公开(公告)号：US20090170951A1

公开(公告)日：2009-07-02

申请号：US12225572

申请日：2007-03-23

Applicant: Yousef Al-Abed

Inventor： Yousef Al-Abed

IPC: A61K31/13 ,  C07C249/00 ,  A61P29/00

CPC classification number: C07C251/86 ,  C07C281/02 ,  C07C311/49

Abstract: Provided are various compounds of Formula (I): Also provided are pharmaceutical compositions comprising the above compounds. Additionally, methods of inhibiting macrophage migration inhibitory factor (MIF) activity in a mammal are provided, as are methods of treating or preventing inflammation in a mammal. Further provided are methods of treating a mammal having sepsis, septicemia, and/or endotoxic shock. Also provided are methods of treating a mammal having an autoimmune disease, and methods of treating a mammal having a tumor.

Abstract translation: 提供式（I）的各种化合物：还提供包含上述化合物的药物组合物。 此外，提供了哺乳动物抑制巨噬细胞迁移抑制因子（MIF）活性的方法，以及治疗或预防哺乳动物炎症的方法。 还提供了治疗具有败血症，败血病和/或内毒素性休克的哺乳动物的方法。 还提供了治疗具有自身免疫疾病的哺乳动物的方法以及治疗具有肿瘤的哺乳动物的方法。

公开(公告)号：US07122571B2

公开(公告)日：2006-10-17

申请号：US10315494

申请日：2002-12-10

Applicant: E. Premkumar Reddy ,  M.V. Ramana Reddy

Inventor： E. Premkumar Reddy ,  M.V. Ramana Reddy

IPC: A61K31/405 ,  A61K31/38 ,  A61K31/34 ,  A61K31/18 ,  C07D209/14 ,  C07D333/20 ,  C07C323/00

CPC classification number: C07D209/14 ,  A61K31/18 ,  A61K31/40 ,  A61K31/44 ,  A61K31/63 ,  C07C311/39 ,  C07C311/49

Abstract: Compounds useful as inhibitors of cyclooxygenase-2 activity have the formulae I or Ia: wherein: Q1, Q2, n, m, X, Y and R are as defined herein.

Abstract translation: 可用作环加氧酶-2活性抑制剂的化合物具有式I或Ia：其中：Q 1，Q 2，n，m，X，Y和R如上所定义 这里。

公开(公告)号：US20060172936A1

公开(公告)日：2006-08-03

申请号：US11212045

申请日：2005-08-25

Applicant: Michael Hale ,  Clarence Andrews ,  Eric Furfine ,  Ronald Sherrill ,  Andrew Spaltenstein ,  Gregory Lowen

Inventor： Michael Hale ,  Clarence Andrews ,  Eric Furfine ,  Ronald Sherrill ,  Andrew Spaltenstein ,  Gregory Lowen

IPC: A61K38/17 ,  A61K31/70 ,  A61K31/325

CPC classification number: C07D213/30 ,  C07C311/48 ,  C07C311/49 ,  C07C2601/08 ,  C07C2601/14 ,  C07D215/48 ,  C07D235/06 ,  C07D235/26 ,  C07D235/30 ,  C07D235/32 ,  C07D241/42 ,  C07D243/04 ,  C07D265/02 ,  C07D277/30 ,  C07D307/20 ,  C07D309/06 ,  C07D309/12 ,  C07D309/22 ,  C07D319/06 ,  C07D401/12 ,  C07D405/12 ,  C07D407/12 ,  C07D413/06 ,  C07D417/12 ,  C07D493/04 ,  C07F9/6561

Abstract: The present invention relates to a novel class of sulfonamides which are aspartyl protease inhibitors. In one embodiment, this invention relates to a novel class of HIV aspartyl protease inhibitors characterized by specific structural and physicochemical features. This invention also relates to pharmaceutical compositions comprising these compounds. The compounds and pharmaceutical compositions of this invention are particularly well suited for inhibiting HIV-1 and HIV-2 protease activity and consequently, may be advantageously used as anti-viral agents against the HIV-1 and HIV-2 viruses. This invention also relates to methods For inhibiting the activity of HIV aspartyl protease using the compounds of this invention and methods for screening compounds for anti-HIV activity.

