公开(公告)号：US09625475B2

公开(公告)日：2017-04-18

申请号：US12727723

申请日：2010-03-19

Applicant: Michael R. Schrimpf ,  Chih-Hung Lee ,  Tao Li ,  Gregory A. Gfesser ,  Kathleen H. Mortell ,  Ramin Faghih ,  Diana L. Nersesian ,  Kevin B. Sippy ,  William H. Bunnelle ,  Marc Scanio ,  Lei Shi ,  Murali Gopalakrishnan ,  Diana L. Donnelly-Roberts ,  Min Hu

Inventor： Michael R. Schrimpf ,  Chih-Hung Lee ,  Tao Li ,  Gregory A. Gfesser ,  Kathleen H. Mortell ,  Ramin Faghih ,  Diana L. Nersesian ,  Kevin B. Sippy ,  William H. Bunnelle ,  Marc Scanio ,  Lei Shi ,  Murali Gopalakrishnan ,  Diana L. Donnelly-Roberts ,  Min Hu

IPC: A61K31/55 ,  C07D487/00 ,  C07D491/00 ,  C07D498/00 ,  C07D513/00 ,  C07D515/00 ,  G01N33/68 ,  C07D471/18 ,  C07D487/10 ,  G01N33/50

CPC classification number: G01N33/6896 ,  C07D471/18 ,  C07D487/10 ,  G01N33/5058 ,  G01N2800/2814 ,  G01N2800/30

Abstract: The present application relates to indole and indoline derivatives of formula (I), (II), (III), (IV), (V), or (VI) wherein a, R1, R2, R3, R4, R5, U, V, W, X, Y, and Z are as defined in the specification. The present application also relates to compositions comprising such compounds, and methods of treating disease conditions using such compounds and compositions, and methods for identifying such compounds.

公开(公告)号：US08314119B2

公开(公告)日：2012-11-20

申请号：US11935157

申请日：2007-11-05

Applicant: Michael R. Schrimpf ,  Diana L. Nersesian ,  Kevin B. Sippy ,  Jianguo Ji ,  Tao Li ,  Marc Scanio ,  Lei Shi ,  Chih-Hung Lee ,  William H. Bunnelle ,  Geoff G. Z. Zhang ,  Paul J. Brackemeyer ,  Shuang Chen ,  Rodger F. Henry

Inventor： Michael R. Schrimpf ,  Diana L. Nersesian ,  Kevin B. Sippy ,  Jianguo Ji ,  Tao Li ,  Marc Scanio ,  Lei Shi ,  Chih-Hung Lee ,  William H. Bunnelle ,  Geoff G. Z. Zhang ,  Paul J. Brackemeyer ,  Shuang Chen ,  Rodger F. Henry

IPC: A61K31/439 ,  C07D221/22

CPC classification number: C07D471/18 ,  A61K31/095 ,  A61K31/439 ,  A61K31/444 ,  A61K31/496 ,  A61K31/497 ,  A61K31/501 ,  A61K31/506 ,  A61K45/06 ,  C07C309/29 ,  C07D451/14 ,  C07D471/08 ,  C07F5/022

Abstract: The invention relates to compounds that are azaadamantane derivatives, particularly ether- or amine-substituted azaadamantane derivatives and salts and prodrugs thereof, compositions comprising such compounds, methods of using such compounds and compositions, processes for preparing such compounds, and intermediates obtained during such processes.

Abstract translation: 本发明涉及作为氮杂金刚烷衍生物的化合物，特别是醚取代或胺取代的氮杂金刚烷衍生物及其盐和前体药物，包含这些化合物的组合物，使用这些化合物和组合物的方法，制备这些化合物的方法以及在此过程中获得的中间体 。

公开(公告)号：US20110288069A1

公开(公告)日：2011-11-24

申请号：US13092332

申请日：2011-04-22

Applicant: William H. Bunnelle ,  Marc Scanio ,  Jason T. Brewer ,  Ying Wang ,  Irini Akritopoulou-Zanze

Inventor： William H. Bunnelle ,  Marc Scanio ,  Jason T. Brewer ,  Ying Wang ,  Irini Akritopoulou-Zanze

IPC: A61K31/5513 ,  A61P25/00 ,  A61K31/551 ,  C07D487/04 ,  C07D487/14

CPC classification number: C07D487/04 ,  C07D487/14

Abstract: The present application relates to benzodiazepine and pyridodiazepine derivatives of formula (I) wherein R1, R2, R3, R4, X1, Y1, Y2, and Y3 are as defined in the specification. The present application also relates to compositions comprising such compounds, and methods of treating disease conditions using such compounds and compositions, and methods for identifying such compounds.

