Patent classifications
C07C233/57
Method and mixture to form functionalized cyclic compounds
A method for producing a homocyclic or heterocyclic compound includes reacting a compound of formula (I) with a compound of formula (II) in presence of a base:
R.sup.1—B-G (I) ##STR00001##
In formula (I), B is an unsaturated moiety selected from substituted or unsubstituted vinylene, ethynylene, aryleneethynylene, substituted or unsubstituted arylenevinylene, and a combination thereof, the vinylene or arylenevinylene has n (=0, 1 or 2) substituent(s) R.sup.2, G is an electron-withdrawing group, R.sup.1 is hydrogen or a substituent, and two of R.sup.1, R.sup.2 and G may joint together to form a ring. In formula (II), R.sup.3 and R.sup.4 are independently hydrogen or a substituent, R.sup.5 is an electron-withdrawing group, and two of R.sup.3, R.sup.4 and R.sup.5 may joint together to form a ring. The conjugate acid of the base has a pK.sub.a in the range of 1 to 15.
Method and mixture to form functionalized cyclic compounds
A method for producing a homocyclic or heterocyclic compound includes reacting a compound of formula (I) with a compound of formula (II) in presence of a base:
R.sup.1—B-G (I) ##STR00001##
In formula (I), B is an unsaturated moiety selected from substituted or unsubstituted vinylene, ethynylene, aryleneethynylene, substituted or unsubstituted arylenevinylene, and a combination thereof, the vinylene or arylenevinylene has n (=0, 1 or 2) substituent(s) R.sup.2, G is an electron-withdrawing group, R.sup.1 is hydrogen or a substituent, and two of R.sup.1, R.sup.2 and G may joint together to form a ring. In formula (II), R.sup.3 and R.sup.4 are independently hydrogen or a substituent, R.sup.5 is an electron-withdrawing group, and two of R.sup.3, R.sup.4 and R.sup.5 may joint together to form a ring. The conjugate acid of the base has a pK.sub.a in the range of 1 to 15.
Substituted pyrrolizines for the treatment of hepatitis B
The present invention relates to a bicyclic nucleocapsid inhibitor and the use of the same as a drug in the treatment of hepatitis B. In particular, disclosed is a compound having a structure shown by the following formula (A1): ##STR00001##
or a stereoisomer or a tautomer thereof, or a pharmaceutically acceptable salt, a hydrate, or a solvate thereof, that can be used as an HBV inhibitor, wherein the definition of each group is as described in detail in the description. The present invention also relates to a pharmaceutical composition comprising the compound and the use of the same in the treatment of hepatitis B.
C7-FLUORO SUBSTITUTED TETRACYCLINE COMPOUNDS
The present invention is directed to a compound represented by Structural Formula (A):
##STR00001##
or a pharmaceutically acceptable salt thereof. The variables for Structural Formula (A) are defined herein. Also described is a pharmaceutical composition comprising the compound of Structural Formula (A) and its therapeutic use.
C7-FLUORO SUBSTITUTED TETRACYCLINE COMPOUNDS
The present invention is directed to a compound represented by Structural Formula (A):
##STR00001##
or a pharmaceutically acceptable salt thereof. The variables for Structural Formula (A) are defined herein. Also described is a pharmaceutical composition comprising the compound of Structural Formula (A) and its therapeutic use.
Multi-tyrosine kinase inhibitors derivatives and methods of use
The present invention is directed to multi-tyrosine kinase inhibitor compounds. The present invention is further directed to compositions comprising those compounds. Finally, the present invention is directed to methods of treating eye conditions including, but not limited to, diabetic background retinopathy, diabetic macular edema, diabetic proliferative retinopathy, diabetic macular edema with proliferative retinopathy, proliferative fibrovascular disease, diabetic macular edema with proliferative fibrovascular disease, retinopathy of prematurity, dry macular degeneration, dry macular degeneration with drusen and wet macular degeneration, using compounds and compositions of the invention.
Multi-tyrosine kinase inhibitors derivatives and methods of use
The present invention is directed to multi-tyrosine kinase inhibitor compounds. The present invention is further directed to compositions comprising those compounds. Finally, the present invention is directed to methods of treating eye conditions including, but not limited to, diabetic background retinopathy, diabetic macular edema, diabetic proliferative retinopathy, diabetic macular edema with proliferative retinopathy, proliferative fibrovascular disease, diabetic macular edema with proliferative fibrovascular disease, retinopathy of prematurity, dry macular degeneration, dry macular degeneration with drusen and wet macular degeneration, using compounds and compositions of the invention.
2,3-DIHYDRO-1H-INDOLE COMPOUNDS
The present invention relates to certain novel 2,3-dihydro-1H-indole compounds, pharmaceutical compositions comprising the compounds, and methods of using the compounds to treat cancer, more particularly for the treatment of cancer selected from the group consisting of melanoma, acute myeloid leukemia, chronic lymphocytic leukemia, colorectal cancer, breast cancer, lung cancer, ovarian cancer, fallopian tube carcinoma, primary peritoneal carcinoma, cervical cancer, gastric cancer, liver cancer, pancreatic cancer, thyroid cancer, glioma, non-Hodgkin's lymphoma, and Hodgkin's lymphoma.
2,3-DIHYDRO-1H-INDOLE COMPOUNDS
The present invention relates to certain novel 2,3-dihydro-1H-indole compounds, pharmaceutical compositions comprising the compounds, and methods of using the compounds to treat cancer, more particularly for the treatment of cancer selected from the group consisting of melanoma, acute myeloid leukemia, chronic lymphocytic leukemia, colorectal cancer, breast cancer, lung cancer, ovarian cancer, fallopian tube carcinoma, primary peritoneal carcinoma, cervical cancer, gastric cancer, liver cancer, pancreatic cancer, thyroid cancer, glioma, non-Hodgkin's lymphoma, and Hodgkin's lymphoma.
NOVEL ADAMANTANE DERIVATIVE COMPOUND
Disclosed is a novel adamantine derivative compound, an isomer thereof, pharmaceutically acceptable salt thereof, prodrug thereof, hydrate thereof or a solvate thereof. Also disclosed is a method for preparing a novel adamantine derivative compound, an isomer thereof, pharmaceutically acceptable salt thereof, prodrug thereof, hydrate thereof or a solvate thereof. The novel adamantane derivative compound or the like has an excellent anti-androgenic effect.