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1. 发明授权

US06682660B2 Ultrasonically generated paramagnetic polymer particles 失效
标题翻译：超声波生成顺磁聚合物颗粒
公开(公告)号：US06682660B2
公开(公告)日：2004-01-27
申请号：US10143903
申请日：2002-05-14
申请人： Irving Sucholeiki , Nak-Ho Sung , Jun Young Lee
发明人： Irving Sucholeiki , Nak-Ho Sung , Jun Young Lee
IPC分类号： H01F100
CPC分类号： C08K3/22 , Y10T428/2991 , Y10T428/2998
摘要： A composite paramagnetic particle and method of making are provided. In one aspect of the invention, a particle comprising a multitude of submicron polymer bead aggregates covalently cross-linked to each other to form larger diameter particles is presented. Distributed throughout the composite paramagnetic particle are vacuous cavities. Each submicron polymer bead has distributed throughout its interior and surface submicron magnetite crystals. In another aspect of the invention, composite particles are made using high energy ultrasound during polymerization of one or more vinyl monomers. In one embodiment, high energy ultrasound is used during an emulsification step and during the early stages of the polymerization process to produce micron sized composite paramagnetic particles. The particles according to the invention exhibit a high percent magnetite incorporation and water and organic solvent stability.
摘要翻译：提供复合顺磁性粒子及其制造方法。在本发明的一个方面，提供了包含彼此共价交联以形成更大直径的颗粒的大量亚微米聚合物珠聚集体的颗粒。分布在整个复合顺磁颗粒中的是空泡。每个亚微米聚合物珠分布在其内部和表面亚微米磁铁矿晶体。在本发明的另一方面，在一种或多种乙烯基单体的聚合过程中，使用高能超声波制备复合颗粒。在一个实施方案中，在乳化步骤期间和在聚合过程的早期阶段使用高能超声波以产生微米级的复合顺磁性颗粒。根据本发明的颗粒表现出高百分比的磁铁矿掺入和水和有机溶剂的稳定性。

2. 发明授权

US06423410B1 Ultrasonically generated paramagnetic polymer particles 失效
标题翻译：超声波生成顺磁聚合物颗粒
公开(公告)号：US06423410B1
公开(公告)日：2002-07-23
申请号：US09365506
申请日：1999-08-02
申请人： Irving Sucholeiki , Nak-Ho Sung , Jun Young Lee
发明人： Irving Sucholeiki , Nak-Ho Sung , Jun Young Lee
IPC分类号： B32B516
CPC分类号： C08K3/22 , Y10T428/2991 , Y10T428/2998
摘要： A composite paramagnetic particle and method of making are provided. In one aspect of the invention, a particle comprising a multitude of submicron polymer bead aggregates covalently cross-linked to each other to form larger diameter particles is presented. Distributed throughout the composite paramagnetic particle are vacuous cavities. Each submicron polymer bead has distributed throughout its interior and surface submicron magnetite crystals. In another aspect of the invention, composite particles are made using high energy ultrasound during polymerization of one or more vinyl monomers. In one embodiment, high energy ultrasound is used during an emulsification step and during the early stages of the polymerization process to produce micron sized composite paramagnetic particles. The particles according to the invention exhibit a high percent magnetite incorporation and water and organic solvent stability.
摘要翻译：提供复合顺磁性粒子及其制造方法。在本发明的一个方面，提供了包含彼此共价交联以形成更大直径的颗粒的大量亚微米聚合物珠聚集体的颗粒。分布在整个复合顺磁颗粒中的是空泡。每个亚微米聚合物珠分布在其内部和表面亚微米磁铁矿晶体。在本发明的另一方面，在一种或多种乙烯基单体的聚合过程中，使用高能超声波制备复合颗粒。在一个实施方案中，在乳化步骤期间和在聚合过程的早期阶段使用高能超声波以产生微米级的复合顺磁性颗粒。根据本发明的颗粒表现出高百分比的磁铁矿掺入和水和有机溶剂的稳定性。

