公开(公告)号：US07632834B2

公开(公告)日：2009-12-15

申请号：US12101462

申请日：2008-04-11

申请人： Thierry Bouyssou ,  Ingo Konetzki ,  Philipp Lustenberger ,  Juergen Mack ,  Andreas Schnapp ,  Dieter Wiedenmayer ,  Christoph Hoenke ,  Klaus Rudolf

发明人： Thierry Bouyssou ,  Ingo Konetzki ,  Philipp Lustenberger ,  Juergen Mack ,  Andreas Schnapp ,  Dieter Wiedenmayer ,  Christoph Hoenke ,  Klaus Rudolf

IPC分类号： A61K31/538 ,  A61K31/536 ,  C07D413/12 ,  C07D413/14

CPC分类号： C07D265/36 ,  C07D413/12

摘要： A compound of formula 1′″ wherein: V is —CH2—, —NH—, or —O—; Ra and Rb are each independently hydrogen, C1-4-alkyl, or halogen-C1-4-alkyl, or Ra and Rb together are a C2-5-alkylene bridge wherein one or more hydrogen atoms are optionally replaced by halogen; R1 and R1′ are each independently hydrogen, C1-6-alkyl, C3-6-cycloalkyl, halogen-C1-6-alkyl, halogen-C3-6-cycloalkyl, or C1-6-alkylene-C3-6-cycloalkyl, or R1 and R1′ together are a C2-5-alkylene bridge wherein one or more hydrogen atoms are optionally replaced by halogen; R2, R2′, R2″, and R2′″ are each independently hydrogen, C1-6-alkyl, halogen-C1-6-alkylene, OH, HO—C1-6-alkylene, —O—C1-6-alkyl, C6-10-aryl, C6-10-aryl-C1-4-alkylene, C6-10-aryl-C1-6-alkylene-O, COOH, COOC1-6-alkyl, O—C1-6-alkylene-COOH, O—C1-6-alkylene-COOC1-6-alkyl, NHSO2—C1-6-alkyl, CN, NH2, NH—C1-6-alkyl, N(C1-6-alkyl)2, NO2, S—C1-6-alkyl, SO2—C1-6-alkyl, SO—C1-6-alkyl, O(CO)C1-6-alkyl, COC1-6-alkyl, NHCOC1-6-alkyl, or halogen; and n is 0, 1, or 2, or an optical isomer thereof, or a corresponding acid addition salt thereof with a pharmacologically acceptable acid, and the use thereof as pharmaceutical compositions, particularly for the treatment of inflammatory and obstructive respiratory complaints.

摘要翻译： 式1“'的化合物，其中：V是-CH 2 - ， - NH-或-O-; R a和R b各自独立地为氢，C 1-4 - 烷基或卤素-C 1-4 - 烷基，或者R a和R b一起是C 2-5亚烷基桥，其中一个或多个氢原子任选被卤素取代; R 1和R 1'各自独立地为氢，C 1-6 - 烷基，C 3-6 - 环烷基，卤素-C 1-6 - 烷基，卤素-C 3-6环烷基或C 1-6亚烷基-C 3-6环烷基， 或者R1和R1'一起是C2-5亚烷基桥，其中一个或多个氢原子任选地被卤素取代; R 2，R 2'，R 2“和R 2”各自独立地为氢，C 1-6 - 烷基，卤素-C 1-6亚烷基，OH，HO-C 1-6 - 亚烷基，-O-C 1-6 - 烷基，C 6-10 - 芳基，C 6-10 - 芳基-C 1-4 - 亚烷基，C 6-10 - 芳基-C 1-6 - 亚烷基-O，COOH，COOC 1-6 - 烷基，O-C 1-6亚烷基 - COOH，O-C 1-6亚烷基-COOC 1-6 - 烷基，NHSO 2 -C 1-6 - 烷基，CN，NH 2，NH-C 1-6 - 烷基，N（C 1-6 - 烷基）2，NO 2， C 1-6 - 烷基，SO 2 -C 1-6 - 烷基，SO-C 1-6 - 烷基，O（CO）C 1-6 - 烷基，CO C 1-6 - 烷基，NHCOC 1-6 - 烷基或卤素; 和n为0,1或2，或其光学异构体或其与药理学上可接受的酸的相应的酸加成盐，以及其作为药物组合物的用途，特别是用于治疗炎性和阻塞性呼吸道疾病。

