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1. 发明申请

US20060223180A1 Methods to mobilize progenitor/stem cells 审中-公开
标题翻译：调动祖细胞/干细胞的方法
公开(公告)号：US20060223180A1
公开(公告)日：2006-10-05
申请号：US11446390
申请日：2006-06-02
申请人： Gary Bridger , Michael Abrams , Geoffrey Henson , Ronald MacFarland , Gary Calandra , Hal Broxmeyer , David Dale
发明人： Gary Bridger , Michael Abrams , Geoffrey Henson , Ronald MacFarland , Gary Calandra , Hal Broxmeyer , David Dale
IPC分类号： A61K31/33 , C12N5/08
CPC分类号： A61K31/395 , A61K31/33 , A61K31/4427 , A61K31/496 , A61K31/55 , A61K31/551 , A61K31/555 , A61K35/28 , A61K38/193 , A61K38/195 , A61K2035/124 , C12N5/0647 , A61K2300/00
摘要： Methods to elevate progenitor and stem cell counts in animal subjects using compounds which bind to the chemokine receptor CXCR4 are disclosed. Preferred embodiments of such compounds are of the formula Z-linker-Z′ (1) or pharmaceutically acceptable salt thereof wherein Z is a cyclic polyamine containing 9-32 ring members of which 3-8 are nitrogen atoms, said nitrogen atoms separated from each other by at least 2 carbon atoms, and wherein said heterocycle may optionally contain additional heteroatoms besides nitrogen and/or may be fused to an additional ring system; or Z is of the formula wherein A comprises a monocyclic or bicyclic fused ring system containing at least one N and B is H or an organic moiety of 1-20 atoms, Z′ may be embodied in a form as defined by Z above, or alternatively may be of the formula —N(R)—(CR2)n—X wherein each R is independently H or straight, branched or cyclic alkyl (1-6C), n is 1 or 2, and X is an aromatic ring, including heteroaromatic rings, or is a mercaptan; “linker” represents a bond, alkylene (1-6C) or may comprise aryl, fused aryl, oxygen atoms contained in an alkylene chain, or may contain keto groups or nitrogen or sulfur atoms.
摘要翻译：公开了使用结合趋化因子受体CXCR4的化合物来提高动物受试者祖细胞和干细胞计数的方法。这些化合物的优选实施方案具有式<？in-line-formula description =“In-line Formulas”end =“lead”？> Z-linker-Z'（1）<？in-line-formula description =“ 其中Z是含有9-32个环成员的环状多胺，其中3-8个是氮原子，所述氮原子彼此分开至少2个碳原子并且其中所述杂环可以任选地含有除氮之外的另外的杂原子和/或可以与另外的环系稠合; 或Z具有下式：其中A包含含有至少一个N的单环或双环稠合环体系，B是H或1-20个原子的有机部分，Z'可以以上述Z所定义的形式实施，或可替代地可以是公式<？in-line-formula description =“In-line Formulas”end =“lead”？> - N（R） - （CR <2> 其中每个R独立地是H或直链，支链或环状的烷基（1-6C），n是1或者 2，X为芳环，包括杂芳环，或为硫醇; “接头”表示键，亚烷基（1-6C）或可包含亚烷基链中所含的芳基，稠合芳基，氧原子，或可含有酮基或氮或硫原子。

