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公开(公告)号:US09585891B2
公开(公告)日:2017-03-07
申请号:US14430953
申请日:2013-09-10
申请人: MERCK PATENT GMBH
IPC分类号: C07C237/06 , C07C235/06 , C07D265/32 , C07D307/16 , C07D295/26 , C07D333/24 , A61K31/5375 , A61K31/16 , A61K31/165 , A61K31/381 , A61K31/4453 , C07C255/54 , C07C275/28 , C07D333/20 , C07C311/04 , C07C311/13 , C07C311/21 , C07D401/12 , C07C317/22 , C07C317/32 , C07D405/12 , C07C235/12 , C07C235/80 , C07C237/22 , C07D211/26 , C07D295/088 , C07D211/58 , C07D295/135 , C07D295/185 , C07D211/96 , C07D213/68 , C07D307/14 , A61K31/341
CPC分类号: A61K31/5375 , A61K31/16 , A61K31/165 , A61K31/341 , A61K31/381 , A61K31/4453 , C07C235/06 , C07C235/12 , C07C235/80 , C07C237/06 , C07C237/22 , C07C255/54 , C07C275/28 , C07C311/04 , C07C311/13 , C07C311/21 , C07C317/22 , C07C317/32 , C07C2601/02 , C07C2601/14 , C07D211/26 , C07D211/58 , C07D211/96 , C07D213/68 , C07D265/32 , C07D295/088 , C07D295/135 , C07D295/185 , C07D295/26 , C07D307/14 , C07D307/16 , C07D333/20 , C07D333/24 , C07D401/12 , C07D405/12
摘要: The present invention relates to alpha hydroxy amides including compounds of formula I: and related compounds and their use in the prophylaxis and treatment of inflammatory disorders and diseases, wherein T1, T2, W and RW have the meanings given in claim 1.
摘要翻译: 本发明涉及包括式I化合物和相关化合物的α-羟基酰胺及其在预防和治疗炎性疾病和疾病中的用途,其中:T1表示以下基团之一:T2-W表示以下基团之一: W表示单键,或选自-CHRc-和-CH = CH-的基团; (CH2)nCet, - (CH2)nCyc, - (CH2)nOAr, - (CH2)nAr, - (CH2)nCet, - (CH2) (OH), - (CH2)nOCyc或A.
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2.Phenalkylamine derivatives, pharmaceutical compositions containing them, and their use in therapy 有权
标题翻译: 苯烷基胺衍生物,含有它们的药物组合物及其在治疗中的用途公开(公告)号:US09238619B2
公开(公告)日:2016-01-19
申请号:US14282712
申请日:2014-05-20
发明人: Frauke Pohlki , Udo Lange , Wilhelm Amberg , Michael Ochse , Berthold Behl , Wilfried Hornberger , Mario Mezler , Charles W. Hutchins , Sean Turner
IPC分类号: A61K31/135 , C07C211/25 , C07C311/06 , C07C311/04 , C07C311/05 , C07C311/10 , C07D205/04 , C07D207/08 , C07D207/267 , C07D231/18 , C07D233/42 , C07D295/135 , C07D401/12 , C07D403/12 , C07D233/84
CPC分类号: C07C311/06 , C07C311/04 , C07C311/05 , C07C311/10 , C07C2601/02 , C07C2601/04 , C07D205/04 , C07D207/08 , C07D207/267 , C07D231/18 , C07D233/42 , C07D233/84 , C07D295/135 , C07D401/12 , C07D403/12
摘要: The present invention relates to phenalkylamine derivatives of the formula (I) or a physiologically tolerated salt thereof. The invention relates to pharmaceutical compositions comprising such phenalkylamine derivatives, and the use of such phenalkylamine derivatives for therapeutic purposes. The phenalkylamine derivatives are GlyT1 inhibitors.
