公开(公告)号：EP1087973A1

公开(公告)日：2001-04-04

申请号：EP99927950.8

申请日：1999-06-11

申请人： Boehringer Ingelheim Pharma KG

发明人： BLECH, Stefan ,  CARTER, Adrian ,  GAIDA, Wolfram ,  HOFFMANN, Matthias ,  KUEFNER-MUEHL, Ulrike ,  MEADE, Christopher, John, Montague ,  POHL, Gerald

IPC分类号： C07D487/14 ,  A61K31/55

CPC分类号： C07D487/14

摘要： The present invention relates to new imidazotriazolopyrimidine derivatives of general formula (I), to methods for preparing the same and to their use as a drug. In this formula, the interrupted lines between nitrogen atoms represent a double link in one of two possible positions so that the radicals R?4 and R6 or R3 and R2¿ cannot be present simultaneously, wherein the radicals R1 to R6 are such as described in the description and the claims.

公开(公告)号：EP1140098A2

公开(公告)日：2001-10-10

申请号：EP99959324.7

申请日：1999-11-24

申请人： Boehringer Ingelheim Pharma KG

发明人： HOFFMANN, Matthias ,  JUNG, Birgit ,  KUEFNER-MUEHL, Ulrike ,  MEADE, Christopher, John, Montague

IPC分类号： A61K31/519

CPC分类号： A61K31/519 ,  A61K31/00

摘要： The invention relates to the utilisation of tricyclic nitrogen heterocycles of general formula (I) as medicaments with a PDE IV-inhibiting effect, the radicals R?1, R2 and R3¿ having the meanings given in the description and in the claims.

公开(公告)号：EP1087973B1

公开(公告)日：2003-01-08

申请号：EP99927950.8

申请日：1999-06-11

申请人： Boehringer Ingelheim Pharma KG

发明人： BLECH, Stefan ,  CARTER, Adrian ,  GAIDA, Wolfram ,  HOFFMANN, Matthias ,  KUEFNER-MUEHL, Ulrike ,  MEADE, Christopher, John, Montague ,  POHL, Gerald

IPC分类号： C07D487/14 ,  A61K31/55

CPC分类号： C07D487/14

摘要： The present invention relates to new imidazotriazolopyrimidine derivatives of general formula (I), to methods for preparing the same and to their use as a drug. In this formula, the interrupted lines between nitrogen atoms represent a double link in one of two possible positions so that the radicals R?4 and R6 or R3 and R2¿ cannot be present simultaneously, wherein the radicals R1 to R6 are such as described in the description and the claims.

摘要翻译： 本发明涉及通式（I）的新型咪唑并三唑并嘧啶衍生物，其制备方法及其作为药物的用途。 在该式中，氮原子之间的中断线代表两个可能位置之一中的双键，使得基团R 4和R 6或R 3和R 2不能同时存在，其中基团R 1至R 6如 说明书和权利要求书。

公开(公告)号：EP1084123A1

公开(公告)日：2001-03-21

申请号：EP99916914.7

申请日：1999-04-13

申请人： Boehringer Ingelheim Pharma KG

发明人： BLECH, Stefan ,  CARTER, Adrian ,  GAIDA, Wolfram ,  GATH, Ursula ,  HOFFMANN, Matthias ,  KUEFNER-MUEHL, Ulrike ,  LEHR, Erich ,  MIERAU, Joachim ,  POHL, Gerald ,  WEISER, Thomas

IPC分类号： C07D473/06 ,  A61K31/52

CPC分类号： C07D473/06 ,  C07D473/04

摘要： The invention relates to novel asymmetrically substituted xanthine derivatives of general formula (I), to methods for producing them and to their use as medicaments with an adenosine-antagonistic effect. The broken line between the nitrogen atoms of the general formula (I) indicates the existence of a double bond in one of two possible positions so that the radicals R?4 and R5¿ cannot be present at the same time. R1 cannot have the meaning of R2 at the same time. The radicals R?1, R2, R3, R4 and R5¿ are defined as follows: R1 is hydrogen, C¿1?-C6 alkyl, C3-C6 alkenyl or C3-C6 alkinyl; R?2¿ is a C¿1?-C6 alkyl, C3-C6 alkenyl or C3-C6 alkinyl radical which is substituted by -OR?6, -SO¿2R?6, -OCOR9, -COOR9, -NR7R8¿, -OCH¿2?CH2-NR?7R8, -CONR7R8¿, -OCH¿2?-CONR?7R8¿ or OCH¿2?CH2-CONR?7R8; R2¿ is a C¿1?-C6 alkyl, C3-C6 alkenyl or C3-C6 alkinyl radical which is substituted by a C-bonded 5 or 6-membered heterocyclic ring which may contain 1, 2, 3 or 4 heteroatoms selected from the following group: oxygen, nitrogen or sulphur; and may optionally be substituted by C1-C4 alkyl or benzyl; R?3 is C¿1-C6 alkyl which can be substituted by OH or optionally, norbornanyl, norbornenyl, adamantyl or noradamantyl substituted by methyl or OH and R4 or R5 is hydrogen, benzyl or benzyl substituted once, twice or three times by methoxy. R6 can mean hydrogen, C¿3?-C6 cycloalkyl or C1-C4 alkyl which may be substituted by -OR?9¿ or -OCOR9, R7 can mean hydrogen, -SO¿2R?6, C1-C4 alkyl, -COR9 or -COOR9; R8 can mean hydrogen, -SO¿2R?6, C1-C4 alkyl, -COR9 or -COOR?9 or R7 and R8¿ can form a 5 or 6-membered ring together with the nitrogen, whereby said ring may contain oxygen or nitrogen as a further heteroatom and may optionally be substituted by C¿1?-C4 alkyl or benzyl; and R?9¿ can mean hydrogen or C¿1?-C4 alkyl, optionally in the form of their racemates, their enantiomers, their diastereomers and their mixtures, and optionally in the form of their pharmacologically safe acid addition salts.