3-Pyrrolylsulfonamide compounds as GPR17 antagonists

Abstract

The present invention relates to a compound represented by formula (I) [Case 1] JPEG2024520882000204.jpg31165 (In the formula, R 1 , R 2 , R 3 and R 4 is as defined in the specification and claims, or a tautomer, stereoisomer, hydrate, solvate, polymorph, prodrug, isotope or co-crystal thereof, or a pharma- ceutically acceptable salt thereof. The invention also relates to a pharmaceutical composition comprising the compound according to the invention and a pharma- ceutically acceptable carrier. The invention also relates to the present compound for use as a medicament and / or diagnostic agent. The invention also relates to the present compound for use in the prophylaxis and / or treatment of a GPR17 mediated disorder, e.g. a disorder or syndrome selected from disorders or syndromes associated with myelination disorders and brain tissue damage.

Description

[Technical Field]

[0001] The present invention relates to novel pyrrolyl-sulfonamide compounds and their use for treating and / or preventing GPR17-mediated disorders. The present invention also relates to said compounds for use as medicaments and / or in diagnostic methods, more preferably for use as medicaments for treating and / or preventing GPR17-mediated disorders. The present invention further relates to pharmaceutical compositions or combined preparations of the compounds, for use as medicaments and / or in diagnostic methods, more preferably for the prevention and / or treatment of GPR17-mediated disorders. The present invention also relates to methods for preparing said compounds. [Background technology]

[0002] GPR17 is a member of a class of membrane receptors called G protein-coupled receptors (GPCRs). These receptors are characterized by a seven-transmembrane domain structure with an intracellular region that couples to numerous intracellular signaling pathways via G proteins. Many GPCRs have been used as targets for pharmaceutical and diagnostic agents. GPR17 is currently considered an orphan GPCR, reflecting the fact that the receptor's endogenous ligand(s) have not been conclusively identified. GPR17 expression has been identified in the central nervous system (CNS), but also outside the CNS in various human organs, such as the heart and kidney, typically in organs undergoing ischemic injury (Lecca et al., Glia. 2020 Oct;68(10):1957-1967). There are two forms of the receptor expressed in humans, differing in that they contain a 28-amino acid sequence at the N-terminus. The short form of the receptor, lacking the 28 amino acids, is generally thought to be expressed in the CNS, while the long form of the receptor is expressed outside the CNS, e.g., in the heart and kidney (Benned-Jensen and Rosenkilde, Br J Pharmacol. 2010 Mar;159(5):1092-1105). The sequence of this receptor is widely conserved across species, with the rodent and human forms of the receptor being approximately 90% identical, so experiments studying GPR17 using mice or rats are expected to reflect the characteristics of human GPR17.

[0003] Although the endogenous ligand(s) for GPR17 have not been conclusively identified, it has been possible to characterize this receptor by inducing its expression in different cell lines, such as HEK293 cells and CHO cells. Using these expression systems, activators and inhibitors of this receptor have been identified. Activators include the compound MDL29,951 (Hennen et al., Sci Signal. 2013 Oct 22;6(298):ra93). Inhibitors include the compounds pranlukast and HAMI3379 (Simon et al., Mol Pharmacol. 2017 May;91(5):518-532; Merten et al., Cell Chem Biol. 2018 Jun 21;25(6):775-786). While these compounds are useful tools for investigating the signaling properties of GPR17, their utility is limited by their lack of selectivity for GPR17. For example, MDL29,951 is approximately ten times more potent as an NMDA receptor antagonist than GPR17 activators, and pranlukast is approximately 1,000 times more potent as an inhibitor of cysteinyl leukotriene receptors.

[0004] Effective modulation of GPR17 activity may have neuroprotective, anti-inflammatory, and anti-ischemic effects and may therefore be useful in treating cerebral, cardiac, and renal ischemia, as well as stroke, and / or improving recovery from these events (Bonfanti et al., Cell Death Dis. 2017 Jun;8(6):e2871). Furthermore, pulmonary fibrosis may be alleviated by suppressing GPR17-mediated inflammation (Zhan et al., Int Immunopharmacol. 2018 Sep;62:261-269). GPR17 modulators are also thought to be involved in food intake, insulin, and leptin responses, and thus may have a role in the treatment of obesity (Ren et al., Cell. 2012 Jun 8;149(6):1314-1326).

[0005] The function of GPR17 in the CNS can be elucidated by experiments in which the receptor was ablated or overexpressed in mice (Chen et al., Nat Neurosci. 2009 Nov;12(11):1398-406). Mice overexpressing GPR17 exhibited defects in the production of myelin, a sheath formed around axons by oligodendrocytes that is necessary for signal transduction and maintenance of neuronal function. As a result of the defect in myelin production, GPR17-overexpressing mice died within one month of birth. Conversely, mice with GPR17 knockout exhibited premature myelination. These findings suggest that GPR17 plays an important role in regulating myelin production. This conclusion is consistent with observations in rodents and humans that GPR17 is selectively expressed in oligodendrocyte progenitor cells (OPCs). OPCs are stem cells found in the brain throughout life. OPCs then differentiate into oligodendrocytes, which can form myelin. The selective expression of GPR17 in OPCs and observations in mice with regulated GPR17 expression are consistent with the conclusion that GPR17 regulates myelin formation (Lecca et al., Glia. 2020 Oct;68(10):1957-1967). Furthermore, these findings also suggest that reducing GPR17 activity with antagonistic or inverse agonist compounds increases myelination. This conclusion is supported by numerous additional findings, including the observation that GPR17- / - mice have enhanced remyelination after toxin-induced injury compared with littermate controls (Ou et al., J Neurosci. 2016 Oct 12;36(41):10560-10573), and also by the finding that a selective GPR17 antagonist enhances remyelination after cuprizone-induced demyelination.

[0006] Myelin is an essential component of a healthy CNS. Impaired myelin formation, myelin damage, and / or impaired myelin repair can cause or be a secondary consequence of certain diseases. One example of a disease primarily resulting from damage to myelin is multiple sclerosis (MS). While the cause of MS is unknown, it affects approximately 400,000 people in the United States and approximately 2.5 million people worldwide, and is approximately three times more likely to occur in women than men. MS is an inflammatory autoimmune disease resulting from an immune attack directed at oligodendrocytes, resulting in myelin damage and ultimately loss of neuronal axons. The direct result is a collection of acute symptoms, such as difficulty moving, speaking, swallowing, dizziness, and fatigue. Symptoms may also include problems with vision, hearing, or balance. The disease can take several forms. One form is associated with relapses and remissions in which acute symptoms resolve over time; this form is called relapsing-remitting multiple sclerosis (RRMS). Another form of the disease, primary progressive MS (PPMS), is characterized by an inability to resolve symptoms between attacks and is considered a more severe form of the disease. In most forms of MS, there is a progressive accumulation of non-resolving symptoms, which leads to an increased burden of disability. Several treatments for MS have received regulatory approval. These treatments affect the frequency of relapses but are far less effective at preventing disability progression. It has been proposed that compounds that promote OPC differentiation, and thus the formation of new oligodendrocytes, may be effective in treating disability progression in MS by promoting repair processes (Lubetzki et al., Lancet Neurol 2020;19:678-88).

[0007] Several other CNS disorders are associated with myelin dysfunction. Acute injuries, such as ischemic or traumatic brain injury, result in damage to myelin (Lecca et al., PLoS One. 2008;3(10):e3579; Shi et al., Exp Neurol. 2015 Oct;272:17-25). Many myelin defects result from genetic mutations or toxin exposure (Duncan and Radcliff, Exp Neurol. 2016 Sep;283(Pt B):452-75). In other diseases, such as Alzheimer's disease, brain volume loss associated with disease progression is partially due to loss of oligodendrocytes and myelin (Chacon de la Rocha et al., Front Cell Neurosci. 2020 Dec 3;14:575-82). Less obvious forms of myelin dysfunction may be associated with disorders such as schizophrenia and autism, where the inability to form fully mature myelin may contribute to the cause or symptoms of the disease (Marie et al., PNAS August 28, 2018, 115(35)E8246-E8255; McPhie et al., Translational Psychiatry 2018.8:230). In each of these cases, promoting the formation of mature, fully functional myelin may have important therapeutic effects. Thus, as a key regulator of OPC maturation, GPR17 antagonists may be beneficial for the treatment of a wide range of disorders.

[0008] There is no known causal treatment or cure for multiple sclerosis or many other myelin disorders. Treatment is typically symptomatic, addressing the inflammatory component of the disease in an effort to improve function after attacks and prevent new attacks. Such immunomodulatory drugs are usually only moderately effective, especially in advanced disease, but can have side effects and be poorly tolerated. Furthermore, most available drugs, such as beta-interferon, glatiramer acetate, or therapeutic antibodies, are only available in injectable form and / or address only the inflammatory component of the disease, not demyelination directly. Other drugs, such as corticosteroids, exhibit relatively nonspecific anti-inflammatory and immunosuppressive effects and therefore can result in chronic side effects, such as those seen in Cushing's syndrome.

[0009] There is a clear need for safe and effective drugs, preferably suitable for oral administration, for the treatment of GPR17-mediated diseases, such as myelinating diseases like MS. Ideally, such drugs would reverse the demyelination process by reducing demyelination and / or promoting remyelination of affected neurons. Chemical compounds that effectively reduce GPR17 receptor activity could meet these requirements.

[0010] Therefore, there is a need for GPR17 modulators, preferably negative GPR17 modulators, that can effectively reduce GPR17 activity. Summary of the Invention

[0011] The present invention is based on the unexpected discovery that a novel class of pyrrolyl-sulfonamide compounds, described below, are negative regulators of GPR17.

[0012] In particular, in a first aspect, the present invention provides a compound of formula (I) as defined in the accompanying claims and specification: [ka] (In the formula, R1 is aryl, heteroaryl, cycloalkyl, cycloalkenyl, cycloalkynyl, heterocyclyl and A 1 -X 1 -, and R 2 is selected from the group comprising hydrogen, halo, cyano, alkyl, alkenyl, alkynyl, haloalkyl, haloalkenyl, haloalkynyl, alkoxy, alkenyloxy, alkynyloxy, alkylthio, alkenylthio, alkynylthio, haloalkoxy, alkoxyalkyl, mono- or di(alkyl)amino, and mono- or di(alkyl)aminoalkyl; R 1 The above aryl, heteroaryl, cycloalkyl, cycloalkenyl, cycloalkynyl, heterocyclyl, X 1 and A 1 Each of may be unsubstituted or may contain one or more Z 1 may be substituted with X 1 -Y 1b -Y 1a -Y 1c - in which Y 1a is a single bond, double bond or triple bond, or -CR 1a =CR 1a -, -C≡C-, -CO-, -O-, -CS-, -S-, -SO2-, -SO-, -SO(NH)-, -CONR 1b -, -NR 1b CO-, -SO2NR 1b -, -NR 1b SO2-, -S(O)-NR 1b - and -NR 1b - selected from the group comprising Y 1b and Y 1c Each of the is a single bond, or C 1~3 Alkylene, C 2~3 Alkenylene, C 2~3 alkynylene, wherein C is independently selected from the group consisting of 1~3 Alkylene, C 2~3 Alkenylene, C 2~3 Each alkynylene may be unsubstituted or may contain one or more R1a where Y 1a is a single bond, a double bond, or a triple bond, Y 1b and Y 1c At least one of the is not a single bond, Each R 1a are independently selected from the group including hydrogen, oxo, thioxo, halo, hydroxy, haloalkyl, alkoxy, alkoxyalkyl, haloalkoxy, haloalkoxyalkyl, mono- or di(alkyl)amino, mono- or di(alkyl)aminoalkyl, and alkyl; A 1 is selected from the group comprising aryl, heteroaryl, cycloalkyl, cycloalkenyl, cycloalkynyl and heterocyclyl; each Z 1are independently selected from halo, cyano, oxo, nitro, thioxo, or hydroxy, thio, alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkylalkyl, cycloalkenyl, cycloalkynyl, cycloalkenylalkyl, cycloalkynylalkyl, aryl, arylalkyl, haloalkyl, haloalkenyl, haloalkynyl, cyanoalkyl, alkoxy, alkenyloxy, alkynyloxy, cyanoalkoxy, alkylthio, alkenylthio, alkynylthio, haloalkoxy, hydroxyalkyl, alkoxyalkyl, cycloalkyloxy, cycloalkylalkoxy, alkoxyalkoxy, carboxyl, alkoxycarbonyl, alkylcarbonyl, arylalkoxy, amino, mono- or di(alkyl)amino, aminoalkyl, mono- or di(alkyl)aminoalkyl, mono- or di(alkyl)aminocarbonyl, heterocyclyl, heteroaryl, heterocyclylalkyl, heteroarylalkyl, arylalkenyl, arylalkynyl, haloalkenyloxy, haloalkynyloxy, hydroxyalkenyl, hydroxyalkoxy alkenyl, alkenyloxyalkyl, alkynyloxyalkyl, alkoxyalkenyl, alkoxyalkynyl, alkenyloxyalkoxy, alkynyloxyalkoxy, alkenyloxycarbonyl, alkynyloxycarbonyl, alkenylcarbonyl, alkynylcarbonyl, aminoalkenyl, aminoalkynyl, mono- or di(alkyl)aminoalkenyl, mono- or di(alkyl)aminoalkynyl, heterocyclylalkenyl, heterocyclylalkynyl, heteroarylalkenyl, heteroarylalkynyl, aryloxy, Aryloxyalkyl, aryloxyalkenyl, aryloxyalkynyl, arylthio, haloalkylthio, cycloalkylthio, alkylsulfinyl, alkylsulfonyl, cycloalkylsulfinyl, cycloalkylsulfonyl, arylsulfinyl, arylsulfonyl, mono- or di(alkyl)aminosulfonyl, mono- or di(alkyl)aminosulfinyl, alkoxycarbonylamino, alkenyloxycarbonylamino, alkynyloxycarbonylamino, alkylcarbonylamino, alkenylcarbonylamino,Alkynylcarbonylamino, cycloalkylcarbonylamino, arylcarbonylamino, cycloalkylcarbonyl, arylcarbonyl, mono- or di(alkyl)aminocarbonyl, alkylcarbonyloxy, alkenylcarbonyloxy, alkynylcarbonyloxy, sulfonyl, sulfinyl, mono- or di(alkyl)aminoalkylamino, mono- or di(alkyl)aminoalkoxy, arylamino, arylaminoalkyl, alkylcarbonyloxyalkyl, alkenylcarbonyloxyalkyl, alkynylcarbonyloxyalkyl, arylcarbonyloxy, arylcarbonyl and R is independently selected from heteroaryloxyalkyl, arylaminocarbonyl, heterocyclyloxy, heteroaryloxy, heteroarylthio, heteroaryloxyalkyl, heteroaryloxyalkenyl, heteroaryloxyalkynyl, heteroarylsulfinyl, heteroarylsulfonyl, heteroarylamino, heteroarylaminoalkyl, heteroarylcarbonylamino, heteroarylcarbonyl, heteroarylcarbonyloxy, heteroarylcarbonyloxyalkyl, and heteroarylaminocarbonyl, each of the foregoing groups may be unsubstituted or may contain one or more Z, 1a may be substituted with and / or two Zs 1 can be taken together with the atom(s) to which they are attached to form an aryl, cycloalkyl, heteroaryl, or heterocyclyl, each of which may be unsubstituted or may be substituted with one or more Z 1a may be substituted with and / or one R 1a is one Z 1 and together with the atom(s) to which they are attached can form a cycloalkyl, a 4- to 10-membered saturated or partially saturated heterocyclyl, a 5- to 10-membered heteroaryl, or an aryl, each of which can be unsubstituted or can be substituted with one or more Z 1a may be substituted with R1b is hydrogen or alkyl, or R 1b is one Z 1 and together with the atom(s) to which they are attached can form a 4- to 10-membered saturated or partially saturated heterocyclyl or a 5- to 10-membered heteroaryl, each of which can be unsubstituted or can be substituted with one or more Z 1a may be substituted with each Z 1a is independently selected from the group comprising halo, cyano, hydroxyl, alkyl, alkenyl, alkynyl, haloalkyl, haloalkenyl, haloalkynyl, alkoxy, alkenyloxy, alkynyloxy, alkylthio, alkenylthio, alkynylthio, haloalkoxy, hydroxyalkyl, alkoxyalkyl, cycloalkyl, cycloalkenyl, cycloalkynyl, cycloalkyloxy, aryl, arylalkyl, amino, mono- or di(alkyl)amino, mono- or di(alkyl)aminoalkyl, and oxo; or R 1 is selected from the group comprising hydrogen, halo, cyano, alkyl, alkenyl, alkynyl, haloalkyl, haloalkenyl, haloalkynyl, alkoxy, alkenyloxy, alkynyloxy, alkylthio, alkenylthio, alkynylthio, haloalkoxy, alkoxyalkyl, mono- or di(alkyl)amino, and mono- or di(alkyl)aminoalkyl; R 2 is aryl, heteroaryl, cycloalkyl, cycloalkenyl, cycloalkynyl, heterocyclyl and A 2 -X 2 - selected from the group comprising R 2 The above aryl, heteroaryl, cycloalkyl, cycloalkenyl, cycloalkynyl, heterocyclyl, X 2 and A 2 Each of may be unsubstituted or may contain one or more Z 2 may be substituted with X 2 -Y 2b -Y 2a -Y 2c- in which Y 2a is a single bond, double bond or triple bond, or -CR 2a =CR 2a -, -C≡C-, -CO-, -O-, -CS-, -S-, -SO2-, -SO-, -SO(NH)-, -CONR 2b -, -NR 2b CO-, -SO2NR 2b -, -NR 2b SO2-, -S(O)-NR 2b - and -NR 2b - selected from the group comprising Y 2b and Y 2c Each of the is a single bond, or C 1~3 Alkylene, C 2~3 Alkenylene, C 2~3 alkynylene, wherein C is independently selected from the group consisting of 1~3 Alkylene, C 2~3 Alkenylene, C 2~3 Each alkynylene may be unsubstituted or may contain one or more R 2a where Y 2a is a single bond, a double bond, or a triple bond, Y 2b and Y 2c At least one of the is not a single bond, Each R 2a are independently selected from the group including hydrogen, oxo, thioxo, halo, hydroxy, haloalkyl, alkoxy, alkoxyalkyl, haloalkoxy, haloalkoxyalkyl, mono- or di(alkyl)amino, mono- or di(alkyl)aminoalkyl, and alkyl; A 2 is selected from the group comprising aryl, heteroaryl, cycloalkyl, cycloalkenyl, cycloalkynyl and heterocyclyl; each Z 2are independently selected from halo, cyano, oxo, nitro, thioxo, or hydroxy, thio, alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkylalkyl, cycloalkenyl, cycloalkynyl, cycloalkenylalkyl, cycloalkynylalkyl, aryl, arylalkyl, arylalkenyl, arylalkynyl, haloalkyl, haloalkenyl, haloalkynyl, cyanoalkyl, alkoxy, alkenyloxy, alkynyloxy, cyanoalkoxy, alkylthio, alkenylthio, alkynylthio O, haloalkoxy, haloalkenyloxy, haloalkynyloxy, hydroxyalkyl, hydroxyalkenyl, hydroxyalkynyl, alkoxyalkyl, alkenyloxyalkyl, alkynyloxyalkyl, alkoxyalkenyl, alkynyl, cycloalkyloxy, cycloalkylalkoxy, alkoxyalkoxy, alkenyloxyalkoxy, alkynyloxyalkoxy, carboxyl, alkoxycarbonyl, alkenyloxycarbonyl, alkynyloxycarbonyl, alkylcarbonyl, alkenylcarbonyl nyl, alkynylcarbonyl, arylalkoxy, amino, mono- or di(alkyl)amino, aminoalkyl, aminoalkenyl, aminoalkynyl, mono- or di(alkyl)aminoalkyl, mono- or di(alkyl)aminoalkenyl, mono- or di(alkyl)aminoalkynyl, mono- or di(alkyl)aminocarbonyl, heterocyclyl, heteroaryl, heterocyclylalkyl, heteroarylalkyl, heterocyclylalkenyl, heterocyclylalkynyl, heteroarylalkenyl, heteroarylalkynyl, aryloxy, aryloxyalkyl, aryloxyalkenyl, aryloxyalkynyl, arylthio, haloalkylthio, cycloalkylthio, alkylsulfinyl, alkylsulfonyl, cycloalkylsulfinyl, cycloalkylsulfonyl, arylsulfinyl, arylsulfonyl, mono- or di(alkyl)aminosulfonyl, mono- or di(alkyl)aminosulfinyl, alkoxycarbonylamino, alkenyloxycarbonylamino, alkynyloxycarbonylamino, alkylcarbonylamino, alkenylcarbonylamino,Alkynylcarbonylamino, cycloalkylcarbonylamino, arylcarbonylamino, cycloalkylcarbonyl, arylcarbonyl, mono- or di(alkyl)aminocarbonyl, alkylcarbonyloxy, alkenylcarbonyloxy, alkynylcarbonyloxy, arylcarbonyloxy, sulfonyl, sulfinyl, mono- or di(alkyl)aminoalkylamino, mono- or di(alkyl)aminoalkoxy, arylamino, arylaminoalkyl, alkylcarbonyloxyalkyl, alkenylcarbonyloxyalkyl, alkynylcarbonyloxyalkyl, arylcarbonyloxy, aryl and R is independently selected from the group comprising heteroarylcarbonyloxyalkyl, arylaminocarbonyl, heterocyclyloxy, heteroaryloxy, heteroarylthio, heteroaryloxyalkyl, heteroaryloxyalkenyl, heteroaryloxyalkynyl, heteroarylsulfinyl, heteroarylsulfonyl, heteroarylamino, heteroarylaminoalkyl, heteroarylcarbonylamino, heteroarylcarbonyl, heteroarylcarbonyloxy, heteroarylcarbonyloxyalkyl and heteroarylaminocarbonyl, each of the foregoing groups may be unsubstituted or may contain one or more Z, 2a may be substituted with and / or two Zs 2 can be taken together with the atom(s) to which they are attached to form an aryl, cycloalkyl, heteroaryl, or heterocyclyl, each of which may be unsubstituted or may be substituted with one or more Z 2a may be substituted with and / or one R 2a is one Z 2 and together with the atom(s) to which they are attached can form a cycloalkyl, a 4- to 10-membered saturated or partially saturated heterocyclyl, a 5- to 10-membered heteroaryl, or an aryl, each of which can be unsubstituted or can be substituted with one or more Z 2a may be substituted with R 2b is hydrogen or alkyl, or R 2b is one Z 2 and together with the atom(s) to which they are attached can form a 4- to 10-membered saturated or partially saturated heterocyclyl or a 5- to 10-membered heteroaryl, each of which can be unsubstituted or can be substituted with one or more Z 2a may be substituted with each Z 2a is independently selected from the group comprising halo, cyano, hydroxyl, alkyl, alkenyl, alkynyl, haloalkyl, haloalkenyl, haloalkynyl, alkoxy, alkenyloxy, alkynyloxy, alkylthio, alkenylthio, alkynylthio, haloalkoxy, hydroxyalkyl, alkoxyalkyl, cycloalkyl, cycloalkenyl, cycloalkynyl, cycloalkyloxy, aryl, arylalkyl, amino, mono- or di(alkyl)amino, mono- or di(alkyl)aminoalkyl, and oxo; R 3 is selected from the group comprising hydrogen, halo, cyano, alkyl, alkenyl, alkynyl, haloalkyl, haloalkenyl, haloalkynyl, alkoxy, alkenyloxy, alkynyloxy, alkylthio, alkenylthio, alkynylthio, haloalkoxy, alkoxyalkyl, mono- or di(alkyl)amino, and mono- or di(alkyl)aminoalkyl; R 4 is aryl or heteroaryl, and each of the aryl and heteroaryl groups may be one or more Z 4 is replaced by each Z 4are independently selected from halo, cyano, oxo, nitro, thioxo, or hydroxy, thio, alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkylalkyl, cycloalkenyl, cycloalkynyl, cycloalkenylalkyl, cycloalkynylalkyl, aryl, arylalkyl, arylalkenyl, arylalkynyl, haloalkyl, haloalkenyl, haloalkynyl, cyanoalkyl, alkoxy, alkenyloxy, alkynyloxy, cyanoalkoxy, alkylthio, alkenylthio, alkynylthio O, haloalkoxy, haloalkenyloxy, haloalkynyloxy, hydroxyalkyl, hydroxyalkenyl, hydroxyalkynyl, alkoxyalkyl, alkenyloxyalkyl, alkynyloxyalkyl, alkoxyalkenyl, alkynyl, cycloalkyloxy, cycloalkylalkoxy, alkoxyalkoxy, alkenyloxyalkoxy, alkynyloxyalkoxy, carboxyl, alkoxycarbonyl, alkenyloxycarbonyl, alkynyloxycarbonyl, alkylcarbonyl, alkenylcarbonyl nyl, alkynylcarbonyl, arylalkoxy, amino, mono- or di(alkyl)amino, aminoalkyl, aminoalkenyl, aminoalkynyl, mono- or di(alkyl)aminoalkyl, mono- or di(alkyl)aminoalkenyl, mono- or di(alkyl)aminoalkynyl, mono- or di(alkyl)aminocarbonyl, heterocyclyl, heteroaryl, heterocyclylalkyl, heteroarylalkyl, heterocyclylalkenyl, heterocyclylalkynyl, heteroarylalkenyl, heteroarylalkynyl, aryloxy, aryloxyalkyl, aryloxyalkenyl, aryloxyalkynyl, arylthio, haloalkylthio, cycloalkylthio, alkylsulfinyl, alkylsulfonyl, cycloalkylsulfinyl, cycloalkylsulfonyl, arylsulfinyl, arylsulfonyl, mono- or di(alkyl)aminosulfonyl, mono- or di(alkyl)aminosulfinyl, alkoxycarbonylamino, alkenyloxycarbonylamino, alkynyloxycarbonylamino, alkylcarbonylamino, alkenylcarbonylamino,Alkynylcarbonylamino, cycloalkylcarbonylamino, arylcarbonylamino, cycloalkylcarbonyl, arylcarbonyl, mono- or di(alkyl)aminocarbonyl, alkylcarbonyloxy, alkenylcarbonyloxy, alkynylcarbonyloxy, arylcarbonyloxy, sulfonyl, sulfinyl, mono- or di(alkyl)aminoalkylamino, mono- or di(alkyl)aminoalkoxy, arylamino, arylaminoalkyl, alkylcarbonyloxyalkyl, alkenylcarbonyloxyalkyl, alkynylcarbonyloxyalkyl, arylcarbonyloxy, aryl and R is independently selected from the group comprising heteroarylcarbonyloxyalkyl, arylaminocarbonyl, heterocyclyloxy, heteroaryloxy, heteroarylthio, heteroaryloxyalkyl, heteroaryloxyalkenyl, heteroaryloxyalkynyl, heteroarylsulfinyl, heteroarylsulfonyl, heteroarylamino, heteroarylaminoalkyl, heteroarylcarbonylamino, heteroarylcarbonyl, heteroarylcarbonyloxy, heteroarylcarbonyloxyalkyl and heteroarylaminocarbonyl, each of the foregoing groups may be unsubstituted or may contain one or more Z, 4a may be substituted with and / or two Zs 4 can be taken together with the atom(s) to which they are attached to form an aryl, cycloalkyl, heteroaryl, or heterocyclyl, each of which may be unsubstituted or may contain one or more Z 4a may be substituted with each Z 4ais independently selected from the group comprising halo, cyano, hydroxyl, alkyl, alkenyl, alkynyl, haloalkyl, haloalkenyl, haloalkynyl, alkoxy, alkenyloxy, alkynyloxy, alkylthio, alkenylthio, alkynylthio, haloalkoxy, hydroxyalkyl, alkoxyalkyl, cycloalkyl, cycloalkenyl, cycloalkynyl, cycloalkyloxy, aryl, arylalkyl, amino, mono- or di(alkyl)amino, mono- or di(alkyl)aminoalkyl, and oxo; however, R 1 A 1 -X 1 - and X 1 is -CO- and A 1 When is heterocyclyl, A 1 is connected to X via the N ring atom of the heterocyclyl 1 is not bound to R 1 When is heteroaryl, R 1 is not oxadiazolyl, R 2 A 2 -X 2 - and X 2 is -CO- and A 2 When is heterocyclyl, A 2 is connected to X via the N ring atom of the heterocyclyl 2 is not bound to R 2 When is heteroaryl, R 2 is not oxadiazolyl, However, the above compound is N,4-bis(4-methylphenyl)-1H-pyrrole-3-sulfonamide; (CAS number 1427286-05-2), N,4-bis(4-chlorophenyl)-1H-pyrrole-3-sulfonamide (not CAS number 1427286-06-3)), or an isomer (such as a tautomer or stereoisomer), hydrate, solvate, polymorph, prodrug, isotope, or co-crystal thereof, or a pharmaceutically acceptable salt thereof.

[0013] In a second aspect, the present invention also provides a pharmaceutical composition comprising a pharmaceutically acceptable carrier and an effective amount of a compound according to the first aspect of the present invention, or a pharmaceutically acceptable salt thereof, as an active ingredient.

[0014] The present invention also encompasses a compound according to the invention or a pharmaceutical composition according to the invention for use as a medicament. The present invention also encompasses a compound according to the invention or a pharmaceutical composition according to the invention for use in the prevention and / or treatment of a GPR17-mediated disorder in a subject or patient in need thereof, preferably an animal, for example a mammal such as a human in need thereof.

[0015] The present invention also relates to methods for the treatment and / or prevention of GPR17-mediated disorders in a subject or patient in need thereof by administering one or more of the compounds, optionally in combination with one or more other pharmaceutical agents, to a subject or patient in need thereof.

[0016] These and other characteristics, features and advantages of the present invention will become apparent from the following detailed description, which illustrates, by way of example, the principles of the invention.

[0017] When describing the present invention, the terms used should be construed in accordance with the following definitions, unless the context dictates otherwise.

[0018] Unless otherwise defined, all terms, including technical and scientific terms, used in disclosing the present invention have the meanings commonly understood by those skilled in the art to which this invention belongs. As a further guide, definitions of the terms used herein are included to better understand the teachings of the present invention. When describing the compounds, processes, methods and uses of the present invention, the terms used should be construed in accordance with the following definitions, unless the context dictates otherwise.

[0019] As used herein, the singular forms "a," "an," and "the" include both singular and plural referents unless the context clearly dictates otherwise. By way of example, "a compound" means one compound or more than one compound.

[0020] In the following sections, different aspects of the invention are defined in more detail. Each aspect so defined can be combined with any other aspect, unless expressly indicated otherwise. In particular, any feature indicated as being preferred or advantageous can be combined with any other feature indicated as being preferred or advantageous.

[0021] As used herein, the terms "comprising," "including," and "comprising" are synonymous with "comprising," "comprises," or "containing," and are inclusive or open-ended and do not exclude additional, unrecited members, elements, or method steps. The terms "comprising," "including," and "comprising" also include the term "consisting of."

[0022] The recitation of numerical ranges using endpoints includes all integers and, where appropriate, fractions subsumed within that range (e.g., 1 to 5, when referring to, for example, the number of elements, can include 1, 2, 3, and 4; when referring to, for example, measurements, can include 1.5, 2, 2.75, and 3.80). The recitation of endpoints also includes the endpoint values ​​themselves (e.g., 1.0 to 5.0 includes both 1.0 and 5.0). Any numerical range recited herein is intended to include all subranges subsumed therein.

[0023] References throughout this specification to "one embodiment" or "an embodiment" mean that a particular feature, structure, or characteristic described in connection with that embodiment is included in at least one embodiment of the present invention. Thus, appearances of the phrase "in one embodiment" or "in an embodiment" in various places throughout this specification do not necessarily all refer to the same embodiment, although they may. Furthermore, particular features, structures, or characteristics may be combined in any suitable manner in one or more embodiments, as would be apparent to one of ordinary skill in the art from this disclosure. Furthermore, although some embodiments described herein include some features and not other features included in other embodiments, combinations of features from different embodiments are within the scope of the present invention and are meant to form different embodiments, as would be understood by one of ordinary skill in the art. For example, in the following claims and specification, any of the embodiments may be used in any combination.

[0024] The term "leaving group" or "LG" as used herein means a chemical group that is susceptible to displacement by a nucleophile or to cleavage or hydrolysis under basic or acidic conditions. In certain embodiments, the leaving group is selected from a halogen atom (e.g., Cl, Br, I) or a sulfonate (e.g., mesylate, tosylate, triflate).

[0025] The term "protecting group" refers to a moiety of a compound that masks or alters the properties of a functional group or the overall compound. The chemical substructure of protecting groups varies widely. One function of protecting groups is to serve as intermediates in the synthesis of the parent drug substance. Chemical protecting groups and strategies for protection / deprotection are well known in the art. See "Protective Groups in Organic Chemistry," Theodora W. Greene (John Wiley & Sons, Inc., New York, 1991). Protecting groups are often utilized to mask the reactivity of particular functional groups to facilitate the efficiency of desired chemical reactions, e.g., forming and breaking chemical bonds in an orderly and planned manner. Protection of a compound's functional group alters other physical properties besides the reactivity of the protected functional group, such as polarity, lipophilicity (hydrophobicity), and other properties that can be measured by common analytical tools. Chemically protected intermediates may themselves be biologically active or inactive.

[0026] Protected compounds may also exhibit altered, and in some cases optimized, properties in vitro and in vivo, such as passage through cell membranes and resistance to enzymatic degradation or sequestration. In this role, protected compounds with intended therapeutic effects are sometimes called prodrugs. Another function of a protecting group is to convert a parent drug into a prodrug, whereby the parent drug is released upon conversion of the prodrug in vivo. Because an active prodrug may be absorbed more effectively than the parent drug, the prodrug may have greater potency in vivo than the parent drug. Protecting groups are removed in vitro in the case of chemical intermediates, or in vivo in the case of prodrugs. For chemical intermediates, it is not particularly important that the product obtained after deprotection, such as an alcohol, is physiologically acceptable, although it is generally more desirable that the product be pharmacologically harmless.

[0027] Whenever the term "substituted" is used herein, it is meant to indicate that one or more hydrogen atoms on the atom designated by the expression "substituted" are replaced with one selected from the designated group, provided that the replacement does not exceed the normal valence of the designated atom, and that the substitution results in a chemically stable compound, i.e., a compound that is sufficiently robust to survive isolation from a reaction mixture.

[0028] The term "halo" or "halogen" as a group or part of a group is generic to fluoro, chloro, bromo, and iodo.

[0029] As used herein, the term "cyano" refers to a -CN group.

[0030] As used herein, the term "oxo" refers to the group ═O.

[0031] As used herein, the term "nitro" refers to the group --NO.sub.2.

[0032] As used herein, the term "thioxo" refers to the group ═S.

[0033] The term "hydroxyl" or "hydroxy" as used herein refers to an --OH group.

[0034] The term "thio" or "thiol" as used herein refers to a -SH group.

[0035] The term “alkyl” as a group or part of a group refers to a group of formula C n H 2n+1where n is a number equal to or greater than 1 and there are no sites of unsaturation. The alkyl groups may be straight or branched chain and may be substituted as indicated herein. Generally, alkyl groups of the present invention contain 1 to 18 carbon atoms, preferably 1 to 10 carbon atoms, more preferably 1 to 6 carbon atoms, and more preferably 1 to 4 carbon atoms. When a subscript is used herein following a carbon atom, the subscript refers to the number of carbon atoms the specified group may contain. For example, "C" as a group or part of a group 1~6 The term "alkyl" refers to a group of the formula C n H 2n+1 where n is a number ranging from 1 to 6. Thus, for example, "C 1~6 "Alkyl" includes all straight or branched chain alkyl groups having 1 to 6 carbon atoms, and thus includes methyl, ethyl, n-propyl, i-propyl, butyl and its isomers (e.g., n-butyl, i-butyl, and t-butyl), pentyl and its isomers, hexyl and its isomers, etc. For example, C 1~4 Alkyl includes all straight or branched alkyl groups having 1 to 4 carbon atoms, and thus includes, for example, methyl, ethyl, n-propyl, i-propyl, 2-methyl-ethyl, butyl and its isomers (e.g., n-butyl, i-butyl and t-butyl), etc. In certain embodiments, the term alkyl includes C 1~12 Alkyl (C 1~12 hydrocarbons), and more specifically C 1~9 Alkyl (C 1~9 hydrocarbons), and more particularly, C 1~6 Alkyl (C 1~6 Non-limiting examples of alkyl include methyl, ethyl, 1-propyl (n-propyl), 2-propyl (iPr), 1-butyl, 2-methyl-1-propyl ( i-Bu), 2-butyl (s-Bu), 2-dimethyl-2-propyl (t-Bu), 1-pentyl (n-pentyl), 2-pentyl, 3-pentyl, 2-methyl-2-butyl, 3-methyl-2-butyl, 3-methyl-1-butyl, 2-methyl-1-butyl, 1-hexyl, 2-hexyl, 3-hexyl, 2-methyl-2-pentyl, 3-methyl-2-pentyl, 4-methyl-2-pentyl , 3-methyl-3-pentyl, 2-methyl-3-pentyl, 2,3-dimethyl-2-butyl, 3,3-dimethyl-2-butyl, n-heptyl, n-octyl, n-nonyl, n-decyl, n-undecyl, n-dodecyl, n-tridecyl, n-tetradecyl, n-pentadecyl, n-hexadecyl, n-heptadecyl, n-octadecyl, n-nonadecyl, and n-icosyl.

[0036] When the suffix "ene" is used in conjunction with an alkyl group (i.e., "alkylene"), it is intended to mean an alkyl group, as defined herein, having two single bonds as points of attachment to other groups. As used herein by itself or as part of another substituent, the term "alkylene," also known as "alkanediyl," refers to a divalent alkyl group, i.e., an alkyl group having two monovalent radical centers derived by removing two hydrogen atoms from the same carbon atom or two different carbon atoms of a parent alkane, i.e., having two single bonds for attachment to two other groups. Alkylene groups may be straight or branched chain and may be substituted as indicated herein. Non-limiting examples of alkylene groups include methylene (-CH2-), ethylene (-CH2-CH2-), methylmethylene (-CH(CH3)-), 1-methyl-ethylene (-CH(CH3)-CH2-), n-propylene (-CH2-CH2-CH2-), 2-methylpropylene (-CH2-CH(CH3)-CH2-), 3-methylpropylene (-CH2-CH2-CH(CH3)-), n-butylene (-CH2-CH2-CH2-CH2-), 2-methylbutylene (-CH2-CH(CH3)-CH2-CH2-), 4-methylbutylene (-CH2-CH2-CH2-CH(CH3)-), pentylene and chain isomers, and hexylene and chain isomers.

[0037] The term "hydrocarbyl" group is used herein according to the definition given below by IUPAC: a univalent group formed by removing a hydrogen atom from a hydrocarbon (i.e., a group containing only carbon and hydrogen).

[0038] The term "alkenyl" as a group or part of a group refers to an alkenyl group having at least one site of unsaturation (usually 1 to 3, preferably 1), i.e., at least one sp 2 Carbon-sp 2 "C" refers to an unsaturated hydrocarbyl group that may be linear or branched and contains one or more carbon-carbon double bonds. Generally, the alkenyl groups of the present invention contain 2 to 20 carbon atoms, preferably 2 to 10 carbon atoms, preferably 2 to 8 carbon atoms, and more preferably 2 to 6 carbon atoms. When a subscript following a carbon atom is used herein, the subscript refers to the number of carbon atoms that the designated group may contain. 2~6 Examples of alkenyl groups are ethenyl, 2-propenyl, 2-butenyl, 3-butenyl, 2-pentenyl and its isomers, 2-hexenyl and its isomers, 2,4-pentadienyl, etc. The double bond may be in either the cis or trans configuration.

[0039] When the suffix "ene" is used in conjunction with an alkenyl group (i.e., "alkenylene"), it is intended to mean an alkenyl group, as defined herein, having two single bonds as points of attachment to other groups. As used herein by itself or as part of another substituent, the term "alkenylene" refers to a divalent alkenyl group, i.e., an alkenyl group having two monovalent centers derived by the removal of two hydrogen atoms from the same carbon atom or two different carbon atoms of a parent alkene, i.e., having two single bonds for attachment to two other groups. Alkenylene groups may be straight or branched chain and may be substituted as set forth herein. Non-limiting examples of alkenylene groups include -CH=CH-, -C(CH3)=CH-, -C(CH3)=C(CH3)-, -CH=CH-CH2-, -CH2-C(CH3)=CH-, -CH2-CH=C(CH3)-, -CH2-CH2-CH=CH-, and the like.

[0040] The term "alkynyl" as a group or part of a group means an alkynyl group having at least one site of unsaturation (usually 1 to 3, preferably 1), i.e., sp 1 Carbon-sp 1 It refers to a branched or straight chain hydrocarbon containing a carbon-carbon triple bond. In certain embodiments, the term alkynyl refers to at least one site of unsaturation (usually 1 to 3, preferably 1), i.e., at least one sp 1 Carbon-sp 1 C as defined in more detail hereinabove, having a carbon-carbon triple bond 2~12 Alkynyl (C 2~12 hydrocarbons), preferably C 2~9 Alkynyl (C 2~9 hydrocarbons), even more preferably C 2~6 Alkynyl (C 2~6 Examples of alkynyl include, but are not limited to, ethynyl (-C≡CH), 3-ethyl-cyclohept-1-ynylene, and 1-propynyl (propargyl, -CHC≡CH).

[0041] When the suffix "ene" is used in conjunction with an alkynyl group, i.e., "alkynylene," it is intended to mean an alkynyl group, as defined herein, having two single bonds as points of attachment to other groups. As used herein by itself or as part of another substituent, the term "alkynylene" refers to a divalent alkynyl group, i.e., an alkynyl group having two single bonds for attachment to two other groups. Alkynylene groups may be straight or branched chain and may be substituted as set forth herein. Non-limiting examples of alkynylene groups include -C≡C-, -CH2-C≡C-, -C≡C-CH2-, -CH2-CH2-C≡C-, and the like.

[0042] The term "cycloalkyl" as a group or part of a group refers to a cyclic alkyl group that is a monovalent saturated hydrocarbyl group having one or more ring structures and containing 3 to 20 carbon atoms, more preferably 3 to 10 carbon atoms, more preferably 3 to 8 carbon atoms, more preferably 3 to 6 carbon atoms. Cycloalkyl includes all saturated hydrocarbon groups containing one or more rings, such as monocyclic, bicyclic, or tricyclic groups. For example, cycloalkyl includes C 3~10 Monocyclic or C 7~18 Polycyclic saturated hydrocarbons include, for example, cyclopropyl, cyclobutyl, cyclopentyl, cyclopropylethylene, methylcyclopropylene, cyclohexyl, cycloheptyl, cyclooctyl, cyclooctylmethylene, norbornyl, fenchyl, trimethyltricycloheptyl, decalinyl, adamantyl, and the like. The additional rings of polycyclic cycloalkyls may be fused, bridged, and / or linked through one or more spiro atoms. When a subscript following a carbon atom is used herein, the subscript refers to the number of carbon atoms the specified group may contain. For example, "C 3~10 The term "cycloalkyl" refers to a cyclic alkyl group containing from 3 to 10 carbon atoms. For example, "C 3~8 The term "cycloalkyl" refers to a cyclic alkyl group containing 3 to 8 carbon atoms. For example, "C 3~6The term "cycloalkyl" refers to a cyclic alkyl group containing from 3 to 6 carbon atoms. For the avoidance of doubt, a fused system of a heterocyclic ring and a cycloalkyl ring is considered to be heterocyclic regardless of the ring attached to the core structure. A fused system of an aryl ring and a cycloalkyl ring is considered to be aryl regardless of the ring attached to the core structure. A fused system of a heteroaryl ring and a cycloalkyl ring is considered to be heteroaryl regardless of the ring attached to the core structure.

[0043] The term "cycloalkenyl" as a group or part of a group means an alkenyl group having at least one site of unsaturation (usually 1 to 3, preferably 1), i.e., sp 2 Carbon-sp 2 It refers to a non-aromatic cyclic alkenyl group having a carbon-carbon double bond and preferably having 4 to 18 carbon atoms, more preferably 4 to 10 carbon atoms, and more preferably 5 to 6 carbon atoms. Cycloalkenyl includes all unsaturated hydrocarbon groups containing one or more rings, including monocyclic, bicyclic, or tricyclic groups. For example, cycloalkenyl includes C 4~10 Monocyclic or C 7~18 Polycyclic hydrocarbons may be included. The additional rings may be fused, bridged, and / or linked through one or more spiro atoms. When a subscript is used herein following a carbon atom, the subscript refers to the number of carbon atoms the specified group may contain. For example, "C 5~10 The term "cycloalkenyl" refers to a cyclic alkenyl group containing from 5 to 10 carbon atoms. For example, "C 5~8 The term "cycloalkenyl" refers to a cyclic alkenyl group containing 5 to 8 carbon atoms. For example, "C 5~6The term "cycloalkyl" refers to a cyclic alkenyl group containing 5 to 6 carbon atoms. Examples include, but are not limited to, cyclobutenyl, cyclopentenyl (-CH), cyclopentenylpropylene, methylcyclohexenylene, and cyclohexenyl (-CH). The double bond may be in a cis or trans configuration. For the avoidance of doubt, a fused system of a heterocyclic ring and a cycloalkenyl ring will be considered heterocyclic, regardless of the ring attached to the core structure. A fused system of an aryl ring and a cycloalkenyl ring will be considered aryl, regardless of the ring attached to the core structure. A fused system of a heteroaryl ring and a cycloalkenyl ring will be considered heteroaryl, regardless of the ring attached to the core structure.

[0044] The term "cycloalkynyl" as a group or part of a group preferably refers to cycloalkynyl groups having from 5 to 18 carbon atoms and at least one site of unsaturation (usually 1 to 3, preferably 1), i.e., sp 1 Carbon-sp 1 It has a carbon-carbon triple bond, C 5~10 Monocyclic or C 7~18 It refers to a non-aromatic hydrocarbon group consisting of or containing a polycyclic hydrocarbon. Examples include, but are not limited to, cyclohept-1-yne, 3-ethyl-cyclohept-1-ynylene, 4-cyclohept-1-yne-methylene, and ethylene-cyclohept-1-yne. In certain embodiments, the term cycloalkynyl refers to at least one site of unsaturation (usually 1 to 3, preferably 1), i.e., sp 1 Carbon-sp 1 C as defined in more detail hereinabove, having a carbon-carbon triple bond 5~10 Cycloalkynyl (cyclic C 5~10 hydrocarbons), preferably C 5~9 Cycloalkynyl (cyclic C 5~9 hydrocarbons), even more preferably C 5~6 Cycloalkynyl (cyclic C 5~6For the avoidance of doubt, a fused system of heterocyclic and cycloalkynyl rings is considered to be heterocyclic, regardless of the ring attached to the core structure. A fused system of aryl and cycloalkynyl rings is considered to be aryl, regardless of the ring attached to the core structure. A fused system of heteroaryl and cycloalkynyl rings is considered to be heteroaryl, regardless of the ring attached to the core structure.

[0045] The term “cycloalkylalkyl” or “cycloalkyl-alkyl” as a group or part of a group refers to a group of the formula —R a -R g (In the formula, R g is cycloalkyl and R a is alkylene as defined herein.

[0046] The term “cycloalkenylalkyl” or “cycloalkenyl-alkyl” as a group or part of a group refers to a group of the formula —R a -R t (In the formula, R t is cycloalkenyl and R a is alkylene as defined herein.

[0047] The term “cycloalkynylalkyl” or “cycloalkynyl-alkyl” as a group or part of a group refers to a group of the formula —R a -R s (In the formula, R s is cycloalkynyl and R a is alkylene as defined herein.

[0048] The term "alkoxy" or "alkyloxy" as a group or part of a group refers to a group of the formula -OR b (In the formula, R b is alkyl as defined herein. 1~6 Non-limiting examples of alkoxy include methoxy, ethoxy, propoxy, isopropoxy, butoxy, isobutoxy, sec-butoxy, tert-butoxy, pentyloxy, and hexyloxy.

[0049] The term "alkenyloxy" as a group or part of a group refers to an alkenyl group of the formula -OR d (In the formula, R d is alkenyl as defined herein).

[0050] The term "alkynyloxy" as a group or part of a group refers to a group of the formula -OR e (In the formula, R e is alkynyl as defined herein.

[0051] The term “alkoxyalkyl” or “alkyloxyalkyl” as a group or part of a group refers to a group of the formula —R a -OR b (In the formula, R a is alkylene and R b is alkyl as defined herein.

[0052] The term “alkenyloxyalkyl” as a group or part of a group refers to an alkenyl group of the formula —R a -OR d (In the formula, R a is alkylene and R d is alkenyl as defined herein).

[0053] The term “alkynyloxyalkyl” as a group or part of a group refers to a group of the formula —R a -OR c (In the formula, R a is alkylene and R c is alkynyl as defined herein.

[0054] The term “alkoxyalkenyl” or “alkyloxyalkenyl” as a group or part of a group refers to an alkyl group of the formula —R h -OR b (In the formula, R h is alkenylene, and R b is alkyl as defined herein.

[0055] The term “alkoxyalkynyl” or “alkynyloxyalkynyl” as a group or part of a group refers to a group of the formula —R i -OR b (In the formula, R i is alkynylene and R b is alkyl as defined herein.

[0056] The term “cyanoalkyl” as a group or part of a group refers to a group of the formula —R a -CN(wherein, R a is alkylene as defined herein.

[0057] The term "cyanoalkoxy" or "cyanoalkyloxy" as a group or part of a group refers to a group of the formula -OR a -CN(wherein, R a is alkylene as defined herein.

[0058] The term "cycloalkoxy" as a group or part of a group refers to a group of the formula -OR g (In the formula, R g is cycloalkyl as defined herein.

[0059] The term "cycloalkylalkoxy" as a group or part of a group refers to a group of the formula -OR a -R g (In the formula, R a is alkylene and R g is cycloalkyl as defined herein.

[0060] The term "alkoxyalkoxy" or "alkyloxyalkyloxy" as a group or part of a group refers to a group of the formula -OR a -OR b (In the formula, R a is alkylene and R b is alkyl as defined herein.

[0061] The term "alkenyloxyalkoxy" or "alkenyloxyalkyloxy" as a group or part of a group refers to an alkenyl group of the formula -OR a -OR d (In the formula, R a is alkylene and R d is alkenyl as defined herein).

[0062] The term "alkynyloxyalkoxy" or "alkynyloxyalkyloxy" as a group or part of a group refers to an alkyl group of the formula -OR a -OR c (In the formula, R a is alkylene and R c is alkynyl as defined herein.

[0063] The term "aryl" as a group or part of a group refers to a polyunsaturated aromatic hydrocarbyl group having a single ring (i.e., phenyl) or multiple aromatic rings fused together (e.g., naphthyl) or covalently bonded together, typically containing 6 to 20, preferably 6 to 10, atoms, in which at least one ring is aromatic. Typical aryl groups include, but are not limited to, one ring derived from benzene, naphthalene, anthracene, biphenyl, etc., or two or three rings fused together. The aromatic ring may contain one to two additional rings. A fused system of a cycloalkyl ring, or a cycloalkenyl ring, or a cycloalkynyl ring with an aryl ring is considered aryl, regardless of the ring attached to the core structure. A fused system of a heterocyclic ring with an aryl ring is considered heterocyclic, regardless of the ring attached to the core structure. A fused system of a heteroaryl ring with an aryl ring is considered heteroaryl, regardless of the ring attached to the core structure. Examples of suitable aryls include C 6~20 Aryl, preferably C 6~10 Aryl, more preferably C 6~9Non-limiting examples of aryl include phenyl, biphenylyl, biphenylenyl, or 1- or 2-naphthalenyl, 1-, 2-, 3-, 4-, 5-, or 6-tetralinyl (also known as "1,2,3,4-tetrahydronaphthalene"), 1-, 2-, 3-, 4-, 5-, 6-, 7-, or 8-azulenyl, 4-, 5-, 6-, or 7-indenyl, 4- or 5-indanyl, 5-, 6-, 7-, or 8-tetrahydronaphthyl, 1,2,3,4-tetrahydronaphthyl, and 1,4-dihydronaphthyl, 1-, 2-, 3-, 4-, or 5-pyrenyl.

