Spiroquinoxaline derivatives as inhibitors of non-apoptotic regulated cell death

Abstract

Compounds that are inhibitors of non-apoptotic regulated cell death and pharmaceutical compositions containing such compounds are provided. The present invention provides the following compound (1) having a specific substituent. TIFF2022169796000176.tif41165 wherein G is phenyl optionally substituted with 1, 2, 3, 4, or 5 independently selected alkyl, alkenyl, alkynyl, aryl, heteroaryl, cycloalkyl, etc., and A is a monocyclic 4-10 membered N-heterocycloalkylene, a monocyclic 4-10 membered O / S-heterocycloalkylene, or a monocyclic 3-10 membered cycloalkylene.

Description

Technical Field

[0001] The technical field of the present invention The present invention relates to compounds that are inhibitors of non-apoptotic regulated cell death and pharmaceutical compositions containing such compounds. Further, the present invention relates to the use of such compounds and pharmaceutical compositions in therapy, particularly in the treatment of conditions, disorders or diseases characterized by non-apoptotic regulated cell death or in which non-apoptotic regulated cell death is likely or plays an essential role. The compounds and pharmaceutical compositions described herein are also related to conditions, disorders or diseases characterized by oxidative stress or in which oxidative stress is likely or plays an essential role, and / or (1) one or more elements of the necrosome; (2) death domain receptors; and / or (3) Toll-like receptors; and / or (4) activation of players in ferroptotic / ferroptosis signaling, or conditions, disorders or diseases in which activation of any of (1)-(3) and / or (4) is likely or plays an essential role, and are useful in the treatment thereof.

[0002] Background of the invention The incidence of many debilitating conditions, disorders and diseases, particularly Alzheimer's disease, Parkinson's disease, myocardial infarction, amyotrophic lateral sclerosis (ALS), organ transplantation and stroke, is continuously increasing in an aging society, and thus this is not only a major health problem but also an increasing socio-economic burden. Moreover, and particularly, treatment strategies for combating these diseases are inadequate or do not exist at all. One major underlying element of many such conditions, disorders and diseases is the role of non-apoptotic regulated cell death and the associated diversity of abnormal cellular processes that ultimately lead to cell death.

[0003] Cell death has traditionally been classified as either apoptosis or necrosis. Apoptosis is now well-known and is used as a term to describe a small set of lethal signaling pathways, the mechanisms of which have been extensively studied. In contrast, necrosis has until relatively recently been regarded as a merely accidental and unregulated process of cell death. Due to the belief that it was not regulated, little effort has been put into the study of necrosis. More recently, support has been found for, described, and a standardized nomenclature recommended for, the forms of regulated cell death mechanisms other than apoptosis (Galluzzi et al. (2012); Cell Death Diff. 19:107-20, especially Table 1 therein), which includes what are called "regulated necrosis" and "necroptosis", which are specific regulated cell death mechanisms independent of apoptosis, described by Hitomi et al. (Cell 135:1311-23 (2008)) and Degterev and co-workers (Nat. Chem. Biol. 1:112-9 (2005)). Galluzzi et al. (2012) describes other forms of regulated cell death, which includes certain new provisional names for highly specific signaling pathways leading to cell death, such as "parthanatos", "paraptosis", and several others (see references in Galluzzi et al. 2012). Another form of non-apoptotic regulated cell death includes "ferroptosis", which was recently described by Dixon and co-workers (Cell 149:1060-72 (2012)) as a non-apoptotic, iron-dependent, oxidative form of cell death. Necroptosis and ferroptosis share many features, but differences can be observed between these phenotypes, and there are expected to be additional modes of regulated cell death and lethal signaling pathways that are described and defined separately from necrosis and the like.

[0004] However, there is increasing evidence that oxidative stress, i.e., a state associated with high levels of reactive oxygen species (ROS), is a common denominator of many such non-apoptotic regulated cell death processes (and also a particular form of apoptosis known as "caspase-independent apoptosis", a regulated cell death pathway that operates in parallel with caspase-dependent apoptosis in response to multiple intracellular stress conditions), and in particular ultimately of most neurodegenerative neurological disorders (Lin, M.T. & Beal, M.F., Nature 443, 787-795 (2006)). Oxidative stress, i.e., an imbalance between the production and removal of ROS, is a potent inducer of cell death. Increased levels of ROS, impairment of ROS control systems, and proteins, lipids and DNA that have undergone oxidative modification are all prominent features in postmortem brain tissue from Alzheimer's, Parkinson's and ALS patients. ROS are also a major causative factor in neuron degeneration in stroke patients. Stroke is a prominent example of tissue damage caused by ROS following ischemia-reperfusion injury. However, tissue damage due to ischemia-reperfusion injury is not limited to the central nervous system, but is also a prominent feature in infarction (myocardial infarction being the most common form of infarction), and is also an important complication in surgery, particularly emphasized during solid organ transplantation. Oxidative stress and / or non-apoptotic regulated cell death are associated with, or are the result of, or are symptoms resulting from, many other conditions, disorders and diseases. Of particular importance are intoxications of cells, tissues, organs or organisms, such as those resulting from or caused by or associated with drug treatment (e.g., nephrotoxicity from cisplatin), drug overdose (e.g., hepatotoxicity from paracetamol), acute poisoning (e.g., from alcohol, paraquat or environmental toxins) or exposure to ionizing radiation. Other conditions, disorders and diseases lead to conditions associated with oxidative stress and / or non-apoptotic regulated cell death, including head trauma, respiratory arrest, frostbite or mechanical injury and burns.Oxidative stress and / or non-apoptotic regulated cell death may also be associated with aesthetic conditions such as UV damage / aging and hair loss in the skin.

[0005] Acidification-induced stress-dependent cell death often occurs in a controlled manner. Although there is no general consensus regarding the use of the term "necrosis" (Vandenabeele et al. (2010) Nat. Rev. Mol. Cell Biol. 11:700-14), the terms "regulated necrosis", "necroptosis", and "ferroptosis" (Dixon et al., Cell, 2012) are used herein and are known in the art to denote (respectively) general and specific forms of controlled - as opposed to accidental - necrosis (Galluzzi et al. 2012). As previously shown, necrosis has long been considered a mere accidental, unregulated form of cell death, but further evidence is accumulating that the execution of certain forms of necrotic cell death is also precisely controlled by a set of signaling pathways and catabolic mechanisms (Galluzzi and Kroemer, Cell 135 26:1161-1163 (2008); Kroemer et al., Cell Death Differ.; 16(1): 3-11, (2009)). For example, death domain receptors (e.g., TNFR1, Fas / CD95, and TRAIL-R) and Toll-like receptors (e.g., TLR3 and TLR4) have been shown to induce necrotic cell death, particularly in the presence of caspase inhibitors - which is strong evidence for non-apoptotic regulated necrosis and necroptosis. TNFR1-, Fas / CD95-, TRAILR-, and TLR3-mediated cell death appears, at first glance, to depend on the kinase RIP1, as this has been shown by their knockout / knockdown and chemical inhibition by necrostatin-1. Little is currently known about the molecular mechanisms of ferroptosis, but this form of non-apoptotic regulated cell death is characterized by the overwhelming, iron-dependent accumulation of lethal lipid ROS, and in at least some cell types, enzymes of the NOX family make an important contribution to this process, and Dixon et al. have hypothesized that in certain cancer cells in which ferroptosis occurs, the executors of death are these ROS themselves.

[0006] There is no consensus on the biochemical changes that can be used to clearly identify acidification stress-dependent or non-apoptotic regulated cell death, although several mediators, organelles, and cellular processes are already involved in such cell death (Kroemer et al., Cell Death Differ.; 16(1): 3-11, (2009)). These phenomena include mitochondrial changes (e.g., uncoupling, production of reactive oxygen species, i.e., ROS, nitrosative stress by nitric oxide or similar compounds, and often mitochondrial membrane permeability transition, i.e., MMP, controlled by cyclophilin D), lysosomal changes (ROS production by the Fenton reaction, increased lysosomal membrane permeability), nuclear changes (hyperactivation of PARP-1 and accompanying NAD+ hydrolysis), lipolysis (following activation of phospholipase, lipoxygenase, and sphingomyelinase), mitochondrial overload, and increased cytoplasmic calcium (Ca 2+ ) concentration leading to activation of non-caspase proteases (e.g., calpain and cathepsin). However, how they are interrelated to each other remains unclear.

[0007] Nevertheless, a crucial role has been shown for receptor-interacting protein (RIP) kinases, particularly serine / threonine kinases RIP1 and RIP3, in controlled necrotic cell death (Declerq et al., Cell 138:229-232 (2009)). The multi-protein complex containing RIP1 and RIP3 is known in the art as the "necrosome". RIP1 and RIP3 form the core complex within the necrosome. The necrosome complex further includes TNF receptor type 1-associated death domain protein (TRADD) and Fas-associated protein with death domain (FADD), caspase 8, serine / threonine protein phosphatase 5 (PGAM5) (Micheau et al., Cell 14:1814-190 (2003) and Wang et al. (2012), Cell 148:228-243) and mixed lineage kinase domain-like protein (MLKL) (Sun et al. (2012), Cell 148:213-227). The necrosome controls the decision between cell survival and controlled necrosis. More specifically, phosphorylation of RIP1 and RIP3 is involved in the effector mechanism of controlled necrosis. In contrast, when caspase 8 is activated, it cleaves RIP1 and RIP3, inhibiting the effector mechanism of controlled necrosis (Vandenabeele et al., Nature Reviews Mol. Cell Biol., 11:700-714 (2010)). Thus, the activation state of caspase 8 appears to be decisive for whether a cell undergoes controlled necrosis or apoptosis by initiating a caspase-activating cascade that promotes apoptosis. Whether FADD or TRADD is truly required for necrosome assembly is not currently clear.

[0008] Apart from caspase 8, negative regulators of TNFR receptor family- or Toll-like receptor-mediated regulated necrosis include the E3 ubiquitin ligases cIAP1 and cIAP2, cFLIP, and TAK1, while the deubiquitinating enzymes CYLD and A20 function as positive regulators of regulated necrosis (Vandenlakker et al, Cell Death Differ 18, 656-665, 2011). Unexpectedly, the long and short isoforms of cFLIP have been shown to have antagonistic functions, with the short isoform promoting and the long isoform inhibiting TLR ligand-induced regulated necrosis (Feoktistova et al., Mol. Cell 43, 449-463, 2011). FAB2 and FAB2 are additional elements of the signaling complexes formed by TNF receptor ligation, but their detailed functions in the control of regulated necrosis are not yet known. TRIF is an adaptor protein with a RIP1 homology interaction motif (RHIM) that couples the signaling complexes formed by ligation of Toll-like receptors TLR3 and TLR4.

[0009] In response to DNA damage-mediated depletion of cIAP1 and cIAP2, a multi-protein complex containing RIP1 and RIP3 that promotes apoptosis or regulated necrosis is formed independently of members of the TNF receptor family. This complex further contains FADD and caspase 8, the latter being the ultimate determinant regarding the choice between apoptosis and regulated necrosis (Tenev et al., Mol. Cell 43, 432-448, 2011).

[0010] RIP1 is found in several types of complexes that mediate the innate immune response against RNA and DNA viruses. In response to the ligation of the pattern recognition receptors RIG-I or MDA5, which recognize viral RNA through interaction with IPS1 (also called MAVS), a complex containing TANK, FADD, TRADD, NEMO, and RIP1 is recruited to the outer mitochondrial membrane. RIP1 shares a RIP1 homotypic interaction motif (RHIM) not only with RIP3 but also with the cytoplasmic DNA sensor DAI and TRIF (the latter is involved in signal transduction through TLR3 and TLR4) for dimerization. Although exemplified for the murine cytomegalovirus protein M45, proteins or peptides containing the RHIM sequence may interfere with the RHIM interaction between RIP1 and RIP3 and thereby inhibit regulated necrosis (consensus sequence: I / V-Q-I / L / V-G-x-x-N-x-M / L / I) (Mack et al., PNAS 105, 3094-3099, 2008; Kaiser et al., J. Immunol. 181, 6427-6434, 2008). So far, sensors of viral RNA and DNA have not been reported to have activities that promote regulated necrosis, but these RIP1-containing protein complexes may still act as molecular switches for oxidative signals that convert survival-promoting (or interferon-inducing) signals into signals that induce regulated necrosis.

[0011] Regarding ferroptosis, Dixon and colleagues (2012) have not been able to rule out the possibility of death-inducing proteins or protein complexes that are activated downstream of ROS accumulation, as observed for the non-apoptotic regulated cell death of that form.

[0012] Thus, controlled necrosis (and potentially other related forms of non-apoptotic regulated cell death such as ferroptosis) may be characterized as a type of cell death that can be avoided by inhibiting - directly or indirectly - the activity and / or interaction of elements of the necrosome or other elements that carry out ferroptotic signaling, in particular, other such elements such as RIP1, RIP3 and one or more members of the ferroptosis pathway (either through genetic or pharmacological means). This represents a convenient means for distinguishing between controlled necrosis (e.g., necroptosis) and accidental forms of necrosis (Kromer et al., Cell Death Differ.; 16(1): 3-11, (2009)).

[0013] In particular, certain spiroquinoxaline derivatives and pharmaceutical compositions thereof for use in the treatment of viral infections are generally disclosed in European Patent Application Publication Nos. 0 509 398 A1 and 0 657 166 A1.

[0014] Among a very large number of other general structures, certain spiroquinoxaline derivatives are generally disclosed as Formula 2.2 in International Publication No. 2007 / 117180 A1, and a few specific spiroquinoxaline compounds are disclosed in its comprehensive Table 12. International Publication No. 2007 / 117180 A1 is mainly concerned with the construction and composition of a large combinatorial library of small molecules that may potentially be bioactive substances and their pharmaceutical compositions. Of the vast number of specific compounds disclosed therein, only a few compounds (not spiroquinoxalines) have been tested and suggested to have anti-cancer properties (Examples 40 and Table 14 thereof).

[0015] Frankowski and co-workers (PNAS 108:6727-32 (2012)) described the synthesis of a small library of Stemona alkaloid analogs (reported to have antitussive activity) condensed with quinoxaline derivatives by spiro carbon (Scheme 4 therein), and the activity of such alkaloid-quinoxaline spiro condensates in various receptor binding assays.

[0016] Various organic chemical methods for the synthesis of quinoxaline derivatives and their spiro forms have been disclosed. These include Kysil et al (Eur. J. Org. Chem. 8:1525-43 (2010)), Lee (Korean Patent Publication No. 2012-105714), Adarvana (Tetrahedron Lett. 52:6108-12 (2011)) and Kolla and Lee (Tetrahedron 66:8938-44 (2010)).

[0017] Other specific spiroquinoxaline compounds are known and commercially available, but their synthesis and utility have not been shown. These include those with CAS Registry Numbers: 1172351-24-4, 1223830-23-6 and 1223982-82-8.

[0018] Accordingly, an object of the present invention is to provide alternative, improved and / or integrated means or methods for addressing one or more problems such as those described above in the treatment (including prophylactic treatment) of one or more conditions, disorders or diseases (or related conditions or symptoms), and / or agents and pharmaceutical compositions useful for such treatment. Such an object underlying the present invention is solved by the subject matter disclosed or defined anywhere in this specification, for example, the subject matter of the appended claims.

[0019] Summary of the Invention In a first aspect, the present invention relates to a state, disorder or disease: (i) characterized by non-apoptotic regulated cell death, or in which non-apoptotic regulated cell death is likely or plays an essential role; (ii) characterized by oxidative stress, or in which oxidative stress is likely or plays an essential role; (iii) characterized by activation of one or more elements of the necrosome, a death domain receptor, and / or a Toll-like receptor, and / or a player in ferroptosis / ferroptotic signaling, or in which activation of any of (1)-(3) and / or (4) is likely or plays an essential role; (iv) a neurodegenerative disease of the central or peripheral nervous system, muscle wasting, muscular dystrophy, ischemia, muscle compartment syndrome, gangrene, bedsore, sepsis, degenerative arthritis, retinal necrosis, heart disease, liver, gastrointestinal or pancreatic disease, ischemic necrosis, diabetes, sickle cell disease, vascular changes, cell death induced by cancer chemotherapy / radiotherapy, and poisoning, or a state, disorder or disease that is a result of, caused by, or associated with any of the foregoing; and / or (v) a form of infection by a virus, bacterium, fungus or other microorganism; a change in cell proliferation, cell differentiation or a decrease in intracellular signaling; unwanted inflammation; cell death of retinal neurons, cardiomyocytes or cells of the immune system or cell death associated with renal failure; neonatal respiratory distress, apnea, incarcerated hernia, placental infarction, iron-load complications, endometriosis, congenital diseases; head trauma / traumatic brain injury, liver injury; injury from environmental radiation; burns; frostbite; mechanical injury and decompression sickness, for use in a method of treating a state, disorder or disease that is a result of, caused by, or associated with any of the foregoing, of the following general formula (I): [Chemical Formula] [wherein, R 1 ~R 5 , ring A, E, L and G are as defined in claim 1] To provide a spiroquinoxaline derivative having the same, and a compound selected from the group consisting of a solvate, salt, complex, polymorph, crystal form, racemic mixture, diastereomer, enantiomer, tautomer, isotope-labeled form, prodrug and combinations thereof.

[0020] In a second aspect, the present application is a method for treating an individual (particularly a human patient) in need of treatment, comprising administering a pharmaceutically effective amount (particularly a therapeutically effective amount) of the following general formula (I): [Chemical formula] [wherein, R 1 ~R 5 , ring A, E, L and G are as defined in claim 2, provided that when ring A is a monocyclic 4- to 10-membered N-heterocycloalkylene, the individual is in a state, disorder or disease of cancer, and / or suffering from, resulting from, or associated with cancer] To provide a method comprising administering a spiroquinoxaline derivative having the same, and a compound selected from the group consisting of a solvate, salt, complex, polymorph, crystal form, racemic mixture, diastereomer, enantiomer, tautomer, isotope-labeled form, prodrug and combinations thereof.

[0021] In a third aspect, the present application is the following general formula (I): [Chemical formula] [wherein, R 1 ~R 5 , ring A, E, L and G are as defined in claim 3] To provide a spiroquinoxaline derivative having the same, and a compound selected from the group consisting of a solvate, a salt, a complex, a polymorph, a crystal form, a racemic mixture, a diastereomer, an enantiomer, a tautomer, an isotope-labeled form, a prodrug, and combinations thereof.

[0022] In a fourth aspect, the present application is for use as a medicament of the following general formula (I): [Chemical formula] [wherein, R 1 ~R 5 , ring A, E, L and G are as specified in claim 4] To provide a spiroquinoxaline derivative having the same, and a compound selected from the group consisting of a solvate, a salt, a complex, a polymorph, a crystal form, a racemic mixture, a diastereomer, an enantiomer, a tautomer, an isotope-labeled form, a prodrug, and combinations thereof.

[0023] In a fifth aspect, the present invention provides a pharmaceutical composition comprising the compound specified in the first or second aspect and a pharmaceutically acceptable excipient. A further aspect of the present invention is disclosed herein.

Brief Description of the Drawings

[0024]

Figure 1

Figure 2

Figure 3

Figure 4

[0025] Detailed Description of the Invention Hereinafter, the present invention will be described in more detail, but it is to be understood that the invention is not limited to the specific methodologies, protocols and reagents described herein, and these may vary. Also, the terms used herein are for the purpose of describing only specific embodiments and are not intended to limit the scope of the present invention, and the scope of the present invention is to be understood as being limited only by the appended claims and other disclosures herein. All technical and scientific terms used herein have the meaning commonly understood by one of ordinary skill in the art, unless otherwise defined.

[0026] Hereinafter, the elements of the present invention will be described in more detail. These elements are listed with respect to specific embodiments, but it should be understood that they may be combined in any manner and in any number to create further embodiments. The various examples and preferred embodiments described should not be construed as limiting the present invention to the specifically recited embodiments. This description is to be understood as supporting and encompassing embodiments that combine the recited embodiments with any number of disclosed and / or preferred elements. Further, any permutations and combinations of all the recited elements in this application should be considered as disclosed by the description of this application, unless the context indicates otherwise. For example, in one embodiment, the R of the compound of the present invention 8is halogen (e.g., Cl), and in another embodiment of the compound of the present invention, if ring A is 4-piperidinylene, then in a preferred embodiment, R of the compound of the present invention 8 is halogen (e.g., Cl) and ring A is 4-piperidinylene.

[0027] Preferably, the terms used herein are defined as described in "A multilingual glossary of biotechnological terms: (IUPAC Recommendations), H.G.W. Leuenberger, B. Nagel, and H. Kolbl, Eds., Helvetica Chimica Acta, CH-4010 Basel, Switzerland, (1995)".

[0028] The practice of the present invention will, unless otherwise specified, use conventional methods of chemistry, biochemistry, and recombinant DNA techniques as described in the literature of the art (e.g., see Molecular Cloning: A Laboratory Manual, 2 nd Edition, J. Sambrook et al. eds., Cold Spring Harbor Laboratory Press, Cold Spring Harbor 1989).

[0029] Throughout this specification and the following claims, unless the context requires otherwise, the words "comprise", "comprises" and "comprising" and variations such as these are to be understood to mean including the stated member, integer or step, or group of members, integers or steps but not excluding any other member, integer or step, or group of members, integers or steps. Terms such as "a", "an" and "the" and similar references used in the context of describing the invention (in particular, the context of the claims) are to be construed to include both the singular and the plural unless the specification specifically states otherwise or the context clearly dictates otherwise. The recitation of numerical ranges herein is merely intended as a shorthand way of referring individually to each separate numerical value falling within the range. Unless otherwise specified herein, each separate numerical value is incorporated into the specification as if it were individually recited herein. Unless otherwise specified herein or the context clearly dictates otherwise, any of the methods described herein can be performed in any suitable order. Any and all examples, or exemplary language (e.g., "such as") provided herein are merely intended to better illustrate the invention and do not pose a limitation to the scope of the invention otherwise claimed. None of the language in this specification should be construed as indicating any non-claimed component as essential to the practice of the invention.

[0030] Throughout the text of this specification, several documents are cited. In each case, whether before or after, the documents cited herein (including all patents, patent applications, scientific publications, manufacturer's specifications, instructions, etc.) are hereby incorporated by reference in their entirety. Nothing in this specification should be construed as an admission that the invention is not entitled to antedate such disclosure by virtue of prior invention.

[0031] The term "alkyl" refers to a monovalent group of a saturated straight-chain or branched-chain hydrocarbon. Preferably, the alkyl group contains 1 to 12 (for example, 1 to 10) carbon atoms, that is, 1, 2, 3, 4, 5, 6, 7, 8, 9, 10, 11, or 12 carbon atoms (for example, 1, 2, 3, 4, 5, 6, 7, 8, 9, or 10 carbon atoms), more preferably 1 to 8 carbon atoms, for example, 1 to 6 or 1 to 4 carbon atoms. Exemplary alkyl groups include methyl, ethyl, propyl, iso-propyl, butyl, iso-butyl, tert-butyl, n-pentyl, iso-pentyl, sec-pentyl, neo-pentyl, 1,2-dimethyl-propyl, iso-amyl, n-hexyl, iso-hexyl, sec-hexyl, n-heptyl, iso-heptyl, n-octyl, 2-ethyl-hexyl, n-nonyl, n-decyl, n-undecyl, n-dodecyl, and the like.

[0032] The term "alkylene" refers to a divalent group of a saturated straight-chain or branched-chain hydrocarbon. Preferably, the alkylene contains 1 to 10 carbon atoms, that is, 1, 2, 3, 4, 5, 6, 7, 8, 9, or 10 carbon atoms, more preferably 1 to 8 carbon atoms, for example, 1 to 6 or 1 to 4 carbon atoms. Exemplary alkylene groups include methylene, ethylene (that is, 1,1-ethylene, 1,2-ethylene), propylene (that is, 1,1-propylene, 1,2-propylene (-CH(CH 3 )CH 2 -), 2,2-propylene (-C(CH 3 ) 2-), and 1,3-propylene), butylene isomers (e.g., 1,1-butylene, 1,2-butylene, 2,2-butylene, 1,3-butylene, 2,3-butylene (cis or trans, or a mixture thereof), 1,4-butylene, 1,1-iso-butylene, 1,2-iso-butylene, and 1,3-iso-butylene), pentylene isomers (e.g., 1,1-pentylene, 1,2-pentylene, 1,3-pentylene, 1,4-pentylene, 1,5-pentylene, 1,1-iso-pentylene, 1,1-sec-pentyl, 1,1-neo-pentyl), hexylene isomers (e.g., 1,1-hexylene, 1,2-hexylene, 1,3-hexylene, 1,4-hexylene, 1,5-hexylene, 1,6-hexylene, and 1,1-iso-hexylene), etc. are included.

[0033] The term "alkenyl" refers to a monovalent group of an unsaturated straight-chain or branched-chain hydrocarbon having at least one carbon-carbon double bond. Generally, the maximum number of carbon-carbon double bonds in an alkenyl group is equal to the integer calculated by dividing the number of carbon atoms in the alkenyl group by 2, and if the number of carbon atoms in the alkenyl group is odd, then rounding the result of that division down to the next lower integer. For example, for an alkenyl group having 9 carbon atoms, the maximum number of carbon-carbon double bonds is 4. Preferably, the alkenyl group has 1 to 4, i.e., 1, 2, 3, or 4 carbon-carbon double bonds. Preferably, the alkenyl group contains 2 to 10 carbon atoms, i.e., 2, 3, 4, 5, 6, 7, 8, 9, or 10 carbon atoms, more preferably, 2 to 8 carbon atoms, for example, 2 to 6 carbon atoms or 2 to 4 carbon atoms. Thus, in a preferred embodiment, the alkenyl group contains 2 to 10 carbon atoms and 1, 2, 3, 4, or 5 carbon-carbon double bonds, more preferably, 2 to 8 carbon atoms and 1, 2, 3, or 4 carbon-carbon double bonds, for example, 2 to 6 carbon atoms and 1, 2, or 3 carbon-carbon double bonds, or 2 to 4 carbon atoms and 1 or 2 carbon-carbon double bonds. The carbon-carbon double bond may be in the cis (Z) conformation or the trans (E) conformation. Exemplary alkenyl groups include vinyl, 1-propenyl, 2-propenyl (i.e., allyl), 1-butenyl, 2-butenyl, 3-butenyl, 1-pentenyl, 2-pentenyl, 3-pentenyl, 4-pentenyl, 1-hexenyl, 2-hexenyl, 3-hexenyl, 4-hexenyl, 5-hexenyl, 1-heptenyl, 2-heptenyl, 3-heptenyl, 4-heptenyl, 5-heptenyl, 6-heptenyl, 1-octenyl, 2-octenyl, 3-octenyl, 4-octenyl, 5-octenyl, 6-octenyl, 7-octenyl, 1-nonenyl, 2-nonenyl, 3-nonenyl, 4-nonenyl, 5-nonenyl, 6-nonenyl, 7-nonenyl, 8-nonenyl, 1-decenyl, 2-decenyl, 3-decenyl, 4-decenyl, 5-decenyl, 6-decenyl, 7-decenyl, 8-decenyl, 9-decenyl, etc. When the alkenyl group is bonded to a nitrogen atom, the double bond cannot be in the alpha position with respect to the nitrogen atom.

[0034] The term "alkenylene" refers to a divalent group of an unsaturated straight-chain or branched-chain hydrocarbon having at least one carbon-carbon double bond. Generally, the maximum number of carbon-carbon double bonds in an alkenylene group is equal to the integer calculated by dividing the number of carbon atoms in the alkenylene group by 2, and if the number of carbon atoms in the alkenylene group is odd, then rounding the result of that division down to the next lower integer. For example, for an alkenylene group having 9 carbon atoms, the maximum number of carbon-carbon double bonds is 4. Preferably, the alkenylene group has 1 to 4, i.e., 1, 2, 3, or 4 carbon-carbon double bonds. Preferably, the alkenylene group contains 2 to 10 carbon atoms, i.e., 2, 3, 4, 5, 6, 7, 8, 9, or 10 carbon atoms, more preferably 2 to 8 carbon atoms, for example, 2 to 6 carbon atoms or 2 to 4 carbon atoms. Thus, in a preferred embodiment, the alkenylene group contains 2 to 10 carbon atoms and 1, 2, 3, 4, or 5 carbon-carbon double bonds, more preferably 2 to 8 carbon atoms and 1, 2, 3, or 4 carbon-carbon double bonds, for example, 2 to 6 carbon atoms and 1, 2, or 3 carbon-carbon double bonds, or 2 to 4 carbon atoms and 1 or 2 carbon-carbon double bonds. The carbon-carbon double bond may be in the cis (Z) conformation or the trans (E) conformation. Exemplary alkenylene groups include ethene-1,2-diyl, vinylidene, 1-propene-1,2-diyl, 1-propene-1,3-diyl, 1-propene-2,3-diyl, allylidene, 1-butene-1,2-diyl, 1-butene-1,3-diyl, 1-butene-1,4-diyl, 1-butene-2,3-diyl, 1-butene-2,4-diyl, 1-butene-3,4-diyl, 2-butene-1,2-diyl, 2-butene-1,3-diyl, 2-butene-1,4-diyl, 2-butene-2,3-diyl, 2-butene-2,4-diyl, 2-butene-3,4-diyl, etc. When the alkenylene group is bonded to a nitrogen atom, the double bond cannot be in the alpha position with respect to the nitrogen atom.

[0035] The term "alkynyl" refers to a monovalent group of an unsaturated straight-chain or branched-chain hydrocarbon having at least one carbon-carbon triple bond. Generally, the maximum number of carbon-carbon triple bonds in an alkynyl group can be equal to the integer calculated by dividing the number of carbon atoms in the alkynyl group by 2, and then rounding down the result of that division to the next lower integer if the number of carbon atoms in the alkynyl group is odd. For example, for an alkynyl group having 9 carbon atoms, the maximum number of carbon-carbon triple bonds is 4. Preferably, the alkynyl group has 1 to 4, i.e., 1, 2, 3, or 4, more preferably 1 or 2 carbon-carbon triple bonds. Preferably, the alkynyl group contains 2 to 10, i.e., 2, 3, 4, 5, 6, 7, 8, 9, or 10 carbon atoms, more preferably 2 to 8 carbon atoms, for example, 2 to 6 carbon atoms or 2 to 4 carbon atoms. Thus, in a preferred embodiment, the alkynyl group contains 2 to 10 carbon atoms and 1, 2, 3, 4, or 5 (preferably 1, 2, or 3) carbon-carbon triple bonds, more preferably 2 to 8 carbon atoms and 1, 2, 3, or 4 (preferably 1 or 2) carbon-carbon triple bonds, for example, 2 to 6 carbon atoms and 1, 2, or 3 carbon-carbon triple bonds, or 2 to 4 carbon atoms and 1 or 2 carbon-carbon triple bonds. Exemplary alkynyl groups include ethynyl, 1-propynyl, 2-propynyl, 1-butynyl, 2-butynyl, 3-butynyl, 1-pentynyl, 2-pentynyl, 3-pentynyl, 4-pentynyl, 1-hexynyl, 2-hexynyl, 3-hexynyl, 4-hexynyl, 5-hexynyl, 1-heptynyl, 2-heptynyl, 3-heptynyl, 4-heptynyl, 5-heptynyl, 6-heptynyl, 1-octynyl, 2-octynyl, 3-octynyl, 4-octynyl, 5-octynyl, 6-octynyl, 7-octynyl, 1-nonynyl, 2-nonynyl, 3-nonynyl, 4-nonynyl, 5-nonynyl, 6-nonynyl, 7-nonynyl, 8-nonynyl, 1-decynyl, 2-decynyl, 3-decynyl, 4-decynyl, 5-decynyl, 6-decynyl, 7-decynyl, 8-decynyl, 9-decynyl, etc. When an alkynyl group is bonded to a nitrogen atom, the triple bond cannot be in the alpha position with respect to the nitrogen atom.

[0036] The term "alkynylene" refers to a divalent group of an unsaturated straight-chain or branched-chain hydrocarbon having at least one carbon-carbon triple bond. Generally, the maximum number of carbon-carbon triple bonds in an alkynylene group is equal to the integer calculated by dividing the number of carbon atoms in the alkynylene group by 2, and if the number of carbon atoms in the alkynylene group is odd, then rounding the result of that division down to the next lower integer. For example, for an alkynylene group having 9 carbon atoms, the maximum number of carbon-carbon triple bonds is 4. Preferably, the alkynylene group has 1 to 4, i.e., 1, 2, 3, or 4, more preferably 1 or 2 carbon-carbon triple bonds. Preferably, the alkynylene group contains 2 to 10, i.e., 2, 3, 4, 5, 6, 7, 8, 9, or 10 carbon atoms, more preferably 2 to 8 carbon atoms, for example, 2 to 6 carbon atoms or 2 to 4 carbon atoms. Thus, in a preferred embodiment, the alkynylene group contains 2 to 10 carbon atoms and 1, 2, 3, 4, or 5 (preferably 1, 2, or 3) carbon-carbon triple bonds, more preferably 2 to 8 carbon atoms and 1, 2, 3, or 4 (preferably 1 or 2) carbon-carbon triple bonds, for example, 2 to 6 carbon atoms and 1, 2, or 3 carbon-carbon triple bonds, or 2 to 4 carbon atoms and 1 or 2 carbon-carbon triple bonds. Exemplary alkynylene groups include ethine-1,2-diyl, 1-propyn-1,3-diyl, 1-propyn-3,3-diyl, 1-butyn-1,3-diyl, 1-butyn-1,4-diyl, 1-butyn-3,4-diyl, 2-butyn-1,4-diyl, and the like. When the alkynylene group is bonded to a nitrogen atom, the triple bond cannot be in the alpha position with respect to the nitrogen atom.

[0037] The term "aryl" or "aromatic ring" refers to a monovalent group of an aromatic cyclic hydrocarbon. Preferably, the aryl group contains carbon atoms that can be arranged in one ring (e.g., phenyl) or two or more fused rings (e.g., naphthyl), with 3 to 14 (e.g., 5 to 10 (such as 5, 6, or 10)) carbon atoms. Exemplary aryl groups include cyclopropenyl, cyclopentadienyl, phenyl, indenyl, naphthyl, azulenyl, fluorenyl, anthryl, and phenanthryl. Preferably, "aryl" refers to a monocyclic ring containing 6 carbon atoms or an aromatic bicyclic ring system containing 10 carbon atoms. Preferred examples are phenyl and naphthyl.

