公开(公告)号：US08618155B2

公开(公告)日：2013-12-31

申请号：US12853202

申请日：2010-08-09

Applicant: Ofir Moreno ,  Sateesh Natarajan ,  David F. Duncan

Inventor： Ofir Moreno ,  Sateesh Natarajan ,  David F. Duncan

IPC: A61K31/415 ,  A61K31/4155

CPC classification number: C07C233/60 ,  A61K31/015 ,  A61K31/095 ,  A61K31/10 ,  A61K31/16 ,  A61K31/165 ,  A61K31/4155 ,  A61K31/4166 ,  A61K31/4184 ,  A61K31/4188 ,  C07C233/62 ,  C07C237/04 ,  C07C237/10 ,  C07C237/42 ,  C07C237/44 ,  C07C323/40 ,  C07C323/63 ,  C07C2601/14 ,  C07D231/40 ,  C07D235/26 ,  C07D401/12 ,  C07D403/04 ,  C07D405/04

Abstract: Provided are small-molecule Trp-p8 modulators, including Trp-p8 agonists and Trp-p8 antagonists, and compositions comprising small-molecule Trp-p8 agonists as well as methods for identifying and characterizing novel small-molecule Trp-p8 modulators and methods for decreasing viability and/or inhibiting growth of Trp-p8 expressing cells, methods for activating Trp-p8-mediated cation influx, methods for stimulating apoptosis and/or necrosis, and related methods for the treatment of diseases, including cancers such as lung, breast, colon, and/or prostate cancers as well as other diseases, such as benign prostatic hyperplasia, that are associated with Trp-p8 expression.

公开(公告)号：US08614243B2

公开(公告)日：2013-12-24

申请号：US12796587

申请日：2010-06-08

Applicant: Ofir Moreno ,  Sateesh Natarajan ,  David F. Duncan

Inventor： Ofir Moreno ,  Sateesh Natarajan ,  David F. Duncan

IPC: A61K31/415 ,  A61K31/4155 ,  C07D401/14 ,  C07D231/40

CPC classification number: C07C237/04 ,  C07C233/60 ,  C07C233/62 ,  C07C237/10 ,  C07C237/42 ,  C07C237/44 ,  C07C323/40 ,  C07C323/63 ,  C07C2601/14 ,  C07D231/40 ,  C07D235/26 ,  C07D401/12 ,  C07D403/04 ,  C07D405/04

Abstract: Provided are small-molecule Trp-p8 modulators, including Trp-p8 agonists and Trp-p8 antagonists, and compositions comprising small-molecule Trp-p8 agonists as well as methods for identifying and characterizing novel small-molecule Trp-p8 modulators and methods for decreasing viability and/or inhibiting growth of Trp-p8 expressing cells, methods for activating Trp-p8-mediated cation influx, methods for stimulating apoptosis and/or necrosis, and related methods for the treatment of diseases, including cancers such as lung, breast, colon, and/or prostate cancers as well as other diseases, such as benign prostatic hyperplasia, that are associated with Trp-p8 expression.

Abstract translation: 提供的是小分子Trp-p8调节剂，包括Trp-p8激动剂和Trp-p8拮抗剂，以及包含小分子Trp-p8激动剂的组合物以及用于鉴定和表征新型小分子Trp-p8调节剂的方法和方法 降低Trp-p8表达细胞的生存力和/或抑制Trp-p8表达细胞的生长，用于激活Trp-p8介导的阳离子流入的方法，用于刺激细胞凋亡和/或坏死的方法以及用于治疗疾病的相关方法，包括癌症如肺，乳腺 ，结肠癌和/或前列腺癌以及与Trp-p8表达相关的其它疾病，例如良性前列腺增生。

公开(公告)号：US20120225871A1

公开(公告)日：2012-09-06

申请号：US12796587

申请日：2010-06-08

Applicant: Ofir Moreno ,  Sateesh Natarajan ,  David F. Duncan

Inventor： Ofir Moreno ,  Sateesh Natarajan ,  David F. Duncan

IPC: A61K31/165 ,  C07D401/12 ,  C07C323/63 ,  C07D231/40 ,  C07D405/04 ,  C07D403/04 ,  C07C233/60 ,  C07D471/04 ,  C07D413/10 ,  A61K31/4184 ,  A61K31/4439 ,  A61K31/167 ,  A61K31/415 ,  A61K31/437 ,  A61K31/5377 ,  A61P35/00 ,  C12N5/09 ,  G01N21/76 ,  G01N21/63 ,  C07D235/26