摘要翻译: 本发明涉及式(I)的苯烷基胺衍生物或其生理上耐受的盐。 本发明涉及包含这种苯烷基胺衍生物的药物组合物,以及这种苯烷基胺衍生物用于治疗目的的用途。 酚烷基胺衍生物是GlyT1抑制剂。
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公开(公告)号:US09096500B2
公开(公告)日:2015-08-04
申请号:US13808639
申请日:2011-07-04
IPC分类号: C07C311/04 , A61K31/18 , C07C311/51 , C07D231/12 , A61K31/277 , A61K31/415 , A61K31/4245 , A61K31/451 , A61K31/495 , A61K31/50 , A61K45/06 , C07D211/22 , C07D237/08 , C07D241/04 , C07D271/06
CPC分类号: C07C311/04 , A61K31/18 , A61K31/277 , A61K31/415 , A61K31/4245 , A61K31/451 , A61K31/495 , A61K31/50 , A61K45/06 , C07C311/51 , C07D211/22 , C07D231/12 , C07D237/08 , C07D241/04 , C07D271/06
摘要: The invention relates to sulfonamide derivatives, to their use in medicine, to compositions containing them, to processes for their preparation and to intermediates used in such processes. More particularly the invention relates to a new sulfonamide Nav1.7 inhibitors of formula (I): or a pharmaceutically acceptable salt thereof, wherein X, Ar1, R1, R2, R3, R4 and R5 are as defined in the description. Nav 1.7 inhibitors are potentially useful in the treatment of a wide range of disorders, particularly pain.
摘要翻译: 本发明涉及磺酰胺衍生物,其在医学上的用途,含有它们的组合物,其制备方法以及在这些方法中使用的中间体。 更具体地,本发明涉及式(I)的新的磺酰胺Nav1.7抑制剂:或其药学上可接受的盐,其中X,Ar1,R1,R2,R3,R4和R5如说明书中所定义。 Nav 1.7抑制剂可用于治疗各种疾病,特别是疼痛。
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4.PREPARATION OF BENZOFURANS AND USE THEREOF AS SYNTHETIC INTERMEDIATES 审中-公开
标题翻译: 苯并呋喃的制备及其作为合成中间体的应用公开(公告)号:US20130046103A1
公开(公告)日:2013-02-21
申请号:US13578113
申请日:2011-02-10
申请人: Ehud Marom , Michael Mizhiritskii , Shai Rubnov
发明人: Ehud Marom , Michael Mizhiritskii , Shai Rubnov
IPC分类号: C07D307/79 , C07C317/28 , C07C311/04 , C07D307/80
CPC分类号: C07D307/79 , C07C311/48 , C07D307/80
摘要: The present invention provides several synthetic methods for preparing N-(2-butylbenzofuran-5-yl)-N-(methylsulfonyl)methanesulfonamide, a compound of formula (3), an intermediate in the preparation of Dronedarone. The present invention further provides a process for preparing Dronedarone, comprising the steps of converting 2-butyl-5-bis(methanesulfon)-amidobenzofuran of formula (3) to Dronedarone, wherein the 2-butyl-5-bis(methanesulfon)-amidobenzofuran of formula (3) is prepared by the processes of the present invention.
摘要翻译: 本发明提供了几种制备N-(2-丁基苯并呋喃-5-基)-N-(甲基磺酰基)甲磺酰胺的合成方法,式(3)化合物是制备决奈达隆的中间体。 本发明还提供了一种制备决奈达隆的方法,包括将式(3)的2-丁基-5-双(甲磺酰) - 氨基苯并呋喃转化成决奈达隆的步骤,其中2-丁基-5-双(甲磺酰) - 氨基苯并呋喃 通过本发明的方法制备式(3)的化合物。
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公开(公告)号:US07235690B2
公开(公告)日:2007-06-26
申请号:US10132163
申请日:2002-04-26
IPC分类号: C07C311/04 , A61K31/18
CPC分类号: C07D207/335 , C07C311/08 , C07C311/21 , C07C311/29 , C07C311/44 , C07C2601/02 , C07C2601/14 , C07D213/40 , C07D213/64 , C07D215/12 , C07D231/12 , C07D231/16 , C07D233/56 , C07D233/64 , C07D235/14 , C07D249/08 , C07D277/28 , C07D307/14 , C07D307/52 , C07D405/12
摘要: The present invention is related to anthranilamides of formula I, in which R(1) to R(7) have the meanings indicated herein, a process for their preparation, their use as medicaments, and pharmaceutical preparations containing them. The compounds act on the Kv1.5 potassium channel and inhibit a potassium current which is referred to as the ultra-rapidly activating delayed rectifier in the atrium of the human heart. The compounds are therefore suitable for use as novel antiarrhythmic agents for the treatment and prophylaxis of atrial arrhythmias (e.g., atrial fibrillation (AF) or atrial flutter).
