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1. 发明授权

US08030524B2 Organic compounds 有权
标题翻译：有机化合物
公开(公告)号：US08030524B2
公开(公告)日：2011-10-04
申请号：US12513263
申请日：2007-11-02
申请人： Jerzy A. Bajgrowicz
发明人： Jerzy A. Bajgrowicz
IPC分类号： C07C49/105
CPC分类号： C07C31/13 , C07C2601/02 , C07C2601/08 , C11B9/003
摘要： Described are 2,2,3-trimethylcyclopentane derivatives of formula 1 wherein R1 is methyl or ethyl; and R2 is hydrogen, methyl or ethyl. The invention furthermore relates to a method of their production a to fragrance compositions comprising them.
摘要翻译：描述了式1的2,2,3-三甲基环戊烷衍生物，其中R 1是甲基或乙基; 并且R 2是氢，甲基或乙基。本发明还涉及一种制备包含它们的香料组合物的方法。

2. 发明申请

US20090036684A1 METHOD FOR PRODUCING 4-OXOQUINOLINE COMPOUND 有权
标题翻译：生产4-氧杂环戊烯化合物的方法
公开(公告)号：US20090036684A1
公开(公告)日：2009-02-05
申请号：US12281889
申请日：2007-03-06
申请人： Koji Matsuda , Koji Ando , Shigeki Ohki , Jun-ichi Hoshi , Takahiro Yamasaki
发明人： Koji Matsuda , Koji Ando , Shigeki Ohki , Jun-ichi Hoshi , Takahiro Yamasaki
IPC分类号： C07D215/00 , C07C69/76 , C07C65/00 , C07C49/105
CPC分类号： C07C229/30 , C07C43/215 , C07C57/72 , C07C57/76 , C07C61/40 , C07C67/333 , C07C67/343 , C07C69/708 , C07C69/716 , C07C69/738 , C07C69/92 , C07C69/94 , C07C229/34 , C07D215/56
摘要： The present invention provides a compound useful as a synthetic intermediate for an anti-HIV agent having an integrase inhibitory activity, and a production method thereof, and a production method of an anti-HIV agent using the synthetic intermediate. Specifically, for example, a compound represented by the formula (2′): wherein R is a fluorine atom or a methoxy group, and R400 is a hydrogen atom or a C1-C4 alkyl group, or a salt thereof, and a production method thereof, and a production method of an anti-HIV agent using the synthetic intermediate.
摘要翻译：本发明提供了可用作具有整合酶抑制活性的抗HIV剂的合成中间体的化合物及其制备方法，以及使用该合成中间体的抗HIV剂的制备方法。具体而言，例如，式（2'）表示的化合物或其盐，其中R为氟原子或甲氧基，R400为氢原子或C1-C4烷基，以及使用该合成中间体的抗HIV剂的制造方法。

3. 发明申请

US20050085557A1 Therapeutic procedures 审中-公开
标题翻译：治疗方法
公开(公告)号：US20050085557A1
公开(公告)日：2005-04-21
申请号：US10934795
申请日：2004-09-03
申请人： Paul Wentworth , Richard Lerner
发明人： Paul Wentworth , Richard Lerner
IPC分类号： A61K31/12 , A61K31/56 , A61K31/575 , A61K39/385 , A61K39/44 , C07C49/105 , C07C49/403 , C07C49/507 , C07C49/633 , C07D313/04 , C07J9/00 , C07J61/00
CPC分类号： C07J61/00 , C07C49/523 , C07C49/757 , C07C59/353 , C07D313/04 , C07J9/00 , C07J9/005
摘要： As illustrated herein, cholesterol is oxidized when it is present in atherosclerotic plaques. This reaction generates cytotoxic cholesterol oxidation or ozonation products. The present application is directed to the products of cholesterol ozonation, binding entities directed against such products, and methods of using such binding entities and cytotoxins to treat a variety of diseases.
摘要翻译：如本文所示，当胆固醇存在于动脉粥样硬化斑块中时，胆固醇被氧化。该反应产生细胞毒性胆固醇氧化或臭氧化产物。本申请涉及胆固醇臭氧化产物，针对这些产品的结合实体，以及使用这些结合实体和细胞毒素治疗各种疾病的方法。

