C07D313/08

INHIBITORS OF NITRIC OXIDE SYNTHASES (NOS), PHARMACEUTICAL PRODUCTS THEREOF, AND METHODS THEREOF
20230286913 · 2023-09-14 · ·

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
20230286913 · 2023-09-14 · ·

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
20220332704 · 2022-10-20 ·

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.

α,β-unsaturated amide compound

An object of the present invention is to provide an α,β-unsaturated amide compound or a pharmaceutically acceptable salt or the like thereof having anticancer activity and the like. The α,β-unsaturated amide compound represented by the following formula (I) or a pharmaceutically acceptable salt or the like thereof has anticancer activity and the like: ##STR00001##
[wherein, “A” represents optionally substituted heterocyclic diyl, R.sup.1 represents hydrogen atom or optionally substituted lower alkyl, R.sup.2 represents optionally substituted aryl, optionally substituted cycloalkyl, optionally substituted aliphatic heterocyclic group or optionally substituted aromatic heterocyclic group, X represents —O—, —S—, —SO.sub.2—, —NR.sup.X1— (wherein, R.sup.X1 represents hydrogen atom or lower alkyl), —CHR.sup.X2— (wherein, R.sup.X2 represents hydrogen atom or hydroxy), —CH═CH—, −CO— or —NH—CO—, and n1 and n2 are the same or different, and each represents 0 or 1].

α,β-unsaturated amide compound

An object of the present invention is to provide an α,β-unsaturated amide compound or a pharmaceutically acceptable salt or the like thereof having anticancer activity and the like. The α,β-unsaturated amide compound represented by the following formula (I) or a pharmaceutically acceptable salt or the like thereof has anticancer activity and the like: ##STR00001##
[wherein, “A” represents optionally substituted heterocyclic diyl, R.sup.1 represents hydrogen atom or optionally substituted lower alkyl, R.sup.2 represents optionally substituted aryl, optionally substituted cycloalkyl, optionally substituted aliphatic heterocyclic group or optionally substituted aromatic heterocyclic group, X represents —O—, —S—, —SO.sub.2—, —NR.sup.X1— (wherein, R.sup.X1 represents hydrogen atom or lower alkyl), —CHR.sup.X2— (wherein, R.sup.X2 represents hydrogen atom or hydroxy), —CH═CH—, −CO— or —NH—CO—, and n1 and n2 are the same or different, and each represents 0 or 1].

Estrogen receptor-modulating compounds
11384068 · 2022-07-12 · ·

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.

Estrogen receptor-modulating compounds
11384068 · 2022-07-12 · ·

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.

Compositions And Methods For Visible-Light-Controlled Ruthenium-Catalyzed Olefin Metathesis
20220219155 · 2022-07-14 ·

The present disclosure provides compositions and methods for metathesizing a first alkenyl or alkynyl group with a second alkenyl or alkynyl group, the composition comprising a ruthenium metathesis catalyst and a photoredox catalyst that is activated by visible light.

Compounds and compositions and uses thereof

Compounds of formula I: ##STR00001##
are disclosed, as are pharmaceutical compositions containing such compounds. Methods of treating neurological or psychiatric diseases and disorders in a subject in need thereof are also disclosed.

Compounds and compositions and uses thereof

Compounds of formula I: ##STR00001##
are disclosed, as are pharmaceutical compositions containing such compounds. Methods of treating neurological or psychiatric diseases and disorders in a subject in need thereof are also disclosed.