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51. 发明公开

EP1406609A4 SUBSTITUTED ARYL COMPOUNDS AS NOVEL CYCLOOXYGENASE-2 SELECTIVE INHIBITORS, COMPOSITIONS AND METHODS OF USE 有权
标题翻译：取代作为一个新的芳基化合物，环氧合酶-2选择性抑制剂，组合物和使用方法
公开(公告)号：EP1406609A4
公开(公告)日：2004-04-14
申请号：EP01998052
申请日：2001-12-21
申请人： NITROMED INC
发明人： KHANAPURE SUBHASH P , GARVEY DAVID S , EARL RICHARD A , EZAWA MAIKO , FANG XINQIN , GASTON RICKY D
IPC分类号： A61K31/10 , A61K31/357 , A61K31/36 , A61K31/443 , A61K31/4525 , A61K45/00 , A61K45/06 , A61P1/04 , A61P1/14 , A61P7/02 , A61P7/04 , A61P9/10 , A61P11/00 , A61P11/06 , A61P11/08 , A61P13/02 , A61P13/12 , A61P15/04 , A61P15/08 , A61P17/00 , A61P17/02 , A61P19/02 , A61P21/02 , A61P25/28 , A61P27/02 , A61P27/16 , A61P29/00 , A61P31/04 , A61P35/00 , A61P35/02 , A61P37/08 , A61P39/02 , A61P43/00 , C07C317/14 , C07C317/22 , C07C317/24 , C07D317/56 , C07D319/08 , C07D319/18 , C07D319/20 , C07D405/06 , C07D413/06 , C07D263/56 , C07D405/04
CPC分类号： C07D319/08 , A61K45/06 , C07D317/56 , C07D319/18 , C07D319/20 , C07D405/06

52. 发明公开

EP1406609A2 SUBSTITUTED ARYL COMPOUNDS AS NOVEL CYCLOOXYGENASE-2 SELECTIVE INHIBITORS, COMPOSITIONS AND METHODS OF USE 有权
标题翻译：取代的芳基化合物作为新的环氧合酶-2选择性抑制剂，组合物和使用方法
公开(公告)号：EP1406609A2
公开(公告)日：2004-04-14
申请号：EP01998052.3
申请日：2001-12-21
申请人： Nitromed, Inc.
发明人： KHANAPURE, Subhash, P. , GARVEY, David, S. , EARL, Richard, A. , EZAWA, Maiko , FANG, Xinqin , GASTON, Ricky, D.
IPC分类号： A61K31/36 , C07D317/56 , C07D263/56 , C07D319/18 , C07D319/20 , C07C317/14 , C07C317/24 , C07D405/04
CPC分类号： C07D319/08 , A61K45/06 , C07D317/56 , C07D319/18 , C07D319/20 , C07D405/06
摘要： The invention describes substituted aryl compounds that are cyclooxygenase 2 (COX-2) selective inhibitors and compositions comprising at elast one cyclooxygenase 2 (COX-2) selective inhibitor, and, optionally, at least one compound that donates, transfers or releases nitric oxide, stimulates endogenous synthesis of nitric oxide, elevates endogenous levels of endothelium-derived relaxing factor or is a substrate for nitric oxide synthase, and/or, optionally, at least one therapeutic agent, such as, steroids, nonsterodal antiinflammatory compounds (NSAID), 5-lipoxygenase (5-LO) inhibitors, leukotriene B4 (LTB4) receptor antagonists, leukotriene A4 (LTA4) hydrolase inhibitors, 5-HT agonists, 3-hydroxy-3-methylglutaryl coenzyme A (HMG-CoA) inhibitors, H2 antagonists, antineoplastic agents, antiplatelet agents,thrombin inhibitors, thromboxane inhibitors, decongestants, diuretics, sedating or non-sedating anti-histamines, inducible nitric oxide synthase inhibitors, opioids, analgesics, Helicobacter pylori inhibitors, proton pump inhibitors, isoprostane inhibitors, and mixtures thereof. The invention also provides novel kits comprising at least one COX-2 selective inhibitor, and, optionally, at least one nitric oxide donor, and/or, optionally, at least one therapeutic agent. The cyclooxygenase 2 selective inhibitors of the invention can be optionally nitrosated and/or nitrosylated. The invention also provides methods for treating inflammation, pain and fever; for treating and/or improving the gastrointestinal properties of COX-2 selective inhibitors; for facilitating wound healing; for treating and/or preventing renal toxicity or other toxicities; for treating and/or preventing other disorders resulting from elevated levels of cyclooxygenase-2; and for improving the cardiovascular profile of COX-2 selective inhibitors.
摘要翻译：本发明描述了作为环加氧酶2（COX-2）选择性抑制剂的取代芳基化合物和包含弹性体一种环氧合酶2（COX-2）选择性抑制剂和任选地至少一种提供，转移或释放一氧化氮的化合物的组合物，刺激内源性一氧化氮合成，提高内源性内皮细胞衍生的松弛因子水平，或者是一氧化氮合酶的底物，和/或任选的至少一种治疗剂，例如类固醇，非水石类抗炎化合物（NSAID），5 （5-LO）抑制剂，白三烯B4（LTB4）受体拮抗剂，白三烯A4（LTA4）水解酶抑制剂，5-HT激动剂，3-羟基-3-甲基戊二酰辅酶A（HMG-CoA）抑制剂，H2拮抗剂，抗肿瘤血栓抑制剂，血栓烷抑制剂，减充血剂，利尿剂，镇静或非镇静抗组胺剂，诱导型一氧化氮合酶抑制剂，阿片样物质，止痛剂，Helic 幽门螺杆菌抑制剂，质子泵抑制剂，异前列烷抑制剂及其混合物。本发明还提供了包含至少一种COX-2选择性抑制剂和任选地至少一种一氧化氮供体和/或任选地至少一种治疗剂的新型试剂盒。本发明的环氧合酶2选择性抑制剂可以任选被亚硝化和/或亚硝基化。本发明还提供治疗炎症，疼痛和发热的方法; 用于治疗和/或改善COX-2选择性抑制剂的胃肠道特性; 用于促进伤口愈合; 用于治疗和/或预防肾毒性或其他毒性; 用于治疗和/或预防由环氧合酶-2水平升高引起的其他疾病; 并用于改善COX-2选择性抑制剂的心血管特征。

