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81. 发明申请

US20100144881A1 CRYSTALLINE FORMS OF A 3-CARBOXYPROPYL-AMINOTETRALIN COMPOUND 有权
标题翻译：三羧酸 - 氨基磷酸酯化合物的结晶形式
公开(公告)号：US20100144881A1
公开(公告)日：2010-06-10
申请号：US12633944
申请日：2009-12-09
申请人： Sean M. Dalziel , Miroslav Rapta
发明人： Sean M. Dalziel , Miroslav Rapta
IPC分类号： A61K31/195 , C07C229/40 , C07C69/95 , C07C303/00 , C07C229/00 , A61P1/00
CPC分类号： C07C229/38 , C07C237/48 , C07C2601/14 , C07C2602/10
摘要： The invention provides crystalline solid forms of (S)-4-((2S,3S)-7-carbamoyl-1,1-diethyl-3-methoxy-1,2,3,4-tetrahydronaphthalen-2-ylamino)-2-cyclohexylmethyl-butyric acid. The invention also provides pharmaceutical compositions comprising such crystalline solid forms, methods of using such crystalline solid forms to treat diseases associated with mu opioid receptor activity, and processes useful for preparing such crystalline solid forms.
摘要翻译：本发明提供了（S）-4 - （（2S，3S）-7-氨甲酰基-1,1-二乙基-3-甲氧基-1,2,3,4-四氢化萘-2-基氨基）-2 环己基甲基 - 丁酸。本发明还提供包含这种结晶固体形式的药物组合物，使用这种结晶固体形式治疗与阿片样物质受体活性有关的疾病的方法，以及可用于制备这种结晶固体形式的方法。

82. 发明授权

US07709677B2 Process of preparing arylethanoldiamines 有权
标题翻译：制备芳基乙醇胺的方法
公开(公告)号：US07709677B2
公开(公告)日：2010-05-04
申请号：US12189941
申请日：2008-08-12
申请人： Jason William Beames Cooke , Bobby Neal Glover , Ronnie Maxwell Lawrence , Matthew Jude Sharp , Maria Fumiko Tymoschenko
发明人： Jason William Beames Cooke , Bobby Neal Glover , Ronnie Maxwell Lawrence , Matthew Jude Sharp , Maria Fumiko Tymoschenko
IPC分类号： C07C229/00 , C07C211/00
CPC分类号： C07D213/79 , C07C257/14 , C07D233/26 , C07D307/68
摘要： An improved process for preparing arylethanoldiamines is described. Compounds of this type are known to be useful as agonists at atypical beta-adrenoceptors (also known as beta-3-adrenoceptors).
摘要翻译：描述了制备芳基乙二胺的改进方法。已知这种类型的化合物可用作非典型β-肾上腺素能受体（也称为β-3-肾上腺素能受体）的激动剂。

83. 发明申请

US20100105097A1 TWO-PHOTON PROBE FOR REAL-TIME MONITORING OF INTRACELLULAR CALCIUM IONS, METHOD FOR PREPARING THE PROBE AND METHOD FOR REAL-TIME MONITORING OF INTRACELLULAR CALCIUM IONS USING THE PROBE, 有权
标题翻译：用于实时监测细胞内钙离子的两光子探针，用于制备探针的方法和使用探针实时监测细胞内钙离子的方法，
公开(公告)号：US20100105097A1
公开(公告)日：2010-04-29
申请号：US11997520
申请日：2008-01-21
申请人： Bong-Rae Cho
发明人： Bong-Rae Cho
IPC分类号： C12Q1/02 , C07C229/00
CPC分类号： C07C237/04 , C07C225/22 , G01N33/582
摘要： A two-photon probe for real-time monitoring of intracellular calcium ions is provided. The two-photon probe is very suitable for real-time imaging of intracellular calcium ions, shows 20-5 O-fold TPEF enhancement in response to Ca2+, has a dissociation constant (Kdτp) of 0.14±0.02 to 0.25±0.03 μM, and emits 5-fold stronger TPEF than currently available one-photon fluorescent Ca2+ probes. Unlike the previously available probes, the two-photon probe can selectively detect dynamic levels of intracellular free Ca2+ in live cells and living tissues without interference from other metal ions and from the membrane-bound probes. Moreover, the two-photon probe is capable of monitoring the calcium waves at a depth of 100-300 μm in live tissues for 1,100-4,000 s using two-photon microscopy (TPM) with no artifacts of photo-bleaching. Further provided are a method for preparing the two-photon probe and a method for real-time monitoring of intracellular calcium ions using the two-photon probe.
摘要翻译：提供了用于实时监测细胞内钙离子的双光子探针。双光子探针非常适用于细胞内钙离子的实时成像，对Ca2 +响应显示20-5 O倍TPEF增强，解离常数（Kdτp）为0.14±0.02〜0.25±0.03μM，比目前可用的单光子荧光Ca2 +探针发射5倍更强的TPEF。与以前可用的探针不同，双光子探针可以选择性地检测活细胞和活组织中细胞内游离Ca 2+的动态水平，而不受其他金属离子和膜结合探针的干扰。此外，双光子探针能够使用双光子显微镜（TPM）在活组织中监测1100-300μm深度的钙波，而不会产生光漂白。还提供了制备双光子探针的方法和使用双光子探针实时监测细胞内钙离子的方法。