CPC classification number: C07C237/04 ,  C07C233/60 ,  C07C233/62 ,  C07C237/10 ,  C07C237/42 ,  C07C237/44 ,  C07C323/40 ,  C07C323/63 ,  C07C2601/14 ,  C07D231/40 ,  C07D235/26 ,  C07D401/12 ,  C07D403/04 ,  C07D405/04

Abstract: Provided are small-molecule Trp-p8 modulators, including Trp-p8 agonists and Trp-p8 antagonists, and compositions comprising small-molecule Trp-p8 agonists as well as methods for identifying and characterizing novel small-molecule Trp-p8 modulators and methods for decreasing viability and/or inhibiting growth of Trp-p8 expressing cells, methods for activating Trp-p8-mediated cation influx, methods for stimulating apoptosis and/or necrosis, and related methods for the treatment of diseases, including cancers such as lung, breast, colon, and/or prostate cancers as well as other diseases, such as benign prostatic hyperplasia, that are associated with Trp-p8 expression.

公开(公告)号：US20120083493A1

公开(公告)日：2012-04-05

申请号：US12853202

申请日：2010-08-09

Applicant: Ofir Moreno ,  Sateesh Natarajan ,  David F. Duncan

Inventor： Ofir Moreno ,  Sateesh Natarajan ,  David F. Duncan

IPC: A61K31/167 ,  A61K31/4184 ,  A61P13/00 ,  A61K31/437 ,  A61K31/5377 ,  A61P13/08 ,  A61K31/4155 ,  A61K31/4439

CPC classification number: C07C233/60 ,  A61K31/015 ,  A61K31/095 ,  A61K31/10 ,  A61K31/16 ,  A61K31/165 ,  A61K31/4155 ,  A61K31/4166 ,  A61K31/4184 ,  A61K31/4188 ,  C07C233/62 ,  C07C237/04 ,  C07C237/10 ,  C07C237/42 ,  C07C237/44 ,  C07C323/40 ,  C07C323/63 ,  C07C2601/14 ,  C07D231/40 ,  C07D235/26 ,  C07D401/12 ,  C07D403/04 ,  C07D405/04

Abstract: Provided are small-molecule Trp-p8 modulators, including Trp-p8 agonists and Trp-p8 antagonists, and compositions comprising small-molecule Trp-p8 agonists as well as methods for identifying and characterizing novel small-molecule Trp-p8 modulators and methods for decreasing viability and/or inhibiting growth of Trp-p8 expressing cells, methods for activating Trp-p8-mediated cation influx, methods for stimulating apoptosis and/or necrosis, and related methods for the treatment of diseases, including cancers such as lung, breast, colon, and/or prostate cancers as well as other diseases, such as benign prostatic hyperplasia, that are associated with Trp-p8 expression.

Abstract translation: 提供的是小分子Trp-p8调节剂，包括Trp-p8激动剂和Trp-p8拮抗剂，以及包含小分子Trp-p8激动剂的组合物以及用于鉴定和表征新型小分子Trp-p8调节剂的方法和方法 降低Trp-p8表达细胞的生存力和/或抑制Trp-p8表达细胞的生长，用于激活Trp-p8介导的阳离子流入的方法，用于刺激细胞凋亡和/或坏死的方法以及用于治疗疾病的相关方法，包括癌症如肺，乳腺 ，结肠癌和/或前列腺癌以及与Trp-p8表达相关的其它疾病，例如良性前列腺增生。

公开(公告)号：US07772266B2

公开(公告)日：2010-08-10

申请号：US11942660

申请日：2007-11-19

Applicant: Ofir Moreno ,  Sateesh Natarajan ,  David F. Duncan

Inventor： Ofir Moreno ,  Sateesh Natarajan ,  David F. Duncan

IPC: A61K31/4166

CPC classification number: C07C233/60 ,  A61K31/015 ,  A61K31/095 ,  A61K31/10 ,  A61K31/16 ,  A61K31/165 ,  A61K31/4155 ,  A61K31/4166 ,  A61K31/4184 ,  A61K31/4188 ,  C07C233/62 ,  C07C237/04 ,  C07C237/10 ,  C07C237/42 ,  C07C237/44 ,  C07C323/40 ,  C07C323/63 ,  C07C2601/14 ,  C07D231/40 ,  C07D235/26 ,  C07D401/12 ,  C07D403/04 ,  C07D405/04

Abstract: Provided are small-molecule Trp-p8 modulators, including Trp-p8 agonists and Trp-p8 antagonists, and compositions comprising small-molecule Trp-p8 agonists as well as methods for identifying and characterizing novel small-molecule Trp-p8 modulators and methods for decreasing viability and/or inhibiting growth of Trp-p8 expressing cells, methods for activating Trp-p8-mediated cation influx, methods for stimulating apoptosis and/or necrosis, and related methods for the treatment of diseases, including cancers such as lung, breast, colon, and/or prostate cancers as well as other diseases, such as benign prostatic hyperplasia, that are associated with Trp-p8 expression.