2. 发明申请

US20060193826A1 Methods to mobilize progenitor/stem cells 有权
标题翻译：调动祖细胞/干细胞的方法
公开(公告)号：US20060193826A1
公开(公告)日：2006-08-31
申请号：US11269773
申请日：2005-11-08
申请人： Gary Bridger , Michael Abrams , Geoffrey Henson , Ronald MacFarland , Gary Calandra , Hal Broxmeyer , David Dale
发明人： Gary Bridger , Michael Abrams , Geoffrey Henson , Ronald MacFarland , Gary Calandra , Hal Broxmeyer , David Dale
IPC分类号： A61K38/19 , A61K31/551 , A61K31/33
CPC分类号： A61K31/395 , A61K31/33 , A61K31/4427 , A61K31/496 , A61K31/55 , A61K31/551 , A61K31/555 , A61K35/28 , A61K38/193 , A61K38/195 , A61K2035/124 , C12N5/0647 , A61K2300/00
摘要： Methods to elevate progenitor and stem cell counts in animal subjects using compounds which bind to the chemokine receptor CXCR4 are disclosed. Preferred embodiments of such compounds are of the formula Z-linker-Z′ (1) or pharmaceutically acceptable salt thereof wherein Z is a cyclic polyamine containing 9-32 ring members of which 3-8 are nitrogen atoms, said nitrogen atoms separated from each other by at least 2 carbon atoms, and wherein said heterocycle may optionally contain additional heteroatoms besides nitrogen and/or may be fused to an additional ring system; or Z is of the formula N wherein A comprises a monocyclic or bicyclic fused ring system containing at least one N and B is H or an organic moiety of 1-20 atoms, Z′ may be embodied in a form as defined by Z above, or alternatively may be of the formula —N(R)—(CR2)n—X wherein each R is independently H or straight, branched or cyclic alkyl (1-6C), n is 1 or 2, and X is an aromatic ring, including heteroaromatic rings, or is a mercaptan; “linker” represents a bond, alkylene (1-6C) or may comprise aryl, fused aryl, oxygen atoms contained in an alkylene chain, or may contain keto groups or nitrogen or sulfur atoms.
摘要翻译：公开了使用结合趋化因子受体CXCR4的化合物来提高动物受试者祖细胞和干细胞计数的方法。这些化合物的优选实施方案具有式<？in-line-formula description =“In-line Formulas”end =“lead”？> Z-linker-Z'（1）<？in-line-formula description =“ 其中Z是含有9-32个环成员的环状多胺，其中3-8个是氮原子，所述氮原子彼此分开至少2个碳原子并且其中所述杂环可以任选地含有除氮之外的另外的杂原子和/或可以与另外的环系稠合; 或Z具有式N，其中A包含含有至少一个N的单环或双环稠合环体系，B是H或1-20个原子的有机部分，Z'可以以Z所定义的形式实施，或者可以具有公式<？in-line-formula description =“In-line Formulas”end =“lead”？> - N（R） - （CR 2 2 N）n 其中每个R独立地为H或直链，支链或环状的烷基（1-6C），n为1，其中每个R独立地为H或直链，支链或环状的烷基（1-6C）或2，X是芳环，包括杂芳环，或是硫醇; “接头”表示键，亚烷基（1-6C）或可包含亚烷基链中所含的芳基，稠合芳基，氧原子，或可含有酮基或氮或硫原子。

3. 发明申请

US20080063624A1 METHODS TO MOBILIZE PROGENITOR/STEM CELLS 有权
标题翻译：移动原核细胞/干细胞的方法
公开(公告)号：US20080063624A1
公开(公告)日：2008-03-13
申请号：US11841837
申请日：2007-08-20
申请人： Gary Bridger , Michael Abrams , Geoffrey Henson , Ronald Macfarland , Gary Calandra , Hal Broxmeyer , David Dale
发明人： Gary Bridger , Michael Abrams , Geoffrey Henson , Ronald Macfarland , Gary Calandra , Hal Broxmeyer , David Dale
IPC分类号： A61K31/395 , A61K31/4427 , A61K38/19 , A61P9/00
CPC分类号： A61K31/395 , A61K31/33 , A61K31/4427 , A61K31/496 , A61K31/55 , A61K31/551 , A61K31/555 , A61K35/28 , A61K38/193 , A61K38/195 , A61K2035/124 , C12N5/0647 , A61K2300/00
摘要： Methods to elevate progenitor and stem cell counts in animal subjects using compounds which bind to the chemokine receptor CXCR4 are disclosed. Preferred embodiments of such compounds are of the formula Z-linker-Z′ (1) or pharmaceutically acceptable salt thereof wherein Z is a cyclic polyamine containing 9-32 ring members of which 3-8 are nitrogen atoms, said nitrogen atoms separated from each other by at least 2 carbon atoms, and wherein said heterocycle may optionally contain additional heteroatoms besides nitrogen and/or may be fused to an additional ring system; wherein A comprises a monocyclic or bicyclic fused ring system containing at least one N and B is H or an organic moiety of 1-20 atoms, Z′ may be embodied in a form as defined by Z above, or alternatively may be of the formula —N(R)—(CR2)n—X wherein each R is independently H or straight, branched or cyclic alkyl (1-6C), n is 1 or 2, and X is an aromatic ring, including heteroaromatic rings, or is a mercaptan; “linker” represents a bond, alkylene (1-6C) or may comprise aryl, fused aryl, oxygen atoms contained in an alkylene chain, or may contain keto groups or nitrogen or sulfur atoms.
摘要翻译：公开了使用结合趋化因子受体CXCR4的化合物来提高动物受试者祖细胞和干细胞计数的方法。这些化合物的优选实施方案具有式<？in-line-formula description =“In-line Formulas”end =“lead”？> Z-linker-Z'（1）<？in-line-formula description =“ 其中Z是含有9-32个环成员的环状多胺，其中3-8个是氮原子，所述氮原子彼此分开至少2个碳原子并且其中所述杂环可以任选地含有除氮之外的另外的杂原子和/或可以与另外的环系稠合; 其中A包含含有至少一个N的单环或双环稠环体系，B是H或1-20个原子的有机部分，Z'可以以上述Z所定义的形式实施，或者可以是式 <？in-line-formula description =“In-line Formulas”end =“lead”？> - N（R） - （CR 2）N < 其中每个R独立地为H或直链，支链或环状烷基（1-6C），n为1或2，X为芳环，包括杂芳环，或是硫醇; “接头”表示键，亚烷基（1-6C）或可包含亚烷基链中所含的芳基，稠合芳基，氧原子，或可含有酮基或氮或硫原子。

