公开(公告)号：US08071622B2

公开(公告)日：2011-12-06

申请号：US11947146

申请日：2007-11-29

申请人： Caterina Bissantz ,  Christophe Grundschober ,  Raffaello Masciadri ,  Hasane Ratni ,  Mark Rogers-Evans ,  Patrick Schnider

发明人： Caterina Bissantz ,  Christophe Grundschober ,  Raffaello Masciadri ,  Hasane Ratni ,  Mark Rogers-Evans ,  Patrick Schnider

IPC分类号： A61K31/454 ,  C07D403/14

CPC分类号： C07D401/14 ,  C07D491/04

摘要： The present invention is concerned with novel indol-2-yl-carbonyl-piperidin-benzoimidazolon and indol-2-yl-carbonyl-piperidin-benzoxazolon derivatives as V1a receptor antagonists, their manufacture, pharmaceutical compositions containing them and their use for the treatment of anxiety and depressive disorders and other diseases. In particular, the present invention concerns compounds of formula (I) wherein R1 to R11, X and Y are as defined in the specification.

摘要翻译： 本发明涉及新的吲哚-2-基 - 羰基 - 哌啶 - 苯并咪唑酮和吲哚-2-基 - 羰基 - 哌啶 - 苯并恶唑酮衍生物作为V1a受体拮抗剂，其制备方法，含有它们的药物组合物及其用于治疗 焦虑抑郁障碍等疾病。 特别地，本发明涉及其中R 1至R 11，X和Y如说明书中所定义的式（I）化合物。

公开(公告)号：US07501432B2

公开(公告)日：2009-03-10

申请号：US11955440

申请日：2007-12-13

申请人： Caterina Bissantz ,  Christophe Grundschober ,  Raffaello Masciadri ,  Hasane Ratni ,  Mark Rogers-Evans ,  Patrick Schnider

发明人： Caterina Bissantz ,  Christophe Grundschober ,  Raffaello Masciadri ,  Hasane Ratni ,  Mark Rogers-Evans ,  Patrick Schnider

IPC分类号： A61K31/438 ,  C07D221/20

CPC分类号： C07D211/16 ,  C07D471/10 ,  C07D491/10 ,  C07D519/00

摘要： The present invention is concerned with novel spiro-piperidine derivatives as V1a receptor antagonists, their manufacture, pharmaceutical compositions containing them and their use as medicaments. The active compounds of the present invention are useful in the prevention and/or treatment of anxiety and depressive disorders and other diseases.In particular, the present invention is concerned with compounds of the general formula (I) wherein R1 to R5, R5′, X, Y and A are as defined in the specification.

公开(公告)号：US20080161304A1

公开(公告)日：2008-07-03

申请号：US11955425

申请日：2007-12-13

申请人： Caterina Bissantz ,  Christophe Grundschober ,  Raffaello Masciadri ,  Hasane Ratni ,  Mark Rogers-Evans ,  Patrick Schnider

发明人： Caterina Bissantz ,  Christophe Grundschober ,  Raffaello Masciadri ,  Hasane Ratni ,  Mark Rogers-Evans ,  Patrick Schnider

IPC分类号： A61K31/5377 ,  C07D471/20 ,  A61K31/438 ,  A61P25/00 ,  A61P9/00 ,  C07D295/00

CPC分类号： C07D211/16 ,  C07D471/10 ,  C07D491/10 ,  C07D519/00

摘要： The present invention is concerned with novel spiro-piperidine derivatives as V1a receptor antagonists, their manufacture, pharmaceutical compositions containing them and their use as medicaments. The active compounds of the present invention are useful in the prevention and/or treatment of anxiety and depressive disorders and other diseases.In particular, the present invention is concerned with compounds of the general formula (I) wherein R1 to R5, R5′, X, Y and A are as defined in the specification.

摘要翻译： 本发明涉及作为V1a受体拮抗剂的新型螺 - 哌啶衍生物，其制备方法，含有它们的药物组合物及其作为药物的用途。 本发明的活性化合物可用于预防和/或治疗焦虑和抑郁症等疾病。 特别地，本发明涉及通式（I）的化合物，其中R 1，R 5，R 5，R 5，X ，Y和A如说明书中所定义。

公开(公告)号：US20080139618A1

公开(公告)日：2008-06-12

申请号：US11947195

申请日：2007-11-29

申请人： Caterina Bissantz ,  Christophe Grundschober ,  Raffaello Masciadri ,  Hasane Ratni ,  Mark Rogers-Evans ,  Patrick Schnider

发明人： Caterina Bissantz ,  Christophe Grundschober ,  Raffaello Masciadri ,  Hasane Ratni ,  Mark Rogers-Evans ,  Patrick Schnider

IPC分类号： A61K31/454 ,  C07D401/08 ,  A61P25/00 ,  C07D401/14

CPC分类号： C07D401/14 ,  C07D491/04

摘要： The present invention is concerned with novel indol-2-yl-carbonyl-piperidin-benzoimidazolon and indol-2-yl-carbonyl-piperidin-benzoxazolon derivatives as V1a receptor antagonists, their manufacture, pharmaceutical compositions containing them and their use for the treatment of anxiety and depressive disorders and other diseases. In particular, the present invention concerns compounds of formula (I) wherein R1 to R11, X and Y are as defined in the specification.

