摘要:
The present invention is directed to compounds of formula I: wherein A is n is 0, 1, or 2; m is 0 or 1; R1 is H or C1-6alkyl and R2 is H, C1-6 alkyl, substituted or unsubstituted aryl, or substituted or unsubstituted heteroaryl; and X is O or N; as well as tautomers and pharmaceutically acceptable salt forms thereof. Uses of these compounds are also described.
摘要翻译:本发明涉及式I化合物:其中A是n是0,1或2; m为0或1; R 1是H或C 1-6烷基,R 2是H,C 1-6烷基,取代或未取代的芳基或取代或未取代的杂芳基; X为O或N; 以及互变异构体及其药学上可接受的盐形式。 还描述了这些化合物的用途。
摘要:
The present invention is directed to carboxylic acid-containing pharmaceutical compounds where the carboxylic acid moieties have been substituted with cycloalkyl-dione derivatives, as well as tautomers and pharmaceutically acceptable salt forms thereof. These bioisosteric replacements improve the compound's ability to effectively cross the blood brain barrier and result in improved pharmacokinetic, toxicological, and/or safety profiles.
摘要:
The present invention is directed to methods of inhibiting a tauopathy in a patient by administration of a compound of formula I: Novel aminothienopyridazine compounds are also described.
摘要:
The present invention relates to TP receptor antagonists, which have the ability to bind to TP receptor and optionally cross the blood brain barrier. The invention also provides compositions and methods for treating a disorder wherein activation of TP receptor is detrimental.
摘要:
Compounds useful for lowering beta amyloid levels are provided. The compounds have the structure of formula Ia: wherein, R1 is lower alkyl, substituted lower alkyl, phenyl, substituted phenyl, benzyl, substituted benzyl, benzyloxy, substituted benzyloxy, or SO2R5; R5 is phenyl, substituted phenyl, heterocycle, substituted heterocycle, alkyl, or substituted alkyl; R2 is lower alkyl, substituted lower alkyl, CF3, alkenyl, substituted alkenyl, alkynyl, substituted alkynyl, phenyl, substituted phenyl, or cycloalkyl; R3 is hydrogen, lower alkyl, or substituted lower alkyl; R4 is phenyl, substituted phenyl, heterocycle, substituted heterocycle, thiophene, or substituted thiophene; R6 is hydrogen, lower alkyl, substituted lower alkyl, CF3, alkenyl, substituted alkenyl, alkynyl, substituted alkynyl, phenyl, substituted phenyl, cycloalkyl, or substituted cycloalkyl; W, X and Y are independently CR7 or N; and R7 is hydrogen, halogen, lower alkyl, or substituted lower alkyl.
摘要翻译:提供了可用于降低β淀粉样蛋白水平的化合物。 化合物具有式Ia的结构:其中R 1是低级烷基,取代的低级烷基,苯基,取代的苯基,苄基,取代的苄基,苄氧基,取代的苄氧基或SO 2, / 5> 5 R 5是苯基,取代的苯基,杂环,取代的杂环,烷基或取代的烷基; R 2是低级烷基,取代的低级烷基,CF 3,烯基,取代的烯基,炔基,取代的炔基,苯基,取代的苯基或环烷基; R 3是氢,低级烷基或取代的低级烷基; R 4是苯基,取代的苯基,杂环,取代的杂环,噻吩或取代的噻吩; R 6是氢,低级烷基,取代的低级烷基,CF 3,烯基,取代的烯基,炔基,取代的炔基,苯基,取代的苯基,环烷基或取代的环烷基; W,X和Y独立地为CR 7或N; R 7是氢,卤素,低级烷基或取代的低级烷基。
摘要:
Compounds useful for lowering beta amyloid levels are provided. The compounds have the structure of formula Ia: wherein, R1 is lower alkyl, substituted lower alkyl, phenyl, substituted phenyl, benzyl, substituted benzyl, benzyloxy, substituted benzyloxy, or SO2R5; R5 is phenyl, substituted phenyl, heterocycle, substituted heterocycle, alkyl, or substituted alkyl; R2 is lower alkyl, substituted lower alkyl, CF3, alkenyl, substituted alkenyl, alkynyl, substituted alkynyl, phenyl, substituted phenyl, or cycloalkyl; R3 is hydrogen, lower alkyl, or substituted lower alkyl; R4 is phenyl, substituted phenyl, heterocycle, substituted heterocycle, thiophene, or substituted thiophene; R6 is hydrogen, lower alkyl, substituted lower alkyl, CF3, alkenyl, substituted alkenyl, alkynyl, substituted alkynyl, phenyl, substituted phenyl, cycloalkyl, or substituted cycloalkyl; W, X and Y are independently CR7 or N; and R7 is hydrogen, halogen, lower alkyl, or substituted lower alkyl.
