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公开(公告)号：US08455490B2
公开(公告)日：2013-06-04
申请号：US13559065
申请日：2012-07-26
申请人： William F. DeGrado , Gregory N. Tew , Michael L. Klein , Dahui Liu , Jing Yuan , Sungwook Choi
发明人： William F. DeGrado , Gregory N. Tew , Michael L. Klein , Dahui Liu , Jing Yuan , Sungwook Choi
IPC分类号： A01N43/58 , A01N43/60 , A01N43/54 , A61K31/50 , A61K31/495 , C07D239/42 , C07D471/04 , C07D471/22 , C07D487/04
CPC分类号： A61K31/17 , A61K31/16 , A61K31/165 , A61K31/495 , C07C233/64 , C07C323/42 , C07C323/44 , C08G18/3225 , C08G73/028 , C08L75/02
摘要： The present invention discloses methods of use of facially amphiphilic polymers and oligomers, including pharmaceutical uses of the polymers and oligomers as antimicrobial agents and antidotes for hemorrhagic complications associated with heparin therapy. The present invention also discloses novel facially amphiphilic polymers and oligomers and their compositions, including pharmaceutical compositions. The present invention further discloses the design and synthesis of facially amphiphilic polymers and oligomers.
摘要翻译： 本发明公开了使用表面两亲性聚合物和低聚物的方法，包括聚合物和低聚物作为抗微生物剂的药物用途和与肝素治疗相关的出血并发症的解毒剂。 本发明还公开了新颖的表面两亲聚合物和低聚物及其组合物，包括药物组合物。 本发明还公开了表面两亲聚合物和低聚物的设计和合成。
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2.发明申请Inhibitors of Integrin Alpha2Beta1 Based on Prolyl Diaminopropionic Acid Scaffold 有权基于脯氨酰二氨基丙酸支架的整合素α2Beta1抑制剂公开(公告)号：US20100179119A1
公开(公告)日：2010-07-15
申请号：US12566162
申请日：2009-09-24
IPC分类号： A61K31/40 , C07D207/16 , C07D211/60 , C07D217/26 , C07D215/48 , C07D277/06 , C07D263/06 , A61K31/397 , A61K31/445 , A61K31/472 , A61K31/47 , A61K31/426 , A61K31/421 , A61P9/00 , A61P9/10 , A61P3/10 , A61P35/00 , A61P31/12
CPC分类号： C07D207/48 , A61K38/00 , C07D205/04 , C07D211/96 , C07D215/58 , C07D217/26 , C07D277/06 , C07K5/06165
摘要： Novel compounds inhibiting the integrin α2β1/GPIa-IIa receptor are disclosed. Also disclosed are pharmaceutical compositions containing the compounds, as well as methods of their therapeutic use. The compounds disclosed are useful, inter alia, as inhibitors of integrin α2β1/GPIa-IIa-mediated activity.
摘要翻译： 公开了抑制整联蛋白α2和bgr1 / GPIa-IIa受体的新型化合物。 还公开了含有这些化合物的药物组合物及其治疗用途的方法。 所公开的化合物尤其可用作整联蛋白α2和bgr1 / GPIa-IIa介导的活性的抑制剂。
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公开(公告)号：US20080176807A1
公开(公告)日：2008-07-24
申请号：US11980785
申请日：2007-10-31
申请人： William F. DeGrado , Gregory N. Tew , Michael L. Klein , Dahui Liu , Jing Yuan , Sungwook Choi
发明人： William F. DeGrado , Gregory N. Tew , Michael L. Klein , Dahui Liu , Jing Yuan , Sungwook Choi
IPC分类号： A61K38/07 , A61K38/05 , C07K5/10 , A61P31/04 , A61P31/12 , A01P1/00 , A61P31/10 , A01N37/44 , C07C233/64
CPC分类号： A61K31/17 , A61K31/16 , A61K31/165 , A61K31/495 , C07C233/64 , C07C323/42 , C07C323/44 , C08G18/3225 , C08G73/028 , C08L75/02
摘要： The present invention discloses methods of use of facially amphiphilic polymers and oligomers, including pharmaceutical uses of the polymers and oligomers as antimicrobial agents and antidotes for hemorrhagic complications associated with heparin therapy. The present invention also discloses novel facially amphiphilic polymers and oligomers and their compositions, including pharmaceutical compositions. The present invention further discloses the design and synthesis of facially amphiphilic polymers and oligomers.