[0038] The term "heteroaryl" or "heteroaromatic ring" means an aryl group as defined above, in which one or more carbon atoms in the aryl group are substituted with a heteroatom O, S or N. Preferably, heteroaryl refers to a 5- or 6-membered aromatic monocyclic ring in which one, two or three carbon atoms are substituted with the same or different heteroatoms O, N or S. Alternatively, it means an aromatic bicyclic or tricyclic ring system in which one, two, three, four or five carbon atoms are substituted with the same or different heteroatoms O, N or S. Preferably, in each ring of the heteroaryl group, the maximum number of O atoms is 1, the maximum number of S atoms is 1, and the maximum total number of O and S atoms is 2. Exemplary heteroaryl groups include furanyl, thienyl, oxazolyl, isoxazolyl, oxadiazolyl (1,2,5- and 1,2,3-), pyrrolyl, imidazolyl, pyrazolyl, triazolyl (1,2,3- and 1,2,4-), tetrazolyl, thiazolyl, isothiazolyl, thiadiazolyl (1,2,3- and 1,2,5-), pyridyl, pyrimidinyl, pyrazinyl, triazinyl (1,2,3-, 1,2,4-, and 1,3,5-), benzofuranyl (1- and 2-), indolyl, isoindolyl, benzothienyl (1- and 2-), 1H-indazolyl, benzimidazolyl, benzoxazolyl, indoxazinyl, benzoisoxazolyl, benzothiazolyl, benzoisothiazolyl, benzotriazolyl, quinolinyl, isoquinolinyl, benzodiazinyl, quinoxalinyl, quinazolinyl, benzotriazinyl (1,2,3- and 1,2,4-benzotriazinyl), pyridazinyl, phenoxazinyl, thiazolopyridinyl, pyrrolothiazolyl, phenothiazinyl, isobenzofuranyl, chromenyl, xanthenyl, phenoxathiinyl, pyrrolidinyl, indolizinyl, indazolyl, purinyl, quinolidinyl, phthalazinyl, naphthyridinyl (1,5-, 1,6-, 1,7-, 1,8- and 2,6-), cinnolinyl, pteridinyl, carbazolyl, phenanthridinyl, acridinyl, perimidinyl, phenanthrolinyl (1,7-, 1,8-, 1,10-, 3,8- and 4,7-), phenazinyl, oxazolopyridinyl, isoxazolopyridinyl, pyrroloxazolyl and pyrrolopyrrolyl.Exemplary 5- or 6-membered heteroaryl groups include furanyl, thienyl, oxazolyl, isoxazolyl, oxadiazolyl (1,2,5- and 1,2,3-), pyrrolyl, imidazolyl, pyrazolyl, triazolyl (1,2,3- and 1,2,4-), thiazolyl, isothiazolyl, thiadiazolyl (1,2,3- and 1,2,5-), pyridyl, pyrimidinyl, pyrazinyl, triazinyl (1,2,3-, 1,2,4- and 1,3,5-) and pyridazinyl.

[0039] The term "cycloalkyl" or "alicyclic" preferably represents a cyclic non-aromatic version of "alkyl" and "alkenyl" having 3 to 14 carbon atoms (e.g., 3 to 10 carbon atoms, i.e., 3, 4, 5, 6, 7, 8, 9 or 10 carbon atoms), more preferably 3 to 7 carbon atoms. Exemplary cycloalkyl groups include cyclopropyl, cyclopropenyl, cyclobutyl, cyclobutenyl, cyclopentyl, cyclopentenyl, cyclohexyl, cyclohexenyl, cycloheptyl, cycloheptenyl, cyclooctyl, cyclooctenyl, cyclononyl, cyclononenyl, cyclodecyl, cyclodecenyl and adamantyl. The term "cycloalkyl" is also intended to include their bicyclic and tricyclic versions. When a bicyclic ring is formed, it is preferred that each ring is linked to each other at two adjacent carbon atoms, but alternatively, the two rings are linked via the same carbon atom, i.e., they form a spiro ring system or they form a "bridged" ring system. Preferred examples of cycloalkyl include C 3 -C 8 -cycloalkyl, especially cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, cycloheptyl, cyclooctyl, spiro[3,3]heptyl, spiro[3,4]octyl, spiro[4,3]octyl, bicyclo[4.1.0]heptyl, bicyclo[3.2.0]heptyl, bicyclo[2.2.1]heptyl, bicyclo[2.2.2]octyl, bicyclo[5.1.0]octyl and bicyclo[4.2.0]octyl.

[0040] The term "cyclopropylene" means a cyclopropyl group as defined above in which one hydrogen atom has been removed to form a divalent group. Cyclopropylene may be bonded to two atoms or moieties through the same carbon atom (1,1-cyclopropylene, i.e., a geminal divalent group), or through two carbon atoms (1,2-cyclopropylene).

[0041] The term "heterocyclyl" or "heterocyclic" means a cycloalkyl group as defined above, wherein 1, 2, 3 or 4 carbon atoms in the cycloalkyl group are replaced by a heteroatom O, S or N. Preferably, in each ring of the heterocyclyl group, the maximum number of O atoms is 1, the maximum number of S atoms is 1, and the maximum total number of O and S atoms is 2. The term "heterocyclyl" is also intended to include partially or fully hydrogenated forms of the above heteroaryl groups (e.g., dihydro, tetrahydro or perhydro forms). Exemplary heterocyclyl groups include morpholino, isochromanyl, chromanyl, pyrrolidinyl, imidazolidinyl, pyrazolidinyl, piperidinyl, piperazinyl, indolinyl, isoindolinyl, di- and tetrahydrofuranyl, di- and tetrahydrothienyl, di- and tetrahydrooxazolyl, di- and tetrahydroisoxazolyl, di- and tetrahydrooxadiazolyl (1,2,5- and 1,2,3-), dihydropyrrolyl, dihydroimidazolyl, dihydropyrazolyl, di- and tetrahydrotriazolyl (1,2,3- and 1,2,4-), di- and tetrahydrothiazolyl, di- and tetrahydrothiadiazolyl (1,2,3- and 1,2,5-), di- and tetrahydropyridyl, di- and tetrahydropyrimidinyl, di- and tetrahydropyrazinyl, di- and tetrahydrotriazinyl (1,2,3-, 1,2,4-, and 1,3,5-), di- and tetrahydrobenzofuranyl (1- and 2-), di- and tetrahydroindolyl, di- and tetrahydroisoindolyl, di- and tetrahydrobenzothienyl (1- and 2), di- and tetrahydro-1H-indazolyl, di- and tetrahydrobenzimidazolyl, di- and tetrahydrobenzoxazolyl, di- and tetrahydroindoxazinyl, di- and tetrahydrobenzisoxazolyl, di- and tetrahydrobenzothiazolyl, di- and tetrahydrobenzisothiazolyl, di- and tetrahydrobenzotriazolyl, di- and tetrahydroquinolinyl, di- and tetrahydroisoquinolinyl, di- and tetrahydrobenzodiazinyl, di- and tetrahydroquinoxalinyl, di- and tetrahydroquinazolinyl, di- and tetrahydrobenzotriazinyl (1,2,3 and 1,2,4-) Di- and tetrahydropyridazinyl, di- and tetrahydrophenoxazinyl, di- and tetrahydrothiazolopyridinyl (e.g., 4,5,6-7-tetrahydro[1,3]thiazolo[5,4-c]pyridinyl or 4,5,6-7-tetrahydro[1,3]thiazolo[4,5-c]pyridinyl, e.g., 4,5,6-7-tetrahydro[1,3]thiazolo[5,4-c]pyridin-2-yl or 4,5,6-7-tetrahydro[1,3]thiazolo[4,5-c]pyridin-2-yl), di- and tetrahydropyrrolothiazolyl (e.g., 5,6-dihydro-4H-pyrrolo[3,4-d][1,3]thiazolyl), di- and tetrahydrophenothiazinyl, di- and tetrahydroisobenzofuranyl, di- and tetrahydrochromenyl, di- and tetrahydroxanthenyl, di- and tetrahydrophenoxathiinyl, di- and tetrahydropyrrolidinyl, di- and tetrahydroindolizinyl, di- and tetrahydroindazolyl, di- and tetrahydropurinyl, di- and tetrahydroquinolizinyl, di- and tetrahydrophthalazinyl, di- and tetrahydronaphthyridinyl (1,5-, 1,6-, 1,7-, 1,8- and 2,6-), di- and tetrahydrocinnolinyl, di- and tetrahydropteridinyl, di- and tetrahydrocarbazolyl, di- and tetrahydrophenanthridinyl, di- and tetrahydroacridinyl, di- and tetrahydropyrimidinyl, di- and tetrahydrophenanthrolinyl (1,7-, 1,8-, 1,10-, 3,8-, and 4,7-), di- and tetrahydrophenazinyl, di- and tetrahydrooxazolopyridinyl, di- and tetrahydroisoxazolopyridinyl, di- and tetrahydropyrrolioxazolyl and di- and tetrahydropyrrolopyrrolyl are included. Exemplary 5- or 6-membered heterocyclyl groups include morpholino, pyrrolidinyl, imidazolidinyl, pyrazolidinyl, piperidinyl, piperazinyl, di- and tetrahydrofuranyl, di- and tetrahydrothienyl, di- and tetrahydrooxazolyl, di- and tetrahydroisoxazolyl, di- and tetrahydrooxadiazolyl (1,2,5- and 1,2,3-), dihydropyrrolyl, dihydroimidazolyl, dihydropyrazolyl, di- and tetrahydrotriazolyl (1,2,3- and 1,2,4-) containing di- and tetrahydrothiazolyl, di- and tetrahydroisothiazolyl, di- and tetrahydrothiadiazolyl (1,2,3- and 1,2,5-), di- and tetrahydropyridyl, di- and tetrahydropyrimidinyl, di- and tetrahydropyrazinyl, di- and tetrahydrotriazinyl (1,2,3-, 1,2,4-, and 1,3,5-), and di- and tetrahydropyridazinyl.,

[0042] As used herein, the term "N-heterocycloalkylene" means a heterocyclyl group synonymous with the above, containing at least one ring nitrogen atom and having one hydrogen atom removed from the same carbon atom to form a geminal divalent group. N-heterocycloalkylene may contain, in addition to the at least one ring nitrogen atom, one, two or three further ring heteroatoms selected from the group consisting of O, S or N. Preferably, in each ring of the N-heterocycloalkylene group, the maximum number of O atoms is 1, the maximum number of S atoms is 1, and the maximum total number of O and S atoms is 2. Preferably, N-heterocycloalkylene is monocyclic, contains one, two or three ring nitrogen atoms, and optionally does not contain an O or S ring atom. The term "N-heterocycloalkylene" also includes a partially or fully hydrogenated form (e.g., dihydro, tetrahydro or perhydro form) (preferably, a partially or fully hydrogenated form of the above monocyclic heteroaryl group) of the above heteroaryl group containing at least one ring nitrogen atom and having one hydrogen atom removed from the same carbon atom to form a geminal divalent group. Thus, according to the present invention, N-heterocycloalkylene may be saturated or unsaturated (i.e., may contain one or more double bonds in the ring), but cannot be aromatic.Exemplary N-heterocycloalkylene groups include azetidinylene (N is at the 2- or 3-position relative to the divalent carbon atom), pyrrolidinylene (N is at the 2- or 3-position), pyrazolidinylene (N is at the 2- and 3- or 3- and 4-positions), imidazolidinylene (N is at the 2- and 4- or 2- and 5-positions), triazolidinylene (N is at the 2, 3- and 4- or 2, 3- and 5-positions), piperidinylene (N is at the 2-, 3- or 4-position), piperazinylene (N is at the 2- and 5-positions), di-, tetra- and hexahydropyridazinylene (N is at the 2- and 3- or 3- and 4-positions), di-, tetra- and hexahydropyrimidinylene (N is at the 2- and 4- or 3- and 5-positions), di- and tetrahydrotriazinylene, azepanylene (N is at the 2-, 3- or 4-position), diazepanylene (N is at the 2- and 3-; 2- and 4-; 2- and 5-; 2- and 6-; 2- and 7-; 3- and 4-; 3- and 5-; 3- and 6- or 4- and 5-positions), triazepanylene (N is at the 2, 3- and 4-; 2, 3- and 5-; 2, 3- and 6-; 2, 3- and 7-; 2, 4- and 5-; 2, 4- and 6-; 2, 4- and 7-; 2, 5- and 6-; 2, 5- and 7-; 3, 4- and 5- or 3, 4- and 6-positions), azocanylene (N is at the 2-, 3-, 4- or 5-position), diazocanylene (N is at the 2- and 3-; 2- and 4-; 2- and 5-; 2- and 6-; 2- and 7-; 2- and 8-; 3- and 4-; 3- and 5-; 3- and 6-; 3- and 7-; 4- and 5- or 4- and 6-positions), triazocanylene (N is at the 2, 3- and 4-; 2, 3- and 5-; 2, 3- and 6-; 2, 3- and 7-; 2, 3- and 8-; 2, 4- and 5-; 2, 4- and 6-; 2, 4- and 7-; 2, 4- and 8-; 2, 5- and 6-; 2, 5- and 7-; 2, 5- and 8-; 2, 6- and 7-; 3, 4- and 5-; 3, 4- and 6-; 3, 4- and 7-; 3, 5- and 6-; 3, 5- and 7- or 4, 5- and 6-positions) and morpholinylene are included.

[0043] As used herein, the term "monocyclic 4- to 10-membered N-heterocycloalkylene" means that 4 to 10 members of the N-heterocycloalkylene are linked in such a manner as to form a single ring (e.g., piperidinylene). Thus, except for the spiro carbon atom of ring A (which belongs to both ring A and the quinoxaline moiety), the remaining 3 to 9 ring atoms of ring A belong only to ring A, i.e., those ring atoms of ring A do not belong to any further rings. Accordingly, according to the present invention, the term "monocyclic 4- to 10-membered N-heterocycloalkylene" does not encompass polycyclic (e.g., bicyclic or tricyclic) structures (e.g., indolinylene) in which at least two ring atoms belong to more than one ring.

[0044] As used herein, the term "O / S - heterocycloalkylene" refers to a heterocyclyl group as defined above, containing at least one ring heteroatom selected from oxygen and sulfur, and having one hydrogen atom removed from the same carbon atom to form a geminal divalent group. Preferably, each ring atom of the O / S - heterocycloalkylene is selected from the group consisting of carbon, oxygen, and sulfur (i.e., preferably, the O / S - heterocycloalkylene does not contain heteroatoms other than oxygen or sulfur). Preferably, in each ring of the O / S - heterocycloalkylene group, the maximum number of O atoms is 2 or 1, the maximum number of S atoms is 2 or 1, and the maximum total number of O and S atoms is 2. Preferably, the O / S - heterocycloalkylene is monocyclic, contains one or two ring heteroatoms selected from oxygen and sulfur, and optionally does not contain ring heteroatoms other than oxygen or sulfur. The term "O / S - heterocycloalkylene" also includes a partially or fully hydrogenated form (e.g., dihydro, tetrahydro, or perhydro form) of the above - mentioned heteroaryl group containing at least one ring heteroatom selected from oxygen and sulfur and having one hydrogen atom removed from the same carbon atom to form a geminal divalent group (preferably, a partially or fully hydrogenated form of the above - mentioned monocyclic heteroaryl group). Thus, according to the present invention, the O / S - heterocycloalkylene may be saturated or unsaturated (i.e., it may contain one or more double bonds in the ring), but it cannot be aromatic.Exemplary O / S-heterocycloalkylene groups include oxetanylene (O at the 2- or 3-position), thietanylene (S at the 2- or 3-position), di- and tetrahydrofuranylene (O at the 2- or 3-position), di- and tetrahydrothienylene (S at the 2- or 3-position), di- and tetrahydropyranylene (O at the 2-, 3- or 4-position), di- and tetrahydrothiopyranylene (S at the 2-, 3- or 4-position), oxepanylene (O at the 2-, 3- or 4-position), thiepanylene (S at the 2-, 3- or 4-position), oxocanylene (O at the 2-, 3-, 4- or 5-position), thiocanylene (S at the 2-, 3-, 4- or 5-position), dioxolanylene (O at the 2- and 4- or 2- and 5-position), dithiolanylene (S at the 2- and 3-; 2- and 4-; 2- and 5- or 3- and 4-position), oxathiolanylene (O at the 2-position and S at the 3- or 4-position; O at the 4-position and S at the 2-position; or O at the 2-position and S at the 5-position), dioxanylene (O at the 2- and 4-; 2- and 5-; 2- and 6- or 3- and 5-position), dithianylene (S at the 2- and 3-; 2- and 4-; 2- and 5-; 2- and 6-; 3- and 4- or 3- and 5-position), oxathianylene (O at the 2-position and S at the 4-, 5- or 6-position; O at the 3-position and S at the 5- or 6-position; or S at the 2-position and O at the 4-position), dioxepanylene (O at the 2- and 4-; 2- and 5-; 2- and 6-; 2- and 7-; 3- and 5- or 3- and 6-position), dithiepanylene (S at the 2- and 3-; 2- and 4-; 2- and 5-; 2- and 6-; 2- and 7-; 3- and 4-; 3- and 5-; 3- and 6- or 4- and 5-position), oxathiepanylene (O at the 2-position and S at the 4-, 5-, 6- or 7-position; O at the 3-position and S at the 5-, 6- or 7-position; O at the 4-position and S at the 6- or 7-position; or S at the 2-position and O at the 4-position), dioxocanylene (O at the 2- and 4-; 2- and 5-; 2- and 6-; 2- and 7-; 2- and 8-; 3- and 5-; 3- and 6-; 3- and 7- or 4- and 6-position), dithiocanylene (S at the 2- and 3-; 2- and 4-; 2- and 5-; 2- and 6-; 2- and 7-; 2- and 8-; 3- and 4-; 3- and 5-; 3- and 6-; 3- and 7-; 4- and 5- or 4- and 6-position) and oxathiocanylene (O at the 2-position and S at the 2-, 3-, 4-, 5-, 6- or 7-position; O at the 3-position and S at the 5-, 6-, 7- or 8-position; O at the 4-position and S at the 6-, 7- or 8-position; S at the 2-position and O at the 4- or 5-position; S at the 3-position and O at the 5-position).

[0045] As used herein, the term "monocyclic 4- to 10-membered O / S-heterocycloalkylene" means that 4 to 10 members of the O / S-heterocycloalkylene are linked in such a manner as to form a single ring (e.g., tetrahydropyranylene). Thus, except for the spiro carbon atom of ring A (which belongs to both ring A and the quinoxaline moiety), the remaining 3 to 9 ring atoms of ring A belong only to ring A, i.e., those ring atoms of ring A do not belong to any further rings. Accordingly, according to the present invention, the term "monocyclic 4- to 10-membered O / S-heterocycloalkylene" does not encompass polycyclic (e.g., bicyclic or tricyclic) structures (e.g., 3,4-dihydro-2H-chromenylene) in which at least two ring atoms belong to more than one ring.

[0046] As used herein, the term "cycloalkylene" means a cycloalkyl group as defined above, in which one hydrogen atom has been removed from the same carbon atom to form a geminal divalent group. Preferably, the cycloalkylene is monocyclic. The term "cycloalkylene" is also intended to include a partially or fully hydrogenated form (e.g., dihydro, tetrahydro or perhydro form) (preferably a partially or fully hydrogenated form of the above monocyclic aryl group) of the above aryl group in which one hydrogen atom has been removed from the same carbon atom to form a geminal divalent group. Thus, according to the present invention, the cycloalkylene may be saturated or unsaturated (i.e., may contain one or more double bonds within the ring), but cannot be aromatic. Exemplary cycloalkylene groups include cyclohexylene, cycloheptylene, cyclopropylene, cyclobutylene, cyclopentylene, cyclooctylene, cyclohexenylene, cycloheptenylene, cyclopropenylene, cyclobutenylene, cyclopentenylene and cyclooctenylene.

[0047] As used herein, the term "monocyclic 3- to 10-membered cycloalkylene" means that 3 to 10 ring carbon atoms of the cycloalkylene are linked in such a manner as to form a single ring (e.g., cyclohexylene). Thus, excluding the spiro carbon atom of ring A (which belongs to both ring A and the quinoxaline moiety), the remaining 2 to 9 ring carbon atoms of ring A belong only to ring A, i.e., those ring carbon atoms of ring A do not belong to any further rings. Accordingly, according to the present invention, the term "monocyclic 3- to 10-membered cycloalkylene" does not encompass polycyclic (e.g., bicyclic or tricyclic) structures (e.g., indanylene) in which at least two ring atoms belong to more than one ring.

[0048] The term "halogen" or "halo" means fluoro, chloro, bromo or iodo.

[0049] The term "azide" means N 3 means.

[0050] As used herein, the term "any two R 9 bonded to the same carbon atom of ring A may together form =X" means that when two monovalent groups (i.e., R 9 ) replace a total of two hydrogen atoms bonded to only one ring carbon atom of ring A, they may form the divalent group =X. For example, according to the present invention, in the following formula:

Chemical formula

Chemical formula

[0051] The term "optionally substituted" means that one or more (e.g., 1 to the maximum number of hydrogen atoms attached to a group, e.g., 1, 2, 3, 4, 5, 6, 7, 8, 9, or 10, e.g., between 1 and 5, 1 and 4, or 1 and 3, or 1 or 2) hydrogen atoms are alkyl (preferably C 1-6 alkyl), alkenyl (preferably C 2-6 alkenyl), alkynyl (preferably C 2-6 alkynyl), aryl (preferably 3- to 14-membered aryl), heteroaryl (preferably 3- to 14-membered heteroaryl), cycloalkyl (preferably 3- to 14-membered cycloalkyl), heterocyclyl (preferably 3- to 14-membered heterocyclyl), halogen, -CN, azide, -NO 2 , -OR 71 , -N(R 72 )(R 73 ), -ON(R 72 )(R 73 ), -N + (-O - )(R 72 )(R 73 ), -S(O) 0-2 R 71 , -S(O) 0-2 OR 71 , -OS(O) 0-2 R 71 , -OS(O) 0-2 OR 71 , -S(O) 0-2 N(R 72 )(R 73 ), -OS(O) 0-2 N(R 72 )(R 73 ), -N(R 71 )S(O) 0-2 R 71 , -NR 71 S(O) 0-2 OR71 、 -NR 71 S(O) 0-2 N(R 72 )(R 73 )、 -C(=X 1 )R 71 、 -C(=X 1 )X 1 R 71 、 -X 1 C(=X 1 )R 71 and -X 1 C(=X 1 )X 1 R 71 etc., may be substituted with a group different from hydrogen (i.e., a first-level substituent), and / or any two first-level substituents bonded to the same carbon atom of a cycloalkyl or heterocyclyl group may together form =X 1 . Here, the alkyl, alkenyl, alkynyl, aryl, heteroaryl, cycloalkyl, and heterocyclyl groups that are first-level substituents may each be substituted with one, two, or three substituents (i.e., second-level substituents), and the second-level substituents are C 1-6 alkyl, C 2-6 alkenyl, C 2-6 alkynyl, 3- to 14-membered aryl, 3- to 14-membered heteroaryl, 3- to 14-membered cycloalkyl, 3- to 14-membered heterocyclyl, halogen, -CF 3 3, -CN, azide, -NO 2 2, -OR 81 3, -N(R 82 )(R 83 )、 -ON(R 82 )(R 83 )、 -N + (-O - )(R 82 )(R 83 )、 -S(O) 0-2 R 81 、 -S(O) 0-2 OR 81 、 -OS(O) 0-2 R 81 、 -OS(O) 0-2 OR 81 、 -S(O) 0-2 N(R 82 )(R83 )、 -OS(O) 0-2 N(R 82 )(R 83 )、 -N(R 81 )S(O) 0-2 R 81 、 -NR 81 S(O) 0-2 OR 81 、 -NR 81 S(O) 0-2 N(R 82 )(R 83 )、 -C(=X 2 )R 81 、 -C(=X 2 )X 2 R 81 、 -X 2 C(=X 2 )R 81 and -X 2 C(=X 2 )X 2 R 81 selected from the group consisting of, and / or any two second-level substituents attached to the same carbon atom of a cycloalkyl or heterocyclyl group may together form =X 2 , wherein the C 1-6 alkyl, C 2-6 alkenyl, C 2-6 alkynyl, 3- to 14-membered aryl, 3- to 14-membered heteroaryl, 3- to 14-membered cycloalkyl, 3- to 14-membered heterocyclyl groups are each optionally substituted with one, two or three substituents (i.e., third-level substituents), and the third-level substituents are independently C 1-3 alkyl, halogen, -CF 3 , -CN, azide, -NO 2 , -OH, -O(C 1-3 alkyl), -S(C 1-3 alkyl), -NH 2 , -NH(C 1-3 alkyl), -N(C 1-3 alkyl) 2 , -NHS(O) 2 (C 1-3 alkyl), -S(O) 2 NH 2-z (C 1-3 alkyl)z , -C(=O)OH, -C(=O)O(C 1-3 alkyl), -C(=O)NH 2-z (C 1-3 alkyl) z , -NHC(=O)(C 1-3 alkyl), -NHC(=NH)NH z-2 (C 1-3 alkyl) z and -N(C 1-3 alkyl)C(=NH)NH 2-z (C 1-3 alkyl) z selected from the group consisting of, where z is 0, 1 or 2, and C 1-3 alkyl is methyl, ethyl, propyl or isopropyl, and / or any two third-level substituents bonded to the same carbon atom of a cycloalkyl or heterocyclyl group may together form =O, =S, =NH or =N(C 1-3 alkyl); R 71 , R 72 and R 73 are independently selected from the group consisting of -H, C 1-6 alkyl, C 2-6 alkenyl, C 2-6 alkynyl, 3- to 7-membered cycloalkyl, 5- or 6-membered aryl, 5- or 6-membered heteroaryl and 3- to 7-membered heterocyclyl, where the alkyl, alkenyl, alkynyl, cycloalkyl, aryl, heteroaryl and heterocyclyl groups are each optionally C 1-3 alkyl, halogen, -CF 3 , -CN, azide, -NO 2 , -OH, -O(C 1-3 alkyl), -S(C 1-3 alkyl), -NH 2 , -NH(C 1-3 alkyl), -N(C 1-3 alkyl) 2 , -NHS(O) 2 (C 1-3 alkyl), -S(O) 2 NH 2-z (C 1-3 alkyl) z, -C(=O)OH, -C(=O)O(C 1-3 alkyl), -C(=O)NH 2-z (C 1-3 alkyl) z , -NHC(=O)(C 1-3 alkyl), -NHC(=NH)NH z-2 (C 1-3 alkyl) z and -N(C 1-3 alkyl)C(=NH)NH 2-z (C 1-3 alkyl) z (z is 0, 1 or 2, and C 1-3 alkyl is methyl, ethyl, propyl or isopropyl) and is substituted with one, two or three substituents selected from the group consisting of; or, R 72 and R 73 together with the nitrogen atom to which they are attached, optionally, C 1-3 alkyl, halogen, -CF 3 , -CN, azide, -NO 2 , -OH, -O(C 1-3 alkyl), -S(C 1-3 alkyl), -NH 2 , -NH(C 1-3 alkyl), -N(C 1-3 alkyl) 2 , -NHS(O) 2 (C 1-3 alkyl), -S(O) 2 NH 2-z (C 1-3 alkyl) z , -C(=O)OH, -C(=O)O(C 1-3 alkyl), -C(=O)NH 2-z (C 1-3 alkyl) z , -NHC(=O)(C 1-3 alkyl), -NHC(=NH)NH z-2 (C 1-3 alkyl) z and -N(C 1-3 alkyl)C(=NH)NH 2-z (C 1-3 alkyl) z (z is 0, 1 or 2, and C1-3 The 5- or 6-membered ring may be formed with 1, 2 or 3 substituents selected from the group consisting of alkyl which is methyl, ethyl, propyl or isopropyl; R 81 , R 82 and R 83 are each independently selected from -H, C 1-4 alkyl, C 2-4 alkenyl, C 2-4 alkynyl, 3- to 6-membered cycloalkyl, 5- or 6-membered aryl, 5- or 6-membered heteroaryl and 3- to 6-membered heterocyclyl, where the alkyl, alkenyl, alkynyl, cycloalkyl, aryl, heteroaryl and heterocyclyl groups may each optionally be substituted with C 1-3 alkyl, halogen, -CF 3 , -CN, azide, -NO 2 , -OH, -O(C 1-3 alkyl), -S(C 1-3 alkyl), -NH 2 , -NH(C 1-3 alkyl), -N(C 1-3 alkyl) 2 , -NHS(O) 2 (C 1-3 alkyl), -S(O) 2 NH 2-z (C 1-3 alkyl) z , -C(=O)OH, -C(=O)O(C 1-3 alkyl), -C(=O)NH 2-z (C 1-3 alkyl) z , -NHC(=O)(C 1-3 alkyl), -NHC(=NH)NH z-2 (C 1-3 alkyl) z and -N(C 1-3 alkyl)C(=NH)NH 2-z (C 1-3 alkyl) z (z is 0, 1 or 2 and C 1-3 alkyl is methyl, ethyl, propyl or isopropyl) and is substituted with 1, 2 or 3 substituents selected from the group; Or, R 82 and R 83 together with the nitrogen atom to which they are attached may optionally form a 5- or 6-membered ring substituted with one, two or three substituents selected from the group consisting of C 1-3 alkyl, halogen, -CF 3 , -CN, azide, -NO 2 , -OH, -O(C 1-3 alkyl), -S(C 1-3 alkyl), -NH 2 , -NH(C 1-3 alkyl), -N(C 1-3 alkyl) 2 , -NHS(O) 2 (C 1-3 alkyl), -S(O) 2 NH 2-z (C 1-3 alkyl) z , -C(=O)OH, -C(=O)O(C 1-3 alkyl), -C(=O)NH 2-z (C 1-3 alkyl) z , -NHC(=O)(C 1-3 alkyl), -NHC(=NH)NH z-2 (C 1-3 alkyl) z and -N(C 1-3 alkyl)C(=NH)NH 2-z (C 1-3 alkyl) z (z is 0, 1 or 2, and C 1-3 alkyl is methyl, ethyl, propyl or isopropyl); X 1 and X 2 are independently O, S and NR 84 (R 84 is -H or C 1-3 alkyl).

[0052] Typical level 1 substituents are preferably C 1-6 alkyl, C 2-6 alkenyl, C 2-6alkynyl, 3- to 14-membered (e.g., 5- or 6-membered) aryl, 3- to 14-membered (e.g., 5- or 6-membered) heteroaryl, 3- to 14-membered (e.g., 3- to 7-membered) cycloalkyl, 3- to 14-membered (e.g., 3- to 7-membered) heterocyclyl, halogen, -CN, azide, -NO 2 , -OR 71 , -N(R 72 )(R 73 ), -S(O) 0-2 R 71 , -S(O) 0-2 OR 71 , -OS(O) 0-2 R 71 , -OS(O) 0-2 OR 71 , -S(O) 0-2 N(R 72 )(R 73 ), -OS(O) 0-2 N(R 72 )(R 73 ), -N(R 71 )S(O) 0-2 R 71 , -NR 71 S(O) 0-2 OR 71 , -C(=X 1 )R 71 , -C(=X 1 )X 1 R 71 , -X 1 C(=X 1 )R 71 and -X 1 C(=X 1 )X 1 R 71 (e.g., C 1-4 alkyl, C 2-4 alkenyl, C 2-4 alkynyl, 5- or 6-membered aryl, 5- or 6-membered heteroaryl, 3- to 7-membered cycloalkyl, 3- to 7-membered heterocyclyl, halogen, -CF 3 , -CN, azide, -NO 2 , -OH, -O(C 1-3 alkyl), -S(C 1-3 alkyl), -NH 2 , -NH(C 1-3 alkyl), -N(C 1-3 alkyl) 2, -NHS(O) 2 (C 1-3 alkyl), -S(O) 2 NH 2-z (C 1-3 alkyl) z , -C(=O)OH, -C(=O)O(C 1-3 alkyl), -C(=O)NH 2-z (C 1-3 alkyl) z , -NHC(=O)(C 1-3 alkyl), -NHC(=NH)NH z-2 (C 1-3 alkyl) z and -N(C 1-3 alkyl)C(=NH)NH 2-z (C 1-3 alkyl) z (z is 0, 1 or 2, and C 1-3 alkyl is methyl, ethyl, propyl or isopropyl)); X 1 is independently selected from O, S, NH and N(CH 3 )); R 71 , R 72 and R 73 are as defined above or, preferably, are independently selected from -H, C 1-4 alkyl, C 2-4 alkenyl, C 2-4 alkynyl, 5- or 6-membered cycloalkyl, 5- or 6-membered aryl, 5- or 6-membered heteroaryl and 5- or 6-membered heterocyclyl, where the alkyl, alkenyl, alkynyl, cycloalkyl, aryl, heteroaryl and heterocyclyl groups may each optionally be C 1-3 alkyl, halogen, -CF 3 , -CN, azide, -NO 2 , -OH, -O(C 1-3 alkyl), -S(C 1-3 alkyl), -NH 2 , -NH(C 1-3 alkyl), -N(C 1-3 alkyl) 2 , -NHS(O) 2 (C 1-3 alkyl), -S(O) 2 NH2-z (C 1-3 Alkyl) z , -C(=O)OH, -C(=O)O(C 1-3 alkyl), -C(=O)NH 2-z (C 1-3 Alkyl) z , -NHC(=O)(C 1-3 alkyl), -NHC(=NH)NH z-2 (C 1-3 Alkyl) z and -N(C 1-3 Alkyl)C(=NH)NH 2-z (C 1-3 Alkyl) z (z is 0, 1 or 2; C 1-3 alkyl is methyl, ethyl, propyl or isopropyl; or R 72 and R 73 together with the nitrogen atom to which they are attached, optionally 1-3 Alkyl, halogen, -CF 3 , -CN, azide, -NO 2 , -OH, -O(C 1-3 alkyl), -S(C 1-3 alkyl), -NH 2 , -NH(C 1-3 alkyl), -N(C 1-3 Alkyl) 2 , -NHS(O) 2 (C 1-3 alkyl), -S(O) 2 NH 2-z (C 1-3 Alkyl) z , -C(=O)OH, -C(=O)O(C 1-3 alkyl), -C(=O)NH 2-z (C 1-3 Alkyl) z , -NHC(=O)(C 1-3 alkyl), -NHC(=NH)NH z-2 (C 1-3 Alkyl) z and -N(C 1-3 Alkyl)C(=NH)NH 2-z (C 1-3 Alkyl)z (z is 0, 1, or 2, and C 1-3 alkyl is methyl, ethyl, propyl, or isopropyl) and may form a 5- or 6-membered ring substituted with one, two, or three substituents selected from the group consisting of

[0053] Typical level 2 substituents are preferably C 1-4 alkyl, C 2-4 alkenyl, C 2-4 alkynyl, 5- or 6-membered aryl, 5- or 6-membered heteroaryl, 5- or 6-membered cycloalkyl, 5- or 6-membered heterocyclyl, halogen, -CF 3 , -CN, azide, -NO 2 , -OH, -O(C 1-3 alkyl), -S(C 1-3 alkyl), -NH 2 , -NH(C 1-3 alkyl), -N(C 1-3 alkyl) 2 , -NHS(O) 2 (C 1-3 alkyl), -S(O) 2 NH 2-z (C 1-3 alkyl) z , -C(=O)OH, -C(=O)O(C 1-3 alkyl), -C(=O)NH 2-z (C 1-3 alkyl) z , -NHC(=O)(C 1-3 alkyl), -NHC(=NH)NH z-2 (C 1-3 alkyl) z and -N(C 1-3 alkyl)C(=NH)NH 2-z (C 1-3 alkyl) z (z is 0, 1, or 2, and C 1-3Alkyl is methyl, ethyl, propyl or isopropyl. Particularly preferred second level substituents include 4-morpholinyl, homomorpholinyl, 4-piperidinyl, homopiperidinyl (i.e. azepanyl, especially 4-azepanyl), 4-piperazinyl, homopiperazinyl (i.e. diazepanyl, especially 2,4-diazepanyl), N-methyl-piperazin-4-yl, N-methyl-homopiperazinyl, -CH 2 CH 2 OCH 3 , -OCH 2 CH 2 OCH 3 , -CH 2 CH 2 NH 2-z (CH 3 ) z , -OCH 2 CH 2 NH 2-z (CH 3 ) z , -CF 3 and -OCF 3 Includes:

[0054] Exemplary third level substituents are preferably phenyl, furanyl, pyrrolyl, thienyl, imidazolyl, oxazolyl, isoxazolyl, thiazolyl, pyridyl, pyrazinyl, pyrimidinyl, pyridazinyl, partially and fully hydrogenated forms of the above groups, morpholino, C 1-3 Alkyl, halogen, -CF 3 , -OH, -OCH 3 , -SCH 3 , -NH 2-z (CH 3 ) z , -C(=O)OH and -C(=O)OCH 3 (z is 0, 1 or 2).

