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1. 发明申请

WO2002102771A1 TRYPTASE INHIBITORS 审中-公开
标题翻译： TRYPTASE抑制剂
公开(公告)号：WO2002102771A1
公开(公告)日：2002-12-27
申请号：PCT/EP2002/006537
申请日：2002-06-14
申请人： ALTANA PHARMA AG , MARTIN, Thomas , ULRICH, Wolf-Rüdiger
发明人： MARTIN, Thomas , ULRICH, Wolf-Rüdiger , BÄR, Thomas , STADLWIESER, Josef , WOLLIN, Stefan-Lutz , ZECH, Karl , SOMMERHOFF, Christian P.
IPC分类号： C07D207/16
CPC分类号： C07D207/16
摘要： Compounds of formula (I) in which M, B1, B2, R1, R2, R6, R7, K1 and K2 have the meanings indicated in the description are novel active tryptase inhibitors.
摘要翻译：其中M，B1，B2，R1，R2，R6，R7，K1和K2具有本说明书所述含义的式（I）化合物是新型活性类胰蛋白酶抑制剂。

2. 发明申请

WO2002074733A3 TRYPTASE-INHIBITORS 审中-公开
公开(公告)号：WO2002074733A3
公开(公告)日：2002-09-26
申请号：PCT/EP2002/002675
申请日：2002-03-12
申请人： ALTANA PHARMA AG , MARTIN, Thomas , ULRICH, Wolf-Rüdiger
发明人： MARTIN, Thomas , ULRICH, Wolf-Rüdiger , BÄR, Thomas , STADLWIESER, Josef , WOLLIN, Stefan-Lutz , ZECH, Karl , SOMMERHOFF, Christian, P.
IPC分类号： C07C271/20
摘要： Compounds of the formula I, wherein M, A1, A2, K1 and K2 have the meanings as indicated below are tryptase inhibitors. M is a central building block containing an acetylene containing linking group. A1 and A2 are carbonyl containing linking groups K1 is -B3-X1, -B3-Y1 or B3-Z1-B5-X1, K2 is -B4-X2, -B4-Y2 or -B4-Z2-B6-X2, B3 and B4 are identical or different and are a bond or 1-4C-alkylene, B5 and B6 are identical or different and are a bond or 1-2C-alkylene, X1 and X2 are identical or different and are amino, aminocarbonyl or amidino, Y1 and Y2 are imidazol -1-yl, Z1 and Z2 are identical or different and are 5,2-pyridinylene, 6-methyl-5,2-pyridinylene, 4,1-piperidinylene, 3,6-indazolylene, 3,6-indolylene, 1,3-phenylene, 1,4-phenylene, 1,3,-cyclohexalene or 1,4-cyclohexylene, the salts of these compounds, and the N-oxides of the nitrogen-containing heteroalryls, heteroarylenes and heterocycloalkylenes, and their salts, where all those compounds are excluded in which, owing to the meaning of the variables, there would be a direct linkage of two hereroatoms or two carbonyl groups.

3. 发明申请

WO2004012731A1 PYRROLIDINE DERIVATIVES AS TRYPTASE INHIBITORS 审中-公开
标题翻译：吡咯啉衍生物作为TRYPTASE抑制剂
公开(公告)号：WO2004012731A1
公开(公告)日：2004-02-12
申请号：PCT/EP2003/008127
申请日：2003-07-24
申请人： ALTANA PHARMA AG , MARTIN, Thomas , ULRICH, Wolf-Rüdiger
发明人： MARTIN, Thomas , ULRICH, Wolf-Rüdiger , MARTIN, Thomas , ULRICH,Wolf-Rüdiger , BÄR, Thomas , SOMMERHOFF, Christian, P.
IPC分类号： A61K31/40
CPC分类号： C07D401/12 , C07D207/16
摘要： Compounds of a certain formula 1 in which M, B1, B2, R2, K1 and K2 have the meanings indicated in the description are novel effective tryptase inhibitors.
摘要翻译：其中M，B1，B2，R2，K1和K2具有说明书中所示含义的某种式1的化合物是新型有效的类胰蛋白酶抑制剂。