摘要翻译： 本发明公开了使用表面两亲性聚合物和低聚物的方法，包括聚合物和低聚物作为抗微生物剂的药物用途和与肝素治疗相关的出血并发症的解毒剂。 本发明还公开了新颖的表面两亲聚合物和低聚物及其组合物，包括药物组合物。 本发明还公开了表面两亲聚合物和低聚物的设计和合成。
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公开(公告)号：US09241917B2
公开(公告)日：2016-01-26
申请号：US10801951
申请日：2004-03-17
申请人： William F. DeGrado , Gregory N. Tew , Michael L. Klein , Dahui Liu , Jing Yuan , Sungwook Choi
发明人： William F. DeGrado , Gregory N. Tew , Michael L. Klein , Dahui Liu , Jing Yuan , Sungwook Choi
IPC分类号： C08G18/00 , A61K31/16 , A61K31/165 , A61K31/495 , C07C233/64 , C07C323/42 , C07C323/44 , C08G18/32 , C08G73/02 , C08L75/02
CPC分类号： A61K31/17 , A61K31/16 , A61K31/165 , A61K31/495 , C07C233/64 , C07C323/42 , C07C323/44 , C08G18/3225 , C08G73/028 , C08L75/02
摘要： The present invention discloses methods of use of facially amphiphilic polymers and oligomers, including pharmaceutical uses of the polymers and oligomers as antimicrobial agents and antidotes for hemorrhagic complications associated with heparin therapy. The present invention also discloses novel facially amphiphilic polymers and oligomers and their compositions, including pharmaceutical compositions. The present invention further discloses the design and synthesis of facially amphiphilic polymers and oligomers.
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公开(公告)号：US08236800B2
公开(公告)日：2012-08-07
申请号：US11980785
申请日：2007-10-31
申请人： William F. DeGrado , Gregory N. Tew , Michael L. Klein , Dahui Liu , Jing Yuan , Sungwook Choi
发明人： William F. DeGrado , Gregory N. Tew , Michael L. Klein , Dahui Liu , Jing Yuan , Sungwook Choi
IPC分类号： A01N43/58 , A01N43/60 , A01N43/54 , A61K31/50 , A61K31/495 , C07D239/42 , C07D471/04 , C07D471/22 , C07D487/04
CPC分类号： A61K31/17 , A61K31/16 , A61K31/165 , A61K31/495 , C07C233/64 , C07C323/42 , C07C323/44 , C08G18/3225 , C08G73/028 , C08L75/02
摘要： The present invention discloses methods of use of facially amphiphilic polymers and oligomers, including pharmaceutical uses of the polymers and oligomers as antimicrobial agents and antidotes for hemorrhagic complications associated with heparin therapy. The present invention also discloses novel facially amphiphilic polymers and oligomers and their compositions, including pharmaceutical compositions. The present invention further discloses the design and synthesis of facially amphiphilic polymers and oligomers.
摘要翻译： 本发明公开了使用表面两亲性聚合物和低聚物的方法，包括聚合物和低聚物作为抗微生物剂的药物用途和与肝素治疗相关的出血并发症的解毒剂。 本发明还公开了新颖的表面两亲聚合物和低聚物及其组合物，包括药物组合物。 本发明还公开了表面两亲聚合物和低聚物的设计和合成。
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公开(公告)号：US20090233968A1
公开(公告)日：2009-09-17
申请号：US11916746
申请日：2006-06-07
IPC分类号： A61K31/445 , A61K31/425 , A61K31/40 , C07D211/22 , C07D277/00 , C07D207/00
CPC分类号： C07D207/48 , C07D211/96 , C07D277/06 , C07K5/06165
摘要： Novel compounds inhibiting the integrin α2β1/GPIa-IIa receptor are disclosed. Also disclosed are pharmaceutical compositions containing the compounds, as well as methods of their therapeutic use. The compounds disclosed are useful, inter alia, as inhibitors of integrin α2β1/GPIa-IIa-mediated activity.
摘要翻译： 公开了抑制整联蛋白α2beta1/ GPIa-IIa受体的新型化合物。 还公开了含有这些化合物的药物组合物及其治疗用途的方法。 所公开的化合物尤其可用作整联蛋白α2beta1/ GPIa-IIa介导活性的抑制剂。
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公开(公告)号：US20170190660A9
公开(公告)日：2017-07-06
申请号：US14252251
申请日：2014-04-14
申请人： Jeffery W. Kelly , Sungwook Choi
发明人： Jeffery W. Kelly , Sungwook Choi
IPC分类号： C07C327/26 , C07C205/43 , C07C69/94 , C07C237/30 , C07C39/21 , G01N33/74 , C07C65/19
CPC分类号： C07C327/26 , A61K31/136 , C07C39/21 , C07C65/19 , C07C69/94 , C07C205/43 , C07C229/64 , C07C237/30 , C07C245/08 , C09B23/14 , C09B23/145 , C09B23/146 , C09B23/148 , C09B29/0007 , C09B29/0014 , C09B29/0029 , C09B29/0048 , C09B29/0051 , C09B29/0055 , C09B29/0059 , C09B29/0066 , C09B29/0085 , C09B29/10 , C09B29/12 , G01N33/6896 , G01N33/74 , G01N2333/4709 , G01N2500/04
摘要： A family of covalent kinetic stabilizer compounds that selectively and covalently react with the prominent plasma protein transthyretin in preference to more than 4000 other human plasma proteins is disclosed. A contemplated compound corresponds in structure to Formula I, below, where the various substituents are defined within, and reacts chemoselectively with one or two of four Lys-15 ε-amino groups within the transthyretin tetramer. The crystal structure confirms the binding orientation of the compound substructure and the conjugating amide bond. A covalent transthyretin kinetic stabilizer exhibits superior amyloid inhibition potency, compared to a non-covalent counterpart, and inhibits cytotoxicity associated with amyloidogenesis.
