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11. 发明申请

WO02072542A3 PH-DEPENDENT NMDA RECEPTOR ANTAGONISTS 审中-公开
标题翻译： PH依赖性NMDA受体拮抗剂
公开(公告)号：WO02072542A3
公开(公告)日：2003-02-27
申请号：PCT/US0207033
申请日：2002-03-08
申请人： UNIV EMORY , DINGLEDINE RAYMOND J , LIOTTA DENNIS C , TRAYNELIS STEPHEN F , SNYDER JAMES P
发明人： DINGLEDINE RAYMOND J , LIOTTA DENNIS C , TRAYNELIS STEPHEN F , SNYDER JAMES P
IPC分类号： A61K31/136 , A61K31/138 , A61K31/18 , A61K31/222 , A61K31/417 , A61K31/4178 , A61K31/421 , A61K31/438 , A61K31/4433 , A61K31/445 , A61K31/4515 , A61K31/4745 , A61K31/495 , A61K31/496 , A61P7/00 , A61P25/02 , A61P25/04 , A61P25/08 , A61P25/14 , A61P25/28 , A61P29/00 , A61P35/00 , A61P43/00 , C07B53/00 , C07C213/02 , C07C217/34 , C07C303/40 , C07C311/08 , C07C311/21 , C07D263/24 , C07D211/18 , A61K31/415 , A61K31/47 , C07D217/16 , C07D263/06
CPC分类号： C07C217/34 , C07C311/08 , C07C311/21 , C07D263/24
摘要： NMDA receptor blockers, including pH-sensitive NMDA receptor blockers, are provided as neuroprotective drugs that are useful in stroke, traumatic brain injury, epilepsy, and other neurologic events that involve acidification of brain or spinal cord tissue. Compositions and methods of this invention are used for treating neurodegeneration resulting from NMDA receptor activation. The compounds described herein have enhanced activity in brain tissue having lower-than normal pH due to pathological conditions such as hypoxia resulting from stroke, traumatic brain injury, global ischemia tat may occur during cardiac surgery, hypoxia tat may occur following cessation of breathing, pre-eclampsia, spinal cord trauma, epilepsy, chronic pain, vascular dementia and glioma tumors. Compounds described herein are also useful in preventing neurodegeneration in patients with Parkinson's Alzheimer's, Huntington's chorea, ALS, and other neurodegenerative conditions known to the art to be responsive to treatment using NMDA receptor blockers. Preferably the compounds provided herein are allosteric NMDA inhibitors.
摘要翻译：提供NMDA受体阻滞剂，包括pH敏感的NMDA受体阻断剂，作为神经保护药物，其可用于中风，创伤性脑损伤，癫痫和涉及脑或脊髓组织酸化的其它神经系统事件。本发明的组合物和方法用于治疗由NMDA受体活化引起的神经变性。本文所述的化合物由于病理状况如卒中引起的缺氧，外伤性脑损伤，全身缺血，可能在心脏手术期间发生，可能会在呼吸停止后发生缺氧，因此具有低于正常pH值的脑组织中的活性增强。癫痫，脊髓创伤，癫痫，慢性疼痛，血管性痴呆和神经胶质瘤。本文描述的化合物还可用于预防帕金森氏老年痴呆症，亨廷顿氏舞蹈症，ALS患者和本领域已知的对NMDA受体阻断剂治疗有反应的其它神经变性病症患者的神经变性。优选地，本文提供的化合物是变构NMDA抑制剂。

