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公开(公告)号：US07396840B2
公开(公告)日：2008-07-08
申请号：US11345987
申请日：2006-02-02
申请人： Gary Bridger , Renato Skerlj , Al Kaller , Curtis Harwig , David Bogucki , Trevor R. Wilson , Jason Crawford , Ernest J. McEachern , Bern Atsma , Siqiao Nan , Yuanxi Zhou , Dominique Schols , Christopher Dennis Smith , Maria Rosaria Di Fluri
发明人： Gary Bridger , Renato Skerlj , Al Kaller , Curtis Harwig , David Bogucki , Trevor R. Wilson , Jason Crawford , Ernest J. McEachern , Bern Atsma , Siqiao Nan , Yuanxi Zhou , Dominique Schols , Christopher Dennis Smith , Maria Rosaria Di Fluri
IPC分类号： A61K31/4436 , A61K31/44 , A61K31/4439 , C07D401/02 , C07D471/02
CPC分类号： C07D401/14 , C07D213/38 , C07D213/65 , C07D401/12 , C07D405/14 , C07D409/14 , C07D413/14 , C07D417/14 , C07D471/04 , C07D493/04
摘要： Tertiary amine compounds that bind chemokine receptors such as CXCR4 and CCR5 are disclosed.
摘要翻译： 公开了结合趋化因子受体如CXCR4和CCR5的叔胺化合物。
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公开(公告)号：US20060128750A1
公开(公告)日：2006-06-15
申请号：US11345987
申请日：2006-02-02
申请人： Gary Bridger , Renato Skerlj , Al Kaller , Curtis Harwig , David Bogucki , Trevor Wilson , Jason Crawford , Ernest McEachern , Bem Atsma , Siqiao Nan , Yuanxi Zhou , Dominique Schols , Christopher Smith , Maria Di Fluri
发明人： Gary Bridger , Renato Skerlj , Al Kaller , Curtis Harwig , David Bogucki , Trevor Wilson , Jason Crawford , Ernest McEachern , Bem Atsma , Siqiao Nan , Yuanxi Zhou , Dominique Schols , Christopher Smith , Maria Di Fluri
IPC分类号： C07D401/14 , A61K31/4709
CPC分类号： C07D401/14 , C07D213/38 , C07D213/65 , C07D401/12 , C07D405/14 , C07D409/14 , C07D413/14 , C07D417/14 , C07D471/04 , C07D493/04
摘要： Tertiary amine compounds that bind chemokine receptors such as CXCR4 and CCR5 are disclosed.
摘要翻译： 公开了结合趋化因子受体如CXCR4和CCR5的叔胺化合物。
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公开(公告)号：US06864265B2
公开(公告)日：2005-03-08
申请号：US09957682
申请日：2001-09-17
申请人： Gary Bridger , Renato Skerlj , Al Kaller , Curtis Harwig , David Bogucki , Trevor R. Wilson , Jason Crawford , Ernest J. Mceachern , Bern Atsma , Siqiao Nan , Yuanxi Zhou , Dominique Schols , Christopher Dennis , Rosaria Maria Di Fluri
发明人： Gary Bridger , Renato Skerlj , Al Kaller , Curtis Harwig , David Bogucki , Trevor R. Wilson , Jason Crawford , Ernest J. Mceachern , Bern Atsma , Siqiao Nan , Yuanxi Zhou , Dominique Schols , Christopher Dennis , Rosaria Maria Di Fluri
IPC分类号： C07D491/052 , A61K31/44 , A61K31/4402 , A61K31/4439 , A61K31/4709 , A61K31/4725 , A61K31/497 , A61K31/506 , A61P31/18 , A61P43/00 , C07D213/38 , C07D213/65 , C07D401/12 , C07D401/14 , C07D405/14 , C07D409/14 , C07D413/14 , C07D417/14 , C07D471/04 , C07D493/04 , A61K31/4436 , C07D471/00
CPC分类号： C07D401/14 , C07D213/38 , C07D213/65 , C07D401/12 , C07D405/14 , C07D409/14 , C07D413/14 , C07D417/14 , C07D471/04 , C07D493/04
摘要： Compounds that bind to chemokine receptors such as CXCR4 and CCR5 demonstrate protective effects against infection of cells by human immunodeficiency virus are disclosed. These compounds contain a tertiary amine[[s]] linked to a core nitrogen via an aromatic or heteroaromatic moiety.
