摘要:
There is provided compounds of formula I, (I) wherein R 1 , R 2 , R 3 R 4 , R 5 , R 6 , R 7a and R 7b have meanings given in the description, and pharmaceutically-acceptable esters, amides, solvates or salts thereof, which compounds are useful in the treatment of diseases in which inhibition of a protein or lipid kinase (e.g. CDK8 and/or Haspin kinase) is desired and/or required, and particularly in the treatment of cancer or a proliferative disease.
摘要:
본 발명은 세포의 티을 수준을 측정하기 위하여 실시간으로 이미징이 가능한 형광 센서에 관한 것이다. 본 발명은 본 발명의 FreSH-트레이서 (Fluorescent Real-time SH group-Tracer)가 생세포에서 티올의 양에 따라 형광 세기가 연속적이고, 비율계량적이며 가역적으로 증감한다는 것을 규명함으로써, 살아있는 세포에서 티올의 양을 실시간으로 정량 또는 정성적으로 검출하는데 현저한 민감성을 갖는바이오 센서로서 유용하게 이용될 수 있다.
摘要:
Compounds of formulas (A) and (B) are disclosed. The compounds of this invention are useful for ameliorating the side effects of therapeutic opiates.
摘要:
Novel compounds of the structural formula (I) are antagonists and/or inverse agonists of the Cannabinoid-1 (CB1) receptor and are useful in the treatment, prevention and suppression of diseases mediated by the CB1 receptor. The compounds of the present invention are useful as centrally acting drugs in the treatment of psychosis, memory deficits, cognitive disorders, Alzheimer's disease, migraine, neuropathy, neuro-inflammatory disorders including multiple sclerosis and Guillain-Barre syndrome and the inflammatory sequelae of viral encephalitis, cerebral vascular accidents, and head trauma, anxiety disorders, stress, epilepsy, Parkinson's disease, Huntington's disease movement disorders, and schizophrenia. The compounds are also useful for the treatment of substance abuse disorders, the treatment of obesity or eating disorders as well as the treatment of asthma, constipation, chronic intestinal pseudo-obstruction, cirrhosis of the liver, non-alcoholic fatty liver disease (NAFLD), non-alcoholic steatohepatitis (NASH), and the promotion of wakefulness.
摘要:
The present invention relates to compounds of the general structure: wherein Y is O, X is O, bond α is absent and bond β is present, or Y is H, X is CH, bond α is present, and bond β is absent; atom Z is a carbon and bonds χ , δ and γ are present, or is a nitrogen and bonds χ , δ and γ are absent; R 1 is -H, -OH, -O-R 7 , -N(H) -R 8 , -N (H) - (CH 2 ) n -NH 2 , -N(R 9 ) (R 10 ), or a piperazine cation; R 2 is either covalently bound to R 9 , or is -H, or is covalently bound to R 3 so as to form a substituted or unsubstituted pyrrole or R 2 is covalently bound to R 9 or R 8 or R 7 ; or R 1 and R 2 are covalently joined to form an aromatic ring; R 3 is either covalently bound to R 2 so as to form a pyrrole, or is, inter alia, -H, -OH, alkyl, or when Z is nitrogen R 3 is =O; R 4 is, inter alia, -H, -OH, or -R 11 NH 2 ; R 5 is, inter alia, -H, -OH, or -R 12 NH 2 , and R 6 is either is covalently bound to R 10 or is -H, or R 6 is covalently bound to R 10 or R 8 or R 7 . This invention also provides processes for making the compounds as well as methods for monitoring activity of monoamine transporters or treating monoamine transporter-associated diseases by employing the compounds.
摘要:
Compounds represented the general formula (I) exhibit affinities for various serotonin receptors (such as 5HT-1A, 2, 6, 7, and so on) and are therefore useful as remedies for central nervous system diseases or the like wherein R and R are each independently hydrogen, lower alkyl, or the like; R and R are each independently hydrogen, lower alkyl, or the like; or alternatively R and R may be united to form a single bond; n is 0 or 1; R is hydrogen; R is hydrogen, hydroxyl, or the like; R is hydrogen; R and R are each independently hydrogen, lower alkylthio, or the like; or alternatively R and R may be united to form a single bond; R is hydrogen, lower alkyl, or the like; R is hydrogen, lower alkyl, or the like; and R is hydrogen or lower alkyl
摘要翻译:表示通式(I)的化合物对各种5-羟色胺受体(例如5HT-1A,2,6,7等)表现出亲和力,因此可用作中枢神经系统疾病等的治疗方法,其中R 1, 和R 2各自独立地为氢,低级烷基等; R 3和R 4各自独立地为氢,低级烷基等; 或者R 1和R 3可以一起形成单键; n为0或1; R 5是氢; R 6是氢,羟基等; R 7是氢; R 8和R 9各自独立地为氢,低级烷硫基等; 或者R 7和R 9可以结合形成单键; R 10是氢,低级烷基等; R 11是氢,低级烷基等; 和R 12是氢或低级烷基
摘要:
The invention concerns new derivatives of tetrahydro-2,3,6,7,1H,5H,11H-(1)benzopyrano (6,7,8,ij)quinolizinone in accordance with formula (I), in which R represents a radical having formula (II), wherein m is equal to 0 or 1, and n is equal to 0 or is a whole number between 1 and 12, provided that n is equal to 0 when m is 0, or the radical having the formula: -NH-(CH2)n-NH2, in which n has the above meaning. Said derivatives can be used as markers for organic compounds, in order to detect them by chemiluminescence or fluorescence.
摘要:
In one aspect, the present disclosure provides compounds and derivatives of CJ-16,264 of the formula (I) wherein the variables are as defined herein. The application also provides compositions, methods of treatment, and methods of synthesis thereof. In some embodiments, these compounds are used in the treatment of bacterial infections or in the treatment of cancer.