4. 发明授权

US6040475A Intermediate compounds for making metabolites of lycopene 失效
标题翻译：用于制备番茄红素代谢物的中间体化合物
公开(公告)号：US6040475A
公开(公告)日：2000-03-21
申请号：US310280
申请日：1999-05-12
申请人： Hanspeter Pfander , Bruno Traber
发明人： Hanspeter Pfander , Bruno Traber
IPC分类号： C07C27/02 , A61P43/00 , C07C29/00 , C07C29/32 , C07C29/36 , C07C29/44 , C07C29/46 , C07C33/12 , C07C35/06 , C07C45/68 , C07C47/02 , C07C47/198 , C07C47/21 , C07C47/267 , C07C49/105 , C07C49/203 , C07C49/24 , C07C67/02 , C07C67/29 , C07C69/02 , C07C69/14 , C07C69/16 , C07F7/04 , C07F7/08 , C07F7/18 , C07F9/28 , C07F9/54
CPC分类号： C07C29/32 , C07C35/06 , C07C45/68 , C07C47/267 , C07C67/29 , C07F9/5435 , C07B2200/07 , C07C2101/08
摘要： This invention is concerned with the synthesis of 3-(1-acetoxy-1-methylethyl)-6-oxo-heptanal; 3-(1-acetoxy-1-methylethyl)-2-formyl-1-methyl-cyclopentanol; 5-[2-hydroxy-5-(1-hydroxy-1-methylethyl)-2-methyl-2-cyclopentyl]-3-methyl-penta-2,4-dien-1-ol and 2,7,11-trimethyl-13-[2-hydroxy-5-(1-hydroxy-1-methylethyl)-2-methyl-cyclopentyl]-trideca-2,4,6,8,10,12-hexaenal which are useful as intermediates for the synthesis of lycopene metabolites.
摘要翻译：本发明涉及3-（1-乙酰氧基-1-甲基乙基）-6-氧代 - 庚醛的合成; 3-（1-乙酰氧基-1-甲基乙基）-2-甲酰基-1-甲基 - 环戊醇; 5- [2-羟基-5-（1-羟基-1-甲基乙基）-2-甲基-2-环戊基] -3-甲基 - 戊-2,4-二烯-1-醇和2,7,11- 三甲基-13- [2-羟基-1-甲基乙基] -2-甲基 - 环戊基] - 十三烷-2,4,6,8,10,12-六烯酸，它们可用作合成番茄红素代谢物。

5. 发明授权

US6030962A Vitamin D.sub.3 analogs with bis C-20 side chains 失效
标题翻译：维生素D3类似物与双C-20侧链
公开(公告)号：US6030962A
公开(公告)日：2000-02-29
申请号：US61664
申请日：1998-04-16
申请人： Percy Sarwood Manchand , Milan Radoje Uskokovic
发明人： Percy Sarwood Manchand , Milan Radoje Uskokovic
IPC分类号： A61K20060101 , C07C20060101 , C07C45/74 , C07C47/21 , C07C401/00 , C07F7/18 , A01N45/00 , C07C49/105
CPC分类号： C07C45/74 , C07C47/21 , C07F7/1856
摘要： This invention provides Vitamin D.sub.3 analogs of the Formula I ##STR1## wherein: X is H.sub.2 or CH.sub.2 ;Y is hydrogen, hydroxy or fluorine;Z is hydroxy;R.sub.1 and R.sub.2 are a (C.sub.1 -C.sub.4) alkyl or fluoroalkyl, or R.sub.1 and R.sub.2 together with C.sub.25 form a (C.sub.3 -C.sub.6) cycloalkyl or cyclofluoroalkyl;R.sub.3 and R.sub.4 are a (C.sub.1 -C.sub.4) alkyl or fluoroalkyl, or R.sub.3 and R.sub.4 together with C.sub.25, form a (C.sub.3 -C.sub.6)cycloalkyl or cyclofluoroalkyl;A is a single bond or a double bond;B.sub.1 is a single bond, an E-double bond, a Z-double bond or a triple bond; andB.sub.2 is a single bond, an E-double bond, a Z-double bond or a triple bond; and prodrugs thereof, intermediates and methods for preparation of these analogs, pharmaceutical compositions containing such analogs and methods for treatment of osteoporosis, hyperparathyroidism and autoimmune diseases.
摘要翻译：本发明提供式I的维生素D3类似物，其中：X是H 2或CH 2; Y是氢，羟基或氟; Z是羟基; R1和R2是（C1-C4）烷基或氟烷基，或R1和R2与C25一起形成（C 3 -C 6）环烷基或环氟烷基; R3和R4是（C1-C4）烷基或氟烷基，或R3和R4与C25一起形成（C 3 -C 6）环烷基或环氟烷基; A是单键或双键; B1是单键，E-双键，Z-双键或三键; B2是单键，E-双键，Z-双键或三键; 其前体药物，制备这些类似物的中间体和方法，含有这些类似物的药物组合物和治疗骨质疏松症，甲状旁腺功能亢进症和自身免疫性疾病的方法。