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8.发明授权Inhibitors of integrin alpha2beta1 based on prolyl diaminopropionic acid scaffold 有权基于脯氨酰二氨基丙酸支架的整合素α2β1抑制剂公开(公告)号：US08987306B2
公开(公告)日：2015-03-24
申请号：US12566162
申请日：2009-09-24
IPC分类号： A01N43/40 , A61K31/445 , A01N43/78 , A61K31/425 , A01N43/36 , A61K31/40 , C07D211/22 , C07D277/00 , C07D207/48 , C07D205/04 , C07D211/96 , C07D215/58 , C07D217/26 , C07D277/06 , C07K5/078 , A61K38/00
CPC分类号： C07D207/48 , A61K38/00 , C07D205/04 , C07D211/96 , C07D215/58 , C07D217/26 , C07D277/06 , C07K5/06165
摘要： Novel compounds inhibiting the integrin α2β1/GPIa-IIa receptor are disclosed. Also disclosed are pharmaceutical compositions containing the compounds, as well as methods of their therapeutic use. The compounds disclosed are useful, inter alia, as inhibitors of integrin α2β1/GPIa-IIa-mediated activity.
摘要翻译： 公开了抑制整联蛋白α2和bgr1 / GPIa-IIa受体的新型化合物。 还公开了含有这些化合物的药物组合物及其治疗用途的方法。 所公开的化合物尤其可用作整联蛋白α2和bgr1 / GPIa-IIa介导的活性的抑制剂。
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公开(公告)号：US20130023561A1
公开(公告)日：2013-01-24
申请号：US13559065
申请日：2012-07-26
申请人： William F. DeGrado , Gregory N. Tew , Michael L. Klein , Dahui Liu , Jing Yuan , Sungwook Choi
发明人： William F. DeGrado , Gregory N. Tew , Michael L. Klein , Dahui Liu , Jing Yuan , Sungwook Choi
IPC分类号： A61K31/167 , A61K31/404 , A01N43/38 , A61K31/4545 , A01P1/00 , A61P31/04 , A61P31/10 , A61P31/12 , A61P31/00 , A01N37/24 , A01N43/40
CPC分类号： A61K31/17 , A61K31/16 , A61K31/165 , A61K31/495 , C07C233/64 , C07C323/42 , C07C323/44 , C08G18/3225 , C08G73/028 , C08L75/02
摘要： The present invention discloses methods of use of facially amphiphilic polymers and oligomers, including pharmaceutical uses of the polymers and oligomers as antimicrobial agents and antidotes for hemorrhagic complications associated with heparin therapy. The present invention also discloses novel facially amphiphilic polymers and oligomers and their compositions, including pharmaceutical compositions. The present invention further discloses the design and synthesis of facially amphiphilic polymers and oligomers.
摘要翻译： 本发明公开了使用表面两亲性聚合物和低聚物的方法，包括聚合物和低聚物作为抗微生物剂的药物用途和与肝素治疗相关的出血并发症的解毒剂。 本发明还公开了新颖的表面两亲聚合物和低聚物及其组合物，包括药物组合物。 本发明还公开了表面两亲聚合物和低聚物的设计和合成。
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公开(公告)号：US07910609B2
公开(公告)日：2011-03-22
申请号：US12237015
申请日：2008-09-24
申请人： William F. DeGrado , Seth E. Snyder , Meredith W. Miller , Sandeep Basra , Joel S. Bennett , Sungwook Choi
发明人： William F. DeGrado , Seth E. Snyder , Meredith W. Miller , Sandeep Basra , Joel S. Bennett , Sungwook Choi
IPC分类号： A01N43/00 , A61K31/397 , C07D277/00 , C07D205/00
CPC分类号： C07D207/48 , C07D211/96 , C07D277/06 , C07K5/06165
摘要： Novel compounds inhibiting the integrin α2β1/GPIa-IIa receptor are disclosed. Also disclosed are pharmaceutical compositions containing the compounds, as well as methods of their therapeutic use. The compounds disclosed are useful, inter alia, as inhibitors of integrin α2β1/GPIa-IIa-mediated activity.
摘要翻译： 公开了抑制整联蛋白α2和bgr1 / GPIa-IIa受体的新型化合物。 还公开了含有这些化合物的药物组合物及其治疗用途的方法。 所公开的化合物尤其可用作整联蛋白α2和bgr1 / GPIa-IIa介导的活性的抑制剂。
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