12. 发明申请

WO0142243A3 PROTEIN KINASE INHIBITORS 审中-公开
标题翻译：蛋白激酶抑制剂
公开(公告)号：WO0142243A3
公开(公告)日：2002-11-07
申请号：PCT/US0033201
申请日：2000-12-07
申请人： ADVANCED MEDICINE INC , GRIFFIN JOHN H , JI YU-HUA , MAMMEN MATHAI , MARQUESS DANIEL , MORAN EDMUND J , WRAY JONATHAN W
发明人： GRIFFIN JOHN H , JI YU-HUA , MAMMEN MATHAI , MARQUESS DANIEL , MORAN EDMUND J , WRAY JONATHAN W
IPC分类号： C07C46/00 , C07C50/38 , C07C217/34 , C07C225/22 , C07C229/60 , C07D231/38 , C07D239/42 , C07D239/94 , C07D243/24 , C07D271/06 , C07D401/04 , C07D401/14 , C07D403/14 , C07D405/14 , C07D413/12 , C07D413/14 , C07D471/04 , C07D487/04 , C07D519/00 , C07F9/38 , C07F9/572 , A61K31/33 , A61K38/06 , C07F9/6558 , C07K5/08
CPC分类号： C07D231/38 , C07C46/00 , C07C50/38 , C07C217/34 , C07C225/22 , C07C229/60 , C07C2602/08 , C07D239/42 , C07D239/94 , C07D243/24 , C07D271/06 , C07D401/04 , C07D401/14 , C07D403/14 , C07D405/14 , C07D413/12 , C07D413/14 , C07D471/04 , C07D487/04 , C07F9/3873 , C07F9/3882 , C07F9/5728
摘要： Disclosed are compounds which inhibit or modulate the activity of protein kinases and pharmaceutical compositions containing such compounds. The disclosed compound contain two or more ligand moieties covalently linked together by one or more linking groups. Such compounds are useful for treating diseases or medical disorders mediated by protein kinases.
摘要翻译：公开了抑制或调节蛋白激酶活性的化合物和含有这些化合物的药物组合物。所公开的化合物含有两个或更多个通过一个或多个连接基团共价连接在一起的配体部分。这些化合物可用于治疗由蛋白激酶介导的疾病或医学病症。

13. 发明申请

WO00005193A1 GUAIACOXYPROPANOLAMINE DERIVATIVES WITH alpha / beta -ADRENERGIC BLOCKING ACTIVITY 审中-公开
标题翻译：具有α/β-ADRENERGIC阻断活性的焦油酰胺胺衍生物
公开(公告)号：WO00005193A1
公开(公告)日：2000-02-03
申请号：PCT/CN1998/000132
申请日：1998-07-23
IPC分类号： C07C217/34 , C07C217/64 , A61K31/155 , C07C217/54
CPC分类号： C07C217/34
摘要： The present invention relates to novel guaiacoxypropanolamine derivatives of formula (I): wherein R is CH2CH=CH2, CH=CHCOOC2H5, CH=CHCH3, CH2NHCO(CH2)7CH3; R3 is OH, OCH3, NHCH2CH3OCH3, CHR6; R4 is OCH3, OC2H5, CHR6; R6 is C1-C6 saturated alkyl, C1-C6 unsaturated alkyl; R2 is (II), (III), (IV), (V), (VI), (VII), (VIII), (IX), (X), (XI). The said compounds of formula (I) have alpha / beta -adrenergic blocking activity. The invention further relates to pharmaceutical composition comprising compound of formula (I) and pharmaceutical acceptable vehicle. The composition also has alpha / beta -adrenergic blocking activity, and is useful in the treatment of acute hypertension.
摘要翻译：本发明涉及式（I）的新型愈创木酚氧丙醇胺衍生物：其中R是CH 2 CH = CH 2，CH = CHCOOC 2 H 5，CH = CHCH 3，CH 2 NHCO（CH 2）7 CH 3; R3是OH，OCH3，NHCH2CH3OCH3，CHR6; R4是OCH3，OC2H5，CHR6; R6是C1-C6饱和烷基，C1-C6不饱和烷基; R2是（II），（III），（IV），（V），（VI），（VII），（VIII），（IX），（X），（XI）。所述式（I）化合物具有α/β-肾上腺素能阻断活性。本发明还涉及包含式（I）化合物和药物可接受载体的药物组合物。该组合物还具有α/β-肾上腺素能阻断活性，可用于治疗急性高血压。

