公开(公告)号：US20070155738A1

公开(公告)日：2007-07-05

申请号：US11602140

申请日：2006-11-20

Applicant: Christoph Steeneck ,  Christian Gege ,  Frank Richter ,  Heiko Kroth ,  Matthias Hochguertel ,  Michael Essers ,  Joshua Van Veldhuizen ,  Bert Nolte ,  Brian Gallagher ,  Tim Feuerstein ,  Matthias Schneider ,  Torsten Arndt ,  Hongbo Deng ,  Ralf Biesinger ,  Xinyuan Wu ,  Harald Bluhm ,  Irving Sucholeiki ,  Arthur Taveras

Inventor： Christoph Steeneck ,  Christian Gege ,  Frank Richter ,  Heiko Kroth ,  Matthias Hochguertel ,  Michael Essers ,  Joshua Van Veldhuizen ,  Bert Nolte ,  Brian Gallagher ,  Tim Feuerstein ,  Matthias Schneider ,  Torsten Arndt ,  Hongbo Deng ,  Ralf Biesinger ,  Xinyuan Wu ,  Harald Bluhm ,  Irving Sucholeiki ,  Arthur Taveras

IPC: A61K31/538 ,  A61K31/5377 ,  A61K31/519 ,  C07D491/04 ,  C07D487/04

CPC classification number: C07D487/04

Abstract: The present invention relates generally to amide group containing pharmaceutical agents, and in particular, to amide containing heterobicyclic metalloprotease inhibitor compounds. More particularly, the present invention provides a new class of heterobicyclic MMP-13 inhibiting and MMP-3 inhibiting compounds, that exhibit an increased potency in relation to currently known MMP-13 and MMP-3 inhibitors.

Abstract translation: 本发明一般涉及含酰胺基的药剂，特别涉及含酰胺的杂双环金属蛋白酶抑制剂化合物。 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，其与当前已知的MMP-13和MMP-3抑制剂相比具有增强的效力。

公开(公告)号：US20070155737A1

公开(公告)日：2007-07-05

申请号：US11602116

申请日：2006-11-20

Applicant: Brian Gallagher ,  Joshua Van Veldhuizen ,  Xinyuan Wu ,  Hongbo Deng ,  Irving Sucholeiki ,  Matthias Hochguertel ,  Harald Bluhm ,  Arthur Taveras

Inventor： Brian Gallagher ,  Joshua Van Veldhuizen ,  Xinyuan Wu ,  Hongbo Deng ,  Irving Sucholeiki ,  Matthias Hochguertel ,  Harald Bluhm ,  Arthur Taveras

IPC: A61K31/5377 ,  C07D491/04 ,  C07D487/04 ,  A61K31/538 ,  A61K31/519

CPC classification number: C07D487/04

Abstract: The present invention relates generally to amide group containing pharmaceutical agents, and in particular, to amide containing heterobicyclic metalloprotease inhibitor compounds. More particularly, the present invention provides a new class of heterobicyclic ADAMTS-4 inhibiting compounds.

Abstract translation: 本发明一般涉及含酰胺基的药物，尤其涉及含酰胺的杂双环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型的异双环ADAMTS-4抑制化合物。

公开(公告)号：US20060293345A1

公开(公告)日：2006-12-28

申请号：US11440087

申请日：2006-05-22

Applicant: Christoph Steeneck ,  Christian Gege ,  Frank Richter ,  Matthias Hochguertel ,  Tim Feuerstein ,  Harald Bluhm ,  Irving Sucholeiki ,  Jurgen Boer ,  Xinyuan Wu ,  Matthias Schneider ,  Bert Nolte ,  Brian Gallagher ,  Joshua Van Veldhuizen ,  Hongbo Dong ,  Michael Essers ,  Heiko Kroth ,  Andrew Kiely ,  Timothy Powers ,  Arthur Taveras

Inventor： Christoph Steeneck ,  Christian Gege ,  Frank Richter ,  Matthias Hochguertel ,  Tim Feuerstein ,  Harald Bluhm ,  Irving Sucholeiki ,  Jurgen Boer ,  Xinyuan Wu ,  Matthias Schneider ,  Bert Nolte ,  Brian Gallagher ,  Joshua Van Veldhuizen ,  Hongbo Dong ,  Michael Essers ,  Heiko Kroth ,  Andrew Kiely ,  Timothy Powers ,  Arthur Taveras

IPC: A61K31/519 ,  C07D491/04 ,  C07D487/04

CPC classification number: C07D487/04

Abstract: The present invention relates generally to amide group containing pharmaceutical agents, and in particular, to amide containing heterobicyclic metalloprotease inhibitor compounds. More particularly, the present invention provides a new class of heterobicyclic MMP-13 inhibiting compounds, that exhibit an increased potency in relation to currently known MMP-13 inhibitors.

