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公开(公告)号:US07595339B2
公开(公告)日:2009-09-29
申请号:US11840417
申请日:2007-08-17
申请人: Jennifer Rebecca Allen , Albert Kudzovi Amegadzie , Kevin Matthew Gardinier , George Stuart Gregory , Stephen Andrew Hitchcock , Paul J. Hoogestraat , Winton Dennis Jones, Jr. , Daryl Lynn Smith
发明人: Jennifer Rebecca Allen , Albert Kudzovi Amegadzie , Kevin Matthew Gardinier , George Stuart Gregory , Stephen Andrew Hitchcock , Paul J. Hoogestraat , Winton Dennis Jones, Jr. , Daryl Lynn Smith
IPC分类号: A61K31/40
CPC分类号: C07D209/10 , C07D209/08 , C07D209/12 , C07D209/14 , C07D209/40 , C07D209/42 , C07D209/96 , C07D231/56 , C07D401/04 , C07D401/12 , C07D403/04 , C07D403/12 , C07D405/04 , C07D405/06 , C07D405/12 , C07D409/04 , C07D417/04 , C07D471/04 , C07D471/10 , C07D491/10
摘要: Novel compounds of structural formula (I) are disclosed. As modulators of the Cannabinoid-1 (CB1) receptor, these compounds are useful in the treatment, prevention and suppression of diseases mediated by the CB1 receptor. As such, compounds of the present invention are useful as in the treatment, prevention and suppression of psychosis, memory deficits, cognitive disorders, migraine, neuropathy, neuro-inflammatory disorders (e.g., multiple sclerosis, Guillain-Barre syndrome and the inflammatory sequelae of viral encephalitis), cerebral vascular accidents, head trauma, anxiety disorders, stress, epilepsy, Parkinson's disease, and schizophrenia. The compounds are also useful for the treatment of substance abuse disorders, particularly to opiates, alcohol, and nicotine. The compounds are also useful for the treatment of obesity or eating disorders associated with excessive food intake and complications associated therewith.
摘要翻译: 公开了结构式(I)的新型化合物。 作为大麻素-1(CB1)受体的调节剂,这些化合物可用于治疗,预防和抑制由CB1受体介导的疾病。 因此,本发明的化合物可用于治疗,预防和抑制精神病,记忆缺陷,认知障碍,偏头痛,神经病,神经炎症性疾病(例如,多发性硬化症,吉兰巴利综合症和炎性后遗症 病毒性脑炎),脑血管意外,头部创伤,焦虑症,压力,癫痫,帕金森病和精神分裂症。 这些化合物也可用于治疗药物滥用障碍,特别是鸦片剂,酒精和尼古丁。 所述化合物还可用于治疗与过量食物摄入和与其相关的并发症相关的肥胖或进食障碍。
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公开(公告)号:US06939946B2
公开(公告)日:2005-09-06
申请号:US10676575
申请日:2003-09-30
申请人: Peter Stanley Borromeo , Jeffrey Daniel Cohen , George Stuart Gregory , Stacy Kay Henle , Stephen Andrew Hitchcock , Louis Nickolaus Jungheim , Daniel Ray Mayhugh , Timothy Alan Shepherd , William Wilson Turner, Jr.
发明人: Peter Stanley Borromeo , Jeffrey Daniel Cohen , George Stuart Gregory , Stacy Kay Henle , Stephen Andrew Hitchcock , Louis Nickolaus Jungheim , Daniel Ray Mayhugh , Timothy Alan Shepherd , William Wilson Turner, Jr.
IPC分类号: A61K9/08 , A61K9/72 , A61K38/00 , A61P31/10 , A61P33/00 , C07K1/06 , C07K7/50 , C07K7/54 , C07K7/56 , C07K7/64
CPC分类号: C07K7/50 , A61K38/00 , C07K7/56 , Y02A50/409
摘要: A method for modifying the cyclic peptide ring system of Echinocandin-type compounds to produce new analogs having antifungal activity is provided. The inventive process comprises opening the cyclic peptide ring, cleaving the terminal ornithine unit, inserting at least one new amino acid or other synthetic unit and closing the ring to produce a new cyclic peptide ring structure. The process allows one to incorporate features such as water-solubility into the cyclic peptide ring nucleus, sites for further modification, increase or decrease the number of amino acid or peptide units within the ring nucleus, and increase or decrease the total number of members within the ring. The invention further provides novel Echinocandin type compounds and their use as antifungal or anti-parasitic agents.
