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1.发明授权5-�(heteroaryl)alkyl!-3-oxo-pyrido�1,2-a!benzimidazole-4-carboxamide derivatives useful in treating central nervous system disorders 失效5 - [（杂芳基）烷基] -3-氧代 - 吡啶并[1,2-a]苯并咪唑-4-甲酰胺衍生物，用于治疗中枢神经系统疾病
公开(公告)号：US5922731A
公开(公告)日：1999-07-13
申请号：US884804
申请日：1997-06-30
IPC分类号： A61K31/435 , A61P25/00 , C07D471/04 , A61K31/44 , C07D471/00 , C07D498/00 , C07D513/00
CPC分类号： C07D471/04
摘要： A compound of the general formula 1; ##STR1## is disclosed as useful in treating disorders of the central nervous system. Pharmaceutical compositions and methods of treatment are also disclosed.
摘要翻译： 通式1的化合物; 被公开用于治疗中枢神经系统疾病。 还公开了药物组合物和治疗方法。
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2.发明授权S-heteroatom containing alkyl substituted-3-oxo-pyrido�1,2-A!benzimidozole-4-carboxamide derivatives useful in treating central nervous system disorders 失效含有可用于治疗中枢神经系统疾病的烷基取代-3-氧代 - 吡啶并[1,2-A]苯甲亚氨基-4-甲酰胺衍生物的S-杂原子
公开(公告)号：US5817668A
公开(公告)日：1998-10-06
申请号：US943578
申请日：1997-10-03
申请人： Allen B. Reitz , Alfonzo D. Jordan , Pauline J. Sanfilippo , Malcolm K. Scott , Anna Vavouyios-Smith
发明人： Allen B. Reitz , Alfonzo D. Jordan , Pauline J. Sanfilippo , Malcolm K. Scott , Anna Vavouyios-Smith
IPC分类号： A61K31/437 , A61K31/496 , A61K31/5377 , A61P25/00 , A61P25/02 , A61P25/22 , A61P25/30 , C07D471/04 , A61K31/435 , A61K31/535
CPC分类号： C07D471/04 , A61K31/437
摘要： A compound of the general formula 1; ##STR1## is disclosed as useful in treating disorders of the central nervous system. Pharmaceutical compositions and methods of treatment are also disclosed.
摘要翻译： 通式1的化合物; 公开了一种治疗中枢神经系统疾病的方法。 还公开了药物组合物和治疗方法。
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3.发明授权2-amino-quinazoline derivatives useful as inhibitors of β-secretase (BACE) 有权可用作β-分泌酶抑制剂的2-氨基 - 喹唑啉衍生物（BACE）公开(公告)号：US08383637B2
公开(公告)日：2013-02-26
申请号：US11197669
申请日：2005-08-04
申请人： Ellen Baxter , Francois Paul Bischoff , Robert E. Boyd , Mirielle Braeken , Steve Coats , Yifang Huang , Alfonzo D. Jordan , Chi Luo , Marc Hubert Mercken , Serge Maria Aloysius Pieters , Allen B. Reitz , Charles H. Reynolds , Tina Morgan Ross , Brett A. Tounge , Mark J. Schulz , Hans Louis Jos De Winter
发明人： Ellen Baxter , Francois Paul Bischoff , Robert E. Boyd , Mirielle Braeken , Steve Coats , Yifang Huang , Alfonzo D. Jordan , Chi Luo , Marc Hubert Mercken , Serge Maria Aloysius Pieters , Allen B. Reitz , Charles H. Reynolds , Tina Morgan Ross , Brett A. Tounge , Mark J. Schulz , Hans Louis Jos De Winter
IPC分类号： A61K31/517 , C07D239/88 , C07D239/94 , C07D401/06 , A61K31/535 , C07D265/30
CPC分类号： C07D413/06 , C07D239/84 , C07D401/06 , C07D403/06 , C07D403/12 , C07D405/06
摘要： The present invention is directed to novel 2-amino-3,4-dihydro-quinazoline derivatives, pharmaceutical compositions containing them and their use in the treatment of Alzheimer's disease (AD) and related disorders. The compounds of the invention are inhibitors of β-secretase, also known as β-site cleaving enzyme and BACE.
摘要翻译： 本发明涉及新的2-氨基-3,4-二氢 - 喹唑啉衍生物，含有它们的药物组合物及其在治疗阿尔茨海默病（AD）和相关病症中的用途。 本发明的化合物是分泌酶的抑制剂，也称为“切割酶”和BACE。
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4.发明授权Neurotrophic pyrrolidines and piperidines, and related compositions and methods 有权神经营养吡咯烷和哌啶，以及相关组合物和方法公开(公告)号：US06809107B1
公开(公告)日：2004-10-26
申请号：US09593852
申请日：2000-06-14
IPC分类号： A61K3147
CPC分类号： C07D413/14 , C07D413/04 , C07D417/14
摘要： This invention provides compounds having the following general structures: This invention also provides pharmaceutical compositions comprising same and methods of using these compositions to treat and prevent disorders characterized by neuronal damage.
