公开(公告)号：US08946205B2

公开(公告)日：2015-02-03

申请号：US13319558

申请日：2010-05-11

Applicant: Jose Maria Cid-Nunez ,  Ana Isabel De Lucas Olivares ,  Andres Avelino Trabanco-Suarez ,  Gregor James MacDonald

Inventor： Jose Maria Cid-Nunez ,  Ana Isabel De Lucas Olivares ,  Andres Avelino Trabanco-Suarez ,  Gregor James MacDonald

IPC: A61K31/553 ,  A61K31/437 ,  A61K31/538 ,  A61K31/506 ,  C07D471/04 ,  C07D519/00 ,  A61K45/06 ,  A61K31/444 ,  A61K9/00 ,  A61K9/06 ,  A61K9/08 ,  A61K9/10 ,  A61K9/20

CPC classification number: C07D471/04 ,  A61K9/0014 ,  A61K9/0095 ,  A61K9/06 ,  A61K9/08 ,  A61K9/10 ,  A61K9/2009 ,  A61K9/2059 ,  A61K31/437 ,  A61K31/444 ,  A61K31/553 ,  A61K45/06 ,  C07D519/00 ,  A61K2300/00

Abstract: The present invention relates to novel triazolo[4,3-a]pyridine derivatives of Formula (I) wherein all radicals are as defined in the claims. The compounds according to the invention are positive allosteric modulators of the metabotropic glutamate receptor subtype 2 (“mGluR2”), which are useful for the treatment or prevention of neurological and psychiatric disorders associated with glutamate dysfunction and diseases in which the mGluR2 subtype of metabotropic receptors is involved. The invention is also directed to pharmaceutical compositions comprising such compounds, to processes to prepare such compounds and compositions, and to the use of such compounds for the prevention or treatment of neurological and psychiatric disorders and diseases in which mGluR2 is involved.

Abstract translation: 本发明涉及式（I）的新的三唑并[4,3-a]吡啶衍生物，其中所有基团如权利要求中所定义。 根据本发明的化合物是代谢型谷氨酸受体亚型2（“mGluR2”）的正变构调节剂，其可用于治疗或预防与谷氨酸功能障碍相关的神经和精神病学障碍以及代谢代谢受体的mGluR2亚型 参与。 本发明还涉及包含这种化合物的药物组合物，制备这些化合物和组合物的方法，以及这些化合物用于预防或治疗其中涉及mGluR2的神经和精神疾病和疾病的用途。

公开(公告)号：US08865725B2

公开(公告)日：2014-10-21

申请号：US13420333

申请日：2012-03-14

Applicant: P. Jeffrey Conn ,  Craig W. Lindsley ,  Shaun R. Stauffer ,  Jose Manuel Bartolome-Nebreda ,  Gregor James MacDonald ,  Susana Conde-Ceide ,  Carrie K. Jones ,  Maria Luz Martin-Martin ,  Han Min Tong

Inventor： P. Jeffrey Conn ,  Craig W. Lindsley ,  Shaun R. Stauffer ,  Jose Manuel Bartolome-Nebreda ,  Gregor James MacDonald ,  Susana Conde-Ceide ,  Carrie K. Jones ,  Maria Luz Martin-Martin ,  Han Min Tong

IPC: A01N43/90 ,  A61K31/519 ,  C07D487/00

CPC classification number: C07D487/04

Abstract: In one aspect, the invention relates to imidazopyrimidin-5(6H)-one analogs, derivatives thereof, and related compounds, which are useful as positive allosteric modulators of the metabotropic glutamate receptor subtype 5 (mGluR5); synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating neurological and psychiatric disorders associated with glutamate dysfunction using the compounds and compositions. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.

