公开(公告)号：US20130267571A1

公开(公告)日：2013-10-10

申请号：US13822826

申请日：2011-09-14

申请人： Mark A. Reed ,  Donald Weaver ,  Shengguo Sun ,  Alexander McLellan ,  Erhu Lu

发明人： Mark A. Reed ,  Donald Weaver ,  Shengguo Sun ,  Alexander McLellan ,  Erhu Lu

IPC分类号： C07C233/09 ,  C07C43/166 ,  C07C57/03 ,  C07D257/04 ,  C07C233/65 ,  C07C233/05 ,  C07C233/07 ,  C07C235/60 ,  C07C43/15 ,  C07C211/21

CPC分类号： C07C233/09 ,  A61K31/045 ,  A61K31/08 ,  A61K31/10 ,  A61K31/12 ,  A61K31/13 ,  A61K31/16 ,  A61K31/18 ,  A61K31/201 ,  A61K31/41 ,  C07C43/15 ,  C07C43/166 ,  C07C57/03 ,  C07C211/21 ,  C07C233/05 ,  C07C233/07 ,  C07C233/65 ,  C07C235/60 ,  C07D257/04

摘要： The present application provides a terpene analogue of Formula (I) or a pharmaceutically acceptable isomer, salt or ester thereof, and methods and uses thereof for treating neurological conditions such as pain in general and neuropathic pain. These terpene analogues can also be used to treat other electrical disorders in the central and peripheral nervous system. Also provided are methods of synthesizing the terpene analogues of Formula I.

摘要翻译： 本申请提供了式（I）的萜烯类似物或其药学上可接受的异构体，盐或酯，以及其用于治疗神经学病症如一般疼痛和神经性疼痛的方法和用途。 这些萜烯类似物也可用于治疗中枢和外周神经系统中的其他电疗障碍。 还提供了合成式I的萜烯类似物的方法。

公开(公告)号：US20070265334A1

公开(公告)日：2007-11-15

申请号：US11707758

申请日：2007-02-16

申请人： Robert Kisilevsky ,  Walter Szarek ,  Donald Weaver

发明人： Robert Kisilevsky ,  Walter Szarek ,  Donald Weaver

IPC分类号： A61K31/095 ,  A61K31/34 ,  A61P3/00 ,  C07C317/04 ,  C07D307/00

CPC分类号： C07H15/04 ,  A61K31/095 ,  A61K31/185 ,  A61K31/255 ,  A61K31/34 ,  A61K31/41 ,  A61K31/70 ,  A61K47/51 ,  A61K47/549 ,  A61K47/55 ,  A61K47/555 ,  A61K47/58 ,  C07C305/10 ,  C07C309/05 ,  C07D491/04 ,  C07H11/00

摘要： Therapeutic compounds and methods for inhibiting amyloid deposition in a subject, whatever its clinical setting, are described. Amyloid deposition is inhibited by the administration to a subject of an effective amount of a therapeutic compound comprising an anionic group and a carrier molecule, or a pharmaceutically acceptable salt thereof, such that an interaction between an amyloidogenic protein and a basement membrane constituent is inhibited. Preferred anionic groups are sulfonates and sulfates. Preferred carrier molecules include carbohydrates, polymers, peptides, peptide derivatives, aliphatic groups, alicyclic groups, heterocyclic groups, aromatic groups and combinations thereof.

摘要翻译： 描述了用于抑制受试者中淀粉样蛋白沉积的治疗化合物和方法，无论其临床情况如何。 通过给予受试者有效量的包含阴离子基团和载体分子或其药学上可接受的盐的治疗化合物或其淀粉样蛋白形成蛋白质与基底膜成分之间的相互作用被抑制来抑制淀粉样蛋白沉积。 优选的阴离子基团是磺酸盐和硫酸盐。 优选的载体分子包括碳水化合物，聚合物，肽，肽衍生物，脂族基团，脂环族基团，杂环基团，芳族基团及其组合。

