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121. 发明申请

US20070060497A1 Reagents for modifying biopharmaceuticals, the use and production thereof 审中-公开
标题翻译：用于改变生物药物的试剂，其使用和生产
公开(公告)号：US20070060497A1
公开(公告)日：2007-03-15
申请号：US10559996
申请日：2004-06-11
申请人： Ralf Krahmer , Frank Leenders
发明人： Ralf Krahmer , Frank Leenders
IPC分类号： A61K38/17 , C40B40/04 , C40B40/10 , C40B30/06 , C07C229/02 , C07C237/02
CPC分类号： C07D207/46 , A61K47/54 , A61K47/60
摘要： The present invention relates to compounds which are suitable for coupling to pharmaceuticals, in particular biopharmaceuticals, and to conjugates composed of the compounds and biomolecules or pharmaceutical active compounds. The compounds according to the invention can be readily formed by means of multicomponent reactions. The invention also relates to the use of the conjugates as an improved formulation of pharmaceuticals, and to their preparation. The invention furthermore provides a laboratory kit for the in-vitro preparation of conjugates which are composed of the compounds according to the invention and pharmaceuticals as well as biotechnological substances, in particular biopharmaceuticals, pharmaceutical active compounds, synthetic molecules or surfaces.
摘要翻译：本发明涉及适用于与药物特别是生物药物偶联的化合物，以及由化合物和生物分子或药物活性化合物组成的缀合物。根据本发明的化合物可以通过多组分反应容易地形成。本发明还涉及缀合物作为药物的改进制剂及其制备的用途。本发明还提供了用于体外制备缀合物的实验室试剂盒，其由根据本发明的化合物和药物以及生物技术物质，特别是生物药物，药物活性化合物，合成分子或表面组成。

122. 发明申请

US20070004801A1 Amidobetaines for oral care applications 有权
标题翻译：氨基甜菜碱用于口腔护理应用
公开(公告)号：US20070004801A1
公开(公告)日：2007-01-04
申请号：US11327202
申请日：2006-01-06
申请人： Nirmal Koshti , Bharat Parab , Shubhangi Naik
发明人： Nirmal Koshti , Bharat Parab , Shubhangi Naik
IPC分类号： A61K31/205 , C07C237/02
CPC分类号： C07C231/12 , A61K31/205 , C07C233/36
摘要： An aqueous composition for oral care application comprising solution of an amidobetaine of the following general Formula I is disclosed; in which R is an alkyl of coconut fatty acids, preferably hydrogenated coconut fatty acids, or a fatty acid mixture group which, on the average, corresponds to coconut fatty acids, wherein the solution has a solids content of 36% by weight, a pH of 4.5 to 6, an alkylamidopropyldimethyl amine content of not more than 0.1% by weight, and a free fatty acid content less than 0.5% by weight, sodium chloride content of 6.0% max and dimethylaminopropylamino betaine (from N,N-dimethyl amino propyl 1,3-diamine (DMAPA) and monochloroacetic acid) content of 30 ppm max, free sodium monochloroacetic acid content of 5 ppm max and free N,N-dimethylamino propyl 1,3-diamine content of 5.0 ppm max.
摘要翻译：公开了一种用于口腔护理应用的含水组合物，其包含以下通式I的氨基甜菜碱溶液; 其中R是椰子脂肪酸的烷基，优选氢化椰子脂肪酸，或平均相当于椰子脂肪酸的脂肪酸混合物组，其中溶液的固体含量为36重量％，pH 为4.5〜6，烷基酰胺基丙基二甲基胺含量为0.1重量％以下，游离脂肪酸含量小于0.5重量％，氯化钠含量为6.0％以上，二甲基氨基丙基氨基甜菜碱（来自N，N-二甲基氨基丙基 1,3-二胺（DMAPA）和一氯乙酸）含量最高为30ppm，游离的一氯乙酸含量最高为5ppm，游离的N，N-二甲基氨基丙基1,3-二胺的含量最高为5.0ppm。

