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41.发明授权Imidazole derivatives, their preparation and their use as intermediates for the preparation of pharmaceutical compositions and pesticides 有权咪唑衍生物，它们的制备及其作为制备药物组合物和农药的中间体的用途公开(公告)号：US07439370B2
公开(公告)日：2008-10-21
申请号：US11124798
申请日：2005-05-09
申请人： Matthias Eckhardt
发明人： Matthias Eckhardt
IPC分类号： C07D403/02 , C07D233/54
CPC分类号： C07D233/90
摘要： The invention relates to new substituted imidazoles of general formula wherein R1 to R3 and X are defined as claims, the tautomers, the enantiomers, the diastereomers, the mixtures thereof and the salts thereof, and processes for preparing them and their use as intermediates for preparing pharmaceutical compositions or pesticides.
摘要翻译： 本发明涉及以下通式的新的取代的咪唑：其中R 1至R 3和X定义为权利要求，互变异构体，对映异构体，非对映异构体，其混合物和 其盐，及其制备方法及其作为制备药物组合物或农药的中间体的用途。
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![Piperazin-1-yl and 2-([1,4]diazepan-1-yl)-imidazo[4,5-d]-pyridazin-4-ones, the preparation thereof and their use as pharmaceutical compositions](/abs-image/US/2007/05/15/US07217711B2/abs.jpg.150x150.jpg)
42.发明授权Piperazin-1-yl and 2-([1,4]diazepan-1-yl)-imidazo[4,5-d]-pyridazin-4-ones, the preparation thereof and their use as pharmaceutical compositions 有权哌嗪-1-基和2 - （[1,4]二氮杂环庚烷-1-基） - 咪唑并[4,5-d] - 哒嗪-4-酮的制备及其作为药物组合物的用途公开(公告)号：US07217711B2
公开(公告)日：2007-05-15
申请号：US11016176
申请日：2004-12-17
申请人： Matthias Eckhardt , Norbert Hauel , Frank Himmelsbach , Iris Kauffmann-Hefner , Elke Langkopf , Mohammad Tadayyon , Leo Thomas
发明人： Matthias Eckhardt , Norbert Hauel , Frank Himmelsbach , Iris Kauffmann-Hefner , Elke Langkopf , Mohammad Tadayyon , Leo Thomas
IPC分类号： C07D487/04 , A61K31/5025 , A61P3/10
CPC分类号： C07D487/04
摘要： The present invention relates to substituted imidazo[4,5-d]pyridazin-4-ones of general formula wherein R1 to R3 and n are defined as in claims 1 to 8, the tautomers, enantiomers, diastereomers, mixtures thereof and the salts thereof which have valuable pharmacological properties, particularly an inhibiting effect on the activity of the enzyme dipeptidylpeptidase-IV (DPP-IV).
摘要翻译： 本发明涉及以下通式的取代咪唑并[4,5-d]哒嗪-4-酮：其中R 1至R 3和n如权利要求1中所定义 至8，其互变异构体，对映异构体，非对映异构体，其混合物及其盐具有有价值的药理学性质，特别是对二肽基肽酶-IV（DPP-IV）的活性的抑制作用。
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43.发明申请Glucopyranosyl-substituted benzyl-benzene derivatives, medicaments containing such compounds, their use and process for their manufacture 有权吡喃葡萄糖基取代的苄基苯衍生物，含有这些化合物的药物，其用途和制备方法公开(公告)号：US20070049537A1
公开(公告)日：2007-03-01
申请号：US11468074
申请日：2006-08-29
CPC分类号： C07D309/10 , C07D407/12
摘要： Glucopyranosyl-substituted benzyl-benzene derivatives of the general formula I where the groups R1 to R6 as well as R7a, R7b, R7c are defined according to claim 1, including the tautomers, the stereoisomers thereof, the mixtures thereof and the salts thereof. The compounds according to the invention are suitable for the treatment of metabolic disorders.