公开(公告)号：US20080139549A1

公开(公告)日：2008-06-12

申请号：US11947851

申请日：2007-11-30

申请人： Caterina Bissantz ,  Christophe Grundschober ,  Raffaello Masciadri ,  Hasane Ratni ,  Mark Rogers-Evans ,  Patrick Schnider

发明人： Caterina Bissantz ,  Christophe Grundschober ,  Raffaello Masciadri ,  Hasane Ratni ,  Mark Rogers-Evans ,  Patrick Schnider

IPC分类号： A61K31/5377 ,  C07D401/08 ,  C07D401/14 ,  A61P25/00 ,  C07D413/14 ,  A61K31/454

CPC分类号： C07D401/04 ,  C07D413/14

摘要： The present invention is concerned with novel indol-2-yl-carbonyl-piperidine derivatives as V1a receptor antagonists, their manufacture, pharmaceutical compositions containing them and their use as medicaments. The active compounds of the present invention are useful in the prevention and/or treatment of anxiety and depressive disorders and other diseases. Present invention is concerned with compounds of the general formula (I) wherein R1 to R6, R8 to R14, R12′, R13′, X and Y are as defined in the specification.

摘要翻译： 本发明涉及作为V1a受体拮抗剂的新型吲哚-2-基 - 羰基 - 哌啶衍生物，其制备方法，含有它们的药物组合物及其作为药物的用途。 本发明的活性化合物可用于预防和/或治疗焦虑和抑郁症等疾病。 本发明涉及其中R 1至R 6，R 8至R 14的通式（I）的化合物， R 12，R 12，R 13，X和Y如说明书中所定义。

公开(公告)号：US08202993B2

公开(公告)日：2012-06-19

申请号：US11947953

申请日：2007-11-30

申请人： Caterina Bissantz ,  Christophe Grundschober ,  Raffaello Masciadri ,  Hasane Ratni ,  Mark Rogers-Evans ,  Patrick Schnider

发明人： Caterina Bissantz ,  Christophe Grundschober ,  Raffaello Masciadri ,  Hasane Ratni ,  Mark Rogers-Evans ,  Patrick Schnider

IPC分类号： C07D401/04 ,  A61K31/438

CPC分类号： C07D471/10 ,  C07D491/10 ,  C07D519/00

摘要： The present invention is concerned with novel indol-2-yl-carbonyl-spiro-piperidine derivatives as V1a receptor antagonists, their manufacture, pharmaceutical compositions containing them and their use for the treatment of anxiety, depressive disorders and other diseases. The compounds of present invention are represented by the general formula (I) wherein R1 to R1, X and Y are as defined in the specification.

摘要翻译： 本发明涉及作为V1a受体拮抗剂的新的吲哚-2-基 - 羰基 - 螺 - 哌啶衍生物，其制备方法，含有它们的药物组合物及其用于治疗焦虑，抑郁障碍和其它疾病的用途。 本发明的化合物由通式（I）表示，其中R 1至R 1，X和Y如说明书中所定义。

公开(公告)号：US08076360B2

公开(公告)日：2011-12-13

申请号：US11947851

申请日：2007-11-30

申请人： Caterina Bissantz ,  Christophe Grundschober ,  Raffaello Masciadri ,  Hasane Ratni ,  Mark Rogers-Evans ,  Patrick Schnider

发明人： Caterina Bissantz ,  Christophe Grundschober ,  Raffaello Masciadri ,  Hasane Ratni ,  Mark Rogers-Evans ,  Patrick Schnider

IPC分类号： A61K31/454 ,  C07D401/14

CPC分类号： C07D401/04 ,  C07D413/14

摘要： The present invention is concerned with novel indol-2-yl-carbonyl-piperidine derivatives as V1a receptor antagonists, their manufacture, pharmaceutical compositions containing them and their use as medicaments. The active compounds of the present invention are useful in the prevention and/or treatment of anxiety and depressive disorders and other diseases. Present invention is concerned with compounds of the general formula (I) wherein R1 to R6, R8 to R14, R12′, R13′, X and Y are as defined in the specification.