摘要翻译： 结合趋化因子受体如CXCR4和CCR5的化合物显示出针对人免疫缺陷病毒感染细胞的保护作用。 这些化合物含有通过芳族或杂芳族部分与核心氮连接的叔胺[[s]]。
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公开(公告)号：US20100105915A1
公开(公告)日：2010-04-29
申请号：US12612488
申请日：2009-11-04
申请人： Gary J. BRIDGER , Renato Skerlj , Ai Kaller , Curtis Harwig , David Bogucki , Trevor R. Wilson , Jason Crawford , Ernest J. Mceachern , Bem Atsma , Siqiao Nan , Yuanxi Zhou , Dominique Schols
发明人： Gary J. BRIDGER , Renato Skerlj , Ai Kaller , Curtis Harwig , David Bogucki , Trevor R. Wilson , Jason Crawford , Ernest J. Mceachern , Bem Atsma , Siqiao Nan , Yuanxi Zhou , Dominique Schols
IPC分类号： C07D401/02
CPC分类号： C07D239/42 , A61K45/06 , C07D213/38 , C07D215/40 , C07D401/12 , C07D401/14 , C07D405/14 , C07D409/14 , C07D413/14 , C07D417/14 , C07D451/04 , C07D471/04 , C07D487/04
摘要： Heterocyclic compounds that bind chemokine receptors and inhibit the binding of their natural ligands are disclosed. The invention compounds are protective against infection by HIV and exert effects characteristic of antagonists to the CXCR4 receptor.
摘要翻译： 公开了结合趋化因子受体并抑制其天然配体结合的杂环化合物。 本发明化合物可防止HIV感染并发挥拮抗剂对CXCR4受体特征的作用。
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公开(公告)号：US20060264434A1
公开(公告)日：2006-11-23
申请号：US11494943
申请日：2006-07-27
申请人： Gary Bridger , Renato Skerlj , Al Kaller , Curtis Harwig , David Bogucki , Trevor Wilson , Jason Crawford , Ernest McEachern , Bem Atsma , Siqiao Nan , Yuanxi Zhou , Dominique Schols
发明人： Gary Bridger , Renato Skerlj , Al Kaller , Curtis Harwig , David Bogucki , Trevor Wilson , Jason Crawford , Ernest McEachern , Bem Atsma , Siqiao Nan , Yuanxi Zhou , Dominique Schols
IPC分类号： A61K31/5377 , A61K31/4545 , A61K31/4439 , C07D401/02 , C07D413/02
CPC分类号： C07D239/42 , A61K45/06 , C07D213/38 , C07D215/40 , C07D401/12 , C07D401/14 , C07D405/14 , C07D409/14 , C07D413/14 , C07D417/14 , C07D451/04 , C07D471/04 , C07D487/04
摘要： This invention relates to a novel class of heterocyclic compounds that bind chemokine receptors, inhibiting the binding of their natural ligands thereby. These compounds result in protective effects against infection by HIV through binding to chemokine receptors, including CXCR4 and CCR5, thus inhibiting the subsequent binding by these chemokines. The present invention provides a compound of Formula I wherein, W is a nitrogen atom and Y is absent or, W is a carbon atom and Y=H; R1 to R7 may be the same or different and are independently selected from hydrogen or straight, branched or cyclic C1-6 alkyl; R8 is a substituted heterocyclic group or a substituted aromatic group Ar is an aromatic or heteroaromatic ring each optionally substituted at single or multiple, non-linking positions with electron-donating or withdrawing groups; n and n′ are independently, 0-2; X is a group of the formula: Wherein, Ring A is an optionally substituted, saturated or unsaturated 5 or 6-membered ring, and P is an optionally substituted carbon atom, an optionally substituted nitrogen atom, sulfur or oxygen atom. Ring B is an optionally substituted 5 to 7-membered ring. Ring A and Ring B in the above formula can be connected to the group W from any position via the group V, wherein V is a chemical bond, a (CH2)n″ group (where n″=0-2) or a C═O group. Z is, (1) a hydrogen atom, (2) an optionally substituted C1-6 alkyl group, (3) a C0-6 alkyl group substituted with an optionally substituted aromatic or heterocyclic group, (4) an optionally substituted C0-6 alkylamino or C3-7 cycloalkylamino group, (5) an optionally substituted carbonyl group or sulfonyl. These compounds further include any pharmaceutically acceptable acid addition salts and metal complexes thereof and any stereoisomeric forms and mixtures of stereoisomeric forms thereof.