84. 发明授权

US07696377B2 Stabilizer and method for stabilizing hydroxylamine, and stabilized hydroxylamine solution 失效
标题翻译：用于稳定羟胺的稳定剂和方法，以及稳定的羟胺溶液
公开(公告)号：US07696377B2
公开(公告)日：2010-04-13
申请号：US11815826
申请日：2006-10-19
申请人： Takanori Aoki , Toshitaka Hiro
发明人： Takanori Aoki , Toshitaka Hiro
IPC分类号： C07C229/00 , C07C239/00
CPC分类号： C01B21/149
摘要： It is the objective to provide a method of stabilizing hydroxylamine at a high temperature and a high concentration or in a case that metal impurities such as Fe got mixed therewith, and a stabilized hydroxylamine solution. A method for stabilizing hydroxylamine related to the present invention is characterized by adding ethylenediamine-N,N′-di(o-hydroxyphenylacetic acid) as a preservation stabilizer.
摘要翻译：目的是提供在高温高浓度下稳定羟胺的方法，或者在诸如Fe之类的金属杂质混合的情况下和稳定的羟胺溶液。用于稳定本发明相关羟胺的方法的特征在于加入乙二胺-N，N'-二（邻羟基苯基乙酸）作为保存稳定剂。

85. 发明申请

US20100087656A1 Compositions Containing Fatty Acids and/or Derivatives Thereof and a Low Temperature Stabilizer 有权
标题翻译：含有脂肪酸和/或其衍生物的组合物和低温稳定剂
公开(公告)号：US20100087656A1
公开(公告)日：2010-04-08
申请号：US12551087
申请日：2009-08-31
申请人： Dries Muller , Pedro Lopes , Mark Brewer , Erik Kelderman , David Broere
发明人： Dries Muller , Pedro Lopes , Mark Brewer , Erik Kelderman , David Broere
IPC分类号： C07C229/00 , C07D233/20
CPC分类号： C10L10/16 , C10L1/143 , C10L1/1608 , C10L1/1616 , C10L1/1881 , C10L1/1883 , C10L1/1885 , C10L1/1886 , C10L1/1888 , C10L1/19 , C10L1/1905 , C10L1/191 , C10L1/2222 , C10L1/2225 , C10L1/224 , C10L1/232 , C10L1/2381 , C10L10/08 , C10L10/14 , C11C3/003 , C11C3/02 , Y02E50/13 , Y02T50/678
摘要： The present invention relates to methods of improving the low temperature storage and performance properties of fatty acids and/or derivatives thereof, as well as compositions containing fatty acids and/or derivatives thereof having superior lower temperature storage and performance properties.
摘要翻译：本发明涉及改善脂肪酸和/或其衍生物的低温储存和性能的方法，以及含有具有优异的较低温度储存和性能特性的脂肪酸和/或其衍生物的组合物。