123. 发明申请

US20060194213A1 Synthesis of 3'-, or 5'-, or internal methacrylamido-modified oligonucleotides 有权
标题翻译： 3'-或5'-或内部甲基丙烯酰胺修饰的寡核苷酸的合成
公开(公告)号：US20060194213A1
公开(公告)日：2006-08-31
申请号：US11066791
申请日：2005-02-25
申请人： Julia Golova , Boris Chernov
发明人： Julia Golova , Boris Chernov
IPC分类号： C12Q1/68 , C07H21/02 , B05D3/02 , C07C237/02
CPC分类号： C07F9/2408 , C07B2200/11 , C07C233/20 , C07C237/22 , C07H21/02 , Y10S977/792
摘要： New modifiers were synthesized for incorporation of a methacrylic function in 3′-, 5′- and internal positions of oligonucleotides during solid phase synthesis. A modifier was used for synthesis of 5′-methacrylated oligonucleotides for preparation of microarrays by a co-polymerization method.
摘要翻译：合成新的改性剂，用于在固相合成期间将寡核苷酸的3'-，5'-和内部位置中的甲基丙烯酸功能引入。用于通过共聚合法合成制备微阵列的5'-甲基丙烯酸酯化寡核苷酸的改良剂。

124. 发明申请

US20060141597A1 Valency platform molecules comprising aminooxy groups 审中-公开
标题翻译：价值平台分子包含氨氧基
公开(公告)号：US20060141597A1
公开(公告)日：2006-06-29
申请号：US11303591
申请日：2005-12-16
申请人： David Jones , Huong-Thu Ton-Nu , Fang Xie , Anping Tao , Tong Xu , Jeffrey Hammaker
发明人： David Jones , Huong-Thu Ton-Nu , Fang Xie , Anping Tao , Tong Xu , Jeffrey Hammaker
IPC分类号： C12N9/00 , C07H21/02 , C08B37/00 , C07K17/14 , C07K14/575 , C07K14/47 , C07K16/46 , C07C237/02
CPC分类号： C07D295/185 , A61K47/54 , A61K47/60 , C07C251/60 , C07C271/16 , C07C271/20 , C07C323/60 , C07D295/205 , C07K14/775 , C08B37/0012 , C08G65/329 , C08G65/33396 , C08G83/003
摘要： Molecules comprising aminooxy groups are provided, wherein the aminooxy groups provide attachment sites for the covalent attachment of other molecules. In one embodiment, polyoxyethylene molecules comprising aminooxy groups are provided that can be conjugated to wide variety of biologically active molecules including poly(amino acids). In another embodiment, valency platform molecules comprising aminooxy groups are provided. The aminooxy groups can be used to form covalent bonds with biological molecules such as poly(amino acids). The aminooxy groups can, for example, react with poly(amino acids) modified to contain carbonyl groups, such as glyoxyl groups, to form a conjugate of the valency platform molecule and the biologically active molecule via an oxime bond. The valency platform molecules comprising aminooxy groups are advantageously reactive in the formation of conjugates, and they also can be readily synthesized to form a composition with very low polydispersity.
摘要翻译：提供包含氨基氧基的分子，其中氨基氧基为其它分子的共价连接提供附着位点。在一个实施方案中，提供了包含氨基氧基的聚氧乙烯分子，其可与多种生物活性分子（包括聚（氨基酸））缀合。在另一个实施方案中，提供了包含氨基氧基的化合物平台分子。氨基氧基可用于与生物分子如聚（氨基酸）形成共价键。例如，氨基氧基可以与经修饰以含有羰基（例如乙醛基）的聚（氨基酸）反应，以通过肟键形成价态平台分子和生物活性分子的缀合物。包含氨基氧基的价态平台分子在缀合物的形成中有利地是反应性的，并且它们也可以容易地合成以形成具有非常低的多分散性的组合物。

125. 发明申请

US20050070483A1 Prodrugs of amino acids with affinity for the alpha2delta-protein 有权
标题翻译：具有对alpha2delta蛋白的亲和力的氨基酸的前药
公开(公告)号：US20050070483A1
公开(公告)日：2005-03-31
申请号：US10946540
申请日：2004-09-21
申请人： Sean Donevan , Augustine Osuma , Andrew Thorpe , David Wustrow
发明人： Sean Donevan , Augustine Osuma , Andrew Thorpe , David Wustrow
IPC分类号： A61P25/00 , C07C237/02 , C07C237/12 , A61K38/04 , C07C233/50 , C07C233/51 , C07D213/55 , C07K5/04
CPC分类号： C07C237/12
摘要： This invention relates to prodrugs of certain amino acids that bind to the alpha-2-delta (α2δ) subunit of a calcium channel. These compounds and their pharmaceutically acceptable salts are useful in the treatment of a variety of psychiatric, pain and other disorders.
摘要翻译：本发明涉及结合钙通道的α-2-δ（α2delta）亚基的某些氨基酸的前药。这些化合物及其药学上可接受的盐可用于治疗各种精神病，疼痛和其它疾病。