4. 发明申请

US20050043367A1 Methods to mobilize progenitor/stem cells 有权
标题翻译：调动祖细胞/干细胞的方法
公开(公告)号：US20050043367A1
公开(公告)日：2005-02-24
申请号：US10456942
申请日：2003-06-05
申请人： Gary Bridger , Michael Abrams , Geoffrey Henson , Ronald MacFarland , Gary Calandra
发明人： Gary Bridger , Michael Abrams , Geoffrey Henson , Ronald MacFarland , Gary Calandra
IPC分类号： A61K31/33 , A61K31/496 , A61K31/55 , A61K31/551 , A61K31/555 , A61K38/00 , A61K38/19 , A61K31/44 , A61K31/137 , A61K31/40
CPC分类号： A61K31/33 , A61K31/496 , A61K31/55 , A61K31/551 , A61K31/555 , A61K38/193 , A61K38/195 , A61K47/555 , A61K2300/00
摘要： Methods to elevate progenitor and stem cell counts in animal subjects using compounds which bind to the chemokine receptor CXCR4 are disclosed. Preferred embodiments of such compounds are of the formula Z-linker-Z′ (1)or pharmaceutically acceptable salt thereof wherein Z is of the formula wherein A comprises a monocyclic or bicyclic fused ring system containing at least one N and B is H or an organic moiety of 1-20 atoms, Z′ is of the formula —Ar(Y)j;wherein Ar is an aromatic or heteroaromatic moiety, and each Y is independently a non-interfering substituent and j is 0-3; and “linker” represents a bond, alkylene (1-6C) or may comprise aryl, fused aryl, oxygen atoms contained in an alkylene chain, or may contain keto groups or nitrogen or sulfur atoms.
摘要翻译：公开了使用结合趋化因子受体CXCR4的化合物来提高动物受试者祖细胞和干细胞计数的方法。这种化合物的优选实施方案是式Z-接头-Z'（1）或其药学上可接受的盐，其中Z具有下式：其中A包含含有至少一个N的单环或双环稠环体系，B是H或有机部分为1-20个原子，Z'为-Ar（Y）j; 其中Ar是芳族或杂芳族部分，并且每个Y独立地是非干扰性取代基，并且j是0-3; 和“接头”表示键，亚烷基（1-6C）或可包含芳基，稠合芳基，亚烷基链中所含的氧原子，或可含有酮基或氮或硫原子。