摘要翻译: 本发明涉及式I的邻氨基苯甲酰胺,其中R(1)至R(7)具有本文所述的含义,其制备方法,用作药物,以及含有它们的药物制剂。 化合物作用于Kv1.5钾通道并抑制在人心脏中心被称为超快速活化延迟整流器的钾电流。 因此,该化合物适合用作新的抗心律不齐剂,用于治疗和预防心律失常(例如心房颤动(AF)或心房扑动))。
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公开(公告)号:US20050096357A1
公开(公告)日:2005-05-05
申请号:US11004751
申请日:2004-12-03
申请人: John Elder , Andrew Forrest , Richard Jarvest , Robert Sheppard
发明人: John Elder , Andrew Forrest , Richard Jarvest , Robert Sheppard
IPC分类号: A61K31/27 , A61K31/34 , A61K31/357 , A61K31/38 , A61K31/381 , A61K31/397 , A61K31/40 , A61K31/4015 , A61K31/415 , A61K31/4178 , A61K31/42 , A61K31/421 , A61K31/44 , A61K31/4402 , A61K31/4406 , A61K31/4409 , A61K31/4412 , A61K31/445 , A61K31/4462 , A61K31/4465 , A61K31/495 , A61K31/4965 , A61K31/505 , A61K31/5375 , A61K31/5377 , A61K31/54 , A61P31/04 , C07C271/06 , C07C271/66 , C07C311/04 , C07C317/18 , C07C323/12 , C07D205/04 , C07D207/12 , C07D207/16 , C07D207/22 , C07D207/26 , C07D207/273 , C07D207/40 , C07D207/404 , C07D211/00 , C07D211/42 , C07D211/46 , C07D211/62 , C07D211/76 , C07D213/04 , C07D213/30 , C07D213/40 , C07D213/64 , C07D231/20 , C07D231/22 , C07D239/30 , C07D239/42 , C07D239/48 , C07D239/54 , C07D241/04 , C07D241/24 , C07D261/02 , C07D261/08 , C07D261/12 , C07D263/24 , C07D265/30 , C07D279/12 , C07D295/00 , C07D295/185 , C07D295/26 , C07D307/20 , C07D307/66 , C07D317/10 , C07D317/24 , C07D319/06 , C07D331/04 , C07D333/32 , C07D333/48 , C07D401/06 , C07D403/06 , C07D413/06 , C07D453/02 , C07D493/04 , A61K31/325 , A61K31/401
CPC分类号: C07D331/04 , C07C271/66 , C07C2601/10 , C07C2603/82 , C07D205/04 , C07D207/12 , C07D207/16 , C07D207/22 , C07D207/26 , C07D207/273 , C07D207/404 , C07D211/42 , C07D211/46 , C07D213/30 , C07D213/40 , C07D213/64 , C07D231/22 , C07D239/30 , C07D239/42 , C07D239/49 , C07D239/54 , C07D261/12 , C07D263/24 , C07D265/30 , C07D295/185 , C07D295/26 , C07D307/20 , C07D307/66 , C07D317/10 , C07D319/06 , C07D333/32 , C07D401/06 , C07D493/04
摘要: Pleuromutilin compounds of the formula: are of use in anti-bacterial therapy.