86. 发明申请

US20100081717A1 Chiral Cyclic Beta-Amino Acids and their Derivatives, Pharmaceutical Compositions Containing Them and the Use of Such Compounds 有权
标题翻译：手性环状β-氨基酸及其衍生物，含有这些化合物及其使用的药物组合物
公开(公告)号：US20100081717A1
公开(公告)日：2010-04-01
申请号：US12513369
申请日：2007-11-14
申请人： Ferenc Fulop , Zsolt Szakonyi
发明人： Ferenc Fulop , Zsolt Szakonyi
IPC分类号： A61K31/195 , C07C229/00
CPC分类号： C07C335/18 , C07B2200/07 , C07C215/42 , C07C229/50 , C07C271/24 , C07C275/30 , C07C275/34 , C07C335/14 , C07C2602/42 , C07C2603/18 , C07D205/12
摘要： The invention relates to chiral cyclic β-amino acids of Formula (I) and their salts formed with pharmaceutically acceptable acids or bases, wherein the main meanings of the substituents are as follows: R stands for C1-4 Alk; X stands for —COOH, —CONH2, —CONH(C1-4 Alk), —CON(C1-4 Alk)2, —COO(C1-4 Alk), —COPhe-O-(C1-4 Alk) or —CH2OH; Y stands for —NH2, —NHBoc, —NHFmoc, —NH(C1-4 Alk), —N(C1-4 Alk)2, —NHCH2Ph, or Ar—NH—C(=X0)—N(R0)— wherein Ar stands for a phenyl group substituted by C1-4 alkoxy or halogen, X0 stands for O or S, and R0 stands for hydrogen or benzyl; and X+Y stands for —CONH— vagy —CON(Boc)-; with the proviso that when X stands for —COOH, then Y may be only different from —NH2. The invention also relates to pharmaceutical compositions having multidrug-resistance reversing effect that contain one or more compound(s) of Formula (I) or a salt thereof and inert pharmaceutical carriers and/or auxiliary agents. The invention also relates to carboxylic acids of Formula (XX) and their salts.
摘要翻译：本发明涉及式（I）的手性环状 - 氨基酸及其与药学上可接受的酸或碱形成的盐，其中取代基的主要含义如下：R代表C1-4烷基; X代表-COOH，-CONH 2，-CONH（C 1-4 Alk），-CON（C 1-4 Alk）2，-COO（C 1-4 Alk），-C OPhe-O-（C 1-4 Alk）或 - CH2OH; Y代表-NH2，-NHBoc，-NHFmoc，-NH（C1-4 Alk），-N（C1-4 Alk）2，-NHCH2Ph或Ar-NH-C（= X0）-N（R0） - 其中Ar表示被C 1-4烷氧基或卤素取代的苯基，X 0表示O或S，R 0表示氢或苄基; 而X + Y代表-CONH- vagy -CON（Boc） - ; 条件是当X代表-COOH时，则Y可以仅与-NH 2不同。本发明还涉及含有一种或多种式（I）化合物或其盐和惰性药物载体和/或辅助剂的具有多重耐药性逆转作用的药物组合物。本发明还涉及式（XX）的羧酸及其盐。

87. 发明授权

US07687660B2 Process for preparing intermediates of HMG-CoA reductase inhibitors 失效
标题翻译：制备HMG-CoA还原酶抑制剂中间体的方法
公开(公告)号：US07687660B2
公开(公告)日：2010-03-30
申请号：US12148533
申请日：2008-04-18
申请人： Vinod Kumar Kansal , Brijnath P. Chaurasia , Hitesh K. Patel , Vrajlal Gothalia , Hiren Gandhi
发明人： Vinod Kumar Kansal , Brijnath P. Chaurasia , Hitesh K. Patel , Vrajlal Gothalia , Hiren Gandhi
IPC分类号： C07C229/00
CPC分类号： C07F9/5352 , C07F7/1804 , C07F9/4006
摘要： The present invention relates to intermediates of rosuvastatin and processes for the production thereof.
摘要翻译：本发明涉及罗苏伐他汀的中间体及其生产方法。

88. 发明申请

US20100075977A1 BETA-3 RECEPTOR LIGANDS AND THEIR USE IN THERAPY 有权
标题翻译： BETA-3受体配体及其在治疗中的使用
公开(公告)号：US20100075977A1
公开(公告)日：2010-03-25
申请号：US12376324
申请日：2007-08-03
申请人： Antonio Scilimati , Maria Grazia Perrone , Ernesto Santandrea
发明人： Antonio Scilimati , Maria Grazia Perrone , Ernesto Santandrea
IPC分类号： A61K31/497 , C07C229/00 , C07D207/04 , C07D241/04 , A61K31/235
CPC分类号： C07D295/26 , C07C217/60
摘要： The present invention relates to new compounds, ligands of the beta-3 adrenergic receptor, their preparation and their use in therapy or as research tools for said receptor; the invention also relates to a process for the preparation of the compounds of the invention and the use of inverse agonists of the beta-3 adrenergic receptor as medicaments.
摘要翻译：本发明涉及新化合物，β-3肾上腺素能受体的配体，其制备及其在治疗中的用途或作为所述受体的研究工具; 本发明还涉及制备本发明化合物的方法以及β-3肾上腺素能受体的反向激动剂作为药物的用途。

