of the present invention may be used for the treatment or prophylaxis of an inflammatory, neoplastic, hematopoetic or immune disorder or condition in addition to other disorders and conditions.

Abstract translation: 本发明提供了作为SHIP1活性的调节剂的用于制备托泊酮和高麦芽凌醇的前体药物，相关化合物及其药物组合物的用途。 本发明的化合物或药物组合物除了其它病症和病症之外，还可用于治疗或预防炎症，肿瘤，造血或免疫疾病或病症。

公开(公告)号：WO2005000878A3

公开(公告)日：2005-01-06

申请号：PCT/US2004/021039

申请日：2004-06-28

Applicant: MIGENIX INC. ,  CAMERON, Dale, R. ,  BOYD, Vincent, A. ,  LEESE, Richard, A. ,  CURRAN, William, V. ,  BORDERS, Donald, B. ,  SGARBI, Paulo, W., M. ,  WACOWICH-SGARBI, Shirley, A. ,  NODWELL, Matthew ,  CHEN, Yuchen ,  JIA, Qi ,  DUGOURD, Dominique

Inventor： CAMERON, Dale, R. ,  BOYD, Vincent, A. ,  LEESE, Richard, A. ,  CURRAN, William, V. ,  BORDERS, Donald, B. ,  SGARBI, Paulo, W., M. ,  WACOWICH-SGARBI, Shirley, A. ,  NODWELL, Matthew ,  CHEN, Yuchen ,  JIA, Qi ,  DUGOURD, Dominique

IPC: C07K7/56

Abstract: The present invention provides derivatives of lipopeptide antibiotics that display antimicrobial activity against microorganisms, methods and compounds for synthesizing such antimicrobial derivatives and analogues, and methods of using the compounds in a variety of contexts, including in the treatment and prevention of microbial infections.

公开(公告)号：WO2007147251A1

公开(公告)日：2007-12-27

申请号：PCT/CA2007/001105

申请日：2007-06-21

Applicant: THE UNIVERSITY OF BRITISH COLUMBIA ,  ANDERSEN, Raymond ,  NODWELL, Matthew ,  MUI, Alice

Inventor： ANDERSEN, Raymond ,  NODWELL, Matthew ,  MUI, Alice

IPC: C07C39/17 ,  A61K31/05 ,  A61K31/085 ,  A61P35/00 ,  C07C43/23

CPC classification number: C07C39/17 ,  C07C43/23 ,  C07C45/29 ,  C07C47/57 ,  C07C65/17 ,  C07C229/08 ,  C07C229/24 ,  C07C229/26 ,  C07C279/14 ,  C07C323/52 ,  C07C2603/40 ,  C07F9/12 ,  C07J61/00

Abstract: The present invention provides the use of pelorol analogs of Formula, ( I ) and pharmaceutical compositions thereof as modulators of SHIP 1 activity. A compound or a pharmaceutical composition of the present invention may be used for the treatment or prophylaxis of an inflammatory, neoplastic, hematopoetic or immune disorder or condition in addition to other disorders and conditions.

Abstract translation: 本发明提供式（I）的托泊酮类似物及其药物组合物作为SHIP1活性的调节剂的用途。 本发明的化合物或药物组合物除了其它病症和病症之外，还可用于治疗或预防炎症，肿瘤，造血或免疫疾病或病症。

公开(公告)号：WO2005000878A8

公开(公告)日：2006-06-08

申请号：PCT/US2004021039

申请日：2004-06-28

Applicant: MIGENIX INC ,  CAMERON DALE R ,  BOYD VINCENT A ,  LEESE RICHARD A ,  CURRAN WILLIAM V ,  BORDERS DONALD B ,  SGARBI PAULO W M ,  WACOWICH-SGARBI SHIRLEY A ,  NODWELL MATTHEW ,  CHEN YUCHEN ,  JIA QI ,  DUGOURD DOMINIQUE

Inventor： CAMERON DALE R ,  BOYD VINCENT A ,  LEESE RICHARD A ,  CURRAN WILLIAM V ,  BORDERS DONALD B ,  SGARBI PAULO W M ,  WACOWICH-SGARBI SHIRLEY A ,  NODWELL MATTHEW ,  CHEN YUCHEN ,  JIA QI ,  DUGOURD DOMINIQUE

IPC: A61K38/12 ,  A61K38/00 ,  A61P31/04 ,  C07K7/56 ,  C07K7/64

CPC classification number: C07K7/56 ,  A61K38/00

Abstract: The present invention provides derivatives of lipopeptide antibiotics that display antimicrobial activity against microorganisms, methods and compounds for synthesizing such antimicrobial derivatives and analogues, and methods of using the compounds in a variety of contexts, including in the treatment and prevention of microbial infections.