[0064] The term "arylalkyl" as a group or part of a group refers to an alkyl, as defined herein, in which at least one hydrogen atom is replaced with at least one aryl, as defined herein. Non-limiting examples of arylalkyl groups include benzyl, phenethyl, dibenzylmethyl, benzyl, 2-phenylethan-1-yl, 2-phenylethen-1-yl, naphthylmethyl, 2-naphthylethyl, and the like. 6~10 Aryl C 1~6 The term "alkyl" means that the alkyl portion of the arylalkyl group can contain 1 to 6 carbon atoms and the aryl portion is 6 to 10 carbon atoms.

[0065] The term "arylalkenyl" as a group or part of a group refers to an alkenyl in which one of the hydrogen atoms bonded to a carbon atom is replaced with an aryl. 6~10 Aryl C 2~6 The term "alkenyl" means that the alkenyl portion of the arylalkenyl group can contain 2 to 6 carbon atoms and the aryl portion can contain 6 to 10 carbon atoms.

[0066] The term "arylalkynyl" as a group or part of a group refers to an alkynyl in which one of the hydrogen atoms bonded to a carbon atom has been replaced with an aryl. 6~10 Aryl C 2~6The term "alkynyl" means that the alkenyl portion of the arylalkynyl group can contain 2 to 6 carbon atoms and the aryl portion can contain 6 to 10 carbon atoms.

[0067] The term "aryloxy" as a group or part of a group refers to a group of the formula -OR f (In the formula, R f is aryl as defined herein.

[0068] The term "arylalkoxy" or "arylalkyloxy" as a group or part of a group refers to an alkyl group of the formula -OR a -R f (In the formula, R f is aryl and R a is alkylene as defined herein.

[0069] The term “aryloxyalkyl” as a group or part of a group refers to a group of the formula —R a -OR f (In the formula, R f is aryl and R a is alkylene as defined herein.

[0070] The term “aryloxyalkenyl” as a group or part of a group refers to an alkyl group of the formula —R h -OR f (In the formula, R f is aryl and R h is alkenylene as defined herein).

[0071] The term “aryloxyalkynyl” as a group or part of a group refers to an aryloxyalkynyl group of the formula —R i -OR f (In the formula, R f is aryl and R i is alkynylene as defined herein.

[0072] The term "arylthio" as a group or part of a group refers to a group of the formula -SR f (In the formula, R fis aryl as defined herein.

[0073] The term "haloalkyl" as a group or part of a group refers to an alkyl group having the meaning defined herein, in which one or more hydrogen atoms have been replaced with a halogen, as defined herein. Non-limiting examples of such haloalkyl groups include chloromethyl, 1-bromoethyl, fluoromethyl, difluoromethyl, trifluoromethyl, 1,1,1-trifluoroethyl, and the like.

[0074] The term "haloalkenyl" as a group or part of a group refers to an alkenyl group having the meaning defined herein, in which one or more hydrogen atoms have been replaced with a halogen, each as defined herein.

[0075] The term "haloalkynyl" as a group or part of a group refers to an alkynyl group having the meaning defined herein, in which one or more hydrogen atoms have been replaced with a halogen, each as defined herein.

[0076] The term "alkylthio" as a group or part of a group refers to a group of the formula -SR b (In the formula, R b is alkyl as defined herein. Non-limiting examples of alkylthio groups include methylthio (-SCH), ethylthio (-SCHCH), n-propylthio, isopropylthio, n-butylthio, isobutylthio, sec-butylthio, tert-butylthio, and the like.

[0077] The term "alkenylthio" as a group or part of a group refers to a group of the formula -SR d (In the formula, R d is alkenyl as defined herein).

[0078] The term "alkynylthio" as a group or part of a group refers to a group of the formula -SR c (In the formula, R c is alkynyl as defined herein.

[0079] The term "haloalkylthio" as a group or part of a group refers to a group of the formula -SR e (In the formula, R e is haloalkyl as defined herein.

[0080] The term "cycloalkylthio" as a group or part of a group refers to a group of the formula -SR g (In the formula, R g is cycloalkyl as defined herein.

[0081] The term "haloalkoxy" as a group or part of a group means a group of the formula -OR e (In the formula, R e is haloalkyl as defined herein. Non-limiting examples of suitable haloalkoxy include fluoromethoxy, difluoromethoxy, trifluoromethoxy, 2,2,2-trifluoroethoxy, 1,1,2,2-tetrafluoroethoxy, 2-fluoroethoxy, 2-chloroethoxy, 2,2-difluoroethoxy, 2,2,2-trichloroethoxy, trichloromethoxy, 2-bromoethoxy, pentafluoroethyl, 3,3,3-trichloropropoxy, and 4,4,4-trichlorobutoxy.

[0082] The term "haloalkenyloxy" as a group or part of a group means a group of the formula -OR j (In the formula, R j is haloalkenyl as defined herein.

[0083] The term "haloalkynyloxy" as a group or part of a group means a group of the formula -OR k (In the formula, R k is haloalkynyl as defined herein.

[0084] The term “hydroxyalkyl” as a group or part of a group refers to a group of the formula —R a -OH(in the formula, R a is alkylene as defined herein.

[0085] The term “hydroxyalkenyl” as a group or part of a group refers to a group of the formula —R h -OH(in the formula, R h is alkenylene as defined herein).

[0086] The term “hydroxyalkynyl” as a group or part of a group refers to a group of the formula —R i -OH(in the formula, R i is alkynylene as defined herein.

[0087] The term "carboxy", "carboxyl" or "hydroxycarbonyl" as a group or part of a group refers to the group -C(=O)-OH.

[0088] The term "carbonyl" as a group or part of a group refers to the group -C(=O)-, also written as -CO-.

[0089] The term "alkoxycarbonyl" or "alkyloxycarbonyl" as a group or part of a group means a group of the formula -C(=O)-OR b (In the formula, R b is alkyl as defined herein.

[0090] The term "alkenyloxycarbonyl" as a group or part of a group refers to an alkenyl group of the formula -C(=O)-OR d (In the formula, R d is alkenyl as defined herein).

[0091] The term "alkynyloxycarbonyl" as a group or part of a group refers to a group of the formula -C(=O)-OR c (In the formula, R c is alkynyl as defined herein.

[0092] The term "alkylcarbonyl" as a group or part of a group refers to a group of the formula -C(=O)-R b (In the formula, R bis alkyl as defined herein.

[0093] The term "alkenylcarbonyl" as a group or part of a group refers to an alkenyl group of the formula -C(=O)-R d (In the formula, R d is alkenyl as defined herein).

[0094] The term "alkynylcarbonyl" as a group or part of a group refers to a group of the formula -C(=O)-R c (In the formula, R c is alkynyl as defined herein.

[0095] The term "cycloalkylcarbonyl" as a group or part of a group refers to a group of the formula -C(=O)-R g (In the formula, R g is cycloalkyl as defined herein.

[0096] The term "arylcarbonyl" as a group or part of a group refers to a group of the formula -C(=O)-R f (In the formula, R f is aryl as defined herein.

[0097] The term "amino" as a group or part of a group refers to the group --NH.sub.2.

[0098] The term “mono- or di-alkylamino” as a group or part of a group refers to a group of the formula —N(R l )(R b )(wherein, R l is hydrogen or alkyl, and R bis alkyl as defined herein. Thus, such terms include monoalkylamino groups (e.g., mono-alkylamino groups such as methylamino and ethylamino) and dialkylamino groups (e.g., di-alkylamino groups such as dimethylamino and diethylamino). Non-limiting examples of suitable mono- or di-alkylamino groups include n-propylamino, isopropylamino, n-butylamino, i-butylamino, sec-butylamino, t-butylamino, pentylamino, n-hexylamino, di-n-propylamino, di-i-propylamino, ethylmethylamino, methyl-n-propylamino, methyl-i-propylamino, n-butylmethylamino, i-butylmethylamino, t-butylmethylamino, ethyl-n-propylamino, ethyl-i-propylamino, n-butylethylamino, i-butylethylamino, t-butylethylamino, di-n-butylamino, di-i-butylamino, methylpentylamino, methylhexylamino, ethylpentylamino, ethylhexylamino, propylpentylamino, propylhexylamino, and the like.

[0099] The term “aminoalkyl” as a group or part of a group refers to a group of the formula —R a -NH2(wherein, R a is alkylene as defined herein.

[0100] The term “aminoalkenyl” as a group or part of a group refers to an aminoalkenyl group of the formula —R h -NH2(wherein, R h is alkenylene as defined herein).

[0101] The term “aminoalkynyl” as a group or part of a group refers to a group of the formula —R i -NH2(wherein, R i is alkynylene as defined herein.

[0102] The term “mono- or di(alkyl)aminoalkyl” as a group or part of a group refers to a group of the formula —R a -N(Rl )(R b )(wherein, R a is alkylene and R l is hydrogen or alkyl, and R b is alkyl as defined herein.

[0103] The term “mono- or di(alkyl)aminoalkenyl” as a group or part of a group refers to a group of the formula —R h -N(R l )(R b )(wherein, R h is alkenylene, and R l is hydrogen or alkyl, and R b is alkyl as defined herein.

[0104] The term “mono- or di(alkyl)aminoalkynyl” as a group or part of a group refers to a group of the formula —R i -N(R l )(R b )(wherein, R i is alkynylene and R l is hydrogen or alkyl, and R b is alkyl as defined herein.

[0105] The term “mono- or di(alkyl)aminocarbonyl” as a group or part of a group refers to a group of the formula —C(═O)—N(R l )(R b )(wherein, R l is hydrogen or alkyl, and R b is alkyl as defined herein.

[0106] The terms "heterocycle" or "heterocyclyl," as used herein, refer to a non-aromatic fully saturated or partially unsaturated ring system containing 3 to 18 atoms, preferably 3 to 14 atoms (3- to 14-membered heterocyclyl) (e.g., 3- to 7-membered monocyclic, 7- to 14-membered bicyclic), including at least one N, O, S, or P, and preferably a total of 3 to 10 ring atoms (3- to 10-membered heterocyclyl), more preferably 4 to 10 atoms (4- to 10-membered heterocyclyl), and even more preferably 5 to 10 atoms (5- to 10-membered heterocyclyl). Each ring of the heterocycle or heterocyclyl may have 1, 2, 3, or 4 heteroatoms selected from N, O, P, and / or S, wherein the N and S heteroatoms may optionally be oxidized, the N heteroatom may optionally be quaternized, and at least one carbon atom of the heterocyclyl may be oxidized to form at least one C=O. A heterocyclyl may be attached to any heteroatom or carbon atom of the ring or ring system, valence permitting. The rings of a polycyclic heterocyclyl or heterocycle may be fused, bridged, and / or linked through one or more spiro atoms. A fused system of an aryl ring and a heterocycle or heterocyclyl is considered a heterocycle or heterocyclyl, regardless of the ring attached to the core structure. A fused system of a heteroaryl ring and a heterocycle or heterocyclyl is considered a heteroaryl, regardless of the ring attached to the core structure.

[0107] Non-limiting exemplary heterocycles or heterocyclic groups include piperidinyl, piperazinyl, homopiperazinyl, morpholinyl, tetrahydropyranyl, tetrahydrofuranyl, pyrrolidinyl, aziridinyl, oxiranyl, thiiranyl, azetidinyl, oxetanyl, thietanyl, imidazolinyl, pyrazolidinylimidazolidinyl, oxazolinyl, isoxazolinyl, oxazolidinyl, isoxazolidinyl, thiazolidinyl, isothiazolidinyl, succinimidyl, indolinyl, isoindolinyl, chromanyl (3 ,4-dihydrobenzo[b]pyranyl), 2H-pyrrolyl, pyrrolinyl (e.g., 1-pyrrolinyl, 2-pyrrolinyl, 3-pyrrolinyl), 4H-quinolidinyl, 2-oxopiperazinyl, pyrazolinyl (e.g., 2-pyrazolinyl, 3-pyrazolinyl), tetrahydro-2H-pyranyl, 2H-pyranyl, 4H-pyranyl, dihydro-2H-pyranyl, 3-dioxolanyl, 1,4-dioxanyl, 2,5-dioximidazolidinyl, 2-oxopiperidinyl, 2-oxopyrrolodinyl, indolinyl , tetrahydrothiophenyl, tetrahydroquinolinyl, tetrahydroisoquinolin-1-yl, tetrahydroisoquinolin-2-yl, tetrahydroisoquinolin-3-yl, tetrahydroisoquinolin-4-yl, thiomorpholin-4-yl, thiomorpholin-4-yl sulfoxide, thiomorpholin-4-yl sulfone, 1,3-dioxolanyl, 1,4-oxathinyl, 1,4-dithianyl, 1,3,5-trioxanyl, 1H-pyrrolidinyl, tetrahydro-1,1-dioxothiophenyl, N-formyl-piperidine Razinyl, thiomorpholinyl, dihydrofuranyl, dihydrothienyl, tetrahydrothienyl, dihydropyrazolyl, dihydroimidazolyl, isothiazolinyl, thiazolinyl, triazolinyl, triazolidinyl, oxadiazolinyl, oxadiazolidinyl, thiadiazolidinyl, thiadiazolinyl, tetrazolidinyl, dihydro-pyridinyl, tetrahydro-pyridinyl, 1,2,3,6-tetrahydropyridinyl, hexahydro-pyridinyl, dihydro-pyrimidinyl, tetrahydro-pyrimidinyl, 1,4,5,6-Tetrahydropyrimidinyl, dihydro-pyrazinyl, tetrahydro-pyrazinyl, dihydro-pyridazinyl, tetrahydro-pyridazinyl, dihydro-triazinyl, tetrahydro-triazinyl, hexahydro-triazinyl, 1,4-diazepanyl, dihydro-indolyl, indolinyl, tetrahydro-indolyl, dihydro-indazolyl, tetrahydro-indazolyl, dihydro-isoindolyl, dihydro-benzofuranyl, tetrahydro-benzofuranyl, dihydro-benzothienyl, tetrahydro-benzothienyl, dihydro-benzyl Benzoimidazolyl, tetrahydro-benzimidazolyl, dihydro-benzoxazolyl, 2,3-dihydrobenzo[d]oxazolyl, tetrahydro-benzoxazolyl, dihydro-benzoxazinyl, 3,4-dihydro-2H-benzo[b][1,4]oxazinyl, tetrahydro-benzoxazinyl, benzo[1,3]dioxolyl, benzo[1,4]dioxanyl, dihydro-purinyl, tetrahydro-purinyl, dihydro-quinolinyl, 1,2,3,4-tetrahydroquinolinyl, dihydro-isoquinolinyl, 3,4-dihydroisoquinolinyl quinolin-(1H)-yl, tetrahydro-isoquinolinyl, 1,2,3,4-tetrahydroisoquinolinyl, dihydro-quinazolinyl, tetrahydro-quinazolinyl, dihydro-quinoxalinyl, tetrahydro-quinoxalinyl, 1,2,3,4-tetrahydroquinoxalinyl, 2,5-dihydro-1H-pyrrolyl, 4,5-dihydro-1H-imidazolyl, hexahydropyrrolo[3,4-b][1,4]oxazin-(2H)-yl, 3,4-dihydro-2H-pyrido[3,2-b][1,4]oxazinyl, (cis)-octahydrocyclopenta[ c]pyrrolyl, hexahydropyrrolo[3,4-b]pyrrol-(1H)-yl, 5H-pyrrolo[3,4-b]pyridin-(7H)-yl, 5,7-dihydro-6H-pyrrolo[3,4-b]pyridinyl, tetrahydro-1H-pyrrolo[3,4-b]pyridin-(2H,7H,7aH)-yl, hexahydro-1H-pyrrolo[3,4-b]pyridin-(2H)-yl, (octahydro-6H-pyrrolo[3,4-b]pyridinyl, hexahydropyrrolo[1,2-a]pyrazin-(1H)-yl, 3,4,6,7,8,8a-hexahydro-1H-pyrrolo[1,2-a]pyrazinyl, 2,3,4,9-tetrahydro-1H-carbazolyl, 1,2,3,4-tetrahydropyrazino[1,2-a]indolyl, 2,3-dihydro-1H-pyrrolo[1,2-a]indolyl, 1,3-dihydro-2H-isoindolyl, octahydro-2H-isoindolyl, 2,5-diazabicyclo[2.2.1]heptanyl, 2-azabicyclo[2.2.1]heptenyl, 3-azabicyclo[3.1.0]hexanyl, 3,6-diazabicyclo[3.1.0]hexanyl, 5-azaspiro[2.4]heptanyl, 4,7-diazaspiro[2.5]o octanyl, 2,6-diazaspiro[3.3]heptanyl, 2,5-diazaspiro[3.4]octanyl, 2,6-diazaspiro[3.4]octanyl, 2,7-diazaspiro[3.5]nonanyl, 2,7-diazaspiro[4.4]nonanyl, 2-azaspiro[4.5]decanyl, 2,8-diazaspiro[4.5]decanyl, 3,6-diazabicyclo[3.2.1]octyl, 1,4-dihydroindeno[1,2-c]pyrazolyl, dihydropyranyl, dihydropyridinyl, dihydroquinolinyl, 8H-indazolino[1,2-d]thiazolyl, tetrahydroimidazo[1,Examples include 2-a]pyridinyl, pyridin-2(1H)-one, and 8-azabicyclo[3.2.1]oct-2-enyl. As used herein, the term "aziridinyl" includes aziridin-1-yl and aziridin-2-yl. As used herein, the term "oxiranyl" includes oxiranyl-2-yl. As used herein, the term "thiiranyl" includes thiiran-2-yl. As used herein, the term "azetidinyl" includes azetidin-1-yl, azetidin-2-yl, and azetidin-3-yl. As used herein, the term "oxetanyl" includes oxetan-2-yl and oxetan-3-yl. As used herein, the term "thietanyl" includes thietan-2-yl and thietan-3-yl. As used herein, the term "pyrrolidinyl" includes pyrrolidin-1-yl, pyrrolidin-2-yl, and pyrrolidin-3-yl. As used herein, the term "tetrahydrofuranyl" includes tetrahydrofuran-2-yl and tetrahydrofuran-3-yl. As used herein, the term "tetrahydrothiophenyl" includes tetrahydrothiophen-2-yl and tetrahydrothiophen-3-yl. As used herein, the term "succinimidyl" includes succinimide-1-yl and succinimide-3-yl. As used herein, the term "dihydropyrrolyl" includes 2,3-dihydropyrrol-1-yl, 2,3-dihydro-1H-pyrrol-2-yl, 2,3-dihydro-1H-pyrrol-3-yl, 2,5-dihydropyrrol-1-yl, 2,5-dihydro-1H-pyrrol-3-yl, and 2,5-dihydropyrrol-5-yl. As used herein, the term "2H-pyrrolyl" includes 2H-pyrrol-2-yl, 2H-pyrrol-3-yl, 2H-pyrrol-4-yl, and 2H-pyrrol-5-yl. As used herein, the term "3H-pyrrolyl" includes 3H-pyrrol-2-yl, 3H-pyrrol-3-yl, 3H-pyrrol-4-yl, and 3H-pyrrol-5-yl. As used herein, the term "dihydrofuranyl" includes 2,3-dihydrofuran-2-yl, 2,3-dihydrofuran-3-yl, 2,3-dihydrofuran-4-yl, 2,3-dihydrofuran-5-yl, 2,3-dihydrofuran-5-yl, 2,3-dihydrofuran-6-yl, 2,3-dihydrofuran-7-yl, 2,3-dihydrofuran-8-yl, 2,3-dihydrofuran-9-yl, 2,3-dihydrofuran-10-yl, 2,3-dihydrofuran-11-yl, 2,3-dihydrofuran-12-yl, 2,3-dihydrofuran-13-yl, 2,3-dihydrofuran-14-yl, 2,3-dihydrofuran-16-yl, 2,3-dihydrofuran-17-yl, 2,3-dihydrofuran-18-yl, 2,3-dihydrofuran-19-yl, 2,3-dihydrofuran-20-yl, 2,3-dihydrofuran-21-yl, 2,3-dihydrofuran-22-yl, 2,3-dihydrofuran-23-yl, 2,3-dihydrofuran-24-yl, 2,3-dihydrofuran-25-yl, 2,3-dihydrofuran-26-yl, 2,3-dihydrofuran-27-yl, 2,3-dihydrofuran-28-yl, 2,3-dihydrofuran-29-yl, 2,3-dihydrofuran-21-yl, 2,3-diIt includes 3-dihydrofuran-5-yl, 2,5-dihydrofuran-2-yl, 2,5-dihydrofuran-3-yl, 2,5-dihydrofuran-4-yl, and 2,5-dihydrofuran-5-yl. As used herein, the term "dihydrothiophenyl" includes 2,3-dihydrothiophen-2-yl, 2,3-dihydrothiophen-3-yl, 2,3-dihydrothiophen-4-yl, 2,3-dihydrothiophen-5-yl, 2,5-dihydrothiophen-2-yl, 2,5-dihydrothiophen-3-yl, 2,5-dihydrothiophen-4-yl, and 2,5-dihydrothiophen-5-yl. As used herein, the term "imidazolidinyl" includes imidazolidin-1-yl, imidazolidin-2-yl, and imidazolidin-4-yl. The term "pyrazolidinyl" as used herein includes pyrazolidin-1-yl, pyrazolidin-3-yl, and pyrazolidin-4-yl. The term "imidazolinyl" as used herein includes imidazolin-1-yl, imidazolin-2-yl, imidazolin-4-yl, and imidazolin-5-yl. The term "pyrazolinyl" as used herein includes 1-pyrazolin-3-yl, 1-pyrazolin-4-yl, 2-pyrazolin-1-yl, 2-pyrazolin-3-yl, 2-pyrazolin-4-yl, 2-pyrazolin-5-yl, 3-pyrazolin-1-yl, 3-pyrazolin-2-yl, 3-pyrazolin-3-yl, 3-pyrazolin-4-yl, and 3-pyrazolin-5-yl. As used herein, the term "dioxolanyl," also known as "1,3-dioxolanyl," includes dioxolan-2-yl, dioxolan-4-yl, and dioxolan-5-yl.The term "dioxolyl," also known as "3-dioxolyl," includes dioxol-2-yl, dioxol-4-yl, and dioxol-5-yl. The term "oxazolidinyl," as used herein, includes oxazolidin-2-yl, oxazolidin-3-yl, oxazolidin-4-yl, and oxazolidin-5-yl. The term "isoxazolidinyl," as used herein, includes isoxazolidin-2-yl, isoxazolidin-3-yl, isoxazolidin-4-yl, and isoxazolidin-5-yl. The term "oxazolinyl" as used herein includes 2-oxazolinyl-2-yl, 2-oxazolinyl-4-yl, 2-oxazolinyl-5-yl, 3-oxazolinyl-2-yl, 3-oxazolinyl-4-yl, 3-oxazolinyl-5-yl, 4-oxazolinyl-2-yl, 4-oxazolinyl-3-yl, 4-oxazolinyl-4-yl and 4-oxazolinyl-5-yl. The term "isoxazolinyl" as used herein includes 2-isoxazolinyl-3-yl, 2-isoxazolinyl-4-yl, 2-isoxazolinyl-5-yl, 3-isoxazolinyl-3-yl, 3-isoxazolinyl-4-yl, 3-isoxazolinyl-5-yl, 4-isoxazolinyl-2-yl, 4-isoxazolinyl-3-yl, 4-isoxazolinyl-4-yl, and 4-isoxazolinyl-5-yl. The term "thiazolidinyl" as used herein includes thiazolidin-2-yl, thiazolidin-3-yl, thiazolidin-4-yl, and thiazolidin-5-yl. The term "isothiazolidinyl" as used herein includes isothiazolin-2-yl, isothiazolin-3-yl, isothiazolin-4-yl, and isothiazolin-5-yl. The term "thiazolinyl" as used herein includes 2-thiazolinyl-2-yl, 2-thiazolinyl-4-yl, 2-thiazolinyl-5-yl, 3-thiazolinyl-2-yl, 3-thiazolinyl-4-yl, 3-thiazolinyl-5-yl, 4-thiazolinyl-2-yl, 4-thiazolinyl-3,

[0023] As used herein, the term "isothiazolinyl" includes 2-isothiazolinyl-3-yl, 2-isothiazolinyl-4-yl, 2-isothiazolinyl-5-yl, 3-isothiazolinyl-3-yl, 3-isothiazolinyl-4-yl, 3-isothiazolinyl-5-yl, 4-isothiazolinyl-2-yl, 4-isothiazolinyl-3-yl, 4-isothiazolinyl-4-yl, and 4-isothiazolinyl-5-yl. As used herein, the term "piperidyl," also known as "piperidinyl," includes piperid-1-yl, piperid-2-yl, piperid-3-yl, and piperid-4-yl. The term "dihydropyridinyl" as used herein includes 1,2-dihydropyridin-1-yl, 1,2-dihydropyridin-2-yl, 1,2-dihydropyridin-3-yl, 1,2-dihydropyridin-4-yl, 1,2-dihydropyridin-5-yl, 1,2-dihydropyridin-6-yl, 1,4-dihydropyridin-1-yl, 1,4-dihydropyridin-2-yl, 1,4-dihydropyridin-3-yl, 1,4-dihydropyridin-4-yl, 2,3-dihydropyridin-2-yl, 2,3-dihydropyridin-3-yl, and the like. yl, 2,3-dihydropyridin-4-yl, 2,3-dihydropyridin-5-yl, 2,3-dihydropyridin-6-yl, 2,5-dihydropyridin-2-yl, 2,5-dihydropyridin-3-yl, 2,5-dihydropyridin-4-yl, 2,5-dihydropyridin-5-yl, 2,5-dihydropyridin-6-yl, 3,4-dihydropyridin-2-yl, 3,4-dihydropyridin-3-yl, 3,4-dihydropyridin-4-yl, 3,4-dihydropyridin-5-yl and 3,4-dihydropyridin-6-yl.The term "tetrahydropyridinyl" as used herein includes 1,2,3,4-tetrahydropyridin-1-yl, 1,2,3,4-tetrahydropyridin-2-yl, 1,2,3,4-tetrahydropyridin-3-yl, 1,2,3,4-tetrahydropyridin-4-yl, 1,2,3,4-tetrahydropyridin-5-yl, 1,2,3,4-tetrahydropyridin-6-yl, 1,2,3,6-tetrahydropyridin-1-yl, 1,2,3,6-tetrahydropyridin-2-yl, 1,2,3,6-tetrahydropyridin-4-yl, 1,2,3,6-tetrahydropyridin-5-yl, 1,2,3,6-tetrahydropyridin-6 ...6-yl, 1,2,3,6-tetrahydropyridin-6-yl, 1,2,3,6-tetrahydropyridin-6-yl, 1,2,3,6-tetrahydropyridin-6-yl, 1,2,3,6-tetrahydropyridin-6-yl, 1,

[0023] As used herein, the term "tetrahydropyranyl," also known as "oxanyl" or "tetrahydro-2H-pyranyl," includes tetrahydropyran-2-yl, tetrahydropyran-3-yl, and tetrahydropyran-4-yl. As used herein, the term "2H-pyranyl" includes 2H-pyran-2-yl, 2H-pyran-3-yl, 2H-pyran-4-yl, 2H-pyran-5-yl, and 2H-pyran-6-yl. As used herein, the term "4H-pyranyl" includes 4H-pyran-2-yl, 4H-pyran-3-yl, and 4H-pyran-4-yl. As used herein, the term "3,4-dihydro-2H-pyranyl" includes 3,4-dihydro-2H-pyran-2-yl, 3,4-dihydro-2H-pyran-3-yl, 3,4-dihydro-2H-pyran-4-yl, 3,4-dihydro-2H-pyran-5-yl, and 3,4-dihydro-2H-pyran-6-yl.As used herein, the term "3,6-dihydro-2H-pyranyl" includes 3,6-dihydro-2H-pyran-2-yl, 3,6-dihydro-2H-pyran-3-yl, 3,6-dihydro-2H-pyran-4-yl, 3,6-dihydro-2H-pyran-5-yl, and 3,6-dihydro-2H-pyran-6-yl. As used herein, the term "tetrahydrothiophenyl" includes tetrahydrothiophen-2-yl, tetrahydrothiophenyl-3-yl, and tetrahydrothiophenyl-4-yl. As used herein, the term "2H-thiopyranyl" includes 2H-thiopyran-2-yl, 2H-thiopyran-3-yl, 2H-thiopyran-4-yl, 2H-thiopyran-5-yl, and 2H-thiopyran-6-yl. As used herein, the term "4H-thiopyranyl" includes 4H-thiopyran-2-yl, 4H-thiopyran-3-yl, and 4H-thiopyran-4-yl. As used herein, the term "3,4-dihydro-2H-thiopyranyl" includes 3,4-dihydro-2H-thiopyran-2-yl, 3,4-dihydro-2H-thiopyran-3-yl, 3,4-dihydro-2H-thiopyran-4-yl, 3,4-dihydro-2H-thiopyran-5-yl, and 3,4-dihydro-2H-thiopyran-6-yl. As used herein, the term "3,6-dihydro-2H-thiopyranyl" includes 3,6-dihydro-2H-thiopyran-2-yl, 3,6-dihydro-2H-thiopyran-3-yl, 3,6-dihydro-2H-thiopyran-4-yl, 3,6-dihydro-2H-thiopyran-5-yl, and 3,6-dihydro-2H-thiopyran-6-yl. As used herein, the term "piperazinyl," also known as "piperazidinyl," includes piperazin-1-yl and piperazin-2-yl. As used herein, the term "morpholinyl" includes morpholin-2-yl, morpholin-3-yl, and morpholin-4-yl. As used herein, the term "thiomorpholinyl" includes thiomorpholin-2-yl, thiomorpholin-3-yl, and thiomorpholin-4-yl.As used herein, the term "dioxanyl" includes 1,2-dioxan-3-yl, 1,2-dioxan-4-yl, 1,3-dioxan-2-yl, 1,3-dioxan-4-yl, 1,3-dioxan-5-yl, and 1,4-dioxan-2-yl. As used herein, the term "dithianyl" includes 1,2-dithian-3-yl, 1,2-dithian-4-yl, 1,3-dithian-2-yl, 1,3-dithian-4-yl, 1,3-dithian-5-yl, and 1,4-dithian-2-yl. As used herein, the term "oxathianyl" includes oxathian-2-yl and oxathian-3-yl. As used herein, the term "trioxanyl" includes 1,2,3-trioxan-4-yl, 1,2,3-trioxan-5-yl, 1,2,4-trioxan-3-yl, 1,2,4-trioxan-5-yl, 1,2,4-trioxan-6-yl, and 1,3,4-trioxan-2-yl. As used herein, the term "azepanyl" includes azepan-1-yl, azepan-2-yl, azepan-3-yl, and azepan-4-yl. As used herein, the term "homopiperazinyl" includes homopiperazin-1-yl, homopiperazin-2-yl, homopiperazin-3-yl, and homopiperazin-4-yl. The term "indolinyl" as used herein includes indolin-1-yl, indolin-2-yl, indolin-3-yl, indolin-4-yl, indolin-5-yl, indolin-6-yl, and indolin-7-yl. The term "quinolizinyl" as used herein includes quinolizidin-1-yl, quinolizidin-2-yl, quinolizidin-3-yl, and quinolizidin-4-yl. The term "isoindolinyl" as used herein includes isoindolin-1-yl, isoindolin-2-yl, isoindolin-3-yl, isoindolin-4-yl, isoindolin-5-yl, isoindolin-6-yl, and isoindolin-7-yl. The term "3H-indolyl" as used herein includes 3H-indol-2-yl, 3H-indol-3-yl, 3H-indol-4-yl, 3H-indol-5-yl, 3H-indol-6-yl, and 3H-indol-7-yl.As used herein, the term "quinolizinyl" includes quinolizidin-1-yl, quinolizidin-2-yl, quinolizidin-3-yl, and quinolizidin-4-yl. As used herein, the term "quinolizinyl" includes quinolizidin-1-yl, quinolizidin-2-yl, quinolizidin-3-yl, and quinolizidin-4-yl. As used herein, the term "tetrahydroquinolinyl" includes tetrahydroquinolin-1-yl, tetrahydroquinolin-2-yl, tetrahydroquinolin-3-yl, tetrahydroquinolin-4-yl, tetrahydroquinolin-5-yl, tetrahydroquinolin-6-yl, tetrahydroquinolin-7-yl, and tetrahydroquinolin-8-yl. As used herein, the term "tetrahydroisoquinolinyl" includes tetrahydroisoquinolin-1-yl, tetrahydroisoquinolin-2-yl, tetrahydroisoquinolin-3-yl, tetrahydroisoquinolin-4-yl, tetrahydroisoquinolin-5-yl, tetrahydroisoquinolin-6-yl, tetrahydroisoquinolin-7-yl, and tetrahydroisoquinolin-8-yl. As used herein, the term "chromanyl" includes chroman-2-yl, chroman-3-yl, chroman-4-yl, chroman-5-yl, chroman-6-yl, chroman-7-yl, and chroman-8-yl. As used herein, the term "1H-pyrrolidine" includes 1H-pyrrolidin-1-yl, 1H-pyrrolidin-2-yl, 1H-pyrrolidin-3-yl, 1H-pyrrolidin-5-yl, 1H-pyrrolidin-6-yl, and 1H-pyrrolidin-7-yl. The term "3H-pyrrolidine" as used herein includes 3H-pyrrolidin-1-yl, 3H-pyrrolidin-2-yl, 3H-pyrrolidin-3-yl, 3H-pyrrolidin-5-yl, 3H-pyrrolidin-6-yl and 3H-pyrrolidin-7-yl.

[0108] The term "heterocyclylalkyl" or "heterocyclyl-alkyl" as a group or part of a group refers to an alkyl, as defined herein, in which at least one hydrogen atom is replaced with at least one heterocyclyl, as defined herein, and has the formula -R a -Ro (In the formula, R a is alkylene and R o is heterocyclyl as defined herein). 1~6 The term "alkyl" refers to heterocyclyl-alkyl, which is a non-aromatic, fully saturated or partially unsaturated ring system of 3 to 10 atoms, where the alkylene portion contains 1 to 6 carbon atoms and the heterocyclyl portion contains at least one N, O, S, or P.

[0109] The term “heterocyclylalkenyl” or “heterocyclyl-alkenyl” as a group or part of a group refers to an alkenyl, as defined herein, in which at least one hydrogen atom is replaced with at least one heterocyclyl, as defined herein, and has the formula —R h -R o (In the formula, R h is alkylene and R o is heterocyclyl as defined herein). 2~6 The term "alkenyl" refers to a heterocyclyl-alkenyl, which is a non-aromatic fully saturated or partially unsaturated ring system of 3 to 10 atoms, containing at least one N, O, S, or P, and wherein the alkenylene portion contains 2 to 6 carbon atoms and the heterocyclyl portion contains at least one N, O, S, or P.

[0110] The term "heterocyclylalkynyl" or "heterocyclyl-alkynyl" as a group or part of a group refers to an alkynyl, as defined herein, in which at least one hydrogen atom is replaced with at least one heterocyclyl, as defined herein, and has the formula -R i -R o (In the formula, R i is alkylene and R o is heterocyclyl as defined herein). 2~6The term "alkynyl" refers to a heterocyclyl-alkynyl, which is a non-aromatic fully saturated or partially unsaturated ring system of 3 to 10 atoms, containing at least one N, O, S, or P, where the alkynylene portion contains 2 to 6 carbon atoms and the heterocyclyl portion contains at least one N, O, S, or P.

[0111] The term "heteroaryl" refers to an aromatic ring system containing 5 to 18 atoms, including at least one N, O, S, or P, and containing one or two rings that may be fused or covalently bonded together, preferably 5 to 14 atoms (5-14-membered heteroaryl), and even more preferably 5 to 10 atoms (5-10-membered heteroaryl), with each ring typically containing 5 to 6 atoms, wherein at least one of the rings is aromatic, the N and S heteroatoms are optionally oxidized, the N heteroatom is optionally quaternized, and at least one carbon atom of the heteroaryl can be oxidized to form at least one C=O. A fused system of a cycloalkyl ring, or a cycloalkenyl ring, or a cycloalkynyl ring with a heteroaryl ring is considered heteroaryl, regardless of the ring attached to the core structure. A fused system of a heterocycle with a heteroaryl ring is considered heteroaryl, regardless of the ring attached to the core structure. A fused system of an aryl ring with a heteroaryl ring is considered heteroaryl, regardless of the ring attached to the core structure. A fused system of an aryl ring with a heteroaryl ring is considered heteroaryl, regardless of the ring attached to the core structure. Non-limiting examples of such heteroaryls include pyridinyl, pyrrolyl, thiophenyl (also called thienyl), furanyl, thiazolyl, isothiazolyl, thiadiazolyl, triazol-2-yl, 1H-pyrazol-5-yl, pyrazolyl, imidazolyl, oxazolyl, isoxazolyl, triazolyl, oxadiazolyl, tetrazolyl, oxatriazolyl, thiatriazolyl, pyrimidinyl, pyrazinyl, pyridazinyl, oxazinyl, dioxinyl, thiazinyl, triazinyl, pyranyl, thiopyranyl, imidazo[2,1-b][1,3]thiazo aryl, thieno[3,2-b]furanyl, thieno[3,2-b]thiophenyl, thieno[2,3-d][1,3]thiazolyl, thieno[2,3-d]imidazolyl, tetrazolo[1,5-a]pyridinyl, indolyl, indolizinyl, isoindolyl, benzofuranyl, isobenzofuranyl, benzothiophenyl, isobenzothiophenyl, indazolyl, benzimidazolyl, benzoxazolyl, 1,3-benzoxazolyl, 1,2-benzisoxazolyl, 2,1-benzisoxazolyl, 1,3-benzothiazolyl, 1,2-benzisothiazolyl, 2,1-benzisothiazolyl, benzotriazolyl, 1,2,3 benzoxadiazolyl, 2,1,3-benzoxadiazolyl, benzo[c][1,2,5]oxadiazolyl, 1,2,3 benzothiadiazolyl, 2,1,3-benzothiadiazolyl, benzo[d]oxazol-2(3H)-one, 2,3-dihydro-benzofuranyl, thienopyridinyl, purinyl, 9H-purinyl, imidazo[1,2-a]pyridinyl, imidazo[1,2-a]pyrazinyl, imidazo[5,1-a]isoquinolinyl, imidazo[1,5-a]pyridinyl, 6-oxo-pyridazin-1(6H)-yl, 2-oxopyridin-1(2H)-yl, 1,3-benzodioxolyl, Examples include quinolinyl, isoquinolinyl, cinnolinyl, quinazolinyl, quinoxalinyl, acridinyl, phthalazinyl, 1,4-dihydroindeno[1,2-c]-1H-pyrazolyl, 2,3-dihydro-1H-inden-1-one, 2,3-dihydro-1H-indenyl, 3,4-dihydroquinolin-2(1H)-one, 5,6-dihydroimidazo[5,1-a]isoquinolinyl, 8H-indeno[1,2-d]thiazolyl, benzo[d]oxazol-2(3H)-one, quinolin-2(1H)-one, quinazolin-4(1H)-one, quinazolin-2,4(1H,3H)-dione, benzo-[d]oxazolyl, and pyrazolo[1,5-a]pyridinyl.

[0112] As used herein, the term "pyrrolyl" (also called azolyl) includes pyrrol-1-yl, pyrrol-2-yl, and pyrrol-3-yl. As used herein, the term "furyl" includes furan-2-yl and furan-3-yl (also called furan-2-yl and furan-3-yl). As used herein, the term "thienyl" includes thiophen-2-yl and thiophen-3-yl (also called thien-2-yl and thien-3-yl). As used herein, the term "pyrazole" (also called 1H-pyrazolyl, 1,2-diazolyl) includes pyrazol-1-yl, pyrazol-3-yl, or 1H-pyrazol-5-yl, pyrazol-4-yl, and pyrazol-5-yl. As used herein, the term "imidazolyl" includes imidazol-1-yl, imidazol-2-yl, imidazol-4-yl, and imidazol-5-yl. As used herein, the term "oxazolyl" (also referred to as 1,3-oxazolyl) includes oxazol-2-yl, oxazol-4-yl, and oxazol-5-yl. As used herein, the term "isoxazolyl" (also referred to as 1,2-oxazolyl) includes isoxazol-3-yl, isoxazol-4-yl, and isoxazol-5-yl. As used herein, the term "thiazolyl" (also referred to as 1,3-thiazolyl) includes thiazol-2-yl, thiazol-4-yl, and thiazol-5-yl (also referred to as 2-thiazolyl, 4-thiazolyl, 5-thiazolyl). As used herein, the term "isothiazolyl" (also referred to as 1,2-thiazolyl) includes isothiazol-3-yl, isothiazol-4-yl, and isothiazol-5-yl. As used herein, the term "triazolyl" includes triazol-2-yl, 1H-triazolyl, and 4H-1,2,4 triazolyl, and "1H-triazolyl" includes 1H-1,2,3-triazol-1-yl, 1H-1,2,3-triazol-4-yl, 1H-1,2,3-triazol-5-yl, 1H-1,2,4-triazol-1-yl, 1H-1,2,4-triazol-3-yl, and 1H-1,2,4-triazol-5-yl."4H-1,2,4-triazolyl" includes 4H-1,2,4-triazol-4-yl and 4H-1,2,4-triazol-3-yl. As used herein, the term "oxadiazolyl" includes 1,2,3-oxadiazol-4-yl, 1,2,3-oxadiazol-5-yl, 1,2,4-oxadiazol-3-yl, 1,2,4-oxadiazol-5-yl, 1,2,5-oxadiazol-3-yl and 1,3,4-oxadiazol-2-yl. As used herein, the term "thiadiazolyl" includes 1,2,3-thiadiazol-4-yl, 1,2,3-thiadiazol-5-yl, 1,2,4-thiadiazol-3-yl, 1,2,4-thiadiazol-5-yl, 1,2,5-thiadiazol-3-yl (also known as furazan-3-yl), and 1,3,4-thiadiazol-2-yl. As used herein, the term "tetrazolyl" includes 1H-tetrazol-1-yl, 1H-tetrazol-5-yl, 2H-tetrazol-2-yl, and 2H-tetrazol-5-yl. As used herein, the term "oxatriazolyl" includes 1,2,3,4-oxatriazol-5-yl and 1,2,3,5-oxatriazol-4-yl. As used herein, the term "thiatriazolyl" includes 1,2,3,4-thiatriazol-5-yl and 1,2,3,5-thiatriazol-4-yl. As used herein, the term "pyridyl" includes pyridin-2-yl, pyridin-3-yl, and pyridin-4-yl (also referred to as 2-pyridyl, 3-pyridyl, and 4-pyridyl). As used herein, the term "pyrimidyl" includes pyrimid-2-yl, pyrimid-4-yl, pyrimid-5-yl, and pyrimid-6-yl. As used herein, the term "pyrazinyl" includes pyrazin-2-yl and pyrazin-3-yl. As used herein, the term "pyridazinyl" includes pyridazin-3-yl and pyridazin-4-yl. As used herein, the term (also referred to as "1,4-oxazinyl") includes 1,4-oxazin-4-yl and 1,4-oxazin-5-yl.As used herein, the term "dioxinyl" (also referred to as "1,4-dioxinyl") includes 1,4-dioxin-2-yl and 1,4-dioxin-3-yl. As used herein, the term "thiazinyl" (also referred to as "1,4-thiazinyl") includes 1,4-thiazin-2-yl, 1,4-thiazin-3-yl, 1,4-thiazin-4-yl, 1,4-thiazin-5-yl, and 1,4-thiazin-6-yl. As used herein, the term "triazinyl" includes 1,3,5-triazin-2-yl, 1,2,4-triazin-3-yl, 1,2,4-triazin-5-yl, 1,2,4-triazin-6-yl, 1,2,3-triazin-4-yl, and 1,2,3-triazin-5-yl. As used herein, the term "imidazo[2,1-b][1,3]thiazolyl" includes imidazo[2,1-b][1,3]thiazo-2-yl, imidazo[2,1-b][1,3]thiazol-3-yl, imidazo[2,1-b][1,3]thiazol-5-yl, and imidazo[2,1-b][1,3]thiazol-6-yl. As used herein, the term "thieno[3,2-b]furanyl" includes thieno[3,2-b]furan-2-yl, thieno[3,2-b]furan-3-yl, thieno[3,2-b]furan-4-yl, and thieno[3,2-b]furan-5-yl. As used herein, the term "thieno[3,2-b]thiophenyl" includes thieno[3,2-b]thien-2-yl, thieno[3,2-b]thien-3-yl, thieno[3,2-b]thien-5-yl, and thieno[3,2-b]thien-6-yl. As used herein, the term "thieno[2,3-d][1,3]thiazolyl" includes thieno[2,3-d][1,3]thiazol-2-yl, thieno[2,3-d][1,3]thiazol-5-yl, and thieno[2,3-d][1,3]thiazol-6-yl. As used herein, the term "thieno[2,3-d]imidazolyl" includes thieno[2,3-d]imidazol-2-yl, thieno[2,3-d]imidazol-4-yl and thieno[2,3-d]imidazol-5-yl.As used herein, the term "tetrazolo[1,5-a]pyridinyl" includes tetrazolo[1,5-a]pyridin-5-yl, tetrazolo[1,5-a]pyridin-6-yl, tetrazolo[1,5-a]pyridin-7-yl, and tetrazolo[1,5-a]pyridin-8-yl. As used herein, the term "indolyl" includes indol-1-yl, indol-2-yl, indol-3-yl, indol-4-yl, indol-5-yl, indol-6-yl, and indol-7-yl. As used herein, the term "indolizinyl" includes indolizin-1-yl, indolizin-2-yl, indolizin-3-yl, indolizin-5-yl, indolizin-6-yl, indolizin-7-yl, and indolizin-8-yl. As used herein, the term "isoindolyl" includes isoindol-1-yl, isoindol-2-yl, isoindol-3-yl, isoindol-4-yl, isoindol-5-yl, isoindol-6-yl, and isoindol-7-yl. As used herein, the term "benzofuranyl" (also called benzo[b]furanyl) includes benzofuran-2-yl, benzofuran-3-yl, benzofuran-4-yl, benzofuran-5-yl, benzofuran-6-yl, and benzofuran-7-yl. As used herein, the term "isobenzofuranyl" (also called benzo[c]furanyl) includes isobenzofuran-1-yl, isobenzofuran-3-yl, isobenzofuran-4-yl, isobenzofuran-5-yl, isobenzofuran-6-yl, and isobenzofuran-7-yl. As used herein, the term "benzothiophenyl" (also known as benzo[b]thienyl) includes 2-benzo[b]thiophenyl, 3-benzo[b]thiophenyl, 4-benzo[b]thiophenyl, 5-benzo[b]thiophenyl, 6-benzo[b]thiophenyl, and 7-benzo[b]thiophenyl (also known as benzothien-2-yl, benzothien-3-yl, benzothien-4-yl, benzothien-5-yl, benzothien-6-yl, benzothien-7-yl).As used herein, the term "isobenzothiophenyl" (also known as benzo[c]thienyl) includes isobenzothien-1-yl, isobenzothien-3-yl, isobenzothien-4-yl, isobenzothien-5-yl, isobenzothien-6-yl, and isobenzothien-7-yl. As used herein, the term "indazolyl" (also known as 1H-indazolyl or 2-azaindolyl) includes 1H-indazol-1-yl, 1H-indazol-3-yl, 1H-indazol-4-yl, 1H-indazol-5-yl, 1H-indazol-6-yl, 1H-indazol-7-yl, 2H-indazol-2-yl, 2H-indazol-3-yl, 2H-indazol-4-yl, 2H-indazol-5-yl, 2H-indazol-6-yl, and 2H-indazol-7-yl. As used herein, the term "benzimidazolyl" includes benzimidazol-1-yl, benzimidazol-2-yl, benzimidazol-4-yl, benzimidazol-5-yl, benzimidazol-6-yl, and benzimidazol-7-yl. As used herein, the term "1,3-benzoxazolyl" includes 1,3-benzoxazol-2-yl, 1,3-benzoxazol-4-yl, 1,3-benzoxazol-5-yl, 1,3-benzoxazol-6-yl, and 1,3-benzoxazol-7-yl. As used herein, the term "1,2-benzisoxazolyl" includes 1,2-benzisoxazol-3-yl, 1,2-benzisoxazol-4-yl, 1,2-benzisoxazol-5-yl, 1,2-benzisoxazol-6-yl, and 1,2-benzisoxazol-7-yl. The term "2,1-benzisoxazolyl" as used herein includes 2,1-benzisoxazol-3-yl, 2,1-benzisoxazol-4-yl, 2,1-benzisoxazol-5-yl, 2,1-benzisoxazol-6-yl and 2,1-benzisoxazol-7-yl.As used herein, the term "1,3-benzothiazolyl" includes 1,3-benzothiazol-2-yl, 1,3-benzothiazol-4-yl, 1,3-benzothiazol-5-yl, 1,3-benzothiazol-6-yl, and 1,3-benzothiazol-7-yl. As used herein, the term "1,2-benzisothiazolyl" includes 1,2-benzisothiazol-3-yl, 1,2-benzisothiazol-4-yl, 1,2-benzisothiazol-5-yl, 1,2-benzisothiazol-6-yl, and 1,2-benzisothiazol-7-yl. As used herein, the term "2,1-benzisothiazolyl" includes 2,1-benzisothiazol-3-yl, 2,1-benzisothiazol-4-yl, 2,1-benzisothiazol-5-yl, 2,1-benzisothiazol-6-yl, and 2,1-benzisothiazol-7-yl. The term "benzotriazolyl" as used herein includes benzotriazol-1-yl, benzotriazol-4-yl, benzotriazol-5-yl, benzotriazol-6-yl, and benzotriazol-7-yl. The term "1,2,3-benzoxadiazolyl" as used herein includes 1,2,3-benzoxadiazol-4-yl, 1,2,3-benzoxadiazol-5-yl, 1,2,3-benzoxadiazol-6-yl, and 1,2,3-benzoxadiazol-7-yl. The term "2,1,3-benzoxadiazolyl" as used herein includes 2,1,3-benzoxadiazol-4-yl, 2,1,3-benzoxadiazol-5-yl, 2,1,3-benzoxadiazol-6-yl, and 2,1,3-benzoxadiazol-7-yl. As used herein, the term "1,2,3-benzothiadiazolyl" includes 1,2,3-benzothiadiazol-4-yl, 1,2,3-benzothiadiazol-5-yl, 1,2,3-benzothiadiazol-6-yl, and 1,2,3-benzothiadiazol-7-yl. As used herein, the term "2,1,3-benzothiadiazolyl" includes 2,1,3-benzothiadiazol-4-yl, 2,1,3-benzothiadiazol-5-yl, 2,1,3-benzothiadiazol-6-yl, and 2,1,3-benzothiadiazol-7-yl. As used herein, the term "thienopyridinyl" includes thieno[2,3-b]pyridinyl, thieno[2,3-c]pyridinyl, thieno[3,2-c]pyridinyl, and thieno[3,2-b]pyridinyl. As used herein, the term "purinyl" includes purin-2-yl, purin-6-yl, purin-7-yl, and purin-8-yl. As used herein, the term "imidazo[1,2-a]pyridinyl" includes imidazo[1,2-a]pyridin-2-yl, imidazo[1,2-a]pyridin-3-yl, imidazo[1,2-a]pyridin-4-yl, imidazo[1,2-a]pyridin-5-yl, imidazo[1,2-a]pyridin-6-yl, and imidazo[1,2-a]pyridin-7-yl.As used herein, the term "1,3-benzodioxolyl" includes 1,3-benzodioxol-4-yl, 1,3-benzodioxol-5-yl, 1,3-benzodioxol-6-yl, and 1,3-benzodioxol-7-yl. As used herein, the term "quinolinyl" includes quinolin-2-yl, quinolin-3-yl, quinolin-4-yl, quinolin-5-yl, quinolin-6-yl, quinolin-7-yl, and quinolin-8-yl. As used herein, the term "isoquinolinyl" includes isoquinolin-1-yl, isoquinolin-3-yl, isoquinolin-4-yl, isoquinolin-5-yl, isoquinolin-6-yl, isoquinolin-7-yl, and isoquinolin-8-yl. As used herein, the term "cinnolinyl" includes cinnolin-3-yl, cinnolin-4-yl, cinnolin-5-yl, cinnolin-6-yl, cinnolin-7-yl, and cinnolin-8-yl. As used herein, the term "quinazolinyl" includes quinazolin-2-yl, quinazolin-4-yl, quinazolin-5-yl, quinazolin-6-yl, quinazolin-7-yl, and quinazolin-8-yl. As used herein, the term "quinoxalinyl" includes quinoxalin-2-yl, quinoxalin-5-yl, and quinoxalin-6-yl.

