Patent classifications
C07F15/0013
Lobaplatin crystal, preparation method and pharmaceutical application
The present invention relates to new crystals A, B and F of lobaplatin as well as preparation methods therefor and pharmaceutical applications thereof. Lobaplatin crystal A has a melting point Tm.p. of 220?5? C. and is obtained by adding a lobaplatin trihydrate to a suspension crystallization solvent. Lobaplatin crystal B has a melting point T.sub.m.p. of 230?5? C. and is obtained by performing solvent evaporation on a lobaplatin trihydrate or by adding a solvent to a lobaplatin dihydrate, and performing room temperature evaporation or solventing-out crystallization and then drying. Lobaplatin crystal F has a melting point Tm.p. of 229?5? C. and is obtained by adding methanol or ethanol to a lobaplatin dihydrate, stirring at room temperature until solids are dissolved, filtering out insolubles, slowly adding an organic solvent, crystallizing out, separating the crystal and drying the crystal. Compared with the existing lobaplatin and lobaplatin trihydrate, the lobaplatin crystals A, B and F have better stability and solubility, are more suitable for preparation of various forms of pharmaceutical preparations, are more suitable for storage and use, and can be better used for treating cancers such as breast cancer, small cell lung cancer, or chronic myeloid leukemia.
Metal Complexes
The present invention relates to metal complexes and to electronic devices, especially organic electroluminescent devices, comprising these metal complexes, especially as emitters.
ARSENOPLATIN ANTI-CANCER AGENTS
Disclosed herein are methods of treating a cancer cell that include contacting a cancer cell with a compound having the structure of formula (I)
##STR00001##
M is Pt, Pd or Ni; Q is As, Sb or Bi; Z.sup.1 is N; Z.sup.2 is O or S; L.sup.1 and L.sup.2 are independently C(O), CR.sup.1 or CR.sup.2; X is a Lewis base; Y.sup.1 and Y.sup.2 are independently selected from OR.sup.3, OR.sup.4, SR.sup.3 and SR.sup.4, wherein R.sup.1 and R.sup.2 are independently selected from hydrogen, halogen, cyano, keto, ester, ether, thiol, thioether, thioester, imino, C.sub.1-C.sub.10 alkyl, C.sub.1-C.sub.10 alkenyl, alkynyl, alkoxyl, amino, amidyl, immino, sulfonyl, sulfoxyl, phosphoryl, phosphoryl ester, glycosyl, aryl, C.sub.3-C.sub.15 cycloalkyl, heteroaryl, and C.sub.3-C.sub.15 heterocycloalkyl; and R.sup.3 and R.sup.4 are independently selected from hydrogen, C.sub.1-C.sub.10 alkyl, C.sub.1-C.sub.10 alkenyl, alkynyl, alkoxyl, amino, amidyl, immino, sulfonyl, sulfoxyl, phosphoryl, phosphoryl ester, glycosyl, aryl, C.sub.3-C.sub.15 cycloalkyl, heteroaryl, and C.sub.3-C.sub.15 heterocycloalkyl.
Arsenoplatin anti-cancer agents
Disclosed herein are conjugates that include a ligand, and a compound having the structure of formula (I) ##STR00001##
M is Pt, Pd or Ni; Q is As, Sb or Bi; Z.sup.1 is N; Z.sup.2 is O or S; L.sup.1 and L.sup.2 are independently C(O), CR.sup.1 or CR.sup.2; X is a Lewis base; Y.sup.1 and Y.sup.2 are independently selected from OR.sup.3, OR.sup.4, SR.sup.3 and SR.sup.4, wherein R.sup.1 and R.sup.2 are independently selected from hydrogen, halogen, cyano, keto, ester, ether, thiol, thioether, thioester, imino, C.sub.1-C.sub.10 alkyl, C.sub.1-C.sub.10 alkenyl, alkynyl, alkoxyl, amino, amidyl, immino, sulfonyl, sulfoxyl, phosphoryl, phosphoryl ester, glycosyl, aryl, C.sub.3-C.sub.15 cycloalkyl, heteroaryl, and C.sub.3-C.sub.15 heterocycloalkyl; and R.sup.3 and R.sup.4 are independently selected from hydrogen, C.sub.1-C.sub.10 alkyl, C.sub.1-C.sub.10 alkenyl, alkynyl, alkoxyl, amino, amidyl, immino, sulfonyl, sulfoxyl, phosphoryl, phosphoryl ester, glycosyl, aryl, C.sub.3-C.sub.15 cycloalkyl, heteroaryl, and C.sub.3-C.sub.15 heterocycloalkyl.
