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1.发明公开CRYSTALLINE FORM OF 1´-(1-METHYLETHYL)- 4´-[(2-FLUORO-4-METHOXYPHENYL)METHYL]-5´-METHYL-1H-PYRAZOL-3´-O-beta-D-GLUCOPYRANOSIDE, A METHOD FOR ITS PREPARATION AND THE USE THEREOF FOR PREPARING MEDICAMENTS 审中-公开4' - [（2-氟-4-甲氧基苯基）甲基] -5'-甲基-1H-吡唑-3'-O-BETA-D-吡喃葡糖苷，METHODS - 的1,1'-（1-甲基乙基）结晶形式 其制备和它们在药品生产
公开(公告)号：EP1976859A1
公开(公告)日：2008-10-08
申请号：EP07703756.2
申请日：2007-01-10
申请人： Boehringer Ingelheim International GmbH , Ajinomoto Co., Inc. , Boehringer Ingelheim Pharma GmbH & Co. KG
发明人： KRAEMER, Gerd , MARTIN, Hans-Jürgen , ADELGOSS, Gebhard , DUGI, Klaus , DURAN, Adil , EICKELMANN, Peter , MAIER, Steffen , PINNETTI, Sabine , RITTER, Regine , SCHILCHER, Gebhard , STREICHER, Ruediger , THOMAS, Leo
IPC分类号： C07H17/02 , A61K31/7056 , A61P3/10
CPC分类号： C07H17/02
摘要： The invention relates to a crystalline form of 1´-(1-methylethyl)- 4´-[(2-fluoro-4- methoxyphenyl)methyl]-5´-methyl-1H-pyrazol-3´-O-β-D-glucopyranoside, to a method for the preparation thereof, as well as to the use thereof for preparing medicaments.
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2.发明公开METHODS FOR PREVENTING AND TREATING METABOLIC DISORDERS AND NEW PYRAZOLE-O-GLYCOSIDE DERIVATIVES 审中-公开FOR预防方法和代谢性疾病和新吡-O-糖苷衍生物的治疗
公开(公告)号：EP1912656A2
公开(公告)日：2008-04-23
申请号：EP06778010.6
申请日：2006-07-27
发明人： HIMMELSBACH, Frank , MAIER, Roland , EICKELMANN, Peter , THOMAS, Leo , BARSOUMIAN, Edward, Leon , DUGI, Klaus , PINNETTI, Sabine , RITTER, Regine , STREICHER, Ruediger , FUJITA, Koichi , HATANAKA, Toshihiro , ISHIDA, Nozomu , MAEZONO, Katsumi , OHSUMI, Koji
IPC分类号： A61K31/7056 , C07H17/02 , A61P3/04 , A61P3/10
CPC分类号： A61K31/7056 , C07H17/02
摘要： The invention relates to methods for preventing or treating metabolic disorders, for improving glycemic control, for preventing progression from impaired glucose tolerance, insulin resistance and/or from metabolic syndrome to type 2 diabetes mellitus, for preventing or treating of complications of diabetes mellitus, for reducing the weight, for preventing or treating the degeneration of pancreatic beta cells, for treating hyperinsulinemia and insulin resistance and diabetes type 1, in patients in need thereof by administering a pharmaceutical composition comprising a pyrazole-O-glycoside as defined in claim 1 , or a prodrug thereof, or a pharmaceutically acceptable salt thereof.
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3.发明公开PHARMACEUTICAL COMPOSITION COMPRISING A PYRAZOLE-O-GLUCOSIDE DERIVATIVE 审中-公开WITH A - 吡唑O-葡萄糖苷衍生物的药物组合物
公开(公告)号：EP2124970A1
公开(公告)日：2009-12-02
申请号：EP08707978.6
申请日：2008-01-18
CPC分类号： A61K45/06 , A61K9/0019 , A61K9/0031 , A61K9/02 , A61K9/145 , A61K9/1623 , A61K9/2018 , A61K9/2072 , A61K9/4858 , A61K31/7056 , A61K2300/00
摘要： The invention relates toa pharmaceutical composition comprising a pyrazole-O-glucoside derivative selected from the group of compounds (1) to (29) according to claim 1 in combination with at least one second therapeutic agent which is suitable in the treatment or prevention of one or more conditions selected from type 1 diabetes mellitus, type 2 diabetes mellitus, impaired glucose tolerance and hyperglycemia. In addition the present invention relates to methods for preventing or treating of metabolic disorders and related conditions.
