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    Phosphoric acid salt of a dipeptidyl peptidase-IV inhibitor
    1.
    发明申请
    Phosphoric acid salt of a dipeptidyl peptidase-IV inhibitor 有权
    二肽基肽酶-IV抑制剂的磷酸盐

    公开(公告)号：US20050032804A1

    公开(公告)日：2005-02-10

    申请号：US10874992

    申请日：2004-06-23

    申请人： Stephen Cypes ,  Alex Chen ,  Russell Ferlita ,  Karl Hansen ,  Ivan Lee ,  Vicky Vydra ,  Robert Wenslow

    发明人： Stephen Cypes ,  Alex Chen ,  Russell Ferlita ,  Karl Hansen ,  Ivan Lee ,  Vicky Vydra ,  Robert Wenslow

    IPC分类号： A61K31/498 ,  A61P3/10 ,  C07D487/04

    CPC分类号： C07D487/04

    摘要： The dihydrogenphosphate salt of 4-oxo-4-[3-(trifluoromethyl)-5,6-dihydro [1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-1-(2,4,5-trifluorophenyl)butan-2-amine is a potent inhibitor of dipeptidyl peptidase-IV and is useful for the prevention and/or treatment of non-insulin dependent diabetes mellitus, also referred to as type 2 diabetes. The invention also relates to a crystalline monohydrate of the dihydrogenphosphate salt as well as a process for its preparation, pharmaceutical compositions containing this novel form and methods of use for the treatment of diabetes, obesity, and high blood pressure.

    摘要翻译： 4-氧代-4- [3-（三氟甲基）-5,6-二氢[1,2,4]三唑并[4,3-a]吡嗪-7（8H） - 基] -1-（ 2,4,5-三氟苯基）丁-2-胺是二肽基肽酶-IV的有效抑制剂，可用于预防和/或治疗非胰岛素依赖性糖尿病，也称为2型糖尿病。 本发明还涉及磷酸二氢盐的结晶一水合物及其制备方法，含有这种新型形式的药物组合物和用于治疗糖尿病，肥胖症和高血压的方法。

    Novel crystalline forms of a phosphoric acid salt of a dipeptidyl peptidase-iv inhibitor
    2.
    发明申请
    Novel crystalline forms of a phosphoric acid salt of a dipeptidyl peptidase-iv inhibitor 审中-公开
    二肽基肽酶-IV抑制剂的磷酸盐的新型结晶形式

    公开(公告)号：US20060287528A1

    公开(公告)日：2006-12-21

    申请号：US10569566

    申请日：2004-08-27

    申请人： Robert Wenslow ,  Joseph Armstrong ,  Alex Chen ,  Stephen Cypes ,  Russell Ferlita ,  Karl Hansen ,  Christopher Lindemann ,  Evangelia Spartalis

    发明人： Robert Wenslow ,  Joseph Armstrong ,  Alex Chen ,  Stephen Cypes ,  Russell Ferlita ,  Karl Hansen ,  Christopher Lindemann ,  Evangelia Spartalis

    IPC分类号： C07D487/04

    CPC分类号： C07D487/04

    摘要： The present invention relates to crystalline anhydrate polymorphs of the dihydrogenphosphate salt of (2R)4-oxo-4-[3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-α]pyrazin-7(8H) yl]-1-(2,4,5-trifluorophenyl)butan-2-amine as well as a process for their preparation, pharmaceutical compositions containing these novel forms, and methods of use of the novel forms and pharmaceutical compositions for the treatment of diabetes, obesity, and high blood pressure. The invention also concerns novel crystalline solvates of the dihydrogenphosphate salt of (2R)-4-oxo-4-[3-(trifluoromethyl)-5,6-dihydro[1,2,4]tria-zolo [4,3-α]pyrazin-7(8H)-yl]-1-(2,4,5-trifluorophenyl)butan-2-amine as well as a crystalline desolvated polymorph and their use for the preparation of the anhydrate polymorphs of the present invention.

    摘要翻译： 本发明涉及（2R）-4-氧代-4- [3-（三氟甲基）-5,6-二氢[1,2,4]三唑并[4,3-a]吡嗪的磷酸二氢盐的晶体无水物多晶型物 -7（8H）基] -1-（2,4,5-三氟苯基）丁-2-胺以及它们的制备方法，含有这些新形式的药物组合物，以及新型形式和药物的使用方法 用于治疗糖尿病，肥胖和高血压的组合物。 本发明还涉及（2R）-4-氧代-4- [3-（三氟甲基）-5,6-二氢[1,2,4]三唑并[4,3-a]的磷酸二氢盐的新结晶溶剂合物 ]吡嗪-7（8H） - 基] -1-（2,4,5-三氟苯基）丁-2-胺以及晶体脱溶化多晶型物及其用于制备本发明的无水物多晶型物的用途。

    Amorphous Form of a Phosphoric Acid Salt of a Dipeptidyl Peptidase-IV Inhibitor
    3.
    发明申请
    Amorphous Form of a Phosphoric Acid Salt of a Dipeptidyl Peptidase-IV Inhibitor 有权
    二肽基肽酶-IV抑制剂的磷酸盐的无定形形式