Abstract translation: 一方面，本发明涉及可用作代谢型谷氨酸受体亚型5（mGluR5）的正变构调节剂的咪唑并嘧啶-5（6H） - 酮类似物及其衍生物和相关化合物。 制备化合物的合成方法; 包含该化合物的药物组合物; 以及使用所述化合物和组合物治疗与谷氨酸官能障碍相关的神经和精神障碍的方法。 该摘要旨在作为用于在特定技术中进行搜索的扫描工具，而不意在限制本发明。

公开(公告)号：US08841323B2

公开(公告)日：2014-09-23

申请号：US12282663

申请日：2007-03-15

Applicant: Jose Maria Cid-Nunez ,  Jose Ignacio Andres-Gil ,  Andres Avelino Trabanco-Suarez ,  Julen Oyarzabal Santamarina ,  Frank Matthias Dautzenberg ,  Gregor James MacDonald ,  Shirley Elizabeth Pullan ,  Robert Johannes Lutjens ,  Guillaume Albert Jacques Duvey ,  Vanthea Nhem ,  Terry Patrick Finn ,  Gagik Melikyan ,  Vincent Mutel

Inventor： Hassan Julien Imogai ,  Jose Maria Cid-Nunez ,  Jose Ignacio Andres-Gil ,  Andres Avelino Trabanco-Suarez ,  Julen Oyarzabal Santamarina ,  Frank Matthias Dautzenberg ,  Gregor James MacDonald ,  Shirley Elizabeth Pullan ,  Robert Johannes Lutjens ,  Guillaume Albert Jacques Duvey ,  Vanthea Nhem ,  Terry Patrick Finn ,  Gagik Melikyan

IPC: A61K31/4439 ,  C07D213/85

CPC classification number: C07D213/85 ,  C07D213/84 ,  C07D401/04 ,  C07D401/06 ,  C07D401/10 ,  C07D401/12 ,  C07D401/14 ,  C07D405/04 ,  C07D405/06 ,  C07D405/12 ,  C07D409/04 ,  C07D413/04 ,  C07D413/10 ,  C07D413/12 ,  C07D417/04 ,  C07D417/12 ,  C07D471/04 ,  C07D471/10 ,  C07D487/08 ,  C07D491/04 ,  C07D491/10 ,  C07D495/04

Abstract: The present invention relates to novel compounds, in particular novel pyridinone derivatives according to Formula (I) wherein all radicals are defined in the application and claims. The compounds according to the invention are positive allosteric modulators of metabotropic receptors-subtype 2 (“mGluR2”) which are useful for the treatment or prevention of neurological and psychiatric disorders associated with glutamate dysfunction and diseases in which the mGluR2 subtype of metabotropic receptors is involved. In particular, such diseases are central nervous system disorders selected from the group of anxiety, schizophrenia, migraine, depression, and epilepsy. The invention is also directed to pharmaceutical compositions and processes to prepare such compounds and compositions, as well as to the use of such compounds for the prevention and treatment of such diseases in which mGluR2 is involved.

Abstract translation: 本发明涉及新型化合物，特别是根据式（I）的新型吡啶酮衍生物，其中所有基团在申请和权利要求书中定义。 根据本发明的化合物是代谢型受体亚型2（“mGluR2”）的正性变构调节剂，其可用于治疗或预防与谷氨酸功能障碍相关的神经和精神障碍以及参与代谢型受体的mGluR2亚型的疾病 。 特别地，这些疾病是选自焦虑，精神分裂症，偏头痛，抑郁症和癫痫组的中枢神经系统疾病。 本发明还涉及制备这些化合物和组合物的药物组合物和方法，以及这些化合物用于预防和治疗其中涉及mGluR2的疾病的用途。

公开(公告)号：US08777680B2

公开(公告)日：2014-07-15

申请号：US13158047

申请日：2011-06-10

Applicant: Kenneth James MacDonald

Inventor： Kenneth James MacDonald

IPC: B60F3/00

CPC classification number: B62B13/18 ,  B60F3/0038 ,  B60F3/0076 ,  B62B15/003 ,  B62B19/00 ,  B62B2206/006 ,  B63B1/14

Abstract: A kit for conversion of a snowmobile for use as a personal watercraft by replacement of the skis with steerable flotation ‘device’ and addition of outrigger flotation ‘device’ to suspend the track in the water while providing flotation to the chassis, along with the flotation provided by the steerable flotation ‘device’. The kit installs to the snowmobile without removing the track or engine drive, and without interference with operator control systems. Wheels may be included in keels of some hulls to allow for ease of access and egress from water to land.

