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1. 发明授权

US09527807B2 Sulfonamide derivative and use thereof 有权
标题翻译：磺酰胺衍生物及其用途
公开(公告)号：US09527807B2
公开(公告)日：2016-12-27
申请号：US14009456
申请日：2012-04-05
申请人： Shoji Fukumoto , Osamu Ujikawa , Shinji Morimoto , Yasutomi Asano , Satoshi Mikami , Norihito Tokunaga , Masakuni Kori , Toshihiro Imaeda , Koichiro Fukuda , Shinji Nakamura , Kouichi Iwanaga
发明人： Shoji Fukumoto , Osamu Ujikawa , Shinji Morimoto , Yasutomi Asano , Satoshi Mikami , Norihito Tokunaga , Masakuni Kori , Toshihiro Imaeda , Koichiro Fukuda , Shinji Nakamura , Kouichi Iwanaga
IPC分类号： C07C311/07 , C07D401/12 , C07D309/14 , C07D295/092 , C07D333/16 , C07D231/12 , C07D211/58 , C07C311/09 , C07C311/14 , C07C317/28 , C07C323/26 , C07D209/04 , C07D213/64 , C07D231/14 , C07D233/68 , C07D261/08 , C07D263/32 , C07D277/24 , C07D277/62 , C07D307/22 , C07D405/12 , C07D413/12 , C07D417/12 , C07D405/14 , C07D309/06 , C07D213/85 , C07D401/04 , C07D237/04 , C07D239/28 , C07D409/12 , C07D493/08 , C07D207/27 , C07D207/273 , C07D277/32 , C07D211/56 , C07D211/76 , C07D295/192 , C07D213/61 , C07D305/06 , C07D233/56
CPC分类号： C07C311/07 , C07C311/09 , C07C311/14 , C07C317/28 , C07C323/26 , C07C2601/02 , C07C2601/08 , C07C2601/14 , C07C2603/74 , C07D207/27 , C07D207/273 , C07D209/04 , C07D211/56 , C07D211/58 , C07D211/76 , C07D213/61 , C07D213/64 , C07D213/85 , C07D231/12 , C07D231/14 , C07D233/56 , C07D233/68 , C07D237/04 , C07D239/28 , C07D261/08 , C07D263/32 , C07D277/24 , C07D277/32 , C07D277/62 , C07D295/092 , C07D295/192 , C07D305/06 , C07D307/22 , C07D309/06 , C07D309/14 , C07D333/16 , C07D401/04 , C07D401/12 , C07D405/12 , C07D405/14 , C07D409/12 , C07D413/12 , C07D417/12 , C07D493/08
摘要： Provided is a compound having an AMPA receptor function enhancing action, and useful as a prophylactic or therapeutic drug for depression, Alzheimer's disease, schizophrenia, attention deficit hyperactivity disorder (ADHD) and the like. A compound represented by the formula (I): wherein each symbol is as defined in the present specification, or a salt thereof.
摘要翻译：提供具有AMPA受体功能增强作用的化合物，可用作抑郁症，阿尔茨海默氏病，精神分裂症，注意力缺陷多动障碍（ADHD）等的预防或治疗药物。由式（I）表示的化合物或其盐，其中每个符号如本说明书中所定义。

