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1. 发明授权

US07776882B2 2-amino-3,4-dihydro-quinoline derivatives useful as inhibitors of β-secretase (BACE) 有权
标题翻译：可用作β-分泌酶抑制剂（BACE）的2-氨基-3,4-二氢 - 喹啉衍生物
公开(公告)号：US07776882B2
公开(公告)日：2010-08-17
申请号：US11671703
申请日：2007-02-06
申请人： Ellen W. Baxter , Allen B. Reitz , Christopher John Creighton
发明人： Ellen W. Baxter , Allen B. Reitz , Christopher John Creighton
IPC分类号： A61K31/44 , A61P25/28 , C07D215/38
CPC分类号： C07D413/14 , C07D215/38 , C07D403/12 , C07D405/06 , C07D405/14
摘要： The present invention is directed to 2-amino-3,4-dihydro-quinoline 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, BACE1, Asp2 and memapsin2.
摘要翻译：本发明涉及2-氨基-3,4-二氢喹啉衍生物，含有它们的药物组合物及其在治疗阿尔茨海默病（AD）和相关疾病中的用途。本发明的化合物是分泌酶抑制剂，也被称为“切割酶”和BACE，BACE1，Asp2和memapsin2。

2. 发明申请

US20080221116A1 ISOXAZOLINE ALPHA 1a/1d ADRENORECEPTOR ANTAGONISTS 审中-公开
标题翻译： ISOXAZOLINE ALPHA 1a / 1d ADRENORECEPTOR ANTAGONISTS
公开(公告)号：US20080221116A1
公开(公告)日：2008-09-11
申请号：US11855757
申请日：2007-09-14
申请人： Ellen W. Baxter , Samuel O. Nortey , Allen B. Reitz
发明人： Ellen W. Baxter , Samuel O. Nortey , Allen B. Reitz
IPC分类号： A61K31/496 , C07D413/14
CPC分类号： C07D413/14
摘要： The present invention relates to isoxazolines useful as selective α1a/α1d adrenoreceptor antagonists for the treatment of benign prostatic hypertrophy and/or lower urinary tract symptoms as well as to pharmaceutical compositions comprising said compounds, processes to prepare these compounds, and the use of these compounds as α1a/α1d adrenoreceptor modulators in a method of treatment.
摘要翻译：本发明涉及可用作治疗良性前列腺肥大和/或下尿路症状的选择性α1A/α1D1肾上腺素受体拮抗剂的异恶唑，以及药物组合物包括所述化合物，制备这些化合物的方法，以及这些化合物在治疗方法中作为α1A/α1D1肾上腺素受体调节剂的用途。

3. 发明授权

US06887876B2 Benzamidine derivatives 有权
标题翻译：苄脒衍生物
公开(公告)号：US06887876B2
公开(公告)日：2005-05-03
申请号：US10014081
申请日：2001-12-11
申请人： Ellen W. Baxter , Samuel O. Nortey , Allen B. Reitz
发明人： Ellen W. Baxter , Samuel O. Nortey , Allen B. Reitz
IPC分类号： A61K31/381 , A61K31/495 , A61K45/06 , C07D295/195 , C07D333/20 , A61K31/496 , C07D295/125 , C07D409/12
CPC分类号： C07D295/195 , A61K31/381 , A61K31/495 , A61K45/06 , C07D333/20 , A61K2300/00
摘要： Benzamidine derivatives are useful delta-opioid receptor modulators, agonists useful as analgesics and antagonists useful as immunosuppressants, antiinflammatory agents, agents for the treatment of neurological and psychiatric conditions, medicaments for drug and alcohol abuse, agents for treating gastritis and diarrhea, cardiovascular agents and agents for the treatment of respiratory diseases.
摘要翻译：苄脒衍生物是有用的δ-阿片受体调节剂，可用作止痛剂的激动剂和可用作免疫抑制剂的拮抗剂，抗炎剂，用于治疗神经和精神病症的药剂，用于药物和酒精滥用的药物，用于治疗胃炎和腹泻的药剂，心血管药剂和用于治疗呼吸系统疾病的药剂。

