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公开(公告)号:US06638930B2
公开(公告)日:2003-10-28
申请号:US09836716
申请日:2001-04-17
申请人: Conrad P. Dorn , Paul E. Finke , Jeffrey J. Hale , Malcolm Maccoss , Sander G. Mills , Shrenik K. Shah , Mark Stuart Chambers , Timothy Harrison , Tamara Ladduwahetty , Brian John Williams
发明人: Conrad P. Dorn , Paul E. Finke , Jeffrey J. Hale , Malcolm Maccoss , Sander G. Mills , Shrenik K. Shah , Mark Stuart Chambers , Timothy Harrison , Tamara Ladduwahetty , Brian John Williams
IPC分类号: A61K315377
CPC分类号: A61K31/41 , A61K31/50 , A61K31/53 , A61K31/535 , A61K31/54 , C07D265/30 , C07D265/32 , C07D279/12 , C07D413/04 , C07D413/06 , C07D413/14 , Y10S514/872
摘要: Substituted heterocycles of the general structural formula: are tachykinin receptor antagonists useful in the treatment of inflammatory diseases, pain or migraine, asthma and emesis, and calcium channel blockers useful in the treatment of cardiovascular conditions such as angina, hypertension or ischemia.
摘要翻译: 取代的通式结构式的杂环是用于治疗炎性疾病,疼痛或偏头痛,哮喘和呕吐的速激肽受体拮抗剂,以及可用于治疗心血管疾病如心绞痛,高血压或缺血的钙通道阻滞剂。
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公开(公告)号:US5872116A
公开(公告)日:1999-02-16
申请号:US959393
申请日:1997-10-28
申请人: Conrad P. Dorn , Paul E. Finke , Jeffrey J. Hale , Malcolm Maccoss , Sander G. Mills , Shrenik K. Shah , Mark Stuart Chambers , Timothy Harrison , Tamara Ladduwahetty , Brian John Williams
发明人: Conrad P. Dorn , Paul E. Finke , Jeffrey J. Hale , Malcolm Maccoss , Sander G. Mills , Shrenik K. Shah , Mark Stuart Chambers , Timothy Harrison , Tamara Ladduwahetty , Brian John Williams
IPC分类号: C07D265/30 , C07D265/32 , C07D279/12 , C07D413/04 , C07D413/06 , C07D413/14 , A61K31/54 , A61K31/50 , A61K31/53 , A61K31/535
CPC分类号: C07D265/30 , C07D265/32 , C07D279/12 , C07D413/04 , C07D413/06 , C07D413/14 , Y10S514/825
摘要: Substituted heterocycles of the general structural formula: ##STR1## are tachykinin receptor antagonists useful in the treatment of inflammatory diseases, pain or migraine, asthma and emesis, and calcium channel blockers useful in the treatment of cardiovascular conditions such as angina, hypertension or ischemia.
摘要翻译: 取代的通式结构式的杂环:
是可用于治疗炎性疾病,疼痛或偏头痛,哮喘和呕吐的速激肽受体拮抗剂,以及可用于治疗心血管疾病如心绞痛,高血压或缺血的钙通道阻滞剂。 -
公开(公告)号:US5719147A
公开(公告)日:1998-02-17
申请号:US525259
申请日:1995-09-08
申请人: Conrad P. Dorn , Paul E. Finke , Jeffrey J. Hale , Malcolm MacCoss , Sander G. Mills , Shrenik K. Shah , Mark Stuart Chambers , Timothy Harrison , Tamara Ladduwahetty , Brian John Williams
发明人: Conrad P. Dorn , Paul E. Finke , Jeffrey J. Hale , Malcolm MacCoss , Sander G. Mills , Shrenik K. Shah , Mark Stuart Chambers , Timothy Harrison , Tamara Ladduwahetty , Brian John Williams
IPC分类号: C07D265/30 , C07D265/32 , C07D279/12 , C07D413/04 , C07D413/06 , C07D413/14 , A61K31/54 , A61K31/535 , C07D417/04
CPC分类号: C07D265/30 , C07D265/32 , C07D279/12 , C07D413/04 , C07D413/06 , C07D413/14 , Y10S514/825
摘要: Substituted heterocycles of the general structural formula: ##STR1## are tachykinin receptor antagonists useful in the treatment of inflammatory diseases, pain or migraine, asthma and emesis, and calcium channel blockers useful in the treatment of cardiovascular conditions such as angina, hypertension or ischemia.