摘要翻译: 具有下列公式的Pleuromutilin化合物:用于抗菌治疗。
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7.Perfluorinated amide salts and their uses as ionic conducting materials 审中-公开
标题翻译: 全氟化酰胺盐及其用作离子导电材料公开(公告)号:US20050074668A1
公开(公告)日:2005-04-07
申请号:US10789453
申请日:2004-02-27
IPC分类号: C07D233/58 , B01F1/00 , B01J31/02 , B01J31/04 , B01J31/06 , B01J31/12 , B01J31/18 , B01J31/22 , C01B31/02 , C04B41/83 , C07B37/02 , C07B37/12 , C07B41/06 , C07B61/00 , C07C45/46 , C07C45/69 , C07C67/00 , C07C255/05 , C07C255/10 , C07C255/13 , C07C255/17 , C07C255/27 , C07C255/31 , C07C255/46 , C07C255/65 , C07C257/14 , C07C309/80 , C07C311/03 , C07C311/04 , C07C311/09 , C07C311/48 , C07C317/04 , C07C317/08 , C07C317/14 , C07C317/22 , C07C317/24 , C07C317/34 , C07C317/44 , C07D207/44 , C07D207/452 , C07D213/76 , C07D219/10 , C07D231/18 , C07D233/56 , C07D233/90 , C07D239/60 , C07D241/46 , C07D241/48 , C07D249/04 , C07D249/08 , C07D249/10 , C07D249/12 , C07D251/66 , C07D251/70 , C07D253/06 , C07D277/64 , C07D277/82 , C07D279/20 , C07D285/00 , C07D285/12 , C07D285/125 , C07D285/135 , C07D285/15 , C07D285/16 , C07D303/34 , C07D303/36 , C07D307/54 , C07D307/64 , C07D311/52 , C07D311/58 , C07D311/72 , C07D311/80 , C07D311/82 , C07D319/06 , C07D333/16 , C07D333/20 , C07D333/24 , C07D405/06 , C07D407/04 , C07D409/12 , C07D417/10 , C07D417/14 , C07D487/22 , C07F1/02 , C07F1/06 , C07F7/10 , C07F7/18 , C07F9/6584 , C07F11/00 , C07F15/00 , C07F17/02 , C08F2/00 , C08F2/48 , C08F4/00 , C08F4/04 , C08F4/46 , C08F4/60 , C08F12/22 , C08F12/26 , C08F12/30 , C08F16/14 , C08F216/14 , C08F222/30 , C08F228/02 , C08G59/68 , C08G65/22 , C08G65/334 , C08G73/00 , C08G73/02 , C08G75/00 , C08G75/14 , C08G77/04 , C08G77/388 , C08G85/00 , C08J3/20 , C08J3/24 , C08J3/28 , C08J7/04 , C08L101/00 , C09B47/04 , C09B57/00 , C09B69/00 , C09B69/02 , C09B69/10 , C09C1/56 , C09C3/10 , C09D11/00 , C09K9/02 , C25B9/00 , G02F1/15 , H01B1/04 , H01B1/06 , H01B1/12 , H01B3/20 , H01G9/02 , H01G11/54 , H01M4/00 , H01M4/02 , H01M4/131 , H01M4/133 , H01M4/134 , H01M4/40 , H01M4/48 , H01M4/485 , H01M4/50 , H01M4/505 , H01M4/52 , H01M4/525 , H01M4/58 , H01M4/60 , H01M4/62 , H01M4/66 , H01M4/96 , H01M6/00 , H01M6/04 , H01M6/06 , H01M6/16 , H01M6/18 , H01M8/00 , H01M10/052 , H01M10/0525 , H01M10/0565 , H01M10/0567 , H01M10/0568 , H01M10/36 , H01M10/40 , C07C311/05 , C07C331/20
