公开(公告)号：US20130053371A1

公开(公告)日：2013-02-28

申请号：US13574018

申请日：2011-01-24

申请人： Joaquin Pastor Fernández ,  Sonia Martinez Gonzalez ,  Rosa Maria Alvarez Escobar ,  Antonlo Rodriguez Hergueta ,  José Ignacio Martin Hernando ,  Francisco Ramos Lima

发明人： Joaquin Pastor Fernández ,  Sonia Martinez Gonzalez ,  Rosa Maria Alvarez Escobar ,  Antonlo Rodriguez Hergueta ,  José Ignacio Martin Hernando ,  Francisco Ramos Lima

IPC分类号： A61K31/5377 ,  A61K31/551 ,  A61P35/00 ,  A61P37/02 ,  A61P31/12 ,  A61P29/00 ,  A61P3/00 ,  A61P25/00 ,  A61P11/00 ,  A61P37/08 ,  A61P37/06 ,  A61P17/06 ,  A61P25/28 ,  A61P5/00 ,  A61P35/02 ,  A61P1/16 ,  A61P19/08 ,  A61P9/10 ,  A61P13/12 ,  C07D487/04

CPC分类号： C07D487/04 ,  A61K31/5377 ,  C07D413/14

摘要： There is provided compounds of formula (I), wherein A1, A4, A4a, A5, B1, B1a, B2, B2a, B3, B3a, B4, B4a and R3 have meanings given in the description, and pharmaceutically-acceptable esters, amides, solvates or salts thereof, which compounds are useful in the treatment of diseases in which inhibition of a protein or lipid kinase (e.g. a PI3-K and/or mTOR) is desired and/or required, and particularly in the treatment of cancer or a proliferative disease.

摘要翻译： 提供式（I）化合物，其中A1，A4，A4a，A5，B1，B1a，B2，B2a，B3，B3a，B4，B4a和R3具有说明书中给出的含义，以及药学上可接受的酯，酰胺 ，其溶剂合物或其盐，该化合物可用于治疗其中期望和/或需要蛋白质或脂质激酶（例如PI3-K和/或mTOR）的抑制的疾病，特别是在治疗癌症或 增生性疾病。

公开(公告)号：US20130029967A1

公开(公告)日：2013-01-31

申请号：US13498059

申请日：2010-09-24

申请人： Joaquin Pastor Fernández ,  Sonia Martinez Gonzalez ,  Rosa Maria Alvarez Escobar ,  Sonsoles Rodriguez Aristegui ,  Esther Gonzales Cantalapiedra ,  Ana Isabel Hernandez Higueras ,  Carmen Varela Busto

发明人： Joaquin Pastor Fernández ,  Sonia Martinez Gonzalez ,  Rosa Maria Alvarez Escobar ,  Sonsoles Rodriguez Aristegui ,  Esther Gonzales Cantalapiedra ,  Ana Isabel Hernandez Higueras ,  Carmen Varela Busto

IPC分类号： A61K31/5377 ,  A61P35/00 ,  C07D471/14

CPC分类号： C07D487/04 ,  C07D487/14 ,  C07D519/00

摘要： There is provided compounds of formula (I), wherein A1, A2, A3, A4, n, the dotted lines, B1, B1a, B2, B2a, B3, B3a, B4, B4a, R2 and R3 have meanings given in the description, and pharmaceutically-acceptable esters, amides, solvates or salts thereof, which compounds are useful in the treatment of diseases in which inhibition of a protein kinase (e.g. a PI3-K and/or mTOR) is desired and/or required, and particularly in the treatment of cancer or a proliferative disease.

摘要翻译： 提供式（I）化合物，其中A1，A2，A3，A4，n，虚线B1，B1a，B2，B2a，B3，B3a，B4，B4a，R2和R3具有说明书中给出的含义 和其药学上可接受的酯，酰胺，溶剂合物或其盐，该化合物可用于治疗其中期望和/或需要抑制蛋白激酶（例如PI3-K和/或mTOR）的疾病，特别是 在治疗癌症或增殖性疾病。

公开(公告)号：US20090012062A1

公开(公告)日：2009-01-08

申请号：US12091365

申请日：2006-12-18

申请人： Jose Ignacio Andres-Gil ,  Manuel Jesus Alcazar-Vaca ,  Rosa Maria Alvarez-Escobar ,  Julen Oyarzabal Santamarina ,  Frank Matthias Dautzenberg ,  Jacqueline Macritchie ,  Donald Simpson ,  Sonia Martinez Gonzalez