2. 发明授权

US09517989B2 2-cycloalkyl resorcinol cannabinergic ligands 有权
标题翻译： 2-环烷基间苯二酚大麻素能配体
公开(公告)号：US09517989B2
公开(公告)日：2016-12-13
申请号：US14436865
申请日：2013-10-17
申请人： Northeastern University
发明人： Alexandros Makriyannis , Marsha R. D'Souza , Shama Bajaj , Spyridon P. Nikas , Ganeshsingh A. Thakur
IPC分类号： C07C39/23 , C07C69/16 , C07C69/18 , C07D311/78 , C07D309/06 , C07C69/63 , C07C39/42 , C07C43/168 , C07D339/06 , C07C47/27 , C07C47/46 , C07C49/747 , C07D295/092 , C07C62/32 , C07C235/40 , C07C247/06 , C07C255/36 , C07C255/38 , C07C43/178 , C07C49/603 , C07C245/24 , C07D295/096 , C07D295/192
CPC分类号： C07C39/23 , C07C39/42 , C07C43/168 , C07C43/1788 , C07C47/27 , C07C47/46 , C07C49/603 , C07C49/747 , C07C62/32 , C07C69/16 , C07C69/18 , C07C69/63 , C07C235/40 , C07C245/24 , C07C247/06 , C07C255/36 , C07C255/38 , C07C2601/02 , C07C2601/04 , C07C2601/08 , C07C2601/14 , C07C2601/16 , C07C2602/42 , C07C2603/04 , C07C2603/74 , C07D295/092 , C07D295/096 , C07D295/192 , C07D309/06 , C07D311/78 , C07D339/06
摘要： The present invention relates to novel 2-cycloalkyl resorcinol compounds; to pharmaceutical compositions comprising the compounds; and to methods of preparing the compounds and uses thereof. The disclosed compounds can bind to and modulate the cannabinoid receptors and thus, they are specific ligands for these receptors. The invented compounds, when administered in a therapeutically effective amount to an individual or animal, results in a sufficiently high level of that compound in the individual or animal to cause a physiological response. The physiological response may be useful to treat a number of physiological conditions.
摘要翻译：本发明涉及新的2-环烷基间苯二酚化合物; 涉及包含该化合物的药物组合物; 以及制备化合物的方法及其用途。所公开的化合物可以结合并调节大麻素受体，因此它们是这些受体的特异性配体。当以治疗有效量施用于个体或动物时，本发明的化合物在个体或动物中导致足够高的该化合物水平以引起生理反应。生理反应可用于治疗许多生理条件。

3. 发明授权

US08748608B2 4-phenylpiperazine derivatives with functionalized linkers as dopamine D3 receptor selective ligands and methods of use 有权
标题翻译：具有官能化接头的4-苯基哌嗪衍生物作为多巴胺D3受体选择性配体和使用方法
公开(公告)号：US08748608B2
公开(公告)日：2014-06-10
申请号：US12664668
申请日：2007-06-15
申请人： Amy Hauck Newman , Peter Grundt , George C. Cyriac , Robert Luedtke , Jianjing Cao
发明人： Amy Hauck Newman , Peter Grundt , George C. Cyriac , Robert Luedtke , Jianjing Cao
IPC分类号： C07D213/56 , C07D209/42 , C07D295/145 , C07D295/15 , C07D307/85
CPC分类号： C07D307/85 , C07D209/42 , C07D209/48 , C07D213/56 , C07D213/64 , C07D213/81 , C07D213/89 , C07D295/092 , C07D295/096 , C07D295/13 , C07D295/145 , C07D333/70 , G01N33/566
摘要： Dopamine D3 receptor antagonists and partial agonists are known to modulate the reinforcing and drug-seeking effects induced by cocaine and other abused substances. By introducing functionality into the butylamide linking chain of the 4-phenylpiperazine class of ligands, improved D3 receptor affinity and selectivity, as well as water solubility, is achieved. A series of linking-chain derivatives are disclosed wherein functionality such as OH or OAc groups have been introduced into the linking chain. In general, these modifications are well tolerated at D3 receptors and achieve high selectivity over D2 and D4 receptors.
摘要翻译：已知多巴胺D3受体拮抗剂和部分激动剂调节可卡因和其他滥用物质诱导的增强和寻求药物作用。通过将功能性引入4-苯基哌嗪类配体的丁酰胺连接链中，实现了改善的D3受体亲和力和选择性以及水溶性。公开了一系列连接链衍生物，其中诸如OH或OAc基团的官能团已被引入连接链。通常，这些修饰在D3受体上具有良好的耐受性，并且相对于D2和D4受体实现高选择性。

