摘要:
A fluorescence based assay for compounds that modulate T-type calcium ion channels and that can be adapted to high throughput screening formats. Modulators of T-type channels are useful to correct functional abnormalities. These abnormalities are associated with epilepsy, pain, schizophrenia, depression, anxiety, cardiac arrhythmia, hypertension, certain types of cancer, diabetes, infertility, sexual dysfunction and other undesirable conditions.
摘要:
Methods and compounds effective in ameliorating conditions characterized by unwanted calcium channel activity, particularly unwanted T-type calcium channel activity are disclosed. Specifically, a series of compounds containing thienopyrimidine or oxoquinazoline derivatives are disclosed of the general formula (1) or formula (2) where X is a linker and Y is an aromatic moiety or N(R5)(R6).
摘要:
Methods and compounds effective in ameliorating conditions characterized by unwanted calcium channel activity, particularly unwanted T-type calcium channel activity are disclosed. Specifically, a series of compounds containing thienopyrimidine or oxoquinazoline derivatives are disclosed of the general formula (1) or formula (2) where X is a linker and Y is an aromatic moiety or N(R5)(R6).
摘要:
Aromatic derivatives of aliphatic diamines are effective in ameliorating conditions characterized by unwanted calcium ion channel activity, especially T-type and N-type channels. These conditions include, for example, stroke and pain. The aromatic derivatives of aliphatic diamines have the formula (I) : (Ar 1 -X 1 ) n NR 1 -X 3 NR 2 -CR 3 (Ar 2 ) 2 wherein Ar 1 is independently a cyclic moiety, X 1 is a linker comprising a chain of 1-5 members; n is 1 or 2; R 1 is absent when n is 2 and when n is 1, R 1 is H, alkyl (1-8C), alkenyl (2-8C) or alkynyl (2-8C); X 3 is alkylene, alkenylene or alkynylene (2-8C); R 2 is H, alkyl (1-8C), alkenyl (2-8C) or alkynyl (2-8C); X 2 is a linker comprising a chain of 2-9 members; R 3 is H, OH or alkyl (1-4C); each Ar 2 independently comprises a 6-membered aromatic ring optionally containing 1-3 nitrogen atoms.
摘要翻译:脂肪族二胺的芳族衍生物可有效改善特征在于不需要的钙离子通道活性的条件,特别是T型和N型通道。 这些病症包括例如中风和疼痛。 脂肪族二胺的芳族衍生物具有式(I):(I 1)其中N 1,N 2,N 2, > - - - - - - - - - - - - - - - - - - - - - (3)其中 Ar 1独立地是环状部分,X 1是包含1-5个成员的链的连接体; n为1或2; 当n为2时,当n为1时,R 1为H,烷基(1-8C),烯基(2-8C)或炔基(2) -8℃); X 3是亚烷基,亚烯基或亚炔基(2-8C); R 2是H,烷基(1-8C),烯基(2-8C)或炔基(2-8C); X 2是包含2-9个成员的链的连接体; R 3是H,OH或烷基(1-4C); 每个Ar 2独立地包含任选含有1-3个氮原子的6元芳族环。
摘要:
New piperazine substituted compounds of formula (1) have been found to be useful in treatinf conditions associated with calcium channel function. These piperazine derivatives are useful in treating conditions such as stroke, pain, anxiety disorders, depression, addiction, gastrointestinal disorders, genitourinary disorders, cardiovascular disease, epilepsy, diabetes and cancer.
摘要:
New piperazine substituted compounds of formula (1) have been found to be useful in treatinf conditions associated with calcium channel function. These piperazine derivatives are useful in treating conditions such as stroke, pain, anxiety disorders, depression, addiction, gastrointestinal disorders, genitourinary disorders, cardiovascular disease, epilepsy, diabetes and cancer.
摘要:
A fluorescence based assay for compounds that modulate T-type calcium ion channels and that can be adapted to high throughput screening formats. Modulators of T-type channels are useful to correct functional abnormalities. These abnormalities are associated with epilepsy, pain, schizophrenia, depression, anxiety, cardiac arrhythmia, hypertension, certain types of cancer, diabetes, infertility, sexual dysfunction and other undesirable conditions.
摘要:
Methods and compounds effective in ameliorating conditions characterized by unwanted calcium channel activity, particularly unwanted T-type calcium channel activity are disclosed. Specifically, a series of compounds containing both a diamide and aromatic functionality are disclosed of the general formula (I) where X 1 and X 2 are linkers.