摘要:
The invention relates to novel compounds for use in the treatment or prophylaxis of cancers and other proliferative conditions that are for example characterized by cells that express cytochrome P450 1 B1 (CYP1B1) and allelic variants thereof. The invention also provides pharmaceutical compositions comprising one or more such compounds for use in medical therapy, for example in the treatment of prophylaxis of cancers or other proliferative conditions, as well as methods for treating cancers or other conditions in human or non-human animal patients. The invention also provides methods for identifying novel compounds for use in the treatment of prophylaxis of cancers and other proliferative conditions that are for example characterized by cells that express CYP1 B1 and allelic variants thereof. The invention also provides a method for determining the efficacy of a compound of the invention in treating cancer.
摘要:
The present disclosure relates to salts and compositions of isophosphoramide mustard and isophosphoramide mustard analogs. In one embodiment the salts can be represented by the formula I: (I) wherein A + represents an ammonium species selected from the protonated (conjugate acid) or quaternary forms of aliphatic amines and aromatic amines, including basic amino acids, heterocyclic amines, substituted and unsubstituted pyridines, guanidines and amidines; and X and Y independently represent leaving groups. Also disclosed herein are methods for making such compounds and formulating pharmaceutical compositions thereof. Methods for administering the disclosed compounds to subjects, particularly to treat hyperproliferative disorders, also are disclosed.
摘要:
The present invention concerns nitrogenated derivatives of narciclasine and pancratistatin of the following general formula (I) as well as their pharmaceutically acceptable salts. The present invention also concerns the use of these compounds in cancer therapy as well as a method for their preparation.
摘要:
The invention relates to novel co-lipids that can be used in combination with lipophilic compounds used as nucleic acid vectors, for making a nucleic-acid vector composition. The invention also relates to nucleic-acid vector compositions containing a combination of (i) a nucleic-acid cationic lipohilic vector and (ii) a co-lipid. In some embodiments, the nucleic-acid vector compositions are in the form of unilamellar or multilamellar vesicles. The invention also relates to a method for the in vitro or in vivo insertion of a nucleic acid of interest into host cells, that comprises the step of contacting said host cells with a nucleic-acid vector composition as described above.
摘要:
A compound of formula (1), particularly where X = O, Y = NR1R2, wherein R1 = R2 = H and Z1 = Z2 = OH, can protect and/or aid the recovery of functionally impaired tissue whose viability is threatened by hypoxia. Typically, the compounds can be used to aid recovery of function of ischaemic tissue during and after open heart surgery. In said formula, X = O or NH, Y = OH, OR?1, NR1R2¿, wherein R?1 and R2¿ are independently H, alkyl, alkenyl (except where applied to OR1), cycloalkyl, aryl, or aralkyl.
摘要:
The present disclosure relates to salts and compositions of isophosphoramide mustard and isophosphoramide mustard analogs. In one embodiment the salts can be represented by the formula I: (I) wherein A+ represents an ammonium species selected from the protonated (conjugate acid) or quaternary forms of aliphatic amines and aromatic amines, including basic amino acids, heterocyclic amines, substituted and unsubstituted pyridines, guanidines and amidines; and X and Y independently represent leaving groups. Also disclosed herein are methods for making such compounds and formulating pharmaceutical compositions thereof. Methods for administering the disclosed compounds to subjects, particularly to treat hyperproliferative disorders, also are disclosed.
摘要:
The invention relates to the use of at least one overexpression inhibitor of DNA repair genes and oncogenes for producing a medicament used for reinforcing the apoptotic effect of cytostatic drugs following chemotherapy.
摘要:
A method of treating or preventing supraventricular tachyarrhythmias is disclosed which comprises the use of a compound which selectively blocks the ultra-rapidly-activating delayed rectifier K+ current (IKur) of the human atrium.