公开(公告)号：WO1992015285A1

公开(公告)日：1992-09-17

申请号：PCT/US1992001762

申请日：1992-03-02

Applicant: WARNER-LAMBERT COMPANY ,  LENTZ, David, J. ,  MORONI, Antonio ,  MURTHY, Kuchi, S. ,  RADEBAUGH, Galen, W. ,  FAWZI, Mahdi ,  WILLIAMS, Michael, G. ,  CHERUKURI, Subraman, Rao ,  CHEN, Tsun-Ming

Inventor： WARNER-LAMBERT COMPANY

IPC: A61K09/20

CPC classification number: A61K9/2059 ,  A61K9/0014 ,  A61K9/1652 ,  A61K47/36

Abstract: This invention relates to controlled release compositions comprising (i) a matrix comprising starch having been processed under shear at temperatures of about 80 DEG C to about 240 DEG C in a closed volume wherein the water content of said matrix was maintained at about 5 % to about 45 % by weight based on the starch/water mix and (ii) an active ingredient, preferably a pharmaceutically active ingredient, wherein said matrix is in intimate contact with said active ingredient and wherein said matrix and pharmaceutically active ingredient are present in amounts sufficient to control the release of the pharmaceutically active ingredient in an effective dose.

Abstract translation: 本发明涉及控释组合物，其包含（i）包含在约80℃至约240℃的温度下在剪切下在封闭体积中处理的淀粉的基质，其中所述基质的水含量保持在约5％至 基于淀粉/水混合物的约45重量％和（ii）活性成分，优选药物活性成分，其中所述基质与所述活性成分紧密接触，并且其中所述基质和药物活性成分以足够的量存在 以有效剂量控制药物活性成分的释放。

公开(公告)号：WO2010039851A9

公开(公告)日：2010-06-24

申请号：PCT/US2009059058

申请日：2009-09-30

Applicant: WYETH LLC ,  BAZHINA NATALIYA ,  DONATO GEORGE JOSEPH ,  FABIAN STEVEN R ,  LOKHNAUTH JOHN ,  MEGATI SREENIVASULU ,  MELUCCI CHARLES ,  OFSLAGER CHRISTIAN ,  PATEL NIKETA ,  RADEBAUGH GALEN ,  SHAH SYED M ,  SZELIGA JAN ,  ZHANG HUYI ,  ZHU TIANMIN

Inventor： BAZHINA NATALIYA ,  DONATO GEORGE JOSEPH ,  FABIAN STEVEN R ,  LOKHNAUTH JOHN ,  MEGATI SREENIVASULU ,  MELUCCI CHARLES ,  OFSLAGER CHRISTIAN ,  PATEL NIKETA ,  RADEBAUGH GALEN ,  SHAH SYED M ,  SZELIGA JAN ,  ZHANG HUYI ,  ZHU TIANMIN

IPC: C07D471/08 ,  A61K31/485 ,  A61P1/10 ,  C07D489/08

CPC classification number: A61K31/485 ,  A61J1/05 ,  A61K9/0019 ,  A61K9/0053 ,  A61K9/08 ,  A61K9/20 ,  A61M5/178 ,  C07D471/08 ,  C07D489/08 ,  Y10T436/145555

Abstract: The present invention provides a compound of formula I wherein X", R1, and R2 are as defined herein, and compositions thereof. The compounds include and are based on an impurity of methylnaltrexone, a peripheral opioid antagonist.

Abstract translation: 本发明提供了其中X“，R 1和R 2如本文所定义的式I化合物及其组合物。该化合物包括并基于甲基纳曲酮，外周阿片样物质拮抗剂的杂质。

公开(公告)号：WO2010039851A1

公开(公告)日：2010-04-08

申请号：PCT/US2009/059058

申请日：2009-09-30

Applicant: WYETH LLC ,  BAZHINA, Nataliya ,  DONATO, George, Joseph ,  FABIAN, Steven, R. ,  LOKHNAUTH, John ,  MEGATI, Sreenivasulu ,  MELUCCI, Charles ,  OFSLAGER, Christian ,  PATEL, Niketa ,  RADEBAUGH, Galen ,  SHAH, Syed, M. ,  SZELIGA, Jan ,  ZHANG, Huyi ,  ZHU, Tianmin

Inventor： BAZHINA, Nataliya ,  DONATO, George, Joseph ,  FABIAN, Steven, R. ,  LOKHNAUTH, John ,  MEGATI, Sreenivasulu ,  MELUCCI, Charles ,  OFSLAGER, Christian ,  PATEL, Niketa ,  RADEBAUGH, Galen ,  SHAH, Syed, M. ,  SZELIGA, Jan ,  ZHANG, Huyi ,  ZHU, Tianmin

IPC: C07D471/08 ,  C07D489/08 ,  A61K31/485 ,  A61P1/10

CPC classification number: A61K31/485 ,  A61J1/05 ,  A61K9/0019 ,  A61K9/0053 ,  A61K9/08 ,  A61K9/20 ,  A61M5/178 ,  C07D471/08 ,  C07D489/08 ,  Y10T436/145555

Abstract: The present invention provides a compound of formula I: wherein X - , R 1 , and R 2 are as defined herein, and compositions thereof. The compounds are peripheral opioid receptors.

Abstract translation: 本发明提供式I化合物：其中X，R 1和R 2如本文所定义，及其组合物。 化合物是周围的阿片受体。