摘要翻译： 基团R 1至R 6的通式I的吡喃葡糖基取代的苄基 - 苯衍生物以及R 7a，R SUP 根据权利要求1，R 7，R 7c定义为包括互变异构体，其立体异构体，其混合物及其盐。 根据本发明的化合物适用于治疗代谢性疾病。
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![Crystalline forms of 1-chloro-4-(beta-D-glucopyranos-1-yl)-2-[4-((R)-tetrahydrofuran-3-yloxy)-benzyl]-benzene, a method for its preparation and the use thereof for preparing medicaments](/abs-image/US/2006/11/09/US20060251728A1/abs.jpg.150x150.jpg)
44.发明申请Crystalline forms of 1-chloro-4-(beta-D-glucopyranos-1-yl)-2-[4-((R)-tetrahydrofuran-3-yloxy)-benzyl]-benzene, a method for its preparation and the use thereof for preparing medicaments 有权1-氯-4-（β-D-吡喃葡萄糖-1-基）-2- [4 - （（R） - 四氢呋喃-3-基氧基） - 苄基] - 苯的结晶形式，其制备方法和 其用于制备药物公开(公告)号：US20060251728A1
公开(公告)日：2006-11-09
申请号：US11408899
申请日：2006-04-21
IPC分类号： A61K9/14
CPC分类号： C07D309/10 , C07D407/12
摘要： The invention relates to crystalline forms of 1-chloro-4-(β-D-glucopyranos-1-yl)-2-[4-((R)-tetrahydrofuran-3-yloxy)-benzyl]-benzene, to a method for the preparation thereof, as well as to the use thereof for preparing medicaments.
摘要翻译： 本发明涉及1-氯-4-（β-D-吡喃葡萄糖-1-基）-2- [4 - （（R） - 四氢呋喃-3-基氧基） - 苄基] - 苯的结晶形式， 用于制备药物，以及其用于制备药物的用途。
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45.发明授权Substituted imidazo-pyridinones and imidazo-pyridazinones, the preparation thereof and their use as pharmaceutical compositions 有权取代的咪唑并 - 吡啶酮和咪唑并哒嗪酮，其制备及其作为药物组合物的用途公开(公告)号：US07109192B2
公开(公告)日：2006-09-19
申请号：US10726214
申请日：2003-12-02
申请人： Norbert Hauel , Frank Himmelsbach , Elke Langkopf , Matthias Eckhardt , Roland Maier , Michael Mark , Mohammad Tadayyon , Iris Kauffmann-Hefner
发明人： Norbert Hauel , Frank Himmelsbach , Elke Langkopf , Matthias Eckhardt , Roland Maier , Michael Mark , Mohammad Tadayyon , Iris Kauffmann-Hefner
IPC分类号： C07D487/04 , C07D471/04 , A61K31/5025 , A61K31/437
CPC分类号： C07D471/04 , C07D487/04
摘要： The present invention relates to substituted imidazo-pyridinones and imidazo-pyridazinones of general formula wherein R1 to R4 are defined as in claim 1, the tautomers, the stereoisomers, the mixtures thereof and the salts thereof, which have valuable pharmacological properties, particularly an inhibitory effect on the activity of the enzyme dipeptidylpeptidase-IV (DPP-IV).
摘要翻译： 本发明涉及通式的取代的咪唑并 - 吡啶酮和咪唑并哒嗪酮，其中R 1至R 4定义如权利要求1，互变异构体，立体异构体， 其具有有价值的药理学特性的其混合物及其盐，特别是酶二肽基肽酶-IV（DPP-IV）的活性的抑制作用。
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46.发明申请Imidazole derivatives, their preparation and their use as intermediates for the preparation of pharmaceutical compositions and pesticides 有权咪唑衍生物，它们的制备及其作为制备药物组合物和农药的中间体的用途公开(公告)号：US20050261352A1
公开(公告)日：2005-11-24
申请号：US11124798
申请日：2005-05-09
申请人： Matthias Eckhardt
发明人： Matthias Eckhardt
IPC分类号： A61K31/4172 , A61K31/4178 , C07D233/54 , C07D233/90 , C07D403/02
CPC分类号： C07D233/90
摘要： The invention relates to new substituted imidazoles of general formula wherein R1 to R3 and X are defined as in the claims, the tautomers, the enantiomers, the diastereomers, the mixtures thereof and the salts thereof, and processes for preparing them and their use as intermediates for preparing pharmaceutical compositions or pesticides.
