Disclosed herein are small molecules that inhibit apoptosis and promote autophagy through the TRADD pathway, and their use for treatment of neurodegenerative diseases. Methods of preparing these small molecules and medicinal efficacy are described.

Disclosed herein are small molecules that inhibit apoptosis and promote autophagy through the TRADD pathway, and their use for treatment of neurodegenerative diseases. Methods of preparing these small molecules and medicinal efficacy are described.

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, a heterocyclic ring, or a condensed ring of two or more rings selected from an aromatic ring, and a heterocyclic ring, wherein ring A is selected from the group consisting of a benzene ring, a naphthalene ring, a quinoxaline ring, a thiophene ring, an indole ring, a benzothiophene ring, an imidazole ring, a quinoline ring, a quinazoline ring, and a pyridine ring; X, R.sup.1 and R.sup.2 represent a substituent on a ring atom constituting ring A, wherein R.sup.1 and R.sup.2 are bonded to adjacent ring atoms of ring A; m represents an integer of 1 or 2; X is a halogen atom, and when m is 2, each X is the same or different; R.sup.1 and R.sup.2 are the same or different; R.sup.1 and R.sup.2 independently represent a group represented from the following groups:

—(CH.sub.2).sub.n—Y—R.sup.4

wherein Y is selected from the group consisting of O, S, SO, SO.sub.2, and Se, n represents an integer of 1 to 8, R.sup.4 represents

##STR00001##

wherein R.sup.41, R.sup.42 and R.sup.47 are the same and are a hydrogen atom

##STR00002##

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, a heterocyclic ring, or a condensed ring of two or more rings selected from an aromatic ring, and a heterocyclic ring, wherein ring A is selected from the group consisting of a benzene ring, a naphthalene ring, a quinoxaline ring, a thiophene ring, an indole ring, a benzothiophene ring, an imidazole ring, a quinoline ring, a quinazoline ring, and a pyridine ring; X, R.sup.1 and R.sup.2 represent a substituent on a ring atom constituting ring A, wherein R.sup.1 and R.sup.2 are bonded to adjacent ring atoms of ring A; m represents an integer of 1 or 2; X is a halogen atom, and when m is 2, each X is the same or different; R.sup.1 and R.sup.2 are the same or different; R.sup.1 and R.sup.2 independently represent a group represented from the following groups:

—(CH.sub.2).sub.n—Y—R.sup.4

wherein Y is selected from the group consisting of O, S, SO, SO.sub.2, and Se, n represents an integer of 1 to 8, R.sup.4 represents

##STR00001##

wherein R.sup.41, R.sup.42 and R.sup.47 are the same and are a hydrogen atom

##STR00002##

The present invention concerns the synthesis and use of formulations of 5-substituted 2, 4-thiazolidinediones, pseudothiohydantoins, and propseudothiohydantoins and 2, 4-thiazolidinediones metforminate salts for topical and systemic treatments of infections caused by herpes simplex viruses and varicella zoster viruses.

The present invention concerns the synthesis and use of formulations of 5-substituted 2, 4-thiazolidinediones, pseudothiohydantoins, and propseudothiohydantoins and 2, 4-thiazolidinediones metforminate salts for topical and systemic treatments of infections caused by herpes simplex viruses and varicella zoster viruses.

The invention relates to compounds of formula (I) as follows: (I) wherein X.sup.1 and X.sup.2, identical or different, are NR.sup.5 or a sulfur atom, Y is a group (C.sub.1-C.sub.10)alkanediyl, Ar.sup.1 and Ar.sup.2, identical or different, are an aryl group optionally substituted by one or several groups selected from a halogen atom, a (C.sub.1-C.sub.6) alkyl, —OR.sup.1, —NR.sup.1R.sup.2 and —COOR.sup.3′ with R.sup.1 and R.sup.2, independently of each other, are a hydrogen atom, a (C-.sub.1-C.sub.6) alkyl group or a —COR.sup.3 group, R.sup.3 and R.sup.4′ independently of each other, are a hydrogen atom or a (C.sub.1-C.sub.6) alkyl group, and R.sup.5 is a hydrogen atom or a (C.sub.1-C.sub.6)alkyl group, or a pharmaceutically acceptable salt and/or solvate thereof, in particular for use in cancer treatment.

##STR00001##

The invention relates to compounds of formula (I) as follows: (I) wherein X.sup.1 and X.sup.2, identical or different, are NR.sup.5 or a sulfur atom, Y is a group (C.sub.1-C.sub.10)alkanediyl, Ar.sup.1 and Ar.sup.2, identical or different, are an aryl group optionally substituted by one or several groups selected from a halogen atom, a (C.sub.1-C.sub.6) alkyl, —OR.sup.1, —NR.sup.1R.sup.2 and —COOR.sup.3′ with R.sup.1 and R.sup.2, independently of each other, are a hydrogen atom, a (C-.sub.1-C.sub.6) alkyl group or a —COR.sup.3 group, R.sup.3 and R.sup.4′ independently of each other, are a hydrogen atom or a (C.sub.1-C.sub.6) alkyl group, and R.sup.5 is a hydrogen atom or a (C.sub.1-C.sub.6)alkyl group, or a pharmaceutically acceptable salt and/or solvate thereof, in particular for use in cancer treatment.

##STR00001##

A corrosion inhibitor for a soft water circulation heating and cooling system, wherein the corrosion inhibitor is pentapentanol core hyperbranched macromolecule functionalized by isothiourea and carboxyl, which has a chemical formula of C.sub.5H.sub.7O.sub.5{COC(CH.sub.3)[CH.sub.2OCOCH.sub.2CH(COOH)SC(NH)NH.sub.2].sub.2}.sub.5. The corrosion inhibitor provided by the present invention is non-phosphorus, biodegradable, non-toxic, low in cost and has good corrosion inhibition effect. Moreover, it has excellent corrosion inhibition performance for circulating heating and cooling systems using soft water as the water source, and can significantly improve the reuse rate of circulating water. The present invention also provides a preparation method of the corrosion inhibitor, which is simple, easy to obtain raw materials and easy to industrialize.

A corrosion inhibitor for a soft water circulation heating and cooling system, wherein the corrosion inhibitor is pentapentanol core hyperbranched macromolecule functionalized by isothiourea and carboxyl, which has a chemical formula of C.sub.5H.sub.7O.sub.5{COC(CH.sub.3)[CH.sub.2OCOCH.sub.2CH(COOH)SC(NH)NH.sub.2].sub.2}.sub.5. The corrosion inhibitor provided by the present invention is non-phosphorus, biodegradable, non-toxic, low in cost and has good corrosion inhibition effect. Moreover, it has excellent corrosion inhibition performance for circulating heating and cooling systems using soft water as the water source, and can significantly improve the reuse rate of circulating water. The present invention also provides a preparation method of the corrosion inhibitor, which is simple, easy to obtain raw materials and easy to industrialize.