[0113] Heteroaryl and heterocycle or heterocyclyl as used herein include, by way of example and not limitation, those groups described in Paquette, Leo A., "Principles of Modern Heterocyclic Chemistry" (WA Benjamin, New York, 1968), especially chapters 1, 3, 4, 6, 7, and 9; "The Chemistry of Heterocyclic Compounds, A series of Monographs" (John Wiley & Sons, New York, 1950 to present), especially editions 13, 14, 16, 19, and 28; Katritzky, Alan R., Rees, C. Wand Scriven, E., "Comprehensive Heterocyclic Chemistry" (Pergamon Press, 1996); and J. Am. Chem. Soc. (1960) 82:5566.

[0114] The term "heteroarylalkyl" or "heteroaryl-alkyl" as a group or part of a group refers to an alkyl, as defined herein, in which at least one hydrogen atom is replaced with at least one heteroaryl, as defined herein, and has the formula -R a -R p (In the formula, R a is alkylene and R p is heteroaryl as defined herein). 1~6 The term "alkyl" refers to heteroaryl-alkyl, where the alkylene portion contains 1 to 6 carbon atoms and the heteroaryl portion is an aromatic ring system containing 5 to 10 atoms, including at least one N, O, S, or P atom.

[0115] The term "heteroarylalkenyl" or "heteroaryl-alkenyl" as a group or part of a group refers to heteroaryl groups having at least one hydrogen atom replaced with at least one heteroaryl, as defined herein, and having the formula -R h -R p (In the formula, Rh is alkenylene, and R p "5- to 10-membered heteroaryl-C" refers to an alkenyl, as defined herein, which may be represented by a group of 2~6 The term "alkenyl" refers to heteroaryl-alkenyl, an aromatic ring system in which the alkenylene portion contains 2 to 6 carbon atoms and the heteroaryl portion contains 5 to 10 atoms, including at least one N, O, S, or P atom.

[0116] The term "heteroarylalkynyl" or "heteroaryl-alkynyl" as a group or part of a group refers to a heteroaryl group having at least one hydrogen atom replaced with at least one heteroaryl as defined herein and having the formula -R i -R p (In the formula, R i is alkenylene, and R p "5- to 10-membered heteroaryl-C" refers to an alkynyl group as defined herein, which may be represented by a group of 2~6 The term "alkynyl" refers to heteroaryl-alkynyl, an aromatic ring system in which the alkynylene portion contains 2 to 6 carbon atoms and the heteroaryl portion contains 5 to 10 atoms, including at least one N, O, S, or P atom.

[0117] The term "sulfinyl" as a group or part of a group refers to the group -S(=O)-H, which can also be written -SO-H.

[0118] The term "alkylsulfinyl" as a group or part of a group refers to a group of the formula -S(=O)-R b (In the formula, R b is alkyl as defined herein.

[0119] The term "cycloalkylsulfinyl" as a group or part of a group refers to a group of the formula -S(=O)-R g (In the formula, R g is cycloalkyl as defined herein.

[0120] The term "arylsulfinyl" as a group or part of a group refers to a group of the formula -S(=O)-R f (In the formula, R f is aryl as defined herein.

[0121] The term “mono- or di(alkyl)aminosulfinyl” as a group or part of a group refers to a group of the formula —S(═O)—N(R l )(R b )(wherein, R l is hydrogen or alkyl, and R b is alkyl as defined herein.

[0122] The term "sulfonyl" as a group or part of a group refers to the group -S(=O)2H, which may also be written as -SO2H.

[0123] The term "alkylsulfonyl" as a group or part of a group refers to a group of the formula -S(=O)-R b (In the formula, R b is alkyl as defined herein.

[0124] The term "cycloalkylsulfonyl" as a group or part of a group refers to a group of the formula -S(=O)-R g (In the formula, R g is cycloalkyl as defined herein.

[0125] The term "arylsulfonyl" as a group or part of a group refers to a group of the formula -S(=O)-R f (In the formula, R f is aryl as defined herein.

[0126] The term “mono- or di(alkyl)aminosulfonyl” as a group or part of a group refers to a group of the formula —S(═O)—N(R l )(R b )(wherein, R l is hydrogen or alkyl, and R bis alkyl as defined herein.

[0127] The term “alkoxycarbonylamino” or “alkyloxycarbonylamino” as a group or part of a group refers to a group of the formula —N(R l )-C(=O)-OR b (In the formula, R l is hydrogen or alkyl, and R b is alkyl as defined herein.

[0128] The term “alkenyloxycarbonylamino” as a group or part of a group refers to an alkenyl group of the formula —N(R l )-C(=O)-OR d (wherein R1 is hydrogen or alkyl, and R d is alkenyl as defined herein).

[0129] The term “alkynyloxycarbonylamino” as a group or part of a group refers to a group of the formula —N(R l )-C(=O)-OR c (In the formula, R l is hydrogen or alkyl, and R c is alkynyl as defined herein.

[0130] The term “alkylcarbonylamino” as a group or part of a group refers to a group of the formula —N(R l )-C(=O)-R b (In the formula, R l is hydrogen or alkyl, and R b is alkyl as defined herein.

[0131] The term “alkenylcarbonylamino” as a group or part of a group refers to an alkenyl group of the formula —N(R l )-C(=O)-R d (In the formula, R l is hydrogen or alkyl, and R d is alkenyl as defined herein).

[0132] The term “alkynylcarbonylamino” as a group or part of a group refers to a group of the formula —N(R l )-C(=O)-R c (In the formula, R l is hydrogen or alkyl, and R c is alkynyl as defined herein.

[0133] The term “cycloalkylcarbonylamino” as a group or part of a group refers to a group of the formula —N(R l )-C(=O)-R g (In the formula, R l is hydrogen or alkyl, and R g is cycloalkyl as defined herein.

[0134] The term “arylcarbonylamino” as a group or part of a group refers to a group of the formula —N(R i )-C(=O)-R f (In the formula, R l is hydrogen or alkyl, and R f is aryl as defined herein.

[0135] The term “mono- or di(alkyl)aminocarbonyl” as a group or part of a group refers to a group of the formula —C(═O)—N(R l )(R b )(wherein, R l is hydrogen or alkyl, and R b is alkyl as defined herein.

[0136] The term "alkylcarbonyloxy" as a group or part of a group refers to a group of the formula -OC(=O)-R b (In the formula, R b is alkyl as defined herein.

[0137] The term "alkenylcarbonyloxy" as a group or part of a group refers to an alkenyl group of the formula -OC(=O)-R d (In the formula, R d is alkenyl as defined herein).

[0138] The term "alkynylcarbonyloxy" as a group or part of a group refers to a group of the formula -OC(=O)-R c (In the formula, R c is alkynyl as defined herein.

[0139] The term "cycloalkylcarbonyloxy" as a group or part of a group refers to a group of the formula -OC(=O)-R g (In the formula, R g is cycloalkyl as defined herein.

[0140] The term "arylcarbonyloxy" as a group or part of a group refers to a group of the formula -OC(=O)-R f (In the formula, R f is aryl as defined herein.

[0141] The term “mono- or di(alkyl)aminoalkylamino” as a group or part of a group refers to a group of the formula —N(R l )-R a -N(R l )(R b )(wherein, R a is alkylene and R l is hydrogen or alkyl, and R b is alkyl as defined herein.

[0142] The term "mono- or di(alkyl)aminoalkoxy" as a group or part of a group refers to a group of the formula -OR a -N(R l )(R b )(wherein, R a is alkylene and R l is hydrogen or alkyl, and R b is alkyl as defined herein.

[0143] The term “arylamino” as a group or part of a group refers to a group of the formula —N(R l )(R f )(wherein, R lis hydrogen or alkyl, and R f is aryl as defined herein.

[0144] The term “arylaminoalkyl” as a group or part of a group refers to a group of the formula —R a -N(R l )(R f )(wherein, R a is alkylene and R l is hydrogen or alkyl, and R f is aryl as defined herein.

[0145] The term "alkylcarbonyloxyalkyl" as a group or part of a group refers to a group of the formula -R a -OC(=O)-R b (In the formula, R a is alkylene and R b is alkyl as defined herein.

[0146] The term “alkenylcarbonyloxyalkyl” as a group or part of a group refers to an alkenyl group of the formula —R a -OC(=O)-R d (In the formula, R a is alkylene and R d is alkenyl as defined herein).

[0147] The term “alkynylcarbonyloxyalkyl” as a group or part of a group refers to a group of the formula —R a -OC(=O)-R c (In the formula, R a is alkylene and R c is alkynyl as defined herein.

[0148] The term "arylcarbonyloxy" as a group or part of a group refers to a group of the formula -OC(=O)-R f (wherein, and R f is aryl as defined herein.

[0149] The term “arylcarbonyloxyalkyl” as a group or part of a group refers to a group of the formula —R a -OC(=O)-R f (In the formula, R a is alkylene and R f is aryl as defined herein)

[0150] The term “arylaminocarbonyl” as a group or part of a group refers to an amino group of the formula —C(═O)—N(R l )(R f )(wherein, R l is hydrogen or alkyl, and R f is aryl as defined herein.

[0151] The term "heterocyclyloxy" as a group or part of a group refers to a group of the formula -OR o (In the formula, R o is heterocyclyl as defined herein.

[0152] The term "heteroaryloxy" as a group or part of a group refers to a heteroaryl group of the formula -OR p (In the formula, R p is heteroaryl as defined herein.

[0153] The term "heteroarylthio" as a group or part of a group refers to a heteroaryl group of the formula -SR p (In the formula, R p is heteroaryl as defined herein.

[0154] The term “heteroaryloxyalkyl” as a group or part of a group refers to a heteroaryl group of the formula —R a -OR p (In the formula, R a is alkylene and R p is heteroaryl as defined herein.

[0155] The term “heteroaryloxyalkenyl” as a group or part of a group refers to a heteroaryl group of the formula —R h-OR p (In the formula, R h is alkenylene, and R p is heteroaryl as defined herein.

[0156] The term “heteroaryloxyalkynyl” as a group or part of a group refers to a heteroaryl group of the formula —R i -OR p (In the formula, R i is alkynylene and R p is heteroaryl as defined herein.

[0157] The term "heteroarylsulfinyl" as a group or part of a group refers to a heteroaryl group of the formula -S(=O)-R p (In the formula, R p is heteroaryl as defined herein.

[0158] The term "heteroarylsulfonyl" as a group or part of a group refers to a heteroaryl group of the formula -S(=O)-R p (In the formula, R p is heteroaryl as defined herein.

[0159] The term “heteroarylamino” as a group or part of a group refers to a heteroaryl group of the formula —N(R l )(R p )(wherein, R l is hydrogen or alkyl, and R p is heteroaryl as defined herein.

[0160] The term “heteroarylaminoalkyl” as a group or part of a group refers to a heteroaryl group of the formula —R a -N(R l )(R p )(wherein, R a is alkylene and R l is hydrogen or alkyl, and R p is heteroaryl as defined herein.

[0161] The term “heteroarylcarbonylamino” as a group or part of a group refers to a heteroaryl group of the formula —N(R l )-C(=O)-R p (In the formula, R l is hydrogen or alkyl, and R p is heteroaryl as defined herein.

[0162] The term "heteroarylcarbonyl" as a group or part of a group refers to a heteroaryl group of the formula -C(=O)-R p (In the formula, R p is heteroaryl as defined herein.

[0163] The term "heteroarylcarbonyloxy" as a group or part of a group refers to a heteroaryl group of the formula -OC(=O)-R p (In the formula, R p is heteroaryl as defined herein.

[0164] The term “heteroarylcarbonyloxyalkyl” as a group or part of a group refers to a heteroaryl group of the formula —R a -OC(=O)-R p (In the formula, R a is alkylene and R p is heteroaryl as defined herein.

[0165] The term “heteroarylaminocarbonyl” as a group or part of a group refers to a heteroaryl group of the formula —C(═O)—N(R l )(R p )(wherein, R l is hydrogen or alkyl, and R p is heteroaryl as defined herein.

[0166] The term "single bond," as used herein with respect to linking groups, i.e., in formulas herein where a particular linking group is selected from a single bond, refers to a molecule in which the linking group is absent, and thus refers to a compound having a direct connection via a single bond between the two moieties that are joined by the linking group.

[0167] The term "double bond," as used herein with respect to a linking group, i.e., such that in formulas herein a particular linking group is selected from a single bond, refers to a molecule in which the linking group is absent, and thus refers to a compound having a direct connection via a double bond between the two moieties joined by the linking group.

[0168] The term "triple bond," as used herein with respect to a linking group, i.e., such that in formulas herein a particular linking group is selected from a single bond, refers to a molecule in which the linking group is absent, and thus refers to a compound having a direct connection via a triple bond between the two moieties that are joined by the linking group.

[0169] Substituent designations found at more than one site in a compound of the invention are intended to be independently selected.

[0170] Substituents are optionally designated with or without a bond. Regardless of the designation of a bond, if the substituent is multivalent (based on its position in the referenced structure), then any and all possible orientations of the substituent are intended.

[0171] As used herein, unless otherwise specified, the term "solvate" includes any combination that may be formed with a derivative of the present invention and a suitable inorganic solvent (e.g., hydrate) or organic solvent, including, but not limited to, alcohols, ketones, esters, ethers, nitriles, and the like.

[0172] Preferred descriptions (features) and embodiments of the methods, compositions, and uses of the present invention are set forth herein below. Each description and embodiment of the present invention so defined can be combined with any other description and / or embodiment, unless expressly indicated to the contrary. In particular, any feature indicated as being preferred or advantageous can be combined with any other feature or description indicated as being preferred or advantageous. The present invention is understood herein in particular by any one or any combination of one or more of the following numbered descriptions and embodiments with any other aspect and / or embodiment:

[0173] 1. Formula (I) [ka] R 1 is aryl, heteroaryl, cycloalkyl, cycloalkenyl, cycloalkynyl, heterocyclyl and A 1 -X 1 -, and R 2 is selected from the group comprising hydrogen, halo, cyano, alkyl, alkenyl, alkynyl, haloalkyl, haloalkenyl, haloalkynyl, alkoxy, alkenyloxy, alkynyloxy, alkylthio, alkenylthio, alkynylthio, haloalkoxy, alkoxyalkyl, mono- or di(alkyl)amino, and mono- or di(alkyl)aminoalkyl; R 1 The above aryl, heteroaryl, cycloalkyl, cycloalkenyl, cycloalkynyl, heterocyclyl, X 1 and A 1 Each of may be unsubstituted or may contain one or more Z 1 may be substituted with X 1 -Y 1b -Y 1a -Y 1c - in which Y 1a is a single bond, double bond or triple bond, or -CR 1a =CR 1a-, -C≡C-, -CO-, -O-, -CS-, -S-, -SO2-, -SO-, -SO(NH)-, -CONR 1b -, -NR 1b CO-, -SO2NR 1b -, -NR 1b SO2-, -S(O)-NR 1b - and -NR 1b - selected from the group comprising Y 1b and Y 1c Each of the is a single bond, or C 1~3 Alkylene, C 2~3 Alkenylene, C 2~3 alkynylene, wherein C is independently selected from the group consisting of 1~3 Alkylene, C 2~3 Alkenylene, C 2~3 Each alkynylene may be unsubstituted or may contain one or more R 1a where Y 1a is a single bond, a double bond, or a triple bond, Y 1b and Y 1c At least one of Y 1a is a triple bond or a double bond, Y 1b and Y 1c is not a single bond, C2 alkenylene, or C2 alkynylene, Each R 1a are independently selected from the group including hydrogen, oxo, thioxo, halo, hydroxy, haloalkyl, alkoxy, alkoxyalkyl, haloalkoxy, haloalkoxyalkyl, mono- or di(alkyl)amino, mono- or di(alkyl)aminoalkyl, and alkyl; A 1 is selected from the group comprising aryl, heteroaryl, cycloalkyl, cycloalkenyl, cycloalkynyl and heterocyclyl; each Z 1are independently selected from halo, cyano, oxo, nitro, thioxo, or hydroxy, thio, alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkylalkyl, cycloalkenyl, cycloalkynyl, cycloalkenylalkyl, cycloalkynylalkyl, aryl, arylalkyl, haloalkyl, haloalkenyl, haloalkynyl, cyanoalkyl, alkoxy, alkenyloxy, alkynyloxy, cyanoalkoxy, alkylthio, alkenylthio, alkynylthio, haloalkoxy, hydroxyalkyl, alkoxyalkyl, cycloalkyloxy, cycloalkylalkoxy, alkoxyalkoxy, carboxyl, alkoxycarbonyl, alkylcarbonyl, arylalkoxy, amino, mono- or di(alkyl)amino, aminoalkyl, mono- or di(alkyl)aminoalkyl, mono- or di(alkyl)aminocarbonyl, heterocyclyl, heteroaryl, heterocyclylalkyl, heteroarylalkyl, arylalkenyl, arylalkynyl, haloalkenyloxy, haloalkynyloxy, hydroxyalkenyl, hydroxyalkoxy alkenyl, alkenyloxyalkyl, alkynyloxyalkyl, alkoxyalkenyl, alkoxyalkynyl, alkenyloxyalkoxy, alkynyloxyalkoxy, alkenyloxycarbonyl, alkynyloxycarbonyl, alkenylcarbonyl, alkynylcarbonyl, aminoalkenyl, aminoalkynyl, mono- or di(alkyl)aminoalkenyl, mono- or di(alkyl)aminoalkynyl, heterocyclylalkenyl, heterocyclylalkynyl, heteroarylalkenyl, heteroarylalkynyl, aryloxy, Aryloxyalkyl, aryloxyalkenyl, aryloxyalkynyl, arylthio, haloalkylthio, cycloalkylthio, alkylsulfinyl, alkylsulfonyl, cycloalkylsulfinyl, cycloalkylsulfonyl, arylsulfinyl, arylsulfonyl, mono- or di(alkyl)aminosulfonyl, mono- or di(alkyl)aminosulfinyl, alkoxycarbonylamino, alkenyloxycarbonylamino, alkynyloxycarbonylamino, alkylcarbonylamino, alkenylcarbonylamino,Alkynylcarbonylamino, cycloalkylcarbonylamino, arylcarbonylamino, cycloalkylcarbonyl, arylcarbonyl, mono- or di(alkyl)aminocarbonyl, alkylcarbonyloxy, alkenylcarbonyloxy, alkynylcarbonyloxy, sulfonyl, sulfinyl, mono- or di(alkyl)aminoalkylamino, mono- or di(alkyl)aminoalkoxy, arylamino, arylaminoalkyl, alkylcarbonyloxyalkyl, alkenylcarbonyloxyalkyl, alkynylcarbonyloxyalkyl, arylcarbonyloxy, arylcarbonyl and R is independently selected from heteroaryloxyalkyl, arylaminocarbonyl, heterocyclyloxy, heteroaryloxy, heteroarylthio, heteroaryloxyalkyl, heteroaryloxyalkenyl, heteroaryloxyalkynyl, heteroarylsulfinyl, heteroarylsulfonyl, heteroarylamino, heteroarylaminoalkyl, heteroarylcarbonylamino, heteroarylcarbonyl, heteroarylcarbonyloxy, heteroarylcarbonyloxyalkyl, and heteroarylaminocarbonyl, each of the foregoing groups may be unsubstituted or may contain one or more Z, 1a may be substituted with and / or two Zs 1 can be taken together with the atom(s) to which they are attached to form an aryl, cycloalkyl, heteroaryl, or heterocyclyl, each of which may be unsubstituted or may be substituted with one or more Z 1a may be substituted with and / or one R 1a is one Z 1 and together with the atom(s) to which they are attached can form a cycloalkyl, a 4- to 10-membered saturated or partially saturated heterocyclyl, a 5- to 10-membered heteroaryl, or an aryl, each of which can be unsubstituted or can be substituted with one or more Z 1a may be substituted with R1b is hydrogen or alkyl, or R 1b is one Z 1 and together with the atom(s) to which they are attached can form a 4- to 10-membered saturated or partially saturated heterocyclyl or a 5- to 10-membered heteroaryl, each of which can be unsubstituted or can be substituted with one or more Z 1a may be substituted with each Z 1a is independently selected from the group comprising halo, cyano, hydroxyl, alkyl, alkenyl, alkynyl, haloalkyl, haloalkenyl, haloalkynyl, alkoxy, alkenyloxy, alkynyloxy, alkylthio, alkenylthio, alkynylthio, haloalkoxy, hydroxyalkyl, alkoxyalkyl, cycloalkyl, cycloalkenyl, cycloalkynyl, cycloalkyloxy, aryl, arylalkyl, amino, mono- or di(alkyl)amino, mono- or di(alkyl)aminoalkyl, and oxo; or R 1 is selected from the group comprising hydrogen, halo, cyano, alkyl, alkenyl, alkynyl, haloalkyl, haloalkenyl, haloalkynyl, alkoxy, alkenyloxy, alkynyloxy, alkylthio, alkenylthio, alkynylthio, haloalkoxy, alkoxyalkyl, mono- or di(alkyl)amino, and mono- or di(alkyl)aminoalkyl; R 2 is aryl, heteroaryl, cycloalkyl, cycloalkenyl, cycloalkynyl, heterocyclyl and A 2 -X 2 - selected from the group comprising R 2 The above aryl, heteroaryl, cycloalkyl, cycloalkenyl, cycloalkynyl, heterocyclyl, X 2 and A 2 Each of may be unsubstituted or may contain one or more Z 2 may be substituted with X 2 -Y 2b -Y 2a -Y 2c- in which Y 2a is a single bond, double bond or triple bond, or -CR 2a =CR 2a -, -C≡C-, -CO-, -O-, -CS-, -S-, -SO2-, -SO-, -SO(NH)-, -CONR 2b -, -NR 2b CO-, -SO2NR 2b -, -NR 2b SO2-, -S(O)-NR 2b - and -NR 2b - selected from the group comprising Y 2b and Y 2c Each of the is a single bond, or C 1~3 Alkylene, C 2~3 Alkenylene, C 2~3 alkynylene, wherein C is independently selected from the group consisting of 1~3 Alkylene, C 2~3 Alkenylene, C 2~3 Each alkynylene may be unsubstituted or may contain one or more R 2a where Y 2a is a single bond, a double bond, or a triple bond, Y 2b and Y 2c At least one of Y 2a is a triple bond or a double bond, Y 2b and Y 2c is not a single bond, C2 alkenylene, or C2 alkynylene, Each R 2a are independently selected from the group including hydrogen, oxo, thioxo, halo, hydroxy, haloalkyl, alkoxy, alkoxyalkyl, haloalkoxy, haloalkoxyalkyl, mono- or di(alkyl)amino, mono- or di(alkyl)aminoalkyl, and alkyl; A 2 is selected from the group comprising aryl, heteroaryl, cycloalkyl, cycloalkenyl, cycloalkynyl and heterocyclyl; each Z 2are independently selected from halo, cyano, oxo, nitro, thioxo, or hydroxy, thio, alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkylalkyl, cycloalkenyl, cycloalkynyl, cycloalkenylalkyl, cycloalkynylalkyl, aryl, arylalkyl, arylalkenyl, arylalkynyl, haloalkyl, haloalkenyl, haloalkynyl, cyanoalkyl, alkoxy, alkenyloxy, alkynyloxy, cyanoalkoxy, alkylthio, alkenylthio, alkynylthio O, haloalkoxy, haloalkenyloxy, haloalkynyloxy, hydroxyalkyl, hydroxyalkenyl, hydroxyalkynyl, alkoxyalkyl, alkenyloxyalkyl, alkynyloxyalkyl, alkoxyalkenyl, alkynyl, cycloalkyloxy, cycloalkylalkoxy, alkoxyalkoxy, alkenyloxyalkoxy, alkynyloxyalkoxy, carboxyl, alkoxycarbonyl, alkenyloxycarbonyl, alkynyloxycarbonyl, alkylcarbonyl, alkenylcarbonyl nyl, alkynylcarbonyl, arylalkoxy, amino, mono- or di(alkyl)amino, aminoalkyl, aminoalkenyl, aminoalkynyl, mono- or di(alkyl)aminoalkyl, mono- or di(alkyl)aminoalkenyl, mono- or di(alkyl)aminoalkynyl, mono- or di(alkyl)aminocarbonyl, heterocyclyl, heteroaryl, heterocyclylalkyl, heteroarylalkyl, heterocyclylalkenyl, heterocyclylalkynyl, heteroarylalkenyl, heteroarylalkynyl, aryloxy, aryloxyalkyl, aryloxyalkenyl, aryloxyalkynyl, arylthio, haloalkylthio, cycloalkylthio, alkylsulfinyl, alkylsulfonyl, cycloalkylsulfinyl, cycloalkylsulfonyl, arylsulfinyl, arylsulfonyl, mono- or di(alkyl)aminosulfonyl, mono- or di(alkyl)aminosulfinyl, alkoxycarbonylamino, alkenyloxycarbonylamino, alkynyloxycarbonylamino, alkylcarbonylamino, alkenylcarbonylamino,Alkynylcarbonylamino, cycloalkylcarbonylamino, arylcarbonylamino, cycloalkylcarbonyl, arylcarbonyl, mono- or di(alkyl)aminocarbonyl, alkylcarbonyloxy, alkenylcarbonyloxy, alkynylcarbonyloxy, arylcarbonyloxy, sulfonyl, sulfinyl, mono- or di(alkyl)aminoalkylamino, mono- or di(alkyl)aminoalkoxy, arylamino, arylaminoalkyl, alkylcarbonyloxyalkyl, alkenylcarbonyloxyalkyl, alkynylcarbonyloxyalkyl, arylcarbonyloxy, aryl and R is independently selected from the group comprising heteroarylcarbonyloxyalkyl, arylaminocarbonyl, heterocyclyloxy, heteroaryloxy, heteroarylthio, heteroaryloxyalkyl, heteroaryloxyalkenyl, heteroaryloxyalkynyl, heteroarylsulfinyl, heteroarylsulfonyl, heteroarylamino, heteroarylaminoalkyl, heteroarylcarbonylamino, heteroarylcarbonyl, heteroarylcarbonyloxy, heteroarylcarbonyloxyalkyl and heteroarylaminocarbonyl, each of the foregoing groups may be unsubstituted or may contain one or more Z, 2a may be substituted with and / or two Zs 2 can be taken together with the atom(s) to which they are attached to form an aryl, cycloalkyl, heteroaryl, or heterocyclyl, each of which may be unsubstituted or may be substituted with one or more Z 2a may be substituted with and / or one R 2a is one Z 2 and together with the atom(s) to which they are attached can form a cycloalkyl, a 4- to 10-membered saturated or partially saturated heterocyclyl, a 5- to 10-membered heteroaryl, or an aryl, each of which can be unsubstituted or can be substituted with one or more Z 2a may be substituted with R 2b is hydrogen or alkyl, or R 2b is one Z 2 and together with the atom(s) to which they are attached can form a 4- to 10-membered saturated or partially saturated heterocyclyl or a 5- to 10-membered heteroaryl, each of which can be unsubstituted or can be substituted with one or more Z 2a may be substituted with each Z 2a is independently selected from the group comprising halo, cyano, hydroxyl, alkyl, alkenyl, alkynyl, haloalkyl, haloalkenyl, haloalkynyl, alkoxy, alkenyloxy, alkynyloxy, alkylthio, alkenylthio, alkynylthio, haloalkoxy, hydroxyalkyl, alkoxyalkyl, cycloalkyl, cycloalkenyl, cycloalkynyl, cycloalkyloxy, aryl, arylalkyl, amino, mono- or di(alkyl)amino, mono- or di(alkyl)aminoalkyl, and oxo; R 3 is selected from the group comprising hydrogen, halo, cyano, alkyl, alkenyl, alkynyl, haloalkyl, haloalkenyl, haloalkynyl, alkoxy, alkenyloxy, alkynyloxy, alkylthio, alkenylthio, alkynylthio, haloalkoxy, alkoxyalkyl, mono- or di(alkyl)amino, and mono- or di(alkyl)aminoalkyl; R 4 is aryl or heteroaryl, Each of the above aryl and heteroaryl groups may be selected from the group consisting of one or more Z 4 is replaced by each Z 4are independently selected from halo, cyano, oxo, nitro, thioxo, or hydroxy, thio, alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkylalkyl, cycloalkenyl, cycloalkynyl, cycloalkenylalkyl, cycloalkynylalkyl, aryl, arylalkyl, arylalkenyl, arylalkynyl, haloalkyl, haloalkenyl, haloalkynyl, cyanoalkyl, alkoxy, alkenyloxy, alkynyloxy, cyanoalkoxy, alkylthio, alkenylthio, alkynylthio O, haloalkoxy, haloalkenyloxy, haloalkynyloxy, hydroxyalkyl, hydroxyalkenyl, hydroxyalkynyl, alkoxyalkyl, alkenyloxyalkyl, alkynyloxyalkyl, alkoxyalkenyl, alkynyl, cycloalkyloxy, cycloalkylalkoxy, alkoxyalkoxy, alkenyloxyalkoxy, alkynyloxyalkoxy, carboxyl, alkoxycarbonyl, alkenyloxycarbonyl, alkynyloxycarbonyl, alkylcarbonyl, alkenylcarbonyl nyl, alkynylcarbonyl, arylalkoxy, amino, mono- or di(alkyl)amino, aminoalkyl, aminoalkenyl, aminoalkynyl, mono- or di(alkyl)aminoalkyl, mono- or di(alkyl)aminoalkenyl, mono- or di(alkyl)aminoalkynyl, mono- or di(alkyl)aminocarbonyl, heterocyclyl, heteroaryl, heterocyclylalkyl, heteroarylalkyl, heterocyclylalkenyl, heterocyclylalkynyl, heteroarylalkenyl, heteroarylalkynyl, aryloxy, aryloxyalkyl, aryloxyalkenyl, aryloxyalkynyl, arylthio, haloalkylthio, cycloalkylthio, alkylsulfinyl, alkylsulfonyl, cycloalkylsulfinyl, cycloalkylsulfonyl, arylsulfinyl, arylsulfonyl, mono- or di(alkyl)aminosulfonyl, mono- or di(alkyl)aminosulfinyl, alkoxycarbonylamino, alkenyloxycarbonylamino, alkynyloxycarbonylamino, alkylcarbonylamino, alkenylcarbonylamino,Alkynylcarbonylamino, cycloalkylcarbonylamino, arylcarbonylamino, cycloalkylcarbonyl, arylcarbonyl, mono- or di(alkyl)aminocarbonyl, alkylcarbonyloxy, alkenylcarbonyloxy, alkynylcarbonyloxy, arylcarbonyloxy, sulfonyl, sulfinyl, mono- or di(alkyl)aminoalkylamino, mono- or di(alkyl)aminoalkoxy, arylamino, arylaminoalkyl, alkylcarbonyloxyalkyl, alkenylcarbonyloxyalkyl, alkynylcarbonyloxyalkyl, arylcarbonyloxy, aryl and R is independently selected from the group comprising heteroarylcarbonyloxyalkyl, arylaminocarbonyl, heterocyclyloxy, heteroaryloxy, heteroarylthio, heteroaryloxyalkyl, heteroaryloxyalkenyl, heteroaryloxyalkynyl, heteroarylsulfinyl, heteroarylsulfonyl, heteroarylamino, heteroarylaminoalkyl, heteroarylcarbonylamino, heteroarylcarbonyl, heteroarylcarbonyloxy, heteroarylcarbonyloxyalkyl and heteroarylaminocarbonyl, each of the foregoing groups may be unsubstituted or may contain one or more Z, 4a may be substituted with and / or two Zs 4 can be taken together with the atom(s) to which they are attached to form an aryl, cycloalkyl, heteroaryl, or heterocyclyl, each of which may be unsubstituted or may contain one or more Z 4a may be substituted with each Z 4ais independently selected from the group comprising halo, cyano, hydroxyl, alkyl, alkenyl, alkynyl, haloalkyl, haloalkenyl, haloalkynyl, alkoxy, alkenyloxy, alkynyloxy, alkylthio, alkenylthio, alkynylthio, haloalkoxy, hydroxyalkyl, alkoxyalkyl, cycloalkyl, cycloalkenyl, cycloalkynyl, cycloalkyloxy, aryl, arylalkyl, amino, mono- or di(alkyl)amino, mono- or di(alkyl)aminoalkyl, and oxo; however, R 1 A 1 -X 1 - and X 1 is -CO- and A 1 When is heterocyclyl, A 1 is connected to X via the N ring atom of the heterocyclyl 1 is not bound to R 1 When is heteroaryl, R 1 is not oxadiazolyl, R 2 A 2 -X 2 - and X 2 is -CO- and A 2 When is heterocyclyl, A 2 is connected to X via the N ring atom of the heterocyclyl 2 is not bound to R 2 When is heteroaryl, R 2 is not oxadiazolyl, However, the above compound is N,4-bis(4-methylphenyl)-1H-pyrrole-3-sulfonamide; (CAS number 1427286-05-2), N,4-bis(4-chlorophenyl)-1H-pyrrole-3-sulfonamide (not CAS number 1427286-06-3), or a tautomer, stereoisomer, hydrate, solvate, polymorph, prodrug, isotope or co-crystal thereof, or a pharmaceutically acceptable salt thereof.

[0174] 2. During the ceremony, R 1 is C 6~10 Aryl, 5-10 membered heteroaryl, C 3~10 Cycloalkyl, C 5~10 Cycloalkenyl, C 5~10 Cycloalkynyl, 3- to 10-membered saturated or partially saturated heterocyclyl, and A 1 -X 1 -, and R 2 is hydrogen, halo, cyano, C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, HaloC 1~6 Alkyl, HaloC 2~6 Alkenyl, HaloC 2~6 Alkynyl, C 1~6 Alkoxy, C 2~6 Alkenyloxy, C 2~6 Alkynyloxy, C 1~6 Alkylthio, C 2~6 Alkenylthio, C 2~6 Alkynylthio, HaloC 1~6 Alkoxy, C 1~6 Alkoxy C 1~6 Alkyl, mono or di(C 1~6 alkyl)amino, and mono- or di-(C 1~6 Alkyl)amino C 1~6 is selected from the group including alkyl, R 1 Above C 6~10 Aryl, 5-10 membered heteroaryl, C 3~10 Cycloalkyl, C 5~10 Cycloalkenyl, C 5~10 cycloalkynyl, 3- to 10-membered saturated or partially saturated heterocyclyl, X 1 and A 1 Each of may be unsubstituted or may contain one or more Z 1 may be substituted with X 1 -Y 1b -Y 1a -Y 1c - in which Y 1a is a single bond, double bond or triple bond, or -CR 1a =CR1a -, -C≡C-, -CO-, -O-, -CS-, -S-, -SO2-, -SO-, -SO(NH)-, -CONR 1b -, -NR 1b CO-, -SO2NR 1b -, -NR 1b SO2-, -S(O)-NR 1b - and -NR 1b -, preferably selected from the group comprising X 1 is -C(R 1a )2-, -CR 1a =CR 1a -, -C≡C-, -CO-, -O-, -CS-, -S-, -SO2-, -SO-, -SO(NH)-, -CONR 1b -, -NR 1b CO-, -SO2NR 1b -, -NR 1b SO2-, -S(O)-NR 1b - and -NR 1b -, preferably selected from the group comprising X 1 is -C(R 1a )2-, -CO-, -O-, -S-, -SO2-, -SO- and -NR 1b -, preferably selected from the group comprising X 1 is -C(R 1a )2-, -CO-, -O- and -NR 1b - selected from the group comprising Y 1b and Y 1c Each of the is a single bond, or C 1~3 Alkylene, C 2~3 Alkenylene, C 2~3 alkynylene, wherein C is independently selected from the group consisting of 1~3 Alkylene, C 2~3 Alkenylene, C 2~3 Each alkynylene may be unsubstituted or may contain one or more R 1a where Y 1a is a single bond, a double bond, or a triple bond, Y 1b and Y 1c At least one of Y 1a is a triple bond or a double bond, Y1b and Y 1c is not a single bond, C2 alkenylene, or C2 alkynylene, Each R 1a is hydrogen, oxo, thioxo, halo, hydroxy, haloC 1~6 Alkyl, C 1~6 Alkoxy, C 1~6 Alkoxy C 1~6 Alkyl, HaloC 1~6 Alkoxy, HaloC 1~6 Alkoxy C 1~6 Alkyl, mono or di(C 1~6 alkyl)amino, mono- or di(C 1~6 Alkyl)amino C 1~6 Alkyl, and C 1~6 alkyl, and preferably each R 1a is hydrogen, halo, hydroxy, haloC 1~6 Alkyl, C 1~6 Alkoxy, C 1~6 Alkoxy C 1~6 Alkyl, HaloC 1~6 Alkoxy, HaloC 1~6 Alkoxy C 1~6 Alkyl, mono or di(C 1~6 alkyl)amino, mono- or di(C 1~6 Alkyl)amino C 1~6 Alkyl, and C 1~6 independently selected from the group consisting of alkyl, A 1 is C 6~10 Aryl, 5-10 membered heteroaryl, C 3~10 Cycloalkyl, C 5~10 Cycloalkenyl, C 5~10 selected from the group consisting of cycloalkynyl, and 3- to 10-membered saturated or partially saturated heterocyclyl; each Z 1 are independently selected from the group including halo, cyano, hydroxy, oxo, nitro, thioxo, or C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 3~10 Cycloalkyl, C 3~10 Cycloalkyl C 1~6Alkyl, C 5~10 Cycloalkenyl, C 5~10 Cycloalkynyl, C 6~10 Aryl, C 6~10 Aryl C 1~6 Alkyl, HaloC 1~6 Alkyl, HaloC 2~6 Alkenyl, HaloC 2~6 Alkynyl, Cyano C 1~6 Alkyl, C 1~6 Alkoxy, C 2~6 Alkenyloxy, C 2~6 Alkynyloxy, Cyano C 1~6 Alkoxy, C 1~6 Alkylthio, C 2~6 Alkenylthio, C 2~6 Alkynylthio, HaloC 1~6 Alkoxy, Hydroxy C 1~6 Alkyl, C 1~6 Alkoxy C 1~6 Alkyl, C 3~10 Cycloalkyloxy, C 3~10 Cycloalkyl C 1~6 Alkoxy, C 1~6 Alkoxy C 1~6 Alkoxy, carboxyl, C 1~6 Alkoxycarbonyl, C 1~6 Alkyl carbonyl, C 6~10 Aryl C 1~6 Alkoxy, mono or di(C 1~6 alkyl)amino, mono- or di(C 1~6 Alkyl)amino C 1~6 Alkyl, mono or di(C 1~6 Alkyl)aminocarbonyl, amino C 1~6 Alkyl, amino, 3- to 10-membered saturated or partially saturated heterocyclyl, 5- to 10-membered heteroaryl, 3- to 10-membered saturated or partially saturated heterocyclylC 1~6 Alkyl, 5-10 membered heteroarylC 1~6 Alkyl, C 6~10 Aryl C 2~6 Alkenyl, C 6~10 Aryl C 2~6 Alkynyl, HaloC 2~6 Alkenyloxy, HaloC 2~6Alkynyloxy, Hydroxy C 2~6 Alkenyl, Hydroxy C 2~6 Alkynyl, C 2~6 Alkenyloxy C 1~6 Alkyl, C 2~6 Alkynyloxy C 1~6 Alkyl, C 2~6 Alkenyloxy C 1~6 Alkoxy, C 2~6 Alkynyloxy C 1~6 Alkoxy, C 2~6 Alkenyloxycarbonyl, C 2~6 Alkynyloxycarbonyl, C 2~6 Alkenylcarbonyl, C 2~6 Alkynylcarbonyl, Amino C 2~6 Alkenyl, Amino C 2~6 Alkynyl, mono- or di(C 1~6 Alkyl)amino C 2~6 Alkenyl, mono- or di(C 1~6 Alkyl)amino C 2~6 Alkynyl, 3-10 membered saturated or partially saturated heterocyclyl C 2~6 Alkenyl, 3-10 membered saturated or partially saturated heterocyclylC 2~6 Alkynyl, 5-10 membered heteroaryl C 2~6 Alkenyl, 5-10 membered heteroaryl C 2~6 Alkynyl, C 6~10 Aryloxy, C 6~10 Aryloxy C 1~6 Alkyl, C 6~10 Aryloxy C 2~6 Alkenyl, C 6~10 Aryloxy C 2~6 Alkynyl, C 6~10 Arylthio, HaloC 1~6 Alkylthio, C 3~10 Cycloalkylthio, C 1~6 Alkylsulfinyl, C 1~6 Alkylsulfonyl, C 3~10 Cycloalkylsulfinyl, C 3~10 Cycloalkylsulfonyl, C 6~10 Arylsulfinyl, C 6~10 Arylsulfonyl, mono- or di-(C 1~6alkyl)aminosulfonyl, mono- or di-(C 1~6 alkyl)aminosulfinyl, C 1~6 Alkoxycarbonylamino, C 2~6 Alkenyloxycarbonylamino, C 2~6 Alkynyloxycarbonylamino, C 1~6 Alkylcarbonylamino, C 2~6 Alkenylcarbonylamino, C 2~6 Alkynylcarbonylamino, C 6~10 Cycloalkylcarbonylamino, C 6~10 Arylcarbonylamino, C 3~10 Cycloalkylcarbonyl, C 6~10 Arylcarbonyl, mono- or di(C 1~6 alkyl)aminocarbonyl, C 1~6 Alkylcarbonyloxy, C 2~6 Alkenylcarbonyloxy, C 2~6 Alkynylcarbonyloxy, C 6~10 Arylcarbonyloxy, C 5~10 Cycloalkenyl C 1~6 Alkyl, C 5~10 Cycloalkynyl C 1~6 Alkyl, sulfonyl, sulfinyl, mono- or di-(C 1~6 Alkyl)amino C 1~6 Alkylamino, mono or di(C 1~6 Alkyl)amino C 1~6 Alkoxy, C 6~10 Arylamino, C 6~10 Arylamino C 1~6 Alkyl, C 1~6 Alkylcarbonyloxy C 1~6 Alkyl, C 2~6 Alkenylcarbonyloxy C 1~6 Alkyl, C 2~6 Alkynylcarbonyloxy C 1~6 Alkyl, C 6~10 Arylcarbonyloxy, C 6~10 Arylcarbonyloxy C 1~6 Alkyl, C 6~10Arylaminocarbonyl, 3- to 10-membered saturated or partially saturated heterocyclyloxy, 5- to 10-membered heteroaryloxy, 5- to 10-membered heteroarylthio, 5- to 10-membered heteroaryloxyC 1~6 Alkyl, 5-10 membered 5-10 membered heteroaryloxyC 2~6 Alkenyl, 5-10 membered heteroaryloxy C 2~6 Alkynyl, 5- to 10-membered heteroarylsulfinyl, 5- to 10-membered heteroarylsulfonyl, 5- to 10-membered heteroarylamino, 5- to 10-membered heteroarylaminoC 1~6 Alkyl, 5- to 10-membered heteroarylcarbonylamino, 5- to 10-membered heteroarylcarbonyl, 5- to 10-membered heteroarylcarbonyloxy, 5- to 10-membered heteroarylcarbonyloxyC 1~6 alkyl, and 5- to 10-membered heteroarylaminocarbonyl, each of which may be unsubstituted or may be selected from the group consisting of one or more Z 1a may be substituted with and / or two Zs 1 together with the atom(s) to which they are attached, form C 6~10 Aryl, 5-10 membered heteroaryl, C 3~10 cycloalkyl, or 3- to 10-membered saturated or partially saturated heterocyclyl, 6~10 Aryl, heteroaryl, C 3~10 Each of the cycloalkyl and heterocyclyl may be unsubstituted or may contain one or more Z 1a may be substituted with and / or one R 1a is one Z 1 and together with the atom(s) to which they are attached, C 4~10 cycloalkyl, or 4- to 10-membered saturated or partially saturated heterocyclyl, or 5- to 10-membered heteroaryl, 4~10 Each cycloalkyl, heterocyclyl, or heteroaryl may be unsubstituted or may contain one or more Z 1a may be substituted with R 1b is hydrogen or C1~6 alkyl or R 1b is one Z 1 and together with the atom(s) to which they are attached can form a 4- to 10-membered saturated or partially saturated heterocyclyl or a 5- to 10-membered heteroaryl, each of which can be unsubstituted or can be substituted with one or more Z 1a may be substituted with each Z 1a are halo, cyano, hydroxyl, C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, HaloC 1~6 Alkyl, HaloC 2~6 Alkenyl, HaloC 2~6 Alkynyl, C 1~6 Alkoxy, C 2~6 Alkenyloxy, C 2~6 Alkynyloxy, C 1~6 Alkylthio, C 2~6 Alkenylthio, C 2~6 Alkynylthio, HaloC 1~6 Alkoxy, Hydroxy C 1~6 Alkyl, C 1~6 Alkoxy C 1~6 Alkyl, C 3~10 Cycloalkyl, C 5~10 Cycloalkenyl, C 5~10 Cycloalkynyl, C 3~10 Cycloalkyloxy, C 6~10 Aryl, C 6~10 Aryl C 1~6 Alkyl, amino, mono or di(C 1~6 alkyl)amino, mono- or di(C 1~6 Alkyl)amino C 1~6 independently selected from the group consisting of alkyl, and oxo; Or R 1 is hydrogen, halo, cyano, C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, HaloC 1~6 Alkyl, HaloC 2~6 Alkenyl, HaloC 2~6 Alkynyl, C1~6 Alkoxy, C 2~6 Alkenyloxy, C 2~6 Alkynyloxy, C 1~6 Alkylthio, C 2~6 Alkenylthio, C 2~6 Alkynylthio, HaloC 1~6 Alkoxy, C 1~6 Alkoxy C 1~6 Alkyl, mono or di(C 1~6 alkyl)amino, and mono- or di-(C 1~6 Alkyl)amino C 1~6 alkyl, R 2 is C 6~10 Aryl, 5-10 membered heteroaryl, C 3~10 Cycloalkyl, C 5~10 Cycloalkenyl, C 5~10 Cycloalkynyl, 3- to 10-membered saturated or partially saturated heterocyclyl, and A 2 -X 2 - selected from the group comprising R 2 Above C 6~10 Aryl, 5-10 membered heteroaryl, C 3~10 Cycloalkyl, C 5~10 Cycloalkenyl, C 5~10 cycloalkynyl, 3- to 10-membered saturated or partially saturated heterocyclyl, X 2 and A 2 Each of may be unsubstituted or may contain one or more Z 2 may be substituted with X 2 -Y 2b -Y 2a -Y 2c - in which Y 2a is a single bond, a double bond, or a triple bond, or -CR 2a =CR 2a -, -C≡C-, -CO-, -O-, -CS-, -S-, -SO2-, -SO-, -SO(NH)-, -CONR 2b -, -NR 2b CO-, -SO2NR 2b -, -NR 2b SO2-, -S(O)-NR 2b - and -NR2b -, preferably selected from the group comprising X 2 is -C(R 2a )2-, -CR 2a =CR 2a -, -C≡C-, -CO-, -O-, -CS-, -S-, -SO2-, -SO-, -SO(NH)-, -CONR 2b -, -NR 2b CO-, -SO2NR 2b -, -NR 2b SO2-, -S(O)-NR 2b - and -NR 2b -, preferably selected from the group comprising X 2 is -C(R 2a )2-, -CO-, -O-, -S-, -SO2-, -SO-, or -NR 2b -, preferably X 2 is -C(R 2a )2-, -CO-, -O-, or -NR 2b - selected from Y 2b and Y 2c Each of the is a single bond, or C 1~3 Alkylene, C 2~3 Alkenylene, C 2~3 alkynylene, wherein C is independently selected from the group consisting of 1~3 Alkylene, C 2~3 Alkenylene, C 2~3 Each alkynylene may be unsubstituted or may contain one or more R 2a where Y 2a is a single bond, a double bond, or a triple bond, Y 2b and Y 2c At least one of Y 2a is a triple bond or a double bond, Y 2b and Y 2c is not a single bond, C2 alkenylene, or C2 alkynylene, Each R 2a is hydrogen, oxo, thioxo, halo, hydroxy, haloC 1~6 Alkyl, C 1~6 Alkoxy, C 1~6 Alkoxy C1~6 Alkyl, HaloC 1~6 Alkoxy, HaloC 1~6 Alkoxy C 1~6 Alkyl, mono or di(C 1~6 alkyl)amino, mono- or di(C 1~6 Alkyl)amino C 1~6 Alkyl, and C 1~6 alkyl, and preferably each R 2a is hydrogen, halo, hydroxy, haloC 1~6 Alkyl, C 1~6 Alkoxy, C 1~6 Alkoxy C 1~6 Alkyl, HaloC 1~6 Alkoxy, HaloC 1~6 Alkoxy C 1~6 Alkyl, mono or di(C 1~6 alkyl)amino, mono- or di(C 1~6 Alkyl)amino C 1~6 Alkyl, and C 1~6 independently selected from the group consisting of alkyl, A 2 is C 6~10 Aryl, 5-10 membered heteroaryl, C 3~10 Cycloalkyl, C 5~10 Cycloalkenyl, C 5~10 selected from the group consisting of cycloalkynyl, and 3- to 10-membered saturated or partially saturated heterocyclyl; each Z 2 are independently selected from the group including halo, cyano, hydroxy, oxo, nitro, thioxo, or C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 3~10 Cycloalkyl, C 3~10 Cycloalkyl C 1~6 Alkyl, C 5~10 Cycloalkenyl, C 5~10 Cycloalkynyl, C 6~10 Aryl, C 6~10 Aryl C 1~6 Alkyl, HaloC 1~6 Alkyl, HaloC 2~6 Alkenyl, HaloC 2~6Alkynyl, Cyano C 1~6 Alkyl, C 1~6 Alkoxy, C 2~6 Alkenyloxy, C 2~6 Alkynyloxy, Cyano C 1~6 Alkoxy, C 1~6 Alkylthio, C 2~6 Alkenylthio, C 2~6 Alkynylthio, HaloC 1~6 Alkoxy, Hydroxy C 1~6 Alkyl, C 1~6 Alkoxy C 1~6 Alkyl, C 3~10 Cycloalkyloxy, C 3~10 Cycloalkyl C 1~6 Alkoxy, C 1~6 Alkoxy C 1~6 Alkoxy, carboxyl, C 1~6 Alkoxycarbonyl, C 1~6 Alkyl carbonyl, C 6~10 Aryl C 1~6 Alkoxy, mono or di(C 1~6 alkyl)amino, mono- or di(C 1~6 Alkyl)amino C 1~6 Alkyl, mono or di(C 1~6 Alkyl)aminocarbonyl, amino C 1~6 Alkyl, amino, 3- to 10-membered saturated or partially saturated heterocyclyl, 5- to 10-membered heteroaryl, 3- to 10-membered saturated or partially saturated heterocyclylC 1~6 Alkyl, 5-10 membered heteroarylC 1~6 Alkyl, C 6~10 Aryl C 2~6 Alkenyl, C 6~10 Aryl C 2~6 Alkynyl, HaloC 2~6 Alkenyloxy, HaloC 2~6 Alkynyloxy, Hydroxy C 2~6 Alkenyl, Hydroxy C 2~6 Alkynyl, C 2~6 Alkenyloxy C 1~6 Alkyl, C 2~6 Alkynyloxy C 1~6 Alkyl, C 2~6 Alkenyloxy C 1~6Alkoxy, C 2~6 Alkynyloxy C 1~6 Alkoxy, C 2~6 Alkenyloxycarbonyl, C 2~6 Alkynyloxycarbonyl, C 2~6 Alkenylcarbonyl, C 2~6 Alkynylcarbonyl, Amino C 2~6 Alkenyl, Amino C 2~6 Alkynyl, mono- or di(C 1~6 Alkyl)amino C 2~6 Alkenyl, mono- or di(C 1~6 Alkyl)amino C 2~6 Alkynyl, 3-10 membered saturated or partially saturated heterocyclyl C 2~6 Alkenyl, 3-10 membered saturated or partially saturated heterocyclylC 2~6 Alkynyl, 5-10 membered heteroaryl C 2~6 Alkenyl, 5-10 membered heteroaryl C 2~6 Alkynyl, C 6~10 Aryloxy, C 6~10 Aryloxy C 1~6 Alkyl, C 6~10 Aryloxy C 2~6 Alkenyl, C 6~10 Aryloxy C 2~6 Alkynyl, C 6~10 Arylthio, HaloC 1~6 Alkylthio, C 3~10 Cycloalkylthio, C 1~6 Alkylsulfinyl, C 1~6 Alkylsulfonyl, C 3~10 Cycloalkylsulfinyl, C 3~10 Cycloalkylsulfonyl, C 6~10 Arylsulfinyl, C 6~10 Arylsulfonyl, mono- or di-(C 1~6 alkyl)aminosulfonyl, mono- or di-(C 1~6 alkyl)aminosulfinyl, C 1~6 Alkoxycarbonylamino, C 2~6 Alkenyloxycarbonylamino, C 2~6 Alkynyloxycarbonylamino, C 1~6 Alkylcarbonylamino, C2~6 Alkenylcarbonylamino, C 2~6 Alkynylcarbonylamino, C 6~10 Cycloalkylcarbonylamino, C 6~10 Arylcarbonylamino, C 3~10 Cycloalkylcarbonyl, C 6~10 Arylcarbonyl, mono- or di(C 1~6 alkyl)aminocarbonyl, C 1~6 Alkylcarbonyloxy, C 2~6 Alkenylcarbonyloxy, C 2~6 Alkynylcarbonyloxy, C 6~10 Arylcarbonyloxy, C 5~10 Cycloalkenyl C 1~6 Alkyl, C 5~10 Cycloalkynyl C 1~6 Alkyl, sulfonyl, sulfinyl, mono- or di-(C 1~6 Alkyl)amino C 1~6 Alkylamino, mono or di(C 1~6 Alkyl)amino C 1~6 Alkoxy, C 6~10 Arylamino, C 6~10 Arylamino C 1~6 Alkyl, C 1~6 Alkylcarbonyloxy C 1~6 Alkyl, C 2~6 Alkenylcarbonyloxy C 1~6 Alkyl, C 2~6 Alkynylcarbonyloxy C 1~6 Alkyl, C 6~10 Arylcarbonyloxy, C 6~10 Arylcarbonyloxy C 1~6 Alkyl, C 6~10 Arylaminocarbonyl, 3- to 10-membered saturated or partially saturated heterocyclyloxy, 5- to 10-membered heteroaryloxy, 5- to 10-membered heteroarylthio, 5- to 10-membered heteroaryloxyC 1~6 Alkyl, 5-10 membered 5-10 membered heteroaryloxyC 2~6 Alkenyl, 5-10 membered heteroaryloxy C 2~6Alkynyl, 5- to 10-membered heteroarylsulfinyl, 5- to 10-membered heteroarylsulfonyl, 5- to 10-membered heteroarylamino, 5- to 10-membered heteroarylaminoC 1~6 Alkyl, 5- to 10-membered heteroarylcarbonylamino, 5- to 10-membered heteroarylcarbonyl, 5- to 10-membered heteroarylcarbonyloxy, 5- to 10-membered heteroarylcarbonyloxyC 1~6 alkyl, and 5- to 10-membered heteroarylaminocarbonyl, each of which may be unsubstituted or may be selected from the group consisting of one or more Z 2a may be substituted with and / or two Zs 2 together with the atom(s) to which they are attached, form C 6~10 Aryl, 5-10 membered heteroaryl, C 3~10 cycloalkyl, or 3- to 10-membered saturated or partially saturated heterocyclyl, 6~10 Aryl, heteroaryl, C 3~10 Each of the cycloalkyl and heterocyclyl may be unsubstituted or may contain one or more Z 2a may be substituted with and / or one R 2a is one Z 2 and together with the atom(s) to which they are attached, C 4~10 cycloalkyl, or 4- to 10-membered saturated or partially saturated heterocyclyl, or 5- to 10-membered heteroaryl, 4~10 Each cycloalkyl, heterocyclyl, or heteroaryl may be unsubstituted or may contain one or more Z 2a may be substituted with R 2b is hydrogen or C 1~6 alkyl or R 2b is one Z 2 and together with the atom(s) to which they are attached can form a 4- to 10-membered saturated or partially saturated heterocyclyl or a 5- to 10-membered heteroaryl, each of which can be unsubstituted or can be substituted with one or more Z2a may be substituted with each Z 2a are halo, cyano, hydroxyl, C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, HaloC 1~6 Alkyl, HaloC 2~6 Alkenyl, HaloC 2~6 Alkynyl, C 1~6 Alkoxy, C 2~6 Alkenyloxy, C 2~6 Alkynyloxy, C 1~6 Alkylthio, C 2~6 Alkenylthio, C 2~6 Alkynylthio, HaloC 1~6 Alkoxy, Hydroxy C 1~6 Alkyl, C 1~6 Alkoxy C 1~6 Alkyl, C 3~10 Cycloalkyl, C 5~10 Cycloalkenyl, C 5~10 Cycloalkynyl, C 3~10 Cycloalkyloxy, C 6~10 Aryl, C 6~10 Aryl C 1~6 Alkyl, amino, mono or di(C 1~6 alkyl)amino, mono- or di(C 1~6 Alkyl)amino C 1~6 independently selected from the group consisting of alkyl, and oxo; R 3 is hydrogen, halo, cyano, C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, HaloC 1~6 Alkyl, HaloC 2~6 Alkenyl, HaloC 2~6 Alkynyl, C 1~6 Alkoxy, C 2~6 Alkenyloxy, C 2~6 Alkynyloxy, C 1~6 Alkylthio, C 2~6 Alkenylthio, C 2~6 Alkynylthio, HaloC 1~6 Alkoxy, C 1~6 Alkoxy C1~6 Alkyl, mono or di(C 1~6 alkyl)amino, and mono- or di-(C 1~6 Alkyl)amino C 1~6 is selected from the group including alkyl, R 4 is C 6~10 aryl or 5- to 10-membered heteroaryl; Above C 6~10 Each of the aryl and 5- to 10-membered heteroaryl may be one or more Z 4 is replaced by each Z 4 are independently selected from halo, cyano, hydroxyl, oxo, nitro, and thioxo; or C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 3~10 Cycloalkyl, C 3~10 Cycloalkyl C 1~6 Alkyl, C 5~10 Cycloalkenyl, C 5~10 Cycloalkynyl, C 6~10 Aryl, C 6~10 Aryl C 1~6 Alkyl, HaloC 1~6 Alkyl, HaloC 2~6 Alkenyl, HaloC 2~6 Alkynyl, Cyano C 1~6 Alkyl, C 1~6 Alkoxy, C 2~6 Alkenyloxy, C 2~6 Alkynyloxy, Cyano C 1~6 Alkoxy, C 1~6 Alkylthio, C 2~6 Alkenylthio, C 2~6 Alkynylthio, HaloC 1~6 Alkoxy, Hydroxy C 1~6 Alkyl, C 1~6 Alkoxy C 1~6 Alkyl, C 3~10 Cycloalkyloxy, C 3~10 Cycloalkyl C 1~6 Alkoxy, C 1~6 Alkoxy C 1~6 Alkoxy, carboxyl, C 1~6Alkoxycarbonyl, C 1~6 Alkyl carbonyl, C 6~10 Aryl C 1~6 Alkoxy, mono or di(C 1~6 (C1-6 alkyl)amino, mono- or di(C1-6 alkyl)amino C 1~6 Alkyl, mono or di(C 1~6 Alkyl)aminocarbonyl, amino C 1~6 Alkyl, amino, 3- to 10-membered saturated or partially saturated heterocyclyl, 5- to 10-membered heteroaryl, 3- to 10-membered saturated or partially saturated heterocyclylC 1~6 Alkyl, 5-10 membered heteroarylC 1~6 Alkyl, C 6~10 Aryl C 2~6 Alkenyl, C 6~10 Aryl C 2~6 Alkynyl, HaloC 2~6 Alkenyloxy, HaloC 2~6 Alkynyloxy, Hydroxy C 2~6 Alkenyl, Hydroxy C 2~6 Alkynyl, C 2~6 Alkenyloxy C 1~6 Alkyl, C 2~6 Alkynyloxy C 1~6 Alkyl, C 2~6 Alkenyloxy C 1~6 Alkoxy, C 2~6 Alkynyloxy C 1~6 Alkoxy, C 2~6 Alkenyloxycarbonyl, C 2~6 Alkynyloxycarbonyl, C 2~6 Alkenylcarbonyl, C 2~6 Alkynylcarbonyl, Amino C 2~6 Alkenyl, Amino C 2~6 Alkynyl, mono- or di(C 1~6 Alkyl)amino C 2~6 Alkenyl, mono- or di(C 1~6 Alkyl)amino C 2~6 Alkynyl, 3-10 membered saturated or partially saturated heterocyclyl C 2~6 Alkenyl, 3-10 membered saturated or partially saturated heterocyclylC 2~6 Alkynyl, 5-10 membered heteroaryl C 2~6Alkenyl, 5-10 membered heteroaryl C 2~6 Alkynyl, C 6~10 Aryloxy, C 6~10 Aryloxy C 1~6 Alkyl, C 6~10 Aryloxy C 2~6 Alkenyl, C 6~10 Aryloxy C 2~6 Alkynyl, C 6~10 Arylthio, HaloC 1~6 Alkylthio, C 3~10 Cycloalkylthio, C 1~6 Alkylsulfinyl, C 1~6 Alkylsulfonyl, C 3~10 Cycloalkylsulfinyl, C 3~10 Cycloalkylsulfonyl, C 6~10 Arylsulfinyl, C 6~10 Arylsulfonyl, mono- or di-(C 1~6 alkyl)aminosulfonyl, mono- or di-(C 1~6 alkyl)aminosulfinyl, C 1~6 Alkoxycarbonylamino, C 2~6 Alkenyloxycarbonylamino, C 2~6 Alkynyloxycarbonylamino, C 1~6 Alkylcarbonylamino, C 2~6 Alkenylcarbonylamino, C 2~6 Alkynylcarbonylamino, C 6~10 Cycloalkylcarbonylamino, C 6~10 Arylcarbonylamino, C 3~10 Cycloalkylcarbonyl, C 6~10 Arylcarbonyl, mono- or di(C 1~6 alkyl)aminocarbonyl, C 1~6 Alkylcarbonyloxy, C 2~6 Alkenylcarbonyloxy, C 2~6 Alkynylcarbonyloxy, C 6~10 Arylcarbonyloxy, C 5~10 Cycloalkenyl C 1~6 Alkyl, C 5~10 Cycloalkynyl C 1~6 Alkyl, sulfonyl, sulfinyl, mono- or di-(C1~6 Alkyl)amino C 1~6 Alkylamino, mono or di(C 1~6 Alkyl)amino C 1~6 Alkoxy, C 6~10 Arylamino, C 6~10 Arylamino C 1~6 Alkyl, C 1~6 Alkylcarbonyloxy C 1~6 Alkyl, C 2~6 Alkenylcarbonyloxy C 1~6 Alkyl, C 2~6 Alkynylcarbonyloxy C 1~6 Alkyl, C 6~10 Arylcarbonyloxy, C 6~10 Arylcarbonyloxy C 1~6 Alkyl, C 6~10 Arylaminocarbonyl, 3- to 10-membered saturated or partially saturated heterocyclyloxy, 5- to 10-membered heteroaryloxy, 5- to 10-membered heteroarylthio, 5- to 10-membered heteroaryloxyC 1~6 Alkyl, 5-10 membered 5-10 membered heteroaryloxyC 2~6 Alkenyl, 5-10 membered heteroaryloxy C 2~6 Alkynyl, 5- to 10-membered heteroarylsulfinyl, 5- to 10-membered heteroarylsulfonyl, 5- to 10-membered heteroarylamino, 5- to 10-membered heteroarylaminoC 1~6 Alkyl, 5- to 10-membered heteroarylcarbonylamino, 5- to 10-membered heteroarylcarbonyl, 5- to 10-membered heteroarylcarbonyloxy, 5- to 10-membered heteroarylcarbonyloxyC 1~6 alkyl, and 5- to 10-membered heteroarylaminocarbonyl, each of which may be unsubstituted or may be selected from the group consisting of one or more Z 4a may be substituted with and / or two Zs 4 together with the atom(s) to which they are attached, form C 6~10 Aryl, 5-10 membered heteroaryl, C 3~10 cycloalkyl, or 3- to 10-membered saturated or partially saturated heterocyclyl, 6~10Aryl, heteroaryl, C 3~10 Each of the cycloalkyl and heterocyclyl may be unsubstituted or may contain one or more Z 4a may be substituted with each Z 4a are halo, cyano, hydroxyl, C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, HaloC 1~6 Alkyl, HaloC 2~6 Alkenyl, HaloC 2~6 Alkynyl, C 1~6 Alkoxy, C 2~6 Alkenyloxy, C 2~6 Alkynyloxy, C 1~6 Alkylthio, C 2~6 Alkenylthio, C 2~6 Alkynylthio, HaloC 1~6 Alkoxy, Hydroxy C 1~6 Alkyl, C 1~6 Alkoxy C 1~6 Alkyl, C 3~10 Cycloalkyl, C 5~10 Cycloalkenyl, C 5~10 Cycloalkynyl, C 3~10 Cycloalkyloxy, C 6~10 Aryl, C 6~10 Aryl C 1~6 Alkyl, amino, mono or di(C 1~6 alkyl)amino, mono- or di(C 1~6 Alkyl)amino C 1~6 The compound of statement 1, wherein each of said groups is independently selected from the group consisting of alkyl, and oxo.