摘要翻译： 本发明提供具有以下一般结构的化合物：本发明还提供包含其的药物组合物和使用这些组合物治疗和预防以神经元损伤为特征的疾病的方法。
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公开(公告)号：US08426429B2
公开(公告)日：2013-04-23
申请号：US11197608
申请日：2005-08-04
申请人： Ellen Baxter , Robert Boyd , Steven J. Coats , Alfonzo D. Jordan , Allen B. Reitz , Charles H. Reynolds , Mark Schulz , Malcolm Scott
发明人： Ellen Baxter , Robert Boyd , Steven J. Coats , Alfonzo D. Jordan , Allen B. Reitz , Charles H. Reynolds , Mark Schulz , Malcolm Scott
IPC分类号： A61K31/517 , C07D239/88 , C07D239/94 , C07D401/06 , A61K31/535 , C07D265/30
CPC分类号： C07D215/227 , C07D401/06 , C07D403/06 , C07D403/12 , C07D405/06 , C07D413/06
摘要： The present invention is directed to novel 2-amino-3,4-dihydro-quinazoline derivatives, pharmaceutical compositions containing them and their use in the treatment of Alzheimer's disease (AD) and related disorders. The compounds of the invention are inhibitors of β-secretase, also known as β-site cleaving enzyme and BACE.
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6.发明授权公开(公告)号：US07319107B2
公开(公告)日：2008-01-15
申请号：US10287096
申请日：2002-11-04
申请人： Magdalena Eisinger , Louis J. Fitzpatrick , Daniel H. Lee , Kevin Pan , Carlos Plata-Salaman , Allen B. Reitz , Virginia L. Smith-Swintosky , Boyu Zhao
发明人： Magdalena Eisinger , Louis J. Fitzpatrick , Daniel H. Lee , Kevin Pan , Carlos Plata-Salaman , Allen B. Reitz , Virginia L. Smith-Swintosky , Boyu Zhao
IPC分类号： A61K31/433 , C07D285/08
CPC分类号： C07D285/08 , A61K8/49 , A61Q5/006 , A61Q19/00 , A61Q19/007 , C07D333/16 , C07D417/12 , C07F9/4018
摘要： The present invention is directed to novel 1,2,4-thiadiazol-2-ium derivatives useful as agonists or antagonists of the melanocortin receptor. More particularly, the compounds of the present invention are useful for the treatment of metabolic, CNS and dermatological disorders such as obesity, impaired oral glucose tolerance, elevated blood glucose levels, type II diabetes, Syndrome X, diabetic retinopathy, spinal cord injury, nerve injury, acute neurodegenerative disorders, chronic neurodegenerative disorders, plexopathies, male erectile dysfunction, dry eyes, acne, dry skin, aged skin, seborrheic dermatitis, rosacea, excessive ear wax, meibomian gland disorder, pseudofolliculitis, yeast infections, dandruff, hidradenitis suppurativa, ocular rosacea and eccrine gland disorder.
摘要翻译： 本发明涉及可用作黑皮质素受体的激动剂或拮抗剂的新颖的1,2,4-噻二唑-2-基衍生物。 更具体地，本发明的化合物可用于治疗代谢，CNS和皮肤病学障碍，例如肥胖症，口服葡萄糖耐量降低，血糖水平升高，II型糖尿病，X综合征，糖尿病性视网膜病变，脊髓损伤，神经 伤口，急性神经退行性疾病，慢性神经退行性疾病，性欲症，男性勃起功能障碍，干眼症，痤疮，干性皮肤，老年皮肤，脂溢性皮炎，酒渣鼻，过度耳垢，睑板腺疾病，假性结石炎，酵母菌感染，头皮屑， 眼红斑痤疮和外分泌腺疾病。
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7.发明授权公开(公告)号：US07049331B2
公开(公告)日：2006-05-23
申请号：US10287095
申请日：2002-11-04
申请人： Magdalena Eisinger , Louis J. Fitzpatrick , Daniel H. Lee , Kevin Pan , Carlos Plata-Salaman , Allen B. Reitz , Virginia L. Smith-Swintosky , Boyu Zhao
发明人： Magdalena Eisinger , Louis J. Fitzpatrick , Daniel H. Lee , Kevin Pan , Carlos Plata-Salaman , Allen B. Reitz , Virginia L. Smith-Swintosky , Boyu Zhao
IPC分类号： A61K31/433 , C07D285/08
CPC分类号： C07D285/08 , A61K8/49 , A61Q5/006 , A61Q19/00 , A61Q19/007 , C07D417/12
摘要： The present invention is directed to novel 1,2,4-thiadiazole derivatives useful as agonists or antagonists of the melanocortin receptor. More particularly, the compounds of the present invention are useful for the treatment of metabolic, CNS and dermatological disorders such as obesity, impaired oral glucose tolerance, elevated blood glucose levels, type II diabetes, Syndrome X, diabetic retinopathy, spinal cord injury, nerve injury, acute neurodegenerative disorders, chronic neurodegenerative disorders, plexopathies, male erectile dysfunction, dry eyes, acne, dry skin, aged skin, seborrheic dermatitis, rosacea, excessive ear wax, meibomian gland disorder, pseudofolliculitis, yeast infections, dandruff, hidradenitis suppurativa, ocular rosacea and eccrine gland disorder.