Abstract translation: 本发明涉及一类新型的磺酰胺，它们是天冬氨酰蛋白酶抑制剂。 在一个实施方案中，本发明涉及以特定结构和物理化学特征为特征的新型HIV天冬氨酰蛋白酶抑制剂。 本发明还涉及包含这些化合物的药物组合物。 本发明的化合物和药物组合物特别适用于抑制HIV-1和HIV-2蛋白酶活性，因此可有利地用作针对HIV-1和HIV-2病毒的抗病毒剂。 本发明还涉及使用本发明化合物抑制HIV天冬氨酰蛋白酶活性的方法和用于筛选抗HIV活性化合物的方法。

公开(公告)号：US06960664B2

公开(公告)日：2005-11-01

申请号：US10152601

申请日：2002-05-22

Applicant: Heinrich Schostarez ,  Robert Alan Chrusciel ,  Rebecca S. Centko

Inventor： Heinrich Schostarez ,  Robert Alan Chrusciel ,  Rebecca S. Centko

IPC: C07D277/20 ,  A61K31/166 ,  A61K31/18 ,  A61K31/426 ,  A61P25/00 ,  A61P25/16 ,  A61P25/28 ,  A61P43/00 ,  C07C243/28 ,  C07C243/32 ,  C07C311/16 ,  C07C311/49 ,  C07D277/56

CPC classification number: C07C243/32 ,  C07C243/28 ,  C07C311/16 ,  C07C311/49

Abstract: Disclosed are compounds of formula: and pharmaceutically acceptable salts and esters thereof, useful in treating and/or preventing Alzheimer's disease and other similar diseases, wherein RN, RC, R1, R2 and R20 are defined herein. These compounds include inhibitors of the beta-secretase enzyme that are useful in the treatment of Alzheimer's disease and other diseases characterized by deposition of A beta peptide in a mammal. The compounds of the invention are useful in pharmaceutical compositions and methods of treatment to reduce A beta peptide formation.

Abstract translation: 公开了可用于治疗和/或预防阿尔茨海默病和其它类似疾病的式的化合物及其药学上可接受的盐和酯，其中R N，R C，R 本文定义了R 1，R 2和R 20。 这些化合物包括β-分泌酶的抑制剂，其可用于治疗阿尔茨海默病和以哺乳动物中Aβ肽沉积为特征的其它疾病。 本发明的化合物可用于降低Aβ肽形成的药物组合物和治疗方法。

公开(公告)号：US06879754B2

公开(公告)日：2005-04-12

申请号：US10188955

申请日：2002-07-03

Applicant: Jianjun Zhang ,  Peiching Ling ,  Jinliang Chen ,  Ming Xu

Inventor： Jianjun Zhang ,  Peiching Ling ,  Jinliang Chen ,  Ming Xu

IPC: A61K31/40 ,  A61K31/44 ,  A61K31/63 ,  C07C311/39 ,  C07C311/49 ,  C07D209/14 ,  G02B6/12 ,  G02B6/124 ,  G02B6/125 ,  G02B6/34 ,  G02B6/35 ,  H04Q11/00

CPC classification number: G02B6/3536 ,  A61K31/40 ,  A61K31/44 ,  A61K31/63 ,  C07C311/39 ,  C07C311/49 ,  C07D209/14 ,  G02B6/12004 ,  G02B6/12007 ,  G02B6/124 ,  G02B6/125 ,  G02B6/29323 ,  G02B6/3502 ,  G02B6/355 ,  G02B6/3566 ,  G02B6/357 ,  G02B2006/12107 ,  G02B2006/12145 ,  H04Q11/0005 ,  H04Q2011/0016 ,  H04Q2011/0024 ,  H04Q2011/0032 ,  H04Q2011/0058

Abstract: The present invention discloses a drop-before-add optical routing and switching system. The drop-before-add optical routing and switching system includes an input waveguide for carrying a multiplexed optical signal comprising optical signals transmitted over a plurality of wavelength channels represented by λ1, λ2, λ3, . . . , λN−1 and λN, where N is a positive integer wherein the input waveguide extending over a first direction. The drop-before-add optical routing and switching system further includes a plurality of second direction waveguides extending over a second direction and intersecting at N intersections with the input waveguide. The drop-before-add optical routing and switching system further includes a plurality of wavelength selective grating switches each disposed on one of the N intersections for selectively transmitting an optical signal of a selected wavelength into an associated one of the second direction waveguide.

