C07D271/04

Compound for inhibiting IDO, a manufacturing method and a use thereof

A compound for inhibiting IDO represented by the following general formula I, ##STR00001## wherein a bond represented by a wavy line “custom character” indicates the structure which represents independently a cis-isomer, a trans-isomer, or a mixture of cis- and trans-isomers; R.sub.1 and R.sub.2 are each independently selected from the group consisting of H, halogen, alkyl, alkoxyl, and haloalkyl; R.sub.3 is selected from the group consisting of cyclopentyl, cyclohexyl, piperazinyl, and piperidyl; and the substitution positions of R.sub.3 are optionally substituted at 1,2 position, 1,3 position or 1,4 position; m and n are an integer number independently selected from 0 to 5. The compound has a strong inhibiting effect on IDO and can be used to manufacture an IDO inhibitor for the prevention and/or treatment of an IDO-mediated disease with the pathologic features of the tryptophan metabolic pathway.

Compound for inhibiting IDO, a manufacturing method and a use thereof

A compound for inhibiting IDO represented by the following general formula I, ##STR00001## wherein a bond represented by a wavy line “custom character” indicates the structure which represents independently a cis-isomer, a trans-isomer, or a mixture of cis- and trans-isomers; R.sub.1 and R.sub.2 are each independently selected from the group consisting of H, halogen, alkyl, alkoxyl, and haloalkyl; R.sub.3 is selected from the group consisting of cyclopentyl, cyclohexyl, piperazinyl, and piperidyl; and the substitution positions of R.sub.3 are optionally substituted at 1,2 position, 1,3 position or 1,4 position; m and n are an integer number independently selected from 0 to 5. The compound has a strong inhibiting effect on IDO and can be used to manufacture an IDO inhibitor for the prevention and/or treatment of an IDO-mediated disease with the pathologic features of the tryptophan metabolic pathway.

PHARMACEUTICAL SALTS/CO-CRYSTALS OF PENTOXIFYLLINE, CLONIDINE AND LINSIDOMINE WITH CAFFEIC, PROTOCATECHUIC OR alpha-LIPOIC ACID AN USE THEREOF FOR TREATMENT OF PAIN

Disclosed are pharmaceutical salts and co-crystals of pentoxifylline, clonidine and linsidomine with caffeic acid, protocatechuic acid or -lipoic acid, and method for preparing thereof. Also disclosed are topical compositions comprising said salts or co-crystals and use thereof for treating pain.

Substituted bicyclic heterocyclic compounds

Disclosed are compounds of Formula (I), or a salt thereof, wherein: X is CR.sub.4 or N; Y is CR.sub.4 or N, provided that Y is N only if X is N; R.sub.1 is Formulae (A) or (B); each W is independently NR.sub.1b or O; Z is a bond or CHR.sub.1d; and R.sub.1, R.sub.2, R.sub.3, R.sub.4, L.sub.1, R.sub.1a, R.sub.1b, R.sub.1c, and n are defined herein. Also disclosed are methods of using such compounds as inhibitors of ROMK, and pharmaceutical compositions comprising such compounds. These compounds are useful in treating cardiovascular diseases. ##STR00001##

Substituted bicyclic heterocyclic compounds

Disclosed are compounds of Formula (I), or a salt thereof, wherein: X is CR.sub.4 or N; Y is CR.sub.4 or N, provided that Y is N only if X is N; R.sub.1 is Formulae (A) or (B); each W is independently NR.sub.1b or O; Z is a bond or CHR.sub.1d; and R.sub.1, R.sub.2, R.sub.3, R.sub.4, L.sub.1, R.sub.1a, R.sub.1b, R.sub.1c, and n are defined herein. Also disclosed are methods of using such compounds as inhibitors of ROMK, and pharmaceutical compositions comprising such compounds. These compounds are useful in treating cardiovascular diseases. ##STR00001##

Benzamide compounds and their use as herbicides

The invention relates to a compound of formula I, ##STR00001##
an N-oxide or an agriculturally suitable salt thereof, wherein the variables are as defined in the specification, and their use as herbicides.

Benzamide compounds and their use as herbicides

The invention relates to a compound of formula I, ##STR00001##
an N-oxide or an agriculturally suitable salt thereof, wherein the variables are as defined in the specification, and their use as herbicides.

NOVEL VIRAL REPLICATION INHIBITORS

The present invention relates to a series of novel compounds, methods to prevent or treat viral infections in animals by using the novel compounds and to said novel compounds for use as a medicine, more preferably for use as a medicine to treat or prevent viral infections, particularly infections with RNA viruses, more particularly infections with viruses belonging to the family of the Flaviviridae, and yet more particularly infections with the Dengue virus. The present invention furthermore relates to pharmaceutical compositions or combination preparations of the novel compounds, to the compositions or preparations for use as a medicine, more preferably for the prevention or treatment of viral infections. The invention also relates to processes for preparation of the compounds.

##STR00001##

NOVEL VIRAL REPLICATION INHIBITORS

The present invention relates to a series of novel compounds, methods to prevent or treat viral infections in animals by using the novel compounds and to said novel compounds for use as a medicine, more preferably for use as a medicine to treat or prevent viral infections, particularly infections with RNA viruses, more particularly infections with viruses belonging to the family of the Flaviviridae, and yet more particularly infections with the Dengue virus. The present invention furthermore relates to pharmaceutical compositions or combination preparations of the novel compounds, to the compositions or preparations for use as a medicine, more preferably for the prevention or treatment of viral infections. The invention also relates to processes for preparation of the compounds.

##STR00001##

SULFONYL AMIDINE AS INDOLEAMINE-2,3-DIOXYGENASE INHIBITOR, AND PREPARATION METHOD THEREFOR AND USE THEREOF
20200207728 · 2020-07-02 ·

Provided in the present application are a sulfonyl amidine as represented by formula (I) as an indoleamine-2,3-dioxygenase inhibitor, and a preparation method therefor and the use thereof. The compound of formula (I) in the present application can be used as an indoleamine-2,3-dioxygenase inhibitor in the preparation of a drug for preventing and/or treating indoleamine-2,3-dioxygenase-mediated diseases.

##STR00001##