14. 发明申请

WO2007045893A3 BETA ADRENERGIC RECEPTOR PHARMACOPHORE 审中-公开
标题翻译：抗体药物受体药物（BETA ADRENERGIC RECEPTOR PHARMACOPHORE）
公开(公告)号：WO2007045893A3
公开(公告)日：2007-11-29
申请号：PCT/GB2006003908
申请日：2006-10-20
申请人： UNIV READING , WATSON KIMBERLY ANN , LAMANNA CLAUDIA MARIA PIA
发明人： WATSON KIMBERLY ANN , LAMANNA CLAUDIA MARIA PIA
IPC分类号： C07C217/34 , C07C233/80 , C07C311/08 , C07C311/13 , C07C311/21 , C07C311/29 , C07C311/46 , C07C311/47 , C07D211/58 , C07D215/22 , C07D401/12 , C07D401/14 , C07D413/14 , C07D417/12 , C07D417/14 , C07F9/30
CPC分类号： C07C311/08 , C07C217/34 , C07C233/43 , C07C233/80 , C07C311/13 , C07C311/21 , C07C311/29 , C07C311/46 , C07C311/47 , C07C2601/14 , C07D211/58 , C07D215/22 , C07D215/227 , C07D401/12 , C07D413/14 , C07D417/12 , C07F9/301 , C07F9/304 , C07F9/60 , G01N2333/726
摘要： The invention provides a pharmacophore for identifying or designing an agonist that binds to a beta-3 adrenergic receptor, wherein the pharmacophore requires the following features: (a) a hydrogen accepting group adjacent to an aromatic moiety; (b) an aromatic moiety containing either an hydroxyl group in the para position or a nitrogen atom in the aromatic ring; (c) a chain having a stereogenic centre bearing a hydroxyl group; (d) a hydrophobic chain having a length of 6 carbon atoms or more; and (e) a hydrophobic chain wherein the direction of the hydrophobic chain is conferred by, or is the same as would be conferred by, the presence of an amide moiety at the start of the chain.
摘要翻译：本发明提供了用于鉴定或设计结合β-3肾上腺素能受体的激动剂的药效团，其中所述药效团需要以下特征：（a）与芳族部分相邻的氢接受基团; （b）在对位具有羟基或芳环中的氮原子的芳族部分; （c）具有带有羟基的立体中心的链; （d）长度为6个碳原子或更多的疏水链; 和（e）疏水链，其中所述疏水链的方向由在链起始处的酰胺部分的存在赋予或与之相同。

15. 发明申请

WO02057215A2 SODIUM CHANNEL MODULATORS 审中-公开
标题翻译：钠通道调节剂
公开(公告)号：WO02057215A2
公开(公告)日：2002-07-25
申请号：PCT/US2002/001307
申请日：2002-01-15
IPC分类号： A61K31/135 , A61K31/401 , A61K31/4152 , A61K31/417 , A61K31/4184 , A61K31/4402 , A61K31/4465 , A61K31/5375 , A61P25/00 , C07C217/08 , C07C217/30 , C07C217/36 , C07C217/76 , C07C217/84 , C07C255/54 , C07D207/09 , C07D211/26 , C07D213/30 , C07D213/38 , C07D213/65 , C07D215/20 , C07D231/12 , C07D233/54 , C07D233/61 , C07D233/76 , C07D235/06 , C07D295/13 , C07D317/54 , C07D333/16 , C07C217/32 , A61K31/33 , C07C217/34
CPC分类号： C07D213/30 , A61K31/135 , A61K31/401 , A61K31/4152 , A61K31/417 , A61K31/4184 , A61K31/4402 , A61K31/4465 , A61K31/5375 , C07C217/08 , C07C217/30 , C07C217/36 , C07C217/76 , C07C217/84 , C07C255/54 , C07C2601/18 , C07C2602/10 , C07D207/09 , C07D211/26 , C07D213/38 , C07D213/65 , C07D215/20 , C07D233/56 , C07D233/64 , C07D235/06 , C07D295/13 , C07D317/54 , C07D333/16
摘要： The invention provides sodium channel modulating compounds which are useful for treating diseases or conditions associated with sodium channel activity, such as neuropathic pain. The invention also provides pharmaceutical compositions comprising a compound of the present invention, as well as therapeutic methods comprising administering such a compound or salt to a mammal (e.g. a human).
摘要翻译：本发明涉及钠通道调节化合物，其用于治疗与钠通道活性相关的疾病或病症，例如神经性疼痛。本发明还提供了包含本发明化合物的药物组合物，以及将这些化合物或盐给予哺乳动物（例如人）的治疗方法。

