摘要:
The present invention provides a compound of formula (I): wherein X is N or CH, Y is NH, O or S, methods for manufacturing these compounds, and their uses as Factor B inhibitors for the treatment of conditions and diseases associated with complement alternative pathway activation such as age-related macular degeneration, diabetic retinopathy and related ophthalmic diseases. The present invention further provides pharmaceutical compositions and combinations of pharmacologically active agents.
摘要:
Provided are a camptothecin compound containing 7-membered lactone ring, as shown in general formula I, and pharmaceutically acceptable salt thereof, as well as the preparation method and use thereof. In general formula I, R1 is H, a C1˜C3 alkyl, acetyl or propionyl; R2 is H, a C1˜C6 alkyl, a C3˜C6 cycloalkyl, piperidyl; or a C1˜C6 alkyl substituted by an amino; R3 is H, a C1˜C3 alkyl, or a C1˜C6 alkyl substituted by an amino; R4 is H, a hydroxyl, or a C1˜C6 alkoxy; R5 is H, or a C1˜C6 alkoxyl; or R4 and R5 are linked to each other to form —OCH2O— or —OCH2CH2O—. The compound has good anti-tumor activity, and can be clinically used via oral administration, intravenous injection, and intramuscular injection, among others.
摘要:
New camptothecin derivatives with the following structure of the formula (I), their use and the pharmaceutical compositions containing the same. The compounds of the present invention have good anti-tumor activities and good solubility in water, and can be used in development of medicines.
摘要:
Rapalogs of formula I, pharmaceutically acceptable salts, pharmaceutical compositions, and preparation methods and uses thereof. The rapalogs have the structure of formula I and can be used as an anti-tumor medicament. Comparing with rapamycin, the rapalogs of the present invention exhibit enhanced water solubility, and improved pharmacological and pharmacokinetic properties by introducing a hydrophilic and polar group such as a hydroxyl.
摘要:
Disclosed are a series of α-amino-N-substituted amide compounds having a structure of the following formula, the pharmaceutically acceptable salts thereof, and the pharmaceutical composition comprising the same. The α-amino-N-substituted amide compounds or the pharmaceutically acceptable salts thereof according to the present invention have anti-tumor and/or anti-cancer activities in vivo and in vitro, can effectively depress the growth of various tumor cells and/or cancer cells, and thus can be used in preparing drugs for treating tumors and/or cancers.
摘要:
Triptolide derivatives of Formula (I), their pharmaceutically acceptable salts and optical isomers, Formula (I): wherein, C5 and C6 are connect with each other by a C-C single bond or double bond; when C5 and C6 are connected with C-C single bond, X and Y represent independently hydrogen, oxygen, hydroxyl, halogen, lower alkyl-oxy, lower alkyl-amino, mercapto, lower alkyl-thio, the group of formula —OCOR, —OSO2OR or —OPO(OH)2, each of which is attached to C5 and C6, R represents —(CH2)nCO2Na, —(CO2)nCO2K, or —(CH2)nCH3, wherein n=1-6; Z represents hydrogen, oxygen, hydroxyl, halogen, lower alkyl-oxy, lower alkyl-amino, mercapto, lower alkyl-thio, the group of formula -OCOR, -OSO2OR or —OPO(OH)2, each of which is linked at C14-position, R represents —(CH2)nCO2Na, —(CO2)nCO2K, or —(CH2)nCH2, wherein n=1-6; wherein, the“______” linked with X, Y, and Z represents the stereochemistry orientations “” or “” , but X and Y cannot both be hydrogen atom at the same time, methods for preparing the triptolides and their use as antiphiogistic agent, immunosuppressive agent or therapeutic agent for other related diseases.
摘要:
An integrated in situ oxide etch process particularly useful for a counterbore dual-damascene structure over copper having in one inter-layer dielectric level a lower nitride stop layer, a lower oxide dielectric, a lower nitride stop layer, an upper oxide dielectric layer, and an anti-reflective coating (ARC). The process is divided into a counterbore etch and a trench etch with photolithography for each, and each step is preferably performed in a high-density plasma reactor having an inductively coupled plasma source primarily generating the plasma and a capacitively coupled pedestal supporting the wafer and producing the bias power. The counterbore etch preferably includes at least four substeps of opening the ARC, etching through the upper oxide and nitride layers, selectively etching the lower oxide layer but stopping on the lower nitride layer, and a post-etch treatment for removing residue. The trench etch preferably includes the five substeps of opening the ARC, etching through the upper oxide layer but stopping on the upper nitride layers, a first post-etch treatment for removing residue, a nitride removal of the exposed portions of the upper and lower nitride layers, and a second post-etch treatment for remaining further residues. The oxide etches selective to nitride are accomplished using a fluorocarbon chemistry with high bias and a high temperature for a silicon-based scavenger for fluorine placed next to the plasma. The nitride etches and removal are accomplished by adding an oxygen-containing gas to a fluorocarbon. The final nitride removal is accomplished with very low bias power to increase selectivity to nitride and reduce sputtering of the underlying copper. The post-etch treatments are oxygen plasmas with zero bias power.
摘要:
A plasma etching process for etching a carbon-based low-k dielectric layer in a multi-layer inter-level dielectric. The low-k dielectric may be divinyl siloxane-benzocyclobutene (BCB), which contains about 4% silicon, the remainder being carbon, hydrogen, and a little oxygen. The BCB etch uses an etching gas of oxygen, a fluorocarbon, and nitrogen and no argon. An N2/O2 ratio of between 1:1 and 3:1 produces vertical walls in the BCB. In a dual-damascene structure, the inter-level dielectric includes two BCB layers, each underlaid by a respective stop layer. Photolithography with an organic photoresist needs a hard mask of silicon oxide or nitride over the upper BCB layer. After the BCB etch has cleared all the photoresist, the bias power applied to the cathode supporting the wafer needs to be set to a low value while the separately controlled plasma source power is set reasonably high, thereby reducing faceting of the exposed hard mask. Chamber pressures of no more than 5 milliTorr increase the selectivity of BCB over photoresist. Substrate temperatures of less than 0° C. increase the BCB etch rate. A low fluorocarbon flow increases the etch rate, but a minimum amount of fluorocarbon is required for the silicon component of BCB. In a counterbore dual-damascene etch, the lower stop layer is composed of nitride, and the preferred fluorocarbon is difluoroethane (CH2F2). A silicon-free carbon-based low-k dielectric can be etched under similar chamber conditions with a etching gas of oxygen and nitrogen in about equal amounts but including no fluorocarbon nor argon.