[0055] The term "aromatic" as used in the context of hydrocarbons means that the entire molecule must be aromatic. For example, when a monocyclic aryl is hydrogenated (either partially or completely), the resulting hydrogenated cyclic structure is classified as cycloalkyl for the purposes of the present invention. Similarly, when a bicyclic or polycyclic aryl (e.g., naphthyl) is hydrogenated, the resulting hydrogenated bicyclic or polycyclic structure (e.g., 1,2-dihydronaphthyl) is classified as cycloalkyl for the purposes of the present invention (even if one of the rings remains aromatic as in 1,2-dihydronaphthyl). In the present application, a similar distinction is made between heteroaryl and heterocyclyl. For example, indolinyl, i.e., the dihydro variant of indolyl, has only one of the rings of the bicyclic structure that is aromatic and one of the ring atoms is a heteroatom, and is therefore classified as heterocyclyl for the purposes of the present invention.

[0056] As used herein, the phrase "partially hydrogenated form" of an unsaturated compound or group formally means that by adding hydrogen to a compound or group that was initially unsaturated, some, but not all, of the unsaturation has been removed without removing all of the unsaturation. As used herein, the phrase "fully hydrogenated form" of an unsaturated compound or group is used interchangeably with the term "perhydro" and formally means that by adding hydrogen to a compound or group that was initially unsaturated, all of the unsaturation has been removed. For example, the partially hydrogenated form of a 5-membered heteroaryl group (such as furan, containing two double bonds in the ring) includes the dihydro form of the 5-membered heteroaryl group (e.g., 2,3-dihydrofuran or 2,5-dihydrofuran), but the tetrahydro form of the 5-membered heteroaryl group (e.g., tetrahydrofuran, i.e., THF) is the fully hydrogenated form (or perhydro form) of the 5-membered heteroaryl group. Similarly, for a 6-membered heteroaryl group having three double bonds in the ring (e.g., pyridyl), the partially hydrogenated form includes the di- and tetrahydro forms (e.g., di- and tetrahydropyridyl), but the hexahydro form (e.g., piperidinyl in the case of the heteroaryl pyridyl) is the fully hydrogenated (or perhydro) derivative of the 6-membered heteroaryl group. Therefore, according to the present invention, when an aryl or heteroaryl contains at least 4 unsaturated moieties consisting of double and triple bonds between ring atoms, the hexahydro form of the aryl or heteroaryl can only be regarded as the partially hydrogenated form.

[0057] As used herein, the terms "optionally" or "optionally" mean that the event, situation or condition described later may or may not occur, and the description includes the case where the event, situation or condition occurs and the case where the event, situation or condition does not occur.

[0058] "Isomers" are compounds that have the same molecular formula but different structures (structural isomers) or different geometric positions of functional groups and / or atoms (stereoisomers). "Enantiomers" are a pair of stereoisomers that are non-superimposable mirror images of each other. "Racemic mixture" or "racemate" contains equal amounts of a pair of enantiomers and is denoted by the prefix (±). "Diastereomers" are stereoisomers that are non-superimposable mirror images of each other. "Tautomers" are structural isomers of the same chemical substance that naturally interconvert with each other even in pure form.

[0059] If the structural formulas shown in this application can be interpreted as encompassing more than one isomer, then the structural formula, unless otherwise expressly stated, includes all possible isomers and thus each such individual isomer. For example, if ring A is of the following formula:

Chemical formula

Chemical formula

[0060] As used herein, "polymorph" means that a solid substance (e.g., a compound) can exist in more than one form or crystal structure, i.e., "polymorphism" or "polymorphic form". In the present invention, the terms "polymorphism", "polymorphic form" and "polymorph" are used interchangeably. According to the present invention, these "polymorphisms" include crystalline forms, amorphous forms, solvates and hydrates. Primarily, the reasons for the existence of different polymorphic forms lie in the use of different conditions during the crystallization process as follows: · Solvent effect (the packing of crystals can be different in polar solvents and non-polar solvents); · Some impurities that inhibit the growth pattern and are favorable for the growth of metastable polymorphs; · The degree of supersaturation when the substance is crystallized (generally, the higher the concentration above the solubility, the higher the possibility of a metastable form); · The temperature at which crystallization is carried out; · The geometry of the covalent bonds (differences lead to polymorphs of the three-dimensional structure); · Changes in stirring conditions.

[0061] Polymorphs may have different chemical, physical and / or pharmacological properties, including but not limited to melting point, X-ray crystal and diffraction pattern, chemical reactivity, solubility, dissolution rate, vapor pressure, density, hygroscopicity, fluidity, stability, compactability and biological availability. Polymorphs may naturally change from a metastable (unstable) form to a stable form at a specific temperature. According to Ostwald's rule, generally, the first to crystallize is not the most stable polymorph, but the least stable polymorph. Thus, the quality, effectiveness, safety, processability and / or manufacture of a compound, such as the compounds of the present invention, may be affected by the polymorph. Often, for reasons of minimal possibility of change to another polymorph, the most stable polymorph of a compound (such as the compounds of the present invention) is selected. However, for reasons other than stability, such as solubility, dissolution rate and / or biological availability, a polymorph that is not the most stable polymorph may be selected.

[0062] As used herein, the term "crystalline form" of a substance means that the smallest elements (i.e., atoms, molecules or ions) of the substance form a crystal structure. The "crystal structure" referred to herein means the unique three-dimensional arrangement of atoms or molecules in a crystalline liquid or solid, characterized by a pattern, a set of atoms arranged in a specific manner and a lattice showing long-range order and symmetry. The lattice is an array of points that repeats periodically in three dimensions, and the pattern is located on the lattice points. The subunit of the lattice is the unit cell. The lattice parameters are the lengths of the edges of the unit cell and the angles between them. The symmetry of a crystal is embodied in its space group. To describe a crystal structure, the following parameters are required: chemical formula, lattice parameters, space group, atomic coordinates and occupancy numbers of point positions.

[0063] As used herein, the term "amorphous form" of a substance means that the smallest elements (i.e., atoms, molecules or ions) of the substance are not arranged in a lattice but are arranged irregularly. Thus, unlike a crystal in which there is short-range order (a certain distance to the next adjacent atom) and long-range order (periodic repetition of the basic lattice), only short-range order exists in the amorphous form.

[0064] As used herein, the term "complex of a compound" refers to a higher-order compound formed by the association of one or more other molecules of the compound. Exemplary complexes of a compound include, but are not limited to, solvates, clusters and chelates of the compound.

[0065] As used herein, the term "solvate" refers to an addition complex of a substance dissolved in a solvent (e.g., an organic solvent (e.g., aliphatic alcohols (methanol, ethanol, n-propanol, isopropanol, etc.), acetone, acetonitrile, ether, etc.), water or a mixture of two or more of these liquids), wherein the addition complex exists in the form of a crystal or a mixed crystal. The amount of solvent contained in the addition complex may be stoichiometric or non-stoichiometric. "Hydrate" is a solvate in which the solvent is water.

[0066] In an isotope-labeled compound, one or more atoms are replaced with corresponding atoms having the same number of protons but different numbers of neutrons. For example, a hydrogen atom may be replaced with a deuterium atom. Exemplary isotopes that can be used in the compounds of the present invention include deuterium, 11 C, 13 C, 14 C, 15 N, 18 F, 32 S, 36 Cl and 125 I.

[0067] The term "half-life" relates to the period required to remove half of the activity, amount, or number of molecules. In the context of the present invention, the half-life of the compound of formula (I) represents the stability of the compound.

[0068] The terms "patient", "individual", or "animal" relate to multicellular animals such as vertebrates. For example, in the context of the present invention, vertebrates include mammals, birds (e.g., poultry), reptiles, amphibians, bony fish, and cartilaginous fish, and in particular, any of the above-mentioned domesticated animals, as well as animals in captivity (especially vertebrates) such as zoo animals (especially vertebrates). In the context of the present invention, mammals include humans, non-human primates, domesticated mammals such as dogs, cats, sheep, cows, goats, pigs, horses, etc., laboratory mammals such as mice, rats, rabbits, guinea pigs, etc., and mammals in captivity such as zoo mammals, but are not limited thereto. The term "animal" as used herein includes humans. Non-limiting specific examples of birds include domesticated poultry, and also include birds such as chickens, turkeys, ducks, geese, pigeons, doves, pheasants, etc., while non-limiting specific examples of bony or cartilaginous fish include those suitable for cultivation by aquiculture, and include bony fish such as salmon, trout, perch, carp, catfish, etc.

[0069] Compound In one embodiment, the present invention provides the following general formula (I):

Chemical formula

[0070] In one embodiment, the spiroquinoxaline derivative has the following general formula (II): [Chemical formula] [wherein, R 1 ~R 5 , E, L, and G are as defined above or below, and ring A is (i) N-heterocycloalkylene, wherein the N-heterocycloalkylene contains one ring nitrogen atom and is 4 to 8 membered (preferably 5, 6, or 7 membered, more preferably 6 or 7 membered), or contains two or three ring nitrogen atoms and is 5 to 8 membered, preferably 5, 6, or 7 membered, more preferably 6 or 7 membered; (ii) O / S-heterocycloalkylene, wherein the O / S-heterocycloalkylene contains one ring oxygen or sulfur atom and is 4 to 8 membered (preferably 5, 6, or 7 membered, more preferably 6 or 7 membered), or contains two ring heteroatoms selected from oxygen and sulfur and is 5 to 8 membered, preferably 5, 6, or 7 membered, more preferably 6 or 7 membered; or (iii) cycloalkylene, wherein the cycloalkylene is 3 to 8 membered, preferably 4, 5, 6, or 7 membered, more preferably 6 or 7 membered) It has. In one embodiment of the spiroquinoxaline derivative of formula (II), ring A itself is unsaturated (i.e., the members of ring A form 1, 2 or 3 (preferably 1 or 2, most preferably 1) double bonds within the ring), but is not aromatic. In another embodiment of the spiroquinoxaline derivative of formula (II), ring A is saturated (i.e., ring A itself has no unsaturation within the ring); provided that when ring A is substituted with one or more (e.g., 1 to the maximum number of hydrogen atoms bonded to ring A, e.g., up to 1, 2, 3, 4, 5, 6, 7, 8, 9 or 10, e.g., between 1 and 5, 1 and 4 or 1 and 3, or 1 or 2) R 9 substituents, R 9 may be unsaturated (i.e., may contain double and / or triple bonds and / or one or more (e.g., 1, 2 or 3) aromatic rings). In any of the above embodiments of the spiroquinoxaline derivative of formula (II), the ring nitrogen, oxygen and / or sulfur atoms of ring A (preferably all ring heteroatoms of ring A) are not in the alpha position relative to the spiro carbon atom (i.e., in this embodiment, preferably, the two atoms in the alpha position relative to the spiro carbon atom of ring A are carbon atoms). In any of the above embodiments of the spiroquinoxaline derivative of formula (II), ring A is in each case independently substituted with one or more (e.g., 1 to the maximum number of hydrogen atoms bonded to ring A, e.g., up to 1, 2, 3, 4, 5, 6, 7, 8, 9 or 10, e.g., between 1 and 5, 1 and 4 or 1 and 3, or 1 or 2) independently selected R 9which is replaced by piperidinylene, azepanylene (e.g., homopiperidinylene), azetidinylene, pyrrolidinylene, azocanylene, pyrazolidinylene, hexahydropyridazinylene, hexahydropyrimidinylene, diazepanylene (e.g., homopiperazinylene), diazocanylene, triazepanylene, triazocanylene, di- and tetrahydropyranylene, di- and tetrahydrothiopyranylene, oxepanylene, thiepanylene, oxetanylene, thietanylene, di- and tetrahydrofuranylene, di- and tetrahydrothienylene, oxocanylene, thiocanylene, dithiolanylene, oxathiolanylene, dioxanylene, dithianylene, oxathianylene, dioxepanylene, dithiepanylene, oxathiepanylene, dioxocanylene, dithiocanylene, oxathiocanylene, cyclohexylene, cycloheptylene, cyclopropylene, cyclobutylene, cyclopentylene, cyclooctylene, cyclohexenylene, cycloheptenylene, cyclopentenylene, cyclooctenylene and their positional isomers. In one embodiment of the spiroquinoxaline derivative of formula (II), ring A may each independently be selected from one or more (e.g., 1 to the maximum number of hydrogen atoms bonded to ring A, e.g., up to 1, 2, 3, 4, 5, 6, 7, 8, 9 or 10, e.g., between 1 to 5, 1 to 4 or 1 to 3, or 1 or 2) of the independently selected R 9which is replaced by 3- and 4-piperidinylene (N is in the 3- or 4-position relative to the spiro carbon atom); 3- and 4-azepanylene, 3-azetidinylene, 3-pyrrolidinylene, 3-, 4- and 5-azonianylene, 3,4-pyrazolidinylene, 3,4-hexahydropyridazinylene, 3,5-hexahydropyrimidinylene, 3,4-, 3,5-, 3,6- and 4,5-diazepanylene, 3,4-, 3,5-, 3,6-, 3,7-, 4,5-, 4,6-diazocanylene, 3- and 4-tetrahydropyranylene (O is in the 3- or 4-position relative to the spiro carbon atom); 3- and 4-tetrahydrothiopyranylene; 3- and 4-oxepanylene; 3- and 4-thiepanylene; 3-oxetanylene; 3-thietanylene; 3-tetrahydrofuranylene; 3-tetrahydrothienylene; 3-, 4- and 5-oxocanylene; 3-, 4- and 5-thiocanylene; 3,4-dithiolanylene; 3,4-oxathiolanylene; 3,5-dioxanylene; 3,4- and 3,5-dithianylene; 3,4-, 3,5- and 4,3-oxathianylene; 3,5- and 3,6-dioxepanylene; 3,4-, 3,5-, 3,6- and 4,5-dithiepanylene; 3,4-, 3,5-, 3,6-, 4,5-, 4,3- and 4,2-oxathiepanylene; 3,5-, 3,6-, 3,7- and 4,6-dioxocanylene; 3,3-, 3,4-, 3,5-, 3,6, 3,7-, 4,5- and 4,6-dithiocanylene; and 3,4-, 3,5-, 3,6-, 3,7-, 4,5-, 4,6-, 4,7-, 4,3-, 5,4- and 5,3-oxathiocanylene, cyclohexylene, cycloheptylene, cyclopropylene, cyclobutylene, cyclopentylene and cyclooctylene, selected from the group consisting of. In one embodiment of the spiroquinoxaline derivative of formula (II), ring A is, in each case, optionally one or more (e.g., 1 to the maximum number of hydrogen atoms bonded to ring A, e.g., up to 1, 2, 3, 4, 5, 6, 7, 8, 9 or 10, e.g., between 1 and 5, 1 and 4 or 1 and 3, or 1 or 2) independently selected R 94-Piperidinylene, 3-piperidinylene, 3-azetidinylene, 3-pyrrolidinylene, 4-azepanylene, 3-azepanylene, 5-azocanylene, 4-azocanylene, 3-azocanylene, 3,6-diazepanylene (e.g., 4-piperidinylene, 3-piperidinylene, 4-azepanylene and 3-azepanylene), 4-tetrahydropyranylene, 4-tetrahydrothiopyranylene, 3-tetrahydropyranylene, 3-tetrahydrothiopyranylene, 4-oxepanylene, 4-thiepanylene, 3-oxepanylene, 3-thiepanylene, 3-oxetanylene, 3-thietanylene, 3-tetrahydrofuranylene, 3-tetrahydrothienylene, 5-oxocanylene, 5-thiocanylene, 4-oxocanylene, 4-thiocanylene (e.g., -tetrahydropyranylene, 4-tetrahydrothiopyranylene, 3-tetrahydropyranylene, 3-tetrahydrothiopyranylene, 4-oxepanylene, 4-thiepanylene, 3-oxepanylene and 3-thiepanylene), cyclohexylene, cycloheptylene, cyclopentylene and cyclooctylene, which is replaced by

[0071] In any of the above embodiments of the spiroquinoxaline derivative of formula (II), ring A may be unsubstituted.

[0072] In any of the above embodiments of the spiroquinoxaline derivative of formula (II), wherein ring A is substituted with one or more (e.g., 1 to the maximum number of hydrogen atoms bonded to ring A, e.g., up to 1, 2, 3, 4, 5, 6, 7, 8, 9 or 10, e.g., between 1 to 5, 1 to 4 or 1 to 3, or 1 or 2) independently selected R 9 In any of the above embodiments of the spiroquinoxaline derivative of formula (II), which is substituted with, (i) only one or more (preferably 1, 2 or 3) ring heteroatoms (selected from nitrogen, oxygen and sulfur, wherein the maximum number of oxygen and sulfur atoms in ring A is preferably 2) of ring A are independently selected R 9 substituted with; or (ii) only one or more (preferably 1, 2 or 3) ring carbon atoms of ring A are independently selected R 9is replaced; (iii) one or more (preferably one, two or three) ring heteroatoms of ring A (selected from nitrogen, oxygen and sulfur, where the maximum number of oxygen and sulfur atoms in ring A is preferably 2) and one or more (preferably one, two or three) ring carbon atoms (e.g., one or two ring heteroatoms and one or two ring carbon atoms) are independently selected R 9 is replaced, or either of the above. For example, when ring A contains one ring heteroatom (selected from nitrogen, oxygen and sulfur), ring A is (i) at the ring heteroatom (preferably, when ring A is a 4- or 5-membered ring, it is at the 3-position, when ring A is a 6- or 7-membered ring, it is at the 3- or 4-position (preferably the 4-position), and when ring A is an 8-membered ring, it is at the 3, 4 or 5-position (preferably the 4- or 5-position)) only R 9 is; (ii) only at one or two ring carbon atoms of ring A, each with one or two independently selected R 9 is; or (iii) at the ring heteroatom (preferably, when ring A is a 4- or 5-membered ring, it is at the 3-position, when ring A is a 6- or 7-membered ring, it is at the 3- or 4-position (preferably the 4-position), and when ring A is an 8-membered ring, it is at the 3, 4 or 5-position (preferably the 4- or 5-position)) R 9 is, and at one or two ring carbon atoms of ring A, each with one or two independently selected R 9 is optionally substituted.

[0073] R 9 substitutes the hydrogen atom bonded to the ring carbon atom of ring A. In any of the above embodiments of the spiroquinoxaline derivative of formula (II), such R 9 are each independently C 1-6 alkyl, C 2-6 alkenyl, C 2-6 alkynyl, 5- or 6-membered aryl, 5- or 6-membered heteroaryl, 3- to 7-membered cycloalkyl, 3- to 7-membered heterocyclyl, halogen, -CN, -OR 11 、-N(R 12 )(R 13 ), -S(O) 0-2 R 11 、-S(O) 1-2 N(R12 )(R 13 )、 -N(R 11 )S(O) 1-2 R 11 、 -NR 11 S(O) 1-2 N(R 12 )(R 13 )、 -C(=X)R 11 、 -C(=X)XR 11 、 -XC(=X)R 11 and -XC(=X)XR 11 may be selected from the group consisting of, wherein said C 1-6 alkyl, C 2-6 alkenyl, C 2-6 alkynyl, 5 - or 6 - membered aryl, 5 - or 6 - membered heteroaryl, 3 - to 7 - membered cycloalkyl, and 3 - to 7 - membered heterocyclyl groups each may optionally be substituted with one or more (e.g., 1 to the maximum number of hydrogen atoms bonded to the C 1-6 alkyl, C 2-6 alkenyl, C 2-6 alkynyl, 5 - or 6 - membered aryl, 5 - or 6 - membered heteroaryl, 3 - to 7 - membered cycloalkyl, or 3 - to 7 - membered heterocyclyl group, e.g., 1, 2, 3, 4, 5, 6, 7, 8, 9, or 10, e.g., between 1 - 5, 1 - 4, or 1 - 3, or 1 or 2) independently selected R 30 and / or any two R 9 bonded to the same carbon atom of ring A may together form =X. In any of the above embodiments of the spiroquinoxaline derivative of formula (II) where R 9 replaces a hydrogen atom bonded to a ring carbon atom of ring A, such R 9 are each independently C 1-4 alkyl, C 2-4 alkenyl, C 2-4 alkynyl, 6 - membered aryl, 5 - or 6 - membered heteroaryl, 3, 5, 6, or 7 - membered cycloalkyl, 3, 5, 6, or 7 - membered heterocyclyl, halogen, -CN, -OR 11 , -N(R 12 )(R 13 ), -S(O) 0-2 R 11 , -S(O) 1-2 N(R12 )(R 13 ), -N(R 11 )S(O) 1-2 R 11 , -NR 11 S(O) 1-2 N(R 12 )(R 13 ), -C(=O)R 11 , -C(=O)OR 11 , -C(=O)SR 11 , -C(=O)N(R 14 )(R 11 ), -C(=S)OR 11 , -N(R 14 )C(=O)R 11 , -OC(=O)R 11 , -OC(=S)R 11 , -N(R 14 )C(=O)N(R 14 )(R 11 ) and -N(R 14 )C(=N(R 14 ))N(R 14 )(R 11 ), wherein the C 1-4 Alkyl, C 2-4 Alkenyl, C 2-4 The alkynyl, 6-membered aryl, 5- or 6-membered heteroaryl, 3-, 5-, 6- or 7-membered cycloalkyl, and 3-, 5-, 6- or 7-membered heterocyclyl groups each optionally contain one, two or three independently selected R 30 and / or any two R bonded to the same carbon atom of ring A 9 may be taken together to form =O or =S. In one embodiment, R 9 When each of the groups replaces a hydrogen atom bonded to a ring carbon atom of ring A, each of the groups independently represents C 1-4 Alkyl; -OH, -O(C 1-3 alkyl), -NH 2-z (CH 3 ) z, substituted with one substituent selected from the group consisting of morpholinyl (e.g., 4-morpholinyl), piperazinyl (e.g., 1-piperazinyl), and N-methylpiperazinyl (e.g., 4-methylpiperazin-1-yl) C 1-4 alkyl; -CF 3 , -CH 2 CF 3 , -CH 2 CHF 2 or -CH 2 CH 2 F, etc., C alkyl substituted with one, two, or three halogens (preferably F); -OCF 1-4 , -OCH 3 CF 2 , -OCH 3 CHF 2 or -OCH 2 CH 2 F, etc., -O(C alkyl substituted with one, two, or three halogens (preferably F)); cyclopropyl; 4-morpholinyl; homomorpholinyl; 4-piperidinyl; homopiperidinyl; 4-piperazinyl; homopiperazinyl; 4-methyl-piperazin-1-yl; N-methyl-homopiperazinyl; halogen; -CN; -OH; =O; -O(optionally -NH 2 F, etc., C alkyl substituted with one, two, or three halogens (preferably F); -OCF 1-4 alkyl); -NH 2-z ; -NH(C 3 ) z alkyl); -S(C 1-3 alkyl); -S(O) 2 (optionally -NH 1-3 (CH 1-3 ) 2 alkyl); -S(O) 1-3 NH 2 (C 2-z alkyl) 3 ; -NHS(O) z (optionally -NH 1-3 (CH 2 ) 2-z (C 1-3 alkyl) z ; -NHS(O) 2 (optionally -NH 2-z (CH 3 ) zC which is replaced by 1-3 alkyl); -C(=O)(optionally -NH 2-z (CH 3 ) z C which is replaced by 1-3 alkyl); -C(=O)OH; -C(=O)O(C 1-3 alkyl); -C(=O)NH 2-z (C 1-3 alkyl) z ; -NHC(=O)(optionally -NH 2-z (CH 3 ) z C which is replaced by 1-3 alkyl); -NHC(=O)NH 2-z (CH 3 ) z ; -NHC(=NH)NH z-2 (C 1-3 alkyl) z ; and -N(C 1-3 alkyl)C(=NH)NH 2-z (C 1-3 alkyl) z (z is 0, 1 or 2, and C 1-3 alkyl is methyl, ethyl, propyl or isopropyl) and is selected from the group consisting of. In one embodiment, R 9 When replacing the hydrogen atom bonded to the ring carbon atom of ring A, each independently, methyl; ethyl; isopropyl; tert-butyl; cyclopropyl; -(CH 2 ) d -NH 2-z (CH 3 ) z ; -O(CH 2 ) d -NH 2-z (CH 3 ) z ; -(CH 2 ) d -O(CH 3 ); -CF 3 ; -CH 2 CF 3 ; -CH 2 CHF 2 ; -CH 2 CH 2 F; -(CH 2 ) d-(4-morpholinyl); -(CH 2 ) d -(1-piperazinyl); -(CH 2 ) d -(4-methylpiperazin-1-yl); 4-morpholinyl; 4-piperazinyl; 4-methyl-piperazin-1-yl; halogen (especially, -F, -Cl, -Br); -NHC(=O) (optionally -NH 2-z (CH 3 ) z substituted C 1-3 alkyl); -NHC(=O)NH 2-z (CH 3 ) z ; -NHS(O) 2 (optionally -NH 2-z (CH 3 ) z substituted C 1-3 alkyl); -C(=O)CH 3 ; -C(=O)CH 2 NH 2-z (CH 3 ) z ; -C(=O)NH 2-z (C 1-3 alkyl) z ; -S(O) 2 (C 1-3 alkyl); -S(O) 2 (CH 2 ) d NH 2-z (CH 3 ) z ; -OH; and -O(C 1-3 alkyl) (z is 0, 1 or 2; d is 1, 2 or 3; C 1-3 alkyl is methyl, ethyl, propyl or isopropyl) and is selected from the group consisting of. In one embodiment, when R 9 substitutes a hydrogen atom bonded to the ring carbon atom of ring A, each is independently methyl; ethyl; isopropyl; cyclopropyl; -(CH 2 ) d -NH 2-z (CH 3 ) z ; -(CH 2 ) d-O(CH 3 ); -CF 3 ; -CH 2 CF 3 ; -CH 2 CHF 2 ; -CH 2 CH 2 F; -NH 2 ; -NH(C 1-3 alkyl); -N(C 1-3 alkyl) 2 ; halogen (especially, -F, -Cl, -Br); -C(=O)CH 3 ; -C(=O)CH 2 NH 2-z (CH 3 ) z ; -C(=O)NH 2-z (C 1-3 alkyl) z ; -S(O) 2 (C 1-3 alkyl); -S(O) 2 (CH 2 ) d NH 2-z (CH 3 ) z ; -OH; and -O(C 1-3 alkyl) (z is 0, 1 or 2; d is 1, 2 or 3; C 1-3 alkyl is methyl, ethyl, propyl or isopropyl) are selected from the group consisting of. In one embodiment, when R 9 substitutes a hydrogen atom bonded to a ring carbon atom of ring A, each is independently methyl; ethyl; isopropyl; cyclopropyl; -(CH 2 ) d -NH 2-z (CH 3 ) z ; -(CH 2 ) d -O(CH 3 ); -CF 3 ; -CH 2 CF 3 ; -CH 2 CHF 2 ; -CH 2 CH 2 F; halogen (especially, -F, -Cl, -Br); -C(=O)CH 3 ; -C(=O)CH2 NH 2-z (CH 3 ) z ;-C(=O)NH 2-z (C 1-3 alkyl) z ;-S(O) 2 (C 1-3 alkyl);-S(O) 2 (CH 2 ) d NH 2-z (CH 3 ) z ;-OH;and -O(C 1-3 alkyl)(z is 0, 1 or 2; d is 1, 2 or 3; C 1-3 alkyl is methyl, ethyl, propyl or isopropyl) selected from the group consisting of. In one embodiment, the ring carbon atoms of ring A are unsubstituted or R which replaces the hydrogen atom bonded to the ring carbon atom 9 is, independently of each other, C 1-4 alkyl (especially methyl), -N(R 12 )(R 13 )(especially NH 2 ) and -N(R 14 )C(=O)R 11 (especially NHC(O)CH 3 ) selected from the group consisting of. In one embodiment, the ring carbon atoms of ring A are unsubstituted or one ring carbon atom of ring A is NH 2 or CH 3 and one R 9 or two R 3 which is CH 9 are substituted.

[0074] R 9 substitutes the hydrogen atom bonded to the ring nitrogen atom of ring A. In any of the above embodiments of the spiroquinoxaline derivative of formula (II), such R 9 is, independently of each other, C 1-12 alkyl (e.g., C 1-8 alkyl or C 1-6 alkyl), C 2-6 alkenyl, C 2-6Alkynyl, 5- or 6-membered aryl, 5- or 6-membered heteroaryl, 3- to 7-membered cycloalkyl, 3- to 7-membered heterocyclyl, -OR 11 , -N(R 12 )(R 13 ), -S(O) 1-2 R 11 , -S(O) 1-2 N(R 12 )(R 13 ), -N(R 11 )S(O) 1-2 R 11 , -NR 11 S(O) 1-2 N(R 12 )(R 13 ), -C(=X)R 11 , -C(=X)XR 11 , -N(R 14 )C(=X)R 11 and -N(R 14 )C(=X)XR 11 and may be selected from the group consisting of, wherein the C 1-12 alkyl (e.g., C 1-8 alkyl or C 1-6 alkyl), C 2-6 alkenyl, C 2-6 alkynyl, 5- or 6-membered aryl, 5- or 6-membered heteroaryl, 3- to 7-membered cycloalkyl and 3- to 7-membered heterocyclyl groups are each optionally substituted with one or more (e.g., 1 to the maximum number of hydrogen atoms bonded to the C 1-12 alkyl (e.g., C 1-8 alkyl or C 1-6 alkyl), C 2-6 alkenyl, C 2-6 alkynyl, 5- or 6-membered aryl, 5- or 6-membered heteroaryl, 3- to 7-membered cycloalkyl or 3- to 7-membered heterocyclyl group, e.g., up to 1, 2, 3, 4, 5, 6, 7, 8, 9 or 10, e.g., between 1 and 5, 1 and 4 or 1 and 3, or 1 or 2) independently selected R 30 groups. In any of the above embodiments of the spiroquinoxaline derivative of formula (II) where R 9 replaces the hydrogen atom bonded to the ring nitrogen atom of ring A, such R 9 are each independently C 1-12Alkyl (e.g., C 1-8 alkyl, C 1-6 alkyl or C 1-4 alkyl), C 2-4 alkenyl, C 2-4 alkynyl, 6-membered aryl, 5- or 6-membered heteroaryl, 3-, 5-, 6- or 7-membered cycloalkyl, 3-, 5-, 6- or 7-membered heterocyclyl, -OR 11 , -N(R 12 )(R 13 ), -S(O) 1-2 R 11 , -S(O) 1-2 N(R 12 )(R 13 ), -N(R 11 )S(O) 1-2 R 11 , -NR 11 S(O) 1-2 N(R 12 )(R 13 ), -C(=O)R 11 , -C(=O)OR 11 , -C(=O)SR 11 , -C(=O)N(R 14 )(R 11 ), -C(=S)OR 11 , -N(R 14 )C(=O)R 11 , -N(R 14 )C(=O)N(R 14 )(R 11 ) and -N(R 14 )C(=N(R 14 ))N(R 14 )(R 11 ), and may be selected from the group consisting of, wherein the C 1-12 alkyl (e.g., C 1-8 alkyl, C 1-6 alkyl or C 1-4 alkyl), C 2-4 alkenyl, C 2-4 alkynyl, 6-membered aryl, 5- or 6-membered heteroaryl, 3-, 5-, 6- or 7-membered cycloalkyl and 3-, 5-, 6- or 7-membered heterocyclyl groups are each optionally substituted with one, two or three independently selected R 30 . In one embodiment, R 9When substituting the hydrogen atom bonded to the ring nitrogen atom of ring A, each independently, C 1-12 alkyl (e.g., C 1-8 alkyl, C 1-6 alkyl or C 1-4 alkyl); -OH, -O(C 1-3 alkyl) and -NH 2-z (CH 3 ) z substituted with one substituent selected from the group consisting of C 1-12 alkyl (e.g., C 1-8 alkyl, C 1-6 alkyl or C 1-4 alkyl); -CF 3 , -CH 2 CF 3 , -CH 2 CHF 2 or -CH 2 CH 2 F, C 1-4 alkyl substituted with one, two or three halogens (preferably F); cyclopropyl; 4-morpholinyl; homomorpholinyl; 4-piperidinyl; homopiperidinyl; 4-piperazinyl; homopiperazinyl; N-methyl-piperazin-4-yl; N-methyl-homopiperazinyl; -OH; -O(C 1-3 alkyl); -NH 2 ; -NH(C 1-3 alkyl); -N(C 1-3 alkyl) 2 ; -S(C 1-3 alkyl); -S(O) 2 (optionally -NH 2-z (CH 3 ) z substituted C 1-3 alkyl); -S(O) 2 NH 2-z (C 1-3 alkyl) z ; -NHS(O) 2 (C 1-3 alkyl); -C(=O)(optionally -NH 2-z (CH 3 ) z substituted C 1-3 alkyl); -C(=O)OH; -C(=O)O(C1-3 alkyl); -C(=O)NH 2-z (C 1-3 alkyl) z ; -NHC(=O)(C 1-3 alkyl); -NHC(=NH)NH z-2 (C 1-3 alkyl) z ; and -N(C 1-3 alkyl)C(=NH)NH 2-z (C 1-3 alkyl) z (z is 0, 1, or 2; C 1-3 alkyl is methyl, ethyl, propyl, or isopropyl) and is selected from the group consisting of. In one embodiment, R 9 When substituting the hydrogen atom bonded to the ring nitrogen atom of ring A, each independently, methyl; ethyl; isopropyl; n-octyl; n-dodecyl; cyclopropyl; -(CH 2 ) d -NH 2-z (CH 3 ) z ; -(CH 2 ) d -O(CH 3 ); -CH 2 CF 3 ; -CH 2 CHF 2 ; -CH 2 CH 2 F; -C(=O)CH 3 ; -C(=O)CH 2 NH 2-z (CH 3 ) z ; -C(=O)NH 2-z (C 1-3 alkyl) z ; -S(O) 2 (C 1-3 alkyl); -S(O) 2 (CH 2 ) d NH 2-z (CH 3 ) z ; -OH; and -O(C 1-3 alkyl) (z is 0, 1, or 2; d is 1, 2, or 3; C 1-3Alkyl is selected from the group consisting of methyl, ethyl, propyl or isopropyl. In one embodiment, R 9 When substituting the hydrogen atom bonded to the ring nitrogen atom of ring A, each is independently methyl; ethyl; isopropyl; cyclopropyl; -(CH 2 ) d -NH 2-z (CH 3 ) z ; -(CH 2 ) d -O(CH 3 ); -CH 2 CF 3 ; -CH 2 CHF 2 ; -CH 2 CH 2 F; -C(=O)CH 3 ; -C(=O)CH 2 NH 2-z (CH 3 ) z ; -C(=O)NH 2-z (C 1-3 alkyl) z ; -S(O) 2 (C 1-3 alkyl); -S(O) 2 (CH 2 ) d NH 2-z (CH 3 ) z ; -OH; and -O(C 1-3 alkyl) (z is 0, 1 or 2; d is 1, 2 or 3; C 1-3 alkyl is methyl, ethyl, propyl or isopropyl) is selected from the group consisting of. In one embodiment, the ring nitrogen atom of ring A is unsubstituted or R which substitutes the hydrogen atom bonded to the ring nitrogen atom 9 is each independently C 1-12 alkyl (especially methyl, n-octyl or n-dodecyl) and -C(=O)R 11 (especially -C(=O)CH 3 or -C(=O)(CH 2 ) 6 CH 3) selected from the group consisting of. In one embodiment, the ring nitrogen atom of ring A is unsubstituted or is one R which is methyl 9 substituted.