公开(公告)号：US5972328A

公开(公告)日：1999-10-26

申请号：US463548

申请日：1995-06-05

申请人： Robert Kisilevsky ,  Walter Szarek ,  Donald Weaver

发明人： Robert Kisilevsky ,  Walter Szarek ,  Donald Weaver

IPC分类号： A61K31/185 ,  A61K31/255 ,  A61K31/41 ,  A61K31/70 ,  A61K31/737 ,  A61K31/795 ,  A61K47/48 ,  A61L33/08 ,  C07H11/00 ,  C07H15/04 ,  A61K31/74 ,  A61K31/785 ,  A61K47/32

CPC分类号： A61K31/185 ,  A61K31/255 ,  A61K31/41 ,  A61K31/70 ,  A61K31/737 ,  A61K31/795 ,  A61K47/48007 ,  A61K47/48023 ,  A61K47/48092 ,  A61K47/481 ,  A61K47/4813 ,  A61K47/48176 ,  A61L33/08 ,  C07H11/00 ,  C07H15/04

摘要： Therapeutic compounds and methods for inhibiting amyloid deposition in a subject, whatever its clinical setting, are described. Amyloid deposition is inhibited by the administration to a subject of an effective amount of a therapeutic compound comprising an anionic group and a carrier molecule, or a pharmaceutically acceptable salt thereof, such that an interaction between an amyloidogenic protein and a basement membrane constituent is inhibited. Preferred anionic groups are sulfonates and sulfates. Preferred carrier molecules include carbohydrates, polymers, peptides, peptide derivatives, aliphatic groups, alicyclic groups, heterocyclic groups, aromatic groups and combinations thereof.

公开(公告)号：US08835476B2

公开(公告)日：2014-09-16

申请号：US11909636

申请日：2006-03-06

申请人： Fan Wu ,  Donald Weaver ,  Chris Barden ,  Christopher McMaster ,  David Byers ,  Annette Henneberry ,  Fuqiang Ban

发明人： Fan Wu ,  Donald Weaver ,  Chris Barden ,  Christopher McMaster ,  David Byers ,  Annette Henneberry ,  Fuqiang Ban

IPC分类号： A01N43/64 ,  A61K31/41 ,  A01N43/06 ,  A61K31/38 ,  C07D257/04 ,  C07D257/10 ,  C07D403/00 ,  C07D487/00 ,  C07D333/02 ,  C07D409/00 ,  C12Q1/18 ,  C07D495/14 ,  C07D409/04 ,  C07D409/14

CPC分类号： C12Q1/18 ,  A61K31/41 ,  C07D409/04 ,  C07D409/14 ,  C07D495/14 ,  Y02A50/473 ,  Y02A50/475 ,  Y02A50/478 ,  Y02A50/481

摘要： The synthesis and activity of novel LpxA inhibitors is described, these inhibitors present antibacterial activity. The compounds were designed based on a receptor model developed using the crystal structure of LpxA and are arranged to have a favorable binding interaction at the active site of the enzyme. In particular, the compounds present the following formula (I) where V, W, X, Y and Z can be independently C, S, N or O and P1, P2 and P3 are ligands to bind to the three points of the proposed pharmacophore model. They can be chosen from a variety of groups.

摘要翻译： 描述了新型LpxA抑制剂的合成和活性，这些抑制剂具有抗菌活性。 基于使用LpxA的晶体结构开发的受体模型设计化合物，并且被设置为在酶的活性位点具有有利的结合相互作用。 特别地，化合物呈现下式（I）其中V，W，X，Y和Z可以独立地为C，S，N或O，并且P1，P2和P3是与所提出的药效团的三个点结合的配体 模型。 他们可以从各种团体中选出。

公开(公告)号：US20070060606A1

公开(公告)日：2007-03-15

申请号：US11508755

申请日：2006-08-23

申请人： Harold Robertson ,  Eileen Denovan-Wright ,  Donald Weaver

发明人： Harold Robertson ,  Eileen Denovan-Wright ,  Donald Weaver

IPC分类号： A61K31/4741 ,  C07D491/02 ,  A61K31/428 ,  C07D417/02

CPC分类号： C07D409/06 ,  C07D413/06 ,  C07D491/04

摘要： Novel compounds that modulate PDE10A, a gene that is primarily expressed in medium spiny neurons of the mammalian striatum and has been found to inhibit striatal output by reducing spiny medium excitability and effect cAMP and cGMP signalling cascades in vivo in rats, and methods for treating psychosis and schizophrenia using the novel compounds. Methods for screening for further compounds to modulate PDE10A activity are also taught.

