利索-全球专利检索

  1. 登录
  2. 注册

搜索结果

9 条记录 (耗时 0.044 秒)

    Novel crystalline forms of an inhibitor of 11-beta-hydroxysteroid dehydrogenase type 1
    4.
    发明申请
    Novel crystalline forms of an inhibitor of 11-beta-hydroxysteroid dehydrogenase type 1 有权
    11型β-羟基类固醇脱氢酶抑制剂的新型结晶形式

    公开(公告)号：US20090186928A1

    公开(公告)日：2009-07-23

    申请号：US10587110

    申请日：2005-01-21

    申请人： Yuri Bereznitski ,  Mark A. Huffman ,  Joseph E. Lynch ,  Matthew Zhao

    发明人： Yuri Bereznitski ,  Mark A. Huffman ,  Joseph E. Lynch ,  Matthew Zhao

    IPC分类号： A61K31/4196 ,  C07D249/08 ,  A61P3/10

    CPC分类号： C07D249/08

    摘要： Novel crystalline salts of 3-[1-(4-chlorophenyl)-trans-3-fluorocyclobutyl]-4,5-dicyclopropyl-r-4H-1,2,4-triazole are potent inhibitors of 11β-hydroxysteroid dehydrogenase Type 1 and are useful for the treatment of conditions associated with Metabolic Syndrome as well as cognitive impairment. The invention also relates to pharmaceutical compositions containing these novel salts, processes to prepare these salts and their pharmaceutical compositions as well as uses thereof for the treatment of Type 2 diabetes, hyperglycemia, obesity, dyslipidemia, hypertension, and cognitive impairment.

    摘要翻译： 3- [1-（4-氯苯基） - 反式-3-氟环丁基] -4,5-二环丙基-r-4H-1,2,4-三唑的新型结晶盐是11β-羟基类固醇脱氢酶的有效抑制剂， 可用于治疗与代谢综合征相关的病症以及认知障碍。 本发明还涉及含有这些新型盐的药物组合物，制备这些盐的方法及其药物组合物及其用于治疗2型糖尿病，高血糖症，肥胖症，血脂异常，高血压和认知障碍的用途。

    Process for making hydroisoindoline tachykinin receptor antagonists
    5.
    发明授权
    Process for making hydroisoindoline tachykinin receptor antagonists 失效
    制备水解异吲哚啉速激肽受体拮抗剂的方法

    公开(公告)号：US07544815B2

    公开(公告)日：2009-06-09

    申请号：US11484208

    申请日：2006-07-11

    申请人： Jeffrey T. Kuethe ,  Jingjun Yin ,  Mark A. Huffman ,  Michel Journet

    发明人： Jeffrey T. Kuethe ,  Jingjun Yin ,  Mark A. Huffman ,  Michel Journet

    IPC分类号： C07D209/44

    CPC分类号： C07D209/44

    摘要： The present invention is directed to a process for preparing certain hydroisoindoline compounds which are useful as neurokinin-1 (NK-1) receptor antagonists, and inhibitors of tachykinin and in particular substance P. The compounds are useful in the treatment of certain disorders, including emesis, urinary incontinence, depression, and anxiety.

    摘要翻译： 本发明涉及一种制备某些可用作神经激肽-1（NK-1）受体拮抗剂，速激肽抑制剂，特别是物质P的水解异吲哚啉化合物的方法。该化合物可用于治疗某些疾病，包括 呕吐，尿失禁，抑郁和焦虑。

    PREPARATION OF ALKYL ESTERS OF N-PROTECTED OXO-AZACYCLOALKYLCARBOXYLIC ACIDS
    8.
    发明申请
    PREPARATION OF ALKYL ESTERS OF N-PROTECTED OXO-AZACYCLOALKYLCARBOXYLIC ACIDS 审中-公开
    N-保护的氧亚氨基甲酰氧基酸的烷基酯的制备

