METHOD FOR THE PREPARATION OF ESTERS OF ANHYDROECGONINE
    71.
    发明公开
    METHOD FOR THE PREPARATION OF ESTERS OF ANHYDROECGONINE 失效
    用于生产anhydroecgonine酯

    公开(公告)号:EP0815109A1

    公开(公告)日:1998-01-07

    申请号:EP96910010.0

    申请日:1996-03-22

    申请人: NEUROSEARCH A/S

    发明人: MOLDT, Peter

    IPC分类号: C07D451

    CPC分类号: C07D451/02

    摘要: A process for the preparation of esters of anhydroecgonine having formula (I), any of its enantiomers or any mixture thereof, or a salt thereof, wherein R is alkyl, or optionally substituted aryl, or arylalkyl; comprising the step of reacting a compound of formula (II), any of its enantiomers or any mixture thereof, or a salt thereof, wherein R1 is hydrogen, alkyl-CO-, or optionally substituted aryl-CO-, or arylalkyl-CO-; with an alcoholate RO-, M+ wherein R is as defined above and M+ is a counter ion, followed by isolation of the resulting compound either as the base or, if desired, in the form of a salt thereof.

    Isatine derivates, their preparation and their use as excitatory amino acid receptor antagonist
    76.
    发明公开
    Isatine derivates, their preparation and their use as excitatory amino acid receptor antagonist 失效
    靛红衍生物,它们的制备和它们作为通过刺激的受体的氨基酸拮抗剂的用途。

    公开(公告)号:EP0667340A1

    公开(公告)日:1995-08-16

    申请号:EP95610002.8

    申请日:1995-01-17

    申请人: NEUROSEARCH A/S

    发明人: Wätjen, Frank

    IPC分类号: C07D209/40 A61K31/40

    CPC分类号: C07D209/40

    摘要: The present patent application discloses compounds having the formula

    or a pharmaceutically acceptable salt thereof
    wherein
    one R²¹ and R²² is alkyl and the other is hydrogen or both of R²¹ and R²² are hydrogen;
    and
    R¹, R², R³, R⁴, R¹¹, R¹², R¹³, and R¹⁴ each independently are hydrogen, halogen, CF₃, CN, or NO₂; provided that at least one of R¹, R², R³, R⁴, R¹¹, R¹², R¹³, and R¹⁴ are different from hydrogen
    The compounds are useful as in vivo active glutamate antagonists.

    摘要翻译: 具有下式的或其药学上可接受的盐,本专利申请的分类盘化合物及其worin一个R <2> <1>和R <2> <2>是烷基并且另一个是氢或两个R <2> <的 1>和R <2> <2>是氢; 和R <1>,R <2> [R <3>,R <4> - [R <1> <1>,R <1> <2>,R <1> <3>,和R <1> <4>每个unabhängig是氢,卤素,CF 3,CN,或NO 2; 提供确实的R的至少一个<1>,R <2> [R <3>,R <4> - [R <1> <1>,R <1> <2>,R <1> <3> 和R <1> <4>不同于氢的化合物作为体内活性谷氨酸拮抗剂是有用的。

    Benzimidazole compounds, their preparation and use
    79.
    发明公开
    Benzimidazole compounds, their preparation and use 失效
    Benzimidazolderivate,Verfahren zu deren Herstellung und Anwendung。

    公开(公告)号:EP0604353A1

    公开(公告)日:1994-06-29

    申请号:EP93610064.3

    申请日:1993-12-20

    申请人: NEUROSEARCH A/S

    摘要: The present invention discloses compounds of the formula

    or a pharmaceutically-acceptable addition salt thereof
    wherein
    R' and R'' independently of each other are hydrogen or alkyl, or R' and R'' together form a 3 to 6 membered alkylene chain;
    one of R¹ and R² is aryl which may be substituted one or more times with halogen, CF₃, CN, OH, alkyl, cycloalkylalkyl, alkenyl, alkynyl, alkoxy, amino, nitro, sulphamoyl, tetrazolyl, CO₂H, CO₂-alkyl and the other of R¹ and R² is hydrogen, halogen, alkoxy, amino or alkyl; and
    R⁴, R⁵, R⁶ and R⁷ independently of each other are hydrogen, halogen, amino, nitro, CN, OH, CF₃, alkyl or alkoxy; and n is 0 or 1; provided that neither of R¹ and R² is phenyl or substituted phenyl when n is 0.
    The compounds are useful as pharmaceuticals, for example, in the treatment of ischemia, anoxia, migraine and psychosis.

