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公开(公告)号：US07045529B2
公开(公告)日：2006-05-16
申请号：US09738666
申请日：2000-12-15
IPC分类号： A61K31/437 , C07D471/04
CPC分类号： C07D471/04 , C07D473/00
摘要： Provided herein are compounds of the formula (I): as well as stereoisomers and pharmaceutically acceptable salts thereof. Such compounds are, because of their ability to antagonize CRF, useful in the treatment of a variety of disorders characterized by execssive CRF expression. These include, for example: affective disorder, anxiety, depression, headache, irritable bowel syndrome, post-traumatic stress disorder, supranuclear palsy, immune suppression, Alzheimer's disease, Huntington's disease, Parkinson's disease, amyotrophic lateral sclerosis, gastrointestinal diseases, anorexia nervosa or other feeding disorder, drug addiction, drug or alcohol withdrawal symptoms, inflammatory diseases, cardiovascular or heart-related diseases, fertility problems, human immunodeficiency virus infections, hemorrhagic stress, obesity, infertility, head and spinal cord traumas, epilepsy, stroke, ulcers, amyotrophic lateral sclerosis and hypoglycemia.
摘要翻译： 本文提供了式（I）的化合物：及其立体异构体及其药学上可接受的盐。 因为这些化合物具有拮抗CRF的能力，其可用于治疗以执行性CRF表达为特征的多种疾病。 这些包括例如：情感障碍，焦虑症，抑郁症，头痛，肠易激综合征，创伤后应激障碍，核核性麻痹，免疫抑制，阿尔茨海默病，亨廷顿氏病，帕金森病，肌萎缩性侧索硬化，胃肠道疾病，神经性厌食症或 其他喂养障碍，药物成瘾，药物或酒精戒断症状，炎症性疾病，心血管疾病或心脏病，肥胖问题，人体免疫缺陷病毒感染，出血性压力，肥胖症，不育症，头部和脊髓创伤，癫痫，中风，溃疡， 肌萎缩性侧索硬化和低血糖。
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2.发明授权Heterocyclyl-substituted ring-fused pyridines and pyrimidines as corticotropin releasing hormone (CRH) antagonists, useful for treating cns and stress-related disorders 有权杂环取代的环稠合吡啶和嘧啶作为促肾上腺皮质激素释放激素（CRH）拮抗剂，可用于治疗cns和应激相关疾病公开(公告)号：US06525056B2
公开(公告)日：2003-02-25
申请号：US09789673
申请日：2001-02-21
IPC分类号： C07D47104
CPC分类号： C07D471/04 , C07D487/04
摘要： Corticotropin releasing factor (CRF) antagonists of Formula (I): and their use in treating psychiatric disorders and neurological diseases, anxiety-related disorders, post-traumatic stress disorder, supranuclear palsy and feeding disorders as well as treatment of immunological, cardiovascular or heart-related diseases and colonic hypersensitivity associated with psychopathological disturbance and stress in mammals.
摘要翻译： 式（I）的促肾上腺皮质激素释放因子（CRF）拮抗剂及其用于治疗精神疾病和神经系统疾病，焦虑相关疾病，创伤后应激障碍，核上性麻痹和进食障碍以及免疫学，心血管或心脏的治疗 与哺乳动物精神病理障碍和压力相关的疾病和结肠超敏反应。
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3.发明授权Heterocyclyl-substituted ring-fused pyridines and pyrimidines as corticotropin releasing hormone(CRH) antagonists, useful for treating CNS and stress-related disorders 有权杂环取代的环稠合吡啶和嘧啶作为促肾上腺皮质激素释放激素（CRH）拮抗剂，用于治疗CNS和应激相关疾病公开(公告)号：US06245769B1
公开(公告)日：2001-06-12
申请号：US09145231
申请日：1998-09-01
IPC分类号： A61K314192
CPC分类号： C07D471/04 , C07D487/04
摘要： Corticotropin releasing factor (CRF) antagonists of Formula (I): and their use in treating psychiatric disorders and neurological diseases, anxiety-related disorders, post-traumatic stress disorder, supranuclear palsy and feeding disorders as well as treatment of immunological, cardiovascular or heart-related diseases and colonic hypersensitivity associated with psychopathological disturbance and stress in mammals.
