公开(公告)号：WO2007027734A2

公开(公告)日：2007-03-08

申请号：PCT/US2006033803

申请日：2006-08-29

Applicant: CHEMOCENTRYX INC ,  CHEN WEI ,  ZHANG PENGLIE ,  AGGEN JAMES B ,  DAIRAGHI DANIEL JOSEPH ,  PENNELL ANDREW M K ,  SEN SUBHABRATA ,  WRIGHT KIM J J

Inventor： CHEN WEI ,  ZHANG PENGLIE ,  AGGEN JAMES B ,  DAIRAGHI DANIEL JOSEPH ,  PENNELL ANDREW M K ,  SEN SUBHABRATA ,  WRIGHT KIM J J

IPC: A61K31/4162 ,  A61K31/397 ,  A61K31/422 ,  A61K31/427 ,  C07D487/02 ,  C07D487/12

CPC classification number: C07D471/10 ,  C07D487/04 ,  C07D487/08

Abstract: Compounds are provided that act as potent modulators of one or more of the CCR1, CCR2 and CCR3 receptors. The compounds are generally fused-, spiro- or bridged-nitrogen heterocycles having an aryl and heteroaryl component and are useful in pharmaceutical compositions, methods for the treatment of CCR1-, CCR2- and/or CCR3-mediated diseases, and as controls in assays for the indentification of competitive receptor antagonists for the above chemokine receptors.

Abstract translation: 提供了作为CCR1，CCR2和CCR3受体中一种或多种的有效调节剂的化合物。 化合物通常是具有芳基和杂芳基组分的稠合，螺或氮杂环，并且可用于药物组合物，用于治疗CCR1，CCR2和/或CCR3介导的疾病的方法，以及用于测定中的对照 用于鉴定上述趋化因子受体的竞争性受体拮抗剂。

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：WO2005005436A3

公开(公告)日：2005-03-10

申请号：PCT/US2004022319

申请日：2004-07-09

Applicant: THERAVANCE INC ,  FATHEREE PAUL R ,  LINSELL MARTIN S ,  MARQUESS DANIEL ,  TRAPP SEAN G ,  MORAN EDMUND J ,  AGGEN JAMES B

Inventor： FATHEREE PAUL R ,  LINSELL MARTIN S ,  MARQUESS DANIEL ,  TRAPP SEAN G ,  MORAN EDMUND J ,  AGGEN JAMES B

IPC: A61K38/14 ,  A61P31/04 ,  C07D501/00 ,  C07K7/64 ,  C07K9/00 ,  A61K31/545

CPC classification number: C07K7/64 ,  C07D501/00 ,  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: 本发明提供了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; 用这种化合物治疗哺乳动物细菌感染的方法; 和用于制备这些化合物的方法和中间体。

公开(公告)号：WO2005005436A2

公开(公告)日：2005-01-20

申请号：PCT/US2004/022319

申请日：2004-07-09

Applicant: THERAVANCE, INC. ,  FATHEREE, Paul, R. ,  LINSELL, Martin S. ,  MARQUESS, Daniel ,  TRAPP, Sean, G. ,  MORAN, Edmund, J. ,  AGGEN, James B.

Inventor： FATHEREE, Paul, R. ,  LINSELL, Martin S. ,  MARQUESS, Daniel ,  TRAPP, Sean, G. ,  MORAN, Edmund, J. ,  AGGEN, James B.

IPC: C07D501/00

CPC classification number: C07K7/64 ,  C07D501/00 ,  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: 本发明提供了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。

公开(公告)号：WO2005056015A1

公开(公告)日：2005-06-23

申请号：PCT/US2004/041509

申请日：2004-12-08

Applicant: CHEMOCENTRYX, INC. ,  PENNELL, Andrew, M., K. ,  AGGEN, James, B. ,  WRIGHT, J., J., Kim ,  SEN, Subhabrata ,  MCMASTER, Brian, E. ,  DAIRAGHI, Daniel, Joseph ,  CHEN, Wei ,  ZHANG, Penglie

Inventor： PENNELL, Andrew, M., K. ,  AGGEN, James, B. ,  WRIGHT, J., J., Kim ,  SEN, Subhabrata ,  MCMASTER, Brian, E. ,  DAIRAGHI, Daniel, Joseph ,  CHEN, Wei ,  ZHANG, Penglie

IPC: A61K31/496

CPC classification number: C07D409/04 ,  C07D231/12 ,  C07D231/16 ,  C07D231/18 ,  C07D231/38 ,  C07D231/56 ,  C07D233/61 ,  C07D235/06 ,  C07D249/08 ,  C07D249/14 ,  C07D257/04 ,  C07D401/04 ,  C07D401/12 ,  C07D401/14 ,  C07D403/04 ,  C07D403/06 ,  C07D403/12 ,  C07D405/04 ,  C07D471/04 ,  C07D473/34

Abstract: Compounds are provided that act as potent antagonists of the CCR1 receptor, and have in vivo anti-inflammatory activity. The compounds are generally aryl piperazine derivatives and are useful in pharmaceutical compositions, methods for the treatment of CCR1-mediated diseases, and as controls in assays for the identification of competitive CCR1 antagonists.