6. 发明授权

US4060639A Broad spectrum antibacterial compositions containing tris-(hydroxymethyl)-aminoethane and dicycloaliphatic-alkyl polyamines 失效
标题翻译：含有三（羟甲基） - 氨基乙烷和二环脂肪族 - 烷基多胺的广谱抗菌组合物
公开(公告)号：US4060639A
公开(公告)日：1977-11-29
申请号：US686428
申请日：1976-05-14
申请人： David P. Jacobus , Eugene L. Dulaney , Nathaniel Grier
发明人： David P. Jacobus , Eugene L. Dulaney , Nathaniel Grier
IPC分类号： A01N33/04 , A01N33/08 , C07C45/00 , C07C45/48 , C07C49/105 , C07C49/21 , A01N9/02 , A01N9/20 , A01N9/22
CPC分类号： C07C49/21 , A01N33/04 , A01N33/08 , C07C45/004 , C07C45/48 , C07C49/105
摘要： A composition comprising tris-(hydroxymethyl)aminomethane and dicyclohexyl-, dicyclohexenyl- and cyclohexylcyclohexenyl-alkyl polyamines, their acid addition salts, and mixtures thereof are useful as antibacterial agents. The composition is particularly useful because of the synergistic improvement obtained against strains of the genus Pseudomonas, as well as other genera.
摘要翻译：包含三 - （羟甲基）氨基甲烷和二环己基 - ，二环己烯基和环己基环己烯基 - 烷基多胺，其酸加成盐及其混合物的组合物可用作抗菌剂。该组合物特别有用，因为针对假单胞菌属的菌株以及其他属获得了协同的改进。

7. 发明授权

US4049417A Alicyclic alkylene polyamine microorganism and algae growth inhibitors 失效
标题翻译：脂环族亚胺多胺微生物和藻类生长抑制剂
公开(公告)号：US4049417A
公开(公告)日：1977-09-20
申请号：US664612
申请日：1976-03-08
申请人： Bruce E. Witzel , Nathaniel Grier , Richard A. Dybas , Robert A. Strelitz
发明人： Bruce E. Witzel , Nathaniel Grier , Richard A. Dybas , Robert A. Strelitz
IPC分类号： C07C45/00 , C07C45/48 , C07C49/105 , C07C49/21 , C07D295/13 , A01N9/20 , A61K31/13 , C07C87/40 , C07C87/45
CPC分类号： C07D295/13 , C07C45/004 , C07C45/48 , C07C49/105 , C07C49/21
摘要： Novel dicyclohexyl, dicyclohexenyl and cyclohexylcyclohexenylalkyl polyamines are useful antimicrobial agents, as well as algae inhibitors. They are especially useful in agriculture to protect plants against diseases such as leaf, stem, and fruit spotting, internal discoloration and decay of fruits and vegetables. These compounds are particularly active against diseases caused by the genera Pseudomonas, Xanthomonas, Erwinia, and Corynebacterium.
摘要翻译：新型二环己基，二环己烯基和环己基环己烯基烷基多胺是有用的抗微生物剂，以及藻类抑制剂。它们特别适用于农业，以保护植物免受诸如叶，茎和果实斑点，水果和蔬菜的内部变色和腐烂等疾病的影响。这些化合物对由假单胞菌属，黄单胞菌属，欧文氏菌属和棒状杆菌属引起的疾病特别有活性。

8. 发明授权

US07521581B2 Catalyst composition and process for producing cross-coupled compound using same 有权
标题翻译：催化剂组合物和使用其制备交联化合物的方法
公开(公告)号：US07521581B2
公开(公告)日：2009-04-21
申请号：US11391567
申请日：2006-03-29
申请人： Shinichi Ishikawa , Hiroshi Awano , Hirokazu Yano , Hisao Equchi
发明人： Shinichi Ishikawa , Hiroshi Awano , Hirokazu Yano , Hisao Equchi
IPC分类号： C07C49/105
CPC分类号： C07C41/30 , B01J31/1805 , B01J31/2404 , B01J2231/4211 , B01J2531/847 , C07B37/04 , C07C1/321 , C07C17/263 , C07C43/215 , C07C253/30 , C07F15/045 , C07C15/52 , C07C15/14 , C07C22/08 , C07C255/54 , C07C43/205
摘要： A catalyst composition for a cross-coupling reaction comprising a nickel salt-amine complex of formula (1), and triphenylphosphine. where R1 thru R4 independently represent alkyl, aryl, heteroaryl or alkenyl; n is an integer of 1-6; and X independently represents halo, hydroxyl, nitrate or acetate group. Using the catalyst composition, a cross-coupling reaction is carried out between a boron-containing compound of formula (2) and a compound of formula (3). where R5 and R6 are the same as R1-R4 defined above; Y independently represents hydroxyl or alkoxy, Z is halo, methanesulfonate or trifluoromethanesulfonate.
摘要翻译：包含式（1）的镍盐 - 胺络合物和三苯基膦的用于交叉偶联反应的催化剂组合物。其中R 1至R 4独立地表示烷基，芳基，杂芳基或烯基; n为1-6的整数; X独立地表示卤素，羟基，硝酸根或乙酸基。使用催化剂组合物，在式（2）的含硼化合物和式（3）的化合物之间进行交叉偶联反应。其中R5和R6与上述定义的R1-R4相同; Y独立地表示羟基或烷氧基，Z是卤素，甲磺酸酯或三氟甲磺酸酯。