16. 发明申请

WO0162705A8 AMINOALCOHOL DERIVATIVES 审中-公开
标题翻译：氨基醇衍生物
公开(公告)号：WO0162705A8
公开(公告)日：2001-09-27
申请号：PCT/JP0101442
申请日：2001-02-26
申请人： FUJISAWA PHARMACEUTICAL CO , TANIGUCHI KIYOSHI , KAYAKIRI HIROSHI , SAKURAI MINORU , FUJII NAOAKI , WASHIZUKA KENICHI , HAMASHIMA HITOSHI , TOMISHIMA YASUYO , HAMADA KAORI , YAMAMOTO NOBUHIRO , ISHIKAWA HIROFUMI , UNAMI NAOKO , MIURA TOSHIKO
发明人： TANIGUCHI KIYOSHI , KAYAKIRI HIROSHI , SAKURAI MINORU , FUJII NAOAKI , WASHIZUKA KENICHI , HAMASHIMA HITOSHI , TOMISHIMA YASUYO , HAMADA KAORI , YAMAMOTO NOBUHIRO , ISHIKAWA HIROFUMI , UNAMI NAOKO , MIURA TOSHIKO
IPC分类号： A61K31/195 , A61K31/403 , A61K31/4045 , A61K31/4406 , A61K31/4439 , A61P1/04 , A61P1/16 , A61P1/18 , A61P3/00 , A61P3/04 , A61P3/06 , A61P3/10 , A61P9/10 , A61P9/12 , A61P11/04 , A61P13/02 , A61P13/04 , A61P25/24 , A61P27/06 , A61P43/00 , C07C213/04 , C07C217/30 , C07C217/32 , C07C217/34 , C07C217/70 , C07C217/86 , C07C225/16 , C07C229/34 , C07C229/38 , C07C237/30 , C07C271/28 , C07C311/08 , C07C311/17 , C07C311/21 , C07C311/40 , C07D209/08 , C07D209/14 , C07D209/88 , C07D213/65 , C07D401/12 , A61K31/133 , C07C311/18 , C07D471/04
CPC分类号： C07D209/08 , C07C217/32 , C07C217/34 , C07C217/70 , C07C217/86 , C07C225/16 , C07C229/34 , C07C229/38 , C07C237/30 , C07C271/28 , C07C311/08 , C07C311/21 , C07D209/88 , C07D213/65 , Y02P20/55
摘要： A compound of the formula (I) wherein X1 is bond or -O(CH2)m- (in which m is an integral number of 1, 2 or 3); X2 is bond, -(CH2)n-, etc. (in which n is an integral number of 1, 2 or 3); R1 is hydrogen or amino protective group; R2 is hydroxy(lower)alkyl or (lower)alkoxy(lower)alkyl; A is phenyl, pyridyl, indolyl or carbazolyl, each of which may be substituted with one or two substituent(s) selected from the group consisting of halogen, hydroxy, lower alkyl, etc.; and B is phenyl or pyridyl, each of which may be substituted with one or two substituent(s) selected from the group consisting of halogen, hydroxy, nitro, etc.; and a pharmaceutically acceptable salt thereof which is useful as a medicament.
摘要翻译：其中X1是键或-O（CH2）m-（其中m是1,2或3的整数）的式（I）化合物; X2是键， - （CH2）n-等（其中n是1,2或3的整数）。 R1是氢或氨基保护基; R2是羟基（低级）烷基或（低级）烷氧基（低级）烷基; A是苯基，吡啶基，吲哚基或咔唑基，它们各自可以被一个或两个选自卤素，羟基，低级烷基等的取代基取代; 和B是苯基或吡啶基，其中的每一个可以被一个或两个选自卤素，羟基，硝基等的取代基取代; 及其药学上可接受的盐，其可用作药物。