Lobaplatin Crystal, Preparation Method And Pharmaceutical Application
The present invention relates to new crystals A, B and F of lobaplatin as well as preparation methods therefor and pharmaceutical applications thereof. Lobaplatin crystal A has a melting point Tm.p. of 2205 C. and is obtained by adding a lobaplatin trihydrate to a suspension crystallization solvent. Lobaplatin crystal B has a melting point T.sub.m.p. of 2305 C. and is obtained by performing solvent evaporation on a lobaplatin trihydrate or by adding a solvent to a lobaplatin dihydrate, and performing room temperature evaporation or solventing-out crystallization and then drying. Lobaplatin crystal F has a melting point Tm.p. of 2295 C. and is obtained by adding methanol or ethanol to a lobaplatin dihydrate, stirring at room temperature until solids are dissolved, filtering out insolubles, slowly adding an organic solvent, crystallizing out, separating the crystal and drying the crystal. Compared with the existing lobaplatin and lobaplatin trihydrate, the lobaplatin crystals A, B and F have better stability and solubility, are more suitable for preparation of various forms of pharmaceutical preparations, are more suitable for storage and use, and can be better used for treating cancers such as breast cancer, small cell lung cancer, or chronic myeloid leukemia.
ARSENOPLATIN ANTI-CANCER AGENTS
Disclosed herein are conjugates that include a ligand, and a compound having the structure of formula (I)
##STR00001##
M is Pt, Pd or Ni; Q is As, Sb or Bi; Z.sup.1 is N; Z.sup.2 is O or S; L.sup.1 and L.sup.2 are independently C(O), CR.sup.1 or CR.sup.2; X is a Lewis base; Y.sup.1 and Y.sup.2 are independently selected from OR.sup.3, OR.sup.4, SR.sup.3 and SR.sup.4, wherein R.sup.1 and R.sup.2 are independently selected from hydrogen, halogen, cyano, keto, ester, ether, thiol, thioether, thioester, imino, C.sub.1-C.sub.10 alkyl, C.sub.1-C.sub.10 alkenyl, alkynyl, alkoxyl, amino, amidyl, immino, sulfonyl, sulfoxyl, phosphoryl, phosphoryl ester, glycosyl, aryl, C.sub.3-C.sub.15 cycloalkyl, heteroaryl, and C.sub.3-C.sub.15 heterocycloalkyl; and R.sup.3 and R.sup.4 are independently selected from hydrogen, C.sub.1-C.sub.10 alkyl, C.sub.1-C.sub.10 alkenyl, alkynyl, alkoxyl, amino, amidyl, immino, sulfonyl, sulfoxyl, phosphoryl, phosphoryl ester, glycosyl, aryl, C.sub.3-C.sub.15 cycloalkyl, heteroaryl, and C.sub.3-C.sub.15 heterocycloalkyl.
SILOXANE FUNCTIONALIZED PLATINUM OXALATE COMPLEX
The present invention is platinum(II) oxalate compound of the following formula: where R.sup.1, R.sup.2, and R.sup.3 are as defined herein. The platinum(II) oxalate compound of the present invention is useful as a catalyst in hydrosilylation reactions, especially the hydrosilylation of curable siloxanes.
##STR00001##