[0075] R 9 is bonded to the ring sulfur atom of ring A. In any of the above embodiments of the spiroquinoxaline derivative of formula (II), such R 9 may each independently be selected from the group consisting of C 1-6 alkyl, C 2-6 alkenyl, C 2-6 alkynyl, 5- or 6-membered aryl, 5- or 6-membered heteroaryl, 3- to 7-membered cycloalkyl, 3- to 7-membered heterocyclyl, -OR 11 and =O, where the C 1-6 alkyl, C 2-6 alkenyl, C 2-6 alkynyl, 5- or 6-membered aryl, 5- or 6-membered heteroaryl, 3- to 7-membered cycloalkyl and 3- to 7-membered heterocyclyl groups may each optionally be substituted with one or more (e.g., 1 to the maximum number of hydrogen atoms bonded to the C 1-6 alkyl, C 2-6 alkenyl, C 2-6 alkynyl, 5- or 6-membered aryl, 5- or 6-membered heteroaryl, 3- to 7-membered cycloalkyl or 3- to 7-membered heterocyclyl group, e.g., 1, 2, 3, 4, 5, 6, 7, 8, 9 or 10, e.g., between 1 and 5, 1 and 4 or 1 and 3, or 1 or 2) independently selected R 30 substituents. R 9 is bonded to the ring sulfur atom of ring A. In any of the above embodiments of the spiroquinoxaline derivative of formula (II), such R 9 may each independently be selected from the group consisting of C 1-4 alkyl, C 2-4 alkenyl, C 2-4 alkynyl, 6-membered aryl, 5- or 6-membered heteroaryl, 3, 5, 6 or 7-membered cycloalkyl, 3, 5, 6 or 7-membered heterocyclyl, -OR 11 and =O, where the C 1-4 alkyl, C 2-4 alkenyl, C2-4 The alkynyl, 6-membered aryl, 5- or 6-membered heteroaryl, 3-, 5-, 6- or 7-membered cycloalkyl and 3-, 5-, 6- or 7-membered heterocyclyl groups are each optionally substituted with one, two or three independently selected R 30 groups. In one embodiment, when R 9 is attached to the ring sulfur atom of Ring A, each is independently methyl, ethyl, C 3 alkyl, C 4 alkyl, -OR 11’ and =O (wherein R 11’ is selected from the group consisting of -H, C 1-6 alkyl, C 2-6 alkenyl, C 2-6 alkynyl, 3- to 7-membered cycloalkyl, 5- or 6-membered aryl (e.g., phenyl), 5- or 6-membered heteroaryl and 3- to 7-membered heterocyclyl), and wherein the methyl, ethyl, C 3 alkyl, C 4 alkyl, C 1-6 alkyl, C 2-6 alkenyl, C 2-6 alkynyl, 3- to 7-membered cycloalkyl, 5- or 6-membered aryl, 5- or 6-membered heteroaryl and 3- to 7-membered heterocyclyl groups are each optionally substituted with one, two or three independently selected R 30’ groups (wherein R 30’ is a first, second or third level substituent as previously specified (in particular, one of the exemplary first, second or third level substituents as previously specified), and in each case is phenyl, furanyl, pyrrolyl, thienyl, imidazolyl, oxazolyl, isoxazolyl, thiazolyl, pyridyl, pyrazinyl, pyrimidinyl, pyridazinyl, the partially and fully hydrogenated forms of the foregoing groups, morpholino, C 1-3 alkyl, halogen, -CF 3 , -OH, -OCH 3 , -SCH 3 , -NH 2-z (CH 3 ) z , -C(=O)OH and -C(=O)OCH 3(z may be selected from the group consisting of 0, 1, or 2). In one embodiment, R 9 , when bonded to the ring sulfur atom of ring A, are each independently methyl; ethyl; isopropyl; benzyl; -OH; =O; and -O(C 1-3 alkyl)(C 1-3 alkyl is methyl, ethyl, propyl, or isopropyl) and are selected from the group consisting of. In one embodiment, the ring sulfur atom of ring A is unsubstituted or is substituted with two =O groups. In one embodiment, the ring sulfur atom of ring A is unsubstituted or ring A contains one sulfur atom substituted with two =O groups (i.e., ring A contains the group -S(=O) 2 -).

[0076] In one embodiment, the spiroquinoxaline derivative has the following general formula (III): [Chemical formula] [wherein, R 1 ~R 5 , ring A, E, and G are as defined above (in particular, for formulas (I) and (II)) or are synonymous with the following, L is C 1-6 alkylene, C 2-6 alkenylene, C 2-6 alkynylene, -(CH 2 ) a -cyclopropylene-(CH 2 ) b -(wherein a and b are each independently selected from integers between 0 and 3) and -(CH 2 ) m -[Y-(CH 2 ) n o -(wherein m is 1, 2, or 3, n is 0, 1, or 2, o is 1, 2, or 3, when n is 0, o is 1, and Y is independently O, S, and -N(R 7’ )-(R 7’ is -H, C 1-6 alkyl, C 2-6 alkenyl, C​2-6 alkynyl, 3- to 7-membered cycloalkyl, 5- or 6-membered aryl, 5- or 6-membered heteroaryl, 3- to 7-membered heterocyclyl, -OR 11 and -NHR 20 selected from the group consisting of) selected from the group consisting of), wherein the C 1-6 alkylene, C 2-6 alkenylene, C 2-6 alkynylene, 1,1-cyclopropylene, -(CH 2 ) m -, -(CH 2 ) n -, C 1-6 alkyl, C 2-6 alkenyl, C 2-6 alkynyl, 3- to 7-membered cycloalkyl, 5- or 6-membered aryl, 5- or 6-membered heteroaryl and 3- to 7-membered heterocyclyl groups each optionally have one or more (e.g., 1 to the C 1-6 alkylene, C 2-6 alkenylene, C 2-6 alkynylene, 1,1-cyclopropylene, -(CH 2 ) m -, -(CH 2 ) n -, C 1-6 alkyl, C 2-6 alkenyl, C 2-6 alkynyl, 3- to 7-membered cycloalkyl, 5- or 6-membered aryl, 5- or 6-membered heteroaryl or 3- to 7-membered heterocyclyl group, the maximum number of hydrogen atoms bonded, e.g., 1, 2, 3, 4, 5, 6, 7, 8, 9 or 10, e.g., between 1 to 5, 1 to 4 or 1 to 3, or 1 or 2) of independently selected R 30 substituted with] has. In one embodiment of the spiroquinoxaline derivative of formula (III), R 1 ~R 5 , ring A, E and G are as defined above (in particular, for formulas (I) and (II)) or synonymous with the following, and L is C 1-4 alkylene, C 2-4 alkenylene, C 2-4 alkynylene, -(CH 2 ) a -1,1-cyclopropylene-(CH2 ) b -(wherein a and b are each independently selected from 0, 1 and 2) and -(CH 2 ) m -[Y-(CH 2 ) n o -(wherein m is 1, 2 or 3, n is 0, 1 or 2, o is 1, 2 or 3, when n is 0, o is 1, and Y is independently selected from the group consisting of O, S and -N(R 7’ )-(R 7’ is selected from the group consisting of -H, C 1-3 alkyl, 3, 5, 6 or 7-membered cycloalkyl, 6-membered aryl, 5 or 6-membered heteroaryl, 3, 5, 6 or 7-membered heterocyclyl, -O(C 1-3 alkyl) and -NHR 20 ). Here, the C 1-4 alkylene, C 2-4 alkenylene, C 2-4 alkynylene, 1,1-cyclopropylene, -(CH 2 ) m -, -(CH 2 ) n -, C 1-3 alkyl, 3, 5, 6 or 7-membered cycloalkyl, 6-membered aryl, 5 or 6-membered heteroaryl and 3, 5, 6 or 7-membered heterocyclyl groups are each optionally substituted with 1, 2 or 3 independently selected R 30 . In one embodiment of the spiroquinoxaline derivative of formula (III), R 1 ~R 5 , rings A, E and G are as defined above (in particular for formulas (I) and (II)) or synonymous with the following, and L is C 1-3 alkylene, -(CH 2 ) a -1,1-cyclopropylene-(CH 2 ) b -(wherein a and b are each independently selected from 0 and 1) and -(CH 2 ) m -[Y-(CH 2 ) n o ​​-(wherein, m is 1 or 2, n is 0, 1 or 2, o is 1 or 2, when n is 0, o is 1, and Y is O) is selected from the group consisting of, here, the C 1-3 alkylene, 1,1 - cyclopropylene, -(CH 2 ) m - and -(CH 2 ) n - groups are each optionally substituted with one, two or three independently selected R 30 . In one embodiment of the spiroquinoxaline derivative of formula (III), R 1 ~R 5 , ring A, E and G are as defined above (especially for formulas (I) and (II)) or have the same meaning as below, and L is methylene; 1,1 - ethylene; 1,2 - ethylene (optionally substituted at the 2 - position with one R 30 (for example, phenyl)); trimethylene (-(CH 2 ) 3 -); 2,2 - propylene (-C(CH 3 ) 2 -); 2,4 - butanediyl; -1,1 - cyclopropylene -; -(CH 2 )-1,1 - cyclopropylene; -1,1 - cyclopropylene-(CH 2 )-; -(CH 2 )-1,1 - cyclopropylene-(CH 2 )-; -CH 2 O-; -(CH 2 ) 2 O-; and -(CH 2 ) 3 O- (for example, methylene; 1,1 - ethylene; 1,2 - ethylene; trimethylene (-(CH 2 ) 3 -); 2,2 - propylene (-C(CH 3 ) 2 -); 1,1 - cyclopropylene; and -(CH 2 ) 2 O-, especially methylene) is selected from the group consisting of. In one embodiment of the spiroquinoxaline derivative of formula (III), R 1 ~R 5, rings A, E, and G are synonymous with the above (especially for formulas (I) and (II)) or the following, and L is methylene; 1,1-ethylene; 1,2-ethylene; trimethylene (-(CH 2 ) 3 -); 2,2-propylene (-(C(CH 3 ) 2 -); -1,1-cyclopropylene-; -(CH 2 )-1,1-cyclopropylene; -1,1-cyclopropylene-(CH 2 )-; -(CH 2 )-1,1-cyclopropylene-(CH 2 )-; -CH 2 O-; -(CH 2 ) 2 O-; and -(CH 2 ) 3 O- (for example, methylene; 1,1-ethylene; 1,2-ethylene; trimethylene (-(CH 2 ) 3 -); 2,2-propylene (-(C(CH 3 ) 2 -); 1,1-cyclopropylene; and -(CH 2 ) 2 O-, especially methylene) and is selected from the group consisting of. In one embodiment of the spiroquinoxaline derivative of formula (III), R 1 ~R 5 , rings A, E, and G are synonymous with the above (especially for formulas (I) and (II)) or the following, and L is, in each case, C 30 alkylene, C 1 alkylene (especially 1,2-ethylene or 1,1-ethylene), C 2 alkylene (especially trimethylene), and C 3 alkylene (especially tetramethylene or 2,4-butanediyl), each of which is substituted with one R 4 and is selected from the group consisting of. In one embodiment of the spiroquinoxaline derivative of formula (III), R 1 ~R 5, rings A, E, and G are synonymous with the above (in particular, for formulas (I) and (II)) or the following, and L is selected from the group consisting of methylene, 1,1-ethylene, 1,2-ethylene, trimethylene, tetramethylene, 2,4-butanediyl, and 2-phenyl-1,2-ethylene (-CH 2 -CH(C 6 H 5 ). In one embodiment of the spiroquinoxaline derivative of formula (III), R 1 ~R 5 , rings A, E, and G are synonymous with the above (in particular, for formulas (I) and (II)) or the following, and L is selected from the group consisting of methylene and 2-phenyl-1,2-ethylene (-CH 2 -CH(C 6 H 5 ).

[0077] In one embodiment, the spiroquinoxaline derivative has the following general formula (IV):

Chemical formula

[0078] In one embodiment, the spiroquinoxaline derivative has the following general formula (V): [Chemical formula] [wherein, R 1 , ring A, E, L and G are as defined above (especially for formulas (I), (II), (III) and (IV)) or have the same meaning as below, R 2 , R 3 , R 4 and R 5is H for each] has. In one embodiment of the spiroquinoxaline derivative of formula (V), R 1 , ring A, E, L and G are as defined above (in particular, for formulas (I), (II), (III) and (IV)) or have the same meaning as below, and R 2 , R 3 , R 4 and R 5 at least one of which is different from H. For example, in one embodiment, R 2 is different from H, and R 3 , R 4 and R 5 are each H; or, R 3 is different from H, and R 2 , R 4 and R 5 are each H; or, R 4 is different from H, and R 2 , R 3 and R 5 are each H; or, R 5 is different from H, and R 2 , R 3 and R 4 are each H; or, R 2 and R 3 both are different from H, and R 4 and R 5 both are H; or, R 2 and R 4 both are different from H, and R 3 and R 5 both are H; or, R 2 and R 5 both are different from H (preferably, in this embodiment, R 2 and R 5 are the same), R 3 and R 4 both are H; or, R 3 and R 4 both are different from H (preferably, in this embodiment, R 3 and R 4 are the same), R 2 and R 5 both are H; or, R 2 , R3 and R 4 is, each different from H, R 5 is H; or, R 2 , R 3 and R 5 is, each different from H, R 4 is H; or, R 2 , R 4 and R 5 is, each different from H, R 3 is H; or, R 3 , R 4 and R 5 is, each different from H, R 2 is H; or, R 2 , R 3 , R 4 and R 5 is, each different from H. In any of the above embodiments, R 2 and R 5 are the same, and / or, R 3 and R 4 are preferably the same.

[0079] In any of the above embodiments (particularly, for formulas (I), (II), (III), (IV) and (V)), R 2 ~R 5 is, when not forming a ring together with another R 2 ~R 5 , each independently, -H, C 1-6 alkyl, C 2-6 alkenyl, C 2-6 alkynyl, 5- or 6-membered aryl, 5- or 6-membered heteroaryl, 3- to 7-membered cycloalkyl, 3- to 7-membered heterocyclyl, halogen, -CN, -OR 11 , -N(R 12 )(R 13 ), -S(O) 0-2 R 11 , -S(O) 1-2 N(R 12 )(R 13 ), -N(R 11 )S(O) 1-2 R 11 , -NR 11 S(O) 1-2 N(R12 )(R 13 )、 -C(=X)R 11 、 -C(=X)XR 11 、 -XC(=X)R 11 and -XC(=X)XR 11 selected from the group consisting of, wherein the C 1-6 alkyl, C 2-6 alkenyl, C 2-6 alkynyl, 5- or 6-membered aryl, 5- or 6-membered heteroaryl, 3- to 7-membered cycloalkyl and 3- to 7-membered heterocyclyl group are each optionally, one or more (e.g., 1 to the C 1-6 alkyl, C 2-6 alkenyl, C 2-6 alkynyl, 5- or 6-membered aryl, 5- or 6-membered heteroaryl, 3- to 7-membered cycloalkyl or 3- to 7-membered heterocyclyl group, the maximum number of hydrogen atoms bonded, e.g., 1, 2, 3, 4, 5, 6, 7, 8, 9 or 10, e.g., between 1 and 5, 1 and 4 or 1 and 3, or 1 or 2) of independently selected R 30 is substituted. In one embodiment, R 2 , R 3 , R 4 and R 5 are, when not taken together with another one of R 2 ~R 5 to form a ring, each independently, -H, C 1-4 alkyl, C 2-4 alkenyl, C 2-4 alkynyl, 6-membered aryl, 5- or 6-membered heteroaryl, 3, 5, 6 or 7-membered cycloalkyl, 3, 5, 6 or 7-membered heterocyclyl, halogen, -CN, -OR 11 , -N(R 12 )(R 13 ), -S(O) 0-2 R 11 , -S(O) 1-2 N(R 12 )(R 13 ), -N(R 11 )S(O) 1-2 R 11 , -NR 11 S(O) 1-2 N(R 12 )(R 13 ), -C(=O)R11 、 -C(=O)OR 11 、 -C(=O)SR 11 、 -C(=O)N(R 14 )(R 11 )、 -C(=S)OR 11 、 -N(R 14 )C(=O)R 11 、 -OC(=O)R 11 、 -OC(=S)R 11 、 -N(R 14 )C(=O)N(R 14 )(R 11 ) and -N(R 14 )C(=N(R 14 ))N(R 14 )(R 11 ) may be selected from the group consisting of, wherein the C 1-4 alkyl, C 2-4 alkenyl, C 2-4 alkynyl, 6-membered aryl, 5- or 6-membered heteroaryl, 3-, 5-, 6- or 7-membered cycloalkyl and 3-, 5-, 6- or 7-membered heterocyclyl group may each, optionally, be substituted with 1, 2 or 3 independently selected R 30 . In one embodiment of the spiroquinoxaline derivative of formula (V), R 1 , ring A, E, L and G are as defined above (in particular for formulas (I), (II), (III) and (IV)) or as defined below, and R 2 , R 3 , R 4 and R 5 , when not taken together with another one of R 2 ~R 5 to form a ring, are each independently H; C 1-4 alkyl; -OH, -O(C 1-3 alkyl) and -NH 2-z (CH 3 ) z substituted with one substituent selected from the group consisting of; C 1-4 alkyl; -CF 3 , -CH 2 CF 3 , -CH 2 CHF 2 or -CH 2 CH 2C substituted with one, two or three halogens (preferably F) such as F 1-4 alkyl; phenyl; cyclopropyl; 5-membered heterocyclyl; 4-morpholinyl; homomorpholinyl; 4-piperidinyl; homopiperidinyl; 4-piperazinyl; homopiperazinyl; N-methyl-piperazin-4-yl; N-methyl-homopiperazinyl; halogen; -CN; -OH; -O(C 1-3 alkyl); -OCF 3 , -OCH 2 CF 3 , -OCH 2 CHF 2 or -OCH 2 CH 2 F; -O(C substituted with one, two or three halogens (preferably F) such as F 1-4 alkyl); -O-phenyl; -NH 2 -; -NH(C 1-3 alkyl); -N(C 1-3 alkyl) 2 -; -S(C 1-3 alkyl); -S(O) 2 (optionally -NH 2-z (CH 3 ) z substituted C 1-3 alkyl); -S(O) 2 NH 2-z (C 1-3 alkyl) z -; -NHS(O) 2 (C 1-3 alkyl); -C(=O)(optionally -NH 2-z (CH 3 ) z substituted C 1-3 alkyl); -C(=O)OH; -C(=O)O(C 1-3 alkyl); -C(=O)NH 2-z (C 1-3 alkyl) z -; -NHC(=O)(C 1-3 alkyl); -NHC(=NH)NH z-2 (C 1-3 alkyl) z ; and -N(C 1-3 alkyl)C(=NH)NH 2-z(C 1-3 (alkyl) z (where z is 0, 1, or 2, and C 1-3 alkyl is methyl, ethyl, propyl, or isopropyl) is selected from the group consisting of, and the phenyl, cyclopropyl, 5-membered heterocyclyl, 4-morpholinyl, homomorpholinyl, 4-piperidinyl, homopiperidinyl, 4-piperazinyl, homopiperazinyl, N-methyl-piperazin-4-yl, N-methyl-homopiperazinyl, and -O-phenyl groups are each, optionally, C 1-3 alkyl, halogen, -CF 3 , -OCF 3 , -OH, -OCH 3 , -SCH 3 , -NH 2-z (CH 3 ) z , -C(=O)OH, and -C(=O)OCH 3 (where z is 0, 1, or 2) and is independently substituted with 1, 2, or 3 substituents selected from the group consisting of. In one embodiment, R 2 , R 3 , R 4 , and R 5 are, when not taken together with another one of R 2 ~R 5 to form a ring, each independently, H; methyl; ethyl; isopropyl; phenyl; cyclopropyl; -(CH 2 ) d -NH 2-z (CH 3 ) z ; -(CH 2 ) d -O(CH 3 ); -CF 3 ; -OCF 3 ; -CH 2 CF 3 ; -CH 2 CHF 2 ; -CH 2 CH 2 F; halogen (especially, -F, -Cl, -Br); -CN; -NH 2 ; -NH(C 1-3 alkyl); -N(C 1-3 alkyl) 2 ; -C(=O)CH3 ;-C(=O)CH 2 NH 2-z (CH 3 ) z ;-C(=O)O(C 1-3 alkyl);-C(=O)NH 2-z (C 1-3 alkyl) z ;-NHC(=O)(C 1-3 alkyl);-S(O) 2 (C 1-3 alkyl);-S(O) 2 (CH 2 ) d NH 2-z (CH 3 ) z ;-OH and -O(C 1-3 alkyl) (z is 0, 1 or 2; d is 1, 2 or 3; C 1-3 alkyl is methyl, ethyl, propyl or isopropyl), and is selected from the group consisting of. In one embodiment of the spiroquinoxaline derivative of formula (V), R 1 , ring A, E, L and G are as defined above (in particular, for formulas (I), (II), (III) and (IV)) or have the same meaning as below, and R 2 , R 3 , R 4 and R 5 are each independently selected from the group consisting of -H, C 1-4 alkyl and halogen, where the C 1-4 alkyl group is optionally substituted with one, two or three independently selected R 30 (in particular, R 2 and R 5 are each -H). In one embodiment of the spiroquinoxaline derivative of formula (V), R 1 , ring A, E, L and G are as defined above (in particular, for formulas (I), (II), (III) and (IV)) or have the same meaning as below, and R 2 , R 3 , R 4 and R 5 are each independently selected from the group consisting of -H, methyl, F, Cl and CF 3 (in particular, R 2 and R 5is each -H). In one embodiment of the spiroquinoxaline derivative of formula (V), R 1 , ring A, E, L and G are as defined above (in particular, for formulas (I), (II), (III) and (IV)) or have the same meaning as below, and R 2 and R 5 are each -H, R 3 is selected from the group consisting of -H, methyl, F and Cl, and R 4 is selected from the group consisting of -H, methyl, F and Cl. In one embodiment of the spiroquinoxaline derivative of formula (V), R 1 , ring A, E, L and G are as defined above (in particular, for formulas (I), (II), (III) and (IV)) or have the same meaning as below, (i) R 2 ~R 5 are each -H; or, (ii) R 2 and R 5 are each -H, and both R 3 and R 4 are F, Cl or methyl.

[0080] (i) R 2 and R 3 , (ii) R 3 and R 4 , and / or (iii) R 4 and R 5 form a ring. In any of the above embodiments, the ring is preferably optionally substituted with one or more (e.g., 1 to the maximum number of hydrogen atoms bonded to the ring, e.g., 1, 2, 3, 4, 5, 6, 7, 8, 9 or 10, e.g., between 1 and 5, 1 and 4 or 1 and 3, or 1 or 2) independently selected R 30 and is a 3- to 7-membered ring (e.g., a ring having 5 or 6 members). The ring is aromatic, alicyclic, heteroaromatic or heterocyclic (the heteroaromatic / heterocyclic ring contains O, S and N(R 40 )(R 40 is R 11 , -OR 11 , -NH y R 20 2-y and -S(O) 1-2 R 11 (R11 , R 20 and y is selected from the group consisting of) (wherein R, R, and y are as defined above) and may contain one or two heteroatoms selected from the group consisting of). In one embodiment, (i) R 2 and R 3 , (ii) R 3 and R 4 , and / or (iii) R 4 and R 5 form a 5- or 6-membered aromatic, alicyclic, heteroaromatic, or heterocyclic ring, and the heteroaromatic / heterocyclic ring contains one or two heteroatoms selected from the group consisting of O, S, and N, and at least one heteroatom is N. In one embodiment, (i) R 2 and R 3 , (ii) R 3 and R 4 , and / or (iii) R 4 and R 5 form a ring selected from the group consisting of cyclopentadiene, furan, pyrrole, thiophene, imidazole, pyrazole, oxazole, isoxazole, thiazole, dioxole (e.g., 1,3-dioxole), benzene, pyridine, pyrazine, pyrimidine, pyridazine, dioxine (e.g., 1,4-dioxine), 1,2,3-triazine, 1,2,4-triazine, and the di- or tetrahydro derivatives of each of the foregoing. In one embodiment, (i) R 2 and R 3 , (ii) R 3 and R 4 , and / or (iii) R 4 and R 5 form a ring selected from the group consisting of cyclopentadiene, furan, pyrrole, thiophene, imidazole, pyrazole, oxazole, isoxazole, thiazole, benzene, pyridine, pyrazine, pyrimidine, pyridazine, 1,2,3-triazine, 1,2,4-triazine, and the di- or tetrahydro derivatives of each of the foregoing. In one embodiment, (i) R 2 and R 3 , (ii) R 3 and R 4, and / or (iii) R 4 and R 5 The ring formed by is cyclopentene (e.g., 2,3-dihydrocyclopentadiene), dioxole (e.g., 1,3-dioxole optionally substituted with one or two halogen atoms (e.g., F) at the 2-position), or dioxine (e.g., 2,3-dihydro-[1,4]-dioxine). In one embodiment, (i) R 2 and R 3 , (ii) R 3 and R 4 , and / or (iii) R 4 and R 5 The total number of rings formed is 0 or 1. Thus, in an embodiment where the total number of rings formed by (i) R 2 and R 3 , (ii) R 3 and R 4 , and / or (iii) R 4 and R 5 is 1, only two adjacent substituents (i.e., either (i) R 2 and R 3 , (ii) R 3 and R 4 or (iii) R 4 and R 5 ) together with the atoms to which they are attached form a ring, where the ring is as defined in any of the above embodiments, and the remainder of R 2 ~R 5 is selected from the group of specific moieties previously specified with respect to the situation where they do not form a ring together. For example, the remainder of R 2 ~R 5 that do not form a ring together is -H, C 1-6 alkyl, C 2-6 alkenyl, C 2-6 alkynyl, 5- or 6-membered aryl, 5- or 6-membered heteroaryl, 3- to 7-membered cycloalkyl, 3- to 7-membered heterocyclyl, halogen, -CN, -OR 11 , -N(R 12 )(R 13 ), -S(O) 0-2 R 11 , -S(O)1-2 N(R 12 )(R 13 )、 -N(R 11 )S(O) 1-2 R 11 、 -NR 11 S(O) 1-2 N(R 12 )(R 13 )、 -C(=X)R 11 、 -C(=X)XR 11 、 -XC(=X)R 11 and -XC(=X)XR 11 may be selected from, where the C 1-6 alkyl, C 2-6 alkenyl, C 2-6 alkynyl, 5- or 6-membered aryl, 5- or 6-membered heteroaryl, 3- to 7-membered cycloalkyl, and 3- to 7-membered heterocyclyl group each, optionally, has one or more (e.g., 1 to the maximum number of hydrogen atoms bonded to the C 1-6 alkyl, C 2-6 alkenyl, C 2-6 alkynyl, 5- or 6-membered aryl, 5- or 6-membered heteroaryl, 3- to 7-membered cycloalkyl, or 3- to 7-membered heterocyclyl group, e.g., 1, 2, 3, 4, 5, 6, 7, 8, 9, or 10, e.g., between 1 and 5, 1 and 4, or 1 and 3, or 1 or 2) independently selected R 30 substituents. In another embodiment, R 2 ~R 5 do not form a ring together.

[0081] In any of the above embodiments, R 2 and R 5 may be the same, and / or R 3 and R 4 may be the same.

[0082] In one embodiment of the spiroquinoxaline derivative of formula (V), R 1 , ring A, E, L, and G are as defined above (particularly for formulas (I), (II), (III), and (IV)) or have the same meaning as below, R 2 , R 3 , R 4 and R5 is, independently, -H, C 1-4 selected from the group consisting of alkyl and halogen, where the C 1-4 alkyl is optionally substituted with one, two or three independently selected R 30 s (in particular, R 2 and R 5 are each -H), or R 3 and R 4 together with the atom to which they are attached may form a 5- or 6-membered ring optionally substituted with one or two independently selected R 30 s. In one embodiment of the spiroquinoxaline derivative of formula (V), R 1 , ring A, E, L and G are as defined above (in particular, for formulas (I), (II), (III) and (IV)) or as defined below, and R 2 , R 3 , R 4 and R 5 are independently selected from the group consisting of -H, methyl, F, Cl and CF 3 s (in particular, R 2 and R 5 are each -H), or R 3 and R 4 together with the atom to which they are attached may form a dioxol or dioxin ring optionally substituted with one or two independently selected halogens (in particular F). In one embodiment of the spiroquinoxaline derivative of formula (V), R 1 , ring A, E, L and G are as defined above (in particular, for formulas (I), (II), (III) and (IV)) or as defined below, R 2 and R 5 are each -H; R 3 is selected from the group consisting of -H, methyl, F and Cl; R 4 is selected from the group consisting of -H, methyl, F and Cl; or R 3 and R 4may, together with the atoms to which they are attached, form a dioxole (especially 1,3-dioxole) or dioxin (especially 2,3-dihydro-[1,4]-dioxin) ring, and the dioxole ring may optionally be substituted with two Fs. In one embodiment of the spiroquinoxaline derivative of formula (V), R 1 ring A, E, L and G are as defined above (especially for formulas (I), (II), (III) and (IV)) or synonymous with the following, (i) R 2 ~R 5 are each -H; (ii) R 2 and R 5 are each -H, and both R 3 and R 4 are F, Cl or methyl; or (iii) R 2 and R 5 are each -H, and R 3 and R 4 together with the atoms to which they are attached form a 2,2-difluoro-1,3-dioxole ring or a 2,3-dihydro-[1,4]-dioxin ring.

[0083] In any of the above embodiments (especially for formulas (I), (II), (III), (IV) and (V)), R 30 may in each case be a typical first, second or third level substituent specified above, and independently, C 1-4 alkyl, C 2-4 alkenyl, C 2-4 alkynyl, 5- or 6-membered aryl, 5- or 6-membered heteroaryl, 5- or 6-membered cycloalkyl, 5-, 6- or 7-membered heterocyclyl, halogen, -CF 3 , -CN, azide, -NO 2 , -OH, -O(C 1-3 alkyl), -S(C 1-3 alkyl), -NH 2 , -NH(C 1-3 alkyl), -N(C 1-3 alkyl) 2 , -NHS(O) 2 (C 1-3 alkyl), -S(O)2 NH 2-z (C 1-3 alkyl) z 、 -C(=O)OH、 -C(=O)O(C 1-3 alkyl)、 -C(=O)NH 2-z (C 1-3 alkyl) z 、 -NHC(=O)(C 1-3 alkyl)、 -NHC(=NH)NH z-2 (C 1-3 alkyl) z and -N(C 1-3 alkyl)C(=NH)NH 2-z (C 1-3 alkyl) z (z is 0, 1 or 2, and C 1-3 alkyl is methyl, ethyl, propyl or isopropyl) selected from the group consisting of (for example, 4 - morpholinyl, homomorpholinyl, 4 - piperidinyl, homopiperidinyl (i.e., azepanyl, especially 4 - azepanyl), 4 - piperazinyl, homopiperazinyl (i.e., diazepanyl, especially 2,4 - diazepanyl), N - methyl - piperazin - 4 - yl, N - methyl - homopiperidinyl, -CH 2 CH 2 OCH 3 、 -OCH 2 CH 2 OCH 3 、 -CH 2 CH 2 NH 2-z (CH 3 ) z 、 -OCH 2 CH 2 NH 2-z (CH3) z 、 -CF 3 、 -OCF 3 ) may be. Or, R 30 is phenyl, furanyl, pyrrolyl, thienyl, imidazolyl, oxazolyl, isoxazolyl, thiazolyl, pyridyl, pyrazinyl, pyrimidinyl, pyridazinyl, the partially and fully hydrogenated forms of the above - mentioned groups, morpholino, C 1-3 alkyl, halogen, -CF 3 、 -OH、 -OCH 3 、 -OCF3 , -SCH 3 , -NH 2-z (CH 3 ) z , -C(=O)OH and -C(=O)OCH 3 (z is 0, 1, or 2) and may be selected from the group consisting of.

[0084] In one embodiment, the spiroquinoxaline derivative has the following general formula (N-I):

Chemical formula

[0085] In one embodiment, the spiroquinoxaline derivative has the following general formula (N-II):

Chemical formula

[0086] In any of the above embodiments of the spiroquinoxaline derivative of formula (N-II), ring A may be unsubstituted.

[0087] When ring A has one or more (for example, 1 to the maximum number of hydrogen atoms bonded to ring A, for example, up to 1, 2, 3, 4, 5, 6, 7, 8, 9 or 10, for example, between 1 and 5, 1 and 4 or 1 and 3, or 1 or 2) independently selected R 9 In any of the above embodiments of the spiroquinoxaline derivative of formula (N-II) which is replaced by, (i) only one or more (preferably 1, 2 or 3) ring nitrogen atoms of ring A are independently selected R 9 which is replaced by; or (ii) only one or more (preferably 1, 2 or 3) ring carbon atoms of ring A are independently selected R 9is replaced; (iii) one or more (preferably one, two or three) ring nitrogen atoms and one or more (preferably one, two or three) ring carbon atoms of ring A (for example, one or two ring nitrogen atoms and one or two ring carbon atoms) are each independently selected from R 9 is replaced, or any of the above. For example, when ring A contains one ring nitrogen atom, ring A is (i) at the ring nitrogen atom (preferably, when ring A is a 4- or 5-membered ring, it is at the 3-position, when ring A is a 6- or 7-membered ring, it is at the 3- or 4-position (preferably the 4-position), and when ring A is an 8-membered ring, it is at the 3, 4 or 5-position (preferably the 4 or 5-position)) only R 9 is; (ii) only at one or two ring carbon atoms of ring A, each with one or two independently selected R 9 is; or (iii) at the ring nitrogen atom (preferably, when ring A is a 4- or 5-membered ring, it is at the 3-position, when ring A is a 6- or 7-membered ring, it is at the 3- or 4-position (preferably the 4-position), and when ring A is an 8-membered ring, it is at the 3, 4 or 5-position (preferably the 4 or 5-position)) R 9 is, and at one or two ring carbon atoms of ring A, each with one or two independently selected R 9 may be substituted.