3. 发明授权

US08765953B2 Compounds and methods for the treatment of pain and other diseases 有权
标题翻译：用于治疗疼痛和其他疾病的化合物和方法
公开(公告)号：US08765953B2
公开(公告)日：2014-07-01
申请号：US13141384
申请日：2009-12-21
申请人： Irving Sucholeiki
发明人： Irving Sucholeiki
IPC分类号： C07D221/02 , C07D209/04 , C07D209/20
CPC分类号： C07D409/12 , A61K31/381 , A61K31/404 , Y02A50/465
摘要： The present invention relates generally to alkyne containing pharmaceutical agents, and in particular, to phenylethynyl-thiophene based metalloprotease inhibitor compounds. More particularly, the present invention provides a new class of MMP inhibiting compounds that exhibit increased potency, metabolic stability and/or reduced toxicity in relation to currently known MMP inhibitors for the treatment of pain and other diseases such as cancer. Additionally, the present invention relates to methods for treating pain in a patient comprising administering to the patient a pain-reducing effective amount of a present compound.
摘要翻译：本发明一般涉及含有炔烃的药剂，特别是苯基乙炔基 - 噻吩基金属蛋白酶抑制剂化合物。更具体地，本发明提供了一类新的MMP抑制化合物，其相对于目前已知的用于治疗疼痛和其它疾病如癌症的MMP抑制剂表现出增加的效力，代谢稳定性和/或降低的毒性。另外，本发明涉及用于治疗患者疼痛的方法，包括向患者施用减少疼痛的有效量的本发明化合物。

4. 发明授权

US08530453B2 Compounds and methods for the treatment of pain and other diseases 有权
标题翻译：用于治疗疼痛和其他疾病的化合物和方法
公开(公告)号：US08530453B2
公开(公告)日：2013-09-10
申请号：US12924214
申请日：2010-09-23
申请人： Irving Sucholeiki
发明人： Irving Sucholeiki
IPC分类号： A01N37/18 , A01N43/40 , A61K31/65 , A61K31/44 , C07D209/00
CPC分类号： A61K31/65 , A61K31/343 , A61K31/38 , A61K31/4035 , A61K31/405 , A61K31/4166 , A61K31/4184 , A61K31/45 , C07C235/82 , C07C237/26 , C07C259/14 , C07C317/44 , C07C323/52 , C07D207/337 , C07D209/18 , C07D209/48 , C07D213/79 , C07D233/76 , C07D235/22 , C07D235/24 , C07D307/85 , C07D309/08
摘要： The present invention relates generally to pharmaceutical agents, and in particular, to metalloprotease inhibitor compounds. More particularly, the present invention provides a new class of dual acting MMP-2 and MMP-9 inhibiting compounds that exhibit increased potency, metabolic stability and/or reduced toxicity in relation to currently known MMP-2 and MMP-9 inhibitors for the treatment of pain and other diseases. Additionally, the present invention relates to methods for treating pain, addiction and/or withdrawal symptoms in a patient comprising administering to the patient a pain-reducing effective amount of a present compound.
摘要翻译：本发明一般涉及药剂，尤其涉及金属蛋白酶抑制剂化合物。更具体地说，本发明提供了一类新的双作用MMP-2和MMP-9抑制化合物，其相对于目前已知的用于治疗的MMP-2和MMP-9抑制剂表现出增加的效力，代谢稳定性和/或降低的毒性的疼痛等疾病。另外，本发明涉及用于治疗患者的疼痛，成瘾和/或戒断症状的方法，包括向患者施用减少疼痛的有效量的本发明化合物。