Abstract translation: 本发明公开了一种前置添加光路由和交换系统。 后添加光路由和交换系统包括用于承载复用光信号的输入波导，该多路复用光信号包括由λ1，λ2，λ3表示的多个波长信道上发送的光信号。 。 。 ，λN-1和λN，其中N是正整数，其中输入波导在第一方向上延伸。 后添加光路由和交换系统还包括多个第二方向波导，其在第二方向上延伸并且在与输入波导的N个交叉处相交。 前置添加光路由和切换系统还包括多个波长选择性光栅开关，每个波长选择光栅开关各自设置在N个相交中的一个上，用于选择性地将所选波长的光信号传输到第二方向波导中的相关联的一个。

公开(公告)号：US20050014841A1

公开(公告)日：2005-01-20

申请号：US10847108

申请日：2004-05-17

Applicant: Lain-Yen Hu ,  Suzanne Kesten ,  Huangshu Lei ,  Todd Ryder ,  David Wustrow

Inventor： Lain-Yen Hu ,  Suzanne Kesten ,  Huangshu Lei ,  Todd Ryder ,  David Wustrow

IPC: A61P3/00 ,  A61K31/18 ,  A61P3/10 ,  A61P9/10 ,  A61P13/02 ,  A61P21/00 ,  A61P25/00 ,  A61P25/04 ,  A61P25/06 ,  A61P25/18 ,  A61P25/22 ,  A61P25/28 ,  A61P25/36 ,  A61P27/02 ,  A61P27/06 ,  A61P43/00 ,  C07C311/30 ,  C07C311/46 ,  C07C311/49

CPC classification number: C07C311/49 ,  C07C2601/14

Abstract: The invention relates to BCAT inhibitors and the use thereof for treating or preventing neuronal loss associated with stroke, ischemia, CNS trauma, hypoglycemia and surgery, as well as treating neurodegenerative diseases including Alzheimer's disease, amyotrophic lateral sclerosis, Huntington's disease and Down's syndrome, treating or preventing the adverse consequences of the overstimulation of the excitatory amino acids, treating anxiety, psychosis, convulsions, aminoglycoside antibiotics-induced hearing loss, migraine headache, chronic pain, neuropathic pain, Parkinson's disease, diabetic retinopathy, glaucoma, CMV retinitis, urinary incontinence, opioid tolerance or withdrawal, and inducing anesthesia, as well as for enhancing cognition.

Abstract translation: 本发明涉及BCAT抑制剂及其用于治疗或预防与中风，缺血，CNS创伤，低血糖和手术相关的神经元损失以及治疗包括阿尔茨海默病，肌萎缩性侧索硬化，亨廷顿病和唐氏综合征的神经变性疾病的治疗或治疗 或预防兴奋性氨基酸过度刺激的不良后果，治疗焦虑症，精神病，抽搐，氨基糖苷类抗生素诱发的听力损失，偏头痛，慢性疼痛，神经性疼痛，帕金森病，糖尿病性视网膜病变，青光眼，CMV视网膜炎，尿失禁 ，阿片类药物耐受或戒断，诱导麻醉以及增强认知功能。

公开(公告)号：US06696487B2

公开(公告)日：2004-02-24

申请号：US09923124

申请日：2001-08-06

Applicant: Vincent Gerusz ,  Darren James Mansfield ,  José Perez ,  David Tickle ,  Jean-Pierre Vors ,  Derek Baldwin ,  Thomas Lawley Hough ,  Dale Robert Mitchell

Inventor： Vincent Gerusz ,  Darren James Mansfield ,  José Perez ,  David Tickle ,  Jean-Pierre Vors ,  Derek Baldwin ,  Thomas Lawley Hough ,  Dale Robert Mitchell