[0088] R 9 In any of the above embodiments of the spiroquinoxaline derivative of formula (N-II) in which R replaces a hydrogen atom bonded to a ring carbon atom of ring A, such R 9 is each independently C 1-6 alkyl, C 2-6 alkenyl, C 2-6 alkynyl, 5- or 6-membered aryl, 5- or 6-membered heteroaryl, 3- to 7-membered cycloalkyl, 3- to 7-membered heterocyclyl, halogen, -CN, -OR 11 , -N(R 12 )(R 13 ), -S(O) 0-2 R 11 , -S(O) 1-2 N(R 12 )(R 13 ), -N(R 11 )S(O) 1-2 R11 , -NR 11 S(O) 1-2 N(R 12 )(R 13 ), -C(=X)R 11 , -C(=X)XR 11 , -XC(=X)R 11 and -XC(=X)XR 11 may be selected from the group consisting of, wherein said C 1-6 alkyl, C 2-6 alkenyl, C 2-6 alkynyl, 5- or 6-membered aryl, 5- or 6-membered heteroaryl, 3- to 7-membered cycloalkyl and 3- to 7-membered heterocyclyl group may each optionally be substituted with one or more (e.g., 1 to the maximum number of hydrogen atoms bonded to said C 1-6 alkyl, C 2-6 alkenyl, C 2-6 alkynyl, 5- or 6-membered aryl, 5- or 6-membered heteroaryl, 3- to 7-membered cycloalkyl or 3- to 7-membered heterocyclyl group, e.g., 1, 2, 3, 4, 5, 6, 7, 8, 9 or 10, e.g., between 1 to 5, 1 to 4 or 1 to 3, or 1 or 2) independently selected R 30 and / or any two R 9 bonded to the same carbon atom of ring A may together form =X. In any of the above embodiments of the spiroquinoxaline derivative of formula (N-II) where R 9 replaces a hydrogen atom bonded to a ring carbon atom of ring A, such R 9 is each independently C 1-4 alkyl, C 2-4 alkenyl, C 2-4 alkynyl, 6-membered aryl, 5- or 6-membered heteroaryl, 3, 5, 6 or 7-membered cycloalkyl, 3, 5, 6 or 7-membered heterocyclyl, halogen, -CN, -OR 11 , -N(R 12 )(R 13 ), -S(O) 0-2 R 11 , -S(O) 1-2 N(R 12 )(R 13 ), -N(R 11 )S(O) 1-2R 11 , -NR 11 S(O) 1-2 N(R 12 )(R 13 ), -C(=O)R 11 , -C(=O)OR 11 , -C(=O)SR 11 , -C(=O)N(R 14 )(R 11 ), -C(=S)OR 11 , -N(R 14 )C(=O)R 11 , -OC(=O)R 11 , -OC(=S)R 11 , -N(R 14 )C(=O)N(R 14 )(R 11 ) and -N(R 14 )C(=N(R 14 ))N(R 14 )(R 11 ), wherein the C 1-4 Alkyl, C 2-4 Alkenyl, C 2-4 The alkynyl, 6-membered aryl, 5- or 6-membered heteroaryl, 3-, 5-, 6- or 7-membered cycloalkyl, and 3-, 5-, 6- or 7-membered heterocyclyl groups each optionally contain one, two or three independently selected R 30 and / or any two R bonded to the same carbon atom of ring A 9 may be taken together to form =O or =S. In one embodiment, R 9 When each of the groups replaces a hydrogen atom bonded to a ring carbon atom of ring A, each of the groups independently represents C 1-4 Alkyl; -OH, -O(C 1-3 alkyl), -NH 2-z (CH 3 ) z , morpholinyl (e.g., 4-morpholinyl), piperazinyl (e.g., 1-piperazinyl), and N-methylpiperazinyl (e.g., 4-methylpiperazin-1-yl), 1-4 Alkyl;-CF 3 , -CH 2CF 3 、 -CH 2 CHF 2 or -CH 2 CH 2 alkyl substituted with one, two or three halogens (preferably F) such as F; -OCF 1-4 、 -OCH 3 、 -OCH 2 CF 3 、 -OCH 2 CHF 2 or -OCH 2 CH 2 F; -O(alkyl substituted with one, two or three halogens (preferably F)) such as F; cyclopropyl; 4 - morpholinyl; homomorpholinyl; 4 - piperidinyl; homopiperidinyl; 4 - piperazinyl; homopiperazinyl; 4 - methyl - piperazin - 1 - yl; N - methyl - homopiperazinyl; halogen; -CN; -OH; =O; -O(optionally -NH 1-4 (CH 2-z (CH 3 ) z substituted alkyl); -NH 1-3 ; -NH(alkyl); -N(alkyl) 2 ; -NH(alkyl); -N(alkyl) 1-3 alkyl); -N(alkyl) 1-3 alkyl) 2 ; -S(alkyl); -S(O) 1-3 (optionally -NH 2 (CH 2-z (CH 3 ) z substituted alkyl); -S(O) 1-3 -NH 2 (alkyl) 2-z (alkyl) 1-3 alkyl); -NHS(O) z (optionally -NH 2 (CH 2-z (CH 3 ) z substituted alkyl); -C(=O)(optionally -NH 1-3 (CH 2-z (CH 3 ) z substituted alkyl); -C(=O)OH; -C(=O)O(alkyl); -C(=O)O(C 1-3 alkyl); -C(=O)O(alkyl); -C(=O)O(C 1-3-C(=O)NH(alkyl); 2-z (C 1-3 (alkyl)) z ;-NHC(=O)-(optionally -NH 2-z (CH 3 ) z substituted C 1-3 (alkyl); -NHC(=O)NH 2-z (CH 3 ) z ;-NHC(=NH)NH z-2 (C 1-3 (alkyl)) z ; and -N(C 1-3 (alkyl))C(=NH)NH 2-z (C 1-3 (alkyl)) z (z is 0, 1, or 2, and C 1-3 (alkyl) is methyl, ethyl, propyl, or isopropyl) is selected from the group consisting of. In one embodiment, when R 9 substitutes the hydrogen atom bonded to the ring carbon atom of ring A, each is independently methyl; ethyl; isopropyl; tert - butyl; cyclopropyl; -(CH 2 ) d -NH 2-z (CH 3 ) z ;-O(CH 2 ) d -NH 2-z (CH 3 ) z ;-(CH 2 ) d -O(CH 3 );-CF 3 ;-CH 2 CF 3 ;-CH 2 CHF 2 ;-CH 2 CH 2 F;-(CH 2 ) d -(4 - morpholinyl);-(CH 2 ) d -(1 - piperazinyl);-(CH 2 ) d-(4-Methylpiperazin-1-yl); 4-morpholinyl; 4-piperazinyl; 4-methyl-piperazin-1-yl; halogen (especially, -F, -Cl, -Br); -NHC(=O) (optionally -NH 2-z (CH 3 ) z substituted C 1-3 alkyl); -NHC(=O)NH 2-z (CH 3 ) z ; -NHS(O) 2 (optionally -NH 2-z (CH 3 ) z substituted C 1-3 alkyl); -C(=O)CH 3 ; -C(=O)CH 2 NH 2-z (CH 3 ) z ; -C(=O)NH 2-z (C 1-3 alkyl) z ; -S(O) 2 (C 1-3 alkyl); -S(O) 2 (CH 2 ) d NH 2-z (CH 3 ) z ; -OH; and -O(C 1-3 alkyl) (z is 0, 1, or 2; d is 1, 2, or 3; C 1-3 alkyl is methyl, ethyl, propyl, or isopropyl) and is selected from the group consisting of. In one embodiment, when R 9 substitutes the hydrogen atom bonded to the ring carbon atom of ring A, each is independently methyl; ethyl; isopropyl; cyclopropyl; -(CH 2 ) d -NH 2-z (CH 3 ) z ; -(CH 2 ) d -O(CH 3 ); -CF 3 ; -CH 2 CF 3 ; -CH 2 CHF2 ;-CH 2 CH 2 F;-NH 2 ;-NH(C 1-3 alkyl);-N(C 1-3 alkyl) 2 ; halogen (especially, -F, -Cl, -Br); -C(=O)CH 3 ;-C(=O)CH 2 NH 2-z (CH 3 ) z ;-C(=O)NH 2-z (C 1-3 alkyl) z ;-S(O) 2 (C 1-3 alkyl);-S(O) 2 (CH 2 ) d NH 2-z (CH 3 ) z ;-OH; and -O(C 1-3 alkyl) (z is 0, 1 or 2; d is 1, 2 or 3; C 1-3 alkyl is methyl, ethyl, propyl or isopropyl) is selected from the group consisting of. In one embodiment, when R 9 substitutes a hydrogen atom bonded to a ring carbon atom of ring A, each is independently methyl; ethyl; isopropyl; cyclopropyl; -(CH 2 ) d -NH 2-z (CH 3 ) z ;-(CH 2 ) d -O(CH 3 );-CF 3 ;-CH 2 CF 3 ;-CH 2 CHF 2 ;-CH 2 CH 2 F; halogen (especially, -F, -Cl, -Br); -C(=O)CH 3 ;-C(=O)CH 2 NH 2-z (CH 3 ) z ;-C(=O)NH 2-z (C1-3 -alkyl) z ;-S(O) 2 (C 1-3 -alkyl);-S(O) 2 (CH 2 ) d NH 2-z (CH 3 ) z ;-OH; and -O(C 1-3 -alkyl) (where z is 0, 1 or 2; d is 1, 2 or 3; C 1-3 -alkyl is methyl, ethyl, propyl or isopropyl) is selected from the group consisting of. In one embodiment, the ring carbon atoms of ring A are unsubstituted or R which replaces the hydrogen atom bonded to the ring carbon atom 9 is, independently of each other, C 1-4 -alkyl (especially methyl), -N(R 12 )(R 13 )(especially NH 2 ) and -N(R 14 )C(=O)R 11 (especially NHC(O)CH 3 ) is selected from the group consisting of. In one embodiment, the ring carbon atoms of ring A are unsubstituted or one ring carbon atom of ring A is replaced by one R which is NH 2 or CH 3 , or two R 9 which are CH 3 . 9 is substituted.

[0089] R 9 which replaces the hydrogen atom bonded to the ring nitrogen atom of ring A, in any of the above embodiments of the spiroquinoxaline derivative of formula (N-II), such R 9 is, independently of each other, C 1-12 -alkyl (for example, C 1-8 -alkyl or C 1-6 -alkyl), C 2-6 -alkenyl, C 2-6 -alkynyl, 5- or 6-membered aryl, 5- or 6-membered heteroaryl, 3- to 7-membered cycloalkyl, 3- to 7-membered heterocyclyl, -OR 11 , -N(R 12 )(R 13), -S(O) 1-2 R 11 , -S(O) 1-2 N(R 12 )(R 13 ), -N(R 11 )S(O) 1-2 R 11 , -NR 11 S(O) 1-2 N(R 12 )(R 13 ), -C(=X)R 11 , -C(=X)XR 11 , -N(R 14 )C(=X)R 11 and -N(R 14 )C(=X)XR 11 wherein the C 1-12 Alkyl (e.g., C 1-8 Alkyl or C 1-6 Alkyl), C 2-6 Alkenyl, C 2-6 The alkynyl, 5- or 6-membered aryl, 5- or 6-membered heteroaryl, 3- to 7-membered cycloalkyl and 3- to 7-membered heterocyclyl groups each optionally have one or more (e.g., 1 to the C 1-12 Alkyl (e.g., C 1-8 Alkyl or C 1-6 Alkyl), C 2-6 Alkenyl, C 2-6 the maximum number of hydrogen atoms bonded to the alkynyl, 5- or 6-membered aryl, 5- or 6-membered heteroaryl, 3- to 7-membered cycloalkyl, or 3- to 7-membered heterocyclyl group, e.g., up to 1, 2, 3, 4, 5, 6, 7, 8, 9, or 10, e.g., between 1 to 5, 1 to 4, or 1 to 3, or 1 or 2) independently selected R 30 It is replaced by R 9 In any of the above embodiments of the spiroquinoxaline derivatives of Formula (N-II), in which R replaces the hydrogen atom bonded to the ring nitrogen atom of Ring A, such R 9 are each independently: C 1-12 Alkyl (e.g., C 1-8 Alkyl, C 1-6 Alkyl or C 1-4 Alkyl), C 2-4 Alkenyl, C2-4 alkynyl, 6-membered aryl, 5- or 6-membered heteroaryl, 3-, 5-, 6- or 7-membered cycloalkyl, 3-, 5-, 6- or 7-membered heterocyclyl, -OR 11 , -N(R 12 )(R 13 ), -S(O) 1-2 R 11 , -S(O) 1-2 N(R 12 )(R 13 ), -N(R 11 )S(O) 1-2 R 11 , -NR 11 S(O) 1-2 N(R 12 )(R 13 ), -C(=O)R 11 , -C(=O)OR 11 , -C(=O)SR 11 , -C(=O)N(R 14 )(R 11 ), -C(=S)OR 11 , -N(R 14 )C(=O)R 11 , -N(R 14 )C(=O)N(R 14 )(R 11 ) and -N(R 14 )(C=N(R 14 ))N(R 14 )(R 11 ), and may be selected from the group consisting of, wherein the C 1-12 alkyl (e.g., C 1-8 alkyl, C 1-6 alkyl or C 1-4 alkyl), C 2-4 alkenyl, C 2-4 alkynyl, 6-membered aryl, 5- or 6-membered heteroaryl, 3-, 5-, 6- or 7-membered cycloalkyl and 3-, 5-, 6- or 7-membered heterocyclyl groups are each optionally substituted with 1, 2 or 3 independently selected R 30 s. In one embodiment, when R 9 replaces the hydrogen atom bonded to the ring nitrogen atom of ring A, each is independently C 1-12 alkyl (e.g., C 1-8 alkyl, C 1-6 alkyl or C1-4 alkyl); -OH, -O(C 1-3 alkyl) and -NH 2-z (CH 3 ) z substituted with one substituent selected from the group consisting of C 1-12 alkyl (e.g., C 1-8 alkyl, C 1-6 alkyl or C 1-4 alkyl); -CF 3 , -CH 2 CF 3 , -CH 2 CHF 2 or -CH 2 CH 2 F, such as C 1-4 alkyl substituted with one, two or three halogens (preferably F); cyclopropyl; 4 - morpholinyl; homomorpholinyl; 4 - piperidinyl; homopiperidinyl; 4 - piperazinyl; homopiperazinyl; N - methyl - piperazin - 4 - yl; N - methyl - homopiperazinyl; -OH; -O(C 1-3 alkyl); -NH 2 ; -NH(C 1-3 alkyl); -N(C 1-3 alkyl) 2 ; -S(C 1-3 alkyl); -S(O) 2 (optionally -NH 2-z (CH 3 ) z substituted C 1-3 alkyl); -S(O) 2 NH 2-z (C 1-3 alkyl) z ; -NHS(O) 2 (C 1-3 alkyl); -C(=O)(optionally -NH 2-z (CH 3 ) z substituted C 1-3 alkyl); -C(=O)OH; -C(=O)O(C 1-3 alkyl); -C(=O)NH 2-z (C 1-3 alkyl) z ; -NHC(=O)(C 1-3-NHC(=NH)NH(alkyl); z-2 (C 1-3 (alkyl) z ; and -N(C 1-3 (alkyl)C(=NH)NH 2-z (C 1-3 (alkyl) z (z is 0, 1 or 2; C 1-3 (alkyl) is selected from the group consisting of methyl, ethyl, propyl or isopropyl). In one embodiment, when R 9 replaces the hydrogen atom bonded to the ring nitrogen atom of ring A, each is independently methyl; ethyl; isopropyl; n-octyl; n-dodecyl; cyclopropyl; -(CH 2 )) d -NH 2-z (CH 3 )) z ; -(CH 2 )) d -O(CH 3 ); -CH 2 CF 3 ; -CH 2 CHF 2 ; -CH 2 CH 2 F; -C(=O)CH 3 ; -C(=O)CH 2 NH 2-z (CH 3 )) z ; -C(=O)NH 2-z (C 1-3 (alkyl)) z ; -S(O) 2 (C 1-3 (alkyl); -S(O) 2 (CH 2 )) d NH 2-z (CH 3 )) z ; -OH; and -O(C 1-3 (alkyl) (z is 0, 1 or 2; d is 1, 2 or 3; C 1-3 (alkyl) is selected from the group consisting of methyl, ethyl, propyl or isopropyl). In one embodiment, R 9When substituting the hydrogen atom bonded to the ring nitrogen atom of ring A, each independently, methyl; ethyl; isopropyl; cyclopropyl; -(CH 2 ) d -NH 2-z (CH 3 ) z ;-(CH 2 ) d -O(CH 3 );-CH 2 CF 3 ;-CH 2 CHF 2 ;-CH 2 CH 2 F;-C(=O)CH 3 ;-C(=O)CH 2 NH 2-z (CH 3 ) z ;-C(=O)NH 2-z (C 1-3 alkyl) z ;-S(O) 2 (C 1-3 alkyl);-S(O) 2 (CH 2 ) d NH 2-z (CH 3 ) z ;-OH; and -O(C 1-3 alkyl) (z is 0, 1, or 2; d is 1, 2, or 3; C 1-3 alkyl is methyl, ethyl, propyl, or isopropyl), and is selected from the group consisting of. In one embodiment, the ring nitrogen atom of ring A is unsubstituted, or R 9 that substitutes the hydrogen atom bonded to the ring nitrogen atom is each independently C 1-12 alkyl (especially methyl, n-octyl, or n-dodecyl) and -C(=O)R 11 (especially -C(=O)CH 3 or -C(=O)(CH 2 ) 6 CH 3 ) and is selected from the group consisting of. In one embodiment, the ring nitrogen atom of ring A is unsubstituted, or is substituted with one R 9 that is methyl.

[0090] In one embodiment, the spiroquinoxaline derivative has the following general formula (N-III):

Chemical formula

[0091] In one embodiment, the spiroquinoxaline derivative has the following general formula (N-IV):

Chemical formula

[0092] In one embodiment, the spiroquinoxaline derivative has the following general formula (N-V): [Chemical formula] [wherein, R 1 , rings A, E, L and G are synonymous with the above (in particular, for formulas (N-I), (N-II), (N-III) and (N-IV)) or below, R 2 , R 3 , R 4 and R 5 are each H] has. In one embodiment of the spiroquinoxaline derivative of formula (N-V), R 1 , ring A, E, L and G are as defined above (in particular, for formulas (N-I), (N-II), (N-III) and (N-IV)) or have the same meaning as below, R 2 , R 3 , R 4 and R 5 at least one of which is different from H. For example, in one embodiment, R 2 is different from H, and R 3 , R 4 and R 5 are each H; or, R 3 is different from H, and R 2 , R 4 and R 5 are each H; or, R 4 is different from H, and R 2 , R 3 and R 5 are each H; or, R 5 is different from H, and R 2 , R 3 and R 4 are each H; or, R 2 and R 3 are both different from H, and R 4 and R 5 are both H; or, R 2 and R 4 are both different from H, and R 3 and R 5 are both H; or, R 2 and R 5 are both different from H (preferably, in this embodiment, R 2 and R 5 are the same), R 3 and R 4 are both H; or, R 3 and R 4 are both different from H (preferably, in this embodiment, R 3 and R 4 are the same), R 2 and R 5 are both H; or, R 2 , R 3 and R4 is different from H respectively, R 5 is H; or, R 2 , R 3 and R 5 are different from H respectively, R 4 is H; or, R 2 , R 4 and R 5 are different from H respectively, R 3 is H; or, R 3 , R 4 and R 5 are different from H respectively, R 2 is H; or, R 2 , R 3 , R 4 and R 5 are different from H respectively. In any of the above embodiments, R 2 and R 5 are the same, and / or, R 3 and R 4 are preferably the same.

[0093] In any of the above embodiments (particularly for formulas (N-I), (N-II), (N-III), (N-IV) and (N-V)), R 2 ~R 5 is another R 2 ~R 5 do not form a ring together, each independently, -H, C 1-6 alkyl, C 2-6 alkenyl, C 2-6 alkynyl, 5- or 6-membered aryl, 5- or 6-membered heteroaryl, 3- to 7-membered cycloalkyl, 3- to 7-membered heterocyclyl, halogen, -CN, -OR 11 , -N(R 12 )(R 13 ), -S(O) 0-2 R 11 , -S(O) 1-2 N(R 12 )(R 13 ), -N(R 11 )S(O) 1-2 R 11 , -NR 11 S(O) 1-2 N(R 12)(R 13 ), -C(=X)R 11 , -C(=X)XR 11 , -XC(=X)R 11 and -XC(=X)XR 11 selected from the group consisting of, wherein the C 1-6 alkyl, C 2-6 alkenyl, C 2-6 alkynyl, 5- or 6-membered aryl, 5- or 6-membered heteroaryl, 3- to 7-membered cycloalkyl and 3- to 7-membered heterocyclyl group each, optionally, one or more (e.g., 1 to the C 1-6 alkyl, C 2-6 alkenyl, C 2-6 alkynyl, 5- or 6-membered aryl, 5- or 6-membered heteroaryl, 3- to 7-membered cycloalkyl or 3- to 7-membered heterocyclyl group and the maximum number of hydrogen atoms bonded, e.g., 1, 2, 3, 4, 5, 6, 7, 8, 9 or 10, e.g., between 1 to 5, 1 to 4 or 1 to 3, or 1 or 2) of independently selected R 30 is substituted. In one embodiment, R 2 , R 3 , R 4 and R 5 are, when not taken together with another one of R 2 ~R 5 to form a ring, each independently, -H, C 1-4 alkyl, C 2-4 alkenyl, C 2-4 alkynyl, 6-membered aryl, 5- or 6-membered heteroaryl, 3, 5, 6 or 7-membered cycloalkyl, 3, 5, 6 or 7-membered heterocyclyl, halogen, -CN, -OR 11 , -N(R 12 )(R 13 ), -S(O) 0-2 R 11 , -S(O) 1-2 N(R 12 )(R 13 ), -N(R 11 )S(O) 1-2 R 11 , -NR 11 S(O) 1-2 N(R 12 )(R 13 ), -C(=O)R 11, -C(=O)OR 11 , -C(=O)SR 11 , -C(=O)N(R 14 )(R 11 ), -C(=S)OR 11 , -N(R 14 )C(=O)R 11 , -OC(=O)R 11 , -OC(=S)R 11 , -N(R 14 )C(=O)N(R 14 )(R 11 ) and -N(R 14 )C(=N(R 14 ))N(R 14 )(R 11 ) may be selected from the group consisting of, wherein said C 1-4 alkyl, C 2-4 alkenyl, C 2-4 alkynyl, 6-membered aryl, 5- or 6-membered heteroaryl, 3-, 5-, 6- or 7-membered cycloalkyl and 3-, 5-, 6- or 7-membered heterocyclyl group may each optionally be substituted with 1, 2 or 3 independently selected R 30 . In one embodiment of the spiroquinoxaline derivative of formula (N-V), R 1 , ring A, E, L and G are as defined above (in particular for formulas (N-I), (N-II), (N-III) and (N-IV)) or as defined below, and R 2 , R 3 , R 4 and R 5 , when not taken together with another one of R 2 ~R 5 to form a ring, are each independently H; C 1-4 alkyl; -OH, -O(C 1-3 alkyl) and -NH 2-z (CH 3 ) z substituted with one substituent selected from the group consisting of; C 1-4 alkyl; -CF 3 , -CH 2 CF 3 , -CH 2 CHF 2 or -CH 2 CH 2C substituted with one, two or three halogens (preferably F) such as F 1-4 alkyl; phenyl; cyclopropyl; 5-membered heterocyclyl; 4-morpholinyl; homomorpholinyl; 4-piperidinyl; homopiperidinyl; 4-piperazinyl; homopiperazinyl; N-methyl-piperazin-4-yl; N-methyl-homopiperazinyl; halogen; -CN; -OH; -O(C 1-3 alkyl); -OCF 3 , -OCH 2 CF 3 , -OCH 2 CHF 2 or -OCH 2 CH 2 F; -O(C substituted with one, two or three halogens (preferably F) such as F 1-4 alkyl); -O-phenyl; -NH 2 -; -NH(C 1-3 alkyl); -N(C 1-3 alkyl) 2 -; -S(C 1-3 alkyl); -S(O) 2 (optionally -NH 2-z (CH 3 ) z substituted C 1-3 alkyl); -S(O) 2 NH 2-z (C 1-3 alkyl) z -; -NHS(O) 2 (C 1-3 alkyl); -C(=O)(optionally -NH 2-z (CH 3 ) z substituted C 1-3 alkyl); -C(=O)OH; -C(=O)O(C 1-3 alkyl); -C(=O)NH 2-z (C 1-3 alkyl) z -; -NHC(=O)(C 1-3 alkyl); -NHC(=NH)NH z-2 (C 1-3 alkyl) z ; and -N(C 1-3 alkyl)C(=NH)NH 2-z(C 1-3 alkyl) z (where z is 0, 1, or 2, and C 1-3 alkyl is selected from the group consisting of methyl, ethyl, propyl, or isopropyl), and the phenyl, cyclopropyl, 5-membered heterocyclyl, 4-morpholinyl, homomorpholinyl, 4-piperidinyl, homopiperidinyl, 4-piperazinyl, homopiperazinyl, N-methyl-piperazin-4-yl, N-methyl-homopiperazinyl, and -O-phenyl groups are each, optionally, C 1-3 alkyl, halogen, -CF 3 , -OCF 3 , -OH, -OCH 3 , -SCH 3 , -NH 2-z (CH 3 ) z , -C(=O)OH, and -C(=O)OCH 3 (where z is 0, 1, or 2) and are independently substituted with one, two, or three substituents selected from the group consisting of. In one embodiment, R 2 , R 3 , R 4 , and R 5 are, when not taken together with another one of R 2 to R 5 to form a ring, each independently, H; methyl; ethyl; isopropyl; phenyl; cyclopropyl; -(CH 2 ) d -NH 2-z (CH 3 ) z ; -(CH 2 ) d -O(CH 3 ); -CF 3 ; -OCF 3 ; -CH 2 CF 3 ; -CH 2 CHF 2 ; -CH 2 CH 2 F; halogen (especially, -F, -Cl, -Br); -CN; -NH 2 ; -NH(C 1-3 alkyl); -N(C 1-3 alkyl) 2 ; -C(=O)CH3 ;-C(=O)CH 2 NH 2-z (CH 3 ) z ;-C(=O)O(C 1-3 alkyl);-C(=O)NH 2-z (C 1-3 alkyl) z ;-NHC(=O)(C 1-3 alkyl);-S(O) 2 (C 1-3 alkyl);-S(O) 2 (CH 2 ) d NH 2-z (CH 3 ) z ;-OH and -O(C 1-3 alkyl) (where z is 0, 1 or 2; d is 1, 2 or 3; C 1-3 alkyl is methyl, ethyl, propyl or isopropyl) is selected from the group consisting of. In one embodiment of the spiroquinoxaline derivative of formula (N-V), R 1 , ring A, E, L and G are as defined above (in particular, for formulas (N-I), (N-II), (N-III) and (N-IV)) or synonymous with the following, R 2 , R 3 , R 4 and R 5 are independently selected from the group consisting of -H, C 1-4 alkyl and halogen, where the C 1-4 alkyl is optionally substituted with one, two or three independently selected R 30 (in particular, R 2 and R 5 are each -H). In one embodiment of the spiroquinoxaline derivative of formula (N-V), R 1 , ring A, E, L and G are as defined above (in particular, for formulas (N-I), (N-II), (N-III) and (N-IV)) or synonymous with the following, R 2 , R 3 , R 4 and R 5 are independently selected from the group consisting of -H, methyl, F, Cl and CF 3 (in particular, R 2 and R5 are each -H). In one embodiment of the spiroquinoxaline derivative of formula (N-V), R 1 , ring A, E, L and G are as defined above (in particular, for formulas (N-I), (N-II), (N-III) and (N-IV)) or synonymous with the following, and R 2 and R 5 are each -H, R 3 is selected from the group consisting of -H, methyl, F and Cl, and R 4 is selected from the group consisting of -H, methyl, F and Cl. In one embodiment of the spiroquinoxaline derivative of formula (N-V), R 1 , ring A, E, L and G are as defined above (in particular, for formulas (N-I), (N-II), (N-III) and (N-IV)) or synonymous with the following, (i) R 2 to R 5 are each H; or, (ii) R 2 and R 5 are each -H, and both R 3 and R 4 are F, Cl or methyl.

[0094] (i) R 2 and R 3 , (ii) R 3 and R 4 , and / or (iii) R 4 and R 5 form a ring, in any of the above embodiments, the ring is preferably optionally substituted with one or more (e.g., 1 to the maximum number of hydrogen atoms bonded to the ring, e.g., 1, 2, 3, 4, 5, 6, 7, 8, 9 or 10, e.g., between 1 and 5, 1 and 4 or 1 and 3, or 1 or 2) independently selected R 30 is a 3- to 7-membered ring (e.g., a ring having 5 or 6 members). The ring is aromatic, cycloaliphatic, heteroaromatic or heterocyclic (the heteroaromatic / heterocyclic ring is O, S and N(R 40 )(R 40 is R 11 , -OR 11 , -NH y R 20 2-y and -S(O)1-2 R 11 (R 11 、R 20 and y, which are as defined above) and selected from the group consisting of) and selected from the group consisting of one or two heteroatoms containing). In one embodiment, (i) R 2 and R 3 , (ii) R 3 and R 4 , and / or (iii) R 4 and R 5 form a 5- or 6-membered aromatic, alicyclic, heteroaromatic or heterocyclic ring, the heteroaromatic / heterocyclic ring contains one or two heteroatoms selected from the group consisting of O, S and N, and at least one heteroatom is N. In one embodiment, (i) R 2 and R 3 , (ii) R 3 and R 4 , and / or (iii) R 4 and R 5 form a cyclopentadiene, furan, pyrrole, thiophene, imidazole, pyrazole, oxazole, isoxazole, thiazole, dioxole (e.g., 1,3-dioxole), benzene, pyridine, pyrazine, pyrimidine, pyridazine, dioxine (e.g., 1,4-dioxine), 1,2,3-triazine, 1,2,4-triazine and the di- or tetrahydro forms of each of the foregoing selected from the group consisting of. In one embodiment, (i) R 2 and R 3 , (ii) R 3 and R 4 , and / or (iii) R 4 and R 5 form a cyclopentene (e.g., 2,3-dihydrocyclopentadiene), dioxole (e.g., 1,3-dioxole optionally substituted at the 2-position with one or two halogen atoms (e.g., F)), or dioxine (e.g., 2,3-dihydro - [1,4] -dioxine). In one embodiment, (i) R 2 and R 3 , (ii) R3 and R 4 , and / or (iii) R 4 and R 5 The total number of rings formed by is 0 or 1. Thus, in embodiments where (i) R 2 and R 3 , (ii) R 3 and R 4 , and / or (iii) R 4 and R 5 the total number of rings formed by is 1, only two adjacent substituents (i.e., either (i) R 2 and R 3 , (ii) R 3 and R 4 or (iii) R 4 and R 5 ) together with the atom to which they are attached form a ring, where the ring is as defined in any of the above embodiments, and the remainder of R 2 ~R 5 is selected from the group of specific moieties previously specified with respect to the situation where they do not form a ring together. For example, the remainder of R 2 ~R 5 that do not form a ring together is -H, C 1-6 alkyl, C 2-6 alkenyl, C 2-6 alkynyl, 5- or 6-membered aryl, 5- or 6-membered heteroaryl, 3- to 7-membered cycloalkyl, 3- to 7-membered heterocyclyl, halogen, -CN, -OR 11 , -N(R 12 )(R 13 ), -S(O) 0-2 R 11 , -S(O) 1-2 N(R 12 )(R 13 ), -N(R 11 )S(O) 1-2 R 11 , -NR 11 S(O) 1-2 N(R 12 )(R 13 ), -C(=X)R 11 , -C(=X)XR 11 , -XC(=X)R 11 and -XC(=X)XR11 may be selected from, where the C 1-6 alkyl, C 2-6 alkenyl, C 2-6 alkynyl, 5- or 6-membered aryl, 5- or 6-membered heteroaryl, 3- to 7-membered cycloalkyl, and 3- to 7-membered heterocyclyl groups may each, optionally, have one or more (e.g., 1 to the C 1-6 alkyl, C 2-6 alkenyl, C 2-6 alkynyl, 5- or 6-membered aryl, 5- or 6-membered heteroaryl, 3- to 7-membered cycloalkyl, or 3- to 7-membered heterocyclyl group, up to the maximum number of hydrogen atoms that can be bonded, e.g., 1, 2, 3, 4, 5, 6, 7, 8, 9, or 10, e.g., between 1 and 5, 1 and 4, or 1 and 3, or 1 or 2) of independently selected R 30 substituents. In another embodiment, R 2 ~R 5 do not form a ring together.

[0095] In any of the above embodiments, R 2 and R 5 may be the same, and / or R 3 and R 4 may be the same.

[0096] In one embodiment of the spiroquinoxaline derivative of formula (N-V), R 1 , ring A, E, L, and G are as defined above (particularly for formulas (N-I), (N-II), (N-III), and (N-IV)) or as defined below, and R 2 , R 3 , R 4 and R 5 are independently selected from the group consisting of -H, C 1-4 alkyl, and halogen, where the C 1-4 alkyl is optionally substituted with one, two, or three independently selected R 30 (particularly where R 2 and R 5 are each -H), or R 3 and R 4together with the atoms to which they are attached, optionally form a 5- or 6-membered ring substituted with one or two independently selected R 30 and may form a 5- or 6-membered ring optionally substituted with one or two independently selected R. In one embodiment of the spiroquinoxaline derivative of formula (N-V), R 1 , ring A, E, L and G are as defined above (in particular for formulae (N-I), (N-II), (N-III) and (N-IV)) or as defined below, and R 2 , R 3 , R 4 and R 5 are independently selected from the group consisting of -H, methyl, F, Cl and CF 3 (in particular, R 2 and R 5 are each -H), or R 3 and R 4 together with the atoms to which they are attached may optionally form a dioxolane or dioxin ring optionally substituted with one or two independently selected halogens (in particular F). In one embodiment of the spiroquinoxaline derivative of formula (N-V), R 1 , ring A, E, L and G are as defined above (in particular for formulae (N-I), (N-II), (N-III) and (N-IV)) or as defined below, R 2 and R 5 are each -H; R 3 is selected from the group consisting of -H, methyl, F and Cl; R 4 is selected from the group consisting of -H, methyl, F and Cl; or R 3 and R 4 together with the atoms to which they are attached may form a dioxolane (in particular 1,3-dioxolane) or dioxin (in particular 2,3-dihydro-[1,4]-dioxin) ring, and the dioxolane ring may optionally be substituted with two Fs. In one embodiment of the spiroquinoxaline derivative of formula (N-V), R 1 , ring A, E, L and G are as defined above (in particular for formulae (N-I), (N-II), (N-III) and (N-IV)) or as defined below, (i) R 2 ~R 5is each -H; (ii) R 2 and R 5 are each -H, and R 3 and R 4 both are F, Cl or methyl; or (iii) R 2 and R 5 are each -H, and R 3 and R 4 together with the atom to which they are attached form a 2,2-difluoro-1,3-dioxolane ring or a 2,3-dihydro-[1,4]-dioxin ring.

[0097] In any of the above embodiments (in particular, for formulas (N-I), (N-II), (N-III), (N-IV) and (N-V)), R 30 may in each case be a typical first, second or third level substituent specified above, and independently, C 1-4 alkyl, C 2-4 alkenyl, C 2-4 alkynyl, 5- or 6-membered aryl, 5- or 6-membered heteroaryl, 5- or 6-membered cycloalkyl, 5-, 6- or 7-membered heterocyclyl, halogen, -CF 3 , -CN, azide, -NO 2 , -OH, -O(C 1-3 alkyl), -S(C 1-3 alkyl), -NH 2 , -NH(C 1-3 alkyl), -N(C 1-3 alkyl) 2 , -NHS(O) 2 (C 1-3 alkyl), -S(O) 2 NH 2-z (C 1-3 alkyl) z , -C(=O)OH, -C(=O)O(C 1-3 alkyl), -C(=O)NH 2-z (C 1-3 alkyl) z , -NHC(=O)(C 1-3 alkyl), -NHC(=NH)NH z-2 (C 1-3 alkyl) z and -N(C1-3 (alkyl)C(=NH)NH 2-z (C 1-3 alkyl) z (z is 0, 1, or 2, and C 1-3 alkyl is selected from the group consisting of methyl, ethyl, propyl, or isopropyl) (e.g., 4-morpholinyl, homomorpholinyl, 4-piperidinyl, homopiperidinyl (i.e., azepanyl, especially 4-azepanyl), 4-piperazinyl, homopiperazinyl (i.e., diazepanyl, especially 2,4-diazepanyl), N-methyl-piperazin-4-yl, N-methyl-homopiperazinyl, -CH 2 CH 2 OCH 3 -OCH 2 CH 2 OCH 3 -CH 2 CH 2 NH 2-z (CH 3 ) z -OCH 2 CH 2 NH 2-z (CH 3 ) z -CF 3 -OCF 3 ) and may be. Alternatively, R 30 is phenyl, furanyl, pyrrolyl, thienyl, imidazolyl, oxazolyl, isoxazolyl, thiazolyl, pyridyl, pyrazinyl, pyrimidinyl, pyridazinyl, the partially and fully hydrogenated forms of the above groups, morpholino, C 1-3 alkyl, halogen, -CF 3 , -OH, -OCH 3 , -OCF 3 , -SCH 3 , -NH 2-z (CH 3 ) z , -C(=O)OH and -C(=O)OCH 3 (z is 0, 1, or 2) and may be selected from the group consisting of.