Abstract translation: 一种用于转换雪地摩托车的套件，用作个人船舶，通过用易于浮选的装置更换滑雪板，并添加外伸支架浮选装置，将轨道悬挂在水中同时向底盘提供浮选以及浮选 由可操纵的浮选装置提供。 该套件安装到雪地车上，而不需要拆卸轨道或发动机驱动，并且不会干扰操作员控制系统。 车轮可能被包括在一些船体的龙骨中，以便于进出水和出水。

公开(公告)号：US08748621B2

公开(公告)日：2014-06-10

申请号：US13556547

申请日：2012-07-24

Applicant: Jose Maria Cid-Nunez ,  Andres Avelino Trabanco-Suarez ,  Gregor James MacDonald ,  Guillaume Albert Jacques Duvey ,  Robert Johannes Lutjens ,  Patrick Terry Finn

Inventor： Jose Maria Cid-Nunez ,  Andres Avelino Trabanco-Suarez ,  Gregor James MacDonald ,  Guillaume Albert Jacques Duvey ,  Robert Johannes Lutjens ,  Patrick Terry Finn

IPC: A61K31/44 ,  C07D211/72 ,  C07D213/64

CPC classification number: C07D213/64 ,  C07D401/12

Abstract: The present invention relates to a method of treating, ameliorating, or controlling a condition in a mammal, including a human, wherein the condition is selected from the group consisting of anxiety disorders, psychotic disorders, substance-dependence related disorders, mood disorders, epilepsy or convulsive disorders, idiopathic Parkinson's disease, and Alzheimer's disease, wherein the method comprises administering to the mammal an effective amount of a compound of Formula (I) wherein all radicals are as defined in the application and claims. In particular, such conditions are central nervous system disorders selected from the group of anxiety, schizophrenia, depression, and epilepsy.

Abstract translation: 本发明涉及一种治疗，改善或控制哺乳动物，包括人的病症的方法，其中所述病症选自焦虑症，精神障碍，物质依赖性相关疾病，情绪障碍，癫痫 或惊厥性疾病，特发性帕金森病和阿尔茨海默氏病，其中所述方法包括向哺乳动物施用有效量的式（I）化合物，其中所有基团如申请和权利要求中所定义。 特别地，这些病症是选自焦虑，精神分裂症，抑郁症和癫痫组的中枢神经系统疾病。

公开(公告)号：US08716282B2

公开(公告)日：2014-05-06

申请号：US13096545

申请日：2011-04-28

Applicant: Joaquin Pastor-Fernández ,  José Manuel Bartolomé-Nebreda ,  Gregor James Macdonald ,  Susana Conde-Ceide ,  Óscar Delgado-González ,  Greta Constantia Peter Vanhoof ,  Michiel Luc Maria Van Gool ,  María Luz Martín-Martín ,  Sergio-Alvar Alonso-de Diego ,  Kelly Ann Swinney ,  Carina Leys ,  Johan Erwin Edmond Weerts ,  Stijn Wuyts

Inventor： Joaquin Pastor-Fernández ,  José Manuel Bartolomé-Nebreda ,  Gregor James Macdonald ,  Susana Conde-Ceide ,  Óscar Delgado-González ,  Greta Constantia Peter Vanhoof ,  Michiel Luc Maria Van Gool ,  María Luz Martín-Martín ,  Sergio-Alvar Alonso-de Diego ,  Kelly Ann Swinney ,  Carina Leys ,  Johan Erwin Edmond Weerts ,  Stijn Wuyts

IPC: A61K31/5025 ,  A61K31/5377 ,  C07D413/14 ,  C07D403/14 ,  C07D487/04

CPC classification number: C07D487/04

Abstract: The present invention relates to novel imidazo[1,2-b]pyridazine derivatives which are inhibitors of the phosphodiesterase 10 enzyme (PDE10) and which are useful for the treatment or prevention of neurological, psychiatric and metabolic disorders in which the PDE10 enzyme is involved. The invention is also directed to pharmaceutical compositions comprising such compounds, to processes to prepare such compounds and compositions, to the use of such compounds or pharmaceutical compositions for the prevention or treatment of neurological, psychiatric and metabolic disorders and diseases.