摘要翻译： 式（I）的促肾上腺皮质激素释放因子（CRF）拮抗剂及其用于治疗精神疾病和神经系统疾病，焦虑相关疾病，创伤后应激障碍，核上性麻痹和进食障碍以及免疫学，心血管或心脏的治疗 与哺乳动物精神病理障碍和压力相关的疾病和结肠超敏反应。
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4.发明授权Aryl- and heteroaryl-substituted tetrahydroisoquinolines and use thereof to block reuptake of norepinephrine, dopamine, and serotonin 有权芳基和杂芳基取代的四氢异喹啉及其用于阻断去甲肾上腺素，多巴胺和5-羟色胺的再摄取公开(公告)号：US08227486B2
公开(公告)日：2012-07-24
申请号：US12252823
申请日：2008-10-16
申请人： Bruce F. Molino , Shuang Liu , Peter R. Guzzo , James P. Beck
发明人： Bruce F. Molino , Shuang Liu , Peter R. Guzzo , James P. Beck
IPC分类号： A01N43/42 , A61K31/47 , C07D217/00
CPC分类号： C07D417/04 , A61K31/4709 , A61K31/4741 , A61K31/4743 , A61K31/502 , A61K31/517 , A61K31/53 , C07D217/00 , C07D217/04 , C07D217/08 , C07D217/12 , C07D217/14 , C07D217/16 , C07D217/20 , C07D401/04 , C07D401/12 , C07D401/14 , C07D403/04 , C07D403/12 , C07D405/04 , C07D405/12 , C07D405/14 , C07D407/04 , C07D409/04 , C07D409/12 , C07D409/14 , C07D413/04 , C07D413/12 , C07D413/14 , C07D417/12 , C07D417/14 , C07D471/04 , C07D487/04 , C07D495/04
摘要： The compounds of the present invention are represented by the chemical structure found in Formula (I): wherein: the carbon atom designated * is in the R or S configuration; and X is a fused bicyclic carbocycle or heterocycle selected from the group consisting of benzofuranyl, benzo[b]thiophenyl, benzoisothiazolyl, benzoisoxazolyl, indazolyl, indolyl, isoindolyl, indolizinyl, benzoimidazolyl, benzooxazolyl, benzothiazolyl, benzotriazolyl, imidazo[1,2-a]pyridinyl, pyrazolo[1,5-a]pyridinyl, [1,2,4]triazolo[4,3 -a]pyridinyl, thieno[2,3-b]pyridinyl, thieno[3,2-b]pyridinyl, 1H-pyrrolo[2,3-b]pyridinyl, indenyl, indanyl, dihydrobenzocycloheptenyl, tetrahydrobenzocycloheptenyl, dihydrobenzothiophenyl, dihydrobenzofuranyl, indolinyl, naphthyl, tetrahydronaphthyl, quinolinyl, isoquinolinyl, 4H-quinolizinyl, 9aH-quinolizinyl, quinazolinyl, cinnolinyl, phthalazinyl, quinoxalinyl, benzo[1,2,3]triazinyl, benzo[1,2,4]triazinyl, 2H-chromenyl, 4H-chromenyl, and a fused bicyclic carbocycle or fused bicyclic heterocycle optionally substituted with substituents (1 to 4 in number) as defined below in R14; with R1, R2, R3, R4, R5, R6, R7, R8, and R14 defined herein.
摘要翻译： 本发明的化合物由式（I）中所示的化学结构表示：其中：指定为*的碳原子为R或S构型; 并且X是选自苯并呋喃基，苯并[b]噻吩基，苯并异噻唑基，苯并异恶唑基，吲唑基，吲哚基，异吲哚基，吲嗪基，苯并咪唑基，苯并恶唑基，苯并噻唑基，苯并三唑基，咪唑并[1,2-a ]吡啶基，吡唑并[1,5-a]吡啶基，[1,2,4]三唑并[4,3-a]吡啶基，噻吩并[2,3-b]吡啶基，噻吩并[3,2-b] 二氢苯并噻吩基，二氢苯并呋喃基，二氢苯并噻吩基，四氢萘基，喹啉基，异喹啉基，4H-喹啉基，9H-喹啉基，喹唑啉基，噌啉基，酞嗪基，喹喔啉基， 苯并[1,2,3]三嗪基，苯并[1,2,4]三嗪基，2H-色烯基，4H-色烯基和稠合的双环碳环或稠合双环杂环，其任选被如所定义的取代基（数目为1至4） 在R14以下 本文定义的R1，R2，R3，R4，R5，R6，R7，R8和R14。
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公开(公告)号：US20090291970A1
公开(公告)日：2009-11-26
申请号：US12509938
申请日：2009-07-27
IPC分类号： A61K31/506 , C07D209/48 , C07D413/12 , C07D417/12 , C07D213/81 , C07D413/14 , A61K31/4035 , A61P25/28 , A61K31/422 , A61K31/427 , A61K31/44 , A61K31/4439
CPC分类号： C07C233/78 , C07C237/34 , C07C255/57 , C07C2601/02 , C07D213/30 , C07D213/81 , C07D239/26 , C07D263/32 , C07D277/30 , C07D413/04
摘要： The invention provides compounds of formula (I): useful in treating Alzheimer's disease and other similar diseases. These compounds include inhibitors of the beta-secretase enzyme that are useful in the treatment of Alzheimer's disease and other diseases characterized by deposition of A beta peptide in a mammal. The compounds of the invention are useful in pharmaceutical compositions and methods of treatment to reduce A beta peptide formation.
