Chronic kidney disease, cancer, chronic inflammatory disorders, nutritional, and genetic deficiency can cause anemia. Hypoxia causes induction of hypoxia-inducible factor (HIF), which stimulates erythropoietin (EPO) synthesis. Prolyl hydroxylase domain (PHD) enzyme inhibition can stabilize hypoxia-inducible factor (HIF). HIF stabilization also decreases hepcidin, a hormone of hepatic origin, which regulates iron homeostasis. PHD inhibitors represent a novel pharmacological treatment of anemia associated with chronic diseases. Many orally active PHD inhibitors like roxadustat, molidustat, vadadustat, and desidustat are in late phase clinical trials. This review discusses the role of PHD inhibitors in the treatment of anemia associated with chronic diseases.

Prolyl Hydroxylase Inhibitors: A Breakthrough in the Therapy of Anemia Associated with Chronic Diseases

Disclosed herein is a compound of formula (I), or a pharmaceutically acceptable salt thereof: 
Also disclosed herein are uses of a compound disclosed herein in the potential treatment or prevention of an IDO-associated disease or disorder. Also disclosed herein are compositions comprising a compound disclosed herein. Further disclosed herein are uses of a composition in the potential treatment or prevention of an IDO-associated disease or disorder.

Novel substituted biaryl compounds as indoleamine 2,3-dioxygenase (ido) inhibitors

The present invention provides a compound represented by formula [I] shown below or a pharmaceutically acceptable salt thereof that has an inhibitory effect on 20-HETE producing enzyme.(in formula [I] above, the structure represented by formula [II] below:represents any of the structures represented by formula group [III] below:R1, R2, R3, and R4independently represent a hydrogen atom, a fluorine atom, methyl, or the like,R5represents any of the structures represented by formula group [IV]:

Pyridine compound substituted with azole

Disclosed is a compound of formula (I): wherein all symbols are defined in the description. Also disclosed are pharmaceutical compositions comprising the compounds, methods of making the compounds, kits comprising the compounds, and methods of using the compounds, compositions and kits for treatment of disorders associated with TREK-1, TREK-2 or both TREK-1 and TREK-2 dysfunction in a mammal.

Activator of trek (twik related k+ channels) channels

The present invention relates to a 3,4-bipyridyl pyrazole derivative, and a preparation method therefor and a medical application thereof. Specifically, the present invention relates to a new 3,4-bipyridyl pyrazole derivative as shown in formula (I), a preparation method for the derivative, a pharmaceutical composition containing the derivative, a use of the derivative as a therapeutic agent, in particular as a TGF-β inhibitor, and a use of the derivative in the preparation of a drug which treats, prevents or reduces cancer mediated by TGF-β overexpression. The substituents in formula (I) have the same definitions as in the description.

3,4-bipyridyl pyrazole derivative, and preparation method therefor and medical application thereof

The present invention provides a compound represented by formula [I'| shown below or a pharmaceutically acceptable salt thereof that has an inhibitory effect on 20-HETE producing enzyme, wherein the structure represented by formula [III] shown below represents any of the structures represented by formula group [IV] shown below, wherein R 1 represents a hydrogen atom, a fluorine atom, methyl, etc.; R 2 , R 3 , and R 4 each independently represent a hydrogen atom, a fluorine atom, or methyl; W represents a single bond, C 1-3 alkanediyl, or the formula -O-CH 2 CH 2 -; and ring A represents (a) substituted C 4-6 cycloalkyl, (b) substituted 4- to 6-membered saturated nitrogen-containing heterocyclyl, (c) substituted phenyl, (d) substituted pyridyl, (e) substituted 2,3-dihydrobenzofuran, (f) 4- to 6-membered saturated oxygen-containing heterocyclyl, etc.

Azole-substituted pyridine compound

The present invention provides a compound represented by formula (I) having a PHD-2-inhibiting action or a pharmacologically acceptable salt thereof (I) (In formula (I), R1 shows a hydrogen atom or optionally substituted C1-3 alkyl; X shows the formula CR2 or a nitrogen atom; R3 shows a hydrogen atom, halogen atom, C1-3 alkyl, or C1-3 alkoxy; Y shows the formula -CONR41-W1-, the formula -CONR42-W2-CO-, a structure represented by formula (β), the formula -CH2NHCO-, formula -CH2OCH2-, or the formula -NHCOCH2-; and ring A shows an optionally substituted C3-8 cycloalkyl, optionally substituted C3-8 cycloalkenyl, optionally substituted aryl, optionally substituted saturated heterocyclyl, or optionally substituted heteroaryl)

Heteroaryl compound substituted by triazolyl

Provided is a compound which has an outstanding GPR119 agonist action. Specifically, a compound represented by general formula (I) or a pharmaceutically permitted salt thereof is provided. (I) [In formula (I), substituent group A represents phenyl or a 5 or 6-membered heteroaryl, W represents a single bond, -O-, -NH-, -OCH2- or -CH2O-, X represents a nitrogen atom or CR21, Y1 represents a nitrogen atom or CR22, Y2 represents a nitrogen atom or CR23, Y3 represents a nitrogen atom or CR24, R21, R22, R23 and R24 which can be the same or different represent a hydrogen atom or C1-6 alkyl, and substituent group B represents (a) C2-6 alkyl, C3-8 cycloalkyl, (C3-8 cycloalkyl)C1-6 alkyl, (aryl)C1-6 alkyl or (saturated heterocyclyl)C1-6 alkyl, (b) -COOR31 (R31 represents C1-6 alkyl, C3-8 cycloalkyl, aryl or saturated heterocyclyl), or (c); 5 or 6-membered heteroaryl represented by general formula (ss). However, a structure represented by formula (A) is excluded.]

Fused heterocyclic compounds

본 발명은, 20-HETE를 산생하는 효소를 저해하는 작용을 갖는 하기 식 [Ⅰ']로 표시되는 화합물 또는 그의 제약학적으로 허용되는 염을 제공한다.(상기 식 [Ⅰ'] 중, 하기 식 [Ⅲ]으로 표시되는 구조는, 하기 식 군 [IV] 중 어느 구조를 나타내며; R은, 수소 원자, 불소 원자, 메틸 등을 나타내고; R, R, 및 R는, 독립적으로 수소 원자, 불소 원자, 또는 메틸을 나타내고; W는, 단결합, C알칸디일, 또는 식 -O-CHCH-를 나타내고; 환 A는, (a) 치환되어 있는 C시클로알킬, (b) 치환되어 있는 질소 원자를 포함하는 4 내지 6원의 포화 헤테로시클릴, (c) 치환되어 있는 페닐, (d) 치환되어 있는 피리딜, (e) 치환되어 있는 2,3-디히드로벤조푸란, (f) 산소 원자를 포함하는 4 내지 6원의 포화 헤테로시클릴 등을 나타냄)

아졸로 치환된 피리딘 화합물

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