IPC: A01N4710

CPC classification number: C07D209/48 ,  A01N43/64 ,  A01N43/78 ,  A01N43/88 ,  A01N47/20 ,  A01N47/30 ,  A01N47/32 ,  A01N47/34 ,  A01N47/38 ,  C07C271/28 ,  C07C275/36 ,  C07C275/64 ,  C07C281/06 ,  C07C311/49 ,  C07C333/24 ,  C07C335/18 ,  C07C335/40 ,  C07C337/06 ,  C07C2601/02 ,  C07D207/09 ,  C07D213/61 ,  C07D213/75 ,  C07D213/77 ,  C07D235/14 ,  C07D239/42 ,  C07D271/06 ,  C07D271/10 ,  C07D285/08 ,  C07D295/21 ,  C07D295/32 ,  C07D307/20 ,  C07D307/68 ,  C07D317/58

Abstract: The invention relates to compounds of formula (I), and also to salts thereof, which have fungicidal activities: in which the various radicals and substituents are as defined in the description, and also to the fungicidal compositions containing them and to methods for combating the phytopathogenic fungi of crops using these compounds and compositions.

Abstract translation: 本发明涉及具有杀真菌活性的式（I）化合物及其盐，其中各种基团和取代基如说明书中所定义，还涉及含有它们的杀真菌组合物，以及用于防治 使用这些化合物和组合物的作物的植物病原真菌。

公开(公告)号：US20040023938A1

公开(公告)日：2004-02-05

申请号：US10390692

申请日：2003-03-19

Inventor： Takanori Tabuchi ,  Tetsuhiro Yamamoto ,  Masaharu Nakayama

IPC: A01N043/00 ,  A01N043/40 ,  A01N041/06 ,  A01N043/36

CPC classification number: C07C327/58 ,  A01N41/06 ,  A01N43/10 ,  A01N43/40 ,  A01N43/42 ,  A01N43/50 ,  A01N43/56 ,  A01N43/58 ,  A01N43/60 ,  A01N43/653 ,  A01N43/80 ,  A01N43/82 ,  A01N43/90 ,  C07C311/13 ,  C07C311/21 ,  C07C311/29 ,  C07C311/44 ,  C07C311/46 ,  C07C311/48 ,  C07C311/49 ,  C07C311/51 ,  C07C317/36 ,  C07C317/48 ,  C07C323/49 ,  C07C323/63 ,  C07C327/48 ,  C07C2601/02 ,  A01N2300/00

Abstract: The present invention relates to microbicides for agricultural or horticultural use containing sulfonamide derivative of, for example, a formula (I): 1 or a salt thereof, nullwherein A1 is (1) an aryl group which may be substituted or (2) a heterocyclic group which may be substituted, X1 is (1) a chemical bond, (2) a methylene group which may be substituted, or (3) a vinylene group which may be substituted, B1 is a five-membered heterocyclic group comprising nitrogen or sulfur atoms as the ring-constructing atoms except for carbon atoms and may be substituted or a condensed heterocyclic group which may be substituted, Z1 is (1) a hydrocarbon group which may be substituted, (2) an acyl group which may be substituted, (3) formyl group, (4) an amino group which may be substituted, (5) a group represented by nullNnullCR1R2 (wherein each of R1 and R2 is a hydrogen atom or a hydrocarbon group which may be substituted), (6) a cyclic amino group, (7) a group represented by nullOR3 (wherein R3 is a hydrogen atom, a hydrocarbon group which may be substituted, an acyl group which may be substituted, formyl group or an alkylsulfonyl group which may be substituted) or (8) nullS(O)nR4 (wherein n stands for an integer from 0 to 2, R4 stands for a hydrogen atom or a hydrocarbon group which may be substituted). The said compounds or the salts thereof are sulfonamide derivatives with microbicidal action, are useful as excellent microbicides for agricultural or horticultural use, because they are safe, and they have little influence on human beings, farm animals, natural enemies, or the environment, and exert excellent control effects even on resistant microbes.