Abstract translation: 本发明一般涉及含酰胺基的药剂，特别涉及含酰胺的杂双环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型的杂双环MMP-13抑制化合物，其表现出与目前已知的MMP-13抑制剂有关的效力。

公开(公告)号：US06277332B1

公开(公告)日：2001-08-21

申请号：US09049245

申请日：1998-03-27

Applicant: Irving Sucholeiki

Inventor： Irving Sucholeiki

IPC: B01F1102

CPC classification number: B01F11/0283 ,  B01F13/0809 ,  B01J19/0046 ,  B01J2219/00283 ,  B01J2219/00308 ,  B01J2219/00328 ,  B01J2219/00351 ,  B01J2219/00414 ,  B01J2219/00454 ,  B01J2219/00459 ,  B01J2219/00486 ,  B01J2219/00495 ,  B01J2219/005 ,  B01J2219/00585 ,  B01J2219/0059 ,  B01J2219/00596 ,  B01J2219/00686 ,  B01J2219/00691 ,  B01J2219/0072 ,  B01J2219/00725 ,  B06B3/02 ,  C07K1/042 ,  C07K1/045 ,  C40B40/10 ,  C40B50/14 ,  C40B60/14 ,  Y10T436/113332

Abstract: The inventive apparatus is comprised of a means for producing cavitation in a complex reaction mixture to enhance the yield of the selected reaction product, a means for controlling the temperature of the complex reaction mixture, especially during cavitation, and a means for affecting magnetic separation of paramagnetic beads to which the selected reaction product is attached from the complex reaction mixture. In one embodiment, the compound(s) or molecule(s) is synthesized in situ, and isolated using the inventive apparatus. The apparatus finds use in the fields of solid phase organic synthesis, and for isolation and purification of a selected compound(s) or molecule (s), especially where automation is desired.

Abstract translation: 本发明的装置包括用于在复合反应混合物中产生空化以提高所选择的反应产物的产率的装置，特别是在空化期间控制复合反应混合物的温度的手段和用于影响磁分离的装置 选择的反应产物从复合反应混合物连接到其上的顺磁珠。 在一个实施方案中，化合物或分子原位合成，并使用本发明的装置分离。 该装置用于固相有机合成领域，并用于选择的化合物或分子的分离和纯化，特别是在需要自动化的情况下。

公开(公告)号：US5835329A

公开(公告)日：1998-11-10

申请号：US462198

申请日：1995-06-05

Applicant: Irving Sucholeiki

Inventor： Irving Sucholeiki

IPC: B03C1/035 ,  H01H47/22

CPC classification number: B03C1/035

Abstract: This invention provides a method and apparatus for agitating magnetic particles, suspended in a solvent using an alternating magnetic field gradient. The apparatus has a housing chamber capable of holding one or more vials containing suspended paramagnetic particles, one or more magnetic field generating devices surrounding the housing chamber and a controller device for controlling the length of time and position of the magnetic field generated.

Abstract translation: 本发明提供一种使用交变磁场梯度搅拌悬浮在溶剂中的磁性颗粒的方法和装置。 该装置具有能够容纳一个或多个包含悬浮的顺磁性颗粒的小瓶的容纳室，围绕容纳室的一个或多个磁场产生装置和用于控制产生的磁场的时间和位置的长度的控制器装置。

公开(公告)号：US5693720A

公开(公告)日：1997-12-02

申请号：US458325

申请日：1995-06-02

Applicant: Irving Sucholeiki

Inventor： Irving Sucholeiki

IPC: C07C323/56 ,  C08F8/34

CPC classification number: C07C323/56

Abstract: A method for photochemical cleavage of carbon-sulfur bonds in conjunction with solid-phase synthesis utilizing a deoxygenated solvent and light to cleave the carbon-sulfur bond from a heterogeneous support. Also disclosed are compounds for use with said photochemical cleavage and methods of preparing them.