5. 发明授权

US07795245B2 Heterobicyclic metalloprotease inhibitors 有权
标题翻译：异双环金属蛋白酶抑制剂
公开(公告)号：US07795245B2
公开(公告)日：2010-09-14
申请号：US12001043
申请日：2007-12-07
申请人： Christoph Steeneck , Christian Gege , Frank Richter , Heiko Kroth , Matthias Hochgurtel , Michael Essors , Joshua Van Veldhuizen , Bert Nolte , Brian M. Gallagher, Jr. , Tim Feuerstein , Matthias Schneider , Torsten Arndt , Hongbo Deng , Ralf Biesinger , Xinyuan Wu , Harald Bluhm , Irving Sucholeiki , Arthur G. Taveras
发明人： Christoph Steeneck , Christian Gege , Frank Richter , Heiko Kroth , Matthias Hochgurtel , Michael Essors , Joshua Van Veldhuizen , Bert Nolte , Brian M. Gallagher, Jr. , Tim Feuerstein , Matthias Schneider , Torsten Arndt , Hongbo Deng , Ralf Biesinger , Xinyuan Wu , Harald Bluhm , Irving Sucholeiki , Arthur G. Taveras
IPC分类号： A61K31/397 , A61K31/519 , A61K31/535 , A01N43/90 , C07D487/00 , C07D413/00
CPC分类号： C07D487/04
摘要： The present invention relates generally to amide group containing pharmaceutical agents, and in particular, to amide containing heterobicyclic metalloprotease inhibitor compounds having the following formulas: wherein R1, R2, R3, and R4 are as defined in the specification. More particularly, the present invention provides a new class of heterobicyclic MMP-13 inhibiting and MMP-3 inhibiting compounds amide containing heterobicyclic compounds, that exhibit an increased potency in relation to currently known MMP-13 and MMP-3 inhibitors.
摘要翻译：本发明一般涉及含酰胺基的药剂，特别涉及具有下式的含酰胺的杂双环金属蛋白酶抑制剂化合物：其中R1，R2，R3和R4如说明书中所定义。更具体地，本发明提供了一类新型的杂双环MMP-13抑制和MMP-3抑制化合物，其含有杂双环化合物的酰胺，其与当前已知的MMP-13和MMP-3抑制剂相比具有增强的效力。

6. 发明申请

US20080207607A1 Heterotricyclic metalloprotease inhibitors 失效
标题翻译：异环金属蛋白酶抑制剂
公开(公告)号：US20080207607A1
公开(公告)日：2008-08-28
申请号：US11986603
申请日：2007-11-20
申请人： Christian Gege , Carine Chevrier , Matthias Schneider , Harald Bluhm , Matthias Hochgurtel , Hongbo Deng , Brian M. Gallagher , Irving Sucholeiki , Arthur Taveras
发明人： Christian Gege , Carine Chevrier , Matthias Schneider , Harald Bluhm , Matthias Hochgurtel , Hongbo Deng , Brian M. Gallagher , Irving Sucholeiki , Arthur Taveras
IPC分类号： A61K31/538 , C07D265/36 , C07D217/00 , A61K31/4725 , A61K31/541 , A61P29/00 , A61K31/519 , C07D239/00 , C07D417/14
CPC分类号： C07D495/04 , C07D239/88 , C07D401/12 , C07D413/12 , C07D471/04 , C07D487/04 , C07D491/04 , C07D495/14 , C07D495/22 , C07D498/04 , C07D513/04
摘要： The present invention relates generally to azatriocyclic containing pharmaceutical agents, and in particular, to azatricyclic metalloprotease inhibiting compounds. More particularly, the present invention provides a new class of azatricyclic MMP-3, MMP-8 and/or MMP-13 inhibiting compounds, that exhibit an increased potency and selectivity in relation to currently known MMP-13, MMP-8 and MMP-3 inhibitors.
摘要翻译：本发明一般涉及含有三氮杂环的药物，尤其涉及氮杂三环金属蛋白酶抑制化合物。更具体地说，本发明提供了一类新型的azatricyclic MMP-3，MMP-8和/或MMP-13抑制化合物，其与当前已知的MMP-13，MMP-8和MMP- 3抑制剂。

