公开(公告)号：WO2008141249A1

公开(公告)日：2008-11-20

申请号：PCT/US2008/063343

申请日：2008-05-09

Applicant: ACADIA PHARMACEUTICALS INC. ,  GE HEALTHCARE, LTD. ,  OLSSON, Roger ,  BURSTEIN, Ethan ,  KNAPP, Anne, Eeg ,  ESKILDSEN, Jorgen ,  CASTILLO, Joel ,  NAIRNE, James ,  IVESON, Veronique, Morisson ,  ROBINS, Edward ,  GIBSON, Alex

Inventor： OLSSON, Roger ,  BURSTEIN, Ethan ,  KNAPP, Anne, Eeg ,  ESKILDSEN, Jorgen ,  CASTILLO, Joel ,  NAIRNE, James ,  IVESON, Veronique, Morisson ,  ROBINS, Edward ,  GIBSON, Alex

IPC: C07D471/04 ,  C07D487/04 ,  A61P29/00 ,  A61P25/00 ,  A61K31/437 ,  A61K31/4985 ,  A61K31/519

CPC classification number: C07D471/04 ,  C07D487/04

Abstract: Disclosed herein are compounds of Formula (I), or a pharmaceutically acceptable salt, ester, amide,thereof; and methods of modulating the activity of a cannabinoid CB2 receptor comprising contacting a compound of Formula I with the cannabinoid CB2 receptor. Also disclosed are methods of imaging of a tissue by positron emission tomography, the method comprising administering to the subject a compound of Formula I, wherein the compound comprises a radioisotope. Also disclosed are methods of measuring the relative concentration of cannabinoid CB2 receptors in tissue of a subject, by using a compound of Formula I which comprises a radioisotope. In addition, method of diagnosing a disorder in a subject are disclosed.

Abstract translation: 本文公开了式（I）的化合物或其药学上可接受的盐，酯，酰胺; 以及调节大麻素CB2受体的活性的方法，包括使式I化合物与大麻素CB2受体接触。 还公开了通过正电子发射断层摄影术对组织进行成像的方法，所述方法包括向受试者施用式I化合物，其中所述化合物包含放射性同位素。 还公开了通过使用包含放射性同位素的式I化合物来测量受试者组织中的大麻素CB 2受体的相对浓度的方法。 此外，公开了患者的病症诊断方法。

公开(公告)号：WO2008052072A2

公开(公告)日：2008-05-02

申请号：PCT/US2007/082414

申请日：2007-10-24

Applicant: ACADIA PHARMACEUTICALS INC. ,  OLSSON, Roger ,  KNAPP, Anne, Eeg ,  ESKILDSEN, Jorgen

Inventor： OLSSON, Roger ,  KNAPP, Anne, Eeg ,  ESKILDSEN, Jorgen

IPC: C07D235/12 ,  A61K31/4184 ,  A61P29/00

CPC classification number: C07D235/12

Abstract: Disclosed herein are benzoimidazole compounds; pharmaceutical compositions comprising a therapeutically effective amount of the same; methods of modulating the activity of an MrgX1 or an MrgX2 receptor using the same; and methods of alleviating acute, chronic and neuropathic pain in a subject using the same. Also disclosed are methods of identifying a benzoimidazole compound that modulates the activity of an MrgX1 or an MrgX2 receptor; methods of identifying a benzoimidazole compound effective for the treatment of pain.

Abstract translation: 本文公开了苯并咪唑化合物; 包含治疗有效量的药物组合物; 使用它们调节MrgX1或MrgX2受体活性的方法; 以及使用该方法减轻受试者中的急性，慢性和神经性疼痛的方法。 还公开了鉴定调节MrgX1或MrgX2受体活性的苯并咪唑化合物的方法; 鉴定有效治疗疼痛的苯并咪唑化合物的方法。

公开(公告)号：WO2008033894A2

公开(公告)日：2008-03-20

申请号：PCT/US2007/078236

申请日：2007-09-12

Applicant: ACADIA PHARMACEUTICALS INC. ,  PIU, Fabrice ,  GIL, Daniel W. ,  OLSSON, Roger ,  GUSTAFSSON, Magnus ,  HYLDTOFT, Lene ,  SIEMASKO, Karyn F. ,  STERN, Michael E.