Abstract translation: 结合使用脱氧溶剂和光从固相合成裂解碳 - 硫键从不均匀载体切割碳 - 硫键的方法。 还公开了用于所述光化学切割的化合物及其制备方法。

公开(公告)号：US20110230452A1

公开(公告)日：2011-09-22

申请号：US12924214

申请日：2010-09-23

Applicant: Irving Sucholeiki

Inventor： Irving Sucholeiki

IPC: A61K31/65 ,  C07D309/08 ,  A61K31/351 ,  C07C235/84 ,  C07C237/44 ,  C07D207/337 ,  A61K31/40 ,  C07D209/18 ,  A61K31/404 ,  C07D213/79 ,  A61K31/44 ,  C07D307/85 ,  A61K31/343 ,  C07D235/24 ,  A61K31/4184 ,  C07D235/22 ,  A61K31/4035 ,  C07D233/76 ,  A61K31/4164 ,  C07C321/30 ,  A61K31/192 ,  A61P25/30 ,  A61P19/00 ,  A61P25/04 ,  A61P31/12 ,  A61P9/00 ,  A61P3/00 ,  A61P25/28

CPC classification number: 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

Abstract: 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.

Abstract translation: 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。

公开(公告)号：US20100249102A1

公开(公告)日：2010-09-30

申请号：US12755326

申请日：2010-04-06

Applicant: Christian Gege ,  Carine Chevrier ,  Matthias Schneider ,  Harald Bluhm ,  Matthias Hochgürtel ,  Hongbo Deng ,  Brian M. Gallagher, JR. ,  Irving Sucholeiki ,  Arthur Taveras

Inventor： Christian Gege ,  Carine Chevrier ,  Matthias Schneider ,  Harald Bluhm ,  Matthias Hochgürtel ,  Hongbo Deng ,  Brian M. Gallagher, JR. ,  Irving Sucholeiki ,  Arthur Taveras

IPC: A61K31/519 ,  A61K31/55 ,  A61K31/538 ,  C07D495/14 ,  C07D495/04 ,  C07D495/22 ,  A61P9/10 ,  A61P19/02 ,  A61P29/00

CPC classification number: C07D495/04 ,  C07D239/88 ,  C07D401/12 ,  C07D413/12 ,  C07D471/04 ,  C07D487/04 ,  C07D491/04 ,  C07D495/14 ,  C07D495/22 ,  C07D498/04 ,  C07D513/04

Abstract: 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.

公开(公告)号：US20080176870A1

公开(公告)日：2008-07-24

申请号：US11986622

申请日：2007-11-20

Applicant: Bert Nolte ,  Irving Sucholeiki ,  Tim Feuerstein ,  Brian M. Gallagher ,  Xinyuan Wu ,  Christoph Steeneck ,  Christian Gege ,  Hongbo Deng ,  Joshua Van Veldhuizen ,  Arthur Taveras

Inventor： Bert Nolte ,  Irving Sucholeiki ,  Tim Feuerstein ,  Brian M. Gallagher ,  Xinyuan Wu ,  Christoph Steeneck ,  Christian Gege ,  Hongbo Deng ,  Joshua Van Veldhuizen ,  Arthur Taveras

IPC: A61K31/495 ,  C07D487/04 ,  A61P19/02 ,  A61P29/00 ,  A61P9/10

CPC classification number: C07D487/04

Abstract: The present invention relates generally to heterobicyclic containing pharmaceutical agents, and in particular, to heterobicyclic metalloprotease inhibitor compounds. More particularly, the present invention provides a new class of heterobicyclic metalloprotease inhibiting compounds that exhibit an increased potency in relation to currently known metalloprotease inhibitors.

Abstract translation: 本发明一般涉及含杂环的药物，特别是涉及杂双环金属蛋白酶抑制剂化合物。 更具体地，本发明提供了一类新型的杂双环金属蛋白酶抑制化合物，其与当前已知的金属蛋白酶抑制剂相比表现出增加的效力。

公开(公告)号：US06682660B2

公开(公告)日：2004-01-27

申请号：US10143903

申请日：2002-05-14

Applicant: Irving Sucholeiki ,  Nak-Ho Sung ,  Jun Young Lee

Inventor： Irving Sucholeiki ,  Nak-Ho Sung ,  Jun Young Lee

IPC: H01F100

CPC classification number: C08K3/22 ,  Y10T428/2991 ,  Y10T428/2998

Abstract: 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.

Abstract translation: 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。