摘要翻译： 本发明提供式（I）化合物：可用于治疗阿尔茨海默病和其他类似疾病。 这些化合物包括β-分泌酶的抑制剂，其可用于治疗阿尔茨海默病和以哺乳动物中Aβ肽沉积为特征的其它疾病。 本发明的化合物可用于降低Aβ肽形成的药物组合物和治疗方法。
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公开(公告)号：US07612090B2
公开(公告)日：2009-11-03
申请号：US10426097
申请日：2003-04-29
申请人： James P. Beck , Matt A. Curry , Mark A. Smith
发明人： James P. Beck , Matt A. Curry , Mark A. Smith
IPC分类号： C07D217/00 , A61K31/47
CPC分类号： C07D401/04 , C07D217/04 , C07D405/04 , C07D409/04 , C07D413/04
摘要： Provided herein are compounds of the formula (I): wherein R1-R8 are as described herein, R4 being aryl or heteroaryl Such compounds are particularly useful in the treatment of a disorder which is created by or is dependent upon decreased availability of serotonin, norepinephrine or dopamine.
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7.发明授权Aryl- and heteroaryl-substituted tetrahydroisoquinolines and use thereof to block reuptake of norepinephrine, dopamine, and serotonin 有权芳基和杂芳基取代的四氢异喹啉及其用于阻断去甲肾上腺素，多巴胺和5-羟色胺的再摄取公开(公告)号：US07541357B2
公开(公告)日：2009-06-02
申请号：US11183066
申请日：2005-07-15
申请人： Bruce F. Molino , Shuang Liu , Peter R. Guzzo , James P. Beck
发明人： Bruce F. Molino , Shuang Liu , Peter R. Guzzo , James P. Beck
IPC分类号： C07D403/04 , C07D217/02 , A61K31/47
CPC分类号： C07D417/04 , A61K31/4709 , A61K31/4741 , A61K31/4743 , A61K31/502 , A61K31/517 , A61K31/53 , C07D217/00 , C07D217/04 , C07D217/08 , C07D217/12 , C07D217/14 , C07D217/16 , C07D217/20 , C07D401/04 , C07D401/12 , C07D401/14 , C07D403/04 , C07D403/12 , C07D405/04 , C07D405/12 , C07D405/14 , C07D407/04 , C07D409/04 , C07D409/12 , C07D409/14 , C07D413/04 , C07D413/12 , C07D413/14 , C07D417/12 , C07D417/14 , C07D471/04 , C07D487/04 , C07D495/04
摘要： The compounds of the present invention are represented by the chemical structure found in Formula (I): wherein: the carbon atom designated * is in the R or S configuration; and X is a fused bicyclic carbocycle or heterocycle selected from the group consisting of benzofuranyl, benzo[b]thiophenyl, benzoisothiazolyl, benzoisoxazolyl, indazolyl, indolyl, isoindolyl, indolizinyl, benzoimidazolyl, benzooxazolyl, benzothiazolyl, benzotriazolyl, imidazo[1,2-a]pyridinyl, pyrazolo[1,5-a]pyridinyl, [1,2,4]triazolo[4,3-a]pyridinyl, thieno[2,3-b]pyridinyl, thieno[3,2-b]pyridinyl, 1H-pyrrolo[2,3-b]pyridinyl, indenyl, indanyl, dihydrobenzocycloheptenyl, tetrahydrobenzocycloheptenyl, dihydrobenzothiophenyl, dihydrobenzofuranyl, indolinyl, naphthyl, tetrahydronaphthyl, quinolinyl, isoquinolinyl, 4H-quinolizinyl, 9aH-quinolizinyl, quinazolinyl, cinnolinyl, phthalazinyl, quinoxalinyl, benzo[1,2,3]triazinyl, benzo[1,2,4]triazinyl, 2H-chromenyl, 4H-chromenyl, and a fused bicyclic carbocycle or fused bicyclic heterocycle optionally substituted with substituents (1 to 4 in number) as defined in R14; with R1, R2, R3, R4, R5, R6, R7, R8, and R14 defined herein.