[0175] 3. During the ceremony, R 1 is C 6~10 Aryl, 5-10 membered heteroaryl, C 3~10 Cycloalkyl, C 5~10 Cycloalkenyl, 3- to 10-membered saturated or partially saturated heterocyclyl and A 1 -X 1 -, preferably R 1 is C 6~10Aryl, 5-10 membered heteroaryl, C 3~10 Cycloalkyl, C 5~10 Cycloalkenyl and A 1 -X 1 -, preferably R 1 is C 6~10 Aryl, 5-8 membered heteroaryl, C 5~8 Cycloalkyl, C 3~8 Cycloalkenyl and A 1 -X 1 -, preferably R 1 is phenyl, 5-6 membered heteroaryl, C 3~6 Cycloalkyl, C 5~6 Cycloalkenyl and A 1 -X 1 -, preferably R 1 is phenyl, 5-6 membered heteroaryl, C 4~5 Cycloalkyl, cyclohexenyl, and A 1 -X 1 -, and R 1 is phenyl, 5-6 membered heteroaryl, C 4~5 selected from the group comprising cycloalkyl and cyclohexenyl; R 1 Above C 6~10 Aryl, 5-10 membered heteroaryl, C 3~10 Cycloalkyl, C 5~10 cycloalkenyl, 3- to 10-membered saturated or partially saturated heterocyclyl, X 1 and A 1 Each of may be unsubstituted or may contain one or more Z 1 may be substituted with R 2 is hydrogen, halo, cyano, C 1~6 Alkyl, C 2~6 Alkenyl, HaloC 1~6 Alkyl, HaloC 2~6 Alkenyl, C 1~6 Alkoxy, C 2~6 Alkenyloxy, C 1~6 Alkylthio, C 2~6 Alkenylthio, HaloC 1~6 Alkoxy, C1~6 Alkoxy C 1~6 Alkyl, mono or di(C 1~6 alkyl)amino and mono- or di-(C 1~6 Alkyl)amino C 1~6 alkyl, preferably R 2 is hydrogen or C 1~6 alkyl, preferably R 2 is hydrogen or C 1~4 alkyl, preferably R 2 is hydrogen or C 1~2 alkyl, preferably R 2 is selected from hydrogen or methyl, preferably R 2 3. The compound of any one of statements 1 or 2, wherein:

[0176] 4. During the ceremony, X 1 -Y 1b -Y 1a -Y 1c - in which Y 1a is a single bond, a double bond, or a triple bond, or -CR 1a =CR 1a -, -C≡C-, -CO-, -O-, -CS-, -S-, -SO2-, -SO-, -SO(NH)-, -CONR 1b -, -NR 1b CO-, -SO2NR 1b -, -NR 1b SO2-, -S(O)-NR 1b - and -NR 1b -, preferably selected from the group comprising X 1 is -C(R 1a )2-, -CR 1a =CR 1a -, -C≡C-, -CO-, -O-, -CS-, -S-, -SO2-, -SO-, -SO(NH)-, -CONR 1b -, -NR 1b CO-, -SO2NR 1b -, -NR 1b SO2-, -S(O)-NR 1b - and -NR 1b-, preferably selected from the group comprising X 1 is -C(R 1a )2-, -CO-, -O-, -CS-, -S-, -SO2-, -SO-, and -NR 1b -, preferably selected from the group comprising X 1 is -C(R 1a )2-, -CO-, -O- or -NR 1b and preferably X 1 is -C(R 1a )2-, -CO- or -NR 1b and preferably X 1 is -C(R 1a )2- or -CO-, preferably X 1 is -C(R 1a )2-, and preferably X 1 is -CH2-, Y 1b and Y 1c Each of the is a single bond, or C 1~3 Alkylene, C 2~3 Alkenylene, C 2~3 alkynylene, wherein C is independently selected from the group consisting of 1~3 Alkylene, C 2~3 Alkenylene, C 2~3 Each alkynylene may be unsubstituted or may contain one or more R 1a where Y 1a is a single bond, a double bond, or a triple bond, Y 1b and Y 1c At least one of Y 1a is a triple bond or a double bond, Y 1b and Y 1c is not a single bond, C2 alkenylene, or C2 alkynylene, Each R 1a is hydrogen, oxo, thioxo, halo, hydroxy, haloC 1~6 Alkyl, C 1~6 Alkoxy, C 1~6 Alkoxy C 1~6 Alkyl, HaloC 1~6 Alkoxy, HaloC 1~6 Alkoxy C1~6 Alkyl, mono or di(C 1~6 alkyl)amino, mono- or di(C 1~6 Alkyl)amino C 1~6 Alkyl, and C 1~6 alkyl, and preferably each R 1a is hydrogen, halo, hydroxy, haloC 1~6 Alkyl, C 1~6 Alkoxy, HaloC 1~6 Alkoxy, and C 1~6 alkyl, and preferably each R 1a is hydrogen, halo, hydroxy, and C 1~6 alkyl, and preferably each R 1a is hydrogen or C 1~6 alkyl, and preferably each R 1a is hydrogen or C 1~4 alkyl, and preferably each R 1a is hydrogen or C 1~2 alkyl, and preferably each R 1a are independently selected from hydrogen or methyl; A 1 is C 6~10 Aryl, 5-10 membered heteroaryl, C 3~10 Cycloalkyl, C 5~10 cycloalkenyl, and 3- to 10-membered saturated or partially saturated heterocyclyl, preferably 1 is C 6~10 Aryl, 5-10 membered heteroaryl, C 3~10 Cycloalkyl, and C 5~10 cycloalkenyl, preferably selected from the group consisting of A 1 is C 6~10 Aryl, 5-10 membered heteroaryl, C 3~6 Cycloalkyl, and C 5~10 cycloalkenyl, preferably selected from the group consisting of A 1 is C 6~10 Aryl, 5-8 membered heteroaryl, C 3~6 Cycloalkyl, and C 5~8cycloalkenyl, preferably selected from the group consisting of A 1 is phenyl, C 3~6 A is selected from the group consisting of cycloalkyl, 5- to 6-membered heteroaryl and cyclohexenyl, preferably 1 is phenyl, C 3~4 cycloalkyl, or 5- to 6-membered heteroaryl; and / or one R 1a is one Z 1 and together with the atom(s) to which they are attached, C 4~10 cycloalkyl, or 4- to 10-membered saturated or partially saturated heterocyclyl, or 5- to 10-membered heteroaryl, 4~10 Each cycloalkyl, heterocyclyl, or heteroaryl may be unsubstituted or may contain one or more Z 1a may be substituted with R 1b is hydrogen or C 1~6 alkyl, and preferably, each R 1b is hydrogen or C 1~4 alkyl, and preferably each R 1b is hydrogen or C 1~2 alkyl, and preferably each R 1b are independently selected from hydrogen or methyl, or R 1b is one Z 1 and together with the atom(s) to which they are attached can form a 4- to 10-membered saturated or partially saturated heterocyclyl or a 5- to 10-membered heteroaryl, each of which can be unsubstituted or can be substituted with one or more Z 1a A compound according to any one of statements 1 to 3, optionally substituted with

[0177] 5. During the ceremony, each Z 1 are independently selected from halo, cyano, hydroxy, oxo, nitro, and thioxo; or C 1~6 Alkyl, C 2~6 Alkenyl, C 3~10 Cycloalkyl, C3~10 Cycloalkyl C 1~6 Alkyl, C 5~10 Cycloalkenyl, C 6~10 Aryl, C 6~10 Aryl C 1~6 Alkyl, HaloC 1~6 Alkyl, HaloC 2~6 Alkenyl, Cyano C 1~6 Alkyl, C 1~6 Alkoxy, C 2~6 Alkenyloxy, Cyano C 1~6 Alkoxy, C 1~6 Alkylthio, C 2~6 Alkenylthio, HaloC 1~6 Alkoxy, Hydroxy C 1~6 Alkyl, C 1~6 Alkoxy C 1~6 Alkyl, C 3~10 Cycloalkyloxy, C 3~10 Cycloalkyl C 1~6 Alkoxy, C 1~6 Alkoxy C 1~6 Alkoxy, carboxyl, C 1~6 Alkoxycarbonyl, C 1~6 Alkyl carbonyl, C 6~10 Aryl C 1~6 Alkoxy, mono or di(C 1~6 alkyl)amino, mono- or di(C 1~6 Alkyl)amino C 1~6 Alkyl, mono or di(C 1~6 Alkyl)aminocarbonyl, amino C 1~6 Alkyl, 3- to 10-membered saturated or partially saturated heterocyclyl, 5- to 10-membered heteroaryl, 3- to 10-membered saturated or partially saturated heterocyclylC 1~6 Alkyl, 5-10 membered heteroarylC 1~6 Alkyl, C 6~10 Aryl C 2~6 Alkenyl, HaloC 2~6 Alkenyloxy, Hydroxy C 2~6 Alkenyl, C 2~6 Alkenyloxy C 1~6 Alkyl, C 2~6 Alkenyloxy C 1~6 Alkoxy, C 2~6Alkenyloxycarbonyl, C 2~6 Alkenylcarbonyl, Amino C 2~6 Alkenyl, mono- or di(C 1~6 Alkyl)amino C 2~6 Alkenyl, 3-10 membered saturated or partially saturated heterocyclylC 2~6 Alkenyl, 5-10 membered heteroaryl C 2~6 Alkenyl, C 6~10 Aryloxy, C 6~10 Aryloxy C 1~6 Alkyl, C 6~10 Aryloxy C 2~6 Alkenyl, C 6~10 Arylthio, HaloC 1~6 Alkylthio, C 3~10 Cycloalkylthio, C 1~6 Alkylsulfinyl, C 1~6 Alkylsulfonyl, C 3~10 Cycloalkylsulfinyl, C 3~10 Cycloalkylsulfonyl, C 6~10 Arylsulfinyl, C 6~10 Arylsulfonyl, mono- or di-(C 1~6 alkyl)aminosulfonyl, mono- or di-(C 1~6 alkyl)aminosulfinyl, C 1~6 Alkoxycarbonylamino, C 2~6 Alkenyloxycarbonylamino, C 1~6 Alkylcarbonylamino, C 2~6 Alkenylcarbonylamino, C 6~10 Cycloalkylcarbonylamino, C 6~10 Arylcarbonylamino, C 3~10 Cycloalkylcarbonyl, C 6~10 Arylcarbonyl, mono- or di(C 1~6 alkyl)aminocarbonyl, C 1~6 Alkylcarbonyloxy, C 2~6 Alkenylcarbonyloxy and C 6~10 arylcarbonyloxy, each of which may be unsubstituted or may contain one or more Z 1a and preferably, each Z 1are independently selected from halo, cyano, oxo, and thioxo; or C 1~6 Alkyl, C 3~10 Cycloalkyl, C 6~10 Aryl, HaloC 1~6 Alkyl, Cyano C 1~6 Alkyl, C 1~6 Alkoxy, Cyano C 1~6 Alkoxy, C 1~6 Alkylthio, HaloC 1~6 Alkoxy, Hydroxy C 1~6 Alkyl, C 1~6 Alkoxy C 1~6 Alkyl, C 3~10 Cycloalkyloxy, C 3~10 Cycloalkyl C 1~6 Alkoxy, C 1~6 Alkoxy C 1~6 Alkoxy, C 1~6 Alkoxycarbonyl, C 1~6 Alkyl carbonyl, C 6~10 Aryl C 1~6 Alkoxy, mono or di(C 1~6 alkyl)amino, mono- or di(C 1~6 Alkyl)amino C 1~6 Alkyl, mono or di(C 1~6 alkyl)aminocarbonyl 3-10 membered saturated or partially saturated heterocyclyl, 5-10 membered heteroaryl, 3-10 membered saturated or partially saturated heterocyclylC 1~6 Alkyl, 5-10 membered heteroarylC 1~6 Alkyl, C 6~10 Aryloxy, C 6~10 Aryloxy C 1~6 Alkyl, C 6~10 Arylthio, HaloC 1~6 Alkylthio, C 3~10 Cycloalkylthio, C 1~6 Alkylsulfinyl, C 1~6 Alkylsulfonyl, C 3~10 Cycloalkylsulfinyl, C 3~10 Cycloalkylsulfonyl, C 6~10 Arylsulfinyl, C 6~10 Arylsulfonyl, mono- or di-(C 1~6alkyl)aminosulfonyl, mono- or di-(C 1~6 alkyl)aminosulfinyl, C 1~6 Alkoxycarbonylamino, C 1~6 Alkylcarbonylamino, C 6~10 Cycloalkylcarbonylamino, C 6~10 Arylcarbonylamino, C 3~10 Cycloalkylcarbonyl, C 6~10 Arylcarbonyl, mono- or di(C 1~6 alkyl)aminocarbonyl, C 1~6 Alkylcarbonyloxy, and C 6~10 arylcarbonyloxy, each of which may be unsubstituted or may contain one or more Z 1a and preferably, each Z 1 are independently selected from halo, cyano, and oxo; or C 1~6 Alkyl, C 3~10 Cycloalkyl, C 6~10 Aryl, HaloC 1~6 Alkyl, Cyano C 1~6 Alkyl, C 1~6 Alkoxy, Cyano C 1~6 Alkoxy, C 1~6 Alkylthio, HaloC 1~6 Alkoxy, Hydroxy C 1~6 Alkyl, C 1~6 Alkoxy C 1~6 Alkyl, C 3~10 Cycloalkyloxy, C 3~10 Cycloalkyl C 1~6 Alkoxy, C 1~6 Alkoxy C 1~6 Alkoxy, C 1~6 Alkoxycarbonyl, C 1~6 Alkyl carbonyl, C 6~10 Aryl C 1~6 Alkoxy, mono or di(C 1~6 and each of the above groups may be unsubstituted or may be selected from the group consisting of one or more Z 1a and preferably, each Z 1are independently selected from halo, cyano, and oxo; or C 1~6 Alkyl, C 3~10 Cycloalkyl, HaloC 1~6 Alkyl, Cyano C 1~6 Alkyl, C 1~6 Alkoxy, Cyano C 1~6 Alkoxy, C 1~6 Alkylthio, HaloC 1~6 Alkoxy, Hydroxy C 1~6 Alkyl, C 1~6 Alkoxy C 1~6 Alkyl, C 3~10 Cycloalkyloxy and C 3~10 Cycloalkyl C 1~6 alkoxy, each of which may be unsubstituted or may be selected from the group consisting of one or more Z 1a and preferably, each Z 1 are independently selected from halo, cyano, and oxo; or C 1~6 Alkyl, HaloC 1~6 Alkyl, C 1~6 Alkoxy, C 1~6 Alkylthio, HaloC 1~6 Alkoxy, Hydroxy C 1~6 Alkyl, C 1~6 Alkoxy C 1~6 Alkyl, C 3~10 Cycloalkyloxy and C 3~10 Cycloalkyl C 1~6 alkoxy, each of which may be unsubstituted or may be selected from the group consisting of one or more Z 1a and preferably, each Z 1 are independently selected from halo, cyano, and oxo; or C 1~4 Alkyl, HaloC 1~4 Alkyl, C 1~4 Alkoxy, C 1~4 Alkylthio, HaloC 1~4 Alkoxy, Hydroxy C 1~4 Alkyl, C 1~4 Alkoxy C 1~4 Alkyl, C 3~6 Cycloalkyloxy and C 3~6 Cycloalkyl C1~4 alkoxy, each of which may be unsubstituted or may be selected from the group consisting of one or more Z 1a and preferably, each Z 1 are independently selected from halo, cyano, and oxo; or C 1~2 Alkyl, HaloC 1~2 Alkyl, C 1~2 Alkoxy, C 1~2 Alkylthio, HaloC 1~2 Alkoxy, Hydroxy C 1~2 Alkyl, C 1~2 Alkoxy C 1~2 Alkyl, C 3~6 Cycloalkyloxy and C 3~6 Cycloalkyl C 1~2 alkoxy, each of which may be unsubstituted or may be selected from the group consisting of one or more Z 1a may be substituted with and / or two Zs 1 together with the atom(s) to which they are attached, form C 6~10 Aryl, 5-10 membered heteroaryl, C 3~10 cycloalkyl, or 3- to 10-membered saturated or partially saturated heterocyclyl, 6~10 Aryl, heteroaryl, C 3~10 Each of the cycloalkyl and heterocyclyl may be unsubstituted or may contain one or more Z 1a and / or two Z 1 together with the atom(s) to which they are attached, form C 6~10 aryl or 5- to 10-membered heteroaryl, 6~10 Each of the aryl and heteroaryl may be unsubstituted or may contain one or more Z 1a and / or two Z 1 together with the atom(s) to which they are attached, form C 6~10 aryl or 5- to 8-membered heteroaryl, 6~10Each of the aryl and heteroaryl may be unsubstituted or may contain one or more Z 1a and / or two Z 1 can be taken together with the atom(s) to which they are attached to form a phenyl or a 5- to 6-membered heteroaryl, each of which may be unsubstituted or may be substituted with one or more Z 1a may be substituted with each Z 1a are halo, cyano, hydroxyl, C 1~6 Alkyl, C 2~6 Alkenyl, HaloC 1~6 Alkyl, HaloC 2~6 Alkenyl, C 1~6 Alkoxy, C 2~6 Alkenyloxy, C 1~6 Alkylthio, C 2~6 Alkenylthio, HaloC 1~6 Alkoxy, Hydroxy C 1~6 Alkyl, C 1~6 Alkoxy C 1~6 Alkyl, C 3~10 Cycloalkyl, C 5~10 Cycloalkenyl, C 3~10 Cycloalkyloxy, C 6~10 Aryl, C 6~10 Aryl C 1~6 Alkyl, amino, mono or di(C 1~6 alkyl)amino, mono- or di(C 1~6 Alkyl)amino C 1~6 and oxo, and preferably each Z 1a are halo, cyano, hydroxyl, C 1~6 Alkyl, HaloC 1~6 Alkyl, C 1~6 Alkoxy, C 1~6 Alkylthio, HaloC 1~6 Alkoxy, Hydroxy C 1~6 Alkyl, C 1~6 Alkoxy C 1~6 Alkyl, C 3~10 Cycloalkyl, C 3~10 Cycloalkyloxy, C 6~10Aryl, C 6~10 Aryl C 1~6 Alkyl, amino, mono or di(C 1~6 alkyl)amino, mono- or di(C 1~6 Alkyl)amino C 1~6 is independently selected from the group consisting of alkyl and oxo, and preferably each Z 1a are halo, cyano, hydroxyl, C 1~6 Alkyl, HaloC 1~6 Alkyl, C 1~6 Alkoxy, C 1~6 Alkylthio, HaloC 1~6 Alkoxy, Hydroxy C 1~6 Alkyl, C 1~6 Alkoxy C 1~6 Alkyl, C 3~10 Cycloalkyl, C 3~10 is independently selected from the group consisting of cycloalkyloxy and oxo, and preferably each Z 1a are halo, cyano, hydroxyl, C 1~6 Alkyl, HaloC 1~6 Alkyl, C 1~6 Alkoxy, HaloC 1~6 Alkoxy, Hydroxy C 1~6 A compound according to any one of statements 1 to 4, independently selected from the group consisting of alkyl and oxo.

[0178] 6. During the ceremony, R 2 is C 6~10 Aryl, 5-10 membered heteroaryl, C 3~10 Cycloalkyl, C 5~10 Cycloalkenyl, 3- to 10-membered saturated or partially saturated heterocyclyl and A 2 -X 2 -, preferably R 2 is C 6~10 Aryl, 5-10 membered heteroaryl, C 3~10 Cycloalkyl, C 5~10 Cycloalkenyl and A 2 -X 2 -, preferably R 2 is C 6~10 Aryl, 5-8 membered heteroaryl, C3~8 Cycloalkyl, C 5~8 Cycloalkenyl and A 2 -X 2 -, preferably R 2 is phenyl, 5-6 membered heteroaryl, C 3~6 Cycloalkyl, C 5~6 Cycloalkenyl and A 2 -X 2 -, preferably R 2 is phenyl, 5-6 membered heteroaryl, C 5~6 Cycloalkyl, C 5~6 Cycloalkenyl and A 2 -X 2 -, preferably R 2 is phenyl, 5-6 membered heteroaryl, cyclopentenyl and A 2 -X 2 -, preferably R 2 is phenyl or A 2 -X 2 -, preferably R 2 is A 2 -X 2 and preferably the 5-6 membered heteroaryl is selected from the group comprising pyridyl, pyrrolyl, pyrazinyl, pyridazinyl, pyrimidinyl, thiophenyl, furanyl, thiazolyl, isothiazolyl and 1,2,5-thiadiazolyl; R 2 Above C 6~10 Aryl, 5-10 membered heteroaryl, C 3~10 Cycloalkyl, C 5~10 cycloalkenyl, 3- to 10-membered saturated or partially saturated heterocyclyl, X 2 and A 2 Each of may be unsubstituted or may contain one or more Z 2 may be substituted with R 1 is hydrogen, halo, cyano, C 1~6 Alkyl, C2~6 Alkenyl, HaloC 1~6 Alkyl, HaloC 2~6 Alkenyl, C 1~6 Alkoxy, C2~6 Alkenyloxy, C 1~6 Alkylthio, C 2~6 Alkenylthio, HaloC 1~6 Alkoxy, C 1~6 Alkoxy C 1~6 Alkyl, mono or di(C 1~6 alkyl)amino and mono- or di-(C 1~6 Alkyl)amino C 1~6 alkyl, preferably R 1 is hydrogen, halo, cyano, C 1~6 Alkyl, HaloC 1~6 Alkyl, C 1~6 Alkoxy, C 1~6 Alkylthio, HaloC 1~6 Alkoxy, C 1~6 Alkoxy C 1~6 Alkyl, mono or di(C 1~6 alkyl)amino, and mono- or di-(C 1~6 Alkyl)amino C 1~6 alkyl, preferably R 1 is hydrogen, halo, cyano, C 1~6 Alkyl, HaloC 1~6 Alkyl, and C 1~6 alkoxy, preferably R 1 is hydrogen or C 1~6 alkyl, preferably R 1 is hydrogen or C 1~4 alkyl, preferably R 1 is hydrogen or C 1~2 alkyl, preferably R 1 is selected from hydrogen or methyl, preferably R 1 3. The compound of any one of statements 1 or 2, wherein:

[0179] 7. During the ceremony, X 2 -Y 2b -Y 2a -Y 2c - in which Y 2a is a single bond, a double bond, or a triple bond, or -CR 2a =CR2a -, -C≡C-, -CO-, -O-, -CS-, -S-, -SO2-, -SO-, -SO(NH)-, -CONR 2b -, -NR 2b CO-, -SO2NR 2b -, -NR 2b SO2-, -S(O)-NR 2b - and -NR 2b -, preferably selected from the group comprising X 2 is -C(R 2a )2-, -CR 2a =CR 2a -, -C≡C-, -CO-, -O-, -CS-, -S-, -SO2-, -SO-, -SO(NH)-, -CONR 2b -, -NR 2b CO-, -SO2NR 2b -, -NR 2b SO2-, -S(O)-NR 2b - and -NR 2b -, preferably selected from the group comprising X 2 is -C(R 2a )2-, -CO-, -O-, -S-, -SO2-, -SO-, or -NR 2b -, preferably X 2 is -C(R 2a )2-, -CO-, -O-, or -NR 2b -, preferably selected from the group comprising X 2 is -C(R 2a )2-, -CO-, -O- or -NR 2b -, preferably X 2 is -C(R 2a )2-, -CO- or -NR 2b and preferably X 2 -C(R 2a )2- or -CO-, preferably X 2 is -C(R 2a )2-, and preferably X 1 is -CH2-, Y 2b and Y 2c Each of the is a single bond, or C 1~3 Alkylene, C 2~3 Alkenylene, C2~3 alkynylene, wherein C is independently selected from the group consisting of 1~3 Alkylene, C 2~3 Alkenylene, C 2~3 Each alkynylene may be unsubstituted or may contain one or more R 2a where Y 2a is a single bond, a double bond, or a triple bond, Y 2b and Y 2c At least one of Y 2a is a triple bond or a double bond, Y 2b and Y 2c is not a single bond, C2 alkenylene, or C2 alkynylene, Each R 2a is hydrogen, oxo, thioxo, halo, hydroxy, haloC 1~6 Alkyl, C 1~6 Alkoxy, C 1~6 Alkoxy C 1~6 Alkyl, HaloC 1~6 Alkoxy, HaloC 1~6 Alkoxy C 1~6 Alkyl, mono or di(C 1~6 alkyl)amino, mono- or di(C 1~6 Alkyl)amino C 1~6 Alkyl, and C 1~6 alkyl, and preferably each R 2a is hydrogen, halo, hydroxy, haloC 1~6 Alkyl, C 1~6 Alkoxy, HaloC 1~6 Alkoxy, and C 1~6 alkyl, and preferably each R 2a is hydrogen, halo, hydroxy, and C 1~6 alkyl, and preferably each R 2a is hydrogen, hydroxyl or C 1~6 alkyl, and preferably each R 2a is hydrogen, hydroxyl or C 1~4 alkyl, and preferably each R 2a is hydrogen, hydroxyl or C1~2 alkyl, and preferably each R 2a are independently selected from hydrogen, hydroxyl, or methyl; A 2 is C 6~10 Aryl, 5-10 membered heteroaryl, C 3~10 Cycloalkyl, C 5~10 cycloalkenyl, and 3- to 10-membered saturated or partially saturated heterocyclyl, preferably 2 is C 6~10 Aryl, 5-10 membered heteroaryl, C 3~10 Cycloalkyl, and C 5~10 cycloalkenyl, preferably selected from the group consisting of A 2 is C 6~10 Aryl, 5-10 membered heteroaryl and C 5~10 cycloalkenyl, preferably selected from the group consisting of A 2 is C 6~10 Aryl, 5-8 membered heteroaryl, C 3~6 Cycloalkyl, and C 5~6 cycloalkenyl, preferably selected from the group consisting of A 2 is phenyl, 5-6 membered heteroaryl, C 3~6 Cycloalkyl, and C 5~6 cycloalkenyl, preferably selected from the group consisting of A 2 is selected from the group consisting of phenyl, 5- to 6-membered heteroaryl and cyclohexenyl, preferably A 2 is selected from phenyl or 5- to 6-membered heteroaryl, preferably A 2 is phenyl, and / or one R 2a is one Z 2 and together with the atom(s) to which they are attached, C 4~10 cycloalkyl, or 4- to 10-membered saturated or partially saturated heterocyclyl, or 5- to 10-membered heteroaryl, 4~10 Each cycloalkyl, heterocyclyl, or heteroaryl may be unsubstituted or may contain one or more Z 2a may be substituted with R 2b is hydrogen or C 1~6 alkyl, and preferably, each R 2b is hydrogen or C 1~4 alkyl, and preferably each R 2b is hydrogen or C 1~2 alkyl, and preferably each R 2b are independently selected from hydrogen or methyl, or R 2b is one Z 2 and together with the atom(s) to which they are attached can form a 4- to 10-membered saturated or partially saturated heterocyclyl or a 5- to 10-membered heteroaryl, each of which can be unsubstituted or can be substituted with one or more Z 2a a compound according to any one of statements 1 to 2 and 6, optionally substituted with

[0180] 8. During the ceremony, each Z 2 are independently selected from halo, cyano, hydroxy, oxo, nitro, and thioxo; or C 1~6 Alkyl, C 2~6 Alkenyl, C 3~10 Cycloalkyl, C 3~10 Cycloalkyl C 1~6 Alkyl, C 5~10 Cycloalkenyl, C 6~10 Aryl, C 6~10 Aryl C 1~6 Alkyl, HaloC 1~6 Alkyl, HaloC 2~6 Alkenyl, Cyano C 1~6 Alkyl, C 1~6 Alkoxy, C 2~6 Alkenyloxy, Cyano C 1~6 Alkoxy, C 1~6 Alkylthio, C 2~6 Alkenylthio, HaloC 1~6 Alkoxy, Hydroxy C 1~6 Alkyl, C 1~6 Alkoxy C 1~6 Alkyl, C 3~10 Cycloalkyloxy, C 3~10Cycloalkyl C 1~6 Alkoxy, C 1~6 Alkoxy C 1~6 Alkoxy, carboxyl, C 1~6 Alkoxycarbonyl, C 1~6 Alkyl carbonyl, C 6~10 Aryl C 1~6 Alkoxy, mono or di(C 1~6 alkyl)amino, mono- or di(C 1~6 Alkyl)amino C 1~6 Alkyl, mono or di(C 1~6 Alkyl)aminocarbonyl, amino C 1~6 Alkyl, 3- to 10-membered saturated or partially saturated heterocyclyl, 5- to 10-membered heteroaryl, 3- to 10-membered saturated or partially saturated heterocyclylC 1~6 Alkyl, 5-10 membered heteroarylC 1~6 Alkyl, C 6~10 Aryl C 2~6 Alkenyl, HaloC 2~6 Alkenyloxy, Hydroxy C 2~6 Alkenyl, C 2~6 Alkenyloxy C 1~6 Alkyl, C 2~6 Alkenyloxy C 1~6 Alkoxy, C 2~6 Alkenyloxycarbonyl, C 2~6 Alkenylcarbonyl, Amino C 2~6 Alkenyl, mono- or di(C 1~6 Alkyl)amino C 2~6 Alkenyl, 3-10 membered saturated or partially saturated heterocyclylC 2~6 Alkenyl, 5-10 membered heteroaryl C 2~6 Alkenyl, C 6~10 Aryloxy, C 6~10 Aryloxy C 1~6 Alkyl, C 6~10 Aryloxy C 2~6 Alkenyl, C 6~10 Arylthio, HaloC 1~6 Alkylthio, C 3~10 Cycloalkylthio, C 1~6 Alkylsulfinyl, C 1~6 Alkylsulfonyl, C 3~10Cycloalkylsulfinyl, C 3~10 Cycloalkylsulfonyl, C 6~10 Arylsulfinyl, C 6~10 Arylsulfonyl, mono- or di-(C 1~6 alkyl)aminosulfonyl, mono- or di-(C 1~6 alkyl)aminosulfinyl, C 1~6 Alkoxycarbonylamino, C 2~6 Alkenyloxycarbonylamino, C 1~6 Alkylcarbonylamino, C 2~6 Alkenylcarbonylamino, C 6~10 Cycloalkylcarbonylamino, C 6~10 Arylcarbonylamino, C 3~10 Cycloalkylcarbonyl, C 6~10 Arylcarbonyl, mono- or di(C 1~6 alkyl)aminocarbonyl, C 1~6 Alkylcarbonyloxy, C 2~6 Alkenylcarbonyloxy and C 6~10 arylcarbonyloxy, each of which may be unsubstituted or may contain one or more Z 2a and preferably, each Z 2 are independently selected from halo, cyano, oxo, and thioxo; or C 1~6 Alkyl, C 3~10 Cycloalkyl, C 6~10 Aryl, HaloC 1~6 Alkyl, Cyano C 1~6 Alkyl, C 1~6 Alkoxy, Cyano C 1~6 Alkoxy, C 1~6 Alkylthio, HaloC 1~6 Alkoxy, Hydroxy C 1~6 Alkyl, C 1~6 Alkoxy C 1~6 Alkyl, C 3~10 Cycloalkyloxy, C 3~10 Cycloalkyl C 1~6 Alkoxy, C 1~6 Alkoxy C 1~6 Alkoxy, C 1~6 Alkoxycarbonyl, C1~6 Alkyl carbonyl, C 6~10 Aryl C 1~6 Alkoxy, mono or di(C 1~6 alkyl)amino, mono- or di(C 1~6 Alkyl)amino C 1~6 Alkyl, mono or di(C 1~6 alkyl)aminocarbonyl 3-10 membered saturated or partially saturated heterocyclyl, 5-10 membered heteroaryl, 3-10 membered saturated or partially saturated heterocyclylC 1~6 Alkyl, 5-10 membered heteroarylC 1~6 Alkyl, C 6~10 Aryloxy, C 6~10 Aryloxy C 1~6 Alkyl, C 6~10 Arylthio, HaloC 1~6 Alkylthio, C 3~10 Cycloalkylthio, C 1~6 Alkylsulfinyl, C 1~6 Alkylsulfonyl, C 3~10 Cycloalkylsulfinyl, C 3~10 Cycloalkylsulfonyl, C 6~10 Arylsulfinyl, C 6~10 Arylsulfonyl, mono- or di-(C 1~6 alkyl)aminosulfonyl, mono- or di-(C 1~6 alkyl)aminosulfinyl, C 1~6 Alkoxycarbonylamino, C 1~6 Alkylcarbonylamino, C 6~10 Cycloalkylcarbonylamino, C 6~10 Arylcarbonylamino, C 3~10 Cycloalkylcarbonyl, C 6~10 Arylcarbonyl, mono- or di(C 1~6 alkyl)aminocarbonyl, C 1~6 Alkylcarbonyloxy, and C 6~10 arylcarbonyloxy, each of which may be unsubstituted or may contain one or more Z 2a and preferably, each Z 2 are independently selected from halo, cyano, and oxo; or C1~6 Alkyl, C 3~10 Cycloalkyl, C 6~10 Aryl, HaloC 1~6 Alkyl, Cyano C 1~6 Alkyl, C 1~6 Alkoxy, Cyano C 1~6 Alkoxy, C 1~6 Alkylthio, HaloC 1~6 Alkoxy, Hydroxy C 1~6 Alkyl, C 1~6 Alkoxy C 1~6 Alkyl, C 3~10 Cycloalkyloxy, C 3~10 Cycloalkyl C 1~6 Alkoxy, C 1~6 Alkoxy C 1~6 Alkoxy, C 1~6 Alkoxycarbonyl, C 1~6 Alkyl carbonyl, C 6~10 Aryl C 1~6 Alkoxy, mono or di(C 1~6 and each of the above groups may be unsubstituted or may be selected from the group consisting of one or more Z 2a and preferably, each Z 2 are independently selected from halo, cyano, and oxo; or C 1~6 Alkyl, C 3~10 Cycloalkyl, HaloC 1~6 Alkyl, Cyano C 1~6 Alkyl, C 1~6 Alkoxy, Cyano C 1~6 Alkoxy, C 1~6 Alkylthio, HaloC 1~6 Alkoxy, Hydroxy C 1~6 Alkyl, C 1~6 Alkoxy C 1~6 Alkyl, C 3~10 Cycloalkyloxy and C 3~10 Cycloalkyl C 1~6 alkoxy, each of which may be unsubstituted or may be selected from the group consisting of one or more Z 2a and preferably, each Z 2 are independently selected from halo, cyano, and oxo; or C1~6 Alkyl, HaloC 1~6 Alkyl, C 1~6 Alkoxy, C 1~6 Alkylthio, HaloC 1~6 Alkoxy, Hydroxy C 1~6 Alkyl, C 1~6 Alkoxy C 1~6 Alkyl, C 3~10 Cycloalkyloxy and C 3~10 Cycloalkyl C 1~6 alkoxy, each of which may be unsubstituted or may be selected from the group consisting of one or more Z 2a and preferably, each Z 2 are independently selected from halo, cyano, and oxo; or C 1~4 Alkyl, HaloC 1~4 Alkyl, C 1~4 Alkoxy, C 1~4 Alkylthio, HaloC 1~4 Alkoxy, Hydroxy C 1~4 Alkyl, C 1~4 Alkoxy C 1~4 Alkyl, C 3~6 Cycloalkyloxy and C 3~6 Cycloalkyl C 1~4 alkoxy, each of which may be unsubstituted or may be selected from the group consisting of one or more Z 2a and preferably, each Z 2 are independently selected from halo, cyano, and oxo; or C 1~2 Alkyl, HaloC 1~2 Alkyl, C 1~2 Alkoxy, C 1~2 Alkylthio, HaloC 1~2 Alkoxy, Hydroxy C 1~2 Alkyl, C 1~2 Alkoxy C 1~2 Alkyl, C 3~6 Cycloalkyloxy and C 3~6 Cycloalkyl C 1~2 alkoxy, each of which may be unsubstituted or may be selected from the group consisting of one or more Z 2a may be substituted with and / or two Zs 2 together with the atom(s) to which they are attached, form C 6~10 Aryl, 5-10 membered heteroaryl, C 3~10 cycloalkyl, or 3- to 10-membered saturated or partially saturated heterocyclyl, 6~10 Aryl, heteroaryl, C 3~10 Each of the cycloalkyl and heterocyclyl may be unsubstituted or may contain one or more Z 2a and / or two Z 2 together with the atom(s) to which they are attached, form C 6~10 aryl or 5- to 10-membered heteroaryl, 6~10 Each of the aryl and heteroaryl may be unsubstituted or may contain one or more Z 2a and / or two Z 2 together with the atom(s) to which they are attached, form C 6~10 aryl or 5- to 8-membered heteroaryl, 6~10 Each of the aryl and heteroaryl may be unsubstituted or may contain one or more Z 2a and / or two Z 2 can be taken together with the atom(s) to which they are attached to form a phenyl or a 5- to 6-membered heteroaryl, each of which may be unsubstituted or may be substituted with one or more Z 2a may be substituted with each Z 2a are halo, cyano, hydroxyl, C 1~6 Alkyl, C 2~6 Alkenyl, HaloC 1~6 Alkyl, HaloC 2~6 Alkenyl, C 1~6 Alkoxy, C 2~6 Alkenyloxy, C 1~6 Alkylthio, C 2~6 Alkenylthio, HaloC 1~6Alkoxy, Hydroxy C 1~6 Alkyl, C 1~6 Alkoxy C 1~6 Alkyl, C 3~10 Cycloalkyl, C 5~10 Cycloalkenyl, C 3~10 Cycloalkyloxy, C 6~10 Aryl, C 6~10 Aryl C 1~6 Alkyl, amino, mono or di(C 1~6 alkyl)amino, mono- or di(C 1~6 Alkyl)amino C 1~6 and oxo, and preferably each Z 2a are halo, cyano, hydroxyl, C 1~6 Alkyl, HaloC 1~6 Alkyl, C 1~6 Alkoxy, C 1~6 Alkylthio, HaloC 1~6 Alkoxy, Hydroxy C 1~6 Alkyl, C 1~6 Alkoxy C 1~6 Alkyl, C 3~10 Cycloalkyl, C 3~10 Cycloalkyloxy, C 6~10 Aryl, C 6~10 Aryl C 1~6 Alkyl, amino, mono or di(C 1~6 alkyl)amino, mono- or di(C 1~6 Alkyl)amino C 1~6 is independently selected from the group consisting of alkyl and oxo, and preferably each Z 2a are halo, cyano, hydroxyl, C 1~6 Alkyl, HaloC 1~6 Alkyl, C 1~6 Alkoxy, C 1~6 Alkylthio, HaloC 1~6 Alkoxy, Hydroxy C 1~6 Alkyl, C 1~6 Alkoxy C 1~6 Alkyl, C 3~10 Cycloalkyl, C 3~10 is independently selected from the group consisting of cycloalkyloxy and oxo, and preferably each Z 2aare halo, cyano, hydroxyl, C 1~6 Alkyl, HaloC 1~6 Alkyl, C 1~6 Alkoxy, HaloC 1~6 Alkoxy, Hydroxy C 1~6 A compound according to any one of statements 1-2, 6-7, independently selected from the group consisting of alkyl and oxo.

