JP2002534388A5 - - Google Patents

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Publication number
JP2002534388A5
JP2002534388A5 JP2000592004A JP2000592004A JP2002534388A5 JP 2002534388 A5 JP2002534388 A5 JP 2002534388A5 JP 2000592004 A JP2000592004 A JP 2000592004A JP 2000592004 A JP2000592004 A JP 2000592004A JP 2002534388 A5 JP2002534388 A5 JP 2002534388A5
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JP
Japan
Prior art keywords
inhibitor
plates
nitroaniline
triplicate
assays
Prior art date
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Granted
Application number
JP2000592004A
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English (en)
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JP2002534388A (ja
JP3822439B2 (ja
Filing date
Publication date
Priority claimed from GBGB9900413.7A external-priority patent/GB9900413D0/en
Priority claimed from GBGB9917294.2A external-priority patent/GB9917294D0/en
Application filed filed Critical
Priority claimed from PCT/GB2000/000032 external-priority patent/WO2000040247A1/en
Publication of JP2002534388A publication Critical patent/JP2002534388A/ja
Publication of JP2002534388A5 publication Critical patent/JP2002534388A5/ja
Application granted granted Critical
Publication of JP3822439B2 publication Critical patent/JP3822439B2/ja
Anticipated expiration legal-status Critical
Expired - Fee Related legal-status Critical Current

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Description

アッセイは９６ウエルＥＬＩＳＡプレート中、３重測定で準備された。１０μｌの２μｇ／ｍｌのトリプシン、２６μｌの希釈阻害剤、及び１９０μｌの基質が連続して加えられた。次にプレートをＢｉｏＲａｏｄ Ｂｅｎｃｈｍａｒｋマイクロプレートリーダー中、３７℃にてインキュベーションした。阻害剤なしの酵素に対するｐ−ニトロアニリンの放出率を、４０５ｎｍにおいて１０分間測定した。
アッセイは９６ウエルＥＬＩＳＡプレート中、３重測定で準備された。１０μｌの５０μｇ／ｍｌのキモトリプシン、５０μｌの希釈阻害剤、及び１９０μｌの基質が連続して加えられた。次にプレートをＢｉｏＲａｏｄ Ｂｅｎｃｈｍａｒｋマイクロプレートリーダー中、３７℃にてインキュベーションした。阻害剤なしの酵素に対するｐ−ニトロアニリンの放出率を、４０５ｎｍにおいて１０分間測定した。
JP2000592004A 1999-01-08 2000-01-06 肥満治療用２−オキシ−４ｈ−３，１−ベンゾオキサジン−４−オン Expired - Fee Related JP3822439B2 (ja)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
GB9900413.7 1999-01-08
GBGB9900413.7A GB9900413D0 (en) 1999-01-08 1999-01-08 Inhibitors
GBGB9917294.2A GB9917294D0 (en) 1999-07-22 1999-07-22 Inhibitors
GB9917294.2 1999-07-22
PCT/GB2000/000032 WO2000040247A1 (en) 1999-01-08 2000-01-06 2-oxy-benzoxazinone derivatives for the treatment of obesity

Publications (3)

Publication Number Publication Date
JP2002534388A JP2002534388A (ja) 2002-10-15
JP2002534388A5 true JP2002534388A5 (ja) 2006-03-09
JP3822439B2 JP3822439B2 (ja) 2006-09-20

Family

ID=26314965

Family Applications (1)

Application Number Title Priority Date Filing Date
JP2000592004A Expired - Fee Related JP3822439B2 (ja) 1999-01-08 2000-01-06 肥満治療用２−オキシ−４ｈ−３，１−ベンゾオキサジン−４−オン

Country Status (24)