[0098] In one embodiment, the spiroquinoxaline derivative has the following general formula (O / S-I): [Chemical formula] [wherein, E is -N(R 6 )-; L is C 1-10 alkylene, C 2-10 alkenylene, C 2-10 alkynylene, 1,1-(CH 2 ) a -cyclopropylene-(CH 2 ) b -(wherein a and b are each independently selected from integers between 0 and 3) and -(CH 2 ) m -[Y-(CH 2 ) n o -(wherein m is an integer between 1 and 6, n is an integer between 0 and 3, o is an integer between 1 and 3, when n is 0, o is 1, and Y is independently selected from O, S, and -N(R 7 )); and the C 1-10 alkylene, C 2-10 alkenylene, C 2-10 alkynylene, 1,1-cyclopropylene, -(CH 2 ) m - and -(CH 2 ) n - groups are each optionally substituted with one or more (e.g., 1 to the maximum number of hydrogen atoms bonded to the C 1-10 alkylene, C 2-10 alkenylene, C 2-10 alkynylene, 1,1-cyclopropylene, -(CH 2 ) m - or -(CH 2 ) n - group, e.g., 1, 2, 3, 4, 5, 6, 7, 8, 9, or 10, e.g., between 1 and 5, 1 and 4, or 1 and 3, or 1 or 2) independently selected R 30 ; G is phenyl optionally substituted with one, two, three, four, or five independently selected R 8 ; ​Ring A is, optionally, a monocyclic 4- to 10-membered O / S-heterocycloalkylene substituted with one or more (e.g., from 1 to the maximum number of hydrogen atoms bonded to ring A, e.g., up to 1, 2, 3, 4, 5, 6, 7, 8, 9, or 10, e.g., between 1 and 5, between 1 and 4, or between 1 and 3, or 1 or 2) independently selected R 9 ; and is a monocyclic 4- to 10-membered O / S-heterocycloalkylene substituted with one or more (e.g., from 1 to the maximum number of hydrogen atoms bonded to ring A, e.g., up to 1, 2, 3, 4, 5, 6, 7, 8, 9, or 10, e.g., between 1 and 5, between 1 and 4, or between 1 and 3, or 1 or 2) independently selected R R 1 is H; R 2 , R 3 , R 4 and R 5 are independently -H, alkyl, alkenyl, alkynyl, aryl, heteroaryl, cycloalkyl, heterocyclyl, halogen, -CN, azide, -NO 2 , -OR 11 , -N(R 12 )(R 13 ), -N(R 11 )(OR 11 ), -S(O) 0-2 R 11 , -S(O) 1-2 OR 11 , -OS(O) 1-2 R 11 , -OS(O) 1-2 OR 11 , -S(O) 1-2 N(R 12 )(R 13 ), -OS(O) 1-2 N(R 12 )(R 13 ), -N(R 11 )S(O) 1-2 R 11 , -NR 11 S(O) 1-2 OR 11 , -NR 11 S(O) 1-2 N(R 12 )(R 13 ), -C(=X)R 11 , -C(=X)XR 11 , -XC(=X)R 11 and -XC(=X)XR 11Selected from the group consisting of, wherein each of said alkyl, alkenyl, alkynyl, aryl, heteroaryl, cycloalkyl and heterocyclyl groups is optionally substituted with one or more (e.g., 1 to the maximum number of hydrogen atoms bonded to said alkyl, alkenyl, alkynyl, aryl, heteroaryl, cycloalkyl or heterocyclyl group, e.g., up to 1, 2, 3, 4, 5, 6, 7, 8, 9 or 10, e.g., between 1 and 5, 1 and 4 or 1 and 3, or 1 or 2) independently selected R 30 or is substituted with; R 2 and R 3 together with the atom to which they are attached may optionally form a ring substituted with one or more (e.g., 1 to the maximum number of hydrogen atoms bonded to said ring, e.g., up to 1, 2, 3, 4, 5, 6, 7, 8, 9 or 10, e.g., between 1 and 5, 1 and 4 or 1 and 3, or 1 or 2) independently selected R 30 ; R 3 and R 4 together with the atom to which they are attached may optionally form a ring substituted with one or more (e.g., 1 to the maximum number of hydrogen atoms bonded to said ring, e.g., up to 1, 2, 3, 4, 5, 6, 7, 8, 9 or 10, e.g., between 1 and 5, 1 and 4 or 1 and 3, or 1 or 2) independently selected R 30 ; and / or, R 4 and R 5 together with the atom to which they are attached may optionally form a ring substituted with one or more (e.g., 1 to the maximum number of hydrogen atoms bonded to said ring, e.g., up to 1, 2, 3, 4, 5, 6, 7, 8, 9 or 10, e.g., between 1 and 5, 1 and 4 or 1 and 3, or 1 or 2) independently selected R 30 ; R 6 is H; R 7 is -H, alkyl, alkenyl, alkynyl, cycloalkyl, aryl, heteroaryl, heterocyclyl, -OR 11 and -NHR 20selected from the group consisting of, wherein said alkyl, alkenyl, alkynyl, cycloalkyl, aryl, heteroaryl and heterocyclyl groups are each optionally substituted with one or more (e.g., 1 to the maximum number of hydrogen atoms bonded to the alkyl, alkenyl, alkynyl, aryl, heteroaryl, cycloalkyl or heterocyclyl group, e.g., up to 1, 2, 3, 4, 5, 6, 7, 8, 9 or 10, e.g., between 1 and 5, 1 and 4 or 1 and 3, or 1 or 2) independently selected R 30 and is substituted with; R 8 is in each case alkyl, alkenyl, alkynyl, aryl, heteroaryl, cycloalkyl, heterocyclyl, halogen, -CN, azide, -NO 2 -OR 11 -N(R 12 )(R 13 ) -N(R 11 )(OR 11 ) -S(O) 0-2 R 11 -S(O) 1-2 OR 11 -OS(O) 1-2 R 11 -OS(O) 1-2 OR 11 -S(O) 1-2 N(R 12 )(R 13 ) -OS(O) 1-2 N(R 12 )(R 13 ) -N(R 11 )S(O) 1-2 R 11 -NR 11 S(O) 1-2 OR 11 -NR 11 S(O) 1-2 N(R 12 )(R 13 ) -C(=X)R 11 -C(=X)XR 11 -XC(=X)R 11 and -XC(=X)XR 11Selected from the group consisting of, wherein said alkyl, alkenyl, alkynyl, aryl, heteroaryl, cycloalkyl and heterocyclyl groups are each optionally one or more (e.g., 1 to the maximum number of hydrogen atoms bonded to the alkyl, alkenyl, alkynyl, aryl, heteroaryl, cycloalkyl or heterocyclyl group, e.g., 1, 2, 3, 4, 5, 6, 7, 8, 9 or 10, e.g., between 1 and 5, 1 and 4 or 1 and 3, or 1 or 2) independently selected R 30 is substituted with; R 9 When substituting a hydrogen atom bonded to a ring carbon atom, alkyl, alkenyl, alkynyl, aryl, heteroaryl, cycloalkyl, heterocyclyl, halogen, -CN, azide, -NO 2 、-OR 11 、-N(R 12 )(R 13 )、-S(O) 0-2 R 11 、-S(O) 1-2 OR 11 、-OS(O) 1-2 R 11 、-OS(O) 1-2 OR 11 、-S(O) 1-2 N(R 12 )(R 13 )、-OS(O) 1-2 N(R 12 )(R 13 )、-N(R 11 )S(O) 1-2 R 11 、-NR 11 S(O) 1-2 OR 11 、-NR 11 S(O) 1-2 N(R 12 )(R 13 )、-C(=X)R 11 、-C(=X)XR 11 、-XC(=X)R 11 and -XC(=X)XR 11Independently selected from the group consisting of, wherein each of the alkyl, alkenyl, alkynyl, aryl, heteroaryl, cycloalkyl and heterocyclyl groups may optionally have one or more (e.g., 1 to the maximum number of hydrogen atoms bonded to the alkyl, alkenyl, alkynyl, aryl, heteroaryl, cycloalkyl or heterocyclyl group, e.g., up to 1, 2, 3, 4, 5, 6, 7, 8, 9 or 10, e.g., between 1 and 5, 1 and 4 or 1 and 3, or 1 or 2) independently selected R 30 substituted, and / or any two Rs bonded to the same carbon atom of ring A 9 may together form =X; or, when R 9 is bonded to the ring sulfur atom of ring A, it is independently selected from the group consisting of alkyl, alkenyl, alkynyl, aryl, heteroaryl, cycloalkyl, heterocyclyl, -OR 11 and =O, wherein each of the alkyl, alkenyl, alkynyl, aryl, heteroaryl, cycloalkyl and heterocyclyl groups may optionally have one or more (e.g., 1 to the maximum number of hydrogen atoms bonded to the alkyl, alkenyl, alkynyl, aryl, heteroaryl, cycloalkyl or heterocyclyl group, e.g., up to 1, 2, 3, 4, 5, 6, 7, 8, 9 or 10, e.g., between 1 and 5, 1 and 4 or 1 and 3, or 1 or 2) independently selected R 30 substituted; X is independently selected from O, S and N(R 14 ); R 11 in each case is selected from the group consisting of -H, alkyl, alkenyl, alkynyl, cycloalkyl, aryl, heteroaryl and heterocyclyl, wherein each of the alkyl, alkenyl, alkynyl, cycloalkyl, aryl, heteroaryl and heterocyclyl groups may optionally have one or more (e.g., 1 to the maximum number of hydrogen atoms bonded to the alkyl, alkenyl, alkynyl, cycloalkyl, aryl, heteroaryl or heterocyclyl group, e.g., up to 1, 2, 3, 4, 5, 6, 7, 8, 9 or 10, e.g., between 1 and 5, 1 and 4 or 1 and 3, or 1 or 2) independently selected R30 is replaced by; R 12 and R 13 in each case are independently selected from the group consisting of -H, alkyl, alkenyl, alkynyl, cycloalkyl, aryl, heteroaryl and heterocyclyl, or R 12 and R 13 may together with the nitrogen atom to which they are attached form the group -N=CR 15 R 16 wherein the alkyl, alkenyl, alkynyl, cycloalkyl, aryl, heteroaryl and heterocyclyl groups are each optionally substituted by one or more (e.g., 1 to the maximum number of hydrogen atoms attached to the alkyl, alkenyl, alkynyl, cycloalkyl, aryl, heteroaryl or heterocyclyl group, e.g., up to 1, 2, 3, 4, 5, 6, 7, 8, 9 or 10, e.g., between 1 and 5, 1 and 4 or 1 and 3, or 1 or 2) independently selected R 30 groups; R 14 is independently selected from the group consisting of -H, alkyl, alkenyl, alkynyl, cycloalkyl, aryl, heteroaryl, heterocyclyl and -OR 11 wherein the alkyl, alkenyl, alkynyl, cycloalkyl, aryl, heteroaryl and heterocyclyl groups are each optionally substituted by one or more (e.g., 1 to the maximum number of hydrogen atoms attached to the alkyl, alkenyl, alkynyl, cycloalkyl, aryl, heteroaryl or heterocyclyl group, e.g., up to 1, 2, 3, 4, 5, 6, 7, 8, 9 or 10, e.g., between 1 and 5, 1 and 4 or 1 and 3, or 1 or 2) independently selected R 30 groups; R 15 and R 16 are independently selected from the group consisting of -H, alkyl, alkenyl, alkynyl, cycloalkyl, aryl, heteroaryl, heterocyclyl and -NH y R 20 2-y 15 and R 16 ​may combine with the atoms to which they are attached to form, optionally, a ring substituted with one or more (e.g., 1 to the maximum number of hydrogen atoms attached to the ring, e.g., up to 1, 2, 3, 4, 5, 6, 7, 8, 9, or 10, e.g., between 1 and 5, 1 and 4, or 1 and 3, or 1 or 2) independently selected R 30 wherein the alkyl, alkenyl, alkynyl, cycloalkyl, aryl, heteroaryl, and heterocyclyl groups may each be optionally substituted with one or more (e.g., 1 to the maximum number of hydrogen atoms attached to the alkyl, alkenyl, alkynyl, cycloalkyl, aryl, heteroaryl, or heterocyclyl group, e.g., up to 1, 2, 3, 4, 5, 6, 7, 8, 9, or 10, e.g., between 1 and 5, 1 and 4, or 1 and 3, or 1 or 2) independently selected R 30 ; y is an integer from 0 to 2; R 20 is selected from the group consisting of alkyl, alkenyl, alkynyl, cycloalkyl, aryl, heteroaryl, and heterocyclyl, wherein the alkyl, alkenyl, alkynyl, cycloalkyl, aryl, heteroaryl, and heterocyclyl groups may each be optionally substituted with one or more (e.g., 1 to the maximum number of hydrogen atoms attached to the alkyl, alkenyl, alkynyl, cycloalkyl, aryl, heteroaryl, or heterocyclyl group, e.g., up to 1, 2, 3, 4, 5, 6, 7, 8, 9, or 10, e.g., between 1 and 5, 1 and 4, or 1 and 3, or 1 or 2) independently selected R 30 ; R 30 is a first-level substituent, and in each case, independently, alkyl, alkenyl, alkynyl, aryl, heteroaryl, cycloalkyl, heterocyclyl, halogen, -CN, azide, -NO 2 , -OR 71 , -N(R 72 )(R 73 ), -S(O) 0-2 R 71 , -S(O) 1-2 OR 71 , -OS(O) 1-2 R 71, -OS(O) 1-2 OR 71 , -S(O) 1-2 N(R 72 )(R 73 ), -OS(O) 1-2 N(R 72 )(R 73 ), -N(R 71 )S(O) 1-2 R 71 , -NR 71 S(O) 1-2 OR 71 , -NR 71 S(O) 1-2 N(R 72 )(R 73 ), -C(=X 1 )R 71 ), -C(=X 1 )X 1 R 71 ), -X 1 C(=X 1 )R 71 and -X 1 C(=X 1 )X 1 R 71 selected from the group consisting of, and / or, any two Rs attached to the same carbon atom of a cycloalkyl or heterocyclyl group 30 may together form =X 1 , wherein the alkyl, alkenyl, alkynyl, aryl, heteroaryl, cycloalkyl and heterocyclyl groups, which are first-level substituents, each may optionally be substituted by one or more (e.g., 1 to the maximum number of hydrogen atoms attached to the alkyl, alkenyl, alkynyl, aryl, heteroaryl, cycloalkyl or heterocyclyl group which is the first-level substituent, e.g., up to 1, 2, 3, 4, 5, 6, 7, 8, 9 or 10, e.g., between 1 and 5, 1 and 4 or 1 and 3, or 1 or 2) second-level substituents, and the second-level substituents are in each case independently C 1-6 alkyl, C 2-6 alkenyl, C 2-6 alkynyl, 3- to 14-membered aryl, 3- to 14-membered heteroaryl, 3- to 14-membered cycloalkyl, 3- to 14-membered heterocyclyl, halogen, -CF 3, -CN, azide, -NO 2 , -OR 81 , -N(R 82 )(R 83 ), -S(O) 0-2 R 81 , -S(O) 1-2 OR 81 , -OS(O) 1-2 R 81 , -OS(O) 1-2 OR 81 , -S(O) 1-2 , -S(O) 82 )(R 83 ), -OS(O) 1-2 , -OS(O) 82 )(R 83 ), -N(R 81 )S(O) 1-2 R 81 , -NR 81 S(O) 1-2 OR 81 , -NR 81 S(O) 1-2 , -NR 82 )(R 83 ), -C(=X 2 )R 81 , -C(=X 2 )X 2 R 81 , -X 2 C(=X 2 )R 81 and -X 2 C(=X 2 )X 2 R 81 selected from the group consisting of, and / or any two second-level substituents bonded to the same carbon atom of a cycloalkyl or heterocyclyl group that is a first-level substituent may together form =X 2 , wherein the C 1-6 alkyl, C 2-6 alkenyl, C 2-6 alkynyl, 3- to 14-membered aryl, 3- to 14-membered heteroaryl, 3- to 14-membered cycloalkyl and 3- to 14-membered heterocyclyl groups each optionally have one or more (e.g., 1 to the C 1-6 alkyl, C 2-6 alkenyl, C 2-6The maximum number of hydrogen atoms bonded to an alkynyl, 3- to 14-membered aryl, 3- to 14-membered heteroaryl, 3- to 14-membered cycloalkyl or 3- to 14-membered heterocyclyl group, for example up to 1, 2, 3, 4, 5, 6, 7, 8, 9 or 10, for example between 1-5, 1-4 or 1-3, or 1 or 2) is substituted with a third-level substituent, which in each case is independently C 1-3 alkyl, halogen, -CF 3 , -CN, azide, -NO 2 , -OH, -O(C 1-3 alkyl), -OCF 3 , -S(C 1-3 alkyl), -NH 2 , -NH(C 1-3 alkyl), -N(C 1-3 alkyl) 2 , -NHS(O) 2 (C 1-3 alkyl), -S(O) 2 NH 2-z (C 1-3 alkyl) z , -C(=O)OH, -C(=O)O(C 1-3 alkyl), -C(=O)NH 2-z (C 1-3 alkyl) z , -NHC(=O)(C 1-3 alkyl), -NHC(=NH)NH z-2 (C 1-3 alkyl) z and -N(C 1-3 alkyl)C(=NH)NH 2-z (C 1-3 alkyl) z selected from the group consisting of, where z is 0, 1 or 2, C 1-3 alkyl is methyl, ethyl, propyl or isopropyl, and / or any two third-level substituents bonded to the same carbon atom of a 3- to 14-membered cycloalkyl or heterocyclyl group that is a second-level substituent may together form =O, =S, =NH or =N(C 1-3 alkyl); R 71 , R 72 and R 73is, independently, -H, C 1-6 alkyl, C 2-6 alkenyl, C 2-6 alkynyl, 3- to 7-membered cycloalkyl, 5- or 6-membered aryl, 5- or 6-membered heteroaryl and 3- to 7-membered heterocyclyl, where the C 1-6 alkyl, C 2-6 alkenyl, C 2-6 alkynyl, 3- to 7-membered cycloalkyl, 5- or 6-membered aryl, 5- or 6-membered heteroaryl and 3- to 7-membered heterocyclyl groups are each, optionally, C 1-3 alkyl, halogen, -CF 3 , -CN, azide, -NO 2 , -OH, -O(C 1-3 alkyl), -OCF 3 , =O, -S(C 1-3 alkyl), -NH 2 , -NH(C 1-3 alkyl), -N(C 1-3 alkyl) 2 , -NHS(O) 2 (C 1-3 alkyl), -S(O) 2 NH 2-z (C 1-3 alkyl) z , -C(=O)(C 1-3 alkyl), -C(=O)OH, -C(=O)O(C 1-3 alkyl), -C(=O)NH 2-z (C 1-3 alkyl) z , -NHC(=O)(C 1-3 alkyl), -NHC(=NH)NH z-2 (C 1-3 alkyl) z and -N(C 1-3 alkyl)C(=NH)NH 2-z (C 1-3 alkyl) z (z is 0, 1 or 2, and C 1-3 alkyl is methyl, ethyl, propyl or isopropyl) and is substituted with one, two or three substituents selected from the group consisting of; R 81 , R 82 and R83 is, independently, -H, C 1-4 alkyl, C 2-4 alkenyl, C 2-4 alkynyl, 3- to 6-membered cycloalkyl, 5- or 6-membered aryl, 5- or 6-membered heteroaryl and 3- to 6-membered heterocyclyl, where the C 1-4 alkyl, C 2-4 alkenyl, C 2-4 alkynyl, 3- to 6-membered cycloalkyl, 5- or 6-membered aryl, 5- or 6-membered heteroaryl and 3- to 6-membered heterocyclyl groups are each, optionally, C 1-3 alkyl, halogen, -CF 3 , -CN, azide, -NO 2 , -OH, -O(C 1-3 alkyl), -OCF 3 , =O, -S(C 1-3 alkyl), -NH 2 , -NH(C 1-3 alkyl), -N(C 1-3 alkyl) 2 , -NHS(O) 2 (C 1-3 alkyl), -S(O) 2 NH 2-z (C 1-3 alkyl) z , -C(=O)(C 1-3 alkyl), -C(=O)OH, -C(=O)O(C 1-3 alkyl), -C(=O)NH 2-z (C 1-3 alkyl) z , -NHC(=O)(C 1-3 alkyl), -NHC(=NH)NH z-2 (C 1-3 alkyl) z and -N(C 1-3 alkyl)C(=NH)NH 2-z (C 1-3 alkyl) z (z is 0, 1 or 2, and C 1-3 alkyl is methyl, ethyl, propyl or isopropyl) and is substituted with one, two or three substituents selected from the group consisting of; X 1 and X 2is, independently, O, S and N(R 84 )(R 84 is -H or C 1-3 alkyl)), selected from] and includes its solvates, salts, complexes, polymorphs, crystalline forms, racemic mixtures, diastereomers, enantiomers, tautomers, isotope-labeled forms, prodrugs, and combinations thereof.

[0099] In one embodiment, the spiroquinoxaline derivative has the following general formula (O / S-II):

Chemical formula

[0100] In any of the above embodiments of the spiroquinoxaline derivative of formula (O / S-II), ring A may be unsubstituted.

[0101] In any of the above embodiments of the spiroquinoxaline derivative of formula (O / S-II) in which ring A is substituted with one or more (e.g., from 1 to the maximum number of hydrogen atoms bonded to ring A, e.g., up to 1, 2, 3, 4, 5, 6, 7, 8, 9, or 10, e.g., between 1 and 5, between 1 and 4, or between 1 and 3, or 1 or 2) independently selected R 9 In any of the above embodiments of the spiroquinoxaline derivative of formula (O / S-II), where one or more (preferably one or two) of the ring sulfur atoms of ring A are substituted with independently selected R 9 Or (ii) only one or more (preferably one, two, or three) of the ring carbon atoms of ring A are substituted with independently selected R 9 Or (iii) one or more (preferably one or two) of the ring sulfur atoms and one or more (preferably one, two, or three) of the ring carbon atoms (e.g., one or two ring heteroatoms and one or two ring carbon atoms) of ring A are substituted with independently selected R 9 For example, when ring A contains one ring sulfur atom, ring A may be substituted with R 9 Only (i) at the ring sulfur atom (preferably, when ring A is 4- or 5-membered, the ring sulfur atom is at the 3-position, when ring A is 6- or 7-membered, the ring sulfur atom is at the 3- or 4-position (preferably the 4-position), and when ring A is 8-membered, the ring sulfur atom is at the 3, 4, or 5-position (preferably the 4- or 5-position)); 9 Or (ii) only at one or two ring carbon atoms of ring A, each with one or two independently selected R 9 Or (iii) at the ring sulfur atom (preferably, when ring A is 4- or 5-membered, the ring sulfur atom is at the 3-position, when ring A is 6- or 7-membered, the ring sulfur atom is at the 3- or 4-position (preferably the 4-position), and when ring A is 8-membered, the ring sulfur atom is at the 3, 4, or 5-position (preferably the 4- or 5-position)) with R 9 And at one or two ring carbon atoms of ring A, each with one or two independently selected R

[0102] R 9In any of the above embodiments of the spiroquinoxaline derivative of formula (O / S-II) that replaces the hydrogen atom bonded to the ring carbon atom of ring A, such R 9 is, independently of each other, C 1-6 alkyl, C 2-6 alkenyl, C 2-6 alkynyl, 5- or 6-membered aryl, 5- or 6-membered heteroaryl, 3- to 7-membered cycloalkyl, 3- to 7-membered heterocyclyl, halogen, -CN, -OR 11 , -N(R 12 )(R 13 ), -S(O) 0-2 R 11 , -S(O) 1-2 N(R 12 )(R 13 ), -N(R 11 )S(O) 1-2 R 11 , -NR 11 S(O) 1-2 N(R 12 )(R 13 ), -C(=X)R 11 , -C(=X)XR 11 , -XC(=X)R 11 and -XC(=X)XR 11 and may be selected from the group consisting of, wherein the C 1-6 alkyl, C 2-6 alkenyl, C 2-6 alkynyl, 5- or 6-membered aryl, 5- or 6-membered heteroaryl, 3- to 7-membered cycloalkyl and 3- to 7-membered heterocyclyl groups are each optionally one or more (e.g., 1 to the maximum number of hydrogen atoms bonded to the C 1-6 alkyl, C 2-6 alkenyl, C 2-6 alkynyl, 5- or 6-membered aryl, 5- or 6-membered heteroaryl, 3- to 7-membered cycloalkyl or 3- to 7-membered heterocyclyl group, e.g., 1, 2, 3, 4, 5, 6, 7, 8, 9 or 10, e.g., between 1 and 5, 1 and 4 or 1 and 3, or 1 or 2) independently selected R 30 substituted, and / or any two R 9 bonded to the same carbon atom of ring A may together form =X. R 9In any of the above embodiments of the spiroquinoxaline derivative of formula (O / S-II) in which a hydrogen atom bonded to a ring carbon atom of ring A is substituted, such R 9 is, independently of each other, C 1-4 alkyl, C 2-4 alkenyl, C 2-4 alkynyl, 6-membered aryl, 5- or 6-membered heteroaryl, 3-, 5-, 6- or 7-membered cycloalkyl, 3-, 5-, 6- or 7-membered heterocyclyl, halogen, -CN, -OR 11 , -N(R 12 )(R 13 ), -S(O) 0-2 R 11 , -S(O) 1-2 N(R 12 )(R 13 ), -N(R 11 )S(O) 1-2 R 11 , -NR 11 S(O) 1-2 N(R 12 )(R 13 ), -C(=O)R 11 , -C(=O)OR 11 , -C(=O)SR 11 , -C(=O)N(R 14 )(R 11 ), -C(=S)OR 11 , -N(R 14 )C(=O)R 11 , -OC(=O)R 11 , -OC(=S)R 11 , -N(R 14 )C(=O)N(R 14 )(R 11 ) and -N(R 14 )C(=N(R 14 ))N(R 14 )(R 11 ), and may be selected from the group consisting of, where the C 1-4 alkyl, C 2-4 alkenyl, C 2-4 alkynyl, 6-membered aryl, 5- or 6-membered heteroaryl, 3-, 5-, 6- or 7-membered cycloalkyl and 3-, 5-, 6- or 7-membered heterocyclyl groups each, optionally, have one, two or three independently selected R 30is replaced, and / or any two Rs attached to the same carbon atom of ring A 9 may together form =O or =S. In one embodiment, when R 9 replaces a hydrogen atom attached to a ring carbon atom of ring A, each is independently C 1-4 alkyl; -OH, -O(C 1-3 alkyl), -NH 2-z (CH 3 ) z , morpholinyl (e.g., 4 - morpholinyl), piperazinyl (e.g., 1 - piperazinyl) and N - methylpiperazinyl (e.g., 4 - methylpiperazin - 1 - yl) and is substituted with one substituent selected from the group consisting of C 1-4 alkyl; -CF 3 , -CH 2 CF 3 , -CH 2 CHF 2 or -CH 2 CH 2 F, i.e., C 1-4 alkyl substituted with one, two or three halogens (preferably F); -OCF 3 , -OCH 2 CF 3 , -OCH 2 CHF 2 or -OCH 2 CH 2 F, i.e., -O(C 1-4 alkyl substituted with one, two or three halogens (preferably F); cyclopropyl; 4 - morpholinyl; homomorpholinyl; 4 - piperidinyl; homopiperidinyl; 4 - piperazinyl; homopiperazinyl; 4 - methyl - piperazin - 1 - yl; N - methyl - homopiperazinyl; halogen; -CN; -OH; =O; -O(optionally -NH 2-z (CH 3 ) z substituted C 1-3 alkyl); -NH 2 ; -NH(C 1-3 alkyl); -N(C 1-3 alkyl) 2 ; -S(C 1-3-S(O)(alkyl); -S(O) 2 (optionally -NH 2-z (CH 3 ) z substituted C 1-3 alkyl); -S(O) 2 NH 2-z (C 1-3 alkyl) z ; -NHS(O) 2 (optionally -NH 2-z (CH 3 ) z substituted C 1-3 alkyl); -C(=O)(optionally -NH 2-z (CH 3 ) z substituted C 1-3 alkyl); -C(=O)OH; -C(=O)O(C 1-3 alkyl); -C(=O)NH 2-z (C 1-3 alkyl) z ; -NHC(=O)(optionally -NH 2-z (CH 3 ) z substituted C 1-3 alkyl); -NHC(=O)NH 2-z (CH 3 ) z ; -NHC(=NH)NH z-2 (C 1-3 alkyl) z ; and -N(C 1-3 alkyl)C(=NH)NH 2-z (C 1-3 alkyl) z (z is 0, 1, or 2, and C 1-3 alkyl is methyl, ethyl, propyl, or isopropyl) is selected from the group consisting of. In one embodiment, when R 9 substitutes a hydrogen atom bonded to a ring carbon atom of ring A, each is independently methyl; ethyl; isopropyl; tert - butyl; cyclopropyl; -(CH 2 ) d -NH 2-z (CH 3 ) z ; -O(CH 2 ) d-NH 2-z (CH 3 ) z ;-(CH 2 ) d -O(CH 3 );-CF 3 ;-CH 2 CF 3 ;-CH 2 CHF 2 ;-CH 2 CH 2 F;-(CH 2 ) d -(4-morpholinyl);-(CH 2 ) d -(1-piperazinyl);-(CH 2 ) d -(4-methylpiperazin-1-yl);4-morpholinyl;4-piperazinyl;4-methyl-piperazin-1-yl; halogen (especially, -F, -Cl, -Br); -NHC(=O) (optionally -NH 2-z (CH 3 ) z substituted C 1-3 alkyl); -NHC(=O)NH 2-z (CH 3 ) z ;-NHS(O) 2 (optionally -NH 2-z (CH 3 ) z substituted C 1-3 alkyl); -C(=O)CH 3 ;-C(=O)CH 2 NH 2-z (CH 3 ) z ;-C(=O)NH 2-z (C 1-3 alkyl) z ;-S(O) 2 (C 1-3 alkyl); -S(O) 2 (CH 2 ) d NH 2-z (CH 3 ) z ;-OH; and -O(C 1-3 alkyl) (z is 0, 1 or 2; d is 1, 2 or 3; C 1-3Alkyl is selected from the group consisting of methyl, ethyl, propyl or isopropyl). In one embodiment, R 9 , when substituting a hydrogen atom bonded to a ring carbon atom of ring A, each independently, methyl; ethyl; isopropyl; cyclopropyl; -(CH 2 ) d -NH 2-z (CH 3 ) z ; -(CH 2 ) d -O(CH 3 ); -CF 3 ; -CH 2 CF 3 ; -CH 2 CHF 2 ; -CH 2 CH 2 F; -NH 2 ; -NH(C 1-3 alkyl); -N(C 1-3 alkyl) 2 ; halogen (especially, -F, -Cl, -Br); -C(=O)CH 3 ; -C(=O)CH 2 NH 2-z (CH 3 ) z ; -C(=O)NH 2-z (C 1-3 alkyl) z ; -S(O) 2 (C 1-3 alkyl); -S(O) 2 (CH 2 ) d NH 2-z (CH 3 ) z ; -OH; and -O(C 1-3 alkyl) (z is 0, 1 or 2; d is 1, 2 or 3; C 1-3 alkyl is selected from the group consisting of methyl, ethyl, propyl or isopropyl). In one embodiment, R 9 , when substituting a hydrogen atom bonded to a ring carbon atom of ring A, each independently, methyl; ethyl; isopropyl; cyclopropyl; -(CH 2 ) d -NH 2-z(CH 3 ) z ;-(CH 2 ) d -O(CH 3 );-CF 3 ;-CH 2 CF 3 ;-CH 2 CHF 2 ;-CH 2 CH 2 F; halogen (especially, -F, -Cl, -Br); -C(=O)CH 3 ;-C(=O)CH 2 NH 2-z (CH 3 ) z ;-C(=O)NH 2-z (C 1-3 alkyl) z ;-S(O) 2 (C 1-3 alkyl);-S(O) 2 (CH 2 ) d NH 2-z (CH 3 ) z ;-OH; and -O(C 1-3 alkyl) (z is 0, 1 or 2; d is 1, 2 or 3; C 1-3 alkyl is methyl, ethyl, propyl or isopropyl) is selected from the group consisting of. In one embodiment, the ring carbon atoms of ring A are unsubstituted or R 9 that replaces the hydrogen atom bonded to the ring carbon atom is each independently C 1-4 alkyl (especially methyl), -N(R 12 )(R 13 ) (especially NH 2 ) and -N(R 14 )C(=O)R 11 (especially NHC(O)CH 3 ) is selected from the group consisting of. In one embodiment, the ring carbon atoms of ring A are unsubstituted or one ring carbon atom of ring A is substituted with one R 2 that is NH 3 or CH 9 , or two R 3 that are CH 9 .

[0103] R 9 In any of the above embodiments of the spiroquinoxaline derivative of formula (O / S-II) where R is attached to the ring sulfur atom of ring A, such R 9 may each independently be selected from the group consisting of C 1-6 alkyl, C 2-6 alkenyl, C 2-6 alkynyl, 5- or 6-membered aryl, 5- or 6-membered heteroaryl, 3- to 7-membered cycloalkyl, 3- to 7-membered heterocyclyl, -OR 11 and =O, wherein the C 1-6 alkyl, C 2-6 alkenyl, C 2-6 alkynyl, 5- or 6-membered aryl, 5- or 6-membered heteroaryl, 3- to 7-membered cycloalkyl and 3- to 7-membered heterocyclyl groups may each optionally be substituted with one or more (e.g., 1 to the maximum number of hydrogen atoms attached to the C 1-6 alkyl, C 2-6 alkenyl, C 2-6 alkynyl, 5- or 6-membered aryl, 5- or 6-membered heteroaryl, 3- to 7-membered cycloalkyl or 3- to 7-membered heterocyclyl group, e.g., up to 1, 2, 3, 4, 5, 6, 7, 8, 9 or 10, e.g., between 1 and 5, 1 and 4 or 1 and 3, or 1 or 2) independently selected R 30 groups. In any of the above embodiments of the spiroquinoxaline derivative of formula (O / S-II) where R is attached to the ring sulfur atom of ring A, such R 9 may each independently be selected from the group consisting of C 9 alkyl, C 1-4 alkenyl, C 2-4 alkynyl, 6-membered aryl, 5- or 6-membered heteroaryl, 3, 5, 6 or 7-membered cycloalkyl, 3, 5, 6 or 7-membered heterocyclyl, -OR 2-4 and =O, wherein the C 11 alkyl, C 1-4 alkenyl, C 2-4 alkynyl, 6-membered aryl, 5- or 6-membered heteroaryl, 3, 5, 6 or 7-membered cycloalkyl and 3, 5, 6 or 7-membered heterocyclyl groups may each optionally be substituted with one or more (e.g., 1 to the maximum number of hydrogen atoms attached to the C 2-4The alkynyl, 6-membered aryl, 5- or 6-membered heteroaryl, 3-, 5-, 6- or 7-membered cycloalkyl and 3-, 5-, 6- or 7-membered heterocyclyl groups are each optionally substituted with one, two or three independently selected R 30 groups. In one embodiment, R 9 , when attached to the ring sulfur atom of Ring A, are each independently methyl, ethyl, C 3 alkyl, C 4 alkyl, -OR 11’ and =O (wherein R 11’ is selected from the group consisting of -H, C 1-6 alkyl, C 2-6 alkenyl, C 2-6 alkynyl, 3- to 7-membered cycloalkyl, 5- or 6-membered aryl (e.g., phenyl), 5- or 6-membered heteroaryl and 3- to 7-membered heterocyclyl), and wherein the methyl, ethyl, C 3 alkyl, C 4 alkyl, C 1-6 alkyl, C 2-6 alkenyl, C 2-6 alkynyl, 3- to 7-membered cycloalkyl, 5- or 6-membered aryl, 5- or 6-membered heteroaryl and 3- to 7-membered heterocyclyl groups are each optionally substituted with one, two or three independently selected R 30’ groups (wherein R 30’ is a first, second or third level substituent as previously specified (in particular, one of the exemplary first, second or third level substituents as previously specified), and in each case is phenyl, furanyl, pyrrolyl, thienyl, imidazolyl, oxazolyl, isoxazolyl, thiazolyl, pyridyl, pyrazinyl, pyrimidinyl, pyridazinyl, the partially and fully hydrogenated forms of the foregoing groups, morpholino, C 1-3 alkyl, halogen, -CF 3 , -OH, -OCH 3 , -SCH 3 , -NH 2-z (CH 3 ) z , -C(=O)OH and -C(=O)OCH 3 (where z is 0, 1 or 2) and may be selected from the group consisting thereof). In one embodiment, R9 When bonded to the ring sulfur atom of ring A, each is independently methyl; ethyl; isopropyl; benzyl; -OH; =O; and -O(C 1-3 alkyl)(C 1-3 alkyl is methyl, ethyl, propyl or isopropyl) and is selected from the group consisting of. In one embodiment, the ring sulfur atom of ring A is unsubstituted or substituted with two =O groups. In one embodiment, the ring sulfur atom of ring A is unsubstituted or ring A contains one sulfur atom substituted with two =O groups (i.e., ring A is the group -S(=O) 2 - containing).