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4.发明公开TRICYCLIC PYRIDINE DERIVATIVES, MEDICAMENTS CONTAINING SUCH COMPOUNDS, THEIR USE AND PROCESS FOR THEIR PREPARATION 有权三环吡啶衍生物，这种含药物，用途和方法FOR THEIR
公开(公告)号：EP2268644A1
公开(公告)日：2011-01-05
申请号：EP09716535.1
申请日：2009-03-02
发明人： WAGNER, Holger , BERTA, Daniela , GIOVANNINI, Riccardo , MAZZACANI, Alessandro , STREICHER, Ruediger , FUCHS, Klaus
IPC分类号： C07D493/04 , C07D493/10 , A61K31/4355 , A61P9/00
CPC分类号： C07D493/04 , C07D493/10
摘要： Compounds of formula (I) wherein the groups R1 to R8 have the meanings indicated in the description, the tautomers.the stereoisomers.the mixtures thereof and the salts thereof have valuable pharmacological properties.which make them useful for the treatment of cardiovascular and related disorders.
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5.发明公开SUBSTITUTED ARYLSULFONYLAMINOMETHYLPHOSPHONIC ACID DERIVATIVES, THEIR PREPARATION AND THEIR USE IN THE TREATMENT OF TYPE I AND II DIABETES MELLITUS 审中-公开取代的芳基磺酰氨基亚甲基膦酸衍生物及其制备和它们在治疗I型和II型糖尿病中的用途
公开(公告)号：EP2185571A1
公开(公告)日：2010-05-19
申请号：EP08786464.1
申请日：2008-07-25
发明人： WAGNER, Holger , LANGKOPF, Elke , ECKHARDT, Matthias , STREICHER, Ruediger , SCHOELCH, Corinna , SCHULER-METZ, Annette , PAUTSCH, Alexander
IPC分类号： C07F9/572 , C07F9/6503 , C07F9/6506 , C07F9/653 , C07F9/6541 , C07F9/6553 , C07F9/6558 , A61K31/67 , A61K31/675 , A61P3/10
CPC分类号： C07F9/5728 , C07F9/65038 , C07F9/65068 , C07F9/65324 , C07F9/6541 , C07F9/655354 , C07F9/65583 , C07F9/65586
摘要： The present invention relates to substituted arylsulphonylaminomethylphosphonic acid derivatives of general formula (I) wherein R, X, Y and Z are defined as in claim 1, the tautomers, enantiomers, diastereomers, mixtures thereof and salts thereof which have valuable pharmacological properties, particularly the suppression of the interaction of glycogen phosphorylase a with the GL subunit of glycogen-associated protein phosphatase 1 (PP1), and their use as pharmaceutical compositions.
摘要翻译： 本发明涉及通式（I）的取代的芳基磺酰基氨基甲基膦酸衍生物，其中R，X，Y和Z如权利要求1所定义，其互变异构体，对映异构体，非对映异构体，混合物及其盐具有有价值的药理学性质，特别是 抑制糖原磷酸化酶a与糖原相关蛋白磷酸酶1（PP1）的GL亚基的相互作用，以及它们作为药物组合物的用途。
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公开(公告)号：EP3820470A1
公开(公告)日：2021-05-19
申请号：EP19740509.5
申请日：2019-07-09
IPC分类号： A61K31/444 , A61K31/4725 , A61K31/505 , A61K31/55 , A61K31/553 , A61P1/16
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7.发明公开TRICYCLIC PYRIDINE DERIVATIVES, MEDICAMENTS CONTAINING SUCH COMPOUNDS, THEIR USE AND PROCESS FOR THEIR PREPARATION 有权三环吡啶衍生物，用这类化合物，它们的用途及其制造方法DRUGS
公开(公告)号：EP2536733A1
公开(公告)日：2012-12-26
申请号：EP11704227.5
申请日：2011-02-17
发明人： WAGNER, Holger , BERTA, Daniela , FUCHS, Klaus , GIOVANNINI, Riccardo , HAMPRECHT, Dieter, Wolfgang , KONETZKI, Ingo , STREICHER, Ruediger , TRIESELMANN, Thomas
IPC分类号： C07D491/04 , C07D215/56 , A61K31/4741 , A61P9/00 , A61P3/06
CPC分类号： C07D491/04 , A61K31/506 , C07D215/56 , C07D491/20
摘要： The present invention relates to compounds defined by formula (I) wherein the variables R
1 -R
8 are defined as in the description, possessing valuable pharmacological activity. Particularly, the compounds are inhibitors of cholesterol ester transfer protein (CETP) and thus are suitable for treatment and prevention of diseases which can be influenced by inhibition of this enzyme.-
