Patent classifications
C07C335/12
Aminoazole derivative
A compound, represented by the following formula or a medically acceptable salt thereof, having an effect of regulating the activity of an androgen receptor. In the formula, X represents S, O; Z represents (R.sup.a).sub.n-A-(CR.sup.13R.sup.14).sub.0-1(CR.sup.11R.sup.12).sub.0-1; A represents aryl, heteroaryl; R.sup.1 represents alkyl, cycloalkyl, alkenyl, alkynyl, alkoxyalkyl, aryl, arylalkyl, heterocycle, heterocyclic alkyl; R.sup.2 represents hydrogen, halogen, alkyl, cycloalkyl, phenyl; R3 represents hydrogen, halogen, alkyl, cycloalkyl, alkoxyalkyl, alkenyl, alkynyl, cycloalkenyl, aryl, arylalkyl, heterocycle, heterocyclic alkyl, acyl, cycloalkylcarbonyl, benzoyl, spiroalkyl, adamantyl, silyl, R.sup.31R.sup.32NCO; R.sup.4 and R.sup.5 represent hydrogen, halogen, alkyl, phenyl, and cycloalkyl. ##STR00001##
Aminoazole derivative
A compound, represented by the following formula or a medically acceptable salt thereof, having an effect of regulating the activity of an androgen receptor. In the formula, X represents S, O; Z represents (R.sup.a).sub.n-A-(CR.sup.13R.sup.14).sub.0-1(CR.sup.11R.sup.12).sub.0-1; A represents aryl, heteroaryl; R.sup.1 represents alkyl, cycloalkyl, alkenyl, alkynyl, alkoxyalkyl, aryl, arylalkyl, heterocycle, heterocyclic alkyl; R.sup.2 represents hydrogen, halogen, alkyl, cycloalkyl, phenyl; R3 represents hydrogen, halogen, alkyl, cycloalkyl, alkoxyalkyl, alkenyl, alkynyl, cycloalkenyl, aryl, arylalkyl, heterocycle, heterocyclic alkyl, acyl, cycloalkylcarbonyl, benzoyl, spiroalkyl, adamantyl, silyl, R.sup.31R.sup.32NCO; R.sup.4 and R.sup.5 represent hydrogen, halogen, alkyl, phenyl, and cycloalkyl. ##STR00001##
ANTIBACTERIAL HYDROPHILIC COMPOUND AND USE THEREOF
The present disclosure provides an antibacterial hydrophilic compound. The antibacterial hydrophilic compound may react, induced by light through a hydrogen abstraction group in the structural formula thereof, with a CH group and thus bind to a surface of a material having the CH group (for example, chemical fibers such as polyester, chinlon, and the like; plastics, rubbers, and other similar materials), which can impart a durable antibacterial activity and hydrophilicity to the material. The antibacterial hydrophilic compound has a relatively strong binding force to the surface of the material without damaging the mechanical properties of the raw material. The present disclosure also provides a modified material that is modified by the antibacterial hydrophilic compound.
CAPSAZEPINE ANALOGS FOR THE TREATMENT OF CANCER AND OTHER PROLIFERATIVE DISEASES
The present disclosure relates generally to derivatives of capsazepine and methods of use thereof. In some aspects, the present disclosure relates to using capsazepine derivatives to treat cancer or other hyperproliferative diseases.
CAPSAZEPINE ANALOGS FOR THE TREATMENT OF CANCER AND OTHER PROLIFERATIVE DISEASES
The present disclosure relates generally to derivatives of capsazepine and methods of use thereof. In some aspects, the present disclosure relates to using capsazepine derivatives to treat cancer or other hyperproliferative diseases.
DIPHENYL THIOUREA AND DIPHENYL UREA DERIVATIVES AS INHIBITORS OF ENDOCYTOSIS
The present invention relates to method of inhibition of cellular endocytosis by treating the cells with compound of formula-1 Diphenylthio urea and Diphenylurea derivatives. Said invention also discloses method of treatment of infectious diseases, neurological disease, cancer, kidney disease in a subject in need thereof by administering therapeutically effective concentration of compounds of Formula-1, Diphenylthio urea and Diphenylurea derivatives which are effective inhibitors of cellular endocytosis. Said invention also discloses compounds of Formula-1, Diphenylthio urea and Diphenylurea derivatives and pharmaceutical composition comprising compounds of Formula-1, Diphenylthio urea and Diphenylurea derivatives along with suitable excipients.
DIPHENYL THIOUREA AND DIPHENYL UREA DERIVATIVES AS INHIBITORS OF ENDOCYTOSIS
The present invention relates to method of inhibition of cellular endocytosis by treating the cells with compound of formula-1 Diphenylthio urea and Diphenylurea derivatives. Said invention also discloses method of treatment of infectious diseases, neurological disease, cancer, kidney disease in a subject in need thereof by administering therapeutically effective concentration of compounds of Formula-1, Diphenylthio urea and Diphenylurea derivatives which are effective inhibitors of cellular endocytosis. Said invention also discloses compounds of Formula-1, Diphenylthio urea and Diphenylurea derivatives and pharmaceutical composition comprising compounds of Formula-1, Diphenylthio urea and Diphenylurea derivatives along with suitable excipients.
THERAPEUTIC COMPOUNDS
The invention provides methods for producing analgesia in an animal comprising administering to the animal a compound of the formula Ia, Ib, Ic, and Id:
##STR00001##
and pharmaceutically acceptable salts thereof, wherein the variables A, R.sup.6, R.sup.7, R.sup.8, R.sup.9, R.sup.x, L, X, Y, and Z have the meaning as described herein.
THERAPEUTIC COMPOUNDS
The invention provides methods for producing analgesia in an animal comprising administering to the animal a compound of the formula Ia, Ib, Ic, and Id:
##STR00001##
and pharmaceutically acceptable salts thereof, wherein the variables A, R.sup.6, R.sup.7, R.sup.8, R.sup.9, R.sup.x, L, X, Y, and Z have the meaning as described herein.
Capsazepine analogs for the treatment of cancer and other proliferative diseases
The present disclosure relates generally to derivatives of capsazepine and methods of use thereof In some aspects, the present disclosure relates to using capsazepine derivatives to treat cancer or other hyperproliferative diseases. In some aspects of the present disclosure, the disclosure provides capsazepine derivatives which may be useful in the treatment of cancer. Such cancers that the compounds may be used to treating include but are not limited to breast, cervical, oral, head, neck, or prostate cancer. In some aspects, the compounds may be useful in treating a tumor by direct injection of the compound into the tumor, particularly an oral tumor. In other aspects, the compounds are administered systemically. The compounds of the present disclosure may also be used to treat the pain associated with a tumor for which it is being administered.