7. 发明授权

US5750412A Paramagnetic scintillation particles and assay 失效
标题翻译：顺磁闪烁颗粒和测定
公开(公告)号：US5750412A
公开(公告)日：1998-05-12
申请号：US699796
申请日：1996-08-19
申请人： Irving Sucholeiki
发明人： Irving Sucholeiki
IPC分类号： G01N33/543 , G01N33/58 , G01N33/60 , G01N33/553 , G01N33/542 , G01N33/546
CPC分类号： G01N33/58 , G01N33/54333 , G01N33/60 , Y10S436/808
摘要： An immunoscintillating composition and method of radioimmunoassay is disclosed whereby polymer coated paramagnetic particles and binding agent such as an antibody are associated by chemical or physical means to provide solid scintillating immunoadsorbent particles which are paramagnetic. These particles are capable of selectively binding or retaining radioactive or labeled antigens or ligands and transmitting radioactive energy to a phosphor or photon emitting substance that is bound by chemical or physical means to the particles. Upon binding of the antigens or ligands to the surface of the particles the particles are separated from the unbound components in solution by application of a magnetic field. The luminescence emitted by the phosphor which is attached to the magnetically separated particles is measured by a scintillator counter and is directly proportional to the radioactive energy released by the labeled antigen bound to the antibody. Upon completion of the measurement the paramagnetic particles can be magnetically separated and the labeled antigens or ligands removed for further analysis and the particles recycled for use in other assays.
摘要翻译：公开了免疫组织化学和放射免疫测定方法，其中聚合物涂覆的顺磁性颗粒和结合剂如抗体通过化学或物理手段相关联，以提供顺磁性的固体闪烁免疫吸附剂颗粒。这些颗粒能够选择性地结合或保留放射性或标记的抗原或配体，并将放射能量传输到通过化学或物理手段结合到颗粒的磷光体或光子发射物质。当抗原或配体与颗粒的表面结合时，颗粒通过施加磁场与溶液中未结合的组分分离。通过闪烁计数器测量由附着在磁分离的颗粒上的荧光体发射的发光，并与与抗体结合的标记抗原释放的放射性能量成正比。测量完成后，顺磁性颗粒可被磁性分离，标记的抗原或配体被去除用于进一步分析，再循环使用的颗粒用于其他测定。

8. 发明申请

US20150274702A1 MATRIX METALLOPROTEINASE INHIBITORS AND METHODS FOR THE TREATMENT OF PAIN AND OTHER DISEASES 有权
标题翻译：基质金属蛋白酶抑制剂及治疗疼痛及其他疾病的方法
公开(公告)号：US20150274702A1
公开(公告)日：2015-10-01
申请号：US14433692
申请日：2012-11-27
申请人： Irving SUCHOLEIKI , AQUILUS PHARMACEUTICALS, INC.
发明人： Irving Sucholeiki
IPC分类号： C07D403/12 , A61K45/06 , C07D413/12 , A61K31/505 , C07D413/14 , A61K31/538 , A61K31/506 , C07D239/28
CPC分类号： C07D403/12 , A61K31/505 , A61K31/506 , A61K31/538 , A61K45/06 , C07D239/28 , C07D413/12 , C07D413/14
摘要： The present invention relates generally to bis-amide containing MMP inhibiting compounds, and more particularly to selectively deuterated bis-amide MMP-13 inhibiting compounds that exhibit increased stability or potency in relation to currently known MMP-13 inhibitors. Additionally, the present invention relates to methods for treating pain and inflammation in a patient comprising administering to the patient a pain-reducing effective amount of a present compound.
摘要翻译：本发明一般涉及含有二酰胺的MMP抑制化合物，更具体地说，涉及与当前已知的MMP-13抑制剂相比显示增加的稳定性或效力的选择性氘代双酰胺MMP-13抑制化合物。另外，本发明涉及用于治疗患者的疼痛和炎症的方法，包括向患者施用减少疼痛的有效量的本发明化合物。