摘要翻译： 调节PDE10A的新型化合物，其主要在哺乳动物纹状体的中等多刺神经元中表达，并且已被发现通过减少大鼠中的多刺培养基兴奋性和影响体内的cAMP和cGMP信号级联来抑制纹状体输出，以及治疗精神病的方法 和使用新化合物的精神分裂症。 还教导了筛选其他化合物以调节PDE10A活性的方法。

公开(公告)号：US20070015813A1

公开(公告)日：2007-01-18

申请号：US11443396

申请日：2006-05-30

申请人： Michael Carter ,  Mark Hadden ,  Donald Weaver ,  Sheila Jacobo ,  Erhu Lu

发明人： Michael Carter ,  Mark Hadden ,  Donald Weaver ,  Sheila Jacobo ,  Erhu Lu

IPC分类号： A61K31/405

CPC分类号： C07D209/14 ,  A61K31/404 ,  A61K31/405 ,  C07D209/12 ,  C07D209/80 ,  C07D403/14 ,  C07D409/04 ,  C07D487/10

摘要： In certain embodiments, the invention is directed to a method for treating a protein folding disorder comprising administering to a subject a compound of the formulas disclosed. In preferred embodiments, the compounds are bis-indole compounds.

摘要翻译： 在某些实施方案中，本发明涉及治疗蛋白质折叠障碍的方法，包括向受试者施用所公开的化学式的化合物。 在优选的实施方案中，化合物是双吲哚化合物。

公开(公告)号：US20060167095A1

公开(公告)日：2006-07-27

申请号：US11316378

申请日：2005-12-22

申请人： Robert Kisilevsky ,  Walter Szarek ,  Donald Weaver

发明人： Robert Kisilevsky ,  Walter Szarek ,  Donald Weaver

IPC分类号： A61K31/185

CPC分类号： C07H15/04 ,  A61K31/095 ,  A61K31/185 ,  A61K31/255 ,  A61K31/34 ,  A61K31/41 ,  A61K31/70 ,  A61K47/51 ,  A61K47/549 ,  A61K47/55 ,  A61K47/555 ,  A61K47/58 ,  C07C305/10 ,  C07C309/05 ,  C07D491/04 ,  C07H11/00

摘要： Therapeutic compounds and methods for inhibiting amyloid deposition in a subject, whatever its clinical setting, are described. Amyloid deposition is inhibited by the administration to a subject of an effective amount of a therapeutic compound comprising an anionic group and a carrier molecule, or a pharmaceutically acceptable salt thereof, such that an interaction between an amyloidogenic protein and a basement membrane constituent is inhibited. Preferred anionic groups are sulfonates and sulfates. Preferred carrier molecules include carbohydrates, polymers, peptides, peptide derivatives, aliphatic groups, alicyclic groups, heterocyclic groups, aromatic groups and combinations thereof.

公开(公告)号：US06271334B1

公开(公告)日：2001-08-07

申请号：US09498681

申请日：2000-02-07

申请人： Jan Wilhelm E. Moos ,  Heide Anne Lochbiler ,  Jason Donald Weaver ,  Latoska Nikita Price ,  Frances Lamb ,  Donald Lynn Rutledge, Jr. ,  Ann Alfred J. Lemaire ,  Antonius Hendrikus G. van Engelen ,  Catharine Marie Den Breejen

发明人： Jan Wilhelm E. Moos ,  Heide Anne Lochbiler ,  Jason Donald Weaver ,  Latoska Nikita Price ,  Frances Lamb ,  Donald Lynn Rutledge, Jr. ,  Ann Alfred J. Lemaire ,  Antonius Hendrikus G. van Engelen ,  Catharine Marie Den Breejen

IPC分类号： C08G1830

CPC分类号： C08G18/7837 ,  C08G18/289 ,  C08G18/3296 ,  C08G18/3844 ,  C08G18/4063 ,  C08G18/792 ,  C08G18/798 ,  C08G2150/50 ,  C09D175/04 ,  Y10T428/3154 ,  Y10T428/31544 ,  Y10T428/31547 ,  Y10T428/31551 ,  Y10T428/31605

摘要： The present invention relates to a coating composition comprising: (a) a bicyclic oxazolidine compound; (b) a monocyclic oxazolidine compound; and (c) an isocyanate functional compound. The invention further relates to a method of coating a substrate with the coating composition and to a substrate coated with the coating composition.