Abstract translation: 本发明涉及作为磷酸二酯酶10酶（PDE10）的抑制剂的新的咪唑并[1,2-b]哒嗪衍生物，它们可用于治疗或预防涉及PDE10酶的神经，精神和代谢紊乱 。 本发明还涉及包含这些化合物的药物组合物，以制备这些化合物和组合物以使用这些化合物或药物组合物来预防或治疗神经，精神和代谢疾病和疾病。

公开(公告)号：US08691813B2

公开(公告)日：2014-04-08

申请号：US13131360

申请日：2009-11-24

Applicant: Jose Maria Cid-Nunez ,  Andres Avelino Trabanco-Suarez ,  Gregor James MacDonald

Inventor： Jose Maria Cid-Nunez ,  Andres Avelino Trabanco-Suarez ,  Gregor James MacDonald

IPC: C07D471/04 ,  A61K31/437

CPC classification number: C07D265/36

Abstract: The present invention relates to novel indole and benzoxazine derivatives which are positive allosteric modulators of the metabotropic glutamate receptor subtype 2 (“mGluR2”) and which are useful for the treatment or prevention of neurological and psychiatric disorders associated with glutamate dysfunction and diseases in which the mGluR2 subtype of metabotropic receptors is involved. The invention is also directed to pharmaceutical compositions comprising such compounds and to the use of such compounds and compositions for the prevention or treatment of neurological and psychiatric disorders and diseases in which mGluR2 is involved.

Abstract translation: 本发明涉及新的吲哚和苯并恶嗪衍生物，其是代谢型谷氨酸受体亚型2（“mGluR2”）的正性变构调节剂，其可用于治疗或预防与谷氨酸能力障碍相关的神经和精神障碍及其中 涉及代谢型受体的mGluR2亚型。 本发明还涉及包含这些化合物的药物组合物以及这些化合物和组合物用于预防或治疗其中涉及mGluR2的神经和精神疾病和疾病的用途。

公开(公告)号：US08637510B2

公开(公告)日：2014-01-28

申请号：US13512464

申请日：2010-11-25

Applicant: Gregor James Macdonald ,  Benoit Christian Albert Ghislain De Boeck ,  Joseph Elisabeth Leenaerts

Inventor： Gregor James Macdonald ,  Benoit Christian Albert Ghislain De Boeck ,  Joseph Elisabeth Leenaerts

IPC: A61K31/535 ,  C07D413/14

CPC classification number: C07D417/14

Abstract: The present invention relates to morpholinothiazole derivatives and pharmaceutically acceptable salts thereof, processes for preparing them, pharmaceutical compositions containing them and their use in therapy. The invention particularly relates to positive allosteric modulators of nicotinic acetylcholine receptors, such positive allosteric modulators having the capability to increase the efficacy of nicotinic receptor agonists.

Abstract translation: 本发明涉及吗啉代噻唑衍生物及其药学上可接受的盐，其制备方法，含有它们的药物组合物及其在治疗中的用途。 本发明特别涉及烟碱乙酰胆碱受体的正变构调节剂，这种正性变构调节剂具有增加烟碱受体激动剂功效的能力。

公开(公告)号：US20130197019A1

公开(公告)日：2013-08-01

申请号：US13803267

申请日：2013-03-14

Applicant: Jose Maria CID-NUNEZ ,  Andres Avelino Trabanco-Suarez ,  Gregor James Macdonald ,  Guillaume Albert Jacques Duvey ,  Robert Johannes Lütjens ,  Terry Patrick Finn

Inventor： Jose Maria CID-NUNEZ ,  Andres Avelino Trabanco-Suarez ,  Gregor James Macdonald ,  Guillaume Albert Jacques Duvey ,  Robert Johannes Lütjens ,  Terry Patrick Finn

