C07D313/08

COMPOUNDS AND COMPOSITIONS AND USES THEREOF

Disclosed are compounds of formula (I):

##STR00001##

and pharmaceutical compositions containing such compounds. Methods of treating neurological or psychiatric disease and disorders in a subject in need are also disclosed.

COMPOUNDS AND COMPOSITIONS AND USES THEREOF

Disclosed are compounds of formula (I):

##STR00001##

and pharmaceutical compositions containing such compounds. Methods of treating neurological or psychiatric disease and disorders in a subject in need are also disclosed.

7-membered fused heterocycles and methods of their synthesis

Disclosed are a new method for synthesizing 7-membered fused heterocycles and compounds synthesized by the new method. The method involves a dual activation strategy using an N-heterocyclic carbene catalyst as a first Lewis base and another second Lewis base. Compounds synthesized by the disclosed method may include new benzoxopinone compounds, as well as benzoxepane compounds and benzoazepinone compounds that optionally may be derived from the disclosed benzoxopinone compounds.

7-membered fused heterocycles and methods of their synthesis

Disclosed are a new method for synthesizing 7-membered fused heterocycles and compounds synthesized by the new method. The method involves a dual activation strategy using an N-heterocyclic carbene catalyst as a first Lewis base and another second Lewis base. Compounds synthesized by the disclosed method may include new benzoxopinone compounds, as well as benzoxepane compounds and benzoazepinone compounds that optionally may be derived from the disclosed benzoxopinone compounds.

PROCESS FOR THE PREPARATION OF COMPOUNDS COMPRISING A 2,5-DIHYDROBENZOXEPINE STRUCTURE BY PHOTOCHEMICAL REARRANGEMENT

The synthesis of chemical compounds having a dihydrobenzoxepine structure. In particular, a process for preparing chemical compounds having a 2,5-dihydro-benzoxepine structure by photochemical rearrangement from chemical compounds having a chromene structure. The process including a step of irradiating with ultraviolet radiation a solution in a solvent of the chemical compounds having a chromene structure.

PROCESS FOR THE PREPARATION OF COMPOUNDS COMPRISING A 2,5-DIHYDROBENZOXEPINE STRUCTURE BY PHOTOCHEMICAL REARRANGEMENT

The synthesis of chemical compounds having a dihydrobenzoxepine structure. In particular, a process for preparing chemical compounds having a 2,5-dihydro-benzoxepine structure by photochemical rearrangement from chemical compounds having a chromene structure. The process including a step of irradiating with ultraviolet radiation a solution in a solvent of the chemical compounds having a chromene structure.

Inhibitors of nitric oxide synthases (NOS), pharmaceutical products thereof, and methods thereof
12325681 · 2025-06-10 · ·

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
12325681 · 2025-06-10 · ·

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.

Estrogen receptor-modulating compounds
12497386 · 2025-12-16 · ·

Described herein are compounds that are estrogen receptor modulators. Also described are pharmaceutical compositions and medicaments that include the compounds described herein, as well as methods of using such estrogen receptor modulators, alone and in combination with other compounds, for treating diseases or conditions that are mediated or dependent upon estrogen receptors.

Mitochondrial permeability transition pore (mPTP)-opening inhibitor, novel compound exhibiting mPTP-opening inhibitory activity, and use therefor

The present invention aims to provide a novel compound having a high mPTP-opening inhibitory activity and/or a useful therapeutic effect on various diseases. An aspect of the present invention relates to a mitochondrial permeability transition pore (mPTP)-opening inhibitor, a medicament or a pharmaceutical composition comprising a compound represented by formula (I), wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6, R.sup.7, R.sup.8, R.sup.9, R.sup.10 and R.sup.11 are the same as defined in the specification and the claims, a stereoisomer thereof, a prodrug thereof, or a pharmaceutically acceptable salt thereof, or a pharmaceutically acceptable solvate thereof, as an active ingredient. Another aspect of the present invention relates to a compound represented by formula (Ia), wherein R.sup.1a, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6, R.sup.7, R.sup.8, R.sup.9, R.sup.10 and R.sup.11 are the same as defined in the specification and the claims, a stereoisomer thereof, a prodrug thereof, or a salt thereof, or a solvate thereof.