Patent classifications
C07C335/04
Substituted thioureas as heat shock protein 70 inhibitors
The invention provides a compound of Formula I, an isomer, a pharmaceutically acceptable salt, or a solvate thereof, and use thereof in manufacture of a medicament for preventing and/or treating a drug-resistant tumor or disease or disorder caused by a drug-resistant bacterium, or use thereof in manufacture of a medicament for preventing and/or treating a tumor, a neurodegenerative disease, an allogeneic graft rejection, or an infection-associated disease or disorder; preferably, the tumor, neurodegenerative disease, allogeneic graft rejection, or infection-associated disease or disorder is a disease or disorder caused by Heat shock protein 70 (Hsp70). The compounds of the invention, which are a class of Hsp70 inhibitors having a novel structure and a high activity, solve the problem concerning drug resistance of tumors, enhance the effect of treating tumors, and provide a new medical strategy for treatment of tumors in clinic. ##STR00001##
INHIBITORS OF NITRIC OXIDE SYNTHASES (NOS), PHARMACEUTICAL PRODUCTS THEREOF, AND METHODS THEREOF
The present invention provides NOS inhibitors such as iNOS inhibitors, or a pharmaceutically acceptable salt, ester, prodrug, complex, solvate, hydrate, or isomer thereof, in any crystalline form or in amorphous form. The inhibitors include 1,1 or 1,2 substituted-ethyl carbamimido thioates, cyclic compounds substituted with a carbamimidoyl sulfanylethylphenyl group and a carbamimidoylsulfanyl group, compounds substituted with a carbamimidoyl sulfanylethyl phenylmethyl group, bis-carbamimidoylsulfanylethyl substituted compounds, 2-propoxypyridine derivatives, alkylamine or heteroalkylamine derivatives, n-aminoethyl n-phenyl amine derivatives, and saturated heterocyclic fused benzene derivatives. Pharmaceutical products comprising the NOS inhibitors such as iNOS inhibitors and the applications thereof in prophylaxis and/or treatment of inflammatory diseases, and proliferative diseases such as cancer including gastro-intestinal, colorectal, gynecological, pancreatic, head and neck, esophageal, breast, lung, and central nervous system tumors, among others, are also provided.
INHIBITORS OF NITRIC OXIDE SYNTHASES (NOS), PHARMACEUTICAL PRODUCTS THEREOF, AND METHODS THEREOF
The present invention provides NOS inhibitors such as iNOS inhibitors, or a pharmaceutically acceptable salt, ester, prodrug, complex, solvate, hydrate, or isomer thereof, in any crystalline form or in amorphous form. The inhibitors include 1,1 or 1,2 substituted-ethyl carbamimido thioates, cyclic compounds substituted with a carbamimidoyl sulfanylethylphenyl group and a carbamimidoylsulfanyl group, compounds substituted with a carbamimidoyl sulfanylethyl phenylmethyl group, bis-carbamimidoylsulfanylethyl substituted compounds, 2-propoxypyridine derivatives, alkylamine or heteroalkylamine derivatives, n-aminoethyl n-phenyl amine derivatives, and saturated heterocyclic fused benzene derivatives. Pharmaceutical products comprising the NOS inhibitors such as iNOS inhibitors and the applications thereof in prophylaxis and/or treatment of inflammatory diseases, and proliferative diseases such as cancer including gastro-intestinal, colorectal, gynecological, pancreatic, head and neck, esophageal, breast, lung, and central nervous system tumors, among others, are also provided.
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.
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.
THERAPEUTIC COMPOUNDS
The invention provides compounds of 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. The compounds are useful for reducing endoplasmic reticulum stress and for producing analgesia in an animal.
Condensed cyclic compound and organic light-emitting device including the same
A condensed cyclic compound and an organic light-emitting device including the same, the compound being represented by Formula 1, below:
Ar.sub.1-(L.sub.11).sub.b1-(L.sub.1).sub.a1-(L.sub.12).sub.b2-Ar.sub.2<Formula 1>
Condensed cyclic compound and organic light-emitting device including the same
A condensed cyclic compound and an organic light-emitting device including the same, the compound being represented by Formula 1, below:
Ar.sub.1-(L.sub.11).sub.b1-(L.sub.1).sub.a1-(L.sub.12).sub.b2-Ar.sub.2<Formula 1>