公开(公告)号：US07375104B2

公开(公告)日：2008-05-20

申请号：US11600417

申请日：2006-11-15

申请人： Thierry Bouyssou ,  Ingo Konetzki ,  Philipp Lustenberger ,  Juergen Mack ,  Andreas Schnapp ,  Dieter Wiedenmayer ,  Christoph Hoenke ,  Klaus Rudolf

发明人： Thierry Bouyssou ,  Ingo Konetzki ,  Philipp Lustenberger ,  Juergen Mack ,  Andreas Schnapp ,  Dieter Wiedenmayer ,  Christoph Hoenke ,  Klaus Rudolf

IPC分类号： C07D413/12 ,  C07D413/14 ,  A61K31/538 ,  A61K31/536

CPC分类号： C07D265/36 ,  C07D413/12

摘要： A compound of formula 1′ wherein: V is —CH2—, —NH—, or —O—; Ra and Rb are each independently hydrogen, C1-4-alkyl, or halogen-C1-4-alkyl, or Ra and Rb together are a C2-5-alkylene bridge wherein one or more hydrogen atoms are optionally replaced by halogen; R1 and R1′ are each independently hydrogen, C1-6-alkyl, C3-6-cycloalkyl, halogen-C1-6-alkyl, halogen-C3-6-cycloalkyl, or C1-6-alkylene-C3-6-cycloalkyl, or R1 and R1′ together are a C2-5-alkylene bridge wherein one or more hydrogen atoms are optionally replaced by halogen; R2, R2′, R2″, and R′″ are each independently hydrogen, C1-6-alkyl, halogen-C1-6-alkylene, OH, HO—C1-6-alkylene, —O—C1-6-alkyl, C6-10-aryl, C6-10-aryl-C1-4-alkylene, C6-10-aryl-C1-6-alkylene-O, COOH, COOC1-6-alkyl, O—C1-6-alkylene-COOH, O—C1-6-alkylene-COOC1-6-alkyl, NHSO2—C1-6-alkyl, CN, NH2, NH—C1-6-alkyl, N(C1-6-alkyl)2, NO2, S—C1-6-alkyl, SO2—C1-6-alkyl, SO—C1-6-alkyl, O(CO)C1-6-alkyl, COC1-6-alkyl, NHCOC1-6-alkyl, or halogen; and n is 0, 1, or 2, or an optical isomer thereof, or a corresponding acid addition salt thereof with a pharmacologically acceptable acid, and the use thereof as pharmaceutical compositions, particularly for the treatment of inflammatory and obstructive respiratory complaints.

公开(公告)号：US20050227975A1

公开(公告)日：2005-10-13

申请号：US11029451

申请日：2005-01-05

申请人： Thierry Bouyssou ,  Ingo Konetzki ,  Philipp Lustenberger ,  Juergen Mack ,  Andreas Schnapp ,  Dieter Wiedenmayer ,  Christoph Hoenke ,  Klaus Rudolf

发明人： Thierry Bouyssou ,  Ingo Konetzki ,  Philipp Lustenberger ,  Juergen Mack ,  Andreas Schnapp ,  Dieter Wiedenmayer ,  Christoph Hoenke ,  Klaus Rudolf

IPC分类号： A61K31/4709 ,  A61K31/517 ,  A61K31/538 ,  C07D265/36 ,  C07D413/02 ,  C07D413/12 ,  C07D43/02

CPC分类号： C07D265/36 ,  C07D413/12

摘要： The present invention relates to compounds of formula 1 wherein the groups X, Ra, Rb, R1, R1′, R2, R2′, R2″, R2′″, V and n may have the meanings given in the claims and in the specification, and the use thereof as pharmaceutical compositions, particularly for the treatment of inflammatory and obstructive respiratory complaints.