9. 发明授权

US07223803B2 Polyethylene (glycol) derivatives with proximal reactive groups 有权
标题翻译：具有近端反应性基团的聚乙烯（二醇）衍生物
公开(公告)号：US07223803B2
公开(公告)日：2007-05-29
申请号：US11314912
申请日：2005-12-21
申请人： J. Milton Harris , Antoni Kozlowski
发明人： J. Milton Harris , Antoni Kozlowski
IPC分类号： C08K3/20 , C08F116/06 , C07C49/00 , C07C49/105 , C07C49/21
CPC分类号： C08G65/33396 , A61K47/60 , C08G65/329 , C08G65/33313 , C08G65/33337 , Y10S530/816
摘要： An activated, substantially water soluble poly(ethylene glycol) is provided having of a linear or branched poly(ethylene glycol) backbone and at least one terminus linked to the backbone through a hydrolytically stable linkage, wherein the terminus is branched and has proximal reactive groups. The free reactive groups are capable of reacting with active moieties in a biologically active agent such as a protein or peptide thus forming conjugates between the activated poly(ethylene glycol) and the biologically active agent.
摘要翻译：提供活化的基本上水溶性的聚（乙二醇），其具有直链或支链的聚（乙二醇）主链和至少一个通过水解稳定键连接至主链的末端，其中末端是支链的且具有近端反应性基团。自由活性基团能够与生物活性剂如蛋白质或肽中的活性部分反应，从而在活化的聚（乙二醇）与生物活性剂之间形成共轭物。

10. 发明申请

US20060205808A1 Anti-inflammatory and cure for ageing, Alzheimer's disease on phloroglucinol derivatives 审中-公开
标题翻译：消炎和治愈老化，阿尔茨海默病对间苯三酚衍生物
公开(公告)号：US20060205808A1
公开(公告)日：2006-09-14
申请号：US11078194
申请日：2005-03-10
申请人： Chun-Nan Lin , Jih-Pyang Wang , Jing-Ru Weng
发明人： Chun-Nan Lin , Jih-Pyang Wang , Jing-Ru Weng
IPC分类号： A61K31/343 , C07C49/105 , C07D307/92 , A61K31/12
CPC分类号： C07D307/92 , C07C49/743 , C07D307/80
摘要： The fresh seeds obtained from the fresh fruits of Garcinia subelliptica, were extracted with chloroform at room temperature. The CHCl3 extract was concentrated under reduced pressure to afford a brown residue. This residue was subjected to column chromatography (silica gel) and eluted with appropriate solvent system to give two phloroglucinol derivatives (Compounds 1 and 4). Compound 1 exhibited potent inhibitory effects on the release of β-glucuronidase and lysozyme from rat neutrophils stimulated with formyl-Met-Leu-Phe(fMLP)/cyto-chalasin B (CB). Compound 1 also exhibited potent inhibitory effect on the superoxide anion generation in rat neutrophils stimulated with fMLP/CB. Compound 4 exhibited potent inhibitory effect on NO production in lipopolysaccharide (LPS)/interferon-γ (IFN-γ)-activation in N9 cells. These Compounds may be developed as anti-inflammatory, anti-cancer agent, cure for ageing, and Alzheimer's disease treatment drugs.
摘要翻译：从藤黄新鲜果实中获得的新鲜种子在室温下用氯仿萃取。将CHCl 3萃取物在减压下浓缩，得到棕色残余物。将该残余物进行柱色谱法（硅胶），并用合适的溶剂系统洗脱，得到两种间苯三酚衍生物（化合物1和4）。化合物1对用甲酰-Mly-Leu-Phe（fMLP）/细胞色素B（CB）刺激的大鼠嗜中性粒细胞释放β-葡糖苷酸酶和溶菌酶具有有效的抑制作用。化合物1还对用fMLP / CB刺激的大鼠嗜中性粒细胞中的超氧阴离子产生表现出有效的抑制作用。化合物4对N9细胞中脂多糖（LPS）/干扰素-γ（IFN-γ）活化的NO产生表现出有效的抑制作用。这些化合物可以被开发为抗炎，抗癌剂，治愈老化和阿尔茨海默病治疗药物。

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