4. 发明授权

US06313309B1 4-thionaphthyl—1H—imidazoles which are useful&agr;22-adrenoceptoR agonists/ antagonists 失效
标题翻译：可用于α2-肾上腺素受体激动剂/拮抗剂的4-硫萘基-1H-咪唑
公开(公告)号：US06313309B1
公开(公告)日：2001-11-06
申请号：US09286395
申请日：1999-04-05
申请人： Ellen W. Baxter , Robert E. Boyd , Michelle C. Jetter , Mark McDonnell , Allen B. Reitz , Tina Morgan Ross
发明人： Ellen W. Baxter , Robert E. Boyd , Michelle C. Jetter , Mark McDonnell , Allen B. Reitz , Tina Morgan Ross
IPC分类号： C07O23354
CPC分类号： C07D409/04
摘要： 4-thionaphthyl-1H-imidazoles are &agr;2-adrenoceptor agonists/antagonists. As delta-opioid receptor agonists, such compounds are useful as analgesics. Depending on their agonist/antagonist effect, such compounds may also be useful agents to treat hypertension, glaucoma, sexual dysfunction, depression, attention deficit hyperactivity disorder, the need for anesthesia or cardiac arrythmia.
摘要翻译： 4-硫萘基-1H-咪唑是α2-肾上腺素受体激动剂/拮抗剂。作为δ-阿片受体激动剂，这些化合物可用作镇痛药。根据其激动剂/拮抗剂的作用，这些化合物也可用于治疗高血压，青光眼，性功能障碍，抑郁症，注意缺陷多动障碍，麻醉或心律失常的需要。

5. 发明授权

US5332743A Benzyl and benzhydryl alcohols 失效
标题翻译：苄基和二苯甲醇
公开(公告)号：US5332743A
公开(公告)日：1994-07-26
申请号：US897487
申请日：1992-06-12
申请人： Ellen W. Baxter , Allen B. Reitz
发明人： Ellen W. Baxter , Allen B. Reitz
IPC分类号： A61K31/445 , A61K31/451 , A61K31/495 , A61P25/18 , C07D211/14 , C07D211/18 , C07D211/22 , C07D211/26 , C07D211/34 , C07D295/08 , C07D295/096 , C07D295/112 , C07D211/12
CPC分类号： C07D295/096 , C07D295/112
摘要： Compounds of the general formula I: ##STR1## are disclosed as potent antipsychotic agents. Novel methods of use and intermediates used to make the compounds of formula I are also disclosed.
摘要翻译：通式I的化合物：作为有效的抗精神病药被公开。还公开了用于制备式I化合物的新型使用方法和中间体。

6. 发明授权

US07932261B2 Macrocycle derivatives useful as inhibitors of β-secretase (BACE) 有权
标题翻译：可用作分泌抑制剂（BACE）的大分子衍生物
公开(公告)号：US07932261B2
公开(公告)日：2011-04-26
申请号：US11671732
申请日：2007-02-06
申请人： Ellen W. Baxter , François P. Bischoff , Hans De Winter , Chih Yung Ho , Yifang Huang , Michael H. Parker , Allen B. Reitz , Charles H. Reynolds , Eric D. Strobel
发明人： Ellen W. Baxter , François P. Bischoff , Hans De Winter , Chih Yung Ho , Yifang Huang , Michael H. Parker , Allen B. Reitz , Charles H. Reynolds , Eric D. Strobel
IPC分类号： C07D487/04 , A61K31/517
CPC分类号： C07D498/08 , C07D487/08
摘要： The present invention is directed to macrocycle 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, BACE1, Asp2 and memapsin2.
摘要翻译：本发明涉及大环衍生物，含有它们的药物组合物及其在治疗阿尔茨海默病（AD）和相关疾病中的用途。本发明的化合物是分泌酶抑制剂，也被称为“切割酶”和BACE，BACE1，Asp2和memapsin2。

7. 发明授权

US07576105B2 Benzyl substituted (piperidin-4-yl)aminobenzamido derivatives 有权
标题翻译：苄基取代的（哌啶-4-基）氨基苯甲酰氨基衍生物
公开(公告)号：US07576105B2
公开(公告)日：2009-08-18
申请号：US11314496
申请日：2005-12-21
申请人： Ellen W. Baxter , Allen B. Reitz
发明人： Ellen W. Baxter , Allen B. Reitz
IPC分类号： A61K31/445 , C07D211/56
CPC分类号： C07D401/12 , C07D211/56 , C07D211/58
摘要： The present invention is directed to N-benzyl substituted (piperidin-4-yl)aminobenzamido derivatives which are delta-opioid receptor modulators.
摘要翻译：本发明涉及作为δ-阿片受体调节剂的N-苄基取代的（哌啶-4-基）氨基苯甲酰氨基衍生物。