摘要翻译： 本发明涉及式1的化合物，其中基团X，R a，R b，R 1，R 1， R 2，R 2，R 2，R“2”，R“2”，R“2” ，V和n可以具有权利要求书和说明书中给出的含义，以及其作为药物组合物的用途，特别是用于治疗炎性和阻塞性呼吸道疾病。

公开(公告)号：US07160882B2

公开(公告)日：2007-01-09

申请号：US11029451

申请日：2005-01-05

申请人： Thierry Bouyssou ,  Ingo Konetzki ,  Philipp Lustenberger ,  Juergen Mack ,  Andreas Schnapp ,  Dieter Wiedenmayer ,  Christoph Hoenke ,  Klaus Rudolf

发明人： Thierry Bouyssou ,  Ingo Konetzki ,  Philipp Lustenberger ,  Juergen Mack ,  Andreas Schnapp ,  Dieter Wiedenmayer ,  Christoph Hoenke ,  Klaus Rudolf

IPC分类号： C07D413/12 ,  C07D413/14 ,  A61K31/538 ,  A61K31/536

CPC分类号： C07D265/36 ,  C07D413/12

摘要： The present invention relates to compounds of formula 1 wherein the groups X, Ra, Rb, R1, R1′, R2, R2′, R2″, R2′″, V and n may have the meanings given in the claims and in the specification, and the use thereof as pharmaceutical compositions, particularly for the treatment of inflammatory and obstructive respiratory complaints.

摘要翻译： 本发明涉及式1的化合物，其中基团X，R a，R b，R 1，R 1， R 2，R 2，R 2，R“2”，R“2”，R“2” ，V和n可以具有权利要求书和说明书中给出的含义，以及其作为药物组合物的用途，特别是用于治疗炎性和阻塞性呼吸道疾病。

公开(公告)号：US07786111B2

公开(公告)日：2010-08-31

申请号：US12258830

申请日：2008-10-27

申请人： Ingo Konetzki ,  Kurt Schromm ,  Hermann Schollenberger ,  Sabine Pestel ,  Andreas Schnapp ,  Thierry Bouyssou ,  Frank Buettner ,  Claudia Heine ,  Klaus Rudolf ,  Philipp Lustenberger ,  Christoph Hoenke

发明人： Ingo Konetzki ,  Kurt Schromm ,  Hermann Schollenberger ,  Sabine Pestel ,  Andreas Schnapp ,  Thierry Bouyssou ,  Frank Buettner ,  Claudia Heine ,  Klaus Rudolf ,  Philipp Lustenberger ,  Christoph Hoenke

IPC分类号： C07D265/36 ,  A61K31/538

CPC分类号： A61K31/535 ,  A61K31/538 ,  C07D265/36

摘要： A pharmaceutical composition comprising a compound of formula 1 wherein: n is 1 or 2; R1 is hydrogen, C1-C4-alkyl, halogen, OH, or —O—C1-C4-alkyl; R2 is hydrogen, C1-C4-alkyl, halogen, OH, or —O—C1-C4-alkyl; R3 is hydrogen, C1-C4-alkyl, OH, halogen, —O—C1-C4-alkyl, —O—C1-C4-alkylene-COOH, or —O—C1-C4-alkylene-CO—O—C1-C4-alkyl, or an acid addition salt thereof with a pharmacologically acceptable acid, or a solvate or hydrate thereof; and a pharmaceutically acceptable excipient or carrier, and methods for using the pharmaceutical formulation in the treatment of chronic obstructive pulmonary disease (COPD).

公开(公告)号：US07423035B2

公开(公告)日：2008-09-09

申请号：US11125757

申请日：2005-05-10

申请人： Ingo Konetzki ,  Thierry Bouyssou ,  Philipp Lustenberger ,  Andreas Schnapp ,  Christoph Hoenke ,  Klaus Rudolf ,  Marco Santagostino

发明人： Ingo Konetzki ,  Thierry Bouyssou ,  Philipp Lustenberger ,  Andreas Schnapp ,  Christoph Hoenke ,  Klaus Rudolf ,  Marco Santagostino

IPC分类号： C07D265/36 ,  A61K31/538 ,  A61K31/138

CPC分类号： C07D265/36 ,  C07C215/60 ,  C07C215/68 ,  C07C217/74 ,  C07C311/08 ,  C07C2601/02 ,  C07C2601/08 ,  C07C2601/14 ,  C07D215/227

摘要： The present invention relates to compounds of formula 1 wherein the groups R1, R2, R3, R4, R5, R6, R7, R8, n, m and X may have the meanings given in the claims and in the specification, and the use thereof as pharmaceutical compositions, particularly for the treatment of inflammatory and obstructive respiratory complaints.