CPC分类号: B01J31/0224 , B01J31/0215 , B01J31/0222 , B01J31/0225 , B01J31/0227 , B01J31/0235 , B01J31/0239 , B01J31/0247 , B01J31/0251 , B01J31/0252 , B01J31/0267 , B01J31/0271 , B01J31/0281 , B01J31/0288 , B01J31/0289 , B01J31/04 , B01J31/06 , B01J31/068 , B01J31/124 , B01J31/1815 , B01J31/2208 , B01J2231/122 , B01J2231/14 , B01J2231/326 , B01J2231/341 , B01J2231/348 , B01J2231/4205 , B01J2231/543 , B01J2531/35 , B01J2531/824 , C07B37/02 , C07B37/12 , C07C45/46 , C07C45/69 , C07C67/00 , C07C255/10 , C07C255/17 , C07C255/27 , C07C255/46 , C07C255/65 , C07C257/14 , C07C311/03 , C07C311/04 , C07C311/09 , C07C311/48 , C07C317/04 , C07C317/08 , C07C317/14 , C07C317/22 , C07C317/24 , C07C317/34 , C07C317/44 , C07C2601/10 , C07C2602/42 , C07D207/452 , C07D213/76 , C07D219/10 , C07D231/18 , C07D233/90 , C07D239/60 , C07D241/42 , C07D249/04 , C07D249/10 , C07D249/12 , C07D251/70 , C07D277/64 , C07D277/82 , C07D285/125 , C07D285/135 , C07D285/15 , C07D285/16 , C07D303/34 , C07D307/54 , C07D307/64 , C07D311/52 , C07D311/58 , C07D311/82 , C07D319/06 , C07D333/16 , C07D333/24 , C07D405/06 , C07D409/12 , C07D417/10 , C07D417/14 , C07F17/02 , C08F4/04 , C08G65/3344 , C09B69/00 , C09B69/02 , C09B69/10 , G02F1/1525 , G02F2001/1518 , H01B1/122 , H01B1/128 , H01G9/022 , H01G9/038 , H01G11/02 , H01G11/62 , H01M4/00 , H01M4/02 , H01M4/131 , H01M4/133 , H01M4/134 , H01M4/382 , H01M4/405 , H01M4/48 , H01M4/485 , H01M4/505 , H01M4/525 , H01M4/5815 , H01M4/5825 , H01M4/60 , H01M4/625 , H01M4/661 , H01M6/00 , H01M6/04 , H01M6/164 , H01M6/166 , H01M6/168 , H01M6/181 , H01M6/183 , H01M10/052 , H01M10/0525 , H01M10/0565 , H01M10/0567 , H01M10/0568 , Y02E60/13 , Y10S430/127 , Y10T29/49108 , Y10T428/2918 , C07C49/84 , C07C49/553
摘要: The invention concerns ionic compounds in which the anionic load has been delocalized. A compound disclosed by the invention is comprised of an amide or one of its salts, including an anionic portion combined with at least one cationic portion M+m in sufficient numbers to ensure overall electronic neutrality; is the compound is further comprised of M as a hydroxonium, a nitrosonium NO+, an ammonium —NH4+, a metallic cation with the valence m, an organic cation with the valence m, or an organometallic cation with the valence m. The anionic portion matches the formula RF—SOx—N-Z, wherein RF is a perfluorinated group, x is 1 or 2, and Z is an electroattractive substituent. The compounds can be used notably for ionic conducting materials, electronic conducting materials, colorants, and the catalysis of various chemical reactions.