4. 发明授权

US07745626B2 Stereoselective alkylation of chiral 2-methyl-4-protected piperazines 失效
标题翻译：手性2-甲基-4-保护的哌嗪的立体选择性烷基化
公开(公告)号：US07745626B2
公开(公告)日：2010-06-29
申请号：US11089858
申请日：2005-03-25
申请人： Wenxue Wu , Hongbiao Liao , David J. Tsai , David R. Andrews , Dinesh Gala , Gary M. Lee , Martin Lawrence Schwartz , Timothy L. McAllister , Xiaoyong Fu , Donal Maloney , Tiruvettipuram K. Thiruvengadam , Chou-Hang Tann
发明人： Wenxue Wu , Hongbiao Liao , David J. Tsai , David R. Andrews , Dinesh Gala , Gary M. Lee , Martin Lawrence Schwartz , Timothy L. McAllister , Xiaoyong Fu , Donal Maloney , Tiruvettipuram K. Thiruvengadam , Chou-Hang Tann
IPC分类号： C07D295/023
CPC分类号： C07D295/185 , C07B2200/07 , C07C45/512 , C07C67/343 , C07C309/73 , C07D295/088 , C07D295/092 , C07D295/192 , C07D295/205 , C07C49/255 , C07C69/734 , C07C49/84
摘要： In an illustrative embodiment, the present invention describes the synthesis of the following compound and similar compounds, in high stereochemical purity by a novel stereoselective alkylation process:
摘要翻译：在说明性实施方案中，本发明通过新的立体选择性烷基化方法描述了具有高立体化学纯度的以下化合物和类似化合物的合成：

5. 发明申请

US20100035959A1 Novel sphingosine kinase type 1 inhibitors, compositions and processes for using same 有权
标题翻译：新型鞘氨醇激酶1型抑制剂，组合物及其使用方法
公开(公告)号：US20100035959A1
公开(公告)日：2010-02-11
申请号：US12387228
申请日：2009-04-29
申请人： Robert Elliot Zipkin , Sarah Spiegel , Jeffrey Kroll Adams
发明人： Robert Elliot Zipkin , Sarah Spiegel , Jeffrey Kroll Adams
IPC分类号： A61K31/40 , C07C215/00 , C12N5/00 , A61K31/135 , C07D207/04 , A61P35/00 , A61P37/00
CPC分类号： A61K31/135 , A61K31/40 , C07C215/28 , C07C323/32 , C07D263/06 , C07D295/092
摘要： Provided are novel compositions which uniquely inhibit sphingosine kinase Type 1 (SphK1) and which are useful in a number of applications including killing or damaging cancer cells, inducing apoptosis, inhibiting growth, metastasis and development of chemoresistance in cancer cells, leukemia, increasing the effectiveness of anti-cancer agents, attenuating immune reactivity, inhibiting survival signaling in cancer cells, and reducing symptoms of multiple sclerosis.
摘要翻译：提供了唯一抑制鞘氨醇激酶1型（SphK1）的新型组合物，其可用于许多应用，包括杀死或损害癌细胞，诱导细胞凋亡，抑制癌细胞中的生长，转移和化学耐药性的发展，增加其有效性的抗癌剂，减轻免疫反应性，抑制癌细胞中的存活信号，并减少多发性硬化症状。

6. 发明申请

US20090018118A1 HETEROCYCLIC COMPOUNDS 审中-公开
标题翻译：杂环化合物
公开(公告)号：US20090018118A1
公开(公告)日：2009-01-15
申请号：US12159409
申请日：2006-12-27
申请人： Uros Urleb , Darko Kocjan , Tina Korosec , Damjana Rozman , Jure Acimovic , Alenka Tomazic , Breda Rode
发明人： Uros Urleb , Darko Kocjan , Tina Korosec , Damjana Rozman , Jure Acimovic , Alenka Tomazic , Breda Rode
IPC分类号： A61K31/551 , C07D401/14 , A61K31/496 , C07D401/06 , A61K31/5377 , C07D401/04
CPC分类号： C07D295/092 , C07D213/30 , C07D213/74 , C07D213/89 , C07D295/088
摘要： The invention is related to novel substituted diazaheterocycles useful as effective antihypercholesterolemic agents, methods of their preparation, and pharmaceutical compositions containing them.
摘要翻译：本发明涉及可用作有效抗高胆固醇血症药的新型取代的双氮杂环，其制备方法和含有它们的药物组合物。