126. 发明授权

US5676923A Substituted DTPA monoamides of the central carboxylic acid group and their metal complexes 失效
标题翻译：中间羧酸基团的取代的DTPA单酰胺及其金属络合物
公开(公告)号：US5676923A
公开(公告)日：1997-10-14
申请号：US484319
申请日：1995-06-07
申请人： Johannes Platzek , Ulrich Niedballa , Peter Mareski , Bernd Raduchel , Hanns-Joachim Weinmann , Andreas Muhler , Bernd Misselwitz
发明人： Johannes Platzek , Ulrich Niedballa , Peter Mareski , Bernd Raduchel , Hanns-Joachim Weinmann , Andreas Muhler , Bernd Misselwitz
IPC分类号： A61K49/00 , A61K49/06 , C07C237/02 , C07C237/06 , C07C237/08 , C07C237/10 , C07C237/12 , C07C271/22 , C07D213/55 , C07D295/185 , C07D225/02 , A61K49/04 , C07C229/02 , C07C271/02 , C07C321/00 , C07D211/70 , C07F1/08 , C07F1/10 , C07F1/12 , C07F9/94 , C07F13/00
CPC分类号： C07D295/185 , A61K49/0002 , A61K49/06 , C07C237/02 , C07C237/06 , C07C237/08 , C07C237/10 , C07C237/12 , C07C271/22 , C07D213/55 , Y10S514/836
摘要： Diethylenetriaminepentaacetic acid monoamide derivatives, their complexes and complex salts, containing an element of atomic numbers 21-29, 31, 32, 39, 42-44, 49 or 57-83, pharmaceutical agents containing these compounds, their use as contrast media and process for their production.
摘要翻译：含有原子序数21-29,31,32,39,42-44,49或57-83的元素的二亚乙基三胺五乙酸单酰胺衍生物，它们的络合物和络合盐，含有这些化合物的药物，它们作为造影剂和方法为他们的生产。

127. 发明授权

US08431733B2 Process for the preparation of (3S)-3-amino-N-cyclopropyl-2-hydroxyalkanamide derivatives 失效
标题翻译：（3S）-3-氨基-N-环丙基-2-羟基烷酰胺衍生物的制备方法
公开(公告)号：US08431733B2
公开(公告)日：2013-04-30
申请号：US12402312
申请日：2009-03-11
申请人： Jeffrey Dener
发明人： Jeffrey Dener
IPC分类号： C07C229/00 , C07C237/02
CPC分类号： C07C231/12 , C07B2200/07 , C07C223/02 , C07C225/26 , C07C229/14 , C07C229/22 , C07C237/04 , C07C259/06 , C07C2601/02 , C07D401/14
摘要： The present invention relates to a process for the preparation of (2S,3S)-3-amino-N-cyclopropyl-2-hydroxyalkanamides, and their use in the preparation of HCV inhibitors and cathepsin inhibitors.
摘要翻译：本发明涉及制备（2S，3S）-3-氨基-N-环丙基-2-羟基烷酰胺的方法及其在制备HCV抑制剂和组织蛋白酶抑制剂中的用途。