[0181] 9. During the ceremony, R 3 is hydrogen, halo, cyano, C 1~6 Alkyl, C 2~6 Alkenyl, HaloC 1~6 Alkyl, HaloC 2~6 Alkenyl, C 1~6 Alkoxy, C 2~6 Alkenyloxy, C 1~6 Alkylthio, C 2~6 Alkenylthio, HaloC 1~6 Alkoxy, C 1~6 Alkoxy C 1~6 Alkyl, mono or di(C 1~6 alkyl)amino, and mono- or di-(C 1~6 Alkyl)amino C 1~6 alkyl, preferably R 3 is hydrogen, halo, cyano, C 1~6 Alkyl, HaloC 1~6 Alkyl, C 1~6 Alkoxy, HaloC 1~6 Alkoxy, C 1~6 Alkoxy C 1~6 Alkyl, mono or di(C 1~6 alkyl)amino, and mono- or di-(C 1~6 Alkyl)amino C 1~6 alkyl, preferably R 3 is hydrogen, halo, cyano, C 1~6 Alkyl, HaloC 1~6 Alkyl, C 1~6 Alkoxy and HaloC 1~6 alkoxy, preferably R 3 is hydrogen, halo, cyano and C 1~6 alkyl, preferably R3 is hydrogen or C 1~6 alkyl, preferably R 3 is hydrogen or C 1~4 alkyl, preferably R 3 is hydrogen or C 1~2 alkyl, preferably R 3 is selected from hydrogen or methyl, preferably R 3 is hydrogen.

[0182] 10. During the ceremony, R 4 is C 6~10 aryl or 5- to 10-membered heteroaryl, preferably R 4 is C 6~10 aryl or 5- to 8-membered heteroaryl, preferably R 4 is phenyl or 5-6 membered heteroaryl, preferably 5-6 membered heteroaryl is selected from the group comprising pyridyl, pyrrolyl, pyrazinyl, pyridazinyl, pyrimidinyl, thiophenyl, furanyl, thiazolyl, isothiazolyl and 1,2,5-thiadiazolyl, phenyl or pyridyl; Above C 6~10 Each of the aryl and 5- to 10-membered heteroaryl may be one or more Z 4 and preferably, 6~10 Each of the aryl and 5- to 10-membered heteroaryl may have two or more Z 4 10. The compound of any one of statements 1 to 9, substituted with:

[0183] 11. During the ceremony, each Z 4 are independently selected from halo, cyano, hydroxyl, oxo, nitro, and thioxo; or C 1~6 Alkyl, C 2~6 Alkenyl, C 3~10 Cycloalkyl, C 3~10 Cycloalkyl C 1~6 Alkyl, C 5~10 Cycloalkenyl, C 6~10 Aryl, C 6~10Aryl C 1~6 Alkyl, HaloC 1~6 Alkyl, HaloC 2~6 Alkenyl, Cyano C 1~6 Alkyl, C 1~6 Alkoxy, C 2~6 Alkenyloxy, Cyano C 1~6 Alkoxy, C 1~6 Alkylthio, C 2~6 Alkenylthio, HaloC 1~6 Alkoxy, Hydroxy C 1~6 Alkyl, C 1~6 Alkoxy C 1~6 Alkyl, C 3~10 Cycloalkyloxy, C 3~10 Cycloalkyl C 1~6 Alkoxy, C 1~6 Alkoxy, carboxyl, C 1~6 Alkoxycarbonyl, C 1~6 Alkyl carbonyl, C 6~10 Aryl C 1~6 Alkoxy, mono or di(C 1~6 alkyl)amino, mono- or di(C 1~6 Alkyl)amino C 1~6 Alkyl, mono or di(C 1~6 Alkyl)aminocarbonyl, amino C 1~6 Alkyl, amino, 3- to 10-membered saturated or partially saturated heterocyclyl, 5- to 10-membered heteroaryl, 3- to 10-membered saturated or partially saturated heterocyclylC 1~6 Alkyl, 5-10 membered heteroarylC 1~6 Alkyl, C 6~10 Aryl C 2~6 Alkenyl, HaloC 2~6 Alkenyloxy, Hydroxy C 2~6 Alkenyl, C 2~6 Alkenyloxy C 1~6 Alkyl, C 2~6 Alkenyloxy C 1~6 Alkoxy, C 2~6 Alkenyloxycarbonyl, C 2~6 Alkenylcarbonyl, Amino C 2~6 Alkenyl, mono- or di(C 1~6 Alkyl)amino C 2~6Alkenyl, 3-10 membered saturated or partially saturated heterocyclylC 2~6 Alkenyl, 5-10 membered heteroaryl C 2~6 Alkenyl, C 6~10 Aryloxy, C 6~10 Aryloxy C 1~6 Alkyl, C 6~10 Aryloxy C 2~6 Alkenyl, C 6~10 Arylthio, HaloC 1~6 Alkylthio, C 3~10 Cycloalkylthio, C 1~6 Alkylsulfinyl, C 1~6 Alkylsulfonyl, C 3~10 Cycloalkylsulfinyl, C 3~10 Cycloalkylsulfonyl, C 6~10 Arylsulfinyl, C 6~10 Arylsulfonyl, mono- or di-(C 1~6 alkyl)aminosulfonyl, mono- or di-(C 1~6 alkyl)aminosulfinyl, C 1~6 Alkoxycarbonylamino, C 2~6 Alkenyloxycarbonylamino, C 1~6 Alkylcarbonylamino, C 2~6 Alkenylcarbonylamino, C 6~10 Cycloalkylcarbonylamino, C 6~10 Arylcarbonylamino, C 3~10 Cycloalkylcarbonyl, C 6~10 Arylcarbonyl, mono- or di(C 1~6 alkyl)aminocarbonyl, C 1~6 Alkylcarbonyloxy, C 2~6 Alkenylcarbonyloxy, and C 6~10 arylcarbonyloxy, each of which may be unsubstituted or may contain one or more Z 4a and preferably, each Z 4 are independently selected from halo, cyano, hydroxyl, oxo, nitro, and thioxo; or C 1~6 Alkyl, C 3~10 Cycloalkyl, C 3~10Cycloalkyl C 1~6 Alkyl, C 6~10 Aryl, C 6~10 Aryl C 1~6 Alkyl, HaloC 1~6 Alkyl, Cyano C 1~6 Alkyl, C 1~6 Alkoxy, Cyano C 1~6 Alkoxy, C 1~6 Alkylthio, HaloC 1~6 Alkoxy, Hydroxy C 1~6 Alkyl, C 1~6 Alkoxy C 1~6 Alkyl, C 3~10 Cycloalkyloxy, C 3~10 Cycloalkyl C 1~6 Alkoxy, C 1~6 Alkoxy C 1~6 Alkoxy, carboxyl, C 1~6 Alkoxycarbonyl, C 1~6 Alkyl carbonyl, C 6~10 Aryl C 1~6 Alkoxy, mono or di(C 1~6 alkyl)amino, mono- or di(C 1~6 Alkyl)amino C 1~6 Alkyl, mono or di(C 1~6 Alkyl)aminocarbonyl, amino C 1~6 Alkyl, amino, 3- to 10-membered saturated or partially saturated heterocyclyl, 5- to 10-membered heteroaryl, 3- to 10-membered saturated or partially saturated heterocyclylC 1~6 Alkyl, 5-10 membered heteroarylC 1~6 Alkyl, C 6~10 Aryloxy, C 6~10 Aryloxy C 1~6 Alkyl, C 6~10 Arylthio, HaloC 1~6 Alkylthio, C 3~10 Cycloalkylthio, C 1~6 Alkylsulfinyl, C 1~6 Alkylsulfonyl, C 3~10 Cycloalkylsulfinyl, C 3~10 Arylsulfonyl, C 6~10 Arylsulfinyl, C 6~10 Arylsulfonyl, mono- or di-(C1~6 alkyl)aminosulfonyl, mono- or di-(C 1~6 alkyl)aminosulfinyl, C 1~6 Alkoxycarbonylamino, C 1~6 Alkylcarbonylamino, C 6~10 Cycloalkylcarbonylamino, C 6~10 Arylcarbonylamino, C 3~10 Cycloalkylcarbonyl, C 6~10 Arylcarbonyl, mono- or di(C 1~6 alkyl)aminocarbonyl, C 1~6 Alkylcarbonyloxy, and C 6~10 arylcarbonyloxy, each of which may be unsubstituted or may contain one or more Z 4a and preferably, each Z 4 are independently selected from halo, cyano, hydroxyl, oxo, nitro, and thioxo; or C 1~6 Alkyl, C 3~10 Cycloalkyl, C 3~10 Cycloalkyl C 1~6 Alkyl, C 6~10 Aryl, C 6~10 Aryl C 1~6 Alkyl, HaloC 1~6 Alkyl, Cyano C 1~6 Alkyl, C 1~6 Alkoxy, Cyano C 1~6 Alkoxy, C 1~6 Alkylthio, HaloC 1~6 Alkoxy, Hydroxy C 1~6 Alkyl, C 1~6 Alkoxy C 1~6 Alkyl, C 3~10 Cycloalkyloxy, C 3~10 Cycloalkyl C 1~6 Alkoxy, C 1~6 Alkoxy C 1~6 Alkoxy, carboxyl, C 1~6 Alkoxycarbonyl, C 1~6 Alkyl carbonyl, C 6~10 Aryl C 1~6Alkoxy, 3- to 10-membered saturated or partially saturated heterocyclyl, 5- to 10-membered heteroaryl, 3- to 10-membered saturated or partially saturated heterocyclylC 1~6 Alkyl and 5-10 membered heteroaryl C 1~6 alkyl, each of the above groups may be unsubstituted or may contain one or more Z 4a and preferably, each Z 4 are independently selected from halo, cyano, hydroxyl, oxo, and thioxo; or C 1~6 Alkyl, C 3~10 Cycloalkyl, C 3~10 Cycloalkyl C 1~6 Alkyl, C 6~10 Aryl, C 6~10 Aryl C 1~6 Alkyl, HaloC 1~6 Alkyl, Cyano C 1~6 Alkyl, C 1~6 Alkoxy, Cyano C 1~6 Alkoxy, C 1~6 Alkylthio, HaloC 1~6 Alkoxy, Hydroxy C 1~6 Alkyl, C 1~6 Alkoxy C 1~6 Alkyl, C 3~10 Cycloalkyloxy, C 3~10 Cycloalkyl C 1~6 Alkoxy, C 1~6 Alkoxy, carboxyl, C 1~6 Alkoxycarbonyl, C 1~6 Alkyl carbonyl, C 6~10 Aryl C 1~6 alkoxy, each of which may be unsubstituted or may be selected from the group consisting of one or more Z 4a and preferably, each Z 4 are independently selected from halo, cyano, hydroxyl, oxo, or C 1~6 Alkyl, C 3~10 Cycloalkyl, C 3~10 Cycloalkyl C 1~6 Alkyl, C 6~10 Aryl, C 6~10 Aryl C 1~6Alkyl, HaloC 1~6 Alkyl, Cyano C 1~6 Alkyl, C 1~6 Alkoxy, Cyano C 1~6 Alkoxy, HaloC 1~6 Alkoxy, C 1~6 Alkoxy C 1~6 Alkyl, C 3~10 Cycloalkyloxy, C 3~10 Cycloalkyl C 1~6 Alkoxy, C 1~6 Alkoxy C 1~6 Alkoxy, C 1~6 Alkoxycarbonyl, C 1~6 alkylcarbonyl, each of which may be unsubstituted or may contain one or more Z 4a and preferably, each Z 4 are independently selected from halo, cyano, and oxo; or C 1~6 Alkyl, C 3~10 Cycloalkyl, C 6~10 Aryl, HaloC 1~6 Alkyl, Cyano C 1~6 Alkyl, C 1~6 Alkoxy, Cyano C 1~6 Alkoxy, HaloC 1~6 Alkoxy, C 1~6 Alkoxy C 1~6 Alkyl, C 3~10 Cycloalkyloxy, C 1~6 Alkoxycarbonyl, C 1~6 alkylcarbonyl, each of which may be unsubstituted or may contain one or more Z 4a and preferably, each Z 4 are independently selected from halo, cyano, and oxo; or C 1~4 Alkyl, C 3~6 Cycloalkyl, C 6~10 Aryl, HaloC 1~4 Alkyl, Cyano C 1~4 Alkyl, C 1~4 Alkoxy, Cyano C 1~4 Alkoxy, HaloC 1~4 Alkoxy, C 1~4 Alkoxy C 1~4 Alkyl, C 3~6 Cycloalkyloxy, C 1~4 Alkoxycarbonyl, C 1~4 alkylcarbonyl, each of which may be unsubstituted or may contain one or more Z 4a and preferably, each Z 4 are independently selected from halo, cyano, and oxo; or C 1~2 Alkyl, C 3~6 Cycloalkyl, phenyl, haloC 1~2 Alkyl, Cyano C 1~2 Alkyl, C 1~2 Alkoxy, Cyano C 1~2 Alkoxy, HaloC 1~2 Alkoxy, C 1~2 Alkoxy C 1~2 Alkyl, C 3~6 Cycloalkyloxy, C 1~2 Alkoxycarbonyl, C 1~2 alkylcarbonyl, each of which may be unsubstituted or may contain one or more Z 4a may be substituted with and / or two Zs 4 together with the atom(s) to which they are attached, form C 6~10 Aryl, 5-10 membered heteroaryl, C 3~10 cycloalkyl, or 3- to 10-membered saturated or partially saturated heterocyclyl, 6~10 Aryl, heteroaryl, C 3~10 Each of the cycloalkyl and heterocyclyl may be unsubstituted or may contain one or more Z 4a and / or two Z 4 together with the atom(s) to which they are attached, form C 6~10 Aryl, 5-8 membered heteroaryl, C 3~10 cycloalkyl, or 3- to 8-membered saturated heterocyclyl, 6~10 Aryl, heterocyclyl, C 3~10Each of the cycloalkyl and heteroaryl may be unsubstituted or may contain one or more Z 4a and / or two Z 4 together with the atom(s) to which they are attached, are phenyl, 5- to 6-membered heteroaryl, C 3~6 Each of the phenyl, heterocyclyl, cycloalkyl, and heteroaryl may be unsubstituted or may be substituted with one or more Z 4a may be substituted with each Z 4a are halo, cyano, hydroxyl, C 1~6 Alkyl, C 2~6 Alkenyl, HaloC 1~6 Alkyl, HaloC 2~6 Alkenyl, C 1~6 Alkoxy, C 2~6 Alkenyloxy, C 1~6 Alkylthio, C 2~6 Alkenylthio, HaloC 1~6 Alkoxy, Hydroxy C 1~6 Alkyl, C 1~6 Alkoxy C 1~6 Alkyl, C 3~10 Cycloalkyl, C 5~10 Cycloalkenyl, C 3~10 Cycloalkyloxy, C 6~10 Aryl, C 6~10 Aryl C 1~6 Alkyl, amino, mono or di(C 1~6 alkyl)amino, mono- or di(C 1~6 Alkyl)amino C 1~6 is independently selected from the group consisting of alkyl and oxo, and preferably each Z 4a are halo, cyano, hydroxyl, C 1~6 Alkyl, HaloC 1~6 Alkyl, C 1~6 Alkoxy, C 1~6 Alkylthio, HaloC 1~6 Alkoxy, Hydroxy C 1~6 Alkyl, C 1~6 Alkoxy C 1~6 Alkyl, C3~10 Cycloalkyl, C 3~10 Cycloalkyloxy, C 6~10 Aryl, C 6~10 Aryl C 1~6 Alkyl, amino, mono or di(C 1~6 alkyl)amino, mono- or di(C 1~6 Alkyl)amino C 1~6 The compound of any one of statements 1-10, wherein the aryl group is independently selected from alkyl, and oxo.

[0184] 12. During the ceremony, R 1 is C 6~10 Aryl, 5-10 membered heteroaryl, C 3~10 Cycloalkyl, C 5~10 Cycloalkenyl, 3- to 10-membered saturated or partially saturated heterocyclyl, and A 1 -X 1 -, and R 2 is hydrogen, halo, cyano, C 1~6 Alkyl, C 2~6 Alkenyl, HaloC 1~6 Alkyl, HaloC 2~6 Alkenyl, C 1~6 Alkoxy, C 2~6 Alkenyloxy, C 1~6 Alkylthio, C 2~6 Alkenylthio, HaloC 1~6 Alkoxy, C 1~6 Alkoxy C 1~6 Alkyl, mono or di(C 1~6 alkyl)amino, and mono- or di-(C 1~6 Alkyl)amino C 1~6 is selected from the group including alkyl, R 1 Above C 6~10 Aryl, 5-10 membered heteroaryl, C 3~10 Cycloalkyl, C 5~10 cycloalkenyl, 3- to 10-membered saturated or partially saturated heterocyclyl, X 1 and A 1 Each of may be unsubstituted or may contain one or more Z 1 may be substituted with X1 is -C(R 1a )2-, -CO-, -O- or -NR 1b - selected from Each R 1a is hydrogen, halo, hydroxy, and C 1~6 independently selected from the group consisting of alkyl, A 1 is C 6~10 Aryl, 5-10 membered heteroaryl, C 3~10 Cycloalkyl, C 5~10 selected from the group consisting of cycloalkenyl, and 3- to 10-membered saturated or partially saturated heterocyclyl; each Z 1 are independently selected from halo, cyano, hydroxy, oxo, nitro, and thioxo; or C 1~6 Alkyl, C 2~6 Alkenyl, C 3~10 Cycloalkyl, C 3~10 Cycloalkyl C 1~6 Alkyl, C 5~10 Cycloalkenyl, C 6~10 Aryl, C 6~10 Aryl C 1~6 Alkyl, HaloC 1~6 Alkyl, HaloC 2~6 Alkenyl, Cyano C 1~6 Alkyl, C 1~6 Alkoxy, C 2~6 Alkenyloxy, Cyano C 1~6 Alkoxy, C 1~6 Alkylthio, C 2~6 Alkenylthio, HaloC 1~6 Alkoxy, Hydroxy C 1~6 Alkyl, C 1~6 Alkoxy C 1~6 Alkyl, C 3~10 Cycloalkyloxy, C 3~10 Cycloalkyl C 1~6 Alkoxy, C 1~6 Alkoxy, carboxyl, C 1~6 Alkoxycarbonyl, C 1~6 Alkyl carbonyl, C 6~10 Aryl C 1~6 Alkoxy, mono or di(C 1~6alkyl)amino, mono- or di(C 1~6 Alkyl)amino C 1~6 Alkyl, mono or di(C 1~6 Alkyl)aminocarbonyl, amino C 1~6 Alkyl, amino, 3- to 10-membered saturated or partially saturated heterocyclyl, 5- to 10-membered heteroaryl, 3- to 10-membered saturated or partially saturated heterocyclylC 1~6 Alkyl and 5-10 membered heteroaryl C 1~6 Alkyl, C 6~10 Aryl C 2~6 Alkenyl, HaloC 2~6 Alkenyloxy, Hydroxy C 2~6 Alkenyl, C 2~6 Alkenyloxy C 1~6 Alkyl, C 2~6 Alkenyloxy C 1~6 Alkoxy, C 2~6 Alkenyloxycarbonyl, C 2~6 Alkenylcarbonyl, Amino C 2~6 Alkenyl, mono- or di(C 1~6 Alkyl)amino C 2~6 Alkenyl, 3-10 membered saturated or partially saturated heterocyclylC 2~6 Alkenyl, 5-10 membered heteroaryl C 2~6 Alkenyl, C 6~10 Aryloxy, C 6~10 Aryloxy C 1~6 Alkyl, C 6~10 Aryloxy C 2~6 Alkenyl, C 6~10 Arylthio, HaloC 1~6 Alkylthio, C 3~10 Cycloalkylthio, C 1~6 Alkylsulfinyl, C 1~6 Alkylsulfonyl, C 3~10 Cycloalkylsulfinyl, C 3~10 Cycloalkylsulfonyl, C 6~10 Arylsulfinyl, C 6~10 Arylsulfonyl, mono- or di-(C 1~6 alkyl)aminosulfonyl, mono- or di-(C 1~6 alkyl)aminosulfinyl, C 1~6Alkoxycarbonylamino, C 2~6 Alkenyloxycarbonylamino, C 1~6 alkylcarbonylamino, C2~6 Alkenylcarbonylamino, C 6~10 Cycloalkylcarbonylamino, C 6~10 Arylcarbonylamino, C 3~10 Cycloalkylcarbonyl, C 6~10 Arylcarbonyl, mono- or di(C 1~6 alkyl)aminocarbonyl, C 1~6 Alkylcarbonyloxy, C 2~6 Alkenylcarbonyloxy, and C 6~10 arylcarbonyloxy, each of which may be unsubstituted or may contain one or more Z 1a may be substituted with and / or two Zs 1 together with the atom(s) to which they are attached, form C 6~10 Aryl, 5-10 membered heteroaryl, C 3~10 cycloalkyl, or 3- to 10-membered saturated or partially saturated heterocyclyl, 6~10 Aryl, heteroaryl, C 3~10 Each of the cycloalkyl and heterocyclyl may be unsubstituted or may contain one or more Z 1a may be substituted with and / or one R 1a is one Z 1 and together with the atom(s) to which they are attached, C 4~10 cycloalkyl, or 4- to 10-membered saturated or partially saturated heterocyclyl, or 5- to 10-membered heteroaryl, 4~10 Each cycloalkyl, heterocyclyl, or heteroaryl may be unsubstituted or may contain one or more Z 1a may be substituted with R 1b is hydrogen or C 1~6 alkyl or R 1b is one Z 1and together with the atom(s) to which they are attached can form a 4- to 10-membered saturated or partially saturated heterocyclyl or a 5- to 10-membered heteroaryl, each of which can be unsubstituted or can be substituted with one or more Z 1a may be substituted with each Z 1a are halo, cyano, hydroxyl, C 1~6 Alkyl, C 2~6 Alkenyl, HaloC 1~6 Alkyl, HaloC 2~6 Alkenyl, C 1~6 Alkoxy, C 2~6 Alkenyloxy, C 1~6 Alkylthio, C 2~6 Alkenylthio, C 2~6 Alkynylthio, HaloC 1~6 Alkoxy, Hydroxy C 1~6 Alkyl, C 1~6 Alkoxy C 1~6 Alkyl, C 3~10 Cycloalkyl, C 5~10 Cycloalkenyl, C 3~10 Cycloalkyloxy, C 6~10 Aryl, C 6~10 Aryl C 1~6 Alkyl, amino, mono or di(C 1~6 alkyl)amino, mono- or di(C 1~6 Alkyl)amino C 1~6 independently selected from the group consisting of alkyl, and oxo; Or R 1 is hydrogen, halo, cyano, C 1~6 Alkyl, C 2~6 Alkenyl, HaloC 1~6 Alkyl, HaloC 2~6 Alkenyl, C 1~6 Alkoxy, C 2~6 Alkenyloxy, C 1~6 Alkylthio, C 2~6 Alkenylthio, HaloC 1~6 Alkoxy, C 1~6 Alkoxy C 1~6 Alkyl, mono or di(C 1~6 alkyl)amino, and mono- or di-(C1~6 Alkyl)amino C 1~6 alkyl, R 2 is C 6~10 Aryl, 5-10 membered heteroaryl, C 3~10 Cycloalkyl, C 5~10 Cycloalkenyl, 3- to 10-membered saturated or partially saturated heterocyclyl, and A 2 -X 2 - selected from the group comprising R 2 Above C 6~10 Aryl, 5-10 membered heteroaryl, C 3~10 Cycloalkyl, C 5~10 cycloalkenyl, 3- to 10-membered saturated or partially saturated heterocyclyl, X 2 and A 2 Each of may be unsubstituted or may contain one or more Z 2 may be substituted with X 2 is -C(R 2a )2-, -CO-, -O- or -NR 2b wherein each R 2a is hydrogen, halo, hydroxy and C 1~6 independently selected from the group consisting of alkyl, A 2 is C 6~10 Aryl, 5-10 membered heteroaryl, C 3~10 Cycloalkyl, C 5~10 selected from the group consisting of cycloalkenyl, and 3- to 10-membered saturated or partially saturated heterocyclyl; each Z 2 are independently selected from halo, cyano, hydroxy, oxo, nitro, and thioxo; or C 1~6 Alkyl, C 2~6 Alkenyl, C 3~10 Cycloalkyl, C 3~10 Cycloalkyl C 1~6 Alkyl, C 5~10 Cycloalkenyl, C 6~10 Aryl, C 6~10 Aryl C 1~6 Alkyl, HaloC 1~6 Alkyl, HaloC 2~6 Alkenyl, Cyano C1~6 Alkyl, C 1~6 Alkoxy, C 2~6 Alkenyloxy, Cyano C 1~6 Alkoxy, C 1~6 Alkylthio, C 2~6 Alkenylthio, HaloC 1~6 Alkoxy, Hydroxy C 1~6 Alkyl, C 1~6 Alkoxy C 1~6 Alkyl, C 3~10 Cycloalkyloxy, C 3~10 Cycloalkyl C 1~6 Alkoxy, C 1~6 Alkoxy, carboxyl, C 1~6 Alkoxycarbonyl, C 1~6 Alkyl carbonyl, C 6~10 Aryl C 1~6 Alkoxy, mono or di(C 1~6 alkyl)amino, mono- or di(C 1~6 Alkyl)amino C 1~6 Alkyl, mono or di(C 1~6 Alkyl)aminocarbonyl, amino C 1~6 Alkyl, amino, 3- to 10-membered saturated or partially saturated heterocyclyl, 5- to 10-membered heteroaryl, 3- to 10-membered saturated or partially saturated heterocyclylC 1~6 Alkyl, 5-10 membered heteroarylC 1~6 Alkyl, C 6~10 Aryl C 2~6 Alkenyl, HaloC 2~6 Alkenyloxy, Hydroxy C 2~6 Alkenyl, C 2~6 Alkenyloxy C 1~6 Alkyl, C 2~6 Alkenyloxy C 1~6 Alkoxy, C 2~6 Alkenyloxycarbonyl, C 2~6 Alkenylcarbonyl, Amino C 2~6 Alkenyl, mono- or di(C 1~6 Alkyl)amino C 2~6 Alkenyl, 3-10 membered saturated or partially saturated heterocyclylC 2~6 Alkenyl, 5-10 membered heteroaryl C 2~6 Alkenyl, C6~10 Aryloxy, C 6~10 Aryloxy C 1~6 Alkyl, C 6~10 Aryloxy C 2~6 Alkenyl, C 6~10 Arylthio, HaloC 1~6 Alkylthio, C 3~10 Cycloalkylthio, C 1~6 Alkylsulfinyl, C 1~6 Alkylsulfonyl, C 3~10 Cycloalkylsulfinyl, C 3~10 Cycloalkylsulfonyl, C 6~10 Arylsulfinyl, C 6~10 Arylsulfonyl, mono- or di-(C 1~6 alkyl)aminosulfonyl, mono- or di-(C 1~6 alkyl)aminosulfinyl, C 1~6 Alkoxycarbonylamino, C 2~6 Alkenyloxycarbonylamino, C 1~6 alkylcarbonylamino, C2~6 Alkenylcarbonylamino, C 6~10 Cycloalkylcarbonylamino, C 6~10 Arylcarbonylamino, C 3~10 Cycloalkylcarbonyl, C 6~10 Arylcarbonyl, mono- or di(C 1~6 alkyl)aminocarbonyl, C 1~6 Alkylcarbonyloxy, C 2~6 Alkenylcarbonyloxy, and C 6~10 arylcarbonyloxy, each of which may be unsubstituted or may contain one or more Z 2a may be substituted with and / or two Zs 2 together with the atom(s) to which they are attached, form C 6~10 Aryl, 5-10 membered heteroaryl, C 3~10 cycloalkyl, or 3- to 10-membered saturated or partially saturated heterocyclyl, 6~10 Aryl, heteroaryl, C 3~10Each of the cycloalkyl and heterocyclyl may be unsubstituted or may contain one or more Z 2a may be substituted with and / or one R 2a is one Z 2 and together with the atom(s) to which they are attached, C 4~10 cycloalkyl, or 4- to 10-membered saturated or partially saturated heterocyclyl, or 5- to 10-membered heteroaryl, 4~10 Each cycloalkyl, heterocyclyl, or heteroaryl may be unsubstituted or may contain one or more Z 2a may be substituted with R 2b is hydrogen or C 1~6 alkyl or R 2b is one Z 2 and together with the atom(s) to which they are attached can form a 4- to 10-membered saturated or partially saturated heterocyclyl or a 5- to 10-membered heteroaryl, each of which can be unsubstituted or can be substituted with one or more Z 2a may be substituted with each Z 2a are halo, cyano, hydroxyl, C 1~6 Alkyl, C 2~6 Alkenyl, HaloC 1~6 Alkyl, HaloC 2~6 Alkenyl, C 1~6 Alkoxy, C 2~6 Alkenyloxy, C 1~6 Alkylthio, C 2~6 Alkenylthio, C 2~6 Alkynylthio, HaloC 1~6 Alkoxy, Hydroxy C 1~6 Alkyl, C 1~6 Alkoxy C 1~6 Alkyl, C 3~10 Cycloalkyl, C 5~10 Cycloalkenyl, C 3~10 Cycloalkyloxy, C 6~10 Aryl, C 6~10 Aryl C 1~6 Alkyl, amino, mono or di(C1~6 alkyl)amino, mono- or di(C 1~6 Alkyl)amino C 1~6 independently selected from the group consisting of alkyl, and oxo; R 3 is hydrogen, halo, cyano, C 1~6 Alkyl, C 2~6 Alkenyl, HaloC 1~6 Alkyl, HaloC 2~6 Alkenyl, C 1~6 Alkoxy, C 2~6 Alkenyloxy, C 1~6 Alkylthio, C 2~6 Alkenylthio, HaloC 1~6 Alkoxy, C 1~6 Alkoxy C 1~6 Alkyl, mono or di(C 1~6 alkyl)amino, and mono- or di-(C 1~6 Alkyl)amino C 1~6 is selected from the group including alkyl, R 4 is C 6~10 aryl or 5- to 10-membered heteroaryl; Above C 6~10 Each of the aryl and 5- to 10-membered heteroaryl may be one or more Z 4 is replaced by each Z 4 are independently selected from halo, cyano, hydroxy, oxo, nitro, and thioxo; or C 1~6 Alkyl, C2 ~6 Alkenyl, C 3~10 Cycloalkyl, C 3~10 Cycloalkyl C 1~6 Alkyl, C 5~10 Cycloalkenyl, C 6~10 Aryl, C 6~10 Aryl C 1~6 Alkyl, HaloC 1~6 Alkyl, HaloC 2~6 Alkenyl, Cyano C 1~6 Alkyl, C 1~6 Alkoxy, C 2~6 Alkenyloxy, Cyano C 1~6 Alkoxy, C 1~6 Alkylthio, C2~6 Alkenylthio, HaloC 1~6 Alkoxy, Hydroxy C 1~6 Alkyl, C 1~6 Alkoxy C 1~6 Alkyl, C 3~10 Cycloalkyloxy, C 3~10 Cycloalkyl C 1~6 Alkoxy, C 1~6 Alkoxy, carboxyl, C 1~6 Alkoxycarbonyl, C 1~6 Alkyl carbonyl, C 6~10 Aryl C 1~6 Alkoxy, mono or di(C 1~6 alkyl)amino, mono- or di(C 1~6 Alkyl)amino C 1~6 Alkyl, mono or di(C 1~6 Alkyl)aminocarbonyl, amino C 1~6 Alkyl, amino, 3- to 10-membered saturated or partially saturated heterocyclyl, 5- to 10-membered heteroaryl, 3- to 10-membered saturated or partially saturated heterocyclylC 1~6 Alkyl, 5-10 membered heteroarylC 1~6 Alkyl, C 6~10 Aryl C 2~6 Alkenyl, HaloC 2~6 Alkenyloxy, Hydroxy C 2~6 Alkenyl, C 2~6 Alkenyloxy C 1~6 Alkyl, C 2~6 Alkenyloxy C 1~6 Alkoxy, C 2~6 Alkenyloxycarbonyl, C 2~6 Alkenylcarbonyl, Amino C 2~6 Alkenyl, mono- or di(C 1~6 Alkyl)amino C 2~6 Alkenyl, 3-10 membered saturated or partially saturated heterocyclylC 2~6 Alkenyl, 5-10 membered heteroaryl C 2~6 Alkenyl, C 6~10 Aryloxy, C 6~10 Aryloxy C 1~6 Alkyl, C 6~10 Aryloxy C 2~6 Alkenyl, C6~10 Arylthio, HaloC 1~6 Alkylthio, C 3~10 Cycloalkylthio, C 1~6 Alkylsulfinyl, C 1~6 Alkylsulfonyl, C 3~10 Cycloalkylsulfinyl, C 3~10 Cycloalkylsulfonyl, C 6~10 Arylsulfinyl, C 6~10 Arylsulfonyl, mono- or di-(C 1~6 alkyl)aminosulfonyl, mono- or di-(C 1~6 alkyl)aminosulfinyl, C 1~6 Alkoxycarbonylamino, C 2~6 Alkenyloxycarbonylamino, C 1~6 alkylcarbonylamino, C2~6 Alkenylcarbonylamino, C 6~10 Cycloalkylcarbonylamino, C 6~10 Arylcarbonylamino, C 3~10 Cycloalkylcarbonyl, C 6~10 Arylcarbonyl, mono- or di(C 1~6 alkyl)aminocarbonyl, C 1~6 Alkylcarbonyloxy, C 2~6 Alkenylcarbonyloxy, and C 6~10 arylcarbonyloxy, each of which may be unsubstituted or may contain one or more Z 4a may be substituted with and / or two Zs 4 together with the atom(s) to which they are attached, form C 6~10 Aryl, 5-10 membered heteroaryl, C 3~10 cycloalkyl, or 3- to 10-membered saturated or partially saturated heterocyclyl, 6~10 Aryl, heteroaryl, C 3~10 Each of the cycloalkyl and heterocyclyl may be unsubstituted or may contain one or more Z 4a may be substituted with each Z 4a are halo, cyano, hydroxyl, C1~6 Alkyl, C 2~6 Alkenyl, HaloC 1~6 Alkyl, HaloC 2~6 Alkenyl, C 1~6 Alkoxy, C 2~6 Alkenyloxy, C 1~6 Alkylthio, C 2~6 Alkenylthio, C 2~6 Alkynylthio, HaloC 1~6 Alkoxy, Hydroxy C 1~6 Alkyl, C 1~6 Alkoxy C 1~6 Alkyl, C 3~10 Cycloalkyl, C 5~10 Cycloalkenyl, C 3~10 Cycloalkyloxy, C 6~10 Aryl, C 6~10 Aryl C 1~6 Alkyl, amino, mono or di(C 1~6 alkyl)amino, mono- or di(C 1~6 Alkyl)amino C 1~6 The compound of any one of statements 1-11, wherein the aryl group is independently selected from the group consisting of alkyl, and oxo.

[0185] 13. During the ceremony, R 1 is C 6~10 Aryl, 5-10 membered heteroaryl, C 3~10 Cycloalkyl, C 5~10 Cycloalkenyl, 3- to 10-membered saturated or partially saturated heterocyclyl, and A 1 -X 1 -, and R 2 is hydrogen, halo, cyano, C 1~6 Alkyl, HaloC 1~6 Alkyl, C 1~6 Alkoxy, C 1~6 Alkylthio, HaloC 1~6 Alkoxy, C 1~6 Alkoxy C 1~6 Alkyl, mono or di(C 1~6 alkyl)amino, and mono- or di-(C 1~6 Alkyl)amino C 1~6 is selected from the group including alkyl, R 1 Above C 6~10 Aryl, 5-10 membered heteroaryl, C 3~10 Cycloalkyl, C 5~10 cycloalkenyl, 3- to 10-membered saturated or partially saturated heterocyclyl, X 1 and A 1 Each of may be unsubstituted or may contain one or more Z 1 may be substituted with X 1 is -C(R 1a )2-, -CO-, -O- or -NR 1b - selected from Each R 1a is hydrogen, halo, hydroxy, and C 1~6 independently selected from the group consisting of alkyl, A 1 is C 6~10 Aryl, 5-10 membered heteroaryl, C 3~10 Cycloalkyl, C 5~10 selected from the group consisting of cycloalkenyl, and 3- to 10-membered saturated or partially saturated heterocyclyl; each Z 1 are independently selected from halo, cyano, hydroxy, oxo, nitro, and thioxo; or C 1~6 Alkyl, C 3~10 Cycloalkyl, C 3~10 Cycloalkyl C 1~6 Alkyl, C 6~10 Aryl, C 6~10 Aryl C 1~6 Alkyl, HaloC 1~6 Alkyl, Cyano C 1~6 Alkyl, C 1~6 Alkoxy, Cyano C 1~6 Alkoxy, C 1~6 Alkylthio, HaloC 1~6 Alkoxy, Hydroxy C 1~6 Alkyl, C 1~6 Alkoxy C 1~6 Alkyl, C 3~10 Cycloalkyloxy, C 3~10 Cycloalkyl C 1~6 Alkoxy, C 1~6 Alkoxy, carboxyl, C 1~6Alkoxycarbonyl, C 1~6 Alkyl carbonyl, C 6~10 Aryl C 1~6 Alkoxy, mono or di(C 1~6 alkyl)amino, mono- or di(C 1~6 Alkyl)amino C 1~6 Alkyl, mono or di(C 1~6 Alkyl)aminocarbonyl, amino C 1~6 Alkyl, amino, 3- to 10-membered saturated or partially saturated heterocyclyl, 5- to 10-membered heteroaryl, 3- to 10-membered saturated or partially saturated heterocyclylC 1~6 Alkyl and 5-10 membered heteroaryl C 1~6 Alkyl, C 6~10 Aryloxy, C 6~10 Aryloxy C 1~6 Alkyl, C 6~10 Arylthio, HaloC 1~6 Alkylthio, C 3~10 Cycloalkylthio, C 1~6 Alkylsulfinyl, C 1~6 Alkylsulfonyl, C 3~10 Cycloalkylsulfinyl, C 3~10 Cycloalkylsulfonyl, C 6~10 Arylsulfinyl, C 6~10 Arylsulfonyl, mono- or di-(C 1~6 alkyl)aminosulfonyl, mono- or di-(C 1~6 alkyl)aminosulfinyl, C 1~6 Alkoxycarbonylamino, C 1~6 Alkylcarbonylamino, C 6~10 Cycloalkylcarbonylamino, C 6~10 Arylcarbonylamino, C 3~10 Cycloalkylcarbonyl, C 6~10 Arylcarbonyl, mono- or di(C 1~6 alkyl)aminocarbonyl, C 1~6 Alkylcarbonyloxy, and C 6~10 arylcarbonyloxy, each of which may be unsubstituted or may contain one or more Z 1a may be substituted with and / or two Zs 1 together with the atom(s) to which they are attached, form C 6~10 Aryl, 5-10 membered heteroaryl, C 3~10 cycloalkyl, or 3- to 10-membered saturated or partially saturated heterocyclyl, 6~10 Aryl, heteroaryl, C 3~10 Each of the cycloalkyl and heterocyclyl may be unsubstituted or may contain one or more Z 1a may be substituted with and / or one R 1a is one Z 1 and together with the atom(s) to which they are attached, C 4~10 cycloalkyl, or 4- to 10-membered saturated or partially saturated heterocyclyl, or 5- to 10-membered heteroaryl, 4~10 Each cycloalkyl, heterocyclyl, or heteroaryl may be unsubstituted or may contain one or more Z 1a may be substituted with R 1b is hydrogen or C 1~6 alkyl or R 1b is one Z 1 and together with the atom(s) to which they are attached can form a 4- to 10-membered saturated or partially saturated heterocyclyl or a 5- to 10-membered heteroaryl, each of which can be unsubstituted or can be substituted with one or more Z 1a may be substituted with each Z 1a are halo, cyano, hydroxyl, C 1~6 Alkyl, HaloC 1~6 Alkyl, C 1~6 Alkoxy, C 1~6 Alkylthio, HaloC 1~6 Alkoxy, Hydroxy C 1~6 Alkyl, C 1~6 Alkoxy C 1~6 Alkyl, C 3~10 Cycloalkyl, C 3~10 Cycloalkyloxy, C 6~10Aryl, C 6~10 Aryl C 1~6 Alkyl, amino, mono or di(C 1~6 alkyl)amino, mono- or di(C 1~6 Alkyl)amino C 1~6 independently selected from the group consisting of alkyl, and oxo; Or R 1 is hydrogen, halo, cyano, C 1~6 Alkyl, HaloC 1~6 Alkyl, C 1~6 Alkoxy, C 1~6 Alkylthio, HaloC 1~6 Alkoxy, C 1~6 Alkoxy C 1~6 Alkyl, mono or di(C 1~6 alkyl)amino, and mono- or di-(C 1~6 Alkyl)amino C 1~6 alkyl, R 2 is C 6~10 Aryl, 5-10 membered heteroaryl, C 3~10 Cycloalkyl, C 5~10 Cycloalkenyl, 3- to 10-membered saturated or partially saturated heterocyclyl, and A 2 -X 2 - selected from the group comprising R 2 Above C 6~10 Aryl, 5-10 membered heteroaryl, C 3~10 Cycloalkyl, C 5~10 cycloalkenyl, 3- to 10-membered saturated or partially saturated heterocyclyl, X 2 and A 2 Each of may be unsubstituted or may contain one or more Z 2 may be substituted with X 2 is -C(R 2a )2-, -CO-, -O- or -NR 2b wherein each R 2a is hydrogen, halo, hydroxy and C 1~6 independently selected from the group consisting of alkyl, A 2 is C 6~10 Aryl, 5-10 membered heteroaryl, C3~10 Cycloalkyl, C 5~10 selected from the group consisting of cycloalkenyl, and 3- to 10-membered saturated or partially saturated heterocyclyl; each Z 2 are independently selected from halo, cyano, hydroxy, oxo, nitro, and thioxo; or C 1~6 Alkyl, C 3~10 Cycloalkyl, C 3~10 Cycloalkyl C 1~6 Alkyl, C 6~10 Aryl, C 6~10 Aryl C 1~6 Alkyl, HaloC 1~6 Alkyl, Cyano C 1~6 Alkyl, C 1~6 Alkoxy, Cyano C 1~6 Alkoxy, C 1~6 Alkylthio, HaloC 1~6 Alkoxy, Hydroxy C 1~6 Alkyl, C 1~6 Alkoxy C 1~6 Alkyl, C 3~10 Cycloalkyloxy, C 3~10 Cycloalkyl C 1~6 Alkoxy, C 1~6 Alkoxy, carboxyl, C 1~6 Alkoxycarbonyl, C 1~6 Alkyl carbonyl, C 6~10 Aryl C 1~6 Alkoxy, mono or di(C 1~6 alkyl)amino, mono- or di(C 1~6 Alkyl)amino C 1~6 Alkyl, mono or di(C 1~6 Alkyl)aminocarbonyl, amino C 1~6 Alkyl, amino, 3- to 10-membered saturated or partially saturated heterocyclyl, 5- to 10-membered heteroaryl, 3- to 10-membered saturated or partially saturated heterocyclylC 1~6 Alkyl, 5-10 membered heteroarylC 1~6 Alkyl, C 6~10 Aryloxy, C 6~10 Aryloxy C 1~6 Alkyl, C 6~10 Arylthio, HaloC 1~6 Alkylthio, C3~10 Cycloalkylthio, C 1~6 Alkylsulfinyl, C 1~6 Alkylsulfonyl, C 3~10 Cycloalkylsulfinyl, C 3~10 Cycloalkylsulfonyl, C 6~10 Arylsulfinyl, C 6~10 Arylsulfonyl, mono- or di-(C 1~6 alkyl)aminosulfonyl, mono- or di-(C 1~6 alkyl)aminosulfinyl, C 1~6 Alkoxycarbonylamino, C 1~6 Alkylcarbonylamino, C 6~10 Cycloalkylcarbonylamino, C 6~10 Arylcarbonylamino, C 3~10 Cycloalkylcarbonyl, C 6~10 Arylcarbonyl, mono- or di(C 1~6 alkyl)aminocarbonyl, C 1~6 Alkylcarbonyloxy, and C 6~10 arylcarbonyloxy, each of which may be unsubstituted or may contain one or more Z 2a may be substituted with and / or two Zs 2 together with the atom(s) to which they are attached, form C 6~10 Aryl, 5-10 membered heteroaryl, C 3~10 cycloalkyl, or 3- to 10-membered saturated or partially saturated heterocyclyl, 6~10 Aryl, heteroaryl, C 3~10 Each of the cycloalkyl and heterocyclyl may be unsubstituted or may contain one or more Z 2a may be substituted with and / or one R 2a is one Z 2 and together with the atom(s) to which they are attached, C 4~10 cycloalkyl, or 4- to 10-membered saturated or partially saturated heterocyclyl, or 5- to 10-membered heteroaryl, 4~10Each cycloalkyl, heterocyclyl, or heteroaryl may be unsubstituted or may contain one or more Z 2a may be substituted with R 2b is hydrogen or C 1~6 alkyl or R 2b is one Z 2 and together with the atom(s) to which they are attached can form a 4- to 10-membered saturated or partially saturated heterocyclyl or a 5- to 10-membered heteroaryl, each of which can be unsubstituted or can be substituted with one or more Z 2a may be substituted with each Z 2a are halo, cyano, hydroxyl, C 1~6 Alkyl, HaloC 1~6 Alkyl, C 1~6 Alkoxy, C 1~6 Alkylthio, HaloC 1~6 Alkoxy, Hydroxy C 1~6 Alkyl, C 1~6 Alkoxy C 1~6 Alkyl, C 3~10 Cycloalkyl, C 3~10 Cycloalkyloxy, C 6~10 Aryl, C 6~10 Aryl C 1~6 Alkyl, amino, mono or di(C 1~6 alkyl)amino, mono- or di(C 1~6 Alkyl)amino C 1~6 independently selected from the group consisting of alkyl, and oxo; R 3 is hydrogen, halo, cyano, C 1~6 Alkyl, HaloC 1~6 Alkyl, C 1~6 Alkoxy, C 1~6 Alkylthio, HaloC 1~6 Alkoxy, C 1~6 Alkoxy C 1~6 Alkyl, mono or di(C 1~6 alkyl)amino, and mono- or di-(C 1~6 Alkyl)amino C 1~6 is selected from the group including alkyl, R4 is C 6~10 aryl or 5- to 10-membered heteroaryl; Above C 6~10 Each of the aryl and 5- to 10-membered heteroaryl may be one or more Z 4 is replaced by each Z 4 are independently selected from halo, cyano, hydroxyl, oxo, nitro, and thioxo; or C 1~6 Alkyl, C 3~10 Cycloalkyl, C 3~10 Cycloalkyl C 1~6 Alkyl, C 6~10 Aryl, C 6~10 Aryl C 1~6 Alkyl, HaloC 1~6 Alkyl, Cyano C 1~6 Alkyl, C 1~6 Alkoxy, Cyano C 1~6 Alkoxy, C 1~6 Alkylthio, HaloC 1~6 Alkoxy, Hydroxy C 1~6 Alkyl, C 1~6 Alkoxy C 1~6 Alkyl, C 3~10 Cycloalkyloxy, C 3~10 Cycloalkyl C 1~6 Alkoxy, C 1~6 Alkoxy, carboxyl, C 1~6 Alkoxycarbonyl, C 1~6 Alkyl carbonyl, C 6~10 Aryl C 1~6 Alkoxy, mono or di(C 1~6 alkyl)amino, mono- or di(C 1~6 Alkyl)amino C 1~6 Alkyl, mono or di(C 1~6 Alkyl)aminocarbonyl, amino C 1~6 Alkyl, amino, 3- to 10-membered saturated or partially saturated heterocyclyl, 5- to 10-membered heteroaryl, 3- to 10-membered saturated or partially saturated heterocyclylC 1~6 Alkyl, 5-10 membered heteroarylC 1~6 Alkyl, C 6~10 Aryloxy, C 6~10 Aryloxy C1~6 Alkyl, C 6~10 Arylthio, HaloC 1~6 Alkylthio, C 3~10 Cycloalkylthio, C 1~6 Alkylsulfinyl, C 1~6 Alkylsulfonyl, C 3~10 Cycloalkylsulfinyl, C 3~10 Cycloalkylsulfonyl, C 6~10 Arylsulfinyl, C 6~10 Arylsulfonyl, mono- or di-(C 1~6 alkyl)aminosulfonyl, mono- or di-(C 1~6 alkyl)aminosulfinyl, C 1~6 Alkoxycarbonylamino, C 1~6 Alkylcarbonylamino, C 6~10 Cycloalkylcarbonylamino, C 6~10 Arylcarbonylamino, C 3~10 Cycloalkylcarbonyl, C 6~10 Arylcarbonyl, mono- or di(C 1~6 alkyl)aminocarbonyl, C 1~6 Alkylcarbonyloxy, and C 6~10 arylcarbonyloxy, each of which may be unsubstituted or may contain one or more Z 4a may be substituted with and / or two Zs 4 together with the atom(s) to which they are attached, form C 6~10 Aryl, 5-10 membered heteroaryl, C 3~10 cycloalkyl, or 3- to 10-membered saturated or partially saturated heterocyclyl, 6~10 Aryl, heteroaryl, C 3~10 Each of the cycloalkyl and heterocyclyl may be unsubstituted or may contain one or more Z 4a may be substituted with each Z 4a are halo, cyano, hydroxyl, C 1~6 Alkyl, HaloC 1~6 Alkyl, C 1~6 Alkoxy, C1~6 Alkylthio, HaloC 1~6 Alkoxy, Hydroxy C 1~6 Alkyl, C 1~6 Alkoxy C 1~6 Alkyl, C 3~10 Cycloalkyl, C 3~10 Cycloalkyloxy, C 6~10 Aryl, C 6~10 Aryl C 1~6 Alkyl, amino, mono or di(C 1~6 alkyl)amino, mono- or di(C 1~6 Alkyl)amino C 1~6 The compound of any one of statements 1-12, wherein the aryl group is independently selected from the group consisting of alkyl, and oxo.