    摘要翻译: 本发明公开了式CHEM的化合物或其药学上可接受的加成盐,其中R'和R“彼此独立地为氢或烷基,或R'和R”一起形成3至6元亚烷基 链; R 1和R 2之一是可以被卤素,CF 3,CN,OH,烷基,环烷基烷基,烯基,炔基,烷氧基,氨基,硝基,氨磺酰基,四唑基,CO 2 H, CO 2 - 烷基,R 1和R 2中的另一个是氢,卤素,烷氧基,氨基或烷基; R 4,R 5,R 6和R 7彼此独立地是氢,卤素,氨基,硝基,CN,OH,CF 3,烷基或烷氧基; n为0或1; 条件是当n为0时,R 1和R 2都不是苯基或取代的苯基。该化合物可用作药物,例如用于治疗缺血,缺氧,偏头痛和精神病。

    Imidazole derivatives as calcium channel blockers
    80.
    发明公开
    Imidazole derivatives as calcium channel blockers 失效
    咪唑啉酮钙钙阻断剂。

    公开(公告)号:EP0598962A1

    公开(公告)日:1994-06-01

    申请号:EP92610082.7

    申请日:1992-11-20

    申请人: NEUROSEARCH A/S

    摘要: The present patent application discloses compounds of the formula

    wherein
    R¹ is C₁₋₁₀-alkyl which may be branched; C₁₋₁₀-unsaturated alkyl; or CHR'''

    wherein R''' is H or

    R² is phenyl which may be substituted one or more times with halogen, CF₃, C₁₋₆-alkoxy, NO₂, CO₂-C₁₋₆-alkyl, methyl; benzyl which may be substituted one or more times with halogen, CF₃, C₁₋₆-alkoxy, NO₂, CO₂-C₁₋₆-alkyl, methyl; pyridyl; or cyclohexyl;
    R³ phenyl which may be substituted one or more times with halogen, CF₃, C₁₋₆-alkoxy, NO₂, CO₂-C₁₋₆-alkyl, methyl; naphthyl which may be substituted one or more times with halogen, CF₃, C₁₋₆-alkoxy, NO₂, CO₂-C₁₋₆-alkyl, methyl; pyridyl; C₁₋₆ unsaturated alkyl; furanyl;
    R⁴ is H, C₁₋₆-alkyl, or benzyl;
    or

    together form

    R⁵ is H, or C₁₋₆-alkyl;
    R' and R'' are each hydrogen or together form an extra benzo ring;
    and wherein the dotted line represents an optional extra bond between the two carbon atoms designated α and β, or a pharmaceutically-acceptable addition salt thereof.
    The compounds are useful as pharmaceuticals, for example in the treatment of Ca overload in brain cells.

    摘要翻译: 本专利申请公开了式CHEM的化合物,其中R 1是可以是支链的C 1-10烷基; C 1-10不饱和烷基; 或CHR“'CHEM,其中R”'是H或 R 2是可以被卤素,CF 3,C 1-6 - 烷氧基,NO 2,CO 2 -C 1 - 取代一次或多次的苯基, 6-烷基,甲基; 可以被卤素,CF 3,C 1-6 - 烷氧基,NO 2,CO 2 -C 1-6 - 烷基,甲基取代一次或多次的苄基; 吡啶基; 或环己基; 可以被卤素,CF 3,C 1-6 - 烷氧基,NO 2,CO 2 -C 1-6 - 烷基,甲基取代一次或多次的R 3苯基; 可以被卤素,CF 3,C 1-6 - 烷氧基,NO 2,CO 2 -C 1-6 - 烷基,甲基取代一次或多次的萘基; 吡啶基; C 1-6不饱和烷基; 呋喃基; R 4是H,C 1-6 - 烷基或苄基; 或一起形成 R 5是H或C 1-6 - 烷基; R'和R“各自为氢或一起形成额外的苯并环; 并且其中虚线表示指定为α和β的两个碳原子之间的任选的额外键或其药学上可接受的加成盐。 这些化合物可用作药物,例如用于治疗脑细胞中的Ca过载。