[0104] In one embodiment, the spiroquinoxaline derivative has the following general formula (O / S-III):

Chemical formula

[0105] In one embodiment, the spiroquinoxaline derivative has the following general formula (O / S-IV): [Chemical formula] [wherein, R 1 ~R 5 , rings A, E, and L are synonymous with the above (especially for formulas (O / S-I), (O / S-II), and (O / S-III)) or the following, G is unsubstituted or phenyl substituted with 1, 2, 3, 4, or 5 (e.g., between 1 and 4 or 1 and 3, or 1 or 2) independently selected R 8 . In any of the above embodiments (including those of formulas (O / S-I) to (O / S-III)) where G is substituted, R 8 is in each case C 1-6 alkyl, C 2-6 alkenyl, C 2-6 alkynyl, 5- or 6-membered aryl, 5- or 6-membered heteroaryl, 3- to 7-membered cycloalkyl, 3- to 7-membered heterocyclyl, halogen, -CN, -OR 11 , -N(R​12 )(R 13 )、 -S(O) 0-2 R 11 、 -S(O) 1-2 N(R 12 )(R 13 )、 -N(R 11 )S(O) 1-2 R 11 、 -NR 11 S(O) 1-2 N(R 12 )(R 13 )、 -C(=X)R 11 、 -C(=X)XR 11 、 -XC(=X)R 11 and -XC(=X)XR 11 may be selected from the group consisting of, wherein said C 1-6 alkyl, C 2-6 alkenyl, C 2-6 alkynyl, 5- or 6-membered aryl, 5- or 6-membered heteroaryl, 3- to 7-membered cycloalkyl and 3- to 7-membered heterocyclyl group may each, optionally, have one or more (e.g., 1 to the maximum number of hydrogen atoms bonded to the C 1-6 alkyl, C 2-6 alkenyl, C 2-6 alkynyl, 5- or 6-membered aryl, 5- or 6-membered heteroaryl, 3- to 7-membered cycloalkyl or 3- to 7-membered heterocyclyl group, e.g., 1, 2, 3, 4, 5, 6, 7, 8, 9 or 10, e.g., between 1 and 5, 1 and 4 or 1 and 3, or 1 or 2) independently selected R 30 substituents. In one embodiment of the spiroquinoxaline derivative of formula (O / S-IV), R 1 ~R 5 , ring A, E and L are as defined above (in particular, for formulas (O / S-I), (O / S-II) and (O / S-III)) or have the same meaning as below, and R 8 is in each case C 1-4 alkyl, C 2-4 alkenyl, C 2-4 alkynyl, 6-membered aryl, 5- or 6-membered heteroaryl, 3, 5, 6 or 7-membered cycloalkyl, 3, 5, 6 or 7-membered heterocyclyl, halogen, -CN, -OR 11 , -N(R 12 )(R13 )、 -S(O) 0-2 R 11 、 -S(O) 1-2 N(R 12 )(R 13 )、 -N(R 11 )S(O) 1-2 R 11 、 -NR 11 S(O) 1-2 N(R 12 )(R 13 )、 -C(=O)R 11 、 -C(=O)OR 11 、 -C(=O)SR 11 、 -C(=O)N(R 14 )(R 11 )、 -C(=S)OR 11 、 -N(R 14 )C(=O)R 11 、 -OC(=O)R 11 、 -OC(=S)R 11 、 -N(R 14 )C(=O)N(R 14 )(R 11 ) and -N(R 14 )(C=N(R 14 ))N(R 14 )(R 11 ) selected from the group consisting of, wherein said C 1-4 alkyl, C 2-4 alkenyl, C 2-4 alkynyl, 6-membered aryl, 5- or 6-membered heteroaryl, 3-, 5-, 6- or 7-membered cycloalkyl and 3-, 5-, 6- or 7-membered heterocyclyl groups are each, optionally, substituted with 1, 2 or 3 independently selected R 30 s. In one embodiment of the spiroquinoxaline derivative of formula (O / S-IV), R 1 ~R 5 , ring A, E and L are as defined above (in particular, for formulas (O / S-I), (O / S-II) and (O / S-III)) or synonymous with the following, and R 8 is, in each case, C 1-4 alkyl; -OH, -O(C 1-3 alkyl) and -NH 2-z (CH 3 ) zC substituted with 1 substituent selected from the group consisting of 1-4 alkyl; -CF 3 ; -CH 2 CF 3 ; -CH 2 CHF 2 or -CH 2 CH 2 F such as C alkyl substituted with 1, 2 or 3 halogens (preferably F); phenyl; cyclopropyl; 5 - membered heterocyclyl (e.g., pyrrolidinyl); 4 - morpholinyl; homomorpholinyl; 4 - piperidinyl; homopiperidinyl; 4 - piperazinyl; homopiperazinyl; N - methyl - piperazin - 4 - yl; N - methyl - homopiperazinyl; halogen; -CN; -OH; -O(C 1-4 alkyl); -OCF 1-3 ; -OCH 3 CF 2 ; -OCH 3 CHF 2 or -OCH 2 CH 2 F such as -O(C alkyl substituted with 1, 2 or 3 halogens (preferably F)); -O - phenyl; -NH 2 ; -NH(C 1-4 alkyl); -N(C 2 alkyl) 1-3 ; -S(C 1-3 alkyl); -S(O) 2 (optionally -NH 1-3 (CH 2 ) 2-z substituted C 3 alkyl); -S(O) z NH 1-3 (C 2 alkyl) 2-z ; -NHS(O) 1-3 (C z alkyl); -C(=O) (optionally -NH 2 (CH 1-3 ) 2-z substituted C 3 alkyl); -C(=O)OH; -C(=O)O(C z alkyl); -C(=O)NH 1-3 ; -C(=O)O 1-3 alkyl); -C(=O)NH2-z (C 1-3 alkyl) z ;-NHC(=O)(C 1-3 alkyl);-NHC(=NH)NH z-2 (C 1-3 alkyl) z ; and -N(C 1-3 alkyl)C(=NH)NH 2-z (C 1-3 alkyl) z (z is 0, 1, or 2, and C 1-3 alkyl is methyl, ethyl, propyl, or isopropyl) selected from the group consisting of, and the phenyl, cyclopropyl, 5-membered heterocyclyl (e.g., pyrrolidinyl), 4-morpholinyl, homomorpholinyl, 4-piperidinyl, homopiperidinyl, 4-piperazinyl, homopiperazinyl, N-methyl-piperazin-4-yl, N-methyl-homopiperazinyl, and -O-phenyl groups are each optionally C 1-3 alkyl, halogen, -CF 3 , -OCF 3 , -OH, -OCH 3 , -SCH 3 , -NH 2-z (CH 3 ) z , -C(=O)OH, and -C(=O)OCH 3 (z is 0, 1, or 2) independently selected from the group consisting of 1, 2, or 3 substituents. In one embodiment, R 8 is each independently methyl; ethyl; isopropyl; tert-butyl; phenyl; cyclopropyl; pyrrolidinyl (e.g., 4-pyrrolidinyl); -(CH 2 ) d -NH 2-z (CH 3 ) z ; -(CH 2 ) d -O(CH 3 ); -CF 3 ; -OCF 3 ; -O-phenyl; -CH 2 CF 3 ; -CH 2 CHF 2 ; -CH 2 CH2 F; halogen (especially -F, -Cl, -Br); -CN; -NH 2 ; -NH(C 1-3 alkyl); -N(C 1-3 alkyl) 2 ; -C(=O)CH 3 ; -C(=O)CH 2 NH 2-z (CH 3 ) z ; -C(=O)OH; -C(=O)O(C 1-3 alkyl); -C(=O)NH 2-z (C 1-3 alkyl) z ; -NHC(=O)(C 1-3 alkyl); -S(O) 2 (C 1-3 alkyl); -S(O) 2 (CH 2 ) d NH 2-z (CH 3 ) z ; -OH; and -O(C 1-3 alkyl) (z is 0, 1, or 2, d is 1, 2, or 3, and C 1-3 alkyl is methyl, ethyl, propyl, or isopropyl) and is selected from the group consisting of. In one embodiment, R 8 is, independently of each other, methyl; ethyl; isopropyl; phenyl; cyclopropyl; pyrrolidinyl (e.g., 4-pyrrolidinyl); -(CH 2 ) d -NH 2-z (CH 3 ) z ; -(CH 2 ) d -O(CH 3 ); -CF 3 ; -OCF 3 ; -O-phenyl; -CH 2 CF 3 ; -CH 2 CHF 2 ; -CH 2 CH 2 F; halogen (especially -F, -Cl, -Br); -CN; -NH 2 ; -NH(C 1-3-N(alkyl); -N(C 1-3 alkyl) 2 -C(=O)CH 3 -C(=O)CH 2 NH 2-z (CH 3 ) z -C(=O)OH; -C(=O)O(C 1-3 alkyl); -C(=O)NH 2-z (C 1-3 alkyl) z -NHC(=O)(C 1-3 alkyl); -S(O) 2 (C 1-3 alkyl); -S(O) 2 (CH 2 ) d NH 2-z (CH 3 ) z -OH; and -O(C 1-3 alkyl) (z is 0, 1 or 2, d is 1, 2 or 3, and C 1-3 alkyl is methyl, ethyl, propyl or isopropyl) and is selected from the group consisting of. In one embodiment of the spiroquinoxaline derivative of formula (O / S-IV), R 1 ~R 5 , ring A, E and L are as defined above (in particular for formulas (O / S-I), (O / S-II) and (O / S-III)) or have the same meaning as below, G is unsubstituted or substituted with 1, 2 or 3 R 8 's, where R 8 is in each case C 1-4 alkyl (especially methyl or tert-butyl); halogen (especially F or Cl); -OR 11 (especially -OCH 3 ); and C 30 alkyl substituted with 1, 2 or 3 independently selected R 1-4 (especially -CF 3 ) and is selected from the group consisting of. In one embodiment of the spiroquinoxaline derivative of formula (O / S-IV), R 1 ~R 5, rings A, E and L are synonymous with the above (especially for formulas (O / S-I), (O / S-II) and (O / S-III)) or the following, and G is unsubstituted or is methyl, F, Cl, -OCH 3 and -CF 3 One or two Rs each independently selected from the group consisting of 8 are substituted. In one embodiment of the spiroquinoxaline derivative of formula (O / S-IV), R 1 ~R 5 , rings A, E and L are synonymous with the above (especially for formulas (O / S-I), (O / S-II) and (O / S-III)) or the following, and G is unsubstituted phenyl, fluorophenyl (especially 3-fluorophenyl), chlorophenyl (especially 2-, 3- or 4-chlorophenyl), methylphenyl (especially 2- or 3-methylphenyl), tert-butylphenyl (especially 4-tert-butylphenyl), methoxyphenyl (especially 3-methoxyphenyl), (trifluoromethyl)phenyl (especially 3- or 4-(trifluoromethyl)phenyl), difluorophenyl (especially 2,4- or 2,6-difluorophenyl), dichlorophenyl (especially 2,4- or 3,4-dichlorophenyl), chlorofluorophenyl (especially 4-chloro-2-fluorophenyl) and dimethylphenyl (especially 3,5-dimethylphenyl) selected from the group consisting of. In one embodiment of the spiroquinoxaline derivative of formula (O / S-IV), R 1 ~R 5 , rings A, E and L are synonymous with the above (especially for formulas (O / S-I), (O / S-II) and (O / S-III)) or the following, and G is selected from the group consisting of unsubstituted phenyl, 2-chlorophenyl, 3-chlorophenyl, 4-chlorophenyl, 3-methylphenyl, 3-(trifluoromethyl)phenyl, 2,6-difluorophenyl, 3,4-dichlorophenyl, 4-chloro-2-fluorophenyl and 3,5-dimethylphenyl.

[0106] In one embodiment, the spiroquinoxaline derivative has the following general formula (O / S-V):

Chemical formula

[0107] In any of the above embodiments (particularly, for formulas (O / S-I), (O / S-II), (O / S-III), (O / S-IV) and (O / S-V)), when R 2 ~R 5 do not form a ring together with another R 2 ~R 5 each independently is -H, C 1-6 alkyl, C 2-6 alkenyl, C 2-6Alkynyl, 5- or 6-membered aryl, 5- or 6-membered heteroaryl, 3- to 7-membered cycloalkyl, 3- to 7-membered heterocyclyl, halogen, -CN, -OR 11 , -N(R 12 )(R 13 ), -S(O) 0-2 R 11 , -S(O) 1-2 N(R 12 )(R 13 ), -N(R 11 )S(O) 1-2 R 11 , -NR 11 S(O) 1-2 N(R 12 )(R 13 ), -C(=X)R 11 , -C(=X)XR 11 , -XC(=X)R 11 and -XC(=X)XR 11 selected from the group consisting of, wherein the C 1-6 alkyl, C 2-6 alkenyl, C 2-6 alkynyl, 5- or 6-membered aryl, 5- or 6-membered heteroaryl, 3- to 7-membered cycloalkyl and 3- to 7-membered heterocyclyl groups each, optionally, one or more (e.g., 1 to the C 1-6 alkyl, C 2-6 alkenyl, C 2-6 alkynyl, 5- or 6-membered aryl, 5- or 6-membered heteroaryl, 3- to 7-membered cycloalkyl or 3- to 7-membered heterocyclyl group binds to the maximum number of hydrogen atoms, e.g., 1, 2, 3, 4, 5, 6, 7, 8, 9 or 10, e.g., between 1 and 5, 1 and 4 or 1 and 3, or 1 or 2) independently selected R 30 substituted. In one embodiment, R 2 , R 3 , R 4 and R 5 when not taken together with another one of R 2 ~R 5 to form a ring, each independently, -H, C 1-4 alkyl, C 2-4 alkenyl, C 2-4alkynyl, 6-membered aryl, 5- or 6-membered heteroaryl, 3-, 5-, 6- or 7-membered cycloalkyl, 3-, 5-, 6- or 7-membered heterocyclyl, halogen, -CN, -OR 11 , -N(R 12 )(R 13 ), -S(O) 0-2 R 11 , -S(O) 1-2 N(R 12 )(R 13 ), -N(R 11 )S(O) 1-2 R 11 , -NR 11 S(O) 1-2 N(R 12 )(R 13 ), -C(=O)R 11 , -C(=O)OR 11 , -C(=O)SR 11 , -C(=O)N(R 14 )(R 11 ), -C(=S)OR 11 , -N(R 14 )C(=O)R 11 , -OC(=O)R 11 , -OC(=S)R 11 , -N(R 14 )C(=O)N(R 14 )(R 11 ) and -N(R 14 )(C=N(R 14 ))N(R 14 )(R 11 ) and may be selected from the group consisting of, wherein the C 1-4 alkyl, C 2-4 alkenyl, C 2-4 alkynyl, 6-membered aryl, 5- or 6-membered heteroaryl, 3-, 5-, 6- or 7-membered cycloalkyl and 3-, 5-, 6- or 7-membered heterocyclyl group may each optionally be substituted with one, two or three independently selected R 30 . In one embodiment of the spiroquinoxaline derivative of formula (O / S-V), R 1 , ring A, E, L and G are as defined above (in particular for formulae (O / S-I), (O / S-II), (O / S-III) and (O / S-IV)) or are synonymous with those below, R 2 , R 3, R 4 and R 5 do not form a ring together with another R 2 ~R 5 each is independently selected from the group consisting of H; C 1-4 alkyl; -OH, -O(C 1-3 alkyl) and -NH 2-z (CH 3 ) z substituted with one substituent selected from the group consisting of C 1-4 alkyl; -CF 3 , -CH 2 CF 3 , -CH 2 CHF 2 or -CH 2 CH 2 F, i.e., C 1-4 alkyl substituted with one, two or three halogens (preferably F); phenyl; cyclopropyl; 5-membered heterocyclyl; 4-morpholinyl; homomorpholinyl; 4-piperidinyl; homopiperidinyl; 4-piperazinyl; homopiperazinyl; N-methyl-piperazin-4-yl; N-methyl-homopiperazinyl; halogen; -CN; -OH; -O(C 1-3 alkyl); -OCF 3 , -OCH 2 CF 3 , -OCH 2 CHF 2 or -OCH 2 CH 2 F, i.e., -O(C 1-4 alkyl substituted with one, two or three halogens (preferably F); -O-phenyl; -NH 2 -; -NH(C 1-3 alkyl); -N(C 1-3 alkyl) 2 -; -S(C 1-3 alkyl); -S(O) 2 (optionally -NH 2-z (CH 3 ) z substituted C 1-3 alkyl); -S(O) 2 NH 2-z (C 1-3 alkyl) z -; -NHS(O)2 (C 1-3 alkyl); -C(=O)(optionally -NH 2-z (CH 3 ) z substituted C 1-3 alkyl); -C(=O)OH; -C(=O)O(C 1-3 alkyl); -C(=O)NH 2-z (C 1-3 alkyl) z ; -NHC(=O)(C 1-3 alkyl); -NHC(=NH)NH z-2 (C 1-3 alkyl) z ; and -N(C 1-3 alkyl)C(=NH)NH 2-z (C 1-3 alkyl) z (z is 0, 1, or 2, and C 1-3 alkyl is methyl, ethyl, propyl, or isopropyl) selected from the group consisting of, and the phenyl, cyclopropyl, 5 - membered heterocyclyl, 4 - morpholinyl, homomorpholinyl, 4 - piperidinyl, homopiperidinyl, 4 - piperazinyl, homopiperazinyl, N - methyl - piperazin - 4 - yl, N - methyl - homopiperazinyl, and -O - phenyl groups are each optionally C 1-3 alkyl, halogen, -CF 3 , -OCF 3 , -OH, -OCH 3 , -SCH 3 , -NH 2-z (CH 3 ) z , -C(=O)OH, and -C(=O)OCH 3 (z is 0, 1, or 2) independently selected from the group consisting of 1, 2, or 3 substituents. In one embodiment, R 2 , R 3 , R 4 and R 5 are, when not forming a ring together with another one of R 2 ~R 5 , each independently, H; methyl; ethyl; isopropyl; phenyl; cyclopropyl; -(CH 2 ) d -NH2-z (CH 3 ) z ;-(CH 2 ) d -O(CH 3 );-CF 3 ;-OCF 3 ;-CH 2 CF 3 ;-CH 2 CHF 2 ;-CH 2 CH 2 F; halogen (especially, -F, -Cl, -Br); -CN; -NH 2 ;-NH(C 1-3 alkyl); -N(C 1-3 alkyl) 2 ;-C(=O)CH 3 ;-C(=O)CH 2 NH 2-z (CH 3 ) z ;-C(=O)O(C 1-3 alkyl); -C(=O)NH 2-z (C 1-3 alkyl) z ;-NHC(=O)(C 1-3 alkyl); -S(O) 2 (C 1-3 alkyl); -S(O) 2 (CH 2 ) d NH 2-z (CH 3 ) z ;-OH and -O(C 1-3 alkyl) (z is 0, 1 or 2; d is 1, 2 or 3; C 1-3 alkyl is methyl, ethyl, propyl or isopropyl) are selected from the group consisting of. In one embodiment of the spiroquinoxaline derivative of formula (O / S-V), R 1 , ring A, E, L and G are as defined above (especially for formulas (O / S-I), (O / S-II), (O / S-III) and (O / S-IV)) or synonymous with the following, and R 2 , R 3 , R 4 and R 5 are independently -H, C 1-4Selected from the group consisting of alkyl and halogen, wherein said C 1-4 alkyl group is optionally substituted with one, two or three independently selected R 30 (in particular, R 2 and R 5 are each -H). In one embodiment of the spiroquinoxaline derivative of formula (O / S-V), R 1 , ring A, E, L and G are as defined above (in particular for formulae (O / S-I), (O / S-II), (O / S-III) and (O / S-IV)) or have the same meaning as below, and R 2 , R 3 , R 4 and R 5 are independently selected from the group consisting of -H, methyl, F, Cl and CF 3 (in particular, R 2 and R 5 are each -H). In one embodiment of the spiroquinoxaline derivative of formula (O / S-V), R 1 , ring A, E, L and G are as defined above (in particular for formulae (O / S-I), (O / S-II), (O / S-III) and (O / S-IV)) or have the same meaning as below, R 2 and R 5 are each -H, R 3 is selected from the group consisting of -H, methyl, F and Cl, and R 4 is selected from the group consisting of -H, methyl, F and Cl. In one embodiment of the spiroquinoxaline derivative of formula (O / S-V), R 1 , ring A, E, L and G are as defined above (in particular for formulae (O / S-I), (O / S-II), (O / S-III) and (O / S-IV)) or have the same meaning as below, (i) R 2 to R 5 are each H; or, (ii) R 2 and R 5 are each -H, and both R 3 and R 4 are F, Cl or methyl.

[0108] (i) R 2 and R 3 , (ii) R 3 and R4 and / or (iii) R 4 and R 5 In any of the above embodiments, where a ring is formed by, the ring is preferably optionally substituted with one or more (e.g., 1 to the maximum number of hydrogen atoms bonded to the ring, e.g., up to 1, 2, 3, 4, 5, 6, 7, 8, 9 or 10, e.g., between 1 and 5, 1 and 4 or 1 and 3, or 1 or 2) independently selected R 30 and is a 3- to 7-membered ring (e.g., a ring having 5 or 6 members). The ring may be aromatic, cycloaliphatic, heteroaromatic or heterocyclic (the heteroaromatic / heterocyclic ring contains one or two heteroatoms selected from the group consisting of O, S and N(R 40 )(R 40 is as defined for R 11 , -OR 11 , -NH y R 20 2-y and -S(O) 1-2 R 11 (R 11 , R 20 and y are as defined above) and is selected from the group consisting of) and contains one or two heteroatoms selected from the group consisting of). In one embodiment, (i) R 2 and R 3 , (ii) R 3 and R 4 , and / or (iii) R 4 and R 5 forms a 5- or 6-membered aromatic, cycloaliphatic, heteroaromatic or heterocyclic ring, the heteroaromatic / heterocyclic ring contains one or two heteroatoms selected from the group consisting of O, S and N, and at least one heteroatom is N. In one embodiment, (i) R 2 and R 3 , (ii) R 3 and R 4 , and / or (iii) R 4 and R 5The ring formed thereby is selected from the group consisting of cyclopentadiene, furan, pyrrole, thiophene, imidazole, pyrazole, oxazole, isoxazole, thiazole, dioxole (e.g., 1,3-dioxole), benzene, pyridine, pyrazine, pyrimidine, pyridazine, dioxine (e.g., 1,4-dioxine), 1,2,3-triazine, 1,2,4-triazine, and the di- or tetrahydro forms of each of the foregoing. In one embodiment, (i) R 2 and R 3 , (ii) R 3 and R 4 , and / or (iii) R 4 and R 5 form a ring that is cyclopentene (e.g., 2,3-dihydrocyclopentadiene), dioxole (e.g., 1,3-dioxole optionally substituted at the 2-position with one or two halogen atoms (e.g., F)), or dioxine (e.g., 2,3-dihydro-[1,4]-dioxine). In one embodiment, (i) R 2 and R 3 , (ii) R 3 and R 4 , and / or (iii) R 4 and R 5 form a total of 0 or 1 ring. Thus, in embodiments where (i) R 2 and R 3 , (ii) R 3 and R 4 , and / or (iii) R 4 and R 5 form a total of 1 ring, only two adjacent substituents (i.e., either (i) R 2 and R 3 , (ii) R 3 and R 4 , or (iii) R 4 and R 5 ) together with the atoms to which they are attached form a ring, where the ring is as defined in any of the foregoing embodiments, and R 2 ~R 5The remainder is selected from the group of specific moieties previously identified for the situation where they do not combine to form a ring. For example, R 2 ~R 5 The remainder is -H, C 1-6 alkyl, C 2-6 alkenyl, C 2-6 alkynyl, 5- or 6-membered aryl, 5- or 6-membered heteroaryl, 3- to 7-membered cycloalkyl, 3- to 7-membered heterocyclyl, halogen, -CN, -OR 11 , -N(R 12 )(R 13 ), -S(O) 0-2 R 11 , -S(O) 1-2 N(R 12 )(R 13 ), -N(R 11 )S(O) 1-2 R 11 , -NR 11 S(O) 1-2 N(R 12 )(R 13 ), -C(=X)R 11 , -C(=X)XR 11 , -XC(=X)R 11 and -XC(=X)XR 11 and may be selected from, where the C 1-6 alkyl, C 2-6 alkenyl, C 2-6 alkynyl, 5- or 6-membered aryl, 5- or 6-membered heteroaryl, 3- to 7-membered cycloalkyl and 3- to 7-membered heterocyclyl groups are each optionally substituted with one or more (e.g., 1 to the maximum number of hydrogen atoms bonded to the C 1-6 alkyl, C 2-6 alkenyl, C 2-6 alkynyl, 5- or 6-membered aryl, 5- or 6-membered heteroaryl, 3- to 7-membered cycloalkyl or 3- to 7-membered heterocyclyl group, e.g., 1, 2, 3, 4, 5, 6, 7, 8, 9 or 10, e.g., between 1 and 5, 1 and 4 or 1 and 3, or 1 or 2) independently selected R 30 groups. In another embodiment, R 2 ~R 5 do not combine to form a ring.

[0109] In any of the above embodiments, R 2 and R 5 may be the same, and / or R 3 and R 4 may be the same.

[0110] In one embodiment of the spiroquinoxaline derivative of formula (O / S-V), R 1 , ring A, E, L and G are as defined above (in particular for formulas (O / S-I), (O / S-II), (O / S-III) and (O / S-IV)) or have the same meaning as below, and R 2 , R 3 , R 4 and R 5 are independently selected from the group consisting of -H, C 1-4 alkyl and halogen, where the C 1-4 alkyl is optionally substituted with one, two or three independently selected R 30 (in particular where R 2 and R 5 are each -H), or R 3 and R 4 together with the atom to which they are attached may form a 5- or 6-membered ring optionally substituted with one or two independently selected R 30 . In one embodiment of the spiroquinoxaline derivative of formula (O / S-V), R 1 , ring A, E, L and G are as defined above (in particular for formulas (O / S-I), (O / S-II), (O / S-III) and (O / S-IV)) or have the same meaning as below, and R 2 , R 3 , R 4 and R 5 are independently selected from the group consisting of -H, methyl, F, Cl and CF 3 (in particular where R 2 and R 5 are each -H), or R 3 and R 4together with the atoms to which they are attached may form, optionally substituted by one or two independently selected halogens (especially F), a dioxole or dioxine ring. In one embodiment of the spiroquinoxaline derivative of formula (O / S-V), R 1 ring A, E, L and G are as defined above (especially for formulas (O / S-I), (O / S-II), (O / S-III) and (O / S-IV)) or as defined below, R 2 and R 5 are each -H; R 3 is selected from the group consisting of -H, methyl, F and Cl; R 4 is selected from the group consisting of -H, methyl, F and Cl; or R 3 and R 4 together with the atoms to which they are attached may form a dioxole (especially 1,3-dioxole) or dioxine (especially 2,3-dihydro-[1,4]-dioxine) ring, which dioxole ring may optionally be substituted by two Fs. In one embodiment of the spiroquinoxaline derivative of formula (O / S-V), R 1 ring A, E, L and G are as defined above (especially for formulas (O / S-I), (O / S-II), (O / S-III) and (O / S-IV)) or as defined below, (i) R 2 to R 5 are each -H; (ii) R 2 and R 5 are each -H and both R 3 and R 4 are F, Cl or methyl; or (iii) R 2 and R 5 are each -H and R 3 and R 4 together with the atoms to which they are attached form a 2,2-difluoro-1,3-dioxole ring or a 2,3-dihydro-[1,4]-dioxine ring.

[0111] In any of the above embodiments (particularly for formulas (O / S-I), (O / S-II), (O / S-III), (O / S-IV) and (O / S-V)), R 30 may in each case be a previously specified typical first, second or third level substituent and independently be C 1-4 alkyl, C 2-4 alkenyl, C 2-4 alkynyl, 5- or 6-membered aryl, 5- or 6-membered heteroaryl, 5- or 6-membered cycloalkyl, 5-, 6- or 7-membered heterocyclyl, halogen, -CF 3 , -CN, azide, -NO 2 , -OH, -O(C 1-3 alkyl), -S(C 1-3 alkyl), -NH 2 , -NH(C 1-3 alkyl), -N(C 1-3 alkyl) 2 , -NHS(O) 2 (C 1-3 alkyl), -S(O) 2 NH 2-z (C 1-3 alkyl) z , -C(=O)OH, -C(=O)O(C 1-3 alkyl), -C(=O)NH 2-z (C 1-3 alkyl) z , -NHC(=O)(C 1-3 alkyl), -NHC(=NH)NH z-2 (C 1-3 alkyl) z and -N(C 1-3 alkyl)C(=NH)NH 2-z (C 1-3 alkyl) z (z is 0, 1 or 2, and C 1-3 alkyl is methyl, ethyl, propyl or isopropyl) selected from the group consisting of (e.g., 4-morpholinyl, homomorpholinyl, 4-piperidinyl, homopiperidinyl (i.e., azepanyl, particularly 4-azepanyl), 4-piperazinyl, homopiperazinyl (i.e., diazepanyl, particularly 2,4-diazepanyl), N-methyl-piperazin-4-yl, N-methyl-homopiperazinyl, -CH 2CH 2 OCH 3 、 -OCH 2 CH 2 OCH 3 、 -CH 2 CH 2 NH 2-z (CH 3 ) z 、 -OCH 2 CH 2 NH 2-z (CH3) z 、 -CF 3 、 -OCF 3 ) may be. Alternatively, R 30 is phenyl, furanyl, pyrrolyl, thienyl, imidazolyl, oxazolyl, isoxazolyl, thiazolyl, pyridyl, pyrazinyl, pyrimidinyl, pyridazinyl, the partially and fully hydrogenated forms of the above groups, morpholino, C 1-3 alkyl, halogen, -CF 3 、 -OH, -OCH 3 、 -OCF 3 、 -SCH 3 、 -NH 2-z (CH 3 ) z 、 -C(=O)OH and -C(=O)OCH 3 (z is 0, 1 or 2) and may be selected from the group consisting of.