Abstract translation: 本发明提供显示抗微生物的抗微生物活性的脂肽抗生素衍生物，用于合成这种抗微生物衍生物和类似物的方法和化合物，以及在多种情况下使用该化合物的方法，包括在治疗和预防微生物感染方面。

公开(公告)号：WO2005025555A3

公开(公告)日：2005-06-23

申请号：PCT/US2004014168

申请日：2004-05-07

Applicant: THERAVANCE INC ,  MORAN EDMUND J ,  JACOBSEN JOHN R ,  LEADBETTER MICHAEL R ,  NODWELL MATTHEW B ,  TRAPP SEAN G ,  AGGEN JAMES B ,  CHURCH TIMOTHY J

Inventor： MORAN EDMUND J ,  JACOBSEN JOHN R ,  LEADBETTER MICHAEL R ,  NODWELL MATTHEW B ,  TRAPP SEAN G ,  AGGEN JAMES B ,  CHURCH TIMOTHY J

IPC: A61K31/136 ,  A61K31/277 ,  A61K31/325 ,  A61K31/33 ,  A61K31/343 ,  A61K31/35 ,  A61K31/36 ,  A61K31/381 ,  A61K31/385 ,  A61K31/405 ,  A61K31/4184 ,  A61K31/423 ,  A61K31/428 ,  A61K31/47 ,  A61K31/4704 ,  A61K31/4706 ,  A61K31/4709 ,  A61K31/58 ,  C07C215/60 ,  C07C217/84 ,  C07C229/38 ,  C07C233/43 ,  C07D213/75 ,  C07D215/22 ,  C07D215/227 ,  C07D215/26 ,  C07D231/22 ,  C07D239/38 ,  C07D239/42 ,  C07D239/46 ,  C07D277/46 ,  C07D311/80 ,  C07D321/10 ,  C07D401/12 ,  C07D409/12 ,  C07D413/12

CPC classification number: A61K31/4706 ,  A61K31/136 ,  A61K31/277 ,  A61K31/325 ,  A61K31/33 ,  A61K31/343 ,  A61K31/35 ,  A61K31/36 ,  A61K31/381 ,  A61K31/385 ,  A61K31/405 ,  A61K31/4184 ,  A61K31/423 ,  A61K31/428 ,  A61K31/47 ,  A61K31/4704 ,  A61K31/4709 ,  A61K31/58 ,  C07C213/04 ,  C07C215/34 ,  C07C215/60 ,  C07C217/84 ,  C07C229/38 ,  C07C233/43 ,  C07C317/36 ,  C07D213/75 ,  C07D215/227 ,  C07D215/26 ,  C07D231/22 ,  C07D239/38 ,  C07D239/42 ,  C07D239/47 ,  C07D239/69 ,  C07D277/46 ,  C07D311/80 ,  C07D321/10 ,  C07D401/12 ,  C07D409/12 ,  C07D413/12 ,  A61K2300/00

Abstract: The invention provides novel beta2 adrenergic receptor agonist compounds of formula (I): wherein R1 - R13 and w have any of the values described in the specification. The invention also provides combinations of such compounds and other therapeutic agents, pharmaceutical compositions comprising such compounds and combinations, methods of using such compounds to treat diseases associated with beta2 adrenergic receptor activity, and processes and intermediates useful for preparing such compounds.

Abstract translation: 本发明提供式（I）的新型β2肾上腺素能受体激动剂化合物：其中R1-R13和w具有说明书中描述的任何值。 本发明还提供了这样的化合物和其它治疗剂的组合，包含这些化合物和组合的药物组合物，使用这些化合物治疗与β2肾上腺素能受体活性相关的疾病的方法，以及可用于制备这些化合物的方法和中间体。

公开(公告)号：WO2005025555A2

公开(公告)日：2005-03-24

申请号：PCT/US2004/014168

申请日：2004-05-07

Applicant: THERAVANCE, INC. ,  MORAN, Edmund, J. ,  JACOBSEN, John, R. ,  LEADBETTER, Michael, R. ,  NODWELL, Matthew, B. ,  TRAPP, Sean, G. ,  AGGEN, James, B. ,  CHURCH, Timothy, J.

Inventor： MORAN, Edmund, J. ,  JACOBSEN, John, R. ,  LEADBETTER, Michael, R. ,  NODWELL, Matthew, B. ,  TRAPP, Sean, G. ,  AGGEN, James, B. ,  CHURCH, Timothy, J.