4. 发明申请

WO2002074732A3 TRYPTASE-INHIBITORS 审中-公开
公开(公告)号：WO2002074732A3
公开(公告)日：2002-09-26
申请号：PCT/EP2002/002674
申请日：2002-03-12
申请人： ALTANA PHARMA AG , MARTIN, Thomas , ULRICH, Wolf-Rüdiger
发明人： MARTIN, Thomas , ULRICH, Wolf-Rüdiger , BÄR, Thomas , STADLWIESER, Josef , WOLLIN, Stefan-Lutz , ZECH, Karl , SOMMERHOFF, Christian, P.
IPC分类号： C07C237/20
摘要： Compounds of formula (I), wherein M, A1, A2, K1, and K2 have the meanings as indicated below are novel effective tryptase inhibitors. M is a central building block containing at least one acetylene moiety. A 1 and A 2 are carboxamide containing linking groups. K1 is -B3-X1, -B3-Y1 or -B3-Z1-B5-X1, K2 is -B4-X2, -B4-Y2 or -B4-Z2-B6-X2, B3 and B4 are identical or different and are a bond or 1-4C-alkylene, B5 and B6 are identical or different and are a bond or 1-2C-alkylene, X1 and X2 are identical or different and are amino, aminocarbonyl or amidino, Y1 and Y2 are imidazol-1-yl, Z1 and Z2 are identical or different and are 5,2-pyridinylene, 6-methyl-5,2-pyridinylene, 4,1-pyridinylene, 3,6-indazolylene, 3,6-indolylene, 1,3-phenylene, 1,4-phenylene, 1,3-cyclohexylene or 1,4-cyclohexylene, the salts of these compounds, and the N-oxides of the nitrogen-containing heteroaryls, heteroarylenes and heterocycloalkylenes, and their salts, where all those compounds are excluded in which, owing to the meaning of the variables A1, A2, A3, A4, B3, B4, Y1, Y2, Z1, Z2, X1 or X2, there would be a direct linkage of two heteroatoms.

5. 发明申请

WO2002074732A2 TRYPTASE-INHIBITORS 审中-公开
标题翻译：类胰蛋白酶抑制剂
公开(公告)号：WO2002074732A2
公开(公告)日：2002-09-26
申请号：PCT/EP2002/002674
申请日：2002-03-12
申请人： ALTANA PHARMA AG , MARTIN, Thomas , ULRICH, Wolf-Rüdiger
发明人： MARTIN, Thomas , ULRICH, Wolf-Rüdiger , BÄR, Thomas , STADLWIESER, Josef , WOLLIN, Stefan-Lutz , ZECH, Karl , SOMMERHOFF, Christian, P.
IPC分类号： C07C237/20
CPC分类号： C07C237/20
摘要： Compounds of the formula I, wherein M, A1, A2, K1 and K2 have the meanings as indicated in the description are novel effective tryptase inhibitors.
摘要翻译：式I的化合物，其中M，A1，A2，K1和K2具有如说明书中指出的含义，是新的有效的类胰蛋白酶抑制剂。

6. 发明申请

WO1996036626A1 CYCLOHEXYL DIHYDROBENZOFURANES 审中-公开
标题翻译： CYCLOHEXYLDIHYDROBENZOFURANE
公开(公告)号：WO1996036626A1
公开(公告)日：1996-11-21
申请号：PCT/EP1996002055
申请日：1996-05-14
申请人： BYK GULDEN LOMBERG CHEMISCHE FABRIK GMBH , ULRICH, Wolf-Rüdiger , MARTIN, Thomas
发明人： BYK GULDEN LOMBERG CHEMISCHE FABRIK GMBH , AMSCHLER, Hermann , BÄR, Thomas , FLOCKERZI, Dieter , GUTTERER, Beate , THIBAUT, Ulrich , HATZELMANN, Armin , BOSS, Hildegard , HÄFNER, Dietrich , KLEY, Hans-Peter , BEUME, Rolf
IPC分类号： C07D307/94
CPC分类号： C07D307/94 , C07D307/86 , Y10S514/826 , Y10S514/886 , Y10S514/889 , Y10S514/914
摘要： Compounds having the formula (I), in which R1, R2, R3, R4 and R5 have the meanings given in the description, are new powerful PDE inhibitors.
摘要翻译：式（I）化合物，其中R1，R2，R3，R4和R5具有说明书中给出的含义，是新的有效的PDE抑制剂。