[0186] 14. During the ceremony, R 1 is C 6~10 Aryl, 5-10 membered heteroaryl, C 3~10 Cycloalkyl, C 5~10 Cycloalkenyl, 3- to 10-membered saturated or partially saturated heterocyclyl, and A 1 -X 1 - selected from the group comprising R 1 Above C 6~10 Aryl, 5-10 membered heteroaryl, C 3~10 Cycloalkyl, C 5~10 cycloalkenyl, 3- to 10-membered saturated or partially saturated heterocyclyl, X 1 and A 1 Each of may be unsubstituted or may contain one or more Z 1 may be substituted with R 2 is hydrogen, halo, cyano, C 1~6 Alkyl and HaloC 1~6 Alkyl, C 1~6 selected from the group including alkoxy, X 1 is -C(R 1a )2-, -CO-, -O- or -NR 1b -, preferably X 1 is -C(R 1a )2-, -CO- or -NR1b and preferably X 1 -C(R 1a )2- or -CO-, preferably X 1 -C(R 1a )2-. Each R 1a is hydrogen, halo, hydroxy, and C 1~6 independently selected from the group consisting of alkyl, A 1 is C 6~10 Aryl, 5-10 membered heteroaryl, C 3~10 Cycloalkyl, C 5~10 cycloalkenyl, and 3- to 10-membered saturated or partially saturated heterocyclyl, preferably 1 is C 6~10 Aryl, 5-10 membered heteroaryl, C 3~10 Cycloalkyl, and C 5~10 cycloalkenyl, preferably selected from the group consisting of A 1 is C 6~10 Aryl, 5- to 10-membered heteroaryl, and C 5~10 cycloalkenyl, each Z 1 are independently selected from halo, cyano, hydroxy, oxo, thioxo, or C 1~6 Alkyl, C 3~10 Cycloalkyl, C 6~10 Aryl, HaloC 1~6 Alkyl, Cyano C 1~6 Alkyl, C 1~6 Alkoxy, Cyano C 1~6 Alkoxy, C 1~6 Alkylthio, HaloC 1~6 Alkoxy, Hydroxy C 1~6 Alkyl, C 1~6 Alkoxy C 1~6 Alkyl, C 3~10 Cycloalkyloxy, C 3~10 Cycloalkyl C 1~6 Alkoxy, C 1~6 Alkoxy C 1~6 Alkoxy, carboxyl, C 1~6 Alkoxycarbonyl, C 1~6Alkyl carbonyl, C 6~10 Aryl C 1~6 Alkoxy, mono or di(C 1~6 alkyl)amino, mono- or di(C 1~6 Alkyl)amino C 1~6 Alkyl, mono or di(C 1~6 Alkyl)aminocarbonyl, amino C 1~6 Alkyl, 3- to 10-membered saturated or partially saturated heterocyclyl, 5- to 10-membered heteroaryl, 3- to 10-membered saturated or partially saturated heterocyclylC 1~6 Alkyl and 5-10 membered heteroaryl C 1~6 alkyl, each of the above groups may be unsubstituted or may contain one or more Z 1a may be substituted with and / or two Zs 1 together with the atom(s) to which they are attached, form C 6~10 Aryl, 5-10 membered heteroaryl, C 3~10 cycloalkyl, or 3- to 10-membered saturated or partially saturated heterocyclyl, 6~10 Aryl, heteroaryl, C 3~10 Each of the cycloalkyl and heterocyclyl may be unsubstituted or may contain one or more Z 1a may be substituted with and / or one R 1a is one Z 1 and together with the atom(s) to which they are attached, C 4~10 cycloalkyl, or 4- to 10-membered saturated or partially saturated heterocyclyl, or 5- to 10-membered heteroaryl, 4~10 Each cycloalkyl, heterocyclyl, or heteroaryl may be unsubstituted or may contain one or more Z 1a may be substituted with R 1b is hydrogen or C 1~6 alkyl or R 1b is one Z 1and together with the atom(s) to which they are attached can form a 4- to 10-membered saturated or partially saturated heterocyclyl or a 5- to 10-membered heteroaryl, each of which can be unsubstituted or can be substituted with one or more Z 1a may be substituted with each Z 1a are halo, cyano, hydroxyl, C 1~6 Alkyl, HaloC 1~6 Alkyl, C 1~6 Alkoxy, C 1~6 Alkylthio, HaloC 1~6 Alkoxy, Hydroxy C 1~6 Alkyl, C 1~6 Alkoxy C 1~6 Alkyl, C 3~10 Cycloalkyl, C 3~10 Cycloalkyloxy, C 6~10 Aryl, C 6~10 Aryl C 1~6 Alkyl, amino, mono or di(C 1~6 alkyl)amino, mono- or di(C 1~6 Alkyl)amino C 1~6 independently selected from the group consisting of alkyl, and oxo; Preferably, heteroaryl is pyridinyl, pyrrolyl, thiophenyl, furanyl, thiazolyl, isothiazolyl, thiadiazolyl, triazol-2-yl, 1H-pyrazol-5-yl, pyrazolyl, imidazolyl, oxazolyl, isoxazolyl, triazolyl, oxadiazolyl, tetrazolyl, oxatriazolyl, thiatriazolyl, pyrimidinyl, pyrazinyl, pyridazinyl, oxazinyl, dioxinyl, thiazinyl, triazinyl, pyranyl, thiopyranyl, imidazo[2,1-b][1,3]thiazolyl, thieno [3,2-b]furanyl, thieno[3,2-b]thiophenyl, thieno[2,3-d][1,3]thiazolyl, thieno[2,3-d]imidazolyl, tetrazolo[1,5-a]pyridinyl, indolyl, indolizinyl, isoindolyl, benzofuranyl, isobenzofuranyl, benzothiophenyl, isobenzothiophenyl, indazolyl, benzimidazolyl, benzoxazolyl, 1,3-benzoxazolyl, 1,2-benzisoxazolyl, 2,1-benzisoxazolyl, 1,3-benzothiazolyl, 1,2-benziso Thiazolyl, 2,1-benzisothiazolyl, benzotriazolyl, 1,2,3 benzoxadiazolyl, 2,1,3-benzoxadiazolyl, benzo[c][1,2,5]oxadiazolyl, 1,2,3 benzothiadiazolyl, 2,1,3-benzothiadiazolyl, benzo[d]oxazol-2(3H)-one, 2,3-dihydro-benzofuranyl, thienopyridinyl, purinyl, 9H-purinyl, imidazo[1,2-a]pyridinyl, imidazo[1,2-a]pyrazinyl, imidazo[5,1-a]isoquinolinyl, imidazo[1, 5-a]pyridinyl, 6-oxo-pyridazin-1(6H)-yl, 2-oxopyridin-1(2H)-yl, 1,3-benzodioxolyl, quinolinyl, isoquinolinyl, cinnolinyl, quinazolinyl, quinoxalinyl, acridinyl, phthalazinyl, 1,4-dihydroindeno[1,2-c]-1H-pyrazolyl, 2,3-dihydro-1H-inden-1-one, 2,3-dihydro-1H-indenyl, 3,4-dihydroquinolin-2(1H)-one, 5,6-dihydroimidazo[5,1-a]isoquinolinyl, 8H-indeno[1,2-d]thiazolyl, benzo[d]oxazol-2(3H)-one, quinolin-2(1H)-one, quinazolin-4(1H)-one, quinazolin-2,4(1H,3H)-dione, benzo-[d]oxazolyl, and pyrazolo[1,5-a]pyridinyl; Preferably, heterocyclyl is piperidinyl, piperazinyl, homopiperazinyl, morpholinyl, tetrahydropyranyl, tetrahydrofuranyl, pyrrolidinyl, aziridinyl, oxiranyl, thiiranyl, azetidinyl, oxetanyl, thietanyl, imidazolinyl, pyrazolidinylimidazolidinyl, oxazolinyl, isoxazolinyl, oxazolidinyl, isoxazolidinyl, thiazolidinyl, isothiazolidinyl, succinimidyl, indolinyl, isoindolinyl, chromanyl (3,4-dihydropyranyl), (also known as benzo[b]pyranyl), 2H-pyrrolyl, pyrrolinyl (e.g., 1-pyrrolinyl, 2-pyrrolinyl, 3-pyrrolinyl), 4H-quinolidinyl, 2-oxopiperazinyl, pyrazolinyl (e.g., 2-pyrazolinyl, 3-pyrazolinyl), tetrahydro-2H-pyranyl, 2H-pyranyl, 4H-pyranyl, dihydro-2H-pyranyl, 3-dioxolanyl, 1,4-dioxanyl, 2,5-dioximidazolidinyl, 2-oxopiperidinyl, 2-oxopyrrolodinyl, indolinyl, tetrahydro-2H-pyranyl, 2H-pyranyl, 4H-pyranyl, dihydro-2H-pyranyl, 3-dioxolanyl, 1,4-dioxanyl, 2,5-dioximidazolidinyl, 2-oxopiperidinyl, 2-oxopyrrolodinyl, indolinyl, tetrahydro-2H-pyranyl, 2H-pyranyl, 4H-pyranyl, dihydro-2H-pyranyl, 3-dioxolanyl, 1,4-dioxanyl, 2,5-dioximidazolidinyl, 2-oxopiperidin ... Hydrothiophenyl, tetrahydroquinolinyl, tetrahydroisoquinolin-1-yl, tetrahydroisoquinolin-2-yl, tetrahydroisoquinolin-3-yl, tetrahydroisoquinolin-4-yl, thiomorpholin-4-yl, thiomorpholin-4-yl sulfoxide, thiomorpholin-4-yl sulfone, 1,3-dioxolanyl, 1,4-oxathinyl, 1,4-dithianyl, 1,3,5-trioxanyl, 1H-pyrrolidinyl, tetrahydro-1,1-dioxothiophenyl, N-formyl-piperazine nyl, thiomorpholinyl, dihydrofuranyl, dihydrothienyl, tetrahydrothienyl, dihydropyrazolyl, dihydroimidazolyl, isothiazolinyl, thiazolinyl, triazolinyl, triazolidinyl, oxadiazolinyl, oxadiazolidinyl, thiadiazolidinyl, thiadiazolinyl, tetrazolidinyl, dihydro-pyridinyl, tetrahydro-pyridinyl, 1,2,3,6-tetrahydropyridinyl, hexahydro-pyridinyl, dihydro-pyrimidinyl, tetrahydro-pyrimidinyl, 1,4,5,6-Tetrahydropyrimidinyl, dihydro-pyrazinyl, tetrahydro-pyrazinyl, dihydro-pyridazinyl, tetrahydro-pyridazinyl, dihydro-triazinyl, tetrahydro-triazinyl, hexahydro-triazinyl, 1,4-diazepanyl, dihydro-indolyl, indolinyl, tetrahydro-indolyl, dihydro-indazolyl, tetrahydro-indazolyl, dihydro-isoindolyl, dihydro-benzofuranyl, tetrahydro-benzofuranyl, dihydro-benzothienyl, tetrahydro-benzothienyl, dihydro-benzyl Benzoimidazolyl, tetrahydro-benzimidazolyl, dihydro-benzoxazolyl, 2,3-dihydrobenzo[d]oxazolyl, tetrahydro-benzoxazolyl, dihydro-benzoxazinyl, 3,4-dihydro-2H-benzo[b][1,4]oxazinyl, tetrahydro-benzoxazinyl, benzo[1,3]dioxolyl, benzo[1,4]dioxanyl, dihydro-purinyl, tetrahydro-purinyl, dihydro-quinolinyl, 1,2,3,4-tetrahydroquinolinyl, dihydro-isoquinolinyl, 3,4-dihydroisoquinolinyl quinolin-(1H)-yl, tetrahydro-isoquinolinyl, 1,2,3,4-tetrahydroisoquinolinyl, dihydro-quinazolinyl, tetrahydro-quinazolinyl, dihydro-quinoxalinyl, tetrahydro-quinoxalinyl, 1,2,3,4-tetrahydroquinoxalinyl, 2,5-dihydro-1H-pyrrolyl, 4,5-dihydro-1H-imidazolyl, hexahydropyrrolo[3,4-b][1,4]oxazin-(2H)-yl, 3,4-dihydro-2H-pyrido[3,2-b][1,4]oxazinyl, (cis)-octahydrocyclopenta[ c]pyrrolyl, hexahydropyrrolo[3,4-b]pyrrol-(1H)-yl, 5H-pyrrolo[3,4-b]pyridin-(7H)-yl, 5,7-dihydro-6H-pyrrolo[3,4-b]pyridinyl, tetrahydro-1H-pyrrolo[3,4-b]pyridin-(2H,7H,7aH)-yl, hexahydro-1H-pyrrolo[3,4-b]pyridin-(2H)-yl, (octahydro-6H-pyrrolo[3,4-b]pyridinyl, hexahydropyrrolo[1,2-a]pyrazin-(1H)-yl, 3,4,6,7,8,8a-hexahydro-1H-pyrrolo[1,2-a]pyrazinyl, 2,3,4,9-tetrahydro-1H-carbazolyl, 1,2,3,4-tetrahydropyrazino[1,2-a]indolyl, 2,3-dihydro-1H-pyrrolo[1,2-a]indolyl, 1,3-dihydro-2H-isoindolyl, octahydro-2H-isoindolyl, 2,5-diazabicyclo[2.2.1]heptanyl, 2-azabicyclo[2.2.1]heptenyl, 3-azabicyclo[3.1.0]hexanyl, 3,6-diazabicyclo[3.1.0]hexanyl, 5-azaspiro[2.4]heptanyl, 4,7-diazaspiro[2.5]octanyl, 2,6-diazaspiro[3.3]heptanyl, 2,5-diazaspiro[3.4]octanyl 14. The compound according to any one of statements 1 to 5, 9 to 13, being selected from the group comprising 1,4-dihydroindeno[1,2-c]pyrazolyl, dihydropyranyl, dihydropyridinyl, dihydroquinolinyl, 8H-indazolino[1,2-d]thiazolyl, tetrahydroimidazo[1,2-a]pyridinyl, pyridin-2(1H)-one, and 8-azabicyclo[3.2.1]oct-2-enyl.

[0187] 15. During the ceremony, R 1 is C 6~10 Aryl, 5-10 membered heteroaryl, C 3~10 Cycloalkyl, C 5~10 Cycloalkenyl, 3- to 10-membered saturated or partially saturated heterocyclyl, and A 1 -X 1 - selected from the group comprising R 1 Above C 6~10 Aryl, 5-10 membered heteroaryl, C 3~10 Cycloalkyl, C 5~10 cycloalkenyl, 3- to 10-membered saturated or partially saturated heterocyclyl, X 1 and A 1 Each of may be unsubstituted or may contain one or more Z1 may be substituted with R 2 is hydrogen or C 1~6 alkyl, X 1 is -C(R 1a )2-, -CO- or -NR 1b and preferably X 1 -C(R 1a )2- or -CO-, preferably X 1 -C(R 1a )2- and Each R 1a is hydrogen or C 1~6 independently selected from alkyl, A 1 is C 6~10 Aryl, 5-10 membered heteroaryl, C 3~10 Cycloalkyl, C 5~10 cycloalkenyl, and 3- to 10-membered saturated or partially saturated heterocyclyl, preferably 1 is C 6~10 Aryl, 5-10 membered heteroaryl, C 3~10 Cycloalkyl, and C 5~10 cycloalkenyl, preferably selected from the group consisting of A 1 is C 6~10 Aryl, 5- to 10-membered heteroaryl, and C 5~10 cycloalkenyl, each Z 1 are independently selected from halo, cyano, oxo, and thioxo; or C 1~6 Alkyl, C 3~10 Cycloalkyl, C 6~10 Aryl, HaloC 1~6 Alkyl, Cyano C 1~6 Alkyl, C 1~6 Alkoxy, Cyano C 1~6 Alkoxy, C 1~6 Alkylthio, HaloC 1~6 Alkoxy, Hydroxy C 1~6 Alkyl, C 1~6 Alkoxy C 1~6 Alkyl, C 3~10 Cycloalkyloxy, C3~10 Cycloalkyl C 1~6 Alkoxy, C 1~6 Alkoxy C 1~6 Alkoxy, C 1~6 Alkoxycarbonyl, C 1~6 Alkyl carbonyl, C 6~10 Aryl C 1~6 Alkoxy, mono or di(C 1~6 alkyl)amino, mono- or di(C 1~6 Alkyl)amino C 1~6 Alkyl, mono or di(C 1~6 Alkyl)aminocarbonyl, amino C 1~6 Alkyl, 3- to 10-membered saturated or partially saturated heterocyclyl, 5- to 10-membered heteroaryl, 3- to 10-membered saturated or partially saturated heterocyclylC 1~6 Alkyl and 5-10 membered heteroaryl C 1~6 alkyl, each of the above groups may be unsubstituted or may contain one or more Z 1a may be substituted with and / or two Zs 1 together with the atom(s) to which they are attached, form C 6~10 Aryl, 5-10 membered heteroaryl, C 3~10 cycloalkyl, or 3- to 10-membered saturated or partially saturated heterocyclyl, 6~10 Aryl, heteroaryl, C 3~10 Each of the cycloalkyl and heterocyclyl may be unsubstituted or may contain one or more Z 1a may be substituted with and / or one R 1a is one Z 1 and together with the atom(s) to which they are attached, C 4~10 cycloalkyl, or 4- to 10-membered saturated or partially saturated heterocyclyl, or 5- to 10-membered heteroaryl, 4~10 Each cycloalkyl, heterocyclyl, or heteroaryl may be unsubstituted or may contain one or more Z 1a may be substituted with R 1bis hydrogen or C 1~6 alkyl or R 1b is one Z 1 and together with the atom(s) to which they are attached can form a 4- to 10-membered saturated or partially saturated heterocyclyl or a 5- to 10-membered heteroaryl, each of which can be unsubstituted or can be substituted with one or more Z 1a may be substituted with each Z 1a are halo, cyano, hydroxyl, C 1~6 Alkyl, HaloC 1~6 Alkyl, C 1~6 Alkoxy, C 1~6 Alkylthio, HaloC 1~6 Alkoxy, Hydroxy C 1~6 Alkyl, C 1~6 Alkoxy C 1~6 Alkyl, C 3~10 Cycloalkyl, C 3~10 Cycloalkyloxy, C 6~10 Aryl, C 6~10 Aryl C 1~6 Alkyl, amino, mono or di(C 1~6 alkyl)amino, mono- or di(C 1~6 Alkyl)amino C 1~6 The compound of any one of statements 1-5, 9-14, wherein the compound is independently selected from the group consisting of alkyl, and oxo.

[0188] 16. During the ceremony, R 1 is C 6~10 Aryl, 5-10 membered heteroaryl, C 3~10 Cycloalkyl, C 5~10 Cycloalkenyl, and A 1 -X 1 - selected from the group comprising R 1 Above C 6~10 Aryl, 5-10 membered heteroaryl, C 3~10 Cycloalkyl, C 5~10 cycloalkenyl, X 1 and A 1 Each of may be unsubstituted or may contain one or more Z1 may be substituted with R 2 is hydrogen or C 1~6 alkyl, preferably R 2 is hydrogen or C 1~4 alkyl, preferably R 2 is hydrogen or C 1~2 alkyl, preferably R 2 is selected from hydrogen or methyl, preferably R 2 is hydrogen, X 1 is -C(R 1a )2- or -CO-, preferably X 1 -C(R 1a )2- and Each R 1a is hydrogen or C 1~6 independently selected from alkyl, A 1 is C 6~10 Aryl, 5-10 membered heteroaryl, C 3~10 Cycloalkyl, and C 5~10 cycloalkenyl, preferably selected from the group consisting of A 1 is C 6~10 Aryl, 5- to 10-membered heteroaryl, and C 5~10 cycloalkenyl, each Z 1 are independently selected from halo, cyano, and oxo; or C 1~6 Alkyl, C 3~10 Cycloalkyl, C 6~10 Aryl, HaloC 1~6 Alkyl, Cyano C 1~6 Alkyl, C 1~6 Alkoxy, Cyano C 1~6 Alkoxy, C 1~6 Alkylthio, HaloC 1~6 Alkoxy, Hydroxy C 1~6 Alkyl, C 1~6 Alkoxy C 1~6 Alkyl, C 3~10 Cycloalkyloxy, C 3~10 Cycloalkyl C 1~6 Alkoxy, C1~6 Alkoxy C 1~6 Alkoxy, C 1~6 Alkoxycarbonyl, C 1~6 Alkyl carbonyl, C 6~10 Aryl C 1~6 Alkoxy, mono or di(C 1~6 alkyl)amino, mono- or di(C 1~6 Alkyl)amino C 1~6 Alkyl, mono or di(C 1~6 Alkyl)aminocarbonyl, amino C 1~6 Alkyl, 3- to 10-membered saturated or partially saturated heterocyclyl, 5- to 10-membered heteroaryl, 3- to 10-membered saturated or partially saturated heterocyclylC 1~6 Alkyl and 5-10 membered heteroaryl C 1~6 alkyl, each of the above groups may be unsubstituted or may contain one or more Z 1a may be substituted with and / or two Zs 1 together with the atom(s) to which they are attached, form C 6~10 aryl or 5- to 10-membered heteroaryl, 6~10 Each of the aryl and heteroaryl may be unsubstituted or may contain one or more Z 1a may be substituted with each Z 1a are halo, cyano, hydroxyl, C 1~6 Alkyl, HaloC 1~6 Alkyl, C 1~6 Alkoxy, C 1~6 Alkylthio, HaloC 1~6 Alkoxy, Hydroxy C 1~6 Alkyl, C 1~6 Alkoxy C 1~6 Alkyl, C 3~10 Cycloalkyl, C 3~10 Cycloalkyloxy, C 6~10 Aryl, C 6~10 Aryl C 1~6 Alkyl, amino, mono or di(C 1~6 alkyl)amino, mono- or di(C 1~6 Alkyl)amino C 1~6The compound of any one of statements 1-5, 9-15, wherein the compound is independently selected from the group consisting of alkyl, and oxo.

[0189] 17. During the ceremony, R 1 is C 6~10 Aryl, 5-10 membered heteroaryl, C 3~10 Cycloalkyl, C 5~10 Cycloalkenyl and A 1 -X 1 -, preferably R 1 is C 6~10 Aryl, 5-8 membered heteroaryl, C 5~8 Cycloalkyl, C 3~8 Cycloalkenyl and A 1 -X 1 -, preferably R 1 is phenyl, 5-6 membered heteroaryl, C 3~6 Cycloalkyl, C 5~6 Cycloalkenyl and A 1 -X 1 -, preferably R 1 is phenyl, 5-6 membered heteroaryl, C 4~5 Cycloalkyl, cyclohexenyl and A 1 -X 1 - selected from the group comprising R 1 Above C 6~10 Aryl, 5-10 membered heteroaryl, C 3~10 Cycloalkyl, C 5~10 cycloalkenyl, X 1 and A 1 Each of may be unsubstituted or may contain one or more Z 1 may be substituted with R 2 is hydrogen or C 1~6 alkyl, preferably R 2 is hydrogen or C 1~4 alkyl, preferably R 2 is hydrogen or C 1~2 alkyl, preferably R 2is selected from hydrogen or methyl, preferably R 2 is hydrogen, X 1 is -C(R 1a )2-, wherein each R 1a is hydrogen or C 1~6 alkyl, and preferably each R 1a is hydrogen or C 1~4 alkyl, and preferably each R 1a is hydrogen or C 1~2 alkyl, and preferably each R 1a are independently selected from hydrogen or methyl, preferably X 1 is -CH2-, A 1 is C 6~10 Aryl, 5- to 10-membered heteroaryl, and C 5~10 cycloalkenyl, preferably selected from the group consisting of A 1 is C 6~10 Aryl, 5- to 10-membered heteroaryl, and C 5~10 cycloalkenyl, preferably C 6~10 Aryl, 5- to 10-membered heteroaryl, and C 5~10 cycloalkenyl, preferably selected from the group consisting of A 1 is C 6~10 Aryl, 5- to 8-membered heteroaryl, and C 5~8 cycloalkenyl, preferably selected from the group consisting of A 1 is selected from the group consisting of phenyl, 5- to 6-membered heteroaryl and cyclohexenyl, preferably A 1 is selected from phenyl or 5- to 6-membered heteroaryl, preferably A 1 is phenyl, each Z 1 are independently selected from halo, cyano, and oxo; or C 1~6 Alkyl, C 3~10 Cycloalkyl, C 6~10 Aryl, HaloC 1~6 Alkyl, Cyano C 1~6 Alkyl, C 1~6 Alkoxy, Cyano C1~6 Alkoxy, C 1~6 Alkylthio, HaloC 1~6 Alkoxy, Hydroxy C 1~6 Alkyl, C 1~6 Alkoxy C 1~6 Alkyl, C 3~10 Cycloalkyloxy, C 3~10 Cycloalkyl C 1~6 Alkoxy, C 1~6 Alkoxy C 1~6 Alkoxy, C 1~6 Alkoxycarbonyl, C 1~6 Alkyl carbonyl, C 6~10 Aryl C 1~6 Alkoxy, mono or di(C 1~6 alkyl)amino, mono- or di(C 1~6 Alkyl)amino C 1~6 Alkyl, mono or di(C 1~6 alkyl)aminocarbonyl, 3- to 10-membered saturated or partially saturated heterocyclyl, 5- to 10-membered heteroaryl, 3- to 10-membered saturated or partially saturated heterocyclylC 1~6 Alkyl and 5-10 membered heteroaryl C 1~6 alkyl, each of which may be unsubstituted or may contain one or more Z 1a and preferably, each Z 1 are independently selected from halo, cyano, and oxo; or C 1~6 Alkyl, C 3~10 Cycloalkyl, C 6~10 Aryl, HaloC 1~6 Alkyl, Cyano C 1~6 Alkyl, C 1~6 Alkoxy, Cyano C 1~6 Alkoxy, C 1~6 Alkylthio, HaloC 1~6 Alkoxy, Hydroxy C 1~6 Alkyl, C 1~6 Alkoxy C 1~6 Alkyl, C 3~10 Cycloalkyloxy, C 3~10 Cycloalkyl C 1~6 Alkoxy, C 1~6 Alkoxy C 1~6Alkoxy, C 1~6 Alkoxycarbonyl, C 1~6 Alkyl carbonyl, C 6~10 Aryl C 1~6 Alkoxy, mono or di(C 1~6 and each of the above groups may be unsubstituted or may contain one or more Z 1a and preferably, each Z 1 are independently selected from halo, cyano, and oxo; or C 1~6 Alkyl, C 3~10 Cycloalkyl, HaloC 1~6 Alkyl, Cyano C 1~6 Alkyl, C 1~6 Alkoxy, Cyano C 1~6 Alkoxy, C 1~6 Alkylthio, HaloC 1~6 Alkoxy, Hydroxy C 1~6 Alkyl, C 1~6 Alkoxy C 1~6 Alkyl, C 3~10 Cycloalkyloxy and C 3~10 Cycloalkyl C 1~6 alkoxy, each of which may be unsubstituted or may be selected from the group consisting of one or more Z 1a and preferably, each Z 1 are independently selected from halo, cyano, and oxo; or C 1~6 Alkyl, HaloC 1~6 Alkyl, C 1~6 Alkoxy, C 1~6ア Lukircio, Haro C 1~6 Alkoxy, Hydroxy C 1~6 Alkyl, C 1~6 Alkoxy C 1~6 Alkyl, C 3~10 Cycloalkyloxy and C 3~10 Cycloalkyl C 1~6 alkoxy, each of which may be unsubstituted or may be selected from the group consisting of one or more Z 1a may be substituted with and / or two Zs 1together with the atom(s) to which they are attached, form C 6~10 aryl or 5- to 10-membered heteroaryl, 6~10 Each of the aryl and heteroaryl may be unsubstituted or may contain one or more Z 1a and / or two Z 1 together with the atom(s) to which they are attached, form C 6~10 aryl or 5- to 8-membered heteroaryl, 6~10 Each of the aryl and heteroaryl may be unsubstituted or may contain one or more Z 1a and / or two Z 1 can be taken together with the atom(s) to which they are attached to form a phenyl or a 5- to 6-membered heteroaryl, each of which may be unsubstituted or may be substituted with one or more Z 1a may be substituted with each Z 1a are halo, cyano, hydroxyl, C 1~6 Alkyl, HaloC 1~6 Alkyl, C 1~6 Alkoxy, C 1~6 Alkylthio, HaloC 1~6 Alkoxy, Hydroxy C 1~6 Alkyl, C 1~6 Alkoxy C 1~6 Alkyl, C 3~10 Cycloalkyl, C 3~10 Cycloalkyloxy, C 6~10 Aryl, C 6~10 Aryl C 1~6 Alkyl, amino, mono or di(C 1~6 alkyl)amino, mono- or di(C 1~6 Alkyl)amino C 1~6 is independently selected from the group consisting of alkyl and oxo, and preferably each Z 1a are halo, cyano, hydroxyl, C 1~6 Alkyl, HaloC 1~6 Alkyl, C 1~6 Alkoxy, C 1~6Alkylthio, HaloC 1~6 Alkoxy, Hydroxy C 1~6 Alkyl, C 1~6 Alkoxy C 1~6 Alkyl, C 3~10 Cycloalkyl, C 3~10 is independently selected from the group consisting of cycloalkyloxy and oxo, and preferably each Z 1a are halo, cyano, hydroxyl, C 1~6 Alkyl, HaloC 1~6 Alkyl, C 1~6 Alkoxy, HaloC 1~6 Alkoxy, Hydroxy C 1~6 The compound of any one of statements 1-5, 9-16, independently selected from the group consisting of alkyl and oxo.

[0190] 18. During the ceremony, R 1 is phenyl, 5-6 membered heteroaryl, C 4~6 Cycloalkyl, C 5~6 Cycloalkenyl and A 1 -X 1 -, preferably R 1 is phenyl, 5-6 membered heteroaryl, C 4~5 Cycloalkyl, cyclohexenyl and A 1 -X 1 -, preferably R 1 is phenyl, 5-6 membered heteroaryl, C 4~6 Cycloalkyl, C 5~6 Cycloalkenyl and A 1 -X 1 -, preferably R 1 is phenyl, 5-6 membered heteroaryl, C 4~5 Preferably, the 5- to 6-membered heteroaryl is selected from the group including pyridyl, pyrrolyl, pyrazinyl, pyridazinyl, pyrimidinyl, thiophenyl, furanyl, thiazolyl, isothiazolyl, and 1,2,5-thiadiazolyl; R 1 The above phenyl, 5- to 6-membered heteroaryl, C 4~6Cycloalkyl, C 5~6 cycloalkenyl, X 1 and A 1 Each of may be unsubstituted or may contain one or more Z 1 may be substituted with R 2 is hydrogen or C 1~6 alkyl, preferably R 2 is hydrogen or C 1~4 alkyl, preferably R 2 is hydrogen or C 1~2 alkyl, preferably R 2 is selected from hydrogen or methyl, preferably R 2 is hydrogen, X 1 is -C(R 1a )2-, wherein each R 1a is hydrogen or C 1~6 alkyl, and preferably each R 1a is hydrogen or C 1~4 alkyl, and preferably each R 1a is hydrogen or C 1~2 alkyl, and preferably each R 1a are independently selected from hydrogen or methyl, preferably X 1 is -CH2-, A 1 is C 6~10 Aryl, 5- to 10-membered heteroaryl, and C 5~10 cycloalkenyl, preferably selected from the group consisting of A 1 is C 6~10 Aryl, 5- to 10-membered heteroaryl, and C 5~10 cycloalkenyl, preferably C 6~10 Aryl, 5- to 10-membered heteroaryl, and C 5~10 cycloalkenyl, preferably selected from the group consisting of A 1 is C 6~10 Aryl, 5- to 8-membered heteroaryl, and C 5~8 cycloalkenyl, preferably selected from the group consisting of A 1is selected from the group consisting of phenyl, 5- to 6-membered heteroaryl, and cyclohexenyl, and preferably A 1 is selected from phenyl or 5- to 6-membered heteroaryl, preferably A 1 is phenyl, preferably the 5-6 membered heteroaryl is selected from the group comprising pyridyl, pyrrolyl, pyrazinyl, pyridazinyl, pyrimidinyl, thiophenyl, furanyl, thiazolyl, isothiazolyl, and 1,2,5 thiadiazolyl; each Z 1 are independently selected from halo, cyano, and oxo; or C 1~6 Alkyl, C 3~10 Cycloalkyl, C 6~10 Aryl, HaloC 1~6 Alkyl, Cyano C 1~6 Alkyl, C 1~6 Alkoxy, Cyano C 1~6 Alkoxy, C 1~6 Alkylthio, HaloC 1~6 Alkoxy, Hydroxy C 1~6 Alkyl, C 1~6 Alkoxy C 1~6 Alkyl, C 3~10 Cycloalkyloxy, C 3~10 Cycloalkyl C 1~6 Alkoxy, C 1~6 Alkoxy C 1~6 Alkoxy, C 1~6 Alkoxycarbonyl, C 1~6 Alkyl carbonyl, C 6~10 Aryl C 1~6 Alkoxy, mono or di(C 1~6 alkyl)amino, mono- or di(C 1~6 Alkyl)amino C 1~6 Alkyl, mono or di(C 1~6 alkyl)aminocarbonyl, 3- to 10-membered saturated or partially saturated heterocyclyl, 5- to 10-membered heteroaryl, 3- to 10-membered saturated or partially saturated heterocyclylC 1~6 Alkyl and 5-10 membered heteroaryl C 1~6 alkyl, each of which may be unsubstituted or may contain one or more Z 1aand preferably, each Z 1 are independently selected from halo, cyano, and oxo; or C 1~6 Alkyl, C 3~10 Cycloalkyl, C 6~10 Aryl, HaloC 1~6 Alkyl, Cyano C 1~6 Alkyl, C 1~6 Alkoxy, Cyano C 1~6 Alkoxy, C 1~6 Alkylthio, HaloC 1~6 Alkoxy, Hydroxy C 1~6 Alkyl, C 1~6 Alkoxy C 1~6 Alkyl, C 3~10 Cycloalkyloxy, C 3~10 Cycloalkyl C 1~6 Alkoxy, C 1~6 Alkoxy C 1~6 Alkoxy, C 1~6 Alkoxycarbonyl, C 1~6 Alkyl carbonyl, C 6~10 Aryl C 1~6 Alkoxy, mono or di(C 1~6 and each of the above groups may be unsubstituted or may contain one or more Z 1a and preferably, each Z 1 are independently selected from halo, cyano, and oxo; or C 1~6 Alkyl, C 3~10 Cycloalkyl, HaloC 1~6 Alkyl, Cyano C 1~6 Alkyl, C 1~6 Alkoxy, Cyano C 1~6 Alkoxy, C 1~6 Alkylthio, HaloC 1~6 Alkoxy, Hydroxy C 1~6 Alkyl, C 1~6 Alkoxy C 1~6 Alkyl, C 3~10 Cycloalkyloxy and C 3~10 Cycloalkyl C 1~6 alkoxy, each of which may be unsubstituted or may be selected from the group consisting of one or more Z 1aand preferably, each Z 1 are independently selected from halo, cyano, and oxo; or C 1~6 Alkyl, HaloC 1~6 Alkyl, C 1~6 Alkoxy, C 1~6ア Lukircio, Haro C 1~6 Alkoxy, Hydroxy C 1~6 Alkyl, C 1~6 Alkoxy C 1~6 Alkyl, C 3~10 Cycloalkyloxy and C 3~10 Cycloalkyl C 1~6 alkoxy, each of which may be unsubstituted or may be selected from the group consisting of one or more Z 1a may be substituted with and / or two Zs 1 together with the atom(s) to which they are attached, form C 6~10 aryl or 5- to 10-membered heteroaryl, 6~10 Each of the aryl and heteroaryl may be unsubstituted or may contain one or more Z 1a and / or two Z 1 together with the atom(s) to which they are attached, form C 6~10 aryl or 5- to 8-membered heteroaryl, 6~10 Each of the aryl and heteroaryl may be unsubstituted or may contain one or more Z 1a and / or two Z 1 can be taken together with the atom(s) to which they are attached to form a phenyl or a 5- to 6-membered heteroaryl, each of which may be unsubstituted or may be substituted with one or more Z 1a may be substituted with each Z 1a are halo, cyano, hydroxyl, C 1~6 Alkyl, HaloC 1~6 Alkyl, C 1~6 Alkoxy, C 1~6 Alkylthio, HaloC1~6 Alkoxy, Hydroxy C 1~6 Alkyl, C 1~6 Alkoxy C 1~6 Alkyl, C 3~10 Cycloalkyl, C 3~10 Cycloalkyloxy, C 6~10 Aryl, C 6~10 Aryl C 1~6 Alkyl, amino, mono or di(C 1~6 alkyl)amino, mono- or di(C 1~6 Alkyl)amino C 1~6 is independently selected from the group consisting of alkyl and oxo, and preferably each Z 1a are halo, cyano, hydroxyl, C 1~6 Alkyl, HaloC 1~6 Alkyl, C 1~6 Alkoxy, C 1~6 Alkylthio, HaloC 1~6 Alkoxy, Hydroxy C 1~6 Alkyl, C 1~6 Alkoxy C 1~6 Alkyl, C 3~10 Cycloalkyl, C 3~10 is independently selected from the group consisting of cycloalkyloxy and oxo, and preferably each Z 1a are halo, cyano, hydroxyl, C 1~6 Alkyl, HaloC 1~6 Alkyl, C 1~6 Alkoxy, HaloC 1~6 Alkoxy, Hydroxy C 1~6 The compound of any one of statements 1-5, 9-17, independently selected from the group consisting of alkyl and oxo.

[0191] 19. During the ceremony, R 1 is hydrogen, halo, cyano, C 1~6 Alkyl, HaloC 1~6 Alkyl, and C 1~6 selected from the group including alkoxy, R 2 is C 6~10 Aryl, 5-10 membered heteroaryl, C 3~10 Cycloalkyl, C 5~10Cycloalkenyl, 3- to 10-membered saturated or partially saturated heterocyclyl, and A 2 -X 2 - selected from the group comprising R 2 Above C 6~10 Aryl, 5-10 membered heteroaryl, C 3~10 Cycloalkyl, C 5~10 cycloalkenyl, 3- to 10-membered saturated or partially saturated heterocyclyl, X 2 and A 2 Each of may be unsubstituted or may contain one or more Z 2 may be substituted with X 2 is -C(R 2a )2-, -CO-, -O- or -NR 2b -, preferably X 2 is -C(R 2a )2-, -CO- or -NR 2b and preferably X 2 -C(R 2a )2- or -CO-, preferably X 2 is -C(R 2a )2-, wherein each R 2a is hydrogen, halo, hydroxy and C 1~6 independently selected from alkyl, A 2 is C 6~10 Aryl, 5-10 membered heteroaryl, C 3~10 Cycloalkyl, C 5~10 cycloalkenyl, and 3- to 10-membered saturated or partially saturated heterocyclyl, preferably 2 is C 6~10 Aryl, 5-10 membered heteroaryl, C 3~10 Cycloalkyl, and C 5~10 cycloalkenyl, preferably selected from the group consisting of A 2 is C 6~10 Aryl, 5- to 10-membered heteroaryl, and C 5~10 cycloalkenyl, each Z 2 are independently selected from halo, cyano, hydroxy, oxo, or C1~6 Alkyl, C 3~10 Cycloalkyl, C 6~10 Aryl, HaloC 1~6 Alkyl, Cyano C 1~6 Alkyl, C 1~6 Alkoxy, Cyano C 1~6 Alkoxy, C 1~6 Alkylthio, HaloC 1~6 Alkoxy, Hydroxy C 1~6 Alkyl, C 1~6 Alkoxy C 1~6 Alkyl, C 3~10 Cycloalkyloxy, C 3~10 Cycloalkyl C 1~6 Alkoxy, C 1~6 Alkoxy C 1~6 Alkoxy, carboxyl, C 1~6 Alkoxycarbonyl, C 1~6 Alkyl carbonyl, C 6~10 Aryl C 1~6 Alkoxy, mono or di(C 1~6 alkyl)amino, mono- or di(C 1~6 Alkyl)amino C 1~6 Alkyl, mono or di(C 1~6 Alkyl)aminocarbonyl, amino C 1~6 Alkyl, 3- to 10-membered saturated or partially saturated heterocyclyl, 5- to 10-membered heteroaryl, 3- to 10-membered saturated or partially saturated heterocyclylC 1~6 Alkyl and 5-10 membered heteroaryl C 1~6 alkyl, each of the above groups may be unsubstituted or may contain one or more Z 2a may be substituted with and / or two Zs 2 together with the atom(s) to which they are attached, form C 6~10 Aryl, 5-10 membered heteroaryl, C 3~10 cycloalkyl, or 3- to 10-membered saturated or partially saturated heterocyclyl, 6~10 Aryl, heteroaryl, C 3~10 Each of the cycloalkyl and heterocyclyl may be unsubstituted or may contain one or more Z 2amay be substituted with and / or one R 2a is one Z 2 and together with the atom(s) to which they are attached, C 4~10 cycloalkyl, or 4- to 10-membered saturated or partially saturated heterocyclyl, or 5- to 10-membered heteroaryl, 4~10 Each cycloalkyl, heterocyclyl, or heteroaryl may be unsubstituted or may contain one or more Z 2a may be substituted with R 2b is hydrogen or C 1~6 alkyl or R 2b is one Z 2 and together with the atom(s) to which they are attached can form a 4- to 10-membered saturated or partially saturated heterocyclyl or a 5- to 10-membered heteroaryl, each of which can be unsubstituted or can be substituted with one or more Z 2a may be substituted with each Z 2a are halo, cyano, hydroxyl, C 1~6 Alkyl, HaloC 1~6 Alkyl, C 1~6 Alkoxy, C 1~6 Alkylthio, HaloC 1~6 Alkoxy, Hydroxy C 1~6 Alkyl, C 1~6 Alkoxy C 1~6 Alkyl, C 3~10 Cycloalkyl, C 3~10 Cycloalkyloxy, C 6~10 Aryl, C 6~10 Aryl C 1~6 Alkyl, amino, mono or di(C 1~6 alkyl)amino, mono- or di(C 1~6 Alkyl)amino C 1~6 independently selected from the group consisting of alkyl, and oxo. Preferably, heteroaryl is pyridinyl, pyrrolyl, thiophenyl, furanyl, thiazolyl, isothiazolyl, thiadiazolyl, triazol-2-yl, 1H-pyrazol-5-yl, pyrazolyl, imidazolyl, oxazolyl, isoxazolyl, triazolyl, oxadiazolyl, tetrazolyl, oxatriazolyl, thiatriazolyl, pyrimidinyl, pyrazinyl, pyridazinyl, oxazinyl, dioxinyl, thiazinyl, triazinyl, pyranyl, thiopyranyl, imidazo[2,1-b][1,3]thiazolyl, thieno [3,2-b]furanyl, thieno[3,2-b]thiophenyl, thieno[2,3-d][1,3]thiazolyl, thieno[2,3-d]imidazolyl, tetrazolo[1,5-a]pyridinyl, indolyl, indolizinyl, isoindolyl, benzofuranyl, isobenzofuranyl, benzothiophenyl, isobenzothiophenyl, indazolyl, benzimidazolyl, benzoxazolyl, 1,3-benzoxazolyl, 1,2-benzisoxazolyl, 2,1-benzisoxazolyl, 1,3-benzothiazolyl, 1,2-benziso Thiazolyl, 2,1-benzisothiazolyl, benzotriazolyl, 1,2,3 benzoxadiazolyl, 2,1,3-benzoxadiazolyl, benzo[c][1,2,5]oxadiazolyl, 1,2,3 benzothiadiazolyl, 2,1,3-benzothiadiazolyl, benzo[d]oxazol-2(3H)-one, 2,3-dihydro-benzofuranyl, thienopyridinyl, purinyl, 9H-purinyl, imidazo[1,2-a]pyridinyl, imidazo[1,2-a]pyrazinyl, imidazo[5,1-a]isoquinolinyl, imidazo[1, 5-a]pyridinyl, 6-oxo-pyridazin-1(6H)-yl, 2-oxopyridin-1(2H)-yl, 1,3-benzodioxolyl, quinolinyl, isoquinolinyl, cinnolinyl, quinazolinyl, quinoxalinyl, acridinyl, phthalazinyl, 1,4-dihydroindeno[1,2-c]-1H-pyrazolyl, 2,3-dihydro-1H-inden-1-one, 2,3-dihydro-1H-indenyl, 3,4-dihydroquinolin-2(1H)-one, 5,6-dihydroimidazo[5,1-a]isoquinolinyl, 8H-indeno[1,2-d]thiazolyl, benzo[d]oxazol-2(3H)-one, quinolin-2(1H)-one, quinazolin-4(1H)-one, quinazolin-2,4(1H,3H)-dione, benzo-[d]oxazolyl, and pyrazolo[1,5-a]pyridinyl; Preferably, heterocyclyl is piperidinyl, piperazinyl, homopiperazinyl, morpholinyl, tetrahydropyranyl, tetrahydrofuranyl, pyrrolidinyl, aziridinyl, oxiranyl, thiiranyl, azetidinyl, oxetanyl, thietanyl, imidazolinyl, pyrazolidinylimidazolidinyl, oxazolinyl, isoxazolinyl, oxazolidinyl, isoxazolidinyl, thiazolidinyl, isothiazolidinyl, succinimidyl, indolinyl, isoindolinyl, chromanyl (3,4-dihydropyranyl), (also known as benzo[b]pyranyl), 2H-pyrrolyl, pyrrolinyl (e.g., 1-pyrrolinyl, 2-pyrrolinyl, 3-pyrrolinyl), 4H-quinolidinyl, 2-oxopiperazinyl, pyrazolinyl (e.g., 2-pyrazolinyl, 3-pyrazolinyl), tetrahydro-2H-pyranyl, 2H-pyranyl, 4H-pyranyl, dihydro-2H-pyranyl, 3-dioxolanyl, 1,4-dioxanyl, 2,5-dioximidazolidinyl, 2-oxopiperidinyl, 2-oxopyrrolodinyl, indolinyl, tetrahydro-2H-pyranyl, 2H-pyranyl, 4H-pyranyl, dihydro-2H-pyranyl, 3-dioxolanyl, 1,4-dioxanyl, 2,5-dioximidazolidinyl, 2-oxopiperidinyl, 2-oxopyrrolodinyl, indolinyl, tetrahydro-2H-pyranyl, 2H-pyranyl, 4H-pyranyl, dihydro-2H-pyranyl, 3-dioxolanyl, 1,4-dioxanyl, 2,5-dioximidazolidinyl, 2-oxopiperidin ... Hydrothiophenyl, tetrahydroquinolinyl, tetrahydroisoquinolin-1-yl, tetrahydroisoquinolin-2-yl, tetrahydroisoquinolin-3-yl, tetrahydroisoquinolin-4-yl, thiomorpholin-4-yl, thiomorpholin-4-yl sulfoxide, thiomorpholin-4-yl sulfone, 1,3-dioxolanyl, 1,4-oxathinyl, 1,4-dithianyl, 1,3,5-trioxanyl, 1H-pyrrolidinyl, tetrahydro-1,1-dioxothiophenyl, N-formyl-piperazine nyl, thiomorpholinyl, dihydrofuranyl, dihydrothienyl, tetrahydrothienyl, dihydropyrazolyl, dihydroimidazolyl, isothiazolinyl, thiazolinyl, triazolinyl, triazolidinyl, oxadiazolinyl, oxadiazolidinyl, thiadiazolidinyl, thiadiazolinyl, tetrazolidinyl, dihydro-pyridinyl, tetrahydro-pyridinyl, 1,2,3,6-tetrahydropyridinyl, hexahydro-pyridinyl, dihydro-pyrimidinyl, tetrahydro-pyrimidinyl, 1,4,5,6-Tetrahydropyrimidinyl, dihydro-pyrazinyl, tetrahydro-pyrazinyl, dihydro-pyridazinyl, tetrahydro-pyridazinyl, dihydro-triazinyl, tetrahydro-triazinyl, hexahydro-triazinyl, 1,4-diazepanyl, dihydro-indolyl, indolinyl, tetrahydro-indolyl, dihydro-indazolyl, tetrahydro-indazolyl, dihydro-isoindolyl, dihydro-benzofuranyl, tetrahydro-benzofuranyl, dihydro-benzothienyl, tetrahydro-benzothienyl, dihydro-benzyl Benzoimidazolyl, tetrahydro-benzimidazolyl, dihydro-benzoxazolyl, 2,3-dihydrobenzo[d]oxazolyl, tetrahydro-benzoxazolyl, dihydro-benzoxazinyl, 3,4-dihydro-2H-benzo[b][1,4]oxazinyl, tetrahydro-benzoxazinyl, benzo[1,3]dioxolyl, benzo[1,4]dioxanyl, dihydro-purinyl, tetrahydro-purinyl, dihydro-quinolinyl, 1,2,3,4-tetrahydroquinolinyl, dihydro-isoquinolinyl, 3,4-dihydroisoquinolinyl quinolin-(1H)-yl, tetrahydro-isoquinolinyl, 1,2,3,4-tetrahydroisoquinolinyl, dihydro-quinazolinyl, tetrahydro-quinazolinyl, dihydro-quinoxalinyl, tetrahydro-quinoxalinyl, 1,2,3,4-tetrahydroquinoxalinyl, 2,5-dihydro-1H-pyrrolyl, 4,5-dihydro-1H-imidazolyl, hexahydropyrrolo[3,4-b][1,4]oxazin-(2H)-yl, 3,4-dihydro-2H-pyrido[3,2-b][1,4]oxazinyl, (cis)-octahydrocyclopenta[ c]pyrrolyl, hexahydropyrrolo[3,4-b]pyrrol-(1H)-yl, 5H-pyrrolo[3,4-b]pyridin-(7H)-yl, 5,7-dihydro-6H-pyrrolo[3,4-b]pyridinyl, tetrahydro-1H-pyrrolo[3,4-b]pyridin-(2H,7H,7aH)-yl, hexahydro-1H-pyrrolo[3,4-b]pyridin-(2H)-yl, (octahydro-6H-pyrrolo[3,4-b]pyridinyl, hexahydropyrrolo[1,2-a]pyrazin-(1H)-yl, 3,4,6,7,8,8a-hexahydro-1H-pyrrolo[1,2-a]pyrazinyl, 2,3,4,9-tetrahydro-1H-carbazolyl, 1,2,3,4-tetrahydropyrazino[1,2-a]indolyl, 2,3-dihydro-1H-pyrrolo[1,2-a]indolyl, 1,3-dihydro-2H-isoindolyl, octahydro-2H-isoindolyl, 2,5-diazabicyclo[2.2.1]heptanyl, 2-azabicyclo[2.2.1]heptenyl, 3-azabicyclo[3.1.0]hexanyl, 3,6-diazabicyclo[3.1.0]hexanyl, 5-azaspiro[2.4]heptanyl, 4,7-diazaspiro[2.5]octanyl, 2,6-diazaspiro[3.3]heptanyl, 2,5-diazaspiro[3.4]octanyl 14. The compound according to any one of statements 1-2, 6-13, being selected from the group comprising 1,4-dihydroindeno[1,2-c]pyrazolyl, dihydropyranyl, dihydropyridinyl, dihydroquinolinyl, 8H-indazolino[1,2-d]thiazolyl, tetrahydroimidazo[1,2-a]pyridinyl, pyridin-2(1H)-one, and 8-azabicyclo[3.2.1]oct-2-enyl.

[0192] 20.R 1 is hydrogen or C 1~6 alkyl, R 2 is C 6~10 Aryl, 5-10 membered heteroaryl, C 3~10 Cycloalkyl, C 5~10 Cycloalkenyl, 3- to 10-membered saturated or partially saturated heterocyclyl, and A 2 -X 2 - selected from the group comprising R 2 Above C 6~10 Aryl, 5-10 membered heteroaryl, C 3~10 Cycloalkyl, C 5~10 cycloalkenyl, 3- to 10-membered saturated or partially saturated heterocyclyl, X 2 and A2 Each of may be unsubstituted or may contain one or more Z 2 may be substituted with X 2 is -C(R 2a )2-, -CO- or -NR 2b and preferably X 2 is -C(R 2a )2- or -CO-, preferably X 2 is -C(R 2a )2-, wherein each R 2a is hydrogen, hydroxyl, or C 1~6 independently selected from alkyl, A 2 is C 6~10 Aryl, 5-10 membered heteroaryl, C 3~10 Cycloalkyl, C 5~10 cycloalkenyl, and 3- to 10-membered saturated or partially saturated heterocyclyl, preferably 2 is C 6~10 Aryl, 5-10 membered heteroaryl, C 3~10 Cycloalkyl, and C 5~10 cycloalkenyl, preferably selected from the group consisting of A 2 is C 6~10 Aryl, 5- to 10-membered heteroaryl, and C 5~10 cycloalkenyl, each Z 2 are independently selected from halo, cyano, oxo, and thioxo; or C 1~6 Alkyl, C 3~10 Cycloalkyl, C 6~10 Aryl, HaloC 1~6 Alkyl, Cyano C 1~6 Alkyl, C 1~6 Alkoxy, Cyano C 1~6 Alkoxy, C 1~6 Alkylthio, HaloC 1~6 Alkoxy, Hydroxy C 1~6 Alkyl, C 1~6 Alkoxy C 1~6 Alkyl, C 3~10 Cycloalkyloxy, C 3~10 Cycloalkyl C1~6 Alkoxy, C 1~6 Alkoxy C 1~6 Alkoxy, C 1~6 Alkoxycarbonyl, C 1~6 Alkyl carbonyl, C 6~10 Aryl C 1~6 Alkoxy, mono or di(C 1~6 alkyl)amino, mono- or di(C 1~6 Alkyl)amino C 1~6 Alkyl, mono or di(C 1~6 Alkyl)aminocarbonyl, amino C 1~6 Alkyl, 3- to 10-membered saturated or partially saturated heterocyclyl, 5- to 10-membered heteroaryl, 3- to 10-membered saturated or partially saturated heterocyclylC 1~6 Alkyl and 5-10 membered heteroaryl C 1~6 alkyl, each of the above groups may be unsubstituted or may contain one or more Z 2a may be substituted with and / or two Zs 2 together with the atom(s) to which they are attached, form C 6~10 Aryl, 5-10 membered heteroaryl, C 3~10 cycloalkyl, or 3- to 10-membered saturated or partially saturated heterocyclyl, 6~10 Aryl, heteroaryl, C 3~10 Each of the cycloalkyl and heterocyclyl may be unsubstituted or may contain one or more Z 2a may be substituted with and / or one R 2a is one Z 2 and together with the atom(s) to which they are attached, C 4~10 cycloalkyl, or 4- to 10-membered saturated or partially saturated heterocyclyl, or 5- to 10-membered heteroaryl, 4~10 Each cycloalkyl, heterocyclyl, or heteroaryl may be unsubstituted or may contain one or more Z 2a may be substituted with R 2b is hydrogen or C 1~6alkyl or R 2b is one Z 2 and together with the atom(s) to which they are attached can form a 4- to 10-membered saturated or partially saturated heterocyclyl or a 5- to 10-membered heteroaryl, each of which can be unsubstituted or can be substituted with one or more Z 2a may be substituted with each Z 2a are halo, cyano, hydroxyl, C 1~6 Alkyl, HaloC 1~6 Alkyl, C 1~6 Alkoxy, C 1~6 Alkylthio, HaloC 1~6 Alkoxy, Hydroxy C 1~6 Alkyl, C 1~6 Alkoxy C 1~6 Alkyl, C 3~10 Cycloalkyl, C 3~10 Cycloalkyloxy, C 6~10 Aryl, C 6~10 Aryl C 1~6 Alkyl, amino, mono or di(C 1~6 alkyl)amino, mono- or di(C 1~6 Alkyl)amino C 1~6 20. The compound of any one of statements 1-2, 6-13, 19, wherein the compound is independently selected from the group consisting of alkyl, and oxo.