53. 发明公开

EP0214823A2 Alkylamide derivatives with H2-receptor antagonistic and cytoprotective action 失效
标题翻译：烷基酰胺与H2 rezeptorantagonistischer和细胞保护作用。
公开(公告)号：EP0214823A2
公开(公告)日：1987-03-18
申请号：EP86306707.0
申请日：1986-08-29
申请人： FUJIREBIO KABUSHIKI KAISHA also trading as FUJIREBIO INC.
发明人： Sekine, Yasuo , Hirakawa, Nobuhiko , Kashiwaba, Noriaki , Yamaura, Tetsuaki , Harada, Hisako , Kutsuma, Teruo , Matsumoto, Hajime , Sekine, Akihiro , Isowa, Yoshikazu
IPC分类号： C07D295/08 , C07D213/70 , C07D277/74 , C07D239/38 , C07D285/12 , C07D307/38 , C07D333/18 , C07D213/32 , C07D277/64 , C07C149/273 , C07D317/56
CPC分类号： C07D213/70 , C07D213/32 , C07D213/38 , C07D213/61 , C07D213/65 , C07D213/79 , C07D239/38 , C07D277/64 , C07D277/74 , C07D285/135 , C07D295/096 , C07D307/38 , C07D307/52 , C07D307/68 , C07D317/56 , C07D333/18 , C07D333/28 , C07D333/38 , C07D405/12 , C07D409/12 , C07D413/12 , C07D417/12
摘要： Alkylamide derivatives having the formula,
These compounds have a strong antiulcer action depend on histamine H 2 -receptor antagonistic action and a cytoprotective action upon gastric mucous membrance.