摘要翻译： 本发明涉及可用作黑皮质素受体的激动剂或拮抗剂的新颖的1,2,4-噻二唑衍生物。 更具体地，本发明的化合物可用于治疗代谢，CNS和皮肤病学障碍，例如肥胖症，口服葡萄糖耐量降低，血糖水平升高，II型糖尿病，X综合征，糖尿病性视网膜病变，脊髓损伤，神经 伤口，急性神经退行性疾病，慢性神经退行性疾病，性欲症，男性勃起功能障碍，干眼症，痤疮，干性皮肤，老年皮肤，脂溢性皮炎，酒渣鼻，过度耳垢，睑板腺疾病，假性结石炎，酵母菌感染，头皮屑， 眼红斑痤疮和外分泌腺疾病。
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8.发明授权公开(公告)号：US08501791B2
公开(公告)日：2013-08-06
申请号：US12835220
申请日：2010-07-13
申请人： Magdalena Eisinger , Louis J. Fitzpatrick , Daniel H. Lee , Kevin Pan , Carlos Plata-Salaman , Allen B. Reitz , Virginia L. Smith-Swintosky , Boyu Zhao
发明人： Magdalena Eisinger , Louis J. Fitzpatrick , Daniel H. Lee , Kevin Pan , Carlos Plata-Salaman , Allen B. Reitz , Virginia L. Smith-Swintosky , Boyu Zhao
IPC分类号： A61K31/433 , C07D285/08
CPC分类号： C07D285/08 , A61K8/49 , A61Q5/006 , A61Q19/00 , A61Q19/007 , C07D333/16 , C07D417/12 , C07F9/4018
摘要： The present invention is directed to novel 1,2,4-thiadiazol-2-ium derivatives useful as agonists or antagonists of the melanocortin receptor. More particularly, the compounds of the present invention are useful for the treatment of metabolic, CNS and dermatological disorders such as obesity, impaired oral glucose tolerance, elevated blood glucose levels, type II diabetes, Syndrome X, diabetic retinopathy, spinal cord injury, nerve injury, acute neurodegenerative disorders, chronic neurodegenerative disorders, plexopathies, male erectile dysfunction, dry eyes, acne, dry skin, aged skin, seborrheic dermatitis, rosacea, excessive ear wax, meibomian gland disorder, pseudofolliculitis, yeast infections, dandruff, hidradenitis suppurativa, ocular rosacea and eccrine gland disorder.