9. 发明授权

US07749996B2 Heterotricyclic metalloprotease inhibitors 失效
标题翻译：异环金属蛋白酶抑制剂
公开(公告)号：US07749996B2
公开(公告)日：2010-07-06
申请号：US11986603
申请日：2007-11-20
申请人： Christian Gege , Carine Chevrier , Matthias Schneider , Harald Bluhm , Matthias Hochgürtel , Hongbo Deng , Brian M. Gallagher, Jr. , Irving Sucholeiki , Arthur Taveras
发明人： Christian Gege , Carine Chevrier , Matthias Schneider , Harald Bluhm , Matthias Hochgürtel , Hongbo Deng , Brian M. Gallagher, Jr. , Irving Sucholeiki , Arthur Taveras
IPC分类号： A61K31/535 , C07D413/00
CPC分类号： C07D495/04 , C07D239/88 , C07D401/12 , C07D413/12 , C07D471/04 , C07D487/04 , C07D491/04 , C07D495/14 , C07D495/22 , C07D498/04 , C07D513/04
摘要： The present invention relates generally to azatriocyclic containing pharmaceutical agents, and in particular, to azatricyclic metalloprotease inhibiting compounds. More particularly, the present invention provides a new class of azatricyclic MMP-3, MMP-8 and/or MMP-13 inhibiting compounds, that exhibit an increased potency and selectivity in relation to currently known MMP-13, MMP-8 and MMP-3 inhibitors.
摘要翻译：本发明一般涉及含有三氮杂环的药物，尤其涉及氮杂三环金属蛋白酶抑制化合物。更具体地说，本发明提供了一类新型的azatricyclic MMP-3，MMP-8和/或MMP-13抑制化合物，其与当前已知的MMP-13，MMP-8和MMP- 3抑制剂。

10. 发明授权

US07713966B2 Heterobicyclic metalloprotease inhibitors 失效
标题翻译：异双环金属蛋白酶抑制剂
公开(公告)号：US07713966B2
公开(公告)日：2010-05-11
申请号：US11986626
申请日：2007-11-20
申请人： Christian Gege , Matthias Schneider , Carine Chevrier , Hongbo Deng , Irving Sucholeiki , Brian M. Gallagher, Jr. , Michael Bosies , Christoph Steeneck , Xinyuan Wu , Matthias Hochgürtel , Bert Nolte , Arthur Taveras
发明人： Christian Gege , Matthias Schneider , Carine Chevrier , Hongbo Deng , Irving Sucholeiki , Brian M. Gallagher, Jr. , Michael Bosies , Christoph Steeneck , Xinyuan Wu , Matthias Hochgürtel , Bert Nolte , Arthur Taveras
IPC分类号： A61K31/535 , C07D265/12 , C07D413/00 , A01N43/00 , A01N43/46 , A61K31/553 , A61K31/554 , A61K31/55 , A61K31/54 , C07D498/00 , C07D291/08 , C07D281/02 , C07D267/02 , C07D223/16 , C07D513/00
CPC分类号： C07D495/04 , C07D239/88 , C07D401/12 , C07D413/12 , C07D471/04 , C07D487/04 , C07D491/04 , C07D495/14 , C07D495/22 , C07D498/04 , C07D513/04
摘要： The present invention relates generally to azabicyclic containing pharmaceutical agents, and in particular, to azabicyclic metalloprotease inhibiting compounds. More particularly, the present invention provides a new class of azabicyclic MMP-3, MMP-8 and/or MMP-13 inhibiting compounds, which exhibit an increased potency and selectivity in relation to currently known MMP-13, MMP-8 and MMP-3 inhibitors.
摘要翻译：本发明一般涉及含有氮杂双环的药物，特别涉及氮杂双环金属蛋白酶抑制化合物。更具体地说，本发明提供了一类新的氮杂双环MMP-3，MMP-8和/或MMP-13抑制化合物，其相对于目前已知的MMP-13，MMP-8和MMP- 3抑制剂。

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