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公开(公告)号：US08101605B2
公开(公告)日：2012-01-24
申请号：US12960318
申请日：2010-12-03
申请人： Lloyd Mackenzie , Tom MacRury , Curtis Harwig , Jeremy Pettigrew , Noor Aini Bhatti , Sam Place , Paul Bird , Vladimir Khlebnikov , Rudong Shan
发明人： Lloyd Mackenzie , Tom MacRury , Curtis Harwig , Jeremy Pettigrew , Noor Aini Bhatti , Sam Place , Paul Bird , Vladimir Khlebnikov , Rudong Shan
IPC分类号： C07D311/78 , C07D335/04 , A61K31/352 , A61K31/382
CPC分类号： C07D335/04 , C07D311/78 , C07D409/06
摘要： Compounds of structure (I): including stereoisomers and pharmaceutically acceptable salts thereof, wherein X, R1, R2, R3, R4, R5, R6 and R7 are as defined herein. Such compounds have activity as SHIP1 modulators, and thus may be used to treat any of a variety of diseases, disorders or conditions that would benefit from SHIP1 modulation. Compositions comprising a compound of structure (I) in combination with a pharmaceutically acceptable carrier or diluent are also disclosed, as are methods of SHIP1 modulation by administration of such compounds to an animal in need thereof.
摘要翻译： 结构（I）的化合物：包括立体异构体及其药学上可接受的盐，其中X，R 1，R 2，R 3，R 4，R 5，R 6和R 7如本文所定义。 这些化合物具有作为SHIP1调节剂的活性，因此可用于治疗将受益于SHIP1调节的各种疾病，障碍或病症中的任何一种。 还公开了包含结构（I）化合物与药学上可接受的载体或稀释剂组合的组合物，以及通过将这些化合物施用于有需要的动物的SHIP1调节方法。
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公开(公告)号：US20070208181A1
公开(公告)日：2007-09-06
申请号：US11683534
申请日：2007-03-08
申请人： Ronald Lauener , David Burgoyne , Patrick Rebstein , Lloyd Mackenzie , Yuanlin Zhou , Yaping Shen
发明人： Ronald Lauener , David Burgoyne , Patrick Rebstein , Lloyd Mackenzie , Yuanlin Zhou , Yaping Shen
IPC分类号： C07D207/24
CPC分类号： C07D207/26 , C07C255/46 , C07C271/60 , C07D213/75 , C07D233/32 , C07D239/10 , C07D473/04 , C07D473/06
摘要： The present invention is directed to a method for reducing the emetogenic effects of PDE inhibitors, and more particularly is directed to compounds having PDE4 inhibition activity with little or no emetogenic side-effects, and chemical methods including benzylation for preparing such compounds. A benzyl group may be attached to either a carbon or nitrogen atom of a PDE4 inhibitor. Suitable benzylation chemistry is to extract a hydrogen from a PDE4 inhibitor, preferably with a base, and then react the resulting nucleophilic PDE4 inhibitor with a benzylating agent, e.g., benzyl bromide or a derivative thereof.
摘要翻译： 本发明涉及一种减少PDE抑制剂的致吐作用的方法，更具体地涉及具有很少或不具有致吐性副作用的具有PDE4抑制活性的化合物，以及包括用于制备这些化合物的苄基化的化学方法。 苄基可以连接到PDE4抑制剂的碳原子或氮原子上。 合适的苄基化学方法是从PDE4抑制剂，优选用碱提取氢，然后使得到的亲核PDE4抑制剂与苄化试剂如苄基溴或其衍生物反应。
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3.发明授权公开(公告)号：US07078194B2
公开(公告)日：2006-07-18
申请号：US09837711
申请日：2001-04-17
CPC分类号： C12P19/04 , C07K2319/02 , C12N9/2408 , C12N9/2414 , C12N9/2445 , C12Y302/01021
摘要： Mutant glycosidase enzymes are formed in which the normal nucleophilic amino acid within the active site has been changed to a nonnucleophilic amino acid. These enzymes cannot hydrolyze disaccharide products, but which can still form them. Using this enzyme, oligosaccharides are synthesized by preparing a mixture of an &agr;glycosyl fluoride and a glycoside acceptor molecule; enzymatically coupling the &agr.glycosyl fluoride to the glycoside acceptor molecule to form a glycosyl glycoside product using the mutant glycosidase enzyme; and recovering the glycosyl glycoside product. Particular enzymes include a mutant form of Agrobacterium &bgr.Glucosidase in which the normal glutamic acid residue at position 358 is replaced with an alanine residue.
摘要翻译： 形成突变糖苷酶，其中活性位点内的正常亲核氨基酸已经改变为非亲核氨基酸。 这些酶不能水解二糖产物，但仍然可以形成它们。 使用该酶，通过制备藻糖基氟化物和糖苷受体分子的混合物合成寡糖; 将糖基氟化物与糖苷受体分子酶促偶联以使用突变糖苷酶形成糖基糖苷产物; 并回收糖基糖苷产物。 特定的酶包括农杆菌和葡萄糖苷酶的突变形式，其中358位的正常谷氨酸残基被丙氨酸残基取代。
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4.发明授权公开(公告)号：US06284494B1
公开(公告)日：2001-09-04
申请号：US09091272
申请日：1998-09-29
IPC分类号： C12P1944
CPC分类号： C12P19/04 , C07K2319/02 , C12N9/2408 , C12N9/2414 , C12N9/2445 , C12Y302/01021
摘要： Mutant glycosidase enzymes are formed in which the normal nucleophilic amino acid within the active site has been changed to a non-nucleophilic amino acid. These enzymes cannot hydrolyze disaccharide products, but which can still form them. Using this enzyme, oligosaccharides are synthesized by preparing a mixture of an &agr;-glycosyl fluoride and a glycoside acceptor molecule; enzymatically coupling the &agr;-glycosyl fluoride to the glycoside acceptor molecule to form a glycosyl glycoside product using the mutant glycosidase enzyme; and recovering the glycosyl glycoside product. Particular enzymes include a mutant form of Agrobacterium &bgr;-Glucosidase in which the normal glutamic acid residue at position 358 is replaced with an alanine residue.