17. 发明申请

WO01042243A2 PROTEIN KINASE INHIBITORS 审中-公开
标题翻译：蛋白激酶抑制剂
公开(公告)号：WO01042243A2
公开(公告)日：2001-06-14
申请号：PCT/US2000/033201
申请日：2000-12-07
IPC分类号： C07C46/00 , C07C50/38 , C07C217/34 , C07C225/22 , C07C229/60 , C07D231/38 , C07D239/42 , C07D239/94 , C07D243/24 , C07D271/06 , C07D401/04 , C07D401/14 , C07D403/14 , C07D405/14 , C07D413/12 , C07D413/14 , C07D471/04 , C07D487/04 , C07D519/00 , C07F9/38 , C07F9/572 , C07D471/00
CPC分类号： C07D231/38 , C07C46/00 , C07C50/38 , C07C217/34 , C07C225/22 , C07C229/60 , C07C2602/08 , C07D239/42 , C07D239/94 , C07D243/24 , C07D271/06 , C07D401/04 , C07D401/14 , C07D403/14 , C07D405/14 , C07D413/12 , C07D413/14 , C07D471/04 , C07D487/04 , C07F9/3873 , C07F9/3882 , C07F9/5728
摘要： Disclosed are compounds which inhibit or modulate the activity of protein kinases and pharmaceutical compositions containing such compounds. The disclosed compound contain two or more ligand moieties covalently linked together by one or more linking groups. Such compounds are useful for treating diseases or medical disorders mediated by protein kinases.
摘要翻译：公开了抑制或调节蛋白激酶活性的化合物和含有这些化合物的药物组合物。所公开的化合物含有两个或更多个通过一个或多个连接基团共价连接在一起的配体部分。这些化合物可用于治疗由蛋白激酶介导的疾病或医学病症。

19. 发明申请

WO98045255A1 CALCILYTIC COMPOUNDS 审中-公开
标题翻译：计算化合物
公开(公告)号：WO98045255A1
公开(公告)日：1998-10-15
申请号：PCT/US1998/006928
申请日：1998-04-08
IPC分类号： C07D295/18 , A61K31/135 , A61K31/165 , A61K31/166 , A61K31/18 , A61K31/19 , A61K31/275 , A61K31/40 , A61K31/4453 , A61K31/495 , A61K31/5375 , A61K31/54 , A61K31/55 , A61P1/02 , A61P3/14 , A61P5/18 , A61P19/00 , A61P19/02 , A61P19/08 , A61P19/10 , A61P35/00 , C07C217/34 , C07C217/36 , C07C217/58 , C07C255/49 , C07C255/54 , C07C255/56 , C07C255/57 , C07C255/59 , C07C255/60 , C07C311/08 , C07C311/16 , C07C311/20 , C07C311/21 , C07C311/29 , C07C311/60 , C07C321/22 , C07C321/28 , C07C323/17 , C07D267/20 , C07D295/00 , C07D295/092 , C07D295/104 , C07D295/192 , C07D295/20 , C07D295/215 , C07D295/22 , C07D295/26 , C07C255/07 , C07C69/74 , C07C69/76 , C07C229/04 , C07C311/03 , C07D223/08 , C07D243/12 , C07D265/30 , C07D273/04 , C07D413/08
CPC分类号： C07D295/192 , C07C255/57 , C07C311/08 , C07C311/21 , C07C311/29 , C07C323/17 , C07C2601/02 , C07C2603/32 , C07D267/20 , C07D295/215
摘要： Novel arylalkylamino compounds exhibiting calcilytic properties are provided.
摘要翻译：提供了具有钙离子性质的新型芳基烷基氨基化合物。

20. 发明申请

WO98041497A1 PROPANOLAMINE DERIVATIVES 审中-公开
标题翻译：丙酰胺衍生物
公开(公告)号：WO98041497A1
公开(公告)日：1998-09-24
申请号：PCT/JP1998/001112
申请日：1998-03-17
IPC分类号： C07C215/64 , C07C217/30 , C07C217/34 , C07C217/74 , A61K31/215 , C07C213/04
CPC分类号： C07C215/64 , C07C217/30 , C07C217/34 , C07C217/74 , C07C2602/10 , C07C2602/12 , Y02P20/55
摘要： Novel propanolamine derivatives of general formula (I) and salts thereof, which exhibit selective sympathomimetic action on the bowel, antiulcer action, antipancreatitic action, lipolytic action and antipollakiuric action; a process for the preparation of them; and drug composition containing the same. In said formula (I) R is hydrogen or lower alkenyloxy; R is carboxy(lower)alkoxy or protected carboxy(lower)alkoxy; R is hydrogen or a nitrogen-protecting group; and n is an integer of 1 or 2.
摘要翻译：通式（I）的新型丙醇胺衍生物及其盐对肠显示选择性交感神经作用，抗溃疡作用，止痛作用，脂肪分解作用和止痒作用; 它们的制备过程; 和含有其的药物组合物。在所述式（I）中，R 1是氢或低级烯氧基; R 2是羧基（低级）烷氧基或保护的羧基（低级）烷氧基; R 3是氢或氮保护基; 且n为1或2的整数。

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