7. 发明授权

US07256205B2 Nitrosated and nitrosylated H2 receptor antagonist compounds, compositions and methods of use 失效
标题翻译：亚硝化和亚硝基化H 2受体拮抗剂化合物，组合物和使用方法
公开(公告)号：US07256205B2
公开(公告)日：2007-08-14
申请号：US11518231
申请日：2006-09-11
申请人： David S. Garvey , L. Gordon Letts , Chia-En Lin , Tiansheng Wang
发明人： David S. Garvey , L. Gordon Letts , Chia-En Lin , Tiansheng Wang
IPC分类号： C07D277/42 , A61K31/426
CPC分类号： C07D233/54 , C07D233/64 , C07D277/48 , C07D295/092 , C07D295/096
摘要： The invention describes novel nitrosated and/or nitrosylated H2 receptor antagonist compounds, and novel compositions comprising at least one H2 receptor antagonist compound that is optionally substituted with at least one NO and/or NO2 group, 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 at least one nonsteroidal antiinflammatory drug, antacid, bismuth-containing reagent or anti-viral agent. The invention also describes methods for treating and/or preventing gastrointestinal disorders; improving gastroprotective properties of H2 receptor antagonists; decreasing the recurrence of ulcers; facilitating ulcer healing; preventing and/or treating inflammations and microbial infections, ophthalmic diseases and disorders, multiple sclerosis, and viral infections; and decreasing or reducing the gastrointestinal toxicity associated with the use of nonsteroidal antiinflammatory compounds.
摘要翻译：本发明描述了新的亚硝化和/或亚硝基化的H 2 O 2受体拮抗剂化合物，以及包含至少一种H 2受体拮抗剂化合物的新组合物，其任选被至少一个NO 和/或NO 2个基团，以及任选地，至少一种捐赠，转移或释放一氧化氮的化合物，刺激一氧化氮的内源性合成，提高内源性内皮水平的内源性松弛因子，或者是一氧化氮合酶的底物和/或至少一种非甾体抗炎药，抗酸剂，含铋试剂或抗病毒剂。本发明还描述了治疗和/或预防胃肠道疾病的方法; 改善H 2受体拮抗剂的胃保护性质; 减少溃疡复发; 促进溃疡愈合; 预防和/或治疗炎症和微生物感染，眼科疾病和病症，多发性硬化和病毒感染; 并减少或减少与使用非甾体抗炎化合物相关的胃肠道毒性。

8. 发明申请

US20070135449A1 Process for selective synthesis of enantiomers of substituted 1-(2-amino-1-phenyl-ethyl)-cyclohexanols 失效
标题翻译：选择性合成取代的1-（2-氨基-1-苯基 - 乙基） - 环己醇的对映异构体的方法
公开(公告)号：US20070135449A1
公开(公告)日：2007-06-14
申请号：US11633207
申请日：2006-12-04
申请人： Paige Mahaney , Madelene Antane , Jerry Sun
发明人： Paige Mahaney , Madelene Antane , Jerry Sun
IPC分类号： A61K31/495 , C07D241/04 , C07C62/30
CPC分类号： C07C213/02 , C07B2200/07 , C07C59/72 , C07C235/34 , C07C2601/14 , C07D263/26 , C07D295/092 , C07D295/096 , C07D295/185 , C07C217/74
摘要： A process for the enantioselective synthesis of an (S)— or (R)-1-[2-dimethylamino)-1-(methoxyphenyl)ethyl]cyclohexanol and analogues or salt thereof are described. The method involves the steps of (a) reacting an (S) or (R) 4-benzyloxazolidinone with a mixed anhydride of a methyoxyphenylacetic acid under conditions which form a oxazolidinone, (4S)— or (4R)-4-benzyl-3-[methyoxyphenyl]acetyl]-oxazolidin-2-one, (b) treating the (4S)— or (4R)-4-benzyl-3-[(methoxyphenyl)acetyl]-1,3-oxazolidin-2-one with an aprotic amine base and titanium chloride in a chlorinated solvent under conditions which permit formation of the corresponding anion, (c) mixing the corresponding anion with titanium chloride and cylcohexanone under conditions which permit an aldol reaction to form the corresponding (4S)— or (4R)-4-benzyl-3-[(2R)-2-(1-hydroxycyclohexyl)-2-(methoxyphenyl)acetyl]-1,3-oxazolidin-2-one, (d) hydrolyzing the (4S)— or (4R)-4-benzyl-3-[(2R)-2-(1-hydroxycyclohexyl)-2-(methoxyphenyl)acetyl]-1,3-oxazolidin-2-one to form a chiral acid (2S or 2R)-(1-hydroxycyclohexyl)-methoxyphenyl)acetic acid, (e) coupling the chiral phenylacid to a secondary amine to form an amide, and (f) reducing the amide to form an (S) or (R) 1[2-dimethylamino)-1-(methoxyphenyl)ethyl]cyclohexanol or a salt thereof.
摘要翻译：描述了（S） - 或（R）-1- [2-二甲基氨基）-1-（甲氧基苯基）乙基]环己醇及其类似物或其盐的对映选择性合成方法。该方法包括以下步骤：（S）或（R）4-苄氧基恶唑烷酮与甲氧基苯乙酸的混合酸酐在形成恶唑烷酮，（4S） - 或（4R）-4-苄基-3 - [甲氧基苯基]乙酰基] - 恶唑烷-2-酮，（b）用（4S） - 或（4R）-4-苄基-3 - [（甲氧基苯基）乙酰] -1,3-恶唑烷-2-酮处理非质子胺基和氯化钛在氯化溶剂中，在允许形成相应阴离子的条件下，（c）在允许醛醇缩合反应形成相应的（4S） - 或（ 4R）-4-苄基-3 - [（2R）-2-（1-羟基环己基）-2-（甲氧基苯基）乙酰基] -1,3-恶唑烷-2-酮，（d）水解（4S） - 或（4R）-4-苄基-3 - [（2R）-2-（1-羟基环己基）-2-（甲氧基苯基）乙酰基] -1,3-恶唑烷-2-酮以形成手性酸（2S或2R） - （1-羟基环己基） - 甲氧基苯基）乙酸，（e）将手性苯基酸偶联至仲胺以形成（f）还原酰胺以形成（S）或（R）1 [2-二甲基氨基）-1-（甲氧基苯基）乙基]环己醇或其盐。

