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1. 发明授权

US07501518B2 Methods of making 2,6-diaryl piperidine derivatives 有权
标题翻译：制备2,6-二芳基哌啶衍生物的方法
公开(公告)号：US07501518B2
公开(公告)日：2009-03-10
申请号：US10977221
申请日：2004-10-28
申请人： Gang Chen , Jason Crawford , Renato Skerlj
发明人： Gang Chen , Jason Crawford , Renato Skerlj
IPC分类号： C07D213/127
CPC分类号： C07D401/14 , C07D211/74 , C07D409/14 , C07D413/14 , C07D417/14
摘要： Methods for preparing 2,6-diaryl piperidine derivatives are described. More particularly, 2,6-diaryl piperidines having formula 1-4 are prepared by cyclocondensation of an aryl or heteroaryl aldehyde with 1,3-acetonedicarboxylic acid.
摘要翻译：描述了制备2,6-二芳基哌啶衍生物的方法。更具体地，具有式1-4的2,6-二芳基哌啶通过芳基或杂芳基醛与1,3-丙酮二羧酸的环化缩合制备。

2. 发明申请

US20050209277A1 Process for the synthesis of CXCR4 antagonist 有权
标题翻译：合成CXCR4拮抗剂的方法
公开(公告)号：US20050209277A1
公开(公告)日：2005-09-22
申请号：US11077896
申请日：2005-03-11
申请人： Jason Crawford , Gang Chen , David Gauthier , Renato Skerlj , Ian Baird , Trevor Wilson
发明人： Jason Crawford , Gang Chen , David Gauthier , Renato Skerlj , Ian Baird , Trevor Wilson
IPC分类号： A61K31/4709 , C07D215/38 , C07D215/40 , C07D401/12 , C07D401/14 , C07D43/02
CPC分类号： C07D401/14 , C07D215/40 , C07D401/12 , Y02P20/55
摘要： This invention relates to a process for synthesizing heterocyclic pharmaceutical compound which binds to the CXCR4 chemokine receptor. In one embodiment, the process comprises: a) reacting a 5,6,7,8-tetrahydroquinolinylamine and an alkyl aldehyde bearing a phthalimide or a di-tertiary-butoxycarbonyl (di-BOC) protecting group to form an imine; b) reducing the imine to form a secondary amine; c) reacting the secondary amine with a haloalkyl substituted heterocyclic compound, to form a phthalimido-protected or di-tert-butoxycarbonyl protected tertiary amine; and d) hydrolyzing the protected amine to obtain a compound having Formula I′
摘要翻译：本发明涉及一种结合CXCR4趋化因子受体的杂环药物化合物的合成方法。在一个实施方案中，该方法包括：a）使5,6,7,8-四氢喹啉基胺和带有邻苯二甲酰亚胺或二叔丁氧基羰基（二-BOC）保护基团的烷基醛反应以形成亚胺; b）还原亚胺以形成仲胺; c）使仲胺与卤代烷基取代的杂环化合物反应，形成邻苯二甲酰亚氨基保护或二叔丁氧羰基保护的叔胺; 和d）水解受保护的胺以获得具有式I'

3. 发明申请

US20060069122A1 Chemokine-binding heterocyclic compound salts, and methods of use thereof 有权
标题翻译：趋化因子结合杂环化合物盐及其使用方法
公开(公告)号：US20060069122A1
公开(公告)日：2006-03-30
申请号：US11235469
申请日：2005-09-26
申请人： Jason Crawford , Yongbao Zhu , Gang Chen , Ian Baird , Renato Skerlj
发明人： Jason Crawford , Yongbao Zhu , Gang Chen , Ian Baird , Renato Skerlj
IPC分类号： A61K31/4709 , C07D403/02
CPC分类号： C07D401/12
摘要： The present invention relates to chemokine-binding heterocyclic compound salts, methods of use thereof, and methods for preparing the same.
摘要翻译：本发明涉及趋化因子结合杂环化合物盐，其使用方法及其制备方法。

4. 发明申请

US20050154201A1 Methods of making 2,6-diaryl piperidine derivatives 有权
标题翻译：制备2,6-二芳基哌啶衍生物的方法
公开(公告)号：US20050154201A1
公开(公告)日：2005-07-14
申请号：US10977221
申请日：2004-10-28
申请人： Gang Chen , Jason Crawford , Renato Skerlj
发明人： Gang Chen , Jason Crawford , Renato Skerlj
IPC分类号： A61K31/444 , C07D43/14 , C07D41/14
CPC分类号： C07D401/14 , C07D211/74 , C07D409/14 , C07D413/14 , C07D417/14
摘要： Methods for preparing 2,6-diaryl piperidine derivatives are described. More particularly, 2,6-diaryl piperidines having formula 1-4 are prepared by cyclocondensation of an aryl or heteroaryl aldehyde with 1,3-acetonedicarboxylic acid.
摘要翻译：描述了制备2,6-二芳基哌啶衍生物的方法。更具体地，具有式1-4的2,6-二芳基哌啶通过芳基或杂芳基醛与1,3-丙酮二羧酸的环化缩合制备。

