摘要:
The present invention relates to peptidomimetic compounds useful as protease inhibitors, particularly as serine protease inhibitors and more particularly as hepatitis C NS3 protease inhibitors; intermediates thereto; their preparation including novel steroselective processes to intermediates. The invention is also directed to pharmaceutical compositions and to methods for using the compounds for inhibiting HCV protease or treating a patient suffering from an HCV infection or physiological condition related to the infection. Also provided are pharmaceutical combinations comprising, in addition to one or more HCV serine protease inhibitors, one or more interferons exhibiting anti-HCV activity and/or one or more compounds having anti HCV activity and a pharmaceutically acceptable carrier, and methods for treating or preventing a HCV infection in a patient using the compositions. The present invention is also directed to a kit or pharmaceutical pack for treating or preventing HCV infection in a patient.
摘要:
The present invention relates to a hydrophilic surface structure of the non-hydrophilic substrate and the manufacturing method for using the same. The hydrophilic substrate surface structure is fabricated by forming an amphiphilic polymer layer, a cross-linked stacking layer, and a hydrophilic layer in sequence on the surface of a non-hydrophilic substrate. For example, the hydrophobic surface of poly(dimethylsiloxane) (PDMS) can be made from hydrophobic to hydrophilic and the hydrophilicity can be retained for a long period of time and resist protein adsorption. The hydrophilic thin films give long term stability to the PDMS surface by resisting hydrophobicity recovery, which is the major problem with PDMS. The disclosed method can further be used in the immobilization of protein and other molecules. This method can also be used for modifying other substrates which suffer problems of surface instability.
摘要:
A solder ball allocation on a chip, and a method of the same are provided. The chip has a substrate, first solder balls and second solder balls. The first solder balls are located on a periphery of the substrate and arranged outwardly. The second solder balls are located in a central part of the substrate and arranged with several first geometric patterns that construct a second geometric pattern. The first geometric patterns are also arranged to divide the chip into several power source blocks. The conflict between the second solder balls and the power source blocks are analyzed to remove the second solder balls with conflicts. The power line can go through the middle directly to avoid the power source bypass, or other reasons that cause the chip unable to work stable. The invention divides the chip into several power source blocks without increase the chip volume and cost.
摘要:
A method of recovering adipic acid and 6-hydroxycaproic acid from the waste solution of alkali metal salts of organic acids coming from the process of cyclohexane oxidation, which comprises:(i) basifying the reaction mixture coming from cyclohexane oxidation with an aqueous solution of an alkali-metal base so that the organic acids essentially comprising adipic acid and 6-hydroxycaproic acid therein, are saponified, extracting the formed alkali metal salts of organic acids from the mixture with water, then acidifying the aqueous extract comprising the alkali metal salts of organic acids to a pH value of 3 or lower with an aqueous solution of a protic inorganic acid, as a result, said aqueous extract is separated into an oily layer and an aqueous layer;(ii) extracting the organic acid from said oily layer obtained from the step (i) with an aqueous solution of a protic inorganic acid, to obtain an aqueous extract;(iii) extracting the organic acid from the aqueous layer obtained from the step (i) with an organic solvent selected from alcohols, ketones, esters or the mixtures thereof, to obtain an oily extract;(iv) extracting the organic acid from the aqueous extract obtained from the step (ii) with an organic solvent selected from alcohols, ketones, esters or mixtures thereof, to obtain an oily extract; and(v) combining and distilling the oily extracts obtained from the steps (iii) and (iv), to recover the organic acid essentially comprising adipic acid and 6-hydroxycaproic acid.
摘要:
The present invention relates to methods for substantially enhancing the stereoselective synthesis of .beta.-anomeric nucleoside analogs. In methods according to the present invention, the introduction of a phenylseleno group onto a blocked lactone sugar precursor may be selected so that the desirable phenylseleno substituent is introduced on the side of the blocked lactone away from the blocking group. This stereospecific introduction of the phenylseleno group in sugar precursor allows the synthesis of nucleoside analogs and in particular, 2',3',-dideoxy- and 2',3'-dideoxy-2',3'-didehydronucleoside analogs in very high yield. In certain preferred embodiments, the preferred phenylseleno blocked lactone is obtained in an amount representing approximately 90% or more of the total amount of the stereoisomers obtained. In even more preferred embodiments, the amount of the preferred stereoisomer is at least 95%, even more preferably at least about 97% of the total amount of phenylseleno blocked lactone produced.
摘要:
R.sup.g is C.sub.1-6 alkyl, C.sub.2-6 alkenyl, C.sub.2-6 alkynyl, C.sub.3-6 cycloalkyl, or a radical of the formula --W--R.sup.x in which W is a bond, C.sub.2-6 alkenediyl, or --(CH.sub.2).sub.t --, in which t is one to six; and R.sup.x is naphthyl, phenyl, or heteroaryl, and furthermore R.sup.x can be optionally substituted with one to three same or different C.sub.1-6 alkyl, C.sub.1-6 alkoxy, halogen or --CF.sub.3 groups;R.sup.2 is --OCOR, H, OH, --OR, --OSO.sub.2 R, --OCONR.sup.o R, --OCONHR, --OCOO(CH.sub.2).sub.t R, or --OCOOR; andR and R.sup.o are independently C.sub.1-6 alkyl, C.sub.2-6 alkenyl, C.sub.3-6 cycloalkyl, C.sub.2-6 alkynyl, or phenyl, optionally substituted with one to three same or different C.sub.1-6 alkyl, C.sub.1-6 alkoxy, halogen or --CF.sub.3 groups.Further provided by this invention are pharmaceutical formulations and intermediates for the the preparation of deoxy taxols of formula I. A method of treating mammalian tumors using a compound of formula I is also provided.
摘要:
The present invention relates to 10-desacetoxytaxol and derivatives thereof, which are useful as antitumor agents. These compounds have the formula ##STR1## wherein R.sub.2 is hydrogen, hydroxy or a protected hydroxy group; R.sub.3 and R.sub.4 are independently hydrogen, hydroxy, a protected hydroxy group, methyl, --SH, --NH.sub.2, or --NR.sub.8 R.sub.9 ; R.sub.5 is R.sub.10, or --OR.sub.10 ; R.sub.6 and R.sub.7 are independently hydrogen, alkyl, or aryl; R.sub.8 and R.sub.9 are independently hydrogen, alkyl, alkenyl, alkynyl, or aryl; and R.sub.10 is alkoxy, alkyl, alkenyl, alkynl, or aryl.