128. 发明申请

US20110190530A1 Polycationic Viscoelastic Compositions 有权
标题翻译：聚阳离子粘弹性组合物
公开(公告)号：US20110190530A1
公开(公告)日：2011-08-04
申请号：US13018112
申请日：2011-01-31
申请人： Paul Knox
发明人： Paul Knox
IPC分类号： C07C69/76 , C07C237/02 , C07C309/00
CPC分类号： A61Q11/00 , A61K8/02 , A61K8/0208 , A61K8/22 , C09K8/602 , C09K8/68 , C09K2208/30 , Y10S507/925 , Y10S507/927 , Y10S507/935
摘要： Viscoelastic compositions are disclosed herein containing an effective amount of one or more random or structurally defined polycationic quaternary ammonium compounds for controlling the viscoelasticity of the composition. In one aspect, the present technology provides polycationic quaternary ammonium compounds that comprise bis-quaternary compound. The bis-quaternary compounds of the present technology can be symmetric or dissymmetric. In another aspect, the present technology provides viscoelastic well bore treatment fluids comprising water, and at least one polycationic quaternary ammonium compound that comprises a bis-quaternary compound. In another aspect, the present technology provides polycationic carboxylates. Preferred viscoelastic compositions of the present technology maintain viscoelasticity at a temperature greater than about 80° C., preferably greater than about 100° C. or 110° C. when the amount of the one or polycationic quaternary compounds is less than about 10% by weight based on the total weight of the composition.
摘要翻译：本文公开的粘弹性组合物含有有效量的一种或多种无规或结构限定的聚阳离子季铵化合物，用于控制组合物的粘弹性。一方面，本技术提供了包含双季化合物的聚阳离子季铵化合物。本技术的双季化合物可以是对称的或不对称的。在另一方面，本技术提供了包含水的粘弹性井眼处理流体和至少一种包含双季化合物的聚阳离子季铵化合物。另一方面，本技术提供聚阳离子羧酸盐。当本技术的优选粘弹性组合物在大于约80℃，优选大于约100℃或110℃的温度下保持粘弹性，当一种或多种阳离子季铵化合物的量小于约10％时，通过基于组合物的总重量的重量。

129. 发明申请

US20100267946A1 PRODRUGS OF GABA ANALOGS, COMPOSITIONS AND USES THEREOF 有权
标题翻译： GABA类似物的组合物及其用途
公开(公告)号：US20100267946A1
公开(公告)日：2010-10-21
申请号：US12828764
申请日：2010-07-01
申请人： Mark A. Gallop , Kenneth C. Cundy , Cindy X. Zhou , Fayang G. Qiu , Fenmei Yao , Jia-Ning Xiang , Ian R. Ollmann
发明人： Mark A. Gallop , Kenneth C. Cundy , Cindy X. Zhou , Fayang G. Qiu , Fenmei Yao , Jia-Ning Xiang , Ian R. Ollmann
IPC分类号： C07D267/06 , C07C229/28 , C07C237/02 , C07D317/34 , C07D405/02 , C07D211/26
CPC分类号： C07C205/43 , A61K38/00 , C07C45/567 , C07C209/48 , C07C229/28 , C07C271/22 , C07C2601/10 , C07C2601/14 , C07D213/80 , C07D267/04 , C07D307/58 , C07D317/32 , C07D317/40 , C07K5/0205 , C07C49/83 , C07C49/17
摘要： The present invention provides prodrugs of GABA analogs, pharmaceutical compositions of prodrugs of GABA analogs and methods for making prodrugs of GABA analogs. The present invention also provides methods for using prodrugs of GABA analogs and methods for using pharmaceutical compositions of prodrugs of GABA analogs for treating or preventing common diseases and/or disorders.
摘要翻译：本发明提供GABA类似物的前体药物，GABA类似物前药的药物组合物和制备GABA类似物前药的方法。本发明还提供使用GABA类似物前药的方法和使用GABA类似物前药药物组合物治疗或预防常见疾病和/或病症的方法。

130. 发明申请

US20100105617A1 C-Terminal Attachment of Two Chemical Groups to Peptides 审中-公开
标题翻译：两个化学基团与肽的C-末端连接
公开(公告)号：US20100105617A1
公开(公告)日：2010-04-29
申请号：US12526277
申请日：2008-02-13
申请人： Bernd Peschke
发明人： Bernd Peschke
IPC分类号： A61K38/27 , C07K1/107 , C07D405/12 , C07C237/02
CPC分类号： C07K1/13 , A61K47/60 , C07C237/22 , C07K1/006 , C12P21/02
摘要： The present invention relates to a method for C-terminal attachment of two property-modifying groups to a peptide.
摘要翻译：本发明涉及两个性质修饰基团与肽的C-末端连接的方法。

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