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公开(公告)号:US06235735B1
公开(公告)日:2001-05-22
申请号:US09526843
申请日:2000-03-16
申请人: Conrad P. Dorn , Jeffrey J Hale , Paul E. Finke , Malcolm Maccoss , Sander G. Mills , Shrenik K. Shah , Mark Stuart Chambers , Tamara Ladduwahetty , Timothy Harrison , Brian John Williams
发明人: Conrad P. Dorn , Jeffrey J Hale , Paul E. Finke , Malcolm Maccoss , Sander G. Mills , Shrenik K. Shah , Mark Stuart Chambers , Tamara Ladduwahetty , Timothy Harrison , Brian John Williams
IPC分类号: A61K315355
CPC分类号: A61K31/41 , A61K31/50 , A61K31/53 , A61K31/535 , A61K31/54 , C07D265/30 , C07D265/32 , C07D279/12 , C07D413/04 , C07D413/06 , C07D413/14 , Y10S514/872
摘要: Substituted heterocycles of the general structural formula: are tachykinin receptor antagonists useful in the treatment of inflammatory diseases, pain or migraine, asthma and emesis, and calcium channel blockers useful in the treatment of cardiovascular conditions such as angina, hypertension or ischemia.
摘要翻译: 取代的通式结构式的杂环是用于治疗炎性疾病,疼痛或偏头痛,哮喘和呕吐的速激肽受体拮抗剂,以及可用于治疗心血管疾病如心绞痛,高血压或缺血的钙通道阻滞剂。
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公开(公告)号:US06048859A
公开(公告)日:2000-04-11
申请号:US251190
申请日:1999-02-16
申请人: Conrad P. Dorn , Paul E. Finke , Jeffrey J. Hale , Malcolm Maccoss , Sander G. Mills , Shrenik K. Shah , Mark Stuart Chambers , Timothy Harrison , Tamara Ladduwahetty , Brian John Williams
发明人: Conrad P. Dorn , Paul E. Finke , Jeffrey J. Hale , Malcolm Maccoss , Sander G. Mills , Shrenik K. Shah , Mark Stuart Chambers , Timothy Harrison , Tamara Ladduwahetty , Brian John Williams
IPC分类号: A61K31/41 , A61K31/50 , A61K31/53 , A61K31/535 , A61K31/5355 , A61K31/54 , A61P1/08 , A61P13/10 , C07D265/30 , C07D265/32 , C07D279/12 , C07D413/04 , C07D413/06 , C07D413/14
CPC分类号: A61K31/41 , A61K31/50 , A61K31/53 , A61K31/535 , A61K31/54 , C07D265/30 , C07D265/32 , C07D279/12 , C07D413/04 , C07D413/06 , C07D413/14 , Y10S514/872
摘要: Substituted heterocycles of the general structural formula: ##STR1## are tachykinin receptor antagonists useful in the treatment of inflammatory diseases, pain or migraine, asthma and emesis, and calcium channel blockers useful in the treatment of cardiovascular conditions such as angina, hypertension or ischemia.
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公开(公告)号:US5637699A
公开(公告)日:1997-06-10
申请号:US445489
申请日:1995-05-22
申请人: Conrad P. Dorn , Jeffrey J. Hale , Paul E. Finke , Malcolm MacCoss , Sander G. Mills , Shrenik K. Shah , Mark S. Chambers , Timothy Harrison , Tamara Ladduwahetty , Brian J. Williams
发明人: Conrad P. Dorn , Jeffrey J. Hale , Paul E. Finke , Malcolm MacCoss , Sander G. Mills , Shrenik K. Shah , Mark S. Chambers , Timothy Harrison , Tamara Ladduwahetty , Brian J. Williams
IPC分类号: C07D265/30 , C07D265/32 , C07D279/12 , C07D413/04 , C07D413/06 , C07D413/14 , C07D413/02 , C07D265/28 , C07D265/34
CPC分类号: C07D265/30 , C07D265/32 , C07D279/12 , C07D413/04 , C07D413/06 , C07D413/14
摘要: Substituted heterocycles of the general structural formula: ##STR1## are tachykinin receptor antagonists useful in the treatment of inflammatory diseases, pain or migraine, asthma and emesis, and calcium channel blockers useful in the treatment of cardiovascular conditions such as angina, hypertension or ischemia.
