公开(公告)号：US08664216B2

公开(公告)日：2014-03-04

申请号：US12613554

申请日：2009-11-06

申请人： Caterina Bissantz ,  Erwin Goetschi ,  Roland Jakob-Roetne ,  Raffaello Masciadri ,  Emmanuel Pinard ,  Hasane Ratni ,  Mark Rogers-Evans ,  Patrick Schnider

发明人： Caterina Bissantz ,  Erwin Goetschi ,  Roland Jakob-Roetne ,  Raffaello Masciadri ,  Emmanuel Pinard ,  Hasane Ratni ,  Mark Rogers-Evans ,  Patrick Schnider

IPC分类号： A61P9/00 ,  A61K31/55 ,  C07D487/12

CPC分类号： C07D487/04 ,  C07D491/107 ,  C07D495/10

摘要： The present invention is concerned with spiro-dihydrotetraazabenzoazulenes, i.e. spiro-5,6-dihydro-4H-2,3,5,10b-tetraaza-benzo[e]azulenes of formula I wherein R1, R2, R3, X, Y, Z, m and n are as described herein. The compounds according to the invention act as V1a receptor modulators and are useful as therapeutics acting peripherally and centrally in the conditions of dysmenorrhea, male or female sexual dysfunction, hypertension, chronic heart failure, inappropriate secretion of vasopressin, liver cirrhosis, nephrotic syndrome, anxiety, depressive disorders, obsessive compulsive disorder, autistic spectrum disorders, schizophrenia, and aggressive behavior.

摘要翻译： 本发明涉及式I的螺 - 二氢四氮杂苯并薁，即螺-5,6-二氢-4H-2,3,5,10b-四氮杂 - 苯并[e]薁其中R1，R2，R3，X，Y， Z，m和n如本文所述。 根据本发明的化合物作为V1a受体调节剂，并且可用作在痛经，男性或女性性功能障碍，高血压，慢性心力衰竭，不适当的血管加压素分泌，肝硬化，肾病综合征，焦虑症的周围和中心作用的治疗剂 抑郁障碍，强迫症，孤独症谱系障碍，精神分裂症和侵略行为。

公开(公告)号：US20100120751A1

公开(公告)日：2010-05-13

申请号：US12613554

申请日：2009-11-06

申请人： Caterina Bissantz ,  Erwin Goetschi ,  Roland Jakob-Roetne ,  Raffaello Masciadri ,  Emmanuel Pinard ,  Hasane Ratni ,  Mark Rogers-Evans ,  Patrick Schnider

发明人： Caterina Bissantz ,  Erwin Goetschi ,  Roland Jakob-Roetne ,  Raffaello Masciadri ,  Emmanuel Pinard ,  Hasane Ratni ,  Mark Rogers-Evans ,  Patrick Schnider

IPC分类号： A61K31/5513 ,  C07D487/14 ,  A61P5/00

CPC分类号： C07D487/04 ,  C07D491/107 ,  C07D495/10

摘要： The present invention is concerned with spiro-dihydrotetraazabenzoazulenes, i.e. spiro-5,6-dihydro-4H-2,3,5,10b-tetraaza-benzo[e]azulenes of formula I wherein R1, R2, R3, X, Y, Z, m and n are as described herein. The compounds according to the invention act as V1a receptor modulators and are useful as therapeutics acting peripherally and centrally in the conditions of dysmenorrhea, male or female sexual dysfunction, hypertension, chronic heart failure, inappropriate secretion of vasopressin, liver cirrhosis, nephrotic syndrome, anxiety, depressive disorders, obsessive compulsive disorder, autistic spectrum disorders, schizophrenia, and aggressive behavior.

摘要翻译： 本发明涉及式I的螺 - 二氢四氮杂苯并薁，即螺-5,6-二氢-4H-2,3,5,10b-四氮杂 - 苯并[e]薁其中R1，R2，R3，X，Y， Z，m和n如本文所述。 根据本发明的化合物作为V1a受体调节剂，并且可用作在痛经，男性或女性性功能障碍，高血压，慢性心力衰竭，不适当的血管加压素分泌，肝硬化，肾病综合征，焦虑症的周围和中心作用的治疗剂 抑郁障碍，强迫症，孤独症谱系障碍，精神分裂症和侵略行为。

公开(公告)号：US20080194610A1

公开(公告)日：2008-08-14

申请号：US11969983

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：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：US20080171760A1

公开(公告)日：2008-07-17

申请号：US11969993

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.

公开(公告)号：US20080171759A1

公开(公告)日：2008-07-17

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 ,  C07D491/10

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.

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.