5. 发明授权

US07183273B2 Chemokine receptor binding heterocyclic compounds 失效
标题翻译：趋化因子受体结合杂环化合物
公开(公告)号：US07183273B2
公开(公告)日：2007-02-27
申请号：US10837467
申请日：2004-04-30
申请人： Gary J. 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
发明人： Gary J. 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
IPC分类号： A61K31/55 , A61K31/47 , A61K31/445 , A61P19/02 , A61P31/18
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。

6. 发明申请

US20050026942A1 Chemokine receptor binding heterocyclic compounds 失效
标题翻译：趋化因子受体结合杂环化合物
公开(公告)号：US20050026942A1
公开(公告)日：2005-02-03
申请号：US10914663
申请日：2004-08-09
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： A61K31/444 , A61K31/4545 , A61K31/455 , A61K31/4706 , A61K31/4709 , A61K31/506 , A61P1/04 , A61P3/10 , A61P5/14 , A61P9/00 , A61P11/00 , A61P11/02 , A61P11/06 , A61P13/12 , A61P17/00 , A61P17/02 , A61P17/04 , A61P17/06 , A61P19/00 , A61P19/02 , A61P21/00 , A61P21/04 , A61P29/00 , A61P31/04 , A61P31/12 , A61P31/18 , A61P31/22 , A61P33/00 , A61P33/02 , A61P33/06 , A61P33/10 , A61P35/00 , A61P35/02 , A61P37/00 , A61P37/02 , A61P37/08 , A61P43/00 , C07D213/81 , C07D215/40 , C07D401/12 , C07D401/14 , C07D413/14 , C07D417/14 , C07D471/04 , C07D491/04 , C07D491/052 , C07D471/02 , A61K31/47 , C07D491/02 , C07D498/02
CPC分类号： C07D213/38 , C07D213/65 , C07D213/81 , C07D215/40 , C07D401/12 , C07D401/14 , C07D413/14 , C07D417/14 , C07D471/04 , C07D491/04
摘要： Tertiary amines containing a multiplicity of heteroaromatic substituents are useful as chemokine receptor modulators.
摘要翻译：含有多个杂芳族取代基的叔胺可用作趋化因子受体调节剂。

7. 发明授权

US06750348B1 Chemokine receptor binding heterocyclic compounds 失效
标题翻译：趋化因子受体结合杂环化合物
公开(公告)号：US06750348B1
公开(公告)日：2004-06-15
申请号：US09535314
申请日：2000-03-24
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
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
IPC分类号： C07D21516
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.
摘要翻译：本发明涉及结合趋化因子受体的新一类杂环化合物，从而抑制其天然配体的结合。这些化合物通过结合趋化因子受体（包括CXCR4和CCR5）导致HIV感染的保护作用，从而抑制随后与这些趋化因子的结合。本发明提供式I化合物，其中W是氮原子，Y不存在，或W是碳原子，Y = H; R 1至R 7可以相同或不同并且独立地选自来自氢或直链，支链或环状的C 1-6烷基; R 8是取代的杂环基或取代的芳族基团Ar是芳族或杂芳族环，其各自任选在单个或多个非连接位置被取代，具有给电子或取代基; n和n'独立地是0-2; X是下式的基团：其中环A是任选取代的饱和或不饱和的5或6元环，并且P是任选取代的碳原子，任选取代的氮原子，硫或氧原子。环B是任选取代的5至7元环。上述式中的环A和环B可以通过组V从任何位置连接到基团W，其中V是化学键，（CH2）n“基团（其中n”= 0-2）或一个C = O组。 Z为（1）氢原子，（2）任选取代的C 1-6烷基，（3）被任意取代的芳族或杂环基团取代的C 0-6烷基，（4）任选取代的C 0-6 烷基氨基或C 3-7环烷基氨基，（5）任选取代的羰基或磺酰基。这些化合物还包括其任何药学上可接受的酸加成盐和金属络合物以及其立体异构体形式及其立体异构形式的混合物。

8. 发明申请

US20100105915A1 CHEMOKINE RECEPTOR BINDING HETEROCYCLIC COMPOUNDS 审中-公开
标题翻译：化合物受体结合杂环化合物
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。

9. 发明申请

US20060264434A1 Chemokine receptor binding heterocyclic compounds 失效
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.

10. 发明授权

US07091217B2 Chemokine receptor binding heterocyclic compounds 失效
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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