摘要翻译： 本发明涉及作为V1a受体拮抗剂的新型吲哚-2-基 - 羰基 - 哌啶衍生物，其制备方法，含有它们的药物组合物及其作为药物的用途。 本发明的活性化合物可用于预防和/或治疗焦虑和抑郁症等疾病。 本发明涉及通式（I）的化合物，其中R 1至R 6，R 8至R 14，R 12'，R 13'，X和Y如说明书中所定义。

公开(公告)号：US08022213B2

公开(公告)日：2011-09-20

申请号：US11947836

申请日：2007-11-30

申请人： Caterina Bissantz ,  Christophe Grundschober ,  Raffaello Masciadri ,  Hasane Ratni ,  Mark Rogers-Evans ,  Patrick Schnider

发明人： Caterina Bissantz ,  Christophe Grundschober ,  Raffaello Masciadri ,  Hasane Ratni ,  Mark Rogers-Evans ,  Patrick Schnider

IPC分类号： C07D401/04 ,  A61K31/438

CPC分类号： C07D471/10 ,  C07D498/10

摘要： Present invention is concerned with novel indol-2-yl-carbonyl-spiro-piperidine derivatives as V1a receptor antagonists, their manufacture, pharmaceutical compositions containing them. The active compounds of the present invention are useful in the treatment of anxiety and depressive disorders and other diseases. The compounds of present invention have the general formula (I) wherein R1 to R11 and X are as defined in the description.

摘要翻译： 本发明涉及作为V1a受体拮抗剂的新的吲哚-2-基 - 羰基 - 螺 - 哌啶衍生物，其制备方法，含有它们的药物组合物。 本发明的活性化合物可用于治疗焦虑抑郁障碍和其它疾病。 本发明的化合物具有通式（I），其中R 1至R 11和X如说明书中所定义。

公开(公告)号：US07498339B2

公开(公告)日：2009-03-03

申请号：US11969975

申请日：2008-01-07

申请人： Caterina Bissantz ,  Erwin Goetschi ,  Christophe Grundschober ,  Raffaello Masciadri ,  Hasane Ratni ,  Mark Rogers-Evans ,  Patrick Schnider

发明人： Caterina Bissantz ,  Erwin Goetschi ,  Christophe Grundschober ,  Raffaello Masciadri ,  Hasane Ratni ,  Mark Rogers-Evans ,  Patrick Schnider

IPC分类号： A61K31/438 ,  C07D491/107

CPC分类号： C07D491/113

摘要： In particular, the present invention is concerned with compounds of the general formula (I) wherein X, Y and R1 to R10 are as described herein. The compounds are V1a receptor antagonists. The invention also relates to the manufacture of compounds of formula I, pharmaceutical compositions containing them and their use for the treatment of anxiety and depressive disorders and other diseases.

摘要翻译： 特别地，本发明涉及通式（I）的化合物，其中X，Y和R 1至R 10如本文所述。 化合物是V1a受体拮抗剂。 本发明还涉及制备式I化合物，含有它们的药物组合物及其用于治疗焦虑和抑郁障碍和其它疾病的用途。

公开(公告)号：US20080269290A1

公开(公告)日：2008-10-30

申请号：US11998371

申请日：2007-11-29

申请人： Caterina Bissantz ,  Christophe Grundschober ,  Raffaello Masciadri ,  Hasane Ratni ,  Mark Rogers-Evans ,  Patrick Schnider

发明人： Caterina Bissantz ,  Christophe Grundschober ,  Raffaello Masciadri ,  Hasane Ratni ,  Mark Rogers-Evans ,  Patrick Schnider

IPC分类号： A61K31/454 ,  C07D211/04 ,  A61P25/22 ,  A61P25/24

CPC分类号： C07D401/14 ,  C07D491/04

摘要： The present invention is concerned with novel indol-2-yl-carbonyl-piperidin-benzoimidazolon and indol-2-yl-carbonyl-piperidin-benzoxazolon derivatives as V1a receptor antagonists, their manufacture, pharmaceutical compositions containing them and their use for the treatment of anxiety and depressive disorders and other diseases. In particular, the present invention concerns compounds of formula (I) wherein R1 to R11, X and Y are as defined in the specification.

摘要翻译： 本发明涉及新的吲哚-2-基 - 羰基 - 哌啶 - 苯并咪唑酮和吲哚-2-基 - 羰基 - 哌啶 - 苯并恶唑酮衍生物作为V1a受体拮抗剂，其制备方法，含有它们的药物组合物及其用于治疗 焦虑抑郁障碍等疾病。 特别地，本发明涉及式（I）的化合物，其中R 1至R 11，X和Y如说明书中所定义。