54. 发明专利

JPWO2016133160A1 スルホンアミド誘導体またはその薬学的に許容される酸付加塩审中-公开
公开(公告)号：JPWO2016133160A1
公开(公告)日：2018-02-15
申请号：JP2017500731
申请日：2016-02-18
申请人：国立大学法人筑波大学 , ボード・オブ・リージエンツ,ザ・ユニバーシテイ・オブ・テキサス・システム
发明人：柳沢正史 , 長瀬博 , 斉藤毅 , 入鹿山容子
IPC分类号： C07C311/29 , A61K31/18 , A61K31/36 , A61K31/4045 , A61K31/426 , A61K31/431 , A61K31/4402 , A61K31/4406 , A61K31/4439 , A61K31/47 , A61K31/472 , A61K31/498 , A61P3/04 , A61P3/10 , A61P25/20 , A61P25/24 , A61P31/04 , A61P43/00 , C07C311/44 , C07D209/20 , C07D213/32 , C07D213/40 , C07D215/48 , C07D217/26 , C07D241/44 , C07D277/56 , C07D307/56 , C07D317/56 , C07D417/04
CPC分类号： A61K31/18 , A61K31/341 , A61K31/36 , A61K31/405 , A61K31/426 , A61K31/4406 , A61K31/4439 , A61K31/47 , A61K31/472 , A61K31/498 , C07C311/29 , C07D209/20 , C07D213/40 , C07D215/48 , C07D215/50 , C07D217/26 , C07D241/44 , C07D277/56 , C07D307/54 , C07D317/56 , C07D417/04
摘要：本発明は、優れたナルコレプシー等の予防剤または治療剤として有用であると期待されるオレキシン受容体作動活性を示す新規低分子化合物を提供することを目的とする。本発明は、優れたオレキシン受容体作動活性を有する一般式(I):(式中の各記号は明細書に記載のものと同義である。)で表されるスルホンアミド誘導体およびその薬学的に許容される酸付加塩、並びに当該誘導体またはその薬学的に許容される酸付加塩を含有するオレキシン受容体作動薬を提供する。

58. 发明专利

JP2005068117A New sulfonyldiazomethane compound, photo acid generator, resist material using the same and method for forming pattern 有权
标题翻译：新型磺基二甲氧基化合物，照相酸发生器，使用其的耐腐蚀材料和形成图案的方法
公开(公告)号：JP2005068117A
公开(公告)日：2005-03-17
申请号：JP2003304060
申请日：2003-08-28
申请人： Shin Etsu Chem Co Ltd , 信越化学工業株式会社
发明人： KOBAYASHI KATSUHIRO , OSAWA YOICHI , KINSHO TAKESHI , FUKUDA EIJI , TANAKA YOSHIO
IPC分类号： C07C317/28 , C07D317/56 , C07D317/72 , C07D319/08 , C09K3/00 , G03C5/18 , G03F7/004 , G03F7/038 , G03F7/039 , H01L21/027
CPC分类号： C07D317/72 , C07C317/28 , C07C2601/14 , C07D319/08 , G03F7/0045 , G03F7/0382 , G03F7/0392 , G03F7/0395 , Y10S430/106 , Y10S430/111
摘要： PROBLEM TO BE SOLVED: To provide a sulfonyldiazomethane compound and a photo acid generator, suitable for a chemical amplification type resist material, a resist material by using them and a method for forming a pattern. SOLUTION: This sulfonyldiazomethane compound expressed by the following general formula (1), e.g. expressed by general formula (1a), the photo acid generator containing the same compound and a chemical amplification type resist material containing (A) a resin changing its solubility to an alkali developing liquid by an action of an acid and (B) the sulfonyldiazomethane compound expressed by general formula (1) and generating the acid by the irradiation of radiation are provided. The method for forming the pattern comprises a process of applying the resist material on a substrate plate, a process of heating, a process of exposing to light and a process of develop-treating as necessary and then developing by using the developing liquid. COPYRIGHT: (C)2005,JPO&NCIPI
摘要翻译：待解决的问题：提供适用于化学放大型抗蚀剂材料的磺酰基二氮甲烷化合物和光酸产生剂，通过使用它们的抗蚀剂材料和形成图案的方法。解决方案：由以下通式（1）表示的该磺酰基重氮甲烷化合物，例如由通式（1a）表示，含有相同化合物的光酸反应器和含有（A）通过酸作用改变其对碱性显影液的溶解性的树脂的化学放大型抗蚀剂材料，（B）磺酰基二氮甲烷化合物提供了由通式（1）表示并通过辐射照射产生酸。形成图案的方法包括在基板上施加抗蚀剂材料的方法，加热方法，曝光过程和必要时进行显影处理，然后通过使用显影液显影。版权所有（C）2005，JPO＆NCIPI