5. 发明申请

US20070116782A1 USE OF RARE EARTH COMPOUNDS FOR THE PREVENTION OF KIDNEY STONE DISEASE 审中-公开
标题翻译：使用稀土化合物进行防治石棺病
公开(公告)号：US20070116782A1
公开(公告)日：2007-05-24
申请号：US11538926
申请日：2006-10-05
申请人： Michael Abrams , Gary Bridger , Simon Fricker , Stefan Idzan
发明人： Michael Abrams , Gary Bridger , Simon Fricker , Stefan Idzan
IPC分类号： A61K33/24
CPC分类号： A61K33/00 , Y10S514/891
摘要： Conditions such as kidney stones, which are characterized by undesired absorption of oxalate from the intestinal tract are conveniently treated using nontoxic salts of rare earth metal ions.
摘要翻译：其特征在于从肠道不期望地吸收草酸盐的肾结石等条件便利地使用稀土金属离子的无毒盐进行处理。

6. 发明申请

US20070060591A1 Chemokine receptor binding heterocyclic compounds 审中-公开
标题翻译：趋化因子受体结合杂环化合物
公开(公告)号：US20070060591A1
公开(公告)日：2007-03-15
申请号：US11599066
申请日：2006-11-13
申请人： Gary Bridger , Eva Boehringer , Dominique Schols , Renato Skerlj , David Bogucki
发明人： Gary Bridger , Eva Boehringer , Dominique Schols , Renato Skerlj , David Bogucki
IPC分类号： A61K31/52 , A61K31/496 , A61K31/4439
CPC分类号： C07D401/12 , A61K31/33 , A61K31/4439 , A61K31/496 , A61K31/52 , C07D257/02 , C07D403/12 , C07D413/12 , C07D417/12 , Y02A50/411
摘要： The present invention is drawn to novel antiviral compounds, pharmaceutical compositions and their use. More specifically this invention is drawn to derivatives of monocyclic polyamines which have activity in standard tests against HIV- or FIV-infected cells as well as other biological activity related to binding of ligands to chemokine receptors that mediate a number of mammalian embryonic developmental processes.
摘要翻译：本发明涉及新的抗病毒化合物，药物组合物及其应用。更具体地，本发明涉及在针对HIV或FIV感染的细胞的标准测试中具有活性的单环多胺的衍生物以及与介导多种哺乳动物胚胎发育过程的配体与趋化因子受体的结合相关的其它生物活性。

7. 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.

8. 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.

9. 发明申请

US20050277670A1 Chemokine receptor binding compounds 失效
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).

10. 发明申请

US20050154005A1 Methods to modulate conditions mediated by the CXCR4 receptor 有权
标题翻译：调节由CXCR4受体介导的病症的方法
公开(公告)号：US20050154005A1
公开(公告)日：2005-07-14
申请号：US10991944
申请日：2004-11-17
申请人： Gary Bridger , Eva Boehringer , Zhongren Wang , Dominique Schols , Renato Skerlj , David Bogucki
发明人： Gary Bridger , Eva Boehringer , Zhongren Wang , Dominique Schols , Renato Skerlj , David Bogucki
IPC分类号： A61K31/381 , A61K31/395 , A61K31/4178 , A61K31/4353 , A61K31/44 , A61K31/4427 , A61K31/4433 , A61K31/444 , A61K31/496 , A61K31/497 , A61K31/52 , A61K31/675 , A61P1/00 , A61P19/02 , A61P21/02 , A61P25/00 , A61P31/12 , A61P31/18 , A61P35/00 , C07D257/02 , C07D401/06 , C07D401/12 , C07D403/12 , C07D409/12 , C07D471/06 , C07D471/08 , C07D473/00 , C07D487/08 , A61K31/4745 , C07D487/14
CPC分类号： C07D473/00 , C04B35/632 , C07D257/02 , C07D401/06 , C07D401/12 , C07D403/12 , C07D409/12 , C07D471/06
摘要： The present invention is drawn to novel antiviral compounds, pharaceutical compositions and their use. More specifically this invention is drawn to derivatives of monocyclic polyamines wihich have activity in standard tests against HIV- or FIV-infected cells as well as other biological activity related to binding of ligands to chemokine receptors that mediate a number of mammalian embryonic developmental processes.
摘要翻译：本发明涉及新型抗病毒化合物，药物组合物及其用途。更具体地，本发明涉及在具有针对HIV或FIV感染细胞的标准测试中具有活性的单环多胺衍生物以及与介导多种哺乳动物胚胎发育过程的配体与趋化因子受体的结合相关的其它生物活性。

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