摘要翻译： 本发明涉及可用作黑皮质素受体的激动剂或拮抗剂的新颖的1,2,4-噻二唑-2-基衍生物。 更具体地，本发明的化合物可用于治疗代谢，CNS和皮肤病学障碍，例如肥胖症，口服葡萄糖耐量降低，血糖水平升高，II型糖尿病，X综合征，糖尿病性视网膜病变，脊髓损伤，神经 伤口，急性神经退行性疾病，慢性神经退行性疾病，性欲症，男性勃起功能障碍，干眼症，痤疮，干性皮肤，老年皮肤，脂溢性皮炎，酒渣鼻，过度耳垢，睑板腺疾病，假性结石炎，酵母菌感染，头皮屑， 眼红斑痤疮和外分泌腺疾病。
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9.发明申请0NOVEL, 1,2,4-THIADIAZOLIUM DERIVATIVES AS MELANOCORTIN RECEPTOR MODULATORS 失效0号，1,2,4-噻二唑衍生物作为米考康宁受体调节剂公开(公告)号：US20100280079A1
公开(公告)日：2010-11-04
申请号：US12835220
申请日：2010-07-13
申请人： Magdalena Eisinger , Louis J. Fitzpatrick , Daniel H. Lee , Kevin Pan , Carlos Plata-Salaman , Allen B. Reitz , Virginia L. Smith-Swintosky , Boyu Zhao
发明人： Magdalena Eisinger , Louis J. Fitzpatrick , Daniel H. Lee , Kevin Pan , Carlos Plata-Salaman , Allen B. Reitz , Virginia L. Smith-Swintosky , Boyu Zhao
IPC分类号： A61K31/433 , A61K31/4439 , A61P25/00 , A61P17/00 , A61P3/00 , A61P15/00
CPC分类号： C07D285/08 , A61K8/49 , A61Q5/006 , A61Q19/00 , A61Q19/007 , C07D333/16 , C07D417/12 , C07F9/4018
摘要： The present invention is directed to novel 1,2,4-thiadiazol-2-ium derivatives useful as agonists or antagonists of the melanocortin receptor. More particularly, the compounds of the present invention are useful for the treatment of metabolic, CNS and dermatological disorders such as obesity, impaired oral glucose tolerance, elevated blood glucose levels, type II diabetes, Syndrome X, diabetic retinopathy, spinal cord injury, nerve injury, acute neurodegenerative disorders, chronic neurodegenerative disorders, plexopathies, male erectile dysfunction, dry eyes, acne, dry skin, aged skin, seborrheic dermatitis, rosacea, excessive ear wax, meibomian gland disorder, pseudofolliculitis, yeast infections, dandruff, hidradenitis suppurativa, ocular rosacea and eccrine gland disorder.
摘要翻译： 本发明涉及可用作黑皮质素受体的激动剂或拮抗剂的新颖的1,2,4-噻二唑-2-基衍生物。 更具体地，本发明的化合物可用于治疗代谢，CNS和皮肤病学障碍，例如肥胖症，口服葡萄糖耐量降低，血糖水平升高，II型糖尿病，X综合征，糖尿病性视网膜病变，脊髓损伤，神经 伤口，急性神经退行性疾病，慢性神经退行性疾病，性欲症，男性勃起功能障碍，干眼症，痤疮，干性皮肤，老年皮肤，脂溢性皮炎，酒渣鼻，过度耳垢，睑板腺疾病，假性结石炎，酵母菌感染，头皮屑， 眼红斑痤疮和外分泌腺疾病。
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10.发明授权公开(公告)号：US07786311B2
公开(公告)日：2010-08-31
申请号：US12221900
申请日：2008-08-05
申请人： Magdalena Eisinger , Louis J. Fitzpatrick , Daniel H. Lee , Kevin Pan , Carlos Plata-Salaman , Allen B. Reitz , Virginia L. Smith-Swintosky , Boyu Zhao
发明人： Magdalena Eisinger , Louis J. Fitzpatrick , Daniel H. Lee , Kevin Pan , Carlos Plata-Salaman , Allen B. Reitz , Virginia L. Smith-Swintosky , Boyu Zhao
IPC分类号： C07D285/08
CPC分类号： C07D285/08 , A61K8/49 , A61Q5/006 , A61Q19/00 , A61Q19/007 , C07D333/16 , C07D417/12 , C07F9/4018
摘要： The present invention is directed to novel 1,2,4-thiadiazol-2-ium derivatives useful as agonists or antagonists of the melanocortin receptor. More particularly, the compounds of the present invention are useful for the treatment of metabolic, CNS and dermatological disorders such as obesity, impaired oral glucose tolerance, elevated blood glucose levels, type II diabetes, Syndrome X, diabetic retinopathy, spinal cord injury, nerve injury, acute neurodegenerative disorders, chronic neurodegenerative disorders, plexopathies, male erectile dysfunction, dry eyes, acne, dry skin, aged skin, seborrheic dermatitis, rosacea, excessive ear wax, meibomian gland disorder, pseudofolliculitis, yeast infections, dandruff, hidradenitis suppurativa, ocular rosacea and eccrine gland disorder.
摘要翻译： 本发明涉及可用作黑皮质素受体的激动剂或拮抗剂的新颖的1,2,4-噻二唑-2-基衍生物。 更具体地，本发明的化合物可用于治疗代谢，CNS和皮肤病学障碍，例如肥胖症，口服葡萄糖耐量降低，血糖水平升高，II型糖尿病，X综合征，糖尿病性视网膜病变，脊髓损伤，神经 伤口，急性神经退行性疾病，慢性神经退行性疾病，性欲症，男性勃起功能障碍，干眼症，痤疮，干性皮肤，老年皮肤，脂溢性皮炎，酒渣鼻，过度耳垢，睑板腺疾病，假性结石炎，酵母菌感染，头皮屑， 眼红斑痤疮和外分泌腺疾病。
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