Inventor： PIU, Fabrice ,  GIL, Daniel W. ,  OLSSON, Roger ,  GUSTAFSSON, Magnus ,  HYLDTOFT, Lene ,  SIEMASKO, Karyn F. ,  STERN, Michael E.

IPC: A61K31/09

CPC classification number: A61K31/09

Abstract: Disclosed herein are methods of treating neuropathic pain, reducing inflammation, reducing IL-4 levels, and reducing IFN-γ levels, using various di-aromatic compounds for use as estrogen receptors β agonists.

Abstract translation: 本文公开了使用各种二芳香族化合物作为雌激素受体β激动剂治疗神经性疼痛，减轻炎症，降低IL-4水平和降低IFN-γ水平的方法。

公开(公告)号：WO2007079239A3

公开(公告)日：2007-11-01

申请号：PCT/US2006049609

申请日：2006-12-29

Applicant: ACADIA PHARM INC ,  BURSTEIN ETHAN ,  EEG KNAPP ANNE ,  OLSSON ROGER ,  ESKILDSEN JORGEN ,  EK FREDRIK

Inventor： BURSTEIN ETHAN ,  EEG KNAPP ANNE ,  OLSSON ROGER ,  ESKILDSEN JORGEN ,  EK FREDRIK

IPC: C07D401/06 ,  A61K31/404 ,  A61P3/04 ,  C07D209/12 ,  C07D401/14 ,  C07D451/02 ,  C07D451/04 ,  C07D451/06 ,  C07D471/04

CPC classification number: C07D401/06 ,  C07D209/12 ,  C07D209/42 ,  C07D401/12 ,  C07D401/14 ,  C07D403/06 ,  C07D403/12 ,  C07D405/14 ,  C07D413/14 ,  C07D417/06 ,  C07D417/08 ,  C07D417/14 ,  C07D451/02 ,  C07D451/04 ,  C07D451/06 ,  C07D451/14 ,  C07D471/04 ,  C07D471/08 ,  C07D471/10 ,  C07D487/08 ,  C07D491/10 ,  C07D519/00

Abstract: Disclosed herein are compounds of Formula I as defined herein, or a pharmaceutically acceptable salt, ester, amide, or prodrug thereof, that modulates the activity of a ghrelin receptor. Disclosed herein are also methods of treating diseases or conditions that comprise administering to a subject in need thereof a therapeutically effective amount of a compound of Formula I.

Abstract translation: 本文公开了调节生长素释放肽受体活性的本文定义的式I化合物或其药学上可接受的盐，酯，酰胺或前药。 本文公开的方法还包括治疗疾病或病症的方法，其包括向有需要的受试者施用治疗有效量的式I化合物。

公开(公告)号：WO2006076317A2

公开(公告)日：2006-07-20

申请号：PCT/US2006000733

申请日：2006-01-09

Applicant: ACADIA PHARM INC ,  SCHLIENGER NATHALIE ,  THYGESEN MIKKEL BOAS ,  PAWLAS JAN ,  BADALASSI FABRIZIO ,  LEWINSKY RASMUS ,  LUND BIRGITTE WINTHER ,  OLSSON ROGER

Inventor： SCHLIENGER NATHALIE ,  THYGESEN MIKKEL BOAS ,  PAWLAS JAN ,  BADALASSI FABRIZIO ,  LEWINSKY RASMUS ,  LUND BIRGITTE WINTHER ,  OLSSON ROGER

IPC: C07D451/02 ,  A61K31/435 ,  A61P3/04 ,  A61P5/26 ,  A61P25/28

CPC classification number: C07D451/02 ,  C07D451/06

Abstract: Disclosed herein is a novel class of aminophenyl compounds having the structure (I) wherein R 1 is cyano or nitro and ring A is a bi- or tricyclic bridged heterocycle and to their use as modulators of androgen receptor for the treatment or prevention of conditions relating thereto.