IPC: A61K31/00

CPC classification number: A61K31/4706 ,  A61K31/136 ,  A61K31/277 ,  A61K31/325 ,  A61K31/33 ,  A61K31/343 ,  A61K31/35 ,  A61K31/36 ,  A61K31/381 ,  A61K31/385 ,  A61K31/405 ,  A61K31/4184 ,  A61K31/423 ,  A61K31/428 ,  A61K31/47 ,  A61K31/4704 ,  A61K31/4709 ,  A61K31/58 ,  C07C213/04 ,  C07C215/34 ,  C07C215/60 ,  C07C217/84 ,  C07C229/38 ,  C07C233/43 ,  C07C317/36 ,  C07D213/75 ,  C07D215/227 ,  C07D215/26 ,  C07D231/22 ,  C07D239/38 ,  C07D239/42 ,  C07D239/47 ,  C07D239/69 ,  C07D277/46 ,  C07D311/80 ,  C07D321/10 ,  C07D401/12 ,  C07D409/12 ,  C07D413/12 ,  A61K2300/00

Abstract: The invention provides novel β2 adrenergic receptor agonist compounds of formula (I): wherein R 1 - R 13 and w have any of the values described in the specification. The invention also provides combinations of such compounds and other therapeutic agents, pharmaceutical compositions comprising such compounds and combinations, methods of using such compounds to treat diseases associated with β2 adrenergic receptor activity, and processes and intermediates useful for preparing such compounds.

Abstract translation: 本发明提供式（I）的新型β2肾上腺素能受体激动剂化合物：其中R1-R13和w具有说明书中描述的任何值。 本发明还提供了这些化合物和其它治疗剂的组合，包含这些化合物和组合的药物组合物，使用这些化合物治疗与β2肾上腺素能受体活性有关的疾病的方法，以及可用于制备这些化合物的方法和中间体。

公开(公告)号：WO2005000878A2

公开(公告)日：2005-01-06

申请号：PCT/US2004021039

申请日：2004-06-28

Applicant: MICROLOGIX BIOTECH INC ,  CAMERON DALE R ,  BOYD VINCENT A ,  LEESE RICHARD A ,  CURRAN WILLIAM V ,  FRANCIS NOREEN D ,  JAROLMEN HOWARD ,  BORDERS DONALD B ,  SGARBI PAULO W M ,  WACOWICH-SGARBI SHIRLEY A ,  NODWELL MATTHEW ,  CHEN YUCHEN ,  JIA QI

Inventor： CAMERON DALE R ,  BOYD VINCENT A ,  LEESE RICHARD A ,  CURRAN WILLIAM V ,  FRANCIS NOREEN D ,  JAROLMEN HOWARD ,  BORDERS DONALD B ,  SGARBI PAULO W M ,  WACOWICH-SGARBI SHIRLEY A ,  NODWELL MATTHEW ,  CHEN YUCHEN ,  JIA QI

IPC: A61K38/00 ,  A61K38/12 ,  A61P31/04 ,  C07K7/56 ,  C07K7/64

CPC classification number: C07K7/56 ,  A61K38/00

Abstract: The present invention provides derivatives of lipopeptide antibiotics that display antimicrobial activity against microorganisms, methods and compounds for synthesizing such antimicrobial derivatives and analogues, and methods of using the compounds in a variety of contexts, including in the treatment and prevention of microbial infections.

Abstract translation: 本发明提供显示抗微生物抗微生物活性的脂肽抗生素衍生物，用于合成这种抗微生物衍生物和类似物的方法和化合物，以及在多种情况下使用该化合物的方法，包括在治疗和预防微生物感染中。

公开(公告)号：WO2004113350A1

公开(公告)日：2004-12-29

申请号：PCT/US2004/016007

申请日：2004-05-21

Applicant: THERAVANCE, INC. ,  LINSELL, Martin, S. ,  MARQUESS, Daniel ,  LONG, Daniel, D. ,  CHINN, Jason, P. ,  NODWELL, Matthew, B. ,  MORAN, Edmund, J. ,  AGGEN, James, B. ,  FATHEREE, Paul, R.

Inventor： LINSELL, Martin, S. ,  MARQUESS, Daniel ,  LONG, Daniel, D. ,  CHINN, Jason, P. ,  NODWELL, Matthew, B. ,  MORAN, Edmund, J. ,  AGGEN, James, B. ,  FATHEREE, Paul, R.

IPC: C07D501/00

CPC classification number: C07D519/00 ,  A61K38/00 ,  C07D501/46 ,  C07K9/008

Abstract: This invention provides cross-linked glycopeptide - cephalosporin compounds and pharmaceutically acceptable salts thereof which are useful as antibiotics. This invention also provides pharmaceutical compositions containing such compounds; methods for treating bacterial infections in a mammal using such compounds; and processes and intermediates useful for preparing such compounds.

Abstract translation: 本发明提供可用作抗生素的交联糖肽 - 头孢菌素化合物及其药学上可接受的盐。 本发明还提供含有这些化合物的药物组合物; 使用这些化合物治疗哺乳动物细菌感染的方法; 以及可用于制备这些化合物的方法和中间体。