Abstract translation: 提供的是小分子Trp-p8调节剂，包括Trp-p8激动剂和Trp-p8拮抗剂，以及包含小分子Trp-p8激动剂的组合物以及用于鉴定和表征新型小分子Trp-p8调节剂的方法和方法 降低Trp-p8表达细胞的生存力和/或抑制Trp-p8表达细胞的生长，用于激活Trp-p8介导的阳离子流入的方法，用于刺激细胞凋亡和/或坏死的方法以及用于治疗疾病的相关方法，包括癌症如肺，乳腺 ，结肠癌和/或前列腺癌以及与Trp-p8表达相关的其它疾病，例如良性前列腺增生。

公开(公告)号：US07741355B2

公开(公告)日：2010-06-22

申请号：US11707546

申请日：2007-02-15

Applicant: Ofir Moreno ,  Sateesh Natarajan ,  David F. Duncan

Inventor： Ofir Moreno ,  Sateesh Natarajan ,  David F. Duncan

IPC: A61K31/4166 ,  C07D235/04 ,  C07D487/04

CPC classification number: C07C237/04 ,  C07C233/60 ,  C07C233/62 ,  C07C237/10 ,  C07C237/42 ,  C07C237/44 ,  C07C323/40 ,  C07C323/63 ,  C07C2601/14 ,  C07D231/40 ,  C07D235/26 ,  C07D401/12 ,  C07D403/04 ,  C07D405/04

Abstract: Provided are small-molecule Trp-p8 modulators, including Trp-p8 agonists and Trp-p8 antagonists, and compositions comprising small-molecule Trp-p8 agonists as well as methods for identifying and characterizing novel small-molecule Trp-p8 modulators and methods for decreasing viability and/or inhibiting growth of Trp-p8 expressing cells, methods for activating Trp-p8-mediated cation influx, methods for stimulating apoptosis and/or necrosis, and related methods for the treatment of diseases, including cancers such as lung, breast, colon, and/or prostate cancers as well as other diseases, such as benign prostatic hyperplasia, that are associated with Trp-p8 expression.

Abstract translation: 提供的是小分子Trp-p8调节剂，包括Trp-p8激动剂和Trp-p8拮抗剂，以及包含小分子Trp-p8激动剂的组合物以及用于鉴定和表征新型小分子Trp-p8调节剂的方法和方法 降低Trp-p8表达细胞的生存力和/或抑制Trp-p8表达细胞的生长，用于激活Trp-p8介导的阳离子流入的方法，用于刺激细胞凋亡和/或坏死的方法以及用于治疗疾病的相关方法，包括癌症如肺，乳腺 ，结肠癌和/或前列腺癌以及与Trp-p8表达相关的其它疾病，例如良性前列腺增生。

公开(公告)号：US20080255185A1

公开(公告)日：2008-10-16

申请号：US11942660

申请日：2007-11-19

Applicant: Ofir Moreno ,  Sateesh Natarajan ,  David F. Duncan

Inventor： Ofir Moreno ,  Sateesh Natarajan ,  David F. Duncan

IPC: A61K31/437 ,  A61K31/4184 ,  A61K31/167 ,  A61K31/415 ,  A61K31/4439

CPC classification number: C07C233/60 ,  A61K31/015 ,  A61K31/095 ,  A61K31/10 ,  A61K31/16 ,  A61K31/165 ,  A61K31/4155 ,  A61K31/4166 ,  A61K31/4184 ,  A61K31/4188 ,  C07C233/62 ,  C07C237/04 ,  C07C237/10 ,  C07C237/42 ,  C07C237/44 ,  C07C323/40 ,  C07C323/63 ,  C07C2601/14 ,  C07D231/40 ,  C07D235/26 ,  C07D401/12 ,  C07D403/04 ,  C07D405/04

Abstract: Provided are small-molecule Trp-p8 modulators, including Trp-p8 agonists and Trp-p8 antagonists, and compositions comprising small-molecule Trp-p8 agonists as well as methods for identifying and characterizing novel small-molecule Trp-p8 modulators and methods for decreasing viability and/or inhibiting growth of Trp-p8 expressing cells, methods for activating Trp-p8-mediated cation influx, methods for stimulating apoptosis and/or necrosis, and related methods for the treatment of diseases, including cancers such as lung, breast, colon, and/or prostate cancers as well as other diseases, such as benign prostatic hyperplasia, that are associated with Trp-p8 expression.