Abstract translation: 本文公开了一类具有结构（I）的新型氨基苯基化合物，其中R 1是氰基或硝基且环A是双环或三环桥连杂环及其作为雄激素受体调节剂的用途， 治疗或预防相关病症。

公开(公告)号：WO2008021463A2

公开(公告)日：2008-02-21

申请号：PCT/US2007/018201

申请日：2007-08-15

Applicant: ACADIA PHARMACEUTICALS, INC. ,  EK, Fredrik ,  OLSSON, Roger ,  OHLSSON, Jorgen

Inventor： EK, Fredrik ,  OLSSON, Roger ,  OHLSSON, Jorgen

IPC: A61K31/5513 ,  A61K31/55 ,  A61P25/24 ,  A61P25/28

CPC classification number: A61K31/5513 ,  A61K31/55

Abstract: Disclosed herein are analogs of clozapine and pharmaceutically acceptable salts, esters, amides, or prodrugs thereof; methods of synthesizing the analogs; and methods of using the analogs for treating neuorpsychiatric disorders. In some embodiments, the analogs are amino substituted diaryl[a,d]cycloheptenes.

Abstract translation: 本文公开了氯氮平及其药学上可接受的盐，酯，酰胺或前药的类似物; 合成类似物的方法; 以及使用类似物治疗神经精神障碍的方法。 在一些实施方案中，类似物是氨基取代的二芳基[a，d]环庚烯。

公开(公告)号：WO2007079239A2

公开(公告)日：2007-07-12

申请号：PCT/US2006/049609

申请日：2006-12-29

Applicant: ACADIA PHARMACEUTICALS INC. ,  BURSTEIN, Ethan ,  EEG KNAPP, Anne ,  OLSSON, Roger ,  ESKILDSEN, Jorgen ,  EK, Fredrik

Inventor： BURSTEIN, Ethan ,  EEG KNAPP, Anne ,  OLSSON, Roger ,  ESKILDSEN, Jorgen ,  EK, Fredrik

IPC: C07D401/06 ,  C07D451/06 ,  C07D451/04 ,  C07D401/14 ,  C07D451/02 ,  C07D471/04 ,  C07D209/12 ,  A61K31/404 ,  A61P3/04

CPC classification number: C07D401/06 ,  C07D209/12 ,  C07D209/42 ,  C07D401/12 ,  C07D401/14 ,  C07D403/06 ,  C07D403/12 ,  C07D405/14 ,  C07D413/14 ,  C07D417/06 ,  C07D417/08 ,  C07D417/14 ,  C07D451/02 ,  C07D451/04 ,  C07D451/06 ,  C07D451/14 ,  C07D471/04 ,  C07D471/08 ,  C07D471/10 ,  C07D487/08 ,  C07D491/10 ,  C07D519/00

Abstract: Disclosed herein are compounds of Formula I as defined herein, or a pharmaceutically acceptable salt, ester, amide, or prodrug thereof, that modulates the activity of a ghrelin receptor. Disclosed herein are also methods of treating diseases or conditions that comprise administering to a subject in need thereof a therapeutically effective amount of a compound of Formula I.

Abstract translation: 本文公开了调节生长素释放肽受体活性的如本文所定义的式I化合物或其药学上可接受的盐，酯，酰胺或前药。 本文还公开了治疗疾病或病症的方法，其包括向有需要的受试者施用治疗有效量的式I化合物。

公开(公告)号：WO2007047737A1

公开(公告)日：2007-04-26

申请号：PCT/US2006/040662

申请日：2006-10-17

Applicant: ACADIA PHARMACEUTICALS INC. ,  OLSSON, Roger ,  EK, Fredrik ,  OTTESEN, Lars, Korsgaard ,  BULOW, Anne

Inventor： OLSSON, Roger ,  EK, Fredrik ,  OTTESEN, Lars, Korsgaard ,  BULOW, Anne