8. 发明授权

US06201025B1 N-aralkylaminotetralins as ligands for the neuropeptide Y Y5 receptor 有权
标题翻译： N-芳烷基氨基螺环素作为神经肽Y Y5受体的配体
公开(公告)号：US06201025B1
公开(公告)日：2001-03-13
申请号：US09413292
申请日：1999-10-06
申请人： Scott L. Dax , Timothy W. Lovenberg , Ellen W. Baxter , John R. Carson , Donald W. Ludovici , Mark A. Youngman
发明人： Scott L. Dax , Timothy W. Lovenberg , Ellen W. Baxter , John R. Carson , Donald W. Ludovici , Mark A. Youngman
IPC分类号： A61K31135
CPC分类号： C07C217/74 , C07B2200/07 , C07C217/58 , C07C2602/10 , C07D209/16 , C07D213/38
摘要： &bgr;-Aminotetralin derivatives of the formula: which are ligands for the neuropeptide Y Y5 (NPY5) receptor, methods of preparation and pharmaceutical compositions containing a &bgr;-aminotetralin derivative as the active ingredient are described. The 62 -aminotetralins are useful in the treatment of disorders and diseases associated with NPY receptor subtype Y5.
摘要翻译：描述了作为神经肽Y Y5（NPY5）受体的配体的制备方法和含有β-氨基四氢卟吩衍生物作为活性成分的药物组合物的下式的β-氨基四氢萘衍生物。 62-氨基四氢叶酸可用于治疗与NPY受体亚型Y5相关的疾病和疾病。

9. 发明授权

US06426356B1 Imidazoethyl thiophenes 有权
标题翻译：咪唑乙基噻吩
公开(公告)号：US06426356B1
公开(公告)日：2002-07-30
申请号：US09440869
申请日：1999-11-16
申请人： Ellen W. Baxter , Michele C. Jetter
发明人： Ellen W. Baxter , Michele C. Jetter
IPC分类号： C07D40906
CPC分类号： C07D409/06 , A61K31/4178 , A61K31/427 , C07D417/06
摘要： Certain imidazoethyl thiophenes/thiazoles and benzothiophenes of the formula: where Z is CH or N; and X is independently selected from the group consisting of hydrogen, C1-4alkyl, bromine, chlorine, iodide, trifluoromethyl, C4-1alkoxy and nitro; are &agr;2-adrenoceptor agonists/antagonists which are useful in the treatment of hypertension, glaucoma, sexual dysfunction, depression, attention deficit hyperactivity disorder, the need for anesthesia, cardiac arrythmia or the need for analgesia.
摘要翻译：某些咪唑乙基噻吩/噻唑和苯并噻吩类化合物，其中Z是CH或N; 和X独立地选自氢，C 1-4烷基，溴，氯，碘，三氟甲基，C 1-4烷氧基和硝基; 是可用于治疗高血压，青光眼，性功能障碍，抑郁症，注意力缺陷多动障碍，麻醉需要，心脏心律失常或需要镇痛的α2-肾上腺素受体激动剂/拮抗剂。

10. 发明授权

US06465486B1 Pyridyl/quinolinyl imidazoles 有权
标题翻译：吡啶基/喹啉基咪唑
公开(公告)号：US06465486B1
公开(公告)日：2002-10-15
申请号：US09524451
申请日：2000-03-10
申请人： Ellen W. Baxter , Robert E. Boyd , John R. Carson , Michele C. Jetter , Allen B. Reitz
发明人： Ellen W. Baxter , Robert E. Boyd , John R. Carson , Michele C. Jetter , Allen B. Reitz
IPC分类号： A61K3147
CPC分类号： C07D401/06 , A61K31/47
摘要： Certain imidazo pyridines/quinolines of the formula: where n is 0, 1, 2; X is independently selected from the group consisting of C1-4alkyl, bromine, chlorine, iodide, trifluoromethyl, C1-4alkoxy, —SO2NH2, nitro, and two adjacent X may be fused to form the moiety: whereby a saturated, partially unsaturated or aromatic six-membered fused ring is formed; Y is independently selected from the group consisting of hydrogen, hydroxy, C1-4alkyl, C1-4alkoxy, trifluoromethyl and phenyl; and Z is independently selected from the group consisting of hydroxy, C1-4alkyl, bromine, chlorine, iodide, trifluoromethyl, C1-4alkoxy, —SO2NH2 and nitro; are &agr;2-adrenoceptor modulators which are useful in the treatment of hypertension, glaucoma, sexual dysfunction, depression, attention deficit hyperactivity disorder, Parkinsonism, the need for anesthesia, cardiac arrythmia or the need for analgesia.
摘要翻译：某些具有下式的咪唑并吡啶/喹啉：其中n是0,1,2; X独立地选自C 1-4烷基，溴，氯，碘，三氟甲基，C 1-4烷氧基，-SO 2 NH 2，硝基和两个相邻 X可以稠合形成部分：由此形成饱和的，部分不饱和的或芳族的六元稠环; Y独立地选自氢，羟基，C 1-4烷基，C 1-4烷氧基，三氟甲基和苯基; 和Z独立地选自羟基，C 1-4烷基，溴，氯，碘，三氟甲基，C 1-4烷氧基，-SO 2 NH 2和硝基;是可用于治疗高血压，青光眼，性功能障碍的α2-肾上腺素能受体调节剂，抑郁症，注意力缺陷多动障碍，帕金森综合征，麻醉需要，心脏心律失常或需要镇痛。

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