摘要翻译： 本发明涉及式1化合物，其中基团R 1，R 2，R 3，R 4， >，R 5，R 6，R 7，R 8，n，m和X可以具有 在权利要求和说明书中给出的含义，以及作为药物组合物的用途，特别是用于治疗炎性和阻塞性呼吸道疾病。

公开(公告)号：US08044046B2

公开(公告)日：2011-10-25

申请号：US11132075

申请日：2005-05-18

申请人： Ingo Konetzki ,  Kurt Schromm ,  Hermann Schollenberger ,  Sabine Pestel ,  Andreas Schnapp ,  Thierry Bouyssou ,  Frank Buettner ,  Claudia Heine ,  Philipp Lustenberger ,  Christoph Hoenke ,  Klaus Rudolf

发明人： Ingo Konetzki ,  Kurt Schromm ,  Hermann Schollenberger ,  Sabine Pestel ,  Andreas Schnapp ,  Thierry Bouyssou ,  Frank Buettner ,  Claudia Heine ,  Philipp Lustenberger ,  Christoph Hoenke ,  Klaus Rudolf

IPC分类号： C07D265/36 ,  A61K31/538

CPC分类号： A61K31/535 ,  A61K31/538 ,  C07D265/36

摘要： A pharmaceutical composition comprising a compound of formula 1 wherein: n is 1 or 2; R1 is hydrogen, C1-C4-alkyl, halogen, OH, or —O—C1-C4-alkyl; R2 is hydrogen, C1-C4-alkyl, halogen, OH, or —O—C1-C4-alkyl; R3 is hydrogen, C1-C4-alkyl, OH, halogen, —O—C1-C4-alkyl, —O—C1-C4-alkylene-COOH, or —O—C1-C4-alkylene-CO—O—C1-C4-alkyl, or an acid addition salt thereof with a pharmacologically acceptable acid, or a solvate or hydrate thereof; and a pharmaceutically acceptable excipient or carrier, and methods for using the pharmaceutical formulation in the treatment of chronic obstructive pulmonary disease (COPD).

摘要翻译： 一种药物组合物，其包含式1的化合物，其中：n为1或2; R1是氢，C1-C4-烷基，卤素，OH或-O-C1-C4-烷基; R2是氢，C1-C4-烷基，卤素，OH或-O-C1-C4-烷基; R3是氢，C1-C4烷基，OH，卤素，-O-C1-C4-烷基，-O-C1-C4-亚烷基-COOH或-O-C1-C4-亚烷基-CO-O-C1- C4烷基或其酸加成盐与其药理学可接受的酸或其溶剂合物或水合物; 和药学上可接受的赋形剂或载体，以及使用该药物制剂治疗慢性阻塞性肺疾病（COPD）的方法。

公开(公告)号：US20070155741A1

公开(公告)日：2007-07-05

申请号：US11677112

申请日：2007-02-21

申请人： Ingo KONETZKI ,  Kurt Schromm ,  Hermann Schollenberger ,  Sabine Pestel ,  Andreas Schnapp ,  Thierry Bouyssou ,  Frank Buettner ,  Claudia Heine ,  Philipp Lustenberger ,  Christoph Hoenke ,  Klaus Rudolf

发明人： Ingo KONETZKI ,  Kurt Schromm ,  Hermann Schollenberger ,  Sabine Pestel ,  Andreas Schnapp ,  Thierry Bouyssou ,  Frank Buettner ,  Claudia Heine ,  Philipp Lustenberger ,  Christoph Hoenke ,  Klaus Rudolf

IPC分类号： A61K31/538 ,  C07D265/36

CPC分类号： A61K31/535 ,  A61K31/538 ,  C07D265/36

摘要： A pharmaceutical composition comprising a compound of formula 1 wherein: n is 1 or 2; R1 is hydrogen, C1-C4-alkyl, halogen, OH, or —O—C1-C4-alkyl; R2 is hydrogen, C1-C4-alkyl, halogen, OH, or —O—C1-C4-alkyl; R3 is hydrogen, C1-C4-alkyl, OH, halogen, —O—C1-C4-alkyl, —O—C1-C4-alkylene-COOH, or —O—C1-C4-alkylene-CO—O—C1-C4-alkyl, or an acid addition salt thereof with a pharmacologically acceptable acid, or a solvate or hydrate thereof; and a pharmaceutically acceptable excipient or carrier, and methods for using the pharmaceutical formulation in the treatment of chronic obstructive pulmonary disease (COPD).