59. 发明专利

JP2000186006A PEST CONTROLLING AND VERMICIDAL USE OF 1- ARYL-1-(SUBSTITUTED THIO, SULFINYL AND SULFONYL)-2- NITROETHANE COMPOUND 失效
公开(公告)号：JP2000186006A
公开(公告)日：2000-07-04
申请号：JP32247899
申请日：1999-11-12
申请人： AMERICAN CYANAMID CO
发明人： WOOD WILLIAM WAKEFIELD , ENOS ANNMARIE
IPC分类号： C07D295/18 , A01N33/18 , A01N33/20 , A01N37/36 , A01N39/00 , A01N43/08 , A01N43/10 , A01N43/40 , A01N43/84 , C07C323/07 , C07C323/09 , C07C323/12 , C07C323/16 , C07C323/52 , C07C323/58 , C07C323/60 , C07D213/32 , C07D295/185 , C07D307/38 , C07D317/56 , C07D333/18 , C07D333/28 , C07D407/12
摘要： PROBLEM TO BE SOLVED: To effectively control pests or parasites such as helminthes, nematodes, insects, Acarina, and the like by contacting the pests or parasites or their feed, habitat or propagation place with a specific compound. SOLUTION: Pests or parasites are controlled by bringing the pests or parasites such as helminthes, nematodes, insects, Acarina, and the like into contact with a 1-aryl-1-(substituted thio, sulfinyl or sulfonyl)-2-nitroethane compound expressed by the formula [Ar is a (substituted) phenyl, a (substituted) 1- or 2-naphtyl, a (substituted) 2-, 3- or 4- pyridyl or the like; R is H, a 1-4C (halo)alkyl, a 2-4C (halo)alkenyl, a (substituted) phenyl or the like; (m) is 0, 1 or 2; R1 is H, a 1-4C alkyl or a (substituted) phenyl].

60. 发明专利

JP2000053566A THERAPEUTIC AGENT FOR GLAUCOMA 失效
公开(公告)号：JP2000053566A
公开(公告)日：2000-02-22
申请号：JP21256299
申请日：1999-06-23
申请人： PFIZER PROD INC
发明人： CAMERON KIMBERLY O'KEEFE , LEFKER BRUCE ALLEN
IPC分类号： C07D239/26 , A61K31/00 , A61K31/18 , A61K31/192 , A61K31/197 , A61K31/341 , A61K31/343 , A61K31/357 , A61K31/36 , A61K31/38 , A61K31/381 , A61K31/40 , A61K31/401 , A61K31/4015 , A61K31/403 , A61K31/404 , A61K31/41 , A61K31/4245 , A61K31/426 , A61K31/433 , A61K31/44 , A61K31/4402 , A61K31/4433 , A61K31/47 , A61K31/4709 , A61K31/496 , A61K31/50 , A61K31/505 , A61P27/06 , C07D207/27 , C07D213/36 , C07D215/18 , C07D241/12 , C07D257/04 , C07D271/12 , C07D277/20 , C07D277/28 , C07D277/46 , C07D285/06 , C07D307/24 , C07D307/52 , C07D307/68 , C07D307/81 , C07D317/56 , C07D319/18 , C07D333/18 , C07D333/20 , C07D333/40 , C07D333/62 , C07D409/12
摘要： PROBLEM TO BE SOLVED: To obtain a therapeutic agent for glaucoma capable of reducing the intraocular pressure of mammals including human by including a specific compound. SOLUTION: This therapeutic agent contains therapeutically effective amount of a compound of the formula [B is N; A is a 1-6C alkylsulfonyl, a 3-7C cycloalkylsulfonyl or the like; Q is a 2-6C alkylene-W-1-3C alkylene, a 3-8C alkylene or the like (W is oxy, thio, sulfino or the like); Z is carboxyl, a 1-6C alkoxycarbonyl, or the like; K is a bond, a 1-8C alkylene or the like; M is a five- to eight-membered ring or the like] such as 7-[(4-butyl-benzyl)- methanesulfonyl-amino]-heptanoic acid or its charmacolocricallw acceatable salt or a prodrug. Preferably, about 0.01 to about 10 mg/kg/day of the compound is topically administered.

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