C07C391/00

NOVEL ORGANOSELENIUM COMPOUNDS, METHOD FOR PRODUCING SAME, AND PHARMACEUTICAL USES THEREOF IN PARTICULAR AS ANTITUMOR AGENTS
20170114011 · 2017-04-27 ·

The invention relates to a selenium compound. Said selenium compound has formula (I), where R.sup.1=alkyl; R.sup.2=H, R.sup.4C(=0), R.sup.4OC(=0), a-aminoacyl, CH.sub.3SeCH.sub.2CH.sub.2CH(NH.sub.2)C(=0), CH.sub.3SeCH.sub.2CH.sub.2CH(OH)C(=0); X=OH, OR.sup.3, NH.sub.2, NR.sup.4R.sup.5, -amino acid, CH.sub.3SeCH.sub.2CH.sub.2CH(COOH)NH, CH.sub.3SeCH.sub.2CH.sub.2CH(COOH)0-; R.sup.3=alkyl; R.sup.4=alkyl, aryl; R.sup.5=H, alkyl, aryl; R.sup.4 and R.sup.5 which can together form a 5- or 6-membered cycloalkyl radical which can comprise a heteroatom; provided that when X=NH-terbutyl, R.sup.2C(=0)CH.sub.3. Said compound can be used as a pharmaceutical substance, in particular as an antitumour substance.

IDO/TDO Inhibitor

A compound of formula (I) given below or a pharmaceutically acceptable salt of the compound is useful as an IDO/TDO inhibitor. Thus, the compound of formula (I) or the pharmaceutically acceptable salt of the compound can be used as, for example, a therapeutic agent for a disease or a disorder selected from tumor, infectious disease, neurodegenerative disorder, cataract, organ transplant rejection, autoimmune disease, postoperative cognitive impairment, and disease related to women's reproductive health [in the following formula (I), ring A represents an aromatic ring, an aliphatic ring, a heterocyclic ring, or a condensed ring of two or more rings selected from an aromatic ring, an aliphatic ring and a heterocyclic ring; X, R.sup.1 and R.sup.2 represent a substituent on a ring atom constituting ring A; m represents an integer of 0 to 6; X represents, for example, a halogen atom; and R.sup.1 and R.sup.2 are the same or different and are selected from, for example, the group consisting of groups of formula (a) or formula (b); and in the following formula (a) and formula (b), Y is selected from the group consisting of O, S, and Se, Z is selected from the group consisting of O, S, and Se, n represents an integer of 1 to 8, r represents an integer of 1 to 8, s represents an integer of 1 to 8, R.sup.4 represents, for example, C(NH)HN.sub.2, and R.sup.6 represents, for example, a substituted or unsubstituted aryl group].

##STR00001##

IDO/TDO Inhibitor

A compound of formula (I) given below or a pharmaceutically acceptable salt of the compound is useful as an IDO/TDO inhibitor. Thus, the compound of formula (I) or the pharmaceutically acceptable salt of the compound can be used as, for example, a therapeutic agent for a disease or a disorder selected from tumor, infectious disease, neurodegenerative disorder, cataract, organ transplant rejection, autoimmune disease, postoperative cognitive impairment, and disease related to women's reproductive health [in the following formula (I), ring A represents an aromatic ring, an aliphatic ring, a heterocyclic ring, or a condensed ring of two or more rings selected from an aromatic ring, an aliphatic ring and a heterocyclic ring; X, R.sup.1 and R.sup.2 represent a substituent on a ring atom constituting ring A; m represents an integer of 0 to 6; X represents, for example, a halogen atom; and R.sup.1 and R.sup.2 are the same or different and are selected from, for example, the group consisting of groups of formula (a) or formula (b); and in the following formula (a) and formula (b), Y is selected from the group consisting of O, S, and Se, Z is selected from the group consisting of O, S, and Se, n represents an integer of 1 to 8, r represents an integer of 1 to 8, s represents an integer of 1 to 8, R.sup.4 represents, for example, C(NH)HN.sub.2, and R.sup.6 represents, for example, a substituted or unsubstituted aryl group].