    公开(公告)号：US20070281941A1

    公开(公告)日：2007-12-06

    申请号：US11660722

    申请日：2005-09-09

    申请人： Russell Ferlita ,  Robert Wenslow

    发明人： Russell Ferlita ,  Robert Wenslow

    IPC分类号： A61K31/4985 ,  A61P3/04 ,  A61P7/12 ,  A61P9/12 ,  C07D487/22

    CPC分类号： C07D487/04

    摘要： The present invention relates to a novel amorphous form of the dihydrogenphosphate salt of (2R)-4-oxo-4-[3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-1-(2,4,5-trifluorophenyl)butan-2-amine as well as a process for its preparation, pharmaceutical compositions containing this novel form, and methods of use of the novel form and pharmaceutical compositions for the treatment of diabetes, obesity, and high blood pressure.

    摘要翻译： 本发明涉及（2R）-4-氧代-4- [3-（三氟甲基）-5,6-二氢[1,2,4]三唑并[4,3-a]的二氢磷酸盐的新型无定形形式 ]吡嗪-7（8H） - 基] -1-（2,4,5-三氟苯基）丁-2-胺以及其制备方法，含有该新型形式的药物组合物，以及使用该新颖的方法 用于治疗糖尿病，肥胖和高血压的形式和药物组合物。

    Novel crystalline form of a phosphoric acid salt of a dipeptidyl peptidase-iv inhibitor
    4.
    发明申请
    Novel crystalline form of a phosphoric acid salt of a dipeptidyl peptidase-iv inhibitor 审中-公开
    二肽基肽酶-IV抑制剂的磷酸盐的新晶体形式

    公开(公告)号：US20070021430A1

    公开(公告)日：2007-01-25

    申请号：US10570409

    申请日：2004-09-17

    申请人： Alex Chen ,  Robert Wenslow

    发明人： Alex Chen ,  Robert Wenslow

    IPC分类号： A61K31/498 ,  C07D487/04

    CPC分类号： C07D487/04

    摘要： The present invention relates to a novel crystalline anhydrate polymorph of the dihydrogenphosphate salt of (2R)-4-oxo-4-[3-trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-1-(2,4,5-trifluorophenyl)butan-2-amine as well as a process for their preparation, pharmaceutical compositions containing this novel form, and methods of use of the novel form and pharmaceutical compositions for the treatment of diabetes, obesity, and high blood pressure.

    摘要翻译： 本发明涉及（2R）-4-氧代-4- [3-三氟甲基）-5,6-二氢[1,2,4]三唑并[4,3-a]的二氢磷酸盐的新型结晶性无水物多晶型物 ]吡嗪-7（8H） - 基] -1-（2,4,5-三氟苯基）丁-2-胺以及它们的制备方法，含有这种新形式的药物组合物，以及使用该新颖的方法 用于治疗糖尿病，肥胖和高血压的形式和药物组合物。

    Process for making carbapenem compounds
    9.
    发明授权
    Process for making carbapenem compounds 有权
    制备碳青霉烯类化合物的方法

    公开(公告)号：US07022841B2

    公开(公告)日：2006-04-04

    申请号：US10485134

    申请日：2002-09-20

    申请人： Raymond Cvetovich ,  Robert Wenslow ,  John M. Williams ,  Daniel Sidler ,  Louis Crocker ,  Hsien-Hsin Tung ,  Brian K. Johnson ,  Joseph Kukura, II ,  Ulf Dolling

    发明人： Raymond Cvetovich ,  Robert Wenslow ,  John M. Williams ,  Daniel Sidler ,  Louis Crocker ,  Hsien-Hsin Tung ,  Brian K. Johnson ,  Joseph Kukura, II ,  Ulf Dolling

    IPC分类号： C07D477/20

    CPC分类号： C07D477/20 ,  C07D477/02

    摘要： The present invention relates to a process for reducing the levels of organic solvents to pharmaceutically acceptable levels in thermally unstable crystalline carbapenem solids represented by formula I: or a salt thereof, wherein R1 and R2, are the same or different, and are selected from H, alkyl, aryl, and heteroaryl, comprising washing a carbapenem solid containing organic solvent with an organic solvent containing water; and using vacuum and/or inert gas (hydrated or dry) at low temperature to produce a compound of formula I containing pharmaceutically acceptable levels of organic solvents, wherein the water content of the crystalline carbapenem solid, correcting for organic solvents, is maintained at about 13% to about 25% during the process.

    摘要翻译： 本发明涉及一种将由式I表示的热不稳定结晶碳青霉烯固体中的有机溶剂水平降低到可药用水平的方法：或其盐，其中R 1和R 2 包括相同或不同的选自H，烷基，芳基和杂芳基，包括用含水的有机溶剂洗涤含有有机溶剂的碳青霉烯固体; 并在低温下使用真空和/或惰性气体（水合或干燥）以产生含有药学上可接受水平的有机溶剂的式I化合物，其中将有机溶剂校正的结晶碳青霉烯固体的水含量保持在约 13％至25％。