    公开(公告)号：US20120053350A1

    公开(公告)日：2012-03-01

    申请号：US13266871

    申请日：2010-04-26

    申请人： Ian Mangion ,  Mark A. Huffman ,  Rebecca T. Ruck ,  Joseph Lynch ,  John Y.L. Chung ,  Benjamin Marcune

    发明人： Ian Mangion ,  Mark A. Huffman ,  Rebecca T. Ruck ,  Joseph Lynch ,  John Y.L. Chung ,  Benjamin Marcune

    IPC分类号： C07D471/08 ,  C07D401/12 ,  C07D211/60

    CPC分类号： C07D471/08 ,  C07D207/28 ,  C07D211/78 ,  C07D401/12 ,  Y02P20/55

    摘要： A process for the preparation of alkyl esters of N-protected oxo-azacycloalkylcarboxylic acids of Formula III: comprises contacting a ketosulfoxonium ylide of Formula II: with an iridium catalyst to obtain Compound III, wherein PG1 is an amine protective group; k is 0, 1, or 2; and RU, R1, R2, and R3 are defined herein. An embodiment of the process further com rises contacting a compound of Formula I: with a sulfoxonium halide of formula (RU)3S(O)Z, wherein Z is halide, in the presence of a strong base to obtain Compound II. Additional embodiments add a series of process steps leading to the synthesis of 7-oxo-1,6-diazabicyclo[3.2.1]octanes suitable for use as β-lactamase inhibitors.

    摘要翻译： 制备式III的N-保护的氧代 - 氮杂环烷基羧酸的烷基酯的方法：包括使式II的酮磺基肟基鎓盐与铱催化剂接触，得到化合物III，其中PG1是胺保护基; k为0,1或2; 并且本文定义了RU，R1，R2和R3。 该方法的一个实施方案使得式I化合物与式（RU）3S（O）Z的氧化锍卤化物（其中Z为卤化物）在强碱存在下接触，得到化合物II。 另外的实施方案添加了一系列方法步骤，导致合成适合用作β-内酰胺酶抑制剂的7-氧代-1,6-二氮杂双环[3.2.1]辛烷。

    Crystalline forms of an inhibitor of 11-β-hydroxysteroid dehydrogenase type 1
    9.
    发明授权
    Crystalline forms of an inhibitor of 11-β-hydroxysteroid dehydrogenase type 1 有权
    11-＆bgr-羟基类固醇脱氢酶1型抑制剂的结晶形式

    公开(公告)号：US07875642B2

    公开(公告)日：2011-01-25

    申请号：US10587110

    申请日：2005-01-21

    申请人： Yuri Bereznitski ,  Mark A. Huffman ,  Joseph E. Lynch ,  Matthew Zhao

    发明人： Yuri Bereznitski ,  Mark A. Huffman ,  Joseph E. Lynch ,  Matthew Zhao

    IPC分类号： A61K31/4196 ,  C07D249/08

    CPC分类号： C07D249/08

    摘要： Novel crystalline salts of 3-[1-(4-chlorophenyl)-trans-3-fluorocyclobutyl]-4,5-dicyclopropyl-r-4H-1,2,4-triazole are potent inhibitors of 11β-hydroxysteroid dehydrogenase Type 1 and are useful for the treatment of conditions associated with Metabolic Syndrome as well as cognitive impairment. The invention also relates to pharmaceutical compositions containing these novel salts, processes to prepare these salts and their pharmaceutical compositions as well as uses thereof for the treatment of Type 2 diabetes, hyperglycemia, obesity, dyslipidemia, hypertension, and cognitive impairment.

    摘要翻译： 3- [1-（4-氯苯基） - 反式-3-氟环丁基] -4,5-二环丙基-r-4H-1,2,4-三唑的新型结晶盐是11β-羟基类固醇脱氢酶1型的有效抑制剂 并且可用于治疗与代谢综合征相关的病症以及认知障碍。 本发明还涉及含有这些新型盐的药物组合物，制备这些盐的方法及其药物组合物及其用于治疗2型糖尿病，高血糖症，肥胖症，血脂异常，高血压和认知障碍的用途。