[0112] In one embodiment, the spiroquinoxaline derivative has the following general formula (C-I): [Chemical formula] [wherein, E is -N(R 6 )-; L is C 1-10 alkylene, C 2-10 alkenylene, C 2-10 alkynylene, 1,1-(CH 2 ) a -cyclopropylene-(CH 2 ) b -(wherein a and b are each independently selected from integers between 0 and 3) and -(CH 2 )m -[Y-(CH 2 ) n o -(wherein m is an integer between 1 and 6, n is an integer between 0 and 3, o is an integer between 1 and 3, and when n is 0, o is 1, and Y is independently selected from the group consisting of O, S, and -N(R 7 )) 1-10 alkylene, C 2-10 alkenylene, C 2-10 alkynylene, 1,1 - cyclopropylene, -(CH 2 ) m - and -(CH 2 ) n - groups are each optionally substituted with one or more (e.g., 1 to the maximum number of hydrogen atoms bonded to the C 1-10 alkylene, C 2-10 alkenylene, C 2-10 alkynylene, 1,1 - cyclopropylene, -(CH 2 ) m - or -(CH 2 ) n - group, e.g., up to 1, 2, 3, 4, 5, 6, 7, 8, 9, or 10, e.g., between 1 and 5, 1 and 4, or 1 and 3, or 1 or 2) independently selected R 30 ; G is optionally phenyl substituted with one, two, three, four, or five independently selected R 8 ; Ring A is optionally a monocyclic 3 - to 10 - membered cycloalkylene substituted with one or more (e.g., 1 to the maximum number of hydrogen atoms bonded to ring A, e.g., up to 1, 2, 3, 4, 5, 6, 7, 8, 9, or 10, e.g., between 1 and 5, 1 and 4, or 1 and 3, or 1 or 2) independently selected R 9 ; R 1 is H; R 2 , R 3 , R 4 and R 5 ​is, independently, -H, alkyl, alkenyl, alkynyl, aryl, heteroaryl, cycloalkyl, heterocyclyl, halogen, -CN, azide, -NO 2 , -OR 11 , -N(R 12 )(R 13 ), -N(R 11 )(OR 11 ), -S(O) 0-2 R 11 , -S(O) 1-2 OR 11 , -OS(O) 1-2 R 11 , -OS(O) 1-2 OR 11 , -S(O) 1-2 N(R 12 )(R 13 ), -OS(O) 1-2 N(R 12 )(R 13 ), -N(R 11 )S(O) 1-2 R 11 , -NR 11 S(O) 1-2 OR 11 , -NR 11 S(O) 1-2 N(R 12 )(R 13 ), -C(=X)R 11 , -C(=X)XR 11 , -XC(=X)R 11 and -XC(=X)XR 11 is selected from the group consisting of, wherein the alkyl, alkenyl, alkynyl, aryl, heteroaryl, cycloalkyl and heterocyclyl groups are each optionally, one or more (e.g., 1 to the maximum number of hydrogen atoms bonded to the alkyl, alkenyl, alkynyl, aryl, heteroaryl, cycloalkyl or heterocyclyl group, e.g., 1, 2, 3, 4, 5, 6, 7, 8, 9 or 10, e.g., between 1 and 5, 1 and 4 or 1 and 3, or 1 or 2) independently selected R 30 substituted, or; R 2 and R 3may, together with the atoms to which they are attached, form a ring optionally substituted with one or more (e.g., 1 to the maximum number of hydrogen atoms attached to the ring, e.g., up to 1, 2, 3, 4, 5, 6, 7, 8, 9, or 10, e.g., between 1 and 5, 1 and 4, or 1 and 3, or 1 or 2) independently selected R 30 ; R 3 and R 4 may, together with the atoms to which they are attached, form a ring optionally substituted with one or more (e.g., 1 to the maximum number of hydrogen atoms attached to the ring, e.g., up to 1, 2, 3, 4, 5, 6, 7, 8, 9, or 10, e.g., between 1 and 5, 1 and 4, or 1 and 3, or 1 or 2) independently selected R 30 ; and / or R 4 and R 5 may, together with the atoms to which they are attached, form a ring optionally substituted with one or more (e.g., 1 to the maximum number of hydrogen atoms attached to the ring, e.g., up to 1, 2, 3, 4, 5, 6, 7, 8, 9, or 10, e.g., between 1 and 5, 1 and 4, or 1 and 3, or 1 or 2) independently selected R 30 ; R 6 is H; R 7 is selected from the group consisting of -H, alkyl, alkenyl, alkynyl, cycloalkyl, aryl, heteroaryl, heterocyclyl, -OR 11 and -NHR 20 , wherein the alkyl, alkenyl, alkynyl, cycloalkyl, aryl, heteroaryl, and heterocyclyl groups are each optionally substituted with one or more (e.g., 1 to the maximum number of hydrogen atoms attached to the alkyl, alkenyl, alkynyl, aryl, heteroaryl, cycloalkyl, or heterocyclyl group, e.g., up to 1, 2, 3, 4, 5, 6, 7, 8, 9, or 10, e.g., between 1 and 5, 1 and 4, or 1 and 3, or 1 or 2) independently selected R 30 ; R 8In each case, it is selected from the group consisting of alkyl, alkenyl, alkynyl, aryl, heteroaryl, cycloalkyl, heterocyclyl, halogen, -CN, azide, -NO 2 -OR 11 -N(R 12 )(R 13 )、-N(R 11 )(OR 11 )、-S(O) 0-2 R 11 、-S(O) 1-2 OR 11 、-OS(O) 1-2 R 11 、-OS(O) 1-2 OR 11 、-S(O) 1-2 N(R 12 )(R 13 )、-OS(O) 1-2 N(R 12 )(R 13 )、-N(R 11 )S(O) 1-2 R 11 、-NR 11 S(O) 1-2 OR 11 、-NR 11 S(O) 1-2 N(R 12 )(R 13 )、-C(=X)R 11 、-C(=X)XR 11 、-XC(=X)R 11 and -XC(=X)XR 11 and is selected from the group consisting of, wherein the alkyl, alkenyl, alkynyl, aryl, heteroaryl, cycloalkyl and heterocyclyl groups are each optionally substituted with one or more (e.g., 1 to the maximum number of hydrogen atoms bonded to the alkyl, alkenyl, alkynyl, aryl, heteroaryl, cycloalkyl or heterocyclyl group, e.g., 1, 2, 3, 4, 5, 6, 7, 8, 9 or 10, e.g., between 1 and 5, 1 and 4 or 1 and 3, or 1 or 2) independently selected R 30 ; R 9 is alkyl, alkenyl, alkynyl, aryl, heteroaryl, cycloalkyl, heterocyclyl, halogen, -CN, azide, -NO2 , -OR 11 , -N(R 12 )(R 13 ), -S(O) 0-2 R 11 , -S(O) 1-2 OR 11 , -OS(O) 1-2 R 11 , -OS(O) 1-2 OR 11 , -S(O) 1-2 , -S(O) 12 N(R 13 )(R 1-2 ), -OS(O) 12 N(R 13 )(R 11 ), -N(R 1-2 )S(O) 11 R 11 , -NR 1-2 S(O) 11 OR 11 S(O) 1-2 , -NR 12 S(O) 13 N(R 11 )(R 11 ), -C(=X)R 11 , -C(=X)XR 11 , -XC(=X)R 30 and -XC(=X)XR 9 are independently selected from the group consisting of, wherein said alkyl, alkenyl, alkynyl, aryl, heteroaryl, cycloalkyl and heterocyclyl groups are each optionally, one or more (e.g., 1 to the maximum number of hydrogen atoms bonded to the alkyl, alkenyl, alkynyl, aryl, heteroaryl, cycloalkyl or heterocyclyl group, e.g., 1, 2, 3, 4, 5, 6, 7, 8, 9 or 10, e.g., between 1 and 5, 1 and 4 or 1 and 3, or 1 or 2) independently selected R X is independently selected from O, S and N(R 14 ); R 11In each case, it is selected from the group consisting of -H, alkyl, alkenyl, alkynyl, cycloalkyl, aryl, heteroaryl and heterocyclyl, wherein the alkyl, alkenyl, alkynyl, cycloalkyl, aryl, heteroaryl and heterocyclyl groups are each optionally substituted with one or more (e.g., 1 to the maximum number of hydrogen atoms bonded to the alkyl, alkenyl, alkynyl, cycloalkyl, aryl, heteroaryl or heterocyclyl group, e.g., up to 1, 2, 3, 4, 5, 6, 7, 8, 9 or 10, e.g., between 1 and 5, 1 and 4 or 1 and 3, or 1 or 2) independently selected R 30 and is substituted with; R 12 and R 13 in each case are independently selected from the group consisting of -H, alkyl, alkenyl, alkynyl, cycloalkyl, aryl, heteroaryl and heterocyclyl, or R 12 and R 13 together with the nitrogen atom to which they are attached may form the group -N=CR 15 R 16 wherein the alkyl, alkenyl, alkynyl, cycloalkyl, aryl, heteroaryl and heterocyclyl groups are each optionally substituted with one or more (e.g., 1 to the maximum number of hydrogen atoms bonded to the alkyl, alkenyl, alkynyl, cycloalkyl, aryl, heteroaryl or heterocyclyl group, e.g., up to 1, 2, 3, 4, 5, 6, 7, 8, 9 or 10, e.g., between 1 and 5, 1 and 4 or 1 and 3, or 1 or 2) independently selected R 30 and is substituted with; R 14 is independently -H, alkyl, alkenyl, alkynyl, cycloalkyl, aryl, heteroaryl, heterocyclyl and -OR 11Selected from the group consisting of, wherein said alkyl, alkenyl, alkynyl, cycloalkyl, aryl, heteroaryl and heterocyclyl groups are each optionally substituted with one or more (e.g., 1 to the maximum number of hydrogen atoms bonded to the alkyl, alkenyl, alkynyl, cycloalkyl, aryl, heteroaryl or heterocyclyl group, e.g., up to 1, 2, 3, 4, 5, 6, 7, 8, 9 or 10, e.g., between 1 and 5, 1 and 4 or 1 and 3, or 1 or 2) independently selected R 30 and is substituted with; R 15 and R 16 are independently -H, alkyl, alkenyl, alkynyl, cycloalkyl, aryl, heteroaryl, heterocyclyl and -NH y R 20 2-y selected from the group consisting of, or R 15 and R 16 together with the atom to which they are attached may optionally form a ring substituted with one or more (e.g., 1 to the maximum number of hydrogen atoms bonded to the ring, e.g., up to 1, 2, 3, 4, 5, 6, 7, 8, 9 or 10, e.g., between 1 and 5, 1 and 4 or 1 and 3, or 1 or 2) independently selected R 30 wherein said alkyl, alkenyl, alkynyl, cycloalkyl, aryl, heteroaryl and heterocyclyl groups are each optionally substituted with one or more (e.g., 1 to the maximum number of hydrogen atoms bonded to the alkyl, alkenyl, alkynyl, cycloalkyl, aryl, heteroaryl or heterocyclyl group, e.g., up to 1, 2, 3, 4, 5, 6, 7, 8, 9 or 10, e.g., between 1 and 5, 1 and 4 or 1 and 3, or 1 or 2) independently selected R 30 and is substituted with; y is an integer from 0 to 2; R 20is selected from the group consisting of alkyl, alkenyl, alkynyl, cycloalkyl, aryl, heteroaryl and heterocyclyl, wherein the alkyl, alkenyl, alkynyl, cycloalkyl, aryl, heteroaryl and heterocyclyl groups are each optionally, one or more (e.g., 1 to the maximum number of hydrogen atoms bonded to the alkyl, alkenyl, alkynyl, cycloalkyl, aryl, heteroaryl or heterocyclyl group, e.g., 1, 2, 3, 4, 5, 6, 7, 8, 9 or 10, e.g., between 1 and 5, 1 and 4 or 1 and 3, or 1 or 2) independently selected R 30 is substituted with; R 30 is a first level substituent, and in each case, independently, alkyl, alkenyl, alkynyl, aryl, heteroaryl, cycloalkyl, heterocyclyl, halogen, -CN, azide, -NO 2 、-OR 71 、-N(R 72 )(R 73 )、-S(O) 0-2 R 71 、-S(O) 1-2 OR 71 、-OS(O) 1-2 R 71 、-OS(O) 1-2 OR 71 、-S(O) 1-2 N(R 72 )(R 73 )、-OS(O) 1-2 N(R 72 )(R 73 )、-N(R 71 )S(O) 1-2 R 71 、-NR 71 S(O) 1-2 OR 71 、-NR 71 S(O) 1-2 N(R 72 )(R 73 )、-C(=X 1 )R 71 、-C(=X 1 )X 1 R 71 、-X 1 C(=X 1 )R 71and -X 1 C(=X 1 )X 1 R 71 selected from the group consisting of, and / or any two Rs attached to the same carbon atom of a cycloalkyl or heterocyclyl group 30 may together form =X 1 , wherein the alkyl, alkenyl, alkynyl, aryl, heteroaryl, cycloalkyl and heterocyclyl groups, which are first-level substituents, each may optionally be substituted by one or more (e.g., 1 to the maximum number of hydrogen atoms attached to the alkyl, alkenyl, alkynyl, aryl, heteroaryl, cycloalkyl or heterocyclyl group that is the first-level substituent, e.g., 1, 2, 3, 4, 5, 6, 7, 8, 9 or 10, e.g., between 1 and 5, 1 and 4 or 1 and 3, or 1 or 2) second-level substituents, and the second-level substituents are in each case independently C 1-6 alkyl, C 2-6 alkenyl, C 2-6 alkynyl, 3- to 14-membered aryl, 3- to 14-membered heteroaryl, 3- to 14-membered cycloalkyl, 3- to 14-membered heterocyclyl, halogen, -CF 3 , -CN, azide, -NO 2 , -OR 81 , -N(R 82 )(R 83 ), -S(O) 0-2 R 81 , -S(O) 1-2 OR 81 , -OS(O) 1-2 R 81 , -OS(O) 1-2 OR 81 , -S(O) 1-2 N(R 82 )(R 83 ), -OS(O) 1-2 N(R 82 )(R 83 ), -N(R 81 )S(O) 1-2 R 81 , -NR 81 S(O) 1-2 OR 81 , -NR 81 S(O)1-2 N(R 82 )(R 83 )、 -C(=X 2 )R 81 、 -C(=X 2 )X 2 R 81 、 -X 2 C(=X 2 )R 81 and -X 2 C(=X 2 )X 2 R 81 selected from the group consisting of, and / or any two second-level substituents bonded to the same carbon atom of a cycloalkyl or heterocyclyl group that is a first-level substituent may together form =X 2 , where the C 1-6 alkyl, C 2-6 alkenyl, C 2-6 alkynyl, 3- to 14-membered aryl, 3- to 14-membered heteroaryl, 3- to 14-membered cycloalkyl, and 3- to 14-membered heterocyclyl groups are each optionally substituted with one or more (e.g., 1 to the maximum number of hydrogen atoms bonded to the C 1-6 alkyl, C 2-6 alkenyl, C 2-6 alkynyl, 3- to 14-membered aryl, 3- to 14-membered heteroaryl, 3- to 14-membered cycloalkyl, or 3- to 14-membered heterocyclyl group that is a second-level substituent, e.g., 1, 2, 3, 4, 5, 6, 7, 8, 9, or 10, e.g., between 1 and 5, 1 and 4, or 1 and 3, or 1 or 2) third-level substituents, and the third-level substituents are in each case independently C 1-3 alkyl, halogen, -CF 3 , -CN, azide, -NO 2 , -OH, -O(C 1-3 alkyl), -OCF 3 , -S(C 1-3 alkyl), -NH 2 , -NH(C 1-3 alkyl), -N(C 1-3 alkyl) 2 , -NHS(O) 2 (C 1-3 alkyl), -S(O) 2 NH2-z (C 1-3 Alkyl) z , -C(=O)OH, -C(=O)O(C 1-3 alkyl), -C(=O)NH 2-z (C 1-3 Alkyl) z , -NHC(=O)(C 1-3 alkyl), -NHC(=NH)NH z-2 (C 1-3 Alkyl) z and -N(C 1-3 Alkyl)C(=NH)NH 2-z (C 1-3 Alkyl) z where z is 0, 1 or 2; 1-3 Alkyl is methyl, ethyl, propyl or isopropyl, and / or any two third level substituents attached to the same carbon atom of a 3- to 14-membered cycloalkyl or heterocyclyl group that is a second level substituent are taken together to be =O, =S, =NH or =N(C 1-3 alkyl); R 71 , R 72 and R 73 are independently -H, C 1-6 Alkyl, C 2-6 Alkenyl, C 2-6 alkynyl, 3- to 7-membered cycloalkyl, 5- or 6-membered aryl, 5- or 6-membered heteroaryl, and 3- to 7-membered heterocyclyl, wherein said C 1-6 Alkyl, C 2-6 Alkenyl, C 2-6 The alkynyl, 3- to 7-membered cycloalkyl, 5- or 6-membered aryl, 5- or 6-membered heteroaryl and 3- to 7-membered heterocyclyl groups are each optionally selected from the group consisting of C 1-3 Alkyl, halogen, -CF 3 , -CN, azide, -NO 2 , -OH, -O(C 1-3 alkyl), -OCF 3 , =O, -S(C 1-3 alkyl), -NH 2 , -NH(C 1-3 alkyl), -N(C1-3 alkyl) 2 -NHS(O) 2 (C 1-3 alkyl), -S(O) 2 NH 2-z (C 1-3 alkyl) z -C(=O)(C 1-3 alkyl), -C(=O)OH, -C(=O)O(C 1-3 alkyl), -C(=O)NH 2-z (C 1-3 alkyl) z -NHC(=O)(C 1-3 alkyl), -NHC(=NH)NH z-2 (C 1-3 alkyl) z and -N(C 1-3 alkyl)C(=NH)NH 2-z (C 1-3 alkyl) z (z is 0, 1 or 2, and C 1-3 alkyl is methyl, ethyl, propyl or isopropyl) and is substituted with one, two or three substituents selected from the group consisting of; R 81 , R 82 and R 83 are independently -H, C 1-4 alkyl, C 2-4 alkenyl, C 2-4 alkynyl, 3-6 membered cycloalkyl, 5- or 6-membered aryl, 5- or 6-membered heteroaryl and 3-6 membered heterocyclyl, where the C 1-4 alkyl, C 2-4 alkenyl, C 2-4 alkynyl, 3-6 membered cycloalkyl, 5- or 6-membered aryl, 5- or 6-membered heteroaryl and 3-6 membered heterocyclyl groups are each optionally C 1-3 alkyl, halogen, -CF 3 , -CN, azide, -NO 2 , -OH, -O(C 1-3 alkyl), -OCF 3 , =O, -S(C 1-3 alkyl), -NH 2 , -NH(C 1-3(alkyl), -N(C 1-3 (alkyl) 2 , -NHS(O) 2 (C 1-3 (alkyl), -S(O) 2 NH 2-z (C 1-3 (alkyl) z , -C(=O)(C 1-3 (alkyl), -C(=O)OH, -C(=O)O(C 1-3 (alkyl), -C(=O)NH 2-z (C 1-3 (alkyl) z , -NHC(=O)(C 1-3 (alkyl), -NHC(=NH)NH z-2 (C 1-3 (alkyl) z and -N(C 1-3 (alkyl)C(=NH)NH 2-z (C 1-3 (alkyl) z (z is 0, 1 or 2, and C 1-3 (alkyl) is selected from the group consisting of methyl, ethyl, propyl or isopropyl) and is substituted with one, two or three substituents selected from the group; X 1 and X 2 are independently O, S and N(R 84 )(R 84 is -H or C 1-3 (alkyl)) selected from; and solvates, salts, complexes, polymorphs, crystal forms, racemic mixtures, diastereomers, enantiomers, tautomers, isotopically labeled forms, prodrugs and combinations thereof.

[0113] In one embodiment, the spiroquinoxaline derivative has the following general formula (C-II): [Chemical formula] [wherein, R 1 ~R 5, E, L, and G are synonymous with those above or below, and the monocyclic ring A, which may be optionally substituted, has 3 to 8 members, preferably 4, 5, 6, or 7 members, more preferably 6 or 7 members. In one embodiment of the spiroquinoxaline derivative of formula (C-II), ring A itself is unsaturated (i.e., 3 to 10 members of ring A form 1, 2, or 3 (preferably 1 or 2, most preferably 1) double bonds within the ring), but not aromatic. In another embodiment of the spiroquinoxaline derivative of formula (C-II), ring A is saturated (i.e., ring A itself has no unsaturation within the ring); provided that when ring A is substituted with one or more (e.g., 1 to the maximum number of hydrogen atoms bonded to ring A, e.g., up to 1, 2, 3, 4, 5, 6, 7, 8, 9, or 10, e.g., between 1 and 5, 1 and 4, or 1 and 3, or 1 or 2) R 9 , R 9 may be unsaturated (i.e., may contain double and / or triple bonds and / or one or more (e.g., 1, 2, or 3) aromatic rings). In any of the above embodiments of the spiroquinoxaline derivative of formula (C-II), ring A is optionally substituted with one or more (e.g., 1 to the maximum number of hydrogen atoms bonded to ring A, e.g., up to 1, 2, 3, 4, 5, 6, 7, 8, 9, or 10, e.g., between 1 and 5, 1 and 4, or 1 and 3, or 1 or 2) independently selected R 9 and may be selected from the group consisting of cyclohexylene, cycloheptylene, cyclopropylene, cyclobutylene, cyclopentylene, cyclooctylene, cyclohexenylene, cycloheptenylene, cyclopentenylene, cyclooctenylene, and their positional isomers. In one embodiment of the spiroquinoxaline derivative of formula (C-II), ring A is optionally substituted with one or more (e.g., 1 to the maximum number of hydrogen atoms bonded to ring A, e.g., up to 1, 2, 3, 4, 5, 6, 7, 8, 9, or 10, e.g., between 1 and 5, 1 and 4, or 1 and 3, or 1 or 2) independently selected R 9Selected from the group consisting of cyclohexylene, cycloheptylene, cyclopropylene, cyclobutylene, cyclopentylene and cyclooctylene, which is substituted by 9 Selected from the group consisting of cyclohexylene, cycloheptylene, cyclopentylene and cyclooctylene, which is substituted by

[0114] In any of the above embodiments of the spiroquinoxaline derivative of formula (C-II), ring A may be unsubstituted.

[0115] In any of the above embodiments of the spiroquinoxaline derivative of formula (C-II) where ring A is substituted with one or more (e.g., 1 to the maximum number of hydrogen atoms bonded to ring A, e.g., up to 1, 2, 3, 4, 5, 6, 7, 8, 9 or 10, e.g., between 1 and 5, 1 and 4 or 1 and 3, or 1 or 2) independently selected R 9 In any of the above embodiments of the spiroquinoxaline derivative of formula (C-II) that is substituted by 9 such R 1-6 are each independently C 2-6 alkyl, C 2-6 alkenyl, C 11 alkynyl, 5- or 6-membered aryl, 5- or 6-membered heteroaryl, 3- to 7-membered cycloalkyl, 3- to 7-membered heterocyclyl, halogen, -CN, -OR 12 ), -N(R 13 )(R 0-2 ), -S(O) 11 R 1-2 ), -S(O) 12 N(R 13 )(R 11 ), -N(R 1-2 ), -NR 11 S(O) 11 ), -NR 1-2 S(O) 12 N(R 13 )(R 11 ), -C(=X)R11 、 -XC(=X)R 11 and -XC(=X)XR 11 which may be selected from the group consisting of, wherein the C 1-6 alkyl, C 2-6 alkenyl, C 2-6 alkynyl, 5- or 6-membered aryl, 5- or 6-membered heteroaryl, 3- to 7-membered cycloalkyl and 3- to 7-membered heterocyclyl group may each, optionally, have one or more (e.g., 1 to the C 1-6 alkyl, C 2-6 alkenyl, C 2-6 alkynyl, 5- or 6-membered aryl, 5- or 6-membered heteroaryl, 3- to 7-membered cycloalkyl or 3- to 7-membered heterocyclyl group) of independently selected R 30 substituents, and / or any two R 9 bonded to the same carbon atom of ring A may together form =X. In any of the above embodiments of the spiroquinoxaline derivative of formula (C-II), R 9 is each independently C 1-4 alkyl, C 2-4 alkenyl, C 2-4 alkynyl, 6-membered aryl, 5- or 6-membered heteroaryl, 3, 5, 6 or 7-membered cycloalkyl, 3, 5, 6 or 7-membered heterocyclyl, halogen, -CN, -OR 11 , -N(R 12 )(R 13 ), -S(O) 0-2 R 11 , -S(O) 1-2 N(R 12 )(R 13 ), -N(R 11 )S(O) 1-2 R 11 , -NR 11 S(O) 1-2 N(R 12 )(R 13 ), -C(=O)R 11 , -C(=O)OR 11 , -C(=O)SR 11 , -C(=O)N(R14 )(R 11 ), -C(=S)OR 11 , -N(R 14 )C(=O)R 11 , -OC(=O)R 11 , -OC(=S)R 11 , -N(R 14 )C(=O)N(R 14 )(R 11 ) and -N(R 14 )C(=N(R 14 ))N(R 14 )(R 11 ), wherein the C 1-4 Alkyl, C 2-4 Alkenyl, C 2-4 The alkynyl, 6-membered aryl, 5- or 6-membered heteroaryl, 3-, 5-, 6- or 7-membered cycloalkyl, and 3-, 5-, 6- or 7-membered heterocyclyl groups each optionally contain one, two or three independently selected R 30 and / or any two R bonded to the same carbon atom of ring A 9 may be taken together to form =O or =S. In one embodiment, R 9 are each independently: C 1-4 Alkyl; -OH, -O(C 1-3 alkyl), -NH 2-z (CH 3 ) z , morpholinyl (e.g., 4-morpholinyl), piperazinyl (e.g., 1-piperazinyl), and N-methylpiperazinyl (e.g., 4-methylpiperazin-1-yl), 1-4 Alkyl;-CF 3 , -CH 2 CF 3 , -CH 2 CHF 2 or -CH 2 CH 2 C substituted with 1, 2 or 3 halogens such as F (preferably F); 1-4 Alkyl;-OCF 3 , -OCH 2 CF 3 , -OCH2 CHF 2 or -OCH 2 CH 2 C substituted with -O (C substituted with 1, 2, or 3 halogens (preferably F), such as -O(1, 2, or 3 halogen (preferably F)-substituted C 1-4 alkyl); cyclopropyl; 4-morpholinyl; homomorpholinyl; 4-piperidinyl; homopiperidinyl; 4-piperazinyl; homopiperazinyl; 4-methyl-piperazin-1-yl; N-methyl-homopiperazinyl; halogen; -CN; -OH; =O; -O(optionally -NH 2-z (CH 3 ) z substituted C 1-3 alkyl); -NH 2 ; -NH(C 1-3 alkyl); -N(C 1-3 alkyl) 2 ; -S(C 1-3 alkyl); -S(O) 2 (optionally -NH 2-z (CH 3 ) z substituted C 1-3 alkyl); -S(O) 2 NH 2-z (C 1-3 alkyl) z ; -NHS(O) 2 (optionally -NH 2-z (CH 3 ) z substituted C 1-3 alkyl); -C(=O)(optionally -NH 2-z (CH 3 ) z substituted C 1-3 alkyl); -C(=O)OH; -C(=O)O(C 1-3 alkyl); -C(=O)NH 2-z (C 1-3 alkyl) z ; -NHC(=O)(optionally -NH 2-z (CH 3 ) z substituted C 1-3 alkyl); -NHC(=O)NH 2-z (CH 3 ) z;-NHC(=NH)NH z-2 (C 1-3 alkyl) z ; and -N(C 1-3 alkyl)C(=NH)NH 2-z (C 1-3 alkyl) z (z is 0, 1 or 2, and C 1-3 alkyl is methyl, ethyl, propyl or isopropyl) is selected from the group consisting of. In one embodiment, R 9 is, independently of each other, methyl; ethyl; isopropyl; tert-butyl; cyclopropyl; -(CH 2 ) d -NH 2-z (CH 3 ) z ;-O(CH 2 ) d -NH 2-z (CH 3 ) z ;-(CH 2 ) d -O(CH 3 );-CF 3 ;-CH 2 CF 3 ;-CH 2 CHF 2 ;-CH 2 CH 2 F;-(CH 2 ) d -(4-morpholinyl);-(CH 2 ) d -(1-piperazinyl);-(CH 2 ) d -(4-methylpiperazin-1-yl); 4-morpholinyl; 4-piperazinyl; 4-methyl-piperazin-1-yl; halogen (especially, -F, -Cl, -Br);-NHC(=O) (optionally -NH 2-z (CH 3 ) z substituted C 1-3 alkyl);-NHC(=O)NH 2-z (CH 3 ) z ;-NHS(O) 2 (optionally -NH 2-z (CH 3 ) zC replaced by 1-3 alkyl); -C(=O)CH 3 ; -C(=O)CH 2 NH 2-z (CH 3 ) z ; -C(=O)NH 2-z (C 1-3 alkyl) z ; -S(O) 2 (C 1-3 alkyl); -S(O) 2 (CH 2 ) d NH 2-z (CH 3 ) z ; -OH; and -O(C 1-3 alkyl) (z is 0, 1 or 2; d is 1, 2 or 3; C 1-3 alkyl is methyl, ethyl, propyl or isopropyl). In one embodiment, R 9 is, independently of each other, methyl; ethyl; isopropyl; cyclopropyl; -(CH 2 ) d -NH 2-z (CH 3 ) z ; -(CH 2 ) d -O(CH 3 ); -CF 3 ; -CH 2 CF 3 ; -CH 2 CHF 2 ; -CH 2 CH 2 F; -NH 2 ; -NH(C 1-3 alkyl); -N(C 1-3 alkyl) 2 ; halogen (especially, -F, -Cl, -Br); -C(=O)CH 3 ; -C(=O)CH 2 NH 2-z (CH 3 ) z ; -C(=O)NH 2-z (C 1-3 alkyl) z ; -S(O) 2 (C 1-3-S(O)(alkyl); 2 (CH 2 ) d NH 2-z (CH 3 ) z ;-OH; and -O(C 1-3 alkyl) (z is 0, 1, or 2; d is 1, 2, or 3; C 1-3 alkyl is methyl, ethyl, propyl, or isopropyl) and is selected from the group consisting of. In one embodiment, when R 9 replaces the hydrogen atom bonded to the ring carbon atom of ring A, each is independently methyl; ethyl; isopropyl; cyclopropyl; -(CH 2 ) d -NH 2-z (CH 3 ) z ;-(CH 2 ) d -O(CH 3 );-CF 3 ;-CH 2 CF 3 ;-CH 2 CHF 2 ;-CH 2 CH 2 F; halogen (especially -F, -Cl, -Br);-C(=O)CH 3 ;-C(=O)CH 2 NH 2-z (CH 3 ) z ;-C(=O)NH 2-z (C 1-3 alkyl) z ;-S(O) 2 (C 1-3 alkyl);-S(O) 2 (CH 2 ) d NH 2-z (CH 3 ) z ;-OH; and -O(C 1-3 alkyl) (z is 0, 1, or 2; d is 1, 2, or 3; C 1-3The alkyl is selected from the group consisting of methyl, ethyl, propyl or isopropyl. In one embodiment, the ring carbon atoms of ring A are unsubstituted or R which replaces the hydrogen atom bonded to the ring carbon atom 9 is, independently of each other, C 1-4 alkyl (especially methyl), -N(R 12 )(R 13 )(especially NH 2 ) and -N(R 14 )C( =O)R 11 (especially NHC(O)CH 3 ) and is selected from the group consisting of. In one embodiment, the ring carbon atoms of ring A are unsubstituted or one ring carbon atom of ring A is NH 2 or CH 3 and one R 9 , or two R 3 which is CH 9 are substituted.

[0116] In any of the above embodiments of the spiroquinoxaline derivative of formula (C-II) in which ring A is substituted with one or more (for example, 1 to the maximum number of hydrogen atoms bonded to ring A, for example, 1, 2, 3, 4, 5, 6, 7, 8, 9 or 10, for example, between 1 and 5, between 1 and 4 or between 1 and 3, or 1 or 2) independently selected R 9 , preferably, R 9 is bonded to ring A at the 3-position when ring A is 4-membered, at the 3- or 4-position when ring A is 5-membered, at the 3, 4 or 5-position when ring A is 6-membered, at the 3, 4, 5 or 6-position when ring A is 7-membered, or at the 3, 4, 5, 6 or 7-position when ring A is 8-membered. In one embodiment, especially when ring A is substituted with one or two independently selected R 9 , R 9 is bonded to ring A at the 3-position when ring A is 4- or 5-membered, at the 3- or 4-position (preferably the 4-position) when ring A is 6- or 7-membered, and at the 3, 4 or 5-position when ring A is 8-membered.

[0117] In one embodiment, the spiroquinoxaline derivative has the following general formula (C-III): [Chemical formula] [In the formula, R 1 ~R 5 , rings A, E and G are synonymous with the above (especially for formulas (C-I) and (C-II)) or the following, L is C 1-6 alkylene, C 2-6 alkenylene, C 2-6 alkynylene, -(CH 2 ) a -cyclopropylene-(CH 2 ) b -(wherein a and b are each independently selected from integers between 0 and 3) and -(CH 2 ) m -[Y-(CH 2 ) n ) o -(wherein m is 1, 2 or 3, n is 0, 1 or 2, o is 1, 2 or 3, when n is 0, o is 1, and Y is independently O, S and -N(R 7’ )-(R 7’ is selected from the group consisting of -H, C 1-6 alkyl, C 2-6 alkenyl, C 2-6 alkynyl, 3- to 7-membered cycloalkyl, 5- or 6-membered aryl, 5- or 6-membered heteroaryl, 3- to 7-membered heterocyclyl, -OR 11 and -NHR 20 )-selected from the group consisting of), where the C 1-6 alkylene, C 2-6 alkenylene, C 2-6 alkynylene, 1,1-cyclopropylene, -(CH 2 ) m -, -(CH 2 ) n -, C 1-6 alkyl, C 2-6 alkenyl, C 2-6 alkynyl, 3- to 7-membered cycloalkyl, 5- or 6-membered aryl, 5- or 6-membered heteroaryl and 3- to 7-membered heterocyclyl groups each may optionally have one or more (for example, 1 to the C 1-6Alkylene, C 2-6 Alkenylene, C 2-6 Alkynylene, 1,1 - cyclopropylene, -(CH 2 ) m -, -(CH 2 ) n -, C 1-6 Alkyl, C 2-6 Alkenyl, C 2-6 Alkynyl, a 3 - to 7 - membered cycloalkyl, a 5 - or 6 - membered aryl, a 5 - or 6 - membered heteroaryl or a 3 - to 7 - membered heterocyclyl group, the maximum number of hydrogen atoms bonded thereto being, for example, up to 1, 2, 3, 4, 5, 6, 7, 8, 9 or 10, for example, between 1 - 5, 1 - 4 or 1 - 3, or 1 or 2), of independently selected R 30 substituted with] having. In one embodiment of the spiroquinoxaline derivative of formula (C - III), R 1 ~R 5 , ring A, E and G are as defined above (in particular for formulas (C - I) and (C - II)) or have the same meaning as below, and L is C 1-4 Alkylene, C 2-4 Alkenylene, C 2-4 Alkynylene, -(CH 2 ) a - 1,1 - cyclopropylene-(CH 2 ) b -(wherein a and b are each independently selected from 0, 1 and 2) and -(CH 2 ) m -[Y-(CH 2 ) n o -(wherein m is 1, 2 or 3, n is 0, 1 or 2, o is 1, 2 or 3, when n is 0, o is 1, and Y is independently selected from O, S and - N(R 7’ )-(R 7’ is selected from the group consisting of - H, C 1-3 alkyl, a 3, 5, 6 or 7 - membered cycloalkyl, a 6 - membered aryl, a 5 or 6 - membered heteroaryl, a 3, 5, 6 or 7 - membered heterocyclyl, - O(C 1-3 alkyl) and - NHR 20 selected from the group consisting of) selected from the group consisting of), where the C 1-4 ​Alkylene, C 2-4 Alkenylene, C 2-4 Alkynylene, 1,1 - cyclopropylene, -(CH 2 ) m -, -(CH 2 ) n -, C 1-3 Alkyl, 3, 5, 6 or 7 - membered cycloalkyl, 6 - membered aryl, 5 or 6 - membered heteroaryl and 3, 5, 6 or 7 - membered heterocyclyl groups are each, optionally, substituted with one, two or three independently selected R 30 . In one embodiment of the spiroquinoxaline derivative of formula (C - III), R 1 ~R 5 , ring A, E and G are as defined above (especially for formula (C - I) and (C - II)) or synonymous with the following, and L is C 1-3 Alkylene, -(CH 2 ) a - 1,1 - cyclopropylene-(CH 2 ) b -(wherein a and b are each independently selected from 0 and 1) and -(CH 2 ) m -[Y-(CH 2 ) n o -(wherein m is 1 o...

Claims

1. The following general formula (I): 【Chemical Formula 60】 [wherein, E is -N(R ６ )-; L is -CH ２ -. G is, optionally, phenyl substituted with one or two groups independently selected from halogen and methyl; Ring A is tetrahydropyranylene spiro-bonded at the 4-position; R １ is H; R ２ and R ５ are each independently selected from the group consisting of -H, halogen, and -OCH ３ ; R ３ and R ４ are each independently selected from the group consisting of -H, halogen, and methyl, or; R ３ and R ４ may, together with the atoms to which they are attached, form an -O-CF ２ -O-ring; R ６ is H; provided that, when Ring A has the following formula: 【Chemical Formula 61】 where R ２ and R ５ are both H, and (i) R ３ and R ４ When both are H, G is not any of 3-methylphenyl, 3-methoxyphenyl, 4-chlorophenyl or 4-fluorophenyl; (ii) R ３ and R ４ when both are methyl, G is not 4-fluorophenyl A spiroquinoxaline derivative, and a compound selected from the group consisting of its solvate, salt, racemic mixture, diastereomer, enantiomer, and tautomer.

2. The compound according to claim 1, wherein G is selected from the group consisting of unsubstituted phenyl, fluorophenyl, chlorophenyl, methylphenyl, difluorophenyl, dichlorophenyl, chlorofluorophenyl, and dimethylphenyl.

3. The compound according to claim 1 or 2, wherein G is selected from the group consisting of unsubstituted phenyl, 3-fluorophenyl, 2-chlorophenyl, 3-chlorophenyl, 4-chlorophenyl, 2- or 3-methylphenyl, 2,4- or 2,6-difluorophenyl, 2,4- or 3,4-dichlorophenyl, 4-chloro-2-fluorophenyl, and 3,5-dimethylphenyl.

4. R ２ 、 R ３ 、 R ４ and R ５ is independently selected from the group consisting of -H and halogen, the compound according to any one of claims 1 to 3.

5. R ２ , R ３ , R ４ and R ５ is -H, the compound according to any one of claims 1 to 4.

6. (i) R ２ ~ R ５ is each -H; (ii) R ２ and R ５ are each -H, and R ３ and R ４ are both F, Cl or methyl; or (iii) R ２ and R ５ are each -H, and R ３ and R ４ together with the atom to which they are attached form a -O-CF ２ -O-ring, a compound according to any one of claims 1 to 3.

7. The compound according to any one of claims 1 to 6, which is the following formula: 【Chemical Formula 62】 and a compound selected from the group consisting of its solvate, salt, racemic mixture, diastereomer, enantiomer, and tautomer.

8. The compound according to any one of claims 1 to 7, which is the following formula: 【Chemical Formula 63】 and a compound selected from the group consisting of its solvate, salt, racemic mixture, diastereomer, enantiomer, and tautomer.

9. The compound according to any one of claims 1 to 7, which is the following formula: 【Chemical Formula 64】 and a compound selected from the group consisting of its solvate, salt, racemic mixture, diastereomer, enantiomer, and tautomer.

10. A pharmaceutical composition comprising a pharmaceutically acceptable excipient and a compound according to any one of claims 1 to 9.

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