9. 发明申请

US20070129377A1 Process for Preparing Substituted Aryl Cycloalkanol Derivatives 审中-公开
标题翻译：制备取代的芳基环烷醇衍生物的方法
公开(公告)号：US20070129377A1
公开(公告)日：2007-06-07
申请号：US11566415
申请日：2006-12-04
申请人： Alexander Gontcharov , Antonia Nikitenko , Jean Schmid , John Potoski
发明人： Alexander Gontcharov , Antonia Nikitenko , Jean Schmid , John Potoski
IPC分类号： A61K31/495 , C07D241/04
CPC分类号： C07D295/084 , C07D295/092 , H04L29/06027 , H04L65/1006 , H04L67/34 , H04L67/36
摘要： Processes are disclosed for preparing substituted aryl cycloalkanol derivatives, particularly chiral substituted aryl cycloalkanol derivatives of the general formula:
摘要翻译：公开了制备取代的芳基环烷醇衍生物的方法，特别是具有以下通式的手性取代的芳基环烷醇衍生物：

10. 发明申请

US20070004788A1 Nitrosated and nitrosylated H2 receptor antagonist compounds, compositions and methods of use 失效
公开(公告)号：US20070004788A1
公开(公告)日：2007-01-04
申请号：US11518231
申请日：2006-09-11
申请人： David Garvey , L. Letts , Chia-En Lin , Tiansheng Wang
发明人： David Garvey , L. Letts , Chia-En Lin , Tiansheng Wang
IPC分类号： A61K31/426
CPC分类号： C07D233/54 , C07D233/64 , C07D277/48 , C07D295/092 , C07D295/096
摘要： The invention describes novel nitrosated and/or nitrosylated H2 receptor antagonist compounds, and novel compositions comprising at least one H2 receptor antagonist compound that is optionally substituted with at least one NO and/or NO2 group, 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 at least one nonsteroidal antiinflammatory drug, antacid, bismuth-containing reagent or anti-viral agent. The invention also describes methods for treating and/or preventing gastrointestinal disorders; improving gastroprotective properties of H2 receptor antagonists; decreasing the recurrence of ulcers; facilitating ulcer healing; preventing and/or treating inflammations and microbial infections, ophthalmic diseases and disorders, multiple sclerosis, and viral infections; and decreasing or reducing the gastrointestinal toxicity associated with the use of nonsteroidal antiinflammatory compounds.

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