7. 发明申请

WO1998022453A1 SUBSTITUTED DIHYDROBENZOFURANS AS PDE INHIBITORS 审中-公开
标题翻译：替代二氢苯并呋喃作为PDE抑制剂
公开(公告)号：WO1998022453A1
公开(公告)日：1998-05-28
申请号：PCT/EP1997006248
申请日：1997-11-11
申请人： BYK GULDEN LOMBERG CHEMISCHE FABRIK GMBH , MARTIN, Thomas , ULRICH, Wolf-Rüdiger
发明人： BYK GULDEN LOMBERG CHEMISCHE FABRIK GMBH , AMSCHLER, Hermann , BÄR, Thomas , FLOCKERZI, Dieter , GUTTERER, Beate , THIBAUT, Ulrich , HATZELMANN, Armin , BOSS, Hildegard , BEUME, Rolf , KLEY, Hans-Peter , HÄFNER, Dietrich
IPC分类号： C07D307/94
CPC分类号： C07D405/04 , C07D307/94 , C07D407/04 , C07D409/04 , C07D493/10 , C07F9/65517
摘要： Compounds of formula (I) in which R1 is 1-6C-alkoxy, 3-7C-cycloalkoxy, 3-7C-cycloalkylmethoxy, benzyloxy or 1-4C-alkoxy which is completely or predominantly substituted by fluorine, R2 is 1-4C-alkyl and R3 is hydrogen or 1-4C-alkyl, or in which R2 and R3, together and including the two carbon atoms to which they are bonded, are a spiro-linked 5-, 6- or 7-membered hydrocarbon ring, if desired interrupted by an oxygen atom or an imino (-NH-) group, R4 is hydrogen, hydroxyl, nitro, cyano, carboxyl, 1-4C-alkoxy or 1-4C-alkoxycarbonyl, A is B, -CH(R5)- or > C = N-R6, where B is oxygen (-O-), imino (-NH-), sulfinyl (-S(O)-), sulfonyl, (-S(O)2-) or carbonylimino (-C(O)NH-) and R5 is carboxyl, 1-4C-alkoxycarbonyl, aminocarbonyl, mono- or di-1-4C-alkylaminocarbonyl, hydroxylaminocarbonyl (-C(O)NHOH), 1-4C-alkoxyaminocarbonyl or a radical of formula (a) where R51 is hydrogen, 1-4C-alkyl or aryl and R52 is hydrogen, 1-4C-alkyl or aryl, where aryl is a phenyl, pyridyl, benzyl or phenethyl radical which can be unsubstituted or mono- or disubstituted by hydroxyl, 1-4C-alkoxy, halogen, amino, cyano or nitro, R6 is hydroxy or 1-4C-alkylcarbonyloxy, and the salts of these compounds are efficacious PDE inhibitors.
摘要翻译： R 1为1-6C-烷氧基，3-7C-环烷氧基，3-7C-环烷基甲氧基，苄氧基或完全或主要被氟取代的1-4C-烷氧基的式（Ⅰ）化合物，R2为1-4C- 烷基和R 3是氢或1-4C-烷基，或其中R 2和R 3一起并包括它们所键合的两个碳原子是螺连接的5-，6-或7-元烃环，如果需要被氧原子或亚氨基（-NH-）基团中断，R4是氢，羟基，硝基，氰基，羧基，1-4C-烷氧基或1-4C-烷氧基羰基，A是B，-CH（R5） - 或 - > C = N-R6，其中B是氧（-O-），亚氨基（-NH-），亚磺酰基（-S（O） - ），磺酰基，（-S（O）2-）或羰基亚氨基（ - C（O）NH-），R 5是羧基，1-4C-烷氧基羰基，氨基羰基，单或二1-4C-烷基氨基羰基，羟基氨基羰基（-C（O）NHOH），1-4C-烷氧基氨基羰基或式（a）其中R51是氢，1-4C-烷基或芳基，R52是氢，1-4C-烷基或芳基，其中芳基是苯基，吡啶基，苄基或苯乙基其可以是未取代的或被羟基，1-4C-烷氧基，卤素，氨基，氰基或硝基单或二取代，R6是羟基或1-4C-烷基羰氧基，并且这些化合物的盐是有效的PDE抑制剂。