摘要翻译: 本发明涉及其中阴离子负荷已经离域的离子化合物。 本发明公开的化合物由酰胺或其盐之一组成,包括与至少一个阳离子部分M + m结合的阴离子部分,其数目足以确保整个电子中性; 化合物还包含M为氢氧化物,亚硝酸铵NO,铵NH4 +,价数m的金属阳离子,价数为m的有机阳离子或价数m的有机金属阳离子。 阴离子部分与式RF-SOx-N-Z匹配,其中RF是全氟化基团,x是1或2,Z是电致吸收取代基。 该化合物特别用于离子导电材料,电子导电材料,着色剂和各种化学反应的催化。
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公开(公告)号:US20050004086A1
公开(公告)日:2005-01-06
申请号:US10825084
申请日:2004-04-15
申请人: Jeffery Raymond , Kang Han , Yuanlin Zhou , Yuehua He , Bradley Noren , James Yee
发明人: Jeffery Raymond , Kang Han , Yuanlin Zhou , Yuehua He , Bradley Noren , James Yee
IPC分类号: C07C35/21 , C07C35/32 , C07C69/013 , C07C69/03 , C07C311/04 , C07D211/58 , C07D213/30 , C07D213/38 , C07D213/74 , C07D233/54 , C07D233/56 , C07D295/096 , C07D307/66 , C07D317/66 , A61K31/56 , A61K31/155 , A61K31/18 , A61K31/19 , A61K31/40 , A61K31/44
CPC分类号: C07C35/32 , C07C35/14 , C07C35/21 , C07C51/083 , C07C51/347 , C07C62/34 , C07C69/013 , C07C213/00 , C07C213/08 , C07C215/42 , C07C233/18 , C07C233/21 , C07C233/72 , C07C247/14 , C07C279/08 , C07C311/04 , C07C315/00 , C07C2601/14 , C07C2602/08 , C07C2602/24 , C07D207/335 , C07D211/58 , C07D213/30 , C07D213/38 , C07D213/74 , C07D233/54 , C07D233/64 , C07D295/096 , C07D307/66 , C07D317/66 , C07D317/70 , Y10S514/825 , Y10S514/826 , Y10S514/863
摘要: Compounds of formula (Ia): wherein R1, R2, R3, R4a, R4b, R5 and R6 are defined herein, as well as other indene derivatives are disclosed herein. Pharmaceutical compositions containing the compounds and methods of using the compounds are also disclosed.
摘要翻译: 式(Ia)化合物:其中R 1,R 2,R 3,R 4a,R 4b,R 5和R 6在本文中定义,以及其它 茚衍生物在本文中公开。 还公开了含有化合物的药物组合物和使用该化合物的方法。
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公开(公告)号:US20020183286A1
公开(公告)日:2002-12-05
申请号:US10098815
申请日:2002-03-15
发明人: Paul Calabresi , Bai-Chuan Pan , James Darnowski
IPC分类号: A61K031/655 , C07C311/29 , C07C311/04
CPC分类号: A61K31/506 , A61K31/18 , A61K31/205 , A61K31/505
摘要: The invention provides a method of inhibiting tumor growth by contacting the tumor with a composition containing a taurine compound. The composition is administered to directly contact a tumor cell at a dose sufficient to induce cell death.
摘要翻译: 本发明提供了通过使肿瘤与含有牛磺酸化合物的组合物接触来抑制肿瘤生长的方法。 施用组合物以足以诱导细胞死亡的剂量直接接触肿瘤细胞。
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10.Substituted alpha-aminosulphonyl-acetohydroxamic acids as therapeutic agents 失效
标题翻译: 取代的α-氨基磺酰基 - 乙酰肟酸作为治疗剂公开(公告)号:US6090852A
公开(公告)日:2000-07-18
申请号:US233883
申请日:1999-01-20
IPC分类号: C12N9/99 , A61K31/00 , A61K31/18 , A61P1/00 , A61P1/02 , A61P9/00 , A61P9/04 , A61P9/10 , A61P17/00 , A61P17/02 , A61P19/00 , A61P19/02 , A61P27/00 , A61P27/02 , A61P29/00 , A61P35/00 , A61P35/04 , A61P43/00 , C07C311/03 , C07C311/04 , C07C311/06 , A61K31/16 , C07C239/08
CPC分类号: C07C311/04 , C07C311/03 , C07C311/06 , Y10S514/821 , Y10S514/824 , Y10S514/825
摘要: Compounds of formula (I): ##STR1## where the substituents are as defined herein, and salts thereof, are matrix metalloprotease inhibitors.
摘要翻译: 式(I)化合物:其中取代基如本文所定义,及其盐是基质金属蛋白酶抑制剂。
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