IPC: C07D419/12 ,  C07D267/20 ,  C07D245/06 ,  C07D225/08 ,  C07D295/18 ,  C07D337/14 ,  C07D281/16 ,  C07F7/08 ,  C07D419/04 ,  C07D417/04 ,  A61P25/00 ,  A61K31/5513 ,  A61K31/554 ,  A61K31/551

CPC classification number: C07D419/12 ,  C07D223/20 ,  C07D225/08 ,  C07D243/38 ,  C07D245/06 ,  C07D267/20 ,  C07D281/16 ,  C07D295/192 ,  C07D337/14 ,  C07D417/04 ,  C07D417/06 ,  C07D417/12 ,  C07D417/14 ,  C07D419/04

Abstract: Disclosed herein is a compound of Formula (I). Also disclosed herein is a method of modulating the activity of a cannabinoid receptor using a compound of Formula (I). Furthermore, disclosed herein is a method of treating a disease or condition that would be alleviated, improved or prevented by administration of a compound that modulates a cannabinoid receptor comprising identifying a subject in need thereof and administering to said subject a therapeutically effective amount of a compound of Formula (I). Also disclosed herein are pharmaceutical compositions comprising a compound of Formula (I).

Abstract translation: 本文公开了式（I）的化合物。 本文还公开了使用式（I）的化合物调节大麻素受体的活性的方法。 此外，本文公开的是治疗可以通过施用调节大麻素受体的化合物减轻，改善或预防的疾病或病症的方法，包括鉴定有需要的受试者，并向所述受试者施用治疗有效量的化合物 的式（I）。 本文还公开了包含式（I）化合物的药物组合物。

公开(公告)号：WO2005047899A3

公开(公告)日：2006-03-30

申请号：PCT/US2004036952

申请日：2004-11-04

Applicant: ACADIA PHARM INC ,  NASH NORMAN ,  SCULLY AUDRA L ,  GARDELL LUIS ,  OLSSON ROGER ,  GUSTAFSSON MAGNUS

Inventor： NASH NORMAN ,  SCULLY AUDRA L ,  GARDELL LUIS ,  OLSSON ROGER ,  GUSTAFSSON MAGNUS

IPC: C07D209/20 ,  C07D233/88 ,  C07D249/10 ,  C07D295/185 ,  C07D401/12 ,  C07D405/12 ,  G01N33/50

CPC classification number: C07D295/185 ,  C04B35/632 ,  C07D209/20 ,  C07D233/88 ,  C07D249/10 ,  C07D401/12 ,  C07D405/12 ,  G01N2333/726

Abstract: Disclosed herein are compounds that selectively activate the FPRL1 receptor. Further disclosed are methods of alleviating inflammatory responses by regulating key steps in leukocyte trafficking and preventing neutrophil-mediated tissue damage by administering to a subject a therapeutically effective amount of the compounds disclosed herein. In addition, methods of modulating, or specifically agonizing, the FPRL1 receptor by administering an effective amount of the compounds disclosed herein are provided.

Abstract translation: 本文公开了选择性活化FPRL1受体的化合物。 进一步公开的是通过调节白细胞运输中的关键步骤并通过向受试者施用治疗有效量的本文公开的化合物来预防嗜中性粒细胞介导的组织损伤来减轻炎症反应的方法。 此外，提供了通过施用有效量的本文公开的化合物调节或特异性激动FPRL1受体的方法。

公开(公告)号：WO2005063254A3

公开(公告)日：2005-07-14

申请号：PCT/US2004/043224

申请日：2004-12-21

Applicant: ACADIA PHARMACEUTICALS INC. ,  EK, Fredrik ,  OLSSON, Roger ,  OHLSSON, Jörgen

Inventor： EK, Fredrik ,  OLSSON, Roger ,  OHLSSON, Jörgen

IPC: A61K31/551

Abstract: Disclosed herein are analogs of clozapine and pharmaceutically acceptable salts, esters, amides, or prodrugs thereof; methods of synthesizing the analogs; and methods of using the analogs for treating neuorpsychiatric disorders. In some embodiments, the analogs are amino substituted diaryl[a,d]cycloheptenes.