发明人： Jose Ignacio Andres-Gil ,  Manuel Jesus Alcazar-Vaca ,  Rosa Maria Alvarez-Escobar ,  Julen Oyarzabal Santamarina ,  Frank Matthias Dautzenberg ,  Jacqueline Macritchie ,  Donald Simpson ,  Sonia Martinez Gonzalez

IPC分类号： A61K31/551 ,  A61K31/497 ,  C07D403/12 ,  A61P25/24 ,  A61P25/18 ,  C07D413/08 ,  A61K31/5377

CPC分类号： C07D241/20 ,  C07D401/04 ,  C07D401/10 ,  C07D401/12 ,  C07D401/14 ,  C07D403/10 ,  C07D403/12 ,  C07D491/10

摘要： The present invention concerns aryl and heteroaryl substituted pyrazinone derivatives having antagonistic melanin-concentrating hormone (MCH) activity, in particular MCH-1 activity according to the general Formula (I) a pharmaceutically acceptable acid or base addition salt thereof, a stereochemically isomeric form thereof, an N-oxide form thereof or a quaternary ammonium salt thereof, wherein the variables are defined in Claim 1. It further relates to their preparation, compositions comprising them and their use as a medicine. The compounds according to the invention are useful for the prevention and/or treatment of psychiatric disorders, including but not limited to anxiety, eating disorders, mood disorders, such as bipolar disorders and depression, psychoses, such as schizophrenia, and sleeping disorders; obesity; diabetes; sexual disorders and neurological disorders.

摘要翻译： 本发明涉及具有拮抗性黑色素浓缩激素（MCH）活性的芳基和杂芳基取代的吡嗪酮衍生物，特别是根据通式（I）的MCH-1活性，其药学上可接受的酸或碱加成盐，其立体化学异构形式 ，其N-氧化物形式或其季铵盐，其中所述变量在权利要求1中定义。它还涉及它们的制备，包含它们的组合物及其作为药物的用途。 根据本发明的化合物可用于预防和/或治疗精神病学障碍，包括但不限于焦虑，进食障碍，情绪障碍，例如双相性精神障碍和抑郁症，精神病如精神分裂症和睡眠障碍; 肥胖; 糖尿病; 性障碍和神经障碍。

公开(公告)号：US08815918B2

公开(公告)日：2014-08-26

申请号：US13262183

申请日：2010-04-01

申请人： Joaquin Pastor Fernández ,  Guido Kurz ,  Sonia Martinez Gonzalez

发明人： Joaquin Pastor Fernández ,  Guido Kurz ,  Sonia Martinez Gonzalez

IPC分类号： A61K31/433 ,  A61K31/4188 ,  C07D285/02 ,  C07D235/00

CPC分类号： C07D513/04

摘要： There is provided compounds of formula (I): wherein R1, R2 and R3 have meanings given in the description, and pharmaceutically-acceptable esters, amides, solvates or salts thereof, which compounds are useful in the treatment of diseases in which inhibition of a protein or lipid kinase (e.g. PI3-K, particularly class I PI3K) is desired and/or required, and particularly in the treatment of cancer.

摘要翻译： 提供式（I）化合物：其中R 1，R 2和R 3具有本说明书中给出的含义及其药学上可接受的酯，酰胺，溶剂化物或其盐，该化合物可用于治疗其中抑制 蛋白质或脂质激酶（例如PI3-K，特别是I型PI3K）是期望和/或需要的，特别是在治疗癌症中。

公开(公告)号：US20120094996A1

公开(公告)日：2012-04-19

申请号：US13262183

申请日：2010-04-01

申请人： Joaquin Pastor Fernández ,  Guido Kurz ,  Sonia Martinez Gonzalez

发明人： Joaquin Pastor Fernández ,  Guido Kurz ,  Sonia Martinez Gonzalez

IPC分类号： A61K31/433 ,  A61K31/4439 ,  A61K31/506 ,  A61K31/5377 ,  A61K31/4545 ,  A61K31/496 ,  A61P35/00 ,  A61P37/00 ,  A61P9/00 ,  A61P31/12 ,  A61P29/00 ,  A61P3/00 ,  A61P25/00 ,  A61P17/06 ,  A61P9/10 ,  A61P3/10 ,  A61P25/28 ,  A61P35/02 ,  C07D513/04

CPC分类号： C07D513/04

摘要： There is provided compounds of formula (I): wherein R1, R2 and R3 have meanings given in the description, and pharmaceutically-acceptable esters, amides, solvates or salts thereof, which compounds are useful in the treatment of diseases in which inhibition of a protein or lipid kinase (e.g. PI3-K, particularly class I PI3K) is desired and/or required, and particularly in the treatment of cancer.