摘要翻译： 本发明涉及通式的新的取代咪唑，其中R 1至R 3和X如权利要求中所定义，互变异构体，对映异构体，非对映异构体，混合物 及其盐，及其制备方法及其作为制备药物组合物或农药的中间体的用途。
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47.发明申请Bicyclic imidazole derivatives, the preparation thereof and their use as pharmaceutical compositions 有权双环咪唑衍生物，其制备及其作为药物组合物的用途公开(公告)号：US20050143377A1
公开(公告)日：2005-06-30
申请号：US11018894
申请日：2004-12-21
申请人： Frank Himmelsbach , Elke Langkopf , Matthias Eckhardt , Norbert Hauel , Mohammad Tadayyon , Leo Thomas
发明人： Frank Himmelsbach , Elke Langkopf , Matthias Eckhardt , Norbert Hauel , Mohammad Tadayyon , Leo Thomas
IPC分类号： A61K31/519 , A61K31/522 , A61K31/5377 , A61P3/00 , A61P19/00 , C07D473/02 , C07D473/04 , C07D473/06 , C07D487/04
CPC分类号： C07D473/04 , C07D473/06 , C07D487/04
摘要： The present invention relates to bicyclic imidazole compounds of general formula wherein R1 to R3 and A are defined as in claims 1 to 8, the tautomers, the enantiomers, the stereoisomers, the mixtures thereof and the salts thereof, which have valuable pharmacological properties, particularly an inhibiting effect on the activity of the enzyme dipeptidylpeptidase-IV (DPP-IV).
摘要翻译： 本发明涉及通式的双环咪唑化合物，其中R 1至R 3和A如权利要求1至8中所定义，互变异构体，对映异构体，立体异构体 ，其混合物及其盐具有有价值的药理学性质，特别是对二肽基肽酶-IV（DPP-IV）的活性的抑制作用。
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48.发明授权Arylisoxazoline derivatives, processes for their preparation and their use as pesticides 有权芳基恶唑啉衍生物，其制备方法及其作为农药的用途公开(公告)号：US06645984B2
公开(公告)日：2003-11-11
申请号：US10102789
申请日：2002-03-22
申请人： Ralf Braun , Oswald Ort , Karl-Josef Haack , Matthias Eckhardt , Waltraud Hempel , Maria-Theresia Thönessen
发明人： Ralf Braun , Oswald Ort , Karl-Josef Haack , Matthias Eckhardt , Waltraud Hempel , Maria-Theresia Thönessen
IPC分类号： A01N4340
CPC分类号： C07D413/10 , A01N43/80 , C07D413/14
摘要： Compounds of the formula (I), are described in which X is halogen, cyano, nitro, (C1-C4)-alkyl, (C1-C4)-alkoxy, (C1-C4)-alkylthio or (C1-C4)-alkylsulfinyl; R1 is halogen, (C1-C4)-haloalkyl, (C1-C4)-alkyl, (C1-C4)-alkoxy, (C1-C4)-haloalkoxy or cyano; m is 0 to 3; n is 1 to 5; Z is oxygen, sulfur, CH2 or NR2; R2 is CN, (C1-C4)-alkoxy-(C1-C4)-alkyl, CHO, (C1-C6)-alkylcarbonyl, (C1-C6)-alkoxycarbonyl or (CW)NR3R4; R3, R4 are H or (C1-C6)-alkyl; W is O or S; G is mono- to tetrasubstituted isoxazoline which is attached in the 3-, 4- or 5-position to the adjacent phenyl ring. The compounds are suitable for use as pesticides.