Abstract translation: 提供的是小分子Trp-p8调节剂，包括Trp-p8激动剂和Trp-p8拮抗剂，以及包含小分子Trp-p8激动剂的组合物以及用于鉴定和表征新型小分子Trp-p8调节剂的方法和方法 降低Trp-p8表达细胞的生存力和/或抑制Trp-p8表达细胞的生长，用于激活Trp-p8介导的阳离子流入的方法，用于刺激细胞凋亡和/或坏死的方法以及用于治疗疾病的相关方法，包括癌症如肺，乳腺 ，结肠癌和/或前列腺癌以及与Trp-p8表达相关的其它疾病，例如良性前列腺增生。

公开(公告)号：US20070232603A1

公开(公告)日：2007-10-04

申请号：US11707546

申请日：2007-02-15

Applicant: Ofir Moreno ,  Sateesh Natarajan ,  David Duncan

Inventor： Ofir Moreno ,  Sateesh Natarajan ,  David Duncan

IPC: A61K31/5377 ,  A61K31/496 ,  A61K31/416 ,  A61K31/4184 ,  A61K31/415 ,  A61K31/16 ,  C07D413/02 ,  C07D403/02

CPC classification number: C07C237/04 ,  C07C233/60 ,  C07C233/62 ,  C07C237/10 ,  C07C237/42 ,  C07C237/44 ,  C07C323/40 ,  C07C323/63 ,  C07C2601/14 ,  C07D231/40 ,  C07D235/26 ,  C07D401/12 ,  C07D403/04 ,  C07D405/04

Abstract: Provided are small-molecule Trp-p8 modulators, including Trp-p8 agonists and Trp-p8 antagonists, and compositions comprising small-molecule Trp-p8 agonists as well as methods for identifying and characterizing novel small-molecule Trp-p8 modulators and methods for decreasing viability and/or inhibiting growth of Trp-p8 expressing cells, methods for activating Trp-p8-mediated cation influx, methods for stimulating apoptosis and/or necrosis, and related methods for the treatment of diseases, including cancers such as lung, breast, colon, and/or prostate cancers as well as other diseases, such as benign prostatic hyperplasia, that are associated with Trp-p8 expression.

Abstract translation: 提供的是小分子Trp-p8调节剂，包括Trp-p8激动剂和Trp-p8拮抗剂，以及包含小分子Trp-p8激动剂的组合物以及用于鉴定和表征新型小分子Trp-p8调节剂的方法和方法 降低Trp-p8表达细胞的生存力和/或抑制Trp-p8表达细胞的生长，用于激活Trp-p8介导的阳离子流入的方法，用于刺激细胞凋亡和/或坏死的方法以及用于治疗疾病的相关方法，包括癌症如肺，乳腺 ，结肠癌和/或前列腺癌以及与Trp-p8表达相关的其它疾病，例如良性前列腺增生。

公开(公告)号：US20050054651A1

公开(公告)日：2005-03-10

申请号：US10923413

申请日：2004-08-20

Applicant: Sateesh Natarajan ,  Ofir Moreno ,  Thomas Graddis ,  David Duncan ,  Reiner Laus ,  Feng Chen

Inventor： Sateesh Natarajan ,  Ofir Moreno ,  Thomas Graddis ,  David Duncan ,  Reiner Laus ,  Feng Chen