摘要翻译： 提供式（I）化合物：其中R 1，R 2和R 3具有本说明书中给出的含义及其药学上可接受的酯，酰胺，溶剂化物或其盐，该化合物可用于治疗其中抑制 蛋白质或脂质激酶（例如PI3-K，特别是I型PI3K）是期望和/或需要的，特别是在治疗癌症中。

公开(公告)号：US20100105694A1

公开(公告)日：2010-04-29

申请号：US12445243

申请日：2007-10-10

申请人： José Ignacio Andrés-Gil ,  Manuel Jesús Alcázar-Vaca ,  Maria Lourdes Linares De La Morena ,  Sonia Martinez Gonzalez ,  Julen Oyarzabal Santamarina ,  Joaquin Pastor-Fernández ,  Juan Antonio Vega-Ramiro ,  Francisca Delgado-Jiménez ,  Wilhelmus Helena Ignatius Maria Drinkenburg

发明人： José Ignacio Andrés-Gil ,  Manuel Jesús Alcázar-Vaca ,  Maria Lourdes Linares De La Morena ,  Sonia Martinez Gonzalez ,  Julen Oyarzabal Santamarina ,  Joaquin Pastor-Fernández ,  Juan Antonio Vega-Ramiro ,  Francisca Delgado-Jiménez ,  Wilhelmus Helena Ignatius Maria Drinkenburg

IPC分类号： A61K31/497 ,  C07D401/12 ,  C07D401/14 ,  C07D405/14 ,  C07D403/04 ,  C07D403/14 ,  C07D413/14 ,  A61P25/00 ,  A61P25/28

CPC分类号： C07D401/12 ,  C07D241/20

摘要： The present invention concerns substituted pyrazinone derivatives according to the general Formula (I) a pharmaceutically acceptable acid or base addition salt thereof, a stereochemically isomeric form thereof, an N-oxide form thereof or a quaternary ammonium salt thereof, wherein the variables are defined in claim 1, having selective 2C-adrenoceptor antagonist activity. It further relates to their preparation, compositions comprising them and their use as a medicine. The compounds according to the invention are useful for the prevention and/or treatment of central nervous system disorders, mood disorders, anxiety disorders, stress-related disorders associated with depression and/or anxiety, cognitive disorders, personality disorders, schizoaffective disorders, Parkinson's disease, dementia of the Alzheimer's type, chronic pain conditions, neurodegenerative diseases, addiction disorders, mood disorders and sexual dysfunction.

摘要翻译： 本发明涉及根据通式（I）的取代的吡嗪酮衍生物，其药学上可接受的酸或碱加成盐，其立体化学异构形式，其N-氧化物形式或其季铵盐，其中变量定义于 权利要求1，具有选择性的2C-肾上腺素受体拮抗剂活性。 它还涉及它们的制备，包含它们的组合物及其作为药物的用途。 根据本发明的化合物可用于预防和/或治疗中枢神经系统疾病，情绪障碍，焦虑障碍，与抑郁和/或焦虑相关的压力相关疾病，认知障碍，人格障碍，分裂情感障碍，帕金森病 ，阿尔茨海默病的痴呆，慢性疼痛病症，神经变性疾病，成瘾症，情绪障碍和性功能障碍。

公开(公告)号：US09073927B2

公开(公告)日：2015-07-07

申请号：US13574018

申请日：2011-01-24

申请人： Joaquin Pastor Fernández ,  Sonia Martinez Gonzalez ,  Rosa Maria Álvarez Escobar ,  Antonio Rodriguez Hergueta ,  Jose Ignacio Martin Hernando ,  Francisco Javier Ramos Lima

发明人： Joaquin Pastor Fernández ,  Sonia Martinez Gonzalez ,  Rosa Maria Álvarez Escobar ,  Antonio Rodriguez Hergueta ,  Jose Ignacio Martin Hernando ,  Francisco Javier Ramos Lima

IPC分类号： A61K31/5377 ,  C07D413/14 ,  C07D487/04

CPC分类号： C07D487/04 ,  A61K31/5377 ,  C07D413/14

摘要： There is provided compounds of formula (I), wherein A1, A4, A4a, A5, B1, B1a, B2, B2a, B3, B3a, B4, B4a and R3 have meanings given in the description, and pharmaceutically-acceptable esters, amides, solvates or salts thereof, which compounds are useful in the treatment of diseases in which inhibition of a protein or lipid kinase (e.g. a PI3-K and/or mTOR) is desired and/or required, and particularly in the treatment of cancer or a proliferative disease.

