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.
摘要:
The present patent application discloses compounds having formula (I) or a pharmaceutically acceptable salt thereof wherein R1, X and R5 have the meanings set further in the specification. A is a ring of five to seven atoms fused with the benzo ring at the positions marked a and b. The compounds are useful in the treatment of cerebrovascular disorders for example.
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:
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。
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.