摘要翻译： 本发明涉及一种涂料组合物，其包含：（a）双环恶唑烷化合物;（b）单环恶唑烷化合物; 和（c）异氰酸酯官能化合物。本发明还涉及一种用涂料组合物涂覆基材和涂覆有涂料组合物的基材的方法。

公开(公告)号：US5840294A

公开(公告)日：1998-11-24

申请号：US542997

申请日：1995-10-13

申请人： Robert Kisilevsky ,  Walter Szarek ,  Donald Weaver

发明人： Robert Kisilevsky ,  Walter Szarek ,  Donald Weaver

IPC分类号： C07D409/04 ,  A61K31/185 ,  A61K31/255 ,  A61K31/41 ,  A61K31/70 ,  A61K31/7024 ,  A61K31/737 ,  A61K31/795 ,  A61K45/00 ,  A61K47/48 ,  A61L33/08 ,  A61P3/10 ,  A61P25/00 ,  A61P25/28 ,  A61P29/00 ,  A61P43/00 ,  C07D257/04 ,  C07H11/00 ,  C07H15/04 ,  A61K31/74 ,  A61F2/02 ,  A61K31/785

CPC分类号： A61K31/185 ,  A61K31/255 ,  A61K31/41 ,  A61K31/70 ,  A61K31/737 ,  A61K31/795 ,  A61K47/48007 ,  A61K47/48023 ,  A61K47/48092 ,  A61K47/481 ,  A61K47/4813 ,  A61K47/48176 ,  A61L33/08 ,  C07H11/00 ,  C07H15/04

摘要： Therapeutic compounds and methods for inhibiting amyloid deposition in a subject, whatever its clinical setting, are described. Amyloid deposition is inhibited by the administration to a subject of an effective amount of a therapeutic compound comprising an anionic group and a carrier molecule, or a pharmaceutically acceptable salt thereof, such that an interaction between an amyloidogenic protein and a basement membrane constituent is inhibited. Preferred anionic groups are sulfonates and sulfates. Preferred carrier molecules include carbohydrates, polymers, peptides, peptide derivatives, aliphatic groups, alicyclic groups, heterocyclic groups, aromatic groups and combinations thereof.

公开(公告)号：US5728375A

公开(公告)日：1998-03-17

申请号：US472692

申请日：1995-06-06

申请人： Robert Kisilevsky ,  Walter Szarek ,  Donald Weaver

发明人： Robert Kisilevsky ,  Walter Szarek ,  Donald Weaver

IPC分类号： A61K31/185 ,  A61K31/255 ,  A61K31/41 ,  A61K31/70 ,  A61K31/737 ,  A61K31/795 ,  A61K47/48 ,  A61L33/08 ,  C07H11/00 ,  C07H15/04 ,  A61K31/74 ,  A61K31/785 ,  A61K47/32

CPC分类号： C07H15/04 ,  A61K31/185 ,  A61K31/255 ,  A61K31/41 ,  A61K31/70 ,  A61K31/737 ,  A61K31/795 ,  A61K47/48007 ,  A61K47/48023 ,  A61K47/48092 ,  A61K47/481 ,  A61K47/4813 ,  A61K47/48176 ,  A61L33/08 ,  C07H11/00

摘要： Therapeutic compounds and methods for inhibiting amyloid deposition in a subject, whatever its clinical setting, are described. Amyloid deposition is inhibited by the administration to a subject of an effective amount of a therapeutic compound comprising an anionic group and a carrier molecule, or a pharmaceutically acceptable salt thereof, such that an interaction between an amyloidogenic protein and a basement membrane constituent is inhibited. Preferred anionic groups are sulfonates and sulfates. Preferred carrier molecules include carbohydrates, polymers, peptides, peptide derivatives, aliphatic groups, alicyclic groups, heterocyclic groups, aromatic groups and combinations thereof.