8.发明授权SUBSTITUTED ARYLSULPHONYLGLYCINES, THE PREPARATION THEREOF AND THE USE THEREOF AS PHARMACEUTICAL COMPOSITIONS 有权取代ARYLSULPHONYLGLYCINE，制备方法及其用途的药物组合物
公开(公告)号：EP2121600B1
公开(公告)日：2012-07-18
申请号：EP08709013.0
申请日：2008-02-15
发明人： WAGNER, Holger , LANGKOPF, Elke , STREICHER, Ruediger , ECKHARDT, Matthias , SCHULER-METZ, Annette , PAUTSCH, Alexander , SCHOELCH, Corinna
IPC分类号： C07D209/04 , C07D401/04 , C07D401/14 , C07D403/04 , C07D403/14 , A61K31/404 , A61K31/416 , A61P3/10
CPC分类号： C07D209/04 , C07D401/04 , C07D401/14 , C07D403/04 , C07D403/14
摘要： The present invention relates to substituted arylsulphonylglycines of general formula wherein R, R4, X, Y, Z and m are defined as in claim 1, the tautomers, enantiomers, diastereomers, mixtures thereof and salts thereof, which have valuable pharmacological properties, particularly the suppression of the interaction of glycogen phosphorylase a with the GL subunit of glycogen- associated protein phosphatase 1 (PP1 ), and their use as pharmaceutical compositions.
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9.发明公开NEW ARYLSULPHONYLGLYCINE DERIVATIVES, THE PREPARATION THEREOF AND THEIR USE AS MEDICAMENTS 审中-公开新ARYLSULPHONYLGLYCINDERIVATE，生产及其作为药物
公开(公告)号：EP2279173A1
公开(公告)日：2011-02-02
申请号：EP09732153.3
申请日：2009-04-17
发明人： LANGKOPF, Elke , HIMMELSBACH, Frank , MACK, Juergen , PAUTSCH, Alexander , SCHOELCH, Corinna , SCHULER-METZ, Annette , STREICHER, Ruediger , WAGNER, Holger
IPC分类号： C07D213/40 , C07D213/74 , C07D215/40 , C07D239/26 , C07D271/06 , C07D271/10 , C07D307/52 , C07D295/15 , C07D295/108 , C07C311/21 , A61K31/47 , A61P3/10
CPC分类号： C07D271/06 , C07C311/21 , C07D213/40 , C07D213/74 , C07D215/40 , C07D239/26 , C07D271/10 , C07D295/108 , C07D295/15 , C07D307/52
摘要： The invention relates to substituted arylsulphonylglycine derivatives of general formula (I) wherein the groups R
a to R
f , A and Z are defined as in the specification and claims, which are suitable for preparing a pharmaceutical composition for the treatment of metabolic disorders, particularly type 1 or type 2 diabetes mellitus.-
10.发明公开ARYLSULFONYLAMINOMETHYLPHOSPHONIC ACID DERIVATIVES, THE PREPARATION THEREOF AND THE USE THEREOF AS PHARMACEUTICAL COMPOSITIONS 审中-公开ARYLSULFONYLAMINOMETHYLPHOSPHONSÄUREDERIVATE，生产及其用途的药物组合物
公开(公告)号：EP2200987A1
公开(公告)日：2010-06-30
申请号：EP08803622.3
申请日：2008-09-04
发明人： LANGKOPF, Elke , PAUTSCH, Alexander , SCHOELCH, Corinna , SCHULER-METZ, Annette , STREICHER, Ruediger , WAGNER, Holger
IPC分类号： C07D215/38 , C07D217/22 , C07D219/08 , C07D237/28 , C07D239/72 , C07D471/04 , A61K31/4353 , A61K31/501 , A61P3/10
CPC分类号： C07D215/38 , C07D217/22 , C07D219/08 , C07D231/56 , C07D237/28 , C07D239/42 , C07D239/72 , C07D239/74 , C07D241/42 , C07D263/56 , C07D277/66 , C07D471/04
摘要： The invention relates tosubstitutedarylsulphonylaminomethylphosphonic acid derivativesof general formula (I) wherein the groups Ra to Rf, A and Z are defined as mentioned in the specification and claims, which are suitable for preparinga medicament for the treatmentof metabolic disorders, particularlytype 1 or type 2 diabetesmellitus.
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