摘要:
There is provided an indole derivative represented by the above formula (I) or a pharmaceutically acceptable salt thereof which is useful for the treatment of malignant tumor or a brain neurodegenerative disease: (wherein C ring represents a benzene ring or a cyclohexene ring; X and Y are the same or different and each represent —CH2—, —CH(OH)—, —CH(ORx)—, —CH(SRY)— or carbonyl; R1 and R2 are the same or different and each represent a hydrogen atom, substituted or unsubstituted lower alkyl, substituted or unsubstituted lower alkenyl or substituted or unsubstituted lower alkanoyl or R1 and R2 form a benzene ring together two carbon atoms each being adjacent thereto; and R3, R4 and R5 are the same or different and each represent a hydrogen atom, substituted or unsubstituted lower alkyl, etc.)
摘要:
This invention relates to substituted piperidine derivatives having at least one six-membered ring substituent. The piperidine derivatives exhibit antitumor activity and are useful as pharmaceuticals such as an antitumor agent.
摘要:
Novel sulfatase inhibitor compounds useful in the treatment of estrogen dependent illnesses are disclosed. These compounds generally comprise a steroid nucleus substituted at the C17 position. Methods for synthesizing these compounds and using them in the therapeutic and/or prophylactic treatment of a patient are also disclosed.
摘要:
UCF116 derivatives represented by formula (I): wherein Q represents and R represents hydrogen, C(═O)R1a (wherein R1a represents methyl, ethyl, propyl, isopropyl, 2,2-dimethylpropyl, pentyl, alkyl having 6 to 10 carbon atoms, 1-propenyl, isopropenyl, 2-methyl-1-propenyl, substituted or unsubstituted alicyclic alkyl having 3 to 5 carbon atoms, substituted or unsubstituted aryl, substituted or unsubstituted aralkyl, a substituted or unsubstituted heterocyclic group, substituted or unsubstituted aralkyloxy, or substituted lower alkyl), C(═X)NHR1b (wherein X represents an oxygen or sulfur atom, and R1b represents substituted or unsubstituted lower alkyl, substituted or unsubstituted alicyclic alkyl, substituted or unsubstituted lower alkoxycarbonyl, substituted or unsubstituted aryl, substituted or unsubstituted aralkyl, or a substituted or unsubstituted heterocyclic group), or SO2R1c (wherein R1c represents substituted or unsubstituted lower alkyl, substituted or unsubstituted aryl, substituted or unsubstituted aralkyl, a substituted or unsubstituted heterocyclic group, or substituted or unsubstituted lower alkenyl), with the proviso that, when Q is R is not benzoyl; salts thereof; isomers thereof; hydrates thereof; or solvates thereof.
摘要:
Radicicol derivatives represented by the following formula (I) having tyrosine kinase inhibition activity or pharmacologically acceptable salts thereof: wherein R1 and R2 are the same or different, and each represents hydrogen, alkanoyl, alkenoyl, tert-butyldiphenylsilyl or tert-butyldimethylsilyl; R3 represents Y—R5 {wherein Y represents substituted or unsubstituted alkylene; and R5 represents CONR6R7 (wherein R6 represents hydrogen, hydroxyl, substituted or unsubstituted lower alkyl, substituted or unsubstituted higher alkyl; R7 represents hydroxyl, substituted lower alkyl), CO2R12 (wherein R12 represents substituted lower alkyl, substituted or unsubstituted higher alkyl, X represents halogen.
摘要翻译:由下式(I)表示的具有酪氨酸激酶抑制活性的衍生物衍生物或其药理学上可接受的盐:其中R1和R2相同或不同,并且各自表示氢,链烷酰基,烯酰基,叔丁基二苯基甲硅烷基或叔丁基二甲基甲硅烷基; R3表示Y-R5 {其中Y表示取代或未取代的亚烷基; 并且R 5表示CONR 6 R 7(其中R 6表示氢,羟基,取代或未取代的低级烷基,取代或未取代的高级烷基; R 7表示羟基,取代的低级烷基),CO 2 R 12(其中R 12表示取代的低级烷基,取代或未取代的高级烷基,X表示 卤素。
摘要:
The present invention relates to chrolactomycin compound represented by the following formula (I): ##STR1## or pharmaceutically acceptable salts thereof having antibacterial and antitumor activities.
摘要:
Described herein is a pyrrolocarbazole derivative and a pharmaceutically acceptable salt thereof having the following formula (I): ##STR1## wherein R.sup.1 is lower alkyl or aralkyl; R.sup.2 is hydrogen, substituted or unsubstituted lower alkyl, lower alkenyl, or substituted or unsubstituted aralkyl; R.sup.3, R.sup.4, R.sup.5, R.sup.6 and R.sup.7 may be the same or different, and are hydrogen, halogen, nitro, substituted or unsubstituted lower alkanoyl, NR.sup.9 R.sup.10, or OR.sup.11 ; R.sup.8 is hydrogen or is combined with R.sup.3 to form --CONR.sup.12 --; and when R.sup.1 is benzyl; R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6, R.sup.7 and R.sup.8 are not simultaneously hydrogen. A compound of the present invention stimulates platelet production and is useful for treatment of thrombocytopenia.
摘要:
The present invention relates to UCK14 compounds having antitumor activity which are represented by the formula: ##STR1## wherein R.sup.1 is hydrogen or --COOC(CH.sub.3).sub.3 ; and R.sup.2 and R.sup.3 are taken together to form --CH.sub.2 --, or each R.sup.2 and R.sup.3 independently are hydrogen,and pharmaceutically acceptable salts thereof.
摘要:
The present invention relates to novel derivatives of K-252, (8R*, 9S*, 11S*)-(-)-9-hydroxy-9-methoxycarbonyl-8-methyl-2,3,9,10-tetrahydro-8,11-epoxy-1H,8H, 11H-2,7b,11a-triazadibenzo[a,g]cycloocta-[c,d,e,]trinden-1-one, and the compounds are represented by formula (I): ##STR1## wherein W.sub.1, W.sub.2, R.sup.1, R.sup.2, R.sup.3, R.sup.4, X and Y represent various substituents. The compounds are physiologically active substances that inhibit protein kinase C and exhibit an antitumor activity, and are useful as medicines.
摘要:
A K-252 compound represented by the formula: ##STR1## wherein R.sup.1 and R.sup.2 are independently H or OH; X represents COOH, COOR or CH.sub.2 OH; Y represents H, R or COR; and Z represents OH, OR or SR, wherein R represents lower alkyl has C-kinase inhibitory activity and is expected to be useful as an active ingredient of anti-tumor agents, etc.