摘要翻译: 提供了一种用于改变棘球in素型化合物的环肽环体系以产生具有抗真菌活性的新类似物的方法。 本发明的方法包括打开环肽环,切割末端鸟氨酸单元,插入至少一个新的氨基酸或其它合成单元并封闭环以产生新的环肽环结构。 该方法允许将诸如水溶性的特征结合到环肽环核中,用于进一步修饰的位点,增加或减少环核内的氨基酸或肽单元的数目,并且增加或减少环核内的成员总数 戒指。 本发明还提供新颖的棘白菌素类化合物及其作为抗真菌剂或抗寄生虫剂的用途。
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公开(公告)号:US06653281B1
公开(公告)日:2003-11-25
申请号:US09763114
申请日:2001-05-24
申请人: Peter Stanley Borromeo , Jeffrey Daniel Cohen , George Stuart Gregory , Stacy Kay Henle , Stephen Andrew Hitchcock , Louis Nickolaus Jungheim , Daniel Ray Mayhugh , Timothy Alan Shepherd , William Wilson Turner, Jr.
发明人: Peter Stanley Borromeo , Jeffrey Daniel Cohen , George Stuart Gregory , Stacy Kay Henle , Stephen Andrew Hitchcock , Louis Nickolaus Jungheim , Daniel Ray Mayhugh , Timothy Alan Shepherd , William Wilson Turner, Jr.
IPC分类号: A61K3812
CPC分类号: C07K7/50 , A61K38/00 , C07K7/56 , Y02A50/409
摘要: A method for modifying the cyclic peptide ring system of Echinocandin-type compounds to produce new analogs having antifungal activity is provided. The inventive process comprises opening the cyclic peptide ring, cleaving the terminal omithine unit, inserting at least one new amino acid or other synthetic unit and closing the ring to produce a new cyclic peptide ring structure. The process allows one to incorporate features such as water-solubility into the cyclic peptide ring nucleus, sites for further modification, increase or decrease the number of amino acid or peptide units within the ring nucleus, and increase or decrease the total number of members within the ring. The invention further provides novel Echinocandin type compounds and their use as antifungal or anti-parasitic agents.
摘要翻译: 提供了一种用于改变棘球in素型化合物的环肽环体系以产生具有抗真菌活性的新类似物的方法。 本发明的方法包括打开环肽环,切割末端氨基甲酸单元,插入至少一个新的氨基酸或其它合成单元并闭合环以产生新的环肽环结构。 该方法允许将诸如水溶性的特征结合到环肽环核中,用于进一步修饰的位点,增加或减少环核内的氨基酸或肽单元的数目,并且增加或减少环核内的成员总数 戒指。 本发明还提供新颖的棘白菌素类化合物及其作为抗真菌剂或抗寄生虫剂的用途。
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公开(公告)号:US07378447B2
公开(公告)日:2008-05-27
申请号:US10546906
申请日:2004-03-12
IPC分类号: A01N37/18 , A01N31/165
CPC分类号: C07C323/41 , C07B2200/07 , C07C257/14 , C07C257/18 , C07C271/24 , C07C2601/02 , C07C2602/08 , C07D213/64 , C07D213/70 , C07D295/125 , C07D295/13
摘要: The present invention relates to compounds of Formula (I): which are agonists of the M-1 muscarinic receptor
摘要翻译: 本发明涉及式(I)化合物:它是M-1毒蕈碱受体的激动剂
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公开(公告)号:US07326731B2
公开(公告)日:2008-02-05
申请号:US10488519
申请日:2002-09-09
申请人: Jennifer Rebecca Allen , Stephen Andrew Hitchcock , James Andrew Jamison , Bin Liu , William Wilson Turner, Jr.
发明人: Jennifer Rebecca Allen , Stephen Andrew Hitchcock , James Andrew Jamison , Bin Liu , William Wilson Turner, Jr.
IPC分类号: A61K31/16 , C07C233/00
CPC分类号: C07D207/325 , C07C257/14 , C07C2602/08 , C07D213/54 , C07D213/56 , C07D213/81 , C07D213/82 , C07D213/84 , C07D241/24 , C07D307/52 , C07D317/28 , C07D333/24 , C07D409/04 , Y02P20/582
摘要: The present invention relates to compounds of Formula I: Formula I which are agonists of the M-1 muscarinic receptor.