89. 发明申请

US20100056780A1 NOVEL O-ACYLOXIME DERIVATIVES, PREPARATION METHOD THEREOF, AND PHARMACEUTICAL COMPOSITION CONTAINING THE SAME FOR PREVENTION AND TREATMENT OF CARDIOVASCULAR DISEASE 有权
标题翻译：新型O-亚氨基衍生物，其制备方法和含有其的药物组合物用于预防和治疗心血管疾病
公开(公告)号：US20100056780A1
公开(公告)日：2010-03-04
申请号：US12614634
申请日：2009-11-09
申请人： Tae-Sook JEONG , Woo-Song LEE , Hyung-Jae JEONG , Yong-Dae PARK , Jong-Min HAN , Hyoung-Chin KIM , Og-Sung MOON , Young-Suk WON
发明人： Tae-Sook JEONG , Woo-Song LEE , Hyung-Jae JEONG , Yong-Dae PARK , Jong-Min HAN , Hyoung-Chin KIM , Og-Sung MOON , Young-Suk WON
IPC分类号： C07D295/10 , C07C229/00 , C07D333/38
CPC分类号： C07C251/68 , C07C251/66 , C07D207/335 , C07D295/205 , C07D307/52 , C07D307/68 , C07D333/22 , C07D333/38
摘要： The present invention relates to novel O-acyloxime derivatives, a preparation method thereof and a pharmaceutical composition comprising the same for prevention and treatment of cardiovascular disease.The O-acyloxime derivatives according to the present invention may valuably be used for prevention and treatment of cardiovascular diseases such as hyperlipidemia, coronary arterial heart disease, atherosclerosis, and myocardial infarction caused by Lp-PLA2, because they have excellent inhibitory effect of Lp-PLA2.
摘要翻译：本发明涉及新型O-酰氧基肟衍生物，其制备方法以及包含其的用于预防和治疗心血管疾病的药物组合物。根据本发明的O-酰氧基肟衍生物可以用于预防和治疗由Lp-PLA2引起的高脂血症，冠状动脉心脏病，动脉粥样硬化和心肌梗塞等心血管疾病，因为它们具有优异的Lp- PLA2。

90. 发明申请

US20100056776A1 METHOD OF PREPARING MACROMOLECULAR CONTRAST AGENTS AND USES THEREOF 有权
标题翻译：制备大分子对比剂的方法及其用途
公开(公告)号：US20100056776A1
公开(公告)日：2010-03-04
申请号：US12513813
申请日：2007-11-06
申请人： Martin W. Brechbiel , Heng Xu
发明人： Martin W. Brechbiel , Heng Xu
IPC分类号： C07D403/12 , C07C229/00 , C07D207/46 , C07D207/40 , C07D257/02
CPC分类号： A61K51/065 , A61K47/59 , A61K47/595 , A61K49/085 , A61K49/124
摘要： Disclosed are methods of preparing a macromolecular conjugated ligand and a metal complex thereof. The metal complex is targeted for use as a contrast agent, for example, in MRI. The method of preparing a macromolecular conjugated ligand comprises: (a) providing a compound of formula (I) wherein R, A, and Pg are as defined herein, (b) reacting the compound of formula (I) with a macromolecular compound (e.g., dendrimer) in an organic solvent medium which is substantially free of water to obtain a macromolecular conjugated compound, and (c) removing the carboxyl-protecting groups to obtain a carboxyl-deprotected macromolecular conjugated compound. The metal complex can be prepared by reacting the carboxyl-deprotected macromolecular conjugated compound with an ion (e.g., Gd(III)). Also disclosed are two carboxyl-protected 1B4M-DTPA intermediate compounds.
摘要翻译：公开了制备大分子共轭配体及其金属络合物的方法。金属络合物被靶向用作造影剂，例如在MRI中。制备大分子缀合配体的方法包括：（a）提供其中R，A和Pg如本文所定义的式（I）化合物，（b）使式（I）化合物与高分子化合物树枝状大分子）在基本上不含水的有机溶剂介质中，得到高分子共轭化合物，（c）除去羧基保护基，得到羧基脱保护的高分子共轭化合物。金属络合物可以通过羧基脱保护的大分子共轭化合物与离子（例如Gd（III））反应来制备。还公开了两种羧基保护的1B4M-DTPA中间体化合物。

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