Abstract translation: 提供了作为CCR1受体的有效拮抗剂并具有体内抗炎活性的化合物。 化合物通常为芳基哌嗪衍生物，并且可用于药物组合物，用于治疗CCR1介导的疾病的方法，以及用于鉴定竞争性CCR1拮抗剂的测定中的对照。

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：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。

公开(公告)号：WO2007027734A3

公开(公告)日：2007-03-08

申请号：PCT/US2006/033803

申请日：2006-08-29

Applicant: CHEMOCENTRYX, INC. ,  CHEN, Wei ,  ZHANG, Penglie ,  AGGEN, James, B. ,  DAIRAGHI, Daniel, Joseph ,  PENNELL, Andrew, M.K. ,  SEN, Subhabrata ,  WRIGHT, Kim, J., J.

Inventor： CHEN, Wei ,  ZHANG, Penglie ,  AGGEN, James, B. ,  DAIRAGHI, Daniel, Joseph ,  PENNELL, Andrew, M.K. ,  SEN, Subhabrata ,  WRIGHT, Kim, J., J.

IPC: C07D403/06

Abstract: Compounds are provided that act as potent modulators of one or more of the CCR1, CCR2 and CCR3 receptors. The compounds are generally fused-, spiro- or bridged-nitrogen heterocycles having an aryl and heteroaryl component and are useful in pharmaceutical compositions, methods for the treatment of CCR1-, CCR2- and/or CCR3-mediated diseases, and as controls in assays for the indentification of competitive receptor antagonists for the above chemokine receptors.

公开(公告)号：WO2005084667A1

公开(公告)日：2005-09-15

申请号：PCT/US2005/007166

申请日：2005-03-02

Applicant: CHEMOCENTRYX, INC. ,  PENNELL, Andrew, M., K. ,  AGGEN, James, B. ,  WRIGHT, J., J., Kim ,  SEN, Subharata ,  CHEN, Wei ,  DAIRAGHI, Daniel, Joseph ,  ZHANG, Penglie

Inventor： PENNELL, Andrew, M., K. ,  AGGEN, James, B. ,  WRIGHT, J., J., Kim ,  SEN, Subharata ,  CHEN, Wei ,  DAIRAGHI, Daniel, Joseph ,  ZHANG, Penglie

IPC: A61K31/4155

CPC classification number: C07D487/04 ,  C07D471/10 ,  C07D487/08

Abstract: Compounds are provided that act as potent modulators of one or more of the CCR1, CCR2 and CCR3 receptors. The compounds are generally fused-, spiro- or bridged-nitrogen heterocycles having an aryl and heteroaryl component and are useful in pharmaceutical compositions, methods for the treatment of CCR1-, CCR2- and/or CCR3-mediated diseases, and as controls in assays for the identification of competitive receptor antagonists for the above chemokine receptors.

Abstract translation: 提供了作为CCR1，CCR2和CCR3受体中一种或多种的有效调节剂的化合物。 化合物通常是具有芳基和杂芳基组分的稠合，螺或氮杂环，并且可用于药物组合物，用于治疗CCR1，CCR2和/或CCR3介导的疾病的方法，以及用于测定中的对照 用于鉴定上述趋化因子受体的竞争性受体拮抗剂。

公开(公告)号：WO2003105853A1

公开(公告)日：2003-12-24

申请号：PCT/US2003/018660

申请日：2003-06-11

Applicant: CHEMOCENTRYX, INC. ,  PENNELL, Andrew, M., K. ,  AGGEN, James, B. ,  WRIGHT, J., J., Kim ,  SEN, Subrabrata ,  MCMASTER, Brian, E. ,  DAIRAGHI, Daniel, Joseph

Inventor： PENNELL, Andrew, M., K. ,  AGGEN, James, B. ,  WRIGHT, J., J., Kim ,  SEN, Subrabrata ,  MCMASTER, Brian, E. ,  DAIRAGHI, Daniel, Joseph

IPC: A61K31/496

CPC classification number: C07D473/34 ,  C07D231/12 ,  C07D231/14 ,  C07D231/16 ,  C07D231/18 ,  C07D231/38 ,  C07D231/56 ,  C07D233/56 ,  C07D235/06 ,  C07D249/12 ,  C07D257/04 ,  C07D401/04 ,  C07D401/12 ,  C07D403/04 ,  C07D403/12 ,  C07D405/04 ,  C07D409/04

Abstract: Compounds are provided that act as potent antagonists of the CCR1 receptor, and which have been further confirmed in animal testing for inflammation, one of the hallmark disease states for CCR1. The compounds are generally aryl piperazine derivatives and are useful in pharmaceutical compositions, methods for the treatment of CCR1-mediated diseases, and as controls in assays for the identification of competitive CCR1 antagonists.

Abstract translation: 提供了作为CCR1受体的有效拮抗剂的化合物，并且在用于CCR1的标志性疾病状态之一的炎症的动物试验中进一步证实了这些化合物。 化合物通常为芳基哌嗪衍生物，并且可用于药物组合物，用于治疗CCR1介导的疾病的方法，以及用于鉴定竞争性CCR1拮抗剂的测定中的对照。