Country Link
US (4) US6624161B2 (ja)
EP (1) EP1143977B3 (ja)
JP (1) JP3822439B2 (ja)
KR (1) KR100678998B1 (ja)
CN (2) CN1915981B (ja)
AR (1) AR022204A1 (ja)
AT (1) ATE293447T1 (ja)
AU (1) AU765147C (ja)
CA (1) CA2359819C (ja)
CH (1) CH1143977H1 (ja)
DE (1) DE60019555C5 (ja)
DK (1) DK1143977T3 (ja)
ES (1) ES2240052T7 (ja)
HK (2) HK1047588B (ja)
HU (1) HUP0105003A3 (ja)
MX (1) MXPA01006921A (ja)
MY (1) MY122578A (ja)
NO (1) NO333922B1 (ja)
NZ (1) NZ512740A (ja)
PL (1) PL207383B1 (ja)
PT (1) PT1143977E (ja)
RU (1) RU2245331C2 (ja)
SI (1) SI1143977T1 (ja)
WO (1) WO2000040247A1 (ja)

Families Citing this family (28)

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AR022204A1 (es) * 1999-01-08 2002-09-04 Norgine Bv Compuesto, proceso para su preparacion, composicion farmaceutica y producto comestible que lo comprende.
GB0001572D0 (en) 2000-01-24 2000-03-15 Alizyme Therapeutics Ltd Inhibitors
US6504028B2 (en) * 2000-07-11 2003-01-07 The Procter & Gamble Co. Process for preparing benzoxazin-4-one polymer conjugates
AU2002331064B2 (en) 2001-08-10 2007-08-23 Palatin Technologies, Inc. Peptidomimetics of biologically active metallopeptides
EP1446125B1 (en) * 2001-08-30 2009-04-29 Alizyme Therapeutics Limited Thieno-(1,3)-oxazin-4-ones with lipase inhibiting activity
KR20040068316A (ko) * 2001-12-20 2004-07-30 오에스아이 파마슈티컬스, 인코포레이티드 판크레아 리파제 저해제 화합물, 그의 합성방법 및사용방법
US8372430B2 (en) 2002-12-17 2013-02-12 The Procter & Gamble Company Compositions, methods, and kits useful for the alleviation of gastrointestinal effects
CA2530634A1 (en) * 2003-06-12 2004-12-23 Menachem Rubinstein Methods of treating obesity and related disorders using tellurium and selenium compounds
GB0319124D0 (en) * 2003-08-14 2003-09-17 Smithkline Beecham Corp Chemical compounds
US20050239859A2 (en) * 2003-09-03 2005-10-27 Solvay Pharmaceuticals Gmbh Novel medical uses of 4,5-dihydro-1h-pyrazole derivatives having cb1- antagonistic activity
US20050124660A1 (en) * 2003-10-27 2005-06-09 Jochen Antel Novel medical uses of compounds showing CB1-antagonistic activity and combination treatment involving said compounds
US20050143441A1 (en) * 2003-10-27 2005-06-30 Jochen Antel Novel medical combination treatment of obesity involving 4,5-dihydro-1H-pyrazole derivatives having CB1-antagonistic activity
US20050244367A1 (en) * 2004-05-03 2005-11-03 Ilypsa, Inc. Phospholipase inhibitors localized in the gastrointestinal lumen
WO2006045799A2 (en) 2004-10-25 2006-05-04 Solvay Pharmaceuticals Gmbh Pharmaceutical compositions comprising cb1 cannabinoid receptor antagonists and potassium channel openers for the treatment of diabetes mellitus type i, obesity and related conditions
US20090082435A1 (en) * 2005-04-28 2009-03-26 The Regents Of The University Of California Methods, Compositions, And Compounds For Modulation Of Monoacylglycerol Lipase, Pain, And Stress-Related Disorders
PT1897558E (pt) 2005-06-09 2013-11-06 Norgine Bv Preparação sólida de 2-hexadeciloxi-6-metil-4h-3,1- benzoxazin-4-ona
JP2010254623A (ja) * 2009-04-24 2010-11-11 Takeda Chem Ind Ltd ベンゾオキサジノン化合物の結晶
DK2575768T3 (en) 2010-05-24 2018-03-12 Swedish Oat Fiber Ab Aqueous Dispersion Comprehensive Galactolipids and Procedures for their Preparation
WO2013092786A1 (en) 2011-12-23 2013-06-27 Norgine B.V. Compositions comprising cetilistat
AU2012101841A4 (en) * 2011-12-23 2013-01-17 Norgine Bv Compositions comprising cetilistat
DE202012104963U1 (de) 2012-12-19 2013-01-14 Norgine B.V. Cetilistat aufweisende Zusammensetzungen
CN103936687B (zh) * 2014-03-24 2016-03-30 重庆东得医药科技有限公司 一种制备西替利司他的方法
CN104374836A (zh) * 2014-09-19 2015-02-25 安徽安科生物工程（集团）股份有限公司 西替利司他及有关杂质的hplc测定方法
CN105622538B (zh) * 2014-10-27 2019-02-01 中国医学科学院药物研究所 一锅法高收率制备新利司他
CN104341370B (zh) * 2014-11-11 2017-02-22 山东创新药物研发有限公司 一种西替利司他的制备方法
CN105669585A (zh) * 2016-01-06 2016-06-15 北京修正创新药物研究院有限公司 一种新利司他的制备方法
CN105566164A (zh) * 2016-01-06 2016-05-11 北京修正创新药物研究院有限公司 一种新利司他杂质的制备方法
WO2018011676A1 (en) * 2016-07-11 2018-01-18 Symed Labs Limited Novel processes for the preparation of 2-oxy-benzoxazinone derivatives