Abstract translation: 本发明涉及用于农业或园艺用途的杀微生物剂，其含有例如式（I）的磺酰胺衍生物或其盐：其中A 1为（1）可被取代的芳基或（2 ）可以被取代的杂环基，X 1是（1）化学键，（2）可以被取代的亚甲基，或（3）可以被取代的亚乙烯基，B 1是 包含氮原子或硫原子的五元杂环基作为除碳原子外的环构成原子并且可以被取代，或可以被取代的稠合杂环基，Z 1是（1）可以被取代的烃基， （2）可以被取代的酰基，（3）甲酰基，（4）可以被取代的氨基，（5）由-N = CR 1 R 2表示的基团 R 1和R 2是氢原子或可被取代的烃基），（6）环状氨基，（7）由-OR 3表示的基团（其中 R 3为氢原子，可被取代的烃基，可被取代的酰基，甲酰基或可被取代的烷基磺酰基）或（8）-S（O）nR 4（ 其中n表示0至2的整数，R 4表示氢原子或可被取代的烃基）。 所述化合物或其盐是具有杀微生物作用的磺酰胺衍生物，因为它们是安全的，对人类，农场动物，天敌或环境几乎没有影响，因此可用作农业或园艺用途的优异杀微生物剂，以及 即使对抗性微生物也能起到优异的防治效果。

公开(公告)号：US20030225084A1

公开(公告)日：2003-12-04

申请号：US10402382

申请日：2003-03-31

Applicant: Gruenenthal GmbH

Inventor： Matthias Gerlach ,  Heinz Uragg ,  Michael Haurand ,  Claudia Katharina Puetz ,  Corinna Maul ,  Boris Chizh

IPC: A61K031/537 ,  A61K031/495 ,  A61K031/445 ,  A61K031/40 ,  A61K031/18

CPC classification number: C07D213/40 ,  C07C311/49 ,  C07C311/64 ,  C07C2601/14 ,  C07D213/75 ,  C07D213/77 ,  C07D231/40 ,  C07D239/26 ,  C07D295/215 ,  C07D295/32 ,  C07D307/52 ,  C07D333/20 ,  C07D401/12 ,  C07D409/12 ,  C07D521/00

Abstract: Sulfonylguanidine compounds corresponding to the tautomeric formulas I and Ia, a method for producing them, pharmaceutical compositions containing them, and methods of using them to prepare medicaments and for treating various medical conditions. The sulfonylguanidine compounds have an affinity for the gabapentin binding site and can be used to treat conditions such as pain, epilepsy, migraine and others.

Abstract translation: 对应于互变异构体式I和Ia的磺酰胍化合物，其制备方法，含有它们的药物组合物及其用于制备药物和用于治疗各种医疗条件的方法。 磺酰胍类化合物对加巴喷丁结合位点具有亲和力，可用于治疗疼痛，癫痫，偏头痛等疾病。

公开(公告)号：US06586617B1

公开(公告)日：2003-07-01

申请号：US09958953

申请日：2001-12-18

Applicant: Takanori Tabuchi ,  Tetsuhiro Yamamoto ,  Masaharu Nakayama

Inventor： Takanori Tabuchi ,  Tetsuhiro Yamamoto ,  Masaharu Nakayama

IPC: C07C25550

CPC classification number: C07C327/58 ,  A01N41/06 ,  A01N43/10 ,  A01N43/40 ,  A01N43/42 ,  A01N43/50 ,  A01N43/56 ,  A01N43/58 ,  A01N43/60 ,  A01N43/653 ,  A01N43/80 ,  A01N43/82 ,  A01N43/90 ,  C07C311/13 ,  C07C311/21 ,  C07C311/29 ,  C07C311/44 ,  C07C311/46 ,  C07C311/48 ,  C07C311/49 ,  C07C311/51 ,  C07C317/36 ,  C07C317/48 ,  C07C323/49 ,  C07C323/63 ,  C07C327/48 ,  C07C2601/02 ,  A01N2300/00

Abstract: The present invention relates to microbicides for agricultural or horticultural use containing a sulfonamide derivative.

Abstract translation: 本发明涉及含有磺酰胺衍生物的用于农业或园艺用途的杀微生物剂。