8. 发明申请

WO1997019946A1 PYRIDOPYRIMIDINES 审中-公开
标题翻译：吡啶并
公开(公告)号：WO1997019946A1
公开(公告)日：1997-06-05
申请号：PCT/EP1996005046
申请日：1996-11-16
申请人： BYK GULDEN LOMBERG CHEMISCHE FABRIK GMBH , ULRICH, Wolf-Rüdiger
发明人： BYK GULDEN LOMBERG CHEMISCHE FABRIK GMBH , BÄR, Thomas , ZIMMERMANN, Peter , BOER, Rainer , GEKELER, Volker , ISE, Wolfgang , BOSS, Hildegard
IPC分类号： C07D471/04
CPC分类号： C07D471/04
摘要： The invention concerns compounds of formula (I) in which the substituents and symbols have the meanings given in the description. These compounds are advantageous resistance modulators.
摘要翻译：式（I）的化合物其中取代基和符号具有在说明书中给出的含义，是有趣性调节剂。

9. 发明申请

WO2002060895A1 DIAZOCINE DERIVATIVES AND THEIR USE AS TRYPTASE INHIBITORS 审中-公开
标题翻译： DIAZOCINE DORIVATIVES及其作为TRYPTASE抑制剂的用途
公开(公告)号：WO2002060895A1
公开(公告)日：2002-08-08
申请号：PCT/EP2002/000831
申请日：2002-01-26
申请人： BYK GULDEN LOMBERG CHEMISCHE FABRIK GMBH , ULRICH, Wolf-Rüdiger
发明人： ULRICH, Wolf-Rüdiger , BÄR, Thomas , MARTIN, Thomas , STADLWIESER, Josef , WOLLIN, Stefan-Lutz , ZECH, Karl , SOMMERHOFF, Christian, P.
IPC分类号： C07D403/14
CPC分类号： C07D403/14
摘要： Compounds of the formula I, in which B1, B2, R1, R2, R6, R7, K1 and K2 are as defined in the description are novel effective tryp-tase inhibitors.
摘要翻译：其中B1，B2，R1，R2，R6，R7，K1和K2如说明书中所定义的式I化合物是新的有效的tryp-tase抑制剂。

10. 发明申请

WO1996036625A1 PHENYL DIHYDROBENZOFURANES 审中-公开
标题翻译： PHENYLDIHYDROBENZOFURANE
公开(公告)号：WO1996036625A1
公开(公告)日：1996-11-21
申请号：PCT/EP1996002031
申请日：1996-05-11
申请人： BYK GULDEN LOMBERG CHEMISCHE FABRIK GMBH , ULRICH, Wolf-Rüdiger
发明人： BYK GULDEN LOMBERG CHEMISCHE FABRIK GMBH , AMSCHLER, Hermann , BÄR, Thomas , GUTTERER, Beate , FLOCKERZI, Dieter , MARTIN, Thomas , THIBAUT, Ulrich , HATZELMANN, Armin , BEUME, Rolf , BOSS, Hildegard , HÄFNER, Dietrich , KLEY, Hans-Peter
IPC分类号： C07D307/94
CPC分类号： C07D307/94 , C07D307/86
摘要： Compounds having the formula (I), in which R1, R2, R3, R4 and R5 have the meanings given in the description, are new and powerful PDE inhibitors.
摘要翻译：式（I）化合物，其中R1，R2，R3，R4和R5具有说明书中给出的含义，是新的有效的PDE抑制剂。

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