Family Cites Families (15)

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DE246996C (ja)
US4657893A (en) * 1984-05-09 1987-04-14 Syntex (U.S.A.) Inc. 4H-3,1-benzoxazin-4-ones and related compounds and use as enzyme inhibitors
US4665070A (en) * 1985-06-25 1987-05-12 Syntex (U.S.A.) Inc. 2-oxy-4H-3,1-benzoxazin-4-ones and pharmaceutical use
US4745116A (en) * 1985-06-25 1988-05-17 Syntex (U.S.A.) Inc. 2-oxy-4H-3,1-benzoxazin-4-ones and related compounds and pharmaceutical use
DD246996A1 (de) * 1986-02-26 1987-06-24 Univ Leipzig Verfahren zur herstellung von gegebenenfalls substituierten 2-alkoxy- bzw. 2-aroxy-3,1-benzoxazin-4-onen
CA1309556C (en) * 1987-06-09 1992-10-27 Masayuki Kokubo 4h-3,1-benzoxazin-4-one compounds and pharmaceutical composition thereoffor the inhibition of serine proteases
US5652237A (en) 1994-09-09 1997-07-29 Warner-Lambert Company 2-substituted-4H-3, 1-benzoxazin-4-ones and benzthiazin-4-ones as inhibitors of complement C1r protease for the treatment of inflammatory processes
US5985872A (en) * 1995-05-24 1999-11-16 G.D. Searle & Co. 2-amino-benzoxazinones for the treatment of viral infections
US5776756A (en) * 1995-08-31 1998-07-07 Toyo Hakko Co., Ltd. Fermentation compositions having superoxide dismutating activity and an antihypertensive agent for treatment of constipation each having the superoxide dismutating activity
US6139833A (en) * 1997-08-08 2000-10-31 Lexicon Genetics Incorporated Targeted gene discovery
US6207371B1 (en) * 1996-10-04 2001-03-27 Lexicon Genetics Incorporated Indexed library of cells containing genomic modifications and methods of making and utilizing the same
US6136566A (en) * 1996-10-04 2000-10-24 Lexicon Graphics Incorporated Indexed library of cells containing genomic modifications and methods of making and utilizing the same
US6130214A (en) * 1997-10-27 2000-10-10 Dr. Reddy's Research Foundation Benzothiazin and benzoxazin derivatives; their preparation and uses
US6080576A (en) * 1998-03-27 2000-06-27 Lexicon Genetics Incorporated Vectors for gene trapping and gene activation
AR022204A1 (es) * 1999-01-08 2002-09-04 Norgine Bv Compuesto, proceso para su preparacion, composicion farmaceutica y producto comestible que lo comprende.

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