[0193] 21.R 1 is hydrogen or C 1~6 alkyl, preferably R 1 is hydrogen or C 1~4 alkyl, preferably R 1 is hydrogen or C 1~2 alkyl, preferably R 1 is selected from hydrogen or methyl, preferably R 1 is hydrogen, R 2 is C 6~10 Aryl, 5-10 membered heteroaryl, C 3~10 Cycloalkyl, C 5~10 Cycloalkenyl, and A 2-X 2 - selected from the group comprising R 2 Above C 6~10 Aryl, 5-10 membered heteroaryl, C 3~10 Cycloalkyl, C 5~10 cycloalkenyl, X 2 and A 2 Each of may be unsubstituted or may contain one or more Z 2 may be substituted with X 2 is -C(R 2a )2- or -CO-, preferably X 2 is -C(R 2a )2-, wherein each R 2a is hydrogen, hydroxyl, or C 1~6 independently selected from alkyl, A 2 is C 6~10 Aryl, 5-10 membered heteroaryl, C 3~10 Cycloalkyl, and C 5~10 cycloalkenyl, preferably selected from the group consisting of A 2 is C 6~10 Aryl, 5- to 10-membered heteroaryl, and C 5~10 cycloalkenyl, each Z 2 are independently selected from halo, cyano, and oxo; or C 1~6 Alkyl, C 3~10 Cycloalkyl, C 6~10 Aryl, HaloC 1~6 Alkyl, Cyano C 1~6 Alkyl, C 1~6 Alkoxy, Cyano C 1~6 Alkoxy, C 1~6 Alkylthio, HaloC 1~6 Alkoxy, Hydroxy C 1~6 Alkyl, C 1~6 Alkoxy C 1~6 Alkyl, C 3~10 Cycloalkyloxy, C 3~10 Cycloalkyl C 1~6 Alkoxy, C 1~6 Alkoxy C 1~6 Alkoxy, C1~6 Alkoxycarbonyl, C 1~6 Alkyl carbonyl, C 6~10 Aryl C 1~6 Alkoxy, mono or di(C 1~6 alkyl)amino, mono- or di(C 1~6 Alkyl)amino C 1~6 Alkyl, mono or di(C 1~6 Alkyl)aminocarbonyl, amino C 1~6 Alkyl, 3- to 10-membered saturated or partially saturated heterocyclyl, 5- to 10-membered heteroaryl, 3- to 10-membered saturated or partially saturated heterocyclylC 1~6 Alkyl and 5-10 membered heteroaryl C 1~6 alkyl, each of the above groups may be unsubstituted or may contain one or more Z 2a may be substituted with and / or two Zs 2 together with the atom(s) to which they are attached, form C 6~10 aryl or 5- to 10-membered heteroaryl, 6~10 Each of the aryl and heteroaryl may be unsubstituted or may contain one or more Z 2a may be substituted with each Z 2a are halo, cyano, hydroxyl, C 1~6 Alkyl, HaloC 1~6 Alkyl, C 1~6 Alkoxy, C 1~6 Alkylthio, HaloC 1~6 Alkoxy, Hydroxy C 1~6 Alkyl, C 1~6 Alkoxy C 1~6 Alkyl, C 3~10 Cycloalkyl, C 3~10 Cycloalkyloxy, C 6~10 Aryl, C 6~10 Aryl C 1~6 Alkyl, amino, mono or di(C 1~6 alkyl)amino, mono- or di(C 1~6 Alkyl)amino C 1~6The compound of any one of statements 1-2, 6-13, 19-20, wherein the compound is independently selected from the group consisting of alkyl, and oxo.

[0194] 22. During the ceremony, R 1 is hydrogen or C 1~6 alkyl, preferably R 1 is hydrogen or C 1~4 alkyl, preferably R 1 is hydrogen or C 1~2 alkyl, preferably R 1 is selected from hydrogen or methyl, preferably R 1 is hydrogen, R 2 is C 6~10 Aryl, 5-10 membered heteroaryl, C 3~10 Cycloalkyl, C 5~10 Cycloalkenyl, and A 2 -X 2 - selected from the group comprising R 2 Above C 6~10 Aryl, 5-10 membered heteroaryl, C 3~10 Cycloalkyl, C 5~10 cycloalkenyl, X 2 and A 2 Each of may be unsubstituted or may contain one or more Z 2 may be substituted with X 2 is -C(R 2a )2- or -CO-, preferably X 2 is -C(R 2a )2-, wherein each R 2a is hydrogen, hydroxyl, or C 1~6 alkyl, and preferably each R 2a is hydrogen, hydroxyl, or C 1~4 alkyl, and preferably each R 2a is hydrogen, hydroxyl, or C 1~2 alkyl, and preferably each R 2aare independently selected from hydrogen, hydroxyl, or methyl, and preferably X 2 is -CH2-, A 2 is C 6~10 Aryl, 5-10 membered heteroaryl, C 3~10 Cycloalkyl, and C 5~10 cycloalkenyl, preferably selected from the group consisting of A 2 is C 6~10 Aryl, 5-10 membered heteroaryl, C 3~8 Cycloalkyl, and C 5~10 cycloalkenyl, preferably selected from the group consisting of A 2 is C 6~10 Aryl, 5-8 membered heteroaryl, C 3~6 Cycloalkyl, and C 5~6 cycloalkenyl, preferably selected from the group consisting of A 2 is phenyl, 5-6 membered heteroaryl, C 3~6 Cycloalkyl, and C 5~6 cycloalkenyl, each Z 2 are independently selected from halo, cyano, and oxo; or C 1~6 Alkyl, C 3~10 Cycloalkyl, C 6~10 Aryl, HaloC 1~6 Alkyl, Cyano C 1~6 Alkyl, C 1~6 Alkoxy, Cyano C 1~6 Alkoxy, C 1~6 Alkylthio, HaloC 1~6 Alkoxy, Hydroxy C 1~6 Alkyl, C 1~6 Alkoxy C 1~6 Alkyl, C 3~10 Cycloalkyloxy, C 3~10 Cycloalkyl C 1~6 Alkoxy, C 1~6 Alkoxy C 1~6 Alkoxy, C 1~6 Alkoxycarbonyl, C 1~6 Alkyl carbonyl, C 6~10 Aryl C 1~6 Alkoxy, mono or di(C1~6 alkyl)amino, mono- or di(C 1~6 Alkyl)amino C 1~6 Alkyl, mono or di(C 1~6 Alkyl)aminocarbonyl, amino C 1~6 alkyl, each of which may be unsubstituted or may contain one or more Z 2a and preferably, each Z 2 are independently selected from halo, cyano, and oxo; or C 1~6 Alkyl, C 3~10 Cycloalkyl, C 6~10 Aryl, HaloC 1~6 Alkyl, Cyano C 1~6 Alkyl, C 1~6 Alkoxy, Cyano C 1~6 Alkoxy, C 1~6 Alkylthio, HaloC 1~6 Alkoxy, Hydroxy C 1~6 Alkyl, C 1~6 Alkoxy C 1~6 Alkyl, C 3~10 Cycloalkyloxy, C 3~10 Cycloalkyl C 1~6 Alkoxy, C 1~6 Alkoxy C 1~6 Alkoxy, C 1~6 alkoxycarbonyl, each of which may be unsubstituted or may contain one or more Z 2a and preferably, each Z 2 are independently selected from halo, cyano, and oxo; or C 1~6 Alkyl, C 3~10 Cycloalkyl, HaloC 1~6 Alkyl, Cyano C 1~6 Alkyl, C 1~6 Alkoxy, Cyano C 1~6 Alkoxy, C 1~6 Alkylthio, HaloC 1~6 Alkoxy, Hydroxy C 1~6 Alkyl, C 1~6 Alkoxy C 1~6 Alkyl, C 3~10 Cycloalkyloxy, C3~10 Cycloalkyl C 1~6 Alkoxy, C 1~6 Alkoxy C 1~6 alkoxy, each of which may be unsubstituted or may be selected from the group consisting of one or more Z 2a and preferably, each Z 2 are independently selected from halo, cyano, and oxo; or C 1~6 Alkyl, HaloC 1~6 Alkyl, C 1~6 Alkoxy, C 1~6ア Lukircio, Haro C 1~6 Alkoxy, Hydroxy C 1~6 Alkyl, C 1~6 Alkoxy C 1~6 Alkyl, C 3~10 Cycloalkyloxy, C 3~10 Cycloalkyl C 1~6 alkoxy, each of which may be unsubstituted or may be selected from the group consisting of one or more Z 2a may be substituted with each Z 2a are halo, cyano, hydroxyl, C 1~6 Alkyl, HaloC 1~6 Alkyl, C 1~6 Alkoxy, C 1~6 Alkylthio, HaloC 1~6 Alkoxy, Hydroxy C 1~6 Alkyl, C 1~6 Alkoxy C 1~6 Alkyl, C 3~10 Cycloalkyl, C 3~10 Cycloalkyloxy, C 6~10 Aryl, C 6~10 Aryl C 1~6 Alkyl, amino, mono or di(C 1~6 alkyl)amino, mono- or di(C 1~6 Alkyl)amino C 1~6 is independently selected from the group consisting of alkyl and oxo, and preferably each Z 2a are halo, cyano, hydroxyl, C 1~6 Alkyl, HaloC 1~6 Alkyl, C 1~6 Alkoxy, C1~6 Alkylthio, HaloC 1~6 Alkoxy, Hydroxy C 1~6 Alkyl, C 1~6 Alkoxy C 1~6 Alkyl, C 3~10 Cycloalkyl, C 3~10 is independently selected from the group consisting of cycloalkyloxy and oxo, and preferably each Z 2a are halo, cyano, hydroxyl, C 1~6 Alkyl, HaloC 1~6 Alkyl, C 1~6 Alkoxy, HaloC 1~6 Alkoxy, Hydroxy C 1~6 The compound of any one of statements 1-2, 6-13, 19-21, independently selected from the group consisting of alkyl and oxo.

[0195] 23. During the ceremony, R 1 is hydrogen or C 1~6 alkyl, preferably R 1 is hydrogen or C 1~4 alkyl, preferably R 1 is hydrogen or C 1~2 alkyl, preferably R 1 is selected from hydrogen or methyl, preferably R 1 is hydrogen, R 2 is C 6~10 Aryl, 5-8 membered heteroaryl, C 3~8 Cycloalkyl, C 5~8 Cycloalkenyl, and A 2 -X 2 -, preferably R 2 is phenyl, 5-6 membered heteroaryl, C 3~6 Cycloalkyl, C 5~6 Cycloalkenyl, and A 2 -X 2 -, preferably R 2 is phenyl, 5-6 membered heteroaryl, C 5~6 Cycloalkyl, C 5~6 Cycloalkenyl, and A2 -X 2 -, preferably R 2 is phenyl, 5-6 membered heteroaryl, cyclopentenyl, and A 2 -X 2 -, preferably R 2 is phenyl or A 2 -X 2 -, preferably R 2 is A 2 -X 2 and preferably, the 5- to 6-membered heteroaryl is selected from the group comprising pyridyl, pyrrolyl, pyrazinyl, pyridazinyl, pyrimidinyl, thiophenyl, furanyl, thiazolyl, isothiazolyl, and 1,2,5-thiadiazolyl; R 2 Above C 6~10 Aryl, 5-10 membered heteroaryl, C 3~10 Cycloalkyl, C 5~10 cycloalkenyl, X 2 and A 2 Each of may be unsubstituted or may contain one or more Z 2 may be substituted with X 2 is -C(R 2a )2-, wherein each R 2a is hydrogen, hydroxyl, or C 1~6 alkyl, and preferably each R 2a is hydrogen, hydroxyl, or C 1~4 alkyl, and preferably each R 2a is hydrogen, hydroxyl, or C 1~2 alkyl, and preferably each R 2a are independently selected from hydrogen, hydroxyl, or methyl, and preferably X 2 is -CH2-, A 2 is C 6~10 Aryl, 5-10 membered heteroaryl, C 3~10 Cycloalkyl, and C 5~10 cycloalkenyl, preferably selected from the group consisting of A 2is C 6~10 Aryl, 5-10 membered heteroaryl, C 3~8 Cycloalkyl, and C 5~10 cycloalkenyl, preferably selected from the group consisting of A 2 is C 6~10 Aryl, 5-8 membered heteroaryl, C 3~6 Cycloalkyl, and C 5~6 cycloalkenyl, preferably selected from the group consisting of A 2 is phenyl, 5-6 membered heteroaryl, C 3~6 Cycloalkyl, and C 5~6 cycloalkenyl, each Z 2 are independently selected from halo, cyano, and oxo; or C 1~6 Alkyl, C 3~10 Cycloalkyl, C 6~10 Aryl, HaloC 1~6 Alkyl, Cyano C 1~6 Alkyl, C 1~6 Alkoxy, Cyano C 1~6 Alkoxy, C 1~6 Alkylthio, HaloC 1~6 Alkoxy, Hydroxy C 1~6 Alkyl, C 1~6 Alkoxy C 1~6 Alkyl, C 3~10 Cycloalkyloxy, C 3~10 Cycloalkyl C 1~6 Alkoxy, C 1~6 Alkoxy C 1~6 Alkoxy, C 1~6 Alkoxycarbonyl, C 1~6 Alkyl carbonyl, C 6~10 Aryl C 1~6 Alkoxy, mono or di(C 1~6 alkyl)amino, mono- or di(C 1~6 Alkyl)amino C 1~6 Alkyl, mono or di(C 1~6 Alkyl)aminocarbonyl, amino C 1~6 alkyl, each of which may be unsubstituted or may contain one or more Z 2aand preferably, each Z 2 are independently selected from halo, cyano, and oxo; or C 1~6 Alkyl, C 3~10 Cycloalkyl, C 6~10 Aryl, HaloC 1~6 Alkyl, Cyano C 1~6 Alkyl, C 1~6 Alkoxy, Cyano C 1~6 Alkoxy, C 1~6 Alkylthio, HaloC 1~6 Alkoxy, Hydroxy C 1~6 Alkyl, C 1~6 Alkoxy C 1~6 Alkyl, C 3~10 Cycloalkyloxy, C 3~10 Cycloalkyl C 1~6 Alkoxy, C 1~6 Alkoxy C 1~6 Alkoxy, C 1~6 alkoxycarbonyl, each of which may be unsubstituted or may contain one or more Z 2a and preferably, each Z 2 are independently selected from halo, cyano, and oxo; or C 1~6 Alkyl, C 3~10 Cycloalkyl, HaloC 1~6 Alkyl, Cyano C 1~6 Alkyl, C 1~6 Alkoxy, Cyano C 1~6 Alkoxy, C 1~6 Alkylthio, HaloC 1~6 Alkoxy, Hydroxy C 1~6 Alkyl, C 1~6 Alkoxy C 1~6 Alkyl, C 3~10 Cycloalkyloxy, C 3~10 Cycloalkyl C 1~6 Alkoxy, C 1~6 Alkoxy C 1~6 alkoxy, each of which may be unsubstituted or may be selected from the group consisting of one or more Z 2a and preferably, each Z 2are independently selected from halo, cyano, and oxo; or C 1~6 Alkyl, HaloC 1~6 Alkyl, C 1~6 Alkoxy, C 1~6ア Lukircio, Haro C 1~6 Alkoxy, Hydroxy C 1~6 Alkyl, C 1~6 Alkoxy C 1~6 Alkyl, C 3~10 Cycloalkyloxy, C 3~10 Cycloalkyl C 1~6 alkoxy, each of which may be unsubstituted or may be selected from the group consisting of one or more Z 2a may be substituted with each Z 2a are halo, cyano, hydroxyl, C 1~6 Alkyl, HaloC 1~6 Alkyl, C 1~6 Alkoxy, C 1~6 Alkylthio, HaloC 1~6 Alkoxy, Hydroxy C 1~6 Alkyl, C 1~6 Alkoxy C 1~6 Alkyl, C 3~10 Cycloalkyl, C 3~10 Cycloalkyloxy, C 6~10 Aryl, C 6~10 Aryl C 1~6 Alkyl, amino, mono or di(C 1~6 alkyl)amino, mono- or di(C 1~6 Alkyl)amino C 1~6 is independently selected from the group consisting of alkyl and oxo, and preferably each Z 2a are halo, cyano, hydroxyl, C 1~6 Alkyl, HaloC 1~6 Alkyl, C 1~6 Alkoxy, C 1~6 Alkylthio, HaloC 1~6 Alkoxy, Hydroxy C 1~6 Alkyl, C 1~6 Alkoxy C 1~6 Alkyl, C 3~10 Cycloalkyl, C 3~10is independently selected from the group consisting of cycloalkyloxy and oxo, and preferably each Z 2a are halo, cyano, hydroxyl, C 1~6 Alkyl, HaloC 1~6 Alkyl, C 1~6 Alkoxy, HaloC 1~6 Alkoxy, Hydroxy C 1~6 The compound of any one of statements 1-2, 6-13, 19-22, independently selected from the group consisting of alkyl and oxo.

[0196] 24. During the ceremony, R 4 is C 6~10 aryl or 5- to 10-membered heteroaryl, preferably R 4 is C 6~10 aryl or 5- to 8-membered heteroaryl, preferably R 4 is phenyl or 5-6 membered heteroaryl, Above C 6~10 Each of the aryl and 5- to 10-membered heteroaryl may be one or more Z 4 and preferably, 6~10 Each of the aryl and 5- to 10-membered heteroaryl may have two or more Z 4 is replaced by each Z 4 are independently selected from halo, cyano, hydroxyl, oxo, nitro, thioxo, or C 1~6 Alkyl, C 3~10 Cycloalkyl, C 3~10 Cycloalkyl C 1~6 Alkyl, C 6~10 Aryl, C 6~10 Aryl C 1~6 Alkyl, HaloC 1~6 Alkyl, Cyano C 1~6 Alkyl, C 1~6 Alkoxy, Cyano C 1~6 Alkoxy, C 1~6 Alkylthio, HaloC 1~6 Alkoxy, Hydroxy C 1~6 Alkyl, C 1~6 Alkoxy C 1~6 Alkyl, C3~10 Cycloalkyloxy, C 3~10 Cycloalkyl C 1~6 Alkoxy, C 1~6 Alkoxy, carboxyl, C 1~6 Alkoxycarbonyl, C 1~6 Alkyl carbonyl, C 6~10 Aryl C 1~6 Alkoxy, mono or di(C 1~6 alkyl)amino, mono- or di(C 1~6 Alkyl)amino C 1~6 Alkyl, mono or di(C 1~6 Alkyl)aminocarbonyl, amino C 1~6 Alkyl, amino, 3- to 10-membered saturated or partially saturated heterocyclyl, 5- to 10-membered heteroaryl, 3- to 10-membered saturated or partially saturated heterocyclylC 1~6 Alkyl and 5-10 membered heteroaryl C 1~6 alkyl, each of which may be unsubstituted or may contain one or more Z 4a and preferably, each Z 4 are independently selected from halo, cyano, hydroxyl, oxo, and nitro; or C 1~6 Alkyl, C 3~10 Cycloalkyl, C 3~10 Cycloalkyl C 1~6 Alkyl, C 6~10 Aryl, C 6~10 Aryl C 1~6 Alkyl, HaloC 1~6 Alkyl, Cyano C 1~6 Alkyl, C 1~6 Alkoxy, Cyano C 1~6 Alkoxy, C 1~6 Alkylthio, HaloC 1~6 Alkoxy, Hydroxy C 1~6 Alkyl, C 1~6 Alkoxy C 1~6 Alkyl, C 3~10 Cycloalkyloxy, C 3~10 Cycloalkyl C 1~6 Alkoxy, C 1~6 Alkoxy, carboxyl, C 1~6 Alkoxycarbonyl, C1~6 Alkyl carbonyl, C 6~10 Aryl C 1~6 Alkoxy, 3- to 10-membered saturated or partially saturated heterocyclyl, 5- to 10-membered heteroaryl, 3- to 10-membered saturated or partially saturated heterocyclylC1-6 alkyl, and 5- to 10-membered heteroarylC 1~6 alkyl, each of which may be unsubstituted or may contain one or more Z 4a and preferably, each Z 4 are independently selected from halo, cyano, hydroxyl, oxo, or C 1~6 Alkyl, C 3~10 Cycloalkyl, C 3~10 Cycloalkyl C 1~6 Alkyl, C 6~10 Aryl, C 6~10 Aryl C 1~6 Alkyl, HaloC 1~6 Alkyl, Cyano C 1~6 Alkyl, C 1~6 Alkoxy, Cyano C 1~6 Alkoxy, C 1~6 Alkylthio, HaloC 1~6 Alkoxy, Hydroxy C 1~6 Alkyl, C 1~6 Alkoxy C 1~6 Alkyl, C 3~10 Cycloalkyloxy, C 3~10 Cycloalkyl C 1~6 Alkoxy, C 1~6 Alkoxy C 1~6 Alkoxy, carboxyl, C 1~6 Alkoxycarbonyl, C 1~6 Alkyl carbonyl, C 6~10 Aryl C 1~6 alkoxy, each of which may be unsubstituted or may be selected from the group consisting of one or more Z 4a and preferably, each Z 4 are independently selected from halo, cyano, hydroxyl, oxo, or C 1~6 Alkyl, C 3~10 Cycloalkyl, C 3~10 Cycloalkyl C 1~6Alkyl, C 6~10 Aryl, C 6~10 Aryl C 1~6 Alkyl, HaloC 1~6 Alkyl, Cyano C 1~6 Alkyl, C 1~6 Alkoxy, Cyano C 1~6 Alkoxy, HaloC 1~6 Alkoxy, C 1~6 Alkoxy C 1~6 Alkyl, C 3~10 Cycloalkyloxy, C 3~10 Cycloalkyl C 1~6 Alkoxy, C 1~6 Alkoxy C 1~6 Alkoxy, C 1~6 Alkoxycarbonyl, C 1~6 alkylcarbonyl, each of which may be unsubstituted or may contain one or more Z 4a and preferably, each Z 4 are independently selected from halo, cyano, and oxo; or C 1~6 Alkyl, C 3~10 Cycloalkyl, C 6~10 Aryl, HaloC 1~6 Alkyl, Cyano C 1~6 Alkyl, C 1~6 Alkoxy, Cyano C 1~6 Alkoxy, HaloC 1~6 Alkoxy, C 1~6 Alkoxy C 1~6 Alkyl, C 3~10 Cycloalkyloxy, C 1~6 Alkoxycarbonyl, C 1~6 alkylcarbonyl, each of which may be unsubstituted or may contain one or more Z 4a may be substituted with and / or two Zs 4 together with the atom(s) to which they are attached, form C 6~10 Aryl, 5-10 membered heteroaryl, C 3~10 cycloalkyl, or 3- to 10-membered saturated or partially saturated heterocyclyl, 6~10Aryl, heteroaryl, C 3~10 Each of the cycloalkyl and heterocyclyl may be unsubstituted or may contain one or more Z 4a and / or two Z 4 together with the atom(s) to which they are attached, form C 6~10 Aryl, 5-8 membered heteroaryl, C 3~10 cycloalkyl, or 3- to 8-membered saturated heterocyclyl, 6~10 Aryl, heterocyclyl, C 3~10 Each of the cycloalkyl and heteroaryl may be unsubstituted or may contain one or more Z 4a and / or two Z 4 together with the atom(s) to which they are attached, are phenyl, 5- to 6-membered heteroaryl, C 3~6 Each of the phenyl, heterocyclyl, cycloalkyl, and heteroaryl may be unsubstituted or may be substituted with one or more Z 4a may be substituted with each Z 4a are halo, cyano, hydroxyl, C 1~6 Alkyl, HaloC 1~6 Alkyl, C 1~6 Alkoxy, C 1~6 Alkylthio, HaloC 1~6 Alkoxy, Hydroxy C 1~6 Alkyl, C 1~6 Alkoxy C 1~6 Alkyl, C 3~10 Cycloalkyl, C 3~10 Cycloalkyloxy, C 6~10 Aryl, C 6~10 Aryl C 1~6 Alkyl, amino, mono or di(C 1~6 alkyl)amino, mono- or di(C 1~6 Alkyl)amino C 1~6 independently selected from the group consisting of alkyl, and oxo; Preferably, heteroaryl is pyridinyl, pyrrolyl, thiophenyl, furanyl, thiazolyl, isothiazolyl, thiadiazolyl, triazol-2-yl, 1H-pyrazol-5-yl, pyrazolyl, imidazolyl, oxazolyl, isoxazolyl, triazolyl, oxadiazolyl, tetrazolyl, oxatriazolyl, thiatriazolyl, pyrimidinyl, pyrazinyl, pyridazinyl, oxazinyl, dioxinyl, thiazinyl, triazinyl, pyranyl, thiopyranyl, imidazo[2,1-b][1,3]thiazolyl, thieno [3,2-b]furanyl, thieno[3,2-b]thiophenyl, thieno[2,3-d][1,3]thiazolyl, thieno[2,3-d]imidazolyl, tetrazolo[1,5-a]pyridinyl, indolyl, indolizinyl, isoindolyl, benzofuranyl, isobenzofuranyl, benzothiophenyl, isobenzothiophenyl, indazolyl, benzimidazolyl, benzoxazolyl, 1,3-benzoxazolyl, 1,2-benzisoxazolyl, 2,1-benzisoxazolyl, 1,3-benzothiazolyl, 1,2-benziso Thiazolyl, 2,1-benzisothiazolyl, benzotriazolyl, 1,2,3 benzoxadiazolyl, 2,1,3-benzoxadiazolyl, benzo[c][1,2,5]oxadiazolyl, 1,2,3 benzothiadiazolyl, 2,1,3-benzothiadiazolyl, benzo[d]oxazol-2(3H)-one, 2,3-dihydro-benzofuranyl, thienopyridinyl, purinyl, 9H-purinyl, imidazo[1,2-a]pyridinyl, imidazo[1,2-a]pyrazinyl, imidazo[5,1-a]isoquinolinyl, imidazo[1, 5-a]pyridinyl, 6-oxo-pyridazin-1(6H)-yl, 2-oxopyridin-1(2H)-yl, 1,3-benzodioxolyl, quinolinyl, isoquinolinyl, cinnolinyl, quinazolinyl, quinoxalinyl, acridinyl, phthalazinyl, 1,4-dihydroindeno[1,2-c]-1H-pyrazolyl, 2,3-dihydro-1H-inden-1-one, 2,3-dihydro-1H-indenyl, 3,4-dihydroquinolin-2(1H)-one, 5,6-dihydroimidazo[5,1-a]isoquinolinyl, 8H-indeno[1,2-d]thiazolyl, benzo[d]oxazol-2(3H)-one, quinolin-2(1H)-one, quinazolin-4(1H)-one, quinazolin-2,4(1H,3H)-dione, benzo-[d]oxazolyl, and pyrazolo[1,5-a]pyridinyl; Preferably, heterocyclyl is piperidinyl, piperazinyl, homopiperazinyl, morpholinyl, tetrahydropyranyl, tetrahydrofuranyl, pyrrolidinyl, aziridinyl, oxiranyl, thiiranyl, azetidinyl, oxetanyl, thietanyl, imidazolinyl, pyrazolidinylimidazolidinyl, oxazolinyl, isoxazolinyl, oxazolidinyl, isoxazolidinyl, thiazolidinyl, isothiazolidinyl, succinimidyl, indolinyl, isoindolinyl, chromanyl (3,4-dihydropyranyl), (also known as benzo[b]pyranyl), 2H-pyrrolyl, pyrrolinyl (e.g., 1-pyrrolinyl, 2-pyrrolinyl, 3-pyrrolinyl), 4H-quinolidinyl, 2-oxopiperazinyl, pyrazolinyl (e.g., 2-pyrazolinyl, 3-pyrazolinyl), tetrahydro-2H-pyranyl, 2H-pyranyl, 4H-pyranyl, dihydro-2H-pyranyl, 3-dioxolanyl, 1,4-dioxanyl, 2,5-dioximidazolidinyl, 2-oxopiperidinyl, 2-oxopyrrolodinyl, indolinyl, tetrahydro-2H-pyranyl, 2H-pyranyl, 4H-pyranyl, dihydro-2H-pyranyl, 3-dioxolanyl, 1,4-dioxanyl, 2,5-dioximidazolidinyl, 2-oxopiperidinyl, 2-oxopyrrolodinyl, indolinyl, tetrahydro-2H-pyranyl, 2H-pyranyl, 4H-pyranyl, dihydro-2H-pyranyl, 3-dioxolanyl, 1,4-dioxanyl, 2,5-dioximidazolidinyl, 2-oxopiperidin ... Hydrothiophenyl, tetrahydroquinolinyl, tetrahydroisoquinolin-1-yl, tetrahydroisoquinolin-2-yl, tetrahydroisoquinolin-3-yl, tetrahydroisoquinolin-4-yl, thiomorpholin-4-yl, thiomorpholin-4-yl sulfoxide, thiomorpholin-4-yl sulfone, 1,3-dioxolanyl, 1,4-oxathinyl, 1,4-dithianyl, 1,3,5-trioxanyl, 1H-pyrrolidinyl, tetrahydro-1,1-dioxothiophenyl, N-formyl-piperazine nyl, thiomorpholinyl, dihydrofuranyl, dihydrothienyl, tetrahydrothienyl, dihydropyrazolyl, dihydroimidazolyl, isothiazolinyl, thiazolinyl, triazolinyl, triazolidinyl, oxadiazolinyl, oxadiazolidinyl, thiadiazolidinyl, thiadiazolinyl, tetrazolidinyl, dihydro-pyridinyl, tetrahydro-pyridinyl, 1,2,3,6-tetrahydropyridinyl, hexahydro-pyridinyl, dihydro-pyrimidinyl, tetrahydro-pyrimidinyl, 1,4,5,6-Tetrahydropyrimidinyl, dihydro-pyrazinyl, tetrahydro-pyrazinyl, dihydro-pyridazinyl, tetrahydro-pyridazinyl, dihydro-triazinyl, tetrahydro-triazinyl, hexahydro-triazinyl, 1,4-diazepanyl, dihydro-indolyl, indolinyl, tetrahydro-indolyl, dihydro-indazolyl, tetrahydro-indazolyl, dihydro-isoindolyl, dihydro-benzofuranyl, tetrahydro-benzofuranyl, dihydro-benzothienyl, tetrahydro-benzothienyl, dihydro-benzyl Benzoimidazolyl, tetrahydro-benzimidazolyl, dihydro-benzoxazolyl, 2,3-dihydrobenzo[d]oxazolyl, tetrahydro-benzoxazolyl, dihydro-benzoxazinyl, 3,4-dihydro-2H-benzo[b][1,4]oxazinyl, tetrahydro-benzoxazinyl, benzo[1,3]dioxolyl, benzo[1,4]dioxanyl, dihydro-purinyl, tetrahydro-purinyl, dihydro-quinolinyl, 1,2,3,4-tetrahydroquinolinyl, dihydro-isoquinolinyl, 3,4-dihydroisoquinolinyl quinolin-(1H)-yl, tetrahydro-isoquinolinyl, 1,2,3,4-tetrahydroisoquinolinyl, dihydro-quinazolinyl, tetrahydro-quinazolinyl, dihydro-quinoxalinyl, tetrahydro-quinoxalinyl, 1,2,3,4-tetrahydroquinoxalinyl, 2,5-dihydro-1H-pyrrolyl, 4,5-dihydro-1H-imidazolyl, hexahydropyrrolo[3,4-b][1,4]oxazin-(2H)-yl, 3,4-dihydro-2H-pyrido[3,2-b][1,4]oxazinyl, (cis)-octahydrocyclopenta[ c]pyrrolyl, hexahydropyrrolo[3,4-b]pyrrol-(1H)-yl, 5H-pyrrolo[3,4-b]pyridin-(7H)-yl, 5,7-dihydro-6H-pyrrolo[3,4-b]pyridinyl, tetrahydro-1H-pyrrolo[3,4-b]pyridin-(2H,7H,7aH)-yl, hexahydro-1H-pyrrolo[3,4-b]pyridin-(2H)-yl, (octahydro-6H-pyrrolo[3,4-b]pyridinyl, hexahydropyrrolo[1,2-a]pyrazin-(1H)-yl, 3,4,6,7,8,8a-hexahydro-1H-pyrrolo[1,2-a]pyrazinyl, 2,3,4,9-tetrahydro-1H-carbazolyl, 1,2,3,4-tetrahydropyrazino[1,2-a]indolyl, 2,3-dihydro-1H-pyrrolo[1,2-a]indolyl, 1,3-dihydro-2H-isoindolyl, octahydro-2H-isoindolyl, 2,5-diazabicyclo[2.2.1]heptanyl, 2-azabicyclo[2.2.1]heptenyl, 3-azabicyclo[3.1.0]hexanyl, 3,6-diazabicyclo[3.1.0]hexanyl, 5-azaspiro[2.4]heptanyl, 4,7-diazaspiro[2.5]octanyl, 2,6-diazaspiro[3.3]heptanyl, 2,5-diazaspiro[3.4]octanyl 14. The compound according to any one of statements 1-2, 6-13, being selected from the group comprising 1,4-dihydroindeno[1,2-c]pyrazolyl, dihydropyranyl, dihydropyridinyl, dihydroquinolinyl, 8H-indazolino[1,2-d]thiazolyl, tetrahydroimidazo[1,2-a]pyridinyl, pyridin-2(1H)-one, and 8-azabicyclo[3.2.1]oct-2-enyl.

[0197] 25. During the ceremony, R 4 is C 6~10 aryl or 5- to 8-membered heteroaryl, preferably R 4 is phenyl or 5-6 membered heteroaryl, Above C 6~10 Each of the aryl and 5- to 10-membered heteroaryl may be one or more Z 4 and preferably, 6~10 Each of the aryl and 5- to 10-membered heteroaryl may have two or more Z 4 is replaced by each Z 4 are independently selected from halo, cyano, hydroxyl, oxo, nitro, and thioxo; or C 1~6 Alkyl, C3~10 Cycloalkyl, C 3~10 Cycloalkyl C 1~6 Alkyl, C 6~10 Aryl, C 6~10 Aryl C 1~6 Alkyl, HaloC 1~6 Alkyl, Cyano C 1~6 Alkyl, C 1~6 Alkoxy, Cyano C 1~6 Alkoxy, C 1~6 Alkylthio, HaloC 1~6 Alkoxy, Hydroxy C 1~6 Alkyl, C 1~6 Alkoxy C 1~6 Alkyl, C 3~10 Cycloalkyloxy, C 3~10 Cycloalkyl C 1~6 Alkoxy, C 1~6 Alkoxy C 1~6 Alkoxy, carboxyl, C 1~6 Alkoxycarbonyl, C 1~6 Alkyl carbonyl, C 6~10 Aryl C 1~6 Alkoxy, 3- to 10-membered saturated or partially saturated heterocyclyl, 5- to 10-membered heteroaryl, 3- to 10-membered saturated or partially saturated heterocyclylC 1~6 Alkyl and 5-10 membered heteroaryl C 1~6 alkyl, each of which may be unsubstituted or may contain one or more Z 4a and preferably, each Z 4 are independently selected from halo, cyano, hydroxyl, oxo, or C 1~6 Alkyl, C 3~10 Cycloalkyl, C 3~10 Cycloalkyl C 1~6 Alkyl, C 6~10 Aryl, C 6~10 Aryl C 1~6 Alkyl, HaloC 1~6 Alkyl, Cyano C 1~6 Alkyl, C 1~6 Alkoxy, Cyano C 1~6 Alkoxy, C 1~6 Alkylthio, HaloC 1~6Alkoxy, Hydroxy C 1~6 Alkyl, C 1~6 Alkoxy C 1~6 Alkyl, C 3~10 Cycloalkyloxy, C 3~10 Cycloalkyl C 1~6 Alkoxy, C 1~6 Alkoxy C 1~6 Alkoxy, carboxyl, C 1~6 Alkoxycarbonyl, C 1~6 Alkyl carbonyl, C 6~10 Aryl C 1~6 alkoxy, each of which may be unsubstituted or may be selected from the group consisting of one or more Z 4a and preferably, each Z 4 are independently selected from halo, cyano, hydroxyl, oxo, or C 1~6 Alkyl, C 3~10 Cycloalkyl, C 3~10 Cycloalkyl C 1~6 Alkyl, C 6~10 Aryl, C 6~10 Aryl C 1~6 Alkyl, HaloC 1~6 Alkyl, Cyano C 1~6 Alkyl, C 1~6 Alkoxy, Cyano C 1~6 Alkoxy, HaloC 1~6 Alkoxy, C 1~6 Alkoxy C 1~6 Alkyl, C 3~10 Cycloalkyloxy, C 3~10 Cycloalkyl C 1~6 Alkoxy, C 1~6 Alkoxy C 1~6 Alkoxy, C 1~6 Alkoxycarbonyl, C 1~6 alkylcarbonyl, each of which may be unsubstituted or may contain one or more Z 4a and preferably, each Z 4 are independently selected from halo, cyano, and oxo; or C 1~6 Alkyl, C 3~10 Cycloalkyl, C 6~10Aryl, HaloC 1~6 Alkyl, Cyano C 1~6 Alkyl, C 1~6 Alkoxy, Cyano C 1~6 Alkoxy, HaloC 1~6 Alkoxy, C 1~6 Alkoxy C 1~6 Alkyl, C 3~10 Cycloalkyloxy, C 1~6 Alkoxycarbonyl, C 1~6 alkylcarbonyl, each of which may be unsubstituted or may contain one or more Z 4a may be substituted with and / or two Zs 4 together with the atom(s) to which they are attached, form C 6~10 Aryl, 5-8 membered heteroaryl, C 3~10 cycloalkyl, or 3- to 8-membered saturated heterocyclyl, 6~10 Aryl, heterocyclyl, C 3~10 Each of the cycloalkyl and heteroaryl may be unsubstituted or may contain one or more Z 4a and / or two Z 4 together with the atom(s) to which they are attached, are phenyl, 5- to 6-membered heteroaryl, C 3~6 Each of the phenyl, heterocyclyl, cycloalkyl, and heteroaryl may be unsubstituted or may be substituted with one or more Z 4a may be substituted with each Z 4a are halo, cyano, hydroxyl, C 1~6 Alkyl, HaloC 1~6 Alkyl, C 1~6 Alkoxy, C 1~6 Alkylthio, HaloC 1~6 Alkoxy, Hydroxy C 1~6 Alkyl, C 1~6 Alkoxy C 1~6 Alkyl, C 3~10 Cycloalkyl, C 3~10Cycloalkyloxy, C 6~10 Aryl, C 6~10 Aryl C 1~6 Alkyl, amino, mono or di(C 1~6 alkyl)amino, mono- or di(C 1~6 Alkyl)amino C 1~6 The compound of any one of statements 1-24, wherein the compound is independently selected from the group consisting of alkyl, and oxo.

[0198] 26. During the ceremony, R 4 is phenyl or 5-6 membered heteroaryl, Each of the above phenyl and 5- to 6-membered heteroaryl may be one or more Z 4 , preferably two or more Z 4 is replaced by each Z 4 are independently selected from halo, cyano, hydroxyl, oxo, and thioxo; or C 1~6 Alkyl, C 3~10 Cycloalkyl, C 3~10 Cycloalkyl C 1~6 Alkyl, C 6~10 Aryl, C 6~10 Aryl C 1~6 Alkyl, HaloC 1~6 Alkyl, Cyano C 1~6 Alkyl, C 1~6 Alkoxy, Cyano C 1~6 Alkoxy, C 1~6 Alkylthio, HaloC 1~6 Alkoxy, Hydroxy C 1~6 Alkyl, C 1~6 Alkoxy C 1~6 Alkyl, C 3~10 Cycloalkyloxy, C 3~10 Cycloalkyl C 1~6 Alkoxy, C 1~6 Alkoxy, carboxyl, C 1~6 Alkoxycarbonyl, C 1~6 Alkyl carbonyl, C 6~10 Aryl C 1~6 alkoxy, each of which may be unsubstituted or may be selected from the group consisting of one or more Z4a and preferably, each Z 4 are independently selected from halo, cyano, hydroxyl, oxo, or C 1~6 Alkyl, C 3~10 Cycloalkyl, C 3~10 Cycloalkyl C 1~6 Alkyl, C 6~10 Aryl, C 6~10 Aryl C 1~6 Alkyl, HaloC 1~6 Alkyl, Cyano C 1~6 Alkyl, C 1~6 Alkoxy, Cyano C 1~6 Alkoxy, HaloC 1~6 Alkoxy, C 1~6 Alkoxy C 1~6 Alkyl, C 3~10 Cycloalkyloxy, C 3~10 Cycloalkyl C 1~6 Alkoxy, C 1~6 Alkoxy C 1~6 Alkoxy, C 1~6 Alkoxycarbonyl, C 1~6 alkylcarbonyl, each of which may be unsubstituted or may contain one or more Z 4a and preferably, each Z 4 are independently selected from halo, cyano, and oxo; or C 1~6 Alkyl, C 3~10 Cycloalkyl, C 6~10 Aryl, HaloC 1~6 Alkyl, Cyano C 1~6 Alkyl, C 1~6 Alkoxy, Cyano C 1~6 Alkoxy, HaloC 1~6 Alkoxy, C 1~6 Alkoxy C 1~6 Alkyl, C 3~10 Cycloalkyloxy, C 1~6 Alkoxycarbonyl, C 1~6 alkylcarbonyl, each of which may be unsubstituted or may contain one or more Z 4a may be substituted with and / or two Zs4 can be taken together with the atom(s) to which they are attached to form a phenyl, a 5-6 membered heteroaryl, a C3-6 cycloalkyl, or a 5-6 membered saturated heterocyclyl, each of which may be unsubstituted or may be substituted with one or more Z 4a may be substituted with each Z 4a are halo, cyano, hydroxyl, C 1~6 Alkyl, HaloC 1~6 Alkyl, C 1~6 Alkoxy, C 1~6 Alkylthio, HaloC 1~6 Alkoxy, Hydroxy C 1~6 Alkyl, C 1~6 Alkoxy C 1~6 Alkyl, C 3~10 Cycloalkyl, C 3~10 Cycloalkyloxy, C 6~10 Aryl, C 6~10 Aryl C 1~6 Alkyl, amino, mono or di(C 1~6 alkyl)amino, mono- or di(C 1~6 Alkyl)amino C 1~6 The compound of any one of statements 1-25, wherein the compound is independently selected from the group consisting of alkyl, and oxo.

[0199] 27. During the ceremony, R 4 is phenyl or 5-6 membered heteroaryl, preferably 5-6 membered heteroaryl is selected from the group comprising pyridyl, pyrrolyl, pyrazinyl, pyridazinyl, pyrimidinyl, thiophenyl, furanyl, thiazolyl, isothiazolyl and 1,2,5-thiadiazolyl, phenyl or pyridyl; Each of the above phenyl and 5- to 6-membered heteroaryl may be one or more Z 4 , preferably two or more Z 4 is replaced by each Z 4 are independently selected from halo, cyano, hydroxyl, oxo, and thioxo; or C 1~6 Alkyl, C3~10 Cycloalkyl, C 3~10 Cycloalkyl C 1~6 Alkyl, C 6~10 Aryl, C 6~10 Aryl C 1~6 Alkyl, HaloC 1~6 Alkyl, Cyano C 1~6 Alkyl, C 1~6 Alkoxy, Cyano C 1~6 Alkoxy, C 1~6 Alkylthio, HaloC 1~6 Alkoxy, Hydroxy C 1~6 Alkyl, C 1~6 Alkoxy C 1~6 Alkyl, C 3~10 Cycloalkyloxy, C 3~10 Cycloalkyl C 1~6 Alkoxy, C 1~6 Alkoxy, carboxyl, C 1~6 Alkoxycarbonyl, C 1~6 Alkyl carbonyl, C 6~10 Aryl C 1~6 alkoxy, each of which may be unsubstituted or may be selected from the group consisting of one or more Z 4a and preferably, each Z 4 are independently selected from halo, cyano, hydroxyl, oxo, or C 1~6 Alkyl, C 3~10 Cycloalkyl, C 3~10 Cycloalkyl C 1~6 Alkyl, C 6~10 Aryl, C 6~10 Aryl C 1~6 Alkyl, HaloC 1~6 Alkyl, Cyano C 1~6 Alkyl, C 1~6 Alkoxy, Cyano C 1~6 Alkoxy, HaloC 1~6 Alkoxy, C 1~6 Alkoxy C 1~6 Alkyl, C 3~10 Cycloalkyloxy, C 3~10 Cycloalkyl C 1~6 Alkoxy, C 1~6 Alkoxy C 1~6 Alkoxy, C1~6 Alkoxycarbonyl, C 1~6 alkylcarbonyl, each of which may be unsubstituted or may contain one or more Z 4a and preferably, each Z 4 are independently selected from halo, cyano, and oxo; or C 1~6 Alkyl, C 3~10 Cycloalkyl, C 6~10 Aryl, HaloC 1~6 Alkyl, Cyano C 1~6 Alkyl, C 1~6 Alkoxy, Cyano C 1~6 Alkoxy, HaloC 1~6 Alkoxy, C 1~6 Alkoxy C 1~6 Alkyl, C 3~10 Cycloalkyloxy, C 1~6 Alkoxycarbonyl, C 1~6 alkylcarbonyl, each of which may be unsubstituted or may contain one or more Z 4a may be substituted with and / or two Zs 4 can be taken together with the atom(s) to which they are attached to form a phenyl, a 5- to 6-membered heteroaryl, or a 5- to 6-membered saturated heterocyclyl, each of which may be unsubstituted or may contain one or more Z 4a may be substituted with each Z 4a are halo, cyano, hydroxyl, C 1~6 Alkyl, HaloC 1~6 Alkyl, C 1~6 Alkoxy, C 1~6 Alkylthio, HaloC 1~6 Alkoxy, Hydroxy C 1~6 Alkyl, C 1~6 Alkoxy C 1~6 Alkyl, C 3~10 Cycloalkyl, C 3~10 Cycloalkyloxy, C 6~10 Aryl, C 6~10 Aryl C 1~6Alkyl, amino, mono or di(C 1~6 alkyl)amino, mono- or di(C 1~6 Alkyl)amino C 1~6 27. The compound of any one of statements 1-26, wherein the compound is independently selected from the group consisting of alkyl, and oxo.

[0200] 28. During the ceremony, R 4 is phenyl or 5-6 membered heteroaryl, preferably the 5-6 membered heteroaryl is selected from the group comprising pyridyl, pyrazinyl, pyridazinyl, pyrimidinyl, pyrrolyl, thiophenyl, furanyl, thiazolyl, isothiazolyl and 1,2,5-thiadiazolyl, more preferably phenyl or pyridyl; Each of the above phenyl and 5- to 6-membered heteroaryl may have two or more Z 4 is replaced by each Z 4 are independently selected from halo, cyano, hydroxyl, oxo, or C 1~6 Alkyl, C 3~10 Cycloalkyl, C 3~10 Cycloalkyl C 1~6 Alkyl, C 6~10 Aryl, C 6~10 Aryl C 1~6 Alkyl, HaloC 1~6 Alkyl, Cyano C 1~6 Alkyl, C 1~6 Alkoxy, Cyano C 1~6 Alkoxy, HaloC 1~6 Alkoxy, C 1~6 Alkoxy C 1~6 Alkyl, C 3~10 Cycloalkyloxy, C 3~10 Cycloalkyl C 1~6 Alkoxy, C 1~6 Alkoxy C 1~6 Alkoxy, C 1~6 Alkoxycarbonyl, C 1~6 alkylcarbonyl, each of which may be unsubstituted or may contain one or more Z 4a and preferably, each Z 4are independently selected from halo, cyano, and oxo; or C 1~6 Alkyl, C 3~10 Cycloalkyl, C 6~10 Aryl, HaloC 1~6 Alkyl, Cyano C 1~6 Alkyl, C 1~6 Alkoxy, Cyano C 1~6 Alkoxy, HaloC 1~6 Alkoxy, C 1~6 Alkoxy C 1~6 Alkyl, C 3~10 Cycloalkyloxy, C 1~6 Alkoxycarbonyl, C 1~6 alkylcarbonyl, each of which may be unsubstituted or may contain one or more Z 4a may be substituted with and / or two Zs 4 can be taken together with the atom(s) to which they are attached to form a phenyl, a 5- to 6-membered heteroaryl (e.g., 1,2,5-thiadiazolyl), or a 5- to 6-membered saturated heterocyclyl (e.g., 1,3-dioxolanyl), each of which may be unsubstituted or may be substituted with one or more Z 4a may be substituted with each Z 4a are halo, cyano, hydroxyl, C 1~6 Alkyl, HaloC 1~6 Alkyl, C 1~6 Alkoxy, HaloC 1~6 Alkoxy, Hydroxy C 1~6 Alkyl, C 1~6 Alkoxy C 1~6 The compound of any one of statements 1-27, wherein the compound is independently selected from the group consisting of alkyl, and oxo.

[0201] 29.Structural formula (II) [ka] (In the formula, X 3 , X 4 , X 5 , X6 and X 7 are independently selected from CH or N, with the proviso that X 3 , X 4 , X 5 , X 6 and X 7 three or more of are not N, and n is an integer selected from 1, 2, 3, or 4; R 1 , R 2 , R 3 and Z 4 has the same meaning as in any one of statements 1 to 28).

[0202] 30. Structural formula (III) or (IV) [ka] (In the formula, X 3 , X 4 , X 5 and X 6 each is independently selected from CH or N; 3 , X 4 , X 5 , X 6 one or two of are N, where n is an integer selected from 1, 2, 3, or 4; R 1 , R 2 , R 3 and Z 4 has the same meaning as in any one of statements 1 to 28).

[0203] 31. Structural formula (V), (VI), (VII), (VIII), (Va), (VIa), (VIIa) or (VIIIa) [ka] (In the formula, X 3 , X 6 each is independently selected from CH or N; 3 , X 6At least one of X is N, and preferably 3 , X 6 and exactly one of the is N, wherein m is an integer selected from 0, 1, 2, or 3; o is an integer selected from 0, 1, or 2; p is an integer selected from 0 or 1; R 1 , R 2 , R 3 and Z 4 has the same meaning as in any one of statements 1 to 28).

[0204] 32. Structural formula (IX), (X) or (XI) [ka] (In the formula, X 8 , X 9 , X 10 , X 11 , and X 12 are independently selected from CH, N, O, or S; u is an integer selected from 0, 1, 2, or 3; and s is an integer selected from 0, 1, 2, 3, or 4; [ka] is any double bond, R 4 , R 1 , R 2 , R 3 and Z 1 has the same meaning as in any one of statements 1 to 28).