摘要翻译： 形成突变糖苷酶，其中活性位点内的正常亲核氨基酸已经改变为非亲核氨基酸。 这些酶不能水解二糖产物，但仍然可以形成它们。 使用该酶，通过制备α-糖基氟化物和糖苷受体分子的混合物来合成寡糖; 将α-糖基氟酶与糖苷受体分子酶促偶联以形成使用突变糖苷酶的糖基糖苷产物; 并回收糖基糖苷产物。 具体的酶包括农杆菌β-葡糖苷酶的突变形式，其中358位的正常谷氨酸残基被丙氨酸残基取代。
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5.发明申请公开(公告)号：US20180130150A1
公开(公告)日：2018-05-10
申请号：US15347827
申请日：2016-11-10
CPC分类号： G06Q50/14 , G06Q10/02 , G06Q30/0236
摘要： The OneRez “Prove Your Local” Travel Platform enables travel suppliers to offer discounted or specialized rates to customers who have self-certified that they reside within a geographical distance set by the Travel Supplier or by OneRez on the system. Customers self-certify at the OneRez web site demonstrating the location of their primary residence, and obtain a Local Membership Identification—enabling them to book travel products at the specified local rate from participating travel suppliers.
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公开(公告)号：US20110136802A1
公开(公告)日：2011-06-09
申请号：US12960318
申请日：2010-12-03
申请人： Lloyd Mackenzie , Tom MacRury , Curtis Harwig , Jeremy Pettigrew , Noor Aini Bhatti , Sam Place , Paul Bird , Vladimir Khlebnikov , Rudong Shan
发明人： Lloyd Mackenzie , Tom MacRury , Curtis Harwig , Jeremy Pettigrew , Noor Aini Bhatti , Sam Place , Paul Bird , Vladimir Khlebnikov , Rudong Shan
IPC分类号： A61K31/5377 , C07D335/04 , A61K31/382 , C07D413/12 , C07D403/10 , A61K31/496 , C07D401/10 , A61K31/4535 , C07D311/78 , A61K31/352 , A61P11/00 , A61P1/00 , A61P19/02 , A61P1/04 , A61P11/06 , A61P25/28 , A61P27/02 , A61P17/06 , A61P35/00
CPC分类号： C07D335/04 , C07D311/78 , C07D409/06
摘要： Compounds of structure (I): including stereoisomers and pharmaceutically acceptable salts thereof, wherein X, R1, R2, R3, R4, R5, R6 and R7 are as defined herein. Such compounds have activity as SHIP1 modulators, and thus may be used to treat any of a variety of diseases, disorders or conditions that would benefit from SHIP1 modulation. Compositions comprising a compound of structure (I) in combination with a pharmaceutically acceptable carrier or diluent are also disclosed, as are methods of SHIP1 modulation by administration of such compounds to an animal in need thereof.
摘要翻译： 结构（I）的化合物：包括立体异构体及其药学上可接受的盐，其中X，R 1，R 2，R 3，R 4，R 5，R 6和R 7如本文所定义。 这些化合物具有作为SHIP1调节剂的活性，因此可用于治疗将受益于SHIP1调节的各种疾病，障碍或病症中的任何一种。 还公开了包含结构（I）化合物与药学上可接受的载体或稀释剂组合的组合物，以及通过将这些化合物施用于有需要的动物的SHIP1调节方法。
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7.发明授权Methods and compositions for synthesis of oligosaccharides, and the products formed thereby 失效用于合成低聚糖的方法和组合物以及由此形成的产品
公开(公告)号：US5716812A
公开(公告)日：1998-02-10
申请号：US571175
申请日：1995-12-12
CPC分类号： C12N9/2414 , C12N9/2408 , C12N9/2445 , C12P19/04 , C12Y302/01021 , C07K2319/02
摘要： Mutant glycosidase enzymes are formed in which the normal nucleophilic amino acid within the active site has been changed to a non-nucleophilic amino acid. These enzymes cannot hydrolyze disaccharide products, but can still form them. Using this enzyme, oligosaccharides are synthesized by preparing a mixture of an .alpha.-glycosyl fluoride and a glycoside acceptor molecule; enzymatically coupling the .alpha.-glycosyl fluoride to the glycoside acceptor molecule to form a glycosyl glycoside product using the mutant glycosidase enzyme; and recovering the glycosyl glycoside product. Particular enzymes include a mutant form of Agrobacterium .beta.-Glucosidase in which the normal glutamic acid residue at position 358 is replaced with an alanine residue.
摘要翻译： 形成突变糖苷酶，其中活性位点内的正常亲核氨基酸已经改变为非亲核氨基酸。 这些酶不能水解二糖产物，但仍然可以形成它们。 使用该酶，通过制备α-糖基氟化物和糖苷受体分子的混合物来合成寡糖; 将α-糖基氟化酶与糖苷受体分子酶促偶联以使用突变糖苷酶形成糖基糖苷产物; 并回收糖基糖苷产物。 特定的酶包括农杆菌β-葡糖苷酶的突变体形式，其中位置358处的正常谷氨酸残基被丙氨酸残基替代。
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