Abstract translation: 本申请涉及式（I）的苯并二氮杂和吡啶并二氮杂衍生物，其中R 1，R 2，R 3，R 4，X 1，Y 1，Y 2和Y 3如说明书中所定义。 本申请还涉及包含这些化合物的组合物，以及使用这些化合物和组合物治疗疾病状况的方法，以及鉴定这些化合物的方法。

公开(公告)号：US20100249105A1

公开(公告)日：2010-09-30

申请号：US12727723

申请日：2010-03-19

Applicant: Michael R. Schrimpf ,  Chih-Hung Lee ,  Tao Li ,  Gregory A. Gfesser ,  Kathleen H. Mortell ,  Ramin Faghih ,  Diana L. Nersesian ,  Kevin B. Sippy ,  William H. Bunnelle ,  Marc Scanio ,  Lei Shi ,  Murali Gopalakrishnan ,  Diana L. Donnelly-Roberts ,  Min Hu

Inventor： Michael R. Schrimpf ,  Chih-Hung Lee ,  Tao Li ,  Gregory A. Gfesser ,  Kathleen H. Mortell ,  Ramin Faghih ,  Diana L. Nersesian ,  Kevin B. Sippy ,  William H. Bunnelle ,  Marc Scanio ,  Lei Shi ,  Murali Gopalakrishnan ,  Diana L. Donnelly-Roberts ,  Min Hu

IPC: A61K31/55 ,  A61P25/28 ,  A61P25/16 ,  A61P25/00 ,  A61P25/18 ,  A61P25/24 ,  A61P25/02 ,  C07D487/04 ,  A61K31/439 ,  C07D471/00

CPC classification number: G01N33/6896 ,  C07D471/18 ,  C07D487/10 ,  G01N33/5058 ,  G01N2800/2814 ,  G01N2800/30

Abstract: The present application relates to indole and indoline derivatives of formula (I), (II), (III), (IV), (V), or (VI) wherein a, R1, R2, R3, R4, R5, U, V, W, X, Y, and Z are as defined in the specification. The present application also relates to compositions comprising such compounds, and methods of treating disease conditions using such compounds and compositions, and methods for identifying such compounds.

公开(公告)号：US20100087471A1

公开(公告)日：2010-04-08

申请号：US12568085

申请日：2009-09-28

Applicant: Michael R. Schrimpf ,  Chih-Hung Lee ,  Tao Li ,  Gregory A. Gfesser ,  Kathleen H. Mortell ,  Ramin Faghih ,  Diana L. Nersesian ,  Kevin B. Sippy ,  William H. Bunnelle ,  Marc Scanio ,  Lei Shi ,  Murali Gopalakrishnan ,  Diana L. Donnelly-Roberts ,  Min Hu

Inventor： Michael R. Schrimpf ,  Chih-Hung Lee ,  Tao Li ,  Gregory A. Gfesser ,  Kathleen H. Mortell ,  Ramin Faghih ,  Diana L. Nersesian ,  Kevin B. Sippy ,  William H. Bunnelle ,  Marc Scanio ,  Lei Shi ,  Murali Gopalakrishnan ,  Diana L. Donnelly-Roberts ,  Min Hu

IPC: A61K31/439 ,  C12Q1/02 ,  C07D471/08

CPC classification number: G01N33/5058 ,  C07D471/18 ,  C07D487/10 ,  C07D487/18 ,  G01N33/6896 ,  G01N2800/28 ,  G01N2800/30

Abstract: The present application relates to indole and indoline derivatives of formula (I), (II), (III), (IV), (V), or (VI) wherein a, R1, R2, R3, R4, R5, U, V, W, X, Y, and Z are as defined in the specification. The present application also relates to compositions comprising such compounds, and methods of treating disease conditions using such compounds and compositions, and methods for identifying such compounds.

Abstract translation: 本申请涉及式（I），（II），（III），（IV），（V）或（VI）的吲哚和二氢吲哚衍生物，其中a，R1，R2，R3，R4，R5， V，W，X，Y和Z如说明书中所定义。 本申请还涉及包含这些化合物的组合物，以及使用这些化合物和组合物治疗疾病状况的方法，以及鉴定这些化合物的方法。

公开(公告)号：US09063126B2

公开(公告)日：2015-06-23

申请号：US12568085

申请日：2009-09-28

Applicant: Michael R. Schrimpf ,  Chih-Hung Lee ,  Tao Li ,  Gregory A. Gfesser ,  Kathleen H. Mortell ,  Ramin Faghih ,  Diana L. Nersesian ,  Kevin B. Sippy ,  William H. Bunnelle ,  Marc Scanio ,  Lei Shi ,  Murali Gopalakrishnan ,  Diana L. Donnelly-Roberts ,  Min Hu