[0205] 33. Structural formula (XII), (XIII), (XIV), (XV), (XVI), (XVII), (XVIII), (XIX), or (XX) [ka] (In the formula, X 8 , X 9 , X 10 and X 11 are independently selected from CH, N, O, or S; 8 , X 9 , X 10 , and X 11 is selected from N, O, and S, u1 is an integer selected from 0, 1, 2, or 3, u is an integer selected from 1 or 2, and s is an integer selected from 0, 1, 2, 3, or 4; [ka] is any double bond, R 1 , R 2 , R 3 , R 4 and Z 1 has the same meaning as in any one of statements 1 to 28.

[0206] 34. Structural formula (II1), (II2) or (II3) [ka] (In the formula, X 3 , X 4 , X 5 , X 6 and X 7 are independently selected from CH or N, with the proviso that X 3 , X 4 , X 5 , X 6 and X 7 three or more of are not N, and n is an integer selected from 1, 2, 3, or 4; In the formula, X 8 , X 9 , X 10 , X 11 , and X 12are independently selected from CH, N, O, or S; u is an integer selected from 0, 1, 2, or 3; and s is an integer selected from 0, 1, 2, 3, or 4; [ka] is any double bond, R 1 , R 2 , R 3 , R 4 , X 2 , Z 1 and Z 4 has the same meaning as in any one of statements 1 to 28.

[0207] 35. Structural formula (III1), (III2), (III3), (III4), (III5), (III6), (III7), (III8), (III9), (IV1), (IV2), (IV3), (IV4), (IV5), (IV6), (IV7), (IV8) or (IV9) [ka] JPEG2024520882000014.jpg108165 (In the formula, X 8 , X 9 , X 10 and X 11 are independently selected from CH, N, O, or S; 8 , X 9 , X 10 , and X 11 is selected from N, O, and S, u1 is an integer selected from 0, 1, 2, or 3, u is an integer selected from 1 or 2, n is an integer selected from 1, 2, 3, or 4, and s is an integer selected from 0, 1, 2, 3, or 4; [ka] is any double bond, In the formula, X 3 , X 4 , X 5 and X 6 each is independently selected from CH or N; 3 , X 4 , X 5 , and X 6 one or two of are N, n is an integer selected from 1, 2, 3, or 4, and s is an integer selected from 0, 1, 2, 3, or 4; R 1 , R 2 , R 3 , R 4 , Z 1 and Z 4 has the same meaning as in any one of statements 1 to 28.

[0208] 36. Structural formula (V1), (VI1), (VII1), (VIII1), (V2), (VI2), (VII2), (VIII2), (V3), (VI3), (VII3), (VIII3), (V4), (VI4), (VII4), (VIII4), (V5), (VI5), (VII5) , (VIII5), (V6), (VI6), (VII6), (VIII6), (V7), (VI7), (VII7), (VIII7), (V8), (VI8), (VII8), (VIII8), (V9), (VI9), (VII9), (VIII9), (Va1), (VIa1), (V IIa1), (VIIIa1), (Va2), (VIa2), (VIIa2), (VIIIa2), (Va3), (VIa3), (VIIa3), (VIIIa3), (Va4), (VIa4), (VIIa4), (VIIIa4), (Va5), (VIa5), (VIIa5), (V IIIa5), (Va6), (VIa6), (VIIa6), (VIIIa6), (Va7), (VIa7), (VIIa7), (VIIIa7), (Va8), (VIa8), (VIIa8), (VIIIa8), (Va9), (VIa9), (VIIa9), or (VIIIa9) [ka] JPEG2024520882000017.jpg245165JPEG2024520882000018.jpg245165JPEG2024520882000019.jpg24516 5JPEG2024520882000020.jpg245165JPEG2024520882000021.jpg245165JPEG2024520882000022.jpg84165 wherein m is an integer selected from 0, 1, 2, or 3; o is an integer selected from 0, 1, or 2; p is an integer selected from 0 or 1; X 3 , X 6 each is independently selected from CH or N; 3 , X 6 At least one of is N and X 8 , X 9 , X 10 and X 11 are independently selected from CH, N, O, or S; 8 , X 9 , X 10 , and X 11 is selected from N, O, and S, u1 is an integer selected from 0, 1, 2, or 3, u is an integer selected from 1 or 2, n is an integer selected from 1, 2, 3, or 4, and s is an integer selected from 0, 1, 2, 3, or 4; [ka] is any double bond, R 1 , R 2 , R 3 , Z 1 , Z 4 and X 2 has the same meaning as in any one of statements 1 to 28).

[0209] 37. The compound according to any one of statements 1-36, wherein said compound is selected from the group of compounds listed in Table A.

[0210] 38. The compound is 2 H, 3 H, 13 C. 11 C. 14 C. 15 N, 18 O. 17 O. 31 P, 32 P, 35 S, 18 F, 36 C.I., 99m Tc, 111 In, 82 Rb, 137 Cs, 123 l, 125 l, 131 l, 67 Ga, 192 lr and 201 38. The compound of any one of statements 1-37, comprising at least one isotope selected from the group comprising TI isotopes.

[0211] 39. A pharmaceutical composition comprising a compound according to any one of statements 1 to 38 and a pharmaceutically acceptable carrier.

[0212] 40. A compound or pharmaceutical composition according to statements 1 to 39 for use as a medicament and / or in a diagnostic method.

[0213] 41. A compound according to any one of statements 1 to 38, or a pharmaceutical composition according to statement 39, for use in the prevention and / or treatment of a GPR17-mediated disorder.

[0214] 42. A compound according to any one of statements 1 to 38, or a pharmaceutical composition according to statement 39, for use in the prevention and / or treatment of a disorder or syndrome selected from disorders or syndromes associated with myelination disorders and brain tissue damage.

[0215] 43. Syndromes or disorders include multiple sclerosis (MS), including all of its various subtypes, such as clinically isolated syndrome (CIS); optic neuropathies, such as acute optic neuritis, chronic relapsing inflammatory optic neuritis, and neuromyelitis optica (NMO, Devic's disease); acute disseminated encephalomyelitis, acute hemorrhagic leukoencephalitis (AHL); periventricular leukomalacia; demyelination due to autoimmune diseases, such as anti-MAG peripheral neuropathy and anti-MOG-related spectrum disorders; genetic disorders with white matter involvement, such as, but not limited to, Sjogren's syndrome, systemic lupus erythematosus, Gaucher disease, and Niemann-Pick disease; leukodystrophies and hereditary leukoencephalopathy and adrenoleukodystrophies; demyelination due to viral or bacterial infection; demyelination due to traumatic brain tissue injury and nerve injury; hypoxia, stroke, or ischemia, or other cardiac conditions 43. A compound for use according to statement 41 or 42, or a pharmaceutical composition for use according to statement 41 or 42, selected from the group of: demyelination in response to vascular disease; demyelination due to exposure to carbon dioxide, cyanide, vitamin deficiency or other CNS toxins; centropontine and extrapontine myelinolysis; Schilder's disease; Balo concentric sclerosis; perinatal encephalopathy; neurodegenerative diseases such as amyotrophic lateral sclerosis (ALS), Alzheimer's disease (AD), multiple system atrophy, Parkinson's disease, Niemann-Pick disease, spinocerebellar ataxia (SCA) and Huntington's disease (HD); psychiatric disorders such as schizophrenia, bipolar disorder, depression and major depressive disorder; and peripheral myelinating diseases such as acute and chronic peripheral demyelinating neuropathies, Dejerine-Sottas syndrome or Charcot-Marie-Tooth disease.

[0216] 44. Syndromes or disorders include multiple sclerosis (MS), including its various subtypes, optic neuritis, neuromyelitis optica (Devic's disease), chronic relapsing inflammatory optic neuritis, acute disseminated encephalomyelitis, acute hemorrhagic leukoencephalitis (AHL), periventricular leukomalacia, demyelination due to viral or bacterial infection, central and extrapontine myelinolysis, demyelination due to traumatic brain tissue injury, demyelination in response to hypoxia, stroke or ischemia or other cardiovascular disease, demyelination due to carbon dioxide, cyanide or other CNS exposure, Schilder's disease, Balo concentric sclerosis, perinatal encephalopathy, muscle atrophy 44. A compound for use according to any one of statements 41 to 43, or a pharmaceutical composition for use according to any one of statements 41 to 43, selected from the group of neurodegenerative diseases such as apoplexy lateral sclerosis (ALS), Alzheimer's disease (AD), multiple system atrophy, Parkinson's disease, spinocerebellar ataxia (SCA) and Huntington's disease, psychiatric disorders such as schizophrenia and bipolar disorder, and peripheral myelination diseases such as leukodystrophies, peripheral neuropathies, Dejerine-Sottas syndrome or Charcot-Marie-Tooth disease.

[0217] 45. A compound according to any one of statements 1 to 38, or a pharmaceutical composition according to statement 39, for use in the prevention and / or treatment of multiple sclerosis (MS).

[0218] 46. ​​A compound according to statement 38 for use as a PET tracer or a SPECT tracer.

[0219] 47. A compound according to statement 46 for use in performing in vivo diagnosis and / or disease monitoring.

[0220] 48. A compound according to any one of statements 1 to 38 for use in the diagnosis and / or monitoring of a GPR17 related disease disclosed herein, preferably a demyelinating disease, preferably the diagnosis and monitoring of multiple sclerosis.

[0221] 49. A compound according to any one of statements 1 to 38 for use in diagnosing and / or monitoring the expression, distribution and / or activation of the GPR17 receptor in vivo, e.g. directly in a subject, e.g. using molecular imaging techniques, or in vitro, e.g. by examining any sample, such as a body fluid or tissue, taken from a subject.

[0222] 50. (a) a compound according to any one of statements 1 to 37, comprising as a first component a PET or PET tracer incorporating at least one radionuclide suitable for PET or SPECT imaging, or a compound according to statement 38; (b) as the second component, i. A compound according to any one of statements 1 to 37, wherein the compound does not incorporate a radionuclide; ii. A GPR17 modulating compound different from the compound of the invention defined in (i), and iii. A kit comprising a therapeutic agent selected from a drug for the treatment of myelin disorders, such as, but not limited to, a drug for use in the treatment of multiple sclerosis, provided that the drug does not have GPR17 modulating activity, and such compounds are known to those skilled in the art, including examples more fully described above.

[0223] 51. A method for preventing and / or treating a GPR17-mediated disorder, comprising administering to a patient in need thereof a therapeutically effective amount of a compound according to any one of statements 1-38.

[0224] 52. A method for preventing and / or treating a syndrome or disorder selected from disorders or syndromes associated with impaired myelination and brain tissue damage, comprising administering to a patient in need thereof a therapeutically effective amount of a compound according to any one of statements 1-38.

[0225] 53. Syndromes or disorders include multiple sclerosis (MS), including all of its various subtypes, such as clinically isolated syndrome (CIS); optic neuropathies, such as acute optic neuritis, chronic relapsing inflammatory optic neuritis, and neuromyelitis optica (NMO, Devic's disease); acute disseminated encephalomyelitis, acute hemorrhagic leukoencephalitis (AHL); periventricular leukomalacia; demyelination due to autoimmune diseases, such as anti-MAG peripheral neuropathy and anti-MOG-related spectrum disorders; inherited disorders with white matter involvement, such as, but not limited to, Sjogren's syndrome, systemic lupus erythematosus, Gaucher disease, and Niemann-Pick disease; leukodystrophies and hereditary leukoencephalopathy and adrenoleukodystrophies; demyelination due to viral or bacterial infection; demyelination due to traumatic brain tissue injury and nerve damage. demyelination in response to hypoxia, stroke or ischemia or other cardiovascular disease; demyelination due to exposure to carbon dioxide, cyanide, vitamin deficiency or other CNS toxins; centropontine and extrapontine myelinolysis; Schilder's disease; Balo concentric sclerosis; perinatal encephalopathy; neurodegenerative diseases such as amyotrophic lateral sclerosis (ALS), Alzheimer's disease (AD), multiple system atrophy, Parkinson's disease, Niemann-Pick disease, spinocerebellar ataxia (SCA) and Huntington's disease (HD); psychiatric disorders such as schizophrenia, bipolar disorder, depression and major depressive disorder; and the group of acute and chronic peripheral demyelinating neuropathies, peripheral myelinating diseases such as Dejerine-Sottas syndrome or Charcot-Marie-Tooth disease.

[0226] 54. Syndromes or disorders including its various subtypes include multiple sclerosis (MS), optic neuritis, neuromyelitis optica (Devic's disease), chronic relapsing inflammatory optic neuritis, acute disseminated encephalomyelitis, acute hemorrhagic leukoencephalitis (AHL), periventricular leukomalacia, demyelination due to viral infection, central and extrapontine myelinolysis, demyelination due to traumatic brain tissue injury, demyelination in response to hypoxia, stroke or ischemia or other cardiovascular diseases, demyelination due to carbon dioxide, cyanide or other CNS exposure, Schilder's disease, Balo concentric sclerosis, perinatal encephalopathy, and neurodegenerative diseases such as amyotrophic lateral sclerosis (ALS). 54. The method of any one of statements 51 to 53, wherein the method is associated with a myelination disorder selected from the group of psychiatric disorders such as Alzheimer's disease (AD), multiple system atrophy, Parkinson's disease, spinocerebellar ataxia (SCA) and Huntington's disease, schizophrenia and bipolar disorder, and peripheral myelination diseases such as leukodystrophies, peripheral neuropathies, Dejerine-Sottas syndrome or Charcot-Marie-Tooth disease.

[0227] The present invention relates to pyrrolyl-sulfonamides of formula (I) and any subgroup thereof, such as those of formula (II), (III), (IV), (V), (VI), (VII), (VIII), (Va), (Via), (VIIa), (VIIIa), (IX), (X), (XI), (XII), (XIII), (XIV), (XV), (XVI), (XVII), (XVIII), (XIX), (XX), (II1), (II2), (II3), (III1), (III2), (III3), (III4), (III5), (III6), (III7), (III8), (III9), (IV1), (IV2), (IV3), (IV4), (IV5), (IV6), (IV7), (IV8), (IV9), (V1), (VI1), (VII1), (VIII1) , (V2), (VI2), (VII2), (VIII2), (V3), (VI3), (VII3), (VIII3), (V4), (VI4), (VII4), (VIII4), (V5), (VI5), (VII5), (VIII5), (V6), (VI6) , (VII6), (VIII6), (V7), (VI7), (VII7), (VIII7), (V8), (VI8), (VII8), (VIII8), (V9), (VI9), (VII9), (VIII9), (Va1), (Via1), (VIIa1) , (VIIIa1), (Va2), (Via2), (VIIa2), (VIIIa2), (Va3), (Via3), (VIIa3), (VIIIa3), (Va4), (Via4), (VIIa4), (VIIIa4), (Va5), (Via5), (V or a compound of Formula IIa5), (VIIIa5), (Va6), (Via6), (VIIa6), (VIIIa6), (Va7), (Via7), (VIIa7), (VIIIa7), (Va8), (Via8), (VIIa8), (VIIIa8), (Va9), (Via9), (VIIa9), or (VIIIa9), or an isomer such as a stereoisomer and a tautomer, a stereoisomer, a salt such as a pharmaceutically and / or physiologically acceptable salt, a hydrate, a solvate, a polymorph, a prodrug, an isotope, or a co-crystal thereof.

[0228] In one embodiment, the present invention provides a compound of formula (I): (In the formula, R 1is aryl, heteroaryl, cycloalkyl, cycloalkenyl, cycloalkynyl, heterocyclyl and A 1 -X 1 -, preferably R 1 is selected from the group comprising aryl, heteroaryl, cycloalkyl, cycloalkenyl, heterocyclyl; R 2 is selected from the group comprising hydrogen, halo, cyano, alkyl, alkenyl, alkynyl, haloalkyl, haloalkenyl, haloalkynyl, alkoxy, alkenyloxy, alkynyloxy, alkylthio, alkenylthio, alkynylthio, haloalkoxy, alkoxyalkyl, mono- or di(alkyl)amino and mono- or di(alkyl)aminoalkyl, preferably R 2 is selected from the group comprising hydrogen, halo, cyano, alkyl, alkenyl, haloalkyl, haloalkenyl, alkoxy, alkenyloxy, alkylthio, alkenylthio, haloalkoxy, alkoxyalkyl, mono- or di-(alkyl)amino, and mono- or di-(alkyl)aminoalkyl) or any subgroup thereof.

[0229] In an alternative embodiment, the present invention provides a compound of formula (I): (In the formula, R 1 is selected from the group comprising hydrogen, halo, cyano, alkyl, alkenyl, alkynyl, haloalkyl, haloalkenyl, haloalkynyl, alkoxy, alkenyloxy, alkynyloxy, alkylthio, alkenylthio, alkynylthio, haloalkoxy, alkoxyalkyl, mono- or di(alkyl)amino and mono- or di(alkyl)aminoalkyl, preferably R 1 is selected from the group comprising hydrogen, halo, cyano, alkyl, alkenyl, haloalkyl, haloalkenyl, alkoxy, alkenyloxy, alkylthio, alkenylthio, haloalkoxy, alkoxyalkyl, mono- or di(alkyl)amino, and mono- or di(alkyl)aminoalkyl; R 2is aryl, heteroaryl, cycloalkyl, cycloalkenyl, cycloalkynyl, heterocyclyl and A 2 -X 2 -, preferably R 2 is aryl, heteroaryl, cycloalkyl, cycloalkenyl, heterocyclyl, and A 2 -X 2 -) or any subgroup thereof.

[0230] In a preferred embodiment of the invention, the compound of formula (I) is selected from the group of compounds listed in Table A below, or an isomer, e.g., stereoisomer and tautomer, stereoisomer, salt, e.g., pharmaceutically and / or physiologically acceptable salt, hydrate, solvate, polymorph, prodrug, isotope, or co-crystal thereof.

[0231] [Table 1] JPEG2024520882000025.jpg237165JPEG2024520882000026.jpg237165JPEG2024520882000027.jpg237165 JPEG2024520882000028.jpg237165JPEG2024520882000029.jpg237165JPEG2024520882000030.jpg237165 JPEG2024520882000031.jpg237165JPEG2024520882000032.jpg237165JPEG2024520882000033.jpg237165 JPEG2024520882000034.jpg237165JPEG2024520882000035.jpg237165JPEG2024520882000036.jpg118165

[0232] Any reference to a compound according to the invention also includes isomers, e.g., stereoisomers and tautomers, salts, e.g., pharmaceutically and / or physiologically acceptable salts, hydrates, solvates, polymorphs, prodrugs, isotopes, and co-crystals of such compounds, unless otherwise specified.

[0233] As used herein, the term "isomer" refers to all possible isomers (but not positional isomers), including tautomers and stereochemical forms that the compounds of the formulae herein may possess. Typically, the structures shown herein illustrate one tautomer or resonance form of a compound, although corresponding alternative configurations are also contemplated.

[0234] Depending on their substitution patterns, compounds of the present invention may or may not possess one or more optical stereocenters and may exist as different enantiomers or diastereomers. All such enantiomers, diastereomers, or other optical isomers are encompassed within the scope of the present invention. Unless otherwise specified, the chemical name of a compound is a name for a mixture of all possible stereochemical isomers, which mixture contains all diastereomers and enantiomers of the basic molecular structure (since compounds of the formulae herein may have at least one chiral center) as well as stereochemically pure or enriched compounds. More specifically, stereocenters may have either the R or S configuration, and bonds may have either the cis or trans configuration. The terms R and S configuration are used herein in accordance with Chemical Abstracts nomenclature. The terms cis and trans are used herein in accordance with Chemical Abstracts nomenclature and include reference to the position of substituents on ring moieties. The absolute stereochemical configuration of compounds of the formulae described herein can be readily determined by one of ordinary skill in the art using well-known methods, such as, for example, X-ray diffraction.

[0235] The term "pharmaceutically acceptable salt" relates to any salt that a compound can form and that is suitable for administration to a subject according to the invention, in particular a human subject. Thus, the compounds of the present invention can optionally be used in the form of salts of the compounds herein, in particular salts of, for example, Na + , Li + , K. + , Ca 2+ and Mg 2+ These salts include pharmaceutically acceptable, non-toxic salts containing the following: (I) (II) (III) (IV ... Furthermore, because compounds can exist in a variety of different forms, the present invention is intended to encompass not only forms of compounds associated with a counterion (e.g., dry salts), but also forms not associated with a counterion (e.g., aqueous or organic solutions). Metal salts are typically prepared by reacting a metal hydroxide with a compound of the present invention. Examples of metal salts prepared in this manner include Li + , Na + and K. +and (iii) a salt containing the compound (III). Less soluble metal salts can be precipitated from the solution of a more soluble salt by the addition of the appropriate metal compound. Furthermore, salts can be formed by acid addition of certain organic and inorganic acids to basic centers, typically amines, or acidic groups. Examples of such suitable acids include, for example, inorganic acids such as hydrohalic acids, e.g., hydrochloric acid or hydrobromic acid, sulfuric acid, nitric acid, phosphoric acid, and the like, or organic acids such as acetic acid, propanoic acid, hydroxyacetic acid, 2-hydroxypropanoic acid, 2-oxopropanoic acid, lactic acid, pyruvic acid, oxalic acid (i.e., ethanedioic acid), malonic acid, succinic acid (i.e., butanedioic acid), maleic ...

Claims

1. Formula (I) 【Chemical 1】 (wherein, R １ is selected from the group consisting of aryl, heteroaryl, cycloalkyl, cycloalkenyl, cycloalkynyl, heterocyclyl and A １ -X １ -, and R ２ is selected from the group consisting of hydrogen, halo, cyano, alkyl, alkenyl, alkynyl, haloalkyl, haloalkenyl, haloalkynyl, alkoxy, alkenyloxy, alkynyloxy, alkylthio, alkenylthio, alkynylthio, haloalkoxy, alkoxyalkyl, mono- or di(alkyl)amino and mono- or di(alkyl)aminoalkyl) R １ said aryl, heteroaryl, cycloalkyl, cycloalkenyl, cycloalkynyl, heterocyclyl, X １ and A １ each of which may be unsubstituted or substituted with one or more Z １ and may be substituted, X １ is -Y １ｂ -Y １ａ -Y １ｃ - and in the formula, Y １ａ is a single bond, a double bond or a triple bond, or -CR １ａ =CR １ａ -, -C≡C-, -CO-, -O-, -CS-, -S-, -SO ２ -, -SO-, -SO(NH)-, -CONR １ｂ -, -NR １ｂ CO-, -SO ２ NR １ｂ -, -NR １ｂ SO ２ -, -S(O)-NR １ｂ -, and -NR １ｂ - and is selected from the group consisting of Y １ｂ and Y １ｃ each of which is independently selected from the group consisting of a single bond, or C １～３ alkylene, C ２～３ alkenylene, C ２～３ alkynylene, and each of the C １～３ alkylene, C ２～３ alkenylene, C ２～３ alkynylene may be unsubstituted or substituted with one or more R １ａ , and where Y １ａ is a single bond, double bond or triple bond, at least one of Y １ｂ and Y １ｃ is not a single bond Each R １ａ is independently selected from the group consisting of hydrogen, oxo, thioxo, halo, hydroxy, haloalkyl, alkoxy, alkoxyalkyl, haloalkoxy, haloalkoxyalkyl, mono- or di(alkyl)amino, mono- or di(alkyl)aminoalkyl, and alkyl, A １ is selected from the group consisting of aryl, heteroaryl, cycloalkyl, cycloalkenyl, cycloalkynyl and heterocyclyl, Each Z １ is independently selected from halo, cyano, oxo, nitro, thioxo, or is hydroxy, thio, alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkylalkyl, cycloalkenyl, cycloalkynyl, cycloalkenylalkyl, cycloalkynylalkyl, aryl, arylalkyl, haloalkyl, haloalkenyl, haloalkynyl, cyanoalkyl, alkoxy, alkenyloxy, alkynyloxy, cyanoalkoxy, alkylthio, alkenylthio, alkynylthio, haloalkoxy, hydroxyalkyl, alkoxyalkyl, cycloalkyloxy, cycloalkylalkoxy, alkoxyalkoxy, carboxyl, alkoxycarbonyl, alkylcarbonyl, arylalkoxy, amino, mono- or di-(alkyl)amino, aminoalkyl, mono- or di-(alkyl)aminoalkyl, mono- or di-(alkyl)aminocarbonyl, heterocyclyl, heteroaryl, heterocyclylalkyl, heteroarylalkyl, arylalkenyl, arylalkynyl, haloalkenyloxy, haloalkynyloxy, hydroxyalkenyl, hydroxyalkynyl, alkenyloxyalkyl, alkynyloxyalkyl, alkoxyalkenyl, alkoxyalkynyl, alkenyloxyalkoxy, alkynyloxyalkoxy, alkenyloxycarbonyl, alkynyloxycarbonyl, alkenylcarbonyl, alkynylcarbonyl, aminoalkenyl, aminoalkynyl, mono- or di-(alkyl)aminoalkenyl, mono- or di-(alkyl)aminoalkynyl, heterocyclylalkenyl, heterocyclylalkynyl, heteroarylalkenyl, heteroarylalkynyl, aryloxy, aryloxyalkyl, aryloxyalkenyl, aryloxyalkynyl, arylthio, haloalkylthio, cycloalkylthio, alkylsulfinyl, alkylsulfonyl, cycloalkylsulfinyl, cycloalkylsulfonyl, arylsulfinyl, arylsulfonyl, mono- or di-(alkyl)aminosulfonyl, mono- or di-(alkyl)aminosulfinyl, alkoxycarbonylamino, alkenyloxycarbonylamino, alkynyloxycarbonylamino, alkylcarbonylamino, alkenylcarbonylamino,Alkynylcarbonylamino, cycloalkylcarbonylamino, arylcarbonylamino, cycloalkylcarbonyl, arylcarbonyl, mono- or di(alkyl)aminocarbonyl, alkylcarbonyloxy, alkenylcarbonyloxy, alkynylcarbonyloxy, sulfonyl, sulfinyl, mono- or di(alkyl)aminoalkylamino, mono- or di(alkyl)aminoalkoxy, arylamino, arylaminoalkyl, alkylcarbonyloxyalkyl, alkenylcarbonyloxyalkyl, alkynylcarbonyloxyalkyl, arylcarbonyloxy, arylcarbonyloxyalkyl, arylaminocarbonyl, heterocyclyloxy, heteroaryloxy, heteroarylthio, heteroaryloxyalkyl, heteroaryloxyalkenyl, heteroaryloxyalkynyl, heteroarylsulfinyl, heteroarylsulfonyl, heteroarylamino, heteroarylaminoalkyl, heteroarylcarbonylamino, heteroarylcarbonyl, heteroarylcarbonyloxy, heteroarylcarbonyloxyalkyl, and heteroarylaminocarbonyl, each independently selected from the group, each of said group may be unsubstituted or substituted with one or more Z, １ａ and may be substituted with and / or two Zs １ together with the atom(s) to which they are attached can form an aryl, cycloalkyl, heteroaryl or heterocyclyl, each of said aryl, cycloalkyl, heteroaryl and heterocyclyl may be unsubstituted or substituted with one or more Zs １ａ and may be substituted and / or one R １ａ is one Z １ and together with the atom(s) to which they are attached, can form a cycloalkyl, 4- to 10-membered saturated or partially saturated heterocyclyl, 5- to 10-membered heteroaryl, or aryl, each of said cycloalkyl, heterocyclyl, heteroaryl or aryl may be unsubstituted or substituted with one or more Z １ａ and may be substituted with R １ｂ is hydrogen or alkyl, or R １ｂ is one Z １ and together with the atom(s) to which they are attached can form a 4- to 10-membered saturated or partially saturated heterocyclyl or a 5- to 10-membered heteroaryl, each of said heterocyclyl or heteroaryl may be unsubstituted or substituted with one or more Z １ａ and may be substituted with Each Z １ａ is independently selected from the group consisting of halo, cyano, hydroxyl, alkyl, alkenyl, alkynyl, haloalkyl, haloalkenyl, haloalkynyl, alkoxy, alkenyloxy, alkynyloxy, alkylthio, alkenylthio, alkynylthio, haloalkoxy, hydroxyalkyl, alkoxyalkyl, cycloalkyl, cycloalkenyl, cycloalkynyl, cycloalkyloxy, aryl, arylalkyl, amino, mono- or di(alkyl)amino, mono- or di(alkyl)aminoalkyl and oxo, or R １ is selected from the group consisting of hydrogen, halo, cyano, alkyl, alkenyl, alkynyl, haloalkyl, haloalkenyl, haloalkynyl, alkoxy, alkenyloxy, alkynyloxy, alkylthio, alkenylthio, alkynylthio, haloalkoxy, alkoxyalkyl, mono- or di(alkyl)amino and mono- or di(alkyl)aminoalkyl, and R ２ is selected from the group consisting of aryl, heteroaryl, cycloalkyl, cycloalkenyl, cycloalkynyl, heterocyclyl and A ２ -X ２ - and is selected from the group comprising R ２ each of said aryl, heteroaryl, cycloalkyl, cycloalkenyl, cycloalkynyl, heterocyclyl, X ２ and A ２ may each be unsubstituted or substituted with one or more Z ２ and X ２ is -Y ２ｂ -Y ２ａ -Y ２ｃ - and in the formula, Y ２ａ is a single bond, a double bond or a triple bond, or -CR ２ａ =CR ２ａ -, -C≡C-, -CO-, -O-, -CS-, -S-, -SO ２ -, -SO-, -SO(NH)-, -CONR ２ｂ -, -NR ２ｂ CO-, -SO ２ NR ２ｂ -, -NR ２ｂ SO ２ -, -S(O)-NR ２ｂ - and -NR ２ｂ - and is selected from the group consisting of Y ２ｂ and Y ２ｃ each of which is independently selected from the group consisting of a single bond, or C １～３ alkylene, C ２～３ alkenylene, C ２～３ alkynylene, and each of said C １～３ alkylene, C ２～３ alkenylene, C ２～３ alkynylene may be unsubstituted or substituted with one or more R ２ａ s, and where Y ２ａ is a single bond, double bond or triple bond, at least one of Y ２ｂ and Y ２ｃ is not a single bond Each R ２ａ is independently selected from the group consisting of hydrogen, oxo, thioxo, halo, hydroxy, haloalkyl, alkoxy, alkoxyalkyl, haloalkoxy, haloalkoxyalkyl, mono- or di(alkyl)amino, mono- or di(alkyl)aminoalkyl, and alkyl, A ２ is selected from the group including aryl, heteroaryl, cycloalkyl, cycloalkenyl, cycloalkynyl and heterocyclyl, Each Z ２ is independently selected from halo, cyano, oxo, nitro, thioxo, or is hydroxy, thio, alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkylalkyl, cycloalkenyl, cycloalkynyl, cycloalkenylalkyl, cycloalkynylalkyl, aryl, arylalkyl, arylalkenyl, arylalkynyl, haloalkyl, haloalkenyl, haloalkynyl, cyanoalkyl, alkoxy, alkenyloxy, alkynyloxy, cyanoalkoxy, alkylthio, alkenylthio, alkynylthio, haloalkoxy, haloalkenyloxy, haloalkynyloxy, hydroxyalkyl, hydroxyalkenyl, hydroxyalkynyl, alkoxyalkyl, alkenyloxyalkyl, alkynyloxyalkyl, alkoxyalkenyl, alkoxyalkynyl, cycloalkyloxy, cycloalkylalkoxy, alkoxyalkoxy, alkenyloxyalkoxy, alkynyloxyalkoxy, carboxyl, alkoxycarbonyl, alkenyloxycarbonyl, alkynyloxycarbonyl, alkylcarbonyl, alkenylcarbonyl, alkynylcarbonyl, arylalkoxy, amino, mono- or di-(alkyl)amino, aminoalkyl, aminoalkenyl, aminoalkynyl, mono- or di-(alkyl)aminoalkyl, mono- or di-(alkyl)aminoalkenyl, mono- or di-(alkyl)aminoalkynyl, mono- or di-(alkyl)aminocarbonyl, heterocyclyl, heteroaryl, heterocyclylalkyl, heteroarylalkyl, heterocyclylalkenyl, heterocyclylalkynyl, heteroarylalkenyl, heteroarylalkynyl, aryloxy, aryloxyalkyl, aryloxyalkenyl, aryloxyalkynyl, arylthio, haloalkylthio, cycloalkylthio, alkylsulfinyl, alkylsulfonyl, cycloalkylsulfinyl, cycloalkylsulfonyl, arylsulfinyl, arylsulfonyl, mono- or di-(alkyl)aminosulfonyl, mono- or di-(alkyl)aminosulfinyl, alkoxycarbonylamino, alkenyloxycarbonylamino, alkynyloxycarbonylamino, alkylcarbonylamino, alkenylcarbonylamino,Alkynylcarbonylamino, cycloalkylcarbonylamino, arylcarbonylamino, cycloalkylcarbonyl, arylcarbonyl, mono- or di(alkyl)aminocarbonyl, alkylcarbonyloxy, alkenylcarbonyloxy, alkynylcarbonyloxy, arylcarbonyloxy, sulfonyl, sulfinyl, mono- or di(alkyl)aminoalkylamino, mono- or di(alkyl)aminoalkoxy, arylamino, arylaminoalkyl, alkylcarbonyloxyalkyl, alkenylcarbonyloxyalkyl, alkynylcarbonyloxyalkyl, arylcarbonyloxy, arylcarbonyloxyalkyl, arylaminocarbonyl, heterocyclyloxy, heteroaryloxy, heteroarylthio, heteroaryloxyalkyl, heteroaryloxyalkenyl, heteroaryloxyalkynyl, heteroarylsulfinyl, heteroarylsulfonyl, heteroarylamino, heteroarylaminoalkyl, heteroarylcarbonylamino, heteroarylcarbonyl, heteroarylcarbonyloxy, heteroarylcarbonyloxyalkyl and heteroarylaminocarbonyl, independently selected from the group consisting of, each of said groups may be unsubstituted or substituted with one or more Z, ２ａ and may be substituted with, and / or two Zs ２ can together with the atom(s) to which they are attached form an aryl, cycloalkyl, heteroaryl or heterocyclyl, each of said aryl, cycloalkyl, heteroaryl and heterocyclyl may be unsubstituted or substituted with one or more Zs ２ａ and may be substituted and / or one R ２ａ is one Z ２ and together with the atom(s) to which they are attached can form cycloalkyl, 4- to 10-membered saturated or partially saturated heterocyclyl, 5- to 10-membered heteroaryl, or aryl, each of said cycloalkyl, heterocyclyl, heteroaryl or aryl may be unsubstituted or substituted with one or more Z ２ａ and may be substituted with R ２ｂ is hydrogen or alkyl, or R ２ｂ is one Z ２ and together with the atom(s) to which they are attached can form a 4- to 10-membered saturated or partially saturated heterocyclyl or a 5- to 10-membered heteroaryl, each of said heterocyclyl or heteroaryl may be unsubstituted or substituted with one or more Z ２ａ and may be substituted with, Each Z ２ａ is independently selected from the group consisting of halo, cyano, hydroxyl, alkyl, alkenyl, alkynyl, haloalkyl, haloalkenyl, haloalkynyl, alkoxy, alkenyloxy, alkynyloxy, alkylthio, alkenylthio, alkynylthio, haloalkoxy, hydroxyalkyl, alkoxyalkyl, cycloalkyl, cycloalkenyl, cycloalkynyl, cycloalkyloxy, aryl, arylalkyl, amino, mono- or di(alkyl)amino, mono- or di(alkyl)aminoalkyl, and oxo; R ３ is selected from the group consisting of hydrogen, halo, cyano, alkyl, alkenyl, alkynyl, haloalkyl, haloalkenyl, haloalkynyl, alkoxy, alkenyloxy, alkynyloxy, alkylthio, alkenylthio, alkynylthio, haloalkoxy, alkoxyalkyl, mono- or di(alkyl)amino and mono- or di(alkyl)aminoalkyl, R ４ is aryl or heteroaryl, Each of said aryl and heteroaryl is substituted with one or more Z ４ and Each Z ４ is independently selected from halo, cyano, oxo, nitro, thioxo, or is hydroxy, thio, alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkylalkyl, cycloalkenyl, cycloalkynyl, cycloalkenylalkyl, cycloalkynylalkyl, aryl, arylalkyl, arylalkenyl, arylalkynyl, haloalkyl, haloalkenyl, haloalkynyl, cyanoalkyl, alkoxy, alkenyloxy, alkynyloxy, cyanoalkoxy, alkylthio, alkenylthio, alkynylthio, haloalkoxy, haloalkenyloxy, haloalkynyloxy, hydroxyalkyl, hydroxyalkenyl, hydroxyalkynyl, alkoxyalkyl, alkenyloxyalkyl, alkynyloxyalkyl, alkoxyalkenyl, alkoxyalkynyl, cycloalkyloxy, cycloalkylalkoxy, alkoxyalkoxy, alkenyloxyalkoxy, alkynyloxyalkoxy, carboxyl, alkoxycarbonyl, alkenyloxycarbonyl, alkynyloxycarbonyl, alkylcarbonyl, alkenylcarbonyl, alkynylcarbonyl, arylalkoxy, amino, mono- or di(alkyl)amino, aminoalkyl, aminoalkenyl, aminoalkynyl, mono- or di(alkyl)aminoalkyl, mono- or di(alkyl)aminoalkenyl, mono- or di(alkyl)aminoalkynyl, mono- or di(alkyl)aminocarbonyl, heterocyclyl, heteroaryl, heterocyclylalkyl, heteroarylalkyl, heterocyclylalkenyl, heterocyclylalkynyl, heteroarylalkenyl, heteroarylalkynyl, aryloxy, aryloxyalkyl, aryloxyalkenyl, aryloxyalkynyl, arylthio, haloalkylthio, cycloalkylthio, alkylsulfinyl, alkylsulfonyl, cycloalkylsulfinyl, cycloalkylsulfonyl, arylsulfinyl, arylsulfonyl, mono- or di(alkyl)aminosulfonyl, mono- or di(alkyl)aminosulfinyl, alkoxycarbonylamino, alkenyloxycarbonylamino, alkynyloxycarbonylamino, alkylcarbonylamino, alkenylcarbonylamino,Alkynylcarbonylamino, cycloalkylcarbonylamino, arylcarbonylamino, cycloalkylcarbonyl, arylcarbonyl, mono- or di(alkyl)aminocarbonyl, alkylcarbonyloxy, alkenylcarbonyloxy, alkynylcarbonyloxy, arylcarbonyloxy, sulfonyl, sulfinyl, mono- or di(alkyl)aminoalkylamino, mono- or di(alkyl)aminoalkoxy, arylamino, arylaminoalkyl, alkylcarbonyloxyalkyl, alkenylcarbonyloxyalkyl, alkynylcarbonyloxyalkyl, arylcarbonyloxy, arylcarbonyloxyalkyl, arylaminocarbonyl, heterocyclyloxy, heteroaryloxy, heteroarylthio, heteroaryloxyalkyl, heteroaryloxyalkenyl, heteroaryloxyalkynyl, heteroarylsulfinyl, heteroarylsulfonyl, heteroarylamino, heteroarylaminoalkyl, heteroarylcarbonylamino, heteroarylcarbonyl, heteroarylcarbonyloxy, heteroarylcarbonyloxyalkyl and heteroarylaminocarbonyl, each independently selected from the group consisting of, each of said groups may be unsubstituted or substituted with one or more Z, ４ａ and may be substituted with, and / or two Zs ４ can, together with the atom(s) to which they are attached, form an aryl, cycloalkyl, heteroaryl or heterocyclyl, each of said aryl, heteroaryl, cycloalkyl, and heterocyclyl may be unsubstituted or substituted with one or more Zs ４ａ and may be substituted Each Z ４ａ is independently selected from the group consisting of halo, cyano, hydroxyl, alkyl, alkenyl, alkynyl, haloalkyl, haloalkenyl, haloalkynyl, alkoxy, alkenyloxy, alkynyloxy, alkylthio, alkenylthio, alkynylthio, haloalkoxy, hydroxyalkyl, alkoxyalkyl, cycloalkyl, cycloalkenyl, cycloalkynyl, cycloalkyloxy, aryl, arylalkyl, amino, mono- or di(alkyl)amino, mono- or di(alkyl)aminoalkyl, and oxo, Provided that R １ is A １ -X １ -, and X １ is -CO-, and A １ is heterocyclyl, A １ is not bonded to X via the N ring atom of the heterocyclyl １ and R １ When R is heteroaryl, １ R is not oxadiazolyl, R ２ is A ２ -X ２ -, and X ２ is -CO-, and A ２ is heterocyclyl, A ２ is not bonded to X via the N ring atoms of the heterocyclyl ２ and R ２ When R is heteroaryl, ２ R is not oxadiazolyl, Provided that the compound is N,4-bis(4-methylphenyl)-1H-pyrrole-3-sulfonamide; (CAS No. 1427286-05-2), a compound other than N,4-bis(4-chlorophenyl)-1H-pyrrole-3-sulfonamide (CAS No. 1427286-06-3), or a tautomer, stereoisomer, hydrate, solvate, polymorph, prodrug, isotope or cocrystal thereof, or a pharmaceutically acceptable salt thereof.

2. R １ is selected from the group consisting of C ６～１０ aryl, 5- to 10-membered heteroaryl, C ３～１０ cycloalkyl, C ５～１０ cycloalkenyl, 3- to 10-membered saturated or partially saturated heterocyclyl, and A １ -X １ -, and is selected from the group consisting of: R １ said C of ６～１０ aryl, 5- to 10-membered heteroaryl, C ３～１０ cycloalkyl, C ５～１０ cycloalkenyl, 3- to 10-membered saturated or partially saturated heterocyclyl, X １ and A １ each of which may be unsubstituted or substituted with one or more Z １ and may be R ２ is hydrogen, halo, cyano, C １～６ alkyl, C ２～６ alkenyl, haloC １～６ alkyl, haloC ２～６ alkenyl, C １～６ alkoxy, C ２～６ alkenyloxy, C １～６ alkylthio, C ２～６ alkenylthio, haloC １～６ alkoxy, C １～６ alkoxyC １～６ alkyl, mono- or di(C １～６ alkyl)amino, and mono- or di(C １～６ alkyl)aminoC １～６ alkyl, and is a compound according to claim 1 selected from the group consisting of.

3. X １ is -Y １ｂ -Y １ａ -Y １ｃ -, wherein Y １ａ is a single bond, a double bond or a triple bond, or -CR １ａ =CR １ａ -, -C≡C-, -CO-, -O-, -CS-, -S-, -SO ２ -, -SO-, -SO(NH)-, -CONR １ｂ -, -NR １ｂ CO-, -SO ２ NR １ｂ -, -NR １ｂ SO ２ -, -S(O)-NR １ｂ - and -NR １ｂ - and is selected from the group consisting of Y １ｂ and Y １ｃ each of which is independently selected from the group consisting of a single bond, or C １～３ alkylene, C ２～３ alkenylene, C ２～３ alkynylene, and each of said C １～３ alkylene, C ２～３ alkenylene, C ２～３ alkynylene may be unsubstituted or substituted with one or more R １ａ wherein when Y １ａ is a single bond, double bond or triple bond, at least one of Y １ｂ and Y １ｃ is not a single bond Each R １ａ is independently selected from the group consisting of hydrogen, oxo, thioxo, halo, hydroxy, haloC １～６ alkyl, C １～６ alkoxy, C １～６ alkoxyC １～６ alkyl, haloC １～６ alkoxy, haloC １～６ alkoxyC １～６ alkyl, mono- or di(C １～６ alkyl)amino, mono- or di(C １～６ alkyl)aminoC １～６ alkyl, and C １～６ alkyl, and is independently selected from the group containing them, A １ is C ６～１０ aryl, 5- to 10-membered heteroaryl, C ３～１０ cycloalkyl, C ５～１０ cycloalkenyl, and is selected from the group consisting of 3- to 10-membered saturated or partially saturated heterocyclyl, and / or, one R １ａ is one Z １ and together with the atom(s) to which they are attached forms a C ４～１０ cycloalkyl, or a 4- to 10-membered saturated or partially saturated heterocyclyl, or a 5- to 10-membered heteroaryl, wherein each of said C ４～１０ cycloalkyl, heterocyclyl or heteroaryl may be unsubstituted or substituted with one or more Z １ａ and may be substituted, R １ｂ is hydrogen or C １～６ alkyl, the compound according to claim 1.

4. R ２ is selected from the group consisting of C ６～１０ aryl, 5- to 10-membered heteroaryl, C ３～１０ cycloalkyl, C ５～１０ cycloalkenyl, 3- to 10-membered saturated or partially saturated heterocyclyl, and A ２ -X ２ -, and is selected from the group consisting of: R ２ said C of ６～１０ aryl, 5- to 10-membered heteroaryl, C ３～１０ cycloalkyl, C ５～１０ cycloalkenyl, 3- to 10-membered saturated or partially saturated heterocyclyl, X ２ and A ２ each of which may be unsubstituted or substituted with one or more Z ２ and may be R １ is hydrogen, halo, cyano, C １～６ alkyl, C ２～６ alkenyl, haloC １～６ alkyl, haloC ２～６ alkenyl, C １～６ alkoxy, C ２～６ alkenyloxy, C １～６ alkylthio, C ２～６ alkenylthio, haloC １～６ alkoxy, C １～６ alkoxyC １～６ alkyl, mono- or di(C １～６ alkyl)amino, and mono- or di(C １～６ alkyl)aminoC １～６ alkyl, and is a compound according to claim 1 selected from the group consisting of.

5. X ２ is -Y ２ｂ -Y ２ａ -Y ２ｃ -, wherein Y ２ａ is a single bond, a double bond or a triple bond, or -CR ２ａ =CR ２ａ -, -C≡C-, -CO-, -O-, -CS-, -S-, -SO ２ -, -SO-, -SO(NH)-, -CONR ２ｂ -, -NR ２ｂ CO-, -SO ２ NR ２ｂ -, -NR ２ｂ SO ２ -, -S(O)-NR ２ｂ -, and -NR ２ｂ - and is selected from the group consisting of Y ２ｂ and Y ２ｃ each of which is independently selected from the group consisting of a single bond, or C １～３ alkylene, C ２～３ alkenylene, C ２～３ alkynylene, and each of said C １～３ alkylene, C ２～３ alkenylene, C ２～３ alkynylene may be unsubstituted or substituted with one or more R ２ａ wherein when Y ２ａ is a single bond, double bond or triple bond, at least one of Y ２ｂ and Y ２ｃ is not a single bond Each R ２ａ is independently selected from the group consisting of hydrogen, oxo, thioxo, halo, hydroxy, haloC １～６ alkyl, C １～６ alkoxy, C １～６ alkoxyC １～６ alkyl, haloC １～６ alkoxy, haloC １～６ alkoxyC １～６ alkyl, mono- or di(C １～６ alkyl)amino, mono- or di(C １～６ alkyl)aminoC １～６ alkyl, and C １～６ alkyl, and is selected independently from the group containing A ２ is C ６～１０ aryl, 5- to 10-membered heteroaryl, C ３～１０ cycloalkyl, C ５～１０ cycloalkenyl, and is selected from the group consisting of 3- to 10-membered saturated or partially saturated heterocyclyl, and / or, one R ２ａ is one Z ２ and together with the atom(s) to which they are attached form a C ４～１０ cycloalkyl, or a 4- to 10-membered saturated or partially saturated heterocyclyl, or a 5- to 10-membered heteroaryl, and each of said C ４～１０ cycloalkyl, heterocyclyl or heteroaryl may be unsubstituted or substituted with one or more Z ２ａ and may be substituted, R ２ｂ is hydrogen or C １～６ alkyl, the compound according to claim 1.

6. R ３ is hydrogen, halo, cyano, C １～６ alkyl, C ２～６ alkenyl, haloC １～６ alkyl, haloC ２～６ alkenyl, C １～６ alkoxy, C ２～６ alkenyloxy, C １～６ alkylthio, C ２～６ alkenylthio, haloC １～６ alkoxy, C １～６ alkoxyC １～６ alkyl, mono- or di(C １～６ alkyl)amino, and mono- or di(C １～６ alkyl)aminoC １～６ alkyl, and is a compound according to claim 1 selected from the group consisting of.

7. R ４ is C ６～１０ aryl or 5- to 10-membered heteroaryl, Said C ６～１０ Each of aryl and 5- to 10-membered heteroaryl is substituted with one or more Z ４ The compound according to claim 1, wherein the compound is substituted with one or more Z

8. Structural formula (II) [Chemical 2] (wherein each of X ３ , X ４ , X ５ , X ６ and X ７ is independently selected from CH or N, provided that three or more of X ３ , X ４ , X ５ , X ６ and X ７ are not N, and n is an integer selected from 1, 2, 3, or 4, R １ , R ２ , R ３ and Z ４ (which has the same meaning as in claim 1), the compound according to claim 1.

9. Structural formula (IX), (X) or (XI) 【Chemical Formula 3】 (wherein X ８ , X ９ , X １０ , X １１ , and X １２ each is independently selected from CH, N, O, or S, u is an integer selected from 0, 1, 2, or 3, s is an integer selected from 0, 1, 2, 3, or 4, 【Chemical Formula 4】 is an arbitrary double bond R ４ , R １ , R ２ , R ３ and Z １ (which has the same meaning as in claim 1), the compound according to claim 1.

10. The compound according to claim 1, wherein the compound is selected from the group consisting of the compounds listed in Table A.

11. A pharmaceutical composition comprising the compound according to claim 1 and a pharmaceutically acceptable carrier.

12. The compound according to any one of claims 1 to 10, or the pharmaceutical composition according to claim 11, for use as a medicament.

13. The compound according to claim 1, for use in the prevention and / or treatment of GPR17-mediated disorders.

14. The pharmaceutical composition according to claim 11, for use in the prevention and / or treatment of GPR17-mediated disorders.

15. The compound according to claim 1, for use in the prevention or treatment of a disorder or syndrome selected from disorders or syndromes associated with demyelination disorders and brain tissue damage.

16. The pharmaceutical composition according to claim 11, for use in the prevention or treatment of a disorder or syndrome selected from disorders or syndromes associated with demyelination disorders and brain tissue damage.

17. wherein the syndrome or disorder is multiple sclerosis (MS) including subtypes; optic neuropathy; acute disseminated encephalomyelitis, acute hemorrhagic leukoencephalitis (AHL); periventricular leukomalacia; demyelination due to autoimmune disease; hereditary diseases with white matter lesions; leukodystrophy and hereditary leukencephalopathy and adrenoleukodystrophy; demyelination due to viral or bacterial infection; demyelination due to traumatic brain tissue injury and nerve injury; demyelination in response to hypoxia, stroke or ischemia or other cardiovascular diseases; demyelination due to exposure to carbon dioxide, cyanide, vitamin deficiency or other CNS toxins; central pontine and extrapontine myelinolysis; Schilder's disease; Baló concentric sclerosis; perinatal encephalopathy; neurodegenerative diseases; mental disorders; and a compound for use according to any one of claims 13 or 15, or a pharmaceutical composition for use according to any one of claims 14 or 16, selected from the group of peripheral myelin formation diseases.

18. wherein the syndrome or disorder is multiple sclerosis (MS); clinically isolated syndrome (CIS); optic neuritis; neuromyelitis optica (Devic's disease); chronic relapsing inflammatory optic neuritis; acute disseminated encephalomyelitis; acute hemorrhagic leukoencephalitis (AHL); periventricular leukomalacia; demyelination due to viral or bacterial infection; central pontine and extrapontine myelinolysis; demyelination due to traumatic brain tissue injury; demyelination in response to hypoxia, stroke or ischemia or other cardiovascular diseases; demyelination due to exposure to carbon dioxide, cyanide or other CNS toxins; Schilder's disease; Baló concentric sclerosis; perinatal encephalopathy; amyotrophic lateral sclerosis (ALS); Alzheimer's disease (AD); multiple system atrophy; Parkinson's disease; spinocerebellar ataxia (SCA); Huntington's disease; schizophrenia; bipolar disorder; leukodystrophy; peripheral neuropathy; Dejerine-Sottas syndrome; and Charcot-Marie-Tooth disease, a compound for use according to claim 17, or a pharmaceutical composition for use.

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