摘要翻译： 提供式（I）化合物，其中A1，A4，A4a，A5，B1，B1a，B2，B2a，B3，B3a，B4，B4a和R3具有说明书中给出的含义，以及药学上可接受的酯，酰胺 ，其溶剂合物或其盐，该化合物可用于治疗其中期望和/或需要蛋白质或脂质激酶（例如PI3-K和/或mTOR）的抑制的疾病，特别是在治疗癌症或 增生性疾病。

公开(公告)号：US20130065881A1

公开(公告)日：2013-03-14

申请号：US13519872

申请日：2010-12-31

申请人： Joaquin Pastor Fernandez ,  Francisco Javier Ramos Lima ,  Ana Isabel Hernandez Higueras ,  Sonia Martinez Gonzalez ,  Jose Ignacio Martin Hernando ,  Carl-Gustave Pierre Saluste ,  Esther Gonzalez Cantalapiedra ,  Carmen Blanco Aparicio ,  Antonio Rodriguez Hergueta ,  Ana Maria Garcia Collazo ,  Antonio Salgado Serrano ,  Beatriz Noya Marino

发明人： Joaquin Pastor Fernandez ,  Francisco Javier Ramos Lima ,  Ana Isabel Hernandez Higueras ,  Sonia Martinez Gonzalez ,  Jose Ignacio Martin Hernando ,  Carl-Gustave Pierre Saluste ,  Esther Gonzalez Cantalapiedra ,  Carmen Blanco Aparicio ,  Antonio Rodriguez Hergueta ,  Ana Maria Garcia Collazo ,  Antonio Salgado Serrano ,  Beatriz Noya Marino

IPC分类号： C07D498/14 ,  C07D487/04 ,  A61K31/5025 ,  C07D519/00 ,  A61K31/55 ,  A61P35/00 ,  A61P9/00 ,  A61P37/02 ,  A61P31/12 ,  A61P29/00 ,  A61P3/00 ,  A61P5/00 ,  A61P25/00 ,  A61P11/00 ,  A61P37/08 ,  A61P17/06 ,  A61P19/08 ,  A61P25/28 ,  A61P9/10 ,  A61P3/10 ,  A61P1/16 ,  A61K31/5383

CPC分类号： C07D491/14 ,  C07D487/14

摘要： There is provided compounds of formula (I), wherein R1, R2, R3 and R4 have meanings given in the description (and which compounds are optionally substituted as indicated in the description), and pharmaceutically-acceptable esters, amides, solvates or salts thereof, which compounds are useful in the treatment of diseases in which inhibition of a protein or lipid kinase (e.g. a PIM family kinase, such as PIM-1, PIM-2 and/or PIM-3) is desired and/or required, and particularly in the treatment of cancer or a proliferative disease. There is also provided combinations comprising the compounds of formula (I).

摘要翻译： 提供式（I）化合物，其中R 1，R 2，R 3和R 4具有在说明书中给出的含义（和哪些化合物任选地如说明书所示取代）和其药学上可接受的酯，酰胺，溶剂化物或其盐 ，哪些化合物可用于治疗其中期望和/或需要抑制蛋白质或脂质激酶（例如PIM家族激酶，例如PIM-1，PIM-2和/或PIM-3）的疾病，以及 特别是在治疗癌症或增殖性疾病方面。 还提供了包含式（I）化合物的组合。

公开(公告)号：US20090281099A1

公开(公告)日：2009-11-12

申请号：US12301546

申请日：2007-05-21

申请人： José Ignacio Andrés-Gil ,  Manuel Jesús Alcázar-Vaca ,  Maria Lourdes Linares De La Morena ,  Sonia Martinez Gonzalez ,  Julen Oyarzabal Santamarina ,  Joaquin Pastor-Fernàndez ,  Juan Antonio Vega Ramiro ,  Francisca Delgado-Jiménez ,  Wilhelmus Helena Drinkenburg

发明人： José Ignacio Andrés-Gil ,  Manuel Jesús Alcázar-Vaca ,  Maria Lourdes Linares De La Morena ,  Sonia Martinez Gonzalez ,  Julen Oyarzabal Santamarina ,  Joaquin Pastor-Fernàndez ,  Juan Antonio Vega Ramiro ,  Francisca Delgado-Jiménez ,  Wilhelmus Helena Drinkenburg