摘要翻译: 本发明涉及作为M-1毒蕈碱受体的激动剂的式I化合物:式I。
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公开(公告)号:US6069238A
公开(公告)日:2000-05-30
申请号:US342073
申请日:1999-06-28
申请人: Stephen Andrew Hitchcock , Chafiq Hamdouchi , Concepcion Sanchez-Martinez , Almudena Rubio Esteban
发明人: Stephen Andrew Hitchcock , Chafiq Hamdouchi , Concepcion Sanchez-Martinez , Almudena Rubio Esteban
CPC分类号: C07H19/01
摘要: An improved and a new synthetic route for the reparation of spirocyclic C-glycoside compounds having the following general structure are described. ##STR1## Novel derivatives of spirocyclic C-glycoside compounds are also disclosed which may be used as intermediates in the synthesis and evaluation of potential pharmaceutically active materials.
摘要翻译: 描述了用于修复具有以下一般结构的螺环C-糖苷化合物的改进和新的合成途径。 还公开了螺环C-糖苷化合物的新型衍生物,其可用作合成和评估潜在的药学活性物质的中间体。
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公开(公告)号:US20080287504A1
公开(公告)日:2008-11-20
申请号:US11840417
申请日:2007-08-17
申请人: Jennifer Rebecca Allen , Albert Kudzovi Amegadzie , Kevin Matthew Gardinier , George Stuart Gregory , Stephen Andrew Hitchcock , Paul J. Hoogestraat , Winton Dennis Jones, JR. , Daryl Lynn Smith
发明人: Jennifer Rebecca Allen , Albert Kudzovi Amegadzie , Kevin Matthew Gardinier , George Stuart Gregory , Stephen Andrew Hitchcock , Paul J. Hoogestraat , Winton Dennis Jones, JR. , Daryl Lynn Smith
IPC分类号: A61K31/404 , A61K31/4439 , A61P3/04
CPC分类号: C07D209/10 , C07D209/08 , C07D209/12 , C07D209/14 , C07D209/40 , C07D209/42 , C07D209/96 , C07D231/56 , C07D401/04 , C07D401/12 , C07D403/04 , C07D403/12 , C07D405/04 , C07D405/06 , C07D405/12 , C07D409/04 , C07D417/04 , C07D471/04 , C07D471/10 , C07D491/10
摘要: Novel compounds of structural formula (I) are disclosed. As modulators of the Cannabinoid-1 (CB1) receptor, these compounds are useful in the treatment, prevention and suppression of diseases mediated by the CB1 receptor. As such, compounds of the present invention are useful as in the treatment, prevention and suppression of psychosis, memory deficits, cognitive disorders, migraine, neuropathy, neuro-inflammatory disorders (e.g., multiple sclerosis, Guillain-Barre syndrome and the inflammatory sequelae of viral encephalitis), cerebral vascular accidents, head trauma, anxiety disorders, stress, epilepsy, Parkinson's disease, and schizophrenia. The compounds are also useful for the treatment of substance abuse disorders, particularly to opiates, alcohol, and nicotine. The compounds are also useful for the treatment of obesity or eating disorders associated with excessive food intake and complications associated therewith.
摘要翻译: 公开了结构式(I)的新型化合物。 作为大麻素-1(CB1)受体的调节剂,这些化合物可用于治疗,预防和抑制由CB1受体介导的疾病。 因此,本发明的化合物可用于治疗,预防和抑制精神病,记忆缺陷,认知障碍,偏头痛,神经病,神经炎症性疾病(例如,多发性硬化症,吉兰巴利综合症和炎性后遗症 病毒性脑炎),脑血管意外,头部创伤,焦虑症,压力,癫痫,帕金森病和精神分裂症。 这些化合物也可用于治疗药物滥用障碍,特别是鸦片剂,酒精和尼古丁。 所述化合物还可用于治疗与过量食物摄入和与其相关的并发症相关的肥胖或进食障碍。
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公开(公告)号:US07265246B2
公开(公告)日:2007-09-04
申请号:US10560757
申请日:2004-06-23
IPC分类号: C07C233/65 , A61K31/165
CPC分类号: C07D207/27 , C07C233/79 , C07C323/25 , C07C2601/02 , C07C2601/14 , C07C2602/08 , C07D207/09 , C07D211/26 , C07D213/32 , C07D213/38 , C07D213/70 , C07D231/12 , C07D231/38 , C07D233/54 , C07D233/64 , C07D235/14 , C07D263/32 , C07D271/10 , C07D277/28 , C07D307/52 , C07D307/56 , C07D333/20 , C07D333/58
摘要: The present invention relates to compounds of Formula I: I which are agonists of the M-1 muscarinic receptor
摘要翻译: 本发明涉及作为M-1毒蕈碱受体的激动剂的式I化合物
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