摘要翻译： 一种药物组合物，其包含式1的化合物，其中：n为1或2; R 1是氢，C 1 -C 4 - 烷基，卤素，OH或-OC 1 - C 4 - 烷基; R 2是氢，C 1 -C 4 - 烷基，卤素，OH或-OC 1 - C 4 - 烷基; R 3是氢，C 1 -C 4 - 烷基，OH，卤素，-OC 1 -C - 烷基，-OC 1 -C 4 - 亚烷基-COOH或-OC 1 -C 3 - 或其酸加成盐与药理学上可接受的酸或溶剂化物或其盐或其盐或其盐 水合物; 和药学上可接受的赋形剂或载体，以及使用该药物制剂治疗慢性阻塞性肺疾病（COPD）的方法。

公开(公告)号：US20050239778A1

公开(公告)日：2005-10-27

申请号：US11109094

申请日：2005-04-19

申请人： Ingo Konetzki ,  Thierry Bouyssou ,  Philipp Lustenberger ,  Michael Pieper ,  Andreas Schnapp ,  Christoph Hoenke ,  Sabine Pestel ,  Klaus Rudolf ,  Michel Pairet

发明人： Ingo Konetzki ,  Thierry Bouyssou ,  Philipp Lustenberger ,  Michael Pieper ,  Andreas Schnapp ,  Christoph Hoenke ,  Sabine Pestel ,  Klaus Rudolf ,  Michel Pairet

IPC分类号： A61K31/538 ,  A61K31/56

CPC分类号： A61K45/06 ,  A61K31/538 ,  A61K31/56 ,  A61K2300/00

摘要： The present invention relates to new medicament combinations which contain in addition to one or more, preferably one, compound of general formula 1 wherein the groups R1, R2 and R3 may have the meanings given in the claims and in the specification, at least one other active substance 2, processes for preparing them and their use as pharmaceutical compositions.

摘要翻译： 本发明涉及除了一种或多种，​​优选一种通式1化合物外还含有基团R 1，R 2和R 2的新药物组合， SUP> 3可以具有权利要求和说明书中给出的含义，至少一种其它活性物质2，其制备方法及其作为药物组合物的用途。

公开(公告)号：US07727984B2

公开(公告)日：2010-06-01

申请号：US11677112

申请日：2007-02-21

申请人： Ingo Konetzki ,  Kurt Schromm ,  Hermann Schollenberger ,  Sabine Pestel ,  Andreas Schnapp ,  Thierry Bouyssou ,  Frank Buettner ,  Claudia Heine ,  Philipp Lustenberger ,  Christoph Hoenke ,  Klaus Rudolf

发明人： Ingo Konetzki ,  Kurt Schromm ,  Hermann Schollenberger ,  Sabine Pestel ,  Andreas Schnapp ,  Thierry Bouyssou ,  Frank Buettner ,  Claudia Heine ,  Philipp Lustenberger ,  Christoph Hoenke ,  Klaus Rudolf

IPC分类号： C07D265/36 ,  A61K31/538

CPC分类号： A61K31/535 ,  A61K31/538 ,  C07D265/36

摘要： A pharmaceutical composition comprising a compound of formula 1 wherein: n is 1 or 2; R1 is hydrogen, C1-C4-alkyl, halogen, OH, or —O—C1-C4-alkyl; R2 is hydrogen, C1-C4-alkyl, halogen, OH, or —O—C1-C4-alkyl; R3 is hydrogen, C1-C4-alkyl, OH, halogen, —O—C1-C4-alkyl, —O—C1-C4-alkylene-COOH, or —O—C1-C4-alkylene-CO—O—C1-C4-alkyl, or an acid addition salt thereof with a pharmacologically acceptable acid, or a solvate or hydrate thereof; and a pharmaceutically acceptable excipient or carrier, and methods for using the pharmaceutical formulation in the treatment of chronic obstructive pulmonary disease (COPD).

摘要翻译： 一种药物组合物，其包含式1的化合物，其中：n为1或2; R1是氢，C1-C4-烷基，卤素，OH或-O-C1-C4-烷基; R2是氢，C1-C4-烷基，卤素，OH或-O-C1-C4-烷基; R3是氢，C1-C4烷基，OH，卤素，-O-C1-C4-烷基，-O-C1-C4-亚烷基-COOH或-O-C1-C4-亚烷基-CO-O-C1- C4烷基或其酸加成盐与其药理学可接受的酸或其溶剂合物或水合物; 和药学上可接受的赋形剂或载体，以及使用该药物制剂治疗慢性阻塞性肺疾病（COPD）的方法。