摘要:
This invention relates to photoswitchable inhibitors of histone deacetylases and methods of using the same. Provided herein are inhibitors of HDAC having photoswitchable modulators of protein function with short thermal relaxation kinetics. The compounds are diazo compounds including a substituted or unsubstituted aryl or heteroaryl ring, wherein at least one of the rings is substituted with one or more HDAC targeting elements.
摘要:
The present invention relates to compounds according to formula (1) and formula (2), which are suitable for use in electronic devices, in particular organic electroluminescent devices.
摘要:
Rylene derivatives are disclosed having the general formula (I), in which the variables have the meanings indicated in the claims. These compounds are used as pigments and I.R. dyes.
摘要:
The invention relates to a pharmaceutical composition comprising topotecan, for use in the treatment of ovarian cancer in a human afflicted therewith, wherein the composition is for parenteral administration to such human employing a course of therapy of from 1.0 to 2.5 mg (e.g. about 1.5 to about 2 mg) of topotecan/m 2 of body surface area per day for about five consecutive days. The invention also relates to a pharmaceutical composition comprising topotecan, for use in the treatment of ovarian cancer in a human afflicted therewith, wherein the composition is for oral administration to such human employing a course of therapy of from 1.5 to 5.0 mg of topotecan/m 2 of body surface area per day for about five consecutive days. The pharmaceutical composition can be an oral or parenteral pharmaceutical composition comprising topotecan and an inert, pharmaceutically acceptable carrier or diluent.
摘要翻译:本发明涉及一种药物组合物,其包含拓扑替康,其用于治疗患有其的人的卵巢癌,其中所述组合物用于肠胃外给药,其使用1.0至2.5mg的治疗疗程(例如约1.5至 约2mg)托泊替康/ m 2体表面积每天约5天。 本发明还涉及一种包含拓扑替康的药物组合物,其用于治疗患有其的人的卵巢癌,其中所述组合物用于口服施用1.5至5.0mg拓扑替康/ m的治疗疗程 每天2次体表面积连续5天。 药物组合物可以是包含托泊替康和惰性的药学上可接受的载体或稀释剂的口服或肠胃外药物组合物。
摘要:
Novel fused polycyclic heterocycle derivatives represented by general formula (I) or pharmacologically acceptable salts thereof which have an excellent antitumor effect, and a process for producing the same, wherein the ring A represents an optionally substituted monocyclic aromatic ring or a fused bicyclic ring wherein at least one of the rings is an aromatic ring; the ring B represents pyrrole, 4H-1,4-dioxane, 4H-1,4-thiazine or 4(1H)-pyridone; the ring C represents an optionally substituted monocyclic or fused bicyclic aromatic ring; and Y represents -e-f (wherein e represents lower alkylene; and f represents amidino, guanidino, or amino optionally substituted by hydroxy or lower alkyl optionally lower-alkylaminated); excluding a combination wherein the rings A and C are each an optionally substituted monocyclic aromatic ring.
---- représente une liaison simple ou double, R 0 représente un atome d'hydrogène ou un groupement hydroxy ou alkoxy, R 1 et R 2 , identiques ou différents, représentent chacun un atome d'hydrogène ou d'halogène ou un groupement alkyle, alkoxy, hydroxy, polyhalogénoalkyle, nitro, amino éventuellement substitué, dans laquelle m représente un entier tel que 1 ≤ m ≤ 4 ou forment ensemble avec les atomes de carbone qui les portent un groupement mono- ou bicyclique de 5 à 12 chaînons, aromatique ou non-aromatique, contenant éventuellement 1 ou 2 hétéroatomes choisis parmi O, S et N, R 3 représente un atome d'hydrogène ou un groupement aryle, hétéroaryle, cycloalkyle, alkyle éventuellement substitué, ou un groupement de formule COR 7 dans laquelle R 7 représente un groupement aryle, alkyle éventuellement substitué, amino éventuellement substitué ou OR 10 dans laquelle R 10 représente un groupement aryle, ou alkyle éventuellement substitué, X représente un atome d'oxygène, de soufre ou un groupement -CH 2 - ou -CH 2 -CH 2 -, Ar représente un groupement aryle, hétéroaryle ou arylalkyle, ses isomères optiques, ses hydrates, ses solvates ainsi que ses sels d'addition à un acide pharmaceutiquement acceptable. Médicaments.