摘要翻译： 其中X为卤素，氰基，硝基，（C 1 -C 4） - 烷基，（C 1 -C 4） - 烷氧基，（C 1 -C 4） - 烷硫基或（C 1 -C 4） - 烷基亚磺酰基 R 1是卤素，（C 1 -C 4） - 卤代烷基，（C 1 -C 4） - 烷基，（C 1 -C 4） - 烷氧基，（C 1 -C 4） - 卤代烷氧基或氰基; m是0-3; 1至5; Z是氧，硫，CH 2或NR 2; R 2是CN，（C 1 -C 4） - 烷氧基 - （C 1 -C 4） - 烷基，CHO，（C 1 -C 6） - 烷基羰基， （C 1 -C 6） - 烷氧基羰基或（CW）NR 3 R 4; R 3，R 4是H或（C 1 -C 6） - 烷基; W是O或S; 到四取代的异恶唑啉，其连接在相邻的苯环的3-，4-或5-位上。 该化合物适合用作农药。
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49.发明授权公开(公告)号：US09328072B2
公开(公告)日：2016-05-03
申请号：US13922889
申请日：2013-06-20
IPC分类号： C07D401/06 , C07D417/06 , C07D413/14 , C07D221/06 , C07D471/04 , C07D221/10 , C07D401/12 , C07D401/14 , C07D405/14 , C07D498/04
CPC分类号： C07D221/10 , C07D221/06 , C07D221/16 , C07D401/04 , C07D401/06 , C07D401/12 , C07D401/14 , C07D405/04 , C07D405/14 , C07D417/06 , C07D471/04 , C07D498/04
摘要： The present invention relates to compounds defined by formula I wherein the variables R1, R2, R3, R4, and m are defined as in claim 1, possessing valuable pharmacological activity. Particularly, the compounds are inhibitors of 11β-hydroxysteroid dehydrogenase (HSD) 1 and thus are suitable for treatment and prevention of diseases which can be influenced by inhibition of this enzyme, such as metabolic diseases, in particular diabetes type 2, obesity, and dyslipidemia.
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50.发明授权Alicyclic carboxylic acid derivatives of benzomorphans and related scaffolds, medicaments containing such compounds and their use 有权苯并呋喃和相关支架的脂环族羧酸衍生物，含有这些化合物的药物及其应用公开(公告)号：US09073870B2
公开(公告)日：2015-07-07
申请号：US14191951
申请日：2014-02-27
IPC分类号： A61K31/439 , C07D221/22 , C07D221/26 , C07D471/18 , C07D491/18 , C07D401/06 , C07D401/08 , C07D401/12 , C07D405/06 , C07D405/12 , C07D491/08
CPC分类号： C07D221/26 , C07D221/22 , C07D401/06 , C07D401/08 , C07D401/12 , C07D405/06 , C07D405/12 , C07D471/18 , C07D491/08 , C07D491/18
摘要： The present invention relates to compounds defined by formula I wherein the groups A, B, X, m, n and o are defined as in claim 1, possessing valuable pharmacological activity. Particularly the compounds are inhibitors of 11β-hydroxysteroid dehydrogenase (HSD) 1 and thus are suitable for treatment and prevention of diseases which can be influenced by inhibition of this enzyme, such as metabolic diseases, in particular diabetes type 2, obesity and dyslipidemia.
摘要翻译： 本发明涉及由式I定义的化合物，其中基团A，B，X，m，n和o如权利要求1所定义，具有有价值的药理学活性。 特别地，化合物是11β-羟基类固醇脱氢酶（HSD）1的抑制剂，因此适用于治疗和预防可受该酶抑制影响的疾病，如代谢疾病，特别是2型糖尿病，肥胖症和血脂异常。
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