IPC: C07D401/04 ,  C07D491/107 ,  A61K31/444 ,  A61K45/06 ,  A61K31/4545

CPC classification number: A61K31/4545 ,  A61K9/0014 ,  A61K9/0019 ,  A61K9/08 ,  A61K9/10 ,  A61K9/2009 ,  A61K9/2013 ,  A61K9/2018 ,  A61K9/2059 ,  A61K31/444 ,  A61K31/5377 ,  A61K45/06 ,  A61K47/10 ,  A61K47/44 ,  C07D211/86 ,  C07D401/04 ,  C07D491/107 ,  C07D493/10 ,  A61K2300/00

Abstract: The present invention relates to novel compounds, in particular novel pyridinone derivatives according to Formula (I) wherein all radicals are as defined in the application and claims. The compounds according to the invention are positive allosteric modulators of metabotropic receptors-subtype 2 (“mGluR2”) which are useful for the treatment or prevention of neurological and psychiatric disorders associated with glutamate dysfunction and diseases in which the mGluR2 subtype of metabotropic receptors is involved. In particular, such diseases are central nervous system disorders selected from the group of anxiety, schizophrenia, migraine, depression, and epilepsy. The invention is also directed to pharmaceutical compositions and processes to prepare such compounds and compositions, as well as to the use of such compounds for the prevention and treatment of such diseases in which mGluR2 is involved.

Abstract translation: 本发明涉及新化合物，特别是根据式（I）的新型吡啶酮衍生物，其中所有基团如申请和权利要求中所定义。 根据本发明的化合物是代谢型受体亚型2（“mGluR2”）的正性变构调节剂，其可用于治疗或预防与谷氨酸功能障碍相关的神经和精神障碍以及参与代谢型受体的mGluR2亚型的疾病 。 特别地，这些疾病是选自焦虑，精神分裂症，偏头痛，抑郁症和癫痫组的中枢神经系统疾病。 本发明还涉及制备这些化合物和组合物的药物组合物和方法，以及这些化合物用于预防和治疗其中涉及mGluR2的疾病的用途。

公开(公告)号：US20120329792A1

公开(公告)日：2012-12-27

申请号：US13583514

申请日：2011-03-08

Applicant: José Manuel Bartolomé-Nebreda ,  Susana Conde-Ceide ,  Gregor James MacDonald ,  Joaquin Pastor-Fernández ,  Michiel Luc Maria Van Gool ,  María Luz Martín-Martín ,  Greta Constantia Peter Vanhoof

Inventor： José Manuel Bartolomé-Nebreda ,  Susana Conde-Ceide ,  Gregor James MacDonald ,  Joaquin Pastor-Fernández ,  Michiel Luc Maria Van Gool ,  María Luz Martín-Martín ,  Greta Constantia Peter Vanhoof

IPC: A61K31/4985 ,  A61K31/5377 ,  A61P25/00 ,  A61P3/00 ,  A61P3/04 ,  A61P25/22 ,  A61P25/28 ,  A61P25/30 ,  A61P25/16 ,  A61P3/10 ,  C07D487/04 ,  A61P25/18

CPC classification number: C07D487/04 ,  A61K31/5377

Abstract: The present invention relates to novel imidazo[1,2-a]pyrazine derivatives which are inhibitors of the phosphodiesterase 10 enzyme (PDE10) and which are useful for the treatment or prevention of neurological, psychiatric and metabolic disorders in which the PDE10 enzyme is involved. The invention is also directed to pharmaceutical compositions comprising such compounds, to processes to prepare such compounds and compositions, to the use of such compounds or pharmaceutical compositions for the prevention or treatment of neurological, psychiatric and metabolic disorders and diseases.

Abstract translation: 本发明涉及作为磷酸二酯酶10酶（PDE10）的抑制剂的新的咪唑并[1,2-a]吡嗪衍生物，其可用于治疗或预防涉及PDE10酶的神经，精神和代谢紊乱 。 本发明还涉及包含这些化合物的药物组合物，以制备这些化合物和组合物以使用这些化合物或药物组合物来预防或治疗神经，精神和代谢疾病和疾病。