摘要翻译:提供了可用于降低β淀粉样蛋白水平的化合物。 所述化合物具有式Ia的结构:其中,R 1为低级烷基,取代的低级烷基,苯基,取代的苯基,苄基,取代的苄基,苄氧基,取代的苄氧基或SO 2 R 5; R5是苯基,取代的苯基,杂环,取代的杂环,烷基或取代的烷基; R2是低级烷基,取代的低级烷基,CF3,烯基,取代的烯基,炔基,取代的炔基,苯基,取代的苯基或环烷基; R3是氢,低级烷基或取代的低级烷基; R4是苯基,取代的苯基,杂环,取代的杂环,噻吩或取代的噻吩; R 6是氢,低级烷基,取代的低级烷基,CF 3,烯基,取代的烯基,炔基,取代的炔基,苯基,取代的苯基,环烷基或取代的环烷基; W,X和Y独立地为CR 7或N; 并且R 7是氢,卤素,低级烷基或取代的低级烷基。
摘要:
Compounds useful for lowering beta amyloid levels are provided. The compounds have the structure of formula Ia: wherein, R1 is lower alkyl, substituted lower alkyl, phenyl, substituted phenyl, benzyl, substituted benzyl, benzyloxy, substituted benzyloxy, or SO2R5; R5 is phenyl, substituted phenyl, heterocycle, substituted heterocycle, alkyl, or substituted alkyl; R2 is lower alkyl, substituted lower alkyl, CF3, alkenyl, substituted alkenyl, alkynyl, substituted alkynyl, phenyl, substituted phenyl, or cycloalkyl; R3 is hydrogen, lower alkyl, or substituted lower alkyl; R4 is phenyl, substituted phenyl, heterocycle, substituted heterocycle, thiophene, or substituted thiophene; R6 is hydrogen, lower alkyl, substituted lower alkyl, CF3, alkenyl, substituted alkenyl, alkynyl, substituted alkynyl, phenyl, substituted phenyl, cycloalkyl, or substituted cycloalkyl; W, X and Y are independently CR7 or N; and R7 is hydrogen, halogen, lower alkyl, or substituted lower alkyl.
摘要翻译:提供了可用于降低β淀粉样蛋白水平的化合物。 所述化合物具有式Ia的结构:其中,R 1为低级烷基,取代的低级烷基,苯基,取代的苯基,苄基,取代的苄基,苄氧基,取代的苄氧基或SO 2 R 5; R5是苯基,取代的苯基,杂环,取代的杂环,烷基或取代的烷基; R2是低级烷基,取代的低级烷基,CF3,烯基,取代的烯基,炔基,取代的炔基,苯基,取代的苯基或环烷基; R3是氢,低级烷基或取代的低级烷基; R4是苯基,取代的苯基,杂环,取代的杂环,噻吩或取代的噻吩; R 6是氢,低级烷基,取代的低级烷基,CF 3,烯基,取代的烯基,炔基,取代的炔基,苯基,取代的苯基,环烷基或取代的环烷基; W,X和Y独立地为CR 7或N; 并且R 7是氢,卤素,低级烷基或取代的低级烷基。
摘要:
Compounds useful for lowering beta amyloid levels are provided. The compounds have the structure of formula Ia: wherein, R1 is lower alkyl, substituted lower alkyl, phenyl, substituted phenyl, benzyl, substituted benzyl, benzyloxy, substituted benzyloxy, or SO2R5; R5 is phenyl, substituted phenyl, heterocycle, substituted heterocycle, alkyl, or substituted alkyl; R2 is lower alkyl, substituted lower alkyl, CF3, alkenyl, substituted alkenyl, alkynyl, substituted alkynyl, phenyl, substituted phenyl, or cycloalkyl; R3 is hydrogen, lower alkyl, or substituted lower alkyl; R4 is phenyl, substituted phenyl, heterocycle, substituted heterocycle, thiophene, or substituted thiophene; R6 is hydrogen, lower alkyl, substituted lower alkyl, CF3, alkenyl, substituted alkenyl, alkynyl, substituted alkynyl, phenyl, substituted phenyl, cycloalkyl, or substituted cycloalkyl; W, X and Y are independently CR7 or N; and R7 is hydrogen, halogen, lower alkyl, or substituted lower alkyl.
摘要翻译:提供了可用于降低β淀粉样蛋白水平的化合物。 化合物具有式Ia的结构:其中R 1是低级烷基,取代的低级烷基,苯基,取代的苯基,苄基,取代的苄基,苄氧基,取代的苄氧基或SO 2, / 5> 5 R 5是苯基,取代的苯基,杂环,取代的杂环,烷基或取代的烷基; R 2是低级烷基,取代的低级烷基,CF 3,烯基,取代的烯基,炔基,取代的炔基,苯基,取代的苯基或环烷基; R 3是氢,低级烷基或取代的低级烷基; R 4是苯基,取代的苯基,杂环,取代的杂环,噻吩或取代的噻吩; R 6是氢,低级烷基,取代的低级烷基,CF 3,烯基,取代的烯基,炔基,取代的炔基,苯基,取代的苯基,环烷基或取代的环烷基; W,X和Y独立地为CR 7或N; R 7是氢,卤素,低级烷基或取代的低级烷基。
摘要:
Isomeric derivatives of 2',3'-dideoxyadenosine and 2',3'-dideoxyguanosine wherein the adenine or guanine base is attached to the 1' position of the iso-dideoxysugar residue by the 9-N position, the novel intermediates used in the synthesis of these compounds, and a method for treating a subject infected with a retrovirus by administering the compounds of the invention.