##STR00001##

Polysubstituted selenium-containing cyclopent(hex)ene skeleton derivative and synthesis method thereof

The present invention provides a polysubstituted selenium-containing cyclopent(hex)ene skeleton derivative and a synthesis method thereof. The polysubstituted selenium-containing cyclopent(hex)ene skeleton derivative is prepared by a one-pot method using an arylacetylene compound and an unsaturated selenide reagent as reaction materials, in the presence of a free radical initiator. The synthesis method of the present invention is simple and efficient, requires no metal catalyst, has mild reaction conditions, and has good functional group tolerance and broad substrate scope. Moreover, cyclopent(hex)ene compounds with different substituents are widely present in active drug molecules, and selenium-containing compounds also have good biological activity against tumors, oxidation, inflammation, bacteria, viruses and others. Therefore, a complex selenide-containing cyclopent(hex)ene skeleton derivative is obtained starting from a simple substrate by the synthesis method of the present invention by constructing a CSe bond through a simple, efficient and sustainable strategy. The present invention has broad application prospects.

Polysubstituted selenium-containing cyclopent(hex)ene skeleton derivative and synthesis method thereof

The present invention provides a polysubstituted selenium-containing cyclopent(hex)ene skeleton derivative and a synthesis method thereof. The polysubstituted selenium-containing cyclopent(hex)ene skeleton derivative is prepared by a one-pot method using an arylacetylene compound and an unsaturated selenide reagent as reaction materials, in the presence of a free radical initiator. The synthesis method of the present invention is simple and efficient, requires no metal catalyst, has mild reaction conditions, and has good functional group tolerance and broad substrate scope. Moreover, cyclopent(hex)ene compounds with different substituents are widely present in active drug molecules, and selenium-containing compounds also have good biological activity against tumors, oxidation, inflammation, bacteria, viruses and others. Therefore, a complex selenide-containing cyclopent(hex)ene skeleton derivative is obtained starting from a simple substrate by the synthesis method of the present invention by constructing a CSe bond through a simple, efficient and sustainable strategy. The present invention has broad application prospects.

ORGANIC DISELENIDE COMPOSITION
20260078087 · 2026-03-19 ·

A novel organic diselenide composition comprises 1,2-bis(4-vinylbenzyl) diselane. The organic diselenide composition may be incorporated with one or more polymers through a chemical bonding process for utilization as an agent against infectious, disease-causing agents.

ORGANIC DISELENIDE COMPOSITION
20260078087 · 2026-03-19 ·

A novel organic diselenide composition comprises 1,2-bis(4-vinylbenzyl) diselane. The organic diselenide composition may be incorporated with one or more polymers through a chemical bonding process for utilization as an agent against infectious, disease-causing agents.

Complexes and Compounds of Mercaptophenols and Curcumin for Therapeutic Applications
20260109720 · 2026-04-23 · ·

Complexes and compounds of phenolic molecules possessing two or more ionizable groups, including curcumin, mercaptophenols, and structurally related derivatives, are disclosed. In certain embodiments, a metal or metalloid or nonmetallic atom is directly bonded to the -carbon of curcumin or exclusively to the sulfur atom of a mercaptophenol, conferring enhanced aqueous solubility and stability under physiological and alkaline conditions. The invention includes compositions, processes for preparation, and therapeutic methods employing such complexes and compounds, which may form pharmaceutically acceptable salts suitable for biomedical applications, including parenteral or systemic administration. The complexes and compounds exhibit antiproliferative, anti-migratory, anti-invasive, and immune-stimulatory activities in cell-based and animal models and are suitable for treatment or management of conditions involving abnormal cell proliferation, pathogenic invasion, or dysregulated immune responses.

Complexes and Compounds of Mercaptophenols and Curcumin for Therapeutic Applications
20260109720 · 2026-04-23 · ·

Complexes and compounds of phenolic molecules possessing two or more ionizable groups, including curcumin, mercaptophenols, and structurally related derivatives, are disclosed. In certain embodiments, a metal or metalloid or nonmetallic atom is directly bonded to the -carbon of curcumin or exclusively to the sulfur atom of a mercaptophenol, conferring enhanced aqueous solubility and stability under physiological and alkaline conditions. The invention includes compositions, processes for preparation, and therapeutic methods employing such complexes and compounds, which may form pharmaceutically acceptable salts suitable for biomedical applications, including parenteral or systemic administration. The complexes and compounds exhibit antiproliferative, anti-migratory, anti-invasive, and immune-stimulatory activities in cell-based and animal models and are suitable for treatment or management of conditions involving abnormal cell proliferation, pathogenic invasion, or dysregulated immune responses.