IPC: A61K31/498 ,  A61K31/517 ,  A61K45/06 ,  C07C311/20 ,  C07C311/37 ,  C07C323/40 ,  C07C323/44 ,  C07C333/06 ,  C07D207/06 ,  C07D207/09 ,  C07D207/32 ,  C07D207/325 ,  C07D209/08 ,  C07D209/14 ,  C07D209/20 ,  C07D209/48 ,  C07D213/40 ,  C07D215/04 ,  C07D215/08 ,  C07D215/46 ,  C07D217/06 ,  C07D231/12 ,  C07D231/14 ,  C07D231/56 ,  C07D235/18 ,  C07D235/26 ,  C07D239/42 ,  C07D241/18 ,  C07D241/44 ,  C07D251/54 ,  C07D263/34 ,  C07D263/56 ,  C07D263/57 ,  C07D279/12 ,  C07D295/096 ,  C07D295/135 ,  C07D295/26 ,  C07D307/52 ,  C07D317/66 ,  C07D333/34 ,  C07D401/04 ,  C07D405/12 ,  C07D413/04 ,  C07D413/12 ,  C07D417/04 ,  C07D471/04 ,  C07D487/04 ,  C07D493/08 ,  C07D495/04 ,  C07D513/04 ,  G01N33/68

CPC classification number: C07C233/60 ,  A61K31/498 ,  A61K31/517 ,  A61K45/06 ,  C07C233/58 ,  C07C243/36 ,  C07C243/38 ,  C07C311/20 ,  C07C311/37 ,  C07C323/40 ,  C07C323/44 ,  C07C333/06 ,  C07C2601/14 ,  C07C2601/18 ,  C07C2602/42 ,  C07D207/06 ,  C07D207/09 ,  C07D207/325 ,  C07D209/08 ,  C07D209/14 ,  C07D209/16 ,  C07D209/20 ,  C07D209/48 ,  C07D211/06 ,  C07D213/40 ,  C07D215/04 ,  C07D215/08 ,  C07D215/46 ,  C07D217/06 ,  C07D223/04 ,  C07D231/12 ,  C07D231/14 ,  C07D231/56 ,  C07D235/18 ,  C07D235/26 ,  C07D239/42 ,  C07D241/18 ,  C07D241/44 ,  C07D241/54 ,  C07D251/54 ,  C07D263/34 ,  C07D263/57 ,  C07D279/12 ,  C07D295/096 ,  C07D295/135 ,  C07D295/155 ,  C07D295/26 ,  C07D307/52 ,  C07D311/16 ,  C07D317/66 ,  C07D333/34 ,  C07D401/04 ,  C07D403/14 ,  C07D405/12 ,  C07D413/04 ,  C07D413/12 ,  C07D417/04 ,  C07D471/04 ,  C07D487/04 ,  C07D493/08 ,  C07D495/04 ,  C07D513/04 ,  G01N33/5011 ,  G01N33/6872 ,  G01N2500/10 ,  A61K2300/00

Abstract: Provided are small-molecule Trp-p8 modulators, including Trp-p8 agonists and Trp-p8 antagonists, and compositions comprising small-molecule Trp-p8 agonists as well as methods for identifying and characterizing novel small-molecule Trp-p8 modulators and methods for decreasing viability and/or inhibiting growth of Trp-p8 expressing cells, methods for activating Trp-p8-mediated cation influx, methods for stimulating apoptosis and/or necrosis, and related methods for the treatment of diseases, including cancers such as lung, breast, colon, and/or prostate cancers as well as other diseases, such as benign prostatic hyperplasia, that are associated with Trp-p8 expression.

Abstract translation: 提供的是小分子Trp-p8调节剂，包括Trp-p8激动剂和Trp-p8拮抗剂，以及包含小分子Trp-p8激动剂的组合物以及用于鉴定和表征新型小分子Trp-p8调节剂的方法和方法 降低Trp-p8表达细胞的生存力和/或抑制Trp-p8表达细胞的生长，用于激活Trp-p8介导的阳离子流入的方法，用于刺激细胞凋亡和/或坏死的方法以及用于治疗疾病的相关方法，包括癌症如肺，乳腺 ，结肠癌和/或前列腺癌以及与Trp-p8表达相关的其它疾病，例如良性前列腺增生。

公开(公告)号：US5888781A

公开(公告)日：1999-03-30

申请号：US815851

申请日：1997-03-12

Applicant: Michael Sierks ,  Sateesh Natarajan

Inventor： Michael Sierks ,  Sateesh Natarajan

IPC: C13K1/06 ,  C12P19/14 ,  C12N9/26 ,  C13K3/00

CPC classification number: C13K1/06

Abstract: A method for increasing the catalytic rate of starch hydrolases comprising reacting a starch hydrolase with a substrate therefor in the presence of about 0.001 to 80% (w/v) of an ethylene glycol or polyethylene glycol.

Abstract translation: 一种用于提高淀粉水解酶的催化速率的方法，包括在约0.001至80％（w / v）的乙二醇或聚乙二醇的存在下使淀粉水解酶与其底物反应。