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公开(公告)号：US07091217B2
公开(公告)日：2006-08-15
申请号：US10799386
申请日：2004-03-11
申请人： Gary Bridger , Renato Skerlj , Al Kaller , Curtis Harwig , David Bogucki , Trevor R. Wilson , Jason Crawford , Ernest J. McEachern , Bem Atsma , Siqiao Nan , Yuanxi Zhou , Dominique Schols , Christopher Dennis Smith , Maria Rosaria Di Fluri
发明人： Gary Bridger , Renato Skerlj , Al Kaller , Curtis Harwig , David Bogucki , Trevor R. Wilson , Jason Crawford , Ernest J. McEachern , Bem Atsma , Siqiao Nan , Yuanxi Zhou , Dominique Schols , Christopher Dennis Smith , Maria Rosaria Di Fluri
IPC分类号： A61K31/47 , C07D221/02
CPC分类号： C07D213/81 , A61K31/4709 , C07D213/38 , C07D213/65 , C07D215/40 , C07D231/12 , C07D233/56 , C07D249/08 , C07D401/12 , C07D401/14 , C07D405/14 , C07D409/14 , C07D413/14 , C07D417/14 , C07D471/04 , C07D491/04 , C07D493/04 , Y02A50/411
摘要： Compounds which modulate chemokine receptor activities are disclosed. These compounds are preferably tertiary amines comprising tetrahydroquinoline and benzimidazole.
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公开(公告)号：US20050277670A1
公开(公告)日：2005-12-15
申请号：US11012002
申请日：2004-12-13
申请人： Yuanxi Zhou , Gary Bridger , Renato Skerlj , David Bogucki , Wen Yang , Elyse Bourque , Jonathan Langille , Tong-Shuang Li , Markus Metz , Maria Di Fluri , Siqiao Nan
发明人： Yuanxi Zhou , Gary Bridger , Renato Skerlj , David Bogucki , Wen Yang , Elyse Bourque , Jonathan Langille , Tong-Shuang Li , Markus Metz , Maria Di Fluri , Siqiao Nan
IPC分类号： A61K31/4545 , C07D401/12 , C07D401/14 , C07D413/14 , C07D417/14 , C12N20060101 , C07D43/02
CPC分类号： C07D401/14 , C07D401/12 , C07D413/14 , C07D417/14
摘要： The present invention relates to chemokine receptor binding compounds, pharmaceutical compositions and their use. More specifically, the present invention relates to modulators of chemokine receptor activity, preferably modulators of CCR5. These compounds demonstrate protective effects against infection of target cells by a human immunodeficiency virus (HIV).