摘要翻译: 取代的通式结构式的杂环:
是可用于治疗炎性疾病,疼痛或偏头痛,哮喘和呕吐的速激肽受体拮抗剂,以及可用于治疗心血管疾病如心绞痛,高血压或缺血的钙通道阻滞剂。 -
公开(公告)号:US5922706A
公开(公告)日:1999-07-13
申请号:US969685
申请日:1997-11-13
申请人: Conrad P. Dorn , Jeffrey J. Hale , Malcolm Maccoss , Sander G. Mills , Shrenik K. Shah , Tamara Ladduwahetty
发明人: Conrad P. Dorn , Jeffrey J. Hale , Malcolm Maccoss , Sander G. Mills , Shrenik K. Shah , Tamara Ladduwahetty
IPC分类号: C07D265/30 , C07D265/32 , C07D279/12 , C07D413/04 , C07D413/06 , C07D413/14 , A61K31/535 , A61K31/54 , C07D417/04
CPC分类号: C07D265/30 , C07D265/32 , C07D279/12 , C07D413/04 , C07D413/06 , C07D413/14 , Y10S514/825
摘要: Substituted heterocycles of the general structural formula: ##STR1## are tachykinin receptor antagonists useful in the treatment of inflammatory diseases, pain or migraine, asthma and emesis, and calcium channel blockers useful in the treatment of cardiovascular conditions such as angina, hypertension or ischemia.
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公开(公告)号:US07592456B2
公开(公告)日:2009-09-22
申请号:US11791195
申请日:2005-11-28
申请人: Mark Stuart Chambers , Neil Roy Curtis , Emanuela Gancia , Myra Gilligan , Alexander Charles Humphries , Tamara Ladduwahetty , Robert James Maxey , Kevin John Merchant
发明人: Mark Stuart Chambers , Neil Roy Curtis , Emanuela Gancia , Myra Gilligan , Alexander Charles Humphries , Tamara Ladduwahetty , Robert James Maxey , Kevin John Merchant
IPC分类号: C07D215/00 , C07D401/02 , C07D401/00 , C07D401/10 , C07C305/00
CPC分类号: C07D401/12 , C07C311/08 , C07C317/14 , C07C317/22 , C07C317/24 , C07C317/32 , C07C317/42 , C07C317/44 , C07C323/65 , C07C2601/04 , C07D213/61 , C07D213/64 , C07D213/70 , C07D215/36 , C07D215/60 , C07D233/64 , C07D241/12 , C07D249/06 , C07D249/08 , C07D249/18 , C07D261/08 , C07D271/10 , C07D277/26 , C07D333/34 , C07D471/04 , C07D473/38
摘要: Compounds of formula (I) are potent and selective 5-HT2A antagonists, useful in treatment of a variety of adverse conditions of the CNS.
摘要翻译: 式(I)化合物是有效和选择性的5-HT2A拮抗剂,可用于治疗各种不良的CNS病症。
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公开(公告)号:US5973156A
公开(公告)日:1999-10-26
申请号:US68723
申请日:1998-05-13
申请人: Mark Stuart Chambers , Sarah Christine Hobbs , Tamara Ladduwahetty , Angus Murray MacLeod , Kevin John Merchant
发明人: Mark Stuart Chambers , Sarah Christine Hobbs , Tamara Ladduwahetty , Angus Murray MacLeod , Kevin John Merchant
IPC分类号: C07D401/06 , C07D413/14 , C07D521/00 , C07D401/14 , A61K31/445 , C07D409/14
CPC分类号: C07D231/12 , C07D233/56 , C07D249/08 , C07D401/06 , C07D413/14
摘要: A class of substituted piperidine and tetrahydropyridine derivatives, linked through the 4-position thereof via an alkylene chain to a fused bicyclic heteroaromatic moiety such as indolyl, and further substituted at the 1-position by an optionally substituted alkyl, alkenyl, alkynyl, cycloalkyl-alkyl, aryl-alkyl or heteroaryl-alkyl moiety, are selective agonists of 5-HT.sub.1 -like receptors, being potent agonists of the human 5-HT.sub.1D.spsb..alpha. receptor subtype whilst processing at least a 10-fold selective affinity for the 5-HT.sub.1D.spsb..alpha. receptor subtype relative to the 5-HT.sub.1D.spsb..beta. subtype; they are therefore useful in the treatment and/or prevention of clinical conditions, in particular migraine and associated disorders, for which a subtype-selective agonist of 5-HT.sub.1D receptors is indicated, whilst eliciting fewer side-effects, notably adverse cardiovascular events, than those associated with non-subtype-selective 5-HT.sub.1D receptor agonists.