IPC分类号： A61K31/5377 ,  A61K31/497 ,  C07D413/14 ,  C07D403/04 ,  C07D401/12

CPC分类号： C07D403/06 ,  C07D241/18 ,  C07D401/12 ,  C07D401/14 ,  C07D405/14

摘要： The present invention concerns substituted pyrazinone derivatives according to the general Formula (I) a pharmaceutically acceptable acid or base addition salt thereof, a stereochemically isomeric form thereof, an N-oxide form thereof or a quaternary ammonium salt thereof, wherein the variables are defined in Claim 1, having selective α2C-adrenoceptor antagonist activity. It further relates to their preparation, compositions comprising them and their use as a medicine. The compounds according to the invention are usefull for the prevention and/or treatment of central nervous system disorders, mood disorders, anxiety disorders, stress-related disorders associated with depression and/or anxiety, cognitive disorders, personality disorders, schizoaffective disorders, Parkinson's disease, dementia of the Alzheimer's type, chronic pain conditions, neurodegenerative diseases, addiction disorders, mood disorders and sexual dysfunction.

摘要翻译： 本发明涉及根据通式（I）的取代的吡嗪酮衍生物，其药学上可接受的酸或碱加成盐，其立体化学异构形式，其N-氧化物形式或其季铵盐，其中变量定义于 权利要求1，具有选择性α2C-肾上腺素受体拮抗剂活性。 它还涉及它们的制备，包含它们的组合物及其作为药物的用途。 根据本发明的化合物可用于预防和/或治疗中枢神经系统疾病，情绪障碍，焦虑障碍，与抑郁和/或焦虑相关的压力相关疾病，认知障碍，人格障碍，分裂情感障碍，帕金森病 ，阿尔茨海默病的痴呆，慢性疼痛病症，神经变性疾病，成瘾症，情绪障碍和性功能障碍。

公开(公告)号：US20090111801A1

公开(公告)日：2009-04-30

申请号：US12297670

申请日：2007-04-19

申请人： Jose Ignacio Andres-Gil ,  Manuel Jesus Alcazar-Vaca ,  Maria Lourdes Linares De La Morena ,  Sonia Martinez Gonzalez ,  Julen Oyarzabal Santamarina ,  Joaquin Pastor-Fernandez ,  Juan Antonio Vega Ramiro ,  Francisca Delgado-Jimenez ,  Wilhelmus Helena Ignatius Maria Drinkenburg

发明人： Jose Ignacio Andres-Gil ,  Manuel Jesus Alcazar-Vaca ,  Maria Lourdes Linares De La Morena ,  Sonia Martinez Gonzalez ,  Julen Oyarzabal Santamarina ,  Joaquin Pastor-Fernandez ,  Juan Antonio Vega Ramiro ,  Francisca Delgado-Jimenez ,  Wilhelmus Helena Ignatius Maria Drinkenburg

IPC分类号： A61K31/538 ,  C07D401/14 ,  A61K31/497 ,  A61P25/00 ,  A61K31/5377 ,  C07D413/14

CPC分类号： C07D401/12 ,  C07D239/47 ,  C07D401/14 ,  C07D403/06 ,  C07D405/06 ,  C07D405/14 ,  C07D409/06 ,  C07D409/14 ,  C07D413/06 ,  C07D413/14 ,  C07D417/06 ,  C07D417/14

摘要： The present invention concerns substituted pyrazinone derivatives according to the general Formula (I), a pharmaceutically acceptable acid or base addition salt thereof, a stereochemically isomeric form thereof, an N-oxide form thereof or a quaternary ammonium salt thereof, wherein the variables are defined in Claim 1, having selective α2C-adrenoceptor antagonist activity. It further relates to their preparation, compositions comprising them and their use as a medicine. The compounds according to the invention are useful for the prevention and/or treatment of central nervous system disorders, mood disorders, anxiety disorders, stress-related disorders associated with depression and/or anxiety, cognitive disorders, personality disorders, schizoaffective disorders, Parkinson's disease, dementia of the Alzheimer's type, chronic pain conditions, neurodegenerative diseases, addiction disorders, mood disorders and sexual dysfunction.

摘要翻译： 本发明涉及根据通式（I）的取代的吡嗪酮衍生物，其药学上可接受的酸或碱加成盐，其立体化学异构形式，其N-氧化物形式或其季铵盐，其中定义了变量 在权利要求1中，具有选择性α2C-肾上腺素受体拮抗剂活性。 它还涉及它们的制备，包含它们的组合物及其作为药物的用途。 根据本发明的化合物可用于预防和/或治疗中枢神经系统疾病，情绪障碍，焦虑障碍，与抑郁和/或焦虑相关的压力相关疾病，认知障碍，人格障碍，分裂情感障碍，帕金森病 ，阿尔茨海默病的痴呆，慢性疼痛病症，神经变性疾病，成瘾症，情绪障碍和性功能障碍。