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公开(公告)号：US07354934B2
公开(公告)日：2008-04-08
申请号：US11301725
申请日：2005-12-13
申请人： Gary J. Bridger , Al Kaller , Curtis Harwig , Renato T. Skerlj , David Bogucki , Trevor R. Wilson , Jason B. Crawford , Ernest J. McEachern , Bem Atsma , Siqiao Nan , Yuanxi Zhou , Dominique Schols , Christopher Dennis Smith , Maria R. Di Fluri
发明人： Gary J. Bridger , Al Kaller , Curtis Harwig , Renato T. Skerlj , David Bogucki , Trevor R. Wilson , Jason B. Crawford , Ernest J. McEachern , Bem Atsma , Siqiao Nan , Yuanxi Zhou , Dominique Schols , Christopher Dennis Smith , Maria R. Di Fluri
IPC分类号： A61K31/4709 , C07D403/12
CPC分类号： C07D401/14 , C07D235/14 , C07D401/12 , C07D403/12 , C07D471/04 , C07D471/06 , C07D491/04
摘要： The invention relates to heterocyclic compounds consisting of a core nitrogen atom surrounded by three pendant groups, wherein two of the three pendant groups are preferably benzimidazolyl methyl and tetrahydroquinolyl, and the third pendant group contains N and optionally contains additional rings. The compounds bind to chemokine receptors, including CXCR4 and CCR5, and demonstrate protective effects against infection of target cells by a human immunodeficiency virus (HIV).
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公开(公告)号：US20060252795A1
公开(公告)日：2006-11-09
申请号：US11487038
申请日：2006-07-14
申请人： Gary Bridger , Renato Skerlj , Al Kaller , Curtis Harwig , David Bogucki , Trevor Wilson , Jason Crawford , Ernest McEachern , Bem Atsma , Siqiao Nan , Yuanxi Zhou , Dominique Schols , Christopher Smith , Maria Di Fluri
发明人： Gary Bridger , Renato Skerlj , Al Kaller , Curtis Harwig , David Bogucki , Trevor Wilson , Jason Crawford , Ernest McEachern , Bem Atsma , Siqiao Nan , Yuanxi Zhou , Dominique Schols , Christopher Smith , Maria Di Fluri
IPC分类号： A61K31/4709
CPC分类号： C07D213/81 , A61K31/4709 , C07D213/38 , C07D213/65 , C07D215/40 , C07D231/12 , C07D233/56 , C07D249/08 , C07D401/12 , C07D401/14 , C07D405/14 , C07D409/14 , C07D413/14 , C07D417/14 , C07D471/04 , C07D491/04 , C07D493/04 , Y02A50/411
摘要： Compounds which modulate chemokine receptor activities are disclosed. These compounds are preferably tertiary amines comprising tetrahydroquinoline and benzimidazole.
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公开(公告)号：US20060100240A1
公开(公告)日：2006-05-11
申请号：US11301725
申请日：2005-12-13
申请人： Gary Bridger , Ai Kaller , Curtis Harwig , Renato Skerlj , David Bogucki , Trevor Wilson , Jason Crawford , Ernest McEachern , Bem Atsma , Siqiao Nan , Yuanxi Zhou , Dominique Schols , Christopher Smith , Maria Di Fluri
发明人： Gary Bridger , Ai Kaller , Curtis Harwig , Renato Skerlj , David Bogucki , Trevor Wilson , Jason Crawford , Ernest McEachern , Bem Atsma , Siqiao Nan , Yuanxi Zhou , Dominique Schols , Christopher Smith , Maria Di Fluri
IPC分类号： A61K31/4709 , C07D403/02 , C07D403/14
CPC分类号： C07D401/14 , C07D235/14 , C07D401/12 , C07D403/12 , C07D471/04 , C07D471/06 , C07D491/04
摘要： The invention relates to heterocyclic compounds consisting of a core nitrogen atom surrounded by three pendant groups, wherein two of the three pendant groups are preferably benzimidazolyl methyl and tetrahydroquinolyl, and the third pendant group contains N and optionally contains additional rings. The compounds bind to chemokine receptors, including CXCR4 and CCR5, and demonstrate protective effects against infection of target cells by a human immunodeficiency virus (HIV).
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