Inventor： Michael R. Schrimpf ,  Chih-Hung Lee ,  Tao Li ,  Gregory A. Gfesser ,  Kathleen H. Mortell ,  Ramin Faghih ,  Diana L. Nersesian ,  Kevin B. Sippy ,  William H. Bunnelle ,  Marc Scanio ,  Lei Shi ,  Murali Gopalakrishnan ,  Diana L. Donnelly-Roberts ,  Min Hu

IPC: A61K31/439 ,  C07D471/08 ,  G01N33/50 ,  C07D471/18 ,  C07D487/10 ,  C07D487/18 ,  G01N33/68

CPC classification number: G01N33/5058 ,  C07D471/18 ,  C07D487/10 ,  C07D487/18 ,  G01N33/6896 ,  G01N2800/28 ,  G01N2800/30

Abstract: The present application relates to indole and indoline derivatives of formula (I), (II), (III), (IV), (V), or (VI) wherein a, R1, R2, R3, R4, R5, U, V, W, X, Y, and Z are as defined in the specification. The present application also relates to compositions comprising such compounds, and methods of treating disease conditions using such compounds and compositions, and methods for identifying such compounds.

Abstract translation: 本申请涉及式（I），（II），（III），（IV），（V）或（VI）的吲哚和二氢吲哚衍生物，其中a，R1，R2，R3，R4，R5， V，W，X，Y和Z如说明书中所定义。 本申请还涉及包含这些化合物的组合物，以及使用这些化合物和组合物治疗疾病状况的方法，以及鉴定这些化合物的方法。

公开(公告)号：US08673896B2

公开(公告)日：2014-03-18

申请号：US13092332

申请日：2011-04-22

Applicant: William H. Bunnelle ,  Marc Scanio ,  Jason T. Brewer ,  Ying Wang ,  Irini Akritopoulou-Zanze

Inventor： William H. Bunnelle ,  Marc Scanio ,  Jason T. Brewer ,  Ying Wang ,  Irini Akritopoulou-Zanze

IPC: A61K31/55 ,  C07D491/00 ,  C07D487/12

CPC classification number: C07D487/04 ,  C07D487/14

Abstract: The present application relates to benzodiazepine and pyridodiazepine derivatives of formula (I) wherein R1, R2, R3, R4, X1, Y1, Y2, and Y3 are as defined in the specification. The present application also relates to compositions comprising such compounds, and methods of treating disease conditions using such compounds and compositions, and methods for identifying such compounds.

Abstract translation: 本申请涉及式（I）的苯并二氮杂和吡啶并二氮杂衍生物，其中R 1，R 2，R 3，R 4，X 1，Y 1，Y 2和Y 3如说明书中所定义。 本申请还涉及包含这些化合物的组合物，以及使用这些化合物和组合物治疗疾病状况的方法，以及鉴定这些化合物的方法。

公开(公告)号：US20080167336A1

公开(公告)日：2008-07-10

申请号：US11935157

申请日：2007-11-05

Applicant: Michael R. Schrimpf ,  Diana L. Nersesian ,  Kevin B. Sippy ,  Jianguo Ji ,  Tao Li ,  Marc Scanio ,  Lei Shi ,  Chih-Hung Lee ,  William H. Bunnelle ,  Geoff G.Z. Zhang ,  Paul J. Brackemeyer ,  Shuang Chen ,  Rodger F. Henry

Inventor： Michael R. Schrimpf ,  Diana L. Nersesian ,  Kevin B. Sippy ,  Jianguo Ji ,  Tao Li ,  Marc Scanio ,  Lei Shi ,  Chih-Hung Lee ,  William H. Bunnelle ,  Geoff G.Z. Zhang ,  Paul J. Brackemeyer ,  Shuang Chen ,  Rodger F. Henry

IPC: A61K31/439 ,  C07D471/08 ,  C07F5/02

CPC classification number: C07D471/18 ,  A61K31/095 ,  A61K31/439 ,  A61K31/444 ,  A61K31/496 ,  A61K31/497 ,  A61K31/501 ,  A61K31/506 ,  A61K45/06 ,  C07C309/29 ,  C07D451/14 ,  C07D471/08 ,  C07F5/022

Abstract: The invention relates to compounds that are azaadamantane derivatives, particularly ether- or amine-substituted azaadamantane derivatives and salts and prodrugs thereof, compositions comprising such compounds, methods of using such compounds and compositions, processes for preparing such compounds, and intermediates obtained during such processes.

Abstract translation: 本发明涉及作为氮杂金刚烷衍生物的化合物，特别是醚取代或胺取代的氮杂金刚烷衍生物及其盐和前体药物，包含这些化合物的组合物，使用这些化合物和组合物的方法，制备这些化合物的方法以及在此过程中获得的中间体 。