摘要翻译: PCT No.PCT / GB96 / 02795 Sec。 371日期1998年5月13日 102(e)日期1998年5月13日PCT 1996年11月14日PCT PCT。 公开号WO97 / 19073 日期1997年5月29日一类取代的哌啶和四氢吡啶衍生物,其通过其4-位通过亚烷基链连接到稠合的双环杂芳族部分如吲哚基,并且在1位被进一步被任选取代的烷基,烯基, 炔基,环烷基 - 烷基,芳基 - 烷基或杂芳基 - 烷基部分是5-HT1样受体的选择性激动剂,其是人类5-HT1Dα受体亚型的有效激动剂,同时处理至少10倍的选择性亲和力 5-HT1Dα受体亚型相对于5-HT1Dβ亚型; 因此,它们可用于治疗和/或预防临床状况,特别是偏头痛和相关疾病,其中指出5-HT1D受体的亚型选择性激动剂,同时引起较少的副作用,特别是不利的心血管事件,比 与非亚型选择性5-HT1D受体激动剂相关的那些。
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公开(公告)号:US20120004221A1
公开(公告)日:2012-01-05
申请号:US13154485
申请日:2011-06-07
申请人: David John Haydon , Lloyd George Czaplewski , Nicholas John Palmer , Dale Robert Mitchell , John Frederick Atherall , Christopher Richard Steele , Tamara Ladduwahetty
发明人: David John Haydon , Lloyd George Czaplewski , Nicholas John Palmer , Dale Robert Mitchell , John Frederick Atherall , Christopher Richard Steele , Tamara Ladduwahetty
IPC分类号: A61K31/437 , A01N43/90 , A61K31/497 , A01P1/00 , A61K31/5377 , A61K31/506 , A61K31/5383 , A61P31/04 , C07D513/04 , A61K31/496
CPC分类号: A61K31/437 , A01N47/36 , A61K31/4375 , A61K31/4439 , A61K31/444 , A61K31/496 , A61K31/497 , A61K31/501 , A61K31/506 , A61K31/5377 , A61K31/5383
摘要: Compounds of formula (I) have antibacterial activity: wherein: m is 0 or 1; Q is hydrogen or cyclopropyl; Alk is an optionally substituted, divalent C1-C6 alkylene, alkenylene or alkynylene radical which may contain an ether (—O—), thioether (—S—) or amino (—NR)— link, wherein R is hydrogen, —CN or C1-C3 alkyl; X is —C(═O)NR6—, —S(O)NR6—, —C(═O)O— or —S(═O)O— wherein R6 is hydrogen, optionally substituted C1-C6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl, -Cyc, or —(C1-C3 alkyl)-Cyc wherein Cyc is optionally substituted monocyclic carbocyclic or heterocyclic having 3-7 ring atoms; Z is N; R2 and R3 are as defined in the description.
摘要翻译: 式(I)化合物具有抗菌活性:其中:m为0或1; Q是氢或环丙基; Alk是可以含有醚(-O-),硫醚(-S-)或氨基(-NR) - 连接的任意取代的二价C1-C6亚烷基,亚烯基或亚炔基,其中R是氢,-CN或 C1-C3烷基; X是-C(= O)NR 6 - , - S(O)NR 6 - , - C(= O)O-或-S(= O)O-,其中R 6是氢,任选取代的C 1 -C 6烷基, C6链烯基,C2-C6炔基,-Cyc或 - (C1-C3烷基)-Cyc,其中Cyc是具有3-7个环原子的任选取代的单环碳环或杂环; Z是N; R2和R3如说明书中所定义。
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