摘要翻译： 本发明的化合物由式（I）中所示的化学结构表示：其中：指定为*的碳原子为R或S构型; 并且X是选自苯并呋喃基，苯并[b]噻吩基，苯并异噻唑基，苯并异恶唑基，吲唑基，吲哚基，异吲哚基，吲嗪基，苯并咪唑基，苯并恶唑基，苯并噻唑基，苯并三唑基，咪唑并[1,2-a 吡啶并[1,5-a]吡啶基，[1,2,4]三唑并[4,3-a]吡啶基，噻吩并[2,3-b]吡啶基，噻吩并[3,2-b] 二氢苯并噻吩基，二氢苯并呋喃基，二氢苯并噻吩基，四氢萘基，喹啉基，异喹啉基，4H-喹啉基，9H-喹啉基，喹唑啉基，噌啉基，酞嗪基，喹喔啉基， 苯并[1,2,3]三嗪基，苯并[1,2,4]三嗪基，2H-色烯基，4H-色烯基和稠合的双环碳环或稠合双环杂环，其任选被如所定义的取代基（数目为1至4） 在R14; 本文定义的R1，R2，R3，R4，R5，R6，R7，R8和R14。
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公开(公告)号：US07456163B2
公开(公告)日：2008-11-25
申请号：US11208382
申请日：2005-08-19
申请人： Shon R. Pulley , James P. Beck , Ruth E. TenBrink , Jon S. Jacobs
发明人： Shon R. Pulley , James P. Beck , Ruth E. TenBrink , Jon S. Jacobs
IPC分类号： C07D273/02 , C07D291/08 , C07D413/04 , C07D413/12 , C07D498/08 , A61P25/28
CPC分类号： C07D413/04 , C07D273/02 , C07D413/12 , C07D413/14
摘要： The present invention is macrocycles of the formula (X): for treating Alzheimer's disease and other similar diseases. These compounds include inhibitors of the beta-secretase enzyme for the treatment of Alzheimer's disease and other diseases characterized by deposition of A beta peptide in a mammal. The compounds of the invention are useful in pharmaceutical compositions and methods of treatment to reduce A beta peptide formation.
摘要翻译： 本发明是式（X）的大环化合物：用于治疗阿尔茨海默病和其他类似疾病。 这些化合物包括用于治疗阿尔茨海默病的β-分泌酶的抑制剂和以哺乳动物中Aβ肽沉积为特征的其它疾病。 本发明的化合物可用于降低Aβ肽形成的药物组合物和治疗方法。
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公开(公告)号：US07442691B2
公开(公告)日：2008-10-28
申请号：US11218879
申请日：2005-09-02
申请人： Shon R. Pulley , James P. Beck , Ruth E. TenBrink
发明人： Shon R. Pulley , James P. Beck , Ruth E. TenBrink
IPC分类号： A61P25/28
CPC分类号： C07D413/12 , C07D273/02
摘要： The present invention are macrocycles of the formula (IX): for treating Alzheimer's disease and other similar diseases. These compounds include inhibitors of the beta-secretase enzyme that are useful in the treatment of Alzheimer's disease and other diseases characterized by deposition of A beta peptide in a mammal. The compounds of the invention are useful in pharmaceutical compositions and methods of treatment to reduce A beta peptide formation.
摘要翻译： 本发明是式（Ⅸ）的大环化合物：用于治疗阿尔茨海默病和其它类似疾病。 这些化合物包括β-分泌酶的抑制剂，其可用于治疗阿尔茨海默病和以哺乳动物中Aβ肽沉积为特征的其它疾病。 本发明的化合物可用于降低Aβ肽形成的药物组合物和治疗方法。
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10.发明授权公开(公告)号：US07309789B2
公开(公告)日：2007-12-18
申请号：US11438725
申请日：2006-05-22
IPC分类号： C07D471/02 , C07D495/02
CPC分类号： C07D491/04 , C07D493/04 , C07D495/04
摘要： Compounds are provided that, by way of their selective neurotransmitter binding useful for the treatment of various neurological and psychological disorders, e.g., ADHD. Such compounds are 4-phenyl substituted tetrahydroisoquinolines having the Formula IA, IB, IIA, IIB, IIIA or IIIC as set forth herein.
摘要翻译： 提供化合物，其通过其可用于治疗各种神经和心理障碍（例如ADHD）的选择性神经递质结合。 这样的化合物是如本文所述的具有式IA，IB，IIA，IIB，IIIA或IIIC的4-苯基取代的四氢异喹啉。
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